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.
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Inventors:
YU SHANGHAI (CN)
YANG FANGLONG (CN)
YAN JINGJING (CN)
WU XIAO (CN)
HE FENG (CN)
TAO WEIKANG (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:
Assignee:
JIANGSU HENGRUI MEDICINE CO (CN)
SHANGHAI HENGRUI PHARMACEUTICAL CO LTD (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
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WO2016106266A1 | 2016-06-30 | |||
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WO2012000595A1 | 2012-01-05 | |||
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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
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"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
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)
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