US20010027202A1 - Omega-carboxyaryl substituted disphenyl ureas as raf kinase inhibitors - Google Patents

Omega-carboxyaryl substituted disphenyl ureas as raf kinase inhibitors Download PDF

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US20010027202A1
US20010027202A1 US09/773,658 US77365801A US2001027202A1 US 20010027202 A1 US20010027202 A1 US 20010027202A1 US 77365801 A US77365801 A US 77365801A US 2001027202 A1 US2001027202 A1 US 2001027202A1
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Prior art keywords
substituted
phenyl
heteroatoms selected
acid
halogen
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US09/773,658
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Inventor
Bernd Riedl
Jaques Dumas
Uday Khire
Timothy Lowinger
William Scott
Roger Smith
Jill Wood
Mary-Katherine Monahan
Reina Natero
Joel Renick
Robert Sibley
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Bayer Healthcare LLC
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Application filed by Individual filed Critical Individual
Priority to US09/773,658 priority Critical patent/US20010027202A1/en
Assigned to BAYER CORPORATION reassignment BAYER CORPORATION ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: DUMAS, JACQUES, MONAHAN, MARY-KATHERINE, NATERO, REINA, RENICK, JOEL, SCOTT, WILLIAM J., SIBLEY, ROBERT N., SMITH, ROGER A., KHIRE, UDAY, RIEDL, BERND, Wood, Jill E., LOWINGER, TIMOTHY B.
Publication of US20010027202A1 publication Critical patent/US20010027202A1/en
Assigned to BAYER HEALTHCARE LLC reassignment BAYER HEALTHCARE LLC ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: BAYER PHARMACEUTICALS CORPORATION
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/06—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
    • C07D295/073—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
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Definitions

  • the compounds can be produced from known compounds (or from starting materials which, in turn, can be produced from known compounds), e.g., through the general preparative methods shown below.
  • the activity of a given compound to inhibit raf kinase can be routinely assayed, e.g., according to procedures disclosed below.
  • the following examples are for illustrative purposes only and are not intended, nor should they be construed to limit the invention in any way.
  • C1a General Method for the Synthesis of Ureas by Reaction of an Isocyanate with an Aniline. Synthesis of N-(4-Chloro-3-(trifluoromethyl)phenyl)-N′-(4-(2-(N-methylcarbamoyl)-4-pyridyloxy)phenyl) Urea
  • Entry 21 4-(4-Methylthiophenoxy)-1-nitrobenzene was oxidized according to Method A19, Step 1 to give 4-(4-methylsulfonylphenoxy)-1-nitrobenzene. The nitrobenzene was reduced according to Method A19, Step 2 to give 4-(4-methylsulfonylphenoxy)-1-aniline. According to Method C1a, 5-(trifluoromethyl)-2-methoxyphenyl isocyanate was reacted with 4-(4-methylsulfonylphenoxy)-1-aniline to afford the urea.
  • N-(5-(Trifluoromethyl)-2-methoxyphenyl)-N′-(4-(3-(5-methoxycarbonylpyridyl)oxy)phenyl) urea was saponified according to Method D4, Step 1, and the corresponding acid was coupled with 4-(2-aminoethyl)morpholine to afford the amide according to Method D4, Step 2.
  • Entry 39 4-(3-Carboxyphenoxy)aniline was synthesized according to Method A11. 5-(Trifluoromethyl)-2-methoxyaniline was converted into 5-(trifluoromethyl)-2-methoxyphenyl isocyanate according to Method B1. 4-(3-Carboxyphenoxy)aniline was reacted with 5-(trifluoromethyl)-2-methoxyphenyl isocyanate according to Method C1f to afford N-(5-(trifluoromethyl)-2-methoxyphenyl)-N′-(3-carboxyphenyl) urea, which was coupled with 4-morpholinoaniline according to Method D1c.
  • Entry 74 4-Chloropyridine-2-carbonyl chloride HCl salt was reacted with 2-hydroxyethylamine according to Method A2, Step 3b to form 4-chloro-N-(2-triisopropylsilyloxy)ethylpyridine-2-carboxamide.
  • 4-Chloro-N-(2-triisopropylsilyloxy)ethylpyridine-2-carboxamide was reacted with triisopropylsilyl chloride, followed by 4-aminophenol according to Method A17 to form 4-(4-(2-(N-(2-triisopropylsilyloxy)ethylcarbamoyl)pyridyloxyaniline.
  • Entry 84 4-Chloropyridine-2-carbonyl chloride HCl salt was reacted with 2-hydroxyethylamine according to Method A2, Step 3b to form 4-chloro-N-(2-triisopropylsilyloxy)ethylpyridine-2-carboxamide.
  • 4-Chloro-N-(2-triisopropylsilyloxy)ethylpyridine-2-carboxamide was reacted with triisopropylsilyl chloride, followed by 4-aminophenol according to Method A17 to form 4-(4-(2-(N-(2-triisopropylsilyloxy)ethylcarbamoyl)pyridyloxyaniline.

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US09/773,658 1999-01-13 2001-02-02 Omega-carboxyaryl substituted disphenyl ureas as raf kinase inhibitors Abandoned US20010027202A1 (en)

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US09/773,658 US20010027202A1 (en) 1999-01-13 2001-02-02 Omega-carboxyaryl substituted disphenyl ureas as raf kinase inhibitors

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US09/773,658 Abandoned US20010027202A1 (en) 1999-01-13 2001-02-02 Omega-carboxyaryl substituted disphenyl ureas as raf kinase inhibitors
US09/773,604 Abandoned US20010034447A1 (en) 1999-01-13 2001-02-02 Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US09/773,672 Abandoned US20010016659A1 (en) 1999-01-13 2001-02-02 Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US09/773,659 Abandoned US20010011135A1 (en) 1999-01-13 2001-02-02 Omega-carboxyaryl subsituted diphenyl ureas as raf kinase inhibitors
US09/773,675 Abandoned US20010011136A1 (en) 1999-01-13 2001-02-02 omega-carboxyyaryl substituted diphenyl ureas as raf kinase inhibitors
US09/948,915 Abandoned US20020042517A1 (en) 1999-01-13 2001-09-10 Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US10/071,248 Expired - Fee Related US7528255B2 (en) 1999-01-13 2002-02-11 Hydroxy, ω-carboxyaryl substituted diphenyl ureas and dirivatives thereof as raf kinase inhibitors
US11/845,595 Abandoned US20080032979A1 (en) 1999-01-13 2007-08-27 Omega-Carboxyaryl Substituted Diphenyl Ureas As Raf Kinease Inhibitors

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US09/773,672 Abandoned US20010016659A1 (en) 1999-01-13 2001-02-02 Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US09/773,659 Abandoned US20010011135A1 (en) 1999-01-13 2001-02-02 Omega-carboxyaryl subsituted diphenyl ureas as raf kinase inhibitors
US09/773,675 Abandoned US20010011136A1 (en) 1999-01-13 2001-02-02 omega-carboxyyaryl substituted diphenyl ureas as raf kinase inhibitors
US09/948,915 Abandoned US20020042517A1 (en) 1999-01-13 2001-09-10 Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US10/071,248 Expired - Fee Related US7528255B2 (en) 1999-01-13 2002-02-11 Hydroxy, ω-carboxyaryl substituted diphenyl ureas and dirivatives thereof as raf kinase inhibitors
US11/845,595 Abandoned US20080032979A1 (en) 1999-01-13 2007-08-27 Omega-Carboxyaryl Substituted Diphenyl Ureas As Raf Kinease Inhibitors

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US20010034447A1 (en) 2001-10-25
US20010011136A1 (en) 2001-08-02
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US20030139605A1 (en) 2003-07-24
FR06C0034I1 (cs) 2006-08-12
FR06C0034I2 (fr) 2007-04-27
EP1140840B1 (en) 2006-03-22
CY1105286T1 (el) 2010-03-03
US20080032979A1 (en) 2008-02-07
US20010011135A1 (en) 2001-08-02
CY2007002I1 (el) 2009-11-04
US7528255B2 (en) 2009-05-05
EP1140840A1 (en) 2001-10-10
US20020042517A1 (en) 2002-04-11
CY2007002I2 (el) 2009-11-04
EP1140840A4 (en) 2002-09-18

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