Nitrogen Bonded Directly At 4-position Patents (Class 544/293)
  • Patent number: 7176312
    Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.
    Type: Grant
    Filed: October 12, 2002
    Date of Patent: February 13, 2007
    Assignees: The Scripps Research Institute, IRM LLC
    Inventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
  • Patent number: 7173038
    Abstract: The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidin-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof, processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as a active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of number of disease states including cancer and rheumatoid arthritis.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: February 6, 2007
    Assignee: AstraZeneca AB
    Inventors: Andrew Peter Thomas, Elaine Sophie Elizabeth Stokes, Laurent Francois Andre Hennequin
  • Patent number: 7160891
    Abstract: The invention concerns the use of the quinazoline derivatives of Formula (I) wherein each of Q1, Z, m, R1, R2, R3 and Q2 have any of the meanings defined in the description in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal
    Type: Grant
    Filed: November 20, 2002
    Date of Patent: January 9, 2007
    Assignee: AstraZeneca AB
    Inventors: Nelly Corine Moore, Keith Oldham
  • Patent number: 7157467
    Abstract: The invention concerns the use of the quinazoline derivatives of Formula (I) Wherein each of m, R1, n, R2 and R3 have any of the meanings defined in the description in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions such as autoimmune diseases like transplant rejection or rheumatoid arthritis in a warm-blooded animal.
    Type: Grant
    Filed: November 20, 2002
    Date of Patent: January 2, 2007
    Assignee: AstraZeneca AB
    Inventors: Nelly Corine Moore, Keith Oldham
  • Patent number: 7157466
    Abstract: Ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorde4rs characterized by aberrant erbB family PTK activity.
    Type: Grant
    Filed: June 28, 2001
    Date of Patent: January 2, 2007
    Assignee: SmithKline Beecham (Cork) Limited
    Inventors: Michael Scott McClure, Martin Howard Osterhout, Frank Roschangar, Mark Joseph Sacchetti
  • Patent number: 7148230
    Abstract: The invention concerns quinazoline derivatives of Formula I wherein R1 and R2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB, particularly EGF, receptor tyrosine kinases.
    Type: Grant
    Filed: June 1, 2004
    Date of Patent: December 12, 2006
    Assignee: AstraZeneca AB
    Inventors: Robert Hugh Bradbury, Jason Grant Kettle, James McCabe, Andrew Turner, Laurent Francois Andre Hennequin
  • Patent number: 7148231
    Abstract: The invention is concerned with a novel polymorph of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. This polymorph exhibits superior properties compared to the previously known forms of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. The [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride is an inhibitor of tyrosine kinase enzymes, and are useful in the treatment of cancer. Also disclosed are methods of making and using the novel polymorph, as well as pharmaceutical compositions containing the novel polymorph.
    Type: Grant
    Filed: February 3, 2004
    Date of Patent: December 12, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andre Gerard Bubendorf, Michael Hennig, Pirmin Hidber, Goesta Rimmler, Franziska Rohrer
  • Patent number: 7141564
    Abstract: Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
    Type: Grant
    Filed: May 24, 2002
    Date of Patent: November 28, 2006
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Gerald Brooks, David Thomas Davies, Graham Elgin Jones, Roger Edward Markwell, Neil David Pearson
  • Patent number: 7132427
    Abstract: This invention relates to compounds of the general formula: in which RA, RB, RC and RD are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: June 21, 2002
    Date of Patent: November 7, 2006
    Assignee: Ariad Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Chester A. Metcalf, III, William C. Shakespeare, Tomi K. Sawyer, Regine Bohacek, Rajeswari Sundaramoorthi
  • Patent number: 7115615
    Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein each of m, R1, n, R2 and R3 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
    Type: Grant
    Filed: August 15, 2001
    Date of Patent: October 3, 2006
    Assignee: AstraZeneca
    Inventors: Laurent Francois Andre Hennequin, Patrick Ple, Christine Marie Paul Lambert
  • Patent number: 7109333
    Abstract: A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) ?wherein L and L? are suitable leaving groups, with a compound of formula (III) UNH2??(III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L?.
    Type: Grant
    Filed: February 3, 2005
    Date of Patent: September 19, 2006
    Assignee: SmithKline Beecham Corporation
    Inventors: Malcolm Clive Carter, George Stuart Cockerill, Stephen Barry Guntrip, Karen Elizabeth Lackey, Kathryn Jane Smith
  • Patent number: 7105669
    Abstract: A compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2 or NR10 where R10 is hydrogen or C1-6 alkyl, and R1, R2, R3, R4, R5, R6, R7, R8 and R9 are various specified organic groups. These compounds are inhibitors of aurora 2 kinase, and are useful in the treatment of cancer.
    Type: Grant
    Filed: September 18, 2000
    Date of Patent: September 12, 2006
    Assignee: AstraZeneca AB
    Inventors: Andrew Austen Mortlock, Nicholas John Keen
  • Patent number: 7084147
    Abstract: Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.
    Type: Grant
    Filed: February 18, 2005
    Date of Patent: August 1, 2006
    Assignee: SmithKline Beecham Corporation
    Inventors: George Stuart Cockerill, Karen Elizabeth Lackey
  • Patent number: 7081461
    Abstract: The use of a compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, NH or NR8 where R8 is hydrogen or C1-6alkyl; Ra is a 3-quinoline group or a group of sub-formula (i) where R5, R6 and R7 are various specific organic groups, in the preparation of a medicament for use in the inhibtion of aurora 2 kinase. Novel compounds of formula (I) and pharmaceutical compositions useful in the treatment of cancer are also described and claimed.
    Type: Grant
    Filed: September 18, 2000
    Date of Patent: July 25, 2006
    Assignee: AstraZeneca AB
    Inventors: Andrew Austen Mortlock, Nicholas John Keen
  • Patent number: 7060825
    Abstract: The invention claimed herein relates to an improvement in a process for synthesizing a compound of formula Ib: wherein R1 and R2 are each individually amino or N-alkyl substituted amino; hydroxy; alkoxy; keto; lower alkyl; or a nitrogen or oxygen protecting group; R3 is hydrogen; hydroxy; alkoxy; trifluoromethyl alkoxy; halo; sulfhydryl or alkylthio; R4 is —C(O)—X; X is hydroxy; alkoxy; or an amino acid residue; in which process a 2-amino-5-nitro-benzonitrile starting reagent is cyclized to form 2,4-diamino-6-nitro-quinazoline, which is converted to 2,4,6-triamino-quinazoline, which is converted to 2,4-diamino-6-cyano-quinazoline, which is converted to 2,4-diamino-6-formyl-quinazoline; in which the improvement includes: reacting an R4-p-benzoic acid alkylene moiety with triethyl phosphite to form a 4-R4-carbonyloxyalkyl-phenyl-alkyldiethylphosphite; and reacting the 2,4-diamino-6-formyl-quinazoline with the 4-R4-carbonyloxyalkyl-phenyl-alkyldiethylphosphite to form the compound of formula Ib.
    Type: Grant
    Filed: July 25, 2003
    Date of Patent: June 13, 2006
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventors: Ye Wu, Harry Kochat
  • Patent number: 7038049
    Abstract: The present disclosure includes compounds, for example a compound according to formula I or a pharmaceutically acceptable salt thereof. The compounds of the present disclosure are useful in methods of treating cancerous conditions.
    Type: Grant
    Filed: May 24, 2004
    Date of Patent: May 2, 2006
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Xing-Ping Liu, Rama Krishna Narla
  • Patent number: 7019012
    Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction med
    Type: Grant
    Filed: December 17, 2001
    Date of Patent: March 28, 2006
    Assignee: Boehringer Ingelheim International Pharma GmbH & Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Stefan Blech, Birgit Jung, Anke Baum, Flavio Solca
  • Patent number: 7012076
    Abstract: Fused bicyclic amines of formula (1) are described wherein Ar is an aryl or heteroaryl group; Y is a —S(O2)— or —C(O)— group; R1 is a hydrogen or halogen atom or an alkyl, haloalkyl, alkoxy, haloalkoxy or cyano group; X is a nitrogen atom or a C(R1a) group where R1a is as defined for R1 and may be the same or different; W and Z are each a carbon atom and together with U form an optionally substituted five- or six-membered monocyclic aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the activity of Class 1 receptor tyrosine kinases and are of use in the prophylaxis and treatment of hyperproliferative disorders such as cancer, psoriasis, restenosis, atherosclerosis and fibrosis.
    Type: Grant
    Filed: March 29, 2001
    Date of Patent: March 14, 2006
    Assignee: Celltech R&D Limited
    Inventors: David Festus Charles Moffat, Peter David Davis
  • Patent number: 7001904
    Abstract: The invention concerns quinazoline and quinoline derivatives of Formula (I) wherein Q1 includes a quinazoline or quinoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2, R3 and R5 is hydrogen or (1-6C)alkyl, provides that one of the parts of groups R2 and R4 together, R3 and R4 together and R5 and R4 together forms a bond; R6 is an optionally substituted group selected from (2-6C) alkenyl, (2-6C) alkynyl, (3-7C)cycloalkyl and (3-7C) cycloalkenyl, or R6 is a substituted (1-6C) alkyl group; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded
    Type: Grant
    Filed: June 19, 2001
    Date of Patent: February 21, 2006
    Assignee: AstraZeneca AB
    Inventor: Jeffrey Philip Poyser
  • Patent number: 7001910
    Abstract: The present invention refers to compounds of the general formula (I), to their possible pharmaceutically acceptable salts and tautomeric forms. The present invention also refers to a process for their production and to their use as antidiabetic and *hypoglycemic agents, alone or in combination with other antidiabetic agents, such as sulfonilureas or biguanides, as well as for the treatment of complications associated to the resistance to the insulin, such as hypertension, hyperuricemia or other cardiovascular, metabolic, endocrine conditions, or other conditions related with diabetes.
    Type: Grant
    Filed: November 15, 2000
    Date of Patent: February 21, 2006
    Assignee: Vita-Invest S.A.
    Inventors: Marisabel Mourelle Mancini, Juan Carlos Del Castillo Nieto, Elisabet De Ramon Amat
  • Patent number: 6972288
    Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rd, A to G and X are defined as in claim 1, the tautomers, the steroisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, their use for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract, and the preparation thereof.
    Type: Grant
    Filed: February 24, 2000
    Date of Patent: December 6, 2005
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Thomas Metz, Flavio Solca, Stefan Blech
  • Patent number: 6933299
    Abstract: Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: August 23, 2005
    Assignee: SmithKline Beecham Corporation
    Inventors: George Stuart Cockerill, Karen Elizabeth Lackey
  • Patent number: 6933300
    Abstract: Inhibitors of JAK3 kinase for the treatment of allergy, and others are described.
    Type: Grant
    Filed: April 23, 2002
    Date of Patent: August 23, 2005
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Ravi Malavia, Elise A. Sudbeck
  • Patent number: 6924285
    Abstract: The present invention relates to bicyclic heterocyclic groups of general formula wherein Ra, Rb, Rc, Rd and X are defined as in claim 1, the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostate hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: August 2, 2005
    Assignee: Boehringer Ingelheim Pharma GmbH & Co.
    Inventors: Frank Himmelsbach, Birgit Jung, Flavio Solca
  • Patent number: 6919338
    Abstract: The use of a compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6alkyl; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2, R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed.
    Type: Grant
    Filed: June 21, 2001
    Date of Patent: July 19, 2005
    Assignee: AstraZeneca AB
    Inventors: Andrew Mortlock, Frederic Jung
  • Patent number: 6911446
    Abstract: The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with quinazoline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the invention describes methods of preventing and treating serine/threonine protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to quinazoline compounds and pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: June 28, 2005
    Assignee: Sugen, Inc.
    Inventors: Peng C. Tang, Gerald McMahon, Heinz Weinberger, Bernhard Kutscher, Harald App
  • Patent number: 6906070
    Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: June 14, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Qi Han, Renhua Li, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
  • Patent number: 6903107
    Abstract: A serine protease inhibitor having the formula (I), in which J is H, R1, R1—O—C(O)—, R1—C(O—, R1—SO2—, R3OOC—(CHR2)p—, (R2a,R2b)N—CO—(CHR2)p— or Het-CO—(CHR2)p—; W is an amino-acid of the formula —NH—CHR1—C(O)—, —NR4—CH((CH2)qC(O)OR1)—C(O)—, —NR4—CH((CH2)qC(O)N(R2a,R2b))—C(O)—, —NR4—CH((CH2)qC(O)Het)-C(O)—, D-1-Tiq, D-3-Tiq, D-Atc, Aic, D-1-Piq, D-3 Piq, glutanyl or a (C1-C6) alkylester thereof; E is —NR2—CH2— or the fragment ?which is unsubstituted or substituted with (1-6C)alkyl, (1-6C)alkoxy or benzyloxy; R1 is selected form (1-12C)alkyl, (2-12C)alkenyl, (2-12C)alkynyl, (3-12C)cycloalkyl and (3-12C)cycloalkyl(1-6C)alkylene, which groups are unsubstituted or substituted with (3-12C)cycloalkyl, (1-6C)alkoxy, oxo, OH, CF3 or halogen, and from (6-14C)aryl, (7-15C)aralkyl, (8-16C)aralkenyl and (14-20C)(bisary)alkyl, wherein the aryl groups are unsubstituted or substituted with (1-6C)alkyl, (3-12C)cycloalkyl, (1-6C)alkoxy, OH, CF3 or halogen; R2, R2a and R2b are each independently selected from H, (1-
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: June 7, 2005
    Assignee: Akzo Nobel N.V.
    Inventors: Cornelis Marius Timmers, Johannes Bernardus Maria Rewinkel
  • Patent number: 6900221
    Abstract: The present invention relates to a stable crystalline form of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride designated the B polymorph, its production in essentially pure form, and its use. The invention also relates to the pharmaceutical compositions containing the stable polymorph B form of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine as hydrochloride, as well other forms of the compound, and to methods of treating hyperproliferative disorders, such as cancer, by administering the compound.
    Type: Grant
    Filed: November 9, 2000
    Date of Patent: May 31, 2005
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Timothy Norris, Jeffrey W. Raggon, Richard D. Connell, James D. Moyer, Michael J. Morin, Shama M. Kajiji, Barbara A. Foster, Karen J. Ferrante, Sandra L. Silberman
  • Patent number: 6897214
    Abstract: The invention concerns quinazoline derivatives of the formula I wherein X1 is a direct link or a group such as CO, C(R2)2 and CH(OR2); wherein Q1 is phenyl, naphthyl or a 5- or 6-membered heteroaryl moiety and Q1 optionally bears up to 3 substituents; wherein m is 1 or 2 and each R1 may be a group such as hydrogen, halogeno and trifluoromethyl; and wherein Q2 may be phenyl or a 9- or 10-membered bicyclic heterocyclic moiety and Q2 optionally bears up to 3 substituents; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.
    Type: Grant
    Filed: May 2, 2002
    Date of Patent: May 24, 2005
    Assignee: Zeneca Limited
    Inventors: Andrew John Barker, Craig Johnstone
  • Patent number: 6897210
    Abstract: The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected
    Type: Grant
    Filed: November 3, 2003
    Date of Patent: May 24, 2005
    Assignees: Zeneca Limited, Zeneca Pharma S. A.
    Inventors: Andrew Peter Thomas, Craig Johnstone, Edward Clayton, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
  • Patent number: 6881753
    Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure: where A, B, D, Q, X1, R, R1, X2 and R2 are as defined herein. These compounds are useful as antiarrhythmic agents. In addition, a method is provided for preventing cardiac arrhythmia employing the above compounds.
    Type: Grant
    Filed: April 14, 2004
    Date of Patent: April 19, 2005
    Assignee: Bristol-Myers Squibb Co.
    Inventors: John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear
  • Patent number: 6867201
    Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R1, R3 and R4 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
    Type: Grant
    Filed: August 22, 2002
    Date of Patent: March 15, 2005
    Assignee: Pfizer Inc
    Inventors: John Charles Kath, Norma Jacqueline Tom, Eric David Cox, Samit Kumar Bhattacharya
  • Patent number: 6849625
    Abstract: The invention concerns quinazoline derivatives of Formula I wherein each of m, R1, n, R2 and R3 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: February 1, 2005
    Assignee: AstraZeneca AB
    Inventors: Christine Marie Paul Lambert, Patrick Ple
  • Publication number: 20040265228
    Abstract: Radiolabeled epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors and their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are disclosed.
    Type: Application
    Filed: September 11, 2003
    Publication date: December 30, 2004
    Inventors: Alexander Levitzki, Eyal Mishani, Giuseppina Ortu, Iris Ben-David, Yulia Rozen
  • Publication number: 20040242604
    Abstract: The invention relates to compounds of formula 1 1
    Type: Application
    Filed: May 20, 2004
    Publication date: December 2, 2004
    Applicant: Pfizer Inc
    Inventors: Samit Kumar Bhattacharya, Jinshan Chen, Richard Damian Connell, John Charles Kath, Goss S. Kauffman, Blaise S. Lippa, Joel Morris
  • Publication number: 20040230055
    Abstract: Substituted alkylmetal reagents such as (trimethylsilylmethyl)lithium are reacted with azaaromatic compounds and/or nitrogen heterocycle compounds to produce functionalized azaaromatic compounds and functionalized nitrogen heterocycle compounds.
    Type: Application
    Filed: April 6, 2004
    Publication date: November 18, 2004
    Inventors: Christopher J. Woltermann, Douglas E. Sutton
  • Publication number: 20040214841
    Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, m, R1, R2, R3 and Q2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
    Type: Application
    Filed: November 5, 2002
    Publication date: October 28, 2004
    Inventors: Laurent Francois Andre Hennequin, Patrick Ple
  • Publication number: 20040209904
    Abstract: Compounds having the formula (I), 1
    Type: Application
    Filed: April 15, 2004
    Publication date: October 21, 2004
    Inventors: James Patrick Dunn, David Michael Goldstein, Christoph Martin Stahl, Teresa Alejandra Trejo-Martin
  • Patent number: 6806274
    Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.
    Type: Grant
    Filed: January 7, 2002
    Date of Patent: October 19, 2004
    Assignee: AstraZeneca UK Limited
    Inventors: Graham C Crawley, Laurent F A Hennequin, Darren McKerrecher, Patrick Ple, Jeffrey Philip Poyser, Christine M P Lambert
  • Patent number: 6800644
    Abstract: The present invention provides a novel nitrogen-containing heterocyclic compound useful as a phosphodiesterase-4 inhibitor, and a medicament comprising the same. Further, the present invention provides a nitrogen-containing heterocyclic compound represented by the following formula, its salt or hydrates thereof, and a medicament comprising the same.
    Type: Grant
    Filed: November 2, 2001
    Date of Patent: October 5, 2004
    Assignee: Eisai Co., Ltd.
    Inventors: Kazuki Miyazaki, Yasutaka Takase, Takao Saeki
  • Publication number: 20040192711
    Abstract: The invention provides novel JAK-3 inhibitors that are useful for treating leukemia and lymphoma. The compounds are also useful to treat or prevent skin cancer, as well as sunburn and UVB-induced skin inflammation. In addition, the compounds of the present invention prevent the immunosuppressive effects of UVB radiation, and are useful to treat or prevent autoimmune diseases, inflammation, and transplant rejection. The invention also provides pharmaceutical compositions comprising compounds of the invention, as well as therapeutic methods for their use.
    Type: Application
    Filed: November 17, 2003
    Publication date: September 30, 2004
    Applicant: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Elise A. Sudbeck, Marina Cetkovic, Ravi Malaviya, Xing-Ping Liu
  • Patent number: 6797710
    Abstract: The present invention relates to antithrombotic compounds comprising the group Q, Q having formula (I), wherein the substructure (i) is a structure selected from (a, b and c), wherein X is O or S; X′ being independently CH or N; and m is 0, 1, 2 or 3; wherein the group Q is bound through an oxygen atom or an optionally substituted nitrogen or carbon atom, or a pharmaceutically acceptable salt thereof or a prodrug thereof. The compounds of the invention are therapeutically active and in particular are antithrombotic agents.
    Type: Grant
    Filed: June 20, 2002
    Date of Patent: September 28, 2004
    Assignee: Akzo Nobel N.V.
    Inventors: Constant Adriaan Anton van Boeckel, Philippus Johannes Marie van Galen, Johannes Bernardus Maria Rewinkel
  • Patent number: 6794389
    Abstract: There is provided an excellent novel analgesic having an analgesic effect which is effective widely against a pain including a chronic pain or an allodynia accompanied with herpes zoster by acting on a nociceptin receptor. The present invention relates to a compound represented by the following formula: or a salt thereof.
    Type: Grant
    Filed: September 25, 2002
    Date of Patent: September 21, 2004
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Masahiko Okana, Kazuya Mori
  • Publication number: 20040176603
    Abstract: The present invention relates to new substituted nitrogen-containing heterobicyclic compounds of general formula 1
    Type: Application
    Filed: December 18, 2003
    Publication date: September 9, 2004
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Henning Priepke, Roland Pfau, Kai Gerlach, Uwe Ries, Wolfgang Wienen, Eckhart Bauer, Herbert Nar
  • Publication number: 20040171620
    Abstract: Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives hereof useful in methods of treatment of bacterial infections in mammals, particularly man.
    Type: Application
    Filed: April 6, 2004
    Publication date: September 2, 2004
    Inventors: Gerald Brooks, David Thomas Davies, Graham Elgin Jones, Roger Edward Markwell, Neil David Pearson
  • Publication number: 20040171586
    Abstract: Compounds of the following formula are disclosed: 1
    Type: Application
    Filed: December 23, 2003
    Publication date: September 2, 2004
    Inventors: Terence P. Keenan, William C. Shakespeare
  • Publication number: 20040162300
    Abstract: The invention is concerned with a novel polymorph of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. This polymorph exhibits superior properties compared to the previously known forms of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. The [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride is an inhibitor of tyrosine kinase enzymes, and are useful in the treatment of cancer. Also disclosed are methods of making and using the novel polymorph, as well as pharmaceutical compositions containing the novel polymorph.
    Type: Application
    Filed: February 3, 2004
    Publication date: August 19, 2004
    Inventors: Andre Gerard Bubendorf, Michael Hennig, Pirmin Hidber, Goesta Rimmler, Franziska Rohrer
  • Publication number: 20040158065
    Abstract: Methods and materials for preparing irreversible inhibitors of tyrosine kinases of general Formula 1 are disclosed. Such inhibitors, which include N-[4-(3-chloro-4-floro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide, are useful for treating cancer, restenosis, atherosclerosis, endometriosis and psoriasis. The disclosed methods employ protecting schemes to minimize undesirable diacryloylamino-quinazoline side products.
    Type: Application
    Filed: February 4, 2004
    Publication date: August 12, 2004
    Inventors: Hubert Barth, Alexander James Bridges, Ronald J. Heemstra, Nicole Marcia Horne, Robert Craig Hughes, Thomas Elliott Jacks, Dennis Joseph McNamara, Simon Schneider, Klaus Steiner, Peter Laurence Toogood, Roy Thomas Winters
  • Publication number: 20040116422
    Abstract: A compound of the formula (I) 1
    Type: Application
    Filed: August 21, 2003
    Publication date: June 17, 2004
    Inventors: Yasunori Kitano, Eiji Kawahara, Tsuyoshi Suzuki, Daisuke Abe, Masahiro Nakajou, Naoko Ueda