Mannkind Corporation

Egyt Gyogyszervegyeszeti Gyar

Egis Gyogyszergyar

Fosun Orinove Pharmatech, Inc.

Basfaktiengesellschaft

Gyogyszerkutato Intezet Kft.

Shanghai Fosun Pharmaceutical Industrial Development Co. Ltd.

Zoltan Zubovics

Warren Stanfield Wade

Qingping Zeng

John Bruce Patterson

Andras Toro

Yun Yang

Zhipeng Wu

Lajos Toldy

Gabor Kovacs

Imre Moravcsik

Antal Simay

Kalman Nagy

Inge Schafer

Gyorgy Krasznai

Ferenc Szederkenyi

Lajos Toldi

Mariann Kurti

Gabor Feher

Eva Kovacs Nee Bozo

Gyorgyi Vereczkey Nee Donath

Ferenc Andrasi

Istvan Elekes

Sandor Elek

Katalin Goldschmidt

Gyorgy Rabloczky

Andras Varro

Laszlo Sebestyen

Zsuzsanna Fittler

Istvan Sziraki

Valeria Vitkoczi

Eszter Hodula

Klara Sutka

Ferene Andrasi

Jozsef Gyimesi

Katalin Szilagyi

Katalin Gorgenyi

Compounds which directly inhibit IRE-1&#x3b1; activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.

IRE-1&#x3b1; inhibitors

Compounds which directly inhibit IRE-1&#x3b1; activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.

This invention relates to novel compounds of the general formula (I) and the pharmaceutically acceptable acid addition salts thereof. In the general formula (I) ##STR1## wherein Lip, A.sup.1, A.sup.2, Het and n are defined as in the specification. The compounds of the general formula (I) inhibit the lipid peroxidation and therefore, they are useful for the treatment or prevention of diseases and conditions wherein the inhibition of lipid peroxidation is desirable.

Piperazine and homopiperazine derivatives, pharmaceutical compositions

The invention relates to an improved process for the preparation of 2,2-dimethyl-5-(2,5-dimethylphenoxy)-pentanoic acid of Formula (I) ##STR1## which comprises reacting an ester of the general Formula (X) ##STR2## wherein X represents halogen and Z stands for a straight or branched chain C.sub.1-8 alkylene group optionally substituted by one or two 2,2-dimethyl-5-halopentanoyloxy group(s), wherein halo represents chlorine or bromine, and in which alkylene group one or two methylene group(s) may be optionally replaced either by hetero atom(s) or by a bivalent heterocyclic group--with an alkali salt of 2,5-dimethylphenol of Formula (II) ##STR3## or with an ester of the latter formed with a lower alkanoic acid, and hydrolizing the aryloxy-substituted ester of the general Formula (XI) thus obtained. ##STR4## Furthermore the invention relates to intermediate compounds of the general Formula (X), wherein X and Z are as stated above, and to a process for the preparation thereof.

Process for the preparation of

The invention relates to an improved process for the preparation of 2,2-dimethyl-5-(2,5-dimethylphenoxy)-pentanoic acid of Formula (I) ##STR1## which comprises reacting an ester of the general Formula (X) ##STR2## wherein X represents halogen and Z stands for a straight or branched chain C.sub.1-8 alkylene group optionally substituted by one or two 2,2-dimethyl-5-halopentanoyloxy group(s), wherein halo represents chlorine or bromine, and in which alkylene group one or two methylene group(s) may be optionally replaced either by hetero atom(s) or by a bivalent heterocyclic group--with an alkali salt of 2,5-dimethylphenol of Formula (II) ##STR3## or with an ester of the latter formed with a lower alkanoic acid, and hydrolizing the aryloxy-substituted ester of the general Formula (XI) thus obtained. Furthermore the invention relates to intermediate compounds of the general Formula (X), wherein X and Z are as stated above, and to a process for the preparation thereof.

The invention is directed to 1-(2,6-Dimethyl-Phenyl-amino)-2-Dimethyl-amino-Propane and the pharmaceutical composition thereof useful for the treatment of cardiac rhythm disorders.

New alkylene diamine derivatives

A compound of the general formula (I), ##STR1## is described wherein R.sup.1 and R.sup.5 each represent a phenyl group optionally substituted with 1 to 3 lower alkoxy, halo, lower alkyl, monohalo-(lower)-alkyl, dihalo-(lower)-alkyl and/or trihalo-(lower)-alkyl groups, R.sup.2 stands for hydrogen or a lower alkyl group optionally substituted with a hydroxy group or 1 to 3 halogen atoms, R.sup.3 and R.sup.4 each represent a hydrogen atom or a lower alkyl group, and R.sup.6 stands for a carbamoyl, thiocarbamoyl or amidino group having optionally one or two lower alkyl and/or lower alkoxycarbonyl substitutes, or a group of the general formula R.sup.7 -CO-wherein R.sup.7 stands for a lower analkoxy group, an aryloxy group, or an aralkoxy group, and n is equal to 0, provided that when R.sup.1 and R.sup.5 each represent a phenyl group, R.sup.2 and R.sup.3 may not stand for hydrogen or a pharmaceutically acceptable acid addition salt, a pure isomer or an isomeric mixture thereof. The compounds posses antiphlogistic and diuretic activity.

1,3-Diaryl-2-imino-imidazolidines and compounds

The invention relates to new compounds of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.5 each represent a phenyl group, optionally substituted,

1,3-Diaryl-2-imino-imidazolidines and compositions thereof

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Budapest, Hungary

Zoltan Zubovics