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41.发明公开New lactyl tetrapeptide, processes for preparation thereof and pharmaceutical compositions containing it 失效乳酰四肽，其制备方法和含有药物组合物的过程。
公开(公告)号：EP0011283A1
公开(公告)日：1980-05-28
申请号：EP79104479.5
申请日：1979-11-14
发明人： Kitaura, Yoshihiko , Nakaguchi, Osamu , Hemmi, Keiji , Aratani, Matsuhiko , Takeno, Hidekazu , Okada, Satoshi , Tanaka, Hirokazu , Hashimoto, Masashi , Kuroda, Yoshio , Iguchi, Eiko , Kohsaka, Masanobu , Aoki, Hatsuo , Imanaka, Hiroshi
IPC分类号： C12P21/02 , C07C103/52 , A61K37/02
CPC分类号： C12R1/465 , A61K38/00 , C07K5/0215
摘要： A lactyl tetrapeptide of the formula
can be prepared by conventional peptide synthesis. One isomer, FR 900156, is obtained by cultivation of a suitable Streptomyces strain such as Str. violaceus ATCC 31481 or Str. olivaceogriseus ATCC 31427.
The invention also relates to a pharmaceutical composition comprising, as an effective ingredient, the above compound in association with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.摘要翻译： 式
的乳酰四肽可以通过常规的肽合成来制备。 一种异构体，FR 900156，通过合适的链霉菌属菌株的培养获得：如海峡菜ATCC 31481或STR Olivaceogriseus ATCC 31,427th因此，本发明涉及一种药物组合物，包括，作为有效成分，在关联的上述化合物用。 药学上可接受的，无毒的基本载体或赋形剂。 -
公开(公告)号：EP0596406B1
公开(公告)日：1998-12-16
申请号：EP93117474.2
申请日：1993-10-28
发明人： Oku, Teruo , Kayakiri, Hiroshi , Satoh, Shigeki , Abe, Yoshito , Sawada, Yuki , Tanaka, Hirokazu
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04
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公开(公告)号：EP0458207B1
公开(公告)日：1997-03-26
申请号：EP91108019.0
申请日：1991-05-17
发明人： Okada, Satoshi , Sawada, Kozo , Kayakiri, Natsuko , Saitoh, Yuki , Tanaka, Hirokazu , Hashimoto, Masashi
IPC分类号： C07D209/12 , C07D209/14 , C07D403/10 , C07D405/06 , C07D413/10 , C07D417/10 , A61K31/40
CPC分类号： C07D403/10 , C07D209/12 , C07D209/14 , C07D209/18 , C07D413/10 , C07D417/10 , Y02P20/55
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44.发明公开
公开(公告)号：EP0457195A3
公开(公告)日：1992-11-19
申请号：EP91107554.7
申请日：1991-05-09
发明人： Hemmi, Keiji , Neya, Masahiro , Fukami, Naoki , Hashimoto, Masashi , Tanaka, Hirokazu , Kayakiri, Natsuko
CPC分类号： C07K5/06156 , A61K38/00 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/0217 , C07K5/0808 , C07K5/101 , Y02P20/55
摘要： The present invention relates to peptide compound and a pharmaceutically acceptable salt thereof which have pharmacological activities such as endothelin antagonistic activity and the like, to processes for its preparation, to a pharmaceutical composition comprising the same, and to a method of using the same for manufacturing a medicament in the treatment and the prevention of endothelin mediated diseases such as hypertension, and the like.
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公开(公告)号：EP0458207A3
公开(公告)日：1992-03-25
申请号：EP91108019.0
申请日：1991-05-17
发明人： Okada, Satoshi , Sawada, Kozo , Kayakiri, Natsuko , Saitoh, Yuki , Tanaka, Hirokazu , Hashimoto, Masashi
IPC分类号： C07D209/12 , C07D209/14 , C07D403/10 , C07D405/06 , C07D413/10 , C07D417/10 , A61K31/40
CPC分类号： C07D403/10 , C07D209/12 , C07D209/14 , C07D209/18 , C07D413/10 , C07D417/10 , Y02P20/55
摘要： The present invention relates to novel indole derivatives and a pharmaceutically acceptable salt thereof which have pharmacological activities such as inhibitory activity on testosteron 5a-reductase and the like, to process for preparation thereof, to a pharmaceutical composition comprising the same and to a use of the same for manufacturing a medicament.
摘要翻译： 吲哚衍生物及其药学上可接受的盐本发明涉及对睾酮5α-还原酶等具有抑制活性等药理活性的新型吲哚衍生物及其药学上可接受的盐及其制备方法，含有该化合物的药物组合物及其用途 与制造药物相同。
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46.发明公开Peptides having endothelin antagonist activity, a process for preparation thereof and pharmaceutical compositions comprising the same 失效肽mit内皮素拮抗剂Aktivität，deren Herstellung und pharmazeutische Zusammensetzungen。
公开(公告)号：EP0457195A2
公开(公告)日：1991-11-21
申请号：EP91107554.7
申请日：1991-05-09
发明人： Hemmi, Keiji , Neya, Masahiro , Fukami, Naoki , Hashimoto, Masashi , Tanaka, Hirokazu , Kayakiri, Natsuko
CPC分类号： C07K5/06156 , A61K38/00 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/0217 , C07K5/0808 , C07K5/101 , Y02P20/55
摘要： The present invention relates to peptide compound and a pharmaceutically acceptable salt thereof which have pharmacological activities such as endothelin antagonistic activity and the like, to processes for its preparation, to a pharmaceutical composition comprising the same, and to a method of using the same for manufacturing a medicament in the treatment and the prevention of endothelin mediated diseases such as hypertension, and the like.
摘要翻译： 本发明涉及具有药理活性如内皮素拮抗活性等的肽化合物及其药学上可接受的盐，涉及其制备方法，涉及包含其的药物组合物及其制备方法 用于治疗和预防内皮素介导的疾病如高血压等的药物。
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47.发明公开Condensed imidazole derivatives and processes for preparation thereof 失效Kondensierte咪唑衍生物和Verfahren zu deren Herstellung。
公开(公告)号：EP0426021A1
公开(公告)日：1991-05-08
申请号：EP90120543.5
申请日：1990-10-26
发明人： Oku, Teruo , Setoi, Hiroyuki , Kayakiri, Hiroshi , Inoue, Takayuki , Kuroda, Akio , Katayama, Akira , Hashimoto, Masashi , Satoh, Sigeki , Tanaka, Hirokazu
IPC分类号： C07D471/04 , A61K31/44 , C07D487/04 , C07D473/00 , C07D473/40 , C07D403/10 , A61K31/52 , A61K31/505 , A61K31/415 , A61K31/495 , A61K31/50
CPC分类号： C07D403/10 , C07D471/04 , C07D473/00 , C07D473/40 , C07D487/04 , Y02P20/55
摘要： A compound of the formula :
wherein R¹ is lower alkyl, halo(lower)alkyl, cyclo(lower)alkyl or lower alkylthio,
R² is hydrogen or imino-protective group,
R³ is hydrogen or halogen,
A is lower alkylene, and
is a group of the formula :
in which
X¹, X², X³ and X⁴ are each
N or CR⁴, in which R⁴ is hydrogen, lower alkyl, lower alkoxy, halogen, halo(lower)alkyl, esterified carboxy, halo(lower)alkoxy or hydroxy,
provided that at least one of X¹, X², X³ and X⁴ is N,
and pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising them as an active ingredient in admixture with a pharmaceutically acceptable carrier or excipient.摘要翻译： 下式化合物：其中R 1为低级烷基，卤代（低级）烷基，环（低级）烷基或低级烷硫基，R 2为氢或亚氨基保护基，R 3为 氢或卤素，A是低级亚烷基，并且
是下式的基团：其中X 1，X 2，X 3和X 4各自为N或CR < 其中R 4为氢，低级烷基，低级烷氧基，卤素，卤代（低级）烷基，酯化羧基，卤代（低级）烷氧基或羟基，条件是X 1， 2，X 3和X 4为N及其药学上可接受的盐，其制备方法和药物组合物包含它们作为活性成分与药学上可接受的载体或赋形剂的混合物。 -
公开(公告)号：EP0367130A3
公开(公告)日：1991-03-13
申请号：EP89119959.8
申请日：1989-10-27
IPC分类号： C07D207/14 , C07D401/06 , C07D417/06 , C07D413/06 , C07D409/06 , C07D405/06 , C07D403/06 , A61K31/40 , A61K31/44 , A61K31/47 , A61K31/495
CPC分类号： C07D207/335 , C07D207/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： A compound of the formula :
wherein
R¹ is alkyl, ar(lower)alkyl which may have suitable substituent(s), or heterocyclic(lower)alkyl,
R² is hydrogen or an acyl group, and
R³ is carboxy(lower)alkyl, protected carboxy(lower)alkyl, carboxyaryl or protected carboxyaryl,
and a pharmaceutically acceptable salt thereof,
processes for their preparation and pharmaceutical compositions comprising them or a pharmaceutically acceptable salt thereof in admixture with pharmaceutically acceptable carriers.-
公开(公告)号：EP0289911A2
公开(公告)日：1988-11-09
申请号：EP88106637.7
申请日：1988-04-26
发明人： Setoi, Hiroyuki , Hirai, Hideo , Marusawa, Hiroshi , Kuroda, Akio , Tanaka, Hirokazu , Hashimoto, Masashi
IPC分类号： C07D207/14 , A61K31/40
CPC分类号： C07D207/16 , C07D207/12 , C07D207/14
摘要： A compound of the formula :
wherein
R¹ is hydrogen or an acyl group,
R² is an acyl group,
R³ is carboxy(lower)alkyl, lower alkyl substituted with carboxy and one or more halogen atom(s), protected carboxy(lower)alkyl, carboxyaryl, protected carboxyaryl, carboxy, protected carboxy, hydroxy(lower)alkyl, sulfino(lower)alkyl, phosphono(lower)alkyl, protected phosphono(lower)alkyl or halo(lower)alkyl,
R⁷ is hydrogen or lower alkyl, and
A is
(in which R⁸ is hydrogen or lower alkyl),
and a pharmaceutically acceptable salt thereof, processes for its preparation and pharmaceutical compositions comprising them. The invention also relates to intermediates of the formula
and process for production thereof.摘要翻译： 下式化合物：其中R 1为氢或酰基，R 2为酰基，R 3为羧基（低级）烷基，被羧基取代的低级烷基和一个或多个 卤素原子，保护的羧基（低级）烷基，羧基芳基，保护的羧基芳基，羧基，被保护的羧基，羟基（低级）烷基，亚磺酰基（低级）烷基，膦酰基（低级）烷基，被保护的膦酰基（低级）烷基或卤素 低级）烷基，R 7是氢或低级烷基，A是
（其中R 8是氢或低级烷基）及其可药用盐，其制备方法和包含它们的药物组合物 。 本发明还涉及式CHEM的中间体及其生产方法。 [R -
50.发明授权N-acyl peptide, processes for their preparation and pharmaceutical compostions thereof 失效N-乙酰基肽，其制备方法及其药物组合物
公开(公告)号：EP0085255B1
公开(公告)日：1986-09-10
申请号：EP82306928.1
申请日：1982-12-23
发明人： Umehara, Kazuyoshi , Yoshida, Keizo , Tanaka, Hirokazu , Uchida, Itsuo , Kohsaka, Masanobu , Imanaka, Hiroshi
CPC分类号： C07K5/06104 , A61K38/00 , C07K5/06052 , C07K5/06078 , C07K5/06086
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