Arena Pharmaceuticals, Inc.

Anthony C Blackburn

Jaimie Karyn Rueter

Antonio Garrido Montalban

Robert M Jones

Sangdon Han

Biman B Pal

Yifeng Xiong

Sonja Strah-Pleynet

Xiuwen Zhu

Jae-Kyu Jung

Lars Thoresen

Dawei Yue

Jayant Thatte

Marlon Carlos

Lee Alani Selvey

Sagar Raj Shakya

You-An Ma

Anna Shifrina

Mark Allen Hadd

Ryan O Castro

Thuy-Anh Tran

Brett Ullman

Scott Stirn

Quyen-Quyen Thuy Do

Maiko Nagura

Zezhi Jesse Shao

Yun Shan

Michael E Morgan

Andrew J Grottick

Libo Yang

Woo Hyun Yoon

Michael D Morgan

William Lucas Betts, Iii

Quyen-Quyen Do

The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1Preceptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

Crystalline l-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(compound1) for use in SIPI receptor-associated disorders

Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CBreceptor;

Cannabinoid receptor modulators

Crystalline L-arginine salt of ()-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound1) for use in S1Preceptor-associated disorders

A simple two-piece easily and inexpensively manufactured cord tightening device and method thereof, the device comprising: a base, cylindrical in form with walls, an interior bottom having ridges, a hollow central column, and a protrusion in the walls with an opening, the protrusion; and a handle, fashioned in the shape of a spool, with a top flange with at least one hole therein, central cylindrical cavity, and bottom flange with ridges on the bottom. The cord tightening device wherein the central cylindrical cavity of the handle fits onto the hollow central column of the base. The cord tightening device may further comprise threading in the hollow central column of the base. The cord tightening device may further comprise a screw. The cord tightening device may further comprise a spring washer. The cord tightening device may further comprise at least two holes in the top flange of the handle. The cord tightening device may further comprise a circular ridge around the central cylindrical cavity of the top flange. The cord tightening device may further comprise ridges on the outer rim of the top flange.

Cord tightening device

Provided are certain methods useful in the treatment of pain comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CBreceptor;

The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CBreceptor and are therefore useful in the treatment of CBreceptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson's disease.

Crystalline forms and processes for the preparation of cannabinoid receptor modulators

The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the beta-3 adrenergic receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a beta-3 adrenergic receptor-mediated disorder, such as, heart failure; cardiac performance in heart failure; mortality, reinfarction, and/or hospitalization in connection with heart failure; acute heart failure; acute decompensated heart failure; congestive heart failure; severe congestive heart failure; organ damage associated with heart failure (e.g., kidney damage or failure, heart valve problems, heart rhythm problems, and/or liver damage); heart failure due to left ventricular dysfunction; heart failure with normal ejection fraction; cardiovascular mortality following myocardial infarction; cardiovascular mortality in patients with left ventricular failure or left ventricular dysfunction; left ventricular failure; left ventricular dysfunction; class II heart failure using the New York Heart Association (NYHA) classification system; class III heart failure using the New York Heart Association (NYHA) classification system; class IV heart failure using the New York Heart Association (NYHA) classification system; LVEF&#x3c;40% by radionuclide ventriculography; LVEF&#x2264;35% by echocardiography or ventricular contrast angiography; and conditions related thereto.

Modulators of the beta-3 adrenergic receptor useful for the treatment or prevention of disorders related thereto

Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3, 4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(compound1) for use in S1Preceptor-associated disorders

Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound 1) for use in SIPI receptor-associated disorders

Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CBreceptor; 

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San Diego, CA, United States of America

Anthony C Blackburn