1,2-diazoles (including Hydrogenated) Patents (Class 548/356.1)
  • Patent number: 9814723
    Abstract: Provided are articles of manufacture, compositions and methods for prophylaxis and/or therapy for disorders involving dizziness and/or vertigo. The articles of manufacture and compositions contain lamotrigen and/or bupropion. The compositions include pharmaceutical compositions which are intended to alleviate dizziness and/or vertigo. In certain aspects the disclosure includes articles of manufacture and kits which include printed material which provides an indication that the articles or compositions are intended to be used for prophylaxis and/or therapy of Meniere's Disease or a symptom thereof.
    Type: Grant
    Filed: June 4, 2015
    Date of Patent: November 14, 2017
    Inventor: Lixin Zhang
  • Patent number: 9732041
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: August 15, 2017
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Paula Ann Boriack-Sjodin, Oscar Miguel Moradei, Lei Jin, Kenneth W. Duncan
  • Patent number: 9040717
    Abstract: A compound represented by the following formula: wherein n is 1 or 2, or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 26, 2015
    Assignee: JAPAN TOBACCO INC.
    Inventors: Takahisa Motomura, Gakujun Shomi
  • Patent number: 9024041
    Abstract: There is provided a compound of formula (I): wherein: J represents (A): or (B): compositions comprising same, processes for preparing said compounds and use thereof in treatment, particularly in the treatment of inflammatory disease, such as asthma, COPD and 15 rheumatoid arthritis.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: May 5, 2015
    Assignee: Respivert Ltd.
    Inventors: John King-Underwood, Peter John Murray, Jonathan Gareth Williams, Ildiko Buck, Stuart Thomas Onions
  • Patent number: 9006283
    Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: April 14, 2015
    Assignee: Acumen Pharmaceuticals, Inc.
    Inventors: Grant A. Krafft, Todd Pray, William F. Goure
  • 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: 8946442
    Abstract: Foams of ionic compounds are described. Methods of making the foams are also provided. The foams are ionic and can be used for catalysis, separations, gas storage, biosensors, electronics, and electrochemical applications.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: February 3, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: Mark Brandon Shiflett, Akimichi Yokozeki
  • Patent number: 8921124
    Abstract: PROBLEM Provided is a novel cyanine dye derivative with a pyrazole skeleton and an indole skeleton, having high sensitivity performance in a shorter wavelength region as compared with a conventional optical system, and showing high water solubility.
    Type: Grant
    Filed: March 30, 2007
    Date of Patent: December 30, 2014
    Assignee: Wako Pure Chemical Industries, Ltd.
    Inventors: Matsuhiro Date, Satoshi Hasaba, Naoyuki Yamamoto
  • Publication number: 20140357872
    Abstract: Disclosed herein is a highly enantio—(75 to 98% ee)and diastereoselective (99 to 100% de)synthesis of functionalised pyrazolidines via tandem a-amination-Corey Chaykovsky reaction of alpha unsubstituted aldehydes.
    Type: Application
    Filed: December 17, 2012
    Publication date: December 4, 2014
    Inventors: Boopathi Senthil Kumar, Vaithiyanathan Venkataramasubramanian, Arumugam Sudalai
  • Patent number: 8901119
    Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: December 2, 2014
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
  • Patent number: 8901313
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: December 2, 2014
    Assignee: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
  • Patent number: 8883839
    Abstract: The present invention relates to tetraline and indane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetraline and indane derivatives, and the use of such tetraline and indane derivatives for therapeutic purposes. The tetraline and indane derivatives are GlyT1 inhibitors.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: November 11, 2014
    Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
    Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins
  • Patent number: 8877794
    Abstract: The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: November 4, 2014
    Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
    Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins, Wilfried Hornberger, Mario Mezler, Sean Turner
  • Patent number: 8859814
    Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: October 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Derek Cogan, Alexander Heim-Riether, Wang Mao, Craig Andrew Miller, Philip Dean Ramsden, Lana Louise Smith Keenan, Roger John Snow, Jiang-Ping Wu, Yu Yang
  • Patent number: 8846743
    Abstract: The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: September 30, 2014
    Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
    Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins
  • Patent number: 8835482
    Abstract: The present invention is concerned with novel substituted indazole and aza-indazole derivatives of Formula (I) wherein R1, R2, R3, R4, Y, A1, A2, A3, A4, X1, X2, X3 and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: May 5, 2010
    Date of Patent: September 16, 2014
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: François Paul Bischoff, Henricus Jacobus Maria Gijsen, Serge Maria Aloysius Pieters, Garrett Berlond Minne
  • Patent number: 8697887
    Abstract: Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: September 5, 2013
    Date of Patent: April 15, 2014
    Assignee: Samumed, LLC
    Inventors: John Hood, Sunil Kumar KC
  • Patent number: 8697911
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: April 15, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
  • Patent number: 8691806
    Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
    Type: Grant
    Filed: June 28, 2012
    Date of Patent: April 8, 2014
    Assignees: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology Limited
    Inventors: Valerio Berdini, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hannah Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
  • Patent number: 8669280
    Abstract: The present invention relates to novel compounds and compositions having antiviral activity. The invention also relates to methods for the therapeutic or prophylactic treatment of viral infections in mammals.
    Type: Grant
    Filed: June 23, 2006
    Date of Patent: March 11, 2014
    Assignee: Biotron Limited
    Inventors: Gary Dinneen Ewart, Wayne Morris Best
  • Patent number: 8664258
    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: March 4, 2014
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Dennis Chapman, Juyi Choi, Konrad Feichtinger, Sangdon Han, Honnappa Jayakumar, Thuy-Anh Tran, Jay Xu, Ning Zou
  • Patent number: 8642637
    Abstract: The pharmaceutically acceptable salts of bicyclo-substituted pyrazolon azo derivatives represented by the general formula (I), their preparation methods, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor. The definitions of substituents in the general formula (I) are the same as the description.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: February 4, 2014
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Peng Cho Tang, Hejun Lü, Hongbo Fei, Yiqian Chen
  • Patent number: 8642634
    Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 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: July 27, 2007
    Date of Patent: February 4, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Robert James Pasteris, Mary Ann Hanagan
  • Patent number: 8618144
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: December 31, 2013
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Peter Lin, Lehua Chang, Scott D. Edmondson
  • Publication number: 20130345120
    Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
    Type: Application
    Filed: March 9, 2012
    Publication date: December 26, 2013
    Applicant: Glaxosmithkline LLC
    Inventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
  • Publication number: 20130296455
    Abstract: Disclosed are a dye that is excellent in solubility and heat-resistance, and a novel compound that is suitable for the dye, and specifically provides a yellow dye having a maximum absorption wavelength in the region of 420 to 470 nm. Also disclosed are a colored (alkali-developable) photosensitive composition and an optical filter using the dye, and specifically provides a color filter that does not decrease luminance and thus is preferable for an image display device such as a liquid crystal display panel. Specifically, disclosed are a novel compound represented by the following general formula (1), a dye using the compound, and a colored (alkali-developable) photosensitive composition and a color filter. The content of the above-mentioned general formula (1) is as described in the description.
    Type: Application
    Filed: December 27, 2011
    Publication date: November 7, 2013
    Applicant: ADEKA CORPORATION
    Inventors: Yosuke Maeda, Masaaki Shimizu, Koichi Shigeno
  • Patent number: 8575362
    Abstract: Methods useful for preparing compounds of formula I: and salts thereof are disclosed. Also disclosed are intermediates useful in the preparation of such compounds.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: November 5, 2013
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Mark S. Bednarz, Hugh Alfred Burgoon, Jr., Shinya Iimura, Ramanaiah C. Kanamarlapudi, Qiuling Song, Wenxue Wu, Jie Yan, Haiming Zhang
  • Patent number: 8546404
    Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
    Type: Grant
    Filed: June 5, 2007
    Date of Patent: October 1, 2013
    Assignee: Merck Sharp & Dohme
    Inventors: Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, Jr., Neng-Yang Shih, Hugh Y. Zhu, Robert Sun, Joseph M. Kelly, Ronald J. Doll, Yang Nan, Tong Wang, Jagdish A. Desai, James J-S Wang, Youhao Dong, Vincent S. Madison, Li Xiao, Alan W. Hruza, M. Arshad Siddiqui, Ahmed A. Samatar, Sunil Paliwal, Hon-Chung Tsui, Azim Alan Celebi, Yiji Wu, Sobhana Babu Boga, Abdul-Basit Alhassan, Xiaolei Gao, Liang Zhu, Mehul Patel
  • Patent number: 8501799
    Abstract: The invention relates to a liquid pharmaceutical composition that contains N-phenylpyrazole derivative as an active principle, benzyl alcohol, and an appropriately selected organic solvent, and to the use of such a composition for preparing a topically applied antiparasitic veterinary drug for preventing and/or treating flea infestation in pets, in particular, in dogs and cats.
    Type: Grant
    Filed: December 16, 2008
    Date of Patent: August 6, 2013
    Assignee: Virbac
    Inventor: Guy Derrieu
  • Patent number: 8476458
    Abstract: The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: July 2, 2013
    Assignees: The Wistar Institute, The John Hopkins University
    Inventors: Ronen Marmorstein, Xin Liu, Philip A. Cole, Ling Wang, Erin M. Bowers, David J. Meyers, Chandrani Mukherjee
  • Patent number: 8470052
    Abstract: Methods for extracting metals from aqueous solutions, by contacting an aqueous solution containing a dissolved metal with a solvent extraction composition having a water-immiscible organic solvent; and a metal extractant compound according to Formula (1) and tautomers and salts thereof, are disclosed herein, wherein substituents R5-8, Y, and Z are as described herein.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: June 25, 2013
    Assignee: Cytec Technology Corp.
    Inventors: John Campbell, Ronald Matthys Swart, Lucy Emeleus, Susan Owens
  • Patent number: 8461184
    Abstract: The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: June 11, 2013
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Bernard J. Vliet Van
  • Patent number: 8445525
    Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: May 21, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Kai Gerlach, Roland Pfau, Norbert Hauel, Iris Kauffmann-Hefner, Georg Dahmann, Herbert Nar, Sandra Handschuh, Wolfgang Wienen, Annette Schuler-Metz
  • Patent number: 8410141
    Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: April 2, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Tetsuya Murata, Yasushi Yoneta, Hidetoshi Kishikawa, Jun Mihara, Daiei Yamazaki, Mamoru Hatazawa, Norio Sasaki, Kei Domon, Eiichi Shimojo, Teruyuki Ichihara, Katsuhiko Shibuya, Masashi Ataka, Ulrich Görgens
  • Patent number: 8343913
    Abstract: A method of reducing antifungal drug resistance in which Hsp inhibitors, such as Hsp90 inhibitors, are used.
    Type: Grant
    Filed: July 5, 2005
    Date of Patent: January 1, 2013
    Assignee: Whitehead Institute for Biomedical Research
    Inventors: Leah Cowen, Susan L. Lindquist
  • Patent number: 8334301
    Abstract: Provided is a compound having a superior acid secretion suppressive action, which shows an antiulcer activity and the like.
    Type: Grant
    Filed: September 24, 2008
    Date of Patent: December 18, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Haruyuki Nishida, Yasuyoshi Arikawa, Keizo Hirase
  • Patent number: 8324258
    Abstract: The present invention relates to a family of guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.
    Type: Grant
    Filed: September 11, 2008
    Date of Patent: December 4, 2012
    Assignee: The Regents of the University of Michigan
    Inventors: Gary D. Glick, Gina Ney
  • Patent number: 8273900
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.
    Type: Grant
    Filed: July 31, 2009
    Date of Patent: September 25, 2012
    Assignee: Novartis AG
    Inventors: David Beattie, Anny-Odile Colson, Andrew James Culshaw, Lisa Sharp, Emily Stanley, Lilya Sviridenko
  • Patent number: 8258168
    Abstract: Compounds corresponding to the formula (I) as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the invention, and methods of treatment using them.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: September 4, 2012
    Assignee: Sanofi
    Inventors: Laurent Dubois, Yannick Evanno, Christian Maloizel, Mireille Sevrin
  • Patent number: 8252826
    Abstract: This invention relates to novel cyclopentyl- and cycloheptylpyrazole derivatives of the formula I wherein A and R1 to R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. The invention relates also to compositions including these compounds and methods of using the compounds.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: August 28, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Bernd Kuhn, Hans Richter, Sven Taylor
  • Patent number: 8247576
    Abstract: The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: August 21, 2012
    Assignees: Astex Therapeutics Limited, Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology Limited
    Inventors: Valerio Berdini, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hannah Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
  • Patent number: 8236845
    Abstract: The present invention relates to heterocyclyl-substituted-tetrahydro-naphthalen-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the treatment or prophylaxis of various disorders of humans or animals.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: August 7, 2012
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover, Helmut H. Buschmann
  • Patent number: 8232308
    Abstract: A method for treating a disease in which Rho kinase is involved. The method is carried out by administering to a patient in need thereof a pharmaceutically effective amount of a compound of the following formula or a pharmaceutically acceptable salt thereof: wherein the ring X is a benzene ring or a pyridine ring; R1 and R2 are hydrogen or alkyl or together form a cycloalkene ring; R3 is hydrogen, substituted alkyl, unsubstituted alkenyl, carboxyl or an ester or an amide thereof, amino or a cyano; R4 is hydrogen, hydroxyl, substituted or unsubstituted alkoxy, unsubstituted alkenyloxy, unsubstituted cycloalkyloxy substituted or unsubstituted alkyl, unsubstituted alkenyl, unsubstituted cycloalkyl, amino, substituted or unsubstituted alkylamino, nitro, cyano or a monocyclic heterocycle; and R5 is a halogen atom or a hydrogen atom.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: July 31, 2012
    Assignees: UBE Industries, Ltd., Santen Pharmaceutical Co., Ltd.
    Inventors: Masahiko Hagihara, Ken-ichi Komori, Hidetoshi Sunamoto, Hiroshi Nishida, Takeshi Matsugi, Tadashi Nakajima, Masakazu Hatano, Kazutaka Kido, Hideaki Hara
  • Patent number: 8232307
    Abstract: The present invention relates to indane-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the treatment of humans or animals.
    Type: Grant
    Filed: July 4, 2008
    Date of Patent: July 31, 2012
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover
  • Patent number: 8212048
    Abstract: A method of producing an aromatic compound of the following formula (3) comprising reacting a compound of the following formula (1) with an olefin compound of the following formula (2) in the presence of a transition metal complex: (wherein, an Ar1 ring represents an aromatic hydrocarbon ring or aromatic heterocyclic ring, an Ar2 ring represents a heterocyclic ring containing X1 and N*, and the X1 represents a nitrogen atom or carbon atom and the N represents a nitrogen atom connecting via a double bond to either one of two adjacent atoms in the Ar2 ring.) (wherein, R1, R2, R3 and R4 represent each independently a hydrogen atom, an alkyl group having 1 to 10 carbon atoms or an aryl group having 6 to 18 carbon atoms.) (wherein, Ar1, Ar2, X1, N*, R1, R2 and R3 represent the same meanings as described above.).
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: July 3, 2012
    Assignees: Sumitomo Chemical Company, Limited, Osaka University
    Inventors: Fumitoshi Kakiuchi, Yusuke Matsuura, Masato Ueda
  • Patent number: 8188135
    Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1, A5, Rx, X4, and z are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Grant
    Filed: September 16, 2009
    Date of Patent: May 29, 2012
    Assignee: Abbott Laboratories
    Inventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Steven P. Latshaw, Teodozyj Kolasa, Tongmei Li, Sridhar Peddi, Bo Liu, Arturo Perez-Medrano, Meena Patel, Xueqing Wang, Derek W. Nelson
  • Patent number: 8153819
    Abstract: Fungicidal mixtures, comprising as active components 1) at least one 1-methylpyrazol-4-ylcarboxanilides of the formula I where X=O or S, R1=C1-C4-alkyl or C1-C4-haloalkyl, R2=hydrogen or halogen, R3, R4 and R5=independently of one another cyano, nitro, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy or C1-C4-alkylthio; and 2) at least one active compound II, selected from the active compound groups A) to F): A) azoles; B) strobilurins; C) carboxamides; D) heterocyclic compounds; E) carbamates; F) other fungicides; in a synergistically effective amount, methods for controlling harmful fungi using mixtures of at least one compound I and at least one active compound II and the use of the compound(s) I with active compounds II for preparing such mixtures, and also compositions and seed comprising such mixtures.
    Type: Grant
    Filed: August 1, 2006
    Date of Patent: April 10, 2012
    Assignee: BASF SE
    Inventors: Jochen Dietz, Markus Gewehr, Siegfried Strathmann, Reinhard Stierl, Frank Werner, Maria Scherer
  • Patent number: 8133851
    Abstract: The present invention relates to heteroaroyl-substituted serinamides of the formula (I) in which the variables A and R1 to R6 are as defined in the description, and to their agriculturally useful salts, to processes and intermediates for their preparation, and to the use of these compounds or of the compositions comprising these compounds for controlling unwanted plants.
    Type: Grant
    Filed: January 10, 2008
    Date of Patent: March 13, 2012
    Assignee: BASF SE
    Inventors: Matthias Witschel, Dschun Song, Eike Hupe, Trevor William Newton, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Robert Reinhard, Bernd Sievernich, Klaus Groβmann, Thomas Ehrhardt
  • Patent number: 8115011
    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 diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
    Type: Grant
    Filed: May 1, 2008
    Date of Patent: February 14, 2012
    Assignee: Madrigal Pharmaceuticals, Inc.
    Inventors: David Robert Bolin, Adrian Wai-Hing Cheung, Fariborz Firooznia, Matthew Michael Hamilton, Lee Apostle McDermott, Yimin Qian, Jenny Tan, Weiya Yun
  • Patent number: 8114899
    Abstract: Compounds corresponding to the formula (I) as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the invention, and methods of treatment using them.
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: February 14, 2012
    Assignee: Sanofi-Aventis
    Inventors: Laurent DuBois, Yannick Evanno, Christian Maloizel, Mireille Sevrin