76140-13-1

Upstream product

• 5709-98-8 (R)-cyclohex-3-enecarboxylic acid 
• 4771-80-6 1,2,5,6-tetrahydrobenzoic acid 

Downstream Products

• 95205-00-8 methyl 2-(benzyloxyamino)butanoate 
• 127308-75-2 (1R,5R)-5-(hydroxymethyl)-2-cyclohexen-1-ol 
• 94160-25-5 hydroxy-3 cyclohexane carboxylate d'ethyle 
• 4350-83-8 6-oxa-bicyclo[3.2.1]octan-7-one 
• 1446003-98-0 C₃₉H₆₂N₄O₁₅S 
• 1446004-02-9 C₆₈H₇₈F₃NO₁₆ 
• 1374760-32-3 C₃₄H₅₉N₃O₁₄ 
• 1374760-31-2 C₃₃H₅₅NO₁₅ 
• 1374760-30-1 C₄₀H₅₉NO₁₆ 
• 1374760-29-8 C₆₈H₈₁NO₁₆ 
• 1374760-28-7 C₇₀H₈₃NO₁₇ 
• 1374760-27-6 C₅₄H₆₃NO₁₅ 
• 1374760-26-5 C₄₇H₅₉NO₁₄ 
• 1374760-25-4 C₅₃H₆₅NO₁₇ 

Relevant academic research and scientific papers

Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases

The oxycyclohexyl acid BMS-986278 (33) is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with a human LPA1 Kb of 6.9 nM. The structure-activity relationship (SAR) studies starting from the LPA1 antagonist clinical compound BMS-986020 (1), which culminated in the discovery of 33, are discussed. The detailed in vitro and in vivo preclinical pharmacology profiles of 33, as well as its pharmacokinetics/metabolism profile, are described. On the basis of its in vivo efficacy in rodent chronic lung fibrosis models and excellent overall ADME (absorption, distribution, metabolism, excretion) properties in multiple preclinical species, 33 was advanced into clinical trials, including an ongoing Phase 2 clinical trial in patients with lung fibrosis (NCT04308681).

METHOD OF PRODUCING IODOLACTONE COMPOUND

PROBLEM TO BE SOLVED: To provide a method of producing an iodolactone compound suitable to the industry in which the total amount of iodine (iodine, iodide and the like) used is reduced. SOLUTION: A method of producing an iodolactone compound represented by the formula (2) is characterized by reacting an unsaturated carboxylic acid represented by the formula (1), an iodide, a halogen oxo acid or salt thereof, and a second acid different from the halogen oxo acid, where compounds represented by the formulas (1) and (2) are as defined in the specification. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT

Tetra-substituted pyridinylimidazoles as dual inhibitors of p38α mitogen-activated protein kinase and c-jun N-terminal kinase 3 for potential treatment of neurodegenerative diseases

Tetra-substituted imidazoles were designed as dual inhibitors of c-Jun N-terminal kinase (JNK) 3 and p38α mitogen-activated protein (MAP) kinase. A library of 45 derivatives was prepared and evaluated in a kinase activity assay for their ability to inhibi

METHODS AND COMPOSITIONS FOR TREATING AND/OR PREVENTING MUCOSITIS

Methods for treating and/or preventing mucositis comprising administering to a subject in need thereof an effective amount of at least one compound chosen from E-selectin antagonists, pharmaceutically acceptable salts of E-selectin antagonists, prodrugs of E- selectin antagonists, and pharmaceutically acceptable salts of prodrugs of E-selectin antagonists, and compositions comprising at least one of such compound.

E-SELECTIN ANTAGONIST COMPOUNDS AND METHODS OF USE

Provided herein are E-selectin antagonist therapeutic agents and improvements thereto and compositions comprising these E-selectin antagonists. Methods are also provided for using these E-selectin antagonist therapeutic agents to treat and/or prevent diseases and disorders treatable by inhibiting binding of an E-selectin to an E-selectin ligand. Also provided herein improvements to E-selectin antagonist giycomimetic compounds that improve the oral bioavailability of the giycomimetic compounds.

Stereospecific decarboxylative allylation of sulfones

Allyl sulfonylacetic esters undergo highly stereospecific, palladium-catalyzed decarboxylative allylation. The reaction allows the stereospecific formation of tertiary homoallylic sulfones in high yield. In contrast to related reactions that proceed at -100 °C and require highly basic preformed organometallics, the decarboxylative coupling described herein occurs under mild nonbasic conditions and requires no stoichiometric additives. Allylation of the intermediate α-sulfonyl anion is more rapid than racemization, leading to a highly enantiospecific process. Density functional theory calculations indicate that the barrier for racemization is 9.9 kcal/mol, so the barrier for allylation must be 9.9 kcal/mol.

PHARMACEUTICAL COMPOSITIONS AND METHODS FOR RELIEVING PAIN AND TREATING CENTRAL NERVOUS SYSTEM DISORDERS

Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas (1 or 2), as described herein. The compounds of Formulas (1 and 2) are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.

FK-506 SYNHETIC STUDIES. 3. AN EFFICIENT ASYMMETRIC SYNTHESIS OF THE C(24)-C(34) FRAGMENT OF FK-506, FR-900520, AND FR-900523

An efficient asymmetric synthesis of the C(24)-C(34) fragment of the FK-506 family of immunosuppressants has been achieved.