BRPI0510929A - derivados de n-(1-(1-benzil-4-fenil-1h-imidazol-2-il)-2,2-dimetilpropil) benzamida e compostos relacionados como inibidores de proteìna de eixo de kinesin (ksp) para o tratamento de cáncer - Google Patents

derivados de n-(1-(1-benzil-4-fenil-1h-imidazol-2-il)-2,2-dimetilpropil) benzamida e compostos relacionados como inibidores de proteìna de eixo de kinesin (ksp) para o tratamento de cáncer

Info

Publication number
BRPI0510929A
BRPI0510929A BRPI0510929-9A BRPI0510929A BRPI0510929A BR PI0510929 A BRPI0510929 A BR PI0510929A BR PI0510929 A BRPI0510929 A BR PI0510929A BR PI0510929 A BRPI0510929 A BR PI0510929A
Authority
BR
Brazil
Prior art keywords
group
optionally substituted
substituted
hydrogen
aryl
Prior art date
Application number
BRPI0510929-9A
Other languages
English (en)
Inventor
Weibo Wang
Paul A Barsanti
Yi Xi
Rustum S Boyce
Sabina Pecchi
Nathan Brammeier
Megan Phillips
Kelly Wayman
Liana Lagniton
Ryan Constantine
Elizabeth Mieuli
Savithri Ramurthy
Elisa Jazan
Anu Sharma
Jain Rama
Sharadha Sabramanian
Paul A Renhowe
Kenneth Bair
David Duhl
Annette Walter
Tinya Abrams
Kay Huh
Eric Martin
Mark Knapp
Vincent Le
Kris Mendenhall
Hong Yang
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=BRPI0510929(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 BRPI0510929A publication Critical patent/BRPI0510929A/pt

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)

Abstract

DERIVADOS DE N-(1-BENZIL-4FENIL-1H-IMIDAZOL-2-IL)-2,2-DIMETILPROPIL) BENZAMIDA E COMPOSTOS RELACIONADOS COMO INIBIDORES DA PROTEìNA CINESINA DO FUSO (KSP PARA O TRATAMENTO DE CáNCER Esta invenção é dirigida aos compostos imidazol substituídos que modulam a atividade de KSP são úteis para o tratamento de cãncer e são representados pela fórmula (I) em que: R¬ 1¬ é selecionado do grupo que consiste em aminoacil, acilamino, carboxil, éster carboxílico, aril e aquil opcionalmente substituído com hidroxi ou halo; R¬ 2¬ é selecionado do grupo que consiste em hidrogênio, alquil e aril; R¬ 3¬ é selecionado do grupo que consiste em hidrogênioe X-A, em que X é selecionado do grupo que consiste em C (O)-, -C(S)-, -S(O)~ 2~ e -S(O)~ 2~-N (R)-, em que R é hidrogênio ou alquil; e A é selecionado do grupo que consiste em hidrogênio, alquil opcionalmente substituído.alcoxi opcionalmente substituído,aril opcionalmente substituído, carboxil, éster carboxílico, aminoacil, heteroaril opcionalmente substituído, heterocíclico opcionalmente substituído e cicloalquil opcionalmente subistituído em que os grupos opcionalmente substituídos são substituídos com 1 a 4 substituintes; R¬ 5¬ é selecionado do grupo que consiste em L-A, em que L é selecionado do grupo que consiste em -S(O)<sym>-, em que q é um ou dois, e C~ 1~ a C~ 5~ alquileno opcionalmente substituído com hidroxi, halo ou acilamino;e A ¬ 1¬ é selecionado do grupo que consiste em aril, aril substituído,heteroaril, heteroaril substituído, heterocíclico, heterocíclico substituido, cicloaquil e cicloalquil subastituido e um de R¬ 6¬ ou R¬ 7¬ é selecionado do grupo que consiste em heterocíclico, abril e heteroaril, todos os quais podem ser opcionalmente substituídos com (R¬ 8¬)<sym> em que R¬ 8¬ e m é um número inteiro de 1 a 3 e o outro de R¬ 6¬ ou R¬ 7¬ é selecionado do grupo que consiste em hidrogêncio,halo e alquil, ou R¬ 6¬ e R¬ 7¬ são ambos hidrogênio; os outros substituintes são definidos nas reivinicações.
BRPI0510929-9A 2004-06-18 2005-06-20 derivados de n-(1-(1-benzil-4-fenil-1h-imidazol-2-il)-2,2-dimetilpropil) benzamida e compostos relacionados como inibidores de proteìna de eixo de kinesin (ksp) para o tratamento de cáncer BRPI0510929A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US58092704P 2004-06-18 2004-06-18
PCT/US2005/022062 WO2006002236A1 (en) 2004-06-18 2005-06-20 N- (1- (1-benzyl -4-phenyl-1h-imidazol-2-yl) -2,2-dymethylpropyl) benzamide derivatives and related compounds as kinesin spindle protein (ksp) inhibitors for the treatment of cancer

Publications (1)

Publication Number Publication Date
BRPI0510929A true BRPI0510929A (pt) 2007-07-17

Family

ID=34980173

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0510929-9A BRPI0510929A (pt) 2004-06-18 2005-06-20 derivados de n-(1-(1-benzil-4-fenil-1h-imidazol-2-il)-2,2-dimetilpropil) benzamida e compostos relacionados como inibidores de proteìna de eixo de kinesin (ksp) para o tratamento de cáncer

Country Status (21)

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

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2427572C2 (ru) * 2004-06-18 2011-08-27 Чирон Корпорейшн N-(1-(1-бензил-4-фенил-1н-имидазол-2-ил)-2,2-диметилпропил)бензамидные производные и родственные соединения в качестве ингибиторов кинезинового белка веретена (ksp) для лечения рака
JP2008509977A (ja) 2004-08-18 2008-04-03 アストラゼネカ アクチボラグ 癌の処置及び予防における選択された縮合複素環の鏡像異性体及びその使用
WO2007011647A2 (en) * 2005-07-15 2007-01-25 Kalypsys, Inc. Inhibitors of mitotic kinesin ksp
MY147188A (en) * 2005-08-09 2012-11-14 Novartis Ag Substituted imidazole compounds as ksp inhibitors
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
MX2008013427A (es) 2006-04-19 2008-11-04 Novartis Ag Compuestos de benzoxazole y benzotiazole sustituidos-6-0 y metodos para inhibir la señalizacion csf-1r.
KR101404360B1 (ko) 2006-09-05 2014-06-09 교와 핫꼬 기린 가부시키가이샤 이미다졸 유도체
SG175609A1 (en) 2006-10-09 2011-11-28 Takeda Pharmaceutical Kinase inhibitors
BRPI0719002A2 (pt) 2006-11-13 2013-12-17 Novartis Ag Compostos de pirazol e triazol substituídos como inibidores de ksp
CA2674318A1 (en) * 2007-01-05 2008-07-17 Novartis Ag Cyclized derivatives as eg-5 inhibitors
US8252832B2 (en) 2007-12-14 2012-08-28 Novartis Ag Kinesin inhibitors as cancer therapeutics
US20110275685A1 (en) 2009-01-26 2011-11-10 Michael Mutz Salt and polymorphs of a kinesin inhibitor compound
CN103153970A (zh) * 2010-04-15 2013-06-12 诺瓦提斯公司 作为ksp抑制剂的*唑和噻唑化合物
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
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
CN105451773A (zh) * 2013-03-15 2016-03-30 诺华股份有限公司 细胞增殖抑制剂及其缀合物
US9498540B2 (en) 2013-03-15 2016-11-22 Novartis Ag Cell proliferation inhibitors and conjugates thereof
EP3086814B1 (de) 2013-12-23 2020-06-24 Bayer Pharma Aktiengesellschaft Binder-konjugate (adcs) mit ksp-inhibitoren
WO2016020791A1 (en) 2014-08-05 2016-02-11 Novartis Ag Ckit antibody drug conjugates
US10485880B2 (en) 2014-12-15 2019-11-26 Bayer Pharma Aktiengesellschaft Antibody-drug conjugates (ADCs) of KSP inhibitors with aglycosylated anti-TWEAKR antibodies
IS2977B (is) 2015-02-23 2017-07-15 Actavis Group Ptc Ehf. Aðferð til framleiðslu á milliefnum sem eru nytsamleg við nýsmíði á elúxadólíni
JP6971858B2 (ja) 2015-06-22 2021-11-24 バイエル ファーマ アクチエンゲゼルシャフト 酵素開裂性基を有する抗体薬物複合体（ａｄｃ）および抗体プロドラッグ複合体（ａｐｄｃ）
CN107921145A (zh) 2015-06-23 2018-04-17 拜耳医药股份有限公司 Ksp抑制剂与抗‑tweakr抗体的抗体药物缀合物（adc）
JP2018528161A (ja) 2015-06-23 2018-09-27 バイエル ファーマ アクチエンゲゼルシャフト Ｋｓｐ阻害剤との部位特異的均一複合体
US11071788B2 (en) 2015-06-23 2021-07-27 Bayer Pharma Aktiengesellschaft Antibody drug conjugates of kinesin spindel protein (KSP) inhibitors with antiB7H3-antibodies
WO2017216028A1 (en) 2016-06-15 2017-12-21 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies
KR102628678B1 (ko) * 2016-12-21 2024-01-25 바이엘 파마 악티엔게젤샤프트 효소적으로 절단가능한 기를 갖는 항체 약물 접합체 (adc)
US11433140B2 (en) 2016-12-21 2022-09-06 Bayer Pharma Aktiengesellschaft Specific antibody drug conjugates (ADCs) having KSP inhibitors
US20210275686A1 (en) 2018-06-18 2021-09-09 Bayer Aktiengesellschaft Binder/active agent conjugates directed against cxcr5, having enzymatically cleavable linkers and improved activity profile
IL283639B2 (en) * 2018-12-20 2024-06-01 Amgen Inc Kif18a inhibitors
CA3230123A1 (en) 2021-08-26 2023-03-02 Derek A. Cogan Spiro indoline inhibitors of kif18a

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
JP2001505585A (ja) 1996-12-16 2001-04-24 藤沢薬品工業株式会社 新規アミド化合物およびそれらの一酸化窒素シンターゼ阻害剤としての用途
US6117940A (en) 1997-10-17 2000-09-12 Mjalli; Adnan M. M. Amino-ketone solid support templates
MXPA01000895A (es) * 1998-08-04 2002-08-20 Astrazeneca Ab Derivados de amida utiles como inhibidores de la produccion de citocinas.
ATE254105T1 (de) * 1998-09-25 2003-11-15 Astrazeneca Ab Benzamid-derivate und ihre verwendung als cytokine inhibitoren
JP2002541146A (ja) 1999-04-02 2002-12-03 ニューロゲン コーポレイション アリールおよびヘテロアリール融合のアミノアルキル−イミダゾール誘導体および糖尿病薬としてのその使用
TWI283577B (en) * 1999-10-11 2007-07-11 Sod Conseils Rech Applic Pharmaceutical composition of imidazole derivatives acting as modulators of sodium channels and the use thereof
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
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
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
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
WO2001094318A2 (en) * 2000-06-05 2001-12-13 Ortho-Mcneil Pharmaceutical, Inc. Method for synthesis of substituted azole libraries
DE60128102T2 (de) * 2000-08-01 2008-01-03 Societe De Conseils De Recherches Et D`Applications Scientifiques (S.C.R.A.S.) Imidazolderivate
JP2004510765A (ja) 2000-10-06 2004-04-08 ニューロジェン・コーポレーション Ｃｒｆ受容体調節物質としてのベンズイミダゾールおよびインドール誘導体類
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
EP1360180A1 (en) 2001-01-19 2003-11-12 Cytokinetics, Inc. Phenothiazine kinesin inhibitors
WO2002056880A1 (en) 2001-01-19 2002-07-25 Cytokinetics, Inc. Triphenylmethane 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
JP2005511581A (ja) 2001-11-07 2005-04-28 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
AU2002346471A1 (en) 2001-11-20 2003-06-10 Cytokinetics, Inc. Process for the racemization of chiral quinazolinones
US20050107404A1 (en) 2001-12-06 2005-05-19 Fraley Mark E. Mitotic kinesin inhibitors
EP1458726B1 (en) 2001-12-06 2009-07-15 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2003049679A2 (en) * 2001-12-06 2003-06-19 Merck & Co., Inc. Mitotic kinesin inhibitors
CA2467726A1 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Mitotic kinesin inhibitors
ATE372341T1 (de) 2001-12-06 2007-09-15 Merck & Co Inc Inhibitoren von mitotischem kinesin
US6906075B2 (en) 2002-01-10 2005-06-14 Neurogen Corp. Melanin concentrating hormone receptor ligands: substituted benzoimidazole analogues
AU2003213092A1 (en) 2002-02-15 2003-09-09 Smithkline Beecham Corporation Syntheses of quinazolinones
EP1492487B1 (en) 2002-03-08 2009-11-11 Merck & Co., Inc. Mitotic kinesin inhibitors
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
JP2006515278A (ja) * 2002-05-08 2006-05-25 ニューロジェン コーポレイション 置換イミダゾリルメチルピリジン及びピラジン誘導体並びにそれらのｇａｂａａ受容体リガンドとしての使用
US7214800B2 (en) 2002-05-09 2007-05-08 Cytokinetics, Inc. Compounds, compositions, and methods
WO2003094839A2 (en) * 2002-05-09 2003-11-20 Cytokinetics, Inc. Pyrimidinone compounds, compositions and methods
WO2004026226A2 (en) 2002-05-10 2004-04-01 Cytokinetics, Inc. Compounds, compositions and methods
US6916827B2 (en) * 2002-05-17 2005-07-12 Neurogen Corporation Substituted ring-fused imidazole derivative: GABAA receptors ligands
AU2003265242A1 (en) 2002-05-23 2003-12-22 Cytokinetics, Inc. Compounds, compositions, and methods
EP1509507A4 (en) 2002-05-23 2006-09-13 Merck & Co Inc INHIBITORS OF MITOTIC KINESINE
ES2282647T3 (es) 2002-06-14 2007-10-16 MERCK &amp; CO., INC. Inhibidores de cinesina mitotica.
ATE446094T1 (de) 2002-06-14 2009-11-15 Merck & Co Inc Mitotische kinesin-hemmer
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
WO2004009036A2 (en) 2002-07-23 2004-01-29 Cytokinetics, Inc. Compounds compositions and methods
KR100492252B1 (ko) 2002-08-09 2005-05-30 한국화학연구원 이미다졸을 포함하는 이차아민으로 치환된 벤조피란유도체 및 그의 제조방법
AU2003262747A1 (en) 2002-08-21 2004-03-11 Cytokinetics, Inc. Compounds, compositions, and methods
JP2005539062A (ja) 2002-09-13 2005-12-22 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
DE60328028D1 (de) * 2002-09-18 2009-07-30 Pfizer Prod Inc Imidazolverbindungen als inhibitoren des transformierenden wachstumsfaktors (twf)
US7557115B2 (en) * 2002-09-30 2009-07-07 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
KR20050075356A (ko) * 2002-10-11 2005-07-20 싸이토키네틱스, 인코포레이티드 화합물, 조성물 및 방법
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
AU2005207835A1 (en) 2004-01-16 2005-08-11 Wyeth Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole
ZA200605526B (en) * 2004-02-12 2007-11-28 Transtech Pharma Inc Substituted azole derivatives, compositions and methods of use
KR20060135035A (ko) * 2004-04-06 2006-12-28 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 유사분열 키네신 억제제
EP1740550A1 (en) 2004-04-14 2007-01-10 Pfizer Limited Sulphur-linked imidazole compounds for the treament of hiv
BRPI0510365A (pt) * 2004-04-28 2007-11-06 Takeda Pharmaceutical composto, método de produção de um composto, antagonista do receptor nk2, pró-droga, agente farmacêutico, métodos para antagonizar um recpetor nk2 e para evitar ou tratar doenças gastrintestinais funcionais, e, uso do composto ou uma pró-droga do mesmo
US7618981B2 (en) 2004-05-06 2009-11-17 Cytokinetics, Inc. Imidazopyridinyl-benzamide anti-cancer agents
RU2427572C2 (ru) * 2004-06-18 2011-08-27 Чирон Корпорейшн N-(1-(1-бензил-4-фенил-1н-имидазол-2-ил)-2,2-диметилпропил)бензамидные производные и родственные соединения в качестве ингибиторов кинезинового белка веретена (ksp) для лечения рака

Also Published As

Publication number Publication date
US20060009472A1 (en) 2006-01-12
TW200612958A (en) 2006-05-01
AU2005258135A1 (en) 2006-01-05
EP1765789A1 (en) 2007-03-28
TNSN06419A1 (en) 2008-02-22
AU2005258135B2 (en) 2011-09-22
MXPA06014909A (es) 2007-02-28
US8318791B2 (en) 2012-11-27
NZ552510A (en) 2010-12-24
ZA200700481B (en) 2008-10-29
ECSP077183A (es) 2007-02-28
IL180147A0 (en) 2007-06-03
JP2011256197A (ja) 2011-12-22
KR20070106961A (ko) 2007-11-06
US8735599B2 (en) 2014-05-27
KR101170925B1 (ko) 2012-08-07
JP2008503501A (ja) 2008-02-07
CA2571002A1 (en) 2006-01-05
RU2007101612A (ru) 2008-08-10
US7576221B2 (en) 2009-08-18
WO2006002236A1 (en) 2006-01-05
EP1765789B1 (en) 2013-02-27
CN1993331A (zh) 2007-07-04
RU2427572C2 (ru) 2011-08-27
ES2409345T3 (es) 2013-06-26
SG153851A1 (en) 2009-07-29
MA28739B1 (fr) 2007-07-02
US20090258016A1 (en) 2009-10-15
NO20070343L (no) 2007-03-05
US20130017196A1 (en) 2013-01-17
JP4836280B2 (ja) 2011-12-14

Similar Documents

Publication Publication Date Title
BRPI0510929A (pt) derivados de n-(1-(1-benzil-4-fenil-1h-imidazol-2-il)-2,2-dimetilpropil) benzamida e compostos relacionados como inibidores de proteìna de eixo de kinesin (ksp) para o tratamento de cáncer
EA200870404A1 (ru) Производные азабицикло[3.1.0.]гексила в качестве модуляторов рецепторов допамина d3
ATE554065T1 (de) Sulfoniumsalz-fotoinitiatoren
WO2004072047A8 (en) Indoles, benzimidazoles or naphhimidazoles as histone deacetylase (hdac) inhibitors
WO2009109991A3 (en) Novel hydrazide containing tyrosine kinase inhibitors
NO20083404L (no) Substituerte imidazoler og deres anvendelse som pestisider
DE60226469D1 (de) Biphenylkarbonsäureamidderivate als p38 kinase-inhibitoren
CY1118498T1 (el) Παραγωγα πυριδαζινονης
EA200900857A1 (ru) Замещённые 1-(3-пиридинил)пиразол-4-ил-уксусные кислоты, способ их получения и их применение в качестве гербицидов и регуляторов роста растений
MX2013002558A (es) Derivado de imidazol de heteroanillo fusionado que tiene efecto de activacion de proteina cinasa activada por monofosfato de adenosina (amk).
EA200600509A1 (ru) Соединения пиримидотиофена
ATE479677T1 (de) Pyrimidinderivate als gpcr-agonisten
BRPI0514632A (pt) derivados de ftalazinona 4-heteroarilmetila substituìdos
DE602004023207D1 (de) Benzimidazol-derivate als mek-hemmer
ATE368045T1 (de) Salze mit cyanoborat-anionen
DK1268445T3 (da) 4-amino-5-cyano-2-anilinopyrimidinderivater og deres anvendelse som inhibitorer af cellecykluskinaser
ATE433981T1 (de) Heterocyclische verbindungen
ATE477256T1 (de) Thienylverbindungen
DE60334536D1 (de) Furylverbindungen
BRPI0601282A (pt) composição, e método de modificar a formação de hidrato de gás
BRPI0810661A2 (pt) [2,6] naftiridinas úteis como inibidoras de quinase proteica.
NO20063090L (no) Amidopyrazolderivater
EA201070781A1 (ru) Производные оксадиазола, активные на сфингозин-1-фосфате (s1p)
CO6331306A2 (es) Derivados de n-heterociclico-imidazo[1,2alfa]piridina-2-carboxamidas su preparacion y su aplicacion en terapeutica
EA200901100A1 (ru) Производные 4-(пирролопиридинил)пиримидин-2-иламина

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 9A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2260 DE 29/04/2014.