1
Marc Gustaaf Celine Verdonck, Patrick René Angibaud, Bruno Roux, Isabelle Noëlle Constance Pilatte, Peter Ten Holte, Janine Arts, Kristof Van Emelen: Substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase. Janssen Pharmaceutica, Rajiv S Shah, June 5, 2012: US08193205 (4 worldwide citation)

This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.


2
Pierre Henri Storck, Bruno Schoentjes, Arnaud Marcel Pierre Piettre, Philipp Ermert, Virginie Sophie Poncelet, Imre Christian Francis Csoka: Inhibitors of the interaction between MDM2 and p53. Janssen Pharmaceutica, Rajiv S Shah, October 16, 2012: US08288377 (3 worldwide citation)

The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: wherein n, s, t, R1, R2, R3, R4, R5, X, Y, Q, Z, G, E and D have defined meanings.


3
Kristof Van Emelen, Janine Arts, Leo Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noëlle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviane Van heusden: Sulfonyl-derivatives as novel or histone deacetylase. Janssen Pharmaceutica, Rajiv S Shah, January 17, 2012: US08097611 (2 worldwide citation)

This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.


4
Jérôme Emile Georges Guillemont, Patrice Palandijian, Marc René De Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts legal representative: HIV inhibiting pyrimidines derivatives. Janssen Pharmaceutica, Rajiv S Shah, December 20, 2011: US08080551 (1 worldwide citation)

HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.


5
Jérôme Emile Georges Guillemont, Paul Theodoor Agnes Stevens, Alex Herman Copmans, Jozef Peeters, Alfred Elisabeth Stappers, Roger Petrus Gerebern Vandecruys, Paul Stoffels: Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile. Janssen Pharmaceutica, Rajiv S Shah, January 24, 2012: US08101629 (1 worldwide citation)

The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation.


6
Jérôme Emile Georges Guillemont, Paul Theodoor Agnes Stevens, Alex Herman Copmans, Jozef Peeters, Alfred Elisabeth Stappers, Roger Petrus Gerebern Vandecruys, Paul Stoffels: Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile. Janssen Pharmaceutica, Rajiv S Shah, June 7, 2011: US07956063 (1 worldwide citation)

The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation.


7
Marc Gaston Venet, Patrick René Angibaud, David William End: Farnesyl transferase inhibiting 1,2-annelated quinoline enantiomer. Janssen Pharmaceutica, Rajiv S Shah, December 11, 2012: US08329714 (1 worldwide citation)

(−)-5-(3-Chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H-imidazol-5-yl)tetrazolo-[1,5-a]quinazoline-7-methanamine and its pharmaceutically acceptable acid addition salts, and the use of such compounds in medicine especially for the treatment of cancer.


8
Marc Gaston Venet, Patrick René Angibaud, David William End: Farnesyl transferase inhibiting 1,2-annelated quinoline enantiomer. Janssen Pharmaceutica, Rajiv S Shah, November 27, 2012: US08318753 (1 worldwide citation)

(−)-5-(3-Chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H-imidazol-5-yl)tetrazolo-[1,5-a]quinazoline-7-methanamine and its pharmaceutically acceptable acid addition salts, and the use of such compounds in medicine especially for the treatment of cancer.


9
Jean Fernand Armand Lacrampe, Christophe Meyer, Bruno Schoentjes, Delphine Yvonne Raymonde Lardeau, Alain Philippe Poncelet, Luc Van Hijfte: Inhibitors of the interaction between MDM2 and P53. Janssen Pharmaceutica, Rajiv S Shah, July 31, 2012: US08232298 (1 worldwide citation)

The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, A and Z have defined meanings.


10
Didier Philippe Robert Schils, Alfred Elisabeth Stappers: Process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)amino]benzonitrile. Tibotec Pharmaceuticals, Rajiv S Shah, January 24, 2012: US08101752 (1 worldwide citation)

This invention relates to a process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)-amino]benzonitrile (I) starting from a 4-oxo-1,6-dihydro-pyrimidinylcarboxylic acid ester (II) or starting from a guanidine derivative which is reacted with an alkoxy-methylene malonic acid ester to an ester (II) ...