Chalcogen Or Nitrogen Bonded Directly To The Pyrazole Ring By Nonionic Bonding Patents (Class 514/407)
  • Patent number: 10676480
    Abstract: Methods of inhibiting the growth or metastasis of a cancer in a subject by inhibiting a Ral GTPase in the subject, and small molecule inhibitors of Ral GTPases useful in the methods of the invention. Pharmaceutical compositions containing the compounds of the invention, and methods of using the same.
    Type: Grant
    Filed: January 7, 2019
    Date of Patent: June 9, 2020
    Assignee: THE REGENTS OF THE UNIVERSITY OF COLORADO, a body corporate
    Inventors: Dan Theodorescu, Michael Fitzpatrick Wempe, David Ross, Chao Yan, Phillip Reigan
  • Patent number: 10646475
    Abstract: The present invention relates to a method for the treatment of cancer or an autoimmune disorder, comprising the administration of a serine hydroxymethyltransferase (SHMT) inhibitor, and in particular the administration of pyrazolopyran compounds of Formula (VI) as presently described, wherein the compounds are capable of inhibiting a mammalian SHMT, such as human SHMT1 and/or SHMT2. The treatment method further comprises the optional administration of an additional agent as a rescue therapy to reduce toxicity, wherein said agent may be chosen from formate, a formate salt, folinic acid, formate ester, or leucovorin.
    Type: Grant
    Filed: March 10, 2016
    Date of Patent: May 12, 2020
    Assignee: The Trustees of Princeton University
    Inventors: Joshua D. Rabinowitz, Hahn Kim, Gregory S. Ducker, Jonathan M. Ghergurovich
  • Patent number: 10456358
    Abstract: This invention is directed to a pharmaceutical composition for drinking water administration comprising isoxazoline compounds of formula (I) and a polysorbate surfactant and diethylene glycol monoethyl ether (transcutol); and the use of the composition to treat or prevent parasite infestations of animals.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: October 29, 2019
    Assignee: Intervet Inc.
    Inventors: Anne Lehay, Annie Flochlay-Sigognault
  • Patent number: 10214515
    Abstract: An indole derivative as expressed by Formula (I), a preparation method thereof, a pharmaceutical salt, and use thereof as a therapeutic agent, especially as a FGFR inhibitor. Each substituent in Formula (I) has identical definition as specified in the specification.
    Type: Grant
    Filed: August 19, 2016
    Date of Patent: February 26, 2019
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Lei Chen, Dongliang Guan, Hua Bai, Xing Yan, Shuai Miao, Songsong Zhu
  • Patent number: 10202397
    Abstract: Methods of inhibiting the growth or metastasis of a cancer in a subject by inhibiting a Ral GTPase in the subject, and small molecule inhibitors of Ral GTPases useful in the methods of the invention. Pharmaceutical compositions containing the compounds of the invention, and methods of using the same.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: February 12, 2019
    Assignee: The Regents of the University of Colorado, a body corporate
    Inventors: Dan Theodorescu, Michael Fitzpatrick Wempe, David Ross, Chao Yan, Phillip Reigan
  • Patent number: 10167263
    Abstract: The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds.
    Type: Grant
    Filed: November 20, 2009
    Date of Patent: January 1, 2019
    Assignees: NORTHWESTERN UNIVERSITY, CAMBRIA PHARMACEUTICALS, INC.
    Inventors: Donald R. Kirsch, Radhia Benmohamed, Anthony C. Arvanites, Richard I. Morimoto, Tian Chen, Richard B. Silverman
  • Patent number: 10047076
    Abstract: The invention relates inter alia to halogen-substituted compounds of the general formula (I) in which the A1-A4, T, W, Q, R1 and Z1-Z3 radicals are as defined in the description. Also described are processes for preparing the compounds of the formula (I). The compounds according to the invention are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.
    Type: Grant
    Filed: April 1, 2015
    Date of Patent: August 14, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Michael Maue, Anne Decor, Thomas Bretschneider, Julia Johanna Hahn, Werner Hallenbach, Reiner Fischer, Hans-Georg Schwarz, Ulrich Goergens, Kerstin Ilg, Klaus Raming, Johannes Koebberling, Walter Huebsch, Andreas Turberg
  • Patent number: 9968589
    Abstract: Methods for treating a variety of diseases that comprises performing auricular anesthesia of various cranial nerves. A pharmaceutical composition is administered to an ear canal of a subject in need of such treatment, the composition including an analgesic and/or at least one anesthetic. Compositions useful in the taught methods are also provided.
    Type: Grant
    Filed: November 3, 2015
    Date of Patent: May 15, 2018
    Inventor: Thomas M Crews
  • Patent number: 9918471
    Abstract: 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 fluoxastrobin, trifloxystrobin, and picoxystrobin, provides synergistic control of selected fungi.
    Type: Grant
    Filed: December 29, 2014
    Date of Patent: March 20, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Greg Kemmitt, Olavo Correa da Silva, John T. Mathieson
  • Patent number: 9913473
    Abstract: The present invention relates to a novel crystalline modification of fipronil, to a process for the preparation of the same, to pesticidal and parasiticidal mixtures and compositions comprising said crystalline modification and to their use for combating pests and parasites.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: March 13, 2018
    Assignee: BASF SE
    Inventors: Heidi Emilia Saxell, Peter Erk, Claude Taranta, Thomas Kröhl, Gerhard Cox, Martin Sukopp, Gautam R. Desiraju, Rahul Banerjee, Prashant M. Bhatt
  • Patent number: 9822079
    Abstract: The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.
    Type: Grant
    Filed: January 26, 2017
    Date of Patent: November 21, 2017
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventor: Sharona Zamir
  • Patent number: 9695127
    Abstract: Disclosed herein are embodiments of a compound capable of treating HIV. In particular disclosed embodiments, the compound is capable of inhibiting Nef, such as by acting as antagonists of HIV Nef function. Also disclosed are embodiments of a method of making the compound, embodiments of a method of using the compound, and embodiments of a method of identifying HIV Nef antagonists. The disclosed compound may be used alone or in combination with other pharmacologically active agents in order to promote reducing drug resistance and/or cumulative toxicity.
    Type: Grant
    Filed: November 6, 2013
    Date of Patent: July 4, 2017
    Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
    Inventors: Thomas E. Smithgall, Lori Ann Emert-Sedlak, Billy W. Day, Jielu Zhao, Prema Chandrasekhar Iyer
  • Patent number: 9655365
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Grant
    Filed: November 19, 2014
    Date of Patent: May 23, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Noormohamed M. Niyaz, Negar Garizi, Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse, Asako Kubota, Paul R. LePlae, Jr., Daniel Knueppel, Christian T. Lowe, Dan Pernich, David A. Demeter, Timothy C. Johnson
  • Patent number: 9591854
    Abstract: The present invention relates to composition comprising a pesticide and an alkoxylate of the formula (I) as defined below. The invention further relates to said alkoxylate. The invention further relates to a method of preparing said composition by bringing the alkoxylate and the pesticide into contact. Finally, the invention relates to a method of controlling phytopathogenic fungi and/or undesired plant growth and/or undesired insect or mite attack and/or for regulating the growth of plants, wherein said composition is allowed to act on the respective pests, their environment or the crop plants to be protected from the respective pest, on the soil and/or on undesired plants and/or on the crop plants and/or on their environment; and to seed containing said composition.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: March 14, 2017
    Assignee: BASF SE
    Inventors: Murat Mertoglu, Rainer Berghaus, Andreas Kunst, Benedikt Crone, Christian Koenig
  • Patent number: 9580389
    Abstract: The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoro ethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: February 28, 2017
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventor: Sharona Zamir
  • Patent number: 9518060
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Grant
    Filed: October 3, 2014
    Date of Patent: December 13, 2016
    Assignee: PFIZER INC.
    Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
  • Patent number: 9457088
    Abstract: The subject matter disclosed herein is directed to stable, highly-effective topical formulations comprising permethrin, fipronil and a solvent system that is sufficient to solubilize these two active ingredients and limit degradation of fipronil to its sulfone, and their uses in topical applications on animals and the environment. Useful formulations comprise from about 30% to about 55% (w/w) permethrin and about 2 to 15% (w/w) fipronil and a solvent system that comprises N-methyl pyrrolidone and a glycol, glycol ether, glycol ester, fatty acid ester or neutral oil, wherein the N-methyl pyrrolidone and glycol, glycol ether, glycol ester, fatty acid ester or neutral oil are present in a weight:weight ratio of from about 1:2.0 to about 1:3.5, glycol, glycol ether, glycol ester, fatty acid ester or neutral oil to n-methyl pyrrolidone. These two actives when combined in the described amounts have been found to have unexpected enhanced repellent activity against stable fly.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: October 4, 2016
    Assignee: MERIAL, INC.
    Inventors: Mark David Soll, James Pate, Lisa A. Baker
  • Patent number: 9215873
    Abstract: The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoroethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.
    Type: Grant
    Filed: March 31, 2014
    Date of Patent: December 22, 2015
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventor: Sharona Zamir
  • Patent number: 9181262
    Abstract: Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
    Type: Grant
    Filed: October 6, 2014
    Date of Patent: November 10, 2015
    Assignees: Merck Sharp & Dohme Corp, Merck Sharp & Dohme Ltd.
    Inventors: Itzia Z. Arroyo, Davida Krueger, Ping Chen, Aaron J. Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
  • Patent number: 9169215
    Abstract: Provided herein are compounds of the formula (I), as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such pulmonary fibrosis.
    Type: Grant
    Filed: September 2, 2013
    Date of Patent: October 27, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: David Budd, Yimin Qian, Ryan Craig Schoenfeld, Achyutharao Sidduri
  • Patent number: 9155305
    Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) prothioconazole and (B) fluxapyroxad and optionally (C) a further fungicidally active compound. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops (e.g. cereals such as wheat, barley, rye, oats, millet and triticale; soya beans; rice; com/maize; oil seed rape including canola; beans, peas, peanuts; sugar beet, fodder beet, beetroot; potatoes; cotton), and to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Grant
    Filed: August 2, 2011
    Date of Patent: October 13, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY
    Inventor: Stephanie Gary
  • Patent number: 9051326
    Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form (I), in which the substituents are as defined in the specification; to compounds of formula (I) for use as androgen receptor modulators. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: June 9, 2015
    Assignee: NOVARTIS AG
    Inventors: Mark Gary Bock, Bharat Lagu, Chetan Pandit, Sanjita Sasmal, Thomas Ullrich
  • Publication number: 20150147282
    Abstract: The present invention relates to topical bioadhesive formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.
    Type: Application
    Filed: November 24, 2014
    Publication date: May 28, 2015
    Inventors: Fredrik JOABSSON, Margareta LINDEN, Krister THURESSON, Fredrik TIBERG
  • Publication number: 20150148373
    Abstract: The invention provides heterocyclic guanidine compounds that inhibit F1F0-ATPase, and methods of using heterocyclic guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 28, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood
  • Publication number: 20150148374
    Abstract: The present invention provides a compound of formula I: 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: Application
    Filed: June 27, 2013
    Publication date: May 28, 2015
    Applicant: NOVARTIS AG
    Inventors: Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
  • Patent number: 9040530
    Abstract: Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: May 26, 2015
    Assignee: PORTOLA PHARMACEUTICALS, INC.
    Inventors: Zhaozhong J. Jia, Brian Kane, Jack Rose, Shawn M. Bauer, Yonghong Song, Qing Xu, Anjali Pandey
  • Publication number: 20150141465
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 21, 2015
    Inventors: Calvin W. YEE, Zhe Li
  • Publication number: 20150141462
    Abstract: The present invention relates to pharmaceutical compositions comprising (a) a pharmaceutically effective amount of an mGluR5 positive allosteric modulator, derivative, prodrug or a pharmaceutically acceptable salt thereof; (b) a pharmaceutically effective amount of an agent selected from an NMDA partial agonist or a GlyT1 inhibitor, derivative, prodrug or a pharmaceutically acceptable salt thereof; and (c) a pharmaceutically acceptable carrier. The present invention also relates to methods for treating drug addiction and preventing a drug relapse in a patient.
    Type: Application
    Filed: June 11, 2013
    Publication date: May 21, 2015
    Inventor: M. Foster Olive
  • Patent number: 9034912
    Abstract: A stable liquid pharmaceutical formulation contains an N-phenylpyrazole derivative, a crystallization inhibitor/viscolizer, and a solvent/co-solvent system including a glycol ether solvent and at least one mono alkyl ester co-solvent; an improved topical veterinary applicator system; and the use of the formulation for the prevention and treatment of infestations with fleas and ticks.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: May 19, 2015
    Inventor: Jugal K. Taneja
  • Publication number: 20150133506
    Abstract: Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I): wherein: R1 is hydrogen, cyano, halogen, R8, formyl, —C(O)R8, —C(O)OR8, —C(O)NR9R10, or —C(S)NH2; R2 is R8 or —S(O)mR11; R3 is methyl, ethyl or C1-C4 haloalkyl; R4, R5 and R7 are independently hydrogen, halogen, alkyl, haloalkyl, cyano or nitro; R6 is halogen, alkyl, haloalkyl, alkoxy, haloalkyloxy, cyano, nitro, —C(O)R12, —S(O)nR12 or SF5; Z is a nitrogen atom or C—R13; R8 is alkyl, haloalkyl, cycloalkyl or halocycloalkyl; R9 is hydrogen, alkyl, haloalkyl or alkoxy; R10 is hydrogen, alkyl, haloalkyl or alkoxy; R11 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl or cycloalkyl; R12 is alkyl or haloalkyl; R13 is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy; m is 0, 1 or 2; and n is 0, 1 or 2; or a salt thereof, the method of making compounds of formula (I) and the use of these compounds against ectoparasites, endoparasites and pests.
    Type: Application
    Filed: July 8, 2014
    Publication date: May 14, 2015
    Applicant: AVENTIS AGRICULTURE
    Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Philip Reid Timmons, William Glenn Cawthorne, JR., Adalberto Perez de Leon
  • Patent number: 9029356
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 12, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Publication number: 20150126493
    Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Vladimir Simov, Willam D. Thomas, Peter L. Toogood, Chad A. Van Huis
  • Patent number: 9023884
    Abstract: The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.
    Type: Grant
    Filed: May 13, 2013
    Date of Patent: May 5, 2015
    Assignee: Adama Makhteshim Ltd.
    Inventor: Sharona Zamir
  • Publication number: 20150119439
    Abstract: The invention provides saturated acyl guanidine compounds that inhibit F1F0-ATPase, and methods of using saturated acyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: April 30, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood, Chad A. Van Huis
  • Publication number: 20150119243
    Abstract: The present invention relates to novel 1-methyl-pyrazole(thio)indanyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Application
    Filed: May 6, 2013
    Publication date: April 30, 2015
    Applicant: Bayer Cropscience AG
    Inventors: Simon Maechling, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Jean-Pierre Vors, Stephane Brunet, Helene Lachaise, Pierre Genix
  • Publication number: 20150111938
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Qiang YANG, Beth LORSBACH, Gregory T. WHITEKER, Carl DeAMICIS, Joseck M. MUHUHI
  • Patent number: 9012478
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: April 21, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • Patent number: 9012487
    Abstract: A compound having formula (I): wherein: R, A, R1 and R2, are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof, as Kinase inhibitors.
    Type: Grant
    Filed: March 2, 2007
    Date of Patent: April 21, 2015
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Tiziano Bandiera, Jay Aaron Bertrand, Paolo Pevarello, Ettore Perrone, Andrea Lombardi Borgia, Sten Christian Orrenius, Mauro Angiolini, Daniele Fancelli
  • Publication number: 20150105389
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Erik Dean RAAUM, Garrett Thomas POTTER, Tai Wei LY
  • Publication number: 20150099696
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed to compounds suitable for the treatment of Disease conditions such as hyperlipidemia.
    Type: Application
    Filed: June 26, 2012
    Publication date: April 9, 2015
    Applicant: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pandya, Sairam V.V.M. Kalapatapu
  • Publication number: 20150099766
    Abstract: The invention relates to compounds of the general formula (I), in which the radicals A1, A2, A3, A4, Lm, Q, R1, T and U have the meaning given in the description and to the use of the compounds for controlling animal pests. In addition, the invention relates to processes and intermediates for the preparation of the compounds according to formula (I).
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Michael MAUE, Isabelle ADELT, Wolfgang GIENCKE, Markus HEIL, Peter JESCHKE, Bernd-Wieland KRÜGER, Friedrich August MÜHLTHAU, Alexander SUDAU, Klaus RAMING, Ulrich EBBINGHAUS-KINTSCHER, Martin ADAMCZEWSKI, Arnd VOERSTE, Ulrich GÖRGENS, Tobias KAPFERER, Mark Wilhelm DREWES, Angela BECKER, Eva-Maria FRANKEN
  • Patent number: 9000024
    Abstract: The present invention provides compounds of Formula I: along with pharmaceutical compositions containing the same, and methods of use thereof in subjects in need of treatment.
    Type: Grant
    Filed: February 5, 2014
    Date of Patent: April 7, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Mark Spyvee, Takashi Satoh, Jonathan Eric Carlson
  • Patent number: 8993613
    Abstract: The invention provides an ectoparasiticidal formulation which comprises an ectoparasiticidal agent, preferably fipronil, as the pesticidally-active ingredient, together with a crystallization inhibitor selected from the group consisting of alkyl-substituted pyrrolidones, and optionally, one or more organic solvents and/or co-solvents. Preferably, the crystallization inhibitor is N-octyl pyrrolidone, and the organic solvent, if present, preferably comprises diethylene glycol monoethyl ether. The ectoparasiticidal formulation surprisingly yields a significantly enhanced speed of kill. Methods for manufacturing the formulation, as well as methods for treating animals infested with ectoparasites, are also disclosed.
    Type: Grant
    Filed: April 1, 2014
    Date of Patent: March 31, 2015
    Assignee: The Hartz Mountain Corporation
    Inventors: W. Lance Hemsarth, Keith Goldman, Ellen McGarvey
  • Publication number: 20150087511
    Abstract: The present invention relates to synergistic mixtures comprising, as active components one insecticidal compound I selected from the group of acrinathrin, allethrin, alpha-cypermethrin, beta-cypermethrin, bifenthrin, cycloprothrin, cyfluthrin, cypermethrin, cyphenothrin, deltamethrin, dimefluthrin, esfenvalerate, etofenprox, fenpropathrin, fenvalerate, flucythrinate, imiprothrin, permethrin, prallethrin, profluthrin, pyrethrin I, pyrethrin II, resmethrin, silafluofen, tau-fluvalinate, tetramethrin, theta-cypermethrin, tralomethrin, transfluthrin and zeta-cypermethrin; and one fungicidal compound II selected from the group of azoxystrobin, coumethoxystrobin, coumoxystrobin, dimoxystrobin, enestroburin, fluoxastrobin, kresoxim-methyl, metominostrobin, orysastrobin, picoxystrobin, pyraclostrobin, pyrametostrobin, pyraoxystrobin, pyribencarb, trifloxysstrobin, 2-(ortho-((2,5-Dimethylphenyl-oxymethylen)phenyl)-3-methoxy-acrylic acid methyl ester, 2-(2-(3-(2,6-dichlorophenyl)-1-methyl-allylideneaminooxymethyl)-phen
    Type: Application
    Filed: December 5, 2014
    Publication date: March 26, 2015
    Inventors: Markus GEWEHR, Egon HADEN, Lutz BRAHM
  • Publication number: 20150087684
    Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of fipronil and etofenprox as the active components, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the mammal's skin, preferably localized over a small surface area.
    Type: Application
    Filed: August 15, 2014
    Publication date: March 26, 2015
    Inventor: Larry Nouvel
  • Publication number: 20150087628
    Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
    Type: Application
    Filed: April 10, 2013
    Publication date: March 26, 2015
    Inventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
  • Patent number: 8987275
    Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: March 24, 2015
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael Gray, Wenjun Zhou, Xianming Deng
  • Publication number: 20150080398
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Erik Dean RAAUM, Garrett Thomas POTTER, Tai Wei LY
  • Publication number: 20150080397
    Abstract: Provided herein are pharmaceutically acceptable salts of 3,5-diaminopyrazoles, for example, pharmaceutically acceptable salts of compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: September 17, 2014
    Publication date: March 19, 2015
    Inventors: Tai Wei LY, Erik Dean RAAUM
  • Publication number: 20150080375
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Application
    Filed: October 14, 2014
    Publication date: March 19, 2015
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Monique Bodil Van Niel, Nicholas Charles Ray, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani, Andrew Peter Cridland, Christopher Hurley