Plural Ring Nitrogens In The Seven-membered Hetero Ring Patents (Class 514/211.08)
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Publication number: 20120252785Abstract: The present invention relates to the use of staurosporines derivatives for the preparation of a drug for the treatment of diseases involving deregulated FLT3 receptor tyrosine kinase activity, especially for the curative and/or prophylactic treatment of leukemias and myelodysplastic syndromes, and to a method of treating diseases involving deregulated FLT3 receptor tyrosine kinase activity.Type: ApplicationFiled: June 15, 2012Publication date: October 4, 2012Applicant: NOVARTIS AGInventors: James Douglas GRIFFIN, Paul William MANLEY
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Publication number: 20120238546Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula (I): Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula (I).Type: ApplicationFiled: June 15, 2010Publication date: September 20, 2012Inventors: Zhaoning Zhu, Xianhai Huang, Anandan Palani, William J. Greenlee, Robert G. Aslanian
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Patent number: 8263586Abstract: The present invention is directed to oxo bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: GrantFiled: May 14, 2008Date of Patent: September 11, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher D. Cox, David B. Whitman
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Publication number: 20120202789Abstract: The present invention relates to the use of specific compounds related to the indolocarbazole K252a, for the preparation of pharmaceutical compositions for the treatment of various forms of cancer.Type: ApplicationFiled: September 2, 2011Publication date: August 9, 2012Applicant: TAUTATIS, INC.Inventor: Hanno Roder
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Patent number: 8236790Abstract: Compounds of formula (I): wherein: R1 and R2, which may be the same or different, each represent a hydrogen or halogen atom or an alkyl, alkoxy, alkylthio, acyl, alkoxycarbonyl, carboxy, hydroxy, hydroxyalkyl, cyano, nitro, amino, substituted or unsubstituted aminocarbonyl, aminosulphonyl, alkylsulphonylaminoalkyl, N-hydroxy-carboximidamide or benzyloxy group, R3 represents a hydrogen atom or an alkyl, cycloalkyl or cycloalkylalkyl group, R4 represents a hydrogen atom or a substituted or unsubstituted alkyl group Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator and/or an NMDA receptor antagonist.Type: GrantFiled: March 19, 2010Date of Patent: August 7, 2012Assignee: Les Laboratories ServierInventors: Alexis Cordi, Patrice Desos, Pierre Lestage, Laurence Danober
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Publication number: 20120190667Abstract: A process for preparing solid dispersions of highly crystalline compounds. The highly crystalline or thermally labile therapeutic compounds are processed in an extruder in combination with a solubilizing agent and optionally a plasticizer. The resulting extrudate features the therapeutic compound in an amorphous state. Particularly useful as the solubilizing agents are surfactants such as poloxamers.Type: ApplicationFiled: March 19, 2012Publication date: July 26, 2012Inventors: Indrajit Ghogh, Jennifer Snyder, Wei-Qin Tong, Sudha Vippagunta
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Patent number: 8222244Abstract: The present invention relates to the use of staurosporines derivatives for the preparation of a drug for the treatment of diseases involving deregulated FLT3 receptor tyrosine kinase activity, especially for the curative and/or prophylactic treatment of leukemias and myelodysplastic syndromes, and to a method of treating diseases involving deregulated FLT3 receptor tyrosine kinase activity.Type: GrantFiled: May 17, 2011Date of Patent: July 17, 2012Assignees: Novartis AG, Dana-Farber Cancer Institute Inc.Inventors: James D Griffin, Paul W Manley
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Publication number: 20120157399Abstract: Provided herein are methods of utilizing bile acid transport inhibitors for the treatment of obesity and diabetes.Type: ApplicationFiled: February 22, 2012Publication date: June 21, 2012Applicant: Satiogen Pharmaceuticals, Inc.Inventors: Andrew A. Young, Bronislava Gedulin, Howard E. Greene
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Publication number: 20120157441Abstract: The present invention relates to the treatment of KIT dependent diseases that are characterized by a mutant form of KIT whereby the mutant KIT is identified and an appropriate inhibitor of the mutant KIT selected form midostaurin, vatalanib and compound A is administered.Type: ApplicationFiled: January 25, 2012Publication date: June 21, 2012Inventors: Elisabeth Buchdunger, Doriano Fabbro
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Publication number: 20120149685Abstract: The present invention refers to the use of a specific indolocarbazole compound of general formula (1) or a pharmaceutically-acceptable a salt thereof for the preparation of a pharmaceutical composition for the prevention or treatment of a neurode-generative and/or dementing illness driven by the molecular pathology of microtubule-associate tau such as Alzheimer's disease, frontal lobe dementia, Pick's disease, Parkinson disease with dementia, corticobasal degeneration, argyrophilic grains disease, or supranuclear palsy. A method for treating or preventing such illnesses is also disclosed. Furthermore, methods for the identification of efficacious inhibitors of neurofibrillary degeneration, and methods for the determination of an appropriate dosage of an inhibitor of the PHF-type tau hyperphosphorylation for the treatment of a condition characterized by neurofibrillary pathology are described.Type: ApplicationFiled: July 19, 2011Publication date: June 14, 2012Applicant: Tautatis, Inc.Inventor: Hanno RODER
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Publication number: 20120149765Abstract: The invention relates to the utilization of a substance for diagnostic determination of sgk1 (serum and glucocorticoid dependent kinase 1) and to the utilization of an active agent in order to influence sgk1 for therapeutic treatment of diseases associated with disordered activity of the tissue factor and to a diagnostic kit related to such substances or such active agents.Type: ApplicationFiled: December 9, 2011Publication date: June 14, 2012Inventor: Florian Lang
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Patent number: 8198435Abstract: The invention relates to a new crystalline form II of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of crystalline form II of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the amorphous forms of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.Type: GrantFiled: November 3, 2005Date of Patent: June 12, 2012Assignee: Novartis AGInventors: Pascale Hoehn, Bernd Koch, Michael Mutz
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Publication number: 20120129833Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of diabetes, obesity, hyperlipidaemia, fatty livers and of disorders of the cardiovascular system.Type: ApplicationFiled: August 19, 2011Publication date: May 24, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ningshu LIU, Kai Thede, Philip Lienau, Arne Scholz, Maher Najjar, Ulf Bomer, Knut Eis, Reiner Fischer
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Publication number: 20120130144Abstract: In one aspect, the present invention provides a method of treating lung cancer, comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor. In another aspect, the present invention provides a method of treating non-small cell lung cancer comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor.Type: ApplicationFiled: February 4, 2010Publication date: May 24, 2012Applicant: BiPar Sciences, Inc.Inventors: Barry M. Sherman, Charles Bradley, Valeria S. Ossovskaya
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Publication number: 20120121684Abstract: Implantable medical devices are disclosed. The devices comprise a coating comprising an interpenetrating network or semi-interpenetrating network. The interpenetrating network or semi-interpenetrating network comprises poly(ethylene glycol) and an aliphatic polyester copolymer. A method of using the implantable device is also provided.Type: ApplicationFiled: January 23, 2012Publication date: May 17, 2012Applicant: Abbott Cardiovascular Systems Inc.Inventors: Mikael Trollsas, Florencia Lim, Syed F.A. Hossainy
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Publication number: 20120114636Abstract: Methods are disclosed for predicting a patient response to anti-Her2 therapy or anti-aromatase therapy. In certain embodiments, the methods involve the identification of low molecular weight cyclin E (LMW-E) in cancers, such as breast cancer cells, as a predictive and prognostic marker. In further embodiments, LMW-E expression by a cancerous or pre-cancerous cell may be used to predict response to an aromatase inhibitor and/or CDK2 inhibitor, and determination of LMW-E expression may be used in the personalization of cancer therapies.Type: ApplicationFiled: March 10, 2010Publication date: May 10, 2012Applicants: The Board of Regents of the University of Texas System, Research Development FoundationInventors: Khandan Keyomarsi, Nikki Delk, Kelly K. Hunt, Hannah Wingate, Elizabeth A. Mittendorf
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Publication number: 20120114663Abstract: Disclosed are methods to treat allergic conditions, including pulmonary and non-pulmonary conditions, in a subject by administering a composition that inhibits Pim kinase. Also disclosed are methods to treat allergic conditions in a subject by administering a composition that induces expression of Runx3.Type: ApplicationFiled: November 10, 2011Publication date: May 10, 2012Applicant: NATIONAL JEWISH HEALTHInventors: Erwin W. Gelfand, Meiqin Wang
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Publication number: 20120114588Abstract: The present invention regards specific IBAT inhibitors with improved effect in prophylaxis and treatment of metabolic syndrome, obesity, disorders of fatty acid metabolism, glucose utilization disorders, disorders in which insulin resistance is involved, diabetes mellitus, type 1 and type 2 diabetes. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.Type: ApplicationFiled: May 26, 2011Publication date: May 10, 2012Applicant: ALBIREO ABInventors: Ingemar Starke, Hans Graffner, Per-Göran Gillberg, Ann-Margret Lindqvist, Bo Angelin
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Patent number: 8168566Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.Type: GrantFiled: January 31, 2011Date of Patent: May 1, 2012Assignee: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Ernst Rudolf F. Gesing, Dieter Feucht, Karl-Heinz Kuck, Peter Lösel, Olga Malsam, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne
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Patent number: 8148362Abstract: The invention provides a novel oxazolidinone derivative represented by the formula (I): wherein Ring A is optionally substituted or fused and represents (A-1) at least 7-membered monocyclic hetero ring containing at least three N atoms; (A-2) at least 6-membered monocyclic hetero ring containing at least two N atoms and at least one O atom; or (A-3) at least 7-membered monocyclic hetero ring containing at least two N atoms and at least one S atom; X1 is a single bond, —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SO2NR5—, and —NR6SO2— (wherein R2-R6 are independently hydrogen or lower alkyl), or lower alkylene or lower alkenylene in which one of the preceding groups may intervene; Ring B is optionally substituted carbocycle or optionally substituted heterocycle; R1 is hydrogen, or an organic residue which is able to bind to the 5-position of oxazolidinone ring in oxazolidinone antimicrobial agent, and an antibacterial agent containing the same.Type: GrantFiled: March 30, 2007Date of Patent: April 3, 2012Assignees: Research Foundation Itsuu Laboratory, Shionogi & Co., Ltd.Inventors: Hideyuki Suzuki, Shoji Hizatate, Iwao Utsunomiya, Koichi Shudo
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Publication number: 20120070410Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: ApplicationFiled: November 5, 2009Publication date: March 22, 2012Inventors: Julius L. Apuy, Darren E. Insko, Joyce J. James
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Patent number: 8138168Abstract: The invention relates to compounds having the formulae: wherein the variables are as defined herein. The invention further relates to methods of making and using these compounds, and pharmaceutical compositions, kits and articles of manufacture comprise the compounds.Type: GrantFiled: September 26, 2008Date of Patent: March 20, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Benjamin Jones, Stephen W. Kaldor, Walter Keung, Andre A. Kiryanov, Zhe Li, Jeffrey A. Stafford, John Tyhonas, Craig Behnke
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Publication number: 20120058954Abstract: The invention relates generally to optical agents, including phototherapeutic agents, for biomedical applications, including phototherapy. The invention includes optical agents, and related therapeutic methods, comprising alicyclic diaza compounds, including 1,2 diaza heterocyclic compounds, having a photolabile N—N bond directly or indirectly linked to at least one carbocyclic aromatic and/or heterocyclic aromatic group. In some embodiments, for example, the invention provides alicyclic diaza compounds for phototherapeutic methods having a photolabile N—N bond that undergoes photoactivated cleavage to produce reactive species, such as radicals, ions, etc., that achieve a desired therapeutic effect, such as selective and/or localized tissue damage and/or cell death.Type: ApplicationFiled: May 12, 2010Publication date: March 8, 2012Inventor: Raghavan Rajagopalan
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Publication number: 20120046242Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.Type: ApplicationFiled: December 21, 2009Publication date: February 23, 2012Applicants: MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTONInventors: Randall T. Moon, Travis L. BIechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
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Patent number: 8119566Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.Type: GrantFiled: August 2, 2004Date of Patent: February 21, 2012Assignee: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Ernst Rudolf F. Gesing, Dieter Feucht, Karl-Heinz Kuck, Peter Lösel, Olga Malsam, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne
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Publication number: 20120039805Abstract: The invention provides diagnostic and therapeutic methods for neoplastic disease patients with neoplasms of for example, the breast, skin, kidney, lung, pancreas, rectum and colon, prostate, bladder, epithelial, non-epithelial; lymphomas, sarcomas, melanomas, and the like, comprising determining the level of caveolin-1 and/or caveolin-2 in stromal cells adjacent to a neoplasm.Type: ApplicationFiled: February 19, 2010Publication date: February 16, 2012Inventors: Michael P. Lisanti, Federica Sotgia, Richard G. Pestell
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Publication number: 20120040963Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.Type: ApplicationFiled: January 31, 2011Publication date: February 16, 2012Applicant: Bayer CropScience AGInventors: Reiner FISCHER, Thomas BRETSCHNEIDER, Ernst Rudolf F. GESING, Dieter FEUCHT, Karl-Heinz KUCK, Peter LÖSEL, Olga MALSAM, Christian ARNOLD, Thomas AULER, Martin Jeffrey HILLS, Heinz KEHNE
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Patent number: 8114865Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer formula (I).Type: GrantFiled: December 14, 2007Date of Patent: February 14, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Marcella Nesi, Ettore Perrone, Roberto Bossi, Paolo Polucci
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Publication number: 20110311451Abstract: The present invention relates to a process for the preparation of polymer conjugates of i?dolocarbazole compounds, in particular of polymer conjugates of K-252a and derivatives thereof, by a synthetic route which results in a highly pure product, with a high product yield. In a further aspect the present invention relates to novel polymer conjugates of K-252a and derivatives thereof, wherein the chemical group linking the polymer unity to the K-252a or to the K-252a derivative compound is characterised by a 5-member oxazolidindionic cyclic structure.Type: ApplicationFiled: December 22, 2009Publication date: December 22, 2011Applicant: CREABILIS S.A.Inventors: Raffaella Bagnod, Luca Beccaria, Luisa Bertarione Rava Rossa, Domenico Criscuolo, Chiara Lorenzetto, Valentina Mainero, Alessandra Marconi, Carlo Pincelli, Silvio Traversa
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Publication number: 20110306593Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.Type: ApplicationFiled: November 11, 2009Publication date: December 15, 2011Inventors: Zhaoning Zhu, William J. Greenlee, Hongmei Li, Monica L. Vicarel, Jun Qin, Pawan Kumar Dhondi, Xianhai Huang, Anandan Palani, Xiaoxiang Liu, Zhong-Yue Sun, Hubert B. Josien, Ruo Xu, David James Cole, Duane A. Burnett, Chad E. Bennett, Troy McCracken, Malcolm MacCoss
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Patent number: 8076321Abstract: The present invention relates to the use of the combination of tyrosine phosphate inhibitors AMN107 and PKC412 for the preparation of a drug for the treatment of a mast cell-related proliferative disease. The present invention is also drawn to a combination treatment of a tyrosine phosphate inhibitor and a TK-inhibitor that is effective against a mast cell-related proliferative disease, including especially systemic mastocytosis (SM) including aggressive SM (ASM) and mast cell leukemia (MCL).Type: GrantFiled: July 19, 2006Date of Patent: December 13, 2011Inventor: Peter Valent
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Patent number: 8076320Abstract: Described are crystalline forms of the pharmaceutical compound “[9S-(9?,10?,12?)]-5,16-Bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9, 12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester”, as well as methods for their use and preparation.Type: GrantFiled: February 24, 2005Date of Patent: December 13, 2011Assignee: Cephalon, Inc.Inventors: Michael Harold Rock, Heidi Lopez De Diego, Kim Lasse Christensen, Ole Nielsen, Anders Buur, Mark Howells
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Patent number: 8071587Abstract: The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: May 25, 2010Date of Patent: December 6, 2011Assignee: N. V. OrganonInventors: Hubert Jan Jozef Loozen, Cornelius Marius Timmers
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Publication number: 20110294783Abstract: The present invention concerns boosting the activity of crop protection materials comprising inhibitors of fatty acid biosynthesis (for example phenyl-substituted cyclic ketoenols) through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: August 10, 2011Publication date: December 1, 2011Applicant: BAYER CROPSCIENCE AGInventors: Reiner FISCHER, Stefan LEHR, Peter MARCZOK, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich SANWALD, Rolf Pontzen
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Publication number: 20110294782Abstract: The present invention provides methods for treating fragile X syndrome and/or other neurodevelopmental disorders by administering small molecule p21-activated kinase (PAK) inhibitors to a patient suffering from, susceptible to, and/or exhibiting one or more symptoms of FXS and/or other neurodevelopmental disorders. The present invention provides specific small molecule PAK inhibitors and pharmaceutical compositions comprising small molecule PAK inhibitors.Type: ApplicationFiled: November 9, 2007Publication date: December 1, 2011Applicant: Massachusetts Institute of TechnologyInventors: Susumu Tonegawa, Mansuo L. Hayashi, Mazen Karaman, Patrick P. Zarrinkar, Daniel K. Treiber
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Publication number: 20110274738Abstract: Provided herein are methods for functionalizing a polymer for forming a coating and coatings and devices formed thereof or for functionalizing a coating or device surface including an polymer.Type: ApplicationFiled: July 19, 2011Publication date: November 10, 2011Inventors: Stephen Dirk Pacetti, Syed Faiyaz Ahmed Hossainy
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Patent number: 8039459Abstract: Nicotine receptor agonists or analogs or derivatives thereof for treating inflammatory pulmonary diseases, and pharmaceutical compositions including nicotine receptor agonists or analogs or derivatives thereof. Compounds of formula wherein R1, R2, Xa and Ya are as defined herein are also provided.Type: GrantFiled: July 15, 2005Date of Patent: October 18, 2011Assignee: Universite LavalInventors: Yvon Cormier, Evelyne Israel-Assayag, Marie-Renée Blanchet, René C. Gaudreault, Philippe Labrie
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Publication number: 20110244017Abstract: The present invention provides an absorbable coating for an implantable device and the methods of making and using the same.Type: ApplicationFiled: March 31, 2010Publication date: October 6, 2011Applicant: ABBOTT CARDIOVASCULAR SYSTEMS INC.Inventors: Lothar W. Kleiner, Syed F.A. Hossainy, Mikael Trollsas, Stephen D. Pacetti
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Patent number: 8008488Abstract: The invention relates to pyrimidin 2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula, A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of the formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X—Y can also jointly represent C?CH, C?CH—CH2 or CH—CH?CH; R1 and R2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents.Type: GrantFiled: March 12, 2004Date of Patent: August 30, 2011Assignee: Abbott GmbH & Co. KGInventors: Hervé Geneste, Andreas Kling, Wilfried Braje, Andreas Haupt, Liliane Unger
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Publication number: 20110183962Abstract: The invention provides methods for modulating, e.g., antagonizing, the activity of the Hedgehog signaling pathway, and for treating Hedgehog related disorders such as cancers (e.g., medulloblastoma). In particular, the invention provides methods for inhibiting aberrant growth states resulting from phenotypes such as Ptch loss-of-function, Hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function by administering to a mammal combinations of Smoothened inhibitors (e.g., a compound of Formula I, Formula II, or Formula III, or any of the compounds listed herein or incorporated by reference) and cholesterol biosynthesis pathway inhibitors (e.g., statins), Gli inhibitors, and/or Phosphatidylinositol 3-kinase (PI3K) inhibitors.Type: ApplicationFiled: September 28, 2009Publication date: July 28, 2011Applicant: Novartis AGInventors: Marion Dorsch, John E. Monahan, Michael Patrick Morrissey, Shifeng Pan, Juliet Williams
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Publication number: 20110172206Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.Type: ApplicationFiled: August 8, 2009Publication date: July 14, 2011Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Donald Jeffrey Zack, Zhiyong Yang, Cynthia Berlinicke, Harry Quigley
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Patent number: 7973032Abstract: This invention relates to staurosporine derivatives are effective when used in combination with ionizing radiation for the delay of progression or treatment of a proliferative disease, especially a disease associated with a PAX/FKHR translocation including a PAX3/FKHR translocation and a PAX7/FKHR translocation, more especially a solid tumor disease such as a Sarcoma, most especially an Alveolar Rhabdomyosarcoma.Type: GrantFiled: November 13, 2006Date of Patent: July 5, 2011Assignee: University of ZurichInventors: Marco Wachtel, Beat W. Schäfer, Ralf Amstutz
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Patent number: 7973031Abstract: The present invention relates to the use of staurosporines derivatives for the preparation of a drug for the treatment of diseases involving deregulated FLT3 receptor tyrosine kinase activity, especially for the curative and/or prophylactic treatment of leukemias and myelodysplastic syndromes, and to a method of treating diseases involving deregulated FLT3 receptor tyrosine kinase activity.Type: GrantFiled: October 29, 2002Date of Patent: July 5, 2011Assignees: Novartis AG, Dana-Farber Cancer Institute IncInventors: James Douglas Griffin, Paul William Manley
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Publication number: 20110136753Abstract: Glycosylated indolocarbazoles, method for obtaining same and uses thereof. This invention relates to rebeccamycin and staurosporine derivatives obtained by fermentation of recombinant bacterial strains. The invention also relates to the methods used to obtain the recombinant strains and the production of rebeccamycin and staurosporine derivatives. The invention also relates to bacterial strains that are of use for the production of rebeccamycin and staurosporine derivatives. Lastly, the rebeccamycin and staurosporine derivatives described herein are applicable to the field of human health, specifically for manufacturing drugs that are of use in the treatment of tumour, neurological and inflammatory diseases.Type: ApplicationFiled: April 6, 2009Publication date: June 9, 2011Applicants: UNIVERSIDAD DE OVIEDO, ENTRECHEM S.L.Inventors: Aaroa Pêrez Salas, César Sánchez Reillo, Alfredo Fernández Braña, Carmen Méndez Fernández, Jose Antonio Salas Fernández, Francisco Morís Varas
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Publication number: 20110130340Abstract: The present invention provides methods of identifying and/or detecting anti-cancer agents. The present invention provides methods of identifying and/or detecting compounds that can activate PARP and/or induce necrosis. The present invention also provides for methods of treating cancer in an individual. The present invention also provides kits for identifying and/or detecting anti-cancer agents.Type: ApplicationFiled: December 6, 2010Publication date: June 2, 2011Inventors: Craig B. Thompson, Wei-Xing Zong
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Publication number: 20110129463Abstract: Provided are quinazolin-4(3A)-one derivatives, which are inhibitors of the ubiquitin ligase activity of a human polypeptide, particularly to POSH inhibitors, and to compositions and methods for the treatment RING E3 ubiquitin ligase related diseases.Type: ApplicationFiled: November 26, 2010Publication date: June 2, 2011Applicant: Proteologics, Ltd.Inventors: Omri EREZ, Philippe NAKACHE
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Publication number: 20110124629Abstract: Described are crystalline forms of the pharmaceutical compound “[9S-(9?,10?,12?)]-5,16-Bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3 -fg:3?,2?,1?-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester”, as well as methods for their use and preparation.Type: ApplicationFiled: January 3, 2011Publication date: May 26, 2011Applicant: CEPHALON, INC.Inventors: Michael Harold Rock, Heidi Lopez De Diego, Kim Lasse Christensen, Ole Nielsen, Anders Buur, Mark Howells
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Publication number: 20110112067Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Applicant: Universitat des SaarlandesInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Publication number: 20110098274Abstract: Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: January 7, 2011Publication date: April 28, 2011Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
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Patent number: 7932255Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates or pharmaceutically acceptable formulations thereof. These compounds may be used to modulate cellular proliferation and to prevent and/or treat proliferative diseases.Type: GrantFiled: April 13, 2006Date of Patent: April 26, 2011Assignee: Novartis AGInventors: Robert Eckl, Roswitha Taube, Michael Almstetter, Michael Thormann, Andreas Treml, Christopher Straub, Zhouliang Chen