Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperidine Ring Patents (Class 546/245)
  • Patent number: 10385020
    Abstract: Methods are provided for the synthesis of key intermediates for the synthesis of Argatroban monohydrate, ethyl (2R,4R)-1-[(2S)-2-amino-5-[[imino(nitroamino)methyl]amino]-1-oxopentyl]-4-methylpiperidine-2-carboxylate compounded with HCl. Such intermediates are also provided.
    Type: Grant
    Filed: May 11, 2018
    Date of Patent: August 20, 2019
    Assignee: LUNDBECK PHARMACEUTICALS ITALY S.P.A.
    Inventors: Mariano Stivanello, Florian Anton Martin Huber, Antonio Ricci
  • Patent number: 10035758
    Abstract: An aminocarboxylic acid is produced from a solution that includes an aminocarboxylate and a solvent. A method of producing the aminocarboxylic acid comprises the step of combining a sulfonic acid and the solution comprising the aminocarboxylate and the solvent to produce a composition. An example of the aminocarboxylate is a salt of methylglycine diacetic acid (MGDA). An example of the sulfonic acid is methane sulfonic acid (MSA). The composition comprises the aminocarboxylic acid. The method further comprises the step of isolating the aminocarboxylic acid from the composition.
    Type: Grant
    Filed: December 9, 2014
    Date of Patent: July 31, 2018
    Assignee: BASF SE
    Inventors: Michael D. Capracotta, Kenneth Zack
  • Patent number: 9994526
    Abstract: Methods are provided for the synthesis of key intermediates for the synthesis of Argatroban monohydrate, ethyl (2R,4R)-1-[(2S)-2-amino-5-[[imino(nitroamino)methyl]amino]-1-oxopentyl]-4-methylpiperidine-2-carboxylate compounded with HCl. Such intermediates are also provided.
    Type: Grant
    Filed: August 12, 2016
    Date of Patent: June 12, 2018
    Assignee: LUNDBECK PHARMACEUTICALS ITALY S.p.A.
    Inventors: Mariano Stivanello, Florian Anton Martin Huber, Antonio Ricci
  • Patent number: 9790182
    Abstract: The present invention describes a novel process for preparing piperidine-4-carbothioamide.
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: October 17, 2017
    Assignee: Bayer CropScience Aktiengesellschaft
    Inventors: Marco Brünjes, Mark James Ford
  • Patent number: 9562574
    Abstract: A controllable coupling assembly and a coupling member for use in the assembly are provided. The member includes a first coupling face oriented to face axially along a rotational axis and has a set of locking formations angularly-spaced about the axis. The member also includes a second coupling face having a reverse pocket which receives a reverse locking element. The pocket defines a first load-bearing surface adapted for abutting engagement with a load-bearing surface of the reverse locking element. The second coupling face is oriented to face radially with respect to the axis. Each of the set of locking formations defines a second load-bearing surface adapted for abutting engagement with a load-bearing surface of a forward locking element.
    Type: Grant
    Filed: March 23, 2016
    Date of Patent: February 7, 2017
    Assignee: Means Industries, Inc.
    Inventor: John W. Kimes
  • Patent number: 9482294
    Abstract: A coupling and control assembly including a sensor for providing an electrical signal for electronic transmission control is provided. The assembly includes a first coupling member which supports the sensor and a locking element and a second coupling member supported for rotation about a rotational axis. The second coupling member has a coupling face oriented to face radially with respect to the axis and has a set of ferromagnetic or magnetic locking formations. An electromechanical component is also supported by the first coupling member. Both the locking element and the sensor are in close-spaced opposition to the coupling face. The sensor senses magnetic flux to produce an electrical output signal indicative of a speed of rotation of the second coupling member. A variable magnetic field is generated in response to rotation of the locking formations past the sensor.
    Type: Grant
    Filed: March 23, 2016
    Date of Patent: November 1, 2016
    Assignee: Means Industries, Inc.
    Inventor: John W. Kimes
  • Patent number: 9029550
    Abstract: Inhibitors of the soluble epoxide exemplary hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: May 12, 2015
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Paul D. Jones, Christophe Morisseau, Huazhang Huang, Hsing-Ju Tsai, Richard Gless, Jr.
  • Patent number: 9006442
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: April 14, 2015
    Assignee: Lupin Limited
    Inventors: Sanjeev Anant Kulkarni, Sachin Madan, Nirmal Kumar Jana, Prashant Vitthalrao Tale, Narasimha Murthy Cheemala, Sachin Jaysing Mahangare, Prashant Popatrao Vidhate, Chaitanya Prabhakar Kulkarni, Sapana Suresh Patel, Amolsing Dattu Patil, Seema Prabhakar Zade, Rohan Mahadev Shinde, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150094474
    Abstract: The present invention relates to derivatives of compounds which are known to be of use in the field of agriculture. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more changes one or more of which may be considered to represent a change of oxidation state relative to the groups in the original compound. We refer to these compounds generally as redox derivatives. The compounds are of use as insecticides, herbicides and insect repellents.
    Type: Application
    Filed: March 13, 2013
    Publication date: April 2, 2015
    Inventors: William Thompson, Peter Jackson, Derek Lindsay, Thomas Screen, Benjamin Moulton, Christopher Urch
  • Publication number: 20150087823
    Abstract: The present invention relates to a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical agent containing the compound as an active ingredient. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt, which is the compound of the present invention, is specifically represented by the general formula (I): wherein X is a substituent such as a 1-pyrrolidyl, a 3-thiazolizyl, or a piperidino, and the compound is highly useful as a pharmaceutical agent, such as a prophylactic or therapeutic agent for a peripheral nerve disorder induced by administration of an anticancer agent, a prophylactic or therapeutic agent for neurodegenerative diseases or mental diseases such as dementia, Alzheimer's disease, Parkinson's disease, diabetic neuropathy, depression, glaucoma, or autistic disorder spectrum, a therapeutic or repairing agent for spinal cord injury, analgesics against various pain diseases, or the like.
    Type: Application
    Filed: April 26, 2013
    Publication date: March 26, 2015
    Inventors: Munekazu Iinuma, Shoei Furukawa, Mitsuru Naiki, Tomonori Matsumoto, Kunihiko Higashiura
  • Patent number: 8987265
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, as well as compositions containing these compounds, have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV:
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: March 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhiwei Yin, Paul Michael Scola
  • Publication number: 20150079035
    Abstract: The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.
    Type: Application
    Filed: April 2, 2013
    Publication date: March 19, 2015
    Inventors: Brent R. Stockwell, Scott J. Dixon, Rachid Skouta
  • Patent number: 8957212
    Abstract: There is intended to provide the novel compounds which generate a base easily when irradiated with long wavelength light (active energy rays), a photobase generator containing the compounds and a photobase generation method, and the present invention relates to the compounds represented by the general formula [1], a photobase generator containing the compounds and a photobase generation method: (wherein, Ar represents any of groups with specific structures selected from the group consisting of an anthracenyl group, an anthraquinonyl group and a pyrenyl group; R1 and R2 each independently represent a hydrogen atom or a linear, branched or cyclic alkyl group having 1 to 10 carbon atoms, or represent ones which can form an alicyclic ring containing nitrogen atom(s) or an aromatic ring containing nitrogen atom(s) together with a nitrogen atom to which they are bound, which the rings having 3 to 8 carbon atoms which may have a substituent, R3 and R4 each independently represent a hydrogen atom, a linear, branc
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: February 17, 2015
    Assignee: Wako Pure Chemical Industries, Ltd.
    Inventors: Ayako Kuramoto, Motoshige Sumino, Nobuhiko Sakai
  • Publication number: 20150038498
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: (I) or a pharmaceutically acceptable salt thereof, wherein Q is CH2, NR4, O, S, S(O) or S(O2), wherein R4 is H, C1-6 alkyl, aryl, or C3-8 cycloalkyl; R1 is a heterocycle or —(CR5R6)1-2NH2, wherein R5 and R6, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH; R2 is OH, NH2 or NHSO2CH3; and R3 is C1-6 alkyl.
    Type: Application
    Filed: March 22, 2013
    Publication date: February 5, 2015
    Inventors: Timothy Allen Blizzard, Tesfaye Biftu
  • Publication number: 20150038493
    Abstract: The present invention relates to a series of molecules derived from 2,3-diaminopropionic acid (DAP), comprising or not comprising an 8-hydroxyquinoline (8-HQ) motif, and to the use of said molecules for trapping an alpha-oxoaldehyde resulting particularly from the degradation of the glucose or for trapping an alpha-beta-unsaturated aldehyde, resulting particularly from the oxidative degradation of fatty acids. These molecules can have a further application in the fields of cosmetics, food processing, and pharmaceuticals.
    Type: Application
    Filed: October 5, 2012
    Publication date: February 5, 2015
    Inventors: Guy Potier, André Nobumichi Sasaki, Nicolas Audic
  • Publication number: 20140363634
    Abstract: Ink contains at least one of a compound represented by the following chemical formula 1, a compound represented by chemical formula 2, a compound represented by chemical formula 3, or a compound represented by chemical formula 4.
    Type: Application
    Filed: May 27, 2014
    Publication date: December 11, 2014
    Inventors: Mitsunobu MORITA, Soh NOGUCHI, Okitoshi KIMURA
  • Publication number: 20140364433
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 11, 2014
    Inventors: Theodore M. KAMENECKA, Yuanjun HE, Rong JIANG, William NGUYEN, Xinyi SONG
  • Publication number: 20140343289
    Abstract: The problem to be solved by the present invention is to ea lily and efficiently produce an amino acid having 2 to 7 carbon atoms as a high-purity solid without complicated operation, which is useful as a synthetic intermediate for medicines or agrochemicals. The present invention is characterized in comprising a step of precipitating solid amino acid with high purity. In the present invention, the by-produced salt composed of the sulfonic acid and the amine was removed to the mother liquor by reacting an amine with a sulfonic acid salt of amino acid in an aprotic polar solvent, or by reacting a sulfonic acid with an amine salt of amino acid in an aprotic polar solvent. The sulfonic acid salt of amino acid, for example, may be produced by reacting a N-(tert-butoxycarbonyl) amino acid with a sulfonic acid, or by reacting an amino acid tert-butyl ester with a sulfonic acid.
    Type: Application
    Filed: January 21, 2013
    Publication date: November 20, 2014
    Applicant: Kaneka Corporation
    Inventors: Masatoshi Ohnuki, Akira Nishiyama
  • Patent number: 8889862
    Abstract: The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: November 18, 2014
    Assignee: Glenmark Pharmaceuticals, S.A.
    Inventors: Sukeerthi Kumar, Abraham Thomas, Sachin Sundarlal Chaudhari, Bipin Parsottam Kansagra, Venkata Ramana Yemireddy, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay, Girish Gudi
  • Patent number: 8889683
    Abstract: The present invention relates to novel quinoxaline compounds of Formula I: as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the quinoxaline compounds and the use of the quinoxaline compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: November 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Clifford Cheng, Gerald W. Shipps, Jr., Xiaohua Huang, Ying Huang, Ning Shao, Ashwin Rao, Anandan Palani, Peter Orth, Johannes H. Voigt, Robert J. Herr, Lana Michele Rossiter, Qi Zeng, Xianfeng Sun
  • Publication number: 20140336375
    Abstract: The disclosure is directed to compounds identified as allosteric modulators of 5-HT 2CR, as well as pharmaceutical compositions and methods using the same. Certain embodiments also include methods of identifying and methods of synthesizing the compounds. Optimization and development of allosteric 5-HT 2CR modulators that bind sites other than the primary ligand binding site generate novel, highly selective, and potent ligands of 5-HT2CR. Such molecules can be used as small molecule probes for the nervous system and as effective therapeutics for a variety of diseases.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 13, 2014
    Applicant: The Board of Regents of the University of Texas system
    Inventors: Jia Zhou, Chunyong Ding, Kathryn A. Cunningham
  • Publication number: 20140336193
    Abstract: The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Inventors: Donald W. Landry, Shi-Xian Deng, Stevan Pecic, Kirsten Alison Rinderspacher
  • Publication number: 20140315950
    Abstract: The present invention relates to Formula (I), wherein—if X=NH, each of R1, R2, R3, R4 represents a hydrogen atom; if X=N, the core is aromatic, and R2, R3 and R4 represent hydrogen atoms, and R1=H, halogen, aryl, heteroaryl, alkenyl or acetylenyl; or R1, R2, R3, R4 are defined such that R1 or R2 or R3 or R4 represents a methyl group, and the three other radicals represent a hydrogen atom.
    Type: Application
    Filed: December 10, 2012
    Publication date: October 23, 2014
    Inventors: Daniel Redoules, Sylvie Daunes-Marion, Stephane Poigny, Marie-Florence Galliano
  • Publication number: 20140309174
    Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.
    Type: Application
    Filed: November 12, 2013
    Publication date: October 16, 2014
    Applicant: Eisai Co., Ltd
    Inventors: James J. Kowalczyk, Galina Kuznetsov, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
  • Patent number: 8853393
    Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: October 7, 2014
    Assignee: Anhui New Star Pharmaceutical Development Co., Ltd.
    Inventors: Ziao Xu, Yuanhai Zhao, Degang Li, Xiaoxiang Li
  • Publication number: 20140288077
    Abstract: In one aspect, the invention relates to substituted 4-phenoxyphenol analogs, derivatives thereof, and related compounds, which are useful as inhibitors of proliferating cell nuclear antigen (PCNA); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating hyperproliferative disorders associated with PCNA using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: July 5, 2012
    Publication date: September 25, 2014
    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL
    Inventors: Naoaki Fujii, Marcelo Actis, Chandanamali Punchihewa, Michele Connelly, Sean Wu
  • Publication number: 20140288045
    Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
  • Publication number: 20140288034
    Abstract: A compound having an ability to bind to an S1P receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like: wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shinji NAKADE, Hirotaka Mizuno, Takeji ONO, Masashi Minami, Hiroshi Saga, Hiroshi Hagiya, Takaki Komiya, Hiromu Habashita, Haruto Kurata, Kazuhiro Ohtsuki, Kensuke Kusumi
  • Publication number: 20140243291
    Abstract: The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
    Type: Application
    Filed: July 27, 2012
    Publication date: August 28, 2014
    Inventors: Sven Guenther, Guochen Chi, Bindu Bera, Travis Mickle
  • Publication number: 20140221649
    Abstract: A novel compound suitable for obtaining a negative-type photosensitive resin composition capable of forming a pattern having favorable adhesiveness at a low light exposure. The compound is represented by the following formula (1). In the formula, R1 and R2 each independently indicate a hydrogen atom or an organic group, but at least one indicates an organic group. R1 and R2 may be bonded to form a ring structure and may contain a hetero atom bond. R3 indicates a single bond or an organic group. R4 to R9 each independently indicate a hydrogen atom, an organic group, etc., but R6 and R7 are never hydroxyl groups. R10 indicates a hydrogen atom or an organic group.
    Type: Application
    Filed: June 15, 2012
    Publication date: August 7, 2014
    Applicants: DAICEL CORPORATION, TOKYO OHKA KOGYO CO., LTD.
    Inventors: Dai Shiota, Mayumi Kuroko, Kunihiro Noda, Yoshinori Tadokoro, Yasuyuki Akai, Hideyuki Takai
  • Publication number: 20140221337
    Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein X1, R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds are useful as potassium ion channel inhibitors.
    Type: Application
    Filed: February 6, 2014
    Publication date: August 7, 2014
    Applicant: Xention Limited
    Inventors: Mushtaq Mulla, Derek Edward John, Richard John Hamlyn, Sasha Louise Garrett, Basil Hartzoulakis, David Madge, John Ford
  • Publication number: 20140193926
    Abstract: The invention provides a novel class of reactive fluorescent agents that are based on a pyrene sulfonic acid nucleus. The agents are readily incorporated into conjugates with other species by reacting the reactive group with a group of complementary reactivity on the other species of the conjugate. Also provided are methods of using the compounds of the invention to detect and/or quantify an analyte in a sample. In an exemplary embodiment, the invention provides multi-color assays incorporating the compounds of the invention.
    Type: Application
    Filed: November 14, 2013
    Publication date: July 10, 2014
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Richard HAUGLAND, Wai-Yee Leung, Jixiang Liu
  • Patent number: 8765949
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: July 1, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heiner Ebel, Sara Frattini, Kai Gerlach, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Marco Santagostino, Stefan Scheuerer, Christofer Tautermann, Thomas Trieselmann
  • Publication number: 20140161729
    Abstract: The present invention is directed to method of using a collection of monomers capable of forming multimers as a fluorescence reporter in different applications such as ligand detection/screening, disease diagnosis, drug discovery or screening, fluorescent labeling and imaging, or other fluorescent methodologies. Each monomer in the collection includes one or more ligand elements useful for binding to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the ligand elements directly or indirectly through a connector. Association of linker elements of different combinations of monomers, with their ligand elements bound to the target molecule to form a multimer, will generate a unique fluorescent signature different from that produced by those monomers either alone or in association with each other in the absence of the target molecule, when subjected to electromagnetic excitement.
    Type: Application
    Filed: April 9, 2012
    Publication date: June 12, 2014
    Applicant: CORNELL UNIVERSITY
    Inventors: Francis Barany, Maneesh Pingle, Donald E. Bergstrom, Sarah F. Giardina, Lee Daniel Arnold
  • Patent number: 8728505
    Abstract: What are described are insect- and mite-repellent compositions comprising at least 2 enantiomers selected from the group of 1-[(S)-sec-butyloxycarbonyl]-2-(S)-(2-hydroxyethyl)piperidine (referred to hereinafter as S,S), 1-[(R)-sec-butyloxycarbonyl]-2-(R)-(+)-(2-hydroxyethyl)piperidine (referred to hereinafter as R,R), 1-[(S)-sec-butoxycarbonyl]-2-(R)-(+)-(2-hydroxyethyl)piperidine (referred to hereinafter as S,R), 1-[(R)-sec-butyloxycarbonyl]-2-(S)-(+)-(2-hydroxyethyl)piperidine (referred to hereinafter as R,S), excluding the racemate mixture thereof, a process for preparation thereof and the use thereof in insect- and mite-repellent formulations.
    Type: Grant
    Filed: June 8, 2011
    Date of Patent: May 20, 2014
    Assignee: Saltigo GmbH
    Inventors: Burkhard Koch, Andreas Job, Nikolaus Müller
  • Patent number: 8729095
    Abstract: A compound of the general formula (I): [wherein, R1 represents a halogen atom, or the like, R2 represents a hydrogen atom, or the like, R3 and R4, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, R5 represents a hydrogen atom, a halogen atom, or the like, R6 represents a hydrogen atom, a halogen atom, or the like, R7 and R8, each independently, represent a hydrogen atom, a halogen atom, or the like, R9 and R10, each independently, represent a hydrogen atom, a C1-4 alkyl group, R11 and R12, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, X represents an oxygen atom, a group —CH2—, or the like, Y represents a nitrogen atom, a group ?CH—, or the like, and Z represents a nitrogen atom, or the like] or a pharmacologically acceptable salt thereof, which has an excellent suppressive action on platelet aggregation, and is useful for prevention and/or treatment of thromboembolism.
    Type: Grant
    Filed: August 27, 2010
    Date of Patent: May 20, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Tatsuya Nishi, Masashi Hasegawa, Yumi Nakamoto, Yuichi Ochiai, Ryoko Kitazawa, Hiroshi Susaki
  • Publication number: 20140120326
    Abstract: A polymerizable compound is provided. The polymerizable compound has two or more polymerizable functional groups in a molecule thereof, wherein one of the two or more polymerizable functional groups of the polymerizable compound is an acrylamide group having the below-mentioned formula (1). The polymerizable compound can be preferably used for inkjet ink.
    Type: Application
    Filed: September 17, 2013
    Publication date: May 1, 2014
    Applicant: RICOH COMPANY, LTD.
    Inventors: Mitsunobu Morita, Soh Noguchi, Okitoshi Kimura
  • Patent number: 8703784
    Abstract: This invention relates to novel fused tricyclic compounds under Formula I that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: April 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoyang Meng, Panduranga Adulla P. Reddy, M. Arshad Siddiqui, Amit K. Mandal, Duan Liu, Lianyun Zhao, Andrew McRiner
  • Patent number: 8697335
    Abstract: A radiation-sensitive resin composition includes a compound, a resin and a radiation-sensitive acid generator. The compound has a structure in which a group represented by a following formula (1) is bound to a nitrogen atom. The resin has an acid-dissociative dissolution-controlling group and has a property such that alkali solubility of the resin increases by an action of an acid. In the formula (1), Y is a monovalent group having 5 to 20 carbon atoms, and “*” represents a bonding hand with the nitrogen atom. In the formula (i), R1, R2 and R3 each independently represent a linear or branched alkyl group having 1 to 4 carbon atoms or a monovalent alicyclic hydrocarbon group having 4 to 12 carbon atoms, or R1 and R2 are linked with each other to form a bivalent alicyclic hydrocarbon group, and “*” represents a bonding hand with the oxygen atom.
    Type: Grant
    Filed: January 17, 2012
    Date of Patent: April 15, 2014
    Assignee: JSR Corporation
    Inventors: Kazuo Nakahara, Mitsuo Sato
  • Publication number: 20140088310
    Abstract: Methods are provided for the synthesis of key intermediates for the synthesis of Argatroban monohydrate, ethyl (2R,4R)-1-[(2S)-2-amino-5-[[imino(nitroamino)methyl]amino]-1-oxopentyl]-4-methylpiperidine-2-carboxylate compounded with HCl. Such intermediates are also provided.
    Type: Application
    Filed: March 26, 2012
    Publication date: March 27, 2014
    Applicant: LUNDBECK PHARMACEUTICALS ITALY S.P.A.
    Inventors: Mariano Stivanello, Florian Anton Martin Huber, Antonio Ricci
  • Publication number: 20140088074
    Abstract: Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
    Type: Application
    Filed: May 29, 2012
    Publication date: March 27, 2014
    Applicant: NEWRON PHARMACEUTICALS S.P.A.
    Inventor: Paolo Pevarello
  • Publication number: 20140081017
    Abstract: The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, the invention relates to compounds, compositions thereof, and methods for selectively enhancing fungal sensitivity to antifungal compounds.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 20, 2014
    Applicant: METHYLGENE INC.
    Inventor: METHYLGENE INC.
  • Publication number: 20140066420
    Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
    Type: Application
    Filed: October 16, 2013
    Publication date: March 6, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Shizuo KASAI, Tomohiro KAKU, Masahiro KAMAURA
  • Patent number: 8642774
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
  • Publication number: 20130344132
    Abstract: The invention provides a method for obtaining local anesthetics encapsulated in liposomes, such as multi vesicular liposomes, with high encapsulation efficiency and slow release in vivo. When the encapsulated anesthetic is administered as a single intracutaneous dose, the duration of anesthesia and half-life of the drug at the local injection site is increased as compared to injection of unencapsulated anesthetic. The maximum tolerated dose of the encapsulated anesthetic is also markedly increased in the liposomal formulation over injection of unencapsulated anesthetic. These results show that the liposomal formulation of local anesthetic is useful for sustained local infiltration and nerve block anesthesia.
    Type: Application
    Filed: March 15, 2013
    Publication date: December 26, 2013
    Applicant: PACIRA PHARMACEUTICALS, INC.
    Inventor: PACIRA PHARMACEUTICALS, INC.
  • Patent number: 8592584
    Abstract: Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.
    Type: Grant
    Filed: April 15, 2011
    Date of Patent: November 26, 2013
    Assignee: The Board of Trustees of the of The University of Illinois
    Inventors: Paul J. Hergenrother, Karson S. Putt, Quinn P. Peterson, Valerie Fako
  • Publication number: 20130281664
    Abstract: The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e.
    Type: Application
    Filed: October 11, 2011
    Publication date: October 24, 2013
    Inventors: David Milstein, Ekambaram Balaraman, Chidambaram Gunanathan, Boopathy Gnanaprakasam, Jing Zhang
  • Publication number: 20130245127
    Abstract: A compound of formula (I) R-L-CO—X ??(I) (wherein R is a C10-24 unsaturated hydrocarbon group optionally interrupted by one or more heteroatoms or groups of heteroatoms selected from S, O, N, SO, SO2, said hydrocarbon group comprising at least 4 non-conjugated double bonds; L is a linking group forming a bridge of 1 to 5 atoms between the R group and the carbonyl CO; and X is an electron withdrawing group) for use in the treatment of rheumatoid arthritis.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 19, 2013
    Applicant: Avexxin AS
    Inventors: Astrid Jullumstro Feuerherm, Berit Johansen
  • Publication number: 20130231478
    Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
    Type: Application
    Filed: July 29, 2011
    Publication date: September 5, 2013
    Inventors: Ziao Xu, Yuanhai Zhao, Degang Li, Xiaoxiang Li
  • Patent number: 8513162
    Abstract: There is provided a halogen-containing organosulfur compound having a controlling effect on arthropod pests represented by the formula (I): wherein m represents 0, 1 or 2; n represents 0, 1 or 2; A represents an optionally substituted 3- to 8-membered saturated heterocyclic group; Q represents a fluorine atom or a C1-C5 haloalkyl group having at least one fluorine atom; R1, R1a and R3 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.; R2, R2a and R4 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.
    Type: Grant
    Filed: December 24, 2009
    Date of Patent: August 20, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Hiromasa Mitsudera