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PE20081850A1 - Derivados ciclizados como inhibidores de la eg-5 - Google Patents

Derivados ciclizados como inhibidores de la eg-5

Info

Publication number
PE20081850A1
PE20081850A1 PE2008000091A PE2008000091A PE20081850A1 PE 20081850 A1 PE20081850 A1 PE 20081850A1 PE 2008000091 A PE2008000091 A PE 2008000091A PE 2008000091 A PE2008000091 A PE 2008000091A PE 20081850 A1 PE20081850 A1 PE 20081850A1
Authority
PE
Peru
Prior art keywords
independently
rent
inhibitors
ona
dimethylpropyl
Prior art date
Application number
PE2008000091A
Other languages
English (en)
Inventor
Rustum Boyce
Eric Martin
Weibo Wang
Hong Yang
Paul A Barsanti
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 PE20081850A1 publication Critical patent/PE20081850A1/es

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Emulsifying, Dispersing, Foam-Producing Or Wetting Agents (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE IMIDAZOL DE FORMULA (I), EN DONDE R1 ES ALQUILO OPCIONALMENTE SUSTITUIDO; R2 ES H, ALQUILO OPCIONALMENTE SUSTITUIDO; L ES -O-, -OCH2-, -CH2OCH2-, -C(O)NR7, -CH2O-, ENTRE OTROS; R3 Y R4 SON INDEPENDIENTEMENTE HALO, ALQUILO OPCIONALMENTE SUSTITUIDO; R5 Y R6 SON INDEPENDIENTEMENTE CIANO, ALQUILO OPCIONALMENTE SUSTITUIDO, ALCOXI, ENTRE OTROS; m Y n SON INDEPENDIENTEMENTE DE 0 A 3; p ES 0 O 1. SON SELECCIONADOS: (S)-5-(AMINOMETIL)-3-((R)-1-(1-BENCIL-4-(2,5-DIFLUOROFENIL)-1H-IMIDAZOL-2-IL)-2,2-DIMETILPROPIL)OXAZOLIDIN-2-ONA, (5S)-5-(AMINOMEIL)-3-[(1R)-1-(1-BENCIL-4-FENIL-1H-IMIDAZOL-2-IL)-2,2-DIMETILPROPIL]-1,3-OXAZIN-2-ONA, ENTRE OTROS. TAMBIEN SE RERIERE A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO DE PREPARACION. ESTOS COMPUESTOS SON INHIBIDORES DE PROTEINAS DE KINESINAS (KSP) EN ESPECIAL DE EG-5, POR LO QUE SON UTILES EN EL TRATAMIENTO DE UNA ENFERMEDAD DE PROLIFERACION CELULAR TAL COMO EL CANCER
PE2008000091A 2007-01-05 2008-01-04 Derivados ciclizados como inhibidores de la eg-5 PE20081850A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US88374007P 2007-01-05 2007-01-05

Publications (1)

Publication Number Publication Date
PE20081850A1 true PE20081850A1 (es) 2009-02-05

Family

ID=39577804

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000091A PE20081850A1 (es) 2007-01-05 2008-01-04 Derivados ciclizados como inhibidores de la eg-5

Country Status (30)

Country Link
US (3) US7820646B2 (es)
EP (1) EP2106399A2 (es)
JP (1) JP2010515687A (es)
KR (1) KR20090097210A (es)
CN (1) CN101622247A (es)
AR (1) AR064760A1 (es)
AU (1) AU2008205169B2 (es)
BR (1) BRPI0806264A2 (es)
CA (1) CA2674318A1 (es)
CL (1) CL2008000029A1 (es)
CO (1) CO6561828A2 (es)
CR (1) CR10879A (es)
DO (1) DOP2009000169A (es)
EA (1) EA200900924A1 (es)
EC (1) ECSP099485A (es)
GE (1) GEP20125415B (es)
GT (1) GT200900192A (es)
HN (1) HN2009001262A (es)
MA (1) MA31080B1 (es)
MX (1) MX2009007260A (es)
NI (1) NI200900134A (es)
NZ (1) NZ577727A (es)
PE (1) PE20081850A1 (es)
SM (1) SMP200900065B (es)
SV (1) SV2009003325A (es)
TN (1) TN2009000287A1 (es)
TW (1) TW200836722A (es)
UA (1) UA97821C2 (es)
WO (1) WO2008086122A2 (es)
ZA (1) ZA200904175B (es)

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US8252832B2 (en) 2007-12-14 2012-08-28 Novartis Ag Kinesin inhibitors as cancer therapeutics
MX2012011910A (es) 2010-04-15 2012-11-29 Novartis Ag Compuestos de triazol como inhibidores de ksp.
WO2011128388A2 (en) * 2010-04-15 2011-10-20 Novartis Ag Oxazole and thiazole compounds as ksp inhibitors
EP2390247A1 (en) * 2010-05-26 2011-11-30 Netherlands Organisation for Scientific Research (Advanced Chemical Technologies for Sustainability) Preparation of caprolactone, caprolactam, 2,5-tetrahydrofuran dimethanol, 1,6-hexanediol or 1,2,6-hexanetriol from 5-hydroxymethyl-2-furfuraldehyde
GB201113538D0 (en) 2011-08-04 2011-09-21 Karobio Ab Novel estrogen receptor ligands
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
KR102329024B1 (ko) * 2013-12-23 2021-11-19 바이엘 파마 악티엔게젤샤프트 키네신 스핀들 단백질(ksp)과의 항체 약물 접합체 (adcs)
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）
CN105330657B (zh) * 2015-12-08 2019-05-21 华润双鹤药业股份有限公司 5-氯-2-[5-(r)-甲基-1,4-二氮杂环庚烷-1-]苯并恶唑的制备方法
CN105367506B (zh) * 2015-12-08 2021-02-05 华润双鹤药业股份有限公司 手性高哌嗪环的制备方法
EP3919518A1 (en) 2016-06-15 2021-12-08 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies
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)
IL291308B2 (en) 2016-12-21 2024-07-01 Bayer Pharma AG Antibody drug conjugates (adcs) having enzymatically cleavable groups
EP3806908A1 (de) 2018-06-18 2021-04-21 Bayer Aktiengesellschaft Gegen cxcr5 gerichtete binder-wirkstoff-konjugate mit enzymatisch spaltbaren linkern und verbessertem wirkungsprofil
CN119859151A (zh) * 2023-10-19 2025-04-22 北京振东光明药物研究院有限公司 从白土苓中分离得到的生物碱类化合物及其制备方法和应用

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Also Published As

Publication number Publication date
HN2009001262A (es) 2012-01-09
JP2010515687A (ja) 2010-05-13
EP2106399A2 (en) 2009-10-07
US20120189623A1 (en) 2012-07-26
CA2674318A1 (en) 2008-07-17
WO2008086122A2 (en) 2008-07-17
KR20090097210A (ko) 2009-09-15
CR10879A (es) 2009-08-05
DOP2009000169A (es) 2009-08-31
ZA200904175B (en) 2010-04-28
CO6561828A2 (es) 2012-11-15
AU2008205169B2 (en) 2012-02-02
GT200900192A (es) 2010-06-24
US20080207589A1 (en) 2008-08-28
TW200836722A (en) 2008-09-16
MX2009007260A (es) 2009-07-10
TN2009000287A1 (en) 2010-12-31
MA31080B1 (fr) 2010-01-04
SMAP200900065A (it) 2009-09-07
SMP200900065B (it) 2010-09-10
ECSP099485A (es) 2009-08-28
CN101622247A (zh) 2010-01-06
AU2008205169A1 (en) 2008-07-17
EA200900924A1 (ru) 2009-12-30
WO2008086122A3 (en) 2008-10-16
US20110003791A1 (en) 2011-01-06
AR064760A1 (es) 2009-04-22
SV2009003325A (es) 2011-08-09
US7820646B2 (en) 2010-10-26
NI200900134A (es) 2010-07-05
GEP20125415B (en) 2012-03-12
UA97821C2 (en) 2012-03-26
CL2008000029A1 (es) 2008-04-04
NZ577727A (en) 2012-03-30
BRPI0806264A2 (pt) 2011-08-30

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