SG11201807543YA - Hepatitis b antiviral agents - Google Patents

Hepatitis b antiviral agents

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Publication number
SG11201807543YA
SG11201807543YA SG11201807543YA SG11201807543YA SG11201807543YA SG 11201807543Y A SG11201807543Y A SG 11201807543YA SG 11201807543Y A SG11201807543Y A SG 11201807543YA SG 11201807543Y A SG11201807543Y A SG 11201807543YA SG 11201807543Y A SG11201807543Y A SG 11201807543YA
Authority
SG
Singapore
Prior art keywords
international
road
hepatitis
pct
hbv
Prior art date
Application number
SG11201807543YA
Inventor
Yao-Ling Qiu
Xuri Gao
Wei Li
Hui Cao
Meizhong Jin
Jorden Kass
Xiaowen Peng
Yat OR
Original Assignee
Enanta Pharm Inc
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 Enanta Pharm Inc filed Critical Enanta Pharm Inc
Publication of SG11201807543YA publication Critical patent/SG11201807543YA/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
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    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
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    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
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    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/223—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of alpha-aminoacids
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    • A61K31/336—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
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    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
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    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
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    • A61K31/365—Lactones
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    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/39—Heterocyclic compounds having sulfur as a ring hetero atom having oxygen in the same ring
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
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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
    • A—HUMAN NECESSITIES
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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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    • A61K31/41—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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    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
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    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
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Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 1111111101111011101010111110101111101110111101110111110111011111111101111011111 International Bureau 0... .... ..Yjd (10) International Publication Number ...... ../ (43) International Publication Date WO 2017/155844 Al 14 September 2017 (14.09.2017) WIP0 I PCT (51) International Patent Classification: (74) Agents: HARLAN, Edgar, W. et al.; Elmore Patent Law A61K 31/42 (2006.01) C07D 261/20 (2006.01) Group, 484 Groton Road, Westford, MA 01886 (US). A61K 31/416 (2006.01) (81) Designated States (unless otherwise indicated, for every (21) International Application Number: kind of national protection available): AE, AG, AL, AM, PCT/US2017/020853 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, (22) International Filing Date: DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, 6 March 2017 (06.03.2017) HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, (25) Filing Language: English KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, (26) Publication Language: English NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (30) Priority Data: RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, 62/304,671 7 March 2016 (07.03.2016) US TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, 62/337,675 17 May 2016 (17.05.2016) US ZA, ZM, ZW. (71) Applicant: ENANTA PHARMACEUTICALS, INC. (84) Designated States (unless otherwise indicated, for every [US/US]; 500 Arsenal Street, Watertown, MA 02472 (US). kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, — (72) Inventors: QIU, Yao-Ling; 29 Linda Road, Andover, MA TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, 01810 (US). GAO, Xuri; 179 Allerton Road, Unit 2, New- TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, ton, MA 02461 (US). LI, Wei; 22 April Lane, Lexington, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, MA 02421 (US). CAO, Hui; 53 Hill Road, Belmont, MA LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, — _ 02478 (US). JIN, Meizhong; 64-105 Hastings St., Welles- SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, ley, MA 02481 (US). KASS, Jorden; 29 Wilson Ave, Apt. GW, KM, ML, MR, NE, SN, TD, TG). #2, Belmont, MA 02478 (US). PENG, Xiaowen; 85 Horse Pond Road, Sudbury, MA 01776 (US). OR, Yat, Sun; 169 Published: = Fayette Street, Watertown, MA 02472 (US). — with international search report (Art. 21(3)) = = = = = = = = = = = Il 7r 7r cc kin kin 1-1 (54) Title: HEPATITIS B ANTIVIRAL AGENTS IN (57) : The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs 1-1 C thereof: X-A -Y -L-R (I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV N life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical corn- ea ) positions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention 7 1 ,1 9 also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
SG11201807543YA 2016-03-07 2017-03-06 Hepatitis b antiviral agents SG11201807543YA (en)

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