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1. 发明授权

US5498627A Octahydro-2-naphthalenecarboxylic acid derivative, its production and use 失效
标题翻译：八氢-2-萘甲酸衍生物，其生产和使用
公开(公告)号：US5498627A
公开(公告)日：1996-03-12
申请号：US421921
申请日：1995-04-14
申请人： Takafumi Ishii , Tsuneaki Hida , Yukimasa Nozaki , Koichiro Ootsu
发明人： Takafumi Ishii , Tsuneaki Hida , Yukimasa Nozaki , Koichiro Ootsu
IPC分类号： C07D207/40 , C12P17/10 , A61K31/40 , C07D207/24
CPC分类号： C07D207/40 , C12P17/10 , C12R1/645
摘要： This invention provides a novel compound TAN-1813 having farnesyltransferase-inhibitory, cell growth-inhibitory, and anti-tumor activities; its production; farnesyltransferase-inhibiting agent; anti-tumor agent; pharmaceutical composition comprising a compound TAN-1813; and a novel microorganism capable of producing said compound.
摘要翻译：本发明提供具有法呢基转移酶抑制，细胞生长抑制和抗肿瘤活性的新型化合物TAN-1813; 其生产; 法呢基转移酶抑制剂; 抗肿瘤药; 包含化合物TAN-1813的药物组合物; 以及能够产生所述化合物的新型微生物。

2. 发明授权

US5459129A Condensed heterocyclic compounds, their production and use 失效
标题翻译：稠合杂环化合物，其生产和使用
公开(公告)号：US5459129A
公开(公告)日：1995-10-17
申请号：US112795
申请日：1993-08-27
申请人： Hiroshi Akimoto , Kazuyoshi Aso , Koichiro Ootsu
发明人： Hiroshi Akimoto , Kazuyoshi Aso , Koichiro Ootsu
IPC分类号： C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/08
CPC分类号： C07D487/04 , C07D491/04 , C07D495/04
摘要： A novel compound of the formula: ##STR1## wherein a ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent cyclic or chain group; either one of Q.sup.1 and Q.sup.2 stands for N and the other stands for N or CH; X stands for an amino group, hydroxyl group or mercapto group; Y stands for H, halogen atom or a group bonded through C, N, 0 or S; Z stands for a straight-chain divalent group having 2 to 5 atoms constituted of optionally substituted carbon atoms or constituted of optionally substituted carbon atoms and one optionally substituted hetero-atom; COOR.sup.1 and COOR.sup.2 independently stand for an optionally esterified carboxyl group; n denotes an integer of 2 to 6; and R.sup.1 may be different in each of n repeating units, or their salts and it is useful as a therapeutic drug for tumor in mammals.
摘要翻译：下式的新化合物：其中环A代表任选取代的5元环; B代表任选取代的二价环状或链状基团; Q1和Q2之一代表N，另一个代表N或CH; X代表氨基，羟基或巯基; Y代表H，卤素原子或通过C，N，O或S键合的基团; Z表示由任选取代的碳原子构成或由任选取代的碳原子和一个任选取代的杂原子构成的具有2至5个原子的直链二价基团; COOR1和COOR2独立地代表任选酯化的羧基; n表示2〜6的整数，并且R 1可以在n个重复单元或其盐中的每一个中不同，并且其可用作哺乳动物肿瘤的治疗药物。

3. 发明授权

US5250296A Immunostimulant agent containing interleukin-2 and 5'-deoxy-5-fluorouridine 失效
标题翻译：含有白细胞介素-2和5'-脱氧-5-氟尿苷的免疫刺激剂
公开(公告)号：US5250296A
公开(公告)日：1993-10-05
申请号：US800366
申请日：1991-11-27
申请人： Koichiro Ootsu
发明人： Koichiro Ootsu
IPC分类号： A61K38/20 , A61K39/39 , A61K37/02 , A61K45/05
CPC分类号： A61K39/39 , A61K38/2013 , A61K2039/55511 , A61K2039/55533
摘要： Disclosed is an immunostimulant agent containing interleukin-2 and 5'-deoxy-5-fluorouridine or a salt thereof in combination, which shows a strong therapeutic effect by synergistic action and weak side effects. The immunostimulant agent may further contain another chemotherapeutic agent and/or another immunotherapeutic agent.

4. 发明授权

US5403843A Pyrrolopyrimidinyalglutaminate derivatives and their use 失效
标题翻译：吡咯并嘧啶酰谷氨酸衍生物及其用途
公开(公告)号：US5403843A
公开(公告)日：1995-04-04
申请号：US926170
申请日：1992-08-07
申请人： Hiroshi Akimoto , Koichiro Ootsu , Fumio Itoh
发明人： Hiroshi Akimoto , Koichiro Ootsu , Fumio Itoh
IPC分类号： C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04 , A61K31/505
CPC分类号： C07D487/04 , C07D491/04 , C07D495/04
摘要： A condensed pyrimidine derivative of the formula (I): ##STR1## wherein the ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent 5- or 6-membered homo- or hetero-cyclic group; X stands for, among others, amino group; Y stands for, among others, hydrogen atom, halogen atom or amino group; Z stands for a divalent aliphatic group having five or less atoms forming straight chain, optionally having nitrogen, whose chain portion may optionally have a hetero-atom; W stands for, among others, --NH--CO-- or --CO--NH--; R.sup.1 stands for an optionally substituted cyclic or chain-like group; COOR.sup.2 stands for an optionally esterified carboxyl group; and p denotes an integer of 1 to 4, provided that when --W--R.sup.1 denotes a moiety represented by the formula: ##STR2## wherein COOR.sup.16 and COOR.sup.17 are, independently, an optionally esterified carboxyl group and n denotes an integer of 1 to 5, p denotes 1, 3 or 4, or a salt thereof, exhibiting highly specific toxicities to various tumor cells and excellent therapeutic effects on methotrexate-resistant tumor cells as well.
摘要翻译：式（I）的稠合嘧啶衍生物：其中环A代表任选取代的5元环; B代表任选取代的二价5-或6-元同 - 或杂 - 环基团; X代表氨基; Y代表氢原子，卤素原子或氨基; Z代表具有五个或更少个原子的二价脂族基，其形成直链，任选具有氮，其链部分可任选具有杂原子; W代表-NH-CO-或-CO-NH-; R1代表任选取代的环状或链状基团; COOR2代表任意酯化的羧基; 并且p表示1至4的整数，条件是当-W-R 1表示由下式表示的部分时：其中COOR 16和COOR 17独立地是任选酯化的羧基，n表示1至5的整数，p表示1,3或4或其盐，对各种肿瘤细胞具有高度特异性的毒性，并且对氨甲蝶呤抗性肿瘤细胞也具有优异的治疗作用。

5. 发明授权

US5268362A Condensed heterocyclic compounds, their production and use 失效
公开(公告)号：US5268362A
公开(公告)日：1993-12-07
申请号：US806893
申请日：1991-12-16
申请人： Hiroshi Akimoto , Kazuyoshi Aso , Koichiro Ootsu
发明人： Hiroshi Akimoto , Kazuyoshi Aso , Koichiro Ootsu
IPC分类号： C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04 , A61K37/02 , C07K5/06
CPC分类号： C07D487/04 , C07D491/04 , C07D495/04
摘要： A novel compound of the formula: ##STR1## wherein a ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent cyclic or chain group; either one of Q.sup.1 and Q.sup.2 stands for N and the other stands for N or CH; X stands for an amino group, hydroxyl group or mercapto group; Y stands for H, halogen atom or a group bonded through C, N, O or S; Z stands for a straight-chain divalent group having 2 to 5 atoms constituted of optionally substituted carbon atoms or constituted of optionally substituted carbon atoms and one optionally substituted hetero-atom; COOR.sup.1 and COOR.sup.2 independently stand for an optionally esterified carboxyl group; n denotes an integer of 2 to 6; and R.sup.1 may be different in each of n repeating units, or their salts and it is useful as a therapeutic drug for tumor in mammals.

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