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1.发明公开PROCESS FOR PRODUCING OPTICALLY ACTIVE 7-SUBSTITUTED-3-(2-AMINOPROPYL)INDOLE DERIVATIVES AND INTERMEDIATES FOR PRODUCING THE SAME 审中-公开PROCESS制备光学活性7-取代3-（2- AMINOPROLYL）吲哚衍生物中介和其制造
公开(公告)号：EP1275730A1
公开(公告)日：2003-01-15
申请号：EP01917707.0
申请日：2001-03-30
发明人： NARITA, Takao , TOYODA, Kunihiro , HIROSE, Yoichiro , TSUCHIDA, Toshio , KATO, Shiro , HARADA, Hiroshi , FUJII, Akihito
IPC分类号： C12P17/10 , C07D209/20
CPC分类号： C07D209/20 , C07D209/16 , C12P13/04 , C12P17/10
摘要： Disclosed are a process for preparation of an optically active 7-substituted 3-(2-aminopropyl)indole compound and an intermediate therefor. In the above preparation process, 7-substituted indole is reacted with L- or DL-serine in the presence of a tryptophan-synthesizing enzyme originating in microorganisms to form corresponding 7-substituted L-tryptophan, and it is subjected, if necessary, to reduction, protection, exchange and elimination.
摘要翻译： 公开了用于制备光学活性7- substituiertem 3-（2-氨基丙基）吲哚化合物中，并在中间用于其的处理。 在上述制备方法中，7-吲哚substituiertem进行反应与L-或DL-丝氨酸色氨酸合成酶的起源微生物中存在，以形成相应的7-substituiertem L-色氨酸，并使其经受，如有必要，以 减量化，保护，交流和消除。
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2.发明授权1- (1-SUBSTITUTED-4-PIPERIDINYL)METHYL]-4-PIPERIDINE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, MEDICINAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATES OF THESE COMPOUNDS 有权1-（1-取代-4-哌啶基）甲基] -4-哌啶衍生物，生产hazzle FOR THEIR医药中间体及其制备方法和混合物
公开(公告)号：EP1076055B1
公开(公告)日：2004-11-24
申请号：EP99913701.1
申请日：1999-04-19
发明人： KATO, Shiro , TOYOTOMI, Yoshihito , TATEISHI, Hirotaka , HARADA, Hiroshi , YOSHIDA, Naoyuki , MORIKAGE, Kazuo , MORIKAGE, Yukiko
IPC分类号： C07D211/58 , C07D211/96 , C07D405/12 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , C07D405/14 , A61P1/04
CPC分类号： C07D405/14 , C07D211/58
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公开(公告)号：EP0801059B1
公开(公告)日：2001-06-27
申请号：EP95937182.4
申请日：1995-11-27
IPC分类号： C07D209/14 , A61K31/40 , C07D209/16
CPC分类号： C07D209/14 , Y10S514/866 , Y10S514/909
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4.发明公开1- (1-SUBSTITUTED-4-PIPERIDINYL)METHYL]-4-PIPERIDINE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, MEDICINAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATES OF THESE COMPOUNDS 有权1-（1-取代-4-哌啶基）甲基] -4-哌啶衍生物，生产hazzle FOR THEIR医药中间体及其制备方法和混合物
公开(公告)号：EP1076055A1
公开(公告)日：2001-02-14
申请号：EP99913701.1
申请日：1999-04-19
发明人： KATO, Shiro , TOYOTOMI, Yoshihito , TATEISHI, Hirotaka , HARADA, Hiroshi , YOSHIDA, Naoyuki , MORIKAGE, Kazuo , MORIKAGE, Yukiko
IPC分类号： C07D211/58 , C07D211/96 , C07D405/12 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54
CPC分类号： C07D405/14 , C07D211/58
摘要： Compounds represented by general formula (I) or physiologically acceptable acid addition salts thereof and medicinal compositions containing these compounds as the active ingredient, wherein Ar represents (Ar-1) or (Ar-2); and A represents -Z-N(Q 1 )(Q 2 ), -CO-R 7 or - (CH 2 ) p -CH(R 8 )-COR 9 . Because of exhibiting strong affinity for 5-HT 4 receptor, these compounds are useful as drugs for accelerating the peristalsis or drugs for improving digestive tract functions.
摘要翻译： 化合物由通式（I）化合物或其生理上可接受的酸加成盐和药用组合物含有这些化合物作为活性成分为代表，worin氩darstellt（AR-1）或（AR-2）; 和A darstellt -Z-N（Q <1>）（Q <2>），-CO-R <7>或 - （CH 2）p-CH（R <8>） - COR <9>。 因为显示强亲和力对5-HT 4受体的，论文化合物作为药物用于加速蠕动或药物用于改善消化道功能是有用的。
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公开(公告)号：EP1235801A2
公开(公告)日：2002-09-04
申请号：EP00977904.2
申请日：2000-11-24
发明人： IWATA, Motokazu , KURIYAMA, Teruaki , FUJITA, Megumi , FUJIWARA, Keiichi216, Suncity-Katsurazaka-Royal , KATO, Shiro , HARADA, Hiroshi , FUJII, Akihito , ODAI, Osamu , KAWASHIMA, Hitoshi
IPC分类号： C07D209/16 , A61K31/404 , A61P3/04
CPC分类号： C07D209/16
摘要： The present invention provides a solid preparation comprising a crystal of [3-[(2R)-[[(2R)-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1H-indol-7-yloxy]acetic acid (Compound A), especially a crystal of Compound A having a particle size of not larger than 100 νm at the cumulative weight distribution value of 50 %, and not larger than 200 νm at the cumulative weight distribution value of 95 %, preferably a solid preparation having the excellent stability and the content uniformity of Compound A, which is prepared by preparing granules of the crystal of Compound A with fillers, disintegrants and binders, and then followed by mixing said granules with external excipients.
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6.发明授权(R)-5-BROMO-N-(1-ETHYL-4-METHYLHEXAHYDRO-1H-1,4-DIAZEPIN-6-YL)-2-METHOXY-6-METHYLAMINO-3-PYRIDINE-CARBOXAMIDE, PROCESS FOR PRODUCING THE SAME AND MEDICINAL COMPOSITION CONTAINING THE SAME 失效（R）-5-溴-N-（1-乙基-4-甲基六氢-1H-1,4-二氮杂-6-基）-2-甲氧基-6-甲胺基-3-吡啶羧酰胺，其制造方法及含 药物制剂
公开(公告)号：EP0855397B1
公开(公告)日：2001-05-09
申请号：EP96924189.2
申请日：1996-07-23
IPC分类号： C07D401/12 , C07D243/08 , A61K31/55
CPC分类号： C07D401/12 , C07D243/08
摘要： The compound represented by formula (I) and physiologically acceptable acid-addition salts thereof. The compounds have an excellent antiemetic effect based on potent antagonism against serotonin S3 and dopamine D2 receptors and, therefore, are usable as an antiemetic agent in the treatment or prevention of various diseases and many digestive symptoms accompanying the administration of drugs, etc.
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7.发明公开(R)-5-BROMO-N-(1-ETHYL-4-METHYLHEXAHYDRO-1H-1,4-DIAZEPIN-6-YL)-2-METHOXY-6-METHYLAMINO-3-PYRIDINE-CARBOXAMIDE, PROCESS FOR PRODUCING THE SAME AND MEDICINAL COMPOSITION CONTAINING THE SAME 失效（R）-5-溴-N-（1-乙基-4-甲基六氢-1H-1,4-二氮杂-6-基）-2-甲氧基-6-甲胺基-3-吡啶甲酰胺，制造方法相同，并且 含药物制剂
公开(公告)号：EP0855397A1
公开(公告)日：1998-07-29
申请号：EP96924189.2
申请日：1996-07-23
IPC分类号： C07D401/12 , C07D243/08 , A61K31/55
CPC分类号： C07D401/12 , C07D243/08
摘要： This invention discloses a compound which is expressed by formula (I) below:
or physiologically acceptable acid addition salts thereof.
The claimed compound exhibits excellent antiemetic effect based on its potent serotonin S 3 and dopamine D 2 receptor antagonistic activities, and is useful for treatment or prophylaxis of various gastrointestinal symptoms which are associated with various diseases and drug administration.摘要翻译： 本发明盘松下面的化合物的所有其由式（I）中过表达：
或其生理上可接受的酸加成盐。 所要求保护的化合物显示出是根据它的有效的血清素S3和多巴胺D2受体拮抗作用的优异的止吐作用，并且是用于治疗或它们与各种疾病和药物施用相关的各种胃肠道症状的预防是有用的。 -
公开(公告)号：EP0801059A1
公开(公告)日：1997-10-15
申请号：EP95937182.4
申请日：1995-11-27
IPC分类号： C07D209/14 , A61K31/40
CPC分类号： C07D209/14 , Y10S514/866 , Y10S514/909
摘要： An indole derivative of the formula:
wherein R 1 is lower alkoxy, lower alkoxycarbonyl-lower alkoxy, carboxy-lower alkoxy , lower alkoxycarbonyl, phenyl-lower alkoxy, lower alkyl being optionally substituted by hydroxy, di-lower alkylaminosulfonyl, etc., R 2 is hydrogen, halogen, lower alkoxy, lower alkoxycarbonyl-lower alkoxy, carboxy-lower alkoxy, etc., R 3 is hydrogen or lower alkyl, R 4 is halogen or trifluoromethyl, R 5 is lower alkyl, or a salt thereof, these compounds being potent β 3 -adrenergic receptor-stimulating agent with excellent adrenoceptor selectivity, and being useful in the prophylaxis or treatment of obesity or diabetes mellitus.摘要翻译： 下式的吲哚衍生物：其中R 1为低级烷氧基，低级烷氧基羰基 - 低级烷氧基，羧基 - 低级烷氧基，低级烷氧基羰基，苯基 - 低级烷氧基，任选被羟基取代的低级烷基，二 - 低级烷基氨基磺酰基等。 ，R2是氢，卤素，低级烷氧基，低级烷氧基羰基 - 低级烷氧基，羧基 - 低级烷氧基等，R3是氢或低级烷基，R4是卤素或三氟甲基，R5是低级烷基或其盐，这些化合物是 有效的β3肾上腺素能受体刺激剂，具有优良的肾上腺素能受体选择性，可用于预防或治疗肥胖症或糖尿病。
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