Centre National De La Recherche Scientifique

Other

Université Paris Descartes

Université De Rennes 1

The University of Texas System

Commissariat a L'energie Atomique Et Aux Energies Alternatives

Institut National De La Sante Et De La Recherche Medicale

The University of Chicago

Universite Claude Bernard – Lyon1

Université De Poitiers

The Rockefeller University

Assistance Publique-hopitaux De Paris

Sorbonne Université

Université Pierre Et Marie Curie

Université Claude Bernard Lyon I

Laurent Meijer

Nassima Oumata

Peter G Schultz

Nathanael S Gray

Sung-Hou Kim

David J Lockhart

Miroslav Strnad

Paul Greengard

Conrad Kunick

Karima Bettayeb

Emile R Bisagni

Michel Legraverend

Philip Cohen

Edward A Sausville

Thomas B Albrecht

Lisa Wodicka

Gérald Guillaumet

Peter Gregory Goekjian

Pascal George

Hervé Galons

Frédéric Becq

Amaury Patin

Yvette Mettey

Rick Gussio

Herve Galons

Aloïse Mabondzo

Benoit Joseph

Luc Demange

Ravi Kumar Jalluri

Florence Popowycz

Christian Berthou

Leandros Skaltsounis

Anne-Cécile Guyot

Serge Timsit

Deborah J Nelson

Jean-Michel Vierfond

Karine Lester

Carl Hirschie Johnson

Charlotte Leuxe

François Liger

Daniel W Zaharevitz

Wade Bresnahan

Aubrey E Thompson

Emmanuel Deau

Frédéric Miege

Judit Ribas

Jacint Boix

Aida Gabdoulkhakova

Bénédicte Menn

Vladimir Riazanski

Marc Flajolet

Philippe Olivier Belmont

Johann Bosson

Emmanuel Mikros

Prokopios Magiatis

Francois Carreaux

Jean-Pierre Bazureau

Steven Renault

Olivier Lozach

Alexios-Le-Andros Skaltsounis

Prokopios Maglatis

Carl Johnson

Sylvain César Léonce Routier

Mattéo Chiurato

Carl Dept Of Biological Sciences U-8212 BSB/MRB Iii Johnson

Rajâa Boulahjar

Benoït Joseph

Stéven Renault

François Carreaux

Deborah Nelson

Benoît Joseph

Bernard Marquet

Virginie Vauthier

Thomas Falguieres

The present invention relates to a compound of formula (I) wherein Rrepresents a (C-C)alkyl group, a spiro(C-C)bicyclic ring, a fused phenyl group, a substituted phenyl group, a R'-L- group, wherein L is either a single bond or a (C-C)alkanediyl group, and R′ represents a (C-C)cycloalkyl group, abridged (C-C)cycloalkyl group, a (C-C)heterocycloalkyl group, or a (C-C)heteroaryl group, or a R′-L- group wherein L is a (C-C)alkanediyl group, and R′ is an optionally substituted phenyl group, and wherein Rrepresents a hydrogen atom or a (C-C)alkyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates. It also relates to said compound for use as a medicament, in particular in the treatment and/or prevention of cognitive deficits associated with Down syndrome; Alzheimer's disease; dementia; tauopathies; Parkinson's disease; CDKL5 Deficiency Disorder; Phelan-McDermid syndrome; autism; type 1 and type 2 diabetes; abnormal folate and methionine metabolism; osteoarthritis; Duchenne muscular dystrophy; several cancers; neuroinflammation, anemia and viral and unicellular infections and for regulating body temperature.

Imidazolone derivatives as inhibitors of protein kinases in particular DYRK1A, CLK1 and/or CLK4

Compound of formula (I) and its addition salts with pharmaceutically acceptable acids, and methods in which an effective amount of the compound or any pharmaceutically acceptable salt thereof is administered (as a medicament) to an individual in need thereof.

Purine derivatives for use as medicament and for use in treating neurodegenerative or neuro-inflammatory disorders

A method for treatment of disease by reduction in macrophages-mediated bacterial killing, including administration to patients in need a compound of formula (I): wherein A is N or CH; B is NO, or S; Ris H, (C-C)alkyl group, methyl(C-C)cycloalkyl group or (C-C)cycloalkyl group; Ris an aryl, arylmethyl group or methylheteroaryl group as methylpyridine and methylthiophene; Ris absent when B is O or S, or is H or (C-C)alkyl group when B is N; Ris (C-C)alkyl group or (C-C)cycloalkyl group, groups bearing a carboxylic acid group, and (C-C)alkyl group or (C-C)cycloalkyl substituted by hydroxyl group, halogen group or methoxy group, when B is N, Rand Rcan together form a 5- or 6-membered heterocycle substituted by carboxylic acid group, substituted by a halogen atom, hydroxyl group, methoxy group or hydroxymethyl group, or pharmaceutically acceptable salt. Also provided are new compounds relating to this use.

Purine derivative compounds for medical use

The invention relates to kinase inhibitors of the formula (I) in which &#x2014;Rto R&#x2550;H; ether or polyether, amino; NO; NH-carbamate; NH&#x2014;CO&#x2014;R, with R such as defined above; Nand derivatives thereof of the 1,2,3-triazole type; &#x2014;R=&#x2014;OH; halogen; &#x2014;OR with R such as defined above; OH-carbamate; OH-carbonate; NH, NH-carbamate; NH&#x2014;CO&#x2014;R, with R such as defined above; Nand derivatives thereof of the 1,2,3-triazole type; N(R,R); &#x2014;R'&#x2550;H or a C1-C12 alkyl, &#x2014;R&#x2550;H; R; (R or R&#x2032;)&#x2014;Si, with R such as defined above; optionally substituted aryl, heteroaryl; halogen (iodine); alkynyl; &#x2014;Rand R&#x2550;H, C-Calkyl; &#x2014;Rand R&#x2550;H, R (or R&#x2032;) such as defined above. These compounds can be used as kinase inhibitors in particular for treating cancer.

Tetrahydrocyclopenta[c]acridine derivatives as kinase inhibitors and biological

Indirubin derivatives of formula (I) wherein R represents -(A)- Ror &#x2014;CO&#x2014;N(R,R) with &#x2022;A being C1-C5 alkylene group, optionally substituted by one or several Aradical, Abeing an halogen Br, OH, ORor NH, Rbeing C1-C5 alkyl; &#x2014;Rbeing halogen, OH, N(R, R); Rand R, identical or different, being C1-C5 alkyl, optionally substituted by Asuch as above defined, or Rand Rare part of a cycle with 5 or 6 elements optionally comprising another heteroatom such as O or N; &#x2022;n=1&#x2212;5. It also relates to the biological application thereof. 

3',6-substituted indirubins and their biological applications

A compound of formula (I), or a pharmaceutically acceptable salt thereof, where Ris a (C-C)alkyl or (C-C)cycloalkyl group; Ris a (C-C)alkyl, (C-C)cycloalkyl, (C-C)alkenyl, (C-C)fluoroalkyl, (C-C)fluoroalkoxy, or (C-C)alkoxy(C-C)alkyl group, substituted: (i) with one to three hydroxyl groups, or (ii) with an NRRgroup, where Rand Rare independently a hydrogen atom or a (C-C)alkyl group; or a pyrrolidinylmethyl group substituted with one to three hydroxyl groups; Ris the same as Ror hydrogen; the Rand Rgroups independently being substitutable with an &#x2014;OCORgroup, where Ris a natural or unnatural amino acid derivative or a piperidyl group; alternatively, Rand Rtogether form a heterocyclic compound; X and Y are independently a substitutable phenyl or heteroaryl group, the heteroaryl group being a thienyl, pyridyl, pyrimidinyl, thiazolyl, pyrrolyl, or furanyl group; and Ris a hydrogen or a (C-C)alkyl group.

[object Object]

Imidazolone derivatives, as medicaments, of formula wherein:

Imidazolone derivatives, method for the preparation thereof and biological applications

The invention relates to new 3'-, 7-substituted-indirubins of formula (I) wherein R represents N&#x2014;OH, N&#x2014;O-alkyl or N&#x2014;O&#x2014;CO-alkyl, NO&#x2014;(R)-Het, N&#x2014;O&#x2014;(Y)&#x2014;N RR, N&#x2014;O&#x2014;CO&#x2014;N(RR), radical with Het representing an aliphatic nitrogeneous heterocycle, Y being an optionally substituted &#x2014;CH&#x2014; radical, n1 being 1 to 3, and X is an halogen atom selected in the group comprising F, Cl, Br, I, and Z is H or CHand the salts thereof. 

7-substituted indirubin-3'oximes and their applications

The invention relates to the use of purine derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives being of formula (I): where R2, R6 and R9, independently=halogen, a R&#x2014;NH&#x2014;, R&#x2014;NH&#x2014;NH&#x2014;, NH&#x2014;R'&#x2014;NH or R&#x2014;NH&#x2014;R&#x2032;&#x2014;NH&#x2014; group, where R=straight or branched chain saturated or unsaturated alkyl, aryl, cycloalkyl, or heterocyclyl group, R&#x2032;=straight or branched chain, saturated or unsaturated alkylene, arylene or cycloalkylene, R and R&#x2032; each include 1 to 8 carbon atoms optionally substituted with one or more &#x2014;OH, halogen, amino or alkyl groups, R2 furthermore may be a heterocycle optionally with a straight or branched chain saturated or unsaturated alkyl, aryl or cycloaryl or a heterocycle optionally substituted by one or more &#x2014;OH, halogen, amino or alkyl groups, R9 furthermore may be a straight or branched chain saturated or unsaturated alkyl, aryl or cycloalkyl and R2 and R9 furthermore may be hydrogen with the exception of 2-(2-hydroxyethylamino)-6-benzylamino-9-methylpurine.

Use of purine derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells

The invention relates to trisubstituted or tetrasubstituted imidazo[4,5b]pyridines, to their uses as well as to a process for manufacturing them. The compounds of the invention are imidazo[4,5b]pyridines. The first general synthesis of 3,5,7 imidazo[4,5b]pyridines is disclosed in the description. The invention founds application, in particular, in the pharmaceutical field.

Perharidines as CDK inhibitors

At least one compound of following formula I: 

Use of purine derivatives for the manufacture of a medicament

The present invention relates to the use of 6-(benzyl-amino)-2(S)-[[1-(hydroxymethyl) propyl]amino]-9-isopropylpurine) or at least one of its pharmaceutical acceptable salts for manufacturing a medication intended for the prevention and/or treatment of neurological diseases, in particular associated with neurological lesions.

Administration of (S)-roscovitine for protection against and/or treatment of neurological diseases

This invention provides 2-, 6, and 9-substituted purine derivatives, particularly 2(1-R hydroxymethylpropylamino)-6-benzylamino-9-isopropyl purine, having, in particular, antiproliferative properties, and suitable for use as pharmaceutical compositions and herbicidal compositions. Also provided are pharmaceutical compositions and herbicidal compositions comprising the 2-, 6, and 9-substituted purine derivatives, and methods of treatment using the 2-, 6, and 9-substituted purine derivatives.

Purine derivatives having, in particular, anti-proliferative properties, and their biological uses

The invention relates to pyrrolo[2,3b]-pyrazine derivatives having the general Formula (I) wherein R2 and R3 are identical or different and represent H, C1-C6 alkyl, said alkyl being a straight or branched-chain alkyl, which can be substituted, R6 is an optionally substituted aromatic cycle Ar or a cycloalkyl, said cycloalkyl being optionally substituted by an aryl group which can also be substituted, R7 is H, C1-C6 alkyl, (alk.)n-hal., CH2-CH&#x2550;CH2, CH2-cycloalkyl, CH2-Ar, with 'alk.' being a C1-C6 alkylene group, n being 1-6, Z is H or CH3. Application as active principle of pharmaceutical compositions, particularly for treating or preventing neurodegenerative disorders and proliferative disorders.

Derivatives of pyrrolo-pyrazines having a kinase inhibitory activity and their biological applications

The invention relates to paullone derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives being of general formula (1): wherein X&#x2550;C&#x2550;O, C&#x2014;S&#x2014;CH, C&#x2014;S, &#x2014;C&#x2014;NHOH, Z&#x2014;C or N, Y&#x2014; with the adjacent ring, a phenyl or thienyl group, the ring(s) of said derivatives being optionally substituted with one or more halogen atoms, hydroxy, alkylenehydroxy, alkynealkylenehydroxy, alkynehydroxycyclohexyl, alkyl, alkoxy, alkylenealkoxy, or alkylenecyano groups where the alkylene group is either saturated or unsaturated, the groups having a straight or branched chain with C1 to C18, said chain being optionally substituted with one or more hydroxy or amino groups, or one or more trifluoromethyl, &#x2014;COM, &#x2014;COOM, or &#x2014;CHCOOM groups (where M=H, C1 to C18 straight or branched chain alkyl, optionally substituted with one or more hydroxy and/or amino groups) nitroso, or cyano, R&#x2550;H, or C1 to C5 alkyl and R&#x2550;H, or &#x2014;C&#x2014;CO&#x2014;(CH)and the physiologically-acceptable salts and derivatives thereof.

Use of paullone derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells

Growing community of inventors

Roscoff, France

Laurent Meijer