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1. 发明授权

US4390536A Piperidine derivatives 失效
公开(公告)号：US4390536A
公开(公告)日：1983-06-28
申请号：US352762
申请日：1982-02-26
申请人： Masayuki Teranishi , Hiroyuki Obase , Haruki Takai , Kazuhiro Kubo , Yutaka Kasuya
发明人： Masayuki Teranishi , Hiroyuki Obase , Haruki Takai , Kazuhiro Kubo , Yutaka Kasuya
IPC分类号： C07D211/58 , C07D417/04 , A61K31/54
CPC分类号： C07D211/58
摘要： New piperidine derivatives which have a useful pharmacological activity such as hypotensive activity are prepared.

2. 发明授权

US4344945A Piperidine derivatives 失效
标题翻译：哌啶衍生物
公开(公告)号：US4344945A
公开(公告)日：1982-08-17
申请号：US241727
申请日：1981-03-09
申请人： Masayuki Teranishi , Hiroyuki Obase , Haruki Takai , Kazuhiro Kubo , Yutaka Kasuya
发明人： Masayuki Teranishi , Hiroyuki Obase , Haruki Takai , Kazuhiro Kubo , Yutaka Kasuya
IPC分类号： C07D211/58 , C07D413/04 , A61K31/445 , A61K31/535 , C07D498/14
CPC分类号： C07D211/58
摘要： New piperidine derivatives which have a useful pharmacological activity such as hypotensive activity are prepared.
摘要翻译：制备具有有用药理活性如降血压活性的新的哌啶衍生物。

3. 发明授权

US4410528A Hypotensive piperidine derivatives 失效
标题翻译：低血压哌啶衍生物
公开(公告)号：US4410528A
公开(公告)日：1983-10-18
申请号：US264810
申请日：1981-05-18
申请人： Masayuki Teranishi , Hiroyuki Obase , Nobuhiro Nakamizo , Kazuhiro Kubo , Yutaka Kasuya
发明人： Masayuki Teranishi , Hiroyuki Obase , Nobuhiro Nakamizo , Kazuhiro Kubo , Yutaka Kasuya
IPC分类号： C07D211/58 , A61K31/505 , C07D401/04
CPC分类号： C07D211/58
摘要： A new piperidine derivative represented by the formula: ##STR1## wherein X is oxygen, sulfur, carbonyl, hydroxymethylene or methylene; R.sub.1 is straight-chain alkylene having 1-4 carbon atoms with or without lower alkyl substituent(s); (A).sub.m and R.sub.2 are usually used substituents; and Y is a monovalent group or a divalent group and is one of the following three groups: ##STR2## wherein when p is 0, B is --N.dbd.N--, ##STR3## and when p is 1, B is ##STR4## wherein (R.sub.3).sub.n is a usually used substituent, has hypotensive activity.
摘要翻译：由下式表示的新的哌啶衍生物：其中X是氧，硫，羰基，羟基亚甲基或亚甲基; R1是具有或不具有低级烷基取代基的具有1-4个碳原子的直链亚烷基; （A）m和R 2通常是取代基; （1）其中当p为0时，B为-N = N-，，当p为1时，B为（3）其中（R3）n是通常使用的取代基，具有降血压作用。

4. 发明授权

US4446141A Hypotensive piperidine derivatives 失效
标题翻译：低血压哌啶衍生物
公开(公告)号：US4446141A
公开(公告)日：1984-05-01
申请号：US191339
申请日：1980-02-02
申请人： Nobuhiro Nakamizo , Hiroyuki Obase , Kazuhiro Kubo , Yutaka Kasuya
发明人： Nobuhiro Nakamizo , Hiroyuki Obase , Kazuhiro Kubo , Yutaka Kasuya
IPC分类号： A61K31/41 , A61P9/12 , C07D401/04 , C07D405/14 , A61K31/445
CPC分类号： C07D401/04 , C07D405/14
摘要： The present invention relates to a novel compound represented by the general formula: ##STR1## wherein Ar represents a naphthyl, phenyl or substituted phenyl group, Q represents ##STR2## wherein R.sub.1 represents a hydrogen atom, or an alkyl, alkanoyl or alkoxycarbonyl group, R represents a hydrogen atom or an alkyl group, and Z represents a substituted benzimidazolinyl group; the broken line in piperidine ring means that 3,4-positions in the piperidine ring are saturated or form a double bond. Said compound and the pharmaceutically acceptable acid addition salts thereof have a hypotensive action and therefore are useful as medicine.
摘要翻译： PCT No.PCT / JP79 / 00141 Sec。 371日期1980年2月2日 102（e）日期1980年1月31日PCT申请日1979年6月1日PCT公布。出版物WO80 / 1980年1月10日。本发明涉及以下通式表示的新化合物：其中Ar表示萘基，苯基或取代苯基，Q表示其中R1表示氢原子，或烷基，烷酰基或烷氧基羰基，R表示氢原子或烷基，Z表示取代的苯并咪唑啉基; 哌啶环中的虚线表示哌啶环中的3,4-位饱和或形成双键。所述化合物及其药学上可接受的酸加成盐具有降血压作用，因此可用作药物。

5. 发明授权

US4147799A Process for reducing blood pressure and blocking .beta.-adrenergic receptor 失效
标题翻译：减少血压和阻止{62-肾上腺素能受体的方法
公开(公告)号：US4147799A
公开(公告)日：1979-04-03
申请号：US463833
申请日：1974-04-24
申请人： Hiroyuki Obase , Yutaka Kasuya
发明人： Hiroyuki Obase , Yutaka Kasuya
IPC分类号： C07D317/58 , A61K31/36
CPC分类号： C07D317/58
摘要： Ethanolamine derivatives and their acid addition salts are prepared (1) by reacting a 1-(3,4-methylenedioxyphenyl)-2-aminoethanol compound or an .alpha.-amino-(3,4-methylenedioxy)acetophenone compound with an alkanal or an alkanone under reduction conditions, (2) by hydrogenating and/or hydrogenolyzing a 1-(3,4-methylenedioxyphenyl)-2-(N-substituted amino)-ethanol compound or an .alpha.-(N-substituted amino)-(3,4-methylenedioxy)acetophenone compound, and (3) by reacting a (3,4-methylenedioxyphenyl)-ethylene oxide compound or a 1-(3,4-methylenedioxyphenyl)-2-substituted ethanol compound with an amine. The ethanolamine derivatives and their salts show .beta.-adrenergic receptor blocking activity, and are expected to be useful in the treatment of heart disease, hypertension, myocardites and pheochromocytoma.
摘要翻译：通过使1-（3,4-亚甲二氧基苯基）-2-氨基乙醇化合物或α-氨基 - （3,4-亚甲二氧基）苯乙酮化合物与链烷醛或烷酮反应制备乙醇胺衍生物及其酸加成盐（1）在还原条件下，（2）通过氢化和/或氢解1-（3,4-亚甲二氧基苯基）-2-（N-取代的氨基） - 乙醇化合物或α-（N-取代的氨基） - （3,4 - 亚甲二氧基）苯乙酮化合物，和（3）使（3,4-亚甲二氧基苯基） - 二氧化乙烯化合物或1-（3,4-亚甲二氧基苯基）-2-取代的乙醇化合物与胺反应。乙醇胺衍生物及其盐显示β-肾上腺素能受体阻断活性，预计可用于治疗心脏病，高血压，心肌和嗜铬细胞瘤。

6. 发明授权

US5302602A Tricyclic thromboxane A.sub.2 antagonists 失效
标题翻译：三环血栓素A2拮抗剂
公开(公告)号：US5302602A
公开(公告)日：1994-04-12
申请号：US884208
申请日：1992-05-18
申请人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii , Hidee Ishii , Kenji Ohmori
发明人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii , Hidee Ishii , Kenji Ohmori
IPC分类号： C07D211/14 , C07D313/12 , C07D333/34 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D471/10 , A61K31/445 , C07D211/22
CPC分类号： C07D405/06 , C07D211/14 , C07D313/12 , C07D333/34 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D471/10
摘要： Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
摘要翻译：具有由式（I）表示的TXA2拮抗活性的新型三环化合物：具有对血栓素A2的有效拮抗作用，还具有抗过敏和/或抗组胺活性，并且预期对缺血性疾病具有预防和治疗作用脑血管疾病等

7. 发明授权

US5143922A Tricyclic thromboxane A.sub.2 antagonists 失效
标题翻译：三环血栓素A2拮抗剂
公开(公告)号：US5143922A
公开(公告)日：1992-09-01
申请号：US616095
申请日：1990-11-20
申请人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii , Hidee Ishii , Kenji Ohmori
发明人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii , Hidee Ishii , Kenji Ohmori
IPC分类号： C07D211/14 , C07D313/12 , C07D333/34 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D471/10
CPC分类号： C07D405/06 , C07D211/14 , C07D313/12 , C07D333/34 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D471/10
摘要： Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic acitvity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
摘要翻译：具有由式（I）表示的TXA2拮抗活性的新型三环化合物：对抗凝血恶烷A2具有有效的拮抗作用，并且还具有抗过敏和/或抗组胺活性，并且预期对缺血性具有预防和治疗作用疾病，脑血管疾病等

8. 发明授权

US5010087A Tricyclic compounds and TXA.sub.2 antagonistic compositions thereof 失效
标题翻译：三环化合物和TXA2拮抗组合物
公开(公告)号：US5010087A
公开(公告)日：1991-04-23
申请号：US381330
申请日：1989-07-18
申请人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii
发明人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii
IPC分类号： C07C311/16 , C07C323/44 , C07C323/48 , C07C323/49 , C07D313/12 , C07D337/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D495/04
CPC分类号： C07D405/12 , C07C311/16 , C07C323/44 , C07C323/48 , C07C323/49 , C07D313/12 , C07D337/12 , C07D407/12 , C07D409/12 , C07D495/04 , C07C2103/32
摘要： Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formula (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.

9. 发明授权

US4999363A Tricyclic compounds 失效
公开(公告)号：US4999363A
公开(公告)日：1991-03-12
申请号：US368242
申请日：1989-06-06
申请人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii
发明人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii
IPC分类号： A61K31/19 , A61K31/00 , A61K31/41 , A61K31/415 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/505 , A61P7/02 , A61P9/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C57/46 , C07C59/13 , C07C63/49 , C07C65/26 , C07C67/00 , C07C229/50 , C07C233/52 , C07C233/81 , C07C235/14 , C07C235/40 , C07C235/54 , C07C235/62 , C07C235/78 , C07C235/82 , C07C235/84 , C07C237/04 , C07C237/24 , C07C237/38 , C07C241/00 , C07C251/20 , C07C317/44 , C07C323/61 , C07D235/06 , C07D313/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D491/056 , C07D521/00
CPC分类号： C07D235/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D313/12 , C07D405/12 , C07D417/12 , C07D471/04 , Y10S514/824 , Y10S514/826
摘要： Novel tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting activity and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.

10. 发明授权

US5478835A Tricyclic compounds and intermediates thereof 失效
标题翻译：三环化合物及其中间体
公开(公告)号：US5478835A
公开(公告)日：1995-12-26
申请号：US236097
申请日：1994-05-02
申请人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo
发明人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo
IPC分类号： A61K31/335 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/215 , A61K31/235 , A61K31/275 , A61K31/38 , A61K31/435 , A61K31/44 , A61K31/55 , A61P3/06 , A61P9/10 , A61P43/00 , C07C233/65 , C07C235/46 , C07C235/48 , C07C237/40 , C07C323/40 , C07C323/62 , C07C327/26 , C07C331/08 , C07D221/16 , C07D223/20 , C07D233/58 , C07D313/12 , C07D337/12 , C07D471/04 , C07D491/04 , C07D491/044 , C07D495/04 , C07C207/00 , C07C237/00
CPC分类号： C07D491/04 , C07C233/65 , C07D223/20 , C07D313/12 , C07D337/12 , C07C2103/32 , Y10S514/824
摘要： Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.
摘要翻译：公开了由式（I）表示的三环化合物：其中R 1，R 2，R 3和R 4各自独立地表示氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基， C 1-6烷基氨基，卤代C 1-6烷基，卤代C 1-6烷氧基，卤素，硝基，氰基，羧基，C 1-6烷氧基羰基，羟甲基，CR 9 R 10 CO 2 R 11（其中R 9，R 10和R 11各自独立地表示氢或C 1-6烷基）或CONR 12 R 13（其中R 12和R 13各自独立地表示氢或C 1-6 - 烷基）; R5表示氢或C1-6烷基; R 6，R 7和R 8各自独立地表示氢，C 1-6烷基，羟基，C 1-6烷氧基，C 1-6烷酰氧基，C 1-6烷硫基，氰硫基或卤素; X表示CH或N; Y1-Y2表示CH2-O，CH2-S（O）n，（其中n表示0,1或2），CH2CH2，CH = CH或CON（R14）（其中R14表示氢或C1-6烷基） Z表示氧或硫，或其药学上可接受的盐。该化合物具有酰基辅酶A：胆固醇酰基转移酶抑制活性，因此预期对高脂血症和动脉硬化具有预防和治疗作用。

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