DOP2009000209A - Sales de adición de ácido, hidratos y polimorfos de la etil-amida del ácido 5-(2,4-dihidroxi-5-isopropilfenil)-4-(4-morfolin-4-il-metil-fenil)-isoxazol-3-carboxílico, y formulaciones que comprenden estas formas - Google Patents
Sales de adición de ácido, hidratos y polimorfos de la etil-amida del ácido 5-(2,4-dihidroxi-5-isopropilfenil)-4-(4-morfolin-4-il-metil-fenil)-isoxazol-3-carboxílico, y formulaciones que comprenden estas formasInfo
- Publication number
- DOP2009000209A DOP2009000209A DO2009000209A DO2009000209A DOP2009000209A DO P2009000209 A DOP2009000209 A DO P2009000209A DO 2009000209 A DO2009000209 A DO 2009000209A DO 2009000209 A DO2009000209 A DO 2009000209A DO P2009000209 A DOP2009000209 A DO P2009000209A
- Authority
- DO
- Dominican Republic
- Prior art keywords
- phenyl
- acid
- forms
- isoxazol
- formulations
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 3
- 150000004677 hydrates Chemical class 0.000 title abstract 2
- 239000002253 acid Substances 0.000 title 2
- 150000003839 salts Chemical class 0.000 abstract 5
- 102100034051 Heat shock protein HSP 90-alpha Human genes 0.000 abstract 2
- 101001016865 Homo sapiens Heat shock protein HSP 90-alpha Proteins 0.000 abstract 2
- 238000009472 formulation Methods 0.000 abstract 2
- 230000001404 mediated effect Effects 0.000 abstract 2
- 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 abstract 1
- RQVMXXBSRHTHTI-UHFFFAOYSA-N 5-(2,4-dihydroxy-5-propan-2-ylphenyl)-N-ethyl-4-(2-methyl-4-morpholin-4-ylphenyl)-1,2-oxazole-3-carboxamide Chemical compound CCNC(=O)c1noc(c1-c1ccc(cc1C)N1CCOCC1)-c1cc(C(C)C)c(O)cc1O RQVMXXBSRHTHTI-UHFFFAOYSA-N 0.000 abstract 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 abstract 1
- QUSNBJAOOMFDIB-UHFFFAOYSA-N Ethylamine Chemical class CCN QUSNBJAOOMFDIB-UHFFFAOYSA-N 0.000 abstract 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 abstract 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 1
- 229910019142 PO4 Inorganic materials 0.000 abstract 1
- 239000007864 aqueous solution Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000011521 glass Substances 0.000 abstract 1
- 238000001990 intravenous administration Methods 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 abstract 1
- 239000010452 phosphate Substances 0.000 abstract 1
- 229940095064 tartrate Drugs 0.000 abstract 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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
La presente invención se refiere a nuevas formas de sal de etilamida del acido 5-(2,4-dihidroxi-5-isopropil-fenil)-4-(4-morfolin-4-ilmetil-fenil)-isoxazol-3-carboxilico, en particular la sal de mesilato, clorhidrato, tartrato, fosfato, y hemi-fumarato de la misma; a formas cristalinas de estas sales; a polimorfos de la etil-amida del acido 5-(2,4-dihidroxi-5-isopropil-fenil)-4-(4-morfolin-4-il-metil-fenil)-isoxazol3-carboxilico; a hidratos y polimorfos de las nuevas formas de sal mencionadas anteriormente; al use de las nuevas formas de sal mencionadas anteriormente, para la fabricación de un medicamento para el tratamiento de un trastorno mediado por Hsp90; a un método para el tratamiento de un trastorno mediado por Hsp90, utilizando las nuevas formas de sal; a formulaciones que comprenden estas formas de sal, en particular soluciones acuosas adecuadas para administración intravenosa; y a recipientes de vidrio ambar que se rellenan con estas formulaciones.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP07103346 | 2007-03-01 |
Publications (1)
Publication Number | Publication Date |
---|---|
DOP2009000209A true DOP2009000209A (es) | 2009-09-15 |
Family
ID=38134307
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DO2009000209A DOP2009000209A (es) | 2007-03-01 | 2009-08-31 | Sales de adición de ácido, hidratos y polimorfos de la etil-amida del ácido 5-(2,4-dihidroxi-5-isopropilfenil)-4-(4-morfolin-4-il-metil-fenil)-isoxazol-3-carboxílico, y formulaciones que comprenden estas formas |
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 |
EP2370437B1 (en) * | 2008-11-25 | 2013-09-04 | Nerviano Medical Sciences S.r.l. | Bicyclic pyrazole and isoxazole derivatives as antitumor and antineurodegenerative agents |
BR112012017994B8 (pt) | 2010-01-21 | 2020-12-08 | Aprea Ab | composição líquida, uso de uma composição líquida, e, métodos para preparar uma composição líquida e para tratamento de um distúrbio |
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 |
---|---|---|---|---|
PT1611112E (pt) * | 2003-02-11 | 2012-11-02 | Cancer Rec Tech Ltd | Compostos de isoxazole como inibidores de proteínas de choque térmico |
US20060070405A1 (en) * | 2004-10-06 | 2006-04-06 | Anheuser-Busch, Inc. | Method for the production of amber glass with reduced sulfur-containing emissions |
EP2120900A2 (en) | 2007-02-15 | 2009-11-25 | 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 KR KR1020097018126A patent/KR20090122218A/ko not_active Application Discontinuation
- 2008-02-28 AT AT08717228T patent/ATE552836T1/de active
- 2008-02-28 NZ NZ578854A patent/NZ578854A/en not_active IP Right Cessation
- 2008-02-28 PT PT08717228T patent/PT2131845E/pt unknown
- 2008-02-28 MX MX2009009233A patent/MX2009009233A/es active IP Right Grant
- 2008-02-28 AR ARP080100831A patent/AR065519A1/es not_active Application Discontinuation
- 2008-02-28 AU AU2008220800A patent/AU2008220800B2/en not_active Ceased
- 2008-02-28 GE GEAP200811444A patent/GEP20115309B/en 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 ES ES08717228T patent/ES2384906T3/es active Active
- 2008-02-28 PL PL08717228T patent/PL2131845T3/pl unknown
- 2008-02-28 UY UY30943A patent/UY30943A1/es not_active Application Discontinuation
- 2008-02-28 EP EP11192158.1A patent/EP2545921A3/en not_active Withdrawn
- 2008-02-28 DK DK08717228.4T patent/DK2131845T3/da active
- 2008-02-28 CN CN201110226727.8A patent/CN102302500A/zh active Pending
- 2008-02-28 EA EA200901141A patent/EA017075B1/ru not_active IP Right Cessation
- 2008-02-28 CA CA002678043A patent/CA2678043A1/en not_active Abandoned
- 2008-02-28 WO PCT/EP2008/052443 patent/WO2008104595A1/en active Application Filing
- 2008-02-28 CN CN200880005490.7A patent/CN101636162A/zh active Pending
- 2008-02-28 RS RS20120263A patent/RS52351B/en unknown
- 2008-02-28 UA UAA200908592A patent/UA101950C2/ru unknown
- 2008-02-28 EP EP08717228A patent/EP2131845B1/en active Active
- 2008-02-28 BR BRPI0807992-7A2A patent/BRPI0807992A2/pt not_active IP Right Cessation
- 2008-02-28 SI SI200830688T patent/SI2131845T1/sl unknown
- 2008-02-29 PE PE2008000418A patent/PE20090166A1/es not_active Application Discontinuation
- 2008-02-29 CL CL200800618A patent/CL2008000618A1/es unknown
- 2008-02-29 TW TW097107239A patent/TW200844102A/zh unknown
- 2008-02-29 PA PA20088771101A patent/PA8771101A1/es unknown
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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 NI NI200900161A patent/NI200900161A/es unknown
- 2009-08-28 EC EC2009009602A patent/ECSP099602A/es unknown
- 2009-08-31 GT GT200900236A patent/GT200900236A/es unknown
- 2009-08-31 DO DO2009000209A patent/DOP2009000209A/es unknown
- 2009-08-31 MA MA32191A patent/MA31204B1/fr 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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