SG11201909083UA - Piperidines as covalent menin inhibitors - Google Patents

Piperidines as covalent menin inhibitors

Info

Publication number
SG11201909083UA
SG11201909083UA SG11201909083UA SG11201909083UA SG 11201909083U A SG11201909083U A SG 11201909083UA SG 11201909083U A SG11201909083U A SG 11201909083UA SG 11201909083U A SG11201909083U A SG 11201909083UA
Authority
SG
Singapore
Prior art keywords
international
ann arbor
menin
piperidines
covalent
Prior art date
Application number
Inventor
Shaomeng Wang
Angelo Aguilar
Shilin Xu
Liyue Huang
Jeanne Stuckey
Xu Tianfeng
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 SG11201909083UA publication Critical patent/SG11201909083UA/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

1 (54) Title: PIPERIDINES AS COVALENT MENIN INHIBITORS IN ir) R id Ot 1 R1° en N1 ) , GC R 8b ''''''' . - 71 'R i j e V r1 N Il A 0 .... 1 . 5 ° R8a o x, z2 (I) (57) : The present disclosure provides compounds represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, R la , R ib R ic , R id , R 2 , R , R 3 8a , R , R 8b 10 , m, and n are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat a condition or disorder responsive to menin inhibition such as cancer. (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 04 October 2018 (04.10.2018) W I PO I PC T oimiolo VIII °nolo III OH H ioo Imo oimIE (10) International Publication Number WO 2018/183857 Al (51) International Patent Classification: A61K 31/445 (2006.01) C07D 401/06 (2006.01) C07D 211/26 (2006.01) (21) International Application Number: PCT/US2018/025417 (22) International Filing Date: 30 March 2018 (30.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/479,520 31 March 2017 (31.03.2017) US (71) Applicant: THE 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 48198 (US). AGUILAR, Angelo; 2364 Stone Rd., Ann Arbor, MI 48105 (US). XU, Shilin; 3578 Green Brier Blvd., Apartment 405C, Ann Arbor, MI 48105 (US). HUANG, Liyue; 3170 Otter Creek Ct., Ann Arbor, MI 48105 (US). STUCKEY, Jeanne; 13536 Lakebrook Drive, Fenton, MI 48430 (US). TIANFENG, Xu; 2153 Ar- bor Circle West, Apartment 205, Ypsilanti, MI 48197 (US). (74) Agent: NAPOLI, James, J.; Marshall, Gerstein & Borun LLP, 233 S. Wacker Drive, 6300 Wills 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, 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). Published: with international search report (Art. 2 I (3)) C
SG11201909083U 2017-03-31 2018-03-30 Piperidines as covalent menin inhibitors SG11201909083UA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762479520P 2017-03-31 2017-03-31
PCT/US2018/025417 WO2018183857A1 (en) 2017-03-31 2018-03-30 Piperidines as covalent menin inhibitors

Publications (1)

Publication Number Publication Date
SG11201909083UA true SG11201909083UA (en) 2019-10-30

Family

ID=63677047

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201909083U SG11201909083UA (en) 2017-03-31 2018-03-30 Piperidines as covalent menin inhibitors

Country Status (13)

Country Link
US (1) US11045448B2 (en)
EP (1) EP3600313A4 (en)
JP (1) JP2020515571A (en)
KR (1) KR20190133224A (en)
CN (1) CN110636843A (en)
AU (1) AU2018243586A1 (en)
BR (1) BR112019020130A2 (en)
CA (1) CA3058448A1 (en)
EA (1) EA201992320A1 (en)
IL (1) IL269542A (en)
MX (1) MX2019011412A (en)
SG (1) SG11201909083UA (en)
WO (1) WO2018183857A1 (en)

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AU2019351820A1 (en) * 2018-10-03 2021-03-04 Agios Pharmaceuticals, Inc. Small molecule menin inhibitors
US11084825B2 (en) 2018-12-31 2021-08-10 Biomea Fusion, Llc Substituted pyridines as irreversible inhibitors of menin-MLL interaction
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WO2021067215A1 (en) 2019-09-30 2021-04-08 Agios Pharmaceuticals, Inc. Piperidine compounds as menin inhibitors
WO2021207310A1 (en) 2020-04-08 2021-10-14 Agios Pharmaceuticals, Inc. Menin inhibitors and methods of use for treating cancer
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Also Published As

Publication number Publication date
IL269542A (en) 2019-11-28
JP2020515571A (en) 2020-05-28
CN110636843A (en) 2019-12-31
BR112019020130A2 (en) 2020-04-22
US11045448B2 (en) 2021-06-29
CA3058448A1 (en) 2018-10-04
WO2018183857A1 (en) 2018-10-04
EA201992320A1 (en) 2020-04-22
KR20190133224A (en) 2019-12-02
MX2019011412A (en) 2020-02-07
EP3600313A4 (en) 2020-09-23
AU2018243586A1 (en) 2019-10-17
EP3600313A1 (en) 2020-02-05
US20200022953A1 (en) 2020-01-23

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