Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Nitrogen Of The Five-membered Hetero Ring (e.g., Indomethacin, Etc.) Patents (Class 548/500)
  • Patent number: 8865130
    Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: October 21, 2014
    Assignee: Vanderbilt University
    Inventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
  • Publication number: 20140256781
    Abstract: The present invention relates to methods for producing particles of indomethacin using dry milling processes as well as compositions comprising indomethacin, medicaments produced using indomethacin in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of indomethacin administered by way of said medicaments.
    Type: Application
    Filed: May 20, 2014
    Publication date: September 11, 2014
    Applicant: ICEUTICA PTY LTD.
    Inventors: Aaron Dodd, Felix Meiser, Marck Norret, Adrian Russell, H. William Bosch
  • Patent number: 8541398
    Abstract: The present invention relates to derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) having improved anti-inflammatory properties useful in the treatment of inflammation, pain and fever. More particularly, NSAIDs are derivatized with a hydrogen sulfide (H2S) releasing moiety to produce novel anti-inflammatory compounds having reduced side effects.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: September 24, 2013
    Assignee: Antibe Therapeutics Inc.
    Inventors: John L. Wallace, Giuseppe Cirino, Vincenzo Santagada, Giuseppe Caliendo
  • Publication number: 20130178466
    Abstract: The invention provides compositions, medicaments and methods of treating microbial infections, and especially respiratory disorders caused by microbial infections. In particular, the invention relates to the treatment of respiratory diseases caused by pathogenic infections using certain either alkyl substituted or un-substituted 2-aryl acetic acid, or 2-aryl, N-hydroxyacetamide derivatives, or pentoxifylline, and to the use of these compounds in methods of treatment.
    Type: Application
    Filed: November 9, 2010
    Publication date: July 11, 2013
    Applicant: BIOCOPEA LIMITED
    Inventors: Robin Mark Bannister, Wilson Caparros Wanderlay, John Brew
  • Publication number: 20130158070
    Abstract: Novel chemical conjugates derived from unsaturated fatty acids and therapeutically active agents, are disclosed. The chemical conjugates are designed and characterized as COX-2 and/or 5-LOX inhibitors and are useful in the treatment of inflammatory diseases and disorders such as Alzheimer's disease, Parkinson's disease, asthma, osteoarthritis, rheumatoid arthritis, pain, primary dysmenorrhea, Crohn's disease and ulcerative colitis.
    Type: Application
    Filed: September 6, 2011
    Publication date: June 20, 2013
    Inventor: Taher Nassar
  • Publication number: 20130065934
    Abstract: The invention relates to fatty acid COX inhibitor derivatives; compositions comprising an effective amount of a fatty acid COX inhibitor derivative; and methods for treating or preventing a metabolic, autoimmune, inflammatory, or neurodegenerative disorder comprising the administration of an effective amount of a fatty acid COX inhibitor derivative.
    Type: Application
    Filed: March 4, 2011
    Publication date: March 14, 2013
    Applicant: CATABASIS PHARMACEUTICALS, INC.
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
  • Publication number: 20130052138
    Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.
    Type: Application
    Filed: March 27, 2012
    Publication date: February 28, 2013
    Applicant: Vanderbilt University
    Inventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
  • Publication number: 20130040884
    Abstract: Novel polypeptide derivatives having protracted profile of action.
    Type: Application
    Filed: March 22, 2012
    Publication date: February 14, 2013
    Inventors: Jesper Lau, Thomas Kruse Hansen, Kjeld Madsen, Paw Bloch, Florencio Zaragoza Dorwald, Nils Langeland Johansen
  • Patent number: 8362027
    Abstract: The present invention is to provide means to treat breast cancer and/or mastitis by topically administering a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent and allowing them efficiently to arrive into the mammary gland. The present invention provides an iontophoretic preparation for treating breast cancer and/or mastitis which contains a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent as an active ingredient and has a donor to be applied on a nipple part for topical administration of the active ingredient from the nipple part to the mammary gland by application of electric potential.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: January 29, 2013
    Assignees: Kowa Co., Ltd., Tokyo University of Science Educational Foundation Administrative Organization
    Inventors: Toshio Inagi, Makoto Kanebako, Hiroshi Terada, Kimiko Makino, Masakazu Toi
  • Publication number: 20120010168
    Abstract: A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; X?C, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed.
    Type: Application
    Filed: November 3, 2009
    Publication date: January 12, 2012
    Inventors: Jeffrey Laskin, Diane Heck, Mou-Tuan Huan, Karine Fabio, C. Jeffrey Lacey, Sherri Young, Pramod Mohanta, Christophe Guillon, Ned Heindel
  • Publication number: 20110269722
    Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.
    Type: Application
    Filed: December 23, 2010
    Publication date: November 3, 2011
    Inventor: Apparao Satyam
  • Publication number: 20110263526
    Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.
    Type: Application
    Filed: April 22, 2011
    Publication date: October 27, 2011
    Applicant: PIRAMAL LIFE SCIENCES LIMITED
    Inventor: Apparao SATYAM
  • Publication number: 20110253944
    Abstract: The present invention relates to a novel polycyclic aromatic organic semiconductor compound having a polycyclic aromatic core, a method for preparing the same, and electronic, optical or electro-optical devices such as an organic semiconductor composition, organic semiconductor thin film, organic field effect transistor and solar cell containing the compound. The novel organic semiconductor compound according to the present invention has high crystallinity and control capability, and facilitates control of doping conditions in the manufacture of organic semiconductor element so that it can be used for diverse applications. The compound can be mass-produced at low cost and has high solubility in organic solvents so that a liquid phase process can be applied to the manufacture of semiconductor elements and the like, thus enabling the mass-production of semiconductor elements and solar cells at low cost.
    Type: Application
    Filed: December 23, 2009
    Publication date: October 20, 2011
    Applicant: LUMINANO CO., LTD.
    Inventors: Sung Hwan Han, Cheon Gyu Cho
  • Patent number: 8034824
    Abstract: The present invention is to provide means to treat breast cancer and/or mastitis by topically administering a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent and allowing them efficiently to arrive into the mammary gland. The present invention provides an iontophoretic preparation for treating breast cancer and/or mastitis which contains a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent as an active ingredient and has a donor to be applied on a nipple part for topical administration of the active ingredient from the nipple part to the mammary gland by application of electric potential.
    Type: Grant
    Filed: October 11, 2006
    Date of Patent: October 11, 2011
    Assignees: Kowa Co., Ltd., Tokyo University of Science Educational Foundation Administrative Organization
    Inventors: Toshio Inagi, Makoto Kanebako, Hiroshi Terada, Kimiko Makino, Masakazu Toi
  • Publication number: 20110230524
    Abstract: The present invention relates to novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, to novel antiviral active ingredients, pharmaceutical compositions, antiviral medicaments, methods for prophylaxis and treatment of viral diseases particularly caused by influenza viruses and infectious hepatisis C (HCV) viruses.
    Type: Application
    Filed: November 27, 2009
    Publication date: September 22, 2011
    Inventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko, Pavel Mikhailovich Yamanushkin, Oleg Dmitrievich Mitkin, Vladimir Yurievich Vvedensky, Vadim Vasilievich Bichko
  • Publication number: 20110150873
    Abstract: The invention relates to the use of Broad-Spectrum Chemokine Inhibitors (BSCIs), and in particular members of the acylaminolactam class of pharmaceutical agents, for the prevention, prophylaxis, treatment or amelioration of symptoms of inflammatory diseases. In particular, improved compositions consisting of BSCI agents combined with one or more additional active pharmaceutical agents in order to achieve improved anti-inflammatory efficacy with a reduced side-effect profile are described and claimed.
    Type: Application
    Filed: December 10, 2008
    Publication date: June 23, 2011
    Applicant: CAMBRIDGE ENTERPRISE LIMITED
    Inventor: David John Grainger
  • Publication number: 20110118455
    Abstract: A protecting group for 1-nitrogen atom of an indole group including a sulfonylethyl carbamate group, wherein the protecting group is represented by the following General Formula (I) and capable of being removed from the 1-nitrogen atom of the indole group in an aprotic solvent: where R represents an alkyl group, a derivative of the alkyl group, a phenyl group or a derivative of the phenyl group.
    Type: Application
    Filed: November 19, 2010
    Publication date: May 19, 2011
    Applicant: FUJITSU LIMITED
    Inventor: Tsuyoshi FUJIHARA
  • Publication number: 20100292289
    Abstract: The present invention relates to the treatment of metabolic syndrome or disorders associated with metabolic syndrome comprising administering a compound of the invention.
    Type: Application
    Filed: November 26, 2008
    Publication date: November 18, 2010
    Applicant: AMPLA Pharmaceuticals Inc.
    Inventor: James R. Hauske
  • Publication number: 20100210607
    Abstract: The present invention relates to derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) having improved anti-inflammatory properties useful in the treatment of inflammation, pain and fever. More particularly, NSAIDs are derivatized with a hydrogen sulfide (H2S) releasing moiety to produce novel anti-inflammatory compounds having reduced side effects.
    Type: Application
    Filed: February 11, 2010
    Publication date: August 19, 2010
    Applicant: ANTIBE THERAPEUTICS INC.
    Inventors: JOHN WALLACE, GIUSEPPE CIRINO, VINCENZO SANTAGADA, GIUSEPPE CALIENDO
  • Patent number: 7741359
    Abstract: The present invention relates to derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) having improved anti-inflammatory properties useful in the treatment of inflammation, pain and fever. More particularly, NSAIDs are derivatized with a hydrogen sulfide (H2S) releasing moiety to produce novel anti-inflammatory compounds having reduced side effects.
    Type: Grant
    Filed: July 18, 2007
    Date of Patent: June 22, 2010
    Assignee: Antibe Therapeutics Inc.
    Inventors: John Wallace, Giuseppe Cirino, Vincenzo Santagada, Giuseppe Caliendo
  • Publication number: 20100152272
    Abstract: Compounds selected from: where DRUG-OH, DRUG-COOH and DRUG-NH2 are biologically active compounds; each X is independently selected from —CH2COO— (glycolic acid moiety), —CH(CH3)COO— (lactic acid moiety), —CH2CH2OCH2COO— (dioxanone moiety), —CH2CH2CH2CH2CH2COO— (caprolactone moiety), —(CH2)yCOO—, where y is 2-4 or 6-24 and —(CH2CH2O)zCH2COO—, where z is 2-24; each Y is independently selected from —COCH2O— (glycolic ester moiety), —COCH(CH3)O— (lactic ester moiety), —COCH2OCH2CH2O— (dioxanone ester moiety), —COCH2CH2CH2CH2CH2O— (caprolactone ester moiety), —CO(CH2)mO—, where m is 2-4 or 6-24 and —COCH2O(CH2CH2O)n— where n is between 2-24; R? is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; and p is 1-6. Multi-functional compounds and drug dimers, oligomers and polymers are also disclosed.
    Type: Application
    Filed: February 17, 2010
    Publication date: June 17, 2010
    Applicant: BEZWADA BIOMEDICAL, LLC
    Inventor: Rao S. Bezwada
  • Publication number: 20100016597
    Abstract: Disclosed is a method for producing pulverized particles of a crystalline organic compound which is poorly water-soluble. Also disclosed is a pulverized organic compound particle produced by such a method. Specifically disclosed is a method for producing a poor water solubility organic compound particle for medical use, which is characterized in that a poor water solubility organic compound for medical use is mixed with a physiologically acceptable salt and a physiologically acceptable polyol, and subjected to wet milling. Also specifically disclosed is a poor water solubility organic compound particle for medical use, which is produced by such a production method.
    Type: Application
    Filed: September 24, 2009
    Publication date: January 21, 2010
    Applicant: Activus Pharma Co., Ltd.
    Inventors: Takashi Hirokawa, Takahiro Tada
  • Publication number: 20090281063
    Abstract: The present invention is to provide means to treat breast cancer and/or mastitis by topically administering a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent and allowing them efficiently to arrive into the mammary gland. The present invention provides an iontophoretic preparation for treating breast cancer and/or mastitis which contains a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent as an active ingredient and has a donor to be applied on a nipple part for topical administration of the active ingredient from the nipple part to the mammary gland by application of electric potential.
    Type: Application
    Filed: October 11, 2006
    Publication date: November 12, 2009
    Applicants: KOWA CO., LTD., TOKYO UNIVERSITY OF SCIENCE EDUCATIONAL FOUNDATION ADMINISTRATIVE ORGANIZATION
    Inventors: Toshio Inagi, Makoto Kanebako, Hiroshi Terada, Kimiko Makino, Masakazu Toi
  • Patent number: 7553865
    Abstract: An object of the present invention is to provide an indomethacin external preparation that has an excellent use feeling and excellent absorbability and causes no phase separation into an oil layer and an aqueous layer, thus exhibiting satisfactory stability of preparation with time. Provided is an indomethacin external preparation containing: 0.1 to 3 wt % of indomethacin; 25 to 50 wt % of alcohol; 0.01 to 5 wt % of gelling agent; 5 to 30 wt % of oil component; 20 to 50 wt % of water; and 0.01 to 10 wt % of one or more components selected from the group consisting of glyceryl monostearate, sorbitan monostearate, stearyl alcohol, and polyethylene glycol monostearate.
    Type: Grant
    Filed: July 22, 2003
    Date of Patent: June 30, 2009
    Assignee: Kowa Company, Ltd.
    Inventors: Hiroyuki Shirai, Tatsuya Nakai, Masami Serizawa, Yasuo Shinoda, Toshio Inagi
  • Publication number: 20090155903
    Abstract: The invention provides compounds, pharmaceutical compositions and methods for the therapeutic treatment and prevention of neurodegenerative disorder and other A?42-related diseases and disorders.
    Type: Application
    Filed: March 21, 2005
    Publication date: June 18, 2009
    Applicant: Myriad Genetics, Incorporated
    Inventors: Rachel M. Slade, Warren S. Weiner, Eric Delmar, Yevgeniya Klimova, Richard Trovato
  • Patent number: 6972294
    Abstract: Disclosed are novel compounds of formula (I) wherein A1, A2, Ar, R5, R6, R8, M, Q, Y, Z, k, m and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). Such conditions include diabetes and obesity.
    Type: Grant
    Filed: April 18, 2000
    Date of Patent: December 6, 2005
    Assignee: Novo Nordisk, A/S
    Inventors: Anthony Murray, Per Sauerberg, Lone Jeppesen, Ingrid Pettersson, Paul Stanley Bury
  • Publication number: 20040180885
    Abstract: Indole derivatives represented by formula (I): 1
    Type: Application
    Filed: March 8, 2004
    Publication date: September 16, 2004
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuhiko Torisu, Kaoru Kobayashi, Fumio Nambu
  • Patent number: 6781000
    Abstract: &agr;-ketoamide compounds useful for treating disorders mediated by 20S proteasome in mammals having the following formula: wherein X2 is Ar or Ar—X3 wherein X3 is is —C═O, or —CH2CO—, and wherein Ar is phenyl, substituted phenyl, indole, substituted indoles, and any other heteroaryls; R1, and R2 are each individually selected from the side chains of the known natural &agr;-amino acids and unnatural amino acids, hydrogen, 1-10 carbon linear and branched alkyl, 1-10 carbon linear and branched substituted alkyl, aryl, substituted aryl, 1-10 carbon linear, branched substituted aryl, alkoxyaryl, 3-8 carbon cycloalkyl, heterocycle substituted heterocycle, heteroaryl and substituted heteroaryl; X1 is selected from hydroxide, monoalkylamino, dialkylamino, alkoxide, arylkoxide and wherein X4 is hydroxide, arylamino, monoalkylamino, dialkylamino, alkoxide, or arylalkoxide; and R3 is selected from the known natural &agr;-amino acids, unnatural amino acids
    Type: Grant
    Filed: July 19, 1999
    Date of Patent: August 24, 2004
    Assignee: CV Theurapeutics, Inc.
    Inventors: Lisa Wang, Robert T. Lum, Steven R. Schow, Alison Joly, Suresh Kerwar, Michael M Wick
  • Publication number: 20040077798
    Abstract: In accordance with the present invention, there are provided novel thermosetting resin compositions which do not require solvent to provide a system having suitable viscosity for convenient handling. Invention compositions have the benefit of undergoing rapid cure. The resulting thermosets are stable to elevated temperatures, are highly flexible, have low moisture uptake and are consequently useful in a variety of applications, e.g., in adhesive applications since they display good adhesion to both the substrate and the device attached thereto.
    Type: Application
    Filed: January 13, 2003
    Publication date: April 22, 2004
    Inventors: Stephen M. Dershem, Puwei Liu
  • Publication number: 20030232988
    Abstract: Methods for making bis-heterocyclic compounds, especially bis-heterocyclic compounds having five and six-membered heterocyclic linkers are described. Also described are methods for making an alpha amino ketone synthon that enables facile syntheses of bisindole compounds, including topsentins and dragmacidins.
    Type: Application
    Filed: December 5, 2002
    Publication date: December 18, 2003
    Inventors: David A. Horne, Kenichi Yakushijin
  • Publication number: 20030220468
    Abstract: In accordance with the present invention, there are provided modified forms of nonsteroidal anti-inflamamatory drugs (NSAIDs). Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.
    Type: Application
    Filed: May 7, 2003
    Publication date: November 27, 2003
    Applicant: Medinox, Inc.
    Inventors: Ching-San Lai, Tingmin Wang
  • Publication number: 20030087902
    Abstract: Disclosed are substituted indoles, pharmaceutical compositions containing such indoles, and their use in treating or preventing PPAR-&ggr; mediated diseases or conditions, such as osteopenia, osteoporosis, cancer, diabetes and atherosclerosis.
    Type: Application
    Filed: October 9, 2001
    Publication date: May 8, 2003
    Inventors: Andreas Stolle, Jacques P. Dumas, William Carley, Philip D.G. Coish, Steven R. Magnuson, Yamin Wang, Dhanapalan Nagarathnam, Derek B. Lowe, Ning Su, William H. Bullock, Ann-Marie Campbell, Ning Qi, Jeremy L. Baryza, James H. Cook
  • Publication number: 20030004156
    Abstract: The present invention relates to novel dihydroindole and tetrahydroquinoline derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
    Type: Application
    Filed: December 11, 2001
    Publication date: January 2, 2003
    Inventors: Johannes Aebi, Jean Ackermann, Alexander Chucholowski, Henrietta Dehmlow, Olivier Morand, Sabine Wallbaum, Thomas Weller, Narendra Panday
  • Publication number: 20020198252
    Abstract: The present invention relates to a process of synthesizing alkylamine-substituted indoles, which are useful as intermediates in the preparation of compounds known to useful in the treatment of cancer and other diseases by inhibiting, regulating and/or modulating tyrosine kinase signal transduction.
    Type: Application
    Filed: May 22, 2002
    Publication date: December 26, 2002
    Inventor: Joseph Payack
  • Publication number: 20020198204
    Abstract: Disclosed are compounds of the formula 1
    Type: Application
    Filed: March 5, 2002
    Publication date: December 26, 2002
    Applicant: Neurogen Corporation, A Corporation of the State of Delaware
    Inventors: Pamela Albaugh, Gang Liu, Alan Hutchison
  • Publication number: 20020188138
    Abstract: The present invention is concerned with the acylation of indoles, specifically the preparation of 3-acylated indoles which may be further treated to provide indoles having an alternative substituent at the 3-position.
    Type: Application
    Filed: July 17, 2002
    Publication date: December 12, 2002
    Applicant: Pfizer Inc.
    Inventor: Jolyon Francis Perkins
  • Patent number: 6469065
    Abstract: The present invention describes novel nitrosated and/or nitrosylated &agr;-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated &agr;-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one &agr;-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: October 22, 2002
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, Joseph D. Schroeder, Inigo Saenez de Tejada, Ricky D. Gaston, Tatiana E. Shelekhin, Tiansheng Wang
  • Publication number: 20020151718
    Abstract: A method for preparing particular pyrrole-carboxamides which selectively bind to GABAa receptors; which comprises reacting 1,3-cycloalkanediones with bromoethylacetate followed by reaction of the resulting product with an acid halide followed by reaction with an aromatic amine and finally with an amonium source at an elevated temperature.
    Type: Application
    Filed: December 3, 2001
    Publication date: October 17, 2002
    Applicant: Pfizer Inc.
    Inventor: John A. Ragan
  • Patent number: 6413937
    Abstract: A combination of an agent which is a substrate for multidrug resistance related protein (MRP) and an inhibitor of MRP which is a nonsteroidal anti-inflammatory drug (NSAID) or a structural analogue thereof for simultaneous, sequential or separate use for increasing the potency of the substrate. The substrates include anti-cancer drugs and transition metal complexes. The combinations can be used to overcome the resistance to MRP substrates exhibited in many conditions, such as resistance to chemotherapy where patients have developed resistance, especially as a result of MRP over-expression to their chemotherapy.
    Type: Grant
    Filed: April 29, 1999
    Date of Patent: July 2, 2002
    Assignee: Dublin City University and Enterprise Ireland
    Inventor: Martin Michael Clynes
  • Patent number: 6297260
    Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.
    Type: Grant
    Filed: October 29, 1999
    Date of Patent: October 2, 2001
    Assignee: NitroMed, Inc.
    Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang
  • Patent number: 6291478
    Abstract: The present application relates to novel compounds belonging to the benzylaminodiacetamide family which have good anti-irritant and soothing properties. The invention also relates to their use in a composition comprising a physiologically acceptable medium, in particular in order to prevent and/or treat certain cutaneous disorders and more particularly in order to treat sensitive skins.
    Type: Grant
    Filed: March 13, 2000
    Date of Patent: September 18, 2001
    Assignee: L'Oreal
    Inventors: Jean-Baptiste Galey, Maria Dalko
  • Publication number: 20010012851
    Abstract: Nitric oxide releasing oxindole prodrugs are described which are useful in methods of treating or preventing pain, inflammation, fever, or gastrointestinal lesions in a patient in need of such treatment, or of modifying an inflammatory disease or condition by favorably affecting the outcome thereof in said patient, wherein there is administered to said patient a therapeutically effective amount of a compound of Formula (I): 1
    Type: Application
    Filed: July 29, 1999
    Publication date: August 9, 2001
    Inventors: KRISTIN M. LUNDY, MICHAEL T. CLARK
  • Patent number: 6066742
    Abstract: Indole derivatives shown by the formulae (1), (2a) and (2b) ##STR1## (wherein R.sup.1 is a protecting group for amino group; R.sup.2 is a protecting group for hydroxyl group; R.sup.3 is a protecting group for hydroxyl group; R.sup.4 is a C.sub.1 -C.sub.6 linear or branched lower alkyl group, or benzyl group), and pyrroloindole derivatives shown by formula (3) ##STR2## (wherein R.sup.1 is a protecting group for amino group; R.sup.2 is a protecting group for hydroxyl group; R.sup.3 is a protecting group for hydroxyl group; R.sup.4 is a C.sub.1 -C.sub.6 linear or branched lower alkyl group, or benzyl group), both of which are intermediates for duocarmycin SA, which is expected to be used as an anticancer agent, and derivatives thereof; and a method for producing the same.
    Type: Grant
    Filed: March 9, 1999
    Date of Patent: May 23, 2000
    Assignees: Kyorin Pharmaceutical Co., Ltd., Sagami Chemical Research Center
    Inventors: Yasumichi Fukuda, Shiro Terashima
  • Patent number: 6063807
    Abstract: Cyclo-oxygenase inhibitor and amidine derivative salts, preparation methods therefor, pharmaceutical compositions containing said salts and the use thereof particularly as NO synthase and cyclo-oxygenase inhibitors, are disclosed.
    Type: Grant
    Filed: January 6, 1998
    Date of Patent: May 16, 2000
    Assignee: Societe de Conseils de Recherches d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre Etienne Chabrier de Lassauniere, Colette Broquet
  • Patent number: 6011053
    Abstract: Antiatherosclerotic agents are provided having the structure: ##STR1## wherein R is a lower alkyl of 1-6 carbon atoms, ##STR2## wherein R.sub.5, R.sub.6, and R.sub.7 are lower alkyl of 1-6 carbon atoms; and R.sub.8, R.sub.9 and R.sub.10 are each, independently, hydrogen or halogen;R.sub.1 and R.sub.2 are each, independently, hydrogen or a lower alkyl of 1-6 carbon atoms; andR.sub.3 and R.sub.4 are each, independently, hydrogen, a lower alkyl of 1-6 carbon atoms or halogen;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 2, 1998
    Date of Patent: January 4, 2000
    Assignee: American Home Products Corporation
    Inventors: Robert J. Steffan, Amedeo A. Failli
  • Patent number: 5965745
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 AND R.sup.2 are as defined, useful in the treatment of asthma, rheumatoid arthritis, osteoarthritis, bronchitis, chronic obstructive airways diseases, psoriasis, allergic rhinitis, atopic dermatitis, shock, and other inflammatory diseases and for blocking the leucotriene D4 receptor, pharmaceutical compositions containing such compounds and methods of blocking leucotriene D4 receptors using such compositions.
    Type: Grant
    Filed: July 1, 1998
    Date of Patent: October 12, 1999
    Assignee: Pfizer Inc
    Inventors: Matthew F. Brown, Anthony Marfat
  • Patent number: 5952355
    Abstract: The present invention relates to propenone derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, or YR.sup.5 (wherein Y represents S or O; and R.sup.5 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or a substituted or unsubstituted cyclic ether residue); R.sup.2 and R.sup.3 independently represent hydrogen, lower alkyl, or substituted or unsubstituted aralkyl, or alternatively R.sup.2 and R.sup.3 are combined to form substituted or unsubstituted methylene or ethylene; R.sup.4 represents hydrogen, hydroxy, lower alkyl, substituted or unsubstituted aralkyl, lower alkoxy, substituted or unsubstituted aralkyloxy, or halogen; and X represents substituted or unsubstituted indolyl; or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 26, 1996
    Date of Patent: September 14, 1999
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Shun-Ichi Ikeda, Uichiro Kimura, Tadashi Ashizawa, Katsushige Gomi, Hiromitsu Saito, Masaji Kasai, Junji Kanazawa, Kimihito Sasaki, Etsuko Nukui, Masami Okabe, Soichiro Sato
  • Patent number: 5886191
    Abstract: The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.
    Type: Grant
    Filed: August 18, 1997
    Date of Patent: March 23, 1999
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
  • Patent number: 5877202
    Abstract: The present invention relates to novel indole derivatives useful in down-regulating estrogen receptor expression. Also included are methods for the treatment of neoplasms or of controlling the growth of a neoplasm in a patient afflicted with a neoplastic disease, especially estrogen-dependent neoplasms such as those associated with breast, ovarian and cervical tissue. Another embodiment of the present invention is a method of prophylactically treating a patient at risk of developing a neoplastic disease state. Also provided is a method for treating autoimmune diseases. Also included are pharmaceutical compositions of the novel indole derivatives.
    Type: Grant
    Filed: January 31, 1996
    Date of Patent: March 2, 1999
    Inventors: Alan J. Bitonti, Ian A. McDonald, Francesco G. Salituro, Jeffrey P. Whitten, Esa T. Jarvi, Paul S. Wright
  • Patent number: 5869518
    Abstract: Azacyloalkane derivatives of general formula ##STR1## in which: R.sub.1 and R.sub.2 represent a hydrogen atom, an alkyl group or a phenyl group, or R.sub.1 and R.sub.2 together form an oxo group, R.sub.3 represents a hydrogen atom or an alkyl group, or alternatively R.sub.3 forms a methylene group, R.sub.4 represents an aromatic group or, when R.sub.3 forms a methylene group, R.sub.4 represents a phenylene group in which one carbon atom is linked to Y and another carbon atom, adjacent to the preceding one, is linked to the said methylene group, R.sub.5 is either a group OR.sub.7, where R.sub.7 is a hydrogen atom or a benzyl group, or an N.sup.4 -methylpiperazinyl group, or alternatively a group NHR.sub.8 where R.sub.8 is a hydroxyl, pyridylmethyl or phenylmethyl group, A is an optionally substituted aromatic ring, n is equal to 1 or 2, X is CH, O or N, and Y is CH.sub.2, O or S, the process for preparing them and their applications in therapy.
    Type: Grant
    Filed: October 31, 1997
    Date of Patent: February 9, 1999
    Assignee: SYNTHELABO
    Inventors: Manuel Bedoya Zurita, Juan Antonio Diaz Martin, Gregorio del Sol Moreno, Ulpiano Martin Escudero Perez, Maria Dolores Jimenez Bargueno, Magali Romanach Ferrer