Nitrogen Bonded Directly At 4-position Patents (Class 544/293)
-
Publication number: 20020115675Abstract: Compounds of the formula 1Type: ApplicationFiled: August 22, 2001Publication date: August 22, 2002Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
-
Patent number: 6432955Abstract: The present invention relates to therapeutically active antithrombotic compounds.Type: GrantFiled: October 4, 2000Date of Patent: August 13, 2002Assignee: Akzo Nobel N.V.Inventors: Constant Adriaan Anton van Boeckel, Philippus Johannes Marie van Galen, Johannes Bernardus Maria Rewinkel
-
Patent number: 6414148Abstract: The invention relates to quinazoline derivatives of formula (1) 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 alkyType: GrantFiled: March 25, 1999Date of Patent: July 2, 2002Assignees: 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
-
Publication number: 20020082271Abstract: Compounds of the formula 1Type: ApplicationFiled: August 22, 2001Publication date: June 27, 2002Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
-
Publication number: 20020082420Abstract: A compound of formula (I) 1Type: ApplicationFiled: August 21, 2001Publication date: June 27, 2002Inventors: Frank Himmelsbach, Elke Langkopf, Stefan Blech, Birgit Jung, Thomas Metz
-
Publication number: 20020082270Abstract: Compounds of the formula 1Type: ApplicationFiled: August 22, 2001Publication date: June 27, 2002Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
-
Publication number: 20020077330Abstract: A compound of formula (I) 1Type: ApplicationFiled: August 15, 2001Publication date: June 20, 2002Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
-
Patent number: 6403580Abstract: Quinazolines of the formula having 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: August 23, 2001Date of Patent: June 11, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
-
Patent number: 6399602Abstract: 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: GrantFiled: September 11, 1998Date of Patent: June 4, 2002Assignee: Zeneca LimitedInventors: Andrew John Barker, Craig Johnstone
-
Publication number: 20020061879Abstract: The present invention is directed to nitrosated or nitrosylated a-adrenergic receptor antagonists, compositions comprising a-adrenergic receptor antagonists that are optionally substituted with at least one NO or NO2 moiety and compounds that donate, transfer or release nitric oxide or elevate levels of endogenous endothelium-derived relaxing factor, and methods for treating sexual dysfunctions in males and females.Type: ApplicationFiled: December 21, 2001Publication date: May 23, 2002Inventors: David S. Garvey, Joseph D. Schroeder, Inigo Saenz de Tejada
-
Patent number: 6384223Abstract: This invention provides a process for preparing compounds of formula 1: wherein: X is phenyl optionally substituted with one or more substituents selected from the group consisting of halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy of 2-7 carbon atoms, carboalkyl of 2-7 carbon atoms, amino, and alkanoylamino of 1-6 carbon atoms; R and R1 are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, or trifluoromethyl; R2 is hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, trifluoromethyl; R3 is independently hydrogen, alkyl of 1-6 carbon atoms, carboxy, carboalkoxy of 1-6 carbon atoms, phenyl, or carboalkyl of 2-7 carbon atoms; n=2-4; or a pharmaceutically acceptable salt thereof, with the proviso that each R3 of Y may be the same or different.Type: GrantFiled: May 4, 2000Date of Patent: May 7, 2002Assignee: American Home Products CorporationInventor: Constantine Gletsos
-
Publication number: 20020042513Abstract: 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: ApplicationFiled: May 16, 2001Publication date: April 11, 2002Applicant: Parker Hughes InstituteInventors: Fatih M. Uckun, Elise A. Sudbeck, Marina Cetkovic, Ravi Malaviya, Xing-Ping Liu
-
Publication number: 20020040028Abstract: Compounds of formula I, 1Type: ApplicationFiled: November 13, 2001Publication date: April 4, 2002Inventor: David Nathan Abraham Fox
-
Patent number: 6362336Abstract: The invention relates to quinazoline derivatives of the formula: [wherein: Y1 represents —O—, —S—, —CH2—, —SO—, —SO2—, —NR5CO—, —CONR6—, —SO2NR7—, —NR8SO2— or —NR9— (wherein R5, R6, R8 and R9 each independently represents hydrogen, alkyl or alkoxyalkyl); R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, alkyl, alkoxy, alkylthio, amino or alkylamino.Type: GrantFiled: June 11, 2001Date of Patent: March 26, 2002Assignees: Zeneca Limited, Zeneca Pharma S. A.Inventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
-
Patent number: 6358962Abstract: Quinazoline compounds and methods for the treatment of cancer and for the treatment of allergic reactions.Type: GrantFiled: February 8, 2001Date of Patent: March 19, 2002Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Xing-Ping Liu, Rama Krishna Narla
-
Publication number: 20020032208Abstract: The invention relates to quinazoline derivatives of the formula: 1Type: ApplicationFiled: June 11, 2001Publication date: March 14, 2002Applicant: ZENECA LIMITEDInventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
-
Patent number: 6352989Abstract: 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. wherein the ring A is an aromatic hydrocarbon ring which may have a heteroatom, the ring B represents (a) a saturated hydrocarbon ring, (b) an unsaturated hydrocarbon ring, (c) a saturated heterocyclic ring or (d) an unsaturated heterocyclic ring, all of which may have a substituent group.Type: GrantFiled: July 26, 2000Date of Patent: March 5, 2002Assignee: Eisai Co., Ltd.Inventors: Kazuki Miyazaki, Yasutaka Takase, Takao Saeki
-
Patent number: 6346359Abstract: Disclosed are a pyrrolopyrimidineone compound represented by the following general formula (1) and a heat-sensitive recording material using the pyrrolopyrimidineone compound as a coupler: General formula (1) wherein R1 and R2 each independently represents a hydrogen atom, a halogen atom, an aryl group, an alkyl group, a cyano group, an acyl group, a carbamoyl group, an alkoxycarbonyl group, an aryloxycarbonyl group, an alkylsulfonyl group, or an arylsulfonyl group; R3 represents an amino group, a substituted amino group, a hydroxyl group, an acyloxy group, an arylcarboxyl group, an alkoxy group, an aryloxy group, an alkylthio group, or an arylthio group; R4 represents a hydrogen atom, a halogen atom, or an electron attracting group whose Hammett substituent constant &sgr;p is 0.2 or more; and L represents a substituent group which can leave when the compound reacts with a diazonium salt.Type: GrantFiled: April 24, 2000Date of Patent: February 12, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Hisao Yamada, Mitsuyuki Tsurumi, Kazunori Nigorikawa
-
Patent number: 6344459Abstract: 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: GrantFiled: June 8, 1999Date of Patent: February 5, 2002Assignee: Warner-Lambert CompanyInventors: Alexander James Bridges, William Alexander Denny, Ellen Myra Dobrusin, Annette Marian Doherty, David William Fry, Dennis Joseph McNamara, Howard Daniel Hollis Showalter, Jeffrey B. Smaill, Hairong Zhou
-
Patent number: 6337332Abstract: Compounds of the structures are useful for treating conditions related to an excess of neuropeptide Y including obesity and circulatory disorders.Type: GrantFiled: August 24, 1999Date of Patent: January 8, 2002Assignee: Pfizer Inc.Inventor: Philip A. Carpino
-
Patent number: 6331543Abstract: 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: September 1, 1999Date of Patent: December 18, 2001Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
-
Patent number: 6329116Abstract: An object of the present invention is to provide a pyrrolo[1,2-a]pyrimidine compound that is useful as a coupler providing excellent hue of a cyan system and sufficient density of formed color. The pyrrolo[1,2-a]pyrimidine compound of the present invention for achieving the object is represented by one of following general formulae (1), (2) and (3).Type: GrantFiled: November 17, 1999Date of Patent: December 11, 2001Assignee: Fuji Photo Film Co., Ltd.Inventors: Hiroshi Sato, Tatsuo Kawabuchi, Mitsuyuki Tsurumi, Tetsunori Matsushita, Hisato Nagase, Kimiatsu Nomura, Yoshihiro Jimbo, Kazunori Nigorikawa
-
Patent number: 6316454Abstract: 6,7-Dimethoxy-4-anilinoquinaozolines of the formula: or pharmaceutically acceptable acid addition salts thereof are disclosed. These novel compounds are useful for inducing apoptosis and preventing metastases of brain tumor cells.Type: GrantFiled: July 26, 1999Date of Patent: November 13, 2001Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Rama Krishna Narla, Xing-Ping Liu
-
Publication number: 20010034351Abstract: The invention relates to compounds of the formula 1 1Type: ApplicationFiled: April 12, 2001Publication date: October 25, 2001Inventors: John Charles Kath, Norma Jacqueline Tom, Zhengyu Liu, Eric David Cox, Joel Morris, Samit Kumar Bhattacharya
-
Patent number: 6291455Abstract: The invention relates to quinazoline derivatives of formula (I) (wherein: R1 represents hydrogen or methoxy; R2 represents methoxy, ethoxy, 2-methoxyethoxy, 3-methoxypropoxy, 2-ethoxyethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, 2-hydroxyethoxy, 3-hydroxypropoxy, 2-(N,N-dimethylamino)ethoxy, 3-(N,N-dimethylamino)propoxy, 2-morpholinoethoxy, 3-morpholinopropoxy, 4-morpholinobutoxy, 2-piperidinoethoxy, 3-piperidinopropoxy, 4-piperidinobutoxy, 2-(piperazin-1-yl)ethoxy, 3-(piperazin-1-yl)propoxy, 4-(piperazin-1-yl)butoxy, 2-(4-methylpiperazin-1-yl)ethoxy, 3-(4methylpiperazin-1-yl)propoxy or 4-(4-methylpiperazin-1-yl)butoxy; the phenyl group bearing (R3)2 is selected from: 2-fluoro-5-hydroxyphenyl, 4-bromo-2-fluorophenyl, 2,4-difluorophenyl, 4-chloro-2-fluorophenyl, 2-fluoro-4-methylphenyl, 2-fluoro-4-methoxyphenyl, 4-bromo-3-hydroxyphenyl, 4-fluoro-3-hydroxyphenyl, 4-chloro-3-hydroxyphenyl, 3-hydroxy-4-methylphenyl, 3-hydroxy-4-methoxyphenyl and 4-cyano-2-fluorophenyl); and salts thereof, processes for their pType: GrantFiled: September 8, 1998Date of Patent: September 18, 2001Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Andrew Peter Thomas, Craig Johnstone, Laurent Francois Andre Hennequin
-
Patent number: 6284764Abstract: 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 with 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: September 4, 2001Assignee: Pfizer Inc.Inventors: John Charles Kath, Norma Jacqueline Tom, Zhengyu Liu, Eric David Cox, Joel Morris, Samit Kumar Bhattacharya
-
Publication number: 20010016588Abstract: Quinazoline compounds and methods for the treatment of cancer and for the treatment of allergic reactions.Type: ApplicationFiled: February 8, 2001Publication date: August 23, 2001Applicant: Hughes InstituteInventors: Fatih M. Uckun, Xing-Ping Liu, Rama Krishna Narla
-
Patent number: 6258820Abstract: Compounds of the formula: wherein: Ra is iodo, (C1-C4)hydroxyalkyl, benzyloxy, OCF3, SCF3, SO3H, SO2F, SO2NR2R3 where R2 is hydrogen or (C1-C4)alkyl and R3 is hydrogen, (C1-C4)alkyl, or phenyl, NR2R4 where R2 is hydrogen or (C1-C4)alkyl and R4 is phenyl; or a group of the formula wherein R5 and R6 are each independently, hydrogen, (C1-C4)alkyl, or (C1-C4) perfluoroalkyl, and R7 is hydrogen, halo, hydroxy, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)hydroxyalkyl, or N(R2)2, where R2 is hydrogen or (C1-C4)alkyl; n is an integer of 1-4; Rb is each, independently, hydrogen, halo, hydroxy, mercapto, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)thioalkyl, (C1-C4)hydroxyalkyl, nitro, cyano, methylenedioxy, ethylenedioxy, COCH3, CF3, OCF3, SCF3, COOH, SO3H, SO2F, phenyl, or phenyl substituted by a group selected from halo, hydroxy, mercapto, (C1-C4)alkyl, (C1-C4) alkoxy, (C1-C4)thioalkyl, (C1-C4)hydroxyalkyl, amino, nitro, cyano, CF3, COOH, SO3H, SO2NR2R3, SO2F where R2 is H or (C1-C4)alkyl andType: GrantFiled: July 20, 1999Date of Patent: July 10, 2001Assignee: Parker Hughes InstituteInventors: Faith M. Uckun, Xing-Ping Liu, Rama Krishna Narla
-
Patent number: 6258951Abstract: The invention relates to quinazoline derivatives of the formula: and salts thereof; processes for their preparation and pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as 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 a number of disease states including cancer and rheumatoid arthritis.Type: GrantFiled: February 9, 2000Date of Patent: July 10, 2001Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
-
Patent number: 6251912Abstract: This invention provides compounds of formula 1 having the structure wherein: X, R1, R2, R3, R4, Z, X, and n are as defined hereinbefore in the specification, which are useful as antineoplastic agents and in the treatment of certain kidney diseases, such as polycystic kidney disease.Type: GrantFiled: July 29, 1998Date of Patent: June 26, 2001Assignee: American Cyanamid CompanyInventors: Allan Wissner, Hwei-Ru Tsou, Bernard D. Johnson, Philip R. Hamann, Nan Zhang
-
Patent number: 6228553Abstract: A pyrrolo[1,2-a]pyrimidine compound providing an excellent color-forming property is provided. Further, a novel cyan color-forming type diazo heat-sensitive recording material having excellent shelf life, image light-resistance and image fixing property is provided. The pyrrolo[1,2-a]pyrimidine compound is represented by following general formula (1). The heat-sensitive recording material comprises a substrate, and on the substrate, a heat-sensitive recording layer containing a diazonium salt compound and a coupler. The coupler contains at least one of pyrrolo[1,2-a]pyrimidine compounds represented by following general formula (1). In the formula, R1 represents an aryl group or the like, R2 represents an alkoxycarbonyl group or the like, R3 and R4 represent an acyl group or the like, and R5 represents a hydrogen atom or the like.Type: GrantFiled: July 8, 1999Date of Patent: May 8, 2001Assignee: Fuji Photo Film Co., Ltd.Inventors: Tetsunori Matsushita, Naoto Yanagihara, Masanobu Takashima, Mitsuyuki Tsurumi
-
Patent number: 6204267Abstract: 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: GrantFiled: May 1, 1998Date of Patent: March 20, 2001Assignee: Sugen, Inc.Inventors: Peng C. Tang, Gerald McMahon, Heinz Weinberger, Bernhard Kutscher, Harald App
-
Patent number: 6197729Abstract: Compounds of formula I where R1 is hydrogen, chlorine, fluorine or methyl, R2 and R3, which may be the same or different from each other, are hydrogen, halogen, cyano, (C1-C4)-alkyl, vinyl, ethynyl, (C1-C4)-alkoxy, (C1-C4)-alkoxy-(C1-C4)-alkyl, fluorovinyl or fluoroethyl, or R2 and R3 together with the linking carbon atoms form a benzo ring, and R4 is (C2-C4)-alkyl, (C2-C4)-alkenyl or (C3-C4)-alkinyl, each of which is substituted by at least two fluorine atoms and optionally substituted by C1-4-alkoxy, cyanomethoxy, (C3-C4)-alkenyloxy or (C3-C4)-alkinyloxy, are useful as pesticides, especially against insects, acarids and fungi. The invention includes a novel process for fluorinating certain pyrimidines.Type: GrantFiled: July 29, 1999Date of Patent: March 6, 2001Assignee: Hoechst Schering AgrevoInventors: Martin Märkl, Wolfgang Schaper, Oswald Ort, Harald Jakobi, Ralf Braun, Gerhard Krautstrunk, Ulrich Sanft, Werner Bonin, Herbert Stark, Sergej Pasenok, Ivan Cabrera
-
Patent number: 6194409Abstract: 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: GrantFiled: October 19, 1999Date of Patent: February 27, 2001Assignee: Akzo Nobel N.V.Inventors: Constant Adriaan Anton van Boeckel, Philippus Johannes Marie van Galen, Johannes Bernardus Maria Rewinkel
-
Patent number: 6184226Abstract: The invention describes compounds of the formula and the pharmaceutically acceptable salts thereof and the pharmaceutically acceptable salts thereof wherein each R2 is independently a noninterfering substituent; m is an integer of 0-4; Z is CH or N; R1 is H, alkyl (1-6C) or arylalkyl optionally substituted on the aryl group with 1-3 substituents independently selected from alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, —SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C); n is 0, 1 or 2; Ar is phenyl, pyridyl, indolyl, or pyrimidyl, each optionally substituted with a group selected from the group consisting of optionally substituted alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C); and R3 is a branched or cyclic alkyl group (5-7C) or is phenyl optionally substituted with 1-2 substiType: GrantFiled: August 28, 1998Date of Patent: February 6, 2001Assignee: Scios Inc.Inventors: Sarvajit Chakravarty, John J. Perumattam, George F. Schreiner, David Y. Liu, John A. Lewicki
-
Patent number: 6184225Abstract: The invention relates to quinazoline derivatives of formula (I) wherein: Z represents —O—, —NH— or —S—; m is an integer from 1 to 5; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluorometlyl, 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—, —NR6—, NR8CO—, —CONR9—SO2NR10— or —NR11SO2—, (wherein R7, R8, R9, R10 and R11 each represents C1-3alkyl, C1-3alkoxyC2-3alkyl); R4 represents a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alType: GrantFiled: August 13, 1998Date of Patent: February 6, 2001Assignee: Zeneca LimitedInventors: Andrew Peter Thomas, Craig Johnstone, Laurent Francois Andre Hennequin
-
Patent number: 6169093Abstract: 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 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: July 7, 1999Date of Patent: January 2, 2001Assignee: Pfizer Inc.Inventor: David Nathan Abraham Fox
-
Patent number: 6153617Abstract: The invention provides compounds of Formula I ##STR1## 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: GrantFiled: March 25, 1999Date of Patent: November 28, 2000Assignee: Warner-Lambert CompanyInventor: Alexander James Bridges
-
Patent number: 6143748Abstract: The present invention is concerned with a process for the preparation of antiviral 1,3-oxathiolane nucleosides comprising an intramolecular glycosylation reaction to produce exclusively the .beta.-diastereomer, and intermediates useful in the process.Type: GrantFiled: September 30, 1997Date of Patent: November 7, 2000Assignee: Glaxo Wellcome Inc.Inventors: Mirna C. Samano, Vicente Samano, Michael David Goodyear
-
Patent number: 6127374Abstract: This invention provides irreversible inhibitors of tyrosine kinases having for formula ##STR1## which compounds are useful for treating cancer, restenosis, atherosclerosis, endometriosis and psoriasis.Type: GrantFiled: March 25, 1999Date of Patent: October 3, 2000Assignee: Warner-Lambert CompanyInventor: Alexander James Bridges
-
Patent number: 6126917Abstract: A radiolabeled compound of a formula: ##STR1## is described. R1 and R2 are each independently selected from the group consisting of hydrogen, alkyl, hydroxy, alkoxy, halo, haloalkyl, carboxy, carbalkoxy and salts thereof; and A, B, C and D are each independently selected from the group consisting of a hydrogen and an electron withdrawing group, provided that at least one of A, B, C and D is [18]fluorine.Type: GrantFiled: June 1, 1999Date of Patent: October 3, 2000Assignee: Hadasit Medical Research Services and Development Ltd.Inventors: Eyal Mishani, Thomas Bonasera, Giuseppina Ortu, Yulia Rozen, Aviv Gazit, Alexander Levitzki
-
Patent number: 6071921Abstract: The invention relates to quinazoline derivatives of the formula: ##STR1## [wherein: Y.sup.1 represents --O--, --S--, --CH.sub.2 --, --SO--, --SO.sub.2 --, --NR.sup.5 CO--, --CONR.sup.6 --, --SO.sub.2 NR.sup.7 --, --NR.sup.8 SO.sub.2 -- or --NR.sup.9 -- (wherein R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 each independently represents hydrogen, alkyl or alkoxyalkyl);R.sup.1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, alkyl, alkoxy, alkylthio, amino or alkylamino.R.sup.2 represents hydrogen, hydroxy, halogeno, alkyl, alkoxy, trifluoromethyl, cyano, amino or nitro;m is an integer from 1 to 5;R.sup.3 represents hydroxy, halogeno, alky, alkoxy, alkanoyloxy, trifluoromethyl, cyano, amino or nitro;R.sup.Type: GrantFiled: December 2, 1998Date of Patent: June 6, 2000Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
-
Patent number: 6057326Abstract: Novel and known bicyclic 4-aralkylaminopyrimidine derivatives of formula (I) wherein A is a benzene or imidazole ring; B is a benzene, tetralin, indane or 2-oxindole ring R is (C.sub.1 -C.sub.4)perfluoroalkyl, phenyl, phenyl-(C.sub.1 -C.sub.4)alkyl, hydroxy-(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy-(C.sub.1 -C.sub.4)alkyl, (C.sub.2 -C.sub.4)acyloxy-(C.sub.1 -C.sub.4)alkyl, halobenzoyloxy-(C.sub.1 -C.sub.4)alkyl, carboxy, carbamoyl, (C.sub.1 -C.sub.4)alkoxycarbonyl, cyano, (C.sub.1 -C.sub.4)alkylcarbonyl, carboxy-(C.sub.1 -C.sub.4)alkyl, carbamoyl-(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxycarbonyl-(C.sub.1 -C.sub.4)alkyl, halo-(C.sub.1 -C.sub.4)alkyl, amino-(C.sub.1 -C.sub.4)alkyl, mono- or di-(C.sub.1 -C.sub.4)alkylamino-(C.sub.1 -C.sub.4)alkyl, sulfo-(C.sub.1 -C.sub.4)alkyl or sulfamido-(C.sub.1 -C.sub.4)alkyl; each of R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen or --NR.sub.5 R.sub.6 in which each of R.sub.Type: GrantFiled: February 6, 1998Date of Patent: May 2, 2000Assignee: Pharmacia & Upjohn S.p.AInventors: Maria Gabriella Brasca, Dario Ballinari, Antonio Longo, Franco Buzzetti
-
Patent number: 5990116Abstract: The invention concerns compounds of formula I ##STR1## wherein the substituents have various meanings, and their use in the prevention or treatment of inflammatory and proliferative skin diseases and cancer.Type: GrantFiled: September 15, 1997Date of Patent: November 23, 1999Assignee: Novartis AGInventor: Peter Nussbaumer
-
Patent number: 5977110Abstract: Substituted cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, serotonergic, antipsychotic, and anxiolytic agents.Type: GrantFiled: March 20, 1998Date of Patent: November 2, 1999Assignee: Warner-Lambert CompanyInventors: Thomas R. Belliotti, Suzanne R. Kesten, Thomas A. Pugsley, David J. Wustrow
-
Patent number: 5962458Abstract: The invention relates to quinazoline derivatives of the formula: ##STR1## ?wherein: Y.sup.1 represents --O--, --S--, --CH.sub.2 --, --SO--, --SO.sub.2 --, --NR.sup.5 CO--, --CONR.sup.6 -, --SO.sub.2 NR.sup.7 -, --NR.sup.8 SO.sub.2 -- or --NR.sup.9 - (wherein R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 each independently represents hydrogen, alkyl or alkoxyalkyl);R.sup.1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, alkyl, alkoxy, alkylthio, amino or alkylamino.R.sup.2 represents hydrogen, hydroxy, halogeno, alkyl, alkoxy, trifluoromethyl, cyano, amino or nitro;m is an integer from 1 to 5;R.sup.3 represents hydroxy, halogeno, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, cyano, amino or nitro;R.sup.Type: GrantFiled: December 17, 1996Date of Patent: October 5, 1999Assignees: Zeneca Limited, Zeneca Pharma S.A.,Inventors: Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin, Andrew Peter Thomas
-
Patent number: 5955464Abstract: The invention concerns 4-anilinoquinazoline derivatives of the formula I ##STR1## wherein m is 1 or 2; each R.sup.1 includes hydrogen, halogeno, (1-4C)alkyl and (1-4C)alkoxy;n is 1, 2 or 3;each R.sup.2 includes hydrogen, hydroxy, halogeno and (1-4C)alkyl; and Ar is a 5- or 9-membered nitrogen-linked heteroaryl moiety containing up to four nitrogen heteroatoms, or Ar is a 5-, 6-, 9- or 10-membered nitrogen-linked unsaturated heterocyclic moiety containing up to three nitrogen heteroatoms which bears one or two substituents selected from oxo and thioxo such as 2-oxo-4-imidazolin-1-yl;or a pharmaceutically-acceptable salt thereof;processes for their preparation, pharmaceutical compositions containing them, and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of proliferative disease such as cancer.Type: GrantFiled: May 22, 1997Date of Patent: September 21, 1999Assignee: Zeneca LimitedInventor: Andrew John Barker
-
Patent number: 5952333Abstract: The invention concerns the quinazoline derivative 6-(2-methoxyethylamino)-7-methoxy-4-(3'-methylanilino)quinazoline, or a pharmaceutically-acceptable salt thereof, processes for its preparation, pharmaceutical compositions containing the compound and the use of the receptor tyrosine kinase inhibitory properties of the compound in the treatments of proliferative disease such as cancer.Type: GrantFiled: September 26, 1997Date of Patent: September 14, 1999Assignee: Zeneca LimitedInventor: Andrew John Barker
-
Patent number: 5942514Abstract: The invention concerns quinazoline derivatives of formula wherein n is 1, 2 or 3 and each R.sup.2 is independently halogeno; and R.sup.1 is 1-4C)alkoxy-(2-4C)alkylamino; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them, and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of proliferative disease such as cancer.Type: GrantFiled: September 26, 1997Date of Patent: August 24, 1999Assignee: Zeneca LimitedInventor: Andrew John Barker
-
Patent number: 5939421Abstract: Compounds having utility as anti-inflammatory agents in general and, more specifically, for the prevention and/or treatment of immunoinflammatory and autoimmune diseases are disclosed. The compounds are quinazoline-containing compounds. Methods are also disclosed for preventing and/or treating inflammatory conditions by administering to an animal in need thereof an effective amount of a compound of this invention, preferably in the form of a pharmaceutical composition.Type: GrantFiled: July 1, 1997Date of Patent: August 17, 1999Assignee: Signal Pharmaceuticals, Inc.Inventors: Moorthy S. S. Palanki, Mark J. Suto