公开(公告)号：US09133224B2

公开(公告)日：2015-09-15

申请号：US13990045

申请日：2011-11-29

Applicant: Andrew P. Crew ,  Hanqing Dong ,  Caterina Ferraro ,  Dan Sherman ,  Kam W. Siu

Inventor： Andrew P. Crew ,  Hanqing Dong ,  Caterina Ferraro ,  Dan Sherman ,  Kam W. Siu

IPC: A61K31/675 ,  C07F9/6584

CPC classification number: C07F9/6584 ,  A61K31/675

Abstract: Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.

Abstract translation: 式（I）化合物：其中变量在本文中定义，以及其药学上可接受的盐，合成，中间体，制剂及其治疗方法，包括FAK抑制有益的癌症。

公开(公告)号：US20120196847A1

公开(公告)日：2012-08-02

申请号：US13446629

申请日：2012-04-13

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: A61K31/4985 ,  A61K31/53 ,  A61P35/00 ,  A61K31/5377 ,  A61K31/551 ,  C07D487/04 ,  A61K31/519

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：US07388012B2

公开(公告)日：2008-06-17

申请号：US11227698

申请日：2005-09-15

Applicant: Andrew Crew ,  An-Hu Li ,  Hanqing Dong ,  Tao Zhang

Inventor： Andrew Crew ,  An-Hu Li ,  Hanqing Dong ,  Tao Zhang

IPC: A61K31/4709 ,  A61K31/381 ,  A61K31/497 ,  C07D215/14 ,  C07D409/12 ,  C07D333/36 ,  C07D333/38

CPC classification number: C07D409/12 ,  C07D409/14

Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A and J 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和J在本文中定义，可用于治疗肿瘤和癌症如肥大细胞增多症/肥大细胞白血病，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，神经母细胞瘤，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：US20070208053A1

公开(公告)日：2007-09-06

申请号：US11654814

申请日：2007-01-18

Applicant: Lee Arnold ,  Xin Chen ,  Hanqing Dong ,  Andrew Garton ,  Mark Mulvihill ,  Colin Sambrook Smith ,  Gerard Thomas ,  Thomas Krulle ,  Jing Wang

Inventor： Lee Arnold ,  Xin Chen ,  Hanqing Dong ,  Andrew Garton ,  Mark Mulvihill ,  Colin Sambrook Smith ,  Gerard Thomas ,  Thomas Krulle ,  Jing Wang

IPC: C07D471/02 ,  A61K31/4745

CPC classification number: C07D471/04

Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X5, X7, R1, and Q1 are defined herein, inhibit kinase enzymes and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer. The compounds are also useful in the treatment of inflammation, allergy, asthma, disease and conditions of the immune system, disease and conditions of the nervous system, cardiovascular diseases, disease and conditions of the eye, dermatological diseases, osteoporosis, diabetes, multiple sclerosis, and infections.

Abstract translation: 下式的化合物及其药学上可接受的盐，其中X 1，X 2，X 3，X 4， X 5，X 5，X 7，R 1和Q 1 在本文中定义，抑制激酶，并且可用于治疗和/或预防过度增殖性疾病如癌症。 该化合物还可用于治疗炎症，过敏，哮喘，免疫系统的疾病和状况，神经系统的疾病和状况，心血管疾病，眼睛疾病和病症，皮肤病，骨质疏松症，糖尿病，多发性硬化 和感染。

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：US20060063773A1

公开(公告)日：2006-03-23

申请号：US11227698

申请日：2005-09-15

Applicant: Andrew Crew ,  An-Hu Li ,  Hanqing Dong ,  Tao Zhang

Inventor： Andrew Crew ,  An-Hu Li ,  Hanqing Dong ,  Tao Zhang

IPC: A61K31/496 ,  A61K31/4709 ,  C07D409/02

CPC classification number: C07D409/12 ,  C07D409/14

Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A and J 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：US08022206B2

公开(公告)日：2011-09-20

申请号：US12366743

申请日：2009-02-06

Applicant: An-Hu Li ,  Arno G. Steinig ,  Andrew Kleinberg ,  Qinghua Weng ,  Mark J. Mulvihill ,  Jing Wang ,  Xin Chen ,  Ti Wang ,  Hanqing Dong ,  Meizhong Jin

Inventor： An-Hu Li ,  Arno G. Steinig ,  Andrew Kleinberg ,  Qinghua Weng ,  Mark J. Mulvihill ,  Jing Wang ,  Xin Chen ,  Ti Wang ,  Hanqing Dong ,  Meizhong Jin

IPC: C07D413/00 ,  C07D403/00 ,  C07D471/02

CPC classification number: C07D491/048

Abstract: Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.

Abstract translation: 呋喃并[3,2-c]吡啶和噻吩并[3,2-c]吡啶化合物及其药学上可接受的盐，制剂，中间体，药物组合物和用途，例如疾病治疗包括癌症，包括 涉及EMT的病症，包括蛋白激酶活性介导的病症，如RON和/或MET。

公开(公告)号：US07465726B2

公开(公告)日：2008-12-16

申请号：US11194158

申请日：2005-08-01

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

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

IPC: A61K31/437 ,  A61K31/496 ,  A61K31/5355 ,  A61K31/541 ,  A61K31/5513 ,  A61K31/551 ,  C07D471/04 ,  C07D223/04 ,  C07D243/08 ,  C07D241/04 ,  C07D413/10 ,  C07D413/06 ,  C07D413/08 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  A61K31/04 ,  A61K31/519 ,  C07D487/04

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：US20060235031A1

公开(公告)日：2006-10-19

申请号：US11095162

申请日：2005-03-31

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

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

IPC: A61K31/52

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: 下式的化合物及其药学上可接受的盐，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，抑制IGF-1R酶，并且可用于治疗和/或预防过度增殖性疾病如癌症，炎症，牛皮癣，过敏/哮喘，免疫系统的疾病和状况，中枢的疾病和状况 神经系统。

公开(公告)号：US20130261086A1

公开(公告)日：2013-10-03

申请号：US13990045

申请日：2011-11-29

Applicant: Andrew P. Crew ,  Hanqing Dong ,  Caterina Ferraro ,  Dan Sherman ,  Kam W. Siu

Inventor： Andrew P. Crew ,  Hanqing Dong ,  Caterina Ferraro ,  Dan Sherman ,  Kam W. Siu

IPC: C07F9/6584

CPC classification number: C07F9/6584 ,  A61K31/675

Abstract: Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.

Abstract translation: 式（I）化合物：其中变量在本文中定义，以及其药学上可接受的盐，合成，中间体，制剂及其治疗方法，包括FAK抑制有益的癌症。