The Second Ring Of The Bicyclo Ring System Is A Five-membered Hetero Ring Including Three Ring Nitrogens (e.g., Triazolo[1,5-a]pyrimidine, Etc.) Patents (Class 514/259.31)
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Publication number: 20090312332Abstract: Adenosine A2A receptor antagonists are useful for the preparation of medicaments against atrial fibrillation in mammals, including humans. It has been found that the adenosine A2A receptor is present in human atrial cardiomyocytes and participates in the pathological mechanisms underlying atrial fibrillation. An advantage of using A2A antagonists over other agents known in the art is that the A2A antagonists specifically target patients with atrial fibrillation.Type: ApplicationFiled: October 10, 2006Publication date: December 17, 2009Applicant: PROYECTO DE BIOMEDICINA CIMA, S.L.Inventors: Rafael Franco Fernandez, Francisco Ciruela Alfréz, Carmen Lluis Biset, Christa Müller, Joan Cinca Cuscullola, Leif Hove-Madsen
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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: 20090280981Abstract: The novel active compound combinations comprising compounds of the formula (I) where R represents methyl or cyclopropyl, and at least one compound selected from the active compound groups (1) to (24) listed in the description have very good insecticidal and fungicidal properties.Type: ApplicationFiled: May 16, 2007Publication date: November 12, 2009Inventors: Peter Jeschke, Robert Velten, Thomas Schenke, Wolfram Andersch, Heike Hungenberg, Wolfgang Thielert
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Patent number: 7598244Abstract: Novel [1,2,4]triazolo[1,5-a]pyrimidine derivative of the general formula (1): (1) its prodrug or a pharmaceutically acceptable salt thereof, which exhibits an antigen presentation inhibiting activity and is useful as a preventive and/or therapeutic agent for immunological rejection and/or graft versus host reaction in organ/bone marrow transplant, autoimmune disease, allergic disease and/or inflammatory disease and also useful as an anticancer drug or as an immunological tolerance inducer for transplanted organ/transplanted bone marrow.Type: GrantFiled: June 2, 2004Date of Patent: October 6, 2009Assignee: Nippon Kayaku Kabushiki KaishaInventors: Akira Masuda, Yoshitaka Satoh, Yuji Akiyama, Kan Saiga, Eriko Toyoda
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Publication number: 20090246293Abstract: The present invention relates to compounds and the use of such compounds for increasing the efficacy of fungicides for controlling oomycete pathogen induced disease or diseases in one or more plants.Type: ApplicationFiled: April 1, 2009Publication date: October 1, 2009Applicant: Dow AgroSciences LLCInventors: Robert J. Ehr, Norman R. Pearson, Ronald Ross, JR., Christian Schobert
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Publication number: 20090247552Abstract: An object of the present invention is to promote penetration of a compound having a Rho kinase inhibitory activity to a topical moiety, and provide an aqueous liquid preparation capable of maintaining a given drug concentration even when administration frequency is reduced. The present invention solves the aforementioned problem by an aqueous liquid preparation containing a compound represented by the following formula (I) wherein each symbol is as defined in the specification, an isomer thereof and/or a pharmaceutically acceptable acid addition salt thereof, and an ion-pairing reagent or a water-soluble polymer.Type: ApplicationFiled: July 30, 2007Publication date: October 1, 2009Inventors: Shirou Sawa, Hiroyuki Fujii
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Publication number: 20090233907Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE 4 mediated disease state.Type: ApplicationFiled: March 20, 2007Publication date: September 17, 2009Applicant: ASTRAZENECA ABInventors: Rupert Austin, Roger Victor Bonnert, Simon Fraser Hunt, Grigorios Nikitidis, Hitesh Jayantilal Sanganee, Peter Olof Sjo, Dan Warner
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Publication number: 20090215797Abstract: The use of an N,N-dimethyl alkylamide or an N-alkanoyl morpholine provides a stable emulsifiable concentrate composition that hinders de-esterification and transesterification of mixtures of a carboxylic acid herbicide and an ester of a different carboxylic acid herbicide. The N,N-dimethyl alkylamide or N-alkanoyl morpholine additionally stabilizes emulsifiable concentrates containing a triazolopyrimidine herbicide having at least one methoxy group on the triazolopyrimidine ring.Type: ApplicationFiled: February 20, 2009Publication date: August 27, 2009Applicant: Dow AgroSciences LLCInventors: Derek J. Hopkins, Robert M. Buttimor
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Publication number: 20090209557Abstract: Compounds according to Formula I, Formula II, Formula III, Formula V, Formula VI, or to Formula VII, and pharmaceutical compositions of compounds that conform to Formula IV or Formula VIII: where R1 through R33 are prescribed, selectively inhibit P. falciparum dihydroorotate dehydrogenase. Accordingly, a method for preventing and treating malaria attaches to such compounds, as well as to pharmaceutically acceptable salts, solvates, stereoisomers, tautomers, and prodrugs thereof.Type: ApplicationFiled: December 19, 2008Publication date: August 20, 2009Inventors: Margaret PHILLIPS, Pradipsinh K. Rathod, Ramesh Gujjar, Alka Marwaha, Susan A. Charman
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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: 20090156602Abstract: The invention provides a pharmaceutical combination comprising: a) at least one agent selected from Bcr-Abl, Flt-3, FAK and RAF kinase inhibitors; and b) at least one JAK kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination.Type: ApplicationFiled: November 22, 2005Publication date: June 18, 2009Inventors: Nigel Graham Cooke, Paul W. Manley
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Publication number: 20090156398Abstract: 5-Alkyl-6-phenylpyrazolopyrimidin-7-ylamines of the formula (I) in which the substituents are defined as in the description, processes for preparing these compounds, compositions comprising them, and their use for controlling phytopathogenic fungi.Type: ApplicationFiled: July 20, 2006Publication date: June 18, 2009Applicant: BASF AktiengesellschaftInventors: Jochen Dietz, Wassilios Grammenos, Udo Hünger, Jan Klaas Lohmann, Jens Renner, Joachim Rheinheimer
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Publication number: 20090149455Abstract: The triazolopyrimidines of the general formula (I) in which R2, R2, R3, R4, R5, R6, R7 and R8 are as defined in the description are highly suitable for use against rust diseases on leguminous plants.Type: ApplicationFiled: May 26, 2006Publication date: June 11, 2009Applicant: Bayer CropScience AGInventors: Olaf Gebauer, Hans-Ludwig Elbe, Jorg Nico Greul, Oliver Guth, Herbert Gayer, Ulrich Heinemann, Stefan Herrmann, Peter Dahmen, Ulrike Wachendorff-Neumann, Ingo Wetcholowsky, Hiroyuki Hadano
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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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Publication number: 20090123561Abstract: Fungicidal mixtures, comprising as active components 1) 1-methylpyrazol-4-ylcarboxanilides I in which X=oxygen or sulfur, R1=halogen, C1-C4-alkyl or C1-C4-haloalkyl, R2?H or halogen and R3=nitro, cyano, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy or C1-C4-alkylthio and 2) at least one active compound II, selected from the active compound groups A) to F): A) azoles; B) strobilurins; C) carboxamides; D) heterocyclic compounds; E) carbamates; F) other fungicides; in a synergistically effective amount, methods for controlling harmful fungi using mixtures of at least one compound I and at least one active compound II and the use of the compound(s) I with active compounds II for preparing such mixtures, and also compositions and seed comprising such mixtures.Type: ApplicationFiled: July 13, 2006Publication date: May 14, 2009Applicant: BASF AKTIENGESELLLSCHAFTInventors: Markus Gewehr, Reinhard Stierl, Jochen Dietz, Bernd Muller, Maria Scherer, Siegfriend Strathmann, Frank Werner, Michael Vonend
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Publication number: 20090124599Abstract: Fungicidal mixtures comprising, as active components 1) the strobilurin derivative of the formula I, and 2) at least one active compound II selected from the group of heterocyclic compounds in a synergistically effective amount, methods for controlling harmful fungi using mixtures of the compound I with active compounds II, the use of the compound I with active compounds II for preparing such mixtures and compositions comprising these mixtures.Type: ApplicationFiled: December 21, 2005Publication date: May 14, 2009Applicant: Basf AktiengesellschaftInventors: Markus Gewehr, Reinherd Stierl, Matthis Niedenbrück, Udo Hünger
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Publication number: 20090118277Abstract: The invention relates to 3-unsubstituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidine compounds, their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase, especially tie-2 kinase, activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.Type: ApplicationFiled: April 2, 2007Publication date: May 7, 2009Inventors: Keiichi Masuya, Andrea Vaupel, Patricia Imbach, Pascal Furet
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Publication number: 20090105210Abstract: The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: January 18, 2006Publication date: April 23, 2009Inventors: Wallace T. Ashton, Charles G. Caldwell, Hong Dong, Ying-Duo Gao, Giovanna Scapin, Ann E. Weber
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Patent number: 7511049Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: July 17, 2007Date of Patent: March 31, 2009Assignees: Schering Corporation, Pharmacopeia, Inc.Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Lawrence W. Dillard, Vinh D. Tran, Zhenmin He, Ray Anthony James, Haengsoon Park
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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: 20080312078Abstract: The invention relates to a 6-phenyl-pyrazolopyrimidine-7-ylamine of formula (I), wherein substituents are defined according to the description. Methods for producing said compounds, agents containing said compounds and the use thereof for controlling phytopathogenic parasitic fungi are also disclosed.Type: ApplicationFiled: July 20, 2006Publication date: December 18, 2008Applicant: Basf AktiengesellschaftInventors: Jochen Dietz, Wassilios Grammenos, Udo Hunger, Jan Klaas Lohmann, Jens Renner, Joachim Rheinheimer
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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: 20080255158Abstract: The invention relates to fungicidal mixtures containing in the form of active agents: a triazolopyrimidine derivative of formula (I) and thiophanate-methyl of formula (II) in synergistically active quantity and to a method for controlling harmful fungi by means of the mixture of the compounds I and II, thereby making it possible to produce said mixtures and the products containing them.Type: ApplicationFiled: March 14, 2005Publication date: October 16, 2008Applicant: BASF AktiengesellschaftInventors: Jordi Tormo I Blasco, Thomas Grote, Maria Scherer, Reinhard Stierl, Siegfried Strathmann, Ulrich Schofl
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Patent number: 7435750Abstract: The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: March 8, 2005Date of Patent: October 14, 2008Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Han-Zhong Zhang, John A. Drewe, P. Sanjeeva Reddy, Shailaja Kasibhatla, Jared Daniel Kuemmerle, Kristin P. Ollis
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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: 20080234295Abstract: Fungicidal mixtures comprising, as active components, 1) azolopyrimidinylamines of the formula I, in which the substituents are as defined in the description and 2) at least one active compound II selected from the following groups: azoles, strobilurins, carboxamides, heterocylic compounds, carbamates and other active compounds selected from the group consisting of guanidines, antibiotics, sulfur-containing heterocyclyl compounds, organophosphorus compounds, organochlorine compounds, inorganic active compounds, growth retardants and cyflufenamid, cymoxanil, dimethirimol, ethirimol, furalaxyl, metrafenone and spiroxamine; in a synergistically effective amount. Methods for controlling harmful fungi using mixtures of the compound I with active compounds II and the use of the compound I with active compounds II for preparing such mixtures, and also compositions comprising these mixtures.Type: ApplicationFiled: July 20, 2006Publication date: September 25, 2008Applicant: BASF AktiengelsellschaftInventors: Christine Beck, Matthias Niedenbruck, Maria Scherer, Reinhard Stierl, Siegfried Strathmann, Udo Hunger
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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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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: 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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Patent number: 7407962Abstract: The present invention provides compounds that are inhibitors of protein kinase, particularly inhibitors of ERK2, GSK3, PKA, CDK2 protein kinases, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.Type: GrantFiled: February 3, 2004Date of Patent: August 5, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, Michael R. Hale, Francois Maltais, Qing Tang
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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: 20080171657Abstract: 5,6-Dialkyl-7-aminoazolopyrimidines of the formula I in which the substituents are as defined below: R1 is alkyl, alkoxymethylene or alkoxyethylene, where the aliphatic groups may be substituted as defined in the description; R2 is n-propyl or n-butyl; 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: July 17, 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: 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: 20080153700Abstract: Fungicidal mixtures comprising, as active components, 1 ) the triazolopyrimidine derivative of the formula I 2) tolylfluanid of the formula II, in a synergistically effective amount, methods for controlling harmful fungi using mixtures of the compound I with the compound II and the use of the compound I with the compound II for preparing such mixtures, and also compositions comprising these mixtures.Type: ApplicationFiled: March 14, 2005Publication date: June 26, 2008Applicant: Basf AktiengesellschaftInventors: Jordi Tormo I Blasco, Thomas Grote, Maria Scherer, Reinhard Stierl, Siegfried Strathmann, Ulrich Schofl
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Publication number: 20080139386Abstract: Fungicidal mixtures for controlling harmful fungi, which mixtures comprise, as active components, 1) the triazolopyrimidine derivative of the formula I and 2) pencycuron of the formula II in a synergistically effective amount, methods for controlling rice pathogens using mixtures of the compound I with the compounds II and the use of the compound I with the compounds II for preparing such mixtures, and also compositions comprising these mixtures.Type: ApplicationFiled: January 13, 2005Publication date: June 12, 2008Applicant: BASF AktiengesellschaftInventors: Jordi Tormo i Blasco, Thomas Grote, Maria Scherer, Reinhard Stierl, Siegfried Strathmann, Ulrich Schofl
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Publication number: 20080139580Abstract: 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: ApplicationFiled: September 14, 2007Publication date: June 12, 2008Applicant: Neurogen CorporationInventors: Linghong Xie, Bingsong Han, Yuelian Xu, George Maynard, Bertrand L. Chenard, Kenneth Shaw, Yang Gao
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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: 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