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91. 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。

92. 发明申请

US20130237519A1 BICYCLIC HETEROCYCLE DERIVATIVES FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION 有权
公开(公告)号：US20130237519A1
公开(公告)日：2013-09-12
申请号：US13599267
申请日：2012-08-30
申请人： Ian Bruce , Sylvie Chamoin , Stephen Paul Collingwood , Pascal Furet , Vikki Furminger , Diana Janus , Sarah Lewis , Jon Christopher Loren , Valentina Molteni , Alex Michael Saunders , Duncan Shaw , Lilya Sviridenko , Christopher Thomson , Ryan West , Vince Yeh
发明人： Ian Bruce , Sylvie Chamoin , Stephen Paul Collingwood , Pascal Furet , Vikki Furminger , Diana Janus , Sarah Lewis , Jon Christopher Loren , Valentina Molteni , Alex Michael Saunders , Duncan Shaw , Lilya Sviridenko , Christopher Thomson , Ryan West , Vince Yeh
IPC分类号： C07D471/04 , A61K31/4545 , A61K31/444 , A61K45/06 , A61K31/5377 , A61K31/496
CPC分类号： C07D471/04 , A61K31/444 , A61K31/4545 , A61K31/4745 , A61K31/496 , A61K31/5377 , A61K45/06
摘要： Bicyclic heterocyclic derivatives of formula I useful in inhibiting PDGF receptor mediated biological activity. wherein A is and R1, R1a, R2, R3, R4, R5, R6 and X are as defined herein.

93. 发明授权

US08440693B2 Substituted isoquinolinones and quinazolinones 有权
标题翻译：取代的异喹啉酮和喹唑啉酮
公开(公告)号：US08440693B2
公开(公告)日：2013-05-14
申请号：US12973474
申请日：2010-12-20
申请人： Joerg Berghausen , Nicole Buschmann , Pascal Furet , François Gessier , Joanna Hergovich Lisztwan , Philipp Holzer , Edgar Jacoby , Joerg Kallen , Keiichi Masuya , Carole Pissot Soldermann , Haixia Ren , Stefan Stutz
发明人： Joerg Berghausen , Nicole Buschmann , Pascal Furet , François Gessier , Joanna Hergovich Lisztwan , Philipp Holzer , Edgar Jacoby , Joerg Kallen , Keiichi Masuya , Carole Pissot Soldermann , Haixia Ren , Stefan Stutz
IPC分类号： A01N37/18 , A61K31/65 , C07D215/00
CPC分类号： C07D239/82 , C07D217/24 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I) wherein Z is CH2 or N—R4 and X, R1, R2, R4, R6, R7 and n 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 MDM2 and/or MDM4, or variants thereof.
摘要翻译：本发明涉及式（I）的取代的含氮双环杂环，其中Z是CH 2或N-R 4，X，R 1，R 2，R 4，R 6，R 7和n如说明书中所定义。这些化合物适用于治疗由MDM2和/或MDM4或其变体的活性介导的病症或疾病。

94. 发明授权

US08431592B2 1,3-dihydro-imidazo[4,5-c]quinolin-2-ones as lipid kinase inhibitors 有权
标题翻译： 1,3-二氢 - 咪唑并[4,5-c]喹啉-2-酮作为脂质激酶抑制剂
公开(公告)号：US08431592B2
公开(公告)日：2013-04-30
申请号：US13165144
申请日：2011-06-21
申请人： Carlos Garcia-Echeverria , Frederic Stauffer , Pascal Furet
发明人： Carlos Garcia-Echeverria , Frederic Stauffer , Pascal Furet
IPC分类号： A61K31/4188
CPC分类号： C07D471/04
摘要： The invention relates to methods of treatment of a proliferative disease which responds to inhibition of PI3-Kinase-related protein kinases, particularly the PI3-kinase, by administration of a novel organic compound of formula (I) to a human or animal requiring such treatment; and methods of treatment of inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease, by administration of such compound.
摘要翻译：本发明涉及通过向需要这种治疗的人或动物施用式（I）的新型有机化合物来治疗对PI3-激酶相关蛋白激酶，特别是PI3激酶的抑制作用的增殖性疾病的治疗方法 ; 以及通过施用该化合物治疗炎性或阻塞性气道疾病如哮喘，通常与移植相关的疾病或增生性疾病如肿瘤疾病的治疗方法。

95. 发明申请

US20130085161A1 PIPERIDINYL SUBSTITUTED 1,3-DIHYDRO-BENZOIMIDAZOL-2-YLIDENEAMINE DERIVATIVES 审中-公开
标题翻译：哌啶基取代的1,3-二氢苯并咪唑-2-甲酰胺衍生物
公开(公告)号：US20130085161A1
公开(公告)日：2013-04-04
申请号：US13704380
申请日：2011-06-16
申请人： Frederic Berst , Pascal Furet , Andreas Marzinzik , Frederic Stauffer
发明人： Frederic Berst , Pascal Furet , Andreas Marzinzik , Frederic Stauffer
IPC分类号： C07D401/04 , A61K31/4545 , C07D401/14 , A61K31/454 , A61K45/06
CPC分类号： C07D401/04 , A61K31/454 , A61K31/4545 , A61K45/06 , C07D401/14
摘要： The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of one or more IGF-1R mediated disorders or diseases.
摘要翻译：本发明涉及式（I）的新衍生物，其中取代基如说明书中所定义; 制备此类衍生物的方法; 包含这些衍生物的药物组合物; 这种衍生物作为药物; 用于治疗一种或多种IGF-1R介导的病症或疾病的衍生物。

96. 发明授权

US08030311B2 Phenylacetamides suitable as protein kinase inhibitors 失效
标题翻译：苯乙酰胺适合作为蛋白激酶抑制剂
公开(公告)号：US08030311B2
公开(公告)日：2011-10-04
申请号：US11914895
申请日：2006-04-12
申请人： Guido Bold , Pascal Furet , Vito Guagnano , Clive McCarthy , Andrea Vaupel
发明人： Guido Bold , Pascal Furet , Vito Guagnano , Clive McCarthy , Andrea Vaupel
IPC分类号： A61K31/497 , A61K31/44 , C07D401/12 , C07D471/02
CPC分类号： C07D235/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D473/00
摘要： The invention relates to compounds of the formula (I) wherein the moieties R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, and salts thereof, as well as their use, methods of use for them and method of their synthesis, and the like. The compounds are protein kinase inhibitors and can, inter alia, be used in the treatment of various proliferative diseases.
摘要翻译：本发明涉及式（I）化合物，其中部分R 1，R 2，R 3，R 9，R 10和Q和X，Y和Z如说明书中所定义，及其盐，以及它们的用途，用于它们及其合成方法等。这些化合物是蛋白激酶抑制剂，尤其可用于治疗各种增殖性疾病。

97. 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。

98. 发明授权

US07652022B2 Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases 失效
标题翻译：用于治疗蛋白激酶依赖性疾病的二芳基脲衍生物
公开(公告)号：US07652022B2
公开(公告)日：2010-01-26
申请号：US10515113
申请日：2003-05-28
申请人： Andreas Floersheimer , Pascal Furet , Paul William Manley , Guido Bold , Eugen Boss , Vito Guagnano , Andrea Vaupel
发明人： Andreas Floersheimer , Pascal Furet , Paul William Manley , Guido Bold , Eugen Boss , Vito Guagnano , Andrea Vaupel
IPC分类号： A01N43/54 , A01N43/40 , A61K31/505 , A61K31/44 , C07D239/02
CPC分类号： C07D213/40 , A61K31/33 , A61K31/395 , C07D213/38 , C07D213/64 , C07D213/68 , C07D213/69 , C07D213/81 , C07D213/84 , C07D213/89 , C07D239/34 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/52 , C07D401/04 , C07D401/12 , C07D403/12
摘要： The invention relates to the use of diaryl urea derivatives in the treatment of protein kinase dependent diseases or for the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diaryl urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising diaryl urea derivatives for the treatment of said diseases, diaryl urea derivatives for use in the treatment of said diseases, novel diaryl urea derivatives, 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：本发明涉及二芳基脲衍生物在治疗蛋白激酶依赖性疾病或用于制备用于治疗所述疾病的药物组合物中的用途，二芳基脲衍生物在治疗所述疾病中的应用方法，药物制剂包括用于治疗所述疾病的二芳基脲衍生物，用于治疗所述疾病的二芳基脲衍生物，新型二芳基脲衍生物，包含这些新型二芳基脲衍生物的药物制剂，制备新型二芳基脲衍生物的方法，或使用上述新型二芳基脲衍生物的方法，和/或这些新型二芳基脲衍生物用于动物或人体的治疗。

99. 发明申请

US20100009978A1 Benzoxazoles and Oxazolopyridines Being Useful as Janus Kinases Inhibitors 失效
标题翻译：苯并恶唑和唑吡吉因作为Janus激酶抑制剂有用
公开(公告)号：US20100009978A1
公开(公告)日：2010-01-14
申请号：US12440298
申请日：2007-09-13
申请人： Marc Gerspacher , Pascal Furet , Eric Vangrevelinghe
发明人： Marc Gerspacher , Pascal Furet , Eric Vangrevelinghe
IPC分类号： A61K31/423 , C07D263/58 , C07D413/14 , C07D417/14 , A61K31/5377 , A61K31/541 , A61P35/00
CPC分类号： C07D263/58 , C07D413/04
摘要： The invention relates to 2,7-disubstituted benzoxazole and 2,4-disubstituted oxazolo[5,4-c]pyridine compounds of the formula I given below, as well as salts thereof, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, these compounds for use in the treatment (including prophylaxis) of the animal, especially human, body (especially with regard to a proliferative disease), the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a protein tyrosine kinase mediated disease (such as a tumor disease) or for the manufacture of a pharmaceutical preparation for use in the treatment of such a disease, a method for the treatment of such a disease and a pharmaceutical preparation for the treatment of a disease as mentioned. The compounds are of the formula I, wherein the symbols are as defined in the description. The compounds inhibit, for example, JAK2 and JAK3.
摘要翻译：本发明涉及以下给出的式I的2,7-二取代苯并恶唑和2,4-二取代的恶唑并[5,4-c]吡啶化合物及其盐，其制备方法及其在用于治疗人或动物体的方法，这些化合物用于动物，特别是人体（特别是关于增殖性疾病）的治疗（包括预防）中，单独使用或与一种或更多其它药物活性化合物 - 用于治疗特别是蛋白质酪氨酸激酶介导的疾病（例如肿瘤疾病）或用于制备用于治疗这种疾病的药物制剂的治疗方法用于治疗所述疾病的疾病和药物制剂。所述化合物具有式I，其中符号如说明书中所定义。该化合物抑制例如JAK2和JAK3。

100. 发明申请

US20090258882A1 2,4-Substituted Quinazolines as Lipid Kinase Inhibitors 审中-公开
标题翻译： 2,4-取代喹唑啉作为脂质激酶抑制剂
公开(公告)号：US20090258882A1
公开(公告)日：2009-10-15
申请号：US12375450
申请日：2007-07-25
申请人： Frederic Stauffer , Pascal Furet
发明人： Frederic Stauffer , Pascal Furet
IPC分类号： A61K31/496 , C07D401/06 , A61K31/517 , A61P35/00 , A61P29/00 , A61P11/00 , A61P37/08 , A61P37/06 , C07D239/72
CPC分类号： C07D239/74 , C07D239/84 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D409/04 , C07D409/14
摘要： The invention relates to compounds of the formula I, which are appropriate for the treatment of kinase, e.g. PI3K-related, diseases, such as proliferative diseases, inflammatory diseases, obstructive airways disorders and transplantation related diseases.
摘要翻译：本发明涉及式I化合物，其适用于治疗激酶，例如， PI3K相关疾病，如增生性疾病，炎性疾病，阻塞性气道疾病和移植相关疾病。

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