The Additional Chalcogen Is Bonded Directly At The 3-position Of The Bicyclo Ring System Patents (Class 540/507)
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Publication number: 20120196851Abstract: The present invention relates to known and novel compounds of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.Type: ApplicationFiled: October 6, 2010Publication date: August 2, 2012Applicant: SIENA BIOTECH S.P.A.Inventors: Maurizio Varrone, Arianna Nencini, Joanna Margaret Quinn, Andrea Caricasole, Annette Cornelia Bakker, Giovanni Gaviraghi, Massimilano Salerno
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Publication number: 20100160299Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.Type: ApplicationFiled: September 30, 2009Publication date: June 24, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: James R. Baker, JR., Xue-min Cheng, Abraham F.L. Van Der Spek, Baohua Mark Huang, Thommey P. Thomas
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Patent number: 7390801Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: May 12, 2006Date of Patent: June 24, 2008Assignees: Athena Neurosciences, Inc., Eli Lilly and CompanyInventors: Eugene D. Thorsett, Michael A. Pleiss, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Bruce A. Dressman, James J. Droste, Steven S. Henry, Russell D. Stucky, Warren J. Porter
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Patent number: 7250410Abstract: The invention concerns novel benzodiazepine derivatives and their uses in the field of therapeutics particularly for treating pathologies involving the activity of a cyclic nucleotide phosphodiesterase. It also concerns methods for preparing them and novel synthesis intermediates.Type: GrantFiled: June 7, 2002Date of Patent: July 31, 2007Assignee: Via Pharmaceuticals, Inc.Inventors: Jean-Jacques Bourguignon, Yan Lagouge, Claire Lugnier, Eveline Klotz, Jean-Paul Macher, Pierre Raboisson, Dominique Schultz
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Patent number: 7029918Abstract: A water-soluble reference standard is useful for immunoassays of a lipophilic drugs. The reference standard is a compound of formula (I): G-(L)n—Y;??(I) where G is a lipophilic drug; L is a linker which is an alkyl group or heteroalkyl group containing from 1 to 20 carbon atoms; n is 0 or 1; and Y is a water-solubilizing group such as —SO3?, —NR—SO3?, —P(?O)(OH)(O?), or —O—P(?O)(OH)(O?); where R is H or an alkyl group of 1 to 10 carbon atoms.Type: GrantFiled: January 25, 2002Date of Patent: April 18, 2006Assignee: Roche Diagnostics Operations, Inc.Inventors: Min Li, Robert S. Wu, Jane S. C. Tsai
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Publication number: 20040220179Abstract: The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions.Type: ApplicationFiled: April 21, 2004Publication date: November 4, 2004Inventors: Tianbao Lu, Karen L. Milkiewicz, Pierre Raboisson, Maxwell David Cummings, Raul R. Calvo, Daniel J. Parks, Louis V. Lafrance, Juan Jose Marugan Sanchez, Joan Gushue, Kristi Leonard
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Patent number: 6686350Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.Type: GrantFiled: January 25, 1999Date of Patent: February 3, 2004Assignee: Biogen, Inc.Inventors: Zhongli Zheng, Carol L. Ensinger, Steven P. Adams
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Patent number: 6492553Abstract: A method for preparing a N-[(aliphatic or aromatic)carbonyl)]-2-aminoacetamide compound, and for preparing a cyclized compound therefrom, as well as novel resin bound intermediate compounds that are useful for preparing such compounds.Type: GrantFiled: August 4, 1999Date of Patent: December 10, 2002Assignee: Aventis Pharamaceuticals Inc.Inventors: Christopher Hulme, George C. Morton, Joseph M. Salvino, Richard F. Labaudiniere, Helen J. Mason, Matthew M. Morrissette, Liang Ma, Marie-Pierre Cherrier
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Patent number: 6462037Abstract: The present invention relates to 1,4-benzodiazepin-2-ones of Formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: May 25, 2000Date of Patent: October 8, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: James D. Rodgers, Barry L. Johnson, Haisheng Wang
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Patent number: 6350870Abstract: The present invention provides a process for preparing crystalline lorazepam substantially free of bound solvent from a lorazepam alcohol solvate or hydrate by suspending the lorazepam solvate in an organic medium selected from ethyl acetate, cyclohexane, dichloromethane, toluene and mixtures thereof. This process is useful in producing the anti-anxiety and sedative agent lorazepam in increased yields. A process for converting lorazepam lower alcohol solvates to lorazepam hydrate is also disclosed.Type: GrantFiled: March 5, 2001Date of Patent: February 26, 2002Assignee: Teva Pharmaceutical Industreis, Ltd.Inventor: Igor Lifshitz
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Patent number: 6255479Abstract: A method for preparing an &agr;-oxolactam comprising, reacting a corresponding &agr;-diazolactam with an oxygen donor, in the presence of a transition metal catalyst, to yield the corresponding &agr;-oxolactam.Type: GrantFiled: December 29, 1998Date of Patent: July 3, 2001Assignee: Research Corporation Technologies, Inc.Inventors: John D. Buynak, Akireddy Srinivasa Rao
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Patent number: 6121258Abstract: The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: August 26, 1997Date of Patent: September 19, 2000Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Neil Gregory Almstead, Rimma Sandler Bradley, Kelly Lynn McDow-Dunham, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo, Thomas Lee Cupps
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Patent number: 6100254Abstract: Disclosed herein are small molecule, non-peptidyl inhibitors of protein tyrosine kinases, and methods for their use. The instant inhibitors are based on a 1,4-benzodiazepin-2-one nucleus. Methods are provided for inhibition of specific protein tyrosine kinases, for example pp60.sup.c-src. Methods are further provided for the use of these inhibitors in situations where the inhibition of a protein tyrosine kinase is indicated, for example, in the treatment of certain diseases in mammals, including humans.Type: GrantFiled: October 10, 1997Date of Patent: August 8, 2000Assignees: Board of Regents, The University of Texas System, The Regents of the University of CaliforniaInventors: Raymond J. A. Budde, Jonathan A. Ellman, Victor A. Levin, Gary E. Gallick, Robert A. Newman
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Patent number: 6015791Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole, and triazoles, in particular those including a cycloheptane structure, that are useful as serine protease inhibitors, including inhibitors for human neutrophil elastase. Compounds of the invention are useful in treating conditions such as adult respiratory distress syndrome, septic shock, and multiple organ failure.Type: GrantFiled: December 4, 1997Date of Patent: January 18, 2000Assignee: Cortech Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5662911Abstract: Benzodiazepine protein conjugates of the formula I ##STR1## wherein R1 is hydrogen, a methyl group or R, R2 is hydrogen, a hydroxyl or an OR group, with R1 or R2 containing an R group,R3 is a halogen, NO2 or NH2,X is hydrogen or a halogen,wherein R is a group of the formula II, wherein Z is a macromolecular immunogen reactive carrier substance and n is 2 or 3.The benzodiazepine protein conjugates are used as immunogens to obtain antibodies to benzodiazepines.The invention also relates to an immunoassay for the detection of benzodiazepines where the so generated antibodies are used.Type: GrantFiled: January 24, 1996Date of Patent: September 2, 1997Assignee: Boehringer Mannheim GmbHInventors: Erasmus Huber, Christian Klein, Hans-Peter Josel, Bruno Zink
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Patent number: 5597922Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a compound which has high binding to the glycine receptor.Type: GrantFiled: July 29, 1994Date of Patent: January 28, 1997Assignees: State of Oregon, Acting by and through the Oregon State Board of Higher Education, Acting for and on Behalf of the Oregon Health Sciences University and the University of Oregon, Acea Pharmaceuticals, Inc., The Regents of the University of CaliforniaInventors: Sui X. Cai, John F. W. Keana, Eckard Weber
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Patent number: 5302715Abstract: The present invention is directed to novel benzodiazepine derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to the benzodiazepine metabolites. The resulting novel antigens may be used for the production of antibodies or receptors using standard methods. Once generated, the antibodies or receptors and the novel derivatives which are covalently attached to proteins, polypeptides or labels may be used in the immunoassay process.Type: GrantFiled: April 6, 1992Date of Patent: April 12, 1994Assignee: Biosite Diagnostics, Inc.Inventors: Kenneth F. Buechler, Joseph B. Noar
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Patent number: 5175159Abstract: Compounds of Formula I are antagonists of oxytocin and are useful in the treatment of preterm labor and dysmenorrhea, and for stoppage of labor prepatory to Caesarean delivery.Type: GrantFiled: December 28, 1990Date of Patent: December 29, 1992Assignee: Merck & Co., Inc.Inventors: Mark G. Bock, Ben E. Evans, Roger M. Freidinger
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Patent number: 4820834Abstract: Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).Type: GrantFiled: March 16, 1987Date of Patent: April 11, 1989Assignee: Merck & Co., Inc.Inventors: Ben E. Evans, Roger M. Freidinger, Mark G. Bock
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Patent number: 4808605Abstract: Compounds of the formula ##STR1## wherein R is lower-alkyl, R.sup.1 is halogen, R.sup.2 is C.sub.1 -C.sub.12 -alkyl, R.sup.3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy, lower-alkoxy-lower-alkylcarbonoyloxy, lower-alkylaminocarbonyloxy, arylaminocarbonyloxy or aryl-lower alkylaminocarbonyloxy, X is C.sub.1 -C.sub.18 -alkylene which optionally can be interrupted by 1,4-phenylene or interrupted or lengthened by 1,4-cyclohexylene, A is di- or tri-substituted 2-imidazolyl attached via an ethylene group or a substituted or unsubstituted heterocycle selected from the group consisting of benzimidazolyl, benzimidazolonyl, imidazo[4,5-c]pyridinyl, imidazo[4,5-c]pyridinonyl, benzthiazolyl, benzodiazepine-2,5-dion-1-yl and pyrrolo[2,1-c]-[1,4]benzodiazepine-5,11-dion-10-yl and n is the number 0 or 1, in the form of racemates and optical antipodes, as well as N-oxides and pharmaceutically usable acid addition salts thereof.Type: GrantFiled: November 10, 1987Date of Patent: February 28, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Roland Jaunin, Hans P. Maki, Franzi Marti, Henri Ramuz
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Patent number: 4777169Abstract: Benzodiazepine derivatives useful in immunoassays for benzodiazepines.Type: GrantFiled: November 6, 1987Date of Patent: October 11, 1988Assignee: Hoffmann-La Roche Inc.Inventors: James V. Earley, Norman W. Gilman