JP2020520949A - 組成物、並びにミトコンドリア脱共役剤を調製及び使用する方法 - Google Patents

組成物、並びにミトコンドリア脱共役剤を調製及び使用する方法 Download PDF

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Publication number
JP2020520949A
JP2020520949A JP2019564449A JP2019564449A JP2020520949A JP 2020520949 A JP2020520949 A JP 2020520949A JP 2019564449 A JP2019564449 A JP 2019564449A JP 2019564449 A JP2019564449 A JP 2019564449A JP 2020520949 A JP2020520949 A JP 2020520949A
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alkyl
nmr
mhz
compound
phenyl
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JP2019564449A
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Japanese (ja)
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JP2020520949A5 (enExample
Inventor
ヘーン、カイル
エル． サントス、ウェブスター
エル． サントス、ウェブスター
エス． チャイルドレス、エリザベス
エス． チャイルドレス、エリザベス
ダイ、ユミン
マリー、ジェイコブ
サンティアゴ−リヴェラ、ホセ
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Verginia, University of, Patent Foundation of
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Verginia, University of, Patent Foundation of
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Publication of JP2020520949A publication Critical patent/JP2020520949A/ja
Publication of JP2020520949A5 publication Critical patent/JP2020520949A5/ja
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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
    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D241/20—Nitrogen atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2019564449A 2017-05-22 2018-05-22 組成物、並びにミトコンドリア脱共役剤を調製及び使用する方法 Pending JP2020520949A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762509249P 2017-05-22 2017-05-22
US62/509,249 2017-05-22
PCT/US2018/033901 WO2018217757A1 (en) 2017-05-22 2018-05-22 Compositions and methods for preparing and using mitochondrial uncouplers

Publications (2)

Publication Number Publication Date
JP2020520949A true JP2020520949A (ja) 2020-07-16
JP2020520949A5 JP2020520949A5 (enExample) 2021-07-26

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JP2019564449A Pending JP2020520949A (ja) 2017-05-22 2018-05-22 組成物、並びにミトコンドリア脱共役剤を調製及び使用する方法

Country Status (4)

Country Link
US (1) US11896591B2 (enExample)
EP (1) EP3630115B1 (enExample)
JP (1) JP2020520949A (enExample)
WO (1) WO2018217757A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3565806T (pt) 2017-01-06 2022-05-19 Rivus Pharmaceuticals Inc Novos derivados de fenilo
EP3781567B1 (en) 2018-04-20 2022-08-24 Virginia Tech Intellectual Properties, Inc. Imidazopyridines useful as mitochondrial uncouplers
EP4482494A4 (en) * 2022-02-21 2026-02-25 Univ Colorado Regents RE-SENSITIZATION OF MULTI-DRUG-RESISTANT GRAM-NEGATIVE (MDR) BACTERIA TO COLISTIN USING IONOPHORES
US20260021071A1 (en) * 2022-06-30 2026-01-22 University Of Florida Research Foundation, Incorporated Small molecule broad-spectrum antibiotics
CN116535420A (zh) * 2023-04-21 2023-08-04 西安近代化学研究所 一种5,6-二氯呋咱并[3,4-b]吡嗪的合成方法
WO2026149323A1 (en) * 2025-01-07 2026-07-16 Shenzhen Hightide Biopharmaceutical Ltd. Compositions and methods of using mitochondrial uncouplers and glp-1 receptor agonists

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007008541A2 (en) * 2005-07-08 2007-01-18 Kalypsys, Inc. Cellular cholesterol absorption modifiers
JP2008515979A (ja) * 2004-10-14 2008-05-15 コンパス ファーマシューティカルズ リミティド ライアビリティ カンパニー フラザノ‘３，４−ビピラジン（ｂｉｐｙｒａｚｉｎｅ）及び抗腫瘍剤としてのその使用
JP2010500994A (ja) * 2006-08-16 2010-01-14 エグゼリクシス， インコーポレイテッド Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
WO2013192388A1 (en) * 2012-06-20 2013-12-27 University Of Virginia Patent Foundation Compositions and methods for regulating glucose homeostasis and insulin action

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL237129A (enExample) 1959-03-14
FR2501680A1 (fr) 1981-03-12 1982-09-17 Elf Aquitaine Synthese de tetra mercaptides stanniques
US4472840A (en) 1981-09-21 1984-09-25 Jefferies Steven R Method of inducing osseous formation by implanting bone graft material
US4559157A (en) 1983-04-21 1985-12-17 Creative Products Resource Associates, Ltd. Cosmetic applicator useful for skin moisturizing
LU84979A1 (fr) 1983-08-30 1985-04-24 Oreal Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux
US4820508A (en) 1987-06-23 1989-04-11 Neutrogena Corporation Skin protective composition
US5606019A (en) 1987-10-29 1997-02-25 Protien Polymer Technologies, Inc. Synthetic protein as implantables
GB2215209B (en) 1988-03-14 1992-08-26 Osmed Inc Method and apparatus for biodegradable, osteogenic, bone graft substitute device
US4992478A (en) 1988-04-04 1991-02-12 Warner-Lambert Company Antiinflammatory skin moisturizing composition and method of preparing same
US4938949A (en) 1988-09-12 1990-07-03 University Of New York Treatment of damaged bone marrow and dosage units therefor
JPH0327172A (ja) 1989-06-19 1991-02-05 Nissan Chem Ind Ltd 布の漂白方法
US5645591A (en) 1990-05-29 1997-07-08 Stryker Corporation Synthetic bone matrix
EP2513125B1 (de) 2009-12-14 2014-10-29 Basf Se Metallkomplexe, enthaltend diazabenzimidazolcarben-liganden und deren verwendung in oleds

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008515979A (ja) * 2004-10-14 2008-05-15 コンパス ファーマシューティカルズ リミティド ライアビリティ カンパニー フラザノ‘３，４−ビピラジン（ｂｉｐｙｒａｚｉｎｅ）及び抗腫瘍剤としてのその使用
WO2007008541A2 (en) * 2005-07-08 2007-01-18 Kalypsys, Inc. Cellular cholesterol absorption modifiers
JP2010500994A (ja) * 2006-08-16 2010-01-14 エグゼリクシス， インコーポレイテッド Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
WO2013192388A1 (en) * 2012-06-20 2013-12-27 University Of Virginia Patent Foundation Compositions and methods for regulating glucose homeostasis and insulin action

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
FERNANDEZ,E. ET AL.: "Solid-phase versus solution synthesis of asymmetrically disubstituted furazano[3,4-b]pyrazines", TETRAHEDRON LETTERS, vol. 43, no. 27, JPN6022006400, 2002, pages 4741 - 4745, ISSN: 0004711125 *
KENWOOD,B.M. ET AL.: "Structure-activity relationships of furazano[3,4-b]pyrazines as mitochondrial uncouplers", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 25, no. 21, JPN6022006401, 2015, pages 4858 - 4861, ISSN: 0004711124 *
STARCHENKOV,I.B. ET AL.: "Chemistry of furazano[3,4-b]pyrazines. 3. Method for the synthesis of 5,6-disubstituted furazano[3,4", CHEMISTRY OF HETEROCYCLIC COMPOUNDS(NEW YORK)(TRANSLATION OF KHIMIYA GETEROTSIKLICHESKIKH SOEDINENII, vol. 33, no. 10, JPN6022006399, 1998, pages 1219 - 1233, ISSN: 0004711126 *
STN INTERNATIONAL，FILE REGISTRY [ONLINE]，[令和４年１月２８日検索]，CAS REGISTRY NO. 1797876-98-2 (, JPN7022000701, ISSN: 0004711127 *

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WO2018217757A1 (en) 2018-11-29
US20200323846A1 (en) 2020-10-15
EP3630115A1 (en) 2020-04-08
US11896591B2 (en) 2024-02-13
EP3630115B1 (en) 2025-12-10

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