Philogen S.p.a.

Eidgenoessische Technische Hochschule Zurich

Medical Research Council

Philochem Ag

Eth Zurich

Eidgenossische Technische Hochschule Zurich

Dario Neri

Gregory Paul Winter

Alessandra Villa

Luciano Zardi

Barbara Carnemolla

Dragan Grabulovski

Giovanni Neri

Samu Melkko

Christoph Schliemann

Jascha-Nikolai Rybak

Christoph Rosli

Lorenzo Tarli

Manuela Kaspar

Willy Decurtins

Moreno Wichert

Francesca Viti

Jörg Scheuermann

Cornelia Halin

Fredrik Nilsson

Dan S Tawfik

Eveline Trachsel

Hans Menssen

Laura Borsi

Andreas Menrad

Nikolaus Krall

Franziska Sophie Bootz

Salvatore Demartis

Adrian Huber

Sarah Wulhfard

Roberto De Luca

Claudia De Lalla

Michela Silacci

Manfred Birchler

Simon Brack

Raphael Franzini

Jorg Scheuermann

Cornelia Winter Halin

Jascha Nikolai Rybak

Christoph Dumelln

Marta Pedretti

Verena Gafner

Michael Detmar

Teresa Hemmerle

Simon Schwager

Silvana Renner

Giulio Casi

Katrin Gutbrodt

Christoph Dumelin

Christoph Roesli

Christoph Rösli

Jascha-Nikolai Raybak

Chistoph RÖSLI

Jascha Rybak

Hans Dietrich Menssen

The application relates to a fusion protein comprising an antibody molecule, or antigen-binding fragment thereof, and a member of the vascular endothelial growth factor family, such as VEGF-C or VEGF-D. The antibody molecule preferably binds an antigen associated with angiogenesis, such as the ED-A isoform of fibronectin. In particular, the application relates to the therapeutic use of such fusion protein in the treatment of an inflammatory disease or disorder.

Vascular endothelial growth factor/anti-fibronectin antibody fusion proteins

The present application relates to conjugates comprising interleukin 2 (IL2), and a mutant of tumour necrosis factor, such as tumour necrosis factor alpha (TNF&#x3b1;), and an antibody molecule. The antibody molecule preferably binds to an antigen associated with neoplastic growth and/or angiogenesis, such as the Extra-Domain A (EDA) or Extra-Domain B (EDB) of fibronectin. The conjugate may be used in the treatment of cancer.

IL2 and TNF mutant immunoconjugates

A library is provided having a plurality of recombinant derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1, where one or more of the derivatives have a specific binding affinity to a protein or peptide that is not a natural SH3 binding ligand. Substantially each of the derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1 has an amino acid sequence with at least 80% sequence identity to the amino acid sequence of SEQ ID NO: 1, and at least 90% identity to the amino acid of SEQ ID NO: 1 outside the src and RT loops. Additionally, the amino acid sequence has at least one amino acid in or positioned up to two amino acids adjacent to the RT loop or the src loop of SEQ ID NO: 1 which is substituted, deleted or added.

Specific and high affinity binding proteins comprising modified SH3 domains of FYN kinase

The invention provides a chemical compound comprising a chemical moiety (p) capable of performing a binding interaction with a target molecule, and an oligonucleotide (b) or functional analogue thereof. The oligonucleotide (b) or functional analogue comprises at least one self-assembly sequence (b1) capable of performing a combination reaction with at least one self-assembly sequence (b1') of a complementary oligonucleotide or functional analogue bound to another chemical compound comprising a chemical moiety (q). In some embodiments, the chemical compound comprises a coding sequence (b1) coding for the identification of the chemical moiety (p) and further comprises at least one self-assembly moiety (m) capable of performing a combination reaction with at least one self-assembly moiety (m&#x2032;) of a similar chemical compound comprising a chemical moiety (q). The invention also provides corresponding libraries of chemical compounds as well as methods of biopanning of for target molecules and of identifying such targets.

Encoded self-assembling chemical libraries (ESACHEL)

The application relates to a conjugate comprising interleukin-22 (IL22) and an antibody molecule. The antibody molecule preferably binds an antigen associated with angiogenesis, such as the ED-A isoform of fibronectin. In particular, the application relates to the therapeutic use of such conjugates in the treatment of a disease/disorder, such as autoimmune diseases, including inflammatory bowel disease (IBD).

IL22 immunoconjugates

The invention relates to an antibody-drug conjugate and an immunocytokine for use in the treatment of a neoplastic or inflammatory disease, as well as molecules comprising an antibody-drug conjugate and an immunocytokine.

Methods of treating a neoplastic disease

This invention relates to the synthesis of nucleic acid-encoded chemical libraries using common adaptor sequences. Nucleic acid strands coupled to chemical moieties may be contacted with identifier oligonucleotides comprising coding sequences encoding the chemical moieties and an adaptor oligonucleotides, such that the adaptor oligonucleotide hybridizes to both the nucleic acid strands and the identifier oligonucleotides to allow ligation of the identifier oligonucleotides to the nucleic acid strands. The adaptor oligonucleotide is then removed. Nucleic acid-encoded chemical libraries, and methods of producing or screening such libraries are provided.

Production of encoded chemical libraries

The invention relates to a binding member that binds the Extra Domain-A (ED-A) isoform of fibronectin for the treatment of lung cancer and lymphoma.

Antigen associated with lung cancers and lymphomas

A binding moiety (B) for Carbonic Anhydrase IX (CAIX), the binding moiety comprising: The binding moiety is univalent, bivalent, or multivalent. A targeted therapeutic agent may comprise the binding moiety. The invention also includes a method for treating a disease expressing elevated levels of CAIX by administering the targeted therapeutic agent.

Small molecule drug conjugates

The present invention relates to a method for the production of a library comprising recombinant derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1 as well as a method for selecting from a library comprising recombinant derivatives of the SH3 domain of the Fyn kinase of SEQ ID NO: 1 one or more of said derivatives having a specific binding affinity to a protein or peptide.

The invention relates to a binding member that binds the Extra Domain-A (ED-A) isoform of fibronectin for the treatment of tumour metastases.

Antigen associated with the neovasculature of tumour metastases

A targeted therapeutic agent comprising a compound of formula I:B-L-D&#x2003;&#x2003;(I),wherein: B is a low molecular weight binding moiety for Carbonic Anhydrase IX (CAIX); D is a drug moiety; and L is a linker group that undergoes cleavage in vivo for releasing said drug moiety in an active form. The drug moiety is suitably a cytotoxic agent for targeted delivery to cancer cells expressing CAIX. The binding moiety B suitably comprises a sulfonamidothiadiazole moiety. The binding moiety B may comprise one, two or more groups capable of binding to CAIX. The linker group suitably comprises a disulfide bond and/or a triazole group and/or a cleavable peptide group.

Encoded self-assembling chemical libraries (esachel)

Specific and high affinity binding proteins comprising modified SH3 domains of Fyn kinase

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Buchs, Switzerland

Dario Neri