Peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

5'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES

The present invention relates to 5′-Substituted Nucleoside Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein B, X, Y, Z, R, R, Rand R are as defined herein. The present invention also relates to compositions comprising at least one 5′-Substituted Nucleoside Derivative, and methods of using the 5′-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. 2. The compound of claim 1 , wherein X is O.3. The compound of claim 1 , wherein Z is C-Calkyl.4. The compound of claim 1 , wherein Ris Calkyl.7. The compound of claim 5 , wherein Y is H and Z is methyl.8. The compound of claim 5 , wherein Y is H and Z is ethyl.9. The compound of claim 5 , wherein Ris H.11. The compound of claim 5 , wherein R is F or —OH.12. The compound of claim 5 , wherein R is F.14. A pharmaceutical composition comprising an effective amount of one or more of the compounds of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.15. The pharmaceutical composition of further comprising an additional therapeutic agent selected from the group consisting of HCV antiviral agents claim 14 , immunomodulators claim 14 , and anti-infective agents.16. The pharmaceutical composition of claim 15 , wherein said additional therapeutic agent is selected from the group consisting of HCV protease inhibitors claim 15 , HCV NS5A inhibitors and HCV NS5B polymerase inhibitors.17. The use of the compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in the preparation of a medicament for inhibiting HCV NS5A activity or for preventing and/or treating infection by HCV in a patient in need thereof.18. A method of treating a patient infected with HCV comprising administering an amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , effective to prevent and/or treat infection by HCV in said patient.19. The method of claim 18 , further ...

Sulfur compounds as inhibitors of Hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): 130-. (canceled)321. The composition of claim , wherein the additional therapeutic agent is an acetylcholinesterase inhibitor.331. The composition of claim , wherein the acetylcholinesterase inhibitor is donepezil.35. The composition of claim 34 , wherein the additional therapeutic agent is an acetylcholinesterase inhibitor.365. The composition of claim claim 34 , wherein the acetylcholinesterase inhibitor is donepezil.38. The method of claim 37 , wherein the treating is for Alzheimer's Disease.39. The method of claim 38 , wherein the treating is for mood disorder.40. The method of claim 39 , wherein the mood disorder is depression.41. The method of claim 38 , further comprising administration of an acetylcholinesterase inhibitor.42. The method of claim 41 , wherein the acetylcholinesterase inhibitor is donepezil.44. The method of claim 43 , wherein the treating is for Alzheimer's Disease.45. The method of claim 43 , wherein the treating is for mood disorder.46. The method of claim 45 , wherein the mood disorder is depression.47. The method of claim 44 , further comprising administration of an acetylcholinesterase inhibitor.48. The method of claim 47 , wherein the acetylcholinesterase inhibitor is donepezil. The invention is directed to certain chromane, isochromane, and dihydroisobenzofuran derivatives, their salts, pharmaceutical compositions comprising them and their use in therapy of the human body. The compounds of the invention have been found to modulate the metabotropic glutamate receptor 2 (mGluR2), and hence are expected to be useful in the treatment of Alzheimer's Disease and other diseases mediated by the mGuR2 receptor.The metabotropic glutamate receptors are known to contain one or more allosteric sites, which may alter the affinity with which glutamate and other metabotropic glutamate (mGuR) ligands bind to the primary binding ...

Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Substituted pyridine and pyrimidine derivatives and their use in treating viral infections

The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.

Diaryl peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention is directed to certain diaryl amide compounds as NS3-Serine protease inhibitors of hepatitis C virus. A particularly preferred compound is of the formula: ...

Inhibitors of hepatitis C virus NS3 protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such peptides as well as methods of using them to treat disorders associated with the HCV protease.

Benzimidazole hexahydrofuro[3,2-b]furan derivatives

The novel benzimidazole hexahydrofuro[3,2-B]furan derivatives of the present invention are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

2-amino-n-heteroaryl-nicotinamides as Nav1.8 inhibitors

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Na v 1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Na v 1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.

CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3Aare as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild congnitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or ...

5′-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

The present invention relates to 5′-Substituted Nucleoside Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein X, Y, Z, R 1 , R 2 and R 3 are as defined herein and B is a 7-deaza-9-purinyl moiety. The present invention also relates to compositions comprising at least one 5′-Substituted Nucleoside Derivative, and methods of using the 5′-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

Macrocyclic NS-3 serine protease inhibitors of hepatitis C virus comprising alkyl and aryl alanine P2 moieties

The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such macrocycles as well as methods of using them to treat disorders associated with the HCV protease.

Novel compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Ethynyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections

The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and pro-drugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.

Compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Novel inhibitors of hepatitis C virus NS3 protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such peptides as well as methods of using them to treat disorders associated with the HCV protease.

Sulfur compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Diaryl peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention is directed to certain diaryl amide compounds as NS3-Serine protease inhibitors of hepatitis C virus. A particularly preferred compound is of the formula:

Novel compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Substituted pyridine and pyrimidine derivatives and their use in treating viral infections

The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.

Novel substituted prolines as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

2-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

The present invention relates to 2′-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Azido Substituted Nucleoside Derivative, and methods of using the 2′-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

Inhibitors of hepatitis C virus NS3 protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Imidazolidinones as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel imidazolidinones which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazolidinones as well as methods of using them to treat disorders associated with the HCV protease.

Macrocyclic NS-3 serine protease inhibitors of hepatitis C virus comprising alkyl and aryl alanine P2 moieties

The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such macrocycles as well as methods of using them to treat disorders associated with the HCV protease.

Compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Substituted pyrazolo[3,4-d]pyrimidines as PDE9 inhibitors

The present invention is directed to pyrazolopyrimidine compounds of the general structural formula I:which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS

The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R, X, Y, Z, R, R, R, R, R, R, R, R, R, Rand n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders. 3. A compound according to claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein:X and Y are each N;{'sub': '3', 'Z is selected from the group consisting of H, —CH, and cyclopropyl; and'}{'sup': '2', 'Ris H.'}9. A compound claim 1 , according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , said compound selected from the group consisting of Compound Nos.:2415, 2502, 2504, 2505, 2508, 2509, 2510, 2511, 2512, 2513, 2514, 2516, 2518, 2519, 2520, 2521, 2526, 2527, 2531, 2532, 2533, 2535, 2536, 2537, 2539, 2540, 2541, 2542, 2543, 2544, 2545, 2546, 2547, 2549, 2550, 2553, 2555, 2556, 2559, 2562, 2563, 2564, 2565, 2566, 2567, 2568, 2569, 2503, 2507, 2517, 2522, 2523, 2524, 2525, 2534, 2538, 2548, 2552, 2554, 2557, 2558, 2560, 2561, 2501, 2506, 2528, 2529, 2530, 3001, 3006, 3007, 3011, 3013, 3016, 3017, 3018, 3019, 3020, 3021, 3022, 3023, 3024, 3025, 3026, 3028, 3029, 3030, 3031, 3032, 3033, 3034, 3035, 3036, 3037, 3038, 3039, 3040, 3041, 3042, 3043, 3044, 3045, 3046, 3047, 3048, 3049, 3050, 3051, 3052, 3053, 3054, 3055, 3056, 3057, 3058, 3059, 3060, 3061, 3062, 3063, 3064, 3065, 3066, 3067, 3068, 3104, 3105, 3106, 3107, 3108, 3109, 3111, 3112, 3113, 3114, 3115, 3116, 3117, 3118, 3119, 3120, 3121, 3122, 3123, 3125, 3126, 3127, 3129, 3130, 3132, 3133, 3135, 3136, 3137, 3138, 3139, 3141, 3142, 3144, 3145, 3146, 3147, 3148, 3149, 3153, 3154, 3155, ...

Peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

NOVEL PEPTIDES AS NS3-SERINE PROTEASE INHIBITORS OF HEPATITIS C VIRUS

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Azabenzimidazole hexahydrofuro[3,2-b]furan derivatives

Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

Novel imidazolidinones as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel imidazolidinones which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazolidinones as well as methods of using them to treat disorders associated with the HCV protease.

Novel compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Novel ketoamides with cyclic P4'S as inhibitors of NS3 protease of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Chromane, isochromane and dihydroisobenzofuran derivatives as mGluR2-negative allosteric modulators, compositions, and their use

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3Aare as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more ...

5′-substituted nucleoside analogs and methods of use thereof for the treatment of viral diseases

The present invention relates to 5′-Substituted Nucleoside Analogs of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, Z, R 1 , R 2 , R 3 and R 3′ are as defined herein. The present invention also relates to compositions comprising at least one 5′-Substituted Nucleoside Analog, and methods of using the 5′-Substituted Nucleoside Analogs for treating or preventing HCV infection in a patient.

Compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R, R, L, X, X, and X, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders. 3. A compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein{'sup': '1', 'Ris selected from the group consisting of phenyl, cyclobutyl, cyclohexyl, cyclopentyl, benzimidazolyl, imidazolyl, imidazopyridinyl, imidazopyridinyl, imidazopyrimidinyl, isoxazolyl, oxadiazolyl, oxadiazolyl, oxazolyl, oxetanyl, piperidinyl, pyrazolyl, pyridinyl, pyrimidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrazolyl, thiadiazolyl, thiazolyl, and triazolyl; and'}{'sup': '1A', 'sub': 1-4', '1-4', '1-4', '1-4', '2', '2', '2', '1-4, 'Ris 1, 2, or 3 groups independently selected from the group consisting of F, OH, —(C)alkyl, —(C)haloalkyl, —(C)alkoxy, —(C)haloalkoxy, cyclopropyl, cyclobutyl, —NH, —C(O)NH, and —S(O)—(C)alkyl.'}4. A compound of claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , wherein{'sup': '2', 'Ris selected from the group consisting of phenyl, azetidinyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, imidazolyl, isothiazolyl, morpholinyl, oxazolyl, piperazinyl, piperidinyl, pyrazolyl, pyridazinyl, pyridinyl, pyrimidinyl, pyrrolidinyl, and thiazolyl; and'}{'sup': '2A', 'sub': 1-4', '1-4', '1-4, 'Ris 1, 2, or 3 groups independently selected from the group consisting of H, halo, CN, —(C)alkyl, —(C)haloalkyl, —(C)alkoxy, cyclopropyl, ...

Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

2'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES

The present invention relates to 2′-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R, Rand Rare as defined herein. The present invention also relates to compositions comprising at least one 2′-Substituted Nucleoside Derivative, and methods of using the 2′-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. 2. The compound of claim 1 , wherein X is O.3. The compound of or claim 1 , wherein Ris methyl.64. The compound of any of - claims 1 , wherein A is —NH.9468. The compound of any one of - or - claim 1 , wherein Ris phenyl.10469. The compound of any one of - or - claim 1 , wherein Ris ethyl or isopropyl.12. The compound of claim 11 , wherein Ris isopropyl.17. The compound of claim 1 , being any one of the compounds numbered 1-99 in the above specification claim 1 , or a pharmaceutically acceptable salt thereof.19. A pharmaceutical composition comprising an effective amount of the compound of any of to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.20. The pharmaceutical composition according to claim 19 , further comprising a second therapeutic agent selected from the group consisting of HCV antiviral agents claim 19 , immunomodulators claim 19 , and anti-infective agents.21. The pharmaceutical composition according to claim 19 , further comprising a third therapeutic agent selected from the group consisting of HCV protease inhibitors claim 19 , HCV NS5A inhibitors and HCV NS5B polymerase inhibitors.22. The use of the compound according to any of to claim 19 , or a pharmaceutically acceptable salt thereof claim 19 , in the preparation of a medicament for inhibiting HCV NS5A activity or for preventing and/or treating infection by HCV in a patient in need thereof.2321. A method of treating a patient infected with HCV comprising the step of administering an amount of (i) the compound according to any of ...

Substituted prolines as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

2-AMINO-N-HETEROARYL-NICOTINAMIDES AS NAV1.8 INHIBITORS

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders. 2. The compound according to wherein Ris hydrogen; or a pharmaceutically acceptable salt thereof.3. The compound according to wherein A is heteroaryl claim 1 , wherein heteroaryl is unsubstituted or substituted with one to four substituents selected from R; or a pharmaceutically acceptable salt thereof.5. The compound according to wherein A is pyridine claim 1 , wherein pyridine is unsubstituted or substituted with one to three substituents selected from R; or a pharmaceutically acceptable salt thereof.8. The compound according to wherein B is pyridine claim 1 , wherein pyridine is unsubstituted or substituted with one to three substituents selected from R; or a pharmaceutically acceptable salt thereof.11. The compound according to wherein Ris selected from the group consisting of: a monocyclic claim 1 , bicyclic or spirocyclic Ccycloalkyl ring claim 1 , and a monocyclic claim 1 , bicyclic or spirocyclic Ccycloheteroalkyl ring claim 1 , wherein the cycloheteroalkyl contains 1-4 heteroatoms independently selected from N(R) claim 1 , O claim 1 , and S claim 1 , and wherein each cycloalkyl and cycloheteroalkyl is unsubstituted or substituted with one to eight substitutents selected from R; or a pharmaceutically acceptable salt thereof.12. The compound according to wherein Ris a monocyclic claim 1 , bicyclic or spirocyclic Ccycloheteroalkyl ring claim 1 , wherein the cycloheteroalkyl contains a nitrogen and 0-3 heteroatoms independently selected from N(R) claim 1 , O claim 1 , and S claim 1 , and wherein each ...

Peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Tetrahydronaphthyridine derivatives as mGluR2-negative allosteric modulators, compositions, and their use

The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, L, X1, X2, and X3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.

ETHYNYL-SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS

The present invention provides compounds of Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and pro-drugs of said compounds, wherein each of R, R, X, Y, Z, R, R, R, R, R, R, R, R, R, Rand n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders. 2. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein:R is selected from aryl, heteroaryl, benzo-fused heteroaryl, cycloalkyl, cycloalkenyl, benzo-fused cycloalkyl, benzo-fused cycloalkenyl, heterocycloalkyl, and benzo-fused heterocycloalkyl,{'sub': 2', '2', '2', '2, 'sup': 10', '10', '11', '10', '10', '11', '10', '10', '11, 'wherein each of said alkyl, said aryl, said heteroaryl, said benzo-fused heteroaryl, said cycloalkyl, said cycloalkenyl, said heterocycloalkyl, said heterocycloaklenyl, and said benzo-fused heterocycloalkyl is unsubstituted or optionally independently substituted with from one to three substituents, which are the same or different, each substituent being independently selected from halo, —OH, —CN, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, heteroalkyl, heterohaloalkyl, -alkyl-OH, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —OC(O)-alkyl, —C(O)NH, —C(O)NHR, —C(O)NRR, —C(O)ONH, —C(O)ONHR, —C(O)ONRR, —NH, —NHR, —NRR, —NO, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said ...

SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS

The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.

Novel inhibitors of hepatitis C virus NS3/NS4a serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Sulfur compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising N-cyclic P2 moieties

The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such macrocycles as well as methods of using them to treat disorders associated with the HCV protease.

CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): 3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein{'sup': '2', 'sub': 3', '3', '2', '2', '2', '3', '3', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '2', '2', '3', '2', '3', '2', '3, 'Ris selected from H, cyclopropyl, —CH, —CH(CH), —CH—OH, —CH—OCH, —CF, —CHCHF, —CHCHF, —CHCF, —CH—O—CHF, —CH—O—CHF, —CH(CH)—O—CHF, —CH(CH)—O—CHF, —CH—NH—CHCF, and —CH—N(CH)—CHCF;'}{'sup': '2A', 'Ris selected from H and methyl;'}{'sup': '3', 'Ris selected from H and methyl; and'}{'sup': '3A', 'Ris selected from H and methyl.'}4. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein{'sup': 2', '2A, 'Rand Rare both methyl; and'}{'sup': 3', '3A, 'Rand Rare both H.'}8. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein:ring B is a moiety selected from the group consisting of phenyl, cyclopentyl, cyclohexyl, pyridinyl, pyrimidinyl, pyrazolyl, thienyl, thiazolyl, thiadiazolyl, isoxazolyl, oxadiazolyl and oxazolyl;n is 0, 1, 2, or 3, provided that the value of n does not exceed the maximum number of substitutable hydrogen atoms on ring B; and{'sup': '1', 'sub': 1', '6', '1', '6', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6, 'each R(when present) is independently selected from the group consisting of halogen, —CN, —OH, —(C-C) alkyl, —O—(C-C) alkyl, —(C-C) haloalkyl, —O—(C-C) haloalkyl, cyclopropyl, cyclobutyl, —NH, —NH(C-C)alkyl, —N(C-Calkyl), —C(O)O(C-C) alkyl, and phenyl.'}9. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein:ring B is a moiety selected from the group consisting of: phenyl, pyrazolyl, pyridinyl, thienyl, isoxazolyl, oxadiazolyl and oxazolyl;n is 0, 1, or 2; and{'sup': '1', 'sub': 3', '2, 'each R(when present) is independently selected from the group consisting of ...

Compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Compounds as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Ketoamides with cyclic P4'S as inhibitors of NS3 protease of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Chromane, isochromane and dihydroisobenzofuran derivatives as mGluR2—negative allosteric modulators, compositions, and their use

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3Aare as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more ...

Azabenzimidazole tetrahydrofuran derivatives

Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

NOVEL INDOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS

Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. 3. The compound according to claim 1 , wherein{'sup': '3', 'T is selected from —CR— and N;'}{'sup': '1', 'U is —CR—;'}{'sup': '2', 'V is —CR—; and'}{'sup': '4', 'W is selected from —CR— and N,'}{'sup': 1', '2, 'sub': 3', '1-6', '2-6', '2-6', '3', '1-6', '2-6', '2-6, 'provided that one of T and W is N, and further provided that if W is N, then Ris selected from hydrogen, halogen, —CN, —CF, —Calkyl, —Calkenyl and —Calkynyl, and if T is N then Ris selected from hydrogen, halogen, —CN, —CF, —Calkyl, —Calkenyl and —Calkynyl;'}or a pharmaceutically acceptable salt thereof.4. The compound according to claim 1 , wherein T is —CR— or N; U is —CR—; V is —CR—; and W is —CR—; or a pharmaceutically acceptable salt thereof.5. The compound according to claim 1 , wherein X is absent or selected from:{'sub': '2', '(1) —CH—,'}(2) —S—,(3) —S(O)—,{'sub': '2', '(4) —S(O)—,'}(5) —O—,{'sub': '2', '(6) —O—CH—,'}{'sub': '2', '(7) —CH—O—,'}{'sub': '2', '(8) —CH—S—,'}(9) —NH—,(10) —C(O)—, and(11) —C(O)NH—,{'sub': 2', '2', '1-6', '2', '2', '1-6', '1-6', '1-6', '2', '2', '1-6', '1-6, 'wherein each CHis unsubstituted or substituted with 1 or 2 substituents selected from: hydroxy, halogen, NH, Calkyl, COH, COCalkyl, and COCalkyl, and wherein each NH is unsubstituted or substituted with 1 substituent selected from: Calkyl, COH, COCalkyl, and COCalkyl;'}or a pharmaceutically acceptable salt thereof.6. The compound according to claim 4 , wherein X is —CH—; or a pharmaceutically acceptable salt thereof.8. The compound according to claim 6 , wherein Y is selected from:{'sub': '1-6', '(1) Calkyl,'}{'sub': '3-10', '(2) Ccycloalkyl, ...

Peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such peptides as well as methods of using them to treat disorders associated with the HCV protease.

Enantio- and stereo specific synthesis of -amino--hydroxy amides

Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.

SULFUR COMPOUNDS AS INHIBITORS OF HEPATITIS C VIRUS NS3 SERINE PROTEASE

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Ketoamides with cyclic P4's as inhibitors of NS3 serine protease of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

2-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

The present invention relates to 2′-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Substituted Nucleoside Derivative, and methods of using the 2′-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising N-cyclic P2 moieties

The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such macrocycles as well as methods of using them to treat disorders associated with the HCV protease.

Indole derivatives useful as anti-diabetic agents

Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Novel compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Novel compounds as inhibitors of hepatitis C virus NS3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

ENANTIO- AND STEREO-SPECIFIC SYNTHESES OF BETA-AMINO-ALPHA- HYDROXY AMIDES

Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed. 123-. (canceled)25. The process of wherein the compounds of Formula II and III are coupled using 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide and 1-hydroxybenzotriazole in the presence of N.N-diisopropylethylamine.26. The process of wherein the compound of Formula IV is oxidized with sodium hypochlorite in the presence of a catalytic or stoichiometric amount of 2 claim 24 ,2 claim 24 ,6 claim 24 ,6 claim 24 ,-tetramethyl-1-piperidinyloxy claim 24 , free radical.28. The process of wherein the compounds of Formula VI and VII are coupled using 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide and 1-hydroxybenzotriazole in the presence of N-methylmorpholine in acetonitrile.29. The process of wherein the compounds of Formula II and III are coupled using 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide and 1-hydroxybenzotriazole in the presence of N.N-diisopropylethylamine.30. The process of wherein the compound of Formula IV is oxidized with sodium hypochlorite in the presence of a catalytic or stoichiometric amount of 2 claim 27 ,2 claim 27 ,6 claim 27 ,6 claim 27 ,-tetramethyl-l-piperidinyloxy claim 27 , free radical.33. The process of wherein Ris methyl.34. The process of wherein the compounds of Formula VI and VII are coupled using 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide and 1-hydroxybenzotriazole in the presence of N-methylmorpholine in acetonitrile.35. The process of wherein the organic solvent in step 2 is ethyl acetate or toluene.36. The process of wherein the antisolvent in step 4 is heptanes.42. The compound of wherein the salt is the hydrochloride.45. The process of wherein the cyclohexanone derivative is VIG.47. The process of for preparing the compound of Formula VI comprising treating an amine of Formula VIBb with phenylchloroformate in ...

Novel inhibitors of Hepatitis C virus NS3 protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

2'-AZIDO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES

The present invention relates to 2′-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R, Rand Rare as defined herein. The present invention also relates to compositions comprising at least one 2′-Azido Substituted Nucleoside Derivative, and methods of using the 2′-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. 2. The compound of claim 1 , wherein X is O.4. The compound of claim 1 , wherein Ris methyl.12. The compound of claim 7 , wherein Ris C-Calkyl.14. The compound of being one of the compounds numbered 1-780 in the above specification.16. A pharmaceutical composition comprising an effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.17. The pharmaceutical composition according to claim 16 , further comprising a second therapeutic agent selected from the group consisting of HCV antiviral agents claim 16 , immunomodulators claim 16 , and anti-infective agents.18. The pharmaceutical composition according to claim 17 , further comprising a third therapeutic agent selected from the group consisting of HCV protease inhibitors claim 17 , HCV NS5A inhibitors and HCV NS5B polymerase inhibitors.19. (canceled)20. A method of treating a patient infected with HCV comprising the step of administering an amount of the compound according to claim 1 , or a pharmaceutically acceptable salt thereof effective to prevent and/or treat infection by HCV in said patient.21. The method according to claim 20 , further comprising the step of administering pegylated-interferon alpha and an HCV protease inhibitor to said patient.22. The method according to claim 20 , further comprising the step of administering ribavirin to said patient.23. The use of the compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in a pharmaceutical composition for inhibiting ...

Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

2-AMINO-N-HETEROARYL-NICOTINAMIDES AS NAV1.8 INHIBITORS

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Na1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Na1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders. 2. The compound according to wherein Ris hydrogen; or a pharmaceutically acceptable salt thereof.3. The compound according to wherein A is heteroaryl claim 1 , wherein heteroaryl is unsubstituted or substituted with one to four substituents selected from R; or a pharmaceutically acceptable salt thereof.5. The compound according to wherein A is pyridine claim 1 , wherein pyridine is unsubstituted or substituted with one to three substituents selected from R; or a pharmaceutically acceptable salt thereof.8. The compound according to wherein B is pyridine claim 1 , wherein pyridine is unsubstituted or substituted with one to three substituents selected from R; or a pharmaceutically acceptable salt thereof.11. The compound according to wherein Ris selected from the group consisting of: a monocyclic claim 1 , bicyclic or spirocyclic Ccycloalkyl ring claim 1 , and a monocyclic claim 1 , bicyclic or spirocyclic Ccycloheteroalkyl ring claim 1 , wherein the cycloheteroalkyl contains 1-4 heteroatoms independently selected from N(R) claim 1 , O claim 1 , and S claim 1 , and wherein each cycloalkyl and cycloheteroalkyl is unsubstituted or substituted with one to eight substitutents selected from R;or a pharmaceutically acceptable salt thereof.12. The compound according to wherein Ris a monocyclic claim 1 , bicyclic or spirocyclic Ccycloheteroalkyl ring claim 1 , wherein the cycloheteroalkyl contains a nitrogen and 0-3 heteroatoms independently selected from N(R) claim 1 , O claim 1 , and S claim 1 , and wherein each ...

Inhibitors of hepatitis C virus NS3/NS4a serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Substituted pyrazolo[3,4-d]pyrimidines as PDE9 inhibitors

The present invention is directed to pyrazolopyrimidine compounds of the general structural formula I: which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

CYCLOBUTYL PYRAZOLOPYRIMIDINE PDE9 INHIBITORS

The present invention is directed to cyclobutyl pyrazolopyrimidine compounds which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Novel ketoamides with cyclic P4's as inhibitors of NS3 serine protease of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

PYRAZOLOPYRIMIDINE PDE9 INHIBITORS

The present invention is directed to amino and alkyl pyrazolopyrimidine compounds which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Novel compounds as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

2-OXOIMIDAZOLIDINE-4-CARBOXAMIDES AS NAV1.8 INHIBITORS

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.

CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): 3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein{'sup': '2', 'sub': 3', '3', '2', '2', '2', '3', '2', '2', '3', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '2', '2', '3', '2', '3', '2', '3, 'Ris selected from H, cyclopropyl, —CH, —CH(CH), —CH—OH, —CH—OCH, —CHF, —CHF, —CF, —CHCHF, —CHCHF, —CHCF, —CH—O—CHF, —CH—O—CHF, —CH(CH)—O—CHF, —CH(CH)—O—CHF, —CH—NH—CHCF, and —CH—N(CH)—CHCF;'}{'sup': '2A', 'Ris selected from H and methyl;'}{'sup': '3', 'Ris selected from H and methyl; and'}{'sup': '3A', 'Ris selected from H and methyl.'}4. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein{'sup': 2', '2A, 'Rand Rare both methyl; and'}{'sup': 3', '3A, 'Rand Rare both H.'}8. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein:ring B is a moiety selected from the group consisting of phenyl, cyclopentyl, cyclohexyl, pyridinyl, pyrimidinyl, pyrazolyl, thienyl, thiazolyl, thiadiazolyl, isoxazolyl, oxadiazolyl and oxazolyl;n is 0, 1, 2, or 3, provided that the value of n does not exceed the maximum number of substitutable hydrogen atoms on ring B; and{'sup': '1', 'sub': 1', '6', '1', '6', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6, 'each R(when present) is independently selected from the group consisting of halogen, —CN, —OH, —(C-C) alkyl, —O—(C-C) alkyl, —(C-C) haloalkyl, —O—(C-C) haloalkyl, cyclopropyl, cyclobutyl, —NH, —NH(C-C)alkyl, —N(C-Calkyl), —C(O)O(C-C) alkyl, and phenyl.'}9. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein:ring B is a moiety selected from the group consisting of: phenyl, pyrazolyl, pyridinyl, thienyl, isoxazolyl, oxadiazolyl and oxazolyl;n is 0, 1, or 2; and{'sup': '1', 'sub': 3', '2, 'each R(when present) is independently selected from ...

5'-SUBSTITUTED NUCLEOSIDE ANALOGS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES

The present invention relates to 5′-Substituted Nucleoside Analogs of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, Z, R, R, Rand R are as defined herein. The present invention also relates to compositions comprising at least one 5′-Substituted Nucleoside Analog, and methods of using the 5′-Substituted Nucleoside Analogs for treating or preventing HCV infection in a patient. 2. The compound of claim 1 , wherein X is O.3. The compound of claim 1 , wherein Z is C-Calkyl.4. The compound of claim 1 , wherein Ris Calkyl.11. The compound of claim 5 , wherein R is halo or —OH.12. The compound of claim 5 , wherein R is F.14. A pharmaceutical composition comprising an effective amount of one or more of the compounds of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.15. The pharmaceutical composition of further comprising an additional therapeutic agent selected from the group consisting of HCV antiviral agents claim 14 , immunomodulators claim 14 , and anti-infective agents.16. The pharmaceutical composition of claim 15 , wherein said additional therapeutic agent is selected from the group consisting of HCV protease inhibitors claim 15 , HCV NS5A inhibitors and HCV NS5B polymerase inhibitors.17. The use of the compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in the preparation of a medicament for inhibiting HCV NS5A activity or for preventing and/or treating infection by HCV in a patient in need thereof.18. A method of treating a patient infected with HCV comprising administering an amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , effective to prevent and/or treat infection by HCV in said patient.19. The method of claim 18 , further comprising the step of administering inhibitor to said patient.20. The method of claim 18 , further comprising the step of administering ribavirin to said patient. The present invention ...

2-AMINO-N-HETEROARYL-NICOTINAMIDES AS NAV1.8 INHIBITORS

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Na1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Na1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders. 2. The compound according to wherein Ris hydrogen; or a pharmaceutically acceptable salt thereof.3. The compound according to wherein A is heteroaryl claim 1 , wherein heteroaryl is unsubstituted or substituted with one to four substituents selected from R; or a pharmaceutically acceptable salt thereof.4. The compound according to wherein A is selected from the group consisting of:(1) pyridine,(2) pyrimidine,(3) pyrazine,(4) indazole,(5) imidazo[1,2-a]pyridine,(6) pyrrolo[3,2-c]pyridine,(7) pyrrolo[2,3-b]pyridine,(8) pyrazole,(9) thiophene, and(10) 1,2,4-oxadiazole,{'sup': 'a', 'wherein A is unsubstituted or substituted with one to four substituents selected from R,'}provided that both A and B are not pyridine;or a pharmaceutically acceptable salt thereof.5. The compound according to wherein A is pyridine claim 1 , wherein pyridine is unsubstituted or substituted with one to four substituents selected from R claim 1 ,provided that both A and B are not pyridine;or a pharmaceutically acceptable salt thereof.6. The compound according to wherein B is selected from the group consisting of:(1) pyrazine,(2) pyridine,(3) pyrimidine, and(4) pyridazine,{'sup': 'b', 'wherein each B is unsubstituted or substituted with one to three substituents selected from R;'}or a pharmaceutically acceptable salt thereof.7. The compound according to wherein B is selected from the group consisting of:(1) pyridine,(2) pyrimidine, and(3) pyridazine,{'sup': 'b', 'wherein each B is unsubstituted or substituted with one to three ...

Pyrazolopyrimidine pde9 inhibitors

which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

NOVEL AZABENZIMIDAZOLE TETRAHYDROFURAN DERIVATIVES

Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. 2. The compound according to wherein one of T claim 1 , V and W is N or N-oxide claim 1 , and U is —CR—; or a pharmaceutically acceptable salt thereof.3. The compound according to wherein T is N or N-oxide; U is —CR—; V is —CR—; and W is —CR—; or a pharmaceutically acceptable salt thereof.4. The compound according to wherein T is N; U is —CR—; V is —CR—; and W is —CR—; or a pharmaceutically acceptable salt thereof.5. The compound according to claim 1 , wherein X is —O—; or a pharmaceutically acceptable salt thereof.8. The compound according to claim 1 , wherein Z is NR; or a pharmaceutically acceptable salt thereof.9. The compound according to claim 1 ,{'sup': 1', '2, 'claim-text': (1) halogen,', {'sub': 2', 'p, '(2) —(CH)aryl-aryl, and'}, {'sub': 2', 'p, '(3) —(CH)aryl-heteroaryl,'}], 'wherein each Rand Ris independently selected from{'sub': 2', '3', '2', '1-6', '1-6', '1-6', '1-6', '2, 'sup': a', '1', '2, 'wherein each CHis unsubstituted or substituted with 1 or 2 substituents selected from: halogen, CF, —OH, —NH, —Calkyl, —OCalkyl, —NHCalkyl, and —N(Calkyl), and wherein each aryl and heteroaryl is unsubstituted or substituted with 1, 2, 3 or 4 substituents independently selected from R, provided that at least one of and only one of Rand Ris halogen;'}or a pharmaceutically acceptable salt thereof.10. The compound according to claims 1 ,{'sup': '1', 'claim-text': [{'sub': 2', 'p, '(1) —(CH)aryl-aryl, and'}, {'sub': 2', 'p, '(2) —(CH)aryl-heteroaryl,'}], 'wherein each Ris independently selected from{'sub': 2', '3', '2', '1-6', '1-6', '1-6', '1-6', '2, 'sup': 'a', 'wherein each CHis ...

NOVEL BENZIMIDAZOLE HEXAHYDROFURO[3,2-B]FURAN DERIVATIVES

The novel benzimidazole hexahydrofuro[3,2-B]furan derivatives of the present invention are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. 2. The compound according to wherein T is CR; U is CR; V is CR; and W is CR claim 1 , wherein Ris hydrogen or halogen; or a pharmaceutically acceptable salt thereof.3. The compound according to wherein T is CR; U is CR; V is CR; and W is CR claim 1 , wherein Ris hydrogen or halogen; and Ris halogen; or a pharmaceutically acceptable salt thereof.4. The compound according to claim 1 , wherein T is CR; U is CR; V is CR; and W is CR claim 1 , wherein Ris hydrogen or halogen; Ris halogen; and Ris hydrogen; or a pharmaceutically acceptable salt thereof.5. The compound according to claim 1 , wherein X is —O—; or a pharmaceutically acceptable salt thereof.9. The compound according to claim 1 , wherein Z is NR; or a pharmaceutically acceptable salt thereof.10. The compound according to claim 1 , each Rand Ris independently selected from:(1) halogen,{'sub': 2', 'p', '2-10, '(2) —(CH)aryl-Ccycloheteroalkyl,'}{'sub': 2', 'p, '(3) —(CH)aryl-aryl, and'}{'sub': 2', 'p, '(4) —(CH)aryl-heteroaryl,'}{'sub': 2', '3', '2', '1-6', '1-6', '1-6', '1-6', '2, 'sup': a', '1', '2, 'wherein each CHis unsubstituted or substituted with 1 or 2 substituents selected from: halogen, CF, —OH, —NH, —Calkyl, —OCalkyl, —NHCalkyl, and —N(Calkyl), and wherein each cycloheteroalkyl, aryl and heteroaryl is unsubstituted or substituted with 1, 2, 3 or 4 substituents independently selected from R, provided that at least one of and only one of Rand Ris halogen; or a pharmaceutically acceptable salt thereof.'}11. The compound according to claim 1 , wherein each Ris independently selected from:{'sub ...

NOVEL AZABENZIMIDAZOLE HEXAHYDROFURO[E,2-B]FURAN DERIVATIVES

Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. 3. The compound according to wherein T is N or N-oxide; U is —CR—; V is —CR—; and W is —CR—; or a pharmaceutically acceptable salt thereof.4. The compound according to wherein T is N; U is —CR—; V is —CR—; and W is —CR—; or a pharmaceutically acceptable salt thereof.6. The compound according to claim 1 , wherein X is —O—; or a pharmaceutically acceptable salt thereof.9. The compound according to claim 1 , wherein Z is NR; or a pharmaceutically acceptable salt thereof.13. The compound according to claim 1 , wherein Ris hydrogen or absent; Ris hydrogen; and Ris selected from: hydrogen claim 1 , —Calkyl and —(CH)OH; or a pharmaceutically acceptable salt thereof.14. The compound according to claim 1 , wherein Ris hydrogen or absent; Ris hydrogen; and Ris hydrogen; or a pharmaceutically acceptable salt thereof.15. The compound according to claim 1 , wherein Ris hydrogen or absent; Ris hydrogen; Ris hydrogen; and Ris halogen; or a pharmaceutically acceptable salt thereof.19. A composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.20. A composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a compound selected from simvastatin claim 1 , ezetimibe and sitagliptin; and a pharmaceutically acceptable carrier.21. (canceled)22. (canceled)23. (canceled)24. (canceled)25. A method of treating or preventing a disorder claim 1 , condition or disease that is responsive to the activation of AMP-activated protein kinase in a patient in need thereof comprising ...

PYRAZOLOPYRIMIDINE PDE9 INHIBITORS

The present invention is directed to pyrazolopyrimidine compounds which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. 3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein A is a cyclobutyl ring claim 1 , which is unsubstituted or substituted with one or more fluoro.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , Rand Rare independently selected from:(1) hydrogen,(2) halogen,(3) hydroxyl,{'sub': '1-6', '(4) Calkyl, which is unsubstituted or substituted with substituents selected from: hydroxy and fluoro,'}{'sub': '1-6', '(5) —O—Calkyl, which is unsubstituted or substituted with substituents selected from fluoro,'}{'sub': '3-6', '(6) Ccycloalkyl,'}{'sub': '2-4', '(7) Calkynyl, and'}(8) —CN.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CH.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen claim 1 , Ris hydrogen and Ris selected from:(1) hydrogen,(2) fluoro,(3) chloro,(4) bromo,(5) hydroxyl,{'sub': '3', '(6) —CH,'}{'sub': '3', '(7) —OCH,'}{'sub': '2', '(8) —CHF,'}{'sub': '3', '(9) —CF,'}{'sub': '2', '(10) —OCHF,'}{'sub': '3', '(11) —OCF,'}{'sub': '3', '(12) —CH2CH,'}{'sub': 3', '2, '(13) —CH(CH),'}{'sub': '3', '(14) —C(CH3),'}(15) —C═CH, and(16) cyclopropyl.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen and Ris hydrogen claim 1 , and Ris selected from:(1) hydrogen,(2) fluoro,{'sub': '3', ...

2'-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

The present invention relates to 2'-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one 2'-Azido Substituted Nucleoside Derivative, and methods of using the 2'-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

2'-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

The present invention relates to 2'-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one 2'-Substituted Nucleoside Derivative, and methods of using the 2'-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

Sulfur compounds as inhibitors of hepatitis c virus ns3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Sulfur compounds as inhiibitors of hepatitis c virus ns3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

5'-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

The present invention relates to 5'-Substituted Nucleoside Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein B, X, Y, Z, R 1 , R 2 , R 3 and R 3' are as defined herein. The present invention also relates to compositions comprising at least one 5'-Substituted Nucleoside Derivative, and methods of using the 5'-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

Novel ketoamides with cyclic p4's as inhibitors of ns3 serine protease of hepatitis c virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Proline compounds as NS3-serine protease inhibitors for use in treatment of hepatitis C virus infection

Macrocyclic NS3-Serine protease inhibitors of hepatitis C virus comprising alkyl and aryl alanine P2 moieties

Disclosed are macrocyclic compounds of formula I, wherein the ring atoms are optionally substituted with hetero- atoms such as O, N or SO2. The compounds are used in the manufacture of medicaments for the treatment of disorders associated with HCV NS3 protease.

Sulfur compounds as inhibitors of hepatitis c virus ns3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

2'-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

DERIVATIVES OF NUCLEOSIDS 2'-SUBSTITUTES AND METHODS OF USE OF THE SAME FOR THE TREATMENT OF VIRAL DISEASES

La presente invención se refiere a derivados de nucleósidos 2'-sustituidos de la fórmula (I):

SULFURED COMPOUNDS AS INHIBITORS OF THE SERINE PROTEASE NS3 OF THE HEPATITIS C VIRUS

SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R1 ES OR8, NR9R10, CHR9R10; R8, R9 Y R10 PUEDEN SER IGUALES O DIFERENTES, SELECCIONANDOSE DE H, ALQUILO, ALQUENILO, ALQUINILO, ENTRE OTROS; A Y M SON CADA UNO R, OR, NHR, HALO, ENTRE OTROS; E ES CH, CR; L ES CH, CR, CH2CR, CRCH2; R, R2 Y R3 SON CADA UNO H, ALQUILO, HETEROALQUILO, ALQUENILO, ENTRE OTROS; Y ES 1, 2, ENTRE OTROS; G ES NH, O; R15, R17, R18 SON CADA UNO H, ALQUILO, ALQUENILO, ALQUINILO, ARILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS A, B, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA SERINA PROTEASA NS3/NS4 DEL VIRUS DE LA HEPATITIS C (VHC) UTILES EN EL TRATAMIENTO DE TRASTORNOS ASOCIADOS CON VHC REFERS TO A COMPOUND OF FORMULA I WHERE R1 IS OR8, NR9R10, CHR9R10; R8, R9 AND R10 MAY BE THE SAME OR DIFFERENT, SELECTED FROM H, ALKYL, ALKENYL, ALKINYL, AMONG OTHERS; A AND M ARE EACH ONE R, OR, NHR, HALO, AMONG OTHERS; E IS CH, CR; L IS CH, CR, CH2CR, CRCH2; R, R2 AND R3 ARE EACH H, ALKYL, HETEROALKYL, ALKENYL, AMONG OTHERS; AND IT IS 1, 2, AMONG OTHERS; G IS NH, O; R15, R17, R18 ARE EACH H, ALKYL, ALKENYL, ALKINYL, ARYL, AMONG OTHERS. THE PREFERRED COMPOUNDS A, B, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE INHIBITORS OF THE SERINE PROTEASE NS3 / NS4 OF THE HEPATITIS C VIRUS (HCV) USEFUL IN THE TREATMENT OF HCV-ASSOCIATED DISORDERS

Macrocyclic ns3-serine protease inhibitors of hepatitis c virus comprising n-cyclic p2 moieties

The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds . In another embodiment, the invention discloses pharmaceutical compositions comprising such macrocycles as well as methods of using them to treat disorders associated with the HCV protease.

Inhibitors of hepatitis c virus ns3/ns4a serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Macrocyclic ns-3 serine protease inhibitors of hepatitis c virus compri sing alkyl and aryl alanine p2 moieties

The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such macrocycles as well as methods of using them to treat disorders associated with the HCV protease.

Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising alkyl and aryl alanine P2 moieties

Chromane, isochromane and dihydroisobenzofuran derivatives as mGluR2-negative allosteric modulators, compositions, and their use

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from (II), (III), (IV), and (V), and ring B, n, R

CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from (II), (III), (IV), and (V), and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.

Proline compounds as ns3-serine protease inhibitors for use in treatment of hepatites c virus infection

The present invention discloses novel compounds of Formula I which have HCV protease inhibitory activity as well as methods for preparing such compounds . In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorder s associated with the HCV protease.

Proline compounds as ns3-serine protease inhibitors for use in treatment of hepatites c virus infection

The present invention discloses novel compounds of Formula I which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Pyrazolopyrimidine pde9 inhibitors

The present invention is directed to pyrazolopyrimidme compounds which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9) The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction

3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis c virus ns3 serine protease

The present invention discloses novel compounds according to formula (I) which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease. Wherein: R1 is H, OR8, NR9R10, wherein R8, R9 and R10 can be the same or different, each being independently selected from the group consisting of H, alkyl-, alkenyl-, alkynyl-, aryl-, heteroalkyl-, heteroaryl-, cycloalkyl-, heterocyclyl-, arylalkyl-, and heteroarylalkyl, or alternately R9 and R10 in NR9R10 are connected to each other such that NR9R10 forms a four to eight-membered heterocyclyl, and likewise independently alternately R9 and R10 in CHR9R10 are connected to each other such that CHR9R10 forms a four to eight-membered cycloalkyl; Y represents a group G-R wherein G is NH or O.

Novel ketoamides with cyclic P4's as inhibitors of NS3 serine protease of hepatitis C virus

DERIVATIVES OF NUCLEOSIDES 2'- SUBSTITUTED AND METHODS OF USE OF THE SAME FOR THE TREATMENT OF VIRAL DISEASES

SE REFIERE A COMPUESTOS DERIVADOS DE NUCLEOSIDOS 2'-SUSTITUIDOS DE FORMULA (I) DONDE X ES O, S O CH2; A ES ALQUENILO(C2-C6), ALQUINILO(C2-C6), -S-(ALQUILO C1-C6), ENTRE OTROS; B ES UNA BASE DE PURINA O PIRIMIDINA NATURAL O NO NATURAL, ENTRE OTROS; R1 ES H, OHP(O)OH-O-P(O)OH, ENTRE OTROS; R2 ES H; O R1 Y R2 SE UNEN PARA FORMAR EL COMPUESTO (a) O (b), EN DONDE R18 ES H, ALQUILO(C1-C6), CICLOALQUILO(C3-C7), ENTRE OTROS; R29 ES H, ALQUILO(C1-C6), HALOALQUILO(C1-C6), ENTRE OTROS; R3 ES ALQUILO(C1-C6), HALOALQUILO(C1-C6), ALQUENILO(C2-C6), ENTRE OTROS. SON COMPUESTOS PREFERIDOS LOS DE FORMULA (i), (ii), ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD DE NS5A DEL VIRUS DE LA HEPATITIS C (VHC) SIENDO UTILES EN EL TRATAMIENTO DE INFECCION POR VHC REFERS TO COMPOUNDS DERIVED FROM 2'-SUBSTITUTED NUCLEOSIDES FROM FORMULA (I) WHERE X IS O, S OR CH2; A is ALKENYL (C2-C6), ALKYNYL (C2-C6), -S- (C1-C6 ALKYL), AMONG OTHERS; B IS A NATURAL OR NON-NATURAL PURINE OR PYRIMIDINE BASE, AMONG OTHERS; R1 IS H, OHP (O) OH-O-P (O) OH, AMONG OTHERS; R2 IS H; OR R1 AND R2 JOIN TO FORM COMPOUND (a) OR (b), WHERE R18 IS H, ALKYL (C1-C6), CYCLOALKYL (C3-C7), AMONG OTHERS; R29 IS H, (C1-C6) ALKYL, (C1-C6) HALOALKYL, AMONG OTHERS; R3 IS ALKYL (C1-C6), HALOALKYL (C1-C6), ALKENYL (C2-C6), AMONG OTHERS. THE PREFERRED COMPOUNDS ARE THOSE OF FORMULA (i), (ii), AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE INHIBITORS OF THE ACTIVITY OF NS5A OF THE HEPATITIS C VIRUS (HCV) AND ARE USEFUL IN THE TREATMENT OF HCV INFECTION

Diaryl peptides as ns3-serine protease inhibitors of hepatits c virus

Novel peptides as ns3-serine protease inhibitors of hepatitis c virus

The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Sulfur compounds as inhibitors of Hepatitis C Virus NS3 serine protease

Sulfur compounds as inhibitors of hepatitis c virus ns3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Chromane, isochromane and dihydroisobenzofuran derivatives as mglur2-negative allosteric modulators, compositions, and their use

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from (II), (III), (IV), and (V), and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild congnitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.

Enantio- and stereo-specific syntheses of -amino- - hydroxy amides

Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.

Diaryl peptides as ns3-serine protease inhibitors of hepatits c virus

The present invention is directed to certain diaryl amide compounds as NS3-Serine protease inhibitors of hepatitis C virus. A particularly preferred compound is of the formula (I).

Substituted pyridine and pyrimidine derivatives and their use in treating viral infections

The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and pro-drugs of said compounds, wherein wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.

Novel peptides as ns3-serine protease inhibitors of hepatitis c virus

Peptides as NS3-serine protease inhibitors of hepatitis C virus

3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis c virus ns3 serine protease

The present invention discloses novel compounds according to formula (I) which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease. Wherein: R1 is H, OR8, NR9R10, wherein R8, R9 and R10 can be the same or different, each being independently selected from the group consisting of H, alkyl-, alkenyl-, alkynyl-, aryl-, heteroalkyl-, heteroaryl-, cycloalkyl-, heterocyclyl-, arylalkyl-, and heteroarylalkyl, or alternately R9 and R10 in NR9R10 are connected to each other such that NR9R10 forms a four to eight-membered heterocyclyl, and likewise independently alternately R9 and R10 in CHR9R10 are connected to each other such that CHR9R10 forms a four to eight-membered cycloalkyl; Y represents a group G-R wherein G is NH or O.

Macrocyclic NS3 Serine Protease Inhibitors for Hepatitis C Virus, Including alkyl and arylalanine P2 residues

PROLIN 3.4 COMPOUNDS (CYCLOPENTIL) FUSED AS INHIBITORS OF THE SERINE PROTEASE NS3 OF THE HEPATITIS VIRUS C.

Un compuesto, o los enantiómeros, estereoisómeros, rotámeros, tautómeros, diastereómeros o racematos de dicho compuesto, o una sal, solvato o éster farmacéuticamente aceptable de dicho compuesto, teniendo dicho compuesto la estructura general mostrada en la Fórmula I: **(Ver fórmula)** donde: R1 es H, OR8 , NR9 R10 , o CHR9 R 10 , donde R8 , R9 y R10 pueden ser iguales o diferentes, seleccionándose cada uno independientemente del grupo que consiste en H, alquilo-, alquenilo-, alquinilo-, arilo-, heteroalquilo-, heteroarilo-, cicloalquilo-, heterociclilo-, arilalquilo-, y heteroarilalquilo, o alternativamente R9 y R10 en NR9 R10 se conectan entre sí de manera que NR9 R10 forma a un heterociclilo de cuatro a ocho miembros, y asimismo independientemente alternativamente R9 y R10 en CHR9 R10 se conectan entre sí de manera que CHR9 R10 forma un cicloalquilo de cuatro a ocho miembros; R2 y R3 pueden ser iguales o diferentes, seleccionándose cada uno independientemente del grupo que consiste en H, alquilo, heteroalquilo, alquenilo, heteroalquenilo, alquinilo, heteroalquinilo, cicloalquilo, heterociclilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo; y se selecciona entre los siguientes radicales: **(Ver fórmula)** donde G es NH u O; y R15 , R16 , R17 , R18 , R19 , R20 , R21 , R22 , R23 , R24 y R25 pueden ser iguales o diferentes, seleccionándose cada uno independientemente del grupo que consiste en H, alquilo, heteroalquilo, alquenilo, heteroalquenilo, alquinilo, heteroalquinilo, cicloalquilo, heterociclilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo, o alternativamente (i) R 17 y R 18 independientemente se conectan entre sí para formar un cicloalquilo o heterociclilo de tres a ocho miembros; (ii) asimismo R15 y R19 independientemente se conectan entre sí para formar a un heterociclilo de cuatro a ocho miembros; (iii) asimismo R15 y R16 independientemente se conectan entre sí para formar a un heterociclilo de cuatro a ocho miembros; (iv) asimismo R15 y ...

Peptides as ns3-serine protease inhibitors of hepatitis c virus

Peptides as NS3-serine protease inhibitors of hepatitis C virus

Peptides of formula (I) as NS3-serine protease inhibitors of hepatitis C virus that have HCV protease inhibitory activity and methods for preparing these peptide compounds are disclosed, wherein the variables are as defined in the specification. Pharmaceutical compositions comprising these compounds that are useful for treating disorders associated with the HCV protease are also disclosed.

Novel benzimidazole hexahydrofuro[3,2-b]furan derivatives

The novel benzimidazole hexahydrofuro[3,2-B]furan derivatives of the present invention are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

Enantio- and stereo-specific syntheses of beta-amino-alpha- hydroxy amides

Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.

Novel peptides as ns3-serine protease inhibitors of hepatitis c virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

5-oxopyrrolidine-3-carboxamides as nav1.8 inhibitors

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.

5'-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

Ketoamides with cyclic p4's as inhibitors of ns3 serine protease of hepatitis c virus

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from (II), (III), (IV), and (V), and ring B, n, R 1 , R 2 , R 2A , R 3 , and R 3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild congnitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.

2'-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

The present invention relates to 2'-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one 2'-Substituted Nucleoside Derivative, and methods of using the 2'-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

Macrocyclic ns3-serine protease inhibitors of hepatitis c virus comprising n-cyclic p2 moietes

Compounds as inhibitors of hepatitis c virus ns3 serine protease

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Peptide compounds, pharmaceutical compositions comprising them and their use

Described are peptide compounds of the general formula (I) wherein the meanings of substituents are mentioned in the claims, pharmaceutical compositions comprising such compounds as well as their use in treating disorders associated with HCV protease. The compounds have the HCV protease inhibitory activity.

Novel peptides as ns3-serine protease inhibitors of hepatitis c virus

Substituted prolines as inhibitors of hepatitis c virus ns3 serine protease

The present invention discloses compounds of formula (I) which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Inhibitors of hepatitis c virus ns3 protease

The present invention discloses novel compounds of formula (I) which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.