ATE552836T1 - 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4- morpholin-4-ylmethyl-phenyl)-isoxazol-3- carboxylsäure-ethylamid mesylat, dessen hydrate und polymorphe, und formulierungen mit diesen formen - Google Patents

5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4- morpholin-4-ylmethyl-phenyl)-isoxazol-3- carboxylsäure-ethylamid mesylat, dessen hydrate und polymorphe, und formulierungen mit diesen formen

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Publication number
ATE552836T1
ATE552836T1 AT08717228T AT08717228T ATE552836T1 AT E552836 T1 ATE552836 T1 AT E552836T1 AT 08717228 T AT08717228 T AT 08717228T AT 08717228 T AT08717228 T AT 08717228T AT E552836 T1 ATE552836 T1 AT E552836T1
Authority
AT
Austria
Prior art keywords
phenyl
polymorphes
isoxazole
ylmethyl
hydrates
Prior art date
Application number
AT08717228T
Other languages
English (en)
Inventor
Martin James Drysdale
Brian William Dymock
Christoph Krell
Michael Mutz
Holger Petersen
Weijia Zheng
Original Assignee
Novartis Ag
Vernalis R&D Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38134307&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ATE552836(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag, Vernalis R&D Ltd filed Critical Novartis Ag
Application granted granted Critical
Publication of ATE552836T1 publication Critical patent/ATE552836T1/de

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Classifications

    • 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
    • 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
    • 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)
AT08717228T 2007-03-01 2008-02-28 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4- morpholin-4-ylmethyl-phenyl)-isoxazol-3- carboxylsäure-ethylamid mesylat, dessen hydrate und polymorphe, und formulierungen mit diesen formen ATE552836T1 (de)

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
ATE552836T1 true ATE552836T1 (de) 2012-04-15

Family

ID=38134307

Family Applications (1)

Application Number Title Priority Date Filing Date
AT08717228T ATE552836T1 (de) 2007-03-01 2008-02-28 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4- morpholin-4-ylmethyl-phenyl)-isoxazol-3- carboxylsäure-ethylamid mesylat, dessen hydrate und polymorphe, und formulierungen mit diesen formen

Country Status (40)

Country Link
US (3) US8163747B2 (de)
EP (2) EP2131845B1 (de)
JP (1) JP2010520176A (de)
KR (1) KR20090122218A (de)
CN (2) CN101636162A (de)
AR (1) AR065519A1 (de)
AT (1) ATE552836T1 (de)
AU (1) AU2008220800B2 (de)
BR (1) BRPI0807992A2 (de)
CA (1) CA2678043A1 (de)
CL (1) CL2008000618A1 (de)
CO (1) CO6210828A2 (de)
CR (1) CR10989A (de)
CY (1) CY1113805T1 (de)
DK (1) DK2131845T3 (de)
DO (1) DOP2009000209A (de)
EA (1) EA017075B1 (de)
EC (1) ECSP099602A (de)
ES (1) ES2384906T3 (de)
GE (1) GEP20115309B (de)
GT (1) GT200900236A (de)
HR (1) HRP20120535T1 (de)
IL (1) IL200401A0 (de)
MA (1) MA31204B1 (de)
MX (1) MX2009009233A (de)
NI (1) NI200900161A (de)
NZ (1) NZ578854A (de)
PA (1) PA8771101A1 (de)
PE (1) PE20090166A1 (de)
PL (1) PL2131845T3 (de)
PT (1) PT2131845E (de)
RS (1) RS52351B (de)
SI (1) SI2131845T1 (de)
SM (1) SMAP200900080A (de)
TN (1) TN2009000357A1 (de)
TW (1) TW200844102A (de)
UA (1) UA101950C2 (de)
UY (1) UY30943A1 (de)
WO (1) WO2008104595A1 (de)
ZA (1) ZA200905417B (de)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
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
WO2010060854A1 (en) 2008-11-25 2010-06-03 Nerviano Medical Sciences S.R.L. Bicyclic pyrazole and isoxazole derivatives as antitumor and antineurodegenerative agents
JP5845193B2 (ja) * 2010-01-21 2016-01-20 アプレア エイビー 過増殖性疾患、自己免疫疾患、および心疾患の治療のための３−キヌクリジノンを含有する水溶液
KR101392086B1 (ko) * 2010-02-17 2014-05-07 일동제약주식회사 신규 5각 헤테로 고리 유도체 및 그 제조방법
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2515726C (en) * 2003-02-11 2012-07-10 Vernalis (Cambridge) Limited Isoxazole compounds
US20060070405A1 (en) * 2004-10-06 2006-04-06 Anheuser-Busch, Inc. Method for the production of amber glass with reduced sulfur-containing emissions
US20100069458A1 (en) 2007-02-15 2010-03-18 Peter Wisdom Atadja Combination of lbh589 with other therapeutic agents for treating cancer
WO2010069458A1 (de) 2008-12-17 2010-06-24 Merck Patent Gmbh Hexahalochromat(lll)-komplexe

Also Published As

Publication number Publication date
AU2008220800A1 (en) 2008-09-04
EP2131845A1 (de) 2009-12-16
EP2545921A2 (de) 2013-01-16
TN2009000357A1 (en) 2010-12-31
NZ578854A (en) 2012-03-30
CN101636162A (zh) 2010-01-27
AU2008220800B2 (en) 2012-02-16
DK2131845T3 (da) 2012-07-16
NI200900161A (es) 2010-07-27
AR065519A1 (es) 2009-06-10
US8163747B2 (en) 2012-04-24
US8487095B2 (en) 2013-07-16
GT200900236A (es) 2011-09-14
CL2008000618A1 (es) 2008-09-12
UA101950C2 (ru) 2013-05-27
CY1113805T1 (el) 2016-07-27
PE20090166A1 (es) 2009-03-14
EP2545921A3 (de) 2013-04-10
PL2131845T3 (pl) 2012-09-28
KR20090122218A (ko) 2009-11-26
UY30943A1 (es) 2008-10-31
US20100093732A1 (en) 2010-04-15
EP2131845B1 (de) 2012-04-11
CA2678043A1 (en) 2008-09-04
CN102302500A (zh) 2012-01-04
MA31204B1 (fr) 2010-02-01
EA017075B1 (ru) 2012-09-28
JP2010520176A (ja) 2010-06-10
PA8771101A1 (es) 2009-02-09
MX2009009233A (es) 2010-06-02
ES2384906T3 (es) 2012-07-13
GEP20115309B (en) 2011-10-25
ECSP099602A (es) 2009-12-28
EA200901141A1 (ru) 2010-04-30
TW200844102A (en) 2008-11-16
PT2131845E (pt) 2012-07-10
WO2008104595A1 (en) 2008-09-04
IL200401A0 (en) 2010-04-29
HRP20120535T1 (hr) 2012-07-31
SMAP200900080A (it) 2010-01-19
CO6210828A2 (es) 2010-10-20
BRPI0807992A2 (pt) 2014-06-17
DOP2009000209A (es) 2009-09-15
ZA200905417B (en) 2010-05-26
CR10989A (es) 2010-03-01
SI2131845T1 (sl) 2013-02-28
US20120172592A1 (en) 2012-07-05
RS52351B (sr) 2012-12-31
HK1139073A1 (en) 2010-09-10
US20130296556A1 (en) 2013-11-07

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