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公开(公告)号:US5185333A
公开(公告)日:1993-02-09
申请号:US721011
申请日:1991-06-26
IPC分类号: C07D265/36 , C07D279/16 , C07D413/12 , C07D417/12 , C07D451/04 , C07D451/14 , C07D453/02
CPC分类号: C07D451/04 , C07D265/36 , C07D279/16 , C07D413/10 , C07D417/12 , C07D451/14 , C07D453/02
摘要: A benzazine compound, a geometrical isomer of said benzazine compound, an optical isomer of said benzazine compound, and a pharmaceutically acceptable salt of said benzazine compound, said benzazine compound being represented by formula (I): ##STR1## wherein each symbol is as defined in the specification. Said benzazine compounds exhibit 5-HT.sub.3 receptor antagonistic activity, and 5-HT.sub.1A receptor and/or 5-HT.sub.2 receptor and/or dopamine D.sub.2 receptor blocking activity so that they are useful as drugs for the prophylaxis or treatment of various digestive diseases vomiting and disturbances in central nervous systems and the like. The intermediates for said benzazine compounds are also disclosed.
摘要翻译: 苯并嗪化合物,所述苯并嗪化合物的几何异构体,所述苯并嗪化合物的光学异构体和所述苯并嗪化合物的药学上可接受的盐,所述苯并嗪化合物由式(I)表示:其中每个符号 如本说明书中所定义。 所述苯并嗪化合物显示5-HT 3受体拮抗活性和5-HT1A受体和/或5-HT2受体和/或多巴胺D2受体阻断活性,使得它们可用作预防或治疗各种消化疾病呕吐和干扰的药物 在中枢神经系统等中。 还公开了所述苯并嗪化合物的中间体。
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公开(公告)号:US5864039A
公开(公告)日:1999-01-26
申请号:US982389
申请日:1997-12-02
申请人: Takeshi Kawakita , Takanobu Kuroita , Takahiro Murozono , Hidetoshi Hakira , Keiichiro Haga , Katsuhiko Ito , Shuji Sonda , Toshio Kawahara , Kiyoshi Asano
发明人: Takeshi Kawakita , Takanobu Kuroita , Takahiro Murozono , Hidetoshi Hakira , Keiichiro Haga , Katsuhiko Ito , Shuji Sonda , Toshio Kawahara , Kiyoshi Asano
IPC分类号: C07D221/02 , C07D265/14
CPC分类号: C07D221/02 , C07D265/14
摘要: Benzoic acid compounds of the formula ##STR1## wherein each symbol is as defined in the specification, optical isomers thereof and pharmaceutically acceptable salts thereof; pharmaceutical composition comprising this compound and pharmaceutically acceptable additive; and serotonin 4 receptor agonists, gastrointestinal prokinetic agents and therapeutic agents for various gastrointestinal diseases, which comprise this compound as active ingredient. The compounds of the present invention have high and selective affinity for serotonin 4 receptor, and show agonistic effects thereon. Accordingly, they are useful medications for the prophylaxis and treatment of various gastrointestinal diseases, central nervous disorders, cardiac function disorders, urinary diseases, and the like, as well as useful anti-nociceptors for analgesic use which increase threshold of pain.
摘要翻译: 式(I)的苯甲酸化合物,其中每个符号如说明书中所定义,其光学异构体和其药学上可接受的盐; 包含该化合物和药学上可接受的添加剂的药物组合物; 和5-羟色胺4受体激动剂,胃肠促动素和各种胃肠道疾病的治疗剂,其包含该化合物作为活性成分。 本发明化合物对5-羟色胺4受体具有高选择性的亲和力,并且对其表现出激动作用。 因此,它们是用于预防和治疗各种胃肠道疾病,中枢神经障碍,心脏功能障碍,尿病等的有用药物,以及增加疼痛阈值的有用的止痛药用抗伤害感受器。
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公开(公告)号:US4414216A
公开(公告)日:1983-11-08
申请号:US390433
申请日:1982-06-21
IPC分类号: C07D405/06 , A61K31/443 , A61K31/445 , A61K31/495 , A61P1/00 , A61P25/26 , C07C29/147 , C07C33/30 , C07D307/10 , C07D307/12 , C07D307/33 , C07D405/14 , C07D471/04 , C07D471/10 , C07D471/20 , C07D513/20 , A61K31/505
CPC分类号: C07D307/33 , C07C29/147 , C07C33/30 , C07D307/10 , C07D307/12 , C07D471/10
摘要: There are disclosed tetrahydrofuran compounds and analogs thereof of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein X is oxygen or sulfur, R.sup.1 and R.sup.2 are each hydrogen, halogen, lower alkyl or lower alkoxy, and Am is a group of the formula: ##STR2## wherein Z is oxygen or sulfur, R.sup.3 is hydrogen or halogen, R.sup.4 is hydrogen, lower alkyl or phenyl which may be substituted by 1 to 3 substituents at any position(s) on the phenyl nucleus, each substituent being independently selected from halogen, lower alkyl and lower alkoxy, and R.sup.5 is hydrogen or lower alkyl. Such compounds are useful as neuroleptics.
摘要翻译: 公开了具有下式的四氢呋喃化合物及其类似物:其中X是氧或硫,R 1和R 2各自是氢,卤素,低级烷基或低级烷氧基,并且Am是一个基团 其中Z是氧或硫,R 3是氢或卤素,R 4是氢,低级烷基或苯基,其可以被1至3个取代基取代在任何位置上 苯基核,每个取代基独立地选自卤素,低级烷基和低级烷氧基,R 5是氢或低级烷基。 这些化合物可用作精神安定药。
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公开(公告)号:US4892872A
公开(公告)日:1990-01-09
申请号:US261067
申请日:1988-10-24
IPC分类号: C07D413/12 , A61K31/435 , A61K31/445 , A61K31/46 , A61K31/535 , A61P1/08 , A61P1/12 , A61P1/14 , A61P25/04 , A61P25/18 , C07D451/04 , C07D451/06 , C07D451/14 , C07D453/02 , C07D498/04
CPC分类号: C07D451/04 , C07D413/12 , C07D453/02
摘要: Benzoxazine compounds of the formula: ##STR1## wherein each symbol is as defined in the specification. The compounds exhibit 5-HT.sub.3 receptor antagonistic activity so that they are useful as antiemetics and so on.
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公开(公告)号:US4720493A
公开(公告)日:1988-01-19
申请号:US799989
申请日:1985-11-20
IPC分类号: A61K31/425 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/535 , A61P1/04 , A61P25/08 , A61P25/20 , C07D333/00 , C07D333/22 , C07D333/38 , C07D417/04 , C07D417/14
CPC分类号: C07D417/04 , C07D333/22 , C07D333/38 , C07D417/14
摘要: Thienylthiazole compounds of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein: R is amino, guanidino, alkylamino, alkenylamino, unsubstituted or optionally substituted phenylamino or acylamino;A is amino, alkylamino, cyclic amino, alkanoylamino, a group of the formula: ##STR2## wherein each symbol is as defined in claim 1; Z is hydrogen or halogen; andm is 0 or 1 to 4,are useful in the treatment of peptic ulcer, acute or chronic gastritis, acute damage of gastric mucous membrane, dimentia and anxiety.
摘要翻译: 下式的噻吩噻唑化合物及其药学上可接受的酸加成盐,其中:R为氨基,胍基,烷基氨基,烯基氨基,未取代或任选取代的苯基氨基或酰氨基; A是氨基,烷基氨基,环状氨基,烷酰基氨基,下式的基团:其中每个符号如权利要求1中所定义; Z是氢或卤素; m为0或1〜4,可用于治疗消化性溃疡,急性或慢性胃炎,胃粘膜急性损伤,疼痛和焦虑。
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公开(公告)号:US4397853A
公开(公告)日:1983-08-09
申请号:US253930
申请日:1981-04-14
IPC分类号: A61K31/415 , A61K31/42 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5377 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/26 , A61P29/00 , C07D261/04 , C07D413/04 , C07D413/06 , C07D413/14 , C07D471/04 , C07D471/10 , C07D471/20
CPC分类号: C07D471/04 , C07D261/04 , C07D471/10
摘要: Isoxazole derivatives represented by the formula ##STR1## wherein Ar, R.sup.1, R.sup.2 and Am are as defined in the specification, or salts thereof. These compounds are useful as drugs such as psychotropic agent, antiemetic agent, etc.
摘要翻译: PCT No.PCT / JP80 / 00286 Sec。 371日期1981年7月28日 102(e)日期1981年4月14日PCT提交1980年11月25日PCT公布。 第WO81 / 01554号公报 日期:1981年6月11日。由式
表示的异唑衍生物,其中Ar,R 1,R 2和Am如说明书中所定义,或其盐。 这些化合物可用作药物如精神药物,止吐剂等。 -
公开(公告)号:US4517299A
公开(公告)日:1985-05-14
申请号:US500883
申请日:1983-06-03
申请人: Hiroshi Imanaka , Toshio Miyoshi , Toshio Konomi , Yoshiaki Kubochi , Seiziro Hattori , Takeshi Kawakita
发明人: Hiroshi Imanaka , Toshio Miyoshi , Toshio Konomi , Yoshiaki Kubochi , Seiziro Hattori , Takeshi Kawakita
CPC分类号: C12P35/06 , C12N9/18 , Y10S435/911
摘要: New acetylesterases are prepared from Aureobasidium pullulans IFO 4466 which are capable of hydrolyzing cephalosporin C to deacetylcephalosporin C.
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公开(公告)号:US4514403A
公开(公告)日:1985-04-30
申请号:US303269
申请日:1981-09-17
申请人: Chiaki Tashiro , Takeshi Kawakita , Ichiro Horii , Koretake Anami
发明人: Chiaki Tashiro , Takeshi Kawakita , Ichiro Horii , Koretake Anami
IPC分类号: A61K31/505 , A61P25/04 , A61P25/20 , C07D401/04
CPC分类号: C07D401/04
摘要: A hydrouracil compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein A represents --CH.dbd.CH--CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, and R represents hydrogen or methyl. Such compounds are useful as analgesics.
摘要翻译: 其中A表示-CH = CH-CH 2 - 或-CH 2 CH 2 - ,R表示氢或甲基,其具有下式的氢化尿嘧啶化合物:其中A表示-CH = CH-CH 2 - 或-CH 2 CH 2 - 。 这些化合物可用作镇痛药。
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公开(公告)号:US5616581A
公开(公告)日:1997-04-01
申请号:US460666
申请日:1995-06-02
IPC分类号: C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C08G65/333 , A61K31/44 , A61K31/535
CPC分类号: C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C08G65/3332
摘要: A pyridine compound of the formula ##STR1## wherein R.sup.1 is a hydrogen, a halogen, an alkyl, an alkoxy or the like, R.sup.2 and R.sup.3 are each a hydrogen, a halogen or an alkyl, --P.dbd.Q-- is --CH.dbd.CH--, --N.dbd.CH-- or --CH.dbd.N--, A is an oxygen atom, a sulfur atom or N(R.sup.4) wherein R.sup.4 is hydrogen, alkyl or the like, n is 0, 1 or 2, B is S(O)p wherein p is 0, 1 or 2, D is a single bond, an alkylene or the like and E is an alkoxyalkyl or --N(R.sup.6)(R.sup.7), and a pharmaceutically acceptable salt thereof have antibacterial activity against Helicobacter pylori, antiulcer activity, gastrointestinal cytoprotective activity, ulcer recurrence, relapse-preventive activity and gastric acid secretion-suppressive activity and are useful as pharmaceutical preparations.
摘要翻译: 式(I)的吡啶化合物其中R 1是氢,卤素,烷基,烷氧基等,R 2和R 3各自是氢,卤素或烷基,-P = Q-是 -CH = CH-,-N = CH-或-CH = N-,A是氧原子,硫原子或其中R4是氢,烷基等的N(R4),n是0,1或2, B是S(O)p,其中p是0,1或2,D是单键,亚烷基等,E是烷氧基烷基或-N(R6)(R7),其药学上可接受的盐具有抗菌性 针对幽门螺杆菌的活性,抗溃疡活性,胃肠细胞保护活性,溃疡复发,复发预防活性和胃酸分泌抑制活性,可用作药物制剂。
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公开(公告)号:US5504082A
公开(公告)日:1996-04-02
申请号:US352183
申请日:1994-12-01
IPC分类号: C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C08G65/333 , A61K31/44 , A61K31/535 , C07D413/14
CPC分类号: C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C08G65/3332
摘要: A pyridine compound of the formula ##STR1## wherein R.sup.1 is a hydrogen, a halogen, an alkyl, an alkoxy or the like, R.sup.2 and R.sup.3 are each a hydrogen, a halogen or an alkyl, --P.dbd.Q-- is --CH.dbd.CH--, --N.dbd.CH-- or --CH.dbd.N--, A is an oxygen atom, a sulfur atom or N(R.sup.4) wherein R.sup.4 is hydrogen, alkyl or the like, n is 0, 1 or 2, B is S(O)p wherein p is 0, 1 or 2, D is a single bond, an alkylene or the like and E is an alkoxyalkyl or --N(R.sup.6)(R.sup.7), and a pharmaceutically acceptable salt thereof have antibacterial activity against Helicobater pylori, antiulcer activity, gastrointestinal cytoprotective activity, ulcer recurrence, relapse-preventive activity and gastric acid secretion-suppressive activity and are useful as pharmaceutical preparations.
摘要翻译: 式(I)的吡啶化合物其中R 1是氢,卤素,烷基,烷氧基等,R 2和R 3各自是氢,卤素或烷基,-P = Q-是 -CH = CH-,-N = CH-或-CH = N-,A是氧原子,硫原子或其中R4是氢,烷基等的N(R4),n是0,1或2, B是S(O)p,其中p是0,1或2,D是单键,亚烷基等,E是烷氧基烷基或-N(R6)(R7),其药学上可接受的盐具有抗菌性 针对幽门螺旋杆菌的活性,抗溃疡活性,胃肠细胞保护活性,溃疡复发,复发预防活性和胃酸分泌抑制活性,可用作药物制剂。
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