At Imidazole Ring Carbon Patents (Class 514/400)
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Patent number: 11654115Abstract: According to the invention there is provided a pharmaceutical composition comprising N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide (C21), or a pharmaceutically-acceptable salt thereof, in which composition the C21 or salt thereof is protected by the presence of a coating comprising an enteric substance. Preferred dosage forms comprise capsules in which C21 or salt thereof is presented in the form of a dry powder mixture or a suspension of particles of C21 in a solvent in which it is insoluble. Such dosage forms find utility in the treatment of lung diseases, such as idiopathic pulmonary fibrosis, sarcoidosis and respiratory virus-induced tissue damage.Type: GrantFiled: March 17, 2022Date of Patent: May 23, 2023Assignee: VICORE PHARMA ABInventors: Ola Camber, Christina Johansson
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Patent number: 11633354Abstract: The disclosure is directed to methods related to creatinine, for example, a method for its safe administration to a human, a method for using creatinine to improve the bioavailability of creatine, and a metn.Type: GrantFiled: April 30, 2021Date of Patent: April 25, 2023Assignee: THERMOLIFE INTERNATIONAL, LLCInventors: Alexandros Nikolaidis, Ronald Kramer
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Patent number: 11634428Abstract: The present invention is concerned with novel deuterated Angiotensin-Converting Enzyme-2 (ACE-2) inhibitors of general structural formula I, their optically active enantiomers and diastereoisomers, and pharmaceutical salts and compositions thereof, as well as combination therapies which include compounds of the present invention, These compounds have high potency and selectivity for Angiotensin-Converting Enzyme-2 (ACE-2) inhibition, and are useful in the treatment of infectious respiratory diseases including the pandemic disease Covid-19, Severe Acute Respiratory Syndrome (SARS-CoV-2), Severe Acute Respiratory Syndrome (SARS-CoV), and other diseases caused by coronaviruses.Type: GrantFiled: March 29, 2021Date of Patent: April 25, 2023Inventor: Daljit Singh Dhanoa
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Patent number: 11597717Abstract: Provided are compounds of Formula Y-Z: The compounds target plexin domain containing 2 (PLXDC2). The compounds can be used to treat conditions such as inflammatory or immune-mediated diseases, diabetes, infectious diseases, and cancers. The compounds can be used to treat such specific conditions as systemic lupus erythematosus, rheumatoid arthritis, multiple sclerosis, autoimmune encephalitis, diabetic nephropathy, diabetic retinopathy, psoriasis, and inflammatory bowel disease, among other conditions.Type: GrantFiled: September 29, 2021Date of Patent: March 7, 2023Assignee: Landos Biopharma, Inc.Inventors: Josep Bassaganya-Riera, Andrew Leber, Raquel Hontecillas, Nuria Tubau-Juni
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Patent number: 11564941Abstract: In one embodiment, a composition is provided, comprising: 0.0005 wt % to 0.05 wt % of silver nitrate, based on a total weight of the composition; 0.01 wt % to 1.0 wt % of hyaluronic acid, based on the total weight of the composition; and 0.05 wt % to 2.5 wt % of allantoin, based on the total weight of the composition. In one embodiment, a method of treating a skin wound is provided, comprising: topically applying a sufficient amount of a composition to the skin wound of a patient to cover the skin wound, the composition comprising: 0.0005 wt % to 0.05 wt % of silver nitrate, based on a total weight of the composition; 0.01 wt % to 0.1 wt % of hyaluronic acid, based on the total weight of the composition; and 0.05 wt % to 2.5 wt % of allantoin, based on the total weight of the composition.Type: GrantFiled: October 29, 2021Date of Patent: January 31, 2023Inventor: Brian Brazzo
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Patent number: 11534377Abstract: The present invention is directed to a hair growth agent for external use comprising chiro-inositol, which is provided as an excellent hair growth agent.Type: GrantFiled: January 26, 2021Date of Patent: December 27, 2022Assignee: KOBAYASHI PHARMACEUTICAL CO., LTD.Inventors: Kosuke Tanaka, Mihoko Kawasaki, Hironori Tomi, Takashi Tsuji
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Patent number: 11389387Abstract: The subject of the application is protein hydrolyzates having specific amounts of the amino acids arginine and lysine, which demonstrate improved properties in hair treatment compositions and in cleansing compositions for skin and hair, and also enzymatic methods for the preparation thereof, and the cosmetic compositions comprising same.Type: GrantFiled: September 5, 2017Date of Patent: July 19, 2022Assignee: BASF SEInventors: Hans-Martin Haake, Christina Kohlmann, Christian Markiefka, Guadalupe Pellon, Ansgar Behler
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Patent number: 11253496Abstract: Provided herein are nutritional, or therapeutic, compositions and methods of use in primarily treating kidney patients suffering from low serum albumin. The compositions are divided into four formulations, comprising: 1) the magnesium salt and/or the calcium salt of the alpha keto acids of: ?-leucine, ?-valine, ?-isoleucine, ?-phenylalanine, ?-hydroxy methionine; and/or ?-tryptophan, and/or ?-tyrosine; 2) L-lysine monoacetate, L-threonine; and/or 3) histidine, tryptophan, and tyrosine, as amino acids or base acids. The specific formulation administered depends in part upon which stage 2-5 of renal disease the patient has. The invention further comprises methods of treatment of disorders associated with low serum albumin using the composition as an over-the-counter pill. The patient's serum albumin is tested on a periodic basis and the selected composition and dose are adjusted accordingly.Type: GrantFiled: November 29, 2018Date of Patent: February 22, 2022Inventor: Edgar L. Hull, Jr.
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Patent number: 11224582Abstract: Amino acid formulations for pancreatic vitality. The formulations comprise a mixture of a plurality of amino acids, wherein the mixture comprises at least one amino acid selected from the group consisting of serine, glutamic acid, and/or carnitine. Methods of enhancing pancreatic vitality, stabilizing blood glucose levels, and improving A1C levels in subjects in need thereof are also described.Type: GrantFiled: April 24, 2018Date of Patent: January 18, 2022Assignee: Almeda Labs LLCInventors: Stacy Tucker, Sushrutha Nagaraj
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Patent number: 11104632Abstract: Vanillin derivative compounds that bind covalently with hemoglobin are provided. Methods of treating sickle cell disease and other hypoxia-related disorders by administering such compounds are also provided.Type: GrantFiled: May 12, 2020Date of Patent: August 31, 2021Assignee: King Abdulaziz UniversityInventors: Abdelsattar Mansour Ebeid Omar, Moustafa El-Sayed El-Araby, Martin K. Safo
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Patent number: 11007164Abstract: Compositions containing one or more kinds of essential amino acids other than leucine and not less than 35 mol % of leucine, relative to the total content of essential amino acids, are useful for preventing or improving dementia or a depressive state, in particular, a depressive state caused by stress, have high safety, and can be continuously ingested or administered.Type: GrantFiled: February 25, 2019Date of Patent: May 18, 2021Assignee: AJINOMOTO CO., INC.Inventor: Shinobu Nishitani
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Patent number: 10959987Abstract: Imidazole-based compounds as hepatitis C virus (HCV) inhibitors. The compounds have an imidazole core that is disubstituted via amide links. Also described are a pharmaceutical composition incorporating the imidazole-based compound, a method of preparing these compounds, and a method for using the pharmaceutical composition in the treatment of HCV infection.Type: GrantFiled: April 15, 2019Date of Patent: March 30, 2021Assignee: King Abdulaziz UniversityInventors: Moustafa E. El-Araby, Abdelsattar Mansour Omar, Mahmoud Abdelkhalek El-Faky, Sameh Hamdy Abdelmageed Soror, Maan Talaat Khayat, Hani Zakariah Asfour, Faida Hassan Bamane
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Patent number: 10898456Abstract: Ingesting an agent containing cystine or a salt thereof, as an active ingredient, is effective for improving exercise-induced gastrointestinal disorder, providing an improvement effect equal to or better than that by the conventional technology on exercise-induced gastrointestinal disorders including exercise-induced decline in gastrointestinal tract barrier function.Type: GrantFiled: December 8, 2017Date of Patent: January 26, 2021Assignee: AJINOMOTO CO., INC.Inventors: Yoshihito Nogusa, Ami Mizugaki
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Patent number: 10881629Abstract: Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.Type: GrantFiled: February 27, 2018Date of Patent: January 5, 2021Assignee: Natural Alternatives International, Inc.Inventors: Roger Harris, Mark Dunnett
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Patent number: 10821096Abstract: Imidazole-based compounds as hepatitis C virus (HCV) inhibitors. The compounds have an imidazole core that is disubstituted via amide links. Also described are a pharmaceutical composition incorporating the imidazole-based compound, a method of preparing these compounds, and a method for using the pharmaceutical composition in the treatment of HCV infection.Type: GrantFiled: August 6, 2020Date of Patent: November 3, 2020Assignee: King Abdulaziz UniversityInventors: Moustafa E. El-Araby, Abdelsattar Mansour Omar, Mahmoud Abdelkhalek El-Faky, Sameh Hamdy Abdelmageed Soror, Maan Talaat Khayat, Hani Zakariah Asfour, Faida Hassan Bamane
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Patent number: 10550089Abstract: The present application relates to certain substituted imidazole and triazole compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating pain, musculoskeletal inflammation, neuroinflammatory disorders, airway inflammation, itch, dermatitis, colitis and related conditions. The compounds are of Formula (I) where X is N or CH, Z and Y are N or C (but both not N) and R1-R3 are as defined herein.Type: GrantFiled: May 11, 2017Date of Patent: February 4, 2020Assignee: Heptares Therapeutics LimitedInventors: John Graham Cumming, Frank Xinhe Wu, Karl Henrik Edman, Hongming Chen, Dean Gordon Brown, Roland Werner Burli, Shawn Donald Johnstone, Giles Albert Brown, Benjamin Gerald Tehan, Barry John Teobald, Miles Stuart Congreve
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Patent number: 10435376Abstract: Disclosed are derivatives of 1H-imidazole-4,5-dicarboxamide and use thereof in preparation of anticoccidial drugs. The derivatives have structural formulae as shown in formulae (I) to (VI). The derivatives of 1H-imidazole-4,5-dicarboxamide as disclosed in the present invention have significant anticoccidial effect, especially against coccidia that show a resistance to other anticoccidial drugs, and thus they can be used in preparation of anticoccidial drug.Type: GrantFiled: November 26, 2015Date of Patent: October 8, 2019Assignee: GUANGZHOU INSIGHTER BIOTECHNOLOGY CO., LTD.Inventors: Xianfeng Peng, Zonghua Qin
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Patent number: 10390553Abstract: Ingesting a food etc. which is in a unit package form per meal and contains, in the unit, not less than 0.3 g of histidine as an ingestion amount per meal is effective for improving mental energy and biorhythm.Type: GrantFiled: April 7, 2016Date of Patent: August 27, 2019Assignee: AJINOMOTO CO., INC.Inventors: Tetsuro Shibakusa, Mayu Sugita, Ikuko Sasahara, Naoto Koyama, Shinobu Seki
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Patent number: 10342826Abstract: The present invention concerns the use of a combination consisting of D-aspartic and L-aspartic acids or L-aspartic acid used alone to stimulate the procreative activity in the man by increment of spermatozoon number and motility.Type: GrantFiled: May 28, 2014Date of Patent: July 9, 2019Assignee: MERCK SERONO S.P.A.Inventors: Salvatore D'Aniello, Enrico D'Aniello
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Patent number: 10028935Abstract: Disclosed are novel stable compounds having anti-oxidant properties and methods of using the compounds for the treatment of diseases or injuries associated with oxidative stress.Type: GrantFiled: January 31, 2017Date of Patent: July 24, 2018Assignee: XPD Holdings, LLCInventors: Marc Bailie, Steven K. Duddy, Jim Herman
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Patent number: 9931371Abstract: A method and a pharmaceutical composition for increasing wound healing in an individual in need thereof, the method comprising administering an angiopoietin like 4 (ANGPTL4) polypeptide or a therapeutically active fragment thereof.Type: GrantFiled: July 3, 2013Date of Patent: April 3, 2018Assignee: Nanyang Technologies UniversityInventors: Nguan Soon Tan, Han Chung Kelvin Chong
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Patent number: 9907770Abstract: Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.Type: GrantFiled: March 31, 2017Date of Patent: March 6, 2018Assignee: Natural Alternatives International, Inc.Inventors: Roger Harris, Mark Dunnett
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Patent number: 9895344Abstract: Novel compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of 7,8-dihydroxyflavone or derivative thereof. Specifically, methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of 7,8-dihydroxyflavone or a derivative thereof. A further method of promoting neuroprotection in a subject also is provided, which includes selecting a subject in need of neuroprotection, and administering to the subject a therapeutically effective amount of 7,8-dihydroxyflavone or a derivative thereof.Type: GrantFiled: July 23, 2009Date of Patent: February 20, 2018Assignee: EMORY UNIVERSITYInventor: Keqiang Ye
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Patent number: 9808444Abstract: Several embodiments provided herein relate to histamine dosing regimens are and uses of such regimens in the restoration of histamine balance in subjects suffering from, for example, histapenia and/or histadelia. Several embodiments also relate to the use of histamine dosing regimens for the treatment and/or prevention of migraine headaches.Type: GrantFiled: November 2, 2016Date of Patent: November 7, 2017Assignee: BioHealthonomics Inc.Inventor: Cristian Arnou
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Patent number: 9789125Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.Type: GrantFiled: June 2, 2016Date of Patent: October 17, 2017Assignee: Allergan Holdings Unlimited CompanyInventors: Luigi Anzalone, Frank J. Villani, Christopher A. Teleha, Penina Feibush, Barry Fegely
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Patent number: 9700548Abstract: The present invention provides combinations comprising a sedating antihistamine and selected indole-based natural products such as L-tryptophan, 5-hydroxytryptophan and melatonin, along with pharmaceutically acceptable calcium and magnesium salts and selected B vitamins. These combinations are useful in providing a medicament for improving sleep in mammals, especially humans.Type: GrantFiled: June 8, 2012Date of Patent: July 11, 2017Assignee: REQUIS PHARMACEUTICALS INC.Inventors: Lars Jacob Stray Knutsen, Judi Lois Knutsen
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Patent number: 9669010Abstract: A method of treating chronic kidney disease by administering to a subject a composition that includes L-arginine, glycine, L-glutamine, L-histidine, L-aspartic acid L-glutamic acid, and L-carnosine.Type: GrantFiled: December 6, 2013Date of Patent: June 6, 2017Assignee: Bio Health Solutions, LLCInventor: James Archer
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Patent number: 9668994Abstract: Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.Type: GrantFiled: March 30, 2015Date of Patent: June 6, 2017Assignee: Natural Alternatives International, Inc.Inventors: Roger Harris, Mark Dunnett
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Patent number: 9629800Abstract: The present invention concerns gastroretentive formulation comprising an active substance granulated with a mixture of a weak gelling agent, a strong gelling agent, and a gas generating agent and process for manufacturing said formulation.Type: GrantFiled: July 19, 2006Date of Patent: April 25, 2017Assignee: ETHYPHARMInventors: Mahendra Chaudhari, Omprakash D. Chandwani, Rajashree S. Yelegaonkar
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Patent number: 9539278Abstract: It has been found that high amounts of aspartate equivalents in combination with vitamin B12 and/or biotin, especially in relative absence of glutamate equivalents, improve the metabolism of ketobodies and/or lactate in a mammal's body, especially in diseased or traumatic conditions. As a result, levels of ketobodies and lactate can be decreased and unphysicologically high acidity normalised. Thus, it is an object of the invention to provide an enteral nutritional or a pharmaceutical composition for the treatment and/or prevention of disturbed ketone and lactate metabolism, i.e. elevated concentrations of ketone bodies, lactate and/or other organic acids and/or insufficient pH homeostasis, especially elevated concentrations of ketone bodies and/or lactate, in a mammal's blood, wherein the composition comprises high amounts of aspartate equivalents in combination with vitamin B12 and/or biotin, preferably in relative absence of glutamate equivalents.Type: GrantFiled: October 16, 2014Date of Patent: January 10, 2017Assignee: N.V. NutriciaInventor: Robert Johan Joseph Hageman
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Patent number: 9511054Abstract: Several embodiments provided herein relate to histamine dosing regimens are and uses of such regimens in the restoration of histamine balance in subjects suffering from, for example, histapenia and/or histadelia. Several embodiments also relate to the use of histamine dosing regimens for the treatment and/or prevention of migraine headaches.Type: GrantFiled: April 10, 2015Date of Patent: December 6, 2016Assignee: BioHealthonomics Inc.Inventor: Cristian Arnou
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Patent number: 9504673Abstract: The invention relates to an agent for the treatment and/or prophylaxis of highly pathogenic infectious diseases, such as highly pathogenic influenza A (in particular, subtypes H5 and H7) and severe acute respirator syndrome caused by the genotype IV coronavirus. The agent is in the form of glutaryl histamine or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition based on glutaryl histamine or a pharmaceutically acceptable salt thereof and to a method for the treatment and/or prophylaxis of highly pathogenic infectious diseases.Type: GrantFiled: May 10, 2010Date of Patent: November 29, 2016Assignee: LTD “Valenta-Intellekt”Inventors: Vladimir Evgenievich Nebolsin, Galina Alexandrovna Zheltukhina, Sergey Vladimirovich Borisevich, Svetlana Yakovlevna Loginova, Alexander Grigorievich Chuchalin
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Patent number: 9500660Abstract: The present invention relates generally to the field of nutrition and health. In particular, the present invention relates to a new biomarker, its use and a method that allows it to diagnose the likelihood to resist diet induced weight gain, and/or to be susceptible to a diet induced weight gain. For example, the biomarker may be isovalerylglycine.Type: GrantFiled: November 25, 2013Date of Patent: November 22, 2016Assignee: Nestec S.A.Inventors: Francois-Pierre Martin, Claire L. Boulange, Ivan Montoliu Rora, Sebastiano Collino, Marc-Emmanuel Dumas, Elaine Holmes, Serge Andre Dominique Rezzi, Jeremy Nicholson, Sunil Kochhar
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Patent number: 9480669Abstract: Disclosed is a method comprising the administration of a 3% amino acid and 3% glycerin solution for the use of prevention and disruption of bacterial biofilms. Also disclosed is method comprising the administration of L-cysteine 0.4 g per 100 ml for the prevention and destruction of fungal biofilms.Type: GrantFiled: January 6, 2015Date of Patent: November 1, 2016Assignee: The Regents of The University of CaliforniaInventors: Thomas Benedict Bryan, Clarissa J. Nobile
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Patent number: 9447112Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 meType: GrantFiled: June 1, 2015Date of Patent: September 20, 2016Assignee: University of KentuckyInventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
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Patent number: 9421267Abstract: Provided herein, in part, is a method of treating a neurological or movement disorder in a patient in need thereof, comprising subcutaneously administering to said patient a pharmaceutically acceptable composition comprising levodopa and optionally carbidopa and optionally entacapone or tolcapone, or pharmaceutically acceptable salts thereof, wherein said composition is administered substantially continuously, and compositions that can be used in the disclosed methods.Type: GrantFiled: November 15, 2011Date of Patent: August 23, 2016Assignee: NeuroDerm, Ltd.Inventors: Oron Yacoby-Zeevi, Mara Nemas
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Patent number: 9364489Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.Type: GrantFiled: July 22, 2015Date of Patent: June 14, 2016Assignee: Forest Tosara LimitedInventors: Luigi Anzalone, Frank J. Villani, Christopher A. Teleha, Penina Feibush, Barry Fegely
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Patent number: 9351960Abstract: The invention relates to medicine and comprises an agent for the treatment of a viral hepatitis C, which is glutaryl histamine or a pharmaceutically acceptable salt thereof. This agent can also be administered in combination with a pegylated interferon and ribavirin. The invention further relates to a pharmaceutical composition for the treatment of a viral hepatitis C. This invention solves the problem of providing a novel agent, which is effective in the treatment of a viral hepatitis C and makes it possible to produce a sustained virologic response.Type: GrantFiled: March 13, 2013Date of Patent: May 31, 2016Assignee: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”Inventors: Vladimir Evgenievich Nebolsin, Dmitry Yurievich Konstantinov, Larisa Leonidovna Popova, Elena Alekseevna Strebkova, Petr Grigorievich Deryabin
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Patent number: 9295649Abstract: The present disclosure relates in part to pharmaceutical compositions comprising polymeric nanoparticles having certain glass transition temperatures. Other aspects of the invention include methods of making such nanoparticles.Type: GrantFiled: December 15, 2010Date of Patent: March 29, 2016Assignee: BIND Therapeutics, Inc.Inventors: Mir Mukkaram Ali, Abhimanyu Sabnis, David Dewitt, Greg Troiano, James Wright, Maria Figueiredo, Michael Figa, Christina Van Geen Hoven, Young-Ho Song, Jason Auer, Tarikh Christopher Campbell
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Patent number: 9193690Abstract: Disclosed herein is a pharmaceutical composition comprising (3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl)methanol and methods of using the composition to treat chronic pain.Type: GrantFiled: November 21, 2014Date of Patent: November 24, 2015Assignee: Allergan, Inc.Inventor: Daniel W. Gil
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Patent number: 9150514Abstract: The invention is directed to methods for treating hypertension or heart failure using 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. In particular embodiments, the invention uses compounds having formula IIIa, IVa, Va: These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity.Type: GrantFiled: October 23, 2014Date of Patent: October 6, 2015Assignee: THERAVANCE BIOPHARMA R&D IP, LLCInventors: 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: 9115091Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.Type: GrantFiled: August 14, 2014Date of Patent: August 25, 2015Assignee: FURIEX PHARMACEUTICALS, INC.Inventors: Luigi Anzalone, Frank J. Villani, Christopher A. Teleha, Penina Feibush, Barry Fegely
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Patent number: 9045434Abstract: A compound and method for treating myocilin glaucoma using a selective Grp94 inhibitor is presented. Clearance of mutant myocilin can be promoted by selectively targeting the endoplasmic reticulum (ER) chaperone Grp94 using siRNA knockdown or small molecule inhibitors. Grp94 contributes to the intracellular accumulation of mutant myocilin. Tailored treatments aimed at disrupting the Grp94/mutant myocilin interaction can be used as a new therapeutic strategy for myocilin glaucoma. The inventors developed a compound having a general backbone structure of geldanamycin (GDA) and radicicol (RDC) in which a more hydrophobic surrogate of the quinone in GDA is linked to the resorcinol in RDC through a cis-amide bioisostere.Type: GrantFiled: November 18, 2013Date of Patent: June 2, 2015Assignees: University of South Florida, The University of KansasInventors: Chad Anthony Dickey, Amirthaa Suntharalingam, Brian S. J. Blagg
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Publication number: 20150147309Abstract: The present invention relates to an allosteric non-inhibitory chaperone of the lysosomal acid alpha-glucosidase (GAA) for use in the treatment of a pathological condition characterized by a deficiency of the lysosomal acid alpha-glucosidase (GAA), to pharmaceutical composition thereof, to a method for increasing the activity of GAA in a subject and to a method for identifying an allosteric non-inhibitory chaperone for GAA.Type: ApplicationFiled: June 6, 2013Publication date: May 28, 2015Inventors: Giancarlo Parenti, Caterina Porto, Marco Moracci, Maria Carmina Ferrara, Beatrice Cobucci-Ponzano, Generoso Andria
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Publication number: 20150148395Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: January 29, 2015Publication date: May 28, 2015Applicant: ALLERGAN, INC.Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
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Publication number: 20150148394Abstract: The present invention relates to method for treating skin diseases and skin conditions in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, or enantiomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: January 29, 2015Publication date: May 28, 2015Inventors: Mohammed I. Dibas, Daniel W. Gil, John E. Donnello, Ken Chow, Liming Wang, Michael E. Garst
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Patent number: 9040563Abstract: Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase IC50 value of 25 nM and a whole cell H-Ras processing IC50 value of 90 nM. Several of the inhibitors proved highly selective for hFTase over the related prenyltransferase enzyme geranylgeranyltransferase-I (GGTase-I).Type: GrantFiled: March 11, 2013Date of Patent: May 26, 2015Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc., Yale UniversityInventors: Said M. Sebti, Andrew Hamilton
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Publication number: 20150133370Abstract: The present invention relates to dietary compositions comprising reduced level of methionine, tryptophan, all amino acids, or protein, dietary compositions comprising glycerol as a substitute for monosaccharides, disaccharides, and polysaccharides, and hypocaloric or calorie free diets with reduced level of energy, carbohydrates, or protein. Also disclosed are methods of using these compositions and diets, as well as fasting, to protect subjects against chemotherapy, radiotherapy, oxidative stress, or aging.Type: ApplicationFiled: September 26, 2014Publication date: May 14, 2015Inventor: Valter Longo
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Publication number: 20150126571Abstract: Disclosed is a method comprising the administration of a 3% amino acid and 3% glycerin solution for the use of prevention and disruption of bacterial biofilms. Also disclosed is method comprising the administration of L-cysteine 0.4 g per 100 ml for the prevention and destruction of fungal biofilms.Type: ApplicationFiled: January 6, 2015Publication date: May 7, 2015Inventor: THOMAS BENEDICT BRYAN
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Publication number: 20150126437Abstract: The disclosure provides compounds useful as insect repellents, compositions comprising such repellents, and methods of repelling an arthropod using such compounds and compositions. The disclosure further provides insect traps and method for identifying ligands and cognates for biological molecules.Type: ApplicationFiled: October 17, 2012Publication date: May 7, 2015Applicant: The Regents of the University of CaliforniaInventors: Anandasankar Ray, Sean Michael Boyle