CN109803648A - 可逆保护的硫醇化亲电脂肪酸作为前药 - Google Patents

可逆保护的硫醇化亲电脂肪酸作为前药 Download PDF

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Publication number
CN109803648A
CN109803648A CN201780062044.9A CN201780062044A CN109803648A CN 109803648 A CN109803648 A CN 109803648A CN 201780062044 A CN201780062044 A CN 201780062044A CN 109803648 A CN109803648 A CN 109803648A
Authority
CN
China
Prior art keywords
acid
fatty acid
carbon
thiolation
activation
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.)
Pending
Application number
CN201780062044.9A
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English (en)
Chinese (zh)
Inventor
布鲁斯·A·弗里曼
尼古拉斯·霍
弗朗西斯科·乔斯·朔普费尔
史蒂文·伍德科克
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.)
University of Pittsburgh
Original Assignee
University of Pittsburgh
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 University of Pittsburgh filed Critical University of Pittsburgh
Publication of CN109803648A publication Critical patent/CN109803648A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C205/00—Compounds containing nitro groups bound to a carbon skeleton
    • C07C205/01—Compounds containing nitro groups bound to a carbon skeleton having nitro groups bound to acyclic carbon atoms
    • C07C205/03—Compounds containing nitro groups bound to a carbon skeleton having nitro groups bound to acyclic carbon atoms of an unsaturated carbon skeleton

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201780062044.9A 2016-10-05 2017-10-04 可逆保护的硫醇化亲电脂肪酸作为前药 Pending CN109803648A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662404368P 2016-10-05 2016-10-05
US62/404,368 2016-10-05
PCT/US2017/055149 WO2018067705A1 (en) 2016-10-05 2017-10-04 Reversibly protected thiolated electrophilic fatty acids as prodrugs

Publications (1)

Publication Number Publication Date
CN109803648A true CN109803648A (zh) 2019-05-24

Family

ID=61832194

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780062044.9A Pending CN109803648A (zh) 2016-10-05 2017-10-04 可逆保护的硫醇化亲电脂肪酸作为前药

Country Status (7)

Country Link
US (3) US10744106B2 (https=)
EP (1) EP3522884B1 (https=)
JP (1) JP2019529501A (https=)
CN (1) CN109803648A (https=)
CA (1) CA3039376A1 (https=)
ES (1) ES2982757T3 (https=)
WO (1) WO2018067705A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10765652B2 (en) 2016-10-05 2020-09-08 University of Pittsburgh—of the Commonwealth System of Higher Education Reversible nitroxide derivatives of nitroalkenes that mediate nitrosating and alkylating reactions
US12390435B2 (en) 2018-11-14 2025-08-19 University of Pittsburgh—of the Commonwealth System of Higher Education Electrophiles and electrophile pro-drugs as RAD51 inhibitors
WO2021242758A1 (en) * 2020-05-26 2021-12-02 Imara Inc. Improved nitro-fatty acid oral dose regimens
CN118845745B (zh) * 2024-09-25 2024-12-17 浙江大学医学院附属第二医院 辛酸钠在制备治疗脓毒症药物中的应用

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009017802A1 (en) 2007-08-01 2009-02-05 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Nitro-fattyacid modulation of type ii diabetes
WO2010014889A2 (en) 2008-08-01 2010-02-04 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Nitro fatty acids as regiomers and related mimetics
EP3045167A1 (en) 2009-07-31 2016-07-20 University of Pittsburgh - Of the Commonwealth System of Higher Education Keto fatty acids as anti-inflammatory agents
WO2013116753A1 (en) 2012-02-03 2013-08-08 University Of Pittsburgh-Of The Commonwelth System Of Higher Education Fatty acids as anti-inflammatory agents
CA3016180A1 (en) 2016-03-04 2017-09-08 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Prevention, treatment and reversal of disease using therapeutically effective amounts of dicarboxylic acid compounds
US10765652B2 (en) 2016-10-05 2020-09-08 University of Pittsburgh—of the Commonwealth System of Higher Education Reversible nitroxide derivatives of nitroalkenes that mediate nitrosating and alkylating reactions

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
LAURA M. S. BAKER 等: "Nitro-fatty Acid Reaction with Glutathione and Cysteine: KINETIC ANALYSIS OF THIOL ALKYLATION BY A MICHAEL ADDITION REACTION", 《J BIOL CHEM.》 *
MOTOHIRO NISHIDA 等: "Hydrogen sulfide anion regulates redox signaling via electrophile sulfhydration", 《NAT CHEM BIOL.》 *
SONIA R. SALVATORE 等: "Characterization and quantification of endogenous fatty acid nitroalkene metabolites in human urine", 《JOURNAL OF LIPID RESEARCH》 *

Also Published As

Publication number Publication date
US20200352890A1 (en) 2020-11-12
EP3522884A4 (en) 2020-05-27
JP2019529501A (ja) 2019-10-17
EP3522884A1 (en) 2019-08-14
US20230321022A1 (en) 2023-10-12
CA3039376A1 (en) 2018-04-12
EP3522884C0 (en) 2024-05-29
ES2982757T3 (es) 2024-10-17
US20190282527A1 (en) 2019-09-19
WO2018067705A1 (en) 2018-04-12
EP3522884B1 (en) 2024-05-29
US10744106B2 (en) 2020-08-18

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Application publication date: 20190524