CA3028355A1 - Glucose uptake inhibitors - Google Patents

Glucose uptake inhibitors Download PDF

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Publication number
CA3028355A1
CA3028355A1 CA3028355A CA3028355A CA3028355A1 CA 3028355 A1 CA3028355 A1 CA 3028355A1 CA 3028355 A CA3028355 A CA 3028355A CA 3028355 A CA3028355 A CA 3028355A CA 3028355 A1 CA3028355 A1 CA 3028355A1
Authority
CA
Canada
Prior art keywords
mixture
mmol
alkyl
amino
pyrimidin
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
CA3028355A
Other languages
English (en)
French (fr)
Inventor
Kellen OLSZEWSKI
Ji-In Kim
Masha POYUROVSKY
Kevin Liu
Anthony BARSOTTI
Koi Morris
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.)
Kadmon Corp LLC
Original Assignee
Kadmon Corp LLC
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 Kadmon Corp LLC filed Critical Kadmon Corp LLC
Publication of CA3028355A1 publication Critical patent/CA3028355A1/en
Abandoned legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/52Purines, e.g. adenine
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CA3028355A 2015-06-26 2016-06-24 Glucose uptake inhibitors Abandoned CA3028355A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562185223P 2015-06-26 2015-06-26
US62/185,223 2015-06-26
PCT/US2016/039365 WO2016210330A1 (en) 2015-06-26 2016-06-24 Glucose uptake inhibitors

Publications (1)

Publication Number Publication Date
CA3028355A1 true CA3028355A1 (en) 2016-12-29

Family

ID=57586425

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3028355A Abandoned CA3028355A1 (en) 2015-06-26 2016-06-24 Glucose uptake inhibitors

Country Status (8)

Country Link
US (2) US10273248B2 (enExample)
EP (1) EP3313825A4 (enExample)
JP (1) JP2018518518A (enExample)
CN (1) CN108349910A (enExample)
CA (1) CA3028355A1 (enExample)
EA (1) EA201890153A1 (enExample)
HK (1) HK1254835A1 (enExample)
WO (1) WO2016210330A1 (enExample)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3048729C (en) * 2017-01-26 2023-01-03 Youla S. Tsantrizos Substituted bicyclic pyrimidine-based compounds and compositions and uses thereof
WO2018201006A1 (en) * 2017-04-28 2018-11-01 Kadmon Corporation, Llc Treatment of inflammatory conditions and autoimmune diseases with glucose uptake inhibitors
CN109020957B (zh) * 2017-06-12 2023-01-13 南京天印健华医药科技有限公司 作为mnk抑制剂的杂环化合物
CA3063616A1 (en) 2017-06-30 2019-12-06 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof
WO2019000683A1 (zh) 2017-06-30 2019-01-03 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
CN110573501B (zh) 2017-06-30 2023-09-29 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
CN109384782A (zh) * 2017-08-04 2019-02-26 厦门大学 取代五元并六元杂环类化合物、其制备方法、药物组合及其用途
US10933061B2 (en) 2017-12-21 2021-03-02 Shepherd Therapeutics, Inc. Pyrvinium pamoate therapies and methods of use
US10689386B2 (en) 2018-03-07 2020-06-23 Duquesne University Of The Holy Spirit Pyrazolo[4,3-d]pyrimidines as antitumor agents
US12030857B2 (en) 2018-06-25 2024-07-09 Kadmon Corporation, Llc Glucose uptake inhibitors
IL292515A (en) * 2019-11-13 2022-06-01 Metabomed Ltd Glucose uptake inhibitors and uses thereof
BR112022010254A2 (pt) * 2019-12-02 2022-09-06 Shanghai Yingli Pharm Co Ltd Composto heterocíclico contendo oxigênio representado pela fórmula i, método para preparar o composto heterocíclico contendo oxigênio, composto, composição farmacêutica e uso composto heterocíclico contendo oxigênio
JP7772771B2 (ja) * 2020-07-14 2025-11-18 武漢朗来科技発展有限公司 Rock阻害剤及びその製造方法と用途
CN112479913A (zh) * 2020-11-19 2021-03-12 安徽修一制药有限公司 一种n,n-二乙基氯代乙酰胺的制备方法
CN112741828B (zh) * 2021-01-08 2022-04-26 武汉大学 药物联用物及其制备方法和用途
US20240109868A1 (en) * 2022-08-29 2024-04-04 Miracure Biotechnology Limited Ep300/cbp modulator, preparation method therefor and use thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2305435T3 (es) * 2002-01-10 2008-11-01 Bayer Healthcare Ag Inhibidores de la rho-quinasa.
EP2220091B1 (en) * 2007-12-14 2012-07-25 Ardea Biosciences, Inc. Reverse transcriptase inhibitors
WO2011046970A1 (en) * 2009-10-12 2011-04-21 Myrexis, Inc. Amino - pyrimidine compounds as inhibitors of tbkl and/or ikk epsilon
WO2012040499A2 (en) * 2010-09-22 2012-03-29 Surface Logix, Inc. Metabolic inhibitors
CA2831634C (en) * 2011-04-21 2019-11-12 Origenis Gmbh Pyrazolo [4,3-d] pyrimidines useful as kinase inhibitors
CN102901456B (zh) 2012-09-12 2015-10-28 深圳深蓝精机有限公司 检测装置及检测圆轴的外径、跳动值、真圆度的方法
EP4116293A3 (en) * 2012-10-05 2023-03-29 Kadmon Corporation, LLC Rho kinase inhibitors
WO2016210331A1 (en) * 2015-06-26 2016-12-29 Kadmon Corporation, Llc Treatment of infectious diseases with glucose uptake inhibitors

Also Published As

Publication number Publication date
HK1254835A1 (zh) 2019-07-26
JP2018518518A (ja) 2018-07-12
US10988484B2 (en) 2021-04-27
US20180298029A1 (en) 2018-10-18
US10273248B2 (en) 2019-04-30
US20190315772A1 (en) 2019-10-17
CN108349910A (zh) 2018-07-31
EP3313825A4 (en) 2019-03-13
EP3313825A1 (en) 2018-05-02
WO2016210330A1 (en) 2016-12-29
EA201890153A1 (ru) 2018-06-29

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20220301