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公开(公告)号:CA1340785C
公开(公告)日:1999-10-12
申请号:CA578630
申请日:1988-09-28
Applicant: PFIZER LTD
Inventor: RICHARDSON KENNETH , COOPER KELVIN , FRAY MICHAEL JONATHAN , STEELE JOHN
IPC: C07D233/60 , A61K31/4406 , A61K31/4418 , A61K31/4427 , A61K31/455 , A61K31/496 , A61K31/52 , A61K31/522 , A61P9/12 , A61P29/00 , A61P37/08 , C07D211/82 , C07D211/90 , C07D213/50 , C07D235/06 , C07D249/08 , C07D263/32 , C07D277/22 , C07D401/10 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D473/30 , C07D513/04 , C07D401/00 , A61K31/395
Abstract: Platelet activating factor antagonists of formula (I): (see formula I) wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C1-C4 alkyl, C1-C4 alkoxy, aryl(C1-C4)alkoxy, fluoro(C1-C4)alkoxy, C1-C4 alkylthio, C1-C4 alkylsulphonyl, hydroxy, trifluoromethyl and cyano, or is phenyl fused to a dioxole ring; R1 and R2 are each independently H or C1-C6 alkyl, or R1 and R2 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C1-C4 alkyl)piperazinyl or N-(C2-C4 alkanoyl)-piperazinyl group; or R2 is H or C1-C4 alkyl and R1 is CN, C3-C7 cycloalkyl, aryl, heteroaryl or a C1-C4 alkyl group substituted by one or more substituents selected from C3-C7 cycloalkyl, C1-C4 alkoxycarbonyl, aryl or heteroaryl; Z is selected from C1-C6 alkoxy, aryl(C1-C4)alkoxy, hydroxy, and -NR4R5 wherein each of R4 and R5 is independently H or C1-C6 alkyl, or R4 and R5 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl or N-(C1-C4 alkyl)piperazinyl group; Y is 1,4 phenylene or pyridine-2,5-diyl, and X is a 5 or 6 membered aromatic heterocyclic group containing one or more nitrogen atoms in its ring; which ring may be fused to a benzene ring or to a further 5- or 6-membered aromatic heterocyclic ring containing one or more nitrogen atoms, at least one of said heterocyclic rings optionally also containing an oxygen or sulphur atom, and being optionally substituted with one or more substituents selected from C1-C4 alkyl, C1-C4 alkoxy, halo, CF3 and CN; and their pharmaceutically acceptable salts.
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公开(公告)号:IE64774B1
公开(公告)日:1995-09-06
申请号:IE34291
申请日:1991-02-01
Applicant: PFIZER LTD
Inventor: RAY STEPHEN JAMES , RICHARDSON KENNETH
IPC: A61K31/41 , A61K31/4196 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/4427 , C07D249/08 , A61K31/443 , A61K31/495 , A61K31/505 , A61P31/04 , A61P31/10 , C07D20060101 , C07D213/61 , C07D239/24 , C07D239/28 , C07D239/30 , C07D401/06 , C07D401/10 , C07D403/06 , C07D403/10 , C07D405/06 , C07D521/00
Abstract: The invention provides antifungal compounds of the formula:- and pharmaceutically acceptable salts thereof, wherein R is phenyl substituted by 1 to 3 substituents each independently selected from halo, -CF3 and -OCF3; R is C1-C4 alkyl; R is H or C1-C4 alkyl; X is CH or N; and Y is F or Cl. a
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公开(公告)号:PT88614B
公开(公告)日:1993-07-30
申请号:PT8861488
申请日:1988-09-28
Applicant: PFIZER LTD
Inventor: RICHARDSON KENNETH , COOPER KELVIN , FRAY MICHAEL JONATHAN , STEELE JOHN
IPC: A61K31/4406 , A61K31/4418 , A61K31/4427 , A61K31/455 , A61K31/496 , A61K31/52 , A61K31/522 , A61P9/12 , A61P29/00 , A61P37/08 , C07D211/82 , C07D211/90 , C07D233/60 , C07D213/50 , C07D235/06 , C07D249/08 , C07D263/32 , C07D277/22 , C07D401/10 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D473/30 , C07D513/04 , C07D463/00 , C07D401/12 , C07C69/753 , A61K31/16 , A61K31/135 , A61K31/19
Abstract: Platelet activating factor antagonists of formula (I): wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C1-C4 alkyl, C1-C4 alkoxy, aryl(C1-C4)alkoxy, fluoro(C1-C4)alkoxy, C1-C4 alkylthio, C1-C4 alkylsulphonyl, hydroxy, trifluoromethyl and cyano, or is phenyl fused to a dioxole ring; R and R are each independently H or C1-C6 alkyl, or R and R together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C1-C4 alkyl)piperazinyl or N-(C2-C4 alkanoyl-piperazinyl group; or R is H or C1-C4 alkyl and R is CN, C3-C7 cycloalkyl, aryl, heteroaryl or a C1-C4 alkyl group substituted by one or more substituents selected from C3-C7 cycloalkyl, C1-C4 alkoxycarbonyl, aryl or heteroaryl; Z is selected from C1-C6 alkoxy, aryl(C1-C4)alkoxy, hydroxy, and -NR R wherein each of R and R is independently H or C1-C6 alkyl, or R and R together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl or N-(C1-C4 alkyl)piperazinyl group; Y is 1,4 phenylene or pyridine-2,5-diyl, and X is a 5 or 6 membered aromatic heterocyclic group containing one or more nitrogen atoms in its ring; which ring may be fused to a benzene ring or to a further 5- or 6-membered aromatic heterocyclic ring containing one or more nitrogen atoms, at least one of said heterocyclic rings optionally also containing an oxygen or sulphur atom, and being optionally substituted with one or more substituents selected from C1-C4 alkyl, C1-C4 alkoxy, halo, CF3 and CN; and their pharmaceutically acceptable salts.
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公开(公告)号:PT89195B
公开(公告)日:1993-06-30
申请号:PT8919588
申请日:1988-12-09
Applicant: PFIZER LTD
Inventor: RAY STEPHEN JAMES , RICHARDSON KENNETH
IPC: A01N43/653 , A01N43/74 , A01N43/76 , A01N43/78 , C07D249/08 , A01N43/84 , A61K31/41 , A61K31/50 , A61K31/535 , A61K31/54 , A61P31/04 , C07D249/14 , C07D401/12 , C07D403/06 , C07D413/12 , C07D417/12 , C07D521/00 , C07D417/14 , C07D413/14 , C07D401/14
Abstract: An antifungal agent of the formula:- where R is a phenyl group optionally substituted by 1 to 3 substituents each independently selected from halo and CF3; R is either (a) a phenyl group substituted by a group of the formula -N=CH-N(C1-C4 alkyl)2, or (b) a 5- or 6-membered aromatic heterocyclic group which is optionally benzo-fused and optionally substituted by 1 or 2 substituents each independently selected from halo, C1-C4 alkyl and halo-(C1 or C2 alkyl), said heterocyclic group being attached to the nitrogen atom of the piperazine ring by a carbon atom; and R is H or CH3; or an O-ester or O-ether thereof which is a C2-C4 alkanoyl or benzoyl ester, or a C1-C4 alkyl, C2-C4 alkenyl, phenyl-(C1-C4 alkyl) or phenyl ether, said phenyl and benzoyl groups of said O-esters and O-ethers being optionally substituted by one or two substituetns each selected from C1-C4 alkyl, halo and halo-(C1 or C2 alkyl); or a pharmaceutically acceptable salt thereof.
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公开(公告)号:NO910670D0
公开(公告)日:1991-02-19
申请号:NO910670
申请日:1991-02-19
Applicant: PFIZER LTD
Inventor: COOPER KELVIN , FRAY MICHAEL JONATHAN , RICHARDSON KENNETH , STEELE JOHN
IPC: C07D20060101 , C07D213/02 , C07D249/08 , C07D263/30 , C07D277/20 , C07D471/04 , C07D513/04 , C07D
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公开(公告)号:PT85607B
公开(公告)日:1990-05-31
申请号:PT8560787
申请日:1987-08-27
Applicant: PFIZER LTD
Inventor: CROSS PETER EDWARD , RICHARDSON KENNETH , COOPER KELVIN , PARRY MICHAEL JOHN
IPC: A61K31/44 , A61K31/455 , A61P37/08 , C07D211/90 , C07D277/46 , C07D285/12 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D521/00 , A61K31/415
Abstract: Compounds of the formula:- wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C1-C4 alkyl, C1-C4 alkoxy, aryl(C1-C4 alkoxy), C1-C4 alkylthio, C1-C4 alkylsulphonyl, hydroxy, trifluoromethyl and cyano; R and R are each independently H or C1-C6 alkyl, or the two groups may be joined together to form with the nitrogen atom to which they are attached a pyrrolidinyl, piperidino, morpholino, piperazinyl or N-(substituted)-piperazinyl group, said substituent being C1-C4 alkyl, C2-C4 alkanoyl or pyridyl; or R is H or C1-C4 alkyl and R is C3-C7 cycloalkyl, aryl, indanyl, or heteroaryl, or a C1-C4 alkyl group substituted by one or more substituents selected from C3-C7 cycloalkyl, C1-C4 alkoxycarbonyl, aryl and heteroaryl; R is C1-C6 alkyl; Y is an alkylene group of from 2 to 8 carbon atoms which may be straight or branched-chain having at least 2 carbon atoms in the chain linking X to the oxygen atom; X is 1-imidazolyl optionally substituted with from 1 to 3 substituents which may be C1-C4 alkyl groups or halo atoms, or wherein the 4 and 5 positions may be linked by -(CH2)p- where p is 3 or 4, and their pharmaceutically acceptable salts are antagonists of PAF and are useful in the treatment of allergic, inflammatory and hypersecretory conditions.
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公开(公告)号:DK71789A
公开(公告)日:1989-08-21
申请号:DK71789
申请日:1989-02-16
Applicant: PFIZER LTD
Inventor: COOPER KELVIN , STEELE JOHN , RICHARDSON KENNETH
IPC: C07D213/82 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/445 , A61K31/53 , A61P29/00 , A61P37/08 , C07D401/12 , C07D401/14 , C07D471/04 , C07D487/04 , C07D521/00
Abstract: Compounds of the formula:- wherein R is phenyl or phenyl substituted by nitro, halo, C1-C4 alkyl, C1-C4 alkoxy, aryl(C1-C4)alkoxy, fluoro(C1-C4)alkoxy, C1-C4 alkylthio, C1-C4 alkylsulphonyl, hydroxy, trifluoromethyl or cyano; R and R are H or C1-C6 alkyl, or the two groups form a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C1-C4 alkyl)piperazinyl or N-(C2-C4 alkanoyl)piperazinyl group; or R is H or C1-C4 alkyl and R is C3-C7 cycloalkyl, aryl, indanyl, or heteroaryl, or a C1-C4 alkyl group substituted by C3-C7 cycloalkyl, C1-C4 alkoxycarbonyl, aryl or heteroaryl; R is OH, C1-C6 alkoxy, aryl(C1-C4 alkoxy), or NR R wherein each of R and R is independently H or C1-C6 alkyl, or the two groups form a pyrrolidinyl, piperidino, morpholino, piperazinyl, or N-(C1-C4 alkyl)piperazinyl group; Y is an alkylene group of from 2 to 8 carbon atoms and X is 1,2,4-triazol-3-yl, 1,2,4-triazol-4-yl or triazolo[2,3-a]pyrid-2-yl optionally substituted by C1-C4 alkyl or phenyl; are antagonists of PAF and are useful in the treatment of allergic, inflammatory and hypersecretory conditions.
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公开(公告)号:DK686088A
公开(公告)日:1989-07-21
申请号:DK686088
申请日:1988-12-09
Applicant: PFIZER LTD
Inventor: RAY STEPHEN JAMES , RICHARDSON KENNETH
IPC: C07D249/08 , A01N43/653 , A01N43/74 , A01N43/76 , A01N43/78 , A01N43/84 , A61K31/41 , A61K31/50 , A61K31/535 , A61K31/54 , A61P31/04 , C07D249/14 , C07D401/12 , C07D403/06 , C07D413/12 , C07D417/12 , C07D521/00 , C07D403/12
Abstract: An antifungal agent of the formula:- where R is a phenyl group optionally substituted by 1 to 3 substituents each independently selected from halo and CF3; R is either (a) a phenyl group substituted by a group of the formula -N=CH-N(C1-C4 alkyl)2, or (b) a 5- or 6-membered aromatic heterocyclic group which is optionally benzo-fused and optionally substituted by 1 or 2 substituents each independently selected from halo, C1-C4 alkyl and halo-(C1 or C2 alkyl), said heterocyclic group being attached to the nitrogen atom of the piperazine ring by a carbon atom; and R is H or CH3; or an O-ester or O-ether thereof which is a C2-C4 alkanoyl or benzoyl ester, or a C1-C4 alkyl, C2-C4 alkenyl, phenyl-(C1-C4 alkyl) or phenyl ether, said phenyl and benzoyl groups of said O-esters and O-ethers being optionally substituted by one or two substituetns each selected from C1-C4 alkyl, halo and halo-(C1 or C2 alkyl); or a pharmaceutically acceptable salt thereof.
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公开(公告)号:ZA8708342B
公开(公告)日:1989-06-28
申请号:ZA8708342
申请日:1987-11-05
Applicant: PFIZER LTD
Inventor: COOPER KELVIN , KELVIN COOPER , RICHARDSON KENNETH , KENNETH RICHARDSON , CROSS PETER EDWARD , PETER EDWARD CROSS , FRAY MICHAEL JONATHAN , MICHAEL JONATHAN FRAY
IPC: A61K20060101 , C07D20060101 , C07D401/12 , C07D401/14 , C07D , A61K
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公开(公告)号:HUT47933A
公开(公告)日:1989-04-28
申请号:HU270888
申请日:1988-05-27
Applicant: PFIZER LTD
Inventor: COOPER KELVIN , FRAY MICHAEL J , RICHARDSON KENNETH
IPC: A61K31/435 , A61K31/505 , A61K31/52 , A61P37/08 , C07D211/90 , C07D471/04 , C07D473/00 , C07D487/04 , A61K31/395
Abstract: Compounds of the formula:- wherein R is phenyl or phenyl substituted by nitro, halo, C1-C4 alkyl, C1-C4 alkoxy, fluoro(C1-C4)alkoxy, aryl(C1-C4)alkoxy, C1-C4 alkylthio, C1-C4 alkylsulphonyl, hydroxy, trifluoromethyl or cyano; R and R are H or C1-C6 alkyl, or the two groups form a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C1-C4 alkyl)piperazinyl or N-(C2-C4 alkanoyl)piperazinyl group; or R is H or C1-C4 alkyl and R is C3-C7 cycloalkyl, aryl, indanyl or heteroaryl, or a C1-C4 alkyl group substituted by C3-C7 cycloalkyl, C1-C4 alkoxycarbonyl, aryl or heteroaryl; R is OH, C1-C6 alkyloxy, aryl(C1-C4 alkoxy), or NR R wherein each of R R is independently H or C1-C6 alkyl, or the two groups form a pyrrolidinyl, piperidino, morpholino, piperazinyl, or N-(C1-C4 alkyl)piperazinyl group; Y is an alkylene group of from 2 to 8 carbon atoms and X is 1-, 2- or 3-imidazopyridyl or 1-, 2- or 3-imidazopyrimidinyl optionally substituted by C1-C4 alkyl, C1-C4 alkoxy, halo, CF3 or CN; are antagonists of PAF and are useful in the treatment of allergic inflammatory and hypersecretory conditions.
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