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)
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Patent number: 8865130Abstract: 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: GrantFiled: March 27, 2012Date of Patent: October 21, 2014Assignee: Vanderbilt UniversityInventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
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Publication number: 20140256781Abstract: 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: ApplicationFiled: May 20, 2014Publication date: September 11, 2014Applicant: ICEUTICA PTY LTD.Inventors: Aaron Dodd, Felix Meiser, Marck Norret, Adrian Russell, H. William Bosch
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Patent number: 8541398Abstract: 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: GrantFiled: February 11, 2010Date of Patent: September 24, 2013Assignee: Antibe Therapeutics Inc.Inventors: John L. Wallace, Giuseppe Cirino, Vincenzo Santagada, Giuseppe Caliendo
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Publication number: 20130178466Abstract: 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: ApplicationFiled: November 9, 2010Publication date: July 11, 2013Applicant: BIOCOPEA LIMITEDInventors: Robin Mark Bannister, Wilson Caparros Wanderlay, John Brew
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Publication number: 20130158070Abstract: 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: ApplicationFiled: September 6, 2011Publication date: June 20, 2013Inventor: Taher Nassar
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Publication number: 20130065934Abstract: 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: ApplicationFiled: March 4, 2011Publication date: March 14, 2013Applicant: CATABASIS PHARMACEUTICALS, INC.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Publication number: 20130052138Abstract: 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: ApplicationFiled: March 27, 2012Publication date: February 28, 2013Applicant: Vanderbilt UniversityInventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
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Publication number: 20130040884Abstract: Novel polypeptide derivatives having protracted profile of action.Type: ApplicationFiled: March 22, 2012Publication date: February 14, 2013Inventors: Jesper Lau, Thomas Kruse Hansen, Kjeld Madsen, Paw Bloch, Florencio Zaragoza Dorwald, Nils Langeland Johansen
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Patent number: 8362027Abstract: 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: GrantFiled: August 8, 2011Date of Patent: January 29, 2013Assignees: Kowa Co., Ltd., Tokyo University of Science Educational Foundation Administrative OrganizationInventors: Toshio Inagi, Makoto Kanebako, Hiroshi Terada, Kimiko Makino, Masakazu Toi
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Publication number: 20120010168Abstract: 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: ApplicationFiled: November 3, 2009Publication date: January 12, 2012Inventors: Jeffrey Laskin, Diane Heck, Mou-Tuan Huan, Karine Fabio, C. Jeffrey Lacey, Sherri Young, Pramod Mohanta, Christophe Guillon, Ned Heindel
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Publication number: 20110269722Abstract: 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: ApplicationFiled: December 23, 2010Publication date: November 3, 2011Inventor: Apparao Satyam
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Publication number: 20110263526Abstract: 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: ApplicationFiled: April 22, 2011Publication date: October 27, 2011Applicant: PIRAMAL LIFE SCIENCES LIMITEDInventor: Apparao SATYAM
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Publication number: 20110253944Abstract: 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: ApplicationFiled: December 23, 2009Publication date: October 20, 2011Applicant: LUMINANO CO., LTD.Inventors: Sung Hwan Han, Cheon Gyu Cho
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Patent number: 8034824Abstract: 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: GrantFiled: October 11, 2006Date of Patent: October 11, 2011Assignees: Kowa Co., Ltd., Tokyo University of Science Educational Foundation Administrative OrganizationInventors: Toshio Inagi, Makoto Kanebako, Hiroshi Terada, Kimiko Makino, Masakazu Toi
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Publication number: 20110230524Abstract: 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: ApplicationFiled: November 27, 2009Publication date: September 22, 2011Inventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko, Pavel Mikhailovich Yamanushkin, Oleg Dmitrievich Mitkin, Vladimir Yurievich Vvedensky, Vadim Vasilievich Bichko
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Publication number: 20110150873Abstract: 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: ApplicationFiled: December 10, 2008Publication date: June 23, 2011Applicant: CAMBRIDGE ENTERPRISE LIMITEDInventor: David John Grainger
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Publication number: 20110118455Abstract: 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: ApplicationFiled: November 19, 2010Publication date: May 19, 2011Applicant: FUJITSU LIMITEDInventor: Tsuyoshi FUJIHARA
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Publication number: 20100292289Abstract: The present invention relates to the treatment of metabolic syndrome or disorders associated with metabolic syndrome comprising administering a compound of the invention.Type: ApplicationFiled: November 26, 2008Publication date: November 18, 2010Applicant: AMPLA Pharmaceuticals Inc.Inventor: James R. Hauske
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Publication number: 20100210607Abstract: 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: ApplicationFiled: February 11, 2010Publication date: August 19, 2010Applicant: ANTIBE THERAPEUTICS INC.Inventors: JOHN WALLACE, GIUSEPPE CIRINO, VINCENZO SANTAGADA, GIUSEPPE CALIENDO
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Patent number: 7741359Abstract: 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: GrantFiled: July 18, 2007Date of Patent: June 22, 2010Assignee: Antibe Therapeutics Inc.Inventors: John Wallace, Giuseppe Cirino, Vincenzo Santagada, Giuseppe Caliendo
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Publication number: 20100152272Abstract: 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: ApplicationFiled: February 17, 2010Publication date: June 17, 2010Applicant: BEZWADA BIOMEDICAL, LLCInventor: Rao S. Bezwada
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Publication number: 20100016597Abstract: 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: ApplicationFiled: September 24, 2009Publication date: January 21, 2010Applicant: Activus Pharma Co., Ltd.Inventors: Takashi Hirokawa, Takahiro Tada
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Publication number: 20090281063Abstract: 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: ApplicationFiled: October 11, 2006Publication date: November 12, 2009Applicants: KOWA CO., LTD., TOKYO UNIVERSITY OF SCIENCE EDUCATIONAL FOUNDATION ADMINISTRATIVE ORGANIZATIONInventors: Toshio Inagi, Makoto Kanebako, Hiroshi Terada, Kimiko Makino, Masakazu Toi
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Patent number: 7553865Abstract: 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: GrantFiled: July 22, 2003Date of Patent: June 30, 2009Assignee: Kowa Company, Ltd.Inventors: Hiroyuki Shirai, Tatsuya Nakai, Masami Serizawa, Yasuo Shinoda, Toshio Inagi
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Publication number: 20090155903Abstract: 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: ApplicationFiled: March 21, 2005Publication date: June 18, 2009Applicant: Myriad Genetics, IncorporatedInventors: Rachel M. Slade, Warren S. Weiner, Eric Delmar, Yevgeniya Klimova, Richard Trovato
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Patent number: 6972294Abstract: 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: GrantFiled: April 18, 2000Date of Patent: December 6, 2005Assignee: Novo Nordisk, A/SInventors: Anthony Murray, Per Sauerberg, Lone Jeppesen, Ingrid Pettersson, Paul Stanley Bury
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Publication number: 20040180885Abstract: Indole derivatives represented by formula (I): 1Type: ApplicationFiled: March 8, 2004Publication date: September 16, 2004Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Kazuhiko Torisu, Kaoru Kobayashi, Fumio Nambu
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Patent number: 6781000Abstract: &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 acidsType: GrantFiled: July 19, 1999Date of Patent: August 24, 2004Assignee: CV Theurapeutics, Inc.Inventors: Lisa Wang, Robert T. Lum, Steven R. Schow, Alison Joly, Suresh Kerwar, Michael M Wick
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Publication number: 20040077798Abstract: 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: ApplicationFiled: January 13, 2003Publication date: April 22, 2004Inventors: Stephen M. Dershem, Puwei Liu
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Publication number: 20030232988Abstract: 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: ApplicationFiled: December 5, 2002Publication date: December 18, 2003Inventors: David A. Horne, Kenichi Yakushijin
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Publication number: 20030220468Abstract: 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: ApplicationFiled: May 7, 2003Publication date: November 27, 2003Applicant: Medinox, Inc.Inventors: Ching-San Lai, Tingmin Wang
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Publication number: 20030087902Abstract: 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: ApplicationFiled: October 9, 2001Publication date: May 8, 2003Inventors: 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
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Publication number: 20030004156Abstract: 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: ApplicationFiled: December 11, 2001Publication date: January 2, 2003Inventors: Johannes Aebi, Jean Ackermann, Alexander Chucholowski, Henrietta Dehmlow, Olivier Morand, Sabine Wallbaum, Thomas Weller, Narendra Panday
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Publication number: 20020198204Abstract: Disclosed are compounds of the formula 1Type: ApplicationFiled: March 5, 2002Publication date: December 26, 2002Applicant: Neurogen Corporation, A Corporation of the State of DelawareInventors: Pamela Albaugh, Gang Liu, Alan Hutchison
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Publication number: 20020198252Abstract: 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: ApplicationFiled: May 22, 2002Publication date: December 26, 2002Inventor: Joseph Payack
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Publication number: 20020188138Abstract: 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: ApplicationFiled: July 17, 2002Publication date: December 12, 2002Applicant: Pfizer Inc.Inventor: Jolyon Francis Perkins
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Patent number: 6469065Abstract: 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: GrantFiled: September 1, 1999Date of Patent: October 22, 2002Assignee: NitroMed, Inc.Inventors: David S. Garvey, Joseph D. Schroeder, Inigo Saenez de Tejada, Ricky D. Gaston, Tatiana E. Shelekhin, Tiansheng Wang
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Publication number: 20020151718Abstract: 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: ApplicationFiled: December 3, 2001Publication date: October 17, 2002Applicant: Pfizer Inc.Inventor: John A. Ragan
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Patent number: 6413937Abstract: 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: GrantFiled: April 29, 1999Date of Patent: July 2, 2002Assignee: Dublin City University and Enterprise IrelandInventor: Martin Michael Clynes
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Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
Patent number: 6297260Abstract: 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: GrantFiled: October 29, 1999Date of Patent: October 2, 2001Assignee: 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: 6291478Abstract: 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: GrantFiled: March 13, 2000Date of Patent: September 18, 2001Assignee: L'OrealInventors: Jean-Baptiste Galey, Maria Dalko
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Publication number: 20010012851Abstract: 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): 1Type: ApplicationFiled: July 29, 1999Publication date: August 9, 2001Inventors: KRISTIN M. LUNDY, MICHAEL T. CLARK
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Patent number: 6066742Abstract: 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: GrantFiled: March 9, 1999Date of Patent: May 23, 2000Assignees: Kyorin Pharmaceutical Co., Ltd., Sagami Chemical Research CenterInventors: Yasumichi Fukuda, Shiro Terashima
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Patent number: 6063807Abstract: 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: GrantFiled: January 6, 1998Date of Patent: May 16, 2000Assignee: Societe de Conseils de Recherches d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Etienne Chabrier de Lassauniere, Colette Broquet
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Patent number: 6011053Abstract: 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: GrantFiled: September 2, 1998Date of Patent: January 4, 2000Assignee: American Home Products CorporationInventors: Robert J. Steffan, Amedeo A. Failli
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Patent number: 5965745Abstract: 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: GrantFiled: July 1, 1998Date of Patent: October 12, 1999Assignee: Pfizer IncInventors: Matthew F. Brown, Anthony Marfat
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Patent number: 5952355Abstract: 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: GrantFiled: November 26, 1996Date of Patent: September 14, 1999Assignee: 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
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Patent number: 5886191Abstract: 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: GrantFiled: August 18, 1997Date of Patent: March 23, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
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Patent number: 5877202Abstract: 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: GrantFiled: January 31, 1996Date of Patent: March 2, 1999Inventors: Alan J. Bitonti, Ian A. McDonald, Francesco G. Salituro, Jeffrey P. Whitten, Esa T. Jarvi, Paul S. Wright
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Patent number: 5869518Abstract: 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: GrantFiled: October 31, 1997Date of Patent: February 9, 1999Assignee: SYNTHELABOInventors: Manuel Bedoya Zurita, Juan Antonio Diaz Martin, Gregorio del Sol Moreno, Ulpiano Martin Escudero Perez, Maria Dolores Jimenez Bargueno, Magali Romanach Ferrer