MACROCYCLIC KINASE INHIBITORS (Fri, 04 Oct 2013)
<p id="p-0001" num="0000">Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.03mm" wi="55.54mm" file="US20130261086A1-20131003-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

PREPARATION OF C-PYRAZINE-METHYLAMINES (Fri, 04 Oct 2013)
<p id="p-0001" num="0000">A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3-dichloropyrazine with a suitable diaryl imine followed by hydrolysis.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.27mm" wi="50.21mm" file="US20130261306A1-20131003-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

FUSED BICYCLIC KINASE INHIBITORS (Fri, 27 Sep 2013)
<p id="p-0001" num="0000">Compounds of Formula I, as shown below and defined herein:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.71mm" wi="69.34mm" file="US20130253197A1-20130926-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of RON, MET or ALK. This Abstract is not limiting of the invention.</li> </ul> </li> </ul> </p>
>> read more

AMINO PYRIMIDINE ANTICANCER COMPOUNDS (Fri, 06 Sep 2013)
<p id="p-0001" num="0000">Compounds of Formula 1, as shown below and defined herein:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.38mm" wi="59.94mm" file="US20130231306A1-20130905-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.</li> </ul> </li> </ul> </p>
>> read more

6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors (Fri, 26 Jul 2013)
<p id="p-0001" num="0000">Compounds of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.40mm" wi="49.28mm" file="US08653268-20140218-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">and pharmaceutically acceptable salts thereof, wherein X<sub>1</sub>, X<sub>2</sub>, X<sub>3</sub>, X<sub>4</sub>, X<sub>5</sub>, X<sub>6</sub>, X<sub>7</sub>, R<sup>1</sup>, and Q<sup>1 </sup>are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.</li> </ul> </li> </ul> </p>
>> read more

PROTON NMR SPECTROSCOPY FOR BIOCHEMICAL SCREENING (Fri, 31 May 2013)
High-Throughput Screening (HTS) of large compound libraries is the method of choice for discovery of lead compounds for drug development. The present invention provides novel, sensitive and broadly applicable NMR screening methods in which the H8 signal of a purine-containing substrate or product, or the H6 signal of a pyrimidine-containing substrate or product, is used to monitor enzymic reactions that utilize such substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of the NMR method to the assay of the enzymes creatine kinase and phosphodiesterase 2A is presented. The methods are applicable to any of a multitude of enzymes that utilize purine nucleoside substrates (e.g. ATP, GTP) or pyrimidine nucleoside substrates (e.g. CTP, UDP-GlcNac), including protein kinases, GTPases, and lipid kinases.
>> read more

DIHYDROPTERIDINONES (Fri, 17 May 2013)
Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention.
>> read more

FUSED BICYCLIC KINASE INHIBITORS (Fri, 23 Nov 2012)
Compounds of Formula (I), pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of MET, RON, ALK, IR, or IGF-1R. This Abstract is not limiting of the invention.
>> read more

Combined treatment with an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors (Fri, 17 Aug 2012)
<p id="p-0001" num="0000">The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein said agent is an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases. The present invention also provides a pharmaceutical composition comprising an EGFR kinase inhibitor and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing the methods of this invention is the compound erlotinib HC1 (also known as TARCEVA®).</p>
>> read more

MACROCYCLIC KINASE INHIBITORS (Fri, 08 Jun 2012)
Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.
>> read more

6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors (Fri, 30 Mar 2012)
<p id="p-0001" num="0000">Compounds of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.40mm" wi="49.28mm" file="US08367826-20130205-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">and pharmaceutically acceptable salts thereof, wherein X<sub>1</sub>, X<sub>2</sub>, X<sub>3</sub>, X<sub>4</sub>, X<sub>5</sub>, X<sub>6</sub>, X<sub>7</sub>, R<sup>1</sup>, and Q<sup>1 </sup>are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.</li> </ul> </li> </ul> </p>
>> read more

7-aminofuropyridine derivatives (Fri, 24 Feb 2012)
<p id="p-0001" num="0000">Compounds of Formula 1, as shown below and defined herein:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.52mm" wi="52.75mm" file="US08378104-20130219-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.</li> </ul> </li> </ul> </p>
>> read more

Preparation of <i>C</i>-pyrazine-methylamines (Fri, 17 Feb 2012)
<p id="p-0001" num="0000">A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3-dichloropyrazine with a suitable diaryl imine followed by hydrolysis.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.18mm" wi="50.29mm" file="US08513415-20130820-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

PROCESS FOR THE PREPARATION OF THE COMPOUND OSI - 906 (Fri, 03 Feb 2012)
Process for preparing the tyrosine kinase inhibitor OSI-906 comprises coupling Compound (2) with Compound (6) under specified conditions.
>> read more

PROCESS FOR THE PREPARATION OF THE COMPOUND OSI - 9 06 (Fri, 03 Feb 2012)
Process for preparing the tyrosine kinase inhibitor OSI-906 comprises coupling Compound (2) with Compound (6) under specified conditions.</p>
>> read more

POLYMORPHS OF OSI-906 (Fri, 30 Dec 2011)
Polymorphic forms of the tyrosine kinase inhibitor OSI-906, preparation, pharmaceutical compositions, and uses thereof. The invention includes methods of treating diseases such as cancer, including cancer mediated at least in part by IGF-1 R and/or IR, with the polymorphs and compositions. This Abstract is not limiting of the invention.
>> read more

POLYMORPHS OF OSI-906 (Fri, 30 Dec 2011)
Polymorphic forms of the tyrosine kinase inhibitor OSI-906, preparation, pharmaceutical compositions, and uses thereof. The invention includes methods of treating diseases such as cancer, including cancer mediated at least in part by IGF-1 R and/or IR, with the polymorphs and compositions. This Abstract is not limiting of the invention.</p>
>> read more

Fused bicyclic kinase inhibitors (Fri, 18 Nov 2011)
<p id="p-0001" num="0000">Compounds of Formula I, as shown below and defined herein:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.71mm" wi="69.34mm" file="US08445510-20130521-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of RON, MET or ALK. This Abstract is not limiting of the invention.</p>
>> read more

FUSED BICYCLIC KINASE INHIBITORS (Fri, 18 Nov 2011)
Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of RON, MET or ALK. This Abstract is not limiting of the invention.
>> read more

FUSED BICYCLIC KINASE INHIBITORS (Fri, 18 Nov 2011)
Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as but not limited to tumors driven at least in part by at least one of RON, MET, IR, IGF-1 R, or ALK. This Abstract is not limiting of the invention.
>> read more

FUSED BICYCLIC KINASE INHIBITORS (Fri, 18 Nov 2011)
Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of RON, MET or ALK. This Abstract is not limiting of the invention.</p>
>> read more

Intermediates for the preparation of fused bicyclic mTOR inhibitors (Thu, 10 Nov 2011)
A compound represented by the formula I or II:
>> read more

Substituted pyrrolo[2,3-b]-pyridines and -pyrazines (Fri, 16 Sep 2011)
<p id="p-0001" num="0000">Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by Ron and/or Met.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.97mm" wi="62.99mm" file="US08592448-20131126-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

SUBSTITUTED-5-AMINOPYRROLO/PYRAZOLOPYRIDINES (Sat, 10 Sep 2011)
Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by RON and/or MET.
>> read more

Fused bicyclic motor inhibitors (Fri, 09 Sep 2011)
<p id="p-0001" num="0000">Compounds represented by Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.91mm" wi="50.04mm" file="US08314111-20121120-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer. </p>
>> read more

7-AMINOFUROPYRIDINE DERIVATIVES (Fri, 19 Aug 2011)
Compounds of Formula (1), as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.
>> read more

7-AMINOFUROPYRIDINE DERIVATIVES (Fri, 19 Aug 2011)
Compounds of Formula (1), as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.</p>
>> read more

Amino pyrimidine anticancer compounds (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">Compounds of Formula 1, as shown below and defined herein:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.38mm" wi="60.11mm" file="US08399433-20130319-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.</li> </ul> </li> </ul> </p>
>> read more

Fused Bicyclic mTor Inhibitors (Thu, 26 May 2011)
Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
>> read more

DEUTERATED TYROSINE KINASE INHIBITORS (Fri, 20 May 2011)
Compounds of Formula I, as shown below and defined herein: enriched in deuterium, and pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by IGF-1 R and/or IR.
>> read more

6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors (Thu, 14 Apr 2011)
A process for the preparation of a compound of formula b comprising reacting a compound of formula a with ammonia in a solvent, wherein A11 is halogen z1 is OH ; and z2 is methyl; or z1 and z2 together define oxo.
>> read more

6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors (Thu, 07 Apr 2011)
The invention provides a compound comprising cis -3-[8-amino-1-(2-phenylquinolin-7-yl)-imidazo[1,5- a ]pyrazin-3-yl]-1-methylcyclobutanol, or a pharmaceutically acceptable salt thereof.
>> read more

mTOR inhibitor salt forms (Fri, 21 Jan 2011)
<p id="p-0001" num="0000">Salt forms of mTOR inhibitors of the Formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.32mm" wi="50.04mm" file="US08557814-20131015-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and methods of preparation, formulation, and use in treating disease. </p>
>> read more

PROCESS FOR SUBSTITUTED 3-AMINO-5-OXO-4,5-DIHYDRO-[1,2,4]TRIAZINES (Fri, 14 Jan 2011)
Processes including preparation of trans-4-[(3-amino-5-oxo-4,5-dihydro-[1,2,4]triazin-6-ylmethyl)-carbamoyl]-cyclohexanecarboxylic acid methyl ester, and its conversion to trans-4-(4-amino-5-susbtituted-imidazo[5,1-ƒ][1,2,4]triazin-7-yl)-cyclohexanecarboxylic acid compounds.
>> read more

PROCESS FOR SUBSTITUTED 3-AMINO-5-OXO-4,5-DIHYDRO-[1,2,4]TRIAZINES (Fri, 14 Jan 2011)
Processes including preparation of trans-4-[(3-amino-5-oxo-4,5-dihydro- [1,2,4]triazin-6-ylmethyl)-carbamoyl]-cyclohexanecarboxylic acid methyl ester, and its conversion to trans-4-(4-amino-5-susbtituted- imidazo[5,1-f][1,2,4]triazin-7-yl)-cyclohexanecarboxylic acid compounds. </p>
>> read more

FURO-AND THIENO[3,2-C]PYRIDINES (Thu, 30 Dec 2010)
Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.
>> read more

AMINO PYRIMIDINE ANTICANCER COMPOUNDS (Fri, 10 Dec 2010)
Compounds of Formula (1), as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.
>> read more

AMINO PYRIMIDINE ANTICANCER COMPOUNDS (Fri, 10 Dec 2010)
Compounds of Formula (1), as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK. </p>
>> read more

PREPARATION OF C-PYRAZINE-METHYLAMINES (Fri, 29 Oct 2010)
A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3- dichloropyrazine with a suitable diaryl imine followed by hydrolysis.
>> read more

PREPARATION OF C-PYRAZINE-METHYLAMINES (Fri, 29 Oct 2010)
A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3- dichloropyrazine with a suitable diaryl imine followed by hydrolysis. </p>
>> read more

Combined treatment with an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors (Fri, 02 Jul 2010)
<p id="p-0001" num="0000">The present invention provides a method for treating NSCL, pancreatic, colon or breast cancer tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein the agent is an mTOR inhibitor, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The present invention also provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein said agent is an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases. The present invention also provides a pharmaceutical composition comprising an EGFR kinase inhibitor and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing the methods of this invention is the compound erlotinib HCl (also known as TARCEVA®).</p>
>> read more

(2 - CARBOXAMIDO) (3 - AMINO) THIOPHENE COMPOUNDS (Thu, 01 Jul 2010)

>> read more

SUBSTITUTED PYRROLO[2,3-B]-PYRIDINES AND-PYRAZINES (Fri, 28 May 2010)
Compounds of Formula I, as shown below and defined herein:(I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by Ron and/or Met.
>> read more

Fused bicyclic mTOR inhibitors (Fri, 23 Apr 2010)
<p id="p-0001" num="0000">Compounds represented by Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.06mm" wi="50.21mm" file="US07943767-20110517-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer. </p>
>> read more

6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors (Thu, 01 Apr 2010)
Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , R 1 , and Q 1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.
>> read more

6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors (Fri, 01 Jan 2010)
<p id="p-0001" num="0000">Compounds of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.15mm" wi="69.93mm" file="US08101613-20120124-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and pharmaceutically acceptable salts thereof, wherein X<sub>1</sub>, X<sub>2</sub>, X<sub>3</sub>, X<sub>4</sub>, X<sub>5</sub>, X<sub>6</sub>, X<sub>7</sub>, R<sup>1</sup>, and Q<sup>1 </sup>are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.</p>
>> read more

SUBSTITUTED IMIDAZOPYR-AND IMIDAZOTRI-AZINES (Fri, 27 Nov 2009)
Fused pyridine-based bicyclic compounds having the structure of Formula (1) as defined herein, pharmaceutically acceptable salts thereof, preparation, compositions, and disease treatment therewith. This abstract does not define or limit the invention.
>> read more

Substituted imidazopyr- and imidazotri-azines (Fri, 20 Nov 2009)
<p id="p-0001" num="0000">Fused pyridine-based bicyclic compounds having the structure of Formula I, as defined herein, pharmaceutically acceptable salts thereof, preparation, compositions, and disease treatment therewith. This abstract does not define or limit the invention.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.15mm" wi="69.85mm" file="US08481733-20130709-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

MTOR INHIBITOR SALT FORMS (Fri, 25 Sep 2009)
Salt forms of mTOR inhibitors of the Formula (I) and methods of preparation, formulation, and use in treating disease.
>> read more

MTOR INHIBITOR SALT FORMS (Fri, 25 Sep 2009)
Salt forms of mTOR inhibitors of the Formula (I) and methods of preparation, formulation, and use in treating disease. </p>
>> read more

2-AMINOPYRIDINE KINASE INHIBITORS (Fri, 14 Aug 2009)
2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, F1t3, FGFR3, Ab1, Aurora A, c-Src, IGF- IR, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition.
>> read more

FURO-AND THIENO[3,2-C] PYRIDINES (Fri, 14 Aug 2009)
Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula (I), and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.
>> read more

FURO- AND THIENO[3,2-C] PYRIDINES (Fri, 14 Aug 2009)
Furo[3,2-c]Pyridine and Thieno[3,2-c] pyridine compounds of Formula (I), and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET. </p>
>> read more

Furo[3,2-C]pyridines (Fri, 07 Aug 2009)
<p id="p-0001" num="0000">Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.77mm" wi="69.85mm" file="US08022206-20110920-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

2-aminopyridine kinase inhibitors (Fri, 07 Aug 2009)
<p id="p-0001" num="0000">2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="16.34mm" wi="54.69mm" file="US08178668-20120515-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

2-ARYL pyrrologpyrimidines for A1 and A3 receptors (Fri, 31 Jul 2009)
<p id="p-0001-en" num="0000">This invention pertains to compounds which specifically inhibit the adenosine A<sub>1 </sub>and A<sub>3 </sub>receptors and the use of these compounds to treat a disease associated with A<sub>3 </sub>adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.</p>
>> read more

IMIDAZOPYRAZINOL DERIVATIVES FOR THE TREATMENT OF CANCERS (Fri, 24 Jul 2009)
Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-IR enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.
>> read more

Imidazopyrazine Tyrosine Kinase Inhibitors (Fri, 17 Jul 2009)
<p id="p-0001-en" num="0000">Compounds of the formula</p> <p id="p-0002-en" num="0000"/> <p id="p-0003-en" num="0000">and pharmaceutically acceptable salts thereof, wherein Q<sup>1 </sup>and R<sup>1 </sup>are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases.</p>
>> read more

Fused bicyclic mTor inhibitors (Fri, 26 Jun 2009)
<p id="p-0001" num="0000">Compounds represented by Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.06mm" wi="50.04mm" file="US07923555-20110412-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer. </p>
>> read more

6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors (Fri, 08 May 2009)
<p id="p-0001-en" num="0000">Compounds of the formula</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="25.15mm" wi="69.85mm" file="US07820662-20101026-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">and pharmaceutically acceptable salts thereof, wherein X<sub>1</sub>, X<sub>2</sub>, X<sub>3</sub>, X<sub>4</sub>, X<sub>5</sub>, X<sub>6</sub>, X<sub>7</sub>, R<sup>1</sup>, and Q<sup>1 </sup>are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.</p>
>> read more

Compounds specific to adenosine A1 and A3 receptors and uses thereof (Thu, 23 Apr 2009)
This invention pertains to compounds which specifically inhibit the adenosine A1 and A3 receptors and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
>> read more

Pyrrolo[2,3d]pyrimidine compositions and their use (Fri, 27 Mar 2009)
<p id="p-0001-en" num="0000">This invention pertains to compounds having the structure:</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="26.84mm" wi="32.68mm" file="us20090082369a1-20090326-c00001.tif" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein R<sub>1 </sub>and R<sub>2 </sub>together form a substituted or unsubstituted heterocyclic ring; R<sub>3 </sub>is a substituted or unsubstituted aryl moiety; R<sub>4 </sub>is a hydrogen atom, an unsubstituted alkyl, or a substituted or unsubstituted aryl moiety; and R<sub>5 </sub>and R<sub>6 </sub>are each independently a halogen atom, a hydrogen atom or a substituted or unsubstituted alkyl, aryl, or alkylaryl moiety, or a pharmaceutically acceptable salt thereof, and the use of these compounds to treat a disease associated with increased levels of adenosine in a subject.</p>
>> read more

N-substituted imidazopyridine c-Kit inhibitors (Fri, 06 Mar 2009)
<p id="p-0001-en" num="0000">Compounds represented by Formula (I):</p> <p id="p-0002-en" num="0000"> <br/> or a pharmaceutically acceptable salt or N-Oxide thereof, are useful in the treatment of cancer. </p>
>> read more

COMBINATION ANTI-CANCER THERAPY COMPRISING AN INHIBITOR OF BOTH MTORC1 AND MT0RC2 (Fri, 16 Jan 2009)
The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an anti-cancer agent or treatment that elevates pAkt levels in tumor cells and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mT0RC2 kinases. Examples of such anti-cancer agents or treatments incude doxorubicin, cisplatin, or ionizing radiation. The present invention also provides a pharmaceutical composition comprising an anti-cancer agent or treatment that elevates pAkt levels in tumor cells and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mT0RC2 kinases, in a pharmaceutically acceptable carrier. The present invention also provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of the anti-cancer agent melphalan or 5-FU, and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mT0RC2 kinases.
>> read more

Pyrrolo[2,3d]Pyrimidine compositions and their use (Thu, 08 Jan 2009)
Novel deazapurines are disclosed which are useful for the treatment of adenosine receptor stimulated diseases.
>> read more

Isothiazole derivatives useful as anticancer agents (Fri, 05 Dec 2008)
<p id="p-0001-en" num="0000">The present invention relates to compounds of the formula 1</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="21.59mm" wi="59.18mm" file="US07790902-20100907-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001-en" list-style="none"> <li> <ul id="ul0002-en" list-style="none"> <li>and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X<sup>1</sup>, R<sup>1</sup>, R<sup>2 </sup>and R<sup>3 </sup>are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.</li> </ul> </li> </ul> </p>
>> read more

Pyrrolopyrimidine A<sub>2B </sub>selective antagonist compounds, their synthesis and use (Fri, 24 Oct 2008)
<p id="p-0001-en" num="0000">The subject invention provides compounds having the structure:</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="26.16mm" wi="31.67mm" file="US07645754-20100112-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001-en" list-style="none"> <li> <ul id="ul0002-en" list-style="none"> <li>wherein, <ul id="ul0003-en" list-style="none"><li>R<sub>1 </sub>is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NR<sub>a</sub>R<sub>b</sub>, —NR<sub>a</sub>R<sub>b</sub>, —NR<sub>a</sub>C(═O)NR<sub>a</sub>R<sub>b</sub>, —NR<sub>a</sub>C(═O)OR<sub>a</sub>, —OC(═O)NR<sub>a</sub>R<sub>b</sub>, or —NHC(═O) R<sub>a</sub>;</li><li>R<sub>2 </sub>is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NR<sub>a</sub>R<sub>b</sub>, —NR<sub>a</sub>R<sub>b</sub>, —NR<sub>a</sub>C(═O)NR<sub>a</sub>R<sub>b</sub>, —NR<sub>a</sub>C(═O)OR<sub>a</sub>, —OC(═O)NR<sub>a</sub>R<sub>b</sub>, or —NHC(═O)R<sub>a</sub>, or</li><li>R<sub>1</sub>, R<sub>2 </sub>and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH<sub>2</sub>)<sub>2</sub>OH or —CH<sub>2</sub>C(═O)OH;</li><li>R<sub>3 </sub>is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C<sub>1</sub>-C<sub>15</sub>)alkyl, (C<sub>1</sub>-C<sub>15</sub>)alkoxy, or —NR<sub>a</sub>R<sub>b</sub>;</li><li>R<sub>4 </sub>is hydrogen or substituted or unsubstituted (C<sub>1</sub>-C<sub>15</sub>)alkyl;</li><li>R<sub>5 </sub>is —(CH<sub>2</sub>)<sub>m</sub>OR<sub>6</sub>, —CHNOR<sub>7</sub>, —C(═O)NR<sub>8</sub>R<sub>9</sub>, —(CH<sub>2</sub>)<sub>m</sub>C(═O)OR<sub>10</sub>, —(CH<sub>2</sub>)<sub>k</sub>C(═O)NR<sub>11</sub>R<sub>12</sub>; <ul id="ul0004-en" list-style="none"><li>wherein R<sup>6 </sup>is a substituted or unsubstituted (C<sub>1</sub>-C<sub>30</sub>)alkyl,</li><li>(C<sub>3</sub>-C<sub>10</sub>)cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring;</li><li>R<sub>7 </sub>is hydrogen, or a substituted or unsubstituted (C<sub>1</sub>-C<sub>30</sub>)alkyl, (C<sub>1</sub>-C<sub>30</sub>)alkylaryl;</li><li>R<sub>8 </sub>and R<sub>9 </sub>are each independently hydrogen, or a substituted or unsubstituted (C<sub>1</sub>-C<sub>30</sub>)alkyl, (C<sub>1</sub>-C<sub>30</sub>)alkylaryl, (C<sub>1</sub>-C<sub>30</sub>)alkylamino, (C<sub>1</sub>-C<sub>30</sub>)alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or</li><li>R<sub>8</sub>, N, and R<sub>9 </sub>together form a substituted or unsubstituted 4-8 membered heterocyclic ring;</li><li>R<sub>10 </sub>is hydrogen or a substituted or unsubstituted (C<sub>1</sub>-C<sub>30</sub>)alkyl, (C<sub>3</sub>-C<sub>10</sub>)cycloalkyl, or an aryl, heteroaryl or heterocyclic ring;</li><li>R<sub>11</sub>, N and R<sub>12 </sub>together form a 4-8 membered heterocyclic ring;</li><li>R<sub>a </sub>and R<sub>b </sub>are each independently hydrogen or alkyl;</li><li>m is 0, 1, 2 or 3; and</li><li>k is 1, 2 or 3, <br/> or a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A<sub>2b </sub>adenosine receptor in a subject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention. </li></ul></li></ul></li> </ul> </li> </ul> </p>
>> read more

FUSED BICYCLIC mTOR INHIBITORS (Thu, 07 Aug 2008)
Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
>> read more

COMBINATION OF IGFR INHIBITOR AND ANTI-CANCER AGENT (Fri, 27 Jun 2008)
The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an anticancer agent and an IGFlR inhibitor compound of Formula (I) combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also encompasses a pharmaceutical composition that is comprised of an anticancer agent and IGFlR inhibitor compound of Formula (I) combination with a pharmaceutically acceptable carrier. The IGFl R inhibitor is represented by Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein.
>> read more

Compounds specific to adenosine A1 receptors and uses thereof (Fri, 21 Mar 2008)
<p id="p-0001-en" num="0000">This invention pertains to compounds which specifically inhibit the adenosine A<sub>1 </sub>receptor and the use of these compounds to treat a disease associated with A<sub>1 </sub>adenosine receptors in a subject. </p>
>> read more

6,6-BICYCLIC RING SUBSTITUTED SULFUR CONTAINING HETEROBICYCLIC PROTEIN KINASE INHIBITORS (Fri, 15 Feb 2008)
Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.
>> read more

Combined treatment with an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors (Fri, 07 Dec 2007)
<p id="p-0001-en" num="0000">The present invention provides a method for treating NSCL, pancreatic, colon or breast cancer tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein the agent is an mTOR inhibitor, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The present invention also provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein said agent is an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases. The present invention also provides a pharmaceutical composition comprising an EGFR kinase inhibitor and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing the methods of this invention is the compound erlotinib HCl (also known as TARCEVA®).</p>
>> read more

Unsaturated mTOR inhibitors (Fri, 02 Nov 2007)
<p id="p-0001-en" num="0000">Compounds represented by Formula (I)</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="25.06mm" wi="50.12mm" file="US07659274-20100209-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer. </p>
>> read more

COMBINED TREATMENT WITH AN EGFR KINASE INHIBITOR AND AN AGENT THAT SENSITIZES TUMOR CELLS TO THE EFFECTS OF EGFR KINASE INHIBITORS (Fri, 21 Sep 2007)
The present invention provides a method for manufacturing a medicament intended for treating NSCL, pancreatic, colon or breast cancer tumors or tumor metastases in combination with an EGFR kinase inhibitor, characterized in that an mTOR inhibitor is used, and wherein the inhibitors are intended for administration either simultaneously or sequentially, and with or without administration of additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The present invention also provides a method for manufacturing a medicament intended for treating tumors or tumor metastases in a patient in combination of an EGFR kinase inhibitor, characterized in that an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases is used, and wherein the inhibitors are intended for administration either simultaneously or sequentially, and with or without administration of additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The present invention also provides a pharmaceutical composition comprising an EGFR kinase inhibitor and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing the methods of this invention is the compound erlotinib HCl (also known as TARCEVA®).
>> read more

N-SUBSTITUTED BENZIMIDAZOLYL C-KIT INHIBITORS AND COMBINATORIAL BENZIMIDAZOLE LIBRARY (Thu, 13 Sep 2007)
Compounds represented by Formula (I) or a pharmaceutically acceptable salt or N-oxide thereof act as c-kit inhibitors and are useful in the treatment of tumors. Combinatorial libraries composed of compounds represented by Formula (I) or benzimidazole compounds represented by Formula (II) are useful in providing compounds to assay for such therapeutically useful compounds.
>> read more

N-PHENYLBENZOTRIAZOLYL C-KIT INHIBITORS (Fri, 17 Aug 2007)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
>> read more

UNSATURATED mTOR INHIBITORS (Fri, 03 Aug 2007)
Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
>> read more

FUSED HETEROBICYCLIC KINASE INHIBITORS (Fri, 27 Jul 2007)
Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit kinase enzymes and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer. The compounds are also useful in the treatment of inflammation, allergy, asthma, disease and conditions of the immune system, disease and conditions of the nervous system, cardiovascular diseases, disease and conditions of the eye, dermatological diseases, osteoporosis, diabetes, multiple sclerosis, and infections.
>> read more

FUSED HETEROBICYCLIC KINASE INHIBITORS (Fri, 27 Jul 2007)
Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit kinase enzymes and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer. The compounds are also useful in the treatment of inflammation, allergy, asthma, disease and conditions of the immune system, disease and conditions of the nervous system, cardiovascular diseases, disease and conditions of the eye, dermatological diseases, osteoporosis, diabetes, multiple sclerosis, and infections. </p>
>> read more

(2-CARBOXAMIDO)(3-AMINO) THIOPHENE COMPOUNDS (Thu, 19 Jul 2007)
Amidoaryl/amidoheteroaryl substituted thiophenes, further substituted with a heteroarylmethylamino group, are useful in the treatment of cancer.
>> read more

Bicyclic protein kinase inhibitors (Fri, 29 Jun 2007)
<p id="p-0001-en" num="0000">Compounds of the Formula</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="25.65mm" wi="49.95mm" file="US07648987-20100119-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> and pharmaceutically acceptable salts thereof, wherein X<sub>1</sub>, X<sub>2</sub>, X<sub>3</sub>, X<sub>4</sub>, X<sub>5</sub>, X<sub>6</sub>, X<sub>7</sub>, R<sup>1</sup>, and Q<sup>1 </sup>are defined herein, inhibit protein kinase enzymes and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system. </p>
>> read more

PYRROLOPYRIDINE KINASE INHIBITING COMPOUNDS (Fri, 15 Jun 2007)
Compounds represented by Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least one of the Ab1, Aurora-A, BIk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mekl, PDK-1, GSK3β, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-IR, Ron, Met, and KDR kinases in animals, including humans, for the treatment and/or prevention of various diseases and conditions such as cancer.
>> read more

PROCESS TO PREPARE SUBSTITUTED IMIDAZOPYRAZINE COMPOUNDS (Fri, 15 Jun 2007)
A method of preparing formula (A) ,wherein, X=C1, Br, I, comprises the step of treating formula (B), with N-chloro-, N-bromo-, or N-iodosuccinimide in a compatible solvent such as dimethylformamide (DMF) at 0-60° C followed by halogenation.
>> read more

BICYCLIC PROTEIN KINASE INHIBITORS (Fri, 08 Jun 2007)
Compounds of the Formula (I) and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit protein kinase enzymes and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.
>> read more

FUSED BICYCLIC mTOR INHIBITORS (Fri, 01 Jun 2007)
Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
>> read more

FUSED BICYCLIC MTOR INHIBITORS (Fri, 01 Jun 2007)
Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer. </p>
>> read more

Fused bicyclic mTOR inhibitors (Fri, 18 May 2007)
<p id="p-0001-en" num="0000">Compounds represented by Formula (I)</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="25.15mm" wi="50.12mm" file="US07700594-20100420-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer. </p>
>> read more

PROCESSES FOR THE PREPARATION OF ISOTHIAZOLE DERIVATIVES (Thu, 17 May 2007)
Processes and intermediates for the preparation of compounds of the Formula (1) and the pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, wherein R<sp>1</sp>, R<sp>2</sp>, and R<sp>3</sp> have the definitions provided herein.
>> read more

Substituted thienol[2,3-d]pyrimidines as kinase inhibitors (Fri, 09 Feb 2007)
<p id="p-0001-en" num="0000">Compounds of the formula</p> <p id="p-0002-en" num="0000"> <br/> and pharmaceutically acceptable salts thereof, wherein X<sub>1</sub>, X<sub>2</sub>, X<sub>3</sub>, and Q<sup>1 </sup>are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system. </p>
>> read more

CYCLITOL LINKER POLYMER CONJUGATE (Fri, 09 Feb 2007)
Conjugating biologically active molecules with polymers, high molecular weight non- immunogenic and lipophilic compounds has been described to improve in vivo profiles of the biologically active molecules. The invention relates to a conjugate comprising a polymer, a biologically active molecule and cyclitol linking the polymer to the biologically active molecule. The invention also relates to an activated polymer composition comprising a polymer, an active functional group and a cyclitol linking the polymer to the active functional group.
>> read more

6,6-BICYCLIC RING SUBSTITUTED HETEROBICYCLIC PROTEIN KINASE INHIBITORS (Thu, 11 Jan 2007)
Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein X<sb>I</sb>, X<sb>2</sb>, X<sb>3</sb>, X<sb>4</sb>, X<sb>5</sb>, X<sb>6</sb>, X<sb>7</sb>, R<sp>1</sp>, and Q<sp>1</sp> are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.
>> read more

Pyrrolo[2,3-d]pyrimidine derivatives which are antagonists of adenosine A1, A2A, and A3 (Thu, 14 Dec 2006)
This invention pertains to pyrrolo [2,3-d] pyramidine derivated compounds which specifically inhibit the adenosine A1, A 2A and A 3 receptors and the use of these compounds to treat a disease associated with A1, A 2A and A 3 adenosine receptors in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
>> read more

VEGF VARIANTS (Fri, 10 Nov 2006)
Applicants have defined the pro-inflammatory domain of the Vascular Endothelial Growth Factor VEGF 164(165) protein molecule using VEGF 164 protein mutants in which the heparin binding domain is inactivated through alanine scanning, site directed mutagenesis. The invention provides novel VEGF variants having a modified heparin binding domain. The VEGF variants modified heparin binding function compared to native VEGF while maintaining receptor binding function. The invention provides compositions and methods for treating disorders relating to angiogenesis and inflammation.
>> read more

VEGF VARIANTS (Fri, 10 Nov 2006)
Applicants have defined the pro-inflammatory domain of the Vascular Endothelial Growth Factor VEGF 164(165) protein molecule using VEGF 164 protein mutants in which the heparin binding domain is inactivated through alanine scanning, site directed mutagenesis. The invention provides novel VEGF variants having a modified heparin binding domain. The VEGF variants modified heparin binding function compared to native VEGF while maintaining receptor binding function. The invention provides compositions and methods for treating disorders relating to angiogenesis and inflammation. </p>
>> read more

(2-carboxamido)(3-amino)thiophene compounds (Fri, 03 Nov 2006)
<p id="p-0001-en" num="0000">A method of treatment of hyperproliferative disorders comprises a step of administering an effective amount of a compound represented by</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="24.72mm" wi="36.49mm" file="US07524859-20090428-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> read more

6,6-Bicyclic ring substituted heterobicyclic protein kinase inhibitors (Fri, 20 Oct 2006)
<p id="p-0001-en" num="0000">Compounds of the formula</p> <p id="p-0002-en" num="0000"> <ul id="ul0001-en" list-style="none"> <li> <ul id="ul0002-en" list-style="none"> <li>and pharmaceutically acceptable salts thereof, wherein X<sub>1</sub>, X<sub>2</sub>, X<sub>3</sub>, X<sub>4</sub>, X<sub>5</sub>, X<sub>6</sub>, X<sub>7</sub>, R<sup>1</sup>, and Q<sup>1 </sup>are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.</li> </ul> </li> </ul> </p>
>> read more

PYRROLO [2,3-D] IMIDAZOLES FOR THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS (Fri, 13 Oct 2006)
Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors and cancers.
>> read more

PYRROLO [2,3-D] IMIDAZOLES FOR THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS (Fri, 13 Oct 2006)
Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors and cancers. </p>
>> read more

Pyrrolo[2,3-D]imidazoles for the treatment of hyperproliferative disorders (Fri, 06 Oct 2006)
<p id="p-0001-en" num="0000">or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors and cancers.</p> <p id="p-0002-en" num="0000"/>
>> read more

Substituted pyrrolo[2.3-B]pyridines (Fri, 22 Sep 2006)
<p id="p-0001-en" num="0000">Compounds represented by Formula (I):</p> <p id="p-0002-en" num="0000"> <ul id="ul0001-en" list-style="none"> <li> <ul id="ul0002-en" list-style="none"> <li>or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mek1, PDK-1, GSK3β, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-1R, Ron, Ret, and KDR kinases in animals, including humans, for the treatment and/or prevention of various diseases and conditions such as cancer.</li> </ul> </li> </ul> </p>
>> read more

N-substituted benzimidazolyl c-Kit inhibitors (Fri, 25 Aug 2006)
<p id="p-0001-en" num="0000">Compounds represented by Formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="34.88mm" wi="53.00mm" file="US07521448-20090421-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer. </p>
>> read more

ISOTHIAZOLE DERIVATIVES USEFUL AS ANTICANCER AGENTS (Thu, 06 Jul 2006)

>> read more

IMIDAZO[1,5-A]PYRAZINES AS TYROSINE KINASE INHIBITORS (Thu, 06 Jul 2006)
Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein Q<sp>1 </sp>and R<sp>1</sp> are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases.
>> read more

N-SUBSTITUTED BENZIMIDAZOLYL C-KIT INHIBITORS AND COMBINATORIAL BENZIMIDAZOLE LIBRARY (Fri, 09 Jun 2006)
Compounds represented by Formula (I) or a pharmaceutically acceptable salt or N-oxide thereof act as c-kit inhibitors and are useful in the treatment of tumors. Combinatorial libraries composed of compounds represented by Formula (I) or benzimidazole compounds represented by Formula (II) are useful in providing compounds to assay for such therapeutically useful compounds.
>> read more

N-SUBSTITUTED BENZIMIDAZOLYL C-KIT INHIBITORS AND COMBINATORIAL BENZIMIDAZOLE LIBRARY (Fri, 09 Jun 2006)
Compounds represented by Formula (I) or a pharmaceutically acceptable salt or N-oxide thereof act as c-kit inhibitors and are useful in the treatment of tumors. Combinatorial libraries composed of compounds represented by Formula (I) or benzimidazole compounds represented by Formula (II) are useful in providing compounds to assay for such therapeutically useful compounds. </p>
>> read more

N-SUBSTITUTED PYRAZOLYL-AMIDYL-BENZIMIDAZOLYL C-KIT INHIBITORS (Thu, 08 Jun 2006)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
>> read more

Integrin antagonists useful as anticancer agents (Fri, 02 Jun 2006)
<p id="p-0001" num="0000">The invention relates to compounds of the Formula 1</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="21.67mm" wi="56.98mm" file="US08003806-20110823-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and to pharmaceutically acceptable salts and solvates thereof, wherein A, X<sup>2</sup>, X<sup>4</sup>, X<sup>5 </sup>and X<sup>1 </sup>are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula 1. </p>
>> read more

N-substituted benzimidazoyl c-Kit inhibitors and combinatorial benzimidazole library (Fri, 02 Jun 2006)
<p id="p-0001-en" num="0000">Compounds represented by Formula (I):</p> <p id="p-0002-en" num="0000"> <br/> or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors. Combinatorial libraries composed of compounds represented by Formula (I) or benzimidazole compounds represented by Formula (II): </p> <p id="p-0003-en" num="0000"> <br/> are useful in providing compounds to assay for such therapeutically useful compounds. </p>
>> read more

(Arylamidoaryl)squaramide compounds (Fri, 26 May 2006)
<p id="p-0001-en" num="0000">Compounds represented by Formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="23.11mm" wi="66.38mm" file="US07829717-20101109-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, Q, Y, R<sup>5</sup>, m and J are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma. </p>
>> read more

3-SUBSTITUTED IMIDAZOPYRIDINE-DERIVATIVES AS C-KIT INHIBITORS (Thu, 25 May 2006)
Compounds represented by Formula (I): (I) or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
>> read more

INTEGRIN ANTAGONISTS USEFUL AS ANTICANCER AGENTS (Fri, 19 May 2006)
The invention relates to compounds of the Formula (1) and to pharmaceutically acceptable salts and solvates thereof, wherein A, X2, X4, X5 and X1 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula (1). The compounds act as integrin antagonists.
>> read more

(2-CARBOXAMIDO)(3-AMINO) THIOPHENE COMPOUNDS (Fri, 05 May 2006)
Amidoaryl/amidoheteroaryl substituted thiophenes, further substituted with a heteroarylmethylamino group, are useful in the treatment of cancer.
>> read more

(2-CARBOXAMIDO)(3-AMINO) THIOPHENE COMPOUNDS (Fri, 05 May 2006)
Amidoaryl/amidoheteroaryl substituted thiophenes, further substituted with a heteroarylmethylamino group, are useful in the treatment of cancer. </p>
>> read more

Imidazopyrazine tyrosine kinase inhibitors (Fri, 21 Apr 2006)
<p id="p-0001-en" num="0000">Compounds of the formula</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="25.15mm" wi="69.77mm" file="US07459554-20081202-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> and pharmaceutically acceptable salts thereof, wherein Q<sup>1 </sup>and R<sup>1 </sup>are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases. </p>
>> read more

(Arylamidoanilino)nitroethylene compounds (Fri, 31 Mar 2006)
<p id="p-0001-en" num="0000">Compounds represented by Formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="21.25mm" wi="65.19mm" file="US07618965-20091117-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, Q, Y, R<sup>1</sup>, R<sup>2</sup>, and R<sup>5 </sup>are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma. </p>
>> read more

(ARYLAMIDOARYL)SQUARAMIDE COMPOUNDS (Fri, 31 Mar 2006)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, Q, Y, R5, m and J are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid crystic carcinoma, acute meyelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcubinam abd oristate carcinoma.
>> read more

(HYDRAZIDO) (AMINO) THIOPHENE COMPOUNDS (Fri, 31 Mar 2006)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A and J are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma.
>> read more

(ARYLAMIDOANILINO) NITROETHYLENE COMPOUNDS (Fri, 31 Mar 2006)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, Q, Y, R1, R2, and R5 are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma..
>> read more

(SPIROCYCLYLAMIDO) AMINOTHIOPHENE COMPOUNDS AS C-KIT PROTO- ONCOGENE INHIBITORS (Fri, 31 Mar 2006)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, R1, X and Y are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma.
>> read more

(ARYLAMIDOARYL) CYANOGUANIDINE COMPOUNDS AS INHIBITORS OF C-KIT PROTO-ONCOGENE (Fri, 31 Mar 2006)
Compounds represented by Formula (I): or a pharmaceutically acceptable slat or N-oxide thereof, wherein A, Q, Y R5 and J are defined herein, are useful in the treatment of cancer.
>> read more

(SPIROCYCLYLAMIDO) AMINOTHIOPHENE COMPOUNDS AS C-KIT PROTO- ONCOGENE INHIBITORS (Fri, 31 Mar 2006)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, R1, X and Y are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma. </p>
>> read more

MERCAPTOAMIDES AS HISTONE DEACETYLASE INHIBITORS (Fri, 17 Mar 2006)
Mercaptoamide compounds, represented by Formulas (IA), (IB), (IIA), and (IIB): or a pharmaceutically acceptable salt thereof, inhibit histone deacetylase enzyme and are useful for the treatment and/or prevention of various infections, cancerous diseases, and conditions.
>> read more

MERCAPTOAMIDES AS HISTONE DEACETYLASE INHIBITORS (Fri, 17 Mar 2006)
Mercaptoamide compounds, represented by Formulas (IA), (IB), (IIA), and (IIB): or a pharmaceutically acceptable salt thereof, inhibit histone deacetylase enzyme and are useful for the treatment and/or prevention of various infections, cancerous diseases, and conditions. </p>
>> read more

PROCESSES FOR THE PREPARATION OF ISOTHIAZOLE DERIVATIVES (Fri, 10 Mar 2006)
Processes and intermediates for the preparation of compounds of the Formula (1) and the pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, wherein R1, R2, and R3 have the definitions provided herein.
>> read more

PROCESSES FOR THE PREPARATION OF ISOTHIAZOLE DERIVATIVES (Fri, 10 Mar 2006)
Processes and intermediates for the preparation of compounds of the Formula (1) and the pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, wherein R1, R2, and R3 have the definitions provided herein. </p>
>> read more

N3-substituted imidazopyridine c-Kit inhibitors (Fri, 17 Feb 2006)
<p id="p-0001-en" num="0000">Compounds represented by Formula (I):</p> <p id="p-0002-en" num="0000"> <br/> or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer. </p>
>> read more

N-substituted pyrazolyl-amidyl-benzimidazolyl c-Kit inhibitors (Fri, 17 Feb 2006)
<p id="p-0001-en" num="0000">Compounds represented by Formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="30.99mm" wi="58.34mm" file="US07485658-20090203-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer. </p>
>> read more

ARYL-AMINO SUBSTITUTED PYRROLOPYRIMIDINE MULTI-KINASE INHIBITING COMPOUNDS (Fri, 17 Feb 2006)
Compounds represented by Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mekl, PDK-1, GSK3ß, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-lR, Ron, Ret, and KDR kinases in animals, including humans, for the treatment and/or prevention of various diseases and conditions such as cancer.
>> read more

ARYL-AMINO SUBSTITUTED PYRROLOPYRIMIDINE MULTI-KINASE INHIBITING COMPOUNDS (Fri, 17 Feb 2006)
Compounds represented by Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mekl, PDK-1, GSK3~, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-lR, Ron, Ret, and KDR kinases in animals, including humans, for the treatment and/or prevention of various diseases and conditions such as cancer. </p>
>> read more

IMIDAZOPYRAZINE AS TYROSINE KINASE INHIBITORS (Fri, 03 Feb 2006)
Compounds of the formula (I): and pharmaceutically acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF- 1 R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases.
>> read more

IMIDAZOPYRAZINE AS TYROSINE KINASE INHIBITORS (Fri, 03 Feb 2006)
Compounds of the formula (I): and pharmaceutically acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF- 1 R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases. </p>
>> read more

Imidazotriazines as protein kinase inhibitors (Fri, 27 Jan 2006)
<p id="p-0001-en" num="0000">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="25.15mm" wi="48.85mm" file="US07741324-20100622-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> and pharmaceuticaly acceptable salts thereof, wherein Q<sup>1 </sup>and R<sup>1 </sup>are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases. </p>
>> read more

Naphthylene derivatives as cytochrome P450 inhibitors (Fri, 13 Jan 2006)
<p id="p-0001-en" num="0000">Compounds of the formula</p> <p id="p-0002-en" num="0000"> <br/> and pharmaceutically acceptable salts thereof, wherein n<b>1</b>, n<b>2</b>, n<b>3</b>, n<b>4</b>, G<sup>1</sup>, Q<sup>1</sup>, Z, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4a</sup>, R<sup>4b</sup>, R<sup>5a</sup>, and R<sup>5b </sup>are defined herein, inhibit the cytochrome P<b>450</b>RAI enzyme and are useful for the treatment and/or prevention of various diseases and conditions which respond to treatment by retinoids and by naturally occurring retinoic acid. </p>
>> read more

Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase (Fri, 25 Nov 2005)
<p id="p-0001-en" num="0000">Compounds represented by Formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="27.26mm" wi="66.55mm" file="US07405210-20080729-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001-en" list-style="none"> <li> <ul id="ul0002-en" list-style="none"> <li>or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.</li> </ul> </li> </ul> </p>
>> read more

(2-CARBOXAMIDO) (3-AMINO) THIOPHENE COMPOUNDS (Thu, 03 Nov 2005)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1 is Formula (II, III, IV, V or VI); R2 is Formula (VII, VIII, IX or X);<sp> </sp>and R3 is C<sb>0-4 </sb>alkyl, are useful in the treatment of cancer.
>> read more

6,6-BICYCLIC RING SUBSTITUTED HETEROBICYCLIC PROTEIN KINASE INHIBITORS (Fri, 21 Oct 2005)
Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein XI, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.
>> read more

6,6-BICYCLIC RING SUBSTITUTED HETEROBICYCLIC PROTEIN KINASE INHIBITORS (Fri, 21 Oct 2005)
Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein XI, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system. </p>
>> read more

(2-Carboxamido)(3-amino)thiophene compounds (Fri, 02 Sep 2005)
<p id="p-0001-en" num="0000">A method of treatment of hyperproliferative disorders comprises administering an effective amount of a compound represented by Formula II:</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="30.99mm" wi="63.75mm" file="US07101893-20060905-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt thereof. </p>
>> read more

Substituted bicyclic derivatives for the treatment of abnormal cell growth (Fri, 22 Jul 2005)
<p id="p-0001-en" num="0000">The invention relates to compounds of the formula 1</p> <p id="p-0002-en" num="0000"> <br/> and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R<sup>1</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>11</sup>, m and p are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1. </p>
>> read more

(2-carboxamido)(3-Amino) thiophene compounds (Fri, 15 Jul 2005)
<p id="p-0001-en" num="0000">Amidoaryl/amidoheteroaryl substituted thiophenes, further substituted with a heteroarylmethylamino group, are useful in the treatment of cancer.</p>
>> read more

Pyrimidine A<sub>2B </sub>selective antagonist compounds, their synthesis and use (Fri, 03 Jun 2005)
<p id="p-0001-en" num="0000">The subject invention provides compounds having the structure:</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="30.90mm" wi="57.32mm" file="US07501407-20090310-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein R<sub>1 </sub>is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R<sub>2 </sub>is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R<sub>3 </sub>is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R<sub>2 </sub>and R<sub>3 </sub>are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R<sub>3 </sub>is oxygen; R<sub>4 </sub>and R<sub>5 </sub>are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R<sub>4</sub>NR<sub>5 </sub>together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; <ul id="ul0001-en" list-style="none"><li><ul id="ul0002-en" list-style="none"><li>R<sub>12 </sub>is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A<sub>2b </sub>adenosine receptor by administering a therapeutically effective amount of the compounds of the invention.</li></ul></li></ul></p>
>> read more

Compounds specific to adenosine A<sub>1 </sub>and A<sub>3 </sub>receptors and uses thereof (Fri, 29 Apr 2005)
<p id="p-0001-en" num="0000">This invention pertains to compounds having the structure:</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="37.85mm" wi="46.06mm" file="US07504407-20090317-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein <ul id="ul0001-en" list-style="none"><li><ul id="ul0002-en" list-style="none"><li>m is 0, 1, 2, or 3;</li><li>R<sub>2 </sub>is a substituted or unsubstituted imidazole or pyrazole wherein the point of attachment of R<sub>2 </sub>to the alkyl chain is not N;</li><li>R<sub>5 </sub>is a hydrogen atom or a substituted or unsubstituted alkyl, aryl, or alkylaryl moiety; and</li><li>R<sub>7 </sub>is a halogen atom, C<sub>1</sub>-C<sub>4 </sub>alkyl, OH, O-alkyl(C<sub>1</sub>-C<sub>4</sub>), NH<sub>2</sub>, or NH-alkyl(C<sub>1</sub>-C<sub>4</sub>),</li></ul></li></ul></p> <p id="p-0003-en" num="0000">which specifically inhibit the adenosine A1 and A3 receptors and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compound.</p>
>> read more

IMIDAZO ‘1, 5 - A ! PYRAZINE TYROSINE KINASE INHIBITORS (Fri, 29 Apr 2005)
Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases.
>> read more

IMIDAZOPYRAZINE TYROSINE KINASE INHIBITORS (Fri, 29 Apr 2005)
Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases. </p>
>> read more

Compounds specific to adenosine A1 receptor and uses thereof (Wed, 13 Apr 2005)
<p id="p-00001-en" num="00001">This invention pertains to compounds which specifically inhibit the adenosine A<sub>1 </sub>receptor and the use of these compounds to treat a disease associated with A<sub>1 </sub>adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.</p>
>> read more

N-SUBSTITUTED BENZIMIDAZOLYL C-KIT INHIBITORS (Fri, 11 Mar 2005)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
>> read more

N-SUBSTITUTED PYRAZOLYL-AMIDYL-BENZIMIDAZOLYL C-KIT INHIBITORS (Fri, 11 Mar 2005)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
>> read more

N3-SUBSTITUTED IMIDAZOPYRIDINE-DERIVATIVES AS C-KIT INHIBITORS (Fri, 11 Mar 2005)
Compounds represented by Formula (I): (I) or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
>> read more

N-SUBSTITUTED BENZIMIDAZOLYL C-KIT INHIBITORS (Fri, 11 Mar 2005)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer. </p>
>> read more

N-SUBSTITUTED PYRAZOLYL-AMIDYL-BENZIMIDAZOLYL C-KIT INHIBITORS (Fri, 11 Mar 2005)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.</p>
>> read more

N3-SUBSTITUTED IMIDAZOPYRIDINE-DERIVATIVES AS C-KIT INHIBITORS (Fri, 11 Mar 2005)
Compounds represented by Formula (I): (I) or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.</p>
>> read more

4-heterocyclo-pyrrolo[2,3d] pyrimidine compositions and their use (Fri, 25 Feb 2005)
<p id="p-0001-en" num="0000">Novel deazapurines are disclosed which are useful for the treatment of adenosine receptor stimulated diseases.</p>
>> read more

5’-AND 3’-CAPPED APTAMERS AND USES THEREFOR (Fri, 18 Feb 2005)
The invention provides compositions and methods for the treating disease using aptamers having 5’-5’and 3’-3’ inverted nucleotide capped ends. In particular, the invention provides 5’-5’ and 3’-3’ capped and-VEGF aptamers of the treatment of neovascularization-related diseases and disorders including age-related macular degeneration.
>> read more

NAPHTHYLENE DERIVATIVES AS CYTOCHROME P450 INHIBITORS (Fri, 28 Jan 2005)
Compounds of the formula (I); and pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, G 1,Q1, Z, R1, R2, R3, R4a, R4b, R5a, and R5b are defined herein, inhibit the cytochrome P450RAI enzyme and are useful for the treatment and/or prevention of various diseases and conditions which respond to treatment by retinoids and by naturally occurring retinoic acid.
>> read more

NAPHTHYLENE DERIVATIVES AS CYTOCHROME P450 INHIBITORS (Fri, 28 Jan 2005)
Compounds of the formula (I); and pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, G 1,Q1, Z, R1, R2, R3, R4a, R4b, R5a, and R5b are defined herein, inhibit the cytochrome P450RAI enzyme and are useful for the treatment and/or prevention of various diseases and conditions which respond to treatment by retinoids and by naturally occurring retinoic acid. </p>
>> read more

PYRROLOPYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE (Thu, 21 Oct 2004)
A compound having the structure wherein, R<sb>1</sb> is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, -C(=O)NR<sb>a</sb>R<sb>b</sb>, -NR<sb>a</sb>R<sb>b</sb>, -NRaC(=O)NR<sb>a</sb>R<sb>b</sb>, -NR<sb>a</sb>C(=O)OR<sb>a</sb>, -OC(=O)NR<sb>a</sb>R<sb>b</sb>, or -NHC(=O)R<sb>a</sb>; R<sb>2</sb> is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxyl, carboxyl, -C(=O)NR<sb>a</sb>R<sb>b</sb>, -NR<sb>a</sb>R<sb>b</sb>, -NR<sb>a</sb>C(=O)NR<sb>a</sb>R<sb>b</sb>, -NR<sb>a</sb>C(=O)OR<sb>a</sb>, -OC(=O)NR<sb>a</sb>R<sb>b</sb>, or -NHC(=O)R<sb>a</sb>, or R<sb>1</sb>, R<sb>2</sb> and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with -(CH<sb>2</sb>)<sb>2</sb>OH or -CH<sb>2</sb>C(=O)OH; R<sb>3</sb> is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C<sb>1</sb>-C<sb>15</sb>)alkyl, (C<sb>1</sb>-C<sb>15</sb>)alkoxyl, or -NR<sb>a</sb>R<sb>b</sb>; R<sb>4</sb> is hydrogen or substituted or unsubstituted (C<sb>1</sb>-C<sb>15</sb>)alkyl; R<sb>5</sb> is -(CH<sb>2</sb>)<sb>m</sb>OR<sb>6</sb>, -CHNOR<sb>7</sb>, -C(=O)NR<sb>8</sb>R<sb>9</sb>, -(CH<sb>2</sb>)<sb>m</sb>C(=O)OR<sb>10</sb>, -(CH<sb>2</sb>)<sb>k</sb>C(=O)NR<sb>11</sb>R<sb>12</sb>.
>> read more

PYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE (Thu, 14 Oct 2004)
The subject invention provides compounds having the structure&colon;&comma; wherein R<sb>1</sb> is substituted or unsubstituted phenyl or a 5−6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms&semi; R<sb>2</sb> is hydrogen&comma; or a substituted or unsubstituted alkyl&comma; −C&lpar;O&rpar;−alkyl&comma; −C&lpar;O&rpar;−O−alkyl&comma; alkoxy&comma; cycloalkyl&comma; alkenyl&comma; monocyclic or bicyclic aryl&comma; heteroaryl or heterocyclic moiety&semi; R<sb>3</sb> is hydrogen&comma; or a substituted or unsubstituted alkyl&comma; −C&lpar;O&rpar;−alkyl&comma; −C&lpar;O&rpar;−O−alkyl&comma; alkoxy&comma; cycloalkyl&comma; alkenyl&comma; monocyclic or bicyclic aryl&comma; heteroaryl or heterocyclic moiety&comma; or R<sb>2</sb> and R<sb>3</sb> are joined to form a heterocyclic ring&semi; wherein the dashed line represents a second bond which may be present or absent&comma; and when present R<sb>3</sb> is oxygen&semi; R<sb>4</sb> and R<sb>5</sb> are each independently substituted or unsubstituted alkyl&comma; −C&lpar;O&rpar;−alkyl&comma; −C&lpar;O&rpar;−O−alkyl&comma; alkoxy&comma; cycloalkyl&comma; alkenyl&comma; monocyclic or bicyclic aryl&comma; heteroaryl or heterocyclic moiety&comma; or R<sb>4</sb>NR<sb>5</sb> together form a substituted or unsubstituted monocyclic or bicyclic&comma; heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms&semi; R<sb>12</sb> is hydrogen&comma; alkyl&comma; halogen or cyano&semi; and n is 0&comma; 1&comma; 2&comma; 3 or 4&comma; or an enantiomer&comma; or a specific tautomer&comma; or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A<sb>2b</sb> adenosine receptor by administering a therapeutically effective amount of the compounds of the invention&period;
>> read more

Compounds specific to adenosine A1 and A3 receptors and uses thereof (Thu, 02 Sep 2004)
This invention pertains to compounds which specifically inhibit the adenosine A<sb>1</sb> and A<sb>3</sb> receptors and the use of these compounds to treat a disease associated with A<sb>3</sb> adenosine receptor in a subject&comma; comprising administering to the subject a therapeutically effective amount of the compounds&period;
>> read more

PROCESSES FOR THE PREPARATION OF SUBSTITUTED BICYCLIC DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH (Thu, 26 Aug 2004)
The invention relates to processes for preparing compounds of formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R?1¿, R?3¿, R?4¿, R?5¿, R?11¿, m and p are as defined herein. The compounds of formula (1) are useful in treating abnormal cell growth in mammals by administering pharmaceutical compositions.
>> read more

(2-CARBOXAMIDO) (3-AMINO) THIOPHENE COMPOUNDS (Fri, 30 Jul 2004)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1 is Formula (II, III, IV, V or VI); R2 is Formula (VII, VIII, IX or X); and R3 is C0-4 alkyl, are useful in the treatment of cancer.
>> read more

(2-CARBOXAMIDO)(3-AMINO) THIOPHENE COMPOUNDS (Fri, 30 Jul 2004)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1 is Formula (II, III, IV, V or VI); R2 is Formula (VII, VIII, IX or X); and R3 is C0-4 alkyl, are useful in the treatment of cancer. </p>
>> read more

COMPOUNDS SPECIFIC TO ADENOSINE A1,A2A, AND A3 RECEPTOR AND USES THEREOF (Thu, 29 Jul 2004)
Abstract <br>is invention pertains to compounds which specifically inhibit the adenosine A<sub>2A</sub>, and A<sub>3</sub> eptors and the use of these compounds to treat a disease associated with A^ A<sub>2A</sub>, and A<sub>3</sub> enosine receptors in a subjects, comprising administering to the subject a therapeutically
>> read more

METHOD FOR PREPARING CAMPTOTHECIN DERIVATIVES AND SOME NOVEL INTERMEDIATES THEREOF (Wed, 02 Jun 2004)
A method of preparing a compound of the formula 994 י" ב בסיון התשס" ד - June 1, 2004 which comprises dihydroxylating a compound of the formula to form a compound of the formula which is subsequently oxidized to the compound of formula I, wherein: R1 and R2, which may be the same or different, are independently selected from hydrogen, lower alkyl, (C3-7) cycloalkyl, (C3-7) cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, or alkoxy alkyl, or (-CH2NR7R8), wherein (i) R7 and R8, which may be the same or different, are independently selected from hydrogen, lower alkyl, (C3-7) cycloalkyl, (C3-7) cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, or lower alkoxy lower alkyl; or (ii) R7 represents hydrogen, lower alkyl, (C3-7) cycloalkyl, (C3-7) cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, 995 י" ב בסיון התשס" ד - June 1, 2004 or lower alkoxy lower alkyl, and R8 represents -COR9, wherein R9 represents hydrogen, lower alkyl, perhalo-lower alkyl, (C3-7) cycloalkyl, (C3-7) cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy, lower alkoxy lower alkyl; or (iii) R7 represents hydrogen or lower alkyl; and R8 represents diphenyl-methyl or -(CH2)tAr wherein t is 0 to 5 and Ar represents phenyl, furyl, pyridyl, N-methylpyrrolyl, imidazolyl optionally substituted with one or more substitutents selected from hydroxy, methyl, halogen, and amino; or (iv) R7 and R8 taken together with the linking nitrogen form a saturated 3 to 7 atom heterocyclic group of the formula Y represents O, S, SO, SO2, CH2 or NR10, wherein R10 represents hydrogen, lower alkyl, perhalo lower alkyl, aryl, aryl substituted with one or more substituents selected from lower alkyl, lower alkoxy, halogen, nitro, amino, lower alkyl amino, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups or -COR11, wherein: R11 represents hydrogen, lower alkyl, perhalo-lower alkyl, lower alkoxy, aryl, aryl substituted with one or more substituents selected from lower alkyl, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups; and R3 and R4 are independently selected from hydrogen, lower alkyl, (C3-7) cycloalkyl, (C3-7) cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, or alkoxy alkyl; or R3 and R4 taken together form a saturated 5 to 6 atom heterocyclic group of the formula wherein n represents the integer 1 or 2; or R3 represents -OCONR12R13, wherein, R12 and R13, which may be the same or different, are independently selected from hydrogen, a substituted or unsubstituted alkyl group with 1-4 carbon atoms or a substituted or unsubstituted carbocyclic or heterocyclic group, or R12 and R13 together with the nitrogen atom to which they are bonded form a heterocyclic ring which may be interrupted with -O-, -S- and/or LN-R14 in which R14 is hydrogen, a substituted or unsubstituted alkyl group with 1-4 carbon atoms or a substituted or unsubstituted phenyl group, and R5 represents hydrogen or alkyl, and R6 represents hydrogen or alkyl, and pharmaceutically acceptable salts thereof. Claimed as new is a compound of the formula 996 י" ב בסיון התשס" ד - June 1, 2004 wherein R1 is -(CH2NR7R8) and R2 is selected from hydrogen, lower alkyl, (C3-7) cycloalkyl, (C3-7) cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, or alkoxy alkyl, or (-CH2NR7R8), wherein: (i) R7 and R8, which may be the same or different, are independently selected from hydrogen, lower alkyl, (C3-7) cycloalkyl, (C3-7) cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, or lower alkoxy lower alkyl; or (ii) R7 represents hydrogen, lower alkyl, (C3-7) cycloalkyl, (C3-7) cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, or lower alkoxy alkyl, and R8 represents -COR9, wherein: R9 represents hydrogen, lower alkyl, perhalo-lower alkyl, (C3-7) cycloalkyl, (C3-7) cycloalkyl lower alkyl, lower alkenyl, hydro
>> read more

Compounds specific to adenosine A1 receptors and uses thereof (Fri, 30 Apr 2004)
<p id="p-a-0001-en">This invention pertains to compounds which specifically inhibit the adenosine A<sub>1 </sub>receptor and the use of these compounds to treat a disease associated with A<sub>1 </sub>adenosine receptors in a subject. </p>
>> read more

Compounds specific to adenosine A, receptors and uses thereof (Fri, 30 Apr 2004)
<p id="p-0001-en" num="0000">This invention pertains to compounds which specifically inhibit the adenosine A<sub>1 </sub>receptor and the use of these compounds to treat a disease associated with A<sub>1 </sub>adenosine receptors in a subject.</p>
>> read more

Compounds specific to adenosine A3 receptor and uses thereof (Wed, 04 Feb 2004)
<p id="p-00001-en">This invention pertains to compounds which specifically inhibit the adenosine A<sub>3</sub>receptor and the use of these compounds to treat a disease associated with A<sub>3</sub>adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.</p>
>> read more

Preparation of a camptothecin derivative by intramolecular cyclisation (Fri, 31 Oct 2003)
<p id="p-00001-en">The present invention relates to a method for the preparation for camptothecin and camptothecin-like compounds and to novel intermediates used in this preparation. In particular, the invention provides a process for the preparation of the camptothecin derivative of formula (I′) known by the chemical name “7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(R,S)-camptothecin”, which comprises cyclising the compound of formula (II′), wherein X is halogen, particularly chloro, bromo, or iodo; and when the compound of formula (I′) is obtained as a mixture of enantiomers optionally resolving the mixture to obtain the desired enantiomer; and/or if desired, converting the resulting compound of formula (I′) or a salt thereof into a physiologically acceptable salt or solvate thereof.</p>
>> read more

Conformationallly constrained peptidomimetics as β-turn templates and modulators of SH3 domains (Wed, 29 Oct 2003)
<p id="p-00001-en">Spirolactam compounds useful as inhibitors of protein-protein interactions modulated by SH3 domains are disclosed. Compounds of the invention are also useful as β-turn mimetics. Also disclosed are libraries of compounds of the invention, pharmaceutical compositions of the compounds of the invention, and methods for using the compounds of the invention to inhibit growth of a cell or to inhibit protein-protein interactions modulated by SH3 domains.</p>
>> read more

Pancreatic lipase inhibitor compounds, their synthesis and use (Fri, 17 Oct 2003)
<p id="p-0001-en" num="0000">The subject invention features compounds having the structure: <chemistry id="chem-us-00001-en" num="00001"><img id="emi-c00001-en" he="19.47mm" wi="34.37mm" file="US07064122-20060620-C00001.TIF" alt="embedded image" img-content="photograph" img-format="png"/></chemistry><br/> wherein X is O, S, CH<sub>2 </sub>or NR<sub>5</sub>; Y is O or S; R<sub>1 </sub>is H, substituted or unsubstituted C<sub>1</sub>-C<sub>15 </sub>alkyl, C<sub>1</sub>-C<sub>8 </sub>alkylaryl, —C(O)OR<sub>4</sub>, —C(O)NR<sub>4</sub>R<sub>5</sub>, —CR<sub>6</sub>R<sub>6′</sub>OR<sub>4</sub>, —CR<sub>6</sub>R<sub>6′</sub>OC(O)R<sub>4</sub>, —CR<sub>6</sub>R<sub>6′</sub>OC(O)NHR<sub>7</sub>, —C(O)NR<sub>10</sub>R<sub>11</sub>, —C(O)NR<sub>8</sub>R<sub>9</sub>NR<sub>8</sub>R<sub>9</sub>, —N(R<sub>5</sub>)C(O)NHR<sub>5</sub>, or CH<sub>2</sub>R<sub>4</sub>; R<sub>2 </sub>is a substituted or unsubstituted, straight chain C<sub>1</sub>—C<sub>30 </sub>alkyl or branched C<sub>3</sub>-C<sub>30 </sub>alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R<sub>3 </sub>is H or substituted or unsubstituted C<sub>1</sub>-C<sub>6 </sub>alkyl or C<sub>3</sub>-C<sub>10 </sub>cycloalkyl; R<sub>4 </sub>is H or a substituted or unsubstituted, straight chain or branched, C<sub>6</sub>-C<sub>30 </sub>alkyl, aryl, —CH<sub>2</sub>-aryl, aryl —C<sub>1</sub>-C<sub>15 </sub>alkyl, heteroaryl-C<sub>1</sub>-C<sub>15</sub>alkyl or C<sub>3</sub>-C<sub>10 </sub>cycloalkyl; R<sub>5 </sub>is H or a substituted or unsubstituted, straight chain or branched, C<sub>6</sub>-C<sub>30 </sub>alkyl, aryl C<sub>1</sub>-C<sub>30</sub>alkyl, heteroarylalkyl or cycloalkyl; R<sub>6 </sub>and R<sub>6′</sub> are each independently H, substituted or unsubstituted C<sub>1</sub>-C<sub>6 </sub>alkyl, dialkyl or C<sub>3</sub>-C<sub>10 </sub>cycloalkyl or together form a 3-7 membered ring system; R<sub>7 </sub>is H or substituted or unsubstituted C<sub>1</sub>-C<sub>12 </sub>alkyl or C<sub>3</sub>-C<sub>10 </sub>cycloalkyl; R<sub>8 </sub>and R<sub>9 </sub>are each independently H, substituted or unsubstituted C<sub>1</sub>-C<sub>6 </sub>alkyl, C<sub>1</sub>-C<sub>6 </sub>alkoxy, C<sub>1</sub>-C<sub>6 </sub>alkylaryl, or NR<sub>8</sub>R<sub>9 </sub>together form a substituted piperazine or piperidine ring or a dihydro-1H-isoquinoline ring system, or a specific enantiomer thereof, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating diabetes or obesity by administering a therapeutically effective amount of the compounds of the invention. </p>
>> read more

Pyrimidine A2b selective antagonist compounds, their synthesis and use (Fri, 29 Aug 2003)
<p id="p-0001-en" num="0000">The subject invention provides compounds having the structure: <chemistry id="chem-us-00001-en" num="00001"><img id="emi-c00001-en" he="29.89mm" wi="55.63mm" file="US06916804-20050712-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/></chemistry> wherein R<sub>1 </sub>is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R<sub>2 </sub>is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R<sub>3 </sub>is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R<sub>2 </sub>and R<sub>3 </sub>are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R<sub>3 </sub>is oxygen; R<sub>4 </sub>and R<sub>5 </sub>are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R<sub>4</sub>NR<sub>5 </sub>together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; R<sub>12 </sub>is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A<sub>2b </sub>adenosine receptor by administering a therapeutically effective amount of the compounds of the invention. </p>
>> read more

Isothiazole derivatives useful as anticancer agents (Fri, 08 Aug 2003)
<p id="p-0001-en" num="0000">The present invention relates to compounds of 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="21.67mm" wi="59.52mm" file="US07405218-20080729-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X<sup>1</sup>, R<sup>1</sup>, R<sup>2 </sup>and R<sup>3 </sup>are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.</p>
>> read more

Bicyclic pyrimidinyl derivatives and methods of use thereof (Fri, 25 Jul 2003)
<p id="p-a-0001-en">This invention pertains to compounds which specifically bind to the adenosine A1, A2a, and A3 receptors and the use of these compounds to treat a disease associated with the A1, A2a, and A3 adenosine receptors in a subject, comprising administering to the subject a therapeutically effective amount of the compounds. </p>
>> read more

PANCREATIC LIPASE INHIBITOR COMPOUNDS, THEIR SYNTHESIS AND USE (Fri, 04 Jul 2003)
The subject invention features compounds having the structure:, wherein X is O, S, CH2 or NR5; Y is O or S; R1 is H, substituted or unsubstituted C1­C15 alkyl, C1-C8 alkylaryl, -C(O)OR4, -C(O)NR4R5, -CR6R6'OR4,-CR6R6'OC(O)R4, - CR6R6'OC(O)NHR7, -C(O)NR1oR11, -C(O)NR8R9 NR8R9, -N(R5)C(O)NHR5, or CH2R4; R2 is a substituted or unsubstituted, straight chain C1-C30 alkyl or branched C3 C30 alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R3 is H or substituted or unsubstituted C1-C6 alkyl or C3-C10 cycloalkyl; R4 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl, -CH2-aryl, aryl -C1-C15 alkyl, heteroaryl-C1-C15alkyl or C3-C10 cycloalkyl; R5 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl C1-C30alkyl, heteroarylalkyl or cycloalkyl; R6 and R6' are each independently H, substituted or unsubstituted C1-C6 alkyl, dialkyl or C3-C10 cycloalkyl or together form a 3-7 membered ring system; R7 is H or substituted or unsubstituted C1-C12 alkyl or C3-C10 cycloalkyl; R8 and R9 are each independently H, substituted or unsubstituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylaryl, or NR8R9 together form a substituted piperazine or piperidine ring or a dihydro-1H-isoquinoline ring system, or a specific enantiomer thereof, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating diabetes or obesity by administering a therapeutically effective amount of the compounds of the invention.
>> read more

PYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE (Fri, 04 Jul 2003)
The subject invention provides compounds having the structure:, wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; R12 is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A2b adenosine receptor by administering a therapeutically effective amount of the compounds of the invention.
>> read more

PYRROLOPYRIMIDINE A2b SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE (Fri, 04 Jul 2003)
A compound having the structure wherein, R1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, -C(=O)NRaRb, -NRaRb, -NRaC(=O)NRaRb, -NRaC(=O)ORa, -OC(=O)NRaRb, or -NHC(=O)Ra; R2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxyl, carboxyl, -C(=O)NRaRb, -NRaRb, -NRaC(=O)NRaRb, -NRaC(=O)ORa, -OC(=O)NRaRb, or -NHC(=O)Ra, or R1, R2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with -(CH2)2OH or -CH2C(=O)OH; R3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C1-C15)alkyl, (C1-C15)alkoxyl, or -NRaRb; R4 is hydrogen or substituted or unsubstituted (C1-C15)alkyl; R5 is -(CH2)mOR6, -CHNOR7, -C(=O)NR8R9, -(CH2)mC(=O)OR10, -(CH2)kC(=O)NR11R12.
>> read more

PYRROLOPYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE (Fri, 04 Jul 2003)
A compound having the structure wherein, R1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, -C(=O)NRaRb, - NRaRb, -NRaC(=O)NRaRb, -NRaC(=O)ORa, -OC(=O)NRaRb, or -NHC(=O)Ra; R2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxyl, carboxyl, -C(=O)NRaRb, -NRaRb, -NRaC(=O)NRaRb, - NRaC(=O)ORa, -OC(=O)NRaRb, or -NHC(=O)Ra, or R1, R2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with -(CH2)2OH or -CH2C(=O)OH; R3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C1-C15)alkyl, (C1-C15)alkoxyl, or - NRaRb; R4 is hydrogen or substituted or unsubstituted (C1-C15)alkyl; R5 is - (CH2)mOR6, -CHNOR7, -C(=O)NR8R9, -(CH2)mC(=O)OR10, -(CH2)kC(=O)NR11R12. </p>
>> read more

PYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE (Fri, 04 Jul 2003)
The subject invention provides compounds having the structure:, wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, -C(O)-alkyl, - C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; R12 is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A2b adenosine receptor by administering a therapeutically effective amount of the compounds of the invention. </p>
>> read more

PANCREATIC LIPASE INHIBITOR COMPOUNDS, THEIR SYNTHESIS AND USE (Fri, 04 Jul 2003)
The subject invention features compounds having the structure:, wherein X is O, S, CH2 or NR5; Y is O or S; R1 is H, substituted or unsubstituted C1~C15 alkyl, C1-C8 alkylaryl, -C(O)OR4, -C(O)NR4R5, -CR6R6'OR4,-CR6R6'OC(O)R4, - CR6R6'OC(O)NHR7, -C(O)NR1oR11, -C(O)NR8R9 NR8R9, -N(R5)C(O)NHR5, or CH2R4; R2 is a substituted or unsubstituted, straight chain C1-C30 alkyl or branched C3 C30 alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R3 is H or substituted or unsubstituted C1-C6 alkyl or C3-C10 cycloalkyl; R4 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl, - CH2-aryl, aryl -C1-C15 alkyl, heteroaryl-C1-C15alkyl or C3-C10 cycloalkyl; R5 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl C1-C30alkyl, heteroarylalkyl or cycloalkyl; R6 and R6' are each independently H, substituted or unsubstituted C1-C6 alkyl, dialkyl or C3-C10 cycloalkyl or together form a 3-7 membered ring system; R7 is H or substituted or unsubstituted C1-C12 alkyl or C3-C10 cycloalkyl; R8 and R9 are each independently H, substituted or unsubstituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylaryl, or NR8R9 together form a substituted piperazine or piperidine ring or a dihydro-1H-isoquinoline ring system, or a specific enantiomer thereof, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating diabetes or obesity by administering a therapeutically effective amount of the compounds of the invention. </p>
>> read more

2-ARYL PYRROLOGPYRIMIDINES FOR A1 AND A3 RECEPTORS (Fri, 13 Jun 2003)
This invention pertains to compounds which specifically inhibit the adenosine A1 and A3 receptors and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
>> read more

COMPOUNDS SPECIFIC TO ADENOSINE A1 AND A3 RECEPTORS AND USES THEREOF (Fri, 13 Jun 2003)
This invention pertains to compounds which specifically inhibit the adenosine A1 and A3 receptors and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds. </p>
>> read more

Compounds specific to adenosine A3 receptor and uses thereof (Fri, 18 Apr 2003)
<p id="p-00001-en">The subject invention provides a compound having the structure:<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06673802-20040106-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry></p> <p id="p-00002-en">or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A3 adenosine receptor by administering a therapeutically effective amount of the compound.</p>
>> read more

ENANTIOMERS OF 6-[(4-CHLORO-PHENYL)-HYDROXY-(3-METHYL-3H-IMIDAZOL-4-YL)-METHYL]4-[3-(3-HYDROXY-3-METHYL-BUT-1-YNYL)-PHENYL]-1-METHYL-1H-QUINOLIN-2-ONE AND SALTS THEREOF, USEFUL IN THE TREATMENT OF CANCER (Fri, 14 Mar 2003)
This invention relates to the enantiomers of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1H-quinolin-2-one, prodrugs thereof, and pharmaceutically acceptable salts and solvates of said compounds and said prodrugs, that are useful in the treatment of hyperproliferative diseases, such as cancers, in mammals. The invention also relates to processes for the production of enantiomerically pure or optically enriched (+)- or (-)-6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1H-quinolin-2-one enantiomers from a mixture containing two enantiomers using continuous chromatography. The invention further relates to the L-(+)-tartaric acid or (S)-(-)-1,1'-binapthyl-2,2'-diyl hydrogenphosphate salts of (+)-6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1H-quinolin-2-one.
>> read more

Compounds specific to adenosine A1 receptors and uses thereof (Fri, 07 Mar 2003)
<p id="p-00001-en">This invention pertains to compounds which specifically inhibit the adenosine A<sub>1</sub>receptor and the use of these compounds to treat a disease associated with A<sub>1</sub>adenosine receptors in a subject.</p>
>> read more

Preparation of a camptothecin derivative by intramolecular cyclisation (Fri, 07 Mar 2003)
<p id="p-00001-en">The present invention relates to a method for the preparation for camptothecin and camptothecin-like compounds and to novel intermediates used in this preparation. In particular, the invention provides a process for the preparation of the camptothecin derivative of formula (I′) known by the chemical name “7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(R,S)-camptothecin”, which comprises cyclising the compound of formula (II′), wherein X is halogen, particularly chloro, bromo, or iodo; and when the compound of formula (I′) is obtained as a mixture of enantiomers optionally resolving the mixture to obtain the desired enantiomer; and/or if desired, converting the resulting compound of formula (I′) or a salt thereof into a physiologically acceptable salt or solvate thereof.</p>
>> read more

4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof (Fri, 21 Feb 2003)
<p id="p-00001-en">This invention pertains to compounds having the structure:<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06664252-20031216-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry></p> <p id="p-00002-en">wherein NR<sub>1</sub>R<sub>2</sub>is a substituted or unsubstituted 4-8 membered ring; wherein R<sub>3</sub>is a substituted or unsubstituted four to six membered ring; wherein R<sub>5</sub>is H, alkyl, substituted alkyl, aryl, arylalkyl, amino, substituted aryl; wherein R<sub>6</sub>is H, alkyl, substituted alkyl, or cycloalkyl; with the proviso that NR<sub>1</sub>R<sub>2</sub>is not 3-acetamido piperadino, 3-hydroxy pyrrolidino, 3-methyloxy carbonylmethyl pyrolidino, or 3-aminocarbonylmethyl pyrrolidino; with the proviso that NR<sub>1</sub>R<sub>2</sub>is 3-hydroxymethyl piperadino only when R<sub>3</sub>is 4-pyridyl; which specifically inhibit the adenosine A<sub>2a</sub>receptor and the use of these compounds to treat a disease associated with A<sub>2a</sub>adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.</p>
>> read more

Preparation of a camptothecin derivative by intramolecular cyclisation (Thu, 07 Nov 2002)
The present invention relates to a method for preparing intermediates useful in the preparation of camptothecin and camptothecin-like compounds and to the intermediates used in this preparation. In particular, the invention provides a process for the preparation of a compound of formula II' <CHEM> wherein X is halogen, which comprises reacting a compound of formula III <CHEM> with a compound of formula IX' <CHEM>
>> read more

Preparation of pyridone-based phosphotyrosine mimetics and uses thereof (Wed, 16 Oct 2002)
<p id="p-00001-en">Novel pyridone mimetics are disclosed which are useful for the treatment of SH2 domain related diseases.</p>
>> read more

COMPOUNDS SPECIFIC TO ADENOSINE A1, A2A, AND A3 RECEPTOR AND USES THEREOF (Thu, 10 Oct 2002)
This invention pertains to compounds which specifically inhibit the adenosine A¿1?, A¿2A?, and A¿3? receptors and the use of these compounds to treat a disease associated with A¿1?, A¿2A?, and A¿3? adenosine receptors in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
>> read more

Preparation of a camptothecin derivative by intramolecular cyclization (Wed, 09 Oct 2002)
<p id="p-00001-en">The present invention relates to a method for the preparation for camptothecin and camptothecin-like compounds and to novel intermediates used in this preparation. In particular, the invention provides a process for the preparation of the camptothecin derivative of formula (I′) known by the chemical name “7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(R,S)-camptothecin”, which comprises cyclising the compound of formula (II′), wherein X is halogen, particularly chloro, bromo, or iodo; and when the compound of formula (I′) is obtained as a mixture of enantiomers optionally resolving the mixture to obtain the desired enantiomer; and/or if desired, converting the resulting compound of formula (I′) or a salt thereof into a physiologically acceptable salt or solvate thereof.</p>
>> read more

Method of inhibiting neoplastic cells with indole derivatives (Fri, 04 Oct 2002)
<p id="p-0001-en" num="0000">A method for inhibiting neoplastic cells and related conditions by exposing them to substituted indole derivatives.</p>
>> read more

COMPOUNDS SPECIFIC TO ADENOSINE A1, A2A, AND A3 RECEPTOR AND USES THEREOF (Fri, 26 Jul 2002)
This invention pertains to compounds which specifically inhibit the adenosine A1, A2A, and A3 receptors and the use of these compounds to treat a disease associated with A1, A2A, and A3 adenosine receptors in a subjects, comprising administering to the subject a therapeutically effective amount of the compounds.
>> read more

COMPOUNDS SPECIFIC TO ADENOSINE A1, A2A, AND A3 RECEPTOR AND USES THEREOF (Fri, 26 Jul 2002)
This invention pertains to compounds which specifically inhibit the adenosine A1, A2A, and A3 receptors and the use of these compounds to treat a disease associated with A1, A2A, and A3 adenosine receptors in a subjects, comprising administering to the subject a therapeutically effective amount of the compounds. </p>
>> read more

Compounds specific to adenosine A3 receptor and uses thereof (Fri, 19 Jul 2002)
<p id="p-0001-en" num="0000">This invention pertains to compounds which specifically inhibit the adenosine A<sub>3 </sub>receptor and the use of these compounds to treat a disease associated with A<sub>3 </sub>adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.</p>
>> read more

Compounds specific to adenosine A1 receptors and uses thereof (Fri, 17 May 2002)
<p id="p-00001-en">This invention pertains to compounds which specifically inhibit the adenosine A<sub>1</sub>receptor and the use of these compounds to treat a disease associated with A<sub>1</sub>adenosine receptors in a subject.</p>
>> read more

Solid phase synthesis of heterocycles (Wed, 24 Apr 2002)
<p id="p-00001-en">Methods and compounds for the synthesis of heterocycles, including pyrimidine-2,4-diones, are disclosed. Also disclosed are solid supports useful for solid phase synthesis, and methods for making the solid supports.</p>
>> read more

Pyrrolo[2,3d]pyrimidine compositions and their use (Fri, 08 Mar 2002)
<p id="p-00001-en">This invention pertains to compounds having the structure:<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06800633-20041005-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry></p> <p id="p-00002-en">wherein</p> <p id="p-00003-en">R<sub>1</sub>and R<sub>2</sub>are each independently a hydrogen atom, substituted alkyl, or a substituted or unsubstituted aryl, or alkylaryl moiety or together form a substituted or unsubstituted heterocyclic ring, provided that both R<sub>1</sub>and R<sub>2</sub>are both not hydrogen atoms or that neither R<sub>1</sub>or R<sub>2</sub>is 1-phenylethyl; R<sub>3</sub>is a substituted or unsubstituted aryl, or alkylaryl moiety; R<sub>4</sub>is a hydrogen atom or a substituted or unsubstituted alkyl, aryl, or alkylaryl moiety; and R<sub>5</sub>and R<sub>6</sub>are each independently a halogen atom, a hydrogen atom or a substituted or unsubstituted alkyl, aryl, or alkylaryl moiety, and the use of these compounds to treat a disease associated with increased levels of adenosine in a subject.</p>
>> read more

Method for preparing camptothecin derivatives (Fri, 14 Dec 2001)
<p id="p-00001-en">The present invention relates to a process for preparing camptothecin and camptothecin analogs of Formula (I) from compounds of Formula (II) and to novel intermediates useful in their preparation,<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06716982-20040406-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry></p> <p id="p-00002-en">wherein R<sub>1</sub>to R<sub>6</sub>represent various substituents.</p>
>> read more

COMPOUNDS SPECIFIC TO ADENOSINE A1 A2A, AND A3 RECEPTORS AND USES THEREOF (Fri, 08 Jun 2001)
This invention pertains to compounds which specifically inhibit the adenosine A1, A2A, and A3 receptors and the use of these compounds to treat a disease associated with A1, A2A, and A3 adenosine receptors in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
>> read more

COMPOUNDS SPECIFIC TO ADENOSINE A1 A2A, AND A3 RECEPTORS AND USES THEREOF (Fri, 08 Jun 2001)
This invention pertains to compounds which specifically inhibit the adenosine A1, A2A, and A3 receptors and the use of these compounds to treat a disease associated with A1, A2A, and A3 adenosine receptors in a subject, comprising administering to the subject a therapeutically effective amount of the compounds. </p>
>> read more

Fluorinated organosilicon compounds and process for the preparation thereof (Wed, 07 Mar 2001)
<p id="p-00001-en">A fluorine-containing organic silicon compound represented by the following formula 1, which is useful as various industrial base materials required to have performances such as water and oil repellency, anti-fouling properties or release properties and as raw materials therefor. Here, A<sup>f</sup>represents a specific polyfluorohydrocarbon group-containing organic group; R<sup>1</sup>and R<sup>2</sup>which are independent of each other, represent bivalent organic groups; R<sup>3</sup>to R<sup>9</sup>which are independent of one another, represent monovalent organic groups; a is an integer of at least 1, and b is an integer of at least 0:<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06197989-20010306-C00001.TIF" img-content="chem"/></chemistry></p>
>> read more

PYRROLO[2,3d]PYRIMIDINE COMPOSITIONS AND THEIR USE (Fri, 10 Dec 1999)
Novel deazapurines are disclosed which are useful for the treatment of adenosine receptor stimulated diseases.
>> read more

Tetracyclic compounds for enhancing biosynthesis of erythropoietin, compositions containing same, and methods of use thereof (Wed, 17 Nov 1999)
<p>The present invention provides a compound in substantially pure form having the structure: ##STR1## wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 may independently be hydrogen, halogen, nitro, CF.sub.3, hydroxy, C.sub.1-5 alkyl, aryl or OR.sub.9, wherein R.sub.9 is C.sub.1-5 alkyl, wherein R.sub.10 is COC.sub.1-5 alkyl; or wherein any two consecutive R groups may be members of a C.sub.5 -C.sub.6 membered ring, and wherein the intracyclic-dashed line represents a covalent bond which may be present or absent, with the proviso that when R.sub.10 is present, the exocyclic-covalent bond is absent, and when R.sub.10 is absent, the exocyclic-covalent bond is present, and with the proviso that when R.sub.10 is absent, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 cannot all be hydrogen and when R.sub.10 is absent, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 cannot all be hydrogen when either R.sub.1, R.sub.2, R.sub.3, or R.sub.4 is hydroxy, or R2 is carboethoxy. The present invention further provides a composition comprising the compound described above in an amount effective to modulate cellular expression of a mammalian gene encoding erythropoietin and a carrier.</p>
>> read more

Fluorine-containing organic compound (Wed, 11 Nov 1998)
<p>A fluorine-containing organic compound of the following formula (1): EQU R.sup.f CH.sub.2 CH.sub.2 CH.sub.2 OCH.sub.2 CH.dbd.CH.sub.2 ( 1) PAL wherein R.sup.f is a C.sub.1-20 fluoroalkyl group.</p>
>> read more

Method for producing a fluorine-containing silicone compound (Wed, 11 Nov 1998)
<p>A method for producing a fluorine-containing silicone compound, which comprises subjecting a fluorine-containing unsaturated compound of the following formula (1) and a hydrosilicone compound having at least one hydrogen atom bonded to a silicon atom to hydrosilylation in the presence of a catalyst to obtain a fluorine-containing silicone compound having a R.sup.f --Q--CR.sup.1 R.sup.2 --CHR.sup.3 --CR.sup.4 R.sup.5 -- group bonded to the silicon atom: EQU R.sup.f --Q--CR.sup.1 R.sup.2 --CR.sup.3 .dbd.CR.sup.4 R.sup.5( 1) PAL wherein R.sup.f is a monovalent fluorine-containing organic group, Q is a single bond or a bivalent organic group, and each of R.sup.1 to R.sup.5 which are independent of one another, is a hydrogen atom or a monovalent organic group, wherein the hydrosilylation is carried out substantially in the absence of a solvent.</p>
>> read more

WATER SOLUBLE 10, 11-ALKYLENEDIOXY COMPTOTHECIN-7-METHANAMINES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (Mon, 05 Jan 1998)

>> read more

Site Search