首页> 外国专利> Derivatives of N - bencensulfonamida - 3.4 - diamino - 3 - substituted cyclobutene 1,2 Dione - - as antagonists of chemokine receptor CXCR2

Derivatives of N - bencensulfonamida - 3.4 - diamino - 3 - substituted cyclobutene 1,2 Dione - - as antagonists of chemokine receptor CXCR2

机译:N-苄磺酰氨基-3.4-二氨基-3-取代的环丁烯1,2,二酮--作为趋化因子受体CXCR2拮抗剂的衍生物。

摘要

Refers to bencen sulfonamide compounds of formula (i) wherein R1 is H, carbociclico (C3 - C10) (C1 - C6 alkyl, optionally substituted by Halogen), cn or Oh, among others; R2 is carbociclico (C3 - (C1 - C10), alkyl, alkoxyl (C1 - C6) optionally substituted C6), among others; R3 is H, haloge No or NC; R4 is H, alkyl, cycloalkyl (C1 C8) (C3, C8), among others; R5 is alkyl (C8, C1)Cycloalkyl (C3, C8) cicloalquenilo (C5 - C8), among others, is cr14 X or n, where R14 is H or alkyl (C1 - C6).Preferred compounds are: 6 - Chloro - 3 - [4 - [2 - ((R) - 1 - phenyl propyl amino) - ciclobut enil - amino] - 1 - hydroxy - 2 - methoxy - N - N - methyl - bencen sulfonamide, 6 - Chloro - hydroxy - 2 - N - N - Methyl - 3 - methoxy - {2 - [(R) - 1 - (2 - methyl - 5 - furan - yl) - propyl] - 4 - amino - ciclobut [- 1 - il - bencen sulfonamide amino} - 3, 6 - Chloro - {3,4 - [2 - [(S) - tetrahydro - thiophene-3 - yl) - amino] - ciclobut - il - 1 - amino) - 2-hydroxy-n - methoxy - N - methyl - bencen sulfonamide, among others. Also refers to a method of Preparation. These compounds are antagonists of chemokine receptor CXCR2 being useful in the treatment of chronic obstructive pulmonary disease, ovarian cancer, emphysema, pulmonary fibrosis
机译:指式(i)的苯磺酰胺化合物,其中R 1为H,咔唑基(C 3 -C 10)(C 1 -C 6烷基,任选地被卤素取代),cn或Oh;以及R2为卡波西科(C3-(C1-C10),烷基,烷氧基(C1-C6)任选取代的C6),等等。 R3是H,基序号或NC; R4为H,烷基,环烷基(C1-C8)(C3,C8)等; R 5是烷基(C 8,C 1)环烷基(C 3,C 8)环烷基萘(C 5-C 8)是cr 14 X或n,其中R 14是H或烷基(C 1-C 6)。 3-[4-[2-((R)-1-苯基丙基氨基)-环丁烯腈-氨基]-1-羟基-2-甲氧基-N-N-甲基-苯磺酰胺,6-氯-羟基-2 -N-N-甲基-3-甲氧基-{2-[(R)-1-(2-甲基-5-呋喃基)-丙基]-4-氨基-环丁草胺[-1-il-苄磺酰胺氨基}-3,6-氯-{3,4-[2-[(S)-四氢-噻吩-3-基)-氨基]-环丁酮-il-1-氨基)-2-羟基-n-甲氧基- N-甲基-苯磺酰胺,等等。也指制备方法。这些化合物是趋化因子受体CXCR2的拮抗剂,可用于治疗慢性阻塞性肺疾病,卵巢癌,肺气肿,肺纤维化

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