The Hospital for Sick Children

Hsc Research and Development Limited Partnership

Other

Hsc Research and Development Limited

Chaim M Roifman

Olga Rounova

Peter M Demin

Thomas Grunberger

Nigel Sharfe

Tom Grunberger

Andrew Freywald

Demin Peter

Octavian Laurand Cimpean

Eyal Gruebaum

Peter Demin

There is described compounds of Formulae I, II, III, IV and V. The compounds of Formulae I, II, III, IV and/or V are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.

Compounds useful for modulating abnormal cell proliferation

Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.

Compounds for modulating cell proliferation

The following compounds of formulae (I) and (III) which may be useful in treating a variety of cell proliferative disorders are disclosed: Formula (I), (II), wherein R, Rand Rare each independently selected from H, OH, Calkyl, Calkoxy, NH, NH&#x2014;Calkyl, N(Calkyl), SH, S&#x2014;Calkyl, NO, CF, OCFand halo; Ris unsubstituted Ar, or Ar substituted with 1-4 substituents, independently selected from Calkyl, Calkoxy and halo; X is selected from (CHCHO)and (CH), and n=1-4. 

There is described compounds of Formula I, and salts, solvates and hydrates thereof: wherein: R, Rand Rare each independently selected from OH, Calkyl, OCalkyl, OC(O)Calkyl, C(O)OCalkyl, NH, NH&#x2014;Calkyl, N(Calkyl)(Calkyl), C(O)NHCalkyl, C(O)N(Calkyl)(Calkyl), SH, SCalkyl, NO, CF, OCFand halogen; and Ar is an aromatic or heteroaromatic group chosen from benzene, naphthalene, quinoline, isoquinoline, indole, pyridine, pyrasine, pyrimidine, imidazole, furan and thiophene, unsubstituted or substituted with 1-4 substituents independently selected from OH, Calkyl, Calkoxy, Calkylenedioxy, NH, NH&#x2014;Calkyl, N(Calkyl)(Calkyl), SH, S&#x2014;Calkyl, NO, CF, OCFand halogen. The compounds of Formula I are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.

Manipulation of the EphB6 receptor and its active Eph partners allow for regulation of T cell responses, including TCR signaling, T cell proliferation, and induction of T cell death. Methods of modulating EphB6 are described as well as various therapeutic applications.

Methods of modulation of the immune system

There is described compounds of Formula I, and salts, solvates and hydrates thereof: wherein: R, Rand Rare each independently selected from OH, Calkyl, OCalkyl, OC(O)Calkyl, C(O)OCalkyl, NH, NH&#x2014;Calkyl, N(Calkyl)(Calkyl), C(O)NHCalkyl, C(O)N(Calkyl)(Calkyl), SH, SCalkyl, NO, CF, OCFand halogen; and Ar is an aromatic or heteroaromatic group chosen from benzene, naphthalene, quinoline, isoquinoline, indole, pyridine, pyrasine, pyrimidine, imidazole, furan and thiophene, unsubstituted or substituted with 1&#x2013;4 substituents independently selected from OH, Calkyl, Calkoxy, Calkylenedioxy, NH, NH&#x2014;Calkyl, N(Calkyl)(C)(Calkyl), SH, S&#x2014;Calkyl, NO, CF, OCFand halogen. The compounds of Formula I are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.

Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders  such as cancer are disclosed. The compounds are of Formula (I).

Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed. The compounds are of the Formula I:

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North York, Canada

Chaim M Roifman