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    (4-PHENYL-PIPERIDIN-1-YL)-[5-1H-PYRAZOL-4YL)-THIOPHEN-3-YL]-METHANONE COMPOUNDS AND THEIR USE
    3.
    发明申请
    (4-PHENYL-PIPERIDIN-1-YL)-[5-1H-PYRAZOL-4YL)-THIOPHEN-3-YL]-METHANONE COMPOUNDS AND THEIR USE 审中-公开
    （4-苯基 - 哌啶-1-基） - [5-1H-吡唑并[4'] - 噻吩-3-基] - 甲酮化合物及其用途

    公开(公告)号：WO2011033255A1

    公开(公告)日：2011-03-24

    申请号：PCT/GB2010/001732

    申请日：2010-09-14

    Applicant: THE UNIVERSITY OF EDINBURGH ,  WEBSTER, Scott, Peter ,  SECKL, Jonathan, Robert ,  WALKER, Brian, Robert ,  WARD, Peter ,  PALLIN, Thomas, David ,  DYKE, Hazel, Joan ,  PERRIOR, Trevor, Robert

    Inventor： WEBSTER, Scott, Peter ,  SECKL, Jonathan, Robert ,  WALKER, Brian, Robert ,  WARD, Peter ,  PALLIN, Thomas, David ,  DYKE, Hazel, Joan ,  PERRIOR, Trevor, Robert

    IPC: C07D409/14 ,  C07D451/02 ,  C07D451/06 ,  A61K31/4439 ,  A61P3/00

    CPC classification number: C07D451/06 ,  C07D409/14 ,  C07D451/02

    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain (4-phenyl-piperidin-1-yl)- [5-(1 H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds that, inter alia, inhibit 11 β-hydroxysteroid dehydrogenase type 1 (11 β-HSD1 ). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 1 1 β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11 β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.

    Abstract translation: 本发明一般涉及治疗化合物领域。 更具体地，本发明涉及某些（4-苯基 - 哌啶-1-基） - [5-（1H-吡唑-4-基） - 噻吩-3-基] - 甲酮化合物，其特别是抑制11 β-羟基类固醇脱氢酶1型（11ß-HSD1）。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内都用于抑制1型1β-羟基类固醇脱氢酶的用途; 治疗通过抑制1型11-羟基类固醇脱氢酶而改善的病症; 治疗代谢综合征，其包括诸如2型糖尿病和肥胖症的疾病，以及包括胰岛素抵抗，高血压，脂质障碍和心血管疾病如缺血性（冠心病）心脏病的相关疾病; 治疗CNS疾病如轻度认知障碍和早期痴呆，包括阿尔茨海默氏病; 等等

    DIHYDRO-BENZO(1,4)OXAZINES AND TETRAHYDROQUINOXALINES
    4.
    发明申请
    DIHYDRO-BENZO(1,4)OXAZINES AND TETRAHYDROQUINOXALINES 审中-公开
    二氢苯并（1,4）氧化合物和四氢喹啉酮

    公开(公告)号：WO0039103B1

    公开(公告)日：2000-09-28

    申请号：PCT/GB9904430

    申请日：1999-12-23

    Applicant: AVENTIS PHARMA LTD ,  BOURZAT JEAN DOMINIQUE ,  COMMERCON ALAIN ,  FILOCHE BRUNO JACQUES CHRISTOP ,  HARRIS NEIL VICTOR ,  PALLIN THOMAS DAVID ,  STUTTLE KEITH ALFRED JAMES

    Inventor： BOURZAT JEAN-DOMINIQUE ,  COMMERCON ALAIN ,  FILOCHE BRUNO JACQUES CHRISTOP ,  HARRIS NEIL VICTOR ,  PALLIN THOMAS DAVID ,  STUTTLE KEITH ALFRED JAMES

    IPC: A61P11/06 ,  A61P29/02 ,  C07D241/38 ,  C07D265/36 ,  A61K31/495 ,  A61K31/535

    CPC classification number: C07D241/38 ,  C07D265/36

    Abstract: The invention is directed to physiologically active compounds of formula (I) wherein R represents R -Z , R -L -R -Z -, R -L -Ar -L -Z - or R -L -Ar -L -R -Z -; R represents hydrogen, halogen, lower alkyl or lower alkoxy; A represents a straight chain C2-3alkylene linkage optionally substituted by one or more groups chosen from alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, imino, oxo, thioxo, or alkyl substituted by -ZR , -NY Y , -CO2R or -C(=O)-NY Y ; L represents a direct bond; an alkenylene, alkylene, alkynylene, cycloalkenylene, cycloalkylene, heteroaryldiyl, heterocycloalkylene or arylene linkage each optionally substituted by (a) an acidic functional group, cyano, oxo, -S(O)mR , R , -C(=O)-R , -C(=O)-OR , -N(R )-C(=O)-R , -N(R )-C(=O)-OR , -N(R )-SO2-R , -NY Y or -[C(=O)-N(R )-C(R )(R )]p-C(=O)-NY Y , or by (b) alkyl substituted by an acidic functional group, or by S(O)mR , -C(=O)-NY Y or -NY Y ; a -[C(=O)-N(R )-C(R )(R )]p-linkage; a-Z -R -linkage; a -C(=O)-CH2-C(=O)-linkage; a -R -Z -R - linkage; a -C(R )(R )-[C(=O)-N(R )-C(R )(R )]p- linkage; or a -L -L -L - linkage; Z is NR or O; Y is carboxy or an acid bioisostere; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 ( alpha 4 beta 1).

    Abstract translation: 本发明涉及式（I）的生理活性化合物，其中R 1表示R 3 -Z 3，R 3 -L 2 -R 4 -Z 3 - ， R 3 -L 3 -Ar 1 -L 4 -Z 3 - 或R 3 -L 3 -Ar 1 -L 2 -R 4 -Z <3> - ; R 2表示氢，卤素，低级烷基或低级烷氧基; A 1表示任选被一个或多个选自烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，亚氨基，氧代，硫代基或被-ZR 6，-NY取代的烷基的基团取代的直链C 2-3亚烷基键。 1→Y 2，-CO 2 R 6或-C（= O）-NY 1 Y 2; L 1表示直接键; 亚烷基，亚炔基，亚环烯基，亚环烷基，杂芳基二基，杂环亚烷基或亚芳基，各自任选被（a）酸性官能团，氰基，氧代，-S（O）m R 9，R 3，-C （= O）-R 3，-C（= O）-OR 3，-N（R 8）-C（= O）-R 9，-N（R 8） -C（= O）-OR 9，-N（R 8）-SO 2 -R 9，-NY 4 Y 5或 - [C（= O） 10））-C（R 5）（R 11）] pC（= O）-NY 4 Y 5或（b）被酸官能团取代的烷基，或被S（ O）m R 9，-C（= O）-NY 4 Y 5或-NY 4 Y 5; a - [C（= O）-N（R 10）-C（R 5）（R 11）] p - 键; A-Z <2> -R <12> - 键; -C（= O）-CH 2 -C（= O） - 链接; -R 12 -Z 2 -R 12 - 键; -C（R 4）（R 13） - [C（= O）-N（R 10）-C（R 5）（R 11）] p键; 或-L 5 -L 6 -L 7 - 键; Z 1是NR 17或O; Y是羧基或酸生物电子等排体; 和相应的N-氧化物及其前药; 和这些化合物及其N-氧化物和前药的药学上可接受的盐和溶剂化物。 这些化合物具有有价值的药物性质，特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4（α4β1）的相互作用的能力。

    3, 3 -DISUBSTITUTED- ( 8 - AZA - BICYCLO [3.2.1] OCT- 8 - YL) -[5- (1H - PYRAZOL - 4 -YL) -THIOPHEN-3 -YL] METHANONES AS INHIBITORS OF 11 (BETA) -HSD1
    9.
    发明申请
    3, 3 -DISUBSTITUTED- ( 8 - AZA - BICYCLO [3.2.1] OCT- 8 - YL) -[5- (1H - PYRAZOL - 4 -YL) -THIOPHEN-3 -YL] METHANONES AS INHIBITORS OF 11 (BETA) -HSD1 审中-公开
    （8-AZA-BICYCLO [3.2.1] OCT-8-YL） - [5-（1H-吡唑-4-基） - 乙二醇] - 甲苯作为11的抑制剂（BETA ）-HSD1

    公开(公告)号：WO2011135276A1

    公开(公告)日：2011-11-03

    申请号：PCT/GB2011/000345

    申请日：2011-03-10

    Applicant: THE UNIVERSITY OF EDINBURGH ,  WEBSTER, Scott, Peter ,  SECKL, Jonathan, Robert ,  WALKER, Brian, Robert ,  WARD, Peter ,  PALLIN, Thomas, David ,  DYKE, Hazel, Joan ,  PERRIOR, Trevor, Robert

    Inventor： WEBSTER, Scott, Peter ,  SECKL, Jonathan, Robert ,  WALKER, Brian, Robert ,  WARD, Peter ,  PALLIN, Thomas, David ,  DYKE, Hazel, Joan ,  PERRIOR, Trevor, Robert

    IPC: C07D409/14 ,  C07D451/02 ,  C07D451/04 ,  C07D451/06 ,  A61K31/4535 ,  A61K31/46 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P25/00 ,  A61P25/28

    CPC classification number: C07D451/06 ,  C07D409/14 ,  C07D451/02 ,  C07D451/04

    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3,3- disubstituted -(8-aza- bicyclo [3.2.1]oct-8-yl)[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, 3,3- disubstituted- (6-aza-bicyclo[3.1.1]hept-6-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, and 4, 4- disubstituted piperidin-1 -yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds of the following formula (I) that, inter alia , inhibit 11 β-hydroxysteroid dehydrogenase type 1 (11 β-HSD1 ). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to inhibit 11 β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11 β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.

    Abstract translation: 本发明一般涉及治疗化合物领域。 更具体地，本发明涉及某些3,3-二取代 - （8-氮杂 - 双环[3.2.1]辛-8-基）[5-（1H-吡唑-4-基） - 噻吩-3-基] - 甲酮，3,3-二取代 - （6-氮杂 - 双环[3.1.1]庚-6-基） - [5-（1H-吡唑-4-基） - 噻吩-3-基] - 甲酮，和 4,4-二取代哌啶-1-基） - [5-（1H-吡唑-4-基） - 噻吩-3-基] - 甲酮化合物，特别是抑制11β- 羟基类固醇脱氢酶1型（11ß-HSD1）。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内两者抑制11型羟基类固醇脱氢酶1型的用途; 治疗通过抑制1型11-羟基类固醇脱氢酶而改善的病症; 治疗代谢综合征，其包括诸如2型糖尿病和肥胖症的疾病，以及包括胰岛素抵抗，高血压，脂质障碍和心血管疾病如缺血性（冠心病）心脏病的相关疾病; 治疗CNS疾病如轻度认知障碍和早期痴呆，包括阿尔茨海默氏病; 等等

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