David W End

US Patent:

6365600, Apr 2, 2002

Filed:

Nov 30, 1999

Appl. No.:

09/445009

Inventors:

David William End - Ambler PA
Michael J. Zelesko - Hatboro PA

Assignee:

Janssen Pharmaceutica, N.V.

International Classification:

A61K 3147

US Classification:

514312, 514154, 514 44

Abstract:

This invention comprises the use of compounds of formula (I) wherein the dotted line represents an optional bond; X is oxygen or sulfur; R is hydrogen, C alkyl, Ar , Ar C alkyl, quinolinylC alkyul, pyridylC alkyl, hydroxyC alkyl, C alkyloxyC alkyl, mono- or di(C alkyl)aminoC alkyl, aminoC alkyl, or a radical of formula âAlk âC(=))âR or âAlk âS(O) âR ; R , R and R each independently are hydrogen, hydroxy, halo, cyano, C alkyl, C alkyloxy, hydroxyC alkyloxy, C alkyloxyC alkyloxy, aminoC alkyloxy, mono- or di(C alkyl)aminoC alkyloxy, Ar Ar C alkyl, Ar -oxy, Ar C alkyloxy, hydroxycarbonyl, C alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C alkenyl; R and R each independently are hydrogen, halo, Ar , C -alkyl, hydroxyC alkyl, C alkyloxyC alkyl, C alkyloxy, C alkylthio, amino, hydroxycarbony, C alkyloxycarbonyl, C alkylS(O)C alkul or C alkylS(O) C alkyl; R and R independenly are hydrogen, halo, cyano, C alkyl, 4,4-dimethyl-oxazolyl, C alkyloxy or Ar oxyl R is hydrogen, C alkyl, cyano, hydroxycarbonyl, C alkyloxycarbonyl, C alkylcarbonylC alkyl, cyanoC alkyl, C alkyloxycarbonylC alkyl, carboxyC alkyl, hydroxyC alkyl, aminoC alkyl, mono- or di(C alkyl)aminoC alkyl, imidazolyl, haloC alkyl, C alkyloxyC alkyl, aminocarbonylC alkyl, or a radical of formula âOâR , âSâR , âNâR R ; R is hydrogen, halo, cyano, C alkyl, C alkyloxycarbonyl, Ar ; R is hydrogen, C alkyl, C alkyloxy or halo; R is hydrogen or C alkyl; for the manufacture of a medicament to inhibit smooth muscle cell proliferation.

US Patent:

6451812, Sep 17, 2002

Filed:

Jan 3, 2001

Appl. No.:

09/743077

Inventors:

David William End - Ambler PA
Marina Lucie Louise Cools - Retie, BE
Jean Pierre Frans Van Wauwe - Beerse, BE

Assignee:

Janssen Pharmaceutica N.V. - Beerse

International Classification:

A61K 3147

US Classification:

514312, 514311, 514314

Abstract:

The present invention is concerned with the finding that farnesyl protein transferase inhibitors are useful for preparing a pharmaceutical composition for treating arthropathies such as rheumatoid arthritis, osteoarthritis, juvenile arthritis, and gout.

US Patent:

6545020, Apr 8, 2003

Filed:

Jan 3, 2001

Appl. No.:

09/743130

Inventors:

Robert Franciscus Van Ginckel - Vorselaar, BE
Wim Joanna Floren - Rijkevorsel, BE
David William End - Ambler PA
Walter Boudewijin Leopold Wouters - Kapellen, BE

Assignee:

Janssen Pharmaceutica, N.V.

International Classification:

A61K 3147

US Classification:

514312, 514311, 514314

Abstract:

The present invention is concerned with the finding that farnesyl protein transferase inhibitors have radiosensitizing properties which makes them useful for preparing a pharmaceutical composition for administration before, during or after irradiation of a tumor for treating cancer in vivo.

US Patent:

6734194, May 11, 2004

Filed:

Jun 18, 2003

Appl. No.:

10/464570

Inventors:

David William End - Ambler PA
Michael J. Zelesko - Hatboro PA

Assignee:

Janssen Pharmaceutica N.V.

International Classification:

A61K 3147

US Classification:

514312, 514154, 514 44

Abstract:

This invention comprises the use of compounds of formula (I) wherein the dotted line represents an optional bond; X is oxygen or sulfur; R is hydrogen, C alkyl, Ar , Ar C alkyl, quinolinylC alkyl, pyridylC alkyl, hydroxyC alkyl, C alkyloxyC alkyl, mono- or di(C alkyl)aminoC alkyl, aminoC alkyl, or a radical of formula âAlk âC( O)âR , âAlk âS(O)âR or âAlk âS(O) âR ; R , R and R each independently are hydrogen, hydroxy, halo, cyano, C alkyl, C alkyloxy, hydroxyC alkyloxy, C alkyloxy C alkyloxy, aminoC alkyloxy, mono- or di(C alkyl)aminoC alkyloxy, Ar , Ar C alkyl, Ar oxy, Ar C alkyloxy, hydroxycarbonyl, C alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C alkenyl; R and R each independently are hydrogen, halo, Ar , C alkyl, hydroxyC alkyl, C alkyloxyC alkyl, C alkyloxy, C alkylthio, amino, hydroxycarbonyl, C alkyloxycarbonyl, C alkylS(O)C alkyl or C alkylS(O) C alkyl; R and R each independently are hydrogen, halo, cyano, C alkyl, 4,4-dimethyl-oxazolyl, C alkyloxy or Ar oxy; R is hydrogen, C alkyl, cyano, hydroxycarbonyl, C alkyloxycarbonyl, C alkylcarbonylC alkyl, cyanoC alkyl, C alkyloxycarbonylC alkyl, carboxyC alkyl, hydroxyC alkyl, aminoC alkyl, mono- or di(C alkyl)aminoC alkyl, imidazolyl, haloC alkyl, C alkyloxyC alkyl, aminocarbonylC alkyl, or a radical of formula âOâR , âSâR , âNâR R ; R is hydrogen, halo, cyano, C alkyl, C alkyloxycarbonyl, Ar ; R is hydrogen, C alkyl, C alkyloxy or halo; R is hydrogen or C alkyl; for the manufacture of a medicament to inhibit smooth muscle cell proliferation.

US Patent:

6743805, Jun 1, 2004

Filed:

Nov 28, 2001

Appl. No.:

09/996147

Inventors:

David William End - Ambler PA
Michael J. Zelesko - Hatboro PA

Assignee:

Janssen Pharmaceutica NV - Beerse

International Classification:

A61K 3147

US Classification:

514312, 514154, 514 44

Abstract:

This invention comprises the use of compounds of formula (I) wherein the dotted line represents an optional bond; X is oxygen or sulfur; R is hydrogen, C alkyl, Ar , Ar C alkyl, quinolinylC alkyl, pyridylC alkyl, hydroxyC alkyl, C alkyloxyC alkyl, mono- or di(C alkyl)aminoC alkyl, aminoC alkyl, or a radical of formula -Alk -C( O)âR , -Alk -S(O)âR or -Alk -S(O) âR ; R , R and R each independently are hydrogen, hydroxy, halo, cyano, C alkyl, C alkyloxy, hydroxyC alkyloxy, C alkyloxyC alkyloxy, aminoC alkyloxy, mono- or di(C alkyl)aminoC alkyloxy, Ar , Ar C alkyl, Ar oxy, Ar C alkyloxy, hydroxycarbonyl, C alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C alkenyl; R and R each independently are hydrogen, halo, Ar , C alkyl, hydroxyC alkyl, C alkyloxyC alkyl, C alkyloxy, C alkylthio, amino, hydroxycarbonyl, C alkyloxycarbonyl, C alkylS(O)C alkyl or C alkylS(O) C alkyl; R and R each independently are hydrogen, halo, cyano, C alkyl, 4,4-dimethyl-oxazolyl, C alkyloxy or Ar oxy; R is hydrogen, C alkyl, cyano, hydroxycarbonyl, C alkyloxycarbonyl, C alkylcarbonylC alkyl, cyanoC alkyl, C alkyloxycarbonylC alkyl, carboxyC alkyl, hydroxyC alkyl, aminoC alkyl, mono- or di(C alkyl)aminoC alkyl, imidazolyl, haloC alkyl, C alkyloxyC alkyl, aminocarbonylC alkyl, or a radical of formula âOâR , âSâ R , âNâR R ; R is hydrogen, halo, cyano, C alkyl, C alkyloxycarbonyl, Ar ; R is hydrogen, C alkyl, C alkyloxy or halo; R is hydrogen or C alkyl; for the manufacture of a medicament to inhibit smooth muscle cell proliferation.

US Patent:

6838467, Jan 4, 2005

Filed:

Feb 20, 2001

Appl. No.:

10/220162

Inventors:

David William End - Ambler PA, US

Assignee:

Janssen Pharmaceutica N. V. - Beerse

International Classification:

A61K 3147

US Classification:

514312

Abstract:

This invention relates to a method of treatment and dosing regimen for treating mammalian tumors by the discontinuous administration of a farnesyl transferase inhibitor over an abbreviated one to five day dosing schedule.

US Patent:

7049324, May 23, 2006

Filed:

Nov 15, 2000

Appl. No.:

10/130322

Inventors:

Ashis Kumar Saha - Harleysville PA, US
David William End - Ambler PA, US
Bart Lieven Daniel De Corte - Southampton PA, US
Henry Joseph Breslin - Lansdale PA, US
Li Liu - Doylestown PA, US

International Classification:

A61K 31/47
C07D 215/38
C07D 249/08

US Classification:

514311, 5482622, 5482676, 546169, 514383

Abstract:

p-00010000.

US Patent:

7253183, Aug 7, 2007

Filed:

Apr 14, 2004

Appl. No.:

10/823862

Inventors:

David William End - Ambler PA, US
Michael J. Zelesko - Hatboro PA, US

Assignee:

Janssen Pharmaceutica N.V. - Beerse

International Classification:

A61K 31/4709

US Classification:

514312, 514154

Abstract:

This invention comprises the use of compounds of formula (I).