DK2114405T3 - Methylparaben cokrystallinsk form "A" of [4-(3-fluor-5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-[5-methansulfonyl-2-((S) -2,2,2-trifluor-1-methyl-ethoxy)-phenyl]-methanon - Google Patents
Methylparaben cokrystallinsk form "A" of [4-(3-fluor-5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-[5-methansulfonyl-2-((S) -2,2,2-trifluor-1-methyl-ethoxy)-phenyl]-methanon Download PDFInfo
- Publication number
- DK2114405T3 DK2114405T3 DK07857734T DK07857734T DK2114405T3 DK 2114405 T3 DK2114405 T3 DK 2114405T3 DK 07857734 T DK07857734 T DK 07857734T DK 07857734 T DK07857734 T DK 07857734T DK 2114405 T3 DK2114405 T3 DK 2114405T3
- Authority
- DK
- Denmark
- Prior art keywords
- piperazin
- methanesulfonyl
- trifluoro
- pyridin
- trifluoromethyl
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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- 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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
Claims (7)
1. Krystallinsk form A af [4-(3-fluor-5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-[5-methansulfonyl-2-((S)-2,2,2-trifluor-l-methyl-ethoxy)-phenyl]-methanon kendetegnet ved mindst tre toppe valgt fra de følgende røntgendiffraktionstoppe opnået med en CuKa-stråling, udtrykt i grader 2Theta = 13,1/ 14,3, 15,4, 16,2, 17,1, 17,2, 17,6, 18,0, 19,8, 20,1, 20,4, 21,0, 22,6 og 24,3 (± 0,2).
2. Krystallinsk form A af [4-(3-fluor-5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-[5-methansulfonyl-2-((S)-2,2,2-trifluor-l-methyl-ethoxy)-phenyl]-methanon kendetegnet ved de følgende røntgendiffraktionstoppe opnået med en CuKa-stråling, udtrykt i grader 2Theta = 13,1, 14,3, 15,4, 16,2, 17,1, 17,2, 17,6, 18,0, 19,8, 20,1, 20,4, 21,0, 22,6 og 24,3 (± 0,2).
3. Krystallinsk form A af [4-(3-fluor-5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-[5-methansulfonyl-2-((S)-2,2,2-trifluor-l-methyl-ethoxy)-phenyl]-methanon kendetegnet ved et infrarødt spektrum med skarpe bånd ved 3032, 1645, 1623, 1600, 1581, 1501, 1342, 1331, 1314, 1291, 1266, 1245, 1154, 1130, 1088, 1054, 1012, 976, 951, 922, 889, 824, 787, 758, 739, 714 og 636 cm1 (± 3 cm1).
4. Forbindelsen [4-(3-fluor-5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-[5-methansulfonyl-2-((S)-2,2,2-trifluor-l-methyl-ethoxy)-phenyl]-methanon, hvor mindst 70% er i en form som beskrevet i et hvilket som helst af kravene 1 til 5.
5. Fremgangsmåde til fremstilling af en krystallinsk form A af [4-(3-fluor-5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-[5-methansulfonyl-2-((S)-2,2,2-trifluor-l-methyl-ethoxy)-phenylj-methanon som beskrevet i et hvilket som helst af kravene 1 til 5, omfattende trinnene af: - enten omkrystallisation af [4-(3-fluor-5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-[5-methansulfonyl-2-((S)-2,2,2-trifluor-l-methyl-ethoxy)-phenyl]-methanon efter podning; - eller omkrystallisation af [4-(3-fluor-5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-[5-methansulfonyl-2-((S)-2,2,2-trifluor-l-methyl-ethoxy)-phenyl]-methanon og spontan krystallisation under ca. 40°C, uden podning.
6. Farmaceutisk sammensætning omfattende en krystallinsk form A af [4-(3-fluor-5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-[5-methansulfonyl-2-((S)-2,2,2-trifluor-l- methyl-ethoxy)-phenyl]-methanon som beskrevet i et hvilket som helst af kravene 1 til 5, som en aktiv bestanddel.
7. Anvendelse afen krystallinsk form A af [4-(3-fluor-5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-[5-methansulfonyl-2-((S)-2,2,2-trifluor-l-methyl-ethoxy)-phenyl]-methanon som beskrevet i et hvilket som helst af kravene 1 til 5 til fremstillingen af et medikament der er effektiv til behandling af psykose, smerte, neurodegerativ dysfunktion i hukommelse og indlæring, skizofreni, demens og andre sygdomme i hvilke kognitive processer er svækkede, såsom opmærksomhedsforstyrrelser, eller Alzheimer's sygdom.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06127269 | 2006-12-28 | ||
| PCT/EP2007/064104 WO2008080821A1 (en) | 2006-12-28 | 2007-12-18 | Crystalline forms glyt1 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2114405T3 true DK2114405T3 (da) | 2015-04-07 |
Family
ID=38988312
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK07857734T DK2114405T3 (da) | 2006-12-28 | 2007-12-18 | Methylparaben cokrystallinsk form "A" of [4-(3-fluor-5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-[5-methansulfonyl-2-((S) -2,2,2-trifluor-1-methyl-ethoxy)-phenyl]-methanon |
Country Status (33)
| Country | Link |
|---|---|
| US (5) | US20080214561A1 (da) |
| EP (1) | EP2114405B1 (da) |
| JP (1) | JP4799666B2 (da) |
| KR (1) | KR101130146B1 (da) |
| CN (1) | CN101573114A (da) |
| AR (1) | AR064545A1 (da) |
| AU (1) | AU2007341356B2 (da) |
| BR (1) | BRPI0720829B8 (da) |
| CA (1) | CA2673667A1 (da) |
| CL (1) | CL2007003830A1 (da) |
| CO (1) | CO6190613A2 (da) |
| CR (1) | CR10846A (da) |
| CY (1) | CY1116350T1 (da) |
| DK (1) | DK2114405T3 (da) |
| EC (1) | ECSP099471A (da) |
| ES (1) | ES2535040T3 (da) |
| HR (1) | HRP20150573T1 (da) |
| HU (1) | HUE025032T2 (da) |
| MA (1) | MA31029B1 (da) |
| MX (1) | MX2009006859A (da) |
| MY (1) | MY188367A (da) |
| NO (1) | NO342150B1 (da) |
| NZ (1) | NZ577502A (da) |
| PE (1) | PE20081556A1 (da) |
| PL (1) | PL2114405T3 (da) |
| PT (1) | PT2114405E (da) |
| RS (1) | RS53910B1 (da) |
| RU (1) | RU2463295C2 (da) |
| SI (1) | SI2114405T1 (da) |
| TW (1) | TWI388552B (da) |
| UA (1) | UA100232C2 (da) |
| WO (1) | WO2008080821A1 (da) |
| ZA (1) | ZA200904423B (da) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2673667A1 (en) | 2006-12-28 | 2008-07-10 | F. Hoffmann-La Roche Ag | Crystalline forms glyt1 |
| EP2400848A4 (en) * | 2009-02-26 | 2012-07-25 | Thar Pharmaceuticals Inc | CRYSTALLIZATION OF PHARMACEUTICAL COMPOUNDS |
| KR101196354B1 (ko) * | 2010-09-03 | 2012-11-01 | 서유헌 | 퇴행성 신경계 뇌 질환의 예방 또는 치료용 약학 조성물 |
| US9328101B2 (en) * | 2012-05-25 | 2016-05-03 | Basf Se | Crystalline form B of 1,5-dimethyl-6-thioxo-3-(2,2,7-trifluoro-3-oxo-4-(prop-2-ynyl)-3,4-dihydro-2H-benzo[B][1,4]oxazin-6-yl)-1,3,5-triazinane-2,4-dione |
| US8927412B1 (en) * | 2013-08-01 | 2015-01-06 | Taiwan Semiconductor Manufacturing Company, Ltd. | Multi-chip package and method of formation |
| MX354615B (es) * | 2013-10-02 | 2018-03-08 | Centro De Investig Y De Estudios Avanzados Del I P N | Uso del propilparabeno comoagente neuroprotector en el daño neuronal inducido por status epilepticus. |
| CN116212025A (zh) | 2020-01-09 | 2023-06-06 | 迪斯克医药公司 | 治疗红细胞生成性原卟啉病、x连锁原卟啉病或先天性红细胞生成性卟啉病的方法 |
| EP4180105A1 (en) * | 2020-07-13 | 2023-05-17 | NGK Insulators, Ltd. | Refining method |
| JP2024518091A (ja) * | 2021-05-14 | 2024-04-24 | ディスク・メディシン・インコーポレイテッド | グリシン輸送阻害剤を用いて赤血球増殖性プロトポルフィリン症、ｘ連鎖プロトポルフィリン症または先天性赤血球増殖性ポルフィリン症を処置する方法 |
| WO2022251458A1 (en) * | 2021-05-27 | 2022-12-01 | Disc Medicine, Inc. | Methods of treating erythropoietic protoporphyria, x-linked protoporphyria, or congenital erythropoietic porphyria with a solid form of bitopertin |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL154370A0 (en) | 2003-02-10 | 2003-09-17 | Chemagis Ltd | Solid amorphous mixtures, processes for the preparation thereof and pharmaceutical compositions containing the same |
| WO2005014563A1 (en) * | 2003-08-11 | 2005-02-17 | F. Hoffmann-La Roche Ag | Piperazine with or-substituted phenyl group and their use as glyt1 inhibitors |
| CA2673667A1 (en) | 2006-12-28 | 2008-07-10 | F. Hoffmann-La Roche Ag | Crystalline forms glyt1 |
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2007
- 2007-12-18 CA CA002673667A patent/CA2673667A1/en not_active Abandoned
- 2007-12-18 MX MX2009006859A patent/MX2009006859A/es active IP Right Grant
- 2007-12-18 ES ES07857734.3T patent/ES2535040T3/es active Active
- 2007-12-18 PL PL07857734T patent/PL2114405T3/pl unknown
- 2007-12-18 HU HUE07857734A patent/HUE025032T2/en unknown
- 2007-12-18 AU AU2007341356A patent/AU2007341356B2/en active Active
- 2007-12-18 PT PT78577343T patent/PT2114405E/pt unknown
- 2007-12-18 JP JP2009543441A patent/JP4799666B2/ja active Active
- 2007-12-18 DK DK07857734T patent/DK2114405T3/da active
- 2007-12-18 EP EP07857734.3A patent/EP2114405B1/en active Active
- 2007-12-18 CN CNA2007800479512A patent/CN101573114A/zh active Pending
- 2007-12-18 UA UAA200907731A patent/UA100232C2/uk unknown
- 2007-12-18 SI SI200731644T patent/SI2114405T1/sl unknown
- 2007-12-18 BR BRPI0720829A patent/BRPI0720829B8/pt active IP Right Grant
- 2007-12-18 WO PCT/EP2007/064104 patent/WO2008080821A1/en active Application Filing
- 2007-12-18 RU RU2009124113/04A patent/RU2463295C2/ru active
- 2007-12-18 RS RS20150229A patent/RS53910B1/en unknown
- 2007-12-18 MY MYPI20092584A patent/MY188367A/en unknown
- 2007-12-18 KR KR1020097015643A patent/KR101130146B1/ko active IP Right Grant
- 2007-12-18 NZ NZ577502A patent/NZ577502A/en unknown
- 2007-12-19 US US12/002,997 patent/US20080214561A1/en not_active Abandoned
- 2007-12-25 TW TW096150002A patent/TWI388552B/zh active
- 2007-12-27 AR ARP070105913A patent/AR064545A1/es not_active Application Discontinuation
- 2007-12-27 CL CL200703830A patent/CL2007003830A1/es unknown
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2008
- 2008-01-02 PE PE2008000055A patent/PE20081556A1/es not_active Application Discontinuation
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2009
- 2009-06-08 CR CR10846A patent/CR10846A/es unknown
- 2009-06-11 CO CO09061117A patent/CO6190613A2/es not_active Application Discontinuation
- 2009-06-19 NO NO20092358A patent/NO342150B1/no unknown
- 2009-06-24 ZA ZA200904423A patent/ZA200904423B/xx unknown
- 2009-06-26 EC EC2009009471A patent/ECSP099471A/es unknown
- 2009-06-29 MA MA32049A patent/MA31029B1/fr unknown
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2010
- 2010-07-22 US US12/841,195 patent/US8039473B2/en not_active Expired - Fee Related
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2011
- 2011-07-22 US US13/188,486 patent/US20110295007A1/en not_active Abandoned
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2012
- 2012-06-13 US US13/495,093 patent/US20120309969A1/en not_active Abandoned
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2013
- 2013-03-13 US US13/798,358 patent/US20130197225A1/en not_active Abandoned
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2015
- 2015-05-20 CY CY20151100451T patent/CY1116350T1/el unknown
- 2015-05-28 HR HRP20150573TT patent/HRP20150573T1/hr unknown
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