Carbocyclic Ring Bonded Directly To A Ring Carbon Of The Quinazoline Ring System Patents (Class 514/266.31)
-
Patent number: 7081461Abstract: 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: GrantFiled: September 18, 2000Date of Patent: July 25, 2006Assignee: AstraZeneca ABInventors: Andrew Austen Mortlock, Nicholas John Keen
-
Patent number: 7060706Abstract: Quinazolinones of formula (I) in which R, R1, R2, R3, R4, Y, n and m have the meaning indicated in Patent claim 1, and their salts or solvates as glycoprotein IbIX antagonistsType: GrantFiled: September 13, 2000Date of Patent: June 13, 2006Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Werner Mederski, Ralf Devant, Gerhard Barnickel, Sabine Bernotat-Danielowski, Guido Melzer, Bertram Cezanne, Daljit Dhanoa, Bao-Ping Zhao, James Rinker, Mark Player, Richard Soll
-
Patent number: 7053216Abstract: Compounds of formula 1 modulate the activity of Rho C: wherein R1 is H, lower alkyl, aralkyl, aryl-lower alkenyl, or —(CH2)nCH(R7)NR8R9, where n is 0–6 inclusive, R7 is H, lower alkyl, aryl, or aralkyl, R8 is H, lower alkyl, cyclo-alkyl, aryl, or aralkyl, and R9 is R, RCO—, ROCO—, or RNHCO—, where R is lower alkyl, cycloalkyl, aryl, or aralkyl, wherein aryl and aralkyl are substituted with 0–3 substituents selected from the group consisting of lower alkyl, halo, nitro, —OH, trifluoromethyl, or lower alkoxy; R2 is lower alkyl, aryl, aralkyl, or —(CHR10)m—(CO)—R11, wherein m is 0–4, R10 is H or lower alkyl, and R11 is lower alkyl, cycloalkyl, aryl, or aralkyl, wherein aryl and aralkyl are substituted with 0–3 substituents selected from the group consisting of lower alkyl, halo, nitro, —OH, trifluoromethyl, or lower alkoxy; R3, R4, R5, and R6, are each independently H, lower alkyl, halo, nitro, OH, lower alkoxy, NH2, lower alkylamino, di(lower alkylamino), trifluoromethyl, or SH; or a pharmaceutically acceType: GrantFiled: November 19, 2002Date of Patent: May 30, 2006Assignee: Iconix Pharmaceuticals, Inc.Inventors: Dongxu Sun, Edward L. Perkins, Stuart Tugendreich
-
Patent number: 6962922Abstract: A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W1 and W2 form together a group of formula —N?X4—W3— as defined in the description, X1, X2 and X3 represent N or C optionally substituted, n is 0 to 8, Z represents —CR12R13, wherein R12 and R13 are as defined in the description, A represents a ring system, the groups R2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.Type: GrantFiled: October 11, 2002Date of Patent: November 8, 2005Assignee: Warner-Lambert Company LLCInventors: Bernard Gaudilliere, Henri Jacobelli, Joseph Armand Picard, Michael William Wilson
-
Patent number: 6890930Abstract: Quinazolinones of formula (I) in which R, R1, R2, R3, R4, Y, Z, and m have the meaning indicated in patent claim 1, and their salts or solvates as glycoprotein IbIX antagonists.Type: GrantFiled: September 13, 2000Date of Patent: May 10, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Werner Mederski, Maria Devant, Gerhard Barnickel, Sabine Bernotat-Danielowski, Guido Melzer, Bertram Cezane, Dalijit Dhanoa, Bao-Ping Zhoa, James Rinker, Mark Player, Richard Soll, Ralf Devant
-
Publication number: 20040254203Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.Type: ApplicationFiled: July 20, 2004Publication date: December 16, 2004Applicant: Cytokinetics, Inc.Inventors: Jeffrey T. Finer, Gustave Bergnes, Whitney W. Smith, John C. Chabala, Bainian Feng
-
Patent number: 6831085Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.Type: GrantFiled: November 28, 2000Date of Patent: December 14, 2004Assignee: Cytokinetics, Inc.Inventors: Gustave Bergnes, Whitney W. Smith, John C. Chabala
-
Publication number: 20040192621Abstract: The present invention relates to an anti-tumor agent containing a tubulin polymerization-inhibitory active substance and an anti-inflammatory active substance. The present invention also relates to an anti-tumor pharmaceutical preparation containing one or more tubulin polymerization-inhibitory active substance and/or anti-inflammatory active substance, which can be individually combined with one or more additional tubulin polymerization-inhibitory active substance and/or anti-inflammatory active substance. The present invention also relates to methods and therapeutic regimens for administering the same to a subject in need thereof.Type: ApplicationFiled: December 24, 2003Publication date: September 30, 2004Applicant: AJINOMOTO CO., INCInventors: Yukio Nihei, Yoshihiro Morinaga, Manabu Suzuki, Yasuyo Suga
-
Publication number: 20040180912Abstract: Use of compound of formula (I), wherein, is, or, and wherein the symbols are as defined, or a pharmaceutically-acceptable and-cleavable ester, or acid addition salt thereof, for the preparation of a medicament for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.Type: ApplicationFiled: December 12, 2003Publication date: September 16, 2004Inventors: Rene Beerli, Ruben Alberto Tommasi, Sven Weiler, Leo Widler
-
Publication number: 20040162299Abstract: The invention relates to novel quinazolines and heterocycles which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating, preventing or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, myoclonus, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition and learning enhancers.Type: ApplicationFiled: February 6, 2004Publication date: August 19, 2004Applicant: Euro-Celtique, S.A.Inventors: Ravi Upasani, Sui X. Cai, Nancy C. Lan, Yan Wang, George Field, David B. Fick
-
Publication number: 20040152696Abstract: This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel 2-substituted bicyclic benzoheterocyclic compounds of Formula I: 1Type: ApplicationFiled: July 29, 2003Publication date: August 5, 2004Applicant: Euro-Celtique S.A.Inventors: Qun Sun, Donald J. Kyle, Samuel F. Victory
-
Patent number: 6759410Abstract: The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolines of formula (1), or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: May 10, 2002Date of Patent: July 6, 2004Assignee: SmithLine Beecham CorporationInventors: Jerry L. Adams, Michael J. Bower, Ralph Hall, Don Edgar Griswold, David C. Underwood
-
Publication number: 20040048882Abstract: This invention comprises the novel compounds of formula (I) wherein r, s, t, Y1—Y2, R1, R2, R3, R4, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: March 24, 2003Publication date: March 11, 2004Inventors: Patrick Rene Angibaud, Marc Gaston Venet, Ashis Kumar Saha, Laurence Anne Mevellec
-
Publication number: 20030220227Abstract: Novel quinazoline derivatives possessing activity as estrogen receptor beta (ER&bgr;) modulators are provided which have the general formula I 1Type: ApplicationFiled: March 13, 2003Publication date: November 27, 2003Inventors: Timur Gungor, James R. Corte
-
Patent number: 6645971Abstract: A compound given by general formula (1): [wherein T represents oxygen or sulfur atom, Y represents alkyl, cycloalkyl group, etc., ring W represents benzene ring, etc., R1 and R2 represent independently hydrogen atom, lower alkyl group, etc., and R3 represents hydrogen atom, alkyl group, etc. Z represents a group given by formula: {wherein A1 and A2 represent independently hydrogen atom, alkyl group, etc. and G represents straight chain alkylene having 1-6 of the carbon number, etc.} or a group given by formula: {wherein n represents 0, 1 or 2, ring E represents 4-8 membered saturated heterocyclic ring containing nitrogen atom(s), and A3 represents hydrogen atom, alkyl group, etc.}], its prodrug or pharmaceutically acceptable salt thereof is an antagonist against muscarinic receptor that is useful as anticholinergic medicaments, and therefore it is useful as pollakiuria or urinary incontinence remedy.Type: GrantFiled: April 10, 2001Date of Patent: November 11, 2003Assignee: Sumitomo Pharmaceuticals Company LimitedInventors: Masami Muraoka, Kazuki Matsui, Koji Morishita, Naohito Ohashi
-
Patent number: 6630479Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.Type: GrantFiled: November 28, 2000Date of Patent: October 7, 2003Assignee: Cytokinetics, Inc.Inventors: Jeffrey T. Finer, Gustave Bergnes, Whitney W. Smith, John C. Chabala, Bainian Feng
-
Publication number: 20030186925Abstract: The present invention is concerned with combinations of a farnesyl transferase inhibitor and an anti-tumor nucleoside derivative for inhibiting the growth of tumor cells and useful in the treatment of cancer.Type: ApplicationFiled: August 28, 2002Publication date: October 2, 2003Inventors: Peter Albert Palmer, Ivan David Horak
-
Publication number: 20030181473Abstract: The present invention is concerned with combinations of a farnesyl transferase inhibitor and a taxane compound for inhibiting the growth of tumor cells and useful in the treatment of cancer.Type: ApplicationFiled: August 28, 2002Publication date: September 25, 2003Inventors: Peter Albert Palmer, Ivan David Horak
-
Publication number: 20030171387Abstract: Compounds of formula 1 modulate the activity of Rho C: 1Type: ApplicationFiled: November 19, 2002Publication date: September 11, 2003Inventors: Dongxu Sun, Edward L. Perkins, Stuart Tugendreich
-
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
-
Publication number: 20030130293Abstract: This invention generally relates to compositions and methods for cancer treatment and, in particular, to compositions able to interact (e.g., bind to) with MUC1 growth factor receptor or its ligands, and methods for treating the same. The invention also relates to assays or use of such compositions for the treatment of patients susceptible to or exhibiting symptoms characteristic of cancer or tumorigenesis. Other compositions of the present invention useful for the treatment or prevention of cancer or tumorigenesis include homologs, analogs, derivatives, enantiomers or functional equivalents. The present compositions can also be packaged in kits in some cases.Type: ApplicationFiled: September 5, 2002Publication date: July 10, 2003Inventor: Cynthia C. Bamdad
-
Publication number: 20030125326Abstract: The present invention is concerned with combinations of two or more farnesyl transferase inhibitors for inhibiting the growth of tumour cells and useful in the treatment of cancer.Type: ApplicationFiled: August 28, 2002Publication date: July 3, 2003Inventor: Mary Ellen Margaret Rybak
-
Publication number: 20030100553Abstract: The present invention is concerned with combinations of a farnesyl transferase inhibitor and a camptothecin compound for inhibiting the growth of tumor cells and useful in the treatment of cancer.Type: ApplicationFiled: August 28, 2002Publication date: May 29, 2003Inventors: Peter Albert Palmer, Ivan David Horak
-
Patent number: 6562831Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.Type: GrantFiled: November 28, 2000Date of Patent: May 13, 2003Assignee: Cytokinetics, Inc.Inventors: Jeffrey T. Finer, Gustave Bergnes, Whitney W. Smith, John C. Chabala, Bainian Feng