Phosphorus Attached Indirectly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 548/413)
  • Patent number: 10308672
    Abstract: A compound represented by formula (3): or an enantiomer thereof can be obtained by comprising: reacting a compound represented by formula (1): or an enantiomer thereof with 6-hydroxyhexanoic acid in a solvent in the presence of an additive such as 1-hydroxybenzotriazole and a condensing agent, and then mixing the resultant reaction mixture, water, and a base such as alkali metal hydroxide to produce a compound represented by formula (2): or an enantiomer thereof; and reacting the compound represented by formula (2) or an enantiomer thereof with 2-cyanoethyl-N,N,N?,N?-tetraisopropylphosphorodiamidite in a solvent in the presence of a coupling activator.
    Type: Grant
    Filed: April 17, 2017
    Date of Patent: June 4, 2019
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Kanako Sato, Hideki Ihara
  • Patent number: 9453222
    Abstract: This invention relates composition and methods for making and using chemically modified oligonucleotides agents for inhibiting gene expression.
    Type: Grant
    Filed: December 24, 2014
    Date of Patent: September 27, 2016
    Assignee: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Venkitasamy Kesavan, Kallanthottathil G. Rajeev
  • Patent number: 9376650
    Abstract: A method for securing the use of an aqueous medium under any substantial exclusion of metal ion interference is disclosed. A phosphonic acid compound containing: a selected phosphonate moiety and a moiety selected from a limited number of species; or hydrocarbon chains containing aminoalkylene phosphonic acid substituents; or alkylamino alkylene phosphonic acids containing an active moiety embodying N, O, and S. The technology can, by way of illustration, be used in numerous applications including secondary oil recovery, scale inhibition, industrial water treatment, paper pulp bleaching, dispersant treatment, sequestering application, brightness reversion avoidance and paper pulp treatment.
    Type: Grant
    Filed: January 21, 2009
    Date of Patent: June 28, 2016
    Assignee: ITALMATCH CHEMICALS SPA
    Inventors: Patrick Notte, Tessa Johnson, Albert Devaux
  • Publication number: 20150133368
    Abstract: Antiviral protease inhibitors, including macrocylic transition state inhibitors and peptidomimetics are disclosed, along with related antiviral compounds, and methods of using the same to treat or prevent viral infection and disease. The compounds possess broad-spectrum activity against viruses that belong to the picornavirus-like supercluster, which include important human and animal pathogens including noroviruses, sapoviruses, enteroviruses, poliovirus, foot-and-mouth disease virus, hepatitis A virus, human rhinovirus (cause of common cold), human coronavirus (another cause of common cold), transmissible gastroenteritis virus, murine hepatitis virus, feline infectious peritonitis virus, and severe acute respiratory syndrome coronavirus.
    Type: Application
    Filed: May 2, 2013
    Publication date: May 14, 2015
    Inventors: Kyeong-Ok Chang, Yunjeong Kim, William C. Groutas
  • Patent number: 8957223
    Abstract: This invention relates composition and methods for making and using chemically modified oligonucleotides agents for inhibiting gene expression.
    Type: Grant
    Filed: October 19, 2012
    Date of Patent: February 17, 2015
    Assignee: Alnylam Pharmaceuticals, Inc.
    Inventors: Muthiah Manoharan, Venkitasamy Kesavan, Kallanthottathil G. Rajeev
  • 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
  • Publication number: 20140309193
    Abstract: There are provided inter alia compounds of formula (I) wherein R1, R2, R3, R4a and R4b are as defined in the specification and their use in therapy, especially in the treatment of bacterial (e.g. pneumococcal) infections.
    Type: Application
    Filed: December 5, 2012
    Publication date: October 16, 2014
    Inventors: Peter William Andrew, Rana Lonnen, Mafalda Pires Damaso, Fritz-Frieder Frickel, Simon Christopher Hirst, Mark William Davies, Daniel Hamza
  • Patent number: 8846941
    Abstract: This document relates to functionalized (e.g., mono- or bi-functional) polymers (e.g., polyethylene glycol and related polymers) as well as methods and materials for making and using such functionalized polymers.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: September 30, 2014
    Assignee: QuiaPEG AB
    Inventor: Marek Kwiatkowski
  • Patent number: 8841257
    Abstract: Compounds which inhibit the activity of signal transducer and activator of transcription 3 (STAT3) are provided together with methods of making and using the same. The compounds are designed to bind to the SH2 domain of STAT3, preventing STAT3 from binding to receptors for interleukin-6 family cytokines, growth factors such as the platelet-derived growth factor, the epidermal growth factor, vascular endothelial growth factor, and other signaling molecules such as leptin. Blocking these interactions prevents STAT3 from being phosphorylated on Tyr705, which is required for the dimerization of STAT3, translocation to the nucleus, binding to STAT3 response elements on promotors, and transcription of genes. In addition to these activities, binding to the SH2 domain of STAT3 breaks up pre-formed dimmers, thereby preventing the transcriptional activity of the inhibitor.
    Type: Grant
    Filed: April 9, 2010
    Date of Patent: September 23, 2014
    Assignee: Board of Regents, The University of Texas System
    Inventors: John S. McMurray, Pijus K. Mandal, Warren S. Liao, Fredika Robertson, Xiaomin Chen, Ramesh Rajaopal, Zhiyong Ren
  • Publication number: 20140228323
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 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 pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Scott Louis COHEN, Dean Franklin Rigel
  • Publication number: 20140171633
    Abstract: Provided is a novel nucleic acid molecule that can be produced easily and efficiently and can inhibit the expression of a gene. The nucleic acid molecule is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes: a region (X); a linker region (Lx); and a region (Xc). The linker region (Lx) is linked between the regions (Xc) and (Xc). The region (Xc) is complementary to the region (X). At least one of the regions (X) and (Xc) includes the expression inhibitory sequence. The linker region (Lx) has a non-nucleotide structure including at least one of a pyrrolidine skeleton and a piperidine skeleton. According to this single-stranded nucleic acid molecule, it is possible to inhibit the expression of the target gene.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 19, 2014
    Applicant: BONAC CORPORATION
    Inventors: Tadaaki Ohgi, Hirotake Hayashi, Hisao Shirohzu, Tomohiro Hamasaki, Akihiro Itoh, Hiroshi Suzuki
  • Patent number: 8742133
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Grant
    Filed: August 13, 2008
    Date of Patent: June 3, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, Lijun Sun, Keizo Koya, Dinesh U. Chimmanamada, Shijie Zhang, Teresa Kowalcyzk-Przewloka, Hao Li
  • Patent number: 8703938
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: April 22, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
  • Patent number: 8703882
    Abstract: Phosphorus-containing benzoxazine-based bisphenols and derivatives thereof are disclosed. The phosphorus-containing benzoxazine-based bisphenols are prepared by reacting DOPO with benzoxazine to form the phosphorus-containing benzoxazine-based bisphenols. The phosphorus-containing benzoxazine-based bisphenols can further to form advanced epoxy resins. The advanced epoxy resins can further be cured to form flame retardant epoxy thermosets.
    Type: Grant
    Filed: December 28, 2010
    Date of Patent: April 22, 2014
    Assignee: National Chunghsing University
    Inventors: Ching-Hsuan Lin, Hung-Tse Lin, Sheng Lung Chang, Yu-Ming Hu
  • Patent number: 8691718
    Abstract: The present invention provides a novel ligand represented by the following formula and a novel transition metal complex having the ligand, which shows superior enantioselectivity and catalytic efficiency, particularly high catalyst activity, in various asymmetric synthesis reactions. A transition metal complex having, as a ligand, a compound represented by the formula wherein R4 is a hydrogen atom or a C1-6 alkyl group optionally having substituent(s), and R5 and R6 are each a C1-6 alkyl group optionally having substituent(s), or the formula is a group represented by the formula wherein ring B is a 3- to 8-membered ring optionally having substituent(s).
    Type: Grant
    Filed: September 20, 2006
    Date of Patent: April 8, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Mitsuhisa Yamano, Mitsutaka Goto, Shinji Kawaguchi, Masatoshi Yamada, Jun-ichi Kawakami
  • Publication number: 20140088303
    Abstract: Disclosed is a method for highly efficiently obtaining an optically active alcohol from a carbonyl compound highly enantioselectively. Also disclosed is a ligand used in such a method. Specifically, an optically active alcohol is obtained by reacting a carbonyl compound and an organozinc compound by using a ligand (L) shown below.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicants: Sekisui Medical Co., Ltd., National University Corporation Nagoya University
    Inventors: Kazuaki ISHIHARA, Manabu HATANO, Takashi MIYAMOTO
  • Publication number: 20140039200
    Abstract: The present invention relates to chiral ligands deriving from ?- and ?-amino acids, and from metal complexes formed from the same. The ligands are useful with catalytic gold complexes, particularly Au(I) complexes.
    Type: Application
    Filed: March 30, 2012
    Publication date: February 6, 2014
    Applicant: The University of Sussex
    Inventors: Eddy Michel Elie Viseux, Christopher Gallop, Mariusz Bobin
  • Publication number: 20140017797
    Abstract: This invention concerns isotopically coded or non-isotopically coded affinity-tags for analysis of certain target molecules in complex samples, in particular for mass spectrometric analysis of proteomic samples. The affinity-tags have the following general formula X-SPACER-OPO3H2, wherein X is a functional group or moiety capable of reacting with a functional group of a protein, peptide, DNA, lipid, sugar and/or steroid. These phosphate affinity tags (‘PTAG’) are capable of high but reversible binding to metal-oxides like TiO2. Due to this property, tagged sample fractions can be isolated from non-tagged sample fraction by affinity chromatography. The binding of organophosphate to metal-oxides remains intact during multiple washings of preferably acidic solutions to remove non-specifically bound components. PTAG's are also envisaged wherein X is selected such that it is capable of binding proteins, peptides, nucleic acid molecules, lipids, carbohydrates, steroids and the like.
    Type: Application
    Filed: December 13, 2011
    Publication date: January 16, 2014
    Applicant: De Staadt der Nederlanden, vert doorde minister van VWS
    Inventor: Jamila Willhelmina Zomer-Elhadari
  • Patent number: 8623522
    Abstract: Provided are a novel aromatic amine derivative having a specific structure and an organic electroluminescence device in which an organic thin layer comprising a single layer or plural layers including a light emitting layer is interposed between a cathode and an anode, wherein at leas one layer of the above organic thin layer contains the aromatic amine derivative described above in the form of a single component or a mixed component. Thus, the organic electroluminescence device is less liable to be crystallized in molecules, improved in a yield in producing the organic electroluminescence device and extended in a lifetime.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: January 7, 2014
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Nobuhiro Yabunouchi, Tetsuya Inoue
  • Patent number: 8624024
    Abstract: Disclosed is a method for highly efficiently obtaining an optically active alcohol from a carbonyl compound highly enantioselectively. Also disclosed is a ligand used in such a method. Specifically, an optically active alcohol is obtained by reacting a carbonyl compound and an organozinc compound by using a ligand (L) shown below.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: January 7, 2014
    Assignees: National University Corporation Nagoya University, Sekisui Medical Co., Ltd.
    Inventors: Kazuaki Ishihara, Manabu Hatano, Takashi Miyamoto
  • Publication number: 20130338110
    Abstract: The inventions disclosed include methods of treating cancers and related neoplasias, especially prostate cancer, with pharmaceutically acceptable salts comprising lipophilic cation moieties linked to nitroxide or linked to hydroxylamine anti-oxidant groups.
    Type: Application
    Filed: May 20, 2013
    Publication date: December 19, 2013
    Inventors: David A. ZARLING, Hirak S. BASU, Balaraman KALYANARAMAN, Joy JOSEPH
  • Publication number: 20130324531
    Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2 and R3 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
    Type: Application
    Filed: May 29, 2013
    Publication date: December 5, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, George Kenneth Ehrlich, Jin-Jun Liu, Hanspeter Michel, Binh Thanh Vu, Chunlin Zhao
  • Publication number: 20130253185
    Abstract: The present invention provides novel compounds and ligands that are useful in transition metal catalyzed cross-coupling reactions. For example, the compounds and ligands of the present invention are useful in palladium or gold catalyzed cross-coupling reactions.
    Type: Application
    Filed: November 17, 2011
    Publication date: September 26, 2013
    Applicant: Dalhousie University
    Inventors: Rylan J. Lundgren, Mark Stradiotto
  • Publication number: 20130244958
    Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2, R3 and R4 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
    Type: Application
    Filed: March 5, 2013
    Publication date: September 19, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Binh Thanh Vu, Chunlin Zhao, Daniel Fishlock
  • Publication number: 20130178445
    Abstract: Benzopyran compounds with strong anti-estrogenic activity and essentially no estrogenic activity are provided, which are OP-1038, which is 3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol, and OP-1074, which is (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol. OP-1074 is a pure anti-estrogen when tested in the agonist mode and a complete anti-estrogen when tested in the antagonist mode. These compounds are useful for the treatment or prevention of a variety of conditions that are modulated through the estrogen receptor in mammals including humans.
    Type: Application
    Filed: December 17, 2012
    Publication date: July 11, 2013
    Applicant: OLEMA PHARMACEUTICALS, INC.
    Inventor: OLEMA PHARMACEUTICALS, INC.
  • Publication number: 20130157982
    Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 11, 2013
    Publication date: June 20, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130157984
    Abstract: The invention provides in part, conjugate compounds. The invention also provides synthesis methods for making the compounds, and uses of the compounds.
    Type: Application
    Filed: November 28, 2012
    Publication date: June 20, 2013
    Inventor: Simon Fraser University
  • Publication number: 20130152314
    Abstract: The invention relates to a composition for dyeing keratin materials, and in particular human keratin fibres such as the hair, comprising at least one 2-pyrrolidone functionalized in the 4 position with an ester or amide radical, and at least one hydrophobic direct dye or a pigment; a dyeing process using this composition. Similarly, the invention relates to the use of the said pyrrolidone combined with a direct dye or a pigment for dyeing keratin materials, and especially to the use of the said pyrrolidone for improving the colour uptake onto the fibres of direct dyes that are sparingly soluble or insoluble in aqueous-alcoholic supports. The invention also relates to novel pyrrolidone derivatives. The present invention makes it possible in particular to obtain direct dyeing on keratin materials that is fast, resistant to washing, chromatic and powerful.
    Type: Application
    Filed: June 8, 2011
    Publication date: June 20, 2013
    Applicant: L'OREAL
    Inventors: Stéphane Sabelle, Madeleine Leduc, Christian Blaise
  • Patent number: 8461195
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: June 11, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Michael N. Greco, Harold R. Almond, Jr., Michael J. Hawkins, Eugene Powell
  • Patent number: 8445695
    Abstract: A method of making a phosphono-substituted dipyrromethane comprises reacting an aldehyde or acetal having at least one phosphono group substituted thereon with pyrrole to produce a phosphono-substituted dipyrromethane; and wherein the phosphono is selected from the group consisting of dialkyl phosphono, diaryl phosphono, and dialkylaryl phosphono. Additional methods, intermediates and products are also described.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: May 21, 2013
    Assignees: North Carolina State University, ZettaCore, Inc.
    Inventors: Jonathan S. Lindsey, Robert S. Loewe, Kannan Muthukumaran, Arounaguiry Ambroise
  • Patent number: 8404862
    Abstract: This invention relates composition and methods for making and using chemically modified oligonucleotides agents for inhibiting gene expression.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: March 26, 2013
    Assignee: Alnylam Pharmaceuticals, Inc.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Venkitasamy Kesavan
  • Publication number: 20130004518
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: Merck, Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
  • Publication number: 20130005938
    Abstract: A series of novel phosphorus-containing compounds having the following formula is provided: in which: R1-R4, A, Q and m are as defined in the specification. A process for the preparation of the compound of formula (I) is also provided. A polymer of formula (PA), and preparation process and use thereof are further provided. A polymer of formula (PI), and preparation process and use thereof are also provided.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 3, 2013
    Applicants: NATIONAL CHUNG HSING UNIVERSITY, CHANG CHUN PLASTICS CO., LTD.
    Inventors: Ching-Hsuan LIN, Tsung Li LIN, Yu-Ting FANG, Kuen-Yuan HWANG, An-Pang TU
  • Publication number: 20120322999
    Abstract: A method of making a phosphono-substituted dipyrromethane comprises reacting an aldehyde or acetal having at least one phosphono group substituted thereon with pyrrole to produce a phosphono-substituted dipyrromethane; and wherein the phosphono is selected from the group consisting of dialkyl phosphono, diaryl phosphono, and dialkylaryl phosphono. Additional methods, intermediates and products are also described.
    Type: Application
    Filed: August 29, 2012
    Publication date: December 20, 2012
    Inventors: Jonathan S. Lindsey, Robert S. Loewe, Kannan Muthukumaran, Arounaguiry Ambroise
  • Patent number: 8334300
    Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.
    Type: Grant
    Filed: March 24, 2011
    Date of Patent: December 18, 2012
    Assignee: Bayer Aktiengesellshaft
    Inventors: Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christophe Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
  • Patent number: 8278439
    Abstract: A method of making a phosphono-substituted dipyrromethane comprises reacting an aldehyde or acetal having at least one phosphono group substituted thereon with pyrrole to produce a phosphono-substituted dipyrromethane; and wherein the phosphono is selected from the group consisting of dialkyl phosphono, diaryl phosphono, and dialkylaryl phosphono. Additional methods, intermediates and products are also described.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: October 2, 2012
    Assignees: North Carolina State University, ZettaCore, Inc.
    Inventors: Jonathan S. Lindsey, Robert S. Loewe, Kannan Muthukumaran, Arounaguiry Ambroise
  • Publication number: 20120214988
    Abstract: Disclosed is a method for highly efficiently obtaining an optically active alcohol from a carbonyl compound highly enantioselectively. Also disclosed is a ligand used in such a method. Specifically, an optically active alcohol is obtained by reacting a carbonyl compound and an organozinc compound by using a ligand (L) shown below.
    Type: Application
    Filed: April 27, 2012
    Publication date: August 23, 2012
    Applicants: Sekisui Medical Co., Ltd., National University Corporation Nagoya University
    Inventors: Kazuaki ISHIHARA, Manabu Hatano, Takashi Miyamoto
  • Publication number: 20120208784
    Abstract: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
    Type: Application
    Filed: April 24, 2012
    Publication date: August 16, 2012
    Applicant: AVENTIS PHARMACEUTICALS INC.
    Inventors: Yong Mi CHOI-SLEDESKI, Julian LEVELL, Gregory Bernard POLI, Mark CZEKAJ, Alan John COLLIS, Roy VAZ
  • Publication number: 20120178940
    Abstract: This document relates to functionalized (e.g., mono- or bi-functional) polymers (e.g., polyethylene glycol and related polymers) as well as methods and materials for making and using such functionalized polymers.
    Type: Application
    Filed: December 13, 2011
    Publication date: July 12, 2012
    Inventor: Marek Kwiatkowski
  • Patent number: 8212039
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: July 3, 2012
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Michael N. Greco, Harold R. Almond, Jr., Michael J. Hawkins, Eugene Powell
  • Patent number: 8198445
    Abstract: Disclosed is a method for highly efficiently obtaining an optically active alcohol from a carbonyl compound highly enantioselectively. Also disclosed is a ligand used in such a method. Specifically, an optically active alcohol is obtained by reacting a carbonyl compound and an organozinc compound by using a ligand (L) shown below.
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: June 12, 2012
    Assignees: National University Corporation Nagoya University, Sekisui Medical Co., Ltd.
    Inventors: Kazuaki Ishihara, Manabu Hatano, Takashi Miyamoto
  • Publication number: 20120142939
    Abstract: The present invention relates to a process for the preparation of intermediates useful in the synthesis of [1[S(R)],2?,4?]-4-cyclohexyl-1-[[[2-methyl-1-oxypropoxy)propoxy](4-phenylbutyl phosphinyl]acetyl]L-proline, and the synthesis thereof, in particular as sodium salt (fosinopril sodium).
    Type: Application
    Filed: November 1, 2011
    Publication date: June 7, 2012
    Applicant: DIPHARMA FRANCIS S.r.l.
    Inventors: Pietro ALLEGRINI, Emanuele ATTOLINO, Alessandro DE MARCO, Fausto GORASSINI, Mario MICHIELETTI
  • Patent number: 8163911
    Abstract: The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: April 24, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Elke Langkopf, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
  • Publication number: 20120082621
    Abstract: Porphyrinic compounds that contain solubilizing groups are described, along with methods of making and using the same and compositions comprising such compounds. Examples of such compounds include compounds compounds of Formula I: wherein: Z is a porphyrinic macrocycle, Alk1 and Alk2 are each independently an alkylidene chain; L is a linking group or is absent; R1 is preferably an ionic group or polar group; R2 is an ionic group, polar group, bioconjugatable group, or targeting group; R3 is present or absent and when present is a halo group, bioconjugatable group, or targeting group, n is O or 1 (that is, the CH group is present, or Alk1 and Alk2 are bonded directly to a carbon of the porphyrinic macrocycle Z); or a salt thereof.
    Type: Application
    Filed: December 9, 2011
    Publication date: April 5, 2012
    Inventors: K. Eszter Borbas, Jonathan S. Lindsey
  • Publication number: 20120053347
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: August 31, 2010
    Publication date: March 1, 2012
    Inventors: Raymond W. Colburn, Scott L. Dax, Christopher Flores, Jay Matthews
  • Publication number: 20120035114
    Abstract: Compounds which inhibit the activity of signal transducer and activator of transcription 3 (STAT3) are provided together with methods of making and using the same. The compounds are designed to bind to the SH2 domain of STAT3, preventing STAT3 from binding to receptors for interleukin-6 family cytokines, growth factors such as the platelet-derived growth factor, the epidermal growth factor, vascular endothelial growth factor, and other signaling molecules such as leptin. Blocking these interactions prevents STAT3 from being phosphorylated on Tyr705, which is required for the dimerization of STAT3, translocation to the nucleus, binding to STAT3 response elements on promotors, and transcription of genes. In addition to these activities, binding to the SH2 domain of STAT3 breaks up pre-formed dimmers, thereby preventing the transcriptional activity of the inhibitor.
    Type: Application
    Filed: April 9, 2010
    Publication date: February 9, 2012
    Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: John S. McMurray, Pijus K. Mandal, Warren S. Liao, Fredika Robertson, Xiaomin Chen, Ramesh Rajaopal, Zhiyong Ren
  • Publication number: 20120022252
    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: July 15, 2011
    Publication date: January 26, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Publication number: 20110319363
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Application
    Filed: December 20, 2010
    Publication date: December 29, 2011
    Inventors: Michael N. Greco, Harold R. Almond, JR., Michael J. Hawkins, Eugene Powell
  • Publication number: 20110281822
    Abstract: Novel aromatic compounds which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: May 11, 2011
    Publication date: November 17, 2011
    Applicant: ALLERGAN, INC.
    Inventors: Janet A. Takeuchi, Ken Chow, Ling Li, Xiaoxia Liu
  • Publication number: 20110263870
    Abstract: The present invention relates to two novel pyrrole derivatives [3-Phenyl-4-(phenylcarbamoyl)-2-(4-fluorophenyl)-5-(1-methylethyl)-pyrrole-1-yl]methyl(diphenyl)phosphine oxide and Diethyl [3-Phenyl-4-(phenylcarbamoyl)-2-(4-fluorophenyl)-5-(1-methylethyl)-pyrrole-1-yl]methylphosphonate. These pyrrole derivatives can be used as intermediates for the synthesis of the anticholesterol drug atorvastatin.
    Type: Application
    Filed: April 21, 2011
    Publication date: October 27, 2011
    Applicant: HELVETICA INDUSTRIES (P) LIMITED
    Inventor: Braja SUNDAR PRADHAN