Chalcogen Or Nitrogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 514/380)
  • Patent number: 10226442
    Abstract: The present invention relates to a composition comprising a lithium salt of an N-substituted glycine compound and a carrier, wherein the lithium salt of the N-substituted glycine compound is of Formula (I): in which R1, R2, and R3 each are independently hydrogen, alkyl, alkenyl, alkynyl, aralkyl, carbocyclyl, aryl, or heteroaryl, or one of R1, R2, and R3 is absent. Also provided in the present invention is a method of mitigating at least one symptom of a neuropsychiatric disorder, comprising administering to a subject in need thereof the lithium salt of an N-substituted glycine compound of Formula (I).
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: March 12, 2019
    Assignee: SyneuRx International (Taiwan) Corp.
    Inventors: Guochuan Emil Tsai, Ching-Hsun Huang, Han-Yi Hsieh, Jing-Jia Huang, Ching-Cheng Wang
  • Patent number: 9993461
    Abstract: Methods of administering and pharmaceutical compositions of a biphenyl sulfonamide compound which is a dual angiotensin and endothelin receptor antagonist are disclosed for treating diseases.
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: June 12, 2018
    Assignee: Ligand Pharmaceuticals Inc.
    Inventors: Jinkun Zhang, Zofia E. Dziewanowska, Rene Belder, Ian Henderson, Joseph B. Bogardus, Zhaoying Zhang
  • Patent number: 9987381
    Abstract: The present invention relates to radiolabeled LPA1 receptor antagonists or pharmaceutically acceptable salts thereof which are useful for the quantitative imaging of LPA1 receptors in mammals.
    Type: Grant
    Filed: October 31, 2014
    Date of Patent: June 5, 2018
    Assignees: BRISTOL-MYERS SQUIBB COMPANY, YALE UNIVERSITY
    Inventors: Thomas Jon Seiders, David J. Donnelly, Samuel J. Bonacorsi, Jr., Kai Cao, Tritin Tran, Adrienne Pena, Joonyoung Kim, Richard E. Carson, Nabeel Nabulsi, Jean-Dominique Gallezot, Yiyun Huang, Jeffrey Roger Roppe
  • Patent number: 9937156
    Abstract: The present disclosure concerns uses for isoxazole compounds or salts or analogs thereof for the treatment of wounds. The present disclosure also concerns devices for delivering a isoxazole compound or salts or an analogs thereof to a wound site.
    Type: Grant
    Filed: October 16, 2014
    Date of Patent: April 10, 2018
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Eric M. Small, Eric N. Olson
  • Patent number: 9877951
    Abstract: Methods are disclosed for treating dementia, including mild cognitive impairment, via administration of D-cycloserine, or a prodrug thereof, on a tolerance-inhibiting basis. Specifically, by administering D-cycloserine on a tolerance-inhibiting basis, tolerance to D-cycloserine is less likely than would occur via daily administration, enhancing benefits and reducing costs and side effects. Pharmaceutical compositions useful for the treatment of dementia are additionally disclosed.
    Type: Grant
    Filed: February 10, 2016
    Date of Patent: January 30, 2018
    Assignee: College of William and Mary
    Inventor: Jason P. McDevitt
  • Patent number: 9789093
    Abstract: This invention provides an oral dosage regimen for the treatment of depression, a pharmaceutically acceptable medication dispensing package containing multiple dosage units of medicaments comprising an oral dosage regimen of D-cycloserine for the treatment of depression, a pharmaceutical composition comprising D-cycloserine formulated for oral administration providing a dosage of 1000 mg/day alone or in combination with antidepressant agents and uses thereof.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: October 17, 2017
    Assignee: Serotech, LLC
    Inventors: Uriel Heresco-Levy, Daniel Javitt
  • Patent number: 9737531
    Abstract: Compositions and methods tor the treatment of depression and psychoses in humans are disclosed. More particularly, the invention is directed to formulations containing antipsychotic and/or antidepressant medications and also containing an NMDAR antagonist. The present invention is also directed to methods for the treatment of humans suffering from depression and other psychoses, including, schizophrenia, by administration of the inventive compositions in antidepressant and/or antipsychotic effective amounts.
    Type: Grant
    Filed: July 7, 2013
    Date of Patent: August 22, 2017
    Assignee: GLYTECH, LLC
    Inventor: Daniel C Javitt
  • Patent number: 9474279
    Abstract: The present invention provides methods comprising applying to a crop of rice plants, the locus thereof, or propagation material thereof, a compound of formula (I): wherein —B1—B2—B3— is —C?N—O—, —C?N—CH2—, —C?CH2—O— or —N—CH2—CH2—; L is a direct bond or methylene; A1 and A2 are C—H, or one of A1 and A2 is C—H and the other is N; X1 is group X R1 is C1-C4alkyl, C1-C4haloalkyl or C3-C6cycloalkyl; R2 is chlorodifluoromethyl or trifluoromethyl; each R3 is independently bromo, chloro, fluoro or trifluoromethyl; R4 is hydrogen, halogen, methyl, halomethyl or cyano; R5 is hydrogen; or R4 and R5 together form a bridging 1,3-butadiene group; p is 2 or 3. Preferably the methods are for control of stemborer, leaffolder, hoppers, Gall midge, whorl maggot, Rice bugs, and/or Black bugs.
    Type: Grant
    Filed: August 9, 2013
    Date of Patent: October 25, 2016
    Assignee: Syngenta Participations AG
    Inventors: Myriem El Qacemi, Jerome Yves Cassayre
  • Patent number: 9375426
    Abstract: The present invention provides a method of screening anti-plasmodial activity of Acriflavin, comprising assessing growth inhibition of plasmodium in vitro in chloroquine susceptible and cloroquine resistant plasmodium by Acriflavin; or measuring in-vivo plasmodium killing ability of Acriflavin; assessing localization of Acriflavin at different stages; and analyzing effect of Acriflavin on gyrase activity wherein said method utilizes Acriflavin in nano-molar range. The present invention relates to potency of Acriflavin (Acriflavin) as an anti-malarial agent both in vitro parasite culture as well as in vivo. More specifically, the invention relates to a method o determining anti-plasmodial activity, Acriflavin as potent anti-malarial agent and also relates to composition(s) comprising Acriflavin.
    Type: Grant
    Filed: July 4, 2013
    Date of Patent: June 28, 2016
    Inventor: Suman Kumar Dhar
  • Patent number: 9320278
    Abstract: The present invention relates to methods, preferably for controlling and/or preventing infestation of boll weevil in cotton, comprising applying to a crop of cotton plants, the locus thereof, or propagation material thereof, a compound of formula (I), wherein -B1-B2-B3- is —C?N—O—, —C?N—CH2—, —C?CH—O— or —N—CH2—CH2—; L is a direct bond or methylene; A1 and A2 are C—H, or one of A1 and A2 is C—H and the other is N; X1 is group X R1 is C1-C4alkyl, C1C4aloalkyl or C3-C6cycloalkyl; R2 is chlorodifluoromethyl or trifluoromethyl; each R3 is independently bromo, chloro, fluoro or trifluoromethyl; R4 is hydrogen, halogen, methyl, halomethyl or cyano; R5 is hydrogen; or R4 and R5 together form a bridging 1,3-butadiene group; p is 2 or 3.
    Type: Grant
    Filed: August 16, 2013
    Date of Patent: April 26, 2016
    Assignee: Syngenta Participations AG
    Inventors: Myriem El Qacemi, Jerome Yves Cassayre
  • Patent number: 9303029
    Abstract: 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: Grant
    Filed: October 26, 2012
    Date of Patent: April 5, 2016
    Assignee: ASTEX THERAPEUTICS LTD
    Inventors: Steven John Woodhead, Christopher William Murray, Valerio Berdini, Gordon Saxty, Gilbert Ebai Besong, Lieven Meerpoel, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet
  • Patent number: 9090573
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: July 28, 2015
    Assignee: AMIRA PHARMACEUTICALS, INC.
    Inventors: Thomas J Seiders, Lucy Zhao, Jeannie Arruda, Bowei Wang, Brian Andrew Stearns, Yem Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Ryan Clark, Heather Renee Coate, Nicholas Simon Stock, Deborah Volkots
  • Publication number: 20150148387
    Abstract: Methamphetamine is a highly addictive psychostimulant that causes profound damage to the brain and other body organs. Post mortem studies of human tissues have linked the use of this drug to diseases associated with aging, such as coronary atherosclerosis, but the molecular mechanism underlying these findings remains unknown. We report now that methamphetamine accelerates cellular senescence in vitro and activates transcription of genes involved in cell-cycle control and inflammation in vivo by stimulating production of the sphingolipid messenger ceramide. This pathogenic cascade is triggered by reactive oxygen species, generated through methamphetamine metabolism via cytochrome P450-2D6, which recruit nuclear factor (NF)-KB to induce expression of enzymes in the de novo pathway of ceramide biosynthesis. Inhibitors of ceramide formation prevent methamphetamine-induced senescence and attenuate systemic inflammation and health deterioration in rats self-administering the drug.
    Type: Application
    Filed: September 30, 2014
    Publication date: May 28, 2015
    Inventors: Daniele Piomelli, Giuseppe Astarita, Agnesa Avanesian, Andrea Cavalli
  • Patent number: 9029410
    Abstract: A pharmaceutical composition, medical food, dietary supplement or micronutrient for the treatment of a movement disorder comprising an NMDAR agonist or partial agonist as active ingredient therein in combination with a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: January 2, 2014
    Date of Patent: May 12, 2015
    Assignee: Sarah Herzog Memorial Hospital Ezrath Nashim Association
    Inventors: Uriel Heresco-Levy, Daniel C. Javitt
  • Patent number: 9029400
    Abstract: The present invention relates to 5-oxoisoxazole derivatives of the formula I, the pharmaceutically usable salts thereof and the use thereof as medicinal substances.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: May 12, 2015
    Assignee: Sanofi
    Inventors: Stefan Petry, Manfred Seidel, Gerhard Zoller, Gunter Müller, Karl-Heinz Baringhaus, Hubert Heuer
  • Publication number: 20150110809
    Abstract: Embodiments of the invention are directed to compounds that inhibit an activity of EP AC proteins and methods of using the same. The inventors have developed a sensitive and robust high throughput screening (HTS) assay for the purpose of identifying EPAC specific inhibitors (Tsalkova et al. (2012) PLOS ONE 7 (1):e30441).
    Type: Application
    Filed: February 8, 2013
    Publication date: April 23, 2015
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Xiaodong Cheng, Jia Zhou, Tamara Tsalkova, Fang Mei, Haijun Chen
  • Patent number: 9012445
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20150105436
    Abstract: Methods for regulating glucagon release and of treating hypoglycemia, and for screening drug candidates for heating hypoglycemia. The methods are useful for treating diabetes melititus and screening drug candidates for potential efficacy.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Inventors: Per-Olof Berggren, Alejandro Caicedo, Over Cabrera
  • Publication number: 20150099758
    Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 9, 2015
    Applicant: Anvyl LLC
    Inventors: David Putnam, Olivier Dasse
  • Patent number: 8980837
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: March 17, 2015
    Assignee: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Patent number: 8975235
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Grant
    Filed: August 14, 2012
    Date of Patent: March 10, 2015
    Assignee: InterMune, Inc.
    Inventors: Brad O. Buckman, John B. Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
  • Publication number: 20150051233
    Abstract: Embodiments of the invention include methods of treating, preventing, and/or reducing the risk of fibrosis in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction of the risk of fibrosis. In at least particular cases, the small molecules are inhibitors of STAT3.
    Type: Application
    Filed: July 18, 2014
    Publication date: February 19, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Sandeep K. Agarwal, Mesias Pedroza
  • Patent number: 8957063
    Abstract: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: February 17, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Monika Ermann, Innocent Mushi
  • Publication number: 20150044239
    Abstract: The present invention relates to compositions and methods for diagnosing, preventing and treating intracranial aneurysm.
    Type: Application
    Filed: March 30, 2012
    Publication date: February 12, 2015
    Applicant: YALE UNIVERSITY
    Inventors: Richard Lifton, Murat Gunel
  • Publication number: 20150038492
    Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.
    Type: Application
    Filed: August 12, 2014
    Publication date: February 5, 2015
    Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
  • Patent number: 8940776
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: January 27, 2015
    Assignee: Genzyme Corporation
    Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
  • Patent number: 8927551
    Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: January 6, 2015
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Patent number: 8921576
    Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: December 30, 2014
    Assignee: Kowa Company, Ltd.
    Inventors: Takahisa Ogamino, Yukiyoshi Yamazaki, Shin Tanikawa, Ayumu Okuda, Tomoaki Fukuda, Okihisa Tokuda, Yoshiharu Miyake, Shinsuke Itoh, Hiroyuki Ishiwata
  • Publication number: 20140378466
    Abstract: 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: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Applicant: ARDEA BIOSCIENCES
    Inventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoul, Zhi Hong
  • Publication number: 20140357611
    Abstract: A method of treating an ocular disorder in a subject includes administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Inventors: Krzysztof Palczewski, Akiko Maeda, Marcin Golczak
  • Publication number: 20140357655
    Abstract: Spiroindoline derivatives, process for their preparation and pharmaceutical compositions thereof, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception and infertility (e.g., assisted reproductive therapy such as in vitro fertilization). The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.
    Type: Application
    Filed: January 15, 2013
    Publication date: December 4, 2014
    Inventors: Olaf Panknin, Stefan Bäurle, Sven Ring, Wolfgang Schwede, Wilhelm Bone, Katrin Nowak-Reppel, Eckhard Bender, Reinhard Nubbemeyer, Mark Jean Gnoth
  • Publication number: 20140343049
    Abstract: The present invention relates to compounds of formula (IA) wherein QA is QA1 or QA2 P is P1, heterocycyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Z, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (IA), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (IA) and to methods of using the compounds of formula (IA) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: August 10, 2012
    Publication date: November 20, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Julie Clementine Toueg, Tomas Smejkal, Sebastian Volker Wendeborn, Jerome Yves Cassayre, Myriem El Qacemi, Bernhard Breit, Lisa Diab, Regis Jean Georges Mondiere, Nicolas Poirier
  • Publication number: 20140336194
    Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.
    Type: Application
    Filed: July 28, 2014
    Publication date: November 13, 2014
    Applicant: NOVARTIS AG
    Inventor: Shi Yin FOO
  • Publication number: 20140329777
    Abstract: 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: Application
    Filed: April 22, 2014
    Publication date: November 6, 2014
    Inventors: Lisa Ann Morici, Saja Asakrah
  • Patent number: 8877786
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R6, A1, A2, X1, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: December 2, 2013
    Date of Patent: November 4, 2014
    Assignee: Novartis AG
    Inventors: Yuki Iwaki, Toshio Kawanami, Gary Michael Ksander, Muneto Moji
  • Publication number: 20140323423
    Abstract: Systems and methods for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and treating hyperglycemia, Alzheimer's disease, sleep disorders, Parkinson's disease, Attention Deficit Disorder and nicotine addiction involve synchronizing and tailoring the administration of nutraceuticals, medications and other substances (for example, stimulants) in accordance with the body's natural circadian rhythms, meal times and other factors. Improved control of blood glucose levels, extended alertness, and weight control, and counteracting of disease symptoms when they are at their worst are possible.
    Type: Application
    Filed: May 2, 2014
    Publication date: October 30, 2014
    Applicant: Chrono Therapeutics, Inc.
    Inventors: Guy DiPierro, Steven A. Giannos
  • Patent number: 8871792
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: October 28, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20140315933
    Abstract: The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or pharmaceutically acceptable salts thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes and to methods of treatment; wherein R1, R2, R3, R4, R5 and R6 are as defined in the description.
    Type: Application
    Filed: April 17, 2014
    Publication date: October 23, 2014
    Applicant: PFIZER LIMITED
    Inventors: Robert McKenzie Owen, Robert Ian Storer
  • Patent number: 8865744
    Abstract: Disclosed are (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.
    Type: Grant
    Filed: May 15, 2014
    Date of Patent: October 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Doris Riether, Florian Paul Christian Binder, Henri Doods, Stephan Georg Mueller, Janet Rachel Nicholson, Achim Sauer
  • Patent number: 8846727
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Patent number: 8846947
    Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: September 30, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • Patent number: 8846936
    Abstract: Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: September 30, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Eugene Richard Hickey, Doris Riether, Monika Ermann
  • Publication number: 20140271955
    Abstract: Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicants: The Scripps Research Institute, The California Institute for Biomedical Research
    Inventors: Peter G. SCHULTZ, Arnab K. CHATTERJEE, Shoutian ZHU, Joshua PAYETTE, Hongchul YOON, Baiyuan YANG
  • Publication number: 20140275037
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Application
    Filed: December 19, 2013
    Publication date: September 18, 2014
    Applicant: Siga Technologies, Inc.
    Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yanming Zhang, Sylvie Laquerre
  • Publication number: 20140256685
    Abstract: The present invention relates to a method for treating dermal inflammation and dermal diseases by local or systemic delivery, in a subject in need of such treatment, which comprises administering a pharmaceutical composition comprising a therapeutically effective amount of at least one agonist of Formyl peptide receptor 2 (FPR2).
    Type: Application
    Filed: March 4, 2014
    Publication date: September 11, 2014
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, John E. Donello, Veena Viswanath, Edward Hsia
  • Publication number: 20140256684
    Abstract: The present invention relates to a method for treating ocular inflammatory diseases in a subject in need of such treatment, which comprises administering a pharmaceutical composition comprising a therapeutically effective amount of at least one agonist of Formyl peptide receptor 2.
    Type: Application
    Filed: March 4, 2014
    Publication date: September 11, 2014
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, John E. Donello, Veena Viswanath
  • Publication number: 20140256702
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: March 4, 2014
    Publication date: September 11, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Erik Fenster, Melissa Fleury, Adam D. Hughes
  • Patent number: 8829034
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: September 9, 2014
    Assignee: Boehringer Ingerlheim International GmbH
    Inventors: Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Parke, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
  • Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • Publication number: 20140243375
    Abstract: The present invention provides compounds of formula I wherein G1 is oxygen; R1 is hydrogen; R2 is group P L is a bond, methylene or ethylene; R3 is hydrogen; R4 is independently hydrogen, cyano, cyano-C1-C8alkyl, C1-C8alkyl, C1-C8haloalkyl, C3-C8cycloalkyl, C3-C8-cycloalkyl where one carbon atom is replaced by O, S, S(O) or SO2, or C3-Cgcycloalkyl-C1-C8alkyl, C3-C8cycloalkyl-C1-C8alkyl where one carbon atom in the cycloalkyl group is replaced by O, S, S(O) or SO2, or C3-C8cycloalkyl-C1-C8haloalkyl, C1-C8hydroxyalkyl, C1-C8alkoxy-C1-C8alkyl, C2-C8alkenyl, C2-C8haloalkenyl, C2-C8alkynyl, C2-C8haloalkynyl, phenyl, phenyl substituted by one to three R6, phenyl-C1-C4alkyl, phenyl-C1-C4alkyl wherein the phenyl moiety is substituted by one to three R6, 5-6 membered heteroaryl-C1-C4alkyl or 5-6 membered heteroaryl-C1-C4alkyl wherein the heteroaryl moiety is substituted by one to three R6, or C1-C4alkyl-(C1-C4alkyl-O—N?)C—CH2—; each R6 is independently halogen, cyano, nitro, C1-C8alkyl, C1-C8haloalkyl, C1-C8alkoxy, or
    Type: Application
    Filed: September 28, 2012
    Publication date: August 28, 2014
    Applicant: Syngenta Participations AG
    Inventors: Myriem El Qacemi, Jerome Yves Cassayre