Plural Ring Nitrogens In The Tricyclo Ring System Patents (Class 544/34)
  • Publication number: 20150031652
    Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
    Type: Application
    Filed: August 1, 2014
    Publication date: January 29, 2015
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
  • Publication number: 20140213581
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A5, A6, A8, R1, R2, R3, R7, X, Y, n and o of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
    Type: Application
    Filed: January 28, 2014
    Publication date: July 31, 2014
    Inventors: Ryan WHITE, Jennifer R. ALLEN, Oleg EPSTEIN, Fang-Tsao HONG, Zihao HUA, Jason Brooks HUMAN, Patricia LOPEZ, Philip R. OLIVIERI, Karina ROMERO, Laurie SCHENKEL, John STELLWAGEN, Nuria A. TAMAYO, Xiao Mei ZHENG
  • Publication number: 20140206663
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    Inventors: Jianfei Wang, Eric C. Breinlinger, Martine Barth, Michael M. Friedman, Fabrice Guillier, Maria A. Argiriadi, Jeremy Edmunds, Dominique Potin, Adrian D. Hobson, Wentao Wu, Dominique Bonafoux, Didier Thomas, Dawn M. George, Linlin Dai, Yang Zhang
  • Publication number: 20140200344
    Abstract: Novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities are provided. A tricyclic heterocyclic compound represented by the formula (Ia): wherein the rings Aa and Ba, Xa, Ya, R1a, R2a, R3a, L1a L2a, L3a and na are as defined in the description.
    Type: Application
    Filed: August 10, 2012
    Publication date: July 17, 2014
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Keishi Hayashi, Tsuneo Watanabe, Koji Toyama, Junji Kamon, Masataka Minami, Miyuki Uni, Mariko Nasu
  • Publication number: 20140171417
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: Mahbub AHMED, Alexander ASHALL-KELLY, Louisa GUERITZ, Jeffrey MCKENNA, Joseph MCKENNA, Simon MUTTON, Rakesh PARMAR, Jon SHEPHERD, Paul WRIGHT
  • Publication number: 20140044789
    Abstract: This invention provides melanin nanoshells and their use for protection against radiation, particularly ionizing radiation, and electronic pulses, and methods of making materials comprising melanin nanoshells.
    Type: Application
    Filed: October 22, 2013
    Publication date: February 13, 2014
    Applicant: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Ekaterina Dadachova, Arturo Casadevall
  • Publication number: 20140045687
    Abstract: The present invention relates to the use of dithiine-dicarboximide compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi and seed coated with at least one such compound. The invention also relates to novel dithiine-dicarboximides, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound.
    Type: Application
    Filed: April 10, 2012
    Publication date: February 13, 2014
    Applicant: BASF SE
    Inventors: Wassilios Grammenos, Nadege Boudet, Richard Riggs, Jochen Dietz, Egon Haden, Marcus Fehr
  • Publication number: 20130315825
    Abstract: Derivatives of phenothiazine, phenoxazine, and phenazine compounds and their use as ?-synuclein ligands are described. Also described are methods of using these compounds and their radiolabeled analogs for the detection, monitoring, and treatment of synucleinopathies, including Parkinson's disease.
    Type: Application
    Filed: May 3, 2013
    Publication date: November 28, 2013
    Applicant: Washington University
    Inventors: Zhude Tu, Robert Mach, Lihai Yu, Paul Kotzbauer
  • Publication number: 20130274239
    Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
    Type: Application
    Filed: May 8, 2013
    Publication date: October 17, 2013
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. A. Kiryanov
  • Publication number: 20120294808
    Abstract: A method of imaging using selective fluorescent emitters and compositions for imaging are described. The method can include contacting a specimen with a composition comprising at least one selective fluorescent emitter of Formulas I through IX and irradiating the specimen with an excitation wavelength. The fluorescence emitted by the selective fluorescent emitter can be detected to generate an image. Formulas I through IX are: wherein: R1=OR4 or NR3R4; R2=OR4, NR3R4, Cl, F or H; R3=H, CH3, C2H5, C3H7 or C4H9; R4=H, CH3, C2H5, C3H7 or C4H9; R5=H or CH2(CH2)nNR3R4; R6=H or CH2(CH2)nNR3R4; R7=OR4, NR3R4, Cl, F or H; R8=N-methylpyridinium or N-methyl-1,2,3,6-tetrahydropyridine; and n=1, 2 or 3.
    Type: Application
    Filed: November 9, 2010
    Publication date: November 22, 2012
    Applicant: UNIVERSITY OF MIAMI
    Inventor: James N. Wilson
  • Publication number: 20120122835
    Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
    Type: Application
    Filed: January 18, 2012
    Publication date: May 17, 2012
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
  • Patent number: 8114595
    Abstract: The present invention relates to methods and reagents for modifying the emission of light from labeled nucleic acids for the purpose of real time detection, analysis, and quantitation of nucleic acid sequences, e.g., using singly labeled probes. These methods and reagents exploit advantageous properties of thiazine dyes and diazine dyes. Furthermore, the use of these light emission modifiers in background reduction, nucleic acid duplex stabilization and other uses is also described. Related kits, reaction mixtures and integrated systems are described.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: February 14, 2012
    Assignee: Roche Molecular Systems, Inc.
    Inventors: Amar P. Gupta, Stephen Gordon Will
  • Publication number: 20110195950
    Abstract: The invention relates to compound of the formula I in which R1 represents an optionally substituted aryl group or an optionally substituted heteroaryl group; R2 represents hydrogen or a substituent different from hydrogen; R3 represents an optionally substituted aryl group, cycloalkyl group, heteroaryl group, heterocyclyl group; X1 represents O, S, NR4, CR42; X2 represents O, S, NR4, CR42; X3 represents O, S, NR4, CR42; X4 represents O, S, NR4, CR42; R4 represents hydrogen or a substituent different from hydrogen; R5 represents hydrogen or alkyl; Y represents O or S; m represents 0, 1, 2 or 3; n represents 0, 1, 2 or 3 in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: August 12, 2008
    Publication date: August 11, 2011
    Inventors: Samuel Hintermann, Konstanze Hurth, Marina Tintelnot-Blomley
  • Publication number: 20110136790
    Abstract: The present invention relates to novel Tricyclic Heterocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Heterocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. R1 is formula (Ia), (Ib) or (Ic); R2 is alkvl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl. any of which can be optionally substituted with R11; M1 is —CH—. —C(halo)- or —N—; Y is —C(O)—, —S—. —S(O)—, —S(O)2—, —CH2— or —O—, such that Y is not —O— when an adjacent atom is N.
    Type: Application
    Filed: July 21, 2009
    Publication date: June 9, 2011
    Inventors: Manuel De Lera Ruiz, MIchael Y Berlin, Junying Zheng, Robert G. Aslanian, Kenvin D. McCormick, Qingbel Zeng
  • Patent number: 7919242
    Abstract: The present invention relates to methods and reagents for modifying the emission of light from labeled nucleic acids for the purpose of real time detection, analysis, and quantitation of nucleic acid sequences, e.g., using singly labeled probes. These methods and reagents exploit advantageous properties of thiazine dyes and diazine dyes. Furthermore, the use of these light emission modifiers in background reduction, nucleic acid duplex stabilization and other uses is also described. Related kits, reaction mixtures and integrated systems are described.
    Type: Grant
    Filed: June 23, 2006
    Date of Patent: April 5, 2011
    Assignee: Roche Molecular Systems, Inc.
    Inventors: Amar P. Gupta, Stephen Gordon Will
  • Patent number: 7875712
    Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; ?between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.
    Type: Grant
    Filed: September 23, 2008
    Date of Patent: January 25, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
  • Publication number: 20100285087
    Abstract: Enantomerically purified phenothiazines are provided as active ingredients of medicaments to limit activity of bone resorbing cells so as to reduce bone loss. Novel phenothiazine derivatives are provided. A method of synthesizing enantiomerically pure phenothiazine derivatives is provided that avoids post-synthetic enantiomeric resolution.
    Type: Application
    Filed: February 1, 2010
    Publication date: November 11, 2010
    Applicant: The University Of Texas
    Inventors: Joseph McDonough, Stanton Furst McHardy
  • Patent number: 7807668
    Abstract: Compounds of formula (I) or formula (II) have anti-inflammatory activity and comprise a new class of NSAIDs. The compounds are useful for treating inflammatory diseases or disorders. The invention also provides pharmaceutical compositions containing these compounds, as well as methods of treating inflammatory diseases or disorders using compounds of formula (III) or formula (IV).
    Type: Grant
    Filed: September 16, 2005
    Date of Patent: October 5, 2010
    Assignees: New Zealand Institute for Crop & Food Research Limited, National Institute of Water and Atmospheric Research Limited, Malaghan Institute of Medical Research
    Inventors: William Alexander Denny, Brent Raymond Copp, Allison Norrie Pearce, Michael Vivian Berridge, Jacquie Lucille Harper, Nigel Brian Perry, Lesley Larsen, Colette Amirah Godfrey
  • Publication number: 20100190763
    Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
    Type: Application
    Filed: January 21, 2010
    Publication date: July 29, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
  • Publication number: 20090215736
    Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.
    Type: Application
    Filed: September 23, 2008
    Publication date: August 27, 2009
    Applicant: Vertex Pharmaceuticals, Incorporated
    Inventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
  • Publication number: 20090192308
    Abstract: Preparation of a new class of heterocyclic compounds pharmacologically active as anti-infectives, structurally correlated with 1,5-dihydro-2H-pyrrol-2-one.
    Type: Application
    Filed: January 6, 2009
    Publication date: July 30, 2009
    Applicant: CPC BIOTECH S. r.l.
    Inventor: Fabio Luigi ARENGHI
  • Patent number: 7462346
    Abstract: Photochemical demethylation reactions in solutions of thiazine dyes, in which the dye molecules act as both sensitizer and substrate, are reduced by quenching triple-state dye molecules, returning them to the unreactive ground state.
    Type: Grant
    Filed: August 28, 2001
    Date of Patent: December 9, 2008
    Assignee: Zila Biotechnology, Inc.
    Inventor: Douglas D. Burkett
  • Patent number: 7245073
    Abstract: It is an object to provide an organic compound that has a bipolar property and also a light emitting property, and further has heat resistance. A quinoxaline derivative represented by a general formula (1) is provided. In the formula, A represents any one of an alkylene chain, silicon (Si), oxygen (O), nitrogen (N), and sulfur (S). R1 to R8, which may be identical or different, individually represent any one of a lower alkyl group, an aryl group, and a heterocyclic group.
    Type: Grant
    Filed: July 28, 2004
    Date of Patent: July 17, 2007
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Satoko Shitagaki, Hiroko Abe, Satoshi Seo
  • Patent number: 7135468
    Abstract: Bacterial protein synthesis-inhibiting compounds having formula (I) and salts, prodrugs, salts of prodrugs, and metabolites thereof, processes for making the compounds and intermediates in the processes, compositions containing the compounds, and methods of using the compounds are disclosed.
    Type: Grant
    Filed: February 4, 2005
    Date of Patent: November 14, 2006
    Assignee: Abbott Laboratories
    Inventors: Mira M. Hinman, Teresa A. Rosenberg, Rolf Wagner
  • Patent number: 6974872
    Abstract: The present invention discloses processes for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: December 13, 2005
    Assignee: AMR Technology, Inc.
    Inventors: Thomas E. D'Ambra, Garry M. Pilling
  • Patent number: 6919458
    Abstract: The present invention relates to a process for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents, The process comprises providing a regiosomer of the following formula: wherein Z is —CG1G2G3, m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydr
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: July 19, 2005
    Assignee: AMR Technology, Inc.
    Inventors: Thomas E. D'Ambra, Garry M. Pilling
  • Patent number: 6916925
    Abstract: Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds arc useful, inter alia, for determining the binding and/or receptor sites of the molecules.
    Type: Grant
    Filed: July 22, 2003
    Date of Patent: July 12, 2005
    Assignee: 3M Innovative Properties Co.
    Inventors: Michael J. Rice, Mark A. Tomai, Ai-Ping Wei
  • Publication number: 20040176362
    Abstract: The invention relates to hydroxamic and carboxylic acid derivatives.
    Type: Application
    Filed: March 17, 2004
    Publication date: September 9, 2004
    Inventors: Duncan Batty, Verity Margaret Sabin, Robert John Watson, Hazel Joan Dyke, Andrew Sharpe, Richard John Davenport, David Alan Owen, Andrew Douglas Baxter
  • Publication number: 20040092737
    Abstract: Benzopiperidine derivatives represented by formula (I), salts thereof or hydrates thereof, processes for producing the same and drugs comprising the same: 1
    Type: Application
    Filed: September 20, 2002
    Publication date: May 13, 2004
    Applicant: Eisai Co., Ltd.
    Inventors: Toshihiko Kaneko, Richard Clark, Norihito Ohi, Fumihiro Ozaki, Tetsuya Kawahara, Atsushi Kamada, Kazuo Okano, Hiromitsu Yokohama, Kenzo Muramoto, Tohru Arai, Masayoshi Ohkuro, Osamu Takenaka, Jiro Sonoda
  • Patent number: 6706707
    Abstract: This invention relates to a compound and the use of the compound of the formula wherein R1, R2, R3, R4 and R5 are as defined in the description, A signifies —CH═CH— or —C≡C—; and B signifies wherein R6 to R26, X and Y are as defined in the specification or a pharmaceutically acceptable salt thereof, for use in pharmaceutical compositions for the treatment or prevention of mGluR5 receptor mediated disorders.
    Type: Grant
    Filed: November 28, 2001
    Date of Patent: March 16, 2004
    Assignee: Hoffman-La Roche Inc.
    Inventors: Vincent Mutel, Jens-Uwe Peters, Juergen Wichmann
  • Patent number: 6703371
    Abstract: The invention relates to pharmaceutically active substances from the group comprising midazolam and compounds with a methyl-substituted nitrogen atom that is the ring atom of a nitrogenous heterocycle. These substances are used to reduce the oxygen consumption during a physical activity. They can be administered together with an effective amount of D-glucose, D-maltose, ethanol, a glucogenic amine, a glucogenic amino acid or an amino acid metabolizable via glyoxylate or a dipeptide or a pharmaceutically acceptable salt of such an amino acid and an effective amount of thiamine, of a pharmaceutically acceptable thiamine salt or of a combination of folic acid and cyanocobalamine, with the proviso that the third component is thiamine or a pharmaceutically acceptable thiamine salt if the second component is D-glucose, D-maltose, a glucogenic amine, a glucogenic amino acid non-metabolizable via glyoxylate, or a dipeptide or a pharmaceutically acceptable salt of such an amino acid.
    Type: Grant
    Filed: January 14, 2002
    Date of Patent: March 9, 2004
    Inventor: Oswald Wiss
  • Patent number: 6642222
    Abstract: The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.
    Type: Grant
    Filed: May 3, 2000
    Date of Patent: November 4, 2003
    Assignee: Abbott Laboratories
    Inventors: William A. Carroll, Konstantinos A. Agrios, Robert J. Altenbach, Irene Drizin, Michael E. Kort
  • Patent number: 6608194
    Abstract: A compound of Formula (Ih) The compounds may be used, inter alia, for preparing beta aryl-alpha-oxy substituted alkylcarboxylic acids.
    Type: Grant
    Filed: May 10, 2001
    Date of Patent: August 19, 2003
    Assignee: Dr. Reddy's Laboratories Limited
    Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rao Bheema Paraselli, Ranga Madhavan Gurram
  • Patent number: 6608048
    Abstract: This invention provides compounds of Formula (I), where A″, Z, X and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
    Type: Grant
    Filed: March 28, 2001
    Date of Patent: August 19, 2003
    Assignee: Wyeth Holdings
    Inventors: Hwei-Ru Tsou, Elsebe Geraldine Overbeek-Klumpers, Allan Wissner
  • Publication number: 20030134847
    Abstract: The invention relates to compound of formula (I): 1
    Type: Application
    Filed: October 9, 2002
    Publication date: July 17, 2003
    Inventors: Gerald Guillaumet, Marie-Claude Viaud, Herve Van De Poel, Philippe Delagrange, Caroline Bennejean, Pierre Renard
  • Publication number: 20030130270
    Abstract: The present invention relates to antithrombotic compounds comprising the group Q, Q having formula (I), wherein the substructure (i) is a structure selected from (a, b and c), wherein X is 0 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: Application
    Filed: June 20, 2002
    Publication date: July 10, 2003
    Inventors: Constant Adriaan Anton van Boeckel, Philippus Johannes Marie van Galen, Johannes Bernardus Maria Rewinkel
  • Patent number: 6583138
    Abstract: The invention provides a novel heterocyclic ring condensed benzothiazine compound which is effective for prevention or remedy of disease, in which histamine, leukotriene and the like participate. The heterocyclic ring condensed benzothiazine compound of the present invention or a pharmacologically acceptable salt thereof is effective for prevention or remedy of disease, in which a chemical mediator, such as histamine, leukotriene and the like, participate, for example, asthma, allergic coryza, atopic dermatitis, hives, hay fever, gastrointestinal allergy, food allergy and the like.
    Type: Grant
    Filed: January 4, 2001
    Date of Patent: June 24, 2003
    Assignee: Eisai Co., Ltd.
    Inventors: Mitsuaki Miyamoto, Tatsuya Yoshiuchi, Keizo Sato, Motohiro Soejima, Takashi Sato, Koichi Kikuchi, Hiroyuki Yoshimura, Katsuhiro Moriya, Yoshinori Sakuma, Shigeru Akasofu, Koji Yamada
  • Publication number: 20030072712
    Abstract: Compounds having structure (1) 1
    Type: Application
    Filed: May 21, 2002
    Publication date: April 17, 2003
    Inventors: Kuei-Ying Lin, Mark D. Matteucci
  • Patent number: 6548666
    Abstract: A compound of Formula (Ig) The compounds may be used, inter alia, for preparing beta aryl-alpha-oxy substituted alkylcarboxylic acids.
    Type: Grant
    Filed: May 10, 2001
    Date of Patent: April 15, 2003
    Assignees: Dr. Reddy's Research Foundation, Reddy-Cheminor, Inc.
    Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rao Bheema Paraselli, Ranga Madhavan Gurram
  • Publication number: 20030055035
    Abstract: 1
    Type: Application
    Filed: May 3, 2000
    Publication date: March 20, 2003
    Inventors: Willilam A. Carroll, Konstantinos A. Agrios, Robert J. Altenbach, Irene Drizin, Michael E. Kort
  • Patent number: 6518423
    Abstract: Benzopiperidine derivatives represented by formula (I), salts thereof or hydrates thereof, processes for producing the same and drugs comprising the same: wherein the variables are as described in the specification. These compounds are useful as drugs efficacious in the prevention and treatment of these various inflammatory diseases and immunologic diseases, such as rheumatoid arthritis, atopic dermatitis, psoriasis, asthma, and rejection reaction accompanying organ transplantation.
    Type: Grant
    Filed: April 5, 1999
    Date of Patent: February 11, 2003
    Assignee: Eisai Co., Ltd.
    Inventors: Toshihiko Kaneko, Richard Clark, Norihito Ohi, Fumihiro Ozaki, Tetsuya Kawahara, Atsushi Kamada, Kazuo Okano, Hiromitsu Yokohama, Kenzo Muramoto, Tohru Arai, Masayoshi Ohkuro, Osamu Takenaka, Jiro Sonoda
  • Publication number: 20030004355
    Abstract: A fused pyrazolyl compound of the following formula: 1
    Type: Application
    Filed: January 24, 2002
    Publication date: January 2, 2003
    Inventors: Che-Ming Teng, Sheng-Chu Kuo, Fang Yu Lee
  • Patent number: 6468996
    Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: October 22, 2002
    Assignees: Novo Nordisk A/S, Dr. Reddy's Research Foundation
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Patent number: 6462038
    Abstract: Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions that are agonists, partial agonists, and antagonists for the androgen receptor (AR) are described. Further, described are the methods of making and use of critical intermediates including a stereoselective synthetic route to intermediates for the AR modulators.
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: October 8, 2002
    Assignee: Ligand Pharmaceuticals, Inc.
    Inventors: Robert Higuchi, Kristen L. Arienti, Mani Neelakandha, Barbara Pio, Lin Zhi, Penghui Chen, Thomas R. Caferro
  • Patent number: 6455534
    Abstract: Described are compounds and a method of inhibiting epidermal growth factor receptor tyrosine kinase by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of Formula II: where: one of A or E is nitrogen, with remaining atoms carbon; X=O, S, NH or NR7, such that R7=lower alkyl (1-4 carbon atoms), OH, NH2, lower alkoxy (1-4 carbon atoms) or lower monoalkylamino (1-4 carbon atoms). Other terms are described in the specification.
    Type: Grant
    Filed: April 2, 2001
    Date of Patent: September 24, 2002
    Assignee: Warner-Lambert Company
    Inventors: Alexander James Bridges, William Alexander Denny, David Fry, Alan Kraker, Robert Frederick Meyer, Gordon William Rewcastle, Andrew Mark Thompson
  • Patent number: 6452011
    Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is or and where m is 1 or 4-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: September 17, 2002
    Assignee: Albany Molecular Research, Inc.
    Inventors: Thomas E. D'Ambra, Garry M. Pilling
  • Patent number: 6444824
    Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is and where m is 1 or 3-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; and R5, R8, and R9 are the same or different and are selected from the group consisting of hyrogen, an alkyl moiety, and an aryl moiety.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: September 3, 2002
    Assignee: Albany Molecular Research, Inc.
    Inventors: Thomas E. D'Ambra, Garry M. Pilling
  • Patent number: 6440960
    Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein m, R, R1, R2, X, Y, A, B and C are as defined herein.
    Type: Grant
    Filed: May 18, 2001
    Date of Patent: August 27, 2002
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Mustapha Haddach, John Patrick Williams, Dragan Marinkovic, Jane Han Bu
  • Patent number: 6384045
    Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: May 7, 2002
    Assignee: Kansas State University Research Foundation
    Inventors: Duy H. Hua, Jean-Pierre Perchellet
  • Patent number: 6372904
    Abstract: A process for synthesizing 2-amino-5-dimethlyaminophenyl thiosulfonic acid comprises the step of oxidizing N,N′-dimethyl-&rgr;-phenylene-diamine in the presence of a source of thiosulfate ions, while maintaining the temperature of the reaction mixture not higher than about 10° C. This compound is useful as an intermediate in the synthesis of toluidine blue O. A process for manufacturing toluidine blue O with improved yield, includes the step of preparing the intermediate 2-amino-5-diethylaminopropyl thiosulfonic acid according to the above described procedure.
    Type: Grant
    Filed: January 11, 2001
    Date of Patent: April 16, 2002
    Assignee: Zila, Inc.
    Inventor: Douglas D. Burkett