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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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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Japan
Prior art keywords
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
Pending legal-status Critical Current

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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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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 (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117024351A (zh) 2017-01-06 2023-11-10 里维斯制药股份有限公司 新型苯基衍生物
KR102900692B1 (ko) * 2018-04-20 2025-12-15 버지니아 테크 인터렉추얼 프라퍼티스, 인크. 미토콘드리아 언커플러로서 유용한 이미다조피리딘
WO2023159248A1 (en) * 2022-02-21 2023-08-24 The Regents Of The University Of Colorado A Body Corporate Re-sensitizing multidrug-resistant (mdr) gram-negative bacteria to colistin using ionophores
WO2024006055A1 (en) * 2022-06-30 2024-01-04 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

Citations (4)

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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

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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
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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

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

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