Patents Assigned to Janssen Pharmaceutical N.V.
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Patent number: 9981919Abstract: 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 -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,Type: GrantFiled: July 20, 2017Date of Patent: May 29, 2018Assignee: Janssen Pharmaceutical N.V.Inventors: Jérôme Emile Georges Guillemont, Patrice Palandjian, 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
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Patent number: 9227935Abstract: The invention relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(?O)—; —C(?O)—C(?O)—; —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —C(?O)—Z—; —NRx—C(?O)—Z—; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —C(?S)—Z—; —NRx—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRx— or —NRx—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein saidType: GrantFiled: December 5, 2014Date of Patent: January 5, 2016Assignee: Janssen Pharmaceutical N.V.Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J. M. De Waepenaert, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
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Publication number: 20130303506Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, 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.Type: ApplicationFiled: July 22, 2013Publication date: November 14, 2013Applicant: Janssen Pharmaceutical N.V.Inventors: Patrick René Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
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Patent number: 8404683Abstract: 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, R3, R4, R5, R6, R7, X, Y, Q and Z have defined meanings.Type: GrantFiled: November 3, 2010Date of Patent: March 26, 2013Assignee: Janssen Pharmaceutical N.V.Inventors: Jean Ferand Armand Lacrampe, Christophe Meyer, Yannick Aimè Eddy Ligny, Imre Christian Francis Csoka, Luc Van Hijfte, Janine Arts, Bruno Schoentjes, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert
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Patent number: 7998979Abstract: The present invention relates to novel substituted quinoline derivatives according to the general formula (Ia) or formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N-oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.Type: GrantFiled: December 4, 2007Date of Patent: August 16, 2011Assignee: Janssen Pharmaceutical N.V.Inventors: Jérôme Emile Georges Guillemont, Magali Madeleine Simone Motte, Koenraad Jozef Lodewijk Marcel Andries, Anil Koul
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Patent number: 7645755Abstract: The invention is directed to compounds of Formula I: wherein A, X, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: GrantFiled: April 20, 2006Date of Patent: January 12, 2010Assignee: Janssen Pharmaceutical N.V.Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Sanath K. Meegalla, M. Jonathan Rudolph, Mark J. Wall, Kenneth J. Wilson, Renee L. Desjarlais, Carl L. Manthey, Christopher Flores, Christopher J. Molloy
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Publication number: 20090253918Abstract: This invention relates to an improved process for preparing the glycine transport 1 (GlyT1) inhibitor (Z)-N-(1-(4-(2-furyl)phenyl)-1-(3-thienyl-prop-1-en-3-yl) sarcosine via the novel intermediate (Z)-3-(4-(2-furyl)phenyl)-3-(3-thienyl)-prop-2-en-1-ol and the preparation of the latter.Type: ApplicationFiled: September 26, 2007Publication date: October 8, 2009Applicant: JANSSEN PHARMACEUTICALS, N.V.Inventors: Ioannis Nicolaos Houpis, Didier Philippe Robert Schils
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Patent number: 7528154Abstract: Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.Type: GrantFiled: October 20, 2006Date of Patent: May 5, 2009Assignee: Janssen Pharmaceutical N.V.Inventors: Lieven Meerpoel, Peter Walter Maria Roevens, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Marcel Viellevoye
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Patent number: 7423147Abstract: Certain non-imidazole heterocyclic compounds are Histamine H3 modulators in the treatment of Histamine H3 receptor mediated diseases.Type: GrantFiled: March 31, 2005Date of Patent: September 9, 2008Assignee: Janssen Pharmaceutical, N.V.Inventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
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Publication number: 20080214597Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents C or N; Y represents C or N; L represents a methyl or a direct bond; Z1 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH? (a) or —CH? (b); Z2 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH? (a) or —CH? (b); R1 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxycarbonyl, NR3R4 or C1-4alkyl optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR5R6 or R1 represents C1-4alkyloxy- optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR7R8; R2 represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy-; R3 and R4 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R5 and R6 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R7 and R8 each inType: ApplicationFiled: August 26, 2005Publication date: September 4, 2008Applicant: JANSSEN PHARMACEUTICAL N.V.Inventors: Libuse Jaraskova, Joannes Theodorus Maria Linders, Louis Jozef Elisabeth Van Der Veken, Gustaaf Henri Maria Willemsens
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Patent number: 7351711Abstract: The present invention is directed to substituted indanyl compounds of Formula (I): Useful for treating integrin-mediated disorders such as, but not limited to unstable angina, thromboemboic disorders, osteoporosis, growth and metastasis of malignant tumors, diabetic retinopathy, arthritis, viral disease and surgical adhesions.Type: GrantFiled: July 28, 2004Date of Patent: April 1, 2008Assignee: Janssen Pharmaceutical, N.V.Inventors: William A. Kinney, Diane K. Luci, Bruce E. Maryanoff
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Patent number: 7301050Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: GrantFiled: September 16, 2004Date of Patent: November 27, 2007Assignee: Janssen Pharmaceutical N.V.Inventors: Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan R. DeAngelis
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Patent number: 7244866Abstract: This invention is directed to carboxamido opioid compounds pharmaceutically useful as agents for treating or modulating a central nervous system disorder and methods for treating or modulating a central nervous system disorder.Type: GrantFiled: May 11, 2005Date of Patent: July 17, 2007Assignee: Janssen Pharmaceutical N.V.Inventors: John R. Carson, Philip M. Pitis
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Patent number: 6663901Abstract: The present invention is concerned with pellets comprising a 710-1180 &mgr;m (16-25 mesh) sugar core, a coating film of a water-soluble polymer and an antifungal agent, and a seal coating layer wherein the residual concentration of dichloromethane is below 600 ppm; pharmaceutical dosage forms comprising said pellets and a method of preparing said pellets.Type: GrantFiled: June 27, 2000Date of Patent: December 16, 2003Assignee: Janssen Pharmaceutical N.V.Inventors: Paul Marie Victor Gilis, Valentin Florent Victor De Conde, Roger Petrus Gerebern Vandecruys
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Publication number: 20030082239Abstract: The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.Type: ApplicationFiled: August 14, 2002Publication date: May 1, 2003Applicant: Janssen Pharmaceutical, N.V.Inventors: Lieven Elvire Colette Baert, Geert Verreck, Dany Thone
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Patent number: 6544979Abstract: This invention concerns the use of compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula —X—COOR5, —X—CONR6R7 or —X—COR10 wherein —X—is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is —CH2—, —CH2—CH2—, —CH═CH—, —CHOH—CHType: GrantFiled: March 15, 2000Date of Patent: April 8, 2003Assignee: Janssen Pharmaceuticals, N.V.Inventor: Henricus Johannes Matheus Snoeck
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Patent number: 6251894Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; ═Q is ═O or ═NR3; X is a covalent bond or —O—, —S—, —NR3—; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted; R2 is Ar2, Ar2C1-6alkyl, Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; L is a piperidine derivative of formula (a-1) or a spiro piperidine derivative of formula (a-2); Ar1 is phenyl or substituted phenyl; Ar2 is naphtalenyl; phenyl or substituted phenyl; and Het is a monocyclic or bicyclic heterocycle; each monocyclic and bicyclic heterocycle may optionally be substituted on a carbon atom; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: June 22, 1998Date of Patent: June 26, 2001Assignee: Janssen Pharmaceuticals N.V.Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck
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Patent number: 5985878Abstract: This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; m is 2 or 3 and n is 1, 2 or 3; wherein 1 or 2 C-atoms of the CH.sub.2 groups of the ##STR1## moiety which may also contain one double bond, may be substituted with C.sub.1-6 alkyl, amino, aminocarbonyl, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkyloxycarbony, C.sub.1-6 alkylcarbonylamino, hydroxy or C.sub.1-6 alkyloxy; and/or 2 C-atoms of said CH.sub.2 groups may be bridged with C.sub.2-4 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, amino, mono- or di(C.sub.1-6 alkyl)amino, Ar, ArNH--, C.sub.3-6 cycloalkyl, hydroxymethyl or benzyloxymethyl; R.sup.2 and R.sup.3 are hydrogen, or taken together may form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH--; in case X represents CH then L is a radical L.sup.1, L.sup.2 or L.sup.3 ; or in case X represents N then L is a radical L.Type: GrantFiled: July 9, 1998Date of Patent: November 16, 1999Assignee: Janssen Pharmaceuticals, N.V.Inventors: Raymond Antoine Stokbroekx, Marcel Jozef Maria Van der Aa, Marc Willems, Lieven Meerpoel, Marcel Gerebernus Maria Luyckx, Robert Tuman
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Patent number: 5369084Abstract: Isonicotinic acid derivatives and related furo-, thieno- and pyrrolo[3,4-c]pyridin-1(3H)-one, -thione and -imine compounds having the formula ##STR1## wherein R is ##STR2## Q is O, S or NR.sup.7 ; Y is O, S or NR.sup.8 ; L is COOR.sup.9, CONR.sup.10 R.sup.11, C(.dbd.S)NR.sup.10 R.sup.11, CN, or a radical of formula ##STR3## the acceptable addition salts, the stereochemically isomeric forms and the N-oxides thereof, having herbicidal properties, compositions containing the same and methods for controlling weeds.Type: GrantFiled: May 6, 1993Date of Patent: November 29, 1994Assignee: Janssen Pharmaceutical N.V.Inventors: Hans-Rudolf Waespe, Guy R. E. Van Lommen, Victor K. Sipido
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Patent number: RE37886Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, as substance-P antagonists; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: August 23, 2001Date of Patent: October 15, 2002Assignee: Janssen Pharmaceuticals, N.V.Inventors: Frans E. Janssens, François M. Sommen, Dominique L. N. G. Surleraux, Joseph E. Leenaerts, Yves E. M. Van Roosbroeck