专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明专利

JP2000128864A PREPARATION FOR BETA 3 ADRENERGIC RECEPTOR AGONIST AND INTERMEDIATE 失效
公开(公告)号：JP2000128864A
公开(公告)日：2000-05-09
申请号：JP29373399
申请日：1999-10-15
申请人： PFIZER PROD INC
发明人： DEVRIES KEITH MICHAEL , RAGGON JEFFREY WILLIAM , SHANKER RAVI MYSORE , URBAN FRANK J , VANDERPLAS BRIAN CLEMENT
IPC分类号： C07D213/74 , A61K31/44 , A61P43/00 , C07D213/16 , C07D213/73 , C07D213/75
摘要： PROBLEM TO BE SOLVED: To obtain a new compound which is an intermediate useful for synthesis of a kind of β-adrenergic receptor agonist and is useful for treatment or prevention of prostate gland diseases. SOLUTION: This compound is represented by formula I [R1 is a halogen, methanesulfonyloxy or the like; R2 is tetrahydrofuranyl, tetrahydropyranyl or the like; R3 is a (substituted beonzoyl or a 1-5C alkanoyl], its enantiomer or its pharmaceutically admissible salt, preferably toluene-4-sulfonic acid 2-(6- acetylamino-pyridin-3-yl)-2(R)-(tert-butyl-dimethyl-silyloxy)-ethyl ester. Furthermore the compound is obtained by reacting a compound of formula II with a silylating agent and a proper base (preferably imidazole) in a solvent which is inert to reaction at about 20-50 deg.C for about 12-18 hr.

2. 发明专利

JP2001151792A METHOD FOR PRODUCING CARBAMATE KETOLIDE ANTIBIOTIC 失效
公开(公告)号：JP2001151792A
公开(公告)日：2001-06-05
申请号：JP2000299453
申请日：2000-09-29
申请人： PFIZER PROD INC
发明人： KANEKO TAKUJI , MCLAUGHLIN ROBERT WILLIAM , MCMILLEN WILLIAM THOMAS , RIPIN DAVID HAROLD BROWN , VANDERPLAS BRIAN CLEMENT
IPC分类号： C07D498/04 , A61K31/7042 , A61K31/7048 , A61P31/00 , A61P31/04 , A61P33/00 , A61P33/02 , C07B61/00 , C07H17/08
摘要： PROBLEM TO BE SOLVED: To obtain a macrolide compound having an activity against various kinds of bacterial and protozoal infections. SOLUTION: This macrolide-based antibiotic comprises a compound represented by the following formula (wherein R1 is an α-branched 3-8C alkyl, 3-8C alkenyl, 3-8C alkynyl or the like in which all thereof may be substituted with 1-3 hydroxyl groups; R2 and R3 are each independently H or a 1-6C alkyl; and each R4 is independently a 6-10C aryl or a 5- to a 10-membered heterocyclic ring or the like; R5 is H or a 1-10C alkyl in which 1-3 carbons of the alkyl may be substituted with a heteroatom selected from O, S and NR2; and the alkyl group is C(O)O(1-10C alkyl), a 1-10C alkoxy, a 1-10C alkanoyl, a halo, nitro, cyano, a 5- to a 10-membered heterocyclic ring, a 6-10C aryl, a 1-10C alkyl or the like).

3. 发明专利

JP2000072744A PRODUCTION OF PYRROLIDINYLHYDROXAMIC ACID COMPOUND 失效
公开(公告)号：JP2000072744A
公开(公告)日：2000-03-07
申请号：JP18308699
申请日：1999-06-29
申请人： PFIZER PROD INC
发明人： DEVRIES KEITH MICHAEL , VANDERPLAS BRIAN CLEMENT
IPC分类号： C07D207/08 , A61K31/00 , A61K31/40 , A61P1/00 , A61P7/00 , A61P7/10 , A61P23/00 , A61P25/04 , A61P29/00 , C07D207/12 , C07D207/16
摘要： PROBLEM TO BE SOLVED: To produce a new compound which is an intermediate for compounds useful as an analgesic agent, an antiinflammatory agent, a diuretic agent, an anesthetic agent or a nervous protective agent for treating a mammalian object, especially a human object in order to treat fits or functional intestinal diseases. SOLUTION: This compound is represented by formula I. The compound is an intermediate for producing 2-(3,4-dichlorophenyl)-N-hydroxy-N-[1-(S)- phenyl-2-(3-hydroxy-pyrrolidin-1-yl)ethyl]acetamide p-methylphenylsulfonate. The compound can be produced by a method for reacting, e.g. a compound represented by formula II (Bn is benzyl) with a compound BzCl (Bz is formula III) in CH2Cl2 and then reacting the resultant compound represented by formula IV using PdC, H2 and TsOH (p-toluenesulfonic acid) in THF at 50 deg.C, etc.

4. 发明专利

BRPI0415459A 未知
公开(公告)号：BRPI0415459A
公开(公告)日：2006-12-19
申请号：BRPI0415459
申请日：2004-10-06
申请人： PFIZER PROD INC
发明人： COE JOTHAM WADSWORTH , MCHARDY STANTON FURST , RAGAN JOHN ANTHONY , TICKNER DEREK LAWRENCE , VANDERPLAS BRIAN CLEMENT
IPC分类号： A61K31/403 , C07D209/02 , C07D209/52
摘要： This present invention relates to a new and improved reductive amination process for the preparation of 3-azabicyclo[3.1.0]hexane derivatives and pharmaceutical compositions comprising such derivatives. The invention particularly relates to using such derivatives to treat certain disorders and conditions, including, for example, irritable bowel syndrome, drug addiction or dependency, alcohol addiction or dependency, depression, and eating disorders.

5. 发明专利

YU57900A SINTEZA KARBAMATNO KETOLIDNIH ANTIBIOTIKA 未知
公开(公告)号：YU57900A
公开(公告)日：2003-02-28
申请号：YUP57900
申请日：2000-09-22
申请人： PFIZER PROD INC
发明人： TAKUSHI KANEKO , MCLAUGHLIN WILIAM ROBERT , MCMILAN WILIAM THOMAS , RIPIN DAVID HAROLD , VANDERPLAS BRIAN CLEMENT
IPC分类号： C07D498/04 , A61K31/7042 , A61K31/7048 , A61P31/00 , A61P31/04 , A61P33/00 , A61P33/02 , C07B61/00 , C07H17/08
摘要： Pronalazak se odnosi na postupak za proizvodnju makrolidnog antinibotika formule: u kojoj R1, R2, R3, R4, R5 su kako je definisano ranije. Ovi antibiotici su korisna antibakterijska i antiprotozojska sredstva kod sisara, uključujući čoveka, kao i kod riba i ptica. Pronalazak takodje obuhvata nova jedinjenja, proizvedenih prilikom pripreme makrolidnog antibiotika.[Invention refers to the procedure for the production of macrolide antibiotic of formula: wherein R1, R2, R3, R4, R5 are as previously defined. These antibiotics are useful antibacterical antiprotosoic means with mammals including men, such as fish and birds. The invention also includes new compounds, produced during the preparation of macrolide antibiotics.

6. 发明专利

BR9902525A 未知
公开(公告)号：BR9902525A
公开(公告)日：2000-05-02
申请号：BR9902525
申请日：1999-07-01
申请人： PFIZER PROD INC
发明人： DEVRIES KEITH MICHAEL , VANDERPLAS BRIAN CLEMENT
IPC分类号： C07D207/08 , A61K31/00 , A61K31/40 , A61P1/00 , A61P7/00 , A61P7/10 , A61P23/00 , A61P25/04 , A61P29/00 , C07D207/12 , C07D207/16
摘要： A method for preparing hydroxamic acid derivatives of the formula: and the salt thereof, wherein A is hydroxy, Ar is phenyl, or phenyl substituted with up to three substituents selected from chloro, methyl and CF3, more preferably 3,4-dichlorophenyl, R is hydrogen, and X is phenyl, naphthyl, biphenyl, indanyl, benzofuranyl, benzothiophenyl, 1-tetralone-6-yl, C1-C4alkylenedioxy, pyridyl, furyl and thienyl, these groups optionally being substituted with up to three substituents selected from halo, C1-C4alkyl, C1-C4alkoxy, hydroxy, NO2, CF3 and SO2CH3. This invention also provides novel intermediates which are useful for preparing compounds of Formula I. The hydroxamic acid derivatives of formula (I), wherein A is hydrogen or hydroxy and R is hydrogen or C1-C4alkyl, exhibit significant agonist activity toward opioid kappa -receptor. Therefore these kappa agonists are particularly useful as an analgesic agent in mammals, especially humans. They are also useful as antiinflammatory, diuretic, anesthetic or neuroprotective agents, or an agent for treatment of stroke or functional bowel diseases such as abdominal pain, for the treatment of a mammalian subject, especially a human subject.

7. 发明专利

ID23462A 未知
公开(公告)号：ID23462A
公开(公告)日：2000-04-27
申请号：ID990637
申请日：1999-07-01
申请人： PFIZER PROD INC
发明人： DEVRIES KEITH MICHAEL , VANDERPLAS BRIAN CLEMENT
IPC分类号： A61K31/00 , C07D207/08 , A61K31/40 , A61P1/00 , A61P7/00 , A61P7/10 , A61P23/00 , A61P25/04 , A61P29/00 , C07D207/12 , C07D207/16 , A61K31/185
摘要： A method for preparing hydroxamic acid derivatives of the formula: and the salt thereof, wherein A is hydroxy, Ar is phenyl, or phenyl substituted with up to three substituents selected from chloro, methyl and CF3, more preferably 3,4-dichlorophenyl, R is hydrogen, and X is phenyl, naphthyl, biphenyl, indanyl, benzofuranyl, benzothiophenyl, 1-tetralone-6-yl, C1-C4alkylenedioxy, pyridyl, furyl and thienyl, these groups optionally being substituted with up to three substituents selected from halo, C1-C4alkyl, C1-C4alkoxy, hydroxy, NO2, CF3 and SO2CH3. This invention also provides novel intermediates which are useful for preparing compounds of Formula I. The hydroxamic acid derivatives of formula (I), wherein A is hydrogen or hydroxy and R is hydrogen or C1-C4alkyl, exhibit significant agonist activity toward opioid kappa -receptor. Therefore these kappa agonists are particularly useful as an analgesic agent in mammals, especially humans. They are also useful as antiinflammatory, diuretic, anesthetic or neuroprotective agents, or an agent for treatment of stroke or functional bowel diseases such as abdominal pain, for the treatment of a mammalian subject, especially a human subject.

8. 发明专利

PL336053A1 NOVEL DERIVATIVES OF AMINO PYRIDINE, METHODS OF OBTAINING THEM, METHODS OBTAINING (4-(2-(2-(6-AMINOPYRIDIN-3-YL(-2(R)-HYDROXYETHYLAMINO)ETHOXY)PHENYL) ACETIC ACID, ITS NOVEL POLYMORPHOUS FORM AND PHARMACEUTIC AGENT 未知
公开(公告)号：PL336053A1
公开(公告)日：2000-04-25
申请号：PL33605399
申请日：1999-10-15
申请人： PFIZER PROD INC
发明人： DEVRIES KEITH MICHAEL , RAGGON JEFFREY WILLIAM , SHANKER RAVI MYSORE , URBAN FRANK JOHN , VANDERPLAS BRIAN CLEMENT
IPC分类号： C07D213/74 , A61K31/44 , A61P43/00 , C07D213/16 , C07D213/73 , C07D213/75 , C07D213/72 , C07D405/06 , C07D401/06
摘要： The instant invention relates to intermediates of Formula II, wherein R , R and R are as defined in the specification, and to processes for preparing such intermediates. This invention also relates to processes for preparing compounds of Formula III, and enantiomers thereof, wherein R , R and R are as defined in the specification. Compounds of Formula II and Formula III are intermediates in the preparation of a potent beta 3 adrenergic receptor agonist. The instant invention also relates to processes for preparing the beta 3 adrenergic receptor agonist using the compounds of Formula II and Formula III.

9. 发明专利

DE69928890D1 未知
公开(公告)号：DE69928890D1
公开(公告)日：2006-01-19
申请号：DE69928890
申请日：1999-10-11
申请人： PFIZER PROD INC
发明人： DEVRIES KEITH MICHAEL , RAGGON JEFFREY WILLIAM , SHANKER RAVI MYSORE , VANDERPLAS BRIAN CLEMENT , URBAN FRANK JOHN
IPC分类号： C07D213/74 , A61K31/44 , A61P43/00 , C07D213/16 , C07D213/73 , C07D213/75
摘要： The instant invention relates to intermediates of Formula II, wherein R , R and R are as defined in the specification, and to processes for preparing such intermediates. This invention also relates to processes for preparing compounds of Formula III, and enantiomers thereof, wherein R , R and R are as defined in the specification. Compounds of Formula II and Formula III are intermediates in the preparation of a potent beta 3 adrenergic receptor agonist. The instant invention also relates to processes for preparing the beta 3 adrenergic receptor agonist using the compounds of Formula II and Formula III.

10. 发明专利

IN187119B A process for preparing carbamate ketolide antibiotics 未知
公开(公告)号：IN187119B
公开(公告)日：2002-02-09
申请号：IN879MU2000
申请日：2000-09-25
申请人： PFIZER PROD INC
发明人： KANEKO TAKUSHI , MCLAUGHIN ROBERT WILLIAM , MCMILLEN WILLIAM THOMAS , RIPIN DAVID HAROLD BROWN , VANDERPLAS BRIAN CLEMENT
IPC分类号： C07D498/04 , A61K31/7042 , A61K31/7048 , A61P31/00 , A61P31/04 , A61P33/00 , A61P33/02 , C07B61/00 , C07H17/08 , C07G11/00
摘要： The invention relates to a method of preparing a macrolide antibiotic of the formula wherein R , R , R , R , R are defined above. These antibiotics are useful as antibacterial and antiprotozoal agents in mammals, including man, as well as in fish and birds. The invention also includes novel compounds made by the preparation of the macrolide antibiotic.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式