Tricyclo Ring System Having The Seven-membered Hetero Ring A One Of The Cyclos Patents (Class 514/217)
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Patent number: 11566000Abstract: A cocrystal containing the 1?R-diastereomer and the 1'S-diastereomer of sofpironium bromide at a ratio of 1:3 (Form CO), a crystal mixture (for example, Form B) containing Form CO and a crystalline form of the 1?R-diastereomer (Form MN), and a method for preparing sofpironium bromide, which is suitable for manufacture of the crystal mixture are provided. Form CO and a crystalline form of sofpironium bromide containing Form CO (for example, Form B) have superior stability without hygroscopic property, and accordingly they can be preferably used as a raw material of medicaments.Type: GrantFiled: November 25, 2020Date of Patent: January 31, 2023Assignee: Botanix SB, Inc.Inventors: Kazuyoshi Marubayashi, Masahito Watanabe, Herbert R. Brinkman
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Patent number: 11535816Abstract: The invention relates to surfactants of general formula (I) in which R1 and R2 represent independently of one another represent H and SO3?X+ with the proviso that at least one of R1 and R2 is not H, n and m represent independently from each other numbers from 0-21 under the proviso that 4<n+m<26, and X+ represents a charge-balancing anion. The surfactants can be incorporated into detergents or cleaning agents, have excellent technological application properties and can be produced based on renewable raw materials.Type: GrantFiled: February 28, 2020Date of Patent: December 27, 2022Assignee: Henkel AG & Co. KGaAInventors: Christian Kropf, Anna Klemmer, Danuta Bedrunka, Regina Palkovits, Peter Hausoul, Lukas Kipshagen, Carsten Stobbe
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Patent number: 11400045Abstract: Disclosed is a pharmaceutical composition in dry powder form for intranasal administration, having an anti-anaphylactic adrenergic receptor agonist in the form of dry powder for intranasal administration, the composition having solid particles of the active agent in combination with at least one functional additive, and solid particles of an inert carrier.Type: GrantFiled: December 28, 2020Date of Patent: August 2, 2022Assignee: Nasus Pharma Ltd.Inventors: Galia Temtsin-Krayz, Pavel Kazhdan
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Patent number: 11352362Abstract: The present disclosure may disclose a new crystal form D of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one ((1S,4R)-7,7-dimethyl-2-oxobicyclo[2.2.1]hept-1-yl) methanesulfonic acid salt, preparation method therefor and a medicinal use. Compared to the existing crystalline forms, this new crystalline form has clear advantages with respect to solubility, stability, and the preparation process.Type: GrantFiled: April 22, 2020Date of Patent: June 7, 2022Assignee: SHANGHAI BEGREAT PHARMATECHInventor: Xiaoming Meng
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Patent number: 11351169Abstract: The present disclosure describes compounds and pharmaceutically acceptable salts thereof and compositions and formulations comprising the same that are useful in methods of treating dyskinesia or related disorders, and methods for treating dyskinesia or related disorders.Type: GrantFiled: December 10, 2018Date of Patent: June 7, 2022Assignee: Melior Pharmaceuticals II, LLCInventors: John Ciallella, John Gruner, Andrew G. Reaume, Michael S. Saporito
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Patent number: 11213497Abstract: Methods and compositions related to molecules and formulations comprising antibiofilm materials are provide, including new formulations of Deep Eutectic Solvents (DES) that are chemically related to choline geranate. Specifically, geranic acid (a component of choline geranate DES) is a molecule from the isoprenoid/terpene family of compounds. Other members of this family as DES components include isoprenoid acids and chemical derivatives thereof.Type: GrantFiled: May 31, 2018Date of Patent: January 4, 2022Assignees: ARIZONA BOARD OF REGENTS ON BEHALF OF NORTHERN ARIZONA UNIVERSITY, TRIAD NATIONAL SECURITY, LLC, DIXIE STATE UNIVERSITY, THE COLLEGE OF NEW JERSEYInventors: Andrew T. Koppisch, Gerrick E. Lindberg, David T. Fox, Joseph Baker, Alexanndra J. Heyert, Rico Del Sesto, Joshua R. Greene
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Patent number: 11173111Abstract: A composition comprising at least one TCA useful in a method for treating an anorectal disorder, a rectal device and method of treating the anorectal disorder by anorectally administering an effective amount of the TCA, e.g. amitriptyline.Type: GrantFiled: September 22, 2020Date of Patent: November 16, 2021Assignee: Rythera Therapeutics, Inc.Inventors: Reginald L. Hardy, Mitchell Brigell
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Patent number: 11124501Abstract: The present invention relates to compounds of formula I as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.Type: GrantFiled: December 6, 2018Date of Patent: September 21, 2021Assignee: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Keith Jones, Carl Rye, Nicola Chessum, Matthew Cheeseman, Adele E. Pasqua, Kurt G. Pike, Paul F. Faulder
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Patent number: 11091501Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 29, 2018Date of Patent: August 17, 2021Assignee: Enanta Pharmaceuticals, Inc.Inventors: In Jong Kim, Jianming Yu, Joseph Panarese, Kevin McGrath, Solymar Negretti-Emmanuelli, Thomas P. Blaisdell, Brian C. Shook, Yat Sun Or
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Patent number: 10959974Abstract: Provided in the present invention are ingenol compounds and a use thereof in preparing an anti-HIV latency drug. In particular, provided in the present invention is a use of ingenol compounds and pharmaceutically acceptable salts thereof for preparing a drug for: (a) intervening with HIV viral latency; (b) activating an HIV virus that has been integrated into mammalian genomes; and/or (c) inducing the expression of the dormant HIV provirus in infected cells. The compounds of the present invention may also be used in combination with antiretroviral drugs to accelerate the removal of latent viral reservoirs.Type: GrantFiled: February 22, 2016Date of Patent: March 30, 2021Assignee: SHANGHAI XIN HAO BIOLOGICAL TECHNOLOGY COMPANYInventors: Longfei Zhang, Pengfei Wang, Zhongjun Ma, Huanzhang Zhu
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Patent number: 10918608Abstract: The present disclosure relates to the use of cannabidiol (CBD) for the treatment of Tuberous Sclerosis Complex (TSC). In particular the TSC is treatment resistant and is characterised by generalised seizures or focal seizures with impairment. The disclosure further relates to the use of CBD in combination with one or more anti-epileptic drugs (AEDs).Type: GrantFiled: October 13, 2015Date of Patent: February 16, 2021Assignee: GW Research LimitedInventors: Geoffrey Guy, Stephen Wright, Elizabeth Thiele
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Patent number: 10888568Abstract: The present invention relates to use of antipsychotic phenothiazine derivative for treatment of cancer. The invention also provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating a cancer, and/or preventing or delaying cancer recurrence based on trifluoperazine. The invention further provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating cancer based on thioridazine and its enantiomers. Additionally, the invention provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating KRAS mutant NSCLC comprising thioridazine.Type: GrantFiled: October 29, 2018Date of Patent: January 12, 2021Assignee: National Yang Ming UniversityInventors: Chi-Ying Huang, Jane Hsiao, Pan-Chyr Yang, Meng-Hua Lee
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Patent number: 10815197Abstract: The present invention discloses an N-sulfonyl benzamide derivative with a heterocyclic substituent, and a preparation method therefor and a pharmaceutical application thereof. More specifically, the invention discloses a compound represented by formula (II) or a pharmaceutically acceptable salt, stereoisomer, solvent compound, or prodrug thereof, and a preparation method therefor and an application thereof. Refer to the specification for definitions of each group in the formula.Type: GrantFiled: January 24, 2017Date of Patent: October 27, 2020Assignees: SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.Inventors: Jiong Lan, Fusheng Zhou, Jinzhu Zhao, Dong Huang, Jing Xie, Yi Hu, Qiang Lv
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Patent number: 10813999Abstract: The invention provides liquid or semi-solid pharmaceutical compositions for topical administration comprising a semifluorinated alkane. The compositions are useful for the delivery of active ingredients into the deep layers of the skin or skin appendages. Various active ingredients may be incorporated, such as immunosuppressants, antiinfectives, antifungal agents, antiinflammatory agents, and retinoids.Type: GrantFiled: September 29, 2017Date of Patent: October 27, 2020Assignee: NOVALIQ GMBHInventors: Bernhard Gunther, Bastian Theisinger, Sonja Theisinger, Dieter Scherer
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Patent number: 10736859Abstract: The present invention relates to pharmaceutical compositions and methods of manufacturing the same, comprising a eutectic of Cyclobenzaprine HCl and mannitol or Amitriptyline HCl and mannitol.Type: GrantFiled: June 3, 2019Date of Patent: August 11, 2020Assignee: Tonix Pharma Holdings LimitedInventors: Marino Nebuloni, Patrizia Colombo
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Patent number: 10709671Abstract: The present invention relates to the use of cannabidiol (CBD) in the treatment of focal seizures. In one embodiment the patients suffering from focal seizures are children and young adults. CBD appears particularly effective in reducing focal seizures in patients suffering with etiologies that include: Lennox-Gastaut Syndrome; Tuberous Sclerosis Complex; Dravet Syndrome; CDKL5; Neuronal ceroid lipofuscinoses (NCL); febrile infection related epilepsy syndrome (FIRES); Aicardi syndrome and brain abnormalities in comparison to other seizure types. Significantly CBD additionally is very effective in the reduction of a sub-type of focal seizures, focal seizures with impairment.Type: GrantFiled: June 16, 2016Date of Patent: July 14, 2020Assignee: GW Research LimitedInventors: Geoffrey Guy, Stephen Wright, Orrin Devinsky
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Patent number: 10662146Abstract: Disclosed herein are pharmaceutical compositions with fencamfamine or fencamfamine related prodrug derivatives. The pharmaceutical compositions are for targeted therapeutic applications including, but not limited to, treating cancer-related fatigue, apathy in Alzheimer's Disease, major depression, and attention deficit-hyperactivity disorder. Also disclosed are methods of synthesizing the pharmaceutical compositions with fencamfamine or fencamfamine related prodrug derivatives.Type: GrantFiled: September 13, 2016Date of Patent: May 26, 2020Assignee: PRAXIS BIORESEARCH, LLCInventors: Sandeep Patil, Ron Bihovsky, Steven A. Smith, Yuhua Ji, Valentino Stella, Daniel D. Long, Daniel Marquess
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Patent number: 10653662Abstract: Methods of preventing early awakenings, and improving sleep efficiency in hours 7 and 8 of a period of sleep, by administration of low doses of doxepin (e.g., 1-6 mg).Type: GrantFiled: March 25, 2019Date of Patent: May 19, 2020Assignees: Currax Pharmaceuticals LLC, ProCom One, Inc.Inventors: Roberta L. Rogowski, Susan E. Dubé, Philip Jochelson, Neil B. Kavey
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Patent number: 10640490Abstract: The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.Type: GrantFiled: November 15, 2017Date of Patent: May 5, 2020Assignee: Yuhan CorporationInventors: Hyun-Joo Lee, Dong-Hoon Kim, Tae-Kyun Kim, Young-Ae Yoon, Jae-Young Sim, Myung-Hun Cha, Eun-Jung Jung, Kyoung-Kyu Ahn, Tai-Au Lee
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Patent number: 10583150Abstract: The present invention relates to a pharmaceutical composition for treating macular degeneration, and more particularly to a pharmaceutical composition for treating macular degeneration, which comprises an inhibitor of mTOR gene expression. The pharmaceutical composition according to the present invention can effectively treat age-related macular degeneration, a representative retinal disease that causes blindness in adults.Type: GrantFiled: March 17, 2017Date of Patent: March 10, 2020Assignee: CuroGene Life Sciences Co., Ltd.Inventors: Young-Ill Lee, Steven Hyun Seung Lee, Tae Kwann Park
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Patent number: 10518112Abstract: Method for ameliorating secondary pulmonary hypertension in a patient including determining a pulmonary vascular resistance (PVR) of the patient suffering from secondary pulmonary hypertension; assessing a change in the PVR in response to a selection treatment; and treating the patient with a pulmonary artery manipulation device to provide pulmonary artery denervation if the patient is determined to suffer from fixed PH, thereby ameliorating the secondary pulmonary hypertension of the patient.Type: GrantFiled: June 16, 2015Date of Patent: December 31, 2019Assignee: SONIVIE LTD.Inventor: Rotem Gilad
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Patent number: 10421779Abstract: The present invention relates to a carbazole compound having anti-virus activity, and more particularly, to a novel compound selected from the group of consisting of a carbazole compound which shows excellent anti-proliferative efficacy against hepatitis C virus (HCV), a pharmaceutically acceptable salt thereof, a hydrate thereof, and an isomer thereof; an anti-virus pharmaceutical composition including the novel compound as an active ingredient; a pharmaceutical composition for preventing or treating liver diseases caused by hepatitis C virus; and a method of preparing the novel compound.Type: GrantFiled: August 25, 2017Date of Patent: September 24, 2019Assignees: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY, POSTECH ACADEMY-INDUSTRY FOUNDATIONInventors: Gyo Chang Keum, Eunice Eun Kyeong Kim, Sung Key Jang, Hee Sun Kim, Ae Nim Pae, Hua Li, Jin Hyeong Park, Jin Sook Kwak
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Patent number: 10420318Abstract: A methylphenidate, particularly including dextro-threo-methylphenidate, is administered to a subject to treat a speech, gait or limb impairment secondary to a genetically acquired pre-frontal cortex processing disease or disorder, particularly including multiple sclerosis, cerebral palsy, Angelman syndrome, Rett syndrome and Fragile-X syndrome.Type: GrantFiled: August 14, 2018Date of Patent: September 24, 2019Assignee: GILROSE PHARMACEUTICALS, LLCInventors: Bruce Roseman, Gilla Kaplan
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Patent number: 10406189Abstract: Compositions and methods for the treatment and prevention of at least one of a sign and a symptom associated with an eye disease are disclosed. Preferred compositions could comprise a liquid formulation including Cineraria maritima and at least one of a nonsteroidal anti-inflammatory drug, a carnosine, and a cannabinoid.Type: GrantFiled: January 13, 2016Date of Patent: September 10, 2019Inventor: Leonidas A. Johnson
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Patent number: 10376523Abstract: An aqueous composition having an excellent antiseptic effect is provided. An aqueous composition containing: a compound represented by Formula (1), a salt thereof, or a solvate of the compound or the salt thereof, where X represents a halogen atom, and a quaternary ammonium surfactant. A method for producing an aqueous composition with an antiseptic effect, by incorporating a compound represented by Formula (1), a salt thereof, or a solvate of the compound or the salt thereof and a quaternary ammonium surfactant into the aqueous composition.Type: GrantFiled: September 25, 2015Date of Patent: August 13, 2019Assignee: KOWA COMPANY, LTD.Inventor: Shin Sugimoto
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Patent number: 10258498Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder mediType: GrantFiled: November 22, 2012Date of Patent: April 16, 2019Assignee: Richter Gedeon NYRT.Inventors: Ferenc Fülöp, László Vigh, Zsolt Török, Botond Penke, Ibolya Horváth, Gábor Balogh, Sándor Bernáth, Ákos Hunya
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Patent number: 10239861Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein R1-R3 have any of the values defined in the specification. The compounds and salts are useful for treating PCAF mediated disorders and/or GCN5 mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as and methods of using said compounds, salts, or compositions in the treatment of various disorders.Type: GrantFiled: July 7, 2017Date of Patent: March 26, 2019Assignees: GENETECH, INC., CONSTELLATION PHARMACEUTICALS, INC.Inventors: Brian K. Albrecht, Daniel J. Burdick, Alexandre Cote, Martin Duplessis, Christopher G. Nasveschuk, Alexander M. Taylor
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Patent number: 10239841Abstract: The invention relates to a production method of pyrazole derivative (6) by reacting compound (5) with an oxidant. wherein R1, R2, R3, X1, X2 and Z1 are as defined herein.Type: GrantFiled: March 23, 2016Date of Patent: March 26, 2019Assignee: AGC Inc.Inventors: Yuichiro Ishibashi, Yosuke Ochi, Noriaki Miyake, Yusuke Yamazaki, Shota Shimizu
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Patent number: 10149838Abstract: The present invention relates to use of novel securinine and norsecurine analogs to bind and/or inhibit myeloperoxidase activity.Type: GrantFiled: October 3, 2014Date of Patent: December 11, 2018Inventors: Mahesh K. Gundluru, Mukesh Agarwal, Zhiqing Xia, Goutam Karan, David Wald
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Patent number: 10085414Abstract: A methylphenidate, particularly including dextro-threo-methylphenidate, is administered to a subject to treat a speech, gait or limb impairment secondary to a genetically acquired pre-frontal cortex processing disease or disorder, particularly including multiple sclerosis, cerebral palsy, Angelman syndrome, Rett syndrome and Fragile-X syndrome.Type: GrantFiled: May 16, 2017Date of Patent: October 2, 2018Assignee: GILROSE PHARMACEUTICALS, LLCInventors: Bruce Roseman, Gilla Kaplan
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Patent number: 9937186Abstract: A genus of arylsulfonamide derivatives of aminocycloalkanols is disclosed. The compounds are of the following genus: The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.Type: GrantFiled: March 10, 2015Date of Patent: April 10, 2018Assignee: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAIInventors: Michael Ohlmeyer, David Kastrinsky
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Patent number: 9937180Abstract: Tricyclic chemical modulators of protein phosphatase 2A are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne.Type: GrantFiled: March 10, 2015Date of Patent: April 10, 2018Assignee: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAIInventors: Michael Ohlmeyer, David Kastrinsky
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Patent number: 9913833Abstract: Methods of treating developmental disorders by administering a pharmaceutical composition of pipradrol or a pharmaceutically acceptable salt thereof are provided. The methods may be used to treat conditions such as epilepsy, Landau-Kleffner Syndrome, Lennox-Gastaut syndrome (LGS) and Dravet syndrome.Type: GrantFiled: April 21, 2017Date of Patent: March 13, 2018Assignee: OVID THERAPEUTICS INCInventor: Matthew During
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Patent number: 9895353Abstract: Described is the use of L-tryptophan for treating a subject with parasomnia and associated methods of treating a subject with parasomnia. Optionally, the subject may be a child or adolescent between about 3 years of age and 18 years of age. The methods and uses described herein are useful for treating parasomnia in a subject exhibiting sleep walking, sleeptalking, confusional arousals, nightmares, night terrors, rhythmic movement disorder, sleep related eating disorder and/or bruxism. Optionally, subjects are treated with a dose L-tryptophan of about between 700 mg and 5 g per day.Type: GrantFiled: September 10, 2014Date of Patent: February 20, 2018Assignee: Zzeemag Inc.Inventors: Colin Shapiro, Louis Van Zyl
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Patent number: 9855277Abstract: The use of 5H-dibenz/b,f/azepine-5-carboxamide derivatives for treating fibromyalgia. Useful 5H-dibenz/b,f/azepine-5-carboxamide derivatives include compounds of the formula (I): where R1 is hydrogen, alkyl, halogenalkyl, aralkyl, cycloalkyl, cycloalkylalkyl, alkoxy, aryl, or pyridyl; the term alkyl means a straight or branched hydrocarbon chain containing from 1 to 18 carbon atoms; the term halogen means fluorine, chlorine, bromine or iodine; the term cycloalkyl means an alicyclic saturated group with 3 to 6 carbon atoms; and the term aryl means an unsubstituted phenyl group or phenyl substituted by alkoxy, halogen or nitro group.Type: GrantFiled: July 27, 2009Date of Patent: January 2, 2018Assignee: BIAL—PORTELA & CA, S.A.Inventor: Patricio Manuel Viera Araújo Soares Da Silva
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Patent number: 9801847Abstract: The invention relates to use of the cis-(Z) isomer or isomeric mixtures containing specified ratios of the cis-(Z) and trans-(E) isomers of doxepin, metabolites of doxepin, pharmaceutically-acceptable salts of doxepin and prodrugs of the same; compositions containing the same, for the treatment of sleep disorders.Type: GrantFiled: October 10, 2016Date of Patent: October 31, 2017Assignees: Pernix Sleep, Inc., ProCom One, Inc.Inventors: Susan E. Dubé, Neil B. Kavey
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Patent number: 9796720Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which the variables are as defined in the specification.Type: GrantFiled: August 21, 2014Date of Patent: October 24, 2017Assignee: Bristol-Myers Squibb CompanyInventors: Michael G. Yang, Zili Xiao, David S. Weinstein
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Patent number: 9763954Abstract: New applications of eslicarbazepine and eslicarbazepine acetate in the treatment of intractable conditions.Type: GrantFiled: December 19, 2013Date of Patent: September 19, 2017Assignee: BIAL—PORTELA & CA, S.A.Inventor: Patricio Manuel Vieira Araújo Soares Da Silva
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Patent number: 9738631Abstract: The invention relates to the compounds of formula I and formula IA or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I and formula IA; and methods for treating or preventing neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of epilepsy, bipolar disorder, trigeminal neuralgia, attention-deficit hyperactivity disorder (ADHD), schizophrenia, neuropathic pain, seizures, bipolar disorder, mania, phantom limb syndrome, complex regional pain syndrome, paroxysmal extreme pain disorder, neuromyotonia, intermittent explosive disorder, borderline personality disorder, Myotonia congenita and post-traumatic stress disorder.Type: GrantFiled: January 28, 2013Date of Patent: August 22, 2017Assignee: CELLIX BIO PRIVATE LIMITEDInventor: Mahesh Kandula
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Patent number: 9695144Abstract: The present disclosure provides dibenzazepine derivatives having Formula I or I(A): and the pharmaceutically acceptable salts and solvates thereof, wherein R3a, R3b, R6, V1, V2, Z1, Z2, Z3, and G are defined as set forth in the specification. The present disclosure is also directed to the use of the compounds of Formula I or I(A), and the pharmaceutically acceptable salts or solvates thereof, to treat a disorder responsive to the blockade of one or more sodium channels. In one embodiment, the compounds of the present disclosure are useful for treating pain.Type: GrantFiled: November 25, 2014Date of Patent: July 4, 2017Assignee: Purdue Pharma L.P.Inventors: Stephen M. Lynch, Laykea Tafesse
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Patent number: 9643929Abstract: A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(?)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX2(L)]2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R1 is chosen from C1-6 alkoxy and C1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R1 can be the same or different, and R2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR3R4R5 and formic acid, [R3R4R5NH][OOCH] and optionally formic acid, or [M][OOCH]x and formic acid, wherein R3, R4 and R5 are C1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.Type: GrantFiled: November 18, 2015Date of Patent: May 9, 2017Assignee: BIAL—PORTELA & CA, S.A.Inventors: David Alexander Learmonth, Gabriela Alexandra Grasa, Antonio Zanotti-Gerosa
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Patent number: 9567291Abstract: This disclosure relates to N-(4-(bis(4-(dimethylamino)phenyl)methylene)-8 -(dimethylamino)naphthalen-1(4H)-ylidene)-N-methylmethanaminium, derivatives, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula I. In certain embodiments, the disclosure relates to methods of treating or preventing Nox related diseases and conditions comprising administering an effective amount of compounds disclosed herein to a subject in need thereof. In certain embodiments, the Nox related disease or condition is cancer.Type: GrantFiled: April 25, 2014Date of Patent: February 14, 2017Assignee: Emory UniversityInventor: Jack Arbiser
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Patent number: 9540358Abstract: Tricyclic chemical modulators of FOXO transcription factor proteins are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne.Type: GrantFiled: August 16, 2012Date of Patent: January 10, 2017Assignee: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAIInventors: Michael Ohlmeyer, Goutham Narla, Neil Dhawan, David Kastrinsky
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Patent number: 9494572Abstract: The present invention relates to anti-cancer therapeutics. In certain aspects, cancers are treated with a combination of an anti-EGFR agent and an agent that increases the activity of the KLF6 tumor suppressor gene and/or an agent that increases activity of the FOXO1 tumor suppressor gene. In a preferred aspect, the anti-EGFR agent erlotinib a tricyclic agent compound, are used in combination to treat non-small cell lung cancer in a patient with primary or acquired drug resistance to erlotinib, and wherein the tricyclic agent is administered in an amount that does not lead to a substantial central nervous system effect. In additional aspects, the invention relates to compositions and kits useful for treating cancers, methods for screening for compounds that enhance the activity of anti-EGFR agent, and methods for determining whether a patient will respond to anti-EGFR therapy.Type: GrantFiled: February 6, 2015Date of Patent: November 15, 2016Assignee: Icahn School of Medicine at Mount SinaiInventors: Goutham Narla, Michael Ohlmeyer, Matthew David Galsky, Suzanna Katz
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6-substituted-3-1,3-benzothiazol-2-one compounds as TARP-gamma 8 dependent AMPA receptor antagonists
Patent number: 9469632Abstract: A TARP ?8 dependant AMPA receptor antagonist of the formula: wherein X is CH or N; A is and R1 is as defined herein; its pharmaceutically acceptable salts, uses, and methods for its preparation are described.Type: GrantFiled: May 21, 2015Date of Patent: October 18, 2016Assignee: Eli Lilly and CompanyInventors: Kevin Matthew Gardinier, Douglas Linn Gernert, Patric James Hahn, Sean Patrick Hollinshead, Albert Khilevich, Daniel Ray Mayhugh, Paul Leslie Ornstein, Warren Jaye Porter, Jon Kevin Reel, Jeffrey Michael Schkeryantz, Patrick Gianpietro Spinazze, Freddie Craig Stevens, Jeffrey Michael Witkin -
Patent number: 9394327Abstract: The uses of antifreeze proteins (AFPs), including polypeptides, peptides, fragments of AFPs, and mimicries of AFPs, as highly efficient additives for crystal growth control are provided. AFPs are demonstrated to efficiently inhibit the nucleation of commercially and pharmaceutically important compounds (e.g., nucleosides, sugars, salts), increase the supersaturation of their solutions, modify their crystal habits, and result in novel morphologies.Type: GrantFiled: March 15, 2013Date of Patent: July 19, 2016Assignee: The Trustees of California State UniversityInventors: Xin Wen, Sen Wang
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Patent number: 9351968Abstract: Methods of treating developmental disorders by administering a pharmaceutical composition of pipradrol or a pharmaceutically acceptable salt thereof are provided. The methods may be used to treat conditions such as epilepsy, Landau-Kleffner Syndrome, Lennox-Gastaut syndrome (LGS) and Dravet syndrome.Type: GrantFiled: October 6, 2015Date of Patent: May 31, 2016Assignee: OVID THERAPEUTICS INCInventor: Matthew During
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Patent number: 9346760Abstract: The present invention provides a novel process for the preparation of substituted optically pure (S)-(+)- or (R)-(?)-10-hydroxy-dihydrodibenz[b,f]azepines or derivatives thereof, starting from 10,11-dihydro-10-oxo-5H-dibenz[b,f]azepines using boronate esters or their derivatives. The present invention also provides use of thus prepared (S)-(+)- or (R)-(?)-10-hydroxy-dihydrodibenz[b,f]azepines for the preparation of their ester such as (S)-(?)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide or (R)-(+)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide. The present invention also provides novel solid state crystalline forms J1, J2, J3, J4 and amorphous form of eslicarbazepine and the process for the preparation thereof. Also, the present invention provides novel solid state crystalline form and amorphous form of eslicarbazepine acetate and the process for the preparation thereof.Type: GrantFiled: March 6, 2012Date of Patent: May 24, 2016Assignee: JUBILANT LIFE SCIENCES LIMITEDInventors: Sujay Biswas, Shailendra Kumar Dubey, Vikas Bansal, Mukesh Masand, Dharam Vir
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Patent number: 9234885Abstract: Methods and assays for treating a subject with a filovirus infection using an agent that inhibits Niemann-Pick CI (NPCI), VPSII, VPSI6, VPSI8, VPS33A, VPS39, VPS41, BLOCISI, BLOCIS2, GNPTAB, PIKFYVE, ARHGAP23 or FIG4. Methods for screening for an agent that treats and/or prevents infection of a subject with a filovirus, where the methods comprise determining whether the agent inhibits one or more of Niemann-Pick CI (NPCI), VPSII, VPSI6, VPSI8, VPS33A, VPS39, VPS41. BLOCISI, BLOCIS2, GNPTAB, PIKFYVE, ARHGAP23 or FIG4, wherein an agent that inhibits one or more of NPCI, VPSII, VPSI6, VPSI8, VPS33A, VPS39, VPS41, BLOCISI, BLOCIS2, GNPTAB, PIKFYVE, ARHGAP23 or FIG4 is a candidate for treating and/or preventing an infection with a filovirus and wherein an agent that does not inhibit NPCI, VPSII, VPSI6, VPSI8, VPS33A. VPS39, VPS41, BLOCISI, BLOCIS2, GNPTAB, PIKFYVE, ARHGAP23 or FIG4 is not a candidate for treating and/or preventing an infection with a filovirus.Type: GrantFiled: January 24, 2012Date of Patent: January 12, 2016Assignees: Albert Einstein College of Medicine, Inc., President and Fellows of Harvard College, Whitehead Institute For Biomedical ResearchInventors: Kartik Chandran, Sean Whelan, Thijn Brummelkamp, Jan Carette, Matthijs Raaben
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Patent number: 9221779Abstract: Novel serotonin reuptake inhibitor compounds which are designed to exert serotonin uptake inhibitory activity in the peripheral system while being devoid of CNS activity, and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with peripheral serotonin levels and/or activity, and/or platelet aggregation.Type: GrantFiled: June 21, 2007Date of Patent: December 29, 2015Assignee: Ramot at Tel-Aviv University Ltd.Inventors: Moshe Rehavi, David Gurwitz