Category «PHASE 1»

MEVOCICLIB

It’s only fair to share… MEVOCICLIB, CAS 1816989-16-8 SY 1365 N-[(1S,3R)-3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]-1-methylcyclohexyl]-5-[[(E)-4-(dimethylamino)but-2-enoyl]amino]pyridine-2-carboxamide N-((lS,3R)-3-(5-chloro-4-(lH-indol-3-yl)pyrimidin-2-ylamino)-l-methylcvclohexyl)-5-((E)-4-(dimethylamino)but-2-enamido)picolinamide HS Tariff Code: 2934.99.9001 Syros Molecular Weight 587.12 Formula C₃₁H₃₅ClN₈O₂ OriginatorSyros Pharmaceuticals ClassAmides; Amines; Antineoplastics; Chlorinated hydrocarbons; Cyclohexanes; Indoles; Pyridines; Pyrimidines; Small molecules Mechanism of ActionCyclin-dependent kinase-activating kinase inhibitors DiscontinuedAcute myeloid leukaemia; Breast cancer; Haematological malignancies; Ovarian cancer; Solid tumours 23 Oct 2019Discontinued – …

SY 5609

It’s only fair to share… [ Fig. 0001] [ Fig. 0002] [ Fig. 0003] [ Fig. 0004]  https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2016058544&tab=FULLTEXT&_cid=P10-KTPTVL-74436-1 SY 5609 CAS 2519828-12-5 Cancer, solid tumor PHASE 1 A highly selective and potent oral inhibitor of cyclin-dependent kinase 7 (CDK7) for potential treatment of advanced solid tumors that harbor the Rb pa thway alterations (Syros Pharmaceuticals, Inc., Cambridge, Massachusetts, USA) …

MAX 40279

It’s only fair to share… MAX 40279, EX-A4057 Max 4; MAX-40279; MAX-40279-001; MAX-40279-01 UNII-DL772G3NN7 2070931-57-4 C22H23FN6OS, 438.5 7-(4-fluoro-2-methoxyphenyl)-6-methyl-N-(1-piperidin-4-ylpyrazol-4-yl)thieno[3,2-d]pyrimidin-2-amine Thieno[3,2-d]pyrimidin-2-amine, 7-(4-fluoro-2-methoxyphenyl)-6-methyl-N-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-   7-(4-FLUORO-2-METHOXYPHENYL)-6-METHYL-N-(1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL) THIENO (3,2-D)PYRIMIDIN-2-AMINE SEMI-FUMARATE CAS 2388506-43-0 7-(4-Fluoro-2-methoxyphenyl)-6-methyl-N-[1-(4-piperidinyl)-1H-pyrazol-4-yl]thieno[3,2-d]pyrimidin-2-amine Originator Maxinovel Pharmaceuticals ClassAntineoplastics Mechanism of ActionFibroblast growth factor receptor antagonists; Fms-like tyrosine kinase 3 inhibitors Orphan Drug StatusYes – Acute myeloid leukaemia Phase IAcute myeloid leukaemia; Solid tumours Most Recent …

TRK-700

It’s only fair to share… TRK-700 CAS 1463432-16-7 C14 H24 N4 O 264.37 1-Propanone, 1-[4-(dimethylamino)-1-piperidinyl]-3-(1-methyl-1H-imidazol-2-yl)- 1-[4-(dimethylamino)piperidin-1-yl]-3-(1-methylimidazol-2-yl)propan-1-one 1-[4-(Dimethylamino)-1-piperidinyl]-3-(1-methyl-1H-imidazol-2-yl)-1-propanone OriginatorToray Industries ClassAnalgesics Mechanism of ActionUndefined mechanism Phase IIPostherpetic neuralgia PreclinicalPeripheral nervous system diseases 12 Sep 2018Pharmacodynamics data from a preclinical trial in Peripheral neuropathy presented at the 17th World Congress on Pain (WCP-2018) 01 Jul 2017Toray Industries completes a phase II trial …

PRN-473

It’s only fair to share…   PRN-473 SAR-444727 1414354-91-8 C30 H30 F N7 O2 Molecular Weight539.60 1-Piperidinepropanenitrile, 3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-α-(2,2-dimethylpropylidene)-β-oxo-, (3R)- (3R)-3-[4-Amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-α-(2,2-dimethylpropylidene)-β-oxo-1-piperidinepropanenitrile 2-(3-(4-amino~3-(2-fiuoro~4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carbonyl)-4,4-dimethylpent-2-enenitrile 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4,4-dimethylpent-2-enenitrile OriginatorPrincipia Biopharma ClassSmall molecules Mechanism of ActionAgammaglobulinaemia tyrosine kinase inhibitors Phase IAutoimmune disorders DiscontinuedArthritis 28 Sep 2020Principia Biopharma has been acquired by Sanofi 22 Jun 2020Principia Biopharma plans a pharmacokinetic phase I trial (In volunteers) for Hypersensitivity …

PF-07321332

It’s only fair to share… PF-07321332 https://clinicaltrials.gov/ct2/show/NCT04756531 PFIZER INITIATES PHASE 1 STUDY OF NOVEL ORAL ANTIVIRAL THERAPEUTIC AGENT AGAINST SARS-COV-2 Tuesday, March 23, 2021 – 11:00am In-vitro studies conducted to date show that the clinical candidate PF-07321332 is a potent protease inhibitor with potent anti-viral activity against SARS-CoV-2 This is the first orally administered coronavirus-specific …

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-90010

It’s only fair to share… CC-90010 C21 H21 N O4 S, 383.46 CAS 1706738-98-8 1(2H)-Isoquinolinone, 4-[2-(cyclopropylmethoxy)-5-(methylsulfonyl)phenyl]-2-methyl- 4-[2-(Cyclopropylmethoxy)-5-(methylsulfonyl)phenyl]-2-methyl-1(2H)-isoquinolinone 4-[2-(Cyclopropylmethoxy)-5-(methanesulfonyl)phenyl]-2-methylisoquinolin-1(2H)-one 4-[2-(Cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one Quanticel Pharmaceuticals Inc, Michael John BennettJuan Manuel BetancortAmogh BoloorStephen W. KaldorJeffrey Alan StaffordJames Marvin Veal Celgene  (now a wholly owned subsidiary of  Bristol-Myers Squibb ) , following its acquisition of  Quanticel , is developing CC-90010, an oral inhibitor of BET (bromodomain and extraterminal) …

IIIM-290

It’s only fair to share…   IIIM-290 4H-1-Benzopyran-4-one, 2-[2-(2,6-dichlorophenyl)ethenyl]-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]- Molecular Weight 462.32 Formula C₂₃H₂₁Cl₂NO₅ CAS No. 2213468-64-3 CSIR-IIIM Jammu has filed an IND Application of “IIIM-290” to Drug Controller General of India for conducting Phase I/Phase II clinical trial of its capsule formulation in patients with locally advanced or metastatic pancreatic cancer. This IND candidate …