Cancer Research Technology Limited

Institute of Cancer Research: Royal Cancer Hospital (the)

The Institute of Cancer Research: Royal Cancer Hospital

Astex Therapeutics Limited

The Institute of Cancer Research : the Royal Cancer Hospital

Delphine Menard

Caroline Joy Springer

Dan Niculescu-Duvaz

Richard Marais

Ion Niculescu-Duvaz

Alfonso Zambon

Arnaud Nourry

Bartholomeus Marinus Josephus Marie Suijkerbuijk

Harmen Dijkstra

Adrian Liam Gill

Richard David Taylor

Esteban Roman Vela

Lawrence Davies

Catherine Gaulon

Bartholomeus Marinus Suijkerbuijk

Richard Malcolm Marais

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (for convenience, collectively referred to herein as 'IP compounds'), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterized by (e.g., driven by) mutant RAS ('mutant RAS cancer'). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer. 

1-(5-tert-butyl-2-phenyl-2H-pyrazol-3-yl)-3-[2-fluoro-4-(1-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-7-yloxy)-phenyl]-urea and related compounds and their use in therapy

The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g.,B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.

Pyrido[2,3-b]pyrazin-8-substituted compounds and their use

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (for convenience, collectively referred to herein as 'IP compounds'), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterised by (e.g., driven by) mutant RAS ('mutant RAS cancer'). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer. 

1-(5-tert-butyl-2-phenyl-2H-pyrazol-3-yl)-3-[2-fluoro-4-(1-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-B]pyridin-7-yloxy)-phenyl]-urea and related compounds and their use in therapy

The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.

Pyrido[2,3-B]pyrazin-8-substituted compounds and their use

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (I) (for convenience, collectively referred to herein as 'IP compounds'), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterized by (e.g., driven by) mutant RAS ('mutant RAS cancer'). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.

The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B&#x2014;RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.

The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.

Imidazo[4, 5-B]pyridin-2-one and oxazolo[4, 5-B] pyridin-2-one compounds and analogs thereof as cancer therapeutic compounds

The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B-RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formula (I): wherein: J is independently &#x2014;O&#x2014; or &#x2014;NR&#x2014;; R, if present, is independently &#x2014;H or a substituent; Ris independently &#x2014;H or a substituent; Y is independently &#x2014;CH&#x2550; or &#x2014;N&#x2550;; Q is independently &#x2014;(CH)&#x2014;M&#x2014;(CH)&#x2014; wherein: j is independently 0, 1 or 2; k is independently 0, 1, or 2; j+k is 0, 1, or 2; M is independently &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;NH&#x2014;, &#x2014;NMe&#x2014;, or &#x2014;CH&#x2014;; each of R, R, R, and Ris independently &#x2014;H or a substituent; and additionally Rand Rtaken together may be &#x2014;CH&#x2550;CH&#x2014;CH&#x2550;CH&#x2014;; L is independently: a linker group formed by a chain of 2, 3, or 4 linker moieties; each linker moiety is independently &#x2014;CH&#x2014;, &#x2014;NR&#x2014;, &#x2014;C(&#x2550;X)&#x2014;, or &#x2014;S(&#x2550;O)&#x2014;; exactly one linker moiety is &#x2014;NR&#x2014;, or: exactly two linker moieties are &#x2014;NR&#x2014;; exactly one linker moiety is &#x2014;C(&#x2550;X)&#x2014;, and no linker moiety is &#x2014;S(&#x2550;O)&#x2014;; or: exactly one linker moiety is &#x2014;S(&#x2550;O)&#x2014;, and no linker moiety is &#x2014;C(&#x2550;X)&#x2014;; no two adjacent linker moieties are &#x2014;NR&#x2014;; X is independently &#x2550;O or &#x2550;S; each Ris independently &#x2014;H or a substituent; A is independently: Ccarboaryl, Cheteroaryl, Ccarbocyclic, Cheterocyclic; and is independently unsubstituted or substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc. 

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Sutton, United Kingdom

Delphine Menard