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47 条记录 (耗时 0.022 秒)

    Pyrazol-5-ones
    2.
    再颁专利
    Pyrazol-5-ones 失效
    吡唑-5-酮

    公开(公告)号：USRE30420E

    公开(公告)日：1980-10-21

    申请号：US765666

    申请日：1977-02-04

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

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

    IPC分类号： C07D231/20 ,  C07D231/24 ,  C07D231/52

    CPC分类号： C07D231/24 ,  C07D231/20 ,  C07D231/52

    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.

    Pyrazole derivatives
    3.
    发明授权
    Pyrazole derivatives 失效
    吡唑衍生物

    公开(公告)号：US4002641A

    公开(公告)日：1977-01-11

    申请号：US532311

    申请日：1974-12-13

    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 ,  A61K31/42 ,  A61K31/495 ,  A61P3/00 ,  A61P7/02 ,  A61P7/10 ,  A61P9/12 ,  C07D231/20 ,  C07D231/22 ,  C07D231/24 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

    CPC分类号： C07D231/20 ,  Y10S514/869

    摘要： Pyrazole derivatives of the formula: ##STR1## and pharmaceutically acceptable nontoxic salts thereof WHEREINR is hydrogen, trifluoromethyl or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is alkyl;R.sup.3 is aryl substituted by:A. one or two of the same or different substituents selected from the group consisting of halogen, trifluoromethyl, alkyl, alkenyl and alkoxy;B. one substituent selected from the group consisting of alkylamino, dialkylamino wherein the alkyl moieties may form a heterocyclic ring with the nitrogen atom to which they are attached, cycloalkyl, cycloalkenyl, trifluoromethoxy, nitro, cyano, carbonamido unsubstituted or substituted by 1 or 2 alkyl moieties, sulphonamido unsubstituted or substituted by 1 or 2 alkyl moieties, and SO.sub.n -alkyl wherein n is 0, 1 or 2;C. one substituent selected from the group consisting of alkylamino, dialkylamino wherein the alkyl moieties may form a heterocyclic ring with the nitrogen atom to which they are attached, cycloalkyl, cycloalkenyl, trifluoromethoxy, nitro, cyano, carbonamido unsubstituted or substituted by 1 or 2 alkyl moieties, sulphonamido unsubstituted or substituted by 1 or 2 alkyl moieties, and SO.sub.n -alkyl wherein n is 0, 1 or 2, and by one or two substituents selected from the group consisting of alkyl, alkenyl, alkoxy, halogen and trifluoromethyl; orD. two substituents on the aryl moiety form a branched or unbranched saturated or unsaturated 5- to 7-membered isocyclic or heterocyclic ring, which ring can also have 1 or 2 oxygen atoms or sulfur atoms; or SO.sub.n -alkyl wherein n is 0, 1 or 2; 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： 下式的吡唑衍生物：其中R为氢，三氟甲基或烷基; R1是氢或烷基; R2是烷基; R3是被下列基团取代的芳基：

    Pyrazol-5-ones
    4.
    发明授权
    Pyrazol-5-ones 失效
    吡唑-5-酮

    公开(公告)号：US3992404A

    公开(公告)日：1976-11-16

    申请号：US578516

    申请日：1975-05-19

    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 ,  C07D231/20 ,  C07D231/38

    CPC分类号： C07D231/52 ,  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 of 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-，式+ q，10和药物可接受的，其非阳离子盐，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：

    5-Sulphonyloxy pyrazole derivatives
    10.
    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。