Login| Sign Up| Help| Contact|

Patent Searching and Data


Title:
FIVE-MEMBERED HETEROARYL RING BRIDGED RING DERIVATIVE, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/068759
Kind Code:
A1
Abstract:
The present invention relates to a five-membered heteroaryl ring bridged ring derivative, a preparation method therefor and the medical use thereof. In particular, the present invention relates to a new five-membered heteroaryl ring bridged ring derivative as shown in general formula (I), a preparation method therefor and a pharmaceutical composition comprising the derivative, and the use thereof as a therapeutic agent, in particular as a TGF-β inhibitor, and the use in the preparation of a drug for treating, preventing or reducing cancers mediated by the over-expression of TGF-β, wherein the definition of each substituent in the general formula (I) is the same as defined in the description.

Inventors:
YU SHANGHAI (CN)
YANG FANGLONG (CN)
YAN JINGJING (CN)
WU XIAO (CN)
HE FENG (CN)
TAO WEIKANG (CN)
Application Number:
PCT/CN2017/106052
Publication Date:
April 19, 2018
Filing Date:
October 13, 2017
Export Citation:
Click for automatic bibliography generation   Help
Assignee:
JIANGSU HENGRUI MEDICINE CO (CN)
SHANGHAI HENGRUI PHARMACEUTICAL CO LTD (CN)
International Classes:
A61K31/4439; C07D471/08; A61K31/444; A61P3/00; A61P9/00; A61P13/12; A61P19/02; A61P19/08; A61P25/00; A61P35/00; C07D487/08
Domestic Patent References:
WO2016106266A12016-06-30
WO2004111046A22004-12-23
WO2012000595A12012-01-05
WO2012002680A22012-01-05
WO2013009140A22013-01-17
WO2016106266A12016-06-30
WO2014022128A12014-02-06
WO2015103137A12015-07-09
WO2010059943A22010-05-27
WO2005092894A12005-10-06
WO2013101974A12013-07-04
WO2009155527A22009-12-23
WO2014210255A12014-12-31
WO2012086735A12012-06-28
WO2015039172A12015-03-26
WO2006052568A22006-05-18
WO2007018818A12007-02-15
WO2010132509A22010-11-18
WO2014005183A12014-01-09
Foreign References:
US20150284362A12015-10-08
US20140134133A12014-05-15
CZ105175294A
JP2011079782A2011-04-21
CN104177390A2014-12-03
US20120095075A12012-04-19
US20100160280A12010-06-24
Other References:
MASSAGUE, J. ANN. REV, CELL. BIOL., vol. 6, 1990, pages 594 - 641
ROBERTS, A. B.: "Peptide Growth Factor and Their receptors", vol. 95, 1990, SPRINGER-VERLAG, pages: 419 - 472
ROBERTS, A. B.SPORN M. B., GROWTH FACTOR, vol. 8, 1993, pages 1 - 9
ALEXANDROW, M. G.MOSES, H. L., CANCER RES., vol. 55, 1995, pages 1452 - 1457
HOJO, M. ET AL., NATURE, vol. 397, 1999, pages 530 - 534
MAEHARA, Y. ET AL., J. CLIN. ONCOL., vol. 17, 1999, pages 607 - 614
PICON, A. ET AL., CANCER EPIDEMIOL. BIOMARKERS PREV., vol. 7, 1998, pages 497 - 504
BITZER, M. ET AL., KIDNEY BLOOD PRESS. RES., vol. 21, 1998, pages 1 - 12
BORDER, W. A. ET AL., NATURE, vol. 346, 1990, pages 371 - 374
SALTIS, J. ET AL., CLIN. EXP. PHARMACOL. PHYSIOL., vol. 23, 1996, pages 193 - 200
MCCAFFREY, T. A. ET AL., J. CLIN. INVEST., vol. 96, 1995, pages 2667 - 2675
PICHT, G. ET AL., GRAEFES ARCH. CLIN. EXP. OPHTHALMOL., vol. 239, 2001, pages 199 - 207
KOTTLER, U. B. ET AL., EXP. EYE RES., vol. 80, 2005, pages 121 - 134
"Angewandte Chemie", vol. 44, 2005, pages: 5710 - 5713
JOURNAL OF ORGANIC CHEMISTRY, vol. 3, no. 2, 2008, pages 4662 - 4670
MOLECULES, vol. 19, no. 10, 2014, pages 15653 - 15672
TETRAHEDRON LETTERS, vol. 54, no. 2, 2013, pages 166 - 169
HETEROATOM CHEMISTRY, vol. 23, no. 4, 2012, pages 399 - 410
See also references of EP 3527570A4
Attorney, Agent or Firm:
GE CHENG & CO., LTD. (CN)
Download PDF: