1,3-thiazoles (including Hydrogenated) Patents (Class 514/365)
  • Patent number: 11040963
    Abstract: The present invention provides piperazine derivatives exhibiting high affinity to the stem region (viral membrane proximal part) of influenza hemagglutinin as determined through competition binding and high virus neutralization activity while having low cytotoxity. Furthermore, the present invention relates to pharmaceutical compositions comprising said piperazine derivatives, methods of preparing said piperazine derivatives, as well as said piperazine derivatives for use in medical prevention or treatment, especially for preventing or treating influenza.
    Type: Grant
    Filed: February 1, 2018
    Date of Patent: June 22, 2021
    Assignee: JANSSEN VACCINES & PREVENTION B.V.
    Inventors: Maria Van Dongen, Jaroslaw Juraszek, Griet Wim Bert Schepens, Charles Edward Lawson, Brian Shook, Maria Tim Hugo Jonckers, Abdellah Tahri, Bernard Pierre Jean-Marie Raboisson, Nestor CHristophe Francis Robert Buyck
  • Patent number: 11033601
    Abstract: Disclosed herein are methods and compositions for treating nonalcoholic fatty liver disease. Specifically exemplified herein is administration of compositions comprising a V1b inhibitor or V1a agonist or V1a stabilizer.
    Type: Grant
    Filed: September 14, 2018
    Date of Patent: June 15, 2021
    Assignee: The Regents of the University of Colorado, a body corporate
    Inventors: Richard J. Johnson, Miguel A. Lanaspa Garcia, Thomas Jensen
  • Patent number: 10980776
    Abstract: The present invention relates to a pharmaceutical combination for use in the treatment of squamous cell carcinoma, comprising a CDK inhibitor selected from the compounds of formula (I); or a pharmaceutically acceptable salt thereof and one or more antineoplastic agents selected from sorafenib, lapatinib, erlotinib, cisplatin, 5-fluorouracil, docetaxel or cetuximab or a pharmaceutically acceptable salt thereof. The said pharmaceutical combination exhibits synergy when used in the treatment of squamous cell carcinoma of head and neck (SCCHN). The invention also relates to a pharmaceutical composition comprising the said combination and a method for the treatment of squamous cell carcinoma of head and neck (SCCHN), using a therapeutically effective amount of said combination.
    Type: Grant
    Filed: February 8, 2019
    Date of Patent: April 20, 2021
    Assignee: PIRAMAL ENTERPRISES LIMITED
    Inventors: Veena Agarwal, Arun Balakrishnan, Giridharan Periyasamy
  • Patent number: 10980782
    Abstract: The present application discloses a pharmaceutical preparation comprising a de-epoxidized epothilone derivative, and especially relates to a preparation formulation of a compound with reduced allergens and toxicity; and also relates to the use thereof in the treatment of tumours, especially the use thereof in the treatment of solid tumours that are resistant to and fail to respond to other conventional chemotherapeutic agents, as well as the use thereof in the treatment of cancers alone or in combination with other tumour drugs or auxiliary drugs.
    Type: Grant
    Filed: February 6, 2017
    Date of Patent: April 20, 2021
    Assignees: BEIJING BIOSTAR TECHNOLOGIES, LTD., CHENGDU BIOSTAR PHARMACEUTICALS, LTD.
    Inventors: Li Tang, Rongguo Qiu
  • Patent number: 10981897
    Abstract: The present invention provides compounds of the formula: (I) wherein: X is O or S; Q1 and Q2 are independently CR5 or N, provided at least one of Q1 and Q2 is N; Y is a direct bond or CH2; R1 is H, optionally substituted alkyl, alkenyl, alkynyl, cycloalkylalkyl, benzyl or oxetan-3-yl-CH2—; R2 is optionally substituted phenyl, pyridine, pyrimidine, pyrazine or pyridazine; R3 is alkyl or haloalkyl; R4 is optionally substituted pyridine, pyrimidine, pyrazine or pyridazine; R5 is H, alkyl, haloalkyl, cycloalkyl, alkoxy, alkoxyC(O)— or (alkoxy)2CH—; or a salt thereof. The compounds are useful for controlling ectoparasites on animals.
    Type: Grant
    Filed: April 30, 2019
    Date of Patent: April 20, 2021
    Assignee: Elanco Tiergesundheit AG
    Inventors: Paolo Tosatti, Jean-Yves Wach
  • Patent number: 10968185
    Abstract: Inhibitor compounds and agents of Cathepsin C, CELA1, CELA3A and/or structurally related molecules thereto, compositions comprising same and uses thereof in the inhibition and/or prevention of cell and/or tissue necrosis are described. The compounds include thiazoles of Formula II, where G1 is an optionally substituted pyrrolidine, an optionally substituted pyridine, an optionally substituted aryl, an optionally substituted piperidine, an optionally substituted piperazine, an optionally substituted imidazolidine, or an optionally substituted pyrazolidine. G3 is or G3 is an optionally substituted alkyl, an optionally substituted aryl or an optionally cyloalkyl. G2 is an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted cyloalkyl or an optionally substituted heterocycle. Various applications for the described compounds, and combination therapies are described as well.
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: April 6, 2021
    Assignee: ELA PHARMA LTD.
    Inventors: Ilana Nathan, Boris Khalfin
  • Patent number: 10954230
    Abstract: This invention relates to a method of preparing inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
    Type: Grant
    Filed: February 14, 2020
    Date of Patent: March 23, 2021
    Assignee: GENZYME CORPORATION
    Inventors: Craig S. Siegel, Rayomand Gimi, Michael Reardon, Jin Zhao
  • Patent number: 10941125
    Abstract: Peroxisome proliferator activated receptor (PPAR) compounds, and methods of using the same for treating bone fractures, treating osteoporosis and/or metabolic bone diseases, and inducing osteogenesis and/or chondrogenesis, are disclosed.
    Type: Grant
    Filed: July 8, 2019
    Date of Patent: March 9, 2021
    Assignee: The University of Toledo
    Inventors: Bruce E. Heck, Dong Hyun Kim, Paul W. Erhardt, Brian Kress
  • Patent number: 10927138
    Abstract: Provided herein are compounds of Formula (I) and uses thereof for inhibiting the activity of D-amino acid oxidase (DAAO) or treating diseases or disorders associated with DAAO, such as a central nervous system (CNS) disorder, obesity, diabetes, or hyperlipidemia. Also provided in the present disclosure are methods of synthesizing the Formula (I) compounds described herein.
    Type: Grant
    Filed: May 29, 2018
    Date of Patent: February 23, 2021
    Assignee: SYNEURX INTERNATIONAL (TAIWAN) CORP.
    Inventors: Guochuan Emil Tsai, Ching-Cheng Wang, Ming-Hong Chien, Tien-Lan Hsieh
  • Patent number: 10776461
    Abstract: Peroxisome proliferator activated receptor (PPAR) compounds, and methods of using the same for treating bone fractures, treating osteoporosis and/or metabolic bone diseases, and inducing osteogenesis and/or chondrogenesis, are disclosed.
    Type: Grant
    Filed: January 14, 2019
    Date of Patent: September 15, 2020
    Assignee: The University of Toledo
    Inventors: Bruce E. Heck, Dong Hyun Kim, Paul W. Erhardt, Brian J. Kress
  • Patent number: 10765629
    Abstract: Described herein is a solid complex comprising (Z)-7-((1R,2R,3R,5S)-2-((S,E)-5-(2,5-dichlorothiophen-3-yl)-3-hydroxypent-1-en-1-yl)-3,5-dihydroxycyclopentyl)hept-5-enamide (hereinafter “Compound 1”) and ?-cyclodextrin, and preparations and uses thereof. Also described herein are certain solid forms, preparations and uses thereof.
    Type: Grant
    Filed: July 24, 2018
    Date of Patent: September 8, 2020
    Assignee: ALLERGAN, INC.
    Inventors: Ke Wu, Evgenyi Shalaev, Prem Swaroop Mohanty, Jinping Wan
  • Patent number: 10723727
    Abstract: The present invention is directed to novel cytotoxic tubulysin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: July 28, 2020
    Assignee: Pfizer Inc.
    Inventors: Chakrapani Subramanyam, Lawrence N. Tumey, Longfei Xie, Carolyn Leverett, Beth C. Vetelino, Sai Chetan K. Sukuru, Sarah Hudson, Venkata Ramana Doppalapudi, Abhijit S. Bhat
  • Patent number: 10675273
    Abstract: Disclosed herein, inter alia, are compounds and methods for increasing spine density in a neuron, and for treatment of neuronal diseases and cancer.
    Type: Grant
    Filed: January 4, 2017
    Date of Patent: June 9, 2020
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventor: Jerry Yang
  • Patent number: 10669588
    Abstract: This invention relates to a novel approach for the identification and stratification of subtypes of cancer, particularly pancreatic ductal adenocarcinoma (PDAC). The invention furthermore relates to a novel approach with respect to the treatment of cancer, particularly pancreatic ductal adenocarcinoma (PDAC).
    Type: Grant
    Filed: September 28, 2015
    Date of Patent: June 2, 2020
    Assignee: HI-STEM GGMBH
    Inventors: Andreas Trumpp, Martin Ronald Sprick, Elisa Noll
  • Patent number: 10632106
    Abstract: Provided herein are methods of cancer treatment by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its structural analogs to a patient with cancer, for example, prostate, liver, lung, ovarian, breast, skin, colon (or rectum), stomach, pancreatic, kidney, bladder, soft tissue, or cervical cancer.
    Type: Grant
    Filed: July 27, 2018
    Date of Patent: April 28, 2020
    Assignee: Ariagen, Inc.
    Inventor: Jiasheng Song
  • Patent number: 10617674
    Abstract: This invention relates to a novel dosage regimen for administration of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide or a pharmaceutically acceptable derivative thereof, namely in the treatment of acute exacerbations of inflammatory conditions.
    Type: Grant
    Filed: March 8, 2016
    Date of Patent: April 14, 2020
    Assignee: MEREO BIOPHARMA 1 LIMITED
    Inventors: Colin Orford, Cyril Clarke, Colm Farrell, Jacqueline Parkin, Stefan De Buck
  • Patent number: 10464942
    Abstract: The invention relates to the process of manufacturing Epothilone compounds of Formulas I-IV. The process of the present invention is totally synthetic, utilizes highly pure and crystalline Epothilone B, and produces ixabepilone in high efficiency, purity, and yield.
    Type: Grant
    Filed: November 20, 2017
    Date of Patent: November 5, 2019
    Assignee: PHARMAREN, LLC
    Inventors: Jalal Haddad, Sourena Nadji
  • Patent number: 10450292
    Abstract: The invention provides compounds that are inhibitors of bacterial RNA polymerase. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: October 22, 2019
    Assignee: Rutgers, The State University of New Jersesy
    Inventors: Richard H. Ebright, Joel Freundlich, Nisha Mittal, Mark Jaskowski, Juan Shen
  • Patent number: 10322110
    Abstract: The present invention relates to therapeutic agents suitable for use in the treatment of microbial infection in mammals. The present invention further relates to the use of pharmaceutical compositions comprising said agents in the treatment of medical conditions in mammals, in particular in the treatment of microbial infection. The agents and pharmaceutical compositions of the invention are of particular relevance in the treatment of diseases associated with antibiotic-resistant microbes. In one particular embodiment, the pharmaceutical composition can have the structural moiety of formula (I) or a pharmaceutically-acceptable salt of said compound: wherein group A is selected from the formulae Group B is aryl, R1 is an optionally substituted aryl ring, an optionally substituted benzyl ring, CH3, or C2 to 6 alkyl, and R2 is hydrogen, an alkyl group, a halogen, or —(CH2)nN(CH3)2 where n is an integer from 1 to 3.
    Type: Grant
    Filed: December 3, 2015
    Date of Patent: June 18, 2019
    Assignee: Procomcure Biotech GmbH
    Inventors: Kamil Önder, Roelf Datema, Dale Mitchell, Ivan Kondratov
  • Patent number: 10315998
    Abstract: The present invention belongs to the field of fungicides, and relates to an amide compound and the preparation method and use thereof. The amide compound is as shown in general formula I: Each substituent in Formula I is defined in the description. The compound of general formula I of the present invention has an outstanding fungicidal activity, and can be used for controlling fungal diseases.
    Type: Grant
    Filed: May 4, 2016
    Date of Patent: June 11, 2019
    Assignee: SHENYANG SINOCHEM AGROCHEMICALS R&D CO., LTD.
    Inventors: Liang Lv, Gang Wang, Zhonggang Shan, Jiyong Liu, Qin Sun, Junfeng Wang, Bin Li
  • Patent number: 10272055
    Abstract: Biguanide compounds and salts thereof are disclosed. Also disclosed are pharmaceutical compositions and therapeutic methods for treating certain diseases including cancer such as breast cancer.
    Type: Grant
    Filed: March 6, 2015
    Date of Patent: April 30, 2019
    Assignees: Regents of the University of Minnesota, The Regents of the University of California
    Inventors: David A. Potter, Zhijun Guo, Elizabeth Amin, Gunda Georg, Tom Poulos, Irina Sevrioukova
  • Patent number: 10245251
    Abstract: The present invention relates to a pharmaceutical combination for use in the treatment of squamous cell carcinoma, comprising a CDK inhibitor selected from the compounds of formula (I); or a pharmaceutically acceptable salt thereof and one or more antineoplastic agents selected from sorafenib, lapatinib, erlotinib, cisplatin, 5-fluorouracil, docetaxel or cetuximab or a pharmaceutically acceptable salt thereof. The said pharmaceutical combination exhibits synergy when used in the treatment of squamous cell carcinoma of head and neck (SCCHN). The invention also relates to a pharmaceutical composition comprising the said combination and a method for the treatment of squamous cell carcinoma of head and neck (SCCHN), using a therapeutically effective amount of said combination.
    Type: Grant
    Filed: July 8, 2016
    Date of Patent: April 2, 2019
    Assignee: PIRAMAL ENTERPRISES LIMITED
    Inventors: Veena Agarwal, Arun Balakrishnan, Giridharan Periyasamy
  • Patent number: 10221169
    Abstract: Disclosed ore substituted aminothiazoles, which can be used for, among other things, the treatment of tuberculosis, pharmaceutical compositions containing the same, and methods of using the same.
    Type: Grant
    Filed: March 23, 2017
    Date of Patent: March 5, 2019
    Assignees: The Broad Institute, Inc., The General Hospital Corporation, The Brigham and Women's Hospital, Inc.
    Inventors: Deborah Hung, Michael Serrano-Wu, Sarah Grant, Tomohiko Kawate
  • Patent number: 10195182
    Abstract: A method of cancer intervention or eradication by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its analogs (the active ingredient) to a subject with cancer is disclosed. An effective dose and dosing frequency of the active ingredient are determined by measuring its blood levels of the subject after dosing. The active ingredient formulated with a carrier system is applied topically, enterally, or parenterally to the subject. The formulated drug can also be administered together with one or more of other cancer therapeutic agents. A maintenance dosing is provided after the subject is free of cancer to insure the cancer eradication. Subjects with cancers of prostate, liver, lung, ovarian, and breast are preferably accepted for treatment.
    Type: Grant
    Filed: June 5, 2017
    Date of Patent: February 5, 2019
    Assignee: Ariagen, Inc.
    Inventor: Jiasheng Song
  • Patent number: 10188639
    Abstract: The invention provides enantiopure deuterium-enriched pioglitazone, pharmaceutical compositions, and methods of treating neurological disorders, cancer, respiratory disorders, metabolic disorders, and other disorders using enantiopure deuterium-enriched pioglitazone. A preferred aspect of the invention provides methods of treating Alzheimer's disease, non-small cell lung cancer, hepatocellular carcinoma, and chronic obstructive pulmonary disease using enantiopure deuterium-enriched pioglitazone.
    Type: Grant
    Filed: January 15, 2015
    Date of Patent: January 29, 2019
    Assignee: DeuteRx, LLC
    Inventors: Sheila DeWitt, Vincent Jacques, Leonardus H. T. van der Ploeg
  • Patent number: 10179780
    Abstract: There are provided: 4-methyl-2-[4-(2-methylpropoxy)-3-(1H-1,2,3,4-tetrazol-1-yl)phenyl]-1,3-thiazole-5-carboxylic acid, a sodium salt thereof and crystals of these, useful as a therapeutic agent and a prophylactic agent for gout, hyperuricemia and the like, and a method for producing the same.
    Type: Grant
    Filed: July 29, 2015
    Date of Patent: January 15, 2019
    Assignee: Teijin Pharma Limited
    Inventors: Asahi Kawana, Hisae Nozato, Chikashi Kanazawa
  • Patent number: 10138216
    Abstract: Described herein are analogues of 2-methyl-3-(2-ethynylthiazol-4-yl)cyclopent-2-enol and the corresponding ketone 3-(2-ethynylthiazol-4-yl)-2-methylcyclopent-2-enone, the analogues having terminal alkyne groups at the 2-position of the thiazole ring. These drug-like molecules, referred to as CETZOLE compounds, are useful to treat non-small cell lung cancer and other forms of cancer. Methods of making and using the compounds, methods of treating various diseases, pharmaceutical compositions, and kits are also disclosed.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: November 27, 2018
    Assignee: The University of Toledo
    Inventors: Viranga Tillekeratne, William Taylor, Sara Fedorka
  • Patent number: 10117877
    Abstract: Disclosed herein are methods, compounds, and compositions for fat reduction, and in particular fat reduction without significant hair growth and/or additional hair growth.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: November 6, 2018
    Assignee: ALLERGAN, INC.
    Inventors: Neil J. Poloso, Jenny Wang, David F. Woodward, Robert M. Burk
  • Patent number: 10092617
    Abstract: The present invention relates to the field of nanotechnology, in particular, to the production of biodegradable polymeric nanoparticles. The present invention provides a biodegradable polymeric nanoparticle made up of a block copolymer and a process for producing the same. The nanoparticles are produced without the use of any emulsifiers and have a size ranging from 30-120 nm. The methods of controlling the drug loading capacity are disclosed along with the process of producing entity-loaded nanoparticles. Compositions comprising the nanoparticles and their use in therapeutics, diagnostics and theranostics are also disclosed.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: October 9, 2018
    Assignee: NANOPROTEAGEN
    Inventor: Harpal Singh
  • Patent number: 10073072
    Abstract: This disclosure describes the results of the studies conducted to develop a dissolution method to monitor release profiles of hydrophobic active pharmaceutical ingredients such as ivermectin with or without pyrantel pamoate from a drug product made of complex matrix that includes, but is not limited to beef, tallow, corn cob and soy protein.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: September 11, 2018
    Assignee: MERIAL INC.
    Inventors: Abu M. Rustum, Satish Kumar, Andrew L. McAdoo
  • Patent number: 10065950
    Abstract: [Problem] Provided is a novel 1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, or a solvate thereof, which is useful as an anti-HIV agent. [Solving Means] The present invention provides a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: September 4, 2018
    Assignee: Japan Tobacco Inc.
    Inventors: Susumu Miyazaki, Yuki Bessho, Kaoru Adachi, Seiji Kawashita, Hirotaka Isoshima, Kengo Oshita, Shunichi Fukuda
  • Patent number: 10043292
    Abstract: A computer-controlled system determines attributes of a frexel, which is an area of human skin, and applies a reflectance modifying agent (RMA) at the pixel level to automatically change the appearance of human features based on one or more digital images. The change may be based on a digital image of the same frexel, for as seen in a prior digital photograph captured previously by the computer-controlled system. The system scans the frexel and uses feature recognition software to compare the person's current features in the frexel with that person's features in the digital image. It then calculates enhancements to the make the current features appear more like the features in the digital image, and it applies the RMA to the frexel to accomplish the enhancements. Or the change may be based on a digital image of another person, through the application of RMAs.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: August 7, 2018
    Assignee: TCMS Transparent Beauty LLC
    Inventors: Albert D. Edgar, David C. Iglehart, Rick B. Yeager
  • Patent number: 10028508
    Abstract: The invention is in the technical field of vector control as well as insecticide-resistant mosquito and bed bug control. The active compound compositions of this invention are used against mosquitos and bed bugs which transmit disease pathogens or which annoy the well-being of humans and animals. The active compound compositions of this invention are in particular useful to overcome target-specific and/or metabolic-specific resistance of mosquitos and bed bugs and are biologically efficient on a variety of surfaces over an extended period of time.
    Type: Grant
    Filed: June 19, 2015
    Date of Patent: July 24, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Karin Horn, Rainer Sonneck, Arnoldus Vermeer, Sebastian Horstmann, Guenther Nentwig, Frederic Schmitt
  • Patent number: 10010535
    Abstract: Iron overload is associated with pathological conditions such as oxidative stress, transfusional iron overload, thalassemia, primary hemochromatosis, secondary hemochromatosis, diabetes, liver disease, heart disease, cancer, radiation injury, neurological or neurodegenerative disorder, Friedreich's ataxia (FRDA), macular degeneration, closed head injury, irritable bowel disease, and reperfusion injury. The present invention provides methods and pharmaceutical compositions using desferrithiocin analogs of Formulae (A) and (J) for treating and/or preventing these pathological conditions, metal (e.g., iron, aluminum, a lanthanide, or an actinide (e.g., uranium)) overload conditions, and infectious diseases (e.g., malaria).
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: July 3, 2018
    Assignee: University of Florida Research Foundation, Incorporated
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 10000474
    Abstract: Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of cancer. Additionally, provided is a method for treating cancer, comprising the step of administering a therapeutically effective amount of a compound according to formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier to a patient in need thereof.
    Type: Grant
    Filed: November 6, 2015
    Date of Patent: June 19, 2018
    Assignee: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Patrick M. Woster, Youxuan Li
  • Patent number: 9918958
    Abstract: The invention provides a method for treating hypoxia in a normal subject, comprising administering 5-HMF to the subject.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: March 20, 2018
    Inventor: Warren Stern
  • Patent number: 9914712
    Abstract: Compounds of general formula (I): wherein R1, R11, Y, R2, n and A are as defined herein are useful as inhibitors or metallo-?-lactamase (MBL) enzymes and can be used for reducing or removing antibiotic resistance in bacteria.
    Type: Grant
    Filed: June 12, 2014
    Date of Patent: March 13, 2018
    Assignee: ANTABIO SAS
    Inventors: Marc Lemonnier, David Davies, Thomas David Pallin
  • Patent number: 9878970
    Abstract: The present invention relates to a novel a process for the preparation of 9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-ylamine which process comprises a) reacting cyclopentadiene in the presence of a radical initiator and CXCl3, wherein X is chloro or bromo, to a compound of formula I1, or aa) reacting cyclopentadiene with CXCl3, wherein X is chloro, in the presence of a metal catalyst to a compound of formula I1, wherein X is chloro, b) reacting the compound of formula I1 with a base in the presence of an appropriate solvent to the compound of formula III, c) and converting the compound of formula III in the presence of 1,2-dehydro-6-nitrobenzene to the compound of formula IV, and d) hydrogenating the compound of formula IV in the presence of a metal catalyst.
    Type: Grant
    Filed: September 27, 2017
    Date of Patent: January 30, 2018
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Denis Gribkov, Bjorn Antelmann, Fanny Bois, Harald Walter, Alain De Mesmaeker
  • Patent number: 9849147
    Abstract: The present invention relates to a fast dissolving tablet comprising a therapeutically effective amount of a phosphate binding polymer, such as sevelamer or pharmaceutically acceptable salt or derivative thereof, that exhibit limited swelling in the oral cavity, has pleasant taste and mouth feel, high phosphate binding capacity with fast binding kinetics and require limited amount of water intake. A process for the preparation thereof is disclosed.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: December 26, 2017
    Assignee: PHARMATHEN S.A.
    Inventors: Evangelos Karavas, Efthimios Koutris, Vasiliki Samara, Analia Diakidou, Georgia Papanikolaou, Panagiotis Mparmpalexis
  • Patent number: 9815826
    Abstract: There are provided crystals of 2-[4-(2,2-dimethylpropoxy)-3-(1H-1,2,3,4-tetrazol-1-yl)phenyl]-4-methyl-1,3-thiazole-5-carboxylic acid which is useful as a therapeutic agent or prophylactic agent for gout, hyperuricemia and the like.
    Type: Grant
    Filed: July 29, 2015
    Date of Patent: November 14, 2017
    Assignee: Teijin Pharma Limited
    Inventors: Asahi Kawana, Yuki Miyazawa
  • Patent number: 9795615
    Abstract: Disclosed herein are methods, compounds, and compositions for fat reduction, and in particular fat reduction without significant hair growth and/or additional hair growth.
    Type: Grant
    Filed: April 29, 2016
    Date of Patent: October 24, 2017
    Assignee: ALLERGAN, INC.
    Inventors: Neil J. Poloso, Jenny Wang, David F. Woodward, Robert M. Burk
  • Patent number: 9694000
    Abstract: A method of cancer intervention or eradication by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its analogs (the active ingredient) to a subject with cancer is disclosed. An effective dose and dosing frequency of the active ingredient are determined by measuring its blood levels of the subject after dosing. The active ingredient formulated with a carrier system is applied topically, enterally, or parenterally to the subject. The formulated drug can also be administered together with one or more of other cancer therapeutic agents. A maintenance dosing is provided after the subject is free of cancer to insure the cancer eradication. Subjects with cancers of prostate, liver, lung, ovarian, and breast are preferably accepted for treatment.
    Type: Grant
    Filed: December 7, 2015
    Date of Patent: July 4, 2017
    Assignee: AHR PHARMACEUTICALS, INC.
    Inventor: Jiasheng Song
  • Patent number: 9682037
    Abstract: Orally disintegrating film dosage forms for delivering active pharmaceutical agents, methods of formulating the dosage forms to retard absorption through the oral mucosa, and methods of using the dosage forms for the treatment of various medical conditions are provided.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: June 20, 2017
    Assignee: APR APPLIED PHARMA RESEARCH SA
    Inventors: Christian Leichs, Armin Breitenbach, Ingo Lehrke, Paolo Galfetti
  • Patent number: 9567309
    Abstract: Compounds represented by structural formulas described herein, such as Structural Formula (I): or a pharmaceutically acceptable salt thereof are useful in treating conditions such as metal overload, oxidative stress, and neoplastic and preneoplastic conditions.
    Type: Grant
    Filed: July 28, 2015
    Date of Patent: February 14, 2017
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 9556169
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: January 31, 2017
    Assignee: Novartis AG
    Inventors: Arnab Kumar Chatterjee, Advait Suresh Nagle, Prasuna Paraselli, Ravinder Reddy Kondreddi, Seh Yong Leong, Pranab Kumar Mishra, Robert Joseph Moreau, Jason Thomas Roland, Wei Lin Sandra Sim, Oliver Simon, Jocelyn Liying Tan, Bryan K S Yeung, Bin Zou, Venkatataiah Bollu
  • Patent number: 9518048
    Abstract: A process for the preparation of teneligliptin.
    Type: Grant
    Filed: August 28, 2013
    Date of Patent: December 13, 2016
    Assignee: Glenmark Pharmaceuticals Limited
    Inventors: Suresh Mahadev Kadam, Bipin Parsottam Kansagra, Ramchandran Vishnue Kale, Jayant Prakashrao Patil, Venkataramana Reddy Yemireddy, Shailendra Nilkanth Bhadane, Uddhav Popat Chaudhar, Ulhas Digambar Patil, Shekhar Bhaskar Bhirud
  • Patent number: 9498537
    Abstract: A method of improving the efficacy of a blood transfusion into a subject is provided comprising administering a composition comprising an EAF PEGylated-blood protein into the subject, prior to, during, or subsequent to the blood transfusion.
    Type: Grant
    Filed: August 7, 2014
    Date of Patent: November 22, 2016
    Assignees: Albert Einstein College of Medicine, Inc., The Regents of the University of California
    Inventors: Seetharama A. Acharya, Marcos Intaglietta
  • Patent number: 9479586
    Abstract: A distributed system for storing digital data is disclosed. The distributed system includes a portable storage device suitable for being connected to a terminal, at least one storage server and a dispatching server. The dispatching server is suitable for retrieving accessibility information indicating that the at least one storage server is accessible by the portable storage device. The portable storage device is suitable for, when connected to the terminal, sending identification information to the dispatching server. The dispatching server is suitable for, upon reception of the identification information, using the identification information for retrieving the accessibility information and for sending the accessibility information to the portable storage device.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: October 25, 2016
    Assignee: Telecom Italia S.p.A.
    Inventors: Pino Castrogiovanni, Giovanni Malnati, Giovanni Martini
  • Patent number: 9447049
    Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: September 20, 2016
    Assignee: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
    Inventors: Wei Li, Min Xiao, James Dalton, Sunjoo Ahn, Duane D. Miller, Jianjuan Chen, Jin Wang
  • Patent number: RE46792
    Abstract: The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: wherein R1 is an aryl group which may have one or more substituents; R2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y1-A1- or or —Y2—C(?O)— wherein Y1 is a group such as —C(?O)—, A1 is a group such as a lower alkylene group, and Y2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.
    Type: Grant
    Filed: June 14, 2017
    Date of Patent: April 17, 2018
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Minoru Okada, Masaya Kato, Norifumi Sato, Tetsuyuki Uno, Hideki Kitagaki, Junpei Haruta, Hidetaka Hiyama, Tomonori Shibata