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    Potentiation of antihypertensive effect of ace inhibitors
    3.
    发明授权
    Potentiation of antihypertensive effect of ace inhibitors 失效
    强化抗抑郁药的降压作用

    公开(公告)号：US4962105A

    公开(公告)日：1990-10-09

    申请号：US109965

    申请日：1987-10-19

    申请人： Gary M. Ksander ,  Mark B. Zimmerman

    发明人： Gary M. Ksander ,  Mark B. Zimmerman

    IPC分类号： A61K31/44 ,  A61K31/55 ,  A61K45/00 ,  A61P9/12

    CPC分类号： A61K31/44 ,  A61K31/55

    摘要： Disclosed is a method of enhancing the antihypertensive effect of an angiotensin converting enzyme inhibitor which comprises the administration to mammals of an effective antihypertensive potentiating amount of 1-(7-carboxyheptyl)-3-methyl-2-(3-pyridyl)-indole, 1-methyl-2-(3-pyridyl)-3-)5-carboxypentyl)-5-chloroindole, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions comprising the 2-(3-pyridyl)-indole derivatie in combination with an angiotensin converting enzyme inhibitor.

    摘要翻译： 公开了一种增强血管紧张素转换酶抑制剂的降压作用的方法，其包括给予哺乳动物有效降压增强量的1-（7-羧基庚基）-3-甲基-2-（3-吡啶基） - 吲哚， 1-甲基-2-（3-吡啶基）-3-）-5-羧基戊基）-5-氯吲哚或其药学上可接受的盐。 还公开了包含与血管紧张素转换酶抑制剂组合的2-（3-吡啶基） - 吲哚衍生物的药物组合物。

    Amino-benzocycloalkane derivatives
    4.
    发明授权
    Amino-benzocycloalkane derivatives 失效
    氨基 - 苯并环烷烃衍生物

    公开(公告)号：US06197798B1

    公开(公告)日：2001-03-06

    申请号：US09357041

    申请日：1999-07-20

    申请人： Cynthia A. Fink ,  Gary M. Ksander ,  Paivi J. Kukkola ,  Eli M. Wallace ,  Mahavir Prashad

    发明人： Cynthia A. Fink ,  Gary M. Ksander ,  Paivi J. Kukkola ,  Eli M. Wallace ,  Mahavir Prashad

    IPC分类号： A61K3144

    CPC分类号： C07D213/82 ,  A61K31/17 ,  A61K31/44 ,  C07C233/80 ,  C07C235/22 ,  C07C235/56 ,  C07C237/20 ,  C07C237/40 ,  C07C237/42 ,  C07C271/24 ,  C07C271/34 ,  C07C271/36 ,  C07C271/56 ,  C07C275/26 ,  C07C301/00 ,  C07C307/08 ,  C07C311/07 ,  C07C311/08 ,  C07C311/20 ,  C07C311/29 ,  C07C313/06 ,  C07C313/12 ,  C07C317/14 ,  C07C323/60 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/12 ,  C07D213/71 ,  C07D261/18 ,  C07D295/088 ,  C07D295/15 ,  C07D295/215 ,  C07D333/34

    摘要： Compounds of the formula I wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, cycloalkyl or heterocyclyl; R2, R3, R4 and R5 are independently hydrogen, optionally substituted alkyl, halo, amino, substituted amino, trifluoromethyl, cyano, carboxyl, alkoxycarbonyl, aralkoxycarbonyl, (alkyl, aryl or aralkyl)-thio, (alkyl, aryl or aralkyl)-oxy, acyloxy, (alkyl, aryl or aralkyl)-aminocarbonyloxy; or any two of R2, R3, R4 and R5 at adjacent positions are alkylenedioxy; R6 is hydrogen, optionally substituted alkyl, amino, substituted amino, acylamino, wherein Ra is hydrogen or optionally substituted alkyl, Rb and Rc are independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; or Rb and Rc together represent lower alkylene or lower alkylene interrupted by O, S, or N—(H, alkyl or aralkyl); Rd is optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; and Re is optionally substituted alkyl, aryl, heterocyclyl, cycloalkyl, amino or substituted amino; and pharmaceutically acceptable salts thereof; and enantiomers thereof; which are useful as inhibitors of microsomal triglyceride transfer protein (MTP) and of apolipoprotein B (ApoB) secretion.

    摘要翻译： R 1，R 2，R 3，R 4和R 5可以被N代替，其中n是1,2或3; R 1是芳基，环烷基或杂环基; R 2，R 3，R 4和R 5 （烷基，芳基或芳烷基） - 硫代，（烷基，芳基或芳烷基） - 氧基，酰氧基，（烷基，芳基或芳烷基） 芳基或芳烷基） - 氨基羰基氧基; 或相邻位置的R 2，R 3，R 4和R 5中的任何两个是亚烷基二氧基; R 6是氢，任选取代的烷基，氨基，取代的氨基，酰氨基，其中R a是氢或任选取代的烷基，R b和R c独立地是氢，任选取代的烷基 ，环烷基，芳基或杂环基; 或R b和R c一起表示被O，S或N-（H，烷基或芳烷基）间隔的低级亚烷基或低级亚烷基; Rd为任选取代的烷基，环烷基，芳基或杂环基; 并且Re是任选取代的烷基，芳基，杂环基，环烷基，氨基或取代的氨基;及其药学上可接受的盐; 及其对映异构体; 其可用作微粒体甘油三酯转运蛋白（MTP）和载脂蛋白B（ApoB）分泌的抑制剂。

    Methods of treatment and pharmaceutical composition
    6.
    发明授权
    Methods of treatment and pharmaceutical composition 有权
    治疗方法和药物组成

    公开(公告)号：US08101659B2

    公开(公告)日：2012-01-24

    申请号：US12147570

    申请日：2008-06-27

    申请人： Gary M Ksander ,  Randy L Webb

    发明人： Gary M Ksander ,  Randy L Webb

    IPC分类号： A61K31/235 ,  A61K31/41 ,  A61K31/195

    CPC分类号： A61K31/41 ,  A61K31/192 ,  A61K31/197 ,  A61K31/216 ,  A61K31/222 ,  A61K45/06 ,  A61K2300/00

    摘要： The invention relates a pharmaceutical composition comprising a combination of: (i) the AT 1-antagonist valsartan or a pharmaceutically acceptable salt thereof; and (ii) a NEP inhibitor or a pharmaceutically acceptable salt thereof and optionally a pharmaceutically acceptable carrier and to a method for the treatment or prevention of a condition or disease selected from the group consisting of hypertension, heart failure, such as (acute and chronic) congestive heart failure, left ventricular dysfunction and hypertrophic cardiomyopathy, diabetic cardiac myopathy, supraventricular and ventricular arrhythmias, atrial fibrillation, atrial flutter, detrimental vascular remodeling, myocardial infarction and its sequelae, atherosclerosis, angina (whether unstable or stable), renal insufficiency (diabetic and non-diabetic), heart failure, angina pectoris, diabetes, secondary aldosteronism, primary and secondary pulmonary hypertension, renal failure conditions, such as diabetic nephropathy, glomerulonephritis, scleroderma, glomerular sclerosis, proteinuria of primary renal disease, and also renal vascular hypertension, diabetic retinopathy, the management of other vascular disorders, such as migraine, peripheral vascular disease, Raynaud's disease, luminal hyperplasia, cognitive dysfunction, such as Alzheimer's, glaucoma and stroke, comprising administering a therapeutically effective amount of the pharmaceutical composition to a mammal in need thereof.

    摘要翻译： 本发明涉及药物组合物，其包含以下组合：（i）AT 1拮抗剂缬沙坦或其药学上可接受的盐; 和（ii）NEP抑制剂或其药学上可接受的盐和任选的药学上可接受的载体，以及用于治疗或预防选自高血压，心力衰竭（如急性和慢性）的病症或疾病的方法 ）充血性心力衰竭，左心室功能障碍和肥大性心肌病，糖尿病性心肌病，室上性和室性心律失常，心房颤动，心房扑动，有害血管重塑，心肌梗死及其后遗症，动脉粥样硬化，心绞痛（不稳定或不稳定），肾功能不全 糖尿病和非糖尿病），心力衰竭，心绞痛，糖尿病，继发性醛固酮增多症，原发性和继发性肺动脉高压，肾衰竭病症如糖尿病性肾病，肾小球性肾炎，硬皮病，肾小球硬化，原发性肾脏疾病的蛋白尿，以及肾血管 高血压，糖尿病视网膜病变，管理 其他血管疾病如偏头痛，外周血管疾病，雷诺氏病，管腔增生，认知功能障碍如阿尔茨海默氏症，青光眼和中风，包括向有需要的哺乳动物施用治疗有效量的药物组合物。

    N-substituted butyramide derivatives useful for treatment of conditions responsive to inhibition of enkephalinase
    7.
    发明授权
    N-substituted butyramide derivatives useful for treatment of conditions responsive to inhibition of enkephalinase 失效
    用于治疗对脑啡肽酶抑制作用的病症的N-取代丁酰胺衍生物

    公开(公告)号：US4939261A

    公开(公告)日：1990-07-03

    申请号：US98755

    申请日：1987-09-17

    申请人： Gary M. Ksander

    发明人： Gary M. Ksander

    IPC分类号： C07C51/487 ,  C07C57/38 ,  C07C233/12 ,  C07D213/50 ,  C07D295/185 ,  C07D307/88 ,  C07J41/00

    CPC分类号： C07D295/185 ,  C07C255/00 ,  C07C51/487 ,  C07C57/38 ,  C07D213/50 ,  C07D307/88 ,  C07J41/0055

    摘要： Disclosed are compounds of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, 2-imidazolyl or 4,5-dihydro-2-imidazolyl or any said grouping substituted by lower alkyl; R and R.sub.0 independently represent hydrogen, lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl in which aryl represents phenyl, pyridyl, thienyl, furyl, biphenyl or naphthyl, each unsubstituted or mono- or di-substituted by halogen, lower alkyl, hydroxy, acyloxy, lower alkoxy, trifluoromethyl or cyano; A represents straight chain (C.sub.2 -C.sub.5)-alkylene; or A represents straight chain (C.sub.2 -C.sub.5)-alkylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by amino or acyl-amino, by amino-lower alkyl, by acylamino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, by aryl or aryl-lower alkyl in which aryl represents phenyl or phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy, acyloxy, trifluoromethyl or cyano; or A represents phenylene or cyclohexylene; pharmaceutically acceptable prodrug derivatives of any said compounds having a free carboxy group; pharmaceutically acceptable salts of any said compounds with a salt-forming group; methods for synthesis; pharmaceutical compositions thereof; and use thereof as enkephalinase inhibitors.

    摘要翻译： 公开了式（I）的化合物，其中X和Y独立地表示羟甲基; 氰基; 羧基; 选自酯化羧基，氨基甲酰基和N-取代的氨基甲酰基的官能改性羧基; 5-四唑基; 2-恶唑基，4,5-二氢-2-恶唑基，2-咪唑基或4,5-二氢-2-咪唑基或被低级烷基取代的任何所述基团; 吡啶基，噻吩基，呋喃基，联苯基或萘基，其中每个未取代或单 - 或二 - 取代的芳基 - 芳基 - 低级烷基， 被卤素，低级烷基，羟基，酰氧基，低级烷氧基，三氟甲基或氰基取代; A表示直链（C 2 -C 5） - 亚烷基; 或A表示被低级烷基，低级烷硫基 - 低级烷基，羟基 - 低级烷基，酰氧基 - 低级烷基，低级烷氧基 - 低级烷基，氨基或酰基 - 氨基取代的直链（C2-C5） - 亚烷基， 由（C 3 -C 7） - 环烷基，（C 3 -C 7） - 环烷基 - 低级烷基，被芳基或芳基 - 低级烷基取代，其中芳基或芳基 - 低级烷基，其中芳基表示苯基或苯基单 - 或 卤素，低级烷基，低级烷氧基，羟基，酰氧基，三氟甲基或氰基二取代; 或A表示亚苯基或亚环己基; 任何所述具有游离羧基的化合物的药学上可接受的前药衍生物; 任何所述化合物与成盐基团的药学上可接受的盐; 合成方法; 其药物组合物; 并将其用作脑啡肽酶抑制剂。

    N-substituted butyramide derivatives
    8.
    发明授权
    N-substituted butyramide derivatives 失效
    N-取代丁酰胺衍生物

    公开(公告)号：US5096925A

    公开(公告)日：1992-03-17

    申请号：US508141

    申请日：1990-04-11

    申请人： Gary M. Ksander

    发明人： Gary M. Ksander

    IPC分类号： A61K31/195 ,  C07C51/487 ,  C07C57/38 ,  C07C255/56 ,  C07D213/50 ,  C07D295/185 ,  C07D307/88 ,  C07J41/00

    CPC分类号： C07D295/185 ,  C07C255/00 ,  C07C51/487 ,  C07C57/38 ,  C07D213/50 ,  C07D307/88 ,  C07J41/0055

    摘要： Disclosed are compounds of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, 2-imidazoly or 4,5-dihydro-2-imidazolyl or any said grouping substituted by lower alkyl; R and R.sub.o independently represent hydrogen, lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl in which aryl represents phenyl, pyridyl, thienyl, furyl, biphenyl or naphthyl, each unsubstituted or mono- or di-substituted by halogen, lower alkyl, hydroxy, acyloxy, lower alkoxy, trifluoromethyl or cyano; A represents straight chain (C.sub.2 -C.sub.5)-alkylene; or A represents straight chain (C.sub.2 -C.sub.5)-alkylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by amino or acyl-amino, by amino-lower alkyl, by acylamino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, by aryl or aryl-lower alkyl in which aryl represents phenyl or phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy, acyloxy, trifluoromethyl or cyano; or A represents phenylene or cyclohexylene; pharmaceutically acceptable prodrug derivatives of any said compounds having a free carboxy group; pharmaceutically acceptable salts of any said compounds with a salt-forming group; methods for synthesis; pharmaceutical compositions thereof; and use thereof as enkephalinase inhibitors.

    摘要翻译： 公开了式（I）的化合物，其中X和Y独立地表示羟甲基; 氰基; 羧基; 选自酯化羧基，氨基甲酰基和N-取代的氨基甲酰基的官能改性羧基; 5-四唑基; 2-恶唑基，4,5-二氢-2-恶唑基，2-咪唑基或4,5-二氢-2-咪唑基或被低级烷基取代的任何所述基团; R和R 4独立地表示氢，低级烷基，（C 3 -C 7） - 环烷基 - 低级烷基或芳基 - 低级烷基，其中芳基表示苯基，吡啶基，噻吩基，呋喃基，联苯基或萘基， 被卤素，低级烷基，羟基，酰氧基，低级烷氧基，三氟甲基或氰基取代; A表示直链（C 2 -C 5） - 亚烷基; 或A表示被低级烷基，低级烷硫基 - 低级烷基，羟基 - 低级烷基，酰氧基 - 低级烷基，低级烷氧基 - 低级烷基，氨基或酰基 - 氨基取代的直链（C2-C5） - 亚烷基， 由（C 3 -C 7） - 环烷基，（C 3 -C 7） - 环烷基 - 低级烷基，被芳基或芳基 - 低级烷基取代，其中芳基或芳基 - 低级烷基，其中芳基表示苯基或苯基单 - 或 卤素，低级烷基，低级烷氧基，羟基，酰氧基，三氟甲基或氰基二取代; 或A表示亚苯基或亚环己基; 任何所述具有游离羧基的化合物的药学上可接受的前药衍生物; 任何所述化合物与成盐基团的药学上可接受的盐; 合成方法; 其药物组合物; 并将其用作脑啡肽酶抑制剂。

    Gamma-r-glutamoyl derivatives
    9.
    发明授权
    Gamma-r-glutamoyl derivatives 失效
    γ-氨基磺酰衍生物

    公开(公告)号：US4678800A

    公开(公告)日：1987-07-07

    申请号：US621302

    申请日：1984-06-15

    申请人： James L. Stanton ,  Gary M. Ksander

    发明人： James L. Stanton ,  Gary M. Ksander

    IPC分类号： C07D209/42 ,  C07D209/12 ,  A61K31/40

    CPC分类号： C07D209/42

    摘要： A compound of the formula ##STR1## wherein R.sub.1 and R.sub.6 independently represent hydroxy, C.sub.1 -C.sub.4 -alkoxy, substituted C.sub.1 -C.sub.4 - alkoxy, amino, or substituted amino, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 -alkyl, or C.sub.2 -C.sub.4 -alkenyl, R.sub.3 represents cyclo-C.sub.3 -C.sub.6 -alkyl, phenyl, phenyl substituted by C.sub.1 -C.sub.4 -alkyl, halogen, nitro, or C.sub.1 -C.sub.4 -alkoxy, or cyclo-C.sub.3 -C.sub.6 -alkyl fused with benzene, or wherein R.sub.2 and R.sub.3 are connected and together with the adjacent --CH-group and the adjacent N-atom form a saturated or partially saturated, monocyclic, five- or six-membered heterocyclic group or form a saturated or partially saturated, bicyclic heterocyclic group containing five or six atoms per ring, R.sub.4 represents hydrogen or C.sub.1 -C.sub.4 -alkyl, and R.sub.5 represents an acyl group, are useful as antihypertensive and cardioactive agents. The invention also relates to processes for preparing the compounds of the formula I and to pharmaceutical compositions.

    摘要翻译： 式（I）的化合物，其中R 1和R 6独立地表示羟基，C 1 -C 4 - 烷氧基，取代的C 1 -C 4 - 烷氧基，氨基或取代的氨基，R 2表示氢，C 1 -C 4烷基或C 2 C 4 - 烯基，R 3表示环-C 3 -C 6烷基，苯基，被C 1 -C 4 - 烷基，卤素，硝基或C 1 -C 4 - 烷氧基取代的苯基，或与苯稠合的环-C 3 -C 6烷基，或 其中R2和R3与相邻的-CH-基团和相邻的N-原子一起形成饱和或部分饱和的单环，五元或六元杂环基团或形成饱和或部分饱和的双环杂环基团，其含有 每个环五个或六个原子，R4代表氢或C1-C4-烷基，R5代表酰基，可用作抗高血压和心脏活性剂。 本发明还涉及制备式I化合物和药物组合物的方法。