Category «PHASE 1»

TAK-981

It’s only fair to share… TAK-981 C25 H28 Cl N5 O5 S2, 578.103 [(1R,2S,4R)-4-[(5-[4-[(1R)-7-Chloro-1,2,3,4-tetrahydroisoquinolin-1-yl]-5-methylthiophene-2-carbonyl]pyrimidin-4-yl)amino]-2-hydroxycyclopentyl]methyl sulfamate [(1R,2S,4R)-4-[[5-[4-[(1R)-7-Chloro-1,2,3,4-tetrahydroisoquinolin-1-yl]-5-methyl-thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxy-cyclopentyl]methyl sulfamate Sulfamic acid, [(1R,2S,4R)-4-[[5-[[4-[(1R)-7-chloro-1,2,3,4-tetrahydro-1-isoquinolinyl]-5-methyl-2-thienyl]carbonyl]-4-pyrimidinyl]amino]-2-hydroxycyclopentyl]methyl ester CAS 1858276-04-6 FREE CAS 1858279-63-6 HYDRATE  MW 578.103 Originator Takeda Oncology Class Antineoplastics Mechanism of Action Small ubiquitin-related modifier protein inhibitors Phase I Lymphoma; Solid tumours 01 Oct 2018 Phase-I clinical trials in Solid tumours (Late-stage disease, Metastatic disease) and and Lymphoma …

BIIB-095

It’s only fair to share… BIIB-095 ROTATION (+) 1493790-64-9 CAS free form, 1493772-48-7 cas Hcl salt cas 1493790-65-0, 1496563-32-6 ,SULPHATE ??? cas 1496563-31-5  SULFATE 1;1 cas 1496563-32-6 SULFATE HYDRATE 1;1;1 (2R,5S)-7-methyl-2-[4-methyl-6-[4-(trifluoromethyl)-phenyl]pyrimidin-2-yl]-1 ,7-diazaspiro[4.4]nonan-6-one 1,7-Diazaspiro[4.4]nonan-6-one, 7-methyl-2-[4-methyl-6-[4-(trifluoromethyl)phenyl]-2-pyrimidinyl]-, (2R,5S)- C20 H21 F3 N4 O, 390.40 Originator Biogen Class Analgesics Mechanism of Action Nav1.7 voltage-gated sodium channel inhibitors Phase I Neuropathic pain 29 Mar 2018 Phase-I clinical trials in Neuropathic pain (In volunteers) in …

VNRX-7145

It’s only fair to share… CAS 1842399-68-1 MF C19 H26 B N O7 MW 391.22 2H-1,2-Benzoxaborin-8-carboxylic acid, 3,4-dihydro-2-hydroxy-3-[(1-oxopropyl)amino]-, (2-ethyl-1-oxobutoxy)methyl ester, (3R)- The VNRX-7145 combination is now in Phase I studies to treat resistant urinary tract infections. VNRX-7145 PATENT WO 2015191907 https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2015191907 ntibiotics are the most effective drugs for curing bacteria-infectious diseases clinically. They have a wide market due to …

LHC 165

It’s only fair to share… LHC165 3-[5-amino-2-[2-[4-[2-(3,3-difluoro-3-phosphonopropoxy)ethoxy]-2-methylphenyl]ethyl]benzo[f][1,7]naphthyridin-8-yl]propanoic acid C29H32F2N3O7P, 603.56 g/mol CAS  1258595-14-0 5-Amino-2-[2-[4-[2-(3,3-difluoro-3-phosphonopropoxy)ethoxy]-2-methylphenyl]ethyl]benzo[f][1,7]naphthyridine-8-propanoic acid Benzo[f][1,7]naphthyridine-8-propanoic acid, 5-amino-2-[2-[4-[2-(3,3-difluoro-3-phosphonopropoxy)ethoxy]-2-methylphenyl]ethyl]- Originator Novartis Class Antineoplastics Mechanism of Action Undefined mechanism Phase I Solid tumours 31 Jan 2018 Phase-I clinical trials in Solid tumours (Combination therapy, Inoperable/Unresectable, Late-stage disease, Metastatic disease, Second-line therapy or greater) in USA, Belgium, Italy, Japan (Intratumoural) (NCT03301896) 31 Jan 2018 Phase-I …

AB 680

It’s only fair to share… AB 680 C20H24ClFN4O9P2, 580.827 g/mol Cas 2105904-82-1 1H-Pyrazolo[3,4-b]pyridin-4-amine, 6-chloro-N-[(1S)-1-(2-fluorophenyl)ethyl]-1-[5-O-[hydroxy(phosphonomethyl)phosphinyl]-β-D-ribofuranosyl]- [[(2R,3S,4R,5R)-5-[6-chloro-4-[[(1S)-1-(2-fluorophenyl)ethyl]amino]pyrazolo[3,4-b]pyridin-1-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]methylphosphonic acid [({[(2R,3S,4R,5R)-5-(6-chloro-4-{[(1S)-1-(2-fluorophenyl)ethyl]amino}-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy}(hydroxy)phosphoryl)methyl]phosphonic Acid Originator C Class Antineoplastics; Small molecules Mechanism of Action 5-nucleotidase inhibitors; Adenosine A2 receptor antagonists Phase I Cancer 19 Nov 2018 Arcus Biosciences plans to initiate a clinical trial in Cancer in first half of 2019 16 Oct 2018 Phase-I clinical trials in Cancer (In …

CMX-8521, CMX-521

It’s only fair to share… CMX-8521, CMX-521 MF C13 H17 N5 O5,  MW 323.30 CAS Number 2077178-99-3 7H-Pyrrolo[2,3-d]pyrimidine-5-carboxamide, 4-amino-2-methyl-7-β-D-ribofuranosyl- Nucleoside analogs (oral, norovirus infection), Chimerix 4-amino-7-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-methyl-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide 4-amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-2-methylpyrrolo[2,3-d]pyrimidine-5-carboxamide CMX8521 is a nucleoside analog that inhibits the norovirus RNA polymerase. CMX8521 has in vitro activity against mouse and human norovirus.Where possible, Chimerix uses its lipid conjugate technology to build nucleoside-analog antivirals that …

PF 06650808

It’s only fair to share… . Picture credit….Bethany Halford PF 06650808 CAS 1822383-80-1 A biologic for cancer treatment (Pfizer Inc.) Originator Pfizer Class Antineoplastics Mechanism of Action Notch-3 receptor antagonists No development reported Solid tumours 24 Jun 2018 Biomarkers information updated 28 Apr 2018 No recent reports of development identified for phase-I development in Solid-tumours(Late-stage disease) in USA (IV) 01 Jul 2017 Pfizer …

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 …