USE OF THE ANTIBODY I-3859 FOR THE DETECTION AND DIAGNOSIS OF CANCER (Fri, 20 Jun 2014)
<p id="p-0001" num="0000">The present invention relates to the use of a novel, isolated anti-CXCR4 antibody in the diagnosis of cancer. In particular, methods for diagnosing and/or prognosing an oncogenic disorder associated with CXCR4 expression, are disclosed.</p>
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NOVEL ANTI-cMET ANTIBODY (Fri, 25 Apr 2014)
<p id="p-0001" num="0000">The invention relates to a novel antibody capable of binding specifically to the human c-Met receptor and/or capable of specifically inhibiting the tyrosine kinase activity of said receptor both in a ligand-dependent and in a ligand-independent manner, with an improved antagonistic activity, said antibody comprising a modified hinge region.</p> <p id="p-0002" num="0000">The invention also relates to a composition comprising such an antibody antagonist to c-Met and its use as a medicament for treating cancer.</p>
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NOVEL ANTI-CXCR4 ANTIBODIES AND THEIR USE FOR THE TREATMENT OF CANCER (Fri, 21 Feb 2014)
<p id="p-0001" num="0000">The present invention relates to a novel isolated antibody, or the derived compounds or functional fragments of same, capable of binding to CXCR4 but also of inducing conformational changed of the CXCR4 homodimers and/or heterodimers.</p> <p id="p-0002" num="0000">More particularly, the present invention relates to the 414H5 and 515H7 antibodies, specific to the CXCR4 protein, as well as their use for the treatment of cancer. Pharmaceutical compositions composed of such antibodies and a process for the selection of such antibodies are also covered.</p>
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TRI - AND TETRACYCLIC PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS AS ANTINEOPLASTIC AGENT (Fri, 31 Jan 2014)
<p id="p-0001" num="0000">The present invention relates to compounds of following general formula (I): and to the pharmaceutically acceptable salts of same, the tautomers of same, the stereoisomers or mixture of stereoisomers in any proportions of same, such as a mixture of enantiomers, notably a racemic mixture, as well as to methods for preparing same and uses of same, notably as an antineoplastic agent.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.46mm" wi="52.66mm" file="US20140031362A1-20140130-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE FOR TREATING A CANCER OVEREXPRESSING TRK (Fri, 31 Jan 2014)
The present invention relates to a compound of following formula (I) or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture, as well as pharmaceutical composition comprising such a compound, for use in the treatment of a cancer associated with the overexpression of at least one Trk protein.
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DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE FOR TREATING PAIN (Fri, 31 Jan 2014)
The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; for use in the treatment of pain.
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Vinyl quinuclidine useful as a synthesis intermediate in the preparation of (R)-mequitazine (Fri, 08 Nov 2013)
<p id="p-0001" num="0000">The present invention relates to the use of the vinyl quinuclidine enantiomer (R) of the following formula 2 as a synthesis intermediate in the preparation of (R)-mequitazine.</p>
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DIARYLPYRIDAZINONE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF FOR THE TREATMENT OF HUMANS (Fri, 11 Oct 2013)
<p id="p-0001" num="0000">The present invention relates to diarylpyridazinone derivatives that block the potassium Kv channels (specifically the Kv1.5, Kv4.3, and Kv11.1 channels) and to the use thereof for the treatment of humans. Said compounds have the general formula (I), where R<sub>1 </sub>and R<sub>2 </sub>are simultaneously or independently one or more groupings such as: halogen, such as F, Br, Cl, a straight or branched C<sub>1</sub>-C<sub>4 </sub>alkyl, hydroxy, a straight or branched C<sub>1</sub>-C<sub>4 </sub>alkoxy, arylsulfonamido, in which the aryl is optionally replaced with a straight or branched C<sub>1</sub>-C<sub>4 </sub>alkyl, or nitrile, as well as the various enantiomers and the mixtures thereof in any proportion, and the pharmaceutically acceptable salts thereof.</p>
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FLUORESCENT CYANINE-POLYAMINE DERIVATIVES AS A DIAGNOSTIC PROBE (Fri, 19 Jul 2013)
<p id="p-0001" num="0000">The invention relates to fluorescent derivatives of cyanines conjugated with a polyamine group, having formula (I), or a pharmaceutically acceptable salt thereof. The invention also relates to the method for preparing said derivatives, diagnostic compositions containing same and the use thereof as a diagnostic probe for the detection of cancer tumours, in particular in vivo.</p>
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TECHNETIUM-99m COMPLEX AS A TOOL FOR THE IN VIVO DIAGNOSIS OF CANCEROUS TUMOURS (Fri, 05 Jul 2013)
<p id="p-0001" num="0000">The invention relates to a compound having formula (I), compositions containing same and preparation methods thereof. The invention also relates to a complex of the compound having formula (I) with technetium-99m and tricine, the use of this complex as a diagnostic probe, diagnostic compositions containing same and methods for preparing the complex and compositions containing same.</p>
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DERIVATIVES OF HETEROARYLSULFONAMIDES, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPY (Fri, 05 Jul 2013)
<p id="p-0001" num="0000">The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C<sub>1</sub>-C<sub>4 </sub>alkyl, or linear or branched C<sub>1</sub>-C<sub>4 </sub>alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents —C(═O)—, or B represents CH when n=0 and D represents —CH<sub>2</sub>O— or when n=1 and D represents —O—, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C<sub>1</sub>-C<sub>4 </sub>alkyl, a linear or branched C<sub>1</sub>-C<sub>4 </sub>alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.38mm" wi="75.01mm" file="US20130172326A1-20130704-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT (Fri, 05 Jul 2013)
<p id="p-0001" num="0000">The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="46.57mm" wi="69.85mm" file="US20130172360A1-20130704-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Nitrogenated derivatives of pancratistatin (Fri, 17 May 2013)
<p id="p-0001" num="0000">The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.99mm" wi="69.85mm" file="US08697064-20140415-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Anti-cMET antibody (Fri, 03 May 2013)
<p id="p-0001" num="0000">Antibody capable of binding specifically to the human c-Met receptor and/or capable of specifically inhibiting the tyrosine kinase activity of said receptor, with an improved antagonistic activity, said antibody comprising a modified hinge region. A composition comprising such an antibody antagonist to c-Met and its use as a medicament for treating cancer.</p>
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Anti-cMET antibody (Fri, 03 May 2013)
<p id="p-0001" num="0000">Antibody capable of binding specifically to the human c-Met receptor and/or capable of specifically inhibiting the tyrosine kinase activity of said receptor, with an improved antagonistic activity, said antibody comprising a modified hinge region. A composition comprising such an antibody antagonist to c-Met and its use as a medicament for treating cancer.</p>
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DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT (Fri, 05 Apr 2013)
<p id="p-0001" num="0000">The present invention relates to a compound of following formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="46.57mm" wi="52.66mm" file="US20130085144A1-20130404-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.</p>
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USE OF THE ANTIBODY I-3859 FOR THE DETECTION AND DIAGNOSIS OF CANCER (Fri, 08 Feb 2013)
The present invention relates to the use of a novel, isolated anti-CXCR4 antibody in the diagnosis of cancer. In particular, methods for diagnosing and/or prognosing an oncogenic disorder associated with CXCR4 expression, are disclosed.
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NOVEL ANTI-CXCR4 ANTIBODY AND ITS USE FOR THE DETECTION AND DIAGNOSIS OF CANCER (Fri, 08 Feb 2013)
The present invention provides a novel, isolated anti-CXCR4 antibody for use in the diagnosis of cancer. In particular, the antibody of the invention recognizes monomeric and homodimeric CXCR4, but not heterodimeric CXCR4
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(Poly)Aminoalkylaminoalkylamide, alkyl-urea, or alkyl-sulfonamide derivatives of epipodophyllotoxin, a process for preparing them, and application thereof in therapy as anticancer agents (Fri, 09 Nov 2012)
<p id="p-0001" num="0000">The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamide, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent.</p>
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Anti-CD151 antibodies and their use in the treatment of cancer (Fri, 09 Nov 2012)
<p id="p-0001" num="0000">The present invention relates to new antibodies capable of binding specifically to the human CD151 protein, especially monoclonal antibodies of murine origin, which are chimeric and humanized, and also to the amino acid and nucleic sequences coding for those antibodies. The invention also includes use of those antibodies as medicaments for the prophylactic and/or therapeutic treatment of cancers and in diagnostic methods or kits for diseases associated with overexpression of the CD151 protein. Finally, the invention includes products and/or compositions comprising such antibodies in association with antibodies and/or anti-cancer agents or conjugated with toxins and/or radioelements and their use in the prevention and/or treatment of certain cancers.</p>
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TRI- AND TETRACYCLIC PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS AS ANTINEOPLASTIC AGENT (Fri, 19 Oct 2012)
The present invention relates to compounds of following general formula (I): and to the pharmaceutically acceptable salts of same, the tautomers of same, the stereoisomers or mixture of stereoisomers in any proportions of same, such as a mixture of enantiomers, notably a racemic mixture, as well as to methods for preparing same and uses of same, notably as an antineoplastic agent.
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Cinnamoyl-piperazine derivatives and their use as par-1 antagonists (Fri, 14 Sep 2012)
<p id="p-0001" num="0000">The present invention relates to compounds of general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="19.56mm" wi="57.74mm" file="US08513258-20130820-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">wherein:</li> <li id="ul0001-0002" num="0000">R<sub>1 </sub>represents: <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">halogen, CN or NO<sub>2</sub>;</li> </ul> </li> <li id="ul0001-0003" num="0000">R<sub>2 </sub>represents: <ul id="ul0003" list-style="none"> <li id="ul0003-0001" num="0000">hydrogen or halogen;</li> </ul> </li> <li id="ul0001-0004" num="0000">n represents: <ul id="ul0004" list-style="none"> <li id="ul0004-0001" num="0000">1 or 2;</li> </ul> </li> <li id="ul0001-0005" num="0000">R<sub>3 </sub>represents: <ul id="ul0005" list-style="none"> <li id="ul0005-0001" num="0000">phenyl substituted by one or more halogens or C<sub>1</sub>-C<sub>6 </sub>alkyls; or a cyclohexyl; <br/> as well as the therapeutically-acceptable salts or solvates thereof. </li> </ul> </li> </ul> </p> <p id="p-0003" num="0000">These compounds are useful as protease-activated receptor-1 (PAR-1) antagonists, particularly in the treatment of thrombosis.</p>
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DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT (Fri, 03 Aug 2012)
The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.
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Anti-cMet antibody and its use for the detection and the diagnosis of cancer (Fri, 15 Jun 2012)
<p id="p-0001" num="0000">The present invention relates to the field of prognosis and/or diagnosis of a proliferative disease in a patient. More particularly, the invention relates to antibodies capable of binding to the human cMet receptor, as well as the amino acid and nucleic acid sequences coding for these antibodies. The invention likewise comprises the use of said antibodies, and corresponding processes, for detecting and diagnosing pathological hyperproliterative oncogenic disorders associated with expression of cMet. In certain embodiments, the disorders are oncogenic disorders associated with increased expression of cMet polypeptide relative to normal or any other pathology connected with the overexpression of cMet. The invention finally comprises products and/or compositions or kits comprising at least such antibodies for the prognosis or diagnostic of certain cancers.</p>
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DERIVATIVES OF HETEROARYLSULFONAMIDES, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPY (Fri, 01 Jun 2012)
The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents −C(=O)-, or B represents CH when n=0 and D represents −CH2O− or when n=1 and D represents −O−, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.
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Derivatives of aryl-{4-halogeno-4-[aminomethyl]-piperidin-1-yl}-methanone, their method of preparation and their use as medicinal products (Fri, 11 May 2012)
<p id="p-0001" num="0000">The present invention concerns compounds of general formula (1) (I) wherein R1 is: —a hydrogen atom, or a halogen, —a straight or branched C<sub>1</sub>-C<sub>6 </sub>alkyl group or a C<sub>1</sub>-C<sub>3 </sub>fluoroalkyl group, —a straight or branched C<sub>1</sub>-C<sub>6 </sub>alcoxy group, a carbamyl group, N-substituted or not by one or two, straight or branched C<sub>1</sub>-C<sub>3 </sub>alkyl groups, or —a cyano group (CN) R2 is: —a hydrogen atom or a straight or branched C<sub>1</sub>-C<sub>6 </sub>alkyl group, HaI<sub>1</sub>, Hal<sub>2 </sub>and Hal<sub>3 </sub>are: —a halogen their addition salts and the hydrates of addition salts with pharmaceutically acceptable mineral acids or organic acids, and their enantiomer forms.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.45mm" wi="74.51mm" file="US08669250-20140311-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Derivatives of aminocyclobutane or aminocyclobutene, their method of preparation and their use as medical products (Fri, 03 Feb 2012)
<p id="p-0001" num="0000">The present invention concerns compounds of general formula (1), where in:—-a- is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C<sub>1</sub>-C<sub>6 </sub>alkyl group, branched or unbranched, saturated or unsaturated, substituted or unsubstituted; the groups R1 and R2 may also form a heterocycle, R3 and R3′ each independently or together are a hydrogen atom or C<sub>1</sub>-C<sub>6 </sub>alkyl group, X is an oxygen atom or a sulphur atom, and the addition salts of the compounds of general formula (1) with pharmaceutically acceptable mineral acids or organic acids.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="18.88mm" wi="54.53mm" file="US08455550-20130604-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NOVEL ANTIBODY FOR THE DIAGNOSIS AND/OR PROGNOSIS OF CANCER (Fri, 20 Jan 2012)
The present invention relates to the field of prognosis and/or diagnosis of a proliferative disease in a patient. More particularly, the invention relates to novel antibodies capable of binding specifically to the human cMet receptor, as well as the amino acid and nucleic acid sequences coding for these antibodies. The invention likewise comprises the use of said antibodies, and corresponding process, for detecting and diagnosing pathological hyperproliferative oncogenic disorders associated with expression of cMet. In certain embodiments, the disorders are oncogenic disorders associated with increased expression of cMet polypeptide relative to normal or any other pathology connected with the over expression of c Met. The invention finally comprises products and/or compositions or kits comprising at least such antibodies for the prognosis or diagnostic of certain cancers.
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NOVEL ANTIBODY FOR THE DIAGNOSIS AND/OR PROGNOSIS OF CANCER (Fri, 20 Jan 2012)
The present invention relates to the field of prognosis and/or diagnosis of a proliferative disease in a patient. More particularly, the invention relates to novel antibodies capable of binding specifically to the human cMet receptor, as well as the amino acid and nucleic acid sequences coding for these antibodies. The invention likewise comprises the use of said antibodies, and corresponding process, for detecting and diagnosing pathological hyperproliferative oncogenic disorders associated with expression of cMet. In certain embodiments, the disorders are oncogenic disorders associated with increased expression of cMet polypeptide relative to normal or any other pathology connected with the over expression of c Met. The invention finally comprises products and/or compositions or kits comprising at least such antibodies for the prognosis or diagnostic of certain cancers.</p>
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DERIVATIVES OF BENZOTHIAZINES, PREPARATION THEREOF AND APPLICATION THEREOF AS DRUGS (Fri, 30 Dec 2011)
<p id="p-0001" num="0000">The object of the present invention is benzothiazine derivatives having the capability of inhibiting 11β-HSD1 not only at an enzymatic level but also at a cell level. The compounds of the present invention are of general formula (I). Wherein notably R<sub>1 </sub>represents a hydrogen or OR1 represents an ester or an ether. R<sub>2 </sub>represents a naphthyl or a 1, 2, 3, 4-tetrahydro-naphthalene or a biphenyl or phenyl pyridine or a substituted phenyl. R<sub>3 </sub>represents a methyl or ethyl; R<sub>4 </sub>and R′<sub>4 </sub>represent a hydrogen.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.38mm" wi="69.85mm" file="US20110319326A1-20111229-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NOVEL ANTI-CMET ANTIBODY (Fri, 09 Dec 2011)
The present invention relates to a novel divalent antibody capable of binding specifically to the human c-Met receptor and/or capable of specifically inhibiting the tyrosine kinase activity of said receptor, preferably both in a ligand-dependent and in a ligand-independent manner as well as the amino acid and nucleic acid sequences coding for said antibody. More preferably said antibody comprises a modified hinge region and exhibits an improved antagonistic activity. More particularly, the antibody according to the invention is capable of inhibiting the c-Met dimerization. The invention likewise comprises the use of said antibody as a medicament for the prophylactic and/or therapeutic treatment of cancers, preferably for cancer characterized by a ligand- independent activation of c-Met,or any pathology connected with the over expression of said receptor as well as in processes or kits for diagnosis of illnesses connected with the over-expression of c-Met. The invention finally comprises products and/or compositions comprising such an antibody in combination with other antibodies and/or chemical compounds directed against other growth factors involved in tumor progression or metastasis and/or compounds and/or anti-cancer agents or agents conjugated with toxins and their use for the prevention and/or the treatment of certain cancers.
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NOVEL ANTI-CMET ANTIBODY (Fri, 09 Dec 2011)
The present invention relates to a novel divalent antibody capable of binding specifically to the human c-Met receptor and/or capable of specifically inhibiting the tyrosine kinase activity of said receptor, preferably both in a ligand-dependent and in a ligand-independent manner as well as the amino acid and nucleic acid sequences coding for said antibody. More preferably said antibody comprises a modified hinge region and exhibits an improved antagonistic activity. More particularly, the antibody according to the invention is capable of inhibiting the c-Met dimerization. The invention likewise comprises the use of said antibody as a medicament for the prophylactic and/or therapeutic treatment of cancers, preferably for cancer characterized by a ligand- independent activation of c-Met,or any pathology connected with the over expression of said receptor as well as in processes or kits for diagnosis of illnesses connected with the over-expression of c-Met. The invention finally comprises products and/or compositions comprising such an antibody in combination with other antibodies and/or chemical compounds directed against other growth factors involved in tumor progression or metastasis and/or compounds and/or anti-cancer agents or agents conjugated with toxins and their use for the prevention and/or the treatment of certain cancers.</p>
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Anti-cMet antibody (Fri, 30 Sep 2011)
<p id="p-0001" num="0000">Antibodies capable of binding to the human c-Met receptor and/or capable of inhibiting the tyrosine kinase activity of said receptor, with an improved antagonistic activity, the antibodies comprising a modified hinge region. A composition comprising one or more of such antibodies antagonist to c-Met and its use as a medicament for treating cancer.</p>
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(Poly) aminoalkylaminoalkylamide, alkyl-urea, or alkyl-sulfonamide derivatives of epipodophyllotoxin, a process for preparing them, and application thereof in therapy as anticancer agents (Fri, 15 Jul 2011)
<p id="p-0001" num="0000">The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamidc, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: —R represents hydrogen or C<sub>1-4</sub>alkyl, —A represents CO(CH<sub>2</sub>)<sub>n </sub>or CONH(CH<sub>2</sub>)<sub>n </sub>where n=2, 3, 4, or 5, —R1 and R2 are as described herein.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="47.07mm" wi="59.69mm" file="US08288567-20121016-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Nitrogenated derivatives of pancratistatin (Fri, 27 May 2011)
<p id="p-0001" num="0000">The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.91mm" wi="69.85mm" file="US08415348-20130409-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NOVEL PHAGE DISPLAY VECTOR (Fri, 27 May 2011)
The invention relates to a minimized phage display vector comprising at least a cloning cassette, a phage display cassette and a bacterial cassette, said cloning cassette comprising a nucleic acid sequence encoding a polypeptide corresponding at least to the intra-domain loop of a constant domain of an antibody. It also relates to their uses for the production of libraries of phages, each phage expressing on its surface a binding protein to be screened for its capacity to bind a binding partner.
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NOVEL PHAGE DISPLAY VECTOR (Fri, 27 May 2011)
The invention relates to a minimized phage display vector comprising at least a cloning cassette, a phage display cassette and a bacterial cassette, said cloning cassette comprising a nucleic acid sequence encoding a polypeptide corresponding at least to the intra-domain loop of a constant domain of an antibody. It also relates to their uses for the production of libraries of phages, each phage expressing on its surface a binding protein to be screened for its capacity to bind a binding partner.</p>
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DERIVATIVES OF TRIAZINES AND URACILS, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPEUTICS (Fri, 20 May 2011)
<p id="p-0001" num="0000">The present invention relates to derivatives of general formula I wherein: —W represents nitrogen, —R<sub>1 </sub>represents: •a hydrogen or a linear or branched C<sub>1</sub>-C<sub>5 </sub>alkyl radical or, •a C<sub>1</sub>-C<sub>3 </sub>alkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C<sub>1</sub>-C<sub>3 </sub>alcoxy, C<sub>3</sub>-C<sub>6 </sub>alkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C<sub>1</sub>-C<sub>3 </sub>N-alkylcarbamoyl groups or, •a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C<sub>1</sub>-C<sub>4 </sub>alkyl, linear or branched C<sub>1</sub>-C<sub>3 </sub>alkoxy groups, •a C<sub>6 </sub>2-oxocycloalkyl radical—R<sub>2 </sub>represents a methyl or heptyl, —m, n are equal to 1, —V represents CH<sub>2</sub>, —X—Y represents —N— (C═O)—, —CH—O—, —Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C<sub>1</sub>-C<sub>4 </sub>alkyl groups.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.99mm" wi="60.28mm" file="US20110118266A1-20110519-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Combination of a c-Met antagonist and an aminoheteroaryl compound for the treatment of cancer (Fri, 20 May 2011)
<p id="p-0001" num="0000">The invention also relates to a composition comprising an antibody antagonist to c-Met and an aminoheteroaryl compound, particularly as a medicament. The present invention also comprises a pharmaceutical composition comprising said anti c-Met antibody and said aminoheteroaryl compound as combination products for simultaneous, separate or sequential use. The invention relates to the use of the composition of the invention for the treatment of cancer in a mammal.</p>
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Anti-c-Met antibody (Fri, 29 Apr 2011)
<p id="p-0001" num="0000">The invention relates to a novel antibody capable of binding specifically to the human c-Met receptor and/or capable of specifically inhibiting the tyrosine kinase activity of said receptor both in a ligand-dependent and in a ligand-independent manner, with an improved antagonistic activity, said antibody comprising a modified hinge region.</p> <p id="p-0002" num="0000">The invention also relates to a composition comprising such an antibody antagonist to c-Met and its use as a medicament for treating cancer.</p>
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PYRAZOLOPYRIDINE DERIVATIVES AS ANTICANCER AGENT (Fri, 22 Apr 2011)
The present invention concerns compounds of following general formula (I): (Formula I) and their pharmaceutically acceptable salts, their method of preparation and their uses, notably as anticancer agent.
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CHIMERIC ANTIBODIES SPECIFIC FOR CD151 AND USE THEREOF IN THE TREATMENT OF CANCER (Fri, 15 Apr 2011)
The present invention relates to new antibodies capable of binding specifically to the human CD151 protein, especially monoclonal antibodies of murine origin, which are chimeric and humanised, and also to the amino acid and nucleic sequences coding for those antibodies. The invention also includes use of those antibodies as medicaments for the prophylactic and/or therapeutic treatment of cancers and in diagnostic methods or kits for diseases associated with overexpression of the CD151 protein. Finally, the invention includes products and/or compositions comprising such antibodies in association with antibodies and/or anti-cancer agents or conjugated with toxins and/or radioelements and their use in the prevention and/or treatment of certain cancers.
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CHIMERIC ANTIBODIES SPECIFIC FOR CD151 AND USE THEREOF IN THE TREATMENT OF CANCER (Fri, 15 Apr 2011)
The present invention relates to new antibodies capable of binding specifically to the human CD151 protein, especially monoclonal antibodies of murine origin, which are chimeric and humanised, and also to the amino acid and nucleic sequences coding for those antibodies. The invention also includes use of those antibodies as medicaments for the prophylactic and/or therapeutic treatment of cancers and in diagnostic methods or kits for diseases associated with overexpression of the CD151 protein. Finally, the invention includes products and/or compositions comprising such antibodies in association with antibodies and/or anti-cancer agents or conjugated with toxins and/or radioelements and their use in the prevention and/or treatment of certain cancers.</p>
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CHROMONE DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATIONS (Fri, 11 Mar 2011)
The present invention relates to chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.
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CHROMONE DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATIONS (Fri, 11 Mar 2011)
The present invention relates to chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.</p>
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ANTI-CMET ANTIBODY AND ITS USE FOR THE DETECTION AND THE DIAGNOSIS OF CANCER (Fri, 25 Feb 2011)
The present invention relates to the field of prognosis and/or diagnosis of a proliferative disease in a patient. More particularly, the invention relates to an antibody capable of binding specifically to the human cMet receptor, as well as the amino acid and nucleic acid sequences coding for this antibody. The invention likewise comprises the use of said antibody, and corresponding processes, for detecting and diagnosing pathological hyperprol iterative oncogenic disorders associated with expression of cMet. In certain embodiments, the disorders are oncogenic disorders associated with increased expression of cMet polypeptide relative to normal or any other pathology connected with the overexpression of cMet. The invention finally comprises products and/or compositions or kits comprising at least such antibody for the prognosis or diagnostic of certain cancers.
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ANTI-CMET ANTIBODY AND ITS USE FOR THE DETECTION AND THE DIAGNOSIS OF CANCER (Fri, 25 Feb 2011)
The present invention relates to the field of prognosis and/or diagnosis of a proliferative disease in a patient. More particularly, the invention relates to an antibody capable of binding specifically to the human cMet receptor, as well as the amino acid and nucleic acid sequences coding for this antibody. The invention likewise comprises the use of said antibody, and corresponding processes, for detecting and diagnosing pathological hyperprol iterative oncogenic disorders associated with expression of cMet. In certain embodiments, the disorders are oncogenic disorders associated with increased expression of cMet polypeptide relative to normal or any other pathology connected with the overexpression of cMet. The invention finally comprises products and/or compositions or kits comprising at least such antibody for the prognosis or diagnostic of certain cancers.</p>
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DERIVATIVES OF 2H PYRIDAZIN- 3 -ONES, THEIR PREPARATION AND THEIR USE AS SCD-1 INHIBITORS (Fri, 11 Feb 2011)
The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: -R1 represents one or more groups such as: trif luoromethyl, halogen such as F, C1, -when n=m=1, W represents CH then Y represents oxygen, -U represents: • either - (C=O) CH2NH- and is branched at position 4 of pyridazinone, then R2 represents H, • or -(C=O)NH- and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, - R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enyzme inhibitors for the treatment of obesitz, tzpe-2 diabetes and lipid disorders.
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Imidazolic compounds and use thereof as alpha-2 adrenergic receptors (Fri, 28 Jan 2011)
<p id="p-0001" num="0000">The invention provides methods of treating a memory deficiency in a subject in need of such treatment, where the methods comprise administering to a subject an effective amount of a compound of formula (1):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.97mm" wi="58.76mm" file="US08188126-20120529-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein: R1 is hydrogen, fluorine or a methoxyl group, R1 being in position 2, 3, 4 or 5 of the aromatic carbocycle; R2 is hydrogen or a methyl group; R3 is hydrogen, a methyl group or an ethyl group; and their pharmaceutically acceptable acid addition salt as well as the isomers and the tautomers thereof. The memory deficiency may be correlated with a memory deficiency induced by scopolamine. </p>
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Anti CXCR4 antibodies and their use for the treatment of cancer (Fri, 28 Jan 2011)
<p id="p-0001" num="0000">The present invention relates to a novel isolated antibody, or the derived compounds or functional fragments of same, capable of binding to CXCR4 but also of inducing conformational changed of the CXCR4 homodimers and/or heterodimers. More particularly, the present invention relates to the 414H5 and 515H7 antibodies, specific to the CXCR4 protein, as well as their use for the treatment of cancer. Pharmaceutical compositions composed of such antibodies and a process for the selection of such antibodies are also covered.</p>
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NOVEL DERIVATIVES OF ARYL-{4-HALOGENO-4-[AMINOMETHYL]-PIPERIDIN-1-YL}-METHANONE, THEIR METHOD OF PREPARATION AND THEIR USE AS MEDICINAL PRODUCTS (Fri, 10 Dec 2010)
The present invention concerns compounds of general formula (1) (I) wherein R1 is: - a hydrogen atom, or a halogen, - a straight or branched C1-C6 alkyl group or a C1-C3 fluoroalkyl group, - a straight or branched C1-C6 alcoxy group, a carbamyl group, N-substituted or not by one or two, straight or branched C1-C3 alkyl groups, or - a cyano group (CN) R2 is: - a hydrogen atom or a straight or branched C1-C6 alkyl group, HaI1, Hal2 and Hal3 are: - a halogen their addition salts and the hydrates of addition salts with pharmaceutically acceptable mineral acids or organic acids, and their enantiomer forms.
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5-[1'-(DECAHYDRO-7-HYDROXY-1,1,3A,7-TETRAMETHYL-1H-CYCLOPROPA[A]NAPHTHALEN-4-YL)-3'-METHYLBUTYL]-2,4,6-TRIHYDROXY-1,3-BENZENEDICARBOXALDEHYDE AS MEDICAMENTS (Fri, 12 Nov 2010)
<p id="p-0001-en" num="0000">The present invention relates to new compounds of formula (I) and to their use as medicaments. Preferably, the said compounds are used in the preparation of a medicament or food supplement intended for the treatment and/or prevention of ailments or pathologies ensuing from a disorder of the reuptake of the following neurotransmitters: dopamine, serotonin and/or noradrenaline.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="42.50mm" wi="67.06mm" file="US20100286284A1-20101111-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p>
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Process for the synthesis of anticancer (poly) aminoalkylaminoacetamide derivatives of epipodophyllotoxin (Fri, 05 Nov 2010)
<p id="p-0001" num="0000">The present invention describes a new process for the preparation of (poly)aminoalkylaminoacetamide compounds of epipodophyllotoxin useful for their applications in therapeutics as anticancer agents. This process comprises a step of condensation of a primary-amine-containing reactant, whose amine functions are not protected, with β-chloroacetamido-4′-epipodophyllotoxin in a polar aprotic organic solvent.</p>
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ANTI CXCR4 ANTIBODIES FOR THE TREATMENT OF HIV (Fri, 05 Nov 2010)
The present invention relates to novel isolated antibodies, or the derived compounds or functional fragments of same, capable of binding to CXCR4 but also of inducing conformational changed of the CXCR4 homodimers and able to inhibit HIV-1 primary isolate replication in PBMC. More particularly, the present invention relates to the 515H7 and 301aE5 monoclonal antibodies, specific to the CXCR4 protein, as well as their use for the treatment of HIV infection. Pharmaceutical compositions composed of such antibodies and a process for the selection of such antibodies are also covered.
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ANTI CXCR4 ANTIBODIES FOR THE TREATMENT OF HIV (Fri, 05 Nov 2010)
The present invention relates to novel isolated antibodies, or the derived compounds or functional fragments of same, capable of binding to CXCR4 but also of inducing conformational changed of the CXCR4 homodimers and able to inhibit HIV-1 primary isolate replication in PBMC. More particularly, the present invention relates to the 515H7 and 301aE5 monoclonal antibodies, specific to the CXCR4 protein, as well as their use for the treatment of HIV infection. Pharmaceutical compositions composed of such antibodies and a process for the selection of such antibodies are also covered. </p>
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DERIVATIVES OF AMINOCYCLOBUTANE OR AMINOCYCLOBUTENE, THEIR METHOD OF PREPARATION AND THEIR USE AS MEDICAL PRODUCTS (Fri, 08 Oct 2010)
The present invention concerns compounds of general formula (1), where in : - -a-is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C1-C6 alkyl group, branched or unbranched, saturated or unsaturated, substituted or unsubstituted; the groups R1 and R2 may also form a heterocycle, R3 and R3' each independently or together are a hydrogen atom or C1-C6 alkyl group, X is an oxygen atom or a sulphur atom, and the addition salts of the compounds of general formula (1) with pharmaceutically acceptable mineral acids or organic acids.
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DERIVATIVES OF BENZOTHIAZINES, PREPARATION THEREOF AND APPLICATION THEREOF AS DRUGS (Sat, 11 Sep 2010)
The object of the present invention is benzothiazine derivatives having the capability of inhibiting 11β-HSD1 not only at an enzymatic level but also at a cell level. The compounds of the present invention are of general formula (I). Wherein notably R1 represents a hydrogen or OR1 represents an ester or an ether. R2 represents a naphthyl or a 1, 2, 3, 4-tetrahydro-naphthalene or a biphenyl or phenyl pyridine or a substituted phenyl. R3 represents a methyl or ethyl; R4 and R'4 represent a hydrogen.
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DERIVATIVES OF BENZOTHIAZINES, PREPARATION THEREOF AND APPLICATION THEREOF AS DRUGS (Sat, 11 Sep 2010)
The object of the present invention is benzothiazine derivatives having the capability of inhibiting 11.beta.-HSD1 not only at an enzymatic level but also at a cell level. The compounds of the present invention are of general formula (I). Wherein notably R1 represents a hydrogen or OR1 represents an ester or an ether. R2 represents a naphthyl or a 1, 2, 3, 4-tetrahydro-naphthalene or a biphenyl or phenyl pyridine or a substituted phenyl. R3 represents a methyl or ethyl; R4 and R'4 represent a hydrogen. </p>
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NOVEL FLUORESCENT DERIVATIVES OF POLYAMINES, METHOD FOR PREPARING SAME AND APPLICATIONS THEREOF AS DIAGNOSIS TOOLS IN THE TREATMENT OF CANCEROUS TUMORS (Fri, 13 Aug 2010)
<p id="p-0001-en" num="0000">The invention relates to novel fluorescent derivatives of polyamines having a benzoxadiazole group, to a method for preparing the same and to the use thereof as diagnosis tools for emphasising the polyamine transport system in cancerous cells in order to adapt the treatment thereof, and thus for selecting patients carrying such tumours in order to adapt their treatment. The derivatives are of the formula (I) or a pharmaceutically acceptable salt thereof, in which: R<sub>1 </sub>is one or more NO<sub>2 </sub>groups in position 4 or 6, or a SO<sub>2</sub>Ph, SO<sub>2</sub>NMe<sub>2</sub>, SO<sub>2</sub>NH<sub>2 </sub>or SO<sub>3</sub>H group; R<sub>2 </sub>is hydrogen, C<sub>1-6 </sub>alkyl, benzyl, a perfluoroalkyl group; the values of a, b, c range from 2 to 5 independently from each other and represent alkylene chains separating the amino groups, and the values of d and e can independently be 0 or 1.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="30.40mm" wi="69.85mm" file="US20100202975A1-20100812-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p>
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ANTI-cMET ANTIBODY (Fri, 25 Jun 2010)
Antibody capable of binding specifically to the human c-Met receptor and/or capable of specifically inhibiting the tyrosine kinase activity of said receptor, with an improved antagonistic activity, said antibody comprising a modified hinge region. A composition comprising such an antibody antagonist to c-Met and its use as a medicament for treating cancer.
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ANTI-CMET ANTIBODY (Fri, 25 Jun 2010)
Antibody capable of binding specifically to the human c-Met receptor and/or capable of specifically inhibiting the tyrosine kinase activity of said receptor, with an improved antagonistic activity, said antibody comprising a modified hinge region. A composition comprising such an antibody antagonist to c-Met and its use as a medicament for treating cancer. </p>
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Anti-CD151 antibodies and their use in the treatment of cancer (Fri, 18 Jun 2010)
<p id="p-0001" num="0000">The present invention relates to new antibodies capable of binding specifically to the human CD151 protein, especially monoclonal antibodies of murine origin, which are chimeric and humanised, and also to the amino acid and nucleic sequences coding for those antibodies. The invention also includes use of those antibodies as medicaments for the prophylactic and/or therapeutic treatment of cancers and in diagnostic methods or kits for diseases associated with overexpression of the CD151 protein. Finally, the invention includes products and/or compositions comprising such antibodies in association with antibodies and/or anti-cancer agents or conjugated with toxins and/or radioelements and their use in the prevention and/or treatment of certain cancers.</p>
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NOVEL ANTI-CMET ANTIBODY (Fri, 11 Jun 2010)
Antibody capable of binding specifically to the human c-Met receptor and/or capable of specifically inhibiting the tyrosine kinase activity of said receptor, with an improved antagonistic activity, said antibody comprising a modified hinge region. A composition comprising such an antibody antagonist to c-Met and its use as a medicament for treating cancer.
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Antibodies inhibiting c-Met dimerization and uses thereof (Fri, 07 May 2010)
<p id="p-0001" num="0000">A process for the selection of anti c-Met antibodies capable of inhibiting both ligand-dependent and ligand-independent activation of c-Met, wherein said process is based on the inhibition of the c-Met dimerization. The present invention also concerns such antibodies and compositions comprising antibodies for the preparation of a medicament to treat cancer including diagnosis process and kits.</p>
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Anti-JAM-A antibodies (Fri, 16 Apr 2010)
<p id="p-0001" num="0000">The present invention relates to novel isolated antibodies, derived compounds, and functional isolated antibody fragments, capable of inhibiting the proliferation of tumor cells in vitro and/or in vivo and obtained by functional screening.</p> <p id="p-0002" num="0000">More particularly, the present invention relates to the 6F4 antibody, specific to the JAM-A protein, as well as its use for the treatment of cancer. Pharmaceutical compositions composed of these antibodies are also covered.</p>
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Fluorinated catharanthine derivatives, their preparation and their utilisation as <i>Vinca </i>dimeric alkaloid precursors (Fri, 16 Apr 2010)
<p id="p-0001" num="0000">The fluorinated derivatives of catharanthine according to the invention respond to the general formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.18mm" wi="69.85mm" file="US08101748-20120124-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which: <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">the dotted line expresses the possibility of the presence of a double bond when the substitution —X is absent or else a single bond when —X designates a substitution for a group: <ul id="ul0003" list-style="none"> <li id="ul0003-0001" num="0000">H,</li> <li id="ul0003-0002" num="0000">OR,</li> <li id="ul0003-0003" num="0000">NR′R″,</li> <li id="ul0003-0004" num="0000">SR, or</li> <li id="ul0003-0005" num="0000">a halogen atom with R, R′ and R″ designating independently of one another a hydrogen atom or a linear or branched alkyl group in C<sub>1 </sub>to C<sub>6</sub>,</li> </ul> </li> <li id="ul0002-0002" num="0000">R<sub>1</sub>, R<sub>2 </sub>and R<sub>3 </sub>represent independently of one another an atom of hydrogen, of fluorine or a methylated group, on the condition nevertheless that at least one of the radicals R<sub>1 </sub>and R<sub>2 </sub>represents an atom of fluorine, and <br/> n=1 or 2. </li> </ul> </li> </ul> </p>
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ANTI CXCR4 ANTIBODIES AND THEIR USE FOR THE TREATMENT OF CANCER (Fri, 09 Apr 2010)
The present invention relates to a novel isolated antibody, or the derived compounds or functional fragments of same, capable of binding to CXCR4 but also of inducing conformational changed of the CXCR4 homodimers and/or heterodimers. More particularly, the present invention relates to the 414H5 and 515H7 antibodies, specific to the CXCR4 protein, as well as their use for the treatment of cancer. Pharmaceutical compositions composed of such antibodies and a process for the selection of such antibodies are also covered.
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NOVEL ANTI CXCR4 ANTIBODIES AND THEIR USE FOR THE TREATMENT OF CANCER (Fri, 09 Apr 2010)
The present invention relates to a novel isolated antibody, or the derived compounds or functional fragments of same, capable of binding to CXCR4 but also of inducing conformational changed of the CXCR4 homodimers and/or heterodimers. More particularly, the present invention relates to the 414H5 and 515H7 antibodies, specific to the CXCR4 protein, as well as their use for the treatment of cancer. Pharmaceutical compositions composed of such antibodies and a process for the selection of such antibodies are also covered. </p>
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NEW (POLY)AMINOALKYLAMINOALKYLAMIDE, ALKYL-UREA, OR ALKYL-SULFONAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN, A PROCESS FOR PREPARING THEM, AND APPLICATION THEREOF IN THERAPY AS ANTICANCER AGENTS (Fri, 26 Feb 2010)
The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamidc, or alkyl-urea or alkyl- sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: - R represents hydrogen or C1-4alkyI, - A represents CO(CH2)n or CONH(CH2)n where n = 2, 3, 4, or 5, - R1 and R2 are as described herein.
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NEW (POLY)AMINOALKYLAMINOALKYLAMIDE, ALKYL-UREA, OR ALKYL-SULFONAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN, A PROCESS FOR PREPARING THEM, AND APPLICATION THEREOF IN THERAPY AS ANTICANCER AGENTS (Fri, 26 Feb 2010)
The present invention relates to new derivatives of epipodophyllotoxin 4- substituted with an optionally substituted (poly)aminoalkylaminoalkylamidc, or alkyl-urea or alkyl- sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: - R represents hydrogen or C1-4alkyl, - A represents CO(CH2)n or CONH(CH2)n where n = 2, 3, 4, or 5, - R1 and R2 are as described herein. </p>
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Anhydrous crystalline vinflunine salts, method of preparation and use thereof as a drug and means of vinflunine purification (Fri, 05 Feb 2010)
<p id="p-0001" num="0000">The present invention relates to anhydrous crystalline vinflunine salts obtained with 1 or 2 equivalents of a pharmaceutically acceptable mineral or organic acid [Acid] 1 or 2 in which [Acid] represents hydrobromic, sulfuric, lactic and fumaric acids for the group of water-soluble crystalline salts, and para-toluene sulfonic, benzoic, mandelic and para-hydroxy benzoic acids for the group of relatively insoluble crystalline salts.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="52.58mm" wi="74.25mm" file="US08343991-20130101-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NITROGENATED DERIVATIVES OF PANCRATISTATIN (Fri, 05 Feb 2010)
The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.
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NITROGENATED DERIVATIVES OF PANCRATISTATIN (Fri, 05 Feb 2010)
The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation. </p>
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DERIVATIVES OF TRIAZINES AND URACILS, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPEUTICS (Fri, 22 Jan 2010)
The present invention relates to derivatives of general formula I wherein : - W represents nitrogen, - R1 represents: • a hydrogen or a linear or branched C1-C5 alkyl radical or, • a C1-C3 alkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C1-C3 alcoxy, C3-C6 alkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C1-C3 N-alkylcarbamoyl groups or, • a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C1-C4 alkyl, linear or branched C1-C3 alkoxy groups, • a C6 2-oxocycloalkyl radical - R2 represents a methyl or heptyl, - m, n are equal to 1, - V represents CH2, - X-Y represents -N- (C=O) -, -CH-O-, - Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C1-C4 alkyl groups.
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COMBINATION OF A C-MET ANTAGONIST AND AN AMINOHETEROARYL COMPOUND FOR THE TREATMENT OF CANCER (Fri, 15 Jan 2010)
The invention also relates to a composition comprising an antibody antagonist to c-Met and an aminoheteroaryl compound, particularly as a medicament. The present invention also comprises a pharmaceutical composition comprising said anti c-Met antibody and said aminoheteroaryl compound as combination products for simultaneous, separate or sequential use. The invention relates to the use of the composition of the invention for the treatment of cancer in a mammal.
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COMBINATION OF A C-MET ANTAGONIST AND AN AMINOHETEROARYL COMPOUND FOR THE TREATMENT OF CANCER (Fri, 15 Jan 2010)
<br/><br/><br/><br/> The invention also relates to a composition comprising an <br/>antibody antagonist to c-Met and an aminoheteroaryl compound, particularly <br/>as a medicament. The present invention also comprises a pharmaceutical <br/>composition comprising said anti c-Met antibody and said amino-heteroaryl <br/>compound as combination products for simultaneous, separate <br/>or sequential use. The invention relates to the use of the composition of <br/>the invention for the treatment of cancer in a mammal.<br/><br/><br/><br/></p>
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Phenylpentadienoyl derivatives and their use as PAR 1 antagonists (Fri, 08 Jan 2010)
<p id="p-0001" num="0000">The present invention relates to compounds of general formula (I): wherein: R<sub>1 </sub>and R<sub>2</sub>, identical or different, represent: an atom of hydrogen or halogen, CN or NO<sub>2</sub>, with R<sub>1 </sub>and R<sub>2 </sub>not representing hydrogen simultaneously, m represents: 1 or 2 n represents: 0, 1 or 2 R<sub>3 </sub>represents: phenyl substituted or not by one or more residues chosen among halogen, hydroxyl or C<sub>1</sub>-C<sub>6 </sub>alkyl; C<sub>2</sub>-C<sub>6 </sub>alkyl substituted or not by one or more residues chosen among halogen or hydroxyl; cycloalkyl; pyridine; thiophene; pyrrole substituted or not by C<sub>1</sub>-C<sub>6 </sub>alkyl; thiazole or furan; or the therapeutically-acceptable salts or solvates thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="21.84mm" wi="72.90mm" file="US08022064-20110920-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Process for the synthesis of N-[3-[(2-methoxyphenyl] sulfanyl] -2-methylpropyl] -3,4-dihydro-2H-1,5-benzoxathiepin-3-amine (Fri, 25 Dec 2009)
<p id="p-0001" num="0000">The invention relates to a new process for the preparation of N-[3-[(2-methoxyphenyl)sulfanyl]-2-methylpropyl]-3,4-dihydro-2H-1,5-benzoxathiepin-3-amine.</p>
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Cinnamoyl-piperazine derivatives and their use as PAR-1 antagonists (Fri, 10 Jul 2009)
<p id="p-0001" num="0000">The present invention relates to compounds of general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="19.64mm" wi="57.74mm" file="US08217046-20120710-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein: <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">R<sub>1 </sub>represents: <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">halogen, CN or NO<sub>2</sub>;</li> </ul> </li> <li id="ul0001-0002" num="0000">R<sub>2 </sub>represents: <ul id="ul0003" list-style="none"> <li id="ul0003-0001" num="0000">hydrogen or halogen;</li> </ul> </li> <li id="ul0001-0003" num="0000">n represents: <ul id="ul0004" list-style="none"> <li id="ul0004-0001" num="0000">1 or 2;</li> </ul> </li> <li id="ul0001-0004" num="0000">R<sub>3 </sub>represents: <ul id="ul0005" list-style="none"> <li id="ul0005-0001" num="0000">phenyl substituted by one or more halogens or C<sub>1</sub>-C<sub>6 </sub>alkyls; or a cyclohexyl;</li> </ul> </li> <li id="ul0001-0005" num="0000">as well as the therapeutically-acceptable salts or solvates thereof.</li> </ul> </p> <p id="p-0003" num="0000">These compounds are useful as protease-activated receptor-1 (PAR-1) antagonists, particularly in the treatment of thrombosis.</p>
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(Poly)aminoacetamide derivatives of epipodophyllotoxin their process of preparation and their applications in therapeutics as anticancer agents (Fri, 03 Jul 2009)
<p id="p-0001-en" num="0000">The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.</p>
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Process For Preparing [2-(2,3- Dihydrobenzofuran - Or Benzofuran-7-Yloxy)Ethyl]-(3 -Cyclopent-1-Ylbenzyl)Amine Derivatives and Synthesis Intermediate (Fri, 27 Mar 2009)
<p id="p-0001-en" num="0000">The invention relates to a process for the preparation of compounds of general formula (3)</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="30.06mm" wi="70.95mm" file="US20090082582A1-20090326-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein: <ul id="ul0001-en" list-style="none"><li><ul id="ul0002-en" list-style="none"><li>(a) represents a single or double bond;</li><li>W represents a group CH, CH<sub>2</sub>, CHCH<sub>3</sub>, CCH<sub>3</sub>, C(CH<sub>3</sub>)<sub>2</sub>, a group C(CH<sub>2</sub>)<sub>2 </sub>(i.e. a carbon atom carrying two methylene groups bonded to one another so as to form a spiro-cyclopropane moiety), with the proviso, however, that when (a) is a double bond then W represents exclusively a group CH or CCH<sub>3 </sub>and when (a) is a single bond then W represents exclusively a group CH<sub>2</sub>, CHCH<sub>3</sub>, C(CH<sub>3</sub>)<sub>2 </sub>or C(CH<sub>2</sub>)<sub>2</sub>.</li></ul></li></ul></p>
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NOVEL ANTIBODIES INHIBITING C-MET DIMERIZATION, AND USES THEREOF (Fri, 16 Jan 2009)
The present inventions relates to a process for the selection of anti c-Met antibodies capable to inhibit both ligand-dependent and ligand-independent activation of c-Met. More particularly, said process is based on the inhibition of the c-Met dimerization. In another aspect, the present invention concerns such antibodies and compositions comprising such antibodies for the preparation of a medicament to treat cancer. Diagnosis process and kits are also part of the invention.
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STABLE PHARMACEUTICAL COMPOSITION COMPRISING A HYDROSOLUBLE VINFLUNINE SALT (Fri, 16 Jan 2009)
Stable pharmaceutical composition consisting of a hydrosoluble vinflunine salt and at least one diluent and one lubricant, said composition being in the form of a solid intended for oral administration. The hydrosoluble vinflunine salt is preferably Vinflunine ditartrate. The pharmaceutical composition is advantageously in the form of a capsule or tablet. The invention also concerns a method of treating cancer pathology comprising the oral administration of the pharmaceutical composition of the invention.
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NOVEL ANTIBODIES INHIBITING C-MET DIMERIZATION, AND USES THEREOF (Fri, 16 Jan 2009)
<br/><br/>The present inventions relates to a process for the selection of anti c-Met <br/>antibodies capable to inhibit both ligand-dependent <br/>and ligand-independent activation of c-Met. More particularly, said process is <br/>based on the inhibition of the c-Met <br/>dimerization. In another aspect, the present invention concerns such <br/>antibodies and compositions comprising such antibodies for the <br/>preparation of a medicament to treat cancer. Diagnosis process and kits are <br/>also part of the invention.<br/></p>
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Synthesising method and benzoxathiepine intermediates (Fri, 26 Sep 2008)
<p id="p-0001" num="0000">The invention relates to preparing derivatives of formula (1), wherein, in particular R<sub>1 </sub>and R<sub>2</sub>, identical or different, represent a hydrogen, flourine or chlorine atom, a hydroxy group, an alkyl radical and an alkoxy radical, R<sub>3 </sub>is an alkyl radical, a hydroxy group, or a methoxy radical, R<sub>4 </sub>is a hydrogen atom or a methyl radical and R<sub>5 </sub>and R<sub>6</sub>, identical or different, represent a hydrogen atom, an alkyl radical, an alkoxy radical, an alkylthio radical, and an alkylamino radical. The inventive method consists in reducing an amid of formula (9).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="67.99mm" wi="73.32mm" file="US07902381-20110308-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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ANHYDROUS CRYSTALLINE VINFLUNINE SALTS, METHOD OF PREPARATION AND USE THEREOF AS A DRUG AND MEANS OF VINFLUNINE PURIFICATION (Fri, 22 Aug 2008)
The present invention relates to anhydrous crystalline vinflunine salts obtained with 1 or 2 equivalents of a pharmaceutically acceptable mineral or organic acid [Acid] 1 or 2 in which [Acid] represents hydrobromic, sulfuric, lactic and fumaric acids for the group of water-soluble crystalline salts, and para-toluene sulfonic, benzoic, mandelic and para- hydroxy benzoic acids for the group of relatively insoluble crystalline salts.
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ANHYDROUS CRYSTALLINE VINFLUNINE SALTS, METHOD OF PREPARATION AND USE THEREOF AS A DRUG AND MEANS OF VINFLUNINE PURIFICATION (Fri, 22 Aug 2008)
The present invention relates to anhydrous crystalline vinflunine salts obtained with 1 or 2 equivalents of a pharmaceutically acceptable mineral or organic acid [Acid] 1 or 2 in which [Acid] represents hydrobromic, sulfuric, lactic and fumaric acids for the group of water-soluble crystalline salts, and para-toluene sulfonic, benzoic, mandelic and para- hydroxy benzoic acids for the group of relatively insoluble crystalline salts.</p>
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TRIPTOLIDE DERIVATIVES FOR USE IN THE TREATMENT OF ACUTE MYELOID LEUKEMIA (Fri, 25 Jul 2008)
The invention is directed to the use of an ester derivatives of triptolide, tripdiolide, 16-hydroxytriptolide, a pharmaceutically acceptable salt thereof, or a combination thereof, for the manufacture of a medicament comprising the triptolide prodrug for the treatment of acute myeloid leukemia.
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1,2,4-triazine derivatives, preparation and use thereof in human therapy (Fri, 11 Jul 2008)
<p id="p-0001-en" num="0000">The invention relates to 3,5-dioxo-(2H,4H)-1,2,4-triazine compounds of formula I</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="30.06mm" wi="72.64mm" file="US07713971-20100511-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> in which the variables are defined herein, as well as additive salts with pharmaceutically acceptable bases and the various enantiomers of compounds having asymmetrical carbons, as well as their mixtures in all proportions, including racemic mixtures in particular. </p>
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(POLY)AMINOACETAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN THEIR PROCESS OF PREPARATION AND THEIR APPLICATIONS IN THERAPEUTICS AS ANTICANCER AGENTS (Thu, 26 Jun 2008)
(poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.
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NOVEL ANTIPROLIFERATION ANTIBODIES (Fri, 30 May 2008)
The present invention relates to novel isolated antibodies, or the derived compounds or functional fragments of same, capable of inhibiting the proliferation of tumor cells in vitro and/or in vivo, said antibodies having been obtained by functional screening. More particularly, the present invention relates to the 6F4 antibody, specific to the JAM-A protein, as well as its use for the treatment of cancer. Pharmaceutical compositions composed of such antibodies are also covered.
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NOVEL ANTIPROLIFERATION ANTIBODIES (Fri, 30 May 2008)
The present invention relates to novel isolated antibodies, or the derived compounds or functional fragments of same, capable of inhibiting the proliferation of tumor cells in vitro and/or in vivo, said antibodies having been obtained by functional screening. More particularly, the present invention relates to the 6F4 antibody, specific to the JAM-A protein, as well as its use for the treatment of cancer. Pharmaceutical compositions composed of such antibodies are also covered.</p>
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1,2,4-TRIAZINE DERIVATIVES,PREPARATION AND USE THEREOF IN HUMAN THERAPY (Thu, 29 May 2008)
</p> <p>concerns 3,5-dioxo-(2H,4H)-l,2,4-tri- 3 azine derivatives of general formula <br> (I), wherein: R<sub>t</sub> and R<sub>2</sub>, identical <br> (I) or different, represent a branched <BR> or linear C<sub>v</sub>-C, alkyl or alkenyl <br> radical, a C<sub>t</sub>-Q alkyl radical <br> <BR> substituted by groups such as R2 Lrifluoromethyl, Cj-Q cycloalkyl, <br> nitrile, C C alkoxycarbonylvinyl, hydroxycarbonylvinyl, -G, alkoxycarbonyi, carboxylate, benzyloxy or phenyl (for which the phenyl ring is optionally substituted by one or more groups such as Ci-C alkoyl, Ci-C<sub>4</sub> alkoxy, nitro, halogen, trifluoromethyl); YRj represents oxygen or NR<sub>3</sub> for which R3 represents hydrogen, a linear or branched C[-C<sub>7</sub> alkyl or alkenyl radical, a C<sub>t</sub>-C< alkyl radical substituted by groups such as trifluoromethyl or phenyl (for which the phenyl ring is optionally substituted by one or more groups such as Ci-C alkoyl, Ci-C<sub>4</sub> alkoxy, nitro, halogen, trifluoromethyl); Z represents an oxygen atom or a carbon atom capable of being bound to the ortho, metaor para positions of the phenyl group of formula I; n can be 0 to 5 when Z=C or 2 to 4 when Z-O; X represents oxygen or sulphur; R,, R<sub>s</sub>, Ri, R<sub>7</sub> and Rg represent hydrogen or fluorine; R<sub>9</sub>, R<sub>l0</sub> and R<sub>u</sub> represent hydrogen or a linear or branched Q-Cj alkyl group as well as the pharmaceutically acceptable base addition salts, and the various enantiomers of compounds having asymmetric carbons, and their mixtures in all proportions including in particular the racemic mixtures. <br> (57) Abregd : Llnvendon conccrne des derives de la 3,5-dioxo-(2H,4H)-l ,2,4-triazine de formule generale (I) dans laquelle - R) et R; peuvent fitre identiques on differents et reprisentent un radical alkyle on alkenyle lineaire ou branch^ en C<sub>r</sub>C<sub>7</sub>, un radical alkyle en Ci-Cj substitue par des groupements tels que, trifluoromithyle, cycloalkyle en Q-Q, nitrile, alkoxycarbonylvinyle en C1-C4, hydroxycarbonylvinyle, alkoxycarbonyle en Ci-Q, carboxylate, benzyloxy ou phenyle (pour lesquels le noyau phenyle est iventuel- IT) lement substitu6 par un ou plusieurs groupements tels que alcoyle en Q-G,, alkoxy en C1-C4, nitro, halogcne, trifluoromithyle). -r YR<sub>3</sub> represente l'oxygene ou NR<sub>3</sub> pour lequel R<sub>3</sub> reprisente 1'hydrogene, un radical alcoyle ou alkenyle lineaire ou branche en C,-C<sub>7</sub>,</p> <p>O un radical alkyle en Ci-C« substitue par des groupements tels que, trifluoromithyle ou phenyle (pour lesquels le noyau phenyle est © iventuellement substitue par un ou plusieurs groupements tels que alcoyle en Ci-C<sub>4</sub>, alkoxy en Ci-C , nitro, halogene, trifluorome- thyle) · Z represente un atome d'oxygene ou un atome de carbone pouvant elre lie aux positions ortho, meta ou para du groupement</p> <p>© phenyle de la formule I ti peul-etre egal a 0 a 5 lorsque Z=C ou 2 a 4 lorsque Ζ=θ, - X represente l'oxygene ou le soufre - ,, R<sub>s</sub>, © R<sub>$</sub>, R<sub>7</sub> et Rg represented 1'hydrogene ou le fluor, - R<sub>9</sub>, R<sub>I0</sub> et R<sub>u</sub> representent l'hydrogene ou un groupement alkyle en C<sub>x</sub>-C<sub>3</sub> lineaire ou branche ainsi que les sels d'addition avec les bases pharmaceutiquement acceptables, et les differents nantiomeres des composes possedant des carbones asymetriques, ainsi que leurs melanges en toutes proportions incluant <br> [Suite sur la page suivarue]
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FLUORINATED CATHARANTHINE DERIVATIVES, THEIR PREPARATION AND THEIR UTILISATION AS VINCA DIMERIC ALKALOID PRECURSORS (Fri, 28 Mar 2008)
The fluorinated derivatives of catharanthine according to the invention respond to the general formula (I) in which: the dotted line expresses the possibility of the presence of a double bond when the substitution -X is absent or else a single bond when -X designates a substitution for a group: H, OR, NR' R', SR, or a halogen atom with R, R' and R' designating independently of one another a hydrogen atom or a linear or branched alkyl group in C1 to C6, R1, R2 and R3 represent independently of one another an atom of hydrogen, of fluorine or a methylated group, on the condition nevertheless that at least one of the radicals R1 and R2 represents an atom of fluorine, and n = 1 or 2.
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FLUORINATED CATHARANTHINE DERIVATIVES, THEIR PREPARATION AND THEIR UTILISATION AS VINCA DIMERIC ALKALOID PRECURSORS (Fri, 28 Mar 2008)
The fluorinated derivatives of catharanthine according to the invention respond to the general formula (I) in which: the dotted line expresses the possibility of the presence of a double bond when the substitution -X is absent or else a single bond when -X designates a substitution for a group: H, OR, NR' R", SR, or a halogen atom with R, R' and R" designating independently of one another a hydrogen atom or a linear or branched alkyl group in C1 to C6, R1, R2 and R3 represent independently of one another an atom of hydrogen, of fluorine or a methylated group, on the condition nevertheless that at least one of the radicals R1 and R2 represents an atom of fluorine, and n = 1 or 2.</p>
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NOVEL CHROMENE AND THIOCHROMENE CARBOXAMIDE DERIVATIVES, METHODS FOR PREPARING SAME AND THERAPEUTIC APPLICATIONS OF SAME (Fri, 25 Jan 2008)
The present invention relates to novel chromene or thiochromene carboxamide derivatives, the preparation of same, pharmaceutical compositions of same and the use of same as dopamine D3 ligands as a medicament for central nervous system disorders.
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NOVEL CHROMENE AND THIOCHROMENE CARBOXAMIDE DERIVATIVES, METHODS FOR PREPARING SAME AND THERAPEUTIC APPLICATIONS OF SAME (Fri, 25 Jan 2008)
The present invention relates to novel chromene or thiochromene carboxamide derivatives, the preparation of same, pharmaceutical compositions of same and the use of same as dopamine D3 ligands as a medicament for central nervous system disorders.</p>
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PHENYLPENTADIENOYL DERIVATIVES AND THEIR USE AS PAR 1 ANTAGONISTS (Fri, 28 Dec 2007)
The present invention relates to compounds of general formula (I): wherein: R1 and R2, identical or different, represent: an atom of hydrogen or halogen, CN or NO2, with R1 and R2 not representing hydrogen simultaneously, m represents: 1 or 2 n represents: 0, 1 or 2 R3 represents: phenyl substituted or not by one or more residues chosen among halogen, hydroxyl or C1-C6 alkyl; C2-C6 alkyl substituted or not by one or more residues chosen among halogen or hydroxyl; cycloalkyl; pyridine; thiophene; pyrrole substituted or not by C1-C6 alkyl; thiazole or furan; or the therapeutically-acceptable salts or solvates thereof.
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CINNAMOYL-PIPERAZINE DERIVATIVES AND THEIR USE AS PAR- I ANTAGONISTS (Fri, 28 Dec 2007)
The present invention relates to compounds of general formula (I), wherein: R1 represents halogen, CN or NO2; R2 represents hydrogen or halogen; n represents 1 or 2; R3 represents phenyl substituted by one or more halogens or C1-C6 alkyls; or a cyclohexyl; as well as the therapeutically-acceptable salts or solvates thereof. These compounds are useful as protease-activated receptor-1 (par-1) antagonists, particularly in the treatment of thrombosis.
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CINNAMOYL-PIPERAZINE DERIVATIVES AND THEIR USE AS PAR-1 ANTAGONISTS (Fri, 28 Dec 2007)
The present invention relates to compounds of general formula (I), wherein: R1 represents halogen, CN or NO2; R2 represents hydrogen or halogen; n represents 1 or 2; R3 represents phenyl substituted by one or more halogens or C1-C6 alkyls; or a cyclohexyl; as well as the therapeutically-acceptable salts or solvates thereof. These compounds are useful as protease-activated receptor-1 (par-1) antagonists, particularly in the treatment of thrombosis.</p>
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PHENYLPENTADIENOYL DERIVATIVES AND THEIR USE AS PAR 1 ANTAGONISTS (Fri, 28 Dec 2007)
The present invention relates to compounds of general formula (I): wherein: R1 and R2, identical or different, represent: an atom of hydrogen or halogen, CN or NO2, with R1 and R2 not representing hydrogen simultaneously, m represents: 1 or 2 n represents: 0, 1 or 2 R3 represents: phenyl substituted or not by one or more residues chosen among halogen, hydroxyl or C1-C6 alkyl; C2-C6 alkyl substituted or not by one or more residues chosen among halogen or hydroxyl; cycloalkyl; pyridine; thiophene; pyrrole substituted or not by C1-C6 alkyl; thiazole or furan; or the therapeutically-acceptable salts or solvates thereof.</p>
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Inclusion complexes containing an active substance, a cyclodextrin and an agent for interaction (Fri, 23 Nov 2007)
<p id="p-0001" num="0000">The invention relates to a method for preparing a soluble inclusion complex comprising one or several active substances which are hardly soluble in an aqueous medium and are included in one or several host molecules, characterised in that it comprises the following succesive stages: (a) one or several active substances are brought into contact with one or several host molecules; (b) initiation of a molecular diffusion stage by bringing a dense pressurized fluid into contact with the mixture obtained in stage (a) in a static mode in the presence of one or several diffusing agents; (c) recovery of the active substance- host molecule molecular complex thus formed; (d) initiation of a stage wherein an interaction agent is added to and mixed with the active substance host molecule molecular complex; (e) recovery of the soluble inclusion compound thus formed. The invention also relates to the soluble inclusion compound which can be obtained by said method, particularly a piroxicam-cyclodextrin-arginine compound.</p>
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Imidazolic compounds and use thereof as alpha-2 adrenergic receptors (Fri, 24 Aug 2007)
<p id="p-0001-en" num="0000">The invention provides methods of treating a memory deficiency in a subject in need of such treatment, where the methods comprise administering to a subject an effective amount of a compound of formula (1):</p> <p id="p-0002-en" num="0000"> <ul id="ul0001-en" list-style="none"> <li> <ul id="ul0002-en" list-style="none"> <li>wherein: R1 is hydrogen, fluorine or a methoxyl group, R1 being in position 2, 3, 4 or 5 of the aromatic carbocycle; R2 is hydrogen or a methyl group; R3 is hydrogen, a methyl group or an ethyl group; and their pharmaceutically acceptable acid addition salt as well as the isomers and the tautomers thereof. The memory deficiency may be correlated with a memory deficiency induced by scopolamine.</li> </ul> </li> </ul> </p>
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CRYSTALLINE FORM OF VINFLUNINE DITARTRATE (Fri, 29 Jun 2007)
The present invention relates to a novel crystalline form of vinflunine, to a process for preparing it, and to its uses in the therapeutic field, in particular for treating cancer.
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CRYSTALLINE FORM OF VINFLUNINE DITARTRATE (Fri, 29 Jun 2007)
The present invention relates to a novel crystalline form of vinflunine, to a process for preparing it, and to its uses in the therapeutic field, in particular for treating cancer. </p>
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METHOD FOR PREPARING (3-CHLORO-4-FLUOROPHENYL)-(4-FLUORO-4-{[(5METHYL-PYRIMIDIN-2-YLMETHYL)-AMINO]-METHYL}-PIPERIDIN-1-YL)-METHANONE AND NOVEL INTERMEDIATE PYRIMIDINE DERIVATIVES (Fri, 13 Apr 2007)
The present invention concerns the method for preparing (3-chloro-4-fluorophenyl)-(4-fluoro-4-{[(5-methyl-pyrimidin-2- ylmethyl)-amino]-methyl}-piperidin-1-yl)-methanone of formula (II) by condensation between 5-methyl-pyrimidin-2-methylamine of formula (I) and cyanohydrin of formula (III).
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Crystalline compound of 4'-demethyl-4'-phosphate-2", 3"-bispentafluorophenoxy-acetyl-4", 6"-ethylidene-beta-d-epipodophyllotoxin glucoside either in its free form or solvated with ethanol (Fri, 23 Feb 2007)
<p id="p-0001-en" num="0000">The invention relates to a crystalline compound of 4′-demethyl-4′-phosphate-2″,3″-bispentafluorophenoxyacetyl-4″,6″-ethylidene-β-D-epipodophyllotoxin glucoside in its free form or solvated with ethanol, advantageously provided in the form of a hemiethanolate solvate. The invention also relates to a method for preparing these compounds and to their use as an anticancer drug. </p>
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ANTIBODIES THAT BIND TO AN EPITOPE ON INSULIN-LIKE GROWTH FACTOR 1 RECEPTOR AND USES THEREOF (Fri, 05 Jan 2007)
The invention relates to the identification of an epitopic region within the extracellular domain of human IGF-1 receptor. Methods of identifying antibodies that specifically bind to the herein disclosed epitopic region together with compositions comprising the antibodies and uses thereof in treating IGF-1 receptor mediated disorders, particularly those that over express IGF-1 receptor are disclosed.
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3-(cyclopenten-1-yl)-benzyl-or 3-(cyclopenten-1-yl)-heteroarylmethyl-amine derivatives and use thereof as medicines for treating schizophrenia (Fri, 24 Nov 2006)
<p id="p-0001-en" num="0000">The invention provides compounds of the formula:</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="29.46mm" wi="71.04mm" file="US07235568-20070626-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein (a) is a single or double bond; W is CH, CH<sub>2</sub>, CHCH<sub>3</sub>, C(CH<sub>3</sub>)<sub>2</sub>, C(CH<sub>2</sub>)<sub>2 </sub>or C(CH<sub>2</sub>)<sub>3</sub>; X is N; and Y is H or F, and salts, hydrates, tautomers, pure enantiomers, and enantiomeric mixtures; and a method of treating schizophrenia comprising administering same. </p>
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Alpha-phenyl acetanilide derivatives having an acat inhibiting activity and the therapeutic application thereof (Fri, 23 Jun 2006)
<p id="p-0001-en" num="0000">The present invention relates to novel analide derivatives of formula I, enantiomers and stereoisomers thereof, and their pharmaceutically acceptable salts. The invention also relates to pharmaceutical compositions containing the compounds and methods of treating hypercholesterolemia and atherosclerosis therewith. </p>
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Aryl-[4-halo-4(heteroarylmethylamino)-methyl]-piperidin-1-1yl]-methanone derivatives, methods for production and use thereof as medicaments (Fri, 12 May 2006)
<p id="p-0001-en" num="0000">The invention relates to compounds of general formula (1) in which X and Y=a carbon with a bonded hydrogen atom (CH) or a nitrogen atom, A=a methyl, fluoromethyl, cyano, hydroxyl, methoxy group, or a chlorine or fluorine atom on condition that when A=methyl (CH3) and X and Y both=a carbon bonded to a hydrogen atom, then B=a chlorine atom, B=a chlorine or a fluorine atom, D=a hydrogen, chlorine, fluorine atom, or a cyano or trifluoromethyl group and E=a hydrogen, fluorine or chlorine atom.</p>
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Imidazolic compounds and use thereof as alpha-2-adrenergic receptors (Fri, 24 Feb 2006)
<p id="p-0001-en" num="0000">The invention provides compounds having the formula (1):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="29.72mm" wi="58.08mm" file="US07220866-20070522-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R1 is hydrogen, fluoro or methoxyl, R1 being in position 2, 3, 4 or 5 of the aromatic carbocycle; R2 is hydrogen or methyl; R3 is hydrogen, methyl or ethyl; and their pharmaceutically acceptable acid addition salts, hydrates of their pharmaceutically acceptable acid addition salts as well as the isomers and the tautomers thereof. </p>
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ALPHA-PHENYL ACETANILIDE DERIVATIVES HAVING AN ACAT INHIBITING ACTIVITY AND THERAPEUTIC APPLICATION THEREOF (Thu, 26 Jan 2006)
</p> <p>group, R2 represents hydro_gen or a methyl radical, R<sub>j</sub> represents hydrogen or a fluorine atom and A represents: grou p a, formula (Π ), wherein n represents an in tejer from 5 to Π, inclusive, R5, which can be identical or different, represent indejpeiidently of one</p> <p>I/) another hydrogen or a flua»rine atom: group b, formula (ID), wherein n, R,, have the same meaning as above. TBic invention also ID relates to the pharmaceutical compositions containing at least one of the aforementioned compounds by way of an active principle ID and to the use of said derivatives for the production of medicaments which are intended for the treatment of hypercholesterolemia to or atherosclerosis. <br>© <br> (57) Abrege : L'invention conceme de nouveaux denves de formule generate (I) dans laquelle: -.R, reprcscntc un groupement hy-o <br>o droxylc ou amino - 2 repr~esente l'hydrogene ou un radical mithyle - reprcsente l'hydrogene 00 un atome de flvnor - A rcprtsente un groupement (ΓΓ) dans Cequel : -n represente un nombre entier de 5 a 11 bomcs incluses -R,, R<sub>5</sub> identiques oum diSerents repre- sentent inddpendamment 3' un ou l<sup>'</sup>autre l'hydrogene ou un atome de fluor (ID) dans leque! n, ont la meme signification que</p> <p>O precedemmenL Ellc conc«erne cgalement Jes compositions pharmaceuliques comprcnant a titre de principe actif ai_j rnoins un de ces com oses ain i e ut s t c e s s e u t e ' ri e t
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3-(Cyclopenten-1-yl)-benzyl-or 3-(cyclopenten-1-yl)-heteroarylmethyl-amine derivatives and use thereof as medicines for treating schizophrenia (Fri, 20 Jan 2006)
<p id="p-0001-en" num="0000">The invention provides compounds of the formula:</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="29.89mm" wi="71.12mm" file="us07163957-20070116-c00001.tif" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> <br/>wherein (a) is a single or double bond; W is CH, CH<sub>2</sub>, CHCH<sub>3</sub>, CCH<sub>3</sub>, C(CH<sub>3</sub>)<sub>2</sub>, C(CH<sub>2</sub>)<sub>2 </sub>or C(CH<sub>2</sub>)<sub>3</sub>, provided that when (a) is a double bond, then W is CH or CCH<sub>3</sub>, and when (a) is a single bond, then W is CH<sub>2</sub>, CHCH<sub>3</sub>, C(CH<sub>3</sub>)<sub>2</sub>, C(CH<sub>2</sub>)<sub>2 </sub>or C(CH<sub>2</sub>)<sub>3</sub>; X is CH or N; and Y is H or F, and salts, hydrates, tautomers, pure enantiomers, and enantiomeric mixtures; and a method of treating schizophrenia comprising administering same.</p>
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NOVEL ARYL-{4-HALO-4-[(HETEROARYLMETHYLAMINO)METHYL]-PIPERIDIN-1-YL}METHANONE DERIVATIVES METHODS FOR PRODUCTION AND USE THEREOF AS MEDICAMENTS (Thu, 29 Dec 2005)
</p> <p>relates to compounds υΓ general <br> formula ( 1 ) in which X and Y = <br> a carbon with a bonded hydrogen <br> (I) atom (CI I) or a nitrogen atom, A <br> = a methyl, fluoromclhy], cyano, <br> hydroxyl, mcthoxy group, or</p> <p>< a chlorine or fluorine atom on <BR> condition that when A = methyl <br> (CH3) and X and Y both = a carbon bonded to a hydrogen atom, then B = a chlorine atom, B = a chlorine or a fluorine atom, D = a hydrogen, chlorine, fluorine atom, or a cyano or irifluoromethyl group and F = a hydrogen, fluorine or chlorine atom. <br>o <br> (57) Abrege : L'inveniion concerne des composes de formule generate ( 1 ) dans laquellc X et Y represenleni un atome de carbone lie a un atome d'hydrogenc (C1 I ) ou un aiome d'azoic ; A represenie un radical melhylc, fluoromelhyle, cyano, hydroxyle, methoxyle, o un aiome de chlore ou un aiome de fluor a la condiiion toutefois, que lorsque A esi un radical melhylc (CI 13), et X el Y represenleni O simullanemenl un aiome dc carbonc lie a un aiome d'hydrogenc, alors, B represenie neccssairement un aiome dc chlore ; B represenie un atome de chlore ou un atome de fluor.D represenie un atome d' hydrogenc, un atome de chlore, un atome de fluor, un groupe cyano ou un rou e trifluoromelh le ; E re resenie un aiome d'b dro ene, de fluor ou de chlore.
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(POLY) AMINOACETAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN THEIR PROCESS OF PREPARATION AND THEIR APPLICATIONS IN THERAPEUTICS AS ANTICANCER AGENTS (Fri, 28 Oct 2005)
The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.
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(POLY)AMINOALKYLAMINOACETAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN, THEIR PROCESS OF PREPARATION AND THEIR APPLICATIONS IN THERAPEUTICS AS ANTICANCER AGENTS (Fri, 28 Oct 2005)
The present invention relates to novel podophyllotoxin derivatives of formula (I), substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents (see formula I) </p>
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IMIDAZOLIC COMPOUNDS AND USE THEREOF AS ALPHA-2 ADRENERGIC RECEPTORS (Thu, 29 Sep 2005)
mula ( 1 ), wherei n: R 1 represents a hydrogen alom, a fluori ne atom <br> or a methoxyl group (OCI L ). the subsli luent R l on (he aromatic <br> carbocycle capable of occupyi ng position 2. 3, 4 or 5 , R2 represents a hydrogen alom or a methyl group, R3 represents a hydrogen atom, a methyl group or an et hyl group, iheir addiiion sai ls and <br> optionally the hydrates of their addiiion sails wi lh pharmaceutically <br> acceptable mineral acids or organic acids as well as the isomers and <br> the tauto ers ihereof.</p> <p>(57) Abrege : L<sup>'</sup>invenlion concerne des composes de formule »e-nerale ( 1 ) dans laquel le - R 1 represen ie un alome d<sup>'</sup> hydrogene, un ato e de tluor ou un groupe methoxyle ( OCH3 ), le subsli iunnl RI sur le carbocycle aromaiique pouvant occuper la position 2, 3, 4 ou 5 ; - R2 represenie un alome d<sup>'</sup>hydrogene ou un groupe methyle ; - R3 represenie un alome d<sup>'</sup> hydrogene, un groupe melhyle ou un groupe eihyle ; leurs sels d<sup>'</sup>addilion et evenluellemenl les hydrates <sup>'</sup>
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1,2,4-TRIAZINES DERIVATIVES, PREPARATION THEREOF AND USE THEREOF IN HUMAN THERAPEUTICS (Fri, 02 Sep 2005)
The invention relates to 3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives of general formulae (I or II), in which in particular: R1 represents hydrogen, a linear or branched C1-C6 alkyl or alkoxy radical, a C5-C6 cycloalkyl radical, a phenyl (C1-C2) alkyl radical or a phenyl radical;-R2 represents hydrogen, a linear or branched Cl-C7 alkyl radical, or a C1-C6 alkyl radical substituted with groups such as trifluoromethyl or phenyl;- linker represents a C2-C6 alkyl chain or -(CH2)n-O- (n = 2 to 5), - R3 represents a group of general formula below for which X = O, linker can be connected to the ortho-, meta- or para-positions of the aromatic of the group R3, R4, R5, R6, R7 and R8 represent hydrogen or fluorine, R9, Rio and R11 represent hydrogen or a linear or branched Cl-C5 alkyl group, in particular R9 and Rio represent the methyl group and R11 represents hydrogen or the ethyl group.
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NOVEL TRICYCLOIMIDAZOLINE DERIVATIVES METHOD FOR PRODUCTION AND USE THEREOF AS MEDICAMENTS (Thu, 01 Sep 2005)
</p> <p>general formula (1) in which Rl = H, F or OCH<sub>3</sub> and <br> may occupy the 2, 3, 4 or 5 position on the aromatic <br> carbocycle, R2 = H or CH<sub>3</sub>, R3 = H, CH<sub>3</sub>, OH or OCH<sub>3></sub> <br> R4 = H and R3 and R4 together can be a carbonyl group <br> (C=0), the addition salts and optionally the hydrates <br> of additional salts with pharmaceutical] y-acceptable <br> mineral or organic acids and the isomers and tautomers <br> thereof.</p> <p>VOIE...PATHWAY
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3β-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof (Fri, 15 Apr 2005)
<p id="p-0001-en" num="0000">The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a bicyclic fused heteroaromatic, such as thieno[2,3-b]pyridine, furo[2,3-b]pyridine, thieno[3,2-b]pyridine, furo[3,2-b]pyridine, thieno[2,3-b]pyrazine, furo[2,3-b]pyrazine, thieno[2,3-c]pyridine, furo[2,3-c]pyridine, thieno[3,2-c]pyridine and furo[3,2-c]pyridine; R1 represents a linear or branched C<sub>1</sub>-C<sub>6 </sub>alkoxy group, a linear or branched C<sub>1</sub>-C<sub>6 </sub>alkylthio group; R2 represents a linear, branched, cyclic C<sub>2</sub>-C<sub>8 </sub>group, a 2- or 3-thienylmethyl group, or a benzyl group optionally substituted by one or several halogens, F, Cl, Br, I, C<sub>1</sub>-C<sub>4</sub>alkyl, C<sub>1</sub>-C<sub>4 </sub>alkoxy, CF3, CN, NO2, OH; and their pharmaceutically acceptable salts. Said compounds are anti-dopaminergic agents.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="19.47mm" wi="66.97mm" file="US07456192-20081125-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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BENZOXATHIEPINE DERIVATIVES AND THEIR USE AS MEDICAMENTS (Thu, 30 Sep 2004)
</p> <p>
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Benzoxathiepine derivatives and their use as medicines (Fri, 02 Jul 2004)
<p id="p-0001-en" num="0000">The invention concerns 3-arylthio-propyl-amino-3,4-dihydro-2H-1,5-aryloxathiepin derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a hydrogen atom, a fluorine atom or a chlorine atom, a hydroxy group, an alkyl, cyclopropyl, alkoxy, cyclopropoxy radical or when they occupy adjacent positions, form with the carbon atoms bearing them a carbon-containing cycle or an oxygen-containing heterocycle with five non-aromatic rings; R3 represents an alkyl radical, a hydroxy group or a methoxy radical; R4 represents a hydrogen atom or a methyl radical; and R5 and R6, identical or different represent a hydrogen atom, an alkyl, alkoxy, alkylthio, alkylamino radical, or the groups OR4 and R5 form with the carbons which bear them a non-aromatic heterocycle with five or six rings containing at least an oxygen atom; and their pharmaceutically acceptable additions salts</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="32.68mm" wi="73.91mm" file="US07109234-20060919-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Synthesis method and intermediates of pyridin-2-yl-methylamine (Fri, 18 Jun 2004)
<p id="p-0001-en" num="0000">The invention concerns a novel method for preparing pyridin-2-yl-methylamine derivatives by reducing amination of cyanohydrins.</p>
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Substituted 1-(piperidin-4-YL)-3-(aryl)-isothioureas, their preparation and therapeutic use (Fri, 23 Jan 2004)
<p id="p-a-0001-en">The invention concerns compounds of formula (I) wherein: R1 and R2, identical or different, represent a saturated or unsaturated alkyl radical, branched or not and containing 1 to 7 carbon atoms; R3 to R8, identical or different, represent a hydrogen, an alkyl branched or not and containing 1 to 5 carbon atoms, an acyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or alkoxy group containing 1 to 5 carbon atoms, a dialkylamino group containing 1 to 5 carbon atoms, a trifluoromethyl or trifluoro methoxyl group; Z represents an oxygen or sulphur atom or methylene; m represents an integer between 0 and 4 inclusively; n represents an integer between 2 and 7 inclusively; and their pure enantiomers and mixtures, the therapeutically acceptable mineral or organic salts of the compounds of formula (I) and their possible hydrates. </p>
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Fluorinated imidazoline benzodioxane, preparation and therapeutic uses thereof (Wed, 27 Aug 2003)
<p id="p-00001-en">The present invention relates to novel fluorinated benzodioxane imidazoline derivatives, to their preparation and to their therapeutic applications.</p> <p id="p-00002-en">The invention is directed more particularly toward the compounds corresponding to the structure of general formula 1:<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06610725-20030826-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry></p> <p id="p-00003-en">in which:</p> <p id="p-00004-en">R represents a linear, branched or cyclized alkyl or alkenyl group containing 1 to 7 carbon atoms, or a benzyl group, and</p> <p id="p-00005-en">the fluorine atom can occupy position 5, 6, 7 or 8, in their racemic form and their dextrorotatory and levorotatory pure enantiomeric forms, and also the addition salts thereof.</p>
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Substitute 1-(piperidin-4-yl)-3-(aryl)-isothioureas, their preparation and therapeutic use (Wed, 25 Jun 2003)
<p id="p-00001-en">The invention concerns compounds of formula (I) wherein: R1 and R2, identical or different, represent a saturated or unsaturated alkyl radical, branched or not and containing 1 to 7 carbon atoms; R3 to R8, identical or different, represent a hydrogen, an alkyl branched or not and containing 1 to 5 carbon atoms, an acyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or alkoxy group containing 1 to 5 carbon atoms, a dialkylamino group containing 1 to 5 carbon atoms, a trifluoromethyl or trifluoro methoxyl group; Z represents an oxygen or sulphur atom or methylene; m represents an integer between 0 and 4 inclusively; n represents an integer between 2 and 7 inclusively; and their pure enantiomers and mixtures, the therapeutically acceptable mineral or organic salts of the compounds of formula (I) and their possible hydrates.<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06583159-20030624-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry></p>
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Substituted 1-(4-piperidyl)-3-(aryl) isothioureas their preparation and their therapeutic application (Wed, 12 Mar 2003)
<p id="p-00001-en"> <chemistry id="chem-us-00001-en"> <img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06531469-20030311-C00001.TIF" img-content="chem" alt="embedded image"/> </chemistry> </p> <p id="p-00002-en">The invention concerns novel substituted N-benzo(thia/oxa)zines-2-yl-1-arylalkyloxyalkyl-4-piperidinamine, their preparation and their therapeutic use. The invention concerns compounds of formula (1) wherein: X represents an oxygen or sulphur atom; Y represents either an alkylene radical, branched or not and containing 2 to 6 carbon atoms or a CH<sub>2</sub>—CH(OH)—CH<sub>2</sub>— radical. R represents a hydrogen, an alkyl radical, branched or not and containing 1 to 7 carbon atoms; R<sub>1</sub>to R<sub>6</sub>, identical or different, represent a hydrogen, a saturated or unsaturated alkyl, branched or not and containing 1 to 5 carbon atoms, a saturated or unsaturated alkyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or acyloxy group comprising 2 to 3 carbon atoms, an alkylamino group containing 1 to 5 carbon atoms, a trifluoro methyl or trifluoro methoxyl group; n is an integer ranging from 1 to 6 inclusively, and their pure, enantiomers or their mixtures, the therapeutically acceptable mineral and organic salts of the compounds of formula (1) and their possible hydrates.</p>
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SUBSTITUTED 1-PIPERIDIN 4 YL 3 ARYL ISOTHIOUREAS THEIR PREPARATION AND THERAPEUTIC USE (Thu, 26 Sep 2002)
<BR></p> <p>The invention concerns compounds of formula (I) wherein: R 1 and R2, identical or different, represent a saturated or unsaturated alkyl radical, branched or not and containing 1 to 7 carbon atoms; R3 to R8, identical or different, represent a hydrogen, an alkyl branched or not and containing 1 to 5 carbon atoms, an acyloxy, branched or not and containing 1 to S carbon atoms, a halogeno, nitro, hydroxy, acyl or alkoxy group containing 1 to 5 carbon atoms, a dialkylamino group containing I to 5 carbon atoms, a trifluoromethy) or trifluoro methoxyl group; Z represents an oxygen or sulphur atom or methylene; m represents an integer between 0 and 4 inclusively; n represents an integer between 2 and 7 inclusively; and their pure enantiomers and mixtures, the therapeutically acceptable mineral or organic salts of the compounds of formula (I) and their possible hydrates.
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Aryl-{4-fluoro-4-[(2-pyridin-2-yl-ethylamino)-methyl]-piperidin-1-yl}-methanone derivatives as 5-ht1 receptor antagonists (Wed, 11 Sep 2002)
<p id="p-00001-en">The invention concerns novel ary1-{4-fluoro-4-[(2-pyridin-2-yl-ethylamino)-methyl]-piperidin-1-yl}-methanone derivatives of formula(1) wherein X is a hydrogen, fluorine or chlorine atom useful as medicines in particular having antidepressant, analgesic, anxiolytic and neuroprotective effects.<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06448268-20020910-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry></p>
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SUBTITUTED 1 4 PIPERIDYL 3 ARYL ISOTHIOUREAS THEIR PREPARATION AND THERAPEUTIC APPLICATION (Thu, 01 Aug 2002)
<BR></p> <p>The invention concerns novel substituted N-benzo(thia oxa)zines-2-yl-l-arylalkyloxyalkyl-4-piperidinamine, their preparation and their therapeutic use. The invention concerns compounds of formula (I) wherein: X represents an oxygen or sulphur atom; Y represents either an alkylene radical, branched or not and containing 2 to 6 carbon atoms or a CH?-CH(OH)-CH2- radical; R represents a hydrogen, an alkyl radical, branched or not and containing 1 to 7 carbon atoms; Ri to RO, identical or different, represent a hydrogen, a saturated or unsaturated alkyl, branched or not and containing I to 5 carbon atoms, a saturated or unsaturated alkyloxy, branched or not and containing I to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or acyloxy group comprising 2 to 3 carbon atoms, an alkylamino group containing 1 to S carbon atoms, a trifluoro methyl or trifluoro methoxyl group; n is an integer ranging from 1 to 6 inclusively; and their pure enantiomers or their mixtures, the therapeutically acceptable mineral and organic salts of the compounds of formula (I) and their possible hydrates.
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[2-substituted-5-[3-thienyl)-benzyl]-2- ([2-isopropoxy-5-fluoro]-phenyoxy)-ethyl]-amine derivatives, method for the production and use thereof as medicaments (Wed, 10 Jul 2002)
<p id="p-00001-en"> <chemistry id="chem-us-00001-en"> <img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06417222-20020709-C00001.TIF" img-content="chem" alt="embedded image"/> </chemistry> </p> <p id="p-00002-en">The present invention relates to novel [(2-substituted-5-[3-thienyl])-benzyl]-[2-([2-isopropoxy-5-fluoro]-phenoxy)-ethyl]-amine derivatives having formula (1) and the use thereof as medicaments, especially anti-psychotic medicaments.</p>
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ARYL 4 FLUORO 4 2 RYRID 2 YLETHYLAMINO METHYL 1 PIPERIDYL METHANONE DERIVATIVES AS 5 HTI RECEPTOR AGONISTS (Thu, 27 Jun 2002)

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Indole derivatives as 5-HT1B and 5-HT1D agonists (Fri, 24 May 2002)
<p id="p-00001-en">The invention concerns novel indole piperazine derivatives of formula (I). It also concerns a method for preparing said compounds and their use as therapeutically active substances, in particular for treating or preventing diseases related to the disfunction of 5-HT<sub>1-like</sub>receptors.</p>
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3-alkoxybenzylamine derivatives and their use as medicines for treating schizophrenia (Wed, 27 Feb 2002)
<p id="p-00001-en">The present invention relates to novel 3-alkoxybenzylamine derivatives of general formula (1):<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06350913-20020226-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry></p> <p id="p-00002-en">which are useful as medicinal products and in particular as antipsychotic agents.</p>
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NOVEL 3 ALKOXYBENZYLAMINE DERIVATIVES AND THEIR USE AS MEDICINAL PRODUCTS FOR TREATING SCHIZOPHRENIA (Thu, 01 Nov 2001)
</p> <p>The present invention relates to novel 3-alkoxybenzylamine derivatives of general formula (1): <br> <BR> <br> formula 1 <br>which are useful as medicinal products and in particular as antipsychotic agents.
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3-oxo-2(H)-1,2,4-triazine derivatives as ligands of 5 HT1A receptors (Wed, 17 Oct 2001)
<p id="p-00001-en">The invention concerns novel 3-oxo-(2H)-1,2,4-triazine derivatives of general formula (I) in which R<sub>1</sub>represents: hydrogen, when A is an optionally substituted nitrogen atom; a linear or branched<sub>1</sub>-C<sub>4</sub>alkyl group; a C<sub>1</sub>-C<sub>4</sub>phenyl alkyl group, the phenyl ring being optionally substituted by one or several groups such as C<sub>1</sub>-C<sub>4</sub>alkyl, C<sub>1</sub>-C<sub>3</sub>alkoxy, halogen, trifluoromethyl. R<sub>2</sub>represents: hydrogen; a linear or branched C<sub>1</sub>-C<sub>4</sub>alkyl radical; a C<sub>1-C</sub><sub>4</sub>phenyl or phenylalkyl group, the phenyl ring being optionally substituted by one or several groups such as C<sub>1</sub>-C<sub>4</sub>alkyl, C<sub>1</sub>-C<sub>3</sub>alkoxy, halogen, trifluoromethyl. A represents an oxygen atom or a nitrogen atom optionally NR<sub>3</sub>substituted. R<sub>3</sub>represents hydrogen or a methyl group. B represents a group such as (IIa) in which Ar itself represents an aromatic structure such as phenyl, pyridyl or pyrimidyl, optionally substituted by one or several groups such as C<sub>1</sub>-C<sub>3</sub>alkyl, C<sub>1</sub>-C<sub>3</sub>alkoxy, hydroxy, trifluoromethyl or halogen and n can be whole numbers ranging between 3 and 5; (IIb) in which Ar is as defined in formula (IIa) and m can be a whole number ranging between 1 and 2; (IIc) in which R<sub>4</sub>represents hydrogen or a C<sub>1</sub>-C<sub>3</sub>alkyl group and n can be whole numbers ranging between 3 and 5.<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06303603-20011016-C00001.TIF" img-content="chem"/></chemistry></p>
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Indole derivatives as 5-HT1B and 5-HT1D agonists (Wed, 22 Aug 2001)
<p id="p-00001-en">The invention concerns novel indole piperazine derivatives of Formula (I):<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06277853-20010821-C00001.TIF" img-content="chem"/></chemistry></p> <p id="p-00002-en">It also concerns a method for preparing said compounds and their use as therapeutically active substances, in particular for treating or preventing diseases related to the dysfunction of 5 -HT<sub>1-like</sub>receptors.</p>
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Cyclohexane derivatives difunctionalised in 1,4 as ligands of 5T H1A receptors (Wed, 21 Feb 2001)
<p id="p-00001-en"> <chemistry id="chem-us-00001-en"> <img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06191130-20010220-C00001.TIF" img-content="chem"/> </chemistry> </p> <p id="p-00002-en">The invention concerns novel cyclohexane derivatives difunctionalised in 1.4 of general formula (1) in which A represents a group such as (IIa) in which Ar itself represents an aromatic structure such as phenyl or pyrimidinyl optionally substituted by one or several groups such as C<sub>1</sub>-C<sub>3</sub>alkyl, C<sub>1</sub>-C<sub>3</sub>alkoxy, trifluoromethyl or halogen (IIb); B represents a heterocyclic group such as: 3,5-dioxo-(2H,4H)-1,2,4 triazine substituted in position 2 (IIIa); 3-oxo-(2H)-1,2,4 triazine substituted in position 5 (IIIb); 3,5-dioxo-6-amino-(2H,4H)-1,2,4-triazine (IIIc) in which R represents a C<sub>1</sub>-C<sub>3</sub>alkyl group. The invention also concerns the salts of compounds of general formula I with pharmaceutically acceptable acids. It also concerns the various “cis” and “trans” isomers and the various enantiomers with asymmetric carbons.</p>
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Methanesulphonate salt of an arylpiperazine derived from tryptamine and its solvates for pharmaceutical use (Wed, 30 Aug 2000)
<p>The invention discloses the methanesulphonate salt of 4-(4-[2-[3-(2-amino-ethyl)-1H-indol-5-yloxy]-acetyl]-piperazin-1-yl)-benzo nitrile, its solvates or hydrates as well as the preparation of the said salt. The invention also discloses the pharmaceutical compositions containing the said salt, useful in the preparation of medicines for treating vasospastic disorders.</p>
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Water-soluble derivatives of epipodophyllotoxin, process for their preparation, their use as medicinal products and their intended use in anti-cancer treatments (Wed, 23 Aug 2000)
<p>Water-soluble derivatives of epipodophyllotoxin, process for their preparation and their use for the treatment of rheumatoid arthritis, complaints caused by human papilloma virus and cancer.</p>
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Pyridin-2-yl-methylamine derivatives, method of preparing and application as medicine (Wed, 02 Feb 2000)
<p>The invention concerns novel pyridin-2-yl-methylamine derivatives of formula (I): ##STR1## in which: u represents hydrogen or methyl; PA1 v represents hydrogen, chlorine, or methyl; PA1 w represents hydrogen, fluorine, or methyl; PA1 x represents hydrogen or fluorine; PA1 y represents chlorine or methyl; PA1 z represents hydrogen, fluorine, chlorine, or methyl; PA1 A represents hydrogen, fluorine, chlorine, C.sub.1 -C.sub.5 alkyl, fluoroalkyl, cyclopropyl, a 5-membered aromatic heterocyclic group, alkoxy or alkythio, amino, cyclic amino, or alkoxycarbonyl. These compounds are useful as medicines, in particular as antidepressants or analgesics.</p>
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Heterocyclic compounds for treating myocardial ischemia (Wed, 05 Jan 2000)
<p>Substituted N-heterocyclyl-1-aryloxyalkyl-4-piperldineamines of formula (I) ##STR1## wherein each of R.sub.1 to R.sub.4, which are the same or different, is hydrogen, optionally branched C.sub.1-4 alkyl, optionally branched C.sub.1-4 alkyloxy, halo, nitro, hydroxy, or trifluoromethyl or trifluoromethoxyl; R.sub.5 is hydrogen, optionally branched C.sub.1-6 alkyl, optionally branched C.sub.7-12 phenylalkyl optionally substituted on the phenyl by one or more radicals having the same definition as R.sub.1 ; W and X are oxygen or sulphur; Y is C.sub.2-6 polymethylene or --CH.sub.2 --CH(OH)--CH.sub.2 --; and n is 0 or 1; and pure R or S isomers of said compounds, where applicable, as well as mixtures thereof, as well as therapeutically-acceptable organic or inorganic salts and hydrates of the compounds and a method for preparing the compounds and their use as drugs are all disclosed.</p>
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3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives (Wed, 03 Nov 1999)
<p>Novel 3,5-dioxo-(2H,4H-triazine derivatives of general formula (I): wherein R.sub.1 is hydrogen, a C.sub.1 -C.sub.4 alkyl radical, phenyl C.sub.1 -C.sub.4 alkyl or phenyl, the phenyl ring being optionally substituted by one or more groupings such as (C.sub.1 -C.sub.3) alkyl, hydroxyl, trifluoromethyl or halogen: R.sub.2 is hydrogen or a (C.sub.1 -C.sub.4) alkyl radical, n can be an integer from 2 to 6; A is a grouping of the aryl piperazino or benzodioxanyl-methylamino or pyridodioxanyl-methylamino type. The invention also concerns a method of preparing said derivatives and pharmaceutical compositions comprising at least one of the compounds of general formula (I) as the active ingredient: ##STR1##</p>
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Naphthamide derivatives of 3-beta-amino azabicyclo octane or nonane as neuroleptic agents (Wed, 29 Sep 1999)
<p>The invention pertains to novel azabicyclo-naphthalene-carboxamide derivatives, a method for preparing same and the use thereof as a medicament. The compounds of the invention are of formula (I). ##STR1##</p>
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Method for preparing an optically pure benzofuran carboxylic acid and use thereof for preparing efaroxan (Wed, 10 Mar 1999)
<p>A method for preparing an optically pure 2-ethyl-2,3-dihydrobenzofurancarboxylic acid of formula II wherein R is a hydrogen atom, halogen, lower alkyl, lower alkoxy or hydroxy is described. ##STR1## The method comprises separating the racemic mixture by selective crystallization with the suitable optically pure enantiomer of 2-phenylglycinol, in a suitable solvent, whereafter the optically pure, crystallized acid of formula II is isolated and recovered. The invention also provides the optically pure 2-ethyl-2,3-dihydro-benzofurancarboxylic acid derivative thus obtained and the use thereof for the preparation of an optically pure derivative of efaroxan.</p>
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Aromatic ethers derived from indoles which are useful as medicaments (Wed, 23 Dec 1998)
<p>The present invention relates to new aromatic ethers derived from indole and having general formula (I) as well as to their preparation methods, pharmaceutical compositions containing them and their utilization as a medicament for the treatment of diseases linked to the dysfunction of the 5HT.sub.1 -like receptors. ##STR1##</p>
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Piperazides derived from arylpiperazine, processes for their preparation, their use as medicaments and pharmaceutical compositions comprising them (Wed, 05 Aug 1998)
<p>Novel 5HT receptor antagonists of general formula (I) ##STR1## in which Ar.sub.1 and Ar.sub.2 are aromatic residues, X is O, NH, CH.sub.2 O, or CH.sub.2 NH, and R.sub.1 is hydrogen or linear or branched alkyl comprising 1-6 carbon atoms, as well as their salts, hydrates, solvates, and physiologically-acceptable bioprecursors for their therapeutic use, their geometric and optical isomers, and their mixtures in all proportions and in racemic form, methods for the preparation of these novel antagonists, and their use in the treatment of a living animal and pharmaceutical compositions comprising them.</p>
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Biodegradable, controlled-release microspheres and process for preparing them (Wed, 01 Apr 1998)
<p>Method for the preparation of a pharmaceutical composition in the form of microspheres controllably releasing at least one water-soluble active ingredient. The method comprises the steps of dissolving the active ingredient in a suitable quantity of water, emulsifying the aqueous solution containing the active ingredient with a solution of at least a dl-lactide-co-glycolide-type matrix copolymer in chlorinated hydrocarbon also containing a low molecular weight polyactide release-modulating agent, which results in a first microfine and homogeneous emulsion; emulsifying the first emulsion thus obtained in an external aqueous phase containing a surface active agent; and removing and evaporating the solvent to produce microspheres which are recovered after filtering, washing, and drying. The microspheres themselves.</p>
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Indole-derived arylpiperazines as ligands for 5HT.sub.1 -like, 5HT.sub.1B and 5HT.sub.1D receptors (Wed, 11 Mar 1998)
<p>Novel indole-derived azylpiperazines of general formula (I), wherein, inter alia, R.sub.1 is NH.sub.2 or NO.sub.2, R'.sub.1, R.sub.2, R'.sub.2, R.sub.3 and R.sub.4 are H, Z is --C-- and X is 0. Methods for preparing such derivatives and the therapeutical uses thereof are also disclosed.</p>
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Etoposide derivatives, process for preparing them, their use as a medicinal product and their use for the preparation of a medicinal product intended for anti-cancer treatment (Wed, 02 Jul 1997)
<p>Compound of the formula (I) in which R' is a hydrogen atom or a radical R and R is an acyl residue. The invention also concerns the use of said compounds in the treatment of cancer and pharmaceutical compositions comprising said compounds. ##STR1##</p>
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1,2-dihydro-2-oxo-3-aminoquinoxaline derivatives, their preparation and their therapeutic application (Wed, 28 May 1997)
<p>1,2-dihydro-2-oxo-3-amino-quinoxaline derivatives of general formula (I) in which R.sub.1 and R.sub.2 are independently hydrogen or a straight or branched C.sub.1 -C.sub.4 alkyl radical, R.sub.3 is a straight or branched C.sub.3 -C.sub.6 alkyl, alkenyl or hydroxy-alkyl grouping, their salts with pharmaceutically-acceptable acids, and a method for preparing them and their use in therapy are disclosed.</p>
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Antimitotic binary alkaloid derivatives from catharanthus roseus (Wed, 16 Apr 1997)
<p>Novel fluorinated derivatives of the vinblastine and vinorelbine family of general formula (1), ##STR1## wherein the symbols have the meanings indicated in the Specification and Claims, and the therapeutically-acceptable salts of these molecules, as well as pharmaceutical compositions thereof. The invention also concerns the application of said compounds in the treatment of a cancer pathology and their methods of preparation.</p>
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3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives as 5HT.sub.1A ligands (Wed, 08 Jan 1997)
<p>A 3,5-dioxo-(2H,4H)-1,2,4-triazine compounds of formula I ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, represent hydrogen or C.sub.1 -C.sub.6 alkyl, n is 2 to 6, inclusive, PAL A represents aryl piperazino II ##STR2## the Ar grouping representing phenyl, naphthyl, pyrimidyl, or pyridyl, unsubstituted or substituted by C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, hydroxy, trifluoromethyl, or halogen, or III benzodioxanyl-methyl-amino or pyridodioxanyl-methyl-amino ##STR3## in which R represents hydrogen or C.sub.1 -C.sub.3 alkyl and X represents a nitrogen or carbon atom, therapeutically-acceptable salts and enantiomers thereof, pharmaceutical compositions thereof, and method for treatment of diseases requiring a 5HT.sub.1A receptor agonist therewith.</p>
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Sulfonamides derived from benzocyclic or benzoheterocyclic acids, their preparation and application in therapeutics (Wed, 01 Feb 1995)
<p>The invention relates to new sulphonamide derivatives of benzo-cyclic or benzo-heterocyclic acids and their derivatives of general formula I ##STR1## in which: R represents a straight-chain or branched lower alkyl radical having 1 to 9 C; PAL a phenyl radical which is unsubstituted or substituted by one or more groups: PA1 straight-chain or branched lower alkyl having 1 to 4 C, halogeno, alkoxy, nitro, amino, dialkylamino or CF.sub.3 ; PA1 a substituted or unsubstituted naphthalene; PA1 a thiophenyl radical; PA1 R.sub.1 represents a hydrogen or a straight-chain or branched lower alkyl or a benzyl; PA1 R.sub.2 represents a hydrogen, a straight-chain or branched lower alkyl group, a substituted or unsubstituted phenyl group or an aralkyl group; PA1 R.sub.3 represents a hydrogen or a straight-chain or branched lower alkyl (1 to 6 C); PA1 --X-- represents a divalent functional radical chosen from the following: --CH.sub.2 --; ##STR2## where R.sub.4 =H or Me; A represents a benzo-cyclic or benzo-heterocyclic divalent radical chosen from the following (a) to (j): ##STR3## and n can assume the values 1 to 4 inclusive; and the therapeutically acceptable organic or inorganic salts (R.sub.3 =H), the pure isomers or diastereoisomers or their mixture and all the pharmaceutical compositions of formula I with other active principles. PAL The invention relates to the application of I as a medicament and the preparation processes.</p>
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2",3",4'-tri(acetyl)-4",6"-ethylidine-.beta.-D-glucopyranosides, their preparation and their use for the preparation of 4'-demethylepipodophyliotoxing ethylidene-.beta.-D-glucopyranoside (Wed, 01 Feb 1995)
<p>The invention relates to 2",3",4'-tris(acetyl)-4",6"-ethylidene-.beta.-D-glucopyranosides, their preparation and their use for the preparation of 4'-demethylepipodophyllotoxin ethylidene-.beta.-D-glucopyranoside. The compounds of the invention are of the formula ##STR1## Their process of preparation comprises the following stages: acylation of a glycosyl derivative PAL acylation of an aglycone PAL coupling of the acylated glycosyl derivative and the acylated aglycone, in the presence of a Lewis acid, the acylation being carried out using an acid chloride, which is optionally identical for the two stages of acylation, in which the carbon in .alpha. of the carbonyl function bears at least one heteroatom chosen from among O and S.</p>
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CARPAINE DERIVATIVES (Thu, 29 Dec 1994)
New carpaine derivatives corresponding to the general formula:</p> <p> <BR></p> <p>2 <br>in which: <br> A represents <br> either a direct bond; <br> or a chain -(CH<sub>2</sub>)<sub>n</sub>-, where n can assume the values 1, 2 or 3; <br> or a chain -CH<sub>2</sub>-X- , where Z represents an oxygen atom or a sulphur atom, <br> Aryl represents a phenyl, naphthyl, furyl, thienyl, benzofuranyl or benzothienyl ring-system; it being possible for these ring-systems to be unsubstituted or substituted with one or more substituents chosen from a halogen atom, a C<sub>x</sub>-C<sub>4</sub> alkyl group, a C<sub>1</sub>-C<sub>4</sub> al oxy group, a nitro group, a cyano group, a trifluoromethyl group or a trifluoromethoxy group; as well as the therapeutically acceptable salts of these molecules . <br> The invention also relates to the use of these compounds in therapy and to the preparation processes.
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NOVEL 2-PHENOXYETHYLAMINE DERIVATIVES,THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS (Thu, 01 Dec 1994)
2-phenoxyethylamine derivatives corresponding to the general formula 1:</p> <p> <BR> <br> 1</p> <p>and also the therapeutically acceptable salts of those molecules .</p> <p>The invention relates also to the application of the compounds of the general formula 1 in therapeutics and to processes for their preparation.
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NEW HETEROCYCLIC 4-(AMINOMETHYL) PIPERIDINE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPEUTICS (Thu, 27 Oct 1994)
Heterocyclic derivatives of 4-aminomethy1-piperidine corresponding to the general formula 1:</p> <p> <BR> <br> 1</p> <p>as well as the therapeutically acceptable salts of these molecules. <br> The invention also relates to the application of the compounds of general formula 1 in therapeutics and to the processes for their preparation.
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New urea derivatives, their preparation and their application in therapy (Wed, 23 Feb 1994)
<p>New urea derivatives corresponding to the general formula 1 ##STR1## in which: R.sup.1 represents a C.sub.1 -C.sub.4 alkyl group; PA0 R.sup.2 represents: PA1 a C.sub.5 -C.sub.7 cycloalkyl group PA1 a cycloalkylmethyl group in which the cycloalkyl radical contains from 5 to 7 carbon atoms PA1 a benzyl group PA1 a benzyl group in which the aromatic ring bears a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a halogen atom or a nitro group; PA1 A represents an oxygen atom or a methylene radical; PA1 n represents 1 or 2; PA0 X represents an oxygen or sulfur atom; PA0 B represents a direct bond, a methylene radical or a carbonyl radical; PAL as well as the therapeutically acceptable salts of these molecules. PAL The invention also relates to the application of the compounds of general formula 1 in therapy, and to the preparation processes.</p>
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Derivatives of 4-aminomethylpiperidine, their preparation and their use as therapeutics (Wed, 16 Feb 1994)
<p>The application discloses pharmacologically-active derivatives of 4-aminomethyl piperidine having the general formula 1 ##STR1## wherein the symbols have the meanings set forth in the Specification, as well as pharmaceutically-acceptable acid addition salts thereof, the use of the compounds as serotoninergic receptor ligands and for the treatment of anxiety, depression, and other related serotoninergic system disorders, pharmaceutical compositions thereof, and a method for their preparation.</p>
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3-hydroxy-substituted-1-phenyl-1,4-dihydro-4-oxopyridazines and derivatives, and use (Wed, 20 Oct 1993)
<p>The application discloses pharmacologically-active 3-hydroxy-1-phenyl-1,4-dihydro-4-oxopyridazine compounds, derivatives thereof, a method for the preparation thereof, pharmaceutical compositions thereof, and a method of treating anxiety and other physiological abnormalities therewith.</p>
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Derivatives of 1-phenyl 1,4-dihydro 3-amino 4-oxo pyridazines, their preparation and their use in therapy (Wed, 23 Oct 1991)
<p>The present invention relates to derivatives of 1-phenyl 1,4-dihydro 3-amino 4-oxo pyridazines of the general formula I: ##STR1## and the production thereof. It also concerns pharmaceutical compositions comprising as active principle a compound of general formula I and use thereof for treatment of central nervous system disturbances, especially as an anxiolytic.</p>
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NEW SULPHONAMIDES DERIVED FROM BENZO-CYCLIC OR BENZO HETEROCYCLIC ACIDS,THEIR PREPARATION AND THEIR APPLICATION IN THERAPY (Thu, 31 Jan 1991)
The invention relates to new sulphonamide derivatives of benzo-cyclic or benzo-heterocyclic acids and their derivatives of general formula I</p> <p> <BR> )<sub>n</sub>-X-A-COOR<sub>3</sub> I <br> In which: <br> R represents a straight-chain or branched lower alkyl radical having 1 to 9 C; <br>a phenyl radical which is unsubstituted or substituted by one or more groups: <br>straight-chain or branched lower alklyl having 1 to 4 C, halogeno, alkoxy, nitro, amino, dialkylamino or CF<sub>3</sub>; <br>a substituted or unsubstituted naphthalene; <br>a thiophenyl radical; <br> R<sub>x</sub> represents a hydrogen or a straight-chain or branched lower alkyl or a benzyl; <br> R<sub>2</sub> represents a hydrogen, a straight-chain or branched lower alkyl group, a substituted or unsubstituted phenyl group or an aralkyl group; <br> R<sub>3</sub> represents a hydrogen or a straight-chain or branched lower alkyl (1 to 6 C); <br> - X - represents a divalent functional radical chosen from the following: -CH<sub>2</sub>-; -CH-OR^; -C=0; -C=N-OR«; and -C=N-W-R<sub>4</sub> where R„=H or Me; '</p> <p>A represents a benzo-cyclic or benzo-heterocyclic divalent radical chosen from the following (a) to (j):
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5-monoaryl as.-triazin-3-ones substituted in 2-position, and their use as medicaments (Wed, 26 Jul 1989)
<p>The present invention concerns new 5-monoaryl as.-triazin-3-ones substituted in 2-position, a method of preparing them, and their use as medicaments. PAL The compounds according to the present invention have general formula (I) ##STR1## in which: the bond represented by a dashed line indicates the presence of an optional double bond; PA0 A represents a direct N--C bond, a straight or branched C.sub.1 to C.sub.5 alkylene, possibly substituted one or more times by --COOR' or by Ar; PA0 R represents --H, --OH, ##STR2## R' represents --H, --OH, straight or branched C.sub.1 to C.sub.7 alkyl, --NH.sub.2 ; PA0 Ar represents an aromatic ring having 5 or 6 members possibly containing a heteroatom such as O, N, S and possibly substituted one or more times by a radical selected from among --OH, C.sub.1 to C.sub.4 alkyl, C.sub.1 and C.sub.4 alkoxy, halogen, --CF.sub.3, acetonyloxy, ##STR3## and .gamma.-butyrolactone; as well as their pharmaceutically acceptable salts.</p>
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ETHERS OF 2 [2-(2-HYDROXY-1,4- BENZODIOXANYL)]-2-IMIDAZOLINE, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL PREPARATION CONTAINING (Fri, 01 Aug 1986)

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2-[2-(2,3-DIHYSROBENZOFURANYL)]-2- IMIDAZOLINE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL PREPARATIONS CONTAINING (Sat, 31 Aug 1985)

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2-2-(1,4-BENZDIOXANYL)-2- IMIDAZOLINE AND NON-TOXIC SALTS THEREOF, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUT (Fri, 01 Feb 1985)

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