Category «PHASE 1»

LORPUCITINIB

It’s only fair to share…   LORPUCITINIB JNJ 64251330 2230282-02-5 UNII-OE1QTY7C25 Molecular Weight 408.50 Formula C22H28N6O2 1-(TRANS-4-(CYANOMETHYL)CYCLOHEXYL)-1,6-DIHYDRO-N-(2-HYDROXY-2-METHYLPROPYL)IMIDAZO(4,5-D)PYRROLO(2,3-B)PYRIDINE-2-ACETAMIDE 2-[3-[4-(cyanomethyl)cyclohexyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]-N-(2-hydroxy-2-methylpropyl)acetamide is a Gut-Restricted JAK Inhibitor for the research of Inflammatory Bowel Disease. Lorpucitinib is an orally bioavailable pan-inhibitor of the Janus associated-kinases (JAKs), with potential immunomodulatory and anti-inflammatory activities. Upon oral administration, lorpucitinib works in the gastrointestinal (GI) tract …

Danavorexton, TAK 925

It’s only fair to share…   Danavorexton,  TAK 925 2114324-48-8 Molecular FormulaC21H32N2O5S Average mass424.554 Da 1-Piperidinecarboxylic acid, 3-[(methylsulfonyl)amino]-2-[[(cis-4-phenylcyclohexyl)oxy]methyl]-, methyl ester, (2R,3S)- Methyl (2R,3S)-3-[(methylsulfonyl)amino]-2-[[(cis-4-phenylcyclohexyl)oxy]methyl]-1-piperidinecarboxylate OriginatorTakeda ClassCyclohexanes; Esters; Ethers; Piperidines; Sleep disorder therapies; Small molecules; Sulfonamides Mechanism of ActionOrexin receptor type 2 agonists Orphan Drug StatusYes – Narcolepsy Phase IHypersomnia; Narcolepsy; Respiration disorders; Sleep apnoea syndrome 01 …

ARIMOCLOMOL

It’s only fair to share… ARIMOCLOMOL アリモクロモル; Formula C14H20ClN3O3 Exact mass 313.1193 Mol weight 313.7799 CAS 289893-25-0 289893-26-1 (Arimoclomol maleate); INN 8300 N-[(2R)-2-hydroxy-3-piperidin-1-ylpropoxy]-1-oxidopyridin-1-ium-3-carboximidoyl chloride BRX 220 Arimoclomol maleate is in a phase III clinical trials by Orphazyme for the treatment of Niemann-Pick disease type C (NP-C). It is also in phase II clinical studies for the …

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 …