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1. 发明授权

US4668682A 2-Phenylalkyl-3-aminoalkyl-4(3H)-quinazolinone compound 失效
标题翻译： 2-苯基烷基-3-氨基烷基-4（3H） - 喹唑啉酮化合物
公开(公告)号：US4668682A
公开(公告)日：1987-05-26
申请号：US753708
申请日：1985-07-10
申请人： Tetsuo Sekiya , Mikio Tsutsui , Daijiro Horii , Akira Ishibashi
发明人： Tetsuo Sekiya , Mikio Tsutsui , Daijiro Horii , Akira Ishibashi
IPC分类号： C07D239/91 , A61K31/505 , A61K31/517 , A61P3/00 , A61P3/14 , A61P9/08 , A61P9/12 , A61P11/08 , C07D239/90 , C07D401/06
CPC分类号： C07D239/90
摘要： Disclosed are a 2-phenylalkyl-3-aminoalkyl-4(3H)-quinazolinone compound of Formula (1): ##STR1## wherein, X represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, a phenoxy group, a benzyloxy group, a halogen atom or a hydroxy group; Y represents an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, a benzyloxy group, a halogen atom or a nitro group; R.sup.1 represents a hydrogen atom or an alkyl group having 1 to 5 carbon atoms; R.sup.2 represents an alkyl group having 1 to 5 carbon atoms or a group of Formula (2) ##STR2## [wherein, Z represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms or a halogen atom; d is an integer of 1 to 3; and l is an integer of 1 to 5]; or R.sup.1 and R.sup.2 represent together with the nitrogen atom to which they are attached, a cyclic amino group of the formula: ##STR3## [wherein, A represents an alkylene group having 2 to 6 carbon atoms or a group of the formula --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --]; a and b are independently an integer of 1 to 3; and n and m are independently an integer of 1 to 5, or a pharmaceutically acceptable acid addition salt thereof, a process for preparing said compound, a composition comprising said compound as an active ingredient and a method of treatment by use of said compound.The compounds of the present invention have calcium antagonistic, vasodilative, and antihypertensive activities.
摘要翻译：公开了式（1）的2-苯基烷基-3-氨基烷基-4（3H） - 喹唑啉酮化合物：其中X表示氢原子，具有1至5个碳原子的烷基，具有1个至5个碳原子，苯氧基，苄氧基，卤原子或羟基; Y表示碳原子数1〜5的烷基，碳原子数1〜5的烷氧基，苄氧基，卤素原子或硝基。 R1表示氢原子或碳原子数1〜5的烷基。 R 2表示碳原子数1〜5的烷基或式（2）的基团[其中，Z表示氢原子，碳原子数1〜5的烷基，碳原子数1〜5的烷氧基或卤素原子; d为1〜3的整数， l为1〜5的整数]。或者R 1和R 2与它们所连接的氮原子一起表示下式的环状氨基：其中A表示碳原子数为2〜6的亚烷基或式 - （CH 2 ）2-O-（CH 2）2 - ]; a和b独立地为1〜3的整数; n和m独立地为1〜5的整数，或其药学上可接受的酸加成盐，制备所述化合物的方法，包含所述化合物作为活性成分的组合物和使用所述化合物的方法。本发明的化合物具有钙拮抗，血管扩张和抗高血压活性。

2. 发明授权

US5053526A Pharmaceuticals containing prostaglandin I.sub.2 失效
标题翻译：含有前列腺素I2的药物
公开(公告)号：US5053526A
公开(公告)日：1991-10-01
申请号：US511945
申请日：1990-04-16
申请人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
发明人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
IPC分类号： A61K31/557 , C07C405/00
CPC分类号： C07C405/0083 , A61K31/557
摘要： Disclosed is a pharmaceutical having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt of its salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group; A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or 1 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof, the asymmetric center in the substituent represented by A is R-configuration or S-configuration or a mixture thereof.The pharmaceuticals containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.
摘要翻译：本发明公开了一种具有循环改善作用和抗溃疡效果的药物，其含有下述式表示的前列腺素I2类似物或其盐的无毒性盐或其环糊精包合物作为有效成分：其中R1表示氢原子，碳原子数1〜12的烷基，碳原子数4〜7的环烷基或苯基; A表示戊基，环戊基，环己基，1-甲基-3-己炔基，2-甲基-3-己炔基，1-甲基己基，2-苯乙基，1,1 2-甲基戊基，2-甲基戊基，1-环己基乙基，2-甲基己基，1-甲基-3-戊炔基或1,6-二甲基-5-庚烯基; 在4-和5-位碳原子之间的双键是E或Z或其混合物，由A表示的取代基中的不对称中心是R-构型或S-构型或其混合物。含有本发明的前列腺素I2类似物作为活性成分的药物具有有效的血小板聚集抑制作用，降血压作用，血管扩张作用和抗溃疡作用，毒性也低。

3. 发明授权

US4699921A Pharmaceuticals containing prostaglandin I.sub.2 失效
标题翻译：含有前列腺素I2的药物
公开(公告)号：US4699921A
公开(公告)日：1987-10-13
申请号：US763618
申请日：1985-08-08
申请人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
发明人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
IPC分类号： C07C59/46 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/12 , C07C51/00 , C07C67/00 , C07C69/732 , C07C405/00
CPC分类号： C07C405/0083 , A61K31/557 , Y02P20/55
摘要： Disclosed is a pharmaceutical composition having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group, A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or a 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof; the asymmetric center in the substituent represented by A is in the R-configuration or the S-configuration or a mixture thereof.Pharmaceutical compositions containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.
摘要翻译：本发明公开了一种具有循环改善作用和抗溃疡效果的药物组合物，其含有下述式表示的前列腺素I 2类似物或其无毒性盐或环糊精包合物作为有效成分：其中R 1表示氢原子，碳原子数1〜12的烷基，碳原子数4〜7的环烷基或苯基，A表示戊基，环戊基，环己基，1-甲基-3-己炔基，2 1-甲基-3-己炔基，1-甲基己基，2-苯乙基，1,1-二甲基戊基，2-甲基戊基，1-环己基乙基，2-甲基己基，1-甲基 -3-戊炔基或2,6-二甲基-5-庚烯基; 4-和5-位的碳原子之间的双键是E或Z或它们的混合物; 由A表示的取代基中的不对称中心是R构型或S-构型或其混合物。含有本发明的前列腺素I2类似物作为活性成分的药物组合物具有有效的血小板聚集抑制作用，降血压作用，血管扩张作用和抗溃疡作用，毒性也低。

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