Two Or More Hetero Atoms In The Five-membered Ring Patents (Class 514/92)
  • Patent number: 9034852
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: May 19, 2015
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Michael Gaul, Lily Lee Searle, Dionisios Rentzeperis
  • Publication number: 20150126475
    Abstract: To provide a pesticidal composition having a broad pesticidal spectrum, having high activity and having a long lasting effect. A pesticidal composition comprising as active ingredients at least one organic phosphorus compound (A) selected from the group consisting of fosthiazate and imicyafos and at least one compound (B) selected from the group consisting of clothianidin, dinotefuran, thiamethoxam, tefluthrin, silafluofen, chlorfluazuron, flufenoxuron and teflubenzuron (excluding a combination of fosthiazate and tefluthrin).
    Type: Application
    Filed: July 2, 2013
    Publication date: May 7, 2015
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventor: Hideshi Yoshimura
  • Publication number: 20150119365
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Application
    Filed: December 29, 2014
    Publication date: April 30, 2015
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Publication number: 20150111853
    Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step.
    Type: Application
    Filed: October 22, 2014
    Publication date: April 23, 2015
    Inventors: Jan-Ji Lai, Pradip M. Pathare, Laxma Kolla, Adrien F. Soret
  • Patent number: 8969578
    Abstract: Disclosed herein are compounds derived from a chemical structure according to the formula (I) wherein X comprises oxygen or sulfur, R1 comprises a phenyl or naphthyl group, R2 comprises an amide group and R3 comprises a phosphate group. The disclosed compounds demonstrate inhibitory activity against STAT3, a protein found in certain tumor tissues and which promotes cellular overproliferation and resistance to apoptosis. The invention includes compositions containing the disclosed compounds, as well as methods of treatment therewith.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: March 3, 2015
    Assignee: University of Central Florida Research Foundation, Inc.
    Inventors: James Turkson, Andrew D. Hamilton
  • Patent number: 8957051
    Abstract: The present invention relates to bicyclic aryl 1,2,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: September 30, 2013
    Date of Patent: February 17, 2015
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Patent number: 8940927
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinase activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: January 27, 2015
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Patent number: 8940718
    Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: January 27, 2015
    Assignee: Gilead Pharmasset LLC
    Inventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James Taylor, Chinh Viet Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
  • Publication number: 20150005261
    Abstract: The invention provides methods for treating fibrosis, as well as methods for modulating mitochondrial peroxide production in a cell, and methods for modulating the import of Rac1 into the mitochondria of a cell.
    Type: Application
    Filed: April 25, 2014
    Publication date: January 1, 2015
    Applicant: University of Iowa Research Foundation
    Inventors: Raymond J. Hohl, A. Brent Carter
  • Patent number: 8921341
    Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: December 30, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James Taylor, Chinh Viet Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
  • Publication number: 20140343017
    Abstract: Provided is a highly safe and effective compound represented by the following general formula (1) or a salt thereof which acts on tubulin and has an anticancer effect, wherein Ar represents an aryl group or a heteroaryl group; Z1, Z2, Z3, and Z4 each independently represent CH, a nitrogen atom, an oxygen atom, or a sulfur atom; R1 represents a hydrogen atom, a halogen atom, an alkyl group, or the like; R2 and R3 are the same or different and each represent a hydrogen atom, a halogen atom, a carboxyl group, or the like; n units of R4 are the same or different and each represent a hydrogen atom, an alkyl group, or the like; and n represents a number of 0 to 4.
    Type: Application
    Filed: January 24, 2013
    Publication date: November 20, 2014
    Applicant: Kabushiki Kaisha Yakult Honsha
    Inventors: Takashi Ikeda, Masahiro Ono, Satoshi Ueno, Ryuta Yamazaki, Takashi Yaegashi, Takeshi Matsuzaki
  • Publication number: 20140314882
    Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 23, 2014
    Inventors: Frederick P. ROTH, Murat COKOL, Hon Nian CHUA
  • Publication number: 20140296183
    Abstract: A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(?O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH?CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Masatoshi KIUCHI, Kaoru MARUKAWA, Nobutaka KOBAYASHI
  • Publication number: 20140274963
    Abstract: The present invention relates to substituted aryl 1,2,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: March 18, 2014
    Publication date: September 18, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, Ken Chow
  • Patent number: 8828973
    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: Grant
    Filed: March 18, 2014
    Date of Patent: September 9, 2014
    Assignee: Allergan, Inc.
    Inventors: Phong X. Nguyen, Todd M. Heidelbaugh, John R. Cappiello
  • Publication number: 20140243292
    Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 11, 2014
    Publication date: August 28, 2014
    Applicant: Sanofi
    Inventors: Werngard CZECHTIZKY, John WESTON, Nils RACKELMANN, Michael PODESCHWA, Petra ARNDT, Klaus WIRTH, Heinz GOEGELEIN, Olaf RITZELER, Volker KRAFT, Patrice BELLEVERGUE, Gary McCORT
  • Publication number: 20140235589
    Abstract: The present invention relates to a mixed agrochemical emulsion composition comprising: an organic phosphorous pesticide represented by formula (I) (wherein, R1 represents a C1-4 linear or branched alkyl group; R2 represents a C1-4 linear or branched alkyl group; R3 represents a nitrogenated heterocyclic group which may have a substituent or a group —OR4 (wherein R4 represents a nitrogenated heterocyclic group which may have a substituent; and X and Y each independently represent an oxygen atom or a sulfur atom, wherein Y is a sulfur atom when X is an oxygen atom, and Y is an oxygen atom when X is a sulfur atom); chloropicrin; and a nonionic surfactant. The composition has excellent storage stability and excellent emulsifying properties in water and can be sprayed and applied conveniently by diluting the composition with water, in spite of a fact that both chloropicrin and the organic phosphorous pesticide, which are effective for the control of pests, are contained.
    Type: Application
    Filed: October 3, 2012
    Publication date: August 21, 2014
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Mikio Sekiguchi, Takao Awazu
  • Publication number: 20140235586
    Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: PTC Therapeutics, Inc.
    Inventors: Jeffrey A. Campbell, Atiyya Kahn, James Takasugi, Ellen Welch
  • Publication number: 20140235585
    Abstract: The present invention relates to substituted diaryl 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 19, 2014
    Publication date: August 21, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, KEN CHOW
  • Publication number: 20140221317
    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: March 18, 2014
    Publication date: August 7, 2014
    Applicant: Allergan, Inc.
    Inventors: PHONG X. NGUYEN, TODD M. HEIDELBAUGH, John R. Cappiello
  • Publication number: 20140206651
    Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.
    Type: Application
    Filed: March 24, 2014
    Publication date: July 24, 2014
    Applicant: Pfizer Inc.
    Inventors: Matthew Frank Brown, Charles Francis Donovan, Edmund Lee Ellsworth, Denton Wade Hoyer, Timothy Allan Johnson, Manjinder Singh Lall, Chris Limberakis, Sean Timothy Murphy, Debra Ann Sherry, Clarke Bentley Taylor, Joseph Scott Warmus
  • Publication number: 20140194390
    Abstract: A method of controlling pest with a pesticidal composition comprising synergistically effective amounts of at least one anthranilamide compound represented by the formula (I) or its salt and other pesticide: wherein each of R1a and R1b which are independent of each other, is halogen; each of R2 and R3 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or cyano; A is alkyl substituted by Y; Y is C3-4 cycloalkyl which may be substituted by at least one substituent selected from the group consisting of halogen, alkyl and haloalkyl; n is 0 or 1; and q is an integer of from 0 to 4; provided that R1a and R1b are not simultaneously chlorine nor bromine.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 10, 2014
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Toru KOYANAGI, Masayuki Morita, Tetsuo Yoneda, Tsuyoshi Ueda, Kazuhisa Kiriyama, Taku Hamamoto
  • Patent number: 8765722
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: June 26, 2013
    Date of Patent: July 1, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
  • Patent number: 8754009
    Abstract: The present invention relates to novel active compound combinations comprising, firstly, a known herbicide selected from the group consisting of glyphosate, glufosinate and glufosinate-ammonium and, secondly, at least one known fungicidally active compound, which combination is highly suitable for controlling unwanted phytopathogenic fungi, in particular soya bean rust. Particular preference is given to using these mixtures on transgenic plants resistant to the herbicides mentioned.
    Type: Grant
    Filed: May 27, 2006
    Date of Patent: June 17, 2014
    Assignee: Bayer CropScience AG
    Inventors: Klaus Stenzel, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Isolde Häuser-Hahn, Marie-Claire Grosjean, Bernard Marc Leroux, Haruko Sawada, Hiroyuki Hadano, Jean-Marie Gouot, Christian Scherb
  • Publication number: 20140162874
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Application
    Filed: February 12, 2014
    Publication date: June 12, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Maurice C. Yap, Ann M. Buysse, Daniel Knueppel, Yu Zhang, Negar Garizi, Noormohamed M. Niyaz, Christian T. Lowe, Ricky Hunter, Tony K. Trullinger, David A. Demeter, Dan Pernich, Carl DeAmicis, Ronald Ross, JR., Timothy C. Johnson
  • Patent number: 8741875
    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: Grant
    Filed: February 11, 2013
    Date of Patent: June 3, 2014
    Assignee: Allergan, Inc.
    Inventors: Todd M. Heidelbaugh, Phong X. Nguyen, John Cappiello
  • Publication number: 20140135291
    Abstract: The present invention relates to novel 2-thio-1,3,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 7, 2013
    Publication date: May 15, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Publication number: 20140128348
    Abstract: The present invention relates to substituted 1,3,4-oxadiazoles-2-thio derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 4, 2013
    Publication date: May 8, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Patent number: 8710031
    Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.
    Type: Grant
    Filed: March 7, 2011
    Date of Patent: April 29, 2014
    Assignee: PTC Therapeutics, Inc.
    Inventors: Jeffrey A. Campbell, Atiyya Kahn, James Takasugi, Ellen Welch
  • Patent number: 8703745
    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: Grant
    Filed: February 21, 2013
    Date of Patent: April 22, 2014
    Assignee: Allergan, Inc.
    Inventors: Todd M. Heidelbaugh, Phong X. Nguyen
  • Publication number: 20140107075
    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 21, 2013
    Publication date: April 17, 2014
    Applicant: ALLERGAN, INC.
    Inventors: TODD M. HEIDELBAUGH, PHONG X. NGUYEN
  • Publication number: 20140100197
    Abstract: The present invention relates to bicyclic aryl 1,2,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: September 30, 2013
    Publication date: April 10, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Publication number: 20140100199
    Abstract: The present invention relates to substituted aryl 1,2,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: September 30, 2013
    Publication date: April 10, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Patent number: 8664204
    Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: March 4, 2014
    Assignee: Threshold Pharmaceuticals, Inc.
    Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao
  • Publication number: 20140057874
    Abstract: Dosage forms or pharmaceutical compositions comprise a compound having the structure of Formula IV: wherein n is a non-negative integer; wherein each Z is an oxazolidinone-containing moiety having antibiotic activity in vivo upon cleaving, wherein M is independently OR1 or NR1R2; wherein R1 and R2 are independently selected from the group consisting of H, an optionally-substituted hydrocarbyl residue or a pharmaceutically acceptable cation; wherein the compound in the dosage form or a pharmaceutical composition is present in an amount effective for treating or preventing an antibacterial infection in a mammalian subject. Methods of preparing and using these dosage forms or pharmaceutical compositions are also disclosed.
    Type: Application
    Filed: October 31, 2013
    Publication date: February 27, 2014
    Applicant: TRIUS THERAPEUTICS, INC.
    Inventors: David Keith Hester, II, Robert J. Duguid, John Finn
  • Publication number: 20140045795
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
    Type: Application
    Filed: October 15, 2013
    Publication date: February 13, 2014
    Applicant: SYNTA PHARMACEUTICALS CORPORATION
    Inventors: Lijun Sun, Christopher Borella, Hao Li, Jun Jiang, Shoujun Chen, Keizo Koya, Takayo Inoue, Zhenjian Du, Kevin Foley, Yaming Wu, Mei Zhang, Weiwen Ying
  • Patent number: 8642278
    Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.
    Type: Grant
    Filed: November 22, 2006
    Date of Patent: February 4, 2014
    Assignee: University of South Florida
    Inventors: Said M. Sebti, Srikumar Chellappan, Nicholas James Lawrence
  • Publication number: 20130338111
    Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.
    Type: Application
    Filed: August 16, 2013
    Publication date: December 19, 2013
    Applicants: Icagen, Inc., Pfizer Limited
    Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
  • Patent number: 8609639
    Abstract: A small-molecule Stat3 dimerization inhibitor, S3I-M2001, is described and the dynamics of intracellular processing of activated Stat3 within the context of the biochemical and biological effects of the Stat3 chemical probe inhibitor are elucidated. S3I-M2001 is a newly-identified oxazole-based peptidomimetic of the Stat3 Src Homology (SH) 2 domain-binding phosphotyrosine peptide that selectively disrupts active Stat3:Stat3 dimers. Stat3-dependent malignant transformation, survival, and migration and invasion of mouse and human cancer cells harboring persistently-activated Stat3 were inhibited by S3I-M2001. S3I-M2001 inhibited Stat3-dependent transcriptional regulation of tumor survival genes, such as Bcl-xL. The disclosed compound is useful as a new potential treatment for certain cancers.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: December 17, 2013
    Assignees: University of South Florida, Yale University, University of Central Florida Research Foundation, Inc.
    Inventors: James Turkson, Said Sebti, Richard Jove, Andrew D. Hamilton
  • Publication number: 20130330365
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Adam D. Hughes, Melissa Fleury
  • Patent number: 8603437
    Abstract: The present invention discloses a method for the enzyme-mediated, site-specific, in-vivo precipitation of a water soluble molecule in an animal. The enzyme is either unique to tumor cells, or is produced within a specific site (e.g., tumor) at concentrations that are higher than that in normal tissues. Alternatively, the enzyme is conjugated to a targeting moiety such as an antibody or a receptor-binding molecule.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: December 10, 2013
    Assignee: President and Fellows of Harvard College
    Inventors: Amin I. Kassis, Ravi S. Harapanhalli
  • Publication number: 20130302280
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: June 26, 2013
    Publication date: November 14, 2013
    Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
  • Patent number: 8575135
    Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: November 5, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James Taylor, Chinh Viet Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
  • Publication number: 20130224170
    Abstract: A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of lipid soluble, hydrophobic active compounds having a chemical structure: wherein R1 is an aromatic backbone and R2 is a sulfur containing ligand. Through formation of disulfide linkages other moieties can be attached to R2 converting the hydrophobic base into a water soluble entity, for ease of delivery, which can be reconverted back to the original compound by biochemical reduction in the blood stream.
    Type: Application
    Filed: March 26, 2013
    Publication date: August 29, 2013
    Applicant: The University of Kentucky Research Foundation
    Inventor: The University of Kentucky Research Foundation
  • Publication number: 20130225531
    Abstract: A composition and method of treating Alzheimer's disease or a dementia of vascular origin are disclosed. The composition and method utilize an endothelin antagonist as the active agent to treat Alzheimer's disease or a dementia of vascular origin in mammals, including humans.
    Type: Application
    Filed: December 19, 2012
    Publication date: August 29, 2013
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventor: The Board Of Trustees Of The University of Illinois
  • Patent number: 8507464
    Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: August 13, 2013
    Assignee: Threshold Pharmaceuticals, Inc.
    Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao, Jacob Kaizerman
  • Patent number: 8501714
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: September 7, 2010
    Date of Patent: August 6, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
  • Patent number: 8497254
    Abstract: The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 14, 2011
    Date of Patent: July 30, 2013
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im
  • Patent number: 8497255
    Abstract: The present invention relates to novel phosphonic acids derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 16, 2011
    Date of Patent: July 30, 2013
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Ken Chow, Wha-Bin Im
  • Patent number: 8486918
    Abstract: The present invention relates to novel phenyl oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 14, 2011
    Date of Patent: July 16, 2013
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im