Novartis Ag

Sloan-kettering Institute for Cancer Research

Samuel Hintermann

Samuel J Danishefsky

Philip O Livingston

Peter W Glunz

Govindaswami Ragupathi

Dalibor Sames

Scott D Kuduk

Lawrence Williams

Bastian Hengerer

Kenneth O Lloyd

Konstanze Hurth

Aleksandar Stojanovic

Xiao-Tao Chen

Yves Auberson

Dirk Behnke

Claudia Betschart

Vinod Shashikant Chaudhari

Simona Cotesta

Henrik Moebitz

Chetan Pandit

Nicolas Soldermann

Sangamesh Badiger

Murali Chebrolu

Xiao Tao Chen

Kaspar Zimmermann

Jacob Bradely Schwarz

Sébastien Jacquier

Arndt Meyer

Zhenxing Du

Jacob B Schwartz

Ulrike Von Krosigk

Hansjoerg Lehmann

Boris Schmidt

Valery Kudryashov

Sangamesch Badiger

Simona Costesta

Provided are substituted quinazolin-4-one compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein R, R, R, R, Rand L are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the class I PI3K kinases. 

Substituted quinazolin-4-one derivatives

The invention relates to compound of the formula (I') in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it. 

Disubstituted heteroaryl-fused pyridines

The present invention relates to novel benzo[1,2,5]oxadiazoles and benzo[1,2,5]thiadiazoles of formula (I) wherein X is O or S, Ris 5-(2-fluoro-ethylamino)-thiazol-2-yl, 5-(2-F-ethylamino)-thiazol-2-yl or a group of formula (a) wherein Y is CH or N, Ris NHCH, NHCH, N(CH)CH, N(CH), N(CH), NH(CH)F, NH(CH)F, N(CH)(CH)F, N(CH)&#x2014;(CH)F, O&#x2014;(CH)F, O&#x2014;(CH)F, CONH(CH)nF or CONH(CH)F (n being in each case 2 to 4) and Ris hydroxy, (C1-4)alkoxy, hydrogen or nitro, in free base or acid addition salt form; their preparation, their use as markers in diagnosis and compositions containing them.

Benzo[1,2,5]oxadiazoles and benzol[1,2,5]thiadiazoles useful as histopathological staining agents, imaging agents and biomarkers

The present invention provides novel glycoconjugates such as glycopeptides, as well as convergent methods for the synthesis thereof. An exemplary preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the glycoconjugates of the invention.

Glycopeptide conjugates and uses thereof

The present invention relates to compounds of formula (I): wherein Ris hydroxy, Calkoxy, amino, Calkyl-amino, di Calkylamino, benzyloxy or C-Calkanoyl, Ris Calkyl, Calkoxy, Calkoxy Calkoxy, CF, halogen, Calkylamino, di Calkylamino, di Calkylamino Calkoxy or N&#x2014;Calkoxy Calkyl-N&#x2014;Calkylamino, N&#x2014;Calkyl-piperazinyl, morpholinyl or pyrrolidinyl-Calkoxy, wherein the Calkyl radicals in Rare optionally further substituted by Calkyl, halogen, cyano, amino, alkoxy or alkylthio, X is N or O, Y is N, O or CH, Z is N or CH, and W is N or CH, provided that (a) Ris not hydroxy or Calkoxy when Ris CF, X is O, Y is CH, Z is N and W is CH, (b) Ris not hydroxy or Calkoxy when Ris CFor chloro, X is N, Y is O, Z is CH and W is CH, (c) Ris not hydroxy when Ris CF, X is O, Y is N, Z is CH and W is CH and (d) X and Y are not simultaneously O, the salts thereof; their preparation, their use and pharmaceutical compositions containing them. 

Heterocyclic compounds useful as Nurr-1 activators

The present invention provides novel &#x3b1;-O-linked glycoconjugates such as &#x3b1;-O-linked glycopeptides, as well convergent methods for synthesis thereof. The general preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the &#x3b1;-O-linked glycoconjugates.

&#x3b1;-O-linked glycoconjugates, methods of preparation and uses thereof

The invention provides compounds of formula I, wherein X, Y, R, R, and Rare as defined in the description, and the preparation thereof. The compounds of formula I are useful as pharmaceuticals.

Isoxazolopyridinones

The present invention provides novel &agr;-O-linked glycoconjugates such as &agr;-O-linked glycopeptides, as well convergent methods for synthesis thereof. The general preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the &agr;-O-linked glycoconjugates.

&agr;-O-linked glycoconjugates, methods of preparation and uses thereof

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Basel, Switzerland

Samuel Hintermann