-
1.发明授权
公开(公告)号：EP0972775B1
公开(公告)日：2004-12-08
申请号：EP98900695.2
申请日：1998-01-22
发明人： FUKUDA, Yasumichi , SHIMAZAWA, Rumiko-Kyorin Seiyaku Unoki Kazokuryou , OOMORI, Yasuo , TERASHIMA, Shiro
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04
摘要： Novel carbamoyloxypyrroloindole derivatives represented by general formula (1) and having antimicrobial and antitumor activities, optical isomers thereof and pharmacologically acceptable salts of the same, and intermediates in producing the same, wherein R1 represents OH or pyrrolidinyl; n is 1 or 2; R2 represents lower (C¿1-4?) alkyl; Y-Y or Y-X represents CH2, CHOH, CH2-CH2, O-CH2 or NMe-CH2; Z?1¿ represents Cl or Br; and Ar1 represents (a), (b), (c), (d) or (e) (wherein Z?2 and Z3¿ represent each O or NH; m is an integer of 1 to 4; and Ar¿2? represents either of the above a, b, c and d).
-
2.发明授权INTERMEDIATES FOR THE PREPARATION OF DUOCARMYCIN SA AND DERIVATIVES THEREOF, AND PROCESS FOR THE PRODUCTION OF THE INTERMEDIATES 失效中间体多卡米星SA的制备和它的衍生物和制备方法的中间体的
公开(公告)号：EP0937726B1
公开(公告)日：2003-03-12
申请号：EP97928473.4
申请日：1997-06-26
IPC分类号： C07D487/04 , C07D209/12 , A61K31/40
CPC分类号： C07D487/04 , C07D209/12 , Y02P20/55
摘要： Indole derivatives of general formulae (1), (2a) and (2b) and pyrroloindole derivatives of general formula (3) useful as intermediates for the preparation of duocarmycin SA and derivatives thereof which are expected to be useful as anticancer drugs; and a process for the preparation of these derivatives, wherein R1 is an amino-protecting group; R2 is a hydroxyl-protecting group; R3 is a hydroxyl-protecting group; and R4 is C1-C6 linear or branched lower alkyl or benzyl.
-
3.发明公开TRIFLUOROMETHYLPYRROLOINDOLE CARBOXYLIC ESTER DERIVATIVE AND PROCESS FOR PRODUCING THE SAME 失效TRIFLUOROMETHYLPYRROLOINDOLCARBONSÄURE的酯衍生物及其制备方法。
公开(公告)号：EP0656360A1
公开(公告)日：1995-06-07
申请号：EP94908108.7
申请日：1993-08-19
IPC分类号： C07D487/04 , C07D487/10
CPC分类号： C07D487/04 , C07D487/10 , Y02P20/55
摘要： Trifluoromethylpyrroloindole carboxylic ester derivatives represented by general formulae (1) and (2) having an antitumor activity, optically active isomers thereof, and pharmacologically acceptable salts thereof, wherein R represents lower alkyl; R¹ represents an α-amino acid residue, etc.; R² represents hydrogen, a hydroxyl-protecting group, etc.; and Y represents halogen, arylsulfonyloxy, etc.
摘要翻译： 由通式Trifluoromethylpyrroloindole羧酸酯衍生物（1）和（2）具有抗肿瘤活性，光学活性的异构体，以及它们的药理学上可接受的盐，worinřdarstellt低级烷基; [R <1> darstelltα氨基酸残基，等。; ř氢<2> darstellt，羟基保护基，等; 和Y darstellt卤素，芳基磺酰氧基等。
-
公开(公告)号：EP0799827B1
公开(公告)日：2004-05-12
申请号：EP95937194.9
申请日：1995-11-28
IPC分类号： C07D487/04 , A61K31/40
CPC分类号： C07D519/00
-
5.发明授权TRIFLUOROMETHYLPYRROLOINDOLE CARBOXYLIC ESTER DERIVATIVE AND PROCESS FOR PRODUCING THE SAME 失效TRIFLUOROMETHYLPYRROLOINDOLCARBONSÄURE和生产其酯衍生物和方法
公开(公告)号：EP0656360B1
公开(公告)日：2002-11-20
申请号：EP94908108.7
申请日：1993-08-19
IPC分类号： C07D487/04 , C07D487/10
CPC分类号： C07D487/04 , C07D487/10 , Y02P20/55
-
6.发明公开INTERMEDIATES FOR THE PREPARATION OF DUOCARMYCIN SA AND DERIVATIVES THEREOF, AND PROCESS FOR THE PRODUCTION OF THE INTERMEDIATES 失效中间产品用于制备双联霉素SA及其衍生物，AND METHOD FOR中间体的生产
公开(公告)号：EP0937726A1
公开(公告)日：1999-08-25
申请号：EP97928473.4
申请日：1997-06-26
IPC分类号： C07D487/04 , C07D209/12 , A61K31/40
CPC分类号： C07D487/04 , C07D209/12 , Y02P20/55
摘要： Indole derivatives shown by the formulae (1), (2a) and (2b)
(wherein R 1 is a protecting group for amino group; R 2 is a protecting group for hydroxyl group; R 3 is a protecting group for hydroxyl group; R 4 is a C 1 -C 6 linear or branched lower alkyl group, or benzyl group), and pyrroloindole derivatives shown by formula (3)
(wherein R 1 is a protecting group for amino group; R 2 is a protecting group for hydroxyl group; R 3 is a protecting group for hydroxyl group; R 4 is a C 1 -C 6 linear or branched lower alkyl group, or benzyl group), both of which are intermediates for duocarmycin SA, which is expected to be used as an anticancer agent, and derivatives thereof; and a method for producing the same.摘要翻译： [R <2>是羟基的保护基团;; R <3>由式餐饮（1），（2a）和（2b）的
（worin - [R <1>是氨基的保护基团中所示的吲哚衍生物 是用于羟基的保护基; R <4>是由式表示的C1-C6直链或支链低级烷基，或苄基），和pyrroloindole衍生物（3） （worin - [R <1>是保护 组为氨基; R <2>是羟基的保护基; R <3>是用于羟基的保护基; R <4>是C1-C6直链或支链低级烷基，或苄基）， 这两者都是用于多卡米星SA中间体，所有这一切都有望被用作抗癌剂，以及它们的衍生物; 及其制造方法。 -
7.发明公开PYRROLOINDOLE DERIVATIVES AND INTERMEDIATES IN PRODUCING THE SAME 失效ZWISCHENPRODUKTE ZU IHRER HERSTELLUNG的PYRROLOINDOL-DERIVATE
公开(公告)号：EP0972775A1
公开(公告)日：2000-01-19
申请号：EP98900695.2
申请日：1998-01-22
发明人： FUKUDA, Yasumichi , SHIMAZAWA, Rumiko-Kyorin Seiyaku Unoki Kazokuryou , OOMORI, Yasuo , TERASHIMA, Shiro
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04
摘要： Pyrroloindole derivatives having antimicrobial and antitumor activities and having a carbamoyloxy group represented by the following general formula (1), optical isomers thereof, and pharmacologically acceptable salts thereof; and intermediates for production thereof:
where R 1 is OH, or a pyrrolidinyl group; n is 1 or 2; R 2 is a lower alkyl group of C 1 -C 4 ; X-Y or Y-X is CH 2 , CHOH, CH 2 -CH 2 , O-CH 2 , or NMe-CH 2 ; Z 1 is Cl or Br; and Ar 1 is
wherein Z 2 and Z 3 area O or NH; m is 0 or an integer of 1 to 4; and Ar 2 is any of the above groups a, b, c, and d.摘要翻译： 具有抗微生物和抗肿瘤活性并具有由以下通式（1）表示的氨基甲酰氧基的吡咯并吲哚衍生物，其旋光异构体及其药理学上可接受的盐; 及其生产中间体：其中R 1为OH或吡咯烷基的
n为1或2; R 2是C 1 -C 4的低级烷基; X-Y或Y-X是CH 2，CHOH，CH 2 -CH 2，O-CH 2或NMe-CH 2; Z 1是Cl或Br; 且Ar 1为 ，其中Z 2和Z 3区域为O或NH; m为0或1〜4的整数; Ar 2是上述a，b，c和d中的任一个。 -
8.发明公开ACRYLAMIDE DERIVATIVES AND PROCESS FOR PRODUCING THE SAME 失效ACRYLAMID-DERIVATE UND VERFAHREN ZU DEREN HERSTELLUNG
公开(公告)号：EP0799827A1
公开(公告)日：1997-10-08
申请号：EP95937194.9
申请日：1995-11-28
IPC分类号： C07D487/04
CPC分类号： C07D519/00
摘要： Acrylamide derivatives represented by General Formula (1) below:
(One specific example of General Formula (1) is methyl (S,S)-3,3,-[3,3'-(1,4-phenylenediacryloyl)]-bis[1-chloromethyl-5-hydroxy-7-trifluoromethyl-1,2,3,6-tetrahydropyrrolo[3,2-e]indole-8-carboxylate.)
The acrylamide derivatives represented by General Formula (1) is highly selective to cancer cells, less toxic, and highly active also against solid tumor.摘要翻译： （1）表示的丙烯酰胺衍生物：通式（1）的一个具体实例是甲基（S，S）-3,3，-a3,3' - （1,4-亚苯基二
酰基）Ü 由通式（1）表示的丙烯酰胺衍生物对癌细胞是高选择性的， 毒性较小，对实体瘤有较高的活性。-
公开(公告)号：EP2275414B1
公开(公告)日：2015-06-10
申请号：EP09738624.7
申请日：2009-04-27
IPC分类号： C07D277/20 , A61K31/415 , A61K31/4155 , A61K31/42 , A61K31/426 , A61K31/428 , A61K31/433 , A61K31/437 , A61K31/44 , A61K31/454 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/5377 , A61P3/10 , A61P43/00 , C07D213/75 , C07D231/38 , C07D241/20 , C07D261/14 , C07D277/44
CPC分类号： C07C309/77 , C07C2601/02 , C07C2601/08 , C07D213/75 , C07D231/38 , C07D241/20 , C07D261/14 , C07D277/20 , C07D277/44 , C07D277/82 , C07D285/08 , C07D405/04 , C07D405/06 , C07D405/12 , C07D417/04 , C07D417/12 , C07D513/04 , C07F9/5442 , C07F9/650964 , C07F9/6539
-
公开(公告)号：EP2275414A1
公开(公告)日：2011-01-19
申请号：EP09738624.7
申请日：2009-04-27
IPC分类号： C07D277/20 , A61K31/415 , A61K31/4155 , A61K31/42 , A61K31/426 , A61K31/428 , A61K31/433 , A61K31/437 , A61K31/44 , A61K31/454 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/5377 , A61P3/10 , A61P43/00 , C07D213/75 , C07D231/38 , C07D241/20 , C07D261/14 , C07D277/44
CPC分类号： C07C309/77 , C07C2601/02 , C07C2601/08 , C07D213/75 , C07D231/38 , C07D241/20 , C07D261/14 , C07D277/20 , C07D277/44 , C07D277/82 , C07D285/08 , C07D405/04 , C07D405/06 , C07D405/12 , C07D417/04 , C07D417/12 , C07D513/04 , C07F9/5442 , C07F9/650964 , C07F9/6539
摘要： A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1):
(wherein R 1 and R 2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C 1 to C 6 alkyl group, a C 1 to C 6 alkoxy group, a C 1 to C 6 alkylsulfonyl group, a C 1 to C 6 alkylsulfinyl group, a C 1 to C 6 alkylsulfonyl group, or a C 1 to C 6 alkoxy-C 1 to C 6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).摘要翻译： 提供了具有降血糖作用的化合物。 该化合物及其药学上可接受的盐可用于治疗或预防糖尿病，肥胖症等。 该化合物由通式（1）表示：（其中R1和R2各自独立地为氢原子，卤素原子，氨基，羟基，羟基氨基，硝基，氰基，氨磺酰基 C1-C6烷基，C1-C6烷氧基，C1-C6烷基磺酰基，C1-C6烷基亚磺酰基，C1-C6烷基磺酰基或C1-C6烷氧基-C1-C6烷基磺酰基， A是取代或未取代的杂芳基）。
-
-
-
-
-
-
-
-
-
搜索结果
33 条记录 (耗时 0.021 秒)
