CA3052810A1 - Benzothiophene estrogen receptor modulators - Google Patents

Benzothiophene estrogen receptor modulators Download PDF

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Publication number
CA3052810A1
CA3052810A1 CA3052810A CA3052810A CA3052810A1 CA 3052810 A1 CA3052810 A1 CA 3052810A1 CA 3052810 A CA3052810 A CA 3052810A CA 3052810 A CA3052810 A CA 3052810A CA 3052810 A1 CA3052810 A1 CA 3052810A1
Authority
CA
Canada
Prior art keywords
compound
pharmaceutically acceptable
formula
acceptable salt
cancer
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.)
Abandoned
Application number
CA3052810A
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English (en)
French (fr)
Inventor
Jay Copeland Strum
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.)
G1 Therapeutics Inc
Original Assignee
G1 Therapeutics 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 G1 Therapeutics Inc filed Critical G1 Therapeutics Inc
Publication of CA3052810A1 publication Critical patent/CA3052810A1/en
Abandoned legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/64Oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/40Heterocyclic 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
    • A61K31/4025Heterocyclic 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/4535Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • 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
    • A61K31/499Spiro-condensed pyrazines or piperazines
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures 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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA3052810A 2017-02-10 2018-02-09 Benzothiophene estrogen receptor modulators Abandoned CA3052810A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201762457643P 2017-02-10 2017-02-10
US62/457,643 2017-02-10
US201762460358P 2017-02-17 2017-02-17
US62/460,358 2017-02-17
US201862614279P 2018-01-05 2018-01-05
US62/614,279 2018-01-05
PCT/US2018/017668 WO2018148576A1 (en) 2017-02-10 2018-02-09 Benzothiophene estrogen receptor modulators

Publications (1)

Publication Number Publication Date
CA3052810A1 true CA3052810A1 (en) 2018-08-16

Family

ID=63106724

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3052810A Abandoned CA3052810A1 (en) 2017-02-10 2018-02-09 Benzothiophene estrogen receptor modulators

Country Status (10)

Country Link
US (3) US10208011B2 (OSRAM)
EP (1) EP3580223A4 (OSRAM)
JP (1) JP2020507566A (OSRAM)
KR (1) KR20190117582A (OSRAM)
CN (1) CN110461853A (OSRAM)
AU (1) AU2018217809A1 (OSRAM)
CA (1) CA3052810A1 (OSRAM)
IL (1) IL268319A (OSRAM)
TW (1) TW201835064A (OSRAM)
WO (1) WO2018148576A1 (OSRAM)

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Publication number Priority date Publication date Assignee Title
EP2968291B1 (en) * 2013-03-15 2025-04-16 Pharmacosmos Holding A/S Hspc-sparing treatments for rb-positive abnormal cellular proliferation
WO2018005863A1 (en) * 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Pyrimidine-based compounds for the treatment of cancer
AU2018205262A1 (en) 2017-01-06 2019-07-11 G1 Therapeutics, Inc. Combination therapy for the treatment of cancer
KR102765922B1 (ko) * 2018-02-06 2025-02-11 더 보오드 오브 트러스티스 오브 더 유니버시티 오브 일리노이즈 선택적인 에스트로겐 수용체 분해제로서의 치환된 벤조티오펜 유사체
CN108203404A (zh) * 2018-03-02 2018-06-26 上海博邦医药科技有限公司 (r)-3-苯基哌啶或/和(s)-3-苯基哌啶以及尼拉帕尼的手性中间体的合成方法
EP3836916A1 (en) * 2018-08-16 2021-06-23 G1 Therapeutics, Inc. Benzothiophene estrogen receptor modulators to treat medical disorders
WO2021065898A1 (ja) 2019-09-30 2021-04-08 日本ケミファ株式会社 アゼパン誘導体
ES3048084T3 (en) 2020-05-19 2025-12-09 Pharmacosmos Holding As Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders
CN113816892A (zh) * 2021-08-27 2021-12-21 安徽鼎旺医药有限公司 一种醋酸巴多昔芬的合成方法
CN113801094A (zh) * 2021-10-29 2021-12-17 中国药科大学 一种2-羰基苯并噻吩类化合物及其制备方法和用途

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Also Published As

Publication number Publication date
TW201835064A (zh) 2018-10-01
US20190119243A1 (en) 2019-04-25
US20180230123A1 (en) 2018-08-16
US10208011B2 (en) 2019-02-19
US20200216406A1 (en) 2020-07-09
US10633362B2 (en) 2020-04-28
IL268319A (en) 2019-09-26
EP3580223A4 (en) 2021-01-06
WO2018148576A1 (en) 2018-08-16
US10981887B2 (en) 2021-04-20
CN110461853A (zh) 2019-11-15
EP3580223A1 (en) 2019-12-18
AU2018217809A1 (en) 2019-08-22
KR20190117582A (ko) 2019-10-16
JP2020507566A (ja) 2020-03-12

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20230809