Category «PHASE 1»

ZY 19489, MMV 253

It’s only fair to share… ZY 19489, MMV 253 C24 H32 FN9, 465.5 CAS 1821293-40-6 MMV253, GTPL10024, MMV674253 N-(4-cyclopropyl-5-fluoro-6-methylpyridin-2-yl)-5-((3R)-2-((1,5-dimethyl-1H-pyrazol-3-yl)amino)-3,4-dimethylpiperazin-1-yl)pyrimidin-2-amine 2-N-(4-cyclopropyl-5-fluoro-6-methylpyridin-2-yl)-5-[(3R)-3,4-dimethylpiperazin-1-yl]-4-N-(1,5-dimethylpyrazol-3-yl)pyrimidine-2,4-diamine N2-(4-Cyclopropyl-5-fluoro-6-methyl-2-pyridinyl)-5-[(3R)-3,4-dimethyl-1-piperazinyl]-N4-(1,5-dimethyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine (R)-N2-(4-Cyclopropyl-5-fluoro-6-methylpyridin-2-yl)-N4-(1,5-dimethyl-1H-pyrazol-3-yl)-5-(3,4-dimethylpiperazin-1-yl)pyrimidine-2,4-diamine SYN IN 201721031453 The invention relates to triaminopyrimidine compd. of formula I, pharmaceutically acceptable salts thereof, hydrates, solvates, polymorphs, optically active forms thereof, in solid state forms useful for preventing or treating malaria.  The invention also relates …

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 …

XL 114, AUR 104 and XL 102, AUR 102 (NO CONCLUSIONS, ONLY PREDICTIONS)

It’s only fair to share… NO CONCLUSIONS, ONLY PREDICTIONS XL 102 XL 114 FOR BOTH, JUST PREDICTION         PREDICTIONS or       N[C@@H](CO)c1nc(on1)[C@@H](NC(=O)N[C@H](C(=O)O)C(C)O)CC(N)=O       (2S)-2-[[(1S)-3-amino-1-[3-[(1R)-1-amino-2-hydroxyethyl]-1,2,4-oxadiazol-5-yl]-3-oxopropyl]carbamoylamino]-3-hydroxybutanoic acid   CAS 2305027-62-5   C12 H20 N6 O7, 360.32Threonine, N-[[[(1S)-3-amino-1-[3-[(1R)-1-amino-2-hydroxyethyl]-1,2,4-oxadiazol-5-yl]-3-oxopropyl]amino]carbonyl]-, (2S,3ξ)-N[C@@H](CO)c1nc(on1)[C@@H](NC(=O)N[C@H](C(=O)O)C(C)O)CC(N)=O ALSO SEE         1673534-76-3C12 H20 N6 O7, 360.32 L-Threonine, N-[[[(1S)-3-amino-1-[3-[(1R)-1-amino-2-hydroxyethyl]-1,2,4-oxadiazol-5-yl]-3-oxopropyl]amino] (2S,3R)-2-[[(1S)-3-amino-1-[3-[(1R)-1-amino-2-hydroxyethyl]-1,2,4-oxadiazol-5-yl]-3-oxopropyl]carbamoylamino]-3-hydroxybutanoic acidN-[[[(1S)-3-Amino-1-[3-[(1R)-1-amino-2-hydroxyethyl]-1,2,4-oxadiazol-5-yl]-3-oxopropyl]amino]carbonyl]-L-threonine   CAS 1673534-76-3   PD-1-IN-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, Nirmatrelvir

It’s only fair to share… PF-07321332, nirmatrelvir UNII-7R9A5P7H32, 7R9A5P7H32, PF07321332 CAS 2628280-40-8, C23H32F3N5O4, 499.5 (1R,2S,5S)-N-[(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin-3-yl]ethyl]-3-[(2S)-3,3-dimethyl-2-[(2,2,2-trifluoroacetyl)amino]butanoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide Paxlovid (1R,2S,5S)-N-((1S)-1-Cyano-2-((3S)-2-oxopyrrolidin-3-yl)ethyl)-6,6-dimethyl-3-(3-methyl-N-(trifluoroacetyl)-L-valyl)-3-azabicyclo(3.1.0)hexane-2-carboxamide https://clinicaltrials.gov/ct2/show/NCT04756531 join me on Linkedin Anthony Melvin Crasto Ph.D – India | LinkedIn join me on Researchgate RESEARCHGATE join me on Facebook Anthony Melvin Crasto Dr. | Facebook Twitter FACEBOOK join me on twitter Anthony Melvin Crasto Dr. | twitter +919321316780 call whatsaapp EMAIL. amcrasto@amcrasto ///////////////////////////////////////////////////////////////////////////// SYN https://pubmed.ncbi.nlm.nih.gov/34726479/ …

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 …