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1. 发明授权

US08552002B2 Compounds and compositions as protein kinase inhibitors 有权
标题翻译：化合物和组合物作为蛋白激酶抑制剂
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。

2. 发明授权

US07855215B2 Cyclic diaryl ureas suitable as tyrosine kinase inhibitors 失效
标题翻译：适合作为酪氨酸激酶抑制剂的环状二芳基脲
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。

3. 发明申请

US20100305113A1 Substituted Imidazopyridazines as Lipid Kinase Inhibitors 审中-公开
标题翻译：取代的咪唑并哒嗪作为脂质激酶抑制剂
公开(公告)号：US20100305113A1
公开(公告)日：2010-12-02
申请号：US12599131
申请日：2008-05-07
申请人： Hans-Georg Capraro , Patricia Imbach , Giorgio Caravatti , Pascal Furet
发明人： Hans-Georg Capraro , Patricia Imbach , Giorgio Caravatti , Pascal Furet
IPC分类号： A61K31/542 , C07D487/04 , A61K31/5025 , A61K31/5377 , A61P35/00 , A61P29/00 , A61P37/08 , A61P9/00
CPC分类号： C07D487/04
摘要： The invention relates to novel compounds of the formula I, as well as other invention embodiments related to these compounds. The compounds are e.g. useful in the treatment of the animal or human body in view of their ability to inhibit protein kinases such as especially PI3 kinase.
摘要翻译：本发明涉及式I的新化合物以及与这些化合物有关的其它发明实施方案。化合物是例如鉴于其抑制蛋白激酶（例如PI3激酶）的能力，可用于动物或人体的治疗。

4. 发明授权

US07691855B2 Phenyl-[4-(3-phenyl-1h-pyrazol-4-yl)-pyrimidin-2-yl)-amine derivatives 失效
标题翻译：苯基 - [4-（3-苯基-1H-吡唑-4-基） - 嘧啶-2-基） - 胺衍生物
公开(公告)号：US07691855B2
公开(公告)日：2010-04-06
申请号：US10520567
申请日：2003-07-08
申请人： Pascal Furet , Patricia Imbach , Timothy Michael Ramsey , Achim Schlapbach , Dieter Scholz , Giorgio Caravatti
发明人： Pascal Furet , Patricia Imbach , Timothy Michael Ramsey , Achim Schlapbach , Dieter Scholz , Giorgio Caravatti
IPC分类号： C07D403/04 , A61K31/505
CPC分类号： C07D403/04 , A61K31/505
摘要： The invention relates to phenyl-[4-(3-phenyl-1H-pyrazol-4-yl)-pyrimidin-2-yl]-amine derivatives and to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumor.
摘要翻译：本发明涉及苯基 - [4-（3-苯基-1H-吡唑-4-基） - 嘧啶-2-基] - 胺衍生物及其制备方法，涉及包含这些衍生物的药物组合物及其用途的这样的衍生物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗特别是增殖性疾病例如肿瘤的药物组合物。

5. 发明申请

US20090069360A1 Organic Compounds 审中-公开
标题翻译：有机化合物
公开(公告)号：US20090069360A1
公开(公告)日：2009-03-12
申请号：US12293257
申请日：2007-03-14
申请人： David Bryant Batt , Rene Beerli , Guido Bold , Giorgio Caravatti , Timothy Michael Ramsey
发明人： David Bryant Batt , Rene Beerli , Guido Bold , Giorgio Caravatti , Timothy Michael Ramsey
IPC分类号： A61K31/506 , C07D401/04 , A61P35/00
CPC分类号： C07D401/04
摘要： The present invention relates to the discovery that certain compounds inhibit, regulate and/or modulate tyrosine and serine/threonine kinase and kinase-like proteins, such as RAF kinase, a serine/threonine kinase that functions in the MAP kinase signaling pathway, and is concerned with compositions which contain these compounds, and methods of using them to treat tyrosine and serine/threonine kinase and kinase-like dependent diseases, such as angiogenesis, cancer and cardiac hypertrophy.
摘要翻译：本发明涉及某些化合物抑制，调控和/或调节酪氨酸和丝氨酸/苏氨酸激酶和激酶样蛋白质，例如在MAP激酶信号通路中起作用的丝氨酸/苏氨酸激酶的RAF激酶，并且是涉及含有这些化合物的组合物，以及使用它们治疗酪氨酸和丝氨酸/苏氨酸激酶和激酶样依赖性疾病如血管生成，癌症和心脏肥大的方法。

6. 发明申请

US20080262021A1 1H-Imidazoquinoline Derivatives as Prote In Kinase Inhibitors 审中-公开
标题翻译： 1H-咪唑并喹啉衍生物作为激酶抑制剂中的蛋白质
公开(公告)号：US20080262021A1
公开(公告)日：2008-10-23
申请号：US10579587
申请日：2004-11-19
申请人： Hans-Georg Capraro , Giorgio Caravatti , Pascal Furet , Carlos Garcia-Echeverria , Patricia Imbach , Frederic Stauffer
发明人： Hans-Georg Capraro , Giorgio Caravatti , Pascal Furet , Carlos Garcia-Echeverria , Patricia Imbach , Frederic Stauffer
IPC分类号： A61K31/4745 , C07D471/04 , A61P35/04
CPC分类号： C07D471/04
摘要： The invention relates to imidazoquinolines of formula (I) for use in the treatment of protein kinase dependent diseases; pharmaceutical preparations comprising an imidazoquinoline, especially for the treatment of a protein kinase dependent disease; novel imidazoquinolines; and a process for the preparation of the novel imidazoquinolines.
摘要翻译：本发明涉及用于治疗蛋白激酶依赖性疾病的式（I）的咪唑并喹啉; 包含咪唑并喹啉的药物制剂，特别是用于治疗蛋白激酶依赖性疾病; 新型咪唑并喹啉; 以及制备新的咪唑并喹啉的方法。

7. 发明授权

US07323469B2 7H-pyrrolo[2,3-d]pyrimidine derivatives 失效
标题翻译： 7H-吡咯并[2,3-d]嘧啶衍生物
公开(公告)号：US07323469B2
公开(公告)日：2008-01-29
申请号：US10783000
申请日：2004-02-20
申请人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Peter Traxler
发明人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Peter Traxler
IPC分类号： A61K31/519 , A61K31/497 , C07D487/04 , A61P35/04
CPC分类号： C07D487/04
摘要： The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumor.
摘要翻译：本发明涉及式I的7H-吡咯并[2,3-d]嘧啶衍生物，其中符号和取代基如说明书中所定义，其制备方法，包含该衍生物的药物组合物及其用途衍生物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗特别是增殖性疾病如肿瘤的药物组合物。

8. 发明授权

US07081532B2 N-phenyl-2-pyrimidine-amine derivatives 有权
标题翻译： N-苯基-2-嘧啶 - 胺衍生物
公开(公告)号：US07081532B2
公开(公告)日：2006-07-25
申请号：US10363841
申请日：2001-09-11
申请人： Hans M Buerger , Giorgio Caravatti , Juerg Zimmermann , Paul W Manley , Werner Breitenstein , Margaret A Cudd
发明人： Hans M Buerger , Giorgio Caravatti , Juerg Zimmermann , Paul W Manley , Werner Breitenstein , Margaret A Cudd
IPC分类号： C07D403/10
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 in the description, to processes for the preparation thereof, to medicaments comprising those compounds, and 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中所定义，其制备方法，含有这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。

9. 发明申请

US20060035897A1 Trifluoromethyl substituted benzamides as kinase inhibitors 审中-公开
标题翻译：三氟甲基取代的苯甲酰胺作为激酶抑制剂
公开(公告)号：US20060035897A1
公开(公告)日：2006-02-16
申请号：US11201348
申请日：2005-08-10
申请人： Giorgio Caravatti , Pascal Furet , Patricia Imbach , Georg Martiny-Baron , Lawrence Perez , Tao Sheng
发明人： Giorgio Caravatti , Pascal Furet , Patricia Imbach , Georg Martiny-Baron , Lawrence Perez , Tao Sheng
IPC分类号： A61K31/502 , A61K31/517 , A61K31/47 , A61K31/428
CPC分类号： C07D277/62 , C07D217/02 , C07D237/30 , C07D239/74 , C07D239/84
摘要： The invention relates to trifluoromethyl substituted benzamide compounds of the formula I, pharmaceuticals comprising these compounds, their use as or for the manufacture of pharmaceuticals, particularly as inhibitors of protein kinases, especially of ephrin receptor kinases, and/or the treatment of a condition, disorder or disease state mediated by a protein kinase activity and/or a proliferative disease, methods of treatment comprising administering the compounds, especially of therapeutic and prophylactic treatment, methods for the manufacture of the compounds and novel intermediates and partial steps for their synthesis.
摘要翻译：本发明涉及式I的三氟甲基取代的苯甲酰胺化合物，包含这些化合物的药物，它们作为药物的用途或用于制造药物，特别是作为蛋白激酶抑制剂，特别是ephrin受体激酶的抑制剂和/或治疗病症，由蛋白激酶活性和/或增殖性疾病介导的紊乱或疾病状态，治疗方法包括施用化合物，特别是治疗和预防性治疗化合物和新中间体的制备方法及其合成的部分步骤。

10. 发明授权

US09763952B2 Dihydro-benzo-oxazine and dihydro-pyrido-oxazine derivatives 有权
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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