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：JPH1059947A

公开(公告)日：1998-03-03

申请号：JP16173897

申请日：1997-06-19

Applicant: HOECHST AG

Inventor： HOLLA WOLFGANG DR ,  BECK GERHARD DR ,  KAMMERMEIER BERNHARD DR ,  KULITZSCHER BERNDT DIPL ING ,  MISCHALOWSKY JUERGEN

IPC: A61K31/415 ,  A61K31/4166 ,  A61P7/02 ,  C07D233/72 ,  C07D233/74 ,  C07D233/76 ,  C07D233/78 ,  C07D233/80

Abstract: PROBLEM TO BE SOLVED: To simply obtain the subject compound useful as an intermediate for producing a pharmaceutically active compound in high optical yield and high chemical yield by resolving a salt of a specific racemic compound with a chiral and non-racemic amino compound. SOLUTION: This chiral and non-racemic compound is represented by formula I (R is H, F, Cl, etc.; R is H, F, a 1-7C alkyl, etc.), e.g. (S)-(4-(4-cyanophenyl)-4- methyl-2,5-dioxoimidazolidin-1-yl)acetic acid. The compound of formula I is obtained by converting a carbonyl compound represented by formula II into hydantoin under conditions of Bucherer reaction, alkylating the hydantoin by using a haloacetic acid ester represented by formula III (R is a 1-6C alkyl or benzyl; X is Cl, Br or I) and further converting the resultant ester to an acid of formula I.

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：DE59307409D1

公开(公告)日：1997-10-30

申请号：DE59307409

申请日：1993-06-28

Applicant: HOECHST AG

Inventor： BECK GERHARD DR ,  JENDRALLA JOACHIM-HEINER DR ,  KESSELER KURT DR

IPC: C07D319/06

公开(公告)号：DE59107442D1

公开(公告)日：1996-04-04

申请号：DE59107442

申请日：1991-04-03

Applicant: HOECHST AG

Inventor： BECK GERHARD DR ,  SCHACHT ULRICH DR ,  KESSELER KURT DR ,  GRANZER ERNOLD DR

IPC: A61K31/35 ,  A61K31/352 ,  A61P3/06 ,  A61P9/10 ,  A61P31/00 ,  C07D211/20 ,  C07D311/30

Abstract: Substituted 3-thia- and 3-oxa-alkylflavones of formula I I wherein R, R1, R2, R3, R4+L, X, m and n have the indicated meanings, a process for the preparation of these compounds and their use as medicaments and pharmaceutical preparations are described. In addition, new intermediates for the preparation of the compounds of formula I are described.

公开(公告)号：ES2082755T3

公开(公告)日：1996-04-01

申请号：ES88710018

申请日：1988-07-07

Applicant: HOECHST AG

Inventor： KESSELER KURT DR ,  BECK GERHARD DR ,  BARTMANN WILHELM PROF DR ,  GRANZER ERNOLD DR

IPC: A61K31/44 ,  A61K31/365 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/505 ,  A61P3/06 ,  A61P9/10 ,  C07D213/55 ,  C07D239/26 ,  C07D405/06 ,  C07D405/14 ,  C07F7/18

Abstract: 3-Desmethylmevalonic acid derivatives of the formula I ( delta -lactone) or II (corresponding dihydroxycarboxylic acid derivative) … … in which A-B, Z, R , R , R and R have the meanings given, are used as medicaments.

公开(公告)号：DK0418648T3

公开(公告)日：1995-06-12

申请号：DK90117043

申请日：1990-09-05

Applicant: HOECHST AG

Inventor： WESS GUENTHER DR ,  JENDRALLA HEINER DR ,  KESSELER KURT DR ,  BECK GERHARD DR

IPC: C07D319/06 ,  A61K31/35 ,  A61K31/357 ,  A61K31/365 ,  A61K31/366 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07C1/24 ,  C07C17/12 ,  C07C17/26 ,  C07C39/08 ,  C07C43/23 ,  C07C45/46 ,  C07C46/04 ,  C07C50/24 ,  C07C69/712 ,  C07C323/20 ,  C07C331/10 ,  C07D309/30

Abstract: Compounds of the formula I and the corresponding open-chain dihydroxy carboxylic acids of the formula II in which X, Y, R , R , R , R , R have the stated meanings, and their pharmacologically acceptable salts with bases and their pharmacologically acceptable esters, process for the preparation of these compounds, their use as drugs, and pharmaceutical preparations are described. Also described are compounds of the formula III in which R , R , R , R , R , X and Y have the stated meanings.

公开(公告)号：AT116979T

公开(公告)日：1995-01-15

申请号：AT90117043

申请日：1990-09-05

Applicant: HOECHST AG

Inventor： JENDRALLA HEINER DR ,  WESS GUENTHER DR ,  KESSELER KURT DR ,  BECK GERHARD DR

IPC: C07D319/06 ,  A61K31/35 ,  A61K31/357 ,  A61K31/365 ,  A61K31/366 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07C1/24 ,  C07C17/12 ,  C07C17/26 ,  C07C39/08 ,  C07C43/23 ,  C07C45/46 ,  C07C46/04 ,  C07C50/24 ,  C07C69/712 ,  C07C323/20 ,  C07C331/10 ,  C07D309/30

Abstract: Compounds of the formula I and the corresponding open-chain dihydroxy carboxylic acids of the formula II in which X, Y, R , R , R , R , R have the stated meanings, and their pharmacologically acceptable salts with bases and their pharmacologically acceptable esters, process for the preparation of these compounds, their use as drugs, and pharmaceutical preparations are described. Also described are compounds of the formula III in which R , R , R , R , R , X and Y have the stated meanings.