WO2012161518A3 - ＲＯＲα의 활성자로서의 신규한 ｔｈｉｏｕｒｅａ 유도체 및 이를 함유하는 약학적 조성물 - Google Patents

ＲＯＲα의 활성자로서의 신규한 ｔｈｉｏｕｒｅａ 유도체 및 이를 함유하는 약학적 조성물 Download PDF

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Publication number
WO2012161518A3
WO2012161518A3 PCT/KR2012/004081 KR2012004081W WO2012161518A3 WO 2012161518 A3 WO2012161518 A3 WO 2012161518A3 KR 2012004081 W KR2012004081 W KR 2012004081W WO 2012161518 A3 WO2012161518 A3 WO 2012161518A3
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WO
WIPO (PCT)
Prior art keywords
rorα
activators
compound
novel
pharmaceutical composition
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Application number
PCT/KR2012/004081
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English (en)
French (fr)
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WO2012161518A2 (ko
Inventor
이미옥
박형근
김은진
손호영
정효준
홍석창
나태영
Original Assignee
서울대학교 산학협력단
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.)
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Publication date
Priority claimed from KR1020110128903A external-priority patent/KR20120130678A/ko
Application filed by 서울대학교 산학협력단 filed Critical 서울대학교 산학협력단
Priority to US15/759,588 priority Critical patent/US10407388B2/en
Publication of WO2012161518A2 publication Critical patent/WO2012161518A2/ko
Publication of WO2012161518A3 publication Critical patent/WO2012161518A3/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C335/00—Thioureas, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C335/04—Derivatives of thiourea
    • C07C335/06—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to acyclic carbon atoms
    • C07C335/10—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C335/12—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton the carbon skeleton containing six-membered aromatic 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
    • A61K31/13—Amines
    • A61K31/145—Amines having sulfur, e.g. thiurams (>N—C(S)—S—C(S)—N< and >N—C(S)—S—S—C(S)—N<), Sulfinylamines (—N=SO), Sulfonylamines (—N=SO2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

본 발명은 RORα 유전자를 활성화시키는 신규한 화합물 또는 그의 염에 관한 것이다. 구체적으로 본 발명은 thiazolidinedione의 하나인 CGP52608을 선도 물질로 하는 신규한 JC1 화합물 또는 이의 약제학적으로 허용가능한 염을 제공한다. 또한, 본 발명은 유효성분으로 상기 신규한 화합물을 포함하는 지질 축적 억제제를 제공한다. 본 발명은 대사성 질환 또는 염증성 질환 치료에 적용될 수 있을 것으로 기대된다.
PCT/KR2012/004081 2011-05-23 2012-05-23 ＲＯＲα의 활성자로서의 신규한 ｔｈｉｏｕｒｅａ 유도체 및 이를 함유하는 약학적 조성물 WO2012161518A2 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US15/759,588 US10407388B2 (en) 2011-05-23 2012-05-23 Thiourea derivatives as activators of RORα and pharmaceutical composition containing same

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
KR20110048455 2011-05-23
KR10-2011-0048455 2011-05-23
KR10-2011-0128903 2011-12-05
KR1020110128903A KR20120130678A (ko) 2011-05-23 2011-12-05 ＲＯＲα의 활성자로서의 신규한 ｔｈｉｏｕｒｅａ 유도체 및 이를 함유하는 약학적 조성물
KR1020120054540A KR101450960B1 (ko) 2011-05-23 2012-05-23 ＲＯＲα의 활성자로서의 신규한 ｔｈｉｏｕｒｅａ 유도체 및 이를 함유하는 약학적 조성물
KR10-2012-0054540 2012-05-23

Publications (2)

Publication Number Publication Date
WO2012161518A2 WO2012161518A2 (ko) 2012-11-29
WO2012161518A3 true WO2012161518A3 (ko) 2013-01-17

Family

ID=47217904

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2012/004081 WO2012161518A2 (ko) 2011-05-23 2012-05-23 ＲＯＲα의 활성자로서의 신규한 ｔｈｉｏｕｒｅａ 유도체 및 이를 함유하는 약학적 조성물

Country Status (3)

Country Link
US (1) US10407388B2 (ko)
KR (1) KR101450960B1 (ko)
WO (1) WO2012161518A2 (ko)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101581665B1 (ko) 2014-08-08 2015-12-31 주식회사 에이치엘앤피 피부질환 치료를 위한 광선치료기
KR20160132534A (ko) 2015-05-11 2016-11-21 경북대학교병원 ＲＯＲα 활성조절제를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
WO2017026830A1 (ko) * 2015-08-12 2017-02-16 서울대학교 산학협력단 티오우레아 유도체를 포함하는 자가면역질환 예방 또는 치료용 약학적 조성물
US10995066B1 (en) * 2019-11-26 2021-05-04 Therasid Bioscience Inc. Method for preparing novel crystalline forms of 1-(4-benzyloxy-benzyl)-3-methyl-thiourea
US11390582B2 (en) * 2019-11-26 2022-07-19 Therasid Bioscience Inc. Polymorphs of 1-(4-benzyloxy-benzyl)-3-methyl-thiourea
CN113181150A (zh) * 2021-04-29 2021-07-30 新乡医学院第二附属医院 Sr1078在制备治疗酒精性肝损伤药物方面的应用、药物组合物
WO2022245067A1 (ko) * 2021-05-17 2022-11-24 서울대학교 산학협력단 RORα의 활성자 JC1-40을 포함하는 근감소증 예방, 개선, 또는 치료를 위한 약학적 조성물
KR20230071841A (ko) 2021-11-15 2023-05-24 서울대학교산학협력단 RORα의 활성자로서의 신규한 티오우레아 유도체 및 이를 포함하는 약학적 조성물
KR102417640B1 (ko) * 2022-05-09 2022-07-06 (주)테라시드바이오사이언스 티오우레아 유도체를 포함하는 섬유화 질환의 예방 또는 치료용 조성물

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3090810A (en) * 1961-01-11 1963-05-21 Baxter Laboratories Inc Benzyl thioureas
US3949089A (en) * 1969-06-23 1976-04-06 Burroughs Wellcome Co. Substituted guanidine compounds as antifibrillatory agents
US3968243A (en) * 1970-06-05 1976-07-06 Burroughs Wellcome Co. Substituted guanidine compounds in the treating of arrythmias
US20020147365A1 (en) * 2000-05-10 2002-10-10 The Fanning Corporation 3-methoxybenzyl thiourea derivatives and improved lipid compositions containing same
US20080286231A1 (en) * 2007-04-18 2008-11-20 Probiodrug Ag Novel inhibitors of glutaminyl cyclase

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3090810A (en) * 1961-01-11 1963-05-21 Baxter Laboratories Inc Benzyl thioureas
US3949089A (en) * 1969-06-23 1976-04-06 Burroughs Wellcome Co. Substituted guanidine compounds as antifibrillatory agents
US3968243A (en) * 1970-06-05 1976-07-06 Burroughs Wellcome Co. Substituted guanidine compounds in the treating of arrythmias
US20020147365A1 (en) * 2000-05-10 2002-10-10 The Fanning Corporation 3-methoxybenzyl thiourea derivatives and improved lipid compositions containing same
US20080286231A1 (en) * 2007-04-18 2008-11-20 Probiodrug Ag Novel inhibitors of glutaminyl cyclase

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
HAN, HO GYU ET AL.: "Synthesis of 2-Benzylimino-1,3-thiazolines and Their Structure Determination", JOURNAL OF THE KOREAN CHEMICAL SOCIETY, vol. 45, 2001, pages 612 - 615 *
KIM, JEONGHAN ET AL.: "Liquid Crystalline Properties of Polyguanidines", MARCROMOLECULES, vol. 37, 2004, pages 8286 - 8292 *

Also Published As

Publication number Publication date
US20180265462A1 (en) 2018-09-20
US10407388B2 (en) 2019-09-10
WO2012161518A2 (ko) 2012-11-29
KR101450960B1 (ko) 2014-10-22
KR20120130733A (ko) 2012-12-03

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