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1.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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公开(公告)号：EP1053247A1
公开(公告)日：2000-11-22
申请号：EP99902855.8
申请日：1999-02-05
发明人： OHKI, Hidenori , MURANO, Kenji , TOJO, Takashi , SHIRAISHI, Nobuyuki , MATSUYA, Takahiro , MATSUDA, Hiroshi , MIZUNO, Hiroaki , BARRETT, David , MATSUDA, Keiji , KAWABATA, Kohji
摘要： This invention relates to new polypeptide compounds represented by general formula (I), wherein R?1, R2, R3 and R4¿ are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on β-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
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3.发明授权
公开(公告)号：EP0699185B1
公开(公告)日：2001-09-05
申请号：EP94914623.7
申请日：1994-05-12
IPC分类号： C07D207/32 , A61K31/395 , C07D407/04 , C07D413/04 , C07D333/24 , C07D521/00 , C07D257/04 , C07D498/04 , C07C279/22 , C07D207/34 , C07D277/30
CPC分类号： C07D207/327 , C07C279/22 , C07D207/335 , C07D207/34 , C07D231/12 , C07D233/56 , C07D249/08 , C07D257/04 , C07D277/30 , C07D333/24 , C07D401/04 , C07D401/10 , C07D413/04
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4.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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5.发明公开
公开(公告)号：EP0699185A1
公开(公告)日：1996-03-06
申请号：EP94914623.0
申请日：1994-05-12
IPC分类号： C07D237 , A61K31 , A61P9 , A61P13 , A61P15 , C07C279 , C07D207 , C07D213 , C07D231 , C07D239 , C07D257 , C07D277 , C07D307 , C07D333 , C07D401 , C07D403 , C07D413 , C07D498 , C07D521
CPC分类号： C07D207/327 , C07C279/22 , C07D207/335 , C07D207/34 , C07D231/12 , C07D233/56 , C07D249/08 , C07D257/04 , C07D277/30 , C07D333/24 , C07D401/04 , C07D401/10 , C07D413/04
摘要： Guanidine derivatives of formula (I), wherein Y is N or C-R1 (in which R1 is hydrogen, lower alkyl, hydroxy, protected hydroxy, etc.), R2 is hydrogen, aryl which may have one suitable substituent, aryloxy, etc., R3 is hydrogen, lower alkoxy, hydroxy, protected hydroxy, etc., Z is N or C-R4 (in which R4 is hydrogen, carboxy, protected carboxy, nitro, halogen, hydroxy(lower)alkyl, etc.), and W is N or C-R12 (in which R12 is hydrogen, lower alkoxy, nitro, hydroxy or protected hydroxy), and pharmaceutically acceptable salts thereof which are useful as a medicament.
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公开(公告)号：EP0773927A2
公开(公告)日：1997-05-21
申请号：EP95926026.0
申请日：1995-07-25
IPC分类号： C07D295 , A61K31 , A61P9 , A61P13 , A61P15 , C07C279 , C07D209 , C07D215 , C07D217 , C07D241 , C07D263 , C07D307 , C07D311 , C07D317 , C07D321 , C07D333 , C07D471
CPC分类号： C07D263/56 , C07C279/22 , C07C2601/10 , C07C2602/10 , C07C2602/12 , C07C2602/28 , C07D209/08 , C07D215/14 , C07D217/02 , C07D241/42 , C07D295/13 , C07D307/46 , C07D307/56 , C07D307/79 , C07D307/80 , C07D307/82 , C07D311/58 , C07D311/96 , C07D317/54 , C07D333/22 , C07D333/28 , C07D333/36 , C07D333/54 , C07D333/56 , C07D333/62 , C07D471/04
摘要： Guanidine derivatives of formula (I) wherein R1 is hydrogen, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, acyl(lower)alkoxy, acyl(lower)alkenyl, or acyl, and R2 is ar(lower)alkenyl; aryl substituted with two suitable substituents; indenyl, indanyl, dihydrobenzocycloheptenyl, di(or tetra or hexa or octa or deca)hydronaphthyl, cyclopentenyl, dihydrothienyl, dihydrofuryl or heterobicyclic group, each of which may have suitable substituent(s); lower alkylthienyl; mono(or di)halothienyl; mono(or di or tri)halo(lower)alkylthienyl; acylthienyl; halofuryl; or mono(or di or tri)halo(lower)alkylfuryl; and a pharmaceutically acceptable salt thereof, which is useful as a medicament.
摘要翻译： PCT No.PCT / JP95 / 01479 Sec。 371日期1997年2月3日 102（e）日期1997年2月3日PCT提交1995年7月25日PCT公布。 公开号WO96 / 04241 日期1996年2月15日制备药物组合物的方法，其包括将权利要求1的化合物或其药学上可接受的盐与药学上可接受的载体混合。
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