Beerse, Belgium
Beerse, Belgium

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Patent
Janssen Pharmaceutical | Date: 2017-01-24

The present invention is directed to co-therapy and methods for the treatment and prevention of glucose-related disorders such as Type 2 diabetes mellitus and Syndrome X. The present invention is further directed to pharmaceutical compositions for the co-therapy and methods described herein.


Patent
Janssen Pharmaceutical | Date: 2017-01-24

Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.


Patent
Janssen Pharmaceutical | Date: 2017-01-19

Disclosed is an antibody which binds to paliperidone, which can be used to detect paliperidone in a sample such as in a competitive immunoassay method. The antibody can be used in a lateral flow assay device for point-of-care detection of paliperidone, including multiplex detection of aripiprazole, olanzapine, quetiapine, risperidone and paliperidone in a single lateral flow assay device.


Patent
Janssen Pharmaceutical | Date: 2017-01-16

This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a^(1)=a^(2)-a^(3)=a^(4)- and -b^(1)=b^(2)-b^(3)=b^(4)- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R^(1 )is hydrogen; aryl; formyl; C_(1-6)alkylcarbonyl; C_(1-6)alkyl; C_(1-6)alkyloxycarbonyl; substituted C_(1-6)alkyl, C_(1-6)alkylcarbonyl, C_(1-6)alkyloxycarbonyl, C_(1-6)alkylcarbonyloxy; substituted C_(1-6)alkyloxyC_(1-6)alkylcarbonyl; R^(2 )is hydroxy, halo, optionally substituted C_(1-6)alkyl, C_(3-7)cycloalkyl, optionally substituted C_(2-6)alkenyl, optionally substituted C_(2-6)alkynyl, C_(1-6)alkyloxy, C_(1-6)alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C_(1-6)alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, S(O)_(p)R^(6), NHS(O)_(p)R^(6), C(O)R^(6), NHC(O)H, C(O)NHNH_(2), NHC(O)R^(6), C(NH)R^(6 )or a 5-membered heterocycle; X_(1 )is NR^(5), NHNH, NN, O, C(O), C_(1-4)alkanediyl, CHOH, S, S(O)_(p), X_(2)C_(1-4)alkanediyl- or C_(1-4)alkanediyl-X_(2); R^(3 )is NHR^(13); NR^(13)R^(14); C(O)NHR^(13); C(O)NR^(13)R^(14); C(O)R^(15); CHNNHC(O)R^(16); substituted C_(1-6)alkyl; optionally substituted C_(1-6)alkyloxyC_(1-6)alkyl; substituted C_(2-6)alkenyl; substituted C_(2-6)alkynyl; C_(1-6)alkyl substituted with hydroxy and a second substituent; C(NOR^(8))C_(1-4)alkyl; R^(7); or X_(3)R^(7); R^(4 )is halo, hydroxy, C_(1-6)alkyl, C_(3-7)cycloalkyl, C_(1-6)alkyloxy, cyano, nitro, polyhaloC_(1-6)alkyl, polyhaloC_(1-6)alkyloxy, aminocarbonyl, C_(1-6)alkyloxycarbonyl, C_(1-6)alkylcarbonyl, formyl, amino, mono- or di(C_(1-4)alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.


Patent
Janssen Pharmaceutical | Date: 2017-01-06

The present invention relates to formulations including compounds of Formula (I), or prodrug, or a pharmaceutically acceptable salt thereof.


Patent
Janssen Pharmaceutical | Date: 2017-01-04

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, m, p, s, t, R^(1), R^(2), R^(3), R^(4), R^(5), R^(6), R^(7), R^(20), X, Y, Q and Z have defined meanings.


The present invention relates to substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrazine derivatives and 5,6,7,8-tetrahydro-4H-pyrazolo[1,5-a][1,4]diazepine derivatives of formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as ROS 1 inhibitors. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.


Patent
Janssen Pharmaceutical | Date: 2017-01-11

The present invention is directed to bicyclic pyrrole derivatives of formula (I), pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example. Type II diabetes mellitus.


Patent
Janssen Pharmaceutical | Date: 2017-03-02

The present invention comprises compounds of Formula I. wherein: R^(1), R^(2), R^(3), R^(4), R^(5), R^(6), R^(7), R^(8), and R^(9 )are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.


A process for preparing [(1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, by the resolution of racemic 4-oxo-1,2-cyclopentanedicarboxylic acid (V), said process comprising:

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