Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Morpholine Ring Patents (Class 514/237.5)
  • Patent number: 11905230
    Abstract: The present invention relates to a novel phenoxyacetic acid derivative represented by the general formula (I), preparation method thereof and use of a pharmaceutical composition containing the derivative in preparing a medicament for treating diabetes and metabolic syndrome. The phenoxyacetic acid derivatives have excellent in vivo hypoglycemic activity, which can be used for preventing or treating diabetes.
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: February 20, 2024
    Assignee: CHINA PHARMACEUTICAL UNIVERSITY
    Inventors: Hai Qian, Wenlong Huang, Chunxia Liu, Jianyong Yang
  • Patent number: 11779284
    Abstract: A basal metabolism estimation device includes: at least one memory configured to store instructions; and at least one processor configured to execute the instructions to: acquire first measurement data related to a left foot and second measurement data related to a right foot; identify a starting timing and an ending timing of a stance phase of each of the left and right feet based on the first and second measurement data; calculate a stride time for one cycle of movement of one of the feet during walking and a degree of asymmetry between the first measurement data in the stance phase of the left foot and the second measurement data in the stance phase of the right foot; and estimate basal metabolism based on the stride time and the degree of asymmetry.
    Type: Grant
    Filed: June 30, 2021
    Date of Patent: October 10, 2023
    Assignee: NEC CORPORATION
    Inventors: Chenhui Huang, Kenichiro Fukushi, Yusuke Sekiguchi, Haruki Yaguchi, Keita Honda, Shinichi Izumi, Dai Owaki
  • Patent number: 11420977
    Abstract: The present invention is directed to compositions, methods and kits for treatment of cancer, e.g. heptacellular carcinoma (HCC). In some embodiments, the present invention discloses the use of a small-molecule compounds of Formula (I)-(V) to inhibit tubulin methylation or to modulate chromatin or cytoskeleton modification in a cell.
    Type: Grant
    Filed: August 2, 2019
    Date of Patent: August 23, 2022
    Assignee: TRUSTEES OF BOSTON UNIVERSITY
    Inventors: Scott Edward Schaus, Ulla Hansen, Hang Gyeong Chin
  • Patent number: 11406642
    Abstract: A composition and method of treatment of neuromuscular, neuromuscular degenerative, neurodegenerative, autoimmune, developmental, traumatic, hearing loss related, and/or metabolic diseases, including spinal muscular atrophy (SMA) syndrome (SMA1, SMA2, SMA3, and SMA4, also called Type I, II, III and IV), traumatic brain injury (TBI), concussion, keratoconjunctivitis sicca (Dry Eye Disease), glaucoma, Sjogren's syndrome, rheumatoid arthritis, post-LASIK surgery, anti-depressants use, Wolfram Syndrome, and Wolcott-Rallison syndrome. The composition is selected from the group consisting of 2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP, bipartite 2,3-dinitrophenol, 2,4-dinitrophenol, 2,5-dinitrophenol, 2,6-dinitrophenol, 3,4-dinitrophenol, or 3,5-dinitrophenol (2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP) prodrugs; Gemini prodrugs, bioprecursor molecules, and combinations thereof. A dose of the composition for treatment of neurodegenerative diseases may be from about 0.
    Type: Grant
    Filed: November 26, 2019
    Date of Patent: August 9, 2022
    Assignees: MITOCHON PHARMACEUTICALS, INC., BIOVENTURES, LLC
    Inventors: John Gerard Geisler, Robert Alonso, Peter Anthony Crooks, Narsimha Reddy Penthala, Zaineb Albayati
  • Patent number: 11298312
    Abstract: The present invention relates to a topical composition and more particularly a topical composition for antimicrobial benefit. According to the present invention there is provided a topical composition comprising Niacinamide and picolinamide wherein the molar ratio of Niacinamide to picolinamide is from I:20 to 20:I.
    Type: Grant
    Filed: March 18, 2020
    Date of Patent: April 12, 2022
    Assignee: CONOPCO, INC.
    Inventors: Amitabha Majumdar, Mruthyunjaya Swamy Mathapathi
  • Patent number: 11135185
    Abstract: The invention provides a method for preventing and/or treating Alzheimer's disease in a subject in need of such treatment, comprising administrating to said subject an effective amount of a curcumin derivative, TML-6, and optionally a pharmaceutically acceptable carrier or excipient.
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: October 5, 2021
    Assignee: Merry Life Biomedical Company, Ltd.
    Inventors: Ih-Jen Su, Kuen-Jer Tsai, Hong-Yi Chang
  • Patent number: 11020392
    Abstract: This present invention discloses a new use of trimetazidine as a hepatoprotective drug in prevention and treatment of liver diseases, wherein trimetazidine is capable of inhibiting activation of resting T lymphocytes to activated lymphocytes, reducing release of cytokines, and reducing the hepatocyte injury caused by the immune system; capable of inhibiting fatty acid metabolism in hepatocytes and optimizing energy process in hepatocytes; and capable of maintaining normal function of mitochondrial permeability transition pores and reducing hepatocyte apoptosis. Clinical research and trial results suggest that, when administered to patients suffering from liver diseases and conditions, trimetazidine is capable of providing significant hepatoprotective function, and effectively decreasing transaminase levels (including alanine aminotransferase, aspartate transaminase, etc.), with such features as shortening the course of disease, reducing the mortality rate, easy and safe use, and low treatment cost.
    Type: Grant
    Filed: August 18, 2016
    Date of Patent: June 1, 2021
    Assignee: Martin Pharmaceuticals, Inc.
    Inventor: Zujiang Yu
  • Patent number: 10881702
    Abstract: The invention relates to a compound selected from among celastrol, the derivatives thereof and the pharmaceutically acceptable salts of celastrol and its derivatives, or a composition comprising such a compound for use in the topical prevention and/or treatment of a tumour or precancerous disease of the skin.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: January 5, 2021
    Assignee: PIERRE FABRE MEDICAMENT
    Inventors: Thien Nguyen, Arnaud Pillon
  • Patent number: 10702498
    Abstract: Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.
    Type: Grant
    Filed: June 30, 2016
    Date of Patent: July 7, 2020
    Assignees: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, FRIEDRICH-ALEXANDER-UNIVERSITAT ERLANGEN-NÜRNBERG, THE BOARD OF TRUSTEES OFTHE LELAND STANFORD JUNIOR UNIVERSITY, THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL
    Inventors: Brian K. Shoichet, Henry Lin, Peter Gmeiner, Aashish Manglik, Brian Kobilka, Bryan L. Roth, Daniela Gisela Dengler
  • Patent number: 10694745
    Abstract: A combination comprising a multi-site contact fungicide, a first systemic fungicide and optionally a second systemic fungicide and a method using the same.
    Type: Grant
    Filed: April 16, 2018
    Date of Patent: June 30, 2020
    Assignee: UPL LIMITED
    Inventors: Gilson Aparecido Hermenegildo de Oliveira, Jaidev Rajnikant Shroff, Vikram Rajnikant Shroff
  • Patent number: 10694744
    Abstract: A combination comprising a multi-site contact fungicide, a first systemic fungicide and optionally a second systemic fungicide and a method using the same.
    Type: Grant
    Filed: August 9, 2017
    Date of Patent: June 30, 2020
    Assignee: UPL LIMITED
    Inventors: Gilson Aparecido Hermenegildo de Oliveira, Jaidev Rajnikant Shroff, Vikram Rajnikant Shroff
  • Patent number: 10662199
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
    Type: Grant
    Filed: October 17, 2017
    Date of Patent: May 26, 2020
    Assignees: The Broad Institute, Inc., The General Hospital Corporation, Massachusetts Institute of Technology
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen J. Haggarty, Yan-Ling Zhang
  • Patent number: 10646446
    Abstract: The present invention relates to a pharmaceutical composition comprising a) a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, b) one or more, e.g. 1, 2 or 3, surfactants with lubricant properties; c) one or more, e.g. 1, 2 or 3, dry binders with disintegrant properties; d) one or more, e.g. 1, 2 or 3, fillers, and e) one or more, e.g. 1, 2 or 3, disintegrants.
    Type: Grant
    Filed: May 1, 2018
    Date of Patent: May 12, 2020
    Assignee: Novartis AG
    Inventors: Hong Wen, Natrajan Kumaraperumal, Richard Nause
  • Patent number: 10556900
    Abstract: The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I): which are tropomyos-in-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Grant
    Filed: April 4, 2016
    Date of Patent: February 11, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Yi Heng Chen, Ping Liu, Dongfang Meng, Jane Yang Wu, Chun Sing Li, Zhiqi Qi
  • Patent number: 10548900
    Abstract: A composition and method of treatment of neuromuscular, neuromuscular degenerative, neurodegenerative, autoimmune, developmental, traumatic, hearing loss related, and/or metabolic diseases, including spinal muscular atrophy (SMA) syndrome (SMA1, SMA2, SMA3, and SMA4, also called Type I, II, III and IV), traumatic brain injury (TBI), concussion, keratoconjunctivitis sicca (Dry Eye Disease), glaucoma, Sjogren's syndrome, rheumatoid arthritis, post-LASIK surgery, anti-depressants use, Wolfram Syndrome, and Wolcott-Rallison syndrome. The composition is selected from the group consisting of 2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP, bipartite 2,3-dinitrophenol, 2,4-dinitrophenol, 2,5-dinitrophenol, 2,6-dinitrophenol, 3,4-dinitrophenol, or 3,5-dinitrophenol (2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP) prodrugs; Gemini prodrugs, bioprecursor molecules, and combinations thereof. A dose of the composition for treatment of neurodegenerative diseases may be from about 0.
    Type: Grant
    Filed: March 7, 2017
    Date of Patent: February 4, 2020
    Assignees: MITOCHON PHARMACEUTICALS, INC., BIOVENTURES, LLC
    Inventors: John Gerard Geisler, Robert Alonso, Peter Anthony Crooks, Narsimha Reddy Penthala, Zaineb Albayati
  • Patent number: 10544185
    Abstract: Disclosed are deuterated chenodeoxycholic acid derivatives and pharmaceutical compositions containing the deuterated chenodeoxycholic acid derivatives. In particular, disclosed is a deuterated chenodeoxycholic acid derivative of formula (I), or a crystal form, pharmaceutically acceptable salt, hydrate or solvate thereof, and a pharmaceutical composition containing the same. The deuterated chenodeoxycholic acid derivatives of formula (I) can be used to treat and/or prevent diseases related to the farnesoid X receptor (FXR) and/or G-protein coupled bile acid receptor, such as nonalcoholic steatohepatitis, nonalcoholic fatty liver diseases, gallstones, primary biliary cirrhosis, and cirrhosis.
    Type: Grant
    Filed: February 16, 2016
    Date of Patent: January 28, 2020
    Assignee: Suzhou Zelgen Biopharmaceuticals Co., Ltd.
    Inventors: Binhua Lv, Zelin Sheng, Chengwei Li
  • Patent number: 10385009
    Abstract: An anthraquinone compound of formula I (such as the compounds of formulae II to X) and processes for making the same are provided. Pharmaceutical compositions for use in the treatment of cancer, optionally in combination with an agent capable of reducing the level of oxygenation of a tumor, are also provided. Additionally, an option for combination with chemotherapeutic and radiotherapeutic modalities to enhance overall tumor cell kill is provided. Methods for the detection of cellular hypoxia, both in vivo and in vitro, are additionally provided.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: August 20, 2019
    Assignee: BIOSTATUS LIMITED
    Inventors: Stefan Ogrodzinski, Paul Smith, Stephanie McKeown, Laurence Patterson, Rachel Jane Errington
  • Patent number: 10364267
    Abstract: The present invention provides compounds of Formula (I) or Formula (II): pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.
    Type: Grant
    Filed: February 22, 2017
    Date of Patent: July 30, 2019
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Guoqiang Wang, Yat Sun Or, Jiang Long, Guoyou Xu, Peng Dai, Ruichao Shen, Xuechao Xing, Jing He
  • Patent number: 10207989
    Abstract: Compounds according to Formula I are provided: and salts thereof, wherein Q1, Q2, R3, R4, X, and Y are as defined herein. Methods for preparing compounds of Formula I are also provided, as well as methods of treating cellular proliferative disorders, such as cancer, using compounds of Formula (I).
    Type: Grant
    Filed: September 18, 2013
    Date of Patent: February 19, 2019
    Assignee: TEMPLE UNIVERSITY—Of The Commonwealth System of Higher Education
    Inventors: M. V. Ramana Reddy, E. Premkumar Reddy
  • Patent number: 10189855
    Abstract: The present invention provides compounds of formula (I), wherein: R1 is unsubstituted C1-C6 alkyl; La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10 aryl; or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.
    Type: Grant
    Filed: August 22, 2017
    Date of Patent: January 29, 2019
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
  • Patent number: 9932294
    Abstract: The invention relates to the compounds of formula I and formula II 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 or formula II; and methods for treating or preventing multiple sclerosis may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of multiple sclerosis and psoriasis.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: April 3, 2018
    Assignee: CELLIX BIO PRIVATE LIMITED
    Inventor: Mahesh Kandula
  • Patent number: 9765054
    Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: September 19, 2017
    Assignee: CHDI Foundation, Inc.
    Inventors: Roland W. Bürli, Andrew J. Stott, Perla Breccia, Celia Dominguez, Ignacio Muñoz-Sanjuàn, Christopher A. Luckhurst, Samantha J. Hughes, Alan F. Haughan
  • Patent number: 9598354
    Abstract: Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.
    Type: Grant
    Filed: May 3, 2015
    Date of Patent: March 21, 2017
    Inventor: Mark Quang Nguyen
  • Patent number: 9593068
    Abstract: The present invention relates to novel compounds, e.g. for use as a medicament. In particular, the present invention relates to novel medicaments, preferably in the treatment and/or prevention of systemic diseases, autoimmune diseases, and/or inflammatory diseases, for example multiple sclerosis and psoriasis.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: March 14, 2017
    Assignee: ratiopharm GmbH
    Inventors: Wolfgang Albrecht, Roland Selig, Sebastian Rabe, Annemarie Maier, Richard Guserle
  • Patent number: 9452972
    Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: September 27, 2016
    Assignee: XenoPort, Inc.
    Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
  • Patent number: 9402819
    Abstract: The present invention relates to the technical field of chemically synthesized drugs, in particular to an anti-HIV drug or prodrug and preparation method and uses thereof. The compound or prodrug compound of the present invention has a structural formula as represented by formula I. The compounds have anti-HIV-1 and anti-HIV-2 virus activity, and have a C8166 therapeutic index as high as 2081.59 and an H9 therapeutic index as high as 303.03. Furthermore, the compounds have high solubility up to 1290-2845.5 ?g/ml in an aqueous solution, and can be formulated into an oral formulation.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: August 2, 2016
    Assignee: Sichuan University
    Inventors: Rui Li, Yuquan Wei
  • Patent number: 9388123
    Abstract: Provided is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: [in the formula, R1 to R5, A, and *1 to *3 are as defined in Description].
    Type: Grant
    Filed: November 28, 2013
    Date of Patent: July 12, 2016
    Assignee: Kyoto University
    Inventors: Takayoshi Suzuki, Yukihiro Itoh, Daisuke Ogasawara, Naoki Miyata, Tamio Mizukami, Ryuzo Sasaki, Akifumi Takaori, Masahiro Kawahara
  • Patent number: 9315481
    Abstract: Compounds, and methods and uses of compounds, and pharmaceutical compositions thereof, are described herein for treating leukemia. In particular, compounds, and methods and uses of compounds, and pharmaceutical compositions thereof, are described herein for treating acute lymphoblastic leukemia (ALL) in its various forms.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: April 19, 2016
    Assignee: Indiana University Research and Technology Corporation
    Inventors: Mark R. Kelley, Melissa L. Fishel, Angelo A. Cardoso
  • Patent number: 9295667
    Abstract: The present invention relates to a pharmaceutical composition for preventing or treating diabetes or fatty liver, and more specifically relates to a pharmaceutical composition for preventing or treating diabetes or fatty liver containing a CYP4A (cytochrome P450A) inhibitor as an active ingredient. According to the present invention, the CYP4A inhibitor suppresses endoplasmic reticulum stress, reduces the blood insulin concentration and suppresses apoptosis of liver cells, and hence exhibits effects in preventing or treating diabetes or fatty liver.
    Type: Grant
    Filed: February 11, 2014
    Date of Patent: March 29, 2016
    Assignee: Korea Basic Science Institute
    Inventors: Gun-Hwa Kim, Soohyun Kim, Jong-Soon Choi, Seung Il Kim, Edmond Changkyun Park
  • Patent number: 9282744
    Abstract: A synergistic fungicide composition, a formulation method and a use thereof are provided. The composition contains two active components A and B, where the active component A is benziothiazolinone, the active component B is one selected from dithianon, dimethomorph, iprodione and epoxiconazol, and the weight ratio of the two components is 1:50 to 50:1, and preferably 1:30 to 30:1. Test results show that, the fungicide composition has a significant synergistic effect, and more importantly, the application amount and the use-cost are reduced. The fungicide composition is effective in preventing and treating certain fungal diseases of crops such as food crops, vegetables and fruits.
    Type: Grant
    Filed: August 20, 2012
    Date of Patent: March 15, 2016
    Assignee: JIANGSU HUIFENG AGROCHEMICAL CO., LTD.
    Inventor: Hangen Zhong
  • Patent number: 9266817
    Abstract: Novel compounds, compositions, 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 a compound containing a catecholamine backbone and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods, compositions, and compounds for the treatment of disorders including neurological disorders, neuropsychiatric disorders, and metabolic disorders 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 administering to the subject a therapeutically effective amount of the described compounds. A further method of promoting neuroprotection in a subject also is provided, which includes administering to the subject a therapeutically effective amount of the described compounds.
    Type: Grant
    Filed: July 21, 2014
    Date of Patent: February 23, 2016
    Assignee: Emory University
    Inventor: Keqiang Ye
  • Patent number: 9265734
    Abstract: This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.
    Type: Grant
    Filed: September 3, 2009
    Date of Patent: February 23, 2016
    Assignee: BIOMARIN PHARMACEUTICAL INC.
    Inventors: James R. Rusche, Norton P. Peet, Allen T. Hopper
  • Publication number: 20150148347
    Abstract: A compound of formula I, wherein the groups R1, R2, R3, X, m, and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Application
    Filed: November 25, 2014
    Publication date: May 28, 2015
    Inventors: Iain LINGARD, Dieter HAMPRECHT
  • Publication number: 20150133297
    Abstract: The present invention relates to new antifungal compositions and their use in the treatment of agricultural products.
    Type: Application
    Filed: April 25, 2013
    Publication date: May 14, 2015
    Inventors: Jacobus Stark, Eva Louise Wilhelmine Sack
  • Publication number: 20150133430
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 14, 2015
    Inventors: Qing XU, Zhe LI
  • Publication number: 20150133405
    Abstract: The present invention relates to the use of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the prophylaxis, treatment and control of aquaporin-mediated conditions, e.g., diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord, e.g., following trauma or ischemic stroke, as well as the edema associated with glioma, meningitis, acute mountain sickness, epileptic seizures, infections, metabolic disorders, hypoxia, water intoxication, hepatic failure, hepatic encephalopathy, diabetic ketoacidosis, abscess, eclampsia, Creutzfeldt-Jakob disease, and lupus cerebritis, as well as edema consequent to microgravity and/or radiation exposure, as well as edema consequent to invasive central nervous system procedures, e.g.
    Type: Application
    Filed: May 8, 2013
    Publication date: May 14, 2015
    Inventors: Marc F. Pelletier, George William Farr, Paul Robert Mcguirk, Christopher H. Hall, Walter F. Boron
  • Patent number: 9006139
    Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.
    Type: Grant
    Filed: August 19, 2014
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
  • Patent number: 9000222
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Grant
    Filed: June 18, 2013
    Date of Patent: April 7, 2015
    Assignee: Androscience Corporation
    Inventors: Charles Shih, Qian Shi, Hui-Kang Wang
  • Publication number: 20150080217
    Abstract: The present invention relates to a method for preparing granules comprising the steps of A) preparing an adjuvanted slurry by milling an aqueous composition Al containing a pesticide and a silica absorbent to yield a pesticidal slurry, and adding an adjuvant to the pesticidal slurry; and B) granulating the adjuvanted slurry, wherein the granulation comprises a fluidized bed granulation or sprouted bed granulation.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 19, 2015
    Inventors: Torsten Knieriem, Klaus Kolb, Payam Michael Miraki Ardestani
  • Publication number: 20150072984
    Abstract: Chemical entities that are curcumin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 12, 2015
    Inventor: Xiangping Qian
  • Publication number: 20150051144
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as hyperlipidemia and also have a beneficial effect on cholesterol.
    Type: Application
    Filed: September 26, 2012
    Publication date: February 19, 2015
    Inventors: Harikishore Pingali, Vrajesh Pandya
  • Publication number: 20150038498
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: (I) or a pharmaceutically acceptable salt thereof, wherein Q is CH2, NR4, O, S, S(O) or S(O2), wherein R4 is H, C1-6 alkyl, aryl, or C3-8 cycloalkyl; R1 is a heterocycle or —(CR5R6)1-2NH2, wherein R5 and R6, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH; R2 is OH, NH2 or NHSO2CH3; and R3 is C1-6 alkyl.
    Type: Application
    Filed: March 22, 2013
    Publication date: February 5, 2015
    Inventors: Timothy Allen Blizzard, Tesfaye Biftu
  • Publication number: 20150038493
    Abstract: The present invention relates to a series of molecules derived from 2,3-diaminopropionic acid (DAP), comprising or not comprising an 8-hydroxyquinoline (8-HQ) motif, and to the use of said molecules for trapping an alpha-oxoaldehyde resulting particularly from the degradation of the glucose or for trapping an alpha-beta-unsaturated aldehyde, resulting particularly from the oxidative degradation of fatty acids. These molecules can have a further application in the fields of cosmetics, food processing, and pharmaceuticals.
    Type: Application
    Filed: October 5, 2012
    Publication date: February 5, 2015
    Inventors: Guy Potier, André Nobumichi Sasaki, Nicolas Audic
  • Publication number: 20150018355
    Abstract: Compounds, and methods and uses of compounds, and pharmaceutical compositions thereof, are described herein for treating leukemia. In particular, compounds, and methods and uses of compounds, and pharmaceutical compositions thereof, are described herein for treating acute lymphoblastic leukemia (ALL) in its various forms.
    Type: Application
    Filed: March 13, 2013
    Publication date: January 15, 2015
    Inventors: Mark R. Kelley, Melissa L. Fishel, Angelo A. Cardoso
  • Publication number: 20140357635
    Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.
    Type: Application
    Filed: August 19, 2014
    Publication date: December 4, 2014
    Inventors: Thomas SEITZ, Ulrike WACHENDORFF-NEUMANN, Peter DAHMEN
  • Patent number: 8895497
    Abstract: Cathepsin S inhibitors having formula (I), (II), (III) or (IV) as shown in the specification. These inhibitors can be used to treat cancer and autoimmune/inflammatory diseases.
    Type: Grant
    Filed: December 6, 2010
    Date of Patent: November 25, 2014
    Assignees: DCB-USA, LLC, National Tsing Hua University, National Health Research Institutes
    Inventors: Chun-Cheng Lin, Wun-Shaing Wayne Chang, Biing-Jiun Uang, Jang-Yang Chang, Jo-Chun Chen, Hsing-Pang Hsieh
  • Publication number: 20140329818
    Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.
    Type: Application
    Filed: June 6, 2014
    Publication date: November 6, 2014
    Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
  • Patent number: 8871762
    Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more carboxamide fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease. Group (A): a group consisting of thifluzamide, oxadixyl, pencycuron, benalaxyl-M, fenhexamid, furametpyr, isopyrazam, isotianil, mepronil, tecloftalam, boscalid, fluopyram, fluopicolide, carpropamid, diclocymet, mandipropamid, dimethomorph, flumorph, penthiopyrad, and bixafen.
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: October 28, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
  • Publication number: 20140301979
    Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 9, 2014
    Applicant: SIGA TECHNOLOGIES, INC.,
    Inventors: Sean M. AMBERG, Dongcheng DAI, Tove C. BOLKEN, Dennis E. HRUBY
  • Publication number: 20140303150
    Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
    Type: Application
    Filed: December 22, 2011
    Publication date: October 9, 2014
    Applicant: LEO Laboratories Limited
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian