Tricyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/267)
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Publication number: 20130225616Abstract: The current invention is directed towards a polymorph of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (I) of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, wherein said polymorph is determined by single crystal X-ray structural analysis and X-ray powder diffraction pattern.Type: ApplicationFiled: August 9, 2011Publication date: August 29, 2013Applicant: VERONA PHARMA PLCInventors: Michael J.A. Walker, Bertrand M.C. Plouvier, Julian S. Northen, Philippe Fernandes
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Publication number: 20130225610Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.Type: ApplicationFiled: March 18, 2013Publication date: August 29, 2013Inventor: Marc Hansen
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Publication number: 20130217685Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.Type: ApplicationFiled: January 8, 2013Publication date: August 22, 2013Applicant: UNIVERSITY OF MASSACHUSETTSInventor: University of Massachusetts
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Publication number: 20130217675Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: February 18, 2011Publication date: August 22, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Patent number: 8513270Abstract: The present invention provides substituted tricyclic heteroaryl compounds, including, for example, pyridoindoles, pyrimidinoindoles and triazinoindoles that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases such as immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: December 20, 2007Date of Patent: August 20, 2013Assignee: Incyte CorporationInventors: Argyrios G. Arvanitis, James D. Rodgers, Louis Storace, Beverly Folmer
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Publication number: 20130210845Abstract: Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.Type: ApplicationFiled: July 22, 2011Publication date: August 15, 2013Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Daniel J. Finley, Randall W. King, Byung-Hoon Lee, Min J. Lee, Timothy C. Gahman
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Patent number: 8507502Abstract: Fused bicyclic or tricyclic compounds of formula (I): wherein A, B, C, X, Y, m, and n are defined herein. Also disclosed are a method for inhibiting EGFR kinase activity and a method for treating cancer with these compounds.Type: GrantFiled: November 9, 2009Date of Patent: August 13, 2013Assignee: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Tsu-An Hsu, Wen-Hsing Lin, Yi-Rong Chen, Yu-Sheng Chao
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Publication number: 20130203746Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: November 16, 2012Publication date: August 8, 2013Inventor: Medivation Technologies Inc.
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Publication number: 20130203789Abstract: The invention includes compounds that inhibit LYN kinase activity. The invention further includes a method of treating, ameliorating or preventing cancer in a subject in need thereof, wherein the cancer is dependent on LYN kinase activity.Type: ApplicationFiled: February 8, 2013Publication date: August 8, 2013Applicant: VASSA INFORMATICSInventor: VASSA INFORMATICS
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Publication number: 20130203777Abstract: Disclosed herein are compounds and compositions thereof which find use in increasing stability of TTR tetramers reducing its tendency to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of TTR and therby decreasing aggegate formation by TTR. Also disclosed herein are methods to screen for candidate compounds that increase stability of TTR. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.Type: ApplicationFiled: May 5, 2011Publication date: August 8, 2013Inventors: Isabella A. Graef, Mamoun Alhamadsheh
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Patent number: 8501755Abstract: This invention relates to compounds of Formula (I), wherein the variables are as disclosed in the specification, to pharmaceutical compositions containing them, to methods of making the compounds and pharmaceutical compositions, and to methods of using the compounds and pharmaceutical compositions for treating or preventing disorders, in particular cancer.Type: GrantFiled: March 20, 2007Date of Patent: August 6, 2013Assignee: Bayer Intellectual Property GmbHInventors: Chengzhi Zhang, Kanwar Sidhu, Mario Lobell, Gaetan Ladouceur, Qian Zhao, Zheng Liu, Kristen M. Allegue, Chetan P. Darne, Jason Newcom
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Patent number: 8501722Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections.Type: GrantFiled: January 21, 2010Date of Patent: August 6, 2013Assignee: The Regents of the University of MichiganInventors: David Ginsburg, Hongmin Sun, Scott Larsen, Bryan Yestrepsky
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Publication number: 20130190273Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: ApplicationFiled: February 19, 2013Publication date: July 25, 2013Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEMInventor: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
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Publication number: 20130190293Abstract: This disclosure is directed to tetracyclic pyrido[4,3-b]indole and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: February 18, 2011Publication date: July 25, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Publication number: 20130190304Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: March 12, 2013Publication date: July 25, 2013Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: Medivation Technologies, Inc.
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Publication number: 20130190305Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R6, A, B, C, n, p, q and r are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: ApplicationFiled: January 22, 2013Publication date: July 25, 2013Applicant: Boehringer Ingelheim International GmbHInventor: Matthias TREU
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Publication number: 20130190335Abstract: Disclosed are compounds of the formula (I) which are fluorescently labeled antagonists of the A3 adenosine receptor: wherein A, R1, R2, and Y are as described herein. Also disclosed are diagnostic compositions and a method of diagnosis of a patient for a possible treatment by an antagonist of the A3 adenosine receptor, involving the use of one or more of these compounds as diagnostic agents.Type: ApplicationFiled: January 24, 2013Publication date: July 25, 2013Applicants: The United State of America, as represented by the Secretary, Department of Health and Human Service, UNIVERSITA DEGLI STUDI DI PADOVA, Universita Degli Studi Di TriesteInventors: The United State of America, as represented by th e Department of Health and Human Services, Universita Degli Studi Di Trieste, UNIVERSITA DEGLI STUDI DI PADOVA
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Publication number: 20130184270Abstract: The present invention relates to: combinations of: component A: one or more 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (A1) or (A2), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B: one or more N-(2-arylamino)aryl sulfonamide compounds of general formula (B), or Lapatinib, or Paclitaxel, or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; and, optionally, component C: one or more further pharmaceutical agents; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and a kit comprising such a combination.Type: ApplicationFiled: April 14, 2011Publication date: July 18, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventor: Ningshu Liu
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Publication number: 20130184271Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: ApplicationFiled: February 19, 2013Publication date: July 18, 2013Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEMInventor: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
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Publication number: 20130184298Abstract: The present invention is directed to dihydrobenzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: September 29, 2011Publication date: July 18, 2013Inventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
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Patent number: 8486955Abstract: Cyclopenta[g]quinazolines of the formula (I):—wherein: A is a group OR or NR0R1 wherein R0 and R1 are each independently hydrogen C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl, or R0 and R1 together with the intermediate N form a five- or six-membered heterocyclic ring; p is an integer in the range 1 to 4; R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar1 is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy; and R3 is a group of one of the following formulae: -A1—Ar2-A2-Y1-A5-CON(R)CH(Y4)Y5-A8-X—Ar4 and pharmaceutically acceptable salts or esters thereof are of therapeutic value particularly in the treatment of cancer.Type: GrantFiled: November 2, 2009Date of Patent: July 16, 2013Assignee: BTG International LimitedInventors: Vassilios Bavetsias, Ann Lesley Jackman
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Publication number: 20130178488Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.Type: ApplicationFiled: September 20, 2011Publication date: July 11, 2013Inventors: Zehong WAN, Xiaomio Zhang, Zhaolong Tong, Kai Long, Sarah E. Dowdell, Eric Steven Manas, Krista Beaver Goodman
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Publication number: 20130172328Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):Type: ApplicationFiled: June 22, 2011Publication date: July 4, 2013Applicant: CROSSWING INC.Inventors: Takahiko Taniguchi, Masato Yoshikawa, Kasei Miura, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Makoto Kamata, Haruhi Kamisaki, John F. Quinn, Joseph Raker, Fatoumata Camara, Yi Wang
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Publication number: 20130171158Abstract: A method of treating or preventing an abnormality of glucose metabolism in a subject, the method comprising administering an antagonist of Inhibitor of Differentiation 1 (Id1) to the subject.Type: ApplicationFiled: June 29, 2011Publication date: July 4, 2013Applicant: GARVAN INSTITUTE OF MEDICAL RESEARCHInventors: Mia Akerfeldt, Ross Laybutt
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Publication number: 20130165437Abstract: A compound according to Formula Ia: wherein L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.Type: ApplicationFiled: December 20, 2012Publication date: June 27, 2013Applicant: GALAPAGOS NVInventor: GALAPAGOS NV
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Publication number: 20130158052Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z are as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors, such as, for example, inflammation.Type: ApplicationFiled: December 3, 2012Publication date: June 20, 2013Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa, Patrick Allison
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Publication number: 20130150353Abstract: This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.Type: ApplicationFiled: August 22, 2011Publication date: June 13, 2013Inventors: Zhaoyang Meng, Panduranga Adulla P. Reddy, M. Arshad Siddiqui, Amit K. Mandal, Duan Liu, Lianyum Zhao, Andrew McRiner
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Patent number: 8461160Abstract: This invention relates to dihydropyrimidinones of the formula wherein X and R1 to R7 are as defined in the description, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.Type: GrantFiled: April 30, 2010Date of Patent: June 11, 2013Assignee: Hoffmann-La Roche, Inc.Inventors: David Banner, Hans Hilpert, Roland Humm, Harald Mauser, Alexander V. Mayweg, Fabienne Ricklin, Mark Rogers-Evans
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Publication number: 20130143896Abstract: The present invention relates to substituted isoxazolo-quinazolines which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular human MPS1 and PERK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: July 20, 2011Publication date: June 6, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Caldarelli, Italo Beria, Nicoletta Colombo, Claudia Piutti, Matteo Salsa, Gabriella Traquandi
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Publication number: 20130131054Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: December 21, 2012Publication date: May 23, 2013Applicant: Medivation Technologies, Inc.Inventor: Medivation Technologies, Inc.
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Publication number: 20130129677Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: December 7, 2012Publication date: May 23, 2013Applicant: Siga Technologies, Inc.Inventor: Siga Technologies, Inc.
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Pharmaceutical formulations comprising salts of a protein kinase inhibitor and methods of using same
Patent number: 8445502Abstract: The present invention relates to pharmaceutical formulations comprising the protein kinase inhibitor, MP470, and methods of using same in treating conditions involving undesirable cell proliferation, such as cancer.Type: GrantFiled: October 18, 2010Date of Patent: May 21, 2013Assignee: Astex Pharmaceuticals, Inc.Inventors: David J. Bearss, Rajashree Joshi-Hangal, Xiao-Hui Liu, Pasit Phiasivongsa, Sanjeev G. Redkar, Hariprasad Vankayalapati -
Patent number: 8445504Abstract: A pyrazolopyrimidine compound represented by formula (1) that inhibits the function of HSP90 as a chaperone protein and that has antitumor activity, a medicament comprising a compound represented by formula (1), a pharmaceutical composition comprising a compound represented by formula (1), and a method for treating cancer using a compound represented by formula (1).Type: GrantFiled: April 20, 2012Date of Patent: May 21, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Hitoshi Ohki, Tooru Okayama, Masahiro Ikeda, Masahiro Ota, Yoshihiro Shibata, Toshiyuki Nakanishi, Yasusi Ueda, Nobuyuki Suzuki, Shinji Matuura
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Patent number: 8445503Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: GrantFiled: December 21, 2010Date of Patent: May 21, 2013Assignee: Elan Pharmaceuticals, Inc.Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Patent number: 8445482Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: GrantFiled: April 25, 2012Date of Patent: May 21, 2013Assignee: Janssen Pharmaceutica NVInventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Publication number: 20130123286Abstract: Certain novel fused quinazoline derivatives of formula (I) as c-Met inhibitors, their synthesis and their uses for treating a c-Met mediated disorder. Methods for treating a c-Met-mediated disorder are also disclosed in the invention.Type: ApplicationFiled: July 14, 2011Publication date: May 16, 2013Inventors: Shaojing Hu, Fei Wang, Wei Long, Xiaoyan Shen, Fenlai Tan, Yinxiang Wang
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Publication number: 20130123238Abstract: The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating or preventing an alcohol-related or addictive disorder. The (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.Type: ApplicationFiled: July 13, 2012Publication date: May 16, 2013Inventors: Anthony Alexander McKinney, Frank Bymaster
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Patent number: 8440654Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: GrantFiled: April 25, 2012Date of Patent: May 14, 2013Assignee: Janssen Pharmaceutica NVInventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Patent number: 8440680Abstract: A chemical compound having the following structural formula wherein optionally at least one of the phenyl —C6H5 groups bound to the Carbon atoms in position 2 and 6 is independently substituted with a methyl —CH3 or ethyl —C2H5 group, and wherein optionally the ?CH2 group in position 10 is substituted with a sulphinyl ?SO or sulphonyl ?SO2 group. Subject-matter of the invention is also a process of manufacture of 2,6-diphenyl-4,8-diazoadamantan-1-one and the use of this chemical compound and above-mentioned derivatives thereof as components for the formulation of solutions with sterilizing and disinfectant effect. The figure shows the IR spectrum of 2,6-diphenyl-4,8-diazoadamantan-1-one.Type: GrantFiled: November 12, 2007Date of Patent: May 14, 2013Assignee: Pietro AffaitatiInventors: Pietro Affaitati, Giancarlo Folchitto
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Publication number: 20130102623Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.Type: ApplicationFiled: October 10, 2012Publication date: April 25, 2013Inventor: Aleem Gangjee
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Publication number: 20130096146Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.Type: ApplicationFiled: October 9, 2012Publication date: April 18, 2013Inventor: Aleem Gangjee
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Patent number: 8420658Abstract: Method and composition of Carboxyamidotriazole orotate for treating age-related macular degeneration and other angiogenesis-dependent diseases.Type: GrantFiled: May 24, 2010Date of Patent: April 16, 2013Assignee: Tactical Therapeutics IncInventor: Rashida A Karmali
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Publication number: 20130085123Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidine compounds, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: ApplicationFiled: May 31, 2011Publication date: April 4, 2013Applicant: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
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Publication number: 20130079323Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.Type: ApplicationFiled: September 10, 2010Publication date: March 28, 2013Applicant: TRIUS THERAPEUTICS, INC.Inventors: Christopher J. Creighton, Leslie William Tari, Zhiyong Chen, Mark Hilgers, Thanh To Lam, Xiaoming Li, Michael Trzoss, Junhu Zhang, John Finn, Daniel Bensen
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Patent number: 8404698Abstract: Quinazoline derivatives represented by the general formula pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for using the compounds for treatment of hyperproliferative disorders are also disclosed.Type: GrantFiled: June 16, 2008Date of Patent: March 26, 2013Assignee: Rexahn Pharmaceuticals, Inc.Inventors: Young Bok Lee, Chang Ho Ahn
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Publication number: 20130071319Abstract: Certain embodiments disclosed herein relate to compositions, methods, devices, systems, and products regarding frozen particles. In certain embodiments, the frozen particles include materials at low temperatures. In certain embodiments, the frozen particles provide vehicles for delivery of particular agents. In certain embodiments, the frozen particles are administered to at least one biological tissue.Type: ApplicationFiled: October 8, 2012Publication date: March 21, 2013Applicant: Searete LLCInventor: Searete LLC
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Publication number: 20130065842Abstract: Heterocyclic compounds, and pharmaceutical compositions thereof, are disclosed as ROR?t modulators that have a formula represented by the following: and wherein n1, n2, R1, R2, R3, and R4 are as described herein. These compounds may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.Type: ApplicationFiled: March 11, 2011Publication date: March 14, 2013Inventors: Dan Littman, Jun R. Huh, Wenwei Huang, Ruili Huang
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Patent number: 8389533Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are gem-disubstituted or spirocyclic pyridine, pyrimidine and triazine derivatives.Type: GrantFiled: April 6, 2009Date of Patent: March 5, 2013Assignee: Amgen Inc.Inventors: Richard V. Connors, Kang Dai, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. McGee, Rajiv Sharma, Xiaodong Wang
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Patent number: 8389532Abstract: The compound having the structural formula I or a pharmaceutically acceptable salt thereof, is disclosed, as well as its use in the treatment of central nervous system diseases, in particular Parkinson's disease, Extra Pyramidal Syndrome, restless legs syndrome and attention deficit hyperactivity disorder, pharmaceutical compositions comprising it, and combinations with other agents.Type: GrantFiled: July 6, 2009Date of Patent: March 5, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Jean E. Lachowicz
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Patent number: RE44205Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted ?m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, ?phenyl-CH(OH)—, or phenyl-C(?NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compType: GrantFiled: April 6, 2012Date of Patent: May 7, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil