Nitrogen Bonded Directly To Ring Carbon Of The Purine Ring System (e.g., Adenine, Etc.) Patents (Class 514/263.4)
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Patent number: 8809351Abstract: The present invention relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib.Type: GrantFiled: February 6, 2013Date of Patent: August 19, 2014Assignee: Innovative Med Concepts, LLC.Inventor: William L. Pridgen
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Patent number: 8809350Abstract: The present invention relates to the use of an inhibitor of CDK2 and/or CDK7 and/or CDK9, or a pharmaceutically acceptable salt thereof, in the preparation of a medicament for treating a disease associated with antinuclear antibodies, wherein the inhibitor of CDK2 and/or CDK7 and/or CDK9 or pharmaceutically acceptable salt thereof is administered in an amount sufficient to down-regulate the levels of antinuclear antibodies. A further aspect of the invention relates to a combination comprising an inhibitor of CDK2 and/or CDK7 and/or CDK9, or a pharmaceutically acceptable salt thereof, and methylprednisolone, and its use in the treatment of diseases associated with antinuclear antibodies, such as SLE.Type: GrantFiled: May 4, 2012Date of Patent: August 19, 2014Assignee: Cyclacel LimitedInventors: Ariela Benigni, Carla Zoja, Giuseppe Remuzzi, Athos Gianella-Borradori
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Publication number: 20140228378Abstract: The invention provides novel substituted cyclopropane carboxamide compounds according to Formula (I), their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.Type: ApplicationFiled: July 7, 2012Publication date: August 14, 2014Applicant: MERCK PATENT GMBHInventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann
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Publication number: 20140221366Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: June 11, 2012Publication date: August 7, 2014Applicant: MERCK PATENT GMBHInventors: Timo Heinrich, Nadia Brugger, Kristopher Josephson
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Publication number: 20140221399Abstract: The present invention relates to methods of treating fibromyalgia by administering a therapeutically-effective combination-dosage of famciclovir and celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination-dosage of famciclovir and celecoxib.Type: ApplicationFiled: April 11, 2014Publication date: August 7, 2014Applicant: INNOVATIVE MED CONCEPTS, LLCInventor: William L. Pridgen
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Publication number: 20140213559Abstract: The present invention provides an inhibitor of intracellular protein degradation for use in the treatment and prevention of muscular dystrophy in a mammal. In particular, the invention provides an autophagy inhibitor and/or an inhibitor of the ubiquitin-proteasome system (such as a proteasome inhibitor) for use in the treatment and prevention of muscular dystrophy (such as congenital muscular dystrophy [e.g. MDC1A) and Duchenne muscular dystrophy [DMD]). The invention further provides corresponding methods of treatment and prevention of muscular dystrophy.Type: ApplicationFiled: May 27, 2011Publication date: July 31, 2014Applicant: MD PHARMA ABInventors: Madeleine Durbeej-Hjalt, Virginie Carmingnac
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Publication number: 20140206697Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.Type: ApplicationFiled: March 26, 2014Publication date: July 24, 2014Applicant: Signal Pharmaceuticals, LLCInventors: STEVEN CLAREEN, VERONIQUE PLANTEVIN-KRENITSKY, MOORTHY PALANKI, YOSHITAKA SATOH
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Publication number: 20140200229Abstract: Disclosed are compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating inflammatory skin diseases.Type: ApplicationFiled: December 28, 2012Publication date: July 17, 2014Applicant: CELLCEUTIX CORPORATIONInventor: KRISHNA MENON
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Publication number: 20140179689Abstract: The subject invention concerns materials and methods for treating diseases and disorders associated with expression of Rho associated kinases (ROCKs). Examples of diseases and disorders contemplated within the scope of the invention include, but are not limited to, oncological disorders, cardiovascular diseases, CNS disorders, and inflammatory disorders. In one embodiment, a method of the invention comprises administering a therapeutically effective amount of one or more compounds of the present invention, or a composition comprising the compounds, to a person or animal in need of treatment. The subject invention also concerns compounds that inhibit ROCKs, and compositions that comprise the inhibitor compounds of the invention. Compounds contemplated within the scope of the invention include, but are not limited to, those compounds shown in Table 5.Type: ApplicationFiled: March 30, 2012Publication date: June 26, 2014Applicant: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.Inventors: Nicholas J. Lawrence, Said M. Sebti, ROBERTA PIREDDU
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Publication number: 20140178337Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.Type: ApplicationFiled: December 19, 2013Publication date: June 26, 2014Inventors: George D. Hartman, Osvaldo A. Flores
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Publication number: 20140170112Abstract: In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising a combination regimen of at least two active ingredients designed to diminish systemic inflammation by targeting (inhibiting) two different, but convergent, signaling pathways, i.e., the sympathetic nervous system and the lipid-derived autacoid system; and methods for making and using these compositions. In alternative embodiments, the compositions of the invention (e.g., the combination of drugs) are used to ameliorate, diminish, treat, block or prevent an inflammatory response secondary to an infection, e.g., a viral infection and/or a reactivation.Type: ApplicationFiled: March 8, 2012Publication date: June 19, 2014Applicant: VICUS THERAPEUTICS, LLCInventors: John Maki, Newell Bascomb, Timothy J. Turner, Fredric Young
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Publication number: 20140163047Abstract: The present invention refers to a composition of a ceramic matrix defined by pseudoboehmite nanoparticles and constructed for carrying and releasing medications in a controlled manner, in the treatment of human beings and animals presenting an organic deficiency which requires the application of said medications. The present invention further refers to the method for preparing said composition, in the form of a ceramic matrix, and also to the method of incorporating the drug acyclovir to said ceramic matrix, forming a tablet.Type: ApplicationFiled: December 4, 2013Publication date: June 12, 2014Applicant: Instituto Presbiteriano MackenzieInventors: Antonio Hortencio Munhoz, JR., Richard Wagner Novickis, Leila Figueiredo De Miranda, Sonia Braunstein Faldini, Mauro Cesar Terence, Roberto Rodrigues Ribeiro
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Publication number: 20140148410Abstract: Disclosed are nucleopeptide compounds that include a nucleobase, and an amino acid. Certain compounds further comprise a glycoside. The compounds may self-assemble to form supramolecular hydrogels. Also, the compounds may be used as a platform to examine specific biological functions (e.g., binding to DNA and RNA) of a dynamic supramolecular system that is able to interact with both proteins and nucleic acids. Other uses include: methods of growing cells and methods of delivering a substance to a cell.Type: ApplicationFiled: December 2, 2013Publication date: May 29, 2014Applicant: Brandeis UniversityInventor: Bing Xu
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Publication number: 20140148496Abstract: ATM kinase is shown to regulate proteasome-mediated protein turnover through suppression of the expression of the ubiquitin-like protein ISG15 (Interferon Stimulated Gene 15). Silencing of the ISG15 pathway restored both the ubiquitin and autophagy pathways, and the UV-mediated degradation of their substrates in A-T cells. The ATM kinase negatively regulates the ISG15 pathway, and the constitutively elevated ISG15 pathway induces proteinopathy in A-T cells, and in A-T patients. These findings indicate that proteasome-mediated protein degradation is impaired in A-T cells due to elevated expression of the ISG15 conjugation pathway, which contributes to progressive neurodegeneration in A-T patients. The ISG15 pathway is a new target for both detection and treatment of A-T Inhibitors if ISG15 expression can be used to inhibit or attenuate neurodegeneration in A-T patients.Type: ApplicationFiled: November 29, 2012Publication date: May 29, 2014Inventor: Shyamal D. Desai
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Publication number: 20140134239Abstract: A composition and method for the treatment of the side-effects associated with the administration of cancer chemotherapeutic agents involves the oral ingestion of a slow release capsule containing adenine. In some embodiments, the slow release capsule also contains orotate. The systemic administration of a proton pump inhibitor decreases systemic absorption of orotate, and the systemic administration of allopurinol decreases the formation of 2,8-dihydroxy adenine from adenine. In an alternative embodiment, cationic liposomes contain purine/pyrimidine precursors. The cationic liposomes bind to the cells lining the mucosa of the intestinal tract and then the contents of the cationic liposome are then taken up in the interior of the cells to prevent the metabolism of the cancer treatment drug 5-FU into a toxic species. A method for prevention of oral stomatitis and a method for treatment of dysplastic tissue are also disclosed.Type: ApplicationFiled: January 23, 2014Publication date: May 15, 2014Applicant: Asymmetric Therapeutics, LLCInventor: John P. Ford
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Patent number: 8703942Abstract: The present disclosure provides inhibitors of Hsp90 and methods of making and using the same. Such compounds are useful as radioimaging ligands and for the treatment of cancer and other conditions where cell growth or maintenance depend on Hsp90 activity.Type: GrantFiled: November 4, 2010Date of Patent: April 22, 2014Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Gabriela Chiosis, Huazhong He, Laura Llauger-Bufi, Joungnam Kim, Steve M. Larson, Peter Smith-Jones
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Publication number: 20140107098Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: ApplicationFiled: December 19, 2013Publication date: April 17, 2014Applicant: Janssen Pharmaceutica NVInventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
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Publication number: 20140100174Abstract: Treatment for Cancer Using A Preparation containing a combination of one or more Natural or Synthetic or a Combination of Natural and Synthetic Boswellic Acids and one or more Natural or Synthetic or a Combination of Natural and Synthetic Cytokinins such as Kinetin, Kinetin Riboside and other Cytokinins and (the Preparation) could also contain one or more Natural or Synthetic or a Combination of Natural and Synthetic plant growth hormones such as Auxins in any percentage ratio for Treating Cancer. The said Components of the said Preperation works by Inducing Apoptosis of the Cancerous cells, by “executing” them by Inducing Caspases-8 and other mechanisms.Type: ApplicationFiled: October 4, 2012Publication date: April 10, 2014Inventor: Kingsley Yianomah Quartey
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Publication number: 20140094475Abstract: Disclosed are solid forms of antiretroviral compounds and anti-oxidative acids, and processes for their preparation. Pharmaceutical compositions using the solid forms are also disclosed.Type: ApplicationFiled: April 9, 2012Publication date: April 3, 2014Applicant: LAURUS LABS PRIVATE LIMITEDInventors: Venkata S. Indukuri, Vamsee K. Muppidi, Sree R. Joga, Seeta R. Gorantla, Satyanarayana Chava
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Publication number: 20140088121Abstract: The disclosure relates to Compounds of Formulae (IA) and (IB): and pharmaceutically acceptable salts thereof wherein Z1, Z2, Z3, Xa, Xb, Xc, Xd, Y, X2, and X4 are as defined herein, compositions comprising an effective amount of a Compound of Formula (IA) and/or (IB), and methods to treat or prevent a condition, such cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (IA) or (IB). The disclosure further relates to compounds of Formulae (IA) and IB) in which X2 is a leaving for introducing a radiolabeled atom, such as 124I or 131I and to methods of using such compounds in the preparation of radiolabeled compounds, particularly for use in imaging.Type: ApplicationFiled: April 5, 2012Publication date: March 27, 2014Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Weilin Sun, Tony Taldone, Pallav Patel, Gabriela Chiosis
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Patent number: 8680076Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing scleroderma, keloids, UV injury, or sunburn, and methods for improving or preventing scar formation.Type: GrantFiled: October 20, 2011Date of Patent: March 25, 2014Assignee: Signal Pharmaceuticals, LLCInventors: Brydon L. Bennett, Brian Edwin Cathers, Kristen Lee Jensen-Pergakes, Heather Raymon, Weilin Xie, Jaman May Maroni
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Publication number: 20140080769Abstract: The present invention provides a compound which is an inhibitor of sphingolipid biosynthesis for use in the treatment of a disease which has a secondary Niemann-Pick type C disease like cellular phenotype.Type: ApplicationFiled: September 13, 2013Publication date: March 20, 2014Applicants: The Chancellor, Masters and Scholars of the University of Oxford, The Government of the United States of America, as represented by the Secretary, Department of HealtInventors: Frances Mary Platt, Emyr Lloyd-Evans, Forbes Dennison Porter
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Publication number: 20140073656Abstract: Novel compounds for the treatment of estrogen receptor-mediated disorders, including breast cancer, and methods of treatment using the novel compounds. The novel compounds, when administered in a safe and effective amount, present extended binding to estrogen receptors in breast tissue without activating the estrogen receptors. Estrogen is blocked from binding to the estrogen receptors for an extended period of time, effectively hindering growth of breast cancer cells.Type: ApplicationFiled: October 10, 2013Publication date: March 13, 2014Applicant: Florida A&M UniversityInventor: John S. Cooperwood
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Publication number: 20140073606Abstract: The present invention relates to 2?-Fluoro-6?-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Heptatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses, especially HBV.Type: ApplicationFiled: November 13, 2013Publication date: March 13, 2014Inventors: Chung K. Chu, Jianing Wang
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Patent number: 8653090Abstract: A composition and method for the treatment of the side-effects associated with the administration of cancer chemotherapeutic agents involves the oral ingestion of a slow release capsule containing adenine and orotate. The administration of a protein pump inhibitor decreases systemic absorption of orotate and the administration of allopurinol decreases the formation of 2,8-dihydroxy adenine from adenine. In an alternative embodiment, cationic liposomes contain purine/pyrimidine precursors. The cationic liposomes bind to the cells lining the mucosa of the intestinal tract and then the contents of the cationic liposome are then taken up in the interior of the cells to prevent the metabolism of the cancer treatment drug 5-FU into a toxic species.Type: GrantFiled: April 13, 2012Date of Patent: February 18, 2014Assignee: Asymmetric Therapeutics, LLCInventor: John P. Ford
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Publication number: 20140037622Abstract: Methods of treating a head and neck cancer are disclosed.Type: ApplicationFiled: August 2, 2013Publication date: February 6, 2014Applicants: UCL BUSINESS PLC, FOUNDATION MEDICINE, INC.Inventors: Chris Hendrik Boshoff, Timothy Robert Fenton, Matthias Alexander Lechner, Philip James Stephens, Matthew J. Hawryluk, Roman Yelensky, Garrett Michael Frampton
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Publication number: 20140037547Abstract: The present invention relates to cGMP protein kinase (PKG) and regulatory domains and methods of use thereof. The structural determination of PKG domains is also described. cGMP independent PKG activators and uses thereof are also described.Type: ApplicationFiled: March 13, 2013Publication date: February 6, 2014Applicant: The University of Vermont and State Agricultural CollegeInventors: Wolfgang Dostmann, Brent W. Osborne, Thomas M. Moon
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Patent number: 8637527Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: GrantFiled: September 12, 2012Date of Patent: January 28, 2014Assignee: Janssen Pharmaceutica NVInventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
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Publication number: 20140024663Abstract: The present invention includes inhibitors of the amino acid transporter ATB0,+ and methods of uses thereof for the treatment of estrogen receptor-positive breast cancer.Type: ApplicationFiled: July 12, 2013Publication date: January 23, 2014Inventors: VADIVEL GANAPATHY, MUTHUSAMY THANGARAJU
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Patent number: 8629151Abstract: This invention relates to compositions, and related compounds and methods, of conjugates of immunomodulatory agents and polymers or unit(s) thereof. The conjugates may be contained within synthetic nanocarriers, and the immunomodulatory agents may be released from the synthetic nanocarriers in a pH sensitive manner.Type: GrantFiled: May 26, 2010Date of Patent: January 14, 2014Assignee: Selecta Biosciences, Inc.Inventors: Charles Zepp, Grayson B. Lipford, Yun Gao, Lloyd Johnston, Fen-ni Fu, Mark J. Keegan, Sam Baldwin
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Publication number: 20140004209Abstract: The subject matter disclosed herein relates to agents and methods of treating neoplasms with an agent that is a kinase inhibitor and is also an inducer of autophagy in combination with an agent that is an inhibitor of autophagy.Type: ApplicationFiled: December 21, 2011Publication date: January 2, 2014Applicant: GENENTECH, INC.Inventors: Kiu Lin, Michael Degtyarev
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Publication number: 20130338173Abstract: The present invention relates to carbocycle-substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 5, 2011Publication date: December 19, 2013Applicant: EPIZYME, INC.Inventors: Edward J. Olhava, Richard Chesworth, Kevin W. Kuntz
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Publication number: 20130331384Abstract: The disclosure provides for novel antimicrobial agents, methods of making, and methods of use thereof.Type: ApplicationFiled: February 14, 2012Publication date: December 12, 2013Applicant: The Regents of the University of CaliforniaInventors: Richard L. Gallo, Teruaki Nakatsuji
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Publication number: 20130324481Abstract: This invention provides for biocompatible, biodegradable eye drop pharmaceutical formulations useful for the treatment of ocular indications. In particular, tocopherols and their esters of low water solubility, notably ?-tocopheryl acetate, are exceptional vehicles for biocompatible, nonirritating topical eye drop formulations that provide sustained release of active agents.Type: ApplicationFiled: August 9, 2013Publication date: December 5, 2013Applicant: Ramscor, Inc.Inventors: Vernon G. Wong, Louis L. Wood
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Patent number: 8592581Abstract: The present invention relates to compounds of formula (I) wherein: R1 and R2 are each independently H, alkyl or haloalkyl; R3 and R4 are each independently H, alkyl, haloalkyl or aryl; R5 is alkyl or cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and where one of X, Y and Z is N and the remainder are CR9; R7, R8 and each R9 are independently H, alkyl or haloalkyl, wherein at least one of R7, R8 and each R9 is other than H. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula (I), and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.Type: GrantFiled: October 5, 2009Date of Patent: November 26, 2013Assignees: Cyclacel Limited, Cancer Research Technology LimitedInventors: Peter William Sheldrake, Butrus Atrash, Simon Green, Edward McDonald, Sheelagh Frame
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Patent number: 8586505Abstract: Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.Type: GrantFiled: July 15, 2010Date of Patent: November 19, 2013Assignee: SDS Biotech K. K.Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Ryutaro Katsuki, Tomoko Muraki
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Patent number: 8586566Abstract: This invention relates to specific compounds and their pharmaceutically acceptable salts of the general formula: wherein Q is —CR?CR?— and Ring A is an aryl, heteroaryl or heterocyclic ring or ring system. This invention also relates to pharmaceutical compositions comprising such specific compounds or their pharmaceutically acceptable salts and a pharmaceutically acceptable carrier or adjuvant.Type: GrantFiled: December 5, 2011Date of Patent: November 19, 2013Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Wei-Sheng Huang, Rajeswari Sundaramoorthi, Xiaotian Zhu, R. Mathew Thomas, William C. Shakespeare, David C. Dalgarno, Tomi K. Sawyer
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Publication number: 20130296346Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, a method of synthesis of said compounds, pharmaceutical compositions comprising them and their use as a medicament for treating inflammatory diseases.Type: ApplicationFiled: November 22, 2011Publication date: November 7, 2013Applicant: Faes Farma, S.A.Inventors: Rosa Rodes Solanes, Neftali Garcia Dominguez, Beatriz Lopez Ortega, Melchor Alvarez De Mon Soto, Antonio De La Hera Martinez, Ana Munoz Munoz, Francisco Ledo Gomez
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Publication number: 20130296271Abstract: Agri-horticultural pest control compositions having outstanding control effect on pests, in particular, agri-horticultural pests, which comprise as active ingredients one or more 4-(3-butynyl)aminopyrimidine derivatives represented by the general formula [I], namely, where R1 is typically selected from among: a) phenyl c) —SiR5R6R7 (R5, R6, and R7 which may be the same or different represent a linear or branched alkyl having 1-6 carbon atoms, a linear or branched haloalkyl having 1-3 carbon atoms which is substituted by one halogen atom, a linear or branched cyanoalkyl having 1-3 carbon atoms which is substituted by one cyano group, and phenyl); d) hydropgen atom; R2 typically represents a hydrogen atom; R3 typically represents a hydrogen atom; R4 represents a hydrogen atom and one or more agri-horticultural pest control compounds selected from among agri-horticultural antimicrobial compounds, say, multi-site contact active compouns, nucleic acids synthesis inhibitory active compounds, mitosis and cellType: ApplicationFiled: December 27, 2011Publication date: November 7, 2013Applicant: SDS Biotech K.K.Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Tomoko Muraki, Ryutaro Katsuki
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Patent number: 8575182Abstract: Certain 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts of the general formula are provided wherein R6 and R9 are as defined in the specification. These 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts are useful in compositions for treating mammalian cells, and especially human skin cells, in order to ameliorate the adverse effects of aging, treat skin disease states, treat immunological responses resulting from or associated with inflammation, and the like.Type: GrantFiled: May 26, 2011Date of Patent: November 5, 2013Assignee: Institute of Experimental Botany, Academy of Sciences of the Czeck RepublicInventors: Lucie Szucova, Marek Zatloukal, Lukas Spichal, Jiri Voller, Karel Dolezal, Miroslav Strnad, Frank J. Massino
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Publication number: 20130289037Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.Type: ApplicationFiled: March 14, 2013Publication date: October 31, 2013Inventor: MILLENNIUM PHARMACEUTICALS, INC
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Patent number: 8552013Abstract: Novel heterocyclic derivatives based on N6-substituted adenine, having anticancer, mitotic, immunosuppressive and antisenescent properties for plant, animal and human cells and methods of their preparation. Included are also pharmaceutical compositions, cosmetic preparations and growth regulators, which contain these derivatives as active compound and the use of these derivatives for the preparation of drugs, cosmetic preparations, in biotechnological processes, in cosmetics and in agriculture.Type: GrantFiled: July 18, 2007Date of Patent: October 8, 2013Assignee: USTAV Experimentalni Botaniky Akademie Ved Ceske RepublikyInventors: Igor Popa, Jan Holub, René Lenobel, Stefaan Werbrouck, Karel Dolezal, Miroslav Strnad, Marek Zatloukal, Frank J. Massino
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Publication number: 20130244964Abstract: The present invention provides an isolated HIV-1 mutant and isolated nucleic acid molecules comprising HIV-RT coding sequences harboring a novel mutation in the S68 codon, and in particular, deletions of the S68 codon. This novel deletion reduces the sensitivity of HIV to various nucleoside reverse transcriptase inhibitors. Methods of using this mutation for selecting effective antiretroviral agents in vitro and in vivo, methods for monitoring infection progression in HIV-infected individuals and methods for avoiding the emergence of and/or to treat individuals infected with HIV comprising mutations, including deletions, at the S68 codon of HIV-RT are provided.Type: ApplicationFiled: November 9, 2012Publication date: September 19, 2013Applicant: EMORY UNIVERSITYInventor: Raymond F. Schinazi
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Publication number: 20130245046Abstract: In the present invention, a novel 2-alkynyl-N9-propargyladenine represented by formula (I) wherein R1 represents a halogen atom, a furyl group, or a triazolyl group; R2 and R3 each represents a hydrogen atom or a C1-8 alkyl group, or form a cycloalkyl group by bonding to each other; and X represents a hydrogen atom or a hydroxyl group, or a pharmaceutically acceptable salt thereof, has a stronger and longer-lasting effect as a therapeutic agent for Parkinsonian syndromes.Type: ApplicationFiled: November 24, 2011Publication date: September 19, 2013Applicant: YAMASA CORPORATIONInventors: Kazuki Endo, Kohei Yamada, Kazuki Deguchi
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Patent number: 8530484Abstract: The method includes the steps of cleansing of the scalp sufficiently to remove material which would otherwise block antiviral medication from reaching hair follicles, heating the scalp to increase the absorption of the antiviral medication and applying the antiviral medication to the scalp in effective amount to suppress viral replication or viral activation present in the nerves leading to the scalp.Type: GrantFiled: November 4, 2009Date of Patent: September 10, 2013Assignee: Loreal SAInventor: Robert E Akridge
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Publication number: 20130231356Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.Type: ApplicationFiled: February 12, 2013Publication date: September 5, 2013Applicant: ICOS CORPORATIONInventors: Edward A. KESICKI, Kerry W. FOWLER, Danwen HUANG, Hua Chee OOI, Amy OLIVER, Kamal Deep PURI, Fuqiang RUAN, Jennifer TREIBERG
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Publication number: 20130225564Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.Type: ApplicationFiled: March 18, 2013Publication date: August 29, 2013Applicant: Signal Pharmaceuticals, LLCInventor: Signal Pharmaceuticals, LLC
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Publication number: 20130203780Abstract: The present invention relates to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor diclofenac. The invention is further related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and diclofenac.Type: ApplicationFiled: February 6, 2013Publication date: August 8, 2013Inventor: William L. Pridgen
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Patent number: 8501724Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: GrantFiled: April 30, 2012Date of Patent: August 6, 2013Assignee: Pharmacyclics, Inc.Inventors: Wei Chen, David J. Loury
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Publication number: 20130197069Abstract: The invention relates to methods and products for treating emotional disorders such as stress induced emotional disorders, as well as related assays and kits. Methods include administering to a subject an effective amount of an agent for targeting the Rac1, Cdk5, p35, PAK-1 pathway to treat the emotional disorder. The agent for targeting the Rac1, Cdk5, p35, PAK-1 pathway may be, for instance, a Rac-1 inhibitor, a Cdk5 inhibitor, a PAK-1 activator, or p35 mobilizing agent.Type: ApplicationFiled: March 27, 2013Publication date: August 1, 2013Applicant: MASSACHUSETTS INSTITUTE OF TECHNOLOGYInventor: MASSACHUSETTS INSTITUTE OF TECHNOLOGY