1,3-thiazoles (including Hydrogenated) Patents (Class 514/365)
  • Patent number: 11897852
    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: February 10, 2021
    Date of Patent: February 13, 2024
    Assignee: The University of Toledo
    Inventors: Bruce E. Heck, Dong Hyun Kim, Paul W. Erhardt, Brian Kress
  • Patent number: 11819023
    Abstract: A natural liquid composition is provided for disinfectant, antibacterial or anticorrosion applications. The natural liquid composition is an electrospun solubilized composition of natural chitosan (CS) and an FDA approved polymer polyvinyl alcohol (PVA). Two fillers, citric acid (CA) and ascorbic acid (AA), added anti-corrosion property to the composite nanofiber solution without affecting the other properties (disinfectant and antibacterial) and have a final synergistic effect of all components together in a final solution form. Embodiment of the invention advances the art by providing a natural solution to overcome at least some of the problems with the currently used agents.
    Type: Grant
    Filed: November 15, 2017
    Date of Patent: November 21, 2023
    Assignee: The American University in Cairo
    Inventors: Wael Mamdouh Sayed Sayed Ahmed, James Kegere
  • Patent number: 11701341
    Abstract: The invention relates to pharmaceutical compositions comprising 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide for use in the treatment of acute exacerbations of chronic obstructive pulmonary disease in human patients having <2% blood eosinophils. The invention also relates to pharmaceutical compositions for the treatment of AECOPD in a human patient having <2% blood eosinophils, comprising administering to the patient three separate therapeutically effective doses of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide over a period of not longer than ten days with at least one day between every dose.
    Type: Grant
    Filed: December 11, 2018
    Date of Patent: July 18, 2023
    Assignee: MEREO BIOPHARMA 1 LIMITED
    Inventors: Alastair MacKinnon, Jacqueline Parkin
  • Patent number: 11613534
    Abstract: Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for vascular disorders that can include, for example, retinopathies, ocular edema, and ocular neovascularization.
    Type: Grant
    Filed: October 28, 2020
    Date of Patent: March 28, 2023
    Assignee: EyePoint Pharmaceuticals, Inc.
    Inventor: John M. Janusz
  • Patent number: 11607403
    Abstract: The therapeutic uses of febuxostat or febuxostat derivatives and compositions comprising febuxostat or febuxostat derivatives to promote neurogenesis for the treatment of disease.
    Type: Grant
    Filed: November 8, 2016
    Date of Patent: March 21, 2023
    Assignee: Morningside Ventures Limited
    Inventors: Nancy Yuk-Yu Ip, Wing-Yu Fu, Fanny Chui Fun Ip, Kit Yu Fu
  • Patent number: 11547698
    Abstract: The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts, R? is H, CN, CH2(OH)R0, CmH2m+1, CnH2n-1, CnH2n-3, two Ra is independently H, or two Ra together form ?O or ?N—W3—R1; A is a C6 to C10 aromatic ring, or a C2 to C10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and C?N, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C6 to C10 aromatic ring or a C2 to C10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is Rc connected with C or RN connected with N.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: January 10, 2023
    Assignee: ARIAGEN, INC.
    Inventors: Luqing Yang, Guodong Li, Suoming Zhang
  • Patent number: 11524004
    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: September 14, 2020
    Date of Patent: December 13, 2022
    Assignee: The University of Toledo
    Inventors: Bruce E. Heck, Dong Hyun Kim, Paul W. Erhardt, Brian J. Kress
  • Patent number: 11459322
    Abstract: The present disclosure relates to indole compounds and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer.
    Type: Grant
    Filed: November 19, 2018
    Date of Patent: October 4, 2022
    Assignee: ARIAGEN, INC.
    Inventors: Peter Colabuono, Graham Johnson, David Douglas Manning, Mark Allan Wolf
  • Patent number: 11427576
    Abstract: The present disclosure relates to indole compounds and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer.
    Type: Grant
    Filed: February 18, 2021
    Date of Patent: August 30, 2022
    Assignee: ARIAGEN, INC.
    Inventors: Peter Colabuono, Graham Johnson, David Douglas Manning, Mark Allan Wolf
  • Patent number: 11390621
    Abstract: The present disclosure relates to indole compounds and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer.
    Type: Grant
    Filed: February 18, 2021
    Date of Patent: July 19, 2022
    Assignee: ARIAGEN, INC.
    Inventors: Graham Johnson, Peter Colabuono, Paul Gerard Pearson, David Douglas Manning
  • Patent number: 11370787
    Abstract: Disclosed herein are embodiments of a pyrazole compound according to formula I. Compositions comprising the compound, and a method for making the composition also are disclosed. The composition may comprise a carrier, such as a polymer and/or the composition may be a spray-dried formulation. Also disclosed is a method for using the compound and/or composition. The compound and/or composition may be useful to inhibit an IRAK protein and/or to ameliorate, treat and/or prevent an IRAK-associated disease or condition in a subject.
    Type: Grant
    Filed: August 28, 2020
    Date of Patent: June 28, 2022
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Lu Chou, Matt Duan, Ihab Darwish, Simon Shaw, Somasekhar Bhamidipati, Vanessa Taylor, Yan Chen, Dazhong Fan, Zhushou Luo
  • Patent number: 11266646
    Abstract: The present application relates to the use of bicyclic-substituted uracil derivatives, alone or in combinations with other active ingredients for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of inflammatory and fibrotic disorders, for the treatment of endometriosis, of endometriosis-associated fibrosis, of adenomyosis and of pain associated with an endometriosis disorder and also of postoperative peritoneal fibrosis and adhesion formation.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: March 8, 2022
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Michaele Peters, Markus Koch, Thomas Zollner
  • Patent number: 11261179
    Abstract: Compounds having the general structure A-L-B are presented wherein A and B are independently an E3 ubiquitin ligase protein binding ligand compound of formula 1A or 1B. Pharmaceutical compositions comprising these compounds and methods of use are also presented.
    Type: Grant
    Filed: April 13, 2018
    Date of Patent: March 1, 2022
    Assignee: University of Dundee
    Inventors: Alessio Ciulli, Chiara Maniaci, Scott J. Hughes, Andrea Testa
  • Patent number: 11236058
    Abstract: The inventive subject matter provides compounds, compositions and methods for lowering serum acid (sUA) for the treatment of gout, and having reduced liver toxicity, associated with CYP2C9 metabolic pathway.
    Type: Grant
    Filed: November 14, 2019
    Date of Patent: February 1, 2022
    Assignee: ARTHROSI THERAPEUTICS, INC.
    Inventors: Shunqi Yan, Li-Tain Yeh, Robert Orr
  • Patent number: 11191755
    Abstract: The invention provides compositions and methods for providing a cardioprotective effect in a subject. Specifically, the invention provides compositions and methods for treating cardiovascular ailments, for example, ischemia/reperfusion (I/R) injury, cardiac arrhythmias, oxidative stress, or cardiac failure by administering a retinoic acid receptor-beta (RAR?) agonist.
    Type: Grant
    Filed: June 14, 2018
    Date of Patent: December 7, 2021
    Assignee: Cornell University
    Inventors: Lorraine J Gudas, Xiao-Han Tang
  • Patent number: 11186555
    Abstract: The present disclosure provides pharmaceutical compositions comprising Gamma-glutamyl cycle inhibitors (GGCI) and certain pharmaceutically acceptable salts thereof, and methods of use.
    Type: Grant
    Filed: June 17, 2019
    Date of Patent: November 30, 2021
    Assignee: CANCER RESEARCH TECHNOLOGY, LLC
    Inventors: David Rubin, Eyal Rubin
  • Patent number: 11160769
    Abstract: This invention relates to pharmaceutical compositions and methods for treating (including managing) or preventing metabolic syndrome related conditions using one or more RAR e.g., RAR agonists. Such conditions include, but are not limited to, diseases in pancreas, liver, kidney, testes, muscle, or adipose tissue, as well as other organs that are associated with high fat diet and/or vitamin A deficiency, as well as other conditions associated with abnormal level of triglyceride, cholesterol and/or glucose.
    Type: Grant
    Filed: January 16, 2015
    Date of Patent: November 2, 2021
    Assignee: Cornell University
    Inventors: Lorraine J Gudas, Yannick Benoit, Ronald Perez, Xiao-Han Tang, Steven Trasino
  • Patent number: 11161839
    Abstract: The present invention relates to compounds of formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: Formula I wherein X1, X2, X3, R1, R2, R3, R4 and R5 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.
    Type: Grant
    Filed: May 25, 2018
    Date of Patent: November 2, 2021
    Assignees: The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology Limited
    Inventors: Benjamin Richard Bellenie, Kwai Ming Jack Cheung, Owen Alexander Davis, Swen Hoelder, Rosemary Huckvale, Matthew Garth Lloyd
  • 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: 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: 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: 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