Chalcogen Attached Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/335)
  • Publication number: 20090181984
    Abstract: This invention relates to a novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivative and its use in the manufacture of pharmaceutical compositions. The compound of the invention is found to be a cholinergic ligand at the nicotinic acetylcholine receptors. Due to its pharmacological profile the compound of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Application
    Filed: May 29, 2007
    Publication date: July 16, 2009
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Daniel B. Timmermann, Steven Charles Loechel
  • Publication number: 20090181983
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, R3 and R11 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: December 13, 2006
    Publication date: July 16, 2009
    Inventor: James R. Corte
  • Publication number: 20090156575
    Abstract: The invention provides compounds of general formula wherein A, B, p, w, x, y, and z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: September 4, 2006
    Publication date: June 18, 2009
    Inventors: Lena Borjesson, Henrik Johansson, Anna Kristoffersson, Igor Shamovsky, Marco Skrinjar, Stephen Connolly, Tero Linnanen
  • Publication number: 20090156804
    Abstract: The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification. According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4?]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.
    Type: Application
    Filed: July 21, 2006
    Publication date: June 18, 2009
    Applicants: MITSUBISHI TANABE PHARMA CORPORATION, SANOFI-AVENTIS
    Inventors: Masahiro Okuyama, Fumiaki Uehara, Hiroshi Iwamura, Kazutoshi Watanabe
  • Publication number: 20090149477
    Abstract: This invention relates to a compound of formula I, wherein R1, R2, m, n and X are as defined herein, or a physiologically tolerated salt thereof, its pharmaceutical composition and use for lowering blood glucose, treating diabetes, or increasing insulin release.
    Type: Application
    Filed: November 10, 2008
    Publication date: June 11, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Elisabeth Defossa, Jochen Goerlitzer, Thomas Klabunde, Viktoria Dietrich, Siegfried Stengelin, Guido Haschke, Andreas Herling, Stefan Bartoschek
  • Publication number: 20090131384
    Abstract: The invention provides novel compounds, methods for treating or preventing a condition related to ER-stress, e.g. hypercholesterolemia, atherosclerosis and related conditions, and pharmaceutical compositions related thereto.
    Type: Application
    Filed: March 22, 2007
    Publication date: May 21, 2009
    Applicant: SYNDEXA PHARMACEUTICALS CORPORATION
    Inventors: Teoman Uysal, Nicholas D.P. Cosford
  • Publication number: 20090124636
    Abstract: The present invention provides compounds of formula (I) wherein R1 to R6 and m are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases, autoimmune diseases, pain, and. in the treatment of infection by HIV and genetically related retroviruses.
    Type: Application
    Filed: March 30, 2007
    Publication date: May 14, 2009
    Inventors: Christopher Gordon Barber, David Cameron Pryde, David Roy Fenwick, Peter Thomas Stephenson
  • Publication number: 20090124635
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, m and n are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.
    Type: Application
    Filed: January 12, 2006
    Publication date: May 14, 2009
    Applicant: PFIZER INC.
    Inventors: Christopher Gordon Barber, David Clive Blakemore, David Cameron Pryde, James Welsh Auld Kinnaird
  • Publication number: 20090118507
    Abstract: The present invention concerns the method for preparing (3-chloro-4-fluorophenyl)-(4-fluoro-4-{[(5-methyl-pyrimidin-2-ylmethyl)-amino]-methyl}-piperidin-1-yl)-methanone of formula (II) by condensation between 5-methyl-pyrimidin-2-methylamine of formula (I) and cyanohydrin of formula (III).
    Type: Application
    Filed: September 22, 2006
    Publication date: May 7, 2009
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Bernard Vacher, Jean-Louis Maurel, Serge Brunel
  • Publication number: 20090118307
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: October 15, 2008
    Publication date: May 7, 2009
    Applicant: CHEMOCENTRYX, INC.
    Inventors: Solomon Ugashe, Zheng Wei, J.J. Wright, Andrew Pennell
  • Patent number: 7521452
    Abstract: The present invention is generally directed to a process to directly prepare pharmaceutically acceptable salts enriched with respect to selected rotameric salts of a basic compound, by creative choice of an acid and a solvent medium. The process is particularly useful in preparing specific rotamers of pharmaceutically useful salts in desired preponderance of a rotamer.
    Type: Grant
    Filed: January 5, 2006
    Date of Patent: April 21, 2009
    Assignee: Schering Corporation
    Inventors: Wenxue Wu, Loc Thanh Tran, Bosco D'Sa, Feng Liang, William Leong, Hong-Chang Lee, Kevin Klopfer, Vijay Sabesen
  • Publication number: 20090099204
    Abstract: The present invention is to provide a compound represented by the general formula (1) exhibiting a high insecticidal effect and an insecticide comprising the compound as an active ingredient. The compound represented by the general formula (1) and an insecticide comprising the compound as an active ingredient, wherein, in the formula, A1, A2, A3 and A4 each represent a carbon atom or the like; R1 and R2 are each a hydrogen atom, an alkyl group or the like; G1 and G2 are each an oxygen atom or the like; X represents a hydrogen atom, a halogen atom or the like; n is an integer of 0 to 4; Q1 represents a substituted phenyl group, a substituted heterocyclic group or the like; Q2 represents a phenyl group having a haloalkyl sulfur group or the like, a heterocyclic group or the like.
    Type: Application
    Filed: June 20, 2006
    Publication date: April 16, 2009
    Applicant: Mitsui Chemicals, Inc.
    Inventors: Kei Yoshida, Yumi Kobayashi, Michikazu Nomura, Nobuyuki Kawahara, Hidenori Daido, Shinichi Inomata
  • Publication number: 20090099205
    Abstract: The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
    Type: Application
    Filed: June 14, 2006
    Publication date: April 16, 2009
    Inventors: Yuanxi Zhou, Elyse Bourque, Yongbao Zhu, Jonathan Langille, Markus Metz, Wen Yang, Ernest J. McEachern, Curtis Harwig, Ian R. Baird, Tong-Shuang Li, Renato T. Skerlj
  • Publication number: 20090099206
    Abstract: Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-2,2,2-trifluoro-1-(3?-methoxybiphenyl-4-yl)ethoxy)pyrimidin-4-yl)phenyl)propanoic acid and salts thereof are disclosed.
    Type: Application
    Filed: October 7, 2008
    Publication date: April 16, 2009
    Inventors: Shinya Iimura, Hui-Yin Li, Qiuling Song, Wenxue Wu, Matthew Mangzhu Zhao
  • Publication number: 20090088571
    Abstract: Disclosed is a multi-step process for preparing a compound of Formula I: wherein R1 to R3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.
    Type: Application
    Filed: December 5, 2008
    Publication date: April 2, 2009
    Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, BOEHRINGER INGELHEIM PHARMACEUTICALS, INC.
    Inventors: Xiao-jun WANG, Thomas WIRTH, Thomas NICOLA, Li ZHANG, Rogelio Perez FRUTOS, Yibo XU, Dhileepkumar KRISHNAMURTHY, Laurence John NUMMY, Richard J. VARSOLONA, Chris Hugh SENANAYAKE, Jutta KROEBER, Diana REEVES
  • Publication number: 20090069282
    Abstract: The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
    Type: Application
    Filed: May 15, 2008
    Publication date: March 12, 2009
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Dirk Stenkamp, Stephan Georg Mueller, Gerald Juergen Roth, Thorsten Lehmann-Lintz, Klaus Rudolf, Philipp Lustenberger, Kirsten Arndt, Ralf R. H. Lotz, Martin Lenter
  • Publication number: 20090054451
    Abstract: The present invention is directed to novel piperidine derivatives and to the use of piperidine derivatives of formula I as agonists of chemokine receptor activity.
    Type: Application
    Filed: August 4, 2008
    Publication date: February 26, 2009
    Applicant: Euroscreen S.A.
    Inventors: Jacques Huck, Frederic Ooms, Christian Tyrchan, Hamid R. Hoveyda
  • Patent number: 7495001
    Abstract: There are presented compounds of the formula wherein R6 and R7 is R4 and R5 or R5 and R6 together with the carbon atoms to which they are attached, form a ring as defined in the description and X1, X2, Y1 to Y4, R1 to R13 and n are as specified in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR? and/or PPAR? agonists.
    Type: Grant
    Filed: October 29, 2004
    Date of Patent: February 24, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Johannes Aebi, Alfred Binggeli, Uwe Grether, Georges Hirth, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr, Matthew Blake Wright
  • Publication number: 20090048238
    Abstract: The invention is concerned with novel biaryl derivatives of formula (I), wherein m, R1, R2, R3, X1, X2 and X3 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.
    Type: Application
    Filed: September 26, 2008
    Publication date: February 19, 2009
    Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
  • Patent number: 7488732
    Abstract: 2-Substituted pyrimidines of the formula I in which the index n and the substituents L, Ra, Rb, Rc, Rz, Ru, Rv, A?, A? and A?? are as defined in the description and: R1 is C3-C10-alkyl, C3-C10-alkenyl, C3-C10-alkynyl, C3-C12-cycloalkyl, C3-C10-cycloalkenyl or a five- to ten-membered saturated, partially unsaturated or aromatic heterocycle which is attached via carbon and contains one to four heteroatoms from the group consisting of O, N and S, R2 is halogen, cyano, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, C1-C4-alkoxy, C3-C4-alkenyloxy or C3-C4-alkynyloxy, where the alkyl, alkenyl and alkynyl radicals of R2 may be substituted by halogen, cyano, nitro, C1-C2-alkoxy or C1-C4-alkoxycarbonyl, and R3 is cyano, CO2Ra, C(?O)NRzRb, C(?O)—N—ORb, C(?S)—NRaRb, C(?NORa)NRzRb, C(?NRa)NRzRb, C(?O)NRa—NRzRb, C(?N—NRzRc)NRaRb, C(?O)Ra, C(?NORb)Ra, C(?N—NRzRb)Ra, CRaRb—ORz, CRaRb—NRzRc, ON(?CRaRb), O—C(?O)Ra, NRaRb?, NRa(C(?O)Rb), NRa(C(?O)ORb), NRa(C(?O)—NRzRb), NRa(C(?NRc)Rb), NRa(N?CRcRb), NRa—NRzRb, NRz—ORa, NRa(C(
    Type: Grant
    Filed: March 30, 2004
    Date of Patent: February 10, 2009
    Assignee: BASF Aktiengesellschaft
    Inventors: Jordi Tormo i Blasco, Carsten Blettner, Bernd Müller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Peter Schäfer, Frank Schieweck, Anja Schwögler, Oliver Wagner, Maria Scherer, Siegfried Strathmann, Ulrich Schöfl, Reinhard Stierl
  • Patent number: 7482349
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated ?-amyloid deposits or ?-amyloid levels in a patient.
    Type: Grant
    Filed: June 15, 2005
    Date of Patent: January 27, 2009
    Assignee: Wyeth
    Inventors: Michael S. Malamas, James J. Erdei, Iwan S. Gunawan, Ping Zhou, Yinfa Yan, Dominic A. Quagliato
  • Publication number: 20090023730
    Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.
    Type: Application
    Filed: February 25, 2008
    Publication date: January 22, 2009
    Applicant: ACHILLION PHARMACEUTICALS
    Inventors: Avinash Phadke, Dawei Chen, Milind Deshpande, Andrew Thurkauf, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
  • Patent number: 7476673
    Abstract: Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RAR? agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: January 13, 2009
    Assignee: Allergan, Inc.
    Inventors: Kwok Yin Tsang, Santosh Sinha, Xiaoxia Liu, Smita Bhat, Roshantha A. Chandraratna
  • Publication number: 20090010860
    Abstract: Disclosed is the use of the compounds of formula wherein Q is —OH; —OR7; —NH2; —NHR7; —NR7R8; or —N?R9; T is —COR5; —CN; or —SO2—(C6-C12)aryl; R1 is hydrogen; —OR7, —SR7; —NHR7; —NR7R8; C1-C22alkyl; C2-C12Alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl, C2-C11heteroaralkyl; C6-C10aryl; or C1-C9heteroaryl; R2 and R3 independently from each other are C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl, C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl; C3-C12cycloheteroalkyl; C2-C11heteroaralkyl, C6-C10aryl; or C1-C9heteroaryl; R4 is cyano; COR7, COOR7; CONH2; CONHR7; CONR7R8; SO2(C6-C12)aryl, C2-C12alk-1-enyl; C3-C12cycloalk-1-enyl; C2-C12alk-1-inyl; C2-C12heteroalkyl, C3-C5heterocycloalkyl, C6-C10aryl; or C1-C9heteroaryl; R5 is —COR7; —COOR7; —OR7; —SR7, —NHR7, —NR7R8; C2-C12alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12alkylphenyl; C1-C12alkoxy-C8-C10aryl; C1-C12heteroalkyl; C2-C11heteroaralkyl; C
    Type: Application
    Filed: June 20, 2005
    Publication date: January 8, 2009
    Inventors: Barbara Wagner, Frank Bienewald, Heinz Wolleb, Olof Wallquist, Bernd Herzog, Thomas Ehlis, Jurg Haase
  • Publication number: 20080318976
    Abstract: ?-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R2a is selected from (1) a group selected from Ra. (2)(CH2)nNRbC(O)Ra. (3)(CH2)nNRbSO2Rd. (4)(CH2)nNRbCO2Ra.(5)(CH2)k-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen.nitro, cyano.ORa.SRa.C1-4 alkyl and C1-3 haloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N.O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or (b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6)(CH2)kCO2Ra. and (7)(CH2)C(O)NRbRc.
    Type: Application
    Filed: December 17, 2004
    Publication date: December 25, 2008
    Inventors: Michael R. Wood, Neville J. Anthony, Mark G. Bock, Scott D. Kuduk
  • Publication number: 20080308770
    Abstract: A quaternary nitrogen-containing corrosion inhibitor of formula wherein is an aromatic, nitrogen-containing ring of 5 to 14 ring atoms, optionally containing an additional N, O or S ring atom and optionally substituted with one or more alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, amino, aminoalkyl, alkoxy, hydroxylalkyl, or cyano groups, or a mixture thereof, Y is a group of formula —OC(O)R1 or —C(O)R1; L is C1-C10 alkyl, C2-C10 alkenyl or a group of formula CH2CH(OR2)CH2—; R1 is C8-C20 alkyl or C8-C20 alkenyl; R2 is H or C(O)R1; R3 and R4 are independently selected from H, alkyl, alkenyl, amino, alkoxy, hydroxylalkyl and cyano; and X is Br, Cl or I is particularly useful for inhibiting corrosion in oil and gas field applications.
    Type: Application
    Filed: June 14, 2007
    Publication date: December 18, 2008
    Inventor: Laxmikant Tiwari
  • Patent number: 7465736
    Abstract: An azole derivative of formula (I) a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of preparing the azole derivative of formula (I).
    Type: Grant
    Filed: June 13, 2003
    Date of Patent: December 16, 2008
    Assignee: Laboratoires Serono S.A.
    Inventors: Pascale Gaillard, Jean-Pierre Gotteland, Isabelle Jeanclaude-Etter, Matthias Schwarz, Russel J. Thomas
  • Publication number: 20080306071
    Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
    Type: Application
    Filed: April 28, 2008
    Publication date: December 11, 2008
    Applicant: Adolor Corporation
    Inventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
  • Patent number: 7462637
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: October 20, 2004
    Date of Patent: December 9, 2008
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Terence A. Kelly, Jin Mi Kim, René Marc Lemieux, Matt Aaron Tschantz
  • Patent number: 7459556
    Abstract: The present invention relates to a process for preparing substituted 8-azabicyclo[3.2.1]octan-3-ols having the structural formula I or a pharmaceutically acceptable salt or solvate thereof, wherein R is benzyl, R5-benzyl, allyl, —C(O)R6, —C(O)OR8 or —CH(R7)2; R1 is optionally substituted aryl or optionally substituted heteroaryl; and R5, R6, R7 and R8 are as defined in the specification; comprising a) reacting an amine of formula II R—NH2??II with 2,5-dimethoxytetrahydrofuran or HC(O)(CH2)2C(O)H, and C(O)(CH2C(O)OR4)2, wherein R4 is H or alkyl, to obtain a compound of formula III b) reacting a compound of formula III with I-R1, alkyl lithium, and optionally a lithium salt, to obtain a compound of formula I; and c) optionally converting a compound of formula I wherein R is benzyl, R5-benzyl, allyl, —C(O)R6 or —C(O)OR8 to a compound of formula I wherein R is —CH(R7)2. Intermediates in the process are also claimed.
    Type: Grant
    Filed: September 13, 2005
    Date of Patent: December 2, 2008
    Assignee: Schering-Plough Ltd.
    Inventors: Ingrid Mergelsberg, Gerald Werne
  • Publication number: 20080293743
    Abstract: The invention provides compounds of formula (I): wherein R1, R2, A, A1 and B are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy. The compounds are useful as MMP inhibitors.
    Type: Application
    Filed: December 14, 2005
    Publication date: November 27, 2008
    Applicant: ASTRAZENECA AB
    Inventors: Balint Gabos, Michael Lundkvist, Magnus Munck Af Rosenschold, Igor Shamovsky, Pavol Zlatoidsky
  • Publication number: 20080293717
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: July 2, 2008
    Publication date: November 27, 2008
    Applicant: CHEMOCENTRYX, INC.
    Inventors: SOLOMON UGASHE, Zheng Wei, J.J. Wright, Andrew Pennell
  • Publication number: 20080287446
    Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Application
    Filed: March 22, 2006
    Publication date: November 20, 2008
    Inventor: Craig J. Mossman
  • Publication number: 20080280915
    Abstract: N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.
    Type: Application
    Filed: February 9, 2007
    Publication date: November 13, 2008
    Inventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Zoltan L. Benko, Gregory T. Whiteker, John F. Daeuble
  • Publication number: 20080275062
    Abstract: There is provided compounds of Formula (I) and salts, solvates, and physiologically functional derivatives thereof: wherein R1 is hydrogen or C1-6alkyl; n is 1, 2, 3 or 4; R2 is aryl, optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, C1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy, C1-4alkoxycarbonyl, C1-4alkylsulfonyl and a group R3R4NSO2 (wherein R3 and R4 are independently hydrogen or C1-4alkyl) and a 5- or 6-membered heteroaryl group; or n is 0 and R1 and R2, together with the nitrogen atom to which they are joined, form a 5- or 6-membered monocyclic heterocyclic ring or a 9- or 10-membered bicyclic heterocyclic ring wherein at least the ring which contains the nitrogen atom to which R1 and R2 are joined is non-aromatic, and wherein the 5- or 6-membered monocyclic heterocyclic ring or the 9- or 10-membered bicyclic heterocyclic ring is optionally substituted by one or two groups selected from the group consistin
    Type: Application
    Filed: January 28, 2005
    Publication date: November 6, 2008
    Inventors: David Harold Drewry, David Kendall Jung, James Andrew Linn, Robert Neil Hunter, Dennis Lee, Robert A. Stavenger, Clark Sehon
  • Publication number: 20080269217
    Abstract: Provided are MC4-R binding compounds of the formula XVII: wherein L2 is a linker group, and P1, P2, P3, P4, Z1, Z2, Z3, Z4, Z5, t, s, and R are as described in the specification. Methods of using the compounds to treat MC4-R associated disorders, such as disorders associated with weight loss, are also provided.
    Type: Application
    Filed: May 1, 2008
    Publication date: October 30, 2008
    Applicant: Ore Pharmaceuticals, Inc.
    Inventors: Tricia J. Vos, Michael E. Solomon, Christopher F. Claiborne, Martin P. Maguire, Mingshi Dai, Michael Patane, Thoma H. Marsilje
  • Publication number: 20080247991
    Abstract: In part, the present invention relates to a compound or polymer comprising a non-protein-binding moiety and at least one protein-binding group. The present invention relates to a method of screening compounds or polymers for the property of inhibiting protein aggregation in solution, a method of preparing a compound or polymer having the property of protein aggregation inhibition in solution, a method of classifying a compound or polymer as either inhibitory of protein aggregation in solution or not inhibitory of protein aggregation in solution, and to a method of determining the preferential binding coefficient, ?XP, of an additive in a protein solution. The present invention also relates to a method of suppressing or preventing aggregation of a protein in solution, a method of decreasing the toxicological risk associated with administering a protein to a mammal in need thereof, and a method of facilitating native folding of a recombinant protein in solution.
    Type: Application
    Filed: February 28, 2005
    Publication date: October 9, 2008
    Inventors: Bernhardt L. Trout, Daniel I.C. Wang, Brian M. Baynes
  • Publication number: 20080242653
    Abstract: Compounds of formula (I) wherein R1, R2, R3, R3a, R3b, R4, and R5 are defined in the description, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Application
    Filed: December 14, 2007
    Publication date: October 2, 2008
    Inventors: Huaqing Liu, Lawrence A. Black, Youssef L. Bennani, Marlon D. Cowart, Zhenping Tian, Paul J. Brackemeyer
  • Patent number: 7427693
    Abstract: Compounds that are useful in compositions for flat panel displays, for example, are provided. The compounds provided are polar, and are useful in low threshold voltage mixtures. The compounds provided have the general structure: CpCOCH2[A]nZ1[B]mZ2PhX1X2Y, where CpCOCH2 is the structure: A and B are independently in each instance selected from the group consisting of 1,4-cyclohexane, 1,4-phenyl, 1,3-dioxan-5,2-diyl; pyridine-5,2-diyl; and pyrimidin-5,2-diyl; n and m are independently in each instance 0, 1 or 2; Z1 and Z2 are independently a single bond, —(CH2)2—, CF2O, OCF2, CH2O, OCH2, —C?C—, COO, OOC; and Y is selected from the group consisting of: F, Cl, CN, OCH2F, CHF2, OCF3, and CF3.
    Type: Grant
    Filed: April 3, 2007
    Date of Patent: September 23, 2008
    Assignee: Daily Polymer Corporation
    Inventor: Xinhua Chen
  • Publication number: 20080227782
    Abstract: This invention is directed to a compound of formula (I): wherein R1, R2, R3 and L1 are as defined herein, a pharmaceutical composition comprising the compound, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma and/or chronic obstructive pulmonary disease (COPD).
    Type: Application
    Filed: April 4, 2008
    Publication date: September 18, 2008
    Applicant: AVENTIS PHARMACEUTICALS INC
    Inventors: Suzanne C. Aldous, John Ziqi Jiang, Jinqi Lu, Liang Ma, Lan Mu, Harry Randall Munson, Jeffrey Stephen Sabol, Sukanthini Thurairatnam, Christopher Loren Vandeusen
  • Publication number: 20080214548
    Abstract: The invention relates to compounds of the formula I and salts thereof, to a process for their manufacture, to their use in the treatment of (especially cysteine protease, such as UCH-L3- and/or USP-2 dependent) diseases or for the manufacture of pharmaceutical formulations against these diseases, methods of treatment of warm-blooded animals comprising administering the compounds and/or their salts to said animals and pharmaceutical preparations, especially for the treatment of the diseases, comprising said compounds and/or salts.
    Type: Application
    Filed: July 17, 2006
    Publication date: September 4, 2008
    Inventors: Stefanie Flohr, Pascal Furet, Patricia Imabach, Ulrich Hommel, Hans-Ulrich litscher, Shirley Gil Parrado, Ulrich Hassiepen, Johann Zimmermann
  • Publication number: 20080194598
    Abstract: The present application relates to pyrimidinecarboxylic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders, in particular dyslipidaemias and arteriosclerosis.
    Type: Application
    Filed: March 7, 2006
    Publication date: August 14, 2008
    Applicant: Bayer HealthCare AG
    Inventors: Elisabeth Woltering, Arounarith Tuch, Elke Dittrich-Wengenroth, Axel Kretschmer, Lars Barfacker, Marcus Bauser, Peter Ellinghaus, Klemens Lustig, Elisabeth Pook, Olaf Weber
  • Patent number: 7407974
    Abstract: The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.
    Type: Grant
    Filed: April 18, 2005
    Date of Patent: August 5, 2008
    Assignee: Pfizer Inc.
    Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
  • Publication number: 20080176867
    Abstract: The invention relates to compounds of formula (I): Wherein X, R1, R2, R3, R4 and R5 are as defined herein. The invention also relates to a method for preparing the aforementioned compounds and to their therapeutic use.
    Type: Application
    Filed: January 3, 2008
    Publication date: July 24, 2008
    Applicant: SANOFI-AVENTIS
    Inventors: Francis BARTH, Christian CONGY, Patrick GUEULE, Murielle RINALDI-CARMONA
  • Publication number: 20080139455
    Abstract: Novel compounds, compositions comprising compounds, and methods for preparing and using compounds are described herein. Methods of treating or ameliorating various conditions, including insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia, manifestations of Syndrome X, congestive heart failure, inflammatory disease of the cardiovascular system, atherosclerosis, restenosis, sepsis, type 1 diabetes, liver damage, and cachexia, by administering compounds described herein. Compounds presented herein may be used to modulate serine palmitoyltransferase activity.
    Type: Application
    Filed: October 12, 2007
    Publication date: June 12, 2008
    Applicant: Forbes Medi-Tech (Research), Inc.
    Inventor: John J. Nestor
  • Patent number: 7378446
    Abstract: The object of the present invention is to provide a compound useful for the prevention and treatment of viral infectious diseases, and particularly liver diseases caused by HCV infection due to its having a high degree of replication inhibitory activity against HCV, its production method, an intermediate compound useful for its production and a pharmaceutical composition containing these compounds, and the present invention relates to a compound represented by the formula (I): (wherein A represents —(CH2)n—, etc.; B represents —(C?O)—, etc.; D represents —(CH2)m—R?, etc.; E represents a hydrogen atom, etc.; G represents —(CH2)p-J, etc.; bond Q represents a single bond or double bond; and R1, R2 and R3 may be the same or different and each represent a hydrogen atom, etc.), a prodrug thereof or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 9, 2004
    Date of Patent: May 27, 2008
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Masayuki Sudoh, Takuo Tsukuda, Miyako Masubuchi, Kenichi Kawasaki, Takeshi Murata, Fumio Watanabe, Hiroshi Fukuda, Susumu Komiyama, Tadakatsu Hayase
  • Publication number: 20080096892
    Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellu-lar activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Even more specifically, the invention provides compounds for modulating c-Kit kinase activity and methods of treating diseases mediated by c-Kit activity utilizing the compounds and pharmaceutical compositions thereof.
    Type: Application
    Filed: August 27, 2004
    Publication date: April 24, 2008
    Applicant: Exelixis, Inc.
    Inventors: Wei Cheng, Erick Wang Co, Moon Hwan Kim, Rhett Ronald Klein, Donna T. Le, Amy Lew Tsuhako, John M. Nuss, Wei Xu, William Bajjalieh
  • Patent number: 7358239
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: April 15, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 7358244
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: May 27, 2004
    Date of Patent: April 15, 2008
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Adam Hughes
  • Patent number: RE40558
    Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: October 28, 2008
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Zaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko