Chemocentryx, Inc.

Ardelyx, Inc.

Dean R Dragoli

Penglie Zhang

Hiroko Tanaka

Xi Chen

Viengkham Malathong

Jay Patrick Powers

Manmohan Reddy Leleti

Ju Yang

Pingchen Fan

Venkat Reddy Mali

Chao Yu

Yandong Li

Jaroslaw Kalisiak

Junfa Fan

Jason Gustaf Lewis

Rajinder Paul Singh

Rebecca M Lui

Jeffrey P McMahon

Sreenivas Punna

Michael Robert Leadbetter

Tao Chen

Christopher W Lange

Jeffrey William Jacobs

Juan Carlos Jaen

Antoni Krasinski

Daniel J Dairaghi

Noah Bell

Irina Dotsenko

Matthew J Walters

Joanne Tan

Rakesh K Jain

Matthew John Siegel

Jeremy Caldwell

Patricia Finn

Gary Luehr

Yibin Zeng

Christopher Carreras

Lianfa Li

Matthew Siegel

Andrew King

Mark M Gleason

Jeffrey P McMAHON

Jarek Kalisiak

Ying He

Jeffrey Mcmahon

Hiroko Tankaka

Daniel Dairaghi

The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.

Compounds useful for treating gastrointestinal tract disorders

Oxindole compounds useful for the treatment of CCR(9) mediated conditions or diseases are provided.

2-oxindole compounds

The invention relates to non-systemic TGR5 agonist useful in the treatment of chemotherapy-induced diarrhea, diabetes, Type II diabetes, gestational diabetes, impaired fasting glucose, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity, metabolic syndrome, ulcerative colitis, Crohn's disease, disorders associated with parenteral nutrition especially during short bowel syndrome, and irritable bowel syndrome (IBS), and other TGR5 associated diseases and disorders, having the Formula:

Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists

Compounds are provided as inhibitors of CXCR2, having the structure:

Inhibitors of CXCR2

The present invention provides a compound of formula (I) or a salt thereof: (Formula (I)) wherein X, L, V, R; R, Rand R, are as defined herein. The claimed compounds inhibit the enzyme 11-hydroxysteroid dehydrogenase type 2 (11-HSD2) and as a result are useful in the treatment of hyperkalemia by preventing cortisol from being oxidised to cortisone and thus allowing it to occupy the mineralocorticoid receptor, thus stimulating potassium excretion.

Glycyrrhetinic acid derivatives for use in treating hyperkalemia

Compounds are provided as chemokine inhibitors having the structure:

Modulators of chemokine receptors

The present invention provides a compound of formula (I) or a salt thereof: (I) wherein X, L, V, R, R, Rand R, are as defined herein. These compounds are inhibitors of 11-hydroxysteroid dehydrogenase type 2 (11-HSD-2) and are used to treat hyperkalemia.

Glycyrrhetinic acid derivatives for treating hyperkalemia

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.

Diazole lactams

The present disclosure is directed to compounds (I') and to their use in methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds (I&#x2032;) and their use in methods for the treatment of hypertension. The present disclosure is also directed to compounds (I&#x2032;) and to their use in methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. 

Inhibitors of NHE-mediated antiport

Compounds are provided as inhibitors of CXCR2, having the structure: 

Compounds are provided as chemokine inhibitors having the structure: 

The invention relates to non-systemic TGR5 agonist useful in the treatment of chemotherapy-induced diarrhea, diabetes, Type II diabetes, gestational diabetes, impaired fasting glucose, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity, metabolic syndrome, ulcerative colitis, Crohn's disease, disorders associated with parenteral nutrition especially during short bowel syndrome, and irritable bowel syndrome (IBS), and other TGR5 associated diseases and disorders, having the Formula: where R, R, R, R, R, X, X, X, X, Q, and n are described herein.

Compounds of formula (I) are provided which are useful in the treatment of diseases or conditions modulated at least in part by CCR6: 

CCR6 compounds

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Los Altos, CA, United States of America

Dean R Dragoli