Donald W Ludovici

US Patent:

6372729, Apr 16, 2002

Filed:

Aug 8, 2000

Appl. No.:

09/634340

Inventors:

Frederik Frans Desiré Daeyaert - Antwerpen, BE
Bart De Corte - Southampton PA
Marc René De Jonge - Tilburg, NL
Jan Heeres - Vosselaar, BE
Chih Yung Ho - Lansdale PA
Paul Adriaan Jan Janssen - Vosselaar, BE
Robert W. Kavash - Glenside PA
Lucien Maria Henricus Koymans - Turnhout, BE
Michael Joseph Kukla - Maple Glen PA
Donald William Ludovici - Quakertown PA

Assignee:

Janssen Pharmaceutica N.V. - Beerse

International Classification:

C07D25166

US Classification:

514113, 514245, 5142362, 544194, 544196, 544197, 544198, 544199, 544208, 544209

Abstract:

This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR or N; n is 0, 1, 2, 3 or 4; R and R are each independently selected from hydrogen, hydroxy, C alkyl, C alkyloxy, C alkylcarbonyl, C alkyloxycarbonyl, aryl, amino, mono- or di(C alkyl)amino, mono- or di(C alkyl)aminocarbonyl wherein each of the aforementioned C alkyl groups may optionally and each individually be substituted; or R and R taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C alkyl)aminoC alkylidene; R is hydrogen, aryl, C alkylcarbonyl, optionally substituted C alkyl; and each R independently is hydroxy, halo, C alkyl, C alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is âXâR or âX-Alk-R ; wherein R and R each independently are indanyl, indolyl or phenyl; each of said indanyl, indolyl or phenyl may be substituted; and X is âNR â, âNHâNHâ, âN Nâ, âOâ, âSâ, âS( O)â or âS( O) â; aryl is optionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and pharmaceutical compositions comprising them.

US Patent:

6380194, Apr 30, 2002

Filed:

Sep 26, 1997

Appl. No.:

08/938602

Inventors:

Paul A. J. Janssen - Vosselaar, BE
Jan Heeres - Vosselaar, BE
Henri E. L. Moereels - Ekeren, BE
Michael Joseph Kukla - Spring House PA
Donald W. Ludovici - Spring House PA

Assignee:

Janssen Pharmaceutica N.V. - Beerse

International Classification:

C07D25150

US Classification:

514245, 544206, 544211

Abstract:

This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R and R are each independently selected from hydrogen; hydroxy; amino; optionally substituted C alkyl; C alkyloxy; C alkylcarbonyl; C alkyloxycarbonyl; Ar ; mono- or di(C alkyl)amino; mono- or di(C alkyl)-aminocarbonyl; dihydro-2(3H)-furanone; or R and R taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C alkyl)amino-C alkylidene; R is hydrogen, Ar , C alkylcarbonyl, C alkyl, C alkyloxycarbonyl, C alkyl substituted with C alkyloxycarbonyl; and R , R , R , R and R are each independently selected from hydrogen, halo, C alkyl, C alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C alkyl; C alkenyl; C alkynyl; C cycloalkyl; Ar is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

US Patent:

6440986, Aug 27, 2002

Filed:

Dec 27, 2000

Appl. No.:

09/749181

Inventors:

Koenraad Jozef Lodewijk Marcel Andries - Beerse, BE
Bart De Corte - Southampton PA
Marc René De Jonge - Tilburg, NL
Jan Heeres - Vosselaar, BE
Chih Yung Ho - Lansdale PA
Marcel August Constant Janssen - Vosselaar, BE
Paul Adriaan Jan Janssen - Vosselaar, BE
Lucien Maria Henricus Koymans - Turnhout, BE
Michael Joseph Kukla - Maple Glen PA
Donald William Ludovici - Quakertown PA
Koen Jeanne Alfons Van Aken - Turnhout, BE

Assignee:

Janssen Pharmaceutica, N.V. - Beerse

International Classification:

C07D23928

US Classification:

514272, 544321, 544320, 544323, 514274, 514275

Abstract:

This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR or N; n is 0 to 4; Q is hydrogen or âNR R ; R and R are selected from hydrogen, hydroxy, C alkyl, C alkyloxy, C alkylcarbonyl, C alkyloxycarbonyl, aryl, amino, mono- or di(C alkyl)amino, mono- or di(C alkyl)aminocarbonyl wherein each C alkyl may optionally be substituted; or R and R taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C alkyl)aminoC alkylidene; R is hydrogen, aryl, C alkylcarbonyl, optionally substituted C alkyl, C alkyloxycarbonyl,; and R is hydroxy, halo, optionally substituted C alkyl, C alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R is hydrogen or C alkyl; L is optionally substituted C alkyl, C alkenyl, C alkynyl, C cycloalkyl; or L is âX âR or âX âAlkâR wherein R and R are optionally substituted phenyl; X and X are âNR â, âNHâNHâ, âN Nâ, âOâ, âSâ, âS( O)â or âS( O) â; Alk is C alkanediyl; aryl is potionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical: for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

US Patent:

6638932, Oct 28, 2003

Filed:

Aug 2, 2001

Appl. No.:

09/831808

Inventors:

Bart De Corte - Southampton PA
Marc René de Jonge - Tilburg, NL
Jan Heeres - Vosselaar, BE
Paul Adriaan Jan Janssen - Vosselaar, BE
Robert W. Kavash - Glenside PA
Lucien Maria Henricus Koymans - Retie, BE
Michael Joseph Kukla - Maple Glen PA
Donald William Ludovici - Quakertown PA
Koen Jeanne Alfons Van Aken - Turnhout, BE

Assignee:

Janssen Pharmaceutica N.V. - Beerse

International Classification:

C07D25116

US Classification:

514241, 544194, 544208, 544209, 544213

Abstract:

This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein âa a âa a â forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R is hydrogen, aryl, formyl, C alkylcarbonyl, C alkyl, C alkyloxycarbonyl or substituted C alkyl; each R independently is hydroxy, halo, optionally substituted C alkyl, C alkenyl or C alkynyl, C cycloalkyl, C alkyloxy, C alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, âS( O) R , âNHâS( O) R , âC( O)R , âNHC( O)H, âC( O)NHNH , âNHC( O)R , âC( NH)R or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C alkyl, C alkenyl, C alkynyl or C cycloalkyl; or L is âXâR wherein R is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl, or pyridazinyl; X is âNR â, âNHâNHâ, âN Nâ, âOâ, âC( O)â, âCHOHâ, âSâ, âS( O)â or âS( O) â; aryl is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

US Patent:

6774235, Aug 10, 2004

Filed:

Feb 5, 2002

Appl. No.:

10/067383

Inventors:

Frederik Frans Desiré Daeyaert - Antwerpen, BE
Bart De Corte - Southampton PA
Marc René De Jonge - Tilburg, NL
Jan Heeres - Vosselaar, BE
Chih Yung Ho - Lansdale PA
Paul Adriaan Jan Janssen - Vosselaar, BE
Robert W. Kavash - Glenside PA
Lucien Maria Henricus Koymans - Turnhout, BE
Michael Joseph Kukla - Maple Glen PA
Donald William Ludovici - Quakertown PA

Assignee:

Janssen Pharmaceutica N.V. - Beerse

International Classification:

C07D25166

US Classification:

544208

Abstract:

This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR or N; n is 0, 1, 2, 3 or 4; R and R are each independently selected from hydrogen, hydroxy, C alkyl, C alkyloxy, C alkylcarbonyl, C alkyloxycarbonyl, aryl, amino, mono- or di(C alkyl)amino, mono- or di(C alkyl)aminocarbonyl wherein each of the aforementioned C alkyl groups may optionally and each individually be substituted; or R and R taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C alkyl)aminoC alkylidene; R is hydrogen, aryl, C alkylcarbonyl, optionally substituted C alkyl; and each R independently is hydroxy, halo, C alkyl, C alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is âXâR or âXâAlkâR ; wherein R and R each independently are indanyl, indolyl or phenyl; each of said indanyl, indolyl or phenyl may be substituted; and X is âNR â, âNHâNHâ, âN Nâ, âOâ, âS â, âS( O)â or âS( O) â; aryl is optionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and pharmaceutical compositions comprising them.

US Patent:

6858609, Feb 22, 2005

Filed:

Nov 15, 2001

Appl. No.:

10/002456

Inventors:

Paul A. J. Janssen - Vosselaar, BE
Jan Heeres - Vosselaar, BE
Henri E. L. Moereels - Ekeren, BE
Michael Joseph Kukla - Spring House PA, US
Donald W. Ludovici - Spring House PA, US

Assignee:

Janssen Pharmaceutica N.V. - Beerse

International Classification:

C07D251/18
C07D251/42
A61K031/53

US Classification:

514245, 5142362, 544205, 544206, 544113, 544211, 544212

Abstract:

This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein Rand Rare each independently selected from hydrogen; hydroxy; amino; optionally substituted Calkyl; Calkyloxy; Calkylcarbonyl; Calkyloxycarbonyl; Ar; mono- or di(Calkyl)amino; mono- or di(Calkyl)-aminocarbonyl; dihydro-2(3H7)-furanone; or Rand Rtaken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(Calkyl)amino-Calkylidene; Ris hydrogen, Ar, Calkylcarbonyl, Calkyl, Calkyloxy-carbonyl, Calkyl substituted with Calkyloxycarbonyl; and R, R, R, Rand Rare each independently selected from hydrogen, halo, Calkyl, Calkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted Calkyl; Calkenyl; Calkynyl; Ccycloalkyl; Aris optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

US Patent:

6878717, Apr 12, 2005

Filed:

Nov 1, 1999

Appl. No.:

09/430966

Inventors:

Bart De Corte - Southampton PA, US
Marc Rene De Jonge - 5045 CA Tilburg, NL
Jan Heeres - Vosselaar, BE
Chih Yung Ho - Lansdale PA, US
Paul Adriaan Jan Janssen - B2350 Vosselaar, BE
Robert W. Kavash - Maple Glen PA, US
Lucien Maria Henricus Koymans - B-2300 Turnhout, BE
Michael Joseph Kukla - Maple Glen PA, US
Donald William Ludovici - Quakertown PA, US
Koen Jeanne Alfons Van Aken - B-2300 Turnhout, BE

International Classification:

A61K031/506
A61P031/18
C07D239/42
C07D239/48
C07D239/50

US Classification:

514269, 514272, 544295, 544296, 544315, 544316, 544322, 544323, 544324

Abstract:

This invention concerns the use of compounds of formula: the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a=-a-a=a- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; Ris hydrogen, aryl, formyl, Calkylcarbonyl, Calkyl, Calkyloxy-carbonyl, substituted Calkyl, or substituted CalkyloxyCalkylcarbonyl; each Rindependently is hydroxy, halo, optionally substituted Calkyl, Calkenyl or Calkynyl, Ccycloalkyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(Calkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-methylthio, —S(═O)R, —NH—S(═O)R, —C(═O)R, —NHC(═O)H, —C(═O)NHNH, —NHC(═O)R, —C(═NH)Ror a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted Calkyl, Calkenyl, Calkynyl or Ccycloalkyl; or L is —X—Rwherein Ris optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)—; Q is hydrogen, Calkyl, halo, polyhalo-Calkyl or an optionally substituted amino group; Y represents hydroxy, halo, Ccycloalkyl, optionally substituted Calkyl, Calkenyl or Calkynyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(Calkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)R, —NH—S(═O)R, —C(═O)R, —NHC(═O)H, —C(═O)NHNH, —NHC(═O)R, —C(═NH)Ror aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

US Patent:

6962916, Nov 8, 2005

Filed:

Mar 26, 2003

Appl. No.:

10/397760

Inventors:

Paul A. J. Janssen - Vosselaar, BE
Jan Heeres - Vosselaar, BE
Henri E. L. Moereels - Ekeren, BE
Michael Joseph Kukla - Spring House PA, US
Donald W. Ludovici - Spring House PA, US

Assignee:

Janssen Pharmaceutica N.V. - Beerse

International Classification:

A61K031/53
A61K031/535

US Classification:

514245, 5142288

Abstract:

This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein Rand Rare each independently selected from hydrogen; hydroxy; amino; optionally substituted Calkyl; Calkyloxy; Calkylcarbonyl; Calkyloxycarbonyl; Ar; mono- or di(Calkyl)amino; mono- or di(Calkyl)aminocarbonyl; dihydro-2(3H)-furanone; or Rand Rtaken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(Calkyl)amino-Calkylidene; Ris hydrogen, Ar, Calkylcarbonyl, Calkyl, Calkyloxycarbonyl, Calkyl substituted with Calkyloxycarbonyl; and R, R, R, Rand Rare each independently selected from hydrogen, halo, Calkyl, Calkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted Calkyl; Calkenyl; Calkynyl; Ccycloalkyl; Aris optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.