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
    • 4. 发明申请
    • 2-(3-SULFONYLAMINO-2-OXOPYRROLIDIN-1-YL)PROPANAMIDES AS FACTOR XA INHIBITORS
    • 2-(3-磺酰氨基-2-氧代吡咯烷-1-基)丙酰胺作为因子XA抑制剂
    • WO2003043981A1
    • 2003-05-30
    • PCT/GB2002/005134
    • 2002-11-13
    • GLAXO GROUP LIMITEDBORTHWICK, Alan, DavidCAMPBELL, MatthewCHAN, ChuenKELLY, Henry, AndersonKING, Nigel, PaulKLEANTHOUS, SavvasMASON, Andrew, McMurtrieSENGER, StefanSMITH, Paul, WilliamWATSON, Nigel, StephenYOUNG, Robert, John
    • BORTHWICK, Alan, DavidCAMPBELL, MatthewCHAN, ChuenKELLY, Henry, AndersonKING, Nigel, PaulKLEANTHOUS, SavvasMASON, Andrew, McMurtrieSENGER, StefanSMITH, Paul, WilliamWATSON, Nigel, StephenYOUNG, Robert, John
    • C07D207/26
    • C07D207/273C07D401/12C07D403/12C07D405/12C07D409/12C07D409/14
    • The invention relates to compounds of formula (I), wherein: R 1 represents hydrogen or -C 1-3 alkylCONR a R b ; One of R 2 and R 3 represents -C 1-3 alkyl and the other represents hydrogen; R 4 represents hydrogen, -C 1-4 alkyl, -C 3-4 alkenyl, -C 2-4 alkylOH, -C 2-4 alkylOC 1-4 alkyl, -C 1-4 alkylCN or -C 0-4 alkylC 3-6 cycloalkyl; R 5 represents -C 2-4 alkylOH, -C 1-4 alkyl, -C 2-4 alkylOC 1-4 alkyl, -C 1-4 alkylCN, -C 1-4 alkylCONR c R d , -C 2-4 alkylNR a R b , -C 2-4 alkylNHCOC 1-3 alkyl, -C 2-4 alkylNHCONR a R b , -C2-4alkylNHSO 2 R e , -C 2-4 alkylSO 2 NR a R b , -C 2-4 alkylNHCO 2 C 1-4 alkyl, -C 2-4 alkylNHC(NH 2 )=NR f , or a group X-Y; X represents -C 1-4 alkylene- optionally substitued by -OH, or a direct link, with the proviso that when X is substituted by -OH, X represents C 2-4 alkylene and the -OH group is not alpha with respect to the amide N atom to which the group X is attached; Y represents -C 3-6 cycloalkyl, phenyl, or an aromatic or non-aromatic 5-, 6- or 7-membered heterocyclic group containing at least one heteroatom selected from O, N or S and optionally substituted at C and/or N atoms by -C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylOH, halogen, -CN, -CF 3 , -NH 2 , -CO 2 H and -OH; R a and R b independently represent hydrogen or -C 1-4 alkyl; R c and R d independently represent hydrogen or -C 1-4 alkyl or together with the N atom to which they are attached form a non-aromatic 5-, 6- or 7- membered heterocyclic group optionally substituted by a heteroatom selected from O, N or S; R e represents -C 1-4 alkyl or -CF 3 ; R f represents NO 2 or CN; R 6 represents a group selected from: (i), (ii), (iii), (iv), (v), Z represents an optional substituent halogen, alk represents alkylene or alkenylene, T represents a heteroatom selected from S or N; and pharmaceutically acceptable derivatives thereof. The invention also relates to processes for the preparation of compounds of formula (I), pharmaceutical compositions containing compounds of formula (I) and to the use of compounds of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
    • 本发明涉及式(I)化合物,其中:R 1表示氢或-C 1-3烷基CONR a R b; R 2和R 3中的一个表示-C 1-3烷基,另一个表示氢; R 4表示氢,-C 1-4烷基,-C 3-4链烯基,-C 2-4烷基,C 2-4烷基,C 1-4烷基,-C 1-4烷基,或C 0-4烷基。 R 5表示-C 2-4芳烷基,C 1-4烷基,-C 2-4烷基,C 1-4烷基,-C 1-4烷基,C 1-4烷基,C R 6,-C 2-4烷基,NR a R b, ,-C2-4烷基NHCOC1-3烷基,-C2-4烷基NHCORRαR2,-C2-4烷基NHSO2R5,-C2-4烷基,SO2NR,R2,-C2-4烷基,NHCO2C1-4烷基, 4烷基NH(NH 2)= NR或基团XY; X代表-C 1-4亚烷基 - 任选被-OH取代或直接连接,条件是当X被-OH取代时,X代表C2-4亚烷基,-OH基团相对于酰胺N原子不是α 组X连接到其上; Y代表-C3-6环烷基,苯基或含有至少一个选自O,N或S的杂原子的芳族或非芳族的5元,6元或7元杂环基,并且任选地在C和/或N原子被C -C 1-3烷基,C 1-3烷氧基,C 1-3烷基OH,卤素,-CN,-CF 3,-NH 2,-CO 2 H和-OH; R a和R b独立地表示氢或-C 1-4烷基; R c和R d独立地表示氢或-C 1-4烷基或与它们所连接的N原子一起形成任选被被选定的杂原子取代的非芳香族5-,6-或7-元杂环基 来自O,N或S; R e表示-C 1-4烷基或-CF 3; R表示NO2或CN; R 6表示选自以下的基团:(i),(ii),(iii),(iv),(v),Z表示任选的取代基卤素,alk表示亚烷基或亚烯基,T表示选自S 或N; 及其药学上可接受的衍生物。 本发明还涉及制备式(I)化合物的方法,包含式(I)化合物的药物组合物和式(I)化合物在医药中的用途,特别是在改善临床病症方面 指示因子Xa抑制剂。
    • 7. 发明申请
    • PYRROLYDIN-2-ONE DERIVATIVES AS INHIBITORS OF THROMBIN AND FACTOR XA
    • 作为硫蛋白和因子XA的抑制剂的吡咯烷-2-酮衍生物
    • WO2004052851A1
    • 2004-06-24
    • PCT/EP2003/013799
    • 2003-12-04
    • GLAXO GROUP LIMITEDBORTHWICK, Alan, DavidCHAN, ChuenKELLY, Henry, AndersonPEACE, SimonSENGER, StefanSHAH, Gita, PunjabhaiSMITH, Stephen, AllanSMITH, StevenWATSON, Nigel, StephenWEST, Robert, IanYOUNG, Robert, John
    • BORTHWICK, Alan, DavidCHAN, ChuenKELLY, Henry, AndersonPEACE, SimonSENGER, StefanSHAH, Gita, PunjabhaiSMITH, Stephen, AllanSMITH, StevenWATSON, Nigel, StephenWEST, Robert, IanYOUNG, Robert, John
    • C07D207/26
    • C07D207/273C07D401/12C07D405/12C07D409/06C07D409/12C07D409/14C07D413/06C07D413/14C07D417/06C07D417/12C07D417/14
    • The invention relates to compounds of formula (I), wherein : R 1 represents hydrogen, C 1-4 alkyl, -CH 2 CO 2 H, -CH 2 CO 2 C 1 - 2 alkyl, or -CH 2 CONR7R 8 ; R 2 and R 3 independently represent hydrogen, -C 1-6 alkyl, -C 1-3 alkylCN, -C 1-3 alkylCO 2 H, -C 1-4 alkylOC 1-4 alkyl, -C 1-4 alkylS(O) n C 1-4 alkyl, -C 1-4 alkylNR 10 R 11 , -C 1-3 alkylNCO 2 C 1-4 alkyl, -C 1-3 alkylCONR 7 R 8 , -C 1-3 alkylCO 2 C 0-2 alkylR 9 , -C 1-3 alkylCOC 0-2 alkylR 9 , -C 1-3 alkylCON(R 8 ) C 0-2 alkylR 9 , -C 1-3 alkylNCO 2 C 0-2 alkylR 9 , -C 1-3 alkylNCOC 0-2 alkylR 9 or -C 0-2 alkylR 9 , with the proviso that one of R 2 and R 3 is hydrogen and the other is a substituent other than hydrogen; n is an integer between 0 and 2; R 4 and R 5 together with the nitrogen atom to which they are attached form a morpholino ring; R 6 represents a group selected from formula (II) wherein T 1 and T 2 independently represent CH 2 , NH, S or O with the proviso that when one of T 1 or T 2 represents NH, S or O the other represents CH 2 ; M represents CH 3 , -OH or PO; V represents CH or N; W represents H, CH 3 , Cl or F; X represents C1, Br, F or -CH 3 ; Y represents CH 3 or CF 3 ; Z represents -CH 3 or F; R 7 and R 8 are independently hydrogen, C 1-4 alkyl or together with the N atom to which they are bonded form a 5- or 6- membered non-aromatic heterocyclic ring, optionally containing an additional heteroatom selected from O, N or S; R 10 and R 11 independently represent C 1-4 alkyl or together with the N atom towhich they are bonded form a 5- or 6- membered non-aromatic heterocyclic ring, optionally containing an additionalheteroatom selected from O, N or S; R 9 represents phenyl or a 5- or 6- membered aromatic or non-aromatic heterocyclic group, containing at least one heteroatom selected from O, N or S, each of which is optionally substituted by 0-2 groups selected from: C 1-3 alkyl or halogen; and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a thrombin inhibitor is indicated.
    • 本发明涉及式(I)化合物,其中:R 1表示氢,C 1-4烷基,-CH 2 CO 2 H,-CH 2 CO 2 C 1-2烷基或-CH 2 CONR 7 R 8; R 2和R 3独立地表示氢,-C 1-6烷基,-C 1-3烷基,C 1-3烷基CO 2 H,-C 1-4烷基,C 1-4烷基,-C 1-4烷基,(O)n C 1-4烷基,-C 1-4烷基NR R 11,-C 1-3烷基,CO 2 C 1-4烷基,-C 1-3烷基CONR 7 R 8,-C 1-3烷基CO 2 C 0-2烷基R 9,-C 1-3烷基C 0 -C 20 - 烷基R 9,-C 1- 3烷基CON(R 8)C 0-2烷基R 9,-C 1-3烷基,CO 2 C 0-2烷基R 9,-C 1-3烷基,C 1-10烷基,R 9或-C 0-2烷基R 9,条件是R 2和R 3是氢,另一个是氢以外的取代基; n是0和2之间的整数; R 4和R 5与它们所连接的氮原子一起形成吗啉代环; R 6表示选自式(II)的基团,其中T 1和T 2独立地表示CH 2,NH,S或O,条件是当T 1或T 2中的一个表示NH,S或O时,另一个表示CH 2; M代表CH3,-OH或PO; V表示CH或N; W表示H,CH 3,Cl或F; X表示C1,Br,F或-CH3; Y表示CH3或CF3; Z表示-CH 3或F; R 7和R 8独立地是氢,C 1-4烷基或与它们所键合的N原子一起形成5-或6-元非芳族杂环,任选地含有另外的选自O, N或S; R 10和R 11独立地表示C 1-4烷基或与其键合的N原子一起形成5-或6-元非芳族杂环,任选地含有选自O,N或S的另外的杂原子; R 9表示苯基或含有至少一个选自O,N或S的杂原子的5-或6-元芳族或非芳族杂环基,其中每一个可任选地被选自以下的0-2个基团取代:C1 烷基或卤素; 及其药学上可接受的衍生物,其制备方法,含有它们的药物组合物及其在医药中的用途,特别用于改善指示凝血酶抑制剂的临床病症。