Chalcogen Or Nitrogen Bonded Directly To The Imidazole Ring By Nonionic Bonding Patents (Class 514/398)
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Patent number: 12037339Abstract: The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of GLP-1 receptor, a pharmaceutical composition comprising a compound of Formula (I), and a method of treating or preventing a disease in which GLP-1 receptor plays a role.Type: GrantFiled: July 20, 2021Date of Patent: July 16, 2024Assignee: Eccogene Inc.Inventors: Zaifang Ren, Xuefeng Sun, Jingye Zhou
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Patent number: 11957737Abstract: Methods of treating or preventing microbial infection in a subject in need of treatment by administering a therapeutically effective amount of ergothioneine, or functional analog, or prodrug, or salt thereof. Ergothioneine may be advantageously administered in conjunction with lactoferrin.Type: GrantFiled: June 30, 2022Date of Patent: April 16, 2024Assignees: COLORADO SEMINARY, OWNER AND OPERATOR OF UNIVERSITY OF DENVER, THE REGENTS OF THE UNIVERSITY OF COLORADOInventors: John Repine, Amani Alhalwani
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Patent number: 11584751Abstract: The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of GLP-1 receptor, a pharmaceutical composition comprising a compound of Formula (I), and a method of treating or preventing a disease in which GLP-1 receptor plays a role.Type: GrantFiled: November 2, 2021Date of Patent: February 21, 2023Assignee: Eccogene (Shanghai) Co., Ltd.Inventors: Zaifang Ren, Xuefeng Sun, Jingye Zhou, Qing Xu
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Patent number: 11541035Abstract: The present disclosure provides oral pharmaceutical compositions comprising: 1) metronidazole or a pharmaceutically acceptable salt thereof; and magnesium aluminum silicate; or 2) metronidazole or a pharmaceutically acceptable salt thereof; magnesium aluminum silicate; and a flavoring agent. Methods of treating infection utilizing the oral pharmaceutical compositions are also provided.Type: GrantFiled: January 16, 2019Date of Patent: January 3, 2023Assignee: Appili Therapeutics Inc.Inventors: Bernard J. Guarino, Jr., Jamie L. Doran, Zorana Radovic, Kevin Sullivan
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Patent number: 11400076Abstract: The object of the present invention is to provide a novel pharmaceutical for suppressing cancer stem cells. In the present invention, a mitochondria inhibitor comprising a 2-nitroimidazole derivative is applied to the cancer stem cell as an active ingredient.Type: GrantFiled: October 2, 2018Date of Patent: August 2, 2022Assignees: KEIO UNIVERSITY, Sun Pharma Japan LimitedInventors: Hideyuki Saya, Oltea Sampetrean, Naoyoshi Koike, Nobuo Kubota
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Patent number: 11207283Abstract: Disclosed are methods, compounds, and compositions for treating infection by an Apicomplexan parasite that include administering a compound that selectively inactivates ornithine aminotransferase of the Apicomplexan parasite. Specifically, the methods, compounds, compounds may be utilized for treating infection by Toxoplasma gondii and toxoplasmosis and for treating infection by Plasmodium falciparum and malaria. The compounds disclosed herein are observed to selectively inactivate Toxoplasma gondii ornithine aminotransferase (TgOAT) relative to human OAT and relative to human ?-aminobutyric aminotransferase (GABA-AT).Type: GrantFiled: March 31, 2020Date of Patent: December 28, 2021Assignees: Northwestern University, The University of ChicagoInventors: Richard B. Silverman, Hoang V. Le, Rima L. McLeod, Dustin D. Hawker
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Patent number: 11013710Abstract: The present invention discloses herein a synergistic composition(s) of bioactive agents for optimizing cellular health. Particularly, a synergistic bioactive composition for optimizing cellular health, wherein the composition comprising therapeutic blend of betaine of thiol histidine and sirtuin activator(s) or salts thereof present in the ratio of 1:0.5 to 1:90, along with pharmaceutically acceptable excipients. In another embodiment, the invention discloses novel synergistic nutritional composition comprising synergistic combination of bioactives L-ergothioneine and nicotinamide mononucleotide chloride present in the ratio ranges from 1:1 to 1:80. The present invention provides promising and effective nutritional composition for improving cellular health by regulating expression of transcriptional factor, pro-inflammatory cytokines, and reducing cell apoptosis, ROS level and DNA damage in the cell.Type: GrantFiled: December 5, 2019Date of Patent: May 25, 2021Assignee: CELAGENEX RESEARCH (INDIA) PVT. LTD.Inventors: Dhiraj Dhamane, Rajendra Prasad Tongra
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Patent number: 10933030Abstract: The present invention relates to a composition comprising paeonol of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient for inhibiting angiogenesis, or for enhancing radiosensitization. The present invention also relates to novel use of paeonol of formula (I) or a pharmaceutically acceptable salt thereof for the manufacture of a composition for inhibiting angiogenesis, or for the manufacture of a composition for enhancing radiosensitization. Also, the present invention relates to a method for inhibiting angiogenesis which comprises administrating to a subject in need thereof an effective amount of paeonol of formula (I) or a pharmaceutically acceptable salt thereof, or a method for enhancing radiosensitization which comprises administrating an effective amount of paeonol of formula (I) or pharmaceutically acceptable salts thereof to a subject in need of radiotherapy.Type: GrantFiled: May 4, 2006Date of Patent: March 2, 2021Assignee: ANGIOLAB, INC.Inventors: Min-Young Kim, Hee-Suk Lee, Ki-Hwan Bae, Yeon-Sook Yun, Jie-Young Song, Young-Soo Han
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Patent number: 10653672Abstract: The invention provides a novel myogenesis promotor, a novel muscle atrophy inhibitor, a novel composition or a novel TAZ activator. The myogenesis promotor, the muscle atrophy inhibitor, the composition and the TAZ activator include a composition represented by the following Formula (I) as an active ingredient. In Formula (I), R1 represents a hydrogen atom or an alkyl group; R2 represents an aryl group, a heterocyclic group, an alkyl group or the like; R3 represents —NR5R6 or —N?C—R7; each of R5 and R6 independently represents a hydrogen atom, an alkyl group or the like; R7 represents —NR10R11, an aryl group or a heterocyclic group; R8 represents a hydrogen atom, an alkyl group or the like; R9 represents a hydrogen atom, an alkyl group or the like; each of R10 and R11 independently represents a hydrogen atom, an alkyl group or the like; R4 represents a cyano group or —C(?O)R12; and R12 represents an aryl group, a heterocyclic group, an alkyl group or the like.Type: GrantFiled: February 6, 2015Date of Patent: May 19, 2020Assignee: National University Corporation Tokyo Medical and Dental UniversityInventors: Yutaka Hata, Hiroyuki Kagechika, Kentaro Nakagawa, Shigeru Ito
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Patent number: 10596155Abstract: The present disclosure provides mucoadhesive aqueous-based gel formulations of metronidazole useful for a variety of purposes including intravaginal application as a therapeutic approach towards the treatment of individuals suffering from and/or diagnosed with bacterial vaginosis.Type: GrantFiled: January 14, 2019Date of Patent: March 24, 2020Assignee: CHEMO RESEARCH, S.L.Inventors: Michael T. Nordsiek, Kodumudi S. Balaji
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Patent number: 10487072Abstract: The present invention relates to a novel imidazole compound or a pharmaceutically acceptable salt thereof having a melanocortin receptor agonistic activity, and medical use thereof. The present invention relates to an imidazole compound represented by general formula [I] [wherein: Ring A represents an optionally substituted aryl group or the like; R1 represents a hydrogen atom, an optionally substituted alkyl group, or the like; R2 represents a hydrogen atom, a halogen atom, or the like; and R3 represents an optionally substituted alkyl group] or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 25, 2016Date of Patent: November 26, 2019Assignee: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Atsushi Sato, Ritsuo Imashiro, Hidekazu Tsujishima, Kouichi Tanimoto, Yasuo Yamamoto, Tetsu Nakane, Chihiro Toshikawa
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Patent number: 10045965Abstract: Disclosed are gel compositions suitable for the topical administration of an active compound having poor solubility and skin penetration, for example, of a COX-2 inhibitor compounds, processes of preparation thereof and methods of use thereof for the treatment of indications treatable by the active compound.Type: GrantFiled: April 9, 2015Date of Patent: August 14, 2018Assignee: EGIS Pharmaceuticals PLCInventors: Endre Mikulásik, Tamás Spaits, Ágota Szakályné Sinka
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Patent number: 9830554Abstract: Audio sensors collaborate for geo-location and tracking of multiple users. Different users can be independently geo-located and tracked within the AI environment. Location is determined from two or more AI clients of known locations that detect an event such as a human voice command to connect a call with a specific user. Responsive to classification of the event in view of the estimated location, a command for an AI action, such as connecting a call between users, is received for a response to the event at the AI clients that detected the event, or others.Type: GrantFiled: November 23, 2016Date of Patent: November 28, 2017Assignee: Lumin, LLCInventors: Nima Lahijani Shams, Suhas Maheshaiah
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Patent number: 9818061Abstract: Audio sensors collaborate for geo-location and tracking of multiple users. Different users can be independently geo-located and tracked within the AI environment. Location is determined from two or more AI clients of known locations that detect an event such as a human voice command to connect a call with a specific user. Responsive to classification of the event in view of the estimated location, a command for an AI action, such as connecting a call between users, is received for a response to the event at the AI clients that detected the event, or others.Type: GrantFiled: September 15, 2016Date of Patent: November 14, 2017Assignee: Lumin, LLCInventors: Nima Lahijani Shams, Suhas Maheshaiah
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Patent number: 9710753Abstract: An artificial intelligence (AI) system leverages collaboration of multiple audio sensors for geo-location of an event. Location information is stored for each of the plurality of geographically-dispersed AI clients. Each of the AI clients can include an audio sensor, a network controller, and a feedback mechanism (e.g., a speaker or an LED) within a common enclosure. Responsive to detection of an event (e.g., involving a human, machine, or ambient condition) at two or more of the plurality of geographically-dispersed AI clients, audio event data is centrally received from audio sensors of the two or more of the plurality of geographically-dispersed AI sensors. A location is estimated based on the location information and the audio event data. Responsive to classification of the event in view of the estimated location, a command is received for a response to the event at the AI clients that detected the event, or others.Type: GrantFiled: October 22, 2014Date of Patent: July 18, 2017Assignee: Lumin, LLCInventors: Nima Lahijani Shams, Vinay Venkatesh Malekal, Narges Banou Nourshahi
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Patent number: 9649298Abstract: The present invention provides a substance comprising a preparation of at least one chemotherapeutic or cytotoxic substance for the use in treatment of a disease of a mammalian patient, especially in the treatment of cancer. The invention suggests a symbiotic or synergistic combination of radiotherapy and chemotherapeutic or cytotoxic drug delivery.Type: GrantFiled: June 4, 2014Date of Patent: May 16, 2017Assignees: Fumedica AG, Universität BernInventors: Valentin Djonov, Beat Steger
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Patent number: 9511053Abstract: Therapeutic compositions capable of removing excess nitric oxide are provided. The therapeutic compositions include nitronyl nitroxide monoradicals, B12 derivatives, flavonoid derivatives, the like and combinations thereof. The therapeutic compositions can be utilized in a number of suitable applications, such as to prevent or treat intradialytic hypotension during dialysis.Type: GrantFiled: December 30, 2015Date of Patent: December 6, 2016Assignees: Baxter International Inc., Baxter Healthcare S.A.Inventors: Sujatha Karoor, Ton That Hai, Cong Jiang, Paul Sanders, Cliff Holmes
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Patent number: 9481652Abstract: The present invention provides a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, which comprises the solid preparation and an environment-controlling agent packaged together. The packaged product of present invention is useful as a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, with which discoloration of the solid preparation is suppressed, and superior storage stability of the solid preparation is obtained.Type: GrantFiled: June 24, 2015Date of Patent: November 1, 2016Assignee: FUJIFILM CorporationInventor: Shumma Nakano
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Patent number: 9433680Abstract: The present invention relates to improved topical gel compositions comprising an active agent, and uses thereof.Type: GrantFiled: July 12, 2013Date of Patent: September 6, 2016Assignee: MERZ PHARMACEUTICALS, LLCInventors: Bhushan Hardas, Donna Dalton, Petra Scheppler, Anja Hensche, Peter Boderke
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Patent number: 9388141Abstract: The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor.Type: GrantFiled: March 14, 2014Date of Patent: July 12, 2016Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KGInventors: Andreas Haupt, Jürgen Dinges, Liliane Unger, Karsten Wicke, Robert Van Waterschoot, Karla Drescher, Ana Relo
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Patent number: 9273008Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: March 19, 2015Date of Patent: March 1, 2016Assignee: Theravance Biopharma R&D IP, LLCInventors: Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell, Brooke Olson
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Patent number: 9249105Abstract: The invention provides crystalline salt forms of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension.Type: GrantFiled: June 27, 2014Date of Patent: February 2, 2016Assignee: Theravance Biopharma R&D IP, LLCInventors: Paul R. Fatheree, Venkat R. Thalladi
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Publication number: 20150148393Abstract: The invention relates to a cosmetic and/or pharmaceutical composition in combination with suitable carriers for topical use, comprising a mixture consisting of methyl sulfonyl methane and at least one compound belonging to the class of 4-alkyl cyclohexanols, which is useful in the treatment of various inflammatory conditions such as rosacea. The composition can act to simultaneously hinder both the release of chemical mediators which are up-regulated in rosacea and their action of causing the activation of TRPV receptors. The composition can reduce the effect of ultraviolet radiations on a skin already affected by an inflammatory process, and particularly, it can reduce the erythema induced by ultraviolet radiations on a skin already affected by an inflammatory process.Type: ApplicationFiled: June 4, 2013Publication date: May 28, 2015Applicant: GENERAL TOPICS S.R.L.Inventor: Gianfranco De Paoli Ambrosi
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Publication number: 20150141476Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, rosacea.Type: ApplicationFiled: January 23, 2015Publication date: May 21, 2015Inventors: Pedro Cuevas Sànchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Gorman, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
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Publication number: 20150133366Abstract: 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: ApplicationFiled: November 12, 2014Publication date: May 14, 2015Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Richard L. Guerrant, Cirle Alcantara Warren, John Hudson Moore, II, Edward van Opstal
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Publication number: 20150133471Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.Type: ApplicationFiled: September 15, 2014Publication date: May 14, 2015Inventors: Gabor Csjernyik, Sofia Karlstrom, Annika Kers, Karin Kolmodin, Martin Nylof, Liselotte Ohberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Soderman, Britt-Marie Swahn, Stefan Von Berg
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Publication number: 20150133518Abstract: The invention provides crystalline salt forms of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension.Type: ApplicationFiled: June 27, 2014Publication date: May 14, 2015Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Paul R. Fatheree, Venkat R. Thalladi
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Patent number: 9012485Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: January 9, 2014Date of Patent: April 21, 2015Assignee: Theravance Biopharma R&D IP, LLCInventors: Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell, Brooke Olson
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Patent number: 9005643Abstract: Disclosure is provided for imidazole-phenyl derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.Type: GrantFiled: April 3, 2009Date of Patent: April 14, 2015Assignee: North Carolina State UniversityInventors: Christian Melander, Justin J. Richards, Cynthia Bunders
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Publication number: 20150093435Abstract: Compositions, and methods of use thereof, are provided for the treatment of painful neuropathy by local or topical delivery of compounds that interact with ?-adrenergic receptors, especially an alpha2 adrenergic agonist such as clonidine, to the entire painful area such that the need for systemic dosing is minimized. The compounds are delivered to or adjacent to painful areas in patients with painful length dependent neuropathy, and other neuropathies that affect the pain signaling fibers in the skin. A preferred compound for the treatment of patients with length dependent neuropathy is clonidine applied in a transdermal patch, gel, ointment, lotion, liposomal formulation, cream, or emulsion, wherein the concentration is sufficient to provide an effective dose in the painful area or immediately adjacent areas.Type: ApplicationFiled: December 9, 2014Publication date: April 2, 2015Inventor: James N. Campbell
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Publication number: 20150093338Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.Type: ApplicationFiled: October 8, 2014Publication date: April 2, 2015Inventor: Michael Farber
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Patent number: 8993584Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as procymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.Type: GrantFiled: July 21, 2011Date of Patent: March 31, 2015Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Koji Sugimoto, Hiroyuki Hayashi
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Publication number: 20150079116Abstract: NK cell licensing predisposes patients to chronic inflammatory disease. Methods and kits to diagnose and treat chronic inflammatory disease based on genetic haplotype and cytokine profile are described herein.Type: ApplicationFiled: April 11, 2013Publication date: March 19, 2015Inventors: Jonathan Braun, Lin Lin
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Patent number: 8980920Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.Type: GrantFiled: May 28, 2010Date of Patent: March 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Patent number: 8980932Abstract: The present invention concerns novel carbonic anhydrase IX inhibitors comprising a nitroimidazole moiety and their use in therapy of hypoxic conditions, in particular cancer treatment, especially chemotherapy and radiotherapy. The compounds of the invention have an increased specificity for the carbonic anhydrase IX enzyme compared to the art. The present invention relates to novel nitroimidazole derivates represented by formula (1).Type: GrantFiled: December 21, 2011Date of Patent: March 17, 2015Assignees: Stichting Maastricht Radiation Oncology “Maastro-Clinic”, Université Montpellier 2 Sciences et TechniquesInventors: Philippe Lambin, Jean-Yves Winum, Claudiu Supuran
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Patent number: 8975411Abstract: An object of the present invention is to provide a pharmaceutical agent useful for treating and preventing neurological disease, having satisfactory solubility and oxidative stress-mediated cell death suppressive activity as well as capable of exhibiting excellent blood-brain barrier permeability. The present invention is directed to an acylaminoimidazole derivative represented by general formula (I) or a salt thereof, and a pharmaceutical and a therapeutic or preventive agent for neurological disease containing the same, as an active ingredient.Type: GrantFiled: July 15, 2011Date of Patent: March 10, 2015Assignees: Neugen Pharma Inc., Wakunaga Pharmaceutical Co., Ltd.Inventors: Joh-E Ikeda, Noriaki Hirayama, Satoshi Inoue, Kazunori Tanaka, Takuya Kanno
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Publication number: 20150065543Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: October 23, 2014Publication date: March 5, 2015Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Patent number: 8962668Abstract: Compositions, and methods of use thereof, are provided for the treatment of painful neuropathy by local or topical delivery of compounds that interact with ?-adrenergic receptors, especially an alpha2 adrenergic agonist such as clonidine, to the entire painful area such that the need for systemic dosing is minimized. The compounds are delivered to or adjacent to painful areas in patients with painful length dependent neuropathy, and other neuropathies that affect the pain signaling fibers in the skin. A preferred compound for the treatment of patients with length dependent neuropathy is clonidine applied in a transdermal patch, gel, ointment, lotion, liposomal formulation, cream, or emulsion, wherein the concentration is sufficient to provide an effective dose in the painful area or immediately adjacent areas.Type: GrantFiled: February 21, 2011Date of Patent: February 24, 2015Assignee: Arcion Therapeutics, Inc.Inventor: James N. Campbell
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Patent number: 8946275Abstract: Cancer can be treated by administration of a hypoxia-activated prodrug, such as TH-302, alone or in combination with other anticancer agents and/or radiation therapy. In combination therapy, the hypoxia-activated prodrug and another anti-cancer agent or radiation therapy may be administered within the same 24-hour period, and administration of the hypoxia-activated prodrug may be completed prior to beginning administration of the other anticancer agent or radiation therapy.Type: GrantFiled: October 21, 2009Date of Patent: February 3, 2015Assignee: Threshold Pharmaceuticals, Inc.Inventors: Stewart Kroll, Mark Matteucci, Charles P. Hart, Jian-Xin Duan, Karen Curd
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Patent number: 8946276Abstract: The present disclosure provides mucoadhesive aqueous-based gel formulations of metronidazole useful for a variety of purposes, including intravaginal application as a therapeutic approach towards the treatment of individuals suffering from and/or diagnosed with bacterial vaginosis.Type: GrantFiled: June 28, 2012Date of Patent: February 3, 2015Assignee: Watson Laboratories, Inc.Inventors: Michael T. Nordsiek, Kodumudi S. Balaji
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Publication number: 20150023955Abstract: The present invention discloses novel agents and methods for diagnosis and treatment of melanoma. Also disclosed are related arrays, kits, and screening methods.Type: ApplicationFiled: September 15, 2014Publication date: January 22, 2015Applicant: THE ROCKEFELLER UNIVERSITYInventors: Sohail Tavazoie, Nora Pencheva
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Publication number: 20150025094Abstract: The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of —S—, —S—S—, —S—(CH2)n—, —NH—, —NH—(CH2)n—, —O—, —S02-, arylene, heteroarylene; R1 is selected from the group consisting of straight or branched C4-C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5-C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or heteroaromatic ring, each optionally substituted with at least one group selected from —COOH, —NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 carboxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, halType: ApplicationFiled: August 1, 2012Publication date: January 22, 2015Applicants: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD., DIAB R&d 1, BAR-IIan UniversityInventors: Shlomo Sasson, Erol Cerasi, Arie Lev Gruzman, Ella Meltzer-Mats
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Patent number: 8933245Abstract: Compositions comprising ergothioneine and a trimethylamine absorber are provided. Also provided are methods for preventing, reducing or minimizing the fishy, amine odor, due to trimethylamine, that is associated with the processing and/or storage of a preparation containing ergothioneine, by combining with the ergothioneine, during processing or prior to storage, a trimethylamine absorber in an amount sufficient to prevent the detection of any trimethylamine odor by the human nose. A method is further provided for ameliorating the methylamine odor associated with an aqueous ergothioneine-containing preparation after it has developed a fishy trimethylamine odor.Type: GrantFiled: November 8, 2012Date of Patent: January 13, 2015Assignee: ELC Management LLCInventor: Daniel B. Yarosh
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Patent number: 8921406Abstract: The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.Type: GrantFiled: August 21, 2006Date of Patent: December 30, 2014Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Andreas Haupt, Francisco Javier Garcia-Ladona, Alfred Hahn
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Publication number: 20140378466Abstract: This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Applicant: ARDEA BIOSCIENCESInventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoul, Zhi Hong
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Publication number: 20140378520Abstract: The invention provides (among other things) small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer.Type: ApplicationFiled: September 4, 2014Publication date: December 25, 2014Inventors: Zhongxu Ren, Jennifer Riggs-Sauthier, Michael D. Bentley
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Patent number: 8912225Abstract: The present invention provides methods for inhibiting VEGF production or secretion in a subject comprising administering to the subject an effective amount of a compound of Formula I. The invention also provides methods for the treatment or prevention of conditions associated with abnormal levels of VEGF production or secretion.Type: GrantFiled: August 31, 2005Date of Patent: December 16, 2014Assignee: Pitney Pharmaceuticals Pty LimitedInventors: David L. Morris, Mohammad H. Pourgholami
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Publication number: 20140364474Abstract: Disclosure is provided for 1,4,5-substituted amino imidazole compounds useful to control microbial growth, compositions including these compounds, devices including these compounds, and methods of using the same.Type: ApplicationFiled: August 21, 2014Publication date: December 11, 2014Inventors: Christian Melander, Zhaoming Su, Lingling Peng
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Publication number: 20140363479Abstract: There is disclosed herein a composition for treating extracellular parasitic infections, the composition comprising one or more of the following combinations: at least one quinolone or fluoroquinolone together with at least one tetracycline, iodoquinol, an azole or imidazole; or at least two agents selected from the group consisting of iodoquinol, thiazolidones, tetracycline, nitroimidazoles, cotrimoxazole and diloxanide furoate.Type: ApplicationFiled: August 21, 2014Publication date: December 11, 2014Inventors: Thomas Julius BORODY, Soledad CARSULA
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Patent number: 8889672Abstract: The invention provides a method of inhibiting atypical protein kinase C (aPKC) comprising contacting an aPKC with a compound having a structure selected from the group consisting of structural formulas (I) to (IX). The invention further provides a method of inhibiting or reducing vascular permeability. The method comprising administering to a subject a composition comprising an amount of a compound having a structure selected from the group consisting of structural formulas (I) to (IX) effective to inhibit or reduce vascular permeability. A method of treating or preventing a disease or disorder characterized by abnormal vascular permeability, a method of inhibiting angiogenesis, a method of inhibiting cancer cell proliferation, a formulation, and a method of preparing a formulation also are provided.Type: GrantFiled: April 27, 2012Date of Patent: November 18, 2014Assignees: The Regents of The University of Michigan, The Penn State Research FoundationInventors: David A. Antonetti, Paul Titchenell