The Cyclopentanohydrophenanthrene Ring System Is Part Of A Polycyclo Ring System Having At Least Five Cyclos Patents (Class 552/510)
  • Patent number: 9796751
    Abstract: A novel glycyrrhetinic acid derivative. The glycyrrhetinic acid derivative is represented by the following general formula.
    Type: Grant
    Filed: November 20, 2014
    Date of Patent: October 24, 2017
    Assignees: INI CORPORATION
    Inventors: Hideyuki Takeuchi, Akio Suzumura
  • Patent number: 9505800
    Abstract: The present invention concerns novel pharmaceutically active triterpene derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C2-8 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus (HIV).
    Type: Grant
    Filed: November 2, 2007
    Date of Patent: November 29, 2016
    Assignee: Myrexis, Inc.
    Inventors: Theodore J. Nitz, Christian Montalbetti, Richard Mears, Xinjie Gai, Edward Glenn
  • Patent number: 9428542
    Abstract: The present invention relates to a lupane triterpenoid derivatives and pharmaceutical use thereof, specifically relates to a lupane triterpenoid derivatives of formula (I)˜(III), a pharmaceutical composition and a combination preparation comprising a lupane triterpenoid derivatives or a pharmaceutically acceptable salt thereof in a therapeutically-effective dose, particularly relates to the use in preparation of a medicament for the treatment of HIV-1/AIDS.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: August 30, 2016
    Assignees: JIANGXI QINGFENG PHARMACEUTICAL INC.
    Inventor: Feng Lu
  • Patent number: 9340513
    Abstract: The present invention relates to a compound characterized by the following Formula I: or a pharmaceutically acceptable salt thereof, wherein X, Y, and Z are as described herein. Compounds of the present invention are useful for the treatment of HIV.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: May 17, 2016
    Assignee: GlaxoSmithKline LLC
    Inventors: Nianhe Han, Brian Alvin Johns, Jun Tang
  • Patent number: 9303058
    Abstract: The present invention relates to betulonic and betulinic acid derivatives and, in particular, to C-28 and C-3 derivatives. The present invention relates to betulonic acid esters, and dihydro-betulonic acid esters. Betulinic acid and derivatives thereof may be bound to a poly(alkylene glycol) (PAG) such as poly(ethylene glycol). Binding may be via a linker, such as a diamine, an amino acid, a peptide, an ester or a carbonate. The compounds of the present invention may be used for the treatment of cancer or a viral infection. The present invention also provides pharmaceutical compositions comprising the compounds of the present invention.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: April 5, 2016
    Inventor: Jean-Claude Leunis
  • Patent number: 9200029
    Abstract: A process for producing triterpene alcohol, comprising sequentially conducting the following steps (A) to (C): (A) subjecting ?-oryzanol to alkaline hydrolysis; (B) mixing the alkaline hydrolysate with a low polarity organic solvent, and extracting triterpene alcohol to obtain a triterpene alcohol-containing low polarity organic solvent; and (C) adding water to the triterpene alcohol-containing low polarity organic solvent thus obtained, removing the low polarity organic solvent, and then melting triterpene alcohol in hot water, followed by cooling.
    Type: Grant
    Filed: August 19, 2011
    Date of Patent: December 1, 2015
    Assignees: Kao Corporation, Tsuno Food Industrial Co., Ltd.
    Inventors: Kohjiro Hashizume, Takuo Tsuno, Koji Kato, Hisahiro Morita
  • Patent number: 9102685
    Abstract: The present invention relates to compounds characterized by having a structure according to the following Formula I: or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: August 11, 2015
    Assignee: GlaxoSmithKline LLC
    Inventor: Brian Alvin Johns
  • Publication number: 20150119373
    Abstract: The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
    Type: Application
    Filed: April 19, 2013
    Publication date: April 30, 2015
    Inventors: Bandi Parthasaradhi Reddy, Vedula Manohar Sharma, Kura Rathnakar Reddy, Mamnoor Prem Kumar, Kasireddy Bhaskar Reddy, Mogili Narsingam, Mukkera Venkati, Lanka VL Subrahmanyam, Ravi Mallikarjun Reddy
  • Publication number: 20150005267
    Abstract: Pharmaceutical compositions for preventing or treating anxiety, comprising betulinic acid or derivatives thereof are provided. Methods for preventing or treating anxiety with betulinic acid or derivatives thereof are also provided. The invention further provides betulinic-acid containing preparations of plants of the family Marcgraviaceae having anxiolytic activity and methods for making such extracts and using them to prevent or treat anxiety in a subject.
    Type: Application
    Filed: September 18, 2014
    Publication date: January 1, 2015
    Inventors: Tony Durst, Zulifiquar Merali, John T. Arnason, E. Pablo Sanchez-Vindas, Luis J. Poveda-Alvarez
  • Publication number: 20150004260
    Abstract: A method of treating prostate cancer by administering a pharmaceutically-acceptable amount of a crude extract of the indigenous Jamaican plant Ball Moss (Tillandsia Recurvata) comprising one or more cycloartane isolates, and the isolates used in the method for eliciting thereby a kinase inhibitory response of prostate cancer cells by selectively inhibiting MRCK? kinase and angiogenesis of (growth of new blood vessels) to reduce the viability of prostate cancer cells. The method and compounds holds promise as a chemopreventive agent, without causing excessive damage to normal cells.
    Type: Application
    Filed: May 6, 2014
    Publication date: January 1, 2015
    Inventors: Henry Lowe, Joseph L. Bryant
  • Patent number: 8906889
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-3 cycloalkenyl triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: wherein X can be a C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6-9 oxaspirocycloalkyl, or C6-9 oxaspirocycloalkenyl ring. These compounds are useful for the treatment of HIV and AIDS.
    Type: Grant
    Filed: February 6, 2013
    Date of Patent: December 9, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jacob Swidorski, Nicholas A. Meanwell, Alicia Regueiro-Ren, Sing-Yuen Sit, Jie Chen, Yan Chen
  • Patent number: 8889854
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: November 18, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ny Sin, Zheng Liu, Jacob Swidorski, Sing-Yuen Sit, Jie Chen, Yan Chen, Nicholas A. Meanwell, Alicia Regueiro-Ren
  • Publication number: 20140296546
    Abstract: The invention discloses a method for producing 30-halogenated betulinic acid. Betulin is used as a raw material and selectively oxidized and halogenated to generate 30-betulinic acid, and the selected oxidation and halogenation agent has high selectivity and does not affect C-3 hydroxyl or carbon-carbon double bonds. Oxidation and halogenation are completed in one step, so the process route is short, the treatment method is simple, and the product is purified easily.
    Type: Application
    Filed: March 15, 2012
    Publication date: October 2, 2014
    Applicant: WENZHOU UNIVERSITY
    Inventors: Xiufeng Yan, Mingjiang Wu, Lihua Wang, Ping Yu, Nan Li
  • Patent number: 8846647
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: September 30, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
  • Patent number: 8828444
    Abstract: The invention relates to an oleogel-forming agent which comprises at least one highly dispersed triterpene. The invention also relates to an oleogel which comprises a nonpolar liquid in an amount ranging from 80% by weight to 99% by weight based on the total weight of the oleogel and an oleogel-forming agent comprising a highly dispersed triterpene in an amount ranging from 1% by weight to 20% by weight based on the total weight of the oleogel. The invention also relates to a method for producing an oleogel.
    Type: Grant
    Filed: August 20, 2013
    Date of Patent: September 9, 2014
    Assignee: Birken AG
    Inventor: Armin Scheffler
  • Publication number: 20140243298
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, alkyl and alkenyl C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: a compound of Formula I a compound of Formula II a compound of Formula III and a compound of Formula IV These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: February 21, 2014
    Publication date: August 28, 2014
    Inventors: Jacob Swidorski, Yan Chen, Sing-Yuen Sit, Nicholas A. Meanwell, Alicia Regueiro-Ren, Jie Chen
  • Patent number: 8802727
    Abstract: The present invention relates to certain novel salts of Betulinic acid derivatives, to process for preparing such compounds, to use the compounds in treating diseases or disorders mediated by HIV infection, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 10, 2011
    Date of Patent: August 12, 2014
    Assignee: Hetero Research Foundation, Hetero Drugs Limited
    Inventors: Bandi Parthasaradhi Reddy, Vedula Manohar Sharma, Kura Rathnakar Reddy, Musku Madhanmohan Reddy
  • Patent number: 8802661
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, modified C-3 and C-28 betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: August 12, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Nicholas A. Meanwell, Sing-Yuen Sit, Jie Chen, Yan Chen, Ny Sin
  • Patent number: 8785424
    Abstract: The present invention relates to a compound of following formula (I): or to a pharmaceutically acceptable salt thereof, as well as to pharmaceutical compositions including same and to the use thereof as a drug, in particular for treating a proliferative disease such as cancer.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: July 22, 2014
    Assignees: Pierre Fabre Medicament, Centre National de la Recherche Scientifique (CNRS)
    Inventors: Christophe Long, Yves Guminski, Fadila Derguini, Joséphine Beck, Frédéric Cantagrel
  • Patent number: 8754068
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, modified C-3 betulinic acid and other structurally related natural products derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: June 17, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alicia Regueiro-Ren, Jacob Swidorski, Zheng Liu, Nicholas A. Meanwell, Sing-Yuen Sit, Jie Chen, Ny Sin
  • Patent number: 8754069
    Abstract: Compounds of Formula I: that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.
    Type: Grant
    Filed: September 20, 2012
    Date of Patent: June 17, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Zheng Liu, Nicholas A. Meanwell, Alicia Regueiro-Ren
  • Patent number: 8748415
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-28 amines of C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: June 10, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alicia Regueiro-Ren, Jacob Swidorski, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell, Zheng Liu
  • Patent number: 8586569
    Abstract: The present invention relates to betulonic and betulinic acid derivatives and, in particular, to C-28 and C-3 derivatives. The present invention relates to betulonic acid esters, dihydro-betulonic acid esters, PAG-modified betulinic acid derivatives, and PAG-modified dihydro-betulinic acid derivatives. Betulinic acid and derivatives thereof may be bound to a poly(alkylene glycol) (PAG) such as poly(ethylene glycol). Binding may be via a linker, such as a diamine, an amino acid, a peptide, an ester or a carbonate. The compounds of the present invention may be used for the treatment of cancer or a viral infection. The present invention also provides pharmaceutical compositions comprising the compounds of the present invention. The present invention further provides processes for the preparation of the compounds of the present invention, for example, from betulin.
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: November 19, 2013
    Inventors: Jean-Claude Leunis, Emmanuel Couche
  • Patent number: 8536160
    Abstract: Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. They are useful for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.
    Type: Grant
    Filed: April 11, 2007
    Date of Patent: September 17, 2013
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Giorgio Fedrizzi, Alessandra Benicchio, Giuseppe Bianchi, Patrizia Ferrari, Mauro Gobbini, Rosamaria Micheletti, Marco Pozzi, Piero Enrico Scotti
  • Patent number: 8536380
    Abstract: The invention relates to an oleogel-forming agent which comprises at least one highly dispersed triterpene. The invention also relates to an oleogel which comprises a nonpolar liquid in an amount ranging from 80% by weight to 99% by weight based on the total weight of the oleogel and an oleogel-forming agent comprising a highly dispersed triterpene in an amount ranging from 1% by weight to 20% by weight based on the total weight of the oleogel. The invention also relates to a method for producing an oleogel.
    Type: Grant
    Filed: June 21, 2005
    Date of Patent: September 17, 2013
    Assignee: Birken GmbH
    Inventor: Armin Scheffler
  • Publication number: 20130203712
    Abstract: In one aspect, the invention relates methods for inhibiting or preventing muscle atrophy or increasing muscle mass by providing to a subject in need thereof an effective amount of ursolic acid, a derivative thereof, or an analog of the ursane scaffold. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: May 19, 2011
    Publication date: August 8, 2013
    Applicant: University of Iowa Research Foundation
    Inventors: Christopher M. Adams, Steven D. Kunkel
  • Publication number: 20130137883
    Abstract: A process for producing triterpene alcohol, comprising sequentially conducting the following steps (A) to (C): (A) subjecting ?-oryzanol to alkaline hydrolysis; (B) mixing the alkaline hydrolysate with a low polarity organic solvent, and extracting triterpene alcohol to obtain a triterpene alcohol-containing low polarity organic solvent; and (C) adding water to the triterpene alcohol-containing low polarity organic solvent thus obtained, removing the low polarity organic solvent, and then melting triterpene alcohol in hot water, followed by cooling.
    Type: Application
    Filed: August 19, 2011
    Publication date: May 30, 2013
    Applicants: TSUNO FOOD INDUSTRIAL CO., LTD., KAO CORPORATION
    Inventors: Kohjiro Hashizume, Takuo Tsuno, Koji Kato, Hisahiro Morita
  • Patent number: 8431556
    Abstract: The invention relates to 21-keto triterpene compounds of formula (I): wherein R1, X and Y are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infections by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.
    Type: Grant
    Filed: July 3, 2010
    Date of Patent: April 30, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Christophe Moinet, Marc Courchesne, Liliane Halab, Nathalie Chauret, Laval Chan Chun Kong
  • Publication number: 20130096094
    Abstract: The present invention relates to compounds of the following formula (I): or a pharmaceutically acceptable salt thereof, a stereoisomer or a mixture of stereoisomers in any proportion, in particular a mixture of enantiomers, and particularly a racemate mixture, in which R represents a (C1-C10)alkyl group substituted with one or more, preferably one or two, groups chosen from COOH and NHR1, with R1 representing a hydrogen atom or a -Alk, —C(O)-Alk or —C(O)O-Alk group, Alk representing a (C1-C6)alkyl group, as well as a method for preparing them, and their use as a medicine, notably for treating an infection with a retrovirus such as HIV.
    Type: Application
    Filed: September 10, 2012
    Publication date: April 18, 2013
    Applicants: Universite Paris Descartes, Centre National de la Recherche Scientifique
    Inventors: Serge Bouaziz, Pascale Coric, Pierre Boulanger, Saw-See Hong, Serge Turcaud, Florence Souquet, Nathalie Chazal, Laurence Briant
  • Publication number: 20130072465
    Abstract: Compounds of Formula I: that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: September 20, 2012
    Publication date: March 21, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130065868
    Abstract: Pharmaceutical compositions for preventing or treating anxiety, comprising betulinic acid or derivatives thereof are provided. Methods for preventing or treating anxiety with betulinic acid or derivatives thereof are also provided. The invention further provides betulinic-acid containing preparations of plants of the family Marcgraviaceae having anxiolytic activity and methods for making such extracts and using them to prevent or treat anxiety in a subject.
    Type: Application
    Filed: November 8, 2012
    Publication date: March 14, 2013
    Applicant: UNIVERSITY OF OTTAWA
    Inventor: University of Ottawa
  • Publication number: 20130035318
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: January 27, 2012
    Publication date: February 7, 2013
    Inventors: ALICIA REGUEIRO-REN, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
  • Publication number: 20130029954
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-28 amines of C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: January 27, 2012
    Publication date: January 31, 2013
    Inventors: Alicia Regueiro-Ren, Jacob Swidorski, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell, Zheng Liu
  • Publication number: 20120302534
    Abstract: The present invention relates to a compound characterized by the following Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X, and Y are as described herein. Compounds of the present invention are useful for the treatment of HIV-1.
    Type: Application
    Filed: February 9, 2011
    Publication date: November 29, 2012
    Inventors: Daxin Gao, Nianhe Han, Zhimin Jin, Fangxian Ning, Jun Tang, Yongyong Wu, Heping Yang
  • Publication number: 20120302530
    Abstract: The present invention discloses 23-hydroxyl-betulinic acid derivatives, including 3-oxo-23-hydroxyl-betulinic acid, 3-oxo-23-hydroxyl-dihydrobetulinic acid, and 23-hydroxyl-dihydrobetulinic acid. The present invention also discloses the preparation methods thereof and medical applications as anti-tumor and anti-HIV agents.
    Type: Application
    Filed: May 13, 2010
    Publication date: November 29, 2012
    Applicant: SUZHOU MAIDIXIAN PHARMACEUTICAL INC.
    Inventors: Nan Zhang, Rong Zhong
  • Publication number: 20120283217
    Abstract: As described herein, the present invention provides compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.
    Type: Application
    Filed: July 16, 2012
    Publication date: November 8, 2012
    Applicant: SATORI PHARMACEUTICALS, INC.
    Inventors: Mark A. Findeis, Steffen P. Creaser
  • Patent number: 8269026
    Abstract: The invention relates to 21-keto triterpene compounds of formula (I): wherein R1, X, and Y are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infections by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.
    Type: Grant
    Filed: July 3, 2010
    Date of Patent: September 18, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Christophe Moinet, Liliane Halab, Nathalie Turcotte, Monica Bubenik, Marc Courchesne, Carl Poisson, Oswy Z. Pereira, Paul Nguyen-Ba, Bingcan Liu, Nathalie Chauret, Caroline Cadilhac, Laval Chan Chun Kong
  • Publication number: 20120214775
    Abstract: Salts of 3-O-(3?,3?-dimethylsuccinyl)Betulinic acid (DSB) are disclosed. Particularly, the preparation, pharmaceutical evaluation, and in vivo bioavailability evaluation of N-methyl-D-glucamine and alkali metal salt forms of DSB are disclosed. Pharmaceutical compositions including these salt forms are used in methods of treating HIV and related diseases. Methods of making the salts of DSB and the pharmaceutical compositions are also provided.
    Type: Application
    Filed: April 30, 2012
    Publication date: August 23, 2012
    Applicant: Myrexis, Inc.
    Inventors: Martin Dale POWER, David Eugene MARTIN
  • Publication number: 20120077777
    Abstract: The present invention relates to a compound of following formula (I): or to a pharmaceutically acceptable salt thereof, as well as to pharmaceutical compositions including same and to the use thereof as a drug, in particular for treating a proliferative disease such as cancer.
    Type: Application
    Filed: May 20, 2010
    Publication date: March 29, 2012
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), PIERRE FABRE MEDICAMENT
    Inventors: Christophe Long, Yves Guminski, Fadila Derguini, Joséphine Beck, Frédéric Cantagrel
  • Publication number: 20120040930
    Abstract: The invention concerns a triterpene alkaloid of general formula (I). The invention also concerns a method for making same and use thereof as medicine.
    Type: Application
    Filed: January 13, 2006
    Publication date: February 16, 2012
    Inventors: Catherine Guillou, Jean-Yves Lallemand, Thibault Sauvaítre, Jordi Molgo, Denyse Herlem, Daniel Guenard, Françoise Khuong-Huu
  • Patent number: 8093413
    Abstract: The invention relates to a method of preparation and isolation of betulin diacetate from birch bark from paper mills and its optional processing to betulin, wherein the birch bark is ground, mixed with two- to twenty-fold excess volume of water and is stirred so that all birch bark is dipped, then the fraction of the birch bark which floats on the surface is collected, said collected fraction is dried at the temperature in the range of from 50 to 85° C. and the betulin contained in the dried birch bark is then subjected to an acetylation reaction, after the acetylation the birch bark is dried at the temperature of from 50 to 100° C. and the formed betulin diacetate is then isolated from the birch bark by supercritical extraction of the birch bark with carbon dioxide at the pressure of 28-35 MPa and the temperature of from 50 to 100° C. and subsequently, the supercritical extract is recrystallized for direct use or for further processing.
    Type: Grant
    Filed: January 9, 2008
    Date of Patent: January 10, 2012
    Assignees: Univerzita Karlova V Praze, Prirodovedecka Fakulta, Univerzita Palackeho V Olomouci and I.Q.A., a.s.
    Inventors: Jan Sarek, Michal Svoboda, Marian Hajduch
  • Patent number: 8088757
    Abstract: The present invention relates to a method of treating cancer selected from the group of cancers consisting of prostate cancer, renal cancer, breast cancer, ovarian cancer, CNS cancer, melanoma, lung cancer, and bladder cancer. This method involves administering to a patient in need of such treatment a therapeutically effective amount of a betulinol derivative compound of Formula (I). Also disclosed are conjugated and immunoconjugated derivatives of the compound of Formula (I) as well as methods of making and using them.
    Type: Grant
    Filed: September 12, 2005
    Date of Patent: January 3, 2012
    Assignee: BioRings LLC
    Inventors: Brij B. Saxena, Premila Rathnam
  • Patent number: 8022055
    Abstract: The invention relates to novel betulinic acid derivatives of formula (I), wherein R is C(?CH2)CH3 or CH(CH3)2; R2 together with the adjacent carbonyl group forms a carboxylic acid, carboxylic acid ester or amide or substituted amide; R3 or R4 are hydrogen or aryl with the proviso that both are not independently hydrogen or alkyl or R3 and R4 are combined together to form an aryl ring optionally substituted with a group X, wherein X is selected from halogen, alkyl, cyano, nitro, alkoxy, amino or substituted amine; Y is N or O; and R1 is zero when Y is O, and R1 is hydrogen, alkyl or aryl alkyl when Y is N, useful for inhibition of tumor cancer cells.
    Type: Grant
    Filed: December 29, 2005
    Date of Patent: September 20, 2011
    Assignee: Dabur Pharma Limited
    Inventors: Rama Mukherjee, Sanjay Kumar Srivastava, Mohammad Jamshed Ahmed Siddiqui, Manu Jaggi, Anu T. Singh, Anand Vardhan, Manoj Kumar Singh, Praveen Rajendran, Hemant Kumar Jajoo, Anand C. Burman, Vivek Kumar, Nidhi Rani, Shiv Kumar Agarwal
  • Publication number: 20110224182
    Abstract: The present invention concerns novel pharmaceutically active compounds, pharmaceutical compositions containing the same, methods of making the compounds, polymorphic forms of the compounds, the compounds for use as medicaments, and use of the compounds for the manufacture of medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are certain salts of 3-O-(3?,3?-dimethylsuccinyl)betulinic acid, also known as “DSB.” The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus (“HIV”).
    Type: Application
    Filed: July 17, 2009
    Publication date: September 15, 2011
    Applicant: Myriad Pharmaceuticals, Incorporated
    Inventors: Peter Bullock, Theodore J. Nitz, Gary Sweetapple
  • Publication number: 20110152229
    Abstract: The present invention provides compounds of the general structure: which are substituted at the 3 and 28 positions, along with pharmaceutical formulations containing the same and methods of treating viral infections employing the same.
    Type: Application
    Filed: November 21, 2007
    Publication date: June 23, 2011
    Inventors: Chin Ho Chen, Li Huang, Kuo-Hsiung Lee
  • Publication number: 20110144069
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection.
    Type: Application
    Filed: October 16, 2007
    Publication date: June 16, 2011
    Applicant: Myriad Genetics, Incorporated
    Inventors: Kraig M. Yager, Esther Arranz Plaza, Dange Vijay Kumar, In Chul Kim
  • Publication number: 20110077227
    Abstract: The invention relates to 21-keto triterpene compounds of formula (I): wherein R1, X, and Y are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infections by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.
    Type: Application
    Filed: July 3, 2010
    Publication date: March 31, 2011
    Inventors: Christophe Moinet, Liliane Halab, Nathalie Turcotte, Monica Bubenik, Marc Courchesne, Carl Poisson, Oswy Z. Pereira, Paul Nguyen-Ba, Bingcan Liu, Nathalie Chauret, Caroline Cadilhac, Laval Chan Chun Kong
  • Patent number: 7858606
    Abstract: The present invention relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, in the preparation of a medicament for treating a patient suffering from leukaemia, cancer or other proliferative disorder. A further embodiment relates to the use a compound of formula (I) in an assay for detecting the phosphorylation state of cellular substrates. The present invention also relates to novel compounds of formula (I), and the chemical synthesis thereof.
    Type: Grant
    Filed: May 23, 2001
    Date of Patent: December 28, 2010
    Assignees: Univerzita Palackeho v Olomouci, Univerzita Karlova V Praze
    Inventors: Marian Hajduch, Jan Sarek
  • Patent number: 7851462
    Abstract: The present invention relates to novel betulinic acid derivatives with increased activity for the treatment of carcinomas and HIV diseases, a method for preparing such novel betulinic acid derivatives as well as their use as pharmaceuticals.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: December 14, 2010
    Assignee: Novelix Pharmaceuticals, Inc.
    Inventors: Edgar Selzer, Burkhard Jansen, Reinhard Paschke
  • Patent number: 7851641
    Abstract: As described herein, the present invention provides compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: December 14, 2010
    Assignee: Satori Pharmaceuticals, Inc.
    Inventors: Mark A. Findeis, Kollol Pal, Frank Schroeder