At Least Five Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/254)
-
Patent number: 7750556Abstract: The present invention relates to the use of triazole derivatives selected from the group consisting of triazolopyrimidine derivatives and triazolouracil derivatives in organic light-emitting diodes (OLEDs), an OLED comprising at least one of the organic triazole derivatives mentioned, a light-emitting layer comprising at least one of the triazole derivatives mentioned, an OLED comprising the light-emitting layer of the invention, a device comprising an OLED according to the invention and also specific novel triazole derivatives.Type: GrantFiled: March 14, 2005Date of Patent: July 6, 2010Assignee: BASF AktiengesellschaftInventors: Thomas Gessner, Christian Lennartz, Hans-Werner Schmidt, Mukundan Thelakkat, Markus Baete
-
Publication number: 20100160349Abstract: This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; C1-6alkyl substituted with formyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl or C1-6alkylcarbonyloxy; X represents a direct bond; —(CH2)n3— or —(CH2)n4—X1a—X1b—; R2 represents an optionally substituted cyclic system; provided that N,3-diphenyl-3H-1,2,3-triazolo[4,5-d]pyrimidin-5-amine is not included; their use, pharmaceutical compositions comprising them and processes for their preparation.Type: ApplicationFiled: January 13, 2006Publication date: June 24, 2010Inventors: Christopher John Love, Ludwig Paul Cooymans, Nele Vandermaesen
-
Publication number: 20100137340Abstract: The invention relates to compounds of Formula (I) wherein the substituents are as defined in claim 1; to compositions comprising said compounds and to their use as pharmaceutical agents.Type: ApplicationFiled: March 3, 2008Publication date: June 3, 2010Inventors: Ralf Glatthar, Samuel Hintermann, Ivan-Toma Vranesic
-
Publication number: 20100130515Abstract: Polymorphic and solvated forms of solid 3-(4-amino-3-methylbenzyl)-7-(furan-2-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine, and methods of making them, are described.Type: ApplicationFiled: July 13, 2009Publication date: May 27, 2010Applicants: BIOGEN IDEC INC., VERNALIS RESEARCH LIMITEDInventors: Slawomir Janicki, Hexi Chang, Weirong Chen, William F. Kiesman, Benjamin Lane, Richard Todd
-
Publication number: 20100069408Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.Type: ApplicationFiled: November 18, 2009Publication date: March 18, 2010Applicant: AstraZeneca ABInventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
-
Publication number: 20100004444Abstract: The present invention relates to a pyrimidine compound (I) useful as a pharmaceutical intermediate, to a process for preparing said pyrimidine compound, to intermediates used in said process, and to the use of said pyrimidine compound in the preparation of pharmaceuticals.Type: ApplicationFiled: September 10, 2009Publication date: January 7, 2010Applicant: AstraZeneca ABInventors: Ulf Larsson, Mattias Magnusson, Tibor Musil, Andreas Palmgren
-
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
-
Patent number: 7622482Abstract: This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.Type: GrantFiled: February 15, 2006Date of Patent: November 24, 2009Assignee: AstraZenecaInventors: Yongxin Han, Michelle Lamb, Peter Mohr, Bin Wang, Tao Wang, Dingwei Yu
-
Publication number: 20090247517Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).Type: ApplicationFiled: October 26, 2005Publication date: October 1, 2009Inventors: Hong Liu, Xiaohui He, Ha-Soon Choi, Kunyong Yang, David H. Woodmansee, Zhicheng Wang, David Archer Ellis, Baogen Wu, Yun He, Truc Ngoc Nguyen
-
Publication number: 20090247556Abstract: The invention provides compounds of formula (Ia), (Ic), (Ig) and (Ik), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).Type: ApplicationFiled: March 30, 2007Publication date: October 1, 2009Applicant: IRM LLCInventors: Xiaohui He, Kunyong Yang, Hong Liu, David Archer Ellis
-
Patent number: 7589097Abstract: The use of a compound of formula (I): wherein R1 is selected from H, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, halogen, CN, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from aryl attached via an unsaturated carbon; R3 is selected from H, alkyl, COR5, CO2R7, CONR5R6, CONR4NR5R6 and SO2R7; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an NR5R6 group, R5 and R6 may be linked to form a heterocyclic group, or where R4, R5 and R6 are in a (CONR4NR5R6) group, R4 and R5 may be linked to form a heterocyclic group; and R7 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or said disorder is depression, cognitive or memory impairment,Type: GrantFiled: December 20, 2007Date of Patent: September 15, 2009Assignee: Vernalis Research LimitedInventors: Roger John Gillespie, Joanne Lerpiniere, Suneel Gaur, Samantha Jayne Bamford, Gemma Caroline Stratton, Stefania Leonardi, Scott Murray Weiss
-
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
-
Publication number: 20090192176Abstract: The invention relates to 1H-pyrazolo[3,4-d]pyrimidine, purine, 7H-purin-8(9H)-one, 3H-[1,2,3]triazolo[4,5-d]pyrimidine, and thieno[3,2-d]pyrimidine compounds, compositions comprising the compounds, and methods for making and using the compounds.Type: ApplicationFiled: January 29, 2009Publication date: July 30, 2009Applicant: WyethInventors: Arie Zask, Christoph Martin Dehnhardt, Joshua Aaron Kaplan, Efren Guillermo Delos Santos, Aranapakam Mudumbai Venkatesan, Jeroen Cunera Verheijen
-
Patent number: 7566722Abstract: The present invention is directed to novel bicyclic triazolopyrimidine compounds of Formula (I) or a form thereof: wherein R1 and R2 are as defined herein, and their methods of preparation and use as ADP inhibitors.Type: GrantFiled: October 31, 2007Date of Patent: July 28, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, Hong Ye, Cailin Chen
-
Patent number: 7563781Abstract: The invention relates to the discovery of triazolopyrimidine derivatives of formula (I), which have been found to exhibit inhibitory activity against the serine-tyrosine and tyrosine kinases.Type: GrantFiled: January 11, 2006Date of Patent: July 21, 2009Assignee: Janssen Pharmaceutica NVInventors: Donald W. Ludovici, Richard W. Connors, Steven J. Coats, Li Liu, Bart L. De Corte, Dana L. Johnson, Mark J. Schulz
-
Publication number: 20090181986Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: January 8, 2009Publication date: July 16, 2009Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
-
Publication number: 20090182140Abstract: An alicyclic heterocyclic compound represented by the following formula or a pharmaceutically acceptable salt thereof: wherein ring A is a heterocyclic ring, ring B is a carbocyclic ring, a heterocyclic ring etc., P1 and P2 are CH or N, q and r are 0 to 2, X is —NH—, —O—, —CH2—, etc., Y is —CH2—, —CO—, —SO2—, etc., Z is —CO—, —SO2—, etc., and R3 is carbocyclic group, heterocyclic group, hydroxyl, alkoxy or amino, is useful as a controlling agent of the function of CCR4 useful for the prevention or treatment for bronchial asthma, atopic dermatitis, etc.Type: ApplicationFiled: November 30, 2006Publication date: July 16, 2009Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Shigeru Furukubo, Hiroshi Miyazaki
-
Patent number: 7560458Abstract: This invention concerns compounds of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines and stereochemically isomeric forms thereof, their use, pharmaceutical compositions comprising them, and processes for their preparation.Type: GrantFiled: July 12, 2004Date of Patent: July 14, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Eddy Jean Edgard Freyne, Christopher John Love, Ludwig Paul Cooymans, Nele Vandermaesen, Peter Jacobus Johannes Antonius Buijnsters, Marc Willems, Werner Constant Johan Embrechts
-
Publication number: 20090118502Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: November 21, 2008Publication date: May 7, 2009Applicant: Rib-X Pharmaceuticals, Inc.Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Josseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
-
Publication number: 20090088397Abstract: A pharmaceutical composition comprising an effective amount of a compound of formulas (I-III) and a pharmaceutically acceptable carrier. Methods for treating a hepatitis virus in a patient comprising administering an effective amount of the compound of formulas (I-III) are also presented.Type: ApplicationFiled: May 4, 2007Publication date: April 2, 2009Inventors: Andrea Cuconati, Timothy M. Block, Xiaodong Xu
-
Publication number: 20090018055Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n2, n3, n4, A, B, D, E, G, J, Y, R1 and R2 are defined herein.Type: ApplicationFiled: April 30, 2008Publication date: January 15, 2009Inventors: John M. Fevig, Dean A. Wacker
-
Publication number: 20090012103Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: July 3, 2008Publication date: January 8, 2009Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
-
Publication number: 20080312257Abstract: The present invention is directed to novel bicyclic triazolopyrimidine compounds of Formula (I) or a form thereof: wherein X1, X2, R1, R2, R3 and R4 are as defined herein, and their methods of preparation and use as ADP inhibitors.Type: ApplicationFiled: October 31, 2007Publication date: December 18, 2008Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, Hong Ye, Cailin Chen
-
Patent number: 7449465Abstract: This invention concerns compounds of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines and stereochemically isomeric forms thereof, their use, pharmaceutical compositions comprising them, and processes for their preparation.Type: GrantFiled: July 12, 2004Date of Patent: November 11, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Eddy Jean Edgard Freyne, Christopher John Love, Ludwig Paul Cooymans, Nele Vandermaesen, Peter Jacobus Johannes Antonius Buijnsters, Marc Willems, Werner Constant Johan Embrechts
-
Publication number: 20080234277Abstract: The invention is concerned with novel aza-pyridopyrimidinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, X1, X2, X3, Y, Z, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used in treating or preventing diseases which are modulated by HM74A agonists.Type: ApplicationFiled: March 17, 2008Publication date: September 25, 2008Inventors: Aurelia Conte, Henrietta Dehmlow, Uwe Grether, Nicole A. Kratochwil, Holger Kuehne, Robert Narquizian, Constantinos G. Panousis, Jens-Uwe Peters, Fabienne Ricklin
-
Publication number: 20080234481Abstract: The present invention relates to a pyrimidine compound (I) useful as a pharmaceutical intermediate, to a process for preparing said pyrimidine compound, to intermediates used in said process, and to the use of said pyrimidine compound in the preparation of pharmaceuticals.Type: ApplicationFiled: April 28, 2008Publication date: September 25, 2008Applicant: AstraZeneca ABInventors: Ulf Larsson, Mattias Magnusson, Tibor Musil, Andreas Palmgren
-
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
-
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
-
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
-
Patent number: 7345047Abstract: The invention provides novel substituted cyclopentane compounds (in particular, substituted [1,2,3]triazolo[4,5-d]pyrimidines), their use as medicaments (in particular, their use as anti-thrombotic agents), compositions containing them and processes for their preparation.Type: GrantFiled: December 10, 2004Date of Patent: March 18, 2008Assignee: AstraZeneca ABInventors: Simon Guile, Barrie Martin
-
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
-
Patent number: 7265124Abstract: The invention provides new forms of a chemical compound of formula (I). The invention relates to forms of a chemical compound (I), in particular to crystalline and amorphous forms, more particularly four crystalline forms and an amorphous form. The invention further relates to processes for the preparation of such forms, to pharmaceutical compositions comprising the compound in crystalline and/or amorphous form and to therapeutic use of such forms.Type: GrantFiled: October 3, 2005Date of Patent: September 4, 2007Assignee: AstraZeneca ABInventors: Martin Bohlin, Steve Cosgrove, Bo Lassen
-
Publication number: 20070191606Abstract: The present invention provides novel 2,2-bis(4-hydroxyphenyl)-alkyl onium salts as illustrated by 2,2-bis(4-hydroxyphenyl)-tridecyl(1,2-dimethylimidazolium)bromide and a process for preparation thereof by hydroxyalkylating acetoacetate to the corresponding hyroxyalkylacetoacetate, dealkoxycarbonylating the hydroxyalkyl acetoacetate to ?-hydroxyalkan-2-one and contacting the ?-hydroxyalkan-2-one with phenol in the presence of an acidic catalyst to give 2,2-bis(4-hydroxyphenyl)alkanol, brominating the 2,2-bis(4-hydroxyphenyl)alkanol to 2,2-bis(4-hydroxyphenyl)alkyl bromide, quaternizing 1,2-dimethylimidazole with the 2,2-bis(4-hydroxyphenyl)alkyl bromide to 2,2-bis(4-hydroxyphenyl)alkyl(1,2-dimethylimidazolium)bromide. The products can be used as reactive modifiers for layered phyllosilicates that can be used in the preparation of polymer-nanocomposites, wherein the said polymers are prepared from 2,2-bis(4-hydroxyphenyl)propane as one of the reacting monomers.Type: ApplicationFiled: October 13, 2006Publication date: August 16, 2007Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Shroff Rama Mallikarjuna, Swaminathan Sivaram
-
Patent number: 7250419Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.Type: GrantFiled: September 21, 2005Date of Patent: July 31, 2007Assignee: AstraZeneca ABInventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
-
Patent number: 7211668Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is sulfur or oxygen; J is nitrogen or C—R?; R1, R? is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy or a functional group having one of following general formulae: wherein A1, A2, A3, A4, A5, is independently selected from H, halogen such as F, Cl, Br or I, CF3, alkyl, preferably C1–C4 alkyl, nitro, nitrile, alkoxy, preferably C1–C4 alkoxy, halogenated (such as F, Cl, Br and I) alkyl, preferably halogenated C1–C4 alkyl, halogenated (such as F, Cl, Br and I) alkoxy, preferably halogenated C1–C4 alkoxy, phenyl, and halogenated (such as F, Cl, Br and I phenyl; R2 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucType: GrantFiled: April 6, 2004Date of Patent: May 1, 2007Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Sung Hee Lee
-
Patent number: 7141575Abstract: The use of a compound of formula (I): wherein R1 is selected from H, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, halogen, CN, NR5R6, NR4CONR5, NR4CONR5R6,NR4CO2R7 and NR4SO2R7; R2 is selected from aryl attached via an unsaturated carbon; R3 is selected from H, alkyl, COR5, CO2R7, CONR5R6, CONR4NR5R6 and SO2R7; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an NR5R6 group, R5 and R6 may be linked to form a heterocyclic group, or where R4, R5 and R6 are in a (CONR4NR5R6) group, R4 and R5 may be linked to form a heterocyclic group; and R7 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or said disorder is depression, cognitive or memory impairment, acuteType: GrantFiled: January 10, 2002Date of Patent: November 28, 2006Assignee: Vernalis Research Ltd.Inventors: Roger John Gillespie, Joanne Lerpiniere, Suneel Gaur, Samantha Jayne Bamford, Gemma Caroline Stratton, Stefania Leonardi, Scott Murray Weiss
-
Patent number: 7129244Abstract: A compound represented by Formula I, or a polymorph, ester, tautomer, enantiomer, diastereomer, pharmaceutically acceptable salt or prodrug thereof, Wherein R1 is halogen, —OR11, —SR11 or lower alkyl; R2 is —NHR8; R4 is —CHR12—, —C(O)—, —C(S)—, —S(O)— or —S2—; and R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 4 to 5 substituents, the heteroaryl group is substituted with 3 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, and the heterocyclic group is substituted with 3 to 5 substituents.Type: GrantFiled: September 20, 2004Date of Patent: October 31, 2006Assignee: Conforma Therapeutics CorporationInventors: Srinivas Rao Kasibhatla, Kevin D. Hong, Marcus F. Boehm
-
Patent number: 7115739Abstract: This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.Type: GrantFiled: September 14, 2001Date of Patent: October 3, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Ronald Knegtel, Hayley Binch, Julian M. C. Golec, Pan Li, Jean-Damien Charier
-
Patent number: 7074929Abstract: This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y.Type: GrantFiled: November 10, 2003Date of Patent: July 11, 2006Assignees: Neurogen Corp., Pfizer, Inc.Inventors: Raymond F. Horvath, Jennifer Tran, Stéphane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
-
Patent number: 7071192Abstract: The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4-represents a radical of formula —CH?CH—CH?CH—; —N—CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N—; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y1 is a bivalent radical of formula —NR2— or —CH(NR2R4)—; X1 is NR4, S, S(?O), S(?O)2, O, CH2, C(?O), CH(?CH2), CH(OH), CH(CH3), CH(OCH3), CH(SCH3), CH(NR5aR5b), CH2—NR4 or NR4—CH2; X2 is a direct bond, CH2, C(?O), NR4, C1-4alkyl-NR4, NR4—C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R3: provided that when R3 is hydroxy or C1-6alkyloxy, then R3 cannot replace a hydrogen atom in the a position relative to a nitrogen atom; G is a diType: GrantFiled: June 20, 2000Date of Patent: July 4, 2006Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Jean Fernand Armand Lacrampe, Jérôme Emile Georges Guillemont, Marc Gaston Venet, Koenraad Jozef Lodewijk Marcel Andries
-
Patent number: 7067663Abstract: Pyrimidine compound (I) useful as a pharmaceutical intermediate, a process for preparing the pyrimidine compound (I), to intermediates used in the process, and use of the pyrimidine compound (I) in the preparation of pharmaceuticals. The process comprises hydrogenating a compound of formula (IV): wherein Ar is a phenyl optionally substituted by halogen, C1-4 alkyl or C1-4 alkoxy; to give a compound of formula (II): and reacting the compound of formula (II) with a salt of a compound of formula (III): to provide the compound of formula (I).Type: GrantFiled: May 31, 2001Date of Patent: June 27, 2006Assignee: AstraZeneca ABInventors: Ulf Larsson, Mattias Magnusson, Tibor Musil, Andreas Palmgren
-
Patent number: 7034032Abstract: The invention provides novel 1,2,3-triazolo[4,5-d]pyrimidine compounds, such as those represented by formula (I): their use as medicaments, particularly in platelet aggregation disorders, compositions containing them and processes for their preparation.Type: GrantFiled: November 7, 2001Date of Patent: April 25, 2006Assignee: AstraZeneca ABInventors: Roger Brown, Simon Guile, Garry Pairaudeau, Brian Springthorpe
-
Patent number: 6974868Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.Type: GrantFiled: December 20, 2002Date of Patent: December 13, 2005Assignee: AstraZeneca ABInventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
-
Patent number: 6858616Abstract: The present application describes nitrogen containing heterobicyclics and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.Type: GrantFiled: April 26, 2002Date of Patent: February 22, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: John M. Fevig, Joseph Cacciola, Charles G. Clark, Qi Han, Patrick Yuk Sun Lam, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan, Karen A. Rossi
-
Patent number: 6844348Abstract: The invention provides a compound of formula (I): wherein R1 is alkyl C1-6 or alkenyl C2-6, both independently optionally substituted by one or more groups selected from alkyl C1-5 or halogen; R2 is cycloalkyl C3-8, optionally substituted by R3; R3 is phenyl, optionally substituted by one or more groups selected from alkyl C1-6 or halogen; R4 and R5 are alkyl C1-6 or together cycloalkyl C3-6. These compounds are useful for the treatment of stable and unstable angina.Type: GrantFiled: November 7, 2001Date of Patent: January 18, 2005Assignee: AstraZeneca ABInventors: Simon Guile, Barrie Martin
-
Publication number: 20040229870Abstract: The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor.Type: ApplicationFiled: November 10, 2003Publication date: November 18, 2004Applicants: NEUROGEN CORPORATION, PFIZER INC.Inventors: Raymond F. Horvath, Jennifer N. Tran, Stephane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
-
Publication number: 20040220186Abstract: The invention provides compounds of Formula (I) 1Type: ApplicationFiled: April 20, 2004Publication date: November 4, 2004Applicant: Pfizer Inc.Inventors: Andrew Simon Bell, Michael Paul DeNinno, Michael John Palmer, Michael Scott Visser
-
Patent number: 6790841Abstract: Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R1 and R2 are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R1X and/or R2X can also be amino acid residues with X as NH.Type: GrantFiled: January 14, 2002Date of Patent: September 14, 2004Assignees: Wayne State University, The Regents of the University of MichiganInventors: Jiri Zemlicka, Yao-Ling Qiu, John C. Drach, Roger G. Ptak
-
Patent number: 6767910Abstract: Compounds of the formula (I) and their use as anti-platelet aggregation compounds.Type: GrantFiled: September 3, 2002Date of Patent: July 27, 2004Assignee: AstraZeneca ABInventor: Barry Teobald
-
Patent number: 6734180Abstract: An inhibitor of NF-&kgr;B comprising as an active ingredient an indan derivative represented by the general formula (I) or a salt thereof.Type: GrantFiled: March 22, 2000Date of Patent: May 11, 2004Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Yoichi Nunokawa, Takashi Nakatsuka, Masayuki Saitoh, Keiichi Abe