Vertex Pharmaceuticals, Inc.

Institut National De La Sante Et De La Recherche Medicale

Laboratoire Francais Du Fractionnement Et Des Biotechnologies

Assistance Publique-hopitaux De Paris

Sorbonne Université

Universite Paris Cité

Inserm (institut National De La Sante Et De La Recherche Medicale)

Wolf Herman Fridman

Guy W Bemis

Mark Andrew Murcko

Michael D Mullican

Robert E Zelle

David J Livingston

David J Lauffer

David Bebbington

Mark James Batchelor

Saroop Singh Matharu

Robert Murdoch

Roger John Gillespie

Julian M C Golec

Keith P Wilson

Michael Su

Philip L Nyce

Andrea L C Robidoux

M Woods Wannamaker

Yong Gu

Julian M Golec

John P Duffy

Christophe De Romeuf

Emmanuel Nony

Nicolas Bihoreau

Dominique Bourel

Jean-luc Teillaud

Catherine Sautes-Fridman

Marie-Caroline Dieu-Nosjean

Priyanka Devi

Sophie Siberil

The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&#x3b2; converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-&#x3b3;-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-&#x3b3;-mediated diseases and decreasing IGIF and IFN-&#x3b3; production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.

Inhibitors of interleukin-1&#x3b2; converting enzyme

The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&#x3b2; converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-&#x3b3;-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-&#x3b3;-mediated diseases and decreasing IGIF and IFN-&#x3b3; production using the compounds and compositions of this invention. This invention also relates to methods for preparing-N-acylamino compounds.

The present invention relates to a method for the production and the selection of human or chim&#xe6;ric or humanized antibodies or molecules that comprise the Fc region of human IgG, capable of modulating the activity of one or several particular Fc receptors, such as the triggering of inhibitory functions through the human type IIB receptors of IgG (FcgammaRIIB/CD32).

Preparation of human, humanized or chimaeric antibodies or polypeptides having different binding profiles to Fcgamma receptors

The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-&ggr;-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-&ggr;-mediated diseases and decreasing IGIF and IFN-&ggr; production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.

Inhibitors of interleukin-1&bgr; converting enzyme

The present invention relates to novel classes of compounds which are inhibitors of interleukin-IB converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-&ggr;-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-&ggr;-mediated diseases and decreasing IGIF and IFN-&ggr; production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.

Inhibitors of Interleukin-1&bgr; converting enzyme

The present invention relates to pyradazino&lsqb;1,2-a&rsqb;&lsqb;1,2&rsqb;diazepine-1-carboxamide compounds of formula:

Inhibitors of interleukin-1&bgr; Converting enzyme inhibitors

The present invention relates to novel classes of compounds which are inhibitors of interleukin-1 .beta. converting enzyme. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 and apoptosis-mediated diseases, including inflammatory diseases, autoimmune diseases, proliferative, infectious, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.

Inhibitors of interleukin-1.beta. converting enzyme

The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against an IL-1 mediated disease, an apoptosis mediated disease, AML, CML, melanoma, myeloma, Kaposi's sarcoma, graft vs host disease, rheumatoid arthritis, inflammatory bowel disorder, psoriasis, osteoarthritis, myeloma, apoptosis, sepsis, rheumatoid arthritis, asthma, Alzheimer's disease, Parkinson's disease, and ischemic heart disease diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.

The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 and apoptosis-mediated diseases, including inflammatory diseases, autoimmune diseases, proliferative, infectious, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.

Inhibitors of interleukin-1.beta.converting enzyme

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Paris, France

Wolf Herman Fridman