Carbon In The Ring Patents (Class 558/288)
  • Patent number: 11008346
    Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: February 21, 2020
    Date of Patent: May 18, 2021
    Assignee: VENATORX PHARMACEUTICALS, INC.
    Inventors: Christopher J. Burns, Denis Daigle, Bin Liu, Randy W. Jackson, Jodie Hamrick, Daniel McGarry, Daniel C. Pevear, Robert E. Lee Trout
  • Patent number: 10435419
    Abstract: The invention relates to novel process for preparation of Tavaborole. The invention also relates to novel polymorphic forms of Tavaborole and process for preparation of those polymorphic forms. The invention also relates to process for purification of Tavaborole to obtain the Tavaborole in significantly high yield and substantially pure form.
    Type: Grant
    Filed: July 21, 2016
    Date of Patent: October 8, 2019
    Assignee: Biophore India Pharmaceuticals PVT. Ltd.
    Inventors: Manik Reddy Pullagurla, Mecheril Valsan Nanda Kumar, Bhaskar Reddy Pitta, Jagadeesh Babu Rangisetty
  • Patent number: 10344069
    Abstract: The present invention relates to a process for the preparation of Liraglutide, which comprises: a) synthesis of suitable fragments (protected) by solid phase peptide synthesis; b) coupling of the suitable fragments on solid support; c) concurrently cleaving the protected peptide from the solid support and de-protecting the peptide; d) purification of Liraglutide (crude) on reverse phase HPLC; e) isolating pure Liraglutide.
    Type: Grant
    Filed: October 31, 2015
    Date of Patent: July 9, 2019
    Assignee: Auro Peptides Ltd.
    Inventors: Suresh Kumar Vadlamani, Patil Nilesh Dagadu, Mohammed Abdul Shafee, Sanjay Devidas Patil, Nagana Goud Agasaladinni
  • Patent number: 9738663
    Abstract: The present invention relates to a process for the preparation of aminoaryl- and aminoheteroaryl boronic acids and esters thereof of formula (I) in high yield. The claimed process uses diarylketal formula (V) to generate an arylbromide of formula (III) in which the amino-group is protected as bisarylmethylidenimino-group, which is then transformed into a formula (I) compound.
    Type: Grant
    Filed: April 30, 2014
    Date of Patent: August 22, 2017
    Assignee: EUTICALS S.P.A.
    Inventors: Michael Nonnenmacher, Torsten Busch
  • Publication number: 20150133402
    Abstract: This invention provides, among other things, novel compounds useful for treating bacterial infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: STEPHEN J. BAKER, VINCENT S. HERNANDEZ, RASHMI SHARMA, JAMES A. NIEMAN, TSUTOMU AKAMA, YONG-KANG ZHANG, JACOB J. PLATTNER, MICHAEL RICHARD KEVIN ALLEY, RAJESHWAR SINGH, FERNANDO ROCK
  • Publication number: 20150119580
    Abstract: Boronic esters and boronic acids are synthesized at ambient temperature in an ethereal solvent by the reaction of Grignard reagents with a boron-containing substrate. The boron-containing substrate may be a boronic ester such as pinacolborane, neopentylglycolborane, or a dialkylaminoborane compound such as diisopropylaminoborane. The Grignard reagents may be pre-formed or generated from an alkyl, alkenyl, aryl, arylalkyl, heteroaryl, vinyl, or allyl halide compound and Mg0. When the boron-containing substrate is a boronic ester, the reactions generally proceed at room temperature without added base in about 1 to 3 hours to form a boronic ester compound. When the boron-containing substrate is a dialkylaminoborane compound, the reactions generally proceed to completion at 0° C. in about 1 hour to form a boronic acid compound.
    Type: Application
    Filed: July 20, 2012
    Publication date: April 30, 2015
    Applicant: The Regents of the University of California
    Inventors: Jacob W. Clary, Bakthan Singaram
  • Publication number: 20150119364
    Abstract: 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: Application
    Filed: November 10, 2014
    Publication date: April 30, 2015
    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 Maples, Jacob J. Plattner, Fernando Rock, Virginia Sanders, Aaron M. Stemphoski, George Petros Yiannikouros, Siead Zegar, Yong-Kang Zhang, Huchen Zhou
  • Patent number: 9000205
    Abstract: The present invention relates to a process for the synthesis of 2-cyanophenylboronic acid and the esters and salts thereof of formula (II), which are intermediates of the synthesis of active pharmaceutical ingredients such as Perampanel or E2040. formula (II): (II).
    Type: Grant
    Filed: July 24, 2013
    Date of Patent: April 7, 2015
    Assignee: F.I.S.—Fabbrica Italiana Sintetici S.p.A.
    Inventors: Francesco Fontana, Emiliano Rossi, Christian De Filippo
  • Publication number: 20150080339
    Abstract: The present disclosure relates to boron-based 4-hydroxytamoxifen and endoxifen prodrugs and the synthesis of the same. Further, the present disclosure teaches the utilization of the boron-based 4-hydroxytamoxifen and endoxifen prodrugs in a treatment for breast cancer.
    Type: Application
    Filed: March 5, 2013
    Publication date: March 19, 2015
    Inventors: Guangdi Wang, Shilong Zheng, Quan Jiang, Qiu Zhong, Qiang Zhang
  • Publication number: 20150072942
    Abstract: 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: Application
    Filed: April 8, 2014
    Publication date: March 12, 2015
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Julian Adams, Yu-Ting Ma, Ross L. Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
  • Patent number: 8975269
    Abstract: 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: Grant
    Filed: July 29, 2014
    Date of Patent: March 10, 2015
    Assignee: Florida State University Research Foundation
    Inventors: D. Tyler McQuade, Jin Kyoon Park, Matthew D. Rexford, Hershel H. Lackey
  • Publication number: 20150065743
    Abstract: Methods for the selective borylation of arenes, including arenes substituted with an electron-withdrawing group (e.g., 1-chloro-3-fluoro-2-substituted benzenes) are provided. The methods can be used, in some embodiments, to efficiently and regioselectively prepare borylated arenes without the need for expensive cryogenic reaction conditions.
    Type: Application
    Filed: September 5, 2014
    Publication date: March 5, 2015
    Inventors: Milton R. Smith, III, Robert E. Maleczka, JR., Hao Li, Chathurika Jayasundara, Jossian Oppenheimer, Dmitrijs Sabasovs
  • Publication number: 20150065459
    Abstract: 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: Application
    Filed: November 10, 2014
    Publication date: March 5, 2015
    Inventors: Stephen J. BAKER, Tsutomu Akama, Carolyn BELLINGER-KAWAHARA, Vincent S. Hernandez, Karin M. Hold, James J. Leyden, Kirk R. Maples, Jacob J. Plattner, Virginia Sanders, Yong-Kang Zhang
  • Publication number: 20150038706
    Abstract: 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: Application
    Filed: March 6, 2014
    Publication date: February 5, 2015
  • Publication number: 20150021586
    Abstract: This invention relates to deuterated aryl-anthracene compounds that are useful in electronic applications. It also relates to electronic devices in which the active layer includes such a deuterated compound.
    Type: Application
    Filed: October 8, 2014
    Publication date: January 22, 2015
    Inventors: DANIEL DAVID LECLOUX, Adam Fennimore, Weiying Gao, Nora Sabina Radu, Weishi Wu, Vsevolod Rostovtsev, Michael Henry Howard, JR., Hong Meng, Yulong Shen, Jeffrey A. Merlo, Eric Maurice Smith
  • Publication number: 20150018311
    Abstract: The present invention relates to compounds of Formula (I) wherein R1 and R3 are hydrogen; R2 and R4, which may be the same or different, are hydrogen, a C1-6 alkyl group optionally substituted by an aryl group which may itself be substituted, the substituent group including an alkyl group or an —OR group in which R is a C1-3 alkyl group, with one or more hydrogen atoms optionally replaced with a halogen atom; or an aryl group which may be substituted, the substituent group including an alkyl group or an —OR group in which R is a C1-3 alkyl group, with one or more hydrogen atoms optionally replaced with a halogen atom; with the proviso that R2 and R4 are not both hydrogen; the atom of R4 which is attached to C? is either a saturated carbon atom or an atom which is part of a 1 substituted aromatic ring; (AA)0-5 is an amino acid, amino acid derivative, peptide of up to 5 amino acids or a peptidomimetic thereof which optionally incorporates an N-terminal capping group, when the group is (AA)0 an N-terminal cappin
    Type: Application
    Filed: January 8, 2013
    Publication date: January 15, 2015
    Applicant: University of Tromsø
    Inventors: Tore Lejon, John Sigurd Svendsen, Alexey Gorovoy, Olga Gozhina
  • Patent number: 8933239
    Abstract: A bis(aryl)acetal has the formula wherein Y1 and Y2 are each independently chloro, bromo, iodo, mesylate, tosylate, triflate, or Bx, provided that Y1 and Y2 are not both selected from chloro, bromo, and iodo; each occurrence of Bx is independently a boron-containing functional group bonded to Ar1 or Ar2 via a boron atom; Ar1 and Ar2 are each independently unsubstituted or substituted C6-18 arylene, or unsubstituted or substituted C3-18 heteroarylene; provided that Ar1 and Ar2 are not covalently linked to each other to form a ring structure that includes —Ar1—O—C—O—Ar2—; and R1 and R2 are each independently hydrogen, unsubstituted or substituted C1-18 linear or branched alkyl, unsubstituted or substituted C3-20 cycloalkyl, unsubstituted or substituted C6-18 aryl, or unsubstituted or substituted C3-20 heteroaryl. The bis(aryl)acetal is useful as a monomer for oligoacetal and polyacetal synthesis via Suzuki polycondensation.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: January 13, 2015
    Assignee: Dow Global Technologies LLC
    Inventors: Matthias S. Ober, Duane R. Romer, John B. Etienne, Pulikkottil J. Thomas
  • Publication number: 20140371446
    Abstract: The disclosure is directed to: (a) phosphacycle ligands; (b) methods of using such phosphacycle ligands in bond forming reactions; and (c) methods of preparing phosphacycle ligands.
    Type: Application
    Filed: August 25, 2014
    Publication date: December 18, 2014
    Applicant: AbbVie Inc.
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Patent number: 8912169
    Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: December 16, 2014
    Assignee: VenatoRx Pharmaceuticals, Inc.
    Inventors: Christopher J. Burns, Denis Daigle, Bin Liu, Daniel McGarry, Daniel C. Pevear, Robert E. Lee Trout
  • Patent number: 8912339
    Abstract: 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: Grant
    Filed: December 20, 2012
    Date of Patent: December 16, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventor: Jossian Oppenheimer
  • Publication number: 20140357886
    Abstract: The present invention relates to a process for the synthesis of 2-cyanophenylboronic acid and the esters and salts thereof of formula (II), which are intermediates of the synthesis of active pharmaceutical ingredients such as Perampanel or E2040. formula (II): (II).
    Type: Application
    Filed: July 24, 2013
    Publication date: December 4, 2014
    Inventors: Francesco Fontana, Emiliano Rossi, Christian De Filippo
  • Publication number: 20140343314
    Abstract: 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: Application
    Filed: August 1, 2014
    Publication date: November 20, 2014
    Inventors: Eric L Elliott, Abu J. Ferdous, Michael J. Kaufman, Sonja A. Komar, Debra L. Mazaik, Quentin J. Mccubbin, Phuong M. Nguyen, Vaithianathan Palaniappan, Raymond D. Skwierczynski, Nobel T. Truong, Csanad M. Varga, Peter N. Zawaneh
  • Patent number: 8889656
    Abstract: 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: Grant
    Filed: April 30, 2013
    Date of Patent: November 18, 2014
    Assignee: Anacor Pharmaceuticals, Inc.
    Inventors: Stephen J. Baker, Tsutomu Akama, Carolyn Bellinger-Kawahara, Vincent S. Hernandez, Karin M. Hold, James J. Leyden, Kirk R. Maples, Jacob J. Plattner, Virginia Sanders, Yong-Kang Zhang
  • Publication number: 20140336402
    Abstract: 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: Application
    Filed: July 29, 2014
    Publication date: November 13, 2014
    Inventors: D. TYLER MCQUADE, JIN KYOON PARK, MATTHEW D. REXFORD, HERSHEL H. LACKEY
  • Patent number: 8859504
    Abstract: 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: Grant
    Filed: November 2, 2012
    Date of Patent: October 14, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Eric L. Elliott, Abu J. Ferdous, Michael J. Kaufman, Sonja A. Komar Lay, Debra L. Mazaik, Quentin J. McCubbin, Phuong M. Nguyen, Vaithianathan Palaniappan, Raymond D. Skwierczynski, Nobel T. Truong, Csanad M. Varga, Peter N. Zawaneh
  • Publication number: 20140288308
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Inventors: Corey James BRUMSTED, Hendrik MOORLAG, Roumen Nikolaev RADINOV, Yi REN, Pius WALDMEIER
  • Publication number: 20140274688
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Lindsey G. Fischer, Erich W. Baum, Gary D. Crouse, Carl DeAmicis, Beth Lorsbach, Jeff Petkus, Thomas C. Sparks, Gregory T. Whiteker
  • Publication number: 20140274954
    Abstract: The present disclosure provides boron-containing diacylhydrazines having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, and R5 are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: Sheela K. CHELLAPPAN, Robert E. Hormann, Inna Shulman
  • Publication number: 20140221631
    Abstract: 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: Application
    Filed: March 7, 2014
    Publication date: August 7, 2014
    Applicant: 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 Maples, Jacob J. Plattner, Fernando Rock, Virginia Sanders, Aaron M. Stemphoski, George Petros Yiannikouros, Siead Zagar, Yong-Kang Zhang, Huchen Zhou
  • Publication number: 20140213810
    Abstract: The invention relates to the preparation of chiral compounds, in particular to the preparation of chiral compounds which may be used as intermediates for the preparation of anti-diabetic agents, preferably sitagliptin.
    Type: Application
    Filed: April 6, 2012
    Publication date: July 31, 2014
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Matej Sova, Zdenko Casar, Gaj Stavber
  • Patent number: 8785674
    Abstract: A process for preparing a compound of formula VI wherein R1 and R6 is hydrogen, substituted or unsubstituted alkyl substituted or unsubstituted aryl, or substituted or unsubstituted aralkyl; R5 is B(OR2)(OR3), or wherein R2 and R3 independently from each other represent substituted or unsubstituted alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted aralkyl; or R2 and R3 cooperatively form a part of a 5- to 10-membered fused or unfused ring, optionally a chiral 5- to 10-membered fused or unfused ring; X is selected from Cl, Br, I; and * indicates a chiral center; is described.
    Type: Grant
    Filed: June 18, 2010
    Date of Patent: July 22, 2014
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Ivana Gazic Smilovic, Zdenko Casar
  • Publication number: 20140194384
    Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents.
    Type: Application
    Filed: January 2, 2014
    Publication date: July 10, 2014
    Inventors: Raja K. Reddy, Tomasz Glinka, Maxim Totrov, Scott Hecker
  • Publication number: 20140194385
    Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents. Other embodiments relate to pharmaceutical compositions containing boronic acid derivatives and additional excipient such as meglumine.
    Type: Application
    Filed: January 2, 2014
    Publication date: July 10, 2014
    Inventors: Raja K. Reddy, Tomasz Glinka, Maxim Totrov, Scott Hecker
  • Patent number: 8772536
    Abstract: 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: Grant
    Filed: August 12, 2013
    Date of Patent: July 8, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Edward J. Olhava, Mihaela Diana Danca
  • Publication number: 20140171390
    Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 19, 2014
    Applicant: VenatoRx Pharmaceuticals, Inc.
    Inventors: Christopher J. BURNS, Denis DAIGLE, Bin LIU, Daniel McGARRY, Daniel C. PEVEAR, Robert E. Lee TROUT
  • Patent number: 8703742
    Abstract: This invention relates to, among other items, benzoxaborole compounds and their use for treating bacterial infections.
    Type: Grant
    Filed: September 7, 2011
    Date of Patent: April 22, 2014
    Assignee: 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
  • Patent number: 8669207
    Abstract: This invention is related to compounds and/or compositions useful against pathogens affecting meats, plants, or plant parts. In one embodiment, the provided compounds are products of certain oxaborole moieties. In a further embodiment, the compound comprises a di-oxaborole compound. Delivery systems are also provided to take advantage of the volatile nature of these compounds and/or compositions.
    Type: Grant
    Filed: July 18, 2013
    Date of Patent: March 11, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Richard Martin Jacobson, Daniel Maclean, Esther Gachango
  • Publication number: 20140051661
    Abstract: The present invention provides resveratrol-based boron-containing analog! methods of use thereof in treatment of dyslipidemias and cancer.
    Type: Application
    Filed: February 15, 2012
    Publication date: February 20, 2014
    Applicants: The Texas A&M University System, Albert Einstein College of Medicine of Yeshiva University
    Inventors: Bhaskar C. Das, Fajun Yang, Xiaoping Zhao, Jeffrey E. Pessin, Haihong Zong, Jun-Yuan Ji
  • Publication number: 20140046086
    Abstract: The present invention provides efficient, economical and environmental friendly methods for synthesis of prostaglandin analogs including tafluprost and intermediates thereof. The invention involves a selective oxidation using in situ boronate ester protection and a unique crystallization method to remove the undesired isomers of fluorinated intermediates.
    Type: Application
    Filed: August 8, 2013
    Publication date: February 13, 2014
    Applicant: Scinopharm (Changshu) Pharmaceuticals, Ltd.
    Inventor: Wen-Hsien Wen
  • Publication number: 20140018301
    Abstract: 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: Application
    Filed: November 2, 2012
    Publication date: January 16, 2014
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Eric L. Elliott, Abu J. Ferdous, Michael J. Kaufman, Sonja A. Komar, Debra L. Mazaik, Quentin J. McCubbin, Phuong M. Nguyen, Vaithianathan Palaniappan, Raymond D. Skwierczynski, Nobel T. Truong, Csanad M. Varga, Peter N. Zawaneh
  • Publication number: 20130345172
    Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to 1 cyclic boronic acid ester derivatives and their use as therapeutic agents.
    Type: Application
    Filed: July 29, 2013
    Publication date: December 26, 2013
    Applicant: Rempex Pharmaceuticals, Inc.
    Inventors: Gavin Hirst, Raja Reddy, Scott Hecker, Maxim Totrov, David C. Griffith, Olga Rodny, Michael N. Dudley, Serge Boyer
  • Publication number: 20130337281
    Abstract: 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: Application
    Filed: August 23, 2013
    Publication date: December 19, 2013
    Applicant: Empire Technology Development LLC
    Inventors: William B. CARLSON, Gregory D. Phelan
  • Publication number: 20130331595
    Abstract: 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: Application
    Filed: August 12, 2013
    Publication date: December 12, 2013
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Edward J. Olhava, Mihaela Diana Danca
  • Publication number: 20130324757
    Abstract: An object of the present invention is to provide a method that enables the easy and efficient (high yield, high selectivity, low cost) preparation of a fluorine-containing olefin substituted with an organic group or groups from a fluorine-containing olefin. [Solution] The method for preparing a fluorine-containing olefin substituted with an organic group or groups, the method comprising a step of reacting a fluorine-containing olefin with an organic boron compound in the presence of an organic transition metal catalyst containing at least one transition metal selected from the group consisting of nickel, palladium, platinum, rhodium, ruthenium, and cobalt.
    Type: Application
    Filed: March 8, 2012
    Publication date: December 5, 2013
    Applicants: Daikin Industries, Osaka University
    Inventors: Takabumi Nagai, Kenji Adachi, Takashi Shibanuma, Sensuke Ogoshi, Masato Ohashi
  • Publication number: 20130316943
    Abstract: Disclosed herein are polybasic bacterial efflux pump inhibitors containing boronic acid functionality and their methods of synthesis, methods of use, and pharmaceutical compositions. Some embodiments include methods of treating or preventing a bacterial infection by co-administering to a subject infected with bacteria or at risk of infection with bacteria the efflux pump inhibitor with another anti-bacterial agent.
    Type: Application
    Filed: February 6, 2012
    Publication date: November 28, 2013
    Applicant: REMPEX PHARMACEUTICALS, INC.
    Inventors: Tomasz Glinka, Robert Higuchi, Scott Hecker, Brian Eastman, Olga Rodny
  • Patent number: 8551976
    Abstract: The present invention provides compounds of Formula I along with compositions containing the same and methods of use thereof in treating oxidative stress.
    Type: Grant
    Filed: August 1, 2012
    Date of Patent: October 8, 2013
    Assignee: Duke University
    Inventors: Katherine J. Franz, Filip Kielar
  • Patent number: 8546357
    Abstract: This invention provides novel compounds, methods of using the compounds, and pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: October 1, 2013
    Assignees: Eli Lilly and Company, Anacor Pharmaceuticals, Inc.
    Inventors: Tsutomu Akama, Terry William Balko, Jean Marie Defauw, Jacob J. Plattner, William Hunter White, Joseph Raymond Winkle, Yong-Kang Zhang, Yasheen Zhou
  • Publication number: 20130252009
    Abstract: 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: Application
    Filed: July 20, 2012
    Publication date: September 26, 2013
    Inventors: William B. CARLSON, Gregory D. Phelan
  • Patent number: 8530689
    Abstract: 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: Grant
    Filed: April 30, 2009
    Date of Patent: September 10, 2013
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Virgil Percec, Brad Matthew Rosen, Daniela A. Wilson, Christopher J. Wilson
  • Publication number: 20130231304
    Abstract: 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: Application
    Filed: March 18, 2011
    Publication date: September 5, 2013
    Applicant: ANACOR PHARMACEUTICALS, INC.
    Inventors: Robert T. Jacobs, Daitao Chen, Matthew Orr, Jacob J. Plattner