Chalcogen Or Nitrogen Attached Directly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/251)
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Patent number: 8633231Abstract: The present invention relates to compounds of the general structure shown in Formula (A): (A): and includes pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: July 8, 2011Date of Patent: January 21, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Duane DeMong, Michael W. Miller, Xing Dai, Andrew Stamford
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Publication number: 20140005239Abstract: The present invention provides novel crystalline polymorphic forms of MDT-637, in particular, crystalline polymorphic forms with physicochemical properties specifically suited for drug production, amorphous formation, composite form, and methods of preparation thereof. The novel polymorphs described herein are useful for the treatment of respiratory disease, such as disease caused by respiratory syncytial virus.Type: ApplicationFiled: June 28, 2013Publication date: January 2, 2014Inventors: Robert O. Cook, Eugene R. Reynolds, Boris Shekunov, Siead I. Zegar
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Publication number: 20130317013Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient.Type: ApplicationFiled: July 25, 2013Publication date: November 28, 2013Inventors: Xavier Billot, Yongxin Han, Robert N. Young
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Publication number: 20130317232Abstract: Embodiments of materials suitable for use as a replacement for Tetrazene and methods of preparing such materials are described. In one embodiment, the material comprises MTX-1, as well as simple salts or complexes derived therefrom. The methods of preparing such materials include combining Tetrazene and an acid to form a suspension, where the acid is nitric acid, sulfuric acid, perchloric acid, or hydrochloric acid. A nitrite salt may be added to the suspension, where the nitrite salt is sodium nitrite, lithium nitrite, potassium nitrite, an aqueous solution of sodium nitrite, an aqueous solution of lithium nitrite, or an aqueous solution of potassium nitrite. In some embodiments, the suspension is stirred until the suspension has a white appearance.Type: ApplicationFiled: August 1, 2013Publication date: November 28, 2013Applicant: PACIFIC SCIENTIFIC ENERGETIC MATERIALS COMPANYInventors: John W. Fronabarger, Michael D. Williams
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Publication number: 20130303779Abstract: The present invention relates to a process for the preparation of a diol sulfone derivative comprising reaction of a halomethyl substrate with a thio-aryl compound to obtain a thio-ether compound, and oxidizing the thio-ether compound to the corresponding sulfone. In case of a chiral halomethyl substrate, the resulting chiral diol sulfone derivative is suitable as a building block for statin type compounds.Type: ApplicationFiled: January 13, 2012Publication date: November 14, 2013Applicant: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.Inventors: Ben De Lange, Peter Hans Riebel, Michael Wolberg, Dennis Heemskerk, Daniel Mink
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Publication number: 20130296563Abstract: The present invention relates to a process for the preparation of a 1-methyl-1H-tetrazole-5-thio derivative comprising reaction of a halomethyl substrate with 1-methyl-H-tetrazole-5-thiol to obtain a thio-ether compound, and oxidizing the thio-ether compound to the corresponding sulfone. In case of a chiral halomethyl substrate, the resulting chiral diol sulfone derivative is suitable as a building block for statin type compounds.Type: ApplicationFiled: January 13, 2012Publication date: November 7, 2013Applicant: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.Inventor: Ben De Lange
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Patent number: 8575205Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.Type: GrantFiled: March 22, 2012Date of Patent: November 5, 2013Assignee: Microdose Therapeutx, Inc.Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laguerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
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Patent number: 8569302Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: GrantFiled: July 19, 2010Date of Patent: October 29, 2013Assignee: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Mertzman, Philip A. Morganelli, William J. Watkins, Hong Ye
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Publication number: 20130274256Abstract: Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.Type: ApplicationFiled: October 11, 2012Publication date: October 17, 2013Applicant: SEQUOIA SCIENCES, INC.Inventor: Sequoia Sciences, Inc.
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Patent number: 8546374Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.Type: GrantFiled: July 9, 2012Date of Patent: October 1, 2013Assignee: Abbvie Inc.Inventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biquin C. Li
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Patent number: 8524914Abstract: The present invention relates to novel intermediate compounds used in preparing Rosuvastatin or the pharmaceutically acceptable salts thereof, to a method for preparing same, and to a method for preparing Rosuvastatin or the pharmaceutically acceptable salts thereof from the intermediates. The preparation method of the present invention has the effect of providing Rosuvastatin hemi-calcium salts with an excellent yield rate.Type: GrantFiled: April 8, 2010Date of Patent: September 3, 2013Assignee: Chong Kun Dang Pharmaceutical Corp.Inventors: Hongwoo Lee, Daejong Park, Choongleol Yoo, Donghyuk Nam, Hohyung Ryu, Dongjin Kim
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Publication number: 20130209760Abstract: The present invention provides an alkyl sulfonated tetrazole compound, a method of preparing the same, an epoxy resin containing the same and a substrate produced therefrom. The epoxy resin is usefully used as a raw material of printed circuit boards, and has high adhesion to metal.Type: ApplicationFiled: May 18, 2012Publication date: August 15, 2013Applicant: SAMSUNG ELECTRO-MECHANICS CO., LTD.Inventors: Young Kwan SEO, Sung Nam CHO, Jun Young KIM, Tae Hoon KIM
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Publication number: 20130190505Abstract: The present invention is a method for promoting hydrothiolation of an unactivated alkenes with a thiol using gallium triflate.Type: ApplicationFiled: September 28, 2011Publication date: July 25, 2013Applicant: Trustees of Dartmouth OfficeInventors: Jimmy Wu, Markku A. Savolainen
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Patent number: 8476432Abstract: The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.Type: GrantFiled: June 30, 2011Date of Patent: July 2, 2013Assignee: Yuhan CorporationInventors: Hyun Ju, Sang-Sun Joung, Hyun-Jik Yi, Ja-Heouk Khoo, Jong-Chul Lim, Jae-Gyu Kim
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Publication number: 20130158087Abstract: Methods and compounds for treating cancer, dmg resistance and/or metastasis are described herein. These methods and compounds can inhibit the expression of aberrant TG2 expression and/or inhibit the binding of GTP to TG2, and thereby prevent the induction of epithelial to mesenchymal transition of cancer cells, and a stem cell-like phenotype.Type: ApplicationFiled: June 21, 2011Publication date: June 20, 2013Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventors: Kapil Mehta, Anupam Kumar, Jansina Fok, Shuxing Zhang
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Publication number: 20130157857Abstract: The present invention relates to an inhibitor for tobacco axillary bud growth, the inhibitor comprising, as an active ingredient, one or more kinds of very-long chain fatty acid synthesis inhibitors such as a chloroacetamide-based herbicide, fentrazamide, cafenstrole or indanofan; an inhibitor for tobacco axillary bud growth, the inhibitor comprising the aforesaid very-long chain fatty acid synthesis inhibitor together with clorthal-dimethyl or an aliphatic alcohol having 6 to 20 carbon atoms; and a method for inhibiting tobacco axillary bud growth which comprises applying the inhibitor for tobacco axillary bud growth. The inhibitor for tobacco axillary bud growth of the present invention shows sustained drug efficacy at a low concentration, induces neither chemical injury nor disease, and can contribute to the improvement in labor productivity.Type: ApplicationFiled: July 26, 2011Publication date: June 20, 2013Applicant: SDS BIOTECH K.K.Inventors: Motoki Tanaka, Keijitsu Tanaka, Takeshi Shibuya, Eiji Ikuta, Kotaro Yoshinaga, Yuki Yamaguchi
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Publication number: 20130158263Abstract: A compound of Formula (1), is disclosed wherein P1 and P2 are alcohol protecting groups or 1,3-diol protecting group, R is selected from: wherein R4a is selected from alkyl, aryl, arylalkyl and cycloalkyl, Rc is selected from H, alkyl, aryl, alkaoxy, haloalkyl, monohaloalkyloxy, and dihaloalkyloxy, Rd is selected from alkyl, aryl, arylalkyl, CF3, halo and NO2 and X is selected from O, N—H, N-alkyl and S, Ra and Rb are same or different and each represents hydrogen, an alkyl group of 1 to 12 carbon atoms, an aryl group of 6 to 12 carbon atoms, or an aralkyl group of 7 to 12 carbon atoms.Type: ApplicationFiled: February 23, 2011Publication date: June 20, 2013Inventors: Shriprakash Dhar Dwivedi, Dhimant Jasubhai Patel, Mahesh Laljibhai Rupapara
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Patent number: 8455657Abstract: A process is described for the preparation of 3-alkylsulfinylbenzoyl derivatives of the formula (IIIa) by reaction of 3-alkylsulfinylbenzoic acids of the formula (Ib) with compounds of the formula (II) in the presence of a chlorinating agent and a base. In the formulae specified above, Y is a radical such as pyrazolyl and cyclohexanedionyl. R1, R2 and R3 are radicals such as halogen, nitro, cyano and alkyl.Type: GrantFiled: December 22, 2011Date of Patent: June 4, 2013Assignee: Bayer Cropscience AGInventors: Mark James Ford, Jan Peter Schmidt, Helmut Kohlhepp
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Publication number: 20130123315Abstract: The present invention relates to compounds of the general structure shown in Formula (A): (A): and includes pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: July 8, 2011Publication date: May 16, 2013Inventors: Duane DeMong, Michael W. Miller, Xing Dai, Andrew Stamford
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Publication number: 20130096168Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R6, A1, A2, X1, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: December 5, 2012Publication date: April 18, 2013Applicant: NOVARTIS AGInventors: Yuki IWAKI, Toshio KAWANAMI, Gary Michael KSANDER, Muneto MOGI
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Publication number: 20130096303Abstract: The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.Type: ApplicationFiled: June 30, 2011Publication date: April 18, 2013Inventors: Hyun Ju, Sang-Sun Joung, Hyun-Jik Yi, Ja-Heouk Khoo, Jong-Chul Lim, Jae-Gyu Kim
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Patent number: 8410154Abstract: Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I. The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and Plasmodium falciparum-induced inflammation. In Formula 1, x is 1 or 2: y is O, 1, 2 or 3; and R1 is selected from the group consisting of hydrogen, alkyl having 1 or 2 carbon atoms, hydroxy, alkoxy having 1 or 2 carbon atoms, fluoro, chloro, bromo, and amino.Type: GrantFiled: April 30, 2009Date of Patent: April 2, 2013Assignee: Wellstat Therapeutics CorporationInventors: James Dennen O'Neil, Shalini Sharma, Ramachandran Arudchandran
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Patent number: 8383660Abstract: Dibenzyl amine compounds and derivatives of Formula I, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.Type: GrantFiled: January 3, 2007Date of Patent: February 26, 2013Assignee: Pfizer Inc.Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry
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Publication number: 20130030022Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: September 26, 2012Publication date: January 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Boehringer Ingelheim International GmbH
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Patent number: 8361959Abstract: The present invention relates to compounds of the general formula: (I) wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: GrantFiled: September 30, 2009Date of Patent: January 29, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Andrew Stamford, Michael W. Miller, Duane Eugene DeMong, William J. Greenlee, Joseph A. Kozlowski, Brian J. Lavey, Michael K. C. Wong, Wensheng Yu, Xing Dai, De-Yi Yang, Guowei Zhou
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Patent number: 8350050Abstract: High-quality bis-(1(2)H-tetrazol-5-yl)amine and a method for easily, safely, and inexpensively producing the compound are provided. The method for producing bis-(1(2)H-tetrazol-5-yl)amine includes the steps of heating to 50 to 120° C. a solution mixture in which a necessary amount of an azide salt and a dicyanamide salt in an amount corresponding to 1 to 80 wt % of a necessary amount are added to a solvent, adding an acid in an amount of 1.54 to 2.22 chemical equivalents of the dicyanamide salt in the solution mixture to carry out a reaction at 50 to 120° C., and then adding an acid and a dicyanamide salt solution in which the remaining dicyanamide salt is dissolved in a solvent to promote the reaction. Bis-(1(2)H-tetrazol-5-yl)amine is obtained according to the production method.Type: GrantFiled: July 14, 2011Date of Patent: January 8, 2013Assignee: Toyo Boseki Kabushiki KaishaInventors: Toshiyuki Toda, Toru Kofukuda
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Publication number: 20120329772Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.Type: ApplicationFiled: July 9, 2012Publication date: December 27, 2012Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biqin C. Li
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Patent number: 8324384Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: February 3, 2010Date of Patent: December 4, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Songnian Lin, Xibin Liao, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
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Publication number: 20120295938Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: March 9, 2012Publication date: November 22, 2012Inventors: BRADLEY TEEGARDEN, DENNIS CHAPMAN, MARC DECAIRE, PETER I. DOSA, KONRAD FEICHTINGER, HONNAPPA JAYAKUMAR, THUY-ANH TRAN, SONJA STRAH-PLEYNET, JAY XU
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Patent number: 8299103Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: June 1, 2010Date of Patent: October 30, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether
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Publication number: 20120238581Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.Type: ApplicationFiled: May 31, 2012Publication date: September 20, 2012Inventors: Andrew J. Souers, Ju Gao, Todd M. Hasen, Rajesh R. Iyengar, Philip R. Kym, Bo Liu, Zhonghua Pei, Vince S. Yeh, Gang Zhao, Zhili Xin
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Publication number: 20120202750Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: ApplicationFiled: January 23, 2012Publication date: August 9, 2012Applicant: Genentech, Inc.Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Publication number: 20120183498Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.Type: ApplicationFiled: March 22, 2012Publication date: July 19, 2012Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laguerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
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Patent number: 8217038Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: GrantFiled: October 7, 2010Date of Patent: July 10, 2012Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20120165540Abstract: A process is described for the preparation of 3-alkylsulfinylbenzoyl derivatives of the formula (IIIa) by reaction of 3-alkylsulfinylbenzoic acids of the formula (Ib) with compounds of the formula (II) in the presence of a chlorinating agent and a base. In the formulae specified above, Y is a radical such as pyrazolyl and cyclohexanedionyl. R1, R2 and R3 are radicals such as halogen, nitro, cyano and alkyl.Type: ApplicationFiled: December 22, 2011Publication date: June 28, 2012Applicant: BAYER CROPSCIENCE AGInventors: Mark James FORD, Jan Peter SCHMIDT, Helmut KOHLHEPP
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Patent number: 8202896Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.Type: GrantFiled: August 11, 2003Date of Patent: June 19, 2012Assignee: Microdose Therapeutx, Inc.Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laguerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
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Patent number: 8198458Abstract: Compounds of formula (I): wherein Ar, X, R1, R2, R3 and R4 are as defined herein. The compounds are useful as reverse transcriptase inhibitors against wild type and single or double mutant strains of HIV.Type: GrantFiled: February 3, 2009Date of Patent: June 12, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Patrick DeRoy, Anne-Marie Faucher, Alexandre Gagnon, Serge R. Landry, Sebastien Morin, Jeffrey O'Meara, Bruno Simoneau, Bounkham Thavonekham, Christiane Yoakim
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Publication number: 20120142917Abstract: Disclosed herein is the use of HLM-008182, as well as its analogues formed via in-house synthesis, as a potent proteasome inhibitors. A new method was developed for HLM-008182 through a four-step protocol and the method was further optimized to a two step protocol. The synthesis in both protocols was regioselective with TiCl4. The reaction was highly efficient with microwave assisted heating and THF as solvent. The modification around the molecule HLM-008182 established primary SAR, indicating that the proteasome inhibition activity was a function of the 2-side chain.Type: ApplicationFiled: September 6, 2011Publication date: June 7, 2012Applicants: H. Lee Moffitt Cancer Center and Research Institute, Inc., UNIVERSITY OF SOUTH FLORIDAInventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
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Publication number: 20120142915Abstract: This disclosure concerns a protected cyclopropylboronic acid comprising a substituted cyclopropyl group and a boronic ester group having a protecting group. The protecting group is an N-methyliminodiacetic acid (MIDA) group or MIDA-based group.Type: ApplicationFiled: December 1, 2011Publication date: June 7, 2012Inventors: Matthew Duncton, Rajinder Singh
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Publication number: 20120136151Abstract: The present invention relates to novel intermediate compounds used in preparing Rosuvastatin or the pharmaceutically acceptable salts thereof, to a method for preparing same, and to a method for preparing Rosuvastatin or the pharmaceutically acceptable salts thereof from the intermediates. The preparation method of the present invention has the effect of providing Rosuvastatin hemi-calcium salts with an excellent yield rate.Type: ApplicationFiled: April 8, 2010Publication date: May 31, 2012Inventors: Hongwoo Lee, Daejong Park, Choongleol Yoo, Donghyuk Nam, Hohyung Ryu, Dongjin Kim
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Publication number: 20120122780Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: May 20, 2010Publication date: May 17, 2012Applicant: Ardea Biosciences Inc.Inventors: Martha De La Rosa, Jean-Luc Girardet
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Publication number: 20120122889Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (I)-(I), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: December 23, 2009Publication date: May 17, 2012Applicant: President and Fellows of Harvard CollegeInventors: Junying Yuan, Emily S. Hsu
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Publication number: 20120102826Abstract: A diesel fuel additive composition, a fuel containing the fuel additive, a method for improving diesel engine performance using the additive. The diesel fuel additive includes a reaction product of (a) a hydrocarbyl-substituted acylating agent and (b) a reactant selected from the group consisting of a nitrogen-containing compound, a hydroxyl-containing compound, and water that provides a reaction product selected from the group consisting (1) a mono-amide/mono-acid or metal free mono-acid salt thereof, (2) a diacid or metal free diacid salt thereof, and (3) mono-ester/mono-acid or metal free mono-acid salt thereof. The reaction product includes at least about 10 molar percent acid groups based on total moles of the reaction product.Type: ApplicationFiled: November 3, 2010Publication date: May 3, 2012Applicant: AFTON CHEMICAL CORPORATIONInventor: Xinggao FANG
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Patent number: 8143418Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.Type: GrantFiled: February 7, 2011Date of Patent: March 27, 2012Assignee: Board of Regents, The University of Texas SystemInventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
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Publication number: 20120071529Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: March 1, 2011Publication date: March 22, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Monika ERMANN, Doris RIETHER, Renee M. ZINDELL
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Publication number: 20120004419Abstract: High-quality bis-(1(2)H-tetrazol-5-yl)amine and a method for easily, safely, and inexpensively producing the compound are provided. The method for producing bis-(1(2)H-tetrazol-5-yl)amine includes the steps of heating to 50 to 120° C. a solution mixture in which a necessary amount of an azide salt and a dicyanamide salt in an amount corresponding to 1 to 80 wt % of a necessary amount are added to a solvent, adding an acid in an amount of 1.54 to 2.22 chemical equivalents of the dicyanamide salt in the solution mixture to carry out a reaction at 50 to 120° C., and then adding an acid and a dicyanamide salt solution in which the remaining dicyanamide salt is dissolved in a solvent to promote the reaction. Bis-(1(2)H-tetrazol-5-yl)amine is obtained according to the production method.Type: ApplicationFiled: July 14, 2011Publication date: January 5, 2012Applicant: TOYO BOSEKI KABUSHIKI KAISHAInventors: Toshiyuki TODA, Toru KOFUKUDA
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Patent number: 8084619Abstract: A novel compound, used for example, as a gas generating fuel, is defined as a compound having the structural formula of R3—R1—R2, wherein R1 is a urea group, R2 is a tetrazolyl group with a C—N bond to the urea group, and R3 may be defined as a non-tetrazolyl, triazolyl, heterocyclic, heterocyclic amine, aliphatic, aliphatic amine, aryl, alkyl, hydrogen, or nitrogen group linked to the free nitrogen on the urea group. A method of making the compound is also provided. A gas generating composition 12 containing the novel compound as a fuel, and an oxidizer is also provided. The novel compound may be contained within a gas generant composition 12, within a gas generator 10. The gas generator 10 may be contained within a gas generating system such as an airbag inflator 10 or seat belt assembly 150, or more broadly within a vehicle occupant protection system 180.Type: GrantFiled: November 1, 2010Date of Patent: December 27, 2011Assignee: TK Holdings, Inc.Inventors: Sudhakar R. Ganta, Graylon K. Williams, Cory G. Miller
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Publication number: 20110306624Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: February 3, 2010Publication date: December 15, 2011Inventors: Songnian Lin, Xibin Liao, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
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Publication number: 20110306542Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.Type: ApplicationFiled: June 9, 2011Publication date: December 15, 2011Applicant: Receptos, Inc.Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Liming Huang, Junko Tamiya, Mark T. Griffith, Thomas Fowler, Andrew Novak, Michael Knaggs, Premji Meghani
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Publication number: 20110301180Abstract: It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner.Type: ApplicationFiled: April 25, 2011Publication date: December 8, 2011Applicant: Stanford UniversityInventors: James P. Collman, Paul Clifford Herrmann, David Alvin Tyvoll, Richard Decreau, Brian Stanley Bull, Christopher Jeffrey Barile