Nitrogen Attached Directly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/161)
  • Patent number: 12139499
    Abstract: The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted benzothiazole compounds of Formula (I), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.
    Type: Grant
    Filed: June 25, 2019
    Date of Patent: November 12, 2024
    Assignee: PTC THERAPEUTICS, INC.
    Inventors: Nanjing Zhang, Suresh Babu, Scott J. Barraza, Anuradha Bhattacharyya, Guangming Chen, Gary Mitchell Karp, Andrew J. Kassick, Anthony R. Mazzotti, Young-Choon Moon, Jana Narasimhan, Nadiya Sydorenko, Anthony Turpoff, Matthew G. Woll, Wuming Yan
  • Patent number: 12060349
    Abstract: The invention relates to inhibitors of glucosylceramide synthase (GCS) of the Formula I: represented by the following structural formula or a pharmaceutically acceptable salt thereof, wherein the variables are as defined herein, useful for the treatment of metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, cystic disease and for the treatment of cancer.
    Type: Grant
    Filed: April 14, 2021
    Date of Patent: August 13, 2024
    Assignee: GENZYME CORPORATION
    Inventors: Elyse Bourque, Mario A. Cabrera-Salazar, Cassandra Celatka, Seng H. Cheng, Bradford Hirth, Andrew Good, Katherine Jancsics, John Marshall, Markus Metz, Ronald K. Scheule, Renato Skerlj, Yibin Xiang, Zhong Zhao, John Leonard, Thomas Natoli, Elina Makino, Herve Husson, Oxana Beskrovnaya
  • Patent number: 11970494
    Abstract: The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
    Type: Grant
    Filed: November 8, 2022
    Date of Patent: April 30, 2024
    Assignee: Ajax Therapeutics, Inc.
    Inventors: Craig E. Masse, Jeremy R. Greenwood, Jiayi Xu, Sayan Mondal, Phani Ghanakota
  • Patent number: 11637244
    Abstract: A compound represented by the following general formula is excellent in light emission properties. R1 and R2 each independently represent a fluorinated alkyl group, D represents a substituent in which Hammett's ?p value is negative, and A represents a substituent in which Hammett's ?p value is positive.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: April 25, 2023
    Assignees: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION, KYULUX, INC.
    Inventors: Yan Geng, Chihaya Adachi, Hajime Nakanotani, Naoto Notsuka, Keiro Nasu
  • Patent number: 11613702
    Abstract: A liquid crystal composition is provided containing a first liquid crystal compound represented by formula (1): and a second liquid crystal compound represented by formula (2): Also provided is a method for producing the liquid crystal composition having a desired wavelength dispersion characteristic.
    Type: Grant
    Filed: May 28, 2019
    Date of Patent: March 28, 2023
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Noriyuki Hida, Haruki Okawa
  • Patent number: 11447469
    Abstract: The present disclosure provides the compound having inhibitory property against TNIK having a specific chemical structure or its pharmaceutically acceptable salt. The present disclosure also provides a composition comprising the compound or its pharmaceutically acceptable salt. The present disclosure also provides a medical use of the compound, its salt or the composition comprising the compound or its pharmaceutically acceptable salt for treating or preventing cancer. The present disclosure also provides a method of treatment or prevention of cancer comprising administering the compound, its salt or the composition comprising the compound or its salt to a subject in need of such treatment or prevention.
    Type: Grant
    Filed: January 31, 2019
    Date of Patent: September 20, 2022
    Assignees: Korea Research Institute of Chemical Technology, Industry-Academic Cooperation Foundation, Yonsei University
    Inventors: Sung Youn Chang, Hyuk Lee, Ki Young Kim, Bum Tae Kim, Sung Soo Kim, Seong Hwan Kim, Hwan Jung Lim, Jung Nyoung Heo, Sang Joon Shin, Sang Youn Park
  • Patent number: 10829486
    Abstract: The present invention provides compounds of Formula (I): pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR. Specifically, the present invention relates to isoxazole derivatives useful as agonists for FXR, and methods for their preparation and use.
    Type: Grant
    Filed: February 11, 2019
    Date of Patent: November 10, 2020
    Assignee: Enanta Pharmacueticals, Inc.
    Inventors: Ruichao Shen, Jun Ma, Guoqiang Wang, Xuechao Xing, Yat Sun Or
  • Patent number: 10179774
    Abstract: Methods for preparing chirally purified substituted 4,5,6,7-tetrahydro-benzothiazole diamines such as, for example, (6R)2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole and purifying a dominant enantiomer of substituted 4,5,6,7-tetrahydro-benzothiazole diamines from entantiomerically enriched mixtures of substituted 4,5,6,7-tetrahydro-benzothiazole diamines are provided herein.
    Type: Grant
    Filed: December 5, 2016
    Date of Patent: January 15, 2019
    Assignee: Knopp Biosciences LLC
    Inventors: Prasad Raje, Rajendrakumar Reddy Gadikota, Jian-Xie Chen, Olga V. Lapina, John M. McCall
  • Patent number: 9540364
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: January 10, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James M. Apgar, Tesfaye Biftu, Ping Chen, Danqing Feng, Jacqueline D. Hicks, Ahmet Kekec, Kenneth J. Leavitt, Bing Li, Iyassu Sebhat, Xiaoxia Qian, Lan Wei, Robert R. Wilkening, Zhicai Wu
  • Patent number: 9334249
    Abstract: Compounds of Formula (I) wherein n, R1, R1A, R2, R4 and Z are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
    Type: Grant
    Filed: October 31, 2013
    Date of Patent: May 10, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Lee Fader, Mathieu Parisien, Carl Thibeault, Louis Morency, Martin Duplessis, Clint James, Sébastien Morin, James Gillard
  • Patent number: 9006229
    Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: April 14, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael L. Mitchell, Paul A. Roethle, Lianhong Xu, Hong Yang, Ryan McFadden, Kerim Babaoglu
  • Publication number: 20150051249
    Abstract: This disclosure features compounds and pharmaceutically acceptable salts thereof that inhibit MCL-1 and/or BFL-1/A1 and compositions containing the same. This disclosure also features combinations that include one or more of the MCL-1/BFL-1/A1 inhibitor compounds described herein, or a pharmaceutically acceptable salt thereof; and one or more additional therapeutic agents (e.g., one or more chemotherapeutic agents (including small molecule and/or anti-body based chemotherapy and/or radiation); e.g., one or more therapeutic agents that modulate apoptosis; e.g., one or more therapeutic agents that bind to and inhibit anti-apoptotic proteins or modulate them indirectly; e.g., one or more therapeutic agents that bind to and inhibit, or indirectly modulate, anti-apoptotic BCL-2, BCL-XL, BCL-w, MCL-1, and/or BFL-1/A1; e.g., one or more therapeutic agents that directly bind to and inhibit anti-apoptotic BCL-2/BCL-XL; e.g., agents such as ABT-199, ABT-263 and ABT-737; e.g.
    Type: Application
    Filed: March 14, 2013
    Publication date: February 19, 2015
    Inventor: Loren D. Walensky
  • Publication number: 20150045346
    Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Application
    Filed: June 27, 2012
    Publication date: February 12, 2015
    Applicants: MERCK SHARP & DOHME CORP., ALECTOS THERAPEUTICS INC.
    Inventors: Tong-Shuang Li, Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Harold G. Selnick
  • Patent number: 8940900
    Abstract: Compounds of the present disclosure are 2,2,2-tri-substituted acetamide derivatives of formula (I), its polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, useful as Glucokinase activator. Processes of their preparation are also described in the disclosure. The disclosure also describes method to characterize partial glucokinase activators.
    Type: Grant
    Filed: February 25, 2008
    Date of Patent: January 27, 2015
    Assignee: Advinus Therapeutics Private Limited
    Inventors: Kasim A. Mookhtiar, Debnath Bhuniya, Bhavesh Dave, Gobind S. Kapkoti, Sujay Basu, Anita Chugh, Siddhartha De, Venkata P. Palle
  • Patent number: 8883833
    Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: November 11, 2014
    Assignee: Decode Genetics EHF
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Munagala Rao
  • Publication number: 20140330011
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 6, 2014
    Publication date: November 6, 2014
    Applicant: CYTOKINETICS, INC
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Patent number: 8865752
    Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.
    Type: Grant
    Filed: July 4, 2013
    Date of Patent: October 21, 2014
    Assignee: Angion Biomedica Corp.
    Inventors: Bijoy Panicker, Dong Sung Lim, Rama K. Mishra, Lambertus J. W. M. Oehlen, James G. Tarrant, Xiaokang Zhu, Dawoon Jung
  • Patent number: 8835428
    Abstract: The present invention relates to isoxazole, thiazole and oxidiazole derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, in particular to the use of these compounds in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1.
    Type: Grant
    Filed: February 24, 2011
    Date of Patent: September 16, 2014
    Assignee: Piramal Enterprises Limited
    Inventors: Ashok Kumar Gangopadhyay, Kishorkumar Shivajirao Kadam, Ravindra Dnyandev Jadhav, Hitesh Mistry, Rajiv Sharma
  • Publication number: 20140235857
    Abstract: The present invention pertains to a compound represented by a formula (I) and a method for producing thereof (in the formula, Ax is an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, Ay is a hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a cycloalkyl group, an alkenyl group having 2 to 18 carbon atoms, an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, or the like. Ax and Ay optionally bond to each other to form a ring, and Q is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like.).
    Type: Application
    Filed: April 27, 2012
    Publication date: August 21, 2014
    Applicant: ZEON CORPORATION
    Inventors: Kei Sakamoto, Kumi Okuyama, Yasushi Nakano
  • Publication number: 20140227320
    Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 14, 2014
    Inventors: Shawn P. Iadonato, Kristin Bedard, Myra Wang Imanaka, Kerry W. Fowler
  • Publication number: 20140206665
    Abstract: The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.
    Type: Application
    Filed: August 10, 2012
    Publication date: July 24, 2014
    Applicants: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Harold G. Selnick, Kun Liu, Ernest J. McEachern, Yuanxi Zhou, Yongbao Zhu
  • Patent number: 8766001
    Abstract: The present invention relates to the improvement in organic electroluminescent devices by using compounds of the formula (1), in particular as hole-injection or hole-transport materials in a hole-injection or hole-transport layer.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: July 1, 2014
    Assignee: Merck Patent GmbH
    Inventors: Christof Pflumm, Arne Buesing, Amir Hossain Parham, Rocco Fortte, Holger Heil, Philipp Stoessel
  • Patent number: 8759380
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: June 24, 2014
    Assignee: Cytokinetics, Inc.
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Publication number: 20140142266
    Abstract: The present invention relates to a polymerizable compound represented by a formula (I). The present invention provides a polymerizable compound, a polymerizable composition, a polymer, and an optically anisotropic article that are capable of obtaining an optical film having a low melting point, having excellent solubility, capable of being manufactured at low cost, and capable of uniform polarized light conversion across a broad wavelength region. [In formula: Y1 to Y6 are independently a chemical single bond, —O—, —O—C(?O)—, —C(?O)—O— etc.; G1 and G2 are independently a divalent C1-C20 aliphatic group etc.; Z1 and Z2 are independently C2-C10 alkenyl group that is substituted with a halogen atom etc.; Ax is a C2-C30 organic group that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring; Ay is a hydrogen atom, a C1-C20 alkyl group, a C2-C20 alkenyl group, a C3-C12 cycloalkyl group etc.; A1 is a trivalent aromatic group etc.
    Type: Application
    Filed: April 27, 2012
    Publication date: May 22, 2014
    Applicant: ZEON CORPORATION
    Inventors: Kei Sakamoto, Kumi Okuyama
  • Publication number: 20140113884
    Abstract: Compounds and compositions comprising epoxyeicosatrienoic acid (EET) analogs that act as EET agonists and are useful as medications in the treatment of drug-induced nephrotoxicity, hypertension and other related conditions. Methods of making and using the compounds and compositions are further described.
    Type: Application
    Filed: April 4, 2012
    Publication date: April 24, 2014
    Inventors: John David Imig, William B. Campell, John Russell Falck
  • Patent number: 8703962
    Abstract: The invention relates to compounds of formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof.
    Type: Grant
    Filed: October 22, 2009
    Date of Patent: April 22, 2014
    Assignee: Purdue Pharma L.P.
    Inventors: Donald J. Kyle, Laykea Tafesse
  • Publication number: 20140107247
    Abstract: The invention provides a polymerizable compound represented by formula (I), a polymerizable composition, and a polymer that have a practical low melting point, can be produced at low cost, and can produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, and an optically anisotropic article.
    Type: Application
    Filed: April 12, 2012
    Publication date: April 17, 2014
    Applicant: ZEON CORPORATION
    Inventors: Kei Sakamoto, Kumi Okuyama
  • Patent number: 8697911
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: April 15, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
  • Publication number: 20140045818
    Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I.
    Type: Application
    Filed: April 20, 2012
    Publication date: February 13, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Michael L. Mitchell, Paul A. Roethle, Lianhong Xu, Hong Yang, Ryan McFadden, Kerim Babaoglu
  • Publication number: 20140018401
    Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.
    Type: Application
    Filed: July 4, 2013
    Publication date: January 16, 2014
    Applicant: ANGION BIOMEDICA CORP
    Inventors: Bijoy Panicker, Dong Sung Lim, Rama K. Mishra, Lambertus J.W.M. Oehlen, James G. Tarrant, Xiaokang Zhu, Dawoon Jung
  • Patent number: 8614213
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: December 24, 2013
    Assignee: Novartis AG
    Inventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
  • Publication number: 20130324537
    Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.
    Type: Application
    Filed: November 21, 2012
    Publication date: December 5, 2013
    Applicants: Abbott Laboratories, Abbott GmbH & Co. KG
    Inventors: Abbott GmbH & Co. KG, Abbott Laboratories, Andrea Hager-Wernet
  • Patent number: 8592424
    Abstract: A method of treating a disease state or condition in humans via topical brainstem afferent stimulation therapy via the administration of a drug to the back of the neck of a human patient at the hairline in close proximity to and under or on the area of skin above the brain stem to provide regional neuro-affective therapy is disclosed.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: November 26, 2013
    Assignee: Afgin Pharma LLC
    Inventor: Ronald Aung-Din
  • Patent number: 8519148
    Abstract: Methods for preparing chirally purified substituted 4,5,6,7-tetrahydro-benzothiazole diamines such as, for example, (6R)2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole and purifying a dominant enantiomer of substituted 4,5,6,7-tetrahydro-benzothiazole diamines from entantiomerically enriched mixtures of substituted 4,5,6,7-tetrahydro-benzothiazole diamines are provided herein.
    Type: Grant
    Filed: March 14, 2008
    Date of Patent: August 27, 2013
    Assignee: Knopp Neurosciences, Inc.
    Inventors: Prasad Raje, Rajendrakumar Reddy Gadikota, Jian-Xie Chen, Olga V. Lapina, John M. McCall
  • Patent number: 8481547
    Abstract: The present invention is directed to substituted benzothiazole and benzoxazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: July 9, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Alfonzo D. Jordan, Renee L. DesJarlais, Dennis J. Hlasta, Michael H. Parker, Carsten Schubert, Kimberly White
  • Publication number: 20130131044
    Abstract: The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Application
    Filed: May 10, 2011
    Publication date: May 23, 2013
    Inventors: Tong-Shuang Li, Ernest J. Mceachern, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu
  • Patent number: 8440705
    Abstract: Compounds and compositions are provided for treatment or amelioration of one or more symptoms of ?-synuclein toxicity, ?-synuclein mediated diseases or diseases in which ?-synuclein fibrils are a symptom or cause of the disease. In one embodiment, the compounds for use in the compositions and methods are heteroaryl acylguanidines, heteroarylhydrazones, dihydropyridones, heteroaryl and aryl styryl ketones, and heteroarylpyrazoles.
    Type: Grant
    Filed: September 16, 2005
    Date of Patent: May 14, 2013
    Assignees: Whitehead Institute for Biomedical Research, FoldRx Pharmaceuticals, Inc.
    Inventors: Susan L. Lindquist, Tiago Outeiro, Richard Labaudinière
  • Publication number: 20130060025
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 12, 2012
    Publication date: March 7, 2013
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Patent number: 8362032
    Abstract: Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists:
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: January 29, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Aarti Sameer Kawatkar, Tara Whitney, Timothy D. Neubert, Nicole Hilgraf, Andreas P. Termin, Esther Martinborough
  • Patent number: 8349880
    Abstract: The present disclosure provides a series of compounds of the formula (I) which reduce ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Grant
    Filed: January 7, 2010
    Date of Patent: January 8, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lawrence R. Marcin, Lorin A. Thompson, III, Kenneth M. Boy, Jason M. Guernon, Mendi A. Higgins, Jianliang Shi, Yong-Jin Wu, Yunhui Zhang, John E. Macor
  • Patent number: 8318781
    Abstract: Disclosed is a novel aralkyl carboxylic acid compound which has an agonistic activity on GPR-120 and/or GPR-40, particularly GPR-120, and is therefore useful as an appetite regulator, an anti-obesity agent, a therapeutic agent for diabetes, a pancreatic beta differentiating cell growth enhancer, a therapeutic agent for metabolic syndrome, a therapeutic agent for a gastrointestinal disease, a therapeutic agent for a neuropathy, a therapeutic agent for a mental disorder, a therapeutic agent for a pulmonary disease, a therapeutic agent for a pituitary hormone secretion disorder or a lipid flavoring/seasoning agent. The aralkyl carboxylic acid compound is represented by the general formula (I).
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: November 27, 2012
    Assignees: Japan Science and Technology Agency, Kyoto University, Nagoya City University
    Inventors: Gozoh Tsujimoto, Akira Hirasawa, Naoki Miyata, Takayoshi Suzuki, Yoshiyuki Takahara, Masaji Ishiguro, Mie Hata
  • Publication number: 20120289522
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: October 1, 2010
    Publication date: November 15, 2012
    Inventors: Thomas J. Seiders, Lucy Zhao, Jeannie Arruda, Bowei Wang, Brian Andrew Stearns, Yen Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Ryan Clark, Heather Renee Coate, Nicholas Simon Stock, Deborah Volkots
  • Publication number: 20120289698
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 13, 2012
    Publication date: November 15, 2012
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Publication number: 20120282629
    Abstract: The present invention relates to compounds suitable for modulating huntingtin protein processing and useful for treating or preventing huntingtin-related disorders. The invention provides pharmaceutical compositions comprising said compounds and methods of syntheses thereof.
    Type: Application
    Filed: August 19, 2010
    Publication date: November 8, 2012
    Applicant: MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZIN
    Inventors: Erich Wanker, Thomas Wiglenda, Julius Tachu Babila, Annett Boddrich, Michael Schmidt, Sandra Neuendorf, Franziska Schiele
  • Publication number: 20120277441
    Abstract: A process for preparing a compound of formula (I) or a salt or solvate thereof, by reacting a compound of formula (IV): with a compound of formula (V): to obtain the compound of formula (I): wherein each R1 is independently a halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy or C1-C6 alkylcarbonyl; R2 is C1-C6 alkyl, C1-C6 haloalkyl, or phenyl optionally substituted with at least one selected from the group consisting of a halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy, and nitro; R3 is C1-C6 alkyl, C3-C8 cycloalkyl, or a phenyl optionally substituted at least one selected from the group consisting of a halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, and C1-C6 haloalkoxy; n is 0, 1, or 2; and X is S atom or O atom.
    Type: Application
    Filed: November 24, 2010
    Publication date: November 1, 2012
    Applicant: Shionogi & Co. Ltd.
    Inventors: Ryosuke Kunitani, Kenji Takaya, Yoshiaki Imamura, Aiko Hasegawa
  • Patent number: 8299265
    Abstract: This invention provides an anorectic or anti-obesity composition comprising a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted lower alkyl, Y is —S(O)n— wherein n is 1 or 2, or —CO—, R2 is hydrogen or lower alkyl, R7 is hydrogen or lower alkyl, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, and Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like.
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: October 30, 2012
    Assignee: Shionogi & Co., Ltd.
    Inventors: Takayuki Okuno, Masahiro Sakagami
  • Patent number: 8226854
    Abstract: A photoelectric conversion device is provided and includes a photoelectric conversion layer containing a compound represented by the following formula (1). Formula (1): In the formula, Z1 represents an atomic group for forming a 5- or 6-membered nitrogen-containing heterocyclic ring; Za represents an atomic group for forming a 5- or 6-membered ring; R1 represents a hydrogen atom, an alkyl group, an alkenyl group, an aryl group or a heterocyclic group; L11 to L14 each represents a methine group which may have a substituent or may form a ring with another methine group; p1 represents 0 or 1; n1 represents an integer of 0 to 4 and when n1 is an integer of 2 or more, each L13 or L14 may be the same as or different from every other L13 or L14; M1 represents an ion for neutralizing the electric charge; and m1 represents a number necessary for neutralization of the electric charge; provided that a compound where Z1 is an atomic group forming a thiazoline nucleus or a thiazole nucleus is excluded.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: July 24, 2012
    Assignee: FUJIFILM Corporation
    Inventors: Rui Shen, Kimiatsu Nomura, Hideyuki Suzuki
  • Publication number: 20120184518
    Abstract: Methods for the treatment and/or prevention of an inflammatory disease or disorder through administration of an inhibitor of a glutaminyl peptide cyclotransferase. Inflammatory diseases or disorders treated or prevented by methods disclosed herein include mild cognitive impairment (MCI), rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis, sepsis and peritonitus. Further provided are respective diagnostic methods, assays and kits.
    Type: Application
    Filed: January 20, 2012
    Publication date: July 19, 2012
    Applicant: PROBIODRUG AG
    Inventors: Stephan Schilling, Holger Cynis, Torsten Hoffman, Hans-Ulrich Demuth
  • Patent number: 8207220
    Abstract: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: June 26, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Patent number: 8202887
    Abstract: The present invention relates to 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broad-spectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: June 19, 2012
    Assignee: Janssen R&D Ireland
    Inventors: Herman De Kock, Tim Hugo Maria Jonckers, Paul Jozef Gabriel Maria Boonants, Stefaan Julien Last, Inge Dierynck, Judith Eva Baumeister, Gerben Albert Van 'T Klooster