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1. 发明申请

US20110105496A1 Methods For The Treatment Of Myosin Heavy Chain-Mediated Conditions Using 4,7-Dihydrothieno[2,3-B]Pyridine Compounds 审中-公开
标题翻译：使用4,7-二氢噻吩并[2,3-B]吡啶化合物治疗肌球蛋白重链介导的病症的方法
公开(公告)号：US20110105496A1
公开(公告)日：2011-05-05
申请号：US12158612
申请日：2006-12-19
申请人： Gabriel G. Gamber , Rishi K. Jain , Gary M. Ksander , Leslie W. McQuire , Lawrence S. Melvin , Moo J. Sung
发明人： Gabriel G. Gamber , Rishi K. Jain , Gary M. Ksander , Leslie W. McQuire , Lawrence S. Melvin , Moo J. Sung
IPC分类号： A61K31/4365 , A61K31/5377 , A61P9/00 , A61P9/10 , A61P3/04 , A61P3/00
CPC分类号： C07D495/04 , A61K31/4365
摘要： This invention relates generally to methods for the treatment of myosin heavy chain (MyHC)-mediated conditions, and in particular, cardiovascular conditions.
摘要翻译：本发明一般涉及治疗肌球蛋白重链（MyHC）介导的病症，特别是心血管疾病的方法。

2. 发明申请

US20090306373A1 4,7-DIHYDROTHIENO[2,3-B]PYRIDINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译： 4,7-二氢噻吩并[2,3-B]吡啶化合物和药物组合物
公开(公告)号：US20090306373A1
公开(公告)日：2009-12-10
申请号：US12158588
申请日：2006-12-19
申请人： Gabriel G. Gamber , Rishi K. Jain , Gary M. Ksander , Leslie W. McQuire , Lawrence S. Melvin , Moo J. Sung
发明人： Gabriel G. Gamber , Rishi K. Jain , Gary M. Ksander , Leslie W. McQuire , Lawrence S. Melvin , Moo J. Sung
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , A61K31/4365
摘要： This invention relates generally to compounds and pharmaceutical compositions for the treatment of myosin heavy chain (MyHC)-mediated conditions, and in particular, cardiovascular conditions.
摘要翻译：本发明一般涉及用于治疗肌球蛋白重链（MyHC）介导的病症，特别是心血管病症的化合物和药物组合物。

3. 发明授权

US06197798B1 Amino-benzocycloalkane derivatives 失效
标题翻译：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。

4. 发明授权

US4939261A N-substituted butyramide derivatives useful for treatment of conditions responsive to inhibition of enkephalinase 失效
标题翻译：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。

5. 发明授权

US5096925A N-substituted butyramide derivatives 失效
标题翻译： 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。

6. 发明授权

US4678800A Gamma-r-glutamoyl derivatives 失效
标题翻译： 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。

7. 发明授权

US4962105A Potentiation of antihypertensive effect of ace inhibitors 失效
标题翻译：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。

8. 发明授权

US5550119A Phosphono substituted tetrazole derivatives as ECE inhibitors 失效
标题翻译：膦酰取代的四唑衍生物作为ECE抑制剂
公开(公告)号：US5550119A
公开(公告)日：1996-08-27
申请号：US403353
申请日：1995-03-02
申请人： St ephane De Lombaert , Arco Y. Jeng , Gary M. Ksander
发明人： St ephane De Lombaert , Arco Y. Jeng , Gary M. Ksander
IPC分类号： C07F9/6524 , C07F9/280
CPC分类号： C07F9/6524
摘要： The present invention relates to the N-phosphonomethyl substituted compounds of formula ##STR1##
摘要翻译：本发明涉及式（I）的N-膦酰基甲基取代的化合物，

9. 发明授权

US5166212A Certain n-substituted butyramide derivatives 失效
标题翻译：某些正取代丁酰胺衍生物
公开(公告)号：US5166212A
公开(公告)日：1992-11-24
申请号：US691625
申请日：1991-04-25
申请人： Gary M. Ksander
发明人： Gary M. Ksander
IPC分类号： C07D209/20 , C07D213/32 , C07D213/56 , C07D213/75 , C07D333/24 , C07H11/04
CPC分类号： C07D213/75 , C07D209/20 , C07D213/32 , C07D213/56 , C07D333/24 , C07H11/04
摘要： Disclosed are compound 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, or each said grouping substituted by lower alkyl; R and R.sub.o independently represent lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl; A represents methylene; or A represents methylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by aryl-lower alkylthio-lower alkyl, by arylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by alkyloxy-lower alkyl, by aryloxy-lower alkyl, by amino-lower alkyl by acylamino-lower alkyl, by guanidino-lower amino-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; pharmaceutically acceptable ester and amide derivatives of any said compounds having a free carboxy group; pharmaceutically acceptable salts; methods for synthesis; pharmaceutical compositions thereof; and use thereof as endopentidase 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，或每个所述基团被低级烷基取代; R和R 4独立地表示低级烷基，（C 3 -C 7） - 环烷基 - 低级烷基或芳基 - 低级烷基; A代表亚甲基; 或A表示被低级烷基，低级烷硫基 - 低级烷基，芳基 - 低级烷硫基 - 低级烷基，芳硫基 - 低级烷基，羟基 - 低级烷基，酰氧基 - 低级烷基，低级烷氧基 - 低级烷基取代的亚甲基，由烷氧基 - 低级烷基，芳氧基 - 低级烷基，氨基 - 低级烷基，酰氨基 - 低级烷基，胍基 - 低级氨基 - 低级烷基，（C 3 -C 7） - 环烷基，（C 3 -C 7） - 环烷基 - 低级烷基，芳基或芳基 - 低级烷基; 任何所述具有游离羧基的化合物的药学上可接受的酯和酰胺衍生物; 药学上可接受的盐; 合成方法; 其药物组合物; 及其作为内切酶抑制剂的用途。

10. 发明授权

US5021430A Certain N-substituted butyramide derivatives 失效
标题翻译：某些N-取代丁酰胺衍生物
公开(公告)号：US5021430A
公开(公告)日：1991-06-04
申请号：US67587
申请日：1987-06-29
申请人： Gary M. Ksander
发明人： Gary M. Ksander
IPC分类号： A61K31/13 , A61K31/135 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/275 , A61P7/10 , A61P9/12 , A61P25/04 , C07D209/20 , C07D213/32 , C07D213/56 , C07D213/75 , C07D333/24 , C07H11/04
CPC分类号： C07D213/75 , C07D209/20 , C07D213/32 , C07D213/56 , C07D333/24 , C07H11/04
摘要： Disclosed are compound 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, or each said grouping substituted by lower alkyl; R and R.sub.o independently represent lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl; A represents methylene; or A represents methylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by aryl-lower alkylthio-lower alkyl, by arylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by aryl-lower alkyloxy-lower alkyl, by aryloxy-lower alkyl, by amino-lower alkyl, by acylamino-lower alkyl, by guanidino-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; pharmaceutically acceptable ester and amide derivatives of any said compounds having a free carboxy group; pharmaceutically acceptable salts; methods for synthesis; pharmaceutical compositions thereof; and use thereof as endopeptidase 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，或每个所述基团被低级烷基取代; R和R 4独立地表示低级烷基，（C 3 -C 7） - 环烷基 - 低级烷基或芳基 - 低级烷基; A代表亚甲基; 或A表示被低级烷基，低级烷硫基 - 低级烷基，芳基 - 低级烷硫基 - 低级烷基，芳硫基 - 低级烷基，羟基 - 低级烷基，酰氧基 - 低级烷基，低级烷氧基 - 低级烷基取代的亚甲基，由芳基 - 低级烷氧基 - 低级烷基，芳氧基 - 低级烷基，氨基 - 低级烷基，酰氨基 - 低级烷基，胍基 - 低级烷基，（C 3 -C 7） - 环烷基，（C 3 -C 7） - 环烷基低级烷基，芳基或芳基 - 低级烷基; 任何所述具有游离羧基的化合物的药学上可接受的酯和酰胺衍生物; 药学上可接受的盐; 合成方法; 其药物组合物; 并将其用作内肽酶抑制剂。

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