PE20061484A1 - Compuestos triciclicos fusionados como inhibidores de la actividad de quinesina de ksp - Google Patents

Compuestos triciclicos fusionados como inhibidores de la actividad de quinesina de ksp

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Publication number
PE20061484A1
PE20061484A1 PE2006000258A PE2006000258A PE20061484A1 PE 20061484 A1 PE20061484 A1 PE 20061484A1 PE 2006000258 A PE2006000258 A PE 2006000258A PE 2006000258 A PE2006000258 A PE 2006000258A PE 20061484 A1 PE20061484 A1 PE 20061484A1
Authority
PE
Peru
Prior art keywords
halo
alkyl
ksp
activity
tetrahydrotien
Prior art date
Application number
PE2006000258A
Other languages
English (en)
Inventor
Jayaram R Tagat
Timothy J Guzi
Marc Labroli
Yushi Xiao
Tao Yu
Hon-Chung Tsui
Stuart W Mccombie
Charles A Lesburg
Jose S Duca
Vincent S Madison
Neng-Yang Shih
Sunil Paliwal
Angela D Kerekes
Cory Poker
Original Assignee
Schering 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
Application filed by Schering Corp filed Critical Schering Corp
Publication of PE20061484A1 publication Critical patent/PE20061484A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/06Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA (I), EN DONDE Y ES UN ANILLO DE 5 A 7 MIEMBROS TAL COMO CICLOALQUILO, CICLOALQUENILO, HETEROCICLILO, ENTRE OTROS, OPCIONALMENTE SUSTITUIDO CON R2 O R6, DONDE R2 ES H, HALO, ALQUILO(C1-C20), CICLOALQUILO(C3-C10), ENTRE OTROS; R6 ES H, ALQUILO(C1-C20), ARILO(C6-C14), ENTRE OTROS; W ES N O C(R12) DONDE R12 ES H, HALO, ALQUILO(C1-C20), ENTRE OTROS, OPCIONALMENTE SUSTITUIDO; X ES N O N-OXIDO; Z ES S, S(=O) O S(=O)2; R1 ES H, ALQUILO(C1-C20), HIDROXI, HALO, CN, ENTRE OTROS; R3 ES H, HALO, ALQUILO(C1-C20), CICLOALQUILO(C3-C10), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 6-TER-BUTIL-5,6,7,8-TETRAHIDROTIEN[2,3-b]QUINOLIN-2-CARBONITRILO, AMIDA DEL ACIDO 6-TER-BUTIL-5,6,7,8-TETRAHIDROTIEN[2,3-b]QUINOLIN-2-CARBOXILICO, AMIDA DEL ACIDO 6-TER-BUTIL-5,6,7,8-TETRAHIDROTIEN[2,3-b]QUINOLIN-2-CARBOTIOICO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN LA ACTIVIDAD DE LA PROTEINA DE QUINESINA DEL HUSO ACROMATICO (KSP) SIENDO UTILES EN EL TRATAMIENTO DE ENFERMEDADES PROLIFERATIVAS TALES COMO CANCER DE PULMON, CANCER DE PANCREAS, HIPERTROFIA CARDIACA, ARTRITIS
PE2006000258A 2005-03-09 2006-03-07 Compuestos triciclicos fusionados como inhibidores de la actividad de quinesina de ksp PE20061484A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US65988805P 2005-03-09 2005-03-09
US71227405P 2005-08-29 2005-08-29

Publications (1)

Publication Number Publication Date
PE20061484A1 true PE20061484A1 (es) 2007-02-05

Family

ID=36660847

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006000258A PE20061484A1 (es) 2005-03-09 2006-03-07 Compuestos triciclicos fusionados como inhibidores de la actividad de quinesina de ksp

Country Status (12)

Country Link
US (1) US20060247320A1 (es)
EP (1) EP1871776A2 (es)
JP (1) JP2008533018A (es)
KR (1) KR20070113267A (es)
AR (1) AR052682A1 (es)
AU (1) AU2006223461A1 (es)
CA (1) CA2599899A1 (es)
IL (1) IL185510A0 (es)
MX (1) MX2007010972A (es)
PE (1) PE20061484A1 (es)
TW (1) TW200700422A (es)
WO (1) WO2006098961A2 (es)

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WO2007011647A2 (en) * 2005-07-15 2007-01-25 Kalypsys, Inc. Inhibitors of mitotic kinesin ksp
WO2007101225A2 (en) * 2006-02-27 2007-09-07 The Board Of Trustees Of The Leland Stanford Junior University Methods to identify inhibitors of the unfolded protein response
CN101687838A (zh) * 2006-12-21 2010-03-31 先灵公司 抑制ksp驱动蛋白活性的吡咯并[3,2-a]吡啶衍生物
WO2008157753A1 (en) * 2007-06-21 2008-12-24 Sma Foundation Methods of treatment for spinal muscular atrophy
CA2702922C (en) 2007-10-19 2018-01-16 Schering Corporation Spiro-condensed 1,3,4-thiadiazole derivatives for inhibiting ksp kinesin activity
US8361959B2 (en) 2008-10-03 2013-01-29 Merck Sharp & Dohme Corp. Spiro-imidazolone derivatives as glucagon receptor antagonists
WO2011002887A1 (en) 2009-07-02 2011-01-06 Schering Corporation FUSED TRICYCLIC COMPOUNDS AS NOVEL mTOR INHIBITORS
EP2473041B1 (en) 2009-09-04 2018-03-07 Merck Sharp & Dohme Corp. Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors
EP2608669B1 (en) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
US20140045847A1 (en) 2011-04-21 2014-02-13 Piramal Enterprises Limited Crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
WO2013016164A1 (en) 2011-07-26 2013-01-31 Merck Sharp & Dohme Corp. FUSED TRICYCLIC COMPOUNDS AS mTOR INHIBITORS
WO2013113716A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
WO2013113788A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
WO2013113720A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
WO2013113776A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
AR089884A1 (es) 2012-02-03 2014-09-24 Basf Se Compuestos fungicidas de pirimidina
EP2809659A1 (en) 2012-02-03 2014-12-10 Basf Se Fungicidal pyrimidine compounds
WO2013113773A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
WO2013135672A1 (en) 2012-03-13 2013-09-19 Basf Se Fungicidal pyrimidine compounds
JP2016506929A (ja) * 2013-01-23 2016-03-07 ザ・ユニバーシティ・オブ・シカゴThe University Of Chicago ヒト銅輸送タンパク質atox1およびccsを阻害するための方法および組成物
US11690847B2 (en) 2016-11-30 2023-07-04 Case Western Reserve University Combinations of 15-PGDH inhibitors with corticosteroids and/or TNF inhibitors and uses thereof
WO2018145080A1 (en) 2017-02-06 2018-08-09 Case Western Reserve University Compositions and methods of modulating short-chain dehydrogenase activity
EP3972590A4 (en) * 2019-05-22 2023-06-14 Merck Sharp & Dohme LLC NATRIURETIC PEPTIDE RECEPTOR A AGONISTS USED TO TREAT CARDIOMETABOLIC DISEASES, KIDNEY DISEASES AND DIABETES

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DE2638828A1 (de) * 1976-08-28 1978-03-09 Thomae Gmbh Dr K Neue thieno-pyridine
EP0127883B1 (en) * 1983-06-02 1989-06-07 American Cyanamid Company (2-Imidazolin-2-yl)thieno and furo(2,3-b) and (3,2-b) pyridines and intermediates for the preparation thereof, and use of said compounds as herbicidal agents.
JP4597519B2 (ja) * 2001-12-06 2010-12-15 メルク・シャープ・エンド・ドーム・コーポレイション 有糸分裂キネシン阻害薬
US7345046B2 (en) * 2003-05-30 2008-03-18 Chiron Corporation Heteroaryl-fused pyrimidinyl compounds as anticancer agents

Also Published As

Publication number Publication date
WO2006098961A2 (en) 2006-09-21
WO2006098961A3 (en) 2007-03-22
KR20070113267A (ko) 2007-11-28
EP1871776A2 (en) 2008-01-02
CA2599899A1 (en) 2006-09-21
TW200700422A (en) 2007-01-01
AR052682A1 (es) 2007-03-28
IL185510A0 (en) 2008-01-06
JP2008533018A (ja) 2008-08-21
US20060247320A1 (en) 2006-11-02
MX2007010972A (es) 2007-09-19
AU2006223461A1 (en) 2006-09-21

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