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Aldosterone synthase inhibitors
专利权人:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
发明人:
HUI YU,SIMON SURPRENANT,PETER NEMOTO,KENNETH MEYERS,KEITH HORNBERGER
申请号:
ARP150103319
公开号:
AR102266A1
申请日:
2015.10.14
申请国别(地区):
AR
年份:
2017
代理人:
摘要:
1. Claim 1: a compound having the properties of equation (1): R 1 is selected from - C (o) nh483222;-C (O) NH (CH₃) and -CN; R² is - (X) -R⁴,Where - (x) is a link, - ch8322-u -;and R⁴ is selected from H; C₁₋₃ alkyl,a. One to four groups were selected from - f y Oh; halogen; - CN; - so832221-c83183323;-C (O) N (alquil C)If - (x) is not -- O-NHC (O) R o -N (CH) C (O) Rprovided that - (X) - is -CH₂- and where R⁵ is selected from C₃₋₆ cycloalkyl and C₁₋₃ alkyl,optionally substituted with one to three -F groups; -NHSO₂-C₁₋₃-alkyl;-CH (cyclopropyl) NHSO₂-C₁₋₃-alkyl;-OCH₂C (O) N (C₁₋₃ alkyl) ₂,If - (x) - is - ch8322a;-S (3DO) (3DNH) CHIf - (x) - is - ch8322a;heterocyclyl selected from tetrahydropyranyl, tetrahydrofuranyl, pyrrolidinyl, 1,1-dioxo [1,2] -thiazine, morpholinyl, oxazolidinyl, piperidinyl, azetidinyl, wherein said heterocyclyl is optionally substituted with one to three groups selected from -C (O) alkyl C₁₋₃,-Halogens - Oh, oxo and c832131 asphalt;-C (o) - isopropene, the condition is - (x) - sea-ch832222;a. The isomers were selected from morfolin-4-ilo, pirrolidin-1-ilo and piperidin-1-ilo, which can be replaced by one or two groups selected from - F and - Oh, cyclopentadienediol c83331 replaced by - CN u-oh;and R³ is H or C₁₋₃-alkyl optionally substituted with -OH; or R² and R³ together form a fused five-membered cycloalkyl ring optionally substituted with -OH; or one of its salts or stereoisomers.Reivindicación 1: Un compuesto, caracterizado porque tiene la fórmula (1) en donde: R¹ se selecciona de -C(O)NH₂, -C(O)NH(CH₃) y -CN; R² es -(X)-R⁴, en donde -(X)- es un enlace, -CH₂- u -O-; y R⁴ se selecciona de H; alquilo C₁₋₃, opcionalmente sustituido con uno a cuatro grupos seleccionados de -F y -OH; halógeno; -CN; -SO₂-alquilo C₁₋₃; -C(O)N(alquil C₁₋₃)₂, siempre que -(X)- no sea -O-; -NHC(O)R⁵ o -N(CH₃)C(O)R⁵, siempre que -(X)- sea -CH₂- y en donde R⁵ se selecciona de cicloalquilo C₃₋₆ y alquilo C₁₋₃, opcionalmente sustituido con uno a tres grupos -F; -NHSO₂-al
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