RU2013136384A - Композиция, содержащая ингибиторы котранспортеров натрия-глюкозы 1 и 2, и способы их применения - Google Patents

Композиция, содержащая ингибиторы котранспортеров натрия-глюкозы 1 и 2, и способы их применения Download PDF

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RU2013136384A
RU2013136384A RU2013136384/15A RU2013136384A RU2013136384A RU 2013136384 A RU2013136384 A RU 2013136384A RU 2013136384/15 A RU2013136384/15 A RU 2013136384/15A RU 2013136384 A RU2013136384 A RU 2013136384A RU 2013136384 A RU2013136384 A RU 2013136384A
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Цзиньлин ЧЭНЬ
Нассер Н. НИАМВЕИА
Кеннет К. Х. ОНГ
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Лексикон Фармасьютикалз, Инк.
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Abstract

1. Твердая дозированная форма, содержащая API и по меньшей мере одно из натриевой соли кроскармеллозы или микрокристаллической целлюлозы, где API представляет кристаллический безводный (2S,3R,4R,5S,6R)-2-(4-хлор-3-(4-этоксибензил)фенил)-6-(метилтио)тетрагидро-2Н-пиран-3,4,5-триол.2. Твердая дозированная форма по п.1, где API представляет кристаллическую безводную форму 1 (2S,3R,4R,5S,6R)-2-(4-хлор-3-(4-этоксибензил)фенил)-6-(метилтио)тетрагидро-2Н-пиран-3,4,5-триола.3. Твердая дозированная форма по п.1, где API представляет кристаллическую безводную форму 2 (2S,3R,4R,5S,6R)-2-(4-хлор-3-(4-этоксибензил)фенил)-6-(метилтио)тетрагидро-2Н-пиран-3,4,5-триола.4. Твердая дозированная форма по п.1, где API находится в количестве 300 мг или ниже.5. Твердая дозированная форма по п.1, которая дополнительно содержит диоксид кремния.6. Твердая дозированная форма по п.1, которая представляет таблетку.7. Твердая дозированная форма по пп.1-6, которая дополнительно содержит второй терапевтический агент, где второй терапевтический агент представляет антидиабетический агент, антигипергликемический агент, гиполипидемический/снижающий уровень липидов агент, агенты против ожирения, антигипертензивный агент или агент, снижающий аппетит.8. Твердая дозированная форма по п.7, где второй терапевтический агент представляет ингибитор DPP-4 (например, ситаглиптин, дутоглиптин).9. Гранула, содержащая API и по меньшей мере одно из натриевой соли кроскармеллозы, коллоидного диоксида кремния и микрокристаллической целлюлозы, где API представляет (2S,3R,4R,5S,6R)-2-(4-хлор-3-(4-этоксибензил)фенил)-6-(метилтио)тетрагидро-2Н-пиран-3,4,5-триол.10. Гранула по п.9, где API представляет кристаллическую безводную форму 1 (2S,3R,4R,5S,6R)-2-(4-хлор-3-

Claims (15)

1. Твердая дозированная форма, содержащая API и по меньшей мере одно из натриевой соли кроскармеллозы или микрокристаллической целлюлозы, где API представляет кристаллический безводный (2S,3R,4R,5S,6R)-2-(4-хлор-3-(4-этоксибензил)фенил)-6-(метилтио)тетрагидро-2Н-пиран-3,4,5-триол.
2. Твердая дозированная форма по п.1, где API представляет кристаллическую безводную форму 1 (2S,3R,4R,5S,6R)-2-(4-хлор-3-(4-этоксибензил)фенил)-6-(метилтио)тетрагидро-2Н-пиран-3,4,5-триола.
3. Твердая дозированная форма по п.1, где API представляет кристаллическую безводную форму 2 (2S,3R,4R,5S,6R)-2-(4-хлор-3-(4-этоксибензил)фенил)-6-(метилтио)тетрагидро-2Н-пиран-3,4,5-триола.
4. Твердая дозированная форма по п.1, где API находится в количестве 300 мг или ниже.
5. Твердая дозированная форма по п.1, которая дополнительно содержит диоксид кремния.
6. Твердая дозированная форма по п.1, которая представляет таблетку.
7. Твердая дозированная форма по пп.1-6, которая дополнительно содержит второй терапевтический агент, где второй терапевтический агент представляет антидиабетический агент, антигипергликемический агент, гиполипидемический/снижающий уровень липидов агент, агенты против ожирения, антигипертензивный агент или агент, снижающий аппетит.
8. Твердая дозированная форма по п.7, где второй терапевтический агент представляет ингибитор DPP-4 (например, ситаглиптин, дутоглиптин).
9. Гранула, содержащая API и по меньшей мере одно из натриевой соли кроскармеллозы, коллоидного диоксида кремния и микрокристаллической целлюлозы, где API представляет (2S,3R,4R,5S,6R)-2-(4-хлор-3-(4-этоксибензил)фенил)-6-(метилтио)тетрагидро-2Н-пиран-3,4,5-триол.
10. Гранула по п.9, где API представляет кристаллическую безводную форму 1 (2S,3R,4R,5S,6R)-2-(4-хлор-3-(4-этоксибензил)фенил)-6-(метилтио)тетрагидро-2Н-пиран-3,4,5-триола.
11. Гранула по п.9, где API представляет кристаллическую безводную форму 2 (2S,3R,4R,5S,6R)-2-(4-хлор-3-(4-этоксибензил)фенил)-6-(метилтио)тетрагидро-2Н-пиран-3,4,5-триола.
12. Применение лекарственной формы по любому из пп.1-8 для улучшения состояния сердечно-сосудистой системы и обмена веществ у пациента.
13. Применение лекарственной формы по любому из пп.1-8 для лечения диабета у пациента.
14. Применение по п.13, где пациент принял или принимает в настоящее время второй терапевтический агент, где второй терапевтический агент представляет антидиабетический агент, антигипергликемический агент, гиполипидемический/снижающий уровень липидов агент, агенты против ожирения, антигипертензивный агент или агент, снижающий аппетит.
15. Применение по п.14, где второе лекарственное средство представляет бигуанид, например метформин, фенформин.
RU2013136384A 2011-01-05 2012-01-03 Композиция, содержащая ингибиторы котранспортеров натрия-глюкозы 1 и 2, и способы их применения RU2669921C2 (ru)

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PCT/US2012/020042 WO2012094293A1 (en) 2011-01-05 2012-01-03 Compositions comprising and methods of using inhibitors of sodium-glucose cotransporters 1 and 2

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Publication number Priority date Publication date Assignee Title
US9200025B2 (en) * 2012-11-20 2015-12-01 Lexicon Pharmaceuticals, Inc. Inhibitors of sodium glucose cotransporter 1
EP3466958B1 (en) * 2016-05-25 2020-04-29 Crystal Pharmaceutical (Suzhou) Co., Ltd. New crystal forms of sodium-glucose co-transporter inhibitor, processes for preparation and use thereof
WO2018231702A1 (en) 2017-06-13 2018-12-20 The Regents Of The University Of California Methods of improving cell-based therapy
CN107540685B (zh) * 2017-09-04 2020-05-05 杭州科巢生物科技有限公司 一种Sotagliflozin的制备方法及其中间体
EP3456320A1 (de) 2017-09-15 2019-03-20 Stada Arzneimittel Ag Dpp-4-inhibitor-mono-zusammensetzung
KR102283677B1 (ko) * 2018-01-05 2021-07-29 산동 단홍 파머수티컬 컴퍼니., 리미티드. Sglt 억제제 및 그 응용
CN110117304A (zh) * 2018-04-23 2019-08-13 中国科学院成都生物研究所 一种钠-葡萄糖协同转运蛋白1和2抑制剂的药物用途
CN110818722B (zh) * 2018-08-14 2022-12-02 苏州鹏旭医药科技有限公司 三种化合物及其制备方法和在合成索格列净中的用途
AU2020310274B2 (en) 2019-07-05 2022-09-29 Shandong Danhong Pharmaceutical Co., Ltd. Crystal form of SGLT inhibitor and application thereof
EP4005568B1 (en) 2019-07-26 2024-07-10 Dongbao Purple Star (Hangzhou) Biopharmaceutical Co., Ltd. Sglts/dpp4 inhibitor and application thereof
EP4054556A4 (en) * 2019-11-07 2023-11-29 Increvet, Inc. SODIUM-GLUCOSE TRANSPORTER INHIBITORS FOR THE MANAGEMENT OF CHRONIC KIDNEY FAILURE, HYPERTENSION AND HEART FAILURE IN PETS
WO2022144465A1 (en) 2021-01-04 2022-07-07 Charité-Universitätsmedizin Berlin Sotagliflozin for improving left atrial function
WO2022155303A1 (en) 2021-01-14 2022-07-21 Lexicon Pharmaceuticals, Inc. Sotagliflozin for treating or preventing cardiovascular diseases

Family Cites Families (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB284425A (en) 1926-11-22 1928-02-02 James Last Improvements in and relating to sand or like moulds for making castings
US3674836A (en) 1968-05-21 1972-07-04 Parke Davis & Co 2,2-dimethyl-{11 -aryloxy-alkanoic acids and salts and esters thereof
US4027009A (en) 1973-06-11 1977-05-31 Merck & Co., Inc. Compositions and methods for depressing blood serum cholesterol
JPS5612114B2 (ru) 1974-06-07 1981-03-18
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
DK149080C (da) 1980-06-06 1986-07-28 Sankyo Co Fremgangsmaade til fremstilling af derivater af ml-236b-carboxylsyre
US4450171A (en) 1980-08-05 1984-05-22 Merck & Co., Inc. Antihypercholesterolemic compounds
US4448784A (en) 1982-04-12 1984-05-15 Hoechst-Roussel Pharmaceuticals, Inc. 1-(Aminoalkylphenyl and aminoalkylbenzyl)-indoles and indolines and analgesic method of use thereof
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
US4499289A (en) 1982-12-03 1985-02-12 G. D. Searle & Co. Octahydronapthalenes
CA1327360C (en) 1983-11-14 1994-03-01 William F. Hoffman Oxo-analogs of mevinolin-like antihypercholesterolemic agents
US4613610A (en) 1984-06-22 1986-09-23 Sandoz Pharmaceuticals Corp. Cholesterol biosynthesis inhibiting pyrazole analogs of mevalonolactone and its derivatives
US4686237A (en) 1984-07-24 1987-08-11 Sandoz Pharmaceuticals Corp. Erythro-(E)-7-[3'-C1-3 alkyl-1'-(3",5"-dimethylphenyl)naphth-2'-yl]-3,5-dihydroxyhept-6-enoic acids and derivatives thereof
US4647576A (en) 1984-09-24 1987-03-03 Warner-Lambert Company Trans-6-[2-(substitutedpyrrol-1-yl)alkyl]-pyran-2-one inhibitors of cholesterol synthesis
DE3581638D1 (de) 1984-12-04 1991-03-07 Sandoz Ag Inden-analoga von mevalonolakton und ihre derivate.
US4668794A (en) 1985-05-22 1987-05-26 Sandoz Pharm. Corp. Intermediate imidazole acrolein analogs
KR900001212B1 (ko) 1985-10-25 1990-02-28 산도즈 파마슈티칼스 코오포레이숀 메바로노락톤 및 그것의 유도체의 헤테로사이클릭 유사체 및 그것의 생산방법 및 약학적인 그것의 용도
FR2596393B1 (fr) 1986-04-01 1988-06-03 Sanofi Sa Derives de l'acide hydroxy-3 dihydroxyoxophosphorio-4 butanoique, leur procede de preparation, leur application comme medicament et les compositions les renfermant
US5614492A (en) 1986-05-05 1997-03-25 The General Hospital Corporation Insulinotropic hormone GLP-1 (7-36) and uses thereof
US4681893A (en) 1986-05-30 1987-07-21 Warner-Lambert Company Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis
GB2205837B (en) 1987-05-22 1991-11-20 Squibb & Sons Inc Phosphorus-containing hmg-coa reductase inhibitors
US4759923A (en) 1987-06-25 1988-07-26 Hercules Incorporated Process for lowering serum cholesterol using poly(diallylmethylamine) derivatives
JP2569746B2 (ja) 1987-08-20 1997-01-08 日産化学工業株式会社 キノリン系メバロノラクトン類
US4924024A (en) 1988-01-11 1990-05-08 E. R. Squibb & Sons, Inc. Phosphorus-containing squalene synthetase inhibitors, new intermediates and method
US4871721A (en) 1988-01-11 1989-10-03 E. R. Squibb & Sons, Inc. Phosphorus-containing squalene synthetase inhibitors
NO177005C (no) 1988-01-20 1995-07-05 Bayer Ag Analogifremgangsmåte for fremstilling av substituerte pyridiner, samt mellomprodukter til bruk ved fremstillingen
US5506219A (en) 1988-08-29 1996-04-09 E. R. Squibb & Sons, Inc. Pyridine anchors for HMG-CoA reductase inhibitors
US5753675A (en) 1989-03-03 1998-05-19 Novartis Pharmaceuticals Corporation Quinoline analogs of mevalonolactone and derivatives thereof
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
US5177080A (en) 1990-12-14 1993-01-05 Bayer Aktiengesellschaft Substituted pyridyl-dihydroxy-heptenoic acid and its salts
JP2648897B2 (ja) 1991-07-01 1997-09-03 塩野義製薬株式会社 ピリミジン誘導体
US5595872A (en) 1992-03-06 1997-01-21 Bristol-Myers Squibb Company Nucleic acids encoding microsomal trigyceride transfer protein
US5470845A (en) 1992-10-28 1995-11-28 Bristol-Myers Squibb Company Methods of using α-phosphonosulfonate squalene synthetase inhibitors including the treatment of atherosclerosis and hypercholesterolemia
US5594016A (en) 1992-12-28 1997-01-14 Mitsubishi Chemical Corporation Naphthalene derivatives
DK0680320T3 (da) 1993-01-19 1999-10-25 Warner Lambert Co Stabilt oralt CI-981-præparat og fremgangsmåde til fremstilling deraf
US5739135A (en) 1993-09-03 1998-04-14 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
US5776983A (en) 1993-12-21 1998-07-07 Bristol-Myers Squibb Company Catecholamine surrogates useful as β3 agonists
US5488064A (en) 1994-05-02 1996-01-30 Bristol-Myers Squibb Company Benzo 1,3 dioxole derivatives
US5385929A (en) 1994-05-04 1995-01-31 Warner-Lambert Company [(Hydroxyphenylamino) carbonyl] pyrroles
US5612359A (en) 1994-08-26 1997-03-18 Bristol-Myers Squibb Company Substituted biphenyl isoxazole sulfonamides
US5491134A (en) 1994-09-16 1996-02-13 Bristol-Myers Squibb Company Sulfonic, phosphonic or phosphiniic acid β3 agonist derivatives
US5541204A (en) 1994-12-02 1996-07-30 Bristol-Myers Squibb Company Aryloxypropanolamine β 3 adrenergic agonists
US5620997A (en) 1995-05-31 1997-04-15 Warner-Lambert Company Isothiazolones
AU6966696A (en) 1995-10-05 1997-04-28 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
EP0873361B1 (en) 1995-12-13 2006-11-02 The Regents Of The University Of California Crystals of the ligand-binding domain of the thyroid hormone receptor complexed to a ligand
US5770615A (en) 1996-04-04 1998-06-23 Bristol-Myers Squibb Company Catecholamine surrogates useful as β3 agonists
US5962440A (en) 1996-05-09 1999-10-05 Bristol-Myers Squibb Company Cyclic phosphonate ester inhibitors of microsomal triglyceride transfer protein and method
US5885983A (en) 1996-05-10 1999-03-23 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
US5827875A (en) 1996-05-10 1998-10-27 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
US5760246A (en) 1996-12-17 1998-06-02 Biller; Scott A. Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method
TW536540B (en) 1997-01-30 2003-06-11 Bristol Myers Squibb Co Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe
GB9713739D0 (en) 1997-06-27 1997-09-03 Karobio Ab Thyroid receptor ligands
CA2319195A1 (en) 1998-02-02 1999-08-05 Trustees Of Tufts College Method of regulating glucose metabolism, and reagents related thereto
EP1062222A1 (en) 1998-03-09 2000-12-27 Fondatech Benelux N.V. Serine peptidase modulators
DE19823831A1 (de) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
DE19828113A1 (de) 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
DE19828114A1 (de) 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV
AU767456B2 (en) 1998-07-06 2003-11-13 Bristol-Myers Squibb Company Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists
AR028299A1 (es) * 1999-09-17 2003-05-07 Novartis Ag Una composicion farmaceutica que comprende nateglinida, un proceso para su preparacion y el uso de dicha composicion para la preparacion de un medicamento para el tratamiento de desordenes metabolicos, especialmente diabetes, o de una enfermedad o condicion asociada con diabetes.
TWI260321B (en) 1999-09-22 2006-08-21 Bristol Myers Squibb Co Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
US6414002B1 (en) 1999-09-22 2002-07-02 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
PH12000002657B1 (en) * 1999-10-12 2006-02-21 Bristol Myers Squibb Co C-aryl glucoside SGLT2 inhibitors
US6515117B2 (en) * 1999-10-12 2003-02-04 Bristol-Myers Squibb Company C-aryl glucoside SGLT2 inhibitors and method
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
US6555519B2 (en) 2000-03-30 2003-04-29 Bristol-Myers Squibb Company O-glucosylated benzamide SGLT2 inhibitors and method
RU2353625C2 (ru) 2001-10-18 2009-04-27 Бристол-Маерс Сквибб Компани Миметики человеческого глюканоподобного пептида-1 и их применение в лечении диабета и родственных состояний
UA80991C2 (en) * 2002-10-07 2007-11-26 Solid preparation containing an insulin resistance improving drug and an active ingredient useful as a remedy for diabetes
US7393836B2 (en) * 2004-07-06 2008-07-01 Boehringer Ingelheim International Gmbh D-xylopyranosyl-substituted phenyl derivatives, medicaments containing such compounds, their use and process for their manufacture
TWI499414B (zh) 2006-09-29 2015-09-11 Lexicon Pharmaceuticals Inc 鈉與葡萄糖第２型共同運輸體（ｃｏ-ｔｒａｎｓｐｏｒｔｅｒ ２）的抑制物與其應用方法
WO2008109591A1 (en) 2007-03-08 2008-09-12 Lexicon Pharmaceuticals, Inc. Phlorizin analogs as inhibitors of sodium glucose co-transporter 2
PE20090185A1 (es) * 2007-03-22 2009-02-28 Bristol Myers Squibb Co Formulaciones farmaceuticas que contienen un inhibidor sglt2
CL2008003653A1 (es) * 2008-01-17 2010-03-05 Mitsubishi Tanabe Pharma Corp Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica.
TWI472521B (zh) 2008-07-17 2015-02-11 Lexicon Pharmaceuticals Inc （２ｓ，３ｒ，４ｒ，５ｓ，６ｒ）－２－（４－氯－３－（４－乙氧苄基）苯基）－６－（甲硫）四氫－２ｈ－哌喃－３，４，５－三醇的固體形態與其使用方法
KR100968825B1 (ko) * 2008-07-18 2010-07-08 현대자동차주식회사 차량용 트위터 스피커
JP5896276B2 (ja) * 2009-02-13 2016-03-30 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １型糖尿病、２型糖尿病、耐糖能障害又は高血糖の治療用ｓｇｌｔ−２阻害薬
SG173619A1 (en) * 2009-02-13 2011-09-29 Boehringer Ingelheim Int Pharmaceutical composition comprising a sglt2 inhibitor, a dpp-iv inhibitor and optionally a further antidiabetic agent and uses thereof
US20110077212A1 (en) * 2009-09-25 2011-03-31 Theracos, Inc. Therapeutic uses of sglt2 inhibitors
WO2011060256A2 (en) * 2009-11-13 2011-05-19 Bristol-Myers Squibb Company Bilayer tablet formulations
TWI562775B (en) * 2010-03-02 2016-12-21 Lexicon Pharmaceuticals Inc Methods of using inhibitors of sodium-glucose cotransporters 1 and 2

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