公开(公告)号：JPH1072463A

公开(公告)日：1998-03-17

申请号：JP16581597

申请日：1997-06-23

Applicant: HOECHST AG

Inventor： BOGER HANS GEORG ,  HOFFMANN AXEL ,  JAHNE GERHARD ,  SCHAFER HANS-LUDWIG ,  KRASS NORBERT

IPC: A61K31/505 ,  A61P3/06 ,  C07D403/04

Abstract: PROBLEM TO BE SOLVED: To obtain a novel compound which can manifest sufficient antihyperlipemic action with (almost) no cytotoxicity and is useful for treatment of liposis and disorder of lipid metabolism. SOLUTION: This novel compound is represented by formula I [R is H, an (F-substituted) 1-8C alkyl; R is an -O-F-substituted 1-8C alkyl, an -S-F- substituted 1-8C alkyl; R is H, F, Cl, Br, R and R may be incorporated to form an -O-F-substituted 1-5C alkylene-O-] or its acid adduct, typically 4- amino-2-(4,4-dimethylimidazolidin-2-one-1-yl)-5-[N-methly-N-(2-trifluo romethoxy) phenyl]pyrimidine-carboxamide. The compound of formula I is prepared by converting 4-amino-2-(4,4-dimethylimidazolidin-2-one-1-yl)-5-carboxylic acid to its acid chloride followed by reaction of the acid chloride with a compound of formula II.

公开(公告)号：CA2083436C

公开(公告)日：2004-05-11

申请号：CA2083436

申请日：1992-11-20

Applicant: HOECHST AG

Inventor： JAHNE GERHARD

IPC: C07D237/00 ,  C07D239/46 ,  C07D239/47 ,  C07D239/52 ,  C07D239/56 ,  C07D249/00 ,  C07D403/04 ,  C07D403/14 ,  C07D521/00

Abstract: Process for the preparation of 5-substituted cytosines and other 4,5-disubstituted pyrimidin-2(1H)-ones, and intermediates arising in the course of this The process for the preparation of compounds of the formula I, (see formula I) wherein compounds of the formula II (see formula II) are converted into an azole derivative of the formula III or an azine derivative of the formula IV (see formula III) (see formula IV) which can subsequently be converted into a compound of the formula I using a nucleophile XH.

公开(公告)号：AU3545093A

公开(公告)日：1993-09-30

申请号：AU3545093

申请日：1993-03-26

Applicant: HOECHST AG

Inventor： JAHNE GERHARD ,  HELSBERG MATTHIAS ,  WINKLER IRVIN ,  GROSS GERHARD ,  SCHOLL THOMAS

IPC: A61K31/52 ,  A61P31/12 ,  C07D473/00 ,  C07D473/32

Abstract: Compounds of the formula 1 in which the radicals R and/or R independently of one another represent acyl radicals of the formula -C(=O)-R (2> where R denotes C1-C3-alkyl and one of the radicals R and R can also denote hydrogen, and their physiologically tolerable salts have an antiviral action.

公开(公告)号：HUT61716A

公开(公告)日：1993-03-01

申请号：HU240692

申请日：1991-06-27

Applicant: HOECHST AG

Inventor： JAHNE GERHARD

IPC: C07C43/315 ,  C07C217/02 ,  C07C321/02 ,  C07F9/08

Abstract: Prepn. of substd. acyclic nucleosides comprises: (a) reaction of an alcohol of formula (I) to give a formaldehyde acetal cpd. of formula (II); and (b) reaction of (II) with a substd., N-contg. heterocycle (III) to introduce the gp. of formula (A). R1, R3 = H or alkyl, opt. substd. by one or mono halo, N3, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynyl thio, dialkylamino, dialkenylamino, dialkynylamino, benzyloxy, benzylthio, dibenzylamino, phthalimide, P(O)(OR4)(OR5), P(R6)(O)(OR5) OCH2P(O)(OR4)(OR5) or OCH2P(R6)(O)(OR5) gps. R2 = alkyl, benzyl, CH2P(O)(OR4)(OR5) or CH2P(R6)(O)(OR5); R4-R6 = 1-6C alkyl.

公开(公告)号：IE922192A1

公开(公告)日：1993-01-13

申请号：IE922192

申请日：1992-07-03

Applicant: HOECHST AG

Inventor： JAHNE GERHARD ,  WINKLER IRVIN ,  HELSBERG MATTHIAS ,  HANEL HEINZ

IPC: C07D249/00 ,  A61K31/395 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/4425 ,  A61K31/50 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61P31/12 ,  A61P33/02 ,  C07D209/48 ,  C07D213/64 ,  C07D213/68 ,  C07D237/14 ,  C07D239/32 ,  C07D239/38 ,  C07D239/46 ,  C07D239/47 ,  C07D239/54 ,  C07D239/553 ,  C07D403/04 ,  C07D471/04 ,  C07D473/00 ,  C07D473/18 ,  C07D473/30 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04 ,  C07D498/04 ,  C07D521/00 ,  C07F7/10 ,  C07D211/74

Abstract: Compounds of the formulae I and II in which the substituents N, R , R and R and also n have the meanings mentioned, have an antiviral and antiparasitic action.

公开(公告)号：PT98095A

公开(公告)日：1992-06-30

申请号：PT9809591

申请日：1991-06-26

Applicant: HOECHST AG

Inventor： JAHNE GERHARD

IPC: A61K31/435 ,  A61K31/52 ,  A61K31/522 ,  A61P31/12 ,  C07C43/315 ,  C07C323/12 ,  C07D207/30 ,  C07D213/64 ,  C07D213/68 ,  C07D233/60 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D239/54 ,  C07D239/553 ,  C07D239/56 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D471/04 ,  C07D473/00 ,  C07D473/06 ,  C07D473/16 ,  C07D473/18 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04 ,  C07F9/32 ,  C07F9/40 ,  C07H19/00 ,  C07C

Abstract: By using symmetrical formaldehyde acetals of the formula … … the substituent … … can advantageously be introduced into nitrogen-containing heterocyclic systems with the formation of acyclic nucleoside analogues.

公开(公告)号：HU910928D0

公开(公告)日：1991-10-28

申请号：HU92891

申请日：1991-03-20

Applicant: HOECHST AG

Inventor： JAHNE GERHARD ,  ROESNER MANFRED ,  WINKLER IRVIN ,  HELSBERG MATTHIAS ,  SCHOLL THOMAS

IPC: A61K31/52 ,  A61K31/522 ,  A61P31/12 ,  A61P31/22 ,  C07D473/00 ,  C07D473/04 ,  C07D473/16 ,  C07D473/18 ,  C07D473/20 ,  C07D473/22 ,  C07D473/24 ,  C07D473/28 ,  C07D473/32 ,  C07D473/34 ,  C07D473/36 ,  C07D473/40

Abstract: Purine derivs. of formula (I) and their salts are new. R1 = H, halo, NH3, OH, 1-6C alkoxy, -O-CH2Ph, -OPh, SH, 1-6C alkylthio, -S-CH2Ph, -SPh, NH2, 1-6C alkylamino, -NH-CH2Ph, -NH-Ph, 2-12C dialkylamino, -N(CH2Ph)2, cyclic dialkylamino, -N(Ph)2, 1-8C acylamino, 2-16C diacylamino, (N-alkyl-2-pyrrolidin-yliden)amino or 2-10C dialkylaminomethylidenamino; R2 = H, halo, N3, OH, SH, NH2, 1-6C alkylamino, 2-12C dialkylamino, -NH-CH2Ph, -N-(CH2Ph)2, cyclic dialkylamino, -NH-Ph, -N(Ph)2, 1-8C acylamino or thioacylamino, 2-16C diacylamino or di(thioacyl)amino; R3 = H, 1-6C alkyl (opt. substd.) or R8, where R8 is a phosphate ester-contg. gp.; R4 = H, 1-6C alkyl, OH, SH, NH2, halo, N3, 1-6C alkoxy, alkylthio or alkylamino, 2-12C dialkylamino, -O-CH2Ph, -S-CH2Ph, -NH-CH2Ph, -N(CH2Ph)2, -NHPh, -N(Ph)2, -OPh, -SPh, 1-8C acyloxy, 1-8C acylthio, 1-8C acylamino, 2-16C diacylamino, -O-(1-4C alkyl)-P(O)(OR6)(OR7) or -O(1-4C alkyl)-P(1-6C alkyl)(=O)(OR6); R5 = H, 1-6C alkyl (opt. substd.). A number of provisos are given in the specification.

公开(公告)号：CA2038589A1

公开(公告)日：1991-09-21

申请号：CA2038589

申请日：1991-03-19

Applicant: HOECHST AG

Inventor： JAHNE GERHARD ,  ROESNER MANFRED ,  WINKLER IRVIN ,  HELSBERG MATTHIAS ,  SCHOLL THOMAS

IPC: A61K31/52 ,  A61K31/522 ,  A61P31/12 ,  A61P31/22 ,  C07D473/00 ,  C07D473/04 ,  C07D473/16 ,  C07D473/18 ,  C07D473/20 ,  C07D473/22 ,  C07D473/24 ,  C07D473/28 ,  C07D473/32 ,  C07D473/34 ,  C07D473/36 ,  C07D473/40 ,  C07F9/547 ,  A61K31/675

Abstract: 1 HOE 90/F 093 of the disclosure: Substituted purines, processes for their preparation and their use as antiviral agents Compounds of the formula I (I) in which the substituents R1 to R5 have the said meanings, have antiviral activity.

公开(公告)号：PT563814E

公开(公告)日：2000-05-31

申请号：PT93105011

申请日：1993-03-26

Applicant: HOECHST AG

Inventor： WINKLER IRVIN ,  HELSBERG MATTHIAS ,  SCHOLL THOMAS ,  JAHNE GERHARD ,  GROSS GERHARD

IPC: A61K31/52 ,  A61P31/12 ,  C07D473/00 ,  C07D473/32

Abstract: Compounds of the formula 1 in which the radicals R and/or R independently of one another represent acyl radicals of the formula -C(=O)-R (2> where R denotes C1-C3-alkyl and one of the radicals R and R can also denote hydrogen, and their physiologically tolerable salts have an antiviral action.

公开(公告)号：ES2111297T3

公开(公告)日：1998-03-01

申请号：ES94912542

申请日：1994-03-24

Applicant: HOECHST AG

Inventor： JAHNE GERHARD ,  HELSBERG MATTHIAS ,  WINKLER IRVIN ,  GROSS GERHARD ,  SCHOLL THOMAS

IPC: A61K31/52 ,  A61P31/12 ,  C07D473/32