Ureido, Guanido, Or Hydrazine Patents (Class 562/439)
  • Patent number: 10059659
    Abstract: The present invention relates to compounds 1, 1a (S-enantiomer) and 1b (R-enantiomer) of the following formula 1, and a method for preparing the same. [formula 1] The novel compound of the formula 1 is used as an important intermediate for preparing compounds 6, 6a (S-enantiomer) and 6b (R-enantiomer) of the following formula 6, which are 2,2?-binaphthol-3-aldehyde derivatives. Also, the present invention provides a method for preparing the compound of formula 1 with a very safe method at low cost.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: August 28, 2018
    Assignee: AMINOLOGICS CO. LTD.
    Inventors: Rae Kyu Chang, Yun Soo Ahn, Heejung Jung, Hyerim Ga, Juwan Maeng, Young-Kook Koh, Young Hee Lee, Kwang Jae Lee, Joonseo Kim, Hyunil Lee, Heungsik Yoon
  • Patent number: 9845288
    Abstract: The present disclosure relates to a t-butylketone binaphthol derivative and a method of preparing the same, the t-butylketone binaphthol derivative being a high-efficiency chiral extracting agent which has a very high chiral selectivity enabling to extract an amino acid from an aqueous solution phase to an organic layer and to facilitate its hydrolysis, and enabling a continuous reuse of the organic layer.
    Type: Grant
    Filed: February 17, 2015
    Date of Patent: December 19, 2017
    Assignees: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION, AMINOLOGICS CO., LTD.
    Inventors: Kwan Mook Kim, Haofei Huang
  • Patent number: 9725391
    Abstract: The present invention relates to a method for preparing enantiomerically pure compounds 1a and 1b of the following formula 1 from racemic compound 1 of the following formula 1. [formula 1] The compounds 1a and 1b of the above formula 1 respectively are important intermediates for a process for preparing the respective compounds 2a and 2b of the following formula 2, which are 2,2?-binaphthol-3-aldehyde derivatives. The following compounds 2a and 2b are useful for preparing enantiomerically pure amino acids. The present invention provides a method for preparing the above compounds 1a and 1b very conveniently and economically, and suitably for mass production.
    Type: Grant
    Filed: November 24, 2011
    Date of Patent: August 8, 2017
    Assignee: Aminologics Co., Ltd.
    Inventors: Hyunil Lee, Heungsik Yoon, Young Hee Lee, Heejung Jung, Young-Kook Koh
  • Patent number: 9309193
    Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: April 12, 2016
    Assignee: Molecular Insight Pharmaceuticals, Inc.
    Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
  • Patent number: 9284266
    Abstract: Disclosed is a method of the synthesis of ramalin. It comprises reacting a glutamic acid derivative, which is prepared using alkylchloroformate, with a hydrazine salt compound, which is prepared from hydroxy aniline, whether protected or not. The synthesis method allows ramalin, excellent in antioxidant and anti-inflammatory activity, to be simply synthesized at stable yield even without use of a highly toxic solvent such as DMF. In addition, the method is cost competitive, and provides ramalin at high efficiency, thus enabling the mass production of ramalin.
    Type: Grant
    Filed: March 26, 2012
    Date of Patent: March 15, 2016
    Assignee: KOREA INSTITUTE OF OCEAN SCIENCE AND TECHNOLOGY
    Inventors: Joung Han Yim, Il Chan Kim, Dockyu Kim, Se Jong Han, Hyoung Seok Lee, Hari Datta Bhattarai, Tai Kyoung Kim, Keun Sik Kim
  • Patent number: 9115160
    Abstract: This invention discloses a solvent-free process for the preparation of cyclophosphamide. According to this invention, there is no solvent used during the reaction step for preparing cyclophosphamide, so that the total volume of the reaction for preparing cyclophosphamide can be reduced and the manufacture of cyclophosphamide can become more efficient. Furthermore, the above solvent-free process for the preparation of cyclophosphamide is more simply operated, more economic, and more environmental friendly than the preparation of cyclophosphamide in the prior art.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: August 25, 2015
    Assignee: SUNNY PHARMTECH INC.
    Inventors: Jien-Heh Tien, Pi-Shan Chiang
  • Patent number: 9040553
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: May 26, 2015
    Assignee: CELL VIABLE CORPORATION
    Inventors: Iraj Lalezari, Jill Fabricant
  • Patent number: 9029401
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: May 12, 2015
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Publication number: 20150119428
    Abstract: Mew tranilast complexes and new tranilast cocrystals are disclosed. These include all tranilast nicotinamide complex, a 1:1 tranilast nicotinamide cocrystal, a 1:1 tranilast saccharin complex, a 1:1 tranilast saccharin cocrystal, a 1:1 tranilast gentisic acid complex, a 1:1 tranilast gentisic acid cocrystal, a 1:1 tranilast salicylic acid complex, a 1:1 tranilast salicylic acid cocrystal, a 1:1 tranilast urea complex, a 1:1 tranilast urea cocrystal, a 1:1 tranilast 4-amtnoben2oic acid complex, a 1:1 tranilast 4-am!nobers2oic acid cocrystal, a 1:1 tranilast 2,4-di?hydroxybenzoic acid complex and a 1:1 tranilast 2,4-dihydroxybenzoic acid cocrystal. Also disclosed are pharmaceutical compositions containing a tranilast complex or cocrystal of the invention and a pharmaceutically acceptable carrier. Methods of treatment using the tranilast complexes and cocrystais as well as the pharmaceutical compositions are disclosed.
    Type: Application
    Filed: March 29, 2013
    Publication date: April 30, 2015
    Inventors: Joanne Holland, Christopher Frampton
  • Patent number: 8993780
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: March 31, 2015
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20150038523
    Abstract: The invention relates to compounds of formula (I): wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-integrin antagonists to target cells expressing alpha-V-beta-3.
    Type: Application
    Filed: January 22, 2013
    Publication date: February 5, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Robert Alan Goodnow, Jr., Matthew Michael Hamilton, Agnieszka Kowalczyk, Achyutharao Sidduri
  • Publication number: 20150038733
    Abstract: Disclosed is a method of the synthesis of ramalin. It comprises reacting a glutamic acid derivative, which is prepared using alkylchloroformate, with a hydrazine salt compound, which is prepared from hydroxy aniline, whether protected or not. The synthesis method allows ramalin, excellent in antioxidant and anti-inflammatory activity, to be simply synthesized at stable yield even without use of a highly toxic solvent such as DMF. In addition, the method is cost competitive, and provides ramalin at high efficiency, thus enabling the mass production of ramalin.
    Type: Application
    Filed: March 26, 2012
    Publication date: February 5, 2015
    Applicant: KOREA INSTITUTE OF OCEAN SCIENCE AND TECHNOLOGY
    Inventors: Joung Han Yim, Il Chan Kim, Dockyu Kim, Se Jong Han, Hyoung Seok Lee, Hari Datta Bhattarai, Tai Kyoung Kim, Keun Sik Kim
  • Publication number: 20150004126
    Abstract: The invention relates to the use of compounds that act on N-alpha acyl glutamine amino acylase enzyme expressed by coryneform bacteria to exert a malodour-counteracting effect, in a composition or article of manufacture suitable for reducing, suppressing or eliminating malodour on inanimate surfaces. The compounds, in particular, may be N-acyl glutamine derivatives.
    Type: Application
    Filed: January 27, 2012
    Publication date: January 1, 2015
    Applicant: GIVAUDAN S.A.
    Inventors: Thierry Audibert, Chinwe Bunting
  • Publication number: 20140369931
    Abstract: Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis.
    Type: Application
    Filed: March 14, 2014
    Publication date: December 18, 2014
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: MARTIN G. POMPER, RONNIE CHARLES MEASE, YING CHEN
  • Publication number: 20140364642
    Abstract: [Problem] Provision of a novel compound having read-through activity and a drug for the treatment of nonsense mutation-type disease containing this compound. [Solution] A compound represented by the following general formula (1): and a pharmaceutical composition containing this compound.
    Type: Application
    Filed: May 30, 2014
    Publication date: December 11, 2014
    Applicant: THE UNIVERSITY OF TOKYO
    Inventors: Yoshio HAYASHI, Akihiro TAGUCHI, Fumika YAKUSHIJI, Yuri YAMAZAKI, Ryoichi MATSUDA, Masataka SHIOZUKA
  • Patent number: 8905997
    Abstract: Disclosed herein are therapeutic compositions for treating and preventing diseases such as neointimal hyperplasia (NIH), where the compositions comprise a therapeutic particle that has a localized association with a blood vessel and a therapeutic agent, such as an anti-NIH agent. Methods of use of the therapeutic compositions are also disclosed.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: December 9, 2014
    Assignee: BIND Therapeutics, Inc.
    Inventors: Amy Grayson, Stephen E. Zale, David Dewitt
  • Publication number: 20140350045
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Application
    Filed: July 11, 2013
    Publication date: November 27, 2014
    Inventors: IRAJ LALEZARI, JILL FABRICANT
  • Patent number: 8895776
    Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: November 25, 2014
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J. M. Sadeque, Anna Shifrina, Young-Jun Shin, Pureza Vallar, Ning Zou
  • Publication number: 20140343138
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: February 14, 2014
    Publication date: November 20, 2014
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Adam D. Hughes, Erik Fenster, Melissa Fleury, Roland Gendron, Edmund J. Moran
  • Patent number: 8883271
    Abstract: The present invention is to provide a novel polymerizable chiral compound (chiral agent) having high left-handed helical twisting power, a polymerizable liquid crystal composition comprising the polymerizable chiral compound and a polymerizable liquid crystal compound, a liquid crystal polymer, and an optically anisotropic body.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: November 11, 2014
    Assignee: Zeon Corporation
    Inventors: Kei Sakamoto, Kentaro Tamura, Kumi Okuyama
  • Patent number: 8865934
    Abstract: The present invention relates to a method for synthesizing ramalin, and more particularly to a method for synthesizing ramalin, which comprises allowing 2-hydrazinylphenol to react with L-glutamic acid having a protected carboxyl group at C-1 and a protected amino group at C-2, and a method for preventing decomposition of the ramalin. According to the present invention, ramalin having excellent antioxidant and anti-inflammatory activities can be synthesized in high yield, and thus can be produced in large amounts. In addition, ramalin can be stably maintained for a long period of time, and thus can be easily used for industrial purposes.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: October 21, 2014
    Assignee: Korea Ocean Research and Development Institute
    Inventors: Joung Han Yim, Il Chan Kim, Sung Gu Lee, Dockyu Kim, Se Jong Han, Hyoung Seok Lee, Seung Jin Kim, Tai Kyoung Kim, Pil-Sung Kang, Heeyong Park, Ha Ju Park, Hye Yeon Koh, Mi Ra Park, Yu-Kyeong Park
  • Publication number: 20140303395
    Abstract: The present invention relates to the use of oligohydroxybenzoic acid derivatives in washing and cleaning agents in order to improve washing or cleaning performance with respect to bleachable stains.
    Type: Application
    Filed: June 18, 2014
    Publication date: October 9, 2014
    Inventors: Christian Kropf, Mareile Job, Christian Umbreit, Siglinde Erpenbach
  • Publication number: 20140275559
    Abstract: This document is related to the preparation of certain (substituted-phenyl)-triazolyl-(substituted phenyl) molecules, and intermediates related thereto, where said intermediates are useful in preparing certain insecticides.
    Type: Application
    Filed: February 27, 2014
    Publication date: September 18, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: James M. RENGA, Anne M. WILSON, Peter BORROMEO, Carl DeAMICIS, Jerod PATZNER
  • Publication number: 20140249180
    Abstract: A tau aggregation inhibitor reduces tau aggregation in cells. The tau aggregation inhibitor can include a catechol structure-containing compound or a salt thereof, and the catechol structure-containing compound can be one of isoprenaline, dopamine, dobutamine, levodopa, levodopa/carbidopa, trimetoquinol, hexoprenaline, methyldopa, and droxidopa. One example of the catechol structure-containing compound is isoprenaline, which can be d-enantiomer of isoprenaline or d/l-racemic mixture of isoprenaline. Tauopathies to be prevented or treated by the inhibitor include AD, Down's syndrome, Pick's disease, corticobasal degeneration, and progressive supranuclear palsy.
    Type: Application
    Filed: October 3, 2012
    Publication date: September 4, 2014
    Applicants: National Center for Geriatrics and Gerontology, THE DOSHISHA
    Inventors: Akihiko Takashima, Yoshiyuki Soeda, Hiroyuki Nagata, Yasuo Ihara, Tomohiro Miyasaka, Hachiro Sugimoto
  • Patent number: 8815917
    Abstract: Described herein is the DP2 antagonist [2?-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4?-trifluoromethyl-biphenyl-3-yl]-acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 antagonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: August 26, 2014
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: Jason Edward Brittain, Brian Andrew Stearns, Christopher David King, Kevin Ross Holme
  • Patent number: 8816076
    Abstract: The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: August 14, 2013
    Date of Patent: August 26, 2014
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 8809578
    Abstract: The present invention relates to a novel compound having excellent antioxidant activity, isolated from Ramalina terebrata, and more particularly to a novel compound, RAMALIN™, having excellent antioxidant activity, isolated from the Antarctic lichen Ramalina terebrata, a method for preparing the RAMALIN™, and a pharmaceutical composition, a functional food and a functional cosmetic composition, which contain the RAMALIN™ as an active ingredient. The RAMALIN™ according to the invention has significantly excellent antioxidant effects compared to commercially available antioxidants, and thus can be widely used in agents for treating oxidation-related diseases, anti-aging functional foods, functional cosmetic products for skin whitening and wrinkle reduction, etc.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: August 19, 2014
    Assignee: Korea Ocean Research and Development Institute
    Inventors: Joung Han Yim, Hong Kum Lee, Hari Datta Bhattarai, Paudel Babita, Il Chan Kim, Soon Gyu Hong, Doc Kyu Kim, Yoo Kyung Lee, Sung Gu Lee, Hyun Cheol Oh
  • Publication number: 20140178326
    Abstract: The invention relates to the use of compounds that act on N-alpha acyl glutamine amino acylase enzyme expressed by coryneform bacteria to exert a malodour-counteracting effect, in a composition or article of manufacture suitable for reducing, suppressing or eliminating malodour on inanimate surfaces. The compounds, in particular, may be N-acyl glutamine derivatives.
    Type: Application
    Filed: January 27, 2012
    Publication date: June 26, 2014
    Applicant: GIVAUDAN S.A.
    Inventors: Thierry Audibert, Chinwe Bunting
  • Publication number: 20140162996
    Abstract: One aspect of the disclosure relates to derivatives of aryl and heterocyclic ureido aryl and heterocyclic carboxamido isobutyric acids, dichlorophenyl urea, curcumin, and 1,3-diazetidine-2,4-dione, and pharmaceutical compositions thereof. The derivatives disclosed herein can modulate development of adipocytes and various cancer cells, including resistant cancer cells and cancer stem cells. Another aspect of the disclosure relates to the use of the derivatives and pharmaceutical compositions disclosed herein in treatment of obesity and various cancers.
    Type: Application
    Filed: July 29, 2013
    Publication date: June 12, 2014
    Applicant: CITY OF HOPE
    Inventors: Samuel RAHBAR, James L. FIGAROLA, Christopher LINCOLN, David HORNE, Rachael MOONEY, Monika POLEWSKI, George SOMLO, Lixin YANG
  • Publication number: 20140094614
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: December 10, 2013
    Publication date: April 3, 2014
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20140088156
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Application
    Filed: February 14, 2012
    Publication date: March 27, 2014
    Applicant: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Patent number: 8658803
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: February 25, 2014
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20140038910
    Abstract: Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods and intermediates useful for making the pharmaceutical agents and methods of using the pharmaceutical agents are also provided.
    Type: Application
    Filed: July 17, 2013
    Publication date: February 6, 2014
    Applicant: Saint Louis University
    Inventors: Peter RUMINSKI, David GRIGGS
  • Publication number: 20140012038
    Abstract: The present invention relates to compounds 1, 1a (S-enantiomer) and 1b (R-enantiomer) of the following formula 1, and a method for preparing the same. [formula 1] The novel compound of the formula 1 is used as an important intermediate for preparing compounds 6, 6a (S-enantiomer) and 6b (R-enantiomer) of the following formula 6, which are 2,2?-binaphthol-3-aldehyde derivatives. Also, the present invention provides a method for preparing the compound of formula 1 with a very safe method at low cost.
    Type: Application
    Filed: December 13, 2011
    Publication date: January 9, 2014
    Applicant: Aminologics Co., Ltd.
    Inventors: Rae Kyu Chang, Yun Soo Ahn, Heejung Jung, Hyerim Ga, Juwan Maeng, Young-Kook Koh, Young Hee Lee, Kwang Jae Lee, Joonseo Kim, Hyunil Lee
  • Patent number: 8617608
    Abstract: The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol. Other aspects of the invention include methods of making such nanoparticles.
    Type: Grant
    Filed: May 28, 2013
    Date of Patent: December 31, 2013
    Assignee: BIND Therapeutics, Inc.
    Inventors: Stephen E. Zale, Greg Troiano, Mir Mukkaram Ali, Jeff Hrkach, James Wright
  • Patent number: 8613954
    Abstract: The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol. Other aspects of the invention include methods of making such nanoparticles.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: December 24, 2013
    Assignee: BIND Therapeutics, Inc.
    Inventors: Stephen E. Zale, Greg Troiano, Mir Mukkaram Ali, Jeff Hrkach, James Wright
  • Publication number: 20130331570
    Abstract: The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: August 14, 2013
    Publication date: December 12, 2013
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 8603501
    Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: December 10, 2013
    Assignee: BIND Therapeutics, Inc.
    Inventors: Stephen E. Zale, Mir Mukkaram Ali
  • Patent number: 8603499
    Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: December 10, 2013
    Assignee: BIND Therapeutics, Inc.
    Inventors: Stephen E. Zale, Mir Mukkaram Ali
  • Patent number: 8603500
    Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: December 10, 2013
    Assignee: BIND Therapeutics, Inc.
    Inventors: Stephen E. Zale, Mir Mukkaram Ali
  • Patent number: 8563041
    Abstract: Disclosed herein are therapeutic compositions for treating and preventing diseases such as neointimal hyperplasia (NIH), where the compositions comprise a therapeutic particle that has a localized association with a blood vessel and a therapeutic agent, such as an anti-NIH agent. Methods of use of the therapeutic compositions are also disclosed.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: October 22, 2013
    Assignee: BIND Therapeutics, Inc.
    Inventors: Amy Grayson, Stephen E. Zale, David Dewitt
  • Patent number: 8541577
    Abstract: The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: November 5, 2012
    Date of Patent: September 24, 2013
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20130237580
    Abstract: The present invention relates to novel peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.
    Type: Application
    Filed: March 7, 2013
    Publication date: September 12, 2013
    Applicant: AURIGENE DISCOVERY TECHNOLOGIES LIMITED
    Inventors: POTTAYIL GOVINDAN NAIR SASIKUMAR, MURALIDHARA RAMACHANDRA, SEETHARAMAIAH SETTY SUDARSHAN NAREMADDEPALLI
  • Publication number: 20130237702
    Abstract: A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi.
    Type: Application
    Filed: August 31, 2012
    Publication date: September 12, 2013
    Applicant: AJINOMOTO CO., INC.
    Inventors: Masayuki SUGIKI, Toru OKAMATSU, Tetsuo YANO, Shinya TANIGUCHI
  • Publication number: 20130217706
    Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease; and other diseases.
    Type: Application
    Filed: September 13, 2012
    Publication date: August 22, 2013
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Yoúng-Jun Shin, Pureza Vallar, Ning Zou
  • Publication number: 20130211133
    Abstract: The present invention relates to a method for synthesizing ramalin, and more particularly to a method for synthesizing ramalin, which comprises allowing 2-hydrazinylphenol to react with L-glutamic acid having a protected carboxyl group at C-1 and a protected amino group at C-2, and a method for preventing decomposition of the ramalin. According to the present invention, ramalin having excellent antioxidant and anti-inflammatory activities can be synthesized in high yield, and thus can be produced in large amounts. In addition, ramalin can be stably maintained for a long period of time, and thus can be easily used for industrial purposes.
    Type: Application
    Filed: July 14, 2011
    Publication date: August 15, 2013
    Applicant: KOREA OCEAN RESEARCH AND DEVELOPMENT INSTITUTE
    Inventors: Joung Han Yim, Il Chan Kim, Sung Gu Lee, Dockyu Kim, Se Jong Han, Hyoung Seok Lee, Seung Jin Kim, Tai Kyoung Kim, Pil-Sung Kang, Heeyong Park, Ha Ju Park, Hye Yeon Koh, Mi Ra Park, Yu-Kyeong Park
  • Publication number: 20130190340
    Abstract: Certain aspects of the invention relate to compounds, compositions and methods that are useful for treating or preventing a disease in a subject by enhancing the degradation of a protein. In other aspects, said compounds can be useful research tools for investigating protein degradation. In other aspects, said compounds are useful research tools for investigating protein function. In certain embodiments, the degraded protein is implicated in a disease or disorder whose pathology is related at least in part to the excessive expression of the protein or the expression of a mutant form of the protein.
    Type: Application
    Filed: June 30, 2011
    Publication date: July 25, 2013
    Applicant: Brandeis University
    Inventors: Lizbeth K. Hedstrom, Marcus Long, Deviprasad R. Gollapalli
  • Patent number: 8487129
    Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: July 16, 2013
    Assignee: Molecular Insight Pharmaceuticals, Inc.
    Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
  • Publication number: 20130116324
    Abstract: The present invention relates to the novel use (anti-inflammatory activity) of Ramalin isolated from the Antarctic lichen Ramalina terebrata, and more specifically to a pharmaceutical composition containing Ramalin as an active ingredient. Ramalin of the invention is a compound derived from natural material, has no toxicity or side effects, and inhibits the expression of inducible nitric oxide synthase (iNOS) in the transcription stage to significantly inhibit the production of nitric oxide (NO) that is a key mediator of inflammatory responses. In addition, it inhibits the activation of the inflammatory mediator NF-?B, inhibits p38 MAPK, ERK1/2 and JNK signaling pathways, and inhibits the expression of the LPS receptor TLR4, suggesting that Ramalin has an excellent anti-inflammatory effect. Thus, the composition containing Ramalin can be effectively used to fundamentally treat or prevent inflammatory diseases or immune diseases and to relieve or alleviate the symptoms of the diseases.
    Type: Application
    Filed: June 2, 2011
    Publication date: May 9, 2013
    Applicant: KOREA OCEAN RESEARCH AND DEVELOPMENT INSTITUTE
    Inventors: Joung Han Yim, Il Chan Kim, Sung Gu Lee, Doc Kyu Kim, Se Jong Han, Hyoung Seok Lee, Sung Jin Kim, Tai Kyoung Kim, Pil-Sung Kang, Heeyong Park, Ha Ju Park, Suhkneung Pyo
  • Patent number: RE46496
    Abstract: The present invention relates to metformin glycinate salt and pharmaceutical compositions thereof for the treatment of diabetes mellitus. The method includes administration of the metformin glycinate salt by various routes selected from oral, intravenous injectable, intramuscular injectable, nasal, intraperitoneal, or sublingual, in order to achieve a reduction in blood glucose levels. The invention further relates to the synthesis of a new 1,1-dimethylbiguanide glycinate salt, called Metformin Glycinate. The resulting salt exhibits advantages over other metformin salts. These advantages are due, in the first place, to the fact that the glycine counterion exhibits hypoglycemic effects by itself. Moreover, the salt exhibits more rapid absorption, reaching higher plasma concentrations than those produced with metformin hydrochloride.
    Type: Grant
    Filed: April 21, 2016
    Date of Patent: August 1, 2017
    Assignee: Laboratorios Silanes S.A. de C.V.
    Inventor: Jose Manuel Francisco Ochoa Lara