TWI491392B - 減少較小,稠密低密度脂蛋白(ldl)粒子之方法 - Google Patents

減少較小,稠密低密度脂蛋白(ldl)粒子之方法 Download PDF

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Publication number
TWI491392B
TWI491392B TW098135183A TW98135183A TWI491392B TW I491392 B TWI491392 B TW I491392B TW 098135183 A TW098135183 A TW 098135183A TW 98135183 A TW98135183 A TW 98135183A TW I491392 B TWI491392 B TW I491392B
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TW
Taiwan
Prior art keywords
ldl
human
mode
compound
particle size
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TW098135183A
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English (en)
Chinese (zh)
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TW201028141A (en
Inventor
David B Karpf
Ronald M Krauss
Yun-Jung Choi
Xueyan Wang
Francine M Gregoire
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Cymabay Therapeutics Inc
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Publication of TW201028141A publication Critical patent/TW201028141A/zh
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Publication of TWI491392B publication Critical patent/TWI491392B/zh

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    • 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
    • A61K31/02Halogenated hydrocarbons
    • A61K31/025Halogenated hydrocarbons carbocyclic
    • A61K31/03Halogenated hydrocarbons carbocyclic aromatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/075Ethers or acetals
    • A61K31/085Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
    • A61K31/09Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/12Ketones
    • 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
    • A61K31/4015Heterocyclic 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 having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00Preparations for use in therapy

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  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
TW098135183A 2008-10-17 2009-10-16 減少較小,稠密低密度脂蛋白(ldl)粒子之方法 TWI491392B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US10648308P 2008-10-17 2008-10-17

Publications (2)

Publication Number Publication Date
TW201028141A TW201028141A (en) 2010-08-01
TWI491392B true TWI491392B (zh) 2015-07-11

Family

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Family Applications (1)

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TW098135183A TWI491392B (zh) 2008-10-17 2009-10-16 減少較小,稠密低密度脂蛋白(ldl)粒子之方法

Country Status (11)

Country Link
US (3) US20100152295A1 (enExample)
EP (1) EP2346498B1 (enExample)
JP (1) JP5694941B2 (enExample)
KR (1) KR20110091680A (enExample)
CN (1) CN102209532B (enExample)
BR (1) BRPI0920170A2 (enExample)
CA (1) CA2740874C (enExample)
ES (1) ES2712052T3 (enExample)
MX (1) MX2011004077A (enExample)
TW (1) TWI491392B (enExample)
WO (1) WO2010045361A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130273154A1 (en) * 2011-03-02 2013-10-17 Joseph M. Fayad Oral formulations Mimetic of Roux-en-Y gastric bypass actions on the ileal brake; Compositions, Methods of Treatment, Diagnostics and Systems for treatment of metabolic syndrome manifestations including insulin resistance, fatty liver disease, hpperlipidemia, and type 2 diabetes
CN110152000A (zh) 2011-03-02 2019-08-23 J·深塔格 用于单独治疗肝脂肪变性或治疗伴有丙型肝炎病毒感染的肝脂肪变性的组合物
CN105764498A (zh) 2013-11-20 2016-07-13 西玛贝医药公司 纯合家族型高胆固醇血症的治疗
SI3119384T1 (sl) 2014-03-20 2018-12-31 Cymabay Therapeutics, Inc. Zdravljenje intrahepatičnih holestatičnih bolezni
US10272058B2 (en) 2014-03-20 2019-04-30 Cymabay Therapeutics, Inc. Treatment of intrahepatic cholestatic diseases
HRP20192299T1 (hr) 2014-04-11 2020-03-06 Cymabay Therapeutics, Inc. Liječenje nafld i nash
MY192385A (en) * 2016-10-05 2022-08-18 Mitobridge Inc Methods of treating acute kidney injury
US10512622B2 (en) 2017-07-14 2019-12-24 Cymabay Therapeutics, Inc. Treatment of intrahepatic cholestatic diseases

Citations (1)

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US20060058393A1 (en) * 2004-09-15 2006-03-16 Deangelis Alan 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs

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ES494769A0 (es) 1979-09-05 1981-07-16 Glaxo Group Ltd Un procedimiento para la pre-paracion de fenoxialcoxifenil- derivados.
AU1856997A (en) 1996-02-02 1997-08-22 Merck & Co., Inc. Method for raising hdl cholesterol levels
US7576131B2 (en) 1999-06-04 2009-08-18 Metabolex, Inc. Use of (-) (3-trihalomethylphenoxy) (4-halophenyl) acetic acid derivatives for treatment of insulin resistance, type 2 diabetes, hyperlipidemia and hyperuricemia
GB9914977D0 (en) 1999-06-25 1999-08-25 Glaxo Group Ltd Chemical compounds
JP2001354671A (ja) 2000-04-14 2001-12-25 Nippon Chemiphar Co Ltd ペルオキシソーム増殖剤応答性受容体δの活性化剤
ATE542805T1 (de) 2000-08-11 2012-02-15 Nippon Chemiphar Co Ppar-delta aktivatoren
WO2002046154A1 (fr) 2000-12-05 2002-06-13 Nippon Chemiphar Co., Ltd. Activateurs $g(d) de recepteur active par un proliferateur du peroxysome
GB0031109D0 (en) 2000-12-20 2001-01-31 Glaxo Group Ltd Chemical compounds
EP1399151A4 (en) 2001-06-11 2004-08-04 Merck & Co Inc METHOD FOR TREATING INFLAMMABLE DISEASES BY ADMINISTRATING A PPAR DELTA AGONIST
GB0121436D0 (en) * 2001-09-04 2001-10-24 Pfizer Ltd Biomodulated multiparticulate formulations
CA2521175A1 (en) * 2003-04-07 2004-10-28 Kalypsys, Inc. Para-sulfonyl substituted phenyl compounds as modulators of ppars
JPWO2004093910A1 (ja) 2003-04-22 2006-07-13 アステラス製薬株式会社 PPARδアゴニストによる脳神経変性疾患治療剤
US7199259B2 (en) 2003-06-20 2007-04-03 Metabolex, Inc. Resolution of α-(phenoxy)phenylacetic acid derivatives
ATE542793T1 (de) * 2003-09-19 2012-02-15 Janssen Pharmaceutica Nv 4-((phenoxyalkyl)thio)-phenoxyessigsäuren und analoga
JP2008500358A (ja) * 2004-05-25 2008-01-10 メタボレックス インコーポレーティッド Pparのモジュレーターとしての、二環式の置換されたトリアゾール、およびこれらの調製方法
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JO3006B1 (ar) * 2005-09-14 2016-09-05 Janssen Pharmaceutica Nv املاح ليسين مبتكرة من مشتقات حامض 4-((فينوكسي الكيل)ثيو) فينوكسي الخليك
SI3119384T1 (sl) * 2014-03-20 2018-12-31 Cymabay Therapeutics, Inc. Zdravljenje intrahepatičnih holestatičnih bolezni
HRP20192299T1 (hr) * 2014-04-11 2020-03-06 Cymabay Therapeutics, Inc. Liječenje nafld i nash

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US20060058393A1 (en) * 2004-09-15 2006-03-16 Deangelis Alan 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Oliver W R et al: "A Selective peroxisome proliferator-activated receptorδagonist promotes reverse cholesterol transport", Proceedings of the National Academy of Sciences, 2001, vol. 98, no. 9, pages 5306-5311 *
Zhang et al: "Discovery of para-alkylthiophenoxyacetic acids as a novel series of potent and selective PPARδ agonists", Bioorganic & Medicinal Chemistry Letters, 2007, vol. 17, no. 14, pages 3855~3859 *

Also Published As

Publication number Publication date
US20160324811A1 (en) 2016-11-10
WO2010045361A1 (en) 2010-04-22
KR20110091680A (ko) 2011-08-12
US20100152295A1 (en) 2010-06-17
JP2012505905A (ja) 2012-03-08
MX2011004077A (es) 2011-08-17
CA2740874A1 (en) 2010-04-22
BRPI0920170A2 (pt) 2016-06-21
TW201028141A (en) 2010-08-01
US11007162B2 (en) 2021-05-18
CA2740874C (en) 2018-02-27
US20190298672A1 (en) 2019-10-03
EP2346498A1 (en) 2011-07-27
EP2346498B1 (en) 2018-12-26
EP2346498A4 (en) 2012-08-01
CN102209532B (zh) 2015-07-22
ES2712052T3 (es) 2019-05-09
JP5694941B2 (ja) 2015-04-01
CN102209532A (zh) 2011-10-05

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