Tag «Phase I»

RP 12146

It’s only fair to share…   RP 12146 RP-12146 is an oral poly (ADP-ribose) polymerase (PARP) inhibitor in phase I clinical development at Rhizen Pharmaceuticals for the treatment of adult patients with locally advanced or metastatic solid tumors. Solid TumorExtensive-stage Small-cell Lung CancerLocally Advanced Breast CancerMetastatic Breast CancerPlatinum-sensitive Ovarian CancerPlatinum-Sensitive Fallopian Tube CarcinomaPlatinum-Sensitive Peritoneal Cancer …

ABBV 744

It’s only fair to share…   ABBV 744 N-Ethyl-4-[2-(4-fluoro-2,6-dimethylphenoxy)-5-(1-hydroxy-1-methylethyl)phenyl]-6,7-dihydro-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide 1H-Pyrrolo[2,3-c]pyridine-2-carboxamide, N-ethyl-4-[2-(4-fluoro-2,6-dimethylphenoxy)-5-(1-hydroxy-1-methylethyl)phenyl]-6,7-dihydro-6-methyl-7-oxo- Molecular Weight 491.55 Formula C₂₈H₃₀FN₃O₄ CAS No. 2138861-99-9 ABBV-744 is a highly BDII-selective BET bromodomain inhibitor, used in the research of inflammatory diseases, cancer, and AIDS. Acute Myeloid Leukemia (AML) Phase I, AbbVie is evaluating oral agent ABBV-744 in early clinical trials for the treatment of metastatic castration …

LNS-8801 (SRR G-1)

It’s only fair to share…   LNS-8801 (SRR G-1) CAS  925419-53-0 Chemokine receptor-like 2 agonist C21 H18 Br N O3, 412.28 Ethanone, 1-[(3aS,4R,9bR)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]- 1-((3aS,4R,9bR)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl)ethan-1-one 1-[(3aS,4R,9bR)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]ethanone G 1 G 1 (estrogen receptor agonist)   Linnaeus Therapeutics Inc NOTE 1-((3aR,4S,9bR)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl)ethan-1-one (RSS G-1 or LNS8812)  Novel crystalline forms of an enantiomerically purified LNS-8801 (SRR G-1), or a derivative useful for treating cancer, …

CC-90009

It’s only fair to share… CC-90009 CC-90009-AML-001 CAS 1860875-51-9 461.8 g/mol, C22H18ClF2N3O4 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide 4-Chloro-N-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-5-yl]methyl]-α,α-difluorobenzeneacetamide Benzeneacetamide, 4-chloro-N-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-5-yl]methyl]-α,α-difluoro- Phase 1 Clinical, Acute myelogenous leukemia, Protein cereblon modulator Useful for treating chronic lymphocytic leukemia, chronic myelocytic leukemia, acute lymphoblastic leukemia or acute myeloid leukemia. Celgene is developing CC-90009, a cereblon E3 ligase modulator, for treating AML; in January 2019, data from a …

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 …

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 …

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 …

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- …