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1. (WO1991009015) MUSCARINIC RECEPTOR ANTAGONISTS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/009015 International Application No.: PCT/EP1990/002042
Publication Date: 27.06.1991 International Filing Date: 28.11.1990
Chapter 2 Demand Filed: 02.07.1991
IPC:
C07D 401/04 (2006.01) ,C07D 405/14 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14
containing three or more hetero rings
Applicants:
PFIZER LIMITED [GB/GB]; Ramsgate Road Sandwich Kent CT13 9NJ, GB (GB)
PFIZER INC. [US/US]; 235 East 42nd Street New York, NY 10017, US (AT, BE, CA, CH, DE, DK, ES, FI, FR, GB, GR, IT, JP, LU, NL, SE)
MACKENZIE, Alexander, Roderick [GB/GB]; GB (UsOnly)
CROSS, Peter, Edward [GB/GB]; GB (UsOnly)
Inventors:
MACKENZIE, Alexander, Roderick; GB
CROSS, Peter, Edward; GB
Agent:
WOOD, David, John ; Pfizer Limited Patents Department Ramsgate Road Sandwich Kent CT13 9NJ, GB
Priority Data:
8928041.612.12.1989GB
Title (EN) MUSCARINIC RECEPTOR ANTAGONISTS
(FR) ANTAGONISTES DE RECEPTEURS MUSCARINIQUES
Abstract:
(EN) A muscarinic receptor antagonist of formula (I) or a pharmaceutically acceptable salt thereof, wherein Y is a direct link, -CH2-, -(CH2)2-, -CH2O- or -CH2S-; and R1 is a group of formulae (a), (b), (c) or Het where R2 and R3 are each independently H, C1-C4 alkyl, C1-C4 alkoxy, -(CH2)nOH, halo, trifluoromethyl, cyano, -(CH2)nNR4R5, -CO(C1-C4 alkyl), -OCO(C1-C4 alkyl), -CH(OH)(C1-C4 alkyl), -C(OH)(C1-C4 alkyl)2, -SO2NH2, -(CH2)nCONR4R5 or -(CH2)nCOO(C1-C4 alkyl); R4 and R5 are each independently H or C1-C4 alkyl; n is 0, 1 or 2; X and X1 are each independently O or CH2; m is 1, 2 or 3; and ''Het'' is pyridyl, pyrazinyl or thienyl. The compounds are particularly useful in the treatment of irritable bowel syndrome.
(FR) Antagoniste de récepteur muscarinique répondant à la formule (I), ou son sel pharmaceutiquement acceptable, dans laquelle Y est une liaison directe, -CH2-, -(CH2)2-, -CH2O- ou -CH2S-; et R1 est un groupe qui répond à les formules (a), (b), (c) ou Het, dans laquelle R2 et R3 sont, indépendamment l'un de l'autre, H, alkyle en C1-C4, alkoxy en C1-C4, -(CH2)nOH, halo, trifluorométhyle, cyano, -(CH2)nNR4R5, -CO(C1-C4 alkyl), -OCO(C1-C4 alkyl), -CH(OH)(C1-C4 alkyl), -C(OH)(C1-C4 alkyl), -C(OH)(C1-C4 alkyl)2, -SO2NH2, -(CH2)nCONR4R5 ou -(CH2)nCOO(C1-C4 alkyl); R4 et R5 sont, indépendamment l'un de l'autre, H ou alkyle en C1-C4; n est 0, 1 ou 2; X et X1 sont, indépendamment l'un de l'autre, O ou CH2; m est 1, 2 ou 3; ''Het'' est pyridyle, pyrazinyle ou thiényle. Ces composés sont utiles notamment au traitement du syndrome de l'intestin irritable.
Designated States: CA, FI, JP, US
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
FI922344EP0505377ES2082013US5281601JPH05501555CA2067816
DE000069024663PT96143DK0505377