C=x Bonded Directly To The Piperidine Ring (x Is Chalcogen) Patents (Class 514/330)
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Publication number: 20110136735Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 30, 2010Publication date: June 9, 2011Inventors: David BARNES, Gregory Raymond BEBERNITZ, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Herbert Franz SCHUSTER, Wei ZHANG
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Publication number: 20110118262Abstract: Disclosed are compounds of formula (I) and compositions of the present invention which are inhibitors of the sodium proton exchanger isoform-1 (NHE-I). Also disclosed are methods of using and making the same.Type: ApplicationFiled: June 24, 2009Publication date: May 19, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin Bentzien, Stephen James Boyer, Jennifer Burke, Anne Bettina Eldrup, Xin Guo, John David Huber, Thomas Martin Kirrane, Fariba Soleymanzadeh, Alan David Swinamer
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Publication number: 20110118314Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: October 15, 2010Publication date: May 19, 2011Inventor: Weiya Yun
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Publication number: 20110112099Abstract: The present invention provides therapeutic agents for a cancer resistant to a protease inhibitor which comprises, as an active ingredient, a benzoyl compound represented by formula (I): [wherein n represents an integer of 1 to 5; R1 represents substituted or unsubstituted lower alkyl, CONR7R8 (wherein R7 and R8, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like), or the like; R2 represents substituted or unsubstituted aryl or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R4 represents a hydrogen atom or the like; and R6 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like] or a pharmaceutically acceptable salt thereof as a heat shock protein 90 (Hsp90) family protein inhibitor, and the like.Type: ApplicationFiled: August 21, 2008Publication date: May 12, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Takayuki Nakashima, Yukimasa Shiotsu
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Patent number: 7939552Abstract: Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.Type: GrantFiled: March 29, 2006Date of Patent: May 10, 2011Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Kunihiko Higashiura, Takashi Ogino, Kazuhito Furukawa
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Publication number: 20110105485Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.Type: ApplicationFiled: July 21, 2010Publication date: May 5, 2011Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
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Publication number: 20110105506Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.Type: ApplicationFiled: May 28, 2010Publication date: May 5, 2011Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
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Publication number: 20110098322Abstract: The present invention provides compounds that can inhibit the activity of soluble epoxide hydrolases. In particular, the present invention provides compounds of Formula I.Type: ApplicationFiled: August 5, 2008Publication date: April 28, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: James R. Sanborn, Bruce D. Hammock, Sung Hee Hwang, Paul D. Jones, Christophe Morisseau
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Patent number: 7932269Abstract: The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3 and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.Type: GrantFiled: January 14, 2009Date of Patent: April 26, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Patent number: 7932267Abstract: The present invention provides methods for treating a flavivirus infection, including hepatitis C virus (HCV) infection, in an individual suffering from a flavivirus infection. In some embodiments, the methods involve administering to an individual in need thereof an effective amount of an agent that inhibits enzymatic activity of a membrane-bound ?-glucosidase inhibitor. In other embodiments, the methods involve administering to an individual in need thereof effective amounts of an ?-glucosidase inhibitor and at least one additional therapeutic agent.Type: GrantFiled: November 12, 2009Date of Patent: April 26, 2011Assignee: Intermune, Inc.Inventors: Lawrence M. Blatt, Hua Tan, Scott Seiwert
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Publication number: 20110091549Abstract: Methods and compositions relate to modulating the release profile of drug molecules from a hydrogel by controlling the kinetics of the pH transition of the hydrogel. The hydrogel is formed by in situ polymerization and includes a drug molecule having a pKa between the pH of the formed hydrogel and the physiologic environment in which the hydrogel is placed.Type: ApplicationFiled: March 16, 2010Publication date: April 21, 2011Inventors: Phillip Blaskovich, Rachit Ohri, Daniel S. Costa
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Publication number: 20110086818Abstract: The invention features methods, compositions, and kits for selective inhibition of pain-and itch sensing neurons (nociceptors and pruriceptors) by drug molecules of small molecule weight, while minimizing effects on non-pain-sensing neurons or other types of cells.Type: ApplicationFiled: March 11, 2009Publication date: April 14, 2011Applicants: Presidents and Fellows of Harvard College, The General Hospital CorporationInventors: Bruce P. Bean, Clifford J. Woolf
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Publication number: 20110071124Abstract: The present invention relates to compounds with activity as inhibitors of sAPP? and A? production, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease and pharmaceutical compositions containing such candidate compounds.Type: ApplicationFiled: August 18, 2010Publication date: March 24, 2011Applicant: The Trustees of Columbia University in the City of New YorkInventors: Tae-wan Kim, Donald W. Landry, Jeremy C. Hwang, Shi Xian Deng, Gangli Gong, Yuli Xie, Yidong Liu, Alison Rinderspacher
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Publication number: 20110065707Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof, wherein A1, A2, R1, R2, R3, R4, R5 and R6 have the significance given herein.Type: ApplicationFiled: September 3, 2010Publication date: March 17, 2011Inventors: Jean Ackermann, Aurelia Conte, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
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Patent number: 7906556Abstract: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.Type: GrantFiled: October 12, 2006Date of Patent: March 15, 2011Assignee: Elan Pharmaceuticals, Inc.Inventors: R. Jeffrey Neitz, Eric Tisdale, Barbara Jagodzinska, Anh Truong, Jay Tung
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Publication number: 20110059991Abstract: The present invention relates to the use of selective insecticidal compositions, characterized by an effective amount of an active compound combination comprising (a) (1) at least one haloalkylnicotinic acid derivative of the formula (I) in which AA and R1A are as defined in the description, or (2) at least one phthalic acid diamide of the formula (II) in which XB, R1B, R2B, R3B, L1B, L2B and L3B are as defined in the description, or (3) at least one anthranilamide of the formula (III) in which A1C, A2C, XC, R1C, R2C, R3C, R4C, R5C, R7C, R8C and R9C are as defined in the description, and (b) at least one crop plant compatibility-improving compound from the group of compounds given in the description, in particular cloquintocet-mexyl, isoxadifen-ethyl and mefenpyr-diethyl for controlling insects and/or arachnids, and a method for controlling insects and/or arachnids using the compositions.Type: ApplicationFiled: November 11, 2010Publication date: March 10, 2011Applicant: Bayer Cropscience AGInventors: Reiner Fischer, Rüdiger Fischer, Christian Funke, Achim Hense, Wolfram Andersch, Heike Hungenberg, Wolfgang Thielert, Udo Reckmann, Lothar Willms, Christian Arnold
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Patent number: 7902181Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: December 10, 2008Date of Patent: March 8, 2011Assignee: AstraZeneca ABInventors: Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
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Publication number: 20110053985Abstract: This invention relates to novel piperidine-4-carboxylic acid phenyl-alkyl-amide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: January 14, 2009Publication date: March 3, 2011Applicant: NEUROSEARCH A/SInventors: Dan Peters, John Paul Redrobe, Elsebet Ostergaard
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Publication number: 20110053904Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.Type: ApplicationFiled: August 19, 2010Publication date: March 3, 2011Inventors: Sabine Kolczewski, Emmanuel Pinard
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Publication number: 20110046156Abstract: Compositions and methods are provided for prophylactic or therapeutic treatment of a mammal for hearing or balance impairments involving neuronal damage, loss, or degeneration, by administration of a therapeutically effective amount of a redox-active therapeutic. Also provided are improved compositions and methods for treatments requiring administration of a pharmaceutical having an ototoxic side-effect in combination with a therapeutically effective amount of a redox-active therapeutic to treat the ototoxicity.Type: ApplicationFiled: March 4, 2009Publication date: February 24, 2011Inventor: Guy M. Miller
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Publication number: 20110046179Abstract: This invention relates to novel piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: August 29, 2007Publication date: February 24, 2011Inventors: Birgitte L. Eriksen, Dan Peters, Bjarne H. Dahl, Elsebet Østergaard Nielsen, John Paul Redrobe
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Publication number: 20110046181Abstract: Methods and compositions for systemically or locally administering by implantation a beneficial agent to a subject are described, and include, for example, depot gel compositions that can be injected into a desired location and which can provide controlled release of a beneficial agent over a short duration of time. The compositions include a low molecular weight biocompatible polymer, a biocompatible solvent having low water miscibility that forms a viscous gel with the polymer and limits water uptake by the implant, and a beneficial agent.Type: ApplicationFiled: September 27, 2010Publication date: February 24, 2011Inventors: Guohua Chen, David Priebe
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Publication number: 20110039819Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: April 9, 2009Publication date: February 17, 2011Inventors: Marion Hitchcock, Ingo Hartung
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Publication number: 20110039818Abstract: S1P receptor modulators or agonists are administered following a dosage regimen whereby during the initial days of treatment the daily dosage is lower than the standard daily dosage.Type: ApplicationFiled: December 22, 2009Publication date: February 17, 2011Inventor: Eric Legangneux
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Publication number: 20110034417Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: ApplicationFiled: October 5, 2010Publication date: February 10, 2011Applicant: Adolor CorporationInventors: Bertrand Le Bourdonnec, Roland E. Dolle
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Patent number: 7879898Abstract: Methods are provided for treating chronic obstructive pulmonary diseases such as emphysema using compounds that activate the signaling pathways of hepatocyte growth factor.Type: GrantFiled: February 12, 2007Date of Patent: February 1, 2011Assignee: Angion Biomedica Corp.Inventor: Yanchun He
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Publication number: 20110021506Abstract: This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceutical compositions and kits comprising the compounds and salts, uses of the compounds and salts to make medicaments, and treatments comprising the administration of the compounds and salts to animals in need of the treatments.Type: ApplicationFiled: December 16, 2008Publication date: January 27, 2011Applicant: INTERVET INTERNATIONAL B.V.Inventors: Christophe Pierre Alain Chassaing, Jörg Schröder, Thomas Simon Ilg, Manfred Uphoff, Thorsten Meyer
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Publication number: 20110020324Abstract: A compound having an ability to bind to an S1P receptor (particularly EDG-6, preferably EDG-1 and EDG-6), for example, the compound represented by formula (I) of the present invention, a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like. wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.Type: ApplicationFiled: September 10, 2010Publication date: January 27, 2011Applicant: ONO PHARMACEUTICAL CO., LTDInventors: Shinji NAKADE, Hirotaka Mizuno, Takeji Ono, Masashi Minami, Hiroshi Saga, Hiroshi Hagiya, Takaki Komiya, Hiromu Habashita, Haruto Kurata, Kazuhiro Ohtsuki, Kensuke Kusumi
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Publication number: 20110020450Abstract: The present invention relates to a titratable dosage transdermal delivery system for systemic delivery of a therapeutic agent or drug. The system comprises a plurality of patch units that are connected along one or more borders. The plurality of patch units are divisible into units along the one or more borders having one or more lines of separation. Each patch unit is surrounded by a border. The therapeutic patch has at least a backing layer and a therapeutic agent comprising layer. The dosage of therapeutic agent delivered to a patient is proportional to the number of patch unit applied per treatment. The system enables systemic administration of a titratable dosage of therapeutic agent, adjustable by the patient under the direction of a physician, through the skin or mucosa. Moreover, the invention relates to a method of making the titratable dosage transdermal delivery system.Type: ApplicationFiled: September 30, 2010Publication date: January 27, 2011Inventor: Curtis Wright, IV
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Publication number: 20110015229Abstract: A method for treating subjects experiencing neuropathic pain is provided. The method involves the application of a solid-forming local anesthetic formulation to a skin surface of the subject experiencing the neuropathic pain and then maintaining the formulation on the skin surface for a period of time sufficient to allow itself to transdermally deliver the local anesthetic to the subject thereby providing relief from the neuropathic pain within about 45 minutes.Type: ApplicationFiled: January 5, 2010Publication date: January 20, 2011Inventors: Jie Zhang, Robert Lippert
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Publication number: 20110014258Abstract: The present invention provides a coating comprising a bioactive material and an antimicrobial agent, wherein the concentration of said antimicrobial agent varies throughout the thickness of the coating.Type: ApplicationFiled: February 27, 2009Publication date: January 20, 2011Applicant: SMITH & NEPHEW, INC.Inventors: Lu Gan, Marcus L. Scott, Shilesh C. Jani, Laura S. Whitsitt
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Publication number: 20110014127Abstract: Described herein are methods for effectively and accurately measuring a patient response upon administration of one or more drugs to the patient. The methods are more sensitive than current methodologies. Also described herein are compositions comprising an analgesic and a sufficient amount of an antihistamine to enhance the analgesic properties of the analgesic. With respect to these compositions, the methods described herein are useful for evaluating qualities of pain, definite improvement, and one or more bodily functions of a subject afflicted with pain. The compositions described herein are useful in improving the quality of pain in a subject or a bodily function of a subject afflicted with pain or definite improvement of a subject afflicted with pain.Type: ApplicationFiled: January 5, 2009Publication date: January 20, 2011Inventor: Bernard P. Schachtel
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Patent number: 7872028Abstract: Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated. levels of renin activity or in the treatment of aspartic protease mediated disorders. Also described is a method for the use of the diaminopropanols in ameliorating or treating renin related disorders in a subject in need thereof.Type: GrantFiled: April 5, 2007Date of Patent: January 18, 2011Assignee: Vitae Pharmaceuticals, Inc.Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty
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Publication number: 20110009451Abstract: The present invention relates to novel anesthetic compositions containing a non-polymeric carrier material and an anesthetic, where the compositions are suitable for providing a sustained local anesthesia without an initial burst and having a duration for about 24 hours or longer. Certain compositions are also provided that include a first anesthetic and a second anesthetic. In such compositions, the second anesthetic is a solvent for the first anesthetic and provides an initial anesthetic effect upon administration to a subject. The non-polymeric carrier may optionally be a high viscosity liquid carrier material such as a suitable sugar ester. The compositions can further include one or more additional ingredients including active and inactive materials. Methods of using the compositions of the invention to produce a sustained anesthetic effect at a site in a subject are also provided. Preferably the composition contains bupivacaine and a sugar ester such as saib.Type: ApplicationFiled: September 15, 2005Publication date: January 13, 2011Inventor: Neil A Verity
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Patent number: 7868009Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I): and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: January 27, 2006Date of Patent: January 11, 2011Assignee: Merck Serono, S.A.Inventors: Dominique Swinnen, Jerome Gonzalez
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Publication number: 20110002992Abstract: The present invention relates to N-sulfonylated amino acid derivatives, where an aryl radical is linked via the sulfonyl group N-terminally to the amino acid and a radical which comprises at least one imino group and at least one further basic group which represents an optionally modified amino, amidino or guanidino group is linked C-terminally via the carbonyl group. The invention likewise relates to processes for preparing these compounds and to their use, in particular as inhibitors of matriptase.Type: ApplicationFiled: July 1, 2010Publication date: January 6, 2011Applicant: The Medicines Company (Leipzig) GmbHInventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz, Anne Stürzebecher, Kerstin Uhland
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Publication number: 20110003784Abstract: Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.Type: ApplicationFiled: June 16, 2010Publication date: January 6, 2011Inventors: David S. Garvey, Gregory J. LaRosa, Jeremy R. Greenwood, Mark L. Brewer, Tan Quach, Jamie B. Côté, Judd Berman
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Publication number: 20100331354Abstract: The present invention relates to pharmaceutical compositions for intranasal administration to a mammal that contain an effective amount of an opioid, a liquid nasal carrier for the opioid, and optionally a sweetener, flavoring agent or masking agent. In some embodiments of the present invention, the pharmaceutical compositions have improved bioavailability. In other embodiments of the present invention, the opioid compositions improve patient compliance.Type: ApplicationFiled: May 28, 2010Publication date: December 30, 2010Inventor: Daniel P. Wermeling
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Publication number: 20100331332Abstract: The invention is directed to a method of treating addiction to drugs of abuse in a subject, comprising administering a therapeutically effective amount of a cabamoyl compound, or pharmaceutically acceptable salt or ester thereof.Type: ApplicationFiled: June 26, 2009Publication date: December 30, 2010Applicant: SK HOLDINGS CO., LTD.Inventors: Sung James Lee, Susan Marie Melnick
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Patent number: 7858624Abstract: Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.Type: GrantFiled: April 5, 2007Date of Patent: December 28, 2010Assignee: Vitae Pharmaceuticals, Inc.Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh
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Patent number: 7858649Abstract: This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are of the general formula (I) and include any of its stereoisomers, any mixture of its stereoisomers, and pharmaceutically acceptable salts thereof. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.Type: GrantFiled: October 12, 2006Date of Patent: December 28, 2010Assignee: Neurosearch A/SInventors: William Dalby Brown, Janus S. Larsen, Lene Teuber, David Tristram Brown, Philip K. Ahring, Naheed Mirza, Elsebet Østergaard Nielsen
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Publication number: 20100324052Abstract: The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin.Type: ApplicationFiled: August 12, 2010Publication date: December 23, 2010Inventors: Olivier Bezencon, Christoph Boss, Daniel Bur, Austin Chih-Yu Chen, Olivier Corminboeuf, Daniel Dube, Walter Fischli, Corinna Grisostomi, Lubos Remen, Sylvia Richard-Bildstein, Thierry Sifferlen, Michel Therien, Thomas Weller
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Publication number: 20100324075Abstract: Compounds, pharmaceutical compositions, and their methods of use in raising serum HDL levels in subjects in need thereof are provided. Also provided are compounds, pharmaceutical compositions, and their methods of use in increasing reverse cholesterol transport in subjects in need thereof. Finally, methods for treating disease by raising serum HDL levels and increasing reverse cholesterol transport are provided.Type: ApplicationFiled: December 19, 2008Publication date: December 23, 2010Applicant: UNIVERSITY OF CINCINNATIInventors: David Y. Hui, Philip N. Howles
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Publication number: 20100317697Abstract: Disclosed are compounds having the formula (I): wherein the R1, R2, R3, X, Y, A, L, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.Type: ApplicationFiled: June 20, 2008Publication date: December 16, 2010Inventors: John J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, Damiano Ghirlanda, Alexey V. Ishchenko, Lara S. Kallander, Brian Lawhorn, Qing Lu, Gerard McGeehan, Beth A. Knapp-Reid, Simon Semus, Robert D. Simpson, Suresh B. Singh, Lamont R. Terrell, Colin Tice, Tritin Tran, Zherong Xu, Jing Yuan, Wei Zhao, Yongdong Y. Zhao
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Publication number: 20100318040Abstract: The present invention includes a catheter locking solution having both antimicrobial and anticoagulant properties including a local anesthetic and a viscosifying agent. The local anesthetic of the present invention may be an amino amide; an amino ester; an aminoacylanilide; an aminoalkyl benzoate; an amino carbonate; an N-phenylamidine compound; an N-aminoalkyl amid; an aminoketone, or combinations and mixtures thereof. In a particular embodiment of the present invention, the local anesthetic is tetracaine or dibucaine.Type: ApplicationFiled: June 9, 2010Publication date: December 16, 2010Applicant: BECTON, DICKINSON AND COMPANYInventors: John J. Kelley, III, Thelma I. Valdes
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Publication number: 20100311665Abstract: Composition and methods of treating pain and reducing or reversing tolerance to opiate analgesics are disclosed. The composition and method utilize an opiate analgesic and an endothelin antagonist as active agents to treat pain in mammals, including humans.Type: ApplicationFiled: August 2, 2010Publication date: December 9, 2010Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventor: Anil Gulati
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Publication number: 20100311782Abstract: Novel 3,4-disubstituted-4-(3-carbamoylphenyl)-piperidinylpropanoic acid compounds and their salts, including pharmaceutically acceptable salts, pharmaceutical compositions and methods of their use are disclosed. The novel compounds are useful, inter alia, as antagonists of opioid receptors.Type: ApplicationFiled: June 7, 2010Publication date: December 9, 2010Applicant: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec
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Publication number: 20100311753Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.Type: ApplicationFiled: June 24, 2010Publication date: December 9, 2010Applicant: ChemoCentryx, Inc.Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay P. Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
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Publication number: 20100305160Abstract: The present invention relates to compositions and methods use in pain reduction, including but not limited to, peripheral nerve blocks. In particular, the present invention relates to compositions and methods for the administration of perineural dexmedetomidine and ropivacaine in combination for increased antinociception in peripheral nerve blocks. In addition, this invention relates to any use of dexmedetomidine alone or in combination with other agents for the purpose of decreasing inflammation around peripheral nerves, thereby decreasing the potential for peripheral nerve injury. Further, the invention relates to the use of dexmedetomidine to reduce inflammation in the muscle to lessen or prevent muscle damage.Type: ApplicationFiled: June 1, 2010Publication date: December 2, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventor: Chad M. Brummett
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Publication number: 20100305090Abstract: The invention relates to meta-substituted phenyl sulfonyl amides of secondary amino acid amides according to the general formula (I), (II), or (III), the production thereof, and the use thereof as matriptase inhibitors, in particular the use thereof as drugs for inhibiting tumor growth and/or metastasization.Type: ApplicationFiled: March 5, 2008Publication date: December 2, 2010Inventors: Torsten Steinmetzer, Andrea Schweinitz, Daniel Donnecke