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1. 发明授权

US4521417A Geranylgeranylacetamide compounds having a piperazine ring, salts thereof, pharmaceutical compositions containing said compounds, and method of treating ulcers in mammals 失效
标题翻译：具有哌嗪环的香叶基香叶基乙酰胺化合物，其盐，含有所述化合物的药物组合物，以及治疗哺乳动物溃疡的方法
公开(公告)号：US4521417A
公开(公告)日：1985-06-04
申请号：US501391
申请日：1983-06-06
申请人： Hiromasa Nakamoto , Michitaka Ogawa , Muneo Kobayashi , Yuki Nogami , Kazuo Kumamoto , Hiroko Murakami , Yoichi Ninagawa , Yoshiaki Omura , Masao Mizuno
发明人： Hiromasa Nakamoto , Michitaka Ogawa , Muneo Kobayashi , Yuki Nogami , Kazuo Kumamoto , Hiroko Murakami , Yoichi Ninagawa , Yoshiaki Omura , Masao Mizuno
IPC分类号： C07D295/18 , A61K31/495 , A61P1/04 , C07D295/185 , C07D241/04
CPC分类号： C07D295/185
摘要： A geranylgeranylacetamide compound having a piperazine ring represented by the following formula (I) ##STR1## wherein R represents a member selected from the class consisting of a hydrogen atom, C.sub.1 -C.sub.5 alkyl groups which are unsubstituted or mono-substituted by a halogen atom, C.sub.2 -C.sub.5 alkenyl groups and C.sub.7 -C.sub.8 aralkyl groups, R.sub.1 represents a C.sub.1 -C.sub.3 alkyl group, and n represents 0, 1 or 2,and a pharmaceutically acceptable acid addition salt thereof. The aforesaid compound can be prepared by reacting geranylgeranylacetic acid or its reactive derivative with a piperazine compound, and thereafter, if desired, transforming the free geranylgeranylacetamide compound thus obtained into its pharmaceutically acceptable acid addition salt. A pharmaceutical composition containing said compound exhibits antiulcerogenic activity, particularly excellent antipeptic ulcerogenic activity, and is useful as an agent for treating ulcers.
摘要翻译：具有下式（I）表示的哌嗪环的香叶基香叶基乙酰胺化合物其中R表示选自氢原子，未被取代或未被单取代的C 1 -C 5烷基的成员卤素原子，C 2 -C 5烯基和C 7 -C 8芳烷基，R 1表示C 1 -C 3烷基，n表示0,1或2，以及其药学上可接受的酸加成盐。上述化合物可以通过将香叶基香叶基香叶基乙酸或其活性衍生物与哌嗪化合物反应制备，然后如果需要，将由此获得的游离er牛儿基ger牛儿基乙酰胺化合物转化为其药学上可接受的酸加成盐。含有所述化合物的药物组合物具有抗溃疡活性，特别优异的消毒性溃疡发生活性，可用作治疗溃疡的药剂。

2. 发明授权

US4082744A 4-Benzazonine derivatives and process for preparation thereof 失效
标题翻译： 4-苯并噻吩衍生物及其制备方法
公开(公告)号：US4082744A
公开(公告)日：1978-04-04
申请号：US707276
申请日：1976-07-21
申请人： Masao Ikeda , Shigeo Miyamoto , Thutomu Nozawa , Akira Kurobe , Osamu Futsukaichi
发明人： Masao Ikeda , Shigeo Miyamoto , Thutomu Nozawa , Akira Kurobe , Osamu Futsukaichi
IPC分类号： C07D223/14 , C07D225/06 , C07D225/08
CPC分类号： C07D223/14 , C07D225/06 , Y10S514/849
摘要： Novel 4-benzazonine derivatives and their salts, and processes for the preparation thereof are disclosed. These 4-benzazonine derivatives are represented by the following general formula: ##STR1## wherein R stands for --H, --OH or a lower alkoxy group such as --OCH.sub.3, R.sub.1 designates --H or a lower alkyl group such as --CH.sub.3 and --CH.sub.2 CH.sub.3, R.sub.2 indicates --H or a lower alkyl group such as --CH.sub.3, R.sub.3 stands for --H, a linear or branched, saturated or unsaturated alkyl group having 1 to 4 carbon atoms, a mono- or di-hydroxy lower alkyl group such as --CH.sub.2 OH and ##STR2## a saturated cyclic hydrocarbon group having 3 to 6 carbon atoms or a substituted or unsubstituted aromatic hydrocarbon group having 6 to 8 carbon atoms, and R.sub.4 designates --H, --OH or .dbd. 0. These compounds have medicinal effects, especially therapeutic activities on the central nervous system, such as analgesic, antitussive and sedative activities.

3. 发明授权

US5321041A Diphenylpyrrolylfuran derivatives 失效
标题翻译：二苯基吡咯衍生物
公开(公告)号：US5321041A
公开(公告)日：1994-06-14
申请号：US140514
申请日：1993-10-25
申请人： Jun Adachi , Mitsugu Ishida , Toshietsu Taniguchi , Yuichi Kato , Toshiyuki Kawagoshi , Tomoaki Tamura , Tetsuo Kadozaki , Tetsuo Miyamoto
发明人： Jun Adachi , Mitsugu Ishida , Toshietsu Taniguchi , Yuichi Kato , Toshiyuki Kawagoshi , Tomoaki Tamura , Tetsuo Kadozaki , Tetsuo Miyamoto
IPC分类号： A61K31/40 , A61K31/4025 , A61P7/02 , A61P29/00 , A61P37/08 , C07D207/32 , C07D207/333 , C07D207/48 , C07D405/04 , C07D207/34
CPC分类号： C07D207/333 , C07D207/48 , C07D405/04
摘要： Diphenylpyrrolyfuran derivatives represented by the following formula (I): ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and independently represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, or a lower alkylsulfenyl group; m and n independently represent an integer of from 1 to 3; R.sub.3 represents a hydrogen atom or a lower alkyl group, R.sub.4 represents a hydrogen atom, a lower alkyl group, or a lower acyl group; and R.sub.5 represents a hydrogen atom, a lower alkyl group which may have one or more suitable substituents, a lower alkoxy- or an aryloxy-carbonyl group, an acyl group, or a sufonyl group, and pharmaceutically acceptable salts thereof are disclosed. The compounds disclosed are useful as anti-inflammatory agent, anti-allergic agents, anti-platelet agents and the like.
摘要翻译：由下式（I）表示的二苯基吡咯并呋喃衍生物：其中R 1和R 2可以相同或不同并且独立地表示氢原子，卤原子，低级烷基，低级烷氧基，低级烷硫基或低级烷硫基; m和n独立地表示1〜3的整数， R3表示氢原子或低级烷基，R4表示氢原子，低级烷基或低级酰基; R5表示氢原子，可以具有一个或多个适当取代基的低级烷基，低级烷氧基或芳氧基 - 羰基，酰基或磺酰基及其药学上可接受的盐。所公开的化合物可用作抗炎剂，抗过敏剂，抗血小板剂等。

4. 发明授权

US4008219A 4-Benzazonine derivatives and process for preparation thereof 失效
标题翻译： 4-苯并氮杂衍生物及其制备方法
公开(公告)号：US4008219A
公开(公告)日：1977-02-15
申请号：US467520
申请日：1974-05-06
申请人： Masao Ikeda , Shigeo Miyamoto , Thutomu Nozawa , Akira Kurobe , Osamu Futsukaichi
发明人： Masao Ikeda , Shigeo Miyamoto , Thutomu Nozawa , Akira Kurobe , Osamu Futsukaichi
IPC分类号： C07D223/14 , C07D225/06
CPC分类号： C07D223/14 , C07D225/06
摘要： Novel 4-Benzazonine derivatives and their salts, and processes for the preparation thereof are disclosed. These 4-benzazonine derivatives are represented by the following general formula: ##STR1## wherein R stands for --H, --OH or a lower alkoxy group such as --OCH.sub.3, R.sub.1 designates --H or a lower alkyl group such as --CH.sub.3 and --CH.sub.2 CH.sub.3, R.sub.2 indicates --H or a lower alkyl group such as --CH.sub.3, R.sub.3 stands for --H, a linear or branched, saturated or unsaturated alkyl group having 1 to 4 carbon atoms, a mono- or di-hydroxy lower alkyl group such as --CH.sub.2 OH and ##STR2## a saturated cyclic hydrocarbon group having 3 to 6 carbon atoms or a substituted or unsubstituted aromatic hydrocarbon group having 6 to 8 carbon atoms, and R.sub.4 designates --H, --OH or = O. These compounds have medicinal effects, especially therapeutic activities on the central nervous system, such as analgesic, antitussive and sedative activities.
摘要翻译：公开了新的4-苯并氮杂衍生物及其盐，以及其制备方法。这些4-苯并氮杂衍生物由以下通式表示：其中R代表-H，-OH或低级烷氧基，例如-OCH 3，R 1表示-H或低级烷基如-CH 3和 - CH 2 CH 3，R 2表示-H或低级烷基如-CH 3，R 3表示-H，直链或支链，饱和或不饱和的具有1至4个碳原子的烷基，一或二羟基低级烷基如作为-CH 2 OH和具有3〜6个碳原子的饱和环状烃基或具有6〜8个碳原子的取代或未取代的芳香族烃基，R4表示-H，-OH或= O.这些化合物具有药效特别是中枢神经系统的治疗活动，如止痛，镇咳和镇静活动。

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