Ring Or Polycyclo Ring System In Substituent E Is Attached Indirectly To The Carboxamide Nitrogen Or To An Amino Nitrogen In Substituent E By Acyclic Nonionic Bonding Patents (Class 564/185)
  • Patent number: 9308193
    Abstract: The present invention relates to kinase inhibitors for the treatment of cancer. Specifically, the present invention relates to the use of aminoactonitrile derivatives (AADs) in the treatment of cancer.
    Type: Grant
    Filed: March 22, 2013
    Date of Patent: April 12, 2016
    Assignee: PITNEY PHARMACEUTICALS PTY LIMITED
    Inventor: David Lawson Morris
  • Patent number: 9000216
    Abstract: An optically active spirolactone compound is highly enantioselectively produced by using an iodoarene derivative which can be synthesized easily and which is not racemized easily. A hypervalent iodine compound precursor (iodoarene derivative) which was able to be designed flexibly was synthesized from 2,6-dihydroxyiodoarene by using 1,2-aminoalcohol as a chiral source in short steps, a hypervalent iodine compound was prepared in a reaction system (in situ) by using a catalyst quantity of the resulting precursor in the presence of a stoichiometric quantity of m-CPBA, and a spirolactonization reaction of 3-(1-hydroxy-2-naphthyl)propionic acid was induced. As a result, a corresponding spirolactone compound was obtained at a high enantiomeric excess.
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: April 7, 2015
    Assignee: National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Muhammet Uyanik, Takeshi Yasui
  • Publication number: 20140308317
    Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.
    Type: Application
    Filed: December 9, 2013
    Publication date: October 16, 2014
    Applicant: CELLCEUTIX CORPORATION
    Inventors: Xiaodong Fan, Yongjiang Xu, Dahui Liu, Michael J. Costanzo
  • Publication number: 20140274692
    Abstract: A compound of formula (I) wherein R1 to R4 are, for example, each hydrogen, R5 is, for example, a substituted phenol; R6 is, for example, hydrogen; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 is, for example, A1 is N or C—X, A3 is C—X, and A2, A4 and A5 are C—H, where X, is, for example, halogen; and its use as a pesticidal agent.
    Type: Application
    Filed: October 31, 2012
    Publication date: September 18, 2014
    Applicant: Syngenta Participations AG
    Inventors: Olivier Loiseleur, Thomas Pitterna, Anthony Cornelius O'Sullivan, Torsten Luksch, Anna Kickova
  • Publication number: 20140113898
    Abstract: The invention relates to bisarylsulfone and dialkylarylsulfone compounds (e.g., compounds according to any of Formulas (I)-(IX) or compounds (1)-(227) of Tables 4 and 5) useful in treating conditions associated with calcium channel function, and particularly conditions associated with N-type calcium channel activity. The invention also relates to pharmaceutical compositions that include these bisarylsulfone compounds, as well methods for the treatment of conditions such as cardiovascular disease, epilepsy, cancer and pain.
    Type: Application
    Filed: November 4, 2011
    Publication date: April 24, 2014
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan A. Pajouhesh, Richard Holland, Yuanxi Zhou, Yongbao Zhu, Michael Edward Grimwood, Navjot Chahal
  • Publication number: 20140107340
    Abstract: The present invention is directed to benzamide containing compounds which inhibit the P2X7 receptor
    Type: Application
    Filed: October 10, 2013
    Publication date: April 17, 2014
    Applicant: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang, Allen T. Hopper
  • Publication number: 20140088157
    Abstract: Provided are an endoparasite control agent comprising a carboxamide derivative represented by the general formula (I): or a salt thereof as an active ingredient, and a method for controlling endoparasites, comprising orally or parenterally administering the endoparasite control agent.
    Type: Application
    Filed: March 1, 2012
    Publication date: March 27, 2014
    Applicants: NIHON NOHYAKU CO., LTD., THE UNIVERSITY OF TOKYO
    Inventors: Kiyoshi Kita, Akiyuki Suwa
  • Patent number: 8642576
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: February 4, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Publication number: 20130338364
    Abstract: An optically active spirolactone compound is highly enantioselectively produced by using an iodoarene derivative which can be synthesized easily and which is not racemized easily. A hypervalent iodine compound precursor (iodoarene derivative) which was able to be designed flexibly was synthesized from 2,6-dihydroxyiodoarene by using 1,2-aminoalcohol as a chiral source in short steps, a hypervalent iodine compound was prepared in a reaction system (in situ) by using a catalyst quantity of the resulting precursor in the presence of a stoichiometric quantity of m-CPBA, and a spirolactonization reaction of 3-(1-hydroxy-2-naphthyl)propionic acid was induced. As a result, a corresponding spirolactone compound was obtained at a high enantiomeric excess.
    Type: Application
    Filed: March 6, 2012
    Publication date: December 19, 2013
    Applicant: NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITY
    Inventors: Kazuaki Ishihara, Muhammet Uyanik, Takeshi Yasui
  • Publication number: 20130331392
    Abstract: The invention provides cycloalkyl guanidine compounds that inhibit F1F0-ATPase, and methods of using cyclalkyl guanidine compounds as therapeutic agents in therapy, such as treating an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: December 8, 2011
    Publication date: December 12, 2013
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood, Chad A. Van Huis
  • Publication number: 20130225612
    Abstract: The invention relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the invention relates to inhibitors of NADPH-oxidase.
    Type: Application
    Filed: May 3, 2012
    Publication date: August 29, 2013
    Applicant: EMORY UNIVERSITY
    Inventors: John David Lambeth, Thota Ganesh, Susan M. Smith, Aiming Sun
  • Patent number: 8436208
    Abstract: A process for the preparation of a substituted 2,2?-dithiophene is described, which process comprises the steps (a), (c) and optional steps (b) and (d): a reaction of a compound of the formula: with a suitable lithium organic compound, preferably Li-alkyl or Li-alkylamide; b) optional exchange of lithium against another metal selected from Mg1 Zn and Cu; c) reaction of the metallated intermediate obtained in step (a) or (b) with a suitable electrophil, which is CO2 or an aldehyde (addition reaction), or a compound Y?—R17 or Y?—R18-Z (substitution reaction), where R17 and R18 are as defined in claim 1; and optionally d) modification of the product obtained in step (c), e.g. by introducing one or more conjugating moieties Y ring closure between suitable monovalent residues R17, exchange or extension of functional groups or substituents such as addition to carbonyl or substitution of carbonyl in R17 or R18.
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: May 7, 2013
    Assignee: BASF SE
    Inventors: Hans Jürg Kirner, Frank Bienewald, Jean-Charles Flores, Olivier Frédéric Aebischer
  • Publication number: 20120322761
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Application
    Filed: August 29, 2012
    Publication date: December 20, 2012
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Patent number: 8314269
    Abstract: A compound of general formula (I) is disclosed. A process for preparing this compound, a fungicidal composition comprising a compound of general formula (I), and method for treating plants by applying a compound of general formula (I) or a composition comprising it are disclosed.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: November 20, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
  • Publication number: 20120252792
    Abstract: The invention provides methods, compositions, and kits for the inhibition of members of the Rho GTPase family. Specifically, the invention provides methods, compositions and kits for the inhibition of RhoA and/or RhoC transcriptional signalling. The invention finds use in treatment of Rho-mediated disease states (e.g., tumor metastasis, inflammation, inflammatory disease), Rho-mediated biological conditions, and in cell signaling research.
    Type: Application
    Filed: September 17, 2010
    Publication date: October 4, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Richard Neubig, Chris Evelyn, Jenny Ryu, Scott Larsen, Jessica Bell
  • Publication number: 20120252839
    Abstract: Compounds are described that are useful for treating an apoptosis-associated disease, which are specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Also described is a method for treating an apoptosis-associated disease in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of an active compound that is specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Several scaffolds of active compounds are described.
    Type: Application
    Filed: April 2, 2012
    Publication date: October 4, 2012
    Applicant: FRED HUTCHINSON CANCER RESEARCH CENTER
    Inventors: David HOCKENBERY, Julian SIMON
  • Patent number: 8202999
    Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: January 6, 2006
    Date of Patent: June 19, 2012
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Shoujun Chen, Zhi-Qiang Xia, Jun Jiang, Yu Xie, Junyi Zhang
  • Patent number: 8168826
    Abstract: The invention is directed to compounds and methods of synthesizing hydroxyethylamino amides and their use in treatment of aspartyl protease mediated diseases and conditions.
    Type: Grant
    Filed: December 3, 2009
    Date of Patent: May 1, 2012
    Assignee: Janssen Pharamcuetica N.V.
    Inventors: Steve J. Coats, Dennis J. Hlasta, Mark J. Schulz
  • Publication number: 20120010248
    Abstract: The present invention provides compounds that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity; and pharmaceutical compositions comprising the compounds. The present invention provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition. The present invention further provides assays for identifying agonists of ALDH2.
    Type: Application
    Filed: August 22, 2011
    Publication date: January 12, 2012
    Inventors: Daria Mochly-Rosen, Che-Hong Chen, Xiaohu Ouyang
  • Patent number: 8093241
    Abstract: The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: wherein A is phenyl which may be substituted by X, benzyl which may be substituted by X, naphthyl which may be substituted by X, a heterocyclic group which may be substituted by X, a fused heterocyclic group which may be substituted by X, indanyl (the indanyl may be substituted by halogen, alkyl or alkoxy) or tetrahydronaphthyl (the tetrahydronaphthyl may be substituted by halogen, alkyl or alkoxy), B is alkyl, cycloalkyl, phenyl which may be substituted by Y, a heterocyclic group which may be substituted by Y, or a condensed heterocyclic group which may be substituted by Y, each of R1 and R2 is alkyl, cyano or —CO2R14, or R1 and R2 may together form a 3- to 6-membered saturated carbocyclic ring, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, —COR15, —S(O)mR16 or —S(O)nNR17R18, which is useful as an active ingredient of pesticides.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: January 10, 2012
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Yuji Nakamura, Masayuki Morita, Tetsuo Yoneda, Kenji Izakura
  • Publication number: 20110281871
    Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.
    Type: Application
    Filed: July 26, 2011
    Publication date: November 17, 2011
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Patent number: 8039669
    Abstract: The invention provides methods and reagents for the metathesis of secondary amides via a transacylation mechanism employing catalytic quantities of an imide initiator and a Brønsted base. Equilibrium-controlled exchange between various amide reactant pairs is demonstrated for substrates bearing a variety of N-alkyl and N-aryl substituents.
    Type: Grant
    Filed: December 1, 2008
    Date of Patent: October 18, 2011
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Christen Bell Smith, Denis A. Kissounko, Samuel H. Gellman, Shannon S. Stahl
  • Publication number: 20110237678
    Abstract: A compound of general formula (I). A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.
    Type: Application
    Filed: April 26, 2011
    Publication date: September 29, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Darren MANSFIELD, Pierre-Yves COQUERON, Heiko RIECK, Philippe DESBORDES, Alain VILLIER, Marie-Claire GROSJEAN-COURNOYER, Pierre GENIX
  • 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: 8008305
    Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.
    Type: Grant
    Filed: July 28, 2008
    Date of Patent: August 30, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Publication number: 20110178077
    Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
    Type: Application
    Filed: June 17, 2009
    Publication date: July 21, 2011
    Inventors: Priscille Brodin, Thierry Christophe, Zaesung No, Jaeseung Kim, Auguste Genovesio, Denis Philippe Cedric Fenistein, Heekyoung Jeon, Fanny Anne Ewann, Sunhee Kang, Saeyeon Lee, Min Jung Seo, Eunjung Park, Monica Contreras Dominguez, Ji Youn Nam, Eun Hye Kim
  • Patent number: 7951973
    Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.
    Type: Grant
    Filed: November 21, 2006
    Date of Patent: May 31, 2011
    Assignee: Bayer CropScience AG
    Inventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
  • Patent number: 7947852
    Abstract: Compounds of formula (I): wherein: R1 represents alkyl, alkenyl, haloalkyl, polyhaloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, X represents a group N—OR2 wherein R2 represents a hydrogen atom or an alkyl group. Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: May 24, 2011
    Assignee: Les Laboratoires Servier
    Inventors: Said Yous, Mohamed Ettaoussi, Ahmed Sabaouni, Pascal Berthelot, Michael Spedding, Philippe Delagrange, Daniel-Henri Caignard, Mark Millan
  • Patent number: 7939552
    Abstract: Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.
    Type: Grant
    Filed: March 29, 2006
    Date of Patent: May 10, 2011
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Kunihiko Higashiura, Takashi Ogino, Kazuhito Furukawa
  • Publication number: 20110039866
    Abstract: Described herein are compounds useful as antagonists of sphingosine-1-phosphate receptors. Further described herein is the use of these compounds and related pharmaceutical compositions to treat disorders associated with sphingosine-1-phosphate-3 (S1P3) receptor modulation.
    Type: Application
    Filed: August 9, 2010
    Publication date: February 17, 2011
    Applicant: ALLERGAN, INC.
    Inventors: Phong X. Nguyen, Todd M. Heidelbaugh, Ken Chow, Michael E. Garst
  • Patent number: 7803841
    Abstract: The disclosure provides EP2 receptor agonist compounds and methods for using the compounds for treating conditions which can be alleviated by agonism of an EP2 receptor.
    Type: Grant
    Filed: December 30, 2008
    Date of Patent: September 28, 2010
    Assignee: Asterand UK Limited
    Inventors: Alexander William Oxford, Richard Jon Davis, Robert Alexander Coleman, Kenneth Lyle Clark, David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Mark Richard Ashton, Edward Andrew Boyd, Shirley Ann Brunton
  • Publication number: 20100216746
    Abstract: The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.
    Type: Application
    Filed: June 5, 2008
    Publication date: August 26, 2010
    Applicant: GLAXOSMITHKLINE LLC
    Inventors: PEK Yoke Chong, Andrew James Peat, Paul Richard Sebahar, Michael Youngman, Huichang Zhang
  • Publication number: 20100093707
    Abstract: The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: wherein A is phenyl which may be substituted by X, benzyl which may be substituted by X, naphthyl which may be substituted by X, a heterocyclic group which may be substituted by X, a fused heterocyclic group which may be substituted by X, indanyl (the indanyl may be substituted by halogen, alkyl or alkoxy) or tetrahydronaphthyl (the tetrahydronaphthyl may be substituted by halogen, alkyl or alkoxy), B is alkyl, cycloalkyl, phenyl which may be substituted by Y, a heterocyclic group which may be substituted by Y, or a condensed heterocyclic group which may be substituted by Y, each of R1 and R2 is alkyl, cyano or —CO2R14, or R1 and R2 may together form a 3- to 6-membered saturated carbocyclic ring, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, —COR15, —S(O)mR16 or —S(O)nNR17R18, which is useful as an active ingredient of pesticides.
    Type: Application
    Filed: December 17, 2009
    Publication date: April 15, 2010
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Yuji NAKAMURA, Masayuki Morita, Tetsuo Yoneda, Kenji Izakura
  • Publication number: 20100016374
    Abstract: Compounds of formula (I) and salts and solvates are provided: wherein R2 is selected from phenyl substituted with n R1 groups, and pyridyl substituted with n R1 groups; n=0, 1 or 2; each R1 is independently selected from the group consisting of halo, C1-4alkyl, C1-4alkoxy, haloC1-4alkyl, haloC1-4alkoxy and cyano; R3 is selected from hydrogen and C1-2 alkyl; R4 is selected from the group consisting of ethyl, n-propyl, i-propyl, n-butyl, i-butyl and t-butyl; or R3 and R4 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered heterocyclic ring optionally substituted with one or more groups X; each X is independently selected from the group consisting of C1-4alkyl, and haloC1-4alkyl; R12 is selected from the group consisting of hydrogen, fluoro, chloro, bromo, methyl and methylthio; R13 is selected from hydrogen, chloro and trifluoromethyl; R14 is selected from hydrogen, trifluoromethyl and chloro; R15 is selected from hydrogen, chloro and trifluoromethyl; R16 is selected
    Type: Application
    Filed: April 3, 2007
    Publication date: January 21, 2010
    Inventors: Steven Coulton, Martin Gilpin, Roderick Alan Porter
  • Patent number: 7642379
    Abstract: The invention relates to compounds of the general formula (I) wherein Ar, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, W, a, b, m, n, o and p are as defined in claim 1, and to any enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are particularly suitable for controlling parasites in warm-blooded animals.
    Type: Grant
    Filed: June 9, 2005
    Date of Patent: January 5, 2010
    Assignee: Novartis AG
    Inventors: Noëlle Gauvry, Pierre Ducray, Thomas Goebel, Ronald Kaminsky
  • Patent number: 7622612
    Abstract: The present invention relates to tricyclic colchicine derivatives represented by the formulas (I) or (II), pharmaceutically acceptable salts thereof, and a method for providing an immuno-suppressive or immuno-modulating effect, an anti-proliferative effect, an anti-inflammatory effect or a method for treating cancer comprising administering to a patient an effective amount of one or more colchicine derivatives:
    Type: Grant
    Filed: July 10, 2006
    Date of Patent: November 24, 2009
    Assignees: Chemtech Research Incorporation, KT & G Corporation
    Inventors: Dong Jo Chang, Eun Young Yoon, Gun Bong Lee, Soon Ok Kim, Wan Joo Kim
  • Publication number: 20090270510
    Abstract: The present invention relates to compounds of formula (I), or salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
    Type: Application
    Filed: December 21, 2005
    Publication date: October 29, 2009
    Applicant: GLAXO GROUP LIMITED
    Inventors: Daniel Marcus Bradley, Clive Leslie Branch, Wai Ngor Chan, Steven Coulton, Martin Leonard Gilpin, Andrew Jonathan Harris, Justine Yeun Quai Lai, Jacqueline Anne Macritchie, Howard Robert Marshall, David John Nash, Roderick Alan Porter, Simone Spada, Kevin Michael Thewlis, Simon Edward Ward
  • Publication number: 20090175788
    Abstract: Compounds of formula (I) and salts and solvates thereof, which are radiolabelled ligands for the glycine 1 transporter, are provided: wherein R1 is 3H, or a C1-6alkyl group incorporating a radionuclide selected from the group consisting of 3H, 11C, 14C, 13N, 15O, 76Br, 18F, 123I, 125I, 131I, 75Br, 76Br, 77Br and 82Br. Use of the compounds for the labelling and diagnostic imaging of the glycine 1 transporter functionality is disclosed.
    Type: Application
    Filed: June 20, 2007
    Publication date: July 9, 2009
    Inventors: Gabriella Gentile, Hugh Jonathan Herdon, Johannes Passchier, Roderick Alan Porter
  • Publication number: 20080287434
    Abstract: The invention relates to a compound of the general formula (I), as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound. The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.
    Type: Application
    Filed: March 19, 2008
    Publication date: November 20, 2008
    Applicant: SANOFI-AVENTIS
    Inventors: Agnes PAPPNE BEHR, Zoltan KAPUI, Peter ARANYI, Sandor BATORI, Veronika BARTANE BODOR, Lajos T. NAGY, Mihalyne T. Santa, Marton VARGA, Gyorgy FERENCZY, Endre MIKUS, Katalin URBAN-SZABO, Judit VARGANE SZEREDI, Erzsebet WALCZ, Edit SUSAN
  • Publication number: 20080227863
    Abstract: The invention relates to compounds of the general formula wherein R1, R2, R3, R4, R5, R6, R7, Ar1, X, Y, a and b are as defined in claim 1, and, if appropriate, enantiomers thereof. The active compounds have advantageous pesticidal properties. They are suitable, in particular, for the control of parasites in and on warm-blooded animals.
    Type: Application
    Filed: July 24, 2006
    Publication date: September 18, 2008
    Inventors: Pierre Ducray, Jorg Fruchtel, Noelle Gauvry, Sandra Schorderet Weber
  • Patent number: 7385085
    Abstract: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
    Type: Grant
    Filed: July 11, 2005
    Date of Patent: June 10, 2008
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Varghese John, Michel Maillard, Barbara Jagodzinska, Jose Aquino, Gary Probst, Jay Tung
  • Patent number: 7378448
    Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed
    Type: Grant
    Filed: March 2, 2005
    Date of Patent: May 27, 2008
    Assignee: Eli Lilly and Company
    Inventors: Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel
  • Patent number: 7312360
    Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables G, L, A, W, E, R2, R3, R4, R5, RN, and Rc are defined herein. These compounds interact with and inhibit the activity of the enzyme beta-secretase. These compounds are therefore useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions and methods of treatment of these diseases are also disclosed.
    Type: Grant
    Filed: December 6, 2002
    Date of Patent: December 25, 2007
    Assignees: Elan Pharmaceuticals, Inc., Pharmacia & Upjohn Company
    Inventors: Ruth TenBrink, Michel Maillard, Martha Warpehoski
  • Publication number: 20070270487
    Abstract: The present invention relates to a novel process suitable for large-scale production of phenyl propane derivatives as well as to novel intermediates in the process.
    Type: Application
    Filed: May 17, 2007
    Publication date: November 22, 2007
    Inventors: Martin Hedberg, Marita Hogberg, Weimin Tong
  • Patent number: 7223774
    Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are also useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
    Type: Grant
    Filed: April 21, 2004
    Date of Patent: May 29, 2007
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Jose Aquino, Varghese John, John Tucker, Roy Hom, Shon Pulley, Ruth Tenbrink
  • Patent number: 7214715
    Abstract: The present invention is substituted amines of formula (X) and of the formula (X?) useful in treating Alzheimer's disease and other similar diseases.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: May 8, 2007
    Assignees: Pharmacia & Upjohn, Elan Pharmaceuticals
    Inventors: James P. Beck, Lawrence Y. Fang, John N. Freskos, Andrea Gailunas, Roy Hom, Barbara Jagodzinska, Varghese John, Michel Maillard, Shon R. Pulley, Ruth E. TenBrink
  • Patent number: 7166746
    Abstract: The invention relates to N-bisaryl- and N-aryl-cycloalkylidenyl-a-hydroxy- and a-alkoxy acetic acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, C1–C12alkyl; C2–C12alkenyl; C2–C12alkynyl; C1–C12haloalkyl; R2 is hydrogen; optionally substituted alkyl; or optionally substituted alkynyl; R3 is optionally substituted aryl or optionally substituted heteroaryl; A is an optionally substituted saturated or unsaturated C3–C8-cycloalkylidene, optionally substituted phenylidene or optionally substituted saturated or unsaturated heterocyclylidene bridge, R4 and R5 are each independently hydrogen or an organic radical, and R6 is hydrogen; tri-C1–C4alkyl-silyl; di-C1–C4alkyl-phenylsilyl; C1–C4alkyl-diphenylsilyl; triphenylsilyl; optionally substituted alkyl; optionally substituted alkenyl or optionally substituted alkynyl.
    Type: Grant
    Filed: July 23, 2003
    Date of Patent: January 23, 2007
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Clemens Lamberth, Martin Zeller, Tibor Goegh
  • Patent number: 7041702
    Abstract: The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: May 9, 2006
    Assignee: Scion Pharmaceuticals, Inc.
    Inventors: Graham J. Durant, Seetharamaiyer Padmanabhan
  • Patent number: 6936736
    Abstract: A compound of the formula: wherein Ar is optionally substituted phenyl, etc.; n is 0, 1 or 2; R1 is hydogen atom, optionally substituted alkyl, etc.; R2 and R3 are independently optionally substituted alkyl, etc.; R4 and R5 are independently hydrogen atom or optionally substituted alkyl; R6 is hydrogen atom, hydroxy or alkyl; or a pharmaceutically acceptable salt thereof is useful as a medicament for treating retinal degenerative disorders and the like.
    Type: Grant
    Filed: March 26, 2002
    Date of Patent: August 30, 2005
    Assignee: Sumitomo Manufacturing Company Limited
    Inventors: Kazuhito Ikeda, Tohru Tatsuno, Hiroki Ogo, Toshio Nishihara, Tatsuya Fujibayashi, Ryu Nagata
  • Patent number: 6855847
    Abstract: A novel process for producing an optically active amide excellent in chemical selectivity and enantioselectivity by asymmetric hydrogenation of an ?,?-unsaturated amide and also allowing the reaction to proceed efficiently even when a trace amount of a catalyst is used relative to the substrate as compared with the amount in a conventional process. An optically active amide is produced by asymmetric hydrogenation of an ?,?-unsaturated amide derivative in the presence of a transition metal complex containing a specific phosphine-phosphorane compound.
    Type: Grant
    Filed: July 22, 2002
    Date of Patent: February 15, 2005
    Assignee: Takasago International Corporation
    Inventors: Kazuhiko Matsumura, Takao Saito