Two Double Bonds Between Ring Members Of The Five-membered Hetero Ring (e.g., Pyrrole, Etc.) Patents (Class 514/427)
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Publication number: 20140031398Abstract: Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? and SO2NR?2, where R? is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted orType: ApplicationFiled: January 27, 2012Publication date: January 30, 2014Inventors: Alessio Moriconi, Gianluca Bianchini, Andrea Aramini, Laura Brandolini, Chiara Liberati, Silvia Bovolenta, Andrea Beccari, Simone Lorenzi
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Publication number: 20140024679Abstract: The present invention provides novel phenylcycloalkylmethylamine derivatives, and methods of preparing phenylcycloalkylmethylamine derivatives. The present invention also provides methods of using phenylcycloalkylmethylamine derivatives and compositions of phenylcycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.Type: ApplicationFiled: December 31, 2012Publication date: January 23, 2014Applicant: Reviva Pharmaceuticals, Inc.Inventor: Reviva Pharmaceuticals, Inc.
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Publication number: 20140004174Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.Type: ApplicationFiled: May 20, 2013Publication date: January 2, 2014Applicant: Pharmacyclics, Inc.Inventors: Erik VERNER, Sriram BALASUBRAMANIAN, Joseph J. BUGGY
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Publication number: 20130338209Abstract: The present invention provides a therapeutic compound of formula (I) and their pharmaceutically acceptable salts for the prevention and treatment of lipodystrophy caused because of HIV infection or combination therapy of HIV-1 protease inhibitors (Pis) and/or reverse transcriptase inhibitors (nRTIs) by neutralizing lipohypertrophy, lipoatrophy and metabolic abnormalities in HIV patient.Type: ApplicationFiled: January 30, 2012Publication date: December 19, 2013Applicant: CADILA HEALTHCARE LIMITEDInventors: Dhiraj Gambhire, Rajendrakumar Hariprasad Jani, Bipin Pandey, Kaushik Sata, Himanshu Kothari, Pankaj Ramanbhai Patel
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Patent number: 8609713Abstract: The invention relates to a series of substituted pyrrole derivatives, compositions comprising the same, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: May 7, 2010Date of Patent: December 17, 2013Assignee: AbbVie Inc.Inventors: Ramin Faghih, Gregory A. Gfesser, Christopher L. Lynch, Murali Gopalakrishnan, Sujatha Gopalakrishnan, John Malysz, Earl J. Gubbins, Rachid El Kouhen, Jinhe Li
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Patent number: 8604027Abstract: A method of contraception is provided which involves delivery of 21 to 27 consecutive days of a progestin in the absence of an estrogen or other steroidal compound, followed by 1 to 7 days without an effective amount of an active agent. Also described is a pharmaceutically useful kit to facilitate delivery of this regimen.Type: GrantFiled: May 3, 2010Date of Patent: December 10, 2013Assignee: Wyeth LLCInventors: Gary Sondermann Grubb, Ginger Dale Constantine
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Publication number: 20130310377Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: ApplicationFiled: December 20, 2012Publication date: November 21, 2013Applicant: Rhizen Phamaceuticals SAInventor: Rhizen Phamaceuticals SA
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Publication number: 20130303585Abstract: Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.Type: ApplicationFiled: January 26, 2012Publication date: November 14, 2013Applicants: UNIVERSITY OF ROCHESTER, TEMPLE UNIVERSITY-OF THE COMMONWEALTH SYSTEM OF HIGHER LEARNING, BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKAInventors: Paul M. Dunman, Patrick D. Olson, Wayne Childers
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Publication number: 20130296355Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: July 3, 2013Publication date: November 7, 2013Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20130281453Abstract: Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.Type: ApplicationFiled: October 21, 2011Publication date: October 24, 2013Applicant: The Scripps Research InstituteInventors: Benjamin Cravatt, Daniel Nomura, Jae W. Chang, Raymond E. Moellering, Dan Bachovehin, Weiwei Li
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Patent number: 8558009Abstract: The present invention relates to compounds of the general formula (I) their derivatives, their analogs, their tautomeric forms, their pharmaceutically acceptable salts, wherein all variables are as defined in the specification.Type: GrantFiled: April 25, 2011Date of Patent: October 15, 2013Assignee: Cadila Healthcare LimitedInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Barot, Saurin Khimshankar Raval, Preeti Saurin Raval, Sujay Basu
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Publication number: 20130261083Abstract: The invention relates to additives enhancing the activity of certain insecticides, to significantly increase the effect of such insecticides when applied to the exterior foliage of a plant, thus increasing the kill rate of feeding insects that are normally protected deep within other tissue structures of the plant.Type: ApplicationFiled: December 9, 2011Publication date: October 3, 2013Applicant: Akzo Nobel Chemicals International B.V.Inventors: James Lyle Hazen, Jinxia Susan Sun
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Patent number: 8530461Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: GrantFiled: December 14, 2012Date of Patent: September 10, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Bernd Nosse, Martin Fleck, Niklas Heine, Gerald Juergen Roth
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Publication number: 20130224114Abstract: The present invention relates to compounds and methods for imaging translocator protein (18 kDa) (TSPO) expression in a subject. This invention also relates to compounds and methods for the treatment of neurodegenerative disorders, inflammation or anxiety in a subject.Type: ApplicationFiled: March 25, 2013Publication date: August 29, 2013Applicant: The University of SydneyInventor: The University of Sydney
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Patent number: 8492379Abstract: The present invention relates to compounds and methods for imaging translocator protein (18 kDa) (TSPO) expression in a subject. This invention also relates to compounds and methods for the treatment of neurodegenerative disorders, inflammation or anxiety in a subject.Type: GrantFiled: December 2, 2008Date of Patent: July 23, 2013Assignee: The University of SydneyInventors: Michael Kassiou, Michelle Louise James, Christopher Andrew Luus
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Publication number: 20130172397Abstract: The invention relates to the use of a compound of general formula (I), wherein R1 and R2 are independently H or C1-C6 alkyl, or R1 and R2 are bound to one another forming an optionally substituted fused benzene ring, R3 is H, C1-C6 alkyl or —CH2—CH(NH2)—COOH and R4 is H, C1-C6 alkyl, or R4 represents (II) or (III) in the preparation of a medicinal product for treating and/or preventing congenital erythropoietic porphyria (CEP).Type: ApplicationFiled: August 5, 2011Publication date: July 4, 2013Applicant: CENTRO DE INVESTIGACIÓN COOPERATIVA EN BIOCIENCIAS-CIC bioGUNEInventors: Oscar Millet Aguilar-Galindo, Ana Laín Torre
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Publication number: 20130165494Abstract: 1,5-diaryl-2-alkylpyrrole-3-substituted nitro esters, of Formula (I) are provided. Such compounds are potent and selective COX-2 inhibitors which are able to release NO in concentrations that make it possible to counteract the side effects due to selective COX-2 inhibition, without giving rise to hypotensive effects. Formula (I) includes compounds wherein the groups R? and R? are: —H, —F, —Cl, —Br, —CH3, —CF3, —OCH3, —SCH3, R1 is methyl, ethyl, trifluoromethyl, hydroxymethyl, methoxymethyl and the substituent in position ?3 of the pyrrole ring is a chain, where the groups X, Y, Z, W and R2 are: X is a carbonyl or a group —(CHR3)—, Y is an oxygen atom or the group —NR3— and Z is a carbonyl or a group —(CHR3)—, or a [—CH(COOH)—] group, or a group —(NR3)—, W is an aliphatic chain substituted with one or two (—O—NO2) groups, R2 is: —H, —OH, —OCH3, or —NHR3. R3 is: —H, —CH3, —CH2CH3, [—CH2(CH3)2]. R?? is methylsulphonyl or sulphonamido.Type: ApplicationFiled: September 7, 2011Publication date: June 27, 2013Applicant: Rottapharm S.p.A.Inventors: Antonio Giordani, Mariangela Biava, Maurizio Anzini, Vicenzo Calderone, Lucio Claudio Rovati
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Patent number: 8470857Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: GrantFiled: August 14, 2009Date of Patent: June 25, 2013Assignee: N30 Pharmaceuticals, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Publication number: 20130158058Abstract: This invention provides compositions and methods of inhibiting, suppressing, or treating a tendinous or musculoskeletal soft tissue injury. The invention further provides a method of ameliorating symptoms associated with a tendinous or musculoskeletal soft tissue injury. Additionally, the invention provides methods for evaluating the risk of developing a tendinous or musculoskeletal soft tissue injury.Type: ApplicationFiled: February 14, 2013Publication date: June 20, 2013Applicant: The Trustees of the University of PennsylvaniaInventor: The Trustees of the University of Pennsylvania
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Patent number: 8466193Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.Type: GrantFiled: April 15, 2009Date of Patent: June 18, 2013Assignee: Pharmacyclics, Inc.Inventors: Erik Verner, Sriram Balasubramanian, Joseph J. Buggy
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Publication number: 20130136794Abstract: Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.Type: ApplicationFiled: April 21, 2011Publication date: May 30, 2013Applicant: PEKING UNIVERSITYInventors: Runtao Li, Zemei Ge, Jingrong Cui, Xingyl Sun, Zhongqing Wang, Xu Yan
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Publication number: 20130116227Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.Type: ApplicationFiled: July 12, 2011Publication date: May 9, 2013Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
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Publication number: 20130101687Abstract: 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: ApplicationFiled: July 13, 2012Publication date: April 25, 2013Inventors: Michael Dean Willis, Marie Elizabeth Saunders, Darryl Ramoutar, Joanna Maria Szymczyk, Frances Nita Krenick, Andrea Rohrbacher
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Patent number: 8420693Abstract: The present invention relates to novel Dipyrrole Compounds, compositions comprising a Dipyrrole Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Dipyrrole Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus. The invention also provides screening assays for compounds that can be used in combination with Dipyrrole Compounds for the treatment of cancer or neoplastic disease, inhibition of cancer cell growth, or treatment of viral infections.Type: GrantFiled: December 22, 2005Date of Patent: April 16, 2013Assignee: Gemin X Pharmaceuticals Canada Inc.Inventors: Giorgio Attardo, Sasmita Triparthy, Elise Rioux, Gerson Gonzalez
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Patent number: 8420677Abstract: Use of DIM and/or its derivatives for prevention, treatment and/or delay of age-related hearing loss in mammals.Type: GrantFiled: February 19, 2009Date of Patent: April 16, 2013Assignee: DSM IP Assets B.V.Inventors: Hubert Hug, Bernd Mussler, Daniel Raederstorff, Ying Wang-Schmidt
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Publication number: 20130090300Abstract: The invention provides inhibitors of influenza endonuclease activity and tools for their discovery.Type: ApplicationFiled: July 20, 2012Publication date: April 11, 2013Inventors: Joseph D. Bauman, Kalyan Das, Disha Patel, Eddy Arnold
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Patent number: 8415359Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hydType: GrantFiled: August 5, 2011Date of Patent: April 9, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Akihiro Furukawa, Takehiro Fukuzaki, Yukari Onishi, Hideki Kobayashi, Takeshi Honda, Yumi Matsui, Masahiro Konishi, Kenjiro Ueda, Tetsuyoshi Matsufuji
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Patent number: 8399506Abstract: The present invention relates to the use of combinations of 4-bromo-2-(4-chloro-phenyl)-5-(trifluoromethyl)-1H-pyrrole-3-carbonitrile and an oxidizing agent, for eradicating, eliminating or reducing aquatic organisms in ballast water or bilge water whereby 4-bromo-2-(4-chloro-phenyl)-5-(trifluoromethyl)-1H-pyrrole-3-carbonitrile and the oxidizing agent are in respective proportions to provide a synergistic effect against fouling organisms. Suitable oxidizing agents are e.g.Type: GrantFiled: August 6, 2007Date of Patent: March 19, 2013Assignee: Janssen Pharmaceutica, NVInventor: Tony Mathilde Jozef Kempen
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Publication number: 20120328569Abstract: Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: March 2, 2011Publication date: December 27, 2012Inventors: Casey Cameron McComas, Nigel J. Liverton, Richard Soll, Peng Li, Xuanjia Peng, Hao Wu, Frank Narjes, Joerg Habermann, Uwe Koch, Shilan Liu
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Patent number: 8338475Abstract: The use of urocanic acid or another pharmaceutically acceptable agent being able to acidify the cell cytoplasm for the manufacture of a pharmaceutical composition useful for causing inhibition or halting of transformed or non-transformed cell proliferation in a person or an animal, where an effective amount of the agent is administered in an essentially non-dissociated form to the person or animal. The use of the agent as an enhancer for other therapeutically active agents, and a pharmaceutical composition, are also disclosed.Type: GrantFiled: April 21, 2006Date of Patent: December 25, 2012Assignee: BioCis Pharma OyInventors: Lasse Leino, Jarmo Laihia
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Publication number: 20120316193Abstract: The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.Type: ApplicationFiled: May 10, 2012Publication date: December 13, 2012Inventors: Megan Foley, Bradley Tait, Matthew Cullen
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Patent number: 8318794Abstract: The invention provides method of use of a porphyrin compound as shown below in preparing a medicament for sonodynamic therapy, and a method of sonodynamic therapy using a porphyrin compound. Said therapy comprises administering a porphyrin compound to a patient and applying sonic wave to the patient, wherein each symbol has the meaning as defined in the description.Type: GrantFiled: November 25, 2008Date of Patent: November 27, 2012Assignee: Science Group Pty. Ltd.Inventors: Xiaohuai Wang, Jiangan Su, Qing Li, Guanglian Zhao, Yifan Luo, Bo Yu
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Publication number: 20120289506Abstract: 5-membered heterocyclic derivatives represented by general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, —N(-D-L-M)2 and the like, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.Type: ApplicationFiled: June 12, 2012Publication date: November 15, 2012Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
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Patent number: 8304419Abstract: The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.Type: GrantFiled: June 5, 2008Date of Patent: November 6, 2012Assignee: GlaxoSmithKline LLCInventors: Pek Yoke Chong, Andrew James Peat, Paul Richard Sebahar, Michael Youngman, Huichang Zhang
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Patent number: 8299066Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.Type: GrantFiled: January 20, 2012Date of Patent: October 30, 2012Assignee: Shionogi & Co., Ltd.Inventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka
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Patent number: 8283376Abstract: The invention relates to the use of substituted 2-aminotetralins of general formula (I) as a medicament for the preventive treatment of Parkinson's disease.Type: GrantFiled: December 23, 2004Date of Patent: October 9, 2012Assignee: UCB Pharma GmbHInventors: Dieter Scheller, Frank Dressen
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Patent number: 8263527Abstract: Insecticidal compositions suitable for use in preparation of insecticidal liquid fertilizers comprising a pyrethroid, a hydrated aluminum-magnesium silicate, and at least one dispersant selected from the group consisting of a sucrose ester, a lignosulfonate, an alkylpolyglycoside, a naphthalenesulfonic acid formaldehyde condensate and a phosphate ester are disclosed.Type: GrantFiled: September 9, 2011Date of Patent: September 11, 2012Assignee: FMC CorporationInventor: Timothy Martin
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Publication number: 20120220593Abstract: A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; R2 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; and X is, for example, a hydroxyl group or a C1-C6 alkoxy group].Type: ApplicationFiled: February 24, 2012Publication date: August 30, 2012Applicant: Daiichi Sankyo Company, LimitedInventors: Kazumasa Aoki, Koji Suda, Toshio Kaneko, Tomio Kimura
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Publication number: 20120214785Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: August 17, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Gerald Juergen ROTH, Martin FLECK, Niklas HEINE, Joerg KLEY, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
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Patent number: 8247423Abstract: Described herein are compositions and methods for using these compositions in the treatment of cancer, tumors, and tumor-related disorders in a subject.Type: GrantFiled: July 11, 2008Date of Patent: August 21, 2012Assignee: Tragara Pharmaceuticals, Inc.Inventors: Thomas M. Estok, Sara L. Zaknoen, Robert K. Mansfield, Tracy Lawhon
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Publication number: 20120196915Abstract: The present invention relates to a new series of 1,2-diphenylpyrroles of formula (I) or their pharmaceutically acceptable salts, or their pharmaceutically acceptable solvates, having antitumor activity, wherein R1 and R2 are individually selected from the group consisting of halogen, optionally substituted O(C1-C4)alkyl and optionally substituted (C1-C4)alkyl; and R3 is selected from the group consisting of H, (C1-C4)alkyl, CONH2 and (C?NH)NH2. It also relates to a process for preparing them, to pharmaceutical compositions containing them, and to their use for the treatment of cancer, in particular lung carcinoma, colorectal carcinoma, breast carcinoma and/or prostate carcinoma.Type: ApplicationFiled: July 28, 2010Publication date: August 2, 2012Applicant: ARGON PHARMA, S.L.Inventors: Ramon Mangues Bafalluy, Isolda Casanova Rigalt, Fernando Albericio Palomera, Mercedes Álvarez, Svetlana Savina
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Patent number: 8217073Abstract: Novel pyrrole derivatives are disclosed as A?42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the A?42 peptide.Type: GrantFiled: May 6, 2010Date of Patent: July 10, 2012Assignee: Myrexis, Inc.Inventors: Warren S. Weiner, Rachel M. Slade, Yevgeniya I. Klimova, Ruth J. Walton, Mark B. Anderson
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Patent number: 8216971Abstract: The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against phyto-pathogenic fungi or damaging insects, and the corresponding methods of treatment using the said composition. More precisely, the subject of the present invention is a pesticide composition based on propamocarb-HCl, an insecticide active substance and optionally a further fungicide active substance.Type: GrantFiled: December 21, 2007Date of Patent: July 10, 2012Assignee: Bayer Intellectual Property GmbHInventors: Koen van Den Eynde, Wolfgang Thielert, Heike Hungenberg
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Patent number: 8212057Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The invention also relates to the process for preparing such compounds, a composition containing such a compound and the use of such a compound and composition in medicine. The compounds lower triglyceride levels in blood and may be useful in the treatment of obesity, hyperlipidaemia, hypercholesteremia, syndrome X and diabetes.Type: GrantFiled: July 25, 2002Date of Patent: July 3, 2012Assignee: Cadila Healthcare LimitedInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Barot, Saurin Khimshankar Raval, Preeti Saurin Raval, Sujay Basu
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Publication number: 20120157462Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of aniline and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.Type: ApplicationFiled: January 30, 2008Publication date: June 21, 2012Inventors: Alan T. Johnson, Guan-Sheng Jiao
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Publication number: 20120149693Abstract: The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C and/or RSK disorders, including diseases and disorders mediated by GPCRs and/or RSKs.Type: ApplicationFiled: May 5, 2010Publication date: June 14, 2012Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.Inventor: Raymond G. Booth
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Patent number: 8188144Abstract: The invention is directed to compounds of Formula (I) or salts thereof. The invention is also directed to use of the compounds of formula (I) in the in vitro preservation of living animal cells. The living cells can be isolated cells, such as stem cells, or groups of cells such as tissue or an organ.Type: GrantFiled: April 9, 2010Date of Patent: May 29, 2012Assignee: Antoxis LimitedInventors: Donald Barton McPhail, Graeme James Cook, Andrew Scott Johnstone
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Publication number: 20120114723Abstract: The present invention relates to a method for controlling fire ants with a single step application of a combination of a bait and a controlled release treatment composition, and to the novel bait/controlled release treatment composition combination used in the method of the present invention.Type: ApplicationFiled: January 13, 2012Publication date: May 10, 2012Inventor: Victor Bruce Steward
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Publication number: 20120114726Abstract: A substrate treated with a composition comprising a pyrethroid, chlorfenapyr and a special acrylate binder is suitable for controlling harmful insects in buildings, for protecting humans and domestic animals from such harmful insects and for protecting humans and domestic animals from vector-transmitted diseases which are transmitted by the harmful insects.Type: ApplicationFiled: July 5, 2010Publication date: May 10, 2012Applicant: BASF SEInventors: Hartmut Leininger, Susanne Stutz, Ulrich Karl
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Publication number: 20120114727Abstract: A sheet-like structure, in particular a net, finished with an insecticidal mixture comprising a) chlorfenapyr and b) one or more pyrethroids from the group consisting of alpha-cypermethrin (b1), deltamethrin (b2), permethrin (b3) and lambda-cyhalothrin (b4), in an amount of (in each case relative to the sheet-like structure) a) 50 to 150 mg/m2 chlorfenapyr; b1) 50 to 150 mg/m2 alpha-cypermethrin; b2) 15 to 45 mg/m2 deltamethrin; b3) 50 to 750 mg/m2 permethrin; b4) 5 to 30 mg/m2 lambda-cyhalothrin, is suitable for controlling harmful insects in buildings and for protecting humans and domestic animals from such harmful insects and from vector-transmitted diseases which are transmitted by the harmful insects.Type: ApplicationFiled: July 5, 2010Publication date: May 10, 2012Applicant: BASF SEInventors: Hartmut Leininger, Susanne Stutz, Ulrich Karl