7035-11-2

Usage

InChI:InChI=1/C8H8Cl2O/c1-11-8-3-2-7(10)4-6(8)5-9/h2-4H,5H2,1H3

Upstream product

• 7035-10-1 (5-chloro-2-methoxyphenyl)methanol 
• 33924-48-0 methyl 5-chloro-2-methoxybenzoate 
• 5330-38-1 4-chloro-2-hydroxymethylphenol 
• 7035-09-8 5-chloro-2-methoxybenzaldehyde 
• 635-93-8 5-chlorosalicyclaldehyde 
• 3438-16-2 5-chloro-2-methoxybenzoic acid 
• 50-00-0 formaldehyd 
• 623-12-1 4-chloromethoxybenzene 

Downstream Products

• 340001-71-0 4-(5-Chloro-2-methoxy-phenyl)-3-phenyl-butyric acid sec-butyl ester 
• 859409-00-0 2-methoxy-5-chlorobenzylazide 
• 7048-38-6 (5-chloro-2-methoxy-phenyl)-acetonitrile 
• 99522-22-2 o-(trimethylsilylmethyl)benzyl alcohol 
• 33206-31-4 3-(2-hydroxyphenyl)-2-propanol 
• 14310-34-0 1,2-bis(2-methoxyphenyl)ethane 
• 202822-68-2 3-[(5-Chloro-2-methoxyphenyl)methyl]-5-[4-(trifluoromethyl)-phenyl]-1,3,4-oxadiazol-2(3H)-one 

Relevant academic research and scientific papers

METHODS OF TREATING CREATINE TRANSPORTER DEFICIENCY

Disclosed are methods of treating creatine transporter deficiency, comprising administering to a mammal in need thereof a therapeutically effective amount of a compound that increases transport of a substrate by a mutant or wild-type creatine transporter. Also disclosed are methods of increasing transport of guanidinoacetic acid or a salt thereof across the blood-brain barrier of a mammal, and methods of decreasing accumulation or the concentration of guanidinoacetic acid or a salt thereof in a mammalian cell.

SMALL MOLECULES TARGETING MUTANT MAMMALIAN PROTEINS

Disclosed are compounds, compositions, and methods useful for treating or preventing a disease or disorder associated with a mutation in a protein.

Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7

A series of acidic diaryl ether heterocyclic sulfonamides that are potent and subtype selective NaV1.7 inhibitors is described. Optimization of early lead matter focused on removal of structural alerts, improving metabolic stability and reducing cytochrome P450 inhibition driven drug-drug interaction concerns to deliver the desired balance of preclinical in vitro properties. Concerns over nonmetabolic routes of clearance, variable clearance in preclinical species, and subsequent low confidence human pharmacokinetic predictions led to the decision to conduct a human microdose study to determine clinical pharmacokinetics. The design strategies and results from preclinical PK and clinical human microdose PK data are described leading to the discovery of the first subtype selective NaV1.7 inhibitor clinical candidate PF-05089771 (34) which binds to a site in the voltage sensing domain.

A BMS - 191011 synthetic method

The invention relates to a synthetic method for a compound BMS-191011. The method comprises the following steps: taking 4-trifluoromethyl benzoyl hydrazine as a raw material and performing steps of oxidative carbonylation, methyl protection, halogenation, amination, deprotection and the like to prepare BMS-191011. The synthetic method adopts a CO balloon for replacing phosgene, so that the reaction toxicity is reduced and the reaction operability is improved. The method has the characteristics of simple and easily available raw materials, mild reaction conditions and simple operation process.

Cycloalkyl-substituted mesyl benzamide derivatives, and preparation method and medical application thereof

The invention relates to cycloalkyl-substitutedmesyl benzamide derivatives, and a preparation method and medical application thereof. The invention particularly discloses compounds disclosed as Formula (I) or pharmaceutically acceptable salts, stereoisomers, solvated compounds or prodrugs thereof, and a preparation method and application thereof. All the groups in the formula are defined in the specification.

SELECTIVE NAV1.7 INHIBITORS FOR THE TREATMENT OF DIABETES

Provided herein are methods for treating or preventing prediabetes or diabetes, or maintaining or lowering blood or plasma glucose or maintaining or lowering blood or plasma glycated hemoglobin comprising administering to a subject in need thereof a therapeutically effective amount of a compound selectively inhibiting NaVl.7. In particular, provided herein are processes for the preparation of and intermediates used in the preparation of compounds selectively inhibiting NaV1.7, such as the compounds of Formula (I) or compounds of Formula (I').

SODIUM CHANNEL MODULATORS FOR THE TREATMENT OF PAIN AND DIABETES

Provided herein are sodium channel modulating Compounds, in particular NaV1.7 modulating compounds of Formula I or compounds of Formula I′: In particular, provided herein are processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions comprising, and therapeutic methods comprising administering such compounds. In particular, provided herein are compounds for the treatment of pain and diabetes.

SODIUM CHANNEL MODULATORS FOR THE TREATMENT OF PAIN

Provided herein are sodium channel modulating Compounds, in particular NaV1.7 modulating compounds of Formula I: In particular, provided herein are processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions comprising, and therapeutic methods comprising administering such compounds. In particular, provided herein are compounds for the treatment of pain.

INDAZOLE DERIVATIVES

The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologic

Piperazinyl CCR1 antagonists-optimization of human liver microsome stability

The synthesis, biological activity, and pharmacokinetic profile of CCR1 antagonists are described.