Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
Type:
Grant
Filed:
July 27, 2012
Date of Patent:
November 25, 2014
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Juan-Miguel Jimenez, Luca Settimo, Damien Fraysse, Guy Brenchley, Christopher John Davis, Andrew W. Miller
Abstract: The invention provides crystalline solid forms of (((S)-1-{(S)-2-[4-(4?-{[6-((2R,5S)-2,5-dimethyl-4-methylcarbamoyl-piperazin-1-yl)-pyridine-3-carbonyl]-amino}-2?-trifluoromethoxy-biphenyl-4-yl)-1H-imidazol-2-yl]-pyrrolidine-1-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat hepatitis C virus infection, and processes useful for preparing such crystalline solid forms.
Type:
Grant
Filed:
April 25, 2013
Date of Patent:
November 11, 2014
Assignee:
Theravance Biopharma R&D IP, LLC
Inventors:
Venkat R. Thalladi, Jerry Nzerem, Xiaojun Huang, Weijiang Zhang
Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
Abstract: The present invention relates to compositions, such as bimatoprost, latanoprost and travoprost, and methods to reduce fat in the body of an individual, for example, by topical administration, injection, and/or implantation of such compositions.
Type:
Grant
Filed:
January 6, 2010
Date of Patent:
September 9, 2014
Assignee:
Topokine Therapeutics, Inc.
Inventors:
Cynthia L. Grosskreutz, Louis R. Pasquale, Michael S. Singer, Murat V. Kalayoglu
Abstract: Disclosed is an anti-foot-and-mouth disease virus agent for an animal belonging to the Family Suidae, which comprises 3-oxo-3,4-dihyro-2-pyrazincarboxamide or a salt thereof. The agent is extremely useful for the prevention or treatment of food-and-mouth disease in an animal belonging to the Family Suidae. Also disclosed is an anti-foot-and-mouth disease virus agent for sheep, which comprises 3-oxo-3,4-dihyro-2-pyrazincarboxamide or a salt thereof. The agent is extremely useful for the prevention, therapy or the like of food-and-mouth disease in sheep.
Abstract: A composition comprising a mixture of chlorohexidine, a surfactant, and a cationic quaternary ammonium compound is suitable for use as an antiseptic and is surprisingly effective against difficult-to-kill organisms such as Mycobacterium tuberculosis and against Methicillin-resistant Staphylococcus aureus (MRSA) while still being suitable for topical application. The composition may include a chelating agent.
Abstract: Disclosed is the use of 5?-androstane(alkyl)-3?,5,6?-triol in preparing neuroprotective drugs. The compound has significant protective effect against neuron injuries caused by cerebral ischemia, spinal cord ischemia or hypoxia and has no obvious toxic reaction within effective dose thereof.
Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, X1, X2, X3, A, n and m are as defined in the application. The compounds of formula I have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
Type:
Grant
Filed:
January 20, 2012
Date of Patent:
July 15, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Frank Himmelsbach, Elke Langkopf, Bernd Nosse
Abstract: The present invention relates to methods of alleviating and inhibiting a lymphoproliferative disorder in a mammal, the method comprising administering one or more rapamycin derivatives (including rapamycin) to the mammal. Further, the invention provides a method for identifying agents which are useful for alleviating and inhibiting a lymphoproliferative disorders, as well as a method for identifying agents which are capable of inhibiting metastasis of lymphatic tumors in a mammal.
Type:
Grant
Filed:
July 6, 2010
Date of Patent:
July 15, 2014
Assignee:
The Trustees of the University of Pennsylvania
Abstract: The present invention relates to methods of alleviating and inhibiting a lymphoproliferative disorder in a mammal, the method comprising administering one or more rapamycin derivatives (including rapamycin) to the mammal. Further, the invention provides a method for identifying agents which are useful for alleviating and inhibiting a lymphoproliferative disorders, as well as a method for identifying agents which are capable of inhibiting metastasis of lymphatic tumors in a mammal.
Type:
Grant
Filed:
June 9, 2010
Date of Patent:
June 24, 2014
Assignee:
The Trustees of the University of Pennsylvania
Abstract: The present disclosure relates to compositions and methods for reducing uric acid levels in a individual in need thereof. The present disclosure further relates to the treatment of hyperuricemia and diseases associated with high uric acid levels in mammals using scyllo-inositol.
Abstract: Provided is an aqueous composition contained in a container, maintaining an excellent water-evaporation-inhibiting effect even when an alkali metal salt or the like is contained in the aqueous composition, and having excellent long-term stability. The aqueous composition contained in a container includes the following components (A) to (D): (A) a polyoxyethylene alkyl or alkenyl ether having an alkyl or alkenyl group having 20 to 24 carbon atoms and an average molar number of ethylene oxide added of 1.5 to 4, (B) a water-soluble polymer, (C) a nonionic surfactant having an ethylene oxide group (but excluding component (A)), and (D) water.
Abstract: Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).
Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
Type:
Grant
Filed:
December 9, 2010
Date of Patent:
March 4, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.
Abstract: A method of inhibiting formation of cancerous metabolites, of inhibiting cytochrome P450 2A13 from forming carcinogen metabolites, and/or inhibiting formation of cancerous lung cells in a subject can include: providing a morpholine compound that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6; administering a therapeutically effective amount of the morpholine compound or derivative to the subject. The morpholine compound or derivative can be substantially more selective for interacting with the cytochrome P450 2A13 over the cytochrome P450 2A6. The morpholine compound or derivative can also be substantially non-interactive with other physiological components. The morpholine compound or derivative can include a structure that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6, such as Compounds 1-34 of Formulas A-D.
Abstract: A method for optimizing the health of humans according to their age and sex is disclosed wherein the method comprises administering to said humans a daily dose of a multiple antioxidant micronutrient composition comprising vitamin A (palmitate), beta-carotene (from natural d. salina), vitamin C (calcium ascorbate), vitamin D-3 (cholecalciferol), natural source vitamin E including both d-alpha tocopherol and d-alpha tocopheryl acid succinate, thiamine mononitrate, riboflavin, niacinamide ascorbate, d-calcium pantothenate, pyridoxine hydrochloride, cyanocobalamin, folic acid (folacin), d-biotin, selenium (l-seleno methionine), chromium picolinate, zinc glycinate, calcium citrate, and magnesium citrate. For persons over the age of about 51, the composition preferably further comprises one or more of co-enzyme Q10, N-acetyl cysteine, and alpha lipoic acid. Preferably, also, vitamin D is added for women over the age of about 36.
Abstract: The present invention relates to steroid-derived cyclopamine analogs and methods for using the same for inhibiting sonic hedgehog signaling and preventing or treating cancer. A method for synthesizing the analogs of the present invention from a steroid is also provided.
Type:
Grant
Filed:
October 30, 2008
Date of Patent:
November 5, 2013
Assignees:
The Wistar Institute, The Trustees of the University of Pennsylvania
Abstract: The present invention relates to methods of alleviating and inhibiting a lymphoproliferative disorder in a mammal, the method comprising administering one or more rapamycin derivatives (including rapamycin) to the mammal. Further, the invention provides a method for identifying agents which are useful for alleviating and inhibiting a lymphoproliferative disorders, as well as a method for identifying agents which are capable of inhibiting metastasis of lymphatic tumors in a mammal.
Type:
Grant
Filed:
June 7, 2010
Date of Patent:
October 29, 2013
Assignee:
The Trustees of the University of Pennsylvania
Abstract: To reduce amounts of fat accumulated in abdominal cavity and to prevent or ameliorate visceral fat type obesity, considered to be a main factor of metabolic syndrome, the present invention provides an agent or a food or drink which contains a compound having a lophenol skeleton, or an organic solvent extract or a hot water extract of a Liliaceae plant, or a fraction thereof containing the compound as an active ingredient.