RU2010126230A - Моносебацинат производного пиразола - Google Patents
Моносебацинат производного пиразола Download PDFInfo
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- RU2010126230A RU2010126230A RU2010126230/04A RU2010126230A RU2010126230A RU 2010126230 A RU2010126230 A RU 2010126230A RU 2010126230/04 A RU2010126230/04 A RU 2010126230/04A RU 2010126230 A RU2010126230 A RU 2010126230A RU 2010126230 A RU2010126230 A RU 2010126230A
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
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- 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
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- 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
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- 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
- A61P3/06—Antihyperlipidemics
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
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- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Emergency Medicine (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
1. Соединение, представленное структурной формулой: ! [Хим.1] ! ! 2. Соединение по п.1, которое является кристаллическим. ! 3. Соединение по п.2, которое имеет характеристические пики при углах дифракции (2θ (°)) 7,6±0,1, 8,5±0,1, 10,6±0,1, 12,8±0,1 и 17,6±0,1 на порошковой рентгеновской дифрактограмме. ! 4. Соединение по п.2, которое имеет эндотермический пик около 130°С на термограмме дифференциальной сканирующей калориметрии. ! 5. Соединение по п.2, которое имеет характеристические пики при значениях химического сдвига (δ (м.д.)) 101,4±0,2, 100,9±0,2, 82,8±0,2, 74,2±0,2, 40,9±0,2, 25,5±0,2, 23,1±0,2 и 22,3±0,2 на твердофазном 13C-ЯМР-спектре. ! 6. Фармацевтическая композиция, которая содержит в качестве активного ингредиента соединение по любому из пп.1-5. ! 7. Фармацевтическая композиция по п.6 для предупреждения или лечения заболевания, связанного с гипергликемией, или заболевания, связанного с повышением уровня галактозы в крови. ! 8. Лекарственное средство, которое содержит соединение по любому из пп.1-5 в комбинации с любым из производных сульфонилмочевины и глинидов. ! 9. Лекарственное средство по п.8, которое содержит соединение по любому из пп.1-5 в комбинации либо с гликлазидом, либо с гидратом митиглинида кальция. ! 10. Лекарственное средство по п.8 или 9 для предупреждения или лечения заболевания, связанного с гипергликемией.
Claims (10)
1. Соединение, представленное структурной формулой:
[Хим.1]
2. Соединение по п.1, которое является кристаллическим.
3. Соединение по п.2, которое имеет характеристические пики при углах дифракции (2θ (°)) 7,6±0,1, 8,5±0,1, 10,6±0,1, 12,8±0,1 и 17,6±0,1 на порошковой рентгеновской дифрактограмме.
4. Соединение по п.2, которое имеет эндотермический пик около 130°С на термограмме дифференциальной сканирующей калориметрии.
5. Соединение по п.2, которое имеет характеристические пики при значениях химического сдвига (δ (м.д.)) 101,4±0,2, 100,9±0,2, 82,8±0,2, 74,2±0,2, 40,9±0,2, 25,5±0,2, 23,1±0,2 и 22,3±0,2 на твердофазном 13C-ЯМР-спектре.
6. Фармацевтическая композиция, которая содержит в качестве активного ингредиента соединение по любому из пп.1-5.
7. Фармацевтическая композиция по п.6 для предупреждения или лечения заболевания, связанного с гипергликемией, или заболевания, связанного с повышением уровня галактозы в крови.
8. Лекарственное средство, которое содержит соединение по любому из пп.1-5 в комбинации с любым из производных сульфонилмочевины и глинидов.
9. Лекарственное средство по п.8, которое содержит соединение по любому из пп.1-5 в комбинации либо с гликлазидом, либо с гидратом митиглинида кальция.
10. Лекарственное средство по п.8 или 9 для предупреждения или лечения заболевания, связанного с гипергликемией.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2007-337985 | 2007-12-27 | ||
| JP2007337985 | 2007-12-27 | ||
| PCT/JP2008/073405 WO2009084531A1 (ja) | 2007-12-27 | 2008-12-24 | ピラゾール誘導体のモノセバシン酸塩 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2010126230A true RU2010126230A (ru) | 2011-12-27 |
| RU2482122C2 RU2482122C2 (ru) | 2013-05-20 |
Family
ID=40824245
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2010126230/04A RU2482122C2 (ru) | 2007-12-27 | 2008-12-24 | Моносебацинат производного пиразола |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8399418B2 (ru) |
| EP (1) | EP2228378B1 (ru) |
| JP (1) | JP5144683B2 (ru) |
| KR (1) | KR101416561B1 (ru) |
| CN (1) | CN101910189B (ru) |
| AU (1) | AU2008344436B2 (ru) |
| BR (1) | BRPI0821773B8 (ru) |
| CA (1) | CA2709530C (ru) |
| ES (1) | ES2548578T3 (ru) |
| IL (1) | IL206576A (ru) |
| MX (1) | MX2010007154A (ru) |
| NZ (1) | NZ586336A (ru) |
| RU (1) | RU2482122C2 (ru) |
| TW (1) | TWI426914B (ru) |
| WO (1) | WO2009084531A1 (ru) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5467040B2 (ja) * | 2008-04-16 | 2014-04-09 | キッセイ薬品工業株式会社 | ピラゾール誘導体の１／２フマル酸塩 |
| WO2011002011A1 (ja) * | 2009-07-01 | 2011-01-06 | キッセイ薬品工業株式会社 | Sglt1阻害薬とdpp-iv阻害薬を組み合わせてなる医薬 |
| JPWO2011002001A1 (ja) * | 2009-07-01 | 2012-12-13 | キッセイ薬品工業株式会社 | ピラゾール誘導体とビグアナイド薬との組み合わせ医薬 |
| TW201105337A (en) * | 2009-07-01 | 2011-02-16 | Dainippon Sumitomo Pharma Co | Medicine derived from a combination of SGLT1-inhibitor and insulin sensitizer |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| 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 |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| 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 |
| 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 |
| EP2760862B1 (en) | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| PL2848254T3 (pl) | 2012-05-07 | 2017-03-31 | Kissei Pharmaceutical Co., Ltd. | Pochodne pirazolu i ich zastosowanie w celach medycznych |
| UA113086C2 (xx) | 2012-05-10 | 2016-12-12 | Піразольні сполуки як інгібітори sglt1 | |
| TW201425326A (zh) | 2012-10-05 | 2014-07-01 | Lilly Co Eli | 新穎脲化合物 |
| KR102078433B1 (ko) | 2013-02-04 | 2020-02-17 | 다이쇼 세이야꾸 가부시끼가이샤 | 변비증의 예방 또는 치료약 |
| AR098670A1 (es) | 2013-11-08 | 2016-06-08 | Lilly Co Eli | Inhibidor de sglt1 |
| MX2020009349A (es) | 2018-03-28 | 2021-04-28 | Avolynt | Método para el tratamiento de la hipoglucemia posprandial. |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2432145C (en) * | 2000-12-28 | 2010-07-13 | Kissei Pharmaceutical Co., Ltd. | Glucopyranosyloxypyrazole derivatives and use thereof in medicines |
| ES2345250T3 (es) * | 2002-08-08 | 2010-09-20 | Kissei Pharmaceutical Co., Ltd. | Derivado de pirazol en la composicion medicinal que contiene el mismo, el uso medicinal del mismo, y un intermedio para la produccion del mismo. |
| JP2004137245A (ja) | 2002-08-23 | 2004-05-13 | Kissei Pharmaceut Co Ltd | ピラゾール誘導体、それを含有する医薬組成物、その医薬用途及びその製造中間体 |
| ZA200501549B (en) * | 2002-08-23 | 2006-07-26 | Kissei Pharmaceutical | Pyrazole derivatives, medicinal composition containing the same, medicinal use thereof and intermediate for the production thereof |
| WO2004019958A1 (ja) * | 2002-08-27 | 2004-03-11 | Kissei Pharmaceutical Co., Ltd. | ピラゾール誘導体、それを含有する医薬組成物及びその医薬用途 |
| AU2003267773A1 (en) * | 2003-10-14 | 2005-04-27 | Council Of Scientific And Industrial Research | (3r, 4r)-trans-3,4-diarylchroman derivatives with estrogenic activity |
| US20060111560A1 (en) * | 2004-11-01 | 2006-05-25 | Glenmark Pharmaceuticals Limited | Process for the preparation of crystalline form II of clarithromycin |
| WO2006097849A1 (en) * | 2005-01-14 | 2006-09-21 | Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. | 9a-carbamoyl and thiocarbamoyl azalides with anti-inflammatory activity |
| AR054425A1 (es) | 2005-01-21 | 2007-06-27 | Astex Therapeutics Ltd | Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico. |
| CN101146791B (zh) * | 2005-01-21 | 2013-01-09 | 阿斯泰克斯治疗有限公司 | 作为激酶抑制剂的4-(2，6-二氯-苯甲酰基氨基)-1h-吡唑-3-甲酸哌啶-4-基酰胺的酸加成盐 |
| JP2008546751A (ja) * | 2005-06-22 | 2008-12-25 | アステックス・セラピューティクス・リミテッド | 医薬組成物 |
| UY30082A1 (es) * | 2006-01-11 | 2007-08-31 | Boehringer Ingelheim Int | Forma cristalina de 1-(1-metiletil)-4`-((2-fluoro-4-metoxifenil)metil)-5`- metil-1h-pirazol-3`-o-b-d-glucopiranosido, un metodo para su preparacion y el uso de la misma para preparar medicamentos |
-
2008
- 2008-12-24 BR BRPI0821773A patent/BRPI0821773B8/pt active IP Right Grant
- 2008-12-24 AU AU2008344436A patent/AU2008344436B2/en active Active
- 2008-12-24 NZ NZ586336A patent/NZ586336A/en unknown
- 2008-12-24 ES ES08867231.6T patent/ES2548578T3/es active Active
- 2008-12-24 US US12/810,476 patent/US8399418B2/en active Active
- 2008-12-24 CA CA2709530A patent/CA2709530C/en active Active
- 2008-12-24 KR KR1020107014837A patent/KR101416561B1/ko not_active Expired - Fee Related
- 2008-12-24 WO PCT/JP2008/073405 patent/WO2009084531A1/ja not_active Ceased
- 2008-12-24 JP JP2009548041A patent/JP5144683B2/ja active Active
- 2008-12-24 RU RU2010126230/04A patent/RU2482122C2/ru active
- 2008-12-24 MX MX2010007154A patent/MX2010007154A/es active IP Right Grant
- 2008-12-24 CN CN2008801230728A patent/CN101910189B/zh active Active
- 2008-12-24 EP EP08867231.6A patent/EP2228378B1/en active Active
- 2008-12-26 TW TW097150903A patent/TWI426914B/zh not_active IP Right Cessation
-
2010
- 2010-06-23 IL IL206576A patent/IL206576A/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| CN101910189B (zh) | 2013-06-19 |
| WO2009084531A1 (ja) | 2009-07-09 |
| EP2228378A4 (en) | 2014-05-28 |
| TW200934504A (en) | 2009-08-16 |
| CN101910189A (zh) | 2010-12-08 |
| NZ586336A (en) | 2011-06-30 |
| CA2709530A1 (en) | 2009-07-02 |
| BRPI0821773B8 (pt) | 2021-05-25 |
| KR101416561B1 (ko) | 2014-07-08 |
| US20100279962A1 (en) | 2010-11-04 |
| CA2709530C (en) | 2016-02-23 |
| KR20100102140A (ko) | 2010-09-20 |
| MX2010007154A (es) | 2010-10-05 |
| RU2482122C2 (ru) | 2013-05-20 |
| BRPI0821773B1 (pt) | 2020-05-19 |
| JPWO2009084531A1 (ja) | 2011-05-19 |
| HK1147100A1 (en) | 2011-07-29 |
| AU2008344436B2 (en) | 2013-08-29 |
| US8399418B2 (en) | 2013-03-19 |
| BRPI0821773A2 (pt) | 2015-06-16 |
| TWI426914B (zh) | 2014-02-21 |
| EP2228378B1 (en) | 2015-09-09 |
| EP2228378A1 (en) | 2010-09-15 |
| ES2548578T3 (es) | 2015-10-19 |
| IL206576A0 (en) | 2010-12-30 |
| JP5144683B2 (ja) | 2013-02-13 |
| IL206576A (en) | 2014-02-27 |
| AU2008344436A1 (en) | 2009-07-09 |
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