University of Minnesota

Lonza Inc.

Pharma Mar, S.a.

Perseptive Biosystems Inc.

Luxembourg Bio Technologies Ltd.

Lonza Ag

Fernando Albericio

George Barany

Samuel Zalipsky

Matthieu Giraud

Steven A Kates

Jane Chang

Jordi Alsina

Knud J Jensen

Ignacio Manzanares

Maria Del Carmen Cuevas Marchante

María Del Carmen Cuevas Marchante

Judit Tulla-Puche

Micheal F Songster

Ariel A Ewenson

Yoav Luxembourg

Nuria A Sol E

Angel Lopez

Nuria A Sole

Josef Vagner

Josef V&aacute;gner

Miriam Royo

Ignacio Rodrigues

Jose Carlos Jimenez

Ernest Giralt

Mercedes Alvarez Domingo

Albert Isidro Liobet

Ayman El-Faham

Núria Bayó-Puxan

Eleonora Marcucci

Miriam Gongora Benitez

Michèle Cristau

Luis Javier Cruz

Albert Isidro Llobet

Fayna Garcia-Martin

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. The invention relates further to a method for the preparation of such specifically protected fragment C-PEP by SPPS by using a linker comprising a specific dipeptide and HG for connecting the growing peptide chain to the resin, which linker forms said DKP group, when the peptide fragment C-PEP is cleaved from the supporting resin; and further to the intermediates of the preparation method.

Diketopiperazine forming dipeptidyl linker

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

Antitumoral compounds

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.

Proton acceptor iminium/carbocation-type coupling agents

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.

Indolesulfonyl protecting groups for protection of guanidino and amino groups

A process is provided for preparing kahalalide F and which leads to other kahalalide mimic compounds having useful biological activity.

Kahalalide F and related compounds

A support material for solid phase synthesis is provided having an amine-containing organic group attached to it through a linker. The support material is of the following general formula (Formula I):

Support material for solid phase organic synthesis

A support material for solid phase synthesis is provided having an amine-containing organic group attached to it through a linker. The support material is of the following general formula (Formula I): ##STR1##

A method for removing an allyl protecting group from an allyl-protected derivative of a biologically relevant amino acid is disclosed. One relevant aspect of the method is the use of soluble organometallic catalyst, such as an organopalladium catalyst. Preferably, soluble tetrakistriphenylphosphine palladium (0) is used. The allyl deprotection method now disclosed is suitable for use on an instrument for automated peptide synthesis. Methods of preparing the soluble organometallic catalyst are also disclosed, as are soluble catalyst compositions.

Automated allyl deprotection in solid-phase synthesis

The present invention pertains to polyethylene glycol (PEG) derivatized graft supports, to methods for making these supports and to methods of using the supports to synthesize peptides by solid-phase synthesis techniques. The PEG-graft supports of this invention comprise functionalized PEG derivatives which are covalently attached to solid supports, such as polystyrene.

Polyethylene glycol derivatives for solid-phase applications

Novel acid-labile tris(alkoxy)benzyl ester handles for use in linking protected amino acid or peptides to a support during peptide synthesis are disclosed. Methods for producing the handles, for linking them to solid support resins and for using the resin-linked handles in peptide synthesis are disclosed.

Hypersensitive acid-labile handle for solid-phase peptide synthesis

Growing community of inventors

Barcelona, Spain

Fernando Albericio