Sanofi-a Ventis Deutschland Gmbh

Sanofi

Aventis Pharma Deutschland, Gmbh

Sanofi-aventis

Armin Hofmeister

Uwe Heinelt

Hans-Jochen Lang

Klaus Wirth

Oliver Plettenburg

Markus Bleich

Michael Gekle

Dieter Kadereit

Joachim Brendel

Stefan Peukert

Matthias Loehn

Heinz-Werner Kleemann

Hans Matter

Manfred Schudok

Jean-Christophe Carry

Sven Ruf

Hans-Willi Jansen

Aimo Kannt

Matthias Löhn

Peter Monecke

Serge Mignani

Kurt Ritter

Baptiste Ronan

Eugen Falk

Herman Schreuder

Marc Nazare

Antony Bigot

Stefan Guessregen

Nis Halland

Jean-Michel Altenburger

Tilo Weiss

Friedemann Schmidt

Yuri Ivashchenko

Matthias Dreyer

Thomas Licher

Uwe Schwahn

Matthias Lohn

Uwe Dietz

Kerstin Jahn-hofmann

Martin Bickel

Wendelin Frick

Katrin Lorenz

Jochen Goerlitzer

Max Hropot

Maxime Lampilas

John Weston

Joerg Czech

Hans-Ludwig Sch&auml;fer

Antonio Ugolini

Alexander Schiffer

Marc Nazaré

Christiane Metz-Weidmann

Markus Kohlmann

Kristin Breitschopf

Martin Hug

Bodo Brunner

Mike Helms

Sabine Scheidler

Pierrick Rival

The present disclosure relates to dsRNAs targeting ANGPTL8, methods of inhibiting ANGPTL8 gene expression, and methods of treating one or more conditions associated with ANGPTL8 gene expression.

RNA compositions and methods for inhibiting ANGPTL8

The present disclosure relates to novel nucleotide precursors and nucleotide analogs that can be incorporated into oligonucleotides, including double-stranded oligonucleotides such as siRNAs. Oligonucleotides containing these analogs have superior biological activity, for example, increased in vitro stability and improved in vivo potency especially duration of action. The improved oligonucleotides are useful for silencing (e.g., reducing or eradicating) the expression of a target gene. In particular embodiments, this invention encompasses specific nucleotide analogs to be included in double-stranded RNAs (dsRNAs), and especially in siRNAs, that can hybridize to messenger RNAs (mRNAs) of interest, so as to reduce or block the expression of target genes of interest. The present compounds have general formula (I), wherein each of Ra, Rb, Rc and Rd is independently, H or a (C1-C6) alkyl group and B is a heterocyclic nucleobase.

Nucleotide precursors, nucleotide analogs and oligomeric compounds containing the same

The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]sulfonamides as pharmaceuticals

The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula (I), (R2)n wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them. 

N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides and their use as pharmaceuticals

The invention relates to 6-cyclohexylamine-substituted isoquinolone derivatives of the formula (I) or isoquinoline derivatives of the formula (I') useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.

Cyclohexylamine isoquinolone derivatives

The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.

Substituted isoquinoline and isoquinolinone derivatives

The invention relates to 6-substituted isoquinolone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.

Cycloalkylamine substituted isoquinolone derivatives

The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.

Isoquinoline derivatives

The invention relates to 6-substituted isoquinoline derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.

Cycloalkylamine substituted isoquinoline derivatives

Cyclohexylamin isoquinolone derivatives

A method for the treatment or prevention in a mammal of a disease associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase comprising administering to the mammal in need thereof at least one compound of the formula (I). 

Substituted isoquinoline and isoquinolinone derivatives as inhibitors of Rho-kinase

The invention relates to 6-piperidinyl-substituted isoquinolone derivatives of the formula (I) or isoquinoline derivatives of the formula (I') useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.

Piperidinyl-substituted isoquinolone derivatives

This invention is directed to the compound of formula (I), compositions containing said compounds to inhibit the sodium-proton exchanger of subtype 3 (NHE3) which are useful in the prevention or treatment of various disorders in a patient suffering from a disease state, such as, renal disorders including acute or chronic renal failure, disorders of biliary function and for respiratory disorders such as snoring or sleep apnea or for stroke.

N-substituted (benzoimidazol-2-yl)phenylamines, processes for their preparation, their use as a medicament or diagnostic aid, and a medicament comprising them

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Oppenheim, Germany

Armin Hofmeister