PE20070352A1 - Compuestos de imidazol sustituidos como inhibidores de ksp - Google Patents

Compuestos de imidazol sustituidos como inhibidores de ksp

Info

Publication number
PE20070352A1
PE20070352A1 PE2006000968A PE2006000968A PE20070352A1 PE 20070352 A1 PE20070352 A1 PE 20070352A1 PE 2006000968 A PE2006000968 A PE 2006000968A PE 2006000968 A PE2006000968 A PE 2006000968A PE 20070352 A1 PE20070352 A1 PE 20070352A1
Authority
PE
Peru
Prior art keywords
substituted
alkyl
imidazol
aminopropyl
carboxamide
Prior art date
Application number
PE2006000968A
Other languages
English (en)
Inventor
Paul A Barsanti
Yi Xia
Kris G Mendenhall
Savithri Ramurthy
Sharadha Subramanian
Nathan M Brammeier
David Duhl
Tinya J Abrams
Paul A Renhowe
Annette O Walter
Ryan Constantine
Rustum Boyce
Megan C Phillips
Liana M Lagniton
Weibo Wang
Original Assignee
Novartis Ag
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
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20070352A1 publication Critical patent/PE20070352A1/es

Links

Classifications

    • 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

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R1 ES AMINOACILO, CARBOXILO, ALQUILO C1-C6, ENTRE OTROS; R2 ES H, ALQUILO C1-C6, ARILO C6-C14; R3 Y R4 SON CADA UNO H, OH, ALQUILO C1-C6 OPCIONALMENTE SUSTITUIDO CON NH2, CN, HALOGENO, NITRO, ENTRE OTROS, CICLOALQUILO C3-C10 OPCIONALMENTE SUSTITUIDO CON OXO, TIOXO, NH2, ENTRE OTROS; R5 ES H, ALQUILO C1-C6 SUSTITUIDO O NO CON NH2, CN, HALOGENO, NITRO, ENTRE OTROS, ALQUENILO C2-C6 SUSTITUIDO O NO, ENTRE OTROS; R6 Y R7 SON CADA UNO CICLOALQUILO C3-C10, ARILO C6-C14, HETEROARILO, ENTRE OTROS; R8 ES L-A1; L ES ALQUILENO C1-C5 SUSTITUIDO O NO CON OH, HALO, ACILAMINO, S(O)q; q ES 1-4; A1 ES ARILO C6-C14, HETEROARILO, HETEROCICLICO, CICLOALQUILO C3-C10 SUSTITUIDO O NO CON OH, NH2, CN, TIOL, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-(3-AMINOPROPIL)-N-{(1R)-1-[1-BENCIL-4-(3-CLOROFENIL)-1H-IMIDAZOL-2-IL]-2-METILPROPIL}MORFOLIN-4-CARBOXAMIDA; N-(3-AMINOPROPIL)-N-{(1R)-1-[1-BENCIL-4-(3-CLOROFENIL)-1H-IMIDAZOL-2-IL]-2-METILPROPIL}PIPERIDIN-1-CARBOXAMIDA; N-(3-AMINOPROPIL)-N-[(1R)-1-(1-BENCIL-4-FENIL-1H-IMIDAZOL-2-IL)-2,2-DIMETILPROPIL]PIPERIDIN-1-CARBOXAMIDA; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA PROTEINA QUINESINA DEL HUSO (KSP) SIENDO UTILES EN EL TRATAMIENTO DE CANCER DE PULMON, DE MAMA, DE PANCREAS, DE ESTOMAGO, LEUCEMIA MIELOIDE
PE2006000968A 2005-08-09 2006-08-09 Compuestos de imidazol sustituidos como inhibidores de ksp PE20070352A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US70690105P 2005-08-09 2005-08-09

Publications (1)

Publication Number Publication Date
PE20070352A1 true PE20070352A1 (es) 2007-05-30

Family

ID=37421032

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006000968A PE20070352A1 (es) 2005-08-09 2006-08-09 Compuestos de imidazol sustituidos como inhibidores de ksp

Country Status (20)

Country Link
US (1) US7626040B2 (es)
EP (1) EP1912972B1 (es)
JP (1) JP4975745B2 (es)
KR (1) KR20080036611A (es)
CN (1) CN101253167A (es)
AR (1) AR056025A1 (es)
AT (1) ATE526324T1 (es)
AU (1) AU2006279991B2 (es)
BR (1) BRPI0614547A2 (es)
CA (1) CA2618747A1 (es)
ES (1) ES2374449T3 (es)
GT (1) GT200600366A (es)
HK (1) HK1111995A1 (es)
MY (1) MY147188A (es)
PE (1) PE20070352A1 (es)
PL (1) PL1912972T3 (es)
PT (1) PT1912972E (es)
RU (1) RU2413721C9 (es)
TW (1) TW200800951A (es)
WO (1) WO2007021794A1 (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8129358B2 (en) * 2006-11-13 2012-03-06 Novartis Ag Substituted pyrazole and triazole compounds as KSP inhibitors
US7820646B2 (en) * 2007-01-05 2010-10-26 Novartis Vaccines And Diagnostics, Inc. Cyclized derivatives as Eg-5 inhibitors
ES2565983T3 (es) 2007-10-19 2016-04-08 Merck Sharp & Dohme Corp. Derivados de 1,3,4-tiadiazol espiro-condensados para inhibir la actividad quinesina de KSP
US8252832B2 (en) 2007-12-14 2012-08-28 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
US9498540B2 (en) 2013-03-15 2016-11-22 Novartis Ag Cell proliferation inhibitors and conjugates thereof
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
DK3086814T3 (da) * 2013-12-23 2020-09-14 Bayer Pharma AG Binder-konjugater (adcs) med ksp-inhibitorer
WO2016020791A1 (en) 2014-08-05 2016-02-11 Novartis Ag Ckit antibody drug conjugates
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）
EP3919518A1 (en) 2016-06-15 2021-12-08 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies
IL291308B1 (en) 2016-12-21 2024-03-01 Bayer Pharma AG Drug-antibody conjugates with enzymatically cleavable groups
CN110072556B (zh) 2016-12-21 2023-05-02 拜耳制药股份公司 具有ksp抑制剂的特异性抗体药物缀合物(adc)
EP3806908A1 (de) 2018-06-18 2021-04-21 Bayer Aktiengesellschaft Gegen cxcr5 gerichtete binder-wirkstoff-konjugate mit enzymatisch spaltbaren linkern und verbessertem wirkungsprofil
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

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
RU2263111C2 (ru) * 1998-06-12 2005-10-27 Сосьете Де Консей Де Решерш Э Д`Аппликасьон Сьентифик Сас Имидазольные производные
KR20020062930A (ko) * 1999-10-27 2002-07-31 싸이토키네틱스, 인코포레이티드 퀴나졸리논을 사용하는 방법 및 조성물
US6545004B1 (en) * 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
WO2001083575A1 (en) 2000-05-02 2001-11-08 Advanced Syntech, Llc A Kentucky Limited Liability Corporation A novel solid support template for preparation of highly functionalized heterocycle compounds
ATE360620T1 (de) * 2000-08-01 2007-05-15 Sod Conseils Rech Applic Imidazolderivate
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
US20040186151A1 (en) 2003-02-12 2004-09-23 Mjalli Adnan M.M. Substituted azole derivatives as therapeutic agents
WO2004100873A2 (en) * 2003-05-07 2004-11-25 Cytokinetics, Inc. Compounds, compositions, and methods
WO2004103282A2 (en) * 2003-05-15 2004-12-02 Cytokinetics, Inc. Compounds, compositions and methods
JP2007532626A (ja) 2004-04-14 2007-11-15 ファイザー・インク Ｈｉｖ治療用硫黄連結イミダゾール化合物
US7618981B2 (en) 2004-05-06 2009-11-17 Cytokinetics, Inc. Imidazopyridinyl-benzamide anti-cancer agents
BRPI0510929A (pt) * 2004-06-18 2007-07-17 Chiron Corp 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

Also Published As

Publication number Publication date
ATE526324T1 (de) 2011-10-15
GT200600366A (es) 2007-05-10
CA2618747A1 (en) 2007-02-22
AU2006279991A1 (en) 2007-02-22
US7626040B2 (en) 2009-12-01
PL1912972T3 (pl) 2012-02-29
MY147188A (en) 2012-11-14
EP1912972A1 (en) 2008-04-23
JP2009504664A (ja) 2009-02-05
JP4975745B2 (ja) 2012-07-11
BRPI0614547A2 (pt) 2011-03-29
RU2008108939A (ru) 2009-09-20
AU2006279991B2 (en) 2011-09-29
RU2413721C9 (ru) 2011-05-20
WO2007021794A1 (en) 2007-02-22
CN101253167A (zh) 2008-08-27
AR056025A1 (es) 2007-09-12
KR20080036611A (ko) 2008-04-28
PT1912972E (pt) 2012-01-06
HK1111995A1 (en) 2008-08-22
ES2374449T3 (es) 2012-02-16
US20070037853A1 (en) 2007-02-15
RU2413721C2 (ru) 2011-03-10
EP1912972B1 (en) 2011-09-28
TW200800951A (en) 2008-01-01

Similar Documents

Publication Publication Date Title
PE20070352A1 (es) Compuestos de imidazol sustituidos como inhibidores de ksp
PE20120546A1 (es) Inhibidores del virus de la hepatitis c
PE20110008A1 (es) Triazolopiridazinas como moduladores de quinasa
PE20220569A1 (es) Compuestos de 1-oxo-isoindolin-5-carboxamida sustituida, composiciones de estos y metodos de tratamiento con dichos compuestos
PE20081169A1 (es) Compuestos tipo pirazol y triazol sustituidos como inhibidores de ksp
PE20160115A1 (es) Compuestos derivados de imidazol como inhibidores de protein quinasa
PE20080677A1 (es) Inhibidores de pirrolotriazina cinaza
MX2007007428A (es) Compuestos heterociclicos, antagonistas de ccr2b.
PE20090365A1 (es) Imidazopirazinas como inhibidores de proteina quinasa
PE20121354A1 (es) Inhibidores del virus de la hepatitis c
PE20120635A1 (es) Dihidropirazolonas sustituidas como inhibidores de hif-propil-4-hidroxilasas
PE20142185A1 (es) Pirrolidina-2-carboxamidas sustituidas
PE20110367A1 (es) DERIVADOS DE 4-CIANO-4-FENIL-PIRROLIDIN-2-CARBOXAMIDAS SUSTITUIDAS COMO INHIBIDORES DE LA INTERACCION p53-MDM2
PE20161073A1 (es) Amino-heteroaril-benzamidas como inhibidores de cinasa
PE20120533A1 (es) Inhibidores del virus de la hepatitis c
PE20121282A1 (es) Antagonistas de espiro-oxindol de mdm2
PE20091842A1 (es) Pirrolidinonas como activadores de glucoquinasa
EA201200653A1 (ru) Гетариламинохинолины
ECSP055987A (es) Derivados de heteroarilcarbamoilbenceno
PE20110931A1 (es) Pirrolidin-2-onas como ligandos de hdm2
UY28885A1 (es) 4-fenilamino-quinazolin-6-il-amidas referencia cruzada a solicitud(es) relacionada(s)
PE20071177A1 (es) Derivados de 3,5-piridina como inhibidores de renina
ATE433981T1 (de) Heterocyclische verbindungen
PE20140302A1 (es) Inhibidores del virus de la hepatitis c
PE20081850A1 (es) Derivados ciclizados como inhibidores de la eg-5

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed