Z Or Y Radical Contains A Nitrogen Atom Patents (Class 514/534)
  • Patent number: 7781472
    Abstract: Disclosed herein are pharmaceutical compositions comprising oxybutynin, or a free base thereof or a pharmaceutically acceptable salt thereof, and pilocarpine, or a free base thereof or a pharmaceutically acceptable salt thereof. Also disclosed are methods of treating a patient suffering from overactive bladder comprising administering to the patient the above pharmaceutical composition.
    Type: Grant
    Filed: February 22, 2010
    Date of Patent: August 24, 2010
    Assignee: TheraVida, Inc.
    Inventor: Mehdi Paborji
  • Patent number: 7776918
    Abstract: The object of the present invention is to provide a pharmaceutical composition for preventing or treating viral infectious diseases. The compounds of the present invention have extremely potent anti-HCV activity and HCV growth inhibitory effects, and since they also only demonstrate mild cytotoxicity in vivo, a pharmaceutical composition containing the compound of the present invention is extremely useful as an anti-HCV preventive/therapeutic agent.
    Type: Grant
    Filed: February 12, 2004
    Date of Patent: August 17, 2010
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Masahiro Aoki, Hideyuki Kato, Masayuki Sudoh, Takuo Tsukuda, Miyako Masubuchi, Kenichi Kawasaki
  • Publication number: 20100196517
    Abstract: This invention generally relates to improvement of the body and skin appearance, for example enhancing the appearance of sagging, wrinkled, or cellulite-afflicted areas of the skin and body, through the local delivery of a nitric oxide donor, for example, using delivery vehicles such as lotions, creams, liquids, and/or transdermal patches. In some embodiments, a delivery vehicle containing a nitric oxide donor, for example, L-arginine (an important biological precursor) or its derivatives in a sufficient concentration to improve the appearance of a selected area of the body may be applied. In certain cases, one or more agents may also be included that aid in the transfer of the nitric oxide donor into the tissue, which may overcome the resistance to transfer into the skin. Non-limiting examples of suitable agents include agents able to create hostile biophysical environments, for instance, choline chloride, magnesium chloride, and/or sodium chloride.
    Type: Application
    Filed: April 15, 2010
    Publication date: August 5, 2010
    Applicant: Strategic Science & Technologies, LLC
    Inventor: Eric Thor Fossel
  • Publication number: 20100189818
    Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.
    Type: Application
    Filed: January 19, 2010
    Publication date: July 29, 2010
    Applicant: Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center
    Inventor: GUOCHUAN EMIL TSAI
  • Publication number: 20100184727
    Abstract: A muscarinic receptor antagonist is useful for the treatment or prevention of a condition associated with excess sebum production or excretion.
    Type: Application
    Filed: June 7, 2007
    Publication date: July 22, 2010
    Applicant: SUMMIT (CAMBRIDGE) LIMITED
    Inventors: Alan Geoffrey Roach, Paul Goldsmith
  • Publication number: 20100179218
    Abstract: Compounds of the following formula are disclosed: Methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of treating patients by administration of the pharmaceutical compositions are disclosed.
    Type: Application
    Filed: February 5, 2010
    Publication date: July 15, 2010
    Applicant: QLT Inc.
    Inventors: WILLIAM L. MATIER, Ghanshyam Patil
  • Publication number: 20100173970
    Abstract: Active compounds of Formula I are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.
    Type: Application
    Filed: February 23, 2010
    Publication date: July 8, 2010
    Inventor: S. Bruce King
  • Patent number: 7750045
    Abstract: 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: Grant
    Filed: August 17, 2005
    Date of Patent: July 6, 2010
    Assignee: Neurotech Pharmaceuticals Co., Ltd.
    Inventors: Byoung Joo Gwag, Young Ae Lee, Bo Rum Ryu, Sung Hwa Yoon, Ho Sang Moon
  • Publication number: 20100168232
    Abstract: The invention provides anticholinergic agents that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different as compared to the characteristics of the anticholinergic agent not attached to the water-soluble oligomer.
    Type: Application
    Filed: March 12, 2008
    Publication date: July 1, 2010
    Applicant: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
  • Publication number: 20100166674
    Abstract: A pharmaceutical composition for transdermal delivery comprising one or more physiologically active agents; one or more dermal penetration enhancers; and a volatile pharmaceutically acceptable carrier comprising a volatile solvent; and wherein the physiologically active agent and dermal penetration enhancer form an amorphous deposit upon evaporation of the volatile carrier, said amorphous deposit forming a reservoir within the stratum corneum; and (A) wherein the composition has a release rate profile of physiologically active agent so as to provide a ratio of the maximum concentration (Cmax) to the average concentration (Cavg) for the physiologically active agent over the dosage interval within the range of 1 to 10.
    Type: Application
    Filed: December 18, 2009
    Publication date: July 1, 2010
    Inventors: Timothy Matthias Morgan, Nina Frances Wilkins, Kathryn Taci-Jane Klose, Barrie Charles Finnin, Barry Leonard Reed
  • Publication number: 20100152704
    Abstract: Implant devices for intravesical administration and local drug delivery. The device has a body which includes a hollow tube formed of a biocompatible material; at least one reservoir in the tube which contains a drug; and one or more apertures through which the drug can be released. The device is configured for minimally invasive insertion into a body cavity, such as the bladder. The hollow tube may be elastomeric to permit the device to be elastically deformed from its initial shape into an elongated shape for passage through a catheter, where following such passage the device can return to or toward its initial shape to facilitate retention of the device in the body cavity. The body may have a narrow, elongated shape effective to permit insertion of the drug delivery device through a catheter without necessarily deforming the body, yet include flexible projections which effect retention within the body cavity.
    Type: Application
    Filed: February 22, 2010
    Publication date: June 17, 2010
    Applicants: MASSACHUSETTS INSTITUTE OF TECHNOLOGY, CHILDREN'S MEDICAL CENTER CORPORATION
    Inventors: Heejin Lee, Karen Daniel, Hong Linh Ho Duc, Michael J. Cima, Mario Castillo, Steven Froelich, Jordan Dimitrakov, Grace Y. Kim
  • Publication number: 20100144762
    Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
    Type: Application
    Filed: February 8, 2010
    Publication date: June 10, 2010
    Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
  • Patent number: 7718646
    Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: May 18, 2010
    Assignee: Sanofi-Aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
  • Publication number: 20100093854
    Abstract: The present invention is directed to a novel process for the preparation of (4-chloro-phenyl)-(3-trifluoromethyl-phenoxy)-acetic acid 2-acetylamino-ethyl ester, useful in the treatment of metabolic disorders and further to a process for the preparation of (4-chloro-phenyl)-(3-trifluoromethyl-phenoxy)-acetic acid, a synthesis intermediate.
    Type: Application
    Filed: April 3, 2009
    Publication date: April 15, 2010
    Inventors: Diego Broggini, Hartmut Burghard Zinser
  • Publication number: 20100093855
    Abstract: The present invention provides the use of (?)(3-trihalomethylphenoxy)(4-halophenyl)acetic acid derivatives and compositions in the treatment of insulin resistance, Type 2 diabetes, hyperlipidemia and hyperuricemia.
    Type: Application
    Filed: July 16, 2009
    Publication date: April 15, 2010
    Applicants: Metabolex, Inc., DiaTex, Inc.
    Inventors: Kenneth L. Luskey, Jian Luo
  • Publication number: 20100048550
    Abstract: The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta(TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.
    Type: Application
    Filed: October 15, 2007
    Publication date: February 25, 2010
    Inventors: Saurin Raval, Preeti Raval, Braj Lohray, Vidya Bhushan Lohray, Pankaj R. Patel
  • Patent number: 7666894
    Abstract: Disclosed herein are pharmaceutical compositions comprising oxybutynin, or a free base thereof or a pharmaceutically acceptable salt thereof, and pilocarpine, or a free base thereof or a pharmaceutically acceptable salt thereof. Also disclosed are methods of treating a patient suffering from overactive bladder comprising administering to the patient the above pharmaceutical composition.
    Type: Grant
    Filed: September 8, 2009
    Date of Patent: February 23, 2010
    Assignee: TheraVida, Inc.
    Inventor: Mehdi Paborji
  • Patent number: 7662861
    Abstract: The present invention provides compositions and methods for administering florfenicol to mammals. The compositions contain a prodrug of florfenicol in a pharmaceutically acceptable carrier. In one embodiment the prodrug is an esterized form of florfenicol. Examples of suitable prodrugs include one or a combination of one or a combination of the following: florfenicol acetate, florfenicol propionate, florfenicol butyrate, florfenicol pentanoate, florfenicol hexanoate, florfenicol heptanoate, florfenicol octanoate, florfenicol nanoate, florfenicol decanoate, florfenicol undecanoate, florfenicol dodecanoate, and florfenicol phthalate. In another embodiment the prodrug is converted into the florfenicol in vivo by the action of one or more endogenous esterases. The invention also provides new compounds, pharmaceutical compositions containing the compounds, and methods for their administration.
    Type: Grant
    Filed: January 31, 2007
    Date of Patent: February 16, 2010
    Assignee: IDEXX Laboratories, Inc.
    Inventors: Yerramilli V. S. N. Murthy, Robert H. Suva
  • Publication number: 20100010084
    Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of retinoids and retinoid-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: July 15, 2009
    Publication date: January 14, 2010
    Inventor: Chongxi Yu
  • Patent number: 7645793
    Abstract: The present invention relates to a process for suppressing the foaming which may occur at the time of the preparation of a solution or a suspension. Particularly, the present invention relates to pharmaceuticals, foods, and the like wherein the foaming at the time of the preparation of a solution or a suspension, which may cause any disadvantage, is suppressed.
    Type: Grant
    Filed: July 16, 2002
    Date of Patent: January 12, 2010
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yasuhiro Miyako, Hideaki Tai, Kazuichi Fujikane
  • Publication number: 20090326058
    Abstract: A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.
    Type: Application
    Filed: March 27, 2009
    Publication date: December 31, 2009
    Applicant: JAPAN TOBACCO INC.
    Inventors: YUKO SHINAGAWA, TERUHIKO INOUE, TOSHIHIRO KIGUCHI, TAKU IKENOGAMI, NAOKI OGAWA, KENJI FUKUDA, TAKASHI NAKAGAWA, MASANORI SHINDO, YUKI SOEJIMA
  • Publication number: 20090318509
    Abstract: Provided are compounds of formula (I) and other compounds. Also provided are pharmaceutical compositions comprising these compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal, and methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock.
    Type: Application
    Filed: June 4, 2007
    Publication date: December 24, 2009
    Inventor: Yousef Al-Abed
  • Patent number: 7632519
    Abstract: Described here are TRPV1 agonist compounds and their methods of synthesis and use. In addition to specifically identified compounds, capsaicin prodrugs, gemini dimers, and mutual prodrugs are also described. Formulations of the TRPV1 agonist compounds may be in the form of a liquid, tablets, capsules, gel, cream, emulsion, a patch, or the like. Methods for treating medical conditions using the compounds, compositions, or prodrugs described, are also provided.
    Type: Grant
    Filed: April 25, 2006
    Date of Patent: December 15, 2009
    Assignee: NeurogesX, Inc.
    Inventors: Gene Curtis Jamieson, Naweed Muhammad, Keith R. Bley
  • Publication number: 20090297591
    Abstract: The present invention is directed to compositions and methods for the transdermal delivery of a pharmaceutically active compound. In some embodiments, the addition of inert pharmaceutical ingredients in place of a portion of adhesive in a transdermal patch formulation increases the rate of skin permeation of a pharmaceutical compound.
    Type: Application
    Filed: May 14, 2009
    Publication date: December 3, 2009
    Applicant: Orient Pharma Co., Ltd.
    Inventors: Chin-Chih Chiang, Tse-Ching Lin, Remy Chen
  • Patent number: 7622460
    Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: November 24, 2009
    Assignee: sanofi-aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
  • Publication number: 20090264385
    Abstract: A stabilized bioadhesive composition containing an alkaline labile drug and a method for its preparation are provided. In one aspect, the composition is a hot-melt extruded (HME) composition comprising a preformed excipient mixture comprising an acidic component and an alkaline thermoplastic matrix-forming material, e.g. polymer. The excipient mixture is formed before blending with an alkaline labile drug. The blend is then hot-melt extruded to form the HME composition. By so doing, the acidic component is able to neutralize or render moderately acidic the excipient mixture. This particular process has been shown to substantially reduce the degradation of an alkaline labile drug during hot-melt extrusion. The excipient mixture softens or melts during hot-melt extrusion. It can dissolve or not dissolve drug-containing particles during extrusion.
    Type: Application
    Filed: March 22, 2007
    Publication date: October 22, 2009
    Inventors: Michael M. Crowley, Justin M. Keen, John J. Koleng, Feng Zhang
  • Publication number: 20090264525
    Abstract: The present invention relates to fatty acid esters of polyols or sulfonated fatty acid esters or sulfonated fatty acid amides containing at least one group Y, where Y stands for CF3—(CH2)a—O—, SF5—, CF3—(CH2)a—S—, CF3CF2S—, [CF3—(CH2)a]2N— or [CF3—(CH2)a]NH—, where a stands for an integer selected from the range from 0 to 5, or formula (I), where Rf stands for CF3—(CH2)r—, CF3—(CH2)r—O—, CF3—(CH2)r—S—, CF3CF2—S—, SF5—(CH2)t— or [CF3—(CH2)r]2N—, [CF3—(CH2)r]NH— or (CF3)2N—(CH2)r—, B stands for a single bond, O, NH, NR, CH2, C(O)—O, C(O), S, CH2—O, O—C(O), N—C(O), C(O)—N, O—C(O)—N, N—C(O)—N, O—SO2 or SO2—O, R stands for alkyl having 1 to 4 C atoms, b stands for 0 or 1 and c stands for 0 or 1, q stands for 0 or 1, where at least one radical from b and q stands for 1, and r stands for 0, 1, 2, 3, 4 or 5, to processes for the preparation of these compounds, and to uses of these surface-active compounds.
    Type: Application
    Filed: July 2, 2007
    Publication date: October 22, 2009
    Applicant: MERCK PATENT GMBH
    Inventors: Wolfgang Hierse, Nikolai (Mykola) Ignatyev, Martin Seidel, Elvira Montenegro, Peer Kirsch, Andreas Bathe
  • Patent number: 7605166
    Abstract: This application relates to methods and compositions for treating rheumatoid arthritis by administering a combination therapy comprising methotrexate and an antibody to alpha-4 integrin or an immunologically active antigen binding fragment in therapeutically effective amounts. The application also relates generally to methods and compositions for treating rheumatoid arthritis by administering a combination therapy comprising methotrexate and small molecule alpha-4 integrin antagonist that inhibits the alpha-4 integrin (?4 integrin) interaction with VCAM-1. The invention further relates to methods of preparing the compounds and methods of using the compounds and compositions.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: October 20, 2009
    Assignee: Elan Pharmaceuticals Inc.
    Inventors: Theodore A. Yednock, Stephen B. Freedman, Ivan Lieberburg, Michael A. Pleiss, Andrei W. Konradi, George Shopp, Elizabeth Messersmith
  • Publication number: 20090258887
    Abstract: The present invention is concerned with novel arylalkyl carboxylic acid derivatives, more specifically, with acylates of arylalkyl carboxylic acids with naturally occurring, non-toxic hydroxy, sulfhydryl, amino or imino compounds, and to compositions containing them. The compositions are preferably cosmetic preparations.
    Type: Application
    Filed: September 14, 2006
    Publication date: October 15, 2009
    Inventors: Raphael Beumer, Jochen Klock, Stefan Martin Stoeckli
  • Publication number: 20090247628
    Abstract: Disclosed herein are substituted phenylcyclohexylglycolate-based muscarinic acetylcholine receptor modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: March 23, 2009
    Publication date: October 1, 2009
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Publication number: 20090203759
    Abstract: The present invention relates to a pharmaceutical formulation comprising: a) one or more NO-releasing NSAID(s) of formula (I); b) one or more surfactants; c) a carbonyl scavenger compound selected from free acid forms, salts, carboxylic acid esters derivatives of a compound of formula (II) H2N—(CH2)m—(C6H4)—COOH??(II) wherein m=0-10; and d) optionally an oil or semi-solid fat and/or a short-chain alcohol.
    Type: Application
    Filed: June 29, 2006
    Publication date: August 13, 2009
    Inventors: Ulla Gasslander, Christina Holmberg
  • Patent number: 7563821
    Abstract: (2R)-2-Phenylcarbonyloxypropyl(2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided.
    Type: Grant
    Filed: December 4, 2006
    Date of Patent: July 21, 2009
    Assignee: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Xuedong Dai, Cindy X. Zhou, Jianhua Li, Mark Q. Nguyen
  • Publication number: 20090182033
    Abstract: Compounds of formula (I) have muscarinic M3 receptor modulating activity; formula (I) wherein R1 is C1-C6-alkyl or a hydrogen atom; and R2 is a hydrogen atom or a group -R5 or a group, -Z-Y—R5, or a group -Z-NR9R10, or a group -Z-N(R9)C(O)R11; and R3 is a lone pair, or C1-C6-alkyl; R4 is selected from one of the groups of formula (a), (b), (c) or (d); formulae (a), (b), (c), (d), Z is a C1-C16-alkylene, C2-C16-alkenylene or C2-C16-alkynylene group; Y is a bond or oxygen atom; R5 is an C1-C6-alkyl, aryl, arylalkyl; aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C1-C8-alkyl)-, heteroaryl(C1-C8-alkyl)-, cycloalkyl or heterocycloalkyl group; R6 is C1-C6-alkyl or a hydrogen atom; R7a and R7b area C1-C6-alkyl group or halogen; n and m are independently 0, 1, 2 or 3; R8a and R8b are independently selected from the group consisting of aryl, aryl-fused-heterocycloalkyl, heteroaryl, C1-C6-alkyl, cycloalkyl and hydrogen; R8c is —OH, C1-C6-alkyl, hydroxy-C1-C6-alkyl, or a hydrogen atom; R8d is C1-C6
    Type: Application
    Filed: December 14, 2006
    Publication date: July 16, 2009
    Applicant: ARGENTA DISCOVERY LTD.
    Inventors: Harry Finch, Nicholas Charles Ray, Monique Bodil Van Niel, Phillip Smith
  • Publication number: 20090176698
    Abstract: The invention relates to compositions comprising benzimidazolone derivatives of formula (I), optionally in form of the free base or in form of the pharmacologically acceptable acid addition salts thereof and methods of treating or preventing urinary incontinence, comprising the administration of a therapeutically effective amount of compound of formula (I), wherein R1, R2, R3, and R4 denote hydrogen or hydroxy with the proviso that R1, R2, R3, and R4 cannot simultaneously represent hydrogen, optionally in form of the free base or in form of the pharmacologically acceptable acid addition salts thereof.
    Type: Application
    Filed: February 16, 2007
    Publication date: July 9, 2009
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Wolfgang Baiker, Angelo Ceci
  • Publication number: 20090163487
    Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.
    Type: Application
    Filed: September 26, 2008
    Publication date: June 25, 2009
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Publication number: 20090163588
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
    Type: Application
    Filed: February 25, 2009
    Publication date: June 25, 2009
    Applicant: SMITHKLINE BEECHAM CORPORATION
    Inventors: Philip Stewart Turnbull, Rodolfo Cadilla, David John Cowan, Andrew Lamont Larkin, Istvan Kaldor, Eugene Lee Stewart
  • Publication number: 20090163457
    Abstract: The invention relates to codrugs having improved properties, methods for preparing and administering them, and methods of formulating and administering the codrugs as pharmaceutical preparations. In certain embodiments, the codrugs can be locally administered to deliver the constituent biologically active compound in a sustained-release fashion, reducing systemic concentrations of the biologically active compound.
    Type: Application
    Filed: November 26, 2008
    Publication date: June 25, 2009
    Applicant: pSivida, Inc.
    Inventors: Paul Ashton, Jianbing Chen, Hong Guo, Grazyna Cynkowska, Tadeusz Cynkowski
  • Patent number: 7550506
    Abstract: The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting.
    Type: Grant
    Filed: July 12, 2005
    Date of Patent: June 23, 2009
    Assignee: XenoPort, Inc.
    Inventors: Feng Xu, Mark A. Gallop, Vivek Sasikumar
  • Publication number: 20090156671
    Abstract: The present application describes deuterium-enriched oxybutynin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: February 10, 2009
    Publication date: June 18, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Publication number: 20090149534
    Abstract: Crystalline modifications of (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol, pharmaceutical compositions which contain these modifications, and the use thereof to treat pain or other conditions.
    Type: Application
    Filed: December 5, 2008
    Publication date: June 11, 2009
    Applicant: GRUENENTHAL GmbH
    Inventor: Michael Gruss
  • Publication number: 20090124669
    Abstract: Novel compounds for the prevention and treatment of dermatological disorders with an immunoallergic, hyperproliferative and inflammatory component, and a method of producing such compounds. The compounds are bioisosteres of substances with avenanthramide structures.
    Type: Application
    Filed: February 21, 2006
    Publication date: May 14, 2009
    Inventor: Carlo Ghisalberti
  • Publication number: 20090124690
    Abstract: The present invention relates to, in part, novel sulfate and bisphenol compounds useful for the recognition, attachment and growth of unwanted biologics on natural and manmade surfaces. Another aspect of the invention relates to combinatorial libraries for producing the same. Another aspect of the invention relates to pharmaceutical formulations comprising the same.
    Type: Application
    Filed: December 12, 2007
    Publication date: May 14, 2009
    Inventors: Randall S. Alberte, Robert D. Smith
  • Publication number: 20090124599
    Abstract: Fungicidal mixtures comprising, as active components 1) the strobilurin derivative of the formula I, and 2) at least one active compound II selected from the group of heterocyclic compounds in a synergistically effective amount, methods for controlling harmful fungi using mixtures of the compound I with active compounds II, the use of the compound I with active compounds II for preparing such mixtures and compositions comprising these mixtures.
    Type: Application
    Filed: December 21, 2005
    Publication date: May 14, 2009
    Applicant: Basf Aktiengesellschaft
    Inventors: Markus Gewehr, Reinherd Stierl, Matthis Niedenbrück, Udo Hünger
  • Publication number: 20090093510
    Abstract: The present invention relates to the use of nitric oxide releasing compounds for retarding or reversing muscular dystrophies such as Duchenne and Becker dystrophies.
    Type: Application
    Filed: January 23, 2007
    Publication date: April 9, 2009
    Inventors: Emilio Clementi, Giulio Cossu, Silvia Brunelli, Ennio Ongini
  • Publication number: 20090088438
    Abstract: Compounds of general formula I, and the salts and solvates thereof, wherein R1 represents the radical 2-benzoylphenylamino; R2 represents —(CH2)s—N(COR3)-A-J-T or —(CH2)s—N(R4)-B-J-T; and s, R3, R4, A, B, J and T have the meanings disclosed herein. These compounds are PPAR? modulators and, therefore, are useful for the treatment or prevention of a condition or a disease mediated by these receptors.
    Type: Application
    Filed: June 25, 2008
    Publication date: April 2, 2009
    Applicant: LABORATORIOS SALVAT, S.A.
    Inventors: Carmen SERRA COMAS, Anna FERNANDEZ SERRAT, Dolors BALSA LOPEZ, Isabel MASIP MASIP, Juan Lorenzo CATENA RUIZ, Jose HIDALGO RODRIGUEZ, Carmen LAGUNAS ARNAL, Carolina SALCEDO ROCA, Andres FERNANDEZ GARCIA
  • Publication number: 20090074887
    Abstract: There are described new active compound combinations of a compound of the formula (I) with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.
    Type: Application
    Filed: May 9, 2008
    Publication date: March 19, 2009
    Applicant: Bayer CropScience AG
    Inventors: Wilhelm Brandes, Heinz-Wilhelm Dehne, Stefan Dutzmann, Karl-Heinz Kuck, Bernd-Wieland Kruger
  • Publication number: 20090076144
    Abstract: The present application describes deuterium-enriched bazedoxifene, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 22, 2008
    Publication date: March 19, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Patent number: 7504431
    Abstract: Compounds of formula I its stereoisomers, solvates, and salts, thereof, wherein: a, b, c, d, f, n, m and Ra are defined herein are are inhibitors of calcium channel function, and are useful in treating calcium channel-dependent disorders, including hypertension.
    Type: Grant
    Filed: April 15, 2005
    Date of Patent: March 17, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jon J. Hangeland, Daniel L. Cheney, Todd J. Friends
  • Publication number: 20090062326
    Abstract: The present disclosure provides methods of treating a tumor using M3 muscarininc receptor antagonists, such as darifenacin. In some examples, the tumor expresses M3 muscarinic receptors, such as tumors associated with smoking. Also provided are compositions that can be used to practice such methods.
    Type: Application
    Filed: March 16, 2007
    Publication date: March 5, 2009
    Inventors: Eliot R. Spindel, Harmanjatinder Sekhon, Pingfang Song
  • Patent number: RE41151
    Abstract: In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflammatory drugs. 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: Grant
    Filed: August 20, 2008
    Date of Patent: February 23, 2010
    Assignee: Medinox, Inc.
    Inventors: Ching-San Lai, Tingmin Wang