SG11201809714TA - Piperidines as menin inhibitors - Google Patents

Piperidines as menin inhibitors

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Publication number
SG11201809714TA
SG11201809714TA SG11201809714TA SG11201809714TA SG11201809714TA SG 11201809714T A SG11201809714T A SG 11201809714TA SG 11201809714T A SG11201809714T A SG 11201809714TA SG 11201809714T A SG11201809714T A SG 11201809714TA SG 11201809714T A SG11201809714T A SG 11201809714TA
Authority
SG
Singapore
Prior art keywords
international
ann arbor
co7d
apartment
formula
Prior art date
Application number
SG11201809714TA
Inventor
Shaomeng Wang
Angelo Aguilar
Ke Zhang
Shilin Xu
Tianfeng Xu
Denzil Bernard
Liyue Huang
Original Assignee
Univ Michigan Regents
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 Univ Michigan Regents filed Critical Univ Michigan Regents
Publication of SG11201809714TA publication Critical patent/SG11201809714TA/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization 1111111111111111111111111111110111111111111111111111111111111111110111111111 International Bureau (10) International Publication Number (43) International Publication Date .....0\"\" WO 2017/192543 Al 09 November 2017 (09.11.2017) W I P0 I P C T (51) International Patent Classification: C07D 401/04 (2006.01) A61K 31/4523 (2006.01) CO7D 401/14 (2006.01) A61K 31/454 (2006.01) CO7D 405/04 (2006.01) A61K 31/4545 (2006.01) CO7D 211/34 (2006.01) A61P 35/00 (2006.01) (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, (21) International Application Number: PCT/US2017/030577 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, (22) International Filing Date: KM, ML, MR, NE, SN, TD, TG). 02 May 2017 (02.05.2017) (25) Filing Language: English Published: — with international search report (Art. 21(3)) (26) Publication Language: English (30) Priority Data: 62/330,350 02 May 2016 (02.05.2016) US (71) Applicant: REGENTS OF THE UNIVERSITY OF MICHIGAN [US/US]; Office of Technology Trans- fer, 1600 Huron Parkway, 2nd Floor, Ann Arbor, MI 48109-2590 (US). _ (72) Inventors: WANG, Shaomeng; 3336 Stirling Ct., Superi- or Township, MI 49198 (US). AGUILAR, Angelo; 2364 - = Stone Rd., Ann Arbor, 48105 (US). ZHANG, Ke; 2411 Stone Rd., Ann Arbor, MI 48105 (US). XU, Shilin; 3578 =_ Green Brier Blvd., Apartment 405C, Ann Arbor, MI 48105 (US). XU, Tianfeng; 2153 Arbor Circle West, Apartment 205, Ypsilanti, 48197 (US). BERNARD, Denzil; 1803 = Pointe Crossing St., Apartment 101, Ann Arbor, MI 48105 = (US). HUANG, Liyue; 3170 Otter Creek Ct., Ann Arbor, MI 48105 (US). = (74) Agent: NAPOLI, James J.; Marshall, Gerstein & Borun = LLP, 233 S. Wacker Drive, 6300 Willis Tower, Chicago, IL 60606-6357 (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, 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. = 1-1 en (54) Title: PIPERIDINES AS MENIN INHIBITORS in ei (57) : The present disclosure provides compounds represented by Formula (I): (Formula(I)) R3b cT - and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R 2 , R 3a , R 3b , A, G, CP x , ,„ X, and Y are as defined as set forth in the specification. The present disclosure also provides compounds IN R 3 R 2 of Formula (I) for use to treat a condition or disorder responsive to menin inhibition such as cancer. 1-1 0 ei G O
SG11201809714TA 2016-05-02 2017-05-02 Piperidines as menin inhibitors SG11201809714TA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662330350P 2016-05-02 2016-05-02
PCT/US2017/030577 WO2017192543A1 (en) 2016-05-02 2017-05-02 Piperidines as menin inhibitors

Publications (1)

Publication Number Publication Date
SG11201809714TA true SG11201809714TA (en) 2018-11-29

Family

ID=58699299

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201809714TA SG11201809714TA (en) 2016-05-02 2017-05-02 Piperidines as menin inhibitors

Country Status (13)

Country Link
US (2) US10899738B2 (en)
EP (1) EP3452461B1 (en)
JP (1) JP6991585B2 (en)
KR (1) KR20190015275A (en)
CN (1) CN109415337B (en)
AU (1) AU2017259436B2 (en)
BR (1) BR112018072570A2 (en)
CA (1) CA3022868A1 (en)
ES (1) ES2899936T3 (en)
IL (2) IL262697B (en)
MX (1) MX2018013433A (en)
SG (1) SG11201809714TA (en)
WO (1) WO2017192543A1 (en)

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TWI703150B (en) 2015-06-04 2020-09-01 美商庫拉腫瘤技術股份有限公司 Methods and compositions for inhibiting the interaction of menin and mll proteins
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JP2021519785A (en) * 2018-03-30 2021-08-12 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Piperidine compounds as covalent menin inhibitors
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CA3112340A1 (en) * 2018-10-03 2020-04-09 The Regents Of The University Of Michigan Small molecule menin inhibitors
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AU2017259436B2 (en) 2021-08-26
BR112018072570A2 (en) 2019-02-19
KR20190015275A (en) 2019-02-13
US10899738B2 (en) 2021-01-26
IL262697A (en) 2018-12-31
WO2017192543A1 (en) 2017-11-09
AU2017259436A1 (en) 2018-12-20
US20210198237A1 (en) 2021-07-01
ES2899936T3 (en) 2022-03-15
CA3022868A1 (en) 2017-11-09
EP3452461B1 (en) 2021-09-08
CN109415337A (en) 2019-03-01
CN109415337B (en) 2022-01-18
MX2018013433A (en) 2019-07-18
JP2019514950A (en) 2019-06-06
IL262697B (en) 2021-04-29
US20190152947A1 (en) 2019-05-23
IL281182A (en) 2021-04-29
EP3452461A1 (en) 2019-03-13
JP6991585B2 (en) 2022-01-12

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