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1. 发明授权

US4678785A Thiadiazine compounds 失效
标题翻译：噻二嗪化合物
公开(公告)号：US4678785A
公开(公告)日：1987-07-07
申请号：US792402
申请日：1985-10-29
申请人： Hideki Ao , Minoru Obata , Jun Inui
发明人： Hideki Ao , Minoru Obata , Jun Inui
IPC分类号： C07D413/04 , A61K31/535 , A61K31/54 , A61P9/04 , A61P9/08 , A61P9/10 , C07D417/04
CPC分类号： C07D417/04
摘要： A thiadiazine compound of the formula: ##STR1## a method for preparing said compound and a pharmaceutical composition containing said compound, wherein X is methylene which may be optionally substituted by an alkyl of up to 3 carbon atoms; R is hydrogen atom or methyl group; and n is an integer of 1 or 2.Since the compounds exhibit potent cardiotonic and coronary vasodilator activities and further inhibitory activity on platelet aggregation, they are useful as cardiotonic and antithrombotic drugs.
摘要翻译：下式的噻二嗪化合物：＆lt; IMAGE＆gt;用于制备所述化合物的方法和含有所述化合物的药物组合物，其中X为任选被至多3个碳原子的烷基取代的亚甲基; R为氢原子或甲基; 并且n为1或2的整数。由于该化合物显示出有力的强心剂和冠状血管扩张剂活性和对血小板聚集的进一步抑制活性，因此它们可用作强心剂和抗血栓形成药物。

2. 发明授权

US4423052A 1,4-Dihydropyridine-3,5-dicarboxylic acid ester derivatives 失效
标题翻译： 1,4-二氢吡啶-3,5-二羧酸酯衍生物
公开(公告)号：US4423052A
公开(公告)日：1983-12-27
申请号：US387856
申请日：1982-06-01
申请人： Kazuhiko Araki , Hideki Ao , Kenichi Aihara , Tomohiko Kimura
发明人： Kazuhiko Araki , Hideki Ao , Kenichi Aihara , Tomohiko Kimura
IPC分类号： A61K31/455 , A61P9/08 , A61P9/10 , A61P9/12 , C07D211/90 , C07D213/55 , A61K31/44
CPC分类号： C07D211/90
摘要： 1,4-Dihydropyridine-3,5-dicarboxylic acid ester derivatives represented by the formula ##STR1## (wherein Ar.sup.1 and Ar.sup.2 are each the same or different and represent an aryl group; R.sup.1 represents a lower alkyl group; R.sup.2 and R.sup.3 are each the same or different and represent a lower alkyl or aralkyl group; n is 1 or 2; and R.sup.4 represents a lower alkyl) or the acid addition salts thereof. These compounds are useful as antihypertensive agents and as agents for treating the disturbances of cardiac or cerebral circulation.
摘要翻译： PCT No.PCT / JP81 / 00262 Sec。 371日期1982年6月1日 102（e）日期1982年6月1日PCT提交1981年10月2日PCT公布。出版物WO82 / 01185 PCT 1982年4月15日，由式“IMAGE”表示的1,4-二氢吡啶-3,5-二羧酸酯衍生物（其中Ar1和Ar2各自相同或不同，表示芳基; R1表示低级烷基; R2和R3各自相同或不同，表示低级烷基或芳烷基; n为1或2; R4表示低级烷基）或其酸加成盐。这些化合物可用作抗高血压药物和用作治疗心脏或脑循环紊乱的药剂。

3. 发明授权

US5677316A 8-methoxy-quinolonecarboxylic acid derivatives 失效
标题翻译： 8-甲氧基 - 喹啉酮羧酸衍生物
公开(公告)号：US5677316A
公开(公告)日：1997-10-14
申请号：US473357
申请日：1995-06-07
申请人： Hideki Ao , Tsuyoshi Kuroda , Kazuyuki Kawasaki , Akihiko Moriguchi , Yoshifumi Ikeda , Shin-ichi Uesato
发明人： Hideki Ao , Tsuyoshi Kuroda , Kazuyuki Kawasaki , Akihiko Moriguchi , Yoshifumi Ikeda , Shin-ichi Uesato
IPC分类号： C07D401/04 , A01N43/42 , A61K31/47 , C07D215/16
CPC分类号： C07D401/04
摘要： 8-Methoxy-quinolonecarboxylic acid derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl, a phenylalkyl or an ester residue hydrolyzable in the living body, R.sub.2 is a hydrogen atom or methyl and n is an integer of 1, optical isomers thereof, pharmaceutically acceptable salts thereof and hydrates thereof. The 8-methoxy-quinolonecarboxylic acid derivatives of the present invention have enforced and a wide range of in vitro and in vivo antibacterial effects against Gram-positive bacteria, while retaining a strong antibacterial effect against Gram-negative bacteria, that the conventional quinolonecarboxylic acid antibacterial agents have. In addition, the compounds of the present invention scarcely show problematic side-effects and are low toxic. Therefore, they are expected to show superior clinical effects as antibacterial agents.
摘要翻译：式（I）的8-甲氧基 - 喹啉酮羧酸衍生物，其中R1是氢原子，低级烷基，苯基烷基或可在生物体中水解的酯残基，R2是氢原子或甲基，n是 1的整数，其光学异构体，其药学上可接受的盐和其水合物。本发明的8-甲氧基 - 喹诺酮羧酸衍生物对革兰氏阳性细菌的体外和体内抗菌作用具有广泛的应用范围，同时保留对革兰氏阴性细菌的强烈的抗菌作用，常规的喹诺酮羧酸抗菌剂代理商有。此外，本发明的化合物几乎不显示有问题的副作用，并且毒性低。因此，作为抗菌剂，预期其具有优异的临床效果。

4. 发明授权

US4618607A 1,4-dihydropyridine-3,5-dicarboxylic acid ester derivatives and pharmaceutical compositions 失效
标题翻译： 1,4-二氢吡啶-3,5-二羧酸酯衍生物和药物组合物
公开(公告)号：US4618607A
公开(公告)日：1986-10-21
申请号：US448576
申请日：1982-12-10
申请人： Kazuhiko Araki , Hideki Ao , Jun Inui , Kenichi Aihara
发明人： Kazuhiko Araki , Hideki Ao , Jun Inui , Kenichi Aihara
IPC分类号： C07D211/90 , C07D213/89 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D407/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/12 , C07D491/10 , A61K31/445 , A61K31/55 , C07D401/14
CPC分类号： C07D213/89 , C07D211/90 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/12 , C07D491/10
摘要： 1,4-Dihydropyridine-3,5-dicarboxylic acid ester derivatives of the general formula: ##STR1## or acid addition salts thereof, wherein W is --CH.dbd. or --N.dbd.; Y is --CH.dbd.CH--, --O--, --S--, --CH.dbd.N(O)p-- (p is zero or 1) or --N(R)-- (R is hydrogen or lower alkyl); X.sup.1, X.sup.2 and X.sup.3 are the same or different, and are each hydrogen, halogen, nitro, trifluoromethyl, cyano or lower alkylthio; Z is aryl or 5- or 6-membered aromatic heterocyclic ring (which may have a substituent or two or three substituents which may be the same or different, and the substituent may be halogen, lower alkyl, lower alkoxy, lower alkanoylamino, cyano, nitro, lower alkylthio, trifluoromethyl, sulfamoyl, di-lower alkylsulfamoyl, amino or di-lower alkylamino); ##STR2## is 5- to 7-membered heterocyclic ring which may have nitrogen atom, oxygen atom, sulfur atom or unsaturated bond on the ring, and may be substituted by lower alkyl, lower alkoxycarbonyl, lower alkanoylamino, ethylenedioxy or --(CH.sub.2).sub.m --OR.sup.4 (R.sup.4 is hydrogen, lower alkyl or lower alkanoyl and m is 0, 1 or 2); R.sup.1 and R.sup.2 are the same or different, and are each lower alkyl; R.sup.3 is lower alkyl, aralkyl, heteroaralkyl; and n is an integer 1 to 5. Such compounds are useful as antihypertensive agents and as therapeutic agents for cardiac and cerebral circulation disorders.
摘要翻译： 1,4-二氢吡啶-3,5-二羧酸酯衍生物或其酸加成盐，其中W是-CH =或-N =; Y是-CH = CH-，-O-，-S-，-CH = N（O）p - （p是0或1）或-N（R） - （R是氢或低级烷基） X1，X2和X3相同或不同，各自为氢，卤素，硝基，三氟甲基，氰基或低级烷硫基; Z是芳基或5-或6-元芳族杂环（其可以具有取代基或两个或三个可以相同或不同的取代基，并且取代基可以是卤素，低级烷基，低级烷氧基，低级烷酰基氨基，氰基，硝基，低级烷硫基，三氟甲基，氨磺酰基，二低级烷基氨磺酰基，氨基或二低级烷基氨基）。可以在环上具有氮原子，氧原子，硫原子或不饱和键的5-至7-元杂环，并且可被低级烷基，低级烷氧基羰基，低级烷酰基氨基，亚乙二氧基或 - （CH 2） m-OR4（R4是氢，低级烷基或低级烷酰基，m是0,1或2）。 R 1和R 2相同或不同，并且各自为低级烷基; R3是低级烷基，芳烷基，杂芳烷基; 并且n为1至5的整数。这些化合物可用作抗高血压剂和作为心脏和脑循环障碍的治疗剂。

5. 发明授权

US5179203A Thiadiazine compound with a novel crystalline form 失效
标题翻译：具有新型结晶形式的噻二嗪化合物
公开(公告)号：US5179203A
公开(公告)日：1993-01-12
申请号：US560634
申请日：1990-07-31
申请人： Hideki Ao , Shinro Setoguchi , Yasuhiko Ishida
发明人： Hideki Ao , Shinro Setoguchi , Yasuhiko Ishida
IPC分类号： C07D417/04
CPC分类号： C07D417/04
摘要： Novel .beta.-form crystals of 6-(3,6-dihydro-2-oxo-2H-1,3,4-thiadiazin-5-yl)-3,4-dihydro-2(1H)-quinolinone useful as cardiotonics.
摘要翻译：用作强心剂的6-（3,6-二氢-2-氧代-2H-1,3,4-噻二嗪-5-基）-3,4-二氢-2（1H） - 喹啉酮的新型β-型晶体。

6. 发明授权

US3932423A Imidazolido(1,5-c)thiazolidine-3-spiro-4-piperidines 失效
标题翻译：咪唑烷（1,5-c）噻唑烷-3-螺-4-哌啶
公开(公告)号：US3932423A
公开(公告)日：1976-01-13
申请号：US473977
申请日：1974-05-28
申请人： Katsuo Arimura , Hideki Ao
发明人： Katsuo Arimura , Hideki Ao
IPC分类号： C07D513/20
CPC分类号： C07D513/20
摘要： Imidazolido[1,5-c]thiazolidine-3-spiro-4'-piperidine compounds of the formula: ##SPC1##Wherein R.sup.1 represents a member selected from the group consisting of a hydrogen atom, an alkyl group of from 1 to 4 carbon atoms, a benzyl group, a p-chlorobenzyl group, a 4,5-dimethoxybenzyl group, a 4,5,6-trimethoxybenzyl group, a phenethyl group, an acetyl group, a benzoyl group, a trimethoxybenzoyl group, a methoxycarbonyl group, an ethoxycarbonyl group, a 4,4-bis(p-fluorophenyl)butyl group and a group of the formula ##SPC2##(in which Y represents a member selected from the group consisting of H, F and CH.sub.3 O, and n represents an integer of 1, 2 or 3); R.sup.2 represents a member selected from the group consisting of a hydrogen atom, an alkyl group of from 1 to 4 carbon atoms, an allyl group, a propargyl group, a cyclohexyl group, a phenyl group, a chlorophenyl group, a dichlorophenyl group, a tolyl group, a nitrophenyl group, a naphthyl group, a benzyl group, a phenethyl group and a cinnamyl group; and X represents a member selected from the group consisting of an oxygen atom and a sulphur atom; and pharmaceutically acceptable acid addition salts thereof. These compounds are useful as drugs for the treatment of schizophrenia, mania and various psychoneuroses.
摘要翻译：具有下式的咪唑烷并[1,5-c]噻唑烷-3-螺-4'-哌啶化合物：

7. 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。

8. 发明授权

US4450165A Dihydropyridine compounds 失效
标题翻译：二氢吡啶化合物
公开(公告)号：US4450165A
公开(公告)日：1984-05-22
申请号：US385141
申请日：1982-06-04
申请人： Kazuhiko Araki , Hideki Ao , Tomohiko Kimura , Kenichi Aihara
发明人： Kazuhiko Araki , Hideki Ao , Tomohiko Kimura , Kenichi Aihara
IPC分类号： A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/455 , A61P9/00 , A61P9/08 , A61P9/12 , C07D307/52 , C07D333/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/47 , C07D213/79 , C07D215/58
CPC分类号： C07D401/12 , C07D307/52 , C07D333/20 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： A dihydropyridine compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein Het is 5- or 6-membered aromatic heteroaryl, R.sup.1 and R.sup.2 are each lower alkyl, R.sup.3 is lower alkyl, R.sup.4 is hydrogen, lower alkyl or aralkyl, R.sup.5 is lower alkyl or aralkyl, and n is 1 or 2. Such compounds are useful as therapeutic agents for myocardial and cerebral ischemic syndroms and hypertension.
摘要翻译：下式的二氢吡啶化合物或其药学上可接受的酸加成盐，其中Het为5-或6-元芳族杂芳基，R 1和R 2各自为低级烷基，R 3为低级烷基，R 4为氢，低级烷基或芳烷基，R5是低级烷基或芳烷基，n是1或2.这些化合物可用作心肌和脑缺血综合征和高血压的治疗剂。

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