Ring Nitrogen Is Shared By Two Cyclos Patents (Class 544/263)
  • Publication number: 20090312312
    Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.
    Type: Application
    Filed: February 12, 2009
    Publication date: December 17, 2009
    Applicant: ALANTOS PHARMACEUTICALS HOLDING, INC.
    Inventors: Christoph STEENECK, Christian GEGE, Frank RICHTER, Heiko KROTH, Matthias HOCHGURTEL, Michael ESSERS, Joshua VAN VELDHUIZEN, Bert NOLTE, Brian M. GALLAGHER, JR., Tim FEUERSTEIN, Matthias SCHNEIDER, Torsten ARNDT, Hongbo DENG, Ralf BIESINGER, Xinyuan WU, Harald BLUHM, Irving SUCHOLEIKI, Arthur G. TAVERAS
  • Publication number: 20090281122
    Abstract: The present invention provides compounds of formula (4), and their pharmaceutically acceptable salts and solvates, which are useful as inhibitors of the Hepatitis C virus (HCV) polymerase enzyme and are also useful for the treatment of HCV infections in HCV-infected mammals. The present invention also provides pharmaceutical compositions comprising compounds of formula (4), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formula (4).
    Type: Application
    Filed: July 15, 2009
    Publication date: November 12, 2009
    Inventors: Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Angelica Linton, John Howard Tatlock
  • Publication number: 20090253716
    Abstract: The present invention provides an amino-imidazolone compound of formula I Also provided are compositions and methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.
    Type: Application
    Filed: June 18, 2009
    Publication date: October 8, 2009
    Inventors: Michael Sotirios Malamas, James Joseph Erdei, Iwan Suwandi Gunawan, Pawel Wojciech Nowak, Boyd Lynn Harrison
  • Publication number: 20090197883
    Abstract: The instant invention provides compounds of Formula (I) which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Application
    Filed: March 3, 2006
    Publication date: August 6, 2009
    Inventors: Helen M. Armstrong, Linda L. Chang, Richard Frenette, Dwight MacDonald, Hyun O. Ok, Michel Therien, Feroze Ujjainwalla
  • Patent number: 7550471
    Abstract: The invention relates to 5-alkyl-7-aminotriazolopyrimidines of the formula (I) and to the salts thereof. In said formula substituents have the following meanings: R1 and R2 each is a hydrogen atom or a group of alkyl, alcenyl, haloalkyl, cycloalky, phenyl or naphtyle, saturated, unstaturated or aromatic heterocycle having from five to six members which contain from one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or R1 and R2 can from together with a connecting them nitrogen atom a cycle of 5 to 6 members containing from one to four nitrogen atoms or from one to three nitrogen atoms and one sulfur or oxygen atom, R3 is a cycloalkyl or bicycloalkyl group, R1, R2 and R3 can be substituted in conformity with a description, and X is an alkyl or alkyl halide group. The inventive methods and intermediary products necessary for producing said compounds, agents containing them and the use therefore for fighting against harmful mushroom are also disclosed.
    Type: Grant
    Filed: November 4, 2003
    Date of Patent: June 23, 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, Eberhard Ammermann, Siegfried Strathmann, Ulrich Schöfl, Reinhard Stierl
  • Publication number: 20090156594
    Abstract: The present disclosure provides heterocyclic protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.
    Type: Application
    Filed: May 21, 2008
    Publication date: June 18, 2009
    Applicant: SGX Pharmaceuticals, Inc.
    Inventors: Pierre-Yves Bounaud, Christopher Ronald Smith, Elizabeth A. Jefferson, Jorg Hendle, Patrick S. Lee, Angelina Marie Thayer, Gavin Charles Hirst
  • Publication number: 20090137607
    Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.
    Type: Application
    Filed: August 14, 2008
    Publication date: May 28, 2009
    Inventors: Swen Holder, Matthias Vennemann, Gerrit Beneke, Armin Zulch, Volker Gekeler, Thomas Beckers, Astrid Zimmermann, Hemant Joshi
  • Publication number: 20090137547
    Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.
    Type: Application
    Filed: December 7, 2007
    Publication date: May 28, 2009
    Inventors: Christoph Steeneck, Christian Gege, Frank Riohter, Holko Kroth, Mouhlee Hochgueriel, Michael Essors, Joshua Van Veldhulzen, Bert Nolte, Brian M. Gallaghor, JR., Tim Feuerstein, Matthias Schneider, Toralen Arndt, Hongbo Deng, Ralf Blesinger, Xinyuan Wu, Harald Bluhm, Irving Sucholelld, Arthur G. Taverse
  • Patent number: 7514441
    Abstract: There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and ?is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.
    Type: Grant
    Filed: August 21, 2003
    Date of Patent: April 7, 2009
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuneo Yasuma, Akira Mori, Masahiro Kawase, Hiroyuki Kimura, Masato Yoshida, Albert Charles Gyorkos, Scott Alan Pratt, Christopher Peter Corrette
  • Patent number: 7507739
    Abstract: This invention relates to certain 6-[(substituted)phenyl]triazolopyrimidine compounds or pharmaceutically acceptable salts thereof, and compositions containing said compounds or pharmaceutically acceptable salts thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 24, 2004
    Date of Patent: March 24, 2009
    Assignee: Wyeth
    Inventors: Nan Zhang, Semiramis Ayral-Kaloustian, Thai Nguyen, Yanzhong Wu, Wei Tong
  • Patent number: 7501383
    Abstract: The invention relates to 5,6-dialkyl-7-amino-triazolopyrimidines of formula (I), in which the substituents are defined as follows: R1 represents alkyl or alkoxyalkyl; R2 represents alkyl, R1 and/or R2 being substituted according to the description. The invention also relates to a method for producing said compounds, to agents containing the latter and to their use for controlling plant-pathogenic fungi.
    Type: Grant
    Filed: March 8, 2005
    Date of Patent: March 10, 2009
    Assignee: BASF Aktiengesellschaft
    Inventors: Jordi Tormo I Blasco, Carsten Blettner, Bernd Müller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Joachim Rheinheimer, Peter Schäfer, Frank Schieweck, Anja Schwögler, Oliver Wagner, Matthias Niedenbruck, Maria Scherer, Siegfried Strathmann, Ulrich Schöfl, Reinhard Stierl
  • Publication number: 20090062286
    Abstract: The invention relates to SMYD3 methyltransferase (SMYD3), SMYD3 binding pockets or SMYD3-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to SMYD3 methyltransferase protein, complexes of SMYD3 methyltransferase protein, homologues thereof, or SMYD3-like protein or protein complexes.
    Type: Application
    Filed: May 5, 2008
    Publication date: March 5, 2009
    Inventors: Kenneth William Foreman, Frances E. Park, Lee Arnold
  • 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
  • Publication number: 20090023921
    Abstract: The present invention relates to methods and compounds useful in the preparation of compounds of the formula (I).
    Type: Application
    Filed: August 16, 2006
    Publication date: January 22, 2009
    Inventors: Christopher Frederick Matthews, Robert William Scott, John Lloyd Tucker
  • Publication number: 20080300135
    Abstract: The present invention relates to 7-amino-6-heteroaryl-1,2,4-triazolo[1,5-a]pyrimidine compounds of the formula (I), in which the substituents Het, R1, R2, X and Y are as defined in the claims and in the description.
    Type: Application
    Filed: July 6, 2006
    Publication date: December 4, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Oliver Wagner, Sarah Ulmschneider, Udo Hunger
  • Publication number: 20080293713
    Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, and R3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.
    Type: Application
    Filed: April 30, 2008
    Publication date: November 27, 2008
    Applicant: Abbott Laboratories
    Inventors: Gang Liu, Zhili Xin, Philip R. Kym, Andrew J. Souers
  • Publication number: 20080280759
    Abstract: 6-(2-Halo-4-alkoxyphenyl)triazolopyrimidines of the formula I in which the substituents are as defined below: R1 is alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, cycloalkenyl, halocycloalkenyl, alkynyl, haloalkynyl or phenyl, naphthyl, or a five- or six-membered saturated, partially unsaturated or aromatic heterocycle which contains one to four heteroatoms from the group consisting of O, N and S, R2 is hydrogen or one of the groups mentioned under R1, R1 and R2 together with the nitrogen atom to which they are attached may also form a five- or six-membered heterocyclyl or heteroaryl which is attached via N and may contain one to three further heteroatoms from the group consisting of O, N and S as ring members; R3 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, phenylalkyl, mono- or dialkoxyalkyl; R1, R2 and/or R3 may be substituted as mentioned in the description; L is hydrogen, fluorine or chlorine; X is cyano, alkyl, alkoxy, alkenyloxy, haloalkoxy or haloa
    Type: Application
    Filed: December 14, 2004
    Publication date: November 13, 2008
    Inventors: Jordi Tormo i Blasco, Carsten Blettner, Bernd Muller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Joachim Rheinheimer, Peter Schafer, Frank Schieweck, Anja Schwogler, Oliver Wagner, Maria Scherer, Siegfried Strathmann, Ulrich Schofl, Reinhard Stierl
  • Publication number: 20080275065
    Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Application
    Filed: October 10, 2005
    Publication date: November 6, 2008
    Applicants: SYNGENTA CROP PROTECTION, INC., SYNGENTA LIMITED
    Inventors: Anthony Cornelius O'Sullivan, David John Hughes, Andre Jeanguenat, Michel Muehlebach, Olivier Loiseleur
  • Publication number: 20080262000
    Abstract: 5-Alkoxyalkyl-6-alkyl-7-aminoazolopyrimidines of the formula I in which the substituents are defined as follows: R1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxyalkyl, cyanoalkyl, and benzyloxyalkyl, where the groups in the aliphatic or aromatic moiety may be unsubstituted or may have substitution by from one to three groups Ra: Ra is halogen, cyano, nitro, hydroxy, cycloalkyl, alkoxy, alkylthio, and NRARB; RA, RB are hydrogen and alkyl; R2 is alkoxyalkyl, phenoxyalkyl, alkylthioalkyl, and phenylthioalkyl, which groups may have no substitution or may have substitution according to the description; R3 is hydrogen and alkyl; A is N and C—RA; processes for preparation of these compounds, compositions comprising them, and their use for controlling phytopathogenic harmful fungi.
    Type: Application
    Filed: February 14, 2006
    Publication date: October 23, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Peter Schafer, Udo Hunger, Maria Scherer, Harald Kohle, Helmut Schiffer, Thomas Grote, Jochen Dietz, Wassilios Grammenos, Jan Klaas Lohmann, Bernd Muller, Joachim Rheinheimer, Frank Schieweck, Anja Schwogler
  • Publication number: 20080255156
    Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein: X1 and X2 are 1-3 substituents independently selected from the group consisting of H, alkyl, halo, —CF3, —OCF3, alkoxy, —OH and —CN; n is 0, 1 or 2; and R and R1 are H or alkyl; also disclosed is the use of the compounds in the treatment of CNS diseases such as Parkinson's disease, alone or in combination with other agents for treating CNS diseases, pharmaceutical compositions comprising them and kits comprising the components of the combinations.
    Type: Application
    Filed: June 25, 2007
    Publication date: October 16, 2008
    Inventors: Martin C. Clasby, Samuel Chackalamannil, Andrew Stamford
  • Publication number: 20080248952
    Abstract: Substituted triazolopyrimidines of the formula I in which the substituents are as defined below: R1 is alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, cycloalkenyl, halocycloalkenyl, alkynyl, haloalkynyl or phenyl, naphthyl, or a five- or six-membered saturated, partially unsaturated or aromatic heterocycle comprising one to four heteroatoms from the group consisting of O, N and S, R2 is hydrogen or a group R1, R1 and R2 together with the nitrogen atom, to which they are attached, may also form a five- or six-membered heterocyclyl or heteroaryl which is attached via N and which may comprise one to three further heteroatoms from the groups consisting of O, N and S as ring member and/or may be substituted according to the description; L is fluorine, chlorine or methyl; X is cyano, C1-C4-alkyl, C1-C4-alkoxy or C1-C2-haloalkoxy, where X is not methyl if R1 and R2 together are n-pentylene or 3-methyl-n-pentylene and L is fluorine, or R1 and R2 together are 3-methyl-n-pentylene and L is
    Type: Application
    Filed: July 6, 2005
    Publication date: October 9, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Carsten Blettner, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Udo Hunger, Bernd Muller, Matthias Niedenbruck, Joachim Rheinheimer, Peter Schafer, Frank Schieweck, Anja Schwogler, Oliver Wagner, Barbara Nave, Maria Scherer, Siegfried Strathmann, Ulrich Schofl, Reinhard Stierl
  • Publication number: 20080249113
    Abstract: Fungicidal mixtures, comprising as active components 1) a 5-chloro-6-phenyl-7-heterocyclylaminotriazolopyrimidine of the formula I, in which D together with the nitrogen atom forms a pyrrolidine, piperidine or azepine ring, which rings are unsubstituted or substituted by one or two methyl groups or by an ethyl, propyl or butyl group; and L is methyl, fluorine or chlorine; and 2) at least one active compound II selected from the following groups: A) azoles; B) strobilurins; C) acylalanines; D) amine derivatives; E) anilinopyrimidines; F) dicarboximides; G) cinnamides and analogs; H) antibiotics; K) dithiocarbamates; L) heterocyclic compounds according to the description; M) sulfur and copper fungicides; N) nitrophenyl derivatives; O) phenylpyrroles; P) sulfenic acid derivatives; Q) other fungicides according to the description; or R) growth retardants; in a synergistically effective amount, novel triazolopyrimidines, methods for controlling harmful fungi using compounds or mixtures of a compound I
    Type: Application
    Filed: July 28, 2005
    Publication date: October 9, 2008
    Inventors: Carsten Blettner, Jochen Dietz, Wassilios Grammenos, Thomas Grote, Udo Hunger, Bernd Muller, Matthias Niedenbruck, Joachim Rheinheimer, Peter Schafer, Frank Schieweck, Anja Schwogler, Barbara Nave, Maria Scherer, Siegfried Strathmann, Ulrich Schofl, Reinhard Stierl
  • Publication number: 20080242860
    Abstract: The present invention relates to a silver halide color photographic light-sensitive material wherein at least one of light-sensitive silver halide emulsion layers includes a silver halide emulsion having a silver chloride content of at least 95 mol % and a silver iodide content of 0.05 mol % to 0.75 mol % and/or a silver bromide content of 0.05 mol % to 4.00 mol % and further at least one compound represented by the following formula (I): X-(L)n-Y ??Formula (I) wherein X represents a group adsorptive to a silver halide, L represents a divalent connecting group comprising one of an atom and an atomic group including at least one of a carbon atom, a nitrogen atom, a sulfur atom and an oxygen atom, Y denotes a reducible group and n denotes an integer of 0 or 1.
    Type: Application
    Filed: June 3, 2008
    Publication date: October 2, 2008
    Applicant: FUJIFILM CORPORATION
    Inventors: Atsushi Matsunaga, Tadashi Inaba, Shinichi Ichikawa
  • Publication number: 20080227795
    Abstract: The invention relates to substituted triazolopyrimidines of formula (I), with the substituents as follows: R1, R2=H, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, cycloalkenyl, halocycloalkenyl, alkinyl, haloalkinyl, phenyl, naphthyl, or a five- or six-membered saturated, partially unsaturated or aromatic heterocycle, comprising one to four heteroatoms of the group O, N or S, R1 and R2 can, together with the nitrogen atom to which it is attached, form a five- or six-membered heterocycle or heteroaryl, bonded via N and containing one to three further heteroatoms from the group O, N and S as ring members, substituted as per the description, L1=fluorine, chlorine or bromine, L2=H, alkyl or alkoxy and X=halogen, cyano, alkyl, haloalkyl, alkoxy or haloalkoxy. The invention further relates to methods and intermediates for production of said compounds, agents comprising the same and use thereof for controlling fungal pests harmful to plants.
    Type: Application
    Filed: January 15, 2005
    Publication date: September 18, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Jordi Tormo i Blasco, Carsten Blettner, Bernd Muller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Joachim Rheinheimer, Peter Schafer, Frank Schieweck, Anja Schwogler, Oliver Wagner, Maria Scherer, Siegfried Strathmann, Ulrich Schofl, Reinhard Stierl
  • Publication number: 20080227796
    Abstract: The present invention relates to novel 7-amino-6-hetaryl-1,2,4-triazolo[1,5-a]pyrimidine compounds and to their agriculturally acceptable salts, and also to their use for controlling harmful fungi, and also to crop protection compositions comprising at least one such compound as active component.
    Type: Application
    Filed: December 16, 2005
    Publication date: September 18, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Oliver Wagner, Thomas Grote, Joachim Rheinheimer, Barbara Nave, Reinhard Stierl
  • Publication number: 20080214395
    Abstract: 5-Methyl-6-phenyltriazolopyrimidinylamines of the formula I, in which the substituents are defined according to the description, processes for preparing these compounds, compositions comprising them and their use for controlling phytopathogenic harmful fungi.
    Type: Application
    Filed: July 20, 2006
    Publication date: September 4, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Jochen Dietz, Thomas Grote, Udo Hunger, Jan Klaas Lohmann, Bernd Muller, Jens Renner, Sarah Ulmschneider, Wassilios Grammenos, Joachim Rheinheimer
  • Patent number: 7419982
    Abstract: The present invention relates to crystalline forms of 5-chloro-6-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-N-[(1S)-2,2,2-trifluoro-1-methylethyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine salts; processes for the production thereof; pharmaceutical compositions thereof; and methods for inhibiting tumor growth therewith.
    Type: Grant
    Filed: May 19, 2006
    Date of Patent: September 2, 2008
    Assignee: Wyeth Holdings Corporation
    Inventors: Fang Fang Qi, Mannching Sherry Ku, Yanzhong Wu, David M. Blum
  • Publication number: 20080207455
    Abstract: 5,6-Dialkyl-7-aminoazolopyrimidines of the formula I in which the substituents are as defined below: R1 is alkyl or alkoxyalkyl, where the aliphatic groups may be substituted as defined in the description; R2 is CHRxCH3, cyclopropyl, CH?CH2 or CH2CH?CH2; Rx is hydrogen, CH3 or CH2CH3 or halomethyl; A is N or CH; R3 is methyl, and, if A is CH, additionally hydrogen; processes and intermediates for preparing these compounds, compositions comprising them and their use for controlling phytopathogenic harmful fungi.
    Type: Application
    Filed: March 1, 2006
    Publication date: August 28, 2008
    Applicant: BASF AKTINGESELLSCHAFT
    Inventors: Peter Schafer, Udo Hunger, Maria Scherer, Harald Kohle, Helmut Schiffer, Thomas Grote, Jochen Dietz, Wassilios Grammenos, Jan Klaas Lohmann, Bernd Muller, Joachim Rheinheimer, Frank Schieweck, Anja Schwogler
  • Patent number: 7417041
    Abstract: Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-? signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.
    Type: Grant
    Filed: February 20, 2004
    Date of Patent: August 26, 2008
    Assignees: Pfizer Inc., Pfizer Products Inc.
    Inventors: Laura C. Blumberg, Michael J. Munchhof, Andrei Shavnya
  • Publication number: 20080200480
    Abstract: 6-Phenyltriazolopyrimidinylamines of the formula I, in which the substituents are defined according to the description, processes for preparing these compounds, compositions comprising them and their use for controlling phytopathogenic harmful fungi.
    Type: Application
    Filed: July 20, 2006
    Publication date: August 21, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Jochen Dietz, Thomas Grote, Udo Hunger, Jan Klaas Lohmann, Bernd Muller, Jens Renner, Sarah Ulmschneider, Wassilios Grammenos, Joachim Rheinheimer
  • Publication number: 20080200675
    Abstract: A process for preparing substituted phenylmalonic esters of the formula in which R is alkyl and Q is halogen, alkyl, alkoxy, haloalkyl or haloalkoxy and the index m is an integer from 1 to 5, where the groups Q can be identical or different if the index m is greater than 1, comprising steps A), B) and C): A) reaction of compounds of the formula II, in which the variables are as defined for formula I to give compounds of the formula III, B) conversion of the compounds of the formula III into ketals of the formula IV in which R? is C1-C4-alkyl or benzyl, C) hydrolysis of the compounds of the formula IV to give compounds of the formula I; novel phenylmalonic ester derivatives, and their use as intermediates.
    Type: Application
    Filed: June 23, 2006
    Publication date: August 21, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Norbert Gotz, Volker Maywald, Michael Keil
  • Publication number: 20080188494
    Abstract: The use of 5-alkyl-6-phenylalkyl-7-aminoazolopyrimidines of the formula I in which the variables are as defined below: Y is alkylene, alkenylene or alkynylene, optionally substituted by alkyl groups; R1 is halogen, cyano, nitro, hydroxyl, mercapto, alkyl, haloalkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, haloalkoxy, alkenyloxy, alkynyloxy, alkylthio, NRARB, alkylcarbonyl, phenyl, naphthyl, or a five- or six-membered saturated, partially unsaturated or aromatic heterocycle which contains one to four heteroatoms from the group consisting of O, N and S; RA, RB is hydrogen, alkyl or alkylcarbonyl; n is zero, 1, 2, 3 or 4; R2 is alkyl, alkenyl, cycloalkyl, alkoxyalkyl or alkylthioalkyl; R3 is hydrogen, halogen, cyano, NRARB, hydroxyl, mercapto, alkyl, haloalkyl, cycloalkyl, alkoxy, alkylthio, cycloalkoxy, cycloalkylthio, carboxyl, formyl, alkylcarbonyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, phenyl, phenoxy, phenylthio, benzyloxy, benzylthio, alkyl-S(O)m—; m is 0, 1 or 2; A is N or
    Type: Application
    Filed: April 24, 2006
    Publication date: August 7, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Jochen Dietz, Wassilios Grammenos, Thomas Grote, Udo Hunger, Jan Klaas Lohmann, Bernd Muller, Joachim Rheinheimer, Peter Schafer, Frank Schieweck, Anja Schwogler
  • Publication number: 20080176870
    Abstract: The present invention relates generally to heterobicyclic containing pharmaceutical agents, and in particular, to heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic metalloprotease inhibiting compounds that exhibit an increased potency in relation to currently known metalloprotease inhibitors.
    Type: Application
    Filed: November 20, 2007
    Publication date: July 24, 2008
    Inventors: Bert Nolte, Irving Sucholeiki, Tim Feuerstein, Brian M. Gallagher, Xinyuan Wu, Christoph Steeneck, Christian Gege, Hongbo Deng, Joshua Van Veldhuizen, Arthur Taveras
  • Publication number: 20080167324
    Abstract: Compounds of Formula I are provided, as are methods for their preparation. The variables in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agents(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
    Type: Application
    Filed: February 28, 2006
    Publication date: July 10, 2008
    Inventors: Yuelian Xu, Linghong Xie
  • Patent number: 7396835
    Abstract: The present invention provides a process for the preparation of 6-[(substituted)phenyl]-triazolopyrimidine dicarboxylic acid salt and as a hydrated salt having the structural formula (I) wherein: R1 is CF3 or C2F5; R2 is H or C1-C3 alkyl; n is an integer of 2, 3, or 4; X is Cl or Br; R3 and R4 are each independently H or C1-C3 alkyl; or R3 and R4 when optionally taken together with the nitrogen atom to which each is attached form a 4 to 6 membered saturated heterocyclic ring having 1-2 nitrogen atoms and 0-1 oxygen atoms or 0-1 sulfur atoms, and optionally substituted with R5; R5 is C1-C3 alkyl; wherein the dotted line is an optional bond.
    Type: Grant
    Filed: December 8, 2004
    Date of Patent: July 8, 2008
    Assignee: Wyeth
    Inventors: Yanzhong Wu, Jean Schmid, Jay Thomas Afragola, David Blum, Semiramis Ayral-Kaloustian
  • Publication number: 20080139581
    Abstract: 2-Substituted 7-aminoazolopyrimidines of the formula I in which the substituents are as defined below: R1 is hydrogen, halogen, cyano, alkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkoxyalkyl, benzyloxyalkyl, alkoxyalkenyl or alkoxyalkynyl; R2 is hydrogen, halogen, cyano, alkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkoxyalkyl and alkylthioalkyl, where the carbon chains in R1 and/or R2 may be substituted according to the description; R3 is halogen, cyano, NRARB, hydroxyl, mercapto, alkyl, haloalkyl, cycloalkyl, alkoxy, alkylthio, cycloalkoxy, cycloalkylthio, carboxyl, formyl, alkylcarbonyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, phenyl, phenoxy, phenylthio, benzyloxy, benzylthio, alkyl-S(O)m—; A is N and CRx; Rx is hydrogen or one of the groups mentioned under R3; processes and intermediates for preparing these compounds, compositions comprising them and their use for controlling phytopathogenic harmful fungi.
    Type: Application
    Filed: March 2, 2006
    Publication date: June 12, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Wassilios Grammenos, Thomas Grote, Udo Hunger, Jan Klaas Lohmann, Bern Muller, Joachim Rheinheimer, Peter Schafer, Anja Schwogler, Michael Rack
  • Publication number: 20080132412
    Abstract: The present invention relates to 7-amino-6-heteroaryl-1,2,4-triazolo[1,5-a]pyrimidine compounds of the formula (I) in which the meanings of the substituents R1, R2, Het, X and Y are as defined in the description.
    Type: Application
    Filed: December 15, 2005
    Publication date: June 5, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Oliver Wagner, Udo Hunger
  • Publication number: 20080125445
    Abstract: 5,6-Dialkyl-7-aminoazolopyrimidines of the formula I in which the substituents are as defined below: R1 is alkyl or alkoxyalkyl, R2 is alkyl, where R1 and/or R2 may be substituted according to the description, A is N or CH, and R3 is CH3 and, if A is CH, additionally hydrogen; processes and intermediates for preparing these compounds, compositions comprising them and their use for controlling phytopathogenic harmful fungi.
    Type: Application
    Filed: March 1, 2006
    Publication date: May 29, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Peter Schafer, Udo Hunger, Maria Scherer, Harald Kohle, Helmut Schiffer, Thomas Grote, Jochen Dietz, Wassilios Grammenos, Jan Klaas Lohmann, Bernd Muller, Joachim Rheinheimer, Frank Schieweck, Anja Schwogler
  • Publication number: 20080119493
    Abstract: The invention relates to 5,6-dialkyl-7-amino-triazolopyrimidines of formula (I), in which the substituents are defined as follows: R1 represents alkyl, alkoxyalkyl, alkenyl or alkynyl; R2 represents alkyl, alkoxyalkyl, alkenyl or alkynyl, R1 and/or R2 being substituted according to the description. The invention also relates to a method for producing said compounds, to agents containing the latter and to their use for controlling plant-pathogenic fungi.
    Type: Application
    Filed: March 8, 2005
    Publication date: May 22, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Jordi Tormo i Blasco, Carsten Blettner, Bernd Muller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Joachim Rheinheimer, Peter Schafer, Frank Schieweck, Anja Schwogler, Oliver Wagner, Matthias Niedenbruck, Maria Scherer, Siegfried Strathmann, Ulrich Schofl, Reinhard Stierl, Udo Hunger
  • Patent number: 7351826
    Abstract: The invention provides compounds of Formula (I) that bind to GABAA receptors. In the above formula, variables are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g.
    Type: Grant
    Filed: February 16, 2004
    Date of Patent: April 1, 2008
    Assignee: Neurogen Corporation
    Inventors: Linghong Xie, Bingsong Han, Yuelian Xu
  • Patent number: 7339058
    Abstract: The N-arylsulfilimine-catalyzed coupling of aromatic sulfonyl chlorides with N-([1,2,4]triazolopyrimidin-2-yl)amines to form N-([1,2,4]triazolo-pyrimidin-2-yl)aryl sulfonamides is improved by the selection of 3-picoline or 3,5-lutidine as the base.
    Type: Grant
    Filed: March 24, 2005
    Date of Patent: March 4, 2008
    Assignee: Dow AgroSciences LLC
    Inventor: Christopher Thomas Hamilton
  • Patent number: 7329663
    Abstract: The invention provides a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pharmaceutically acceptable salt thereof and further provides a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by interacting with tubulin and microtubules and promoting microtubule polymerization which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: February 12, 2008
    Assignee: Wyeth
    Inventors: Mark R. Schmitt, Donald R. Kirsch, Jane E. Harris, Carl F. Beyer, Klaus-Jüergen Pees, Paul A. Carter, Waldemar Pfrengle, Guido Albert
  • Patent number: 7300908
    Abstract: Triazolopyrimidines of formula (I), wherein the index and substituents have the following meaning: n=0 or a whole number of 1-5; R=halogen, cyano, hydroxy, cyanate, alkyl, alkenyl, alkinyl, halogenalkyl, halogenalkenyl, alkoxy, alkenyloxy, alkinyloxy, halogenalkoxy, cycloalkyl, cycloalkenyl, cycloalkoxy, alkoxycarbonyl, alkenyloxycarbonyl, alkinyloxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkoximinoalkyl, alkenyloximinocarbonyl, alkinyloximinoalkyl, alkylcarbonyl, alkenylcarbonyl, alkinylcarbonyl, cycloalkylcarbonyl or a five to ten membered saturated, partially unsaturated or aromatic heterocycle, containing one to four heteroatoms from the group O, N or S; R1=alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, phenyl, naphthyl or a five to ten membered saturated, partially unsaturated or aromatic heterocycle, containing one to four heteroatoms from the group O, N or S, R and/or R1 being able to be substituted according to the description; R2=alkyl, alkenyl or alkinyl which can be s
    Type: Grant
    Filed: July 3, 2002
    Date of Patent: November 27, 2007
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Müller, Hubert Sauter, Markus Gewehr, Wassilios Grammenos, Jordi Tormo i Blasco, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schäfer, Frank Schieweck, Michael Rack, Gisela Lorenz, Siegfried Strathmann, Eberhard Ammermann, Reinhard Stierl
  • Publication number: 20070259860
    Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
    Type: Application
    Filed: April 25, 2007
    Publication date: November 8, 2007
    Applicants: AstraZeneca AB, NPS PHARMACEUTICALS, INC.
    Inventors: Andreas Wallberg, Karolina Nilsson, Kenneth Granberg, Saswati Ghosal, Abdelmalik Slassi, Louise Edwards, Methvin Isaac, Tao Xin, Tomislav Stefanac, Peter Dove
  • Patent number: 7271170
    Abstract: Compounds of Formula I are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
    Type: Grant
    Filed: July 23, 2004
    Date of Patent: September 18, 2007
    Assignee: Neurogen Corporation
    Inventors: Linghong Xie, Bingsong Han, Yuelian Xu, George Maynard, Bertrand L. Chenard, Kenneth Shaw, Yang Gao
  • Patent number: 7205316
    Abstract: Compounds of formula (I) wherein R1 or R2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R1, R2, R3, R3a, R3b, R4, R5, L, X, X?, Y, Y?, Z, and Z? are as defined herein, 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: Grant
    Filed: May 6, 2005
    Date of Patent: April 17, 2007
    Assignee: Abbott Laboratories
    Inventors: Robert J. Altenbach, Lawrence A. Black, Marlon D. Cowart, Huaqing Liu
  • Patent number: 7189680
    Abstract: The invention relates to novel triazolopyrimidines of the formula in which R1, R2, R3 and X have the meanings given in the disclosure, and acid addition salts thereof, to a plurality of processes for preparing these novel substances, and to their use for controlling unwanted microorganisms. The invention further relates to novel amines and carbamates of the formulae indicated in the description and to processes for preparing these intermediates.
    Type: Grant
    Filed: April 16, 2002
    Date of Patent: March 13, 2007
    Assignee: Bayer Cropscience AG
    Inventors: Olaf Gebauer, Jörg Nico Greul, Ulrich Heinemann, Hans-Ludwig Elbe, Bernd-Wieland Krüger, Ralf Dunkel, Arnd Voerste, Ronald Ebbert, Astrid Mauler-Machnik, Ulrike Wachendorff-Neumann, Karl-Heinz Kuck, Yoshinori Kitagawa
  • Patent number: 7186831
    Abstract: This invention relates to novel triazolopyrimidines of the formula in which R1, R2, R3, R4and X have the meanings given in the disclosure, to a plurality of processes for preparing these novel substances, and to their use for controlling unwanted microorganisms. This invention further relates to novel intermediates of the formulae and processes for their preparation and additionally relates to novel amines and carbamates of the formulae given in the disclosure and processes for their preparation.
    Type: Grant
    Filed: April 18, 2002
    Date of Patent: March 6, 2007
    Assignee: Bayer Cropscience LP
    Inventors: Olaf Gebauer, Jörg Nico Greul, Ulrich Heinemann, Hans-Ludwig Elbe, Bernd-Wieland Krüger, Fritz Maurer, Ralf Dunkel, Arnd Voerste, Ronald Ebbert, Ulrike Wachendorff-Neumann, Yoshinori Kitagawa, Astrid Mauler-Machnik, Karl-Heinz Kuck
  • Patent number: 7151105
    Abstract: The present invention provides compounds of formula (4), and their pharmaceutically acceptable salts and solvates, which are useful as inhibitors of the Hepatitis C virus (HCV) polymerase enzyme and are also useful for the treatment of HCV infections in HCV-infected mammals. The present invention also provides pharmaceutical compositions comprising compounds of formula (4), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formula (4).
    Type: Grant
    Filed: August 15, 2005
    Date of Patent: December 19, 2006
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Angelica Linton, John Howard Tatlock
  • Patent number: RE40332
    Abstract: The novel compounds of formula I: wherein (R1, R2, Hal and L1 through L5 are defined in the specification) show selective fungicidal activity. The new compounds may be processed with carriers and adjuvants to produce fungicidal compositions.
    Type: Grant
    Filed: August 20, 2003
    Date of Patent: May 20, 2008
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus-Juergen Pees, Guenter Krummel, Henry Van Tuyl Cotter, Guido Albert, Annerose Rehnig, Leslie May, Waldemar Pfrengle