Pyrazoles Patents (Class 514/406)
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Patent number: 10562858Abstract: A crystal form of 2-(3,5-dimethyl-1H-pyrazol-1-yl)-5-methylphenol which is stable and has high purity for preservation, industrial manufacturing, and circulation, and process for providing the same by using a boron compound.Type: GrantFiled: August 12, 2015Date of Patent: February 18, 2020Assignee: MEIJI SEIKA PHARMA CO., LTD.Inventors: Toshiro Sasaki, Takahiro Imai, Kenichiro Mori, Makoto Ohyama, Takashi Watanabe
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Patent number: 10543193Abstract: The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein.Type: GrantFiled: August 7, 2018Date of Patent: January 28, 2020Assignee: ARENA PHARMACEUTICALS, INC.Inventors: Marlon Carlos, Weitong Dong, Mark Macias, Suzanne Michiko Sato, Lee Alani Selvey
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Patent number: 10525144Abstract: The present invention provides compounds and a method for the targeted delivery of Mitochondrial Angiotensin Receptor Blockers (MARBs) to the Mitochondrial Angiotensin System (MAS) for the treatment of diseases caused by angiotensin-related mitochondrial dysfunction. The compounds include a mitochondrial targeting signal, a residue of a drug molecule, a functional moiety, and a scaffold moiety.Type: GrantFiled: November 10, 2015Date of Patent: January 7, 2020Assignee: THE JOHNS HOPKINS UNIVERSITYInventors: Honggang Cui, Peter M. Abadir, Jeremy D. Walston, Andrew G. Cheetham
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Patent number: 10519137Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: November 13, 2017Date of Patent: December 31, 2019Assignee: ASTEX THERAPEUTICS LTDInventors: Gordon Saxty, Christopher William Murray, Valerio Berdini, Gilbert Ebai Besong, Steven John Woodhead, Michael Reader, Laurence Anne Mevellec, Patrick René Angibaud, Eddy Jean Edgard Freyne, Timothy Pietro Suren Perera, Berthold Wroblowski, Alexandra Papanikos, Olivier Alexis Georges Querolle, Isabelle Noëlle Constance Pilatte, Pascal Ghislain André Bonnet, Werner Constant Johan Embrechts, Rhalid Akkari, Lieven Meerpoel
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Patent number: 10513497Abstract: Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of Formula I and Formula Ib as well as crystalline types of Formula IX (AG-10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification.Type: GrantFiled: February 16, 2018Date of Patent: December 24, 2019Assignee: EIDOS THERAPEUTICS, INC.Inventors: Pooran Chand, Yogesh Kumar Gupta, Rakesh Kumar Kumawat, Mamoun Alhamadsheh, Robert Zamboni
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Patent number: 10493089Abstract: A solid composition comprising sofosbuvir and at least one pharmaceutically acceptable matrix compound wherein at least 99 weight-% of the sofosbuvir comprised in the composition are present in amorphous form, at least 99 weight-% of the solid composition consist of the sofosbuvir and the at least one matrix compound, and wherein the solid composition contains the sofosbuvir in an amount of at least 55 weight-% based on the combined weight of the sofosbuvir and the at least one matrix compound.Type: GrantFiled: April 2, 2015Date of Patent: December 3, 2019Assignee: Sandoz AGInventor: Nolwenn Martin
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Patent number: 10472328Abstract: Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: GrantFiled: December 19, 2018Date of Patent: November 12, 2019Assignee: TOLERO PHARMACEUTICALS, INC.Inventors: Koc-Kan Ho, Yong Xu, Michael David Saunders, Xiaohui Liu, Scott Albert Pearce, Kevin Bret Wright, Jason Marc Foulks, Kenneth Mark Parnell, Steven Brian Kanner, David Lee Vollmer, Jihua Liu
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Patent number: 10471079Abstract: Combinations of certain analgesics with COX-II inhibitors, related pharmaceutical compositions, including advantageous galenical forms containing these combinations, and the use of such combinations in methods of treatment, in particular for the treatment of pain.Type: GrantFiled: June 7, 2016Date of Patent: November 12, 2019Assignee: GRUENENTHAL GMBHInventors: Klaus Schiene, Guenter Haase, Babette-Yvonne Koegel, Elmar Friderichs, Ulrich Jahnel
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Patent number: 10449253Abstract: A method of delivering or sequestering anesthetic agents by adsorption of such agents by porous partially fluorinated compounds which display high weight adsorption capacities. Such compounds have a non-covalent organic framework with a central ring, such as hexa, tetra, tri or di substituted benzenes which may be substituted or unsubstituted with alternating electron poor and electron rich groups such as tetra-, tri-, or di-fluorobenzenes, oligocyanobenzenes, oligochlorobenzene, and benzene, pirydone, triazole, pyrazole, pyridine, and substituted benzenes so that the compound forms a porous supramolecular structure; and adsorbs the anesthetic agent within the pores of a the compound.Type: GrantFiled: October 3, 2018Date of Patent: October 22, 2019Assignee: UNIVERSITY OF HOUSTON SYSTEMInventors: Ognjen Miljanic, Teng-Hao Chen, Watchareeya Kaveevivitchai
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Patent number: 10415093Abstract: Methods for diagnosing or monitoring endometriosis in a mammal are provided. The methods include the steps of determining the expression levels of BDNF and its receptor, Ntrk2, in a biological sample from the mammal, and determining that the mammal has endometriosis when the BDNF and Ntrk2 expression levels in the sample are elevated.Type: GrantFiled: April 8, 2016Date of Patent: September 17, 2019Assignees: MCMASTER UNIVERSITY, THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Warren Foster, Nicholas Leyland, Jocelyne Wessels, Sanjay Agarwal
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Patent number: 10385051Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: GrantFiled: October 22, 2018Date of Patent: August 20, 2019Assignee: CELGENE QUANTICEL RESEARCH, INC.Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
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Patent number: 10376527Abstract: The present invention relates to a stable oral liquid pharmaceutical composition of celecoxib or its pharmaceutically acceptable salts thereof. The celecoxib present in the compositions as described herein do not show any precipitation when subjected in Fasted-State Simulated Gastric Fluid (FaSSGF) at pH 2.0, temperature of 37° C.±0.5° C. and under stirring at a speed of 50 rpm at least for 60 minutes. It also relates to the process of preparing and method of using said composition of celecoxib.Type: GrantFiled: March 15, 2018Date of Patent: August 13, 2019Assignee: DR. REDDY'S LABORATORIES LTD.Inventors: Ankit Baheti, Bijay Kumar Padhi, Supritha Vakada, Rajeev Singh Raghuvanshi
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Patent number: 10314841Abstract: The present invention provides compounds of Formula (II) for the treatment of cancer, rheumatoid arthritis and other diseases.Type: GrantFiled: January 9, 2015Date of Patent: June 11, 2019Assignee: Merck Patent GmbHInventors: Catherine Jorand-Lebrun, Reinaldo Jones
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Pyrazole derivatives as TNIK, IKK? and TBK1 inhibitor and pharmaceutical composition comprising same
Patent number: 10294207Abstract: Provided is pyrazole derivatives as a TNIK (Traf2- and NCK-interacting kinase), IKK? (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the pyrazole derivative according to the present invention effectively inhibits TNIK, IKK? and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.Type: GrantFiled: March 29, 2016Date of Patent: May 21, 2019Assignee: GREEN CROSS CORPORATIONInventors: Soongyu Choi, Kisoo Park, Hee Jeong Seo, Eun-Jung Park, Younggyu Kong, Ickhwan Son, Sang-ho Ma, Kwang-Seop Song, Min Ju Kim, So Ok Park, Man-Young Cha, Mi-Soon Kim, Sang Mi Kang, Dong Hyuk Jang, Jangwon Hong -
Patent number: 10287298Abstract: The present invention concerns compounds of formula (I), enantiomers, mixture of enantiomers, diastereoisomers and mixture of diasteroisomers thereof formula (I): wherein at least one of W, X and Y is selected from the group consisting of —NR1R2; —NR3—(CH2)n—NR4R5; —O—(CH2)n—NR4R5; —NR3—(CH2)n—N?R6R7R8; and —O—(CH2)n—N?R6R7R8 and Z is a functional group capable of chelating iron salts. The present invention also concerns the compounds of formula (I) for use as a drug, in particular, in the treatment of cancer and malaria.Type: GrantFiled: September 14, 2015Date of Patent: May 14, 2019Assignees: Centre National de la Recherche Scientifique (CNRS), Institut National de la Sante et de la Recherche Medicale (INSERM), Universite Paris DescartesInventors: Maryam Mehrpour, Raphael Rodriguez, Antje Hienzsch, Mai Trang, Ahmed Hamai
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Patent number: 10251853Abstract: The present invention relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib.Type: GrantFiled: November 22, 2017Date of Patent: April 9, 2019Assignee: INNOVATIVE MED CONCEPTS, LLCInventor: William L. Pridgen
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Patent number: 10214492Abstract: Disclosed herein are compounds and compositions useful in the treatment of MCT4 mediated diseases, such as proliferative and inflammatory diseases, having the structure of Formula I: Methods of inhibition MCT4 activity in a human or animal subject are also provided.Type: GrantFiled: December 12, 2017Date of Patent: February 26, 2019Assignee: Vettore, LLCInventors: Kenneth Mark Parnell, John McCall, Donna Romero
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Patent number: 10174034Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: GrantFiled: February 19, 2015Date of Patent: January 8, 2019Assignee: RHIZEN PHARMACEUTICALS SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Kanthikiran V S Varansi, Gayatri Swaroop Merikapudi, Swaroop Kumar V. S. Vakkalanka
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Patent number: 10172959Abstract: A delivery system for active agents, and methods of making and using the systems, are provided. The delivery systems have (i) a ligand that is selective for an endogeneous plasma protein in the serum of a subject; and, (ii) a linker configured for operatively attaching the ligand covalently to an active agent to increase the half-life of the active agent in the serum.Type: GrantFiled: March 1, 2017Date of Patent: January 8, 2019Inventor: Mamoun M Alhamadsheh
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Patent number: 10165775Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.Type: GrantFiled: March 16, 2017Date of Patent: January 1, 2019Assignee: Dow AgroSciences LLCInventors: Noormohamed M. Niyaz, Negar Garizi, Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse, Asako Kubota, Paul R. LePlae, Jr., Daniel I. Knueppel, Christian T. Lowe, Dan Pernich, David A. Demeter, Timothy C. Johnson
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Patent number: 10149473Abstract: New aminoindanes amides are described, having general formula (I) the relative phytosanitary compositions and their use for the control of phytopathogenic fungi.Type: GrantFiled: September 21, 2017Date of Patent: December 11, 2018Assignee: STICHTING I-F PRODUCT COLLABORATIONInventors: Isabella Venturini, Matteo Santino Vazzola, Entela Sinani, Franco Pellacini, Lucio Filippini
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Patent number: 10130095Abstract: The present invention relates to novel compositions comprising certain pyrazolecarboxylic acid alkoxyamides according to formula (I) in combination with certain fungicides, to a process for preparing these compositions and to the use thereof as biologically active compositions, especially for the control of harmful microorganisms in plants and in the protection of materials and as plant growth regulators.Type: GrantFiled: February 17, 2015Date of Patent: November 20, 2018Assignee: BASF AGRO B.V.Inventors: Pierre-Yves Coqueron, Ulrike Wachendorff-Neumann, Sebastian Hoffmann, Philippe Desbordes, Pierre Cristau, Peter Dahmen
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Patent number: 10117935Abstract: A method of delivering or sequestering anesthetic agents by adsorption of such agents by porous partially fluorinated compounds which display high weight adsorption capacities.Type: GrantFiled: December 10, 2015Date of Patent: November 6, 2018Assignee: UNIVERSITY OF HOUSTON SYSTEMInventors: Ognjen Miljanic, Teng-Hao Chen, Watchareeya Kaveevivitchai
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Patent number: 10071075Abstract: The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein.Type: GrantFiled: August 21, 2017Date of Patent: September 11, 2018Assignee: Arena Pharmaceuticals, Inc.Inventors: Marlon Carlos, Weitong Dong, Mark Macias, Suzanne Michiko Sato, Lee Alani Selvey
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Patent number: 10067132Abstract: A diagnostic method for determining prognosis of a myocardial infarcted patient, wherein the amounts of FXIII protein are determined on the day of myocardial infarction (t0) and at least on the following three days (t1 to t3), wherein a lowering of FXIII amount on any one of t0 to t3 below a threshold value is indicative of an increased risk of poor prognosis.Type: GrantFiled: August 4, 2016Date of Patent: September 4, 2018Inventor: Donato Gemmati
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Patent number: 10047055Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of LXR-associated diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.Type: GrantFiled: September 4, 2014Date of Patent: August 14, 2018Assignee: Ralexar Therapeutics, Inc.Inventor: Raju Mohan
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Patent number: 10034860Abstract: Described herein are methods of treating locally advanced or metastatic estrogen receptor positive breast cancer.Type: GrantFiled: May 8, 2017Date of Patent: July 31, 2018Assignee: Genentech, Inc.Inventors: Edna Chow Maneval, Boa Tran H. Troung, Isan Chen, Jeffrey H. Hager, Debasish F. Roychowdhury
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Patent number: 10034846Abstract: The present invention relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib.Type: GrantFiled: May 17, 2017Date of Patent: July 31, 2018Assignee: INNOVATIVE MED CONCEPTS, LLCInventor: William L. Pridgen
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Patent number: 10022355Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor and their uses for the treatment of REM sleep behavior disorder.Type: GrantFiled: June 10, 2016Date of Patent: July 17, 2018Assignee: Axovant Sciences GmbHInventors: Lawrence Tim Friedhoff, Shankar Ramaswamy, Yandong Wen
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Patent number: 9974771Abstract: Compositions and methods for reducing the level of prions in a prion-infected cells or host by exposing prion infected cells, tissues and organs to AR-12 and the AR-12 analog AR-14 to reduce the prion level by at least about 90%.Type: GrantFiled: February 28, 2017Date of Patent: May 22, 2018Assignees: OHIO STATE INNOVATION FOUNDATION, UTI LIMITED PARTNERSHIPInventors: Hermann M. Schaetzl, Basant Abdulrahman, Sabine Gilch, Alexander Zukiwski, Stefan Proniuk
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Patent number: 9961897Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, X, R1, R1a and R2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: GrantFiled: August 15, 2014Date of Patent: May 8, 2018Assignee: E I DU PONT DE NEMOURS AND COMPANYInventors: Andrew Edmund Taggi, James Francis Bereznak
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Patent number: 9951023Abstract: A method for the preparation of compounds of formula (I), for example, N-methyl-3-difluoromethyl-5-fluorpyrazole aldehyde, starting from compounds of formula (II), for example, N-methyl-3-haloalkyl-5 chloropyrazole aldehyde, comprising simultaneous fluorination (one step process) of haloalkyl group in position 3 and replacing haloatom in position 5 by fluorine.Type: GrantFiled: September 4, 2014Date of Patent: April 24, 2018Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Norbert Lui, Sergii Pazenok
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Patent number: 9949990Abstract: The present invention relates to a stable oral liquid pharmaceutical composition of celecoxib or its pharmaceutically acceptable salts thereof. The celecoxib present in the compositions as described herein do not show any precipitation when subjected in Fasted-State Simulated Gastric Fluid (FaSSGF) at pH 2.0, temperature of 37° C.±0.5° C. and under stirring at a speed of 50 rpm at least for 60 minutes. It also relates to the process of preparing and method of using said composition of celecoxib.Type: GrantFiled: September 22, 2017Date of Patent: April 24, 2018Assignee: DR. REDDY'S LABORATORIES LTD.Inventors: Ankit Baheti, Bijay Kumar Padhi, Supritha Vakada, Rajeev Singh Raghuvanshi
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Patent number: 9907806Abstract: The invention relates to pharmaceutical compositions for emergency contraception, to the use of levonorgestrel in combination with COX inhibitors for the preparation of pharmaceutical compositions for the stated purpose, and to a method for preparing these pharmaceutical compositions.Type: GrantFiled: December 12, 2014Date of Patent: March 6, 2018Assignee: BAYER INTELLECTUAL PROPERTY, GmbHInventors: Bernhard Lindenthal, Rolf Schürmann, Sascha General
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Patent number: 9896476Abstract: The glycyrrhetic acid derivatives can include: The glycyrrhetic acid derivatives can be used to treat inflammation and/or ulcers.Type: GrantFiled: September 21, 2017Date of Patent: February 20, 2018Assignee: KING SAUD UNIVERSITYInventors: Abd El-Galil E. Amr, Mohamed A. Al-Omar, Nagy Mahmoud Hassan Khalifa
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Patent number: 9889145Abstract: Methods to treat infectious diseases are disclosed herein. Some embodiments of the invention include administration of one or more COX inhibitors (e.g., COX-1 or COX-2 inhibitors) to treat infectious diseases. Other embodiments of the invention include administration of one or more COX inhibitors (e.g., COX-1 or COX-2 inhibitors) and administration of one or more antibiotics to treat infectious diseases.Type: GrantFiled: April 22, 2014Date of Patent: February 13, 2018Assignee: THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUNDInventors: Lisa Ann Morici, Saja Asakrah
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Patent number: 9878985Abstract: The present invention relates to novel benzocyclobutane(thio) carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.Type: GrantFiled: October 28, 2014Date of Patent: January 30, 2018Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Christophe Dubost, Ulrike Wachendorff-Neumann, Philipp Winter, Stephane Brunet, Jean-Pierre Vors, Cyril Montagne
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Patent number: 9844221Abstract: The present invention relates to methods for controlling apple scab caused by Venturia inaequalis comprising spraying the bark of an apple tree with an effective amount of 3-(difluoromethyl)-1-methyl-N-[(3R)-1,1,3-trimethyl-2,3-dihydroinden-4-yl]pyrazole-4-carboxamide and a surfactant.Type: GrantFiled: June 30, 2016Date of Patent: December 19, 2017Assignee: VALENT U.S.A. CORPORATIONInventor: Billy R. Corbin, Jr.
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Patent number: 9833433Abstract: Embodiments of the present disclosure provide for compositions including an antimicrobial agent, pharmaceutical compositions including the composition or pharmaceutical composition, methods of treating a condition or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.Type: GrantFiled: August 9, 2017Date of Patent: December 5, 2017Assignee: Board of Supervisors of Louisiana State University and Agricultural and Mechanical CollegeInventors: Chu Chen, Jian Zhang
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Patent number: 9820969Abstract: This invention relates to, in part, methods and compositions that are useful for the diagnosis, treatment, or prevention of a blinding eye disease, including in the discovery of drugs that are efficacious against these diseases. Diseases include, for example, age related macular degeneration and reticular pseudodrusen disease, and the methods described herein include, for example, the method named delayed near infrared analysis (DNIRA).Type: GrantFiled: August 15, 2016Date of Patent: November 21, 2017Assignee: TRANSLATUM MEDICUS INC.Inventor: Shelley Romayne Boyd
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Patent number: 9801856Abstract: The present invention relates to certain compositions of a 5-HT2A serotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improvise sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like.Type: GrantFiled: April 6, 2015Date of Patent: October 31, 2017Assignee: Arena Pharmaceuticals, Inc.Inventors: Lee Alani Selvey, Marlon Carlos, Paul Maffuid, Yun Shan, William L. Betts, III, Deam Windate Given, III, Ryan M. Hart, Zezhi Jesse Shao
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Patent number: 9783503Abstract: Described herein are amorphous and crystalline forms of pharmaceutically acceptable salts of the estrogen receptor modulator (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl) phenyl)acrylic acid. Also described are pharmaceutical compositions suitable for administration to a mammal that include the estrogen receptor modulator, and methods of using the estrogen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with estrogen receptor activity.Type: GrantFiled: August 10, 2015Date of Patent: October 10, 2017Assignee: GENENTECH, INC.Inventors: Nicholas D. Smith, Mark R. Herbert
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Patent number: 9775349Abstract: The present invention relates to novel mixtures, to processes for preparing these compounds, to compositions comprising these mixtures, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms or pests in crop protection and in the protection of materials and as plant growth regulators.Type: GrantFiled: November 27, 2013Date of Patent: October 3, 2017Assignee: BAYER CROPSCIENCE AGInventors: Haruko Sawada, Ulrike Wachendorff-Neumann, Elke Hellwege, Heiko Rieck, Stefan Herrmann
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Patent number: 9775352Abstract: Provided is a method which exerts an excellent effect in controlling a pest in a field of soybean, corn or cotton, using a SDHI compound and a PPO-inhibiting compound.Type: GrantFiled: February 20, 2015Date of Patent: October 3, 2017Assignee: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Yoshinao Sada
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Patent number: 9771345Abstract: The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.Type: GrantFiled: October 7, 2010Date of Patent: September 26, 2017Assignees: Cornell University, Purdue Research Foundation, BlinkBio, Inc.Inventors: Francis Barany, Maneesh Pingle, Sarah Filippa Giardina, Donald Bergstrom, Lee Daniel Arnold
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Patent number: 9765031Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CB1 receptor mediating scaffold conjugated to (ii) a second therapeutic scaffold.Type: GrantFiled: November 12, 2013Date of Patent: September 19, 2017Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: George Kunos, Malliga Iyer, Resat Cinar, Kenner C. Rice
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Patent number: 9765034Abstract: The present invention relates to novel 1-methyl-3-dihalogenomehtyl-5-halogenopyrazole(thio)biphenyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.Type: GrantFiled: May 6, 2013Date of Patent: September 19, 2017Inventors: Simon Maechling, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Jean-Pierre Vors, Stephane Brunet, Helene Lachaise
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Patent number: 9765049Abstract: The present invention relates to fungicidal N-cycloalkyl-N-[(fusedphenyl)methylene] carboxamide derivatives, for example, compounds of formula (I), and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control ofphytopathogenic fungi of plants using these compounds or their compositions.Type: GrantFiled: June 24, 2014Date of Patent: September 19, 2017Assignee: BAYER CROPSCIENCE AGInventors: Peter Dahmen, Philippe Desbordes, Philippe Rinolfi, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann
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Patent number: 9768385Abstract: The present invention relates to a compound of a formula (I) or (II), to the use of this compound in an electronic device, and to an electronic device comprising one or more compounds of the formula (I) or (II). The invention furthermore relates to the preparation of the compound of the formula (I) or (II) and to a formulation comprising one or more compounds of the formula (I) or (II).Type: GrantFiled: March 15, 2012Date of Patent: September 19, 2017Assignee: Merck Patent GmbHInventors: Christof Pflumm, Irina Martynova, Teresa Mujica-Fernaud
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Patent number: 9745270Abstract: The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein.Type: GrantFiled: May 2, 2016Date of Patent: August 29, 2017Assignee: Arena Pharmaceuticals, Inc.Inventors: Marlon Carlos, Weitong Dong, Mark Macias, Suzanne Michiko Sato, Lee Alani Selvey