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

레티노이드 수용체-선택적 경로와 관련된 방법 및 조성물 Download PDF

Info

Publication number
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
Authority
KR
South Korea
Prior art keywords
sulindac
cells
rxrα
delete delete
alpha
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.)
Expired - Fee Related
Application number
KR1020127031894A
Other languages
English (en)
Korean (ko)
Other versions
KR20130113932A (ko
Inventor
시아오-쿤 장
잉 수
후 조우
웬 리우
페이-치앙 후앙
Original Assignee
샌포드 번햄 프레비즈 메디컬 디스커버리 인스티튜트
시아먼 유니버시티
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 샌포드 번햄 프레비즈 메디컬 디스커버리 인스티튜트, 시아먼 유니버시티 filed Critical 샌포드 번햄 프레비즈 메디컬 디스커버리 인스티튜트
Publication of KR20130113932A publication Critical patent/KR20130113932A/ko
Application granted granted Critical
Publication of KR101889290B1 publication Critical patent/KR101889290B1/ko
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/192Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/01Hydrocarbons
    • A61K31/015Hydrocarbons carbocyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/10Heterocyclic 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
    • C07D295/112Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196Carboxylic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/275Nitriles; Isonitriles
    • A61K31/277Nitriles; Isonitriles having a ring, e.g. verapamil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/4021-aryl substituted, e.g. piretanide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4402Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
    • A61K38/191Tumor necrosis factors [TNF], e.g. lymphotoxin [LT], i.e. TNF-beta
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/57Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/52Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing halogen
    • C07C57/62Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing halogen containing six-membered aromatic rings and other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40Unsaturated compounds
    • C07C59/58Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/72Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings and other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/55Acids; Esters
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5011Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing antineoplastic activity
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/70567Nuclear receptors, e.g. retinoic acid receptor [RAR], RXR, nuclear orphan receptors
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2510/00Detection of programmed cell death, i.e. apoptosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Zoology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Toxicology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
KR1020127031894A 2010-05-06 2011-05-06 레티노이드 수용체-선택적 경로와 관련된 방법 및 조성물 Expired - Fee Related KR101889290B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
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

Publications (2)

Publication Number Publication Date
KR20130113932A KR20130113932A (ko) 2013-10-16
KR101889290B1 true KR101889290B1 (ko) 2018-08-20

Family

ID=44904518

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020127031894A Expired - Fee Related KR101889290B1 (ko) 2010-05-06 2011-05-06 레티노이드 수용체-선택적 경로와 관련된 방법 및 조성물

Country Status (9)

Country Link
US (2) US9611235B2 (enExample)
EP (1) EP2571497B1 (enExample)
JP (2) JP2013533212A (enExample)
KR (1) KR101889290B1 (enExample)
CN (2) CN103002887B (enExample)
AU (1) AU2011249857B2 (enExample)
CA (1) CA2798692C (enExample)
ES (1) ES2702532T3 (enExample)
WO (1) WO2011140525A2 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9611235B2 (en) 2010-05-06 2017-04-04 Sanford-Burnham Medical Research Institute Methods and compositions related to a retinoid receptor-selective pathway
CN103491772A (zh) * 2011-04-01 2014-01-01 南方研究所 舒林酸衍生物、其用途及其制备
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
KR20230024976A (ko) * 2020-06-12 2023-02-21 누크미토 파마슈티컬스 컴퍼니, 리미티드 인덴 화합물, 이의 약제학적 조성물, 및 이의 치료학적 적용
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
EP4619369A1 (en) * 2022-11-16 2025-09-24 Nucmito Pharmaceuticals Co., Ltd. Indene compounds, pharmaceutical compositions thereof, and their therapeutic applications

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
WO2001012858A1 (en) 1999-08-16 2001-02-22 The Johns Hopkins University PPARδ 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
EP1668362A4 (en) 2003-08-13 2007-07-04 Burnham Inst CYTOPLASMATIC ACTIVITY OF THE RETINOID-X RECEPTOR AND ITS REGULATION BY LIGANDING AND DIMERIZATION
WO2006102439A2 (en) * 2005-03-23 2006-09-28 Florida Atlantic University Treatment or prevention of cancer and precancerous disorders
JP5337491B2 (ja) * 2006-01-04 2013-11-06 サザン リサーチ インスティテュート スリンダクの誘導体類、その使用及びその調製
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
US9611235B2 (en) 2010-05-06 2017-04-04 Sanford-Burnham Medical Research Institute Methods and compositions related to a retinoid receptor-selective pathway
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*

Also Published As

Publication number Publication date
CA2798692C (en) 2019-04-30
WO2011140525A2 (en) 2011-11-10
CA2798692A1 (en) 2011-11-10
CN107050007B (zh) 2020-06-30
US9611235B2 (en) 2017-04-04
KR20130113932A (ko) 2013-10-16
US20150266842A1 (en) 2015-09-24
EP2571497A2 (en) 2013-03-27
EP2571497A4 (en) 2013-12-04
JP2017008050A (ja) 2017-01-12
WO2011140525A3 (en) 2012-03-22
US10087156B2 (en) 2018-10-02
US20170313668A1 (en) 2017-11-02
AU2011249857B2 (en) 2015-03-12
AU2011249857A1 (en) 2012-12-06
JP6375340B2 (ja) 2018-08-15
CN103002887B (zh) 2016-12-21
CN107050007A (zh) 2017-08-18
CN103002887A (zh) 2013-03-27
EP2571497B1 (en) 2018-09-19
ES2702532T3 (es) 2019-03-01
JP2013533212A (ja) 2013-08-22

Similar Documents

Publication Publication Date Title
US10087156B2 (en) Methods and compositions related to retinoid receptor-selective pathway
Liu et al. A unique pharmacophore for activation of the nuclear orphan receptor Nur77 in vivo and in vitro
Kumbhare et al. Synthesis and biological evaluation of novel Mannich bases of 2-arylimidazo [2, 1-b] benzothiazoles as potential anti-cancer agents
Li et al. Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities
Xu et al. Structure–activity relationship study enables the discovery of a novel berberine analogue as the RXRα activator to inhibit colon cancer
Chen et al. Bt354 as a new STAT3 signaling pathway inhibitor against triple negative breast cancer
Zhang et al. Targeting truncated RXRα for cancer therapy
Festuccia et al. Trifluoroibuprofen inhibits α-methylacyl coenzyme A racemase (AMACR/P504S), reduces cancer cell proliferation and inhibits in vivo tumor growth in aggressive prostate cancer models
Kamal et al. Quinazolino linked 4β-amidopodophyllotoxin conjugates regulate angiogenic pathway and control breast cancer cell proliferation
Chen et al. A COX-2 inhibitor nimesulide analog selectively induces apoptosis in Her2 overexpressing breast cancer cells via cytochrome c dependent mechanisms
Deng et al. Identification of novel dual-target estrogen receptor α degraders with tubulin inhibitory activity for the treatment of endocrine-resistant breast cancer
Liu et al. Disrupting CCT-β: β-tubulin selectively kills CCT-β overexpressed cancer cells through MAPKs activation
Qin et al. Discovery of 5-(Pyrimidin-2-ylamino)-1 H-indole-2-carboxamide Derivatives as Nur77 Modulators with Selective and Potent Activity Against Triple-Negative Breast Cancer
US20030236294A1 (en) Compounds and methods for inducing apoptosis in proliferating cells
Watanabe et al. Discovery of a “gatekeeper” antagonist that blocks entry pathway to retinoid X receptors (RXRs) without allosteric ligand inhibition in permissive RXR heterodimers
Zhu et al. Discovery of Novel 5-Cyano-3-phenylindole-Based LSD1/HDAC Dual Inhibitors for Colorectal Cancer Treatment
Wu et al. Green synthesis and anti-tumor efficacy via inducing pyroptosis of novel 1H-benzo [e] indole-2 (3H)-one spirocyclic derivatives
Xia et al. Analogues of orphan nuclear receptor small heterodimer partner ligand and apoptosis inducer (E)-4-[3-(1-adamantyl)-4-hydroxyphenyl]-3-chlorocinnamic acid. 2. Impact of 3-chloro group replacement on inhibition of proliferation and induction of apoptosis of leukemia and cancer cell lines
Wang et al. Discovery of atorvastatin as a tetramer stabilizer of nuclear receptor RXRα through structure-based virtual screening
WO2019167973A1 (en) Cell cycle progression inhibitor
Xia et al. Heteroatom-substituted analogues of orphan nuclear receptor small heterodimer partner ligand and apoptosis inducer (E)-4-[3-(1-Adamantyl)-4-hydroxyphenyl]-3-chlorocinnamic acid
Mügge et al. Aspirin metabolite sodium salicylate selectively inhibits transcriptional activity of ATF6α and downstream target genes
Varlı et al. Development and synthesis of diffractaic acid analogs as potent inhibitors of colorectal cancer stem cell traits
Dawson et al. HETERODIMER PARTNER (SHP)
Dawson et al. Use of Retinoid Receptor Ligands to Identify Other Nuclear Receptor Ligands: Retinoid‐Related Molecules are Ligands for the Small Heterodimer Partner (SHP)“Orphan” Receptor

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

AMND Amendment
P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

A201 Request for examination
PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

AMND Amendment
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PN2301 Change of applicant

St.27 status event code: A-3-3-R10-R13-asn-PN2301

St.27 status event code: A-3-3-R10-R11-asn-PN2301

E90F Notification of reason for final refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

AMND Amendment
P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

E601 Decision to refuse application
E801 Decision on dismissal of amendment
PE0601 Decision on rejection of patent

St.27 status event code: N-2-6-B10-B15-exm-PE0601

PE0801 Dismissal of amendment

St.27 status event code: A-2-2-P10-P12-nap-PE0801

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PX0901 Re-examination

St.27 status event code: A-2-3-E10-E12-rex-PX0901

PX0701 Decision of registration after re-examination

St.27 status event code: A-3-4-F10-F13-rex-PX0701

PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20210811

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20210811