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61. 发明专利

JPH08225503A PRODUCTION OF 2-FLUOROCYCLOPROPYLAMINE AND NEW CYCLOPROPYLAMINE DERIVATIVE 失效
公开(公告)号：JPH08225503A
公开(公告)日：1996-09-03
申请号：JP31159195
申请日：1995-11-06
申请人： BAYER AG
发明人： NORUBERUTO RUI , ARUBUREHITO MARUHOORUTO , SHIYUTEFUAN BEEMU
IPC分类号： C07C231/12 , C07C209/00 , C07C211/37 , C07C233/06 , C07C233/14 , C07C271/06 , C07C271/24 , C07C271/36

62. 发明专利

JPH0826002B2 失效
公开(公告)号：JPH0826002B2
公开(公告)日：1996-03-13
申请号：JP24851192
申请日：1992-08-05
申请人： DAIICHI SEIYAKU CO
发明人： HAYAKAWA ISAO , SHINKO SHOGO , YOKOHAMA SHUICHI , IMAMURA MASAZUMI
IPC分类号： C07C211/37 , A61K31/47 , A61K31/495 , A61P31/04 , C07C67/00 , C07C209/00 , C07C209/56 , C07C229/34 , C07C253/00 , C07C255/50 , C07D215/00 , C07D215/56 , C07D241/00 , C07D401/04 , C07D401/14

63. 发明专利

JPH07316134A 1-(2-HALOGENOCYCLOPROPYL)QUINOLINECARBOXYLIC ACID DERIVATIVE 失效
公开(公告)号：JPH07316134A
公开(公告)日：1995-12-05
申请号：JP24851192
申请日：1992-08-05
申请人： DAIICHI SEIYAKU CO
发明人： HAYAKAWA ISAO , SHINKO SHOGO , YOKOHAMA SHUICHI , IMAMURA MASAZUMI
IPC分类号： C07C211/37 , A61K31/47 , A61K31/495 , A61P31/04 , C07C67/00 , C07C209/00 , C07C209/56 , C07C229/34 , C07C253/00 , C07C255/50 , C07D215/00 , C07D215/56 , C07D241/00 , C07D401/04 , C07D401/14
摘要： PURPOSE:To obtain a new compound having a quinolinecarboxylic acid skeleton, useful as an intermediate for synthesizing medicines, esp. antimicrobial agents. CONSTITUTION:The compound of formula I (X and X are each halogen or H; X and X are each halogen; R is H or a lower alkyl), e.g. 1-(1,2-cis-2- fluorocyclopropyl)-6,7-difluoro-1, 4-dihydro-4-oxoquinoline-3-carboxylic acid. The compound of formula I is obtained by reaction between a 3-ethoxy-2-(2,4,5- trifluorobenzoyl)acrylic ethyl ester of formula II (R is C2H5) and cis-1-amino-2- fluorocyclopropane followed by reaction of the product with sodium hydride. The compound of formula I, which has moderate liposolubility and solubility to water, is useful as a medicine hopeful of good oral absorbability and in vivo kinetics.

64. 发明专利

JPH05163232A N-(2-FLUOROCYCLOPROPYL)CARBAMATE DERIVATIVE AND ITS PRODUCTION 失效
公开(公告)号：JPH05163232A
公开(公告)日：1993-06-29
申请号：JP33487591
申请日：1991-12-18
申请人： DAIICHI SEIYAKU CO , SAGAMI CHEM RES
发明人： KAMATA MASAHIRO , HAYAKAWA ISAO , AKIBA TOSHIFUMI , TERAJIMA ATSURO , TAMURA OSAMU , KOBAYASHI YUKO , HASHIMOTO MASARU , KATO TADASHI , NAKATANI KAZUHIKO
IPC分类号： C07C209/88 , C07C211/37 , C07C269/06 , C07C271/24
摘要： PURPOSE:To obtain (1R*,2S*)-2-fluorocyclopropylamine useful as a raw material for producing quinolone derivatives which are excellent antimicrobial agents in an extremely short step by passing an N-vinylcarbamate derivative as a starting raw material through a specific intermediate. CONSTITUTION:A compound expressed by formula 2 (Y is alkyl having 1-3 aryl groups at the 1-position or 4-10C trialkylmethyl) is subjected to addition reaction with a monofluorocarbene to provide an N-[(1R*,2S*)-2- fluorocyclopropyl]carbamate derivative expressed by formula 1. The alkoxycarbonyl group of the compound is then removed to afford the objective (1R*,2S*)-2-fluorocyclopropylamine, having the cis-configuration and expressed by formula 3. The removal of the alkoxycarbonyl group is carried out by hydrolysis when Y is the alkyl and treatment with a strong acid when Y is the trialkylmethyl.

66. 发明专利

JPS62228044A CATALYTIC HYDROGENATION 失效
公开(公告)号：JPS62228044A
公开(公告)日：1987-10-06
申请号：JP1120687
申请日：1987-01-20
申请人： AIR PROD & CHEM
发明人： JIEREMIA PATORITSUKU KEESHII , MAIKERU JIYOSEFU FUASORUKA
IPC分类号： C07B61/00 , B01J23/00 , B01J23/46 , C07C65/24 , C07C67/00 , C07C209/00 , C07C209/68 , C07C209/72 , C07C211/36 , C07C211/37 , C07C211/54

67. 发明专利

JPS6212760A 1-(2-HALOGENOCYCLOPROPYL)QUINOLINECARBOXYLIC ACID DERIVATIVE 失效
公开(公告)号：JPS6212760A
公开(公告)日：1987-01-21
申请号：JP28042785
申请日：1985-12-13
申请人： DAIICHI SEIYAKU CO
发明人： HAYAKAWA ISAO , SHINKO SHOGO , YOKOHAMA SHUICHI , IMAMURA MASAZUMI
IPC分类号： C07C211/37 , A61K31/47 , A61K31/495 , A61P31/04 , C07C67/00 , C07C209/00 , C07C209/56 , C07C229/34 , C07C253/00 , C07C255/50 , C07D215/00 , C07D215/56 , C07D241/00 , C07D401/04 , C07D401/14
摘要： NEW MATERIAL:A compound expressed by formula I (X and X are halogen or H; X is halogen; R -R are H or lower alkyl) and a salt thereof. EXAMPLE:1-(cis-2-Fluorocyclopropyl)-6-fluoro-1,4-dihydro-7-(4--methyl- 1-pipera zinyl)-4-oxoquinoline-3-carboxylic acid. USE:A medicine, useful particularly as an antimicrobial agent, having powerful antimicrobial activity and expected to have oral absorbability and in vivo movement. PREPARATION:For example, 1-(2-fluorocyclopropyl)-6,7-difluoro-1,4-dihydro-4- oxoquinoline-3-carboxylic acid ester expressed by formula III (R is lower alkyl) is hydrolyzed under acidic or alkaline conditions to give a carboxylic acid expressed by formula IV, which is then reacted with a (substituted) piperazine in a solvent to afford the aimed compound expressed by formula I (X and X are F; X is H).

68. 发明专利

JPS58109451A PERFLUOROBICYCLOHEPTANE COMPOUND 失效
公开(公告)号：JPS58109451A
公开(公告)日：1983-06-29
申请号：JP20747681
申请日：1981-12-21
申请人： GREEN CROSS CORP
发明人： YOKOYAMA KAZUMASA , FUKAYA TSUTOMU , TSUDA YOSHIO , ONO TAIZOU , ARAKAWA YOSHIO , INOUE YOSHIHISA , NAITOU YOUICHIROU , SUYAMA TADAKAZU , NAITOU RIYOUICHI
IPC分类号： C25B3/08 , A61K31/13 , A61P7/08 , C07C67/00 , C07C209/00 , C07C211/37
摘要： NEW MATERIAL:The compound of formula (R1 and R2 are lower perfluoroalkyl) which may have lower perfluoroalkyl substituent group at an arbitrary position on the cycloaliphatic ring. EXAMPLE:Perfluoro-N-ethyl-N-methyl-2-norbornylamine. USE:The oxygen-transporting component for blood substitute, oxygen transporting liquid, etc. PROCESS:The compound of formula is prepared by fluorinating the perhydro compound corresponding to the compound of formula by conventional fluorination technique such as electrochemical fluorination, cobalt fluorination, electrolytic fluorination, etc. For example, anhydrous hydrogen fluoride and a perhydro compound are mixed and dissolved with each other in an electrolyzer, and electrolyzed. The compound of formula is separated and purified from the precipitate at the bottom of the electrolyzer.

69. 发明公开

EP2103598A1 Fluorierte Cycloalkyl-derivatisierte Benzoylguanidine, Verfahren zu ihre Herstellung, ihre Verwendung als Medikament, sowie sie enthaltendes Medikament 审中-公开
标题翻译：氟化环烷基衍生的benzoylguanidines，它们的制备方法，它们作为药物的用途，以及含有它们的药物
公开(公告)号：EP2103598A1
公开(公告)日：2009-09-23
申请号：EP09005497.4
申请日：2003-06-02
申请人： Sanofi-Aventis Deutschland GmbH
发明人： Kleemann, Heinz-Werner, Dr.
IPC分类号： C07C317/46 , C07C317/48 , C07C317/44 , A61K31/155 , A61P9/10 , C07C35/48 , C07C211/37
CPC分类号： C07C317/48 , C07C317/46 , C07C2601/04
摘要： Fluorierte Cycloalkyl-derivatisierte Benzoylguanidine der Formel I

sind als antiarrhythmische Arzneimittel mit cardioprotektiver Komponente zur Infarktprophylaxe und der Infarktbehandlung sowie zur Behandlung der angina pectoris geeignet.
Sie inhibieren auch präventiv die pathophysiologischen Vorgänge beim Entstehen ischämisch induzierter Schäden, insbesondere bei der Auslösung ischämisch induzierter Herzarrhythmien und der Herzinsuffizienz.
摘要翻译： N - （（4- Polyfluorocycloalkyl氧基，巯基或氨基）苯甲酰基）-guanidines衍生物（I）是新的。式（I）的苯甲酰基胍衍生物及其盐是新的。 [图像] X：O，S或NR 6; -R 6 H，1-4C烷基或 - （CH2）K-CF 3; K，L，M，N，P，R：0-3; Q = 0-3，提供没有M + N + P + Q + R =至少2; 的R 1 H，1-4C烷基，F，Cl或7，NR 8 R 9或1-4C-全氟烷基; ，R 7 - ，R 9 H，1-4C烷基或 - （CH 2）T-CF 3; T：0-4; R 2 H，氟，氯，1-4C烷基或CF 3; ，R 3 H，氟，氯，1-4C烷基，CF 3或SOüR 1 0; U：0-2; 的R 1 01-4C烷基或NR 1 1 R 1 2; 的R 1 1，R 1 2 H或1-4C烷基; ，R 4为H，F，氯，1-4C烷基，OR 1 3，NR 1 4R 1 5或1-4C-全氟烷基; R 1 3 - 1个R 5 H，1-4C烷基或 - （CH2）W-CF 3; 女：0-4; 和R 5H或F.活性：Vasotropic; 抗心律失常; Cardiant; 抗心绞痛; 脑保护; 抑制细胞生长; 抗动脉硬化; 降血脂; 低血压; 抗惊厥; 镇静剂; 抗抑郁药; 抗精神病药; 降糖; 溶栓; 抗凝血剂; 嗜肝; Nephrotropic; 抗炎; 抗原虫; 抗疟药; 抗甲状腺。作用机理：蜂窝钠 - 质子逆向转运蛋白（NHE）抑制剂。 N-（4-（3,3-二氟环丁氧基）-5-甲磺酰基-2-甲基 - 苯甲酰基）-guanidines（Ia）的有IC 5 0 5.9 nM的抑制NHE1的。

70. 发明公开

EP1487778A1 SUBSTITUIERTE 4-AMINOCYCLOHEXANOLE 有权
标题翻译：替代物4-AMINOCYCLOHEXANOLE
公开(公告)号：EP1487778A1
公开(公告)日：2004-12-22
申请号：EP03708253.4
申请日：2003-03-18
申请人： Grünenthal GmbH
发明人： SUNDERMANN, Bernd , HENNIES, Hagen-Heinrich , ENGLBERGER, Werner , KÖGEL, Babette-Yvonne
IPC分类号： C07C211/35 , C07C211/37 , C07D209/04 , C07D333/46 , A61P25/24 , A61P25/28
CPC分类号： C07C217/52 , C07C2601/14 , C07D209/18 , C07D333/20
摘要： The invention relates to substituted 4-aminocyclohexanols, to methods for producing them, to drugs containing said compounds and to the use of substituted 4-aminocyclohexanols in the production of drugs for the treatment of various indications, especially pain.
摘要翻译：取代的4-氨基环己醇，其制备方法，包含这些化合物的药物组合物以及在制备用于治疗各种适应症，特别是疼痛以及治疗这些适应症的药物组合物中的取代的4-氨基环己醇的用途。

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