Novartis Ag

Novatis Ag

Andreas Marzinzik

Pascal Furet

Paul William Manley

Joseph Schoepfer

Bahaa Salem

Robert Martin Grotzfeld

Wolfgang Jahnke

Darryl Jones

Xavier Francois Andre Pelle

Philipp Grosche

Nils Ostermann

Saliha Moussaoui

Werner Breitenstein

Stefanie Flohr

Keiichi Masuya

Claus Ehrhardt

Edgar Jacoby

Alec Nathanson Flyer

Mohindra Seepersaud

Josef Gottfried Meingassner

Stephanie Kay Dodd

Fumiaki Yokokawa

Lauren Gilchrist Monovich

Juergen Klaus Maibaum

Ian Lewis

Takanori Kanazawa

Stefan Andreas Randl

Tajesh Jayprakash Patel

Andrei Alexandrovich Golosov

Kazuhide Konishi

Ulrich Hassiepen

Shimpei Kawakami

Juerg Zimmermann

Eugene Yuejin Liu

Ursula Bodendorf

Bernd Gerhartz

Frederic Berst

Claus Erhardt

Johannes Ottl

Patrick Crawford Reid

Erich Alois Spieser

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 present invention relates to compounds of formula (I): 

Benzamide derivatives for inhibiting the activity of ABL1, ABL2 and BCR-ABL1

The present invention relates to compounds of formula I: 

Compounds and compositions for inhibiting the activity of ABL1, ABL2 and BCR-ABL1

The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers. 

The present invention relates to compounds of formula I: in which Y, Y, Y, Y, Y, R, R, Rand Rare defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers. 

The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers. 

The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.

Kallikrein 7 modulators

The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The preferred compounds (which can also be present as salts) have the formula I wherein R1, R2, T, R3 and R4 are as defined in the specification. 

Organic compounds

Growing community of inventors

Weil, Germany

Andreas Marzinzik