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Derivatives of N - cyclopropyl - (1h indazol 4,5,6,7 tetrahydro - - - - 5 - il) - benzamide as inhibitor of HSD1 11B
专利权人:
ASTELLAS PHARMA INC.
发明人:
申请号:
ARP120103883
公开号:
AR088378A1
申请日:
2012.10.18
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
The publication of an advantageous compound as a pharmaceutical ingredient for the treatment of diseases related to class 11b dehydrogenase, such as dementia, schizophrenia, depression, pain (especially neuropathic or fibrotic pain),Diabetes (especially type 2 diabetes)Insulin resistance, etc.: it is found that a bicyclic heterocyclic compound (when cyclohexane is fused with a 5-6 member monocyclohexane, only one of which is a heterogenous nitrogen atom) is replaced by an acid group such as a group. (straight) similar aroilamino or similar pharmaceutically acceptable salts have excellent inhibitory effect on 11b-hsd1. Therefore, this bicyclic heterocyclic compound can be used to treat dementia, schizophrenia, depression, pain (especially neuropathic pain or fibrosis).Diabetes (especially type 2 diabetes)1. Insulin resistance and other. Requirements 1: compound represented by formula (1) or acceptable salt of drug; [the symbol in the formula indicates: Ring A: a single periodic heteromorphism of 5 to 6 members, which can be replaced, and only the nitrogen atom is the heteroatom; the atom existing in the position where the ring merges with the adjacent ring is the carbon atom, R1: low tar, halo low tar, or substituted cyclopentyl, R2: halo or low tar, R3: arilo, isohalo or low tar isohalo;Here, each arilo and heretic represented by R 3 can be replaced, N: the whole 0-3 and a dotted line represent a simple link or a double link].Dar a conocer un compuesto ventajoso como ingrediente activo de una composición farmacéutica para el tratamiento de enfermedades relacionadas con la 11b-hidroxiesteroide deshidrogenasa tipo 1 tales como demencia, esquizofrenia, depresión, dolor (en particular, dolor neuropático o fibromialgia), diabetes (en particular, diabetes mellitus tipo II), la resistencia a la insulina y demás. Se descubrió que un compuesto heterocíclico bicíclico (el heterociclo bicíclico se forma cuando un anillo de ciclohexano se fusiona a un heterociclo monocíclico de
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