Category «PHASE 1»

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 …

AMG 176

It’s only fair to share…   AMG 176 C33 H41 Cl N2 O5 S, 613.21 14E/8’E Spiro[5,7-etheno-1H,11H-cyclobut[i][1,4]oxazepino[3,4-f][1,2,7]thiadiazacyclohexadecine-2(3H),1′(2′H)-naphthalen]-8(9H)-one, 6′-chloro-3′,4′,12,13,16,16a,17,18,18a,19-decahydro-16-methoxy-11,12-dimethyl-, 10,10-dioxide, (1′S,11R,12S,14E,16S,16aR,18aR)- (1S,3’R,6’R,7’S,8’E,1 l’R,12’R)-6-CHLORO-7′-METHOXY-l 1′-METHYL- 12′-( 1 -METHYL)-3 ,4-DIHYDRO-2H, 15 Ή-SPIRO [NAPHTHALENE- 1 ,22′- [20]OXA[13]THIA[1,14]DIAZATETRACYCLO[14.7.2.03‘6.019‘24]PENTACOS A[8,16,18,24]TETRAEN]-15′-ONE 13 ‘,13 ‘-DIOXIDE E FORM 1883727-34-1 . . . 14Z/8’Z Spiro[5,7-etheno-1H,11H-cyclobut[i][1,4]oxazepino[3,4-f][1,2,7]thiadiazacyclohexadecine-2(3H),1′(2′H)-naphthalen]-8(9H)-one, 6′-chloro-3′,4′,12,13,16,16a,17,18,18a,19-decahydro-16-methoxy-11,12-dimethyl-, 10,10-dioxide, (1′S,11R,12S,14Z,16S,16aR,18aR)- (1S,3’R,6’R,7’S,8’Z,1 l’R,12’R)-6-CHLORO-7′-METHOXY-l 1′-METHYL- 12′-( 1 -METHYL)-3 ,4-DIHYDRO-2H, 15 Ή-SPIRO …

FGF 401

It’s only fair to share… FGF 401 NVP-FGF-401 CAS 1708971-55-4 MF C25 H30 N8 O4, MW 506.56 1,8-Naphthyridine-1(2H)-carboxamide, N-[5-cyano-4-[(2-methoxyethyl)amino]-2-pyridinyl]-7-formyl-3,4-dihydro-6-[(4-methyl-2-oxo-1-piperazinyl)methyl]- N-[5-Cyano-4-[(2-methoxyethyl)amino]-2-pyridinyl]-7-formyl-3,4-dihydro-6-[(4-methyl-2-oxo-1-piperazinyl)methyl]-1,8-naphthyridine-1(2H)-carboxamide /V-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1 -yl)methyl)-3,4-dihydro-1 ,8-naphthyridine-1 (2H)-carboxamide Phase I/II Hepatocellular carcinoma; Solid tumours  Originator Novartis Developer Novartis Oncology Class Antineoplastics Mechanism of Action Type 4 fibroblast growth factor receptor antagonists 26 Jan 2016 Phase-I/II clinical trials in Solid tumours and Hepatocellular carcinoma in USA, Hong …

PRN 1371

It’s only fair to share… PRN 1371 Molecular Formula C26H30Cl2N6O4 Average mass 561.460 cas 1802929-43-6 8-[3-(4-Acryloyl-1-piperazinyl)propyl]-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one 6-(2,6-Dichloro-3,5-dimethoxyphenyl)-2-(methylamino)-8-[3-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]propyl]pyrido[2,3-d]pyrimidin-7(8H)-one Phase I Solid tumours Originator Principia Biopharma Class Small molecules Mechanism of Action Fibroblast growth factor receptor antagonists 06 Jun 2016 Adverse events data from a phase I trial in Solid tumours presented at the 52nd Annual Meeting of the American Society of Clinical Oncology (ASCO- …

BLU 554

It’s only fair to share… BLU 554 FGFR4 Inhibitor N-[(3S,4S)-3-[[6-(2,6-Dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl]amino]tetrahydro-2H-pyran-4-yl]-2-propenamide N-[(3S,4S)-3-[[6-(2,6-Dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino]tetrahydro-2H-pyran-4-yl]acrylamide CAS No. 1707289-21-1 Formula C24H24Cl2N4O4 MolWeight 503.378 PHASE 1 BLU-554 is a potent fibroblast growth factor receptor 4 (FGFR4) inhibitor. IC50 & Target: FGFR4[1] InVitro: Fibroblast growth factor receptor 4 (FGFR-4) is a protein that in humans is encoded by the FGFR-4 gene. This …