公开(公告)号：EP0212260A1

公开(公告)日：1987-03-04

申请号：EP86109786.3

申请日：1986-07-16

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： Araki, Kazuhiko ,  Uemori, Satoru ,  Kuroda, Tsuyoshi ,  Moriguchi, Akihiko

IPC分类号： C07D499/68 ,  C07D499/14

CPC分类号： C07D499/00

摘要： A process for preparing a stable Bacampicillin 6β-halopenicillanate which comprises reacting Bacampicillin hydrochloride with an alkali metal salt or an amine salt of 6β-halopenicillanic acid under heating. The salt produced by the method of the present invention is remarkably stable against coloration and thermal decomposition in the long term storage.

摘要翻译： 制备稳定的卡泊菌素6β-卤代青霉烷酸的方法，其包括在加热下使卡泊舒林盐酸盐与6β-卤代青霉烷酸的碱金属盐或胺盐反应。 通过本发明的方法生产的盐对于长期储存中的着色和热分解是非常稳定的。

公开(公告)号：EP0311948A3

公开(公告)日：1990-05-09

申请号：EP88116770.4

申请日：1988-10-10

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： Araki, Kazuhiko ,  Kuroda, Tsuyoshi ,  Uemori, Satoru ,  Moriguchi, Akihiko ,  Ikeda, Yoshifumi

IPC分类号： C07D413/04 ,  A61K31/535

CPC分类号： C07D413/04

摘要： A quinolonecarboxylic acid compound of the formula I
wherein R¹ is an alkyl group, a cycloalkyl group, a haloalkyl group, an alkenyl group, mono- or di-alkylamino groups, a phenyl group or a substituted phenyl group by one to three substituents selected from the group consisting of a halogen atom, an alkyl group, an alkoxy group, a hydroxy group, a nitro group or an amino group, R² is a hydrogen atom, an alkyl group, a cycloalkyl group, an acyl group or an alkoxy­carbonyl group, R³ is a hydrogen atom, an alkyl group or an aralkyl group, or R² and R³ together with the adjacent nitrogen atom form heterocyclic ring, R⁴ is a hydrogen atom or an alkyl group, R⁵ is a hydrogen atom, an alkyl group, an aralkyl group or an ester residue which is readily hydrolyzable in vivo, X is a hydrogen atom, a halogen atom or an alkyl group, n is integer of 1 to 3, and a salt thereof, and pharmaceutical use thereof. Said compounds exhibit antibacterial activities and are useful for the treatment of various infectious diseases.

公开(公告)号：EP0088903A2

公开(公告)日：1983-09-21

申请号：EP83101513.6

申请日：1983-02-17

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： Araki, Kazuhiko ,  Ao, Hideki ,  Inui, Jun ,  Aihara, Ken-ichi

IPC分类号： C07D211/90 ,  C07D405/12 ,  C07D405/04 ,  C07D409/12 ,  C07D409/04 ,  C07D409/14 ,  A61K31/455 ,  A61K31/38

CPC分类号： C07D213/89 ,  C07D211/90 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D491/10

摘要： 1,4-Dihydropyridine-3,5-dicarboxylic acid ester derivatives of the general formula:
or acid addition salts thereof, wherein W is -CH= or -N=; Y is -CH= CH -, -0-, -S-, -CH=N(O)p- (p is zero or 1) or -N(R)- (R is hydrogen or lower alkyl); X 1 , X 2 and X 3 are the same or different, and are each hydrogen, halogen, nitro, trifluoromethyl, cyano or lower alkylthio; Z is aryl or 5- or 6-membered aromatic heterocyclic ring (which may have a substituent or two or three substituents which may be the same or different, and the substituent may be halogen, lower alkyl, lower alkoxy, lower alkanoylamino, cyano, nitro, lower alkylthio, trifluoromethyl, sulfamoyl, di-lower alkylsulfamoyl, amino or di-lower alkylamino); -N A is 5- to 7-membered heterocyclic ring which may have nitrogen atom, oxygen atom, sulfur atom or unsaturated bond on the ring, and may be substituted by lower alkyl, lower alkoxycarbonyl, lower alkanoylamino, ethylenedioxy or ―(CH 2 ) m ―OR 4 (R 4 is hydrogen, lower alkyl or lower alkanoyl and m is 0, 1 or 2); R' and R 2 are the same or different, and are eaah lower alkyl; R 3 is lower alkyl, aralkyl, heteroaralkyl; and n is an integer 1 to 5. Such compounds are useful as antihypertensive agents and as therapeutic agents for cardiac and cerebral circulation disorders.

公开(公告)号：EP0088903B1

公开(公告)日：1988-11-23

申请号：EP83101513.6

申请日：1983-02-17

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： Araki, Kazuhiko ,  Ao, Hideki ,  Inui, Jun ,  Aihara, Ken-ichi

IPC分类号： C07D211/90 ,  C07D405/12 ,  C07D405/04 ,  C07D409/12 ,  C07D409/04 ,  C07D409/14 ,  A61K31/455 ,  A61K31/38

CPC分类号： C07D213/89 ,  C07D211/90 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D491/10

公开(公告)号：EP0217142A3

公开(公告)日：1988-01-07

申请号：EP86111938

申请日：1986-08-28

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： Tsuda, Yoshinao ,  Mishina, Tadashi ,  Obata, Minoru ,  Araki, Kazuhiko ,  Inui, Jun ,  Nakamura, Tadao

IPC分类号： C07D487/04 ,  A61K31/505 ,  C07D239/00 ,  C07D231/00 ,  C07D235/00 ,  C07D249/00

CPC分类号： C07D487/04

摘要： A polyazaheterocycle compound of the formula:
or a pharmaceutically acceptable salt thereof, wherein each symbol is as defined in the specification. Said compounds exhibit calcium antagonistic and or calcium agonistic activities

公开(公告)号：EP0328700A1

公开(公告)日：1989-08-23

申请号：EP88102251.1

申请日：1988-02-17

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： Tsuda, Yoshinao ,  Mishina, Tadashi ,  Obata, Minoru ,  Araki, Kazuhiko ,  Inui, Jun ,  Nakamura, Tadao

IPC分类号： C07D487/04 ,  A61K31/505

CPC分类号： C07D487/04

摘要： Isopropyl 5-(2-aminoethoxymethyl)-3-cyano-7-(2,3-­difluorophenyl)-4,7-dihydropyrazolo[1,5-a]pyrimidine-6-­carboxylate or pharmaceutically acceptable acid addition salt and/or hydrate thereof is disclosed.
Such compound has specifically mild and long lasting hypotensive activity and higher bioavailability by the oral administration.

摘要翻译： -3-（2-氨基乙氧基甲基）-3-氰基-7-（2,3-二氟苯基）-4,7-二氢吡唑并[1,5-a]嘧啶-6-羧酸异丙酯或其药学上可接受的酸加成盐和/或 公开了其水合物。 这种化合物通过口服给药具有特别温和和持久的低血压活性和较高的生物利用度。

公开(公告)号：EP0217142A2

公开(公告)日：1987-04-08

申请号：EP86111938.6

申请日：1986-08-28

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： Tsuda, Yoshinao ,  Mishina, Tadashi ,  Obata, Minoru ,  Araki, Kazuhiko ,  Inui, Jun ,  Nakamura, Tadao

IPC分类号： C07D487/04 ,  A61K31/505

CPC分类号： C07D487/04

摘要： A polyazaheterocycle compound of the formula:
or a pharmaceutically acceptable salt thereof, wherein each symbol is as defined in the specification.
Said compounds exhibit calcium antagonistic and or calcium agonistic activities

摘要翻译： 下式的聚氮杂环化合物：或其药学上可接受的盐，其中每个符号如说明书中所定义。 所述化合物表现出钙拮抗活性或钙激动活性

公开(公告)号：EP0088903A3

公开(公告)日：1984-11-28

申请号：EP83101513

申请日：1983-02-17

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： Araki, Kazuhiko ,  Ao, Hideki ,  Inui, Jun ,  Aihara, Ken-ichi

IPC分类号： C07D211/90 ,  C07D405/12 ,  C07D405/04 ,  C07D409/12 ,  C07D409/04 ,  C07D409/14 ,  A61K31/455 ,  A61K31/38

CPC分类号： C07D213/89 ,  C07D211/90 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D491/10

摘要： 1,4-Dihydropyridine-3,5-dicarboxylic acid ester derivatives of the general formula:
or acid addition salts thereof, wherein W is -CH= or -N=; Y is -CH= CH -, -0-, -S-, -CH=N(O)p- (p is zero or 1) or -N(R)- (R is hydrogen or lower alkyl); X 1 , X 2 and X 3 are the same or different, and are each hydrogen, halogen, nitro, trifluoromethyl, cyano or lower alkylthio; Z is aryl or 5- or 6-membered aromatic heterocyclic ring (which may have a substituent or two or three substituents which may be the same or different, and the substituent may be halogen, lower alkyl, lower alkoxy, lower alkanoylamino, cyano, nitro, lower alkylthio, trifluoromethyl, sulfamoyl, di-lower alkylsulfamoyl, amino or di-lower alkylamino); -N A is 5- to 7-membered heterocyclic ring which may have nitrogen atom, oxygen atom, sulfur atom or unsaturated bond on the ring, and may be substituted by lower alkyl, lower alkoxycarbonyl, lower alkanoylamino, ethylenedioxy or ―(CH 2 ) m ―OR 4 (R 4 is hydrogen, lower alkyl or lower alkanoyl and m is 0, 1 or 2); R' and R 2 are the same or different, and are eaah lower alkyl; R 3 is lower alkyl, aralkyl, heteroaralkyl; and n is an integer 1 to 5. Such compounds are useful as antihypertensive agents and as therapeutic agents for cardiac and cerebral circulation disorders.

公开(公告)号：EP0311948A2

公开(公告)日：1989-04-19

申请号：EP88116770.4

申请日：1988-10-10

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： Araki, Kazuhiko ,  Kuroda, Tsuyoshi ,  Uemori, Satoru ,  Moriguchi, Akihiko ,  Ikeda, Yoshifumi

IPC分类号： C07D413/04 ,  A61K31/535

CPC分类号： C07D413/04

摘要： A quinolonecarboxylic acid compound of the formula I
wherein R¹ is an alkyl group, a cycloalkyl group, a haloalkyl group, an alkenyl group, mono- or di-alkylamino groups, a phenyl group or a substituted phenyl group by one to three substituents selected from the group consisting of a halogen atom, an alkyl group, an alkoxy group, a hydroxy group, a nitro group or an amino group, R² is a hydrogen atom, an alkyl group, a cycloalkyl group, an acyl group or an alkoxy­carbonyl group, R³ is a hydrogen atom, an alkyl group or an aralkyl group, or R² and R³ together with the adjacent nitrogen atom form heterocyclic ring, R⁴ is a hydrogen atom or an alkyl group, R⁵ is a hydrogen atom, an alkyl group, an aralkyl group or an ester residue which is readily hydrolyzable in vivo, X is a hydrogen atom, a halogen atom or an alkyl group, n is integer of 1 to 3, and a salt thereof, and pharmaceutical use thereof.
Said compounds exhibit antibacterial activities and are useful for the treatment of various infectious diseases.

摘要翻译： 其中R 1为烷基，环烷基，卤代烷基，链烯基，单 - 或二 - 烷基氨基，苯基或取代的苯基的喹啉酮羧酸化合物，其中R 1为 一至三个选自卤素原子，烷基，烷氧基，羟基，硝基或氨基的取代基，R 2是氢原子，烷基，环烷基 ，酰基或烷氧基羰基，R 3是氢原子，烷基或芳烷基，或R 2和R 3与相邻的氮原子一起形成杂环，R 4， 是氢原子或烷基，R 5是氢原子，烷基，芳烷基或在体内容易水解的酯残基，X是氢原子，卤素原子或烷基， n为1〜3的整数，及其盐及其药物用途。 所述化合物表现出抗菌活性，可用于治疗各种感染性疾病。

公开(公告)号：EP0068171B1

公开(公告)日：1985-10-09

申请号：EP82104885.7

申请日：1982-06-03

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： Araki, Kazuhiko ,  Ao, Hideki ,  Kimura, Tomohiko ,  Aihara, Kenichi

IPC分类号： C07D401/12 ,  C07D407/12 ,  C07D409/12 ,  A61K31/445

CPC分类号： C07D401/12 ,  C07D307/52 ,  C07D333/20 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12