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1. (EP0505377) MUSCARINIC RECEPTOR ANTAGONISTS

Office : European Patent Office
Application Number: 90917074 Application Date: 28.11.1990
Publication Number: 0505377 Publication Date: 30.09.1992
Publication Kind : B1
Prior PCT appl.: Application Number:EP1990002042 ; Publication Number: Click to see the data
IPC:
C 07D
C 07D
A61K 31/445
C 07D
A61K 31/4427
A 61K
A61K 31/443
A61K 31/4433
A61P 1/12
C07D 401/04
C07D 405/14
C07D 409/14
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
211
Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
80
having two double bonds between ring members or between ring members and non-ring members
84
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
86
Oxygen atoms
88
attached in positions 2 and 6, e.g. glutarimide
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
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
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
443
containing a five-membered ring with oxygen as a ring hetero atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
4433
containing a six-membered ring with oxygen as a ring hetero atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
12
Antidiarrhoeals
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
14
containing three or more hetero rings
CPC:
C07D 401/04
C07D 405/14
Applicants: PFIZER LTD
PFIZER
Inventors: MACKENZIE ALEXANDER RODERICK
CROSS PETER EDWARD PFIZER CENT
Priority Data: 9002042 28.11.1990 EP
8928041 12.12.1989 GB
Title: (DE) MUSCARIN-REZEPTOR-ANTAGONISTEN
(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.
Also published as:
FI922344ES2082013US5281601JPH05501555CA2067816DE000069024663
PT96143DK0505377WO/1991/009015