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    Triazolo-benzodiazepine-1-ethanamines as diuretics
    6.
    发明授权
    Triazolo-benzodiazepine-1-ethanamines as diuretics 失效
    三氮唑 - 苯并二氮杂-1-乙胺作为利尿剂

    公开(公告)号：US4689413A

    公开(公告)日：1987-08-25

    申请号：US697089

    申请日：1985-01-31

    Applicant: Jackson B. Hester, Jr. ,  James H. Ludens

    Inventor： Jackson B. Hester, Jr. ,  James H. Ludens

    IPC: C07D487/04

    CPC classification number: C07D487/04

    Abstract: Triazolo-benzodiazepine-1-ethanamines of the formulas ##STR1## where R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and Ring A are as defined in the specification, e.g., 8-chloro-N,N-dimethyl-.beta.,6-diphenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-1-ethanamine, and pharmacologically acceptable salts thereof, have been found to have substantial diuretic, natriuretic, but little, if any, kaliuretic activity, which can be used alone, or concomittently with other diuretic drugs such as furosemide or hydrochlorothiazide and/or with antihypertensive agents such as propranolol, captopril, minoxidil, prazosin, guanadrel sulfate, whose actions are supplemented by the action of a diuretic drug.

    Abstract translation: 其中R，R 1，R 2，R 3，R 4和环A如本说明书中所定义的三唑并 - 苯并二氮杂-1-乙胺，其中R 1，R 2，R 3，R 4和环A如本说明书中所定义，例如8-氯-N， 已经发现β，6-二苯基-4H- [1,2,4]三唑并[4,3-a] [1,4]苯并二氮杂-1-乙胺及其药理学上可接受的盐具有实质的利尿，利尿钠， 但可以单独使用或与其他利尿药物如呋塞米或氢氯噻嗪和/或与抗高血压药物如普萘洛尔，卡托普利，米诺地尔，哌唑嗪，硫酸胍酸酐联合使用的少量（如果有的话）活性，其作用由 利尿药物的作用。

    2,4-Dihydr o-2(omega-aminoalkyl)-1H-[1,2,4]triazolo[3,4-c]benzoxazin-1-one anti-alle rgy drug compounds, compositions and use
    7.
    发明授权
    2,4-Dihydr o-2(omega-aminoalkyl)-1H-[1,2,4]triazolo[3,4-c]benzoxazin-1-one anti-alle rgy drug compounds, compositions and use 失效
    2,4-二氢-2（ω-氨基烷基）-1H- [1,2,4]三唑并[3,4-c]苯并恶嗪-1-酮抗过敏药物化合物，组合物和用途

    公开(公告)号：US4547499A

    公开(公告)日：1985-10-15

    申请号：US609035

    申请日：1984-05-10

    Applicant: Jackson B. Hester, Jr.

    Inventor： Jackson B. Hester, Jr.

    IPC: C07D498/04 ,  A61K31/535

    CPC classification number: C07D498/04

    Abstract: 2,4-Dihydro-2-(omega-aminoalkyl)-1H-[1,2,4]triazolo[3,4-c][1,4]benzoxazin-1-ones of the formula ##STR1## where n and -NRR are as defined in the specification, e.g., 2-[4-[4-(2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)piperadinyl]butyl]-2,4-dihydro-1H-[1,2,4]triazolo[3,4-c][1,4]benzoxazin-1-one, are disclosed. They are useful for treating hypertension or allergy conditions in humans and valuable animals.

    Abstract translation: 2,4-二氢-2-（ω-氨基烷基）-1H- [1,2,4]三唑并[3,4-c] [1,4]苯并恶嗪-1-酮 ）其中n和-NRR如说明书中所定义，例如2- [4- [4-（2,3-二氢-2-氧代-1H-苯并咪唑-1-基）哌啶基]丁基] -2,4 - 二氢-1H- [1,2,4]三唑并[3,4-c] [1,4]苯并恶嗪-1-酮。 它们可用于治疗人类和有价值动物的高血压或过敏症状。

    1-Ethanamine-triazolo-benzodiazepines as diuretics
    8.
    发明授权
    1-Ethanamine-triazolo-benzodiazepines as diuretics 失效
    1-乙胺 - 三唑并苯并二氮杂卓作为利尿剂

    公开(公告)号：US4514407A

    公开(公告)日：1985-04-30

    申请号：US476181

    申请日：1983-03-17

    Applicant: Jackson B. Hester, Jr. ,  James H. Ludens

    Inventor： Jackson B. Hester, Jr. ,  James H. Ludens

    IPC: C07D487/04 ,  A61K31/55

    CPC classification number: C07D487/04

    Abstract: Triazolo-benzodiazepine-1-ethanamines of the formulas ##STR1## where R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and Ring A are as defined in the specification, e.g., 8-chloro-N,N-dimethyl-.beta.,6-diphenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-1-ethanamine, and pharmacologically acceptable salts thereof, have been found to have substantial diuretic, natriuretic, but little, if any, kaliuretic activity, which can be used alone, or concomittently with other diuretic drugs such as furosemide or hydrochlorothiazide and/or with antihypertensive agents such as propranolo, captopril, minoxidil, prazosin, guanadrel sulfate, whose actions are supplemented by the action of a diuretic drug.

    Abstract translation: 其中R，R 1，R 2，R 3，R 4和环A如本说明书中所定义的三唑并 - 苯并二氮杂-1-乙胺，其中R 1，R 2，R 3，R 4和环A如本说明书中所定义，例如8-氯-N， 已经发现β，6-二苯基-4H- [1,2,4]三唑并[4,3-a] [1,4]苯并二氮杂-1-乙胺及其药理学上可接受的盐具有实质的利尿，利尿钠， 但可以单独使用或与其他利尿药物例如呋塞米或氢氯噻嗪和/或与抗高血压药物如普萘洛尔，卡托普利，米诺地尔，哌唑嗪，硫酸胍酸酐联合使用的少量（如果有的话）活性，其作用由 利尿药物的作用。

    Antihypertensive use of triazolobenzodiazepines
    9.
    发明授权
    Antihypertensive use of triazolobenzodiazepines 失效
    抗高血压药物使用三唑并苯二氮卓类药物

    公开(公告)号：US4455307A

    公开(公告)日：1984-06-19

    申请号：US455780

    申请日：1983-01-05

    Applicant: Jackson B. Hester, Jr.

    Inventor： Jackson B. Hester, Jr.

    IPC: A61K31/55 ,  C07D498/04 ,  C07D487/04

    CPC classification number: A61K31/55 ,  C07D498/04

    Abstract: This specification concerns the use to treat hypertension in mammals of novel and known 4H-s-triazolo[4,3-a][1,4]benzodiazepines, known 4H-s-triazolo[4,3-a][1,3,4]benzotriazepines and 2,4-dihydro-2-alkyl-1H-s-triazolo[4,3-a][1,4]benzodiazepin-1-ones, and novel 2,4-dihydro-2-alkyl-1H-s-triazolo[4,3-a][1,4]benzodiazepin-1-thiones.

    Abstract translation: 本说明书涉及用于治疗哺乳动物中新兴且已知的4H-三唑并[4,3-a] [1,4]苯并二氮杂卓的已知的4H-三唑并[4,3-a] [1,3 ，4]苯并三氮杂和2,4-二氢-2-烷基-1H- s-三唑并[4,3-a] [1,4]苯并二吖庚因-1-酮，新的2,4-二氢-2-烷基 - 1H-三唑并[4,3-a] [1,4]苯并二氮杂-1-thiones。

    Amino-4H-s-triazolo[4,3-a][1,4]benzodiazepines
    10.
    发明授权
    Amino-4H-s-triazolo[4,3-a][1,4]benzodiazepines 失效
    氨基-4H-三唑并[4,3-a] [1,4]苯并二氮杂卓

    公开(公告)号：US4296239A

    公开(公告)日：1981-10-20

    申请号：US61976

    申请日：1979-07-30

    Applicant: Jackson B. Hester, Jr.

    Inventor： Jackson B. Hester, Jr.

    IPC: C07D249/08 ,  C07D487/04 ,  C07D211/68

    CPC classification number: C07D487/04 ,  C07D249/08

    Abstract: 6-Amino-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.3 -alkyl, R.sub.1 is hydrogen or halogen, and the two R.sub.2 groups are taken together with the nitrogen to which they are bonded to complete a nitrogen ring moiety selected from the group consisting of pyrrolidino, piperidino, morpholino and 3,6-dihydro-1(2H)-pyridyl, and the pharmacologically acceptable salts thereof, are central nervous system depressant drugs which are useful in effective dosages in domestic and zoo animals for their calming and tranquilizing uses during shipment and to reduce aggressive behavior. In man these compounds are potentially useful for controlling anxiety and schizophrenia and for their sedative, muscle relaxant and anti-convulsant activity.

    Abstract translation: 其中R为氢或C 1至C 3 - 烷基，R 1为氢或卤素的6-氨基-4H-哒嗪并[4,3-a] [1,4]苯并二氮杂，其中R 2为氢或卤素， 与它们所键合的氮原子一起形成选自吡咯烷子基，哌啶子基，吗啉代和3,6-二氢-1（2H） - 吡啶基的氮环部分，其药理学上可接受的盐是 中枢神经系统抑制药物，可用于家畜和动物园动物的有效剂量，用于运送期间的镇静和镇静用途，并减少侵略行为。 在这些化合物中，这些化合物可用于控制焦虑和精神分裂症以及其镇静，肌肉松弛和抗惊厥活性。

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