Nitrogen Bonded Directly At 4-position Patents (Class 544/293)
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Publication number: 20040102463Abstract: The present invention relates to the anhydrous and hydrate forms of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate. The invention also relates to pharmaceutical compositions containing N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate and to methods of treating hyperproliferative disorders, such as cancer, by administering N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate.Type: ApplicationFiled: November 17, 2003Publication date: May 27, 2004Applicant: OSI Pharmaceuticals, Inc.Inventors: Douglas John Meldrum Allen, Timothy Norris, Jeffrey William Raggon, Dinos Paul Santafianos, Ravi Mysore Shanker
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Publication number: 20040087511Abstract: A compound of Formula (1): 1Type: ApplicationFiled: August 1, 2003Publication date: May 6, 2004Inventors: Takuya Shiraishi, Shojiro Kadono, Masayuki Haramura, Haruhiko Sato, Toshiro Kozono, Takaki Koga, Akihisa Sakamoto
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Patent number: 6727256Abstract: Substituted heteroaromatic compounds of formula (I), wherein X is N or CH; Y is CR1 and V is N; or Y is N and V is CR1; or Y is CR1 and V is CR2; or Y is CR2 and V is CR1; R1 represents a group CH3SO2CH2CH2NHCH2—Ar—, wherein Ar is selected from phenyl, furan, thiophene, pyrrole and thiazole, each of which may optionally be substituted by one or two halo, C1-4alkyl or C1-4alkoxy groups; R2 is selected from the group comprising hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkoxy, C1-4alkylamino and di[C1-4alkyl]amino; U represents a phenyl, pyridyl, 3H-imidazolyl, indolyl, isoindolyl, indolinyl, isoindolinyl, 1H-indazolyl, 2,3-dihydro-1H-indazolyl, 1H-benzimidazolyl, 2,3-dihydro-1H-benzimidazolyl or 1H-benzotriazolyl group, substituted by an R3 group and optionally substituted by at least one independently selected R4 group; R3 is selected from a group comprising benzyl, halo-, dihalo- and trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- and trihalobenzyType: GrantFiled: June 30, 2000Date of Patent: April 27, 2004Assignee: SmithKline Beecham CorporationInventors: Malcolm Clive Carter, George Stuart Cockerill, Stephen Barry Guntrip, Karen Elizabeth Lackey, Kathryn Jane Smith
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Patent number: 6713485Abstract: The present invention relates to substituted heteroaromatic compounds, methods for their preparation, pharmaceutical compositions containing them and their use in medicine. Specifically, the invention relates to quinazoline derivatives useful in treating disorders mediated by protein tyrosine kinase activity, in particular erbB-2 and/or EGFR activity.Type: GrantFiled: February 8, 2002Date of Patent: March 30, 2004Assignee: SmithKline Beecham CorporationInventors: Malcolm Clive Carter, George Stuart Cockerill, Stephen Barry Guntrip, Karen Elizabeth Lackey, Kathryn Jane Smith
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Patent number: 6706721Abstract: The present invention relates to the anhydrous and hydrate forms of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate. The invention also relates to pharmaceutical compositions containing N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate and to methods of treating hyperproliferative disorders, such as cancer, by administering N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate.Type: GrantFiled: July 29, 1999Date of Patent: March 16, 2004Assignee: OSI Pharmaceuticals, Inc.Inventors: Douglas John Meldrum Allen, Timothy Norris, Jeffrey William Raggon, Dinos Paul Santafianos, Ravi Mysore Shanker
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Publication number: 20040048880Abstract: The present invention relates to bicyclic heterocyclic groups of general formula 1Type: ApplicationFiled: March 27, 2003Publication date: March 11, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Birgit Jung, Flavio Solca
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Publication number: 20040044014Abstract: The present invention relates to bicyclic heterocycles of general formula 1Type: ApplicationFiled: April 17, 2003Publication date: March 4, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Birgit Jung, Flavio Solca
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Publication number: 20040039002Abstract: Quinazoline compounds and methods for the treatment of cancer and for the treatment of allergic reactions.Type: ApplicationFiled: June 5, 2003Publication date: February 26, 2004Applicant: Parker Hughes InstituteInventors: Fatih M. Uckun, Xing-Ping Liu, Rama Krishna Narla
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Publication number: 20040038977Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders.Type: ApplicationFiled: November 22, 2002Publication date: February 26, 2004Applicant: G.D. Searle & Co.Inventors: Jeffery S. Carter, Mark G. Obukowicz, Balekudru Devadas, John J. Talley, David L. Brown, Matthew J. Graneto, Stephen R. Bertenshaw, Donald J. Rogier, Srinivasan Raj Nagarajan, Cathleen E. Hanau, Susan J. Hartmann, Cindy L. Ludwig, Suzanne Metz, Donald E. Korte
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Patent number: 6673803Abstract: 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 groupType: GrantFiled: February 25, 2002Date of Patent: January 6, 2004Assignee: Zeneca LimitedInventors: Andrew Peter Thomas, Craig Johnstone, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
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Publication number: 20030236261Abstract: Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described.Type: ApplicationFiled: March 19, 2003Publication date: December 25, 2003Applicant: Icagen, Inc.Inventors: Aimee Dolores Reed, Michael Francis Gross, Serge Beaudoin
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Publication number: 20030229051Abstract: The present invention provides compounds that are irreversible inhibitors of tyrosine kinases. Also provided is a method of treating cancer, restenosis, atherosclerosis, endometriosis, and psoriasis and a pharmaceutical composition that comprises a compound that is an irreversible inhibitor of tyrosine kinases.Type: ApplicationFiled: May 20, 2003Publication date: December 11, 2003Inventors: Alexander James Bridges, William Alexander Denny, Ellen Myra Dobrusin, Annette Marian Doherty, David William Fry, Dennis Joseph McNamara, Howard Daniel Hollis Showalker, Jeffrey B. Smaill, Hairong Zhou
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Patent number: 6660746Abstract: The present invention relates to compounds of formula I: wherein R1, R2, and R3 have the meanings indicated in the specification, which are valuable pharmaceutical active compounds for the therapy and prophylaxis of diseases such as cardiovascular disorders such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses, or atherosclerosis. Compounds of formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for the preparation of compounds formula I, methods of therapy and prophylaxis of the designated disease states and for the production of pharmaceuticals therefor, and pharmaceutical compositions which comprise at least one compound of formula I.Type: GrantFiled: February 4, 2000Date of Patent: December 9, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schönafinger, Hartmut Strobel
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Patent number: 6653301Abstract: This invention describes novel pyrazole compounds of formula IIa: wherein R1 is T-Ring D, wherein 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 taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: December 19, 2001Date of Patent: November 25, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Robert Davies, Julian M. C. Golec, David Kay, Ronald Knegtel, Sanjay Patel
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Publication number: 20030216417Abstract: The invention concerns amide derivatives of Formula (I), wherein: G is N or CH; R1 is a group such as hydroxy, halo, trifluoromethyl, C1-6alkyl and C1-6alkoxy; each of R2 and R3 is hydrogen, halo, C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 is a group such as hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy and C3-7cycloalkyl, or R4 is of the Formula (IC): —K-J, wherein J is aryl, heteroaryl or heterocyclyl and K is a bond or a group such as oxy and imino, R5 is a group such as hydrogen, halo and trifluoromethyl; m is 1-3 and q is 0-4; or pharmaceutically acceptable salts or in vivo cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: May 20, 2003Publication date: November 20, 2003Applicant: ASTRAZENECA ABInventor: John G. Cumming
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Patent number: 6649620Abstract: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents an aryl group or a heteroaryl group, optionally substituted by C1-4 alkyl or SO2NH2; R3 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent, or represents a cyclic group of formula Ia, or represents a chain of formula Ib, and pharmaceutically acceptable salts thereof, are useful in the treatment of a variety of disorders including benign prostatic hyperplasia.Type: GrantFiled: September 23, 2002Date of Patent: November 18, 2003Assignee: Pfizer Inc.Inventors: Alan John Collis, David Nathan Fox
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Patent number: 6645969Abstract: This invention relates to the modulation and/or inhibition of cell signaling, cell proliferation, cell inflammatory response, the control of abnormal cell growth and cell reproduction. More specifically, this invention relates to the use of mono- and/or bicyclic aryl or heteroaryl quinazoline compounds in inhibiting cell proliferation, including compounds which are useful protein tyrosine kinase (PTK) inhibitors. The method of treating cell proliferation and/or differentiation or mediator release using said quinazoline compounds and their use in pharmaceutical compositions is described.Type: GrantFiled: May 18, 1995Date of Patent: November 11, 2003Assignee: Aventis Pharmaceuticals Inc.Inventors: Michael R. Myers, Alfred P. Spada, Martin P. Maguire, Paul E. Persons, Asher Zilberstein, Chin-Yi Jenny Hsu, Susan E. Johnson
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Patent number: 6642242Abstract: The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent —OCH2—, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof.Type: GrantFiled: March 19, 2001Date of Patent: November 4, 2003Assignee: Pfizer Inc.Inventors: Alan John Collis, David Nathan Abraham Fox, Julie Newman
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Patent number: 6638939Abstract: Quinazoline compounds and methods for the treatment of cancer and for the treatment of allergic reactions.Type: GrantFiled: August 7, 2001Date of Patent: October 28, 2003Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Xing-Ping Liu, Rama Krishna Narla
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Publication number: 20030186995Abstract: The invention relates to compounds of the formula 1 1Type: ApplicationFiled: January 21, 2003Publication date: October 2, 2003Applicant: Pfizer Inc.Inventors: John Charles Kath, Tom Norma Jacqueline, Liu Zhengyu, Eric David Cox, Joel Morris, Samit Kumar Bhattacharya
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Patent number: 6627634Abstract: Bicyclic heterocycles of general formula wherein: Ra to Rd, A to C and X are as defined herein, the tautomers, the stereoisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, 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, diseases of the lungs and respiratory tract, and the preparation thereof.Type: GrantFiled: March 23, 2001Date of Patent: September 30, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
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Patent number: 6617329Abstract: Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and air-ways, and the preparation thereof.Type: GrantFiled: August 23, 2001Date of Patent: September 9, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
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Patent number: 6613772Abstract: Compounds of the formula I in which R1, R2, R3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and therapy of cardiovascular diseases such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance.Type: GrantFiled: June 16, 2000Date of Patent: September 2, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schönafinger, Hartmut Strobel, Peter Schindler
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Patent number: 6610678Abstract: This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR6R7, OR6 or SR7; R2 is hydrogen, C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is Ar1 or Het1; R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R6 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R7 is hydrogen, C1-8alkyl, mono- or di(C3-6cyclo-alkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar2CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl; or R6 and R7 taken together with the nitrogen atom to which they are attached maType: GrantFiled: October 8, 2002Date of Patent: August 26, 2003Inventors: Charles Huang, Keith M. Wilcoxen, Chen Chen, Mustapha Haddach, James R. McCarthy
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Patent number: 6602882Abstract: Piperidine derivatives and pharmaceutical derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.Type: GrantFiled: May 24, 2001Date of Patent: August 5, 2003Assignee: SmithKline Beecham p.l.c.Inventors: David Thomas Davies, Roger Edward Markwell, Neil David Pearson, Andrew Kenneth Takle
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Publication number: 20030144506Abstract: The invention relates to processes for preparing compounds of the formula 1 1Type: ApplicationFiled: December 2, 2002Publication date: July 31, 2003Applicant: Pfizer Inc.Inventor: David Harold Brown
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Substituted pyrimidines, processes for their preparation, and their use as pesticides and fungicides
Patent number: 6596727Abstract: Substituted 4-amino- and 4-alkoxy-cycloalkylpyrimidines, processes for their preparation, and their use as pesticides and fungicides The invention relates to compounds of the formula in which R1, R2, R3 and Q are as defined in the description, X is NH or oxygen and E is a bond or a 1- to 4-membered carbon chain, to a process for their preparation, to agents containing them, and to their use in the control of pests and as fungicides.Type: GrantFiled: March 15, 1996Date of Patent: July 22, 2003Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Schaper, Rainer Preuss, Gerhard Salbeck, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lümmen, Werner Bonin -
Patent number: 6593333Abstract: The invention concerns amide derivatives of Formula (I), wherein: G is N or CH; R1 is a group such as hydroxy, halo, trifluoromethyl, C1-6alkyl and C1-6alkoxy; each of R2 and R3 is hydrogen, halo, C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 is a group such as hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy and C3-7cycloalkyl, or R4 is of the Formula (IC): —K—J, wherein J is aryl, heteroaryl or heterocyclyl and K is a bond or a group such as oxy and imino, R5 is a group such as hydrogen, halo and trifluoromethyl: m is 1-3 and q is 0-4; or pharmaceutically acceptable salts or in vivo cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: GrantFiled: March 23, 2001Date of Patent: July 15, 2003Assignee: Astrazeneca ABInventor: John G Cumming
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Publication number: 20030100573Abstract: This invention relates to compounds of the general formula: 1Type: ApplicationFiled: June 21, 2002Publication date: May 29, 2003Inventors: Yihan Wang, Chester A. Metcalf, William C. Shakespeare, Tomi K. Sawyer, Regine Bohacek
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Publication number: 20030087881Abstract: The present invention provides compounds that are irreversible inhibitors of tyrosine kinases. Also provided is a method of treating cancer, restenosis, atherosclerosis, endometriosis, and psoriasis and a pharmaceutical composition that comprises a compound that is an irreversible inhibitor of tyrosine kinases.Type: ApplicationFiled: October 17, 2002Publication date: May 8, 2003Inventor: Alexander James Bridges
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Patent number: 6545003Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: January 21, 2000Date of Patent: April 8, 2003Assignees: Elan Pharmaceuticals, Inc., American Home ProductsInventors: Francine S. Grant, Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett
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Publication number: 20030040521Abstract: Novel pyrimidine derivatives of formula I 1Type: ApplicationFiled: May 4, 2001Publication date: February 27, 2003Inventor: Harald Walter
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Patent number: 6521629Abstract: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-4 alkoxy optionally substituted by one or more fluorine atoms; R3 represents a 5- or 6-membered heterocyclic ring, the ring being optionally substituted; R4 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent, or represents a cyclic group of formula Ia, or represents a chain of formula Ib, and pharmaceutically acceptable salts thereof; are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.Type: GrantFiled: November 13, 2001Date of Patent: February 18, 2003Assignee: Pfizer Inc.Inventor: David Nathan Abraham Fox
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Publication number: 20030027829Abstract: Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described.Type: ApplicationFiled: July 24, 2001Publication date: February 6, 2003Inventors: Aimee Dolores Reed, Michael Francis Gross, Serge Beaudoin
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Publication number: 20030018029Abstract: The invention concerns quinazoline derivatives of the formula I 1Type: ApplicationFiled: May 2, 2002Publication date: January 23, 2003Applicant: ZENECA LIMITEDInventors: Andrew John Barker, Craig Johnstone
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Publication number: 20030004339Abstract: The invention provides a process for the production of a compound of formula (A) or a pharmaceutically acceptable salt or solvate thereof: 1Type: ApplicationFiled: May 13, 2002Publication date: January 2, 2003Applicant: Pfizer Inc.Inventors: Jens Bertil Ahman, Paul Blaise Hodgson, Sarah Jane Lewandowski, Robert Walton
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Publication number: 20020177601Abstract: A compound of formula (I) 1Type: ApplicationFiled: August 23, 2001Publication date: November 28, 2002Inventors: Frank Himmelsbach, Elke Langkopf, Stefan Blech, Birgit Jung, Thomas Metz, Flavio Solca
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Publication number: 20020173509Abstract: A compound of general formula I 1Type: ApplicationFiled: December 17, 2001Publication date: November 21, 2002Inventors: Frank Himmelsbach, Elke Langkopf, Stefan Blech, Birgit Jung, Anke Baum, Flavio Solca
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Publication number: 20020173646Abstract: 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, C1-13 alkyl, 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, C1-3 alkyl 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 coType: ApplicationFiled: February 25, 2002Publication date: November 21, 2002Applicant: ZENECA LIMITEDInventors: Andrew Peter Thomas, Craig Johnstone, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
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Publication number: 20020169180Abstract: The present invention relates to bicyclic heterocycles of general formula 1Type: ApplicationFiled: December 10, 2001Publication date: November 14, 2002Inventors: Frank Himmelsbach, Elke Langkopf, Thomas Metz, Flavio Solca, Birgit Jung, Anke Baum
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Patent number: 6476040Abstract: The present invention relates to methods and intermediates for preparing compounds of the formula 1 and the pharmaceutically acceptable salts and solvates thereof, as well as structurally related compounds, wherein R1, R2 and R15 are as defined herein. The foregoing compounds are useful in the treatment of hyperproliferative disorders, such as cancers, in mammals.Type: GrantFiled: March 30, 2000Date of Patent: November 5, 2002Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Timothy Norris, Dinos P. Santafianos, Richard S. Lehner
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Patent number: 6476031Abstract: The invention is directed to methods to inhibit TGF-&bgr; and/or p38-&agr; kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.Type: GrantFiled: August 27, 1999Date of Patent: November 5, 2002Assignee: Scios, Inc.Inventors: Sarvajit Chakravarty, Sundeep Dugar, John J. Perumattam, George F. Schreiner, David Y. Liu, John A. Lewicki
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Publication number: 20020161226Abstract: Novel substituted quinozaline compounds and conjugates useful to inhibit the growth of brain tumor cells and to inhibit adhesion and migration of brain tumor cells. The compounds of the invention include 4-(3′-bromo-4′-hydroxy phenyl)-amino-6,7-dimethoxyquinazoline and this compound covalently bound to EGF.Type: ApplicationFiled: July 11, 2001Publication date: October 31, 2002Applicant: Parker Hughes InstituteInventors: Fatih M. Uckun, Rama Krishna Narla, Xing-Ping Liu
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Patent number: 6465449Abstract: 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: GrantFiled: January 20, 2000Date of Patent: October 15, 2002Assignee: Pfizer Inc.Inventors: John Charles Kath, Norma Jacqueline Tom, Eric David Cox, Samit Kumar Bhattacharya
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Publication number: 20020147205Abstract: The present invention relates to substituted heteroaromatic compounds, methods for their preparation, pharmaceutical compositions containing them and their use in medicine. Specifically, the invention relates to quinazoline derivatives useful in treating disorders mediated by protein tyrosine kinase activity, in particular erbB-2 and/or EGFR activity.Type: ApplicationFiled: February 8, 2002Publication date: October 10, 2002Inventors: Malcolm Clive Carter, George Stuart Cockerill, Stephen Barry Guntrip, Karen Elizabeth Lackey, Kathryn Jane Smith
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Patent number: 6462044Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.Type: GrantFiled: August 30, 2001Date of Patent: October 8, 2002Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
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Publication number: 20020137757Abstract: Quinazoline compounds and methods for the treatment of cancer and for the treatment of allergic reactions.Type: ApplicationFiled: August 7, 2001Publication date: September 26, 2002Applicant: Parker Hughes InstituteInventors: Fatih M. Uckun, Xing-Ping Liu, Rama Krishna Narla
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Patent number: 6455527Abstract: Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN ; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nocicepType: GrantFiled: January 25, 2001Date of Patent: September 24, 2002Assignee: Schering CorporationInventors: Deen Tulshian, Ginny D. Ho, Lisa S. Silverman, Julius J. Matasi, Robbie L. McLeod, John A. Hey, Richard W. Chapman, Ana Bercovici, Francis M. Cuss
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Patent number: 6452005Abstract: Inhibitors of JAK3 kinase for the treatment of allergy inhibit mast cell degranulation an dmediator release.Type: GrantFiled: February 22, 2001Date of Patent: September 17, 2002Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Ravi Malaviya, Elise A. Sudbeck
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Patent number: 6444672Abstract: The present invention relates to heterocyclic antithrombotic compounds comprising a compound of the Formula I, wherein X′ is independently CH or N, and m is 0, 1, 2 or 3, or a pharmaceutically acceptable salt or prodrug thereof.Type: GrantFiled: April 17, 2000Date of Patent: September 3, 2002Assignee: Akzo Nobel N.V.Inventors: Constant Adriaan Anton van Boeckel, Philippus Johannes Marie van Galen, Johannes Bernardus Maria Rewinkel