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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

Info

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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/4365—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic 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
    • C07D495/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic 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
    • C07D495/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems

Landscapes

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

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007011647A2 (en) * 2005-07-15 2007-01-25 Kalypsys, Inc. Inhibitors of mitotic kinesin ksp
CA2638734A1 (en) * 2006-02-27 2007-09-07 The Board Of Trustees Of The Leland Stanford Junior University Inhibitors of the unfolded protein response and methods for their use
WO2008079293A1 (en) * 2006-12-21 2008-07-03 Schering Corporation Pyrrolo [3, 2-a] pyridine derivatives for inhibiting ksp kinesin activity
WO2008157753A1 (en) * 2007-06-21 2008-12-24 Sma Foundation Methods of treatment for spinal muscular atrophy
EP2220061B1 (en) 2007-10-19 2016-02-17 Merck Sharp & Dohme Corp. Spiro-condensed 1, 3, 4-thiadiazole derivatives for inhibiting ksp kinesin activity
EP2350020B1 (en) 2008-10-03 2014-08-13 Merck Sharp & Dohme Corp. Spiro-imidazolone derivatives as glucagon receptor antagonists
US8609675B2 (en) 2009-07-02 2013-12-17 Merck Sharp & Dohme Corp. 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
IN2013MN02170A (es) 2011-04-21 2015-06-12 Piramal Entpr Ltd
US8901142B2 (en) 2011-07-26 2014-12-02 Merck Sharp & Dohme Corp. Fused tricyclic compounds as mTOR inhibitors
WO2013113788A1 (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
WO2013113773A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
IN2014DN07220A (es) 2012-02-03 2015-04-24 Basf Se
CN104220428A (zh) 2012-02-03 2014-12-17 巴斯夫欧洲公司 杀真菌嘧啶化合物
WO2013113716A1 (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
WO2013135672A1 (en) 2012-03-13 2013-09-19 Basf Se Fungicidal pyrimidine compounds
EP2948438A4 (en) * 2013-01-23 2016-10-05 Univ Chicago METHOD AND COMPOSITIONS FOR INHIBITING THE HUMAN COPPER TRAFFICKING PROTEIN ATOX1 AND CCS
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
NZ796735A (en) 2017-02-06 2025-12-19 Univ Case Western Reserve Compositions and methods of modulating short-chain dehydrogenase activity
CN120463720A (zh) 2018-11-21 2025-08-12 卡斯西部储备大学 调节短链脱氢酶活性的组合物和方法
US12440496B2 (en) 2019-05-22 2025-10-14 Merck Sharp & Dohme Llc Natriuretic peptide receptor a agonists useful for the treatment of cardiometabolic diseases, kidney disease and diabetes

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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.
DE60222302T2 (de) * 2001-12-06 2008-05-29 Merck & Co., Inc. Inhibitoren von mitotischem kinesin
US7345046B2 (en) * 2003-05-30 2008-03-18 Chiron Corporation Heteroaryl-fused pyrimidinyl compounds as anticancer agents

Also Published As

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

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