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
    • 1. 发明申请
    • PROCESS FOR PREPARING BICYCLIC COMPOUNDS
    • 制备双相化合物的方法
    • WO2006108689A2
    • 2006-10-19
    • PCT/EP2006/003480
    • 2006-04-06
    • SB PHARMCO PUERTO RICO INCNEUROCRINE BIOSCIENCES INCANDREOTTI, DanieleBACCHI, SergioDELPOGETTO, MonicaGUELFI, SimonePERBONI, AlcideRIBECAI, AriannaSPADA, SimoneSTABILE, PaoloTAMPIERI, Marsia
    • ANDREOTTI, DanieleBACCHI, SergioDELPOGETTO, MonicaGUELFI, SimonePERBONI, AlcideRIBECAI, AriannaSPADA, SimoneSTABILE, PaoloTAMPIERI, Marsia
    • C07D471/04A61K31/437A61P1/00A61P25/00
    • C07D471/04C07D207/22
    • The present invention relates to a novel process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper (I) (Ia)wherein R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C(O)R 5 , nitro, -NR 6 R 7 , cyano, and a group R 8 ; R 1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR 6 R 7 or cyano; R 5 is a C1-C4 alkyl, -OR 6 or -NR 6 R 7 ; R 6 is hydrogen or C1-C6 alkyl; R 7 is hydrogen or C1-C6 alkyl; R 8 is a 5-6 membered heterocycle, which may be saturated or may contain one to three double bonds, and which may be substituted by 1 or more R 11 groups; R 9 is a C1-C6 alkyl that may be substituted by one or more groups selected from: C3-C7 cycloalkyl, C1-C6 alkoxy, haloC1-C6 alkoxy, hydroxy, haloC1-C6 alkyl; R11 is C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, or C(O)NR 6 R 7 ; X is halogen; and R'' corresponds to R; R'' 1 corresponds to R 1 ; R 2 is hydrogen, C3-C7 cycloalkyl, or a group R 9 ; R 3 is C3-C7 cycloalkyl, or a group R 9 ; or R 2 and R 3 together with N form a 5-14 membered heterocycle, which may be substituted by 1 to 3 R 10 groups; R'' 4 is hydrogen; R'' 5 corresponds to R 5 ; R'' 6 corresponds to R 6 ; R'' 7 corresponds to R 7 ; R'' 8 corresponds to R 8 ; R'' 9 corresponds to R 9 ; R 10 is a group R 8 , C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, C(O)NR 6 R 7 , phenyl which may be substituted by 1 to 4 R 11 groups; R'' 11 corresponds to R 11 .
    • 本发明涉及由式(I)的中间体化合物通过铜催化的偶联反应制备式(IA)化合物的新方法,其为促肾上腺皮质激素释放因子(CRF)受体的有效和特异性拮抗剂 I)(Ia)其中R是芳基或杂芳基,其各自可以被1至4个选自以下的基团取代:卤素,C 1 -C 6烷基,C 1 -C 6烷氧基,卤代C 1 -C 6烷基,C 2 -C 6烯基,C 2 -C 6炔基,卤代C 1 -C 6烷氧基,C(O)R 5,硝基,-NR 6 R 7,氰基和 基团R 8; R 1是氢,C 1 -C 6烷基,C 2 -C 6烯基,C 2 -C 6炔基,卤代C 1 -C 6烷基,卤代C 1 -C 6烷氧基,卤素,NR 6 R 7或氰基; R 5是C 1 -C 4烷基,-OR 6或-NR 6 R 7; R 6是氢或C 1 -C 6烷基; R 7是氢或C 1 -C 6烷基; R 8是5-6元杂环,其可以是饱和的或可以含有一至三个双键,并且其可以被1个或更多个R 11个基团取代; R 9是可以被一个或多个选自以下的基团取代的C 1 -C 6烷基:C 3 -C 7环烷基,C 1 -C 6烷氧基,卤代C 1 -C 6烷氧基,羟基,卤代C 1 -C 6烷基; R 11是C 3 -C 7环烷基,C 1 -C 6烷基,C 1 -C 6烷氧基,卤代C 1 -C 6烷基,C 2 -C 6烯基,C 2 -C 6炔基,卤代C 1 -C 6烷氧基,羟基,卤素,硝基,氰基或C( O)NR 6 - [R 7 ; X是卤素; 并且R“对应于R; R“1 对应于R 1; R 2是氢,C 3 -C 7环烷基或基团R 9; R 3是C 3 -C 7环烷基或基团R 9; 或R 2和R 3与N一起形成5-14元杂环,其可以被1至3个R 10个基团取代; R“4是氢; R“5”对应于R 5; R“6”对应于R 6; R“7对应于R 7; R“8对应于R 8; R“9对应于R 9; R 10是基团R 8,C 3 -C 7环烷基,C 1 -C 6烷基,C 1 -C 6烷氧基,卤代C 1 -C 6烷基,C 2 -C 6链烯基, C 6炔基,卤代C 1 -C 6烷氧基,羟基,卤素,硝基,氰基,C(O)NR 6 R 7,可被1至4个R 11个组; R“”11“对应于R 11。
    • 4. 发明申请
    • PIPERIDYLCARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF TACHYKINIM-MEDIATED DISEASES
    • 哌啶甲酰胺衍生物及其在治疗TACHYKINIM介导性疾病中的应用
    • WO2003066589A1
    • 2003-08-14
    • PCT/GB2003/000499
    • 2003-02-05
    • GLAXO GROUP LIMITEDALVARO, GiuseppePAIO, AlfredoPONTIROLI, AlessandroSPADA, SimoneTRANQUILLINI, Maria, Elvira
    • ALVARO, GiuseppePAIO, AlfredoPONTIROLI, AlessandroSPADA, SimoneTRANQUILLINI, Maria, Elvira
    • C07D211/58
    • C07D401/04C07D211/58C07D405/12
    • The present invention relates to piperidine derivatives of formula (I) wherein R represents halogen or C 1-4 alkyl; R 1 represents hydrogen or C 1-4 alkyl; R 2 represents hydrogen , C 1-4 alkyl or R 2 together with R 3 represents C 3-7 cycloalkyl; R 3 represents hydrogen, C 1-4 alkyl, C 3-7 cycloalkyl or C 3-6 alkenyl; or R 1 and R 3 together with nitrogen and carbon atom to which they are attached respectively represent a 5 to 6 membered heterocyclic group; R 4 represents trifluoromethyl, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethoxy or halogen; R is hydrogen and R is NR 7 R 8 or R 5 is NR 8 R 9 and R 6 is hydrogen; R 7 represents hydrogen or C 1-4 alkyl or R 7 and R 8 together with nitrogen to which they are attached are a saturated 5 to 7 membered heterocyclic group containing oxygen; R 8 represents hydrogen, phenyl, C 3-7 cycloalkyl, (CH2)pC(O)NR 10 R 11 , a saturated 5 to 7 membered heterocyclic group containing 1 to 3 heteroatoms selected from oxygen, sulphur and nitrogen and optionally substituted by C 1-4 alkyl, S(O) 2 C 1-4 alkyl or C(O) C 1-4 alkyl, a 5 membered heteroaryl group containing 1 to 3 heteroatoms selected from oxygen, sulphur and nitrogen and optionally substituted by C 1-4 alkyl S(O) 2 C 1-4 alkyl or C(O) C 1-4 alkyl or R 8 represents a 6 membered heteroaryl group containing 1 to 3 nitrogen atoms and optionally substituted by C 1-4 alkyl, S(O) 2 C 1-4 alkyl or C(O) C 1-4 alkyl; or R 8 is a C 1-6 alkyl group optionally substituted by one or two groups selected from fluorine, phenyl(optionally substituted by C 1-4 alkyl, C(O) C 1-4 alkyl or halogen), =O, C 3-7 cycloalkyl, hydroxy, amino, dimethylamino, aminocarbonyl, C 1-4 alkoxy or trifluoromethyl; R 9 is hydrogen, C 1-4 alkyl or R 9 and R 8 together with nitrogen to which they are attached are a 5 to 7 membered heterocyclic group optionally containing another heroatom selected from oxygen, sulphur and nitrogen and optionally substituted by one or two groups selected from C 1-4 alkyl, =O, S(O) 2 C 1-4 alkyl, C(O) C 3-7 cycloalkyl or C(O) C 1-4 alkyl; R 10 and R 11 are independently hydrogen or C 1-4 alkyl group; X represents a nitrogen atom and Y is CH or X represents CH and Y is nitrogen;m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p is zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof; the process for their preparation and their use in the treatment of conditions mediated by tachykinins.
    • 本发明涉及式I的哌啶衍生物,其中R表示卤素或C 1-4烷基R 1表示氢或C 1-4烷基R 2表示氢,C 1-4烷基或R 2与R 3表示C 3-7环烷基R 3表示氢,C 1 -4-烷基,C 3-7环烷基或C 3-6烯基或R 1和R 3与它们所连接的氮原子和碳原子分别表示5至6元杂环基,R 4表示三氟甲基,C 1-4烷基,C 1-4烷氧基 ,三氟甲氧基或卤素R是氢,R是NR7R8或R5是NR8R9,R6是氢,R7代表氢或C1-4烷基或R7和R8与它们所连接的氮一起是含有氧的饱和5至7元杂环基 R 8表示氢,苯基,C 3-7环烷基,CH 2 pCONR 10 R 11,饱和5至7元杂环基,其含有1-3个选自氧,硫和氮的杂原子,且任选被C 1-4烷基,SO 2 C 1-4烷基或 CO C 1-4烷基,含有1至3个选自氧,硫和氮的杂原子并且任选被C 1-4烷基SO 2 C 1-4烷基或CO C 1-4烷基取代的5元杂芳基或R 8表示含有 1至3个氮原子,任选被C 1-4烷基,SO 2 C 1-4烷基或CO C 1-4烷基取代,或R 8是任选被一个或两个选自氟取代的C1-6烷基,被氟取代,被C1-4烷基取代 烷基,CO C 1-4烷基或卤素,= O,C 3-7环烷基,羟基,氨基,二甲基氨基,氨基羰基,C 1-4烷氧基或三氟甲基R 9是氢,C 1-4烷基或R 9和R 8与它们 任选地含有选自氧,硫和氮的另一个主原子,并且任选被一个或两个选自C 1-4烷基,O,SO 2 C 1-4烷基,CO C 3-7环烷基或基团的基团取代的5至7元杂环基, CO C 1-4烷基R 10和R 11独立地是氢或C 1-4烷基 基团X表示氮原子,Y表示CH或X表示CH,Y表示氮
    • 9. 发明申请
    • PIPERIDINE DERIVATIVES
    • 哌啶衍生物
    • WO2003066635A1
    • 2003-08-14
    • PCT/EP2003/001308
    • 2003-02-10
    • GLAXO GROUP LIMITEDALVARO, GiuseppeDI FABIO, RomanoTRANQUILLINI, Maria, ElviraSPADA, Simone
    • ALVARO, GiuseppeDI FABIO, RomanoTRANQUILLINI, Maria, ElviraSPADA, Simone
    • C07D487/04
    • C07D487/04A61K31/445
    • The present invention relates to piperidine derivatives of formula (I): R represents halogen or C 1-4 alkyl; R 1 represents C 1-4 alkyl; R 2 or R 3 independently represent hydrogen or C 1-4 alkyl; R 4 represents trifluoromethyl, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethoxy or halogen; R 5 represents hydrogen , C 1-4 alkyl or C 3-7 cycloalkyl; R 6 is hydrogen and R 7 is a radical of formula (W): R 6 is a radical of formula (W) and R 7 is hydrogen; X represents CH 2 , NR 5 or O; Y represents Nitrogen and Z is CH or Y represents CH and Z is Nitrogen; A represents C(O) or S(O)q, provided that when Y is nitrogen and Z is CH, A is not S(O)q; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p and q are independently an integer from 1 to 2; and pharmaceutically acceptable salts and solvates thereof. The process for their preparation and their use in the treatment of condition mediated by tachykinins.
    • 本发明涉及式(I)的哌啶衍生物:R代表卤素或C 1-4烷基; R1表示C1-4烷基; R2或R3独立地表示氢或C1-4烷基; R 4表示三氟甲基,C 1-4烷基,C 1-4烷氧基,三氟甲氧基或卤素; R5代表氢,C1-4烷基或C3-7环烷基; R6是氢,R7是式(W)的基团:R6是式(W)的基团,R7是氢; X表示CH 2,NR 5或O; Y表示氮,Z表示CH或Y表示CH,Z表示氮; A表示C(O)或S(O)q,条件是当Y为氮且Z为CH时,A不为S(O)q; m为0或1〜3的整数; n为1〜3的整数, p和q独立地为1至2的整数; 及其药学上可接受的盐和溶剂化物。 其制备方法及其用于治疗由速激肽介导的病症。