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Alternative nuclear analysis of the 6th-6th bicyclic aromatic ring for pmt5 inhibitors
专利权人:
JANSSEN PHARMACEUTICA NV
发明人:
申请号:
ARP160102600
公开号:
AR105820A1
申请日:
2016.08.25
申请国别(地区):
AR
年份:
2017
代理人:
摘要:
1. Claim 1: a formula compound (1),R1 represents hydrogen O-C (= O) - (c832131 / 83248ax);RZ represents hydrogen O-C (= O) - (c832131 / 83248ax);It stands for... O-CH₂- or -CF₂-;Z for - ch832222 -,-X-CR R --CR 3DCR --CR R -CR R - o -C C-And when it stands for - ch832222-o-cf832222-Z can also represent - o-o-cr-8309; - 7491; - r8309; - 7495x -;R⁵ᵃ,R⁵ᵇ,RRRR⁵ᶠ,R⁵ᵍ and R⁵ʰ each independently represent hydrogen or C₁₋₄ alkyl;X stands for... O-S-O-NHR1-R¹¹ represents hydrogen, C₁₋₄ alkyl or C₁₋₄ alkyl substituted with a substituent selected from the group consisting of -OH, -O- (C₁₋₄ alkyl),R2,-NH832222,-NH- (C₁₋₄-alkyl) and -N (C₁₋₄-alkyl) ₂;R2 represents a heterocyclic ring composed of 4, 5, 6 or 7 members, in which there is a nitrogen atom and an optional oxygen atom; in the ring, the heterocyclic ring consisting of 4, 5, 6 or 7 members is connected with the other parts of the molecule by a cyclic nitrogen atom; Ar stands for a ring-shaped double ring aromatic system composed of 10 members, consisting of 6 compressed members. Optionally, one nitrogen atom is used to replace one carbon atom, provided that when the nitrogen atom replaces one of the two concentrated carbon atoms, one carbon group is It exists in the system;AR was replaced by one, two, three or four substitutes selected from the halo group;-NH- (C₁₋₄-alkyl),-N (C₁₋₄ alkyl) ₂,-NHR¹⁰ᵈ,-8304; 7580; 830404; 74969;cyano, -CF₃,-C (3DO) -NH-C (= O) - NH - (lessor c832131;-C (= O) - (c83218331 = 83248)C₁₋₄-C-alkyloxy (= O) -O- (C₁₋₄-alkyl),cycloalkyl C₃₋₆,-O- (C₃₋₆ cycloalkyl),-NH- (C₃₋₆ cycloalkyl),-N (cicloalquilo C)C₂₋₆ alkenyl,C₁₋₄-alkyl substituted with a C₁₋₄-alkyloxy and C₁₋₄-alkyl optionally substituted with a -NR¹⁰ᵃR¹⁰ᵇ;R¹⁰ᵃ and R¹⁰ᵇ each independently represent hydrogen or C₁₋₄ alkyl;R¹⁰ᶜ and R¹⁰ᵈ each independently represent C₃₋₆ cycloalkyl;R1 m3;R1 830808;C₃₋₆ cycloalkyl substituted with one, two or three substituents each independently selected from the group consisting of halo, -OH and -O- (C₁₋₄ al
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