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    5-Sulphonyloxy pyrazole derivatives
    5.
    发明授权
    5-Sulphonyloxy pyrazole derivatives 失效
    5-磺酰氧基吡唑衍生物

    公开(公告)号：US4122281A

    公开(公告)日：1978-10-24

    申请号：US757872

    申请日：1977-01-10

    申请人： Eike Moller ,  Karl Meng ,  Egbert Wehinger ,  Harald Horstmann

    发明人： Eike Moller ,  Karl Meng ,  Egbert Wehinger ,  Harald Horstmann

    IPC分类号： C07D231/20

    CPC分类号： C07D231/20 ,  Y10S514/869

    摘要： Pyrazole derivatives of the formula: ##STR1## and pharmaceutically acceptable nontoxic salts thereof wherein R is hydrogen, trifluoromethyl or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is alkyl;R.sup.3 is a substituted aryl moiety orR.sup.3 is naphthyl or pyridyl; andR.sup.4 is R.sup.5 CO wherein R.sup.5 is alkyl unsubstituted or substituted by 1, 2 or 3 halogen moieties, by alkoxy, or by mono- or dialkylamino; lower alkoxy; dialkylamino; thiophene; phenyl unsubstituted or substituted by 1 or 2 alkyl, trifluoromethyl, alkoxy, nitro or halogen moieties; or a 5- to 7-membered heterocycle unsubstituted or substituted by 1 or 2 halogen, alkyl or nitro moieties; orR.sup.4 is Z-SO.sub.2 wherein Z is alkyl, phenyl or phenyl substituted by 1 or 2 alkyl, halogen, nitro, trifluoromethyl or trifluoromethylsulphonyl moieties; or dichloroquinoxalinyl. The pyrazole derivatives and their salts are useful as diuretics, saluretics and antihypertensives.

    摘要翻译： 具有下式的吡唑衍生物：其中R是氢，三氟甲基或烷基;和其药学上可接受的无毒盐，其中R是氢，三氟甲基或烷基; R1是氢或烷基; R2是烷基; R3是取代的芳基部分或R3是萘基或吡啶基; 并且R 4是R 5 CO，其中R 5是未被取代的或被1,2或3个卤素部分取代的烷基，被烷氧基取代，或被一或二烷基氨基取代; 低级烷氧基 二烷基氨基; 噻吩 未取代或被1或2个烷基，三氟甲基，烷氧基，硝基或卤素部分取代的苯基; 或未被取代或被1或2个卤素，烷基或硝基部分取代的5至7元杂环; 或R4是Z-SO2，其中Z是烷基，苯基或被1或2个烷基，卤素，硝基，三氟甲基或三氟甲基磺酰基部分取代的苯基; 或二氯喹喔啉。 吡唑衍生物及其盐可用作利尿剂，saluretics和抗高血压药。

    Pyrazol-5-ones
    6.
    发明授权
    Pyrazol-5-ones 失效

    公开(公告)号：US4000294A

    公开(公告)日：1976-12-28

    申请号：US632165

    申请日：1975-11-14

    申请人： Eike Moller ,  Karl Meng ,  Egbert Wehinger ,  Harald Horstmann

    发明人： Eike Moller ,  Karl Meng ,  Egbert Wehinger ,  Harald Horstmann

    IPC分类号： C07D231/52 ,  A61K31/415

    CPC分类号： C07D231/52 ,  Y10S514/869

    摘要： 1-Substituted pyrazole-5-ones of the formula ##STR1## and pharmaceutically acceptable, nontoxic salts thereof, wherein R is hydrogen or amino;R.sup.1 is hydrogen, alkyl, alkenyl, unsubstituted or substituted aryl or unsubstituted or substituted aralky;X isA. ethylene, ethylene wherein 1 hydrogen atom on one of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, ethylene wherein 1 hydrogen atom on each of the two carbon atoms is substituted by alkyl of 1 to 4 carbon atoms or said ethylene which is linked to R.sup.2 via an oxygen or sulphur atom;B. propenyl, propenyl wherein 1 hydrogen atom on one, two or three of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, said propenyl being linked to the N.sup.1 atom of the pyrazol ring via its methylene moiety; orC. methylene;Provided that when X is methylene, R.sup.1 is not hydrogen if R is amino;R.sup.2 is aryl unsubstituted or substituted by:A. 1 or 2 of the same or different substituents selected from the group consisting of halogen, trifluoromethyl, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms, and lower alkoxy;B. cycloalkyl of 5, 6 or 7 carbon atoms or cycloalkenyl of 5, 6 or 7 carbon atoms;C. alkylamino, dialkylamino, cyano, trifluoromethoxy, nitro, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, or said carbamoyl wherein the nitrogen atom is a member of a heterocyclic ring, sulphamyl, alkylsulphamyl, dialkylsulphamyl, or said sulphamyl wherein the nitrogen is a member of a heterocyclic ring, or --SO.sub.n alkyl wherein n is 0, 1 or 2;D. alkylamino, dialkylamino, cyano, trifluoromethoxy, nitro, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, or said carbamoyl wherein the nitrogen atom is a member of a heterocyclic ring, sulphamyl, alkylsulphamyl, dialkylsulphamyl or said sulphamyl wherein the nitrogen is a member of a heterocyclic ring, or --SO.sub.n -- alkyl wherein n is 0, 1 or 2, and 1 or 2 of the same or different substituents selected from the group consisting of alkyl, alkenyl, alkoxy, halogen, and trifluoromethyl; orE. a fused, saturated or unsaturated 5-, 6-, or 7-membered ring or said ring containing 1 or 2 oxygen or sulphur atoms;are useful for their diuretic, saluretic, antihypertensive and antithrombotic effects.

    1,4-Dihydropyridine esters
    7.
    发明授权
    1,4-Dihydropyridine esters 失效
    1,4-二氢吡啶酯

    公开(公告)号：US3971796A

    公开(公告)日：1976-07-27

    申请号：US609153

    申请日：1975-08-29

    申请人： Friedrich Bossert ,  Egbert Wehinger ,  Wulf Vater ,  Kurt Stoepel

    发明人： Friedrich Bossert ,  Egbert Wehinger ,  Wulf Vater ,  Kurt Stoepel

    IPC分类号： C07D401/04 ,  C07D213/55

    CPC分类号： C07D401/04 ,  Y10S514/929

    摘要： A new class of 1,4-dihydropyridines which are characterized by the presence of ester substitutes at positions 3 and 5 of the nucleus and by the presence of an alkoxyalkyl at position 2. The products exhibit coronary activity and have particular application as coronary dilators, antifibrillators, anti-hypertensives, and as muscular and vascular spasmolytics.

    摘要翻译： 一类新的1,4-二氢吡啶，其特征在于在核的位置3和5处存在酯取代基，并且在位置2处存在烷氧基烷基。产物表现出冠状动力，并且具有特定用途作为冠状动脉扩张器， 抗纤颤器，抗高血压药，以及肌肉和血管解压药。

    Pyrazol-5-ones
    8.
    发明授权
    Pyrazol-5-ones 失效
    吡唑-5-酮

    公开(公告)号：US3952008A

    公开(公告)日：1976-04-20

    申请号：US461285

    申请日：1974-04-15

    申请人： Eike Moller ,  Karl Meng ,  Egbert Wehinger ,  Harald Horstmann

    发明人： Eike Moller ,  Karl Meng ,  Egbert Wehinger ,  Harald Horstmann

    IPC分类号： A61K31/415 ,  A61P7/02 ,  A61P7/10 ,  A61P9/12 ,  C07D231/20 ,  C07D231/24 ,  C07D231/52 ,  C07D231/38 ,  C07D401/06

    CPC分类号： C07D231/52 ,  C07D231/20 ,  C07D231/24 ,  Y10S514/822 ,  Y10S514/869

    摘要： 1-Substituted pyrazole-5-ones of the formula ##SPC1##And pharmaceutically acceptable, nontoxic salts thereof,WhereinR is hydrogen or amino;R.sup.1 is hydrogen, alkyl, alkenyl, unsubstituted or substituted aryl or unsubstituted or substituted aralky;X isA. ethylene, ethylene wherein 1 hydrogen atom on one of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, ethylene wherein 1 hydrogen atom on each of the two carbon atoms is substituted by alkyl of 1 to 4 carbon atoms or said ethylene which is linked to R.sup.2 via an oxygen or sulphur atom;B. propenyl, propenyl wherein 1 hydrogen atom on one, two or three of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, said propenyl being linked to the N.sup.1 atom of the pyrazol ring via its methylene moiety; orC. methylene; provided that when X is methylene, R.sup.1 is not hydrogen if R is amino;R.sup.2 is aryl unsubstituted or substituted by:A. 1 or 2 of the same or different substituents selected from the group consisting of halogen, trifluoromethyl, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms and lower alkoxy;B. cycloalkyl of 5, 6 or 7 carbon atoms or cycloalkenyl of 5, 6 or 7 carbon atoms;C. alkylamino, dialkylamino, cyano, trifluoromethoxy, nitro, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, or said carbamoyl wherein the nitrogen atom is a member of a heterocyclic ring, sulphamyl, alkylsulphamyl, dialkylsulphamyl, or said sulphamyl wherein the nitrogen is a member of a heterocyclic ring, or --SO.sub.n alkyl wherein n is 0, 1 or 2;D. alkylamino, dialkylamino, cyano, trifluoromethoxy, nitro, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, or said carbamoyl wherein the nitrogen atom is a member of a heterocyclic ring, sulphamyl, alkylsulphamyl, dialkylsulphamyl or said sulphamyl wherein the nitrogen is a member of a heterocyclic ring, or --SO.sub.n alkyl wherein n is 0, 1 or 2, and 1 or 2 of the same or different substituents selected from the group consisting of alkyl, alkenyl, alkoxy, halogen, and trifluoromethyl; orE. a fused, saturated or unsaturated 5-, 6-, or 7-membered ring or said ring containing 1 or 2 oxygen or sulphur atoms;Are useful for their diuretic, saluretic, antihypertensive and antithrombotic effects.

    摘要翻译： 1-取代的吡唑-5-酮，其具有式和药学上可接受的非对映体，其中R是氢或氨基; R1是氢，烷基，烯基，未取代或取代的芳基或未取代或取代的芳基; X是A.乙烯，其中一个碳原子上的1个氢原子的1个氢原子是由1至4个碳原子的烷基取代的，在两个碳原子上的1个氢原子被1至4个碳原子的烷基取代的乙烯 或通过氧或硫原子与R2连接的乙烯; B.丙烯，丙烯，其中1个氢原子在一个碳原子上，两个或三个碳原子被1至4个碳原子的烷基取代，通过其亚甲基部分连接到吡唑环的N1原子上。 或C. METHYLENE; 当X是亚甲基时，如果R是氨基，则R1不是氢; R2是未取代的或被下列基团取代的芳基：

    Certain nitratoalkyl ester dihydropyridines having antihypertensive properties
    9.
    发明授权
    Certain nitratoalkyl ester dihydropyridines having antihypertensive properties 失效
    某些具有抗高血压特性的硝基烷基酯二氢吡啶类

    公开(公告)号：US4565824A

    公开(公告)日：1986-01-21

    申请号：US550321

    申请日：1983-11-09

    申请人： Egbert Wehinger ,  Horst Meyer ,  Stanislav Kazda ,  Andreas Knorr

    发明人： Egbert Wehinger ,  Horst Meyer ,  Stanislav Kazda ,  Andreas Knorr

    IPC分类号： A61K31/455 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D211/90

    CPC分类号： C07D211/90

    摘要： Dihydropyridines of the formula ##STR1## in which R is aryl or heterocyclic,R.sup.1, R.sup.2 and R.sup.3 each is hydrogen or various organic radicals,Y is oxygen, or optionally substituted --NH--,Z is --O--NO.sub.2 or --O--NO,X is --COR.sup.4, --COOR.sup.5 or --CO--Y--A--Z,R.sup.4 is alkyl, phenyl, benzyl or an amino radical, andR.sup.5 is an organic radical,or pharmaceutically acceptable acid addition salts thereof, exhibit circulation active properties, e.g. they can be used as antihypertensives, as peripheral and cerebral vasodilators and as coronary therapeutics.

    摘要翻译： 式中，R为芳基或杂环，R 1，R 2和R 3各自为氢或各种有机基团，Y为氧或任选取代的-NH-，Z为-O-NO 2或-O-NO X为-COR 4，-COOR 5或-CO-YAZ，R 4为烷基，苯基，苄基或氨基，R 5为有机基团或其药学上可接受的酸加成盐，具有循环活性，例如 它们可以作为抗高血压药物，作为外周血脑血管扩张剂和冠脉治疗药。