Title:
MACROCYCLIC KINASE INHIBITOR
Document Type and Number:
WIPO Patent Application WO/2019/201282
Kind Code:
A1
Abstract:
Disclosed is a macrocyclic kinase inhibitor, wherein the compound, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof is as shown in formula I. Experiments show that the new compound as shown in formula I disclosed in the present invention exhibits an excellent TRK inhibitory activity, has a significant inhibitory effect on TRKA-mutant cell growth, and exhibits an excellent inhibitory effect on in vivo tumor growth, thus providing a new choice for the clinical treatment of diseases associated with abnormal TRK activity.
Inventors:
LI JIN (CN)
ZHANG DENGYOU (CN)
FENG JINGCHAO (CN)
WANG ZHI (CN)
PAN LEICHANG (CN)
HU JING (CN)
CHEN WEI (CN)
ZHANG DENGYOU (CN)
FENG JINGCHAO (CN)
WANG ZHI (CN)
PAN LEICHANG (CN)
HU JING (CN)
CHEN WEI (CN)
Application Number:
PCT/CN2019/083086
Publication Date:
October 24, 2019
Filing Date:
April 17, 2019
Export Citation:
Assignee:
HITGEN INC (CN)
International Classes:
C07D498/22; A61K31/519; A61P35/00; C07D498/18
Domestic Patent References:
| WO2010085597A1 | 2010-07-29 |
Foreign References:
| CN1894260A | 2007-01-10 | |||
| CN102757448A | 2012-10-31 | |||
| CN107735399A | 2018-02-23 | |||
| CN105164136A | 2015-12-16 |
Other References:
ZAHN, P.K. ET AL., J. PAIN, no. 5, 2004, pages 157 - 163
SHELTON, D.L. ET AL., PAIN, no. 116, 2005, pages 8 - 16
MATAYOSHI, S. ET AL., J. PHYSIOL, no. 569, 2005, pages 685 - 695
THOMPSON, S.W. ET AL., PROC. NATL. ACAD. SCI., no. 96, 1999, pages 7714 - 7718
LI, C.Q. ET AL., MOLECULAR PAIN, no. 28, 2008, pages 1 - 11
BRODEUR, G.M. ET AL., NAT. REV. CANCER, no. 3, 2003, pages 203 - 216
TRUZZI, F. ET AL., DERMATO-ENDOCRINOLOGY, no. 1, 2008, pages 32 - 36
JIN, W. ET AL., CARCINOGENESIS, no. 11, 2010, pages 1939 - 1947
DU, J, WORLD J. GASTROENTEROLOGY, no. 7, 2003, pages 1431 - 1434
PIEROTTIA, M.A. ET AL., CANCER LETTERS, no. 232, 2006, pages 90 - 98
ERIC ADRIAENSSENS, E. ET AL., CANCER RES, no. 68, 2008, pages 346 - 351
FREUND, M.V. ET AL., PHARMACOLOGY & THERAPEUTICS, no. 117, 2008, pages 52 - 76
MOLA, F.F. ET AL., GUT, no. 46, 2000, pages 670 - 678
DOU, Y.C., ARCH. DERMA. RES., no. 298, 2006, pages 31 - 37
SOHRABJI, F. ET AL., NEUROENDOCRINOLOGY, no. 27, 2006, pages 404 - 414
See also references of EP 3783000A4
SHELTON, D.L. ET AL., PAIN, no. 116, 2005, pages 8 - 16
MATAYOSHI, S. ET AL., J. PHYSIOL, no. 569, 2005, pages 685 - 695
THOMPSON, S.W. ET AL., PROC. NATL. ACAD. SCI., no. 96, 1999, pages 7714 - 7718
LI, C.Q. ET AL., MOLECULAR PAIN, no. 28, 2008, pages 1 - 11
BRODEUR, G.M. ET AL., NAT. REV. CANCER, no. 3, 2003, pages 203 - 216
TRUZZI, F. ET AL., DERMATO-ENDOCRINOLOGY, no. 1, 2008, pages 32 - 36
JIN, W. ET AL., CARCINOGENESIS, no. 11, 2010, pages 1939 - 1947
DU, J, WORLD J. GASTROENTEROLOGY, no. 7, 2003, pages 1431 - 1434
PIEROTTIA, M.A. ET AL., CANCER LETTERS, no. 232, 2006, pages 90 - 98
ERIC ADRIAENSSENS, E. ET AL., CANCER RES, no. 68, 2008, pages 346 - 351
FREUND, M.V. ET AL., PHARMACOLOGY & THERAPEUTICS, no. 117, 2008, pages 52 - 76
MOLA, F.F. ET AL., GUT, no. 46, 2000, pages 670 - 678
DOU, Y.C., ARCH. DERMA. RES., no. 298, 2006, pages 31 - 37
SOHRABJI, F. ET AL., NEUROENDOCRINOLOGY, no. 27, 2006, pages 404 - 414
See also references of EP 3783000A4
Attorney, Agent or Firm:
GAOYUNG INTELLECTUAL PROPERTY AGENCY (GENERAL PARTNERSHIP) (CN)
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