公开(公告)号：US08710048B2

公开(公告)日：2014-04-29

申请号：US13453202

申请日：2012-04-23

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 B. 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 B. Pfister ,  Allan S. Wagman ,  Victoria Sung ,  Martin Sendzik

IPC: A61K31/4439 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/55 ,  C07D413/14 ,  C07D417/14 ,  C07D413/12 ,  A61P35/02 ,  A61P35/00 ,  A61P19/10 ,  A61P9/10 ,  A61P13/12

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：US08293769B2

公开(公告)日：2012-10-23

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: A61K31/5377 ,  A61K31/519 ,  A61K31/506 ,  A61K31/501 ,  A61K31/497 ,  A61K31/4745 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/444 ,  A61K31/4439 ,  C07D495/04 ,  C07D487/04 ,  C07D417/12 ,  C07D417/14 ,  C07D413/12 ,  C07D413/14

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：US08202876B2

公开(公告)日：2012-06-19

申请号：US12444129

申请日：2007-09-24

Applicant: Pamela Albaugh ,  Gregory B. Chopiuk ,  Qiang Ding ,  Shenlin Huang ,  Zuosheng Liu ,  Shifeng Pan ,  Pingda Ren ,  Xia Wang ,  Xing Wang ,  Yongping Xie ,  Chengzhi Zhang ,  Qiong Zhang ,  Guobao Zhang ,  Daniel Poon ,  Paul Renhowe ,  Martin Sendzik

Inventor： Pamela Albaugh ,  Gregory B. Chopiuk ,  Qiang Ding ,  Shenlin Huang ,  Zuosheng Liu ,  Shifeng Pan ,  Pingda Ren ,  Xia Wang ,  Xing Wang ,  Yongping Xie ,  Chengzhi Zhang ,  Qiong Zhang ,  Guobao Zhang ,  Daniel Poon ,  Paul Renhowe ,  Martin Sendzik

IPC: C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D231/00 ,  C07D403/02 ,  A01N43/56 ,  A61K31/415

CPC classification number: C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases.

Abstract translation: 本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及Abl，ARG，BCR异常活化的疾病或病症 -Abl，BRK，EphB，Fms，Fyn，KDR，c-Kit，LCK，PDGF-R，b-Raf，c-Raf，SAPK2，Src，Tie2和TrkB激酶。

公开(公告)号：US08129394B2

公开(公告)日：2012-03-06

申请号：US12383035

申请日：2009-03-19

Applicant: Zilin Hunag ,  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 Hunag ,  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: A61K31/4965 ,  A61K31/505 ,  A01N43/54 ,  C07D403/00 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00

CPC classification number: C07D498/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: Novel imidazole compounds of the general formula are disclosed, wherein R1 and R2 comprise heteroaryl groups. These compounds and compositions containing them are useful in methods to treat Raf kinase-mediated disorders such as cancer.

Abstract translation: 公开了通式的新型咪唑化合物，其中R 1和R 2包含杂芳基。 这些含有它们的化合物和组合物可用于治疗Raf激酶介导的疾病如癌症的方法。

公开(公告)号：US20100261679A1

公开(公告)日：2010-10-14

申请号：US12738277

申请日：2008-10-16

Applicant: James Sutton ,  Martin Sendzik ,  Weibo Wang

Inventor： James Sutton ,  Martin Sendzik ,  Weibo Wang

IPC: A61K31/66 ,  C12N5/071 ,  A61K31/4709 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/4439 ,  C07D215/38 ,  C07D401/12 ,  C07D413/12 ,  C07D417/10 ,  A61P35/00

CPC classification number: A61K31/4184 ,  A61K31/4188 ,  A61K31/428 ,  A61K31/429 ,  A61K31/47 ,  A61K31/517

Abstract: Disclosed herein are compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof, 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. 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: 本文公开了化合物及其氧化物，酯，前药，溶剂化物和药学上可接受的盐，化合物的组合物，单独或与至少一种另外的治疗剂组合与药学上可接受的载体，以及该化合物的用途， 单独或与至少一种另外的治疗剂组合。 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：US07420089B2

公开(公告)日：2008-09-02

申请号：US11834558

申请日：2007-08-06

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

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

IPC: C07C259/04 ,  C07C239/00 ,  A61K31/215 ,  A61K31/19

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：US20080004331A1

公开(公告)日：2008-01-03

申请号：US11834558

申请日：2007-08-06

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

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

IPC: A61K31/4025 ,  A61K31/195 ,  A61K31/403 ,  A61K31/4523 ,  C07C229/02 ,  C07D307/78 ,  C07D333/52 ,  C07D405/12

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.

公开(公告)号：US20170348312A1

公开(公告)日：2017-12-07

申请号：US15538348

申请日：2015-12-21

Applicant: Ho Man CHAN ,  Xiang-Ju Justin GU ,  Ying HUANG ,  Ling LI ,  Yuan MI ,  Wei QI ,  Martin SENDZIK ,  Yongfeng SUN ,  Long WANG ,  Zhengtian YU ,  Hailong ZHANG ,  Ji Yue (Jeff) ZHANG ,  Man ZHANG ,  Qiong ZHANG ,  Kehao ZHAO

Inventor： Ho Man CHAN ,  Xiang-Ju Justin GU ,  Ying HUANG ,  Ling LI ,  Yuan MI ,  Wei QI ,  Martin SENDZIK ,  Yongfeng SUN ,  Long WANG ,  Zhengtian YU ,  Hailong ZHANG ,  Ji Yue (Jeff) ZHANG ,  Man ZHANG ,  Qiong ZHANG ,  Kehao ZHAO

IPC: A61K31/519 ,  A61K31/551 ,  A61K31/541 ,  C07D487/04 ,  A61K31/5377

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D487/04

Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein R1, R2, R3, R4, R5, and n are as defined herein.

公开(公告)号：US08957068B2

公开(公告)日：2015-02-17

申请号：US14347481

申请日：2012-09-26

Applicant: Thomas Raymond Caferro ,  Young Shin Cho ,  Abran Q. Costales ,  Huangshu Lei ,  Francois Lenoir ,  Julian Roy Levell ,  Gang Liu ,  Mark G. Palermo ,  Keith Bruce Pfister ,  Martin Sendzik ,  Cynthia Shafer ,  Michael David Shultz ,  Troy Smith ,  James Clifford Sutton ,  Bakary-Barry Toure ,  Fan Yang ,  Qian Zhao

Inventor： Thomas Raymond Caferro ,  Young Shin Cho ,  Abran Q. Costales ,  Huangshu Lei ,  Francois Lenoir ,  Julian Roy Levell ,  Gang Liu ,  Mark G. Palermo ,  Keith Bruce Pfister ,  Martin Sendzik ,  Cynthia Shafer ,  Michael David Shultz ,  Troy Smith ,  James Clifford Sutton ,  Bakary-Barry Toure ,  Fan Yang ,  Qian Zhao

IPC: C07D413/04 ,  C07D413/14 ,  A61K31/506 ,  C07D487/04 ,  C07D471/04 ,  C07D487/08 ,  C07D417/14 ,  C07D498/10

CPC classification number: C07D413/14 ,  C07D413/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D498/10 ,  C07D513/04

Abstract: The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined 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）化合物或其药学上可接受的盐，其中R 1 -R 6在本文中定义。 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：US20130324530A1

公开(公告)日：2013-12-05

申请号：US13885640

申请日：2011-11-17

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

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

IPC: C07D213/74 ,  C07D401/14 ,  C07D409/14 ,  C07D405/14

CPC classification number: C07D213/74 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

Abstract: The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are pharmaceutical compositions containing these compounds and methods of treating a disease or condition mediated by CDK9 using these compounds and compositions.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，对映体，立体异构体，旋转异构体，互变异构体，非对映体或其外消旋物。 还提供含有这些化合物的药物组合物和使用这些化合物和组合物治疗由CDK9介导的疾病或病症的方法。