| Patent Number |
Title Of Patent |
Date Issued |
| H1992 |
Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their pharmaceuti |
September 4, 2001 |
| The present invention relates to compounds of formula I: ##STR1##wherein Ar is an aryl group or a heteroaryl group; X is --NH--OH or --OH; R.sub.1 is H, --CH(R.sub.3)(R.sub.4), --C(O)R.sub.3, a cycloalkyl group, a heterocycloalkyl group, an aryl group, or a heteroaryl group, wherein |
| 7465842 |
Enantioselective biotransformation for preparation of protein tyrosine kinase inhibitor intermed |
December 16, 2008 |
| 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 resolution, chemical es |
| 7462713 |
Tricyclic compounds protein kinase inhibitors for enhancing the efficacy of anti-neoplastic agen |
December 9, 2008 |
| Protein kinase, such as CHK-1, inhibiting tricyclic compounds of the following formula (wherein R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification) ##STR00001## pharmaceutical compositions containing effective amounts of said compounds or their salts are useful as a single |
| 7462634 |
N-(pyridin-2-yl)-sulfonamide derivatives |
December 9, 2008 |
| 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 a medicament which |
| 7452537 |
P-cadherin antibodies |
November 18, 2008 |
| 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-cadherin antibodies and |
| 7429578 |
Tricyclic inhibitors of poly(ADP-ribose) polymerases |
September 30, 2008 |
| 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. ##STR00001## As cancer therapeutics, the compounds of |
| 7381824 |
Quinoline derivatives |
June 3, 2008 |
| The invention relates to compounds represented by Formula (I): ##STR00001## and to pharmaceutically acceptable salts or solvates of said compounds, wherein each of A, R.sup.3-8, X.sup.3, X.sup.5, m, and n are defined herein. The invention also relates to pharmaceutical compositions |
| 7323562 |
Method of preparing poly(ADP-ribose) polymerases inhibitors |
January 29, 2008 |
| 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-promoted indole |
| 7268126 |
Polymorphic and amorphous forms of the phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phen |
September 11, 2007 |
| 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 component of a pharmac |
| 7232912 |
Indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell pr |
June 19, 2007 |
| 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, e.g., kinases-dependent diseases to modulate and/or inhibit unwanted cell |
| 7232910 |
Methods of preparing indazole compounds |
June 19, 2007 |
| The present invention relates to methods for preparing indazole compounds of formula I, which are useful as modulators and/or inhibitors of protein kinases. ##STR00001## The present invention also relates to intermediate compounds useful in the preparation of compounds of formula I. |
| 7217714 |
CCR5 modulators |
May 15, 2007 |
| Compounds of Formula 1 [R.sub.egion .alpha.]-[R.sub.egion .beta.]-[R.sub.egion .gamma.]-[R.sub.egion .delta.] (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds. |
| 7208500 |
Thienopyridine-phenylacetamides and their derivatives useful as new anti-angiogenic agents |
April 24, 2007 |
| The invention relates to compounds represented by Formula (I): ##STR00001## and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein each of X.sup.1 X.sup.5 and R.sup.1 R.sup.5 are defined herein. The invention also relates t |
| 7179918 |
HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materia |
February 20, 2007 |
| Compounds of the formula: ##STR00001## 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 compositions containing these compounds, are useful for |
| 7179910 |
3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors |
February 20, 2007 |
| 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 cellular disorders |
| 7173059 |
Intermediates useful in the synthesis of HIV-protease inhibitors and methods for preparing the s |
February 6, 2007 |
| 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. ##STR00001## |
| 7151105 |
Inhibitors of Hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments us |
December 19, 2006 |
| 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 mammals. The pres |
| 7148226 |
Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments us |
December 12, 2006 |
| The invention relates to compounds of the formula 1 ##STR00001## and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R.sup.1 and R.sup.2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mam |
| 7141587 |
Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods f |
November 28, 2006 |
| 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 unwanted cell prolif |
| 7141585 |
Pyrazole derivatives |
November 28, 2006 |
| This invention relates to the use of pyrazole derivatives of the formula ##STR00001## and pharmaceutically acceptable salts and solvates thereof, in the manufacture of a reverse transcriptase inhibitor or modulator, to certain novel such pyrazole derivatives and to processes for the |
| 7141581 |
Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods f |
November 28, 2006 |
| 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 unwanted cell prolif |
| 7138408 |
HIV integrase inhibitors, pharmaceutical compositions and methods for their use |
November 21, 2006 |
| Beta-carboline hydroxamic acid compounds represented by formula (I) ##STR00001## are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase |
| 7135482 |
HIV-integrase inhibitors, pharmaceutical compositions, and methods for their use |
November 14, 2006 |
| Bicyclic hydroxamate compounds represented by the Formula I: ##STR00001## are described. The bicyclic hydroxamate compounds and compositions containing those compounds may be used to inhibit or modulate an enzyme activity of HIV Integrase and to treat HIV mediated diseases and condit |
| 7132533 |
Tricyclic compounds protein kinase inhibitors for enhancing the efficacy of anti-neoplastic agen |
November 7, 2006 |
| Protein kinase, such as CHK-1, inhibiting tricyclic compounds of the following formula (wherein R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification) ##STR00001## pharmaceutical compositions containing effective amounts of said compounds or their salts are useful as a single |
| 7125905 |
Pyrrole substituted 2-indolinone protein kinase inhibitors |
October 24, 2006 |
| 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 cellular disorders |
| 7115658 |
Inhibitors of hepatitis C virus RNA-dependent RNA polymerase |
October 3, 2006 |
| 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 ##STR00001## |
| 7112603 |
Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives |
September 26, 2006 |
| 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 abnormal PK activity ut |
| 7109228 |
Pyrazole derivatives |
September 19, 2006 |
| This invention relates to pyrazole derivatives of formula (I) ##STR00001## or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such |
| 7101878 |
Non-peptide GNRH agents, methods and intermediates for their preparation |
September 5, 2006 |
| 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 disorders and steroid hor |
| 7094909 |
HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materia |
August 22, 2006 |
| 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, ##STR00001## which are useful as inhibitors of the HIV protease enzyme. |
| 7070071 |
Dispensing apparatus and method for liquid products, particularly medicinal products |
July 4, 2006 |
| A dispensing apparatus for a liquid product, the apparatus comprising a) a housing (2) or frame (3), b) a receptacle (4) for the liquid with a feed nozzle (4a) arranged substantially stationary with respect to the housing or frame, c) a dosing chamber (11) having an orifice (11a), d) a |
| 7063687 |
Eye fluid applicator |
June 20, 2006 |
| An eye fluid applicator comprising a) a hand grip part having a distal end and a proximal end, the distal end and the proximal end defining a axis therebetween and a distal direction and a proximal direction along said axis, b) a container, or a seat for a container, having a bottle part |
| 7053107 |
Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods f |
May 30, 2006 |
| Indazole compounds that modulate and/or inhibit the ophthalmic diseases and 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 |
| 7045646 |
Process to produce enantiomerically enriched alcohols and amines |
May 16, 2006 |
| This invention describes a convenient method for the preparation and use of a ruthenium catalyst for a chiral reduction of ketones and imines. |
| 7045528 |
Benzofused heterozryl amide derivatives of thienopyridines useful as therapeutic agents, pharmac |
May 16, 2006 |
| The invention relates to compounds represented by the formula I ##STR00001## and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, wherein Z, Y, R.sup.11 and R.sup.14, R.sup.15, R.sup.16, and |
| 7022846 |
Metabolites of prinomastat and their synthesis |
April 4, 2006 |
| Metabolites of a matrix metalloproteinase inhibitor prinomastat and their synthesis. These metabolites are: (3S)-N-hydroxy-4-(4-((1-oxy-pyrid-4-yl)oxy)benzenesulfonyl)-2,2-dimethyl-- tetrahydro-2H-1,4-thiazine-3-carboxamide (M6); (3S)-2,2-dimethyl-1,1-dioxo-4-[4-(1-oxy-pyridin-4-yloxy |
| 7008953 |
3, 5 Disubstituted indazole compounds, pharmaceutical compositions, and methods for mediating or |
March 7, 2006 |
| 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 and/or inhibit unwa |
| 7001912 |
HIV-integrase inhibitors, pharmaceutical compositions, and methods for their use |
February 21, 2006 |
| Beta-carboline hydroxamic acid compounds represented by formula (I) ##STR00001## are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase |
| 6995171 |
Bicyclic pyrimidine and pyrimidine derivatives useful as anticancer agents |
February 7, 2006 |
| The invention relates to compounds of the formulas 1 and 2 ##STR00001## and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein X, R.sup.1 and R.sup.11 are as defined herein. The invention also relates to pharmaceutical composit |
| 6995142 |
Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their |
February 7, 2006 |
| Peptido and peptidomimetic compounds of the formula: ##STR00001## wherein the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containi |
| 6989384 |
Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their |
January 24, 2006 |
| Compounds of the formula: ##STR00001## 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 compositions containing these compounds, are usefu |
| 6977302 |
Triazole derivatives useful in therapy |
December 20, 2005 |
| The invention provides compounds of formula I,wherein R.sup.1 represents the non-hydroxy portion of a triazole antifungal compound of the type comprising a tertiary hydroxy group; or a pharmaceutically acceptable sat thereof.The compounds of the invention are useful in the treatment of funga |
| 6974834 |
Process for preparing enantiomerically enriched (1S,4R) 1-acetoxy-4-hydroxycyclopent-2-ene |
December 13, 2005 |
| 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. ##STR1## |
| 6967198 |
Tricyclic compounds protein kinase inhibitors for enhancing the efficacy of anti-neoplastic agen |
November 22, 2005 |
| Protein kinase, such as CHK-1, inhibiting tricyclic compounds of the following formula (wherein R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification) ##STR1##pharmaceutical compositions containing effective amounts of said compounds or their salts are useful as a single a |
| 6964957 |
Fused pyrazole compounds, pharmaceutical compositions, and methods for modulating or inhibiting |
November 15, 2005 |
| Pyrazole compounds represented by the formula: ##STR1##are described. The pyrazole compounds and pharmaceutical compositions containing them may be used in inhibiting ERAB or HADH2 activity and in treating ERAB, HADH2 or amyloid-.beta. mediated diseases and conditions. |
| 6953858 |
HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materia |
October 11, 2005 |
| Compounds of the formula: ##STR1##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 compositions containing these compounds, are useful for trea |
| 6933312 |
Pyrazole derivatives |
August 23, 2005 |
| This invention relates to pyrazole derivatives of formula (I) ##STR1##or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R.sup.1 to R.sup.4, n W, X and Y are defined in the description, and to processes for the preparation thereof, intermediates used in their |
| 6919461 |
Indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell pr |
July 19, 2005 |
| 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, e.g., kinases-dependent diseases to modulate and/or inhibit unwanted cell |
| 6906198 |
Antipicornaviral compounds, their preparation and use |
June 14, 2005 |
| Peptido and peptidomimetic compounds of the formula: ##STR1##wherein the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing the |
| 6903132 |
Non-peptide GnRH agents, pharmaceutical compositions and methods for their use |
June 7, 2005 |
| Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-depend |
