KR101722289B1 - 피부과 질환 또는 증상의 치료에 유용한 ｔｏｆａ 유사체 - Google Patents

피부과 질환 또는 증상의 치료에 유용한 ｔｏｆａ 유사체 Download PDF

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KR101722289B1
KR101722289B1 KR1020127001491A KR20127001491A KR101722289B1 KR 101722289 B1 KR101722289 B1 KR 101722289B1 KR 1020127001491 A KR1020127001491 A KR 1020127001491A KR 20127001491 A KR20127001491 A KR 20127001491A KR 101722289 B1 KR101722289 B1 KR 101722289B1
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tetradecyloxy
furan
carboxylate
compound
alkyl
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KR20120047234A (ko
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티모띠 스캇 다이날드
지오프레이 씨. 윈터스
데이비드 더블유.씨. 헌트
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데르미라 (캐나다), 인코포레이티드
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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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • 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
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • 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
    • A61K31/365—Lactones
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/08—Antiseborrheics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or 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
    • C07D307/58—One oxygen atom, e.g. butenolide
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or 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
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Furan Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020127001491A 2009-07-08 2010-07-01 피부과 질환 또는 증상의 치료에 유용한 ｔｏｆａ 유사체 Expired - Fee Related KR101722289B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22404209P 2009-07-08 2009-07-08
US61/224,042 2009-07-08
PCT/US2010/040795 WO2011005660A1 (en) 2009-07-08 2010-07-01 Tofa analogs useful in treating dermatological disorders or conditions

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KR20120047234A KR20120047234A (ko) 2012-05-11
KR101722289B1 true KR101722289B1 (ko) 2017-03-31

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US (3) US8884034B2 (enExample)
EP (2) EP2451796B1 (enExample)
JP (1) JP5753844B2 (enExample)
KR (1) KR101722289B1 (enExample)
CN (2) CN102482249B (enExample)
AU (1) AU2010270797B2 (enExample)
BR (1) BR112012000254A2 (enExample)
CA (1) CA2766643C (enExample)
DK (1) DK2451796T3 (enExample)
ES (2) ES2540232T3 (enExample)
IL (1) IL217421A0 (enExample)
MX (1) MX2012000435A (enExample)
NZ (1) NZ597375A (enExample)
RU (1) RU2561729C2 (enExample)
SG (1) SG176983A1 (enExample)
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CN107406400B (zh) 2015-02-05 2020-08-04 德米拉公司 用于制备(5-十四烷氧基)呋喃-2-甲酸2-((2-乙氧基-2-氧代乙基)(甲基)氨基)-2-氧代乙酯的合成方法
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US11129818B2 (en) 2017-06-07 2021-09-28 Arcutis Biotherapeutics, Inc. Topical roflumilast formulation having improved delivery and plasma half life
US9895359B1 (en) 2017-06-07 2018-02-20 Arcutis, Inc. Inhibition of crystal growth of roflumilast
US12011437B1 (en) 2017-06-07 2024-06-18 Arcutis Biotherapeutics, Inc. Roflumilast formulations with an improved pharmacokinetic profile
US20210161870A1 (en) 2017-06-07 2021-06-03 Arcutis Biotherapeutics, Inc. Roflumilast formulations with an improved pharmacokinetic profile
CN110799187B (zh) 2017-06-30 2023-10-03 汇科锦公司 螺内酯化合物
WO2019072478A1 (en) 2017-10-10 2019-04-18 Galderma Research & Development SPECIFIC ACETYL-COA CARBOXYLASE INHIBITORS FOR USE IN THE TREATMENT AND / OR PREVENTION OF ACNE
JP6950524B2 (ja) * 2017-12-28 2021-10-13 トヨタ自動車株式会社 ハイブリッド車両の制御装置
EP3801461A2 (en) 2018-06-04 2021-04-14 Arcutis, Inc. Method and formulation for improving roflumilast skin penetration lag time
RU2678307C1 (ru) * 2018-11-13 2019-01-25 Индивидуальный предприниматель Талагаева Елена Владимировна Активная против акне добавка к парфюмерно-косметическим продуктам
CN109608415B (zh) * 2019-01-21 2020-12-01 暨南大学 噻唑甲酰胺类化合物及其合成和应用
US20200330429A1 (en) * 2019-04-22 2020-10-22 Nestlé Skin Health Sa Method of treating truncal acne with trifarotene
WO2021226370A1 (en) * 2020-05-07 2021-11-11 Arcutis Biotherapeutics, Inc. Treatment of skin conditions using high krafft temperature anionic surfactants
US11707454B2 (en) 2020-12-04 2023-07-25 Arcutis Biotherapeutics, Inc. Topical roflumilast formulation having antifungal properties
CN114767665B (zh) * 2021-06-11 2023-10-10 同济大学 5-十四烷氧基-2-呋喃甲酸在制备用于治疗银屑病样皮炎的药物中的用途
CN117881649A (zh) * 2021-07-02 2024-04-12 安基生技新药股份有限公司 二甲基姜黄素的外用调配物
DE102022201276A1 (de) 2022-02-08 2023-08-10 Beiersdorf Aktiengesellschaft Neue TOFA-Analoga, Zubereitungen zur Sebumreduktion mit einem Gehalt an solchen Analoga und die kosmetische und/oder therapeutische Verwendung solcher Analoga als wirksames Prinzip zur Sebumreduktion oder -verhinderung
DE102022201277A1 (de) 2022-02-08 2023-08-10 Beiersdorf Aktiengesellschaft Neue TOFA-Analoga, Zubereitungen zur Sebumreduktion mit einem Gehalt an solchen Analoga und die kosmetische und/oder therapeutische Verwendung solcher Analoga als wirksames Prinzip zur Sebumreduktion oder -verhinderung
WO2024058848A1 (en) 2022-09-15 2024-03-21 Arcutis Biotherapeutics, Inc. Pharmaceutical compositions of roflumilast and solvents capable of dissolving high amounts of the drug
WO2025160513A1 (en) * 2024-01-26 2025-07-31 Rerx Therapeutics, Inc. Crystalline forms of 5-(tetradecyloxy)furan-2-carboxylic acid and salts thereof
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JP2012532871A (ja) 2012-12-20
EP2451796B1 (en) 2013-04-17
US8884034B2 (en) 2014-11-11
IL217421A0 (en) 2012-02-29
RU2012104244A (ru) 2013-09-27
CN105017187A (zh) 2015-11-04
KR20120047234A (ko) 2012-05-11
ES2421723T3 (es) 2013-09-05
AU2010270797A1 (en) 2012-02-02
BR112012000254A2 (pt) 2016-02-16
US20120208807A1 (en) 2012-08-16
EP2451796A1 (en) 2012-05-16
EP2641906B1 (en) 2015-04-22
RU2561729C2 (ru) 2015-09-10
CA2766643C (en) 2017-01-03
AU2010270797B2 (en) 2015-03-19
SG176983A1 (en) 2012-02-28
HK1189886A1 (en) 2014-06-20
US9782382B2 (en) 2017-10-10
CN102482249B (zh) 2016-06-08

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