Dsm IP Assets B.v.

Bayer Aktiengesellschaft

Wilex Ag

Novartis Corporation

Ciba-geigy Corporation

Syngenta Crop Protection, Inc.

Novartis Finance Corporation

Novartis Crop Protection, Inc.

Pentapharm Ag

Bayer Aktiengsellschaft

Hugo Ziegler

Stephan Trah

Rene Zurfluh

Saleem Farooq

Peter Wikstroem

Marc Heidl

Ren&eacute; Zurfl&uuml;h

Dominik Imfeld

Henry Szczepanski

Martin Eberle

Alfons Pascual

Daniel Stierli

Roger Graham Hall

Anthony Cornelius O'Sullivan

Martin Zeller

Albert Pfiffner

Christian Ludin

Fredrik Cederbaum

Anita Schnyder

Andr&eacute; Jeanguenat

Hans P Isenring

Roger G Hall

Piero Geotti-Bianchini

Jörg Stürzebecher

Rudolf Waditschatka

Peter Ackermann

Wolfgang Stutz

Beat Zehnder

Christian Pillonel

Stefan Martin Stoeckli

Remo Campiche

Linhua Wang

Martin Stöckli

Stephen Trah

Denis Neff

Edward Kelsall

Dagmar Prasa

Dominic Imfeld

Roman Wille

The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (Hor ammoniumformiateformate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

Method for producing 3-amidinophenylalanine derivatives

The present invention relates to a novel composition comprising danielone and derivatives thereof as well as to the use of such compositions in skin lightening. More particularly, the present invention relates to danielone and derivatives thereof for use in topical compositions for smoothening skin color irregularities, for reducing melanin formation in the human skin, for lightening/brightening human skin and/or for treatment of pigmentation disorders which comprises topically administering an effective amount of danielone and derivatives thereof to the appropriate skin area of a person in need of such beautifying agent, or treatment.

Use of danielone and derivatives thereof in skin care

Cosmetic composition which can be applied topically, comprising at least one compound of the general formula (I) in which Ris H, C-C-alkyl, cycloalkyl or aryl-C-C-alkyl, n is 1-4, X is &#x2014;O&#x2014;, &#x2014;NH&#x2014; or &#x2014;NR&#x2014; and RH or C-C-alkyl; and at least one compound corresponding to the above formula (I) but in which XRwith X having the possible meaning of &#x2014;NH&#x2014; is the residue of an alpha-amino acid; use of these compounds and of the composition for stimulating the synthesis of the proteins of the basement membrane; and also both those compounds of the formula (I) in which X is &#x2014;NR&#x2014; and both Rand Rare different from H, and the compounds corresponding to formula (I) but in which XRwith X having the possible meaning of &#x2014;NH&#x2014; is the residue of an alpha-amino acid, as such.

Cosmetic composition for stimulating the synthesis of proteins of the basement membrane

The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (Hor ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

The present invention relates to compositions comprising a peptide with 2-12 amino acids substituted with a lipophilic moiety and a water soluble salt of an alkali, earth alkaline metal or transition metal. Furthermore, the invention relates to a container comprising such compositions. Additionally, the invention relates to the use of a water soluble salt of an alkali, earth alkaline metal or transition metal for reducing the adhesion of a peptide with 2-12 amino acids substituted with a lipophilic moiety to a surface.

Composition

The invention relates to compounds and to the cosmetically acceptable salts thereof, which correspond to general formula (I), wherein: Rrepresents H, &#x2014;C(O)&#x2014;R, &#x2014;SO&#x2014;Ror &#x2014;C(O)&#x2014;XR; Rand R, independent of one another, represent (CH)&#x2014;NHor (CH)&#x2014;NHC(NH)NH; n equals 1 4; Rrepresents linear or branched C-Calkyl that is optionally substituted by hydroxy; Rand R, independent of one another, represent hydrogen, optionally substituted (C-C)alkyl, optionally substituted C-Calkenyl, optionally substituted phenyl, optionally substituted phenyl-C-Calkyl or 9-fluorenyl-methyl; X represents oxygen (&#x2014;O&#x2014;) or NH&#x2014;; or XRwith X&#x2550;O also represents the esters of a-tocopherol, tocotrienol or retinol, with the provision that Rand Rdo not represent hydrogen and X does not represent oxygen at the same time. The invention also relates to the production of the compounds of general formula (I) and to a cosmetically active composition that contains at least one compound of formula (I).

Tripeptides and derivatives thereof for cosmetic application in order to improve skin structure

Cosmetic composition which can be applied topically, comprising at least one compound of the general formula (I) in which Ris H, C-C-alkyl, cycloalkyl or aryl-C-C-alkyl, n is 1-4, X is &#x2014;O&#x2014;, &#x2014;NH&#x2014; or &#x2014;NR&#x2014; and RH or C-C-alkyl; and at least one compound corresponding to the above formula (I) but in which XRwith X having the possible meaning of &#x2014;NH&#x2014; is the residue of an alpha-amino acid; use of these compounds and of the composition for stimulating the synthesis of the proteins of the basement membrane; and also both those compounds of the formula (I) in which X is &#x2014;NR&#x2014; and both Rand Rare different from H, and the compounds corresponding to formula (I) but in which XRwith X having the possible meaning of &#x2014;NH&#x2014; is the residue of an alpha-amino acid, as such. 

Topical application agents against mimic and age-related wrinkles

The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidinophenylalanine derivatives under gentle conditions (Hor ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

The invention relates to compounds and to the cosmetically acceptable salts thereof, which correspond to general formula (I), wherein: Rrepresents H, &#x2014;C(O)&#x2014;R, &#x2014;SO&#x2014;Ror &#x2014;C(O)&#x2014;XR; Rand R, independent of one another, represent (CH)&#x2014;NHor (CH)&#x2014;NHC(NH)NH; n equals 1 4; Rrepresents linear or branched C-Calkyl that is optionally substituted by hydroxy; Rand R, independent of one another, represent hydrogen, optionally substituted (C-C) alkyl, optionally substituted C-Calkenyl, optionally substituted phenyl, optionally substituted phenyl-C-Calkyl or 9-fluorenyl-methyl; X represents oxygen (&#x2014;O&#x2014;) or &#x2014;NH&#x2014;; or XRwith X&#x2550;O also represents the esters of a-tocopherol, tocotrienol or retinol, with the provision that Rand Rdo not represent hydrogen and X does not represent oxygen at the same time. The invention also relates to the production of the compounds of general formula (I) and to a cosmetically active composition that contains at least one compound of formula (I). 

The invention relates to compounds of general formula (I) and acid addition salts thereof, where the various symbols have the meanings given in the description and claims, the production and use thereof as substrate for the detection of TAFIa, a fibrinolysis inhibiting enzyme. The detection occurs by using the absorption between 400 and 412 nm, arising as a result of the formation of 3-carboxy-4-nitrothiophenol from Ellman's reagent as a function of time. 

Substrates for TAFI (A)

Oligopeptides and derivatives thereof, peptide analogs and derivatives thereof as well as pharmaceutically acceptable salts of these compounds, which correspond to general formula (I) wherein

Dermopharmaceutically and cosmetically active oligopeptides

The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidinophenylalanine derivatives under gentle conditions (Hor ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H, Pd/C, AcOH or HOI/ethanol, 1&#x2013;3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

The present invention relates to a method of protecting plants against attack or infestation by phytopathogenic organisms, such as nematodes or especially microorganisms, preferably fungi, bacteria and viruses, or combinations of two or more of these organisms, by applying at least one compound of the formula (I): wherein n is 0 or 1, Ris halogen, alkoxy, haloalkyl, haloalkoxy or alkyl, Ris hydrogen, halogen, alkyl, haloalkyl, alkoxy or haloalkoxy, each of R, Rand Ris, independently of the others, hydrogen, lower alkyl or halogen, and Ris as defined in claimThe invention also relates to new compounds of formula (I), their preparation, use and compositions comprising said compound 

N-phenyl-4-(4-pyridyl)-2-pyrimidineamine derivatives

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Witterswil, Switzerland

Hugo Ziegler