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    1,2-diamino compounds, processes for their preparation and pharmaceutical compositions containing them
    2.
    发明授权
    1,2-diamino compounds, processes for their preparation and pharmaceutical compositions containing them 失效

    公开(公告)号：US4927834A

    公开(公告)日：1990-05-22

    申请号：US230946

    申请日：1988-08-11

    Applicant: Herbert Leinert ,  Christos Tsaklakidis ,  Gisbert Sponer

    Inventor： Herbert Leinert ,  Christos Tsaklakidis ,  Gisbert Sponer

    IPC: A61K31/215 ,  A61K31/135 ,  A61K31/19 ,  A61K31/33 ,  A61K31/34 ,  A61K31/341 ,  A61K31/357 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61P9/00 ,  A61P9/08 ,  C07D213/38 ,  C07D213/74 ,  C07D295/12 ,  C07D295/13 ,  C07D307/52 ,  C07D317/58 ,  C07D317/66 ,  C07D333/20 ,  C07D521/00

    CPC classification number: C07D213/74 ,  C07D213/38 ,  C07D295/13 ,  C07D307/52 ,  C07D317/58 ,  C07D317/66 ,  C07D333/20

    Abstract: The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1 is a straight-chained or branched C.sub.1 -C.sub.12 -alkyl radical which can be substituted by phenyl, naphthyl or a C.sub.3 -C.sub.7 -cycloalkyl radical; a straight-chained or branched C.sub.2 -C.sub.6 -alkenyl radical which can be substituted by a C.sub.3 -C.sub.7 -cycloalkyl radical or a phenyl or naphthyl radical; a C.sub.3 -C.sub.7 -cycloalkyl radical or a mono- or bicyclic aromatic radical which is unsubstituted or substituted one or more times, the substituents being C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, carboxyl or carbethoxy, R.sub.2 and R.sub.3, which can be the same or different, are straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.6 -alkyl radicals which are optionally substituted by hydroxyl, C.sub.1 -C.sub.3 -alkoxy or C.sub.1 -C.sub.3 -alkoxy-C.sub.1 -C.sub.3 -alkoxy or, together with the nitrogen atom to which they are attached, form a saturated or unsaturated ring which can contain further heteroatoms and is optionally substituted by a lower alkyl or lower alkoxy radical or by an oxygen atom, A is a valency bond or a straight-chained or branched alkylene radical containing up to 6 and preferably up to 3 carbon atoms, R.sub.4 is a mono- or bicyclic aromatic or heteroaromatic radical which is unsubstituted or substituted one or more times, whereby the substituents are alkyl, C.sub.2 -C.sub.6 -alkenyl, alkoxy, C.sub.2 -C.sub.6 -alkenyloxy, hydroxyalkyl, C.sub.2 -C.sub.6 -alkylenedioxy, hydroxyalkoxy, alkoxyethoxy, alkylamino, dialkylamino, alkoxycarbonylethyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylsulphonyloxy, carboxyl, alkoxycarbonyl, aminocarbonyl, mono- or dialkylaminocarbonyl, haloalkyl or cyano, as well as halogen atoms, such as chlorine, bromine or fluorine, X is a valency bond or a straight-chained or branched, saturated or unsaturated hydrocarbon radical containing up to 6 carbon atoms, Y is a valency bond or an oxygen atom and R.sub.5 is a C.sub.3 -C.sub.7 -cycloalkyl radical or a mono- or bicyclic aromatic or heteroaromatic radical which is unsubstituted or substituted one or more times, the substituents being alkyl, alkoxy, C.sub.2 -C.sub.6 -alkenyloxy, aralkoxy, hydroxyl, hydroxyalkoxy, alkoxyalkoxy, alkoxycarbonylalkoxy, C.sub.1 -C.sub.2 -alkenylenedioxy, dialkylamino, alkylthio, alkylsulphinyl, alkyl-sulphonyl, alkylsulphonyloxy, hydroxyalkyl, carboxyl, alkoxycarbonyl, aminocarbonyl, mono- or dialkylaminocarbonyl or cyano, as well as halogen atoms, such as chlorine, bromine or fluorine, with the proviso that Y cannot be an oxygen atom when X is a valency bond and that when R.sub.1 is a saturated hydrocarbon radical, X must be a radical with at least 2 carbon atoms; as well as the pharmacologically acceptable salts thereof and the optical isomers thereof.The present invention also provides processes for the preparation of these 1,2-diamino compounds and pharmaceutical compositions containing them.

    Method of treatment for decreasing mortality resulting from congestive heart failure
    3.
    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

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

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

    IPC: 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 classification number: A61K31/403 ,  A61K31/7048

    Abstract: 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.

    Abstract translation: 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
    4.
    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

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

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

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

    CPC classification number: A61K31/403 ,  A61K31/7048 ,  A61K2300/00

    Abstract: 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.

    Abstract translation: 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。

    Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions
    8.
    发明授权
    Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions 失效
    （4） - 氧丙醇胺化合物和治疗组合物

    公开(公告)号：US4503067A

    公开(公告)日：1985-03-05

    申请号：US479921

    申请日：1983-04-04

    Applicant: Fritz Wiedemann ,  Wolfgang Kampe ,  Max Thiel ,  Gisbert Sponer ,  Egon Roesch ,  Karl Dietmann

    Inventor： Fritz Wiedemann ,  Wolfgang Kampe ,  Max Thiel ,  Gisbert Sponer ,  Egon Roesch ,  Karl Dietmann

    IPC: A61K31/40 ,  A61K31/403 ,  A61P9/08 ,  A61P25/02 ,  C07D209/88 ,  C07D317/64 ,  C07D401/12 ,  C07D405/12 ,  C07D209/82

    CPC classification number: C07D209/88 ,  C07D317/64

    Abstract: Carbazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkanoyl or aroyl;R.sub.2 is hydrogen, lower alkyl or arylalkyl;R.sub.3 is hydrogen or lower alkyl;R.sub.4 is hydrogen or lower alkyl, 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 mono- or bicyclic aryl or pyridyl;R.sub.5 and R.sub.6 are individually selected from hydrogen, halogen, hydroxyl, lower alkyl, aminocarbonyl, lower alkoxy, aralkyloxy, lower alkylthio, lower alkylsulphinyl or lower alkylsulphonyl;R.sub.5 and R.sub.6 together can represent methylenedioxy;and the salts thereof with physiologically acceptable acids are outstandingly effective in the treatment and prophylaxis of circulatory and cardiac diseases, e.g., hypertension and angina pectoris.

    Abstract translation: 式（I）的羧基 - （4） - 氧丙醇胺化合物，其中R 1是氢，低级烷酰基或芳酰基; R2是氢，低级烷基或芳基烷基; R3是氢或低级烷基; R4是氢或低级烷基，或者当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是单环或双环芳基或吡啶基; R5和R6分别选自氢，卤素，羟基，低级烷基，氨基羰基，低级烷氧基，芳烷氧基，低级烷硫基，低级烷基亚磺酰基或低级烷基磺酰基; R5和R6一起可以代表亚甲二氧基; 并且其与生理上可接受的酸的盐在治疗和预防循环和心脏疾病例如高血压和心绞痛方面是显着的。

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