公开(公告)号：JPH1059948A

公开(公告)日：1998-03-03

申请号：JP14561797

申请日：1997-06-03

Applicant: HOECHST AG

Inventor： STILZ HANS ULRICH DR ,  BECK GERHARD DR ,  RADAU MANFRED DR

IPC: C07D233/78 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4164 ,  A61K31/4166 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/14 ,  A61P35/00 ,  A61P35/04 ,  C07D233/72 ,  C07D233/74 ,  C07D233/76

Abstract: PROBLEM TO BE SOLVED: To obtain the subject compound useful as a medicine in a non- hygroscopic form by including a specific ethyl ester and maleic acid in a form of a salt. SOLUTION: This 3-(2-(4-(4-(amino-imino-methyl)-phenyl)-4-methyl-2,5-dioxo- imidazolidin-1-yl)-acetylamino)-3-phenyl-propionic acid ethyl ester salt is represented by formula I (HB is maleic acid). The salt is obtained by carrying out anion exchange between maleic acid and a maleic acid salt by using a compound of formula II (HV is an arbitrary inorganic or organic acid different from maleic acid). The compound of formula I is useful as a platelet aggregation inhibitor, a medicine for preventing thrombosis, an inhibitor of metastasis of cancer cell and a medicine for treating and preventing coronary vessel-based or cerebral blood vessel-based diseases.

公开(公告)号：CZ20798A3

公开(公告)日：1998-08-12

申请号：CZ20798

申请日：1998-01-22

Applicant: HOECHST AG

Inventor： AHRENS GERHARD DR ,  MENTRUP EDGAR DR ,  MAAS JOCHEN DR ,  RADAU MANFRED DR

IPC: A61K9/20 ,  A61K9/00 ,  A61K31/47 ,  A61K31/496 ,  A61K31/5383 ,  A61K47/12 ,  A61P31/04

Abstract: Preparation of orally applicable, fast release pharmaceutical preparations (I) of quinolone antibiotics with masked flavour comprises mixing the quinolone derivative with at least one higher fatty acid and heating to 30-140 degrees C. Also claimed are the preparations prepared.

公开(公告)号：CZ9800207A3

公开(公告)日：1998-08-12

申请号：CZ20798

申请日：1998-01-22

Applicant: HOECHST AG

Inventor： AHRENS GERHARD DR ,  MENTRUP EDGAR DR ,  MAAS JOCHEN DR ,  RADAU MANFRED DR

IPC: A61K9/20 ,  A61K9/00 ,  A61K31/47 ,  A61K31/496 ,  A61K31/5383 ,  A61K47/12 ,  A61P31/04

CPC classification number: A61K9/0095 ,  A61K31/496 ,  A61K31/5383 ,  A61K47/12

公开(公告)号：AT74513T

公开(公告)日：1992-04-15

申请号：AT88119014

申请日：1988-11-15

Applicant: HOECHST AG

Inventor： FUELBERTH WERNER DR ,  LEEB RICHARD DR ,  RADAU MANFRED DR ,  STAMMBERGER WILLI DR

IPC: A61K38/00 ,  A61K9/16 ,  A61K9/20 ,  A61K9/36 ,  A61K9/50 ,  A61K38/04 ,  A61K38/55 ,  A61K47/02 ,  A61K47/30 ,  A61K47/38 ,  A61P9/12 ,  A61P43/00 ,  C07K1/00 ,  C07K5/06 ,  C07K5/062 ,  C07K14/81 ,  C08G59/40 ,  A61K37/02

公开(公告)号：CZ292672B6

公开(公告)日：2003-11-12

申请号：CZ172997

申请日：1997-06-04

Applicant: HOECHST AG

Inventor： STILZ HANS ULRICH DR ,  BECK GERHARD DR ,  RADAU MANFRED DR

IPC: C07D233/78 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4164 ,  A61K31/4166 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/14 ,  A61P35/00 ,  A61P35/04 ,  C07D233/72 ,  C07D233/74 ,  C07D233/76

Abstract: The present invention relates to a hydrogen maleate of 3-(2-(4-(4-(aminoiminomethyl)phenyl)-4-methyl-2,5-dioxoimidazolidin-1-yl)acetylamino)-3-phenylpropionic acid ethyl ester of the general formula I, in which HB represents maleic acid, as well as physiologically acceptable salts thereof, processes of their preparation, their use in medicaments and pharmaceutical preparations in which these compounds are comprised.

公开(公告)号：DE3739690A1

公开(公告)日：1989-06-08

申请号：DE3739690

申请日：1987-11-24

Applicant: HOECHST AG

Inventor： FUELBERTH WERNER DR ,  LEEB RICHARD DR ,  RADAU MANFRED DR ,  STAMMBERGER WILLI DR

IPC: A61K38/00 ,  A61K9/16 ,  A61K9/20 ,  A61K9/36 ,  A61K9/50 ,  A61K38/04 ,  A61K38/55 ,  A61K47/02 ,  A61K47/30 ,  A61K47/38 ,  A61P9/12 ,  A61P43/00 ,  C07K1/00 ,  C07K5/06 ,  C07K5/062 ,  C07K14/81 ,  C08G59/40

Abstract: Stabilised compounds of the formula I in which R, R , R , R , R and R have the stated meanings, and process for the preparation thereof are described. The stabilised compounds are suitable for the production of pharmaceutical preparations.

公开(公告)号：CZ9701729A3

公开(公告)日：1997-12-17

申请号：CZ172997

申请日：1997-06-04

Applicant: HOECHST AG

Inventor： STILZ HANS ULRICH DR ,  BECK GERHARD DR ,  RADAU MANFRED DR

IPC: C07D233/78 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4164 ,  A61K31/4166 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/14 ,  A61P35/00 ,  A61P35/04 ,  C07D233/72 ,  C07D233/74 ,  C07D233/76 ,  A61K31/395

CPC classification number: C07D233/76

公开(公告)号：CZ172997A3

公开(公告)日：1997-12-17

申请号：CZ172997

申请日：1997-06-04

Applicant: HOECHST AG

Inventor： STILZ HANS ULRICH DR ,  BECK GERHARD DR ,  RADAU MANFRED DR

IPC: C07D233/78 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4164 ,  A61K31/4166 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/14 ,  A61P35/00 ,  A61P35/04 ,  C07D233/72 ,  C07D233/74 ,  C07D233/76 ,  A61K31/395

Abstract: Ethyl 3-(2-(4-(4-(aminoiminomethyl)phenyl)-4-methyl-2,5-dioxoimidazolidin-1- yl)acetylamino)-3-phenylpropionate hydrogen maleate of formula (I) is new. HB = maleic acid. All stereoisomers and their mixtures and salts are included.

公开(公告)号：DE19622489A1

公开(公告)日：1997-12-11

申请号：DE19622489

申请日：1996-06-05

Applicant: HOECHST AG

Inventor： STILZ HANS ULRICH DR ,  BECK GERHARD DR ,  RADAU MANFRED DR

IPC: C07D233/78 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4164 ,  A61K31/4166 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/14 ,  A61P35/00 ,  A61P35/04 ,  C07D233/72 ,  C07D233/74 ,  C07D233/76 ,  C07C57/145

Abstract: Ethyl 3-(2-(4-(4-(aminoiminomethyl)phenyl)-4-methyl-2,5-dioxoimidazolidin-1- yl)acetylamino)-3-phenylpropionate hydrogen maleate of formula (I) is new. HB = maleic acid. All stereoisomers and their mixtures and salts are included.

公开(公告)号：DE3869919D1

公开(公告)日：1992-05-14

申请号：DE3869919

申请日：1988-11-15

Applicant: HOECHST AG

Inventor： FUELBERTH WERNER DR ,  LEEB RICHARD DR ,  RADAU MANFRED DR ,  STAMMBERGER WILLI DR

IPC: A61K38/00 ,  A61K9/16 ,  A61K9/20 ,  A61K9/36 ,  A61K9/50 ,  A61K38/04 ,  A61K38/55 ,  A61K47/02 ,  A61K47/30 ,  A61K47/38 ,  A61P9/12 ,  A61P43/00 ,  C07K1/00 ,  C07K5/06 ,  C07K5/062 ,  C07K14/81 ,  C08G59/40 ,  A61K37/02

Abstract: N-aminocarbonylmethyl -alpha-amino acid derivs. of formula (I) or their physiologically acceptable salts are stabilised (a) by a protective polymeric coating and/or (b) by addn. of an acceptable buffer which, in a pharmaceutical compsn. in presence of moisture, provides a weakly acidic to weakly basic pH. R is H, 1-4C alkyl or phenyl, R1 is 1-4C alkyl or -(CH2)m-NAB, m is 1-4, A and B are H or 1-4C alkyl, R2 is H, 1-4C alkyl or benzyl, R3 is H or 1-4C alkyl, R4 and R5 together complete a heterocyclic, mono- bi- or tri-cyclic ring system, hydrogenated or partly hydrogenated, contg. one N and 4-15 ring C and opt. substd. by 1 or 2 1-4C alkoxy. (I) is ramipril (Ia, 2-(N-((S)-1-ethoxycarbonyl -3-phenylpropyl-L-alanyl (15,35,55)-2-azabicyclo (3,3,0) octane-3-carboxylic acid).