JP2013525290A - Ｋｓｐ阻害剤としてのオキサゾールおよびチアゾール化合物 - Google Patents

Ｋｓｐ阻害剤としてのオキサゾールおよびチアゾール化合物 Download PDF

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JP2013525290A
JP2013525290A JP2013504270A JP2013504270A JP2013525290A JP 2013525290 A JP2013525290 A JP 2013525290A JP 2013504270 A JP2013504270 A JP 2013504270A JP 2013504270 A JP2013504270 A JP 2013504270A JP 2013525290 A JP2013525290 A JP 2013525290A
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JP2013525290A5 (enExample
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ポール・エイ・バーサンティ
ユ・ディング
ハン・ウソク
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ノバルティス アーゲー
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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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2013504270A 2010-04-15 2011-04-13 Ｋｓｐ阻害剤としてのオキサゾールおよびチアゾール化合物 Pending JP2013525290A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US32467810P 2010-04-15 2010-04-15
US61/324,678 2010-04-15
PCT/EP2011/055855 WO2011128388A2 (en) 2010-04-15 2011-04-13 Oxazole and thiazole compounds as ksp inhibitors

Publications (2)

Publication Number Publication Date
JP2013525290A true JP2013525290A (ja) 2013-06-20
JP2013525290A5 JP2013525290A5 (enExample) 2014-04-24

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JP2013504270A Pending JP2013525290A (ja) 2010-04-15 2011-04-13 Ｋｓｐ阻害剤としてのオキサゾールおよびチアゾール化合物

Country Status (5)

Country Link
US (1) US8748626B2 (enExample)
EP (1) EP2558452A2 (enExample)
JP (1) JP2013525290A (enExample)
CN (1) CN103153970A (enExample)
WO (1) WO2011128388A2 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013523867A (ja) * 2010-04-15 2013-06-17 ノバルティス アーゲー Ｋｓｐ阻害剤としてのトリアゾール化合物

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2968591A1 (en) * 2013-03-15 2016-01-20 Novartis AG Cell proliferation inhibitors and conjugates thereof
WO2015113920A1 (en) * 2014-01-29 2015-08-06 Bayer Pharma Aktiengesellschaft Amino-substituted isothiazoles
EP2980088A1 (en) * 2014-07-28 2016-02-03 Bayer Pharma Aktiengesellschaft Amino-substituted isothiazoles
WO2016020791A1 (en) 2014-08-05 2016-02-11 Novartis Ag Ckit antibody drug conjugates

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008502721A (ja) * 2004-05-21 2008-01-31 ノバルティス ヴァクシンズ アンド ダイアグノスティクス， インコーポレイテッド 分裂キネシンインヒビターとしての置換キノリン誘導体
JP2008503501A (ja) * 2004-06-18 2008-02-07 カイロン コーポレイション 癌を治療するためのキネシンスピンドルタンパク質（ｋｓｐ）阻害剤としてのｎ−（１−（１−ベンジル−４−フェニル−１ｈ−イミダゾール−２−イル）−２，２−ジメチルプロピル）ベンズアミド誘導体および関連化合物
JP2008517057A (ja) * 2004-10-19 2008-05-22 ノバルティス ヴァクシンズ アンド ダイアグノスティクス， インコーポレイテッド インドールおよびベンゾイミダゾール誘導体
JP2008527038A (ja) * 2005-01-19 2008-07-24 メルク エンド カムパニー インコーポレーテッド 有糸分裂キネシン阻害剤
JP2008535839A (ja) * 2005-04-07 2008-09-04 メルク エンド カムパニー インコーポレーテッド 有糸分裂キネシン阻害剤
WO2009077448A1 (en) * 2007-12-14 2009-06-25 Novartis Ag Kinesin inhibitors as cancer therapeutics
JP2009542658A (ja) * 2006-06-27 2009-12-03 ザ プロクター アンド ギャンブル カンパニー ヒトプロテインチロシンホスファターゼβ阻害剤および使用法
JP2010509365A (ja) * 2006-11-13 2010-03-25 ノバルティス アーゲー Ｋｓｐ阻害剤としての置換ピラゾールおよびトリアゾール化合物
JP2013523867A (ja) * 2010-04-15 2013-06-17 ノバルティス アーゲー Ｋｓｐ阻害剤としてのトリアゾール化合物

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US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4501728A (en) 1983-01-06 1985-02-26 Technology Unlimited, Inc. Masking of liposomes from RES recognition
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US4837028A (en) 1986-12-24 1989-06-06 Liposome Technology, Inc. Liposomes with enhanced circulation time
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NO318318B1 (no) * 2003-06-27 2005-02-28 Tandberg Telecom As Fremgangsmate for forbedret koding av video
GEP20125415B (en) * 2007-01-05 2012-03-12 Novartis Ag Imidazole derivatives as kinesin spindle protein inhibitors (eg-5)
AU2008257044A1 (en) * 2007-05-24 2008-12-04 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
WO2009052288A1 (en) * 2007-10-19 2009-04-23 Schering Corporation Spiro-condensed 1, 3, 4-thiadiazole derivatives for inhibiting ksp kinesin activity

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JP2008502721A (ja) * 2004-05-21 2008-01-31 ノバルティス ヴァクシンズ アンド ダイアグノスティクス， インコーポレイテッド 分裂キネシンインヒビターとしての置換キノリン誘導体
JP2008503501A (ja) * 2004-06-18 2008-02-07 カイロン コーポレイション 癌を治療するためのキネシンスピンドルタンパク質（ｋｓｐ）阻害剤としてのｎ−（１−（１−ベンジル−４−フェニル−１ｈ−イミダゾール−２−イル）−２，２−ジメチルプロピル）ベンズアミド誘導体および関連化合物
JP2008517057A (ja) * 2004-10-19 2008-05-22 ノバルティス ヴァクシンズ アンド ダイアグノスティクス， インコーポレイテッド インドールおよびベンゾイミダゾール誘導体
JP2008527038A (ja) * 2005-01-19 2008-07-24 メルク エンド カムパニー インコーポレーテッド 有糸分裂キネシン阻害剤
JP2008535839A (ja) * 2005-04-07 2008-09-04 メルク エンド カムパニー インコーポレーテッド 有糸分裂キネシン阻害剤
JP2009542658A (ja) * 2006-06-27 2009-12-03 ザ プロクター アンド ギャンブル カンパニー ヒトプロテインチロシンホスファターゼβ阻害剤および使用法
JP2010509365A (ja) * 2006-11-13 2010-03-25 ノバルティス アーゲー Ｋｓｐ阻害剤としての置換ピラゾールおよびトリアゾール化合物
WO2009077448A1 (en) * 2007-12-14 2009-06-25 Novartis Ag Kinesin inhibitors as cancer therapeutics
JP2013523867A (ja) * 2010-04-15 2013-06-17 ノバルティス アーゲー Ｋｓｐ阻害剤としてのトリアゾール化合物

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013523867A (ja) * 2010-04-15 2013-06-17 ノバルティス アーゲー Ｋｓｐ阻害剤としてのトリアゾール化合物

Also Published As

Publication number Publication date
US8748626B2 (en) 2014-06-10
CN103153970A (zh) 2013-06-12
WO2011128388A2 (en) 2011-10-20
US20130224186A1 (en) 2013-08-29
WO2011128388A3 (en) 2013-03-14
EP2558452A2 (en) 2013-02-20

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