Category «PHASE 1»

Development of a concise, scalable synthesis of a CCR1 antagonist utilizing a continuous flow Curtius rearrangement

It’s only fair to share… Development of a concise, scalable synthesis of a CCR1 antagonist utilizing a continuous flow Curtius rearrangement Green Chem., 2017, Advance Article DOI: 10.1039/C6GC03123D, Paper Maurice A. Marsini, Frederic G. Buono, Jon C. Lorenz, Bing-Shiou Yang, Jonathan T. Reeves, Kanwar Sidhu, Max Sarvestani, Zhulin Tan, Yongda Zhang, Ning Li, Heewon Lee, …

FOTAGLIPTIN

It’s only fair to share…   FOTAGLIPTIN CAS 1312954-58-7 342.37, C17 H19 F N6 O Benzonitrile, 2-[[3-[(3R)-3-amino-1-piperidinyl]-6-methyl-5-oxo-1,2,4-triazin-4(5H)-yl]methyl]-4-fluoro- (R)-2-((3-(3-amino-piperidin-1-yl)-6-methyl-5-oxo-1,2,4-piperazine-4(5H)-yl)methyl)-4-fluorobenzonitrile, BENZOATE 1403496-40-1 (R) 2- Methyl-5-oxo-1,2,4-triazin-4 (5H) -yl) methyl) -4-fluorobenzonitrile (3- benzoate (compound benzoate A), of the formula: the C . 17 the H 19 the FN . 6 O · the C . 7 the H . 6 O 2 …

HS-10168

It’s only fair to share… HS-10168 CAS 1394346-15-6 471.26, C21 H19 Cl2 F2 N2 O2 P (R)-(4-(6-Amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)-3-fluorophenyl)dimethylphosphine Oxide (HS-10168) 2-Pyridinamine, 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[4-(dimethylphosphinyl)-2-fluorophenyl]- HS-10168 is a potent and selective mesenchymal epithelial transition factor/anaplastic lymphoma kinase (c-Met/ALK) inhibitor that has advanced into Phase I clinical trials.(1, 2) Inventors Baihua Hu, Kan He, Minsheng Zhang Applicant Jiangsu Hansoh Pharmaceutical Co., …

Citarinostat

It’s only fair to share… Citarinostat Treatment of Hematological Malignancies,  Molecular Formula, C24-H26-Cl-N5-O3, Molecular Weight, 467.9544, RN: 1316215-12-9 UNII: 441P620G3P 2-[(2-Chlorophenyl)phenylamino]-N-[7-(hydroxyamino)-7-oxoheptyl]-5-pyrimidinecarboxamide 2-((2-Chlorophenyl)phenylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)-5-pyrimidinecarboxamide 5-Pyrimidinecarboxamide, 2-((2-chlorophenyl)phenylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)- ACY-241; HDAC-IN-2 Histone deacetylase-6 inhibitor Acute myelogenous leukemia; Cancer; Mantle cell lymphoma; Multiple myeloma Mechanism of ActionHDAC6 protein inhibitors Highest Development Phases Phase IIMultiple myeloma Phase IMalignant melanoma; Non-small cell lung cancer; Solid …

CPP 115

It’s only fair to share… (+)-(1S,4S)-4-Amino-3-(difluoromethylene)-1-cyclopentanecarboxylic acid 640897-20-7 CAS PHASE 1 NORTHWESTERN UNIVERSITY .INNOVATORS Sponsor: Catalyst Pharmaceuticals, Inc. CPP-115 free base; UNII-5TD9324Z2U; CHEMBL146927; 640897-20-7; (1S,3S)-3-Amino-4-difluoromethylenyl-1-cyclopentanoic acid; (+)-(1S,4S)-4-Amino-3-(difluoromethylene)-1-cyclopentanecarboxylic acid Molecular Formula: C7H9F2NO2 Molecular Weight: 177.151 g/mol Originator Northwestern University Developer Catalyst Pharmaceutical Partners Class Aminobutyric acids; Antiepileptic drugs; Small molecules Mechanism of Action 4-aminobutyrate transaminase inhibitors Orphan Drug Status Yes – …

Verubecestat (MK-8931)

It’s only fair to share… Verubecestat (MK-8931) Merck Alzheimer’s drugs Verubecestat (MK-8931) is an oral β- amyloid precursor protein cleaving enzyme (BACE1 or β-secretase enzyme) inhibitor, is currently in Phase III clinical trials Verubecestat MK 8931, MK-8931, SCH 900931 2-Pyridinecarboxamide, N- (3 – ((5R) -3-amino-5,6-dihydro-2,5-dimethyl-1 , 1-dioxido-2H-1,2,4-thiadiazin-5-yl) -4-fluorophenyl) -5-fluoro- N-[3-[(5R)-3-amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-fluoropyridine-2-carboxamide CAS : 1286770-55-5 C17 H17 …

CB-618

It’s only fair to share…   CB-618, CB-238618 CAS 1463520-70-8 C8 H10 N4 O6 S, 290.25 Sulfuric acid, mono[(1R,2S,5R)-2-(1,3,4-oxadiazol-2-yl)-7-oxo-1,6-diazabicyclo[3.2.1]oct-6-yl] ester (25, 5R)-sulfuric acid mono-(2-[l,3,4]oxadiazol-2-yl-7-oxo-l,6-diaza-bicyclo[3.2.1]oct-6-yl) ester SODIUM SALT sodium salt of (2S,5R)-sulfuric acid mono-(2-[1,3,4]oxadiazol-2-yl-7-oxo-1,6-diaza-bicyclo[3.2.1]oct-6-yl)ester CAS 1628207-16-8 C8 H10 N4 O6 S . Na Sulfuric acid, mono[(1R,2S,5R)-2-(1,3,4-oxadiazol-2-yl)-7-oxo-1,6-diazabicyclo[3.2.1]oct-6-yl] ester, sodium salt (1:1) PATENTS WO2013149121 US 20140275001 US 20150094472 WO 2016081452 Infection, multidrug …

BMS 906024

It’s only fair to share… BMS 906024 cas 1401066-79-2 MF C26H26F6N4O3 MW 556.500 (2R,3S)-N-[(3S)-1-Methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]-2,3-bis(3,3,3-trifluoropropyl)succinamide Butanediamide, N1-((3S)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluorophenyl)-, (2R,3S)- (2R,35)-N-((35)-l-Methyl-2-oxo-5-phenyl-2,3-dihydro-lH-l,4-benzodiazepin-3-yl)-3- (2,2,2-trifluoroethyl)-2-(3,3,3-trifluoropropyl)succinamide Claude Quesnelle, Soong-Hoon Kim, Francis Lee, Ashvinikumar Gavai Applicant Bristol-Myers Squibb Company Ashvinikumar Gavai   Claude Quesnelle Senior Research Investigator/Chemist at Bristol-Myers Squibb RICHARD LEE BMS-906024 is a novel, potent Notch receptor inhibitor . Cancers have a tendency …

VT 1129

It’s only fair to share… VT 1129 1340593-70-5 CAS MF C22 H14 F7 N5 O2, MW 513.37 2-Pyridineethanol, α-(2,4-difluorophenyl)-β,β-difluoro-α-(1H-tetrazol-1-ylmethyl)-5-[4-(trifluoromethoxy)phenyl]-, (αR)- R ISOMER ROTATION + Originator Viamet Pharmaceuticals Class Antifungals; Small molecules Mechanism of Action 14-alpha demethylase inhibitors Orphan Drug Status Yes – Cryptococcosis On Fast track Cryptococcosis Phase I Cryptococcosis Most Recent Events 01 Jun 2016 VT 1129 receives Fast Track designation for Cryptococcosis …