Abstract: 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 (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

Abstract: The invention relates to compounds and to the cosmetically acceptable salts thereof, which correspond to general formula (I), wherein: R1 represents H, —C(O)—R6, —SO2—R6 or —C(O)—XR6; R2 and R4, independent of one another, represent (CH2)n—NH2 or (CH2)3—NHC(NH)NH2; n equals 1 4; R3 represents linear or branched C1-C4 alkyl that is optionally substituted by hydroxy; R5 and R6, independent of one another, represent hydrogen, optionally substituted (C1-C24) alkyl, optionally substituted C2-C24 alkenyl, optionally substituted phenyl, optionally substituted phenyl-C1-C4 alkyl or 9-fluorenyl-methyl; X represents oxygen (—O—) or —NH—; or XR5 with X?O also represents the esters of a-tocopherol, tocotrienol or retinol, with the provision that R1 and R5 do 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).

Abstract: 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.

Abstract: 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 R1 represents H, —C(O)—R7, —SO2—R7, —C(O)—OR7 or —C(O)—N(R7)2 R2 represents, independent of one another, H or —(C1-C4)-alkyl, R3 and R6 represent, independent of one another, —(CH2)q—N(R1)R8 R4 and R5 represent, independent of one another, —CH2—OR2, —CH(CH3)OR8 or —CH2—CH2—OR8 R7 represents hydrogen, optionally substituted (C1-C19)-alkyl; optionally substituted (C1-C19)-alkenyl; phenyl-(C1-C4)-alkyl whose phenyl radical is optionally substituted with amino in the para position R8 represents H, —(C1-C4)-alkyl, —C(O)—R7, —C(O)—OR7, —C(O)—N(R7)2 or —SO2—R7 X represents oxygen (—O—) or —NH—; or XR7, with X=O, also represents the esters of ?-tocopherol, tocotrienol or retinol or the carboxylic acid (with R7=H) m, n, p represent, independent of one another, zero or 1 and q in R3 and R6 represent, independent of one a

Abstract: Topical composition for use especially as a skin lightener, characterized in that it contains an effective amount of at least one compound of general formula (I) or a mixture of such compounds and/or an acid addition salt thereof: in which X is NH or a direct bond and n is 2, 3 or 4, preferably 2 or 3, and its use for lightening skin colour, for depigmenting liver spots and for evening out non-uniformities in skin colouration. The invention further relates to dermatologically effective compositions containing at least one disulfide of general formula (I) and at least one additional skin care ingredient.

Abstract: Cosmetic composition which can be applied topically, comprising at least one compound of the general formula (I) in which R1 is H, C1-C20-alkyl, cycloalkyl or aryl-C1-C4-alkyl, n is 1-4, X is —O—, —NH— or —NR2— and R2H or C1-C20-alkyl; and at least one compound corresponding to the above formula (I) but in which XR1 with X having the possible meaning of —NH— 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 —NR2— and both R1 and R2 are different from H, and the compounds corresponding to formula (I) but in which XR1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid, as such.

Abstract: The compounds of formula (I) wherein X represents a bond or NH—CH(C?O)—(CH2)3+n—NH—R5, n represents 0, 1 or 2, R1, R4 and R5—independently from each other—represent hydrogen, possibly substituted C1-C6-alkyl, amidino or tetra-C1-C6-alkylamidinium, R2 represents hydrogen or possibly substituted C1-C6-alkyl or R1 and R2 together with the residue to which they are bound represent a 5- to 7-membered, saturated ring, R3 represents C1-C12-alkoxy, C1-C12-alkylamino, possibly substituted aryl-C1-C6-alkylamino, possibly substituted heteroaryl-C1-C6-alkylamino, possibly substituted aryl-C1-C6-alkoxy or possibly substituted heteroaryl-C1-C6-alkoxy, and R6 represents hydrogen or, when n is 1, also amino or together with R1 and the residue to which R6 and R1 are bound a 5- to 7-membered, saturated ring, as well as their physiologically acceptable salts are new.

Abstract: 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 (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

Abstract: The invention relates to compounds and to the cosmetically acceptable salts thereof, which correspond to general formula (I), wherein: R1 represents H, —C(O)—R6, —SO2—R6 or —C(O)—XR6; R2 and R4, independent of one another, represent (CH2)n—NH2 or (CH2)3—NHC(NH)NH2; n equals 1 4; R3 represents linear or branched C1-C4 alkyl that is optionally substituted by hydroxy; R5 and R6, independent of one another, represent hydrogen, optionally substituted (C1-C24) alkyl, optionally substituted C2-C24 alkenyl, optionally substituted phenyl, optionally substituted phenyl-C1-C4 alkyl or 9-fluorenyl-methyl; X represents oxygen (—O—) or —NH—; or XR5 with X=O also represents the esters of a-tocopherol, tocotrienol or retinol, with the provision that R1 and R5 do 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).

Abstract: 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 (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HOI/ethanol, 1–3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

Abstract: 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, R1 is halogen, alkoxy, haloalkyl, haloalkoxy or alkyl, R2 is hydrogen, halogen, alkyl, haloalkyl, alkoxy or haloalkoxy, each of R3, R4 and R5 is, independently of the others, hydrogen, lower alkyl or halogen, and R6 is as defined in claim 1.

Abstract: The invention relates to novel N-phenyl-4-(4-pyridyl)-2-pyrimidineamine derivatives of the general formula (I) wherein the sum of (m+p) together is 0, 1, 2 or 3; n and q are independently of each other 0 or 1, and the sum of (m+p+q) together is 1, 2, 3 or 4; R1 is hydrogen, halogen, alkoxy, haloalkyl, haloalkoxy or alkyl; R2 is hydrogen, C1–C6-alkyl, C1–C6-haloalkyl or C1–C6-alkoxy; R2A is hydrogen, C1–C6-alkyl, C3–C4-alkenyl or C3–C4-alkynyl; each of R3, R4, R5 and R6 is, independently of the others, hydrogen, C1–C6-alkyl, C1–C6-haloalkyl, hydroxy-C1–C6-alkyl or C1–C6-alkoxy-C1–C6-alkyl, or the ring members CR3R4 or CR5R6 or CR2R2A are independently of each other a carbonyl group (C?O) or a group C?S; X is C?O, C?S, S?O or O?S?O; Y is O, S, C?O, CH2, —N(R8)—, —O—N(R8)—, —N(R8)—O— or NH—; R7 is hydrogen, C1–C4-alkyl, C3–C4-alkenyl, C3–C4-alkynyl, —CH2OR8, CH2SR8, —C(O)R8, —C(O)OR8, SO2R8, SOR8 or SR8; and R8 is C1–C8-alkyl, C1–C8-alkoxyalkyl, C1–C8 haloalkyl or phenylC1–C2-alkyl wherein the phenyl may be subs

Abstract: 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.

Abstract: The invention relates to methods for producing enantiomer-pure 3-amidinophenylalanine derivatives, based on 3-cyanophenylalanine derivatives, which are used as pharmaceutically active urolinase inhibitors. The inventive production methods give novel intermediates, namely 3-hydroxyamidino- and 3-amidrazono-phenylalanine derivatives. These intermediates or the acetyl derivatives thereof can be reduced to the desired 3-amidinophenylalanine derivatives under mild conditions (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, ambient temperature, normal pressure, or H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomer purity of up to 99.9 %.

Abstract: 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 R1 represents H, —C(O)—R7, —SO2—R7, —C(O)—OR7 or —C(O)—N(R7)2 R2 represents, independent of one another, H or —(C1-C4)-alkyl, R3 and R6 represent, independent of one another, —(CH2)q—N(R1)R8 R4 and R5 represent, independent of one another, —CH2—OR2, —CH(CH3)OR8 or —CH2—CH2—OR8 R7 represents hydrogen, optionally substituted (C1-C19)-alkyl; optionally substituted (C1-C19)-alkenyl; phenyl-(C1-C4)-alkyl whose phenyl radical is optionally substituted with amino in the para position R8 represents H, —(C1-C4)-alkyl, —C(O)—R7, —C(O)—OR7, —C(O)—N(R7)2 or —SO2—R7 X represents oxygen (—O—) or —NH—; or XR7, with X=O, also represents the esters of ?-tocopherol, tocotrienol or retinol or the carboxylic acid (with R7=H) m, n, p represent, independent of one another, zero or 1 and q in R3 and R6 represent, independent of one

Abstract: The invention relates to the compounds of general formula (I), that are present with respect to R1 as racemates as well as L- or D-configured compounds and as E/Z mixtures as well as E or Z isomers and in which the various symbols are defined as in the description and the claims, as well as to the salts thereof, for use as therapeutic agents and for diagnostic purposes. The inventive compounds can be processed to medicaments or to diagnostic agents that are used for the diagnosis, therapy and prevention of urokinase- or urokinase-receptor associated diseases, for example for the treatment of tumors. The compounds are highly efficient in inhibiting growth and/or spread of malign tumors, for example tumor spread of pancreatic cancer, tumor growth of breast cancer and the formation of tumor metastases. The compounds of formula (I) and the salts thereof can be produced by conventional methods.

Abstract: The invention relates to the compounds of general formula (I), that are present with respect to R1 as racemates as well as L- or D-configured compounds and as E/Z mixtures as well as E or Z isomers and in which the various symbols are defined as in the description and the claims, as well as to the salts thereof, for use as therapeutic agents and for diagnostic purposes. The inventive compounds can be processed to medicaments or to diagnostic agents that are used for the diagnosis, therapy and prevention of urokinase- or urokinase-receptor associated diseases, for example for the treatment of tumors. The compounds are highly efficient in inhibiting growth and/or spread of malign tumors, for example tumor spread of pancreatic cancer, tumor growth of breast cancer and the formation of tumor metastases. The compounds of formula (I) and the salts thereof can be produced by conventional methods.

Abstract: The present invention relates to a novel improved process and intermediates for the process of preparing the oxime intermediates of formula (II) wherein R1 is hydrogen, fluoro or chloro, and R2 is methyl, ethyl, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy, cyano, fluoro, chloro or bromo. The novel process comprises diazotizing an aniline of formula (VI) reacting the resulting diazonium salt with isopropenylacetate of formula (X) and reacting the resulting ketone of formula (XI) with an organic nitrite in the presence of hydrogene chloride, and methylating the resulting ketooxime of formula (VIII) with a methylating agent and reacting the resulting O-methyl ketooxime of formula (IX) with hydroxylamine. The compounds of formula (II) are intermediates for highly active fungicides from the class of the atrobilurins.

Abstract: The invention relates to novel N-phenyl-4-(4-pyridyl)-2-pyrimidineamine derivatives of the general formula (1) wherein the sum of (m+p) together is 0, 1, 2 or 3; n and q are independently of each other 0 or 1, and the sum of (m+p+q) together is 1, 2, 3 or 4; R1 is hydrogen, halogen, alkoxy, haloalkyl, haloalkoxy or alkyl; R2 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl or C1-C6-alkoxy; R2A is hydrogen, C1-C6-alkyl, C3-C4-alkenyl or C3-C4-alkynyl; each of R3, R4, R5 and R6 is, independently of the others, hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, hydroxy-C1-C6-alkyl or C1-C6-alkoxy-C1-C6-alkyl, or the ring members CR3R4 or CR5R6 or CR2R2A are independently of each other a carbonyl group (C═O) or a group C═S; X is C═O, C═S, S═O or O═S=O; Y is O, S, C═O, CH2A, —N(R8)—, —O—N(R8)—, —N(R8)—O— or NH—; R7 is hydrogen, C1-C4-alkyl, C3-C4-alkenyl, C3-C4-alkynyl, —CH2OR8, CH2SR8, —C(O)R8, —C(O)OR8,

Abstract: The invention relates to a process for the preparation of compounds of the formula 1