CN106604746B - 用于治疗耐药性癌症的脂肪酸合成酶抑制剂 - Google Patents

用于治疗耐药性癌症的脂肪酸合成酶抑制剂 Download PDF

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CN106604746B
CN106604746B CN201580042834.1A CN201580042834A CN106604746B CN 106604746 B CN106604746 B CN 106604746B CN 201580042834 A CN201580042834 A CN 201580042834A CN 106604746 B CN106604746 B CN 106604746B
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alkyl
formula
taxane
compound
treating
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CN106604746A (zh
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T·S·霍耶尔
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Ganglai Pharmaceutical Co ltd
Sagimit Biosciences
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3V Biosciences Inc
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    • 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
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/643—Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6921—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a particulate, a powder, an adsorbate, a bead or a sphere
    • A61K47/6927—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a particulate, a powder, an adsorbate, a bead or a sphere the form being a solid microparticle having no hollow or gas-filled cores
    • A61K47/6929—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a particulate, a powder, an adsorbate, a bead or a sphere the form being a solid microparticle having no hollow or gas-filled cores the form being a nanoparticle, e.g. an immuno-nanoparticle
    • A61K47/6931—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a particulate, a powder, an adsorbate, a bead or a sphere the form being a solid microparticle having no hollow or gas-filled cores the form being a nanoparticle, e.g. an immuno-nanoparticle the material constituting the nanoparticle being a polymer
    • A61K47/6935—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a particulate, a powder, an adsorbate, a bead or a sphere the form being a solid microparticle having no hollow or gas-filled cores the form being a nanoparticle, e.g. an immuno-nanoparticle the material constituting the nanoparticle being a polymer the polymer being obtained otherwise than by reactions involving carbon to carbon unsaturated bonds, e.g. polyesters, polyamides or polyglycerol
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nanotechnology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201580042834.1A 2014-08-15 2015-08-14 用于治疗耐药性癌症的脂肪酸合成酶抑制剂 Active CN106604746B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462038113P 2014-08-15 2014-08-15
US62/038,113 2014-08-15
PCT/US2015/045244 WO2016025816A1 (en) 2014-08-15 2015-08-14 Fatty acid synthase inhibitor for use in the treatment of drug resistant cancer

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CN106604746A CN106604746A (zh) 2017-04-26
CN106604746B true CN106604746B (zh) 2020-07-10

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US (1) US10363249B2 (enExample)
EP (1) EP3179990B1 (enExample)
JP (2) JP6691909B2 (enExample)
KR (1) KR102504168B1 (enExample)
CN (1) CN106604746B (enExample)
ES (1) ES2833454T3 (enExample)
WO (1) WO2016025816A1 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170119786A1 (en) 2011-03-08 2017-05-04 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis
CA2877999C (en) * 2012-07-03 2021-02-23 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis
JP6691909B2 (ja) 2014-08-15 2020-05-13 サギメット バイオサイエンシーズ インコーポレイテッド 薬物耐性癌の治療で用いるための脂肪酸シンターゼ阻害剤
EP3277675B1 (en) 2015-03-19 2022-01-19 Sagimet Biosciences Inc. Heterocyclic modulators of lipid synthesis
JP7668509B2 (ja) * 2016-11-11 2025-04-25 サギメット バイオサイエンシーズ インコーポレイテッド 脂質合成の複素環式モジュレーター
EP3801069A4 (en) 2018-06-01 2022-03-16 Cornell University MULTIPLE THERAPY FOR DISEASE OR DISORDER ASSOCIATED WITH PI3K
CN108853060B (zh) * 2018-09-06 2020-09-18 中山万汉制药有限公司 一种包含奥利司他的纳米微球及其制备方法和用途
US20220400732A1 (en) * 2019-03-21 2022-12-22 Cornell University Anti-fructose therapy for colorectal and small intestine cancers
CN113577053A (zh) * 2021-08-10 2021-11-02 重庆大学附属肿瘤医院 木犀草素在制备靶向抑制卵巢癌干细胞的药物中的应用

Citations (1)

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WO2012122391A1 (en) * 2011-03-08 2012-09-13 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis

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PL1959951T3 (pl) 2005-12-01 2010-06-30 Hoffmann La Roche Heteroarylo-podstawione pochodne piperydyny jako inhibitory l-cpt1
AU2007292306A1 (en) 2006-09-05 2008-03-13 Bipar Sciences, Inc. Inhibition of fatty acid synthesis by PARP inhibitors and methods of treatment thereof
WO2008059214A1 (en) 2006-11-13 2008-05-22 Astrazeneca Ab Bisamlde derivatives and use thereof as fatty acid synthase inhibitors
TW200831092A (en) 2006-12-21 2008-08-01 Astrazeneca Ab Therapeutic agents
TW200833663A (en) 2006-12-21 2008-08-16 Astrazeneca Ab Therapeutic agents
WO2008075077A1 (en) 2006-12-21 2008-06-26 Astrazeneca Ab Piperidine derivatives for the treatment of obesity
US9624173B2 (en) 2011-03-08 2017-04-18 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis
US20170119786A1 (en) 2011-03-08 2017-05-04 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis
TWI522348B (zh) 2011-03-08 2016-02-21 ３ Ｖ生物科技公司 脂質合成之雜環調節劑
US20130287791A1 (en) * 2012-04-25 2013-10-31 C. Wilson Xu Modulation of histone h2b monoubiquitination and treatment of cancer
CA2877999C (en) 2012-07-03 2021-02-23 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis
EP3083583B1 (en) 2013-12-20 2020-11-18 Sagimet Biosciences Inc. Heterocyclic modulators of lipid synthesis and combinations thereof
EP3092232B1 (en) 2014-01-07 2022-03-09 Sagimet Biosciences Inc. Heterocyclic modulators of lipid synthesis for use against cancer and viral infections
JP6691909B2 (ja) 2014-08-15 2020-05-13 サギメット バイオサイエンシーズ インコーポレイテッド 薬物耐性癌の治療で用いるための脂肪酸シンターゼ阻害剤
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Also Published As

Publication number Publication date
KR102504168B1 (ko) 2023-02-27
KR20170034391A (ko) 2017-03-28
JP2017524003A (ja) 2017-08-24
WO2016025816A1 (en) 2016-02-18
EP3179990B1 (en) 2020-10-14
US20170273964A1 (en) 2017-09-28
ES2833454T3 (es) 2021-06-15
EP3179990A1 (en) 2017-06-21
CN106604746A (zh) 2017-04-26
JP6691909B2 (ja) 2020-05-13
JP2020055878A (ja) 2020-04-09
US10363249B2 (en) 2019-07-30

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