LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS

Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided. 5. The compound or pharmaceutically acceptable salt of claim 2 , wherein m=1 claim 2 , and wherein Ris hydrogen and Ris selected from the group consisting of optionally substituted phenyl claim 2 , imidazole claim 2 , pyridine claim 2 , thiazole claim 2 , and oxazole.6. The compound or pharmaceutically acceptable salt thereof of claim 2 , wherein m=1 claim 2 , and wherein Rand Rare joined together with the atom to which they are attached to form an optionally substituted azetidine claim 2 , an optionally substituted oxetane claim 2 , an optionally substituted beta-lactam claim 2 , an optionally substituted tetrahydropyran claim 2 , an optionally substituted cyclopropyl claim 2 , an optionally substituted cyclobutyl claim 2 , an optionally substituted cyclopentyl claim 2 , or an optionally substituted cyclohexyl.711.-. (canceled)13. (canceled)15. (canceled)18. (canceled)20. (canceled)21. (canceled)22. (canceled)24. The compound or salt thereof of claim 1 , selected from compounds of Table 1 claim 1 , and pharmaceutically acceptable salts thereof.25. The compound or salt thereof of claim 1 , selected from compounds of Table 2 claim 1 , and pharmaceutically acceptable salts thereof.26. The compound or salt thereof of claim 1 , selected from compounds of Table 3 claim 1 , and pharmaceutically acceptable salts thereof.28. The compound or pharmaceutically acceptable salt thereof of claim 27 , wherein Rand Rare joined together with the atom to which they are attached to form an optionally substituted azetidine claim 27 , an optionally substituted oxetane claim 27 , an optionally substituted beta-lactam claim 27 , an optionally substituted tetrahydropyran claim 27 , an optionally ...

Anti-Fibrotic Pyridinones

Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders. 2. The compound of claim 1 , wherein{'sup': 2', '5', '6', '7', '8, 'Ris selected from the group consisting of halogen, —OR, —NRR, and —C(O)R;'}{'sup': 3', '9, 'sub': 2', 'n', '2', 'n', '3-10', '2', 'n, 'Ris selected from the group consisting of phenyl, —(CH)-(5-10 membered heteroaryl), —(CH)—(Ccarbocyclyl), and —(CH)-(3-10 membered heterocyclyl), each optionally substituted with one or more R;'}{'sup': 9', '5', '14', '15', '8', '16, 'sub': 1-6', '2-6', '2-6', '1-6', '2-8', '3-10', '6-10', '2', '2, 'each Ris independently selected from the group consisting of halogen, optionally substituted Calkyl, optionally substituted Calkenyl, optionally substituted Calkynyl, optionally substituted Calkylthio, optionally substituted Calkoxyalkyl, optionally substituted Ccarbocyclyl, optionally substituted Caryl, —OR, —NRR, —C(O)R, —SOR, and —NO; and'}{'sup': '11', 'sub': 1-6', '2-6', '2-6', '1-6, 'each Ris independently selected from the group consisting of halogen, —CN, optionally substituted Calkyl, optionally substituted Calkenyl, optionally substituted Calkynyl, and optionally substituted Calkoxy.'}3. The compound of claim 1 , wherein Ris a Caryl optionally substituted with one or more R.4. The compound of claim 3 , wherein Ris a phenyl optionally substituted with one or more R.5. The compound of claim 1 , wherein Ris a 5-10 membered heteroaryl optionally substituted with one or more R.6. The compound of claim 5 , wherein Ris a pyrazolyl or 1-methyl pyrazolyl optionally substituted with one or more R.7. The compound of claim 1 , wherein each Ris independently selected from halogen claim 1 , or optionally substituted Calkyl.8. (canceled)9. The compound of claim 7 , wherein Ris methyl.1011.-. (canceled)12. The compound of claim 1 , wherein Ris —CN.13. The compound of claim 1 , wherein Ris —OR.14. The compound of claim 13 , wherein Ris selected from hydrogen ...

Anti-fibrotic pyridinones

Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.

Purine derivatives and their use as anti-coagulants

This invention is directed to purine derivatives of the following formulae: ##STR1## wherein Z 1 is --O--, --N(R 10 )-- or --CH 2 O--; Z 2 is --O--, --N(R 10 )-- or --OCH 2 --; R 1 and R 4 are each independently hydrogen, halo, alkyl, --OR 10 , --C(O)OR 10 , --C(O)N(R 10 )R 11 , --N(R 10 )R 11 , --N(R 10 )C(O)R 10 , or --N(H)S(O) 2 R 13 ; R 2 is --C(NH)NH 2 , --C(NH)N(H)OR 10 , --C(NH)N(H)C(O)OR 13 , --C(NH)N(H)C(O)R 10 , --C(NH)N(H)S(O) 2 R 13 , or --C(NH)N(H)C(O)N(H)R 10 ; R 3 is halo, alkyl, haloalkyl, haloalkoxy, ureido, cyano, guanidino, --OR 10 , --C(NH)NH 2 , --C(NH)N(H)OR 10 , --C(O)N(R 10 )R 11 , --R 12 --C(O)N(R 10 )R 11 , --CH(OH)C(O)N(R 10 )R 11 , --N(R 10 )R 11 , --R 12 --N(R 10 )R 11 , --C(O)OR 10 , --R 12 --C(O)OR 10 , --N(R 10 )C(O)R 10 , (1,2)-tetrahydropyrimidinyl (optionally substituted by alkyl), (1,2)-imidazolyl (optionally substituted by alkyl), or (1,2)-imidazolinyl (optionally substituted by alkyl); R 5 is hydrogen, halo, alkyl, cycloalkyl, haloakyl, aryl, aralkyl, alkylthio, hydroxy, mercapto, alkoxy, or --N(R 10 )R 11 ; and R 6 is defined herein. These compounds are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

NEW MACROCICLIC INHIBITORS BASED ON PIRROLIDINYL OF THE VIRUS REPLICATION OF HEPATITIS C

Compuestos de las fórmulas generales I, II, III, IV, V, VI, VII y X, y composiciones, incluyendo composiciones farmacéuticas, que comprenden dichos compuestos. Además, las realizaciones proveen métodos de tratamiento, incluyendo métodos para tratar una infección de virus de hepatitis C y métodos para tratar la fibrosis hepática, donde los métodos generalmente comprenden administrarle a un individuo que lo necesita una cantidad eficaz de uno de los compuestos o las composiciones de la invención. Compounds of the general formulas I, II, III, IV, V, VI, VII and X, and compositions, including pharmaceutical compositions, comprising said compounds. In addition, the embodiments provide methods of treatment, including methods for treating a hepatitis C virus infection and methods for treating liver fibrosis, where the methods generally comprise administering to an individual in need an effective amount of one of the compounds or compounds. Compositions of the invention.

Menthol substituted antithrombotic pai-1 inhibitors

This invention is directed to menthol-substituted compounds and their pharmaceutically acceptable salts which are useful as antithrombotic agents by inhibiting plasminogen activator inhibitor-1 (PAI-1). In addition, the present invention relates to pharmaceutical compositions and their pharmaceutically acceptable salts, containing the menthol substituted compounds, derivatives of the menthol substituted compounds, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

BENZAMIDINE DERIVATIVES AND THEIR USE AS ANTICOAGULANTS

Benzamidine derivatives, their preparation and use as anticoagulants

Lysophosphatidic acid receptor antagonists

Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.

Plasma carboxypeptidase b inhibitors

Compounds of the following formula (I), for example: (1), wherein R1, R2, R3 and R4 are described herein, are useful as inhibitors of plasma carboxpeptidase B. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.

Plasma carboxypeptidase B inhibitors

Compounds of the following formula (I), for example: wherein R 1 , R 2 , R 3 , and R 4 are described herein, are useful as inhibitors of plasma carboxypeptidase B. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.

Benzamidine derivatives their preparation and their use as anti-coagulants

This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity. Accordingly, in one aspect, this invention provides compounds selected from the group consisting of formulae (I), (II), (III), (IV), (V), (VI), (VII), and (VIII), wherein: A is -C(R11)= or -N=; Z1 and Z2 are independently -O-, -N(R8)-, -S-, or -OCH2-; R1 and R3 are independently hydrogen, halo, alkyl, haloalkyl, alkoxy, haloalkoxy, nitro, -N(R8)R9, -C(O)OR8, -C(O)N(R8)CH2C(O)N(R8)R9, -N(R8)C(O)N(R8)R9, -N(R8)C(O)R8, -N(R8)S(O)2R12, or -N(R8)C(O)N(R8)CH2C(O)N(R8)R9; R2 is hydrogen; halo; alkyl; haloalkoxy; -OR8; -C(O)OR8; -C(O)N(R8)R9; -N(R8)R9; -C(O)N(R8)(CH2)m C(O)OR8 (where m is 0 to 3); -N(R8)(CH2)n C(O)OR8 (where n is 1 to 3); -N((CH2)n N(R1)R9)(CH2)n C(O)OR8 (where each n is 1 to 3); -O(CH2)n C(O)N(R8)R9 (where n is 1 to 3); -O(CH2)p C(O)OR8 (where p is 1 to 6); -N(R8)(CH2)n C(O)N(R8)(CH2)n C(O)OR8 (where each n is independently 1 to 3); morpholin-4-yl; 3-tetrahydrofuranoxyl; etc.; R4 and R7 are independently hydrogen, halo, alkyl, nitro, -OR8, -C(O)OR8, -C(O)N(R8)R9, -N(R8)R9, -N(H)C(O)R8, or -N(H)S(O)2R12; R5 is -C(NH)NH2, -C(NH)N(H)OR8, -C(NH)N(H)C(O)OR12, -C(NH)N(H)S(O)2R12, -C(NH)N(H)C(O)N(R8)R9, or -C(NH)N(H)C(O)R8; R6 is halo, alkyl, haloalkyl, haloalkoxy, nitro, amino, ureido, guanidino, -OR8, -C(NH)NH2, -C(NH)NHOH, -C(O)R10, -(CH2)m C(O)N(R8)R9 (where m is 0 to 3), -CH(OH)C(O)N(R8)R9, -(CH2)m N(R8)R9 (where m is 0 to 3), -(CH2)m C(O)0R8 (where m is 0 to 3), -N(H)C(O)R8, (1,2)-tetrahydropyrimidinyl (optionally substituted by alkyl), (1,2)-imidazolyl (optionally substituted by alkyl), or (1,2)-imidazolinyl (optionally substituted by alkyl); each R8 and R9 is independently hydrogen alkyl, aryl, or aralkyl; R10 is hydrogen, alkyl, aryl, aralkyl, 1-pyrrolidinyl, 4- ...

Benzamidine derivatives and their use as anti-coagulants

This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

Lysophosphatidic acid receptor antagonists

Piperazine derivatives and their use as anti-inflammatory agents

The invention is directed to acyl piperazine derivatiaves of formula Ia (see formula Ia) which are useful as anti-inflammatory agents. This invention is also directe d to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.</S DOAB>

Benzamidine derivatives and their use as anti-coagulants

This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

Benzamidine derivatives their preparation and their use as anti-coagulants

This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity. Accordingly, in one aspect, this invention provides compounds selected from the group consisting of formulae (I), (II), (III), (IV), (V), (VI), (VII), and (VIII), wherein: A is -C(R11)= or -N=; Z1 and Z2 are independently -O-, -N(R8)-, -S-, or -OCH2-; R1 and R3 are independently hydrogen, halo, alkyl, haloalkyl, alkoxy, haloalkoxy, nitro, -N(R8)R9, -C(O)OR8, -C(O)N(R8)CH2C(O)N(R8)R9, -N(R8)C(O)N(R8)R9, -N(R8)C(O)R8, -N(R8)S(O)2R12, or -N(R8)C(O)N(R8)CH2C(O)N(R8)R9; R2 is hydrogen; halo; alkyl; haloalkoxy; -OR8; -C(O)OR8; -C(O)N(R8)R9; -N(R8)R9; -C(O)N(R8)(CH2)m C(O)OR8 (where m is 0 to 3); -N(R8)(CH2)n C(O)OR8 (where n is 1 to 3); -N((CH2)n N(R1)R9)(CH2)n C(O)OR8 (where each n is 1 to 3); -O(CH2)n C(O)N(R8)R9 (where n is 1 to 3); -O(CH2)p C(O)OR8 (where p is 1 to 6); -N(R8)(CH2)n C(O)N(R8)(CH2)n C(O)OR8 (where each n is independently 1 to 3); morpholin-4-yl; 3-tetrahydrofuranoxyl; etc.; R4 and R7 are independently hydrogen, halo, alkyl, nitro, -OR8, -C(O)OR8, -C(O)N(R8)R9, -N(R8)R9, -N(H)C(O)R8, or -N(H)S(O)2R12; R5 is -C(NH)NH2, -C(NH)N(H)OR8, -C(NH)N(H)C(O)OR12, -C(NH)N(H)S(O)2R12, -C(NH)N(H)C(O)N(R8)R9, or -C(NH)N(H)C(O)R8; R6 is halo, alkyl, haloalkyl, haloalkoxy, nitro, amino, ureido, guanidino, -OR8, -C(NH)NH2, -C(NH)NHOH, -C(O)R10, -(CH2)m C(O)N(R8)R9 (where m is 0 to 3), -CH(OH)C(O)N(R8)R9, -(CH2)m N(R8)R9 (where m is 0 to 3), -(CH2)m C(O)0R8 (where m is 0 to 3), -N(H)C(O)R8, (1,2)-tetrahydropyrimidinyl (optionally substituted by alkyl), (1,2)-imidazolyl (optionally substituted by alkyl), or (1,2)-imidazolinyl (optionally substituted by alkyl); each R8 and R9 is independently hydrogen alkyl, aryl, or aralkyl; R10 is hydrogen, alkyl, aryl, aralkyl, 1-pyrrolidinyl, 4- ...

BENZAMIDINE DERIVATIVES, THEIR PRODUCTION AND THEIR USE AS ANTI-COAGULANTS

Piperazine derivatives and their use as anti-inflammatory agents

This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.

Plasma carboxypeptidase b inhibitors

Compounds of the following formula (I), for example: (1), wherein R1, R2, R3, and R4 are described herein, are useful as inhibitors of plasma carboxypeptidase B. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.

Lysophosphatidic acid receptor antagonists

Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.

Piperazine derivatives and their use as anti-inflammatory agents

This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.

Bicyclic pyrimidine derivatives and their use as anti-coagulants

This invention is directed to bicyclic pyrimidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

Novel Inhibitors of Hepatitis C Virus Replication

The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Plasma carboxypeptidase b inhibitors

Compounds of the following formula (I), for example: (1), wherein R1, R2, R3, and R4 are described herein, are useful as inhibitors of plasma carboxypeptidase B. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.

Piperazine derivatives and their use as anti-inflammatory agents

This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.

Piperazine derivatives and their use as anti-inflammatory agents

Plasma carboxypeptidase b inhibitors

Compounds of the following formula (I), for example: (1), wherein R1, R2, R3, and R4 are described herein, are useful as inhibitors of plasma carboxypeptidase B. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.

Benzamidin-derivate, deren herstellung und deren verwendung als anti-koagulantien

Piperazin-derivate und ihre verwendung als entzündungshemmende mittel

Piperazin-derivate und ihre verwendung als entzündungshemmende mittel

Vorrichtung und verfahren für mehrfachen chemischen reaktionen