The Nitrogen Of The Z Radical Is Directly Bonded To A Benzene Ring Which Is Directly Bonded To The C(=o) Group Patents (Class 514/535)
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Patent number: 7510722Abstract: An aerosol tiny mist hazer apparatus. The apparatus has an aerosol can that contains about 10% by weight Methyl Anthranilate oil and about 90% by weight of an isobutane and propane propellant mixture. The apparatus has an aerosol valve with a vapor tap at the top and having a fine aerosol nozzle for producing a fine, evenly dispersed and stable haze having particle sizes less than 20 microns (in the form of a breathable haze) for use in maintaining birds flying away.Type: GrantFiled: May 6, 2005Date of Patent: March 31, 2009Inventor: Gary Crawford
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Publication number: 20090054485Abstract: A therapeutic method is provided to treat neutrophil-associated pulmonary diseases, such as chronic obstructive pulmonary disease, by locally administering to a mammal in need of such treatment, an effective amount of a topical anesthetic, such as lidocaine, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 8, 2008Publication date: February 26, 2009Inventors: Gerald J. Gleich, Loren W. Hunt, JR.
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Publication number: 20090048296Abstract: A transdermal topical anesthetic formulation, which can be used to ameliorate or inhibit neuropathic pain, has been developed. In the preferred embodiment, the topical anesthetic is a local anesthetic such as lidocaine, most preferably lidocaine free-base in a gel, and the dosage of the local anesthetic is effective in the painful area or immediately adjacent areas, to ameliorate or eliminate the pain. High concentration of local anesthetic in solution in the carrier is used to drive rapid release and uptake of the drug. Relief is typically obtained for a period of several hours.Type: ApplicationFiled: August 15, 2008Publication date: February 19, 2009Inventors: James N. Campbell, Arthur F. Michaelis
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Publication number: 20090041832Abstract: Transdermal drug delivery patches and methods of their production are described. The patches can be made such that the accommodate highly plasticizing drugs such as selegiline and/or the use of protonated forms of various drugs.Type: ApplicationFiled: September 29, 2008Publication date: February 12, 2009Inventors: Sharad K. Govil, Ludwig J. Weimann
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Publication number: 20090036491Abstract: A pharmaceutically delivery system and method of use therefor are described comprising a pharmaceutically active agent and acidified nitrite as an agent to produce local production of nitric oxide at the skin surface. The dosage form may be in any pharmaceutically acceptable carrier means and comprises an acidifying agent adapted to reduce the pH at the environment. In one embodiment, a barrier consisting of a membrane allows diffusions of the anaesthetic and nitrite ions while preventing direct contact of the skin and acidifying agent.Type: ApplicationFiled: September 3, 2008Publication date: February 5, 2009Inventors: Arthur T. Tucker, Nigel Benjamin
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Publication number: 20090023730Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.Type: ApplicationFiled: February 25, 2008Publication date: January 22, 2009Applicant: ACHILLION PHARMACEUTICALSInventors: Avinash Phadke, Dawei Chen, Milind Deshpande, Andrew Thurkauf, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
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Publication number: 20090012061Abstract: The present invention relates to a method of treating cellular proliferative diseases, in particular cancer, which comprises administering a modulator of the activity of the mitotic kinesin KSP, wherein the activity of the KSP modulator is dependent on the presence of microtubules. It is believed that the KSP modulators utilized in the instant method bind to the KSP protein in a previously unreported manner, since the compounds do not bind competitively with respect to either microtubules or ATP, the substrates of KSP. The modulators useful in the instant methods are furthermore not active against the non-microtubule stimulated activity of KSP. Cellular proliferative diseases that may be treated using the method disclosed herein are, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.Type: ApplicationFiled: September 9, 2005Publication date: January 8, 2009Inventors: Timothy A. Blizzard, Carolyn A. Buser-Doepner, Douglas E. Frantz, Kelly Hamilton, Myle Hoang, Ling Lee, Christopher R. Moyes, Jerry A. Murry, Arash Soheili
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Publication number: 20090012141Abstract: The present invention includes compound compositions and methods of making compounds that include an oligo-benzamide compound having at least two optionally substituted benzamides.Type: ApplicationFiled: March 13, 2008Publication date: January 8, 2009Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventor: Jung-Mo Ahn
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Publication number: 20080317729Abstract: This invention relates to ammonium salts and stable storable ammonium salts and ammonium salt/mineral salt clathrate compounds (inclusion compounds, clusters) having acid dibasic anionic acid residues such as bicarbonate, to methods for producing them and to pharmaco-medical and chemical synthetic applications for said compounds.Type: ApplicationFiled: July 20, 2005Publication date: December 25, 2008Inventors: Helmut Kasch, Uwe Reuter, Ralf Oettmeier
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Publication number: 20080306149Abstract: The present invention concerns a new use for a composition comprising chloroprocaine HCl, and in particular its use for the manufacture of a drug for intrathecal narcosis. The present invention also concerns a new composition comprising chloroprocaine HCl, being particularly suited to this new use, as well as a new method for manufacturing said composition.Type: ApplicationFiled: September 5, 2006Publication date: December 11, 2008Inventors: Augusto Mitidieri, Elisabetta Donati
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Patent number: 7459585Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: March 24, 2005Date of Patent: December 2, 2008Assignee: Ajinomoto Co., Inc.Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
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Publication number: 20080268050Abstract: Sprayable topical skin barriers for protecting and promoting healing of skin, and for providing comfort to a patient, comprise (i) a semi-solid hydrocarbon in a range by weight from about 25.0% to about 90.0%, (ii) a water-absorbing compound having a particle size range of about 0.5 microns to 20.0 microns, in a range by weight from about 5.0% to about 75.0%, and (iii) a solvent in a range by weight from about 10.0% to about 70.0%. The sprayable topical skin barriers have properties of effective adhesion to skin, protection from moisture and waste, transparency, sprayability, and smoothness to touch.Type: ApplicationFiled: April 30, 2007Publication date: October 30, 2008Inventors: Donald L. Gerrish, Charles E. Boyer
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Publication number: 20080255232Abstract: Compounds useful in the treatment of disorders characterized by deposits of amyloid aggregates are herein described together with pharmaceutical compounds containing the same. In particular the compounds of the present invention are those having the Formula (I) as reported below, where the radicals have the meaning indicated in the description.Type: ApplicationFiled: October 12, 2006Publication date: October 16, 2008Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.Inventors: Patrizia Minetti, Roberto Di Santo
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Publication number: 20080249107Abstract: Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols, indices and substituents have the following meaning R1?H, CN, NO2, CF3, F, Cl, Br, I, CH3 R2?H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl and either R1 or R2 must be H R3?H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl then X is e.g. with R4 being H, CH3, CH2CH3 or and Y being or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds of formulas (Ia) or (Ib). The compounds are applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.Type: ApplicationFiled: March 18, 2005Publication date: October 9, 2008Applicant: REVOTAR BIOPHARMACEUTICALS AGInventors: Remo Kranich, Ewald Mirko Aydt
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Publication number: 20080227859Abstract: The present invention relates to a tetrafluorobenzyl derivative and a pharmaceutical composition for prevention and treatment of acute and chronic neurodegenerative disease in central nervous system and ophthalmic diseases containing the same. The tetrafluorobenzyl derivative of the present invention can effectively be used to prevent and treat chronic neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and Huntington's disease, degenerative brain disease such as epilepsy and ischemic brain disease such as stroke.Type: ApplicationFiled: March 11, 2008Publication date: September 18, 2008Applicant: AmKor Pharma, Inc.Inventors: Byoung-Joo Gwag, Sung-Hwa Yoon, Ho-Sang Moon, Eun-Chan Park, Seok-Joon Won, Young-Ae Lee, Hae-Un Lee
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Publication number: 20080193492Abstract: This invention relates to novel compositions and methods of use by which the compositions of this invention are applied topically to one or more body parts of at least two individuals who bring said body parts into contact with the other individual and, when said body parts come into contact with each other, permit the formulations to interact and thereby achieve an unexpected sensation to each individual.Type: ApplicationFiled: August 21, 2007Publication date: August 14, 2008Inventors: Nawaz Ahmad, Cheng-Ji Cui, Bryant Ison
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Publication number: 20080166310Abstract: A regime or regimen for promoting and/or inducing and/or stimulating the pigmentation of keratin materials and/or for preventing and/or limiting the depigmentation and/or bleaching and/or for preventing and/or limiting the canities thereof, more particularly of human keratin fibers such as the hair, beard hair, moustache hair, the eyelashes and the eyebrows, includes administering to an individual in need of such treatment at least one 2-oxyacetamide compound of formula (I), or a salt and/or solvate thereof:Type: ApplicationFiled: December 10, 2007Publication date: July 10, 2008Applicant: L'OREALInventors: Roger Rozot, Philippe Breton, Michel Neuwels, Christophe Boulle
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Publication number: 20080145446Abstract: By providing a reusable support base or carrier which is constructed for being easily held by the user in the person's hand, and incorporating additives, therapeutic agents and/or medicinal components therein, a highly effective and easily employed, multi-purpose hand and/or skin cleaner, sanitizer, drug delivery, and exercise system is realized. Preferably, the support base or carrier is formed from soft, pliable, compressible and/or flexible material which is easily manipulated by the user in the person's hand or on the skin surface of other areas of the person's body. By employing selected additives or combinations thereof, a multi-purpose, highly effective, and unique hand or skin cleaning, sanitizing, and drug delivery system is realized in a system which also improves and enhances the individual's ability to obtain exercising of the hand.Type: ApplicationFiled: August 13, 2007Publication date: June 19, 2008Inventors: Chris Johnson, Drew O'Connell
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Publication number: 20080125424Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: July 10, 2007Publication date: May 29, 2008Inventors: Pierre DePrez, Sarah E. Lively, Taoues Temal
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Patent number: 7319160Abstract: The present invention relates to a tetrafluorobenzyl derivative and a pharmaceutical composition for prevention and treatment of acute and chronic neurodegenerative disease in central nervous system and ophthalmic diseases containing the same. The tetrafluorobenzyl derivative of the present invention can effectively be used to prevent and treat chronic neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and Huntington's disease, degenerative brain disease such as epilepsy and ischemic brain disease such as stroke.Type: GrantFiled: November 22, 2006Date of Patent: January 15, 2008Assignee: AmKor Pharma, Inc.Inventors: Byoung Joo Gwag, Sung Hwa Yoon, Ho Sang Moon, Eun Chan Park, Seok Joon Won, Young Ae Lee, Hae Un Lee
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Publication number: 20070264339Abstract: A stabilized semi-solid delivery vehicle contains a polyorthoester and an excipient, and a pharmaceutical composition contains an active agent, optionally a stabilizing agent, and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed.Type: ApplicationFiled: December 1, 2006Publication date: November 15, 2007Inventors: Devang Shah, John Barr, Brian Baxter, Jorge Heller
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Patent number: 7273887Abstract: The topical anesthetic formulation of the present invention is typically a solution that preferably includes lidocaine, USP as the active anesthetic ingredient with benzyl alcohol and isopropyl alcohol. This invention deals with problems commonly associated with topical application of local anesthetics such as: slow onset of action; need for occlusion; messiness of creams, ointments or gels; and rapid loss of effect due to rapid systemic dispersion. The invention permits enhanced penetration of the anesthetic and thereby allows for a lesser total dosage of pharmaceutically active ingredient. The use of a lesser total dosage also decreases systemic toxicity.Type: GrantFiled: October 23, 2000Date of Patent: September 25, 2007Assignee: Transdermatech, Inc.Inventor: Scott Wepfer
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Patent number: 7247654Abstract: The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel 3,4-disubstituted benzamidines and benzylamines, or a stereoisomer or pharmaceutically acceptable salt form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor Xa, factor XIa, factor IXa, and/or factor VIIa. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.Type: GrantFiled: June 1, 2004Date of Patent: July 24, 2007Assignee: Bristol-Myers Squibb CompanyInventors: E. Scott Priestley, Xiaojun Zhang
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Patent number: 7244848Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: January 24, 2006Date of Patent: July 17, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobs Jozef Backx
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Patent number: 7153869Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: March 12, 2004Date of Patent: December 26, 2006Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Patent number: 7135586Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: November 15, 2001Date of Patent: November 14, 2006Assignee: Janssen Pharmaceutica, NVInventors: Lieven Meerpoel, Leo Jacobs Jozef Backx
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Patent number: 7115767Abstract: The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by ghrelin including anorexia, cancer cachexia, eating disorders, age-related decline in body composition, weight gain, obesity, and diabetes mellitus.Type: GrantFiled: July 16, 2004Date of Patent: October 3, 2006Assignee: Abbott LaboratoriesInventors: Bo Liu, Gang Liu, Lissa T. J. Nelson, Jyoti R. Patel, Hing L. Sham, Zhili Xin, Hongyu Zhao
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Patent number: 7074820Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: April 23, 2001Date of Patent: July 11, 2006Assignee: AstraZeneca ABInventor: Thomas Antonsson
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Patent number: 7064229Abstract: The present invention relates to compounds of the general formula (I), processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory diseasesType: GrantFiled: June 24, 2002Date of Patent: June 20, 2006Assignee: Bayer Healthcare AGInventors: Thomas Rolle, Thomas Lehmann, Markus Albers, Gerhard Muller, Gerhard Hessler, Rudiger Fischer, Masaomi Tajimi, Karl Ziegelbauer, Kevin Bacon, Haruki Hasegawa, Hiromi Okigami
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Patent number: 7053245Abstract: This invention relates to N-acylamino aryl derivatives of the formula where R1, R21, R22, R23, R24, R3, R4, R5, R6, R7, R8, R, and n are as defined herein and where X is —CHRO, —OCHR—, —CH2S—, —SCH2—, —CH2CH2—, —CH?CH— or —C?C—. The compounds of the invention are selective monoamine oxidase B inhibitors, and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B, for example, for the treatment of Alzheimer's disease or senile dementia.Type: GrantFiled: May 5, 2004Date of Patent: May 30, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 6964982Abstract: The present invention provides compositions and methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death. The invention includes synthesis of 5-benzylamino salicylic acid (BAS) and its derivatives. BAS and its derivatives protect cortical neurons from toxic insults by N-methyl-D-aspartate, Zn2+, and reactive oxygen species. Thus, the present invention provides compositions and methods for treating stroke, traumatic brain and spinal cord injury, epilepsy, and neurodegenerative diseases that are accompanied by severe neuronal loss via excitotoxicity, Zn2+ neurotoxicity, and free radical neurotoxicity.Type: GrantFiled: July 29, 2002Date of Patent: November 15, 2005Assignee: Neurotech Co., Ltd.Inventors: Byoung Joo Gwag, Young Ae Lee, Bo Rum Ryu, Sung Hwa Yoon, Ho Sang Moon
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Patent number: 6964782Abstract: Disclosed are several preferred embodiments of hydrogen peroxide which are packaged with ease of use and extended shelf-life in mind. The embodiments include foam, mist, gel, and disposable towelette forms of H2O2. Optional ingredients of topical pain relievers and skin protectants are also disclosed, as are their methods of use.Type: GrantFiled: July 7, 2003Date of Patent: November 15, 2005Assignee: Tec Labs, Inc.Inventors: Robert Lee Smith, Steven Dale Smith, Wendy S. Langley, John Mark Christensen, Vernon W. Smith
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Patent number: 6958146Abstract: Various exemplary compounds, compositions and methods are disclosed. An exemplary composition includes an insecticide comprising a formula weight greater than approximately 220 and a compound comprising an insect stimulant and a formula weight less than approximately 220. An exemplary method includes applying an insecticide comprising a formula weight greater than approximately 220 and applying a compound comprising an insect stimulant and a formula weight less than approximately 220. Exemplary compounds optionally include semiochemicals of insects, plants and/or animals. Other exemplary compounds, compositions and/or methods are also disclosed.Type: GrantFiled: May 28, 2003Date of Patent: October 25, 2005Assignee: Bug Buster Ltd.Inventors: Leonard R. Askham, Charles F. Dunham, Leonard D. Felix, Jr.
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Patent number: 6951844Abstract: New thyroid receptor ligands are provided which have the general formula I wherein R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C3-7 cycloalkyl; R2 and R3 are each independently hydrogen, halogen, substituted or unsubstituted C1-4 alkyl, or substituted or unsubstituted C3-6 cycloalkyl, wherein at least one of R2 and R3 is other than hydrogen; R4 is a carboxylic acid selected from the group consisting of (CH2)nCOOH, (CH)2COOH, NHCO(CH2)nCOOH, CONH(CH2)nCOOH and NH(CH2)mCOOH; n is an integer from 0 to 4; and m is an integer from 1 to 4. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.Type: GrantFiled: September 21, 2004Date of Patent: October 4, 2005Assignee: Bristol Myers Squibb CompanyInventor: Jon J. Hangeland
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Patent number: 6949585Abstract: The present invention provides a compound which has cytokine production inhibitory activity and is useful for the treatment of diseases which is associated with cytokine. The compound is represented by the following general formula (I) [wherein A represents a cyclic group which may be substituted; the partial structure -DE- represents a group represented by —CH2CH2— or —CH?CH—; W represents a group represented by —CH2—, —CH2CH2—, —CH?CH— or —CH?; the partial structure >XY— represents a group represented by >CH—(CH2)n—, >C?CH—, >CH—CH2—CH(OH)—, >CH—CH2—C(?O)—, >CH—O— or >CH—O—CO—, provided that when W is —CH?, then XY— represents C—(CH2)p—; Z represents a divalent aliphatic hydrocarbon group; R1 and R2, which may be the same or different, each represents a hydrogen atom, or a hydroxyl, alkoxy or alkoxyalkoxy group; m is an integer of 0 or 1].Type: GrantFiled: April 1, 2002Date of Patent: September 27, 2005Assignee: Eisai Co., Ltd.Inventors: Yoshihito Eguchi, Ken-ichi Chiba, Masaki Goto, Hiroshi Obaishi, Yoshikazu Kuboi
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Patent number: 6949575Abstract: The present invention provides compounds of Formula (I) and a method of treating Alzheimer's disease using a compound of Formula (I), wherein: R1 and R2 include alkyl and phenylalkyl; R3 is hydrogen or alkyl; and R4 and R5 include alkyl, alkoxy, carboxyl, alkoxycarbonyl, and nitro. Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of Formula (I) and a method of imaging amyloid deposits using compounds of Formula (I).Type: GrantFiled: April 25, 2001Date of Patent: September 27, 2005Assignee: Pfizer Inc.Inventors: Nancy Sue Barta, Christopher Franklin Bigge
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Patent number: 6946474Abstract: The present invention provides trichloroethyl-sulfonylurea-containing compounds that inhibit glycing transporters, pharmaceutical compositions comprising such compounds, methods for using such compounds for inhibiting glycine transporters and methods for using such compounds for the treatment of disease states in which glycine is involved.Type: GrantFiled: September 13, 2001Date of Patent: September 20, 2005Assignee: Merck & Co., Inc.Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
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Patent number: 6943191Abstract: Disubstituted lavendustin A analogs that are PTK inhibitors having antiproliferative activity are described. Preferred compounds of the disclosure, without limitation, satisfy either Formula 1 or Formula 2. The present disclosure also provides pharmaceutical compositions comprising effective amounts of disubstituted lavendustin A analogs and potentially comprising other active ingredients, other materials conventionally used in the formulation of pharmaceutical compositions, and mixtures thereof. The compounds and compositions of the disclosure can be used for treating subjects to, for example, inhibit the proliferation of living cells in the treatment of proliferative diseases.Type: GrantFiled: February 24, 1999Date of Patent: September 13, 2005Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Venkatachala L. Narayanan, Edward A. Sausville, Gurmeet Kaur, Ravi K. Varma
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Patent number: 6921539Abstract: The invention provides therapeutic antimicrobial compositions and methods for their use based on natural organic phenolic compounds combined with pharmacological agents. The antimicrobial activities of each carvacrol and thymol are believed to be enhanced, while the pharmacological properties of procaine and related compounds are added to provide their unique properties to facilitate usefulness and effectiveness in humans. The therapeutic compositions are active against bacterial, fungal, and protozoan infections. The forms of the invention are intended to treat various internal infections through parenteral, subcutaneous, intradermal, intravenous, and intramuscular injections. They are also intended as useful agents to treat microbial infections that have become resistant to conventional anitibiotics as well as secondary opportunistic infections.Type: GrantFiled: February 18, 2003Date of Patent: July 26, 2005Inventor: Dusan Ninkov
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Patent number: 6916837Abstract: Amidino derivatives represented by the following general formula (I): {where X is a group represented by R1SO2NR2— (wherein R1 represents optionally substituted C6-14 aryl, etc. and R2 represents hydrogen atom, etc.), etc., Ar1 represents 2,6-naphthylene, etc., R3 represents hydrogen atom, etc. and Y represents carboxyphenyl, etc.} and their pharmacologically acceptable salts or solvates.Type: GrantFiled: November 14, 2002Date of Patent: July 12, 2005Assignee: Eisai Co., Ltd.Inventors: Takashi Satoh, Yasushi Okamoto, Osamu Asano, Nobuhisa Watanabe, Tadashi Nagakura, Takao Saeki, Atsushi Inoue, Masahiro Sakurai
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Patent number: 6897236Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 independently represent one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, or phenyl; R1 and R2 further represented by nitro and R3 by carboxy; R4 represents hydrogen, (C1-C3)alkyl, or allyl; Q represents a bond, or —C(R6)(R7)(—O—C?O)—, in which formula R6 and R7 independently represent hydrogen, trifluoromethyl, or (C1-C4)alkyl; Y represents either (C5-C15)alkyl, (C2-C15)olefinic group, (C3-C10)monocyclic hydrocarbon, or phenyl, any of which may be optionally substituted with one or more, same or different substituents represented by the formula R5; or (C1-C4)alkyl substituted with at least one or more substituents with the formula R5; or Y represents a group of formula —CH2—(Z—O)n—Z where Z is a (C1-C3)alkyl,Type: GrantFiled: July 11, 2000Date of Patent: May 24, 2005Assignee: Leo Pharmaceutical Products, Ltd.Inventors: Erik Rytter Ottosen, Heinz Wilhelm Dannacher
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Patent number: 6881756Abstract: The present invention relates to a method for reducing inflammation in the skin and/or treating inflammatory skin disorders, pain, or pruritis by topically applying a composition comprising totarol or a pharmaceutically-acceptable ester thereof.Type: GrantFiled: September 17, 2002Date of Patent: April 19, 2005Assignee: Johnson & Johnson Consumer Companies, Inc.Inventor: Gerard J. Gendimenico
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Patent number: 6861449Abstract: A therapeutic method is provided to treat neutrophil-associated pulmonary diseases, such as chronic obstructive pulmonary disease, by locally administering to a mammal in need of such treatment, an effective amount of a topical anesthetic, such as lidocaine, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 20, 2002Date of Patent: March 1, 2005Assignee: Mayo Foundation for Medical Education and ResearchInventors: Gerald J. Gleich, Loren W. Hunt, Jr.
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Patent number: 6844003Abstract: The invention relates to novel compounds of formula (I) wherein R1 represents a polymer, aryl or alkyl group, R2 presents a hydrogen atom, a halogen atom, a radical CN, CF3, OH, OCF3, COOH, R7, OR7 or OCOR7, R3 represents an aryl or alkyl halogen, R4 represents an alkyl radical. The invention also relates to a cosmetic composition comprising said compounds and to the use thereof to reduce and/or curb hair loss i.e.Type: GrantFiled: April 4, 2003Date of Patent: January 18, 2005Assignee: L'OrealInventors: Jean-Baptiste Galey, Maria Dalko, Lionel Breton
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Patent number: 6838472Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.Type: GrantFiled: September 17, 2002Date of Patent: January 4, 2005Assignee: Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
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Patent number: 6831102Abstract: New thyroid receptor ligands are provided which have the general formula I: wherein R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C3-7 cycloalkyl; R2 and R3 are each independently hydrogen, halogen, substituted or unsubstituted C1-4 alkyl, or substituted or unsubstituted C3-6 cycloalkyl, wherein at least one of R2 and R3 is other than hydrogen; R4 is a carboxylic acid selected from the group consisting of (CH2)nCOOH, (CH)2COOH, NHCO(CH2)nCOOH, CONH(CH2)nCOOH and NH(CH2)mCOOH; n is an integer from 0 to 4; and m is an integer from 1 to 4. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.Type: GrantFiled: December 6, 2002Date of Patent: December 14, 2004Assignee: Bristol-Myers Squibb CompanyInventor: Jon J. Hangeland
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Patent number: 6790866Abstract: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is —COR1, —CH═CH—COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4). The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.Type: GrantFiled: July 30, 2002Date of Patent: September 14, 2004Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Yuuki Nagao
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Publication number: 20040176290Abstract: Neonatal mice with classic inherited retinal degeneration (Pdebrd1/Pdebrd1) are disclosed which fail to mount reactive retinal neovascularization in a mouse model of oxygen-induced proliferative retinopathy. Also disclosed is a comparable human paradigm: spontaneous regression of retinal neovascularization associated with long-standing diabetes mellitus which occurs when retinitis pigmentosa becomes clinically evident. Both mouse and human data indicate that reactive retinal neovascularization either fails to develop or regresses when the number of photoreceptor cells is markedly reduced. The results show that a functional mechanism underlying this anti-angiogenic state is failure of the predicted up-regulation of vascular endothelial growth factor (VEGF), although other growth factors may also be involved. Preventive and therapeutic methods useful against both proliferative and degenerative retinopathies are also disclosed.Type: ApplicationFiled: May 11, 2004Publication date: September 9, 2004Inventors: Renata Pasqualini, Wadih Arap
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Patent number: 6787562Abstract: Compounds of the formula I; useful for the treatment of pain wherein A, Z, B, R1, X and D are as defined in the specification, methods of making such compounds, methods of using such compounds and pharmaceutical compositions containing such compounds.Type: GrantFiled: October 31, 2002Date of Patent: September 7, 2004Assignee: Zeneca Ltd.Inventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner