The Cyclopentanohydrophenanthrene Ring System Is Part Of A Polycyclo Ring System Having At Least Five Cyclos Patents (Class 552/510)
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Patent number: 9796751Abstract: A novel glycyrrhetinic acid derivative. The glycyrrhetinic acid derivative is represented by the following general formula.Type: GrantFiled: November 20, 2014Date of Patent: October 24, 2017Assignees: INI CORPORATIONInventors: Hideyuki Takeuchi, Akio Suzumura
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Patent number: 9505800Abstract: 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: GrantFiled: November 2, 2007Date of Patent: November 29, 2016Assignee: Myrexis, Inc.Inventors: Theodore J. Nitz, Christian Montalbetti, Richard Mears, Xinjie Gai, Edward Glenn
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Patent number: 9428542Abstract: 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: GrantFiled: January 30, 2013Date of Patent: August 30, 2016Assignees: JIANGXI QINGFENG PHARMACEUTICAL INC.Inventor: Feng Lu
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Patent number: 9340513Abstract: 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: GrantFiled: December 14, 2012Date of Patent: May 17, 2016Assignee: GlaxoSmithKline LLCInventors: Nianhe Han, Brian Alvin Johns, Jun Tang
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Patent number: 9303058Abstract: 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: GrantFiled: November 8, 2013Date of Patent: April 5, 2016Inventor: Jean-Claude Leunis
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Patent number: 9200029Abstract: 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: GrantFiled: August 19, 2011Date of Patent: December 1, 2015Assignees: Kao Corporation, Tsuno Food Industrial Co., Ltd.Inventors: Kohjiro Hashizume, Takuo Tsuno, Koji Kato, Hisahiro Morita
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Patent number: 9102685Abstract: 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: GrantFiled: December 14, 2012Date of Patent: August 11, 2015Assignee: GlaxoSmithKline LLCInventor: Brian Alvin Johns
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Publication number: 20150119373Abstract: 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: ApplicationFiled: April 19, 2013Publication date: April 30, 2015Inventors: 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
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Publication number: 20150005267Abstract: 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: ApplicationFiled: September 18, 2014Publication date: January 1, 2015Inventors: Tony Durst, Zulifiquar Merali, John T. Arnason, E. Pablo Sanchez-Vindas, Luis J. Poveda-Alvarez
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Publication number: 20150004260Abstract: 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: ApplicationFiled: May 6, 2014Publication date: January 1, 2015Inventors: Henry Lowe, Joseph L. Bryant
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Patent number: 8906889Abstract: 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: GrantFiled: February 6, 2013Date of Patent: December 9, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Jacob Swidorski, Nicholas A. Meanwell, Alicia Regueiro-Ren, Sing-Yuen Sit, Jie Chen, Yan Chen
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Patent number: 8889854Abstract: 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: GrantFiled: March 13, 2013Date of Patent: November 18, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Ny Sin, Zheng Liu, Jacob Swidorski, Sing-Yuen Sit, Jie Chen, Yan Chen, Nicholas A. Meanwell, Alicia Regueiro-Ren
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Publication number: 20140296546Abstract: 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: ApplicationFiled: March 15, 2012Publication date: October 2, 2014Applicant: WENZHOU UNIVERSITYInventors: Xiufeng Yan, Mingjiang Wu, Lihua Wang, Ping Yu, Nan Li
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Patent number: 8846647Abstract: 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: GrantFiled: January 27, 2012Date of Patent: September 30, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
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Patent number: 8828444Abstract: 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: GrantFiled: August 20, 2013Date of Patent: September 9, 2014Assignee: Birken AGInventor: Armin Scheffler
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Publication number: 20140243298Abstract: 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: ApplicationFiled: February 21, 2014Publication date: August 28, 2014Inventors: Jacob Swidorski, Yan Chen, Sing-Yuen Sit, Nicholas A. Meanwell, Alicia Regueiro-Ren, Jie Chen
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Patent number: 8802727Abstract: 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: GrantFiled: January 10, 2011Date of Patent: August 12, 2014Assignee: Hetero Research Foundation, Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Vedula Manohar Sharma, Kura Rathnakar Reddy, Musku Madhanmohan Reddy
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Patent number: 8802661Abstract: 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: GrantFiled: June 2, 2011Date of Patent: August 12, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Nicholas A. Meanwell, Sing-Yuen Sit, Jie Chen, Yan Chen, Ny Sin
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Patent number: 8785424Abstract: 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: GrantFiled: May 20, 2010Date of Patent: July 22, 2014Assignees: Pierre Fabre Medicament, Centre National de la Recherche Scientifique (CNRS)Inventors: Christophe Long, Yves Guminski, Fadila Derguini, Joséphine Beck, Frédéric Cantagrel
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Patent number: 8754069Abstract: 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: GrantFiled: September 20, 2012Date of Patent: June 17, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Zheng Liu, Nicholas A. Meanwell, Alicia Regueiro-Ren
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Patent number: 8754068Abstract: 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: GrantFiled: June 2, 2011Date of Patent: June 17, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Alicia Regueiro-Ren, Jacob Swidorski, Zheng Liu, Nicholas A. Meanwell, Sing-Yuen Sit, Jie Chen, Ny Sin
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Patent number: 8748415Abstract: 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: GrantFiled: January 27, 2012Date of Patent: June 10, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Alicia Regueiro-Ren, Jacob Swidorski, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell, Zheng Liu
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Patent number: 8586569Abstract: 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: GrantFiled: September 4, 2008Date of Patent: November 19, 2013Inventors: Jean-Claude Leunis, Emmanuel Couche
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Patent number: 8536380Abstract: 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: GrantFiled: June 21, 2005Date of Patent: September 17, 2013Assignee: Birken GmbHInventor: Armin Scheffler
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Patent number: 8536160Abstract: 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: GrantFiled: April 11, 2007Date of Patent: September 17, 2013Assignee: 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
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Publication number: 20130203712Abstract: 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: ApplicationFiled: May 19, 2011Publication date: August 8, 2013Applicant: University of Iowa Research FoundationInventors: Christopher M. Adams, Steven D. Kunkel
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Publication number: 20130137883Abstract: 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: ApplicationFiled: August 19, 2011Publication date: May 30, 2013Applicants: TSUNO FOOD INDUSTRIAL CO., LTD., KAO CORPORATIONInventors: Kohjiro Hashizume, Takuo Tsuno, Koji Kato, Hisahiro Morita
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Patent number: 8431556Abstract: 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: GrantFiled: July 3, 2010Date of Patent: April 30, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Christophe Moinet, Marc Courchesne, Liliane Halab, Nathalie Chauret, Laval Chan Chun Kong
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Publication number: 20130096094Abstract: 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: ApplicationFiled: September 10, 2012Publication date: April 18, 2013Applicants: Universite Paris Descartes, Centre National de la Recherche ScientifiqueInventors: Serge Bouaziz, Pascale Coric, Pierre Boulanger, Saw-See Hong, Serge Turcaud, Florence Souquet, Nathalie Chazal, Laurence Briant
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Publication number: 20130072465Abstract: 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: ApplicationFiled: September 20, 2012Publication date: March 21, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130065868Abstract: 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: ApplicationFiled: November 8, 2012Publication date: March 14, 2013Applicant: UNIVERSITY OF OTTAWAInventor: University of Ottawa
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Publication number: 20130035318Abstract: 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: ApplicationFiled: January 27, 2012Publication date: February 7, 2013Inventors: ALICIA REGUEIRO-REN, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
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Publication number: 20130029954Abstract: 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: ApplicationFiled: January 27, 2012Publication date: January 31, 2013Inventors: Alicia Regueiro-Ren, Jacob Swidorski, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell, Zheng Liu
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Publication number: 20120302530Abstract: 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: ApplicationFiled: May 13, 2010Publication date: November 29, 2012Applicant: SUZHOU MAIDIXIAN PHARMACEUTICAL INC.Inventors: Nan Zhang, Rong Zhong
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Publication number: 20120302534Abstract: 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: ApplicationFiled: February 9, 2011Publication date: November 29, 2012Inventors: Daxin Gao, Nianhe Han, Zhimin Jin, Fangxian Ning, Jun Tang, Yongyong Wu, Heping Yang
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Publication number: 20120283217Abstract: 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: ApplicationFiled: July 16, 2012Publication date: November 8, 2012Applicant: SATORI PHARMACEUTICALS, INC.Inventors: Mark A. Findeis, Steffen P. Creaser
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Patent number: 8269026Abstract: 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: GrantFiled: July 3, 2010Date of Patent: September 18, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: 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
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Publication number: 20120214775Abstract: 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: ApplicationFiled: April 30, 2012Publication date: August 23, 2012Applicant: Myrexis, Inc.Inventors: Martin Dale POWER, David Eugene MARTIN
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Publication number: 20120077777Abstract: 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: ApplicationFiled: May 20, 2010Publication date: March 29, 2012Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), PIERRE FABRE MEDICAMENTInventors: Christophe Long, Yves Guminski, Fadila Derguini, Joséphine Beck, Frédéric Cantagrel
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Publication number: 20120040930Abstract: 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: ApplicationFiled: January 13, 2006Publication date: February 16, 2012Inventors: Catherine Guillou, Jean-Yves Lallemand, Thibault Sauvaítre, Jordi Molgo, Denyse Herlem, Daniel Guenard, Françoise Khuong-Huu
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Patent number: 8093413Abstract: 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: GrantFiled: January 9, 2008Date of Patent: January 10, 2012Assignees: Univerzita Karlova V Praze, Prirodovedecka Fakulta, Univerzita Palackeho V Olomouci and I.Q.A., a.s.Inventors: Jan Sarek, Michal Svoboda, Marian Hajduch
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Patent number: 8088757Abstract: 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: GrantFiled: September 12, 2005Date of Patent: January 3, 2012Assignee: BioRings LLCInventors: Brij B. Saxena, Premila Rathnam
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Patent number: 8022055Abstract: 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: GrantFiled: December 29, 2005Date of Patent: September 20, 2011Assignee: Dabur Pharma LimitedInventors: 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
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Publication number: 20110224182Abstract: 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: ApplicationFiled: July 17, 2009Publication date: September 15, 2011Applicant: Myriad Pharmaceuticals, IncorporatedInventors: Peter Bullock, Theodore J. Nitz, Gary Sweetapple
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Publication number: 20110152229Abstract: 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: ApplicationFiled: November 21, 2007Publication date: June 23, 2011Inventors: Chin Ho Chen, Li Huang, Kuo-Hsiung Lee
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Publication number: 20110144069Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection.Type: ApplicationFiled: October 16, 2007Publication date: June 16, 2011Applicant: Myriad Genetics, IncorporatedInventors: Kraig M. Yager, Esther Arranz Plaza, Dange Vijay Kumar, In Chul Kim
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Publication number: 20110077227Abstract: 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: ApplicationFiled: July 3, 2010Publication date: March 31, 2011Inventors: 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
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Patent number: 7858606Abstract: 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: GrantFiled: May 23, 2001Date of Patent: December 28, 2010Assignees: Univerzita Palackeho v Olomouci, Univerzita Karlova V PrazeInventors: Marian Hajduch, Jan Sarek
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Patent number: 7851641Abstract: 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: GrantFiled: May 16, 2006Date of Patent: December 14, 2010Assignee: Satori Pharmaceuticals, Inc.Inventors: Mark A. Findeis, Kollol Pal, Frank Schroeder
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Patent number: 7851462Abstract: 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: GrantFiled: December 21, 2007Date of Patent: December 14, 2010Assignee: Novelix Pharmaceuticals, Inc.Inventors: Edgar Selzer, Burkhard Jansen, Reinhard Paschke