Palobiofarma S.l.

Novartis Ag

Juan Alberto Camacho Gomez

Julio Cesar Castro-Palomino Laria

John Scott Cameron

Sanela Bilic

Danny Roland Howard, Jr

Lyhen Gonzalez Lio

Danny Roland Howard

Julio Cesar Castro- Palomino Laria

Adela Mendoza Lizaldez

Jr Danny Roland Howard

This invention relates to an active metabolite of 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimindin-4-amine that modulates the activity of adenosine A2a receptor. In particular, the present invention relates to pharmaceutical compositions comprising 1-(4-amino-5-bromo-6-(1H-pyrazol-1-yl)-pyrimidin-2-yl)-1H-pyrazol-4-ol, as well as processes for its preparation and its use in the treatment of cancer alone of in combination with one or more immunotherapeutic agents.

1-(4-amino-5-bromo-6-(1H-pyrazol-1-yl)pyrimidin-2-yl)-1H-pyrazol-4-ol and use thereof in the treatment of cancer

The present invention relates to 5-bromo-2,6-di-(1H-pyrazol-1-yl)pyrimidin-4-amine, its pharmaceutically acceptable salts and co-crystals thereof and to pharmaceutical compositions comprising said compounds for use in the treatment of cancer.

5-bromo-2,6-di-(1H-pyrazol-1-yl)pyrimidin-4-amine for use in the treatment of cancer

New 4-amino-pyrimidine derivatives as potent antagonists of the adenosine Areceptor formula (I): (I) The invention provides as well a method for preparing such compounds, pharmaceutical compositions comprising an effective amount of these compounds and the use of such compounds in the manufacture of a medicament to treat pathological affections that can be improved by antagonism of the adenosine Areceptor. 

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This compounds correspond to the formula (I), where: Rrepresents and aryl or heteroaryl group optionally substituted by one or more substituents selected from the group consisting of halogen atoms, straight or branched optionally substituted lower alkyl, cycloalkyl, hydroxy, straight or branched, optionally substituted lower alkoxy, cyano, or &#x2014;COR', wherein R&#x2032; represents a hydrogen atom or a straight or branched, optionally substituted lower alkyl group; Rrepresents a group selected from: a) a straight or branched lower alkyl group substituted by one or more carboxylic groups (&#x2014;COOH) and optionally substituted by one or more halogen atoms; b) a cycloalkyl group substituted by one or more carboxylic groups (&#x2014;COOH) and optionally substituted by one or more halogen atoms; c) a straight or branched alkylcycloalkyl or cycloalkylalkyl group substituted by one or more carboxylic groups (&#x2014;COOH) and optionally substituted by one or more halogen atoms. Formula (I). 

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Barcelona, Spain

Juan Alberto Camacho Gomez