CA3168069A1 - Setd2 inhibitors and related methods and uses, including combination therapies - Google Patents

Setd2 inhibitors and related methods and uses, including combination therapies Download PDF

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Publication number
CA3168069A1
CA3168069A1 CA3168069A CA3168069A CA3168069A1 CA 3168069 A1 CA3168069 A1 CA 3168069A1 CA 3168069 A CA3168069 A CA 3168069A CA 3168069 A CA3168069 A CA 3168069A CA 3168069 A1 CA3168069 A1 CA 3168069A1
Authority
CA
Canada
Prior art keywords
alkyl
methyl
indole
fluoro
carboxamide
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA3168069A
Other languages
English (en)
French (fr)
Inventor
Maria Alejandra Raimondi
Jennifer Anne TOTMAN
Vinny MOTWANI
Katherine Louise Cosmopoulos
John Lampe
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Epizyme Inc
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA3168069A1 publication Critical patent/CA3168069A1/en
Pending legal-status Critical Current

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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
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/40—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
    • A61K31/407—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 condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
CA3168069A 2020-02-19 2021-02-19 Setd2 inhibitors and related methods and uses, including combination therapies Pending CA3168069A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202062978692P 2020-02-19 2020-02-19
US62/978,692 2020-02-19
PCT/US2021/018863 WO2021168313A1 (en) 2020-02-19 2021-02-19 Setd2 inhibitors and related methods and uses, including combination therapies

Publications (1)

Publication Number Publication Date
CA3168069A1 true CA3168069A1 (en) 2021-08-26

Family

ID=77391740

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3168069A Pending CA3168069A1 (en) 2020-02-19 2021-02-19 Setd2 inhibitors and related methods and uses, including combination therapies

Country Status (11)

Country Link
US (1) US20230133671A1 (https=)
EP (1) EP4107157A4 (https=)
JP (1) JP2023514280A (https=)
KR (1) KR20220143116A (https=)
CN (2) CN121695288A (https=)
AU (1) AU2021224855A1 (https=)
BR (1) BR112022016573A2 (https=)
CA (1) CA3168069A1 (https=)
IL (1) IL295654A (https=)
MX (1) MX2022010171A (https=)
WO (1) WO2021168313A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020530844A (ja) 2017-08-14 2020-10-29 エピザイム，インコーポレイティド Ｓｅｔｄ２を阻害することにより癌を処置する方法
CN111093660A (zh) * 2017-09-05 2020-05-01 Epizyme股份有限公司 用于治疗癌症的组合疗法
CN112585119A (zh) 2018-08-14 2021-03-30 Epizyme股份有限公司 经取代的吲哚及其使用方法
US20240299352A1 (en) * 2021-06-09 2024-09-12 Epizyme, Inc. Combination therapies with setd2 inhibitors
JP2024539726A (ja) * 2021-11-01 2024-10-29 エピザイム，インコーポレイティド Ｎ－（（１ｒ，３ｓ）－３－（４－アセチルピペラジン－１－イル）シクロヘキシル）－４－フルオロ－７－メチル－１ｈ－インドール－２－カルボキサミドの結晶形態

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4595766A (en) * 1984-10-26 1986-06-17 Ciba-Geigy Corporation Process for the preparation of an indoline carboxylic acid
US20100035862A1 (en) * 2008-06-25 2010-02-11 Abbott Laboratories Novel aza-cyclic indole-2-carboxamides and methods of use thereof
NZ725860A (en) * 2014-04-04 2019-08-30 Iomet Pharma Ltd Indole derivatives for use in medicine
WO2016040505A1 (en) * 2014-09-10 2016-03-17 Epizyme, Inc. Smyd inhibitors
CN112585119A (zh) * 2018-08-14 2021-03-30 Epizyme股份有限公司 经取代的吲哚及其使用方法
SG11202105325QA (en) * 2018-11-30 2021-06-29 Epizyme Inc Methods of treating whsc1-overexpressing cancers by inhibiting setd2

Also Published As

Publication number Publication date
EP4107157A4 (en) 2024-03-13
MX2022010171A (es) 2022-12-06
BR112022016573A2 (pt) 2022-11-08
WO2021168313A1 (en) 2021-08-26
KR20220143116A (ko) 2022-10-24
EP4107157A1 (en) 2022-12-28
CN115380033B (zh) 2026-01-09
AU2021224855A1 (en) 2022-09-08
CN121695288A (zh) 2026-03-20
CN115380033A (zh) 2022-11-22
US20230133671A1 (en) 2023-05-04
IL295654A (en) 2022-10-01
JP2023514280A (ja) 2023-04-05

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