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1. 发明专利

JP2002105083A NEW METHOD 审中-公开
公开(公告)号：JP2002105083A
公开(公告)日：2002-04-10
申请号：JP2001233551
申请日：2001-08-01
申请人： PFIZER
发明人： BEST DESMOND JOHN , BURTON GEORGE , GASSON BRIAN CHARLES , OSBORNE NEAL FREDERICK , WALKER GRAHAM
IPC分类号： C07D463/06 , C07D463/16 , C07D501/00 , C07D501/04 , C07D501/20 , C07D501/24 , C07D501/26 , C07D501/60 , C07D505/06 , C07D505/16 , C07D505/18
摘要： PROBLEM TO BE SOLVED: To provide a method of preparing a cephalosporin compound and an intermediate for preparation of these compound. SOLUTION: This method cyclizes a compound of formula (III) to obtain a compound expressed by formula (II). [R1 is H, a methoxy or formamide group; R2 is an acryl group; CO2R3 is a carboxyl group or a carboxylic acid salt anion or a carboxy protecting group; R4 is H, an alkyl group, alkenyl group, alkynyl group, alkoxy group, hydroxyl group, halogen atom, amino group or the like; X is S, SO, SO2, O or CH2: m is 1 or 2; dotted line means that the compound (II) and (III) can be 2- or 3-cephem based compound and in the case of a substituent R4 is not H then the hydrogen atoms bonding to carbon atoms in the side chain may be substituted].

2. 发明专利

DE69231978D1 未知
公开(公告)号：DE69231978D1
公开(公告)日：2001-09-06
申请号：DE69231978
申请日：1992-12-01
申请人： PFIZER
发明人： BURTON GEORGE , FELL CHRISTOPHER
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D498/04 , C07D501/00 , C07D501/18 , C07D501/20 , C07D501/24 , A61K31/435 , A61K31/535 , C07D463/00

3. 发明专利

DE69032681T2 未知
公开(公告)号：DE69032681T2
公开(公告)日：1999-02-25
申请号：DE69032681
申请日：1990-03-26
申请人： PFIZER
发明人： BATESON JOHN HARGREAVES , BURTON GEORGE , FELL STEPHEN CHRISTOPHER MARTI
IPC分类号： C07D477/00 , A61K20060101 , A61K31/00 , A61K31/397 , A61K31/435 , A61K31/4353 , A61K31/535 , A61K31/5365 , A61K31/545 , A61K31/546 , A61P31/00 , A61P31/04 , C07D20060101 , C07D463/00 , C07D498/04 , C07D501/18 , C07D501/20 , C07D501/24 , C07D501/56 , C07D505/00
摘要： beta -Lactam compounds of the formula (Ia) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics: wherein R is hydrogen, methoxy or formamido; R is an acyl group, in particular that of an antibacterially active cephalosporin; CO2R is a carboxy group or a carboxylate anion; R is a gamma -lactone ring optionally containing an endocyclic double bond, which ring is optionally substituted at any carbon atom by alkyl, dialkylamino, alkoxy, hydroxy, halogen or aryl, which in the case of more than one substituent may be the same or different, or is optionally di-substituted at two adjacent carbon atoms, which are available for substitution, to form an aromatic fused bicyclic system; and X is S, SO, SO2, O or CH2.

4. 发明专利

ES2121745T3 未知
公开(公告)号：ES2121745T3
公开(公告)日：1998-12-16
申请号：ES90303177
申请日：1990-03-26
申请人： PFIZER
发明人： BATESON JOHN HARGREAVES , BURTON GEORGE , FELL STEPHEN CHRISTOPHER MARTI
IPC分类号： C07D477/00 , A61K20060101 , A61K31/00 , A61K31/397 , A61K31/435 , A61K31/4353 , A61K31/535 , A61K31/5365 , A61K31/545 , A61K31/546 , A61P31/00 , A61P31/04 , C07D20060101 , C07D463/00 , C07D498/04 , C07D501/18 , C07D501/20 , C07D501/24 , C07D501/56 , C07D505/00
摘要： beta -Lactam compounds of the formula (Ia) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics: wherein R is hydrogen, methoxy or formamido; R is an acyl group, in particular that of an antibacterially active cephalosporin; CO2R is a carboxy group or a carboxylate anion; R is a gamma -lactone ring optionally containing an endocyclic double bond, which ring is optionally substituted at any carbon atom by alkyl, dialkylamino, alkoxy, hydroxy, halogen or aryl, which in the case of more than one substituent may be the same or different, or is optionally di-substituted at two adjacent carbon atoms, which are available for substitution, to form an aromatic fused bicyclic system; and X is S, SO, SO2, O or CH2.

5. 发明专利

AT171705T 未知
公开(公告)号：AT171705T
公开(公告)日：1998-10-15
申请号：AT90303177
申请日：1990-03-26
申请人： PFIZER
发明人： BATESON JOHN HARGREAVES , BURTON GEORGE , FELL STEPHEN CHRISTOPHER MARTI , PARK
IPC分类号： C07D477/00 , A61K20060101 , A61K31/00 , A61K31/397 , A61K31/435 , A61K31/4353 , A61K31/535 , A61K31/5365 , A61K31/545 , A61K31/546 , A61P31/00 , A61P31/04 , C07D20060101 , C07D463/00 , C07D498/04 , C07D501/18 , C07D501/20 , C07D501/24 , C07D501/56 , C07D505/00
摘要： beta -Lactam compounds of the formula (Ia) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics: wherein R is hydrogen, methoxy or formamido; R is an acyl group, in particular that of an antibacterially active cephalosporin; CO2R is a carboxy group or a carboxylate anion; R is a gamma -lactone ring optionally containing an endocyclic double bond, which ring is optionally substituted at any carbon atom by alkyl, dialkylamino, alkoxy, hydroxy, halogen or aryl, which in the case of more than one substituent may be the same or different, or is optionally di-substituted at two adjacent carbon atoms, which are available for substitution, to form an aromatic fused bicyclic system; and X is S, SO, SO2, O or CH2.

6. 发明专利

CA2359744C CEPHALOSPORINS AND HOMOLOGUES PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS 未知
公开(公告)号：CA2359744C
公开(公告)日：2007-02-13
申请号：CA2359744
申请日：1991-07-22
申请人： PFIZER LTD
发明人： FELL STEPHEN CHRISTOPHER MARTI , BATESON JOHN HARGREAVES , BURTON GEORGE
IPC分类号： A61K31/545 , C07D501/20 , A61K31/397 , A61K31/546 , A61P31/04 , C07D20060101 , C07D205/08 , C07D205/09 , C07D463/00 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/08 , C07D501/18 , C07D501/24 , C07D501/48 , C07D501/50 , C07D501/52 , C07D501/54 , C07D501/56 , C07D505/00
摘要： B-Lactam antibiotics of formula (I) or a salt thereof, wherein R1 is hydrogen, methoxy or formamido; R2 is an acyl group; CO2R3 is a carboxy group or a carboxylate anion, or R3is a readily removable carboxy protecting group; R4 represents up to four substituents; X is S, SO, SO2, O or CH2; m is 1 or 2; and n is 0, useful in the treatment of bacterial infections in humans and animals.

7. 发明专利

ES2252158T3 PROCEDIMIENTO PARA LA PREPARACION DE COMPUESTOS DE CEFALOSPORINA Y PRODUCTOS INTERMEDIOS PARA LA SINTESIS DE ESTOS COMPUESTOS. 未知
公开(公告)号：ES2252158T3
公开(公告)日：2006-05-16
申请号：ES01306325
申请日：2001-07-23
申请人： PFIZER
发明人： BURTON GEORGE , BEST DESMOND JOHN , GASSON BRIAN CHARLES , OSBORNE NEAL FREDERICK , WALKER GRAHAM
IPC分类号： C07D463/06 , C07D463/16 , C07D501/00 , C07D501/04 , C07D501/20 , C07D501/24 , C07D501/26 , C07D501/60 , C07D505/06 , C07D505/16 , C07D505/18
摘要： Un proceso para la preparación de un compuesto de fórmula (II) que incluye la etapa de ciclizar un compuesto de fórmula (III) fórmulas (II) y (III) en las que: R1 es hidrógeno, metoxi o formamido, R2 es un grupo acilo, CO2R3 es un grupo carboxi o un anión carboxilato, o R3 es un grupo protector de carboxi fácilmente separable, R4 representa hidrógeno o hasta cuatro sustituyentes, que pueden ser iguales o diferentes, seleccionados de alquilo, alquenilo, alquinilo, alcoxi, hidroxi, halógeno, amino, alquilamino, acilamino, dialquilamino, CO2R, CONR2, SO2NR2 (en los que R es hidrógeno o alquilo C1-C6), arilo y heterociclilo, X es S, SO, SO2, O o CH2, m es 1 ó 2, y la línea de puntos indica que los compuestos (II) y (III) pueden ser un sistema de 2-cefemo o o 33-cefemo, y, en la fórmula (III), cuando los sustituyentes R4 son distintos de hidrógeno pueden reemplazar a cualquiera de los átomos de hidrógeno unidos a átomos de carbono de la cadena lateral, y en las que los términos ¿alquilo¿, ¿alquenilo¿, ¿alquinilo¿ y ¿alcoxi¿ significan grupos de cadena lineal o ramificada que contienen 1 a 6 átomos de carbono; el término ¿arilo¿ significa fenilo y naftilo, sustituido opcionalmente cada uno con hasta cinco grupos seleccionados de grupos halógeno, mercapto, alquilo C1-C6, fenilo, alcoxi C1-C6, hidroxialquilo C1-C6, mercaptoalquilo C1-C6, haloalquilo C1-C6, hidroxi, amino, nitro, carboxi, (alquil C1-C6) carboniloxi, alcoxicarbonilo, formilo o (alquil C1-C6) carbonilo y el término ¿heterociclilo¿ significa anillos aromáticos y no aromáticos, simples y condensados, que contienen en cada anillo hasta cuatro heteroátomos seleccionados de oxígeno, nitrógeno y azufre, anillos que pueden no estar sustituidos o estar sustituidos por hasta tres grupos seleccionados de grupos halógeno, alquilo C1-C6, alcoxi C1-C6, haloalquilo C1-C6, hidroxi, carboxi, sales carboxi, ésteres carboxi, arilo y oxo, y en los que cada anillo heterocíclico tiene 4 a 7 átomos en el anillo.

8. 发明专利

AT314377T 未知
公开(公告)号：AT314377T
公开(公告)日：2006-01-15
申请号：AT01306325
申请日：2001-07-23
申请人： PFIZER
发明人： BURTON GEORGE , RAMSGATE ROAD , BEST DESMOND JOHN PFIZER GLOBA , GASSON BRIAN CHARLES PFIZER GL , OSBORNE NEAL FREDERICK PFIZER , WALKER GRAHAM PFIZER GLOBAL RE
IPC分类号： C07D463/06 , C07D463/16 , C07D501/00 , C07D501/04 , C07D501/20 , C07D501/24 , C07D501/26 , C07D501/60 , C07D505/06 , C07D505/16 , C07D505/18
摘要： There is provided a process for the preparation of a compound according to Formula (II): which includes the step of cyclising a compound of Formula (III): wherein R , R , R , R , X and m have meanings which are given in the description.

9. 发明专利

DE69331047D1 未知
公开(公告)号：DE69331047D1
公开(公告)日：2001-12-06
申请号：DE69331047
申请日：1993-01-14
申请人： PFIZER
发明人： BURTON GEORGE , GASSON BRIAN CHARLES , FELL STEPHEN CHRISTOPHER MARTI
IPC分类号： A61K31/535 , A61K31/5383 , A61K31/54 , A61K31/542 , A61P31/04 , C07D405/06 , C07D498/04 , C07D507/02 , C07D507/04 , C07D507/06 , C07D507/08 , C07D513/04
摘要： PCT No. PCT/GB93/00068 Sec. 371 Date Jul. 20, 1994 Sec. 102(e) Date Jul. 20, 1994 PCT Filed Jan. 14, 1993 PCT Pub. No. WO93/15085 PCT Pub. Date Aug. 5, 1993Compounds of the formula: (I) wherein R1 is hydrogen, methoxy or formamido; R2 is an acyl group, in particular that of an antibacterially active cephalosporin; CO2R3 is a carboxy group or a carboxylate anion, or R3 is a readily removable carboxy promoting group or a pharmaceutically acceptable salt-forming group or in vivo hydrolysable ester group; R4 represents hydrogen or up to four substituents, which my be present on any of the carbon atoms in the ring system shown, selected from alkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, amino, alkylamino, acylamino, dialkylamino, CO2R, CONR2, SO2NR2 where R is hydrogen or alkyl, aryl and heterocyclyl, which may be the same or different and wherein any R4 aryl substituent is optionally substituted by one or more substituents selected from the list from which R4 is selected Y is O, S, SO or SO2; n is 0 or 1; and m is 1 or 2; for use in the treatment of bacterial infections in humans and animals.

10. 发明专利

DE69131714D1 未知
公开(公告)号：DE69131714D1
公开(公告)日：1999-11-18
申请号：DE69131714
申请日：1991-07-22
申请人： PFIZER
发明人： BATESON JOHN HARGREAVES , BURTON GEORGE , FELL STEPHEN CHRISTOPHER MARTI
IPC分类号： A61K31/545 , A61K31/397 , A61K31/546 , A61P31/04 , C07D20060101 , C07D205/08 , C07D205/09 , C07D463/00 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/08 , C07D501/18 , C07D501/20 , C07D501/24 , C07D501/48 , C07D501/50 , C07D501/52 , C07D501/54 , C07D501/56 , C07D505/00 , A61K31/435
摘要： beta -Lactam antibiotics of formula (I) or a salt thereof, wherein R is hydrogen, methoxy or formamido; R is an acyl group; CO2R is a carboxy group or a carboxylate anion, or R is a readily removable carboxy protecting group; R represents up to four substituents; X is S, SO, SO2, O or CH2; m is 1 or 2; and n is 0, useful in the treatment of bacterial infections in humans and animals.

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