Xenon Pharmaceuticals Inc.

Novartis Pharma Ag

Xenon Genetics Inc.

Michael D Winther

Heinz W Gschwend

Shaoyi Sun

Serguei Sviridov

Rajender Kamboj

Shifeng Liu

Vishnumurthy Kodumuru

Melwyn A Abreo

Wenbao Li

Chi Tu

Daniel F Harvey

Zaihui Zhang

Mark W Holladay

Nagasree Chakka

Vandna Raina

Mikhail Kondratenko

Sultan Chowdhury

Mikhail A Chafeev

Jian-Min Fu

Duanjie Hou

Mark Gray-Keller

Mehran Seid Bagherzadeh

Sengen Sun

Cindy J Hudson

Yigal Paul Goldberg

Andreas Billich

Roberto Justo De Antueno

Solomon O Nwaka

D Kenneth Jenkins

Andre Ponton

Stephen John Allen

Martin Haardt

Leah Christine Knickle

Richard Masten Fine

Boris Klebansky

Robert Fraser

Kashinath Sadalapure

Y Paul Goldberg

Mikhail A Kondratenko

Jian-min Fu

Mikhail Chafev

Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): 

Pyridyl derivatives and their use as therapeutic agents

Piperazine derivatives as stearoyl-coa desaturase inhibitors and their use as therapeutic agents

Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human include administering to a mammal in need thereof a compound of formula (I): 

Pyridazine derivatives and their use as therapeutic agents

This invention is directed to the use of SCD-1 inhibitors of the formula (I): where x, y, V, W, G, J, L, M, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein, in combination with other drug therapies to treat adverse weight gain. 

Combination therapy

Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): wherein W, V, x, y, R, R, R, R, R, R, R, Ra, R, Ra, R, R, Rand Rare defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed. 

Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human include administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R, R, R, R, R, R, R, R, R, R, Rand Rare defined herein.

Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (Ia): where x, y, W, V, R, R, R, R, R, R, R, R, R, R, Rand Rare defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): wherein: W is &#x2014;O&#x2014;, &#x2014;N(R1)&#x2014;, C(O), S(O)t; (where t is 0, 1 or 2), N(R1)S(O)2, S(O)2N(R1), C(O)N(R1) or N(R1)C(O)N(R1); and V is C(O), C(S), C(O)N(R1)&#x2014;, C(O)O&#x2014;, S(O)2&#x2014;, S(O)2N(R1)&#x2014; or C(R11)H; and x, y, R1, R2, R3, R4, R5, R6, R7, R7, R8, R8, R9, R9, R10 and R10are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed. 

Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where G, J, L, M, x, y, W, V, R, R, R, R, R, R, R, R, R, R, R, R, Rand Ra are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed. 

Piperazine derivatives and their use as therapeutic agents

Novel compounds useful in the treatment of, prevention of or protection against diseases and/or conditions related to metabolic syndrome and lipid metabolism, especially diseases of fatty acid and cholesterol metabolism, such as those mediated by stearoyl-CoA desaturase, are disclosed along with methods of employing said compounds for such uses.

Pyridylpiperazines and aminonicotinamides and their use as therapeutic agents

The present invention relates to elongase genes, their polypeptides and their control regions, and the use of such genes, polypeptides and control regions in determining compositions for use in the treatment of disease. The identified compositions regulate the expression of the elongase genes or modulate the activity of their protein products. The nucleotide and amino acid sequences are taught for ELG4, ELG6 and ELG7. The control sequences and function are taught for ELG1, ELG2, ELG3, ELG4, ELG5, ELG6 and ELG7.

Human elongase genes and uses thereof

High throughput screening assays for the identification of potential therapeutic agents able to modulate the activity of enzymes of fatty acid biosynthesis, especially desaturases and/or elongases, are disclosed along with therapeutic uses of the agents identified by such assays for the prevention and/or treatment of diseases related to fatty acid metabolism. Substrates useful in such assays are also described.

High throughput screening assays using fatty acid synthetic enzymes

Drug screening assays useful in the discovery of pharmaceutically active compounds for use in the treatment of diseases involving abnormal lipid metabolism including diabetic neuropathy are taught. In particular, the control region of delta-5-desaturase gene is taught as a target for the drug screening methods, which serve to identify nucleotides, proteins, compounds and/or other pharmacological agents, which modulate the activity of desaturase enzymes or regulate the level of expression of the desaturase genes. Cell-based and cell lysate assays are taught for detecting components that interact with the desaturase enzymes and modify fatty acid profiles. In addition, cell-based and cell lysate assays are used to identify functional and regulatory elements controlling expression of the desaturase genes as well as to screen for components that modulate the transcriptional activity of the desaturase genes. Also taught is the gene for rat delta-5-desaturase.

Methods for screening compounds that modulate lipid metabolism

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Vancouver, Canada

Michael D Winther