Ring Nitrogen Is Shared By Two Cyclos Patents (Class 544/263)
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Publication number: 20090312312Abstract: 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: ApplicationFiled: February 12, 2009Publication date: December 17, 2009Applicant: 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
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Publication number: 20090281122Abstract: 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: ApplicationFiled: July 15, 2009Publication date: November 12, 2009Inventors: Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Angelica Linton, John Howard Tatlock
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Publication number: 20090253716Abstract: 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: ApplicationFiled: June 18, 2009Publication date: October 8, 2009Inventors: Michael Sotirios Malamas, James Joseph Erdei, Iwan Suwandi Gunawan, Pawel Wojciech Nowak, Boyd Lynn Harrison
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Publication number: 20090197883Abstract: 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: ApplicationFiled: March 3, 2006Publication date: August 6, 2009Inventors: Helen M. Armstrong, Linda L. Chang, Richard Frenette, Dwight MacDonald, Hyun O. Ok, Michel Therien, Feroze Ujjainwalla
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Patent number: 7550471Abstract: 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: GrantFiled: November 4, 2003Date of Patent: June 23, 2009Assignee: BASF AktiengesellschaftInventors: 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
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Publication number: 20090156594Abstract: The present disclosure provides heterocyclic protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.Type: ApplicationFiled: May 21, 2008Publication date: June 18, 2009Applicant: SGX Pharmaceuticals, Inc.Inventors: Pierre-Yves Bounaud, Christopher Ronald Smith, Elizabeth A. Jefferson, Jorg Hendle, Patrick S. Lee, Angelina Marie Thayer, Gavin Charles Hirst
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Publication number: 20090137607Abstract: 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: ApplicationFiled: August 14, 2008Publication date: May 28, 2009Inventors: Swen Holder, Matthias Vennemann, Gerrit Beneke, Armin Zulch, Volker Gekeler, Thomas Beckers, Astrid Zimmermann, Hemant Joshi
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Publication number: 20090137547Abstract: 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: ApplicationFiled: December 7, 2007Publication date: May 28, 2009Inventors: 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
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Patent number: 7514441Abstract: 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: GrantFiled: August 21, 2003Date of Patent: April 7, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuneo Yasuma, Akira Mori, Masahiro Kawase, Hiroyuki Kimura, Masato Yoshida, Albert Charles Gyorkos, Scott Alan Pratt, Christopher Peter Corrette
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Patent number: 7507739Abstract: 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: GrantFiled: September 24, 2004Date of Patent: March 24, 2009Assignee: WyethInventors: Nan Zhang, Semiramis Ayral-Kaloustian, Thai Nguyen, Yanzhong Wu, Wei Tong
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Patent number: 7501383Abstract: 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: GrantFiled: March 8, 2005Date of Patent: March 10, 2009Assignee: BASF AktiengesellschaftInventors: 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
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Publication number: 20090062286Abstract: 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: ApplicationFiled: May 5, 2008Publication date: March 5, 2009Inventors: Kenneth William Foreman, Frances E. Park, Lee Arnold
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Publication number: 20090054451Abstract: 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: ApplicationFiled: August 4, 2008Publication date: February 26, 2009Applicant: Euroscreen S.A.Inventors: Jacques Huck, Frederic Ooms, Christian Tyrchan, Hamid R. Hoveyda
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Publication number: 20090023921Abstract: The present invention relates to methods and compounds useful in the preparation of compounds of the formula (I).Type: ApplicationFiled: August 16, 2006Publication date: January 22, 2009Inventors: Christopher Frederick Matthews, Robert William Scott, John Lloyd Tucker
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Publication number: 20080300135Abstract: 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: ApplicationFiled: July 6, 2006Publication date: December 4, 2008Applicant: BASF AktiengesellschaftInventors: Oliver Wagner, Sarah Ulmschneider, Udo Hunger
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Publication number: 20080293713Abstract: 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: ApplicationFiled: April 30, 2008Publication date: November 27, 2008Applicant: Abbott LaboratoriesInventors: Gang Liu, Zhili Xin, Philip R. Kym, Andrew J. Souers
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Publication number: 20080280759Abstract: 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 haloaType: ApplicationFiled: December 14, 2004Publication date: November 13, 2008Inventors: 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
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Publication number: 20080275065Abstract: 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: ApplicationFiled: October 10, 2005Publication date: November 6, 2008Applicants: SYNGENTA CROP PROTECTION, INC., SYNGENTA LIMITEDInventors: Anthony Cornelius O'Sullivan, David John Hughes, Andre Jeanguenat, Michel Muehlebach, Olivier Loiseleur
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Publication number: 20080262000Abstract: 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: ApplicationFiled: February 14, 2006Publication date: October 23, 2008Applicant: BASF AktiengesellschaftInventors: 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
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Publication number: 20080255156Abstract: 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: ApplicationFiled: June 25, 2007Publication date: October 16, 2008Inventors: Martin C. Clasby, Samuel Chackalamannil, Andrew Stamford
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Publication number: 20080248952Abstract: 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 isType: ApplicationFiled: July 6, 2005Publication date: October 9, 2008Applicant: BASF AktiengesellschaftInventors: 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
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Publication number: 20080249113Abstract: 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 IType: ApplicationFiled: July 28, 2005Publication date: October 9, 2008Inventors: 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
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Publication number: 20080242860Abstract: 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: ApplicationFiled: June 3, 2008Publication date: October 2, 2008Applicant: FUJIFILM CORPORATIONInventors: Atsushi Matsunaga, Tadashi Inaba, Shinichi Ichikawa
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Publication number: 20080227795Abstract: 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: ApplicationFiled: January 15, 2005Publication date: September 18, 2008Applicant: BASF AktiengesellschaftInventors: 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
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Publication number: 20080227796Abstract: 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: ApplicationFiled: December 16, 2005Publication date: September 18, 2008Applicant: BASF AktiengesellschaftInventors: Oliver Wagner, Thomas Grote, Joachim Rheinheimer, Barbara Nave, Reinhard Stierl
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Publication number: 20080214395Abstract: 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: ApplicationFiled: July 20, 2006Publication date: September 4, 2008Applicant: BASF AktiengesellschaftInventors: Jochen Dietz, Thomas Grote, Udo Hunger, Jan Klaas Lohmann, Bernd Muller, Jens Renner, Sarah Ulmschneider, Wassilios Grammenos, Joachim Rheinheimer
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Patent number: 7419982Abstract: 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: GrantFiled: May 19, 2006Date of Patent: September 2, 2008Assignee: Wyeth Holdings CorporationInventors: Fang Fang Qi, Mannching Sherry Ku, Yanzhong Wu, David M. Blum
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Publication number: 20080207455Abstract: 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: ApplicationFiled: March 1, 2006Publication date: August 28, 2008Applicant: BASF AKTINGESELLSCHAFTInventors: 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
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Patent number: 7417041Abstract: 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: GrantFiled: February 20, 2004Date of Patent: August 26, 2008Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Laura C. Blumberg, Michael J. Munchhof, Andrei Shavnya
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Publication number: 20080200480Abstract: 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: ApplicationFiled: July 20, 2006Publication date: August 21, 2008Applicant: BASF AktiengesellschaftInventors: Jochen Dietz, Thomas Grote, Udo Hunger, Jan Klaas Lohmann, Bernd Muller, Jens Renner, Sarah Ulmschneider, Wassilios Grammenos, Joachim Rheinheimer
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Publication number: 20080200675Abstract: 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: ApplicationFiled: June 23, 2006Publication date: August 21, 2008Applicant: BASF AktiengesellschaftInventors: Norbert Gotz, Volker Maywald, Michael Keil
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Publication number: 20080188494Abstract: 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 orType: ApplicationFiled: April 24, 2006Publication date: August 7, 2008Applicant: BASF AktiengesellschaftInventors: Jochen Dietz, Wassilios Grammenos, Thomas Grote, Udo Hunger, Jan Klaas Lohmann, Bernd Muller, Joachim Rheinheimer, Peter Schafer, Frank Schieweck, Anja Schwogler
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Publication number: 20080176870Abstract: 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: ApplicationFiled: November 20, 2007Publication date: July 24, 2008Inventors: Bert Nolte, Irving Sucholeiki, Tim Feuerstein, Brian M. Gallagher, Xinyuan Wu, Christoph Steeneck, Christian Gege, Hongbo Deng, Joshua Van Veldhuizen, Arthur Taveras
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Publication number: 20080167324Abstract: 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: ApplicationFiled: February 28, 2006Publication date: July 10, 2008Inventors: Yuelian Xu, Linghong Xie
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Patent number: 7396835Abstract: 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: GrantFiled: December 8, 2004Date of Patent: July 8, 2008Assignee: WyethInventors: Yanzhong Wu, Jean Schmid, Jay Thomas Afragola, David Blum, Semiramis Ayral-Kaloustian
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Publication number: 20080139581Abstract: 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: ApplicationFiled: March 2, 2006Publication date: June 12, 2008Applicant: BASF AktiengesellschaftInventors: Wassilios Grammenos, Thomas Grote, Udo Hunger, Jan Klaas Lohmann, Bern Muller, Joachim Rheinheimer, Peter Schafer, Anja Schwogler, Michael Rack
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Publication number: 20080132412Abstract: 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: ApplicationFiled: December 15, 2005Publication date: June 5, 2008Applicant: BASF AktiengesellschaftInventors: Oliver Wagner, Udo Hunger
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Publication number: 20080125445Abstract: 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: ApplicationFiled: March 1, 2006Publication date: May 29, 2008Applicant: BASF AktiengesellschaftInventors: 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
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Publication number: 20080119493Abstract: 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: ApplicationFiled: March 8, 2005Publication date: May 22, 2008Applicant: BASF AktiengesellschaftInventors: 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
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Patent number: 7351826Abstract: 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: GrantFiled: February 16, 2004Date of Patent: April 1, 2008Assignee: Neurogen CorporationInventors: Linghong Xie, Bingsong Han, Yuelian Xu
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Patent number: 7339058Abstract: 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: GrantFiled: March 24, 2005Date of Patent: March 4, 2008Assignee: Dow AgroSciences LLCInventor: Christopher Thomas Hamilton
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Patent number: 7329663Abstract: 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: GrantFiled: June 29, 2001Date of Patent: February 12, 2008Assignee: WyethInventors: Mark R. Schmitt, Donald R. Kirsch, Jane E. Harris, Carl F. Beyer, Klaus-Jüergen Pees, Paul A. Carter, Waldemar Pfrengle, Guido Albert
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Patent number: 7300908Abstract: 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 sType: GrantFiled: July 3, 2002Date of Patent: November 27, 2007Assignee: BASF AktiengesellschaftInventors: 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
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Publication number: 20070259860Abstract: 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: ApplicationFiled: April 25, 2007Publication date: November 8, 2007Applicants: 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
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Patent number: 7271170Abstract: 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: GrantFiled: July 23, 2004Date of Patent: September 18, 2007Assignee: Neurogen CorporationInventors: Linghong Xie, Bingsong Han, Yuelian Xu, George Maynard, Bertrand L. Chenard, Kenneth Shaw, Yang Gao
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Patent number: 7205316Abstract: 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: GrantFiled: May 6, 2005Date of Patent: April 17, 2007Assignee: Abbott LaboratoriesInventors: Robert J. Altenbach, Lawrence A. Black, Marlon D. Cowart, Huaqing Liu
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Patent number: 7189680Abstract: 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: GrantFiled: April 16, 2002Date of Patent: March 13, 2007Assignee: Bayer Cropscience AGInventors: 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
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Patent number: 7186831Abstract: 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: GrantFiled: April 18, 2002Date of Patent: March 6, 2007Assignee: Bayer Cropscience LPInventors: 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
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Patent number: 7151105Abstract: 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: GrantFiled: August 15, 2005Date of Patent: December 19, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Angelica Linton, John Howard Tatlock
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Patent number: RE40332Abstract: 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: GrantFiled: August 20, 2003Date of Patent: May 20, 2008Assignee: BASF AktiengesellschaftInventors: Klaus-Juergen Pees, Guenter Krummel, Henry Van Tuyl Cotter, Guido Albert, Annerose Rehnig, Leslie May, Waldemar Pfrengle