Bayer Aktiengesellschaft

Chinese Academy of Medical Sciences

Other

Bayer Corporation

The Wistar Institute

Bayer Healthcare LLC

Bayer Aktiengesellschaft & Chinese

Wolfgang Hartwig

Rudolf Schohe-Loop

Bodo Junge

Zhan Gao

Heinrich Meier

Bernard Schmidt

Teunis Schuurman

Maarten De Jonge

Dieter Habich

Thanos D Halazonetis

Karl G Metzger

Hans-Joachim Zeiler

Ulrich Niewohner

Elisabeth Perzborn

Rainer Endermann

Erwin Bischoff

Matthias Schramm

Gunter Schmidt

Ingo Haller

Wilfried Schrock

Fred R Heiker

Helmuth Schutz

The present invention provides peptides and peptidomimetics corresponding to part or to the entirety of the region encompassed by residues 360-386 of human p53, said peptides and peptidomimetics characterized by the ability to activate DNA binding of wild-type p53 and of select tumor-derived p53 mutants. Pharmaceutical compositions of the compounds of the invention and methods of using these compositions therapeutically are also provided.

Peptides and peptidomimetics with structural similarity to human p53 that activate p53 function

The present invention provides peptides and peptidomimetics corresponding to part or to the entirety of the region encompassed by residues 360&#x2013;386 of human p53, said peptides and peptidomimetics characterized by the ability to activate DNA binding of wild-type p53 and of select tumor-derived p53 mutants. Pharmaceutical compositions of the compounds of the invention and methods of using these compositions therapeutically are also provided.

The present invention provides peptides and peptidomimetics corresponding to part or to the entirety of the region encompassed by residues 360-386 of human p53, said peptides and peptidomimetics characterized by the ability to activate DNA binding of wild-type p53 and to select tumor-derived p53 mutants. Pharmaceutical compositions of the compounds of the invention and methods of using these compositions therapeutically are also provided.

Novel phenyl-substituted 1,4-dihydropyridines, prepared by reacting halogenophenyl-aldehydes with &bgr;-ketoesters, if appropriate with isolation of the ylidene compounds and enamines. The substances can be employed as active compounds in medicaments, in particular in cerebrally active compositions.

Phenyl-substituted 1,4-dihydropyridines

Peptides and peptidomimetics with structural similarity to human P53 that activate P53 function

4-Phenyl-3-substituted 1,4-dihydropyridine esters are prepared by reaction of benzaldehydes with ketoesters and enamines, if appropriate with isolation of the ylidene intermediate products, or by esterification of corresponding dihydropyridinecarboxylic acids with alcohols. The new 4-phenyl-3-substituted 1,4-dihydropyridine esters can be employed as active compounds in medicaments for the treatment of the central nervous system, in particular as cerebral therapeutics.

4-phenyl-3-substituted 1,4-dihydropyridine esters

4-Heterocyclyl-substituted dihydropyridines are prepared by reacting appropriate aldehydes with .beta.-keto esters and aminocrotonic acid esters, or by esterifying 4-heterocyclyl-substituted dihydropyridinecarboxylic acids. The 4-heterocyclyl-substituted dihydropyridines can be employed in medicaments, in particular for the treatment of disorders of the central nervous system.

Heterocyclyl substituted dihydropyridines

2,8-Disubstituted quinazolinones are prepared by first subjecting the quinazolinone basic skeleton to condensation by customary reactions and then introducing the desired substituents into the 8-position. The compounds are suitable as active compounds in medicaments, in particular for the treatment of inflammations, thromboembolic diseases and cardiovascular diseases.

2,8-disubstituted quinazolinones

The present invention relates to the new compound rac-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)1,4 -dihydro-2,6-dimethylpyridine-3,5-dicarboxylate and its pure enantiomers, processes for their preparation and their use as medicaments, in particular for the treatment of cerebral and neuronal disorders, and a new intermediate for their preparation.

Isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,

The invention relates to new aryl-substituted alkoxycarbonyl-1,4-dihydropyridine-5-carboxylic acid esters, processes for their preparation and their use in medicaments, in particular as agents having a cerebral action.

Aryl-substituted alkoxycarbonyl-1,4-dihydropyridine-5-carboxylic acid

4-Heterocyclyl-substituted dihydropyridines are prepared by reacting appropriate aldehydes with .beta.-keto esters and aminocrotonic acid esters, or by esterifying 4-hetero-cyclyl-substituted dihydropyridinecarboxylic acids. The 4-heterocyclyl-substituted dihydropyridines can be employed in medicaments, in particular for the treatment of disorders of the central nervous system.

Growing community of inventors

Stamford, CT, United States of America

Wolfgang Hartwig