发明名称 NOVEL CYCLOSPORIN DERIVATIVES AND USES THEREOF
摘要 The present invention relates to a compound of the Formula (I)): or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing viral infections, inflammation, dry eye, central nervous disorders, cardiovascular diseases, cancer, obesity, diabetes, muscular dystrophy, and hair loss.;
申请公布号 US2016039879(A1) 申请公布日期 2016.02.11
申请号 US201414775101 申请日期 2014.03.17
申请人 SU Zhengyu;LONG Zhengyu;YANG Suizhou;S&T Global Inc. 发明人 SU Zhuang;LONG Zhengyu;YANG Suizhou
分类号 C07K7/64 主分类号 C07K7/64
代理机构 代理人
主权项 1. A compound of Formula (I):or pharmaceutically acceptable salt thereof, wherein:R8 is n-butyl, (E)-but-2-enyl,—(CH2)4—SR9, —(CH2)4—(C═O)OR9, or —(CH2)3—(C═O)OR9;each occurrence of R9 is independently hydrogen or (C1-C6)alkyl;R2 is ethyl, 1-hydroxyethyl, isopropyl or n-propyl;W is O, CH2, NR1, or S;R1 is hydrogen; (C1-C6)alkyl, optionally substituted by one or more groups RD which may be the same or different; (C2-C6)alkenyl or (C2-C6)alkynyl; (C3-C7)cycloalkyl optionally substituted with (C1-C6)alkyl; phenyl optionally substituted with from one to five groups which may be the same or different selected from halogen, —O(C1-C6)alkyl, —C(═O)O(C1-C6)alkyl, amino, alkylamino and dialkylamino; or a heterocyclic ring which may be saturated or unsaturated containing five or six ring atoms and from one to three heteroatoms which may be the same or different selected from nitrogen, sulfur and oxygen; or R1 and R3 together with the nitrogen atom to which they are attached, form a saturated or unsaturated heterocyclic ring containing from three to seven ring atoms, which ring may optionally contain another heteroatom selected from the group consisting of nitrogen, oxygen and sulfur and may be optionally substituted by from one to four groups which may be the same or different selected from the group consisting of (C1-C6)alkyl, phenyl and benzyl;R3 is: (C7-C12)alkyl, optionally substituted by one or more groups R4 which may be the same or different, wherein one or more CH2 moiety in the alkyl chain may be optionally substituted by O or S; (C7-C12)alkenyl, optionally substituted by one or more groups which may be the same or different selected from halogen, hydroxy, amino, monoalkylamino and dialkylamino; or (C7-C12)alkynyl, optionally substituted by one or one or more groups which may be the same or different selected from halogen, hydroxy, amino, monoalkylamino and dialkylamino;R7 isR5 is: H; (C1-C6)alkyl, optionally substituted by one or more groups R6 which may be the same or different; (C2-C6)alkenyl, optionally substituted by one or more groups which may be the same or different selected from hydroxy, (C1-C6)alkyl, aryl, (CH2)pORA, O(CH2)mOH, O(CH2)mO(CH2)pOH, O(CH2)mNRARB, O(CH2)mO(CH2)mNRARB, (CH2)pNRARB, (CH2)pNRC(CH2)pNRARB, (CH2)pNRC(CH2)pNRC(CH2)pNRARB, (CH2)pC(═O)NRARB, (CH2)pC(═O)ORA; (C2-C6)alkynyl, optionally substituted by one or one or more groups which may be the same or different selected from halogen, hydroxy, amino, monoalkylamino and dialkylamino; (C3-C7)cycloalkyl, optionally substituted by one or more groups which may be the same or different selected from halogen, hydroxy, amino, monoalkylamino and dialkylamino; phenyl or CH2-phenyl, optionally substituted by one or more groups which may be the same or different selected from halogen, hydroxy, (C1-C6)alkyl, (CH2)pORA, (CH2)pNRARB, (CH2)pC(═O)NRARB, (CH2)pC(═O)ORA;each occurrence of R4 is independently halogen, hydroxy, (C3-C7)cycloalkyl, aryl, ORA, O(CH2)mORA, O(CH2)mO(CH2)mORA, C(═O)(C1-C6)alkyl, C(═O)ORA, C(═O)NRARB, —NRARB, —NRCCH2(CH2)pNRARB, NRC[CH2(CH2)pNRA]mCH2(CH2)nNRARB, O[CH2(CH2)pO]mCH2(CH2)nORA, OCH2(CH2)pNRARB, or O[CH2(CH2)pO]mCH2(CH2)nNRARB;each occurrence of R6 is independently halogen, hydroxy, aryl, S(C1-C6)alkyl, SRA, ORA, O(CH2)mORA, O(CH2)pO(CH2)pORA, C(═O)ORA, C(═O)NRARB, NRARB, O(CH2)mNRARB, O(CH2)mO(CH2)mNRARB, NRC(CH2)mNRARB, or NRC(CH2)mNRC(CH2)mNRARB, wherein said aryl or phenyl is optionally substituted by one or more groups which may be the same or different selected from halogen, hydroxy, (C1-C6)alkyl, (CH2)pORA, (CH2)pNRARB, (CH2)pC(═O)NRARB and (CH2)pC(═O)ORA;each occurrence of RA and RB is independently: hydrogen; (C1-C6)alkyl, optionally substituted by one or more groups RD which may be the same or different; (C2-C6)alkenyl or (C2-C6)alkynyl; (C3-C7)cycloalkyl optionally substituted with (C1-C6)alkyl; phenyl optionally substituted with from one to five groups which may be the same or different selected from halogen, —O(C1-C6)alkyl, —C(═O)O(C1-C6)alkyl, amino, alkylamino and dialkylamino; or a heterocyclic ring which may be saturated or unsaturated containing five or six ring atoms and from one to three heteroatoms which may be the same or different selected from nitrogen, sulfur and oxygen; or RA and RB, together with the nitrogen atom to which they are attached, form a saturated or unsaturated heterocyclic ring containing from three to seven ring atoms, which ring may optionally contain another heteroatom selected from the group consisting of nitrogen, oxygen and sulfur and may be optionally substituted by from one to four groups which may be the same or different selected from the group consisting of alkyl, phenyl and benzyl;each occurrence of RC is independently hydrogen or (C1-C6)alkyl;p is an integer of 0, 1, 2, 3, 4, or 5; andm is an integer of 1, 2, 3, 4 or 5.
地址 US