WO2003070727A1 - Thiazolyl urea compounds for the treatment of cancer - Google Patents

Thiazolyl urea compounds for the treatment of cancer Download PDF

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Publication number
WO2003070727A1
WO2003070727A1 PCT/US2003/004537 US0304537W WO03070727A1 WO 2003070727 A1 WO2003070727 A1 WO 2003070727A1 US 0304537 W US0304537 W US 0304537W WO 03070727 A1 WO03070727 A1 WO 03070727A1
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WIPO (PCT)
Prior art keywords
pyridin
urea
thiazol
optionally substituted
piperidin
Prior art date
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Ceased
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PCT/US2003/004537
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English (en)
French (fr)
Inventor
Vincent Santora
Benny C. Askew
Frenel F. De Morin
Andrew Hague
Ellen Laber
Aiwen Li
Gang Liu
Patricia Lopez
Rana Nomak
Christopher Tegley
Kevin Yang
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Amgen Inc
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Amgen Inc
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Publication date
Application filed by Amgen Inc filed Critical Amgen Inc
Priority to JP2003569634A priority Critical patent/JP2006509715A/ja
Priority to AU2003215231A priority patent/AU2003215231A1/en
Priority to MXPA04007970A priority patent/MXPA04007970A/es
Priority to CA002476411A priority patent/CA2476411A1/en
Priority to EP03711046A priority patent/EP1483263A1/en
Publication of WO2003070727A1 publication Critical patent/WO2003070727A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • C07D233/56—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 only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • 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
    • C07D417/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/06—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing isoquinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

Definitions

  • Cell proliferation is the rapid reproduction of cells, such as by cell division.
  • the cell cycle which controls cell proliferation, is itself controlled by a family of serine-threonine kinases called cyclin dependent kinases (CDKs) .
  • CDKs cyclin dependent kinases
  • the regulation of CDK activation is complex, and requires the association of the CDK with a member of the cyclin family of regulatory subunits .
  • a further level of regulation occurs through both activating and inactivating phosphorylations of the CDK subunit.
  • the coordinate activation and inactivation of different cyclin/CDK complexes is necessary for normal progression through the cell cycle. Both the critical Gl-S and G2-M transitions are controlled by the activation of different cyclin/CDK activities.
  • C 2 -haloalkyl hydroxy, C ⁇ -C-alkylthio, cyano, C ⁇ -C 2 - haloalkyloxy, aminosulfonyl, (6-membered N- containing heterocyclyl) sulfonyl, C ⁇ -C 2 - haloalkylcarbonylaminosulfonyl, and (optionally substituted phenyl) aminosulfonyl, and 6-membered nitrogen-containing heterocyclyl substituted with one or more substituents independently selected from pyridyl, phenyl, C 1 -C4 alkyl, C ⁇ -C 2 haloalkyl, C ⁇ -C 2 alkoxy, halo, piperidinyl, morpholinyl, C ⁇ -C 2 alkylpiperazinyl, Ci- C 3 alkylaminothiocarbonyl , N,N-di-C ⁇ -C-alkylamino- C ⁇ -C 4 -al
  • hydroxyalkylamino denotes amino groups which have been substituted with a hydroxyalkyl radical, as defined above.
  • aryla ino denotes amino groups which have been substituted with one or two aryl radicals, such as N- phenylamino.
  • arylamino radicals may be further substituted on the aryl ring portion of the radical.
  • the present invention preferably includes compounds that selectively inhibit GSK, CDK2 and/or CDK5.
  • the present invention also comprises the use of a compound of the invention, or pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment either acutely or chronically of a cell proliferation or apoptosis mediated disease state, including those described previously.
  • the compounds of the present invention are also useful in the manufacture of an anti- cancer medicament.
  • the compounds of the present invention are also useful in the manufacture of a medicament to attenuate or prevent disorders through inhibition of CDKs and other kinases.
  • the compounds of the present invention are also useful in the manufacture of a medicament to treat neurological disorders.
  • antineoplastic agents available in commercial use, in clinical evaluation and in pre-clinical development, which would be selected for treatment of neoplasia by combination drug chemotherapy.
  • Such antineoplastic agents fall into several major categories, namely, antibiotic-type agents, alkylating agents, antimetabolite agents, hormonal agents, immunological agents, interferon-type agents and a category of miscellaneous agents.
  • Examples of appropriate acids are tartaric, diacetyltartaric, dibenzoyltartaric, ditoluoyltartaric, and camphorsulfonic acid and then separation of the mixture of diastereoisomers by crystallization followed by liberation of the optically active bases from these salts.
  • a different process for separation of optical isomers involves the use of a chiral chromatography column optimally chosen to maximize the separation of the enantiomers .
  • Still another available method involves synthesis of covalent diastereoisomeric molecules by reacting compounds of the invention with an optically pure acid in an activated form or an optically pure isocyanate.
  • the 4-hydroxy piperidine 80 is hydrated, such as with strong acid, preferably H 2 S0 , at a temperature above RT, preferably above 75°C, more preferably at about 100°C, to form the tetrahydro-bipyridine 81.
  • the 2-bromo-pyridine 81 is aminated, such as with NH 4 OH, in the presence of Cu powder at a temperature above RT, preferably above about 75°C, more preferably at about 100°C, to form the amino- pyridine 82.
  • the reaction is run in a sealed tube.
  • Oxalyl chloride (2.1 mL, 3.81 mmol) in dry CH 2 Cl 2 was cooled to -70°C followed by adding DMSO (0.6 mL, 8.39 mmol) dropwise. After stirred for 5 min under -60°C, l-(6-bromo- pyridin-2-yl) -ethanol (770 mg, 3.81 mmol) in dry CH 2 C1 2 (10 mL) was added dropwise. After stirred for 30 min, TEA (2.7 mL, 19.83 mmol) was added and the resulting mixture was warmed to RT and stirred for 1 h. The reaction mixture was quenched with H 2 0.

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  • Chemical & Material Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
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  • Ophthalmology & Optometry (AREA)
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  • Plural Heterocyclic Compounds (AREA)
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PCT/US2003/004537 2002-02-15 2003-02-13 Thiazolyl urea compounds for the treatment of cancer Ceased WO2003070727A1 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
JP2003569634A JP2006509715A (ja) 2002-02-15 2003-02-13 癌の治療用チアゾイル尿素化合物
AU2003215231A AU2003215231A1 (en) 2002-02-15 2003-02-13 Thiazolyl urea compounds for the treatment of cancer
MXPA04007970A MXPA04007970A (es) 2002-02-15 2003-02-13 Compuestos de tiazolil urea para el tratamiento de cancer.
CA002476411A CA2476411A1 (en) 2002-02-15 2003-02-13 Thiazolyl urea compounds for the treatment of cancer
EP03711046A EP1483263A1 (en) 2002-02-15 2003-02-13 Thiazolyl urea compounds for the treatment of cancer

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10/077,124 2002-02-15
US10/077,124 US6645990B2 (en) 2000-08-15 2002-02-15 Thiazolyl urea compounds and methods of uses

Publications (1)

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WO2003070727A1 true WO2003070727A1 (en) 2003-08-28

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US (3) US6645990B2 (https=)
EP (1) EP1483263A1 (https=)
JP (1) JP2006509715A (https=)
AU (1) AU2003215231A1 (https=)
CA (1) CA2476411A1 (https=)
MX (1) MXPA04007970A (https=)
PL (1) PL372211A1 (https=)
WO (1) WO2003070727A1 (https=)

Cited By (20)

* Cited by examiner, † Cited by third party
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WO2004002481A1 (en) * 2002-06-27 2004-01-08 Novo Nordisk A/S Aryl carbonyl derivatives as therapeutic agents
WO2006070192A1 (en) 2004-12-30 2006-07-06 Astex Therapeutics Limited Thiazole and isothiazole derivatives that modulate the acivity of cdk, gsk and aurora kynases
WO2007106525A1 (en) * 2006-03-13 2007-09-20 The Regents Of The University Of California Piperidinyl, indolyl, pirinidyl, morpholinyl and benzimidazolyl urea derivatives as inhibitors of soluble epoxide hydrolase for the treatment of hypertension, inflammations and other diseases
US7662910B2 (en) 2004-10-20 2010-02-16 The Regents Of The University Of California Inhibitors for the soluble epoxide hydrolase
AU2005264988B2 (en) * 2004-06-17 2011-09-22 Cytokinetics, Inc. Substituted urea derivatives for treating cardiac diseases
WO2013010946A2 (en) 2011-07-15 2013-01-24 Basf Se Pesticidal methods using substituted 3-pyridyl thiazole compounds and derivatives for combating animal pests i
US8445495B2 (en) 2005-12-15 2013-05-21 Cytokinetics, Inc. Certain Chemical entities, compositions and methods
US8455652B2 (en) 2003-04-03 2013-06-04 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Inhibitors for the soluble epoxide hydrolase
US8513302B2 (en) 2003-04-03 2013-08-20 The Regents Of The University Of California Reducing nephropathy with inhibitors of soluble epoxide hydrolase and epoxyeicosanoids
US8835506B2 (en) 2008-06-05 2014-09-16 Stc.Unm Methods and related compositions for the treatment of cancer
USRE45183E1 (en) 2004-01-06 2014-10-07 Novo Nordisk A/S Heteroaryl-ureas and their use as glucokinase activators
WO2015071230A1 (en) * 2013-11-15 2015-05-21 Bayer Cropscience Ag Catalytic hydrogenation of nitriles
US9296693B2 (en) 2010-01-29 2016-03-29 The Regents Of The University Of California Acyl piperidine inhibitors of soluble epoxide hydrolase
US9771379B2 (en) 2015-09-24 2017-09-26 Pfizer Inc. N-(2-(2-amino-6-substituted-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]OXAZIN-8a(8H)-yl)-thiazol-4-yl) amides
WO2020030924A1 (en) * 2018-08-10 2020-02-13 Artios Pharma Limited Thiazoleureas as anticancer agents
WO2021204626A1 (en) 2020-04-06 2021-10-14 Almirall, S.A. Aryl and heteroaryl-carboxamide substituted heteroaryl compounds as tyk2 inhibitors
WO2022117064A1 (en) * 2020-12-04 2022-06-09 Eubulus Biotherapeutics Inc. Heteroaryl-acetylenes, pharmaceutical compositions thereof, and their therapeutic applications
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