RU2008143362A - Сокристаллическая форма производного с-гликозида c l-пролином - Google Patents
Сокристаллическая форма производного с-гликозида c l-пролином Download PDFInfo
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- RU2008143362A RU2008143362A RU2008143362/04A RU2008143362A RU2008143362A RU 2008143362 A RU2008143362 A RU 2008143362A RU 2008143362/04 A RU2008143362/04 A RU 2008143362/04A RU 2008143362 A RU2008143362 A RU 2008143362A RU 2008143362 A RU2008143362 A RU 2008143362A
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- Prior art keywords
- crystalline form
- pharmaceutical composition
- form according
- proline
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- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 title claims abstract 5
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 12
- 206010012601 diabetes mellitus Diseases 0.000 claims abstract 8
- 238000000113 differential scanning calorimetry Methods 0.000 claims abstract 8
- 238000005259 measurement Methods 0.000 claims abstract 8
- -1 1-benzothien-2-ylmethyl Chemical group 0.000 claims abstract 4
- 229930182821 L-proline Natural products 0.000 claims abstract 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims abstract 4
- 229960002429 proline Drugs 0.000 claims abstract 4
- 239000004480 active ingredient Substances 0.000 claims abstract 2
- 239000003795 chemical substances by application Substances 0.000 claims abstract 2
- 238000004519 manufacturing process Methods 0.000 claims abstract 2
- 238000000034 method Methods 0.000 claims abstract 2
- 238000011287 therapeutic dose Methods 0.000 claims abstract 2
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
1. Сокристаллическая форма (1S)-1,5-ангидро-1-[3-(1-бензотиен-2-илметил)-4-фторфенил]-D-глюцита с L-пролином. ! 2. Сокристаллическая форма по п.1, где молярное соотношение (1S)-1,5-ангидро-1-[3-(1-бензотиен-2-илметил)-4-фторфенил]-D-глюцита с L-пролином составляет 1:1. !3. Сокристаллическая форма по п.1, имеющая эндотермический пик от 201 до 203°С, по данным измерений при помощи дифференциальной сканирующей калориметрии (анализа DSC). ! 4. Сокристаллическая форма по п.1, имеющая пики при 2θ(°) 4,14, 8,98, 12,4, 16,5, 17,5, 18,7, 20,5 и 21,5, по данным измерения дифракции рентгеновского излучения на порошке. ! 5. Сокристаллическая форма по п.1, имеющая эндотермический пик от 201 до 203°С, по данным измерений при помощи дифференциальной сканирующей калориметрии (анализа DSC) и пики при 2θ(°) 4,14, 8,98, 12,4, 16,5, 17,5, 18,7, 20,5 и 21,5, по данным измерения дифракции рентгеновского излучения на порошке. ! 6. Фармацевтическая композиция, включающая сокристаллическую форму по любому из пп.1-5 в качестве активного ингредиента. ! 7. Фармацевтическая композиция, полученная с использованием сокристаллической формы по любому из пп.1-5. ! 8. Фармацевтическая композиция по п.6, далее включающая фармацевтически приемлемый наполнитель. ! 9. Фармацевтическая композиция по п.7, далее включающая фармацевтически приемлемый наполнитель. !10. Фармацевтическая композиция по п.6, являющаяся средством для лечения диабета. !11. Фармацевтическая композиция по п.7, являющаяся средством для лечения диабета. !12. Применение сокристаллической формы в соответствии с любым из пп.1-5, для производства средства для лечения диабета. ! 13. Способ лечения диабета, включающий введение пациенту эффективной терапевтической дозы сокристаллич
Claims (13)
1. Сокристаллическая форма (1S)-1,5-ангидро-1-[3-(1-бензотиен-2-илметил)-4-фторфенил]-D-глюцита с L-пролином.
2. Сокристаллическая форма по п.1, где молярное соотношение (1S)-1,5-ангидро-1-[3-(1-бензотиен-2-илметил)-4-фторфенил]-D-глюцита с L-пролином составляет 1:1.
3. Сокристаллическая форма по п.1, имеющая эндотермический пик от 201 до 203°С, по данным измерений при помощи дифференциальной сканирующей калориметрии (анализа DSC).
4. Сокристаллическая форма по п.1, имеющая пики при 2θ(°) 4,14, 8,98, 12,4, 16,5, 17,5, 18,7, 20,5 и 21,5, по данным измерения дифракции рентгеновского излучения на порошке.
5. Сокристаллическая форма по п.1, имеющая эндотермический пик от 201 до 203°С, по данным измерений при помощи дифференциальной сканирующей калориметрии (анализа DSC) и пики при 2θ(°) 4,14, 8,98, 12,4, 16,5, 17,5, 18,7, 20,5 и 21,5, по данным измерения дифракции рентгеновского излучения на порошке.
6. Фармацевтическая композиция, включающая сокристаллическую форму по любому из пп.1-5 в качестве активного ингредиента.
7. Фармацевтическая композиция, полученная с использованием сокристаллической формы по любому из пп.1-5.
8. Фармацевтическая композиция по п.6, далее включающая фармацевтически приемлемый наполнитель.
9. Фармацевтическая композиция по п.7, далее включающая фармацевтически приемлемый наполнитель.
10. Фармацевтическая композиция по п.6, являющаяся средством для лечения диабета.
11. Фармацевтическая композиция по п.7, являющаяся средством для лечения диабета.
12. Применение сокристаллической формы в соответствии с любым из пп.1-5, для производства средства для лечения диабета.
13. Способ лечения диабета, включающий введение пациенту эффективной терапевтической дозы сокристаллической формы по любому из пп.1-5 пациенту.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2006103711 | 2006-04-05 | ||
| JP2006-103711 | 2006-04-05 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2008143362A true RU2008143362A (ru) | 2010-05-10 |
| RU2408595C2 RU2408595C2 (ru) | 2011-01-10 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2008143362/04A RU2408595C2 (ru) | 2006-04-05 | 2007-04-04 | Сокристаллическая форма производного с-гликозида c l-пролином |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8097592B2 (ru) |
| EP (1) | EP2009010A4 (ru) |
| JP (1) | JP5210154B2 (ru) |
| KR (2) | KR101243039B1 (ru) |
| CN (1) | CN101443328B (ru) |
| AU (1) | AU2007232763B2 (ru) |
| BR (1) | BRPI0710581A2 (ru) |
| CA (1) | CA2649022C (ru) |
| IL (1) | IL194512A0 (ru) |
| MX (1) | MX2008012705A (ru) |
| NO (1) | NO20084659L (ru) |
| RU (1) | RU2408595C2 (ru) |
| TW (1) | TWI370818B (ru) |
| WO (1) | WO2007114475A1 (ru) |
| ZA (1) | ZA200809201B (ru) |
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| BRPI0408140B8 (pt) * | 2003-03-14 | 2018-12-11 | Astellas Pharma Inc | derivado de c-glicosídeo ou seu sal, composição farmacêutica e uso do derivado de c-glicosídeo ou seu sal |
| TW200726755A (en) * | 2005-07-07 | 2007-07-16 | Astellas Pharma Inc | A crystalline choline salt of an azulene derivative |
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| JP2023523596A (ja) | 2020-04-22 | 2023-06-06 | バイエル アクチェンゲゼルシャフト | 心血管疾患および/または腎疾患を治療および/または予防するためのフィネレノンとsglt2阻害剤の組み合わせ |
| KR102660615B1 (ko) * | 2020-10-28 | 2024-04-26 | 동방에프티엘(주) | 이프라글리플로진의 신규 공결정 및 이의 제조 방법 |
| CN113234028B (zh) * | 2021-04-29 | 2022-08-26 | 上海大学 | 一种5-氟尿嘧啶与肌氨酸的共晶体及其制备方法与用途 |
| WO2023006718A1 (en) | 2021-07-28 | 2023-02-02 | Boehringer Ingelheim Vetmedica Gmbh | Use of sglt-2 inhibitors for the prevention and/or treatment of cardiac diseases in non-human mammals excluding felines, in particular canines |
| CA3224673A1 (en) | 2021-07-28 | 2023-02-02 | Boehringer Ingelheim Vetmedica Gmbh | Use of sglt-2 inhibitors for the prevention and/or treatment of renal diseases in non-human mammals |
| WO2023006745A1 (en) | 2021-07-28 | 2023-02-02 | Boehringer Ingelheim Vetmedica Gmbh | Use of sglt-2 inhibitors for the prevention and/or treatment of hypertension in non-human mammals |
| JP2025501336A (ja) | 2021-12-30 | 2025-01-17 | ニューアムステルダム ファーマ ベー.フェー. | オビセトラピブとsglt2阻害剤との組み合わせ |
| AU2023277704A1 (en) | 2022-05-25 | 2024-12-05 | Boehringer Ingelheim Vetmedica Gmbh | Aqueous pharmaceutical compositions comprising sglt-2 inhibitors |
| KR20240044194A (ko) * | 2022-09-28 | 2024-04-04 | 주식회사 대웅제약 | 이나보글리플로진의 신규한 공결정 |
| AU2024233233A1 (en) | 2023-03-06 | 2025-09-11 | Boehringer Ingelheim Vetmedica Gmbh | Systems for delivery of liquid pharmaceutical compositions in particular comprising one or more sglt-2 inhibitor(s) |
| TW202446389A (zh) | 2023-04-24 | 2024-12-01 | 荷蘭商新阿姆斯特丹製藥公司 | 非晶形奧比特拉(obicetrapib)與sglt2抑制劑之組合 |
| WO2024240632A1 (en) | 2023-05-24 | 2024-11-28 | Boehringer Ingelheim Vetmedica Gmbh | Combination treatment and/or prevention of cardiac diseases in non-human mammals comprising one or more sglt-2 inhibitors and pimobendan and/or telmisartan |
| TW202508455A (zh) | 2023-05-24 | 2025-03-01 | 德商百靈佳殷格翰維美迪加股份有限公司 | 包含一或多種sglt-2抑制劑及替米沙坦(telmisartan)之非人類哺乳動物之腎臟疾病及/或高血壓之組合治療及/或預防 |
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| PH12000002657B1 (en) * | 1999-10-12 | 2006-02-21 | Bristol Myers Squibb Co | C-aryl glucoside SGLT2 inhibitors |
| US6683056B2 (en) * | 2000-03-30 | 2004-01-27 | Bristol-Myers Squibb Company | O-aryl glucoside SGLT2 inhibitors and method |
| WO2002083066A2 (en) * | 2001-04-11 | 2002-10-24 | Bristol-Myers Squibb Company | Amino acid complexes of c-aryl glucosides for treatment of diabetes and method |
| BRPI0408140B8 (pt) * | 2003-03-14 | 2018-12-11 | Astellas Pharma Inc | derivado de c-glicosídeo ou seu sal, composição farmacêutica e uso do derivado de c-glicosídeo ou seu sal |
| LT2896397T (lt) | 2003-08-01 | 2017-11-27 | Mitsubishi Tanabe Pharma Corporation | Nauji junginiai, turintys inhibitorinį aktyvumą prieš nuo natrio priklausomą gliukozės transporterį |
| AU2004270238B2 (en) * | 2003-09-04 | 2010-07-29 | Cephalon, Inc. | Modafinil compositions |
| TWI370818B (en) | 2006-04-05 | 2012-08-21 | Astellas Pharma Inc | Cocrystal of c-glycoside derivative and l-proline |
| US7919598B2 (en) * | 2006-06-28 | 2011-04-05 | Bristol-Myers Squibb Company | Crystal structures of SGLT2 inhibitors and processes for preparing same |
| CN101568537A (zh) | 2006-12-21 | 2009-10-28 | 安斯泰来制药有限公司 | C-糖苷衍生物的制造方法及其合成中间体 |
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2007
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- 2007-04-04 CN CN2007800169018A patent/CN101443328B/zh active Active
- 2007-04-04 KR KR1020087027002A patent/KR101243039B1/ko active Active
- 2007-04-04 WO PCT/JP2007/057597 patent/WO2007114475A1/ja not_active Ceased
- 2007-04-04 KR KR1020127002361A patent/KR20120025001A/ko not_active Ceased
- 2007-04-04 JP JP2008508716A patent/JP5210154B2/ja active Active
- 2007-04-04 MX MX2008012705A patent/MX2008012705A/es active IP Right Grant
- 2007-04-04 RU RU2008143362/04A patent/RU2408595C2/ru not_active IP Right Cessation
- 2007-04-04 AU AU2007232763A patent/AU2007232763B2/en not_active Ceased
- 2007-04-04 BR BRPI0710581-9A patent/BRPI0710581A2/pt not_active IP Right Cessation
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- 2007-04-04 EP EP07741033A patent/EP2009010A4/en not_active Withdrawn
- 2007-04-04 US US12/296,056 patent/US8097592B2/en not_active Expired - Fee Related
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Also Published As
| Publication number | Publication date |
|---|---|
| KR101243039B1 (ko) | 2013-03-20 |
| WO2007114475A1 (ja) | 2007-10-11 |
| NO20084659L (no) | 2009-01-02 |
| CN101443328A (zh) | 2009-05-27 |
| ZA200809201B (en) | 2009-12-30 |
| US20090143316A1 (en) | 2009-06-04 |
| EP2009010A4 (en) | 2012-06-13 |
| CA2649022A1 (en) | 2007-10-11 |
| MX2008012705A (es) | 2008-10-15 |
| CA2649022C (en) | 2012-05-29 |
| EP2009010A1 (en) | 2008-12-31 |
| KR20090015912A (ko) | 2009-02-12 |
| JPWO2007114475A1 (ja) | 2009-08-20 |
| CN101443328B (zh) | 2012-07-25 |
| IL194512A0 (en) | 2009-08-03 |
| TW200811152A (en) | 2008-03-01 |
| AU2007232763B2 (en) | 2011-07-28 |
| JP5210154B2 (ja) | 2013-06-12 |
| AU2007232763A1 (en) | 2007-10-11 |
| RU2408595C2 (ru) | 2011-01-10 |
| KR20120025001A (ko) | 2012-03-14 |
| TWI370818B (en) | 2012-08-21 |
| US8097592B2 (en) | 2012-01-17 |
| BRPI0710581A2 (pt) | 2011-08-16 |
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