HRP20120535T1 - Dihidroksi izopropil fenil morfolin ilmetil fenil izoksazol karboksilna kiselina etilamid mesilat njegovi hidrati i polimorfi te formulacije koje sadrže te oblike - Google Patents
Dihidroksi izopropil fenil morfolin ilmetil fenil izoksazol karboksilna kiselina etilamid mesilat njegovi hidrati i polimorfi te formulacije koje sadrže te oblike Download PDFInfo
- Publication number
- HRP20120535T1 HRP20120535T1 HRP20120535AT HRP20120535T HRP20120535T1 HR P20120535 T1 HRP20120535 T1 HR P20120535T1 HR P20120535A T HRP20120535A T HR P20120535AT HR P20120535 T HRP20120535 T HR P20120535T HR P20120535 T1 HRP20120535 T1 HR P20120535T1
- Authority
- HR
- Croatia
- Prior art keywords
- phenyl
- morpholin
- ylmethyl
- dihydroxy
- carboxylic acid
- Prior art date
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- ZMAQNODASNQSRR-UHFFFAOYSA-N 5-(2,4-dihydroxy-5-propan-2-ylphenyl)-N-ethyl-4-[4-(morpholin-4-ylmethyl)phenyl]-1,2-oxazole-3-carboxamide methanesulfonic acid Chemical compound CS(O)(=O)=O.CCNC(=O)C1=NOC(C=2C(=CC(O)=C(C(C)C)C=2)O)=C1C(C=C1)=CC=C1CN1CCOCC1 ZMAQNODASNQSRR-UHFFFAOYSA-N 0.000 title claims 3
- 238000009472 formulation Methods 0.000 title claims 3
- 239000000203 mixture Substances 0.000 title claims 3
- 150000004677 hydrates Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 7
- -1 Dihydroxy Isopropyl Phenyl Morpholine Chemical compound 0.000 claims abstract 3
- VJZBSHKIQOPPRU-UHFFFAOYSA-N 5-(2,4-dihydroxy-5-propan-2-ylphenyl)-4-[4-(morpholin-4-ylmethyl)phenyl]-1,2-oxazole-3-carboxylic acid Chemical compound C1=C(O)C(C(C)C)=CC(C2=C(C(C(O)=O)=NO2)C=2C=CC(CN3CCOCC3)=CC=2)=C1O VJZBSHKIQOPPRU-UHFFFAOYSA-N 0.000 claims 6
- ATWDUWYFCBVNET-UHFFFAOYSA-N ethylammonium methanesulfonate Chemical compound CC[NH3+].CS([O-])(=O)=O ATWDUWYFCBVNET-UHFFFAOYSA-N 0.000 claims 6
- 238000002441 X-ray diffraction Methods 0.000 claims 3
- 239000007864 aqueous solution Substances 0.000 claims 2
- 239000013078 crystal Substances 0.000 claims 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- NDAZATDQFDPQBD-UHFFFAOYSA-N luminespib Chemical compound CCNC(=O)C1=NOC(C=2C(=CC(O)=C(C(C)C)C=2)O)=C1C(C=C1)=CC=C1CN1CCOCC1 NDAZATDQFDPQBD-UHFFFAOYSA-N 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
Classifications
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
- C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Spoj naznačen time da je dihidroksi izopropil fenil morfolin ilmetil fenil izoksazol karboksilna kiselina etilamid mesilat Patent sadrži još patentnih zahtjeva
Claims (9)
1. Spoj, naznačen time, da je 5-(2,4-dihidroksi-5-izopropil-fenil)-4-(4-morfolin-4-ilmetil-fenil)-izoksazol-3-karboksilna kiselina etilamid mesilat.
2. Kristalni oblik, naznačen time, da je od spoja 5-(2,4-dihidroksi-5-izopropil-fenil)-4-(4-morfolin-4-ilmetil-fenil)-izoksazol-3-karboksilna kiselina etilamid mesilat.
3. Kristalni oblik prema zahtjevu 2, naznačen time, da je 5-(2,4-dihidroksi-5-izopropil-fenil)-4-(4-morfolin-4-ilmetil-fenil)-izoksazol-3-karboksilna kiselina etilamid mesilat anhidrat.
4. Kristalni oblik I, naznačen time, da je od spoja 5-(2,4-dihidroksi-5-izopropil-fenil)-4-(4-morfolin-4-ilmetil-fenil)-izoksazol-3-karboksilna kiselina etilamid mesilat anhidrat, s uzorkom difrakcije X-zraka izraženim u razmacima od 2-teta vrijednosti, koji sadrži vršne vrijednosti na 8,0; 11,9; 13,9; 14,2; 16,7; 18,5; 19,4; 22,7; 23,3 ± 0,2 stupnj(ev)a.
5. Kristalni oblik prema zahtjevu 2, naznačen time, da je to hidrat od spoja 5-(2,4-dihidroksi-5-izopropil-fenil)-4-(4-morfolin-4-ilmetil-fenil)-izoksazol-3-karboksilna kiselina etilamid mesilat.
6. Hidratni oblik HA, naznačen time, da je od spoja 5-(2,4-dihidroksi-5-izopropil-fenil)-4-(4-morfolin-4-ilmetil-fenil)-izoksazol-3-karboksilna kiselina etilamid mesilat, koji pokazuje dijagram difrakcije X-zraka izražen u razmaku od 2-teta vrijednosti, koji sadrži vršne vrijednosti na 11,0; 11,6; 14,1; 18,1; 20,1; 20,5; 21,1; 21,7; 21,9; 25,8 ± 0,2 stupnj(ev)a.
7. Hidratni oblik HB, naznačen time, da je od spoja 5-(2,4-dihidroksi-5-izopropil-fenil)-4-(4-morfolin-4-ilmetil-fenil)-izoksazol-3-karboksilna kiselina etilamid mesilat, koji pokazuje dijagram difrakcije X-zraka izražen u razdoblju od 2-teta vrijednosti, koji sadrži vršne vrijednosti na 6,2; 10,1; 12,6; 14,5; 18,0; 18,5; 19,0; 20,4; 20,9; 21,8; 22,2; 25,4 ± 0,2 stupnj(ev)a.
8. Formulacija, naznačena time, da obuhvaća 5-(2,4-dihidroksi-5-izopropil-fenil)-4-(4-morfolin-4-ilmetil-fenil)-izoksazol-3-karboksilna kiselina etilamid mesilat, gdje se radi o vodenoj otopini koja sadrži 5-(2,4-dihidroksi-5-izopropil-fenil)-4-(4-morfolin-4-ilmetil-fenil)-izoksazol-3-karboksilna kiselina etilamid mesilata slobodnog od bilo koje ostale soli, s pH vrijednosti između 3,2 i 5,2.
9. Formulacija, naznačena time, da se sastoji od izotonične vodene otopine mesilatne soli od spoja 5-(2,4-dihidroksi-5-izopropil-fenil)-4-(4-morfolin-4-ilmetil-fenil)-izoksazol-3-karboksilna kiselina etilamid i 5 masenih% glukoze ili manitola.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07103346 | 2007-03-01 | ||
| PCT/EP2008/052443 WO2008104595A1 (en) | 2007-03-01 | 2008-02-28 | Acid addition salts, hydrates and polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide and formulations comprising these forms |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120535T1 true HRP20120535T1 (hr) | 2012-07-31 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20120535AT HRP20120535T1 (hr) | 2007-03-01 | 2012-06-28 | Dihidroksi izopropil fenil morfolin ilmetil fenil izoksazol karboksilna kiselina etilamid mesilat njegovi hidrati i polimorfi te formulacije koje sadrže te oblike |
Country Status (41)
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200922595A (en) * | 2007-10-12 | 2009-06-01 | Novartis Ag | Organic compounds |
| TWI450898B (zh) * | 2008-07-04 | 2014-09-01 | Sigma Tau Res Switzerland Sa | 具有抗腫瘤活性之芳基異唑化合物 |
| US8309578B2 (en) | 2008-11-25 | 2012-11-13 | Nerviano Medical Sciences S.R.L. | Bicyclic pyrazole and isoxazole derivatives as antitumor and antineurodegenerative agents |
| ES2578513T3 (es) * | 2010-01-21 | 2016-07-27 | Aprea Ab | Solución acuosa que comprende 3-quinuclidinona para el tratamiento de enfermedades hiperproliferativas, autoinmunes y cardiacas |
| WO2011102660A2 (en) * | 2010-02-17 | 2011-08-25 | Ildong Pharm Co., Ltd. | A novel 5-membered heterocycle derivatives and manufacturing process thereof |
| KR20120031854A (ko) | 2010-09-27 | 2012-04-04 | 한국전자통신연구원 | 시간 및 주파수 특징을 이용하는 음악 음원 분리 장치 및 방법 |
| WO2013015661A2 (en) * | 2011-07-28 | 2013-01-31 | Ildong Pharm Co.,Ltd. | Novel prodrugs of 5-(2,4-dihydroxy-5-isopropylphenyl)-n-ethyl-4-(5-methyl1-1,2,4-oxadiazol-3-yl)isoxazole-3-carboxamide |
| FR3039401B1 (fr) * | 2015-07-31 | 2018-07-13 | Les Laboratoires Servier | Nouvelle association entre le 3-[(3-{[4-(4-morpholinylmethyl)-1h-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1h-indol-5-yl)methyl]-1,3-thiazolidine-2,4-dione et un inhibiteur de la tyr kinase du egfr |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1771235B (zh) * | 2003-02-11 | 2010-04-28 | 弗奈利斯(剑桥)有限公司 | 异噁唑化合物 |
| US20060070405A1 (en) * | 2004-10-06 | 2006-04-06 | Anheuser-Busch, Inc. | Method for the production of amber glass with reduced sulfur-containing emissions |
| WO2008100985A2 (en) | 2007-02-15 | 2008-08-21 | Novartis Ag | Combination of lbh589 with other therapeutic agents for treating cancer |
| WO2010069458A1 (de) | 2008-12-17 | 2010-06-24 | Merck Patent Gmbh | Hexahalochromat(lll)-komplexe |
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2008
- 2008-02-28 PL PL08717228T patent/PL2131845T3/pl unknown
- 2008-02-28 JP JP2009551218A patent/JP2010520176A/ja active Pending
- 2008-02-28 US US12/529,090 patent/US8163747B2/en active Active
- 2008-02-28 AR ARP080100831A patent/AR065519A1/es not_active Application Discontinuation
- 2008-02-28 BR BRPI0807992-7A2A patent/BRPI0807992A2/pt not_active IP Right Cessation
- 2008-02-28 EP EP08717228A patent/EP2131845B1/en active Active
- 2008-02-28 CA CA002678043A patent/CA2678043A1/en not_active Abandoned
- 2008-02-28 UA UAA200908592A patent/UA101950C2/ru unknown
- 2008-02-28 UY UY30943A patent/UY30943A1/es not_active Application Discontinuation
- 2008-02-28 MX MX2009009233A patent/MX2009009233A/es active IP Right Grant
- 2008-02-28 ES ES08717228T patent/ES2384906T3/es active Active
- 2008-02-28 SI SI200830688T patent/SI2131845T1/sl unknown
- 2008-02-28 EP EP11192158.1A patent/EP2545921A3/en not_active Withdrawn
- 2008-02-28 AT AT08717228T patent/ATE552836T1/de active
- 2008-02-28 RS RS20120263A patent/RS52351B/en unknown
- 2008-02-28 KR KR1020097018126A patent/KR20090122218A/ko not_active Application Discontinuation
- 2008-02-28 CN CN201110226727.8A patent/CN102302500A/zh active Pending
- 2008-02-28 GE GEAP200811444A patent/GEP20115309B/en unknown
- 2008-02-28 PT PT08717228T patent/PT2131845E/pt unknown
- 2008-02-28 EA EA200901141A patent/EA017075B1/ru not_active IP Right Cessation
- 2008-02-28 NZ NZ578854A patent/NZ578854A/en not_active IP Right Cessation
- 2008-02-28 AU AU2008220800A patent/AU2008220800B2/en not_active Ceased
- 2008-02-28 DK DK08717228.4T patent/DK2131845T3/da active
- 2008-02-28 CN CN200880005490.7A patent/CN101636162A/zh active Pending
- 2008-02-28 WO PCT/EP2008/052443 patent/WO2008104595A1/en active Application Filing
- 2008-02-29 TW TW097107239A patent/TW200844102A/zh unknown
- 2008-02-29 CL CL200800618A patent/CL2008000618A1/es unknown
- 2008-02-29 PA PA20088771101A patent/PA8771101A1/es unknown
- 2008-02-29 PE PE2008000418A patent/PE20090166A1/es not_active Application Discontinuation
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2009
- 2009-08-03 ZA ZA200905417A patent/ZA200905417B/xx unknown
- 2009-08-13 IL IL200401A patent/IL200401A0/en unknown
- 2009-08-21 CR CR10989A patent/CR10989A/es not_active Application Discontinuation
- 2009-08-28 TN TNP2009000357A patent/TN2009000357A1/fr unknown
- 2009-08-28 EC EC2009009602A patent/ECSP099602A/es unknown
- 2009-08-28 NI NI200900161A patent/NI200900161A/es unknown
- 2009-08-31 DO DO2009000209A patent/DOP2009000209A/es unknown
- 2009-08-31 MA MA32191A patent/MA31204B1/fr unknown
- 2009-08-31 GT GT200900236A patent/GT200900236A/es unknown
- 2009-09-01 CO CO09092694A patent/CO6210828A2/es not_active Application Discontinuation
- 2009-09-30 SM SM200900080T patent/SMAP200900080A/it unknown
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2010
- 2010-06-09 HK HK10105737.5A patent/HK1139073A1/xx not_active IP Right Cessation
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2012
- 2012-03-08 US US13/415,268 patent/US8487095B2/en active Active
- 2012-06-28 HR HRP20120535AT patent/HRP20120535T1/hr unknown
- 2012-07-09 CY CY20121100610T patent/CY1113805T1/el unknown
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2013
- 2013-07-10 US US13/938,659 patent/US20130296556A1/en not_active Abandoned
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