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1. 发明授权

US4552874A Pyrazolooxazines, pyrazolothiazines, and pryazoloquinolines and their use as medicaments 失效
标题翻译：吡唑并恶嗪，吡唑并噻嗪和吡唑并喹啉及其作为药物的用途
公开(公告)号：US4552874A
公开(公告)日：1985-11-12
申请号：US462864
申请日：1983-02-01
申请人： Mithat Mardin , Rudolf Sundermann , Friedrich Hoffmeister , Wolf-Dieter Busse , Harald Horstmann , Siegfried Raddatz
发明人： Mithat Mardin , Rudolf Sundermann , Friedrich Hoffmeister , Wolf-Dieter Busse , Harald Horstmann , Siegfried Raddatz
IPC分类号： A61K31/435 , A61K31/535 , A61K31/54 , A61P1/04 , A61P7/02 , A61P9/10 , A61P29/00 , A61P43/00 , C07D265/36 , C07D471/04 , C07D498/04 , C07D498/14 , C07D513/04
CPC分类号： C07D471/04 , C07D265/36 , C07D513/04
摘要： The invention relates to pyrazolooxazines, pyrazolothiazines and pyrazoloquinolines defined herein by Formula I. The invention also includes compositions containing said Formula I compounds and methods for the use of said compounds and compositions for their lipoxygenase-inhibiting properties. Also included in the invention are methods for the manufacture of said compounds of Formula I.
摘要翻译：本发明涉及由式I定义的吡唑并恶嗪，吡唑并噻嗪和吡唑并喹啉。本发明还包括含有所述式I化合物的组合物和所述化合物和组合物用于其脂氧合酶抑制性质的方法。本发明还包括制备所述式I化合物的方法。

2. 发明授权

US4256749A Fluorine-containing 1,4-dihydropyridine compounds, pharmaceutical compositions thereof and their medicinal use 失效
标题翻译：含氟的1,4-二氢吡啶化合物及其药物组合物及其医药用途
公开(公告)号：US4256749A
公开(公告)日：1981-03-17
申请号：US74048
申请日：1979-09-10
申请人： Harald Horstmann , Friedrich Bossert , Arend Heise , Stanislav Kazda
发明人： Harald Horstmann , Friedrich Bossert , Arend Heise , Stanislav Kazda
IPC分类号： A61K31/445 , A61K31/451 , A61K31/455 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/08 , C07D211/90 , C07D401/04 , A61K31/44 , C07D213/55
CPC分类号： C07D401/04 , C07D211/90
摘要： The invention relates to fluorine-containing 1,4-dihydropyridine compounds and method for their preparation. Also included are compositions containing said fluorine-containing 1,4-dihydropyridine compounds and the use of said compounds and compositions as agents for influencing circulation.
摘要翻译：本发明涉及含氟1,4-二氢吡啶化合物及其制备方法。还包括含有所述含氟1,4-二氢吡啶化合物的组合物以及所述化合物和组合物作为影响循环的试剂的用途。

3. 再颁专利

USRE30420E Pyrazol-5-ones 失效
标题翻译：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.

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

US4956361A New combination products having an antidepressant action 失效
标题翻译：具有抗抑郁作用的新组合产品
公开(公告)号：US4956361A
公开(公告)日：1990-09-11
申请号：US370425
申请日：1989-06-23
申请人： Jorg Traber , Harald Horstmann
发明人： Jorg Traber , Harald Horstmann
IPC分类号： C07D211/90 , A61K31/44 , A61K31/455 , A61K31/55 , A61P25/24 , A61P25/26
CPC分类号： A61K31/44 , A61K31/55
摘要： The invention relates to combination products with a synergistic action and antidepressant activity, containing substances having antidepressant activity and compounds having antagonistic activity and belonging to the class of dihydropyridines, and to the use of the dihydropyridines in antidepressants.
摘要翻译：本发明涉及具有协同作用和抗抑郁活性的组合产品，其含有具有抗抑郁活性的物质和具有拮抗活性且属于二氢吡啶类的化合物，以及二氢吡啶类在抗抑郁药中的用途。

7. 发明授权

US4937343A 2-pyrimidinyl-1-piperazine derivatives 失效
标题翻译： 2-嘧啶基-1-哌嗪衍生物
公开(公告)号：US4937343A
公开(公告)日：1990-06-26
申请号：US247813
申请日：1988-09-22
申请人： Peter-Rudolf Seidel , Harald Horstmann , Jorg Traber , Wolfgang Dompert , Thomas Glaser , Teunis Schuurman
发明人： Peter-Rudolf Seidel , Harald Horstmann , Jorg Traber , Wolfgang Dompert , Thomas Glaser , Teunis Schuurman
IPC分类号： A61K31/505 , A61K31/517 , A61K31/54 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P29/00 , C07D239/42 , C07D239/96 , C07D401/12 , C07D403/04 , C07D403/12 , C07D403/14 , C07D417/12
CPC分类号： C07D239/42 , C07D239/96 , C07D401/12 , C07D403/04 , C07D403/12 , C07D403/14 , C07D417/12
摘要： The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.

8. 发明授权

US4871767A Medicament preparations 失效
标题翻译：药物制剂
公开(公告)号：US4871767A
公开(公告)日：1989-10-03
申请号：US93839
申请日：1987-09-04
申请人： Bernhard Beckermann , Hans-Dieter Dell , Harald Horstmann , Reinhold Kraus
发明人： Bernhard Beckermann , Hans-Dieter Dell , Harald Horstmann , Reinhold Kraus
IPC分类号： A61K31/245 , A61K31/24 , A61P25/04 , A61P29/00
CPC分类号： A61K31/24 , Y10S514/936
摘要： Medicament preparations contain 2-(2-hydroxyethoxy)-ethyl N-(.alpha.,.alpha.,.alpha.-trifluoro-m-tolyl)-anthranilate and dimethyl sulphoxide.
摘要翻译：药物制剂含有2-（2-羟基乙氧基） - 乙基N-（α，α，α-三氟 - 间甲苯基） - 邻氨基苯甲酸酯和二甲基亚砜。

9. 发明授权

US4710491A N-glycosylated carboxylic acid derivatives as agents for combating rheumatic diseases 失效
标题翻译： N-糖基化羧酸衍生物作为抗风湿病的药剂
公开(公告)号：US4710491A
公开(公告)日：1987-12-01
申请号：US681965
申请日：1984-12-14
申请人： Oswald Lockhoff , Peter Stadler , Hans-Georg Opitz , Harald Horstmann , Bodo Junge , Bernhard Pelster
发明人： Oswald Lockhoff , Peter Stadler , Hans-Georg Opitz , Harald Horstmann , Bodo Junge , Bernhard Pelster
IPC分类号： A61K31/70 , A61K31/7008 , A61K31/7024 , A61K31/7028 , A61P29/00 , C07H5/06 , C07H13/04 , C07H13/06 , C07H15/04 , C07H15/12 , C07H15/18
CPC分类号： C07H13/04 , C07H13/06 , C07H15/04 , C07H15/18
摘要： A method of combating rheumatic diseases which comprises administering to a patient afflicted therewith an amount effective to combat such disease of a compound of the formula ##STR1## in which Z is a glycosyl radical bonded via the anomeric carbon atom,R.sub.1 is hydrogen or an optionally substituted hydrocarbon radical with up to 30 C atoms, which hydrocarbon radical is optionally interrupted by O, N or S, andR.sub.2 is hydrogen or an alkyl or aralkyl radical with up to 30 C atoms, which is optionally interrupted by O, N or S or substituted by an oxygen-containing group or halogen,with the proviso that COR.sub.1 is not an acyl group with 1-5 C atoms if R.sub.2 is alkyl with 10-20 C atoms.
摘要翻译：一种抗风湿性疾病的方法，其包括对患有其有效抗击下列化合物的疾病的患者施用：其中Z是通过端基异构体碳原子键合的糖基，R1是氢或任选的具有多达30个C原子的取代的烃基，该烃基任选地被O，N或S间隔，并且R 2是氢或具有至多30个C原子的烷基或芳烷基，其任选地被O，N或S 或被含氧基团或卤素取代，条件是如果R2是具有10-20个C原子的烷基，则COR1不是具有1-5个C原子的酰基。

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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