The Ring System Contains At Least Three Cyclos Patents (Class 558/429)
  • Patent number: 9656951
    Abstract: The present invention relates to polymorphic forms of the compound of Formula I (i.e., ethyl 2-cyano-3,12-dioxoIeana-1,9(11)-dien-28-oate (CDDO ethyl ester)) and methods of using them for treating a variety of disease states such as cancer and condisitons associated with inflammation.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: May 23, 2017
    Assignee: Applied Pharmaceutical Science, Inc.
    Inventors: Xiaohong Zhang, Lu Song, Wendong Sun, Kaiyang Liu, Chunlei Han
  • Patent number: 9000188
    Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: April 7, 2015
    Assignee: Trustees of Dartmouth College
    Inventors: Tadashi Honda, Emilie David, Dale Mierke
  • Publication number: 20140315997
    Abstract: The present invention relates to polymorphic forms of the compound of Formula I (i.e., ethyl 2-cyano-3,12-dioxoIeana-1,9(11)-dien-28-oate (CDDO ethyl ester)) and methods of using them for treating a variety of disease states such as cancer and condisitons associated with inflammation.
    Type: Application
    Filed: December 6, 2012
    Publication date: October 23, 2014
    Inventors: Xiaohong Zhang, Lv Song, Wendong Sun, Kaiyang Liu, Chunlei Han
  • Publication number: 20140275241
    Abstract: The present disclosure is generally directed to neuroactive substituted cyclopent[a]anthracenes as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventor: Douglas Covey
  • Publication number: 20140256805
    Abstract: The present disclosure is generally directed to neuroactive substituted cyclopenta[b]phenanthrenes as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 11, 2014
    Inventor: Douglas Covey
  • Publication number: 20140221231
    Abstract: A method is described that uses ROR gamma t, or ROR alpha to diagnose rosacea and/or to screen inhibitors of Th17 differentiation, notably in inhibiting ROR gamma t or ROR alpha. Also described is a method of using these screened inhibitors in rosacea treatment.
    Type: Application
    Filed: June 25, 2012
    Publication date: August 7, 2014
    Applicant: Galderma Research & Development
    Inventor: Martin Steinhoff
  • Patent number: 8778990
    Abstract: This invention features betulinic acid derivatives having the formula: wherein the variables are defined herein. The invention also provides related compounds and intermediates thereof, as well as pharmaceutical compositions, kits, and articles of manufacture comprising such compounds. Treatment methods and methods of manufacture are also provided.
    Type: Grant
    Filed: October 29, 2009
    Date of Patent: July 15, 2014
    Assignees: Trustees of Dartmouth College, Reata Pharmaceuticals, Inc.
    Inventors: Tadashi Honda, Michael B. Sporn, Karen T. Liby, Gordon W. Gribble, Robert M. Kral, Jr., Melean Visnick
  • Publication number: 20140100227
    Abstract: Disclosed herein are novel C17-alkanediyl and alkenediyl derivatives of oleanolic acid, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.
    Type: Application
    Filed: September 10, 2013
    Publication date: April 10, 2014
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventors: Christopher F. BENDER, Xin JIANG, Eric ANDERSON, Melean VISNICK
  • Publication number: 20140088188
    Abstract: Disclosed herein are novel C13-hydroxy derivatives of oleanolic acid, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.
    Type: Application
    Filed: September 10, 2013
    Publication date: March 27, 2014
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventors: Xin JIANG, Christopher F. BENDER, Melean VISNICK
  • Publication number: 20140088277
    Abstract: This invention relates to a reaction product obtained by contacting a polymer comprising units derived from dicyclopentadiene with a vinyl terminated macromonomer, a vinyl monomer or a vinylene monomer, in the presence of a metathesis catalyst, where the vinyl monomer or vinylene monomer is represented by the formula: wherein each X is, independently, —CO2R, —CONR1R2, CN, a C1 to a C20 alkyl group; R is a C1 to a C20 alkyl group or an aromatic group; each R1 and R2 is, independently, a hydrogen, a C1 to a C20 alkyl group, or an aromatic group; each R5 is, independently, a hydrogen atom or a C1 to a C40 alkyl group; each Ar is, independently, an aromatic group; and each n is, independently, from 0 to about 40.
    Type: Application
    Filed: September 19, 2013
    Publication date: March 27, 2014
    Inventors: Ian C. Stewart, John R. Hagadorn, Mun F. Tse, George Rodriguez, Patrick Brant
  • Publication number: 20140073700
    Abstract: The present application relates to: (a) compounds of Formula (I): and salts thereof, wherein Y and Z are as defined in the specification; (b) compositions comprising such compounds and salts; and (c) methods of use of such compounds, salts, and compositions, particularly use for the treatment and prevention of diseases such as those associated with oxidative stress and inflammation.
    Type: Application
    Filed: September 10, 2013
    Publication date: March 13, 2014
    Inventors: Rolf Wagner, Hui-Ju Chen, Jason Shanley, Andrew Bogdan, Jasmina Marjanovic, Xiu Wang, Diana Donnelly-Roberts
  • Publication number: 20140066408
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: January 14, 2013
    Publication date: March 6, 2014
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventor: REATA PHARMACEUTICALS, INC.
  • Publication number: 20130324600
    Abstract: The invention relates to compounds of general formula (I) wherein R is (C1-C7)alkyl, (C2-C7)alkenyl or (C2-C7)alkynyl; wherein R is substituted with R1; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
    Type: Application
    Filed: December 22, 2011
    Publication date: December 5, 2013
    Applicant: LEO LABORATORIES LIMITED
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg
  • Publication number: 20130324599
    Abstract: The present invention relates generally to the compound: N-((4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-octadecahydropicen-4a-yl)-2,2-difluoropropanamide, polymorphic forms thereof, methods for preparation and use thereof, pharmaceutical compositions thereof, and kits and articles of manufacture thereof.
    Type: Application
    Filed: April 24, 2013
    Publication date: December 5, 2013
    Applicant: Reata Pharmaceuticals, Inc.
    Inventors: Eric ANDERSON, Xiaofeng LIU, Andrea DECKER
  • Publication number: 20130317007
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: April 11, 2013
    Publication date: November 28, 2013
    Applicant: Reata Pharmaceuticals, Inc.
    Inventors: Eric ANDERSON, Xin JIANG, Melean VISNICK
  • Publication number: 20130274256
    Abstract: Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.
    Type: Application
    Filed: October 11, 2012
    Publication date: October 17, 2013
    Applicant: SEQUOIA SCIENCES, INC.
    Inventor: Sequoia Sciences, Inc.
  • Publication number: 20130274480
    Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.
    Type: Application
    Filed: October 4, 2012
    Publication date: October 17, 2013
    Inventors: Tadashi Honda, Emilie David, Dale Mierke
  • Publication number: 20130237721
    Abstract: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.
    Type: Application
    Filed: August 24, 2011
    Publication date: September 12, 2013
    Inventors: Gordon W. Gribble, Tadashi Honda, Michael B. Sporn, Nanjoo Suh
  • Patent number: 8455544
    Abstract: The present invention concerns methods for treating and preventing renal/kidney disease, insulin resistance/diabetes, fatty liver disease, and/or endothelial dysfunction/cardiovascular disease using synthetic triterpenoids, optionally in combination with a second treatment or prophylaxis.
    Type: Grant
    Filed: January 26, 2012
    Date of Patent: June 4, 2013
    Assignees: Reata Pharmaecuticals, Inc., Trustees of Dartmouth College
    Inventors: Michael B. Sporn, Karen T. Liby, Gordon W. Gribble, Tadashi Honda, Robert M. Kral, Colin J. Meyer
  • Publication number: 20120330050
    Abstract: A triterpenoid compound, methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester), has a non-crystalline, glassy solid form and a non-hydrous crystalline form that can prepared, for example, from a saturated methanol solution. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form. Each form of CDDO methyl ester is a superior candidate for use, typically in solid dosage form, for treating a variety of disease states, generally associated with inflammation.
    Type: Application
    Filed: June 29, 2012
    Publication date: December 27, 2012
    Inventors: John WALLING, Stephan D. Parent, David T. Jonaitis, Robert M. Kral, JR.
  • Publication number: 20120295886
    Abstract: The present disclosure provides compounds having affinity for the M2 proton channel, useful for the treatment of viral infections such as influenza, which are of the Formula (I): wherein R1, R2, and Y are as defined herein. Methods of preparing the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds in the treatment of viral infections such as influenza are also provided.
    Type: Application
    Filed: May 18, 2012
    Publication date: November 22, 2012
    Applicant: INFLUMEDIX, INC.
    Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
  • Publication number: 20120252776
    Abstract: Disclosed herein are novel C4-monomethyl triterpenoid compounds and derivatives thereof, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.
    Type: Application
    Filed: March 12, 2012
    Publication date: October 4, 2012
    Inventors: Eric Anderson, Christopher F. Bender, Xiaofeng Liu, Xin Jiang, Melean Visnick
  • Publication number: 20120245374
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: January 11, 2012
    Publication date: September 27, 2012
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
  • Publication number: 20120238767
    Abstract: Disclosed herein are novel oleanolic acid derivatives. Methods of preparing these compounds are also disclosed. The oleanolic acid derivatives of this invention may be used for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
    Type: Application
    Filed: November 11, 2011
    Publication date: September 20, 2012
    Inventors: Xin Jiang, Jack Greiner, Lester L. Maravetz, Stephen S. Szucs, Melean Visnick
  • Publication number: 20120101149
    Abstract: This invention features betulinic acid derivatives having the formula: wherein the variables are defined herein. The invention also provides related compounds and intermediates thereof, as well as pharmaceutical compositions, kits, and articles of manufacture comprising such compounds. Treatment methods and methods of manufacture are also provided.
    Type: Application
    Filed: October 29, 2009
    Publication date: April 26, 2012
    Inventors: Tadashi Honda, Michael B. Sporn, Karen T. Liby, Gordon W. Gribble, Robert M. Kral, JR., Melean Visnick
  • Publication number: 20120071684
    Abstract: A triterpenoid compound, methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester), has a non-crystalline, glassy solid form and a non-hydrous crystalline form that can prepared, for example, from a saturated methanol solution. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form. Each form of CDDO methyl ester is a superior candidate for use, typically in solid dosage form, for treating a variety of disease states, generally associated with inflammation.
    Type: Application
    Filed: November 29, 2011
    Publication date: March 22, 2012
    Inventors: John Walling, Stephan D. Parent, David T. Jonaitis, Robert M. Kral, JR.
  • Patent number: 8129429
    Abstract: The present invention concerns methods for treating and preventing renal/kidney disease, insulin resistance/diabetes, fatty liver disease, and/or endothelial dysfunction/cardiovascular disease using synthetic triterpenoids, optionally in combination with a second treatment or prophylaxis.
    Type: Grant
    Filed: January 12, 2009
    Date of Patent: March 6, 2012
    Assignees: Reata Pharmaceuticals, Inc., Trustees of Dartmouth College
    Inventors: Michael B. Sporn, Karen T. Liby, Gordon W. Gribble, Tadashi Honda, Robert M. Kral, Colin J. Meyer
  • Publication number: 20120046455
    Abstract: A process for the preparation of a 1,1-cyclopropane(nitrile)(electron-acceptor), the process comprising treating an olefin with an acceptor/acceptor-substituted ?-cyanodiazo reagent in the presence of a catalytic amount of a metal porphyrin catalyst.
    Type: Application
    Filed: August 16, 2011
    Publication date: February 23, 2012
    Inventors: X. Peter Zhang, Shifa Zhu
  • Patent number: 8067465
    Abstract: Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: November 29, 2011
    Assignee: The Trustees of Dartmouth College
    Inventors: Tadashi Honda, Frank G. Favaloro, Gordon W. Gribble, Michael B. Sporn, Nanjoo Suh
  • Publication number: 20110232178
    Abstract: Compounds and methods that release 1-methylcyclopropene, 1-trifluoromethylcyclopropene, and other substituted cyclopropenes are disclosed. The compounds and methods overcome present limitations for storage, transportation, and application of the cyclopropene containing compounds by using light, including sunlight, and/or heat as the primary release trigger. Additional products released include innocuous gases and value added aryl-group compounds.
    Type: Application
    Filed: March 23, 2011
    Publication date: September 29, 2011
    Inventors: John Perrin Davis, Cheryl D. Stevenson
  • Publication number: 20110082053
    Abstract: Provided is a molecular rectifier comprised of a diamondoid molecule and an electron acceptor attached to the diamondoid molecule. The electron acceptor is generally an electron accepting aromatic species which is covalently attached to the diamondoid.
    Type: Application
    Filed: January 30, 2009
    Publication date: April 7, 2011
    Inventors: Wanli Yang, Zhi-Xun Shen, Harindran C. Manoharan, Nicholas A. Melosh, Michael A. Kelly, Andrey A. Fokin, Peter R. Schreiner, Jason C. Randel
  • Publication number: 20110065762
    Abstract: The present invention relates, in part, to methods of treatment, prevention, and inhibition of viral disorders. In one aspect, the present invention relates to inhibition of the M2 proton channel of influenza viruses (e.g. influenza A virus) and other similar viroporins (e.g., VP24 of Ebola and Marburg viruses; and NS3 protein of Bluetongue). The present invention further relates, inter alia, to compounds which have been shown to possess antiviral activity, in particular, inhibiting the M2 proton channel of influenza viruses.
    Type: Application
    Filed: September 13, 2010
    Publication date: March 17, 2011
    Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
  • Publication number: 20110021448
    Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
    Type: Application
    Filed: December 4, 2009
    Publication date: January 27, 2011
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: BRUCE D. HAMMOCK, IN-HAE KIM, CHRISTOPHE MORISSEAU, TAKAHO WATANABE, JOHN W. NEWMAN
  • Publication number: 20100273801
    Abstract: The invention relates to compouns derived from betulin, and to the use thereof as antibacterial agents in pharmaceutical and cosmetic applications.
    Type: Application
    Filed: June 6, 2007
    Publication date: October 28, 2010
    Applicant: Valition teknillinen tutikimuskeskus
    Inventors: Jari Yli-Kauhaluoma, Salme Koskimies, Sami Alakurtti, Taru Mäkelä, Päivi Tammela
  • Publication number: 20100261930
    Abstract: Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.
    Type: Application
    Filed: March 11, 2010
    Publication date: October 14, 2010
    Inventors: Tadashi Honda, Frank G. Favaloro, Gordon W. Gribble, Michael B. Sporn, Nanjoo Suh
  • Patent number: 7678830
    Abstract: Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.
    Type: Grant
    Filed: February 7, 2007
    Date of Patent: March 16, 2010
    Assignee: Trustees of Dartmouth College
    Inventors: Tadashi Honda, Frank G. Favaloro, Gordon W. Gribble, Michael B. Sporn, Nanjoo Suh
  • Publication number: 20100048892
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: April 20, 2009
    Publication date: February 25, 2010
    Inventors: Eric ANDERSON, Xin JIANG, Melean VISNICK
  • Publication number: 20090318551
    Abstract: This invention relates to novel AKBA analogs of the formula I given below: Where in R1, R2, R3, R4 and R5 in each of the said analogs are: 1. R1?OCHO, R2?H, R3?COOH, R4 & R5?O 2. R1?OCOCH2Cl, R2?H, R3?COOH, R4 & R5?O 3. R1=5?-O-methylgalloyloxy, R2?H, R3?COOH, R4 & R5?O 4. R1?OCOCH2CH2COOH, R2?H, R3?COOH, R4 & R5?O 5. R1=8?,9?-Dihydro-4?-hydroxycinnamoyloxy, R2?H, R3?COOH, R4 & R5?O 6. R1=4?-Hydroxycinnamoyloxy, R2?H, R3?COOH, R4 & R5?O 7. R1=3?,4?-Dimethoxycinnamoyloxy, R2?H, R3?COOH, R4 & R5?O 8. R1=3?,4?-Dihydroxy-5?-methoxycinnamoyloxy, R2?H, R3?COOH, R4 & R5?O 9. R1?OCOCH2NH(tert-BOC), R2?H, R3?COOCH3, R4 & R5?O 10. R1?OCOCH2NH2HCl, R2?H, R3?COOH, R4 & R5?O 11. R1?OCOCH(CH3)NH2HCl, R2?H, R3?COOH, R4 & R5?O 12. R1?H, R2?OH, R3?COOCH3, R4 & R5?O 13. R1?H, R2?Br, R3?COOCH3, R4 & R5?O 14. R1?CN, R2?H, R3?COOCH3, R4 & R5?O 15. R1?SH, R2?H, R3?COOCH3, R4 & R5?O 16. R1 & R2?N(OH), R3?COOCH3, R4 & R5?O 17.
    Type: Application
    Filed: August 28, 2009
    Publication date: December 24, 2009
    Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Subbaraju Gottumukkala, Trimurtulu Golakoti
  • Publication number: 20090203634
    Abstract: Amooranin (AMR) has been found to cause tumor cell death through G2/M cell cycle arrest, caspase activation, and apoptosis. Furthermore, it has been demonstrated that AMR is a substrate for P-glycoprotein. Based on these activities, AMR compounds, including AMR analogs, can be used in the treatment of a number of diseases in which aberrant cellular proliferation occurs such as drug-sensitive and drug-resistant cancers, autoimmune disorders, and inflammatory diseases.
    Type: Application
    Filed: April 14, 2006
    Publication date: August 13, 2009
    Applicant: Variety Children's Hospital d/b/a Miami Children's Hospital
    Inventors: Cheppail Ramachandran, P.K. Raveendran Nair, Steven J. Melnick
  • Publication number: 20090156854
    Abstract: The present invention provides an adamantane derivative (I) having a structure represented by the general formula (I); an adamantane derivative (II) having a structure represented by the general formula (II); and a process for producing those adamantane derivatives. An alcohol form of an adamantane compound is reacted with a sulfonyl compound to obtain the adamantane derivative (II), which is then reacted with an alcohol to obtain the adamantane derivative (I). The adamantane derivative (I) and adamantane derivative (II) each having the structure represented by the general formula (I) and general formula (II), respectively, is a novel adamantyl (meth)acrylate compound and useful as a monomer for functional resins such as a photosensitive resin in the field of photolithography.
    Type: Application
    Filed: February 2, 2009
    Publication date: June 18, 2009
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Naoyoshi HATAKEYAMA, Shinji Tanaka, Hidetoshi Ono, Yasunari Okada
  • Publication number: 20080261985
    Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
    Type: Application
    Filed: November 16, 2007
    Publication date: October 23, 2008
    Inventors: Tadashi Honda, Chitra Sundararajan, Gordon W. Gribble, Michael B. Sporn, Karen T. Liby
  • Patent number: 7211589
    Abstract: The present invention provides a novel compound exhibiting an excellent suppressing effect to cell injury caused by radicals and neurotoxicity induced by excitatory nuerotransmitters such as glutamate. Specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Z represents a bivalent organic group and the like of from 2 to 3 carbon atom(s) which may have a substituent; and R3 represents a carboxyl group and the like.
    Type: Grant
    Filed: April 25, 2002
    Date of Patent: May 1, 2007
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Akinori Akaike, Hachiro Sugimoto, Yukio Nishizawa, Masahiro Yonaga, Naoki Asakawa, Naoki Asai, Nariyasu Mano, Taro Terauchi, Takashi Doko
  • Patent number: 7176237
    Abstract: Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.
    Type: Grant
    Filed: January 15, 2003
    Date of Patent: February 13, 2007
    Assignee: The Trustees of Dartmouth College
    Inventors: Tadashi Honda, Frank G. Favaloro, Gordon W. Gribble, Michael B. Sporn, Nanjoo Suh
  • Publication number: 20040180930
    Abstract: The present invention provides a novel compound exhibiting an excellent suppressing effect to cell injury caused by radicals and neurotoxicity induced by excitatory nuerotransmitters such as glutamate. Specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.
    Type: Application
    Filed: October 9, 2003
    Publication date: September 16, 2004
    Inventors: Akinori Akaike, Hachiro Sugimoto, Yukio Nishizawa, Masahiro Yonaga, Naoki Asakawa, Naoki Asai, Nariyasu Mano, Taro Terauchi, Takashi Doko
  • Publication number: 20040002463
    Abstract: New triterpenoid derivatives with various substituents at the C-17 position of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO) were synthesized. Among them, 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-onitrile (CNDDO), 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl) imidazole, 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl)-2-methylimidazole, 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl)-4-methylimidazole show extremely high inhibitory activity (IC50=0.01-1 pM level) against production of nitric oxide induced by interferon-&ggr; in mouse macrophages. These compounds can be used in the prevention or treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, rheumatoid arthritis, and other inflammatory diseases. All the new triterpenoid derivatives are more potent than previously known CDDO.
    Type: Application
    Filed: May 12, 2003
    Publication date: January 1, 2004
    Applicant: The Trustees of Dartmouth College
    Inventors: Tadashi Honda, Yukiko Honda, Gordon W. Gribble, Michael B. Sporn, Nanjoo Suh
  • Publication number: 20030232786
    Abstract: Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.
    Type: Application
    Filed: January 15, 2003
    Publication date: December 18, 2003
    Inventors: Tadashi Honda, Frank G. Favaloro, Gordon W. Gribble, Michael B. Sporn, Nanjoo Suh
  • Publication number: 20020155496
    Abstract: The invention concerns a saturated or unsaturated abietane derivative of general formula (I) wherein: Z is selected among —COOR5, —CONR1R2, —COONR3R4, —COR6, —CON, —COOR5, —CHOHR7, —SR8, —OR8, —CN, —CNO, —CNS, —NCO, —NCS and —R1R2CR9; wherein R1, R2, R3 and R4 represent a hydrogen atom, a C1-C10 alkyl, a C6-C20 aryl optionally substituted, a C7-C10 alkene, a C1-C10 alkyne, or an aminoacyl or peptidyl optionally substituted; or R1 and R2 or R3 and R4 together form a cycle or a heterocycle; R5 represents a hydrogen, a C1-C10 alkyl, a C1-C10 alkene, a C1-C10 alkyne, or an aryl optionally substituted into C6-C20; R6 represents a hydrogen, a halogen, a C1-C10 alkyl, a C1-C10 alkene, a C1-C10 alkyne, or an aryl optionally substituted into C6-C20; R7 represents a hydrogen, a C1-C10 alkyl, a C1-C10 alkene, or a C1-C10 alkyne; R8 represents a hydrogen, a C1-C10 alkyl, a C1-C10 alkene, or a C1-C10 alkyne; and R9 is selected among
    Type: Application
    Filed: January 30, 2001
    Publication date: October 24, 2002
    Inventors: Marie Helene Charles, Nadia Piga, Nicole Battail-Poirot, Laurent Veron, Thierry Delair, Bernard Mandrand
  • Publication number: 20020042535
    Abstract: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.
    Type: Application
    Filed: August 9, 2001
    Publication date: April 11, 2002
    Applicant: Trustees of Dartmouth College
    Inventors: Gordon W. Gribble, Tadashi Honda, Michael B. Sporn, Nanjoo Suh
  • Patent number: RE45288
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: December 9, 2014
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
  • Patent number: RE45325
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: January 6, 2015
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick