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80 条记录 (耗时 0.04 秒)

    Naphthalenedione nitric oxide synthase (NOS) inhibitors
    63.
    发明授权
    Naphthalenedione nitric oxide synthase (NOS) inhibitors 失效

    公开(公告)号：US5866569A

    公开(公告)日：1999-02-02

    申请号：US928183

    申请日：1997-09-12

    申请人： Adnan M. M. Mjalli ,  Sepehar Sarshar ,  Chengzhi Zhang

    发明人： Adnan M. M. Mjalli ,  Sepehar Sarshar ,  Chengzhi Zhang

    IPC分类号： A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/12 ,  A61K31/415

    CPC分类号： A61K31/495 ,  A61K31/496

    摘要： There are disclosed methods useful for the inhibition of inducible nitric oxide synthase by the adminstration of a compound of the formula I:. when R.sub.2 is H then R.sub.1 is selected from the group consisting of:1) aryl,--NH--C.sub.0 -C.sub.10 alkyl -aryl, N-(C.sub.0 -C.sub.10 alkyl substituted aryl).sub.2, --C.sub.0 -C.sub.10 alkyl substituted aryl, --N(C.sub.0 -C.sub.10 alkyl substituted aryl)(C.sub.0 -C.sub.10 alkyl), wherein "Aryl" is optionally attached to Compound I through C or N and is selected from the group consisting of isoindanolyl, isoindolinyl, tetrahydroquinolyl, phenyl, naphthyl, pyridyl, furyl, pyrryl, thienyl, isothiazolyl, imidazolyl, benzimidazolyl, triazolyl, tetrazolyl, pyrazinyl,pyrimidyl, quinolyl, isoquinolyl, benzofuryl, benzothienyl, pyrazolyl, indolyl, isoindolyl, purinyl, carbazolyl, isoxazolyl, thiazolyl, oxazolyl, benzthiazolyl, and benzoxazolyl; and the term "substituted aryl" denotes mono-, di- and/or tri-substituted aryl wherein aryl is as defined above and in which the substituents are independently selected from the group consistng of H, trifluoromethyl, amino, hydroxy, halo, nitro, --O--C.sub.1 -C.sub.6 alkyl, --S--C.sub.1 -C.sub.6 alkyl, --NH--C.sub.1 -C.sub.6 alkyl, --N (C.sub.1 -C.sub.6 allyl).sub.2, --C(O) --C.sub.1 -C.sub.6 alkyl, --NHC(O) C.sub.1 -C.sub.6 alkyl, --C.sub.1 -C.sub.11 COO.sub.2 R wherein R.dbd.C.sub.1 -C.sub.11 alkyl, or --C.sub.1 -C.sub.11 alkylphenyl, --C.sub.1 -C.sub.11 CONHR wherein R.dbd.C.sub.1 -C.sub.11 alkyl or C.sub.1 -C.sub.11 alkylphenyl, carboxy, --C(O) O C.sub.1 -C.sub.6 alkyl; trans-CH.dbd.CHCO.sub.2 R; wherein R.dbd.C.sub.1 -C.sub.11 alkyl or C.sub.1 -C.sub.6 alkylphenyl, trans CH.dbd.CHCONHR; wherein R.dbd.C.sub.1 -C.sub.11 alkyl or C.sub.1 -C.sub.11 alkylphenyl;2) cyclic --N(CH.sub.2 CH.sub.2).sub.2 Y, cyclic NCHA(CH.sub.2).sub.3, or --NH C.sub.2 -C.sub.11 alkyl-Y wherein A=i) C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkylaryl or,ii) COZR.sub.3 wherein Z=oxygen, NH and R.sub.3 =H, or C.sub.1 -C.sub.10 alkyl, or C.sub.0 -C.sub.10 alkylaryl wherein aryl group is as defined in (1) above, and Y=i) oxygen,or S, or NH orii) NC.sub.0 -C.sub.10 alkyl oriii) NC.sub.1 -C.sub.10 alkylsubstituted aryl,iv) NC=ZMR.sub.3 or COZR.sub.3 wherein Z=oxygen, or NH; M=C, oxygen, N, and R.sub.3 is C.sub.0 -C.sub.10 alkyl substituted aryl; wherein Z is as defined in (2iv) above and R.sub.3 is C.sub.0 -C.sub.10 alkylsubstituted aryl wherein "substituted aryl" is as defined above.; R.sub.2 is hydrogen; or R.sub.1 and R.sub.2 taken together forming another aryl group; and X is hydrogen, halo, alkyl, alkoxy, hydroxy, nitro, amino, trifluoromethyl and aryl, to a patient in need of such inhibition such as hypotension, inflammtion, autoimmune diseases, and septic shock and the like.

    Biphenyl-3-carboxylic acid modulators of beta-3-adrenoreceptor
    65.
    发明授权
    Biphenyl-3-carboxylic acid modulators of beta-3-adrenoreceptor 失效
    β-3-肾上腺素受体的联苯-3-羧酸调节剂

    公开(公告)号：US08778998B2

    公开(公告)日：2014-07-15

    申请号：US12757444

    申请日：2010-04-09

    申请人： Chengzhi Zhang

    发明人： Chengzhi Zhang

    IPC分类号： A61K31/195 ,  C07C59/48

    CPC分类号： A61K31/196 ,  A61K31/136 ,  A61K45/06 ,  C07B2200/05 ,  C07C229/52

    摘要： The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof, wherein R1-R23 are independently selected from the group consisting of hydrogen and deuterium; and at least one of R1-R23 is deuterium.

    摘要翻译： 本发明涉及β-3-肾上腺素受体活性的新的联苯-3-羧酸调节剂，其药物组合物及其使用方法，其中R 1 -R 23独立地选自氢和氘; 并且R1-R23中的至少一个是氘。