The Nitrogen Is In Same Side Chain As Ester Function Patents (Class 560/38)
  • Publication number: 20150148559
    Abstract: The invention provides new processes for making and purifying amino acid compounds, which are useful in the preparation of AKT inhibitors used in the treatment of diseases such as cancer, including the compound (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 28, 2015
    Applicant: Genentech, Inc.
    Inventor: Travis Remarchuk
  • Publication number: 20150119589
    Abstract: This invention relates to methods for making oxetan-3-ylmethanamines having the formula (I) wherein R1? and R2? are as defined herein. The methods of the invention provide the compounds of formula (I) in high yields and under conditions amenable for large-scale commercial production.
    Type: Application
    Filed: May 1, 2013
    Publication date: April 30, 2015
    Inventors: Magnus Carl Arne Eriksson, Suresh R. Kapadia, Jonathan Timothy Reeves, Xingzhong Zeng
  • Publication number: 20150079163
    Abstract: The present disclosure provides antimicrobial compounds, compositions comprising such antimicrobial compounds, and methods of their use, in particular, antibacterial compounds and antifungal compounds. In certain aspects, the antimicrobial compounds are effective against pathogens of hospital-acquired infections. In certain aspects, the antimicrobial compounds are effective against pathogens that are resistant to antibiotics. The antimicrobial compounds can be used in antibacterial compositions, antifungal compositions, antiseptic compositions and disinfectant compositions. The antimicrobial compounds can be used as adjuncts in antibacterial compositions and antifungal compositions.
    Type: Application
    Filed: September 25, 2014
    Publication date: March 19, 2015
    Inventors: Bassam B. DAMAJ, Richard Martin
  • Publication number: 20150038705
    Abstract: Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, reduce biofilms, and/or inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.
    Type: Application
    Filed: October 6, 2014
    Publication date: February 5, 2015
    Inventors: DUSTIN WILLIAMS, RYAN LOOPER, SUJEEVINI JEYAPALINA, TRAVIS HAUSSENER, PAUL R. SEBAHAR, HARI KANNA REDDY
  • Publication number: 20150011628
    Abstract: The invention relates to substituted diphenylamine compounds using as antitumor agents. The structure of the compounds is represented as the general formula (I): The groups are as defined as specification. The compound represented by formula (I) showed potent antitumor activity, especially to cure or alleviate the cancer causing by cancer cells of human tissue or organ. The preferred cancers are: colon cancer, liver cancer, lymph cancer, lung cancer, esophageal cancer, breast cancer, central nervous system cancer, melanoma, ovarian cancer, cervical cancer, renal cancer, leukemia, prostatic cancer, pancreatic cancer, bladder cancer, rectal cancer, osteosarcoma, nasopharynx cancer or stomach cancer.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 8, 2015
    Inventors: Changling Liu, Baoshan Chai, Huichao Li, Aiying Guan
  • Publication number: 20140357713
    Abstract: The present disclosure provides antimicrobial compounds, compositions comprising such antimicrobial compounds, and methods of their use, in particular, antibacterial compounds and antifungal compounds. In certain aspects, the antimicrobial compounds are effective against pathogens of hospital-acquired infections. In certain aspects, the antimicrobial compounds are effective against pathogens that are resistant to antibiotics. The antimicrobial compounds can be used in antibacterial compositions, antifungal compositions, antiseptic compositions and disinfectant compositions. The antimicrobial compounds can be used as adjuncts in antibacterial compositions and antifungal compositions.
    Type: Application
    Filed: May 7, 2014
    Publication date: December 4, 2014
    Applicant: NexMed Holdings, Inc.
    Inventors: Bassam B. Damaj, Richard Martin
  • Patent number: 8900796
    Abstract: The present invention provides an acid generator generates a sulfonic acid represented by the following general formula (1) in response to high-energy beam or heat: To provide a novel acid generator which is suitably used as an acid generator for a resist composition, which solves the problems of LER and a depth of focus and can be effectively and widely used particularly without degradation of a resolution, a chemically amplified resist composition using the same, and a patterning process.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: December 2, 2014
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Masaki Ohashi, Tomohiro Kobayashi, Masayoshi Sagehashi
  • Patent number: 8900625
    Abstract: The present disclosure provides antimicrobial compounds, compositions comprising such antimicrobial compounds, and methods of their use, in particular, antibacterial compounds and antifungal compounds. In certain aspects, the antimicrobial compounds are effective against pathogens of hospital-acquired infections. In certain aspects, the antimicrobial compounds are effective against pathogens that are resistant to antibiotics. The antimicrobial compounds can be used in antibacterial compositions, antifungal compositions, antiseptic compositions and disinfectant compositions. The antimicrobial compounds can be used as adjuncts in antibacterial compositions and antifungal compositions.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: December 2, 2014
    Assignee: Nexmed Holdings, Inc.
    Inventors: Bassam B. Damaj, Richard M. Martin
  • Publication number: 20140288323
    Abstract: The present invention provides, inter alia, a cyclopropenimine Brønsted base catalyst and a cyclopropenimine scaffold for use as a Brønsted base catalyst. This cyclopropenimine has the structure (100). Methods for making such a cyclopropenimine are also provided. Further provided are processes for carrying out an organic synthetic reaction and processes for catalyzing a proton transfer reaction enantioselectively using such a cyclopropenimine Brønsted base catalyst.
    Type: Application
    Filed: October 15, 2012
    Publication date: September 25, 2014
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Tristan Hayes Lambert, Jeffrey Bandar
  • Publication number: 20140249320
    Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
    Type: Application
    Filed: March 25, 2014
    Publication date: September 4, 2014
    Inventors: David Hook, Thomas Ruch, Bernard Riss, Bernhard Wietfeld, Gottfried Sedelmeier, Matthias Napp, Markus Bänziger, Steven Hawker, Lech Ciszewski, Liladhar Murlidhar Waykole
  • 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
  • Publication number: 20140197365
    Abstract: An electrically conductive pulp suitable for use as a reinforcement comprises from 60 to 96 weight percent of fibers of aromatic polyamide, aromatic copolyamide or mixtures thereof and from 4 to 40 weight percent of conductive material coated onto the fibers wherein the conductive material comprises (i) a polymer of aniline, or (ii) a random copolymer formed from aniline and one or more substituted aniline co-monomers that exist in the protonated emeraldine salt form.
    Type: Application
    Filed: January 17, 2013
    Publication date: July 17, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Gary Delmar Jaycox, Jeffrey S. Downey
  • Publication number: 20140194508
    Abstract: The present invention provides novel cycloalkylmethylamine analogs, and methods of preparing cycloalkylmethylamine analogs. The present invention also provides methods of using cycloalkylmethylamine analogs and compositions of cycloalkylmethylamine analogs. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications.
    Type: Application
    Filed: March 10, 2014
    Publication date: July 10, 2014
    Applicant: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan BHAT, Seema Rani Bhat
  • Publication number: 20140194427
    Abstract: Provided is a compound of formula (I): or a pharmaceutically acceptable salt thereof. Also provided is a method of treating, prophylaxis, or amelioration of a disease, comprising administering to a subject in need of treatment for the disease an effective amount of a compound of formula (I) described herein. In one embodiment, the method is a neurodegenerative disease, such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, Huntington's disease, or Alzheimer's disease.
    Type: Application
    Filed: March 7, 2014
    Publication date: July 10, 2014
    Applicant: Biogen IDEC MA Inc.
    Inventor: Jianhua CHAO
  • Publication number: 20140187558
    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: May 25, 2012
    Publication date: July 3, 2014
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Zdenko Casar, Gaj Stavber
  • Publication number: 20140170207
    Abstract: The present disclosure provides antimicrobial compounds, compositions comprising such antimicrobial compounds, and methods of their use, in particular, antibacterial compounds and antifungal compounds. In certain aspects, the antimicrobial compounds are effective against pathogens of hospital-acquired infections. In certain aspects, the antimicrobial compounds are effective against pathogens that are resistant to antibiotics. The antimicrobial compounds can be used in antibacterial compositions, antifungal compositions, antiseptic compositions and disinfectant compositions. The antimicrobial compounds can be used as adjuncts in antibacterial compositions and antifungal compositions.
    Type: Application
    Filed: March 15, 2013
    Publication date: June 19, 2014
    Inventors: Bassam B. Damaj, Richard M. Martin
  • Publication number: 20140161830
    Abstract: Provided herein are lipidoids that may be prepared from the conjugate addition of alkylamines to acrylates. In some embodiments, provided lipidoids are biodegradable and may be used in a variety of drug delivery systems. Given the amino moiety of the lipidoids, they are well-suited for the delivery of polynucleotides, in addition to other agents. Nanoparticles containing the inventive lipidoids and polynucleotides have been prepared and have been shown to be effective in delivering siRNA.
    Type: Application
    Filed: November 25, 2013
    Publication date: June 12, 2014
    Applicant: Massachusetts Institute of Technology
    Inventors: Daniel Griffith Anderson, Kathryn Ann Whitehead, Joseph R. Dorkin, Arturo Jose Vegas, Yunlong Zhang
  • Publication number: 20140128616
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: January 10, 2014
    Publication date: May 8, 2014
    Applicant: SANOFI
    Inventors: Sven RUF, Josef PERNERSTORFER, Thorsten SADOWSKI, Georg HORSTICK, Herman SCHREUDER, Christian BUNING, Thomas OLPP, Bodo SCHEIPER, Klaus WIRTH
  • Patent number: 8664426
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: March 4, 2014
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Publication number: 20140031230
    Abstract: An object of the present invention is to provide an auxin biosynthesis inhibitor superior to L-AOPP. The object can be attained by a compound represented by general formula (I): wherein, R1 to R5 and X are the same as defined in the specification or a salt or solvate thereof.
    Type: Application
    Filed: February 28, 2012
    Publication date: January 30, 2014
    Inventors: Yukihisa Shimada, Ko Kikuzato, Megumi Narukawa, Tadao Asami, Kazuo Soeno
  • Patent number: 8637620
    Abstract: The invention relates to a process for preparing a polymeric material doped with metal elements, comprising a step of polymerization of at least one monomer comprising at least one ethylenic function, said monomer being complexed with a metal element. Use of the materials obtained by means of this process as catalysts, or luminescent or magnetic materials, or as elements for laser targets.
    Type: Grant
    Filed: October 7, 2008
    Date of Patent: January 28, 2014
    Assignee: Commissariat A l'Energie Atomique et aux Energies Alternatives
    Inventors: Alexia Balland Longeau, Louis Moreau, Jérôme Thibonnet, Emilie Velasquez
  • Publication number: 20140005292
    Abstract: A compound represented by the following general formula (1). In the formula, A represents a benzene ring, a naphthalene ring and the like, wherein these rings may be substituted with a halogen atom and the like, R1 represents a hydrogen atom and the like, R2 represents a C1-35 hydrocarbon group having or not having at least one group selected from an epoxy group, 4-vinylphenyl group and a (meth)acryloyloxy group, or a hydrogen atom, wherein at least one of R2 with n occurrences is a C3-35 hydrocarbon group having at least one group selected from an epoxy group, a 4-vinylphenyl group and a (meth)acryloyloxy group, n represents an integer of 1 to 6, and X represents a nitrogen atom, an oxygen atom, a sulfur atom, a phosphorus atom, or an n-valent organic group having 35 or less carbon atoms.
    Type: Application
    Filed: April 12, 2012
    Publication date: January 2, 2014
    Applicant: Adeka Corporation
    Inventors: Yosuke Maeda, Masaaki Shimizu, Koich Shigeno
  • Patent number: 8609721
    Abstract: The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.
    Type: Grant
    Filed: February 11, 2008
    Date of Patent: December 17, 2013
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Jarda T. Wroblewski, Fajun Nan
  • Patent number: 8598347
    Abstract: The present invention relates to an improved method for manufacturing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention allows reduction of production costs by reacting low cost reagents, improves yield and is adaptable for mass production.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: December 3, 2013
    Assignee: Dong-A Pharmaceutical. Co., Ltd
    Inventors: Woo Young Kwak, Heung Jae Kim, Jong Pil Min, Tae Hyun Yoon, Hyun Joo Shim, Moohi Yoo
  • Publication number: 20130289223
    Abstract: A pharmaceutically-active polymeric compound of the general formula (I), Y-[Yn-LINK B-X]m-LINK B??(I) wherein (i) X is a coupled biological coupling agent of the general formula (II) Bio-LINK A-Bio??(II) wherein Bio is a biologically active agent fragment or precursor thereof linked to LINK A through a hydrolysable covalent bond; and LINK A is a coupled central flexible linear first segment of <2000 theoretical molecular weight linked to each of said Bio fragments; (ii) Y is LINK B-OLIGO; wherein (a) LINK B is a coupled second segment linking one OLIGO to another OLIGO and an OLIGO to X or precursor thereof; and (b) OLIGO is a short length of polymer segment having a molecular weight of less than 5,000 and comprising less than 100 monomeric repeating units; (iii) m is 1-40; and (iv) n is selected from 2-50. The compounds are useful as biomaterials, particularly, providing antibacterial activity in vivo.
    Type: Application
    Filed: December 17, 2012
    Publication date: October 31, 2013
    Inventors: J. Paul SANTERRE, Mei LI
  • Patent number: 8519175
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: October 8, 2012
    Date of Patent: August 27, 2013
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Patent number: 8519156
    Abstract: The present invention relates to compound of formula I, which are functionalized, non-phenolic amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: December 30, 2012
    Date of Patent: August 27, 2013
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Patent number: 8507715
    Abstract: An optically active ?-aminocarbonyl compound is obtained by a Mannich reaction between an aldimine in which: nitrogen is protected and a malonic acid diester, in the presence of optically active BINOL and dialkyl magnesium (in which two alkyl groups are the same or different) in an amount 1 to 2 molar times the amount of the BINOL.
    Type: Grant
    Filed: June 22, 2011
    Date of Patent: August 13, 2013
    Assignee: National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Manabu Hatano, Takahiro Horibe
  • Publication number: 20130204033
    Abstract: Antiproliferative compounds having a structure represented by formula (II), where n, R1, R2, R3, R4, and R5 are as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody:
    Type: Application
    Filed: January 29, 2013
    Publication date: August 8, 2013
    Applicant: Medarex, Inc.
    Inventor: Medarex, Inc.
  • Publication number: 20130178624
    Abstract: The present invention concerns the compounds of formula wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl, —O—N?CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-4
    Type: Application
    Filed: January 18, 2013
    Publication date: July 11, 2013
    Applicant: Janssen Pharmaceutica N.V.
    Inventor: Janssen Pharmaceutica N.V.
  • Publication number: 20130116446
    Abstract: The present invention relates to compound of formula I, which are functionalized, non-phenolic amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Application
    Filed: December 30, 2012
    Publication date: May 9, 2013
    Applicant: BEZWADA BIOMEDICAL, LLC
    Inventor: Bezwada Biomedical, LLC
  • Publication number: 20130079543
    Abstract: An optically active ?-aminocarbonyl compound is obtained by a Mannich reaction between an aldimine in which: nitrogen is protected and a malonic acid diester, in the presence of optically active BINOL and dialkyl magnesium (in which two alkyl groups are the same or different) in an amount 1 to 2 molar times the amount of the BINOL.
    Type: Application
    Filed: June 22, 2011
    Publication date: March 28, 2013
    Applicant: NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITY
    Inventors: Kazuaki Ishihara, Manabu Hatano, Takahiro Horibe
  • Patent number: 8399662
    Abstract: The present invention relates to novel O-acyloxime derivatives, a preparation method thereof and a pharmaceutical composition comprising the same for prevention and treatment of cardiovascular disease. The O-acyloxime derivatives according to the present invention may valuably be used for prevention and treatment of cardiovascular diseases such as hyperlipidemia, coronary arterial heart disease, atherosclerosis, and myocardial infarction caused by Lp-PLA2, because they have excellent inhibitory effect of Lp-PLA2.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: March 19, 2013
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Tae-Sook Jeong, Woo-Song Lee, Hyung-Jae Jeong, Yong-Dae Park, Jong-Min Han, Hyoung-Chin Kim, Og-Sung Moon, Young-Suk Won
  • Publication number: 20130046004
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: January 26, 2011
    Publication date: February 21, 2013
    Applicant: SANOFI
    Inventors: Sven Ruf, Josef Pernerstorfer, Thorsten Sadowski, Georg Horstick, Herman Schreuder, Christian Buning, Thomas Olpp, Bodo Scheiper, Klaus Wirth
  • Patent number: 8377986
    Abstract: The compound 3,3-dimethyl-butyric acid 4-((S)-2-amino-2-methoxycarbonyl-ethyl)-2-(3,3-dimethyl-butyryloxy)-phenyl ester of formula (I) has dopaminergic properties.
    Type: Grant
    Filed: August 4, 2008
    Date of Patent: February 19, 2013
    Assignee: Proximagen Ltd.
    Inventor: Christopher Hobbs
  • Publication number: 20130035487
    Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
    Type: Application
    Filed: September 5, 2012
    Publication date: February 7, 2013
    Applicant: Intrexon Corporation
    Inventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
  • Patent number: 8338632
    Abstract: The present invention provides novel cycloalkylmethylamine analogs, and methods of preparing cycloalkylmethylamine analogs. The present invention also provides methods of using cycloalkylmethylamine analogs and compositions of cycloalkylmethylamine analogs. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: December 25, 2012
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Seema Rani Bhat
  • Patent number: 8309754
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: December 24, 2011
    Date of Patent: November 13, 2012
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Patent number: 8293948
    Abstract: A reagent for organic synthesis with which a chemical reaction can be conducted in a liquid phase and unnecessary compound(s) can be easily separated at low cost from the liquid phase after completion of the reaction. The reagent for organic synthesis reversibly changes from a liquid-phase state to a solid-phase state with changes in solution composition and/or solution temperature, and is for use in organic synthesis reactions. This reagent for organic syntheses facilitates process development. With the reagent, research on and development of, e.g., medicines through, e.g., compound library synthesis, etc. can be accelerated. It can hence contribute to technical innovations in the biochemical industry and chemical industry.
    Type: Grant
    Filed: January 9, 2012
    Date of Patent: October 23, 2012
    Assignee: Jitsubo Co., Ltd.
    Inventors: Kazuhiro Chiba, Shokaku Kim, Yusuke Kono
  • Patent number: 8288566
    Abstract: Provided is an enantioselective, palladium-catalyzed method for the preparation of ?-amino-?,?-unsaturated carboxylic acid derivatives having the formulas II, III, VII and VIII:
    Type: Grant
    Filed: November 16, 2009
    Date of Patent: October 16, 2012
    Assignee: Novartis AG
    Inventors: Murat Acemoglu, Andreas Pfaltz, Claude Schaerer
  • Patent number: 8263798
    Abstract: The present invention discloses an optically active quarternary ammonium salt having axial asymmetry and a method for producing an ?-amino acid and a derivative thereof using the same. The optically active quarternary ammonium salt having axial asymmetry of the present invention is a chiral phase-transfer catalyst that has a simple structure and that can be produced in a smaller number of process steps. The compound of the present invention is very useful as a phase-transfer catalyst in the synthesis of an ?-alkyl-?-amino acid and a derivative thereof as well as an ?,?-dialkyl-?-amino acid and a derivative thereof. Therefore, the compound of the present invention can be used in the development of novel foods and pharmaceuticals.
    Type: Grant
    Filed: December 28, 2011
    Date of Patent: September 11, 2012
    Assignee: Nagase & Co., Ltd.
    Inventors: Keiji Maruoka, Kenichiro Yamamoto, Yukifumi Nishimoto
  • Publication number: 20120210634
    Abstract: The present invention relates to the novel compounds of the formula (I), as well as to their manufacture and use and compositions comprising them. The invention also relates to a change in oxidation reactions of hydrocarbons admixed to these compounds. Furthermore the invention relates to (bio)diesel fuel comprising such compounds.
    Type: Application
    Filed: September 14, 2010
    Publication date: August 23, 2012
    Inventors: Max Hugentobler, Steffen Ruf, Bettina Wuestenberg
  • Patent number: 8247603
    Abstract: The present invention concerns deuterated catecholamine derivatives as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated catecholamine derivatives as well as physiologically acceptable salts thereof, and also pharmaceutical compositions, which contain these compounds, also in combination with enzyme inhibitors, for the treatment of dopamine deficiency diseases or diseases which are based on disrupted tyrosine transport or disrupted tyrosine decarboxylase, as well as other disorders.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: August 21, 2012
    Assignee: Birds Pharma GmbH Berolina Innovative
    Inventors: Rudolf-Giesbert Alken, Frank Schneider
  • Publication number: 20120172601
    Abstract: Disclosed is a novel zinc cluster compound represented by general formula (1): Zn4O (OCOR)6 (RCOOH)n, wherein R represents an alkyl group which has 1 to 4 carbon atoms and may be substituted with a halogen atom, and n represents 0.1 to 1, and also disclosed are a method for producing the compound and a reaction using the compound.
    Type: Application
    Filed: May 31, 2010
    Publication date: July 5, 2012
    Applicant: TAKASAGO INTERNATIONAL CORPORATION
    Inventors: Yoshimasa Matsushima, Hideki Nara, Takahiro Fujiwara
  • Publication number: 20120172392
    Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.
    Type: Application
    Filed: March 7, 2012
    Publication date: July 5, 2012
    Inventors: LUISA M. SALTER-CID, ERIC Y. WANG, MARY T. MACDONALD, JINGJING ZHAO
  • Publication number: 20120142916
    Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
    Type: Application
    Filed: December 21, 2011
    Publication date: June 7, 2012
    Inventors: David Hook, Thomas Ruch, Bernhard Riss, Bernhard Wietfeld, Gottfried Sedelmeier, Matthias Napp, Markus Bänziger, Steven Hawker, Lech Ciszewski, Liladhar Murtidhar Waykole
  • Publication number: 20120123144
    Abstract: The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as oral anti-diabetic drug. Starting from L-aspartic acid derivate of formula IV the invention describes preparation of the chiral (R)-?-amino acid of formula II known as a precursor in the synthesis of Sitagliptin (formula I).
    Type: Application
    Filed: May 18, 2011
    Publication date: May 17, 2012
    Applicant: Drug Process Licensing Associates, LLC
    Inventor: Milan Soukup
  • Patent number: 8168820
    Abstract: The present invention concerns deuterated catecholamine derivatives as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated catecholamine derivatives as well as physiologically compatible salts thereof, and also pharmaceutical compositions, which contain these compounds, also in combination with enzyme inhibitors, for the treatment of dopamine deficiency diseases or diseases which are based on disrupted tyrosine transport or disrupted tyrosine decarboxylase, as well as other disorders.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: May 1, 2012
    Assignee: BDD Berolina Drug Development GmbH
    Inventor: Rudolf-Giesbert Alken
  • Publication number: 20120101184
    Abstract: Presently described are curable compositions comprising a mixture of at least one (e.g. free-radically) polymerizable ionic liquid and at least one other ethylenically unsaturated monomer, oligomer, or polymer. The polymerizable ionic liquid is characterized as having an air to nitrogen curing exotherm ratio of at least 0.70. Also described are articles and methods of making articles from such curable compositions. A monofunctional polymerizable ionic liquid is also described comprising a non-polymerizable substituted imidazolium cationic group and a polymerizable sulfonate anion.
    Type: Application
    Filed: August 26, 2010
    Publication date: April 26, 2012
    Inventors: Yizhong Wang, Joel D. Oxman, Larry R. Krepski, Peiwang Zhu, Kevin M. Lewandowski, Brian N. Holmes, Richard L. Severance, Joseph D. Rule, Thomas P. Klun
  • Patent number: RE43632
    Abstract: The invention relates to compounds of formula: wherein R1 is selected from the group consisting of fatty acid acyl groups of 12 to 30 carbon atoms and fatty alcohol groups of 12 to 30 carbon atoms, and wherein R2 is selected from the group consisting of H, fatty acid acyl of 12 to 30 carbon atoms and fatty alcohol groups of 12 to 30 carbon atoms, the same as or different from R1, and the residue of a nutrient, drug, or other bioactive compound, and to the use of these compounds to deliver drugs and other bioactive compounds.
    Type: Grant
    Filed: May 1, 1996
    Date of Patent: September 4, 2012
    Assignee: Scarista, Ltd.
    Inventors: David B. Horrobin, Sherri Clarkson, legal representative, Mehar Manku, Philip Knowles, Peter Redden, Andrea Pitt, Paul Bradley, Paul Wakefield, Austin McMordie