公开(公告)号：EP1660085A1

公开(公告)日：2006-05-31

申请号：EP04763848.1

申请日：2004-08-06

申请人： Pharmacia Italia S.p.A.

发明人： VANOTTI, Ermes ,  D'ALESSIO, Roberto ,  TIBOLLA, Marcellino ,  VARASI, Mario ,  MONTAGNOLI, Alessia ,  SANTOCANALE, Corrado ,  MARTINA, Katia ,  MENICHINCHERI, Maria

IPC分类号： A61K31/444 ,  A61P35/00 ,  A61P25/28 ,  A61P31/12 ,  A61P37/00 ,  A61P13/08 ,  A61P17/06 ,  A61P9/10 ,  A61P11/00 ,  A61P19/02 ,  A61P13/12 ,  A61K45/06 ,  C07D519/00 ,  C07D471/04

CPC分类号： C07D471/04 ,  A61K31/444 ,  A61K31/4745 ,  A61K45/06 ,  A61K2300/00

摘要： Pyridylpyrrole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

公开(公告)号：EP1478357A2

公开(公告)日：2004-11-24

申请号：EP03714744.4

申请日：2003-02-18

申请人： Pharmacia Italia S.p.A.

发明人： D'ALESSIO, Roberto ,  BARGIOTTI, Alberto ,  BRASCA, Maria, Gabriella ,  ERMOLI, Antonella ,  PEVARELLO, Paolo ,  TIBOLLA, Marcellino

IPC分类号： A61K31/415 ,  C07D487/04 ,  A61P25/28 ,  A61P31/12 ,  A61P35/00

CPC分类号： C07D403/04 ,  A61K31/415 ,  C07D231/54 ,  C07D403/06 ,  C07D413/04 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04

摘要： Compounds which are tricyclic pyrazole derivatives and analogues thereof, as set forth in the specification, or pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them are disclosed; these compounds or compositions are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders.

公开(公告)号：EP1660475A1

公开(公告)日：2006-05-31

申请号：EP04763883.8

申请日：2004-08-06

申请人： Pharmacia Italia S.p.A.

发明人： VANOTTI, Ermes ,  D'ALESSIO, Roberto ,  TIBOLLA, Marcellino ,  VARASI, Mario ,  MONTAGNOLI, Alessia ,  SANTOCANALE, Corrado ,  ORSINI, Paolo ,  PILLAN, Antonio

IPC分类号： C07D401/04 ,  C07D519/00 ,  A61K31/506 ,  A61K31/52 ,  A61P35/00 ,  A61P25/28 ,  A61P31/12 ,  A61P37/00 ,  A61P13/08 ,  A61P17/06 ,  A61P9/10 ,  A61P11/00 ,  A61P19/02 ,  A61P13/12 ,  A61K45/06

CPC分类号： C07D471/04 ,  A61K31/506 ,  A61K31/513 ,  A61K31/52 ,  A61K41/00 ,  A61K45/06 ,  A61K2300/00

摘要： Pyrimidylpyrrole derivatives of formula (1) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

公开(公告)号：EP0686147B1

公开(公告)日：2002-09-25

申请号：EP95902113.0

申请日：1994-12-02

申请人： Pharmacia Italia S.p.A.

发明人： DORIA, Gianfederico ,  ISETTA, Anna, Maria ,  TIBOLLA, Marcellino ,  FORNASIERO, Maria, Chiara ,  FERRARI, Mario ,  TRIZIO, Domenico

IPC分类号： C07D207/44 ,  A61K31/40

CPC分类号： C07D207/44 ,  A61K31/40 ,  A61K31/535 ,  C07D207/36

摘要： New and known 5-[(2H-pyrrol-2-ylidene)methyl]-2,2'-bi-1H-pyrrole derivatives, having immunomodulating activity and, represented by general formula (I) wherein, subject to a proviso, R1 represents hydrogen, phenyl, C1-C20 alkyl or C2-C20 alkenyl, wherein the alkyl and alkenyl groups may be unsubstituted or substituted by 1 to 3 substituents chosen independently from halogen, C1-C6 alkoxy, hydroxy, aryl and aryloxy; R2 represents hydrogen, C1-C6 alkyl, cyano, carboxy or (C1-C6 alkoxy)carbonyl; R3 represents halogen, hydroxy or C1-C11 alkoxy unsubstituted or substituted by phenyl; R4 represents hydrogen, C1-C6 alkyl or phenyl; each or R5 and R6 independently represents hydrogen, C2-C20 alkanoyl, C3-C20 alkenoyl, phenyl, C1-C20 alkyl or C2-C20 alkenyl, wherein the alkanoyl, alkenoyl, alkyl and the alkenyl groups may be unsubstituted or substituted by 1 to 3 substituents chosen independently from halogen, C1-C6 alkoxy, hydroxy, aryl, aryloxy, cyano, carboxy, (C1-C6 alkoxy)carbonyl, (C3-C4 alkenyl)carbamoyl, aralkylcarbamoyl, arylcarbamoyl and -CONRcRd in which each of Rc and Rd independently is hydrogen or C1-C6 alkyl or Rc and Rd, taken together with the nitrogen atom to which they are linked, form a morpholino or piperidino ring; or two of R4, R5 and R6 taken together form a C4-C12 polymethylene chain, which can be unsubstituted or substituted by a C1-C12 alkyl, by a C2-C12 alkenyl or by a C1-C12 alkylidene group, wherein the alkyl, alkenyl and alkylidene groups may be in turn unsubstituted or substituted by a substituent chosen from halogen, C1-C6 alkoxy, hydroxy, cyano, carboxy, (C1-C6 alkoxy)carbonyl, aryloxy and aryl; the remaining one being hydrogen or C1-C12 alkyl; and the pharmaceutically acceptable salts thereof, are disclosed.

摘要翻译： 新的和已知的5-Ä（2H-吡咯-2-亚基）甲基-2,2'-联-1H-吡咯衍生物，具有免疫调节活性，并由以下通式（I）表示，其中， 条件是R 1表示氢，苯基，C 1 -C 20烷基或C 2 -C 20烯基，其中烷基和烯基可以是未取代的或被1至3个独立地选自卤素，C 1 -C 6烷氧基，羟基，芳基和芳氧基 ; R 2表示氢，C 1 -C 6烷基，氰基，羧基或（C 1 -C 6烷氧基）羰基; R3表示卤素，羟基或未取代或被苯基取代的C1-C11烷氧基; R4代表氢，C1-C6烷基或苯基; 每个或R 5和R 6独立地表示氢，C 2 -C 20烷酰基，C 3 -C 20链烯酰基，苯基，C 1 -C 20烷基或C 2 -C 20烯基，其中烷酰基，烯酰基，烷基和烯基可以是未取代的或被1至 3个独立地选自卤素，C 1 -C 6烷氧基，羟基，芳基，芳氧基，氰基，羧基，（C 1 -C 6烷氧基）羰基，（C 3 -C 4烯基）氨基甲酰基，芳烷基氨基甲酰基，芳基氨基甲酰基和-CONRcRd的取代基，其中Rc和 Rd独立地是与它们所连接的氮原子一起形成吗啉代或哌啶子基的氢或C 1 -C 6烷基或R c和R d， R 2，R 2，R 5和R 6一起形成C 4 -C 12多亚甲基链，其可以是未取代的或被C 1 -C 12烷基取代，被C 2 -C 12烯基或C 1 -C 12亚烷基取代，其中烷基， 烯基和亚烷基可以是未取代的或被选自卤素，C 1 -C 6烷氧基，羟基，氰基，羧基，（C 1 -C 6烷氧基）羰基，芳氧基和芳基的取代基取代。 剩余的一个是氢或C 1 -C 12烷基; 及其药学上可接受的盐。