WO2005024755A3 - Medicaments destines au traitement de troubles neurodegeneratifs ou de diabetes - Google Patents

Medicaments destines au traitement de troubles neurodegeneratifs ou de diabetes Download PDF

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Publication number
WO2005024755A3
WO2005024755A3 PCT/US2004/011922 US2004011922W WO2005024755A3 WO 2005024755 A3 WO2005024755 A3 WO 2005024755A3 US 2004011922 W US2004011922 W US 2004011922W WO 2005024755 A3 WO2005024755 A3 WO 2005024755A3
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WIPO (PCT)
Prior art keywords
diabetes
kinase
treatment
compounds
protein
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PCT/US2004/011922
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English (en)
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WO2005024755A2 (fr
Inventor
Daniel L Flynn
Peter A Petillo
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Deciphera Pharmaceuticals Llc
Daniel L Flynn
Peter A Petillo
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
Priority claimed from US10/746,460 external-priority patent/US7144911B2/en
Priority claimed from US10/746,607 external-priority patent/US7279576B2/en
Priority claimed from US10/746,545 external-priority patent/US20040171075A1/en
Application filed by Deciphera Pharmaceuticals Llc, Daniel L Flynn, Peter A Petillo filed Critical Deciphera Pharmaceuticals Llc
Publication of WO2005024755A2 publication Critical patent/WO2005024755A2/fr
Publication of WO2005024755A3 publication Critical patent/WO2005024755A3/fr

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/44—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
    • C07D207/444—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
    • C07D207/448—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide
    • C07D207/452—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide with hydrocarbon radicals, substituted by hetero atoms, directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/44—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
    • C07D207/444—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
    • C07D207/456—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • 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
    • 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne des nouveaux composés et des méthodes permettant de traiter des formes humaines de maladies neurodégénératives, des diabètes, des états mentaux, des maladies inflammatoires, des accidents vasculaires cérébraux et des cancers. Les composés décrits dans cette invention sont des petits inhibiteurs moléculaires de protéines kinase-3 de glycogène synthétase. Cette invention concerne également des produits d'addition composés constitués de petits inhibiteurs moléculaires et de protéines kinase-3 GSK ; ces composés sont liés aux protéines kinases dans la région d'une poche de commande d'interruption de protéines afin de modifier la conformation et/ou l'activité protéique des kinases.
PCT/US2004/011922 2002-12-31 2004-04-15 Medicaments destines au traitement de troubles neurodegeneratifs ou de diabetes WO2005024755A2 (fr)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
US43730402P 2002-12-31 2002-12-31
US46380403P 2003-04-18 2003-04-18
US60/463,804 2003-04-18
US10/746,607 2003-12-24
US10/746,460 US7144911B2 (en) 2002-12-31 2003-12-24 Anti-inflammatory medicaments
US10/746,460 2003-12-24
US10/746,607 US7279576B2 (en) 2002-12-31 2003-12-24 Anti-cancer medicaments
US10/746,545 US20040171075A1 (en) 2002-12-31 2003-12-24 Modulation of protein functionalities
US10/746,545 2003-12-24
US10/437,304 2003-12-31

Publications (2)

Publication Number Publication Date
WO2005024755A2 WO2005024755A2 (fr) 2005-03-17
WO2005024755A3 true WO2005024755A3 (fr) 2005-04-21

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ID=34317765

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PCT/US2004/011922 WO2005024755A2 (fr) 2002-12-31 2004-04-15 Medicaments destines au traitement de troubles neurodegeneratifs ou de diabetes

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Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006045581A1 (fr) * 2004-10-21 2006-05-04 Neuropharma, S.A. Utilisation de 1, 2, 4-thiadiazolidine-3, 5-diones en tant qu'activateurs de ppar
CN101720323A (zh) * 2007-04-11 2010-06-02 三井有限公司 具有抗癌活性的化合物
CN105130967B (zh) 2011-05-13 2018-04-17 阵列生物制药公司 作为trka激酶抑制剂的吡咯烷基脲和吡咯烷基硫脲化合物
US8461179B1 (en) 2012-06-07 2013-06-11 Deciphera Pharmaceuticals, Llc Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
US9546156B2 (en) 2012-11-13 2017-01-17 Array Biopharma Inc. N-bicyclic aryl,N'-pyrazolyl urea, thiourea, guanidine cyanoguanidine compounds as TrkA kinase inhibitors
US9828360B2 (en) 2012-11-13 2017-11-28 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
RS55593B1 (sr) 2012-11-13 2017-06-30 Array Biopharma Inc Jedinjenja biciklične uree, tiouree, guanidina i cijanoguanidina korisna za lečenje bola
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078417A1 (fr) 2012-11-13 2014-05-22 Array Biopharma Inc. Composés de pyrazolylurée, d'urée, de thiourée, de guanidine et de cyanoguianidine en tant qu'inhibiteurs de la trka kinase
WO2014078325A1 (fr) 2012-11-13 2014-05-22 Array Biopharma Inc. Composés de n-aryle monocycliques, n'-pyrazolyl-urée, thiourée, guanidine et cyanoguanidine utiles comme inhibiteurs de trka kinase
WO2014078331A1 (fr) 2012-11-13 2014-05-22 Array Biopharma Inc. Composés de n-(arylalkyle)-n'-pyrazolyle-urée, de thiourée, de guanidine et de cyanoguanidine en tant qu'inhibiteurs de la kinase trka
US9822118B2 (en) 2012-11-13 2017-11-21 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
MX365733B (es) 2012-11-13 2019-06-12 Array Biopharma Inc Compuestos de n-pirrolidinil, n' -pirazolil-urea, tiourea, guanidina y cianoguanidina como inhibidores de trka cinasa.
US9790178B2 (en) 2012-11-13 2017-10-17 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
CR20160583A (es) 2014-05-15 2017-02-23 Array Biopharma Inc 1-((3s,4r)-4-(3-fluorofenil)-1-(2-metoxietil)pirrolidin-3-il)-3-(4-metil-3-(2-metilpirimidin-5-il)-1-fenil-1h-pirazol-5-il)urea como inhibidor de trka cinasa
KR20200115607A (ko) 2018-01-31 2020-10-07 데시페라 파마슈티칼스, 엘엘씨. 위장관 기질 종양의 치료를 위한 병용 요법
KR20220045189A (ko) 2019-08-12 2022-04-12 데시페라 파마슈티칼스, 엘엘씨. 위장관 기질 종양을 치료하는 방법
WO2021030405A1 (fr) 2019-08-12 2021-02-18 Deciphera Pharmaceuticals, Llc Ripretinib pour le traitement de tumeurs stromales gastro-intestinales
IL293864A (en) 2019-12-30 2022-08-01 Deciphera Pharmaceuticals Llc Preparations of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3- phenylurea
KR20220123057A (ko) 2019-12-30 2022-09-05 데시페라 파마슈티칼스, 엘엘씨. 비정질 키나아제 억제제 제형 및 이의 사용 방법
WO2021163572A1 (fr) * 2020-02-14 2021-08-19 Bowroju Suresh Kuarm Nouveaux analogues de tdzd en tant qu'agents qui retardent, préviennent ou inversent des maladies associées à l'âge; et en tant qu'agents anticancéreux et antileucémiques
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3335147A (en) * 1965-04-29 1967-08-08 Us Vitamin Pharm Corp Anilino-pyridinium-maleimides
US4474598A (en) * 1983-06-27 1984-10-02 Shell Oil Company Oxazolyl-substituted thiadiazolidinediones
WO2000021927A2 (fr) * 1998-10-08 2000-04-20 Smithkline Beecham Plc Procede et composes
ES2166328A1 (es) * 2000-05-11 2002-04-01 Consejo Superior Investigacion Inhibidores heterociclicos del enzima gsk 3 utiles en el tratamiento de procesos neurodegenerativos e hiperproliferativos

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3335147A (en) * 1965-04-29 1967-08-08 Us Vitamin Pharm Corp Anilino-pyridinium-maleimides
US4474598A (en) * 1983-06-27 1984-10-02 Shell Oil Company Oxazolyl-substituted thiadiazolidinediones
WO2000021927A2 (fr) * 1998-10-08 2000-04-20 Smithkline Beecham Plc Procede et composes
ES2166328A1 (es) * 2000-05-11 2002-04-01 Consejo Superior Investigacion Inhibidores heterociclicos del enzima gsk 3 utiles en el tratamiento de procesos neurodegenerativos e hiperproliferativos

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
BISHOP ET AL: "A chemical switch for inhibitor-sensitive alleles of any protein kinase", NATURE, vol. 407, 21 September 2000 (2000-09-21), pages 395 - 401, XP002985907 *
JOHNSON ET AL: "Active and Inactive Protein Kinases: Structural Basis for Regulation", CELL, vol. 85, 19 April 1996 (1996-04-19), pages 149 - 158, XP002985906 *
MARTINEZ ET AL: "First Non-ATP Competitive Glycogen Synthase Kinase 3beta (GSK-3beta) Inhinitors: Thiadiazolidinones (TDZD) as Potential Drugs for the treatment of Alzheimer s Disease", J MED CHEM, vol. 45, 13 February 2002 (2002-02-13), pages 1292 - 1299, XP002292084 *
YUKI ET AL: "Studies on Antiviral Agents. II. Synthesis and biological Activity of Maleimide Derivatives", CHEM PHARM BULL (TOKYO), vol. 15, no. 8, 1967, pages 1101 - 1106, XP002985950 *

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