Category «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 …

SHR-0532

It’s only fair to share… SHR-0532 CAS 2166329-09-3 C24 H26 N4 O5 . C4 H6 O6 2-Pyridinecarboxamide, 5-cyano-N-[1-[(2R)-2-(1,3-dihydro-4-methyl-1-oxo-5-isobenzofuranyl)-2-hydroxyethyl]-4-piperidinyl]-4-methoxy-, (2R,3R)-2,3-dihydroxybutanedioate (1:1) FREE FORM 1945997-37-4 C24 H26 N4 O5 450.49 2-Pyridinecarboxamide, 5-cyano-N-[1-[(2R)-2-(1,3-dihydro-4-methyl-1-oxo-5-isobenzofuranyl)-2-hydroxyethyl]-4-piperidinyl]-4-methoxy- 5-Cyano-N-[1-[(2R)-2-(1,3-dihydro-4-methyl-1-oxo-5-isobenzofuranyl)-2-hydroxyethyl]-4-piperidinyl]-4-methoxy-2-pyridinecarboxamide KCNJ potassium channel-1 inhibitor, Hypertension; Renal insufficiency Originator Jiangsu Hengrui Medicine Co. Class Antihypertensives Mechanism of Action Undefined mechanism Preclinical Hypertension 03 Jun 2019 Jiangsu Hengrui Medicine Co. plans a phase I trial for Hypertension (PO) in June 2019 (NCT03971929) …

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 …