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    Method of treatment for decreasing mortality resulting from congestive heart failure
    1.
    发明授权
    Method of treatment for decreasing mortality resulting from congestive heart failure 失效
    减少充血性心力衰竭引起的死亡率的治疗方法

    公开(公告)号：US5760069A

    公开(公告)日：1998-06-02

    申请号：US483635

    申请日：1995-06-07

    申请人： Mary Ann Lukas-Laskey ,  Robert Ruffolo, Jr. ,  Neil Howard Shusterman ,  Gisbert Sponer ,  Klaus Strein

    发明人： Mary Ann Lukas-Laskey ,  Robert Ruffolo, Jr. ,  Neil Howard Shusterman ,  Gisbert Sponer ,  Klaus Strein

    IPC分类号： C07D207/16 ,  A61K31/196 ,  A61K31/34 ,  A61K31/40 ,  A61K31/401 ,  A61K31/403 ,  A61K31/404 ,  A61K31/44 ,  A61K31/54 ,  A61K31/549 ,  A61K31/662 ,  A61K31/70 ,  A61K31/702 ,  A61K38/00 ,  A61K45/00 ,  A61K45/06 ,  A61P9/00 ,  A61P9/04 ,  C07D209/88 ,  A61K31/585

    CPC分类号： A61K31/403 ,  A61K31/7048

    摘要： A method of treatment using a compound of Formula I: ##STR1## wherein: R.sub.1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl; R.sub.2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl; R.sub.3 is hydrogen or lower alkyl of up to 6 carbon atoms; R.sub.4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--; X is a valency bond, --CH.sub.2, oxygen or sulfur; Ar is selected from phenyl, naphthyl, indanyl and tetrahydronaphthyl; R.sub.5 and R.sub.6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a --CONH.sub.2 -- group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkysulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; or R.sub.5 and R.sub.6 together represent methylenedioxy; or a pharmaceutically acceptable salt thereof, alone or in conjunction with one or more other therapeutic agents, said agents being selected from the group consisting of ACE inhibitors, diuretics, and digoxin for decreasing mortality resulting from congestive heart failure (CHF) in mammals, particularly humans.

    摘要翻译： 使用式I化合物的方法：其中：R1是氢，至多6个碳原子的低级烷酰基或选自苯甲酰基和萘甲酰基的芳酰基; R2是氢，至多6个碳原子的低级烷基或选自苄基，苯基乙基和苯基丙基的芳基烷基; R3是氢或至多6个碳原子的低级烷基; R4是氢或至多6个碳原子的低级烷基，或当X是氧时，R4与R5一起可以代表-CH2-O-; X是价键，-CH 2，氧或硫; Ar选自苯基，萘基，茚满基和四氢萘基; R 5和R 6分别选自氢，氟，氯，溴，羟基，至多6个碳原子的低级烷基，-CONH 2 - 基，至多6个碳原子的低级烷氧基，苄氧基，至多6个碳的低级烷硫基 原子，低至6个碳原子的低级烷基亚磺酰基和至多6个碳原子的低级烷基磺酰基; 或R5和R6一起表示亚甲二氧基; 特别是用于降低哺乳动物充血性心力衰竭（CHF）引起的死亡率的ACE抑制剂，利尿剂和地高辛，所述药物单独或与一种或多种其它治疗剂联合使用，或其药学上可接受的盐， 人类。

    Method of treatment for decreasing mortality resulting from congestive heart failure
    3.
    再颁专利
    Method of treatment for decreasing mortality resulting from congestive heart failure 有权
    减少充血性心力衰竭引起的死亡率的治疗方法

    公开(公告)号：USRE40000E1

    公开(公告)日：2008-01-08

    申请号：US10721020

    申请日：2003-11-25

    申请人： Mary Ann Lukas-Laskey ,  Robert Ruffolo, Jr. ,  Neil Howard Shusterman ,  Gisbert Sponer ,  Klaus Strein

    发明人： Mary Ann Lukas-Laskey ,  Robert Ruffolo, Jr. ,  Neil Howard Shusterman ,  Gisbert Sponer ,  Klaus Strein

    IPC分类号： A61K31/40 ,  A61K31/585 ,  A61K31/54 ,  A61K31/41 ,  A61K31/34

    CPC分类号： A61K31/403 ,  A61K31/7048 ,  A61K2300/00

    摘要： A method of treatment using a compound of Formula I: wherein: R1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl; R2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl; R3 is hydrogen or lower alkyl of up to 6 carbon atoms; R4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R4 together with R5 can represent —CH2—O—; X is a valency bond, —CH2, oxygen or sulfur; Ar is selected from phenyl, naphthyl, indanyl and tetrahydronapthyl; R5 and R6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a —CONH2— group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkysulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; or R5 and R6 together represent methylenedioxy; or a pharmaceutically acceptable salt thereof, alone or in conjunction with one or more other therapeutic agents, said agents being selected from the group consisting of ACE inhibitors, diuretics, and digoxin for decreasing mortality resulting from congestive heart failure (CHF) in mammals, particularly humans.

    摘要翻译： 使用式I化合物的方法：其中：R 1是氢，至多6个碳原子的低级烷酰基或选自苯甲酰基和萘甲酰基的芳酰基; R 2是氢，至多6个碳原子的低级烷基或选自苄基，苯基乙基和苯基丙基的芳基烷基; R 3是氢或至多6个碳原子的低级烷基; R 4是氢或至多6个碳原子的低级烷基，或者当X是氧时，R 4与R 5一起可代表 - CH 2 -O-; X是价键，-CH 2，氧或硫; Ar选自苯基，萘基，茚满基和四氢萘基; R 5和R 6分别选自氢，氟，氯，溴，羟基，至多6个碳原子的低级烷基，-CONH 2， 最多6个碳原子的低级烷氧基，至多6个碳原子的低级烷硫基，至多6个碳原子的低级烷基亚磺酰基和至多6个碳原子的低级烷基磺酰基; 或R 5和R 6一起代表亚甲二氧基; 特别是用于降低哺乳动物充血性心力衰竭（CHF）引起的死亡率的ACE抑制剂，利尿剂和地高辛，所述药物单独或与一种或多种其它治疗剂联合使用，或其药学上可接受的盐， 人类。

    3-Cyano-indoles as cardioselective agents
    9.
    发明授权
    3-Cyano-indoles as cardioselective agents 失效
    3-氰基 - 吲哚作为心脏选择剂

    公开(公告)号：US4468520A

    公开(公告)日：1984-08-28

    申请号：US288075

    申请日：1981-07-29

    申请人： Helmut Michel ,  Wolfgang Kampe ,  Roland Ofenloch ,  Karl Dietmann ,  Gisbert Sponer

    发明人： Helmut Michel ,  Wolfgang Kampe ,  Roland Ofenloch ,  Karl Dietmann ,  Gisbert Sponer

    IPC分类号： C07D209/12 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/00 ,  C07D209/08 ,  C07D209/42 ,  C07D209/43 ,  C07D209/04

    CPC分类号： C07D209/08

    摘要： The present invention provides aminopropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkanoyl or an aroyl radical, R.sub.2 is a lower alkyl radical or a radical of the general formula: ##STR2## wherein X is a valency bond, a methylene group or an oxygen or sulphur atom, Ar is a monocyclic, carbo- or heterocyclic aryl radical, R.sub.6 and R.sub.7, which can be the same or different, are hydrogen atoms or lower alkyl radicals, R.sub.8 and R.sub.9, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, alkenyl radicals, alkynyl radicals, alkyl radicals, lower alkoxy radicals, aralkoxy radicals, alkenyloxy radicals, alkynyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or acylamino radicals; or R.sub.2 is a 1,4-benzodioxan-2-ylmethyl radical, R'.sub.2 is a hydrogen atom or a benzyl radical, R.sub.3 is a carboxyl group or a lower alkoxycarbonyl, aminocarbonyl, cyano, oximinomethyl, formyl, hydroxymethyl or lower alkoxycarbimidoyl radical, R.sub.4 is a hydrogen atom or a lower alkyl radical or a --CH.sub.2 --O--R.sub.1 radical, R.sub.1 having the same meaning as above, and R.sub.5 is a hydrogen atom or a lower alkyl radical; the optionally-active forms and racemates thereof and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention is concerned with the use of these compounds for the prophylaxis and treatment of heart and circulatory diseases.

    摘要翻译： 本发明提供以下通式的氨基丙醇衍生物：其中R1是氢原子或低级烷酰基或芳酰基，R2是低级烷基或通式如下的基团：其中 X是价键，亚甲基或氧或硫原子，Ar是单环，碳或杂环芳基，R6和R7可以相同或不同，是氢原子或低级烷基，R8和 R9可相同或不同，为氢或卤原子，羟基，低级烷酰基，烯基，炔基，烷基，低级烷氧基，芳烷氧基，烯氧基，炔氧基，低级烷硫基，氨基羰基 自由基，氨基磺酰基或酰氨基; 或R 2为1,4-苯并二恶烷-2-基甲基，R'2为氢原子或苄基，R 3为羧基或低级烷氧基羰基，氨基羰基，氰基，肟基甲基，甲酰基，羟甲基或低级烷氧基甲脒基 R4是氢原子或低级烷基或-CH2-O-R1基，R1具有与上述相同的含义，R 5是氢原子或低级烷基; 其任选活性形式和外消旋物及其药理学上可接受的盐。 本发明还提供了制备这些化合物的方法和含有它们的药物组合物。 此外，本发明涉及这些化合物用于预防和治疗心脏和循环系统疾病的用途。

    Quinoxalinyloxy-amino-propanol compounds with blood pressure lowering and .beta.-blocking properties, their use and pharmaceutical compositions containing them
    10.
    发明授权
    Quinoxalinyloxy-amino-propanol compounds with blood pressure lowering and .beta.-blocking properties, their use and pharmaceutical compositions containing them 失效
    具有降血压和β-阻断性能的喹喔啉氧基 - 氨基 - 丙醇化合物，它们的用途和含有它们的药物组合物

    公开(公告)号：US4438116A

    公开(公告)日：1984-03-20

    申请号：US302894

    申请日：1981-09-16

    申请人： Carl H. Ross ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Gisbert Sponer ,  Egon Roesch

    发明人： Carl H. Ross ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Gisbert Sponer ,  Egon Roesch

    IPC分类号： A61K31/505 ,  A61P9/00 ,  C07D241/38 ,  C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  A61K31/495 ,  C07D241/42

    CPC分类号： C07D241/38 ,  C07D241/44 ,  Y10S514/929

    摘要： An aminopropanol compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from hydrogen and lower alkyl; orR.sub.1 and R.sub.2 together represent an alkylene radical;R.sub.3 is hydrogen or acyl;A is one of the following structures ##STR2## wherein R.sub.4 is hydrogen or lower alkyl optionally substituted by hydroxyl halogen and lower alkylthio; andR.sub.5 and R.sub.6 are individually selected from lower alkyl;B is alkylamino which optionally carries a phenyl and a phenoxy radical optionally substituted by at at least one of halogen, hydroxyl or lower alkyl, lower acyl, lower alkylthio, acylamino, aminocarbonyl, lower alkoxy, lower alkenyloxy, phenoxy, lower alkenyl, lower alkylsulphonyl, lower alkylsulphinyl or haloalkyl; orB is an aryl- or heteroaryloxymethylpiperidine radical optionally substituted by at least one of halogen hydroxyl or lower alkyl, hydroxyl alkyl or carboxamido alkyl, or by lower alkoxy, lower acyl, amino, carboxamido, lower alkylcarbonylamido or lower alkylsulphonylamino;and the pharmacologically acceptable salts thereof, are outstandingly effective beta blockers and blood-pressure depressants.

    摘要翻译： 式IMAMA的氨基丙醇化合物，其中R 1和R 2分别选自氢和低级烷基; 或者R 1和R 2一起表示亚烷基; R3是氢或酰基; A是下列结构之一，其中R4是氢或任选被羟基卤素和低级烷硫基取代的低级烷基; 并且R 5和R 6分别选自低级烷基; B是烷基氨基，其任选地带有苯基和苯氧基，其任选被至少一个卤素，羟基或低级烷基，低级酰基，低级烷硫基，酰氨基，氨基羰基，低级烷氧基，低级烯氧基，苯氧基，低级烯基，低级烷基磺酰基 ，低级烷基亚磺酰基或卤代烷基; 或B是任选被卤素羟基或低级烷基，羟基烷基或甲酰胺基烷基中的至少一个取代的芳基或杂芳氧基甲基哌啶基，或由低级烷氧基，低级酰基，氨基，甲酰氨基，低级烷基羰基酰氨基或低级烷基磺酰基氨基取代; 和其药理学上可接受的盐是显着有效的β受体阻滞剂和降压药。