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1. (WO1997016430) HEXAHYDRO-5-IMINO-1,4-HETEROAZEPINE DERIVATIVES AS INHIBITORS OF NITRIC OXIDE SYNTHASES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/016430 International Application No.: PCT/US1996/017447
Publication Date: 09.05.1997 International Filing Date: 28.10.1996
Chapter 2 Demand Filed: 19.05.1997
IPC:
C07D 243/08 (2006.01) ,C07D 267/16 (2006.01) ,C07D 281/06 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
243
Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
06
having the nitrogen atoms in positions 1 and 4
08
not condensed with other rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
267
Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
02
Seven-membered rings
08
having the hetero atoms in positions 1 and 4
12
condensed with carbocyclic rings or ring systems
16
condensed with two six-membered rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
281
Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
02
Seven-membered rings
04
having the hetero atoms in positions 1 and 4
06
not condensed with other rings
Applicants:
MERCK & CO., INC. [US/US]; 126 East Lincoln Avenue Rahway, NJ 07065, US (AllExceptUS)
CALDWELL, Charles, G. [US/US]; US (UsOnly)
HAGMANN, William, K. [US/US]; US (UsOnly)
MacCOSS, Malcolm [GB/US]; US (UsOnly)
SHAH, Shrenik, K. [IN/US]; US (UsOnly)
SHANKARAN, Kothandaraman [IN/US]; US (UsOnly)
FURMAN, Karla, L. [US/US]; US (UsOnly)
Inventors:
CALDWELL, Charles, G.; US
HAGMANN, William, K.; US
MacCOSS, Malcolm; US
SHAH, Shrenik, K.; US
SHANKARAN, Kothandaraman; US
FURMAN, Karla, L.; US
Common
Representative:
MERCK & CO., INC.; 126 East Lincoln Avenue Rahway, NJ 07065, US
Priority Data:
60/007,17201.11.1995US
60/009,01221.12.1995US
9605162.812.03.1996GB
9605700.519.03.1996GB
Title (EN) HEXAHYDRO-5-IMINO-1,4-HETEROAZEPINE DERIVATIVES AS INHIBITORS OF NITRIC OXIDE SYNTHASES
(FR) DERIVES DE L'HEXAHYDRO-5-IMINO-1,4-HETEROAZEPINE INHIBITEURS DES SYNTHASES DE L'OXYDE NITRIQUE
Abstract:
(EN) Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. These diseases and disorders include hypotension, septic shock, toxic shock syndrome, hemodialysis, IL-2 therapy such as in cancer patients, cachexia, immunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn, eczema or psoriasis and respiratory conditions such as bronchitis, asthma, oxidant-induced lung injury and acute respiratory distress (ARDS), glomerulonephritis, restenosis, inflammatory sequelae of viral infections, myocarditis, heart failure, atherosclerosis, osteoarthritis, rheumatoid arthritis, septic arthritis, chronic or inflammatory bowel disease, ulcerative colitis, Crohn's disease, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension, retinitis and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis.
(FR) L'invention porte sur des composés de formule (I) et leurs sels pharmacocompatibles s'avérant utiles pour le traitement de maladies et affections dues à la synthase de l'oxyde nitrique et notamment de troubles neurodégénératifs, de troubles de la motilité gastro-intestinale et d'inflammations. Ces maladies et affections englobent l'hypotension, le choc septique, le syndrome de choc toxique, l'hémodialyse, le traitement de cancéreux par l'IL-2, la cachexie, l'immuno-suppression accompagnant les thérapies de transplantation, les troubles à caractère auto-immunitaire ou inflammatoire tels que les coups de soleil, l'eczéma ou le psoriasis et les troubles respiratoires tels que la bronchite, l'asthme, les lésions pulmonaires dues à des oxydants et l'emphysème pulmonaire, la glomérulonéphrite, les resténoses, les séquelles inflammatoires d'infections virales, les myocardites, l'insuffisance cardiaque, l'athérosclérose, l'arthrose, la polyarthrite rhumatoïde, l'arthrite aiguë suppurée, les troubles intestinaux chroniques ou inflammatoires, la rectocolite hémorragique, la maladie de Crohn, le lupus érythémateux systémique, des troubles oculaires tels que le glaucome, la rétinite ou l'uvéite, les diabètes de type 1, le diabète sucré insulinodépendant, et la fibrose kystique du pancréas.
Designated States: AL, AM, AU, AZ, BA, BB, BG, BR, BY, CA, CN, CU, CZ, EE, GE, HU, IL, IS, JP, KG, KR, KZ, LC, LK, LR, LT, LV, MD, MG, MK, MN, MX, NO, NZ, PL, RO, RU, SG, SI, SK, TJ, TM, TR, TT, UA, US, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0861238JPH11501327CA2234641AU1996075287