It’s only fair to share… Ervogastat CAS 2186700-33-2 Non-alcoholic Steatohepatitis (NASH) with Liver Fibrosis (FAST TRACK – U.S.) 2-[5-(3-ethoxypyridin-2-yl)oxypyridin-3-yl]-N-[(3S)-oxolan-3-yl]pyrimidine-5-carboxamide Phase IINon-alcoholic fatty liver disease; Non-alcoholic steatohepatitis Ervogastat is an experimental small-molecule drug and selective diacylglycerol O-acyltransferase 2 inhibitor developed by Pfizer for non-alcoholic steatohepatitis.[1] Its development was previously halted by the company but resumed in 2022.[2] Scheme SIDE CHAIN MAIN https://doi.org/10.1021/acs.jmedchem.2c01200 SYN …
Category «Phase 2»
Eclitasertib
It’s only fair to share… Eclitasertib CAS 2125450-76-0 5-benzyl-N-[(3S)-5-methyl-4-oxo-2,3-dihydropyrido[3,2-b][1,4]oxazepin-3-yl]-1H-1,2,4-triazole-3-carboxamide Molecular Weight 378.38 Formula C19H18N6O3 SAR443122, was investigated in several clinical trials to evaluate its safety and efficacy. NCT04469621 was studied in severe COVID-19 patients, while NCT05588843 is currently recruiting participants with ulcerative colitis. Additionally, NCT04781816, which was completed with results, focused on patients with cutaneous …
Davelizomib
It’s only fair to share… Davelizomib Molecular Weight 481.25 Formula C21H26BF2N3O7 CAS No. 2409841-51-4 {(4S)-2-[(1R)-1-{2-[(2S)-1-(2,4-difluorophenyl)azetidine-2- carboxamido]acetamido}-3-methylbutyl]-5-oxo-1,3,2- dioxaborolan-4-yl}acetic acid proteasome inhibitor, antineoplastic 2-[(4S)-2-[(1R)-1-[[2-[[(2S)-1-(2,4-difluorophenyl)azetidine-2-carbonyl]amino]acetyl]amino]-3-methylbutyl]-5-oxo-1,3,2-dioxaborolan-4-yl]acetic acid T3LN9U6BRF Davelizomib is proteasome inhibitor with antineoplastic effect. DAVELIZOMIB is a small molecule drug with a maximum clinical trial phase of II and has 1 investigational indication. Multiple myeloma (MM) is a malignant proliferative …
Crisugabalin
It’s only fair to share… Crisugabalin Cas 2209104-84-5 2-[(1S,2S,3R,6S,8S)-2-(aminomethyl)-2-tricyclo[4.2.1.03,8]nonanyl]acetic acid WeightAverage: 209.289Monoisotopic: 209.141578856 Chemical FormulaC12H19NO2 Tricyclo[4.2.1.03,8]nonane-2-acetic acid, 2-(aminomethyl)-, (1S,2S,3R,6S,8S)- (1S,2S,3R,6S,8S)-2-(Aminomethyl)tricyclo[4.2.1.03,8]nonane-2-acetic acid Crisugabalin (HSK16149) is a selective GABA analog in development for the treatment of chronic pain. It has a wider therapeutic index than pregabalin, which has a similar mechanism of action. In China, it was approved in May 2024 for the treatment of …
Clesacostat
It’s only fair to share… Clesacostat PF 05221304, 752DF9PPPI CAS 1370448-25-1 WeightAverage: 502.571Monoisotopic: 502.221620082 Chemical FormulaC28H30N4O5 4-[6-methoxy-4-(7-oxo-1-propan-2-ylspiro[4,6-dihydroindazole-5,4′-piperidine]-1′-carbonyl)pyridin-2-yl]benzoic acid Clesacostat is under investigation in clinical trial NCT04321031 (Metabolic Interventions to Resolve Non-alcoholic Steatohepatitis (NASH) With Fibrosis (MIRNA)). CLESACOSTAT is a small molecule drug with a maximum clinical trial phase of II (across all indications) and has …
Bezisterim, HE 3286; NE-3107
It’s only fair to share… Bezisterim, HE 3286; NE-3107 CAS 1001100-69-1 (1R,3aS,3bR,4R,7S,9aR,9bS,11aS)-1-ethynyl-9a,11a-dimethyl-1H,2H,3H,3aH,3bH,4H,6H,7H,8H,9H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthrene-1,4,7-triol (3S,7R,8R,9S,10R,13S,14S,17R)-17-ethynyl-10,13-dimethyl-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene-3,7,17-triol Formula C21H30O3 Molar mass 330.468 g·mol−1 17alpha-pregn-5-en-20-yne-3beta,7beta,17-triol Q27286562(3beta,7beta,17alpha)-Pregn-5-en-20-yne-3,7,17-triol17.ALPHA.-ETHYNYL-5-ANDROSTENE-3.BETA.,7.BETA.,17.BETA.-TRIOLPREGN-5-EN-20-YNE-3,7,17-TRIOL, (3.BETA.,7.BETA.,17.ALPHA.)- Bezisterim (developmental code names NE3107, HE3286) is a synthetic analogue of androstenetriol that is believed to have anti-inflammatory and insulin-sensitizing effects in the brain.[1] The compound crosses the blood–brain barrier and does not activate any neurotransmitter receptors.[2] It has been tested as a treatment for Alzheimer’s disease,[3][4][5][6] Parkinson’s disease,[1] and traumatic brain injury.[7] The drug is …
Bexicaserin
It’s only fair to share… Bexicaserin CAS 2035818-24-5 Formula C15H19F2N3O Molar mass 295.334 g·mol−1 LP352; LP-352; AN352; AN-352 (3R)-N-(2,2-difluoroethyl)-3-methyl-1,10-diazatricyclo[6.4.1.04,13]trideca-4,6,8(13)-triene-5-carboxamide Bexicaserin is under investigation in clinical trial NCT05626634 (Open-label, Long-term Safety Study of LP352 in Subjects With Developmental and Epileptic Encephalopathy). PATENT Arena Pharmaceuticals, Inc.WO2023172685 Arena Pharmaceuticals, Inc., WO2016176177 https://patents.google.com/patent/WO2016176177A1/en Example 1: Syntheses of Compounds of Table …
Zelatriazin
It’s only fair to share… Zelatriazin, C18H15F3N4O3, 392.3 g/mol 1929519-13-0 NBI-1065846 or TAK-041 Phase 2 (S)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide Zelatriazin (NBI-1065846 or TAK-041) is a small-molecule agonist of GPR139. It was developed for schizophrenia and anhedonia in depression but trials were unsuccessful and its development was discontinued in 2023.[1][2][3][4][5][6][7] SCHEME SYN WO2016081736 https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2016081736&_cid=P21-M0X9BK-38013-1 Example 2: (S)-2-(4-oxobenzo[d][l,2,3]triazin-3(4H)-yl)-N-(l-(4-(trifluoromethoxy)phenyl)ethyl)acetamide [0166] To a vial containing 2-(4-oxobenzo[d][l,2,3]triazin-3(4H)-yl)acetic acid (15 mg, …
EIDD-2173, ATI-2173, Fosclevudine alafenamide
It’s only fair to share… EIDD-2173; also known as ATI-2173 Fosclevudine alafenamide Molecular Weight 529.45 Formula C22H29FN3O9P CAS No. 1951476-79-1 phase 2 Hepatitis B virus (HBV) is an infectious disease that targets the liver resulting in either an acute infection, with symptoms arising in 45 to 160 days, or a chronic infection, which 350 …
MAVORIXAFOR
It’s only fair to share… MAVORIXAFOR AMD 070 N1-(1H-BENZIMIDAZOL-2-YLMETHYL)-N1-((S)-5,6,7,8-TETRAHYDROQUINOLIN-8-YL)-BUTANE-1,4-DIAMINE Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively. Molecular Weight 349.47 Appearance Solid Formula C21H27N5 CAS No. …