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1. 发明公开

EP0549348A1 Arylidene-heterocyclic derivatives, process for their preparation and their use as tyrisine kinase inhibitors 失效
标题翻译： Arylidenes杂环衍生物，它们的制备方法和它们作为Tyrisine激酶抑制剂的用途。
公开(公告)号：EP0549348A1
公开(公告)日：1993-06-30
申请号：EP92311767.5
申请日：1992-12-23
申请人： PHARMACIA S.p.A.
发明人： Buzzetti, Franco , Fustinoni, Silvia , Brasca, Maria Gabriella , Penco, Sergio
IPC分类号： C07D217/24 , C07D275/06 , C07D417/06 , C07D401/06 , A61K31/47 , A61K31/425
CPC分类号： C07D275/06 , C07D217/24 , C07D401/06 , C07D417/06
摘要： The invention relates to compounds of formula

wherein
Ar is mono-or bicyclic ring system chosen from benzene, naphthalene, tetrahydronaphthalene, quinoline and indole; Het is

R is hydrogen, halogen, hydroxy, C₁-C₆ alkoxy, C₂-C₆ acyloxy, cyano, nitro, amino or -COOR₃ in which R₃ is hydrogen or C₁-C₆ alkyl;
R₁ is hydrogen, hydroxy, C₁-C₆ alkyl, C₁-C₆ alkoxy, C₂-C₆ acyloxy, cyano, nitro, amino or -COOR₃ in which R₃ is as defined above;
R₂ is hydrogen, halogen, hydroxy or C₁-C₆ alkyl; and the pharmaceutically acceptable salts thereof, and wherein when at the same time the (Ar) R₁ R₂ group represents unsubstituted phenyl or 4-chloro-, 4-cyano-, 4-amino- or 3,4-dimethoxy-phenyl and Het is a 4-homophthalimide group, then R is other than hydrogen, which are useful as anti-proliferative agents.
摘要翻译：本发明涉及式I的化合物 worin Ar是单或从苯，萘，四氢萘，喹啉和吲哚选择二环环系; Het是 R是氢，卤素，羟基，C1-C6烷氧基，C2-C6酰氧基，氰基，硝基，氨基或-COOR 3，其中R 3为氢或C1-C6烷基; R1是氢，羟基，C1-C6烷基，C1-C6烷氧基，C2-C6酰氧基，氰基，硝基，氨基或-COOR 3，其中R 3如以上所定义; R2是氢，卤素，羟基或C1-C6烷基; 和其药学上可接受的盐，并在同一时间worin当（Ar）的R 1基团R2 darstellt unsubstituiertem苯基或4-氯，4-氰基，4-氨基或3,4-二甲氧基 - 苯基和Het是 4- homophthalimide基，则R不是氢，其是作为抗增殖剂的其它。

2. 发明公开

EP0558950A1 3-aryl-glycidic ester derivatives and process for their preparation 失效
标题翻译： 3-Aryl-Glycidsäureester和Verfahren zu ihrer Herstellung。
公开(公告)号：EP0558950A1
公开(公告)日：1993-09-08
申请号：EP93101767.7
申请日：1993-02-05
申请人： PHARMACIA S.p.A.
发明人： Buzzetti, Franco , Brasca, Maria Gabriella , Fustinoni, Silvia , Penco, Sergio
IPC分类号： C07D303/48 , C07D405/04 , A61K31/335 , A61K31/40 , A61K31/47
CPC分类号： C07D405/04 , C07D303/48
摘要： The present invention relates to 3-aryl-oxirane derivatives of formula

wherein
Ar is a mono- or bicyclic ring system chosen from naphthalene, 5', 6', 7', 8'-tetrahydronaphthalene, quinoline and indole;
each of R and R₁ independently is hydrogen or a substituent chosen from halogen, hydroxy, C₁-C₆ alkyl, C₁-C₆ alkoxy, C₂-C₆ acyloxy, cyano and nitro;
one of X and Y is hydrogen, cyano, -COOR₂ or -CONR₃R₄ in which R₂ is C₁-C₆ alkyl and each of R₃ and R₄ independently is hydrogen or C₁-C₆ alkyl, and the other one of X and Y independently is cyano, -COOR₂ or CONR₃R₄ wherein R₂, R₃ and R₄ are as defined above, and the pharmaceutically acceptable salts thereof, which are useful in therapy as tyrosine kinase inhibitors,in particular as anti-proliferative agents and in the treatment of coronary artery disease.
摘要翻译：本发明涉及式的3-芳基 - 环氧乙烷衍生物，其中Ar是选自萘，5'，6'，7'，8'-四氢萘，喹啉和吲哚的单环或双环体系; R和R 1各自独立地是氢或选自卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 2 -C 6酰氧基，氰基和硝基的取代基; X和Y中的一个是氢，氰基，-COOR 2或-CONR 3 R 4，其中R 2是C 1 -C 6烷基，R 3和R 4各自独立地是氢或C 1 -C 6烷基，X和Y中的另一个独立地是氰基， -COOR2或CONR3R4，其中R2，R3和R4如上定义，及其药学上可接受的盐，其可用于治疗作为酪氨酸激酶抑制剂，特别是作为抗增殖剂和用于治疗冠状动脉疾病。

3. 发明公开

EP0525472A2 Methylen-oxindole derivatives and process for their preparation 失效
标题翻译：亚甲基氧化酶和维生素
公开(公告)号：EP0525472A2
公开(公告)日：1993-02-03
申请号：EP92111757.8
申请日：1992-07-10
申请人： PHARMACIA S.p.A.
发明人： Buzzetti, Franco , Longo, Antonio , Colombo, Maristella
IPC分类号： C07D403/06 , C07D209/30 , A61K31/40 , A61K31/405
CPC分类号： C07D209/34
摘要： The invention provides new methylen-indole derivatives of formula (I)

wherein

R is a group

in which
R 4 is hydrogen, hydroxy, C 1 -C 6 alkoxy, C 2 -C 6 alkanoyloxy, carboxy, nitro or NHR 7 , wherein R 7 is hydrogen or C 1 -C 6 alkyl;
R 5 is hydrogen, C 1 -C 6 alkyl or halogen; and
R 6 is hydrogen or C 1 -C 6 alkyl;
n is zero, 1 or 2;
R 1 is hydrogen, C 1 -C 6 alkyl or C 2 -C 6 alkanoyl;
R 2 is hydrogen, C 1 -C 6 alkyl, halogen, cyano, carboxyl, nitro or -NHR 7 in which R 7 is as defined above;
R 3 is hydrogen, C 1 -C 6 alkyl or C 2 -C 6 alkanoyl; and

the pharmaceutically acceptable salts thereof; and wherein, when,at the same time, R 2 is hydrogen, C 1 -C 6 alkyl, halogen or cyano and R 3 is hydrogen, R 1 and n being as defined above, then at least one of R 4 , R 5 and R 6 is other than hydrogen, which are useful as tyrosine kinase inhibitors.
摘要翻译：本发明提供新的式（I）亚甲基 - 吲哚衍生物，其中R是一个基团，其中R 4是氢，羟基，C 1 -C 6烷氧基，C 2 -C 6烷酰氧基，羧基，硝基或NHR 7，其中R 7 是氢或C 1 -C 6烷基; R5是氢，C1-C6烷基或卤素; R6为氢或C1-C6烷基; n为零，1或2; R1是氢，C1-C6烷基或C2-C6烷酰基; R2是氢，C1-C6烷基，卤素，氰基，羧基，硝基或-NHR7，其中R7如上定义; R3是氢，C1-C6烷基或C2-C6烷酰基; 及其药学上可接受的盐; 并且其中当R2同时为氢时，C1-C6烷基，卤素或氰基，R3为氢，R1和n定义如上，则R4，R5和R6中的至少一个不是氢，其可用作酪氨酸激酶抑制剂。

4. 发明授权

EP0558950B1 3-aryl-glycidic ester derivatives and process for their preparation 失效
标题翻译： 3-芳基缩水甘油酸酯，以及它们的制备方法
公开(公告)号：EP0558950B1
公开(公告)日：1996-12-04
申请号：EP93101767.7
申请日：1993-02-05
申请人： PHARMACIA S.p.A.
发明人： Buzzetti, Franco , Brasca, Maria Gabriella , Fustinoni, Silvia , Penco, Sergio
IPC分类号： C07D303/48 , C07D405/04 , A61K31/335 , A61K31/40 , A61K31/47
CPC分类号： C07D405/04 , C07D303/48

5. 发明公开

EP0662473A1 2-Oxindole derivatives as tyrosine kinase inhibitors 失效
标题翻译： 2-Oxindolderivate als酪氨酸激酶抑制剂。
公开(公告)号：EP0662473A1
公开(公告)日：1995-07-12
申请号：EP95102495.9
申请日：1991-02-26
申请人： PHARMACIA S.p.A.
发明人： Buzzetti, Franco , Longo, Antonio , Colombo, Maristella
IPC分类号： C07D209/34 , A61K31/40 , C07D401/06
CPC分类号： C07D215/227 , C07C59/52 , C07C59/54 , C07C235/34 , C07C255/36 , C07C255/41 , C07C327/44 , C07C2602/10 , C07D209/34 , C07D215/14 , C07D215/20 , C07D215/233 , C07D215/26 , C07D401/06 , C07D403/06
摘要： A compound of general formula (I)

wherein

Y is a bicyclic ring system chosen from (B), (A), (E), (F) and (G)

R is

R₁ is hydrogen, C₁-C₆ alkyl or C₂-C₆ alkanoyl;
R₂ is hydrogen, halogen, cyano or C₁-C₆ alkyl;
n is zero or an integer of 1 to 3: n is zero or an integer of 1 to 3 when Y is a ring system (A), whereas it is zero, 1 or 2 when Y is a ring system (B), (E), (F) or (G); and the pharmaceutically acceptable salts thereof; and wherein each of the substituents R, OR₂ and R₂ may be independently on either of the aryl or eteroaryl moieties of the bicyclic ring system (A), (E), (F) and (G), whereas only the benzene moiety may be substituted in the bicyclic ring (B).

The compounds of the present invention possess specific tyrosine kinase inhibiting activity. Hence they can be useful in the treatment of cancer and other pathological proliferative conditions.
摘要翻译：通式（I）的化合物其中Y是选自（B），（A），（E），（F）和（G）的化合物。，C 1 -C 6烷基或C 2 -C 6烷酰基; R2是氢，卤素，氰基或C1-C6烷基; 当Y为环状体系（A）时，n为0或1〜3的整数，n为0或1〜3的整数，Y为环状体系（B）时为0或1， E），（F）或（G）; 及其药学上可接受的盐; 并且其中取代基R，OR 2和R 2中的每一个可以独立地在二环系统（A），（E），（F）和（G）的芳基或芳基部分的任一个上，而只有苯部分可以是在双环（B）中被取代。本发明的化合物具有特异的酪氨酸激酶抑制活性。因此，它们可用于治疗癌症和其他病理性增殖病症。

6. 发明公开

EP0525472A3 Methylen-oxindole derivatives and process for their preparation 失效
标题翻译：甲氧基衍生物及其制备方法
公开(公告)号：EP0525472A3
公开(公告)日：1993-02-24
申请号：EP92111757.8
申请日：1992-07-10
申请人： PHARMACIA S.p.A.
发明人： Buzzetti, Franco , Longo, Antonio , Colombo, Maristella
IPC分类号： C07D403/06 , C07D209/30 , A61K31/40 , A61K31/405
CPC分类号： C07D209/34
摘要： The invention provides new methylen-indole derivatives of formula (I)

wherein
R is a group

in which R 4 is hydrogen, hydroxy, C 1 -C 6 alkoxy, C 2 -C 6 alkanoyloxy, carboxy, nitro or NHR 7 , wherein R 7 is hydrogen or C 1 -C 6 alkyl; R 5 is hydrogen, C 1 -C 6 alkyl or halogen; and R 6 is hydrogen or C 1 -C 6 alkyl; n is zero, 1 or 2; R 1 is hydrogen, C 1 -C 6 alkyl or C 2 -C 6 alkanoyl; R 2 is hydrogen, C 1 -C 6 alkyl, halogen, cyano, carboxyl, nitro or -NHR 7 in which R 7 is as defined above; R 3 is hydrogen, C 1 -C 6 alkyl or C 2 -C 6 alkanoyl; and
the pharmaceutically acceptable salts thereof; and wherein, when,at the same time, R 2 is hydrogen, C 1 -C 6 alkyl, halogen or cyano and R 3 is hydrogen, R 1 and n being as defined above, then at least one of R 4 , R 5 and R 6 is other than hydrogen, which are useful as tyrosine kinase inhibitors.

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