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1. 发明授权

US4960770A 2-alkyl thieno(triazolo)diazepine compounds and pharmaceutical uses thereof 失效
标题翻译： 2-三烷基噻吩并（三唑并）二氮杂化合物及其药物用途
公开(公告)号：US4960770A
公开(公告)日：1990-10-02
申请号：US304989
申请日：1989-01-11
申请人： Minoru Moriwaki , Masao Abe , Hiroshi Mikashima , Tetsuya Tahara
发明人： Minoru Moriwaki , Masao Abe , Hiroshi Mikashima , Tetsuya Tahara
IPC分类号： A61K31/55 , A61P7/00 , A61P9/00 , A61P9/08 , A61P9/10 , C07D495/04 , C07D495/14
CPC分类号： C07D495/04 , C07D495/14
摘要： A thienotriazolodiazepine compound of the formula: ##STR1## wherein Ar is phenyl, pyridyl, substituted phenyl or substituted pyridyl; R.sup.1 and R.sup.3 are the same or different and each is hydrogen, alkyl having 1 to 4 carbon atoms; R.sup.2 is hydrogen, alkyl having 1 to 4 carbon atoms or trifluoromethyl; R.sup.4 is straight or branched chain alkyl, alkenyl or alkynyl having 6 to 18 carbon atoms, or a thienodiazepine compound of the formula: ##STR2## wherein Ar, R.sup.1, R.sup.2 and R.sup.4 are as defined above, and pharmaceutically acceptable acid addition salt thereof.These compounds are useful as drugs for the treatment of circulatory diseases and various PAF-induced diseases. The compound (II) is also useful as an intermediate for preparing the compound (I).

2. 发明授权

US4910194A Thienotriazolodiazepine compounds and pharmaceutical uses thereof 失效
标题翻译：噻吩并三唑并噻嗪类化合物及其药物用途
公开(公告)号：US4910194A
公开(公告)日：1990-03-20
申请号：US352536
申请日：1989-05-16
申请人： Minoru Moriwaki , Yoichi Akiyama , Kenichi Demizu , Hiroshi Mikashima
发明人： Minoru Moriwaki , Yoichi Akiyama , Kenichi Demizu , Hiroshi Mikashima
IPC分类号： A61K31/55 , A61P3/04 , A61P7/02 , A61P7/10 , A61P9/00 , A61P11/00 , A61P29/00 , A61P37/08 , C07D495/14
CPC分类号： C07D495/14
摘要： A thienotriazolodiazepine compound of the formula: ##STR1## wherein each symbol is as defined in the spedification, or a pharmaceutically acceptable acid addition salt thereof, and pharmaceutically uses thereof.Said compounds exhibit PAF-antagonistic acitivty and are useful for the prevention or treatment of various PAF-induced diseases.

3. 发明授权

US4581369A Imidazole derivatives 失效
标题翻译：咪唑衍生物
公开(公告)号：US4581369A
公开(公告)日：1986-04-08
申请号：US556231
申请日：1983-10-31
申请人： Mineo Tsuruda , Takanori Oe , Kazuyuki Kawasaki , Hiroshi Mikashima , Hiroshi Yasuda
发明人： Mineo Tsuruda , Takanori Oe , Kazuyuki Kawasaki , Hiroshi Mikashima , Hiroshi Yasuda
IPC分类号： C07D233/56 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P1/16 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/00 , C07D233/60 , C07D233/61 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/04 , C07D409/10 , C07D409/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： An imidazole derivative of the formula: ##STR1## wherein each of R.sup.1 and R.sup.4 is a hydrogen atom or a lower alkyl group; each of R.sup.2 and R.sup.3 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an aralkyloxy group, a nitro group or an amino group; A is --O--, --S--, --CH.dbd.CH-- pr --CH.dbd.N--; Z is an aryl group, a thienyl group, a pyridyl group or a furyl group, in which definition these aromatic (heterocyclic) rings may have 1 to 3 substituents, each substituent being independently selected from a halogen atom, a lower alkyl group, a cyclic alkyl group, a lower alkoxy group, a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group, a carboxy-lower-alkoxy group, a di-lower-alkylamino-lower-alkoxy group and a nitro group; and a pharmaceutically acceptable acid addition salt thereof, a method for preparing the same and a pharmaceutical composition containing such compound. Such compounds have inhibitory activities on biosynthesis of thromboxane A.sub.2, inhibitory activities on platelet aggregation, vasodilative activities and protective effects on liver disorders.
摘要翻译： PCT No.PCT / JP83 / 00060 Sec。 371日期：1983年10月31日 102（e）1983年10月31日日期PCT提交1983年2月28日PCT公布。出版物WO83 / 03096 日期：1983年9月15日。下式的咪唑衍生物：其中R 1和R 4各自为氢原子或低级烷基; R2和R3各自为氢原子，卤素原子，羟基，低级烷基，低级烷氧基，芳烷氧基，硝基或氨基; A是-O - ， - S - ， - CH = CH-Pr -CH = N-; Z是芳基，噻吩基，吡啶基或呋喃基，其中这些芳族（杂环）环可以具有1至3个取代基，每个取代基独立地选自卤素原子，低级烷基，羟基，羧基，低级烷氧基羰基，羧基 - 低级烷氧基，二低级烷基氨基 - 低级烷氧基和硝基; 及其药学上可接受的酸加成盐，其制备方法和含有该化合物的药物组合物。这些化合物对凝血恶烷A2的生物合成，对血小板聚集的抑制活性，血管扩张活性和对肝脏疾病的保护作用具有抑制活性。

4. 发明授权

US4661603A Imidazole derivatives 失效
标题翻译：咪唑衍生物
公开(公告)号：US4661603A
公开(公告)日：1987-04-28
申请号：US823633
申请日：1986-01-29
申请人： Mineo Tsuruda , Takanori Oe , Kazuyuki Kawasaki , Hiroshi Mikashima , Hiroshi Yasuda
发明人： Mineo Tsuruda , Takanori Oe , Kazuyuki Kawasaki , Hiroshi Mikashima , Hiroshi Yasuda
IPC分类号： C07D233/60 , C07D521/00 , A61K31/415
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： .alpha.-(2,6-dimethyl-4-carboxyphenyl)-2-methyl-5-(1-imidazolyl)-benzenemethanol, pharmaceutically acceptable metal salts forms thereof, acid addition salt forms thereof, amino acid addition salt forms thereof, hydrate forms thereof and mixtures thereof.Such compounds have inhibitory activities on biosynthesis of thromboxane A.sub.2, inhibitory activities on platelet aggregation, vasodilative activities and protective effects against liver disorders.
摘要翻译： α-（2,6-二甲基-4-羧基苯基）-2-甲基-5-（1-咪唑基） - 苯甲醇，其药学上可接受的金属盐形式，其酸加成盐形式，其氨基酸加成盐形式，水合物形式及其混合物。这些化合物对凝血恶烷A2的生物合成具有抑制活性，对血小板聚集的抑制活性，血管扩张活性和对肝脏疾病的保护作用。

5. 发明授权

US4713381A Oxodiazine compounds and pharmaceutical compositions thereof 失效
标题翻译： Oxodiazine化合物及其药物组合物
公开(公告)号：US4713381A
公开(公告)日：1987-12-15
申请号：US867170
申请日：1986-05-27
申请人： Hideki Ao , Minoru Obata , Tsutomu Yamanaka , Hiroshi Mikashima
发明人： Hideki Ao , Minoru Obata , Tsutomu Yamanaka , Hiroshi Mikashima
IPC分类号： C07D471/04 , C07D487/04 , C07D513/04 , A61K31/535 , A61K31/54
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04
摘要： An oxodiazine compound of the formula: ##STR1## or a pharamceutically acceptable acid addition salt thereof, wherein each of R.sup.1 and R.sup.2 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-C.sub.1-4 alkoxy, phenyl-C.sub.1-4 alkyl-oxy which may be optionally substituted by at least one substituent selected from the group consisting of halogen, C.sub.1-4 alkyl and C.sub.1-4 alkoxy on the phenyl nucleus, or phenyl which may be substituted by at least one substituent selected from the group consisting of halogen, C.sub.1-4 alkyl and C.sub.1-4 alkoxy on the phenyl nucleus; X is --S--, --CH.dbd.N-- or --C(R.sup.3).dbd.C(R.sup.4)--, where each of R.sup.3 and R.sup.4 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-C.sub.1-4 alkoxy or phenyl-C.sub.1-4 alkyl-oxy which may be optionally substituted by at least one substituent selected from the group consisting of halogen, C.sub.1-4 alkyl and C.sub.1-4 alkoxy on the phenyl nucleus; and one of A and B is oxygen, sulfur or --NH-- and the other is --C(R.sup.5) (R.sup.6)--, where each of R.sup.5 and R.sup.6 is hydrogen or C.sub.1-4 alkyl.Such compounds are useful as antithrombotic agents, antianginal agents, coronary circulation improving agent, cerebral circulation improving agents, peripheral circulation improving agents, analgesics and antiinflammatory agents.
摘要翻译：下式的氧代二嗪化合物或其药学上可接受的酸加成盐，其中R 1和R 2各自为氢，卤素，C 1-4烷基，C 1-4烷氧基，C 1-4烷氧基-C 1-4烷氧基，苯基-C 1-4烷基氧基，其可任选被至少一个选自以下的取代基取代：苯基核上的卤素，C 1-4烷基和C 1-4烷氧基，或可被至少一个选自苯基核上的卤素，C 1-4烷基和C 1-4烷氧基的取代基; X是-S-， - CH = N-或-C（R 3）= C（R 4） - ，其中R 3和R 4各自是氢，卤素，C 1-4烷基，C 1-4烷氧基，C 1-4烷氧基 - C 1-4烷氧基或苯基-C 1-4烷氧基，其可任选被至少一个选自苯基核上的卤素，C 1-4烷基和C 1-4烷氧基的取代基取代; A和B之一是氧，硫或-NH-，另一个是-C（R 5）（R 6） - ，其中R 5和R 6各自是氢或C 1-4烷基。这些化合物可用作抗血栓形成剂，抗心绞痛剂，冠状循环改善剂，脑循环改善剂，外周循环改善剂，止痛剂和抗炎剂。

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