Fundacion Para La Investigacion Medica Aplicada

Fundación La Investigación Médica Aplicada

Maria Obdulia Rabal Gracia

Julen Oyarzabal Santamarina

Juan José Lasarte Sagastibelza

Inés Noelia Casares Lagar

María Del Mar Cuadrado Tejedor

Juan Antonio Sánchez Arias

Ana María García Osta

Xabier Aguirre Ena

Felipe Prósper Cardoso

Teresa Lozano Moreda

Edurne San José Enériz

Ana Ugarte Baztán

Juan Roberto Rodríguez Madoz

Rafael Franco Fernández

Juan Roberto Rodriguez Madoz

Felipe Prosper Cardoso

Ana María GARCÍA Osta

Edurne San Jose Eneriz

The present invention provides peptides of general formula (I) and salts thereof, wherein: Rand R, taken together, form a birradical linker; and R' is hydrogen; or, alternatively, Ris selected from hydrogen, &#x2014;C(&#x2550;O)&#x2014;CH&#x2014;NH&#x2014;C(&#x2550;O)&#x2014;(C-C)alkyl, and &#x2014;C(&#x2550;O)&#x2014;(C-C)alkyl; one of Rand R&#x2032; is hydrogen and the other is selected from &#x2014;C(&#x2550;O)NRR, and &#x2014;C(&#x2550;O)OH; and Rand Rare same or different and are selected from hydrogen and (C-C)alkyl. These peptides are highly efficient in binding and inhibiting FoxP3, being efficient in inhibiting and blocking Treg cell functionality, which make them useful in the treatment of cancer. The present invention also provides constructs comprising the peptide of formula (I) as well as combinations comprising the peptide of formula (I), the construct or both. 

FOXP3-binding peptides and uses thereof

FoxP3-binding peptides and uses thereof

It relates to the compounds of formula (I), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, wherein A, R, R, and Rare as defined herein, which are inhibitors of one or more DNMTs selected from the group consisting of DNMT1, DNMT3A and DNMT3B. It also relates to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of cancer, fibrosis and/or immunomodulation. 

Compounds as inhibitors of DNA methyltransferases

Novel compounds for use in cognition improvement It relates to certain compounds having a polycyclic structure and a &#x2014;(C&#x2550;O)NRRmoiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurode-generative diseases.

Compounds for use in cognition improvement

It relates to the use of compounds of formula (I'), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, as anticancer agents and as agents for generating induced pluripotent stem cells. Compounds of formula (I&#x2032;), wherein R&#x2032; is an alcoxy group, a hydrocarbon chain or a ring system, and R, R, and Rare as defined herein, are dual inhibitors of histone methyltransferases and DNA methyltransferases. It also relates to the compounds of formula (I&#x2032;), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, wherein R&#x2032; is phenyl or 5- to 6-membered heteroaromatic ring, both optionally fused to another rings (i.e., compounds of formula (I)). It also relates to pharmaceutical or veterinary compositions containing compounds of formula (I). 

Compounds as dual inhibitors of histone methyltransferases and DNA methyltransferases

It relates to certain compounds having a polycyclic structure and a hydroxamic acid moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to a process for their preparation, as well as to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurodegenerative diseases. wherein Bis a radical selected from the group consisting of formula (A&#x2033;), formula (B&#x2033;), formula (C&#x2033;), and formula (D&#x2033;): 

Compounds as dual inhibitors of phosphodiesterases and histone deacetylases

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Pamplona, Spain

Maria Obdulia Rabal Gracia