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    Indolizine Derivatives
    32.
    发明申请
    Indolizine Derivatives 审中-公开
    中氮衍生物

    公开(公告)号：US20090163534A1

    公开(公告)日：2009-06-25

    申请号：US11993412

    申请日：2006-06-26

    申请人： George Hynd ,  Nicholas Charles Ray ,  Harry Finch ,  David Middlemiss ,  Michael Colin Cramp ,  Paul Matthew Blaney ,  Karen Williams ,  Yan Griffon ,  Trevor Keith Harrison ,  Peter Crackett

    发明人： George Hynd ,  Nicholas Charles Ray ,  Harry Finch ,  David Middlemiss ,  Michael Colin Cramp ,  Paul Matthew Blaney ,  Karen Williams ,  Yan Griffon ,  Trevor Keith Harrison ,  Peter Crackett

    IPC分类号： A61K31/437 ,  C07D221/04 ,  A61P29/00

    CPC分类号： C07D471/04

    摘要： Compounds of formula (I) are ligands of the CRTH2 receptor and are useful in the treatment of respiratory disease: Formula (I) wherein R1, R2, R3 and R4 each independently are hydrogen, C1C6alkyl, fully or partially fluorinated C1C6alkyl, halo, —S(O)nR10, —SO2N(R10)2, —N(R10)2, —C(O)N(R10)2, —NR10C(O)R9, —CO2R10, —C(O)R9, —NO2, —CN or —OR11; wherein each R9 is independently C1C6alkyl, aryl, heteroaryl; R10 is independently hydrogen, C1C6alkyl, aryl, or heteroaryl; R11 is hydrogen, C1C6alkyl, fully or partially fluorinated C1C6alkyl or a group —SO2R9; n is 0, 1 or 2; R5 is C1C6alkyl, fully or partially fluorinated C1C6alkyl. C1C6alkenyl, C1C6alkynyl, optionally substituted aryl, or optionally substituted heteroaryl; R6 is hydrogen, C1C6alkyl or fully or partially fluorinated C1C6alkyl; R7 and R5 are independently hydrogen or C1C6alkyl, or R7 and R5 together with the atom to which they are attached form a cycloalkyl group; and X is —CHR6—, —S(O)n—, —NR6SO2— or —SO2NR6— wherein n is 0, 1 or 2.

    摘要翻译： 式（I）化合物是CRTH2受体的配体，可用于治疗呼吸系统疾病：其中R 1，R 2，R 3和R 4各自独立地为氢，C 1 -C 6烷基，完全或部分氟化的C 1 -C 6烷基，卤素， S（O）nR10，-SO2N（R10）2，-N（R10）2，-C（O）N（R10）2，-NR10C（O）R9，-CO2R10，-C（O） ，-CN或-OR11; 其中每个R 9独立地为C 1 -C 6烷基，芳基，杂芳基; R 10独立地是氢，C 1 -C 6烷基，芳基或杂芳基; R 11是氢，C 1 -C 6烷基，完全或部分氟化的C 1 -C 6烷基或基团-SO 2 R 9; n为0,1或2; R5是C1C6烷基，完全或部分氟化的C1C6烷基。 C 1 -C 6烯基，C 1 -C 6炔基，任选取代的芳基或任选取代的杂芳基; R6是氢，C1C6烷基或完全或部分氟化的C 1 -C 6烷基; R 7和R 5独立地为氢或C 1 -C 6烷基，或者R 7和R 5与它们所连接的原子一起形成环烷基; 且X为-CHR 6 - ， - S（O）n - ， - NR 6 SO 2 - 或-SO 2 NR 6 - ，其中n为0,1或2。

    Heterocyclic inhibitors of 5-.alpha.-testosterone reductase
    36.
    发明授权
    Heterocyclic inhibitors of 5-.alpha.-testosterone reductase 失效
    5-α-睾酮还原酶的杂环抑制剂

    公开(公告)号：US5302589A

    公开(公告)日：1994-04-12

    申请号：US927091

    申请日：1992-08-07

    申请人： Stephen V. Frye ,  David Middlemiss ,  Francis G. Fang

    发明人： Stephen V. Frye ,  David Middlemiss ,  Francis G. Fang

    IPC分类号： C07D471/06 ,  A61K31/435

    CPC分类号： C07D471/06

    摘要： The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10 whereinR.sup.9 and R.sup.10 arei) independently, hydrogen or lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower alkoxy, adamantyl, aryl, benzyl, diphenylmethyl, norbornyl orii) taken together with the linking nitrogen to form a 4 to 8 atom heterocyclic group, ##STR3## wherein; Y represents O, CH.sub.2, --N.dbd., NH or N(lower alkyl) optionally substituted with one or more lower alkyl groups;Ar is an aromatic group of 6 to 12 carbons;R.sup.4 is hydrogen or methyl;Z is --O--, --NH--, --N(lower alkyl), --S--, --SO--, --SO.sub.2, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, CO, CO.sub.2, O.sub.2 C, --N.dbd.N-- --CH.dbd.N-- or --N.dbd.CH--;n and m are independently 0, 1 or 2;and pharmaceutically acceptable salts thereof;their preparation, medical use and pharmaceutical formulations.

    摘要翻译： 本发明涉及式（I）的某些取代的17β-取代的羰基-6-氮杂雄甾-4-烯-3-酮：其中R 1和R 2独立地是氢或低级烷基， 带有R1和R2的碳之间的键是单键或双键，或ii）一起形成-CH 2 - 基以形成环丙烷环，并且具有R 1和R 2的碳之间的键是单键; X为，其中R 5，R 6，R 7和R 8独立地为氢或低级烷基，p和q独立地为0或1; R3为低级烷基，低级烯基，低级环烷基，低级烷氧基，硫代吡啶基，金刚烷基，-NR9R10或-Ar-NR9R10，其中R9和R10为i）独立地为氢或低级烷基，低级烯基，低级炔基，低级环烷基， ，金刚烷基，芳基，苄基，二苯甲基，降冰片基或ii）与连接氮一起形成4至8个原子的杂环基，其中; Y表示任选被一个或多个低级烷基取代的O，CH 2，-N =，NH或N（低级烷基） Ar为6〜12个碳原子的芳香族基团; R4是氢或甲基; Z是-O - ， - NH - ， - N（低级烷基），-S - ， - SO - ， - SO 2，-CH 2 CH 2 - ， - CH = CH-，CO，CO 2， CH = N-或-N = CH-; n和m独立地为0,1或2; 及其药学上可接受的盐; 其制剂，医疗用途和药物配方。