Abstract: Provided are methods of treatment of a sphingosine 1-phosphate subtype 1 (S1P1) receptor-associated disorder comprising prescribing and/or administering to an individual in need thereof a standard dose of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.

Abstract: Provided in some embodiments are titration packages, kits, and methods of treating pulmonary arterial hypertension comprising prescribing and/or administering to a patient in need thereof 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, via a titration scheme that comprises the up-titration of Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, over a period of no more than about nine weeks until an optimized dose is administered.

Abstract: The present invention relates to crystalline salts of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid, and pharmaceutical compositions comprising them that are useful as SiP1 receptor modulator. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid identified as an SiP1 receptor modulator is useful in the treatment of SiP1 receptor-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 vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof and their use in methods for the alleviation and/or treatment of visceral pain, for example abdominal pain; pelvic pain; male pelvic pain; pain from an internal organ; bladder pain; painful bladder syndrome; post-surgical abdominal pain (e.g., GI resection, hysterectomy, oophorectomy, C-section, and the like); or pain arising from or related to: pancreatitis (e.g., chronic pancreatitis), prostatitis (e.g., chronic prostatitis), inflammatory bowel disease (e.g., Crohn's disease), endometriosis, interstitial cystitis, prostatitis (e.g., chronic prostatitis), epididymitis (e.g., chronic epididymitis), or post-surgical abdominal lesions. In some embodiments, the visceral pain is consequent to inflammatory bowel disease, for example Crohn's disease.

Abstract: Provided is a solvate that is 1-ethyl-3-((R)-3-((S)-2-hydroxy-3-(3-(methylsulfonyl)phenoxy)propylamino)-1-oxa-8-azaspiro[4.5]decan-8-ylsulfonyl)quinolin-4(1H)-one mesylate hemihydrate Form 2, and pharmaceutical compositions thereof that modulate the activity of the beta-3 adrenergic receptor.

Abstract: Provided are methods of treatment of a sphingosine 1-phosphate subtype 1 (S1P1) receptor-associated disorder comprising prescribing and/or administering to an individual in need thereof a standard dose of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl) benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

Abstract: Provided is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, that is a modulator of 5-HT2A and can be used in treating diseases and disorders associated with 5-HT2A serotonin receptor expression and/or activity. Thus, also provided are methods of treating 5HT2A-related diseases and disorders.

Abstract: The present invention relates to methods of treating renal cystic disease and/or cardiorenal syndrome by administrating certain compounds that modulate the activity of the beta-3 adrenergic receptor.

Abstract: The invention relates to 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to the 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) for use as a medicament, pharmaceutical compositions comprising at least a compound of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

Abstract: 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 CB2 receptor;

Abstract: The present invention relates to, inter alia, methods of treatment and combinations of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid (Compound 1) useful for the treatment of extra-intestinal manifestations (EIM) in an individual with inflammatory bowel disease (BBD) and for the treatment of pyoderma gangrenosum (PG). In some embodiments, the methods further comprise administering Compound 1, or a pharmaceutically salt, solvate, or hydrate thereof, in combination with a therapeutically effective amount of a compound selected from the group consisting of: a corticosteroid, a 5-aminosalicylic acid derivative, and a TNF-alpha inhibitor; or a corticosteroid, an immunosuppressant, a biologic, an anti-inflammatory agent, and an antibiotic.

Abstract: Provided are methods useful in the prophylaxis or treatment of an S1P1 modulated disease in different populations of individuals, including those with hepatic impairment. In some methods, etrasimod is prescribed or administered to an individual in need of treatment wherein the dose is not adjusted for the patient having mild, moderate, or severe hepatic impairment.

Abstract: Provided are methods of treating or preventing Raynaud's, comprising prescribing and/or administering to an individual in need thereof 3-methoxy-N-[3-(2-methylpyrazol-3-yl)-4-(2-morpholin-4-ylethoxy)phenyl]benzamide (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

Abstract: Provided are methods of treatment of a sphingosine 1-phosphate subtype 1 (S1P1) receptor-associated disorder comprising prescribing and/or administering to an individual in need thereof a standard dose of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta [b]indol-3-yl)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, in an amount equivalent to about 1.5 to about 2.5 mg of Compound 1, for example, a disease or disorder mediated by lymphocytes, an autoimmune disease or disorder, an inflammatory disease or disorder, ankylosing spondylitis, biliary cirrhosis, cancer, psoriasis, psoriatic arthritis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, inflammatory bowel disease, ulcerative colitis, type I diabetes, hypertensive nephropathy, glomerulosclerosis, myocardial ischemia-reperfusion injury, and acne.

Abstract: Provided are methods of treatment of abdominal pain due to IBS, comprising administering to an individual in need thereof (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 or a pharmaceutically acceptable salt or crystal form thereof.

Abstract: 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 and related disorders thereto.

Abstract: 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 S1P1 receptor-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).

Abstract: Provided are methods for the parenteral use of 3-methoxy-N-[3-(2-methylpyrazol-3-yl)-4-(2-morpholin-4-ylethoxy)phenyl]benzamide, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and the sequential use of parenteral and oral formulations of 3-methoxy-N-[3-(2-methylpyrazol-3-yl)-4-(2-morpholin-4-ylethoxy)phenyl]benzamide, or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.