公开(公告)号：US20100099679A1

公开(公告)日：2010-04-22

申请号：US12622545

申请日：2009-11-20

Applicant: Xin Chen ,  Heather Coate ,  Andrew Philip Crew ,  Han-Qing Dong ,  Ayako Honda ,  Mark Joseph Mulvihill ,  Paula A.R. Tavares ,  Jing Wang ,  Douglas S. Werner ,  Kristen Michelle Mulvihill ,  Kam W. Siu ,  Bijoy Panicker ,  Apoorba Bharadwaj ,  Lee D. Arnold ,  Meizhong Jin ,  Brian Volk ,  Quinghua Weng ,  James David Beard

Inventor： Xin Chen ,  Heather Coate ,  Andrew Philip Crew ,  Han-Qing Dong ,  Ayako Honda ,  Mark Joseph Mulvihill ,  Paula A.R. Tavares ,  Jing Wang ,  Douglas S. Werner ,  Kristen Michelle Mulvihill ,  Kam W. Siu ,  Bijoy Panicker ,  Apoorba Bharadwaj ,  Lee D. Arnold ,  Meizhong Jin ,  Brian Volk ,  Quinghua Weng ,  James David Beard

IPC: A61K31/53 ,  C07D487/04 ,  A61K31/4985 ,  A61P35/00

CPC classification number: C07D487/04 ,  A61K31/5025 ,  C07D253/07 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.

Abstract translation: 由式（I）表示的化合物或其药学上可接受的盐是mTOR的抑制剂，可用于治疗癌症。

公开(公告)号：US07696225B2

公开(公告)日：2010-04-13

申请号：US10973870

申请日：2004-10-26

Applicant: Jason Bloxham ,  Andrew Phillip Crew ,  Ayako Honda ,  An-Hu Li ,  Bijoy Panicker ,  Graham Michael Wynne ,  Lawrence Tardibono, Jr.

Inventor： Jason Bloxham ,  Andrew Phillip Crew ,  Ayako Honda ,  An-Hu Li ,  Bijoy Panicker ,  Graham Michael Wynne ,  Lawrence Tardibono, Jr.

IPC: A61K31/4745 ,  A61K31/4709 ,  A61K31/4436

CPC classification number: A61K31/381 ,  A61K31/437 ,  A61K31/4436 ,  A61K31/4709 ,  A61K31/4745 ,  A61K45/06 ,  C07D409/12 ,  C07D409/14 ,  C07D471/04 ,  A61K2300/00

Abstract: Amidoaryl/amidoheteroaryl substituted thiophenes, further substituted with a heteroarylmethylamino group, are useful in the treatment of cancer.

Abstract translation: 进一步被杂芳基甲基氨基取代的酰胺芳基/酰胺基芳基取代的噻吩可用于治疗癌症。

公开(公告)号：US20060211678A1

公开(公告)日：2006-09-21

申请号：US11194158

申请日：2005-08-01

Applicant: Saleh Ahmed ,  Oscar Barba ,  Jason Bloxham ,  Graham Dawson ,  Wiliam Gattrell ,  John Kitchin ,  Neil Anthony Pegg ,  Imaad Saba ,  Shazia Sadiq ,  Colin Peter Sambrook Smith ,  Don Smyth ,  Amo Steing ,  Robin Wilkes ,  Bijoy Panicker ,  Paula Tavares ,  Matthew Cox ,  An-Hu Li ,  Hanqing Dong ,  Lifu Ma ,  Kenneth Foreman ,  Qinghua Weng ,  Kathryn Stolz

Inventor： Saleh Ahmed ,  Oscar Barba ,  Jason Bloxham ,  Graham Dawson ,  Wiliam Gattrell ,  John Kitchin ,  Neil Anthony Pegg ,  Imaad Saba ,  Shazia Sadiq ,  Colin Peter Sambrook Smith ,  Don Smyth ,  Amo Steing ,  Robin Wilkes ,  Bijoy Panicker ,  Paula Tavares ,  Matthew Cox ,  An-Hu Li ,  Hanqing Dong ,  Lifu Ma ,  Kenneth Foreman ,  Qinghua Weng ,  Kathryn Stolz

IPC: A61K31/5377 ,  A61K31/519 ,  A61K31/496 ,  A61K31/4745 ,  C07D487/02 ,  C07D471/02

CPC classification number: C07D471/02 ,  C07D487/02 ,  C07D487/04

Abstract: Compounds represented by Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mek1, PDK-1, GSK3β, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-1R, Ron, Ret, and KDR kinases in animals, including humans, for the treatment and/or prevention of various diseases and conditions such as cancer.

Abstract translation: 由式（I）表示的化合物或其立体异构体或其药学上可接受的盐是Abl，Aurora-A，Blk，c-Raf，cSRC，Src，PRK2，FGFR3，Flt3，Lck，Mek1，PDK中的至少两种的抑制剂 -1，GSK3beta，EGFR，p70S6K，BMX，SGK，CaMKII，Tie-2，IGF-1R，Ron，Ret和KDR激酶，用于治疗和/或预防各种疾病和病症， 癌症。

公开(公告)号：US20060069121A1

公开(公告)日：2006-03-30

申请号：US11227697

申请日：2005-09-15

Applicant: Andrew Crew ,  An-Hu Li ,  Bijoy Panicker

Inventor： Andrew Crew ,  An-Hu Li ,  Bijoy Panicker

IPC: A61K31/4709 ,  C07D409/14

CPC classification number: C07D409/12 ,  C07D409/14

Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, Q, Y, R1, R2, and R5 are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma.

Abstract translation: 由式（I）表示的化合物：

公开(公告)号：US20050154014A1

公开(公告)日：2005-07-14

申请号：US10973870

申请日：2004-10-26

Applicant: Jason Bloxham ,  Andrew Crew ,  Ayako Honda ,  An-Hu Li ,  Bijoy Panicker ,  Lawrence Tardibono ,  Graham Wynne

Inventor： Jason Bloxham ,  Andrew Crew ,  Ayako Honda ,  An-Hu Li ,  Bijoy Panicker ,  Lawrence Tardibono ,  Graham Wynne

IPC: A61K31/381 ,  A61K31/437 ,  A61K31/4436 ,  A61K31/4709 ,  A61K31/4745 ,  A61K45/06 ,  C07D409/12 ,  C07D409/14 ,  C07D471/04 ,  C07D49/02

CPC classification number: A61K31/381 ,  A61K31/437 ,  A61K31/4436 ,  A61K31/4709 ,  A61K31/4745 ,  A61K45/06 ,  C07D409/12 ,  C07D409/14 ,  C07D471/04 ,  A61K2300/00

Abstract: Amidoaryl/amidoheteroaryl substituted thiophenes, further substituted with a heteroarylmethylamino group, are useful in the treatment of cancer.

Abstract translation: 进一步被杂芳基甲基氨基取代的酰胺芳基/酰胺基芳基取代的噻吩可用于治疗癌症。

公开(公告)号：US20150306078A1

公开(公告)日：2015-10-29

申请号：US14704829

申请日：2015-05-05

Applicant: Bijoy PANICKER ,  Rama K. MISHRA ,  Dong Sung LIM ,  Lambertus J.W.M. OEHLEN ,  Dawoon JUNG

Inventor： Bijoy PANICKER ,  Rama K. MISHRA ,  Dong Sung LIM ,  Lambertus J.W.M. OEHLEN ,  Dawoon JUNG

IPC: A61K31/437 ,  A61K31/5377 ,  A61K31/496

CPC classification number: A61K31/437 ,  A61K31/496 ,  A61K31/5377

Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving abnormal or excessive fibrosis.

Abstract translation: 本发明提供具有一般结构式（I）的化合物及其药学上可接受的衍生物，如本文中一般和本类和亚类所述，并且另外提供其药物组合物，以及用于治疗任何一种 涉及异常或过度纤维化的病症或疾病。

公开(公告)号：US09040555B2

公开(公告)日：2015-05-26

申请号：US14374210

申请日：2013-01-26

Applicant: Bijoy Panicker ,  Rama K. Mishra ,  Dong Sung Lim ,  Lambertus J. W. M. Oehlen ,  Dawoon Jung

Inventor： Bijoy Panicker ,  Rama K. Mishra ,  Dong Sung Lim ,  Lambertus J. W. M. Oehlen ,  Dawoon Jung

IPC: C07D401/02 ,  C07D401/10 ,  C07D401/14 ,  A61K31/4353 ,  A61K31/437 ,  C07D471/04

CPC classification number: A61K31/4353 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  C07D401/02 ,  C07D401/14 ,  C07D471/04

Abstract: The present invention provides compounds having the general structural formula (I), and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving abnormal or excessive fibrosis.

Abstract translation: 本发明提供具有一般结构式（I）的化合物及其药学上可接受的衍生物，如本文中一般和本领域和亚类所述，并且另外提供其药物组合物及其用于治疗任何 涉及异常或过度纤维化的病情或疾病数。

公开(公告)号：US08513433B2

公开(公告)日：2013-08-20

申请号：US13381856

申请日：2010-07-02

Applicant: Bijoy Panicker ,  Dong Sung Lim ,  David E. Smith

Inventor： Bijoy Panicker ,  Dong Sung Lim ,  David E. Smith

IPC: A61K31/4184 ,  C07D403/04 ,  C07D401/04

CPC classification number: C07D403/04 ,  C07D401/04

Abstract: Compounds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such compounds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.

Abstract translation: 提供了抑制聚ADP-核糖合成酶（PARP）的活性的化合物和药物组合物。 这些化合物可用于治疗各种疾病，病症和损伤如中风，心肌梗死，各种器官的缺血灌注损伤，创伤性脑损伤，动脉粥样硬化，炎性疾病和癌症。

公开(公告)号：US20130165651A1

公开(公告)日：2013-06-27

申请号：US13767947

申请日：2013-02-15

Applicant: Xin Chen ,  Heather Coate ,  Andrew Philip Crew ,  Han-Qing Dong ,  Ayako Honda ,  Mark Joseph Mulvihill ,  Paula A.R. Tavares ,  Jing Wang ,  Douglas S. Werner ,  Kristen Michelle Mulvihill ,  Kam W. Siu ,  Bijoy Panicker ,  Apoorba Bharadwaj ,  Lee D. Arnold ,  Meizhong Jin ,  Brian Volk ,  Qinghua Weng ,  James David Beard

Inventor： Xin Chen ,  Heather Coate ,  Andrew Philip Crew ,  Han-Qing Dong ,  Ayako Honda ,  Mark Joseph Mulvihill ,  Paula A.R. Tavares ,  Jing Wang ,  Douglas S. Werner ,  Kristen Michelle Mulvihill ,  Kam W. Siu ,  Bijoy Panicker ,  Apoorba Bharadwaj ,  Lee D. Arnold ,  Meizhong Jin ,  Brian Volk ,  Qinghua Weng ,  James David Beard

IPC: C07D487/04

CPC classification number: C07D487/04 ,  A61K31/5025 ,  C07D253/07 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.

Abstract translation: 由式（I）表示的化合物或其药学上可接受的盐是mTOR的抑制剂，可用于治疗癌症。

公开(公告)号：US08378104B2

公开(公告)日：2013-02-19

申请号：US13025281

申请日：2011-02-11

Applicant: Keith R. Hornberger ,  Dan M. Berger ,  Xin Chen ,  Andrew P. Crew ,  Hanqing Dong ,  Andrew Kleinberg ,  An-Hu Li ,  Lifu Ma ,  Mark J. Mulvihill ,  Bijoy Panicker ,  Kam W. Siu ,  Arno G. Steinig ,  James G. Tarrant ,  Jing Wang ,  Qinghua Weng ,  Rajaram Sangem ,  Ramesh C. Gupta

Inventor： Keith R. Hornberger ,  Dan M. Berger ,  Xin Chen ,  Andrew P. Crew ,  Hanqing Dong ,  Andrew Kleinberg ,  An-Hu Li ,  Lifu Ma ,  Mark J. Mulvihill ,  Bijoy Panicker ,  Kam W. Siu ,  Arno G. Steinig ,  James G. Tarrant ,  Jing Wang ,  Qinghua Weng ,  Rajaram Sangem ,  Ramesh C. Gupta

IPC: C07D471/02

CPC classification number: C07D491/048

Abstract: Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.

Abstract translation: 式1的化合物，如下文所定义：其药学上可接受的盐，合成，中间体，制剂及其治疗方法，包括治疗癌症，例如至少部分由TAK1驱动的肿瘤，或适合于 TAK1抑制剂有效。 本发明并不限于本发明。