Assignee: Agouron Pharmaceuticals, Inc.

Location: San Diego, CA
No. of patents: 59

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Number	Title	Issue Date
8067591	Pyrrolopyrazole, potent kinase inhibitors Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4. ...	11/29/2011
7928214	P-cadherin antibodies The present invention relates to antibodies including human antibodies and antigen-binding portions thereof that bind to P-cadherin, and that function to inhibit P-cadherin. The invention also relates to heavy and light chain immunoglobulins derived from human P-cad...	04/19/2011
7858643	Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal ce...	12/28/2010
7807159	Antibodies to myostatin The present invention relates to antibodies including human antibodies and antigen-binding portions thereof that bind to myostatin, and that function to inhibit myostatin. The invention also relates to human anti-myostatin antibodies and antigen-binding portions the...	10/05/2010
7465842	Enantioselective biotransformation for preparation of protein tyrosine kinase inhibitor intermediates The invention relates to biocatalytic methods for preparing enantiomerically pure stereoisomers of 1-(2,6-dichloro-3-fluorophenyl)ethanol. Disclosed are methods of preparation of the desired (S)-enantiomer, which methods are based on a combination of enzymatic resol...	12/16/2008
7462713	Tricyclic compounds protein kinase inhibitors for enhancing the efficacy of anti-neoplastic agents and radiation therapy Protein kinase, such as CHK-1, inhibiting tricyclic compounds of the following formula (wherein R2, R3 and R4 are as defined in the specification) pharmaceutical compositions containing effe...	12/09/2008
7462634	N-(pyridin-2-yl)-sulfonamide derivatives The present invention relates to novel compounds, to pharmaceutical compositions comprising the compounds described herein, their pharmaceutically acceptable salts, hydrates and solvates, as well as to the use of the compounds in medicine and for the preparation of ...	12/09/2008
7452537	P-cadherin antibodies The present invention relates to antibodies including human antibodies and antigen-binding portions thereof that bind to P-cadherin, and that function to inhibit P-cadherin. The invention also relates to heavy and light chain immunoglobulins derived from human P-cad...	11/18/2008
7429578	Tricyclic inhibitors of poly(ADP-ribose) polymerases Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. ...	09/30/2008
7381824	Quinoline derivatives The invention relates to compounds represented by Formula (I): and to pharmaceutically acceptable salts or solvates of said compounds, wherein each of A, R3-8, X3, X5, m, and n are defined h...	06/03/2008
7323562	Method of preparing poly(ADP-ribose) polymerases inhibitors This invention relates to a new and convergent route to small molecule inhibitors of poly(ADP-ribose) polymerase, such as 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, via a key Sonogashira coupling reaction and a CuI...	01/29/2008
7268126	Polymorphic and amorphous forms of the phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-ce]indol-6-one The present invention relates to novel polymorphic and amorphous forms of a phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a compo...	09/11/2007
7232910	Methods of preparing indazole compounds The present invention relates to methods for preparing indazole compounds of formula I, which are useful as modulators and/or inhibitors of protein kinases. The present invention also relates to intermediate comp...	06/19/2007
7217714	CCR5 modulators Compounds of Formula 1 [Region α]−[Region β]−[Region γ]−[Region δ] (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...	05/15/2007
7208500	Thienopyridine-phenylacetamides and their derivatives useful as new anti-angiogenic agents The invention relates to compounds represented by Formula (I): and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein each of X1–X5	04/24/2007
7179918	HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis Compounds of the formula: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceuti...	02/20/2007
7179910	3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related c...	02/20/2007
7173059	Intermediates useful in the synthesis of HIV-protease inhibitors and methods for preparing the same Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed. ...	02/06/2007
7151105	Inhibitors of Hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same The present invention provides compounds of formula (4), and their pharmaceutically acceptable salts and solvates, which are useful as inhibitors of the Hepatitis C virus (HCV) polymerase enzyme and are also useful for the treatment of HCV infections in HCV-infected...	12/19/2006
7148226	Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The ...	12/12/2006
7141585	Pyrazole derivatives This invention relates to the use of pyrazole derivatives of the formula and pharmaceutically acceptable salts and solvates thereof, in the manufacture of a reverse transcriptase inhibitor or modulator, to certain ...	11/28/2006
7141581	Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit un...	11/28/2006
7138408	HIV integrase inhibitors, pharmaceutical compositions and methods for their use Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the a...	11/21/2006
7135482	HIV-integrase inhibitors, pharmaceutical compositions, and methods for their use Bicyclic hydroxamate compounds represented by the Formula I: are described. The bicyclic hydroxamate compounds and compositions containing those compounds may be used to inhibit or modulate an enzyme activity of ...	11/14/2006
7132533	Tricyclic compounds protein kinase inhibitors for enhancing the efficacy of anti-neoplastic agents and radiation therapy Protein kinase, such as CHK-1, inhibiting tricyclic compounds of the following formula (wherein R2, R3 and R4 are as defined in the specification) pharmaceutical compositions cont...	11/07/2006
7125905	Pyrrole substituted 2-indolinone protein kinase inhibitors The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related c...	10/24/2006
7115658	Inhibitors of hepatitis C virus RNA-dependent RNA polymerase Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus ...	10/03/2006
7112603	Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to a...	09/26/2006
7101878	Non-peptide GNRH agents, methods and intermediates for their preparation Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorde...	09/05/2006
7094909	HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis The present invention concerns processes for preparing compounds of formula (I-H), or a prodrug, pharmaceutically active metabolite, or pharmaceutically active salt or solvate thereof, which are useful as inhibit...	08/22/2006
7045646	Process to produce enantiomerically enriched alcohols and amines This invention describes a convenient method for the preparation and use of a ruthenium catalyst for a chiral reduction of ketones and imines. ...	05/16/2006
7008953	3, 5 Disubstituted indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation 3,5 disubstituted indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating CDK dependent diseases to modulate a...	03/07/2006
7001912	HIV-integrase inhibitors, pharmaceutical compositions, and methods for their use Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity...	02/21/2006
6995142	Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis Peptido and peptidomimetic compounds of the formula: wherein the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compoun...	02/07/2006
6995171	Bicyclic pyrimidine and pyrimidine derivatives useful as anticancer agents The invention relates to compounds of the formulas 1 and 2 and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein X, R1 and R11 are as de...	02/07/2006
6989384	Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical ...	01/24/2006
6977302	Triazole derivatives useful in therapy The invention provides compounds of formula I, R1—OP(O)(OH)2 I wherein R1 represents the non-hydroxy portion of a triazole antifungal compound of the type comprising a tertiary hydroxy group; or a pharmaceu...	12/20/2005
6974834	Process for preparing enantiomerically enriched (1S,4R) 1-acetoxy-4-hydroxycyclopent-2-ene This invention relates to a process for the synthesis of enantiomerically enriched (1S,4R) 1-acetoxy-4-hydroxycyclopent-2-ene of Formula I, a compound useful as an intermediate in the synthesis of prostaglandins and prostanoids. ...	12/13/2005
6967198	Tricyclic compounds protein kinase inhibitors for enhancing the efficacy of anti-neoplastic agents and radiation therapy Protein kinase, such as CHK-1, inhibiting tricyclic compounds of the following formula (wherein R2, R3 and R4 are as defined in the specification) pharmaceutical compositions containing...	11/22/2005
6953858	HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis Compounds of the formula: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical co...	10/11/2005

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Assignee: Agouron Pharmaceuticals, Inc.