EP0055583A1
Expired / Lapsed
EP
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Antihypertensives
Assignee: Pfizer Ltd
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Filing: 1981-12-22
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Granted: —
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Expires: 2001-12-22
Abstract
Abstract Antihypertensives of the formula:- or a pharmaceutically-acceptable acid-addition salt thereof, wherein "Het" is a pyrimidinyl, pyrazinyl, pyridazinyl or triazinyl group linked to the piperazine ring by one of its carbon atoms, said group being optionally substituted by one or two substituents selected from C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, aryl, aryloxy, C 1 -C 4 alkyl substituted by aryl, C 1 -C 4 alkoxy substituted by aryl, C 1 -C 4 alkylthio, halo and -NR'R where R 1 is hydrogen or C 1 -C 4 alkyl and R 2 is hydrogen, C 1 -C 4 alkyl, C 3 -C 7 cycloalkyl, aryl or C 1 -C 4 alkyl substituted by aryl, or R 1 and R 2 taken together with the nitrogen atom to which they are attached represent a 1-pyrrolidinyl group or a 6-membered saturated heterocyclic group optionally containing a further heteroatom selected from 0, S and N, or said group "Het" is optionally substituted by a single 6,7-dimethoxy-1,2,3,4-tetrahydro- isoquinol-2-yl group.
Inventors
- 👤 Simon Fraser Campbell
- 👤 Rhona Margret Plews
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-03 10:29
CPC Classifications
C; C07; C07D; C07D403/00; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/32; C07D239/34; A; A61; A61P; A61P9/00; A61P9/12; C07D237/00; C07D237/02; C07D237/06; C07D237/10; C07D237/22; C07D239/42; C07D239/46; C07D239/47; C07D239/48; C07D239/70; C07D239/72; C07D239/95; C07D251/00; C07D251/02; C07D251/12; C07D251/26; C07D251/40; C07D251/42; C07D251/44; C07D251/46
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
169 words
A compound of the fprmula:- or a pharmaceutically-acceptable acid-addition salt thereof, wherein "Het" is a pyrimidinyl, pyrazinyl, pyridazinyl or triazinyl group linked to the piperazine ring by one of its carbon atoms, said group being optionally substituted by one or two substituents selected from C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, aryl, aryloxy, C 1 -C 4 alkyl substituted by aryl, C 1 -C 4 alkoxy substituted by aryl, C 1 -C 4 alkylthio, halo and -NR 1 R 2 where R is hydrogen or C 1 -C 4 alkyl and R 2 is hydrogen, C 1 -C 4 alkyl, C 3 -C 7 cycloalkyl, aryl, or C 1 -C 4 alkyl substituted by aryl, or R 1 and R 2 taken together with the nitrogen atom to which they are attached represent a 1-pyrrolidinyl group or a 6-membered saturated heterocyclic group optionally containing a further heteroatom selected from 0, S and N, or said group "Het" is optionally substituted by a single 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl group.
Claim 2
Dependent Claim
169 words
A compound of the fprmula:- or a pharmaceutically-acceptable acid-addition salt thereof, wherein "Het" is a pyrimidinyl, pyrazinyl, pyridazinyl or triazinyl group linked to the piperazine ring by one of its carbon atoms, said group being optionally substituted by one or two substituents selected from C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, aryl, aryloxy, C 1 -C 4 alkyl substituted by aryl, C 1 -C 4 alkoxy substituted by aryl, C 1 -C 4 alkylthio, halo and -NR 1 R 2 where R is hydrogen or C 1 -C 4 alkyl and R 2 is hydrogen, C 1 -C 4 alkyl, C 3 -C 7 cycloalkyl, aryl, or C 1 -C 4 alkyl substituted by aryl, or R 1 and R 2 taken together with the nitrogen atom to which they are attached represent a 1-pyrrolidinyl group or a 6-membered saturated heterocyclic group optionally containing a further heteroatom selected from 0, S and N, or said group "Het" is optionally substituted by a single 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl group.
Claim 3
Dependent Claim
30 words
A compound as claimed in claim 1 wherein "Het" is a pyrimidin-2-yl, pyrimidin-4-yl, 1,3,5-triazin-2-yl, pyridazin-3-yl or pyrazin-2-yl group optionally substituted by one or two substituents as defined in claim 1.
Claim 4
Dependent Claim
39 words
A compound as claimed in claim 1 or 2 wherein said aryl and aryloxy groups are, respectively, phenyl or phenoxy, both optionally substituted by 1 or 2 substituents selected from C 1 -C 4 alkyl, C1-C4 alkoxy, and halo.
Claim 5
Dependent Claim
111 words
A compound as claimed in any one of claims I to 3 wherein "Het" is unsubstituted or substituted by 1 or 2 substituents selected from C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, phenyl, phenoxy, C 1 -C 4 alkylthio, halo and -NR 1 R 2 where R 1 is hydrogen or C 1 -C 4 alkyl and R 2 is hydrogen, C 1 -C 4 alkyl, phenyl or C 3 -C 7 cycloalkyl, or R 1 and R 2 taken together with the nitrogen atom to which they are attached represent a morpholino group, or where said group "Het" is optionally substituted by a single 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl group.
Claim 6
Dependent Claim
171 words
A compound as claimed in any one of the precediing claims wherein "Het" is selected from:- (a) 2- or 4-pyrimidinyl unsubstituted or substituted by 1 or 2 substituents selected from C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, phenyl, phenoxy, C 1 -C 4 alkylthio, halo, or -NR 1 R 2 where R 1 is hydrogen or C 1 -C 4 alkyl, and R 2 is hydrogen, C 1 -C 4 alkyl, C 3 -C 7 cycloalkyl or phenyl, or R 1 and R 2 taken together with the nitrogen atom to which they are attached represent a morpholino group; or 2- or 4-pyrimidiinyl substituted by a single 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl group; (b) l,3,5-triazin-2-yl substituted by 2 substituents se3lected from C 1 -C 4 alkoxy, phenoxy and -NHR 2 where R 2 is hydrogen or C 1 -C 4 alkyl; (c) 3-pyridazinyl unsubstituted or substituted by I substituent selected from C 1 -C 4 alkoxy, hydroxy, phenyl, phenoxy, halo and -N(C 1 -C 4 alkyl) 2 ; and (d) 2-pyrazinyl.
Claim 7
Dependent Claim
8 words
A compound as claim 1 where "Het" is
Claim 8
Dependent Claim
71 words
A process for preparing a compound of the formula (I) or salt thereof as claimed in claim 1, which comprises reacting a compound of the formula:- wherein Q is a facile leaving group, with a piperazine of the formula:- wherein "Het" is as defined in claim 1, followed by, optionally, conversion of the product of the formula (I) into a pharmaceutically acceptable acid addition salt by reaction with a non-toxic acid.
Claim 9
Dependent Claim
71 words
A process for preparing a compound of the formula (I) or salt thereof as claimed in claim 1, which comprises reacting a compound of the formula:- with a compound of the formula:- wherein Q is a facile leaving group and "Het" is as defined in claim 1, followed by, optionally, conversion of a product of the formula (I) into a pharmaceutically acceptable acid addition salt by reaction with a non-toxic acid.
Claim 10
Dependent Claim
29 words
A process as claimed in claim 7 or 8, wherein the reaction of the quinazoline and the heterocycle is carried out in the presence of a tertiary amine base.
Claim 11
Dependent Claim
67 words
A process for preparing a compound of the formula (I) as claimed in claim 1 : in which "Het" is substituted by NR 1 R 2 wherein R 1 and R 2 are as defined in claim 1, which comprises reacting the corresponding compound of the formula (I) in which "Het" is substituted by halo with an amine of the formula R I R 2 NH .
Claim 12
Dependent Claim
31 words
A pharmaceutical composition comprising a compound of the formula (I) as claimed in claim 1 or a pharmaceutically acceptable acid addition salt thereof, together with a pharmaceutically acceptable diluent or carrier.
References Cited (Backward Citations)
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