The Five-membered Hetero Ring Consists Of One Nitrogen And Four Carbons Patents (Class 514/408)
  • Publication number: 20030153548
    Abstract: The invention relates to a method of treating a diabetic condition by administering a therapeutically effective amount of a histamine-3 receptor antagonist, including benzofuran and benzopyran derivatives of formula (I), aminoalkoxybiphenylcarboxamide compounds of formula (III), and aminoetherbiphenyl compounds of formula (IV) as described herein.
    Type: Application
    Filed: December 23, 2002
    Publication date: August 14, 2003
    Inventors: Arthur A. Hancock, Eugene N. Bush, Marlon D. Cowart, Peer B. Jacobson, Terry J. Opgenorth, Youssef Bennani
  • Publication number: 20030153602
    Abstract: A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders.
    Type: Application
    Filed: December 27, 2002
    Publication date: August 14, 2003
    Applicant: G.D. Searle & Co.
    Inventors: John J. Talley, Stephen R. Bertenshaw, Paul W. Collins, Thomas D. Penning, David B. Reitz, Roland S. Rogers
  • Publication number: 20030153559
    Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.
    Type: Application
    Filed: November 20, 2002
    Publication date: August 14, 2003
    Inventors: Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
  • Patent number: 6605605
    Abstract: Provided herein are medicinal compositions of matter that comprise an estrogenic medication component and a cruciferous indole component (indole 3-carbinol, diindolylmethane, or any derivative thereof. Through use of the compositions of the invention a heretofore unobserved synergy is observed in the treatment of perimenopause, menopause or any other cause of ovarian failure. The invention also provides procedures for administering the composition to a patient who is afflicted with perimenopause, menopause or any other cause of ovarian failure.
    Type: Grant
    Filed: November 10, 2001
    Date of Patent: August 12, 2003
    Inventor: Milton Hammerly
  • Publication number: 20030144310
    Abstract: This invention provides a compound having the structure: 1
    Type: Application
    Filed: September 24, 2002
    Publication date: July 31, 2003
    Inventors: Lakmal W. Boteju, Michael J. Konkel, Joel K. Kawakami, John Wetzel
  • 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
  • Publication number: 20030144323
    Abstract: Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
    Type: Application
    Filed: December 2, 2002
    Publication date: July 31, 2003
    Inventors: Richard Apodaca, Wei Xiao, Jill A. Jablonowski
  • Publication number: 20030144322
    Abstract: The invention provides a compound of formula (I): 1
    Type: Application
    Filed: October 23, 2002
    Publication date: July 31, 2003
    Inventors: Alan P. Kozikowski, Gian Luca Araldi
  • Publication number: 20030144272
    Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided.
    Type: Application
    Filed: May 15, 2002
    Publication date: July 31, 2003
    Inventors: Virendra Kumar, Deqi Guo, Michael Anthony Marella, Alan L. Maycock
  • Publication number: 20030144261
    Abstract: The present invention discloses compounds, which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Application
    Filed: October 23, 2002
    Publication date: July 31, 2003
    Applicant: Schering Corporation
    Inventors: Anandan Palani, Sherry A. Shapiro, Mark D. McBriar, Jing Su
  • Patent number: 6599511
    Abstract: Desoxypeganine and its pharmaceutically acceptable acid addition salts can be used in the treatment of drug addiction or drug dependence. Said substances are administered preferably in a continuos and controlled manner. The pharmaceutical administration form enables controlled release, e.g. for oral transdermal or another route of parenteral administration.
    Type: Grant
    Filed: October 17, 2001
    Date of Patent: July 29, 2003
    Assignees: LTS Lohmann Therapie-Systeme AG, HF Aezneimittelforschung GmbH
    Inventors: Bodo Asmussen, Thomas Hille, Hans-Rainer Hoffmann, Klaus Opitz
  • Patent number: 6599931
    Abstract: A test system for characterizing the compatibility of bioactive substances with polyvinylpyrrolidones in a solid dispersion consisting of one or more bioactive substances and 1,3-bis(1-pyrrolidonyl)butane.
    Type: Grant
    Filed: September 18, 1999
    Date of Patent: July 29, 2003
    Assignee: Abbott GmbH & Co. KG
    Inventors: Jörg Breitenbach, Robert Heger, Dirk Simon, Bernd Liepold
  • Publication number: 20030139458
    Abstract: A method of treating a neurodegenerative or cardiovascular disorder with a compound of the following formula: 1
    Type: Application
    Filed: December 10, 2002
    Publication date: July 24, 2003
    Inventors: Yansheng Du, Martin R. Farlow, Ruyu Du
  • Publication number: 20030139387
    Abstract: The present invention concerns methods for treating or preventing neurological disorders characterized by dysfunction of nicotinic acetylcholine receptors by co-administration of metanicotine and at least one compound which exhibits antagonist activity, or both agonistic and antagonists activity, toward one or more nicotinic acetylcholine receptor subtypes. The subject invention, in another aspect, pertains to pharmaceutical compositions containing metanicotine and at least one compound which inhibits antagonistic activity, or both agonistic and antagonistic activity, toward one or more nicotinic acetylcholine receptor subtypes.
    Type: Application
    Filed: December 31, 2001
    Publication date: July 24, 2003
    Inventor: Roger L. Papke
  • Publication number: 20030139448
    Abstract: The present invention relates to substituted N-(cyclopropylmethyl)azacycloalkanes of the following formula (I): 1
    Type: Application
    Filed: December 13, 2002
    Publication date: July 24, 2003
    Inventor: Henry Jacobelli
  • Publication number: 20030139402
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Application
    Filed: September 20, 2002
    Publication date: July 24, 2003
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
  • Publication number: 20030139390
    Abstract: Modulators of PPAR&ggr; activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.
    Type: Application
    Filed: July 30, 2002
    Publication date: July 24, 2003
    Applicant: Tularik Inc.
    Inventors: Lawrence R. McGee, Jonathan B. Houze, Steven M. Rubenstein
  • Publication number: 20030139459
    Abstract: A veterinary preparation for fleas is described, which consists of an amount that is effective against fleas of a combination of a compound of formula (I), wherein R1 hydrogen, C1-C6-alkyl or C3-C7-cycloalkyl; R2 is hydrogen, C1-C6-alkyl or C3-C7-cycloalkyl; R3 is hydrogen or C1-C6-alkyl; and A is heterocycly which is unsubstituted or substituted once or repeatedly by identical or different halogen atoms; and a compound of formula (II), wherein X is halogen, X1 is hydrogen or halogen; X2 is hydrogen or halogen; Y is partially or completely halogenated C1-C6-alkoxy, or partially or completely halogenated C1-C6-alkoxy which is interrupted by one oxygen atom, or partially or completely halogenated C2-C6-alkenyl; Y1 is hydrogen or halogen; Y2 is hydrogen or halogen; Y3 is hydrogen or halogen; Z1 is hydrogen or C1-C3-alkyl; and Z2 is hydrogen or C1-C3-alkyl; and a physiologically acceptable formulation excipient.
    Type: Application
    Filed: December 12, 2002
    Publication date: July 24, 2003
    Inventors: Olivier Tinembart, Michel Franc, Jean Steffan
  • Publication number: 20030139456
    Abstract: Methods and kits for treament of glaucoma are disclosed. In general, the methods of the invention include administering a therapeutically effective amount of a deprenyl compound to a subject such that the subject is treated for glaucoma.
    Type: Application
    Filed: August 2, 2002
    Publication date: July 24, 2003
    Inventor: William G. Tatton
  • Publication number: 20030134821
    Abstract: The invention provides methods and compositions for promoting neural cell growth and/or regeneration. The general methods involve contacting with an activator of a cyclic nucleotide dependent protein kinase a neural cell subject to growth repulsion mediated by a neural cell growth repulsion factor. The activator may comprise a direct or an indirect activator of the protein kinase; the repulsion factor typically comprises one or more natural, endogenous proteins mediating localized repulsion or inhibition of neural cell growth; and the target cells are generally vertebrate neurons, typically injured mammalian neurons. The subject compositions include mixtures comprising a neural cell, an activator of a cyclic nucleotide dependent protein kinase and a neural cell growth repulsion factor.
    Type: Application
    Filed: October 17, 2002
    Publication date: July 17, 2003
    Inventors: Hong-jun Song, Mu-ming Poo, Guo-li Ming, Marc Tessier-Lavigne, Zhigang He
  • Publication number: 20030130272
    Abstract: Use of compound of Formula (I): at least one of R1, R2, R5 and R6 is a group —AB and the others are independently selected from hydrogen, hydroxy, alkoxy or acyloxy, a group —AB a group -amino-(R7)nX—Y wherein R7 is a divalent organic radical and n is 0 or 1; R3 and R4are independently oxo, hydroxy or hydrogen; the or each A is independently a spacer group of formula -amino-(R7)n—X— which is bonded to the anthracene ring via the amino group nitrogen and to B via —X—, X is independently selected from O, NH and C(O); B is an amino acid residue or a peptide group or isostere thereof and Y is hydrogen or a capping group, or a physiologically acceptable derivative of such compound for the manufacture of a medicament for the treatment of cancers or microbial infections having cells exhibiting topoisomerase I activity characterised in that the group -amino-(R7)n—X— incorporates an optionally substituted heterocyclic ring directly attached to the anthroquinone rin
    Type: Application
    Filed: July 15, 2002
    Publication date: July 10, 2003
    Inventors: David John Mincher, Agnes Turnbull, Graeme Gillies Kay
  • Publication number: 20030130256
    Abstract: The present invention relates to cyclized amide derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
    Type: Application
    Filed: February 5, 2003
    Publication date: July 10, 2003
    Inventors: David Lauffer, Michael Mullican, Brian Ledford
  • Publication number: 20030130238
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: November 1, 2002
    Publication date: July 10, 2003
    Applicant: American Cyanamid Company
    Inventors: Vincent Premaratna Sandanayaka, Efren Guillermo Delos Santos
  • Publication number: 20030130322
    Abstract: The present invention relates to a method of treating alcoholism or alcohol dependence in a mammal, including a human, by administering to the mammal a monoamine reuptake inhibitor in combination with an opioid antagonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a monoamine reuptake inhibitor and an opioid antagonist.
    Type: Application
    Filed: May 22, 2002
    Publication date: July 10, 2003
    Applicant: Pfizer Inc.
    Inventor: Harry R. Howard
  • Patent number: 6589975
    Abstract: Novel uses of biologically active bis-heterocyclic e.g. bis-indole alkaloid compounds which have improved activity are disclosed. Pharmaceutical compositions containing the compounds are also disclosed. Specifically, the novel utility pertains to the anti-immunogenic and neurogenic inflammatory properties exhibited by the bis-indole compounds and their analogs.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: July 8, 2003
    Assignees: The Regents of the University of California, Harbor Branch Oceanographic Inst.
    Inventors: Robert S. Jacobs, Claudia E. Moya, Amy E. Wright
  • Publication number: 20030125306
    Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.
    Type: Application
    Filed: December 13, 2002
    Publication date: July 3, 2003
    Applicant: CircaGen Pharmaceutical, a Delaware corporation
    Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman, Norbert L. Wiech
  • Publication number: 20030125389
    Abstract: The invention provides compounds that are useful for the treatment of bacterial infections in mammals.
    Type: Application
    Filed: July 25, 2002
    Publication date: July 3, 2003
    Inventors: Bore G. Raju, Sampathkumar Anandan, Joaquim Trias, Prudencio S. Herradura, Kathleen H. Mortell, Dinesh V. Patel
  • Patent number: 6586478
    Abstract: Methods and compositions for improving sleep in individuals with sleep disorders or other conditions which interfere with normal sleep via administration of a NO-mimetic are provided.
    Type: Grant
    Filed: February 22, 2001
    Date of Patent: July 1, 2003
    Assignee: Cellegy Canada
    Inventors: C. Bruce Ackman, Michael A. Adams, Jeremy P. W. Heaton, Jodan D. Ratz
  • Publication number: 20030119860
    Abstract: A method is disclosed for the treatment of non-rheumatoid arthritis by administering to a mammal in need thereof a therapeutically effective amount of an sPLA 2 inhibitor.
    Type: Application
    Filed: February 24, 2000
    Publication date: June 26, 2003
    Inventor: WILLIAM LOUIS MACIAS
  • Publication number: 20030119864
    Abstract: A family of compounds capable of inhibiting the activity of farnesyl transferase.
    Type: Application
    Filed: October 18, 2002
    Publication date: June 26, 2003
    Applicant: Biomeasure Incorporated, a Massachusetts corporation
    Inventors: Thomas D. Gordon, Barry A. Morgan
  • Publication number: 20030119853
    Abstract: Compounds of formula (1): 1
    Type: Application
    Filed: December 20, 2002
    Publication date: June 26, 2003
    Inventors: Sarah Catherine Archibald, John Clifford Head, Graham John Warrellow, John Robert Porter
  • Publication number: 20030114500
    Abstract: Nitrogen heterocycles that inhibit aspartyl protease are disclosed, as are methods of treating diseases, particularly HIV, using these compounds.
    Type: Application
    Filed: October 22, 2001
    Publication date: June 19, 2003
    Inventors: Guoqiang Wang, Yat Sun Or, John Rougas, Steven Wayne Riesinger
  • Publication number: 20030114499
    Abstract: This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them.
    Type: Application
    Filed: June 12, 2002
    Publication date: June 19, 2003
    Inventors: Joachim Brendel, Thomas Bohme, Stefan Peukert, Heinz-Werner Kleemann
  • Publication number: 20030109560
    Abstract: Novel compounds of general formula (I), the use of these compounds as medicaments, pharmaceuticaly compositions comprising the compounds and methods of treatment employing these compounds and compostiones. The present compounds may be useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). The compounds exert their effects by modulating the PPAR&ggr; response in a partial agonist manner.
    Type: Application
    Filed: July 29, 2002
    Publication date: June 12, 2003
    Inventors: Lone Jeppesen, Paul Stanley Bury, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
  • Publication number: 20030109559
    Abstract: Disclosed are compounds of the formula (I): 1
    Type: Application
    Filed: July 11, 2002
    Publication date: June 12, 2003
    Inventors: Andrea Gailunas, John A. Tucker, Ruth TenBrink, John Mickelson
  • Publication number: 20030109502
    Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.
    Type: Application
    Filed: April 12, 2001
    Publication date: June 12, 2003
    Inventors: Chaim M. Roifman, Thomas Grunberger, Olga Rounova, Demin Peter, Nigel Sharfe
  • Patent number: 6576612
    Abstract: The present invention relates to an administration schedule comprising the intravenous administration of a &agr;-halogen-acryloyl distamycin derivative of formula (I) wherein R is a bromine or chlorine atom; or a pharmaceutically acceptable salt thereof. The above administration allows the treatment of a variety of tumors in mammals.
    Type: Grant
    Filed: October 2, 2000
    Date of Patent: June 10, 2003
    Assignees: Pharmacia Italia S.p.A., Pharmacia & Upjohn Company
    Inventors: Camilla Fowst, Franzanne Vreeland, Maria Cristina Rosa Geroni
  • Publication number: 20030105097
    Abstract: The invention provides compounds of formula (I) 1
    Type: Application
    Filed: May 6, 2002
    Publication date: June 5, 2003
    Applicant: Pfizer Inc.
    Inventors: Andrew Simon, Alan Stobie
  • Publication number: 20030105143
    Abstract: The present invention relates to the use of compounds of the general Formula (I) 1
    Type: Application
    Filed: March 8, 2002
    Publication date: June 5, 2003
    Inventors: Aldo Ammendola, Bernd Kramer, Wael Saeb
  • Publication number: 20030105079
    Abstract: The present invention relates to novel 1,2- or 1,3-diamine and amide compounds and pharmaceutically useful salts thereof and methods for treating central nervous system diseases. The present 1,2- or 1,3-diamine and amide compounds have high binding affinity to the sigma receptor.
    Type: Application
    Filed: June 12, 2002
    Publication date: June 5, 2003
    Inventors: Yong-Moon Choi, Yong-Kil Kim, Chun-Eung Park, Eun-Ho Lee
  • Publication number: 20030100584
    Abstract: The invention relates to novel selective inhibitors of the urokinase plasminogen activator (uPA, EC 3.4.21.31), of the arylguanidine type.
    Type: Application
    Filed: September 20, 2002
    Publication date: May 29, 2003
    Inventors: Viktor Magdolen, Stefan Speri, Joerg Stuerzebecher, Olaf Wilhelm, Nuria Arroyo De Prada, Luis Moroder, Robert Huber, Uwe Jacob, Wolfram Bode
  • Publication number: 20030100547
    Abstract: Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula: 1
    Type: Application
    Filed: August 30, 2002
    Publication date: May 29, 2003
    Applicant: University of Kentucky Research Foundation
    Inventors: Linda P. Dwoskin, Peter A. Crooks, Marlon D. Jones
  • Publication number: 20030100580
    Abstract: P51084 The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.
    Type: Application
    Filed: June 13, 2002
    Publication date: May 29, 2003
    Inventors: Dashyant Dhanak, Steven David Knight
  • Publication number: 20030096792
    Abstract: Methods are disclosed for the treatment and prevention of disorders and conditions such as, but are not limited to: eating disorders; weight gain; obesity; irritable bowel syndrome; obsessive-compulsive disorders; platelet adhesion; apnea; affective disorders such as attention deficit disorders, depression, and anxiety; male and female sexual function disorders; restless leg syndrome; osteoarthritis; substance abuse including nicotine and cocaine addiction; narcolepsy; pain such as neuropathic pain, diabetic neuropathy, and chronic pain; migraines; cerebral function disorders; chronic disorders such as premenstrual syndrome; and incontinence.
    Type: Application
    Filed: October 23, 2002
    Publication date: May 22, 2003
    Applicant: Sepracor, Inc.
    Inventors: Thomas P. Jerussi, Chrisantha H. Senanayake, Qun K. Fang
  • Publication number: 20030092748
    Abstract: 1
    Type: Application
    Filed: July 18, 2002
    Publication date: May 15, 2003
    Inventors: Stephen Douglas Barrett, Haile Tecle, Richard John Booth
  • Publication number: 20030092746
    Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
    Type: Application
    Filed: May 21, 2001
    Publication date: May 15, 2003
    Inventors: William K. Hagmann, Stephen E. DeLaszlo, Theodore Kamenecka, Malcolm MacCoss
  • Publication number: 20030092708
    Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): 1
    Type: Application
    Filed: May 22, 2002
    Publication date: May 15, 2003
    Applicant: Japan Tobacco, Inc., a Japan Corporation
    Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
  • Publication number: 20030092755
    Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I): 1
    Type: Application
    Filed: July 30, 2002
    Publication date: May 15, 2003
    Inventors: David W. Boykin, M. Syed Rahmathullah, RIchard R. Tidwell, James E. Hall
  • Publication number: 20030087890
    Abstract: The present application describes novel 1,2-disubsituted cyclic derivatives of formula I: 1
    Type: Application
    Filed: January 9, 2002
    Publication date: May 8, 2003
    Inventors: Chu-Biao Xue, Carl Decicco, Xiaohua He
  • Publication number: 20030087945
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: June 13, 2002
    Publication date: May 8, 2003
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase