Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
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Patent number: 10118910Abstract: This invention is benzothiophene-based estrogen receptor downregulators and their compositions and uses to treat estrogen-related medical disorders.Type: GrantFiled: December 9, 2016Date of Patent: November 6, 2018Assignee: The Board of Trustees of the University of IllinoisInventors: Gregory R. Thatcher, Rui Xiong, Jiong Zhao, Debra A. Tonetti
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Patent number: 10112909Abstract: The disclosure describes methods of synthesis of phosphonate ester compounds. The methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity and stability. Also disclosed are morphic forms of phosphonate ester compounds.Type: GrantFiled: December 1, 2017Date of Patent: October 30, 2018Assignee: Chimerix, Inc.Inventors: Roy Wendell Ware, Aaron Leigh Downey
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Patent number: 10105365Abstract: The present disclosure relates to solid dosage forms comprising antiviral compounds and methods of using such dosage forms to treat antiviral infection.Type: GrantFiled: June 30, 2017Date of Patent: October 23, 2018Assignee: AbbVie Inc.Inventors: Jonathan M. Miller, John B. Morris, Nancy E. Sever, Eric A. Schmitt, Ping X. Gao, Yi Shi, Yi Gao, Bernd Liepold, Anna Moosmann, Mirko Pauli, Fatih Durak, Thomas Kessler, Peter Hoelig, Karin Rosenblatt, Drazen Kostelac, Rajeev Gokhale, Mark Costello, Carl Knable, Susan George
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Patent number: 10058551Abstract: The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizopherenea, substance abuse disorders, sleep disorders or epilepsy.Type: GrantFiled: October 2, 2017Date of Patent: August 28, 2018Assignee: Autifony Therapeutics LimitedInventors: Giuseppe Alvaro, Anne Decor, Stefano Fontana, Dieter Hamprecht, Charles Large, Agostino Marasco
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Patent number: 10051862Abstract: A fungicidal composition containing a fungicidally effective amount of the compound of Formula I: 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide to provide synergistic control of selected fungi wherein the at least one fungicide is a multi-site inhibitor or a strobilurin inhibitor.Type: GrantFiled: December 13, 2016Date of Patent: August 21, 2018Assignee: ADAMA MAKHTESHIM LTD.Inventors: W. John Owen, Chenglin Yao, Beth Lorsbach
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Patent number: 10045534Abstract: A fungicidal composition containing a fungicidally effective amount of the compound of Formula I: 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide to provide synergistic control of selected fungi, wherein the at least one fungicide is a succinate dehydrogenase-inhibitor.Type: GrantFiled: December 13, 2016Date of Patent: August 14, 2018Assignee: ADAMA MAKHTESHIM LTD.Inventors: W. John Owen, Chenglin Yao, Beth Lorsbach
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Patent number: 10045533Abstract: A fungicidal composition containing a fungicidally effective amount of the compound of Formula I: 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide to provide synergistic control of selected fungi wherein the at least one fungicide is a fungicidal sterol biosynthesis-inhibitor.Type: GrantFiled: December 13, 2016Date of Patent: August 14, 2018Assignee: ADAMA MAKHTESHIM LTD.Inventors: W. John Owen, Chenglin Yao, Beth Lorsbach
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Patent number: 10023564Abstract: Disclosed herein are novel GRK2 inhibitors and methods for their use in treating or preventing heart disease, such as cardiac failure, cardiac hypertrophy, and hypertension. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: wherein the substituents are as described.Type: GrantFiled: August 10, 2015Date of Patent: July 17, 2018Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Scott D. Larsen, Kristoff Homan, Helen Waldschmidt, John J. G. Tesmer
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Patent number: 10016424Abstract: The present invention relates to a compound which is an antagonist of the GluK2/GluK5 receptor or an inhibitor of the GluK2/GluK5 receptor expression for use in the treatment or the prevention of epilepsy.Type: GrantFiled: September 16, 2014Date of Patent: July 10, 2018Assignees: INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE, UNIVERSITÉ D'AIX MARSEILLE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE BORDEAUXInventors: Valerie Crepel, Christophe Mulle, Angelique Peret
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Patent number: 10015964Abstract: The present invention provides a fungicidal composition useful as an agricultural and horticultural fungicide having remarkably improved controlling effects against plant diseases, and a method for controlling plant diseases using the composition. A fungicidal composition comprising, as active ingredients, (a) 3-(2,3,4-trimethoxy-6-methylbenzoyl)-5-chloro-2-methoxy-4-methylpyridine (pyriofenone) or its salt and (b) at least one fungicide selected from the group consisting of bixafen, fluxapyroxad, penflufen, isopyrazam, fluopyram, ametoctradin, fenpyrazamine and sedaxane, and a method for controlling plant diseases, which comprises applying the fungicidal composition to plants.Type: GrantFiled: June 15, 2012Date of Patent: July 10, 2018Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Munekazu Ogawa, Yuzuka Kawai
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Patent number: 9987280Abstract: Provided herein are, inter alia, methods and compositions for treating or preventing diseases using SIRT1 inhibitors. The methods provided herein are particularly useful for treating or preventing age-related hematological diseases as well as cancerous hematological diseases. Further provided herein are hematopoietic cells useful for treating or preventing hematological diseases.Type: GrantFiled: August 11, 2014Date of Patent: June 5, 2018Assignee: City of HopeInventors: WenYong Chen, Zhiqiang Wang
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Patent number: 9988687Abstract: A method of classifying a patient for eligibility for cancer therapy based on the presence or absence of splicing variants in a sample of the patient's cancer tissue. Also, a method of screening cancer therapies for efficacy against splicing variants. More specifically, the methods relate to novel splicing variants of genes associated with cancer risk and survival, particularly splicing variants of PIK3CD, FGFR3, TSC2, RASGRP2, ITGA4, MET, NF1 and BAK1. Also more specifically, the methods relate to classifying a patient for eligibility for cancer therapy involving the use of GS-1101.Type: GrantFiled: March 5, 2015Date of Patent: June 5, 2018Assignee: THE GEORGE WASHINGTON UNIVERISTYInventors: Norman Lee, Bi-Dar Wang
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Patent number: 9877966Abstract: The invention provides therapeutic compositions and methods for the inhibition of metastasis and for treatment of cancers in human and non-human mammals that are directed to the coformulation and/or coadministration of a dehydropyrimidine dehydrogenase inhibitor such as gimeracil and a pyrrolopyrimidine compound.Type: GrantFiled: August 10, 2016Date of Patent: January 30, 2018Inventors: Eugene J. Oliva, Paul Diamond
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Patent number: 9850215Abstract: Provided herein are 5-fluoro-4-imino-3-(alkyl/substituted alkyl)-1-(arylsulfonyl)-3,4-dihydropyrimidin-2(1H)-one and processes for their preparation which may include the use of an alkali carbonate and an alkylating agentType: GrantFiled: June 3, 2016Date of Patent: December 26, 2017Assignee: ADAMA MAKHTESHIM LTD.Inventors: Nakyen Choy, Ronald Ross, Jr.
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Patent number: 9802933Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.Type: GrantFiled: December 15, 2016Date of Patent: October 31, 2017Assignee: SciFluor Life Sciences, Inc.Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
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Patent number: 9776985Abstract: Provided is a novel process for the preparation of alogliptin.Type: GrantFiled: May 20, 2014Date of Patent: October 3, 2017Assignee: GLENMARK PHARMACEUTICALS LIMITEDInventors: Navin Ganesh Bhatt, Samir Naik, Ajay Kumar Sharma, Mahendra Joma Choraghe, Shekhar Bhaskar Bhirud
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Patent number: 9770406Abstract: The invention relates to a medicament containing a compound of general formula (I), where R1=independently, a straight or branched, saturated, singly- or multiply-unsaturated, optionally substituted C11-C21 alkyl, alkylene or alkinyl group, preferably a C11-C15 alkyl, alkylene or alkinyl group, particularly a C11-C13 alkyl, alkylene or alkinyl group, most preferably a C13 alkyl group, R2=independently, a straight or branched C1-C8 alkyl, alkylene or alkinyl group, preferably a C1-C6 alkyl, alkylene or alkinyl group, in particular a C2-C4 alkyl, alkylene or alkinyl group, most preferably a C3 alkyl group, a —[CH2—(CH2)m-O]nH group with n=1 to 10, preferably n=1 to 5, to m=1 to 5, preferably m=1 to 3, a —CH2—[CH—(OH)]p[CH2—R3]- group, where R3=independently H or OH, p=1 to 7, preferably p=1 to 4, a pentose group or a hexose group, as therapeutically active agent, alone or in combination with one or several further pharmaceutical agents as a combination preparation for the treatment of viral skin diseases and/orType: GrantFiled: September 21, 2010Date of Patent: September 26, 2017Assignee: Medigene AGInventors: Yunik Chang, Robert Lathrop, Erwin Böhm, Irene Gander-Meisterernst, Regina Greger, Johanna Holldack, Ulrich Moebius
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Patent number: 9676714Abstract: Disclosed are a sulfonylindole derivative useful for the prevention or treatment of peptic ulcer, gastritis or reflux esophagitis, a method of preparing the same, and a pharmaceutical composition containing the same.Type: GrantFiled: October 2, 2014Date of Patent: June 13, 2017Assignee: Daewoong Pharmaceutical Co., Ltd.Inventors: Kyung A Yu, Ji Sung Yoon, Deok Ki Eom, Yeon Im Lee, Hye Ryun Shin, Jun Hee Lee, Ha Nee Seo, Ji Duck Kim, Sang Ho Lee, Chun Ho Lee
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Patent number: 9669030Abstract: The present invention relates to the prophylaxis of acute noise-induced hearing loss by administering a compound of formula (I): wherein: W is group (Wa), group (Wb) or group (Wc):Type: GrantFiled: May 22, 2013Date of Patent: June 6, 2017Assignee: AUTIFONY THERAPEUTICS LIMITEDInventor: Charles Large
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Patent number: 9642808Abstract: Extended release pharmaceutical compositions comprising mycophenolate sodium as the active agent, wherein the said composition exhibits a characteristic release profile when subjected to in-vitro dissolution study, and wherein said mycophenolate sodium is released in a sustained manner in-vivo for a prolonged duration in such quantities that substantially alleviates or at least reduces the chances of causing any associated gastrointestinal side effect(s) without compromising the bioavailability of the said active agent are provided. The present invention also provides process of preparing dosage form compositions and prophylactic and/or therapeutic methods of using such dosage form. The compositions of the present invention are useful for the management such as prophylaxis, amelioration and/or treatment of immunosuppressant indicated disease(s)/disorder(s) especially for the treatment or prevention of organ, tissue or cellular allograft or xenograft rejection, e.g.Type: GrantFiled: August 11, 2008Date of Patent: May 9, 2017Assignee: PANACEA BIOTECH LIMITEDInventors: Rajesh Jain, Sukhjeet Singh, Sampath Kumar Devarajan
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Patent number: 9642368Abstract: This present disclosure is related to the field of 3-alkyl-5-fluoro-4-substituted-imino-3,4-5 dihydropyrimidin-2(1H)-ones and their derivatives and to the use of these compounds as fungicides. Also provided are methods of controlling a fungal disease such as Septoria tritici, comprising administering an effective amount of the fungicide compound to at lease one surface associated with the plant, seed or soil.Type: GrantFiled: December 23, 2013Date of Patent: May 9, 2017Assignee: ADAMA MAKHTESHIM LTD.Inventors: Beth Lorsbach, Ronald Ross, W. John Owen, Jeffery D. Webster, Lindsay Stelzer, Chenglin Yao, Paul R. LePlae, Jr., Chris V. Galliford
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Patent number: 9642373Abstract: The present invention provides novel insecticidal formulations comprising an effective concentration of: 1) at least one or more essential oils and an insecticidal soap; 2) at least one or more essential oils, an insecticidal soap, and pyrethrins; 3) at least one or more essential oils and pyrethrins; 4) at least one or more essential oils, an insecticidal soap and a synergist, such as sodium lauryl sulfate, sodium dodecyl sulfate or lecithin; 5) at least one or more essential oils, an insecticidal soap, a synergist, and pyrethrins; and 6) at least one or more essential oils, a synergist, and pyrethrins. A carrier oil, such as mineral oil, may be added to any of the foregoing formulations.Type: GrantFiled: March 20, 2014Date of Patent: May 9, 2017Assignee: WOODSTREAM CORPORATIONInventor: David L. Anderson
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Patent number: 9624213Abstract: Compounds active on protein kinases are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: GrantFiled: February 1, 2012Date of Patent: April 18, 2017Assignee: Plexxikon Inc.Inventors: Prabha Ibrahim, Chao Zhang, Wayne Spevak, Jiazhong Zhang, Guoxian Wu, Jack Lin, Hanna Cho, Marika Nespi, Songyuan Shi, Todd Ewing, Ying Zhang
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Patent number: 9597316Abstract: Provided herein are compounds, comprising Formula (I) or Formula (II), and their pharmaceutically acceptable salts. Also provided are pharmaceutical compositions comprising a pharmaceutically acceptable excipient and at least one compound of Formula (I) and (II), singly or in combination with other pharmaceutically active ingredients, such as anti-inflammatory agents or anticancer agents. These compounds and pharmaceutical compositions are useful for treating inflammation or an inflammation related disorder in a subject via administration to the subject. These compounds and pharmaceutical compositions are also useful for inhibiting COX-2, for treating cancer, for reducing the size of a neoplasm, and for inhibiting tubulin polymerization in a cell.Type: GrantFiled: December 26, 2013Date of Patent: March 21, 2017Assignee: BIOVENTURES LLCInventors: Narsimha Reddy Penthala, Peter Crooks
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Patent number: 9592231Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelia A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.Type: GrantFiled: September 19, 2014Date of Patent: March 14, 2017Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
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Patent number: 9593114Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.Type: GrantFiled: January 19, 2016Date of Patent: March 14, 2017Assignee: SciFluor Life Sciences, Inc.Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
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Patent number: 9538753Abstract: A fungicidal composition containing a fungicidally effective amount of the compound of Formula I: 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide selected from the group consisting of mancozeb, chlorothalonil, pyraclostrobin, fluoxastrobin, azoxystrobin, trifloxystrobin, picoxystrobin, and kresoxim-methyl provides synergistic control of selected fungi.Type: GrantFiled: December 30, 2014Date of Patent: January 10, 2017Assignee: ADAMA MAKHTESHIM LTD.Inventors: W. John Owen, Chenglin Yao, Beth Lorsbach
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Patent number: 9532570Abstract: A fungicidal composition containing a fungicidally effective amount of the compound of Formula I: 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide selected from the group consisting of fluxapyroxad, benzovindiflupyr, penthiopyrad, isopyrazam, boscalid, and fluopyram provides synergistic control of selected fungi.Type: GrantFiled: December 30, 2014Date of Patent: January 3, 2017Assignee: ADAMA MAKHTESHIM LTD.Inventors: W. John Owen, Chenglin Yao, Beth Lorsbach
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Patent number: 9526245Abstract: A fungicidal composition containing a fungicidally effective amount of the compound of Formula I: 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide selected from the group consisting of: prothioconazole, epoxiconazole, cyproconazole, myclobutanil, metconazole, difenoconazole, propiconazole, fluquinconazole, and flutriafol provides synergistic control.Type: GrantFiled: December 30, 2014Date of Patent: December 27, 2016Assignee: ADAMA MAKHTESHIM LTD.Inventors: W. John Owen, Chenglin Yao, Beth Lorsbach
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Patent number: 9487534Abstract: In addition to containing and protecting the viral genome, the capsid (protein shell) of hepatitis B virus (HBV) plays critical roles in the viral life cycle including regulation of intracellular trafficking and nucleic acid metabolism. Substituted pyrimidine modulators of the assembly of the HBV capsid structure and methods for their use are described.Type: GrantFiled: August 2, 2012Date of Patent: November 8, 2016Assignees: Scripps Research Institute, A Not-for-Profit Public Benefit Corporation of California, Indiana University Research and Technology CorporationInventors: Adam Zlotnick, M. G. Finn
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Patent number: 9399626Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.Type: GrantFiled: June 9, 2014Date of Patent: July 26, 2016Assignee: Pfizer Inc.Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
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Patent number: 9382286Abstract: A method and composition for the treatment, prevention and/or prophylaxis of a host, and in particular, a human, infected with Epstein-Barr virus (EBV), is provided that includes administering an effective amount of a 5-substituted uracil nucleoside or its pharmaceutically acceptable salt or prodrug, optionally in a pharmaceutically acceptable diluent or excipient.Type: GrantFiled: December 4, 2013Date of Patent: July 5, 2016Assignees: EMORY UNIVERSITY, BETH ISRAEL DEACONESS MEDICAL CENTER, INC.Inventors: Raymond F. Schinazi, Junxing Shi, Joyce D. Fingeroth, Erik Gustafson
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Patent number: 9382204Abstract: The present invention provides STAT3 inhibitors which preferentially suppress proliferation of cancer over non-cancer cells and inhibit migration and invasion of malignant cells. The inhibitors of the present invention selectively inhibit STAT3 binding to DNA without affecting the activation and dimerization of STAT3. Furthermore, the inhibitors of the present invention inhibit expression of STAT3 downstream target genes and STAT3 binding to chromatin in situ.Type: GrantFiled: September 25, 2014Date of Patent: July 5, 2016Assignee: Indiana University Research and Technology CorporationInventor: Jian-Ting Zhang
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Patent number: 9345709Abstract: The present invention directs a compound represented by formula (I).Type: GrantFiled: May 21, 2015Date of Patent: May 24, 2016Assignee: OncoTherapy Science, Inc.Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Joel R. Walker, Raymond Huntley
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Patent number: 9271496Abstract: A fungicidal composition containing a fungicidally effective amount of a compound of Formula I: (3S,6S,7R,8R)-8-benzyl-3-(3-((isobutyryloxy)methoxy)-4-methoxypicolinamido)-6-methyl-4,9-dioxo-1,5-dioxonan-7-yl isobutyrate, and at least one fungicide selected from the group consisting of: benzovindiflupyr and penthiopyrad provides synergistic control of selected fungi.Type: GrantFiled: December 29, 2014Date of Patent: March 1, 2016Assignee: Dow AgroSciences LLCInventor: Greg Kemmitt
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Patent number: 9271497Abstract: This present disclosure is related to the field of 1-(substituted-benzoyl)-5-fluoro-4-imino-3-methyl-3,4-dihydropyrimidin-2(1H)-ones and their derivatives and to the use of these compounds as fungicides. Fungicides are compounds, of natural or synthetic origin, which act to protect and/or cure plants against damage caused by agriculturally relevant fungi. Generally, no single fungicide is useful in all situations. Consequently, research is ongoing to produce fungicides that may have better performance, are easier to use, and cost less. The present disclosure relates to 1-(substituted-benzoyl)-5-fluoro-4-imino-3-methyl-3,4-dihydropyrimidin-2(1H)-one compounds and their use as fungicides. The compounds of the present disclosure may offer protection against fungi and fungi like organisms including ascomycetes, basidiomycetes, deuteromycetes, and oomycetes.Type: GrantFiled: December 23, 2013Date of Patent: March 1, 2016Assignee: Dow AgroSciences LLCInventors: Beth Lorsbach, W. John Owen, Lindsay Stelzer, Chenglin Yao
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Patent number: 9249107Abstract: The invention relates to a compound of the formula wherein the substituents are as defined herein, and a pharmaceutically acceptable salt of the compound of formula (1). The compounds of formula (1) and their salts possess inflammation inhibiting properties and are therefore useful in the treatment and prevention of conditions related to inflammations such as inflammatory joint diseases. The compounds of formula (1) are also useful for the treatment of diseases where chronic inflammation is the underlying cause. This application relates to compounds of formula (1), methods for their preparation, pharmaceutical compositions comprising these compounds, and their use for the preparation of a medicament for the treatment of humans and animals.Type: GrantFiled: September 20, 2013Date of Patent: February 2, 2016Inventor: Hubert Maehr
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Patent number: 9221782Abstract: There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. The compound is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.Type: GrantFiled: April 15, 2014Date of Patent: December 29, 2015Assignee: AstraZeneca ABInventors: Stephen Connolly, Mark Richard Ebden, Iain Alastair Stewart Walters, Thomas Langer, Alan Robert Steven, Craig Robert Stewart, Paula Margaret Tomlin, Andrew John Williams
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Patent number: 9204653Abstract: This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.Type: GrantFiled: September 19, 2013Date of Patent: December 8, 2015Assignee: Dow AgroSciences LLCInventors: Timothy Boebel, Kristy Bryan, Carla J. R. Klittich, Beth Lorsbach, Timothy P. Martin, Mark A. Pobanz, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao, W. John Owen
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Patent number: 9199946Abstract: The present invention provides compounds of Formula (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: GrantFiled: March 29, 2013Date of Patent: December 1, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang, Ji Jiang
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Patent number: 9174997Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: GrantFiled: October 23, 2014Date of Patent: November 3, 2015Assignee: Bayer Intellectual Property GmbHInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Jens Schamberger
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Patent number: 9174968Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.Type: GrantFiled: December 15, 2014Date of Patent: November 3, 2015Assignee: Glaxo Group LimitedInventors: Yun Jin, Zehong Wan, Qing Zhang
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Patent number: 9174970Abstract: This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.Type: GrantFiled: January 22, 2009Date of Patent: November 3, 2015Assignee: Dow AgroSciences LLCInventors: Zoltan L. Benko, Timothy Boebel, Nneka T. Breaux, Kristy Bryan, George E. Davis, Jeffrey B. Epp, Beth Lorsbach, Timothy P. Martin, Kevin G. Meyer, Bassam S. Nader, W. John Owen, Mark A. Pobanz, James M. Ruiz, Frisby D. Smith, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao, David H. Young
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Patent number: 9139559Abstract: Compounds of Formula (I) promote axonal outgrowth angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases, peripheral arterial occlusive diseases, or after-effects of these diseases. in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R0, R1 and R2 are each independently a hydrogen atom, an alkyl group, or an amino group; E is an oxygen atom or an —NR8 group (wherein R8 is an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, or —CO—; and Q is a hydrogen atom or a phenyl group.Type: GrantFiled: February 5, 2014Date of Patent: September 22, 2015Assignee: DAIICHI SANKYO COMPANY, LIMITEDInventors: Naohiro Takemoto, Kenji Murata, Norihito Murayama, Chikaomi Yamada
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Patent number: 9139536Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: GrantFiled: March 15, 2013Date of Patent: September 22, 2015Assignee: AbbVie Inc.Inventors: Charles A. Flentge, Douglas K. Hutchinson, David A. Betebenner, David A. DeGoey, Pamela L. Donner, Warren M. Kati, Allan C. Krueger, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, Christopher E. Motter, John K. Pratt, John T. Randolph, Todd W. Rockway, Kent D. Stewart, Rolf Wagner, Shuang Chen, Yi Gao, Xiaochun Lou, Geoff G. Z. Zhang
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Patent number: 9084788Abstract: The invention encompasses protectant agents including uracil or a metabolite thereof that effectively treat the cutaneous toxicities and dermatological side-effects associated with chemotherapeutic agents. Specifically, and surprisingly, the compositions of the invention including uracil or a metabolite thereof are effective for treating various dermatoses including atopic dermatitis, irritant contact dermatitis, radiation-induced dermatitis, dry skin dermatitis, papulopustular rashes, xerosis, pruitus, actinic keratosis, and genital warts.Type: GrantFiled: August 3, 2012Date of Patent: July 21, 2015Assignee: Asymmetric Therapeutics, LLCInventor: John P. Ford
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Patent number: 9067937Abstract: The present invention directs a compound represented by formula (I).Type: GrantFiled: December 21, 2012Date of Patent: June 30, 2015Assignee: OncoTherapy Science, Inc.Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Joel R. Walker, Raymond Huntley
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Patent number: 9062059Abstract: The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: August 20, 2012Date of Patent: June 23, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher D. Cox, Vadim Y. Dudkin, Jeffrey Kern, Mark E. Layton, Izzat T. Raheem
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Patent number: 9044509Abstract: A process is provided for protecting a primate host from a self-replicating infection by an immunodeficiency retrovirus. Protection is achieved by administering to the primate host a combination of a pharmaceutically effective amount of a nucleoside reverse transcriptase inhibitor and a pharmaceutically effective amount of a nucleotide reverse transcriptase inhibitor prior to exposure to the immunodeficiency retrovirus. The administration is effective if provided in a single dose within 24 hours of the exposure. A regime of regular daily doses is also effective in providing protection against an immunodeficiency retrovirus becoming self-replicating after infecting a primate host.Type: GrantFiled: January 31, 2007Date of Patent: June 2, 2015Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Walid M. Heneine, Thomas M. Folks, Robert Janssen, Ronald Otten, Jose Gerardo Garcia Lerma
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Publication number: 20150148359Abstract: Uses of a compound of any of Formulas I-VI as a cytotoxic inhibitor of undifferentiated cells are disclosed herein, as well as pharmaceutical compositions comprising a compound of any of Formulas I-VI, and methods for identifying a lead candidate for inhibiting undifferentiated cells. Further disclosed are uses of an SCD-1 inhibitor as a cytotoxic inhibitor of undifferentiated cells.Type: ApplicationFiled: May 22, 2013Publication date: May 28, 2015Inventors: Uri Ben-David, Nissim Benvenisty, Payal Arora, Qing-Fen Gan, Ralph J. Garippa