CY1112622T1 - Παραγωγα υποκατεστημενου αρυλαλκανοϊκου οξεος ως αγωνιστες ppar pan με ισχυρη αντιυπεργλυκαιμικη και αντιυπερλιπιδαιμικη δραστικοτητα - Google Patents

Παραγωγα υποκατεστημενου αρυλαλκανοϊκου οξεος ως αγωνιστες ppar pan με ισχυρη αντιυπεργλυκαιμικη και αντιυπερλιπιδαιμικη δραστικοτητα

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Publication number
CY1112622T1
CY1112622T1 CY20121100349T CY121100349T CY1112622T1 CY 1112622 T1 CY1112622 T1 CY 1112622T1 CY 20121100349 T CY20121100349 T CY 20121100349T CY 121100349 T CY121100349 T CY 121100349T CY 1112622 T1 CY1112622 T1 CY 1112622T1
Authority
CY
Cyprus
Prior art keywords
antipyretic
ppar
acid derivatives
arylalkanoic acid
potent
Prior art date
Application number
CY20121100349T
Other languages
English (en)
Inventor
Xian-Ping Lu
Zhibin Li
Chenzhong Liao
Leming Shi
Zhende Liu
Baoshun Ma
Zhiqiang Ning
Song Shan
Tuo Deng
Original Assignee
Shenzhen Chipscreen Biosciences Ltd.
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 Shenzhen Chipscreen Biosciences Ltd. filed Critical Shenzhen Chipscreen Biosciences Ltd.
Publication of CY1112622T1 publication Critical patent/CY1112622T1/el

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • 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
    • 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
    • A61K31/403—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 condensed with carbocyclic rings, e.g. carbazole
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/86—Carbazoles; Hydrogenated carbazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/24—Heterocyclic 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
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/46—Oxygen atoms
    • C07D213/50—Ketonic radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Αποκαλυπτόμενη είναι η παρασκευή και η φαρμακευτική χρήση παραγώγων υποκατεστημένου αρυλαλκανοϊκού οξέος του Τύπου Ι, όπου ο δακτύλιος Α, ο δακτύλιος Β, R1, R2, R3, R4, R5, Χ, Αlk1, Αlk2, Αr1 και Αr2 είναι όπως ορίζεται στην προδιαγραφή. Αυτές οι ενώσεις, ως εκλεκτικοί αγωνιστές που ενεργοποιούν τους ενεργοποιημένους από πολλαπλασιαστή περοξισώματος υποδοχείς (ΡΡΑR), ιδιαιτέρως τα ετεροδιμερή ΡΧR/ΡΡΑRάλφα, ΡΧR/ΡΡΑRγάμμα και ΡΧR/ΡΡΑRδέλτα είναι χρήσιμα στη θεραπεία και πρόληψη διαβήτη τύπου 2 και συναφούς μεταβολικού συνδρόμου όπως υπέρτασης, παχυσαρκίας, αντοχής ινσουλίνης, υπερλιπιδαιμίας, υπεργλυκαιμίας, υπερχοληστερολαιμίας, αθηροσκλήρωσης, νόσου της στεφανιαίας αρτηρίας και άλλων καρδιαγγειακών διαταραχών, με βελτιωμένο προφίλ παρενεργειών που κοινώς συνδυάζεται με τους συνηθισμένους αγωνιστές ΡΡΑRγάμμα.
CY20121100349T 2002-11-26 2012-04-09 Παραγωγα υποκατεστημενου αρυλαλκανοϊκου οξεος ως αγωνιστες ppar pan με ισχυρη αντιυπεργλυκαιμικη και αντιυπερλιπιδαιμικη δραστικοτητα CY1112622T1 (el)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US42922102P 2002-11-26 2002-11-26
US46936803P 2003-05-09 2003-05-09
US10/715,622 US7268157B2 (en) 2002-11-26 2003-11-18 Substituted arylalcanoic acid derivatives as PPAR pan agonists with potent antihyperglycemic and antihyperlipidemic activity
EP03772525A EP1569904B1 (en) 2002-11-26 2003-11-21 Substituted arylalcanoic acid derivatives as ppar pan agonists with potent antihyperglycemic and antihyperlipidemic activity

Publications (1)

Publication Number Publication Date
CY1112622T1 true CY1112622T1 (el) 2016-02-10

Family

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CY20121100349T CY1112622T1 (el) 2002-11-26 2012-04-09 Παραγωγα υποκατεστημενου αρυλαλκανοϊκου οξεος ως αγωνιστες ppar pan με ισχυρη αντιυπεργλυκαιμικη και αντιυπερλιπιδαιμικη δραστικοτητα

Country Status (14)

Country Link
US (2) US7268157B2 (el)
EP (1) EP1569904B1 (el)
JP (1) JP4750556B2 (el)
KR (1) KR20050075386A (el)
AT (1) ATE540925T1 (el)
AU (1) AU2003280154B2 (el)
CA (1) CA2504718C (el)
CY (1) CY1112622T1 (el)
DK (1) DK1569904T3 (el)
ES (1) ES2382312T3 (el)
HK (1) HK1083021A1 (el)
PT (1) PT1569904E (el)
SI (1) SI1569904T1 (el)
WO (1) WO2004048333A1 (el)

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JP4880591B2 (ja) 2004-06-04 2012-02-22 テバ ファーマシューティカル インダストリーズ リミティド イルベサルタンを含む医薬組成物
WO2006046779A1 (ja) * 2004-10-29 2006-05-04 Zeria Pharmaceutical Co., Ltd. カルバゾール誘導体、その溶媒和物、又は薬学的に許容されるその塩
US20090197947A1 (en) * 2008-02-01 2009-08-06 The Research Foundation Of State University Of New York Medicaments and methods for lowering plasma lipid levels and screening drugs
CN105801468B (zh) * 2014-12-31 2018-08-17 深圳微芯生物科技股份有限公司 一种苯丙氨酸类化合物的盐及其无定形体
CN112479977B (zh) * 2016-09-27 2022-07-19 深圳微芯生物科技股份有限公司 一种取代的苯基丙酸化合物对映异构体及其制备方法、组合物和应用
CN107868033B (zh) * 2016-09-27 2021-05-18 深圳微芯生物科技股份有限公司 一种苯丙氨酸类化合物的制备方法
CN110467560A (zh) 2018-05-09 2019-11-19 深圳微芯生物科技股份有限公司 一种苯基氨基丙酸钠衍生物、其制备方法和应用
CN112516137A (zh) * 2019-09-19 2021-03-19 深圳微芯生物科技股份有限公司 西格列羧及其衍生物用于伴有脂代谢异常的2型糖尿病治疗的用途
CN111437393B (zh) * 2020-04-30 2021-03-02 深圳微芯生物科技股份有限公司 用于糖尿病及其并发症治疗的联合用药及其药物组合物

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US6054453A (en) 1997-10-27 2000-04-25 Redd's Research Foundation Tricyclic compounds and their use in medicine process for their preparation and pharmaceutical compositions containing them
US6440961B1 (en) * 1997-10-27 2002-08-27 Dr. Reddy's Research Foundation Tricyclic compounds and their use in medicine: process for their preparation and pharmaceutical compositions containing them
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US20030055076A1 (en) * 2001-07-30 2003-03-20 Lone Jeppesen Novel compounds, their preparation and use

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Publication number Publication date
EP1569904B1 (en) 2012-01-11
US20080051321A1 (en) 2008-02-28
JP2006519171A (ja) 2006-08-24
KR20050075386A (ko) 2005-07-20
CA2504718A1 (en) 2004-06-10
JP4750556B2 (ja) 2011-08-17
PT1569904E (pt) 2012-04-19
ATE540925T1 (de) 2012-01-15
US7268157B2 (en) 2007-09-11
DK1569904T3 (da) 2012-04-30
HK1083021A1 (en) 2006-06-23
SI1569904T1 (sl) 2012-06-29
US20040142921A1 (en) 2004-07-22
CA2504718C (en) 2012-01-31
EP1569904A1 (en) 2005-09-07
WO2004048333A1 (en) 2004-06-10
EP1569904A4 (en) 2008-04-16
ES2382312T3 (es) 2012-06-07
AU2003280154A1 (en) 2004-06-18
AU2003280154B2 (en) 2009-04-02

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