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1. 发明授权

US4122281A 5-Sulphonyloxy pyrazole derivatives 失效
标题翻译： 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。

2. 发明授权

US4000294A 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.

3. 发明授权

US3952008A Pyrazol-5-ones 失效
标题翻译：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：

4. 发明授权

US4002641A Pyrazole derivatives 失效
标题翻译：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：

5. 发明授权

US3992404A Pyrazol-5-ones 失效
标题翻译：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：

6. 发明授权

US4122280A Pyrazole derivatives 失效
标题翻译：吡唑衍生物
公开(公告)号：US4122280A
公开(公告)日：1978-10-24
申请号：US672302
申请日：1976-03-31
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;R.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; 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。

7. 发明授权

US4112227A Pyrazol-5-ones 失效
标题翻译：吡唑-5-酮
公开(公告)号：US4112227A
公开(公告)日：1978-09-05
申请号：US543664
申请日：1975-01-24
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 , C07D231/24 , C07D231/52 , A61K31/415
CPC分类号： C07D231/52 , C07D231/20 , C07D231/24 , 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 is(a) 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; or(c) 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, trifluoro-methoxy, 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 cabamoyl 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; or(e) 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-酮及其药学上可接受的无毒盐，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个氢原子是由1至4个碳原子的烷基取代的1个氢原子，每个碳原子上的1个氢原子被1至4个碳所代替的亚烷基取代的乙烯通过氧原子或硫原子连接到R2上的异构体或乙烯; （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）甲基; 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：

8. 发明授权

US4018890A Pyrazol-5-one pharmaceutical compositions and methods for effecting diuresis, saluresis and for treating hypertension 失效
标题翻译：吡唑-5-酮药物组合物和用于治疗高血压的利尿剂，药物和治疗方法
公开(公告)号：US4018890A
公开(公告)日：1977-04-19
申请号：US459408
申请日：1974-04-09
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 , C07D231/52 , A61K31/415
CPC分类号： C07D231/52 , C07D231/20 , Y10S514/869
摘要： Pharmaceutical compositions useful for effecting diuresis and saluresis and for treating hypertension in humans and animals are produced by combining a pyrazol-5-one of the formula: ##SPC1##Or a pharmaceutically acceptable nontoxic salt thereofWhereinR is hydrogen, lower alkyl or amino;X is methylene, ethylene, methylene wherein 1 hydrogen atom is substituted by lower alkyl, or ethylene wherein 1 hydrogen atom is substituted by lower alkyl or 1 hydrogen atom on each of the two carbon atoms is substituted by lower alkyl;Y is a direct bond, oxygen or sulphur, provided that when X is methylene wherein 1 hydrogen atom is substituted by alkyl of 1 to 4 carbon atoms, Y is a direct bond;Z is aryl of 6 to 10 carbon atoms 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 4 carbon atoms, alkenyl or 2 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, and alkenoxy of 2 to 4 carbon atoms;B. cycloalkyl of 5, 6 or 7 carbon atoms, or cycloalkenyl of 5, 6 or 7 carbon atoms;C. lower alkylamino, dilower alkylamino, trifluoromethoxy, nitro, cyano, carbamoyl, lower alkylcarbamoyl, dilower alkylcarbamoyl, sulphamyl, lower alkylsulphamyl, dilower alkylsulphamyl, --SO.sub.n --lower alkyl wherein n is 0, 1 or 2, or said dialkylamino, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, sulphamyl, alkylsulphamyl, or dialkylsulphamyl, the nitrogen atom of which is a member of a 5-, 6- or 7-membered ring or said ring which additionally contains an oxygen atom;D. lower alkylamino, dilower alkylamino, trifluoromethoxy, nitro, cyano, carbamoyl, lower alkylcarbamoyl, dilower alkylcarbamoyl, sulphamyl, lower alkylsulphamyl, dilower alkylsulphamyl, or --SO.sub.n --lower alkyl wherein n is 0, 1 or 2, and 1 or 2 substituents selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkenyl of 2 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkenoxy of 2 to 4 carbon atoms, halogen and trifluoromethyl; orE. a fused, saturated or unsaturated 5-, 6- or 7-membered ring or said ring additionally containing 1 or 2 oxygen or sulphur atoms,In combination with a pharmaceutically acceptable nontoxic inert diluent or carrier.The compositions are preferably administered orally or parenterally and in the latter case, sterile or isotonic aqueous solutions are preferred.
摘要翻译：通过将下列通式的吡唑-5-酮组合而制备用于实现利尿和黄疸以及用于治疗人和动物高血压的药物组合物：

9. 发明授权

US3950528A 1-Substituted-3-amino-pyrazol-5-ones 失效
公开(公告)号：US3950528A
公开(公告)日：1976-04-13
申请号：US515448
申请日：1974-10-17
申请人： Harald Horstmann , Karl Meng , Egbert Wehinger
发明人： Harald Horstmann , Karl Meng , Egbert Wehinger
IPC分类号： A61K31/415
CPC分类号： Y10S514/869
摘要： Pharmaceutical compositions are prepared which comprise a diuretically effective amount, a saluretically effect amount or an antihypertensive amount of a compound of the formula ##SPC1##Or a pharmaceutically acceptable non-toxic salt thereof, wherein R is aryl which is either unsubstituted or substituted byA. 1, 2 or 3 identical or different substituents selected from the group consisting of halogen, alkyl of 1 to 8 carbon atoms, alkoxy of 1 to 8 carbon atoms, alkenoxy of 2 to 6 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, trifluoromethyl, trifluoromethoxy and phenyl;B. 1 or 2 identical or different substituents selected from the group consisting of nitro, cyano, lower alkylamino of 1 to 4 carbon atoms, a carbonamido moiety of the formula ##EQU1## and a sulphonamido moiety of the formula ##EQU2## wherein R.sub.1 and R.sub.2 are each hydrogen or straight or branched chain alkyl of 1 to 4 carbon atoms, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached are linked together to form a 5-, 6- or 7-membered heterocyclic ring wherein the nitrogen atom is the only heteroatom or wherein oxygen is also present as a ring member;C. one substituent selected from the group consisting of dialkylamino of 1 to 4 carbon atoms in each alkyl moiety, nitro, cyano and SO.sub.n -alkyl of 1 to 4 carbon atoms, wherein n is 0, 1 or 2;D. one substituent selected from the group consisting of a moiety of the formula ##EQU3## wherein R.sub.1 and R.sub.2 are as above defined, nitro, cyano, a carbonamido moiety of the formula ##EQU4## wherein R.sub.1 and R.sub.2 are as above defined, a sulphonamide moiety of the formula ##EQU5## wherein R.sub.1 and R.sub.2 are as above defined, and SO.sub.n -alkyl of 1 to 4 carbon atoms, wherein n is 0, 1 or 2, and 1 or 2 substituents selected from the group consisting of alkyl of 1 to 8 carbon atoms, alkoxy of 1 to 6 carbon atoms, halogen and trifluoromethyl;E. an annellated-branched or unbranched, saturated or unsaturated, 5-, 6- or 7-membered isocyclic or heterocyclic ring having 1 or more heteroatoms selected from the group consisting of oxygen and sulphur and wherein said aryl moiety is either unsubstituted or chlorosubstituted;F. --O--(CH.sub.2).sub.n.sub.' --N(alkyl).sub.2, wherein the alkyl groups contain a total of 2 to 4 carbon atoms and n'is 2 or 3; orG. two different substituents selected from the group consisting of alkyl of 1 to 8 carbon atoms, phenyl, halogen, alkoxy of 1 to 8 carbon atoms, trifluoromethyl, trifluoromethoxy, lower alkylamino, nitro, cyano, SO.sub.n --alkyl of 1 to 4 carbon atoms, wherein n is 0, 1 or 2, a carbonamido moiety of the formula ##EQU6## and a sulphonamido moiety of the formula ##EQU7## wherein R.sub.3 and R.sub.4 are each hydrogen or alkyl of 1 to 4 carbon atoms;in combination with a pharmaceutically acceptable non-toxic inert diluent or carrier.Diuretic therapy, saluretic therapy and antihypertensive therapy is effected in humans and animals by administering an effective amount of the active ingredient as above defined.

10. 发明授权

US3949083A Pyrazol-5-ones 失效
标题翻译：吡唑-5-酮
公开(公告)号：US3949083A
公开(公告)日：1976-04-06
申请号：US459407
申请日：1974-04-09
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 , C07D231/52 , A61K31/415
CPC分类号： C07D231/52 , C07D231/20 , Y10S514/869
摘要： Pharmaceutical compositions useful for effecting diuresis and saluresis and for treating hypertension in humans and animals are produced by combining a pyrazol-5-one of the formula: ##SPC1##Or a pharmaceutically acceptable nontoxic salt thereof whereinR is hydrogen, lower alkyl or amino;R.sup.1 is lower alkyl, alkenyl of 2 to 4 carbon atoms, monoaryl or monoaralkyl unsubstituted or substituted in the aryl moiety by 1 or 2 of the same or different substituents selected from the group consisting of lower alkyl, lower alkenyl, lower alkoxy, lower alkenoxy, halogen, nitro, cyano and trifluoromethyl;X is methylene, ethylene, methylene wherein 1 hydrogen atom is substituted by lower alkyl, or ethylene wherein 1 hydrogen atom is substituted by lower alkyl or 1 hydrogen atom on each of the two carbon atoms is substituted by lower alkyl;Y is a direct bond, oxygen or sulphur, provided that when X is methylene, Y is a direct bond; andZ is aryl unsubstituted or nuclear substituted by:A. 3 halogens;B. 1 or 2 of the same or different substituents selected from the group consisting of halogen, trifluoromethyl, lower alkyl, lower alkenyl, lower alkoxy, lower alkenoxy, cycloalkyl of 5 to 7 carbon atoms and cycloalkenyl of 5 to 7 carbon atoms;C. lower alkylamino, dilower alkylamino, trifluoromethoxy, nitro, cyano, carbamoyl, lower alkylcarbamoyl, dilower alkylcarbamoyl, sulphamyl, lower alkylsulphamyl, dilower alkylsulphamyl, or --SO.sub.n --lower alkyl wherein n is 0, 1 or 2;D. lower alkylamino, dilower alkylamino, trifluoromethoxy, nitro, cyano, carbamoyl, lower alkylcarbamoyl, dilower alkylcarbamoyl, sulphamyl, lower alkylsulphamyl, dilower alkylsulphamyl, or --SO.sub.n --lower alkyl wherein n is 0, 1 or 2, and 1 or 2 of the same or different substituents selected from the group consisting of lower alkyl, lower alkenyl, lower alkoxy, halogen, and trifluoromethyl;E. dilower alkylamino, carbamoyl, lower alkylcarbamoyl, dilower alkylcarbamoyl, sulphamyl, lower alkylsulphamyl, or dilower alkylsulphamyl wherein the nitrogen atom is a member of 5-, 6- or 7-membered heterocyclic ring or said ring which contains oxygen as an additional ring member; orF. a fused, saturated or unsaturated 5-, 6- or 7-membered ring or said ring which additionally contains 1 or 2 oxygen atoms or 1 sulphur atom,With a pharmaceutically acceptable nontoxic inert diluent or carrier.The compositions are preferably administered orally or parenterally and in the latter case, sterile or isotonic aqueous solutions are preferred.
摘要翻译：通过将下列通式的吡唑-5-酮组合而制备用于实现利尿和黄疸以及用于治疗人和动物高血压的药物组合物：

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