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41. 发明授权

US4113957A 1-Substituted pyrazoles 失效
标题翻译： 1-取代的吡唑
公开(公告)号：US4113957A
公开(公告)日：1978-09-12
申请号：US693971
申请日：1976-06-08
申请人： Eike Moller , Karl-August Meng, deceased , Egbert Wehinger , Harald Horstmann , Friedel Seuter
发明人： Eike Moller , Karl-August Meng, deceased , Egbert Wehinger , Harald Horstmann , Friedel Seuter
IPC分类号： C07D231/20
CPC分类号： C07D231/20 , Y10S514/822 , Y10S514/869
摘要： Pyrazoles of the formula ##STR1## wherein R is hydrogen, alkyl, trifluoromethyl, aryl, aralkyl or a heterocycle;R.sup.1 is hydrogen, alkyl, aryl or aralkyl;R.sup.3 is an unsubstituted or substituted carboacyl or sulphonyl moiety;X is (a) methylene; (b) ethylene; (c) ethylene wherein 1 hydrogen atom on one or both of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms; (d) ethylene, or ethylene wherein 1 hydrogen atom on one or both of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, linked to R.sup.2 via an oxygen or sulphur atom; (e) propenyl; of (f) propenyl wherein a hydrogen atom on 1, 2 or 3 of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms; said propenyl moiety being linked to the N.sup.1 atom via a methylene moiety; andR.sup.2 is aryl unsubstituted or substituted by 1 or 2 of the same or different substituents selected from the group consisting of alkyl, alkenyl, alkoxy, halo, trifluoromethyl, trifluoromethoxy, cycloalkyl, cycloalkenyl, mono- or di-alkylamino, nitro, cyano, unsubstituted or substituted carboxamido, unsubstituted or substituted sulphonamido and SO.sub.n -alkyl wherein n is 0 to 2, or aryl having 2 substituents which together form a branched or unbranched, saturated or unsaturated 5- to 7-membered isocyclic or heterocyclic ring, said heterocyclic ring containing 1 or 2 oxygen or sulphur atoms, or pyridyl;Are useful for their diuretic, saluretic, antihypertensive and antithrombotic properties.

42. 发明授权

US4113872A 4-Substituted pyrazoles 失效
公开(公告)号：US4113872A
公开(公告)日：1978-09-12
申请号：US766235
申请日：1977-02-07
申请人： Eike Moller , Karl Meng, deceased , Egbert Wehinger , Harald Horstmann , Friedel Seuter
发明人： Eike Moller , Karl Meng, deceased , Egbert Wehinger , Harald Horstmann , Friedel Seuter
IPC分类号： C07D231/20 , C07D231/28 , A61K31/415
CPC分类号： C07D231/20 , C07D231/28 , Y10S514/822 , Y10S514/869
摘要： Pyrazoles of the formula ##STR1## wherein R is hydrogen, alkyl, aryl, aralkyl, trifluoromethyl or a heterocycle;R.sup.1 is aryl or aralkyl unsubstituted or substituted by halo, trifluoromethyl, alkyl, alkoxy or nitro; or a halo-substituted alkylthio moiety;R.sup.2 is lower alkyl; phenyl; or benzyl;R.sup.3 is aryl unsubstituted or substituted by alkyl, alkenyl, alkoxy, halo, trifluoromethyl, trifluoromethoxy, mono- or di-alkylamino, nitro, cyano, carboxamido, sulphonamido or SO.sub.n -alkyl; phenyl having fused thereto a 5- to 7-membered isocyclic or heterocyclic ring, said heterocyclic ring having 1 or 2 oxygen or sulphur heteroatoms; or pyridyl; andR.sup.4 is unsubstituted or substituted carboacyl or sulphonyl; are useful for their diuretic, saluretic, antihypertensive and antithrombotic properties.

43. 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：

44. 发明授权

US4053621A 1-[2-(.beta.Naphthyloxy)ethyl]-3-methylpyrazolone-(5) and antithrombotic and antithrombolytic compositions and methods utilizing them 失效
标题翻译： 1-（2-（'萘基）乙基）-3-甲基吡唑啉酮（5）和抗生素和抗微生物组合物及其利用其的方法
公开(公告)号：US4053621A
公开(公告)日：1977-10-11
申请号：US582773
申请日：1975-06-02
申请人： Eike Moller , Karl Meng, deceased , Harald Horstmann , Friedel Seuter , Egbert Wehinger
发明人： Eike Moller , Karl Meng, deceased , Harald Horstmann , Friedel Seuter , Egbert Wehinger
IPC分类号： A61K31/415 , A61P7/02 , C07D231/20 , A61K31/295 , C07D231/08 , C07F15/02
CPC分类号： C07D231/20
摘要： 1-[2-(.beta.-Naphthyloxy)ethyl]-3-methylpyrazolone-(5) and its salts are useful in the treatment and prophylaxis of thrombotic conditions. The compound is prepared through the reaction of 2-(.beta.-naphthyloxy)ethylhydrazine with either an acetoacetate or an ester of tetrolic acid, or through the condensation of 3-methylpyrazolinone-(5) with a derivative of 2-(.beta.-naphthyloxy)ethane, optionally with subsequent salt formation.

45. 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：

46. 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.

47. 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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