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公开(公告)号:US5514701A
公开(公告)日:1996-05-07
申请号:US95350
申请日:1993-07-23
IPC分类号: C07D207/14 , C07D207/32 , C07D207/335 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D521/00 , A61K31/40
CPC分类号: C07D207/335 , C07D207/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , Y10S514/826
摘要: This invention relates to pyrrolidine derivatives and pharmaceutically acceptable salts, their pharmaceutical compositions, and methods of use as thromboxane A.sub.2 antagonists and/or thromboxane A.sub.2 synthetase inhibitors in the treatment of thrombotic diseases, asthma or nephritis, e.g. of the formula: ##STR1## wherein R.sup.1 is thienyl(lower)alkyl, furyl(lower)alkyl or pyrrolyl(lower)alkyl.
摘要翻译: 本发明涉及吡咯烷衍生物及其药学上可接受的盐,其药物组合物,以及作为血栓素A2拮抗剂和/或血栓素A2合成酶抑制剂用于治疗血栓性疾病,哮喘或肾炎的方法。 (低级)烷基或吡咯基(低级)烷基。
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公开(公告)号:US5130323A
公开(公告)日:1992-07-14
申请号:US421399
申请日:1989-10-13
IPC分类号: A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/495 , A61P1/04 , A61P9/00 , A61P9/10 , A61P29/00 , A61P37/08 , A61P43/00 , C07D207/14 , C07D207/32 , C07D207/335 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D521/00
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: The invention relates to pyrrolidine derivatives having thromboxane A.sub.2 antagonism and TXA.sub.2 synthetase-inhibitory activity, of the formula ##STR1## wherein R.sup.1 is pyridyl(lower)alkyl, R.sup.2 is an acyl group selected from the group consisting of lower alkanoyl, lower alkoxycarbonyl, lower alkylsulfonyl, phenylsulfonyl, benzoyl, phenyl(lower)alkanoyl, cyclo(lower)alkyl(lower)alkanoyl, phenyl(lower)alkoxycarbonyl and phenylcarbamoyl, each of which may have 1 to 3 substituent(s) selected from the group consisting of halogen, lower alkyl, lower alkoxy, nitro and mono(or di or tri)halo(lower)alkyl, andR.sup.3 is carboxy(lower)alkyl, protected carboxy(lower)alkyl, carboxyphenyl or protected carboxyphenyl,or a pharmaceutically acceptable salt thereof.
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公开(公告)号:US5264453A
公开(公告)日:1993-11-23
申请号:US843196
申请日:1992-02-28
IPC分类号: C07D207/14 , C07D207/32 , C07D207/335 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D521/00 , C07D207/10 , A61K31/40
CPC分类号: C07D207/335 , C07D207/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , Y10S514/826
摘要: This invention relates to pyrrolidine derivatives and pharmaceutically acceptable salts thereof of the structure ##STR1## where R.sup.1, R.sup.2, and R.sup.3 are as defined herein. These compounds are for pharmaceutical use in treating thrombotic diseases, asthma or nephritis.
摘要翻译: 本发明涉及其中R1,R2和R3如本文所定义的结构“IMAGE”的吡咯烷衍生物及其药学上可接受的盐。 这些化合物用于治疗血栓性疾病,哮喘或肾炎的药物。
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公开(公告)号:US4929639A
公开(公告)日:1990-05-29
申请号:US208665
申请日:1988-06-20
申请人: Hiroyuki Setoi , Akio Kuroda , Hirokazu Tanaka , Hideo Hirai , Hiroshi Marusawa , Masashi Hashimoto
发明人: Hiroyuki Setoi , Akio Kuroda , Hirokazu Tanaka , Hideo Hirai , Hiroshi Marusawa , Masashi Hashimoto
IPC分类号: A61K31/357 , A61P7/02 , C07D309/06 , C07D319/06 , C07D405/12 , C07D409/12
CPC分类号: C07D405/12 , C07D309/06 , C07D319/06 , C07D409/12
摘要: The invention relates to treatment of diseases caused by thromboxane A.sub.2 comprising administering a compound ##STR1## wherein R.sup.1 is hydrogen or lower alkyl,R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl andR.sup.3 is --CH.dbd.N--R.sup.4 in which R.sup.4 is arylureido or arylthioureido andX is --O--,or a pharmaceutically acceptable salt thereof.
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公开(公告)号:US4916152A
公开(公告)日:1990-04-10
申请号:US187240
申请日:1988-04-28
申请人: Hiroyuki Setoi , Hideo Hirai , Hiroshi Marusawa , Akio Kuroda , Hirokazu Tanaka , Masashi Hashimoto
发明人: Hiroyuki Setoi , Hideo Hirai , Hiroshi Marusawa , Akio Kuroda , Hirokazu Tanaka , Masashi Hashimoto
IPC分类号: A61K31/40 , A61K31/4025 , A61K31/66 , A61P7/00 , A61P7/02 , A61P11/00 , A61P13/02 , A61P15/00 , C07D207/12 , C07D207/14 , C07D207/16 , C07D409/12 , C07F9/572
CPC分类号: C07D207/16 , C07D207/12 , C07D207/14
摘要: The invention relates to novel compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkoxycarbonyl, phenylsulfonyl, phenylsulfonyl substituted with 1 to 3 substituent(s) selected from the group consisting of halogen, nitro, lower alkoxy, mono (or di or tri)halo(lower)alkyl and lower alkyl, phenylcarbamoyl, lower alkylsulfonyl, benzoyl or thienylsulfonyl;R.sup.2 is phenylsulfonyl or phenylsulfonyl substituted with 1 to 3 substituent(s) selected from the group consisting of halogen, lower alkyl, lower alkoxy and mono(or di or tri)halo(lower)alkyl,R.sup.3 is carboxy(lower)alkyl, lower alkyl substituted with carboxy and 1 to 3 halogen atom(s), esterified carboxy(lower)alkyl, carbamoyl(lower)alkyl, lower alkylsulfonylcarbamoyl(lower)alkyl, phenylsulfonylcarbamoyl(lower)alkyl, carboxyphenyl, esterified carboxyphenyl, carboxy, esterified carboxy, hydroxy(lower)alkyl, sulfino(lower)alkyl, phosphono(lower)alkyl, di(lower)alkoxyphosphoryl(lower)alkyl or halo(lower)alkyl,R.sup.7 is hydrogen or lower alkyl, andA is ##STR2## in which R.sup.8 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt thereof, useful as therapeutic agents for thrombosis, asthma and nephritis.
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公开(公告)号:US4743614A
公开(公告)日:1988-05-10
申请号:US859587
申请日:1986-03-04
IPC分类号: A61K38/00 , C07D207/20 , C07D233/54 , C07K5/072 , C12P13/00 , A61K31/165 , A61K31/195 , A61K31/405 , A61K31/415
CPC分类号: C07D233/64 , C07D207/20 , C07K5/06113 , C12P13/005 , C12P13/02 , C12P13/04 , C12R1/645 , A61K38/00
摘要: Novel compounds of the following formula have restorative pharmacological activities in immuno-deficient hosts, ##STR1## wherein R.sup.1 is amino or a protected amino group,R.sup.2 is hydrogen, carboxy or a protected carboxy group,R.sup.3 is hydrogen, carboxy or a protected carboxy group,R.sup.4 is lower alkyl, amino(lower)alkyl, protected amino(lower)alkyl, carbamoyl(lower)alkyl or protected carbamoyl(lower)alkyl,R.sup.5 is hydrogen or lower alkyl, andR.sup.6 is hydrogen, hydroxyphenyl(lower)alkyl, imidazolyl(lower)alkyl or indolyl(lower)alkyl.
摘要翻译: 下式的新化合物在免疫缺陷型宿主中具有恢复性药理学活性,其中R1是氨基或被保护的氨基,R2是氢,羧基或被保护的羧基,R3是氢,羧基或被保护的羧基 ,R4是低级烷基,氨基(低级)烷基,被保护的氨基(低级)烷基,氨基甲酰基(低级)烷基或被保护的氨基甲酰基(低级)烷基,R5是氢或低级烷基,R6是氢,羟基苯基(低级)烷基, 咪唑基(低级)烷基或吲哚基(低级)烷基。
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公开(公告)号:US5538950A
公开(公告)日:1996-07-23
申请号:US232156
申请日:1994-05-12
申请人: Keiji Hemmi , Masahiro Neya , Naoki Fukami , Masashi Hashimoto , Hirokazu Tanaka , Natsuko Kayakiri
发明人: Keiji Hemmi , Masahiro Neya , Naoki Fukami , Masashi Hashimoto , Hirokazu Tanaka , Natsuko Kayakiri
IPC分类号: A61K38/22 , A61K38/00 , A61P9/12 , C07K1/113 , C07K5/078 , C07K5/083 , C07K5/103 , C07K5/117 , C07K5/08
CPC分类号: C07K5/06156 , C07K5/0808 , C07K5/1005 , C07K5/1024 , A61K38/00
摘要: A compound of the formula: ##STR1## in which R.sup.3 is hydrogen or lower alkyl, R.sup.4 is pyridyl (lower) alkyl; andR.sup.1, R.sup.2, R.sup.5 and A are defined in the description;or a pharmaceutically acceptable salt thereof, which have endothelin antagonistic activity.
摘要翻译: PCT No.PCT / JP92 / 01405 Sec。 371日期:1994年5月12日 102(e)日期1994年5月12日PCT提交1992年10月30日PCT公布。 公开号WO93 / 10144 日期:1993年5月27日分子式为下式的化合物:其中R 3为氢或低级烷基,R 4为吡啶基(低级)烷基; 在说明书中定义了R1,R2,R5和A; 或其药学上可接受的盐,其具有内皮素拮抗活性。
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公开(公告)号:USRE32992E
公开(公告)日:1989-07-18
申请号:US611733
申请日:1984-05-18
申请人: Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka , Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto
发明人: Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka , Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto
CPC分类号: C07C243/00 , C07K5/0215 , C07K5/06026 , C07K5/06052 , C07K5/06069 , C07K5/06078 , C07K9/005 , C12R1/465 , A61K38/00 , Y02P20/55
摘要: The invention deals with novel peptides useful for the therapeutic treatment of infectious diseases caused by pathogenic microorganisms. Included is the peptide FR900156 having the structure: ##STR1## as well as the peptides of the structure ##STR2## wherein R.sup.1 is acyl;R.sub.b.sup.1 is hydrogen, methyl, isopropyl, hydroxymethyl, protected hydroxymethyl or benzyl;R.sup.2 is hydrogen, carboxy, protected carboxy, or a group of the formula: ##STR3## wherein R.sub.a.sup.2 is mono- or di-carboxy lower alkyl or ar(carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy,R.sub.b.sup.2 is hydrogen or lower alkyl;R.sup.p and R.sup.q are each hydrogen, carboxy, protected carboxy, with proviso that when one of R.sup.2 and R.sup.q is hydrogen, then the other is carboxy or protected carboxy;R.sup.r is hydrogen or amino protective group; m is an integer 1 to 3, and n is 1 .Iadd.provided that when R.sup.1 is benzyloxycarbonyl R.sub.5.sup.1 is methyl, m is an integer 2 and n is an integer 1, then R.sup.2 is not protected carboxy, and .Iaddend.provided that when R.sup.1 is .[.hydrogen,.]. t-butoxycarbonyl or N-acetylmuramyl, R.sub.b.sup.1 is methyl, m is an integer 2 and n is an integer 1, then R.sup.2 is hydrogen, protected carboxy or a group of the formula: ##STR4## wherein R.sub.a.sup.2 is mono- or di-carboxy lower alkyl having 1 and 3 to 6, carbon atoms, .[..alpha.-carboxyethyl,.]. .Iadd.--CH.sub.2 --CH.sub.2 --COOH, .Iaddend.ar(carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy and R.sub.b.sup.2 is as defined above, or its pharmaceutically acceptable salt.
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公开(公告)号:US4725582A
公开(公告)日:1988-02-16
申请号:US377836
申请日:1982-05-13
申请人: Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Takeno Hidekazu , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
发明人: Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Takeno Hidekazu , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
CPC分类号: C07C243/00 , C07K5/0215 , C07K5/06026 , C07K5/06052 , C07K5/06069 , C07K5/06078 , C07K9/005 , C12R1/465 , A61K38/00 , Y02P20/55
摘要: The invention concerns peptides, having the pharmaceutical property of enhancing the immune response, having the structure: ##STR1## wherein R.sup.1 is alkanoyl,R.sub.b.sup.1 is hydrogen, methyl, isopropyl, hydroxymethyl, protected hydroxymethyl or benzyl,R.sup.2 is hydrogen, carboxy, protected carboxy or a group of the formula: ##STR2## wherein R.sub.a.sup.2 is mono- or di-carboxy (or protected carboxy) lower alkyl or ar(carboxy or protected carboxy) lower alkyl whose aryl moiety is substituted by hydroxy or not substituted,R.sub.b.sup.2 is hydrogen or lower alkyl,R.sup.p is hydrogen, carboxy or protected carboxy,R.sup.q is carboxy, protected carboxy or a group of the formula ##STR3## wherein R.sub.a.sup.2 and R.sub.b.sup.2 are each as defined above, R.sup.r is hydrogen or amino protective group,m is an integer 1 to 3, andn is an integer 1.
摘要翻译: 本发明涉及具有以下结构的具有增强免疫应答的药学性质的肽:其中R 1是烷酰基,R 1b是氢,甲基,异丙基,羟甲基,被保护的羟甲基或苄基,R 2是氢,羧基,被保护的羧基 或下式的基团:其中R 2a是其芳基部分被羟基或未取代的单或二羧基(或保护的羧基)低级烷基或芳(羧基或被保护的羧基)低级烷基,R 2b是氢 或低级烷基,Rp是氢,羧基或受保护的羧基,Rq是羧基,被保护的羧基或下式的基团:其中Ra2和Rb2各自如上定义,Rr是氢或氨基保护基,m是整数 1〜3,n为整数1。
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公开(公告)号:US5430022A
公开(公告)日:1995-07-04
申请号:US86094
申请日:1993-07-06
申请人: Keiji Hemmi , Masahiro Neya , Naoki Fukami , Masashi Hashimoto , Hirokazu Tanaka , Natsuko Kayakiri
发明人: Keiji Hemmi , Masahiro Neya , Naoki Fukami , Masashi Hashimoto , Hirokazu Tanaka , Natsuko Kayakiri
IPC分类号: A61K38/00 , C07K5/02 , C07K5/078 , C07K5/083 , C07K5/103 , A61K38/06 , C07K1/02 , C07K1/06 , C07K5/08
CPC分类号: C07K5/06156 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/0217 , C07K5/0808 , C07K5/101 , A61K38/00
摘要: Peptide compounds of the formula (I') ##STR1## in which R.sup.1 is acyl,R.sup.2 is lower alkyl, cyclo(lower)alkyl(lower)alkyl or optionally substituted heterocyclic(lower)alkyl,R.sup.3 is optionally substituted heterocyclic(lower)alkyl or optionally substituted ar(lower)alkyl,R.sup.4 is lower alkyl, amino(lower)alkyl, protected amino(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl or optionally substituted heterocyclic(lower)alkyl,R.sup.5 is carboxy, protected carboxy, carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.6 is hydrogen, lower alkyl, C.sub.6-10 ar(lower)alkyl amino(lower)alkyl, protected amino(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl, or heterocyclic(lower)alkyl,R.sup.7 is hydrogen or lower alkyl, andA is --O--, --NH--, lower alkylimino or lower alkylene, or a pharmaceutically acceptable salt thereof are disclosed. The compounds can be used to treat and prevent endothelin mediated diseases such as hypertension. The preparation of such peptides is also disclosed.
摘要翻译: 式(I')的肽化合物其中R 1是酰基,R 2是低级烷基,环(低级)烷基(低级)烷基或任选取代的杂环(低级)烷基),其中R 1是任选取代的杂环 (低级)烷基或任选取代的芳(低级)烷基,R 4是低级烷基,氨基(低级)烷基,保护的氨基(低级)烷基,羧基 烷基,R 5为羧基,保护的羧基,羧基(低级)烷基或保护的羧基(低级)烷基,R6为氢,低级烷基,C6-10ar(低级)烷基氨基(低级)烷基,被保护的氨基 (低级)烷基,受保护的羧基(低级)烷基或杂环(低级)烷基,R7是氢或低级烷基,A是-O - , - NH-,低级烷基亚氨基或低级亚烷基或其药学上可接受的盐是 披露 该化合物可用于治疗和预防内皮素介导的疾病如高血压。 还公开了这种肽的制备。
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