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61 条记录 (耗时 0.046 秒)

    Ring fused pyrazole derivatives as CRF antagonists
    11.
    发明授权
    Ring fused pyrazole derivatives as CRF antagonists 失效
    环稠合吡唑衍生物作为CRF拮抗剂

    公开(公告)号：US07053103B2

    公开(公告)日：2006-05-30

    申请号：US10914368

    申请日：2004-08-09

    申请人： David Garrett Loughhead ,  Counde O'Yang

    发明人： David Garrett Loughhead ,  Counde O'Yang

    IPC分类号： A61K31/44 ,  C07D471/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein Ar is optionally substituted aryl or heteroaryl, R1–R4 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.

    摘要翻译： 本发明涉及通常为CRF-1受体拮抗剂并由式I或式II表示的化合物：其中Ar为任选取代的芳基或杂芳基，R 1 -R 4， SUP>如规范中所定义; 或各异构体，异构体的外消旋或非外消旋混合物或其药学上可接受的盐。 本发明还涉及制备这些化合物的方法，含有这些化合物的药物组合物及其用作治疗剂的方法。

    Ring fused pyrazole derivatives as CRF antagonists
    14.
    发明授权
    Ring fused pyrazole derivatives as CRF antagonists 失效
    环稠合吡唑衍生物作为CRF拮抗剂

    公开(公告)号：US06821984B2

    公开(公告)日：2004-11-23

    申请号：US10308386

    申请日：2002-12-03

    申请人： David Garrett Loughhead ,  Counde O'Yang

    发明人： David Garrett Loughhead ,  Counde O'Yang

    IPC分类号： A61K31437

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein Ar is optionally substituted aryl or heteroaryl, R1-R4 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.

    摘要翻译： 本发明涉及通常为CRF-1受体拮抗剂并由式I或式II表示的化合物：其中Ar为任选取代的芳基或杂芳基，R 1 -R 4如说明书中所定义; 或各异构体，异构体的外消旋或非外消旋混合物或其药学上可接受的盐。 本发明还涉及制备这些化合物的方法，含有这些化合物的药物组合物及其用作治疗剂的方法。

    Substituted 2(4-piperidyl)-4(3H)-quinazolinones and 2-(4-piperidyl)-4(3H)-azaquinazolinones
    15.
    发明授权
    Substituted 2(4-piperidyl)-4(3H)-quinazolinones and 2-(4-piperidyl)-4(3H)-azaquinazolinones 失效
    取代的2（4-哌啶基）-4（3H） - 喹唑啉酮和2-（4-哌啶基）-4（3H） - 氮杂喹唑啉酮

    公开(公告)号：US06258819B1

    公开(公告)日：2001-07-10

    申请号：US09626806

    申请日：2000-07-27

    申请人： Robin Douglas Clark ,  Counde O'Yang

    发明人： Robin Douglas Clark ,  Counde O'Yang

    IPC分类号： A01N4354

    CPC分类号： C07D401/14 ,  C07D471/04

    摘要： This invention relates to compounds which are generally alpha1A/B-receptor antagonists and which are represented by Formula I: wherein the substituents are as defined in the specification; or pharmaceutically acceptable salts, hydrates, or N-oxides thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and a process for their preparation.

    摘要翻译： 本发明涉及通常为α1A/ B-受体拮抗剂并由式I表示的化合物：其中取代基如说明书中所定义; 或其药学上可接受的盐，水合物或N-氧化物。 本发明还涉及含有这些化合物的药物组合物，其用作治疗剂的方法及其制备方法。

    2-imidazoline, 2-oxazoline, 2-thiazoline, and 4-imidazole derivatives of methylphenyl, methoxyphenyl, and aminophenyl alkylsulfonamides and ureas and their use
    16.
    发明授权
    2-imidazoline, 2-oxazoline, 2-thiazoline, and 4-imidazole derivatives of methylphenyl, methoxyphenyl, and aminophenyl alkylsulfonamides and ureas and their use 失效
    2-咪唑啉，2-恶唑啉，2-噻唑啉和甲基苯基，甲氧基苯基和氨基苯基烷基磺酰胺和脲的4-咪唑衍生物及其用途

    公开(公告)号：US5952362A

    公开(公告)日：1999-09-14

    申请号：US89779

    申请日：1998-06-03

    申请人： Richard Leo Cournoyer ,  Paul Francis Keitz ,  Counde O'Yang ,  Dennis Mitsugu Yasuda

    发明人： Richard Leo Cournoyer ,  Paul Francis Keitz ,  Counde O'Yang ,  Dennis Mitsugu Yasuda

    IPC分类号： C07D233/20 ,  A61K31/00 ,  A61K31/415 ,  A61K31/4174 ,  A61K31/4178 ,  A61K31/42 ,  A61K31/421 ,  A61K31/425 ,  A61P3/00 ,  A61P3/04 ,  A61P13/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P27/00 ,  A61P27/16 ,  A61P43/00 ,  C07D20060101 ,  C07D209/08 ,  C07D233/08 ,  C07D233/22 ,  C07D233/24 ,  C07D233/50 ,  C07D233/54 ,  C07D233/64 ,  C07D233/66 ,  C07D263/28 ,  C07D263/38 ,  C07D263/64 ,  C07D277/10 ,  C07D277/18 ,  C07D277/28 ,  C07D277/34 ,  C07D277/38 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D413/06 ,  C07D413/12

    CPC分类号： C07D233/64 ,  C07D233/22 ,  C07D233/24 ,  C07D233/50 ,  C07D263/28 ,  C07D403/06 ,  C07D403/12

    摘要： The present invention concerns novel compounds represented by the Formula: ##STR1## wherein: A is R.sup.1.sub.q (R.sup.3 R.sup.60 N).sub.m (Z)(NR.sup.2).sub.n ; m and q are each 0 or 1, with the proviso that when q is 1, m is 0 and when q is 0, m is 1; Z is C.dbd.O or SO.sub.2 ; n is 1 with the proviso that, when Z is C.dbd.O, m is 1; X is --NH--, --CH.sub.2 --, or --OCH.sub.2 --; Y is 2-imidazoline, 2-oxazoline, 2-thiazoline, or 4-imidazole; R.sup.1 is H, lower alkyl, or phenyl, with the proviso that, when R.sup.1 is H, m is 1; R.sup.2, R.sup.3, R.sup.60 are each independently H, lower alkyl, or phenyl; R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are each independently hydrogen, lower alkyl, --CF.sub.3, lower alkoxy, halogen, phenyl, lower alkeny, hydroxyl, lower alkylsulfonamido, or lower cycloalkyl, wherein R.sup.2 and R.sup.7 optionally may be taken together to form alkylene or alkenylene of 2 to 3 atoms in an unsubstituted or optionally substituted 5- or 6-membered ring, wherein the optional substituents on the ring are halo, lower alkyl, or --CN, with the proviso that, when R.sup.7 is hydroxyl or lower alkylsulfonamido, then X is not --NH-- when Y is 2-imidazoline. The compounds include pharmaceutically acceptable salts of the above. In the above formula A may be, for example, (R.sup.1 SO.sub.2 NR.sup.2 --), (R.sup.3 R.sup.60 NSO.sub.2 NR.sup.2 --), or (R.sup.3 R.sup.60 NCONR.sup.2 --). The invention also includes the use of the above compounds, and compositions containing them, as alpha.sub.1A/1L agonists in the treatment of various disease states such as urinary incontinence, nasal congestion, priapism, depression, anxiety, dementia, senility, Alzheimer's, deficiencies in attentiveness and cognition, and eating disorders such as obesity, bulimia, and anorexia.

    摘要翻译： 本发明涉及由下式表示的新化合物：其中：A为R 1q（R 3 R 60 N）m（Z）（NR 2）n; m和q各自为0或1，条件是当q为1时，m为0，当q为0时，m为1; Z是C = O或SO 2; n为1，条件是当Z为C = O时，m为1; X是-NH-，-CH 2 - 或-OCH 2 - ; Y是2-咪唑啉，2-恶唑啉，2-噻唑啉或4-咪唑; R 1为H，低级烷基或苯基，条件是当R 1为H时，m为1; R 2，R 3，R 60各自独立地为H，低级烷基或苯基; R4，R5，R6和R7各自独立地为氢，低级烷基，-CF3，低级烷氧基，卤素，苯基，低级烯基，羟基，低级烷基亚磺酰氨基或低级环烷基，其中R2和R7任选地可以一起形成亚烷基 或未取代或任选取代的5元或6元环中2至3个原子的亚烯基，其中环上任选取代基为卤素，低级烷基或-CN，前提条件是当R 7为羟基或低级烷基亚磺酰氨基 那么当Y是2-咪唑啉时，X不是-NH-。 所述化合物包括上述药学上可接受的盐。 在上述式A中可以是例如（R 1 SO 2 NR 2 - ），（R 3 R 60 NSO 2 NR 2 - ）或（R 3 R 60 NCONR 2 - ）。 本发明还包括上述化合物和含有它们的组合物作为α1A/ 1L激动剂在治疗各种疾病状态如尿失禁，鼻充血，阴茎异常勃起，抑郁，焦虑，痴呆，衰老，阿尔茨海默病，阿尔茨海默病， 注意力和认知，以及进食障碍，如肥胖，贪食症和厌食症。

    IMIDAZOLINYLMETHYL ARYL SULFONAMIDE
    17.
    发明申请
    IMIDAZOLINYLMETHYL ARYL SULFONAMIDE 审中-公开
    咪唑啉基甲磺酸亚磺酰胺

    公开(公告)号：US20110230535A1

    公开(公告)日：2011-09-22

    申请号：US13152611

    申请日：2011-06-03

    申请人： Counde O'Yang ,  Robert Greenhouse

    发明人： Counde O'Yang ,  Robert Greenhouse

    IPC分类号： A61K31/4174 ,  C07D233/24 ,  A61P11/02 ,  A61P13/00

    CPC分类号： C07D233/24

    摘要： This invention relates to an alpha-1A receptor partial agonist, which is represented by Formula I: and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing formula I, methods for their use as therapeutic agents, and methods of preparation thereof.

    摘要翻译： 本发明涉及由式I表示的α-1A受体部分激动剂及其药学上可接受的盐或溶剂化物。 本发明还涉及含有式I的药物组合物，其用作治疗剂的方法及其制备方法。

    Ring fused pyrazole derivatives as CRF antagonists
    20.
    发明授权
    Ring fused pyrazole derivatives as CRF antagonists 失效
    环稠合吡唑衍生物作为CRF拮抗剂

    公开(公告)号：US07268146B2

    公开(公告)日：2007-09-11

    申请号：US11348036

    申请日：2006-02-06

    申请人： David Garrett Loughhead ,  Counde O'Yang

    发明人： David Garrett Loughhead ,  Counde O'Yang

    IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D471/02 ,  C07D491/02 ,  C07D498/02

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein Ar is optionally substituted aryl or heteroaryl, R1-R4 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.

    摘要翻译： 本发明涉及通常为CRF-1受体拮抗剂并由式I或式II表示的化合物：其中Ar为任选取代的芳基或杂芳基，R 1 -R 4， SUP>如规范中所定义; 或各异构体，异构体的外消旋或非外消旋混合物或其药学上可接受的盐。 本发明还涉及制备这些化合物的方法，含有这些化合物的药物组合物及其用作治疗剂的方法。