The Additional Hetero Ring Is A Diazine Patents (Class 514/252.02)
  • Publication number: 20040198739
    Abstract: This invention concerns HIV replication inhibitors of formula (I) the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents pheynl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl;n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl, substituted C1-6alkyl, C1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH?2?, —NHC(═O)R6, —C(═NH)R6 or a 5-membered hetrocycl; X1 is —NR5—,
    Type: Application
    Filed: February 3, 2004
    Publication date: October 7, 2004
    Inventors: Jerome Emile Georges Guillemont, Patrice Palandjian, Marc Rene de Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desire Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen
  • Publication number: 20040186102
    Abstract: The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use.
    Type: Application
    Filed: February 20, 2004
    Publication date: September 23, 2004
    Inventors: Chengde Wu, C. Eric Anderson, Huong Bui, Brian Dupre, Daxin Gao, George W. Holland, Jamal Kassir, Wen Li, Junmei Wang
  • Publication number: 20040180899
    Abstract: The invention relates to new phthalazine derivatives of formula (I), wherein R1 and R2: a) are independently in each case a lower alkyl; b) together form a bridge of subformula (I*), wherein the bond is achieved via the two terminal C atoms and m is 0 to 4; or c) together form a bridge of subformula (I**), wherein one or two of the ring members T1, T2, T3 and T4 are nitrogen, and the others are in each case CH, and the bond is achieved via atoms T1 and T4; A, B, D, E and T are independently N or CH subject to the proviso that at least one and not more than three of these radicals are N; X is imino, oxa, or thia; Y is hydrogen, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or unsubstituted or substituted cycloalkyl; and wherein the bonds characterized in subformula (I*) by a wavy line are either single or double bonds; to an N-oxide of a compound of formula I; a tautomer or mixture of tautomers of a compound of formula (I) of an N-oxide thereof; and a pharmaceutically acceptable s
    Type: Application
    Filed: March 29, 2004
    Publication date: September 16, 2004
    Inventors: Guido Bold, Paul William Manley
  • Publication number: 20040180878
    Abstract: The invention relates to compounds of formula: 1
    Type: Application
    Filed: January 16, 2004
    Publication date: September 16, 2004
    Inventors: Alain Di Malta, Georges Garcia, Richard Roux, Bruno Schoentjes, Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
  • Publication number: 20040180887
    Abstract: This invention relates to N-aroyl cyclic amine derivatives of formula (1), wherein X represents a bond, oxygen, NR3 or a group (CH2), wherein n represents 1, 2 or 3; Y represents CH2, CO, CH(OH), or CH2CH(OH); Het is an optionally substituted bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; Ar2 represents an optionally substituted phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S and their use as pharmaceuticals, specifically as orexin receptor antagonists.
    Type: Application
    Filed: April 26, 2004
    Publication date: September 16, 2004
    Inventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
  • Publication number: 20040162282
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: December 9, 2003
    Publication date: August 19, 2004
    Applicant: ChemoCentryx, Inc.
    Inventors: Andrew M.K. Pennell, James B. Aggen, J.J. Kim Wright, Subhabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi
  • Patent number: 6777416
    Abstract: The invention relates to novel isoxazolo pyrimidinones of general formula (I), a method for producing the same and the pharmaceutical use thereof.
    Type: Grant
    Filed: October 22, 2002
    Date of Patent: August 17, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Niewöhner, Helmut Haning, Thomas Lampe, Mazen Es-Sayed, Gunter Schmidt, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn, Karl-Heinz Schlemmer
  • Patent number: 6777412
    Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: wherein X is CH2O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an optionally substituted phenyl group or an optionally substituted heterocylyl group.
    Type: Grant
    Filed: June 27, 2003
    Date of Patent: August 17, 2004
    Assignee: Syngenta Limited
    Inventors: John Martin Clough, Christopher Richard Ayles Godfrey, Ian Thomas Streeting, Rex Cheetham, Paul John de Fraine, David Bartholomew, James John Eshelby
  • Publication number: 20040157845
    Abstract: Compounds having the general structure 1
    Type: Application
    Filed: February 9, 2004
    Publication date: August 12, 2004
    Applicant: Amgen Inc.
    Inventors: Elizabeth M. Doherty, Christopher H. Fotsch, Nianhe Han, Randall W. Hungate, Qingyian Liu, Mark H. Norman, Ning Xi, Shimin Xu
  • Publication number: 20040127497
    Abstract: The present invention relates to pyridyl substituted heterocycles and hydro isomers thereof and pharmaceutical compositions thereof that inhibit replication and/or proliferation of HCV virus. The present invention also relates to the use of the pyridyl heterocycles and hydro isomers thereof and/or pharmaceutical compositions comprising the compounds to treat or prevent HCV infections.
    Type: Application
    Filed: August 22, 2003
    Publication date: July 1, 2004
    Inventors: Rajinder Singh, Dane Goff, John Partridge
  • Publication number: 20040110725
    Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: 1
    Type: Application
    Filed: September 22, 2003
    Publication date: June 10, 2004
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Roland E. Dolle, Denton W. Hoyer, Tina Morgan Ross, James M. Rinker, Stanley J. Schmidt, Mark A. Ator
  • Patent number: 6747028
    Abstract: This invention concerns compounds of formula (I) prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and methods of their use in treating respiratory syncytial viral infections.
    Type: Grant
    Filed: December 27, 2001
    Date of Patent: June 8, 2004
    Assignee: Hanssen Pharmaceutica, N.V.
    Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Koenraad Jozef Lodewijk Marcel Andries
  • Publication number: 20040106616
    Abstract: Substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: January 21, 2003
    Publication date: June 3, 2004
    Inventors: Rajagopal Bakthavatchalam, Charles A. Blum, Harry Brielmann, Timothy M. Caldwell, Stephane De Lombaert, Kevin J. Hodgetts, Taeyoung Yoon, Xiaozhang Zheng
  • Publication number: 20040097501
    Abstract: This invention describes novel triazole compounds of formula IX: 1
    Type: Application
    Filed: September 14, 2001
    Publication date: May 20, 2004
    Inventors: David Bebbington, Ronald Knegtel, Hayley Binch, Julian Golec, Pan Li, Jean-Damien Charier
  • Patent number: 6734187
    Abstract: Purine derivatives represented by the following formula and salts thereof: wherein R1 represents a C1-C4 alkyl group or difluoromethyl group; R2 represents tetrahydrofuranyl group, a C1-C7 alkyl group and the like; X represents hydrogen atom, a halogen atom or nitro group; and A represents a group represented by the following formula: wherein R3 represents hydrogen atom, a halogen atom and the like; R4 and R5 represent hydrogen atom, a halogen atom, a C1-C4 alkyl group, a C1-C4 alkoxyl group and the like, which are useful as active ingredients of medicaments such as antiasthmatic agents.
    Type: Grant
    Filed: July 23, 2002
    Date of Patent: May 11, 2004
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Toshihiko Tanaka, Eiichirou Iwashita, Akiko Tarao, Akira Amenomori, Yuya Ono
  • Patent number: 6730672
    Abstract: The invention concerns compounds of formula (I) wherein each of G1, G2 and G3 is CH or N; m is 1 or 2; R1 includes hydrogen, halogeno and (1-4C)alkyl; M1 is a group of the formula: NR2—L1—T1R3 in which R2 and R3 together form a (1-4C)alkylene group, L1 includes (1-4C)alkylene, and T1 is CH or N; A may be a direct link; M2 is a group of the formula: (T2R4)r—L2—T3R5 in which r is 0 or 1, each of T2 and T3 is CH or N, each of R4 and R5 is hydrogen or (1-4C)alkyl, or R4 and R5 together form a (1-4C)alkylene group, and L2 includes (1-4C)alkylene; M3 may be a direct link to X; X includes sulphonyl; and Q includes naphthyl and a heterocyclic moiety; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use as antithrombotic or anticoagulant agents.
    Type: Grant
    Filed: March 8, 2001
    Date of Patent: May 4, 2004
    Assignee: Zeneca Limited
    Inventors: Alan Wellington Faull, Andrew Stocker, Colette Marie Mayo, John Preston
  • Patent number: 6730668
    Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; each R2 unit is independently selected from the group consisting of: a) hydrogen; b) —(CH2)jO(CH2)nR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —(CH2)jCON(R10)2; g) —(CH2)jOCON(R10)2; h) two R2 units can be taken together to form a carbonyl unit; i) and mixtures thereof; R8, R9a, R9b, and R10 are each independently hydrogen, C1-C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 units can be take together to form a carbocyclic or heterocyclic ring
    Type: Grant
    Filed: September 18, 2002
    Date of Patent: May 4, 2004
    Assignee: The Procter & Gamble Company
    Inventors: Michael Philip Clark, Matthew John Laufersweiler, Jane Far-Jine Djung, Michael George Natchus, Biswanath De
  • Publication number: 20040082571
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: June 11, 2003
    Publication date: April 29, 2004
    Applicant: ChemoCentryx, Inc.
    Inventors: Andrew M.K. Pennell, James B. Aggen, J.J. Kim Wright, Subrabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi
  • Patent number: 6723726
    Abstract: Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds of formula (I), wherein X is N or CH; A represents a fused 5, 6 or 7-membered heterocyclic ring containing 1 to 5 heteroatoms which may be the same or different and which are selected from N, O or S(O)m, wherein m is as defined above, the heterocyclic ring containing a total of 1, 2 or 3 double bonds inclusive of the bond in the pyridine or pyrimidine ring to which it is fused, with the provisos that the heterocyclic ring does not form part of a purine and that the fused heterocyclic ring does not contain two adjacent O or S(O)m atoms.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: April 20, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: George Stuart Cockerill, Malcolm Clive Carter, Stephen Barry Guntrip, Kathryn Jane Smith
  • Publication number: 20040067954
    Abstract: This invention relates to compounds of the formula (I) in which R1, R2, R3, X and Q are as defined above and their use as PDE IV inhibitors.
    Type: Application
    Filed: June 23, 2003
    Publication date: April 8, 2004
    Inventors: Hans-Michael Eggenweiler, Michael Wolf, Norbert Beier, Joachim Leibrock, Michael Gassen, Thomas Ehring
  • Publication number: 20040063679
    Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
    Type: Application
    Filed: September 27, 2002
    Publication date: April 1, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals Inc.
    Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R.R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel
  • Publication number: 20040063705
    Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer.
    Type: Application
    Filed: August 21, 2002
    Publication date: April 1, 2004
    Inventors: Jean-Christophe Harmange, Shon Booker, John L. Buchanan, Stuart Chaffee, Perry M. Novak, Simon Van Der Plas, Xiaotian Zhu
  • Publication number: 20040063709
    Abstract: Disclosed compounds of the formula (I) 1
    Type: Application
    Filed: January 2, 2003
    Publication date: April 1, 2004
    Applicant: SCHERING CORPORATION
    Inventors: Arthur G. Taveras, Michael Dwyer, Jianping Chao, John J. Baldwin, J. Robert Merritt, Ge Li, Jianhua Chao, Younong Yu
  • Publication number: 20040058933
    Abstract: The present invention relates to novel compounds, the preparation and use, particularly therapeutic, thereof. More specifically, it relates to compounds derived from aryl carbamates, the preparation and use thereof, particularly in the field of human and animal health. The compounds according to the invention are preferably 5-HT4 serotoninergic receptor ligands and can therefore be used in the therapeutic or prophylactic treatment of any disorder involving a 5-HT4 receptor. The invention also relates to pharmaceutical compositions comprising such compounds, the preparation and use thereof and treatment methods using said compounds.
    Type: Application
    Filed: August 13, 2003
    Publication date: March 25, 2004
    Inventors: Eric Nicolai, Sophie Curtet, James Sicsic, Frank Lezoualc'h, Rodolphe Fischemeister, Michel Langlois, Magali Maillet, Michele Launay
  • Patent number: 6710046
    Abstract: Disclosed is a pharmaceutical composition for modulating immunity, which comprises a benzimidazole, represented by the following general formula (I), a 3H tautomer, an optically active enantiomer or a pharmaceutically acceptable acid-addition salt thereof wherein, R represents an alkyl group having 1 to 5 carbon atoms, a hydroxyphenyl group or a methoxyphenyl group.
    Type: Grant
    Filed: April 23, 2001
    Date of Patent: March 23, 2004
    Assignee: Toray Industries, Inc.
    Inventor: Akira Matsumori
  • Patent number: 6710047
    Abstract: The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* or (iii) together form a bridge in subformula I** wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etheritied or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, p
    Type: Grant
    Filed: January 7, 2003
    Date of Patent: March 23, 2004
    Assignee: Novartis AG
    Inventors: Guido Bold, Jörg Frei, Peter Traxler, Karl-Heinz Altmann, Helmut Mett, David Raymond Stover, Jeanette Marjorie Wood
  • Publication number: 20040053933
    Abstract: Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders.
    Type: Application
    Filed: May 9, 2003
    Publication date: March 18, 2004
    Applicant: Neurocrine Biosciences, Inc.
    Inventors: Joseph Pontillo, Dragan Marinkovic, Marion C. Lanier, Joe Anh Tran, Melissa Arellano, Jessica Parker, Jodie Nelson, Chen Chen, Fabio C. Tucci, Caroline Chen, Wanlong Jiang, Nicole White
  • Publication number: 20040048861
    Abstract: This invention provides a method of treating a disease state in mammals that is alleviated by treatment with a protein kinase inhibitor, especially an ERK inhibitor, which method comprises administering a compound having the pharmacophoric features Grp1, Grp2 and Grp3: 1
    Type: Application
    Filed: May 13, 2003
    Publication date: March 11, 2004
    Inventors: Guy Bemis, Xiaoling Xie
  • Publication number: 20040048862
    Abstract: The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins.
    Type: Application
    Filed: August 8, 2003
    Publication date: March 11, 2004
    Inventors: Giuseppe Alvaro, Romano Di Fabio, Riccardo Giovannini, Giuseppe Guercio, Yves St-Denis, Antonella Ursini
  • Publication number: 20040038976
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: May 21, 2003
    Publication date: February 26, 2004
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
  • Publication number: 20040038969
    Abstract: Compounds having the general structure 1
    Type: Application
    Filed: May 20, 2003
    Publication date: February 26, 2004
    Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Vassil I. Ognyanov, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Liping H. Pettus, Hui-Ling Wang, Xianghong Wang, Premilla Arasasingham
  • Publication number: 20040034026
    Abstract: The invention relates to a combination which comprises a first active ingredient which is a vasculostatic compound and a second active ingredient which decreases the activity of the epidermal growth factor (EGF), in particular, for the delay of progression or treatment of a disease associated with deregulated angiogenesis, especially a proliferative disease; a pharmaceutical composition comprising such a combination; a commercial package comprising such a combination as a combined preparation; and to a method of treatment of a warm-blooded animal, especially a human.
    Type: Application
    Filed: May 21, 2003
    Publication date: February 19, 2004
    Inventors: Jeannette M Wood, Ralf Brandt, Guido Bold, Peter Traxler
  • Publication number: 20040029876
    Abstract: This invention relates to novel acylamino cyclopropane derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as modulators of dopamine D3 receptors and for the treatment of anxiety, psychosis, substance abuse, Parkinson's disease, sexual dysfunction, and other central nervous system disorders.
    Type: Application
    Filed: July 29, 2003
    Publication date: February 12, 2004
    Applicant: Pfizer Inc
    Inventors: Anton F. J. Fliri, Anthony R. Reinhold
  • Publication number: 20040029887
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: April 29, 2003
    Publication date: February 12, 2004
    Inventors: Pramila A. Bhatia, Jerome F. Daanen, Ahmed A. Hakeem, Teodozyj Kolasa, Mark A. Matulenko, Kathleen H. Mortell, Meena V. Patel, Andrew O. Stewart, Xueqing Wang, Zhiren Xia, Henry Q. Zhang
  • Publication number: 20040019059
    Abstract: The present invention is concerned with the compounds of formula 1
    Type: Application
    Filed: March 31, 2003
    Publication date: January 29, 2004
    Inventors: Eddy Jean Edgard Freyne, Jose Ignacio Andres-Gil, Frederik Dirk Deroose, Davy Petrus Franciscus Maria Petit, Maria Encarnacion Matesanz-Ballesteros, Rosa Maria Alvarez Escobar
  • Publication number: 20040014756
    Abstract: Compounds having the formula 1
    Type: Application
    Filed: March 20, 2003
    Publication date: January 22, 2004
    Inventors: Michael R. Michaelides, Michael L. Curtin, Yujia Dai, Steven K. Davidsen, Robin R. Frey, Yan Guo, Zhiqin Ji
  • Publication number: 20040014765
    Abstract: Disclosed are novel inhibitors of Chk-1 and methods of using the same for therapy.
    Type: Application
    Filed: May 28, 2003
    Publication date: January 22, 2004
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Robert George Boyle, Hassan Julien Imogai, Michael Cherry
  • Publication number: 20040009979
    Abstract: The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R1 is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are also described.
    Type: Application
    Filed: October 23, 2002
    Publication date: January 15, 2004
    Applicant: ZENECA LIMITED
    Inventors: Roger J. Butlin, Thorsten Nowak, Jeremy N. Burrows, Michael H. Block
  • Publication number: 20040002488
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: May 29, 2002
    Publication date: January 1, 2004
    Inventor: Marlon D. Cowart
  • Patent number: 6670362
    Abstract: Compounds of formula (I), pharmaceutical formulations thereof and the use of such compounds for treating endothelin mediated diseases or conditions are described herein. The compounds of the present invention have affinity for endothelin receptors, are selective for ETA over ETB, and thus are useful in the treatment of conditions mediated by endothelin.
    Type: Grant
    Filed: September 12, 2001
    Date of Patent: December 30, 2003
    Assignee: Pfizer Inc.
    Inventors: Bernard Joseph Banks, Anthony Logan Chubb, Douglas James Critcher, James John Eshelby, Darren John Schulz
  • Publication number: 20030236259
    Abstract: Novel aryl- and heteroarylpiperazines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
    Type: Application
    Filed: March 7, 2003
    Publication date: December 25, 2003
    Inventors: Rolf Hohlweg, Florencio Zaragoza Dorwald, Henrik Stephensen, Ingrid Pettersson, Bernd Peschke
  • Publication number: 20030232836
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: May 23, 2002
    Publication date: December 18, 2003
    Inventors: Andrew O. Stewart, Teodozyj Kolasa
  • Publication number: 20030232804
    Abstract: The present application describes glycinamidic compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
    Type: Application
    Filed: November 25, 2002
    Publication date: December 18, 2003
    Inventors: Donald J.P. Pinto, Wei Han, Zilun Hu, Jennifer Qiao
  • Publication number: 20030232788
    Abstract: This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.
    Type: Application
    Filed: February 7, 2003
    Publication date: December 18, 2003
    Applicant: Idun Pharmaceuticals, Inc.
    Inventors: Donald S. Karanewsky, Vincent J. Kalish, Edward D. Robinson, Brett R. Ullman
  • Publication number: 20030232808
    Abstract: Described is a sulfonyl derivative represented by the following formula (I): 1
    Type: Application
    Filed: December 20, 2002
    Publication date: December 18, 2003
    Applicant: DAIICHI PHARMACEUTICAL CO., LTD.
    Inventors: Syozo Kobayashi, Satoshi Komoriya, Masayuki Ito, Tsutomu Nagata, Akiyoshi Mochizuki, Noriyasu Haginoya, Takayasu Nagahara, Haruhiko Horino
  • Publication number: 20030229094
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: May 23, 2003
    Publication date: December 11, 2003
    Inventors: Pramila A. Bhatia, Jerome F. Daanen, Ahmed A. Hakeem, Teodozyj Kolasa, Mark A. Matulenko, Kathleen H. Mortell, Meena V. Patel, Andrew O. Stewart, Xueqing Wang, Zhiren Xia, Henry Q. Zhang
  • Patent number: 6660738
    Abstract: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.
    Type: Grant
    Filed: July 17, 2001
    Date of Patent: December 9, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Daniel Bur, Alexander Chucholowski, Henrietta Dehmlow
  • Publication number: 20030225088
    Abstract: The invention relates to substituted aromatic polycyclic tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.
    Type: Application
    Filed: September 26, 2002
    Publication date: December 4, 2003
    Applicant: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Mark A. Massa, Jane L. Wang, Deborah A. Mischke, Barry L. Parnas, Melvin L. Rueppel
  • Publication number: 20030225099
    Abstract: Ortho, meta-substituted bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.
    Type: Application
    Filed: June 4, 2003
    Publication date: December 4, 2003
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleemann
  • Publication number: 20030225098
    Abstract: The present application is directed to pyrazolopyrirnidine and furopyrimidine analogs of the formula (I) 1
    Type: Application
    Filed: March 21, 2003
    Publication date: December 4, 2003
    Inventors: Gavin C. Hirst, Lee D. Arnold, Andrew Burchat, Neil Wishart, David Calderwood, Carol K. Wada, Michael R. Michaelides, Zhiqin Ji, Melanie Muckey