New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series
摘要:
Aromatase inhibition is the new standard of care for estrogen receptor positive breast cancer and has also potential for treatment of other diseases such as endometriosis. Simple and readily available 3-pyridyl arylethers and 1-aryl pyrrolo[2,3-c]pyridines recapitulating the key pharmacophore elements of Letrozole (1) are described and their structure-activity relationships are discussed. Potent and ligand efficient leads such as compound 23 (IC50 = 59 nM on aromatase) have been identified. (c) 2012 Elsevier Ltd. All rights reserved.
The present invention provides certain compounds according to formula (I) which are inhibitors of SSAO activity
wherein V, W, X, Y, Z, R
1
and R
2
are as defined in the specification.
IMIDAZO[4,5-C]PYRIDINE AND PYRROLO[2,3-C]PYRIDINE DERIVATIVES AS SSAO INHIBITORS
申请人:PROXIMAGEN LIMITED
公开号:US20160046622A1
公开(公告)日:2016-02-18
The compounds of formula (I) are inhibitors of semicarbazide-sensitive amine oxidase (SSAO) activity useful in the treatment of inflammation, an inflammatory disease, an immune or an autoimmune disorder, or inhibition of tumour growth.