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71. 发明专利

HUT47222A PROCESS FOR PRODUCTION OF MEDICAL COMPOSITIONS SUITABLE FOR TREATMENT OF DESEASES OF CORONARY ARTERY AND BRAIN ARTERY SYSTEM 未知
公开(公告)号：HUT47222A
公开(公告)日：1989-02-28
申请号：HU78388
申请日：1988-02-18
申请人： BOEHRINGER INGELHEIM KG
发明人： SCHNORRENBERG GERD , ROOS OTTO , LOESEL WALTER , ARNDTS DIETRICH , SPECK GEORG , STRELLER ILSE
IPC分类号： C07D209/42 , A61K31/33 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/44 , A61K31/47 , A61K31/472 , A61K38/00 , A61K38/55 , A61P9/08 , A61P9/10 , A61P25/28 , C07D209/44 , C07D217/26 , C07D471/04 , C07D491/048 , C07D495/04 , A61K37/64
摘要： A compound as in formula I or its salts is used to treat coronary diseases or organic brain syndrome.

72. 发明专利

HU196203B PROCESS FOR PRODUCTION OF NEW 12-AMINE-PIRIDAZINE/4'5': 3,4/-PIROLLO-ISOQUINOLINES AND MEDICAL COMPOUNDS CONTAINING THEM 未知
公开(公告)号：HU196203B
公开(公告)日：1988-10-28
申请号：HU18386
申请日：1986-01-14
申请人： BOEHRINGER INGELHEIM KG
发明人： LOESEL WALTER , REICHL RICHARD , ROOS OTTO , SCHNORRENBERG GERD , ENSINGER HELMUT
IPC分类号： A61K31/00 , A61K31/50 , A61P9/00 , A61P25/28 , C07D471/00 , C07D471/14 , A61K31/395
摘要： 1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE 12-Amino-pyridazino[4',5':3,4]pyrrolo[2,1-a]isoquinolines of general formula I see diagramm : EP0190563,P15,F1 wherein R1 and R2 , which may be identical or different, each represent hydrogen, C3-7 cycloalkyl, C2-5 alkenyl, phenyl (optionally mono- or disubstituted by halogen atoms or methoxy groups), propargyl, a straight-chained or branched, saturated or unsaturated alkyl group with 1 to 5 carbon atoms which may be substituted by hydroxy, alkoxy with 1 to 4 carbon atoms, halogen, NH2 , NH-alkyl with 1 to 2 carbon atoms, N,N-dialkyl with 1 to 2 carbon atoms, NH-acyl with 2 to 4 carbon atoms, cycloalkyl with 3 to 7 carbon atoms, phenyl (optionally substituted by halogen, alkyl with 1 to 2 carbon atoms, alkoxy with 1 to 2 carbon atoms, NH-alkyl with 1 to 2 carbon atoms, N,N-dialkyl with 1 to 2 carbon atoms, NH2 , N-acyl with 2 to 3 carbon atoms), furyl, thienyl, a nitrogen-containing heterocyclic 5- or 6-membered ring which may optionally contain as a further heteroatom an oxygen or sulphur atom (and the ring may optionally be substituted by alkyl with 1 to 4 carbon atoms), or R1 and R2 together with the nitrogen atom represent a 3- to 7-membered ring which may optionally contain as a further heteroatom an oxygen or nitrogen atom [the ring may be optionally substituted by phenyl (C1-4 ) alkyl (this phenyl ring in turn being mono- or disubstituted by halogen atoms or methoxy groups)], or R2 , if R1 represents hydrogen, represents -NH2 , di(C1-2 ) alkylamino, acetonylamino, -NH(C2-3 ) acyl, alkylsulphonyl or alkyloxycarbonyl group with 1 to 3 carbon atoms in the alkyl chain, a isopropylideneimino group see diagramm : EP0190563,P15,F2 or a heterocyclic 5- or 6-membered ring containing a nitrogen atom and optionally containing as a further heteroatom an oxygen, nitrogen or sulphur atom, R3 , R4 and R5 , which may be identical or different, represent hydrogen or alkyl groups with 1 to 4 carbon atoms, R7 and R8 , which may be identical or different, represent hydroxy, alkoxy with 1 to 4 carbon atoms or alkylthio groups with 1 to 4 carbon atoms, and R6 and R9 , which may be identical or different, represent hydrogen, hydroxy, alkoxy with 1 to 4 carbon atoms or alkylthio groups with 1 to 4 carbon atoms or a group see diagramm : EP0190563,P16,F1 wherein R10 represents hydrogen or alkyl with 1 to 4 carbon atoms and R11 represents alkyl with 1 to 4 carbon atoms any such alkyl group being optionally substituted by a hydroxy, methoxy or furfuryl group and physiologically acceptable acid addition salts thereof. 1. Claims for the Contracting State : AT Process for preparing a 12-amino-pyridazino[4',5':3,4]pyrrolo[2,1-a]isoquinoline of general formula see diagramm : EP0190563,P17,F1 wherein R1 and R2 , which may be identical or different, each represent hydrogen, C3-7 cycloalkyl, C2-5 alkenyl, phenyl (optionally mono- or disubstituted by halogen atoms or methoxy groups), propargyl, a straight-chained or branched, saturated or unsaturated alkyl group with 1 to 5 carbon atoms which may be substituted by hydroxy, alkoxy with 1 to 4 carbon atoms, halogen, NH2 , NH-alkyl with 1 to 2 carbon atoms, N,N-dialkyl with 1 to 2 carbon atoms, NH-acyl with 2 to 4 carbon atoms, cycloalkyl with 3 to 7 carbon atoms, phenyl (optionally substituted by halogen, alkyl with 1 to 2 carbon atoms, alkoxy with 1 to 2 carbon atoms, NH-alkyl with 1 to 2 carbon atoms, N,N-dialkyl with 1 to 2 carbon atoms, NH2 , N-acyl with 2 to 3 carbon atoms), furyl, thienyl, a nitrogen-containing heterocyclic 5- or 6-membered ring which may optionally contain as a further heteroatom an oxygen or sulphur atom (and the ring may optionally be substituted by alkyl with 1 to 4 carbon atoms), or R1 and R2 together with the nitrogen atom represent a 3- to 7-membered ring which may optionally contain as a further heteroatom an oxygen or nitrogen atom [the ring may optionally be substituted by phenyl (C1-4 ) alkyl (this phenyl ring in turn being mono- or disubstituted by halogen atoms or methoxy groups)], or R2 , if R1 represents hydrogen, represents -NH2 , di(C1-2 ) alkylamino, acetonylamino, -NH(C2-3 ) acyl, alkylsulphonyl or alkyloxycarbonyl group with 1 to a carbon atoms in the alkyl chain, a isopropylideneimino group see diagramm : EP0190563,P17,F2 or a heterocyclic 5- or 6-membered ring containing a nitrogen atom and optionally containing as a further heteroatom an oxygen, nitrogen or sulphur atom, R3 , R4 and R5 , which may be identical or different, represent hydrogen or alkyl groups with 1 to 4 carbon atoms, R7 and R8 , which may be identical or different, represent hydroxy, alkoxy with 1 to 4 carbon atoms or alkylthio groups with 1 to 4 carbon atoms, and R6 and R9 , which may be identical or different, represent hydrogen, hydroxy, alkoxy with 1 to 4 carbon atoms or alkylthio groups with 1 to 4 carbon atoms or a group see diagramm : EP0190563,P17,F3 wherein R10 represents hydrogen or alkyl with 1 to 4 carbon atoms and R11 represents alkyl with 1 to 4 carbon atoms any such alkyl group being optionally substituted by a hydroxy, methoxy or furfuryl group or a physiologically acceptable acid addition salt thereof, characterised in that a 3,4-dihydro-12-methyl-mercapto- pyridazino[4',5':3,4]pyrrolo[2,1-a]isoquinoline of general formula II see diagramm : EP0190563,P18,F1 wherein the groups R3 , R4 , R5 , R6 , R7 , R8 and R9 are as hereinbefore defined, is reacted with a compound of general formula III see diagramm : EP0190563,P18,F2 wherein R1 and R2 are as hereinbefore defined, and in that a compound thus obtained is optionally converted, in a manner known per se, into a physiologically acceptable acid addition salt.

73. 发明专利

NO881759A 未知
公开(公告)号：NO881759A
公开(公告)日：1988-10-25
申请号：NO881759
申请日：1988-04-22
申请人： BOEHRINGER INGELHEIM KG
发明人： LOESEL WALTER , ROOS OTTO , SCHNORRENBERG GERD , ARNDST DIETRICH , SPECK GEORG , STRELLER ILSE , KUHN FRANZ JOSEF , SCHINGNITZ GUENTHER
IPC分类号： A61K31/435 , A61K31/47 , A61K31/472 , A61P9/08 , A61P9/10 , C07D217/02 , C07D217/04 , C07D217/14 , C07D217/16 , C07D221/20 , C07D401/12 , C07D405/12 , C07D491/04 , C07D495/04 , C07D519/00 , C07D217/00 , C07D495/00
CPC分类号： C07D221/20 , C07D217/02 , C07D217/04 , C07D217/14 , C07D401/12 , C07D405/12 , C07D491/04 , C07D495/04

74. 发明专利

DD261155A5 未知
公开(公告)号：DD261155A5
公开(公告)日：1988-10-19
申请号：DD28803986
申请日：1986-03-19
申请人： BOEHRINGER INGELHEIM KG
发明人： LOESEL WALTER , ROOS OTTO , SCHNORRENBERG GERD , ARNDTS DIETRICH , HINZEN DIETER , KUHN FRANZ-JOSEF , LEHR ERICH , REICHL RICHARD , STRELLER ILSE , SPECK GEORG
IPC分类号： A61K31/435 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/535 , A61P3/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/28 , C07D333/00 , C07D471/04 , C07D495/14 , C07D217/00 , C07D233/00

75. 发明专利

DD258612A5 未知
公开(公告)号：DD258612A5
公开(公告)日：1988-07-27
申请号：DD29418186
申请日：1986-09-05
申请人： BOEHRINGER INGELHEIM KG
发明人： ROSS OTTO , SCHNORRENBERG GERD , LOESEL WALTER , WIEDEMANN INGRID , GAIDA WOLFRAM , HOEFKE WOLFGANG
IPC分类号： C07K14/81 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07K1/113 , C07K5/06 , C07K5/068 , A61K37/64
摘要： The amino acid derivatives have the general formula in which R is H, acetyl, benzoyl, pivaloyl or the radical P is one of the numbers 1-4; A is a residue of one of the alpha -amino acids or R2 is hydrogen, C1-C4-alkyl, straight-chain or branched, C5-C7-cycloalkyl, it being possible for a phenyl ring to be fused on, phenyl, phenyl-C1-C4-alkyl, a hetero-C1-C4-alkyl radical where the heterocycle consists of a 5- or 6-membered ring with 1-2 of the hetero atoms O, S or N, R3 is hydrogen, C1-C4-alkyl, straight-chain or branched, phenyl, phenyl-C1-C4-alkyl or a hetero-C1-C4-alkyl radical where the heterocycle consists of a 5- or 6-membered ring with 1-2of the hetero atoms O, S or N, or R2 and R3 together form with the N and the C atom a 5-, 6- or 7-membered ring which can be saturated or contain one double bond, or a 4-, 5- or 6-membered ring which contains one or more of the hetero atoms O, S or N; R4 is OH, C1-C4- omega -hydroxyalkyl, C1-C4-alkoxy, phenyl-C1-C4-alkoxy, C1-C4-alkylamino, (C1-C4)2-dialkylamino, one of the groups or an alpha -amino acid which is linked in the manner of a peptide to the CO group of the molecule; R5 is C1-C4-alkyl, C1-C3-alkenyl, C1-C3-alkynyl, straight-chain or branched, hydroxyl, nitro, amino, C1-C4-alkoxy, mercapto, C1-C4- alkylthio, hydroxy-C1-C4-alkyl, mercapto-C1-C4-alkyl, F, Cl, Br, amino-C1-C4-alkyl, sulphonamido, methylenedioxy, fluoro-C1-C4-alkyl, chloro-C1-C4-alkyl, bromo-C1-C4-alkyl, cyano or trifluoromethyl; R6 is hydrogen or methyl; R7 is C1-C4-alkyl, straight-chain or branched, where the alkyl radical can be substituted by F, Cl, Br, CF3, phenyl or pyridyl; X, Y and Z are O, S, NR8, CR9, CHR9, with the proviso that only one of the radicals X, Y and Z can be O, S, and one or two of the radicals X, Y and Z can be NR8; R8 is hydrogen or C1-C4-alkyl, straight-chain or branched; R9 is hydrogen or, together with a vicinal radical R9, a phenyl ring or, for m and n = 1, the dihydro form thereof with double bond in conjugation with the C-terminal carboxyl group and m and n are each 0, 1 or 2, where the total of m and n is 1 or 2. The compounds are strong inhibitors of angiotensin I converting enzyme and are intended for use as hypotensive agents.

76. 发明专利

CS255896B2 PROCESS FOR PREPARING DERIVATIVES OF AMINOACIDS 未知
公开(公告)号：CS255896B2
公开(公告)日：1988-03-15
申请号：CS714185
申请日：1985-10-04
申请人： BOEHRINGER INGELHEIM KG
发明人： ROOS OTTO , SCHNORRENBERG GERD , LOESEL WALTER , WIEDEMANN INGRID , GAIDA WOLFGANG , HOEFKE WOLFGANG
IPC分类号： C07K14/81 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07K1/113 , C07K5/06 , C07K5/068 , C07K5/00 , C07C101/00
摘要： The amino acid derivatives have the general formula in which R is H, acetyl, benzoyl, pivaloyl or the radical P is one of the numbers 1-4; A is a residue of one of the alpha -amino acids or R2 is hydrogen, C1-C4-alkyl, straight-chain or branched, C5-C7-cycloalkyl, it being possible for a phenyl ring to be fused on, phenyl, phenyl-C1-C4-alkyl, a hetero-C1-C4-alkyl radical where the heterocycle consists of a 5- or 6-membered ring with 1-2 of the hetero atoms O, S or N, R3 is hydrogen, C1-C4-alkyl, straight-chain or branched, phenyl, phenyl-C1-C4-alkyl or a hetero-C1-C4-alkyl radical where the heterocycle consists of a 5- or 6-membered ring with 1-2of the hetero atoms O, S or N, or R2 and R3 together form with the N and the C atom a 5-, 6- or 7-membered ring which can be saturated or contain one double bond, or a 4-, 5- or 6-membered ring which contains one or more of the hetero atoms O, S or N; R4 is OH, C1-C4- omega -hydroxyalkyl, C1-C4-alkoxy, phenyl-C1-C4-alkoxy, C1-C4-alkylamino, (C1-C4)2-dialkylamino, one of the groups or an alpha -amino acid which is linked in the manner of a peptide to the CO group of the molecule; R5 is C1-C4-alkyl, C1-C3-alkenyl, C1-C3-alkynyl, straight-chain or branched, hydroxyl, nitro, amino, C1-C4-alkoxy, mercapto, C1-C4- alkylthio, hydroxy-C1-C4-alkyl, mercapto-C1-C4-alkyl, F, Cl, Br, amino-C1-C4-alkyl, sulphonamido, methylenedioxy, fluoro-C1-C4-alkyl, chloro-C1-C4-alkyl, bromo-C1-C4-alkyl, cyano or trifluoromethyl; R6 is hydrogen or methyl; R7 is C1-C4-alkyl, straight-chain or branched, where the alkyl radical can be substituted by F, Cl, Br, CF3, phenyl or pyridyl; X, Y and Z are O, S, NR8, CR9, CHR9, with the proviso that only one of the radicals X, Y and Z can be O, S, and one or two of the radicals X, Y and Z can be NR8; R8 is hydrogen or C1-C4-alkyl, straight-chain or branched; R9 is hydrogen or, together with a vicinal radical R9, a phenyl ring or, for m and n = 1, the dihydro form thereof with double bond in conjugation with the C-terminal carboxyl group and m and n are each 0, 1 or 2, where the total of m and n is 1 or 2. The compounds are strong inhibitors of angiotensin I converting enzyme and are intended for use as hypotensive agents.

77. 发明专利

CS254345B2 METHOD OF AMINO ACIDS' DERIVATIVES PRODUCTION 未知
公开(公告)号：CS254345B2
公开(公告)日：1988-01-15
申请号：CS624285
申请日：1985-09-02
申请人： BOEHRINGER INGELHEIM KG
发明人： ROOS OTTO , LOESEL WALTER , SCHNORRENBERG GERD , WIEDEMANN INGRID , GAIDA WOLFRAM , HOEFKE WOLFGANG
IPC分类号： C07D495/04 , A61K31/401 , A61K31/435 , A61K38/00 , A61K38/05 , A61K38/55 , A61P9/12 , A61P43/00 , C07K1/113 , C07K5/06 , C07K5/062 , C07K14/81 , C07K7/04
摘要： The derivatives have the general formula in which R1 is H, phenyl, benzyl, phenethyl; R2 is H, acetyl, benzoyl, 3-sulphonamido-4-chlorobenzoyl, 3-sulphonamido-4-chloro-6-hydroxybenzoyl, 3-sulphonamido-4-chloro-5-[(furyl)amino]benzoyl, 2,3-dichloro-4-( beta -phenylacryloyl) phenoxyacetyl, pivaloyl, C1-C2-alkylaminocarbonyl, C1-C2-alkylaminothiocarbonyl, acyl or the radical A is the residue of one of the alpha -amino acids or R3 is hydrogen, C1-C4-alkyl, straight-chain or branched, C5-C7-cycloalkyl, it being possible for a phenyl ring to be fused on, phenyl, phenyl-C1-C4-alkyl, a hetero-C1-C4-alkyl radical where the heterocycle consists of a 5- or 6-membered ring with 1-2 of the hetero atoms O, S or N, R4 is hydrogen, C1-C4-alkyl, straight-chain or branched, phenyl, phenyl-C1-C4-alkyl or a hetero-C1-C4-alkyl radical where the heterocycle consists of a 5- or 6-membered ring with 1-2 of the hetero atoms O, S or N, or R3 and R4 together form with the N and the C atom a 5-, 6- or 7-membered ring which can be saturated or contain one double bond, or a 4-, 5- or 6-membered ring which contains one or two more of the hetero atoms O, S or N; R5 is OH, C1-C4- omega -hydroxyalkoxy, C1-C4-alkoxy, phenyl-C1-C4-alkoxy, C1-C4-alkylamino, (C1-C4)2-dialkylamino, one of the groups or an alpha -amino acid which is linked in the manner of a peptide to the CO group of the molecule; R6 is C1-C4-alkyl, C1-C3-alkenyl, C1-C3-alkynyl, straight-chain or branched, hydroxyl, nitro, amino, C1-C4-alkoxy, mercapto, C1-C4- alkylthio, hydroxy-C1-C4-alkyl,mercapto-C1-C4-alkyl, F, Cl, Br, amino-C1-C4-alkyl, sulphonamido, methylenedioxy, fluoro-C1-C4-alkyl, chloro-C1-C4-alkyl, bromo-C1-C4-alkyl, cyano or trifluoromethyl; R7 is hydrogen or methyl; R8 is C1-C4-alkyl, straight-chain or branched, where the alkyl radical can be substituted by F, Cl, Br, CF3, phenyl or pyridyl; X, Y and Z are O, S, CR10, CHR10, with the proviso that only one of the radicals X, Y and Z can be O, S, and one or two radicals X, Y and Z can be NR9; R9 is hydrogen or C1-C4-alkyl, straight-chain or branched; R10 is hydrogen or, together with a vicinal radical R10, a phenyl ring or, for m and n = 1, the dihydro form thereof with the double bond in conjugation with the C-terminal carboxyl group and m and n are each 0, 1 or 2, where the total of m and n is 1 or 2, and are strong inhibitors of angiotensin I converting enzyme and are intended for use as hypotensive agents.

78. 发明专利

NO912230L 未知
公开(公告)号：NO912230L
公开(公告)日：1987-12-28
申请号：NO912230
申请日：1991-06-11
申请人： BOEHRINGER INGELHEIM KG
发明人： LOESEL WALTER , SCHNORRENBERG GERD , ROOS OTTO , ARNDTS DIETRICH , STRELLER ILSE , TRAUNECKER WERNER
IPC分类号： C07D217/00 , C07D217/20 , C07D401/00 , C07D401/04 , C07D405/12 , C07D413/12 , C07D471/00 , C07D471/04 , C07D491/00 , C07D495/00 , C07D495/04

79. 发明专利

NO870408A 未知
公开(公告)号：NO870408A
公开(公告)日：1987-08-04
申请号：NO870408
申请日：1987-02-02
申请人： BOEHRINGER INGELHEIM KG
发明人： LOSEL WALTER , ROOS OTTO , SCHNORRENBERG GERD , ARNDTS DIETRICH , KUHN FRANZ-JOSEF , LEHR ERICH , REICHL RICHARD , SCHINGNITZ GUNTER , SPECK GEORG
IPC分类号： C07D333/00 , A61K31/47 , A61P3/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P43/00 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14 , C07D491/056 , C07D521/00 , C07D405/00 , C07D403/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D405/04 , C07D405/14 , C07D409/14

80. 发明专利

FI863358A 未知
公开(公告)号：FI863358A
公开(公告)日：1987-02-23
申请号：FI863358
申请日：1986-08-20
申请人： BOEHRINGER INGELHEIM KG
发明人： SCHNORRENBERG GERD , ROOS OTTO , LOESEL WALTER , WIEDEMANN INGRID , GAIDA WOLFRAM , HOEFKE WOLFGANG , ARNDTS DIETRICH , STRELLER ILSE
IPC分类号： C07K14/81 , A61K31/198 , A61K31/381 , A61K31/435 , A61K38/00 , A61K38/55 , A61P9/00 , A61P9/12 , A61P43/00 , C07D471/04 , C07D491/048 , C07D495/04 , C07K1/113 , C07K5/02 , C07K5/06 , C07D
摘要： Amino acid derivatives of general formula (I) (the definitions of the various symbols being explained in the specification) are suitable for treating high blood pressure and for cardioprotection. The new compounds are prepared and used in the usual way.

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