Drug Approvals International – Page 116 – All about Drugs Live by Dr Anthony Melvin Crasto

LASMIDITAN

LASMIDITAN, COL-144 , LY-573144 Molecular FormulaC19H18F3N3O2 Average mass377.360 Da ласмидитан لاسميديتان 613677-28-4 HYDROCHLORIDE 439239-90-4 (free base) SUCCINATE 439239-92-6 2,4,6-Trifluoro-N-[6-(1-methylpiperidin-4-ylcarbonyl)pyridin-2-yl]benzamide 2,4,6-trifluoro-N-{6-[(1-methylpiperidin-4-yl)carbonyl]pyridin-2-yl}benzamide CoLucid Pharmaceuticals, PHASE 3, MIGRAINE UNII:760I9WM792 Lasmiditan is an oral medication used in the termination of migraine headaches that was first approved for use in the United States in October 2019. A high-affinity, highly selective serotonin 5-HT(1F) …

NASTORAZEPIDE

Nastorazepide (Z-360) CAS: 209219-38-5 Chemical Formula: C29H36N4O5 Molecular Weight: 520.61994 UNII-R22TMY97SG; 209219-38-5; Phase II, treatment of pancreatic cancer. (R)-3-(3-(5-cyclohexyl-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-3-yl)ureido)benzoic acid Nastorazepide, also known as Z-360, is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. Z-360 binds to the gastrin/CCK-2 receptor, thereby preventing receptor activation by gastrin, a peptide hormone …

OLINCIGUAT

OLINCIGUAT cas 1628732-62-6 Chemical Formula: C21H16F5N7O3 UNII-PD5F4ZXD21 Molecular Weight: 509.4 Olinciguat is a guanylate cyclase activator drug candidate. (2R)-3,3,3-trifluoro-2-{[(5-fluoro-2-{1-[(2-fluorophenyl)methyl]- 5-(1,2-oxazol-3-yl)-1H-pyrazol- 3-yl}pyrimidin-4-yl)amino]methyl}-2-hydroxypropanamide Originator Ironwood Pharmaceuticals Class Antifibrotics; Cardiovascular therapies Mechanism of Action Soluble guanylyl cyclase agonists Orphan Drug StatusNo New Molecular EntityYes Highest Development Phases Phase II Gastrointestinal disorders; Sickle cell anaemia Phase I Cardiovascular disorders; Fibrosis Most Recent Events 03 …

OXCARBAZEPINE

Oxcarbazepine KIN-493, GP-47680, Trileptal Molecular FormulaC15H12N2O2 Average mass252.268 Da 10-Oxo-10,11-dihydro-dibenzo[b,f]azepine-5-carboxylic acid amide 28721-07-5 [RN] 5H-Dibenz[b,f]azepine-5-carboxamide, 10,11-dihydro-10-oxo- UV Spectroscopy The UV absorption spectrum of carbamazepine in methanol shown in Fig. 1 was recorded using Shimadzu UV–vis Spectrometer 1601 PC. The compound exhibited maxima at 288 and 259 nm. Clarke reported the following: methanol—237 and 285 nm (A …

BICTEGRAVIR, NEW PATENT, WO 2018005328, CONCERT PHARMA

BICTEGRAVIR, NEW PATENT, WO 2018005328, CONCERT PHARMA WO2018005328) DEUTERATED BICTEGRAVIR CONCERT PHARMACEUTICALS, INC. TUNG, Roger, D.; (US) Concert CEO Roger Tung Novel deuterated forms of bictegravir is claimed. Gilead Sciences is developing the integrase inhibitor bictegravir as an oral tablet for the treatment of HIV-1 infection. This invention relates to deuterated forms of bictegravir, and …

TRILACICLIB, G1T28

Trilaciclib Molecular FormulaC24H30N8O Average mass446.548 Da G1T 28 CAS 1374743-00-6 2′-{[5-(4-Methyl-1-piperazinyl)-2-pyridinyl]amino}-7′,8′-dihydro-6’H-spiro[cyclohexane-1,9′-pyrazino[1′,2′:1,5]pyrrolo[2,3-d]pyrimidin]-6′-one G1T28, SHR 6390 Spiro[cyclohexane-1,9′(6’H)-pyrazino[1‘,2’:1,5]pyrrolo[2,3-d]pyrimidin]-6′-one, 7′,8′-dihydro-2‘-[[5-(4-methyl-1-piperazinyl)-2-pyridinyl]amino]- 7′,8′-Dihydro-2′-[[5-(4-methyl-1-piperazinyl)-2-pyridinyl]amino]spiro[cyclohexane-1,9′(6’H)-pyrazino[1′,2′:1,5]pyrrolo[2,3-d]pyrimidin]-6′-one 2′-[[5-(4-Methylpiperazin-1-yl)pyridin-2-yl]amino}-7′,8′-dihydro-6’H-spiro[cyclohexane-1,9′-pyrazino[1′,2′:1,5]pyrrolo[2,3-d]pyrimidin]-6′-one UNII:U6072DO9XG Reduction of Chemotherapy-Induced Myelosuppression Trilaciclib dihydrochloride 1977495-97-8 In phase II clinical development as a chemoprotectant at G1 Therapeutics for first- or second-line treatment in patients with metastatic triple negative breast cancer, in combination with gemcitabine and carboplatin …

WO-2018001353, APREMILAST, NEW PATENT, ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD

WO-2018001353, APREMILAST, NEW PATENT, ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD (WO2018001353) METHOD FOR PREPARING APREMILAST ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD DU, Xiaoqiu; (CN). ZHOU, Lianchao; (CN). LIU, Jiegen; (CN) https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2018001353&recNum=1&maxRec=&office=&prevFilter=&sortOption=&queryString=&tab=FullText EN)Method one: (S) -1- (3-ethoxy-4-methoxyphenyl) -2- (methylsulfonyl) ethylamine N-acetyl-L-leucine salt of formula II is reacted with 3-acetylaminophthalic anhydride of formula III in an aprotic solvent to …

(2R,3S,4R,5R)-1-(3-((5-(4-Fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-2,3,4,5,6-pentahydroxyhexan-1-one

CAS 1672658-93-3 C24 H25 F O6 S, 460.52 D-Glucopyranose, 1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]- CAS 1809403-04-0 C24 H25 F O6 S, 460.52 D-Glucose, 1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]- WO2017/93949 (2R,3S,4R,5R)-1-(3-((5-(4-Fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-2,3,4,5,6-pentahydroxyhexan-1-one 12 From the FT-IR spectra of 12 contain a signal at 1674 cm–1, this signal is strongly indicative of a carbonyl ketone being present in 12 In 13C NMR and HMBC correlations spectra, the chemical shift at 199.75 ppm was observed. Analysis of the …

ELAGOLIX

ELAGOLIX Molecular FormulaC32H30F5N3O5 Average mass631.590 Da NBI56418, ABT 620 UNII:5B2546MB5Z 4-({(1R)-2-[5-(2-Fluoro-3-methoxyphenyl)-3-[2-fluoro-6-(trifluoromethyl)benzyl]-4-methyl-2,6-dioxo-3,6-dihydro-1(2H)-pyrimidinyl]-1-phenylethyl}amino)butanoic acid 834153-87-6 FREE ACID SODIUM SALT 832720-36-2 Acide 4-({(1R)-2-[5-(2-fluoro-3-méthoxyphényl)-3-[2-fluoro-6-(trifluorométhyl)benzyl]-4-méthyl-2,6-dioxo-3,6-dihydro-1(2H)-pyrimidinyl]-1-phényléthyl}amino)butanoïque Butanoic acid, 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]- GNRH antagonist, Endometriosis Endometriosis PREREGISTERED Phase III Uterine leiomyoma WO2001055119A2, Inventors Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers, Applicant Neurocrine Biosciences, Inc. WO 2005007165 PDT PATENT Inventors Zhiqiang Guo, Yongsheng Chen, Dongpei Wu, Chen …

Empesertib , BAY 1161909

Empesertib , BAY 1161909, Mps1-IN-5, (-)-BAY-1161909 CAS 1443763-60-7 Chemical Formula: C29H26FN5O4S Molecular Weight: 559.6164 [a]D20 : -78.9° (in DMSO). WO 2014198647 UNII-02Y3Z2756M (αR)-4-Fluoro-N-[4-[2-[[2-methoxy-4-(methylsulfonyl)phenyl]amino][1,2,4]triazolo[1,5-a]pyridin-6-yl]phenyl]-α-methylbenzeneacetamide (R)-2-(4-fluorophenyl)-N-(4-(2-((2-methoxy-4-(methylsulfonyl)phenyl)amino)-[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl)propanamide (2R)-2-(4-Fluorophenyl)-N-(4-(2-((4-(methanesulfonyl)-2-methoxyphenyl)amino)(1,2,4)triazolo(1,5-a)pyridin-6-yl)phenyl)propanamide Benzeneacetamide, 4-fluoro-N-(4-(2-((2-methoxy-4-(methylsulfonyl)phenyl)amino)(1,2,4)triazolo(1,5-a)pyridin-6-yl)phenyl)-alpha-methyl-, (alphaR)- PHASE 1, BAYER, CANCER PRODUCT PATENT, WO2013087579, https://www.google.com/patents/WO2013087579A1 SYNTHESIS, WO 2014198647 Analytical UPLC-MS was performed as follows: Method A: System: UPLC Acquity (Waters) with PDA Detector und Waters ZQ mass spectrometer; Column: Acquity …