Piqur Therapeutics Ag

Vandria Sa

Universitat Basel

Universitaet Basel

Torqur Ag

University of Pennsylvania

Torqur

Florent Beaufils

Paul Hebeisen

Christopher Rinsch

Eileen Mary Seward

Jonathan Mark Sutton

Penelope Andreux

Jean-Baptiste Langlois

Peter C Sennhenn

Thomas Christian Fessard

Said Oumouch

Ian Linney

Jamie D Knight

Doriano Fabbro

Matthias Wymann

Vladimir Cmiljanovic

Denise Rageot

Thomas Bohnacker

Alexander Sele

John T Seykora

Petra Hillmann-Wuellner

Anton Stuetz

Wolfgang Loscher

Petra Hillmann-Wüllner

Eileen Jackson

Wolfgang Löscher

Hoa Huu Phuc Nguyen

Claudia Brandt

Petra Hillmann-Wullner

Hoa Huu Nguyen

Alexander Markus Sele

Disclosed are compounds, compositions, and methods useful for treating neuronal and mitochondrial diseases.

Urolithin derivatives and methods of use thereof

The present invention is relates to a compound of formula (I), wherein X, Xand Xare, independently of each other, N or CH; with the proviso that at least two of XXand Xare N; Y is N or CH; W is H or F; with the proviso that when W is F, then X, Xand Xare N; Rand Rare independently of each other (i) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein Rand Rare independently of each other H, C-Calkyl optionally substituted with one or two OH, C-Cfluoroalkyl, C-Calkoxy, C1alkoxyC-Calkyl, CN, or C(O)O—C-Calkyl; or Rand Rform together a bivalent residue —RR— selected from C-Calkylene optionally substituted with 1 to 4 F, —CH—O—CH—, —CH—NH—CH—, or any of the structures wherein the arrows denote the bonds in formula (II); or (ii) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R; wherein Ris independently at each occurrence C-Calkyl optionally substituted with one or two OH, C-Cfluoroalkyl, C-CalkoxyC-Calkyl, C-Ccycloalkyl; or two Rsubstituents form together a bivalent residue-RR— selected from Ci-C3alkylene optionally substituted with 1 to 4 F, —CH—O—CH— or —O—CHCH—O—; with the proviso that at least one of Randis a morpholinyl of formula II; and prodrugs, metabolites, tautomers, solvates and pharmaceutically acceptable salts thereof, for use in the prevention or treatment of a skin lesion in a subject.

Treatment of skin lesions

The present invention is relates to a compound of formula (I),

Treatment of neurological disorders

The invention relates to novel phosphoinositide 3-kinase (PI3K), mammalian target of rapamycin (mTOR) and PI3K-related kinase (PIKKs) inhibitor compounds of formula (I), wherein X, Xand Xare N or CH, with the proviso that at least two of X, Xand Xare N; Y is N or CH, These compounds are useful, either alone or in combination with further therapeutic agents, for treating disorders mediated by lipid kinases.

Difluoromethyl-aminopyridines and difluoromethyl-aminopyrimidines

The present invention is relates to a compound of formula (I), wherein wherein the arrow denotes the bond in formula (I); andwherein Rand Rare independently of each other H, C-Calkyl optionally substituted with one or two OH, C-Cfluoroalkyl, C-Calkoxy, C-CalkoxyC-Calkyl, CN, or C(O)O&#x2014;C-Calkyl; or Rand Rform together a bivalent residue &#x2014;RR&#x2014; selected from C-Calkylene optionally substituted with 1 to 4 F, &#x2014;CH&#x2014;O&#x2014;CH&#x2014;, &#x2014;CH&#x2014;NH&#x2014;CH&#x2014;, or any of the structures wherein the arrows denote the bonds in formula (II); or

The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I) wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.

Manufacturing process for triazine, pyrimidine and pyridine derivatives

The invention relates to novel phosphoinositide 3-kinase (PI3k), mammalian target of rapamycin (mTOR) and PI3k-related kinase (PIKKs) inhibitor compounds of formula (I), wherein X, Xand Xare N or CH, with the proviso that at least two of X, Xand Xare N; Y is N or CH, These compounds are useful, either alone or in combination with further therapeutic agents, for treating disorders mediated by lipid kinases.

The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I), wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form. 

The invention relates to novel phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor compounds of formula (I) and (II), which are conformationally restricted, and for which the meaning of the substituents are listed in the description. Preferred compounds are those wherein X isoxygen, Ris morpholino and Ris substituted phenyl or heteroaryl. These compounds are useful, either alone or in combination with further therapeutic agents, for treating disorders mediated by lipid kinases. 

Conformationally restricted P13K and mTOR inhibitors

Growing community of inventors

Bartenheim, France

Florent Beaufils