SG11201809989XA - Seco macrolide compounds - Google Patents

Seco macrolide compounds

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Publication number
SG11201809989XA
SG11201809989XA SG11201809989XA SG11201809989XA SG11201809989XA SG 11201809989X A SG11201809989X A SG 11201809989XA SG 11201809989X A SG11201809989X A SG 11201809989XA SG 11201809989X A SG11201809989X A SG 11201809989XA SG 11201809989X A SG11201809989X A SG 11201809989XA
Authority
SG
Singapore
Prior art keywords
zagreb
prilaz
baruna
fidelta
filipovica
Prior art date
Application number
SG11201809989XA
Inventor
Andrea Fajdetic
Skugor Maja Matanovic
Ivaylo Elenkov
Goran Kragol
Mirjana Bukvic
Istuk Zorica Marusic
Sanja Kostrun
Dinko Ziher
Renata Rupcic
Kristina Butkovic
Marko Duksi
Landek Ivana Ozimec
Dijana Pesic
Antun Hutinec
Milan Mesic
Gordon Saxty
Visnja Poljak
Original Assignee
Fidelta D O O
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Fidelta D O O filed Critical Fidelta D O O
Publication of SG11201809989XA publication Critical patent/SG11201809989XA/en

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    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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  • Pyrane Compounds (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization 1 MI 11111 0 11101 HOE 010 1111 1 0 I MINH HE 1101 OE 1111011110111111 International Bureau (10) International Publication Number (43) International Publication Date .....0\"\"\"1 WO 2017/194452 Al 16 November 2017 (16.11.2017) WIPO I PCT (51) International Patent Classification: Zagreb (HR). POLJAK, Visnja; Nuevolution Ronneggade C07H 17/02 (2006.01) A61K 31/7048 (2006.01) 8, 2100 Copenhagen (DK). C07H 17/08 (2006.01) A61K 31/7052 (2006.01) C07D 273/01 (2006.01) A61P 37/00 (2006.01) (74) Agent: BAR, Gregory, Louis, Joseph; Galapagos NV, Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). (21) International Application Number: PCT/EP2017/060889 (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (22) International Filing Date: 08 May 2017 (08.05.2017) 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, (25) Filing Language: English HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, (26) Publication Language: English KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, (30) Priority Data: 1608236.4 11 May 2016 (11.05.2016) GB 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, (71) Applicant: FIDELTA D.O.O. [HR/HR]; Prilaz Baruna TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. Filipovica 29, 10000 Zagreb (HR). (84) Designated States (unless otherwise indicated, for every (72) Inventors: FAJDETIC, Andrea; Istarska 62, 10000 Za- greb (HR). MATANOVIC SKUGOR, Maja; Havidice- va 10, 10000 Zagreb (HR). ELENKOV, Ivaylo; Fidelta d.o.o. Prilaz baruna, Filipovica 29, 10000 Zagreb (HR). KRAGOL, Goran; Fidelta d.o.o. Prilaz baruna, Filipovi- ca 29, 10000 Zagreb (HR). BUKVIC, Mirjana; Fidelta d.o.o. Prilaz baruna, Filipovica 29, 10000 Zagreb (HR). MARUSIC ISTUK, Zorica; Fidelta d.o.o. Prilaz baruna, Filipovica 29, 10000 Zagreb (HR). KOSTRUN, Sanja; kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (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), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). = Fidelta d.o.o. Prilaz baruna, Filipovica 29, 10000 Zagreb Declarations under Rule 4.17: (HR). ZIHER, Dinko; Fidelta d.o.o. Prilaz baruna, Fil- — as to applicant's entitlement to apply for and be granted a ipovica 29, 10000 Zagreb (HR). RUPCIC, Renata; Fidelta patent (Rule 4.17(ii)) d.o.o. Prilaz baruna, Filipovica 29, 10000 Zagreb (HR). — of inventorship (Rule 4.17(iv)) BUTKOVIC, Kristina; Fidelta d.o.o. Prilaz baruna, Fil- ipovica 29, 10000 Zagreb (HR). DUKSI, Marko; Fildelta Published: d.o.o. Prilaz baruna, Filipovica 29, 10000 Zagreb (HR). — with international search report (Art. 21(3)) OZIMEC LANDEK, Ivana; Fidelta d.o.o. Prilaz baruna, Filipovica 29, 10000 Zagreb (HR). PESIC, Dijana; Fidelta d.o.o. Prilaz baruna, Filipovica 29, 10000 Zagreb (HR). HUTINEC, Antun; Fidelta d.o.o. Prilaz baruna, Filipovi- ca 29, 10000 Zagreb (HR). MESIC, Milan; Fidelta d.o.o. Prilaz baruna, Filipovica 29, 10000 Zagreb (HR). SAXTY, Gordon; Fidelta d.o.o. Prilaz baruna, Filipovica 29, 10000 Title: SECO MACROLIDE COMPOUNDS (54) 1-1 (57) : The present invention relates to seco (opened ring) macrolide compounds of for- .4 R N Z 1 Z2 mula (I), to the process for preparation thereof, to the use of said seco macrolide compounds as based based macrocycles ei kn macrolide macrocycles, to macrolide p X' /9a 8 obtained from said seco macrolide compounds, to the process for preparation of macrolide based 1 71' macrocycles, to the pharmaceutical compositions comprising macrolide based macrocycles, and to 71' A 2 the use of macrolide based macrocycles as therapeutic agents. 01 5 Il R 1 Xi' R2a Ir . \"' © Il R 2b (I) ei B i BZ O
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