Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/243)
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Patent number: 7737144Abstract: The invention relates to pyrimido[5,4-e][1,2,4]triazine-5,7-diones, pharmaceutically acceptable salts thereof and physiologically functional derivatives. The invention therefore relates to compounds of the formula I, in which the radicals have the given meanings, and to their physiologically tolerated salts and processes for preparing them. The compounds are suitable for use as antidiabetics, for example.Type: GrantFiled: June 28, 2007Date of Patent: June 15, 2010Assignee: Sanofi-Aventis Deutschland GmbHInventors: Stefan Petry, Karl-Heinz Baringhaus, Norbert Tennagels, Guenter Mueller
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Publication number: 20100144736Abstract: The invention relates to novel biphenyl thio-urea derivatives of Formula (I), wherein A represents hydroxy or tetrazolyl; R1 represents halo, hydroxy or phenyl, which phenyl may optionally be substituted with halo; and R2 and R3, independent of each other, represent halo, trifluoromethyl, nitro and/or phenyl, that are found to be potent modulators of ion channels and, as such, they are valuable candidates for the treatment of disease or disorders as diverse as those which are responsive to modulation of ion channels.Type: ApplicationFiled: December 17, 2007Publication date: June 10, 2010Applicant: NeuroSearch A/SInventors: Antonio Nardi, Joachim Demnitz, Morten Grunnet, Palle Christophersen, David Spencer Jones, Elsebet Østergaard Nielsen, Dorte Strøbæk, Lars Siim Madsen
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Publication number: 20100144610Abstract: An aspect of the present invention provides for a medicament including a solution containing pleconaril or a pharmaceutically acceptable salt thereof, wherein at least one solvent including the solution is a pleconaril-dissolving hydrofluorocarbon.Type: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Inventors: Saeed M. Chaudhry, Julianne Berry, Joel A. Sequeira
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Publication number: 20100136137Abstract: This invention relates to a synergistic therapeutic combination of anti-cancer compounds which comprises a) a panHER/VEGFR2 kinase inhibitor, and b) a platinum compound, and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use. The invention also relates to treating certain cancers utilizing the combination of the invention.Type: ApplicationFiled: October 31, 2007Publication date: June 3, 2010Inventors: Tai W. Wong, Jean Soria, Guido Kroemer
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Publication number: 20100137318Abstract: A compound of a formula (I): wherein R1 represents a C3-10 branched alkyl group which may be substituted; R2 represents a hydrogen atom or a C1-4 alkyl group which may be substituted; R3 represents a C1-4 alkyl group which may be substituted or a halogen atom; R4 represents a C1-4 alkyl group which may be substituted; and ring 1 represents a cyclic group which has planarity and may have a substituent group, a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof, is useful as a medicinal component having CRF antagonistic activity for the prevention and/or treatment of a neuropsychiatric disease, a peripheral organ disease and the like.Type: ApplicationFiled: April 25, 2008Publication date: June 3, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Tetsuji Saito, Tetsuo Obitsu, Yoshifumi Kagamiishi
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Publication number: 20100137319Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.Type: ApplicationFiled: February 5, 2010Publication date: June 3, 2010Inventors: Harold Mastalerz, Dolatral M. Vyas, George L. Trainor, Ashvinikumar V. Gavai
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Publication number: 20100137253Abstract: Compositions and uses associated with the MT477 family of compounds are disclosed. Particular structural features and properties of the compounds are described in detail. Uses include administering an MT477 family member to a patient for therapeutic purposes. Compositions include chemicals belonging to the MT477 family and pharmaceuticals that contain such chemicals.Type: ApplicationFiled: December 10, 2009Publication date: June 3, 2010Applicant: Medisyn Technologies, Inc.Inventors: Javier Llompart, Jorge Galvez, Kollol Pal
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Publication number: 20100130467Abstract: The present invention is directed to [1,2,4]triazolo[4,3-b][1,2,4]triazines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.Type: ApplicationFiled: January 28, 2010Publication date: May 27, 2010Inventors: Jincong Zhuo, Colin Zhang, Meizhong Xu, Ding-Quan Qian, Wenqing Yao, Ravi Kumar Jalluri
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Publication number: 20100130498Abstract: The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.Type: ApplicationFiled: March 31, 2008Publication date: May 27, 2010Applicant: Deutshes Institut Fur Ernahrungsforschung Potsdam- RehbruckeInventors: Maik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
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Patent number: 7723330Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: March 6, 2007Date of Patent: May 25, 2010Assignees: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
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Publication number: 20100120758Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: ApplicationFiled: September 3, 2009Publication date: May 13, 2010Applicant: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
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Publication number: 20100119508Abstract: The present invention relates to new phenylacetic acid inhibitors of cyclooxygenase activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 11, 2009Publication date: May 13, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manoucherhr M. Shahbaz
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Publication number: 20100120763Abstract: The invention relates to imidazo[5,1-c][1,2,4]benzotriazine derivatives of formula I: which are inhibitors of phosphodiesterase 2 or 10 useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type 2 diabetes, metabolic syndrome, glucose intolerance, and pain.Type: ApplicationFiled: November 6, 2009Publication date: May 13, 2010Applicant: WYETHInventors: Hans Stange, Barbara Langen, Ute Egerland, Norbert Hoefgen, Martina Priebs, Michael S. Malamas, James Joseph Erdei, Yike Ni
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Publication number: 20100120762Abstract: The invention relates to triazine derivatives of formula (I): which are inhibitors of phosphodiesterase 2 or 10, useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type 2 diabetes, metabolic syndrome, glucose intolerance, and pain.Type: ApplicationFiled: November 6, 2009Publication date: May 13, 2010Applicant: WYETHInventors: Hans Stange, Barbara Langen, Ute Egerland, Norbert Hoefgen, Martina Priebs, Michael S. Malamas, James Joseph Erdei, Yike Ni
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Publication number: 20100120739Abstract: The present disclosure relates to triazolopyridazine protein kinase modulators of Formula (I), methods of using these compounds to treat diseases mediated by kinase activity.Type: ApplicationFiled: October 18, 2007Publication date: May 13, 2010Inventors: Christopher Ronald Smith, Pierre- Yves Bounaud, Elizabeth Anne Jefferson, Patrick S. Lee, Eduardo Torres
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Patent number: 7713972Abstract: The present invention provides the compounds inhibiting PDE 7 selectively, and therefore, enhances cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is imidazotriazinone compound represented by the following formula (IA) or (IB): especially, R1 is cyclohexyl group, R2 is methyl group; R3 is a hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; substituted or unsubstituted C1-C6 alkyl group; substituted or unsubstituted C2-C6 alkenyl group; saturated or unsaturated heterocycloalkyl group which is substituted or unsubstituted; a group: —NR5R6, —C(O)R7, —SO2R7, —OR8, —NR8COR7, —NR8S02R7; A is CR4; and B is CH.Type: GrantFiled: June 11, 2004Date of Patent: May 11, 2010Assignee: Asubio Pharma Co., Ltd.Inventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
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Patent number: 7713973Abstract: Compounds, pharmaceutical compositions and kits are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: GrantFiled: October 14, 2005Date of Patent: May 11, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Qing Dong, David J. Hosfield, Bheema R. Paraselli, Nicholas Scorah, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
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Patent number: 7713966Abstract: The present invention relates generally to azabicyclic containing pharmaceutical agents, and in particular, to azabicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azabicyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, which exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: GrantFiled: November 20, 2007Date of Patent: May 11, 2010Assignee: Alantos Pharmaceuticals Holding, Inc.Inventors: Christian Gege, Matthias Schneider, Carine Chevrier, Hongbo Deng, Irving Sucholeiki, Brian M. Gallagher, Jr., Michael Bosies, Christoph Steeneck, Xinyuan Wu, Matthias Hochgürtel, Bert Nolte, Arthur Taveras
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Publication number: 20100113454Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anti-cancer agents and for the treatment of Alzheimer's Disease.Type: ApplicationFiled: April 17, 2008Publication date: May 6, 2010Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Anthony J. Sampognaro, Mark D. Wittman
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Publication number: 20100112048Abstract: The present invention relates to a synergistic combination for preventing the onset and/or progression of dementia or Alzheimer's disease in individuals at increased risk thereof for example because of family history, genetic factors, and/or environmental factors. This combination comprises synergistically effective amounts of vitamin C, vitamin E, DHA and at least one NSAID such as ibuprofen.Type: ApplicationFiled: July 19, 2006Publication date: May 6, 2010Inventor: Majid Fotuhi
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Publication number: 20100113455Abstract: A method of treating bone pain caused by osteoarthritis by administering to a patient an effective amount of a composition containing a bone edema medication, such as a vasoactive medication or phosphodiesterase inhibitor, including a PDE-5 inhibitor.Type: ApplicationFiled: January 11, 2010Publication date: May 6, 2010Inventor: Joseph Bernstein
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Publication number: 20100113453Abstract: The invention provides methods and compositions for treating anxiety-related disorders in a subject. The methods include sublingually administering D-cycloserine to a subject with the anxiety-related disorder, either alone or in combination with extinction training.Type: ApplicationFiled: April 10, 2008Publication date: May 6, 2010Inventors: Jason P. McDevitt, Michael Davis, Kerry J. Ressler
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Publication number: 20100113452Abstract: The present invention relates to pharmaceutical compositions and combinations for treating, preventing or managing pulmonary hypertension comprising small molecule heterocyclic pharmaceuticals, and more particularly, substituted pyridines and pyridazines optionally combined with at least one additional therapeutic agent.Type: ApplicationFiled: April 3, 2007Publication date: May 6, 2010Applicant: BAYER HEALTHCARE AGInventors: Martina Klein, Peter Sandner, Reiner Frey, Bernd Riedl, Olaf Christensen
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Publication number: 20100105689Abstract: This invention relates to novel 1,4- and 1,5-diarylsubstituted 1,2,3-triazole derivatives that are found to be potent modulators of potassium channels and, as such, they are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to modulation of potassium channels.Type: ApplicationFiled: January 17, 2008Publication date: April 29, 2010Inventors: Antonio Nardi, Morten Grunnet, Joachim Demnitz, Palle Christophersen, David Spencer Jones, Elsebet Østergaard Nielsen, Dorte Strøbæk, Lars Siim Madsen
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Publication number: 20100104624Abstract: Described here are compositions and methods for treating side-effects of vasodilator therapy. The compositions may include both a vasodilator and a side-effect alleviating agent in a single dosage form. Alternatively, the vasodilator and side-effect alleviating agent may be formulated separately, each in its own dosage form. The compositions may be packaged as kits for use with various medical conditions.Type: ApplicationFiled: June 11, 2009Publication date: April 29, 2010Inventors: Peter LANGECKER, Bryan T. Oronsky
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Publication number: 20100105676Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, [PLEASE INSERT CHEMICAL STRUCTURE HERE] (I) are useful as kinase modulators, including Btk modulation, wherein R1, R2, R4, Q, Y, A and D are as defined herein.Type: ApplicationFiled: March 20, 2008Publication date: April 29, 2010Inventors: Chunjian Liu, Katerina Leftheris, Andrew J. Tebben
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Patent number: 7704999Abstract: The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.Type: GrantFiled: December 21, 2007Date of Patent: April 27, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Niewöhner, Maria Niewöhner, legal representative, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jörg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Serno, Marc Nowakowski
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Publication number: 20100099679Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.Type: ApplicationFiled: November 20, 2009Publication date: April 22, 2010Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A.R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Quinghua Weng, James David Beard
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Patent number: 7700594Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.Type: GrantFiled: November 15, 2006Date of Patent: April 20, 2010Assignee: OSI Pharmaceuticals, Inc.Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A. R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Qinghua Weng, James David Beard
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Publication number: 20100093719Abstract: A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or pharmaceutically acceptable salt, stereoisomer, or hydrate thereof, wherein R1 is lower alkyl, R2 and R3 are independently selected from lower alkyl, and lower alkenyl and lower alkynyl, wherein the lower alkyl, lower alkenyl, and lower alkynyl may be optionally substituted with one or more halogen, lower alkoxy, hydroxy, CN, NO2, amino, acylamino, amido, carbonyl, and alkylthio, A is N or C—H, B is N, C—H, C—(SO2—R4), or C—CO—R4, D is N, C—H, C—(SO2—R4) or C—CO—R4, E is N or C—H, wherein only one of A, B or E may be N, and one of B or D is C—(SO2—R4) or C—CO—R4, R4 is a group having the formula: in which each R5, R6, R7 and R8 are independently selected from H and lower alkyl, wherein the lower alkyl may be optionally substituted with one or more halogen, lower alkoxy, hydroxy, CN, NO2, amino, acylamino, amido, carbonyl, and alkylthio; and additionally or alternatively R6 and R5Type: ApplicationFiled: September 30, 2009Publication date: April 15, 2010Applicant: SURFACE LOGIX, INC.Inventors: Stewart CAMPBELL, David DUFFY, Michael GROGAN, Steven KATES, Emanuele OSTUNI, Olivier SCHUELLER, Paul SWEETNAM
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Publication number: 20100093738Abstract: The present invention relates to compounds of the formula I and their use for controlling phytopathogenic fungi, and also to fungicidal mixtures comprising a compound of the formula I, where the variables and substituents have the meanings defined in the claims and in the description.Type: ApplicationFiled: October 8, 2006Publication date: April 15, 2010Applicant: BASF SEInventors: Bernd Müller, Jens Renner, Egon Haden
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Patent number: 7696206Abstract: The application claims a compound of the formula or a salt, a hydrate, or a hydrate of a salt thereof. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of erectile dysfunction.Type: GrantFiled: September 29, 2009Date of Patent: April 13, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Niewöhner, Maria Niewöhner, legal representative, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jorg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Serno, Marc Nowakowski
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Publication number: 20100081661Abstract: Inhibitors of microbial heme oxygenase and their use for treatment of microbial infections and bioremediation. The inhibitors of microbial heme oxygenase are useful against a new class of antimicrobial agents to target infections that are persistently difficult to combat with the current spectrum of antimicrobial agents. Screening methods for selecting inhibitors of microbial heme oxygenase.Type: ApplicationFiled: July 24, 2007Publication date: April 1, 2010Applicant: UNIVERSITY OF MARYLAND, BALTIMOREInventors: Angela Wilks, Alexander MacKerrel, JR., Lena Furci, Pedro Lopes
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Publication number: 20100081655Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: ApplicationFiled: August 14, 2009Publication date: April 1, 2010Applicant: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
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Publication number: 20100081610Abstract: The present invention relates to ?-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase using the compounds.Type: ApplicationFiled: August 21, 2007Publication date: April 1, 2010Inventors: Viswajanani J. Sattigeri, Venkata P. Palle, Manoj Kumar Khera, Ranaheer Reddy, Manoj Kumar Tiwari, Ajay Soni, Abdul Rehman Abdul Rauf, Sony Joseph, Arpita Musib, Sunanda G. Dastidar, Punit Kumar Srivastava
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Publication number: 20100081662Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB, TrkC or Flt-3 thereby making them useful as anticancer agents.Type: ApplicationFiled: November 2, 2007Publication date: April 1, 2010Inventors: Brian E. Fink, Ping Chen
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Publication number: 20100075958Abstract: This invention relates to pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.Type: ApplicationFiled: July 20, 2009Publication date: March 25, 2010Applicant: Bayer Pharmaceuticals CorporationInventors: Julie A. Dixon, Catherine Brennan, Karl Miranda, Brent Chandler, Barton Phillips, Jianmei Fan, Michael Brands, Andrea McClure, Benjamin Jones, Wenlang Fu, Donald Bierer, Steven Magnuson, Harold C.E. Kluender
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Patent number: 7683060Abstract: The present invention is directed to [1,2,4]triazolo[4,3-b][1,2,4]triazines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.Type: GrantFiled: August 6, 2007Date of Patent: March 23, 2010Assignee: Incyte CorporationInventors: Jincong Zhuo, Colin Zhang, Meizhong Xu, Ding-Quan Qian, Wenqing Yao, Ravi Kumar Jalluri
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Publication number: 20100063038Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: December 1, 2006Publication date: March 11, 2010Inventors: Julie Dixon, Barton Phillips, Furahi Achebe, Harold Kluender, Jason Newcom, Kyle Parcella, Stephen J. O'Connor, Steven Magnuson, Zhenqui Hong, Zhonghua Zhang, Zheng Liu, Uday Khire, Lei Wang, Martin Michels, Brent Chandler
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Patent number: 7674790Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.Type: GrantFiled: January 13, 2006Date of Patent: March 9, 2010Assignee: Schering CorporationInventors: Sydney Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Leonore C. Witchey-Lakshmanan
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Patent number: 7671054Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: GrantFiled: October 15, 2007Date of Patent: March 2, 2010Assignee: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen, Soo Jin Lee
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Patent number: 7671199Abstract: The invention relates to an improved process for preparing [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester of the formula: Compound I has been shown to be useful for the treatment of certain types of cancer.Type: GrantFiled: April 20, 2007Date of Patent: March 2, 2010Assignee: Britsol-Myers Squibb CompanyInventors: Gerard A. Crispino, Mourad Hamedi, Thomas L. LaPorte, John E. Thornton, Jaan A. Pesti, Zhongmin Xu, Paul C. Lobben, David K. Leahy, Jale Muslehiddinoglu, Chiajen Lai, Lori Ann Spangler, Robert P. Discordia, Francis S. Gibson
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Publication number: 20100048575Abstract: The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use: Formula (I) wherein R3, R4, R5, R6, Y, Het1, T, U, V, W, X, Ru, Rv and Rw are as defined in claim 1Type: ApplicationFiled: October 25, 2007Publication date: February 25, 2010Inventors: Philippe Guedat, Xavier Jacq, Frédéric Colland, Laurent Daviet, Etienne Formstecher, Jean-Christophe Rain, Matteo Colombo
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Publication number: 20100035882Abstract: The invention relates to the use of PDE2A inhibitors for the manufacture of a medicament for the treatment and/or prophylaxis of coronary diseases, especially stable and unstable angina pectoris, acute myocardial infarction, prophylaxis of myocardial infarction, heart failure, and high blood pressure and the sequelae of atherosclerosis, and vascular disorders, disorders of the kidney, especially renal failure, inflammatory disorders, erectile dysfunction and prevention of sudden heart death.Type: ApplicationFiled: October 2, 2007Publication date: February 11, 2010Inventors: Peter Ellinghaus, Andreas Wilmen, Martin Hendrix, Adrian Tersteegen
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Publication number: 20100029630Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: ApplicationFiled: July 27, 2009Publication date: February 4, 2010Applicant: Chongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen, Soo Jin Lee
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Publication number: 20100022503Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: January 4, 2008Publication date: January 28, 2010Inventors: Marco Dodier, Claude A. Quesnelle, Anne Marinier
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Publication number: 20100016323Abstract: The application claims a compound of the formula or a salt, a hydrate, or a hydrate of a salt thereof. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of erectile dysfunction.Type: ApplicationFiled: September 29, 2009Publication date: January 21, 2010Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Niewöhner, Maria Niewöhner, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jörg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Serno, Marc Nowakowski
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Patent number: 7645756Abstract: The invention provides a compound or its pharmaceutically-acceptable salt of formula wherein A1 is a hydrogen, etc.; j and k are 0 or 1; is a double bond, etc.; is a double bond, etc.; one of W1 and W2 is E—O—W, etc., and the other is a hydrogen atom, etc.; E is a divalent group derived from a benzene ring, etc., by removing two hydrogen atoms therefrom; W is a group of formula (II-1): which has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for prevention or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.Type: GrantFiled: February 17, 2005Date of Patent: January 12, 2010Assignee: Banyu Pharmaceutical Co. Ltd.Inventors: Toshiyuki Takahashi, Akio Kanatani, Shigeru Tokita, Ryo Yoshimoto
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Publication number: 20090318436Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: October 14, 2008Publication date: December 24, 2009Applicant: Amgen Inc.Inventors: Brian K. Albrecht, David Bauer, Steven Bellon, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Randall W. Hungate, Tae-Seong Kim, Richard T. Lewis, Longbin Liu, Julia Lohman, Mark H. Norman, Michelle Potashman, Aaron C. Siegmund, Stephanie K. Springer, Markian Stec, Ning Xi, Kevin Yang
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Publication number: 20090312331Abstract: Processes are provided for selectively preparing novel stable crystalline salt forms, selectively and consistently, namely, preparing Form N-1 of the methanesulfonic acid salt, and Form N-1 and Form N-4 of the hydrochloric acid salt of the p38 kinase inhibitor 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide. The processes preferably employ solvent systems including formic acid/acetone and formic acid/methylethyl ketone which produce crystals having suitable flow properties and desired particle size, and solvents such as N,N-dimethylformamide and N,N-dimethylacetamide may be employed as well. Novel Form N-1 crystals of the Form N-1 and Form N-4 crystals of the hydrochloride salt and Form N-1 crystals of the methanesulfonic acid salt of the above free base, pharmaceutical compositions containing such novel forms and a method of treating p38 kinase associated conditions, including rheumatoid arthritis are also provided.Type: ApplicationFiled: June 4, 2009Publication date: December 17, 2009Inventors: Soojin Kim, Mary F. Malley, Zhongping Shi