Patents Represented by Attorney, Agent or Law Firm F. Aaron Dubberley
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Patent number: 7279305Abstract: A newly identified gene, DIS1 is disrupted by a (1;11)(q42.1;q14.3) translocation which segregates with schizophrenia. We have examined the genomic structure of DIS1 and found that the gene consists of 13 exons estimated to extend across at least 300 kb of DNA. Exon 11 contains an alternative splice site which removes 66 nucleotides from the open reading frame. The final intron of DIS1 belongs to the rare AT-AC class of introns. 8 expressed sequence tags (ESTs) located within introns 3, 7, 9 and 10 of DIS1 have also been identified. These ESTs have not yet been assigned to DIS1 and may therefore represent further novel genes in the region.Type: GrantFiled: November 28, 2000Date of Patent: October 9, 2007Assignee: N.V. OrganonInventors: David Porteous, Kirsty Millar, Douglas Blackwood, Walter John Muir
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Patent number: 7252934Abstract: Interaction of Rel proteins and steroid receptors is known to result in repression of target genes. Here we describe the discovery of a new mechanism in which Rel proteins and steroid receptors act synergistically to activate a regulatory element. This mechanism is shown to influence the expression of the brain-specific 5HT1A receptor wherein the estrogen receptor acts synergistically with the Nuclear Factor kappa B to enhance the activity of the promoter for the 5HT1A receptor gene. In addition, synergistic effects of Rel proteins with the mineralocorticoid receptor were observed, showing that synergism with Rel proteins may be expected for other steroid receptors as well. The synergism between Rel proteins and estrogen receptor or mineralocorticoid receptor provides a tool for the development of compounds that interact with the estrogen or mineralocorticoid receptor in such a way that only the synergistic effect is modulated whereas other effects are left intact.Type: GrantFiled: March 6, 2001Date of Patent: August 7, 2007Assignee: N.V. OrganonInventors: Christine J. C. Boersma, Paulus Theodorus Maria Van Der Saag, Sacha Wissink, Bart Van Der Burg
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Patent number: 7229789Abstract: A process is disclosed for releasing proteins from cells and/or inactivating viruses. In the process, a host cell containing a protein of interest is contacted with a solution of an effective amount of a detergent.Type: GrantFiled: January 19, 2001Date of Patent: June 12, 2007Assignee: N.V. OrganonInventor: Scot R. Shepard
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Patent number: 7223579Abstract: The invention relates to an isolated polynucleotide sequence comprising a nucleic acid sequence encoding the amino acid sequence of KshA protein or of KshB protein, encoded by nucleotides 499–1695 of SEQ ID NO: 1 or by nucleotides 387–1427 of SEQ ID NO:2, respectively, and functional homologues thereof. The polynucleotides of the invention can be used to construct genetically modified microorganisms blocked in 3-ketosteroid 9?-hydroxylase activity, which are useful in the microbial degradation of steroids to accumulate certain steroid products.Type: GrantFiled: February 19, 2003Date of Patent: May 29, 2007Assignee: N.V. OrganonInventors: Robert Van Der Geize, Peter Van Der Meijden, Gerda Hessels, Lubbert Dijkhuizen
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Patent number: 6818667Abstract: The present invention relates to novel compounds of the formula I in which R(1), R(2), R(3) and R(4) are, independently of each other, hydrogen or an alkyl radical. The compounds of the formula I are inhibitors of KDR kinase and, due to their antiangiogenic effect, are suitable for preventing and/or treating malignant diseases. The compounds of the formula I can be obtained by fermenting the microorganism Eurotium echinulatum Delacroix (DSM 13872) or by chemically derivatizing the compounds which are obtained after fermenting said microorganism. The invention consequently also relates to a process for preparing the compounds of the formula I, to the use of the compounds of the formula I for preparing a pharmaceutical for treating malignant diseases and diseases which can be treated by inhibiting KDR kinase, and also to pharmaceutical preparations which have a content of at least one compound of the formula I.Type: GrantFiled: June 26, 2002Date of Patent: November 16, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Claudia Eder, Herbert Kogler, Luigi Toti
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Patent number: 6818441Abstract: Improved vectors and related materials and methods are disclosed.Type: GrantFiled: June 16, 2000Date of Patent: November 16, 2004Assignees: Aventis Pharmaceuticals Inc., Ariad Pharmaceuticals Inc.Inventors: Trudy Grossman, Ian MacNeil, Paul R. August
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Patent number: 6777544Abstract: The present invention relates to PNA derivatives which carry, at the N terminus of the PNA backbone, a phosphoryl radical. The phosphoryl radical can be, for example, a phosphate radical, or a substituted phosphoryl radical, with substituted phosphoryl derivatives carrying, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the abovementioned PNA derivatives and to their use as pharmaceuticals and diagnostic agents.Type: GrantFiled: April 17, 2001Date of Patent: August 17, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Eugen Uhlmann, Gerhard Breipohl, David William Will
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Patent number: 6720153Abstract: This invention is directed to a bioassay for determining the functionality of parathyroid hormone compounds. More particularly, this invention is directed to a bioassay wherein the compound to be tested is added to a culture of parathyroid hormone receptor expressing cells bearing a reporter gene under the transcriptional control of multiple c-AMP responsive elements.Type: GrantFiled: August 31, 1999Date of Patent: April 13, 2004Assignee: Aventis Pharmaceuticals Inc.Inventors: Richard F. Labaudiniere, Kin T. Yu, Gregg R. Crumley, Clarence C. Morse
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Patent number: 6489479Abstract: The present invention is concerned with an improved process for the manufacture of mixed anhydrides. The process comprises adding an adjuvant base to a mixture of acid and reactive acid derivative. It is especially suitable for use in the synthesis of peptides and/or for the manufacture of pharmaceutically active substances or corresponding intermediates.Type: GrantFiled: July 22, 1999Date of Patent: December 3, 2002Assignee: Hoffman-La Roche Inc.Inventors: Martin Karpf, René Trussardi
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Patent number: 6479670Abstract: This invention relates to new selective retinoid acid receptor agonists of formula I wherein the symbols are as defined in the specification to their pharmaceutically acceptable salts, individual isomers or to a racemic or non-racemic mixture; to pharmaceutical compositions containing them, and to methods for their use as therapeutic agents.Type: GrantFiled: July 12, 2000Date of Patent: November 12, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Paula Nanette Belloni, Peter Mohr
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Patent number: 6462076Abstract: The present invention relates to beta-amino acid nitrile derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are cysteine protease inhibitors useful for the treatment of diseases associated with cysteine proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.Type: GrantFiled: June 1, 2001Date of Patent: October 8, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Tobias Gabriel, Michael Pech, Rosa Maria Rodriguez Sarmiento
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Patent number: 6458844Abstract: It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (I BD).Type: GrantFiled: May 23, 2001Date of Patent: October 1, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Kenneth Gregory Hull, Achytharao Sidduri, Jefferson Wright Tilley
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Patent number: 6447996Abstract: Polypeptides having galanin receptor activity, genetic material for expressing same, any recombinant cell expressing said polypeptides, and the use thereof, are disclosed.Type: GrantFiled: August 15, 1996Date of Patent: September 10, 2002Assignee: Aventis Pharma S.A.Inventors: Estelle Habert-Ortoli, Brigitte Amiranoff, Isabelle Loquet
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Patent number: 6441185Abstract: Improved process of compounds of formula III in which A denotes CH═CH or S W denotes O X denotes S, O or NR2 in which the residue R2 is hydrogen or C1-C6 alkyl, Y denotes CH or N R denotes naphthyl, thienyl or phenyl which is optionally monosubstituted or disubstituted with C1-C3 alkyl, CF3, C1-C3 alkoxy, F, Cl or bromine, R1 denotes hydrogen or C1-C6 alkyl and n denotes 1-3 by reducing a compound of the general formula IV, in which A, W, X, Y, R, R1 and n have the meanings stated above with activated aluminum in a protic solvent, as well as new compounds of formula III and pharmaceutical preparations containing these compounds.Type: GrantFiled: February 14, 2001Date of Patent: August 27, 2002Assignee: Roche Diagnostics GmbHInventors: Hans-Frieder Kühnle, Ernst-Christian Witte, Hans-Peter Wolff
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Patent number: 6419955Abstract: The present invention relates to a process for the preparation of bisphonate-containing pharmaceutical compositions for oral administration wherein the active substance is wet-granulated in a fluidized-bed granulator and the wet granulate is dried in the fluidised bed granulator. The dried granulate is further processed to produce desired dosage forms.Type: GrantFiled: October 7, 1999Date of Patent: July 16, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Rolf-Dieter Gabel, Jörn Möckel, Heinrich Woog
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Patent number: 6388071Abstract: Para-alkynyl phenyl heteroaromatic amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.Type: GrantFiled: April 25, 2001Date of Patent: May 14, 2002Assignee: Hoffmann-La Roche Inc.Inventor: Paige Erin Mahaney
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Patent number: 6388088Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.Type: GrantFiled: October 11, 2001Date of Patent: May 14, 2002Assignee: Hoffman-La Roche Inc.Inventor: Achyutharao Sidduri
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Patent number: 6388084Abstract: Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: November 21, 2000Date of Patent: May 14, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Gerald Lewis Kaplan, Achyutharao Sidduri, Jefferson Wright Tilley
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Patent number: 6369232Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.Type: GrantFiled: August 8, 2001Date of Patent: April 9, 2002Assignee: Hoffmann-La Roche Inc.Inventor: Achyutharao Sidduri
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Patent number: D551759Type: GrantFiled: November 3, 2005Date of Patent: September 25, 2007Assignee: N. V. OrganonInventors: Maurice Petrus Wilhelmus Tak, Iris Epkjen Hobo-V. D. Graaf