公开(公告)号：US20140275083A1

公开(公告)日：2014-09-18

申请号：US14208015

申请日：2014-03-13

Applicant: Thomas Raymond CAFERRO ,  Zhuoliang CHEN ,  Young Shin CHO ,  Abran Q. COSTALES ,  Julian Roy LEVELL ,  Gang LIU ,  James R. MANNING ,  Martin SENDZIK ,  Cynthia SHAFER ,  Michael David SHULTZ ,  James SUTTON ,  Yaping WANG ,  Qian ZHAO

Inventor： Thomas Raymond CAFERRO ,  Zhuoliang CHEN ,  Young Shin CHO ,  Abran Q. COSTALES ,  Julian Roy LEVELL ,  Gang LIU ,  James R. MANNING ,  Martin SENDZIK ,  Cynthia SHAFER ,  Michael David SHULTZ ,  James SUTTON ,  Yaping WANG ,  Qian ZHAO

IPC: C07D413/04 ,  A61K31/5377 ,  C07D417/14 ,  C07D413/14 ,  A61K31/506

CPC classification number: C07D413/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D417/14

Abstract: The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

Abstract translation: 本发明涉及式（I）：或其药学上可接受的盐，其中R1，R2a，R2b和R3-R7为本文。 本发明还涉及含有式（I）化合物的组合物以及这些化合物在抑制具有新形态活性的突变体IDH蛋白质中的用途。 本发明还涉及式（I）化合物在治疗与这种突变体IDH蛋白相关的疾病或病症中的用途，包括但不限于细胞增殖病症如癌症。

公开(公告)号：US20130303507A1

公开(公告)日：2013-11-14

申请号：US13981283

申请日：2012-01-20

Applicant: William R. Antonios-McCrea ,  Paul A. Barsanti ,  Cheng Hu ,  Xianming Jin ,  Eric Martin ,  Yue Pan ,  Xiaodong Lin ,  Keith B. Pfister ,  Paul A. Renhowe ,  Martin Sendzik ,  James Sutton ,  Lifeng Wan

Inventor： William R. Antonios-McCrea ,  Paul A. Barsanti ,  Cheng Hu ,  Xianming Jin ,  Eric Martin ,  Yue Pan ,  Xiaodong Lin ,  Keith B. Pfister ,  Paul A. Renhowe ,  Martin Sendzik ,  James Sutton ,  Lifeng Wan

IPC: C07D401/14 ,  C07D401/04 ,  C07D491/107 ,  C07D409/14 ,  C07D413/14 ,  C07D487/04 ,  C07D213/74 ,  C07D405/14

CPC classification number: C07D401/14 ,  C07D213/74 ,  C07D401/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/04 ,  C07D491/107

Abstract: The present invention provides a compound of formula (II): where R1 is a substituted alkyl, heterocyclic, or cycloalkyl, group, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof, and pharmaceutical compositions comprising these compounds. Also provided are methods of using these compounds to treat a disease or condition mediated by CDK9, such as cancers and other conditions described herein.

Abstract translation: 本发明提供式（II）化合物：其中R 1是取代的烷基，杂环或环烷基，基团及其药学上可接受的盐，对映异构体，立体异构体，旋转异构体，互变异构体，非对映异构体或外消旋物，以及包含它们的药物组合物 化合物。 还提供了使用这些化合物治疗由CDK9介导的疾病或病症的方法，例如本文所述的癌症和其它病症。

公开(公告)号：US20100280006A1

公开(公告)日：2010-11-04

申请号：US12387946

申请日：2009-05-08

Applicant: James C. Sutton ,  Marion Wiesmann ,  Weibo Wang ,  Mika Lindvall ,  Jiong Lan ,  Savithri Ramurthy ,  Anu Sharma ,  Elizabeth J. Mieuli ,  Liana M. Klivansky ,  William Lenahan ,  Susan Kaufman ,  Hong Yang ,  Simon C. Ng ,  Keith Pfister ,  Allan S. Wagman ,  Victoria Sung ,  Martin Sendzik

Inventor： James C. Sutton ,  Marion Wiesmann ,  Weibo Wang ,  Mika Lindvall ,  Jiong Lan ,  Savithri Ramurthy ,  Anu Sharma ,  Elizabeth J. Mieuli ,  Liana M. Klivansky ,  William Lenahan ,  Susan Kaufman ,  Hong Yang ,  Simon C. Ng ,  Keith Pfister ,  Allan S. Wagman ,  Victoria Sung ,  Martin Sendzik

IPC: A61K31/55 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/444 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4709 ,  A61K31/437 ,  A61K31/428 ,  A61K31/506 ,  A61P35/02 ,  A61P35/00 ,  A61P19/02 ,  A61P29/00 ,  A61P19/10 ,  A61P9/10 ,  A61P43/00 ,  C12N5/02

CPC classification number: C07D413/12 ,  C07D417/12

Abstract: Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.

Abstract translation: 公开了苯并恶唑和苯并噻唑化合物及其立体异构体，互变异构体，溶剂合物，氧化物，酯和前药及其药学上可接受的盐。 还公开了单独或与至少一种另外的治疗剂组合的化合物与药学上可接受的载体的组合，以及化合物单独或与至少一种另外的治疗剂组合的用途。 这些实施方案可用于抑制细胞增殖，抑制肿瘤的生长和/或复分解，治疗或预防癌症，治疗或预防退行性骨疾病如类风湿性关节炎和/或抑制分子如CSF-1R。

公开(公告)号：US20100130490A1

公开(公告)日：2010-05-27

申请号：US12451326

申请日：2008-05-20

Applicant: Simon C. Ng ,  Keith B. Pfister ,  Martin Sendzik ,  James Sutton ,  Allan S. Wagman ,  Marion Wiesmann

Inventor： Simon C. Ng ,  Keith B. Pfister ,  Martin Sendzik ,  James Sutton ,  Allan S. Wagman ,  Marion Wiesmann

IPC: A61K31/428 ,  C12N5/00 ,  A61K31/5377 ,  A61K31/501 ,  A61K31/497 ,  A61K31/519 ,  A61K31/517 ,  A61K31/506 ,  A61K31/4439 ,  C07D417/12 ,  C07D487/04 ,  C07D417/14 ,  C07D277/82 ,  A61P35/00 ,  A61P19/10 ,  A61P19/02 ,  A61P13/00

CPC classification number: C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04

Abstract: Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.

Abstract translation: 公开了苯并恶唑和苯并噻唑化合物及其氧化物，酯，前药，溶剂合物及其药学上可接受的盐。 还公开了单独或与至少一种另外的治疗剂组合的化合物与药学上可接受的载体的组合，以及化合物单独或与至少一种另外的治疗剂组合的用途。 这些实施方案可用于抑制细胞增殖，抑制肿瘤的生长和/或复分解，治疗或预防癌症，治疗或预防退行性骨疾病如类风湿性关节炎和/或抑制分子如CSF 1R。

公开(公告)号：US20070293540A1

公开(公告)日：2007-12-20

申请号：US11830686

申请日：2007-07-30

Applicant: Erik Verner ,  Martin Sendzik ,  Chitra Baskaran ,  Joseph Buggy ,  James Robinson

Inventor： Erik Verner ,  Martin Sendzik ,  Chitra Baskaran ,  Joseph Buggy ,  James Robinson

IPC: A61K31/195 ,  A61K31/34 ,  A61K31/38 ,  A61K31/445 ,  A61P35/00 ,  C07C259/04 ,  C07D307/78 ,  C07D333/52 ,  C07D405/02

CPC classification number: A61K31/343 ,  A61K31/18 ,  A61K31/33 ,  A61K31/34 ,  A61K31/4015 ,  A61K31/4415 ,  A61K41/00 ,  A61K45/06 ,  A61N5/10 ,  C07C259/10 ,  C07C2601/02 ,  C07D207/12 ,  C07D207/327 ,  C07D207/34 ,  C07D209/08 ,  C07D209/18 ,  C07D209/42 ,  C07D209/44 ,  C07D211/46 ,  C07D213/56 ,  C07D213/74 ,  C07D213/81 ,  C07D213/82 ,  C07D215/08 ,  C07D215/18 ,  C07D215/48 ,  C07D215/54 ,  C07D217/04 ,  C07D217/06 ,  C07D217/26 ,  C07D231/56 ,  C07D235/06 ,  C07D235/24 ,  C07D241/52 ,  C07D249/18 ,  C07D261/18 ,  C07D263/58 ,  C07D277/30 ,  C07D277/42 ,  C07D277/56 ,  C07D277/68 ,  C07D307/54 ,  C07D307/68 ,  C07D307/79 ,  C07D307/81 ,  C07D307/85 ,  C07D307/86 ,  C07D317/60 ,  C07D333/16 ,  C07D333/24 ,  C07D333/28 ,  C07D333/38 ,  C07D333/70 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  A61K2300/00

Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

Abstract translation: 本发明涉及可用于治疗丙型肝炎的某些异羟肟酸衍生物。这些化合物也是组蛋白脱乙酰酶的抑制剂，因此可用于治疗与组蛋白脱乙酰酶活性相关的疾病。 还公开了制备这些化合物的药物组合物和方法。

公开(公告)号：US10308660B2

公开(公告)日：2019-06-04

申请号：US15736989

申请日：2016-06-15

Applicant: Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Matthew J. LaMarche ,  Martin Sendzik ,  Victoriano Tamez, Jr. ,  Bing Yu

Inventor： Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Matthew J. LaMarche ,  Martin Sendzik ,  Victoriano Tamez, Jr. ,  Bing Yu

IPC: C07D401/04 ,  C07D491/107 ,  C07D401/14 ,  A61P35/00

Abstract: The present invention relates to compounds of formula I: in which X1, X2, X3, Y1, Y2, Y3, R1, R2, R3a, R4a, R4b, R5a, R5b, R6a and R6b 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：US10077276B2

公开(公告)日：2018-09-18

申请号：US15110511

申请日：2015-01-16

Applicant: 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

Inventor： 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: C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10 ,  C07D401/14

Abstract: 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.

公开(公告)号：US20180251471A1

公开(公告)日：2018-09-06

申请号：US15736989

申请日：2016-06-15

Applicant: Zhuoliang CHEN ,  Jorge Garcia FORTANET ,  Matthew J. LAMARCHE ,  Martin SENDZIK ,  Victoriano TAMEZ, JR. ,  Bing YU

Inventor： Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Matthew J. LaMarche ,  Martin Sendzik ,  Victoriano Tamez, JR. ,  Bing Yu

IPC: C07D491/107 ,  C07D401/14 ,  C07D401/04 ,  A61P35/00

CPC classification number: C07D491/107 ,  A61P35/00 ,  C07D401/04 ,  C07D401/14

Abstract: The present invention relates to compounds of formula I: in which X1, X2, X3, Y1, Y2, Y3, R1, R2, R3a, R4a, R4b, R5a, R5b, R6a and R6b 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：US09938295B2

公开(公告)日：2018-04-10

申请号：US15110511

申请日：2015-01-16

Applicant: 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

Inventor： 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: C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10

Abstract: 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.

公开(公告)号：US20130210818A1

公开(公告)日：2013-08-15

申请号：US13396339

申请日：2012-02-14

Applicant: Zilin Huang ,  Jeff Jin ,  Timothy Machajewski ,  William R. Antonios-McCrea ,  Maureen McKenna ,  Daniel Poon ,  Paul A. Renhowe ,  Martin Sendzik ,  Cynthia Shafer ,  Aaron Smith ,  Yongjin Xu ,  Qiong Zhang ,  Zheng Chen

Inventor： Zilin Huang ,  Jeff Jin ,  Timothy Machajewski ,  William R. Antonios-McCrea ,  Maureen McKenna ,  Daniel Poon ,  Paul A. Renhowe ,  Martin Sendzik ,  Cynthia Shafer ,  Aaron Smith ,  Yongjin Xu ,  Qiong Zhang ,  Zheng Chen

IPC: A61K31/444 ,  A61K31/506 ,  C07D403/14 ,  C07D405/14 ,  A61K31/4439 ,  C07D417/14 ,  C07D471/04 ,  C07D413/14 ,  A61K31/496 ,  C07D487/04 ,  A61K31/4985 ,  C07D498/04 ,  A61K31/5383 ,  A61K31/4709 ,  A61K31/5377 ,  A61P35/00 ,  C07D401/14

CPC classification number: A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5383 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04 ,  A61K2300/00

Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

Abstract translation: 提供了新的取代的杂环化合物，含有它们的组合物，以及使用它们来抑制Raf激酶活性的方法。 新化合物和组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗Raf激酶介导的病症，例如癌症。