JP2016041701A5 - - Google Patents
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- Publication number
- JP2016041701A5 JP2016041701A5 JP2015193990A JP2015193990A JP2016041701A5 JP 2016041701 A5 JP2016041701 A5 JP 2016041701A5 JP 2015193990 A JP2015193990 A JP 2015193990A JP 2015193990 A JP2015193990 A JP 2015193990A JP 2016041701 A5 JP2016041701 A5 JP 2016041701A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- composition according
- ethoxybenzyl
- triol
- pyran
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- QKDRXGFQVGOQKS-CRSSMBPESA-N (2S,3R,4R,5S,6R)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-methylsulfanyloxane-3,4,5-triol Chemical compound C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](SC)O2)O)=CC=C1Cl QKDRXGFQVGOQKS-CRSSMBPESA-N 0.000 claims 8
- 238000000634 powder X-ray diffraction Methods 0.000 claims 3
- 206010012601 Diabetes mellitus Diseases 0.000 claims 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 208000008787 Cardiovascular Disease Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 238000001237 Raman spectrum Methods 0.000 claims 1
- 201000001320 atherosclerosis Diseases 0.000 claims 1
- 239000007894 caplet Substances 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 201000010874 syndrome Diseases 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
Claims (11)
- 無水（２Ｓ，３Ｒ，４Ｒ，５Ｓ，６Ｒ）−２−（４−クロロ−３−（４−エトキシベンジル）フェニル）−６−（メチルチオ）テトラヒドロ−２Ｈ−ピラン−３，４，５−トリオールの結晶及び薬学的に許容される賦形剤を含む医薬組成物。
- 錠剤、カプセル、又はカプレットの形態である、請求項１に記載の医薬組成物。
- アテローム性動脈硬化症、循環器疾患、糖尿病、高血糖、高血圧、脂質障害、肥満、又はＸ症候群の治療又は管理用である、請求項１又は２に記載の医薬組成物。
- 糖尿病の治療又は管理用である、請求項１〜３のいずれかに記載の医薬組成物。
- 無水（２Ｓ，３Ｒ，４Ｒ，５Ｓ，６Ｒ）−２−（４−クロロ−３−（４−エトキシベンジル）フェニル）−６−（メチルチオ）テトラヒドロ−２Ｈ−ピラン−３，４，５−トリオールの結晶が、１２４℃±５．０℃にＤＳＣ吸熱を有する、請求項１〜４のいずれかに記載の医薬組成物。
- 無水（２Ｓ，３Ｒ，４Ｒ，５Ｓ，６Ｒ）−２−（４−クロロ−３−（４−エトキシベンジル）フェニル）−６−（メチルチオ）テトラヒドロ−２Ｈ−ピラン−３，４，５−トリオールの結晶が、４．０°、８．１°、９．８°、１４．０°及び／又は１９．３°の２θ±０．３度のうちの１つ又は複数のピークを有するＸ線粉末回折パターンを有する、請求項１〜４のいずれかに記載の医薬組成物。
- 無水（２Ｓ，３Ｒ，４Ｒ，５Ｓ，６Ｒ）−２−（４−クロロ−３−（４−エトキシベンジル）フェニル）−６−（メチルチオ）テトラヒドロ−２Ｈ−ピラン−３，４，５−トリオールの結晶が、１４．０°の２θ±０．３度のピークを有するＸ線粉末回折パターンを有する、請求項６に記載の医薬組成物。
- 無水（２Ｓ，３Ｒ，４Ｒ，５Ｓ，６Ｒ）−２−（４−クロロ−３−（４−エトキシベンジル）フェニル）−６−（メチルチオ）テトラヒドロ−２Ｈ−ピラン−３，４，５−トリオールの結晶が、３０６８ｃｍ −１ 、２９２９ｃｍ −１ 、２８８８ｃｍ −１ 、２８８１ｃｍ −１ 、１６１５ｃｍ −１ 、１６０３ｃｍ −１ 、１２４４ｃｍ −１ 、１０３７ｃｍ −１ 、６９２ｃｍ −１ 及び／又は３７２ｃｍ −１ のうちの１つ又は複数のピークを有するラマンスペクトルを有する、請求項１〜４のいずれかに記載の医薬組成物。
- 無水（２Ｓ，３Ｒ，４Ｒ，５Ｓ，６Ｒ）−２−（４−クロロ−３−（４−エトキシベンジル）フェニル）−６−（メチルチオ）テトラヒドロ−２Ｈ−ピラン−３，４，５−トリオールの結晶が、１３４℃±５．０℃のＤＳＣ吸熱を有する、請求項１〜４のいずれかに記載の医薬組成物。
- 無水（２Ｓ，３Ｒ，４Ｒ，５Ｓ，６Ｒ）−２−（４−クロロ−３−（４−エトキシベンジル）フェニル）−６−（メチルチオ）テトラヒドロ−２Ｈ−ピラン−３，４，５−トリオールの結晶が、４．４°、４．８°、１４．５°、１４．７°、１５．５°、２１．２°、２２．１°及び／又は２３．８°の２θ±０．３度のうちの１つ又は複数のピークを有するＸ線粉末回折パターンを有する、請求項１〜４のいずれかに記載の医薬組成物。
- 無水（２Ｓ，３Ｒ，４Ｒ，５Ｓ，６Ｒ）−２−（４−クロロ−３−（４−エトキシベンジル）フェニル）−６−（メチルチオ）テトラヒドロ−２Ｈ−ピラン−３，４，５−トリオールの結晶が、４．４°の２θ±０．３度のピークを有するＸ線粉末回折パターンを有する、請求項１０に記載の医薬組成物。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8142308P | 2008-07-17 | 2008-07-17 | |
| US61/081,423 | 2008-07-17 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011518868A Division JP2011528366A (ja) | 2008-07-17 | 2009-07-15 | （２ｓ，３ｒ，４ｒ，５ｓ，６ｒ）−２−（４−クロロ−３−（４−エトキシベンジル）フェニル）−６−（メチルチオ）テトラヒドロ−２ｈ−ピラン−３，４，５−トリオールの固体形態及びその使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016041701A JP2016041701A (ja) | 2016-03-31 |
| JP2016041701A5 true JP2016041701A5 (ja) | 2016-12-28 |
| JP6283337B2 JP6283337B2 (ja) | 2018-02-21 |
Family
ID=41137707
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011518868A Pending JP2011528366A (ja) | 2008-07-17 | 2009-07-15 | （２ｓ，３ｒ，４ｒ，５ｓ，６ｒ）−２−（４−クロロ−３−（４−エトキシベンジル）フェニル）−６−（メチルチオ）テトラヒドロ−２ｈ−ピラン−３，４，５−トリオールの固体形態及びその使用方法 |
| JP2015193990A Active JP6283337B2 (ja) | 2008-07-17 | 2015-09-30 | （２ｓ，３ｒ，４ｒ，５ｓ，６ｒ）−２−（４−クロロ−３−（４−エトキシベンジル）フェニル）−６−（メチルチオ）テトラヒドロ−２ｈ−ピラン−３，４，５−トリオールの固体形態及びその使用方法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011518868A Pending JP2011528366A (ja) | 2008-07-17 | 2009-07-15 | （２ｓ，３ｒ，４ｒ，５ｓ，６ｒ）−２−（４−クロロ−３−（４−エトキシベンジル）フェニル）−６−（メチルチオ）テトラヒドロ−２ｈ−ピラン−３，４，５−トリオールの固体形態及びその使用方法 |
Country Status (29)
| Country | Link |
|---|---|
| US (2) | US8217156B2 (ja) |
| EP (1) | EP2332947B1 (ja) |
| JP (2) | JP2011528366A (ja) |
| KR (2) | KR101707246B1 (ja) |
| CN (2) | CN107629097A (ja) |
| AR (1) | AR072807A1 (ja) |
| AU (1) | AU2009270973B2 (ja) |
| BR (1) | BRPI0916191A2 (ja) |
| CA (1) | CA2730931A1 (ja) |
| CL (1) | CL2009001595A1 (ja) |
| CO (1) | CO6351797A2 (ja) |
| DK (1) | DK2332947T3 (ja) |
| ES (1) | ES2656357T3 (ja) |
| HK (1) | HK1243713A1 (ja) |
| HU (1) | HUE035400T2 (ja) |
| IL (1) | IL210269A (ja) |
| MX (1) | MX2011000503A (ja) |
| NO (1) | NO2332947T3 (ja) |
| NZ (1) | NZ590184A (ja) |
| PE (1) | PE20100260A1 (ja) |
| PL (1) | PL2332947T3 (ja) |
| PT (1) | PT2332947T (ja) |
| RU (1) | RU2505543C2 (ja) |
| SG (1) | SG185317A1 (ja) |
| TW (1) | TWI472521B (ja) |
| UA (1) | UA106048C2 (ja) |
| UY (1) | UY31992A (ja) |
| WO (1) | WO2010009197A1 (ja) |
| ZA (1) | ZA201100175B (ja) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| BRPI0813840A2 (pt) | 2007-07-26 | 2017-06-06 | Lexicon Pharmaceuticals Inc | métodos e compostos úteis para a preparação de inibidores de cotransportador 2 de glicose de sódio |
| MX2011000637A (es) | 2008-07-15 | 2011-05-02 | Theracos Inc | Derivados deuretados de bencilbenceno y metodos de uso. |
| 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 |
| TWI562775B (en) * | 2010-03-02 | 2016-12-21 | Lexicon Pharmaceuticals Inc | Methods of using inhibitors of sodium-glucose cotransporters 1 and 2 |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| CN102453026A (zh) | 2010-10-27 | 2012-05-16 | 上海艾力斯医药科技有限公司 | C-芳基葡糖苷衍生物、制备方法及其应用 |
| TWI631963B (zh) * | 2011-01-05 | 2018-08-11 | 雷西肯製藥股份有限公司 | 包含鈉－葡萄糖共同輸送體１與２之抑制劑的組合物與應用方法 |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| DK2925735T3 (da) * | 2012-11-20 | 2019-06-17 | Lexicon Pharmaceuticals Inc | Inhibitorer for natriumglucose-cotransporter 1 |
| US20160272645A1 (en) | 2013-10-18 | 2016-09-22 | Medivation Technologies, Inc. | Heterocyclic Compounds and Methods of Use |
| WO2015058084A1 (en) | 2013-10-18 | 2015-04-23 | Medivation Technologies, Inc. | Heterocyclic compounds and methods of use |
| JP6938376B2 (ja) | 2015-07-30 | 2021-09-22 | 公益財団法人微生物化学研究会 | 多剤耐性菌に有効な新規アミノグリコシド抗生物質 |
| 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 |
| WO2018067805A1 (en) | 2016-10-06 | 2018-04-12 | Teva Pharmaceutical Industries Ltd. | Solid state forms of sotagliflozin |
| EP3528800A1 (en) | 2016-10-19 | 2019-08-28 | Boehringer Ingelheim International GmbH | Combinations comprising an ssao/vap-1 inhibitor and a sglt2 inhibitor, uses thereof |
| EP3781166A1 (en) | 2018-04-17 | 2021-02-24 | Boehringer Ingelheim International GmbH | Pharmaceutical composition, methods for treating and uses thereof |
| 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 |
| JP2022502393A (ja) * | 2018-09-26 | 2022-01-11 | レクシコン ファーマシューティカルズ インコーポレイテッド | Ｎ−（１−（（２−（ジメチルアミノ）エチル）アミノ）−２−メチル−１−オキソプロパン−２−イル）−４−（４−（２−メチル−５−（（２ｓ，３ｒ，４ｒ，５ｓ，６ｒ）−３，４，５−トリヒドロキシ−６−（メチルチオ）テトラヒドロ−２ｈ−ピラン−２−イル）ベンジル）フェニル）ブタンアミドの結晶形態及びそれらの合成方法 |
| EP3873599B1 (en) | 2018-10-29 | 2023-09-27 | Boehringer Ingelheim International GmbH | Pyridinyl sulfonamide derivatives, pharmaceutical compositions and uses thereof |
| FI3873600T3 (fi) | 2018-10-29 | 2023-12-07 | Boehringer Ingelheim Int | Pyridinyylisulfonamidijohdannaisia, farmaseuttisia koostumuksia ja niiden käytöt |
| CN109824687B (zh) * | 2019-03-26 | 2022-03-22 | 上海凌凯医药科技有限公司 | 呋喃木糖衍生物的新合成方法 |
| US20220324897A1 (en) * | 2019-07-05 | 2022-10-13 | Shandong Danhong Pharmaceutical Co., Ltd. | Crystal form of sglt inhibitor and application thereof |
| EP3771480A1 (en) | 2019-08-01 | 2021-02-03 | Lexicon Pharmaceuticals, Inc. | Continuous process for preparing the crystalline form ii of sotagliflozin |
| EP3771718A1 (en) | 2019-08-01 | 2021-02-03 | Lexicon Pharmaceuticals, Inc. | Process for preparing the crystalline form ii of sotagliflozin |
| 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 |
| CN113880701A (zh) * | 2021-10-10 | 2022-01-04 | 浙江司太立制药股份有限公司 | 一种抗糖尿病药物中间体及其制备方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3870699A (en) * | 1973-03-06 | 1975-03-11 | Upjohn Co | Lincomycin analogs |
| JP2003519698A (ja) * | 2000-01-07 | 2003-06-24 | トランスフォーム ファーマスーティカルズ，インコーポレイテッド | 多様な固体形態のハイスループットでの形成、同定および分析 |
| WO2006018150A1 (de) | 2004-08-11 | 2006-02-23 | Boehringer Ingelheim International Gmbh | D-xylopyranosyl-phenyl-substituierte cyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung |
| ATE445608T1 (de) | 2005-02-23 | 2009-10-15 | Boehringer Ingelheim Int | Glucopyranosylsubstituierte ((hetero)arylethynyl- benzyl)-benzenderivative und deren verwendung als inhibitoren des natriumabhängigen glucose- cotransporters typ 2 (sglt2) |
| CN1820858A (zh) * | 2006-03-10 | 2006-08-23 | 广西中医学院制药厂 | 多相物料喷雾方法及装置 |
| 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 |
| BRPI0813840A2 (pt) * | 2007-07-26 | 2017-06-06 | Lexicon Pharmaceuticals Inc | métodos e compostos úteis para a preparação de inibidores de cotransportador 2 de glicose de sódio |
| 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 |
-
2009
- 2009-07-01 TW TW98122274A patent/TWI472521B/zh active
- 2009-07-15 HU HUE11155100A patent/HUE035400T2/en unknown
- 2009-07-15 SG SG2012077681A patent/SG185317A1/en unknown
- 2009-07-15 NO NO11155100A patent/NO2332947T3/no unknown
- 2009-07-15 BR BRPI0916191A patent/BRPI0916191A2/pt not_active Application Discontinuation
- 2009-07-15 KR KR1020117001024A patent/KR101707246B1/ko active IP Right Grant
- 2009-07-15 PE PE2009000944A patent/PE20100260A1/es not_active Application Discontinuation
- 2009-07-15 JP JP2011518868A patent/JP2011528366A/ja active Pending
- 2009-07-15 ES ES11155100.8T patent/ES2656357T3/es active Active
- 2009-07-15 EP EP11155100.8A patent/EP2332947B1/en active Active
- 2009-07-15 CN CN201710477527.7A patent/CN107629097A/zh not_active Withdrawn
- 2009-07-15 PL PL11155100T patent/PL2332947T3/pl unknown
- 2009-07-15 RU RU2011105797/04A patent/RU2505543C2/ru active
- 2009-07-15 NZ NZ590184A patent/NZ590184A/xx unknown
- 2009-07-15 WO PCT/US2009/050636 patent/WO2010009197A1/en active Application Filing
- 2009-07-15 UA UAA201101832A patent/UA106048C2/uk unknown
- 2009-07-15 AU AU2009270973A patent/AU2009270973B2/en active Active
- 2009-07-15 AR ARP090102685A patent/AR072807A1/es unknown
- 2009-07-15 US US12/503,225 patent/US8217156B2/en active Active
- 2009-07-15 CL CL2009001595A patent/CL2009001595A1/es unknown
- 2009-07-15 DK DK11155100.8T patent/DK2332947T3/da active
- 2009-07-15 PT PT111551008T patent/PT2332947T/pt unknown
- 2009-07-15 CA CA2730931A patent/CA2730931A1/en not_active Abandoned
- 2009-07-15 KR KR1020177001061A patent/KR20170010069A/ko not_active Application Discontinuation
- 2009-07-15 MX MX2011000503A patent/MX2011000503A/es active IP Right Grant
- 2009-07-15 CN CN2009801279245A patent/CN102112483A/zh active Pending
- 2009-07-16 UY UY0001031992A patent/UY31992A/es not_active Application Discontinuation
-
2010
- 2010-12-26 IL IL210269A patent/IL210269A/en active IP Right Grant
-
2011
- 2011-01-06 ZA ZA2011/00175A patent/ZA201100175B/en unknown
- 2011-02-09 CO CO11014849A patent/CO6351797A2/es not_active Application Discontinuation
-
2012
- 2012-06-22 US US13/530,645 patent/US9067962B2/en active Active
-
2015
- 2015-09-30 JP JP2015193990A patent/JP6283337B2/ja active Active
-
2018
- 2018-03-02 HK HK18103068.1A patent/HK1243713A1/zh unknown
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