Oryzon Genomics S.a.

Almirall, S.a.

Alberto Ortega Muñoz

Matthew Colin Thor Fyfe

Carlos Puig Duran

Marc Martinell Pedemonte

Julio Cesar Castro-Palomino Laria

Nuria Valls Vidal

Julio Cesar Castro Palomino Laria

Guido Kurz

Maria De Los Àngeles Estiarte Martinez

Tamara Maes

Silvia Gual Roig

Maria Isabel Crespo Crespo

Maria De Los Ángeles Estiarte-Martinez

Nathalie Guibourt

Iñigo Tirapu Fernandez De La Cuesta

Cristina Mascaro Crusat

Elena Carceller González

Jonathan Alleman Baker

Jordi Bach Tana

María De Los Ángeles Estiarte Martínez

Maria De Los Ángeles Estiarte-Martínez

Núrla Valls Vidal

Julio Castro-Palomino Lária

Maria De Los Ángeles Estiarte Martinez

Matthew Colin Fyfe

Maria De Estiarte-Martinez

Inigo Tirapu Fernandez De La Cuesta

The invention relates to methods to determine KDM1A target engagement and chemoprobes useful therefor. In particular, the invention relates to non-peptidic KDM1A chemoprobes carrying a tag or label that can be used to assess KDM1A target engagement in cells and tissues. These chemoprobes can also be used to identify KDM1A interacting factors and analyze expression levels of KDM1A.

Methods to determine KDM1A target engagement and chemoprobes useful therefor

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. 

(Hetero)aryl cyclopropylamine compounds as LSD1 inhibitors

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX). 

Arylcyclopropylamine based demethylase inhibitors of LSD1 and their medical use

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. 

The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A'), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A&#x2032;) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, &#x2014;CHC(=0)NH, heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is &#x2014;NH&#x2014;; (L) is chosen from a single bond, &#x2014;CH&#x2014;, &#x2014;CHCH&#x2014;, &#x2014;CHCHCH&#x2014;, and &#x2014;CHCHCHCH&#x2014;; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from &#x2014;NH, &#x2014;NH(C-Calkyl), &#x2014;N(C-Calkyl)(C-Calkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A&#x2032;)X-(A)-(B)&#x2014;(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer.

Lysine specific demethylase-1 inhibitors and their use

The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection. 

Cyclopropylamine derivatives useful as LSD1 inhibitors

The present invention relates to the use of potent selective LSD inhibitors and LSD/MAO-B inhibitors for treating or preventing viral infections. Furthermore, the present invention relates to the new use of cyclopropylamine acetamide derivatives or cyclopropylamine derivatives, as defined herein, for treating or preventing viral infection and treating or preventing reactivation of a virus after latency.

Potent selective LSD1 inhibitors and dual LSD1/MAO-B inhibitors for antiviral use

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. 

The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A'), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A&#x2032;) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, &#x2014;CHC(&#x2550;0)NH, heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is &#x2014;NH&#x2014;; (L) is chosen from a single bond, &#x2014;CH&#x2014;, &#x2014;CHCH&#x2014;, &#x2014;CHCHCH&#x2014;, and &#x2014;CHCHCHCH&#x2014;; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from &#x2014;NH, &#x2014;NH(C-Calkyl), &#x2014;N(C-Calkyl)(C-Calkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A&#x2032;)X-(A)-(B)&#x2014;(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer.

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Barcelona, Spain

Alberto Ortega Muñoz