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41. 发明专利

CA1203236A HETEROARYLOXYPROPANOLAMINES 未知
公开(公告)号：CA1203236A
公开(公告)日：1986-04-15
申请号：CA408114
申请日：1982-07-27
申请人： BOEHRINGER MANNHEIM GMBH
发明人： WIEDEMANN FRITZ , MICHEL HELMUT , WECKERLE WOLFGANG , ROESCH EGON , STREIN KLAUS
IPC分类号： A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/433 , A61K31/495 , A61K31/496 , A61P9/04 , C07D209/08 , C07D209/12 , C07D209/32 , C07D209/42 , C07D209/43 , C07D209/44 , C07D209/88 , C07D231/56 , C07D235/04 , C07D235/06 , C07D235/08 , C07D235/26 , C07D241/40 , C07D241/42 , C07D241/52 , C07D249/18 , C07D285/14 , C07D209/04
摘要： The present invention provides heteroaryloxypropanolamines of the general formula: (I) wherein A is a bi- or tricyclic heteroaromatic radical, which is optionally partly hydrogenated, X is a straightchained or branched alkylene chain containing 2 to 6 carbon atoms, R1 and R2, which can be the same or different, are hydrogen atoms or lower alkyl or benzyl radicals, R3, R4 and R5, which can be the same or different, are hydrogen atoms or lower alkyl, benzyl, formyl, lower alkanoyl, cyano, hydroxymethyl, lower alkoxycarbonyl or carbamoyl radicals or the divalent substituents sulphur or oxygen and R6, R7 and R8, which can be the same or different, are hydrogen or halogen atoms, lower alkyl, nitro, amino, lower alkylthio or lower alkoxy radicals or R6 and R7 together represent an optionally unsaturated trimethylene chain; and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions containing them.

42. 发明专利

HU183085B PROCESS FOR PREPARING NEW PHENOXY-ALKYL-CARBOXYLIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEREOF 未知
公开(公告)号：HU183085B
公开(公告)日：1984-04-28
申请号：HUBO001768
申请日：1979-03-01
申请人： BOEHRINGER MANNHEIM GMBH
发明人： WITTE ERNST-CHRISTIAN , WOLF HANS P , THIEL MAX , STEGMEIER KARLHEINZ , ROESCH EGON
IPC分类号： A61K31/19 , A61K31/085 , A61K31/165 , A61K31/18 , A61K31/195 , A61K31/22 , A61P3/06 , A61P7/02 , C07C67/00 , C07C301/00 , C07C303/38 , C07C303/40 , C07C311/03 , C07C311/04 , C07C311/06 , C07C311/14 , C07C311/16 , C07C311/17 , C07C311/29 , C07D209/48 , C07C143/72 , C07C59/70
摘要： Phenoxyalkylcarboxylic acid compounds of the formula wherein R is hydrogen or lower alkyl R1 is alkyl or aryl, aralkyl or aralkenyl radical, the aryl moiety of which can be substituted one or more times by halogen, hydroxyl, trifluoromethyl or lower alkyl, alkoxy or acyl R2 and R3 are individually selected from hydrogen or lower alkyl, and n is 0, 1, 2 or 3 and the physiologically acceptable salts, esters and amides thereof; are outstandingly effective in inhibiting thrombocyte aggregation.

43. 发明专利

DD202548A5 未知
公开(公告)号：DD202548A5
公开(公告)日：1983-09-21
申请号：DD24222082
申请日：1982-08-03
申请人： BOEHRINGER MANNHEIM GMBH
发明人： WIEDEMANN FRITZ , MICHEL HELMUT , WECKERLE WOLFGANG , ROESCH EGON , STEIN KLAUS
IPC分类号： A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/433 , A61K31/495 , A61K31/496 , A61P9/04 , C07D209/08 , C07D209/12 , C07D209/32 , C07D209/42 , C07D209/43 , C07D209/44 , C07D209/88 , C07D231/56 , C07D235/04 , C07D235/06 , C07D235/08 , C07D235/26 , C07D241/40 , C07D241/42 , C07D241/52 , C07D249/18 , C07D285/14 , C07D241/36
摘要： The present invention provides heteroaryloxypropanolamines and pharmaceutical compositions containing them, for combating, and for the prophylaxis of, cardiac and circulatory diseases. The heteroaryloxypropanolamines of the present invention are of the general formula: wherein A is a bi- or tricyclic heteroaromatic radical, which is optionally partly hydrogenated, X is a straight-chained or branched alkylene chain containing 2 to 6 carbon atoms, R1 and R2, which can be the same or different, are hydrogen atoms or lower alkyl or benzyl radicals, R3, R4 and R5, which can be the same or different, are hydrogen atoms or lower alkyl, benzyl, formyl, lower alkanoyl, cyano, hydroxymethyl, lower alkoxycarbonyl or carbamoyl radicals or the divalent substituents sulfur or oxygen and R6, R7 and R8, which can be the same or different, are hydrogen or halogen atoms, lower alkyl, nitro, amino, lower alkylthio or lower alkoxy radicals or R6 and R7 together represent an optionally unsaturated trimethylene chain; and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions containing them.

44. 发明专利

CA1145338A AMINOPROPANOL DERIVATIVES 未知
公开(公告)号：CA1145338A
公开(公告)日：1983-04-26
申请号：CA352092
申请日：1980-05-16
申请人： BOEHRINGER MANNHEIM GMBH
发明人： ROSS CARL H , KAMPE WOLFGANG , BARTSCH WOLFGANG , SPONER GISBERT , ROESCH EGON
IPC分类号： A61K31/495 , A61K31/505 , A61P9/00 , C07D211/22 , C07D213/64 , C07D235/26 , C07D241/38 , C07D241/44 , C07D401/12 , C07D401/14 , C07D241/36 , C07D401/00
摘要： The present invention provides aminopropanol derivatives of the general formula: (I) wherein R1 and R2, which can be the same or different, are hydrogen atoms or lower alkyl radicals or together represent an alkylene radical, R3 is a hydrogen atom or an acyl radical, A is one of the following structural elements: , , or in which R4 is a hydrogen atom or a lower alkyl radical, which is optionally substituted by hydroxyl, halogen, phenyl or alkylthio and R5 and R6, which can be the same or different, are lower alkyl radicals, and B is an alkylamino radical which optionally carries a phenyl and/or phenoxy radical, which can be substituted one or more times by halogen, hydroxyl, lower alkyl, lower acyl, lower alkylthio, acylamino, aminocarbonyl, lower alkoxy, lower alkenyloxy, phenoxy, lower alkenyl, lower alkylsulphonyl, lower alkylsulphinyl or haloalkyl, or is an an aryl- or heteroaryloxymethylpiperidine radical, which is optionally substituted onr or more times by halogen, hydroxyl or lower alkyl, which optionally carries a hydroxyl or carboxamido substituent, a lower alkoxy, lower acyl, amino, carboxamido, lower alkylcarbonylamido or lower alkylsulphonylamino radical; and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them and is also concerned with the use thereof as pharmaceuticals for combating cardiac and circulatory diseases.

45. 发明专利

FI804085L 未知
公开(公告)号：FI804085L
公开(公告)日：1981-07-08
申请号：FI804085
申请日：1980-12-31
申请人： BOEHRINGER MANNHEIM GMBH
发明人： WITTE ERNST-CHRISTIAN , WOLFF HANS PETER , STEGMEIER KARLHEINZ , ROESCH EGON
IPC分类号： A61K31/18 , A61K31/185 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/235 , A61P3/06 , A61P7/02 , A61P9/10 , C07C67/00 , C07C301/00 , C07C303/38 , C07C303/40 , C07C311/00 , C07C311/06 , C07C311/19 , C07C
摘要： The invention provides sulphonamides of the formula (I) wherein R is a hydrogen atom or a lower alkyl radical; R1 is alkyl, aryl, aralkyl or aralkenyl, the aryl moiety of which in each case can be optionally substituted one or more times by hydroxyl, halogen, trifluoromethyl, lower alkyl or alkoxy or by acyl, carboxy or alkoxycarbonyl; n is 1, 2 or 3; and W is a valence bond or a divalent aliphatic hydrocarbon linkage and the physiologically acceptable salts, esters and amides of such compound. These compounds have excellent pharmacological lipid depressing activity and inhibit thrombocyte aggregation.

46. 发明专利

MX3750E 未知
公开(公告)号：MX3750E
公开(公告)日：1981-06-15
申请号：MX511375
申请日：1975-02-20
申请人： BOEHRINGER MANNHEIM GMBH
发明人： WITTE ERNST CHRISTIAN , THIEL MAX , SPONER GISBERT , ROESCH EGON , STACH KURT
IPC分类号： A61K31/495 , C07D295/04

47. 发明专利

DD143607A5 未知
公开(公告)号：DD143607A5
公开(公告)日：1980-09-03
申请号：DD21209679
申请日：1979-04-09
申请人： BOEHRINGER MANNHEIM GMBH
发明人： WIEDEMANN FRITZ , KAMPE WOLFGANG , THIEL MAX , SPONER GISBERT , ROESCH EGON , DIETMANN KARL
IPC分类号： A61K31/40 , A61K31/403 , A61P9/08 , A61P25/02 , C07D209/88 , C07D317/64 , C07D401/12 , C07D405/12
摘要： Carbazolyl-(4)-oxypropanolamine compounds of the formula (I) wherein R1 is hydrogen, lower alkanoyl or aroyl; R2 is hydrogen, lower alkyl or arylalkyl; R3 is hydrogen or lower alkyl; R4 is hydrogen or lower alkyl, or when X is oxygen, R4 together with R5 can represent -CH2-O-; X is a valency bond, -CH2-, oxygen or sulfur; Ar is mono- or bicyclic aryl or pyridyl; R5 and R6 are individually selected from hydrogen, halogen, hydroxyl, lower alkyl, aminocarbonyl, lower alkoxy, aralkyloxy, lower alkylthio, lower alkylsulphinyl or lower alkylsulphonyl; R5 and R6 together can represent methylenedioxy; and the salts thereof with physiologically acceptable acids are outstandingly effective in the treatment and prophylaxis of circulatory and cardiac diseases, e.g., hypertension and angina pectoris.

48. 发明专利

YU35017B PROCESS FOR PREPARING 4-(-(COUMARIN-7-YL-OXY)-ALKYL)-PIPERAZINE 未知
公开(公告)号：YU35017B
公开(公告)日：1980-06-30
申请号：YU125572
申请日：1972-05-11
申请人： BOEHRINGER MANNHEIM GMBH
发明人： WITTE ERNST-CHRISTIAN , STACH KURT , THIEL MAX , ROESCH ANDRONIKI , ROESCH EGON
IPC分类号： A61K31/35 , A61K31/351 , A61K31/352 , A61K31/495 , C07D309/16 , A61P3/00 , A61P29/00 , A61P37/08 , C07D309/32 , C07D311/16 , C07D405/00 , C07D311/00 , C07D295/00 , A61K31/33
摘要： 1335946 Coumarin-7-yloxyalkyl-piperazine derivatives BOEHRINGER MANNHEIM GmbH 11 May 1972 [14 May 1971] 22070/72 Heading C2C Novel compounds of the Formula (I) wherein R 1 is a hydrogen atom or a C 1-5 alkyl radical, R 2 is a C 1-5 alkyl radical, R 3 is an unsubstituted or substituted phenyl or benzyl radical, the substituents, when present, being halogen atoms or C 1-5 alkyl or C 1-5 alkoxy radicals, and n is 1, 2 or 3; and the pharmacologically compatible salts thereof, may be obtained by (a) condensing a compound of the Formula (II) in which X is a halogen atom, with a 7-hydroxy- 3 - R 1 - 4 - R 2 - substituted - coumarin, (b) condensation of a compound of the Formula (IV) with an R 3 -substituted-piperazine, (c) condensation of a compound of Formula (I), in which R 3 is H, with a compound of the formula X.R 3 , in which R 3 is an unsubstituted or substituted benzyl radical; or (d) condensation of a compound of the Formula (VII) with an amine of formula H 2 N-R 3 , and thereafter, if desired, converting the products into their physiologically compatible salts. Pharmaceutical compositions having antiinflammatory and anti-allergic action comprise at least one compound of the Formula (I) in admixture with a solid or liquid pharmaceutical diluent or carrier, for example in the form of tablets or dragees or suspended or dissolved in water or an oil.

49. 发明专利

AU3888578A 4-HYDROXY-2-BENZIMIDAZOLINONE DERIVATIVES 未知
公开(公告)号：AU3888578A
公开(公告)日：1980-02-21
申请号：AU3888578
申请日：1978-08-14
申请人： BOEHRINGER MANNHEIM GMBH
发明人： ROSS CARL HEINZ , FRIEBE WALTER-GUNAR , KAMPE WOLFGANG , BARTSCH WOLFGANG , ROESCH EGON
IPC分类号： A61K31/415 , A61K31/4184 , A61P9/00 , A61P25/02 , C07D235/02 , C07D235/26

50. 发明专利

YU125572A PROCESS FOR PREPARING 4-((COUMARIN-7-YL-OXY)-ALKYL)-PIPERAZINE DERIVATIVES 未知
公开(公告)号：YU125572A
公开(公告)日：1979-12-31
申请号：YU125572
申请日：1972-05-11
申请人： BOEHRINGER MANNHEIM GMBH
发明人： WITTE ERNST-CHRISTIAN , STACH KURT , THIEL MAX , ROESCH ANDRONIKI , ROESCH EGON
IPC分类号： A61K31/35 , A61K31/351 , A61K31/352 , A61K31/495 , C07D309/16 , A61P3/00 , A61P29/00 , A61P37/08 , C07D309/32 , C07D311/16 , C07D405/00 , C07D311/00 , C07D295/00 , A61K31/33
摘要： 1335946 Coumarin-7-yloxyalkyl-piperazine derivatives BOEHRINGER MANNHEIM GmbH 11 May 1972 [14 May 1971] 22070/72 Heading C2C Novel compounds of the Formula (I) wherein R 1 is a hydrogen atom or a C 1-5 alkyl radical, R 2 is a C 1-5 alkyl radical, R 3 is an unsubstituted or substituted phenyl or benzyl radical, the substituents, when present, being halogen atoms or C 1-5 alkyl or C 1-5 alkoxy radicals, and n is 1, 2 or 3; and the pharmacologically compatible salts thereof, may be obtained by (a) condensing a compound of the Formula (II) in which X is a halogen atom, with a 7-hydroxy- 3 - R 1 - 4 - R 2 - substituted - coumarin, (b) condensation of a compound of the Formula (IV) with an R 3 -substituted-piperazine, (c) condensation of a compound of Formula (I), in which R 3 is H, with a compound of the formula X.R 3 , in which R 3 is an unsubstituted or substituted benzyl radical; or (d) condensation of a compound of the Formula (VII) with an amine of formula H 2 N-R 3 , and thereafter, if desired, converting the products into their physiologically compatible salts. Pharmaceutical compositions having antiinflammatory and anti-allergic action comprise at least one compound of the Formula (I) in admixture with a solid or liquid pharmaceutical diluent or carrier, for example in the form of tablets or dragees or suspended or dissolved in water or an oil.

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