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1.发明授权NOVEL BENZOTHIOPHENE DERIVATIVES, THEIR PREPARATION AND USE AS UROKINASE INHIBITORS 失效苯并噻吩，生产和使用作为抑制剂尿激酶
公开(公告)号：EP0927177B1
公开(公告)日：2003-11-26
申请号：EP97940354.0
申请日：1997-09-12
发明人： TANAKA, Akito , MIZUNO, Hiroaki , SAKURAI, Minoru
IPC分类号： C07D333/60 , C07D307/85 , C07D513/04 , C07D333/80 , A61K31/38 , A61K31/34 , A61K31/54
CPC分类号： C07D513/04 , C07D307/85 , C07D333/70 , C07D333/80 , Y02P20/55
摘要： A compound of formula (I) in which R1 is hydrogen, optionally substituted lower alkylcarbamoyl(lower)alkylidene, lower alkylidene, lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, protected carboxy(lower)alkyl, carboxy(lower)alkyl, hydroxy(lower)alkyl, optionally substituted lower alkylcarbamoyl(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkanoyl, protected carboxy(lower)alkanoyl, aroyl, lower alkanoyl, or optionally substituted arylcarbymoyl(lower)alkyl; R2 is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl; R3 is hydrogen or amidino-protective group; A is lower alkylene or carbonyl; X is (1), (2) or (3); Y is lower alkylene, -S- or -SO¿2?-; Z is -S- or -O-; and the line: ----- is a single bond or a double bond, or pharmaceutically acceptable salts thereof, which is useful as a medicament.
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公开(公告)号：EP1070046A1
公开(公告)日：2001-01-24
申请号：EP99909333.9
申请日：1999-03-25
发明人： TANIGUCHI, Kiyoshi , SAKURAI, Minoru , FUJII, Naoaki , HOSOI, Kumi , TOMISHIMA, Yasuyo , TAKASUGI, Hisashi , SOGABE, Hajime , ISHIKAWA, Hirofumi , HANIOKA, Naomi
IPC分类号： C07C217/38 , A61K31/135
CPC分类号： C07D213/40 , A61K31/165 , A61K31/223 , A61K31/404 , A61K31/4045 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4468 , A61K31/495 , A61K31/501 , A61K31/5375 , C07C215/46 , C07C217/30 , C07C217/74 , C07C219/24 , C07C229/18 , C07C229/50 , C07C233/25 , C07C233/43 , C07C233/80 , C07C235/20 , C07C235/24 , C07C237/48 , C07C271/24 , C07C271/30 , C07C271/58 , C07C275/22 , C07C279/22 , C07C307/02 , C07C307/10 , C07C311/08 , C07C311/18 , C07C317/32 , C07C323/25 , C07C323/41 , C07C2601/06 , C07C2601/14 , C07C2602/12 , C07D209/08 , C07D209/16 , C07D211/26 , C07D213/73 , C07D213/85 , C07D233/60 , C07D235/26 , C07D277/46 , C07D295/185 , C07D401/04 , C07D417/14
摘要： This invention relates to new propanolamine derivatives or salts thereof represented by general formula (I), wherein each symbol is as defined in the specification or salts thereof which are β3 adrergenic receptor agonists and therefore have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment of diseases indicated in the specification to a human being or an animal.
摘要翻译： 本申请涉及使用选自式（IV），（V），（VI），（VII）和（VIII）的化合物的β3肾上腺素能受体激动剂
CHEM> CHEM> CHEM > 用于制造用于预防和/或治疗排尿困难的药物。 在上述式中，各种基团，取代基和变量具有说明书中给出的含义。 -
3.发明公开AMINOALCOHOL DERIVATIVES AND THEIR USE AS BETA 3 ADRENERGIC AGONISTS 审中-公开氨基醇衍生物在DEREN VERWENDUNG ALS BETA 3 ADRENERGISCHE ANTAGONISTEN
公开(公告)号：EP1107944A1
公开(公告)日：2001-06-20
申请号：EP99938596.6
申请日：1999-08-23
IPC分类号： C07C215/06 , A61K31/138 , A61P1/00
CPC分类号： C07C323/25 , C07C215/54 , C07C217/30 , C07C217/58 , C07C217/60 , C07C217/62 , C07C217/72 , C07C217/86 , C07C229/34 , C07C229/38 , C07C233/43 , C07C237/08 , C07C271/28 , C07C311/08 , C07C311/28 , C07C317/36 , C07C323/32 , C07C2601/08
摘要： This invention relates to new aminoalcohol derivatives or salts thereof represented by formula (I) wherein each symbol is as defined in the specification or salts thereof which have β3 adrenergic agonist activity and therefore have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment of diseases indicated in the specification to a human being or an animal.
摘要翻译： 本发明涉及由式（I）表示的新的氨基醇衍生物或其盐，其中每个符号如说明书中所定义或其具有β3肾上腺素能激动剂活性，因此具有肠选择性拟交感神经，抗溃疡性，抗胰腺炎， 脂肪分解，抗尿失禁和抗尿频活动，其制备方法，包含其的药物组合物和预防和/或治疗本说明书中对人或动物的疾病的方法 。
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公开(公告)号：EP0976720A1
公开(公告)日：2000-02-02
申请号：EP98907258.2
申请日：1998-03-17
发明人： TANIGUCHI, Kiyoshi , SAKURAI, Minoru , HASHIMOTO, Norio , OKAMOTO, Takumi , TSUBAKI, Kazunori , SHIMIZU, Yasuyo , TAKASUGI, Hisashi
IPC分类号： C07C217/74 , C07C213/04 , A61K31/215
CPC分类号： C07C215/64 , C07C217/30 , C07C217/34 , C07C217/74 , C07C2602/10 , C07C2602/12 , Y02P20/55
摘要： This invention relates to new propanolamine derivatives presented by the following formula [I] :
wherein
R 1 is hydrogen or lower alkenyloxy,
R 2 is carboxy(lower)alkoxy or protected carboxy(lower)alkoxy,
R 3 is hydrogen or N-protective group,
n is an integer of 1 or 2,
and salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-pollakisuria activities, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.摘要翻译： 本发明涉及由下式表示的新的丙醇胺衍生物：其中R 1是氢或低级烯氧基，R 2是羧基（低级）烷氧基或被保护的羧基（低级）烷氧基，R 3， 是氢或N-保护基，n是1或2的整数，以及其具有肠选择性交感神经兴奋剂，抗溃疡性，抗胰腺炎，脂肪分解和抗花粉病活性的盐，其制备方法和 包含其的药物组合物。
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5.发明公开AMINOALCOHOL DERIVATIVES AND THEIR USE AS BETA 3 ADRENERGIC AGONISTS 审中-公开氨基醇衍生物及其AS BETA 3肾上腺素能激动剂
公开(公告)号：EP1140849A1
公开(公告)日：2001-10-10
申请号：EP99961305.2
申请日：1999-12-22
发明人： TANIGUCHI, Kiyoshi , SAKURAI, Minoru , KATO, Takeshi , FUJII, Naoaki , WASHIZUKA, Kenichi , TOMISHIMA, Yasuyo , TAKASUGI, Hisashi , KOHNO, Yutaka , YAMAMOTO, Nobuhiro , TANIMURA, Naoko , ISHIKAWA, Hirohumi
IPC分类号： C07D213/80 , C07D213/85 , C07D213/64 , C07D213/82 , C07D213/89 , C07D239/80 , C07D277/68 , C07D241/44 , C07D215/22 , C07D217/24 , C07D219/06
CPC分类号： C07D213/643 , C07C215/20 , C07C311/08 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/85 , C07D213/89 , C07D215/233 , C07D215/48 , C07D217/24 , C07D219/06 , C07D239/34 , C07D239/80 , C07D241/18 , C07D241/44 , C07D277/68 , C07D471/04
摘要： A compound of formula (I) wherein X1 is bond or -OCH2-; X2 is -(CH2)n-, in which n is 1, 2 or 3; X3 is bond, -O-, -S-, -OCH2-, or -NH-; R1 is phenyl or pyridyl each of which may have one or two substituent(s) selected from the group consisting of hydroxy, halogen, etc.; R2 is hydrogen, (lower)alkoxycarbonyl, etc.; R3 is hydroxy(lower)alkyl; halo(lower)alkyl, etc.; R4 is aryl or unsaturated heterocyclic group, each of which may have one or two substituent(s) selected from the group consisting of lower alkyl, hydroxy, carbamoyl, halogen, lower alkoxy, etc.; and a salt thereof which is useful as a medicament.
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6.发明公开NOVEL BENZOTHIOPHENE DERIVATIVES, THEIR PREPARATION AND USE AS UROKINASE INHIBITORS 失效苯并噻吩，生产和使用作为抑制剂尿激酶
公开(公告)号：EP0927177A1
公开(公告)日：1999-07-07
申请号：EP97940354.0
申请日：1997-09-12
发明人： TANAKA, Akito , MIZUNO, Hiroaki , SAKURAI, Minoru
CPC分类号： C07D513/04 , C07D307/85 , C07D333/70 , C07D333/80 , Y02P20/55
摘要： A compound of formula (I) in which R1 is hydrogen, optionally substituted lower alkylcarbamoyl(lower)alkylidene, lower alkylidene, lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, protected carboxy(lower)alkyl, carboxy(lower)alkyl, hydroxy(lower)alkyl, optionally substituted lower alkylcarbamoyl(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkanoyl, protected carboxy(lower)alkanoyl, aroyl, lower alkanoyl, or optionally substituted arylcarbymoyl(lower)alkyl; R2 is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl; R3 is hydrogen or amidino-protective group; A is lower alkylene or carbonyl; X is (1), (2) or (3); Y is lower alkylene, -S- or -SO¿2?-; Z is -S- or -O-; and the line: ----- is a single bond or a double bond, or pharmaceutically acceptable salts thereof, which is useful as a medicament.
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