Additional Ring Containing Patents (Class 546/342)
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Patent number: 12233163Abstract: The present invention relates to microspheres comprising a core material, wherein the microsphere is perfectly spherical and has a moisture content less than 1%, and the method of manufacturing the same. The present invention is useful in the manufacture of sustained and modified release active pharmaceutical ingredient (API) microspheres, as a free flowing excipient for mini-tablets and in the manufacture of API dispersions.Type: GrantFiled: February 8, 2022Date of Patent: February 25, 2025Assignee: SPI Pharma, Inc.Inventors: Cecil W. Propst, Marc W. Meadows, Michael S. Todd
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Patent number: 11555014Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of prostaglandins or prostaglandin analogs which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent prostaglandins or prostaglandin analogs after crossing the biological barrier and thus can render treatments for the conditions that the parent prostaglandins or prostaglandin analogs can. Additionally, the HPPs are capable of reaching areas that parent prostaglandins or prostaglandin analogs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.Type: GrantFiled: April 2, 2009Date of Patent: January 17, 2023Assignee: Techfields Pharma Co., Ltd.Inventors: Chongxi Yu, Lina Xu
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Patent number: 11278496Abstract: Microspheres comprising a core material, wherein the microspheres have a circularity greater than 0.95 and an aspect ratio greater than 0.95, and methods of manufacturing the same. The microspheres may be useful in the manufacture of sustained and modified release active pharmaceutical ingredient (API) microspheres, as a free flowing excipient for mini-tablets and in the manufacture of API dispersions.Type: GrantFiled: April 1, 2019Date of Patent: March 22, 2022Assignee: SPI Pharma, Inc.Inventors: Cecil W. Propst, Marc W. Meadows, Michael S. Todd
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Patent number: 11150247Abstract: The present disclosure relates to a method for detecting a core polypeptide of a hepatitis C virus (HCV) in a sample from a subject involving (a) contacting said sample with a base and with a surfactant having a cationic detergent, and (b) detecting a core polypeptide of the HCV in the sample. The present invention further relates to a method for pre-processing a sample from a subject for detection of HCV, involving contacting the sample with a base and with a surfactant having a cationic detergent; and to a pre-processing reagent for detecting HCV in a sample, having a base and a surfactant including a cationic detergent, wherein the surfactant also has a nonionic detergent. Moreover, the present disclosure further relates to kits, uses, and devices related to the methods disclosed.Type: GrantFiled: November 29, 2018Date of Patent: October 19, 2021Assignee: Roche Diagnostics Operations, Inc.Inventors: Ralf Bollhagen, Barbara Upmeier, Toralf Zarnt, Peter Muench, Manfred Ginter
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Patent number: 10717762Abstract: This document relates to an abiraterone derivative, 2-(((3S,8R,9S,10R,13S,14S)-10,13-dimethyl-17-(pyridin-3-yl)-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl)oxy)-2-oxoacetic acid (ABOA). This document also relates to compositions comprising a non-covalently bound complex comprising ABOA and human serum albumin, wherein the ABOA and the human serum albumin in the composition have a ratio of weight from about 1:1 to about 1:2000. This document also relates to compositions comprising ABOA and human serum albumin, wherein the ABOA and the human serum albumin in the composition have a ratio of weight from about 1:1 to about 1:2000. This document also relates to compositions consisting essentially of ABOA and human serum albumin, wherein the ABOA and the human serum albumin in the composition have a ratio of weight from about 1:1 to about 1:2000.Type: GrantFiled: October 11, 2017Date of Patent: July 21, 2020Inventor: Qun Sun
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Patent number: 10626071Abstract: Compounds and compositions are provided that inhibit histone deacylase activity and which expand renal progenitor cell populations and improve kidney function in a damaged kidney. Methods of use of the compounds and compositions are provided.Type: GrantFiled: April 24, 2018Date of Patent: April 21, 2020Assignee: University of Pittsburgh—Of the Commonwealth System of Higher EducationInventors: Billy W. Day, Neil Hukriede
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Patent number: 10160705Abstract: Compounds and compositions are provided that inhibit histone deacylase activity and which expand renal progenitor cell populations and improve kidney function in a damaged kidney. Methods of use of the compounds and compositions are provided.Type: GrantFiled: February 10, 2012Date of Patent: December 25, 2018Assignee: University of Pittsburgh—Of the Commonwealth System of Higher EducationInventors: Billy W. Day, Neil Hukriede
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Publication number: 20150141471Abstract: The present invention relates to compounds of the formula (I), wherein the residues R1 to R6, V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present, or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.Type: ApplicationFiled: May 16, 2013Publication date: May 21, 2015Inventors: Marc Nazare, Detlef Kozian, Andreas Evers, Werngard Czechtizky
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Publication number: 20150111891Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.Type: ApplicationFiled: January 3, 2013Publication date: April 23, 2015Applicant: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Hongyan Guo, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Randall W. Vivian, Lianhong Xu, Hong Yang
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Publication number: 20150045378Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.Type: ApplicationFiled: February 12, 2013Publication date: February 12, 2015Inventors: Seiji Miwatashi, Hideo Suzuki, Tomohiro Okawa, Yasufumi Miyamoto, Takeshi Yamasaki, Yuko Hitomi, Yasuhiro Hirata
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Publication number: 20150018515Abstract: A method of producing an epoxy compound, which comprises reacting hydrogen peroxide with a compound having a carbon-carbon double bond, in the presence of at least one of a tungsten compound and a molybdenum compound; and an onium salt comprising 20 or more carbon atoms and one or more of substituents convertible to a functional group containing an active hydrogen or a salt thereof.Type: ApplicationFiled: September 30, 2014Publication date: January 15, 2015Applicant: MITSUBISHI CHEMICAL CORPORATIONInventors: Akemi HOSOKAWA, Haruhiko KUSAKA
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Publication number: 20150018321Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: September 25, 2014Publication date: January 15, 2015Applicant: Chiesi Farmaceutici S.p.A.Inventors: Maurizio DELCANALE, Elisabetta ARMANI, Gabriele AMARI
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Publication number: 20140378423Abstract: 1-Phenyl-2-pyridinyl alkyl alcohol compounds are effective as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and may be used to prevent and/or treat certain diseases or conditions.Type: ApplicationFiled: September 10, 2014Publication date: December 25, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Gabriele Amari, Elisabetta Armani, Maurizio Delcanale
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Publication number: 20140371232Abstract: Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.Type: ApplicationFiled: December 18, 2012Publication date: December 18, 2014Inventors: Zhuorong Li, Xingyue Ji, Situ Xue, Guanghui Zheng, Yuhuan Li, Peizhen Tao, Jiandong Jiang
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Publication number: 20140343284Abstract: A compound of Formula 2 is disclosed wherein R1, MA and MB are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 1 wherein RI and X are as defined in the disclosure comprising contacting a compound of Formula 2 with a halogenating agent. Also disclosed is a method for preparing a compound of Formula 4 wherein R1, R3 and R4 are as defined in the disclosure, comprising reacting a compound of Formula 5 wherein R3 and R4 are as defined in the disclosure with a compound of Formula 1, with a compound of Formula 1, the process of preparing the compound of Formula 4 includes the step of preparing the compound of Formula 1 from the compound of Formula 2 by the method disclosed above. Also disclosed is compound that is methyl 3,5-dichlorobenzeneethanimidate methyl 3,5-dichlorobenzeneethanimidate or ethyl 3,5-dichlorobenzeneethanimidate or salts thereof.Type: ApplicationFiled: December 13, 2012Publication date: November 20, 2014Inventor: Wenming Zhang
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Publication number: 20140343079Abstract: The invention provides compounds of formulae (I), (II), (III), and (IV): and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers and Alzheimer's disease.Type: ApplicationFiled: September 13, 2012Publication date: November 20, 2014Applicants: Behalf of Arizona State UniversityInventors: Carl E. Wagner, Peter W. Jurutka, Pamela A. Marshall
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Publication number: 20140323510Abstract: Disclosed herein is a compound of the formula Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.Type: ApplicationFiled: May 8, 2014Publication date: October 30, 2014Applicant: Allergan, Inc.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Publication number: 20140315960Abstract: The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.Type: ApplicationFiled: October 31, 2012Publication date: October 23, 2014Inventor: Claus Selch LARSEN
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Publication number: 20140187786Abstract: Compounds that are 1,3,4-trisubstituted benzenes which modulate (e.g., inhibit) the activity of ?-secretase. The compounds are expected to reduce the level of A?42 in patients and be useful in the treatment of diseases (e.g., Alzheimer's disease) characterized by elevated levels of A?42 and/or the formation of A? plaques.Type: ApplicationFiled: July 18, 2013Publication date: July 3, 2014Applicant: EnVivo Pharmaceuticals, Inc.Inventors: Gideon Shapiro, Richard Chesworth
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Publication number: 20140186872Abstract: The present invention provides compounds having the formula A: (A) or pharmaceutically acceptable salt thereof, wherein W, R1, R2 and R5 are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as cytotoxic agents towards proliferating and/or quiescent cancer stem cells, and thus are useful, for example, for the treatment of cancer.Type: ApplicationFiled: June 6, 2012Publication date: July 3, 2014Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE- CNRS, UNIVERSITE DE STRASBOURGInventors: Marie Feve, Maria Zeniou-Meyer, Jacques Haiech, Herve Chneiweiss, Marie-Claude Kilhoffer, Samir Mameri, Marcel Hibert
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Publication number: 20140179723Abstract: Statin compositions are disclosed for stimulating neurite growth from spiral ganglion neurons in the inner ear and methods for preventing damage to or treating damage of auditory neurons and/or hair cells of the cochlea following acoustic or toxic insult.Type: ApplicationFiled: December 13, 2013Publication date: June 26, 2014Inventors: Donna S. Whitlon, Claus-Peter Richter
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Publication number: 20140142074Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Applicant: Chiesi Farmaceutici S.p.A.Inventors: Elisabetta ARMANI, Gabriele Amari, Carmelida Capaldi, Oriana Esposito, Ilaria Peretto
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Publication number: 20140135301Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: January 22, 2014Publication date: May 15, 2014Applicant: Chiesi Farmaceutici S.p.A.Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
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Publication number: 20140094466Abstract: In alternative embodiments, the invention provides compositions that inhibit the polypeptide SSH-2, or SlingSHot-2, a phosphatase enzyme that regulates actin filaments, and methods for making and using them, including methods comprising administering compositions of the invention to regulate or modify actin filament polymerization by inhibiting SSH-2, where in one embodiment compositions of the invention slow or inhibit F-actin depolymerization and severing. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit cell motility and/or internal remodeling. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit, or reverse, or ameliorate the progression of a cancer or a metastasis or other uncontrolled or unregulated cell growth, and/or Alzheimer's disease.Type: ApplicationFiled: March 15, 2012Publication date: April 3, 2014Inventors: Jason H. Haga, Shu Chien, Matt Mui, Marshall J. Levesque, Phillip D. Pham
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Publication number: 20140080852Abstract: Disclosed are compounds of formula: that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.Type: ApplicationFiled: October 25, 2013Publication date: March 20, 2014Applicant: FIBROSTATIN, S.L.Inventors: Juan Saus, Santos Fustero, Juan F Sanz-Cervera, Enrique Pérez-Payá, Raül Blasco, Francisco Revert-Ros, Fernando Revert
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Publication number: 20140057882Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and the treatment of certain conditions such as COPD.Type: ApplicationFiled: October 8, 2013Publication date: February 27, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Elisabetta ARMANI, GABRIELE AMARI, LAURA CARZANIGA, CARMELIDA CAPALDI, ORIANA ESPOSITO, GINO VILLETTI, RENATO DE FANTI
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Patent number: 8633182Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.Type: GrantFiled: May 22, 2013Date of Patent: January 21, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Dieter Hamprecht, Sara Frattini, Iain Lingard, Stefan Peters
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Patent number: 8586607Abstract: There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.Type: GrantFiled: July 23, 2009Date of Patent: November 19, 2013Assignee: Syddansk UniversitetInventors: Trond Ulven, Elisabeth Christiansen
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Publication number: 20130296573Abstract: A protected organoboronic acid includes a boron having an sp3 hybridization, a conformationally rigid protecting group bonded to the boron, and an organic group bonded to the boron through a boron-carbon bond. A method of performing a chemical reaction includes contacting a protected organoboronic acid with a reagent, the protected organoboronic acid including a boron having an sp3 hybridization, a conformationally rigid protecting group bonded to the boron, and an organic group bonded to the boron through a boron-carbon bond. The organic group is chemically transformed, and the boron is not chemically transformed.Type: ApplicationFiled: October 18, 2012Publication date: November 7, 2013Applicant: The Board of Trustees of the University of IllinoisInventors: Martin D. Burke, Eric P. Gillis, Suk Joong Lee, David M. Knapp, Kaitlyn C. Gray
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Publication number: 20130281705Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.Type: ApplicationFiled: June 18, 2013Publication date: October 24, 2013Inventor: Shalini SHARMA
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Publication number: 20130224657Abstract: The present invention provides an acid generator generates a sulfonic acid represented by the following general formula (1) in response to high-energy beam or heat: To provide a novel acid generator which is suitably used as an acid generator for a resist composition, which solves the problems of LER and a depth of focus and can be effectively and widely used particularly without degradation of a resolution, a chemically amplified resist composition using the same, and a patterning process.Type: ApplicationFiled: February 15, 2013Publication date: August 29, 2013Applicant: SHIN-ETSU CHEMICAL CO., LTD.Inventor: SHIN-ETSU CHEMICAL CO., LTD.
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Patent number: 8519145Abstract: The present invention relates to a compound as a peroxisome proliferator activated receptor (PPAR) activator and a hydrate, a solvate, a stereoisomer and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition, a cosmetic composition, a muscle strengthening agent, a memory improving agent, a therapeutic agent for dementia and Parkinson's disease, a functional food and a feed composition containing the same.Type: GrantFiled: December 1, 2007Date of Patent: August 27, 2013Assignee: Seoul National University Industry FoundationInventors: Heonjoong Kang, Jungwook Chin, Jaehwan Lee
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Publication number: 20130203727Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).Type: ApplicationFiled: July 1, 2011Publication date: August 8, 2013Applicant: GILEAD SCIENCES, INC.Inventors: Kerim Babaoglu, Elizabeth Bacon, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, Paul Hrvatin, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Paul Roethle, James Taylor, James D. Trenkle, Randall W. Vivian, Lianhong Xu
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Publication number: 20130203747Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: November 21, 2012Publication date: August 8, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130190502Abstract: Disclosed is a selective ester production process of an alcoholic hydroxyl group, which proceeds under chemically mild conditions, while having adequate environmental suitability, operability and economical efficiency. Specifically disclosed is a process for producing an ester compound, which is characterized in that an alcohol and a carboxylic acid ester compound are reacted in the presence of a compound containing zinc element, thereby selectively acylating a hydroxyl group of the alcohol.Type: ApplicationFiled: March 5, 2013Publication date: July 25, 2013Applicant: Takasago International CorporationInventor: Takasago International Corporation
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Publication number: 20130190504Abstract: A process for the preparation of functional molecules using the thiol-ene coupling reaction and a process for the preparation of protected functional thiols, specifically thioesters is provided. The methods may be used to make functional polymers and other molecules. The method of making a functionalized polymer using a thiol-ene reaction comprises: providing a functionalized thioester having the following formula: wherein R is a functional group and COR? is a protecting group; cleaving the functionalized thioester, forming a functional thiol and an acyl group; providing a polymer having a pendant vinyl group; and reacting the polymer with the functional thiol whereby a functionalized polymer is formed, wherein the functional thiol is not isolated prior to reacting with the polymer.Type: ApplicationFiled: October 1, 2012Publication date: July 25, 2013Inventors: Ralph L. DAVID, Julia A. KORNFIELD
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Publication number: 20130172558Abstract: Naproxen-based ferroelectric liquid crystal (FLC) or nematic liquid crystal chiral compounds, which can be used in liquid crystal compositions useful for electro-optical and display device applications. The liquid crystal can be a ferroelectric liquid crystal. Also provided is a display device that includes the Naproxen-based ferroelectric liquid crystal (FLC) or nematic liquid crystal chiral compound. Also provided is a method of preparing a liquid crystal display device on silicon that includes incorporating the Naproxen-based ferroelectric liquid crystal (FLC) or nematic liquid crystal chiral compound, into a liquid crystal display on silicon by disposing the compound in a liquid crystal, or the liquid crystal, onto a silicon surface.Type: ApplicationFiled: January 4, 2012Publication date: July 4, 2013Inventors: Yongqiang Zhang, Kundalika More, William Thurmes
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Publication number: 20130150381Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of dis orders related to aberrant levels of uric acid.Type: ApplicationFiled: June 15, 2011Publication date: June 13, 2013Applicant: ARDEA BIOSCIENCE, INC.Inventors: Samedy Ouk, Jean-Michel Vernier, Esmir Gunic
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Publication number: 20130137648Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: January 23, 2013Publication date: May 30, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Patent number: 8431713Abstract: Provided are compounds having the Formula I or salts thereof, wherein R2, L, R3, R11, D2 and R13 are as defined herein, that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: GrantFiled: January 16, 2008Date of Patent: April 30, 2013Assignee: Array BioPharma, Inc.Inventors: Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Rustam Ferdinand Garrey, Ronald Jay Hinklin, Ajay Singh, Timothy M. Turner
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Patent number: 8420812Abstract: A process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein D, J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process of heteroaryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional heteroaryl-1-alkynes of the formula I.Type: GrantFiled: December 23, 2009Date of Patent: April 16, 2013Assignee: SanofiInventors: Omar Rkyek, Marc Nazare, Andreas Lindenschmidt, Jorge Alonso, Matthias Urmann, Nis Halland
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Patent number: 8410282Abstract: This compounds correspond to the formula (I), where: R1 represents and aryl or heteroaryl group optionally substituted by one or more substituents selected from the group consisting of halogen atoms, straight or branched optionally substituted lower alkyl, cycloalkyl, hydroxy, straight or branched, optionally substituted lower alkoxy, cyano, or —CO2R?, wherein R? represents a hydrogen atom or a straight or branched, optionally substituted lower alkyl group; R2 represents a group selected from: a) a straight or branched lower alkyl group substituted by one or more carboxylic groups (—COOH) and optionally substituted by one or more halogen atoms; b) a cycloalkyl group substituted by one or more carboxylic groups (—COOH) and optionally substituted by one or more halogen atoms; c) a straight or branched alkylcycloalkyl or cycloalkylalkyl group substituted by one or more carboxylic groups (—COOH) and optionally substituted by one or more halogen atoms. Formula (I).Type: GrantFiled: September 30, 2008Date of Patent: April 2, 2013Assignee: Palobiofarma, S.L.Inventors: Lyhen Gonzalez Lio, Juan Alberto Camacho Gomez
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Publication number: 20130079313Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.Type: ApplicationFiled: September 26, 2012Publication date: March 28, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Publication number: 20130053364Abstract: The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: ApplicationFiled: April 23, 2012Publication date: February 28, 2013Inventors: Hazel J. Dyke, Susan M. Cramp, Thomas D. Pallin, Janusz J. Kulagowski, John G. Montana, Robert Zahler
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Patent number: 8357718Abstract: Compounds represented by formula: wherein X, Y and Z are as defined herein, pharmaceutically acceptable salts thereof, and related compounds, are suitable for use in treating or preventing a Flaviviridae viral infection in a host.Type: GrantFiled: February 4, 2008Date of Patent: January 22, 2013Assignee: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Nghe Nguyen-Ba, Liliane Halab, Bettina Hamelin, Oswy Z. Pereira, Carl Poisson, Melanie Proulx, Thumkunta Jagadeeswar Reddy, Zhang Ming-Qiang
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Publication number: 20130012487Abstract: 1-Phenyl-2-pyridinyl alkyl alcohol compounds are effective as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and may be used to prevent and/or treat certain diseases or conditions.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventors: Gabriele AMARI, Elisabetta Armani, Maurizio Delcanale
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Publication number: 20120271055Abstract: The present invention relates to a compound as a peroxisome proliferator activated receptor (PPAR) activator and a hydrate, a solvate, a stereoisomer and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition, a cosmetic composition, a muscle strengthening agent, a memory improving agent, a therapeutic agent for dementia and Parkinson's disease, a functional food and a feed composition containing the same.Type: ApplicationFiled: December 1, 2007Publication date: October 25, 2012Applicant: SEOUL NATIONAL UNIVERSITY INDUSTRY FOUNDATIONInventors: Heonjoong Kang, Jungwook Chin, Jaehwan Lee
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Patent number: 8278317Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: July 18, 2006Date of Patent: October 2, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: B. Wesley Trotter, Kausik K. Nanda, Scott E. Wolkenberg, M. Brad Nolt, David Wisnoski
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Patent number: 8212048Abstract: A method of producing an aromatic compound of the following formula (3) comprising reacting a compound of the following formula (1) with an olefin compound of the following formula (2) in the presence of a transition metal complex: (wherein, an Ar1 ring represents an aromatic hydrocarbon ring or aromatic heterocyclic ring, an Ar2 ring represents a heterocyclic ring containing X1 and N*, and the X1 represents a nitrogen atom or carbon atom and the N represents a nitrogen atom connecting via a double bond to either one of two adjacent atoms in the Ar2 ring.) (wherein, R1, R2, R3 and R4 represent each independently a hydrogen atom, an alkyl group having 1 to 10 carbon atoms or an aryl group having 6 to 18 carbon atoms.) (wherein, Ar1, Ar2, X1, N*, R1, R2 and R3 represent the same meanings as described above.).Type: GrantFiled: February 2, 2007Date of Patent: July 3, 2012Assignees: Sumitomo Chemical Company, Limited, Osaka UniversityInventors: Fumitoshi Kakiuchi, Yusuke Matsuura, Masato Ueda
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Publication number: 20120156255Abstract: A polymeric matrix for delivery of an HMG CoA reductase inhibitor such as a statin to tissue such as cardiac tissue in need thereof for the treatment or prevention of a disease or defect such as atrial fibrillation has been developed. In the preferred embodiment, a statin is delivered by means of a patch sutured to cardiac tissue at the time of cardiothoracic surgery. In the most preferred embodiment, the patch is a biodegradable material providing controlled or sustained release over a prolonged period of time, such as a week. Suitable materials include extracellular matrix, or other biodegradable hydrogels or polymeric materials providing sustained or controlled release of statin at the site of application.Type: ApplicationFiled: December 16, 2011Publication date: June 21, 2012Inventors: Jaipal Singh, Nicolas Chronos