Novartis Ag

Ian Lewis

Rainer Albert

Wilfried Bauer

Gisbert Weckbecker

Christian Bruns

Bernhard Wietfeld

David Bodmer

Mark Meisenbach

Heribert Hellstern

Pascal Furet

Frederic Zecri

Nicolas Soldermann

Alexander Baxter Smith

Giorgio Caravatti

Konstanze Hurth

Sylvie Chamoin

Henrik Moebitz

Gebhard Thoma

Philipp Grosche

Nigel Graham Cooke

Alec Nathanson Flyer

Mohindra Seepersaud

Frank Stowasser

Lauren Gilchrist Monovich

Anette Von Matt

Andreas Marzinzik

Tajesh Jayprakash Patel

Andrei Alexandrovich Golosov

Frédéric Stauffer

Nicola Tufilli

Gregory John Hollingworth

Christina Hebach

Frédéric Zecri

Ivo Felner

Romain Wolf

Karen Kammertoens

Klemens Hogenauer

Rolf Baenteli

Markus Streiff

Eugene Yuejin Liu

Ross Strang

Hans-Günter Zerwes

Jiri Kovarik

Paulo Antonio Fernandes Gomes Dos Santos

Klemens Hoegenauer

Fraser Glickman

Christoph Kalis

Nicola Tuffilli

Nagarajan Chandramouli

Johannes Ottl

Patrick Crawford Reid

Klemens Högenauer

The disclosure relates to inhibitors of PCSK9 useful in the treatment of lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I):

Cyclic peptides as proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors for the treatment of metabolic disorders

The invention relates to new uses of PI3K inhibitors, wherein said inhibitors have an inhibitory action on the PI3K isoform delta for the treatment of immunopathology in a subject suffering from a disease or disorder selected from malaria, leishmaniasis, trypanosomiasis, toxoplasmosis and/or neurocysticercosis, via functional inhibition of TLR9 of the infected subject.

Use of inhibitors of the activity or function of PI3K

The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R, R, Rand Rare 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 PI3K enzymes.

Dihydro-benzo-oxazine and dihydro-pyrido-oxazine derivatives

The invention provides cyclo[{4-(NH&#x2014;CH&#x2014;NH&#x2014;CO&#x2014;O&#x2014;)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.

Somatostatin analogues

The invention provides cyclo[{4-(NH&#x2014;CH&#x2014;NH&#x2014;CO&#x2014;O-)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.

Disclosed are ergoline derivatives, Formula (I), wherein either each of Rand R, independently, is H; optionally Rand/or R-substituted-phenyl or -phenyl-Calkyl; optionally Rand/or R-substituted-heteroaryl or -heteroaryl-Calkyl; optionally Rand/or R-substituted heteroaryl N-oxide; optionally R-substituted C-Calkyl; optionally R-substituted C-Calkenyl, optionally R-substituted C-Calkynyl; optionally R-substituted C-Ccycloalkyl, or optionally R-substituted C-Ccycloalkenyl; or Rand Rform together with the nitrogen atom to which they are attached an optionally R-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; Ris H; OR; CHRR; (CH)NRR; CH&#x2014;CH&#x2014;OR; CH&#x2014;CO&#x2014;NRR; or CO&#x2014;CHRR; Ris F; Cl; Br; I; OR; NRRor has one of the significances given for R; and Rhas one of the significances given for R, in free form or in salt form for preventing or treating disorders or diseases mediated by interactions between chemokine receptors and their ligands. 

Ergoline derivatives

Somatostain analogues comprising the amino acid sequence of the formula (I): -(D/L)Trp-Lys-X,-X,, wherein X,is a substituted Thr, Ser, Tyr, Glu or Cys residue and X,is an &agr;-amino acid having an aromatic residue on the C,side chain, or an amino acid unit selected from Dab, Dpr, Dpm, His (Bzl)HyPro, thienyl-Ala, cyclohexyl-Ala and t.-butyl-Ala, the residue Lys of said sequence corresponding to the residue Lys,of the native somatostatin-14, in free form, in salt form or complexed with a detectable element have interesting pharmacological properties.

Somatostatin peptides

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Riehen, Switzerland

Ian Lewis