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1. 发明授权

US4894453A 2-substituted alkoxy-3-substituted-pyrazines 失效
标题翻译： 2-取代的烷氧基-3-取代 - 吡嗪
公开(公告)号：US4894453A
公开(公告)日：1990-01-16
申请号：US68228
申请日：1987-06-30
申请人： Masao Yaso , Yukio Suzuki , Kensuke Shibata , Daisuke Mochizuki , Eiichi Hayashi
发明人： Masao Yaso , Yukio Suzuki , Kensuke Shibata , Daisuke Mochizuki , Eiichi Hayashi
IPC分类号： C07D241/18 , C07D241/44
CPC分类号： C07D241/44 , C07D241/18
摘要： A compound of the formula ##STR1## wherein Q is --CO-- or --CH.sub.2 --, R is hydroxyl, lower alkoxy, halogen, --NH-lower alkylene-OH, --NH-lower alkylene-arylthio, --NH-lower alkylene-halogen, ##STR2## in which ##STR3## is dilower alkylamino, cycloalkylamino, morpholino, ##STR4## in which R.sub.9 is hydrogen, lower alkyl or aryl, R.sub.10 is hydrogen, lower alkyl, hydroxy-lower alkyl, hydroxy-lower alkoxy-lower alkyl or di(aryl)-lower alkyl, m is an integer from 4 to 6, n is 2 or 3, R.sub.1 is alkyl or aryl-lower alkyl, R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene, and R.sub.4 is hydrogen, lower alkyl or aryl, in which aryl is phenyl which is optionally substituted with a group selected from the group consisting of 1-3 halogen, nitro, lower alkyl and lower alkoxy, or a pharmaceutically acceptable salt thereof, inhibits blood platelet aggregation, has vasodilating activity and inhibits lipoperoxide generation.
摘要翻译：其中Q为-CO-或-CH 2 - ，R为羟基，低级烷氧基，卤素，-NH-低级亚烷基-OH，-NH-低级亚烷基 - 芳硫基，-NH-低级亚烷基 - 卤素，其中是二元烷基氨基，环烷基氨基，吗啉代，其中R9是氢，低级烷基或芳基，R10是氢，低级烷基，羟基 - 低级烷基，羟基 - 低级烷氧基 - 低级烷基或二（芳基） - 低级烷基，m为4-6的整数，n为2或3，R 1为烷基或芳基 - 低级烷基，R 2和R 3为低级烷基，或一起形成四亚甲基，并且R 4是氢，低级烷基或芳基，其中芳基是苯基，其任选被选自1-3个卤素，硝基，低级烷基和低级烷氧基的基团取代，或药学上可接受的其盐抑制血小板聚集，具有血管扩张活性并抑制脂肪过氧化物产生。

2. 发明授权

US5001237A 2-substituted alkoxy-3-substituted-pyrazines 失效
标题翻译： 2-取代的烷氧基-3-取代 - 吡嗪
公开(公告)号：US5001237A
公开(公告)日：1991-03-19
申请号：US381958
申请日：1989-07-19
申请人： Masao Yaso , Yukio Suzuki , Kensuke Shibata , Daisuke Mochizuki , Eiichi Hayashi
发明人： Masao Yaso , Yukio Suzuki , Kensuke Shibata , Daisuke Mochizuki , Eiichi Hayashi
IPC分类号： C07D241/18 , C07D241/44
CPC分类号： C07D241/44 , C07D241/18
摘要： A compound of the formula ##STR1## wherein Q is --CO-- or --CH.sub.2 --, R is hydroxyl, lower alkoxy, halogen, --NH-lower alkylene-OH, --NH-lower alkylene-arylthio, --NH-lower alkylene-halogen, ##STR2## is dilower alkylamino, cycloalkylamino, morpholino, ##STR3## in which R.sub.9 is hydrogen, lower alkyl or aryl, R.sub.10 is hydrogen, lower alkyl, hydroxy-lower alkyl, hydroxy-lower alkoxy-lower alkyl or di(aryl)-lower alkyl, m is an integer from 4 to 6, n is 2 or 3, R.sub.1 is alkyl or aryl-lower alkyl, R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene, and R.sub.4 is hydrogen, lower alkyl or aryl, in which aryl is phenyl which is optionally substituted with a group selected from the group consisting of 1-3 halogen, nitro, lower alkyl and lower alkoxy, or a pharmaceutically acceptable salt thereof, inhibits blood platelet aggregation, has vasodilating activity and inhibits lipoperoxide generation.

3. 发明授权

US4870176A 1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives 失效
标题翻译： 1-取代的烷基-1,2-二氢-2-吡嗪酮衍生物
公开(公告)号：US4870176A
公开(公告)日：1989-09-26
申请号：US260013
申请日：1988-10-19
申请人： Masao Yaso , Yukio Suzuki , Kensuke Shibata , Eiichi Hayashi
发明人： Masao Yaso , Yukio Suzuki , Kensuke Shibata , Eiichi Hayashi
IPC分类号： C07D241/18 , C07D241/44 , C07D403/06 , C07D409/12 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D241/18 , C07D241/44 , C07D249/08 , C07D403/06 , C07D409/12
摘要： 1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives of the formula ##STR1## wherein A is lower alkylene; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; R.sub.2 and R.sub.3 are each lower alkyl; and R is selected from the group consisting of hydroxyl, halogen, lower alkanoyloxy, R.sub.4 -carbamoyloxy and arylthio, in which R.sub.4 is lower alkyl or aryl; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.
摘要翻译： 1-取代的式IMAMA的烷基-1,2-二氢-2-吡嗪酮衍生物，其中A是低级亚烷基; R 1选自烷基，苯基 - 低级烷基和取代的苯基 - 低级烷基; R2和R3各自为低级烷基; 并且R选自羟基，卤素，低级烷酰氧基，R 4 - 氨基甲酰氧基和芳硫基，其中R 4是低级烷基或芳基; 及其药学上可接受的盐。该化合物可用作血小板聚集抑制，血管舒张和抗脂肪过氧化物产生的药剂。

4. 发明授权

US4877877A 1-substituted alkyl-2-oxo-hexahydroquinoxaline derivatives 失效
标题翻译： 1-取代的烷基-2-氧代 - 六氢喹喔啉衍生物
公开(公告)号：US4877877A
公开(公告)日：1989-10-31
申请号：US260904
申请日：1988-10-19
申请人： Masao Yaso , Yukio Suzuki , Kensuke Shibata , Eiichi Hayashi
发明人： Masao Yaso , Yukio Suzuki , Kensuke Shibata , Eiichi Hayashi
IPC分类号： C07D243/00 , A61K31/495 , A61K31/535 , A61K31/55 , A61P3/06 , A61P7/02 , A61P9/08 , C07D241/18 , C07D241/44 , C07D247/00 , C07D333/00 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/12 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D241/18 , C07D241/44 , C07D249/08 , C07D403/06 , C07D409/12
摘要： 1-Substituted alkyl-2-oxo-hexahydroquinoxaline derivatives of the formula ##STR1## wherein A is lower alkylene; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; and R is selected from the group consisting of hydroxyl, halogen, lower alkanocyloxy, R.sub.4 -carbamoyloxy and arylthio, in which R.sub.4 is lower alkyl or aryl; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

5. 发明授权

US4837319A 1-substituted alkyl-1,2-dihydro-2-pyrazinone derivatives 失效
标题翻译： 1-取代的烷基-1,2-二氢-2-吡嗪酮衍生物
公开(公告)号：US4837319A
公开(公告)日：1989-06-06
申请号：US20012
申请日：1987-02-25
申请人： Masao Yaso , Yukio Suzuki , Kensuke Shibata , Eiichi Hayashi
发明人： Masao Yaso , Yukio Suzuki , Kensuke Shibata , Eiichi Hayashi
IPC分类号： C07D243/00 , A61K31/495 , A61K31/535 , A61K31/55 , A61P3/06 , A61P7/02 , A61P9/08 , C07D241/18 , C07D241/44 , C07D247/00 , C07D333/00 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/12 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D241/18 , C07D241/44 , C07D249/08 , C07D403/06 , C07D409/12
摘要： 1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives of the formula ##STR1## wherein A is lower alkyl; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene and R is selected from the group consisting of hydroxyl, hologen, lower alkanoyloxy R.sub.4 -carbamoyloxy, arylthio, 1-methyltetrazole-5-yl-thio, 1-imidazole, morpholino, ##STR2## in which R.sub.4 is lower alkyl or aryl, R.sub.5 is lhydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A, R.sub.1, R.sub.2 and R.sub.3 are as defined above, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

6. 发明授权

US4877875A 1-Substituted alkyl-2-oxo-hexahydroquinoxaline derivatives 失效
标题翻译： 1-取代的烷基-2-氧代 - 六氢喹喔啉衍生物
公开(公告)号：US4877875A
公开(公告)日：1989-10-31
申请号：US259992
申请日：1988-10-19
申请人： Masao Yaso , Yukio Suzuki , Kensuke Shibata , Eiichi Hayashi
发明人： Masao Yaso , Yukio Suzuki , Kensuke Shibata , Eiichi Hayashi
IPC分类号： C07D243/00 , A61K31/495 , A61K31/535 , A61K31/55 , A61P3/06 , A61P7/02 , A61P9/08 , C07D241/18 , C07D241/44 , C07D247/00 , C07D333/00 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/12 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D241/18 , C07D241/44 , C07D249/08 , C07D403/06 , C07D409/12
摘要： 1-Substituted alkyl-2-oxo-hexahydroquinoxaline derivatives of the formula ##STR1## wherein A is lower alkylene; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; and R is selected from the group consisting of 1-methyltetrazole-5-yl-thio, 1-imidazolyl, morpholino, ##STR2## in which R.sub.5 is hydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A and R.sub.1 are as defined above, R.sub.2 and R.sub.3 are each lower alkyl or together form tetramethylene, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

7. 发明授权

US4870171A 1-Substituted alkyl-2-oxo-1,2-dihydroquinoxaline derivatives 失效
标题翻译： 1-取代的烷基-2-氧代-1,2-二氢喹喔啉衍生物
公开(公告)号：US4870171A
公开(公告)日：1989-09-26
申请号：US235733
申请日：1988-08-22
申请人： Masao Yaso , Yukio Suzuki , Eiichi Honda , Kensuke Shibata , Hiroyuki Kinoshita , Noriyasu Takayanagi , Tetsu Saito , Eiichi Hayashi
发明人： Masao Yaso , Yukio Suzuki , Eiichi Honda , Kensuke Shibata , Hiroyuki Kinoshita , Noriyasu Takayanagi , Tetsu Saito , Eiichi Hayashi
IPC分类号： A61K31/495 , A61P9/12 , A61P25/02 , C07D241/44
CPC分类号： C07D241/44
摘要： A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl, R.sup.2 is hydrogen, lower alkoxy or halogen, and A is lower alkylene, or a pharmacologically acceptable salt thereof, has sympatholytic .alpha.-receptor blocking activity and is useful for the treatment of hypertension.

8. 发明授权

US4870175A 6-substituted alkoxy-2-oxo-1,2-dihydroquinoxaline derivatives 失效
标题翻译： 6-取代的烷氧基-2-氧代-1,2-二氢喹喔啉衍生物
公开(公告)号：US4870175A
公开(公告)日：1989-09-26
申请号：US253546
申请日：1988-10-05
申请人： Yukio Suzuki , Masao Yaso , Katumi Nisimura , Kenzi Saeki , Noriyasu Takayanagi , Tetsu Saito , Eiichi Hayashi
发明人： Yukio Suzuki , Masao Yaso , Katumi Nisimura , Kenzi Saeki , Noriyasu Takayanagi , Tetsu Saito , Eiichi Hayashi
IPC分类号： A61K31/495 , A61P7/02 , C07D241/44 , C07D403/12
CPC分类号： C07D403/12 , C07D241/44
摘要： A compound of the formula ##STR1## wherein Z is N or NH, is a single or double bond, R.sub.1 is hydrogen, C.sub.1-20 alkyl or optionally substituted phenyl, A is lower alkylene, R is carboxyl, lower alkoxycarbonyl, ##STR2## or 1-cycloalkyl-tetrazole-5-yl, R.sub.2 is lower alkyl, hydroxy-lower alkyl or optionally substituted phenyl-lower alkyl, R.sub.3 is lower alkyl or cycloalkyl, or R.sub.2 and R.sub.3 together constitute ##STR3## and R.sub.5 and R.sub.6 are hydrogen or optionally substituted phenyl, or a pharmacologically acceptable salt thereof, has platelet aggregation inhibitory activity and/or cyclic AMP/phosphodiesterase inhibitory activity.

9. 发明授权

US4721713A Process for inhibiting blood platelet aggregation and promoting vasodilation 失效
标题翻译：抑制血小板聚集和促进血管舒张的方法
公开(公告)号：US4721713A
公开(公告)日：1988-01-26
申请号：US58890
申请日：1987-06-05
申请人： Eiichi Hayashi , Noriyasu Takayanagi , Katsumi Nishimura , Masao Yaso , Yukio Suzuki
发明人： Eiichi Hayashi , Noriyasu Takayanagi , Katsumi Nishimura , Masao Yaso , Yukio Suzuki
IPC分类号： C07D241/18 , A61K31/495 , A61P7/02
CPC分类号： A61K31/495 , Y10S514/822 , Y10S514/929
摘要： A method for inhibiting blood platelet aggregation in humans, and promoting vasodilation in humans, by administering to a human in need of the same an effective amount of 2-hydroxy-3-isopropyl-5,6-dimethylpyrazine or a hydrate or a pharmaceutically acceptable non-toxic salt thereof. Administration can be orally in an amount of about 0.02-12 mg/kg body weight per day, or parenterally in an amount of about 0.01-6 mg/kg of body weight per day.

10. 发明授权

US5578596A 2-alkoxy-5,6,7,8-tetrahydroquinoxaline derivatives, and production method and use thereof 失效
标题翻译： 2-烷氧基-5,6,7,8-四氢喹喔啉衍生物及其制备方法和用途
公开(公告)号：US5578596A
公开(公告)日：1996-11-26
申请号：US432168
申请日：1995-05-08
申请人： Hideyuki Watanabe , Masao Yaso , Daisuke Mochizuki
发明人： Hideyuki Watanabe , Masao Yaso , Daisuke Mochizuki
IPC分类号： C07D241/44 , C07D401/12 , C07D403/12 , A61K31/495 , A61K31/505
CPC分类号： C07D401/12 , C07D241/44 , C07D403/12
摘要： Disclosed are a compound represented by formula (1) and a non-toxic salt thereof, a production method thereof, and a pharmaceutical composition for treating a serotonergic neuron-related disease comprising the same as an active ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; R.sup.2 represents a pyridyl group which is unsubstituted or substituted with 1 to 3 substituents each independently selected from the group consisting of a halogen atom, a lower alkyl group, a trifluoromethyl group, a lower alkoxy group, a carbamoyl group and a cyano group, or a pyrimidinyl group which is unsubstituted or substituted with 1 to 2 substituents each independently selected from the group consisting of a lower alkyl group and a lower alkoxy group; and n is an integer of from 2 to 5. Compound (1) of the present invention and a non-toxic salt thereof have a strong affinity for serotonin 1A receptor and, therefore, they are useful for preventing and treating serotonergic neuron-related diseases, such as motion sickness, space sickness, emesis, dizziness, depression, anxiety, eating disorder, and the like.
摘要翻译： PCT No.PCT / JP93 / 01589第 371日期1995年5月8日 102（e）日期1995年5月8日PCT提交1993年11月4日PCT公布。公开号WO94 / 11362 日期1994年5月25日公开是由式（1）表示的化合物及其无毒盐及其制备方法和用于治疗含有其作为活性成分的血清素能神经元相关疾病的药物组合物：（1）其中R1表示氢原子或低级烷基; R2表示未取代的或被1-3个独立地选自卤素原子，低级烷基，三氟甲基，低级烷氧基，氨基甲酰基和氰基的取代基取代的吡啶基，或未取代或被1-2个独立地选自低级烷基和低级烷氧基的取代基取代的嘧啶基; 和n为2〜5的整数。本发明化合物（1）及其无毒盐对5-羟色胺1A受体具有强亲和力，因此可用于预防和治疗5-羟色胺能神经元相关疾病，如晕车，空间病，呕吐，眩晕，抑郁，焦虑，饮食失调等。

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