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    Neurotransmitter releasers useful for cognition enhancement
    1.
    发明授权
    Neurotransmitter releasers useful for cognition enhancement 失效
    神经递质释放剂可用于认知增强

    公开(公告)号：US5532247A

    公开(公告)日：1996-07-02

    申请号：US392648

    申请日：1995-02-23

    申请人： Wendell W. Wilkerson ,  Richard A. Earl ,  Matthew E. Voss

    发明人： Wendell W. Wilkerson ,  Richard A. Earl ,  Matthew E. Voss

    IPC分类号： C07D213/50 ,  C07D401/06 ,  C07D403/06 ,  A61K31/44 ,  C07D213/16 ,  C07D213/18 ,  C07D213/26

    CPC分类号： C07D401/06 ,  C07D213/50 ,  C07D403/06

    摘要： Compounds of Formula I have been shown to enhance the release of the neurotransmitter acetylcholine and thus may be useful in the treatment of diseases learning and cognition.The compounds of this invention are ##STR1## where Q is ##STR2## A and B are independently selected from H, R.sup.4, --OH and --OCOR.sup.4, orA and B together form .dbd.O, .dbd.S, .dbd.CH.sub.2, .dbd.CHR.sup.4, .dbd.C(R.sup.4), .dbd.NOH, .dbd.NOR.sup.4, 1,3-dioxane, 1,3-dioxolane, 1,3-dithiane or 1,3-dithiolane;R.sup.1 is 4-,3-, or 2-pyridyl, 2-fluoro-4-pyridyl or 3-fluoro-4-pyridyl;R.sup.3, R.sup.4 and R.sup.5 are herein defined;and physiologically suitable salts thereof.

    摘要翻译： 已经显示式I化合物增强神经递质乙酰胆碱的释放，因此可用于治疗疾病学习和认知。 本发明的化合物是其中Q为A且B独立地选自H，R 4，-OH和-OCOR 4或A和B一起形成= O，= S，= CH 2， = CHR 4，= C（R 4），= NOH，= NOR 4，1,3-二恶烷，1,3-二氧戊环，1,3-二噻烷或1,3-二硫戊环; R1是4-，3-或2-吡啶基，2-氟-4-吡啶基或3-氟-4-吡啶基; 本文定义R3，R4和R5; 和其生理适合的盐。

    Neurotransmitter releasers useful for cognition enhancement
    2.
    发明授权
    Neurotransmitter releasers useful for cognition enhancement 失效
    神经递质释放剂可用于认知增强

    公开(公告)号：US5414004A

    公开(公告)日：1995-05-09

    申请号：US124523

    申请日：1993-09-20

    申请人： Wendell W. Wilkerson ,  Richard A. Earl ,  Matthew E. Voss

    发明人： Wendell W. Wilkerson ,  Richard A. Earl ,  Matthew E. Voss

    IPC分类号： C07D239/26 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/495 ,  A61P25/28 ,  C07D213/24 ,  C07D213/44 ,  C07D213/50 ,  C07D213/55 ,  C07D213/57 ,  C07D213/61 ,  C07D241/12 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D401/14

    CPC分类号： C07D401/06 ,  C07D213/50 ,  C07D213/55 ,  C07D213/57 ,  C07D403/06 ,  C07D405/06

    摘要： Compounds of the following formula have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man involving learning and cognition, where subnormal levels of this neurochemical are found ##STR1## wherein R.sup.1 is 4-,3-, or 2-pyridyl, 2-fluoro-4-pyridyl or 3-fluoro-4-pyridyl;R.sup.2 is alkyl of 1 to 10 carbons, cycloalkyl of 3 to 8 carbons, 2-,3-, or 4-pyridyl, Phe or Phe-W;Phe is a phenyl group;W is F, Cl, Br, R.sup.4, --OH, --OR.sup.4, --NO.sub.2, --NH.sub.2, --NHR.sup.4, --NR4R.sup.4, --CN, --S(O)m --R.sup.4 ;R.sup.3 is H, F, Cl, Br, --CN, --OH, --NO.sub.2, --NH.sub.2, --CF.sub.3, --NHR.sup.4, --NR.sup.4 R.sup.4, R.sup.4, --OR.sup.4, --S(O).sub.m --R.sup.4R.sup.4 is alkyl of 1 to 4 carbons, CH.sub.2 Phe-- or Phe--;R.sup.5 is --(CH.sub.2).sub.n --Y or --OCOR.sup.4 ;Y is NH.sub.2, --NHR.sup.4, --NR.sup.4 R.sup.4, --NHCOR.sup.4, --NHCO.sub.2 R.sup.4, F, Cl, Br, OR.sup.4, --S(O).sub.m R.sup.4, --CO.sub.2 H, --CO.sub.2 R.sup.4, --CN, --CONR.sup.4 R.sup.4, --CON HR.sup.4, CONHR.sup.4, --CONH.sub.2, --COR.sup.4 ; --CH.dbd.CHCO.sub.2 R.sup.4, OCOR.sup.4, CO.tbd.CCO.sub.2 R.sup.4, --CH.dbd.CHR.sup.4, or --C.tbd.CR.sup.4 ;m is 0, 1 or 2;n is 1 to 7;and physiologically suitable salts thereof.

    摘要翻译： 已经显示下式的化合物增强神经递质乙酰胆碱的释放，因此可用于治疗涉及学习和认知的人的疾病，其中发现该神经化学物质的次正常水平其中R1是4- ，3-或2-吡啶基，2-氟-4-吡啶基或3-氟-4-吡啶基; R2是1至10个碳的烷基，3至8个碳原子的环烷基，2-，3-或4-吡啶基，Phe或Phe-W; Phe是苯基; W是F，Cl，Br，R 4，-OH，-OR 4，-NO 2，-NH 2，-NHR 4，-NR 4 R 4，-CN，-S（O）m -R 4; R3是H，F，Cl，Br，-CN，-OH，-NO2，-NH2，-CF3，-NHR4，-NR4R4，R4，-OR4，-S（O）m -R4 R4是1〜 4个碳，CH2Phe-或Phe-; R5是 - （CH2）n-Y或-OCOR4; Y是NH 2，-NHR 4，-NR 4 R 4，-NHCOR 4，-NHCO 2 R 4，F，Cl，Br，OR 4，-S（O）m R 4，-CO 2 H，-CO 2 R 4，-CN，-CONR 4 R 4，-CON HR 4，CONHR 4， CONH2，-COR4; -CH = CHCO 2 R 4，OCOR 4，CO 3，CCO 2 R 4，-CH = CHR 4或-C 3 CH 3 CR 4; m为0,1或2; n为1〜7; 和其生理适合的盐。

    Nitric oxide enhancing diuretic compounds, compositions and methods of use
    5.
    发明授权
    Nitric oxide enhancing diuretic compounds, compositions and methods of use 失效
    一氧化氮增强利尿剂，组合物和使用方法

    公开(公告)号：US07396829B2

    公开(公告)日：2008-07-08

    申请号：US11360599

    申请日：2006-02-24

    申请人： David S. Garvey ,  L. Gordon Letts ,  Richard A. Earl ,  Maiko Ezawa ,  Xinqin Fang ,  Ricky D. Gaston ,  Subhash P. Khanapure ,  Chia-En Lin ,  Ramani R. Ranatunge ,  Cheri A. Stevenson ,  Shiow-Jyi Wey

    发明人： David S. Garvey ,  L. Gordon Letts ,  Richard A. Earl ,  Maiko Ezawa ,  Xinqin Fang ,  Ricky D. Gaston ,  Subhash P. Khanapure ,  Chia-En Lin ,  Ramani R. Ranatunge ,  Cheri A. Stevenson ,  Shiow-Jyi Wey

    IPC分类号： C07D417/02 ,  A61K31/549

    CPC分类号： C07D285/30 ,  C07D285/28 ,  C07D285/32 ,  C07D417/04 ,  C07D417/06 ,  C07D513/10

    摘要： The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia. The nitric oxide enhancing diuretic compounds comprise at least one nitric oxide enhancing group linked to the diuretic compound through one or more sites such as carbon, oxygen and/or nitrogen via a bond or moiety that cannot be hydrolyzed.

    摘要翻译： 本发明描述了包含至少一种一氧化氮增强利尿剂或其药学上可接受的盐，和任选的至少一种一氧化氮增强化合物和/或至少一种治疗剂的新型组合物和试剂盒。 本发明还提供了（a）处理由过量水和/或电解质滞留导致的条件的方法; （二）治疗心血管疾病; （c）治疗血管性疾病; （d）治疗糖尿病; （e）治疗由氧化应激引起的疾病; （f）治疗内皮功能障碍; （g）治疗由内皮功能障碍引起的疾病; （h）治疗肝硬化; （j）治疗先兆子痫; （k）治疗骨质疏松症; （l）治疗肾病; （m）治疗外周血管疾病; （n）治疗门静脉高压; （o）治疗中枢神经系统疾病; （p）治疗代谢综合症; （q）治疗性功能障碍; 和（r）高脂血症。 一氧化氮增强利尿化合物包含通过一个或多个位点如碳，氧和/或氮通过不能水解的键或部分与利尿剂化合物连接的至少一个一氧化氮增强基团。

    Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use
    6.
    发明授权
    Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use 失效

    公开(公告)号：US06462044B2

    公开(公告)日：2002-10-08

    申请号：US09941691

    申请日：2001-08-30

    申请人： David S. Garvey ,  Inigo Saenz de Tejada ,  Richard A. Earl ,  Subhash P. Khanapure

    发明人： David S. Garvey ,  Inigo Saenz de Tejada ,  Richard A. Earl ,  Subhash P. Khanapure

    IPC分类号： A61K31519

    CPC分类号： A61K31/195 ,  A61K31/075 ,  A61K31/21 ,  A61K31/34 ,  A61K31/40 ,  A61K31/44 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/50 ,  A61K31/501 ,  A61K31/519 ,  A61K45/06 ,  C07D405/14 ,  C07D487/04

    摘要： The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing diseases induced by the increased metabolism of cyclic guanosine 3′,5′-monophosphate (cGMP), such as hypertension, pulmonary hypertension, congestive heart failure, renal failure, myocardial infraction, stable, unstable and variant (Prinzmetal) angina, atherosclerosis, cardiac edema, renal insufficiency, nephrotic edema, hepatic edema, stroke, asthma, bronchitis, chronic obstructive pulmonary disease (COPD), cystic fibrosis, dementia, immunodeficiency, premature labor, dysmenorrhoea, benign prostatic hyperplasis (BPH), bladder outlet obstruction, incontinence, conditions of reduced blood vessel patency, e.g., postpercutaneous transluminal coronary angioplasty (post-PTCA), peripheral vascular disease, allergic rhinitis, glucoma, and diseases characterized by disorders of gut motility, e.g., irritable bowel syndrome (IBS).

    Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use
    10.
    发明授权
    Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use 有权
    硝化非甾体抗炎化合物，组合物和使用方法

    公开(公告)号：US07883714B2

    公开(公告)日：2011-02-08

    申请号：US12636306

    申请日：2009-12-11

    申请人： Richard A. Earl ,  Maiko Ezawa ,  Xinqin Fang ,  David S. Garvey ,  Ricky D. Gaston ,  Subhash P. Khanapure ,  L. Gordon Letts ,  Chia-En Lin ,  Ramani R. Ranatunge ,  Stewart K. Richardson ,  Joseph D. Schroeder ,  Cheri A. Stevenson ,  Shiow-Jyi Wey

    发明人： Richard A. Earl ,  Maiko Ezawa ,  Xinqin Fang ,  David S. Garvey ,  Ricky D. Gaston ,  Subhash P. Khanapure ,  L. Gordon Letts ,  Chia-En Lin ,  Ramani R. Ranatunge ,  Stewart K. Richardson ,  Joseph D. Schroeder ,  Cheri A. Stevenson ,  Shiow-Jyi Wey

    IPC分类号： A61K9/00 ,  A61K31/21 ,  C07C203/04

    CPC分类号： C07D493/04 ,  C07C291/02 ,  C07C311/17 ,  C07C317/18 ,  C07C323/12 ,  C07C327/28 ,  C07D209/18 ,  C07D211/22 ,  C07D211/56

    摘要： The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.

    摘要翻译： 本发明描述了新型亚硝化非甾体抗炎药（NSAID）及其药学上可接受的盐，以及包含至少一种亚硝化NSAID的新组合物，以及任选地至少一种捐赠，转移或释放一氧化氮的化合物，刺激一氧化氮的内源性合成 升高内源性内源性松弛因子水平，或是一氧化氮合酶的底物和/或至少一种治疗剂。 本发明还提供了包含至少一种亚硝化NSAID和至少一种捐赠，转移或释放一氧化氮的化合物的新型组合物，提高内源性内皮衍生的舒张因子水平，刺激一氧化氮的内源性合成，或是一氧化氮的底物 合酶和/或至少一种治疗剂。 本发明还提供了包含至少一种亚硝化NSAID和任选的至少一种一氧化氮供体和/或至少一种治疗剂的新型试剂盒。 本发明还提供了治疗炎症，疼痛和发烧的方法; 用于治疗胃肠道疾病; 促进伤口愈合; 用于治疗和/或预防由使用非甾体抗炎化合物引起的胃肠道，肾脏和/或呼吸道毒性物质; 用于治疗炎性疾病状态和/或病症; 并用于治疗和/或预防眼科疾病和/或病症。