Patents Represented by Attorney Gabriel Lopez
-
Patent number: 7049324Abstract: a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(?O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; ?Z1—Z2?Z3— represents a radical of formula ?N—N?CH— (a-1), ?N—CH?N— (a-2), ?CH—N?N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(?O), C(?S), or a direct bond, R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyType: GrantFiled: November 15, 2000Date of Patent: May 23, 2006Inventors: Ashis Kumar Saha, David William End, Bart Lieven Daniel De Corte, Henry Joseph Breslin, Li Liu
-
Patent number: 6987110Abstract: The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: GrantFiled: June 4, 2003Date of Patent: January 17, 2006Assignee: Janssen Pharmaceutica N.V.Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, Hong Ye, Bruce R. Conway, Keith Demarest
-
Patent number: 6960597Abstract: The invention is directed to aza-bridged-bicyclic compounds having Formula (I): and pharmaceutically acceptable salts thereof. The compounds are useful (?4 integrin receptor antagonists and, in particular, ?4?1 and ?4?7 integrin receptor antagonists. The invention is further directed to methods for use of the instant compounds for treating integrin mediated disorders including, but not limited to, inflammatory disorders, autoimmune disorders and cell-proliferative disorders, methods for preparing the compounds and methods for preparing the intermediates, derivatives and pharmaceutical compositions thereof.Type: GrantFiled: June 26, 2001Date of Patent: November 1, 2005Assignee: Orth-McNeil Pharmaceutical, Inc.Inventors: Alexey B. Dyatkin, Bruce E. Maryanoff, William J. Hoekstra, Wei He, William A. Kinney
-
Patent number: 6951857Abstract: The present invention is concerned with the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p represents 0, 1, 2 or 3; q represents 0, 1, 2, 3 or 4; R1 represents hydrogen, C1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, mercapto, C1-6alkylthio, C3-7cycloalkyl, aryl or C1-6alkyl substituted with mono- or di(C1-6alkyl)amino, C1-6alkyloxy, aryl or Het; R2 represents cyano or a radical of formula —C(?X)—Y—R5; wherein X represents O or S; Y represents O, S, NR6 or a direct bond; R5 represents hydrogen; C3-7cycloalkyl; aryl or optionally substituted C1-6alkyl; and where Y is a direct bond, R5 may also be halo or Het; R3 and R4 each independently represents halo, haloC1-6alkyl, C1-6alkyl, hydroxy, C1-6alkyloxy, C1-6alkylcarbonyloxy, mercapto, C1-6alkylthio, C1-6alkylsulfonyl, C1-6alkylsulfinyl, haloC1-6alkylsulfonyl, aryl, cyano, nitro, amino, mono- and di(C1-6alkyl)amino or (C1-6alkylcarbonyl)amino; aryl repreType: GrantFiled: May 9, 2003Date of Patent: October 4, 2005Inventors: Eddy Jean Edgard Freyne, Gustaaf Maria Boeckx, Jean Pierre Frans Van Wauwe, Gaston Stanislas Marcella Diels
-
Patent number: 6943149Abstract: The invention is directed to novel benzimidazolone peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted benzimidazolone peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.Type: GrantFiled: March 17, 2003Date of Patent: September 13, 2005Assignees: Ortho McNeil Pharmaceutical, Inc., Millennium Pharmaceuticals, Inc.Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly B. White
-
Patent number: 6936604Abstract: The invention is directed to bridged bicyclic amino acid-derived [1,4]benzodiazepine compounds, intermediates and pharmaceutical compositions thereof useful as vasopressin receptor antagonists and methods for treating vasopressin mediated disorders.Type: GrantFiled: October 11, 2002Date of Patent: August 30, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Alexey B. Dyatkin, William J. Hoekstra, Bruce E. Maryanoff
-
Patent number: 6894046Abstract: The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 4; X is O, S, NR5 or a direct bond; Y is O, S, NR5 or S(O)2; R1 independently is C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is Het1, C3-7cycloalkyl or optionally substituted C1-6alkyl and if X is O, S or NR5, then R2 may also represent aminocarbonyl, aminothiocarbonyl, C1-4alkylcarbonyl, C1-4alkylthiocarbonyl, arylcarbonyl, arylthiocarbonyl, Het1carbonyl or Het1thiocarbonyl; R3 and R4 independently are hydrogen, C1-6alkyl or C3-7cycloalkyl; R3 and R4 form a C2-6alkanediyl; R5 is hydrogen or C1-4alkyl; R6 is a sulfonyl or sulfinyl derivative; R7 and R8 are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, —Y—C1-4alkanediyl-C(?O)—O—RType: GrantFiled: March 19, 2001Date of Patent: May 17, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy Jean Edgard Freyne, Jean Fernand Armand Lacrampe, Frederik Dirk Deroose, Marc Gaston Venet
-
Patent number: 6867207Abstract: The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, p and q are 0, 1, 2, 3 or 4 and q is also 5; X is O, S, NR3 or a direct bond; R1 is hydrogen, hydroxy, halo, optionally substituted amino, optionally substituted C1-6alkyl, C1-6alkyloxy, C3-7cycloalkyl or aryl; R2 is aryl, Het1, C3-7cycloalkyl, optionally substituted C1-6alkyl; and if X is O, S or NR3, then R2 may also be a carbonyl or thiocarbonyl linked substituent; R3 is hydrogen or C1-4alkyl; R4 and R5 independently are optionally substituted C1-6alkyl, halo, hydroxy, mercapto, C1-6alkyloxy, C1-6akylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6 or NR7R8; R6 is substituted sulfonyl or sulfinyl; R7 and R8 are hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R9 and R10 are each independently selected from hydrogen, optionally substituted C1-4alkyType: GrantFiled: June 26, 2001Date of Patent: March 15, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Jean Fernand Armand Lacrampe, Eddy Jean Edgard Freyne, Marc Gaston Venet, Gustaaf Maria Boeckx
-
Patent number: 6844459Abstract: Pharmaceutical compositions comprising a cyclosporin in a novel galenic formulations for oral administration. The compositions typically comprise a cyclosporin, 1,2-propylene glycol, a mixed mono-, di- and tri-glyceride and a hydrophilic surfactant. Further a refined glycerol-transesterified corn oil is provided representing a mixed mono-, di- and tri-glyceride suitable for the novel formulation. Dosage forms include in particular oral dosage forms.Type: GrantFiled: May 20, 2003Date of Patent: January 18, 2005Assignee: Novartis AGInventors: Birgit Hauer, Armin Meinzer, Ulrich Posanski, Jacky Vonderscher
-
Patent number: 6838467Abstract: This invention relates to a method of treatment and dosing regimen for treating mammalian tumors by the discontinuous administration of a farnesyl transferase inhibitor over an abbreviated one to five day dosing schedule.Type: GrantFiled: February 20, 2001Date of Patent: January 4, 2005Assignee: Janssen Pharmaceutica N. V.Inventor: David William End
-
Patent number: 6803364Abstract: The present invention is concerned with the compounds of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein p is 0 to 4; q is 0 to 5; X is O, S, NR3 or a direct bond; or —X—R2 is CN; R1 is H, OH, halo, NH2, mono- or di(C1-4alkyl)NH2, C1-6alkyl, C1-6alkylO, C3-7cycloalkyl, aryl, arylC1-6alkyl, NH2C1-4akyl, mono- or di(C1-4alkyl)NH2C1-4akyl or mono- or di(C1-4alkyl)NH2C1-4alkylNH2; R2 is aryl, Het1, optionally substituted C3-7cycloalkyl, optionally substituted C1-6alkyl; R3 is H or C1-4alkyl; R4 and R5 are —C(═O)—Z—R14, C1-6alkyl, halo, polyhaloC1-6alkyl, OH, mercapto, C1-6alkylO, C1-6alkylthio, C1-6alkylC(═O)O, aryl, cyano, nitro, Het3, R6, NR7R8 or C1-4alkyl substituted with —C(═O)—Z—R14, Het3, R6 or NR7R8; Z is O, S, NH, —CH2O or —CH2—S—; R14 is H, C1-20acyl, optionally substituted C1-20alkyl, optionally substituted C3-20alkenyl, C3-2Type: GrantFiled: August 29, 2001Date of Patent: October 12, 2004Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy Jean Edgard Freyne, Frederik Dirk Deroose, Jean Fernand Armand Lacrampe, Werner Constant Johan Embrechts, Jerome Michel Claude Fortin
-
Patent number: 6740753Abstract: A novel crystal form the pharmaceutical compound olanzapine, processes for its preparation and its pharmaceutical use are disclosed.Type: GrantFiled: December 19, 2001Date of Patent: May 25, 2004Assignee: Geneva Pharmaceuticals, Inc.Inventors: Julian Davies, James Edward Gano
-
Patent number: 6723339Abstract: The present invention provides a hard gelatine capsule containing a pharmaceutical composition comprising cyclosporin A in a mixture with a surfactant of HLB value at least 10, substantially free of any oil and when a hydrophilic phase is present, the hydrophilic phase being a polyethylene glycol and/or a lower alkanol provided that any lower alkanol present is present in less than 12% of the total weight of the composition absent the hard gelatine capsule.Type: GrantFiled: November 6, 2001Date of Patent: April 20, 2004Assignee: Novartis AGInventors: Armin Meinzer, Barbara Haeberlin
-
Patent number: 6723831Abstract: Polyamide conjugates comprising either (a) a xenoantigenic group; or (b) a biologically active group and a macromolecular, macro- or microscopic entity; bound to a polyamide backbone, processes for their preparation and the use of these conjugates in therapeutic compositions.Type: GrantFiled: April 16, 2002Date of Patent: April 20, 2004Assignee: Novartis AGInventors: Rudolf Duthaler, Andreas Katopodis, Willy Kinzy, Reinhold Öhrlein, Gebhard Thoma
-
Patent number: 6713305Abstract: There are provided membrane-associated polypeptides having the sequence shown in SEQ ID Nos. 1 and 9. Also provided are immunogenic determinants derived from said polypeptides and antibodies raised thereto. The polypeptides, their derived antigenic determinants and the antibodies are useful for the diagnosis and treatment of metastatic potential in tumors.Type: GrantFiled: October 23, 1998Date of Patent: March 30, 2004Assignee: Novartis AGInventors: Felix Bachmann, Max M. Burger
-
Patent number: 6703372Abstract: Azithromycin in the form of a stable monohydrate and processes for the preparation of azithromycin in the form of an, e.g. stable, monohydrate.Type: GrantFiled: December 18, 2001Date of Patent: March 9, 2004Assignee: Biochemie S.A.Inventors: Victor Centellas, Rafael Garcia, Marta Poch, José Diago, Johannes Ludescher, Immaculada Bosch
-
Patent number: 6693095Abstract: A compound of formula wherein W, V, R1, R5, R2, R3 and R4 have various meanings, a process for their production and their use as a pharmaceutical.Type: GrantFiled: November 13, 2001Date of Patent: February 17, 2004Assignee: Biochemie Gesellschaft m.b.H.Inventors: Gerd Ascher, Josef Wieser, Michael Schranz, Johannes Ludescher, Johannes Hildebrandt
-
Patent number: 6635745Abstract: Monoclonal antibodies to rapamycin and to 40-O-alkylated derivatives of rapamycin are provided, together with novel haptens, immunogenic conjugates, and processes for making them and assay kits for using them.Type: GrantFiled: January 9, 2001Date of Patent: October 21, 2003Assignee: Novartis AGInventors: Richard Sedrani, Valérie Quesniaux Ryffel
-
Patent number: 6623753Abstract: The invention concerns liposomal preparations comprising as the active agent a compound of formula I in free base form or in acid addition salt form. It also concerns a method of preparation of such liposomal preparations by encapsulating a compound of formula I with an appropriate liposome forming material, a corresponding pharmaceutical compositions, and methods of treatment of systemic, topical and pulmonal fungal infections.Type: GrantFiled: June 24, 1997Date of Patent: September 23, 2003Assignee: Novartis AGInventors: David Bodmer, Thomas Kissel, Friedrich Richter, Harry Tiemessen
-
Patent number: 6620325Abstract: This invention provides a process for purifying a cyclosporin, e.g. cyclosporin A, or a macrolide, to a high degree of purity on a large scale. In another aspect this invention provides a bulk quantity of cyclosporin A with an impurity level of less than about 0.7%, e.g. about 0.5%, and compositions thereof.Type: GrantFiled: October 29, 2001Date of Patent: September 16, 2003Assignee: Novartis AGInventors: Peter Fuenfschilling, Berthold Schenkel