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1. 发明授权

US3925446A 1-Aryloxy-2-hydroxy-3-alkynylamino-propanes 失效
标题翻译： 1-芳氧基-2-羟基-3-炔基氨基丙烷
公开(公告)号：US3925446A
公开(公告)日：1975-12-09
申请号：US44471374
申请日：1974-02-22
申请人： BOEHRINGER SOHN INGELHEIM
发明人： KOPPE HERBERT , KUMMER WERNER , STAHLE HELMUT , MUACEVIC GOJKO
IPC分类号： A61K31/135 , A61K31/138 , A61K31/165 , A61K31/19 , A61K31/24 , A61K31/245 , A61K31/357 , A61K31/36 , A61P9/00 , A61P25/02 , C07B57/00 , C07C67/00 , C07C213/00 , C07C213/02 , C07C217/30 , C07C217/32 , C07C217/56 , C07C217/84 , C07C227/00 , C07C227/08 , C07C227/16 , C07C227/18 , C07C227/20 , C07C227/22 , C07C229/64 , C07C231/00 , C07C231/12 , C07C233/00 , C07C233/16 , C07C233/20 , C07C233/25 , C07C233/43 , C07C233/54 , C07C235/34 , C07C235/46 , C07C239/00 , C07C253/00 , C07C253/30 , C07C255/37 , C07C255/53 , C07C255/54 , C07C255/58 , C07C269/00 , C07C275/34 , C07D317/64 , C07C121/80
CPC分类号： C07C255/00 , C07C275/34
摘要： wherein R1, R2, R3, R4 and R5 are hydrogen or various substituents, and their physiologically compatible acid addition salts, as well as the process for producing the compounds, therapeutic compositions and methods. The 1-aryloxy-2-hydroxy-3alkynylamino-propanes have andrenolytic properties and bloodpressure reducing properties.

Racemic and optically active compounds of the formula
摘要翻译：式R 4 | | O-CH 2 -CHOH-CH 2 -NH-CC 3 CH 2 -CH 2 R 5的外消旋和旋光活性化合物其中R1，R2，R3，R4和R5是氢或各种取代基，以及它们的生理上相容的酸加成盐，以及生产化合物的方法，治疗组合物和方法。 1-芳氧基-2-羟基-3-炔基氨基丙烷具有溶血性质和降血压性质。

2. 发明授权

US3644469A 1-(cyanophenoxy)-2-hydroxy-3-sec.-alkylamino-propanes 失效
标题翻译： 1-（氰基苯氧基）-2-羟基-3-甲基 - 氨基亚氨基丙酸酯
公开(公告)号：US3644469A
公开(公告)日：1972-02-22
申请号：US3644469D
申请日：1968-12-18
申请人： BOEHRINGER SOHN INGELHEIM
发明人： KOPPE HERBERT , KUMMER WERNER , STAHLE HELMUT , ZEILE KARL , TRAUNECKER WERNER
IPC分类号： A61K31/04 , A61K31/135 , A61K31/14 , A61K31/195 , A61K31/215 , A61K31/275 , C07C67/00 , C07C253/00 , C07C255/54 , C07D317/64 , C07C121/52 , C07C121/66
CPC分类号： C07D317/64 , A61K31/04 , A61K31/135 , A61K31/14 , A61K31/195 , A61K31/215 , A61K31/275 , A61K31/505
摘要： RACEMIC MIXTURES AND OPTICALLY ACTIVE ISOMERS OF 1PHENOXY - 2- HYDROXY -3- SEC, - ALKYLAMINO - PROPANES OF THE FORMULA

R,R1,(R2-CH(-R3)-NH-CH2-CH(-OH)-CH2-O-)BENZENE

WHEREIN R IS SELECTED FROM THE GROUP CONSISTING OF

-(CH2)X-CN

-(CH2)X-NH2 AND -(CH2)X+1-OH WHERE X IS 0,1, 2 OR 3, CARBOXYL, ALKOXYCARBONYL OR 1 TO 5 CARBON ATOMS OF THE ALKOXYL PART AND ALKENYLOXY AND ALKYNYLOXY OF 2 TO 5 CARBON ATOMS, R1 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HALOGEN, LOWER ALKYL AND LOWER ALKOXY OF 1 TO 5 CARBON ATOMS, LOWER ALKENYL OF 2 TO 5 CARBON ATOMS, CYANO AND NITRO AND R AND R1 TAKEN TOGETHER MAY BE METHYLENEDIOXY, R2 IS AN ALKYL OF 1 TO 5 CARBON ATOMS AND R3 IS ALKYL OR 2 TO 6 CARBON ATOMS AND THEIR NON-TOXIC, PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS HAVING B-ADRENOLYTIC AND BLOOD PRESSURE REDUCING PROPERTIES.

3. 发明授权

US3887552A 5-Oxo-2,3-dihydro-imidazo(1,2-a)-s-triazines 失效
标题翻译： 5-氧代-2,3-二氢 - 咪唑并（1,2-a）-s-三嗪
公开(公告)号：US3887552A
公开(公告)日：1975-06-03
申请号：US45028974
申请日：1974-03-12
申请人： BOEHRINGER SOHN INGELHEIM
发明人： STAHLE HELMUT , KOPPE HERBERT , KUMMER WERNER , HOEFKE WOLFGANG
IPC分类号： C07D403/04 , A61K31/53 , A61P1/04 , A61P3/00 , A61P7/10 , A61P9/12 , A61P25/04 , A61P25/24 , A61P25/26 , C07D487/04 , C07D57/34
CPC分类号： A61K31/53 , C07D487/04
摘要： Compounds of the formula

WHEREIN R1 is phenyl or mono-, di- or tri-substituted phenyl, THE SUBSTITUENTS BEING EACH HALOGEN, METHYL, METHOXY OR TRIFLUOROMETHYL, AND R2 is hydrogen, phenyl or halo-phenyl; THE COMPOUNDS ARE USEFUL AS ANTIDEPRESSANTS.
摘要翻译：式WHEREIN R 1的化合物是苯基或单 - ，二 - 或三 - 取代的苯基，每个卤素，甲基，甲氧基或三氟甲基的取代基，R 2是氢，苯基或卤代 - 苯基; 化合物作为抗生素有用。

4. 发明授权

US3622579A Derivatives of 2-anilino-1,3-diazacyclopentene-(2) 失效
标题翻译： 2-苯胺基-1,3-二氮杂环戊烯的衍生物（2）
公开(公告)号：US3622579A
公开(公告)日：1971-11-23
申请号：US3622579D
申请日：1969-08-28
申请人： BOEHRINGER SOHN INGELHEIM
发明人： STAHLE HELMUT , KOPPE HERBERT , INGELHEIM KARL ZEILE , HOEEKE WOLFGANG , SAMTLEBEN HANS-WOLFGANG
IPC分类号： C07D233/50 , C07D49/34
CPC分类号： C07D233/50
摘要： The compounds are 2-(disubstituted-anilino)-1,3diazacyclopentenes-(2) and acid addition salts thereof, useful as hypotensives in warm-blooded animals.

5. 发明授权

US3872147A 1-phenoxy-2-hydroxy-3-alkylamino-propanes 失效
标题翻译： 1-苯氧基-2-羟基-3-烷基氨基丙酸
公开(公告)号：US3872147A
公开(公告)日：1975-03-18
申请号：US20431671
申请日：1971-12-02
申请人： BOEHRINGER SOHN INGELHEIM
发明人： KOPPE HERBERT , KUMMER WERNER , STAHLE HELMUT , ZEILE KARL , ENGELHARDT ALBRECHT
IPC分类号： A61K31/235 , A61K31/13 , A61K31/135 , A61K31/24 , A61K31/275 , A61K31/505 , A61P9/08 , A61P9/10 , A61P9/12 , C07C67/00 , C07C213/00 , C07C217/32 , C07C253/00 , C07C255/54 , C07D309/12 , C07C121/78
CPC分类号： C07D309/12 , A61K31/135 , A61K31/505 , A61K2300/00
摘要： The compounds are 1-phenoxy-2-hydroxy-3-alkylamino-propanes and non-toxic acid addition salts thereof, useful as Beta adrenolytics and hypotensives in warm-blooded animals.
摘要翻译：该化合物是1-温热血动物中可用作β-肾上腺素和低血糖的1-苯氧基-2-羟基-3-烷基氨基丙烷及其无毒的酸加成盐。

6. 发明授权

US3872121A 2-(Phenyl-amino-2-imidazolines and salts thereof 失效
标题翻译： 2-（苯基 - 氨基-2-咪唑啉及其盐
公开(公告)号：US3872121A
公开(公告)日：1975-03-18
申请号：US35541273
申请日：1973-04-30
申请人： BOEHRINGER SOHN INGELHEIM
发明人： KUMMER WERNER , STAHLE HELMUT , KOPPE HERBERT , HOEFKE WOLFGANG
IPC分类号： C07D233/50 , C07D239/06 , C07D401/12 , C07D403/04 , C07D57/00
CPC分类号： C07D233/50
摘要： Compounds of the formula

WHEREIN R1, R2 and R3, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, methyl, ethyl, ethoxy, trifluoromethyl or cyano, and R4 and R5, which must be different, are each hydrogen,

WHERE R6 and R7, which may be identical to or different from each other, are each hydrogen, methyl or optionally substituted phenyl, or, together with each other, ethylene or propylene, R8 and R9, which may be identical to or different from each other, are each hydrogen, halogen, methyl or nitro, A is nitrogen or -CH-, and N IS 0 OR 1, AND NON-TOXIC, PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF; THE COMPOUNDS AS WELL AS THE SALTS ARE USEFUL AS HYPOTENSIVES.
摘要翻译：可以相同或不同的式WHEREIN R 1，R 2和R 3的化合物各自为氢，氟，氯，溴，甲基，乙基，乙氧基，三氟甲基或氰基，R4和R5必须为不同的是各自为氢，其中可以彼此相同或不同的R 6和R 7各自为氢，甲基或任选取代的苯基，或彼此一起形成乙烯或丙烯，R 8和R 9，其可以是相同或不同，分别为氢，卤素，甲基或硝基，A为氮或-CH-，N为0或1，以及非毒性，药理学上可接受的酸添加量; 化合物作为有效的低分子化合物。

7. 发明授权

US3468887A Process for the preparation of 2-phenylamino-1,3-diazacycloalkenes-2 失效
标题翻译：制备2-苯基-1,3-二氮杂环戊烯-2的方法
公开(公告)号：US3468887A
公开(公告)日：1969-09-23
申请号：US67775567
申请日：1967-10-24
申请人： BOEHRINGER SOHN INGELHEIM
发明人： STAHLE HELMUT , ZEILE KARL
IPC分类号： A61K31/00 , C07D233/50 , C07D239/14 , C07D49/30 , A61K27/00 , C07D49/00
CPC分类号： A61K31/00 , C07D233/50 , C07D239/14

8. 发明授权

US3914432A Pharmaceutical compositions containing a 1-(cyano-phenoxy)-2-hydroxy-3-alkylamino-propane and method of use 失效
标题翻译：含有1-（氰基 - 苯氧基）-2-羟基-3-烷基氨基丙烷的药物组合物及其使用方法
公开(公告)号：US3914432A
公开(公告)日：1975-10-21
申请号：US54143075
申请日：1975-01-16
申请人： BOEHRINGER SOHN INGELHEIM
发明人： KOPPE HERBERT , KUMMER WERNER , STAHLE HELMUT , ZEILE KARL , ENGELHARDT ALBRECHT
IPC分类号： A61K31/135 , A61K31/505 , C07D309/12 , A61K31/275
CPC分类号： C07D309/12 , A61K31/135 , A61K31/505 , A61K2300/00
摘要： Pharmaceutical compositions containing as an active ingredient a compound of the formula

wherein R is branched alkyl of 5 to 8 carbon atoms containing a quaternary carbon atom which is attached directly or through an alkylene chain of 1 to 4 carbon atoms to the amino nitrogen atom, and R2 is hydrogen or chlorine, OR A NON-TOXIC, PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALT THEREOF; AND A METHOD OF USING THE SAME AS Beta -ADRENOLYTICS AND HYPOTENSIVES.
摘要翻译：含有式CN | R2-O-CH2-CH-CH2-NH-R | OH化合物作为活性成分的药物组合物，其中R是含有直接连接的季碳原子的5-8个碳原子的支链烷基，通过1至4个碳原子的亚烷基链连接到氨基氮原子上，R2是氢或氯，或非毒性，药理学上可接受的酸加成盐; 以及将其用作β-萘二甲酸和低聚物的方法。

9. 发明授权

US3888898A N,n'-bis-(3-phenoxy-2-hydroxy-propyl)-alkenediamines and salts thereof 失效
标题翻译： N，N'-BIS-（3-苯氧基-2-羟基丙基） - 二烯丙基胺及其盐
公开(公告)号：US3888898A
公开(公告)日：1975-06-10
申请号：US33626973
申请日：1973-02-27
申请人： BOEHRINGER SOHN INGELHEIM
发明人： KOPPE HERBERT , STAHLE HELMUT , KUMMER WERNER , MUACEVIC GOJKO , TRAUNECKER WERNER
IPC分类号： A61K31/135 , A61K31/16 , A61K31/165 , A61K31/19 , A61K31/215 , A61P25/02 , C07C67/00 , C07C213/00 , C07C217/32 , C07C217/48 , C07C233/18 , C07C233/25 , C07C233/36 , C07C233/43 , C07C233/47 , C07C233/54 , C07C235/46 , C07C235/60 , C07C237/30 , C07C239/00 , C07C253/00 , C07C255/54 , C07C275/24 , C07C275/34 , C07C121/78
CPC分类号： C07C275/34 , C07C275/24
摘要： Compounds of the formula

WHEREIN R1 is -OH; -COOH; -CONH2; -NO2; -CF3; halogen; alkyl of 4 to 5 carbon atoms; alkoxy of 4 to 5 carbon atoms; alkenyl of 3 to 5 carbon atoms; alkynyl of 2 to 5 carbon atoms; alkenyloxy of 3 to 5 carbon atoms; alkynyloxy of 3 to 5 carbon atoms; acyl; alkylthio of 1 to 4 carbon atoms; hydroxyalkyl of 1 to 5 carbon atoms; aryl; aryl-lower alkyl; aryloxy; arylamino; aryl-lower alkoxy; aryloxy-lower alkyl; cycloalkyl of 3 to 7 carbon atoms; alkoxyalkyl of 2 to 4 carbon atoms; alkylsulfonylamido of 1 to 4 carbon atoms; dialkylsulfonamido of 2 to 8 carbon atoms; -(CH2)x-CN; -(CH2)x-NH2; -(CH2)x-NH-COOR5; -(CH2)x-NH-acyl; -(CH2)x-NH-CO-NR6R7; -COOR; where X IS 0, 1, 2 OR 3, R is alkyl of 1 to 4 carbon atoms, R5 is alkyl of 1 to 3 carbon atoms, and R6 and R7 are each hydrogen, alkyl of 1 to 4 carbon atoms, alkenyl of 3 to 5 carbon atoms or, together with each other and the nitrogen atom to which they are attached, a 5- to 6membered heterocycle; OR, WHERE R4 is other than hydrogen, also alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms; R2 is hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 5 carbon atoms, alkenyl of 2 to 5 carbon atoms or alkenyloxy of 2 to 5 carbon atoms; R3 is hydrogen, halogen, alkyl of 1 to 5 carbon atoms or alkoxy of 1 to 5 carbon atoms; R2 and R3, together with each other, form a saturated or unsaturated carbocyclic ring or heterocyclic ring; R4 is hydrogen, alkyl of 1 to 5 carbon atoms or aralkyl; and N IS AN INTEGER FROM 1 TO 10, INCLUSIVE; AND THEIR NON-TOXIC, PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS; THE COMPOUNDS AS WELL AS THEIR SALTS ARE USEFUL AS Beta ADRENERGIC BLOCKING AGENTS AND HYPOTENSIVES.

10. 发明授权

US3595961A Hypotensive compositions containing 2-(2' - halo-anilino) - 1,3 -diazacyclopentenes-(2) and methods of using the same 失效
标题翻译：含有2-（2'-羟基 - 苯胺基）-1,3-二氮杂环戊烯的低分子组合物 - （2）及其使用方法
公开(公告)号：US3595961A
公开(公告)日：1971-07-27
申请号：US81720069
申请日：1969-04-17
申请人： BOEHRINGER SOHN INGELHEIM
发明人： STAHLE HELMUT , KOPPE HERBERT , ZEILE KARL , WOLF MARTIN , HOEFKE WOLFGANG
IPC分类号： C07D233/50 , A61K15/12
CPC分类号： C07D233/50
摘要： HYPOTENSIVE COMPOSITIONS COMPRISING A DERIVATIVE OF 2(2''-HALO-ANILINO)-1,3-DIAZACYCLOPENTENE-(2) AS AN ACTIVE INGREDIENT, AND A METHOD OF REDUCING THE BLOOD PRESSURE IN WARM-BLOODED ANIMALS THEREWITH.

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