CN106456998B - 西格列汀丹宁酸盐复合物 - Google Patents

西格列汀丹宁酸盐复合物 Download PDF

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Publication number
CN106456998B
CN106456998B CN201580020211.4A CN201580020211A CN106456998B CN 106456998 B CN106456998 B CN 106456998B CN 201580020211 A CN201580020211 A CN 201580020211A CN 106456998 B CN106456998 B CN 106456998B
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China
Prior art keywords
sitagliptin
tannin
complex
oral dosage
dosage form
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CN201580020211.4A
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Chinese (zh)
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CN106456998A (zh
Inventor
W.奥姆万查
R.伯拉奇
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Merck Sharp and Dohme BV
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Merck Sharp and Dohme LLC
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    • 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
    • A61K31/7032—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a polyol, i.e. compounds having two or more free or esterified hydroxy groups, including the hydroxy group involved in the glycosidic linkage, e.g. monoglucosyldiacylglycerides, lactobionic acid, gangliosides
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Emergency Medicine (AREA)
  • Molecular Biology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Zoology (AREA)
  • Endocrinology (AREA)
  • Biophysics (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201580020211.4A 2014-04-17 2015-04-13 西格列汀丹宁酸盐复合物 Active CN106456998B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461980641P 2014-04-17 2014-04-17
US61/980641 2014-04-17
PCT/US2015/025504 WO2015160678A1 (en) 2014-04-17 2015-04-13 Sitagliptin tannate complex

Publications (2)

Publication Number Publication Date
CN106456998A CN106456998A (zh) 2017-02-22
CN106456998B true CN106456998B (zh) 2020-07-28

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CN201580020211.4A Active CN106456998B (zh) 2014-04-17 2015-04-13 西格列汀丹宁酸盐复合物

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US (1) US9833463B2 (enExample)
EP (1) EP3131631B1 (enExample)
JP (1) JP6523328B2 (enExample)
KR (1) KR102351813B1 (enExample)
CN (1) CN106456998B (enExample)
AU (1) AU2015247921B2 (enExample)
BR (1) BR112016023839A8 (enExample)
CA (1) CA2945681A1 (enExample)
ES (1) ES2932383T3 (enExample)
MX (1) MX374598B (enExample)
RU (1) RU2696588C2 (enExample)
WO (1) WO2015160678A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201818969A (zh) * 2016-10-19 2018-06-01 日商帝化製藥股份有限公司 在生體內之藥物溶出控制用組成物
US11096890B2 (en) 2017-09-29 2021-08-24 Merck Sharp & Dohme Corp. Chewable dosage forms containing sitagliptin and metformin
WO2025090920A1 (en) * 2023-10-25 2025-05-01 Piton Therapeutics, Inc. Compositions and methods for treating dysfunction of glucose metabolism and/or regulation

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007035198A2 (en) * 2005-07-25 2007-03-29 Merck & Co., Inc. Dodecylsulfate salt of a dipeptidyl peptidase-iv inhibitor
WO2007050485A2 (en) * 2005-10-25 2007-05-03 Merck & Co., Inc. Combination of a dipeptidyl peptidase-4 inhibitor and an anti-hypertensive agent for the treatment of diabetes and hypertension
CN101600346A (zh) * 2006-12-14 2009-12-09 泰华制药工业有限公司 雷沙吉兰的单宁酸盐
CN102388047A (zh) * 2009-02-11 2012-03-21 力奇制药公司 西他列汀的新盐

Family Cites Families (23)

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WO1997028149A1 (en) 1996-02-02 1997-08-07 Merck & Co., Inc. Method for raising hdl cholesterol levels
US5663415A (en) 1996-06-28 1997-09-02 Jame Fine Chemicals, Inc. Process for preparing antihistamine tannates
AR008789A1 (es) 1996-07-31 2000-02-23 Bayer Corp Piridinas y bifenilos substituidos
WO1999001423A1 (en) 1997-07-01 1999-01-14 Novo Nordisk A/S Glucagon antagonists/inverse agonists
US6613942B1 (en) 1997-07-01 2003-09-02 Novo Nordisk A/S Glucagon antagonists/inverse agonists
WO2000042026A1 (en) 1999-01-15 2000-07-20 Novo Nordisk A/S Non-peptide glp-1 agonists
AU4537900A (en) 1999-05-17 2000-12-05 Agouron Pharmaceuticals, Inc. Glucagon antagonists/inverse agonists
RU2269354C2 (ru) 1999-09-28 2006-02-10 Байер Корпорейшн Агонисты рецептора-3(r3) пептида-активатора гипофизарной аденилатциклазы(расар) и способы их фармакологического применения
CN101624391A (zh) 2001-06-11 2010-01-13 病毒化学医药公司 用作黄病毒感染抗病毒剂的噻吩衍生物
UA74912C2 (en) * 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
US20030083354A1 (en) 2001-10-26 2003-05-01 Pediamed Pharmaceuticals, Inc. Phenylephrine tannate and pyrilamine tannate salts in pharmaceutical compositions
US20030114535A1 (en) 2001-12-14 2003-06-19 Jame Fine Chemicals, Inc. Dextrochlorpheniramine tannate
US6670370B1 (en) 2001-12-14 2003-12-30 Jame Fine Chemicals, Inc. Dextromethorphan tannate
JO2625B1 (en) * 2003-06-24 2011-11-01 ميرك شارب اند دوم كوربوريشن Phosphoric acid salts of dipeptidyl betidase inhibitor 4
CA2536251C (en) 2003-09-02 2009-08-04 Merck & Co., Inc. Novel crystalline forms of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
EP1667524A4 (en) 2003-09-23 2009-01-14 Merck & Co Inc NEW CRYSTALLINE FORM OF A PHOSPHORIC ACID SALT OF A DIPEPTIDYLPEPTIDASE IV INHIBITOR
EP1708571A4 (en) 2004-01-16 2009-07-08 Merck & Co Inc NEW CRYSTALLINE SALTS OF A DIPEPTIDYLPEPTIDASE IV HEMMER
US20050202050A1 (en) * 2004-03-12 2005-09-15 Kiel Jeffrey S. Single tank process for preparing tannate liquid and semi-solid dosage forms
WO2006033848A1 (en) 2004-09-15 2006-03-30 Merck & Co., Inc. Amorphous form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
US20060270722A1 (en) * 2005-05-31 2006-11-30 Thornberry Nancy A Combination of a dipeptidyl peptidase-IV inhibitor and a dual PPAR agonist for the treatment of diabetes and obesity
JP2011506442A (ja) * 2007-12-11 2011-03-03 コンジュケム バイオテクノロジーズ インコーポレイテッド インスリン分泌性ペプチド結合体の製剤
US8003672B2 (en) * 2008-04-21 2011-08-23 Merck Sharp & Dohme Corp. CB-1 receptor modulator formulations
US9211263B2 (en) 2012-01-06 2015-12-15 Elcelyx Therapeutics, Inc. Compositions and methods of treating metabolic disorders

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007035198A2 (en) * 2005-07-25 2007-03-29 Merck & Co., Inc. Dodecylsulfate salt of a dipeptidyl peptidase-iv inhibitor
WO2007050485A2 (en) * 2005-10-25 2007-05-03 Merck & Co., Inc. Combination of a dipeptidyl peptidase-4 inhibitor and an anti-hypertensive agent for the treatment of diabetes and hypertension
CN101600346A (zh) * 2006-12-14 2009-12-09 泰华制药工业有限公司 雷沙吉兰的单宁酸盐
CN102388047A (zh) * 2009-02-11 2012-03-21 力奇制药公司 西他列汀的新盐

Also Published As

Publication number Publication date
MX374598B (es) 2025-03-06
CA2945681A1 (en) 2015-10-22
RU2016144695A (ru) 2018-05-21
CN106456998A (zh) 2017-02-22
JP2017511350A (ja) 2017-04-20
EP3131631B1 (en) 2022-11-16
KR102351813B1 (ko) 2022-01-18
BR112016023839A2 (pt) 2017-08-15
ES2932383T3 (es) 2023-01-18
WO2015160678A1 (en) 2015-10-22
JP6523328B2 (ja) 2019-05-29
AU2015247921A1 (en) 2016-10-13
BR112016023839A8 (pt) 2023-04-11
RU2016144695A3 (enExample) 2018-10-11
RU2696588C2 (ru) 2019-08-05
MX2016013588A (es) 2017-01-26
US9833463B2 (en) 2017-12-05
EP3131631A1 (en) 2017-02-22
EP3131631A4 (en) 2017-11-29
US20170042922A1 (en) 2017-02-16
KR20160145008A (ko) 2016-12-19
AU2015247921B2 (en) 2019-07-11

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