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    (4-PHENYL-PIPERIDIN-1-YL)-[5-1H-PYRAZOL-4YL)-THIOPHEN-3-YL]-METHANONE COMPOUNDS AND THEIR USE
    1.
    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

    PREPARATION OF HALOGENATED ALCOHOLS
    2.
    发明申请
    PREPARATION OF HALOGENATED ALCOHOLS 审中-公开
    氢化酒精的制备

    公开(公告)号：WO1996016010A1

    公开(公告)日：1996-05-30

    申请号：PCT/GB1995002571

    申请日：1995-11-02

    Applicant: ZENECA LIMITED ,  BOWDEN, Martin, Charles ,  BROWN, Stephen, Martin ,  PERRIOR, Trevor, Robert

    Inventor： ZENECA LIMITED

    IPC: C07C29/38

    CPC classification number: C07C29/38 ,  C07C33/423

    Abstract: The invention provides an improved process for preparing a halogenated alcohol of formula (I): CX X X -CH(OH)CH=C(CH3)2, wherein X , X and X are halo, which comprises reacting a compound of formula (II): CX X X H with 3-methylbut-2-en-1-al in the presence of a strong base and an inert solvent. The compounds of formula (I) are useful as intermediates in the manufacture of insecticides.

    Abstract translation: 本发明提供了制备式（I）的卤代醇的改进方法：CX 1 X 2 -X 3（CH 2）CH（OH）CH = C（CH 3）2，其中X 1， 2>和X 3是卤素，其包括使式（II）化合物：CX 1 X 2 X 3 H与3-甲基丁-2-烯-1-醇在存在下反应， 强碱和惰性溶剂。 式（I）的化合物可用作制造杀虫剂的中间体。

    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
    8.
    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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