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    COMPOUNDS ACTIVE AT THE GLUCOCORTICOID RECEPTOR II
    1.
    发明申请
    COMPOUNDS ACTIVE AT THE GLUCOCORTICOID RECEPTOR II 审中-公开
    在糖皮质激素受体II上具有活性的化合物II

    公开(公告)号：WO0243648A8

    公开(公告)日：2002-09-06

    申请号：PCT/IB0102302

    申请日：2001-11-28

    Applicant: KAROBIO AB ,  ABBOTT LAB ,  PELCMAN BENJAMIN ,  GUSTAFSSON ANNIKA ,  KYM PHILIP R

    Inventor： PELCMAN BENJAMIN ,  GUSTAFSSON ANNIKA ,  KYM PHILIP R

    IPC: C07D295/08 ,  A61K31/192 ,  A61K31/36 ,  A61K31/426 ,  A61K31/4409 ,  A61K31/4453 ,  A61K31/5375 ,  A61P1/04 ,  A61P3/04 ,  A61P3/06 ,  A61P3/08 ,  A61P3/10 ,  A61P3/14 ,  A61P5/46 ,  A61P7/02 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P15/08 ,  A61P17/00 ,  A61P17/02 ,  A61P19/02 ,  A61P19/08 ,  A61P25/02 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P27/00 ,  A61P27/06 ,  A61P29/00 ,  A61P31/18 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07C59/90 ,  C07C69/76 ,  C07C205/34 ,  C07C205/35 ,  C07C323/12 ,  C07D213/30 ,  C07D277/24 ,  C07D295/092 ,  C07D317/62 ,  A61K

    CPC classification number: C07D213/30 ,  C07C59/90 ,  C07C69/76 ,  C07C205/35 ,  C07C323/12 ,  C07D277/24 ,  C07D295/088 ,  C07D317/62

    Abstract: This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula 1: wherein X is selected from: CH2, CHYR , CHYC(O)R , C=O, C=S, and C=NOR ,; Y is selected from: O, S, and NR ; R is selected from: COOH and heteroaryl; R and R are independently of each other selected from: hydrogen, halogen, and C1-6 alkyl, provided that one of R or R is other than hydrogen; R is selected from: C1-6-alkyl, C2-6 alkenyl, C2-6-alkynyl, halogen, (R )(R )N, R C(Z)N(R ), R OC(Z)N(R ), (R )(R )NC(Z)N(R ),R S(O)2N(R ), (R )(R )NS(O)2N(R ), and R SC (Z)N(R );R is selected from: (i) C1-6-alkyl which is substituted by a group selected from A, provided that A is not halogen; (ii) C7-12-alkyl, C2-12-alkenyl and C2-12-alkynyl; (iii) C1-12-alkyl, where one or more carbon atoms are replaced by Y, and where one or more carbons are optionally substituted by a group selected from A, provided that if more than one carbon is replaced by Y, the said Y groups are not directly connected to each other; R is selected from: C1-12-alkyl, C3-8-cycloalkyl, C3-8-heterocycloalkyl, C2-6-alkenyl, and C2-6-alkynyl, aryl, and heteroaryl; R is optionally selected from hydrogen; R , R , R and R are independently of each other selected from: hydrogen, C1-6-alkyl, C3-8-cycloalkyl, C2-6-alkenyl, C2-6-alkynyl, and C3-8-heterocycloalkyl, aryl and heteroaryl; or where any pair of R , R , R and R together with the atom or atoms to which they are bound form a ring having 3-7 ring members; or pharmaceutically acceptable salts, stereoisomers or prodrugs thereof.

    Abstract translation: 本发明涉及作为肝选择性糖皮质激素受体拮抗剂的新化合物，制备这些化合物的方法，以及在治疗和调节代谢，特别是降低血糖水平中使用这些化合物的方法。 所提及的化合物是根据式1的化合物：其中X选自：CH 2，CHYR 7，CHYC（O）R 7，C = O，C = S和C = NOR 8， ; Y选自：O，S和NR 8; R 1选自：COOH和杂芳基; R 2和R 3彼此独立地选自：氢，卤素和C 1-6烷基，条件是R 2或R 3中的一个不是氢; R 4选自：C 1-6 - 烷基，C 2-6烯基，C 2-6 - 炔基，卤素，（R 9）（R 10）N，R 8 C（Z）N （R 11），R 8 OC（Z）N（R 11），（R 9）（R 10）NC（Z）N（R 11），R 8 （O）2 N（R 11），（R 9）（R 10）NS（O）2 N（R 11）和R 8 SC（Z）N（R 10） R 5选自：（i）被选自A的基团取代的C 1-6 - 烷基，条件是A不是卤素; （ii）C 7-12 - 烷基，C 2-12 - 烯基和C 2-12 - 炔基; （iii）其中一个或多个碳原子被Y取代并且其中一个或多个碳任选被选自A的基团取代的C 1-12 - 烷基，条件是如果多于一个碳被Y取代，则所述 Y组不直接相互连接; R 6选自：C 1-12 - 烷基，C 3-8 - 环烷基，C 3-8 - 杂环烷基，C 2-6 - 烯基和C 2-6 - 炔基，芳基和杂芳基; R 7任选地选自氢; R 8，R 9，R 10和R 11彼此独立地选自：氢，C 1-6 - 烷基，C 3-8 - 环烷基，C 2-6 - 链烯基，C 2-6 炔基和C 3-8 - 杂环烷基，芳基和杂芳基; 或者其中任何一对R 8，R 9，R 10和R 11与它们所键合的一个或多个原子一起形成具有3-7个环成员的环; 或其药学上可接受的盐，立体异构体或前药。

    COMPOUNDS ACTIVE AT THE GLUCOCORTICOID RECEPTOR II
    3.
    发明申请
    COMPOUNDS ACTIVE AT THE GLUCOCORTICOID RECEPTOR II 审中-公开
    化合物在GLUCOCORTICOID受体II中有活性

    公开(公告)号：WO0243648A2

    公开(公告)日：2002-06-06

    申请号：PCT/IB0102302

    申请日：2001-11-28

    Applicant: KAROBIO AB ,  ABBOTT LAB ,  PELCMAN BENJAMIN ,  GUSTAFSSON ANNIKA ,  KYM PHILIP R

    Inventor： PELCMAN BENJAMIN ,  GUSTAFSSON ANNIKA ,  KYM PHILIP R

    IPC: C07D295/08 ,  A61K31/192 ,  A61K31/36 ,  A61K31/426 ,  A61K31/4409 ,  A61K31/4453 ,  A61K31/5375 ,  A61P1/04 ,  A61P3/04 ,  A61P3/06 ,  A61P3/08 ,  A61P3/10 ,  A61P3/14 ,  A61P5/46 ,  A61P7/02 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P15/08 ,  A61P17/00 ,  A61P17/02 ,  A61P19/02 ,  A61P19/08 ,  A61P25/02 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P27/00 ,  A61P27/06 ,  A61P29/00 ,  A61P31/18 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07C59/90 ,  C07C69/76 ,  C07C205/34 ,  C07C205/35 ,  C07C323/12 ,  C07D213/30 ,  C07D277/24 ,  C07D295/092 ,  C07D317/62 ,  A61K

    CPC classification number: C07D213/30 ,  C07C59/90 ,  C07C69/76 ,  C07C205/35 ,  C07C323/12 ,  C07D277/24 ,  C07D295/088 ,  C07D317/62

    Abstract: This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula 1: wherein X is selected from: CH2, CHYR , CHYC(O)R , C=O, C=S, and C=NOR ,; Y is selected from: O, S, and NR ; R is selected from: COOH and heteroaryl; R and R are independently of each other selected from: hydrogen, halogen, and C1-6 alkyl, provided that one of R or R is other than hydrogen; R is selected from: C1-6-alkyl, C2-6 alkenyl, C2-6-alkynyl, halogen, (R )(R )N, R C(Z)N(R ), R OC(Z)N(R ), (R )(R )NC(Z)N(R ),R S(O)2N(R ), (R )(R )NS(O)2N(R ), and R SC (Z)N(R );R is selected from: (i) C1-6-alkyl which is substituted by a group selected from A, provided that A is not halogen; (ii) C7-12-alkyl, C2-12-alkenyl and C2-12-alkynyl; (iii) C1-12-alkyl, where one or more carbon atoms are replaced by Y, and where one or more carbons are optionally substituted by a group selected from A, provided that if more than one carbon is replaced by Y, the said Y groups are not directly connected to each other; R is selected from: C1-12-alkyl, C3-8-cycloalkyl, C3-8-heterocycloalkyl, C2-6-alkenyl, and C2-6-alkynyl, aryl, and heteroaryl; R is optionally selected from hydrogen; R , R , R and R are independently of each other selected from: hydrogen, C1-6-alkyl, C3-8-cycloalkyl, C2-6-alkenyl, C2-6-alkynyl, and C3-8-heterocycloalkyl, aryl and heteroaryl; or where any pair of R , R , R and R together with the atom or atoms to which they are bound form a ring having 3-7 ring members; or pharmaceutically acceptable salts, stereoisomers or prodrugs thereof.

    Abstract translation: 本发明涉及作为肝选择性糖皮质激素受体拮抗剂的新型化合物，制备这些化合物的方法，以及在治疗和调节代谢中尤其是降低血糖水平使用这些化合物的方法。 所谓的化合物是根据式1的化合物：其中X选自：CH 2，CHYR 7，CHYC（O）R 7，C = O，C = S和C = NOR 8， ; Y选自：O，S和NR 8; R 1选自：COOH和杂芳基; R 2和R 3彼此独立地选自：氢，卤素和C 1-6烷基，条件是R 2或R 3中的一个不是氢; R 4选自：C 1-6 - 烷基，C 2-6烯基，C 2-6炔基，卤素，（R 9）（R 10）N，R 8 C（Z）N （R 11），R 8 OC（Z）N（R 11），（R 9）（R 10）NC（Z）N（R 11） S（O）2 N（R 11），（R 9）（R 10）NS（O）2 N（R 11）和R 8 SC（Z） 11））; R 5选自：（i）被选自A的基团取代的C 1-6 - 烷基，条件是A不是卤素; （ii）C 7-12 - 烷基，C 2-12 - 烯基和C 2-12 - 炔基; （iii）C 1-12 - 烷基，其中一个或多个碳原子被Y代替，并且其中一个或多个碳任选地被选自A的基团取代，条件是如果多于一个碳被Y替代，则所述 Y组不直接相连; R 6选自：C 1-12 - 烷基，C 3-8 - 环烷基，C 3-8 - 杂环烷基，C 2-6 - 烯基和C 2-6 - 炔基，芳基和杂芳基; R 7任选地选自氢; R 8，R 9，R 10和R 11彼此独立地选自：氢，C 1-6 - 烷基，C 3-8 - 环烷基，C 2-6烯基，C 2-6 - 炔基和C 3-8 - 杂环烷基，芳基和杂芳基; 或者其中任何一对R 8，R 9，R 10和R 11与它们所连接的原子或原子一起形成具有3-7个环成员的环; 或其药学上可接受的盐，立体异构体或前药。

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