Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/393)
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Publication number: 20140364470Abstract: The invention relates to a phosphate salt or a nitrate salt of 4-(R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl-3-fluoro-benzonitrile, especially in crystalline form, and specific forms of these salts, as well as related invention embodiments. The salts and salt forms allow for the prophylactic and/or therapeutic treatment of aldosterone synthase and/or aromatase mediated diseases or disorders.Type: ApplicationFiled: January 15, 2013Publication date: December 11, 2014Applicant: Novartis AGInventors: Paul Alan Sutton, Eric Loeser
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Publication number: 20140357621Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.Type: ApplicationFiled: August 14, 2014Publication date: December 4, 2014Applicant: Novartis AGInventors: Gary Michael Ksander, Erik Meredith, Lauren Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
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Patent number: 8895599Abstract: The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: June 28, 2013Date of Patent: November 25, 2014Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Irina Neagu, Michael Ohlmeyer, Vidyadhar M. Paradkar, Kurt W. Saionz, Koushi Iwata, Takashi Okamura, Tadao Shibutani
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Patent number: 8895597Abstract: The additive effect of combined intracranial carmustine (“BCNU”) with intracranial temozolomide (“TMZ”), and particularly in combination with radiation (“XRT”), in the treatment of two rat intracranial glioma models, the 9L gliosarcoma and the F98 glioma, demonstrates that local delivery of both drugs, especially in combination with radiation, is far more effective than delivery of either drug alone or one systemically and one locally, either with or without radiation. The triple therapy showed a significant improvement in survival when compared to controls (p=0.0004), local BCNU (p=0.0043), oral TMZ (p=0.0026), local TMZ (p=0.0105), and the combinations of either BCNU and XRT (p=0.0378) or oral TMZ and local BCNU (p=0.0154).Type: GrantFiled: June 17, 2011Date of Patent: November 25, 2014Inventors: Violette Renard Recinos, Betty Tyler, Sarah Brem Sunshine, Henry Brem
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Publication number: 20140343045Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: ApplicationFiled: May 23, 2014Publication date: November 20, 2014Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Patent number: 8883826Abstract: The present invention relates to novel compounds of formula I wherein W, n, X and W? are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.Type: GrantFiled: December 20, 2011Date of Patent: November 11, 2014Assignee: Addex Pharma SAInventors: Anne-Sophie Bessis, Christelle Bolea, Beatrice Bonnet, Mark Epping-Jordan, Nicolas Poirier, Sonia-Maria Poli, Jean-Philippe Rocher, Yves Thollon
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Patent number: 8865911Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.Type: GrantFiled: March 15, 2013Date of Patent: October 21, 2014Assignee: Astrazeneca ABInventors: Gabor Csjernyik, Sofia Karlstrom, Annika Kers, Karin Kolmodin, Martin Nylof, Liselotte Ohberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Soderman, Britt-Marie Swahn, Stefan Von Berg
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Publication number: 20140309197Abstract: The present invention relates to stabilized pharmaceutical formulations prepared from solutions comprising an antineoplastic compound having a cyclic or non-cyclic hydrazine, triazine, or tetrazine group, or a pharmaceutically acceptable salt thereof, and a stabilizer, wherein the stabilizer is an antioxidant and/or more susceptible to nucleophilic attack than the antineoplastic compound.Type: ApplicationFiled: June 25, 2014Publication date: October 16, 2014Inventors: Mahmoud S. AlSwisi, Mahmoud A.A. Ghannam
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Publication number: 20140308243Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B—Z—W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 16, 2014Publication date: October 16, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Yao-Ling Qiu, Hui Cao, Xiaowen Peng, Zhigang Chen, Yat Sun Or
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Patent number: 8859599Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.Type: GrantFiled: February 11, 2010Date of Patent: October 14, 2014Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
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Patent number: 8853212Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: February 17, 2011Date of Patent: October 7, 2014Assignee: Merck Sharp & Dohme CorpInventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
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Publication number: 20140286931Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventor: Chengzhi Zhang
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Publication number: 20140288059Abstract: PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention.Type: ApplicationFiled: April 25, 2014Publication date: September 25, 2014Applicant: THE PENN STATE RESEARCH FOUNDATIONInventors: Gong Chen, Yanming Wang, Pingxin Li, Jing Hu, Shu Wang, Yuji Wang
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Publication number: 20140288115Abstract: It is discovered that noscapine is effective in treating temozolomide (TMZ)-resistant brain cancer. Provided are compositions and methods of treating brain cancer patients, in particular those that are TMZ-resistant. The patients are treated by administration of a therapeutically effective amount of noscapine or an analog thereof. In certain aspects, TMZ is also administered to the patients. Examples of brain cancers include glioma such as glioblastoma multiforme.Type: ApplicationFiled: June 6, 2014Publication date: September 25, 2014Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Thomas C. Chen, Florence M. Hofman, Stan G. Louie, Axel H. Schonthal, Nicos A. Petasis
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Publication number: 20140275195Abstract: The present invention relates to stabilized pharmaceutical formulations prepared from solutions comprising an antineoplastic compound having a cyclic or non-cyclic hydrazine, triazine, or tetrazine group, or a pharmaceutically acceptable salt thereof, and a stabilizer, wherein the stabilizer is an antioxidant and/or more susceptible to nucleophilic attack than the antineoplastic compound.Type: ApplicationFiled: March 14, 2013Publication date: September 18, 2014Inventors: Mahmoud S. AlSwisi, Mahmoud A.A. Ghannam
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Publication number: 20140256693Abstract: The present invention mainly aims to provide a drug for the prophylaxis or treatment of androgen-independent prostate cancer, which is highly useful as a pharmaceutical agent. The present invention provides a drug for the prophylaxis or treatment of androgen-independent prostate cancer, containing a steroid C17,20 lyase inhibitor, particularly, a compound represented by the formula (I): wherein n is an integer of 1 to 3, and Ar is an aromatic ring optionally having substituent(s), or a salt thereof or a prodrug thereof.Type: ApplicationFiled: February 5, 2014Publication date: September 11, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masuo Yamaoka, Takahito Hara
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Patent number: 8828429Abstract: The present invention relates to a controlled release capsule preparation for oral administration, which contains (i) a granule containing a physiologically active substance which is a compound represented by the formula: wherein n is an integer of 1 to 3, and Ar is an aromatic ring optionally having substituent(s), or a salt thereof, and a hydrophilic polymer, and coated with an enteric coating agent and the like, and (ii) a fluidizer. According to the present invention, a controlled release composition for oral administration of an imidazole derivative, which has steroid C17,20-lyase inhibiting activity and which has remarkably improved sustainability of the blood concentration, is provided.Type: GrantFiled: March 3, 2006Date of Patent: September 9, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Hajime Ishida, Yukihiro Nomura
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Publication number: 20140242190Abstract: Methods for preventing and/or reducing side effects of an anti-cancer agent in a subject in need thereof are disclosed. The method comprises administering to the subject, who is under an anti-cancer agent treatment, a composition comprising a therapeutically effective amount of isolated deoxyelephantopin and/or an analogue thereof; and a pharmaceutically acceptable carrier.Type: ApplicationFiled: May 2, 2014Publication date: August 28, 2014Applicant: Academia SinicaInventors: Lie-Fen SHYUR, Wen-Wan CHAO, Ya-Wen CHENG
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Patent number: 8815918Abstract: There is provided compounds of formula (I): wherein R1, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K) is desired and/or required, and particularly in the treatment of cancer.Type: GrantFiled: April 1, 2010Date of Patent: August 26, 2014Assignee: Centro Nacional de Investigaciones Oncologicas (CNIO)Inventors: Joaquin Pastor Fernández, Guido Kurz, Sonia Martinez Gonzalez
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Patent number: 8815926Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: GrantFiled: January 24, 2013Date of Patent: August 26, 2014Assignee: Novartis AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Lv Liao, Robert Mah, Liang Mao, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Publication number: 20140221338Abstract: The present invention provides compounds of Formula (Ia): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: August 6, 2012Publication date: August 7, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Donald J. P. Pinto, James R. Corte, Paul J. Gilligan, Tianan Fang, Leon M. Smith, II, Yufeng Wang, Wu Yang, William R. Ewing
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Publication number: 20140221442Abstract: The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of glioblastoma multiforme. Dianhydrogalactitol acts as an alkylating agent on DNA that creates N7 methylation. Dianhydrogalactitol is effective in suppressing the growth of cancer stem cells and is active against tumors that are refractory to temozolomide; the drug acts independently of the MGMT repair mechanism.Type: ApplicationFiled: April 4, 2014Publication date: August 7, 2014Applicant: Del Mar PharmaceuticalsInventors: Jeffrey A. Bacha, Dennis Brown, Sandra Dunn, Anne Steinø
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Publication number: 20140205672Abstract: A controlled release composition for oral administration, which comprises a physiologically active substance which is a compound represented by the formula: wherein n is an integer of 1 to 3, and Ar is an aromatic ring which may be substituted, or a salt thereof, and a hydrophilic polymer, or a controlled release composition for oral administration, wherein a core containing the physiologically active substance is coated with a coating layer containing a polymer, is provided.Type: ApplicationFiled: January 17, 2014Publication date: July 24, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Shigeo Yanai, Kazumichi Yamamoto
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Patent number: 8785475Abstract: Lipoic acid derivatives and pharmaceutical formulations containing lipoic acid derivatives are useful in the treatment and prevention of disease characterized by disease cells that are sensitive to lipoic acid derivatives.Type: GrantFiled: April 17, 2008Date of Patent: July 22, 2014Assignee: Cornerstone Pharmaceuticals, Inc.Inventors: Paul Bingham, Tom Kwok, Zuzana Zachar
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Publication number: 20140194477Abstract: The invention relates to phosphorylation inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating cell proliferative disorders, especially cancer.Type: ApplicationFiled: October 8, 2013Publication date: July 10, 2014Applicant: Roswell Park Cancer InstituteInventors: William G. Cance, Vita Golubovskaya, Elena V. Kurenova
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Publication number: 20140179734Abstract: Provided is a transdermal absorption-type patch containing a serotonin receptor antagonist, which has a short transdermal absorption delay time (lag time), and in which the maximum transdermal permeation rate of the drug can be reached within a short time and the drug can disappear from circulating blood rapidly. That is, provided is a patch containing a serotonin receptor antagonist, wherein the patch contains an adhesive layer comprising a non-functional acrylic adhesive, a water-soluble organic amine, a fatty acid ester, and a serotonin receptor antagonist such as granisetron as an active ingredient.Type: ApplicationFiled: July 4, 2012Publication date: June 26, 2014Inventors: Takashi Kamakura, Daiki Takano
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Patent number: 8759400Abstract: The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, this invention relates to compositions and methods for selectively enhancing fungal sensitivity to antifungal compounds.Type: GrantFiled: December 19, 2006Date of Patent: June 24, 2014Assignee: MethylGene Inc.Inventors: Nafsika Georgopapadakou, Wenqi Hu, Nadia Campeol, Jean Bedard, Robert Deziel, Alain Ajamian
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Publication number: 20140171392Abstract: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4) alkyl, or —(C1-C4) alkyl-(C5-C7) aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4) alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10) aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 13, 2013Publication date: June 19, 2014Applicant: Novartis AGInventors: Qi-Ying Hu, Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Christoph Schumacher
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Patent number: 8754121Abstract: Methods for treating melanoma in a subject in need thereof are disclosed. The method comprises administering to the subject a composition comprising a therapeutically effective amount of deoxyelephantopin or an analogue thereof; and a pharmaceutically acceptable carrier. Methods of inhibiting proliferation, migration and/or metastasis of melanoma cells in a subject in need thereof are also disclosed. Also disclosed are methods for reducing side effects of an anti-cancer agent in a subject in need thereof.Type: GrantFiled: August 19, 2011Date of Patent: June 17, 2014Assignee: Academia SinicaInventors: Lie-Fen Shyur, Wen-Wan Chao, Ya-Wen Cheng
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Publication number: 20140162996Abstract: One aspect of the disclosure relates to derivatives of aryl and heterocyclic ureido aryl and heterocyclic carboxamido isobutyric acids, dichlorophenyl urea, curcumin, and 1,3-diazetidine-2,4-dione, and pharmaceutical compositions thereof. The derivatives disclosed herein can modulate development of adipocytes and various cancer cells, including resistant cancer cells and cancer stem cells. Another aspect of the disclosure relates to the use of the derivatives and pharmaceutical compositions disclosed herein in treatment of obesity and various cancers.Type: ApplicationFiled: July 29, 2013Publication date: June 12, 2014Applicant: CITY OF HOPEInventors: Samuel RAHBAR, James L. FIGAROLA, Christopher LINCOLN, David HORNE, Rachael MOONEY, Monika POLEWSKI, George SOMLO, Lixin YANG
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Patent number: 8741904Abstract: Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin ? and rifaximin ? useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.Type: GrantFiled: July 25, 2013Date of Patent: June 3, 2014Assignee: Alfa Wassermann S.p.A.Inventors: Giuseppe Claudio Viscomi, Manuela Campana, Donatella Confortini, Maria Barbanti, Dario Braga
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Patent number: 8741888Abstract: A sleep composition including zolpidem and quetiapine in combination provides a healthy sleep pattern allowing the user to get seven or eight hours sleep. The amount of each ingredient in the combination is lower than the amount usually needed to provide this amount of sleep when the ingredients are being used alone.Type: GrantFiled: November 29, 2010Date of Patent: June 3, 2014Inventor: Carl A. Forest
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Publication number: 20140147411Abstract: In certain embodiments, the disclosure relates to methods of treating cancer comprising administering an effective amount a tyrosine kinase inhibitor in combination with an immunotherapy to a subject in need thereof. In certain embodiments, the disclosure relates to methods of treating cancer comprising: i) analyzing both chromosomes in a cell from a subject for the a V600E mutation of BRAF; and ii) determining if both of the chromosomes contain the V600E mutation, then treating the subject comprising the step of administering an effective amount a tyrosine kinase inhibitor in combination with an immunotherapy to the subject.Type: ApplicationFiled: November 12, 2013Publication date: May 29, 2014Applicants: U.S. GOVERNMENT represented by the UNITED STATES DEPARTMENT OF VETERANS AFFAIRS, EMORY UNIVERSITYInventors: Brian Paul Pollack, Bishu Sapkota, Charles E. Hill
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Publication number: 20140142152Abstract: The invention includes, in part, methods and compounds for treating cancer including, but not limited to gliomas, melanomas, and neuroblastomas. In some embodiments of the invention, a glyceryltriacetate compound is administered to a subject in an amount effective to treat or prevent a cancer in the subject.Type: ApplicationFiled: July 19, 2012Publication date: May 22, 2014Applicant: University of Vermont and State Agricultural CollegeInventor: Diane M. Jaworski
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Publication number: 20140134275Abstract: The invention features compositions and methods that are useful for the treatment of neoplasia (e.g., pancreatic cancer, colon cancer, brain cancer) by increasing DNA damage, reducing nucleotide synthesis, and reducing base excision repair (BER).Type: ApplicationFiled: April 20, 2012Publication date: May 15, 2014Applicant: University of Florida Research FoundationInventors: Satya Narayan, Aruna S. Jaiswal, David A. Ostov, Sukwon Hong
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Patent number: 8722715Abstract: The present application relates to N-chlorinated oxazolidinone, hydantoin and imidazolidinone compounds of Formula I or pharmaceutically acceptable salts thereof, and associated compositions and methods of use as antimicrobial agents.Type: GrantFiled: November 4, 2009Date of Patent: May 13, 2014Assignee: NovaBay PharmaceuticalsInventors: Rakesh K. Jain, Eddy Low, Charles Francavilla, Timothy P. Shiau, Bum Kim, Satheesh K. Nair
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Publication number: 20140127272Abstract: The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of ?-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.Type: ApplicationFiled: October 31, 2013Publication date: May 8, 2014Applicant: Cedars-Sinai Medical CenterInventors: John S. Yu, Bong Seop Lee
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Publication number: 20140121155Abstract: Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.Type: ApplicationFiled: December 27, 2013Publication date: May 1, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Jack Z. Gougoutas, Mary F. Malley, John D. DiMarco, Xiaotian S. Yin, Chenkou Wei, Jurong Yu, Truc Chi Vu, Gregory Scott Jones, Scott A. Savage
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Patent number: 8710052Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: GrantFiled: October 18, 2012Date of Patent: April 29, 2014Assignee: Hydra Biosciences, Inc.Inventor: Jayhong A. Chong
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Publication number: 20140113891Abstract: Methods for treating cancer using compounds that inhibit human DNA ligases. Methods for using compounds that inhibit human DNA ligases to provide insights into the reaction mechanisms of human DNA ligases, for example to identify the human DNA ligase involved in different DNA repair pathways. Screening methods for compounds that inhibit human DNA ligases.Type: ApplicationFiled: April 17, 2013Publication date: April 24, 2014Inventors: Alan E. Tomkinson, Xi Chen, Barbara Dziegielewska, Alexander D. Mackerell, Shijun Zhong, Gerald M. Wilson
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Publication number: 20140112885Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: October 8, 2013Publication date: April 24, 2014Applicant: GILEAD SCIENCES, INC.Inventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James Taylor, Chinh Viet Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
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Patent number: 8703811Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.Type: GrantFiled: May 7, 2009Date of Patent: April 22, 2014Assignees: Genzyme Corporation, Massachusetts Institute of Technology, President and Fellows of Harvard CollegeInventors: Cecilia Bastos, Michael L. Booker, Cassandra A. Celatka, Jon C. Clardy, Joseph Cortese, Vishal P. Patel, Renato Skerlj, Roger C. Wiegand, Dyann F. Wirth
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Publication number: 20140105886Abstract: Glioblastoma multiforme (GBM) is an aggressive form of brain cancer. Biomarkers for GBM that provide prognostic and predictive information are useful because they provide the physician valuable information regarding treatment options for GBM. The present invention provides a method to quantify such biomarkers. Thus, the method relates to the quantification of GSK3?, S6, CREB, PTEN, AKT and mTOR biomarkers and the use of AQUA® analysis to estimate a patient's risk and benefit to treatment using an inhibitor of the AGC-family kinase. Unlike traditional IHC, the AQUA® system is objective and produces quantitative in situ protein expression data on a continuous scale. The present invention uses the AQUA system to provide a robust and standardized diagnostic assay that can be used in a clinical setting to provide prognostic and predictive information.Type: ApplicationFiled: July 9, 2013Publication date: April 17, 2014Inventors: Waldron Donald E., Pinard Robert, Gustavson Mark
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1H-benzimidazole-4-carboxamides substituted with phenyl at the 2-position are potent PARP inhibitors
Patent number: 8697736Abstract: Compound having formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds having formula (I), methods of treatment comprising compounds having formula (I), and methods of inhibiting the PARP enzyme comprising compounds having formula (I).Type: GrantFiled: September 29, 2006Date of Patent: April 15, 2014Assignee: AbbVie Inc.Inventors: Thomas D. Penning, Sheela A. Thomas, Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Vincent L. Giranda -
Publication number: 20140093503Abstract: The present application discloses new taxane analogs, intermediates and methods for producing them. The present application is also directed to pharmaceutical formulations comprising abeo-taxanes and methods of treating cancer with the abeo-taxanes.Type: ApplicationFiled: April 6, 2012Publication date: April 3, 2014Applicant: Arbor Therapeutics, LLCInventors: James D. McChesney, John T. Henry, Sylesh Venkataraman, Mahesh Kumar Gundluru
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Publication number: 20140088166Abstract: 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: ApplicationFiled: December 2, 2013Publication date: March 27, 2014Inventors: Sydney Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Lenore C. Witchey-Lakshmanan
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Publication number: 20140080783Abstract: The present invention relates to the field of oncology and provides compositions and methods for treating specific cancers, including non small cell lung cancer, breast cancer, thyroid cancer, pancreatic cancer, colon cancer, melanoma, hepatoma and adenocarcinoma. Particularly, compositions and methods involving administration, either simultaneously or sequentially, of pharmaceutical combinations comprising (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide with other compounds, to patients suffering from cancer are described.Type: ApplicationFiled: November 18, 2013Publication date: March 20, 2014Applicant: ARDEA BIOSCIENCES, INC.Inventor: Mark CHAPMAN
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Patent number: 8673953Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.Type: GrantFiled: January 6, 2012Date of Patent: March 18, 2014Assignee: Allergan, Inc.Inventors: Stuart D. Shanler, Andrew Ondo
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Publication number: 20140051689Abstract: Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B-C) may be CH2—CH2 etc., (R1) may be phenyl and substituted forms thereof, (R2) may be assorted substituents.Type: ApplicationFiled: October 24, 2013Publication date: February 20, 2014Applicant: Biota Scientific Management Pty Ltd.Inventors: Silas Bond, Vanessa Anne Sanford, John Nicholas Lambert, Chin Yu Lim, Alistair George Draffan, Roland Henry Nearn, Jeffrey Peter Mitchell
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Patent number: 8653260Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: June 20, 2012Date of Patent: February 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu