Abstract: The present application discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the application discloses the use of these compounds, a method for therapy and to pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
April 28, 2014
Date of Patent:
September 15, 2015
Assignee:
ANIONA APS
Inventors:
Dan Peters, Gordon Munro, Elsebet Ostergaard Nielsen, Karin Sandager Nielsen
Abstract: Provided herein are pharmaceutical formulations, methods, and systems for treating regional fat deposits and fat-related conditions and indications. Methods comprise administering a pharmaceutical formulation consisting essentially of a long-acting beta-2 adrenergic receptor agonist, for example, salmeterol, suitable for subcutaneous administration. Methods further comprise administering a pharmaceutical formulation that is suitable for subcutaneous injection comprising: (a) a lipophilic long-acting selective beta-2 adrenergic receptor agonist and/or glucocorticosteroid, or a salt, optical isomer, racemate, solvate, or polymorph thereof; and (b) at least one subcutaneously acceptable inactive ingredient.
Type:
Grant
Filed:
May 26, 2010
Date of Patent:
September 15, 2015
Assignee:
NEOTHETICS, INC.
Inventors:
John Daniel Dobak, Kenneth Walter Locke
Abstract: Methods of treating a patient in need thereof, comprising administering to the critically ill patient an intravenous pharmaceutical composition comprising ibuprofen in an amount effective to treat at least one condition in the patient chosen from pain, inflammation, and fever and to provide a clinically relevant effect on mean arterial pressure of the patients during the dosage interval comprising no increase or no statistically significant increase in mean arterial pressure.
Abstract: The present application relates to novel bicyclic azaheterocycles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
Type:
Grant
Filed:
August 31, 2011
Date of Patent:
August 4, 2015
Assignee:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Lars Bärfacker, Stefan Weigand
Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Type:
Grant
Filed:
February 6, 2013
Date of Patent:
August 4, 2015
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Haoran Zhao, Rao Kolluri, Carlos Valdez, Kin Tso, Rajinder Singh, John Ramphal
Abstract: The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified sub-structures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.
Type:
Grant
Filed:
September 5, 2013
Date of Patent:
August 4, 2015
Assignees:
AbbVie B.V., AbbVie Inc.
Inventors:
Pieter Smid, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Leonardus A. J. M. Sliedregt, Maria J. P. van Dongen, Jacobus A. J. den Hartog, Adrian Hobson
Abstract: A pharmaceutical composition adapted for pulmonary administration by inhalation is described, wherein the composition comprises a glitazone and one or more pharmaceutically acceptable carriers and/or excipients, wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer, and wherein the glitazone is pioglitazone or rosiglitazone or a pharmaceutically acceptable salt thereof, and wherein the glitazone is in the form of microparticles.
Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine, or 1-(2-methylpropyl)-1H-imidazo[4,5 c]quinolin-4-amine, i.e., imiquimod, to treat genital/perianal warts with shorter durations of therapy than currently prescribed for the commercially available for Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating genital/perianal warts with an acceptable safety profile and dosing regimens that are shorter and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat genital/perianal warts are also disclosed and described.
Type:
Grant
Filed:
November 27, 2013
Date of Patent:
July 14, 2015
Assignee:
Medicis Pharmaceutical Corporation
Inventors:
Michael T. Nordsiek, Jefferson J. Gregory
Abstract: The present invention provides a composition and method for inhibiting the growth of microorganisms in industrial water systems. Methods employing the composition comprising halogen-based hydantoin or hydantoin-stabilized halogen in combination with peracetic acid demonstrate synergistic control of microbial growth, particularly control of slime deposition.
Abstract: In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.
Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
Type:
Grant
Filed:
September 20, 2013
Date of Patent:
June 9, 2015
Assignee:
Medivation Technologies, Inc.
Inventors:
David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.
Abstract: The present invention relates to the use of a combination of glycine, proline, and optionally a natural or synthetic viscosity-controlling polymer, and/or lysine and/or leucine, to prepare a composition for the treatment of osteoarthritis.
Type:
Grant
Filed:
July 22, 2013
Date of Patent:
May 26, 2015
Assignee:
PROFESSIONAL DIETETICS, S.R.L.
Inventors:
Franco Conti, Francesco Saverio Dioguardi
Abstract: A composition for maintaining a function of platelets, the composition comprising, as an active ingredient, a compound represented by the following general formula (I) or a salt thereof, or a solvate thereof: wherein X represents a phenylene group; Y represents any one of a hydrogen atom and —(CH2)mR1; wherein m represents an integer of any one of 0 to 4; and R1 is any one of —NR5COR2, —NR5SO2R2, and —NR3R4; wherein R2 represents any one of a C1 to C6 alkyl group, an aryl group, a C1 to C6 alkoxy group, and the like; R3 and R4 represent a C1 to C6 alkyl group or the like; and R5 represents any one of a hydrogen atom, a C1 to C6 alkyl group, and the like; and Z represents any one of a hydrogen atom and a C1 to C6 alkyl group.
Type:
Grant
Filed:
September 16, 2011
Date of Patent:
May 19, 2015
Assignees:
THE UNIVERSITY OF TOKYO, KAKEN PHARMACEUTICAL CO., LTD.
Inventors:
Koji Eto, Ryoko Ohnishi, Hiromitsu Nakauchi, Takahiko Murata
Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
Type:
Grant
Filed:
November 19, 2010
Date of Patent:
May 19, 2015
Assignee:
SK Chemicals Co., Ltd.
Inventors:
Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
Type:
Grant
Filed:
March 7, 2013
Date of Patent:
May 19, 2015
Assignee:
Medivation Technologies, Inc.
Inventors:
David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
Abstract: In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.
Abstract: Methods and compositions containing oxytocin or an oxytocin analog, such as carbetocin, are provided for the prevention and treatment of autism spectrum disorders, related disorders and symptoms of such disorders. The methods and compositions of this disclosure are effective in the treatment of social withdrawal, eye contact avoidance, repetitive behaviors, anxiety, attention deficit, hyperactivity, depression, loss of speech, verbal communication difficulties, aversion to touch, visual difficulties, comprehension difficulties, and sound and light sensitivity. Additional compositions and methods are provided which employ oxytocin or an oxytocin analog in combination with a secondary or adjunctive therapeutic agent to yield more effective treatment tools against autism spectrum disorders and related disorders.
Type:
Grant
Filed:
August 5, 2011
Date of Patent:
May 5, 2015
Assignee:
Retrophin, Inc.
Inventors:
Alexis Kays Leonard, Joshua Orion Sestak, Henry R. Costantino, Anthony P. Sileno, Lalit Raj Peddakota, Kayvon Emile Sharghi, Garland M. Bellamy, Jason Philip Gesty, Steven C. Quay
Abstract: The disclosure is directed to a monohydrate crystalline form of 3-(5-(4-(3-fluoropropyl)piperazin-1-yl)benzimidazol-2-yl)-1-azaazulen-2-one, possessing diffraction peaks of about 12.9°, 15.9°, 17.9°, 21.2°, 22.9°, 23.5° and 24.5°. Its preparation method and pharmaceutical composition thereof are also provided.
Type:
Grant
Filed:
August 15, 2013
Date of Patent:
April 21, 2015
Assignee:
Industrial Technology Research Institute
Abstract: Compounds having formulas (I) to (VIII), salts thereof, or combinations thereof and pharmaceutical compositions comprising one or more these compounds are described herein for the treatment of HIV and neurodegenerative effects caused by HIV. Also provided herein are methods and a kit for inhibiting HIV-1, treating latent HIV in the brain, and preventing HIV-mediated cognitive decline and HIV dementia comprising administering the compounds having the formulas (I) to (VIII) and pharmaceutical compositions comprising the compounds having these formulas. The compounds having formulas I through VIII are curcumin analogs which are advantageously characterized as having anti-retroviral, neuroprotective, anti-glucosidase, and anti-HIV integrase properties. In one aspect, the pharmaceutical composition is delivered intranasally.