C=x Bonded Directly To The Nitrogen Which Is Bonded Directly To The Thiazole Ring (x Is Chalcogen) Patents (Class 514/371)
  • Patent number: 10836706
    Abstract: Disclosed herein are compounds of formula I: and salts thereof. Also disclosed are compositions comprising compounds of formula I and methods using compounds of formula I.
    Type: Grant
    Filed: February 23, 2017
    Date of Patent: November 17, 2020
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Ajit Parhi, Gifty A. Blankson, Liping Wang, Xiao Chen, Yongzheng Zhang, Malvika Kaul, Daniel S. Pilch
  • Patent number: 10765664
    Abstract: Disclosed herein are methods for treating or preventing a disease comprising administering a pharmaceutical composition comprising a therapeutically-effective amount of nitazoxanide to a subject having the disease, wherein the disease is causally linked to infection by one or more pathogens selected from the group consisting of members of the genus Ebolavirus, members of the genus Marburgvirus, members of the species dengue virus, human immunodeficiency viruses 1 and 2, and members of the species Mycobacterium tuberculosis.
    Type: Grant
    Filed: April 23, 2019
    Date of Patent: September 8, 2020
    Assignee: Children's Medical Center Corporation
    Inventors: Anne Goldfeld, Luke Jasenosky, Viraga Haridas, Shahin Ranjbar
  • Patent number: 10653678
    Abstract: The present invention relates to synergistic combination of active ingredients for use in the treatment of fibrotic diseases.
    Type: Grant
    Filed: April 20, 2018
    Date of Patent: May 19, 2020
    Assignee: GENFIT
    Inventors: Robert Walczak, Corinne Foucart, Philippe Delataille
  • Patent number: 10464885
    Abstract: The present invention relates to a compound and its preparation method and use and corresponding targeted drug delivery systems and chemotherapeutic drugs. The compound is a novel compound or a pharmaceutically acceptable salt thereof for treating small cell lung cancer, characterized in that, the compound has the general formula I, wherein R is acyloxy group. The present invention also relates to a preparation method of the compound, to use of the compound for the preparation of a chemotherapeutic drug for treating small cell lung cancer, to a targeted drug delivery system including the compound, and to a chemotherapeutic drug including the compound and for treating small cell lung cancer.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: November 5, 2019
    Assignee: BEIJING XINDE RUNXING TECHNOLOGY CO., LTD.
    Inventors: Xuechun Lu, Xiaohua Chi, Chengcheng Tang, Lei Shi
  • Patent number: 10245252
    Abstract: Use of alkylamidothiazoles in cosmetic or dermatological preparations for the prophylaxis and treatment of sensitive skin, itching, dry skin, and of inflammatory states of the human skin.
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: April 2, 2019
    Assignee: BEIERSDORF AG
    Inventors: Ludger Kolbe, Cathrin Scherner, Ursula Wennsorra, Tobias Mann
  • Patent number: 10201530
    Abstract: Provided herein are methods of treating cancer in a subject by administering COH29 ((N-(4-(3,4-dihydroxyphenyl)-5-phenylthiazol-2-yl)-3,4-dihydroxybenzamide)). The methods of treating include treating a BRCA1-defective subject, a PARP1 inhibitor-resistant subject or a DNA-damaging anti-cancer agent resistant subject. The methods include treating cancer by administering COH29 and a DNA-damaging anti-cancer agent in a combined synergistic amount.
    Type: Grant
    Filed: February 20, 2018
    Date of Patent: February 12, 2019
    Assignee: City of Hope
    Inventor: Yun Yen
  • Patent number: 10005720
    Abstract: The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
    Type: Grant
    Filed: April 4, 2014
    Date of Patent: June 26, 2018
    Assignees: North Carolina Central University, The University of North Carolina at Chapel Hill
    Inventors: Jonathan Z. Sexton, Jay E. Brenman, David L. Musso
  • Patent number: 9931322
    Abstract: Provided herein are methods of treating cancer in a subject, by administering COH29 ((N-(4-(3,4-dihydroxyphenyl)-5-phenylthiazol-2-yl)-3,4-dihydroxybenzamide)). The methods of treating include treating a BRCA1-defective subject, a PARP1 inhibitor-resistant subject or a DNA-damaging anti-cancer agent resistant subject. The methods include treating cancer by administering COH29 and a DNA-damaging anti-cancer agent in a combined synergistic amount.
    Type: Grant
    Filed: August 19, 2016
    Date of Patent: April 3, 2018
    Assignee: City of Hope
    Inventor: Yun Yen
  • Patent number: 9796692
    Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: October 24, 2017
    Assignee: CITY OF HOPE
    Inventors: David Horne, Christopher Lincoln
  • Patent number: 9316633
    Abstract: Provided herein are methods for identifying and characterizing agents that alter the volume of a cell. Methods are provided for rapid screening and identification of an agent that alters the capability of a small, neutrally charged solute transporter to transport the solute across a cell membrane. The methods described herein may be used to identify and characterize inhibitors of urea transporters, to identify and characterize inhibitors of aquaporins, and to identify and characterize inhibitors of other small, neutrally charged solutes such as glucose.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: April 19, 2016
    Assignee: The Regents of the University of California
    Inventors: Alan S. Verkman, Marc Harris Levin
  • Patent number: 9149527
    Abstract: Provided herein are substituted furanyl compounds, pharmaceutical compositions comprising the compounds, methods of their preparation, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or amelioration of various disorders, including cancer and proliferative disorders. In one embodiment, the compounds provided herein modulate eIF4E activity. In one embodiment, the compounds provided herein modulate the Hedgehog pathway activity. In one embodiment, the compounds provided herein are used in combination with surgery, radiation therapy, immuno therapy and/or one or more additional anticancer drugs for the treatment, prevention, and/or amelioration of cancer and proliferative disorders.
    Type: Grant
    Filed: April 10, 2014
    Date of Patent: October 6, 2015
    Assignee: NovoMedix, LLC
    Inventors: Leah M. Fung, Kyle W. H. Chan, Cathy A. Swindlehurst
  • Patent number: 9107913
    Abstract: The present disclosure relates to methods for treating viral hepatitis, compounds useful in the treatment of viral hepatitis, and pharmaceutical compositions comprising such compounds. In one embodiment, pharmaceutical compositions comprising nitazoxanide, tizoxanide, or derivatives and/or mixtures thereof are provided, as well as methods of treating hepatitis C using such compositions.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: August 18, 2015
    Assignee: ROMARK LABORATORIES, L.C.
    Inventor: Jean-Francois Rossignol
  • Patent number: 9102637
    Abstract: The present invention relates to novel bicyclic thiazole compounds that inhibit Traf2- and Nck-interacting kinase (TNIK), and as such are useful as TNIK inhibitors administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. The bicyclic thiazole compounds are showed by a next formula (I). (wherein R1, R2, R3 and Q are as defined in the specification), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: August 11, 2015
    Assignees: CARNA BIOSCIENCES, INC., NATIONAL CANCER CENTER
    Inventors: Masaaki Sawa, Hideki Moriyama, Tesshi Yamada, Miki Shitashige, Yusuke Kawase, Yuko Uno
  • Publication number: 20150148385
    Abstract: The present inventor has found out that the following criteria enable to ensure an effect for increasing the platelet count while preventing an excessive increase in the platelet count; “when the platelet count has increased by a certain amount and reached to a sufficient level of the platelet count during administration of a pharmaceutical composition containing a compound having a thrombopoietin receptor agonistic activity, administration of the pharmaceutical composition is discontinued thereafter”.
    Type: Application
    Filed: June 28, 2013
    Publication date: May 28, 2015
    Inventors: Takeshi Kano, Takahiro Fukuhara, Takayuki Katsube
  • Publication number: 20150141475
    Abstract: A therapeutic agent for impaired gastric accommodation which contains as an active ingredient a compound represented by the general formula (1): (wherein R1 represents a hydrogen atom, a hydroxyl group or a halogen atom; A represents a furyl group, a thienyl group, a thiazolyl group or an oxazolyl group; R2 and R3 each represents an alkyl group with 1 to 5 carbon atoms; and n represents an integer of 2 to 4), or an acid addition salt thereof. Use of a therapeutic agent of the present invention greatly alleviates symptoms caused by said disorders, such as early satiety and bloating, because it improves relaxation of gastric fundus and impaired gastric accommodation.
    Type: Application
    Filed: December 22, 2014
    Publication date: May 21, 2015
    Applicant: ZERIA PHARMACEUTICAL CO., LTD.
    Inventors: Yugo MATSUNAGA, Shigeru Ueki, Hiroki Kato, Shiro Kobayashi
  • Publication number: 20150133366
    Abstract: C. difficile infection (CDI) is the most common cause of antibiotic-associated diarrhea. Unfortunately, antibiotic therapy remains as the standard treatment for this antibiotic-induced disease and relapses are common. Antibiotic treatment typically is given for 10 to 14 days for initial or second episode of CDI. For recurrent episodes, more prolonged courses are recommended. It is disclosed herein that lower dose or shorter course of the antimicrobial treatment is sufficient to treat the disease and prevent recurrent disease by enabling a good immunologic response to infection, and perhaps also by better preserving normal flora, thus protecting against relapses or reinfection.
    Type: Application
    Filed: November 12, 2014
    Publication date: May 14, 2015
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Richard L. Guerrant, Cirle Alcantara Warren, John Hudson Moore, II, Edward van Opstal
  • Publication number: 20150126507
    Abstract: The invention is directed, in part, to compounds of structure (I) to treat or prevent hearing loss. Compounds of the present invention also promote sensory hair cell regeneration. Particular compositions comprise compounds of structure (I), and optionally one or more small molecules that increase the proliferation of supporting cells.
    Type: Application
    Filed: September 5, 2014
    Publication date: May 7, 2015
    Inventors: Robert Scott Thies, Zhiyong Wang, Bonnie Jacques, Chin-Chun Jean Lu
  • Publication number: 20150126534
    Abstract: Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.
    Type: Application
    Filed: October 7, 2014
    Publication date: May 7, 2015
    Inventors: Alan Hornsby Davidson, Alan Hastings Drummond, Lindsey Ann Needham
  • Publication number: 20150126527
    Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 7, 2015
    Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Young-Jun Shin, Pureza Vallar, Ning Zou
  • Publication number: 20150126566
    Abstract: The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 7, 2015
    Inventors: Sara Hadida-Ruah, Fredrick Van Goor, Mark Miller, Jason McCartney, Jinglan Zhou, Vijayalaksmi Arumugam
  • Publication number: 20150111868
    Abstract: The present invention is concerned with novel 1,3-dihydro-2H-benzimidazol-2-one derivatives substituted with heterocycles having formula (I) stereoisomeric forms thereof, and the pharmaceutically acceptable addition salts, and the solvates thereof, wherein R4, R5, Z and Het have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.
    Type: Application
    Filed: June 14, 2013
    Publication date: April 23, 2015
    Applicant: Jansen R&D Ireland
    Inventors: Abdellah Tahri, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Sandrine Marie Helene Vendeville, Lili Hu, Samuel Dominique Demin, Ludwig Paul Cooymans
  • Publication number: 20150105433
    Abstract: Provided herein are methods for preventing or treating a viral infection in a subject, wherein the viral infection is mediated by a virus comprising one or more viral RNA molecules translated by a ribosomal shunting mechanism or a non-IRES mediated mechanism. The methods comprise administering to a subject an agent that reduces ribosomal protein (Rps25) expression or function. Also provided are methods of inhibiting or promoting ribosomal shunting-mediated translation or non-IRES mediated translation. Also provided are methods of screening for an agent that inhibits or promotes ribosomal shunting-mediated translation or non-IRES mediated translation.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 16, 2015
    Inventor: Sunnie R. Thompson
  • Publication number: 20150105441
    Abstract: Disclosed herein are methods of treating a patient at risk of developing or having a neurofibromatosis or a sporadic schwannoma. In exemplary embodiments, the method involves administering to a subject in need an effective amount of a LIMK modulating agent. Also disclosed are compounds newly identified to be inhibitors of Merlin-null Schwann cell proliferation and/or survival.
    Type: Application
    Filed: March 13, 2013
    Publication date: April 16, 2015
    Inventor: Cristina Fernandez-Valle
  • Publication number: 20150094307
    Abstract: Amino, amido, and heterocyclic compounds are disclosed. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia/reperfusion injury, cardiovascular disease and other diseases related to RAGE activity.
    Type: Application
    Filed: October 1, 2014
    Publication date: April 2, 2015
    Inventors: Ann Marie Schmidt, Ravichandran Ramasamy, Alexander Shekhtman, Vivek Rai, Michaele B. Manigrasso
  • Patent number: 8993567
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: March 31, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
  • Patent number: 8980892
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: March 17, 2015
    Assignees: Syngenta Crop Protection LLC, Syngenta Limited
    Inventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
  • Publication number: 20150064262
    Abstract: Disclosed is a pharmaceutical nitazoxanide composition comprising: (a) an immediate release fraction comprising nitazoxanide non-coated granules or non-granulated powder, and (b) a pH-dependent release fraction comprising granules of nitazoxanide coated with one or more polymers having a pH-dependent solubility.
    Type: Application
    Filed: January 27, 2012
    Publication date: March 5, 2015
    Applicant: SIEGFRIED RHEIN S.A. DE C.V.
    Inventor: Esteban Alejandro Fiore
  • Publication number: 20150057281
    Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Especially preferred compounds disrupt Nek2/Hec1 binding and are therefore useful as chemotherapeutic agent for neoplastic diseases.
    Type: Application
    Filed: October 29, 2014
    Publication date: February 26, 2015
    Inventors: Johnson LAU, Jiann-Jyh HUANG
  • Publication number: 20150057272
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: August 1, 2014
    Publication date: February 26, 2015
    Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • Publication number: 20150051177
    Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Inventor: Darren Orton
  • Publication number: 20150051193
    Abstract: Compounds and methods are provided for the treatment of pathogen infections. In some embodiments, the anti-infective compounds have broad spectrum activity against a variety of infective diseases, where the diseases are caused by pathogens containing a basic amino acid PIP-2 pincer (BAAPP) domain that interacts with phosphatidylinositol 4,5-bisphosphate (PIP-2) to mediate pathogen replication. Also provided are methods of inhibiting a PI4-kinase and methods of inhibiting viral infection. In some embodiments, the compound is a PI4-kinase inhibiting compound that is a 5-aryl-thiazole. The subject compounds may be formulated or provided to a subject in combination with a second anti-infective agent, e.g. interferon, ribivarin, and the like.
    Type: Application
    Filed: October 5, 2012
    Publication date: February 19, 2015
    Inventors: Jeffrey S. Glenn, Michael A. Gelman, Brandon Tavshanjian, Kevan Shokat, Ingrid Choong
  • Publication number: 20150038483
    Abstract: The present invention is related to a compound represented by formula (I) wherein R1 is a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted aromatic carbocyclyl, or the like; X is —N(R3)—, —O—, or —S—; Y is ?C(R4)—, or ?N—; Z is —N(R7)—, —O—, or —S—; R2 is substituted or unsubstituted alkyloxy, or the like, or a group represented by the following formula: —(CR2aR2b)n—R2c, wherein R2a is each independently a hydrogen atom, halogen, or the like; R2b is each independently a hydrogen atom, halogen, or the like; R2a and R2b which are attached to the same carbon atom may be taken together to form oxo, a substituted or unsubstituted non-aromatic carbocycle, or the like; two of R2a which are attached to the adjacent carbon atoms and/or two of R2b which are attached to the adjacent carbon atoms may be taken together to form a bond; R2c is substituted or unsubstituted aromatic carbocyclyl, or the like; n is an integer from 1 to 3; R3 and R7 are each independently a hydrogen atom, sub
    Type: Application
    Filed: March 26, 2013
    Publication date: February 5, 2015
    Inventors: Akira Yukimasa, Naotake Kobayashi, Kenji Takaya, Yoshio Hato
  • Publication number: 20150038523
    Abstract: The invention relates to compounds of formula (I): wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-integrin antagonists to target cells expressing alpha-V-beta-3.
    Type: Application
    Filed: January 22, 2013
    Publication date: February 5, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Robert Alan Goodnow, Jr., Matthew Michael Hamilton, Agnieszka Kowalczyk, Achyutharao Sidduri
  • Patent number: 8946440
    Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).
    Type: Grant
    Filed: April 27, 2009
    Date of Patent: February 3, 2015
    Assignees: Kyorin Pharmaceutical Co., Ltd., Teijin Pharma Limited
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Masanori Yamamoto
  • Publication number: 20150030610
    Abstract: Disclosed herein are combinatorial therapies for treating or preventing reoccurrence of cancer. The therapies involve inhibition of LIMK1 in conjunction with taxane therapy. Specifically exemplified herein is co-administration of a LIMK1 RNA interfering molecule along with administration of a taxane.
    Type: Application
    Filed: February 7, 2013
    Publication date: January 29, 2015
    Applicant: University of Central Florida Research Foundation, Inc.
    Inventor: Ratna Chakrabarti
  • 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: 8940771
    Abstract: The present invention relates to compounds of formula I and its salts, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: January 27, 2015
    Assignee: Novartis AG
    Inventors: Giorgio Caravatti, Robin Alec Fairhurst, Pascal Furet, Vito Guagnano, Patricia Imbach
  • Patent number: 8940271
    Abstract: The invention includes compositions for transmucosal administration to an animal comprising at least one active agent and a pharmaceutically acceptable carrier. A preferred active agent is selected from the group consisting of meloxicam, carprofen, enrofloxacin, clemastine, diphenhydramine, digoxin, levothyroxine, cyclosporine, ondansetron, lysine, zolpidem, propofol, nitenpyram, ivermectin, milbemycin, and pharmaceutically acceptable salts, solvates and esters thereof. In another embodiment, the invention includes methods of treating or preventing a condition in an animal comprising transmucosally administering a composition comprising a therapeutically or prophylactically effective amount of an active agent and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: January 27, 2015
    Assignee: Abbott Laboratories
    Inventors: Mark C. Heit, Antonio M. Benitz, Dennis F. Steadman, David M. Petrick
  • Publication number: 20150025076
    Abstract: The present invention relates to modulator of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: October 6, 2014
    Publication date: January 22, 2015
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Ashvani K. Singh, Thomas Cleveland, Lewis R. Makings, Matthew Hamilton, Peter D.J. Grootenhuis
  • Publication number: 20150018330
    Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.
    Type: Application
    Filed: July 30, 2014
    Publication date: January 15, 2015
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. MacDonald, Thomas Eric Ballard, JR.
  • Patent number: 8921576
    Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: December 30, 2014
    Assignee: Kowa Company, Ltd.
    Inventors: Takahisa Ogamino, Yukiyoshi Yamazaki, Shin Tanikawa, Ayumu Okuda, Tomoaki Fukuda, Okihisa Tokuda, Yoshiharu Miyake, Shinsuke Itoh, Hiroyuki Ishiwata
  • Publication number: 20140378510
    Abstract: Provided herein are small molecule activators of calcium-activated chloride channels. These small molecules may be used for treatment of diseases and disorders that are treatable by activating calcium-activated chloride channels, such as cystic fibrosis, disorders related to salivary gland dysfunction (for example, Sjogren's syndrome and dysfunction following radiation injury), dry eye syndrome, and intestinal hypomotility.
    Type: Application
    Filed: August 3, 2012
    Publication date: December 25, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Alan S. Verkman, Wan Namkung
  • Patent number: 8907092
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1-M-U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3?, R4, R4? and R5, are as described herein.
    Type: Grant
    Filed: April 29, 2008
    Date of Patent: December 9, 2014
    Assignee: Genentech, Inc.
    Inventors: John A. Flygare, Frederick Cohen, Kurt Deshayes, Michael F. T. Koehler, Lewis J. Gazzard, Lan Wang, Chudi Ndubaku
  • Patent number: 8895587
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: November 25, 2014
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Patent number: 8895592
    Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein L1, A1, R1g, z, R2, R3, and R4 are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: November 25, 2014
    Assignee: AbbVie Inc.
    Inventors: Jennifer M. Frost, Steven P. Latshaw, Michael J. Dart, William A. Carroll, Arturo Perez-Medrano, Teodozyj Kolasa, Meena V. Patel, Derek W. Nelson, Tongmei Li, Sridhar Peddi, Xueqing Wang, Bo Liu
  • Patent number: 8889718
    Abstract: Method of treating central nervous systems disease by administering wherein n is an integer of from 0 to 3; R1A is a 5-membered aromatic heterocyclic group containing at least one oxygen atom; R2A is —COR8 (wherein R8 is aryl); R3A is hydrogen or lower alkyl; and R12 represents cycloalkyl, aryl, aralkyl, alicyclic heterocyclic group, aromatic heterocyclic group, alicyclic hetocyclic-alkyl, or aromatic heterocyclic-alkyl, and R1A, R2A, R3A and R12 are individually optionally substituted.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: November 18, 2014
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Takao Nakajima, Masamori Sugawara, Shin-ichi Uchida, Tetsuji Ohno, Yuji Nomoto, Noriaki Uesaka, Yoshisuke Nakasato
  • Patent number: 8889722
    Abstract: An optically active 4-phenylthiazole derivative having a thrombopoietin receptor agonist activity and a pharmaceutical composition containing the present compound as an active ingredient are created, and a platelet production regulating agent which can be orally administered is provided. Disclosed is a pharmaceutical composition containing, as an active ingredient, an optically active compound represented by the formula: wherein, R1 is a halogen atom or C1-C3 alkyloxy; R2 is C1-C8 alkyl; R3 is C1-C8 alkyl; R4 and R5 are each independently a fluorine atom or chlorine atom; R6 is C1-C3 alkyl or C1-C3 alkyloxy; * indicates that a carbon atom marked with an asterisk is an asymmetric carbon, a pharmaceutically acceptable salt thereof, or a solvate thereof.
    Type: Grant
    Filed: February 13, 2013
    Date of Patent: November 18, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masami Takayama, Noriyuki Kurose
  • Patent number: 8889862
    Abstract: The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: November 18, 2014
    Assignee: Glenmark Pharmaceuticals, S.A.
    Inventors: Sukeerthi Kumar, Abraham Thomas, Sachin Sundarlal Chaudhari, Bipin Parsottam Kansagra, Venkata Ramana Yemireddy, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay, Girish Gudi
  • Patent number: 8883473
    Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: November 11, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Kristi A. Leonard, Richard Scott Alexander, Joseph Kent Barbay, Roger F. Bone, Carl Crysler, Ingrid Christa Deckman, Paul F. Jackson, Lawrence C. Kuo, Frank A. Lewandowski, Diane M. Maguire, Carl Manthey, Cynthia M. Milligan, Beverley Moore, Kenneth J. Rhodes, Robert H. Scannevin, Celine Schalk-Hihi, Barry Springer, John C. Spurlino, Matthew J. Todd, Brett A. Tounge, Aihua Wang
  • Patent number: 8883793
    Abstract: Compounds represented by the formula (I) or pharmaceutically acceptable salts thereof: R2—Y—Z-Q-A-R1??Formula (I) wherein R1, R2, Y, Z, Q, and A are as defined. These compounds are inhibitors of tubulin polymerization by binding at colchicines binding site and are useful in the treatment of tumors or mitotic diseases such as cancers, gout, and other conditions associated with abnormal cell proliferation.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: November 11, 2014
    Assignee: Development Center for Biotechnology
    Inventors: Meng-Hsin Chen, Shih-Hsien Chuang, Yi-Jen Chen, Lien-Hsiang Chang, Tsung-Hui Li, Ching-Hui Chen, Win-Yin Wei