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1. (WO2018201076) MACROLIDES WITH MODIFIED DESOSAMINE SUGARS AND USES THEREOF
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/201076 International Application No.: PCT/US2018/030002
Publication Date: 01.11.2018 International Filing Date: 27.04.2018
IPC:
C07H 17/08 (2006.01) ,C07H 15/18 (2006.01) ,A61K 31/7048 (2006.01) ,A61P 31/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
17
Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
04
Heterocyclic radicals containing only oxygen as ring hetero atoms
08
Hetero rings containing eight or more ring members, e.g. erythromycins
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15
Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
18
Acyclic radicals, substituted by carbocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
7042
Compounds having saccharide radicals and heterocyclic rings
7048
having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04
Antibacterial agents
Applicants:
MACROLIDE PHARMACEUTICALS INC. [US/US]; 480 Arsenal St., Suite 130 Watertown, MA 02472, US
PRESIDENT AND FELLOWS OF HARVARD COLLEGE [US/US]; 17 Quincy Street Cambridge, MA 02138, US
Inventors:
MYERS, Andrew, G.; US
ZHANG, Ziyang; US
FUKUZAKI, Takehiro; US
ILANDARI DEWAGE, Udara Anulai, Premachandra; US
ALLU, Senkara, Rao; US
CLARK, Roger, B.; US
LAWRENCE, Jonathan, F.; US
AUSTIN, Wesley, Francis; US
LI, Xiben; US
WANG, Wenying; US
LAHIRI, Sushmita, D.; US
ICHIKAWA, Yoshitaka; US
Agent:
BERVEN, Heidi, M.; US
Priority Data:
62/491,89028.04.2017US
62/522,58120.06.2017US
Title (EN) MACROLIDES WITH MODIFIED DESOSAMINE SUGARS AND USES THEREOF
(FR) MACROLIDES À SUCRES MODIFIÉS DE TYPE DÉSOSAMINE ET UTILISATIONS DE CEUX-CI
Abstract:
(EN) Provided are macrolide compounds for the treatment of infectious diseases. The macrolides disclosed herein include 14-membered ketolides and 14-15-membered azaketolides, and may comprise modified sugars which are desosamine analogues. The disclosed macrolides may have a bicyclic structure. Also provided are pharmaceutical compositions and methods of treating infectious diseases, and in particular, disease which results from Gram negative bacteria using the disclosed macrolides. This disclosure additionally provides methods of preparing the macrolides by a strategy that enables late- stage modification of the 6'-position of the sugar moiety, thereby allowing facile access to previously difficult-to-make macrolide compounds.
(FR) L'invention concerne des composés macrolides pour le traitement de maladies infectieuses. Les macrolides de l'invention comprennent des cétolides à 14 chaînons et des azacétolides à 14-15 chaînons, et peuvent comprendre des sucres modifiés qui sont des analogues de désosamine. Les macrolides selon l'invention peuvent avoir une structure bicyclique. L'invention concerne également des compositions pharmaceutiques et des procédés de traitement de maladies infectieuses, et en particulier, une maladie qui résulte de bactéries à Gram négatif à l'aide des macrolides décrits. La présente invention concerne en outre des procédés de préparation des macrolides par une stratégie qui permet une modification à un stade tardif de la position 6' de la fraction sucre, permettant ainsi un accès facile à des composés macrolides auparavant difficiles à produire.
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)