Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/393)
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Patent number: 8426457Abstract: Methods of improving skin quality are disclosed. Generally, the methods include topically administering an IRM compound to a treatment area of skin for a period of time and in an amount effective for improving the quality of the skin. Suitable IRM compound compounds include agonists of one or more TLRs.Type: GrantFiled: March 12, 2004Date of Patent: April 23, 2013Assignee: Medicis Pharmaceutical CorporationInventors: Richard L. Miller, James H. Lee, Mary L. Owens
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Publication number: 20130096169Abstract: This invention relates to compositions and methods utilizing a chemotherapeutic drug and 6-bromoindirubin3?-oxime (BIO) for the treatment of cancer, including glioblastoma multiforme. The present invention demonstrates that BIO works synergistically with chemotherapeutic drugs to increase the cytotoxic effects of these drugs in glioma cells.Type: ApplicationFiled: December 7, 2012Publication date: April 18, 2013Applicant: CEDARS-SINAI MEDICAL CENTERInventor: CEDARS-SINAI MEDICAL CENTER
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Publication number: 20130096162Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: December 3, 2012Publication date: April 18, 2013Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Publication number: 20130090364Abstract: Compounds represented by formula I or pharmaceutically acceptable salts thereof, wherein A, B, B?, X, Y, R1, R2, R2?, R3, R3?, R4, R4?, R5, R5?m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: September 24, 2012Publication date: April 11, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Patent number: 8415483Abstract: 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: December 20, 2011Date of Patent: April 9, 2013Assignee: AstraZeneca ABInventors: Gabor Csjernyik, Sofia Karlström, Annika Kers, Karin Kolmodin, Martin Nylöf, Liselotte Öhberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Söderman, Britt-Marie Swahn, Stefan Von Berg
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Publication number: 20130084334Abstract: The invention relates to novel pharmaceutical compositions highly dosed with biotin, as well as to the use thereof in treating visual impairments which are related, in particular, to optic atrophy.Type: ApplicationFiled: April 5, 2011Publication date: April 4, 2013Applicant: Assistance Publique - Hopitaux de ParisInventors: Frédéric Sedel, Agnès Bellanger
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Patent number: 8409574Abstract: Provided herein are compounds and methods for the treatment of brain cancer in a mammal, wherein the method comprises the administration to the mammal a compound that stabilizes tubulin dimers or microtubles at G2-M interface during mitosis but is not a substrate for MDR protein. In particular, the present application relates to the use of an orally effective abeo-taxane, alone or in combination with temozolomide or bevacizumab, for the treatment of brain cancer.Type: GrantFiled: August 20, 2010Date of Patent: April 2, 2013Inventors: James D. McChesney, Gilles Tapolsky, David E. Emerson, John Marshall, Tauseef Ahmed, Allen Cohn, Michael Kurman, Manuel Modiano
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Patent number: 8399444Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, processes for their preparation, pharmaceutical compositions containing these compounds, and their use in the treatment of allergic disorders, such as allergic rhinitis and asthma.Type: GrantFiled: December 16, 2009Date of Patent: March 19, 2013Assignee: GlaxoSmithKline Intellectual Property Development Ltd.Inventors: Ian Baxter Campbell, Simon Peace, John Martin Pritchard, Daniel Tape, Robert Charles Wheeler
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Publication number: 20130065893Abstract: The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, R5, R7 and p are defined herein. The invention also relates to 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: November 29, 2010Publication date: March 14, 2013Applicant: NOVARTIS AGInventors: Robert Sun, Lauren G. Monovich, Sylvie Chamoin, John Westbrook
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Patent number: 8394968Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: July 29, 2010Date of Patent: March 12, 2013Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey Lee Romine
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Publication number: 20130059018Abstract: This invention relates to the use of phytocannabinoids, either in an isolated form or in the form of a botanical drug substance (BDS) in the treatment of cancer. Preferably the cancer to be treated is cancer of the prostate, cancer of the breast or cancer of the colon.Type: ApplicationFiled: March 11, 2011Publication date: March 7, 2013Applicants: OTSUKA PHARMACEUTICAL CO., LIMITED, GW PHARMA LIMITEDInventors: Daniela Parolaro, Paola Massi, Angelo Antonio Izzo, Francesca Borelli, Gabriella Aviello, Vincenzo Di Marzo, Luciano De Petrocellis, Aniello Schiano Moriello, Alessia Ligresti, Ruth Alexandra Ross, Lesley Ann Ford, Sharon Anavi-Goffer, Manuel Guzman, Guillermo Velasco, Mar Lorente, Sofia Torres, Tetsuro Kikuchi, Geoffrey Guy, Colin Stott, Stephen Wright, Alan Sutton, David Potter, Etienne De Meijer
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Patent number: 8389558Abstract: The present invention is directed to pharmaceutical compositions comprising bendamustine and one or more amphiphilic anionic compounds and self assembled aggregates, which aggregates exhibit enhanced stability in aqueous solutions, including plasma, are disclosed. The unexpectedly enhanced stability afforded by such aggregates permits patients to be treated with bendamustine in lower and/or with less frequent dosages or to improve its therapeutic effect while using the same as presently used treatment protocol.Type: GrantFiled: July 19, 2010Date of Patent: March 5, 2013Assignee: Supratek Pharma Inc.Inventors: Valery Alakhov, Grzegroz Pietrzynski, Patel Kishore, Thomasz Popek
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Patent number: 8389554Abstract: Novel imidazo[2,1-b][1,3,4]thiadiazole derivatives of formula (I) wherein R1 and R2 have the meaning according to claim 1, are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: July 1, 2009Date of Patent: March 5, 2013Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Guenter Hoelzemann, Hartmut Greiner, Emilie Rossignol, Dominique Swinnen
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Patent number: 8383663Abstract: The present invention is directed to pharmaceutical compositions including: (a) bendamustine, (b) a first charged cyclopolysaccharide, and (c) a stabilizing agent which is a second charged cyclopolysaccharide having a charge opposite to that of the first charged cyclopolysaccharide. The composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. The compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.Type: GrantFiled: February 22, 2011Date of Patent: February 26, 2013Assignee: Supratek Pharma Inc.Inventors: Valery Alakhov, Grzegorz Pietrzynski, Patel Kishore, Thomasz Popek
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Publication number: 20130045957Abstract: Provided herein are methods for preventing and/or reducing the severity of drug induced ototoxicity. Provided herein are methods for recovery from hearing loss due to drug-induced ototoxicity.Type: ApplicationFiled: February 16, 2012Publication date: February 21, 2013Applicant: Otonomy, Inc.Inventors: Fabrice Piu, Qiang Ye, Luis Dellamary, Carl Lebel
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Patent number: 8377945Abstract: This disclosure concerns compounds which are useful as inhibitors of spleen tyrosine kinase (Syk) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of Syk. This disclosure also relates to pharmaceutical compositions containing 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: June 14, 2010Date of Patent: February 19, 2013Assignee: Rigel Pharmaceuticals Inc.Inventors: Jing Zhang, Rajinder Singh, Dane Goff, Taisei Kinoshita
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Publication number: 20130030237Abstract: Provided herein are pharmaceutical compositions and methods of treating cancer wherein the cytotoxic activity of an anticancer agent is potentiated by the combination of base excision repair (BER) pathway inhibitors.Type: ApplicationFiled: April 15, 2011Publication date: January 31, 2013Inventor: Charles Theuer
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Publication number: 20130029964Abstract: An object of the present invention is to provide a novel low molecular weight compound exhibiting an osteogenesis-promoting action. This object is achieved by a compound having the general formula (I) or a pharmacologically acceptable salt thereof. In the general formula (I), R1 and R2 represent hydrogen atoms, and the like; R3 represents a hydrogen atom, and the like; X, Y, and Z represent nitrogen atoms, and the like; A represents a phenylene group, and the like; n represents 1 or 2, and the like; and V and W represent oxygen atoms, and the like.Type: ApplicationFiled: August 27, 2012Publication date: January 31, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kazumasa Aoki, Satoshi Matsui, Kenji Yoshikawa, Hiroki Shimizu, Junko Sasaki, Katsuyoshi Nakajima, Osamu Kanno, Kiyoshi Oizumi
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Publication number: 20130028989Abstract: Targeting uncontrolled cell proliferation and resistance to DNA damaging chemotherapeutics with at least one reagent has significant potential in cancer treatment. Replication Protein A, the eukaryotic single-strand (ss) DNA binding protein, is essential for genomic maintenance and stability via roles in both DNA replication and repair. Reported herein are small molecules that inhibits the in vitro, in vivo, and cellular ssDNA binding activity of RPA, thereby disrupting the eukaryotic cell cycle, inducing cytotoxicity and increasing the efficacy of chemotherapeutic agents damage DNA, and/or disrupt its replication and/or function. These results provide new insights into the mechanism of RPA-ssDNA interactions in chromosome maintenance and stability. This represents a molecularly targeted eukaryotic DNA binding inhibitor and demonstrates the utility of targeting a protein-DNA interaction as a means of studying the cell cycle and providing a therapeutic strategy for cancer treatment.Type: ApplicationFiled: February 5, 2011Publication date: January 31, 2013Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventors: John J. Turchi, Sarah Shuck
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Publication number: 20130023574Abstract: Provided are a method for generating a data set for integrated proteomics analysis, whereby expression level variations of both of proteins and genes can be integrally united together and, moreover, highly accurate and appropriate analysis results can be obtained compared with the existing cases where the expression variation amount of proteins or genes is singly analyzed, an integrated proteomics analysis method, a method for identifying a protein causative of a disease or the like using these methods, and a method of using the same???.Type: ApplicationFiled: March 31, 2011Publication date: January 24, 2013Applicant: National University Corporation Kumamoto UniversityInventors: Norie Araki, Souhei Mizuguchi, Daiki Kobayashi, Nobuyuki Tsubota, Takashi Morikawa, Junichi Kuratsu, Masayo Wilson Morifuji
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Patent number: 8354434Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: GrantFiled: January 15, 2007Date of Patent: January 15, 2013Assignee: Purdue Pharma L.P.Inventor: Xiaoming Zhou
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Publication number: 20130011483Abstract: Formulations of mazindol having superior stability and methods of administering same are provided. The formulations may be immediate, enhanced, or otherwise delayed release formulations of mazindol.Type: ApplicationFiled: March 30, 2011Publication date: January 10, 2013Inventors: Argaw Kidane, Padmanabh P. Bhatt
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Publication number: 20130004481Abstract: The invention describes anti-cancer therapies comprising using dual Aurora kinase/MEK inhibitors as described herein.Type: ApplicationFiled: January 5, 2012Publication date: January 3, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Flavio Solca, Ulrich Guertler, Michael Sanderson, Ulrike Tontsch-Grunt, Irene Waizenegger
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Publication number: 20120316150Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1, R2, R3, R4, R5 and R6 are as defined herein: and compositions, processes for the preparation, and uses thereof, e.g. in the treatment of endometriosis or uterine fibroids.Type: ApplicationFiled: June 18, 2012Publication date: December 13, 2012Inventors: KARL RICHARD GIBSON, Martin Peter Green, Toby James Underwood, Florian Wakenhut
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Publication number: 20120308668Abstract: The present invention relates to the field of human health, and more particularly to the treatment of attention deficit/hyperactivity disorder (ADHD) with mazindol. The latter can be administered as monotherapy or in combination with one or more compounds, including psychostimulants, for the indication of ADHD and associated or co-morbid symptoms.Type: ApplicationFiled: August 21, 2012Publication date: December 6, 2012Applicant: ASSISTANCE PUBLIQUE-HOPITAUX DE PARISInventor: Eric Konofal
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Publication number: 20120302615Abstract: The invention comprises a method of treatment of CNS disorders by a pharmaceutical agent exhibiting combined noradrenergic, serotonergic or dopaminergic reuptake transporter inhibitory and ?-opioid agonistic activity.Type: ApplicationFiled: December 2, 2010Publication date: November 29, 2012Inventor: Christopher D. Breder
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Patent number: 8318728Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: GrantFiled: May 14, 2009Date of Patent: November 27, 2012Assignee: Hydra Biosciences, Inc.Inventor: Jayhong A. Chong
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Publication number: 20120295888Abstract: 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: January 13, 2011Publication date: November 22, 2012Inventors: Qi-Ying Hu, Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Christoph Schumacher
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Patent number: 8314097Abstract: 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: GrantFiled: August 23, 2006Date of Patent: November 20, 2012Assignee: Novartis AGInventors: Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
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Patent number: 8314134Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.Type: GrantFiled: March 5, 2010Date of Patent: November 20, 2012Assignee: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Jun Jiang, Hao Li, David James, Dinesh Chimmanamada, Christopher Borella, Lijun Sun, Yu Xie, Mats Holmqvist, Jerome Mahiou, Zhiqiang Xia
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Publication number: 20120283304Abstract: The present invention relates to a parenteral formulation of Temozolomide comprising an excipient selected from the group consisting of bulking agents, buffers, pH adjusting agents, with the proviso that the formulation is free of dissolution enhancing agents.Type: ApplicationFiled: December 22, 2010Publication date: November 8, 2012Applicant: SAHAJ LIFE SCIENCES PVT. LTD.Inventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty
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Publication number: 20120282179Abstract: Methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments are described, wherein R1 is halo; R2 is halo; and Q is CH or N.Type: ApplicationFiled: August 6, 2010Publication date: November 8, 2012Applicant: Exelixis, Inc.Inventors: Dana T. Aftab, Thomas Mueller, Aaron Weitzman, Jaymes Holland
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Patent number: 8304409Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.Type: GrantFiled: December 11, 2009Date of Patent: November 6, 2012Assignee: Nicox S.A.Inventors: Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
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Publication number: 20120277217Abstract: Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.Type: ApplicationFiled: October 27, 2010Publication date: November 1, 2012Applicant: NewLink Genetics CorporationInventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Xiaoxia Zhang
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Publication number: 20120277240Abstract: 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: ApplicationFiled: February 17, 2011Publication date: November 1, 2012Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
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Publication number: 20120277215Abstract: 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: July 2, 2012Publication date: November 1, 2012Inventors: Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
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Patent number: 8299079Abstract: This application relates to the use of one or more parasympathomimetic drugs in combination with one or more alpha agonists to create optically beneficial miosis to, for example, temporarily treat presbyopia. The invention provides a pharmaceutical preparation comprising a therapeutically effective amount of one or more parasympathomimetic drugs or cholinesterase inhibitors, or a pharmaceutically acceptable salt thereof, in combination with one or more alpha agonists or antagonists, or a pharmaceutically acceptable salt thereof. The invention further provides for a method for treating, ameliorating or reducing presbyopia of a patient having an eye, comprising administering to said eye a pharmaceutically effective amount of the ophthalmic preparation.Type: GrantFiled: December 20, 2010Date of Patent: October 30, 2012Inventor: Herbert E. Kaufman
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Patent number: 8299109Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available ALDARA 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for ALDARA 5% imiquimod cream to treat actinic keratosis are also disclosed and described.Type: GrantFiled: July 13, 2011Date of Patent: October 30, 2012Assignee: Medicis Pharmaceutical CorporationInventors: Michael T. Nordsiek, Sharon F. Levy, James H. Lee, James H. Kulp, Kodumudi S. Balaji, Tze-Chiang Meng, Jason J. Wu, Valyn S. Bahm, Robert Babilon
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Publication number: 20120270899Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a cardiovascular disease in an individual using such pharmaceutical compositions.Type: ApplicationFiled: February 3, 2012Publication date: October 25, 2012Inventors: Robin Mark Bannister, John Brew, Suzanne Jane Dilly, Gregory Alan Stoloff, Wilson Caparros-Wanderley
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Patent number: 8293779Abstract: The present invention relates to the field of human health, and more particularly to the treatment of attention deficit/hyperactivity disorder (ADHD) with mazindol. The latter can be administered as monotherapy or in combination with one or more compounds, including psychostimulants, for the indication of ADHD and associated or co-morbid symptoms.Type: GrantFiled: April 11, 2007Date of Patent: October 23, 2012Assignee: Assistance Publique-Hopitaux de ParisInventor: Eric Konofal
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Publication number: 20120264752Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: June 22, 2012Publication date: October 18, 2012Applicant: THERAVANCE, INC.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Patent number: 8288424Abstract: Substituted tetrahydroimidazopyridine compounds corresponding to formula I: in which R1, R2 and R3 have defined meanings, processes for preparing such compounds, pharmaceutical compositions containing such compounds, and the use of such compounds for treating or inhibiting pain, epilepsy, migraine, anxiety or urinary incontinence.Type: GrantFiled: January 21, 2009Date of Patent: October 16, 2012Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Stefan Oberboersch, Sven Kuehnert, Gregor Bahrenberg, Achim Kless
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Publication number: 20120258181Abstract: The present invention relates to combinations between artemisinin-based potent anti-malarial agents, selected from the group consisting of ART, DHA and ARM, and a further chemotherapeutic drug selected from the group consisting of a camptothecin derivative, or a PARP-1 inhibitor, or an intercalating DNA agent, or an alkylating agent. Such combinations, showed medium to strong synergism in various models of cancer, in particular in NSCL.Type: ApplicationFiled: December 6, 2010Publication date: October 11, 2012Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.Inventors: Claudio Pisano, Loredana Vesci
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Publication number: 20120258992Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: June 19, 2012Publication date: October 11, 2012Applicant: THERAVANCE, INC.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20120252856Abstract: The present invention relates to methods of dividing cancer into subgroups based upon Akt pathway gene expression. In one embodiment, the present invention provides a method of diagnosing glioblastoma multiforme (GBM) subtype in an individual by determining the presence of an abnormal expression of an Akt pathway gene cluster and diagnosing the cancer subtype in the individual.Type: ApplicationFiled: December 10, 2010Publication date: October 4, 2012Applicant: Dignity HealthInventors: Anna Joy, Burt G. Feuerstein, Ivan Smimov
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Publication number: 20120245126Abstract: Nitromethylene analogues of imidacloprid and divalent and oxabridged heterocyclic neonicotinoid compounds constructed by dialdehydes, preparation methods and uses thereof are disclosed. Compounds represented by formula (A) or (B), their optical isomers or agrochemically acceptable salts are provided. Agrochemical compositions comprising the said compounds, their optical isomers or agrochemically acceptable salts, the uses of the said agrochemical compositions and the preparation methods of the said compounds, their optical isomers or agrochemically acceptable salts are also disclosed. The compounds and their derivatives have high insecticidal activities to several farming and forestry pests including homoptera and lepidoptera pests, such as aphis, fulgorid, whitefly, leafhopper, common thrips, cotton bollworm, cabbage caterpillar, cabbage moth, cotton leafworm and armyworm.Type: ApplicationFiled: December 9, 2010Publication date: September 27, 2012Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Xuhong Qian, Zhong Li, Xusheng Shao, Xiaoyong Xu, Zhiping Xu, Gonghua Song
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Publication number: 20120237502Abstract: The present invention relates to a method for the prevention or treatment of certain breast cancers or ovarian cancer comprising administering to a patient in need thereof of a therapeutically effective amount of a 17,20-lyase inhibitor, wherein the breast cancer or ovarian cancer is estrogen receptor (ER) negative.Type: ApplicationFiled: November 18, 2011Publication date: September 20, 2012Applicant: Takeda Pharmaceutical Company LimitedInventor: James W. Darnowski
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Publication number: 20120230989Abstract: This document provides methods and materials related to treating renal cell carcinoma. For example, methods and materials for assessing a cancer patient (e.g., a renal cell carcinoma patient) for tumor or peritumoral tissue containing CD14+ cells and proceeding with a cancer treatment option (e.g., a renal cell carcinoma treatment option) based on the presence, absence, or level of CD14+ cells present within the tumor or peritumoral tissue are provided.Type: ApplicationFiled: November 8, 2010Publication date: September 13, 2012Applicant: MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCHInventor: Allan B. Dietz
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Patent number: 8263615Abstract: Heterocyclic compounds of the general formula (I) are provided in which R, R1, R2, R3, R4 and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldostereone synthase inhibitors,Type: GrantFiled: October 8, 2010Date of Patent: September 11, 2012Assignee: Novartis AGInventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Michael Quirmbach, Christiane Marti, Aleksandar Stojanovic, Stefan Stutz
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Publication number: 20120220640Abstract: The present invention relates to computer-implemented methods and system for analysing a biomarker which cycles in a subject. In some other aspects, the present invention relates to analysing a biomarker which at least initially increases or decreases in amount in a subject following a treatment for a disease. In further aspects, the present invention relates to computer-implemented methods and systems for determining a preferred time to administer a therapy to treat a disease in a subject. The present invention also relates to computer program product to implement the methods. Further, the present invention relates to methods of determining the timing of treating a disease in a subject in which the immune system is cycling.Type: ApplicationFiled: May 27, 2010Publication date: August 30, 2012Applicant: IMMUNAID PTY LTDInventors: Martin Leonard Ashdown, Andrew Robinson