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1. (WO2019004936) PROCESS FOR PREPARING LIFITEGRAST AND INTERMEDIATES THEREOF
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Pub. No.: WO/2019/004936 International Application No.: PCT/SG2018/050310
Publication Date: 03.01.2019 International Filing Date: 26.06.2018
IPC:
C07D 405/06 (2006.01) ,A61K 31/4725 (2006.01) ,A61K 9/00 (2006.01) ,A61P 27/02 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
47
Quinolines; Isoquinolines
472
Non-condensed isoquinolines, e.g. papaverine
4725
containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27
Drugs for disorders of the senses
02
Ophthalmic agents
Applicants:
SCINOPHARM TAIWAN, LTD.; No. 1, Nan-Ke 8th Road, Southern Taiwan Science Park, Shan-Hua, Tainan, 74144, TW
SCINOPHARM SINGAPORE PTE, LTD. [SG/SG]; 50, Raffles Place #06-00, Singapore Land Tower, Singapore 048623, SG (SG)
Inventors:
WU, Ming-Chih; TW
HSIAO, Tsung-Yu; TW
Agent:
MATTEUCCI, Gianfranco; SG
Priority Data:
62/527,86830.06.2017US
Title (EN) PROCESS FOR PREPARING LIFITEGRAST AND INTERMEDIATES THEREOF
(FR) PROCÉDÉ POUR LA PRÉPARATION DE LIFITEGRAST ET D'INTERMÉDIAIRES DE CELUI-CI
Abstract:
(EN) The present disclosure provides efficient, economical, and improved processes for synthesizing lifitegrast and intermediates thereof. The currently discloses processes provide a direct synthetic route, avoiding protection or deprotection steps. The currently disclosed process also provides processes for synthesizing lifitegrast using a reduced number of synthetic steps.
(FR) La présente invention concerne des procédés efficaces, économiques et améliorés pour la synthèse de lifitegrast et de ses intermédiaires. Les procédés selon la présente invention fournissent une route synthétique directe, évitant les étapes de protection ou de déprotection. Le procédé selon l'invention concerne également des méthodes de synthèse de lifitegrast à l'aide d'un nombre réduit d'étapes synthétiques.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)