Additional Hetero Ring Patents (Class 514/397)
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Publication number: 20110294668Abstract: Disclosure is provided for methods of preventing, removing or inhibiting microbial biofilm formation or microbial infection in a plant or plant part thereof, including applying thereto a treatment effective amount of an active compound as described herein, or an agriculturally acceptable salt thereof. Methods of enhancing a microbicide (e.g., including a copper, antibiotic, bacteriophage, etc.) and/or plant defense activator are also provided, including applying an active compound as described herein. Compositions comprising an active compound as described herein in an agriculturally acceptable carrier are also provided, and in some embodiments the compositions further include a microbicide (e.g., including copper, antibiotic, bacteriophage, etc.) and/or plant defense activator.Type: ApplicationFiled: December 7, 2009Publication date: December 1, 2011Applicant: NORTH CAROLINA STATE UNIVERSITYInventors: Christian Melander, John Cavanagh, David F. Ritchie, Steven A. Rogers, Robert W. Huigens, III
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Publication number: 20110294819Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: ApplicationFiled: December 21, 2010Publication date: December 1, 2011Inventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
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Patent number: 8067455Abstract: The present invention provides a prodrug of propofol and crystalline forms thereof, methods of making the propofol prodrug and crystalline forms thereof, pharmaceutical compositions of the propofol prodrug and crystalline forms thereof, methods of using the propofol prodrug and crystalline forms thereof and pharmaceutical compositions thereof to treat diseases or disorders such as headache pain, post-chemotherapy or post-operative surgery nausea and vomiting, neurodegenerative disorders, and mood disorders.Type: GrantFiled: October 2, 2009Date of Patent: November 29, 2011Assignee: XenoPort, Inc.Inventors: Feng Xu, Mark A. Gallop, Vivek Sasikumar, Usha Dilip
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Publication number: 20110286961Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: December 1, 2010Publication date: November 24, 2011Inventors: Makonen Belema, Jeffrey Lee Romine, Van N. Nguyen, Gan Wang, Omar D. Lopez, Denis R. St. Laurent, Qi Chen, John A. Bender, Zhong Yang, Piyasena Hewawasam, Ningning Xu, Nicholas A. Meanwell, John A. Easter, Bao-Ning Su, Michael J. Smith
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Publication number: 20110288040Abstract: The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like.Type: ApplicationFiled: August 5, 2011Publication date: November 24, 2011Applicant: Takeda Pharmaceutical Company LimitedInventors: Atsushi Hasuoka, Terufumi Takagi, Masahiro Kajino, Haruyuki Nishida
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Patent number: 8063090Abstract: The present invention relates to diphenylmethyl imidazole mineralocorticoid receptor modulators compounds having the structure and their use in treating cardiovascular events.Type: GrantFiled: March 19, 2008Date of Patent: November 22, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Philip E. Brandish, James C. Hershey, Mark E. Fraley, Justin T. Steen
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Publication number: 20110280909Abstract: Methods and systems are described for a rapid and sustainable change in the pigment melanin content of melanocytes of the iris stroma, thereby to change the color of the eye. Also described are nanoparticle compositions for lightening the pigmented tissues or treating a pigmented tissue related disease.Type: ApplicationFiled: January 29, 2010Publication date: November 17, 2011Inventor: Kambiz Thomas Moazed
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Publication number: 20110281875Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: July 8, 2011Publication date: November 17, 2011Inventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
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Publication number: 20110280824Abstract: The present disclosure provides copolymers including a first monomer including at least one phospholipid possessing at least one vinyl group and a second monomer including a furanone possessing vinyl and/or acrylate groups. Compositions, medical devices, and coatings including such copolymers are also provided.Type: ApplicationFiled: July 26, 2011Publication date: November 17, 2011Applicant: Tyco Healthcare Group LPInventor: Joshua B. Stopek
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Publication number: 20110281910Abstract: This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: November 9, 2010Publication date: November 17, 2011Inventors: Rico Lavoie, John A. Bender, Jeffrey Lee Romine, Edward H. Ruediger, Carol Bachand, Omar D. Lopez, Qi Chen, Makonen Belema, John F. Kadow, Lawrence G. Hamann
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Patent number: 8058269Abstract: There is provided compounds of the formula wherein R6, V, W, X, Y, Q and n are as described. The compounds exhibit activity as anticancer agents.Type: GrantFiled: September 17, 2007Date of Patent: November 15, 2011Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Song Yang, Jing Zhang, Zhuming Zhang
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Patent number: 8058303Abstract: Provided is a pharmaceutical composition for external use which includes the following components: 1) luliconazole and/or a salt thereof; 2) N-methyl-2-pyrollidone; and 3) benzyl alcohol and/or diester of a dibasic acid. The diester of the dibasic acid is a diethyl ester or a diisopropyl ester of a dibasic acid having 6-10 carbon atoms. The pharmaceutical composition is useful for the treatment of a mycotic disease such as foot trichophytosis, trichophytosis corporis, trichophytosis on a hard keratin or hyperkeratotic portion, onychomycosis, particularly on a nail, or dermatomycosis.Type: GrantFiled: October 2, 2006Date of Patent: November 15, 2011Assignees: Nihon Nohyaku Co, Ltd, Pola Pharma IncInventors: Toyohiko Miki, Hiroyuki Fujii, Akira Nozawa, Hirokazu Kobayashi
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Publication number: 20110275684Abstract: The present invention relates to novel benzotriazole derivatives, efficacious in animal models of CNS disorders and, as such, valuable candidates for the prevention or treatment of CNS (Central Nervous System) diseases or disorders. In other aspects the invention relates to pharmaceutical compositions comprising the benzotriazole derivatives of the invention and to the use of these compounds for therapeutic applications.Type: ApplicationFiled: January 18, 2010Publication date: November 10, 2011Applicant: NEUROSEARCH A/SInventors: Antonio Nardi, Helle Kirstein Erichsen, Dan Peters, Karin de Linde Troelsen
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Publication number: 20110275625Abstract: Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).Type: ApplicationFiled: November 5, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Shuang Liang, Sabine Schlyer, Lana Louise Smith Keenan, Steven John Taylor, Bernd Wellenzohn, Dieter Wiedenmayer, Zhaoming Xiong, Qiang Zhang
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Publication number: 20110274648Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: November 4, 2010Publication date: November 10, 2011Inventors: Rico Lavoie, John A. Bender, Zhong Yang, Makonen Belema, Omar D. Lopez, Qi Chen, Gan Wang, Piyasena Hewawasam
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Patent number: 8053457Abstract: The invention relates to 3-heterocyclyl indolyl compounds of formula I capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively: wherein R1, R2, R3, R4, RA, Y and Y are as defined in the specification. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.Type: GrantFiled: March 27, 2008Date of Patent: November 8, 2011Assignee: Novartis AGInventors: Andreas Boettcher, Nicole Buschmann, Pascal Furet, Jean-Marc Groell, Jorg Kallen, Joanna Hergovich Lisztwan, Keiichi Masuya, Lorenz Mayr, Andrea Vaupel
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Publication number: 20110269742Abstract: Disclosed are Serotonin 5-HT2B receptor inhibitors of the formula I. Also disclosed are methods of making and methods of using these compounds.Type: ApplicationFiled: December 14, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Derek Cogan, Neil Moss, Christopher Ronald Sarko, Samantha Jayne Bamford, Pui Leng Loke, Spencer Charles R. Napier, Heather Tye, Mark Whittaker
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Publication number: 20110269769Abstract: The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.Type: ApplicationFiled: June 4, 2009Publication date: November 3, 2011Inventors: Linus S. Lin, Marc D. Chioda, Ping Liu, Ravi P. Nargund
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Publication number: 20110268697Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: July 6, 2011Publication date: November 3, 2011Inventors: Soojin Kim, Qi Gao, Fukang Yang
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Publication number: 20110262517Abstract: Described herein are methods of inhibiting angiogenesis, and treating or preventing a disease or disorder (or symptoms thereof) associated with angiogenesis, wherein an anti-angiogenesis compound is administered to a subject.Type: ApplicationFiled: April 7, 2008Publication date: October 27, 2011Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Jun O. Liu, Curtis R. Chong, Jing Xu, Jun Lu, Shridhar Bhat
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Publication number: 20110263668Abstract: The present invention relates to the field of cardiology. More specifically, the present invention relates to the use of ?3 adrenoreceptor agonists to treat cardiac hypertrophy and heart failure. In a specific embodiment, a method for treating cardiac hypertrophy comprises the step of administering a therapeutically effective amount of a ?3 adrenoreceptor agonist to a patient diagnosed with cardiac hypertrophy. In a more specific embodiment, the method for treating cardiac hypertrophy comprises the step of administering a therapeutically effective amount of the ?3 adrenoreceptor agonist BRL 26830A to a patient diagnosed with cardiac hypertrophy. In a further embodiment, the present invention provides a method for treating a cardiovascular disease or condition associated with cardiac hypertrophy comprising the step of administering a therapeutically effective amount of a ?3 adrenoreceptor agonist to a patient diagnosed with cardiac hypertrophy.Type: ApplicationFiled: July 1, 2010Publication date: October 27, 2011Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Lili Ayala Barouch, David A. Kass, An L. Moens
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Publication number: 20110263614Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.Type: ApplicationFiled: March 14, 2011Publication date: October 27, 2011Inventors: Roger Bonnert, Rukhsana Mohammed, Mark Robert Dickinson
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Publication number: 20110263619Abstract: The present invention relates to use of an inhibitor of the renin-angiotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF).Type: ApplicationFiled: December 1, 2010Publication date: October 27, 2011Inventors: Bernward Schölkens, Norbert Bender, Badrudin Rangoonwala, Gilles Dagenais, Hertzel Gerstein, Anders Ljunggren, Salim Yusuf
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Publication number: 20110257199Abstract: Novel dicationic terphenyl compounds and their aza analogues. Methods for combating microbial infections with novel dicationic terphenyl compounds and their aza analogues. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues.Type: ApplicationFiled: June 17, 2011Publication date: October 20, 2011Inventors: Richard R. Tidwell, David W. Boykin, W. David Wilson, Reto Brun, Karl Werbovetz, Mohamed A. Ismail, Reem K. Arafa, Laixing Hu
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Publication number: 20110256097Abstract: Methods are provided for treating a subject for a condition. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is modulated during at least one predetermined phase of the subject's menstrual cycle to alter the parasympathetic activity/sympathetic activity ratio in a manner that is effective to treat the subject for the condition. The subject methods find use in the treatment of a variety of different conditions, including various disease conditions, that increase in severity and/or occurrence during one or more phases of the menstrual cycle. Also provided are systems and kits for use in practicing the subject methods.Type: ApplicationFiled: June 27, 2011Publication date: October 20, 2011Inventors: Yun Anthony Joonkyoo, Patrick Yuarn-Bor Lee
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Publication number: 20110257235Abstract: The present disclosure relates to certain new and known triazolium and/or imidazolium salts and to their therapeutic use, for example in methods of treating or preventing an infection by a Plasmodium or Babesia parasite in a subject in need thereof. The triazolium and imidazolium salts are compounds of the Formula (I) or (II): wherein R1-R4, R1?-R3?, R8-R11, X, X?, X?, Y, Y? and Y? are as defined in the disclosure.Type: ApplicationFiled: September 4, 2009Publication date: October 20, 2011Inventors: Ian E. Crandall, Walter A. Szarek, Jason Z. Vlahakis
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Patent number: 8039452Abstract: An object of the present invention is to provide a medicinal composition useful for external application in the treatment of a fungal infection reaching the lower part of a thick keratin layer. Provided is an antifungal medicinal composition, comprising: (1) a film-forming agent; (2) a water-soluble plasticizer in a form of a solid or a paste at 20° C. at 1 atm; and (3) an antifungal compound represented by a general formula (1) and/or a physiologically acceptable salt thereof.Type: GrantFiled: June 10, 2003Date of Patent: October 18, 2011Assignee: Pola Pharma Inc.Inventors: Hideaki Sasagawa, Madoka Ito, Takuji Nakashima, Akira Nozawa
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Publication number: 20110251146Abstract: A topical, foamable composition is provided that includes at least one antifungal agent that is able to penetrate the upper layers of skin and is retained in or on an area to be treated for a prolonged period of time, and that has a residual non-volatile component content less than 25%. In addition, a method of treating fungal diseases including jock itch, tinea, dandruff and sebborheic dermatitis is provided, and includes applying to the affected area of patient requiring such treatment an antifungal composition.Type: ApplicationFiled: June 21, 2011Publication date: October 13, 2011Applicant: STIEFEL RESEARCH AUSTRALIA PTY LTDInventors: Greg DAVEY, Albert Zorko ABRAM
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Publication number: 20110251233Abstract: The invention provides a formulation for transmucosal administration of at least one active ingredient from the setron family, the formulation comprising said active ingredient in base form and/or in salt form, a hydroalcoholic solution titrating at least 30° alcohol, and optionally a pH correcting agent, said active principle being present in the state of stable and complete dissolution in the hydroalcoholic solution. The invention also provides a method of preparing this formulation and its use for the treatment and prevention of major nausea and/or vomiting syndromes, and also for the treatment and prevention of digestive spasms.Type: ApplicationFiled: December 17, 2009Publication date: October 13, 2011Inventors: Philippe Perovitch, Marc Maury
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Publication number: 20110251251Abstract: The invention relates to a crystalline polymorph of a pharmaceutically acceptable salt of an optically active anti-fungal imidazole compound of formula (III), the pharmaceutical and agricultural compositions containing such polymorph, its use in the treatment or prevention of skin or mucous membrane infections caused by fungi or yeasts in humans or pets, and its use in the treatment or prevention of agricultural diseases produced by such infectious agents.Type: ApplicationFiled: December 9, 2009Publication date: October 13, 2011Applicant: FERRER INTERNACIONAL, S.AInventors: Mónica Delgardo, Carles Albet, Inés Petschen, Marta Tarruella
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Publication number: 20110251168Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: June 16, 2011Publication date: October 13, 2011Inventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
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Publication number: 20110251246Abstract: The invention provides methods for the identification of small molecules that inhibit MUC1 oligomerization, and the functions flowing therefrom. In addition, small molecules that prevent MUC1 oligomerization are disclosed. Identified molecules will find use in treating a variety of MUC1-related inflammatory conditions, including MUC1-related cancers.Type: ApplicationFiled: March 10, 2011Publication date: October 13, 2011Inventors: Donald W. Kufe, Surender Kharbanda
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Publication number: 20110251249Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: June 22, 2011Publication date: October 13, 2011Applicant: THERAVANCE, INC.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20110244051Abstract: Disclosed herein are pharmaceutical compositions comprising a plurality of first beads each comprising: a core; a first layer comprising pilocarpine or a pharmaceutically acceptable salt thereof; and a second layer comprising a first polymer. Also disclosed are pharmaceutical compositions comprising a plurality of second beads each comprising: a core; and a first layer comprising tolterodine or a pharmaceutically acceptable salt thereof. Further disclosed are pharmaceutical formulations comprising: a) a plurality of the first beads; b) a plurality of the second beads; or c) a plurality of the first beads and a plurality of the second beads.Type: ApplicationFiled: April 1, 2011Publication date: October 6, 2011Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Roger S. FLUGEL
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Publication number: 20110245294Abstract: Disclosed herein are methods of treating a patient suffering from overactive bladder (OAB) comprising administering to the patient a combination of antimuscarinic or anticholinergic agent and muscarinic agonist for the treatment of poor quality of sleep in the OAB patient.Type: ApplicationFiled: April 1, 2011Publication date: October 6, 2011Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Roger S. FLUGEL
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Publication number: 20110245265Abstract: Methods to treat or prevent acute kidney injury and chronic kidney injury in subjects using CXCR4 antagonists are disclosed.Type: ApplicationFiled: August 28, 2009Publication date: October 6, 2011Applicant: GENZYME CORPORATIONInventors: Anna Zuk, Steven Ledbetter, Nibedita Chattopadhyay
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Patent number: 8030339Abstract: This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. 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: October 4, 2011Assignee: 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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Patent number: 8030343Abstract: Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with an ?-(3,4-disubstituted phenyl)alkyl group and in the 4- and/or 5-position with a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF? and phosphodiesterase. A typical embodiment is 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4,5-diaminoisoindoline-1,3-dione.Type: GrantFiled: October 14, 2003Date of Patent: October 4, 2011Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller
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Publication number: 20110237636Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: September 24, 2010Publication date: September 29, 2011Inventors: Makonen Belema, Piyasena Hewawasam
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Publication number: 20110237579Abstract: The invention relates to non-macrocyclic, non-peptidic, substituted heterocyclic compounds useful for inhibiting hepatitis C virus (“HCV”) replication, particularly functions of the non-structural 5A (“NS5A”) protein of HCVType: ApplicationFiled: December 2, 2009Publication date: September 29, 2011Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20110237563Abstract: The present invention related to the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with critical buccal condition, leading to difficulties in swallowing oral medicine forms and thus difficulties in treating said illnesses. Particularly, the present invention discloses the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with dysphagia and/or odynophagia and/or aspiration risk. Another aspect of the present invention is the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for the treatment of dysphagia and/or odynophagia and/or aspiration risk.Type: ApplicationFiled: March 23, 2010Publication date: September 29, 2011Inventor: Dominique Costantini
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Patent number: 8026266Abstract: Compositions, and methods of use thereof, are provided for the treatment of painful neuropathy by local or topical delivery of compounds that interact with ?-adrenergic receptors, especially an alpha2 adrenergic agonist such as clonidine, to the entire painful area such that the need for systemic dosing is minimized. The compounds are delivered to or adjacent to painful areas in patients with painful length dependent neuropathy, and other neuropathies that affect the pain signaling fibers in the skin. A preferred compound for the treatment of patients with length dependent neuropathy is clonidine applied in a transdermal patch, gel, ointment, lotion, liposomal formulation, cream, or emulsion, wherein the concentration is sufficient to provide an effective dose in the painful area or immediately adjacent areas.Type: GrantFiled: November 7, 2006Date of Patent: September 27, 2011Assignee: Arcion Therapeutics, Inc.Inventor: James N. Campbell
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Publication number: 20110229571Abstract: Pharmaceutical compositions containing selective imidazoline receptor agonists combined with angiotensin II receptor blockers, particularly, pharmaceutical compositions containing Moxonidine and Eprosartan mesylate, as well as the use of such compositions for the treatment of hypertension, especially in hypertensive patients suffering from type II diabetes or susceptible to developing type II diabetes.Type: ApplicationFiled: May 26, 2011Publication date: September 22, 2011Applicant: Abbott Products GmbHInventors: Dominique BAUM, Gerhard-Wilhelm Bielenberg, Bernd Boedecker, Dirk Thormaehlen
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Patent number: 8022072Abstract: An azolylmethylidenehydrazine derivative represented by the formula (I) wherein Ar is an aryl group optionally having substituent(s) or a heteroaryl group optionally having substituent(s), R1 and R2 are the same or different and each is an alkyl group, a cycloalkyl group, an aralkyl group optionally having substituent(s), an aryl group optionally having substituent(s), a heteroarylalkyl group optionally having substituent(s), or R1 and R2 are bonded to each other to form a nitrogen-containing heterocyclic group optionally having substituent(s), and X is CH or a nitrogen atom, or a pharmacologically acceptable salt thereof is useful as a medicament, particularly as an antifungal agent, or an anti-inflammatory agent or an antiallergic agent.Type: GrantFiled: June 17, 2008Date of Patent: September 20, 2011Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Hironobu Ogura, Yoshiyuki Tatsumi, Yuji Fukamizu
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Publication number: 20110224255Abstract: The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.Type: ApplicationFiled: May 19, 2011Publication date: September 15, 2011Inventors: Henry Joseph Breslin, Hans Louis Jos De Winter, Michael Joseph Kukla
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Publication number: 20110224252Abstract: The present invention relates to novel imidazole derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is halogen, C1-C4alkyl or C1-C4haloalkyl; R2 is an optionally substituted aryl or heteroaryl; R3 is halogen; R4 is hydrogen, halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy or cyano; R5 is halogen; X is N or C(R); and R is hydrogen, halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy or cyano; or an agrochemically usable salt form thereof; provided that when X is C(R), R2 cannot be an optionally substituted aryl.Type: ApplicationFiled: October 24, 2008Publication date: September 15, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Raphael Dumeunier, Clemens Lamberth, Stephan Trah, Sebastian Wendeborn
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Publication number: 20110224211Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: November 19, 2009Publication date: September 15, 2011Inventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Ron Roberts, Wieslaw Kazmierski, Richard Grimes
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Publication number: 20110218155Abstract: The invention provides a method for identifying a compound which modulates the activity of a BCL-2 family polypeptide, the method comprising: a) contacting said BCL-2 family polypeptide with a compound under conditions suitable for modulation of the activity of said BCL-2 family polypeptide; and b) detecting modulation of the activity of said BCL-2 family polypeptide by the compound, wherein the compound interacts with a binding site comprising one or more of an ?1 helix, ?2 helix, a loop between ?1-?2, ?.6 helix, and select residues of ?4, ?.5, and ?.8 helices in said BCL-2 family polypeptide; wherein the interaction of the compound with the binding site occurs at a horizontal hydrophobic groove with or without a perimeter of charged and hydrophilic residues, a superior juxta-loop, an inferior juxta-loop, or combination thereof.Type: ApplicationFiled: October 9, 2009Publication date: September 8, 2011Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Loren D. Walensky, Evripidis Gavathiotis
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Publication number: 20110217261Abstract: The present invention relates to pharmaceutical agents administered to a subject either in combination or in series for the treatment of a flaviviridae viral infection, for example, hepatitis C virus (HCV), wherein treatment comprises administering a compound effective to inhibit the function of the HCV NS5A protein and an additional compound or combinations of compounds having anti-HCV activity.Type: ApplicationFiled: August 5, 2010Publication date: September 8, 2011Inventors: Yat Sun Or, Christopher M. Owens, Bradley B. Brasher, Yao-Ling Qiu, Lijuan Jiang
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Publication number: 20110217387Abstract: A pharmaceutical composition for the treatment of fibromyalgia, which includes pilocarpine or a pharmacologically acceptable salt thereof. The pharmaceutical composition can be used as a novel therapeutic agent for fibromyalgia.Type: ApplicationFiled: May 15, 2009Publication date: September 8, 2011Applicant: AXIS, INC.Inventors: Kusuki Nishioka, Hiroshi Oka, Rieko Nohara