Janssen Pharmaceutical

Beerse, Belgium

Janssen Pharmaceutical

Beerse, Belgium
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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: 2017-04-05

The amorphous form of the sodium salt of the macrocyclic inhibitor of HCV of formula:


Patent
Microfluidics, Janssen Pharmaceutical and NXP Semiconductors | Date: 2017-02-15

The invention relates to a channel for trapping particles to be fed to said channel with a fluid, said channel having a bottom and opposite sidewalls, the sidewalls defining a width of the channel, said channel further comprising:- a first channel part;- a second channel part in fluid through flow connection with said first channel part and downstream of said first channel part;- an elevated structure provided in said channel that divides said channel in said first channel part and said second channel part and for trapping particles in said first channel part;- at least one flow gap provided by said elevated structure for providing said fluid through flow connection between the first channel part and the second channel part for allowing, in use, at least some fluid to flow past said elevated structure into said second channel part while trapping said particles in said first channel part;wherein said elevated structure is substantially U-shaped and has a base extending substantially between the opposite sidewalls of the channel and two legs extending from the base in an upstream direction, wherein at least part of said U-shaped elevated structure defines at least part of a particle trapping area for trapping the particles to be fed to said channel. The invention further relates to a flow cell comprising such a channel. The invention also relates to an assembly comprising such a flow cell and a detection means. The invention also relates to a method for trapping particles in such a channel. And finally, the invention relates to a method for analyzing a sample using such an assembly.


Patent
Janssen Pharmaceutical | Date: 2017-01-04

The present invention is directed to novel opioid receptor modulators of Formula: (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.


Patent
Janssen Pharmaceutical | Date: 2017-01-04

The present invention is directed to compounds having P2X7 modulating properties. The invention also relates to pharmaceutical compositions comprising these compounds. Methods of making and using these compounds are also within the scope of the invention.


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: 2017-01-16

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.


Grant
Agency: European Commission | Branch: H2020 | Program: RIA | Phase: NMBP-01-2016 | Award Amount: 7.59M | Year: 2017

Objectives The H-CCAT project designs, upscales and shapes hybrid catalysts for the C-H functionalization of aromatic compounds. These solid catalysts will possess better recoverability, higher turnover numbers and better selectivity than current homogeneous catalysts for these reactions. The solid catalysts are applied at demonstration scale in the step-economical production of arylated or alkenylated aromatics, yielding motifs of active pharmaceutical ingredients. Methodology We will design heterogeneous hybrid catalysts featuring deactivation-resistant active sites, based on N-heterocyclic carbenes (NHCs) or diimine ligands and active metal ions. Via efficient, one-step protocols based on self-assembly, these sites will be embedded in robust porous hybrid materials like hybrid silica or metal-organic frameworks. Deactivation or metal aggregation will be prevented by site isolation or by efficient metal reoxidation (for the oxidative alkenylations). Metal leaching is precluded by using strong bonds between metals and embedded ligands like NHCs. Flow protocols will be designed to maximize the turnover numbers. Catalyst synthesis will be scaled up to kg scale, using efficient one-step protocols, minimizing use of solvents or waste formation. Soft shaping methods, e.g. spray drying, will preserve porosity and activity of the hybrid solids. A demonstration is conducted at minipilot scale at the J&J site (Belgium), allowing LCA analysis, techno-economic assessment and elaboration of the business plan. Relevance to work program The catalysts feature new, deactivation resistant active sites; their TOF/TON is maximized by an appropriate porous structure which even can be swelling. Catalysts are produced using innovative one-step protocols to form porous hybrid catalysts as powders or even immediately as shaped objects. The molecules targeted have strong biological and pharmaceutical relevance; they target diseases like influenza, cancer or HIV (case study: Rilpivirine).

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