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1. 发明申请

WO8806160A3 AMINO ACID DERIVATIVES,PROCESS FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：氨基酸衍生物及其生产和药物化合物的方法
公开(公告)号：WO8806160A3
公开(公告)日：1988-10-06
申请号：PCT/EP8800120
申请日：1988-02-19
申请人： BOEHRINGER INGELHEIM KG , ROOS OTTO , LOESEL WALTER , SCHNORRENBERG GERD , GAIDA WOLFRAM , HOEFKE WOLFGANG , WIEDEMANN INGRID , ARNDTS DIETRICH , SPECK GEORG
发明人： ROOS OTTO , LOESEL WALTER , SCHNORRENBERG GERD , GAIDA WOLFRAM , HOEFKE WOLFGANG , WIEDEMANN INGRID , ARNDTS DIETRICH , SPECK GEORG
IPC分类号： A61K38/00 , C07K5/06 , A61K37/02
CPC分类号： C07K5/06086 , A61K38/00 , C07K5/06026
摘要： New amino acid derivatives having general formula (I) and their salts, in which A represents the remainder of a bi-cyclic alpha-amino acid with the formula (a), (b), (c), (d), (e), (f), (g), (h), (i) or (j). The new compounds prove effective in lowering-blood pressure and in protecting the heart and brain.

2. 发明专利

PH24246A NEW 1-ARYLOXY-DIHYDROBENZOTHIADIAZINYLALKYLAMINO-ALKANES,PHARMACEUTICAL COMPOSITIONS CONTAINING SAME AND METHOD OF USE THEREOF 未知
公开(公告)号：PH24246A
公开(公告)日：1990-05-04
申请号：PH35852
申请日：1987-09-25
申请人： BOEHRINGER INGELHEIM KG
发明人： KOPPE HERBERT , ESSER FRANZ , GAIDA WOLFRAM , SPECK GEORG , HOEFKE WOLFGANG
IPC分类号： A61K31/54 , A61K31/5415 , A61P9/12 , C07D285/24 , C07D285/26 , C07D285/30 , C07D417/12
摘要： Compounds of the formula … … (the meaning of the symbols is explained in the description) can be prepared by processes known per se and are used as medicaments.

3. 发明专利

NO873996A 未知
公开(公告)号：NO873996A
公开(公告)日：1988-03-28
申请号：NO873996
申请日：1987-09-24
申请人： BOEHRINGER INGELHEIM KG
发明人： KOPPE HERBERT , ESSER FRANZ , GAIDA WOLFRAM , HOEFKE WOLFGANG , SPECK GEORG
IPC分类号： A61K31/54 , A61K31/5415 , A61P9/12 , C07D285/24 , C07D285/26 , C07D285/30 , C07D417/12 , C07D285/00
CPC分类号： C07D417/12 , C07D285/24 , C07D285/30

4. 发明专利

FI874172A0 未知
公开(公告)号：FI874172A0
公开(公告)日：1987-09-24
申请号：FI874172
申请日：1987-09-24
申请人： BOEHRINGER INGELHEIM KG
发明人： KOEPPE HERBERT , ESSER FRANZ , GAIDA WOLFRAM , HOEFKE WOLFGANG , SPECK GEORG
IPC分类号： A61K31/54 , A61K31/5415 , A61P9/12 , C07D285/24 , C07D285/26 , C07D285/30 , C07D417/12 , C07D
摘要： Compounds of the formula … … (the meaning of the symbols is explained in the description) can be prepared by processes known per se and are used as medicaments.

5. 发明专利

HU191637B PROCESS FOR PRODUCING PIPERIDINE DERIVATIVES 未知
公开(公告)号：HU191637B
公开(公告)日：1987-03-30
申请号：HU330783
申请日：1983-09-23
申请人： BOEHRINGER INGELHEIM KG
发明人： MENTRUP ANTON , RENTH ERNST-OTTO , SCHROMM KURT , HOEFKE WOLFGANG , GAIDA WOLFRAM
IPC分类号： C07D239/95 , A61K31/505 , A61K31/517 , A61P9/08 , A61P9/12 , A61P25/02 , C07D263/44 , C07D401/14 , C07D413/04 , C07D413/14 , C07D491/056 , C07D413/12 , A61K31/445
摘要： Compounds of the formula wherein R1 and R2, which may be identical to or different from each other, are each independently hydrogen, straight or branched alkyl of 1 to 8 carbon atoms or arylmethyl; or R1 and R2, together with each other, are -(CH2)4 or -(CH2)5-; and R3 and R4, which may be identical to or different from each other, are each independently hydrogen, straight or branched alkyl of 1 to 4 carbon atoms or arylmethyl; or R3 and R4, together with each other, are -CH3- or -CH2-CH2-; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful for the treatment of cardiovascular diseases, especially hypertension.

6. 发明专利

DD238981A5 未知
公开(公告)号：DD238981A5
公开(公告)日：1986-09-10
申请号：DD28141585
申请日：1985-10-03
申请人： BOEHRINGER INGELHEIM KG
发明人： ROOS 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
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.

7. 发明专利

HUT39192A PROCESS FOR PREPARING AMINO ACID-DERIVATIVES 未知
公开(公告)号：HUT39192A
公开(公告)日：1986-08-28
申请号：HU385485
申请日：1985-10-04
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： C07K14/81 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07K1/113 , C07K5/06 , C07K5/068 , A61K37/02
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.

8. 发明专利

DK454185D0 未知
公开(公告)号：DK454185D0
公开(公告)日：1985-10-04
申请号：DK454185
申请日：1985-10-04
申请人： BOEHRINGER INGELHEIM KG
发明人： ROOS 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 , C07K
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.

9. 发明专利

NO851029L 未知
公开(公告)号：NO851029L
公开(公告)日：1985-09-17
申请号：NO851029
申请日：1985-03-15
申请人： BOEHRINGER INGELHEIM KG
发明人： ABELE WOLFGANG , KOEPPE HERBERT , ESSER FRANZ , GAIDA WOLFRAM , HOEFKE WOLFGANG , STRELLER ILSE , REICHL RICHARD , TRAUNECKER WERNER
IPC分类号： A61K31/335 , A61K31/35 , A61K31/352 , A61K31/357 , A61K31/36 , A61P3/00 , A61P3/14 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D311/76 , C07D313/08 , C07D317/00 , C07D405/12 , C07D407/12 , C07D
摘要： Isochromans and oxepines of the formula (I) in which R denotes a hydrogen atom or a straight or branched alkyl group having up to 4 C atoms, R denotes a hydrogen atom or a straight or branched alkyl group having up to 4 C atoms or, together with R , denotes an alkylene group having 3 to 5 C atoms, R denotes a hydrogen atom or a straight or branched alkyl group having up to 4 C atoms, R denotes a hydrogen atom or a straight or branched alkyl group having up to 4 C atoms, R denotes a hydrogen atom or a straight or branched alkyl group having 1 to 6 C atoms or a pyridinyl group, R denotes a hydrogen atom, a fluorine, chlorine or bromine atom, a straight or branched alkyl group having 1 to 6 C atoms, a hydroxyl or alkoxy group having 1 to 4 C atoms or a trifluoromethyl group, R denotes a hydrogen atom, a fluorine, chlorine or bromine atom, a straight or branched alkyl group having 1 to 6 C atoms, a hydroxyl or alkoxy group having 1 to 4 C atoms or, together with R , denotes a methylenedioxy group, R denotes a hydrogen atom, or a hydroxyl or alkoxy group having 1 to 4 C atoms, m denotes the numbers 1 or 2 and n denotes the numbers 1, 2 or 3, and their acid addition salts. The compounds have calcium antagonist and antihypertensive activity.

10. 发明专利

FI853354A0 未知
公开(公告)号：FI853354A0
公开(公告)日：1985-09-02
申请号：FI853354
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 , C07K
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.

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