公开(公告)号：EP0262785A1

公开(公告)日：1988-04-06

申请号：EP87307446.2

申请日：1987-08-24

申请人： BEECHAM GROUP PLC

发明人： Ainsworth, Anthony Trevor ,  Smith, David Glynn ,  Arch Jonathan Robert Sanders

IPC分类号： C07C217/54 ,  A61K31/135

CPC分类号： A61K31/135

摘要： N-[2-(4-carboxymethoxyphenyl)-1-(R)-1-methylethyl]-2-(R)-2-hydroxy 2-(3-chlorophenyl)ethanamine or the methyl ester thereof, or a pharmaceutically acceptable salt thereof, ('the RR-isomer') optionally in admixture with N-[2-(4-carboxymethoxyphenyl)-1-(S)-1-methylethyl]-2-(S)-2-hydroxy-2-(3 chlorophenyl)ethanamine, or the methyl ester thereof, or a pharmaceutically acceptable salt thereof, ('the SS-isomer') wherein the SS-isomer forms less than 50% by weight of the mixture of the RR- and SS- isomers; a process for preparing such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds and compositions in medicine and agriculture.

摘要翻译： N- [2-（4-羧基甲氧基苯基）-1-（R）-1-甲基乙基] -2-（R）-2-羟基2-（3-氯苯基）乙胺或其甲酯或其药学上可接受的盐 （“RR-异构体”），任选与N- [2-（4-羧基甲氧基苯基）-1-（S）-1-甲基乙基] -2-（S）-2-羟基-2-（3 氯苯基）乙胺或其甲酯或其药学上可接受的盐（“SS-异构体”），其中SS-异构体形成少于RR-和SS-异构体的混合物的50重量％ 制备这种化合物的方法，包含这些化合物的药物组合物以及这些化合物和组合物在医药和农业中的用途。

公开(公告)号：EP0114752B1

公开(公告)日：1988-04-06

申请号：EP84300339.3

申请日：1984-01-19

申请人： BEECHAM GROUP PLC

发明人： Milner, Peter Henry

IPC分类号： C07D501/20 ,  C07D499/44 ,  A61K31/545 ,  A61K31/43

CPC分类号： C07D241/08 ,  C07D499/00

公开(公告)号：EP0261964A2

公开(公告)日：1988-03-30

申请号：EP87308444.6

申请日：1987-09-24

申请人： BEECHAM GROUP PLC

发明人： King, Francis David

IPC分类号： C07D451/14 ,  C07D451/04 ,  A61K31/44 ,  A61K31/46

CPC分类号： C07D451/04 ,  C07D451/14

摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof:
wherein
X is CH or N;
Y is NH or O;
R₁ is hydrogen or halogen;
R₂ is a group of formula (a), (b) or (c)

wherein n is 2 or 3; p and q are independently 1 to 3; and
R₄ or R₅ is C 1-4 ;
R₃ is C 1-10 acyl, C 1-6 alkoxycarbonyl, optionally substituted phenoxycarbonyl or benzyloxycarbonyl, or R₆R₇NCO or R₆R₇NS(O) m wherein m is 1 or 2 and R₆ and R₇ are independently C 1-6 alkyl groups or together are C 4-6 polymethylene; having 5-HT₃ antagonist activity, a process for their preparation and their use as pharmaceuticals.

摘要翻译： 式（I）化合物及其药学上可接受的盐：其中X是CH或N; Y是NH或O; R 1是氢或卤素; R 2是式（a），（b）或（c）的基团，其中n是2或3; p和q独立地为1至3; 和R 4或R 5是C 1-4; R 3是C 1-10酰基，C 1-6烷氧羰基，任选取代的苯氧羰基或苄氧羰基，或R 6 R 8 NCO或R 6 R 8 NS（O）m，其中m是1或2，R 6和R 6独立地是C 1-6烷基或一起是C 4-6多亚甲基 ; 具有5-HT 3拮抗剂活性，它们的制备方法以及它们作为药物的用途。

公开(公告)号：EP0254582A3

公开(公告)日：1988-03-30

申请号：EP87306546

申请日：1987-07-24

申请人： BEECHAM GROUP PLC

发明人： Gasson, Brian Charles ,  Pearson, Michael John

IPC分类号： C07D499/70 ,  C07D213/73 ,  C07D213/74 ,  C07D239/42 ,  C07D285/08 ,  A61K31/43

CPC分类号： C07D499/00

摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or in - vivo hydrolysable ester thereof:
wherein R¹ is a 5 or 6 membered sulphur and/or nitrogen containing heterocyclic group substituted by an optionally protected amino group, with the proviso that R¹ is not 2-aminothiazol-4-yl, and R is hydrogen; optionally substituted C 1-12 alkyl; optionally substituted C 2-12 alkenyl or alkynyl; carbocyclyl; aryl or heterocyclyl. These compounds have antibacterial properties, and therefore are of use in the treatment of bacterial infections in humans and animals caused by a wide range of organisms.

公开(公告)号：EP0260790A2

公开(公告)日：1988-03-23

申请号：EP87306195.6

申请日：1987-07-14

申请人： BEECHAM GROUP PLC

发明人： Hamilton, Thomas Conway ,  Buckingham, Robin Edwin

IPC分类号： A61K31/44

CPC分类号： A61K31/44

摘要： A method for the treatment and/or prophylaxis of incontinence in mammals, which method comprises administering to the mammal an effective amount of the compound pinacidil or a pharmaceutically acceptable salt or solvate thereof.

摘要翻译： 一种用于治疗和/或预防哺乳动物失禁的方法，该方法包括向哺乳动物施用有效量的化合物pinacidil或其药学上可接受的盐或溶剂合物。

公开(公告)号：EP0255297A2

公开(公告)日：1988-02-03

申请号：EP87306545.2

申请日：1987-07-24

申请人： BEECHAM GROUP PLC

发明人： King, Francis David

IPC分类号： C07D451/04 ,  A61K31/46

CPC分类号： C07D451/04

摘要： Compounds of formula (I), or a pharmaceutically acceptable salt thereof:
wherein:

Het is monocyclic heteroaryl having two adjacent carbon atoms, a and b, depicted in formula (I);
R 1 and R 2 are independently selected from hydrogen, halogen, CF 3 , C 1-6 alkyl and C 1-6 alkoxy;
R 3 is hydroxy, C 1-6 alkoxy, C 3-7 alkenyl-methoxy, phenoxy or phenyl C 1-4 alkoxy in which either phenyl moiety may be substituted by one or two C 1-6 alkyl, C 1-6 alkoxy or halo; CO 2 R 6 wherein R 6 is hydrogen or C 1-6 alkyl, CONR 7 R 8 or SO 2 NR 7 R 8 wherein R 7 and R a are independently hydrogen or C 1-6 alkyl or together are C 4-6 polymethylene, NO 2 , (CH 2 ) m O9 R wherein m is 1 or 2 and R 9 is C 1-6 alkyl or S(O) n R 10 wherein n is 0, 1 or 2 and R, o is C 1-6 alkyl;
L is NH or 0;
Z is a group of formula (a), (b) or (c):


wherein n is 2 or 3; p is 1 or 2; q is 1 to 3; r is 1 to 3; and
R 4 or R 5 is C 1-4 alkyl; having 5-HT 3 antagonist activity, a process for their preparation and their use as pharmaceuticals.

摘要翻译： （I）或其药学上可接受的盐式I的化合物： worin：Het是具有两个相邻的碳原子，a和b，在式（I）中所示的单环杂芳基; R1和R2独立地选自氢，卤素，CF 3，C 1-6烷基和C 1-6烷氧基; R 3为羟基，C 1-6烷氧基，C 3-7链烯基甲氧基，其中苯氧基或苯基C 1-4烷氧基可以是被一个或两个C 1-6烷基，C 1-6烷氧基或卤素取代的苯基任部分; CO2R6 worin R6是氢或C 1-6烷基，CONR7R8或SO2NR7R8 worin R7和R8独立地是氢或C 1-6烷基或一起为C 4-6聚亚甲基，NO 2，（CH 2）mOR9 worin m是1或2和R 9是C1 1-6烷基或S（O）NR10 worin n为0，1或2，R 10是C 1-6烷基; L是NH或O; Z为下式基团的（a），（b）或（c）中的; 2 worin n是或3; p是1或2; q为1至3; r为1至3; 和R 4或R 5是C 1-4烷基; 具有5-HT 3拮抗剂活性，其制备方法及其作为药物的用途。

公开(公告)号：EP0254582A2

公开(公告)日：1988-01-27

申请号：EP87306546.0

申请日：1987-07-24

申请人： BEECHAM GROUP PLC

发明人： Gasson, Brian Charles ,  Pearson, Michael John

IPC分类号： C07D499/70 ,  C07D213/73 ,  C07D213/74 ,  C07D239/42 ,  C07D285/08 ,  A61K31/43

CPC分类号： C07D499/00

摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or in - vivo hydrolysable ester thereof:
wherein R¹ is a 5 or 6 membered sulphur and/or nitrogen containing heterocyclic group substituted by an optionally protected amino group, with the proviso that R¹ is not 2-aminothiazol-4-yl, and R is hydrogen; optionally substituted C 1-12 alkyl; optionally substituted C 2-12 alkenyl or alkynyl; carbocyclyl; aryl or heterocyclyl.
These compounds have antibacterial properties, and therefore are of use in the treatment of bacterial infections in humans and animals caused by a wide range of organisms.

摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐或体内可水解的酯：其中R 1是被任选地被取代的5或6元硫和/或含氮杂环基团 保护的氨基，条件是R 1不是2-氨基噻唑-4-基，R是氢; 任选取代的C 1-12烷基; 任选取代的C 2-12烯基或炔基; 碳环; 芳基或杂环基。 这些化合物具有抗菌性质，因此可用于治疗由各种生物引起的人和动物细菌感染。

公开(公告)号：EP0196849A3

公开(公告)日：1988-01-07

申请号：EP86302145

申请日：1986-03-24

申请人： BEECHAM GROUP PLC

发明人： Smith, David Glynn ,  White, Susan Mary

IPC分类号： C07C91/18 ,  C07C93/06 ,  C07C91/34 ,  C07C91/40 ,  A61K31/135 ,  C07C87/18 ,  C07C93/08

CPC分类号： A61K31/135 ,  A23K20/111 ,  A61K31/165

摘要： A compound of formula (I):
or a pharmaceutically acceptable salt thereof, wherein R A is a group of formula (a):
wherein T represents a group of formula (b):
wherein Q is
, and where
R' is a hydrogen or halogen atom or a -CF 3 , OR 4 , NHR 4 , -NHCOR 4 , -NHCONH 2 , NHSO 2 R 4 , CH 2 OR 4 or -CH 2 SO 2 R 4 group: R 2 is a hydrogen or halogen atom or an -OR 4 group; R 3 is a hydrogen or halogen atome; and R 4 is hydrogen, C 1-6 alkyl or benzyl; X' is a bond or -OCH 2 -; X 2 is a group of formula -CR 5 R 6 -CH 2 -A-wherein R 5 and R 6 are independently hydrogen or methyl; and A is a bond, -CH 2 -, or O; T' represents a hydrogen atom or a group of formula (b) as defined above in respect of T, such that T' and T may be the same or different; R C represents a group (a) as defined above in respect of R A , such that R C and R A may be the same or different; provided that when R A and R C each represent a group of formula:
wherein R is oH or -O-benzyl; then when A is a bond, -CH 2 - or -0, R' is not -CH 2 OH or NHSO 2 -C 1-4 alkyl; processes for the preparation of such compounds and their use in medicine and agriculture.

公开(公告)号：EP0250071A1

公开(公告)日：1987-12-23

申请号：EP87303535.6

申请日：1987-04-22

申请人： BEECHAM GROUP PLC

发明人： Robinson, Jeffery Hugh Beecham Pharmaceuticals ,  Dodd, Ian Beecham Pharmaceuticals

IPC分类号： C12N9/48 ,  C12N9/68 ,  C12N9/72 ,  C07K15/00 ,  C12N15/00 ,  A61K37/54

CPC分类号： C12N9/6435 ,  A61K38/00 ,  C07K2319/00 ,  C12N9/6462 ,  C12N9/96 ,  C12Y304/21007 ,  C12Y304/21073

摘要： A hybrid protein which comprises plasmin A-chain linked to urokinase B-chain, the catalytic site of which is blocked by a removable blocking group.

摘要翻译： 一种杂合蛋白，其包含与尿激酶B链连接的纤溶酶A链，其催化位点被可除去的封闭基团阻断。

公开(公告)号：EP0214818A3

公开(公告)日：1987-12-16

申请号：EP86306690

申请日：1986-08-29

申请人： BEECHAM GROUP PLC

发明人： Cassidy, Frederick ,  Stemp, Geoffrey ,  Evans, John Morris

IPC分类号： C07D311/68 ,  C07D311/70 ,  A61K31/35

CPC分类号： C07D311/70 ,  C07D311/68

摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof: R
wherein:
one of R, and R 2 is hydrogen or C 1-4 alkyl and the other is C 1-4 alkyl or R, and R 2 together are C 2-5 -polymethylene; either R 3 is hydrogen, hydroxy, C 1-6 alkoxy or C 1-7 acyloxy and R 4 is hydrogen or R 3 and R 4 together are a bond; R 5 is hydrogen, C 1-6 alkyl optionally substituted by halogen, hydroxy, C 1-6 alkoxy, C 1-6 alkoxycarbonyl, carboxy or amino optionally substituted by one or two independent C 1-6 alkyl groups, or C 2-6 alkenyl, amino optionally substituted by a C 1-6 alkyl or C 1-6 alkenyl group or by a C 1-6 alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C 1-6 alkyl, C 1-6 alkoxy or halogen, or aryl or heteroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C 1-6 alkyl, C 1-6 alkoxy, hydroxy, halogen, trifluoromethyl, nitro, cyano, C 1-12 carboxylic acyl, or amino or aminocarbonyl optionally substituted by one or two C 1-6 alkyl groups and R 6 is hydrogen or C 1-6 alkyl, or R 5 and R 6 together are-CH 2 -(CH 2 ) n -Z-(CH) m - wherein m and n are 0 to 2 such that m + n is 1 or 2 and Z is CH 2 , 0, S or NR wherein R is hyydrogen, C 1-9 alkyl, C 2-7 alkanoyl, phenyl C 1-4 -alkyl, naphthylcarbonyl, phenylcarbonyl or benzylcarbonyl optionally substituted in the phenyl or naphthyl ring by one or two of C 1-6 alkyl, C 1-6 alkoxy or halogen; mono- or bi-cyclic- heteroarylcarbonyl; X is oxygen or sulphur; Y and Q are electron withdrawing groups; and the nitrogen-containing group in the 4-position being trans to the R 3 group when R 3 is hydroxy, C 1-6 alkoxy or C 1-7 acyloxy; having blood pressure lowering activity, a process and intermediates for their preparation and their use as pharmaceuticals.