公开(公告)号：US20080096883A1

公开(公告)日：2008-04-24

申请号：US11573235

申请日：2005-08-10

申请人： Giorgio Caravatti ,  Pascal Furet ,  Patricia Imbach ,  Georg Martiny-Baron ,  Lawrence Blas Perez ,  Tao Sheng

发明人： Giorgio Caravatti ,  Pascal Furet ,  Patricia Imbach ,  Georg Martiny-Baron ,  Lawrence Blas Perez ,  Tao Sheng

IPC分类号： A61K31/5375 ,  A61K31/426 ,  A61K31/47 ,  A61K31/497 ,  C07D217/00 ,  C07D239/72 ,  C07D403/00 ,  C07D413/02 ,  C07D277/62 ,  C07D237/30 ,  A61P43/00 ,  A61K31/50 ,  A61K31/517

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 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，它们作为或用于制造药物的用途，特别是作为蛋白激酶的抑制剂和/或病症，病症或疾病状态介导的治疗 通过蛋白激酶活性和/或增殖性疾病，治疗方法包括施用化合物，特别是治疗和预防治疗的化合物和新中间体的制备方法及其合成的部分步骤。

公开(公告)号：US20090306107A1

公开(公告)日：2009-12-10

申请号：US11908913

申请日：2006-03-17

申请人： Lawrence Blas Perez ,  Tao Sheng

发明人： Lawrence Blas Perez ,  Tao Sheng

IPC分类号： A61K31/519 ,  C07D471/04 ,  A61P35/00

CPC分类号： C07D471/14 ,  C07D487/04

摘要： The present invention relates to compounds that are useful to 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. The application is also 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, and with other subject matter.

摘要翻译： 本发明涉及可用于抑制，调节和/或调节酪氨酸和丝氨酸/苏氨酸激酶和激酶样蛋白质的化合物，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。 该应用还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，癌症和心脏肥大以及其它主题的方法。

公开(公告)号：US09815813B2

公开(公告)日：2017-11-14

申请号：US15110504

申请日：2015-01-16

申请人： Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Sarah Williams ,  Martin Sendzik

发明人： Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Sarah Williams ,  Martin Sendzik

IPC分类号： A61K31/4427 ,  C07D401/04 ,  C07D401/14 ,  C07D241/26 ,  C07D249/14

CPC分类号： C07D401/04 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14

摘要： The present invention relates to compounds of formula I: in which Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US08957074B2

公开(公告)日：2015-02-17

申请号：US13579359

申请日：2011-02-17

申请人： Christopher Thomas Brain ,  Young Shin Cho ,  John William Giraldes ,  Bharat Lagu ,  Julian Roy Levell ,  Michael J. Luzzio ,  Lawrence Blas Perez ,  Yaping Wang ,  Fan Yang

发明人： Christopher Thomas Brain ,  Young Shin Cho ,  John William Giraldes ,  Bharat Lagu ,  Julian Roy Levell ,  Michael J. Luzzio ,  Lawrence Blas Perez ,  Yaping Wang ,  Fan Yang

IPC分类号： A61K31/50 ,  A61K31/501 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D498/20 ,  C07D487/04 ,  C07D519/00 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08 ,  C07D498/08

CPC分类号： C07D487/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10 ,  C07D498/08 ,  C07D498/10 ,  C07D498/20 ,  C07D519/00

摘要： The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R1, R2Y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

摘要翻译： 本发明涉及新的式（I）吡咯并嘧啶化合物，其中R 1，R 2 Y，R 4，R 8 -R 11，A和L在本文中定义，并且包括其药学上可接受的盐。 本发明的化合物是CDK4 / 6抑制剂，可用于治疗由CDK4 / 6介导的疾病和病症，如癌症，包括外套细胞淋巴瘤，脂肪肉瘤，非小细胞肺癌，黑素瘤，鳞状细胞食管癌 癌症和乳腺癌。 本发明还涉及包含本发明化合物的药物组合物。 本发明还涉及抑制CDK4 / 6活性的方法以及使用本发明化合物或包含本发明化合物的药物组合物治疗与之相关的病症。

公开(公告)号：US20130131063A1

公开(公告)日：2013-05-23

申请号：US13472136

申请日：2012-05-15

申请人： Alfredo C. Castro ,  Kristopher M. Depew ,  Michael J. Grogan ,  Charles W. Johannes ,  Edward B. Holson ,  Brian T. Hopkins ,  Gregg F. Keaney ,  Nii O. Koney ,  Tao Liu ,  David A. Mann ,  Marta Nevalainen ,  Stephane Peluso ,  Lawrence Blas Perez ,  Daniel A. Snyder ,  Thomas T. Tibbitts

发明人： Alfredo C. Castro ,  Kristopher M. Depew ,  Michael J. Grogan ,  Charles W. Johannes ,  Edward B. Holson ,  Brian T. Hopkins ,  Gregg F. Keaney ,  Nii O. Koney ,  Tao Liu ,  David A. Mann ,  Marta Nevalainen ,  Stephane Peluso ,  Lawrence Blas Perez ,  Daniel A. Snyder ,  Thomas T. Tibbitts

IPC分类号： C07D261/02 ,  C07D417/12 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/496 ,  A61K31/42 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  C07D413/10 ,  C07D413/12 ,  A61K45/06

CPC分类号： C07D261/02 ,  A61K31/42 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12

摘要： The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.

摘要翻译： 本发明涉及与bcl蛋白结合并抑制Bcl功能的含异唑烷的化合物。 该化合物可用于治疗和调节与过度增生相关的疾病，例如癌症。

公开(公告)号：US20180362496A1

公开(公告)日：2018-12-20

申请号：US16117674

申请日：2018-08-30

申请人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Denise Grunenfelder ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Travis Matthew Stams ,  Sarah Williams

发明人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Denise Grunenfelder ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Travis Matthew Stams ,  Sarah Williams

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D241/26 ,  C07D471/04 ,  C07D409/14 ,  C07D239/48 ,  C07D487/04 ,  C07D403/04 ,  C07D249/14

摘要： The present invention relates to compounds of formula I: in which m, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a and R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US07169817B2

公开(公告)日：2007-01-30

申请号：US10445967

申请日：2003-05-27

申请人： Shifeng Pan ,  Nathanael S. Gray ,  Wenqui Gao ,  Klaus Hinterding ,  Sophie Lefebvre ,  Yuan Mi ,  Peter Nussbaumer ,  Wei Wang ,  Federic Zecri ,  Fan Yi ,  Lawrence Blas Perez ,  Kenneth Richad la Montagne ,  Peter Ettmayer

发明人： Shifeng Pan ,  Nathanael S. Gray ,  Wenqui Gao ,  Klaus Hinterding ,  Sophie Lefebvre ,  Yuan Mi ,  Peter Nussbaumer ,  Wei Wang ,  Federic Zecri ,  Fan Yi ,  Lawrence Blas Perez ,  Kenneth Richad la Montagne ,  Peter Ettmayer

IPC分类号： C07C211/03 ,  C07C251/32 ,  A61K31/15 ,  A61K31/137

CPC分类号： C07D263/57 ,  C07C215/28 ,  C07C215/46 ,  C07C217/54 ,  C07C237/30 ,  C07C251/48 ,  C07C255/13 ,  C07C255/43 ,  C07C255/58 ,  C07C311/08 ,  C07C2601/02 ,  C07C2601/08 ,  C07D261/08 ,  C07D317/58 ,  C07D333/20 ,  C07F9/094

摘要： The present invention relates to biphenylyl derivatives, processes for their production, their uses and pharmaceutical compositions containing them. Compounds according to the present invention are based upon the chemical formula: wherein the substituents have the values mentioned herein.

摘要翻译： 本发明涉及联苯衍生物，其制备方法及其用途和含有它们的药物组合物。 根据本发明的化合物基于以下化学式：其中取代基具有本文提及的值。

公开(公告)号：US06552065B2

公开(公告)日：2003-04-22

申请号：US09944275

申请日：2001-08-31

申请人： Stacy William Remiszewski ,  Kenneth Walter Bair ,  Richard William Versace ,  Lawrence Blas Perez ,  Michael Alan Green ,  Lidia Cristina Sambucetti ,  Sushil Sharma

发明人： Stacy William Remiszewski ,  Kenneth Walter Bair ,  Richard William Versace ,  Lawrence Blas Perez ,  Michael Alan Green ,  Lidia Cristina Sambucetti ,  Sushil Sharma

IPC分类号： A61K3140

CPC分类号： C07D401/12 ,  C04B35/632 ,  C07C259/06 ,  C07D209/16 ,  C07D233/64 ,  C07D295/155 ,  C07D307/81 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04

摘要： The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.

公开(公告)号：US20170204080A1

公开(公告)日：2017-07-20

申请号：US15110498

申请日：2015-01-16

申请人： Christine Hiu-tung CHEN ,  Zhuoliang CHEN ,  Jorge Garcia FORTANET ,  Denise GRUNENFELDER ,  Rajesh KARKI ,  Mitsunori KATO ,  Matthew J. LAMARCHE ,  Lawrence Blas PEREZ ,  Travis Matthew STAMS ,  Sarah WILLIAMS

发明人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Denise Grunenfelder ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Travis Matthew Stams ,  Sarah Williams

IPC分类号： C07D401/04 ,  C07D487/04 ,  C07D403/04 ,  C07D401/14 ,  C07D409/14 ,  C07D471/04

CPC分类号： C07D401/04 ,  C07D239/48 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04

摘要： The present invention relates to compounds of formula I: in which m, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a and R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US20170015680A1

公开(公告)日：2017-01-19

申请号：US15110511

申请日：2015-01-16

申请人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Troy Douglas Smith ,  Sarah Williams ,  John William Giraldes ,  Martin Sendzik ,  Bakary-Barry Toure

发明人： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Troy Douglas Smith ,  Sarah Williams ,  John William Giraldes ,  Martin Sendzik ,  Bakary-Barry Toure

IPC分类号： C07D498/10 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10 ,  C07D401/04 ,  C07D401/14

CPC分类号： C07D498/10 ,  C07B2200/07 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10

摘要： The present invention relates to compounds of formula I: in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

摘要翻译： 其中p，q，Y1，Y2，R1，R2a，R2b，R3a，R3b，R4a，R4b，R5a，R5b，R7和R8定义在发明概述中; 能够抑制SHP2的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物来管理与SHP2的异常活性相关的疾病或病症的方法。