Tag «PHASE 1»

Picropodophyllin

It’s only fair to share… Picropodophyllin Picropodophyllotoxin CAS 477-47-4 AXL1717, NSC 36407, BRN 0099161 414.4 g/mol, C22H22O8 (5R,5aR,8aS,9R)-5-hydroxy-9-(3,4,5-trimethoxyphenyl)-5a,6,8a,9-tetrahydro-5H-[2]benzofuro[5,6-f][1,3]benzodioxol-8-one Furo(3′,4′:6,7)naphtho(2,3-d)-1,3-dioxol-6(5aH)-one, 5,8,8a,9-tetrahydro-9-hydroxy-5-(3,4,5-trimethoxyphenyl)-, (5R-(5-alpha,5a-alpha,8a-alpha,9-alpha))- 5-19-10-00665 (Beilstein Handbook Reference) Axelar is developing picropodophyllin, a small-molecule IGF-1 receptor antagonist for the treatment of cancer including NSCLC and malignant astrocytoma. In February 2019, a phase Ia study was planned to initiate for solid tumor …

HEC-68498

It’s only fair to share…   HEC-68498, CT-365 CAS 1621718-37-3 C20 H13 F2 N5 O3 S 441.41 Benzenesulfonamide, N-[5-(3-cyanopyrazolo[1,5-a]pyridin-5-yl)-2-methoxy-3-pyridinyl]-2,4-difluoro- N-[5-(3-Cyanopyrazolo[1,5-a]pyridin-5-yl)-2-methoxy-3-pyridinyl]-2,4-difluorobenzenesulfonamide HEC Pharm , Calitor Sciences Llc; Sunshine Lake Pharma Co Ltd PHASE 1, idiopathic pulmonary fibrosis and solid tumors Phosphoinositide 3-kinase inhibitor; mTOR inhibitor Originator HEC Pharm Developer HEC Pharm; Sunshine Lake Pharma Class Anti-inflammatories; Antifibrotics; Isoenzymes Mechanism of Action 1 Phosphatidylinositol 3 kinase inhibitors; MTOR protein inhibitors …

GNE-0877

It’s only fair to share…     GNE-0877 Maybe  DNL-151 ? CAS 1374828-69-9 Chemical Formula: C14H16F3N7 Molecular Weight: 339.31895 2-methyl-2-(3-methyl-4-(4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-1H-pyrazol-1-yl)propanenitrile Denali Therapeutics Inc, useful for treating Alzheimer’s disease, breast tumor, type I diabetes mellitus and Crohn’s disease GNE-0877 is a highly potent and selective LRRK2 inhibitor. Leucine-rich repeat kinase 2 (LRRK2) has drawn significant interest in the neuroscience …

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 …

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 …