Chalcogen Or Nitrogen Bonded Directly To The Pyrazole Ring By Nonionic Bonding Patents (Class 514/407)
  • Patent number: 8778837
    Abstract: The invention relates to the novel use of known active substance combinations which consist firstly of 3,4-dichloro-2?-cyano-1,2-thiazole-5-carboxanilide, of the formula which is known, and secondly further known insecticidal active substances, for controlling animal pests, especially arthropods, in particular insects.
    Type: Grant
    Filed: November 27, 2008
    Date of Patent: July 15, 2014
    Assignee: Bayer CropScience AG
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Heike Hungenberg, Wolfgang Thielert
  • Publication number: 20140193347
    Abstract: The present invention relates to pre-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 preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. 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: September 4, 2013
    Publication date: July 10, 2014
    Applicant: CAMURUS AB
    Inventors: Krister THURESSON, Fredrik TIBERG, Markus JOHANSSON, Ian HARWIGSSON, Fredrik JOABSSON, Markus JOHNSSON
  • Publication number: 20140193472
    Abstract: The present invention relates to microcapsules, formulations comprising such microcapsules and to methods of combating phytopathogenic pests in paddy rice fields based on such microcapsules.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 10, 2014
    Applicant: BASF SE
    Inventors: Christian Sowa, Gerhard Peter Dohmen, Martin Obermann, Nadine Riediger, Kristin Klappach, Manuel Schmitt, Reinhard Stierl
  • Patent number: 8772328
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: October 22, 2013
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ann E. Weber
  • Patent number: 8765791
    Abstract: The present invention relates to methods for treating cancer by administering a therapeutically effective amount of compound of formula (I), such as selective NPY5R antagonist MK-0557 (trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H), 1?-cyclohexane]-4?-carboxamide), or a pharmaceutically acceptable salt thereof, to a subject in need thereof The methods can further comprise administering a chemotherapeutic agent to the subject in need thereof.
    Type: Grant
    Filed: March 10, 2009
    Date of Patent: July 1, 2014
    Assignee: University Health Network
    Inventor: Guohua Pan
  • Patent number: 8765748
    Abstract: The present invention is directed to a compound is represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: July 1, 2014
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Bryan T. Forrest, Radoslaw Laufer, Miklos Feher, Peter Brent Sampson, Guohua Pan, Sze-Wan Li, Yong Liu
  • Publication number: 20140179733
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: ChemoCentryx, Inc.
    Inventors: Xi Chen, Dean R. Dragoli, Pingchen Fan, Juan C. Jaen, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
  • Publication number: 20140171420
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 19, 2014
    Applicant: ChemoCentryx, Inc.
    Inventors: Xi Chen, Pingchen Fan, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang, Dean Dragoli
  • Publication number: 20140171469
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: July 3, 2013
    Publication date: June 19, 2014
    Applicant: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • Patent number: 8754115
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: June 17, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Jeffrey Keith Long, Paula Louise Sharpe, Amy X Ding
  • Publication number: 20140162997
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, ring A, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: June 12, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Mark Wall, Nalin Subasinghe, Zhihua Sui, Christopher Flores
  • Patent number: 8748341
    Abstract: The present invention relates to synergistic mixtures comprising, as active components, chlorfenapyr as insecticidal compound I and a fungicidal compound II selected from the group of azoxystrobin, coumethoxystrobin, coumoxystrobin, dimoxystrobin, enestroburin, fluoxastrobin, kresoxim-methyl, metominostrobin, orysastrobin, pico-xystrobin, 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)-phenyl)-2-methoxyimino-N-methyl-acetamide.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: June 10, 2014
    Assignee: BASF SE
    Inventors: Markus Gewehr, Egon Haden, Lutz Brahm
  • Patent number: 8748339
    Abstract: The present invention relates to a composition, comprising a 5-amino-3-oxo-2,3-dihydro-pyrazole of the formula I as defined in the claims and the description and at least one active compound II selected from groups A) to I) in a synergistically effective amount.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: June 10, 2014
    Assignee: BASF SE
    Inventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Egon Haden
  • Publication number: 20140155452
    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: Application
    Filed: February 5, 2014
    Publication date: June 5, 2014
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Mark Spyvee, Takashi Satoh, Jonathan Eric Carlson
  • Patent number: 8741809
    Abstract: The present invention relates to a novel liquid formulation for crop protection which comprises a) pyraclostrobin; b) at least one organic solvent S1 with a water solubility of less than 2 g/l at 20° C.; c) at least one organic solvent S2 with a water solubility of at least 2 g/l at 20° C., where S2 comprises at least one solvent S2.1 with a water solubility of more than 200 g/l at 20° C. and optionally at least one solvent S2.2 with a water solubility of 2 to 200 g/l at 20° C.; d) at least one anionic surface-active substance SA1; e) at least one nonionic surface-active substance SA2; and f) water. The invention also relates to the use of the crop protection formulation for treatment of plants and seed, and to corresponding methods.
    Type: Grant
    Filed: October 9, 2009
    Date of Patent: June 3, 2014
    Assignee: BASF SE
    Inventors: Ulrike Troppmann, Wolfgang Meier, Guenter Oetter, Ulrich Steinbrenner, Tatjana Levy, Jurith Montag, Tanja Brunner, Reiner Weiler
  • Patent number: 8735431
    Abstract: The invention relates to novel insecticidal active compound combinations comprising, firstly, anthranilamides and, secondly, further insecticidally active compounds as defined in the description, which combinations are highly suitable for controlling animal pests, such as insects.
    Type: Grant
    Filed: November 20, 2004
    Date of Patent: May 27, 2014
    Assignee: Bayer CropScience AG
    Inventors: Christian Funke, Reiner Fischer, Rüdiger Fischer, Heike Hungenberg, Wolfram Andersch, Wolfgang Thielert, Anton Kraus
  • Patent number: 8735321
    Abstract: An object of the present invention is a process for the preparation of particles which comprise two agrochemical active ingredients in amorphous form, where a melt comprising the two molten agrochemical active ingredients is emulsified in an aqueous solution and cooled. A further object is the use of an agrochemical active ingredient for inhibiting the crystallization of another agrochemical active ingredient in a preparation process for particles which comprise the two agrochemical active ingredients in amorphous form, where a melt comprising the two molten agrochemical active ingredients is emulsified in an aqueous solution and cooled. A further object is particles which comprise two agrochemical active ingredients in amorphous form. The use in plant protection is also described.
    Type: Grant
    Filed: May 6, 2009
    Date of Patent: May 27, 2014
    Assignee: BASF SE
    Inventors: Ulrike Troppmann, Winfried Mayer, Sebastian Koltzenburg, Rafel Israels, Andreas Bauder, Ulf Schlotterbeck
  • Publication number: 20140142142
    Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, 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 animal's skin, preferably localized over a small surface area.
    Type: Application
    Filed: January 27, 2014
    Publication date: May 22, 2014
    Applicant: Sergeant's Pet Care Products, Inc.
    Inventor: Larry Nouvel
  • Publication number: 20140140973
    Abstract: This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention further relates to a bezoxazinone compound of Formula 10 wherein R4 through R8 are as defined in the disclosure, useful for preparation of a compound of Formula I.
    Type: Application
    Filed: January 27, 2014
    Publication date: May 22, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: GEORGE PHILIP LAHM, Stephen Frederick McCann, Kanu Maganbhai Patel, Thomas Paul Selby, Thomas Martin Stevenson
  • Publication number: 20140142156
    Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.
    Type: Application
    Filed: December 12, 2013
    Publication date: May 22, 2014
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Helen E. BLACKWELL, Christine E. McINNIS
  • Patent number: 8722577
    Abstract: The present invention relates to a composition containing (A) at least one specific carbamate fungicide, (B) at least one specific insecticide and optionally (C) at least one azole, the use of this composition for improving plant health and a method for improving plant health by treating a plant, its propagules or the locus where the plant is growing or is to grow with the above composition.
    Type: Grant
    Filed: February 5, 2008
    Date of Patent: May 13, 2014
    Assignee: BASF SE
    Inventors: Dirk Voeste, Egon Haden, Marco-Antonio Tavares-Rodrigues, Edson Begliomini
  • Publication number: 20140128435
    Abstract: The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R4, R5, R6 and R7 are as defined in the specification; or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
    Type: Application
    Filed: January 10, 2014
    Publication date: May 8, 2014
    Applicant: KARO BIO AB
    Inventors: Joakim Löfstedt, Xiongyu Wu, Lars Krüger
  • Publication number: 20140128406
    Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or x-N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.
    Type: Application
    Filed: June 27, 2012
    Publication date: May 8, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Fredrik Emil Malcolm Cederbaum
  • Publication number: 20140128397
    Abstract: The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells.
    Type: Application
    Filed: January 20, 2012
    Publication date: May 8, 2014
    Inventors: John Irwin, Patrick Sutphin, Denise Chan, Sandra Turcotte, Amato Giaccia, Edwin Lai, Olga Razorenova, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Raymond Tabibiazar
  • Publication number: 20140120069
    Abstract: The present invention describes novel amphoteric materials based on crosslinked hyaluronic acid, according to the general formula (I), and a method of preparation of said materials. Further, the invention relates to the material containing entrapped active agents (e.g. drugs, growth factors etc.) and a method of preparation thereof. Moreover, the present invention relates to the use of said materials for controlled release systems, in tissue engineering, wound dressing or tissue regeneration.
    Type: Application
    Filed: April 19, 2012
    Publication date: May 1, 2014
    Applicant: CONTIPRO BIOTECH S.R.O.
    Inventors: Gloria Huerta-Angeles, Drahomira Chladkova, Radovan Buffa, Sofiane Kettou, Vladimir Velebny
  • Publication number: 20140121103
    Abstract: The present invention relates to synergistic mixtures comprising at least one compound I and at least one active compound II as defined herein and to the use of these mixtures for combating phytopathogenic fungi, and to seeds coated with at least one such mixture. The invention also relates methods for combating harmful fungi using such mixtures.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 1, 2014
    Applicant: BASF SE
    Inventors: Nadege Boudet, Wassilios Grammenos, Jochen Dietz, Egon Haden, Richard Riggs, Bernd Müller, Jan Klaas Lohmann, Jurith Montag, Ian Robert Craig
  • Publication number: 20140121184
    Abstract: Insecticidal compositions have at least one active agent and at least one insecticide. The active agent can include perilla oil, a component found in perilla oil, or a perillaldehyde or carvone analog. The insecticide can include a pyrethrum, pyrethrin, pyrethroid, neonicotinoid, chlofenapyr, ethiprole, sulfoxoflor, carbamate, organophosphate, or organochlorine. Methods for controlling insects include contacting an insect with an effective amount of a composition described in this specification. Modified plants that produce an active agent can be contacted with an insecticide.
    Type: Application
    Filed: January 7, 2014
    Publication date: May 1, 2014
    Applicant: Clarke Mosquito Control Products, Inc.
    Inventors: Michael Dean Willis, Marie Elizabeth Saunders, Darryl Ramoutar, Joanna Maria Szymczyk, Frances Nita Krenick, Andrea Rohrbacher
  • Patent number: 8710053
    Abstract: A plant disease control composition comprising a carboxamide compound represented by following formula (I), wherein R1 represents a hydrogen atom or a methyl group, and R2 represents a methyl group, a difluoromethyl group or a trifluoromethyl group, and one or more QoI compounds selected from group (A) consisting of dimoxystrobin, azoxystrobin, fluoxastrobin, pyraclostrobin, kresoxim-methyl, picoxystrobin, trifloxystrobin and N-methyl-alpha-methoxyimino-2-[(2,5-dimethylphenoxy)methyl]phenylacetamide is provided by the present invention, and this composition has excellent effect for controlling a plant disease.
    Type: Grant
    Filed: April 25, 2011
    Date of Patent: April 29, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Yuichi Matsuzaki
  • Patent number: 8703649
    Abstract: The present invention relates to formulation comprising at least (i) two pesticidal compounds A and B dissolved in a lactic acid ester and wherein a) both A and B have melting points below 900 C b) both A and B are selected from the following list: pyraclos-trobin, metalaxyl, mefenoxam, trifloxystrobin, imazalil, pro-chloraz and ipconazole with the proviso that A is different from B (ii) at least one pesticidal compound C present in solid particles, and having a melting point of 900 C and above, and to their use as seed treatment formulation as well as their use for plant protection, including seed and crop protection.
    Type: Grant
    Filed: July 20, 2010
    Date of Patent: April 22, 2014
    Assignee: BASF SE
    Inventors: Rafel Israels, Katharine Klamczynski, Marco Kuhns, Ulf Schlotterbeck
  • Publication number: 20140107111
    Abstract: The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat type-2 diabetes-associated pain and related symptoms.
    Type: Application
    Filed: May 18, 2012
    Publication date: April 17, 2014
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Jose Miguel Vela Hernandez, Maria Isabel Martin Fontelles
  • Publication number: 20140107070
    Abstract: This disclosure features fungicidal combinations that include a paraffinic oil and an emulsifier. The combinations can further include one or more of the following: pigments, silicone surfactants, anti-settling agents, conventional fungicides such as demethylation inhibitors (DMI) and quinone outside inhibitors (Qol) and water. The fungicidal combinations are used for controlling infection of a crop plant by a fungal pathogen.
    Type: Application
    Filed: June 4, 2012
    Publication date: April 17, 2014
    Applicant: SUNCOR ENERGY INC.
    Inventors: Michael Fefer, Jun Liu
  • Publication number: 20140105839
    Abstract: The present invention relates to a compound of the following formula (I): as well as its process of preparation, pharmaceutical and cosmetics composition comprising it and use thereof, notably as an inhibitor of the sodium-dependent glucose co-transporter, such as SGLT1, SGLT2 and SGLT3, in particular in the treatment or prevention of diabetes, and more particularly type-II diabetes, diabetes-related complications, such as arthritis of the lower extremities, cardiac infarction, renal insufficiency, neuropathy or blindness, hyperglycemia, hyperinsulinemia, obesity, hypertriglyceridemia, X syndrome and arteriosclerosis, as well as for its use as an anticancer, anti-infective, anti-viral, anti-thrombotic or anti-inflammatory drug, or for lightening, bleaching, depigmenting the skin, removing blemishes from the skin, particularly age spots and freckles, or preventing pigmentation of the skin.
    Type: Application
    Filed: May 29, 2012
    Publication date: April 17, 2014
    Applicant: TF-CHEM
    Inventors: Geraldine Deliencourt-Godefroy, Lenaig Lopes
  • Publication number: 20140107165
    Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, 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 animal's skin, preferably localized over a small surface area.
    Type: Application
    Filed: November 22, 2013
    Publication date: April 17, 2014
    Applicant: Sergeant's Pet Care Products, Inc.
    Inventor: Larry Nouvel
  • Publication number: 20140106965
    Abstract: The present invention relates to a composition comprising a water-insoluble pesticide and an alkoxylated polyalkyleneimine. The invention furthermore relates to a method of preparing this composition; to the use of this composition for dispersing agrochemical active substances; 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 the 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 furthermore to seed comprising the composition.
    Type: Application
    Filed: May 21, 2012
    Publication date: April 17, 2014
    Applicant: BASF SE
    Inventors: Gerhard Schnabel, Paul Klingelhoefer
  • Patent number: 8697696
    Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: April 15, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Stephen Deems Gabriel, Andrew Thomas
  • Publication number: 20140100258
    Abstract: Invented is a method of treating cardiovascular disease/injury, in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a non-peptide TPO receptor agonist to such mammal.
    Type: Application
    Filed: December 9, 2013
    Publication date: April 10, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Connie L. ERICKSON-MILLER, Julian JENKINS
  • Publication number: 20140100211
    Abstract: Pyrrolidine derivatives of the formula and their use as medicaments for the treatment of obesity and type 2 diabetes.
    Type: Application
    Filed: October 1, 2013
    Publication date: April 10, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
  • Patent number: 8691862
    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: April 27, 2011
    Date of Patent: April 8, 2014
    Assignee: Makhteshim Chemical Works Ltd.
    Inventor: Sharona Zamir
  • Patent number: 8686018
    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: March 12, 2013
    Date of Patent: April 1, 2014
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Mark Spyvee, Takashi Satoh, Jonathan Eric Carlson
  • Publication number: 20140088094
    Abstract: The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroquinoline and related compounds are provided.
    Type: Application
    Filed: November 8, 2011
    Publication date: March 27, 2014
    Applicants: Merck Sharp & Dohme Corp., Lycera Corporation
    Inventors: Gary D. Glick, Peter L. Toogood, Arthur Glenn Romero, Chad A. Van Huis, Thomas Daniel Aicher, Carl Kaub, Matthew N. Mattson, William David Thomas, Karin Ann Sttein, Erik Krogh-Jespersen, Zhan Wang
  • Publication number: 20140088165
    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: Application
    Filed: December 2, 2013
    Publication date: March 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Yuki Iwaki, Toshio KAWANAMI, Gary Michael Ksander, Muneto Moji
  • Publication number: 20140088153
    Abstract: The invention relates to compounds of the general formula (I) in which the radicals A1, A2, A3, A4, L, Q, R1, T and W have the meaning given in the description and to the use of the compounds for controlling animal pests. The invention furthermore relates to processes and intermediates for preparing the compounds of formula (I).
    Type: Application
    Filed: March 12, 2012
    Publication date: March 27, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Michael Maue, Isabelle Adelt, Markus Heil, Peter Jeschke, Tobias Kapferer, Friedrich August Muehlthau, Alexander Sudau, Olga Malsam, Peter Loesel, Arnd Voerste, Ulrich Goergens
  • Publication number: 20140088105
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 27, 2014
    Applicant: NOVARTIS AG
    Inventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
  • Publication number: 20140088158
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK
  • Publication number: 20140080883
    Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, 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 animal's skin, preferably localized over a small surface area.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 20, 2014
    Applicant: Sergeant's Pet Care Products, Inc.
    Inventor: Larry Nouvel
  • Publication number: 20140080702
    Abstract: The present invention relates to a composition comprising an agrochemical active substance and a copolymer which comprises an N-vinylcarboxamide and a diallyldialkylammonium salt incorporated into the polymer. The invention furthermore relates to a method of preparing this composition; to the use of this composition for dispersing agrochemical active substances; 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 the 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 furthermore to seed comprising the composition.
    Type: Application
    Filed: May 24, 2012
    Publication date: March 20, 2014
    Applicant: BASF SE
    Inventors: Gerhard Schnabel, Ruth Wirschem, Paul Klingelhoefer, Lucelena Patricio Cardoso
  • Publication number: 20140080884
    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: Application
    Filed: June 25, 2012
    Publication date: March 20, 2014
    Applicants: Merck Sharp & Dohme Ltd., Merck Sharp & Dohme Corp.
    Inventors: Itzia Arroyo, Davida Krueger, Ping Chen, Aaron Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
  • Patent number: 8673901
    Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein X1, R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds are useful as potassium ion channel inhibitors.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: March 18, 2014
    Assignee: Xention Limited
    Inventors: Mushtaq Mulla, Derek Edward John, Richard John Hamlyn, Sasha Louise Garrett, Basil Hartzoulakis, David Madge, John Ford
  • Patent number: 8664257
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 26, 2011
    Date of Patent: March 4, 2014
    Assignee: Sanofi
    Inventors: Sven Ruf, Josef Pernerstorfer, Thorsten Sadowski, Georg Horstick, Herman Schreuder, Christian Buning, Thomas Olpp, Bodo Scheiper, Klaus Wirth
  • Patent number: 8658686
    Abstract: Novel therapeutic agents for myeloma are provided. A therapeutic agent for multiple myeloma containing a pyrazole compound represented by the formula (1): wherein R1 is C1-C6 alkyl, C1-C6 alkyl substituted with R17, C1-C6 haloalkyl, phenyl, phenyl substituted with a R11's or the like, R2 is a hydrogen atom, C1-C6 alkyl, phenyl or phenyl optionally substituted with e R21's or the like, R3 is a hydrogen atom or the like, X is a single bond or —(CR6R7)n—, each of R4 and R5 is independently C1-C6 alkyl or the like, R6 and R7 are hydrogen atoms or C1-C6 alkyl, R8 is phenyl, phenyl optionally substituted with k R81's or the like, a tautomer of the compound or a pharmaceutically acceptable salt or solvate thereof, as an active ingredient.
    Type: Grant
    Filed: December 1, 2011
    Date of Patent: February 25, 2014
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Taito Nishino, Katsuaki Miyaji, Shunsuke Iwamoto, Takumi Mikashima, Koichiro Saruhashi, Yo Kishikawa