Category «Preclinical»

LINZAGOLIX

It’s only fair to share… LINZAGOLIX CAS 935283-04-8 C22H15F3N2O7S Hormone Antagonists 3-[5-[(2,3-difluoro-6-methoxyphenyl)methoxy]-2-fluoro-4-methoxyphenyl]-2,4-dioxo-1H-thieno[3,4-d]pyrimidine-5-carboxylic acid WHO 10711 Treatment of Endometriosis Pain and Uterine Myoma-Associated Heavy Menstrual Bleeding OriginatorKissei Pharmaceutical DeveloperKissei Pharmaceutical; ObsEva Class2 ring heterocyclic compounds; Antihormones; Antineoplastics; Carboxylic acids; Fluorinated hydrocarbons; Ketones; Pyrimidines; Small molecules; Thiophenes Mechanism of ActionLHRH receptor antagonists PreregistrationUterine leiomyoma Phase IIIEndometriosis Phase IIAdenomyosis …

JNJ-A07

It’s only fair to share…     JNJ-A07 S + FORM CAS 2135640-93-4 ROT (+)S Butanoic acid, 4-[3-[[1-(4-chlorophenyl)-2-[2,3-dihydro-6-(trifluoromethoxy)-1H-indol-1-yl]-2-oxoethyl]amino]-5-methoxyphenoxy]-, (+)- (+)-4-[3-[[1-(4-Chlorophenyl)-2-[2,3-dihydro-6-(trifluoromethoxy)-1H-indol-1-yl]-2-oxoethyl]amino]-5-methoxyphenoxy]butanoic acid (+)-4-[3-([(1S)-1-(4-Chlorophenyl)-2-oxo-2-[6-(trifluoromethoxy)-2,3-dihydro-1H-indol-1-yl]ethyl]amino)-5-methoxyphenoxy]butanoic acid Molecular Formula C28 H26 Cl F3 N2 O6 Molecular Weight 578.964 REF Kaptein, S.J.F., Goethals, O., Kiemel, D. et al. A pan-serotype dengue virus inhibitor targeting the NS3–NS4B interaction. Nature (2021). https://doi.org/10.1038/s41586-021-03990-6 JNJ-018 CAS 2135640-91-2 +/-, R,S CAS 2135640-92-3 …

JBI-802 BY JUBILANT

It’s only fair to share… EXAMPLE O=C(OC)/C=C/c1ccc(CNC2CC2c2ccc(F)cc2)cc1 EXAMPLE ONLY JBI-802 Myeloid Leukemia Therapy Solid Tumors Therapy Epigenetic Modifier Modulators Histone Deacetylase 6 (HDAC6) Inhibitors Lysine-Specific Histone Demethylase 1A (KDM1A; LSD1) Inhibitors   Jubilant Therapeutics Announces Successful Completion of Pre-IND Meeting with FDA for its Novel Dual LSD1 and HDAC6 Inhibitor JB1-802 https://markets.businessinsider.com/news/stocks/jubilant-therapeutics-announces-successful-completion-of-pre-ind-meeting-with-fda-for-its-novel-dual-lsd1-and-hdac6-inhibitor-jb1-802-1030834551 PRESS RELEASE PR …

ADX-103

It’s only fair to share…   ADX-103 CAS 916056-81-0 Preclinical, Antiinflammatory Ophthalmic Agents, Diabetic Retinopathy, Agents for Ophthalmic Drugs MF C16 H16 N2 O2 5-Amino-α,α-dimethyl-2-phenyl-6-benzoxazolemethanol MW 268.31 6-Benzoxazolemethanol, 5-amino-α,α-dimethyl-2-phenyl- Aldeyra Therapeutics Inc ADX-103 , an aldehyde trap being investigated by Aldeyra for the treatment of dry eye syndrome; in May 2018, preclinical data were presented at 2018 ARVO Meeting in Honolulu, …

SK1-I , BML 258

It’s only fair to share…   SK1-I , BML 258 Sphingosine kinase 1 (SphK1) inhibitor; antiproliferative (1E)-1,2,4-Trideoxy-4-(methylamino)-1-(4-pentylphenyl)-D-erythro-pent-1-enitol (E,2R,3S)-2-(Methylamino)-5-(4-pentylphenyl)pent-4-ene-1,3-diol D-erythro-Pent-1-enitol, 1,2,4-trideoxy-4-(methylamino)-1-(4-pentylphenyl)-, (1E)- Name: (2R,3S,4E)-N-methyl-5-(4′-pentylphenyl)-2-aminopent-4-ene-1,3-diol . HCl Formula: C17H27NO2 . HCl MW: 313.9 CAS: 1072443-89-0   Originator Enzo Biochem; Virginia Commonwealth University Developer Enzo Biochem Class Antineoplastics; Small molecules Mechanism of Action Sphingosine kinase inhibitors Preclinical Autoimmune hepatitis; Haematological malignancies; Liver cancer; Solid tumours …

SYN-01

It’s only fair to share…     SYN-01, SYN-510 Synthena AG Preclinical Synthena , presumed to be under license from  University of Bern , is investigating (presumably SYN-01 ), a lead from the tricyclo(tc)-DNA based antisense oligonucleotides (AON) developed using its proprietary tricyclo-DNA technology platform, for the treatment of Duchenne muscular dystrophy. In January 2017, …

HS-10340

It’s only fair to share…   HS-10340 CAS 2156639-66-4 MF C26 H31 N7 O5 MW 521.57 1,8-Naphthyridine-1(2H)-carboxamide, N-[5-cyano-4-[[(1R)-2-methoxy-1-methylethyl]amino]-2-pyridinyl]-7-formyl-3,4-dihydro-6-[(tetrahydro-2-oxo-1,3-oxazepin-3(2H)-yl)methyl]- (R)-N-(5-cyano-4-((1-methoxypropan-2-yl)amino)pyridin-2-yl)-7-formyl-6-((2-carbonyl)-1,3-oxazepine-3-yl)methyl)-3,4-dihydro-1,8-naphthyridin-1(2H)-carboxamide CAS 2307670-65-9 Jiangsu Hansoh Pharmaceutical Group Co Ltd Being investigated by Jiangsu Hansoh, Shanghai Hansoh Biomedical and Changzhou Hengbang Pharmaceutical ; in June 2018, the product was being developed as a class 1 chemical drug in China. Useful for treating liver cancer, gastric …

CS-3001

It’s only fair to share…   CS-3001 BB 7, VX 033 CAS 2159116-56-8 Propanoic acid, 2-[[5-bromo-4-(3-cyclopropyl-5,5-difluoro-4,5,6,7-tetrahydrobenzo[c]thien-1-yl)-4H-1,2,4-triazol-3-yl]thio]-2-methyl- Molecular Weight, 478.37 C17 H18 Br F2 N3 O2 S2 CStone Pharmaceuticals Co Ltd, JUNE 2018 IND FILED CHINA URAT1 inhibitor – useful for treating hyperuricemia and gout. The compound was originally claimed in WO2017202291 , covering thiophene derivative URAT1 inhibitors, useful for treating hyperuricemia …

TL-487

It’s only fair to share… TL-487 CAS  1469746-55-1 2-Butenamide, N-[3-cyano-7-ethoxy-4-[(4-phenoxyphenyl)amino]-6-quinolinyl]-4-(dimethylamino)-, (2E)- Molecular Weight, 507.58, MF C30 H29 N5 O3 Teligene Inc(2E)-N-[3-Cyano-7-ethoxy-4-[(4-phenoxyphenyl)amino]-6-quinolinyl]-4-(dimethylamino)-2-butenamide (E)-N-(3-cyano-7-ethoxy-4-((4-phenoxyphenyl)amino)quinolin-6-yl)-4-(dimethylamino)but-2-enamide Maleate in anhydrous or monohydrate CAS, 2326561-36-6, AND 2326561-38-8 form are BTK and HER-2 kinase inhibitor useful for treating cancer Useful for treating breast cancer, ovary cancer and colon cancer. are BTK and HER-2 kinase inhibitor useful for treating cancer. Anticancer …

HM04 or H0900

It’s only fair to share…   HM04 or H0900 Cas 1808913-24-7 MF C20 H22 Cl2 F3 N5 O MW 476.32 Urea, N‘-[(1R)-1-[2,3-dichloro-4-(2-pyrazinyl)phenyl]-2,2,2-trifluoroethyl]-N-methyl-N-(1-methyl-4-piperidinyl)- (R)-3-(1-(2,3-dichloro-4-(pyrazin-2-yl)phenyl)-2,2,2-trifluoroethyl)-1-methyl-1-(1-methylpiperidin-4-yl) urea The compound was disclosed in WO2015134839 . Helsinn under license from Novo Nordisk , is investigating ghrelin antagonists for treating obesity, Prader-Willi syndrome and other metabolic disorders; in May 2015, the program was listed as being in preclinical …