KR101889290B1 - 레티노이드 수용체-선택적 경로와 관련된 방법 및 조성물 - Google Patents

레티노이드 수용체-선택적 경로와 관련된 방법 및 조성물 Download PDF

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KR101889290B1
KR101889290B1 KR1020127031894A KR20127031894A KR101889290B1 KR 101889290 B1 KR101889290 B1 KR 101889290B1 KR 1020127031894 A KR1020127031894 A KR 1020127031894A KR 20127031894 A KR20127031894 A KR 20127031894A KR 101889290 B1 KR101889290 B1 KR 101889290B1
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sulindac
cells
rxrα
delete delete
alpha
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KR20130113932A (ko
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시아오-쿤 장
잉 수
후 조우
웬 리우
페이-치앙 후앙
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샌포드 번햄 프레비즈 메디컬 디스커버리 인스티튜트
시아먼 유니버시티
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
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    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
    • C07D295/112—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • A—HUMAN NECESSITIES
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    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
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KR1020127031894A 2010-05-06 2011-05-06 레티노이드 수용체-선택적 경로와 관련된 방법 및 조성물 Expired - Fee Related KR101889290B1 (ko)

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US33212410P 2010-05-06 2010-05-06
US61/332,124 2010-05-06
PCT/US2011/035651 WO2011140525A2 (en) 2010-05-06 2011-05-06 Methods and compositions related to a retinoid receptor-selective pathway

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US (2) US9611235B2 (https=)
EP (1) EP2571497B1 (https=)
JP (2) JP2013533212A (https=)
KR (1) KR101889290B1 (https=)
CN (2) CN107050007B (https=)
AU (1) AU2011249857B2 (https=)
CA (1) CA2798692C (https=)
ES (1) ES2702532T3 (https=)
WO (1) WO2011140525A2 (https=)

Families Citing this family (7)

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JP2013533212A (ja) 2010-05-06 2013-08-22 サンフォード−バーナム メディカル リサーチ インスティテュート レチノイド受容体に選択的な経路に関する方法および組成物
JP2014517813A (ja) * 2011-04-01 2014-07-24 サザン リサーチ インスティテュート スリンダク誘導体、その使用及びその調製
WO2015100267A1 (en) * 2013-12-23 2015-07-02 Sanford-Burnham Medical Research Institute Methods and compositions for treating cancer
WO2017193086A1 (en) * 2016-05-06 2017-11-09 Tarrex Biopharma Inc. Therapeutic compounds and methods
US20230234909A1 (en) * 2020-06-12 2023-07-27 Nucmito Pharmaceuticals Co. Ltd. Indene compounds, pharmaceutical compositions thereof, and their therapeutic applications
CN117916215A (zh) * 2021-05-15 2024-04-19 藤济(厦门)生物医药科技有限公司 茚化合物、其药物组合物及其治疗应用
CN120513226A (zh) * 2022-11-16 2025-08-19 藤济(厦门)生物医药科技有限公司 茚化合物、其药物组合物及其治疗应用

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005247807A (ja) * 2004-03-08 2005-09-15 Japan Science & Technology Agency Ｎｓａｉｄを利用した癌治療用組成物

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU6909000A (en) 1999-08-16 2001-03-13 Johns Hopkins University, The Ppardelta links apc to chemopreventive drugs
DE10163426A1 (de) 2001-12-21 2003-07-03 Max Planck Gesellschaft Pharmakologisch wirksame Inden-Derivate
AU2003298020A1 (en) * 2002-11-26 2004-06-18 Florida Atlantic University Catalytic antioxidants and methods of use
WO2005037189A2 (en) 2003-08-13 2005-04-28 The Burnham Institute Cytoplasmic activity of retinoid x receptor and its regulation by ligands and dimerization
EP1865972B1 (en) 2005-03-23 2013-11-06 CHS Pharma, Inc. Treatment or prevention of cancer and precancerous disorders
AU2007205208B2 (en) * 2006-01-04 2012-11-01 Southern Research Institute Derivatives of sulindac, use thereof and preparation thereof
WO2010070379A1 (en) 2008-12-17 2010-06-24 Centre National De La Recherche Scientifique Rxr-ppargamma agonist/growth factor inhibitor combination therapy for inducing apoptosis and the treatment of cancer
JP2013533212A (ja) 2010-05-06 2013-08-22 サンフォード−バーナム メディカル リサーチ インスティテュート レチノイド受容体に選択的な経路に関する方法および組成物
CN102030642A (zh) 2010-12-03 2011-04-27 厦门大学 舒林酸类似物的中间体的合成方法与应用
WO2015100267A1 (en) 2013-12-23 2015-07-02 Sanford-Burnham Medical Research Institute Methods and compositions for treating cancer
WO2017193086A1 (en) 2016-05-06 2017-11-09 Tarrex Biopharma Inc. Therapeutic compounds and methods

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005247807A (ja) * 2004-03-08 2005-09-15 Japan Science & Technology Agency Ｎｓａｉｄを利用した癌治療用組成物

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Biochimica et Biophysica Acta, 1999, vol. 1428, pp. 68~76*
Bioorganic & Medicinal Chemistry Letters, 2009, vol. 19, pp. 3271~3274*
Journal of Medicinal Chemistry, 2008, vol. 51, No. 16, pp. 4911~4919*

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CA2798692A1 (en) 2011-11-10
CA2798692C (en) 2019-04-30
ES2702532T3 (es) 2019-03-01
EP2571497B1 (en) 2018-09-19
EP2571497A2 (en) 2013-03-27
WO2011140525A2 (en) 2011-11-10
KR20130113932A (ko) 2013-10-16
US20170313668A1 (en) 2017-11-02
CN107050007B (zh) 2020-06-30
CN103002887B (zh) 2016-12-21
US10087156B2 (en) 2018-10-02
AU2011249857A1 (en) 2012-12-06
JP2013533212A (ja) 2013-08-22
US20150266842A1 (en) 2015-09-24
AU2011249857B2 (en) 2015-03-12
JP2017008050A (ja) 2017-01-12
CN107050007A (zh) 2017-08-18
JP6375340B2 (ja) 2018-08-15
CN103002887A (zh) 2013-03-27
WO2011140525A3 (en) 2012-03-22
EP2571497A4 (en) 2013-12-04

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