The Ring Is Bonded Directly To The Carbonyl Patents (Class 564/183)
  • Patent number: 11130754
    Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, and HET 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: October 12, 2018
    Date of Patent: September 28, 2021
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pingrong Liu, Craig Andrew Miller, Maolin Yu, Zhonghua Zhang, Sabine Ruppel, Anil K. Padayana
  • Patent number: 10570087
    Abstract: The present invention relates to a pseudo-ceramide compound and a preparation method therefor. According to the present invention, the pseudo-ceramide compound has a molecular structure and a function similar to those of a natural ceramide, can be readily synthesized, and has excellent solubility in an organic solvent and excellent stability, and thus the pseudo-ceramide compound can be used as an alternative to a natural ceramide. Therefore, the pseudo-ceramide compound of the present invention can be widely applied to a skin preparation for external use, a cosmetic composition, and the like for reinforcing and maintaining a skin barrier function.
    Type: Grant
    Filed: September 14, 2017
    Date of Patent: February 25, 2020
    Assignee: AMOREPACIFIC CORPORATION
    Inventors: Yung Hyup Joo, Jae Won Yoo, Yong Jin Kim, Ho Sik Rho, John Hwan Lee
  • Publication number: 20150126734
    Abstract: The present disclosure relates to a single pot process for preparation of a N,N-di substituted carboxamide compounds of formula (I), said process comprising: reacting a carboxylic acid with a di-substituted carbamoyl chloride in presence of an organic tertiary base to obtain the N,N-di substituted carboxamide compounds of formula (I). The process of the present disclosure involves a simple step, and it is energy and time saving process for preparation of N,N-di substituted carboxamides.
    Type: Application
    Filed: December 20, 2011
    Publication date: May 7, 2015
    Applicant: DIRECTOR GENERAL, DEFENCE RESEARCH & DEVELOPMENT ORGNISATION
    Inventors: Ambati Narasimha Rao, Kumaran Ganesan, Rajagopalan Vijayaraghavan
  • Publication number: 20150099900
    Abstract: An efficient and eco-friendly process for producing amide compounds comprising contacting a primary amine with molecular oxygen-containing gas, solvent and ammonia solution in the presence of a non-precious metal-containing ordered, mesoporous solid catalyst is disclosed.
    Type: Application
    Filed: March 4, 2013
    Publication date: April 9, 2015
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Darbha Srinivas, Anuj Kumar, Nepak Devadutta
  • Patent number: 8952179
    Abstract: Industrial synthesis process for the compound of formula (I):
    Type: Grant
    Filed: December 11, 2013
    Date of Patent: February 10, 2015
    Assignee: Les Laboratories Servier
    Inventors: Nicolas Robert, Jean-Michel Lerestif, Jean-Pierre Lecouve, Marina Gaillard, Loic Meunier, Philippe Letellier, Mathieu Boiret
  • Publication number: 20140378461
    Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides.
    Type: Application
    Filed: February 14, 2013
    Publication date: December 25, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Anthony Cornelius O'Sullivan, Olivier Loiseleur, Daniel Stierli, Torsten Luksch, Thomas Pitterna
  • Patent number: 8889731
    Abstract: This invention relates to compositions of one or more compounds that incorporate one or more allyl sulfide, allyl disulfide or allyl polysulfide moieties, or one or more allyl sulfide, allyl disulfide or allyl polysulfide moieties and one or more hydroxyl groups, used in effective amount in formulations, including emulsions, to repel blood-feeding ectoparasitic arthropods, including mosquitoes, and to deter them from landing and feeding when applied to the skin, clothing or environment of animals, including humans. Said compounds can include, but are not limited to, 8-allyl-sulfanyloctan-1-ol. This invention also relates to compositions comprising one or more of said compounds in further combination with other arthropod repellent and deterrent compounds, including vanillin. These compounds may be formulated with inert ingredients to form a liquid, gel, paste, soap, spray, aerosol or powder.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: November 18, 2014
    Assignee: Contech Enterprises Inc.
    Inventors: Regine M. Gries, Gerhard G. Gries, Grigori Khaskin, Norman Avelino, Cory Campbell
  • Patent number: 8809402
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: August 19, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Minmin Yang
  • Patent number: 8795631
    Abstract: The present invention relates to 18F radio-chemistry and in particular to a method for synthesising radiofluorinated amides and amines. The method of the invention has particular application in the radiosynthesis of a variety of 18F-labelled positron emission tomography (PET) tracers.
    Type: Grant
    Filed: October 20, 2009
    Date of Patent: August 5, 2014
    Assignees: HammerSmith Imanet Limited, GE Healthcare Limited
    Inventors: Robert James Domett Nairne, Erik Arstad, Matthias Eberhard Glaser
  • Patent number: 8664274
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel sulfonyl semicarbazides, carbonyl semicarbazides, semicarbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pinchinde, and VSV), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: July 6, 2011
    Date of Patent: March 4, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Dongcheng Dai, Tove Bolken, Dennis E. Hruby, Thomas R. Bailey
  • Publication number: 20140058106
    Abstract: Described herein are fluorinated organic compounds and methods of making fluorinated organic compounds, for example, using palladium complexes. Also described herein are compositions and kits containing compounds and palladium complexes described herein.
    Type: Application
    Filed: July 29, 2013
    Publication date: February 27, 2014
    Inventors: Tobias Ritter, Takeru Furuya, Hanns M. Kaiser
  • Patent number: 8658697
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel sulfonyl semicarbazides, carbonyl semicarbazides, semicarbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pinchinde, and VSV), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: February 25, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Dongcheng Dai, Tove Bolken, Dennis E. Hruby, Thomas R. Bailey
  • Publication number: 20130303757
    Abstract: One aspect of the present invention relates to novel compounds that can be used to prepare radiolabeled compounds in an effective manner. A second aspect of the present invention relates to a method of synthesizing radiolabeled compounds.
    Type: Application
    Filed: February 25, 2013
    Publication date: November 14, 2013
    Inventors: Duncan H. HUNTER, Mustafa JANABI
  • Publication number: 20130296383
    Abstract: The present invention relates to decahydro-1,4-methanonaphthalen carboxamide derivatives of formula (Ia) or (Ib); their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Application
    Filed: November 14, 2011
    Publication date: November 7, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jörg Greul, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann
  • Publication number: 20130231351
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Application
    Filed: January 23, 2013
    Publication date: September 5, 2013
    Applicant: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Publication number: 20130123505
    Abstract: A carboxamide can be produced in a high yield by a method for producing a carboxamide, for example, represented by formula (4): (wherein R1 and R3 are as defined below), the method comprising a step of allowing a carboxylic acid ester represented by formula (1): (wherein R1 represents an optionally substituented C1-C20 hydrocarbon group or an optionally substituented C3-C20 heterocyclic group, and R2 represents an optionally substituented C1-C20 hydrocarbon group), an amine represented by formula (2): R3—NH2 ??(2) (wherein R3 represents a hydrogen atom or an optionally substituented C1-C20 hydrocarbon group), and a formamide compound represented by formula (3): (wherein R3 is as defined above) to react in the presence of a metal alkoxide.
    Type: Application
    Filed: July 13, 2011
    Publication date: May 16, 2013
    Inventors: Junichi Tomokawa, Takahiro Kimura, Norihiko Hirata
  • Publication number: 20130035328
    Abstract: The invention relates to compounds having antiviral activity and methods utilizing the compounds to treat viral infections.
    Type: Application
    Filed: July 19, 2012
    Publication date: February 7, 2013
    Inventors: Peter William Gage, Gary Dinneen Ewart, Lauren Elizabeth Wilson, Wayne Best, Anita Premkumar
  • Publication number: 20130005972
    Abstract: A method for generating a radiolabeled tracer. The method includes providing a phosphine molecule having at least one carbocyclic, aromatic, or pyrrolidinyl ring with an OH substitute. The OH of this phosphines molecule is then condensed with an acid to produce a phosphine ester. Staudinger ligation is then performed to generate the radiolabeled tracer by treating the phosphine ester with a radiolabeled azide having a PET radioisotope moiety.
    Type: Application
    Filed: March 29, 2011
    Publication date: January 3, 2013
    Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.
    Inventors: Dhanalakshmi Kasi, Umesh Gangadharmath, Joseph Walsh, Hartmuth Kolb
  • Patent number: 8334305
    Abstract: Novel substituted amide inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: December 18, 2012
    Assignee: High Point Pharmaceuticals, LLC
    Inventor: Soren Ebdrup
  • Publication number: 20120302752
    Abstract: Methods are described for efficient and regioselective reactions that are Ru-catalyzed and either (i) amide-directed C—H, C—N, C—O activation/C—C bond forming reactions, (ii) ester-directed C—O and C—N activation/C—C bond forming reactions, or (iii) amide-directed C—O activation/hydrodemethoxylation reactions. All of these reactions of directed C—H, C—N, C—O activation/coupling reactions establish a catalytic base-free DoM-cross coupling process at non-cryogenic temperature. High regioselectivity, yields, operational simplicity, low cost, and convenient scale-up make these reactions suitable for industrial applications. Many previously unknown amide-substituted or ester-substituted aryl and heteroaryl compounds are presented with synthetic details also provided.
    Type: Application
    Filed: May 24, 2012
    Publication date: November 29, 2012
    Inventors: Yigang Zhao, Victor A. Snieckus
  • Patent number: 8278483
    Abstract: The present invention provides processes for the synthesis of novel Shikimic acid head-group containing non-toxic cationic amphiphiles capable of facilitating transport of biological macromolecules into cells.
    Type: Grant
    Filed: February 7, 2007
    Date of Patent: October 2, 2012
    Assignee: Council of Scientific & Industrial Research
    Inventors: Yenugonda Venkata Mahidhar, Arabinda Chaudhuri, Rama Mukherjee
  • Publication number: 20120232278
    Abstract: The present invention provides novel aryl pyrrolidines having an excellent insecticidal action as insecticides. Aryl pyrrolidines represented by the formula (I) and use thereof as insecticide.
    Type: Application
    Filed: May 15, 2012
    Publication date: September 13, 2012
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Jun MIHARA, Tetsuya MURATA, Daiei YAMAZAKI, Yasushi YONETA, Katsuhiko SHIBUYA, Eiichi SHIMOJO, Ulrich GÖRGENS
  • Publication number: 20120214858
    Abstract: Imidamide (amidine) analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumors.
    Type: Application
    Filed: August 16, 2010
    Publication date: August 23, 2012
    Applicant: University of Virginia Patent Foundation
    Inventors: Kevin R. Lynch, Timothy L. Macdonald, Thomas P. Mathews, Andrew Kennedy, Yugesh Kharel
  • Publication number: 20120190820
    Abstract: Provided are methods for forming a reactive S-nitroso thioacid (NTA), comprising nitrosation of a thioacid with a nitrosation reagent. Also provided are methods for: acylating a nucleophile including selective acylation with a high degree of selectivity toward amines over hydroxyls; amide or peptide bond formation; forming a dipeptide or polypeptide; and peptide coupling/ligation, comprising use of thioacid and amine starting materials, wherein the reactions are mediated by very reactive S-nitroso thioacid (NTA) intermediates enabling extremely fast reactions under mild conditions, providing for broad applications.
    Type: Application
    Filed: January 26, 2012
    Publication date: July 26, 2012
    Inventors: Ming Xian, Jia Pan
  • Publication number: 20120184438
    Abstract: This invention relates to agrochemical compositions comprising a benzamide compound of formula (I) where R1 is fluoro, methoxy or C1-4 alkyl; R2 and R3 are each independently optionally substituted C1-6 alkyl or optionally substituted C2-6 alkenyl; or R3 is hydrogen and R3 is optionally substituted C5-8 alkyl or optionally substituted C4-6 alkenyl or optionally substituted benzyl; or R2 and R3 and the nitrogen atom to which they are both attached together form an optionally substituted 5-, 6- or 7-membered ring, which ring optionally contains at least one further heteroatom selected from O, N and S; to the use of those benzamide compounds as solvents; to certain novel compounds of formula (I); and to a process for preparing those novel compounds.
    Type: Application
    Filed: July 15, 2010
    Publication date: July 19, 2012
    Applicant: SYNGENTA CROP PROTECTION, LLC
    Inventors: Gordon Alistair Bell, David Stock, Jeffrey Steven Wailes
  • Patent number: 8173841
    Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: May 8, 2012
    Assignee: Xention Limited
    Inventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
  • Publication number: 20120028960
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Application
    Filed: July 30, 2010
    Publication date: February 2, 2012
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Publication number: 20120004310
    Abstract: Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule.
    Type: Application
    Filed: May 27, 2011
    Publication date: January 5, 2012
    Inventors: Frank M. LONGO, Stephen M. Massa, Sandeep Gupta
  • Patent number: 8084614
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Grant
    Filed: April 4, 2008
    Date of Patent: December 27, 2011
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Richard Lowe, Willy Moree, Nicole Smith, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
  • Patent number: 8049037
    Abstract: This invention provides compounds as shown below, in which either all of Z1-6 are carbon or one of Z1-6 is nitrogen and the rest are carbon, and in which other substituents are defined herein, which are sphingosine-1-phosphate antagonists.
    Type: Grant
    Filed: August 12, 2009
    Date of Patent: November 1, 2011
    Assignee: Allergan, Inc.
    Inventors: Phong X. Nguyen, Todd M. Heidelbaugh, Ken Chow
  • Publication number: 20110213146
    Abstract: One aspect of the invention relates to a method of animation or amidation, comprising the step of combining a substrate, comprising a reactive C—H bond, and an amine or amide, comprising a reactive N—H bond, in the presence of an oxidizing agent and a metal-containing catalyst, thereby forming a product with a covalent bond between the carbon of the reactive C—H bond and the nitrogen of the reactive N—H bond.
    Type: Application
    Filed: September 3, 2009
    Publication date: September 1, 2011
    Applicant: Georgetown University
    Inventor: Timothy H. Warren
  • Patent number: 7994221
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel sulfonyl semicarbazides, carbonyl semicarbazides, semicarbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pinchinde, and VSV), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: January 17, 2007
    Date of Patent: August 9, 2011
    Assignee: Siga Technologies, Inc.
    Inventors: Dongcheng Dai, Tové C. Bolken, Dennis E. Hruby, Thomas R. Bailey
  • Publication number: 20110189089
    Abstract: The present invention relates to 18F radio-chemistry and in particular to a method for synthesising radiofluorinated amides and amines. The method of the invention has particular application in the radiosynthesis of a variety of 18F-labelled positron emission tomography (PET) tracers.
    Type: Application
    Filed: October 20, 2009
    Publication date: August 4, 2011
    Inventors: Robert James Domett Nairne, Erik Arstad, Matthias Eberhard Glaser
  • Publication number: 20110178102
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Application
    Filed: June 30, 2004
    Publication date: July 21, 2011
    Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
    Inventors: Vern L Schramm, Anthony A. Suave
  • Publication number: 20110159050
    Abstract: Disclosed is a process for modifying the morphology and/or polymorphism of an organic substance, which process comprises treating the solid substance, or a solution or dispersion thereof, with one or more amphiphilic proteins.
    Type: Application
    Filed: June 23, 2009
    Publication date: June 30, 2011
    Applicant: BASF SE
    Inventors: Andreas Hafner, Andreas Buthe, Paul Adriaan Van Der Schaaf, Franz Kaufmann, Gordon Bradley
  • Patent number: 7956010
    Abstract: Disclosed is an amide compound represented by the formula (1) below, which has excellent plant disease controlling activity. In the formula, X1 represents a fluorine atom or a methoxy group; X2 represents a hydrogen atom, a halogen atom, a C1-C4 alkyl group or the like; X3 represents a halogen atom, a C1-C4 alkyl group or the like; Z represents an oxygen atom or a sulfur atom; and A represents an A1-CR11R12R13 group, an A2-Cy1 group or an A3-Cy2 group, wherein A1 represents a CH2 group or the like, A2 represents a single bond, a CH2 group or the like, A3 represents a C1-C3 haloalkyl group, a C2-C4 alkenyl group or the like, Cy1 represents a C3-C6 cycloalkyl group substituted with a C1-C6 alkoxy group or the like, Cy2 represents a C3-C6 cycloalkyl group which may be substituted with a halogen atom or the like, R11 and R12 independently represent a C1-C4 alkyl group, and R13 represents a halogen atom, a hydroxyl group or the like.
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: June 7, 2011
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takashi Komori, Mayumi Kubota, Yuichi Matsuzaki
  • Publication number: 20110106241
    Abstract: Amidine analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumor cells.
    Type: Application
    Filed: October 2, 2010
    Publication date: May 5, 2011
    Inventors: Kevin R. Lynch, Timothy L. Macdonald, Yugesh Kharel, Thomas P. Mathews, Brian R. Wamhoff
  • Patent number: 7932421
    Abstract: The present invention provides N-cyclohexyl benzamide and benzeneacetamide compounds according to formula (I): where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, m, n, p, and q are as defined in the description; as well as pharmaceutical compositions comprising the same, methods of use of the compounds and compositions of the invention for the treatment of conditions associated with hydroxysteroid dehydrogenases (e.g., 11?-HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.
    Type: Grant
    Filed: December 12, 2007
    Date of Patent: April 26, 2011
    Assignee: Amgen Inc.
    Inventors: Chester Chenguang Yuan, Nianhe Han, Qingyian Liu, Dustin McMinn, Jay Powers
  • Publication number: 20110086405
    Abstract: Disclosed is a method for producing a hydroxylated form of a compound having an adamantane skeleton, which is useful as an intermediate for functional resins and pharmaceutical products, with high yield and at low cost. Specifically, a hydroxylated form of a compound having an adamantane skeleton can be obtained by using cytochrome P450. More specifically, an N-(5-hydroxy-2-adamantyl)-benzamide derivative can be produced by hydroxylating an N-(2-adamantyl)-benzamide derivative.
    Type: Application
    Filed: September 25, 2008
    Publication date: April 14, 2011
    Inventors: Taijiro Tomikawa, Yuuichi Mitsuda
  • Publication number: 20100324159
    Abstract: Embodiments of the present invention are directed to porous resins for solid phase extractions. The resins feature at least one hydrophobic component, at least one hydrophilic component and at least one ion exchange functional group. The resins exhibit superior wetting and ion exchange performance.
    Type: Application
    Filed: August 12, 2010
    Publication date: December 23, 2010
    Applicant: Waters Technologies Corporation
    Inventors: Peter Jeng Jong LEE, John E. O'Gara
  • Patent number: 7763750
    Abstract: A novel process for producing a 2-halogenobenzamide compound useful as a raw material or active ingredient for medicines and agricultural chemicals. The process, which is for producing a 2-halogenobenzamide compound represented by the general formula (I): (wherein R1, R2, R3, R4, and R6 may be the same or different and each represents hydrogen or C1-6 alkyl; R5 represents C1-6 alkyl; k is 1 or 2; Y1, Y2, Y3, and Y4 may be the same or different and each represents hydrogen, halogeno, etc.; and X represents chlorine, bromine, or iodine), is characterized by reacting an benzamide compound with a halogenating agent in the presence of a palladium catalyst to obtain a substituted benzamide compound and then reacting the resultant substituted benzamide compound with an oxidizing agent after or without isolating the substituted benzamide compound.
    Type: Grant
    Filed: December 22, 2004
    Date of Patent: July 27, 2010
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Noboru Abe, Hiroki Kodama, Akihiko Yoshiura
  • Publication number: 20100048701
    Abstract: Disclosed is an amide compound represented by the formula (1) below, which has excellent plant disease controlling activity. In the formula, X1 represents a fluorine atom or a methoxy group; X2 represents a hydrogen atom, a halogen atom, a C1-C4 alkyl group or the like; X3 represents a halogen atom, a C1-C4 alkyl group or the like; Z represents an oxygen atom or a sulfur atom; and A represents an A1-CR11R12R13 group, an A2-Cy1 group or an A3-Cy2 group, wherein A1 represents a CH2 group or the like, A2 represents a single bond, a CH2 group or the like, A3 represents a C1-C3 haloalkyl group, a C2-C4 alkenyl group or the like, Cy1 represents a C3-C6 cycloalkyl group substituted with a C1-C6 alkoxy group or the like, Cy2 represents a C3-C6 cycloalkyl group which may be substituted with a halogen atom or the like, R11 and R12 independently represent a C1-C4 alkyl group, and R13 represents a halogen atom, a hydroxyl group or the like.
    Type: Application
    Filed: April 25, 2008
    Publication date: February 25, 2010
    Inventors: Takashi Komori, Mayumi Kubota, Yuichi Matsuzaki
  • Patent number: 7618996
    Abstract: Compounds of Formula (I) that act as antagonists at the mu, kappa and/or delta opioid receptors and therefore useful in the treatment of diseases, conditions and/or disorders that benefit from such antagonism in animals are described herein. where R1, R2, R3, R4, R5, and R6 are described herein.
    Type: Grant
    Filed: September 10, 2007
    Date of Patent: November 17, 2009
    Assignee: Pfizer Inc.
    Inventors: Roger B. Ruggeri, George T. Magnus-Aryitey
  • Publication number: 20090270470
    Abstract: Compounds of formula I, wherein R1, Z, X, Y, M and R2 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical composition containing the same, methods of using the same for therapeutic purposes and methods of making the same.
    Type: Application
    Filed: May 8, 2006
    Publication date: October 29, 2009
    Applicant: AstraZeneca AB
    Inventors: Catrin Jonasson, Hakan Molin, Berit Molin, Didier Rotticci
  • Publication number: 20090069407
    Abstract: This invention relates to compositions of one or more compounds that incorporate one or more allyl sulfide, allyl disulfide or allyl polysulfide moieties, or one or more allyl sulfide, allyl disulfide or allyl polysulfide moieties and one or more hydroxyl groups, used in effective amount in formulations, including emulsions, to repel blood-feeding ectoparasitic arthropods, including mosquitoes, and to deter them from landing and feeding when applied to the skin, clothing or environment of animals, including humans. Said compounds can include, but are not limited to, 8-allyl-sulfanyloctan-1-ol. This invention also relates to compositions comprising one or more of said compounds in further combination with other arthropod repellent and deterrent compounds, including vanillin. These compounds may be formulated with inert ingredients to form a liquid, gel, paste, soap, spray, aerosol or powder.
    Type: Application
    Filed: March 28, 2008
    Publication date: March 12, 2009
    Applicant: PHERO TECH INTERNATIONAL INC.
    Inventors: Regine M. GRIES, Gerhard G. GRIES, Grigori KHASKIN, Norman AVELINO, Cory CAMPBELL
  • Publication number: 20090047379
    Abstract: The present invention relates to novel benzamide compounds may be used to provide desirable property of sweetness and to a foodstuff, chewing gum, medicinal product, toothpaste, alcoholic beverage, aqueous beverage, snack, sauce, confection, baked good, dairy product or cereal.
    Type: Application
    Filed: August 17, 2007
    Publication date: February 19, 2009
    Inventors: Mark L. Dewis, Debra Merrit, Kevin Miller, Zhen Chen, Laurens Reiber
  • Patent number: 7476764
    Abstract: There is provided a series of novel phenylcarboxyamides of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and Y as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: July 27, 2006
    Date of Patent: January 13, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yong-Jin Wu, Yunhui Zhang
  • Publication number: 20080319055
    Abstract: A method of providing a cooling sensation to the skin or the mucous membranes of the body by applying thereto a compound of Formula I in which X is H or (CH2)n—R, n is 0 or 1, Y and Z are selected independently from the group consisting of H, OH, phenyl, C1-C4 straight or branched alkyl, or, a C1-C4 straight or branched alkoxy, or X and Y form together a bivalent radical selected from the group consisting of —O—CH2—O—, —N?CH—O— and —N?CH—S— which forms together with the carbon atoms to which they are attached a 5-membered ring; and R is a group with non-bonding electrons, R1 is H or C1-C5 branched alkyl, R2 and R3 are C1-C4 branched alkyls, or R2 and R3 taken together form a monocyclic, bicyclic or tricyclic radical of up to 10 carbons provided that R1, R2 and R3 together comprise at least 6 carbons. The compounds may be incorporated into products such as dentifrices, foodstuffs, confectionery, beverages, and cosmetic and medicinal preparations.
    Type: Application
    Filed: March 15, 2006
    Publication date: December 25, 2008
    Applicant: GIVAUDAN SA
    Inventors: Lucienne Cole, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack
  • Publication number: 20080220005
    Abstract: The present invention provides a process for producing a comb polymer comprising the steps of: a) providing: (i) (w+z) molar equivalents of a monomer; (ii) one molar equivalent of an initiator compound of formula (IX), wherein B3 represents a halogen, B2 represents H or a halogen, Y1 represents a group capable of attaching the residue of an antibody or fragment thereof or capable of being converted into such a group, L represents a linker group, y is 1, 2 or 3, w is at least 1 and z is 0 or greater; (iii) a catalyst capable of catalysing the polymerisation of a plurality of the monomers to produce the comb polymer; and b) causing the catalyst to catalyse, in combination with the initiator, the polymerisation of a plurality of the monomers (i) to produce the comb polymer.
    Type: Application
    Filed: September 12, 2006
    Publication date: September 11, 2008
    Applicant: UCB PHARMA S.A.
    Inventors: Timothy John Norman, Benjamin Charles De Candole, Mezher Hussein Ali
  • Patent number: 7371887
    Abstract: Amphiphilic oligo(p-phenylene vinylene) compounds and methods of use en route to self-assembled composites and device fabrication.
    Type: Grant
    Filed: December 6, 2004
    Date of Patent: May 13, 2008
    Assignee: Northwestern University
    Inventors: Samuel I. Stupp, James F. Hulvat, Marina Sofos, Keisuke Tajima