CN104230866A - 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
CN104230866A
CN104230866A CN201410345395.9A CN201410345395A CN104230866A CN 104230866 A CN104230866 A CN 104230866A CN 201410345395 A CN201410345395 A CN 201410345395A CN 104230866 A CN104230866 A CN 104230866A
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China
Prior art keywords
reagent
inhibitor
compound
diabetic
combine
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Pending
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CN201410345395.9A
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English (en)
Chinese (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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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of CN104230866A publication Critical patent/CN104230866A/zh
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    • 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
    • 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
    • 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
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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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
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    • 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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    • 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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  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
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  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (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)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (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)
CN201410345395.9A 2002-05-20 2003-05-15 C-芳基葡糖苷sglt2抑制剂和方法 Pending CN104230866A (zh)

Applications Claiming Priority (2)

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

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CNB038113538A Division CN100534997C (zh) 2002-05-20 2003-05-15 C-芳基葡糖苷sglt2抑制剂和方法

Publications (1)

Publication Number Publication Date
CN104230866A true CN104230866A (zh) 2014-12-24

Family

ID=29582046

Family Applications (5)

Application Number Title Priority Date Filing Date
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
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

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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

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CNA2007101089864A Pending CN101092409A (zh) 2002-05-20 2003-05-15 C－芳基葡糖苷sglt2抑制剂和方法
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

Country Status (39)

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US (1) US6515117B2 (2)
EP (1) EP1506211B1 (2)
JP (4) JP5090621B2 (2)
KR (1) KR101021752B1 (2)
CN (5) CN102627676B (2)
AR (1) AR040032A1 (2)
AT (1) ATE353334T1 (2)
AU (1) AU2003237886B2 (2)
BE (2) BE2013C025I2 (2)
BR (2) BR122017015091B8 (2)
CA (1) CA2486539C (2)
CY (3) CY1106465T1 (2)
DE (1) DE60311649T2 (2)
DK (1) DK1506211T3 (2)
ES (1) ES2280759T3 (2)
FR (2) FR13C0022I2 (2)
GE (1) GEP20084403B (2)
HK (1) HK1205120A1 (2)
HR (1) HRP20041084B1 (2)
IL (1) IL165119A0 (2)
IN (1) IN2004DE03573A (2)
IS (1) IS7529A (2)
LT (1) LTC1506211I2 (2)
LU (2) LU92182I2 (2)
ME (2) MEP13008A (2)
MX (1) MX249731B (2)
MY (1) MY142499A (2)
NO (4) NO329107B1 (2)
NZ (1) NZ536605A (2)
PE (1) PE20040760A1 (2)
PL (1) PL210304B1 (2)
PT (1) PT1506211E (2)
RS (1) RS51469B (2)
RU (4) RU2337916C2 (2)
SI (1) SI1506211T1 (2)
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UA (1) UA77306C2 (2)
WO (1) WO2003099836A1 (2)
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Cited By (12)

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CN104478959A (zh) * 2015-01-14 2015-04-01 佛山市赛维斯医药科技有限公司 含腈基联苯双葡萄糖苷结构化合物、其制备方法和用途
CN104478966A (zh) * 2015-01-14 2015-04-01 佛山市赛维斯医药科技有限公司 含苯胺噻唑基的o-半乳糖苷衍生物、其制备方法和用途
CN104478965A (zh) * 2015-01-15 2015-04-01 佛山市赛维斯医药科技有限公司 一类烷氧基苯基s-葡萄糖苷衍生物、其制备方法和用途
CN104478968A (zh) * 2015-01-14 2015-04-01 佛山市赛维斯医药科技有限公司 含噻唑基的o-半乳糖苷衍生物、其制备方法和用途
CN104478957A (zh) * 2015-01-14 2015-04-01 佛山市赛维斯医药科技有限公司 一种含腈基苯和双o-葡萄糖苷衍生物、其制备方法和用途
CN104478963A (zh) * 2015-01-15 2015-04-01 佛山市赛维斯医药科技有限公司 一种含腈基苯s-葡萄糖苷结构的化合物及其用途
CN104497070A (zh) * 2015-01-15 2015-04-08 佛山市赛维斯医药科技有限公司 一种含三氟甲基苯s-葡萄糖苷结构的化合物和用途
CN104530149A (zh) * 2015-01-14 2015-04-22 佛山市赛维斯医药科技有限公司 卤代苯基双o-葡萄糖苷衍生物、其制备方法和用途
CN105218329A (zh) * 2015-10-15 2016-01-06 上海应用技术学院 一种列净类似物中间体及其制备方法
WO2016206604A1 (zh) * 2015-06-23 2016-12-29 中国科学院上海药物研究所 一种c, o-螺环芳基糖苷类化合物及其制备和应用
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
CN108699098A (zh) * 2016-01-04 2018-10-23 第药品株式会社 具有稠合苯环的c-葡糖苷衍生物或其药物学可接受的盐、其制备方法以及包含其的药物组合物

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CN1020944C (zh) * 1990-01-30 1993-05-26 阿图尔-费希尔股份公司费希尔厂 紧固件
US6515117B2 (en) * 1999-10-12 2003-02-04 Bristol-Myers Squibb Company C-aryl glucoside SGLT2 inhibitors and method
FR2809310B1 (fr) * 2000-05-26 2004-02-13 Centre Nat Rech Scient Utilisation de derives de biguanide pour fabriquer un medicament ayant un effet cicatrisant
EP1345602B1 (en) 2000-11-30 2010-07-21 Novodermix International Limited Wound healing
EP1368349B1 (de) * 2001-02-24 2007-02-14 Boehringer Ingelheim Pharma GmbH & Co.KG Xanthinderivate, deren herstellung und deren verwendung als arzneimittel
US6936590B2 (en) * 2001-03-13 2005-08-30 Bristol Myers Squibb Company C-aryl glucoside SGLT2 inhibitors and method
CN100577175C (zh) * 2001-04-04 2010-01-06 奥索-麦克尼尔药品公司 包括葡萄糖重吸收抑制剂和ppar调节剂的联合疗法
AU2002254567B2 (en) * 2001-04-11 2007-10-11 Bristol-Myers Squibb Company Amino acid complexes of C-aryl glucosides for treatment of diabetes and method
WO2003020737A1 (en) * 2001-09-05 2003-03-13 Bristol-Myers Squibb Company O-pyrazole glucoside sglt2 inhibitors and method of use
TWI254635B (en) * 2002-08-05 2006-05-11 Yamanouchi Pharma Co Ltd Azulene derivative and salt thereof
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
US7576063B2 (en) * 2002-10-04 2009-08-18 Kissei Pharmaceutical Co., Ltd. Pyrazole derivative, medicinal composition containing the same, medicinal use thereof and intermediate in producing the same
DE10258007B4 (de) * 2002-12-12 2006-02-09 Sanofi-Aventis Deutschland Gmbh Aromatische Fluorglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel
JP2006516257A (ja) * 2003-01-03 2006-06-29 ブリストル−マイヤーズ　スクイブ　カンパニー Ｃ−アリールグルコシドｓｇｌｔ２阻害剤の製造法
EP1457206A1 (en) * 2003-03-13 2004-09-15 Fournier Laboratories Ireland Limited Combined use of a fibrate and orlistat for the treatment of obesity
ES2363941T3 (es) 2003-03-14 2011-08-19 Astellas Pharma Inc. Derivados de c-glucósido para el tratamiento de diabetes.
JP2004300102A (ja) * 2003-03-31 2004-10-28 Kissei Pharmaceut Co Ltd 縮合複素環誘導体、それを含有する医薬組成物およびその医薬用途
WO2005011592A2 (en) * 2003-08-01 2005-02-10 Janssen Pharmaceutica N.V. Substituted indazole-o-glucosides
ES2531660T3 (es) 2003-08-01 2015-03-18 Mitsubishi Tanabe Pharma Corporation Compuestos novedosos que tienen actividad inhibidora frente a transportador de glucosa dependiente de sodio
WO2005012242A2 (en) * 2003-08-01 2005-02-10 Janssen Pharmaceutica Nv Substituted benzimidazole-, benztriazole-, and benzimidazolone-o-glucosides
US8785403B2 (en) 2003-08-01 2014-07-22 Mitsubishi Tanabe Pharma Corporation Glucopyranoside compound
TW200526678A (en) * 2003-08-01 2005-08-16 Janssen Pharmaceutica Nv Substituted indole-O-glucosides
EP1679965A4 (en) * 2003-08-01 2009-05-27 Janssen Pharmaceutica Nv SUBSTITUTED ANELLIERED HETEROCYCLIC C-GLYCOSIDES
US7371759B2 (en) * 2003-09-25 2008-05-13 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
US7420059B2 (en) * 2003-11-20 2008-09-02 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
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CN105218329B (zh) * 2015-10-15 2017-05-03 上海应用技术学院 一种列净类似物中间体及其制备方法
CN108699098A (zh) * 2016-01-04 2018-10-23 第药品株式会社 具有稠合苯环的c-葡糖苷衍生物或其药物学可接受的盐、其制备方法以及包含其的药物组合物
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CN108218928B (zh) * 2016-12-13 2020-06-30 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

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