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70 条记录 (耗时 0.079 秒)

    Carboxamide derivatives as therapeutic agents
    46.
    发明授权
    Carboxamide derivatives as therapeutic agents 失效
    甲酰胺衍生物作为治疗剂

    公开(公告)号：US07423177B2

    公开(公告)日：2008-09-09

    申请号：US10091759

    申请日：2002-03-05

    申请人： Adnan M. M. Mjalli ,  Robert C. Andrews ,  Ramesh Gopalaswamy ,  Chris Wysong

    发明人： Adnan M. M. Mjalli ,  Robert C. Andrews ,  Ramesh Gopalaswamy ,  Chris Wysong

    IPC分类号： C07C237/00 ,  C07C233/00 ,  C07C235/00 ,  A01N37/18

    CPC分类号： C07D231/12 ,  C07C235/38 ,  C07C237/20 ,  C07C271/22 ,  C07C2601/08 ,  C07C2603/18 ,  C07D207/16 ,  C07D211/34 ,  C07D217/26 ,  C07D233/56 ,  C07D249/08 ,  C07D309/04

    摘要： This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

    摘要翻译： 本发明提供某些化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作晚期糖基化终产物（RAGE）的受体与其配体如晚期糖基化终产物（AGE），S100 /钙粒蛋白/ EN-RAGE，β-淀粉样蛋白和两性蛋白之间相互作用的调节剂 ，以及由RAGE引起的人类疾病的管理，治疗，控制或辅助治疗。 这些疾病或疾病状态包括急性和慢性炎症，糖尿病晚期并发症的发展，例如血管通透性增加，肾病，动脉粥样硬化和视网膜病变，阿尔茨海默病的发展，勃起功能障碍和肿瘤侵袭和转移。

    Benzimidazole derivatives as therapeutic agents
    49.
    发明授权
    Benzimidazole derivatives as therapeutic agents 失效
    苯并咪唑衍生物作为治疗剂

    公开(公告)号：US07329684B2

    公开(公告)日：2008-02-12

    申请号：US11225277

    申请日：2005-09-13

    申请人： Adnan M. M. Mjalli ,  Ramesh Gopalaswamy

    发明人： Adnan M. M. Mjalli ,  Ramesh Gopalaswamy

    IPC分类号： A61K31/4184 ,  C07D235/14

    CPC分类号： A61K31/4188 ,  C07D235/14 ,  C07D235/16

    摘要： This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

    摘要翻译： 本发明提供某些化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作晚期糖基化终产物（RAGE）的受体与其配体如晚期糖基化终产物（AGE），S100 /钙粒蛋白/ EN-RAGE，β-淀粉样蛋白和两性蛋白之间相互作用的调节剂 ，以及由RAGE引起的人类疾病的管理，治疗，控制或辅助治疗。 这些疾病或疾病状态包括急性和慢性炎症，糖尿病晚期并发症的发展，例如血管通透性增加，肾病，动脉粥样硬化和视网膜病变，阿尔茨海默病的发展，勃起功能障碍和肿瘤侵袭和转移。

    Naphthalenedione nitric oxide synthase (NOS) inhibitors
    50.
    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.