Drug Approvals International – Page 16 – All about Drugs Live by Dr Anthony Melvin Crasto

Evetifator

Evetifator CAS 2278265-85-1 MF C20H19ClF3N3O4 MW457.8 g/mol 2-(4-chlorophenoxy)-N-[3-[5-[3-(trifluoromethoxy)cyclobutyl]-1,3,4-oxadiazol-2-yl]-1-bicyclo[1.1.1]pentanyl]acetamide 2-(4-chlorophenoxy)-N-(3-{5-[(1s,3s)-3-(trifluoromethoxy)cyclobutyl]-1,3,4-oxadiazol-2-yl}bicyclo [1.1.1]pentan-1-yl)acetamideeukaryotic translation initiation factor 2B (eIF2B) activator, DNL-343, DNL 343, FYL3Y9D7SK Evetifator (also known as DNL343) is a potent, selective, and brain-penetrant small molecule activator of eukaryotic initiation factor 2B (eIF2B). As of 2026, it is primarily being investigated for the treatment of neurodegenerative diseases, such as …

Evategrel

Evategrel CAS 2760609-74-1 MF C21H26ClNO7S MW 472.0 g/mol (2Z)-2-[(4R)-1-[(1S)-1-(2-chlorophenyl)-2-methoxy-2-oxoethyl]-4-(propan-2-yloxycarbonyloxymethylsulfanyl)piperidin-3-ylidene]acetic acid (Z)-[(4R)-1-[(1S)-1-(2-chlorophenyl)-2-methoxy-2-oxoethyl]-4-{[({[(propan-2-yl)oxy]carbonyl}oxy)methyl]sulfanyl}piperidin-3-ylidene]acetic acidplatelet aggregation inhibitor, CG-0255, CG 0255, 9FKJ76ZX22 Evategrel (CG-0255) is a promising new antiplatelet drug, a thioether prodrug, designed to improve upon clopidogrel (Plavix) by offering faster action, consistent potency, and overcoming resistance, with both oral and intravenous (IV) formulations available for emergency use. It works by rapidly …

Enrupatinib

Enrupatinib CAS 2222689-47-4 MF C27H26N6O3 MW 482.5 g/mol 6-[3-methoxy-4-[(6-methyl-3-pyridinyl)methoxy]anilino]-3-morpholin-4-ylquinoxaline-5-carbonitrile colony-stimulating factor 1 receptor (CSF1R) inhibitor, antineoplastic, EI 1071, EI-1071, 9L35RVQ9J6 ENRUPATINIB is a small molecule drug with a maximum clinical trial phase of II and has 1 investigational indication. EI-1071 is a selective Colony Stimulating Factor-1 Receptor kinase inhibitor. SYN PAT https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=FF56F70B79B734C8ED557D6943D76B2E.wapp1nC?docId=WO2025067450&_cid=P12-MKLYYQ-95450-1 PAT https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2018071348&_cid=P12-MKLZ1L-03304-1 PAT AS …

Emestedastat

Emestedastat CAS 1346013-80-6 MF C19H19N5O2S MW381.5 g/mol [(1R,3r,5S)-3-hydroxy-3-(pyrimidin-2-yl)-8-azabicyclo[3.2.1]octan-8-yl][5-(1H-pyrazol-4-yl)thiophen-3-yl]methanone11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor, UE-2343, UE 2343, 106ELK29GH Emestedastat (proposed brand name Xanamem; developmental code name UE-2343) is a steroidogenesis inhibitor which is under development for the treatment of major depressive disorder, Alzheimer’s disease, and fragile X syndrome.[1][2] It specifically acts as a centrally penetrant inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) and thereby inhibits the synthesis of the glucocorticoid steroid hormone cortisol.[1][3][4][2] As of August 2024, …

Direclidine

Direclidine CAS 1803346-98-6 MF C19H30N4O2 MW346.5 g/mol ethyl 2-[4-(2-methylpyrazol-3-yl)piperidin-1-yl]-6-azaspiro[3.4]octane-6-carboxylate 6-Azaspiro[3.4]octane-6-carboxylic acid, 2-[4-(1-methyl-1H-pyrazol-5-yl)-1-piperidinyl]-, ethyl ester, cis- ethyl (2r,4s)-2-[4-(1-methyl-1H-pyrazol-5-yl)piperidin-1-yl]-6-azaspiro[3.4]octane-6-carboxylatemuscarinic M4 receptor positive allosteric modulator, TXB4V44U24, NBI-1117568, NBI 1117568 Direclidine (INNTooltip International Nonproprietary Name;[2] developmental code names NBI-1117568, HTL-0016878)[1] is an investigational antipsychotic drug for schizophrenia[3] that was out-licensed from Nxera Pharma to Neurocrine Biosciences, a United States-based pharmaceutical company.[4][1][5] It is an oral small molecule.[6][7] Direclidine (NBI-1117568) is an investigational, oral drug in Phase 3 trials …

Dezecapavir

Dezecapavir CAS 2570323-59-8 MF C37H29ClF9N9O5S MW918.19 1H-Cyclopropa[3,4]cyclopenta[1,2-c]pyrazole-1-acetamide, N-[(1S)-1-[(3S)-3-[4-chloro-1-methyl-3-[(methylsulfonyl)amino]-1H-indazol-7-yl]-3,4-dihydro-4-oxo-7-(3,3,3-trifluoropropoxy)pyrido[2,3-d]pyrimidin-2-yl]-2-(3,5-difluorophenyl)ethyl]-3-(difluoromethyl)-5,5-difluoro-3b,4,4a,5-tetrahydro-, (3bS,4aR)- N-[(1S)-1-[(3P)-3-[4-chloro-3-(methanesulfonamido)-1-methyl-1H-indazol-7-yl]-4-oxo-7-(3,3,3-trifluoropropoxy)-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl]-2-(3,5-difluorophenyl)ethyl]-2-[(3bS,4aR)-3-(difluoromethyl)-5,5-difluoro-3b,4,4a,5-tetrahydro-1Hcyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl]acetamideinhibitor of viral replication, antiviral, SEK9LN2LSM, VH 4011499, VH4011499, VH-4011499, VH 499, GSK2838232, GSK 2838232 Dezecapavir is a potent experimental antiviral compound, specifically a novel HIV-1 capsid inhibitor, developed to block HIV replication by targeting the virus’s capsid protein, showing high effectiveness in lab settings (low nM …

Deulorlatinib

Deulorlatinib CAS 2131126-33-3 MFC21H162H3FN6O2, MW 409.4 g/mol (10R)-7-amino-12-fluoro-2-(2H3)methyl-10,16-dimethyl15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitriletyrosine kinase inhibitor, antineoplastic, 7PW3UT8C9B, TGRX 326, TGRX-326 Deulorlatinib is an orally bioavailable inhibitor of the receptor tyrosine kinases anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1), with potential antineoplastic activity. Upon oral administration, deulorlatinib targets, binds to and inhibits the activity of ALK and ROS1, which leads to the …

Cenacitinib

Cenacitinib CAS 2641636-52-2 MF C19H19F2N7O3 MW431.4 Urea, N-[(1R,2S)-2-fluorocyclopropyl]-N′-[5-[(7-fluoro-2,3-dihydro-1,4-benzodioxin-5-yl)amino]-7-(methylamino)pyrazolo[1,5-a]pyrimidin-3-yl]- N-{5-[(7-fluoro-2,3-dihydro-1,4-benzodioxin-5-yl)amino]-7-(methylamino)pyrazolo[1,5-a]pyrimidin-3-yl}-N′-[(1R,2S)-2-fluorocyclopropyl]urea Janus kinase inhibitor, anti-inflammatory, VTX958, VTX 958, SB88R8KGL3 VTX958 for the Treatment of Moderately to Severely Active Crohn’s Disease CTID: NCT05688852 Phase: Phase 2 Status: Terminated Date: 2025-07-03 SYN [US20210139486] https://patentscope.wipo.int/search/en/detail.jsf?docId=US323750705&_cid=P22-MKEUDK-45432-1 Example 4: Synthesis of 1-(5-((7-fluoro-2,3-dihydrobenzo[b][1,4]dioxin-5-yl)amino)-7-(methylamino)pyrazolo[1,5-a]pyrimidin-3-yl)-3-((1R,2S)-2-fluorocyclopropyl)urea (5) Step 1: To a solution of 1E (100 g, 288 mmol) and 2E …

Casdatifan

Casdatifan CAS 2709069-30-5 MF C21H17F4NO3S, 439.4 g/mol (5R,6S,8R)-3,5,6-trifluoro-8-[(1S,2R)-2-fluoro-1-hydroxy-7-(methanesulfonyl)-2,3-dihydro-1H-inden-4-yl]-5,6,7,8-tetrahydronaphthalene-1-carbonitrile (5R,6S,8R)-3,5,6-trifluoro-8-[(1S,2R)-2-fluoro-1-hydroxy-7-methylsulfonyl-2,3-dihydro-1H-inden-4-yl]-5,6,7,8-tetrahydronaphthalene-1-carbonitrile (5R,6S,8R)-3,5,6-trifluoro-8-[(1S,2R)-2-fluoro-1-hydroxy-7-methylsulfonyl-2,3-dihydro-1H-inden-4-yl]-5,6,7,8-tetrahydronaphthalene-1-carbonitrile (5R,6S,8R)-3,5,6-trifluoro-8-[(1S,2R)-2-fluoro-1-hydroxy-7-methanesulfonyl-2, 3-dihydro-1H-inden-4-yl]-5,6,7,8-tetrahydronaphthalene-1-carbonitrilehypoxia-inducible factor (HIF) inhibitor, antineoplastic, AB 521, DP73UWL6LE Casdatifan is an orally bioavailable allosteric inhibitor of hypoxia inducible factor (HIF)-2alpha, with potential antineoplastic activity. Upon oral administration, casdatifan targets and allosterically binds to a hydrophobic pocket on HIF-2alpha leading to a confirmational change that prevents …

Cambritaxestat

Cambritaxestat CAS 1979939-16-6 MFC25H22ClF3N4O2 MW502.9 g/mol N-[(1S)-1-(4-chlorophenyl)ethyl]-3-[3-[[4-(trifluoromethoxy)phenyl]methyl]imidazo[4,5-b]pyridin-2-yl]propanamide N-[(1S)-1-(4-chlorophenyl)ethyl]-3-(3-{[4-(trifluoromethoxy)phenyl]methyl}-3H-imidazo[4,5-b]pyridin-2-yl)propanamideautotaxin inhibitor, antineoplastic, Orphan Drug, IOA 289, IOA-289, IOA289, LYY3P2KA27, CRT 0273750 Cambritaxestat is an autotaxin inhibitor. Cambritaxestat is an orally bioavailable small molecule inhibitor of autotaxin (ATX; ectonucleotide pyrophosphatase/phosphodiesterase family member 2; ENPP2), with potential antifibrotic and antineoplastic activities. Upon oral administration, cambritaxestat targets and binds to both …