Tricyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 544/32)
  • 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: 20140073631
    Abstract: Disclosed are guanidine and biguanidine derivatives which have anti-viral and antibacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds. Methods of treating infections using the guanidine and biguanidine derivatives are also disclosed.
    Type: Application
    Filed: September 10, 2013
    Publication date: March 13, 2014
    Applicant: Vymed Corporation
    Inventor: B. Vithal SHETTY
  • Publication number: 20130210806
    Abstract: The present invention is directed to tricyclic indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 15, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Janssen Pharmaceutica, NV
  • Publication number: 20130131051
    Abstract: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein X is selected from the group of CH2, O, and NR2; m=0 or 1; R1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is a bond, —NHCO—, —NH—, or L and Z together can be absent; Z is a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, haloC1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, acetyl, and methanesulfonyl; and R3, R4 and R5 are independently selected from hydrogen or C1-4alkyl.
    Type: Application
    Filed: May 22, 2012
    Publication date: May 23, 2013
    Inventors: LORIN A. THOMPSON, III, Jianliang Shi, Yong-Jin Wu, Lawrence R. Marcin, Ramkumar Rajamani, Mendi A. Higgins
  • Patent number: 8093381
    Abstract: The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): in which R1, R2, R3, R4, R5, R6, R7, and X are as defined in Claim 1.
    Type: Grant
    Filed: May 22, 2008
    Date of Patent: January 10, 2012
    Assignee: Biocodex
    Inventors: Laurence Berthon-Cedille, Marie-Emmanuelle Leguern, Gilles Renaud, Francis Tombret
  • Publication number: 20110319398
    Abstract: The disclosure relates to compounds and methods of inhibiting type three secretion system effector molecules, to methods of detecting compounds that inhibit Yops translocation, and to methods of treating or preventing infections by administering compounds described herein to a subject in need thereof.
    Type: Application
    Filed: June 1, 2011
    Publication date: December 29, 2011
    Applicant: TUFTS UNIVERSITY
    Inventor: Joan Mecsas
  • Publication number: 20110158989
    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: March 4, 2011
    Publication date: June 30, 2011
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
  • 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
  • Patent number: 7799776
    Abstract: Inhibitors of indoleamine 2,3-dioxygenase (IDO) are provided as are pharmaceutical compositions containing such inhibitors as well as the use of such inhibitors and compositions for the treatment of a condition in a mammalian subject characterized by pathology of the IDO-mediated tryptophan metabolic pathway. Such conditions may involve suppression of T-cell mediated immune response or may directly result from depletion of tryptophan or accumulation of a product of tryptophan degradation. Specific disease conditions include cataracts, age-related yellowing in the eye, neurodegenerative disorders, mood disorders, cancer and various bacterial/viral infections. IDO inhibitors of this invention are substituted naphthalene and anthracene diones. Novel compounds of this invention include the following taurine-substituted naphthaquinone structure.
    Type: Grant
    Filed: July 13, 2005
    Date of Patent: September 21, 2010
    Assignee: The University of British Columbia
    Inventors: Raymond J. Andersen, Alban Pereira, Xin-Hui Huang, Grant Mauk, Eduardo Vottero, Michel Roberge, Aruna Balgi
  • Publication number: 20100234363
    Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor.
    Type: Application
    Filed: September 17, 2008
    Publication date: September 16, 2010
    Applicants: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC., SHIONOGI & CO., LTD.
    Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
  • Patent number: 7772227
    Abstract: The invention relates to tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivative having the general Formula (I) wherein X is CH2, O or S; R represents 1-3 substituents independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy and halogen; R1 is (C5-8)cycloalkyl; R2 is H or (C1-4)alkyl; R3, R3?, R4? R4?, R5, R5? and R6? are independently hydrogen or (C1-4)-alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; R6 is hydrogen or (C1-4)alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; or R6 forms together with R7 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; R7 forms together with R6 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; or R7 is H, (C1-4)alkyl or (C3-5)cycloalkyl, the alkyl groups being optionally substituted with OH, halogen or (C1-4)alkyloxy; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 13, 2004
    Date of Patent: August 10, 2010
    Assignee: N.V. Organon
    Inventor: Julia Adam-Worrall
  • Publication number: 20100069374
    Abstract: This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3
    Type: Application
    Filed: November 17, 2009
    Publication date: March 18, 2010
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Kazuhiko Ohrai, Yukohiro Shigeta, Osamu Uesugi, Takumi Okada, Tomoyuki Matsuda
  • Publication number: 20090328258
    Abstract: This present invention provides methods of enhancing the growth of a microorganism or plant by increasing its melanin content and exposing it to radiation, and methods of using melanized microorganisms to contain or exclude radiation.
    Type: Application
    Filed: April 2, 2007
    Publication date: December 31, 2009
    Inventors: Ekaterina Dadachova, Ruth Bryan, Arturo Casadevall
  • Patent number: 7579343
    Abstract: 1H-Pyrrolo-1,4-thiazines and a process for the preparation thereof are described. These compounds are useful as enzyme inhibitors in cells, particularly for medical uses.
    Type: Grant
    Filed: September 6, 2006
    Date of Patent: August 25, 2009
    Assignee: Board of Trustees of Michigan State University
    Inventors: Rawle Hollingsworth, Li Gao
  • Publication number: 20090042868
    Abstract: Inhibitors of indoleamine 2,3-dioxygenase (IDO) are provided as are pharmaceutical compositions containing such inhibitors as well as the use of such inhibitors and compositions for the treatment of a condition in a mammalian subject characterized by pathology of the IDO-mediated tryptophan metabolic pathway. Such conditions may involve suppression of T-cell mediated immune response or may directly result from depletion of tryptophan or accumulation of a product of tryptophan degradation. Specific disease conditions include cataracts, age-related yellowing in the eye, neurodegenerative disorders, mood disorders, cancer and various bacterial/viral infections. IDO inhibitors of this invention are substituted naphthalene and anthracene diones. Novel compounds of this invention include the following taurine-substituted naphthaquinone structure.
    Type: Application
    Filed: July 13, 2005
    Publication date: February 12, 2009
    Applicant: THE UNIVERSITY OF BRITISH COLUMBIA
    Inventors: Raymond J. ANDERSEN, Alban PEREIRA, Xin-Hui HUANG, Grant MAUK, Eduardo VOTTERO, Michel ROBERGE, Aruna BALGI
  • Patent number: 6887868
    Abstract: The present invention provides compounds of Formula (I): wherein: R1, R2, R3, R4, R5, R6 R7, R8, n, m, and X have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired.
    Type: Grant
    Filed: September 19, 2002
    Date of Patent: May 3, 2005
    Assignee: Pharmacia & Upjohn Company
    Inventor: Jian-Min Fu
  • Publication number: 20040167124
    Abstract: Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.
    Type: Application
    Filed: October 16, 2003
    Publication date: August 26, 2004
    Applicant: GILEAD SCIENCES, INC.
    Inventors: James M. Chen, Xiaowu Chen, Maria Fardis, Haolun Jin, Choung U. Kim, Laura N. Schacherer
  • Publication number: 20040106597
    Abstract: Novel fused indazoles and indoles are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.
    Type: Application
    Filed: November 25, 2003
    Publication date: June 3, 2004
    Inventors: Jesse A. May, Anura P. Dantanarayana
  • Patent number: 6703401
    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 clear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: November 27, 2001
    Date of Patent: March 9, 2004
    Assignees: Novo Nordisk A/S, Dr. Reddy's Research Foundation
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • 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: 6699989
    Abstract: Disclosed are guanidine and biguanidine derivatives which have anti-viral and anti-bacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds.
    Type: Grant
    Filed: August 28, 2000
    Date of Patent: March 2, 2004
    Inventor: B. Vithal Shetty
  • Publication number: 20030229026
    Abstract: The present invention provides selective kinase inhibitors of formula (I).
    Type: Application
    Filed: December 2, 2002
    Publication date: December 11, 2003
    Inventors: Rima Salim Al-Awar, Kyle Andrew Hecker, James Edward Ray, Jianping Huang, Sajan Joseph, Tiechao Li, Michael Paal, Radhakrishnan Rathnachalam, Chuan Shih, Philip Parker Waid, Xun Zhou, Guoxin Zhu
  • Publication number: 20030212061
    Abstract: The present invention relates to a group of aza-thioxanthenone compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-thioxanthenone compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.
    Type: Application
    Filed: March 12, 2002
    Publication date: November 13, 2003
    Inventor: Simon N. Haydar
  • Publication number: 20030186970
    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: Application
    Filed: September 9, 2002
    Publication date: October 2, 2003
    Inventors: Robert Higuchi, Kristen L. Arienti, Mani Neelakandha, Barbara Pio, Lin Zhi, Penghui Chen, Thomas R. Caferro
  • Patent number: 6624159
    Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: September 23, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventors: David John Anderson, Gordon L. Bundy, Fred L. Ciske, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Ronald Turner, Valerie A. Vaillancourt, Allison J. Wolf
  • Publication number: 20030144275
    Abstract: The present invention is directed to a procedure for making an enantiomerically enriched compound containing a hydronaphthalene ring structure. The process involves reacting oxabenzonorbornadienes with nucleophiles using rhodium as a catalyst and in the presence of a phosphine ligand. The compounds synthesized may be used in pharmaceutical preparations for the treatment of a variety of diseases and conditions.
    Type: Application
    Filed: December 12, 2002
    Publication date: July 31, 2003
    Applicant: AstraZeneca AB
    Inventors: Keith Fagnou, Mark Lautens
  • 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: 20030105087
    Abstract: The invention relates to compound of formula (I): 1
    Type: Application
    Filed: October 9, 2002
    Publication date: June 5, 2003
    Inventors: Gerald Guillaumet, Marie-Claude Viaud, Herve Van De Poel, Philippe Delagrange, Caroline Bennejean, Pierre Renard
  • Publication number: 20030055031
    Abstract: Methods of using compounds of formula (I): 1
    Type: Application
    Filed: July 25, 2002
    Publication date: March 20, 2003
    Applicant: Rhone-Poulenc Rorer S.A.
    Inventors: Jean-Claude Hardy, Jean Bouquerel, Patrick Nemecek, Jean-Claude Aloup, Serge Mignani, Jean-Francois Peyronel
  • Publication number: 20030032652
    Abstract: The invention relates to hydroxamic and carboxylic acid derivatives.
    Type: Application
    Filed: September 6, 2002
    Publication date: February 13, 2003
    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: 20020183314
    Abstract: Novel non-steroidal tricyclic quinolinone and tricyclic quinoline compounds and compositions that are agonists, partial agonists and/or antagonists for androgen receptors (AR), their preparation and their uses are described.
    Type: Application
    Filed: February 22, 2002
    Publication date: December 5, 2002
    Applicant: Ligand Pharmaceuticals Incorporated
    Inventors: Robert I. Higuchi, Lin Zhi, Donald S. Karanewsky, Anthony W. Thompson, Thomas R. Caferro, Neelakandha S. Mani, Jyun-Hung Chen, Marquis L. Cummings, James P. Edwards, Mark E. Adams, Charlotte L.F. Deckhut
  • Publication number: 20020128263
    Abstract: This invention relates to a compound and the use of the compound of the formula 1
    Type: Application
    Filed: November 28, 2001
    Publication date: September 12, 2002
    Inventors: Vincent Mutel, Jens-Uwe Peters, Juergen Wichmann
  • Patent number: 6448241
    Abstract: Compounds of formula (I): their racemates, enantiomers, diastereoisomers and inorganic acid salts and organic acid salts thereof, processes for preparing them and the medicaments containing them are discussed.
    Type: Grant
    Filed: May 24, 2001
    Date of Patent: September 10, 2002
    Assignee: Aventis Pharma S.A.
    Inventors: Jean-Claude Hardy, Jean Bouquerel, Patrick Nemecek, Jean-Claude Aloup, Serge Mignani, Jean-François Peyronel
  • Patent number: 6444812
    Abstract: This invention concerns intermediates in the preparation of compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; —A— is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, Ar—C1-6alkyl, Ar-oxy, Ar—C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar-oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy, or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alky
    Type: Grant
    Filed: November 29, 2000
    Date of Patent: September 3, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marc Gaston Venet, Patrick René Angibaud, Yannick Aimé Eddy Ligny, Virginie Sophie Poncelet, Gerard Charles Sanz
  • Publication number: 20020115853
    Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: 1
    Type: Application
    Filed: February 12, 2002
    Publication date: August 22, 2002
    Inventors: Puwen Zhang, Reinhold H. W. Bender, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
  • Patent number: 6426416
    Abstract: The process for chemically modifying metal-free, colored anthraquinone or condensed anthraquinone compounds or the compounds prepared by said process for improving one or more properties thereof such as water dispersibility, compatibility with other organics, or increased chemical reactivity, wherein the process includes providing material with from 1-6 sulfonylhalide groups or sulfonate ester groups or mixtures thereof, and contacting the material under sulfonamido forming conditions with one or more reactants containing one or more poly(oxyalkylene) moieties, each of the reactants having from 1 to 4 functional amino groups, and each of the poly(oxyalkylene) moieties being comprised of from about 4 to about 200 epoxide reactant residues at least about 50 mole percent of which residues contain 2-4 carbons and wherein the total of said epoxide reactant residues is from about 4 to about 600.
    Type: Grant
    Filed: January 6, 2000
    Date of Patent: July 30, 2002
    Assignee: Millikan & Companay
    Inventors: Max Allen Weaver, Edward William Kluger, David Jesse Moody
  • Publication number: 20020065268
    Abstract: The present invention relates to compounds of the general formula (I) 1
    Type: Application
    Filed: November 27, 2001
    Publication date: May 30, 2002
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Publication number: 20020055502
    Abstract: The present invention relates to compounds of the general formula (I) 1
    Type: Application
    Filed: November 27, 2001
    Publication date: May 9, 2002
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • 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: 6380235
    Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alknyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstitut
    Type: Grant
    Filed: April 19, 2000
    Date of Patent: April 30, 2002
    Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.
    Inventors: Puwen Zhang, Reinhold H. W. Bender, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
  • Publication number: 20020049203
    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.
    Type: Application
    Filed: May 18, 2001
    Publication date: April 25, 2002
    Inventors: Mustapha Haddach, John Patrick Williams, Dragan Marinkovic, Jane Han Bu
  • Patent number: 6365586
    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: April 2, 2002
    Assignees: Novo Nordisk A/S, Dr. Reddy's Research Foundation
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Patent number: 6348460
    Abstract: A 1,2,3-thiadiazole derivative represented by general formula (I): [wherein R1 is hydrogen atom, halogen atom, (C1-C6) alkyl, phenyl, etc., R2 is the following group (A) or group (B): (wherein R3 is halogen atom, cyano, etc., R4 is hydrogen atom, halogen atom, cyano, etc., X and Y, same or different, are oxygen atom or sulfur atom, n is 0-3, R5 is hydrogen atom, (C1-C20) alkyl, etc., R6 is (C1-C20) alkyl, (C2-C20) alkenyl, etc., and m is 0-2)]; a plant disease controller containing said compound as active ingredient; and a method for using said controller.
    Type: Grant
    Filed: November 10, 1999
    Date of Patent: February 19, 2002
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Kenji Tsubata, Takashi Shimaoka, Tateki Nishida, Kazuhiro Takagi, Koji Baba, Sohkichi Tajima
  • Patent number: 6187786
    Abstract: This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; —A— is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, Ar—C1-6alkyl, Ar-oxy, Ar—C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar-oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy, or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alkyl; R6 hydrogen, hydroxy, halo, cyano
    Type: Grant
    Filed: December 20, 1999
    Date of Patent: February 13, 2001
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marc Gaston Venet, Patrick René Angibaud, Yannick Aimé Eddy Ligny, Virginie Sophie Poncelet, Gerard Charles Sanz
  • Patent number: 6121278
    Abstract: A compound of formula I: ##STR1## or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein:Y represents the atoms necessary to form a fused 5- to 6-membered, aromatic or non-aromatic, heterocyclic ring containing at least one nitrogen heteroatom in a 1,3-relationship with the nitrogen atom depicted in formula I, wherein Y may be unsubstituted or substituted with at least one alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, double bonded oxygen, or --COOR.sup.5 group, or a moiety selected from the group consisting of: ##STR2## wherein R.sup.5 and R.sup.7 are independently hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, or aryl.
    Type: Grant
    Filed: September 1, 1998
    Date of Patent: September 19, 2000
    Assignee: Guilford Pharmaceuticals, Inc.
    Inventors: Paul F. Jackson, Keith M. Maclin, Jie Zhang
  • Patent number: 6071947
    Abstract: The present invention relates to substituted (1H-indol-2-yl)-5[(2H-pyrrol-2-ylidene) methyl]-1H-pyrrole compounds and their use as immunomodulating agents, to the preparation of the compounds and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: June 6, 2000
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Roberto D'Alessio, Marcellino Tibolla, Alberto Bargiotti, Anna Maria Isetta, Mario Ferrari, Francesco Colotta
  • Patent number: 6057315
    Abstract: Described are antibacterial agents of formula (I): X is O, S or N--R.sub.8 ; R.sub.1, R.sub.2, R.sub.3 and R.sub.8 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, R heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR.sub.2, NR'COR', CN, CO.sub.2 R' or CONR.sub.2 ', halogen, CN, CO.sub.2 R, COR, CON(R).sub.2, CON(R").sub.2, SR, SON, SCO.sub.2 R or SCON(R).sub.2 ; R.sub.4 is H, straight or branched alkyl of from 1-6 carbon atoms, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR.sub.2, NR'COR', CN, CO.sub.2 R' or CONR.sub.2 ', halogen, CN, NO.sub.2, N(R).sub.2, NRCOR, NRCOR", COR, CO.sub.2 R, CON(R).sub.2, CON(R").sub.2, NRCON(R).sub.
    Type: Grant
    Filed: March 29, 1999
    Date of Patent: May 2, 2000
    Assignee: Warner-Lambertt Company
    Inventors: John Michael Domagala, Edmund Lee Ellsworth, Michael Andrew Stier, Liren Huang, Ronald George Micetich, Rajeshwar Singh, Stephen Keith Wrigley, Shouming Wang, Michael Roe, David Michael Thornton
  • Patent number: 5998409
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: December 7, 1999
    Assignee: SmithKline Beecham plc
    Inventors: Laramie Mary Gaster, Paul Adrian Wyman
  • Patent number: 5990122
    Abstract: The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by a tricyclic amine radical, their salts, processes for their preparation and antibacterial compositions comprising these compounds.
    Type: Grant
    Filed: January 7, 1998
    Date of Patent: November 23, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uwe Petersen, Thomas Schenke, Thomas Jaetsch, Stephan Bartel, Klaus Dieter Bremm, Rainer Endermann, Karl Georg Metzger
  • Patent number: 5985871
    Abstract: Compounds having a certain benzoxazine ring system and their precursors are disclosed which are useful for enhancing synaptic responses mediated by AMPA receptors. Also disclosed are methods for preparing such compounds, and methods for their use in treating subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number of excitatory synapses or in the number of AMPA receptors. The invention compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors and for improving memory encoding.
    Type: Grant
    Filed: December 24, 1997
    Date of Patent: November 16, 1999
    Assignee: Cortex Pharmaceuticals, Inc.
    Inventors: Gary A. Rogers, Christopher Marrs