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Assignee: Janssen Pharmaceutica NV


Location: BE
No. of patents: 57

1    
NumberTitleIssue Date
80763586-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE)
The present invention is directed to 6-substituted-thio-2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD), mild cognitive impairment, senility and/or dementia. The compounds of the p...
12/13/2011
7993638Cancer treatment combining lymphodepleting agent with CTLs and cytokines
In a cancer treatment combining cell therapy with chemotherapy, autologous CD8+ T cells are obtained from a patient, activated ex vivo by contacting them with xenogenic antigen presenting cells loaded with selected peptide antigen, thereby generating anti...
08/09/2011
7968580Imidazolidin-2-one derivatives as selective androgen receptor modulators (SARMS)
The present invention is directed to novel imidazolidin-2-one derivatives having a structure according to Formula I wherein a, b, R1, R2, R3, and R4 are as defined above, pharmace...
06/28/2011
7951829Benzimidazole modulators of VR1
The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them. ...
05/31/2011
7947694Substituted pyrazolo[3,4-D]pyrimidines as cell cycle kinase inhibitors
This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X1 and X2 have defined meanings, having cel...
05/24/2011
7939052Method of measuring the biological activity of an urotensin II receptor
Administration of U-II to rats caused an increase in the redness or the skin temperature of the ear of the rats. The increase was inhibited by compounds that decease the biological activity of the U-II/UT receptor. Thus, the present invention provides methods of mea...
05/10/2011
79323992-substituted benzimidazoles as selective androgen receptor modulators (SARMS)
The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. ...
04/26/2011
7928246Dihydroisoindolones as allosteric modulators of glucokinase
The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating glucokinase mediated disorders. More particularly, the c...
04/19/2011
79282381,2,3,4-tetrahydro-quinoline derivatives as CETP inhibitors
The invention is directed to compounds of Formula (I) described herein useful as CETP inhibitors, compositions containing them, and methods of using them. ...
04/19/2011
7897781Cold menthol receptor-1 antagonists
The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated d...
03/01/2011
7897771Fused heterocyclic compounds
Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases. ...
03/01/2011
7897636Sulfamide derivative useful for the treatment of epilepsy
The present invention is directed to novel sulfamide derivatives, pharmaceutical compositions comprising said compounds and methods for the treatment of epilepsy and related disorders comprising administering to a subject in need thereof, said compounds, either alon...
03/01/2011
7893064Hydrazone derivatives as kinase inhibitors
The present invention is directed to novel bicyclic pyrimidine compounds of Formula (I) or a form or composition thereof as inhibitors of ATP-protein kinase interactions, wherein substituents on each side of the iminomethyl...
02/22/2011
7887845Antiviral compositions
The present invention is concerned with pharmaceutical compositions of antiviral compounds which can be administered to a mammal, in particular a human, suffering from a viral infection. These compositions comprise particles obtainable by melt-extruding a mixture co...
02/15/2011
7846930Diaryl-substituted tetrahydroisoquinolines as histamine Hreceptor and serotonin transporter modulators
Certain diaryl-substituted tetrahydroisoquinoline compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases. ...
12/07/2010
7879895Benzimidazole derivatives useful as selective androgen receptor modulators (SARMS)
The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. ...
02/01/2011
7875621Substituted 2-alkyl quinazolinone derivatives as PARP inhibitors
The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions containing compounds of formula (I) wherein R1, R3, L, X, Y and Z have defin...
01/25/2011
7872138Process for the preparation of substituted-1,2,3,4-tetrahydroisoquinoline derivatives
The present invention is directed to a process for the synthesis of substituted-1,2,3,4-tetrahydroisoquinoline derivatives, useful as intermediates in the synthesis of pharmaceutical agents. ...
01/18/2011
7872044Inhibitors of chymase
The present invention is directed to a compound of Formula (I): or an enantiomer, diastereomer, polymorph or pharmaceutically acceptable salt thereof and methods for preparing said compounds and compositions, intermediates ...
01/18/2011
7868023Thiophene sulfoximines, compositions thereof, and methods of treating complement-mediated diseases and conditions
Disclosed are compounds for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade. The compounds are of Formula I or a solvate, hydrate, pharmaceutically acceptabl...
01/11/2011
7851498Hexahydro-cyclooctyl pyrazole cannabinoid modulators
This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or...
12/14/2010
7838553Benzopyran derivatives as potassium channel openers
The present invention is directed to novel benzopyran derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel. ...
11/23/2010
7825244Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: wherein R1, R2, R99, and X are as defined herein, the use of such compounds in the synthesis of prote...
11/02/2010
7825151Hexahydro-cyclooctyl pyrazole cannabinoid modulators
This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or...
11/02/2010
7825110Substituted spiroheterocycles
The invention is directed to nonpeptide substituted spiroheterobenzazepine of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as tho...
11/02/2010
7820650Antifungal 4-substituted 5,6-dihydro-4H-pyrrolo [1,2-a][1,4]benzodiazepines
The present invention concerns compounds for use as a medicine having the formula the N-oxide forms, the salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 represent...
10/26/2010
7820630Substituted indole-O-glucosides
Substituted indole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed. ...
10/26/2010
7816390N-substituted tricyclic 3-aminopyrazoles as anti-mitotic tubulin polymerization inhibitors
The invention is directed to compounds having the following structures: N-(3-ethoxyphenyl)-1,4-dihydro-6-ethoxy-7-(3-hydroxypropoxy)-1-methylindeno[1,2-c]pyrazole-3-amine; 3-[3-(3...
10/19/2010
7816331Substituted indazole-O-glucosides
Substituted indazole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed. ...
10/19/2010
7816330Substituted benzimidazole-, benztriazole-, and benzimidazolone-O-glucosides
This invention relates to substituted benzimidazole-O-glucosides, benztriazole-O-glucosides, and benzimidazolone-O-glucosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X. ...
10/19/2010
7816328Substituted fused heterocyclic C-glycosides
This invention relates to substituted fused heterocyclic C-glycosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X. ...
10/19/2010
7812183Benzopyran derivatives as potassium channel openers
The present invention is directed to novel benzopyran derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel. ...
10/12/2010
78038232-amino-4,5-trisubstituted thiazolyl derivatives
This invention concerns the use of a compound of formula (I′) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alky...
09/28/2010
7803793Heterocyclic derived metalloprotease inhibitors
This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metallop...
09/28/2010
7799785Substituted tetracyclic tetahydrofuran, pyrrolidine and tetrahydrothiophene derivatives
This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptor...
09/21/2010
7795440N-substituted tricyclic 1-aminopyrazoles as inhibitors for the treatment of cell proliferative disorders
The invention is directed to N-substituted tricyclic 3-AMINOPYRAZOLE derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directe...
09/14/2010
7795261Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists
This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined N...
09/14/2010
7790895Quinoline derivatives as potassium ion channel openers
The present invention is directed to novel quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to ion channels such as potassium channels. ...
09/07/2010
7790894Mycobacterial inhibitors
The present invention relates to novel substituted quinoline derivatives according to the general Formula (I) and pharmaceutically acceptable addition salts thereof, wherein the variable moieties are as defined in the speci...
09/07/2010
7759331Pyridine-containing macroheterococylic compounds as kinase inhibitors
This invention is directed to pyridine-containing macroheterocyclic compounds useful as kinase inhibitors, methods for producing such compounds and methods for treating or preventing a kinase mediated disorder. ...
07/20/2010
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