Tag «PHASE 1»

Epitinib

It’s only fair to share… Epitinib succinate; HMPL-813; Huposuan yipitini 1203902-67-3, 430.50, C24 H26 N6 O2 1-Piperazinecarboxamide, 4-ethyl-N-[4-[(3-ethynylphenyl)amino]-7-methoxy-6-quinazolinyl]- 4-Ethyl-N-[4-[(3-ethynylphenyl)amino]-7-methoxy-6-quinazolinyl]-1-piperazinecarboxamide Cancer; Glioblastoma; Non-small-cell lung cancer Epitinib is in phase I clinical trials by Hutchison MediPharma for the treatment of solid tumours. Epitinib succinate is an oral EGFR tyrosine kinase inhibitor in early clinical development at Hutchison China MediTech (Chi-Med) for the …

CIFORADENANT

It’s only fair to share… CIFORADENANT 1202402-40-1 Chemical Formula: C20H21N7O3 Molecular Weight: 407.434 CPI-444, CPI 444, CPI444, V81444, V-81444, V 81444, UNII 8KFO2187CP  Corvus Pharmaceuticals, Inc. PHASE 1 (S)-7-(5-methylfuran-2-yl)-3-((6-(((tetrahydrofuran-3-yl)oxy)methyl)pyridin-2-yl)methyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine 3H-1,2,3-TRIAZOLO(4,5-D)PYRIMIDIN-5-AMINE, 7-(5-METHYL-2-FURANYL)-3-((6-((((3S)-TETRAHYDRO-3-FURANYL)OXY)METHYL)-2-PYRIDINYL)METHYL)- (73 S)-15 -methyl-6-oxa-2(7,3)-[1,2,3]triazolo[4,5- d]pyrimidina-4(2,6)-pyridina-1(2)-furana-7(3)- oxolanaheptaphan-25 -amine adenosine receptor antagonist Ciforadenant, also known as CPI-444 and V81444, is an orally administered antagonist of the adenosine A2A receptor. …

GDC 0853, Fenebrutinib

It’s only fair to share…   . Picture credit….Bethany Halford GDC 0853, Fenebrutinib GDC-0853; RG 7845 Molecular Formula: C37H44N8O4 Molecular Weight: 664.79646 g/mol 2-[3-(hydroxymethyl)-4-[1-methyl-5-[(7-methyl-6,8-dihydro-5H-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)amino]-6-oxo-3-pyridyl]-2-pyridyl]-3,4,6,7,8,9-hexahydropyrazino[1,2-a]indol-1-one 3-[3-(hydroxymethyl)-4-[1-methyl-5-[[5-[2-methyl-4-(oxetan-3-yl)piperazin-1-yl]pyridin-2-yl]amino]-6-oxopyridin-3-yl]pyridin-2-yl]-7,7-dimethyl-1,2,6,8-tetrahydrocyclopenta[3,4]pyrrolo[3,5-b]pyrazin-4-one 3-[3-(hydroxymethyl)-4-[5-[[5-[(2S)-2-methyl-4-(oxetan-3-yl)piperazin-1-yl]-2-pyridyl]amino]-6-oxo-1H-pyridin-3-yl]-2-pyridyl]-7,7-dimethyl-1,2,6,8-tetrahydrocyclopenta[3,4]pyrrolo[3,5-b]pyrazin-4-one 2H-Cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one, 2-[1,6-dihydro-3′-(hydroxymethyl)-1-methyl-5-[[5-[(2S) -2-methyl-4-(3-oxetanyl)-1-piperazinyl]-2-pyridinyl]amino] -6-oxo[3,4′-bipyridin]-2′-yl]-3,4,7,8-tetrahydro-7,7- dimethyl- s ISoMER 1434048-34-6 desired r iSoMER 1434048-57-3 undesired   Phase 1 Patients with Patients with Resistant B-Cell Lymphoma or Chronic Lymphocytic Leukemia.. @genentech‘s Btk inhibitor https://clinicaltrials.gov/ct2/show/NCT01991184 Bruton tyrosine …

YINLITINIB

It’s only fair to share…   YINLITINIB error EMAIL ME amcrasto@gmail.com (E)-4-[(4aR,7aS)-2,3,4a,5,7,7a-hexahydro-[1,4]dioxino[2,3-c]pyrrol-6-yl]-N-[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-6-yl]but-2-enamide (E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)-4-((4aR,7aS)-tetrahydro-2H-[1,4]dioxin[2,3-c]pyrrol-6(3H)-yl)but-2-enamide CAS 1637253-79-2 2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-[(4aR,7aS)-hexahydro-6H-1,4-dioxino[2,3-c]pyrrol-6-yl]-, (2E)-rel– C25 H25 Cl F N5 O4, 513.95 DNT-04110 ; yinlitinib maleate , Guangdong Hec Pharmaceutical Use for treating proliferative diseases, atherosclerosis and pulmonary fibrosis Phase I CHINA NOTE AND USE YOUR JUDGMENT ON DRUG SUBSTANCE, EMAIL ME amcrasto@gmail.com Molecular Formula: C25H25ClFN5O4 Molecular Weight: …

Empesertib , BAY 1161909

It’s only fair to share… Empesertib , BAY 1161909, Mps1-IN-5,  (-)-BAY-1161909 CAS 1443763-60-7 Chemical Formula: C29H26FN5O4S Molecular Weight: 559.6164 [a]D20 : -78.9° (in DMSO). WO 2014198647 UNII-02Y3Z2756M (αR)-4-Fluoro-N-[4-[2-[[2-methoxy-4-(methylsulfonyl)phenyl]amino][1,2,4]triazolo[1,5-a]pyridin-6-yl]phenyl]-α-methylbenzeneacetamide (R)-2-(4-fluorophenyl)-N-(4-(2-((2-methoxy-4-(methylsulfonyl)phenyl)amino)-[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl)propanamide (2R)-2-(4-Fluorophenyl)-N-(4-(2-((4-(methanesulfonyl)-2-methoxyphenyl)amino)(1,2,4)triazolo(1,5-a)pyridin-6-yl)phenyl)propanamide Benzeneacetamide, 4-fluoro-N-(4-(2-((2-methoxy-4-(methylsulfonyl)phenyl)amino)(1,2,4)triazolo(1,5-a)pyridin-6-yl)phenyl)-alpha-methyl-, (alphaR)- PHASE 1, BAYER, CANCER PRODUCT PATENT, WO2013087579, https://www.google.com/patents/WO2013087579A1   SYNTHESIS,  WO 2014198647 Analytical UPLC-MS was performed as follows: Method A: System: UPLC Acquity (Waters) with PDA Detector und Waters …

PH 46A

It’s only fair to share… PH 46A cas  1421332-97-9 C27 H24 O3, 396.48 Benzoic acid, 4-[[(1S,2S)-2,3-dihydro-1-hydroxy[2,2′-bi-1H-inden]-2-yl]methyl]-, methyl ester Methyl 4-(((1S,2S)-1-hydroxy-2,3-dihydro-1H,1’H-[2,2′-biinden]-2-yl)methyl)benzoate FREE ACID CAS  1380445-03-3, Benzoic acid, 4-[[(1S,2S)-2,3-dihydro-1-hydroxy[2,2′-bi-1H-inden]-2-yl]methyl]- N-Methyl-(D)-Glucamine salt (NMDG) 1380445-04-4 C26 H22 O3 . C7 H17 N O5 D-Glucitol, 1-deoxy-1-(methylamino)-, 4-[[(1S,2S)-2,3-dihydro-1-hydroxy[2,2′-bi-1H-inden]-2-yl]methyl]benzoate (1:1) PH46A, belonging to a class of 1,2-Indane dimers, has been developed by  Trino Therapeutics Ltd research group as a potential therapeutic agent …

AD 35

It’s only fair to share… AD 35 IND-120499 MF C24 H27 N3 O3 Molecular Weight, 405.49 Spiro[cyclopropane-1,5′-[5H-1,3]dioxolo[4,5-f]isoindol]-7′(6′H)-one, 6′-[2-[1-(2-pyridinylmethyl)-4-piperidinyl]ethyl]- 6′-[2-[1-(2-Pyridinylmethyl)-4-piperidinyl]ethyl]spiro[cyclopropane-1,5′-[5H-1,3]dioxolo[4,5-f]isoindol]-7′(6’H)-one 1531586-58-9 CAS FREE FORM 1531586-64-7  PHOSPHATE 1531586-62-5  HYDROCHLORIDE Zhejiang Hisun Pharmaceutical Co Ltd AD-35 is known to be a neuroprotectant, useful for treating Alzheimer’s diseases. Zhejiang Hisun Pharmaceutical is developing an oral tablet formulation of AD-35, for treating Alzheimers disease …

BMS 986205

It’s only fair to share… BMS 986205 (2R)-N-(4-Chlorophenyl)-2-[cis-4-(6-fluoro-4-quinolinyl)cyclohexyl]propanamide Cyclohexaneacetamide, N-(4-chlorophenyl)-4-(6-fluoro-4-quinolinyl)-α-methyl-, cis- Cyclohexaneacetamide, N-(4-chlorophenyl)-4-(6-fluoro-4-quinolinyl)-α-methyl-, cis-(αR)- (i?)-N-(4-chlorophenyl)-2- c 5-4-(6-fluoroquinolin-4-yl)cyclohexyl)propanamide CAS: 1923833-60-6 Phase 1 cancer BMS-986205, ONO-7701,  F- 001287 Molecular Formula C24H24ClFN2O Average mass 410.912 Da Originator Bristol-Myers Squibb Class Antineoplastics 01 Feb 2016 Phase-I/II clinical trials in Cancer (Combination therapy, Late-stage disease, Second-line therapy or greater) in Canada (PO) (NCT02658890) 31 Jan 2016 Preclinical …

BLU 285

It’s only fair to share… BLU-285 CAS 1703793-34-3 Molecular FormulaC26H27FN10 Average mass498.558 Da (1S)-1-(4-Fluorophenyl)-1-(2-{4-[6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]-1-piperazinyl}-5-pyrimidinyl)ethanamine 5-Pyrimidinemethanamine, α-(4-fluorophenyl)-α-methyl-2-[4-[6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]-1-piperazinyl]-, (αS)- 5-Pyrimidinemethanamine, α-(4-fluorophenyl)-α-methyl-2-[4-[6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]-1-piperazinyl]-, (αS)- Originator Blueprint Medicines Class Antineoplastics; Skin disorder therapies; Small molecules Mechanism of Action Platelet-derived growth factor alpha receptor modulators; Proto oncogene protein c-kit inhibitors Orphan Drug Status Yes – Systemic mastocytosis; Gastrointestinal stromal tumours Phase I Gastrointestinal stromal tumours; Solid tumours; …

GSK 3008348

It’s only fair to share… GSK 3008348 (3S)-3-[3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl]-4-{(3S)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]-1-pyrrolidinyl}butanoic acid cas 1629249-33-7 1-Pyrrolidinebutanoic acid, β-[3-(3,5-dimethyl-1H-pyrazol-1-yl)phenyl]-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]-, (βS,3R)- (S)-3-(3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl)-4-((R)-3-(2-(5,6,7,8-tetrahydro-1,8- naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic acid (βS,3R)-β-[3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl]-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]-1-pyrrolidinebutanoic acid Molecular Formula C29H37N5O2 Average mass 487.636 Da   CAS Number: 1629249-40-6 Molecular Weight: 524.1 Molecular Formula: C29H38ClN5O2 Originator GlaxoSmithKline Mechanism of Action Integrin alphaV antagonists Phase I Idiopathic pulmonary fibrosis 06 Mar 2017 GlaxoSmithKline plans a phase I trial for Idiopathic pulmonary …