Tropanes (including Nor Or Dehydro Form) Patents (Class 514/304)
  • Patent number: 11739098
    Abstract: Disclosed are compounds of Formula (I) or salts thereof, wherein Ring Het, R1, R2, R3, R4, R5, m, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: March 21, 2022
    Date of Patent: August 29, 2023
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, Dharmpal S. Dodd, Christopher P. Mussari, Trevor C. Sherwood, John L. Gilmore, Tasir Shamsul Haque, Brian K. Whiteley, David R. Tortolani, Shoshana L. Posy, John E. Macor, Louis J. Lombardo, Ramesh Kumar Sistla, Anupama Kandhi Ramachandra Reddy, Subramanya Hegde, Laxman Pasunoori, Sreekantha Ratna Kumar
  • Patent number: 11642339
    Abstract: The present invention relates to methods and pharmaceutical compositions for treatment of all symptoms of gastroparesis in a human patient, the method comprising administering to the human patient between about 0.5 mg/day to about 30 mg/day, about 0.5 mg/day to about 15 mg/day, about 0.5 mg/day to about 5 mg/day, or about 5 mg/day, of velusetrag or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: July 30, 2018
    Date of Patent: May 9, 2023
    Assignees: THERAVANCE BIOPHARMA R&D IP, LLC, ALFASIGMA S.P.A.
    Inventors: Christopher Noel Barnes, Giuseppe Claudio Viscomi, Cecilia Renzulli, Maria Grimaldi
  • Patent number: 11504360
    Abstract: The present invention generally relates to compositions and methods for treating a neurological disorder in a subject, the method including administering to the subject in need of such treatment a composition including a therapeutically effective amount of a CCR5 antagonist. The CCR5 antagonist may be, for example, maraviroc. The neurological disorder may be, for example, Alzheimer's disease, Parkinson's disease, dementia with Lewy bodies or multiple system atrophy.
    Type: Grant
    Filed: December 28, 2018
    Date of Patent: November 22, 2022
    Assignee: Rush University Medical Center
    Inventor: Kalipada Pahan
  • Patent number: 11382909
    Abstract: Provided herein is an ophthalmic composition. In some embodiments, the ophthalmic composition includes a low concentration of an ophthalmic agent for treatment of an ophthalmic disorder or condition; and an ophthalmically acceptable carrier, wherein the ophthalmic agent is distributed with substantial uniformity throughout the ophthalmically acceptable carrier. Further disclosed herein include an ophthalmic composition including a low concentration of an ophthalmic agent and deuterated water. Also disclosed herein are methods of arresting or preventing myopia development by administering to an eye of an individual in need thereof an effective amount of an ophthalmic composition as described herein.
    Type: Grant
    Filed: November 7, 2019
    Date of Patent: July 12, 2022
    Assignee: SYDNEXIS, INC.
    Inventors: Gregory I. Ostrow, Kenneth J. Widder, David S. Baker, Harun Takruri
  • Patent number: 11325904
    Abstract: In various embodiments, compositions and methods are provided for treatment and/or prevention of amyloidogenic diseases. In certain embodiments, the methods entail administering an effective amount of a tropinol ester to a subject in need thereof for prophylactic or therapeutic effect. The methods are particularly useful for prophylactic and therapeutic treatment of Alzheimer's disease. In certain embodiments, methods of reducing the risk, lessening the severity, or delaying the progression or onset of a disease characterized by beta-amyloid deposits in the brain of a mammal are also provided. In certain embodiments, methods of directly or indirectly inhibiting the C-terminal cleavage of APP resulting in the formation of APP-C31 peptide and APPneo (AP-P664) in a mammal are provided.
    Type: Grant
    Filed: August 1, 2012
    Date of Patent: May 10, 2022
    Assignee: BUCK INSTITUTE FOR RESEARCH ON AGING
    Inventors: Varghese John, Dale E. Bredesen
  • Patent number: 11253507
    Abstract: Methods of preventing or delaying onset of myopia in pre-myopic patients and also methods of reducing or preventing progression of myopia in patients having low myopia through the use of compositions comprising less than 0.025% of atropine are disclosed.
    Type: Grant
    Filed: February 20, 2018
    Date of Patent: February 22, 2022
    Assignee: Singapore Health Services Ptd Ltd
    Inventors: Donald Tiang Hwee Tan, Audrey Chia, Roger Beuerman, Amutha Barathi Veluchamy
  • Patent number: 10953002
    Abstract: Provided herein is an ophthalmic composition. In some embodiments, the ophthalmic composition includes a low concentration of an ophthalmic agent for treatment of an ophthalmic disorder or condition; and an ophthalmically acceptable carrier, wherein the ophthalmic agent is distributed with substantial uniformity throughout the ophthalmically acceptable carrier. Further disclosed herein include an ophthalmic composition including a low concentration of an ophthalmic agent and deuterated water. Also disclosed herein are methods of arresting or preventing myopia development by administering to an eye of an individual in need thereof an effective amount of an ophthalmic composition as described herein.
    Type: Grant
    Filed: February 7, 2020
    Date of Patent: March 23, 2021
    Assignee: SYDNEXIS, INC.
    Inventors: Gregory I. Ostrow, Kenneth J. Widder, David S. Baker, Harun Takruri
  • Patent number: 10940145
    Abstract: Provided herein is an ophthalmic composition. In some embodiments, the ophthalmic composition includes a low concentration of an ophthalmic agent for treatment of an ophthalmic disorder or condition; and an ophthalmically acceptable carrier, wherein the ophthalmic agent is distributed with substantial uniformity throughout the ophthalmically acceptable carrier. Further disclosed herein include an ophthalmic composition including a low concentration of an ophthalmic agent and deuterated water. Also disclosed herein are methods of arresting or preventing myopia development by administering to an eye of an individual in need thereof an effective amount of an ophthalmic composition as described herein.
    Type: Grant
    Filed: February 7, 2020
    Date of Patent: March 9, 2021
    Assignee: SYDNEXIS, INC.
    Inventors: Gregory I. Ostrow, Kenneth J. Widder, David S. Baker, Harun Takruri
  • Patent number: 10888557
    Abstract: Provided herein is an ophthalmic composition. In some embodiments, the ophthalmic composition includes a low concentration of an ophthalmic agent for treatment of an ophthalmic disorder or condition; and an ophthalmically acceptable carrier, wherein the ophthalmic agent is distributed with substantial uniformity throughout the ophthalmically acceptable carrier. Further disclosed herein include an ophthalmic composition including a low concentration of an ophthalmic agent and deuterated water. Also disclosed herein are methods of arresting or preventing myopia development by administering to an eye of an individual in need thereof an effective amount of an ophthalmic composition as described herein.
    Type: Grant
    Filed: February 7, 2020
    Date of Patent: January 12, 2021
    Assignee: SYDNEXIS, INC.
    Inventors: Gregory I. Ostrow, Kenneth J. Widder, David S. Baker, Harun Takruri
  • Patent number: 10842787
    Abstract: Provided herein is an ophthalmic composition. In some embodiments, the ophthalmic composition includes a low concentration of an ophthalmic agent for treatment of an ophthalmic disorder or condition; and an ophthalmically acceptable carrier, wherein the ophthalmic agent is distributed with substantial uniformity throughout the ophthalmically acceptable carrier. Further disclosed herein include an ophthalmic composition including a low concentration of an ophthalmic agent and deuterated water. Also disclosed herein are methods of arresting or preventing myopia development by administering to an eye of an individual in need thereof an effective amount of an ophthalmic composition as described herein.
    Type: Grant
    Filed: April 25, 2016
    Date of Patent: November 24, 2020
    Assignee: SYDNEXIS, INC.
    Inventors: Gregory I. Ostrow, Kenneth J. Widder, David S. Baker, Harun Takruri
  • Patent number: 10813923
    Abstract: Provided herein is an ophthalmic composition. In some embodiments, the ophthalmic composition includes a low concentration of an ophthalmic agent for treatment of an ophthalmic disorder or condition; and an ophthalmically acceptable carrier, wherein the ophthalmic agent is distributed with substantial uniformity throughout the ophthalmically acceptable carrier. Further disclosed herein include an ophthalmic composition including a low concentration of an ophthalmic agent and deuterated water. Also disclosed herein are methods of arresting or preventing myopia development by administering to an eye of an individual in need thereof an effective amount of an ophthalmic composition as described herein.
    Type: Grant
    Filed: June 22, 2020
    Date of Patent: October 27, 2020
    Assignee: SYDNEXIS, INC.
    Inventors: Gregory I. Ostrow, Kenneth J. Widder, David S. Baker, Harun Takruri
  • Patent number: 10695338
    Abstract: Methods and compositions for treating a lysosomal movement associated disease in an animal, in which the position of lysosomes can influence disease progression, comprising administering an effective amount of a first lysosome migration inhibitor or a pharmaceutically acceptable salt, solvate, clathrate, stereoisomer, enantiomer or prodrug thereof.
    Type: Grant
    Filed: May 6, 2016
    Date of Patent: June 30, 2020
    Assignee: Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
    Inventors: James Allen Cardelli, Magdalena Liliana Circu, Samantha Sarah Dykes, Hazem Edmond El-Osta
  • Patent number: 10610525
    Abstract: The inventive subject matter is directed to compositions and methods for sterile and storage stable low-dose atropine formulations with improved stability. Most preferably, the compositions presented herein are substantially preservative free and exhibit less than 0.35% tropic acid from degradation of atropine. Advantageously, contemplated formulations are also substantially free of preservatives.
    Type: Grant
    Filed: February 20, 2019
    Date of Patent: April 7, 2020
    Assignee: Nevakar Inc.
    Inventors: Navneet Puri, Prem Sagar Akasapu, Irfan A. Mohammed, Kumaresh Soppimath, Iouri V. Ilitchev
  • Patent number: 10583132
    Abstract: The inventive subject matter is directed to compositions and methods for sterile and storage stable low-dose atropine formulations with improved stability. Most preferably, the compositions presented herein are substantially preservative free and exhibit less than 0.35% tropic acid from degradation of atropine. Advantageously, contemplated formulations are also substantially free of preservatives.
    Type: Grant
    Filed: February 20, 2019
    Date of Patent: March 10, 2020
    Assignee: Nevakar Inc.
    Inventors: Navneet Puri, Prem Sagar Akasapu, Irfan A. Mohammed, Kumaresh Soppimath, Iouri V. Ilitchev
  • Patent number: 10576074
    Abstract: The inventive subject matter is directed to compositions and methods for sterile and storage stable low-dose atropine formulations with improved stability. Most preferably, the compositions presented herein are substantially preservative free and exhibit less than 0.35% tropic acid from degradation of atropine. Advantageously, contemplated formulations are also substantially free of preservatives.
    Type: Grant
    Filed: February 20, 2019
    Date of Patent: March 3, 2020
    Assignee: Nevakar Inc.
    Inventors: Navneet Puri, Prem Sagar Akasapu, Irfan A. Mohammed, Kumaresh Soppimath, Iouri V. Ilitchev
  • Patent number: 10568875
    Abstract: The inventive subject matter is directed to compositions and methods for sterile and storage stable low-dose atropine formulations with improved stability. Most preferably, the compositions presented herein are substantially preservative free and exhibit less than 0.35% tropic acid from degradation of atropine. Advantageously, contemplated formulations are also substantially free of preservatives.
    Type: Grant
    Filed: February 20, 2019
    Date of Patent: February 25, 2020
    Assignee: Nevakar Inc.
    Inventors: Navneet Puri, Prem Sagar Akasapu, Irfan A. Mohammed, Kumaresh Soppimath, Iouri V. Ilitchev
  • Patent number: 10556899
    Abstract: Provided is a method for preparing a tropane derivative, maraviroc, including reacting a compound of formula (II) with a compound of formula (I), wherein the compound of formula (II) is prepared by the steps of acetylation of a compound of formula (III), activation and substitution of a compound of formula (IV) by a chlorination agent, cyclization of a compound of formula (V), and debenzylation of a compound of formula (VI) by hydrogenation. Hence, the present disclosure provides a method for preparing maraviroc with good yield and simple operation.
    Type: Grant
    Filed: January 25, 2019
    Date of Patent: February 11, 2020
    Assignee: SCI Pharmtech, Inc.
    Inventors: Heng-Yen Wang, Chen-Yi Kao
  • Patent number: 10548887
    Abstract: Pharmaceutical compositions containing a combination of anti-chondrogenesis agents are disclosed. Methods of reducing scleral chondrogenesis, reducing one or more ocular chondrogenic proteins, reducing inflammation induced chondrogenesis and treating myopia by administering an effective amount of one or more anti-chondrogenesis agents are also provided. The pharmaceutical compositions are useful for treating myopia.
    Type: Grant
    Filed: April 20, 2018
    Date of Patent: February 4, 2020
    Assignees: Kaohsiung Chang Gung Memorial Hospital, Philip WU
    Inventors: Pei-Chang Wu, Chia-Ling Tsai, Chueh-Tan Chen
  • Patent number: 10364242
    Abstract: Pharmaceutical compositions make up a compound acting as inhibitor of N-acylethanolamine-hydrolyzing acid amidase (NAAA), may be used for the therapeutical treatment and prevention of pain and inflammatory disorders and other disorders which benefit from the modulation of fatty acid ethanolamines, particularly palmitoylethanolamide (PEA). The compound is used in methods of inhibiting NAAA and methods of therapeutical treatment and prevention of pain and inflammation.
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: July 30, 2019
    Assignee: FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIA
    Inventors: Fabio Bertozzi, Tiziano Bandiera
  • Patent number: 10251875
    Abstract: The inventive subject matter is directed to compositions and methods for sterile and storage stable low-dose atropine formulations with improved stability. Most preferably, the compositions presented herein are substantially preservative free and exhibit less than 0.35% tropic acid from degradation of atropine. Advantageously, contemplated formulations are also substantially free of preservatives.
    Type: Grant
    Filed: May 10, 2018
    Date of Patent: April 9, 2019
    Assignee: Nevakar Inc.
    Inventors: Navneet Puri, Prem Sagar Akasapu, Irfan A. Mohammed, Kumaresh Soppimath, Iouri V. Ilitchev, Tao Zhang
  • Patent number: 10005711
    Abstract: The present invention relates to a process suitable for adoption to large scale manufacture of 1-isopropyl-3-{5-[1-(3-methoxypropyl)piperidin-4-yl]-[1,3,4]oxadiazol-2-yl}-1H-indazole oxalate of formula (I), which is a selective 5-HT4 receptor ligand intended for the symptomatic treatment of Alzheimer's disease and other disorders of memory and cognition like Attention deficient hyperactivity, Parkinson's and Schizophrenia.
    Type: Grant
    Filed: October 23, 2014
    Date of Patent: June 26, 2018
    Assignee: SUVEN LIFE SCIENCES LIMITED
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Venkateswarlu Jasti
  • Patent number: 9944601
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Grant
    Filed: September 21, 2016
    Date of Patent: April 17, 2018
    Assignee: ORYZON GENOMICS, S.A.
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Àngeles Estiarte Martinez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Patent number: 9827250
    Abstract: Ophthalmic devices, such as contact lenses, may incorporate myopia control optics in combination with therapeutic agents also known to control myopia to create a drug delivery mechanism to inhibit or arrest the progression of myopia in individuals. Any number of contact lenses incorporating myopia control optics may be combined with a therapeutic agent such as atropine, atropine sulphate monohydrate, and/or pirenzepine.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: November 28, 2017
    Assignee: Johnson & Johnson Vision Care, Inc.
    Inventors: Khaled Chehab, Arthur H. Shedden, Jr., Xu Cheng
  • Patent number: 9603817
    Abstract: The invention features a method for inhibiting one or more voltage-gated ion channels in a cell by contacting the cell with (i) a first compound that activates a channel-forming receptor that is present on nociceptors and/or pruriceptors; and (ii) a second compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels, wherein the second compound is capable of entering nociceptors or pruriceptors through the channel-forming receptor when the receptor is activated. The invention also features a quarternary amine derivative or other permanently or transiently charged derivative of a compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels.
    Type: Grant
    Filed: September 25, 2014
    Date of Patent: March 28, 2017
    Assignees: President and Fellows of Harvard College, The General Hospital Corporation
    Inventors: Bruce P. Bean, Clifford J. Woolf
  • Patent number: 9605315
    Abstract: The present invention provides minimally invasive methods of detecting, diagnosing, and assessing neuronal damage associated with traumatic brain injury (TBI) or chronic traumatic encephalopathy (CTE). Specific species of microRNAs (miRNA), small, noncoding RNA molecules that play gene regulatory functions, are correlated with cellular damage and oxidative stress following TBI or CTE, allowing for rapid, minimally-invasive diagnosis and assessment of brain injury. The early identification and longitudinal assessment of neuronal damage in subjects suffering from or at risk of suffering from a TBI (e.g., football players, boxers, military personnel, fall victims) will improve clinical outcomes by guiding critical medical and behavioral decision making.
    Type: Grant
    Filed: March 26, 2015
    Date of Patent: March 28, 2017
    Assignee: The University of Montana
    Inventors: Sarjubhai Patel, Thomas Rau
  • Patent number: 9402840
    Abstract: The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: August 2, 2016
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Paul R. Fatheree, S. Derek Turner, Adam A. Goldblum, Robert S. Chao, Daniel Genov
  • Patent number: 9387184
    Abstract: This invention relates to the use of pharmaceutical compositions comprising a therapeutically effective combination of Tesofensine and Metoprolol for preventing the cardiovascular side effects of Tesofensine, while leaving the robust inhibitory efficacy on food intake and body weight loss unaffected.
    Type: Grant
    Filed: November 10, 2015
    Date of Patent: July 12, 2016
    Assignee: Saniona A/S
    Inventors: Henrik Bjork Hansen, Morten Grunnet, Bo Hjorth Bentzen, Lars Hyveled-Nielsen, Jorgen Buus Lassen, Claus Sundgreen
  • Patent number: 9353106
    Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: January 13, 2015
    Date of Patent: May 31, 2016
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-Ki Choi, Adam A. Goldblum
  • Patent number: 9345699
    Abstract: The invention provides isoquinoline, quinoline, and quinazoline derivatives to treat a variety of disorders, diseases and pathologic conditions, and more specifically to the use of isoquinoline, quinoline, and quinazoline derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds to the treatment of hyperproliferative diseases and pathologic angiogenesis.
    Type: Grant
    Filed: June 9, 2010
    Date of Patent: May 24, 2016
    Assignee: NantBioScience, Inc.
    Inventors: Chunlin Tao, Xiaowen Sun, Hongna Han, Lukasz Koroniak, Neil Desai
  • Patent number: 9265780
    Abstract: A method of enhancing the activity of lysosomal ?-Galactosidase A (?-Gal A) in mammalian cells and for treatment of Fabry disease by administration of 1-deoxy-galactonojirimycin and related compounds.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: February 23, 2016
    Assignee: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI
    Inventors: Jian-Qiang Fan, Satoshi Ishii
  • Patent number: 9241938
    Abstract: This invention relates to the use of trigonelline compounds to increase muscle weight during periods of activity or to inhibit muscle loss during periods of inactivity.
    Type: Grant
    Filed: November 20, 2014
    Date of Patent: January 26, 2016
    Assignee: DSM IP ASSETS B.V.
    Inventors: Angelika Friedel, Karin Kuratli, Christof Wehrli, Karin Wertz, Swen Wolfram, Ying Wang-Schmidt
  • Patent number: 9233106
    Abstract: The present invention relates to methods of using cocaine-binding-site ligands and cocaine-binding-site RNA aptamers to treat or prevent Alzheimer's Disease and to reduce or prevent aggregation of beta-amyloid peptides in a subject.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: January 12, 2016
    Assignee: CORNELL RESEARCH FOUNDATION, INC.
    Inventors: George P. Hess, Moataz M. Gadalla
  • Patent number: 9211271
    Abstract: This invention relates to the use of pharmaceutical compositions comprising a therapeutically effective combination of Tesofensine and Metoprolol for preventing the cardiovascular side effects of Tesofensine, while leaving the robust inhibitory efficacy on food intake and body weight loss unaffected.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: December 15, 2015
    Assignee: SANIONA A/S
    Inventors: Henrik Björk Hansen, Morten Grunnet, Bo Hjorth Bentzen, Lars Hyveled-Nielsen, Jørgen Buus Lassen, Claus Sundgreen
  • Patent number: 9199993
    Abstract: The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: June 26, 2014
    Date of Patent: December 1, 2015
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Daisuke Roland Saito, Daniel D. Long, Lan Jiang, Bryan Frieman
  • Patent number: 9163012
    Abstract: This invention relates to novel compounds of the invention pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: October 20, 2015
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Colin M. Tice, Linghang Zhuang, Katerina Leftheris, Yuanjie Ye, Suresh B. Singh
  • Patent number: 9133184
    Abstract: The present application discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the application discloses the use of these compounds, a method for therapy and to pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: April 28, 2014
    Date of Patent: September 15, 2015
    Assignee: ANIONA APS
    Inventors: Dan Peters, Gordon Munro, Elsebet Ostergaard Nielsen, Karin Sandager Nielsen
  • Patent number: 9126994
    Abstract: The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: September 8, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Paul R. Fatheree, S. Derek Turner, Adam A. Goldblum, Robert S. Chao, Daniel Genov
  • Patent number: 9108921
    Abstract: Compounds of general formula I: and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: August 18, 2015
    Assignee: AGIOS PHARMACEUTICALS, INC
    Inventors: Giovanni Cianchetta, Janeta Popovici-Muller, Robert Zahler, Sheldon Cao, Xiaolei Wang, Zhixiong Ye
  • Publication number: 20150148344
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
  • Publication number: 20150099015
    Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.
    Type: Application
    Filed: November 24, 2014
    Publication date: April 9, 2015
    Inventor: Guochuan Emil TSAI
  • Publication number: 20150099765
    Abstract: Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Michael L. Hendrickson, Jeffrey C. Ockuly, Trevor M. Twose, Melinda L. Verdone, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson
  • Patent number: 8999972
    Abstract: The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, and depression. This invention could also be used for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: April 7, 2015
    Assignee: Neuronascent, Inc.
    Inventor: Judith Kelleher-Andersson
  • Patent number: 8999975
    Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2 and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are inhibitors of Cathepsin C.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: April 7, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Marc Grundl, Thorsten Oost, Alexander Pautsch, Stefan Peters, Doris Riether, Wolfgang Wienen
  • Patent number: 8993592
    Abstract: Provided is a cyclic amine compound, represented by the following formula (I) that has superior acaricidal activity, has superior properties and safety, and which can be synthesized industrially advantageously, a salt thereof and an acaricide: (wherein, Cy1 and Cy2 respectively and independently represent, for example, an aryl group, R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b and R5a respectively and independently represent, for example, a hydrogen atom, R1a and R2a or R3a and R4a may together form, for example, an ethylene group, R10, R11, R20 and R21 respectively and independently represent, for example, an alkyl group, R10 or R11 may respectively or mutually, or together with an atom that bonds on Cy1, form a ring, R20 or R21 on Cy2 may respectively or mutually, or with an atom that bonds on Cy2, form a ring, m represents an integer of 0 to 5, n represents an integer of 0 to 5, p represents an integer of 0 to 5, and r represents an integer of 0 to 5).
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: March 31, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isami Hamamoto, Keiji Koizumi, Makio Yano, Masahiro Kawaguchi, Hazumi Nomura, Tetsuya Haruyama
  • Patent number: 8987249
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ralf Anderskewitz, Florian Binder, Matthias Grauert, Marc Grundl, Peter Wilhelm Haebel, Thorsten Oost, Alexander Pautsch, Stefan Peters, Viktor Vintonyak
  • Publication number: 20150079028
    Abstract: Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.
    Type: Application
    Filed: August 5, 2013
    Publication date: March 19, 2015
    Applicant: SUNSHINE LAKE PHARMA CO., LTD
    Inventors: Yingjun Zhang, Jaincun Zhang, Hongming Xie, Qingyun Ren, Yumei Tan, Huichao Luo
  • Patent number: 8980912
    Abstract: The present invention provides a cyclic amine compound represented by formula (I) (in formula (I), Cy1 and Cy2 independently represent a C6-10 aryl group or a heterocyclyl group; R1a to R5a independently represent a hydrogen atom or an unsubstituted or substituted C1-6 alkyl group; R10, R11, R20 and R21 independently represent an unsubstituted or substituted C1-6 alkyl group, an unsubstituted or substituted C1-6 alkoxy group, a halogen atom or the like; m, n, p, and r each represent an integer of 0 to 5; and Y represents an oxygen atom or the like) or salt thereof, and an acaricide including the same.
    Type: Grant
    Filed: February 24, 2011
    Date of Patent: March 17, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isami Hamamoto, Keiji Koizumi, Masahiro Kawaguchi, Hisashi Tanigawa, Takehiko Nakamura, Tomomi Kobayashi
  • Publication number: 20150072970
    Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.
    Type: Application
    Filed: May 19, 2014
    Publication date: March 12, 2015
    Applicant: MELINTA THERAPEUTICS, INC.
    Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
  • Publication number: 20150073014
    Abstract: The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.
    Type: Application
    Filed: July 16, 2014
    Publication date: March 12, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Sean M. Dalziel, Leticia M. Preza, Miroslav Rapta, Pierre-Jean Colson
  • Publication number: 20150065471
    Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventors: Carlos Puig Duran, Francesc Carrera Carrera, Juan Bautista PĂ©rez Garcia, Enrique Moyes Valles, Iolanda Marchueta Hereu