公开(公告)号：US20180008581A1

公开(公告)日：2018-01-11

申请号：US15462859

申请日：2017-03-19

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: A61K31/4353 ,  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.

公开(公告)号：US20150158853A1

公开(公告)日：2015-06-11

申请号：US14493976

申请日：2014-09-23

Applicant: Bijoy Panicker ,  Dong Sung Lim ,  Rama K. Mishra ,  Lambertus J.W.M. Oehlen ,  James G. Tarrant ,  Xiaokang Zhu ,  Dawoon Jung

Inventor： Bijoy Panicker ,  Dong Sung Lim ,  Rama K. Mishra ,  Lambertus J.W.M. Oehlen ,  James G. Tarrant ,  Xiaokang Zhu ,  Dawoon Jung

IPC: C07D417/06 ,  C07D417/14

CPC classification number: C07D417/06 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

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 fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.

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 涉及纤维化和增殖的病症或疾病，其中抗纤维化或抗增殖活性是有益的。

公开(公告)号：US08735405B2

公开(公告)日：2014-05-27

申请号：US13446629

申请日：2012-04-13

Applicant: Lee D. Arnold ,  Cara Cesario ,  Heather Coate ,  Andrew P. Crew ,  Hanqing Dong ,  Kenneth Foreman ,  Ayako Honda ,  Radoslaw Laufer ,  An-Hu Li ,  Kristen Michelle Mulvihill ,  Mark J. Mulvihill ,  Anthony I. Nigro ,  Bijoy Panicker ,  Arno G. Steinig ,  Yingchuan Sun ,  Quinghua Weng ,  Douglas S. Werner ,  Michael J. Wyle ,  Tao Zhang

Inventor： Lee D. Arnold ,  Cara Cesario ,  Heather Coate ,  Andrew P. Crew ,  Hanqing Dong ,  Kenneth Foreman ,  Ayako Honda ,  Radoslaw Laufer ,  An-Hu Li ,  Kristen Michelle Mulvihill ,  Mark J. Mulvihill ,  Anthony I. Nigro ,  Bijoy Panicker ,  Arno G. Steinig ,  Yingchuan Sun ,  Quinghua Weng ,  Douglas S. Werner ,  Michael J. Wyle ,  Tao Zhang

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC classification number: C07F5/025 ,  C07D471/04 ,  C07D487/04

Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.

Abstract translation: 其中X 1，X 2，X 3，X 4，X 5，X 6，X 7，R 1和Q 1在本文中定义的式及其药学上可接受的盐的化合物抑制IGF-1R酶，并且可用于治疗和/或预防 过度增生性疾病如癌症，炎症，牛皮癣，过敏/哮喘，免疫系统的疾病和状况，中枢神经系统的疾病和状况。

公开(公告)号：US20130102643A1

公开(公告)日：2013-04-25

申请号：US13700730

申请日：2011-06-01

Applicant: Bijoy Panicker ,  Lambertus J.W.M. Oehlen ,  James G. Tarrant ,  Dong Sung Lim ,  Xiaokang Zhu ,  Dawoon Jung ,  Rama K. Mishra

Inventor： Bijoy Panicker ,  Lambertus J.W.M. Oehlen ,  James G. Tarrant ,  Dong Sung Lim ,  Xiaokang Zhu ,  Dawoon Jung ,  Rama K. Mishra

IPC: C07D417/06

CPC classification number: C07D417/06 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

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 fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.

公开(公告)号：US20120077979A1

公开(公告)日：2012-03-29

申请号：US13308694

申请日：2011-12-01

Applicant: Lee D. Arnold ,  Heather Coate ,  Andrew Philip Crew ,  Hanqing Dong ,  Kenneth Foreman ,  Ayako Honda ,  Radoslaw Laufer ,  An-Hu Li ,  Kristen Michelle Mulvihill ,  Mark Joseph Mulvihill ,  Anthony Nigro ,  Bijoy Panicker ,  Arno G. Steinig ,  Qingua Weng ,  Douglas S. Werner ,  Michael J. Wyle ,  Tao Zhang ,  Cara Cesario ,  Yingchuan Sun

Inventor： Lee D. Arnold ,  Heather Coate ,  Andrew Philip Crew ,  Hanqing Dong ,  Kenneth Foreman ,  Ayako Honda ,  Radoslaw Laufer ,  An-Hu Li ,  Kristen Michelle Mulvihill ,  Mark Joseph Mulvihill ,  Anthony Nigro ,  Bijoy Panicker ,  Arno G. Steinig ,  Qingua Weng ,  Douglas S. Werner ,  Michael J. Wyle ,  Tao Zhang ,  Cara Cesario ,  Yingchuan Sun

IPC: C07D487/04 ,  C07F5/02

CPC classification number: C07F5/025 ,  C07D471/04 ,  C07D487/04

Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.

Abstract translation: 其中X 1，X 2，X 3，X 4，X 5，X 6，X 7，R 1和Q 1在本文中定义的式及其药学上可接受的盐的化合物抑制IGF-1R酶，并且可用于治疗和/或预防 过度增生性疾病如癌症，炎症，牛皮癣，过敏/哮喘，免疫系统的疾病和状况，中枢神经系统的疾病和状况。

公开(公告)号：US07820662B2

公开(公告)日：2010-10-26

申请号：US12244947

申请日：2008-10-03

Applicant: Lee D. Arnold ,  Cara Cesario ,  Heather Coate ,  Andrew Philip Crew ,  Hanqing Dong ,  Kenneth Foreman ,  Ayako Honda ,  Radoslaw Laufer ,  An-Hu Li ,  Kristen Michelle Mulvihill ,  Mark J. Mulvihill ,  Anthony I. Nigro ,  Bijoy Panicker ,  Arno G. Steinig ,  Yingchuan Sun ,  Quinghua Weng ,  Douglas S. Werner ,  Michael J. Wyle ,  Tao Zhang

Inventor： Lee D. Arnold ,  Cara Cesario ,  Heather Coate ,  Andrew Philip Crew ,  Hanqing Dong ,  Kenneth Foreman ,  Ayako Honda ,  Radoslaw Laufer ,  An-Hu Li ,  Kristen Michelle Mulvihill ,  Mark J. Mulvihill ,  Anthony I. Nigro ,  Bijoy Panicker ,  Arno G. Steinig ,  Yingchuan Sun ,  Quinghua Weng ,  Douglas S. Werner ,  Michael J. Wyle ,  Tao Zhang

IPC: C07D487/00 ,  A01N43/64

CPC classification number: C07F5/025 ,  C07D471/04 ,  C07D487/04

Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.

Abstract translation: 其中X 1，X 2，X 3，X 4，X 5，X 6，X 7，R 1和Q 1在本文中定义的式及其药学上可接受的盐的化合物抑制IGF-1R酶，并且可用于治疗和/或预防 过度增生性疾病如癌症，炎症，牛皮癣，过敏/哮喘，免疫系统的疾病和状况，中枢神经系统的疾病和状况。

公开(公告)号：US07700594B2

公开(公告)日：2010-04-20

申请号：US11599663

申请日：2006-11-15

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 ,  C07D401/14 ,  C07D403/04 ,  A61K31/53 ,  A61K31/4523 ,  A61K35/00

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：US07618965B2

公开(公告)日：2009-11-17

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: A61K31/535 ,  A61K31/47 ,  C07D413/00 ,  C07D215/00 ,  C07D215/02

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: 式（I）表示的化合物或其药学上可接受的盐或N-氧化物，其中A，Q，Y，R 1，R 2和R 5在本文中定义，可用于治疗肿瘤和癌症，例如肥大细胞增多症/桅杆 细胞白血病，胃肠道间质瘤（GIST），生殖细胞肿瘤，小细胞肺癌（SCLC），鼻窦自然杀伤/ T细胞淋巴瘤，睾丸癌（精原细胞瘤），甲状腺癌，恶性黑素瘤，卵巢癌，腺样囊性癌， 急性骨髓性白血病（AML），乳腺癌，儿科T细胞急性淋巴细胞白血病，成神经细胞瘤，肥大细胞白血病，血管肉瘤，间变性大细胞淋巴瘤，子宫内膜癌和前列腺癌。

公开(公告)号：US20090118499A1

公开(公告)日：2009-05-07

申请号：US12244947

申请日：2008-10-03

Applicant: Lee D. Arnold ,  Heather Coate ,  Andrew Philip Crew ,  Hanqing Dong ,  Kenneth Foreman ,  Ayako Honda ,  Radoslaw Laufer ,  An-Hu Li ,  Kristen Michelle Mulvihill ,  Mark Joseph Mulvihill ,  Anthony Nigro ,  Bijoy Panicker ,  Arno G. Steinig ,  Quinghua Weng ,  Douglas S. Werner ,  Michael J. Wyle ,  Tao Zhang ,  Cara Cesario ,  Yingchuan Sun

Inventor： Lee D. Arnold ,  Heather Coate ,  Andrew Philip Crew ,  Hanqing Dong ,  Kenneth Foreman ,  Ayako Honda ,  Radoslaw Laufer ,  An-Hu Li ,  Kristen Michelle Mulvihill ,  Mark Joseph Mulvihill ,  Anthony Nigro ,  Bijoy Panicker ,  Arno G. Steinig ,  Quinghua Weng ,  Douglas S. Werner ,  Michael J. Wyle ,  Tao Zhang ,  Cara Cesario ,  Yingchuan Sun

IPC: C07D487/04

CPC classification number: C07F5/025 ,  C07D471/04 ,  C07D487/04

Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.

公开(公告)号：US08772326B2

公开(公告)日：2014-07-08

申请号：US13003514

申请日：2009-07-09

Applicant: Weizhong Cai ,  Prakash Narayan ,  Bijoy Panicker ,  David E. Smith

Inventor： Weizhong Cai ,  Prakash Narayan ,  Bijoy Panicker ,  David E. Smith

IPC: A01N43/56 ,  A61K31/415 ,  A01N43/00 ,  A61K31/55 ,  A01N57/00 ,  A61K31/675 ,  C07D231/00

CPC classification number: C07D409/14 ,  A61K9/0019 ,  A61K9/145 ,  A61K9/146 ,  A61K9/1652 ,  A61K9/19 ,  A61K9/4866 ,  A61K31/415 ,  A61K31/4155 ,  C07D231/12 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06

Abstract: The present invention provides compositions and formulations of compounds having formula (I) and pharmaceutically acceptable derivatives thereof, wherein p, R1, R2 and B are 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 injuries, conditions or diseases in which HGF/SF or the activities thereof, or agonists or antagonists thereof have a therapeutically useful role. In addition, methods are provided for treating such diseases or diseases starting at a time after the onset of the injury, condition or disease.

Abstract translation: 本发明提供具有式（I）的化合物及其药学上可接受的衍生物的组合物和制剂，其中p，R 1，R 2和B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，以及用于 其用于治疗HGF / SF或其活性或其激动剂或拮抗剂具有治疗有用作用的许多损伤，病症或疾病中的任何一种。 此外，提供了用于治疗在损伤，病症或疾病发作后的时间开始的这些疾病或疾病的方法。