Patents Issued in January 3, 2017
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Patent number: 9532954Abstract: The invention relates to tablet comprising granules dispersed in at least one hydrophilic compound or matrix. The granules contain an active agent, at least one amphiphilic compound and at least one lipophilic compound. The tablet may include a gastro-resistant film coating.Type: GrantFiled: June 18, 2014Date of Patent: January 3, 2017Assignee: COSMO TECHNOLOGIES LIMITEDInventors: Roberto Villa, Massimo Pedrani, Mauro Ajani, Lorenzo Fossati
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Patent number: 9532955Abstract: Nanocrystals, compositions, and methods that aid particle transport in mucus are provided. In some embodiments, the compositions and methods involve making mucus-penetrating particles (MPP) without any polymeric carriers, or with minimal use of polymeric carriers. The compositions and methods may include, in some embodiments, modifying the surface coatings of particles formed of pharmaceutical agents that have a low water solubility. Such methods and compositions can be used to achieve efficient transport of particles of pharmaceutical agents though mucus barriers in the body for a wide spectrum of applications, including drug delivery, imaging, and diagnostic applications. In certain embodiments, a pharmaceutical composition including such particles is well-suited for administration routes involving the particles passing through a mucosal barrier.Type: GrantFiled: June 20, 2016Date of Patent: January 3, 2017Assignees: Kala Pharmaceuticals, Inc., The Johns Hopkins UniversityInventors: Alexey Popov, Elizabeth M. Enlow, James Bourassa, Colin R. Gardner, Hongming Chen, Laura M. Ensign, Samuel K. Lai, Tao Yu, Justin Hanes, Ming Yang
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Patent number: 9532956Abstract: The present invention generally relates to polymers and particles, such as nanoparticles. The particles and polymers generally include one or more buffering components. Additionally, the particles and polymers may include two or more components that impart useful properties (functionalities). The particles and polymers, for example, may include a buffering component and a degradable component. As described herein, the particles and polymers may also include a hydrophilic component and/or a cleavable bond component. The particles and polymers described herein have been found to be particularly effective when used for delivery of one or more agents, such as one or more pharmaceutical agents. Other aspects of the invention are directed to methods of using or administering such particles or polymers, kits involving such particles or polymers, and the like.Type: GrantFiled: April 18, 2010Date of Patent: January 3, 2017Assignees: Massachusetts Institute of Technology, The Brigham and Women's Hospital Inc.Inventors: Aleksandar Filip Radovic-Moreno, Weiwei Gao, Archana Swami, Gershon Golomb, Robert S. Langer, Omid C. Farokhzad
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Patent number: 9532957Abstract: The present invention provides a stabilization method, a preservation method and the like method of reduced coenzyme Q10, which is useful as functional nutritive foods, specific health foods and the like. Furthermore, the present invention provides a method for efficiently obtaining reduced coenzyme Q10 of high quality and by a method suitable for a commercial production. It is possible to handle and stably preserve reduced coenzyme Q10 under a condition that oxidation by a molecular oxygen is inhibited by contacting reduced coenzyme Q10 with, an ascorbic acid and citric acid or a related compound thereof, and thus a stabilized composition is obtained. Moreover, reduced coenzyme Q10 is converted into a crystalline state in such a condition that the formation of oxidized coenzyme Q10 as a byproduct is minimized by crystallizing reduced coenzyme Q10 in the presence of ascorbic acid or a related compound thereof etc., and thus a reduced coenzyme Q10 crystal of high quality is produced.Type: GrantFiled: March 5, 2014Date of Patent: January 3, 2017Assignee: KANEKA CORPORATIONInventors: Takahiro Ueda, Tadao Ono, Mitsutoshi Moro, Shiro Kitamura, Yasuyoshi Ueda
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Patent number: 9532958Abstract: A method for producing powders for inhalation includes a first mixing step of stirring a first active ingredient and a carrier in the presence of a milling medium, and mixing the first active ingredient and the carrier while crumbling the agglomerates of the first active ingredient to obtain a mixture of the carrier and the first active ingredient; and a second mixing step of adding fine powders to the mixture obtained in the first mixing step, and stirring and mixing the mixture and the fine powders in the presence of a milling medium.Type: GrantFiled: February 25, 2013Date of Patent: January 3, 2017Assignee: CliniPro Co., Ltd.Inventor: Shinichi Ono
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Patent number: 9532959Abstract: Methods and compositions for reducing frequency of urination are disclosed. The methods comprise administering to a subject having a condition that resulting in undesired frequency of urination an effective amount of a pharmaceutical composition comprising one or more prostaglandin pathway inhibitors. The pharmaceutical compositions comprise one or more prostaglandin pathway inhibitors and a pharmaceutically acceptable carrier.Type: GrantFiled: June 6, 2014Date of Patent: January 3, 2017Assignee: WELLESLEY PHARMACEUTICALS, LLCInventors: David A. Dill, Frank J. Rauscher, III
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Patent number: 9532960Abstract: A method for using metformin and sodium butyrate in combination to treat a cancer patient with K-ras mutation is disclosed. When administering the pharmaceutical composition to a cancer patient, Metformin and sodium butyrate offer cooperatively therapeutic efficacy. The present invention also discloses a pharmaceutical composition and a pharmaceutical kit containing both aforementioned. The application of the method, the pharmaceutical composition and the pharmaceutical kit of the present invention are advantageous for improving the treatment effect to cancer patients with K-ras mutation.Type: GrantFiled: January 17, 2014Date of Patent: January 3, 2017Assignee: JOHNPRO BIOTECH INC.Inventors: Kwan-Hwa Chi, Yu-Shan Wang, Chao-Chun Chang
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Patent number: 9532961Abstract: The present invention provides a method for preventing blood-brain barrier reperfusion injury in a mammalian blood-brain barrier endothelial cell during reperfusion following ischemic stroke comprising administering an effective amount of a ?-glutamyl-D-cysteine antioxidant to the subject and a kit for doing the same.Type: GrantFiled: April 23, 2013Date of Patent: January 3, 2017Assignee: Rosalind Franklin University of Medicine and ScienceInventor: Darryl R Peterson
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Patent number: 9532962Abstract: Use of medium-chain length fatty acids such as capric acid, caprylic acid or lauric acid and their salts or mono- or di- or triglycerides as nephroprotection agents to protect against renal failure progression in chronic kidney diseases This includes the treatment of kidney diseases associated with nephrectomy, renal fibrosis, glomerular sclerosis and end-stage renal disease Also includes the protection of the kidney against cytotoxic agent used in chemotherapy or autoimmune diseases or transplantation Further includes the treatment of renal failure progression associated with hypertension, infarct, tumor, diabetes mellitus, autoimmunity or inflammation.Type: GrantFiled: November 3, 2008Date of Patent: January 3, 2017Assignee: PROMETIC PHARMA SMT LIMITEDInventors: Vincent Pichette, Francois Leblond, Mouna Lagraoui, Lyne Gagnon
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Compositions comprising a fatty acid oil mixture and a free fatty acid, and methods and uses thereof
Patent number: 9532963Abstract: Compositions comprising a fatty acid oil mixture and at least one free fatty acid, and uses thereof are disclosed. Further disclosed are preconcentrates capable of forming a self-nanoemulsifying drug delivery system (SNEDDS), a self-microemulsifying drug delivery system (SMEDDS) or self-emulsifying drug delivery systems (SEDDS) in an aqueous solution. Preferred fatty acids are eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) in a form chosen from ethyl ester and triglyceride.Type: GrantFiled: March 9, 2010Date of Patent: January 3, 2017Assignee: Pronova Biopharma Norge ASInventors: Svein Olaf Hustvedt, Preben Houlberg Olesen, Gunnar Berge, Anette Müllertz -
Patent number: 9532964Abstract: The present invention concerns a food supplement comprising Salvia sclarea seeds, or flour, oil or pulp or extracts obtained from the seeds as well as finished food products comprising the food supplement. The present invention further concerns a nutraceutical or cosmetic preparation comprising as an active ingredient Salvia sclarea seeds, or flour, oil or pulp or extracts obtained from the seeds.Type: GrantFiled: July 19, 2013Date of Patent: January 3, 2017Assignee: STATE OF ISRAEL, MINISTRY OF AGRICULTURE & RURAL DEVELOPMENT, AGRICULTURE RESEARCH ORGANIZATION (ARO) (VOLCANI CENTER)Inventors: Nativ Dudai, Zohara Yaniv Bacharach, Eli Putievsky, Diah Saadi, Dan Schafferman, David Chaimovitsh
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Patent number: 9532965Abstract: A Salvia hispanica L. derived seed oil extract composition of matter containing from 60-88% PUFAs in a ratio of from 3.1:1-3.3:1 of ALA to LA, 4-10% of C-18 mono-unsaturated fatty acid, 1-5% of C-18 saturated fatty acid and 4-8% of C-16 saturated fatty acid in a mixed triglyceride form stable at room temperature of 12-24 months containing a mixture of selected antioxidants.Type: GrantFiled: September 27, 2013Date of Patent: January 3, 2017Assignee: U.S. NUTRACEUTICALS, LLCInventors: John A. Minatelli, W. Stephen Hill, Rudi E. Moerck, Uy Nguyen
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Patent number: 9532966Abstract: The invention relates to the use of specifically designed lipid component with optimal fatty acid profile, an enhanced portion of the palmitic acid residues in the sn-2 position and present as lipid globules with a phospholipid coating for an early in life diet for improving the development of a healthy body composition, in particular prevention of obesity, later in life.Type: GrantFiled: June 18, 2012Date of Patent: January 3, 2017Assignee: N.V. NutriciaInventors: Eline Marleen Van Der Beek, Marieke Abrahamse-Berkeveld, Annemarie Oosting, Martine Sandra Alles
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Patent number: 9532967Abstract: Disclosed is the use of the compounds represented by formula (I) in the preparation of a medicament against tumor angiogenesis, wherein R1 and R2 are each independently C1-C8 alkylidene group or C2-C8 alkenylidene group; A1 and A2 are each independently aryl, isoaryl, or aryl or isoaryl optionally substituted by halogen, —CN, —NO2, —OH, —SH, —OR3, —SR3, —R3, —R3—OR4, —C(O)R3, —S(O)R3, —S(O)2R3, —NR4R5, —C(O)OR3, —C(O)NR4R5, —O(O)CR4, —S(O)CR4 or —NR4(O)CR5, wherein R3 is C1-C4 alkyl, R4 and R5 are each independently hydrogen, C1-C4 alkyl, aryl or substituted aryl; and X and Y are each independently oxygen; and the compound of formula (I) does not include phenethyl caffeate.Type: GrantFiled: December 8, 2011Date of Patent: January 3, 2017Inventors: Junyi Liu, Yansheng Du, Jirun Peng, Zhizhong Ma
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Patent number: 9532968Abstract: Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.Type: GrantFiled: August 30, 2015Date of Patent: January 3, 2017Inventor: Mark Quang Nguyen
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Patent number: 9532969Abstract: A method for treating psoriasis including the steps of applying an isothiocyanate functional surfactant to an area affected by psoriasis, wherein the isothiocyanate functional surfactant comprises at least one isothiocyanate functional group associated with an aliphatic and/or aromatic carbon atom of the isothiocyanate functional surfactant.Type: GrantFiled: January 17, 2012Date of Patent: January 3, 2017Assignee: The William M. Yarbrough FoundationInventor: Michael E. Silver
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Patent number: 9532970Abstract: Compositions comprising LSF compositions and treatment regiments comprising administration of LSF containing compositions are disclosed. Compositions and/or regiments may optionally include the administration of vitamins, minerals, and anti-oxidants. Methods for using these compositions and treatment regimens for treating subjects for diseases, including diseases associated with inflammation and/or oxidative stress, are provided. Various methods for use of the LSF compositions for inhibition of histone deacetylases (HDACs) in various cells, tissues, and/or conditions are also provided.Type: GrantFiled: July 8, 2015Date of Patent: January 3, 2017Inventors: Darlene E. McCord, Thomas Karagiannis
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Patent number: 9532971Abstract: The invention disclosed herein generally relates to low-dose oral doxepin pharmaceutical formulations and the use of these formulations to promote sleep.Type: GrantFiled: May 20, 2013Date of Patent: January 3, 2017Assignee: Pernix Sleep, Inc.Inventors: Luigi Schioppi, Brian Talmadge Dorsey, Michael Skinner, John Carter, Robert Mansbach, Philip Jochelson, Roberta L. Rogowski, Cara Baron Casseday, Meredith Perry, Bryan Knox
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Patent number: 9532972Abstract: Disclosed herein are combinatorial therapies for treating or preventing reoccurrence of cancer. The therapies involve inhibition of LIMK1 in conjunction with taxane therapy. Specifically exemplified herein is co-administration of a LIMK1 RNA interfering molecule along with administration of a taxane.Type: GrantFiled: February 7, 2013Date of Patent: January 3, 2017Assignee: UNIVERSITY OF CENTRAL FLORIDA RESEARCH FOUNDATION, INC.Inventor: Ratna Chakrabarti
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Patent number: 9532973Abstract: A compound of formula (I-1) wherein n equals 0 or 1, Z represents O or S, R1 represents one group chosen among the group consisting of hydrogen, C1-C7 alkyl, substituted, or not, by a halogen, a hydroxyl or a —O—R12 group, wherein R12 is a C1-C7 alkyl, a group —CH2—O—CO—R5 wherein R5 is chosen among a hydrogen atom and a C1-C7 alkyl, substituted or not by at least one halogen, a group —O—R13, wherein R13 is chosen among hydrogen and a C1-C7 alkyl, an amine or a —CH2-amine, R?1 represents a group chosen among hydrogen and —O—R14, wherein R14 is chosen among hydrogen and a C1-C7 alkyl, and R2 is chosen among the group consisting of a C1-C7 alkyl, a C3-C6 cycloalkyl, an aryl group, and an heteroaryl group for the treatment of pathologies involving excess activity of at least one member of the kallikrein family.Type: GrantFiled: March 10, 2015Date of Patent: January 3, 2017Assignees: UNIVERSITE PIERRE ET MARIE CURIE (PARIS 6), UNIVERSITE DE LIEGEInventors: Michele Reboud-Ravaux, Chahrazade Yerroum-El Amri, Xiao Tan, Lixian Qin, Maurice Pagano, Alain Hovnanian, Laetitia Furio, Bernard Pirotte
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Patent number: 9532974Abstract: The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.Type: GrantFiled: August 27, 2015Date of Patent: January 3, 2017Assignee: Targacept, Inc.Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Ronald Joseph Heemstra, Matt S. Melvin, Jason Speake, Yunde Xiao, Daniel Yohannes
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Patent number: 9532975Abstract: The present invention is to provide uses of the L-oxiracetam in preparation of medicines for preventing or treating coma. Experimental results show that L-oxiracetam wake-promoting effects of alcoholism-induced coma is obvious, and D-oxiracetam has basically no effect. The effect of the above wake-promoting effects of L-oxiracetam is 2 times greater than racemic oxiracetam. The wake-promoting effects of L-oxiracetam on trauma or anesthesia-induced coma are both significant.Type: GrantFiled: April 24, 2012Date of Patent: January 3, 2017Assignee: CHONGQING RUNZE PHARMACEUTICAL COMPANY LIMITED.Inventor: Lei Ye
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Patent number: 9532976Abstract: The invention provides methods of treating a diabetic subject comprising administering a glucosylceramide synthase inhibitor to the subject.Type: GrantFiled: August 20, 2014Date of Patent: January 3, 2017Assignee: Genzyme CorporationInventors: Seng H. Cheng, Nelson S. Yew, Ronald K. Scheule, Hongmei Zhao
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Patent number: 9532977Abstract: Provided herein are controlled release oral dosage forms of poorly soluble drugs, methods of making the dosage forms, and methods of their use for the treatment of various diseases and/or disorders.Type: GrantFiled: November 11, 2015Date of Patent: January 3, 2017Assignee: Celgene CorporationInventors: Ming J. Chen, Ho-Wah Hui, Xiaole Shen
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Patent number: 9532978Abstract: This invention provides topical localized formulations comprising an isoxazoline compound and a pharmaceutically or veterinary acceptable liquid carrier vehicle comprising N,N-diethyl-3-methylbenzamide as a solvent and an improved method for controlling, and preventing parasite infestation in animals.Type: GrantFiled: September 28, 2015Date of Patent: January 3, 2017Assignee: Intervet Inc.Inventors: Stefan Fuchs, Anja Regina Heckeroth, Ramona Müller, Heike Williams, Hartmut Zoller
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Patent number: 9532979Abstract: The present inventions relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drugs lopinavir and ritonavir. The solid composition and aqueous dispersion additionally comprise a mixture of a hydrophilic polymer and a surfactant. The surfactant is selected from vitamin-E-polyethylene glycol-succinate (Vit-E-PEG-succinate), a polyoxyethylene sorbitan fatty acid ester, N-alkyldimethylbenzylammonium chloride, sodium deoxycholate, dioctyl sodium sulfosuccinate, polyethyleneglycol-12-hydroxystearate, polyvinyl alcohol (PVA), and a block copolymer of polyoxyethylene and polyoxypropylene, or a combination thereof. The hydrophilic polymer is suitably selected from polyvinyl alcohol (PVA), a polyvinyl alcohol-polyethylene glycol graft copolymer, a block copolymer of polyoxyethylene and polyoxypropylene, polyethylene glycol, hydroxypropyl methyl cellulose (HPMC), and polyvinylpyrrolidone, or a combination thereof.Type: GrantFiled: September 7, 2012Date of Patent: January 3, 2017Assignee: The University of LiverpoolInventors: Marco Norman Giardiello, Thomas Oliver McDonald, Andrew Owen, Steven Paul Rannard, Philip John Martin, Darren Lee Smith
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Patent number: 9532980Abstract: The invention provides methods for treating A? peptide related disorders such as Alzheimer's disease comprising administering a therapeutically effective amount of a CK1 modulator to a patient in need thereof.Type: GrantFiled: October 24, 2007Date of Patent: January 3, 2017Assignee: The Rockefeller UniversityInventors: Marc Flajolet, Paul Greengard
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Patent number: 9532981Abstract: The present invention relates to a method for producing artificial skin, comprising: adding a matrix metalloproteinase inhibitor and a heparanase inhibitor to an artificial skin formation culture medium comprising human epidermal keratinocytes and human dermal fibroblasts, culturing the cells in the artificial skin formation culture medium, and forming artificial skin.Type: GrantFiled: September 25, 2014Date of Patent: January 3, 2017Assignee: Shiseido Company, Ltd.Inventors: Shunsuke Iriyama, Kenichi Umishio, Makoto Tsunenaga, Shinji Inomata, Eijiro Adachi
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Patent number: 9532982Abstract: The present invention relates to a pharmaceutical combination comprising a 2-carboxamide cycloamino urea derivative compound of formula (I) and at least one aromatase inhibitor for the treatment of cancer; the uses of such combinations in the treatment of cancer; and to a method of treating warm-blooded animals including humans suffering cancer by administering to said animal in need of such treatment an effective dose of a 2-carboxamide cycloamino urea derivative compound of formula (I) in combination with at least one aromatase inhibitor.Type: GrantFiled: September 18, 2013Date of Patent: January 3, 2017Assignee: Novartis AGInventors: Michael Goldbrunner, Xizhong Huang
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Patent number: 9532983Abstract: Benzofuran compound, composition thereof, kit thereof, and/or method thereof. A benzofuran-2-carboxamide moiety may be N-arylated and/or N-alkylated, and the resulting benzofuran compound may be a sigma receptor ligand that binds to, e.g., a ?1 receptor and/or a ?2 receptor with relatively high affinity and/or selectivity. For example, the benzofuran compound may be 5,6-dimethoxy-3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide, 3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide, or 6-methoxy-3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide. The composition may include the benzofuran compound and a pharmaceutically acceptable carrier.Type: GrantFiled: July 31, 2014Date of Patent: January 3, 2017Assignee: Savannah State UniversityInventor: Karla-Sue C. Marriott
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Patent number: 9532984Abstract: This invention relates to a synergistic pharmaceutical combination of glucose lowering drugs and autophagy inhibitors, kits containing such combinations, and methods of using such combinations to treat subjects suffering from cancers carrying a specific KRAS mutation. This invention also relates to a theranostic method for cancer treatment.Type: GrantFiled: June 11, 2012Date of Patent: January 3, 2017Assignee: The Translational Genomics Research InstituteInventor: Stephen T. Gately
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Patent number: 9532985Abstract: The invention relates to methods of treating, reducing the symptoms of, or preventing a post-traumatic stress syndrome by administration of tetrahydroquinoline derivatives of formula I wherein R1 and R2 each independently represent (C1-C4)alkoxy, R3 represents aryl-(C1-C4)alkyl or heteroaryl-(C1-C4)alkyl, and R4 represents hydrogen or (C1-C4)alkyl, or pharmaceutically acceptable salts thereof.Type: GrantFiled: October 9, 2008Date of Patent: January 3, 2017Assignee: ACTELION PHARMACEUTICALS LTD.Inventor: Francois Jenck
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Patent number: 9532986Abstract: Methods of treatment of NTM lung infections using formulations of liposomal ciprofloxacin. Specific liposome formulations and delivery of such for treatment of respiratory tract infections and other medical conditions, and devices and formulations used in connection with such are described.Type: GrantFiled: March 31, 2015Date of Patent: January 3, 2017Assignees: ARADIGM CORPORATION, OREGON STATE UNIVERSITYInventors: Igor Gonda, James Blanchard, David C. Cipolla, Luiz Eduardo Moreira Bermudez
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Patent number: 9532987Abstract: The invention provides combinations comprising a MEK inhibitor (such as GDC-0973 or GDC-0623), or a pharmaceutically acceptable salt thereof and an ERK inhibitor (such as GDC-0994). The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.Type: GrantFiled: August 29, 2014Date of Patent: January 3, 2017Assignee: Genentech, Inc.Inventors: Marcia Belvin, John Moffat, Mark Merchant
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Patent number: 9532988Abstract: The present patent application relates to a pharmaceutical composition comprising a TRPA1 antagonist and an analgesic agent. Particularly, the present patent application provides a pharmaceutical composition comprising a thienopyrimidinedione compound as a TRPA1 antagonist and an analgesic agent; and use of such composition for treating pain in a subject.Type: GrantFiled: October 14, 2014Date of Patent: January 3, 2017Assignee: GLENMARK PHARMACEUTICALS S.A.Inventors: Srinivas Gullapalli, Praveen Kumar Gupta, Maulik Nitinkumar Gandhi
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Patent number: 9532989Abstract: The present invention relates to compounds of Formula P-I where the variables (e.g. R1, Y, A, R1, Ra, Ra?, Rb, Rb?, Rc, Rc?, Rd, Rd?, Re, or Re?) and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.Type: GrantFiled: June 4, 2015Date of Patent: January 3, 2017Assignees: THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES, ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI, THE ROCKEFELLER UNIVERSITYInventors: Barry S. Coller, Craig Thomas, Marta Filizola, Joshua McCoy, Wenwei Huang, Min Shen
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Patent number: 9532990Abstract: Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.Type: GrantFiled: March 18, 2016Date of Patent: January 3, 2017Assignee: Zhejiang DTRM Biopharma Co. Ltd.Inventor: Wei He
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Patent number: 9532991Abstract: A risperidone sustained release microsphere formulation is provided. The microsphere formulation includes risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.Type: GrantFiled: July 22, 2016Date of Patent: January 3, 2017Assignees: Shandong Luye Pharmaceutical Co., Ltd., Nanjing Luye Pharmaceutical Co., LtdInventors: Kaoxiang Sun, Rongcai Liang, Qilin Wang, Wenyan Wang, Wanhui Liu, Youxin Li
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Patent number: 9532992Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: GrantFiled: June 17, 2015Date of Patent: January 3, 2017Assignee: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, John Emmerson Campbell, Masashi Seki
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Patent number: 9532993Abstract: Aprepitant L-proline solvate compositions and aprepitant L-proline solvate cocrystals are disclosed as well as pharmaceutical compositions containing them. The compositions and cocrystals of the invention are: 1:1:1 aprepitant L-proline methanol composition; a 1:1:1 aprepitant L-proline methanol cocrystal; a 1:1:1:1 aprepitant L-proline ethanol composition; a 1:1:1 aprepitant L-proline ethanol cocrystal; 1 1:1:1 aprepitant L-proline n-propanol composition; and a 1:1:1 aprepitant L-proline n-propanol cocrystal: The aprepitant L-proline solvate compositions or cocrystals may be used in the same way as aprepitant to treat or prevent disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pain, cancer, a skin disease, itch a respiratory disease, or an addiction.Type: GrantFiled: November 21, 2012Date of Patent: January 3, 2017Assignee: NUFORMIX LIMITEDInventors: Joanne Holland, Christopher Frampton, Alan Chorlton, Daniel Gooding
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Patent number: 9532994Abstract: The present invention discloses agents and methods for inducing osteoblastic cellular differentiation, as well as the use of such agents and methods to treat patients to maintain bone mass, enhance bone formation and/or bone repair. Exemplary agents include oxysterols, alone or in combination with particular oxysterols, or other agents, such as bone morphogenic proteins, known to assist in bone formation. The invention further includes medicaments including oxysterols for the treatment of bone disorders and implants to facilitate bone repair.Type: GrantFiled: August 30, 2004Date of Patent: January 3, 2017Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventor: Farhad Parhami
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Patent number: 9532995Abstract: Endometriosis, including endometriosis externa, endometrioma, adenomyosis, adenomyomas, adenomyotic nodules of the uterosacral ligaments, and endometriotic nodules, such as scar endometriosis are effectively treated by the intralesional administration, including transvaginal, endoscopic or open surgical administration including via laparotomy, of a progestogen. Compositions therefor also are provided.Type: GrantFiled: August 27, 2004Date of Patent: January 3, 2017Assignee: MISCON TRADING S.A.Inventor: Mirudhubashini Govindarajan
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Patent number: 9532996Abstract: Doxycycline formulations with a reduced food effect are disclosed. Particularly disclosed are modified release formulations which can be administered once a day and exhibit a reduced food effect. Methods of treating inflammatory conductions such as rosacea or inflammatory symptoms such as the papules and pustules of rosacea or acne vulgaris are also disclosed.Type: GrantFiled: November 19, 2015Date of Patent: January 3, 2017Assignee: Dr. Reddy's Laboratories Ltd.Inventors: Ankit Baheti, Bijay Kumar Padhi, Rajeev Singh Raghuvanshi
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Patent number: 9532997Abstract: Disclosed herein are novel methods and compositions useful for promoting intestinal stem cell function. The methods and compositions are particularly useful for stimulating the proliferation of and/or self-renewal of intestinal stem cells, as well as for minimizing, preventing, or ameliorating cellular damage resulting from incidental or accidental exposure to radiation (e.g., cancer radiation therapy).Type: GrantFiled: April 3, 2013Date of Patent: January 3, 2017Assignee: Whitehead Institute for Biomedical ResearchInventors: Pekka Katajisto, Michael Pacold, David M. Sabatini, Omer Yilmaz
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Patent number: 9532998Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.Type: GrantFiled: January 13, 2016Date of Patent: January 3, 2017Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
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Patent number: 9532999Abstract: The present invention relates to methods of treating infectious, inflammatory and post-traumatic disorders by administering various compounds newly discovered to have TLR4 inhibitory activity. In addition to methods of treatment, the present invention further provides for pharmaceutical compositions comprising said compounds, together with a suitable pharmaceutical carrier. Because TLR4 is the most upstream receptor in the pro-inflammatory LPS signaling cascade, treatments of the invention, which inhibit or antagonize TLR4 action, may avoid the pitfalls associated with other cytokine inhibitors that act further down the pathway and accordingly play a less specific (and perhaps non-critical) role.Type: GrantFiled: May 20, 2015Date of Patent: January 3, 2017Assignee: UNIVERSITY OF PITTSBURGH—OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATIONInventors: Peter Wipf, Matthew D. Neal, Sodhi P. Chhinder, David J. Hackam
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Patent number: 9533000Abstract: A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a concentrated formulation of aztreonam, or a pharmaceutically acceptable salt thereof, delivered as an aerosol or dry powder formulation.Type: GrantFiled: October 4, 2013Date of Patent: January 3, 2017Assignee: GILEAD SCIENCES, INC.Inventor: Alan Bruce Montgomery
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Patent number: 9533001Abstract: Bioactive, hydroforming luminal liner compositions are formed of high molecular weight crystalline, absorbable copolyesters dissolved in a liquid derivative of a polyether glycol that undergoes transformation into a tissue-adhering, resilient interior cover or liner for the controlled release of its bioactive payload at clinically compromised conduits in humans as in the case of bacteria- and yeast-infected vaginal canals, esophagi, and arteries following angioplasty.Type: GrantFiled: June 8, 2015Date of Patent: January 3, 2017Assignee: Poly-Med, Inc.Inventors: Shalaby W. Shalaby, Georgios T. Hilas, Kenneth David Gray
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Patent number: 9533002Abstract: The invention provides methods of treatment of metabolic syndrome with HSP90 inhibitors, particularly HSP90? inhibitors. The invention provides methods of diagnosis and monitoring of metabolic syndrome using HSP90, particularly HSP90?, expression and activity level.Type: GrantFiled: May 24, 2013Date of Patent: January 3, 2017Assignee: Berg LLCInventors: Niven Rajin Narain, Rangaprasad Sarangarajan, Vivek K. Vishnudas, Enxuan Jing
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Patent number: 9533003Abstract: It is disclosed a method for the treatment of hepatitis B (HBV) infection or HBV/hepatitis D (HDV) co-infection, the method comprising administering to a subject in need of treatment a first pharmaceutically acceptable agent that removes the hepatitis B surface antigen from the blood and a second pharmaceutically acceptable agent which stimulates immune function.Type: GrantFiled: September 15, 2015Date of Patent: January 3, 2017Assignee: REPLICOR INC.Inventors: Michel Bazinet, Andrew Vaillant