SG11201900328WA - Inhibitors of cyclin-dependent kinase 7 (cdk7) - Google Patents

Inhibitors of cyclin-dependent kinase 7 (cdk7)

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Publication number
SG11201900328WA
SG11201900328WA SG11201900328WA SG11201900328WA SG11201900328WA SG 11201900328W A SG11201900328W A SG 11201900328WA SG 11201900328W A SG11201900328W A SG 11201900328WA SG 11201900328W A SG11201900328W A SG 11201900328WA SG 11201900328W A SG11201900328W A SG 11201900328WA
Authority
SG
Singapore
Prior art keywords
quebec
international
avenue
cdk7
cyclin
Prior art date
Application number
SG11201900328WA
Inventor
Jason Marineau
Robert Zahler
Stephane Ciblat
Dana Winter
Anzhelika Kabro
Stephanie Roy
Darby Schmidt
Claudio Chuaqui
Goran Malojcic
Henri Piras
Kenneth Whitmore
Kate-Iyn Lund
Bill Sinko
Kevin Sprott
Original Assignee
Jason Marineau
Robert Zahler
Stephane Ciblat
Dana Winter
Anzhelika Kabro
Stephanie Roy
Darby Schmidt
Claudio Chuaqui
Goran Malojcic
Henri Piras
Kenneth Whitmore
Lund Kate Iyn
Bill Sinko
Kevin Sprott
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 Jason Marineau, Robert Zahler, Stephane Ciblat, Dana Winter, Anzhelika Kabro, Stephanie Roy, Darby Schmidt, Claudio Chuaqui, Goran Malojcic, Henri Piras, Kenneth Whitmore, Lund Kate Iyn, Bill Sinko, Kevin Sprott filed Critical Jason Marineau
Publication of SG11201900328WA publication Critical patent/SG11201900328WA/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1#11101111 0 11101 HOE 3E1 0 0111111 0111 OM HEIR 1111 OEN Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/013867 Al 18 January 2018 (18.01.2018) W I PO I PCT (51) International Patent Classification: MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, C07D 401/14 (2006.01) A61K 31/506 (2006.01) OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, A61P 35/00 (2006.01) SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, (21) International Application Number: TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. PCT/US2017/042017 (84) Designated States (unless otherwise indicated, for every (22) International Filing Date: kind of regional protection available): ARIPO (BW, GH, 13 July 2017 (13.07.2017) GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (25) Filing Language: English TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (26) Publication Language: English 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, (30) Priority Data: TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, 62/361,852 13 July 2016 (13.07.2016) US KM, ML, MR, NE, SN, TD, TG). (72) Inventors; and Published: (71) Applicants: MARINEAU, Jason, J. [US/US]; 2 MacKin- — with international search report (Art. 21(3)) tosh Street, Franklin, MA 02038 (US). ZAHLER, Robert — before the expiration of the time limit for amending the [US/US]; 5 East Welling Avenue, Pennington, NJ 08534 claims and to be republished in the event of receipt of (US). CIBLAT, Stephane [CA/CA]; 607-408 Rue Saint amendments (Rule 48.2(h)) Jacques, Montreal, Quebec, H2Y 1S2 (CA). WINTER, _ Dana, K. [CA/CA]; 431 Chemin de la Montagne, Rigaud, — Quebec, JOP 1P0 (CA). KABRO, Anzhelika [CA/CA]; = 815, 49e Avenue, Lachine, Quebec, H8T 2T3 (CA). ROY, 815, 49e Avenue, Lachine, = Stephanie [CA/CA]; Quebec, H8T 2T3 (CA). SCHMIDT, Darby [US/US]; 14 Mead Rd., Arlington, MA 02474 CHUAQUI, Claudio (US). 83 Menotomy Rd., Arlington, MA 02476 = [US/US]; (US). MALOJCIC, Goran [HR/US]; 1 Emerson Place, Apt = 7C, Boston, MA 02114 PIRAS, Henri (US). [FR/CA]; 201-6416 Rue de Ecores, Montreal, Quebec, H2G 2J5 (CA). = WHITMORE, Kenneth, Matthew [CA/CA]; 4974-217 = Place de la Savane, Montreal, Quebec, H4P OB1 (CA). — LUND, Kate-Iyn [CA/CA]; 15, 56e Avenue, Lachine, Que- bec, H8T 3B8 SINKO, Bill 37 Wyvern St., (CA). [US/US]; = Roslindale, MA 02131 (US). SPROTT, Kevin [US/US]; 40 = Rolling Lane, Needham, MA 02492 (US). (74) Agent: LARKIN, Angelyn et al.; Goodwin Procter LLP, 100 Northern Avenue, Boston, MA 02210 (US). = = (81) Designated States (unless otherwise indicated, for every = kind AE, AG, AL, AM, of national protection available): 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, Il IN (54) Title: INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7) of (57) : The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hy- en drates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involv- C ing the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple ----. myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. WD Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity 11 c;;;; ) of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. ei O
SG11201900328WA 2016-07-13 2017-07-13 Inhibitors of cyclin-dependent kinase 7 (cdk7) SG11201900328WA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662361852P 2016-07-13 2016-07-13
PCT/US2017/042017 WO2018013867A1 (en) 2016-07-13 2017-07-13 Inhibitors of cyclin dependnt kinase 7 (cdk7)

Publications (1)

Publication Number Publication Date
SG11201900328WA true SG11201900328WA (en) 2019-02-27

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SG11201900328WA SG11201900328WA (en) 2016-07-13 2017-07-13 Inhibitors of cyclin-dependent kinase 7 (cdk7)
SG10202012466PA SG10202012466PA (en) 2016-07-13 2017-07-13 Inhibitors of cyclin-dependent kinase 7 (cdk7)

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US (1) US20230062491A1 (en)
EP (1) EP3484871B1 (en)
JP (2) JP7058636B2 (en)
KR (1) KR102587758B1 (en)
CN (1) CN110036004A (en)
AU (2) AU2017295863B2 (en)
BR (1) BR112019000716A2 (en)
CA (1) CA3030795A1 (en)
ES (1) ES2954278T3 (en)
IL (2) IL264222B (en)
MX (2) MX2019000527A (en)
RU (1) RU2019103870A (en)
SG (2) SG11201900328WA (en)
WO (1) WO2018013867A1 (en)
ZA (1) ZA201900874B (en)

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IL264222B (en) 2022-05-01
RU2019103870A (en) 2020-08-14
JP2022020860A (en) 2022-02-01
SG10202012466PA (en) 2021-01-28
WO2018013867A8 (en) 2018-11-15
ZA201900874B (en) 2023-12-20
IL292422A (en) 2022-06-01
CN110036004A (en) 2019-07-19
JP7058636B2 (en) 2022-04-22
ES2954278T3 (en) 2023-11-21
KR102587758B1 (en) 2023-10-12
WO2018013867A1 (en) 2018-01-18
JP7460593B2 (en) 2024-04-02
AU2017295863B2 (en) 2022-07-07
IL264222A (en) 2019-02-28
EP4295852A2 (en) 2023-12-27
US20230062491A1 (en) 2023-03-02
RU2019103870A3 (en) 2020-11-09
MX2019000527A (en) 2019-08-12
CA3030795A1 (en) 2018-01-18
MX2022005898A (en) 2022-06-27
AU2022246416A1 (en) 2022-11-03
AU2017295863A1 (en) 2019-02-07
EP3484871B1 (en) 2023-06-07
KR20190038841A (en) 2019-04-09
JP2019527217A (en) 2019-09-26
BR112019000716A2 (en) 2019-05-07
EP3484871A1 (en) 2019-05-22

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