Carbon In The Ring Patents (Class 558/288)
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Publication number: 20130252009Abstract: A dioxaborinane compound, or salt thereof, where boron has two oxy substituents, each independently substituted with H, alkyl, alkenyl, aryl, —C(O)R3, —C(O)OR3, —C(O)NHR3, or the two oxy substituents, together with the oxygen atoms to which they are bonded, join to form a 5- or 6-membered ring; and R3 is H, alkyl, alkenyl, or aryl, where the alkyl and alkenyl are optionally interrupted with one or more oxygen or sulfur atoms; and where boron also has the substituent -L-X1—PG1; where L may be absent, or alkylenyl, alkenylenyl, or arylene, where the alkylenyl and alkenylenyl are optionally interrupted with one or more oxygen or sulfur atoms; X1 is absent, or is amino, oxo, thio, or phosphino; and PG1 is a polymerizable group. The dioxaborinane compound can be used as a wood preservative.Type: ApplicationFiled: July 20, 2012Publication date: September 26, 2013Inventors: William B. CARLSON, Gregory D. Phelan
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Patent number: 8530689Abstract: The invention concerns processes for the synthesis of a compound of the formula: wherein: R1 and R2 are each, independently, C1-C12 alkyl, CO2R3, OR4, R5(OR6), or C6-C18 aryl; R3-R6 are each, independently, C1-C12 alkyl or C6-C12 aryl; and n and m are each, independently, O or an integer from 1-5; said process comprising:—contacting a compound of the formula H0-R7-0H with BH3 and a compound of the formula in the presence of a nickel-containing catalyst to produce a first product, where R7 is a C2-C12 hydrocarbon group and X is a halogen, OMs or OTs;—contacting the first product in situ with a compound of the formula: in the presence of a nickel-containing catalyst to produce a compound of formula I, where Z is a halogen.Type: GrantFiled: April 30, 2009Date of Patent: September 10, 2013Assignee: The Trustees Of The University Of PennsylvaniaInventors: Virgil Percec, Brad Matthew Rosen, Daniela A. Wilson, Christopher J. Wilson
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Publication number: 20130231304Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.Type: ApplicationFiled: March 18, 2011Publication date: September 5, 2013Applicant: ANACOR PHARMACEUTICALS, INC.Inventors: Robert T. Jacobs, Daitao Chen, Matthew Orr, Jacob J. Plattner
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Publication number: 20130210053Abstract: The invention provides luminescent solid-state compositions comprising difluoroboron beta-diketonates wherein the compositions can exhibit mechanochromic luminescence. The mechanochromic effect on the luminescence can be reversible, such as thermally reversible. Various solid-state forms of the invention can have emission spectra that differ from the properties of the respective difluoroboron beta-diketonate in solution. The mechanochromic effect can be stimulated by pressure such as hand-writing, and can be reversed over a period of minutes to hours at room temperature. The invention also provides methods of making and methods of using the solid-state compositions, such as for sensors and for information displays for use in biological sensing, and in art, design, and consumer products.Type: ApplicationFiled: December 1, 2010Publication date: August 15, 2013Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Cassandra L. Fraser, Guoqing Zhang
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Patent number: 8507711Abstract: A flame-retardant compound has a structure represented by formula (2): (Ar2—O—CO—O—)nA2-X-A1(—O—CO—O—Ar1)m??(2) wherein A1 and A2 each independently represents a substituted or unsubstituted aromatic group; X represents a divalent group represented by —S—, —O—, —CO—, —CN—, —CH2—, —C(CH3)2—, —CH(CH3)—, —NH—, —SO— or —SO2—; Ar1 and Ar2 each independently represents a substituted or unsubstituted phenyl group; and m and n each independently represents an integer of 1 to 3.Type: GrantFiled: December 20, 2011Date of Patent: August 13, 2013Assignee: Fuji Xerox Co., Ltd.Inventors: Masato Mikami, Masayuki Okoshi, Kazuya Yamanoi
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Publication number: 20130203988Abstract: The invention relates to processes of making bortezomib of formula (1) enantiomers thereof and/or intermediates thereof, comprising at least one step of coupling a carboxylic acid with an amine, wherein the coupling step is performed in a presence of the compound of formula (8), wherein A is C1-C6 alkyl group, preferably wherein A is n-propyl group.Type: ApplicationFiled: October 14, 2010Publication date: August 8, 2013Applicant: Synthon BVInventors: Jakub Castulik, Miroslav Zabadal
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Publication number: 20130190332Abstract: Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.Type: ApplicationFiled: July 7, 2011Publication date: July 25, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Stuart Ince, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer, William Scott
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Publication number: 20130184484Abstract: The present invention relates to the process for preparing a boronic acid or ester chemically, in which an aromatic compound is reacted with a boronating agent, in the presence of magnesium metal (Mg0). The invention also relates to the boronic acids or esters that can be obtained by means of this process and to the use thereof for example as a synthesis intermediate, in the Suzuki reaction, in the pharmaceutical or alternatively electronics field.Type: ApplicationFiled: March 5, 2013Publication date: July 18, 2013Applicant: Universite De Nice Sophia AntipolisInventor: Universite De Nice Sophia Antipolis
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Publication number: 20130172565Abstract: Methods include formation of 4-chloro-2-fluoro-3-substituted-phenylboronic acid pinacol esters. The method comprises contacting a 1-chloro-3-fluoro-2-substituted benzene with an alkyl lithium to form a lithiated 1-chloro-3-fluoro-2-substituted benzene. The lithiated 1-chloro-3-fluoro-2-substituted benzene is contacted with an electrophilic boronic acid derivative to form a 4-chloro-2-fluoro-3-substituted-phenylboronate. The 4-chloro-2-fluoro-3-substituted-phenylboronate is reacted with an aqueous base to form a (4-chloro-2-fluoro-3-substituted-phenyl)trihydroxyborate. The (4-chloro-2-fluoro-3-substituted-phenyl)trihydroxyborate is reacted with an acid to form a 4 chloro-2-fluoro-3-substituted-phenylboronic acid. The 4-chloro-2-fluoro-3-substituted-phenylboronic acid is reacted with 2,3-dimethyl-2,3-butanediol to form 4-chloro-2-fluoro-3-substituted-phenylboronic acid pinacol esters.Type: ApplicationFiled: December 20, 2012Publication date: July 4, 2013Applicant: DOW AGROSCIENCES LLCInventor: DOW AGROSCIENCES LLC
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Publication number: 20130165390Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: ApplicationFiled: November 2, 2012Publication date: June 27, 2013Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventor: Millennium Pharmaceuticals, Inc.
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Patent number: 8470803Abstract: This invention provides, among other things, novel compounds useful for treating inflammatory conditions, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.Type: GrantFiled: September 10, 2009Date of Patent: June 25, 2013Assignee: Anacor Pharmaceuticals, Inc.Inventors: Tsutomu Akama, Jacob J. Plattner
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Patent number: 8461135Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.Type: GrantFiled: September 19, 2011Date of Patent: June 11, 2013Assignee: Anacor Pharmaceuticals, Inc.Inventors: Tsutomu Akama, Yong-Kang Zhang, Charles Z. Ding, Jacob J. Plattner, Kirk R. Maples, Yvonne Freund, Virginia Sanders, Yi Xia, Stephen J. Baker, James A. Nieman, Xiaosong Lu, Marcelo Sales, Rashmi Sharma, Rajeshwar Singh, Robert T. Jacobs, Daitao Chen, Michael Richard Kevin Alley
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Patent number: 8440642Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.Type: GrantFiled: September 1, 2011Date of Patent: May 14, 2013Assignee: Anacor Pharmaceuticals, Inc.Inventors: Stephen J. Baker, Tsutomu Akama, Carolyn Bellinger-Kawahara, Vincent S. Hernandez, Karin M. Hold, James J. Leyden, Kirk Maples, Jacob J. Plattner, Virginia Sanders, Yong-Kang Zhang
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Publication number: 20130085277Abstract: The present invention relates to a process for the preparation of bortezomib (Formula I) and its intermediates.Type: ApplicationFiled: February 9, 2011Publication date: April 4, 2013Applicant: RANBAXY LABORATORIES LIMITEDInventors: Satish Kumar, Venugopal Venkatarama Durvasula, Parendu Dhirajlal Rathod, Ram Chander Aryan
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Publication number: 20130079305Abstract: 3-substituted vinylboronates and their use in the treatment of cancer such as colorectal cancer are disclosed. In some embodiments, the 3-substituted vinylboronates have the general Formula I: with the variables in the formula being as defined in the specification.Type: ApplicationFiled: May 31, 2011Publication date: March 28, 2013Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.Inventors: Morris Srebnik, Abed Al-Aziz Quntar, Alina Botvinik, Arie Dagan
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Publication number: 20130035501Abstract: The present invention is a process comprising contacting a compound of formula 6: or a pharmaceutically acceptable salt thereof; with a deprotecting reagent to form a compound of formula A: or a pharmaceutically acceptable salt thereof; where R is H or OR1; R1 and each R1? are protecting groups; R1? is H or OH, and n is 0, 1, 2, 3, 4, or 5.Type: ApplicationFiled: April 6, 2011Publication date: February 7, 2013Applicant: GLAXOSMITHKLINE LLCInventors: Jose J. Conde, John Anthony Kowalski, Matthew Allen Zajac
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Publication number: 20130035311Abstract: The present invention provides compounds of Formula I along with compositions containing the same and methods of use thereof in treating oxidative stress.Type: ApplicationFiled: August 1, 2012Publication date: February 7, 2013Inventors: Katherine J. Franz, Filip Kielar
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Publication number: 20130023689Abstract: The present invention relates to a process for the borylation of organohalides.Type: ApplicationFiled: July 19, 2012Publication date: January 24, 2013Applicant: BASF SEInventors: Joachim Schmidt-Leithoff, Stefan Pichlmair, Charles Bello
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Patent number: 8349814Abstract: The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.Type: GrantFiled: March 16, 2011Date of Patent: January 8, 2013Assignee: Infinity Pharmaceuticals, Inc.Inventors: Julian Adams, Mark L. Behnke, Alfredo C. Castro, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Tao Liu, Daniel A. Snyder, Thomas T. Tibbitts
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Publication number: 20130005968Abstract: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.Type: ApplicationFiled: September 14, 2012Publication date: January 3, 2013
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Patent number: 8343944Abstract: This invention largely relates to 3,4,6-trisubstituted benzoxaborole compounds, and their use for treating bacterial infections.Type: GrantFiled: July 27, 2010Date of Patent: January 1, 2013Assignee: Anacor Pharmaceuticals, Inc.Inventors: Yi Xia, Michael Richard Kevin Alley, Yasheen Zhou, Rajeshwar Singh, Charles Ding, Kathy Cao, Jacob J. Plattner, Ligong Ou, Guofeng Jia, Neerja Saraswat, Sreekanth Ramachandran, Ding Zhou
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Publication number: 20120302434Abstract: The present invention provides a catalyst complex or ligand, and compositions thereof, for use in a variety of organic reactions having high reactivity and enantioselectivity. The catalyst is a N-heterocyclic carbene having three fused rings with first and second rings being six-membered rings and the third being a five-membered ring. The first ring is fused to the second and has four substituents. The second ring has two nitrogens flanking a carbene atom with one nitrogen bound to a substituent. The carbene atom may optionally be bonded to a metal. The third ring is fused to the second ring and contains two nitrogens. The third ring of the catalyst has a double bond and two substituents on adjacent non-fused carbons. A non-fused nitrogen of the third ring is partially bonded to another substituent. Methods for the synthesis and use of the catalyst embodiments of the present invention are also provided.Type: ApplicationFiled: May 22, 2012Publication date: November 29, 2012Applicant: FLORIDA STATE UNIVERSITY RESEARCH FOUNDATIONInventors: D. TYLER MCQUADE, Jin Kyoon Park, Matthew D. Rexford, Hershel H. Lackey
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Publication number: 20120289733Abstract: Borates, compositions comprising chiral (cyclic and acyclic) and achiral (cyclic and acyclic) borates; chiral (cyclic and acyclic) and achiral (cyclic and acyclic) biborates; and methods for their synthesis. Additionally, a significantly improved synthetic protocol for the synthesis of wide range of boronates starting from borates or biborates and Grignard or organolithium reagents that can be used for kilo lab and commercial scale production.Type: ApplicationFiled: May 11, 2012Publication date: November 15, 2012Applicant: Anderson Development CompanyInventors: Glenn L. HEISE, Malgorzata Myslinska
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Publication number: 20120289699Abstract: The present invention provides a synthetic process for producing bortezomib using a novel intermediate. The present invention also provides a process for purifying bortezomib anhydride, and a new crystalline polymorph of bortezomib anhydride.Type: ApplicationFiled: May 12, 2011Publication date: November 15, 2012Inventors: Julian Paul Henschke, Aiping Xie, Xin Yan Huang, Yung Fa Chen
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Publication number: 20120289686Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.Type: ApplicationFiled: January 23, 2012Publication date: November 15, 2012Applicant: Anacor Pharmaceuticals, Inc.Inventors: Stephen J. Baker, Tsutomu Akama, Michael Richard Kevin Alley, Stephen J. Benkovic, Michael DiPierro, Vincent S. Hernandez, Karin M. Hold, Isaac Kennedy, Igor Likhotvorik, Weimin Mao, Kirk R. Maples, Jacob J. Plattner, Fernando Rock, Virginia Sanders, Aaron M. Stemphoski, George Petros Yiannikouros, Siead Zagar, Yong-Kang Zhang, Huchen Zhou
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Publication number: 20120252789Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, M4, Y1, Y2, V, W, n, m and o have the meanings given in Claim 1, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.Type: ApplicationFiled: November 22, 2010Publication date: October 4, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Frank Stieber, Dirk Wienke
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Publication number: 20120226041Abstract: The invention provides catalysts and methods for preparing boronate esters. The methods can include the borylation of a secondary or primary C—H bond, for example, by contacting a reactant having a methylene or methyl and a diboron bis-ester in the presence of an effective catalyst. The contacting can be in the presence of an iridium complex, to effect borylation of the secondary or primary C—H bond, thereby providing the boronate ester. The boronate esters can be readily isolated and/or converted into other useful compounds and intermediates.Type: ApplicationFiled: March 5, 2012Publication date: September 6, 2012Applicant: The Board of Trustees of the University of IllinoisInventors: John F. Hartwig, Carl W. Liskey
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Publication number: 20120220794Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of halogenoalkanes.Type: ApplicationFiled: June 18, 2010Publication date: August 30, 2012Applicant: LEK PHARMACEUTICALS D.D.Inventors: Ivana Gazic Smilovic, Zdenko Casar
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Publication number: 20120184768Abstract: Preparation method of aromatic boronate compound is provided, in which the is as follows: reacting aromatic amine Ar-NH2, with diboronic ester and alkyl nitrite in the presence of organic solvent, where Ar represents non-heterocyclic aryl. It enables for the first time the preparation of aromatic boronate from aromatic amine in one step by the present method.Type: ApplicationFiled: August 27, 2010Publication date: July 19, 2012Applicant: PEKING UNIVERSITYInventors: Fanyang Mo, Yubo Jiang, Di Qiu, Wengang Yao, Yan Zhang, Jianbo Wang
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Publication number: 20120129926Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating trifluoromethylphenylene cyclopentylene compounds represented in formula (I) and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.Type: ApplicationFiled: May 26, 2010Publication date: May 24, 2012Applicant: LEO PHARMA A/SInventor: Bjarne Nørremark
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Publication number: 20120115813Abstract: This invention relates to, among other items, benzoxaborole compounds and their use for treating bacterial infections.Type: ApplicationFiled: September 7, 2011Publication date: May 10, 2012Applicant: Anacor Pharmaceuticals, Inc.Inventors: Vincent S. Hernandez, Charles Ding, Jacob J. Plattner, Michael Richard Kevin Alley, Fernando Rock, Suoming Zhang, Eric Easom, Xianfeng Li, Ding Zhou
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Publication number: 20120053170Abstract: The present invention relates to nicotinamide derivatives of formula (I), to compositions containing same, and to the therapeutic use thereof, in particular as anticancer drugs. The invention also relates to the method for preparing said compounds, as well as to some of the intermediate products.Type: ApplicationFiled: March 22, 2010Publication date: March 1, 2012Applicant: SANOFIInventors: Jérome Arigon, Claude Bernhart, Monsif Bouaboula, Romain Combet, Sandrine Hilairet, Samir Jegham
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Patent number: 8115026Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.Type: GrantFiled: December 2, 2009Date of Patent: February 14, 2012Assignee: Anacor Pharmaceuticals, Inc.Inventors: Stephen J. Baker, Tsutomu Akama, Michael Richard Kevin Alley, Steven J. Benkovic, Michael DiPierro, Vincent S. Hernandez, Karin M. Hold, Isaac Kennedy, Igor Likhotvorik, Weimin Mao, Kirk R. Maples, Jacob J. Plattner, Fernando Rock, Virginia Sanders, Aaron M. Stemphoski, George Petros Yiannikouros, Siead Zegar, Yong-Kang Zhang, Huchen Zhou
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Patent number: 8106031Abstract: Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.Type: GrantFiled: May 2, 2007Date of Patent: January 31, 2012Assignee: Anacor Pharmaceuticals, Inc.Inventors: Ving Lee, Jacob J. Plattner, Stephen J. Benkovic, Stephen J. Baker, Kirk R. Maples, Carolyn Bellinger-Kawahara, Tsutomu Akama, Yong-Kang Zhang, Rajeshwar Singh, Vittorio A. Sauro
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Publication number: 20110306560Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.Type: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Julian Adams, Yu-Tung Ma, Ross Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
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Publication number: 20110282090Abstract: The present invention relates to the process for preparing a boronic acid or ester chemically, in which an aromatic compound is reacted with a boronating agent, in the presence of magnesium metal (Mg0). The invention also relates to the boronic acids or esters that can be obtained by means of this process and to the use thereof for example as a synthesis intermediate, in the Suzuki reaction, in the pharmaceutical or alternatively electronics field.Type: ApplicationFiled: November 2, 2009Publication date: November 17, 2011Applicant: Universite De Nice Sophia AntipolisInventors: Isabel Dunach, Sandra Olivero, Christine Pintaric
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Patent number: 8039451Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.Type: GrantFiled: July 21, 2009Date of Patent: October 18, 2011Assignee: Anacor Pharmaceuticals, Inc.Inventors: Stephen J. Baker, Tsutomu Akama, Carolyn Bellinger-Kawahara, Vincent S. Hernandez, Karin M. Hold, James J. Leyden, Kirk Maples, Jacob J. Plattner, Virginia Sanders, Yong-Kang Zhang
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Patent number: 8039450Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.Type: GrantFiled: March 5, 2009Date of Patent: October 18, 2011Assignee: Anacor Pharmaceuticals, Inc.Inventors: Tsutomu Akama, Yong-Kang Zhang, Charles Z. Ding, Jacob J. Plattner, Kirk R. Maples, Yvonne Freund, Virginia Sanders, Yi Xia, Stephen J. Baker, James A. Nieman, Xiaosong Lu, Marcelo Sales, Rashmi Sharma, Rajeshwar Singh, Robert Jacobs, Daitao Chen, Michael Richard Kevin Alley
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Publication number: 20110230440Abstract: The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.Type: ApplicationFiled: March 16, 2011Publication date: September 22, 2011Inventors: Julian Adams, Mark L. Behnke, Alfredo C. Castro, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Tao Liu, Daniel A. Snyder, Thomas T. Tibbitts
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Publication number: 20110207957Abstract: The invention concerns processes for the synthesis of a compound of the formula: wherein: R1 and R2 are each, independently, C1-C12 alkyl, CO2R3, OR4, R5(OR6), or C6-C18 aryl; R3-R6 are each, independently, C1-C12 alkyl or C6-C12 aryl; and n and m are each, independently, O or an integer from 1-5; said process comprising: —contacting a compound of the formula H0-R7-0H with BH3 and a compound of the formula in the presence of a nickel-containing catalyst to produce a first product, where R7 is a C2-C12 hydrocarbon group and X is a halogen, OMs or OTs; —contacting the first product in situ with a compound of the formula: in the presence of a nickel-containing catalyst to produce a compound of formula I, where Z is a halogen.Type: ApplicationFiled: April 30, 2009Publication date: August 25, 2011Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: Virgil Percec, Brad Matthew Rosen, Daniela A. Wilson, Christopher J. Wilson
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Publication number: 20110207701Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.Type: ApplicationFiled: August 16, 2010Publication date: August 25, 2011Applicant: Anacor Pharmaceuticals, Inc.Inventors: Huchen Zhou, Dazhong Ding, Yasheen Zhou, Yong-Kang Zhang, Jacob J. Plattner
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Publication number: 20110190235Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.Type: ApplicationFiled: August 6, 2010Publication date: August 4, 2011Applicant: Anacor Pharmaceuticals, Inc.Inventors: Daitao Chen, Matthew Orr, Jessica Sligar, Robert Jacobs, Jacob J. Plattner
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Publication number: 20110172187Abstract: This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.Type: ApplicationFiled: November 11, 2010Publication date: July 14, 2011Applicant: Anacor Pharmaceuticals, Inc.Inventors: Vincent S. HERNANDEZ, Xiangeng Li, Suoming ZHANG, Tsutomu AKAMA, Yanchen ZHANG, Yang LIU, Jacob J. PLATTNER, Michael Richard Kevin ALLEY, Yasheen ZHOU, James A. NIEMAN
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Publication number: 20110136763Abstract: This invention largely relates to 3,4,6-trisubstituted benzoxaborole compounds, and their use for treating bacterial infections.Type: ApplicationFiled: July 27, 2010Publication date: June 9, 2011Applicants: Anacor Pharmaceuticals, Inc., GlaxoSmithKline LLCInventors: Yi Xia, Michael Richard Kevin Alley, Yasheen Zhou, Rajeshwar Singh, Charles Ding, Kathy Cao, Jacob J. Plattner, Ligong Ou, Guofeng Jia, Neerja Saraswat, Sreekanth Ramachandran, Ding Zhou
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Publication number: 20110060146Abstract: The present invention provides a compound represented by the following general formula (I): or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing such a compound, and the like. The compound or a pharmaceutically acceptable salt thereof, the pharmaceutical composition containing such a compound, or the like is useful as a medicine or the like for therapy of benign prostatic hyperplasia, cancer, osteoporosis, psoriasis, secondary hyperparathyroidism, chronic glomerulonephritis, lupus nephritis and/or diabetic nephropathy and the like.Type: ApplicationFiled: November 15, 2010Publication date: March 10, 2011Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: TADAKATSU TAKAHASHI, YOSHIYUKI ONO, HIROTAKA KASHIWAGI, TSUYOSHI HANEISHI, KAZUKI SHIMIZU
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Publication number: 20100267981Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.Type: ApplicationFiled: December 2, 2009Publication date: October 21, 2010Applicant: Anacor Pharmaceuticals, Inc.Inventors: Stephen J. Baker, Tsutomu Akama, Michael Richard Kevin Alley, Steven J. Benkovic, Michael DiPierro, Vincent S. Hernandez, Karin M. Hold, Isaac Kennedy, Igor Likhotvorik, Weimin Mao, Kirk R. Maples, Jacob J. Plattner, Fernando Rock, Virginia Sanders, Aaron M. Stemphoski, George Petros Yiannikouros, Siead Zegar, Yong-Kang Zhang, Huchen Zhou
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Patent number: 7767657Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.Type: GrantFiled: August 16, 2006Date of Patent: August 3, 2010Assignee: Anacor Pharmaceuticals, Inc.Inventors: Stephen J. Baker, Tsutomu Akama, Vincent S. Hernandez, Karin M. Hold, Kirk R. Maples, Jacob J. Plattner, Virginia Sanders, Yong-Kang Zhang, Gregory Fieldson
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Publication number: 20100174072Abstract: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.Type: ApplicationFiled: February 16, 2010Publication date: July 8, 2010
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Patent number: 7714159Abstract: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.Type: GrantFiled: March 24, 2005Date of Patent: May 11, 2010
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Publication number: 20090325903Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: ApplicationFiled: June 16, 2009Publication date: December 31, 2009Applicant: Millennium Pharmaceuticals, Inc.Inventors: Eric L. Elliott, Abu J. Ferdous, Michael J. Kaufman, Sonja A. Komar, Debra L. Mazaik, Quentin J. McCubbin, Phuong Nguyen, Vaithianathan Palaniappan, Raymond D. Skwierczynski, Nobel T. Truong, Csanad M. Varga, Peter N. Zawaneh