CN1993331A - N－(1－(1－苄基－4－苯基－1h－咪唑－2－基 )－2 , 2－二甲基丙基)苯甲酰胺衍生物和相关化合物作为用于治疗癌症的驱动蛋白纺锤蛋白(ksp)抑制剂 - Google Patents

N－(1－(1－苄基－4－苯基－1h－咪唑－2－基 )－2 , 2－二甲基丙基)苯甲酰胺衍生物和相关化合物作为用于治疗癌症的驱动蛋白纺锤蛋白(ksp)抑制剂 Download PDF

Info

Publication number
CN1993331A
CN1993331A CNA2005800262037A CN200580026203A CN1993331A CN 1993331 A CN1993331 A CN 1993331A CN A2005800262037 A CNA2005800262037 A CN A2005800262037A CN 200580026203 A CN200580026203 A CN 200580026203A CN 1993331 A CN1993331 A CN 1993331A
Authority
CN
China
Prior art keywords
bases
imidazoles
propyls
methyl
phenyl
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
CNA2005800262037A
Other languages
English (en)
Chinese (zh)
Inventor
王为波
P·A·巴杉蒂
Y·希
R·S·博埃斯
S·佩奇
N·布拉默尔
M·菲利浦斯
K·门登豪
K·威曼
L·M·拉格尼顿
R·康斯坦丁
H·杨
E·米厄利
S·拉莫西
E·加赞
A·沙尔马
J·拉马
S·萨布马尼安
P·伦豪
K·W·贝尔
D·杜尔
A·瓦尔特
T·阿布拉姆斯
K·许
E·马丁
M·奈普
V·列
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis Vaccines and Diagnostics Inc
Original Assignee
Chiron Corp
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=34980173&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN1993331(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Chiron Corp filed Critical Chiron Corp
Publication of CN1993331A publication Critical patent/CN1993331A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/24—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D405/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D413/06—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 only aliphatic carbon 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CNA2005800262037A 2004-06-18 2005-06-20 N－(1－(1－苄基－4－苯基－1h－咪唑－2－基 )－2 , 2－二甲基丙基)苯甲酰胺衍生物和相关化合物作为用于治疗癌症的驱动蛋白纺锤蛋白(ksp)抑制剂 Pending CN1993331A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US58092704P 2004-06-18 2004-06-18
US60/580,927 2004-06-18

Publications (1)

Publication Number Publication Date
CN1993331A true CN1993331A (zh) 2007-07-04

Family

ID=34980173

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA2005800262037A Pending CN1993331A (zh) 2004-06-18 2005-06-20 N－(1－(1－苄基－4－苯基－1h－咪唑－2－基 )－2 , 2－二甲基丙基)苯甲酰胺衍生物和相关化合物作为用于治疗癌症的驱动蛋白纺锤蛋白(ksp)抑制剂

Country Status (21)

Country Link
US (3) US7576221B2 (enExample)
EP (1) EP1765789B1 (enExample)
JP (2) JP4836280B2 (enExample)
KR (1) KR101170925B1 (enExample)
CN (1) CN1993331A (enExample)
AU (1) AU2005258135B2 (enExample)
BR (1) BRPI0510929A (enExample)
CA (1) CA2571002A1 (enExample)
EC (1) ECSP077183A (enExample)
ES (1) ES2409345T3 (enExample)
IL (1) IL180147A0 (enExample)
MA (1) MA28739B1 (enExample)
MX (1) MXPA06014909A (enExample)
NO (1) NO20070343L (enExample)
NZ (1) NZ552510A (enExample)
RU (1) RU2427572C2 (enExample)
SG (1) SG153851A1 (enExample)
TN (1) TNSN06419A1 (enExample)
TW (1) TW200612958A (enExample)
WO (1) WO2006002236A1 (enExample)
ZA (1) ZA200700481B (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102844307A (zh) * 2010-04-15 2012-12-26 诺瓦提斯公司 作为ksp抑制剂的三唑化合物
CN101939005B (zh) * 2007-12-14 2015-12-16 诺华股份有限公司 作为癌症治疗剂的驱动蛋白抑制剂
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）
CN107635586A (zh) * 2014-12-15 2018-01-26 拜耳医药股份有限公司 Ksp抑制剂与无糖基化抗‑tweakr抗体的抗体‑药物缀合物(adc)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7576221B2 (en) * 2004-06-18 2009-08-18 Novartis Vaccines And Diagnostics, Inc. Substituted imidazole derivatives
UY29070A1 (es) 2004-08-18 2006-03-31 Astrazeneca Ab Enantiómeros de heterocíclicos fusionados y sus usos
WO2007011647A2 (en) * 2005-07-15 2007-01-25 Kalypsys, Inc. Inhibitors of mitotic kinesin ksp
TW200800951A (en) * 2005-08-09 2008-01-01 Novartis Ag Substituted imidazole compounds as KSP inhibitors
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
PE20080359A1 (es) 2006-04-19 2008-06-06 Novartis Ag Compuestos de benzoxazol y benzotiazol 6-0-sustituidos y metodos de inhibicion de la senalizacion de csf-1r
EP2090570B1 (en) 2006-09-05 2011-11-09 Kyowa Hakko Kirin Co., Ltd. Imidazole derivative
JP2010505962A (ja) 2006-10-09 2010-02-25 武田薬品工業株式会社 キナーゼ阻害剤
US7902240B2 (en) * 2006-11-13 2011-03-08 Novartis Ag Substituted pyrazole and triazole compounds as KSP inhibitors
EP2106399A2 (en) * 2007-01-05 2009-10-07 Novartis AG Imidazole derivatives as kinesin spindle protein inhibitors (eg-5)
US20110275685A1 (en) 2009-01-26 2011-11-10 Michael Mutz Salt and polymorphs of a kinesin inhibitor compound
US8748626B2 (en) 2010-04-15 2014-06-10 Novartis Ag Oxazole and thiazole compounds as KSP inhibitors
DE102010025663A1 (de) 2010-06-30 2012-01-05 Karl-Heinz Glüsenkamp Neue beta-Aminoaldehyd-Derivate, Verfahren zu ihrer Herstellung und ihre chemische Verwendung als reaktive Intermediate
US8809372B2 (en) 2011-09-30 2014-08-19 Asana Biosciences, Llc Pyridine derivatives
WO2014151030A1 (en) * 2013-03-15 2014-09-25 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
IS2977B (is) 2015-02-23 2017-07-15 Actavis Group Ptc Ehf. Aðferð til framleiðslu á milliefnum sem eru nytsamleg við nýsmíði á elúxadólíni
SG10201908685QA (en) 2015-06-22 2019-10-30 Bayer Pharma AG Antibody drug conjugates (adcs) and antibody prodrug conjugates (apdcs) with enzymatically cleavable groups
JP2018525334A (ja) 2015-06-23 2018-09-06 バイエル ファーマ アクチエンゲゼルシャフト キネシンスピンドルタンパク質（ｋｓｐ）阻害剤の抗ｔｗｅａｋｒ抗体との抗体薬物複合体
CA2990300A1 (en) 2015-06-23 2016-12-29 Hans-Georg Lerchen Site specific homogeneous conjugates with ksp inhibitors
CA2990411A1 (en) 2015-06-23 2016-12-29 Bayer Pharma Aktiengesellschaft Antibody drug conjugates of kinesin spindel protein (ksp) inhibitors with anti-b7h3-antibodies
CA3027445A1 (en) 2016-06-15 2017-12-21 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies
WO2018114804A1 (de) 2016-12-21 2018-06-28 Bayer Pharma Aktiengesellschaft Spezifische antikörper-wirkstoff-konjugate (adcs) mit ksp-inhibitoren
MX2019007641A (es) 2016-12-21 2019-09-09 Bayer Pharma AG Conjugados de ligando-farmaco (adcs) con grupos escindibles enzimaticamente.
CN112601553A (zh) 2018-06-18 2021-04-02 拜耳股份有限公司 具有可酶切的接头和改善的活性谱的针对cxcr5的结合剂-药物缀合物
CA3123871A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
TW202317092A (zh) 2021-08-26 2023-05-01 美商佛拉斯托醫療公司 Ｋｉｆ１８ａ之吲哚啉抑制劑

Family Cites Families (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2550959C3 (de) * 1975-11-13 1980-12-04 Hoechst Ag, 6000 Frankfurt Tetrazolyl-imidazole und Tetrazolyl--benzimidazole, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel
WO1998027108A2 (en) 1996-12-16 1998-06-25 Fujisawa Pharmaceutical Co., Ltd. New amide compounds and their use as nitric oxide synthase inhibitors
US6117940A (en) 1997-10-17 2000-09-12 Mjalli; Adnan M. M. Amino-ketone solid support templates
BR9912729A (pt) * 1998-08-04 2001-05-02 Astrazeneca Ab Derivado de amida, processo para prepará-lo, e, uso do mesmo
AU761361B2 (en) * 1998-09-25 2003-06-05 Astrazeneca Ab Benzamide derivatives and their use as cytokine inhibitors
CA2369549A1 (en) 1999-04-02 2000-10-12 Robert W. Desimone Aryl and heteroaryl fused aminoalkyl-imidazole derivatives and their use as antidiabetics
US7291641B2 (en) * 1999-10-11 2007-11-06 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Derivatives of heterocycles with 5 members, their preparation and their use as medicaments
US20040132788A1 (en) * 1999-10-11 2004-07-08 Chabrier De Lassauniere Pierre-Etienne Derivatives of heterocycles with 5 members, their preparation and their use as medicaments
TWI292316B (en) * 1999-10-11 2008-01-11 Sod Conseils Rech Applic Pharmaceutical composition of thiazole derivatives intended to inhibit mao and/or lipidic peroxidation and/or to act as modulators of sodium channels and the use thereof
US6545004B1 (en) * 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
EP1686120A3 (en) 1999-10-27 2007-05-30 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
US6620882B1 (en) 2000-05-02 2003-09-16 Advanced Syntech, Llc Solid support template for preparation of highly functionalized heterocycle compounds
US6683191B2 (en) 2000-06-05 2004-01-27 Ortho-Mcneil Pharmaceuticals, Inc. Method for synthesis of substituted azole libraries
US6951948B2 (en) 2000-06-05 2005-10-04 Ortho-Mcneil Pharmaceutical, Inc. Method for synthesis of substituted azole libraries
KR20030020960A (ko) * 2000-08-01 2003-03-10 소시에떼 더 콘세이유 더 레세르세 에 다플리까띠옹 시엔띠피끄, 에스.아.에스. 이미다졸일 유도체
WO2002028839A1 (en) 2000-10-06 2002-04-11 Neurogen Corporation Benzimidazole and indole derivatives as crf receptor modulators
JP2002190437A (ja) 2000-12-20 2002-07-05 Advantest Corp 電子ビーム露光装置及び校正方法
WO2002056880A1 (en) 2001-01-19 2002-07-25 Cytokinetics, Inc. Triphenylmethane kinesin inhibitors
US6992082B2 (en) 2001-01-19 2006-01-31 Cytokinetics, Inc. Phenothiazine kinesin inhibitors
US6610723B2 (en) * 2001-01-29 2003-08-26 Hoffmann-La Roche Inc. Imidazole derivatives
US7049303B2 (en) 2001-11-07 2006-05-23 Medical Research Council Inhibition of viruses
US7060705B2 (en) 2001-11-07 2006-06-13 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2003043995A1 (en) 2001-11-20 2003-05-30 Cytokinetics, Inc. Process for the racemization of chiral quinazolinones
US7244723B2 (en) 2001-12-06 2007-07-17 Merck & Co., Inc. Substituted furopyrimidinones as a mitotic kinesin inhibitors
CA2467916A1 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Mitotic kinesin inhibitors
JP4391825B2 (ja) 2001-12-06 2009-12-24 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
EP1481077B1 (en) * 2001-12-06 2009-11-04 Merck & Co., Inc. Mitotic kinesin inhibitors
US7378411B2 (en) 2001-12-06 2008-05-27 Merck & Co., Inc. Substituted thienopyrimidinones as a mitotic kinesin inhibitor
US6906075B2 (en) 2002-01-10 2005-06-14 Neurogen Corp. Melanin concentrating hormone receptor ligands: substituted benzoimidazole analogues
US7009049B2 (en) 2002-02-15 2006-03-07 Cytokinetics, Inc. Syntheses of quinazolinones
CA2478068C (en) 2002-03-08 2011-02-08 Merck & Co., Inc. Dihydropyrazole compounds useful for treating or preventing cancer
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
DE10211770A1 (de) 2002-03-14 2003-10-02 Boehringer Ingelheim Pharma Neue substituierte Piperidine, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
AU2003245259A1 (en) 2002-05-02 2003-11-17 Neurogen Corporation Substituted imidazole derivatives: gabaa receptor ligands
US6982268B2 (en) 2002-05-08 2006-01-03 Neurogen Corporation Substituted imidazolylmethyl pyridine and pyrazine derivatives GABAA receptor ligands
US7214800B2 (en) 2002-05-09 2007-05-08 Cytokinetics, Inc. Compounds, compositions, and methods
US7166595B2 (en) * 2002-05-09 2007-01-23 Cytokinetics, Inc. Compounds, methods and compositions
EP1507534A4 (en) 2002-05-10 2006-11-08 Cytokinetics Inc COMPOUNDS, COMPOSITIONS AND METHODS
CA2486339A1 (en) 2002-05-17 2003-11-27 Neurogen Corporation Substituted ring-fused imidazole derivates: gabaa receptor ligands
US7038048B2 (en) * 2002-05-23 2006-05-02 Cytokinetics, Inc. 3H-pyridopyrimidin-4-one compounds, compositions, and methods of their use
AU2003231799A1 (en) 2002-05-23 2003-12-12 Merck & Co., Inc. Mitotic kinesin inhibitors
JP4463679B2 (ja) 2002-06-14 2010-05-19 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
JP4377323B2 (ja) 2002-06-14 2009-12-02 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
WO2004001489A1 (ja) 2002-06-19 2003-12-31 Mitsubishi Denki Kabushiki Kaisha 光変調器
EP1551962A4 (en) 2002-07-08 2007-08-01 Merck & Co Inc MITOTIC KINESIN BINDING CENTER
RU2233736C2 (ru) 2002-07-11 2004-08-10 Раховский Вадим Израилович Нанометрическое позиционирующее устройство
DE60326248D1 (de) 2002-07-17 2009-04-02 Cytokinetics Inc Verbindungen, zusammensetzungen und verfahren zur behandlung von zellulären proliferativen erkrankungen
JP2006501201A (ja) 2002-07-23 2006-01-12 サイトキネティクス・インコーポレーテッド 化合物、組成物および方法
KR100492252B1 (ko) 2002-08-09 2005-05-30 한국화학연구원 이미다졸을 포함하는 이차아민으로 치환된 벤조피란유도체 및 그의 제조방법
EP1539180A4 (en) 2002-08-21 2006-08-30 Cytokinetics Inc COMPOUNDS, COMPOSITIONS AND METHODS
WO2004024086A2 (en) 2002-09-13 2004-03-25 Cytokinetics, Inc. Compounds, compositions and methods
WO2004026859A1 (en) 2002-09-18 2004-04-01 Pfizer Products Inc. Novel imidazole compounds as transforming growth factor (tgf) inhibitors
EP1558083A4 (en) * 2002-09-30 2008-04-16 Cytokinetics Inc COMPOUNDS, COMPOSITIONS AND METHODS
CN100579579C (zh) 2002-10-01 2010-01-13 诺华疫苗和诊断公司 抗癌及抗感染性疾病组合物及其使用方法
MXPA05003830A (es) * 2002-10-11 2005-06-23 Cytokinetics Inc Compuestos, composiciones y metodos.
JP2006508102A (ja) 2002-11-08 2006-03-09 ニューロジェン・コーポレイション Ｇａｂａａ受容体のリガンドとしての４−イミダゾール−１−イルメチル−ピリミジン誘導体
US20040186151A1 (en) 2003-02-12 2004-09-23 Mjalli Adnan M.M. Substituted azole derivatives as therapeutic agents
US7662581B1 (en) * 2003-12-18 2010-02-16 Novartis Vaccines And Diagnostics, Inc. Eg5 co-crystals
DE602005016775D1 (de) 2004-01-16 2009-11-05 Wyeth Corp Heterocyclische, ein azol enthaltende sulfonamidinhibitoren der beta-amyloid-produktion
AU2005214349B2 (en) * 2004-02-12 2011-11-03 Transtech Pharma, Inc. Substituted azole derivatives, compositions, and methods of use
JP4895220B2 (ja) * 2004-04-06 2012-03-14 ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド キネシン有糸分裂インヒビター
US20080132549A1 (en) 2004-04-14 2008-06-05 Pfizer Inc. Sulphur-Linked Imidazone Compounds for the Treatment of Hiv/Aids
US7592453B2 (en) 2004-04-28 2009-09-22 Takeda Pharmaceutical Company Limited Fused quinoline derivative and use thereof
US7618981B2 (en) 2004-05-06 2009-11-17 Cytokinetics, Inc. Imidazopyridinyl-benzamide anti-cancer agents
US7576221B2 (en) * 2004-06-18 2009-08-18 Novartis Vaccines And Diagnostics, Inc. Substituted imidazole derivatives

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101939005B (zh) * 2007-12-14 2015-12-16 诺华股份有限公司 作为癌症治疗剂的驱动蛋白抑制剂
CN102844307A (zh) * 2010-04-15 2012-12-26 诺瓦提斯公司 作为ksp抑制剂的三唑化合物
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）
CN106163568B (zh) * 2013-12-23 2021-03-23 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）
CN107635586A (zh) * 2014-12-15 2018-01-26 拜耳医药股份有限公司 Ksp抑制剂与无糖基化抗‑tweakr抗体的抗体‑药物缀合物(adc)
CN107635586B (zh) * 2014-12-15 2021-09-24 拜耳医药股份有限公司 Ksp抑制剂与无糖基化抗-tweakr抗体的抗体-药物缀合物(adc)

Also Published As

Publication number Publication date
WO2006002236A1 (en) 2006-01-05
KR20070106961A (ko) 2007-11-06
EP1765789A1 (en) 2007-03-28
NO20070343L (no) 2007-03-05
JP4836280B2 (ja) 2011-12-14
BRPI0510929A (pt) 2007-07-17
MA28739B1 (fr) 2007-07-02
AU2005258135B2 (en) 2011-09-22
TW200612958A (en) 2006-05-01
EP1765789B1 (en) 2013-02-27
SG153851A1 (en) 2009-07-29
CA2571002A1 (en) 2006-01-05
ECSP077183A (es) 2007-02-28
IL180147A0 (en) 2007-06-03
US20130017196A1 (en) 2013-01-17
US20060009472A1 (en) 2006-01-12
NZ552510A (en) 2010-12-24
ZA200700481B (en) 2008-10-29
US8735599B2 (en) 2014-05-27
AU2005258135A1 (en) 2006-01-05
RU2007101612A (ru) 2008-08-10
JP2011256197A (ja) 2011-12-22
ES2409345T3 (es) 2013-06-26
US7576221B2 (en) 2009-08-18
JP2008503501A (ja) 2008-02-07
US20090258016A1 (en) 2009-10-15
TNSN06419A1 (en) 2008-02-22
KR101170925B1 (ko) 2012-08-07
US8318791B2 (en) 2012-11-27
MXPA06014909A (es) 2007-02-28
RU2427572C2 (ru) 2011-08-27

Similar Documents

Publication Publication Date Title
CN1993331A (zh) N－(1－(1－苄基－4－苯基－1h－咪唑－2－基 )－2 , 2－二甲基丙基)苯甲酰胺衍生物和相关化合物作为用于治疗癌症的驱动蛋白纺锤蛋白(ksp)抑制剂
CN1273466C (zh) 具有唑基的喹啉衍生物和喹唑啉衍生物
CN1267431C (zh) 取代的喹唑啉衍生物及其在制备作为抑制剂的药物中的用途
CN1269813C (zh) 作为细胞增生抑制剂的咪唑－5－基－2－苯胺基－嘧啶
CN1290165A (zh) 苯并噻唑蛋白酪氨酸激酶抑制剂
CN1044237C (zh) 4,1－苯并氧氮杂䓬衍生物和其用途
CN1989969A (zh) 蛋白酪氨酸激酶的环状抑制剂
CN1325390A (zh) 2－脲基噻唑衍生物及其制备方法和作为抗肿瘤剂的应用
CN1678586A (zh) 取代的喹啉ccr5受体拮抗剂
CN1910183A (zh) 四氢咔啉化合物作为抗癌药
CN1798749A (zh) 作为抗癌剂的杂芳基－稠合的嘧啶基化合物
CN101048402A (zh) 咔唑衍生物、其溶剂合物或其药学上允许的盐
CN1444582A (zh) 杂环化合物,它们的制备和用途
CN1503793A (zh) N-取代的非芳基-杂环nmda/nr2b拮抗剂
CN1250776A (zh) 杂双环衍生物
CN1809563A (zh) 吡啶并[1,2－a]嘧啶－4－酮化合物用作抗癌药
CN1625555A (zh) 喹唑啉化合物
CN1575284A (zh) 作为激酶抑制剂的取代的三唑二胺衍生物
CN1665788A (zh) 嘧啶酮类化合物、组合物及方法
CN1568187A (zh) 2h－2,3－二氮杂萘－1－酮和其使用方法
CN1553899A (zh) 抑制肝细胞生长因子受体自磷酸化的喹啉衍生物和喹唑啉衍生物以及含有这些化合物的药物组合物
CN1597667A (zh) 用作血管生成抑制剂的喹唑啉衍生物
CN1348370A (zh) 环状蛋白酪氨酸激酶抑制剂
CN1535266A (zh) 用作mGluR2拮抗剂Ⅱ的二氢-苯并[b][1,4]二氮杂�-2-酮衍生物
CN1889951A (zh) 取代的苯并唑及其用作raf激酶抑制剂的应用

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C12 Rejection of a patent application after its publication
RJ01 Rejection of invention patent application after publication

Open date: 20070704