Patent US2378906A successfully refreshed from Google Patents.
Patent EP0089167B1 successfully refreshed from Google Patents.
EP0089167B1
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EP
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Dihydropyridine anti-ischaemic and antihypertensive agents, processes for their production, and pharmaceutical compositions containing them
Assignee: Pfizer Ltd
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Filing: 1983-03-08
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Granted: 1986-10-15
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Expires: 2003-03-08
Abstract
Abstract Dihydropyridines of the formula:- <CHEM> and their pharmaceutically acceptable acid addition salts wherein Y is -(CH2)2-, -(CH2)3-, -CH2CH(CH3)- or -CH2C(CH3)2-; R is aryl or heteroaryl; R<1> and R<2> are each independently C1-C4 alkyl or 2-methoxyethyl; and R<3> is hydrogen, C1-C4 alkyl, 2-(C1-C4 alkoxyl) ethyl, cyclopropylmethyl, benzyl, or -(CH2)mCOR<4> where m is 1, 2 or 3 and R<4> is hydroxy, C1-C4 alkoxy or - NR<R>5<6> where R<5> and R<6> are each independently hydrogen or C1-C4 alkyl, pharmaceutical compositions containing them, and processes for their production. <??>The compounds are particularly useful in the treatment or prevention of a variety of cardiac conditions, e.g, angina pectoris.
Inventors
- 👤 Simon Fraser Campbell
- 👤 Peter Edward Cross
- 👤 John Kendrick Stubbs
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-24 15:03
CPC Classifications
C; C07; C07D; C07D211/00; C07D211/04; C07D211/80; C07D211/84; C07D211/86; C07D209/00; C07D209/02; C07D209/44; C07D209/48; A; A61; A61P; A61P9/00; A61P9/06; A61P9/10; A61P9/12; C07C; C07C247/00; C07D211/90; C07D401/00; C07D401/02; C07D401/12; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
37 words
A dihydropyridine of the formula:- or a pharmaceutically acceptable acid addition salt thereof wherein Y is ―(CH 2 ) 2 ―, ―(CH 2 )3―, -CH 2 CH(CH 3 )- or ―CH 2 C(CH 3 ) 2 ―,
Claim 2
Dependent Claim
37 words
A dihydropyridine of the formula:- or a pharmaceutically acceptable acid addition salt thereof wherein Y is ―(CH 2 ) 2 ―, ―(CH 2 )3―, -CH 2 CH(CH 3 )- or ―CH 2 C(CH 3 ) 2 ―,
Claim 3
Dependent Claim
145 words
R is selected from (a) a phenyl group optionally substituted by one or two substituents each selected from nitro, halo, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, trifluoromethyl, and cyano, (b) a 1- or 2-naphthyl group, and (c) benzofuranyl; benzothienyl; pyridyl optionally monosubstituted by methyl or cyano; quinolyl; benzoxazolyl; benzothiazolyl; furyl; pyrimidinyl; thiazolyl; 2,1,3-benzoxadiazol-4-yl; 2,1,3-benzo- thiadiazol-4-yl; or thienyl optionally monosubstituted by halo or C 1 ―C 4 alkyl; R 1 and R 2 are each independently C 1 -C 4 alkyl or 2-methoxyethyl; and R 3 is hydrogen, C 1 ―C 4 alkyl, 2-(C1―C4 alkoxy)ethyl, cyclopropylmethyl, benzyl, or―(CH 2 ) m COR 4 where m is 1, 2 or 3 and R 4 is hydroxy, C 1 -C 4 alkoxy or ―NR 5 R 6 where R 5 and R 6 are each independently hydrogen or C 1 -C 4 alkyl.
Claim 4
Dependent Claim
145 words
R is selected from (a) a phenyl group optionally substituted by one or two substituents each selected from nitro, halo, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, trifluoromethyl, and cyano, (b) a 1- or 2-naphthyl group, and (c) benzofuranyl; benzothienyl; pyridyl optionally monosubstituted by methyl or cyano; quinolyl; benzoxazolyl; benzothiazolyl; furyl; pyrimidinyl; thiazolyl; 2,1,3-benzoxadiazol-4-yl; 2,1,3-benzo- thiadiazol-4-yl; or thienyl optionally monosubstituted by halo or C 1 ―C 4 alkyl; R 1 and R 2 are each independently C 1 -C 4 alkyl or 2-methoxyethyl; and R 3 is hydrogen, C 1 ―C 4 alkyl, 2-(C1―C4 alkoxy)ethyl, cyclopropylmethyl, benzyl, or―(CH 2 ) m COR 4 where m is 1, 2 or 3 and R 4 is hydroxy, C 1 -C 4 alkoxy or ―NR 5 R 6 where R 5 and R 6 are each independently hydrogen or C 1 -C 4 alkyl.
Claim 5
Dependent Claim
19 words
A compound as claimed in claim 1, wherein R is phenyl, 2-chlorophenyl, 2-fluorophenyl, 2-methoxyphenyl, 3-chlorophenyl, 2-chloro-3-hydroxyphenyl, 2-chloro-6-fluorophenyl, or 2,3-dichlorophenyl.
Claim 6
Dependent Claim
21 words
A compound as claimed in either of the preceding claims, wherein Y is―(CH 2 ) 2 or―CH 2 CH(CH 3 )―.
Claim 7
Dependent Claim
46 words
A compound as claimed in any one of the preceding claims, wherein R 3 is H, CH 3 , benzyl, 2-methoxyethyl, -CH 2 COOCH 3 , -CH 2 COOC 2 H s , -CH 2 CONH 2 , -CH 2 CONHCH 3 or -CH 2 COOH.
Claim 8
Dependent Claim
16 words
A compound as claimed in claim 4, wherein R 3 is H or CH 3 .
Claim 9
Dependent Claim
39 words
A compound as claimed in claim 1, wherein R is 2-chlorophenyl, R 1 is CH 3 , R is C 2 H 5 , Y is―(CH 2 ) 2 ― and R 3 is H or CH 3 .
Claim 10
Dependent Claim
20 words
A compound as claimed in any one of the preceding claims, which is in the form of a maleate salt.
Claim 11
Dependent Claim
26 words
A pharmaceutical composition comprising a compound of the formula (I) or a pharmaceutically acceptable acid addition salt thereof together with a pharmaceutically acceptable diluent or carrier.
Claim 12
Dependent Claim
26 words
A pharmaceutical composition comprising a compound of the formula (I) or a pharmaceutically acceptable acid addition salt thereof together with a pharmaceutically acceptable diluent or carrier.
Claim 13
Dependent Claim
39 words
A compound of the formula (I) or a pharmaceutically acceptable acid addition salt thereof as claimed in any one of claims 1 to 7, for use in treating ischaemic heart disease, especially angina, or hypertension, in a human being.
References Cited (Backward Citations)
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