AR089554A1 - Formas cristalinas de un inhibidor de la dipeptidil peptidasa-iv - Google Patents
Formas cristalinas de un inhibidor de la dipeptidil peptidasa-ivInfo
- Publication number
- AR089554A1 AR089554A1 ARP120102322A ARP120102322A AR089554A1 AR 089554 A1 AR089554 A1 AR 089554A1 AR P120102322 A ARP120102322 A AR P120102322A AR P120102322 A ARP120102322 A AR P120102322A AR 089554 A1 AR089554 A1 AR 089554A1
- Authority
- AR
- Argentina
- Prior art keywords
- inhibitor
- crystal forms
- forms
- treatment
- pharmaceutical compositions
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 239000013078 crystal Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 2
- -1 2,5-difluorophenyl Chemical group 0.000 abstract 1
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 abstract 1
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 1
- 230000003389 potentiating effect Effects 0.000 abstract 1
Classifications
-
- 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
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
-
- 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
- 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
-
- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161502497P | 2011-06-29 | 2011-06-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR089554A1 true AR089554A1 (es) | 2014-09-03 |
Family
ID=47424494
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120102322A AR089554A1 (es) | 2011-06-29 | 2012-06-28 | Formas cristalinas de un inhibidor de la dipeptidil peptidasa-iv |
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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| JP5165582B2 (ja) | 2005-12-16 | 2013-03-21 | メルク・シャープ・エンド・ドーム・コーポレイション | ジペプチジルペプチダーゼ−４インヒビターとメトホルミンとを組み合わせた医薬組成物 |
| JP5111398B2 (ja) | 2006-01-25 | 2013-01-09 | メルク・シャープ・エンド・ドーム・コーポレイション | 糖尿病の治療又は予防のためのジペプチジルペプチダーゼｉｖ阻害剤としてのアミノシクロヘキサン類 |
| WO2007097931A2 (en) | 2006-02-15 | 2007-08-30 | Merck & Co., Inc. | Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes |
| TW200806669A (en) * | 2006-03-28 | 2008-02-01 | Merck & Co Inc | Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes |
| CA2652367A1 (en) | 2006-05-16 | 2007-11-29 | Merck & Co., Inc. | Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes |
| JP5232160B2 (ja) | 2006-11-14 | 2013-07-10 | メルク・シャープ・アンド・ドーム・コーポレーション | 糖尿病の治療又は予防のためのジペプチジルペプチダーゼｉｖインヒビターとしての三環式芳香族複素環化合物 |
| JP5313246B2 (ja) | 2007-08-21 | 2013-10-09 | メルク・シャープ・アンド・ドーム・コーポレーション | 糖尿病の治療又は予防のためのジペプチジルペプチダーゼ−ｉｖ阻害剤としてのヘテロシクリル化合物 |
| JO2870B1 (en) * | 2008-11-13 | 2015-03-15 | ميرك شارب اند دوهم كورب | Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes |
| EP2228366B1 (de) | 2009-03-12 | 2011-12-28 | Archimica GmbH | Verfahren zur Herstellung von 2-Amino-4-(halogenalkyl)pyridin-Derivaten durch Cyclisierung geeigneter Nitril-Vorstufen mit Stickstoff-Verbindungen |
| IN2012DN00721A (enExample) * | 2009-09-02 | 2015-06-19 | Merck Sharp & Dohme | |
| US8716482B2 (en) | 2009-09-25 | 2014-05-06 | Merck Sharp & Dohme Corp. | Substituted aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes |
| EP2571876B1 (en) | 2010-05-21 | 2016-09-07 | Merck Sharp & Dohme Corp. | Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes |
| WO2012078448A1 (en) | 2010-12-06 | 2012-06-14 | Schering Corporation | Tricyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors |
| US8907086B2 (en) | 2011-03-03 | 2014-12-09 | Merck Sharp & Dohme Corp. | Fused bicyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors |
| US8895603B2 (en) | 2011-06-29 | 2014-11-25 | Merck Sharp & Dohme Corp. | Crystalline forms of a dipeptidyl peptidase-IV inhibitor |
| WO2013006526A2 (en) | 2011-07-05 | 2013-01-10 | Merck Sharp & Dohme Corp. | Tricyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors |
| JP6480788B2 (ja) * | 2015-04-07 | 2019-03-13 | 株式会社マキタ | 打撃工具 |
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- 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
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- 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
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