Medicinal Chemistry International

DRUG PATENTS INTERNATIONAL

MILVEXIAN

https://newdrugapprovals.org/2020/10/24/milvexian/

DRUG PATENTS INTERNATIONAL

Cetuximab Sarotalocan Sodium (Genetical Recombination)

Cetuximab Sarotalocan Sodium is an antibody-drug-conjugate (molecular weight: 156,000-158,000) consisting of tetrasodium salt of Sarotalocan (6-({[3-({(OC-6-13)-bis({3-[bis(3-sulfopropyl)(3-sulfonatopropyl)azaniumyl]propyl}dimethylsilanolato-κO,κO')[(phtalocyaninato(2-)κN29,κN30,κN31,κN32)-1-yl]silicon}oxy)propoxy]carbonyl}amino)hexanoyl (C70H96N11O24S6Si3; molecular weight: 1,752.22)) attached to an average of 2-3 Lys residues of Cetuximab.

[2166339-33-7 , Cetuximab sarotalocan]

https://newdrugapprovals.org/2020/10/12/cetuximab-sarotalocan-sodium/

DRUG PATENTS INTERNATIONAL

Bulevirtide acetate

SEE

https://newdrugapprovals.org/2020/09/26/bulevirtide-acetate/

////////////2020 APPROVALS, ブレビルチド酢酸塩, BULEVIRTIDE ACETATE, EU 2020, MYR GMBH, ORPHAN DESIGNATION, PEPTIDE

DRUG PATENTS INTERNATIONAL

MDSFSANQEI RYSEVTPYHV TSVWTKGVTP PANFTQGEDV FHAPYVANQG WYDITKTFNG

KDDLLCGAAT AGNMLHWWFD QNKDQIKRYL EEHPEKQKIN FNGEQMFDVK EAIDTKNHQL
DSKLFEYFKE KAFPYLSTKH LGVFPDHVID MFINGYRLSL TNHGPTPVKE GSKDPRGGIF
DAVFTRGDQS KLLTSRHDFK EKNLKEISDL IKKELTEGKA LGLSHTYANV RINHVINLWG
ADFDSNGNLK AIYVTDSDSN ASIGMKKYFV GVNSAGKVAI SAKEIKEDNI GAQVLGLFTL
STGQDSWNQT N

Imlifidase

イムリフィダーゼ;

READ AT

https://newdrugapprovals.org/2020/09/22/imlifidase/

DRUG PATENTS INTERNATIONAL

Clascoterone

https://newdrugapprovals.org/2020/09/18/clascoterone/

DRUG PATENTS INTERNATIONAL

Copper dotatate Cu-64.png

2D chemical structure of 1426155-87-4

Figure imgf000004_0001

Copper Cu 64 dotatate

銅(Cu64)ドータテート;

READ AT

http://medcheminternational.blogspot.com/

DRUG PATENTS INTERNATIONAL

Abstract

An environmentally benign decarboxylative cyclization in water has been developed to synthesize 4-quinolones from readily available isatoic anhydrides and 1,3-dicarbonyl compounds. Isatins are also compatible for the reaction to generate 4-quinolones in the presence of TBHP in DMSO. This protocol provides excellent yields under mild conditions for a broad scope of 4-quinolones, and has good functional group tolerance. Only un-harmful carbon dioxide and water are released in this procedure. Moreover, the newly synthesized products have also been selected for anti-malarial examination against the chloroquine drug-sensitive Plasmodium falciparum 3D7 strain. 3u is found to display excellent anti-malarial activity with an IC₅₀ value of 33 nM.

Eco-friendly decarboxylative cyclization in water: practical access to the anti-malarial 4-quinolones

Yue Ma,^a Yongping Zhu,^a Dong Zhang,^a Yuqing Meng,^a Tian Tang,^a Kun Wang,^a Ji Ma,^a Jigang Wang^a and Peng Sun*^a

Author affiliations

*Corresponding authors

^aArtermisinin Research Center and Institute of Chinese Meteria Medica, Academy of Chinese Medical Sciences, Beijing, P. R. China
E-mail:psun@icmm.ac.cn

https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C8GC03570A?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract
ethyl 2-(4-(benzyloxy)phenyl)-4-oxo-1,4-dihydroquinoline-3-carboxylate (3u) White solid, m.p. 288-289 oC;
1H NMR (600 MHz, DMSO-d6) δ 12.14 (s, 1H), 8.13 (d, J = 8.0 Hz, 1H), 7.72 (ddd, J = 8.4, 7.1, 1.5 Hz, 1H), 7.64 (d, J = 8.3 Hz, 1H), 7.52 (td, J = 8.5, 1.7 Hz, 1H), 7.43 – 7.35 (m, 4H), 7.29 – 7.21 (m, 4H), 7.10 (td, J = 7.5, 0.5 Hz, 1H), 5.17 (s, 2H), 3.91 (q, J = 7.1 Hz, 2H), 2.00 (s, 1H), 0.83 (t, J = 7.1 Hz, 3H) ppm;
13C NMR (150 MHz, DMSO-d6) δ 174.1, 166.2, 156.2, 148.0, 139.8, 137.2, 132.8, 132.0, 130.5, 129.4, 128.7, 128.2, 127.6, 125.5, 125.2, 124.3, 123.6, 120.9, 118.9, 116.4, 115.8, 113.5, 70.2, 60.2, 14.0 ppm;
HRMS (ESI) calcd for [C25H21NO4+H]+ 400.1471, found 400.1463.