The Additional Ring Shares The 1,2-positions Of The Cyclopentanohydrophenanthrene Ring System Patents (Class 552/511)
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Publication number: 20130210787Abstract: 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: ApplicationFiled: February 6, 2013Publication date: August 15, 2013Applicant: BRISTOL-MYERS SQUIBB COMPANYInventor: Bristol-Myers Squibb Company
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Publication number: 20100286106Abstract: Treating and/or preventing prostate problems and/or metastases, by selectively occluding various groin vessels and tools for selective occluding of various groin veins, including, for example, the deferential vein. Optionally providing anti-androgen treatment after such occluding.Type: ApplicationFiled: July 13, 2008Publication date: November 11, 2010Inventors: Yigal Gat, Menachem Goren
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Publication number: 20100240630Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection.Type: ApplicationFiled: June 4, 2010Publication date: September 23, 2010Applicant: Myriad Pharmaceuticals, Inc..Inventors: Dange Vijay KUMAR, Kraig M. Yager, David A. Gerrish, Christophe Hoarau, Mark B. Anderson
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Publication number: 20090149429Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection.Type: ApplicationFiled: June 22, 2006Publication date: June 11, 2009Applicant: Myriad Genetics, IncorporatedInventors: Esther Arranz Plaza, Kraig M. Yager, David Allen Gerrish, Mark B. Anderson, In Chul Kim, Dange Vijay Kumar
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Publication number: 20090148542Abstract: The present invention relates to a composition comprising an extract of Tiarella polyphylla, and tiarellic acid isolated therefrom having anti-inflammatory, anti-allergic and anti-asthmatic activity. The extract of Tiarella polyphylla and the tiarellic acid isolated therefrom shows the inhibitory effect on the LTC4 release in vitro test and the suppressive effect on the IgE level and the cytokine (IL-4, IL-5 and IL-13) production, airway hyperresponsiveness, and leukocyte infiltration in OVA-induced asthmatic mice. Therefore, it can be used as the therapeutics or functional health food for treating and preventing inflammatory, allergic and asthmatic disease.Type: ApplicationFiled: July 18, 2006Publication date: June 11, 2009Applicant: Korea Research Institute of Bioscience and BiotechnologyInventors: Hyeong Kyu Lee, Sei Ryang Oh, Kyung Seop Ahn, Joong Ku Lee, Sang Ku Lee, Jung Hee Kim, Doo Young Kim, Gui Hua Quan, Ok Kyoung Kwon, Eun Ah Kim, Soon Ja Choi, Guang Hai Shen, Mi Jin Kim, Bo Young Park, Byung Sun Min, Gyoon Hee Han, Hea Young Park, Gun Cheol Kim, Joo Heon Kim, So Young Kim
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Publication number: 20090068257Abstract: 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: ApplicationFiled: September 4, 2008Publication date: March 12, 2009Inventors: Jean-Claude Leunis, Emmanuel Couche
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Publication number: 20090062243Abstract: The present invention comprises lupine-type triterpenoids that inhibit cell proliferations, in particular cancer and conditions associated with cancer. For example, associated malignancies include ovarian cancer, cervical cancer, breast cancer, colorectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases. Thus, the present invention also comprising pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit cancer and treat, prevent, or inhibit the foregoing diseases.Type: ApplicationFiled: July 10, 2008Publication date: March 5, 2009Applicant: ADVANCED LIFE SCIENCES, INC.Inventors: Ali Koohang, Aye Aye Mar, Erika Szotek, Ze-Qi Xu, David A. Eiznhamer, Michael T. Flavin
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Publication number: 20090042846Abstract: This invention relates to certain sugar esters of phytosterols of formula (I).Type: ApplicationFiled: September 15, 2008Publication date: February 12, 2009Applicant: BIODERM RESEARCHInventor: SHYAM K. GUPTA
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Publication number: 20090023698Abstract: The present invention provides a method for preparing a compound of formula (I), the method comprising contacting a compound of formula (II) with an effective amount of a compound of formula (III) or (IV). The present invention also provides a method for preparing a compound of formula (VI), the method comprising contacting a compound of formula (II) with an effective amount of one or more of 2,2-dimethylsuccinic acid, 2,2 dimethylbutanedioyl dichloride, 2,2-dimethylbutanedioyl dibromide, and 2,2 dimethylsuccinic anhydride. The present invention also provides a compound obtained from the method of the present invention.Type: ApplicationFiled: March 29, 2006Publication date: January 22, 2009Inventors: Pavel A. Krasutsky, Oksana Kolomitsyna
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Patent number: 7365221Abstract: Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have Formula I as described herein, or pharmaceutically acceptable salts thereof; wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl or ester thereof; R2 is hydrogen, halogen, hydroxyl or —OR3, R3 is C2-C20 substituted or unsubstituted carboxyacyl; and R4 is hydrogen or C(C6H5)3; wherein the dashed line represents an optional double bond between C20 and C29.Type: GrantFiled: June 18, 2004Date of Patent: April 29, 2008Assignees: Panacos Pharmaceuticals, Inc., The University of North Carolina at Chapel Hill, Niigata University of Pharmacy and Applied Life SciencesInventors: Graham P. Allaway, Carl T. Wild, Yoshiki Kashiwada, Kuo-Hsiung Lee
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Publication number: 20040204389Abstract: The present invention provides compounds of the general structure: 1Type: ApplicationFiled: April 14, 2003Publication date: October 14, 2004Inventors: Chin Ho Chen, Li Huang
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Publication number: 20040131629Abstract: Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have Formula I as described herein, or pharmaceutically acceptable salts thereof, wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl, R2 is hydrogen, chloro, bromo, or hydroxy, R4 is hydrogen or C(C6H5)3; wherein the dashed line represents an optional double bond between C20 and C29.Type: ApplicationFiled: September 26, 2003Publication date: July 8, 2004Applicants: Panacos Pharmaceuticals, Inc., The University of North Carolina at Chapel Hill, Niigata University of Pharmacy and Applied ScienceInventors: Graham P. Allaway, Carl T. Wild, Yoshiki Kashiwada, Kuo-Hsiung Lee
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Publication number: 20040072807Abstract: The invention is directed to methods of treating fungal and yeast infections using lupeol or solvates, hydrates, or clathrates thereof. The method also encompasses methods of treating fungal and yeast infections by administering to a mammal in need of such treatment a therapeutically effective amount of lupeol. Among the methods used include topical formulations for the improvement of skin appearance.Type: ApplicationFiled: May 7, 2003Publication date: April 15, 2004Inventors: David J. Gibson, Robert M. Carlson
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Publication number: 20040024230Abstract: The present invention relates to improved methods for synthesising cyproterone acetate (17&agr;-Acetoxy-6-chloro-1&agr;, 2&agr;-methylene-4,6-pregnadiene-3,20-dione) from solasodine.Type: ApplicationFiled: April 25, 2003Publication date: February 5, 2004Applicant: Boehringer Ingelheim International GmbHInventors: Aranya Manosroi, Jiradej Manosroi, Duang Buddhasukh, Pattana Sripalakit, Roland Maier, Rolf G. Werner
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Publication number: 20040001837Abstract: The present invention is directed to betulinol derivatives and betulinol-antibody conjugates having the formulae: 1Type: ApplicationFiled: June 3, 1998Publication date: January 1, 2004Inventors: ARKADIY L. BOMSHTEYN, PREMILA RATHNAM, BRIJ B. SAXENA
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Publication number: 20030153776Abstract: The invention relates to an improved process for obtaining pure crystalline betulin which is substantially free from betulinic acid, from an extract of birch bark.Type: ApplicationFiled: January 31, 2003Publication date: August 14, 2003Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Markus Sauter, Carsten Bender
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Publication number: 20030149286Abstract: The invention relates to an improved process for obtaining highly pure, crystalline betulinic acid from a methanolic extract of ground plane tree cortex and/or plane tree bark, as well as highly pure crystalline betulinic acid which is solvated with one equivalent of ethanol.Type: ApplicationFiled: January 31, 2003Publication date: August 7, 2003Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventor: Markus Sauter
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Publication number: 20030073858Abstract: The present invention provides a method for preparing betulin-3-acetate including alcoholyzing betulin 3,28-dibenzoate; a process for preparing betulin-3-acetate including: (1) acylating betulin to provide betulin 3,28-dibenzoate and (2) alcoholyzing betulin 3,28-dibenzoate to provide betulin-3-acetate; and a process for preparing betulinic acid including: (1) acylating betulin to provide betulin 3,28-dibenzoate; (2) alcoholyzing betulin 3,28-dibenzoate to provide betulin-3-acetate; (3) oxidizing betulin-3-acetate to provide betulinic aldehyde-3-acetate; (4) oxidizing betulinic aldehyde-3-acetate to provide betulinic acid-3-acetate; and (5) deprotecting betulinic acid-3-acetate to provide betulinic acid.Type: ApplicationFiled: July 11, 2002Publication date: April 17, 2003Inventors: Pavel A. Krasutsky, Robert M. Carlson, Vitaliy V. Nesterenko
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Publication number: 20030036540Abstract: The present invention is directed to betulinol derivatives and betulinol-antibody conjugates having the formulae: 1Type: ApplicationFiled: August 2, 2002Publication date: February 20, 2003Inventors: Arkadiy L. Bomshteyn, Premila Rathnam, Brij B. Saxena
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Publication number: 20020052352Abstract: A composition and method of preventing or inhibiting tumor growth and, more particularly, of treating a malignant tumor, using prodrugs of plant-derived compounds and derivatives is disclosed. In the method, a composition containing betulinic acid or a betulinic acid derivative is administered in a prodrug form to release betulinic acid or a betulinic acid derivative in vivo at the tumor site.Type: ApplicationFiled: August 15, 2001Publication date: May 2, 2002Inventors: John M. Pezzuto, Jerome W. Kosmeder, Ze-Qi Xu, Nian En Zhou, Miriam Elaine Goldsmith
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Publication number: 20020028960Abstract: The present invention provides a method for preparing betulin-3-acetate including alcoholyzing betulin 3,28-dibenzoate; a process for preparing betulin-3-acetate including: (1) acylating betulin to provide betulin 3,28-dibenzoate and (2) alcoholyzing betulin 3,28-dibenzoate to provide betulin-3-acetate; and a process for preparing betulinic acid including: (1) acylating betulin to provide betulin 3,28-dibenzoate; (2) alcoholyzing betulin 3,28-dibenzoate to provide betulin-3-acetate; (3) oxidizing betulin-3-acetate to provide betulinic aldehyde-3-acetate; (4) oxidizing betulinic aldehyde-3-acetate to provide betulinic acid-3-acetate; and (5) deprotecting betulinic acid-3-acetate to provide betulinic acid.Type: ApplicationFiled: June 29, 2001Publication date: March 7, 2002Applicant: Naturtek, LLC, Regents of the University of MinnesotaInventors: Pavel A. Krasutsky, Robert M. Carlson, Vitaliy V. Nesterenko
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Publication number: 20020016482Abstract: The present invention provides a method for preparing betulin-3-acetate including alcoholyzing betulin 3,28-dibenzoate; a process for preparing betulin-3-acetate including: (1) acylating betulin to provide betulin 3,28-dibenzoate and (2) alcoholyzing betulin 3,28-dibenzoate to provide betulin-3-acetate; and a process for preparing betulinic acid including: (1) acylating betulin to provide betulin 3,28-dibenzoate; (2) alcoholyzing betulin 3,28-dibenzoate to provide betulin-3-acetate; (3) oxidizing betulin-3-acetate to provide betulinic aldehyde-3-acetate; (4) oxidizing betulinic aldehyde-3-acetate to provide betulinic acid-3-acetate; and (5) deprotecting betulinic acid-3-acetate to provide betulinic acid.Type: ApplicationFiled: April 23, 2001Publication date: February 7, 2002Inventor: Pavel A. Krasutsky
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Patent number: 6180803Abstract: The invention relates to compounds of the formula: in which R1, R2, R3, R4, R5, R6, n and X are as defined in the specification, and to pharmaceutical compositions containing them. These compounds are excellent progestogens which are devoid of residual androgenic activity.Type: GrantFiled: November 5, 1998Date of Patent: January 30, 2001Assignee: Laboratoire TheramexInventors: Alain Piasco, Jean Lafay, R{acute over (e)}mi Delansorne, Jacques Paris, Jean-Claude Pascal
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Patent number: 5849724Abstract: A Chrysosporium strain No. CBS 123.95, mutants and derivatives thereof, and a method for preparing non-peptide compounds using said strain, are disclosed. Novel compounds of general formula (I), pharmaceutical compositions containing same, and the use of said compounds in anticancer treatments, are also disclosed.Type: GrantFiled: August 8, 1997Date of Patent: December 15, 1998Assignee: Rhone-Poulenc Rorer S.A.Inventors: Jean Leboul, Didier Van der Pyl, Jean-Jacques Debernard
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Patent number: 5703066Abstract: In this invention, the new etheno- and ethano-19,11-bridged 4-estrenes of general formula I ##STR1## are described, in whichW, R.sup.1, R.sup.2, R.sup.6a, R.sup.6b, R.sup.7, R.sup.14, R.sup.15, R.sup.16, R.sup.11, R.sup.11' and R.sup.19 have the meaning indicated in the description, as well as a process for their production.The new compounds have strong progestational activity and are suitable for the production of pharmaceutical agents.Type: GrantFiled: June 7, 1995Date of Patent: December 30, 1997Assignee: Schering AktiengesellschaftInventors: Eckhard Ottow, Wolfgang Schwede, Wolfgang Halfbrodt, Karl-Heinrich Fritzemeier, Rolf Krattenmacher
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Patent number: 5439901Abstract: The present invention relates to the compound cyproterone thiopivalate (CTP) and compositions comprising CTP. The present invention further relates to methods of treating acne and/or sebaceous gland activity comprising topical application of CTP. The present invention additionally relates to methods of regulating hair growth comprising application of compositions comprising CTP.Type: GrantFiled: July 23, 1993Date of Patent: August 8, 1995Assignee: The Procter & Gamble CompanyInventors: Richard J. Schwen, Mark R. Sine, Raphael Warren
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Patent number: 5244886Abstract: New 11.beta.-phenyl-14.beta.H-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N.about.OH, and M and N are either jointly a second compound or L is a hydrogen atom and M is an .alpha.-permanent hydroxy group and either A and B together are a second compound and D is a hydrogen atom, where R.sup.1 is a five or six-part heteroalkyl residue or a cycloalkyl, cycloalkenyl or aryl residue or A is a hydrogen atom and B and D together are a methylene bridge, where R.sup.1 besides the aforementioned residues may be a possibly substituted hydrocarbon residue with up to 10 C atoms, a possibly substituted amino group, a hydroxy or C.sub.1-8 alkoxy, mercapto or thioalkyl group, R.sup.2 is a methyl or ethyl residue, and R.sup.3 /R.sup.4 represents the usual combination of substituents on the C17 atom in steroid chemistry, having antigestagenic and other properties.Type: GrantFiled: March 20, 1991Date of Patent: September 14, 1993Assignee: Schering AktiengesellschaftInventors: Stefan Scholz, Gunter Neef, Eckhard Ottow, Walter Elger, Sybille Beier, Krzysztof Chwalisz
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Patent number: 4988684Abstract: A compound of the formula ##STR1## wherein R is selected from the group consisting of alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.1 is alkyl of 1 to 6 carbon atoms unsubstituted or substituted with at least one member of the group consisting of alkoxy and alkylthio of 1 to 4 carbon atoms, --NO.sub.2, --CN and halogen, X and Y together are .dbd.O or Y is hydrogen and X is --OH, etherified --OH or esterified --OH, the dotted lines in the 1(2), 6(7) and 9(11) positions indicate a possible double bond with the proviso that R.sub.1 is alkyl of 1 to 6 carbon atoms when X and Y are .dbd.O and there is a double bond in at least one of the 1(2), 6(7) and 9(11) positions having aromatase inhibiting activity.Type: GrantFiled: December 21, 1989Date of Patent: January 29, 1991Assignee: Roussel UclafInventors: Jean-Francois Gourvest, Dominique Lesuisse, Daniel Philibert, Jean P. Vevert