Tetrazoles (including Hydrogenated) Patents (Class 514/381)
  • Patent number: 10100039
    Abstract: Disclosed are polymorph of allisartan isoproxil and a pharmaceutical composition thereof. The polymorph is non-electrostatic, highly flowable and highly stable, and can be used for treating hypertension and complications thereof.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: October 16, 2018
    Assignee: SHENZHEN SALUBRIS PHARMACEUTICALS CO., LTD
    Inventors: Duanming Tan, Jun Ou
  • Patent number: 10053448
    Abstract: A tetrazolinone compound represented by formula (1): wherein R1 represents a hydrogen atom, a C1-C3 alkyl group optionally having one or more halogen atoms, a C1-C3 alkoxy group optionally having one or more halogen atoms, a halogen atom, a cyano group, or a C1-C3 alkylthio group optionally having one or more halogen atoms; and R2 represents a C1-C3 alkyl group optionally having one or more halogen atoms, a C1-C3 alkoxy group optionally having one or more halogen atoms, a hydrogen atom, a halogen atom, or a C3-C4 cycloalkyl group optionally having one or more halogen atoms, has excellent control activity against plant diseases.
    Type: Grant
    Filed: March 28, 2016
    Date of Patent: August 21, 2018
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Nao Maehata, Sadayuki Arimori
  • Patent number: 9955693
    Abstract: Phytopathogenic filamentous fungi other than oomycete microorganisms are controlled using at least one compound selected from among tetrazoyloxime derivatives represented by formula (I) and salts thereof. In formula (I), X represents a C1 to C6 alkyl group or the like, n represents an integer of 0 to 5, Y represents a C1 to C6 alkyl group, Z represents a hydrogen atom or an amino group or the like, Q represents a hydrogen atom or a C1 to C8 alkyl group or the like, R represents a halogeno group or a C1 to C6 alkoxy group, and m represents an integer of 0 to 3.
    Type: Grant
    Filed: February 24, 2014
    Date of Patent: May 1, 2018
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Tomoyuki Saiga, Kazushige Kato, Shinya Watanabe, Akie Fukuyo
  • Patent number: 9918964
    Abstract: It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner.
    Type: Grant
    Filed: April 25, 2011
    Date of Patent: March 20, 2018
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: James P. Collman, Paul Clifford Herrmann, David Alvin Tyvoll, Richard Decreau, Brian Stanley Bull, Christopher Jeffrey Barile
  • Patent number: 9856214
    Abstract: The invention provides EBNA1 inhibitors, and pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by EBNA1 activity such as, but not limited to, cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and/or rheumatoid arthritis. The compounds and compositions of the invention are further useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. The compounds and compositions of the invention are further useful for the treatment of diseases caused by lytic EBV infection.
    Type: Grant
    Filed: November 14, 2014
    Date of Patent: January 2, 2018
    Assignee: THE WISTAR INSTITUTE OF ANATOMY AND BIOLOGY
    Inventors: Troy E. Messick, Garry R. Smith, Allen B. Reitz, Paul M. Lieberman, Mark E. McDonnell, Yan Zhang, Venkata Velvadapu
  • Patent number: 9801866
    Abstract: Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: October 31, 2017
    Assignee: Rigl Pharmaceutical, Inc.
    Inventors: Matthew Duncton, Somasekhar Bhamidipati, Jiaxin Yu, Ihab Darwish, Rajinder Singh
  • Patent number: 9763953
    Abstract: The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugs”, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.
    Type: Grant
    Filed: April 11, 2013
    Date of Patent: September 19, 2017
    Assignee: NEURODYN LIFE SCIENCES INC.
    Inventor: Alfred Maelicke
  • Patent number: 9725423
    Abstract: The compound represented by formula (1): wherein R4 and R5 each represents a hydrogen atom, a halogen atom, or a C1-C3 alkyl group; R6 represents a C1-C4 alkyl group, a C3-C6 cycloalkyl group, or the like; R7, R8, and R9 each represents a hydrogen atom, a halogen atom, or the like; R10 represents a C1-C3 alkyl group, or the like; R13 represents a C1-C3 alkyl group, or the like; and Q represents a phenyl group, or the like; has an excellent control effect on pests.
    Type: Grant
    Filed: November 20, 2013
    Date of Patent: August 8, 2017
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Nao Hasegawa, Sadayuki Arimori, Yuichi Matsuzaki
  • Patent number: 9701175
    Abstract: A hybrid vehicle includes an exhaust turbine disposed in an exhaust path coupled to an electric machine and a compressor for an air-conditioning system. The vehicle includes a controller that controls the electric machine based on a difference between the power demand of the compressor and the power generated by the exhaust turbine. The electric machine may operate as a motor or a generator based on the difference. The vehicle may include a first clutch coupled to the electric machine and the compressor. The vehicle may include a second clutch coupled between the exhaust turbine and the electric machine. The controller may control the clutches based on the power demand and the power generated.
    Type: Grant
    Filed: April 14, 2015
    Date of Patent: July 11, 2017
    Assignee: Ford Global Technologies, LLC
    Inventors: Kenneth James Miller, Thomas G. Leone
  • Patent number: 9573904
    Abstract: An aromatic compound represented by formula (1): wherein R1 and R2 each independently represents a halogen atom, a C1-C4 alkyl group, or a C1-C4 haloalkyl group; m and n each independently represents an integer of 0 to 4; R3 and R4 each represents a hydrogen atom; Y represents formula: —OC(?X)ZR5 or —SC(?X)ZR5; R5 represents a C1-C3 alkyl group optionally having one or more halogen atoms; Z represents a sulfur atom, NR8, or a direct bond; R8 represents a C1-C3 alkyl group or a hydrogen atom; Q represents a pyrazolyl group optionally having a substituent; and W and X each independently represents an oxygen atom or a sulfur atom, has excellent control activity against pests.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: February 21, 2017
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Takayuki Shioda
  • Patent number: 9499499
    Abstract: The invention relates to new salts of valsartan or crystalline, also partly crystalline and amorphous salts of valsartan, the respective production and usage, and pharmaceutical preparations containing such a salt.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: November 22, 2016
    Assignee: Novartis AG
    Inventors: Erwin Marti, Hans Rudolf Oswald, Peter Buehlmayer, Wolfgang Marterer
  • Patent number: 9475781
    Abstract: Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: October 25, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Matthew Duncton, Somasekhar Bhamidipati, Jiaxin Yu, Ihab Darwish, Rajinder Singh
  • Patent number: 9447069
    Abstract: The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR.
    Type: Grant
    Filed: April 30, 2013
    Date of Patent: September 20, 2016
    Assignee: INNOV17 LLC
    Inventors: Anderson Gaweco, Jefferson W. Tilley, John Walker, Samantha Palmer, James Blinn
  • Patent number: 9440952
    Abstract: The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: September 13, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Kallol Basu, Duane DeMong, Jack Scott, Hong Liu, Xing Dai, Joel M. Harris, Bernard Neustadt, Andrew Stamford, Marc Poirier, John A. McCauley, Thomas Greshock, Heather Stevenson, John Sanders, Jonathan Kern
  • Patent number: 9381172
    Abstract: Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.
    Type: Grant
    Filed: May 12, 2012
    Date of Patent: July 5, 2016
    Assignee: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: Brian Clem, Sucheta Telang, John Trent, Jason Chesney, Pooran Chand, Gilles Tapolsky
  • Patent number: 9382588
    Abstract: The present invention includes methods for identifying patients who will be resistant to endocrine therapy during breast cancer treatment and determining patient outcome. The methods are based on identifying increased expression of PBX1, or the cistrome signature associated therewith, in breast tissue samples.
    Type: Grant
    Filed: February 15, 2012
    Date of Patent: July 5, 2016
    Assignee: Trustees of Dartmouth College
    Inventors: Mathieu Lupien, Luca Magnani
  • Patent number: 9371528
    Abstract: The invention relates generally to methods and compositions for treating sinusitis, asthma, or polyps. The invention also relates to methods and compositions for treating nasal polyps.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: June 21, 2016
    Assignee: Massachusetts Eye and Ear Infirmary
    Inventors: Konstantina M. Stankovic, Ralph Metson
  • Patent number: 9333233
    Abstract: The present invention provides, among other things, method of treating stroke including a step of administering an angiotensin (1-7) peptide to a subject suffering from a stroke, approximately 24 hours after the stroke. In some embodiments, treatment begins more than 24 hours after the stroke. In some embodiments, administration of an angiotensin (1-7) peptide results in a reduction in the intensity, severity, duration, and/or frequency of at least one symptom or feature of the one or more complications of stroke.
    Type: Grant
    Filed: November 20, 2014
    Date of Patent: May 10, 2016
    Assignee: TARIX PHARMACEUTICALS LTD.
    Inventor: Richard Franklin
  • Patent number: 9314450
    Abstract: The invention relates to pharmaceutical compositions comprising: (a) at least one angiotensin receptor blocker or a pharmaceutically acceptable salt thereof, and (b) at least one chemokine receptor pathway inhibitor or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising: (a) at least one angiotensin receptor blocker or a pharmaceutically acceptable salt thereof; and (b) at least one chemokine receptor pathway inhibitor or a pharmaceutically acceptable salt thereof which inhibits a component of the chemokine receptor pathway other than the chemokine receptor. Oral sustained release pharmaceutical compositions comprising the pharmaceutical composition, as well as injectable sustained release pharmaceutical compositions comprising the pharmaceutical composition are described. The invention further relates to tablets, capsules, injectable suspensions, and compositions for pulmonary or nasal delivery comprising the pharmaceutical composition.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: April 19, 2016
    Assignee: DIMERIX BIOSCIENCE PTY LTD.
    Inventors: Kevin D. G. Pfleger, Elizabeth McCall, James Williams
  • Patent number: 9295255
    Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: March 29, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Seitz, Jurgen Benting, Ulrike Wachendorff-Neumann
  • Patent number: 9243001
    Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: January 26, 2016
    Assignee: Epizyme, Inc.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • Patent number: 9179678
    Abstract: The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein A1, A2, A3, A4, A5, X, R1, R2 and R6 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), and to their use for controlling weeds, in particular in crops of useful plants.
    Type: Grant
    Filed: March 27, 2013
    Date of Patent: November 10, 2015
    Assignee: Syngenta Limited
    Inventors: Glynn Mitchell, Olivia Anabelle Sageot
  • Patent number: 9173849
    Abstract: The present invention provides a solid preparation containing compound (I) or a salt thereof, a pH control agent and a calcium antagonist, which is superior in the dissolution property, stability and the like.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: November 3, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kazuhiro Hirata, Junya Nomura, Yutaka Tanoue
  • Patent number: 9102622
    Abstract: Disclosed are compounds of formula R—X—Y that may be used to inhibit the action of fatty acid amide hydrolase (FAAH). Inhibition of fatty acid amide hydrolase (FAAH) will slow the normal degradation and inactivation of endogenous cannabinoid ligands by FAAH hydrolysis and allow higher levels of those endogenous cannabinergic ligands to remain present. These higher levels of endocannabinoid ligands provide increased stimulation of the cannabinoid CB1 and CB2 receptors and produce physiological effects related to the activation of the cannabinoid receptors. They will also enhance the effects of other exogenous cannabinergic ligands and allow them to produce their effects at lower concentrations as compared to systems in which fatty acid amide hydrolase (FAAH) action is hot inhibited. Thus, a compound that inhibits the inactivation of endogenous cannabinoid ligands by fatty acid amide hydrolase (FAAH) may increase the levels of endocannabinoids and, thus, enhance the activation of cannabinoid receptors.
    Type: Grant
    Filed: July 27, 2007
    Date of Patent: August 11, 2015
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
  • Patent number: 9078446
    Abstract: Use of N-(tetrazol-4-yl)- or N-(triazol-3-yl)arylcarboxamides of formula (I) or salts thereof for controlling unwanted plants in areas of transgenic crop plants being tolerant to HPPD inhibitor herbicides by containing one or more chimeric gene(s) comprising (I) a DNA sequence encoding hydroxyphenylpyruvate dioxygenase (HPPD) derived from a member of a group of organisms consisting of (a) Avena, (b) Pseudomonas, (c) Synechococcoideae, (d) Blepharismidae, (e) Rhodococcus, (f) Picrophilaceae, (g) Kordia, or (II) comprising one or more mutated DNA sequences of HPPD encoding genes of the before defined organisms.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: July 14, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Fabien Poree, Andreas Almsick, Ralf Braun, Bernd Laber, Ruediger Hain
  • Patent number: 9073891
    Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: July 7, 2015
    Assignee: Imago Pharmaceuticals, Inc.
    Inventors: Hing L. Sham, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
  • Patent number: 9066936
    Abstract: The present invention provides a solid pharmaceutical composition containing compound (I) having an angiotensin II receptor antagonistic action and defined in the specification and a pH control agent, which composition is superior in the stability and dissolution property of compound (I).
    Type: Grant
    Filed: March 26, 2008
    Date of Patent: June 30, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shuji Yoneyama, Yutaka Tanoue
  • Patent number: 9056844
    Abstract: A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.
    Type: Grant
    Filed: November 15, 2011
    Date of Patent: June 16, 2015
    Assignee: Eli Lilly and Company
    Inventors: Bruce Anthony Dressman, Mark Donald Chappell, Adam Michael Fivush, Charles Howard Mitch, Paul Leslie Ornstein, Eric George Tromiczak, Tatiana Natali Vetman
  • Patent number: 9040569
    Abstract: The present invention provides novel crystalline polymorphic forms of MDT-637, in particular, crystalline polymorphic forms with physicochemical properties specifically suited for drug production, amorphous formation, composite form, and methods of preparation thereof. The novel polymorphs described herein are useful for the treatment of respiratory disease, such as disease caused by respiratory syncytial virus.
    Type: Grant
    Filed: June 28, 2013
    Date of Patent: May 26, 2015
    Assignee: MICRODOSE THERAPEUTX
    Inventors: Robert O. Cook, Eugene R. Reynolds, Boris Shekunov, Siead I. Zegar
  • Publication number: 20150141464
    Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit cdk5 -mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
    Type: Application
    Filed: November 20, 2012
    Publication date: May 21, 2015
    Inventors: Amy S. RIPKA, Jeffrey O. SAUNDERS
  • Publication number: 20150133378
    Abstract: A method for identifying a kidney transplant recipient at an increased risk of developing interstitial fibrosis or tubular atrophy which comprises obtaining a post-transplant urine sample from the kidney transplant recipient; measuring the level of clusterin in the urine sample; comparing the level of clusterin in the patient sample to the level of clusterin in a control sample from the urine of a non-fibrotic kidney transplant recipient; diagnosing a kidney transplant recipient with a clusterin level that is significantly higher than the clusterin level in the control as being at an increased risk of developing interstitial fibrosis or tubular atrophy.
    Type: Application
    Filed: April 17, 2013
    Publication date: May 14, 2015
    Inventors: Barbara Murphy, Philip J. O'Connell
  • Publication number: 20150133414
    Abstract: It was determined whether SNPs in SLC4A5 are associated with salt sensitivity of blood pressure (BP). Subjects consumed an isocaloric constant diet with a randomized order of 7 days low Na+ (10 mmol/d) and 7 days high Na+ (300 mmol/d) intake. Salt sensitivity was defined as a ?7 mm Hg increase in mean arterial pressure (MAP). 35 polymorphisms in 17 candidate genes were assayed. Association analyses with salt sensitivity revealed three variants that associated with salt sensitivity, two in SLC4A5 (rs7571842, rs10177833; P<0.001), and one in GRK4 (rs1801058; P=0.020). Paradoxical changes in blood pressure in response to changes in salt intake were also found associated with a SNP for DRD2 (rs6276). In conclusion, SLC4A5 variants are strongly associated with salt sensitivity of BP in Caucasian and a DRD2 SNP is a marker for paradoxical response to salt intake.
    Type: Application
    Filed: April 22, 2013
    Publication date: May 14, 2015
    Applicant: University of Virginia Patent Foundation
    Inventors: Robin A. Felder, Robert M. Carey, John E. Jones, Pedro A. Jose, Scott M. Williams
  • Publication number: 20150133500
    Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: and pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein W1, W2, W3, W4, U, G, m, R1, and R2 are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II to V as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 14, 2015
    Inventors: Laykea Tafesse, Jiangchao Yao, Xiaoming Zhou
  • Publication number: 20150126568
    Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing hypertension and diabetic kidney disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of diabetes related renal complications, hypertension, albuminuria, Heart Diseases, ESRD, Kidney GFR complications, Vascular Disease, Ventricular Septal Defect, vascular dilation, high blood pressure, congestive heart failure (CHF), post-myocardial infarction (MI).
    Type: Application
    Filed: August 18, 2013
    Publication date: May 7, 2015
    Inventor: Mahesh Kandula
  • Patent number: 9023874
    Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: May 5, 2015
    Assignee: Merial, Inc.
    Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
  • Publication number: 20150119329
    Abstract: The present invention is directed to a composition for the treatment or prevention of cerebral malaria that comprises an angiotensin receptor type-2 agonist and an antimalaria drug. The present invention is further directed to methods for treating and preventing cerebral malaria that involve administering an angiotensin receptor type-2 agonist and/or an angiotensin receptor type-1 antagonist.
    Type: Application
    Filed: April 16, 2013
    Publication date: April 30, 2015
    Applicant: NEW YORK UNIVERSITY
    Inventors: Ana Maria Rodriguez Fernandez, Julio Gallego-Delgado
  • Publication number: 20150105392
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Patent number: 9006454
    Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: April 14, 2015
    Assignee: Merck Serono S.A.
    Inventors: Siva Sanjeeva Rao Thunuguntla, Hosahalli Subramanya, Satish Reddy Kunnam, Sekhar Reddy Sanivaru Vijay, Chakrapani Bingi, Raviraj Kusanur, Matthias Schwarz, Michael Arlt
  • Publication number: 20150099730
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.
    Type: Application
    Filed: September 6, 2013
    Publication date: April 9, 2015
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Peter J. Connolly
  • Patent number: 8993614
    Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2, R3 and R4 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: March 31, 2015
    Assignee: F. Hoffmann-La Roche AG
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Binh Thanh Vu, Chunlin Zhao, Daniel Fishlock
  • Publication number: 20150087512
    Abstract: The subject invention is directed toward antimicrobial agents and methods of treating and preventing infection by pathogenic microorganisms and endophytic microorganisms in a plant through the use of SecA inhibitors.
    Type: Application
    Filed: September 26, 2014
    Publication date: March 26, 2015
    Inventors: Nian WANG, Nagaraju AKULA
  • Publication number: 20150087617
    Abstract: The invention provides indole and indoline derivatives and slats thereof, compositions comprising them and uses thereof for the treatment of diseases and disorders.
    Type: Application
    Filed: April 2, 2013
    Publication date: March 26, 2015
    Inventors: Abraham Nudelman, Marta Weinstock-Rosin
  • Patent number: 8987315
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: December 29, 2010
    Date of Patent: March 24, 2015
    Assignee: Innocrin Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
  • Publication number: 20150080412
    Abstract: The invention disclosed herein is directed to compounds of Formula (I) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula (I), or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a of a therapeutically effective amount of a selective PPAR? antagonist.
    Type: Application
    Filed: March 7, 2013
    Publication date: March 19, 2015
    Applicant: INCEPTION 2, INC.
    Inventors: Nicholas Simon Stock, Austin Chih-Yu Chen, Yalda Mostofi Bravo, Jason Duarte Jacintho, Jill Melissa Baccei, Brian Andrew Stearns, Ryan Christopher Clark, Yen Pham Truong
  • 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: 8980920
    Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: March 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Patent number: 8981110
    Abstract: The present invention provides novel process for preparation of olmesartan medoxomil (I) substantially free of olmesartan acid impurity (II) comprising, reacting trityl olmesartan medoxomil (III) with acid, filtering the precipitate of trityl alcohol, subjecting the filtrate to agitated thin film drying and recovering olmesartan medoxomil (I).
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: March 17, 2015
    Assignee: Lupin Limited
    Inventors: Rajendra Vishwanath Firke, Ujjwal Komalsing Sisodiya, Chandrakant Shriram Bhangale, Radhakrishna Bhikaji Shivdavkar, Himanshu Madhav Godbole, Girij Pal Singh
  • Patent number: 8975288
    Abstract: A compound or its pharmaceutically acceptable salt, as well as a pharmaceutical, composition containing that compound or salt dissolved or dispersed in a pharmaceutically acceptable carrier, and a method of using that compound or salt in an antibacterial treatment. A contemplated compound corresponds in structure to structural Formula I or a pharmaceutically acceptable salt of that compound, wherein V is O or NR9, Y is halogen, OR10, C1-C4 hydrocarbyl or NHR10, Z is NR2—X—R1 or CH2—R8, n is 1-6, X is H, S(O)2, C(O), C(O)NR7, C(NH)NR7 or C(O)O, and R1, R2, R7, R8, R9 and R10 are defined within.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: March 10, 2015
    Assignee: The Penn State Research Foundation
    Inventors: Kenneth Charles Keiler, John Nandwa Alumasa
  • Publication number: 20150065506
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Application
    Filed: August 13, 2014
    Publication date: March 5, 2015
    Applicant: ROCHE PALO ALTO LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Publication number: 20150065543
    Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: October 23, 2014
    Publication date: March 5, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson