会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 2. 发明授权
    • SPIRO-AZACYCLIC DERIVATIVES, THEIR PREPARATION AND THEIR USE AS TACHYKININ ANTAGONISTS
    • 螺氮杂衍生物,生产与应用,速激肽拮抗剂
    • EP0929554B1
    • 2006-03-15
    • EP97919167.3
    • 1997-09-18
    • MERCK SHARP & DOHME LTD.
    • HAWORTH, Karen ElizabethSEWARD, Eileen MarySWAIN, Christopher John
    • C07D491/107A61K31/445C07D307/00C07D221/00
    • C07D491/10
    • Substituted spiro-azacyclic derivatives of structural formula (I), wherein R1 represents hydrogen, hydroxy, C¿1-6?alkyl, C2-6alkenyl, C3-7cycloalkyl optionally substituted alkyl, optionally substituted alkoxy, C2-6alkenyloxy, C3-7cycloalkoxy, phenoxy, benzyloxy, cyano, halogen, NR?11COR14, NRaRb, SRa, SORa, SO¿2Ra or OSO¿2R?a; R2 represents hydrogen, halogen, C¿1-6?alkyl or C1-6alkoxy; or when R?2¿ is adjacent to R1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; R4 represents hydrogen, halogen, C¿1-6?alkyl, C1-6alkoxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SR?a, SORa, SO¿2Ra, CO2R?a, CONRaRb, C¿2-6alkenyl, C2-6alkynyl or C1-4alkyl substituted by C1-4alkoxy; R5 represents hydrogen, halogen, C¿1-6?alkyl, trifluoromethyl or C1-6alkoxy substituted by C1-4alkoxy; R?6¿ represents hydrogen, CORa, CO2Ra, COCONRaRb, COCO¿2R?a, optionally substituted C¿1-6?alkyl; or R?6¿ represents a group of the formula -CH¿2?C CCH2NR?7R8; or R6¿ represents C¿1-6?alkyl, optionally substituted by oxo, substituted by a 5-membered or 6-membered heterocyclic ring containing 1, 2 or 3 nitrogen atoms optionally substituted by =O or =S and optionally substituted by a group of the formula ZNR?7R8; R9 and R10¿ each independently represents hydrogen, halogen, C¿1-6?alkyl, CH2OR?d¿, oxo, CO¿2R?a or CONRaRb; p is zero or 1; q is 1 or 2; and X represents -CH¿2?- or -CH2CH2-; Y represents -CH=, -CH2-, -CH2CH= or -CH2CH2-, with the proviso that the sum total of carbon atoms in X+Y is 2 or 3; and when X is -CH2- and Y is -CH= or -CH2CH=, the broken line represents a double bond; or a pharmaceutically acceptable salt thereof, are tachykinin receptor antagonists of use, for example, in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
    • 4. 发明授权
    • AZACYCLIC COMPOUNDS
    • AZACYCLIC化合物
    • EP0652866B1
    • 1998-11-25
    • EP93917877.8
    • 1993-07-20
    • MERCK SHARP & DOHME LTD.
    • SEWARD, Eileen MarySWAIN, Christopher John
    • C07D211/42C07D401/12C07D207/12C07D211/54A61K31/445A61K31/40
    • C07D401/12C07D207/12C07D211/42C07D211/54C07D405/12
    • Compounds of Formula (I), and salts and prodrugs thereof, wherein n is 1, 2 or 3; X represents O or S; R1 is optionally substituted phenyl; R2 is aryl or heteroaryl; R?4 and R5¿ are independently H, halo, C¿1-6?alkyl, oxo, CH2OR?a, CO¿2Ra or CONRaRb; R8 represents C(COORa)2, C(CONRaRb)2 or C1-6alkyl substituted by C(=NR?a)NRbNRcCO¿2Rd, CONHNRaRb, C(S)NR?aRb, CONRaC¿1-6alkylR?12, CONR13C¿2-6alkynyl, CONR13C2-6alkenyl, COCONR?aRb, CONRaC(NRb)NRcRd, CONR13SO¿2Ra, SO2NR?13CORa, CONRa¿heteroaryl or COR?q; Ra, Rb, Rc and Rd¿ are each H, C¿1-6?alkyl, phenyl or trifluoromethyl. R?12¿ represents OR?a, CONRaRb¿ or heteroaryl; R13 represents H or C¿1-6?alkyl; and R?q¿ represents a group (a) where Q represents the residue of a non-aromatic azacyclic or azabicyclic ring system; are tachykinin antagonists useful in therapy.
    • 式(I)化合物及其盐和前药,其中n为1,2或3; X代表O或S; R1是任选取代的苯基; R2是芳基或杂芳基; R 4和R 5独立地为H,卤素,C 1-6烷基,氧代,CH 2 OR a,CO 2 R a或CONR a R b; R 8代表C(COOR a)2,C(CONR a R b)2或被C(= NR a)NR b NR c CO 2 R d,CONHNR a R b,C(S)NR a R b,CONR a C 1-6烷基R 12,CONR 13 C CONR a C(NR b)NR c R d,CONR 13 SO 2 R a,SO 2 NR 13 R 13 R a,CONR a杂芳基或COR 2 q; Ra,Rb,Rc和Rd分别为H,C1-6烷基,苯基或三氟甲基。 R 12'代表OR'a,CONR a R b或杂芳基; R13代表H或C1-6烷基; R a表示基团(a),其中Q表示非芳族氮杂环或氮杂双环体系的残基; 是用于治疗的速激肽拮抗剂。
    • 9. 发明公开
    • SPIRO-AZACYCLIC DERIVATIVES, THEIR PREPARATION AND THEIR USE AS TACHYKININ ANTAGONISTS
    • 螺氮杂衍生物,生产与应用,速激肽拮抗剂
    • EP0929554A1
    • 1999-07-21
    • EP97919167.0
    • 1997-09-18
    • MERCK SHARP & DOHME LTD.
    • HAWORTH, Karen ElizabethSEWARD, Eileen MarySWAIN, Christopher John
    • A61P25A61K31A61P1A61P9A61P11A61P13A61P15A61P17A61P19A61P27A61P29A61P35A61P37A61P43C07D491
    • C07D491/10
    • Substituted spiro-azacyclic derivatives of structural formula (I), wherein R1 represents hydrogen, hydroxy, C¿1-6?alkyl, C2-6alkenyl, C3-7cycloalkyl optionally substituted alkyl, optionally substituted alkoxy, C2-6alkenyloxy, C3-7cycloalkoxy, phenoxy, benzyloxy, cyano, halogen, NR?11COR14, NRaRb, SRa, SORa, SO¿2Ra or OSO¿2R?a; R2 represents hydrogen, halogen, C¿1-6?alkyl or C1-6alkoxy; or when R?2¿ is adjacent to R1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; R4 represents hydrogen, halogen, C¿1-6?alkyl, C1-6alkoxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SR?a, SORa, SO¿2Ra, CO2R?a, CONRaRb, C¿2-6alkenyl, C2-6alkynyl or C1-4alkyl substituted by C1-4alkoxy; R5 represents hydrogen, halogen, C¿1-6?alkyl, trifluoromethyl or C1-6alkoxy substituted by C1-4alkoxy; R?6¿ represents hydrogen, CORa, CO2Ra, COCONRaRb, COCO¿2R?a, optionally substituted C¿1-6?alkyl; or R?6¿ represents a group of the formula -CH¿2?C CCH2NR?7R8; or R6¿ represents C¿1-6?alkyl, optionally substituted by oxo, substituted by a 5-membered or 6-membered heterocyclic ring containing 1, 2 or 3 nitrogen atoms optionally substituted by =O or =S and optionally substituted by a group of the formula ZNR?7R8; R9 and R10¿ each independently represents hydrogen, halogen, C¿1-6?alkyl, CH2OR?d¿, oxo, CO¿2R?a or CONRaRb; p is zero or 1; q is 1 or 2; and X represents -CH¿2?- or -CH2CH2-; Y represents -CH=, -CH2-, -CH2CH= or -CH2CH2-, with the proviso that the sum total of carbon atoms in X+Y is 2 or 3; and when X is -CH2- and Y is -CH= or -CH2CH=, the broken line represents a double bond; or a pharmaceutically acceptable salt thereof, are tachykinin receptor antagonists of use, for example, in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.