SG11201808912QA - Targeted nucleic acid conjugate compositions - Google Patents
Targeted nucleic acid conjugate compositionsInfo
- Publication number
- SG11201808912QA SG11201808912QA SG11201808912QA SG11201808912QA SG11201808912QA SG 11201808912Q A SG11201808912Q A SG 11201808912QA SG 11201808912Q A SG11201808912Q A SG 11201808912QA SG 11201808912Q A SG11201808912Q A SG 11201808912QA SG 11201808912Q A SG11201808912Q A SG 11201808912QA
- Authority
- SG
- Singapore
- Prior art keywords
- international
- british columbia
- burnaby
- rule
- glenlyon
- Prior art date
Links
- 150000007523 nucleic acids Chemical class 0.000 title abstract 4
- 102000039446 nucleic acids Human genes 0.000 title abstract 4
- 108020004707 nucleic acids Proteins 0.000 title abstract 4
- 239000000203 mixture Substances 0.000 title abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 208000005331 Hepatitis D Diseases 0.000 abstract 1
- 229940126587 biotherapeutics Drugs 0.000 abstract 1
- 208000006454 hepatitis Diseases 0.000 abstract 1
- 231100000283 hepatitis Toxicity 0.000 abstract 1
- 208000002672 hepatitis B Diseases 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 125000005647 linker group Chemical group 0.000 abstract 1
- 210000004185 liver Anatomy 0.000 abstract 1
- 208000019423 liver disease Diseases 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 238000010189 synthetic method Methods 0.000 abstract 1
- 230000008685 targeting Effects 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 239000002023 wood Substances 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
-
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- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7088—Compounds having three or more nucleosides or nucleotides
- A61K31/713—Double-stranded nucleic acids or oligonucleotides
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- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
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- A61K47/554—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
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- C07C237/08—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
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- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
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- C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
- C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
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- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/40—Oxygen atoms
- C07D211/42—Oxygen atoms attached in position 3 or 5
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- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
WO 17 / 177 3 26 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2017/177326 Al 19 October 2017 (19.10.2017) WIPO I PCT (51) International Patent Classification: C12N 15/113 (2010.01) CO7D 209/52 (2006.01) A61K 47/54 (2017.01) C07F 9/40 (2006.01) CO7C 217/52 (2006.01) CO7H 15/26 (2006.01) CO7C 235/06 (2006.01) CO7H 21/00 (2006.01) CO7C 237/08 (2006.01) CO7H 21/02 (2006.01) CO7C 237/20 (2006.01) C07J 63/00 (2006.01) CO7D 207/08 (2006.01) C07J 9/00 (2006.01) CO7D 207/12 (2006.01) Cl 2N 15/87 (2006.01) CO7D 209/12 (2006.01) (21) International Application Number: PCT/CA2017/050447 (22) International Filing Date: 11 April 2017 (11.04.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/321,034 11 April 2016 (11.04.2016) US 62/417,156 3 November 2016 (03.11.2016) US 62/438,310 22 December 2016 (22.12.2016) US (71) Applicant: PROTIVA BIOTHERAPEUTICS, INC. [CA/CA]; 100-8900 Glenlyon Parkway, Burnaby, British Columbia V5J 5J8 (CA). (72) Inventors; and (71) Applicants : HEYES, James [CA/CA]; 100-8900 Glenly- on Parkway, Burnaby, British Columbia V5J 5J8 (CA). HOLLAND, Richard J. [CA/CA]; 100-8900 Glenlyon Parkway, Burnaby, British Columbia V5J 5J8 (CA). MARTIN, Alan D. [CA/CA]; 100-8900 Glenlyon Park- way, Burnaby, British Columbia V5J 5J8 (CA). WOOD, Mark [CA/CA]; 100-8900 Glenlyon Parkway, Burnaby, British Columbia V5J 5J8 (CA). (74) Agent: SMART & BIGGAR; PO Box 11115, #2300- 1055 West Georgia Street, Vancouver, British Columbia V6E 3P3 (CA). (81) Designated States (unless otherwise indicated, for every kind of national protection available): 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, 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. (84) Designated States (unless otherwise indicated, for every 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). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.1700) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: — with international search report (Art. 21(3)) [Continued on next page] (54) Title: TARGETED NUCLEIC ACID CONJUGATE COMPOSITIONS 1 11111 11111111 0 111 0 1 11111 11111 0 10 1111 I 1 1 1 0 10 1110 11111 0 111 0 111 1111 1111111 1111 0 11 1111 HN '10° 0 O H OAc NH AGO O NH X d Figure 1 (57) : The invention provides conjugates that comprise a targeting moiety, a nucleic acid, and optional linking groups as well as synthetic intermediates and synthetic methods useful for preparing the conjugates. The conjugates are useful to target thera- peutic nucleic acids to the liver and to treat liver diseases including hepatitis (e.g. hepatitis B and hepatitis D). WO 2017/177326 Al MIDEDIMOM0101011101010MOIDEHIIIMMEMOVOIMIE before the expiration of the time limit for amending the — with sequence listing part of description (Rule 5.2(a)) claims and to be republished in the event of receipt of amendments (Rule 48.2(h))
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