Additional Six-membered Hetero Ring Consisting Of Five Ring Carbons And One Ring Nitrogen Attached Directly Or Indirectly To The 1,3-diazine By Nonionic Bonding Patents (Class 514/252.18)
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Patent number: 8501740Abstract: Methods of preventing the development and reversing or partially reversing opioid tolerance in a subject are provided herein. Such methods include the step of administering to a subject in need thereof a therapeutically effective amount of a PDGFR modulator or EGFR modulator alone or together with an opiate analgesic. The methods can also be used for the treatment of refractory neuropathic pain, physical dependence or addiction.Type: GrantFiled: October 8, 2008Date of Patent: August 6, 2013Assignee: Board of Regents, The University of Texas SystemInventor: Howard Gutstein
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Publication number: 20130197009Abstract: [Problem] An object of the present invention is to provide a novel anticancer drug which is useful for treating prostate cancer accompanying androgen receptor mutation [Means for Solution] The present inventors conducted thorough research on mutant androgen-related diseases for which the traditional anti-androgen drugs become ineffective. As a result, they found that the compound, which is an active ingredient of the pharmaceutical composition of the present invention, exhibits an inhibitory action against transcriptional activation in a human mutant androgen receptor (AR), and has an excellent antitumor action in a human prostate cancer-bearing mouse, thereby completing the present invention. Accordingly, the compound, which is an active ingredient of the pharmaceutical composition of the present invention, is useful for a series of androgen receptor-related diseases including prostate cancer.Type: ApplicationFiled: October 21, 2011Publication date: August 1, 2013Applicant: ASTELLAS PHARMA INC.Inventors: Yukitaka Ideyama, Sadao Kuromitsu, Takashi Furutani, Masayoshi Takeda, Satoshi Konagai, Tomohiro Yamada, Nobuaki Taniguchi, Yutaka Kondoh, Masaaki Hirano, Kazushi Watanabe, Takashi Sugane, Akio Kakefuda
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Publication number: 20130195988Abstract: A vascular embolization gelling agent for sustained release of drugs for treating tumors having a drug and a drug carrier. The drugs are antitumor drugs. The drug carrier includes poloxamer polymer and polyvinylpyrrolidone or gel made of the combination, and may be purified before use. The drug carrier accounts for 5-65% of the gel. The particle size of the gel is in the range of 10 nm-150 ?m. The embolization agent is a liquid gel at normal temperature, to facilitate direct transcatheter injection, and is rapidly solidified to the gel state in body with the increase of the temperature; it is used to encapsulate different drugs on demand, and can achieve dual efficacy of embolization and drug treatment through local sustained release of the drug. The present invention can be used as the embolization agent for endovascular interventional therapy for transcatheter arterial chemoembolization of various benign and malignant tumors.Type: ApplicationFiled: March 8, 2013Publication date: August 1, 2013Applicant: Shanghai Cancer InstituteInventor: Shanghai Cancer Institute
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Patent number: 8492383Abstract: The invention relates to a combination which comprises (a) a nitrogen mustard analogue selected from chlorambucil, chlornaphazine, estramustine, mechlorethamine, mechlorethamine oxide hydrochloride, navembichin, phenestrine, prednimustine, trofosfamide or uracil mustard and (b) 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of formula or a pharmaceutically acceptable salt thereof, the invention pertains to the use of said combination for the treatment chronic lymphocytic leukemia.Type: GrantFiled: August 19, 2009Date of Patent: July 23, 2013Assignee: Jewish General HospitalInventors: Lawrence C Panasci, Raquel S Aloyz
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Publication number: 20130184287Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.Type: ApplicationFiled: February 18, 2011Publication date: July 18, 2013Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael Gray, Wenjun Zhou, Xianming Deng
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Publication number: 20130184259Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.Type: ApplicationFiled: November 16, 2012Publication date: July 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: VERTEX PHARMACEUTICALS INCORPORATED
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Publication number: 20130184248Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: January 11, 2013Publication date: July 18, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF
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Patent number: 8486933Abstract: Described herein are compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein L1, R1, R2, R3, R4, R5, and m are defined in the description. Methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as IGF-1R are also disclosed.Type: GrantFiled: May 26, 2010Date of Patent: July 16, 2013Assignee: AbbVie Inc.Inventors: Gary T. Wang, Robert A. Mantei, Scott A. Erickson, Steve D. Fidanze, George S. Sheppard, Jieyi Wang, Randy L. Bell
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Publication number: 20130172656Abstract: Novel Uses of an aromatic ester isolated from Armillaria mellea, particularly, armillaridin, are disclosed herein. The armillaridin is useful for manufacturing a medicament or a pharmaceutical composition for suppressing the growth of cancerous cells or for enhancing susceptibility of esophageal cancerous cells to a radiation treatment, in a subject.Type: ApplicationFiled: January 3, 2012Publication date: July 4, 2013Inventors: Yu-Jen Chen, Chien-Chih Chen
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Publication number: 20130164259Abstract: The present invention relates to 1,4-Substituted Piperazine Derivatives, compositions comprising one or more 1,4-Substituted Piperazine Derivatives, and methods of using the 1,4-Substituted Piperazine Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: December 20, 2010Publication date: June 27, 2013Inventors: Cliff C. Cheng, Xiaohua Huang, Gerald W. Shipps, JR.
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Publication number: 20130158095Abstract: The present inventors found that a fusion gene present in some cancer patients is an oncogene. The present invention relates to a polypeptide as a novel fusion protein, a polynucleotide encoding the polypeptide, a vector comprising the polynucleotide, a transformed cell comprising the vector, a method for detecting the fusion protein or polynucleotide, a method for screening a therapeutic agent for cancer, and a method for treating cancer that is shown to be positive for the fusion gene. Further, the present invention relates kit, primer set, and probe useful in the detection of cancer that is shown to be positive for the fusion gene.Type: ApplicationFiled: May 10, 2012Publication date: June 20, 2013Applicants: CureGene K.K., Astellas Pharma Inc.Inventors: Hiroyuki Mano, Sadao Kuromitsu, Nobuaki Shindo, Takatoshi Soga, Takashi Furutani
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Publication number: 20130158019Abstract: Compounds of Formula I are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: May 4, 2011Publication date: June 20, 2013Applicant: AMGEN INC.Inventors: Marian C. Bryan, Alan C. Cheng, Elizabeth M. Doherty, James R. Falsey, Ingrid M. Fellows, Joseph L. Kim, Richard T. Lewis, Michele H. Potashman, Douglas A. Whittington
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Patent number: 8466156Abstract: The present invention relates to 2-phenyl-4-cyclopropyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.Type: GrantFiled: April 9, 2009Date of Patent: June 18, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Eva Caroff, Emmanuel Meyer
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Publication number: 20130150375Abstract: A method of treatment of depression in a person also taking non-Steroidal anti-inflammatory drugs (NSAIDs) by administering gepirone as either a short term or long term therapy.Type: ApplicationFiled: December 10, 2012Publication date: June 13, 2013Applicant: Fabre-Kramer Pharmaceuticals.Inc.Inventor: Fabre-Kramer Pharmaceuticals, Inc.
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Publication number: 20130150356Abstract: The present invention relates to acyl piperazine derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: ApplicationFiled: August 9, 2011Publication date: June 13, 2013Applicant: RAQUALIA PHARMA INC.Inventors: Mikiko Morita, Shuzo Watanabe
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Publication number: 20130137661Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.Type: ApplicationFiled: November 19, 2010Publication date: May 30, 2013Applicant: SK CHEMICALS CO. LTD.Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
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Patent number: 8450317Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R5, A, B, D and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: April 27, 2010Date of Patent: May 28, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Jennifer A. Kowalski, Daniel Richard Marshall, Anthony S. Prokopowicz, III, Sabine Schlyer, Robert Sibley, Ronald John Sorcek, Di Wu, Frank Wu, Erick Richard Roush Young
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Publication number: 20130131076Abstract: This application describes a novel technology in drug discovery and drug-based imaging/detection: the wrapping technology. This technology is based on identified singularities in the structure of soluble proteins. In contrast with drug-design approaches based on standard structural considerations, the packing of a protein, or more precisely, its dehydron pattern, may be used as a selectivity filter to design small-molecule inhibitors. The wrapping technology described herein is a novel form of rational drug design for avoiding side effects in drug therapy and sharpening the inhibitory impact of drugs on the oncokinome.Type: ApplicationFiled: October 29, 2007Publication date: May 23, 2013Applicant: The Board of Regents of the University of Texas SystemInventors: Ariel Fernandez, William Bornmann, Gabriel Lopez-Berestein, Angela Sanguino, Zheng-Hong Peng, Anil K. Sood
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Publication number: 20130123241Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.Type: ApplicationFiled: May 10, 2011Publication date: May 16, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
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Publication number: 20130123252Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: July 21, 2011Publication date: May 16, 2013Applicant: NOVARTIS AGInventors: David Barnes, Scott Louis Cohen, Jiping Fu, Lei Shu, Rui Zheng
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Publication number: 20130121963Abstract: This disclosure relates to novel N-phenyl-2-pyrimidineamines and pharmaceutically acceptable salts thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering protein-tyrosine kinase inhibitors.Type: ApplicationFiled: May 16, 2012Publication date: May 16, 2013Applicant: Concert Pharmaceuticals Inc.Inventors: Scott L. Harbeson, Julie F. Liu, Roger Tung
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Publication number: 20130109653Abstract: The present invention provides a substituted pyridine compound or a pharmacologically acceptable salt thereof which has excellent CETP inhibition activity and is useful as a medicament. The present invention provides a compound represented by a general formula (I), wherein R1 is H, optionally substituted alkyl, OH, optionally substituted alkoxy, alkylsulfonyl, optionally substituted amino, carboxy, optionally substituted carbonyl, CN, halogeno, optionally substituted phenyl, optionally substituted aromatic heterocyclyl, optionally substituted saturated heterocyclyl, optionally substituted saturated heterocyclyloxy or optionally substituted saturated heterocyclylcarbonyl, etc., and the like.Type: ApplicationFiled: July 8, 2011Publication date: May 2, 2013Applicants: UBE INDUSTRIES, LTD., DAIICHI SANKYO COMPANY, LIMITEDInventors: Tsuyoshi Nakamura, Hidenori Namiki, Naoki Terasaka, Akiko Shima, Masahiko Hagihara, Noriaki Iwase, Katsunori Takata, Osamu Kikuchi, Kazunari Tsuboike, Hiroyuki Setoguchi, Kenji Yoneda, Hidetoshi Sunamoto, Koji Ito
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Patent number: 8431572Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.Type: GrantFiled: July 6, 2011Date of Patent: April 30, 2013Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Patent number: 8431578Abstract: Compounds of formula (I) in free or salt or solvate form, where T1, T2, and T3 have the meanings as indicated in the specification, are useful for treating inflammatory or obstructive airways, pulmonary hypertension, pulmonary fibrosis, liver fibrosis, muscle diseases and systemic skeletal disorders. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: January 9, 2009Date of Patent: April 30, 2013Assignee: Novartis AGInventors: Peter Hunt, Catherine Leblanc, Robert Alexander Pulz, Nikolaus Johannes Stiefl
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Patent number: 8426418Abstract: Methods to treat cancer patients, especially melanoma patients, who have BRAF mutations and have become resistant to BRAF mutant kinase inhibitors employ inhibitors of multiple receptor tyrosine kinases. In addition, methods are described for identifying pharmaceutical compositions and drugs that will be successful in treating these patients.Type: GrantFiled: August 26, 2011Date of Patent: April 23, 2013Assignee: CollabRx Inc.Inventors: Robert Coopersmith, Raphael Lehrer
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Patent number: 8426417Abstract: Substituted pyrrolo-pyrimidine 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.Type: GrantFiled: September 25, 2008Date of Patent: April 23, 2013Assignee: Nerviano Medical Sciences S.r.l.Inventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Helena Posteri, Marina Caldarelli, Walter Ceccarelli, Barbara Valsasina
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Publication number: 20130096104Abstract: The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4, R5 and R16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy, as an inhibitor of TYK2 kinase and conditions related, such as inflammatory illnesses, inflammatory bowel disease or psoriasis.Type: ApplicationFiled: March 15, 2011Publication date: April 18, 2013Applicant: GENENTECH, INC.Inventors: Yingjie Lai, Jun Liang, Steven R. Magnuson, Kirk D. Robarge, Vickie H. Tsui, Birong Zhang, Aihe Zhou
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Publication number: 20130096115Abstract: Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from autism.Type: ApplicationFiled: December 21, 2010Publication date: April 18, 2013Applicant: AFRAXIS, INC.Inventors: Jay Lichter, David Campbell, Benedikt Vollrath, Sergio G. Durón
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Publication number: 20130095100Abstract: This invention relates to novel 2-{6-[4-(2-hydroxy-ethyl)-piperazin-1-yl]-2-methyl-pyrimidin-4-ylamino}-thiazole-5-carboxylic acid (2-chloro-6-methyl-phenyl)-amide derivatives, and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by the inhibition of kinases including Src-kinase and Bcr-Abl kinase.Type: ApplicationFiled: December 6, 2012Publication date: April 18, 2013Applicant: Concert Pharmaceuticals, Inc.Inventor: Concert Pharmaceuticals, Inc.
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Publication number: 20130096134Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with pi 105 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelodysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: ApplicationFiled: June 30, 2011Publication date: April 18, 2013Applicant: Amgen Inc.Inventors: Jason A. Duquette, Brian Lucas
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Patent number: 8420630Abstract: The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterized by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.Type: GrantFiled: February 24, 2010Date of Patent: April 16, 2013Assignees: Boehringer Ingelheim Pharma GmbH & Co. KG, Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Georg Dahmann, Frank Himmelsbach, Bernd Krist, Martin Lenter, Alexander Pautsch, Gisela Schnapp, Martin Steegmaier, Helmut Wittneben, Anthony S. Prokopowicz, Walter Spevak, Andreas Schoop, Steffen Steurer
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Publication number: 20130085145Abstract: The present invention provides a pharmaceutical tablet, comprising Imatinib in an amount of 50-75% w/w of the total tablet weight and comprising at least one pharmaceutically acceptable excipient without a binding agent and the process for preparation of the same.Type: ApplicationFiled: January 10, 2011Publication date: April 4, 2013Applicant: SUVEN LIFE SCIENCES LIMITEDInventor: Ravula Sayisiva Prasad
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Publication number: 20130085131Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with pi 110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LympType: ApplicationFiled: June 30, 2011Publication date: April 4, 2013Applicant: Amgen Inc.Inventors: Minna Bui, Benjamin Fisher, Xiaolin Hao, Brian Lucas
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Publication number: 20130072485Abstract: The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.Type: ApplicationFiled: November 6, 2012Publication date: March 21, 2013Applicants: Dana-Farber Cancer Institute, Inc., Whitehead Institute for Biomedical ResearchInventors: Whitehead Institute for Biomedical Research, Dana-Farber Cancer Institute, Inc.
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Publication number: 20130072497Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.Type: ApplicationFiled: November 14, 2012Publication date: March 21, 2013Applicant: Dow AgroSciences LLCInventor: Dow AgroSciences LLC
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Publication number: 20130065899Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: November 2, 2012Publication date: March 14, 2013Applicant: CELGENE AVILOMICS RESEARCH, INC.Inventor: Celgene Avilomics Research, Inc.
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Publication number: 20130065858Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: ApplicationFiled: October 22, 2012Publication date: March 14, 2013Applicants: SUNESIS PHARMACEUTICALS, INC., MILLENNIUM PHARMACEUTICALS, INC.Inventors: MILLENNIUM PHARMACEUTICALS, INC., SUNESIS PHARMACEUTICALS, INC.
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Publication number: 20130064815Abstract: Compositions comprising an autophagy inhibitor and at least one of an NADPH modulator or a glutathione inhibitor are provided. Methods of inhibiting or killing a quiescent cell are provided. Methods of treating cancer are provided. Methods of identifying compositions that inhibit or kill quiescent cells are provided. Methods of identifying compositions that inhibit or kill quiescent cells are provided. Methods of inducing apoptosis are provided. Methods of sensitizing quiescent cells to proteasome inhibitors are provided.Type: ApplicationFiled: September 12, 2012Publication date: March 14, 2013Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventor: Hilary Coller
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PYRIDYLTHIAZOLE-BASED UREAS AS INHIBITORS OF RHO ASSOCIATED PROTEIN KINASE (ROCK) AND METHODS OF USE
Publication number: 20130059839Abstract: Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.Type: ApplicationFiled: April 18, 2011Publication date: March 7, 2013Applicant: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.Inventors: Nicholas J. Lawrence, Roberta Pireddu, Said M. Sebti -
Publication number: 20130059858Abstract: Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, where-in A, L, m, n, o, p, R2, R3, R3, R4 and R5 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: ApplicationFiled: May 4, 2011Publication date: March 7, 2013Applicant: Bristol-Myers Squibb CompanyInventors: Xiang-Yang Ye, Dean A. Wacker, Jeffrey A. Robl
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Publication number: 20130059830Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.Type: ApplicationFiled: May 16, 2011Publication date: March 7, 2013Inventors: Fa-Xiang Ding, Jinlong Jiang, Dong-Ming Shen, Zhi-Cai Shi, Min Shu, Cangming Yang
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Publication number: 20130059824Abstract: Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from Mild Cognitive Impairment.Type: ApplicationFiled: November 23, 2010Publication date: March 7, 2013Applicant: AFRAXis, Inc.Inventors: Jay Lichter, David Campbell, Benedikt Vollrath, Sergio G. Durón
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Publication number: 20130053345Abstract: Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: ApplicationFiled: May 4, 2011Publication date: February 28, 2013Inventors: Xiang-Yang Ye, Dean A. Wacker, Jeffrey A. Robl, Ying Wang
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Publication number: 20130053383Abstract: Herein are disclosed indazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: May 5, 2011Publication date: February 28, 2013Inventors: Celine Duquenne, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
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Patent number: 8377924Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: January 21, 2010Date of Patent: February 19, 2013Assignee: Rigel Pharmaceuticals Inc.Inventors: Rajinder Singh, Huí Li, Haoran Zhao, Rao Kolluri, Kin Tso, John Ramphal, Shihai Gu, Carlos Valdez, Jing Zhang, Emily Stauffer, Matthew Duncton, Salvador Alvarez
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Publication number: 20130040957Abstract: The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives, enantiomers, diastereomers, solvates and pharmaceutical salts thereof, and their uses in the treatment, prevention and modulation of various diseases including chronic liver diseases, liver cirrhosis, liver fibrosis, hepatocellular carcinoma, liver cancer, renal cell carcinoma, kidney cancer, colorectal cancer, brain cancer, breast cancer, blood cancer, lung cancer, thyroid cancer, ovarian cancer, pancreas cancer, prostate cancer, stomach cancer, testicular cancer, uterus cancer, intestinal cancer, skin cancer, and other forms of cancer, carcinoid tumors, teratocarcinoma, tumor progression, metastasis and fibrosis in the neuroendocrine neoplasia, fibrotic processes as well as a disease state modulated directly or indirectly with 5-HT receptors, 5-HT1, 5-HT1A, 5-HT2 receptors, 5-HT2A and 5-HT2B receptors, dopamine receptors and multiple kinase pathways.Type: ApplicationFiled: October 12, 2012Publication date: February 14, 2013Inventor: Daljit Singh Dhanoa
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Publication number: 20130040930Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: April 27, 2011Publication date: February 14, 2013Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
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Publication number: 20130039885Abstract: The present invention relates to methods for preventing or treating Human Immunodeficiency Virus (HIV) infection, inflammatory conditions, and graft-versus-host-disease (GVHD) in a subject. Therapeutic compositions of the present invention comprise Leukocidin E (LukE) and/or D proteins or polypeptides. The invention further relates to methods of treating Staphylococcus aureus infection by administering a composition comprising a CCR5 antagonist or any molecule that blocks LukE/D interaction with CCR5+ cells in an amount effective to treat the S. aureus infection in the subject.Type: ApplicationFiled: June 19, 2012Publication date: February 14, 2013Applicant: NEW YORK UNIVERSITYInventors: Victor J. TORRES, Derya UNUTMAZ, Francis ALONZO, III
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Publication number: 20130040958Abstract: Methods for making Imatinib mesylate of formula (I): having low levels of organic solvent are provided. Also provided are alpha and beta forms of Imatinib mesylate and methods for treating conditions such as chronic myelogenous leukaemia by administering same.Type: ApplicationFiled: July 11, 2012Publication date: February 14, 2013Applicant: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Ennio GRENDELE, Marco GALVAGNI
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Patent number: 8367674Abstract: This invention relates to novel compounds that are piperazine derivatives, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel piperazine compounds that are derivatives of the chemokine CCR5 receptor antagonist, vicriviroc. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering chemokine CCR5 receptor antagonists, such as vicriviroc. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving vicriviroc.Type: GrantFiled: April 17, 2009Date of Patent: February 5, 2013Assignee: CoNCERT Pharmaceuticals, Inc.Inventors: Julie F. Liu, Rose Persichetti