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1. 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.

2. 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.

3. 发明授权

US4112109A 4-Substituted pyrazoles 失效
标题翻译： 4-取代的吡唑
公开(公告)号：US4112109A
公开(公告)日：1978-09-05
申请号：US766187
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.
摘要翻译：其中R为氢，烷基，芳基，芳烷基，三氟甲基或杂环的吡唑类化合物。 R 1为未取代或被卤素，三氟甲基，烷基，烷氧基或硝基取代的芳基或芳烷基; 或卤素取代的烷硫基部分; R2是低级烷基; 苯基; 或苄基; R 3为未取代的或被烷基，烯基，烷氧基，卤素，三氟甲基，三氟甲氧基，单 - 或二 - 烷基氨基，硝基，氰基，甲酰氨基，磺酰氨基或SO-烷基取代的芳基; 与5至7元环或杂环稠合的苯基，所述杂环具有1或2个氧或硫杂原子; 或吡啶基; 并且R 4是未取代的或取代的碳酰基或磺酰基; 有用于他们的DIYTIC，SALURETIC，ANTIHYPERTENSIVE和抗生素属性。

4. 发明授权

US4117145A 1-Substituted pyrazoles 失效
公开(公告)号：US4117145A
公开(公告)日：1978-09-26
申请号：US766715
申请日：1977-02-08
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 , A61K31/415 , A61K31/445
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; or (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.

5. 发明授权

US4099011A 4-Substituted pyrazoles 失效
标题翻译： 4-取代的吡唑
公开(公告)号：US4099011A
公开(公告)日：1978-07-04
申请号：US693970
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 , C07D231/28
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.

6. 发明授权

US4207325A 4-Substituted pyrazoles 失效
标题翻译： 4-取代的吡唑
公开(公告)号：US4207325A
公开(公告)日：1980-06-10
申请号：US870219
申请日：1978-01-17
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 , C07D231/28 , A61K31/415
CPC分类号： C07D231/20 , C07D231/28 , Y10S514/869
摘要： Pyrazoles of the formula ##STR1## whereinR 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, cycloalkyl, cycloalkenyl, 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.
摘要翻译：吡唑类化合物

7. 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.

8. 发明授权

US4117143A 1-Substituted pyrazoles 失效
公开(公告)号：US4117143A
公开(公告)日：1978-09-26
申请号：US766684
申请日：1977-02-08
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 , A61K31/415 , A61K31/445
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.2 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; or (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 substitutents 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.

9. 发明授权

US4265898A Imidazo[2,1-b]-[1,3,4]-thiadiazole compounds, composition and their medicinal use 失效
标题翻译：咪唑并[2,1-b] - [1,3,4]噻二唑化合物，组成及其药用
公开(公告)号：US4265898A
公开(公告)日：1981-05-05
申请号：US37626
申请日：1979-05-10
申请人： Harald Horstmann , Karl-August Meng, deceased , by Matthias Meng, legal representative , Friedel Seuter , Eike Moller
发明人： Harald Horstmann , Karl-August Meng, deceased , by Matthias Meng, legal representative , Friedel Seuter , Eike Moller
IPC分类号： A61K31/41 , A61P7/02 , A61P29/00 , C07D233/84 , C07D285/12 , C07D285/135 , C07D513/04
CPC分类号： C07D285/135 , C07D233/84 , C07D513/04 , Y10S514/822
摘要： The present invention relates to certain new imidazo [2,1-b]-[1,3,4]-thiadiazole compounds, to the provision of pharmaceutical compositions containing said compounds and to the use of said compounds and compositions as antithrombotic agents and thrombolytic agents.
摘要翻译：本发明涉及某些新的咪唑并[2,1-b] - [1,3,4] - 噻二唑化合物，提供含有所述化合物的药物组合物以及所述化合物和组合物作为抗血栓形成剂和溶栓剂的用途代理商

10. 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。

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