JP2018115191A5 - - Google Patents
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- Publication number
- JP2018115191A5 JP2018115191A5 JP2018055962A JP2018055962A JP2018115191A5 JP 2018115191 A5 JP2018115191 A5 JP 2018115191A5 JP 2018055962 A JP2018055962 A JP 2018055962A JP 2018055962 A JP2018055962 A JP 2018055962A JP 2018115191 A5 JP2018115191 A5 JP 2018115191A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline
- crystal
- crystalline form
- dihydropyrrolo
- difluorophenyl
- 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.)
- Withdrawn
Links
- 239000013078 crystal Substances 0.000 claims 4
- -1 2,5-difluorophenyl Chemical group 0.000 claims 2
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 2
- 238000005481 NMR spectroscopy Methods 0.000 claims 2
- 238000000113 differential scanning calorimetry Methods 0.000 claims 2
- 230000008018 melting Effects 0.000 claims 2
- 238000002844 melting Methods 0.000 claims 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 2
- WUUOEJJGRCQGBQ-UHFFFAOYSA-N oxan-3-amine Chemical compound NC1CCCOC1 WUUOEJJGRCQGBQ-UHFFFAOYSA-N 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 238000002411 thermogravimetry Methods 0.000 claims 2
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000008186 active pharmaceutical agent Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 239000002178 crystalline material Substances 0.000 claims 1
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000008025 crystallization Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940088679 drug related substance Drugs 0.000 claims 1
- JMMWKPVZQRWMSS-UHFFFAOYSA-N isopropanol acetate Natural products CC(C)OC(C)=O JMMWKPVZQRWMSS-UHFFFAOYSA-N 0.000 claims 1
- 229940011051 isopropyl acetate Drugs 0.000 claims 1
- GWYFCOCPABKNJV-UHFFFAOYSA-N isovaleric acid Chemical compound CC(C)CC(O)=O GWYFCOCPABKNJV-UHFFFAOYSA-N 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000004580 weight loss Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161502497P | 2011-06-29 | 2011-06-29 | |
| US61/502,497 | 2011-06-29 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016198829A Division JP2017039752A (ja) | 2011-06-29 | 2016-10-07 | ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018115191A JP2018115191A (ja) | 2018-07-26 |
| JP2018115191A5 true JP2018115191A5 (enExample) | 2018-09-06 |
Family
ID=47424494
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014518880A Active JP5873554B2 (ja) | 2011-06-29 | 2012-06-25 | キラルジペプチジルペプチダーゼ−ｉｖ阻害剤の調製プロセス |
| JP2014518879A Pending JP2014518266A (ja) | 2011-06-29 | 2012-06-25 | ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形 |
| JP2016198829A Pending JP2017039752A (ja) | 2011-06-29 | 2016-10-07 | ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形 |
| JP2018055962A Withdrawn JP2018115191A (ja) | 2011-06-29 | 2018-03-23 | ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形 |
Family Applications Before (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014518880A Active JP5873554B2 (ja) | 2011-06-29 | 2012-06-25 | キラルジペプチジルペプチダーゼ−ｉｖ阻害剤の調製プロセス |
| JP2014518879A Pending JP2014518266A (ja) | 2011-06-29 | 2012-06-25 | ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形 |
| JP2016198829A Pending JP2017039752A (ja) | 2011-06-29 | 2016-10-07 | ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形 |
Country Status (12)
| Country | Link |
|---|---|
| US (4) | US8895603B2 (enExample) |
| EP (2) | EP2726075A4 (enExample) |
| JP (4) | JP5873554B2 (enExample) |
| KR (2) | KR20140034862A (enExample) |
| CN (3) | CN106946886A (enExample) |
| AR (1) | AR089554A1 (enExample) |
| AU (2) | AU2012275638A1 (enExample) |
| CA (2) | CA2838738A1 (enExample) |
| MX (2) | MX2013014892A (enExample) |
| RU (2) | RU2014102764A (enExample) |
| TW (1) | TWI574965B (enExample) |
| WO (2) | WO2013003249A1 (enExample) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8895603B2 (en) | 2011-06-29 | 2014-11-25 | Merck Sharp & Dohme Corp. | Crystalline forms of a dipeptidyl peptidase-IV inhibitor |
| WO2013122920A1 (en) | 2012-02-17 | 2013-08-22 | Merck Sharp & Dohme Corp. | Dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes |
| EP2874622A4 (en) | 2012-07-23 | 2015-12-30 | Merck Sharp & Dohme | TREATMENT OF DIABETES WITH DIPEPTIDYLPEPTIDASE IV INHIBITORS |
| WO2014018355A1 (en) | 2012-07-23 | 2014-01-30 | Merck Sharp & Dohme Corp. | Treating diabetes with dipeptidyl peptidase-iv inhibitors |
| TWI500613B (zh) | 2012-10-17 | 2015-09-21 | Cadila Healthcare Ltd | 新穎之雜環化合物 |
| US9937153B2 (en) | 2013-08-30 | 2018-04-10 | Merck Sharp & Dohme Ltd. | Oral pharmaceutical formulation of omarigliptin |
| EP2997008B1 (en) | 2014-03-20 | 2016-06-29 | F.I.S.- Fabbrica Italiana Sintetici S.p.A. | Process for the preparation of key intermediates of omarigliptin |
| CN105037367A (zh) * | 2014-04-18 | 2015-11-11 | 四川海思科制药有限公司 | 氨基六元环类衍生物及其在医药上的应用 |
| CN105085528A (zh) * | 2014-05-15 | 2015-11-25 | 成都贝斯凯瑞生物科技有限公司 | 作为二肽基肽酶-iv抑制剂的氨基四氢吡喃衍生物 |
| JP6574474B2 (ja) * | 2014-07-21 | 2019-09-11 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | キラルジペプチジルペプチダーゼ−ｉｖ阻害剤の製造方法 |
| CN106660981B (zh) * | 2014-07-29 | 2019-06-25 | 广东东阳光药业有限公司 | 2,3-二取代-5-氧代吡喃化合物的制备方法 |
| CN106316888B (zh) * | 2015-06-29 | 2018-05-18 | 深圳翰宇药业股份有限公司 | 一种手性氨基吡喃酮类化合物的合成方法 |
| WO2017032705A1 (en) | 2015-08-25 | 2017-03-02 | Sandoz Ag | Crystalline form of omarigliptin |
| CN105130995B (zh) * | 2015-09-09 | 2017-08-11 | 杭州成邦医药科技有限公司 | 吡咯酮类化合物及其制备方法和应用 |
| WO2017081590A1 (en) * | 2015-11-09 | 2017-05-18 | Sun Pharmaceutical Industries Limited | Process for the preparation of omarigliptin |
| CN105348286B (zh) * | 2015-11-25 | 2018-12-18 | 中山奕安泰医药科技有限公司 | 一种2-甲基磺酰基-2,4,5,6-四氢吡咯[3，4-c]吡唑苯磺酸盐的制备方法 |
| WO2017093209A1 (en) | 2015-12-03 | 2017-06-08 | F.I.S. - Fabbrica Italiana Sintetici S.P.A. | Process for preparing aminotetrahydropyrans |
| CN105399744B (zh) * | 2015-12-17 | 2017-07-18 | 黄燕鸽 | 一种奥格列汀的合成方法 |
| EP3181565A1 (en) | 2015-12-18 | 2017-06-21 | Sandoz Ag | Crystalline omarigliptin salts |
| EP3395819B1 (en) * | 2015-12-25 | 2023-05-31 | Sichuan Haisco Pharmaceutical Co., Ltd. | Crystal form of substituted aminopyran derivative |
| CN106928228B (zh) * | 2015-12-29 | 2019-08-30 | 杭州普晒医药科技有限公司 | 奥格列汀盐及其晶型、它们的制备方法和药物组合物 |
| CN107652291B (zh) * | 2016-07-26 | 2020-07-14 | 中国科学院上海药物研究所 | 一种制备手性四氢吡喃衍生物的方法 |
| EP3498704A4 (en) * | 2016-08-12 | 2020-03-04 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | LONG-ACTING DPP-IV INHIBITOR CRYSTAL AND ITS SALT |
| CN107793389B (zh) * | 2016-09-05 | 2021-06-29 | 中国科学院上海药物研究所 | 手性四氢吡喃衍生物及其制备与用途 |
| KR102599958B1 (ko) * | 2016-09-28 | 2023-11-09 | (주)아모레퍼시픽 | (r)-n-[4-(1-아미노-에틸)-2,6-다이플루오로-페닐]-메테인설폰아마이드의 제조방법 |
| CN106674227B (zh) * | 2016-12-06 | 2019-03-19 | 上海博志研新药物技术有限公司 | 一种奥格列汀及其中间体的制备方法 |
| EP3335703A1 (en) | 2016-12-16 | 2018-06-20 | Hexal AG | Pharmaceutical composition comprising omarigliptin |
| EP3335701A1 (en) | 2016-12-16 | 2018-06-20 | Hexal AG | Pharmaceutical composition comprising omarigliptin |
| EP3335704A1 (en) | 2016-12-16 | 2018-06-20 | Hexal AG | Pharmaceutical composition comprising omarigliptin |
| KR102007135B1 (ko) | 2017-03-20 | 2019-08-02 | 포르마 세라퓨틱스 인크. | 피루베이트 키나제 (pkr) 활성화제로서의 피롤로피롤 조성물 |
| EP3852791B1 (en) | 2018-09-19 | 2024-07-03 | Novo Nordisk Health Care AG | Activating pyruvate kinase r |
| US20200129485A1 (en) | 2018-09-19 | 2020-04-30 | Forma Therapeutics, Inc. | Treating sickle cell disease with a pyruvate kinase r activating compound |
| CN113831266B (zh) * | 2019-01-22 | 2024-04-05 | 河南医学高等专科学校 | 1-(2,5-二氟苯基)-1-氧代戊-4-炔-2-基氨基甲酸烷基酯的合成 |
| CN110453177A (zh) * | 2019-08-06 | 2019-11-15 | 太仓碧奇新材料研发有限公司 | 一种柔性有机整流器的制备方法 |
| US20220378756A1 (en) | 2019-09-19 | 2022-12-01 | Forma Therapeutics, Inc. | Activating pyruvate kinase r |
| CN111793071B (zh) * | 2020-07-06 | 2021-06-04 | 四川凯科医药科技有限公司 | 奥格列汀的合成工艺 |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
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-
2012
- 2012-06-25 US US14/118,998 patent/US8895603B2/en active Active
- 2012-06-25 AU AU2012275638A patent/AU2012275638A1/en not_active Abandoned
- 2012-06-25 EP EP12803996.3A patent/EP2726075A4/en not_active Withdrawn
- 2012-06-25 KR KR1020137034363A patent/KR20140034862A/ko not_active Withdrawn
- 2012-06-25 CN CN201610882581.5A patent/CN106946886A/zh active Pending
- 2012-06-25 TW TW101122687A patent/TWI574965B/zh not_active IP Right Cessation
- 2012-06-25 WO PCT/US2012/043922 patent/WO2013003249A1/en not_active Ceased
- 2012-06-25 KR KR1020137034362A patent/KR20140034861A/ko not_active Withdrawn
- 2012-06-25 CN CN201280032077.6A patent/CN103987388A/zh active Pending
- 2012-06-25 MX MX2013014892A patent/MX2013014892A/es not_active Application Discontinuation
- 2012-06-25 US US14/119,063 patent/US9187488B2/en active Active
- 2012-06-25 JP JP2014518880A patent/JP5873554B2/ja active Active
- 2012-06-25 WO PCT/US2012/043924 patent/WO2013003250A1/en not_active Ceased
- 2012-06-25 MX MX2013014891A patent/MX341299B/es active IP Right Grant
- 2012-06-25 CN CN201280032105.4A patent/CN103702562A/zh active Pending
- 2012-06-25 RU RU2014102764/04A patent/RU2014102764A/ru not_active Application Discontinuation
- 2012-06-25 CA CA2838738A patent/CA2838738A1/en not_active Abandoned
- 2012-06-25 CA CA2838748A patent/CA2838748A1/en not_active Abandoned
- 2012-06-25 AU AU2012275637A patent/AU2012275637B2/en not_active Ceased
- 2012-06-25 JP JP2014518879A patent/JP2014518266A/ja active Pending
- 2012-06-25 EP EP12804259.5A patent/EP2725905A4/en not_active Withdrawn
- 2012-06-25 RU RU2014102773/04A patent/RU2598072C2/ru not_active IP Right Cessation
- 2012-06-28 AR ARP120102322A patent/AR089554A1/es unknown
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2014
- 2014-10-06 US US14/507,001 patent/US9181262B2/en active Active
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2015
- 2015-10-02 US US14/873,641 patent/US9527855B2/en active Active
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2016
- 2016-10-07 JP JP2016198829A patent/JP2017039752A/ja active Pending
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2018
- 2018-03-23 JP JP2018055962A patent/JP2018115191A/ja not_active Withdrawn
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