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Chemical compounds, their preparation and use (Thu, 25 May 1995)
A compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein X is halogen, amino, perhalomethyl, cyano, C¿1-6?-alkoxy, C¿1-6?-alkylthio or C¿1-6?-alkylamino; A is methyl, halomethyl, cyanomethyl, aminomethyl, vinyl, methylthiomethyl or methoxymethyl; R?1¿ is selected from optionally substituted $i(N)-bonded heterocyclics. The compounds have been found useful for treating central nervous system ailments.
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NOVEL HETEROCYCLIC CARBOXYLIC ACIDS (Wed, 28 Apr 1993)
This compound has the general formula I wherein Y is -CH2-CH(R1)(R2), -CH=C(R1)(R2) or -CH-N(R1)(R2) wherein R1 and R2 are optionally substituted C3-8 cycloalkyl, phenyl or thienyl; s is 1,2 or 3; X is -CH2-, -O- or -N(R3)- (wherein R3 is H or C1-6 alkyl); r is 2, 3 or 4; R4 and R5 each represents hydrogen or may together be a bond and R6 is OH or C1-8 alkoxy provided that X is not -CH2- when Y is -CH2-CH(R1)(R2) or -CH=C(R1)(R2) or a geometric or optical isomer thereof or a pharmaceutically acceptable salt thereof. A process for preparing a compound of formula I is claimed. A pharmaceutical composition containing a compound of formula I useful in treating a central nervous system ailment related to GABA uptake is claimed.
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3,4-DIHYDRO-1H-ISOQUINOLINE-2-CARBOXYLIC ACID 5-AMINOPYRIDIN-2-YL ESTERS (Thu, 24 Aug 2006)
Novel compounds of formula (I), pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.
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Chemical compounds, their preparation and use (Mon, 24 Mar 1997)

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3,4-dihydro-1H-isoquinoline-2-carboxylic acid 5-aminopyridin-2-yl esters (Thu, 19 Jul 2007)
Novel compounds of formula (I), pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.
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HETEROCYCLIC COMPOUNDS AND THEIR PREPARATION AND USE (Wed, 27 Jan 1993)
Psychopharmaceutical imidazoquinoxaline compounds have the formula wherein Q is -COCHR2COR1; R1 and R2 independently are hydrogen, straight or branched C1-6-alkyl, or C3-7-cycloakyl; R3 is hydrogen, straight or branched C1-6-alkyl, straight or branched C2-6-alkenyl, or aralkyl or aroylalkyl which may optionally be substituted with halogen or C1-6-alkoxy; R4 and R5 independently are hydrogen, halogen, C1-6-alkyl or trifluoromethyl.
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CRYSTALLINE R- GUANIDINES, ARGININE OR (L) -ARGININE (2S) -2- ETHOXY -3-{4- [2-(10H -PHENOXAZIN -10-YL)ETHOXY]PHENYL}PROPANOATE (Thu, 26 Oct 2000)
The present invention relates to crystalline R- guanidines of (2S) -2- Ethoxy-3- {4-[2- (10H -phenoxazin -10-yl) ethoxy]phenyl} propanoate, its preparations and its use as therapeutic agents. More specifically the present invention relates to crystalline Arginine (2S) -2- Ethoxy-3- {4-[2- (10H -phenoxazin -10-yl) ethoxy] phenyl} propanoate, preferably (L)- Arginine (2S) -2- Ethoxy-3- {4-[2- (10H -phenoxazin -10-yl) ethoxy] phenyl} propanoate, its preparation and its use as therapeutic agent.
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NOVEL AMINOAZETIDINE, -PYRROLIDINE AND -PIPERIDINE DERIVATIVES (Thu, 27 Mar 2003)
Novel aminoazetidine, -pyrrolidine, and -piperidine derivatives of the general formula (I): use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
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SUBSTITUTED PIPERIDINES WITH SELECTIVE BINDING TO HISTAMINE H3-RECEPTOR (Thu, 27 Mar 2003)
A novel class of substituted piperidines, of formula I pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.
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SUBSTITUTED HEXAHYDROPYRROLO[1,2-A]PYRAZINES, OCTAHYDROPYRIDO[1,2-A]PYRAZINES AND DECAHYDROPYRAZINO[1,2-A]AZEPINES (Thu, 18 Dec 2003)
Novel substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
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NOVEL GLUCAGON ANTAGONISTS (Thu, 08 Jul 2004)
Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.
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Novel heterocyclic compounds (Fri, 30 Nov 2001)
Patent 277763 Compounds of formula I wherein, R1 and R2 are independently hydrogen, halogen, trifluoromethyl, C1-6 -alkyl or C1-6 -alkoxy; Y is >N-CH2-, >CH-CH2- or >C=CH- wherein only the bolded atom participates in the ring system; X is ���O-, -S-, -CR7R8-, -CH2CH2-, -CH=CH-CH2-, -CH2-CH=CH, -CH2CH2CH2-, -CH=CH-, NR9-(C=O)-, -O-CH2-, -(C=O)- or ���(S=O)- wherein R7, R8 and R9 are independently hydrogen or C1-6-alkyl; r is 1, 2, or 3; m is 1 or 2; n is 1 when m is 1 and n is 0 when m is 2; R4 and R5 are hydrogen when m is 1; R4 and R5 are hydrogen or form a bond when m is 2; and R6 is OH or C1-8 -alkoxy; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds 10-(3-(3-carbomethoxy-1-piperidyl)propyl)phenothiazine and 10-(3-(3-carbohexoxy-1-piperidyl)propyl)phenthiazine are not included. These compounds are useful in treating neurogenci inflammation, diabetic neuropathy and rheumatoid arthritis.
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NOVEL GLUCAGON ANTAGONISTS/INVERSE AGONISTS (Thu, 08 Jan 2004)
Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.
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SUBSTITUTED PIPERIDINES AND THEIR USE FOR THE TREATMENT OF DISEASES RELATED TO THE HISTAMINE H3 RECEPTOR (Thu, 17 Apr 2003)
A novel class of substituted piperidines, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of diseases and dis-orders in which an interaction with the histamine H3 receptor is beneficial.
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AMIDES OF AMINOALKYL-SUBSTITUTED AZETIDINES, PYRROLIDINES, PIPERIDINES AND AZEPANES (Thu, 07 Aug 2003)
Novel amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
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A MODIFIED POLYPEPTIDE (Thu, 07 Jan 1999)
The present invention relates to modified polypeptides with reduced respiratory allergenicity having coupled polymeric molecules with a molecular weight from 100 up to 750 Da, covalently to the parent polypeptide having a molecular weight from 5 to 100 kDa, industrial composition comprising modified polypeptide with reduced respiratory allergenicity, skin care products, the use of modified polypeptides for reducing the allergenicity of industrial composition and products and finally a method for reducing the allergenicity of polypeptides.
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PYRIDAZINYL- PIPERAZINES AND THEIR USE AS HISTAMINE H3 RECEPTOR LIGANDS (Thu, 03 Feb 2005)
The present invention relates to piperazines of formula I. The compounds show a high and selective binding affinity for the histamine H3 receptor, indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases or disorders related to the histamine H3 receptor.
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HETEROCYCLIC COMPOUNDS AND THEIR PREPARATION AND USE (Fri, 24 Feb 1995)
The specification relates to compounds of formulae where R1 and R2 are independently hydrogen, alkyl, halogen, NO2, NH2, CN, CF3, SO2NR4R5 where R4 and R5 are independently hydrogen or alkyl, or COR6 where R6 is alkyl; and R3 is hydrogen, alkyl or CF3; and pharmaceutically acceptable salts thereof, with the proviso that the compound [1,2,4]triazolo[4,3-a]quinoxaline-1,4(2H,5H)-dione is excluded. The compounds are useful in treating indications related to hyperactivity of excitatory neurotransmitters.
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[1,2,4]triazolo[4,3-a]quinoxaline compounds, their preparation and use (Mon, 24 Nov 1997)
[1,2,4]triazolo[4,3-a]quinoxaline derivatives of general formula (I) wherein one of R1 and R2 is a 5- or 6-membered N-containing heterocyclic ring optionally substituted, or a fused ring system comprising a 5- or 6-membered N-containing heterocyclic ring optionally substituted; and the other of R1 and R2 is H, alkyl, alkoxy, halogen, NO2, NH2, CN, CF3, COC1-6-alkyl or SO2NR'R'', wherein R' and R'' are independently H or alkyl and X is O or S; and pharmaceutically acceptable salts thereof have affinity for the AMPA receptors and are antagonists in connection with this type of receptors which makes them useful in the treatment of CNS ailments, especially in the treatment of any of the numerous indications caused by hyperactivity of excitatory amino acids.
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HISTS1MINE H3 RECEPTOR ANTAGONISTS (Thu, 11 Jan 2007)
Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.
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