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公开(公告)号:AT47838T
公开(公告)日:1989-11-15
申请号:AT85103730
申请日:1982-12-24
Applicant: HOECHST AG
Inventor: URBACH HANSJOERG DR , HENNING RAINER DR , TEETZ VOLKER DR , GEIGER ROLF PROF DR , BECKER REINHARD DR , GAUL HOLGER
IPC: A61K31/40 , C07D209/42 , C07D209/52
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公开(公告)号:DE3072064D1
公开(公告)日:1988-02-11
申请号:DE3072064
申请日:1980-09-13
Applicant: HOECHST AG
Inventor: GEIGER ROLF PROF DR , TEETZ VOLKER DR , SCHOLKENS BERNWARD DR , WISSMANN HANS DR
IPC: A61K31/40 , A61K31/405 , A61K31/45 , A61K31/47 , A61K31/472 , A61P9/12 , C07D209/42 , C07D215/48 , C07D217/26 , C07D339/04 , C07D401/12 , C07D409/06 , C07K5/06
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公开(公告)号:DE3532036A1
公开(公告)日:1987-03-26
申请号:DE3532036
申请日:1985-09-09
Applicant: HOECHST AG
Inventor: BECKER REINHARD DR , GEIGER ROLF PROF DR , HENNING RAINER DR , TEETZ VOLKER DR , URBACH HANSJOERG DR
IPC: A61K45/06 , A61K31/40 , A61K31/635 , A61K38/00 , A61K38/55 , A61P7/10 , A61P9/12 , A61P43/00 , A61K31/19 , A61K31/34
Abstract: The preparation contains an angiotensin converting enzyme inhibitor and a loop diuretic.
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公开(公告)号:DE3275293D1
公开(公告)日:1987-03-05
申请号:DE3275293
申请日:1982-12-24
Applicant: HOECHST AG
Inventor: URBACH HANSJORG DR , HENNING RAINER DR , TEETZ VOLKER DR , GEIGER ROLF PROF DR , BECKER REINHARD DR , GAUL HOLGER
IPC: A61K38/55 , A61K31/40 , A61K31/403 , A61K31/404 , A61K38/00 , A61P7/10 , A61P9/08 , A61P9/12 , C07D209/02 , C07D209/08 , C07D209/32 , C07D209/34 , C07D209/42 , C07D209/52 , C07D215/22 , C07D215/227 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06
Abstract: 1. Claims for the Contracting states ; BE, CH, DE, FR, GB, IT, Li, Lu, NL, SE A compound of the formula I see diagramm : EP0084164,P21,F7 in which the hydrogen atoms on the bridgehead C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2, R1 denotes methyl, R2 denotes hydrogen, (C1 -C4 )-alkyl or benzyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes phenyl, and its physiologically acceptable salts. 1. Claims for the Contracting state : Austria A process for the preparation of the compounds of the formula I see diagramm : EP0084164,P24,F4 in which the hydrogen atoms on the bridgehead C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2, R1 denotes methyl, R2 denotes hydrogen, (C1 -C4 )-alkyl or benzyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes phenyl, and its physiologically acceptable salts, which a) comprises reacting a compound of the formula II see diagramm : EP0084164,P24,F6 wherein R1 , R2 , X, Y and Z have the meanings as in formula I, with a compound of the formula III see diagramm : EP0084164,P25,F1 in which the H atoms on the C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2 and W denotes a radical which can be cleaved off by hydrogenolysis or by acid, and subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl groups, or b) for the preparation of compounds of the formula I, in which Y and Z together denote oxygen, comprises b1 ) reacting a compound of the formula IV see diagramm : EP0084164,P25,F3 in which the H atoms on the C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n and R1 have the meanings as in formula I and W has the meaning as in formula III, with a compound of the formula V, R2 O2 C-CH = CH-CO-X wherein R2 and X have the meanings as in formula I, and subsequently splitting off the radical W and, if appropriate, also the radical R2 to form the free carboxyl groups, or, b2 ) reacting a compound of the formula IV mentioned under b1 ) with a compound of the general formula VI, wherein R2 has the meaning as in formula I, and with a compound of the general formula VII OHC-CO2 R2 X-CO-CH3 wherein X has the meaning as in formula I, subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl group, or c) for the preparation of compounds of the formula I, in which Y and Z each denote hydrogen, comprises c1 ) reacting a compound of the formula IV mentioned under b1 ) with a compound of the formula VIII see diagramm : EP0084164,P25,F2 wherein R2 and X have the meanings as in formula I, reducing the Schiff's bases obtained and subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl groups, or c2 ) catalytically reducing a compound of the formula I in which Y and Z together denote oxygen, with hydrogen, or d) for the preparation of compounds of the formula I, in which Y denotes hydroxyl and Z denotes hydrogen, comprises reducing a compound of the formula I, in which Y and Z together denote oxygen, catalytically with hydrogen or with a reducing agent, such as sodium borohydride, and, if appropriate, converting the compounds obtained according to (a)-(d) into their physiologically acceptable salts.
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公开(公告)号:AT25244T
公开(公告)日:1987-02-15
申请号:AT82112007
申请日:1982-12-24
Applicant: HOECHST AG
Inventor: URBACH HANSJOERG DR , HENNING RAINER DR , TEETZ VOLKER DR , GEIGER ROLF PROF DR , BECKER REINHARD DR , GAUL HOLGER
IPC: A61K38/00 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/52 , C07D215/22 , C07D215/227 , C07K5/02 , A61K31/40
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公开(公告)号:DE3364838D1
公开(公告)日:1986-09-04
申请号:DE3364838
申请日:1983-03-10
Applicant: HOECHST AG
Inventor: OBERMEIER RAINER DR , GEIGER ROLF PROF DR , GRAU ULRICH DR
Abstract: The invention relates to a process for the preparation of insulins from analogs of preproinsulins, which comprises reacting preproinsulin analogs, at a pH below the isoelectric point of the insulins in the presence of trypsin or a trypsin-like endopeptidase, with an ester of natural amino acids or their derivatives and then cleaving off the ester group and other protective groups which may optionally be present.
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公开(公告)号:DE3421614A1
公开(公告)日:1985-12-12
申请号:DE3421614
申请日:1984-06-09
Applicant: HOECHST AG
Inventor: KOENIG WOLFGANG DR , GEIGER ROLF PROF DR , OBERMEIER RAINER DR , MUELLNER HUBERT DR
Abstract: The invention relates to a process for the preparation of peptides of the general formula Arg-Lys-S-Val-Y in which S denotes glutamic acid or alpha -aminoadipic acid and Y denotes tyrosine or tryptophan or esters or amides thereof, which comprises subjecting tetrapeptides of the formula Z-Arg(Z'2)-Lys(Z')-S-(Bzl)-Val-OH in which Z' represents a protective group of the benzyl type, to a condensation reaction with corresponding tyrosine esters or amides or tryptophan esters or amides and removing the protective groups by hydrogenation. The invention furthermore relates to tetrapeptides as intermediate products of this process.
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公开(公告)号:GR78608B
公开(公告)日:1984-09-27
申请号:GR830171779
申请日:1983-06-28
Applicant: HOECHST AG
Inventor: KONIG WOLFGANG DR , GEIGER ROLF PROF DR , OBERMEIER RAINER DR , MULLNER HUBERT DR
IPC: C07K14/52 , A61K38/00 , A61K38/21 , A61K39/39 , A61P35/00 , A61P37/00 , C07K7/06 , C07K14/555 , C07K14/565
Abstract: The invention provides a nonapeptide of the formula I Glu-Asp-Ser-Ser-Ser-Thr-Gly-Trp-Asn-OH (I) a process for the preparation thereof and its use, furthermore intermediates for preparing a compound of the formula I.
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公开(公告)号:GR78453B
公开(公告)日:1984-09-27
申请号:GR830170765
申请日:1983-03-11
Applicant: HOECHST AG
Inventor: OBERMEIER RAINER DR , GEIGER ROLF PROF DR , GRAU ULRICH DR
Abstract: The invention relates to a process for the preparation of insulins from analogs of preproinsulins, which comprises reacting preproinsulin analogs, at a pH below the isoelectric point of the insulins in the presence of trypsin or a trypsin-like endopeptidase, with an ester of natural amino acids or their derivatives and then cleaving off the ester group and other protective groups which may optionally be present.
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公开(公告)号:GR77381B
公开(公告)日:1984-09-11
申请号:GR820169702
申请日:1982-11-03
Applicant: HOECHST AG
Inventor: TEETZ YOLKER DR , GEIGER ROLF PROF DR , URBACH HANSIORG DR , BECKER REINHARD DR , SCHOLKERS BERNWARD DR
IPC: C07C227/08 , A61K31/40 , A61K31/403 , A61K38/00 , A61P9/12 , C07C227/10 , C07C227/16 , C07C229/28 , C07C229/36 , C07C237/06 , C07D209/52 , C07D451/04 , C07K5/02 , C07K5/06
Abstract: Compounds of the formula I (I) in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring alpha -aminoacid, which may be protected, R2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
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