Category «PHASE 1»

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: …

THELIATINIB

It’s only fair to share…     THELIATINIB CAS: 1353644-70-8 Chemical Formula: C25H26N6O2 Molecular Weight: 442.523 HMPL-309; HMPL 309; HMPL309; Theliatinib. Originator Hutchison MediPharma Class Antineoplastics; Small molecules Mechanism of Action Epidermal growth factor receptor antagonists Highest Development Phases Phase I Oesophageal cancer; Solid tumours Most Recent Events 29 Sep 2017 Efficacy and adverse events data from a phase I …

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 …

AZD 9567

It’s only fair to share… AZD 9567 CAS 1893415-00-3 1893415-64-9  as MONOHYDRATE 2,2-Difluoro-N-[(1R,2S)-3-methyl-1-[[1-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-1H-indazol-5-yl]oxy]-1-phenylbutan-2-yl]propanamide Propanamide, N-[(1S)-1-[(R)-[[1-(1,6-dihydro-1-methyl-6-oxo-3-pyridinyl)-1H-indazol-5-yl]oxy]phenylmethyl]-2-methylpropyl]-2,2-difluoro- 2,2-difluoro-N-[(1R,2S)-3-methyl-1-[1-(1-methyl-6-oxopyridin-3-yl)indazol-5-yl]oxy-1-phenylbutan-2-yl]propanamide 2,2-difluoro- V-[(lR,25)-3-methyl-l-{[l-(l-methyl-6-oxo-l,6-dihydropyridin-3-yl)-lH-indazol-5-yl]oxy}-l-phenylbutan-2-yl]propanamide MF C27 H28 F2 N4 O3, MF 494.533 AstraZeneca INNOVATOR AZD-9567, a glucocorticoid receptor modulator, is in early clinical development at AstraZeneca in healthy male volunteers. Phase I Rheumatoid arthritis Originator AstraZeneca Class Antirheumatics Mechanism of Action Glucocorticoid receptor modulators 01 Sep 2016 AstraZeneca completes a …

PF 06648671

It’s only fair to share… PF-06648671, PF 06648671,  PF-6648671 CAS 1587727-31-8 C25 H23 Cl F4 N4 O3 538.92 2H-Pyrido[1,2-a]pyrazine-1,6-dione, 2-[(1S)-1-[(2S,5R)-5-[4-chloro-5-fluoro-2-(trifluoromethyl)phenyl]tetrahydro-2-furanyl]ethyl]-3,4-dihydro-7-(4-methyl-1H-imidazol-1-yl)- Phase I Alzheimer’s disease Originator Pfizer 01 Nov 2016 Pfizer completes a phase I pharmacokinetics trial in Healthy volunteers in USA (PO) (NCT02883114) 01 Oct 2016 Pfizer completes a phase I trial in Healthy volunteers in Belgium (NCT02440100) 01 …