Polycyclo Ring System Patents (Class 514/680)
  • Publication number: 20090312437
    Abstract: Compositions derived from Rheum palmatum are provided. Also provided are methods of using said extracts to induce apoptosis in specific cells, especially in a human.
    Type: Application
    Filed: June 5, 2009
    Publication date: December 17, 2009
    Inventor: Isaac Cohen
  • Publication number: 20090312413
    Abstract: A composition comprising tanshinone compounds selected from the group consisting of miltirone, 1,2-didehydromiltirone, tanshinone IIA, tanshinone I and dihydrotanshinone I isolated from Salviae miltiorrhizae Bunge showing potent inhibiting effect on the aggregation and toxicity of beta-amyloid and recovering activity of memory learning disorder confirmed by Y maze study and Passive Avoidance study. Therefore it can be used as the therapeutics or health food for treating and preventing cognitive function disorder with safe.
    Type: Application
    Filed: October 4, 2006
    Publication date: December 17, 2009
    Applicants: DIGITAL BIOTECH CO., LTD., ILSUNG PHARMACEUTICALS CO., LTD.
    Inventors: Sang Seob Song, Young Ho Kim, Jong Moon Kim, Hee Kim, Hee Jin Ha, Hoon Yi Jung
  • Publication number: 20090149551
    Abstract: 4b,5,6,7,8,8a-cis-hexahydro-2-hydroxy-4b,8,8a-trimethylphenanthren-9,10-dione (OHCT) is a fully oxidized compound based on the 2-hydroxy-cis-terpenone (HCT). Because OHCT is fully oxidized, it is more stable and less likely to damage cells or cell constituents such as DNA. OHCT has antimalarial activity, noncompetitive inhibitory activity against carcinogenic conversion of aflotoxin B1 (AFB1) to exo-AFB1-epoxide thus inihibiting AFB1 induced cellular toxicity, and inhibitory activity against TCDD induced cellular toxicity.
    Type: Application
    Filed: August 22, 2008
    Publication date: June 11, 2009
    Inventors: Qibing Zhou, Ghislaine Mayer, Lin Zhang, Jennifer K. Stewart
  • Publication number: 20090137687
    Abstract: This invention relates to novel tricyclic quinone and catechol compositions, compositions containing prodrugs of tricyclic quinone and catechol compositions, and methods of use for the treatment of solid tumor cancers and other vascular proliferative disorders. In certain aspects, the compositions of the invention are capable of generating both a vascular targeting effect and tumor cell cytotoxicity (e.g., by oxidative stress) in order to achieve an enhanced anti-tumor response in a patient.
    Type: Application
    Filed: June 19, 2008
    Publication date: May 28, 2009
    Applicants: OXiGENE, Inc., Baylor University
    Inventors: David Chaplin, Kevin G. Pinney, Peter Wardman, Vani P. Mocharla, Lisa K. Folkes
  • Publication number: 20090117040
    Abstract: The present invention relates to pharmaceutical and diagnostic compositions as well as to the use of the active substances contained therein for preparing a pharmaceutical or a diagnostic composition for the treatment or diagnosis of neurodegenerative disorders or amyloid diseases.
    Type: Application
    Filed: February 11, 2005
    Publication date: May 7, 2009
    Applicant: Max-Delbrug-Centrum Fur Molekulare Medizin
    Inventors: Erich Wanker, Sabine Engemann, Susanne Rautenberg, Annett Boeddrich, Phoebe Markovic, Dagmar Ehrnhofer, Martin Herbst, Jacqueline Walther
  • Publication number: 20090110731
    Abstract: Particles are provided for use in restorative procedures to treat and/or retard alopecia The particles include poly[bis(trifluoroethoxy)phosphazene] and/or a derivatives thereof which may be present throughout the particles or within an outer coating of the particles. The particles may also include a core having a hydrogel formed from an acrylic-based polymer. Such particles may be provided to a user in various colors or with customized coloration to match desired scalp colors. Moreover, such particles may be loaded to provide localized treatment with an active component agent directed at restoration of normal function and hair production within the hair follicle.
    Type: Application
    Filed: October 30, 2007
    Publication date: April 30, 2009
    Applicant: CELONOVA BIOSCIENCES, INC.
    Inventors: Olaf Fritz, Ulf Fritz, Ronald Wojcik, Ralph E. Gaskins, JR.
  • Publication number: 20090099251
    Abstract: The present invention refers to tricyclic diterpenes and their derivatives of the formulae (I) and (II), wherein R1 is hydrogen or C1-6-alkyl; R2 is hydroxy, C3-5-acyloxy, hydroxymethyl, 1,3-dihydroxypropyl or C1-6-alkyl; R3 and R4 independently from each other are hydrogen, hydroxy, hydroxymethyl, C1-5-acyloxy or C1-6-alkoxy; R5 is C1-6-alkyl, hydroxymethyl carboxy or methoxycarbonyl; R9 is hydrogen, hydroxymethyl, methoxy, oxo or C1-5-acyloxy; R10 is hydrogen, or R5 and R9 taken together are —CH2—O— or —O—CH2—; or R5 and R10 taken together are —CO—O—, —O—CO—, —CH2—O— or —O—CH2—; R6 is hydrogen, or R5 and R6 together form a bond; R7 and R8 independently from each other are C1-6-alkyl, carboxy, x-hydroxy-Cx-alkyl (with x being an integer from 1 to 6), or C1-6-alkoxycarbonyl with the proviso that at least one of R7 and R8 is C1-6-alkyl; R11 and R12 are both hydrogen or R11 and R12 together are oxo, with the further proviso for formula (I) that if R2 is hydroxy R1 is C1-6-alkyl, for use as medicaments for the t
    Type: Application
    Filed: November 22, 2007
    Publication date: April 16, 2009
    Inventors: Antoine De Saizieu, Ann Fowler, Regina Goralczyk, Claus Kilpert, Goede Schueler, Christof Wehrli
  • Publication number: 20090082470
    Abstract: STAT3 inhibiting molecules and composition prevent intraoccular neovascularization and inflammation. STA-21-related compounds, for example CLT-005, are shown to prevent dimerization of STAT3, thereby inhibiting STAT3 activity. Inhibition of activity is shown to reduce intraoccular inflammation and neovascularization, symptoms of eye-related diseases such as age-related macular degeneration. Inhibition of STAT3 prevents STAT3 from transcriptionally activating downstream gene targets that are known to be associated with retinal inflammation and neovascularization and such disorders as age-related macular degeneration.
    Type: Application
    Filed: September 24, 2008
    Publication date: March 26, 2009
    Inventor: Rafal Farjo
  • Publication number: 20090068143
    Abstract: The present invention relates to orally effective ligands of the peripheral cannabinoid receptor CB2, especially (+)-?-pinene derivatives, and to pharmaceutical compositions thereof, which are useful for prevention, alleviation or treatment of autoimmune neurodegenerative disorders, in particular multiple sclerosis and associated symptoms. Methods of the invention are useful when the active ingredient is administered alone or in combination with existing therapeutic modalities. The compositions are administered by oral route.
    Type: Application
    Filed: February 24, 2005
    Publication date: March 12, 2009
    Applicant: PHARMOS CORPORATION
    Inventors: Avihai Yacovan, Avi Bar-Joseph, Sigal Meilin, Shimon Amselem
  • Patent number: 7488493
    Abstract: A performance aid for increasing the effectiveness of a bioactive agent, and a composition including both the performance and the bioactive agent. The performance aid increases the effectiveness of the bioactive agent by providing a composition that adheres well to a surface but also increases transferability of the bioactive agent to a target animal that contacts the treated surface.
    Type: Grant
    Filed: April 23, 2004
    Date of Patent: February 10, 2009
    Assignee: Arkion Life Sciences, LLC
    Inventors: Kenneth E. Ballinger, Jr., Michele Santer
  • Publication number: 20080319067
    Abstract: The compounds of formula I in which R1, R2, R3, R31, R4, R5, R6 and R7 have the meanings as indicated in the description, are novel effective PDE4 inhibitors.
    Type: Application
    Filed: December 17, 2007
    Publication date: December 25, 2008
    Inventors: Ulrich Kautz, Beate Schmidt
  • Publication number: 20080306164
    Abstract: The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17?-hydroxy steroid dehydro-genase type 1.
    Type: Application
    Filed: August 15, 2008
    Publication date: December 11, 2008
    Inventors: Alexander Hillisch, Olaf Peters, Christian Gege, Wilko Regenhardt, Gabriele Moeller, Dominga Deluca, Jerzy Adamski, Walter Elger, Birgitt Schneider
  • Patent number: 7435757
    Abstract: The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17?-hydroxy steroid dehydro-genase type 1.
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: October 14, 2008
    Assignee: Schering AG
    Inventors: Alexander Hillisch, Olaf Peters, Christian Gege, Wilko Regenhardt, Gabriele Moeller, Dominga Deluca, Jerzy Adamski, Walter Elger, Birgitt Schneider
  • Patent number: 7432284
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Pagets disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
    Type: Grant
    Filed: September 15, 2003
    Date of Patent: October 7, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Dann LeRoy Parker, Robert R. Wilkening, Dongfang Meng, Ronald W. Ratcliffe
  • Patent number: 7432303
    Abstract: The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, including angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.
    Type: Grant
    Filed: March 8, 2005
    Date of Patent: October 7, 2008
    Assignees: James and Emory University
    Inventors: J. Phillip Bowen, Thomas Philip Robinson, Tedman Ehlers, David Goldsmith, Jack Arbiser
  • Publication number: 20080226759
    Abstract: A system for treating addictions includes genetic testing to determine the presence of allelic variants of genes shown to be associated with impulsive/addictive behaviors and a tailored rehabilitation regimen of specific physical exercise, special diet and particular dietary supplements to optimize the way mood elevation is achieved in the patient. The system further includes individual and group counseling and initial oxygen therapy. The genetic testing assesses the presence of gene polymorphism in at least one of D2 dopamine receptor gene (DRD2), dopamine transporter gene (DAT1), dopamine beta-hydroxylase gene (DBH) and serotonin transporter (SERT) gene. The dietary supplements are tailored to stimulate production of neuromediators or neurotransmitters, depending upon the polymorphism determined. The exercises include static and dynamic routines also tailored to the results of the genetic testing.
    Type: Application
    Filed: March 15, 2007
    Publication date: September 18, 2008
    Inventor: Yakov Marshak
  • Publication number: 20080201871
    Abstract: Quaternary ammonium salts were incorporated into anthraquinone dyes via a stable linkage. The structure of the antimicrobial colorants were characterized by Fourier Transform Infrared (FTIR), Nuclear Magnetic Resonance (NMR) and UV-vis spectrometry. The dyes demonstrated excellent antimicrobial ability against both gram-negative and gram-positive bacteria in aqueous solution, as indicated by very low minimum inhibitory concentration (MIC). The colorants showed excellent stability in water under light, continuous heating as well as acidic and alkaline conditions.
    Type: Application
    Filed: October 10, 2007
    Publication date: August 28, 2008
    Applicant: The Regents of the University of California
    Inventors: Gang Sun, Junshu Liu
  • Publication number: 20080161372
    Abstract: This invention relates to the treatment of hypertension, cardiac dysfunction or stroke by the administration of an estrogen receptor beta (ER&bgr;) selective agonist either as a single agent, or in combination with other agents.
    Type: Application
    Filed: April 1, 2005
    Publication date: July 3, 2008
    Inventor: Susan P. Rohrer
  • Publication number: 20080102089
    Abstract: Various medical conditions previously treated by injection or surgery are effectively treated by a topical application of a composition of urea and a chemotherapeutic agent. Such agents include sclerosing agents, varodilators and botulinum toxin. Conditions as diverse as spider veins, erectile dysfunction and facial wrinkles can be effectively treated with the compositions.
    Type: Application
    Filed: October 30, 2006
    Publication date: May 1, 2008
    Inventor: John V. Cappello
  • Publication number: 20080027141
    Abstract: Disclosed herein are 1,3-dihydroxyl-9,10-anthraquinone and 3-[(3-amino)-propoxy]-9,10-anthraquinone derivatives, in particular 1,3-dihydroxy-4-prenyl-9,10-anthraquinone and 3-[3-(4-methylpiperazinyl)-propoxy]-9,10-anthraquinone, which are found to have inhibitory activities against several types of human tumor/cancer cells and thus can be used in the manufacture of pharmaceutical compositions for use in the treatment of tumors/cancers.
    Type: Application
    Filed: July 5, 2006
    Publication date: January 31, 2008
    Applicant: Kaohsiung Medical University
    Inventors: Chun-Nan Lin, Shen-Jeu Won, Chi-Hung Teng
  • Patent number: 7265248
    Abstract: A colchicine derivative and a method of using a colchicine derivative as a pharmacological agent in the treatment of malaria are provided.
    Type: Grant
    Filed: April 28, 2006
    Date of Patent: September 4, 2007
    Assignee: Technology Innovations, LLC
    Inventors: Jack A. Tuszynski, Stephen H. Curry
  • Patent number: 7230139
    Abstract: The present invention relates to Diterpenoid Compounds, compositions comprising an effective amount of a Diterpenoid Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering an effective amount of a Diterpenoid Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, or for inducing apoptosis in a cancer or neoplastic cell. The compounds, compositions, and methods of the invention are further useful for treating or preventing a fungal infection. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a fungus.
    Type: Grant
    Filed: June 10, 2004
    Date of Patent: June 12, 2007
    Assignee: Gemin X Biotechnologies
    Inventors: Jean-Francois Lavallee, Terrence W. Doyle, Elise Rioux, Laurent Belec, Daniel Rabouin, Xavier Billot, Samuel Fortin
  • Patent number: 7217844
    Abstract: The present invention relates to Diterpenoid Compounds, compositions comprising an effective amount of a Diterpenoid Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering an effective amount of a Diterpenoid Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, or for inducing apoptosis in a cancer or neoplastic cell. The compounds, compositions, and methods of the invention are further useful for treating or preventing a fungal infection. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a fungus.
    Type: Grant
    Filed: December 1, 2003
    Date of Patent: May 15, 2007
    Assignee: Gemin X Biotechnologies
    Inventors: Pierre Beauparlant, Giorgio Attardo, Zhiying Zhang, Angela M. Stafford, Rosa Ubillas, James B. McAlpine, Jean-Francois Lavallee, Samuel Fortin, Sasmita Tripathy
  • Patent number: 7157477
    Abstract: The invention involves a methods and compositions for use in photodynamic therapy. Novel perylenequinone derivatives, conjugates comprising perylenequinone derivatives and a binding agent, and methods of treatment using these compositions are disclosed. The present invention relates to the field of photosensitizers possessing photodynamic activities. They possess high photodynamic activities and low dark toxicities, which makes them as more potent photodynamic agents than HPD against cancer and AIDS virus.
    Type: Grant
    Filed: October 24, 2001
    Date of Patent: January 2, 2007
    Assignees: Altachem Pharma Ltd., Institute of Photographic Chemistry Academia Sinica
    Inventors: Manhua Zhang, Shangjie Xu, Tao Wu, Shen Chen, Tao Shen
  • Patent number: 7151196
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, age-related mild cognitive impairment, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, irritable bowel syndrome, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.
    Type: Grant
    Filed: October 28, 2005
    Date of Patent: December 19, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Robert R. Wilkening, Amy Fried
  • Patent number: 7122518
    Abstract: A method is provided for preventing or reducing the adverse effects of photodynamic therapy such as collateral damage by regulating the localized phototoxicity of an effector photosensitizer molecule. During photodynamic therapy, the activity of the effector photosensitizer molecule in neighboring tissues of the tissue targeted for destruction is quenched by a quenching photosensitizer molecule.
    Type: Grant
    Filed: November 25, 2003
    Date of Patent: October 17, 2006
    Assignee: New York University
    Inventor: Gad Lavie
  • Patent number: 7101917
    Abstract: Methods of utilizing compounds of general formulas I and II as modulators and affinity labels of the MPTP complex are elucidated. Furthermore, methods for modulating the activity of the MPTP complex, methods for determining the presence of a component of the MPTP complex, and methods for identifying an active agent that modulates the activity of the MPTP complex, specifically methods for identifying an active agent that modulates the activity of the MPTP complex by interacting with the VDAC1 component are identified. Moreover, novel compounds of general formulas I and II are disclosed.
    Type: Grant
    Filed: April 5, 2004
    Date of Patent: September 5, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andrea Cesura, Emmanuel Pinard
  • Patent number: 7087599
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
    Type: Grant
    Filed: February 14, 2001
    Date of Patent: August 8, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Dann LeRoy Parker, Jr., Ronald W. Ratcliffe, Robert R. Wilkening, Kenneth J. Wildonger
  • Patent number: 7060686
    Abstract: Methods for treating, preventing, or inhibiting diseases and disorders associated with inflammation, cell-proliferation, and pain comprising the administration of a compound having the structural formula wherein R1 is a hydrogen, alkyl, aryl, hydroxyalkyl, cycloalkyl, cycloalkenyl, carboxylic acid, alkylamino or amide group having from 2 to 20 carbon atoms, R2, R3, and R4 are each independently hydrogen or an acyl residue having from 1 to 6 carbon atoms, R5 is hydrogen, CH3, or CH2OH, and R6 is an organo group such as a hydrocarbon having from 1 to 10 carbon atoms are disclosed. Other seco-pseudopterosins and compounds related to pseudopterosins are disclosed.
    Type: Grant
    Filed: August 2, 2004
    Date of Patent: June 13, 2006
    Assignees: The Regents of the University of California, Florida Atlantic University Board of Trustees
    Inventors: Robert S. Jacobs, Russell G. Kerr
  • Patent number: 6958159
    Abstract: The present invention relates to an improved pharmaceutical composition useful for the topical treatment of burns, cuts, wounds, abrasions and the like, and to methods of treatment of injured body surfaces such as skin.
    Type: Grant
    Filed: March 26, 2001
    Date of Patent: October 25, 2005
    Assignee: Chiltern Pharmaceuticals, Pty Ltd.
    Inventor: Robert Alan Smith
  • Patent number: 6949250
    Abstract: We have now discovered that certain 9,10-anthraquinone derivatives we developed possess potent activity against O. perornata while possessing a sufficiently high level of solubility in water to make their activity against O. perornata viable. These compounds possess a high level of activity against O. perornata yet are relatively non-toxic to green algae and fishes. The compounds also possess a relatively short half-life. The compounds represent a new means to providing compounds possessing a high degree of selective activity against blue-green algae while being physiologically tolerated by catfish and green algae. The compounds provide a means for controlling blue-green algae in managed bodies of water that are destined for public use or consumption.
    Type: Grant
    Filed: December 16, 2002
    Date of Patent: September 27, 2005
    Assignees: The United States of America as represented by the Secretary of Agriculture, The University of Mississippi
    Inventors: Kevin K. Schrader, N. P. Dhammika Nanayakkara
  • Patent number: 6949557
    Abstract: The invention relates to the use of novel anthracene based compounds for the inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing such compounds. The invention relates more specifically to the use of hydroanthracene based compounds for the inhibition and/or prevention of cancer of the colon, pancreas, prostate, lung, larynx, ovary, breast, glioblastoma, oral cavity, endothelial cells and leukemias. The agents of the invention form a distinct class, distinct from the anthracene, anthrone or anthraquinone derivatives.
    Type: Grant
    Filed: April 29, 2003
    Date of Patent: September 27, 2005
    Assignee: Dabur Research Foundation
    Inventors: Asish Kumar Banerjee, Venkatachalam Sesha Giri, Rama Mukherjee, Kamal K. Kapoor, Gautam Desiraju, Manu Jaggi, Anu T. Singh, Sankar Kumar Dutta, Kalapatapu V. V. M. Sairam
  • Patent number: 6936571
    Abstract: The present invention provides an agricultural fungicidal composition containing active compounds selected from perylenequinonoid derivatives or salts thereof. The invention also relates the application of the composition against fungal plant infections.
    Type: Grant
    Filed: October 21, 2002
    Date of Patent: August 30, 2005
    Inventors: Hongyu Zhnag, Weizhong Liu
  • Patent number: 6906059
    Abstract: The use of benzazepin-N-acetic acid derivatives which contain an oxo group in the a position to the nitrogen atom and are substituted in the 3 position by a 1-(carboxyalkyl)-cyclopentyl-carbonyl-amino radical, and of their salts and biolabile esters, for the prophylaxis and/or treatment of heart damage caused by cardiotoxic doses of medicaments or chemicals, in larger mammals and in particular humans. The invention is particularly applicable to the prophylaxis and/or treatment of heart damage, in particular to the myocardium, which may occur during cytostatic chemotherapy. The invention also includes the use of the afore-mentioned benzazepin-N-acetic acid derivatives for adjuvant treatment in therapies in which medicaments having oxidative-toxic side-effects are used, and the preparation of medicaments suitable for this prophylaxis and/or treatment or adjuvant treatment.
    Type: Grant
    Filed: January 14, 2002
    Date of Patent: June 14, 2005
    Assignee: Solvay Pharmaceuticals
    Inventors: Zsuzsanna Lonovics, Julius Gy. Papp, Dirk Thormaehlen, Harald Waldeck, Zsuzsanna Rozsa
  • Patent number: 6903238
    Abstract: This invention provides estrogen receptor modulators of formula I, having the structure R1, R2, and R3 are as defined in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 11, 2002
    Date of Patent: June 7, 2005
    Assignee: Wyeth
    Inventors: Robert E. McDevitt, Folake O. Adebi, Heather A. Harris, James C. Keith, Jr., Leo M. Albert
  • Patent number: 6894073
    Abstract: The disclosure concerns novel use of diterpene compound as a therapeutic agent of inlfammation, immune disease or cancer. More particularly, the present invention relates to novel use of diterpene compound that include kamebanin, kamebacetal A, kamebakaurin, and exisanin A, which would be effective for the treatment inflammation, immune disease or cancer by inhibiting the production of nitric oxide, prostaglandin, and TNF-a1 through the suppression of NF-k B activity.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: May 17, 2005
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Jung-Joon Lee, Jeong-Hyung Lee, Hang-Sub Kim, Young-Soo Hong, Bang-Yeon Hwang
  • Patent number: 6867235
    Abstract: Hypericin, helianthrone and derivatives thereof of general formula (I) wherein the dotted line between positions 11 and 12 represent an optional C11-C12 bond; R is independently selected from the group consisting of hydroxy, C1-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; R? is independently selected from the group consisting of hydroxy and C1-C10 alkoxy; R? is independently selected from the group consisting of hydrogen, hydroxy, C1-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; and R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen, hydroxy, chloro, bromo, C1-C10 alkyl, C1-C10 alkoxy, and C1-C10 alkoxycarbonyl, provided that R? is not hydrogen when there is a C11-C12 bond, are useful as inhibitors of angiogenesis and can be used to prevent formation of metastases and restenosis and for the treatment of angiogenesis-associated ophthalmologic disorders.
    Type: Grant
    Filed: July 30, 2002
    Date of Patent: March 15, 2005
    Assignees: Yeda Research and Development Co. Ltd., New York University
    Inventors: Yehuda Mazur, Gad Lavie
  • Publication number: 20040248864
    Abstract: An anthroquinone such as diacerein is useful for the treatment of renal conditions and conditions (such as SLE) which lead to renal damage.
    Type: Application
    Filed: July 30, 2004
    Publication date: December 9, 2004
    Inventors: Robin Mark Bannister, Alan Rothaul, Nicola Cooper
  • Publication number: 20040235783
    Abstract: The present invention relates to a pharmaceutical composition comprising at least one active compound having cytostatic activity, at least one biological electron acceptor and customary pharmaceutical additives, and to its use for the treatment of tumor diseases, in particular for the treatment of cancer.
    Type: Application
    Filed: June 29, 2004
    Publication date: November 25, 2004
    Inventors: Miklos Ghyczy, Jorg Hager, Armin Wendel
  • Publication number: 20040224926
    Abstract: A method for inhibiting or blocking molecular generating and/or inducing functions of molecules using an inhibitory or blocking agent of the formula: 1
    Type: Application
    Filed: November 24, 2003
    Publication date: November 11, 2004
    Inventors: Shozo Koyama, Yoshihiro Yamaguchi
  • Publication number: 20040220257
    Abstract: Methods of utilizing compounds of general formulas I and II as modulators and affinity labels of the MPTP complex are elucidated. Furthermore, methods for modulating the activity of the MPTP complex, methods for determining the presence of a component of the MPTP complex, and methods for identifying an active agent that modulates the activity of the MPTP complex, specifically methods for identifying an active agent that modulates the activity of the MPTP complex by interacting with the VDAC1 component are identified. Moreover, novel compounds of general formulas I and II are disclosed.
    Type: Application
    Filed: April 5, 2004
    Publication date: November 4, 2004
    Inventors: Andrea Cesura, Emmanuel Pinard
  • Patent number: 6812255
    Abstract: The invention relates to the use of anti-cancer drug of a natural compound of vegetal origin, known as aloe-emodin (AE). Indeed, said compound has proved to have a specific biological activity of inhibition on the growth of neuroectodermal tumors, without evident toxic effects. The compound, according to the present invention, has also proved to be cell-specific and it does not show any inhibition on the growth of other cell types such as, for instance, fibroblasts. This pharmacological profile, i.e., tumor-targeting and absence of toxicity, makes said compound particularly advantageous in the treatment of neuroectodermal tumors. Pharmaceutical compositions containing said pharmacological agent can therefore be usefully used in the treatment of the foresaid pathologies.
    Type: Grant
    Filed: November 27, 2002
    Date of Patent: November 2, 2004
    Assignee: Universita Degli Studi Di Padova
    Inventors: Giorgio Palu′, Modesto Carli, Teresa Pecere
  • Publication number: 20040198827
    Abstract: The present invention relates to the use of rhein or diacerhein compounds to treat and prevent vascular diseases that cause obstruction of the vascular system such as blood vessel restenosis and atherosclerosis.
    Type: Application
    Filed: April 27, 2004
    Publication date: October 7, 2004
    Applicant: Transition Therapeutics Inc., a Canada corporation
    Inventors: Tony Cruz, Aleksandra Pastrak
  • Patent number: 6790463
    Abstract: The use of a pharmaceutical formulation in treating coronary arteriosclerosis and a two-component pharmaceutical formulation. The pharmaceutical formulation contains peroxidic species or reaction products resulting from oxidation of an alkene, such as geraniol, by an oxygen-containing oxidizing agent, such as ozone; a penetrating solvent, such as dimithyl sulfoxide; a dye containing a chelated metal, such as hematoporphyrin; and an aromatic redox compound, such as benzoquinone.
    Type: Grant
    Filed: March 30, 2001
    Date of Patent: September 14, 2004
    Inventors: Robert F. Hofmann, Robert H. Carpenter
  • Patent number: 6777447
    Abstract: Benzylidene cyclohexanone, cyclopentanone and acteone derivatives and therapeutic methods of using same are disclosed. The compounds are non-toxic and exhibit potent anti-inflammatory, antibacterial and antioxidation activity. Also, certain compounds of the invention inhibit glutathione S-transferase (“GST”), but do not irritate the gastrointestinal tract. Pharmaceutical compositions containing the compounds of the invention and pharmaceutically acceptable carriers are also disclosed.
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: August 17, 2004
    Inventors: Mochammad Samhoedi Reksohadiprodjo, Henk Timmerman, Sardjiman Dummy, Supardjan Amir Margono, Sudibyo Martono, Sugiyanto Dummy, Lukman Rahman Hakim, Nurlaila Dummy, Arief Rahman Hakim, Ika Puspitasari, Arief Nurrochmad, Purwantiningsih Dummy, Oetari Dummy, Tedjo Yuwono
  • Patent number: 6773727
    Abstract: Low concentrations of gossypol and related phyllophage toxins from cotton improve the effectiveness of insecticidal agents against social insects, including cockroaches, and particularly termites and ants. Levels of gossypol and other cotton phyllophage toxins which are sufficiently low as to be non-biocidal to social insects alone, will significantly increase the control efficacy of other insecticidal agents. Consequently, use of these low levels of these cotton phyllophage toxins allows the levels of insecticidal agents necessary for effectively controlling the insects to be significantly reduced relative to applications without cotton phyllophage toxins. Furthermore, insecticidal agents which are normally ineffective for control of social insects when used alone, may be effective when used in conjunction with the cotton phyllophage toxins.
    Type: Grant
    Filed: August 13, 2001
    Date of Patent: August 10, 2004
    Assignee: The United States of America as represented by the Secretary of Agriculture
    Inventors: Maria G. Rojas, Juan A. Morales-Ramos, Peter J. Wan
  • Publication number: 20040152645
    Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo.
    Type: Application
    Filed: January 20, 2004
    Publication date: August 5, 2004
    Applicants: Board of Trustees of Michigan State University, The Regents of the University of California
    Inventors: Robert H. Cichewicz, Muraleedharan G. Nair, James H. McKerrow
  • Publication number: 20040137088
    Abstract: The invention relates to an improved and stable (i.e. colour-stable and, optionally, stable with regard to its hyperforin content) extract from the overground parts of Hypericum perforatum L., to a method for the preparation thereof, and to pharmaceutical preparations and topical medicaments that contain this extract; in particular, gels for treating skin and mucous membrane irritations and disorders such as acne, atopic dermatitis, neuro-dermatitis, psoriasis, stomatitis, herpes zoster, herpes labialis (lip herpes), warts, varicella (chicken-pox), sores, burns and other bacterial and viral skin and mucous membrane infections and skin disorders that are accompanied by cell proliferation and inflammation.
    Type: Application
    Filed: February 23, 2004
    Publication date: July 15, 2004
    Inventors: Egon Koch, Clemens Erdelmeier, Joachim Herrmann
  • Publication number: 20040121968
    Abstract: A method of inhibiting angiogenesis in a mammal is disclosed, which employs a pharmaceutically acceptable composition containing a selective inhibitor of protein kinase CK2 (also known as casein kinase II) enzymatic activity, such as emodin, aloe-emodin, 5,6-dichloro-1-&bgr;-D-ribofuranosylbenzimidazole (DRB), and 4,5,6,7-tetrabromobenzotriazole (TBB). Also disclosed is a use of a selective inhibitor of protein kinase CK2 enzymatic activity in the manufacture of a medicament for inhibiting angiogenesis. An in vitro method of screening a potential antiangiogenic agent is also disclosed. A kit for the treatment of a disease by inhibiting angiogenesis is disclosed that contains the pharmaceutically acceptable composition containing a selective inhibitor of protein kinase CK2 enzymatic activity.
    Type: Application
    Filed: December 23, 2002
    Publication date: June 24, 2004
    Inventors: Alexander Ljubimov, Raquel Castellon, Maria Grant
  • Patent number: RE39199
    Abstract: A psoriasis treatment composition derived from the plant Asphodelus Microcarpus includes 3-methylanthralin, chrysophanol, aloe-emodin, aloe-emodin monoacetate, and/or derivatives thereof. The composition is prepared by extracting a liquid from the Asphodelus Microcarpus root and mixing the liquid with acetic acid. A method of treatment includes applying the composition to an affected area of skin at a frequency sufficient to effect an alleviation of symptoms, typically once per day for 14-56 days.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: July 18, 2006
    Inventors: Naseba Moady, Marzook Moady