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公开(公告)号:US5516775A
公开(公告)日:1996-05-14
申请号:US103493
申请日:1993-08-06
申请人: Jurg Zimmermann , Giorgio Caravatti
发明人: Jurg Zimmermann , Giorgio Caravatti
IPC分类号: A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/505 , A61P35/00 , A61P43/00 , C07D239/42 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D409/04 , C07D417/04 , A61K31/53 , A61K31/535 , A61K31/54
CPC分类号: A61K31/505
摘要: The invention relates to the use of known N-phenyl-2-pyrimidine derivatives for inhibiting proteinkinase C in warm-blooded animals as antitumor agents. ##STR1## The substituents in formula I are as defined in claim 1.
摘要翻译: 本发明涉及已知的N-苯基-2-嘧啶衍生物在温血动物中抑制蛋白游离酶C作为抗肿瘤剂的用途。 (I)式I中的取代基如权利要求1中所定义。
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公开(公告)号:US09763952B2
公开(公告)日:2017-09-19
申请号:US14976998
申请日:2015-12-21
申请人: Giorgio Caravatti , Sylvie Chamoin , Pascal Furet , Klemens Hogenauer , Konstanze Hurth , Karen Kammertoens , Ian Lewis , Henrik Moebitz , Alexander Baxter Smith , Nicolas Soldermann , Romain Wolf , Frederic Zecri
发明人: Giorgio Caravatti , Sylvie Chamoin , Pascal Furet , Klemens Hogenauer , Konstanze Hurth , Karen Kammertoens , Ian Lewis , Henrik Moebitz , Alexander Baxter Smith , Nicolas Soldermann , Romain Wolf , Frederic Zecri
IPC分类号: A61K31/538 , A61K31/5383 , C07D498/04 , C07D413/14 , C12Q1/25 , C12N9/12
CPC分类号: A61K31/5383 , A61K31/538 , C07D413/14 , C07D498/04 , C12N9/12 , C12Q1/25 , C12Q1/686 , Y02A50/409 , Y02A50/411
摘要: The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R1, R5, R7 and R30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
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公开(公告)号:US09458177B2
公开(公告)日:2016-10-04
申请号:US14478523
申请日:2014-09-05
申请人: Giorgio Caravatti , Robin Alec Fairhurst , Pascal Furet , Clive McCarthy , Heinrich Rueeger , Frank Hans Seiler , Frédéric Stauffer
发明人: Giorgio Caravatti , Robin Alec Fairhurst , Pascal Furet , Clive McCarthy , Heinrich Rueeger , Frank Hans Seiler , Frédéric Stauffer
IPC分类号: C07D403/04 , C07D498/04 , C07D413/14 , A61K31/5377 , A61K45/06
CPC分类号: C07D498/04 , A61K31/5377 , A61K45/06 , C07D413/14
摘要: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.
摘要翻译: 本发明涉及作为PI3K(磷脂酰肌醇-3-激酶)抑制剂的恶唑烷-2-酮取代的嘧啶化合物及其药物组合物,其制备方法和用于治疗依赖于 PI3K。
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公开(公告)号:US20090137804A1
公开(公告)日:2009-05-28
申请号:US11570983
申请日:2005-06-23
申请人: Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul W. Manley , Joseph Schoepfer , Carsten Spanka
发明人: Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul W. Manley , Joseph Schoepfer , Carsten Spanka
IPC分类号: A61K31/50 , C07D239/12 , A61P35/00
CPC分类号: C07D239/48 , C07D251/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要: The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.
摘要翻译: 本发明涉及式(I)化合物,其中取代基X1,R1,R2,R3和R4具有本发明说明书中阐述和解释的含义,制备这些化合物的方法,含有它们的药物组合物 ,其任选与一种或多种其它药学活性化合物组合用于治疗对蛋白激酶活性的抑制作出反应的疾病的用途,以及治疗这种疾病的方法。
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公开(公告)号:US20070265292A1
公开(公告)日:2007-11-15
申请号:US11828367
申请日:2007-07-26
申请人: Hans Buerger , Giorgio Caravatti , Juerg Zimmermann , Paul Manley , Werner Breitenstein , Margaret Cudd
发明人: Hans Buerger , Giorgio Caravatti , Juerg Zimmermann , Paul Manley , Werner Breitenstein , Margaret Cudd
IPC分类号: A61K31/506
CPC分类号: C07D401/04 , A61K31/506
摘要: The invention relates to N-phenyl-2-pyrimidine-amine derivatives of formula I wherein the substituents are defined as indicated in the description, to processes for the preparation thereof, to medicaments comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.
摘要翻译: 本发明涉及式I的N-苯基-2-嘧啶 - 胺衍生物,其中取代基如说明书所述定义,其制备方法,包括那些化合物的药物及其在制备 用于治疗温血动物(包括人)的药物组合物。
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公开(公告)号:US5639911A
公开(公告)日:1997-06-17
申请号:US485248
申请日:1995-06-07
申请人: Jaroslav Stanek , Jorg Frei , Giorgio Caravatti
发明人: Jaroslav Stanek , Jorg Frei , Giorgio Caravatti
IPC分类号: C07C281/12 , C07C281/18 , C07C337/08 , C07C281/00
CPC分类号: C07C337/08 , C07C281/12 , C07C281/18 , C07C2102/06 , C07C2102/08
摘要: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.
摘要翻译: 式I的化合物其中A,X,Z和R 1 -R 5如说明书中所定义,其盐具有有价值的药物性质,尤其对肿瘤有效。 它们是以本身已知的方式准备的。
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公开(公告)号:US5354761A
公开(公告)日:1994-10-11
申请号:US69660
申请日:1993-06-01
IPC分类号: A61K31/44 , A61K31/4402 , A61K31/4418 , A61P33/02 , C07D213/78 , C07D213/81 , C07D213/83 , C07D401/04
CPC分类号: C07D213/78 , C07D213/81 , C07D213/83
摘要: Compounds of formula I ##STR1## wherein Y, Z, S, S', m, n and R.sub.1 -R.sub.4 are as defined in the description, have valuable pharmaceutical properties and are effective especially against protozoal infections. They are prepared in a manner known per se.
摘要翻译: 其中Y,Z,S,S',m,n和R 1 -R 4如说明书中所定义的式I化合物(I)具有有价值的药物性质,并且尤其对抗原生动物感染是有效的。 它们是以本身已知的方式准备的。
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公开(公告)号:US5238941A
公开(公告)日:1993-08-24
申请号:US849262
申请日:1992-03-11
IPC分类号: C07C281/18 , C07C337/08 , C07D213/78 , C07D239/30 , C07D401/04
CPC分类号: C07D213/78 , C07C281/18 , C07C337/08 , C07D239/30 , C07D401/04
摘要: Compounds of formula I ##STR1## wherein A, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Y, Z and R.sub.1 to R.sub.6 have the meanings given in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.
摘要翻译: 其中A,X 1,X 2,X 3,X 4,Y,Z和R 1至R 6具有说明书中给出的含义的式I化合物(I)具有有价值的药物性质,尤其对肿瘤有效。 它们是以本身已知的方式准备的。
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公开(公告)号:US08552002B2
公开(公告)日:2013-10-08
申请号:US11570983
申请日:2005-06-23
申请人: Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul William Manley , Joseph Schoepfer , Carsten Spanka
发明人: Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul William Manley , Joseph Schoepfer , Carsten Spanka
IPC分类号: A01N43/54 , C07D239/02
CPC分类号: C07D239/48 , C07D251/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要: The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.
摘要翻译: 本发明涉及式(I)化合物,其中取代基X1,R1,R2,R3和R4具有本发明说明书中阐述和解释的含义,制备这些化合物的方法,含有它们的药物组合物 ,其任选与一种或多种其它药学活性化合物组合用于治疗对蛋白激酶活性的抑制作出反应的疾病的用途,以及治疗这种疾病的方法。
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公开(公告)号:US07855215B2
公开(公告)日:2010-12-21
申请号:US11575601
申请日:2005-09-27
申请人: Guido Bold , Giorgio Caravatti , Andreas Floersheimer , Pascal Furet , Paul W Manley , Carole Pissot Soldermann , Andrea Vaupel
发明人: Guido Bold , Giorgio Caravatti , Andreas Floersheimer , Pascal Furet , Paul W Manley , Carole Pissot Soldermann , Andrea Vaupel
IPC分类号: A61K31/505 , A61K31/506 , C07D239/02 , C07D401/12 , C07D413/12
CPC分类号: C07D417/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D417/14
摘要: The invention relates to novel compounds of Formula I: wherein p is 1, 2 or 3; n is 0, 1, 2 or 3; m is 0, 1, 2 or 3; A is CRc, S, NRc or O, where Rc is H or lower alkyl; X, Y and Z are each independently selected from N or C—R3, wherein at least two of X, Y and Z are N; and each Ra is independently selected from hydrogen and lower-alkyl; each Rb is hydrogen or lower-alkyl; G is a group Ar or represents CN or unsubstituted or substituted lower alkyl; Ar is a saturated or unsaturated cyclic group, which is substituted or unsubstituted and maybe a five or six membered monocyclic or a 8, 9, 10, 11 or 12 membered bicyclic or tricyclic ring and may contain 0, 1, 2 or 3 heteroatoms selected from O, N and S; and wherein the radicals have R1, R2, R3 and R4 have the meanings as defined herein, to salts, esters, N-oxides or prodrugs thereof; and their use in the treatment of protein kinase dependent diseases, their use in the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diary urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising these novel diaryl urea derivatives, processes for the manufacture of the novel diaryl urea derivatives, the use or methods of use of the novel diaryl urea derivatives as mentioned above, and/or these novel diaryl urea derivatives for use in the treatment of the animal or human body.
摘要翻译: 本发明涉及式I的新化合物:其中p是1,2或3; n为0,1,2或3; m为0,1,2或3; A是CRc,S,NRc或O,其中Rc是H或低级烷基; X,Y和Z各自独立地选自N或C-R 3,其中X,Y和Z中的至少两个是N; 并且每个R a独立地选自氢和低级烷基; 每个R b是氢或低级烷基; G是基团Ar或代表CN或未取代或取代的低级烷基; Ar是饱和或不饱和的环状基团,其是取代或未取代的,并且可以是五或六元单环或8,9,10,11或12元双环或三环,并且可以含有0,1,2或3个选自 来自O,N和S; 并且其中所述基团的R1,R2,R3和R4具有如本文所定义的含义,其盐,酯,N-氧化物或前药; 以及它们在治疗蛋白激酶依赖性疾病中的应用,它们在制备用于治疗所述疾病的药物组合物中的应用,用于治疗所述疾病的日用脲衍生物的使用方法,包含这些新型二芳基脲 衍生物,制备新型二芳基脲衍生物的方法,上述新型二芳基脲衍生物的使用或使用方法,和/或这些新型二芳基脲衍生物用于动物或人体的治疗。
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