CN100534997C - C-芳基葡糖苷sglt2抑制剂和方法 - Google Patents

C-芳基葡糖苷sglt2抑制剂和方法 Download PDF

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Publication number
CN100534997C
CN100534997C CNB038113538A CN03811353A CN100534997C CN 100534997 C CN100534997 C CN 100534997C CN B038113538 A CNB038113538 A CN B038113538A CN 03811353 A CN03811353 A CN 03811353A CN 100534997 C CN100534997 C CN 100534997C
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Prior art keywords
compound
agents
inhibitors
disclosed
sglt2
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Expired - Lifetime
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CNB038113538A
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Chinese (zh)
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CN1653075A (zh
Inventor
B·埃尔斯沃斯
W·N·沃什伯恩
P·M·谢尔
G·吴
W·孟
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AstraZeneca AB
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Bristol Myers Squibb Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/10—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00—Ethers; Compounds having groups, groups or groups
    • C07C43/02—Ethers
    • C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
    • C07C43/225—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing halogen
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A—HUMAN NECESSITIES
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    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
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    • 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
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    • 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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/45—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by condensation
    • C07C45/46—Friedel-Crafts reactions
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/76—Ketones containing a keto group bound to a six-membered aromatic ring
    • C07C49/84—Ketones containing a keto group bound to a six-membered aromatic ring containing ether groups, groups, groups, or groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/203—Monocyclic carbocyclic rings other than cyclohexane rings; Bicyclic carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/04—Carbocyclic radicals

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (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)
CNB038113538A 2002-05-20 2003-05-15 C-芳基葡糖苷sglt2抑制剂和方法 Expired - Lifetime CN100534997C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10/151,436 2002-05-20
US10/151,436 US6515117B2 (en) 1999-10-12 2002-05-20 C-aryl glucoside SGLT2 inhibitors and method

Related Child Applications (4)

Application Number Title Priority Date Filing Date
CN201210054766.9A Division CN102627676B (zh) 2002-05-20 2003-05-15 C-芳基葡糖苷sglt2抑制剂和方法
CN2009101586866A Division CN101628905B (zh) 2002-05-20 2003-05-15 C-芳基葡糖苷sglt2抑制剂和方法
CNA2007101089864A Division CN101092409A (zh) 2002-05-20 2003-05-15 C－芳基葡糖苷sglt2抑制剂和方法
CN201410345395.9A Division CN104230866A (zh) 2002-05-20 2003-05-15 C-芳基葡糖苷sglt2抑制剂和方法

Publications (2)

Publication Number Publication Date
CN1653075A CN1653075A (zh) 2005-08-10
CN100534997C true CN100534997C (zh) 2009-09-02

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ID=29582046

Family Applications (5)

Application Number Title Priority Date Filing Date
CNB038113538A Expired - Lifetime CN100534997C (zh) 2002-05-20 2003-05-15 C-芳基葡糖苷sglt2抑制剂和方法
CN2009101586866A Expired - Lifetime CN101628905B (zh) 2002-05-20 2003-05-15 C-芳基葡糖苷sglt2抑制剂和方法
CN201210054766.9A Expired - Lifetime CN102627676B (zh) 2002-05-20 2003-05-15 C-芳基葡糖苷sglt2抑制剂和方法
CN201410345395.9A Pending CN104230866A (zh) 2002-05-20 2003-05-15 C-芳基葡糖苷sglt2抑制剂和方法
CNA2007101089864A Pending CN101092409A (zh) 2002-05-20 2003-05-15 C－芳基葡糖苷sglt2抑制剂和方法

Family Applications After (4)

Application Number Title Priority Date Filing Date
CN2009101586866A Expired - Lifetime CN101628905B (zh) 2002-05-20 2003-05-15 C-芳基葡糖苷sglt2抑制剂和方法
CN201210054766.9A Expired - Lifetime CN102627676B (zh) 2002-05-20 2003-05-15 C-芳基葡糖苷sglt2抑制剂和方法
CN201410345395.9A Pending CN104230866A (zh) 2002-05-20 2003-05-15 C-芳基葡糖苷sglt2抑制剂和方法
CNA2007101089864A Pending CN101092409A (zh) 2002-05-20 2003-05-15 C－芳基葡糖苷sglt2抑制剂和方法

Country Status (39)

Country Link
US (1) US6515117B2 (OSRAM)
EP (1) EP1506211B1 (OSRAM)
JP (4) JP5090621B2 (OSRAM)
KR (1) KR101021752B1 (OSRAM)
CN (5) CN100534997C (OSRAM)
AR (1) AR040032A1 (OSRAM)
AT (1) ATE353334T1 (OSRAM)
AU (1) AU2003237886B2 (OSRAM)
BE (2) BE2013C025I2 (OSRAM)
BR (2) BRPI0311323B8 (OSRAM)
CA (1) CA2486539C (OSRAM)
CY (3) CY1106465T1 (OSRAM)
DE (1) DE60311649T2 (OSRAM)
DK (1) DK1506211T3 (OSRAM)
ES (1) ES2280759T3 (OSRAM)
FR (2) FR13C0022I2 (OSRAM)
GE (1) GEP20084403B (OSRAM)
HK (1) HK1205120A1 (OSRAM)
HR (1) HRP20041084B1 (OSRAM)
IL (1) IL165119A0 (OSRAM)
IN (1) IN2004DE03573A (OSRAM)
IS (1) IS7529A (OSRAM)
LT (1) LTC1506211I2 (OSRAM)
LU (2) LU92182I2 (OSRAM)
ME (2) MEP13008A (OSRAM)
MX (1) MX249731B (OSRAM)
MY (1) MY142499A (OSRAM)
NO (4) NO329107B1 (OSRAM)
NZ (1) NZ536605A (OSRAM)
PE (1) PE20040760A1 (OSRAM)
PL (1) PL210304B1 (OSRAM)
PT (1) PT1506211E (OSRAM)
RS (1) RS51469B (OSRAM)
RU (4) RU2337916C2 (OSRAM)
SI (1) SI1506211T1 (OSRAM)
TW (1) TWI310770B (OSRAM)
UA (1) UA77306C2 (OSRAM)
WO (1) WO2003099836A1 (OSRAM)
ZA (1) ZA200409295B (OSRAM)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108218928A (zh) * 2016-12-13 2018-06-29 华润双鹤药业股份有限公司 葡萄糖苷的二环衍生物及其制备方法和用途
WO2022067724A1 (zh) 2020-09-30 2022-04-07 北京睿创康泰医药研究院有限公司 一种sglt-2抑制剂·肌氨酸共晶体及其制备方法和应用

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