CN101253167A - 作为ksp抑制剂的取代的咪唑化合物 - Google Patents

作为ksp抑制剂的取代的咪唑化合物 Download PDF

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Publication number
CN101253167A
CN101253167A CNA2006800293472A CN200680029347A CN101253167A CN 101253167 A CN101253167 A CN 101253167A CN A2006800293472 A CNA2006800293472 A CN A2006800293472A CN 200680029347 A CN200680029347 A CN 200680029347A CN 101253167 A CN101253167 A CN 101253167A
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CN
China
Prior art keywords
phenyl
benzyl
imidazoles
dimethyl
fluoro
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CNA2006800293472A
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English (en)
Chinese (zh)
Inventor
P·A·巴杉蒂
夏奕
王为波
K·G·门登豪尔
L·M·拉格尼顿
S·拉莫西
M·C·菲利浦斯
S·萨布拉马尼安
R·博埃斯
N·M·布拉默尔
R·康斯坦丁
D·杜尔
A·O·瓦尔特
T·J·阿布拉姆斯
P·A·任豪
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Novartis AG
Original Assignee
Novartis AG
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Filing date
Publication date
Application filed by Novartis AG filed Critical Novartis AG
Publication of CN101253167A publication Critical patent/CN101253167A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CNA2006800293472A 2005-08-09 2006-08-09 作为ksp抑制剂的取代的咪唑化合物 Pending CN101253167A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US70690105P 2005-08-09 2005-08-09
US60/706,901 2005-08-09

Publications (1)

Publication Number Publication Date
CN101253167A true CN101253167A (zh) 2008-08-27

Family

ID=37421032

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA2006800293472A Pending CN101253167A (zh) 2005-08-09 2006-08-09 作为ksp抑制剂的取代的咪唑化合物

Country Status (19)

Country Link
US (1) US7626040B2 (enExample)
EP (1) EP1912972B1 (enExample)
JP (1) JP4975745B2 (enExample)
KR (1) KR20080036611A (enExample)
CN (1) CN101253167A (enExample)
AR (1) AR056025A1 (enExample)
AT (1) ATE526324T1 (enExample)
AU (1) AU2006279991B2 (enExample)
BR (1) BRPI0614547A2 (enExample)
CA (1) CA2618747A1 (enExample)
ES (1) ES2374449T3 (enExample)
GT (1) GT200600366A (enExample)
MY (1) MY147188A (enExample)
PE (1) PE20070352A1 (enExample)
PL (1) PL1912972T3 (enExample)
PT (1) PT1912972E (enExample)
RU (1) RU2413721C9 (enExample)
TW (1) TW200800951A (enExample)
WO (1) WO2007021794A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106163568A (zh) * 2013-12-23 2016-11-23 拜耳制药股份公司 含纺锤体驱动蛋白（ksp）的抗体药物偶联物（adc）
CN109481436A (zh) * 2018-08-21 2019-03-19 广东医科大学 血栓素a2合成酶抑制剂奥扎格雷在制备治疗吸烟所致肺癌药物中的应用

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2009005071A (es) * 2006-11-13 2009-05-25 Novartis Ag Compuestos de pirazol y triazol sustituidos como inhibidores de ksp.
GEP20125415B (en) * 2007-01-05 2012-03-12 Novartis Ag Imidazole derivatives as kinesin spindle protein inhibitors (eg-5)
WO2009052288A1 (en) 2007-10-19 2009-04-23 Schering Corporation Spiro-condensed 1, 3, 4-thiadiazole derivatives for inhibiting ksp kinesin activity
US8252832B2 (en) * 2007-12-14 2012-08-28 Novartis Ag Kinesin inhibitors as cancer therapeutics
EP2558450A1 (en) 2010-04-15 2013-02-20 Novartis AG Triazole compounds as ksp inhibitors
EP2968591A1 (en) * 2013-03-15 2016-01-20 Novartis AG Cell proliferation inhibitors and conjugates thereof
US9498540B2 (en) 2013-03-15 2016-11-22 Novartis Ag Cell proliferation inhibitors and conjugates thereof
WO2016020791A1 (en) 2014-08-05 2016-02-11 Novartis Ag Ckit antibody drug conjugates
SG11201710639YA (en) * 2015-06-22 2018-01-30 Bayer Pharma AG Antibody drug conjugates (adcs) and antibody prodrug conjugates (apdcs) with enzymatically cleavable groups
CA2990398A1 (en) * 2015-06-23 2016-12-29 Bayer Pharma Aktiengesellschaft Antibody drug conjugates of kinesin spindel protein (ksp) inhibitors with anti-cd123-antibodies
WO2017216028A1 (en) 2016-06-15 2017-12-21 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies
US11433140B2 (en) 2016-12-21 2022-09-06 Bayer Pharma Aktiengesellschaft Specific antibody drug conjugates (ADCs) having KSP inhibitors
AU2017380871C1 (en) 2016-12-21 2025-05-15 Bayer Aktiengesellschaft Antibody drug conjugates (ADCs) having enzymatically cleavable groups
CA3103327A1 (en) 2018-06-18 2019-12-26 Bayer Aktiengesellschaft Binder/active agent conjugates directed against cxcr5, having enzymatically cleavable linkers and improved activity profile

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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
US4837028A (en) 1986-12-24 1989-06-06 Liposome Technology, Inc. Liposomes with enhanced circulation time
US5011472A (en) 1988-09-06 1991-04-30 Brown University Research Foundation Implantable delivery system for biological factors
EP0946587A2 (en) 1996-12-16 1999-10-06 Fujisawa Pharmaceutical Co., Ltd. New amide compounds
US6117940A (en) 1997-10-17 2000-09-12 Mjalli; Adnan M. M. Amino-ketone solid support templates
HUP0202648A3 (en) * 1998-06-12 2003-02-28 Sod Conseils Rech Applic Imidazolyl derivatives, pharmaceutical compositions containing them and their use
EP1226129B1 (en) * 1999-10-27 2006-05-24 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
US6545004B1 (en) * 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
AU2001227812A1 (en) 2000-05-02 2001-11-12 Advanced Syntech, Llc A Kentucky Limited Liability Corporation A novel solid support template for preparation of highly functionalized heterocycle compounds
US7566734B2 (en) * 2000-08-01 2009-07-28 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Imidazolyl derivatives
DE10211770A1 (de) 2002-03-14 2003-10-02 Boehringer Ingelheim Pharma Neue substituierte Piperidine, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
US7026312B2 (en) 2002-03-14 2006-04-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Substituted piperidines, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof
RU2005100783A (ru) * 2002-06-14 2005-07-20 Мерк энд Ко., Инк. (US) Ингибиторы митотического кинезина
US20040186151A1 (en) 2003-02-12 2004-09-23 Mjalli Adnan M.M. Substituted azole derivatives as therapeutic agents
EP1620092A4 (en) * 2003-05-07 2008-04-16 Cytokinetics Inc COMPOUNDS, COMPOSITIONS AND METHODS
WO2004103282A2 (en) * 2003-05-15 2004-12-02 Cytokinetics, Inc. Compounds, compositions and methods
EP1740550A1 (en) 2004-04-14 2007-01-10 Pfizer Limited Sulphur-linked imidazole compounds for the treament of hiv
US7618981B2 (en) 2004-05-06 2009-11-17 Cytokinetics, Inc. Imidazopyridinyl-benzamide anti-cancer agents
MXPA06014909A (es) * 2004-06-18 2007-02-28 Chiron Corp Derivados de n-(1-(1-bencil -4-fenil-1h -imidazol -2-il)-2, 2-dimetilpropil) benzamida y compuestos relacionados como inhibidores de proteina de huso de cinesina (ksp) para el tratamiento del cancer.

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106163568A (zh) * 2013-12-23 2016-11-23 拜耳制药股份公司 含纺锤体驱动蛋白（ksp）的抗体药物偶联物（adc）
CN109481436A (zh) * 2018-08-21 2019-03-19 广东医科大学 血栓素a2合成酶抑制剂奥扎格雷在制备治疗吸烟所致肺癌药物中的应用

Also Published As

Publication number Publication date
RU2413721C9 (ru) 2011-05-20
GT200600366A (es) 2007-05-10
EP1912972A1 (en) 2008-04-23
CA2618747A1 (en) 2007-02-22
US7626040B2 (en) 2009-12-01
EP1912972B1 (en) 2011-09-28
ES2374449T3 (es) 2012-02-16
AU2006279991A1 (en) 2007-02-22
KR20080036611A (ko) 2008-04-28
RU2413721C2 (ru) 2011-03-10
BRPI0614547A2 (pt) 2011-03-29
AR056025A1 (es) 2007-09-12
PT1912972E (pt) 2012-01-06
ATE526324T1 (de) 2011-10-15
PE20070352A1 (es) 2007-05-30
MY147188A (en) 2012-11-14
PL1912972T3 (pl) 2012-02-29
AU2006279991B2 (en) 2011-09-29
RU2008108939A (ru) 2009-09-20
JP2009504664A (ja) 2009-02-05
US20070037853A1 (en) 2007-02-15
JP4975745B2 (ja) 2012-07-11
WO2007021794A1 (en) 2007-02-22
HK1111995A1 (en) 2008-08-22
TW200800951A (en) 2008-01-01

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SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Open date: 20080827