Chalcogen Bonded Directly At 2-position Patents (Class 544/286)
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Patent number: 7405030Abstract: An optical recording medium containing one or more compounds selected from imide compounds having a metallocene residue in a recording layer and an imide compound represented by a general formula (1): wherein a ring AR represents a substituted or unsubstituted aromatic ring residue or a residue formed by combining two or more aromatic ring residues via one or more linking groups; n represents the number of imide groups bonded to the ring AR; Am represents any one of substituents A1 to An bonded to a nitrogen atom of each imide group; and m represents an integer of from 1 to n, with the proviso that at least one substituent selected from the group consisting of A1 to An is one having at least one substituted or unsubstituted metallocene residue.Type: GrantFiled: July 10, 2007Date of Patent: July 29, 2008Assignee: Mitsui Chemicals, Inc.Inventors: Akira Ogiso, Hiroyoshi Shiozaki, Tsutomu Ishida, Hisashi Tsukahara, Tsutami Misawa, Koji Inoue, Tadashi Koike, Keiji Ueno, Yuji Inatomi, Ryousuke Nara
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Publication number: 20080176830Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: ApplicationFiled: April 13, 2006Publication date: July 24, 2008Inventors: Nicholas D. Adams, Michael Gerard Darcy, Dashyant Dhanak, Kevin J. Duffy, Duke M. Fitch, Steven David Knight, Kenneth Allen Newlander, Antony N. Shaw
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Publication number: 20080167329Abstract: The present invention is directed to quinazolinone compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.Type: ApplicationFiled: March 8, 2006Publication date: July 10, 2008Inventors: James C. Barrow, Rowena V. Cube, Phung Le Ngo, Kenneth E. Rittle, Zhiqiang Yang, Steven D. Young
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Patent number: 7368453Abstract: A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the formula IA and IB.Type: GrantFiled: November 19, 2004Date of Patent: May 6, 2008Assignees: Chiron Corporation, Glaxo SmithKlineInventors: Rustum S. Boyce, Jason D. Speake, James Phillips
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Patent number: 7358239Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 7329665Abstract: An optically active form of the quinazolinone derivatives represented by the general formula (1): [wherein Y represents a phenyl group or C2-C7 alkyl group; E represents —CH? or nitrogen atom; and R represents a C1-C4 alkyl group and so on], or pharmaceutically acceptable salts thereof, has a selective antagonism for the M3 muscarinic receptor and depressant action on the frequency of rhythmic bladder contractions, and it is useful for the treatment of pollakiuria and urinary incontinence.Type: GrantFiled: August 2, 2002Date of Patent: February 12, 2008Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Masami Muraoka, Kazuki Matsui, Takaaki Yamamoto, Koji Morishita, Masatoshi Yuri, Seiji Katayama, Naohito Ohashi
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Patent number: 7312211Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases.Type: GrantFiled: August 26, 2004Date of Patent: December 25, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
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Patent number: 7259260Abstract: An optical recording medium containing one or more compounds selected from imide compounds having a metallocene residue in a recording layer and an imide compound represented by a general formula (1): wherein a ring AR represents a substituted or unsubstituted aromatic ring residue or a residue formed by combining two or more aromatic ring residues via one or more linking groups; n represents the number of imide groups bonded to the ring AR; Am represents any one of substituents A1 to An bonded to a nitrogen atom of each imide group; and m represents an integer of from 1 to n, with the proviso that at least one substituent selected from the group consisting of A1 to An is one having at least one substituted or unsubstituted metallocene residue.Type: GrantFiled: October 22, 2002Date of Patent: August 21, 2007Assignee: Mitsui Chemicals, Inc.Inventors: Akira Ogiso, Hiroyoshi Shiozaki, Tsutomu Ishida
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Patent number: 7230001Abstract: The present invention relates to compounds of general formula R—Z1—Z2—Z3—R1, ??(I) wherein R, R1 and Z1 to Z3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: GrantFiled: October 24, 2000Date of Patent: June 12, 2007Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Henri Doods, Gerhard Hallermayer, Eckhart Bauer
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Patent number: 7196087Abstract: Compounds of the formula I: and pharmaceutically acceptable salts thereof, wherein X is CH or N, Y is C or S, Z is —(CRaRb)r— or —SO2—, A is —NR3— or —O—, R2 is optionally substituted aryl or optionally substituted heteroaryl, n is 1 or 2, m is 1 when Y is C and m is 2 when Y is S, and p, q, r, R1, R3, R4, R5, R6, R7, R8, R9, R10, Ra and Rb are as defined herein. The compounds are useful in the treatment of 5-HT6 and 5-HT2A mediated diseases.Type: GrantFiled: January 14, 2005Date of Patent: March 27, 2007Assignee: Roche Palo Alto LLCInventors: Nancy Elisabeth Krauss, Meng Sui, Shu-Hai Zhao
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Patent number: 7176312Abstract: 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: GrantFiled: October 12, 2002Date of Patent: February 13, 2007Assignees: The Scripps Research Institute, IRM LLCInventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
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Patent number: 7161002Abstract: The present invention provides novel quinazolinone compositions of matter comprising enantiomerically pure compound represented by Formula I: or a pharmaceutically acceptable salt thereof, having a detectable amount of one or more starting material and/or reagent used in the synthesis thereof.Type: GrantFiled: October 20, 2005Date of Patent: January 9, 2007Assignees: Cytokinetics, Inc., SmithKline Beecham CorporationInventors: Gustave Bergnes, Edward Ha, George Yiannikourous, Panos Kalaritis, Brandon E. Yonce, Kurt Alan Welday, Jr.
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Patent number: 7094784Abstract: 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 nociceptin receptor inhibitors useful in theType: GrantFiled: January 21, 2004Date of Patent: August 22, 2006Assignee: 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: 7087612Abstract: This invention relates to 3H-quinazolin-4-one derivatives as defined in the specification and claims, to a process for their preparation, to pharmaceutical compositions comprising them and to their use as selective monoamine oxidase B inhibitors.Type: GrantFiled: December 13, 2003Date of Patent: August 8, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Patent number: 7060825Abstract: 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: GrantFiled: July 25, 2003Date of Patent: June 13, 2006Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Ye Wu, Harry Kochat
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Patent number: 7053098Abstract: Novel substituted quinazoline compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: GrantFiled: November 21, 2000Date of Patent: May 30, 2006Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Michael J. Bower, Jeffrey C. Boehm, Don Edgar Griswold, David C. Underwood
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Patent number: 7053099Abstract: Novel substituted quinazoline compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: GrantFiled: November 21, 2000Date of Patent: May 30, 2006Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Michael J. Bower, Ralph Hall, Don Edgar Griswold, David C. Underwood
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Patent number: 7049438Abstract: 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 diseaseType: GrantFiled: June 1, 2001Date of Patent: May 23, 2006Assignee: AstraZeneca ABInventors: Laurent François André Hennequin, Patrick Ple
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Patent number: 7037880Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.Type: GrantFiled: August 8, 2002Date of Patent: May 2, 2006Assignee: Nissan Chemical Industries, Ltd.Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
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Patent number: 6982270Abstract: Substituted quinazolinone compounds of formula (I) and compositions thereof for use in therapy as CSBP/p38 kinase inhibitors.Type: GrantFiled: November 21, 2000Date of Patent: January 3, 2006Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Michael J. Bower, Jeffrey C. Boehm, Don Edgar Griswold, David C. Underwood
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Patent number: 6949541Abstract: The present invention relates to substituted piperidines of general formula wherein A1, A2, R, R1 and R2 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: GrantFiled: December 22, 2000Date of Patent: September 27, 2005Assignee: Boehringer Ingelheim Pharma KGInventors: Klaus Rudolf, Henri Doods, Eckhart Bauer, Rudolf Hurnaus, Wolfgang Eberlein, Alexander Dreyer, Stephan Georg Mueller
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Patent number: 6949643Abstract: The invention provides certain thiazolopyrimidine compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof: in which: A is a group of formula (a) or (b): processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapyType: GrantFiled: April 12, 2002Date of Patent: September 27, 2005Assignee: AstraZeneca ABInventor: Roger Bonnert
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Patent number: 6936606Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases.Type: GrantFiled: September 27, 2002Date of Patent: August 30, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel
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Patent number: 6900222Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is aType: GrantFiled: May 23, 2000Date of Patent: May 31, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Publication number: 20040209905Abstract: An object of the present invention is to provide compounds which have antitumor activity and do not change cytomorphosis.Type: ApplicationFiled: May 10, 2004Publication date: October 21, 2004Applicant: KIRIN BEER KABUSHIKI KAISHAInventors: Kazuo Kubo, Yasunari Fujiwara, Toshiyuki Isoe
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Patent number: 6806274Abstract: 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: GrantFiled: January 7, 2002Date of Patent: October 19, 2004Assignee: AstraZeneca UK LimitedInventors: Graham C Crawley, Laurent F A Hennequin, Darren McKerrecher, Patrick Ple, Jeffrey Philip Poyser, Christine M P Lambert
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Publication number: 20040198724Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.Type: ApplicationFiled: December 23, 2003Publication date: October 7, 2004Applicant: ICAgen, Inc.Inventors: Grant A. McNaughton-Smith, James B. Thomas, George S. Amato
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Patent number: 6800626Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention relates to compounds having the formula: or pharmaceutically acceptable salts thereof, wherein R, R1, Q1, Q2, X, Y, Z, A, and n are as described in the specification. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: December 20, 2002Date of Patent: October 5, 2004Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Guy Bemis, John Cochran
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Publication number: 20040186116Abstract: The present invention relates to compounds that inhibit phosphatases, compositions thereof, and methods of using those compounds and compositions for treating diseases.Type: ApplicationFiled: December 31, 2003Publication date: September 23, 2004Inventors: Jeffrey O. Saunders, Gregory F. Miknis, Alexandre J. Buckmelter, Kevin W. Hunt, James F. Blake, Guy P.A. Vigers, Xicheng Sun
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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
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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
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Publication number: 20040157865Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to naphthol, quinoline and isoquinoline-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.Type: ApplicationFiled: July 10, 2003Publication date: August 12, 2004Inventors: Ellen Codd, Scott L. Dax, Michele Jetter, Mark McDonnell, James J. McNally, Mark Youngman
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Publication number: 20040142950Abstract: This invention provides compounds of Formula I 1Type: ApplicationFiled: December 18, 2003Publication date: July 22, 2004Inventors: Amy Mae Bunker, Joseph Armand Picard
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Publication number: 20040142951Abstract: This invention relates to 3H-quinazolin-4-one derivatives as defined in the specification and claims, to a process for their preparation, to pharmaceutical compositions comprising them and to their use as selective monoamine oxidase B inhibitors.Type: ApplicationFiled: December 13, 2003Publication date: July 22, 2004Inventors: Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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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
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Publication number: 20040067969Abstract: The present invention provides intermediates, synthetic methods and novel quinazolinone compositions of matter.Type: ApplicationFiled: February 14, 2003Publication date: April 8, 2004Inventors: Gustave Bergnes, Edward Ha, George Yiannikouros, Panos Kalaritis, Brandon E. Yonce, Kurt Alan Welday
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Publication number: 20040067968Abstract: This invention comprises the novel compounds of formula (I): 1Type: ApplicationFiled: June 26, 2003Publication date: April 8, 2004Inventors: Patrick Rene Angibaud, Marc Gaston Venet, Virginie Sophie Poncelet
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Publication number: 20040063734Abstract: The present invention relates to quinazolinone compounds of formula (I): 1Type: ApplicationFiled: July 31, 2003Publication date: April 1, 2004Inventor: Jeffrey Corbett
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Publication number: 20040063944Abstract: This invention comprises the novel compounds of formula (I) 1Type: ApplicationFiled: June 26, 2003Publication date: April 1, 2004Inventors: Patrick Rene Angibaud, Marc Gaston Venet
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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
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Publication number: 20030232846Abstract: This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors.Type: ApplicationFiled: June 10, 2002Publication date: December 18, 2003Inventors: Julian M. C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Binch
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Publication number: 20030220355Abstract: A compound selected from those of formula (I): 1Type: ApplicationFiled: April 16, 2003Publication date: November 27, 2003Inventors: Bernard Gaudilliere, Henry Jacobelli, Catherine Kostlan, Jie Jack Li, Wen-Song Yue
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Patent number: 6653300Abstract: This invention describes novel pyrazole compounds of formula I′: wherein Q′ is —O—, —C(R6′)2—, 1,2-cyclopropanediyl, 1,2-cyclobutanediyl, or 1,3-cyclopropanediyl, and 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 independently selected from T—R3 or L—Z—R3, or 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, Julian Golec, Jeremy Green, David Kay, Ronald Knegtel, Andrew Miller, Ronald Tomlison, Pan Li
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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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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
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Patent number: 6600043Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: December 27, 2000Date of Patent: July 29, 2003Assignee: BASF AktiengesellschaftInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Müller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Publication number: 20030092722Abstract: The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I: 1Type: ApplicationFiled: June 11, 2002Publication date: May 15, 2003Inventors: Jeffrey W. Corbett, Soo S. Ko
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Patent number: 6555686Abstract: This invention relates generally to the asymmetric synthesis of quinazolin-2-ones that are useful as inhibitors of HIV reverse transcriptase. The synthesis is accomplished through the chiral ligand mediated addition of cyclopropylacetylide.Type: GrantFiled: July 20, 2001Date of Patent: April 29, 2003Assignee: Bristol-Myers Squibb PharmaInventors: Rodney L. Parsons, Roberta L. Dorow, Akin H. Davulcu, Joseph M. Fortunak, Gregory D. Harris, Goss S. Kauffman, William A. Nugent, Lilian A. Radesca
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Patent number: 6552015Abstract: The present invention is directed to a compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, Y, U, W, k, A, E, V, R4 and R5 are as defined herein, pharmaceutical compositions thereof, and methods of use thereof in the inhibition of serotonin reuptake, the inhibition of the binding of 5-HT2A serotonin receptors and the treatment of diseases, conditions or disorders of the central nervous system. Further, the present invention is also directed to methods for the preparation of compounds of formula (I) and intermediates useful therefor.Type: GrantFiled: August 1, 2001Date of Patent: April 22, 2003Assignee: Pfizer Inc.Inventors: Anton Franz Joseph Fliri, Todd William Butler, Randall James Gallaschun
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Patent number: 6528508Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention relates to compounds having the formula: or pharmaceutically acceptable salts thereof, wherein R, R1, Q1, Q2, X, Y, Z, A, and n are as described in the specification. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: December 11, 2000Date of Patent: March 4, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Guy Bemis, John Cochran