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    • 8. 再颁专利
      USRE30420E Pyrazol-5-ones 失效
    • Pyrazol-5-ones
    • 吡唑-5-酮
    • USRE30420E
    • 1980-10-21
    • US765666
    • 1977-02-04
    • Eike Moller , Karl-August Meng, deceased , Egbert Wehinger , Harald Horstmann
    • Eike Moller , Karl-August Meng, deceased , Egbert Wehinger , Harald Horstmann
    • C07D231/20 , C07D231/24 , C07D231/52
    • C07D231/24 , C07D231/20 , C07D231/52
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明授权
      US4002641A Pyrazole derivatives 失效
    • Pyrazole derivatives
    • 吡唑衍生物
    • US4002641A
    • 1977-01-11
    • US532311
    • 1974-12-13
    • Eike Moller , Karl Meng , Egbert Wehinger , Harald Horstmann
    • Eike Moller , Karl Meng , Egbert Wehinger , Harald Horstmann
    • 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
    • C07D231/20 , Y10S514/869
    • 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.
    • 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：
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 10. 发明授权
      US3992404A Pyrazol-5-ones 失效
    • Pyrazol-5-ones
    • 吡唑-5-酮
    • US3992404A
    • 1976-11-16
    • US578516
    • 1975-05-19
    • Eike Moller , Karl Meng , Egbert Wehinger , Harald Horstmann
    • Eike Moller , Karl Meng , Egbert Wehinger , Harald Horstmann
    • C07D231/52 , C07D231/20 , C07D231/38
    • C07D231/52 , Y10S514/822 , Y10S514/869
    • 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.
    • 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：
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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