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70 条记录 (耗时 0.079 秒)

    Heterocycle derivatives as PPAR-gamma agonists
    51.
    发明授权
    Heterocycle derivatives as PPAR-gamma agonists 失效
    杂环衍生物作为PPAR-γ激动剂

    公开(公告)号：US06462046B2

    公开(公告)日：2002-10-08

    申请号：US09734458

    申请日：2000-12-11

    申请人： Boliang Lou ,  Adnan M. M. Mjalli

    发明人： Boliang Lou ,  Adnan M. M. Mjalli

    IPC分类号： A61K31496

    CPC分类号： C07D401/06 ,  C07D241/04 ,  C07D241/08 ,  C07D405/12

    摘要： Compounds having the structure are peroxisome proliferator-activated receptor-gamma (PPAR-gamma) selective agonists and as such are useful in the modulation of blood glucose and the increase of insulin sensitivity in mammals. This activity of the piperazine derivatives of the invention make them particularly useful in the treatment of those conditions selected from the group consisting of diabetes, atherosclerosis, hyperglycemia, hyperlipidemia, obesity, syndrome X, insulin resistance, hypertension, heart failure and cardiovascular disease in mammals.

    摘要翻译： 具有结构的化合物是过氧化物酶体增殖物激活受体-γ（PPAR-γ）选择性激动剂，因此可用于调节血糖和哺乳动物胰岛素敏感性的增加。 本发明的哌嗪衍生物的这种活性使得它们特别可用于治疗选自以下的那些病症：糖尿病，动脉粥样硬化，高血糖症，高脂血症，肥胖症，综合征X，胰岛素抵抗，高血压，心力衰竭和哺乳动物心血管疾病 。

    Nucleic acid molecules encoding rage fusion proteins
    52.
    发明授权
    Nucleic acid molecules encoding rage fusion proteins 失效
    编码狂犬病融合蛋白的核酸分子

    公开(公告)号：US08344120B2

    公开(公告)日：2013-01-01

    申请号：US13158748

    申请日：2011-06-13

    申请人： Adnan M. M. Mjalli ,  Robert Rothlein ,  Ye Edward Tian ,  Jeffrey C. Webster

    发明人： Adnan M. M. Mjalli ,  Robert Rothlein ,  Ye Edward Tian ,  Jeffrey C. Webster

    IPC分类号： C07H21/04

    CPC分类号： C07K14/70503 ,  A61K38/00 ,  C07K2319/30 ,  C12N15/62

    摘要： Disclosed are RAGE fusion proteins comprising RAGE polypeptide sequences linked to a second, non-RAGE polypeptide. The RAGE fusion protein may utilize a RAGE polypeptide domain comprising a RAGE ligand binding site and an interdomain linker directly linked to the N-terminus of an immunoglobulin CH2 domain. Also disclosed are RAGE fusion protein formulations and the use of the RAGE fusion proteins and RAGE fusion protein formulations as therapeutics for RAGE-mediated pathologies.

    摘要翻译： 公开了包含与第二非RAGE多肽连接的RAGE多肽序列的RAGE融合蛋白。 RAGE融合蛋白可以利用包含RAGE配体结合位点的RAGE多肽结构域和直接连接到免疫球蛋白CH2结构域的N末端的域间连接。 还公开了RAGE融合蛋白制剂以及使用RAGE融合蛋白和RAGE融合蛋白制剂作为RAGE介导的病理学的治疗剂。

    Benzimidazole derivatives as therapeutic agents
    58.
    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
    59.
    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.