SG11201900699QA - Drug conjugates with self-stabilizing linkers having improved physiochemical properties - Google Patents

Drug conjugates with self-stabilizing linkers having improved physiochemical properties

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Publication number
SG11201900699QA
SG11201900699QA SG11201900699QA SG11201900699QA SG11201900699QA SG 11201900699Q A SG11201900699Q A SG 11201900699QA SG 11201900699Q A SG11201900699Q A SG 11201900699QA SG 11201900699Q A SG11201900699Q A SG 11201900699QA SG 11201900699Q A SG11201900699Q A SG 11201900699QA
Authority
SG
Singapore
Prior art keywords
international
conjugate
self
pct
applicant
Prior art date
Application number
SG11201900699QA
Inventor
Philip Moquist
Original Assignee
Seattle Genetics 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 Seattle Genetics Inc filed Critical Seattle Genetics Inc
Publication of SG11201900699QA publication Critical patent/SG11201900699QA/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Abstract

Time (days) (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 15 February 2018 (15.02.2018) WIP0 I PCT ~~~~~~~~~~~~~ 011101VIIIVIIIVIII olo olll om iflo Hs (10) International Publication Number WO 2018/031690 Al (51) International Patent Classification: A61K 39/00 (2006.01) C07D 207/36 (2006.01) C07K 5/062 (2006.01) (21) International Application Number: PCT/US2017/046157 (22) International Filing Date: 09 August 2017 (09.08.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/372,455 09 August 2016 (09.08.2016) US (71) Applicant: SEATTLE GENETICS, INC. [US/US]; 21823 30th Drive SE, Bothell, Washington 98021 (US). (72) Inventor: MOQUIST, Philip; 21823 30th Drive SE, Both- ell, Washington 98021 (US). (74) Agent: CASTELLINO, Angelo et al.; SEATTLE GENETICS, INC., 21823 30TH Drive SE, Bothell, Wash- ington 98021 (US). (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, 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. (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 4.17(ii)) 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)) (54) Title: DRUG CONJUGATES WITH SELF-STABILIZING LINKERS HAVING IMPROVED PHYSIOCHEMICAL PROP- = ERTIES 125 C 100 - c r7 E 75 50 O 25 -41-- Conjugate A --ra- Conjugate B Conjugate C -4- Conjugate M FIG. 2 (57) : Compounds and compositions are disclosed in which a Drug Unit is linked to a targeting Ligand Unit through a self- stabilizing Linker Unit from which a drug compound or active drug moiety is released at the targeted site of action. Methods for treating diseases characterized by the targeted abnormal cells, such as cancer or an autoimmune disease using the compounds and compositions of the invention are also disclosed. W O 20 18/03 1690 Al
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