The Nitrogen Is Bonded Directly To A Ring And Is In Same Side Chain As Ester Function Patents (Class 560/43)
  • Patent number: 11064696
    Abstract: Described herein are agricultural methods for controlling pests on and/or increasing the plant health of a cultivated plant, with at least one modification, using a pesticidal carboxamide compound or a mixtures thereof. In particular, methods of controlling harmful insects, which are resistant to an insecticidal trait of the plant, are provided. In addition, the use of a pesticidal carboxamide compound or mixtures thereof for protecting a plant, plant propagation material, seeds or the locus of growth, against the attack or infestation by pests, wherein the plant has been modified by mutagenesis or genetic engineering, and for controlling pests that are resistant to an insecticidal trait of the plant are described.
    Type: Grant
    Filed: April 6, 2016
    Date of Patent: July 20, 2021
    Assignee: BASF AGROCHEMICAL PRODUCTS B.V.
    Inventors: Tatjana Sikuljak, Robert Reinhard, Klaus Daeschner, Alejandro Arevalo
  • Patent number: 11021494
    Abstract: The method relates to the field of asymmetric allylic amination and comprises preparing a chiral N-substituted allylic amine compound from the corresponding allylic substrates and substituted hydroxylamines, in the presence of a catalyst, said catalyst comprising copper compounds and a chiral ligand. Examples of chiral amine compounds which can be made using the method include Vigabatrin, Ezetimibe Terbinafine, Naftifine 3-methylmorphine, Sertraline, Cinacalcet, Mefloquine hydrochloride, and Rivastigmine. There are over 20,000 known bioactive molecules with chiral N-substituted allylic amine substructure. The method may also be used to produce non-natural chiral 13-aminoacid esters, a sub-class of chiral N-substituted allylic amine compounds. Examples of 13-aminoacid ester which can be produced by the disclosed method, include, but are not limited to, N-(2-methylpent-1-en-3-yl)benzenamine and Ethyl 2-methylene-3-(phenylamino)butanoate.
    Type: Grant
    Filed: December 6, 2018
    Date of Patent: June 1, 2021
    Assignee: University of Louisiana at Lafayette
    Inventors: Radhey S. Srivastava, Siva Murru
  • Patent number: 10701937
    Abstract: Compositions and methods of using a pesticidal mixture PM that includes at least one compound of formula I defined above, an insecticide and a fungicide for protecting crop, plant propagation material, or soil or water in which the plants are growing, against attack or infestation by invertebrate pests and/or phytopathogenic fungi are described. Also described is a seed treatment composition that includes the pesticidal mixture PM, as well as seeds treated using the pesticidal mixture PM or the seed treatment composition. Methods for controlling invertebrate pests and/or phytopathogenic fungi on crop plants are described that include contacting the plant or the plant propagation material; the pest or its food supply, habitat or breeding ground; and/or the fungi or habitat, with an effective amount of the pesticidal mixture PM or the seed treatment composition. Binary mixtures of a compound of formula I and a second pesticidal component are also described.
    Type: Grant
    Filed: February 3, 2016
    Date of Patent: July 7, 2020
    Assignee: BASF SE
    Inventors: Ronald Wilhelm, Florent Mazuir, Sebastian Soergel
  • Patent number: 10647660
    Abstract: Provided is a method of producing an aromatic amide derivative represented by Formula (I), which method includes a process a containing reacting an aniline derivative represented by Formula (II) with a carboxylic acid derivative represented by Formula (III) in the presence of a base to obtain an imide compound represented by Formula (IV) and a process b containing hydrolyzing the imide compound represented by Formula (IV) to obtain the aromatic amide derivative represented by Formula (I): wherein R1 represents a C1-C4 haloalkyl group, etc.; each of R2 and R3 independently represents a hydrogen atom, a halogen atom, etc.; R4 represents a hydrogen atom, a C1-C4 alkyl group, etc.; each of X1 and X2 independently represents a halogen atom, a C1-C4 haloalkyl group, etc.; and Q represents a C1-C4 alkyl group, a phenyl group, a pyridyl group, etc.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: May 12, 2020
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Yusuke Takahashi, Hideaki Ikishima, Hironari Okura
  • Patent number: 10040900
    Abstract: This invention relates to a radically curable resin composition comprising: a) An unsaturated polyester resin and/or a methacrylate functional resin, b) Reactive diluent, c) A copper salt, copper complex, iron salt and/or iron complex, and d) An enaminone.
    Type: Grant
    Filed: November 12, 2013
    Date of Patent: August 7, 2018
    Assignee: AKZO NOBEL CHEMICALS INTERNATIONAL B.V.
    Inventors: Iris Hilker, Johan Franz Gradus Antonius Jansen, Willem Posthumus
  • Patent number: 9296685
    Abstract: Method of producing a nanoparticle suspension with the steps (i) preparation of an emulsion of a disperse polar phase, where the aqueous phase comprises one or more precursor substances forming the nanoparticles, in a continuous organic phase in the presence of an emulsifier stabilizing the emulsion, (ii) conversion of the one or more precursor substances to nanoparticles in the disperse aqueous phase, (iii) breaking of the emulsion and phase separation, where the nanoparticle suspension is obtained as one phase, (iv) separation off of the nanoparticle suspension, (v) optionally isolation of the nanoparticles from the nanoparticle suspension, wherein the emulsifier is selected from compounds of the general formula (I) in which X is O, NH, Y is C(O), NH, R is a saturated or a mono- or polyunsaturated, linear or branched hydrocarbon radical having 6 to 30 carbon atoms and R1 is hydrogen or C1-C4-alkyl, and R2 is a saturated or a mono- or polyunsaturated, linear or branched hydrocarbon radical having 1 to 30 car
    Type: Grant
    Filed: March 7, 2011
    Date of Patent: March 29, 2016
    Assignee: BASF SE
    Inventors: Robert Engel, Wolfgang Gerlinger, Stefan Braese, Thierry Muller, Christina Belenki, Heike P. Schuchmann, Marion Gedrat
  • Patent number: 9108942
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I; and methods for treating or preventing moderate to severe pain, may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of muscle pain, spasticity, neuropathic pain, fibromyalgia, post-operative pain, muscle spasticity, headache, chronic pain, sub-chronic pain and local pain.
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: August 18, 2015
    Inventor: Mahesh Kandula
  • Patent number: 9017922
    Abstract: A chemically amplified resist composition comprising a base polymer and an amine quencher in the form of a ?-alanine, ?-aminobutyric acid, 5-aminovaleric acid, 6-aminocaproic acid, 7-aminoheptanoic acid. 8-aminooctanoic acid or 9-aminononanoic acid derivative having an unsubstituted carboxyl group has a high contrast of alkaline dissolution in rate before and after exposure and forms a pattern of good profile at a high resolution, minimal roughness and wide DOF.
    Type: Grant
    Filed: September 10, 2013
    Date of Patent: April 28, 2015
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Jun Hatakeyama, Masayoshi Sagehashi
  • Publication number: 20150051407
    Abstract: The present invention relates to a novel process for preparing cis-alkoxy-substituted spirocyclic phenylacetylamino acid esters and cis-alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives, and also to novel intermediates and starting materials which are produced and/or used in the process according to the invention.
    Type: Application
    Filed: March 25, 2013
    Publication date: February 19, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Taraneh Farida, Berndt Maiwald, Martin Littmann, Winfried Etzel
  • Patent number: 8952190
    Abstract: Compounds of formula (I): wherein Ar represents an, optionally substituted, aryl or heteroaryl group, R represents an, optionally substituted, aryl or heteroaryl group, an optionally substituted straight or branched chain C1.10-alkyl, R1 is H or methyl, X is an extender group, n is 0 or an integer between 1 and 12 inclusive, A is a polyol residue wherein the unsubstituted polyol from which the residue is derived has at least y OH groups, and y is an integer>1, can easily be prepared, and are useful as synergists in radiation curing.
    Type: Grant
    Filed: March 25, 2011
    Date of Patent: February 10, 2015
    Assignee: Sun Chemical B.V.
    Inventors: Robert Stephen Davidson, Shaun Lawrence Herlihy
  • Patent number: 8900796
    Abstract: The present invention provides an acid generator generates a sulfonic acid represented by the following general formula (1) in response to high-energy beam or heat: To provide a novel acid generator which is suitably used as an acid generator for a resist composition, which solves the problems of LER and a depth of focus and can be effectively and widely used particularly without degradation of a resolution, a chemically amplified resist composition using the same, and a patterning process.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: December 2, 2014
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Masaki Ohashi, Tomohiro Kobayashi, Masayoshi Sagehashi
  • Patent number: 8871976
    Abstract: The invention includes a compound represented by the following structural formula: wherein is described herein. The compounds of the invention are useful in staining embryonic stem cells.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: October 28, 2014
    Assignees: National University of Singapore, Agency for Science, Technology and Research
    Inventors: Young-Tae Chang, Sung Chan Lee, Nam Young Kang
  • Publication number: 20140315960
    Abstract: The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.
    Type: Application
    Filed: October 31, 2012
    Publication date: October 23, 2014
    Inventor: Claus Selch LARSEN
  • Publication number: 20140309193
    Abstract: There are provided inter alia compounds of formula (I) wherein R1, R2, R3, R4a and R4b are as defined in the specification and their use in therapy, especially in the treatment of bacterial (e.g. pneumococcal) infections.
    Type: Application
    Filed: December 5, 2012
    Publication date: October 16, 2014
    Inventors: Peter William Andrew, Rana Lonnen, Mafalda Pires Damaso, Fritz-Frieder Frickel, Simon Christopher Hirst, Mark William Davies, Daniel Hamza
  • Patent number: 8853440
    Abstract: An amide derivative represented by Formula (3), which exhibits excellent efficacy in pest control effect, is produced by allowing a compound represented by the following Formula (1) and a compound represented by Formula (2) to react with each other. In Formula (1) to Formula (3), Y1 and Y2 each represent a halogen atom or a haloalkyl group; Rf represents a C3-C4 perfluoroalkyl group; and R1 and R2 each represent a hydrogen atom or an alkyl group; LG represents a leaving group; T represents a hydrogen atom or a fluorine atom; X1, X3, X4, and X5 each represent a hydrogen atom, a halogen atom, or the like; and A represents a nitrogen atom, a methine group, or the like.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: October 7, 2014
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Youji Aoki, Yumi Kobayashi, Hidenori Daido, Hiroyuki Katsuta, Hidetaka Tsukada, Atsushi Hirabayashi, Yusuke Takahashi, Michikazu Nomura, Atsuko Kawahara
  • Publication number: 20140296560
    Abstract: An amide derivative represented by Formula (3), which exhibits excellent efficacy in pest control effect, is produced by allowing a compound represented by the following Formula (1) and a compound represented by Formula (2) to react with each other. In Formula (1) to Formula (3), Y1 and Y2 each represent a halogen atom or a haloalkyl group; Rf represents a C3-C4 perfluoroalkyl group; and R1 and R2 each represent a hydrogen atom or an alkyl group; LG represents a leaving group; T represents a hydrogen atom or a fluorine atom; X1, X3, X4, and X5 each represent a hydrogen atom, a halogen atom, or the like; and A represents a nitrogen atom, a methine group, or the like.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Youji Aoki, Yumi Kobayashi, Hidenori Daido, Hiroyuki Katsuta, Hidetaka Tsukada, Atsushi Hirabayashi, Yusuke Takahashi, Michikazu Nomura, Atsuko Kawahara
  • Patent number: 8846946
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, geminally alkoxy/alkylspirocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Grant
    Filed: January 31, 2013
    Date of Patent: September 30, 2014
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Jan Dittgen, Dieter Feucht, Ulrich Görgens, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Arnd Voerste, Eva-Maria Franken, Olga Malsam
  • Publication number: 20140228592
    Abstract: The invention discloses a one pot process for the arylation of ?-dicarbonyl compounds. Particularly, the present invention discloses transition-metal-free, chemo-selective, one pot process for the C-arylation of malonamide esters having Formula I at room temperature provide temperature range to obtain the arylated compounds of formula II with good yield, wherein the arylated compounds are selected from mono-arylated compound and di-arylated compound or mixture thereof.
    Type: Application
    Filed: September 12, 2012
    Publication date: August 14, 2014
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Mhaske Baburao Santosh, Ranjeet Ashokrao Dhokale, Pramod Rameshrao Thakare
  • Publication number: 20140142333
    Abstract: Aniline derivatives for anticancer treatment including a compound of the Formula 1, or a derivative thereof, as an active ingredient,
    Type: Application
    Filed: February 4, 2014
    Publication date: May 22, 2014
    Applicant: NEOMICS Co, Ltd.
    Inventors: Sunghoon KIM, Hee Sook Lee, Young Sun Oh, Dae Gyu Kim
  • Patent number: 8729257
    Abstract: This invention relates to a novel class of hybrid lipid compound based on pentaerythritol, their intermediates, preparation methods and uses thereof. Different kinds of functional groups such as alkyl chain, siloxane group, azobenzene, porphyrins, cholesterol, benzene ring and carboxyl were introduced into the four hydroxyl groups of pentaerythritol through chemical reaction to obtain the final hybrid lipid compounds based on pentaerythritol. Cerasomes prepared from such lipids have uniform size, silicate network surface, good stability and biocompatibility, and the leakage of drugs is not easy. The present liposome can be used as functional materials such as drugs or drug carriers, or used for optical storage and molecular devices, simulation, design and synthesis of artificial systems, nano-composite membrane materials and the removal of organic pollutants, etc., in addition, the preparation method of the present invention is simple, and it is easy for industrial production.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: May 20, 2014
    Assignee: Harbin Institute of Technology
    Inventors: Zhifei Dai, Xiaolong Liang, Xiuli Yue
  • Publication number: 20140107368
    Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.
    Type: Application
    Filed: December 11, 2013
    Publication date: April 17, 2014
    Applicant: Mitsui Chemicals Agro, Inc.
    Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
  • Patent number: 8691869
    Abstract: The present invention relates to a pharmaceutical formulation comprising: a) one or more NO-releasing NSAID(s) of formula (I); b) one or more surfactants; c) a carbonyl scavenger compound selected from free acid forms, salts, carboxylic acid esters derivatives of a compound of formula (II) H2N—(CH2)m—(C6H4)—COOH??(II) wherein m=0-10; and d) optionally an oil or semi-solid fat and/or a short-chain alcohol.
    Type: Grant
    Filed: June 29, 2006
    Date of Patent: April 8, 2014
    Assignee: Nicox S.A.
    Inventors: Ulla Gasslander, Christina Holmberg
  • Publication number: 20140031368
    Abstract: This disclosure is related to compounds having the structure wherein Ar1, Ar2, R1-R6, Z, m, n, o, and p are defined herein. This disclosure also relates to pharmaceutical compositions comprising the above compounds and methods for their use.
    Type: Application
    Filed: July 8, 2013
    Publication date: January 30, 2014
    Applicants: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK, SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Ronald Breslow, Paul A. Marks, K. G. Abhilash, Jianing Wang
  • Publication number: 20140020808
    Abstract: A rubber composition obtained by kneading at least one selected from the group consisting of (A1), (B1), (C1) and (D1), a rubber component and a filler, and a method of improving the viscoelastic property of vulcanized rubber, comprising a first step of kneading at least one selected from the group consisting of (A1), (B1), (C1) and (D1), a rubber component, a filler and a sulfur component and a second step of thermally treating the kneaded material obtained in the previous step.
    Type: Application
    Filed: April 24, 2012
    Publication date: January 23, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yosuke Watanabe, Orhan Ozturk, Yasuo Uekita
  • Publication number: 20140005235
    Abstract: The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests wherein A1, A2, A3, A4, A5, A6, G1, G2, R1, R2, R3, L, Q1, Q2, R4, R5, R6, R7, Q2, Y1, Y2, Y3, Y4, Y5, Y6, Y7, Y8, and Y9 are as defined in claim 1; or salts or N-oxides thereof.
    Type: Application
    Filed: March 19, 2012
    Publication date: January 2, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Pierre Joseph, Marcel Jung, Ottmar Franz Hueter, Peter Renold, Thomas Pitterna
  • Patent number: 8598308
    Abstract: The invention relates to novel multifunctional dendrimer structures with a high loading capacity. Said dendrimer structures include a nucleus having at least a first generation or an end generation covalently bonded thereto. The first generation is formed by at least two of the following structures, namely: a spacer, a load, a branching element. In addition, a plurality of sequences (known as intermediary generations) with at least two of the aforementioned structures can be joined to the first generation. The terminal generation is formed by at least three of the following structures, namely: a spacer, a load, a branching element and a terminal.
    Type: Grant
    Filed: October 24, 2008
    Date of Patent: December 3, 2013
    Assignee: Instituto Tecnológico y de Estudios Superiores de Monterrey
    Inventors: Mario Moises Alvarez, Jesus Angel Valencia Gallegos
  • Publication number: 20130224790
    Abstract: The invention includes a compound represented by the following structural formula: wherein is described herein. The compounds of the invention are useful in staining embryonic stem cells.
    Type: Application
    Filed: August 26, 2011
    Publication date: August 29, 2013
    Applicants: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH, NATIONAL UNIVERSITY OF SINGAPORE
    Inventors: Young-Tae Chang, Sung Chan Lee, Nam Young Kang
  • Publication number: 20130224657
    Abstract: The present invention provides an acid generator generates a sulfonic acid represented by the following general formula (1) in response to high-energy beam or heat: To provide a novel acid generator which is suitably used as an acid generator for a resist composition, which solves the problems of LER and a depth of focus and can be effectively and widely used particularly without degradation of a resolution, a chemically amplified resist composition using the same, and a patterning process.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 29, 2013
    Applicant: SHIN-ETSU CHEMICAL CO., LTD.
    Inventor: SHIN-ETSU CHEMICAL CO., LTD.
  • Publication number: 20130204009
    Abstract: There is provided a more industrially advantageous process for preparing novel pyridine derivatives expected to be used as medicines. A process for preparing 3-[(6-hydroxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzoic acid esters as intermediates with high quality, in short steps and in a high yield, as well as novel benzoic acid esters as their precursors and a process for preparing the same.
    Type: Application
    Filed: February 26, 2013
    Publication date: August 8, 2013
    Applicant: Daiichi Sankyo Company, Limited
    Inventor: Daiichi Sankyo Company, Limited
  • Publication number: 20130184343
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Application
    Filed: March 4, 2013
    Publication date: July 18, 2013
    Applicants: Syngenta Crop Protection LLC, Syngenta Participations AG
    Inventor: Syngenta Participations AG
  • Patent number: 8486642
    Abstract: The present invention provides a method of synthesizing compounds of Formula I: wherein: R1 is a label (e.g., a detectable groups; an anti-tumor agents); L is present or absent and when present is a linking group; and x represents an integer from 1 to 10; or a pharmaceutically acceptable salt thereof. the compounds are useful for, among other things, identifying cysteine sulfenic acids in proteins and monitoring oxidative damage in proteins and cells.
    Type: Grant
    Filed: August 23, 2010
    Date of Patent: July 16, 2013
    Assignee: Wake Forest University Health Sciences
    Inventors: Leslie B. Poole, S. Bruce King, Jacquelyn S. Fetrow
  • Publication number: 20130178624
    Abstract: The present invention concerns the compounds of formula wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl, —O—N?CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-4
    Type: Application
    Filed: January 18, 2013
    Publication date: July 11, 2013
    Applicant: Janssen Pharmaceutica N.V.
    Inventor: Janssen Pharmaceutica N.V.
  • Patent number: 8481725
    Abstract: Cycloalkylcarbonylamino acid derivatives, which are raw material intermediates of a novel cycloalkane carboxamide derivative that selectively inhibits cathepsin K, and a production process thereof, are provided. A cycloalkylcarbonylamino acid derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof: (wherein, R1 and R2 represent alkyl groups, alkenyl groups, alkynyl groups, aromatic hydrocarbon groups, heterocyclic groups or the like, and ring A represents a cyclic alkylidene group having 5, 6 or 7 carbon atoms).
    Type: Grant
    Filed: January 10, 2007
    Date of Patent: July 9, 2013
    Assignee: Seikagaku Corporation
    Inventors: Nobuo Kobayashi, Tsuneo Koji, Hisatomo Kunii
  • Publication number: 20130165682
    Abstract: The present invention relates to a method for the synthesis of an ? amino acetal, comprising (i) oxidizing a tertiary amine in the presence of a copper catalyst, at least one oxidant and a solvent, or (ii) reacting a secondary amine and an aliphatic aldehyde in the presence of a copper catalyst, at least one oxidant and a solvent.
    Type: Application
    Filed: July 6, 2011
    Publication date: June 27, 2013
    Applicant: NANYANG TECHNOLOGICAL UNIVERSITY
    Inventors: Teck Peng Loh, Jiesheng Tian
  • Patent number: 8470871
    Abstract: Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: June 25, 2013
    Assignee: Galderma Research & Development
    Inventors: Thibaud Biadatti, Laurence Dumais, Catherine Soulet, Sandrine Talano, Sebastien Daver
  • Publication number: 20130096319
    Abstract: The present invention is related to a novel process for the preparation of amisulpride (I) which involves: methylation of 4-amino-salicylic-acid (VI) with dimethyl sulphate and base, optionally in presence of TBAB to obtain 4-amino-2-methoxy methyl benzoate (VII) and (ii) oxidation of 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX) or 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) with oxidizing agent in the presence of sodium tungstate or ammonium molybdate to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid (IV) or 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) respectively.
    Type: Application
    Filed: June 9, 2011
    Publication date: April 18, 2013
    Applicant: Lupin Limited
    Inventors: Dinesh Jayntibhai Paghdar, Mahesh Ramkumar Kolekar, Tushar Nandkumar Deshpande, Suryaprakash Pandurang Patil, Yuvraj Atmaram Chavan, Purna Chandra Ray, Girij Pal Singh
  • Patent number: 8420851
    Abstract: The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta (TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 15, 2007
    Date of Patent: April 16, 2013
    Assignee: Cadila Healthcare Limited
    Inventors: Saurin Raval, Preeti Raval, Braj Bhushan Lohray, Vidya Bhushan Lohray, Pankaj R. Patel
  • Publication number: 20130035446
    Abstract: The present invention relates to polymer, homo- or copolymer or oligomer for the photoalignment of liquid crystals comprising a main chain and a side chain, wherein the side chain comprises a difluoromethylene group, compositions thereof, and its use for optical and electro optical devices, especially liquid crystal devices (LCDs).
    Type: Application
    Filed: April 19, 2011
    Publication date: February 7, 2013
    Applicant: ROLIC AG
    Inventors: Jean-Francois Eckert, Satish Palika, Andreas Schuster
  • Patent number: 8367677
    Abstract: Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols, indices and substituents have the following meaning R1?H, CN, NO2, CF3, F, Cl, Br, I, CH3 R2?H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl and either R1 or R2 must be H R3?H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl then X is e.g. with R4 being H, CH3, CH2CH3 or and Y being or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds of formulas (Ia) or (Ib). The compounds are applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
    Type: Grant
    Filed: March 18, 2005
    Date of Patent: February 5, 2013
    Assignee: Revotar Biopharmaceuticals AG
    Inventors: Remo Kranich, Ewald Mirko Aydt
  • Publication number: 20130012611
    Abstract: Compounds of formula (I): wherein Ar represents an, optionally substituted, aryl or heteroaryl group, R represents an, optionally substituted, aryl or heteroaryl group, an optionally substituted straight or branched chain C1.10-alkyl, R1 is H or methyl, X is an extender group, n is 0 or an integer between 1 and 12 inclusive, A is a polyol residue wherein the unsubstituted polyol from which the residue is derived has at least y OH groups, and y is an integer>1, can easily be prepared, and are useful as synergists in radiation curing.
    Type: Application
    Filed: March 25, 2011
    Publication date: January 10, 2013
    Inventors: Robert Stephen Davidson, Shaun Lawrence Herlihy
  • Publication number: 20130012735
    Abstract: Sitagliptin intermediate compounds of formula (f) and methods of preparation and use thereof are disclosed. Compounds of formula (f) are prepared by the following steps: compounds of formula (a) are subjected to electrophilic reaction with benzyl halides to form compounds of formula (b), which then react with compounds of formula (i) to form novel compounds of formula (e). Gignard agents formed from 2,4,5-trifluoro brmobenzene and magnesium metal react with compounds of formula (e) to afford compounds of formula (f), which are novel intermediates for the preparation of Sitagliptin intermediates of formula (g). Compounds of formula (f) are subjected to reduction by Pd/C, debenzylation, substitution of protecting group to form compounds of formula (g). Compounds of formula (a), (b), (i), (e), (f), and (g) have the following structures, in which R is protecting group of carboxyl and R2 is (substituted) hydrocarbyl.
    Type: Application
    Filed: March 22, 2011
    Publication date: January 10, 2013
    Applicant: ZHEJIANG JIUZHOU PHARMACEAUTICAL CO., LTD.
    Inventors: Hongjun Gao, Min Li
  • Publication number: 20120330030
    Abstract: Provided is an enantioselective, palladium-catalyzed method for the preparation of ?-amino-?,?-unsaturated carboxylic acid derivatives having the formulas II, III, VII and VIII:
    Type: Application
    Filed: September 6, 2012
    Publication date: December 27, 2012
    Inventors: Murat Acemoglu, Andreas Pfaltz, Claude Shaerer
  • Publication number: 20120309997
    Abstract: The present invention relates to enantiomerically enriched aminodiphosphine ligands where the chirality is located in the phosphorus atom and their preparation process, to catalysts containing them and their preparation process, as well as their use in asymmetric synthesis.
    Type: Application
    Filed: October 13, 2010
    Publication date: December 6, 2012
    Applicant: ENANTIA, S.L.
    Inventors: Mónica Alonso Xalma, Xavier Verdaguer Espaulella, Marc Revés Vilaplana, Antoni Riera Escalé
  • Patent number: 8318969
    Abstract: This invention provides alignment materials for liquid crystal display device of vertical alignment mode and methods for the preparation of the same, and more particularly, it provides diaminobenzene derivatives represented by the following formula 1: wherein n is an integer of 1 to 5 and R is an alkyl or alkoxy group of 3 to 5 carbon atoms, which align liquid crystal in uniform and vertical way, have not only excellent mechanical properties such as heat resistance and surface strength but also high pretilt angles of liquid crystal and in particular, can make response rate of liquid crystal fast, methods for the preparation of the same and liquid crystal alignment films using the same.
    Type: Grant
    Filed: February 9, 2007
    Date of Patent: November 27, 2012
    Assignee: Dongjin Semichem Co., Ltd.
    Inventors: Jin wook Choi, Eung jae Park, Jae cheol Park, Yong bae Kim
  • Patent number: 8288566
    Abstract: Provided is an enantioselective, palladium-catalyzed method for the preparation of ?-amino-?,?-unsaturated carboxylic acid derivatives having the formulas II, III, VII and VIII:
    Type: Grant
    Filed: November 16, 2009
    Date of Patent: October 16, 2012
    Assignee: Novartis AG
    Inventors: Murat Acemoglu, Andreas Pfaltz, Claude Schaerer
  • Patent number: 8227507
    Abstract: Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: July 24, 2012
    Assignee: Galderma Research & Development
    Inventors: Thibaud Biadatti, Laurence Dumais, Catherine Soulet, Sandrine Talano, Sebastien Daver
  • Publication number: 20120142668
    Abstract: Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.
    Type: Application
    Filed: August 11, 2010
    Publication date: June 7, 2012
    Inventors: Niall Anderson, Ann M. Bullion, Neysa Nevins, Michael R. Palovich, Steven L. Sollis, Michael D. Wall, Jakob Busch-Petersen, Brian Evans, Huijie Li
  • Publication number: 20120141938
    Abstract: A chemically amplified resist composition comprising a base polymer, an acid generator, and an amine quencher in the form of a ?-alanine, ?-aminobutyric acid or 5-aminovaleric acid derivative having an acid labile group-substituted carboxyl group has a high contrast of alkaline dissolution rate before and after exposure and forms a pattern of good profile at a high resolution, minimal roughness and wide focus margin.
    Type: Application
    Filed: December 5, 2011
    Publication date: June 7, 2012
    Applicant: SHIN-ETSU CHEMICAL CO., LTD.
    Inventors: Jun Hatakeyama, Masayoshi Sagehashi, Takeru Watanabe
  • Patent number: 8188307
    Abstract: Disclosed is an industrially advantageous production method of optically active ?-amino acid of formula (5a), which includes subjecting an enaminoester of formula (4a) to an asymmetric hydrogenation: wherein * shows an asymmetric carbon atom.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: May 29, 2012
    Assignee: Takasago International Corporation
    Inventors: Takashi Moroi, Tsukasa Sotoguchi, Kazuhiko Matsumura, Motonobu Takenaka, Wataru Kuriyama, Toshiyuki Murayama, Hideki Nara, Tohru Yokozawa, Kenji Yagi
  • Publication number: 20120129888
    Abstract: Novel compounds are continually sought after to treat and prevent disorders. The invention relates to N-(2-oxo-1-phenylpiperidin-3-yl)sulfonamides useful for contributing to the search and identification of new lead compounds which can modulate the functional activity of a biological target.
    Type: Application
    Filed: December 22, 2011
    Publication date: May 24, 2012
    Inventors: JOSEP CASTELLS BOLIART, David Enrique Miguel Centeno, Marta Pascual Gilabert