DK2681220T3 - Hidtil ukendte salte af dpp-iv-inhibitor - Google Patents
Hidtil ukendte salte af dpp-iv-inhibitor Download PDFInfo
- Publication number
- DK2681220T3 DK2681220T3 DK12766329.2T DK12766329T DK2681220T3 DK 2681220 T3 DK2681220 T3 DK 2681220T3 DK 12766329 T DK12766329 T DK 12766329T DK 2681220 T3 DK2681220 T3 DK 2681220T3
- Authority
- DK
- Denmark
- Prior art keywords
- dihydro
- oxo
- trifluoromethyl
- triazolo
- amine
- Prior art date
Links
Classifications
-
- 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
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (3)
1. Den krystallinske form II af (2R)-4-oxo-4-[3-(trifluormethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorphenyl)butan-2-aminbesylat med et karakteristik røntgenpulverdiffraktionsmønster med peaks udtrykt som 2Θ ved 5,69, 7,45, 10,08, 11,41, 13,09, 18,34, 22,52 og 22,97 ± 0,2 grader 2-theta.
2.
Fremgangsmåde til fremstilling af den krystallinske form II af (2R)-4-oxo-4-[3-(trifluormethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorphenyl)butan-2-aminbesylat ifølge krav 1, hvilken fremgangsmåde omfatter (a) omsætning af den frie base (formel I) under egnede reaktionsbetingelser med benzensulfonsyren i egnet opløsningsmiddel udvalgt fra en blanding af estere og vand, en blanding af estere, ethere og vand, en blanding af estere, alkoholer og vand, en blanding af ester, carbonhydrider og vand, en blanding af estere, ketoner og vand; (b) egnet fjernelse af opløsningsmidlet for at opnå den krystallinske form II af (2R)-4-oxo-4-[3-(trifluormethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1 -(2,4,5- trifluorphenyl)butan-2-aminbesylat.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN590MU2011 | 2011-03-03 | ||
| IN1948MU2011 | 2011-07-06 | ||
| IN2777MU2011 | 2011-09-30 | ||
| PCT/IN2012/000148 WO2012147092A2 (en) | 2011-03-03 | 2012-03-02 | Novel salts of dpp-iv inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2681220T3 true DK2681220T3 (da) | 2015-11-30 |
Family
ID=54290089
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK12766329.2T DK2681220T3 (da) | 2011-03-03 | 2012-03-02 | Hidtil ukendte salte af dpp-iv-inhibitor |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9108972B2 (da) |
| EP (4) | EP2860180A1 (da) |
| JP (1) | JP2014510071A (da) |
| KR (1) | KR20130132631A (da) |
| CN (2) | CN103476778A (da) |
| AU (1) | AU2012247127B2 (da) |
| BR (1) | BR112013022504A8 (da) |
| DK (1) | DK2681220T3 (da) |
| ES (1) | ES2548269T3 (da) |
| MX (1) | MX2013010027A (da) |
| PH (1) | PH12015501536A1 (da) |
| SG (2) | SG10201405403QA (da) |
| WO (1) | WO2012147092A2 (da) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140350023A1 (en) * | 2011-12-08 | 2014-11-27 | Ranbaxy Laboratories Limited | Amorphous form of sitagliptin salts |
| MX2016016260A (es) * | 2016-12-08 | 2018-06-07 | Alparis Sa De Cv | Nuevas formas solidas de sitagliptina. |
| GR1010089B (el) | 2020-09-15 | 2021-09-27 | Φαρματεν Α.Β.Ε.Ε. | Στερεη φαρμακοτεχνικη μορφη περιεχουσα σιταγλιπτινη και μεθοδος παρασκευης αυτης |
| GR1010234B (el) | 2021-04-27 | 2022-05-18 | Φαρματεν Α.Β.Ε.Ε., | Φαρμακευτικο σκευασμα που περιλαμβανει συνδυασμο σιταγλιπτινης και μετφορμινης και μεθοδος για την παρασκευη αυτου |
| WO2023139276A1 (en) | 2022-01-24 | 2023-07-27 | Zaklady Farmaceutyczne Polpharma S.A. | Process for preparing crystalline sitagliptin hydrochloride monohydrate |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3174901A (en) * | 1963-01-31 | 1965-03-23 | Jan Marcel Didier Aron Samuel | Process for the oral treatment of diabetes |
| UA74912C2 (en) * | 2001-07-06 | 2006-02-15 | Merck & Co Inc | Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes |
| JO2625B1 (en) | 2003-06-24 | 2011-11-01 | ميرك شارب اند دوم كوربوريشن | Phosphoric acid salts of dipeptidyl betidase inhibitor 4 |
| EP1662876A4 (en) | 2003-09-02 | 2009-01-14 | Merck & Co Inc | NOVEL CRYSTALLINE FORMS OF A PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR |
| EP1667524A4 (en) | 2003-09-23 | 2009-01-14 | Merck & Co Inc | NOVEL CRYSTALLINE FORM OF A PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTASE-IV INHIBITOR |
| WO2005072530A1 (en) * | 2004-01-16 | 2005-08-11 | Merck & Co., Inc. | Novel crystalline salts of a dipeptidyl peptidase-iv inhibitor |
| US7612072B2 (en) | 2004-09-15 | 2009-11-03 | Merck & Co., Inc. | Amorphous form of a phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor |
| JP5069678B2 (ja) * | 2005-05-25 | 2012-11-07 | 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 |
| WO2007035198A2 (en) | 2005-07-25 | 2007-03-29 | Merck & Co., Inc. | Dodecylsulfate salt of a dipeptidyl peptidase-iv inhibitor |
| AU2006306420A1 (en) * | 2005-10-25 | 2007-05-03 | Merck Sharp & Dohme Corp. | Combination of a dipeptidyl peptidase-4 inhibitor and an anti-hypertensive agent for the treatment of diabetes and hypertension |
| CN101484411A (zh) | 2006-06-27 | 2009-07-15 | 桑多斯股份公司 | 盐的新制备方法 |
| EP2076518A1 (en) * | 2006-10-12 | 2009-07-08 | Xenon Pharmaceuticals Inc. | Tricyclic spiro-oxindole derivatives and their uses as therapeutic agents |
| BRPI0719210A2 (pt) * | 2006-10-12 | 2015-05-05 | Xenon Pharmaceuticals Inc | Uso de compostos espiro-oxindol como agentes terapêuticos |
| EP2019113A1 (en) * | 2007-07-26 | 2009-01-28 | Anadys Pharmaceuticals, Inc. | New Crystalline Salts of 5-Amino-3-(2',3'-di-O-acetyl-beta-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one |
| MX2010001371A (es) * | 2007-08-09 | 2010-03-10 | Rensselaer Polytech Inst | Carboxamidas opioides cuaternarias. |
| CA2707790C (en) * | 2007-12-20 | 2015-04-21 | Dr. Reddy's Laboratories Limited | Processes for the preparation of sitagliptin and pharmaceutically acceptable salts thereof |
| EP2650297A1 (en) | 2008-07-03 | 2013-10-16 | Ratiopharm GmbH | Crystalline salts of sitagliptin |
| FR2933692B1 (fr) * | 2008-07-10 | 2022-12-02 | Univ Nancy 1 Henri Poincare | Nouveaux composes, leur utilisation comme medicaments, et leur procede de preparation |
| WO2010012781A2 (en) | 2008-07-29 | 2010-02-04 | Medichem, S.A. | New crystalline salt forms of a 5,6,7,8-tetrahydro-1,2,4- triazolo[4,3-a]pyrazine derivative |
| EP2331545B1 (en) | 2008-08-27 | 2013-10-02 | Cadila Healthcare Limited | Improved process for preparation of (2r)-4-oxo-4-[3- (trifluoromethyl)-5,6-dihydro [1,2,4]-triazolo[4,3-a]pyrazin- 7(8h)-yl]-l-(2,4,5-trifluorophenyl)butan-2-amine&new impurities in preparation thereof |
| US8278486B2 (en) * | 2008-12-31 | 2012-10-02 | Chiral Quest, Inc. | Process and intermediates for the preparation of N-acylated-4-aryl beta-amino acid derivatives |
| EP2218721A1 (en) | 2009-02-11 | 2010-08-18 | LEK Pharmaceuticals d.d. | Novel salts of sitagliptin |
| WO2010117738A2 (en) | 2009-03-30 | 2010-10-14 | Teva Pharmaceutical Industries Ltd. | Solid state forms of sitagliptin salts |
| EP2407469A1 (en) | 2010-07-13 | 2012-01-18 | Chemo Ibérica, S.A. | Salt of sitagliptin |
| WO2013001457A1 (en) * | 2011-06-30 | 2013-01-03 | Ranbaxy Laboratories Limited | Novel salts of sitagliptin |
-
2012
- 2012-03-02 EP EP20140196352 patent/EP2860180A1/en not_active Withdrawn
- 2012-03-02 JP JP2013555995A patent/JP2014510071A/ja active Pending
- 2012-03-02 KR KR1020137026089A patent/KR20130132631A/ko not_active Application Discontinuation
- 2012-03-02 WO PCT/IN2012/000148 patent/WO2012147092A2/en active Application Filing
- 2012-03-02 SG SG10201405403QA patent/SG10201405403QA/en unknown
- 2012-03-02 DK DK12766329.2T patent/DK2681220T3/da active
- 2012-03-02 MX MX2013010027A patent/MX2013010027A/es not_active Application Discontinuation
- 2012-03-02 BR BR112013022504A patent/BR112013022504A8/pt not_active IP Right Cessation
- 2012-03-02 ES ES12766329.2T patent/ES2548269T3/es active Active
- 2012-03-02 US US14/002,541 patent/US9108972B2/en not_active Expired - Fee Related
- 2012-03-02 CN CN2012800168764A patent/CN103476778A/zh active Pending
- 2012-03-02 SG SG2013064886A patent/SG192973A1/en unknown
- 2012-03-02 EP EP14171186.1A patent/EP2789616A1/en not_active Withdrawn
- 2012-03-02 EP EP12766329.2A patent/EP2681220B1/en not_active Not-in-force
- 2012-03-02 EP EP14196602.8A patent/EP2899194A1/en not_active Withdrawn
- 2012-03-02 AU AU2012247127A patent/AU2012247127B2/en not_active Expired - Fee Related
- 2012-03-02 CN CN201510112504.7A patent/CN104788456A/zh active Pending
-
2015
- 2015-07-08 PH PH12015501536A patent/PH12015501536A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ES2548269T3 (es) | 2015-10-15 |
| EP2860180A1 (en) | 2015-04-15 |
| WO2012147092A3 (en) | 2013-03-14 |
| EP2681220B1 (en) | 2015-08-19 |
| BR112013022504A8 (pt) | 2018-01-23 |
| AU2012247127B2 (en) | 2016-01-28 |
| BR112013022504A2 (pt) | 2016-07-19 |
| PH12015501536A1 (en) | 2015-09-21 |
| KR20130132631A (ko) | 2013-12-04 |
| SG192973A1 (en) | 2013-09-30 |
| JP2014510071A (ja) | 2014-04-24 |
| EP2789616A1 (en) | 2014-10-15 |
| CN103476778A (zh) | 2013-12-25 |
| WO2012147092A2 (en) | 2012-11-01 |
| MX2013010027A (es) | 2014-02-11 |
| SG10201405403QA (en) | 2014-11-27 |
| EP2681220A2 (en) | 2014-01-08 |
| CN104788456A (zh) | 2015-07-22 |
| US9108972B2 (en) | 2015-08-18 |
| AU2012247127A1 (en) | 2013-10-03 |
| US20140051856A1 (en) | 2014-02-20 |
| EP2899194A1 (en) | 2015-07-29 |
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