AU2008220800B2 - 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 - Google Patents

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 Download PDF

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Publication number
AU2008220800B2
AU2008220800B2 AU2008220800A AU2008220800A AU2008220800B2 AU 2008220800 B2 AU2008220800 B2 AU 2008220800B2 AU 2008220800 A AU2008220800 A AU 2008220800A AU 2008220800 A AU2008220800 A AU 2008220800A AU 2008220800 B2 AU2008220800 B2 AU 2008220800B2
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AU
Australia
Prior art keywords
phenyl
isoxazole
ylmethyl
isopropyl
morpholin
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AU2008220800A
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AU2008220800A1 (en
Inventor
Martin James Drysdale
Brian William Dymock
Christoph Krell
Michael Mutz
Holger Petersen
Weijia Zheng
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Novartis AG
Vernalis R&D Ltd
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Novartis AG
Vernalis R&D Ltd
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Publication of AU2008220800A1 publication Critical patent/AU2008220800A1/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/14Heterocyclic 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
    • C07D295/155Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06Heterocyclic 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
    • C07D261/10Heterocyclic 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
    • C07D261/18Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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)
  • 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)
AU2008220800A 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 Ceased AU2008220800B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP07103346.8 2007-03-01
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 (2)

Publication Number Publication Date
AU2008220800A1 AU2008220800A1 (en) 2008-09-04
AU2008220800B2 true AU2008220800B2 (en) 2012-02-16

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ID=38134307

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AU2008220800A Ceased AU2008220800B2 (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

Country Status (40)

Country Link
US (3) US8163747B2 (enExample)
EP (2) EP2545921A3 (enExample)
JP (1) JP2010520176A (enExample)
KR (1) KR20090122218A (enExample)
CN (2) CN101636162A (enExample)
AR (1) AR065519A1 (enExample)
AT (1) ATE552836T1 (enExample)
AU (1) AU2008220800B2 (enExample)
BR (1) BRPI0807992A2 (enExample)
CA (1) CA2678043A1 (enExample)
CL (1) CL2008000618A1 (enExample)
CO (1) CO6210828A2 (enExample)
CR (1) CR10989A (enExample)
CY (1) CY1113805T1 (enExample)
DK (1) DK2131845T3 (enExample)
DO (1) DOP2009000209A (enExample)
EA (1) EA017075B1 (enExample)
EC (1) ECSP099602A (enExample)
ES (1) ES2384906T3 (enExample)
GE (1) GEP20115309B (enExample)
GT (1) GT200900236A (enExample)
HR (1) HRP20120535T1 (enExample)
IL (1) IL200401A0 (enExample)
MA (1) MA31204B1 (enExample)
MX (1) MX2009009233A (enExample)
NI (1) NI200900161A (enExample)
NZ (1) NZ578854A (enExample)
PA (1) PA8771101A1 (enExample)
PE (1) PE20090166A1 (enExample)
PL (1) PL2131845T3 (enExample)
PT (1) PT2131845E (enExample)
RS (1) RS52351B (enExample)
SI (1) SI2131845T1 (enExample)
SM (1) SMAP200900080A (enExample)
TN (1) TN2009000357A1 (enExample)
TW (1) TW200844102A (enExample)
UA (1) UA101950C2 (enExample)
UY (1) UY30943A1 (enExample)
WO (1) WO2008104595A1 (enExample)
ZA (1) ZA200905417B (enExample)

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
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
JP2013519727A (ja) * 2010-02-17 2013-05-30 イルドン ファーム シーオー.,エルティーディー. 新規の5員複素環誘導体及びその製造方法
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004072051A1 (en) * 2003-02-11 2004-08-26 Vernalis (Cambridge) Limited Isoxazole compounds as inhibitors of heat shock proteins
US20060070405A1 (en) * 2004-10-06 2006-04-06 Anheuser-Busch, Inc. Method for the production of amber glass with reduced sulfur-containing emissions

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2677651A1 (en) 2007-02-15 2008-08-21 Novartis Ag Combinations of therapeutic agents for treating cancer
WO2010069458A1 (de) 2008-12-17 2010-06-24 Merck Patent Gmbh Hexahalochromat(lll)-komplexe

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004072051A1 (en) * 2003-02-11 2004-08-26 Vernalis (Cambridge) Limited Isoxazole compounds as inhibitors of heat shock proteins
US20060070405A1 (en) * 2004-10-06 2006-04-06 Anheuser-Busch, Inc. Method for the production of amber glass with reduced sulfur-containing emissions

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
D2: MORISSETTE S. L. et al., ADV. DRUG DELIVERY REVIEWS, vol. 56, no. 3, 2004, pages 275-300; *
D3: CAIRA M R, TOPICS IN CURRENT CHEMISTRY, VOL. 198, 1998, pages 163-208; *
D4: TONG W-Q et al., PHARM. DEVEL. AND TECHNOLOGY, vol. 3, no. 2, May 1998, pages 215-223; *
D5: GOULD P L, INT. JOURNAL OF PHARMACEUTICS, Vol. 33, no. 1/3, 1986, pages 201-217; *

Also Published As

Publication number Publication date
SI2131845T1 (sl) 2013-02-28
BRPI0807992A2 (pt) 2014-06-17
DOP2009000209A (es) 2009-09-15
WO2008104595A1 (en) 2008-09-04
UA101950C2 (ru) 2013-05-27
GEP20115309B (en) 2011-10-25
PE20090166A1 (es) 2009-03-14
TN2009000357A1 (en) 2010-12-31
ZA200905417B (en) 2010-05-26
NI200900161A (es) 2010-07-27
CR10989A (es) 2010-03-01
ATE552836T1 (de) 2012-04-15
CL2008000618A1 (es) 2008-09-12
AU2008220800A1 (en) 2008-09-04
CN101636162A (zh) 2010-01-27
DK2131845T3 (da) 2012-07-16
EP2545921A3 (en) 2013-04-10
MA31204B1 (fr) 2010-02-01
MX2009009233A (es) 2010-06-02
EP2545921A2 (en) 2013-01-16
RS52351B (sr) 2012-12-31
KR20090122218A (ko) 2009-11-26
CY1113805T1 (el) 2016-07-27
ECSP099602A (es) 2009-12-28
US20120172592A1 (en) 2012-07-05
PA8771101A1 (es) 2009-02-09
US8487095B2 (en) 2013-07-16
EA017075B1 (ru) 2012-09-28
CN102302500A (zh) 2012-01-04
NZ578854A (en) 2012-03-30
ES2384906T3 (es) 2012-07-13
CO6210828A2 (es) 2010-10-20
EP2131845B1 (en) 2012-04-11
GT200900236A (es) 2011-09-14
US20130296556A1 (en) 2013-11-07
US20100093732A1 (en) 2010-04-15
SMAP200900080A (it) 2010-01-19
UY30943A1 (es) 2008-10-31
AR065519A1 (es) 2009-06-10
PT2131845E (pt) 2012-07-10
EP2131845A1 (en) 2009-12-16
EA200901141A1 (ru) 2010-04-30
TW200844102A (en) 2008-11-16
HK1139073A1 (en) 2010-09-10
JP2010520176A (ja) 2010-06-10
IL200401A0 (en) 2010-04-29
PL2131845T3 (pl) 2012-09-28
CA2678043A1 (en) 2008-09-04
US8163747B2 (en) 2012-04-24
HRP20120535T1 (hr) 2012-07-31

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