DK2614058T3 - Polymorfer og salte af n-[5-[4-(5-{[(2r,6s)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1h-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid. - Google Patents
Polymorfer og salte af n-[5-[4-(5-{[(2r,6s)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1h-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid. Download PDFInfo
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- DK2614058T3 DK2614058T3 DK11755311.5T DK11755311T DK2614058T3 DK 2614058 T3 DK2614058 T3 DK 2614058T3 DK 11755311 T DK11755311 T DK 11755311T DK 2614058 T3 DK2614058 T3 DK 2614058T3
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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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (14)
1. Polymorf (Form II) af /V-[5-[4-(5-{[(2Æ,6S)-2,6-dimethyl-4-nnorpholinyl]nnethyl}- 1.3- oxazol-2-yl)-l/-/-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid, kendet egnet ved, at den tilvejebringer et XRPD-mønster omfattende en top (°2Θ) ved 9,2 ± 0,1.
2. Polymorf ifølge krav 1, kendetegnet ved, at den tilvejebringer et XRPD-mønster omfattende toppe i alt væsentligt som angivet i tabel 1 Tabel 1
3. Polymorf ifølge krav 1 eller krav 2 i at den tilvejebringer et XRPD-mønster i alt væsentligt ifølge figur 1.
4. Polymorf (Form III) af /V-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl)·- 1.3- oxazol-2-yl)-lH-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid, k e n d e t egnet ved, at den tilvejebringer et XRPD-mønster omfattende en top (°2Θ) ved 6,7 ± 0,1.
5. Polymorf ifølge krav 5, kendetegnet ved, at den tilvejebringer et XRPD-mønster omfattende toppe i alt væsentligt som angivet i tabel 2 Tabel 2
6. Polymorf ifølge krav 4 eller krav 5, kendetegnet ved, at den tilvejebringer et XRPD-mønster i alt væsentligt ifølge figur 2.
7. Polymorf (Form IV) af /V-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl>- l,3-oxazol-2-yl)-lH-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid, kendet egnet ved, at den tilvejebringer et XRPD-mønster omfattende en top (°2Θ) ved omkring 5,8.
8. Polymorf ifølge krav 7, kendetegnet ved, at den tilvejebringer et XRPD-mønster omfattende toppe i alt væsentligt som angivet i tabel 3 Tabel 3
9. Polymorf ifølge krav 7 eller krav 8, kendetegnet ved, at den tilvejebringer et XRPD-mønster i alt væsentligt ifølge figur 3.
10. Salt af /V-[5-[4-(5-{[(2/?,6S)-2,6-dimethyl-4-morpholinyl]methyl>-l,3-oxazol-2-yl)-lH-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid som er natrium-, tosy-lat-, maleat-, hemipamoat-, heminaphthalendisulfonat-, mesitylensulfonat-, hemibiphenyl-disulfonat-, 2-naphthalensulfonat- (napsylat-), hemicinnamat-, hemisebacat-, hemipyro-mellitat- eller hemibenzendiacrylatsaltet.
11. Farmaceutisk sammensætning omfattende en polymorf eller et salt, som defineret i et hvilket som helst af krav 1 til 10 og én eller flere farmaceutisk acceptable excipien-ser.
12. Polymorf eller salt, som defineret i et hvilket som helst af krav 1 til 10 til anvendelse i medicinsk terapi.
13. Polymorf eller salt, som defineret i et hvilket som helst af krav 1 til 10 til anvendelse i behandling af en lidelse medieret af uhensigtsmæssig PI3-kinaseaktivitet.
14. Anvendelse af en polymorf eller et salt, som defineret i et hvilket som helst af krav 1 til 10 til fremstilling af et lægemiddel til anvendelse i behandling af en lidelse medieret af uhensigtsmæssig PI3-kinaseaktivitet.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38074810P | 2010-09-08 | 2010-09-08 | |
| PCT/EP2011/065419 WO2012032067A1 (en) | 2010-09-08 | 2011-09-06 | Polymorphs and salts of n- [5- [4- (5- { [(2r,6s) -2, 6 - dimethyl - 4 -morpholinyl] methyl} - 1, 3 - oxazol - 2 - yl) - 1h- inda zol-6-yl] -2- (methyloxy) - 3 - pyridinyl] methanesulfonamide |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2614058T3 true DK2614058T3 (da) | 2015-09-28 |
Family
ID=44645691
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK11755311.5T DK2614058T3 (da) | 2010-09-08 | 2011-09-06 | Polymorfer og salte af n-[5-[4-(5-{[(2r,6s)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1h-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid. |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US8735390B2 (da) |
| EP (1) | EP2614058B1 (da) |
| JP (1) | JP5965402B2 (da) |
| DK (1) | DK2614058T3 (da) |
| ES (1) | ES2548036T3 (da) |
| HR (1) | HRP20151017T1 (da) |
| HU (1) | HUE026059T2 (da) |
| PL (1) | PL2614058T3 (da) |
| PT (1) | PT2614058E (da) |
| RS (1) | RS54286B1 (da) |
| SI (1) | SI2614058T1 (da) |
| SM (1) | SMT201500223B (da) |
| WO (1) | WO2012032067A1 (da) |
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-
2011
- 2011-09-06 DK DK11755311.5T patent/DK2614058T3/da active
- 2011-09-06 SI SI201130595T patent/SI2614058T1/sl unknown
- 2011-09-06 PT PT117553115T patent/PT2614058E/pt unknown
- 2011-09-06 JP JP2013527583A patent/JP5965402B2/ja active Active
- 2011-09-06 HU HUE11755311A patent/HUE026059T2/en unknown
- 2011-09-06 RS RS20150611A patent/RS54286B1/sr unknown
- 2011-09-06 PL PL11755311T patent/PL2614058T3/pl unknown
- 2011-09-06 WO PCT/EP2011/065419 patent/WO2012032067A1/en not_active Ceased
- 2011-09-06 EP EP11755311.5A patent/EP2614058B1/en active Active
- 2011-09-06 HR HRP20151017TT patent/HRP20151017T1/hr unknown
- 2011-09-06 ES ES11755311.5T patent/ES2548036T3/es active Active
- 2011-09-06 US US13/821,585 patent/US8735390B2/en active Active
-
2015
- 2015-09-22 SM SM201500223T patent/SMT201500223B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US8735390B2 (en) | 2014-05-27 |
| PL2614058T3 (pl) | 2015-12-31 |
| HUE026059T2 (en) | 2016-05-30 |
| SI2614058T1 (sl) | 2015-10-30 |
| EP2614058B1 (en) | 2015-07-08 |
| SMT201500223B (it) | 2015-10-30 |
| RS54286B1 (sr) | 2016-02-29 |
| PT2614058E (pt) | 2015-10-27 |
| WO2012032067A1 (en) | 2012-03-15 |
| EP2614058A1 (en) | 2013-07-17 |
| JP2013537175A (ja) | 2013-09-30 |
| JP5965402B2 (ja) | 2016-08-03 |
| US20130165441A1 (en) | 2013-06-27 |
| ES2548036T3 (es) | 2015-10-13 |
| HRP20151017T1 (hr) | 2015-10-23 |
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