67197-54-0

Upstream product

• 89720-77-4 4-bromo-1-bromomethyl-2-chlorobenzene 
• 151-50-8 potassium cyanide 
• 59748-90-2 4-Bromo-2-chloro-benzoic Acid 
• 185315-48-4 (4-bromo-2-chlorophenyl)methanol 
• 89794-02-5 4-bromo-2-chlorotoluene 
• 773837-37-9 sodium cyanide 
• 916516-89-7 2-(4-bromo-2-chlorophenyl)acetic acid 

Downstream Products

• 849934-94-7 methyl 2-(4-bromo-2-chlorophenyl)acetate 
• 749929-86-0 2-(4-Bromo-2-chloro-phenyl)-2-methyl-propionitrile 
• 1261606-45-4 (4-bromo-2-chlorophenyl)acetic acid ethyl ester 
• 849934-95-8 methyl 2-(2-chloro-4-(1,1,2,2-tetramethyl-1λ4,2λ4,4-dioxaborolan-4-yl)phenyl)acetate 
• 916516-89-7 2-(4-bromo-2-chlorophenyl)acetic acid 
• 1122568-26-6 2-(4-bromo-2-chlorophenyl)-3-{4-[2-(2,6-dichloro-4-methylphenoxy)-ethoxy]phenyl}propanenitrile 
• 1366037-97-9 C₂₇H₂₇ClF₂N₂O 
• 1366038-72-3 C₂₂H₂₃BrClF₂NO₂ 
• 1247090-99-8 C₂₁H₂₄BrClN₂O₂ 
• 1366038-80-3 C₂₂H₂₆BrClN₂O₃ 
• 1247086-08-3 C₂₆H₂₈ClN₃O 

Relevant academic research and scientific papers

HETEROCYCLIC FXR MODULATORS

The present technology is directed to compounds of formula (I), compositions, and methods related to modulation of FXR. In particular, the present compounds and compositions may be used to treat FXR-mediated disorders and conditions, including, e.g., liver disease, hyperlipidemia, hypercholesteremia, obesity, metabolic syndrome, cardiovascular disease, gastrointestinal disease, and atherosclerosis, and renal disease.

An optimized synthesis of the potent and selective Pak1 inhibitor FRAX-1036

FRAX-1036 is a p21-activated kinase I inhibitor of significant interest to cancer biologists yet no commercial providers or detailed procedures are available. In this Letter, we chronicle the optimized synthesis of FRAX-1036, one of the most specific Pak1

SERINE/THREONINE KINASE INHIBITORS

Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, n, r, s and t are as defined herein and which compounds are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.

Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pKa Polar Moiety

Signaling pathways intersecting with the p21-activated kinases (PAKs) play important roles in tumorigenesis and cancer progression. By recognizing that the limitations of FRAX1036 (1) were chiefly associated with the highly basic amine it contained, we devised a mitigation strategy to address several issues such as hERG activity. The 5-amino-1,3-dioxanyl moiety was identified as an effective means of reducing pKa and logP simultaneously. When positioned properly within the scaffold, this group conferred several benefits including potency, pharmacokinetics, and selectivity. Mouse xenograft PK/PD studies were carried out using an advanced compound, G-5555 (12), derived from this approach. These studies concluded that dose-dependent pathway modulation was achievable and paves the way for further in vivo investigations of PAK1 function in cancer and other diseases.

2- PYRIDONE COMPOUND

PROBLEM TO BE SOLVED: To provide a compound that has excellent glucokinase (GK) activating action and is useful as a pharmaceutical. SOLUTION: The present invention provides a 2-pyridone compound represented by formula [1], and a tautomer or stereoisomer of the compound, or their pharmacologically acceptable salts, or their solvates (where R1 is RA-ZA-; RA is any of a carboxy group, a sulfo group or formula [5]). COPYRIGHT: (C)2016,JPOandINPIT

8-ETHYL-6-(ARYL)PYRIDO [2,3-D]PYRIMIDIN-7(8H) -ONES FOR THE TREATMENT OF NERVOUS SYSTEM DISORDERS AND CANCER

Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders or neurofibromatosis. Also described herein are methods of utilizing PAK inhibitors for the treatment of cancer.

RENIN INHIBITORS

The present invention relates to biphenyl compounds of formula (I). These compounds are renin inhibitors of a non- peptidic nature and of low molecular weight. The invention further relates to a pharmaceutical composition containing said compounds, as wel

2-AMINOBUTANOL COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES

The present invention provides a novel compound having few side effects such as bradycardia and the like and having superior peripheral blood lymphocyte-decreasing effect. The present invention provides a 2-aminobutanol compound represented by the following formula (I) wherein R1 is a hydrogen atom or P(=O)(OH)2, R2 is an alkyl having 1 to 4 carbon atoms optionally substituted by hydroxyl group(s) or optionally substituted by halogen atom(s), R3 is a hydrogen atom; a halogen atom; cyano; an alkyl having 1 to 4 carbon atoms optionally substituted by halogen atom(s); or an acyl having 2 to 5 carbon atoms optionally substituted by halogen atom(s), X is an oxygen atom, a sulfur atom, carbonyl or NR4 wherein R4 is a hydrogen atom or an alkyl having 1 to 4 carbon atoms, Ar1 is an optionally substituted arylene or an optionally substituted heteroarylene, and Ar2 is an optionally substituted aryl or an optionally substituted heteroaryl, provided that when X is an oxygen atom, Ar1 is phenylene and Ar2 is phenyl, then the phenyl for Ar2 should be substituted, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof, as well as a production method of the above-mentioned 2-aminobutanol compound.

BENZIMIDAZOLE DERIVATIVES USEFUL IN TREATMENT OF VALLINOID RECE TOR TRPVL RELATED DISORDERS

The claimed invention provides benzimidazole derivatives antagonists of VRl, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds of Formula I may be used in the treatment of osteoarthritis,

TISSUE FACTOR PRODUCTION INHIBITOR

A medicament which has an activity of inhibiting production of tissue factor and comprises an LXR ligand as an active ingredient; and a medicament for treatment and/or prophylaxis of vascular restenosis following angioplasty, endarterectomy, percutaneous transluminal coronary angioplasty (PTCA) or stent implantation, or treatment and/or prophylaxis of blood coagulation diseases, diseases induced by platelet aggregation including stable or unstable angina pectoris, cardiovascular and cerebrovascular diseases including thromboembolism formation diseases accompanying diabetes, rethrombosis following thrombolysis, cerebral ischemic attack, infarction, stroke, ischemia-derived dementia, peripheral artery disease, thromboembolism formation diseases during use of an aorta-coronary artery bypass, glomerulosclerosis, renal embolism, tumor or cancer metastasis, which comprises an LXR ligand as an active ingredient.