Abstract: Peptide analogs which are endowed with the property of at least partially reactivating a mutant p53 protein are provided. Also provided are uses thereof in the treatment of diseases associated with mutant p53.

Abstract: The invention discloses a method for the preparation of a peptide by liquid phase coupling of two fragments, an N-terminal fragment and a C-terminal fragment of the desired peptide, wherein the C-terminal fragment is protected on its C-terminal COOH by a psWang linker; the method is demonstrated with liraglutide wherein the C-terminal fragment carries the Palmitoyl-Glu-OtBu residue on the Lys.

Abstract: The invention relates to peptidic compounds, which peptidic compounds are compounds of formula (I)?, or a pharmaceutically acceptable salt, or solvate, or N-oxide, or stereoisomer thereof: wherein R1; R2; s; t; u; Aa78 and G1 are as defined herein. The peptidic compounds are useful in activating the Nrf2 pathway.

Abstract: The invention discloses a method for the preparation of a peptide by liquid phase coupling of two fragments, an N-terminal fragment and a C-terminal fragment of the desired peptide, wherein the C-terminal fragment is protected on its C-terminal COOH by a psWang linker; the method is demonstrated with liraglutide wherein the C-terminal fragment carries the Palmitoyl-Glu-OtBu residue on the Lys.

Abstract: The invention discloses a method for the preparation of N-omega-(1,2-dimethylindole-3-sulfonyl)-L-arginine and its derivatives using L-ornithine.

Abstract: The invention discloses a method for the preparation of N-omega-(1,2-dimethylindole-3-sulfonyl)-L-arginine and its derivatives using L-ornithine.

Abstract: The present invention relates to a compound of formula (I) (R1-Arg-Gly-Asp-Gly-Ala-Asn-Pro-Asn-Ala-Ala-Gly-R2), formula II (R5-Arg-Gly-Asp-Gly-Pro-Gln-Gly-Pro-Gln-R6), or formula III (R9-Trp-Arg-Phe-Gln-Trp-Gln-Phe-Glu-Gln-R10), and to compositions comprising a compound of formulas I, II or III, as well as the use of said compounds and/or said compositions in the cosmetic treatment of skin and/or hair, and to the use thereof for inducing the formation of collagen.

Abstract: The invention relates to conjugates in which a sterol is functionalized by an ether bond with a water-soluble polymer to which a guiding ligand is bound. These conjugates improve the physico-chemical and delivery properties of their carrying vesicles, making these more stable, homogeneous and effective. A method for their preparation, a pharmaceutical composition containing said liposomes, and their therapeutic use are described as well.

Abstract: The present invention relates to a compound of formula (I) and to compositions comprising said compound, as well as the use of said compound and/or said compositions in the cosmetic treatment of skin and/or hair, and to the use thereof for inducing the formation of collagen.

Abstract: The invention relates to conjugates in which a sterol is functionalized by an ether bond with a water-soluble polymer to which a guiding ligand is bound. These conjugates improve the physico-chemical and delivery properties of their carrying vesicles, making these more stable, homogeneous and effective. A method for their preparation, a pharmaceutical composition containing said liposomes, and their therapeutic use are described as well.

Abstract: The invention relates to a method for homogeneous solution phase peptide synthesis (HSPPS) of a N-terminal peptide fragment PEP-N and a C-terminal peptide fragment C-PEP, with C-PEP carrying a specific diketopiperazine (DKP) comprising C-terminal protecting group, which contains a handle group HG, with HG being connected to the C-terminus of the peptide fragmcnt; thereby this specific DKP comprising C-terminal protecting group can be selectively cleaved from the peptide as a conventionally used C-terminal protecting group. By the use of this DKP and HG comprising C-terminal protecting group, certain process steps in convergent peptide synthesis based on a combination of HSPPS and solid phase peptide synthesis (SPPS) can be avoided.

Abstract: The invention relates to a method for homogeneous solution phase peptide synthesis (HSPPS) of a N-terminal peptide fragment PEP-N and a C-terminal peptide fragment C-PEP, with C-PEP carrying a specific diketopiperazine (DKP) comprising C-terminal protecting group, which contains a handle group HG, with HG being connected to the C-terminus of the peptide fragment; thereby this specific DKP comprising C-terminal protecting group can be selectively cleaved from the peptide as a conventionally used C-terminal protecting group. By the use of this DKP and HG comprising C-terminal protecting group, certain process steps in convergent peptide synthesis based on a combination of HSPPS and solid phase peptide synthesis (SPPS) can be avoided.

Abstract: Antitumoral compounds of Formula I, and pharmaceutically acceptable salts, derivatives, tautomers, prodrugs or stereoisomers thereof useful as antitumour agents.

Abstract: The invention relates to a method for homogeneous solution phase peptide synthesis (HSPPS) of a N-terminal peptide fragment PEP-N and a C-terminal peptide fragment C-PEP, with C-PEP carrying a specific diketopiperazine (DKP) comprising C-terminal protecting group, which contains a handle group HG, with HG being connected to the C-terminus of the peptide fragment; thereby this specific DKP comprising C-terminal protecting group can be selectively cleaved from the peptide as a conventionally used C-terminal protecting group. By the use of this DKP and HG comprising C-terminal protecting group, certain process steps in convergent peptide synthesis based on a combination of HSPPS and solid phase peptide synthesis (SPPS) can be avoided.

Abstract: Compounds of formula (I) or their pharmaceutically acceptable salts, or their stereoisomers or mixtures of stereoisomers, where: R1 is selected from the group consisting of: phenyl, and phenyl mono-, di-, or tri-substituted by a radical independently selected from the group consisting of F, Cl, Br, I, (C1-C6)-alkyl, COO—(C1-C6)-alkyl, and (C1-C6)-alkoxy; and R2 is a radical selected from the same group as R1, further including a phenyl substituted in 4-position by a radical independently selected from the group consisting of —O(CH2)CONH(CH2)3CH3 and OCH2COOC(CH3)3, a biphenyl-4-yl, thiazol-2-yl, and a thiazol-2-yl mono- or di-substituted by a radical selected from F and phenyl; inhibit cell proliferation of tumor cells independently of p53 protein and may also induce apoptosis in several tumor cells independently of p53 protein, being useful for the treatment of several types of cancer.

Abstract: Novel iminium-type coupling agents containing proton acceptors in their iminium moiety, which can be used beneficially as coupling agents in various chemical polypeptide and/or polynucleotide syntheses, and are particularly useful as yield enhancing and racemization suppressing coupling agents for use in peptide syntheses, are disclosed. Further disclosed are a process of preparing such iminium-type coupling agents and their use in the preparation of polypeptides and/or polynucleotides.

Abstract: Compounds of formula (I) or their pharmaceutically acceptable salts, or their stereoisomers or mixtures of stereoisomers, where: R1 is selected from the group consisting of: phenyl, and phenyl mono-, di-, or tri-substituted by a radical independently selected from the group consisting of F, Cl, Br, I, (C1-C6)-alkyl, COO-(C1-C6)-alkyl, and (C1-C6)-alkoxy; and R2 is a radical selected from the same group as R1, further including a phenyl substituted in 4-position by a radical independently selected from the group consisting of —O(CH2)CONH(CH2)3CH3 and OCH2COOC(CH3)3, a biphenyl-4-yl, thiazol-2-yl, and a thiazol-2-yl mono- or di-substituted by a radical selected from F and phenyl; inhibit cell proliferation of tumor cells independently of p53 protein and may also induce apoptosis in several tumor cells independently of p53 protein, being useful for the treatment of several types of cancer.

Abstract: The invention relates to indolesulfonyl halogenides which are useful for the protection of organic compounds comprising at least one guanidino moiety and/or at least one amino group. The invention further relates to a process for their preparation and their use as protecting reagents. The invention also relates to the process for the protecting reaction and to the protected compounds thereof.

Abstract: The present invention relates to a new series of 1,2-diphenylpyrroles of formula (I) or their pharmaceutically acceptable salts, or their pharmaceutically acceptable solvates, having antitumor activity, wherein R1 and R2 are individually selected from the group consisting of halogen, optionally substituted O(C1-C4)alkyl and optionally substituted (C1-C4)alkyl; and R3 is selected from the group consisting of H, (C1-C4)alkyl, CONH2 and (C?NH)NH2. It also relates to a process for preparing them, to pharmaceutical compositions containing them, and to their use for the treatment of cancer, in particular lung carcinoma, colorectal carcinoma, breast carcinoma and/or prostate carcinoma.

Abstract: Antitumoral compounds of Formula I, and pharmaceutically acceptable salts, derivatives, tautomers, prodrugs or stereoisomers thereof useful as antitumour agents.