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    Triazole derivatives which are SMO antagonists
    4.
    发明申请
    Triazole derivatives which are SMO antagonists 有权
    作为SMO拮抗剂的三唑衍生物

    公开(公告)号：US20080262051A1

    公开(公告)日：2008-10-23

    申请号：US12082933

    申请日：2008-04-15

    申请人： James M. Balkovec ,  Rolf Thieringer ,  Sherman T. Waddell

    发明人： James M. Balkovec ,  Rolf Thieringer ,  Sherman T. Waddell

    IPC分类号： A61K31/4245 ,  A61P35/00

    CPC分类号： A61K31/4196 ,  A61K31/4245

    摘要： The present invention provides a method for the treatment or prevention of conditions which can be ameliorated by Smo antagonism, which method comprises administration to a patient in need thereof of an effective amount of a compound of formula I or a composition comprising a compound of formula I: or a pharmaceutically acceptable salt or solvate thereof; wherein: 2 of X, Y and Z represent nitrogen atoms, and the other represents an oxygen atom; R1 and R2 are taken together with the atom to which they are attached and represent a cyclobutyl ring, optionally substituted with 1-2 fluorine atoms, and R3 represents hydrogen or a fluorine atom; or R1 represents methyl, R2 represents methyl or a fluorine atom and R3 represents a fluorine atom.

    摘要翻译： 本发明提供了治疗或预防可通过Smo拮抗作用改善的病症的方法，该方法包括向有需要的患者施用有效量的式I化合物或包含式I化合物的组合物 ：或其药学上可接受的盐或溶剂合物; 其中：X，Y和Z中的2个表示氮原子，另一个表示氧原子; R 1和R 2与它们所连接的原子一起表示任选被1-2个氟原子取代的环丁基环，R“ 3表示氢或氟原子; 或R 1表示甲基，R 2表示甲基或氟原子，R 3表示氟原子。

    11-&bgr;-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
    5.
    发明授权
    11-&bgr;-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia 有权
    用于治疗糖尿病，肥胖和血脂异常的11-β-羟基类固醇脱氢酶1抑制剂

    公开(公告)号：US06730690B2

    公开(公告)日：2004-05-04

    申请号：US10457682

    申请日：2003-06-09

    申请人： Steven H. Olson ,  James M. Balkovec ,  Yuping Zhu

    发明人： Steven H. Olson ,  James M. Balkovec ,  Yuping Zhu

    IPC分类号： A61K314196

    CPC分类号： C07D249/08

    摘要： Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: are selective inhibitors of the 11&bgr;-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.

    摘要翻译： 具有式I的化合物，包括其药学上可接受的盐，水合物和溶剂化物：是11beta-HSD1酶的选择性抑制剂。 这些化合物可用于治疗糖尿病，例如非胰岛素依赖性糖尿病（NIDDM），高血糖症，肥胖症，胰岛素抵抗，甲状腺脂肪血症，高脂血症，高血压，X综合征和与NIDDM相关的其他症状。

    Cyclohexapeptidyl amine compounds
    6.
    发明授权
    Cyclohexapeptidyl amine compounds 失效
    环己酰胺胺化合物

    公开(公告)号：US06268338B1

    公开(公告)日：2001-07-31

    申请号：US08055996

    申请日：1993-04-30

    申请人： James M. Balkovec ,  Frances Aileen Bouffard ,  James F. Dropinski ,  Robert A. Zambias

    发明人： James M. Balkovec ,  Frances Aileen Bouffard ,  James F. Dropinski ,  Robert A. Zambias

    IPC分类号： A61K3800

    CPC分类号： C07K7/56 ,  A61K38/00

    摘要： Cyclohexapeptidyl amine compounds are disclosed of the formula: or its acid addition salt, wherein: R1 is H or OH; R2 is H or OH; R3 is QCnH2nNRVRVI, QCnH2nNRVRVIRVII+Y−, or Q(CH2)1-3CRVIIIRIXNHRX. R4 is H or OH; R5 is H, OH or CH3; R6 is H or CH3; RI is wherein Ra is C1-C10 alkyl; or (CH2)qNRbRc wherein Rb and Rc are independently H, C1-C10 alkyl or Rb and Rc taken together are wherein Rd is C1-C16 alkyl, phenyl or benzyl; RII is H, C1-4 alkyl or benzyl; RIII is H, C1-4 alkyl or benzyl; RIV is RII and RIII taken together as —(CH2)4— or —(CH2)5—; RV is H, C1-C4 alkyl or benzyl; RVI is H, C1-C4 alkyl or benzyl or RV and RVI together is —(CH2)4— or —(CH2)5—; RVII is H or C1-C4 alkyl; RVIII is H, (CH2)mH, (CH2)mOH, (CH2)mNH2 or COX wherein X is NH2, OH or O(CH2)mH; RIX is H, (CH2)mH, or together with RVIII is ═O (carbonyl); RX is H (except when RVIII and RIX are H, C(═NH)NH2, C(═NH)CH2)0-3H, CO(CH2)0-3H, CO(CH2)mNH2, (CH2)2-4OH or (CH2)2-4NH2; Q is O or S; Y is an anion of a pharmaceutically acceptable salt each m is independently an integer from 1 to 3, inclusive; n is an integer from 2 to 4, inclusive; p is an integer from 1 to 2, inclusive and q is an integer from 2 to 4, inclusive.

    摘要翻译： 公开了下式：或其酸加成盐的环己酰胺化合物，其中：R1是H或OH; R2是H或OH; R3是QCnH2nNRVRVI，QCnH2nNRVRVIRVII + Y-或Q（CH2）1-3CRVIIIRIXNHRX.R4是H 或OH; R 5是H，OH或CH 3; R 6是H或CH 3; R 1是其中R a是C 1 -C 10烷基; 或（CH 2）q NR b R c其中R b和R c独立地为H，C 1 -C 10烷基或R b和R c在一起，其中R 1为C 1 -C 16烷基，苯基或苄基; R II为H，C 1-4烷基或苄基; R III为H，Cl -4-烷基或苄基; RIV是RII和RIII，一起作为 - （CH 2）4 - 或 - （CH 2）5 - ; RV是H，C 1 -C 4烷基或苄基; R VI是H，C 1 -C 4烷基或苄基或 RV和RVI一起是 - （CH 2）4 - 或 - （CH 2）5; RVII是H或C 1 -C 4烷基; RVIII是H，（CH 2）m H，（CH 2）m OH，（CH 2）m NH 2或COX，其中X是NH 2 ，OH或O（CH 2）m H; RIX为H，（CH 2）m H或与RVIII一起为=（（羰基））; RX为H（除非当RVIII和RIX为H时，C（= NH）NH 2，C（ = NH）CH 2）0-3H，CO（CH 2）0-3H，CO（CH 2）m NH 2，（CH 2）2-4 OH或（CH 2）2-4 NH 2; Q为O或S; Y为药学上阴离子 可接受的salteach m独立地为1〜3的整数，包括0和n; n为2〜4的整数，p为2〜4的整数，q为2〜4的整数。