Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/100)
  • Publication number: 20080221070
    Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion. The Bone Active Portion is derived from an estrogenic agent. Compounds can also include a Blocking Group (RP) that reduces or eliminates the estrogenic activity of the Bone Active Portion.
    Type: Application
    Filed: March 6, 2008
    Publication date: September 11, 2008
    Inventors: William M. Pierce, K. Grant Taylor, Leonard C. Waite
  • Patent number: 7419657
    Abstract: The present invention relates to the identification of lipid oxidizing abzymes as a key pathogenic factor in atherosclerotic disorders. Methods and means for the reduction of abzyme mediated lipid oxidation in the vascular system are provided as therapeutic approaches for the treatment of atherosclerotic disorders. Methods are provide for determining the efficacy of treatment.
    Type: Grant
    Filed: August 22, 2002
    Date of Patent: September 2, 2008
    Assignee: Cambridge Theranostics Ltd.
    Inventor: Ivan Petyaev
  • Patent number: 7417156
    Abstract: In only two steps and in 65% overall yield, natural trioxane artemisinin (I) was converted on gram scale into C-10-carba trioxane dimer (3). This new, very stable dimer was then transformed easily in one additional step into four different dimers (4-7). Alcohol and diol dimers (4 and 5) and ketone dimer (7) are 10 times more antimalarially potent in vitro than artemisinin (I), and alcohol and diol dimers (4 and 5) are strongly inhibitory but not cytotoxic toward several human cancer cell lines. Water-soluble carboxylic acid derivatives (8a-10c and 12) were easily prepared from dimers (4-6); they are thermally stable even at 60° C. for 24 hours, are more orally efficacious as antimalarials than either artelinic acid or sodium artesunate, and have potent and selective anticancer activities.
    Type: Grant
    Filed: September 26, 2003
    Date of Patent: August 26, 2008
    Assignee: Johns Hopkins University
    Inventors: Gary H. Posner, Theresa A. Shapiro, Surojit Sur, Tanzina Labonte, Kristina Borstnik, Ik-Hyeon Paik, Andrew J. McRiner
  • Publication number: 20080171724
    Abstract: Phosphorus substituted mycophenolate oxime derivatives with anti-cancer, anti-viral, anti-inflammatory anti-tissue/organ transplant rejection properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit tumor growth, viral growth, inflammation, and tissue/organ transplant rejection and/or are useful therapeutically for the treatment or prevention of cancer, viral infection, inflammation and tissue/organ transplant rejection, as well as in assays for the detection of cancer, viral infection, inflammation and tissue/organ transplant rejection.
    Type: Application
    Filed: October 26, 2005
    Publication date: July 17, 2008
    Applicant: GILEAD SCIENCES, INC.
    Inventors: William J. Watkins, Aesop Cho
  • Publication number: 20080139512
    Abstract: The invention pertains to compositions and methods to treat the adverse effects of mustard chemicals and other toxic compounds, such as chemical warfare agents, exposure to which normally induces vesicating type response in mammals. In a rodent eye model at fixed concentrations of such a vesicant, compositions comprising a matrix metalloproteinase inhibitor, MMPI, a significant reduction in morbidity is achieved. with increased concentrations of the compositions of this invention, as compared with vehicle alone. Furthermore, compositions comprising the MMPI and in addition, an anti-inflammatory compound, in a vehicle appropriate to the type of tissue damage to be protected against from vesicant exposure, achieves both reduction in total tissue damage and inflammation, as compared with anti-inflammatory composition alone. Chemicals having more than one property, such as MMPI and AIA properties, are also disclosed.
    Type: Application
    Filed: January 30, 2006
    Publication date: June 12, 2008
    Applicants: Quick-Med Technologies, Inc., University of Florida Research Foundation, Inc.
    Inventors: David S. Lerner, Gregory Schultz
  • Publication number: 20080139389
    Abstract: The present invention relates to the use of fungicidally active carboxamides for seed treatment, for corresponding seed dressings comprising these carboxamides, to a process for controlling phytopathogenic fungi by treating the seed with fungicidally active carboxamides, and also to seed which has been treated with the fungicidally active carboxamides.
    Type: Application
    Filed: June 16, 2005
    Publication date: June 12, 2008
    Inventors: Geoff Kneen, Anne Suty-Heinze, Peter Dahmen, Yasuo Araki, Takuma Shigyo, Hans-Ludwig Elbe
  • Publication number: 20080118579
    Abstract: The invention relates to a medical device comprising non-sintered bioactive glass particles or fibres having a diameter in the range 5-100 ?m, bioactive glass comprising SiO2, Na2O, CaO, K2O, MgO, B2O3 and P2O5, wherein the amount of SiO2 is 50-65 wt-% of the final total weight, Na2O is 5-26 wt-% of the final total weight, CaO is 10-25 wt-% of the final total weight, K2O is 0-15 wt-% of the final total weight, MgO is 0-6 wt-% of the final total weight, B2O3 is 0-4 wt-% of the final total weight, and P2O5 is 0-4 wt-% of the final total weight, provided that the total amount of Na2O and K2O is 10-30 wt-% of the final total weight The device is essentially drug free. The invention also relates to the use of said composition for treating lesions associated with compromised or poor vascularisation and for preventing avascular fibrosis.
    Type: Application
    Filed: November 2, 2005
    Publication date: May 22, 2008
    Applicant: VIVOXID OY
    Inventors: Hannu Jarvelainen, Matti Laato, Jukka Salonen, Erik Vedel
  • Publication number: 20080095866
    Abstract: The present invention provides topical compositions containing phosphorylated polyphenols in combination with a topically acceptable carrier. The compositions of the invention provide a means for delayed delivery of the polyphenol to keratinous tissues, such as skin, hair and nails, with enzymes of the keratinous tissue dephosphorylating the polyphenol, and returning it to its native active form. The compositions are particularly useful in the regulation of skin conditions.
    Type: Application
    Filed: September 14, 2004
    Publication date: April 24, 2008
    Applicants: AJINOMOTO OMNICHEM S.A., ESTEE LAUDER COORDINATION CENTER N.V.
    Inventors: Lieve Declercq, Hugo Corstjens, Daniel Maes, Willy Van Brussel, Geert Schelkens
  • Publication number: 20080026074
    Abstract: A method for the treatment of skin damage using strontium divalent ion in a dermatologically acceptable carrier is provided, usually an essential oil distillate. The compositions are applied topically to improve appearance of skin damaged by sun or by natural aging. The compositions may additionally include antioxidant molecules such as vitamin E, ferulic acid and vitamin C.
    Type: Application
    Filed: July 27, 2006
    Publication date: January 31, 2008
    Inventors: Hannah Naomi Sivak, Mary Hunter
  • Publication number: 20080014277
    Abstract: The present invention provides compositions for and methods of delivering a therapeutically-effective dose of a malodorous, sulfide or disulfide group-containing compound, for example glutathione (reduced) and/or glutathione disulfide, in a vehicle that is effective to reduce the unpleasant odor and/or taste of the compound. The invention further provides methods for reducing the amount of oxidation occurring when sulfide group-containing compounds, such as glutathione, are incorporated into sugar and or sugar-free hard candies without subjecting the glutathione to thermal and or moisture degradation where degradation is expressed as oxidation. The invention further provides vehicle compositions including the protected sulfide group-containing compounds and their use as medicaments. The sulfide group-containing compounds are protected from degradation by their dispersion into fats, oils, and/or fractionated or partially hydrogenated oils prior to their blending into the vehicle.
    Type: Application
    Filed: July 14, 2006
    Publication date: January 17, 2008
    Inventor: Mario W. Medri
  • Patent number: 7232809
    Abstract: The invention provides mitochondrially targeted antioxidant compounds. A compound of the invention comprises a lipophilic cation covalently coupled to an antioxidant moiety. In preferred embodiments, the lipophilic cation is the triphenyl phosphonium cation, and the compound is of the formula P(Ph3)+XR.Z? where X is a linking group, Z is an anion and R is an antioxidant moiety. Also provided are pharmaceutical compositions containing the mitochondrially targeted antioxidant compounds, and methods of therapy or prophylaxis of patients who would benefit from reduced oxidative stress, which comprise the step of administering the compounds of the invention.
    Type: Grant
    Filed: July 5, 2005
    Date of Patent: June 19, 2007
    Assignee: Antipodean Pharmaceuticals, Inc.
    Inventors: Michael P. Murphy, Robin A. J. Smith
  • Patent number: 7229979
    Abstract: Methods of treating a host suffering from restenosis are provided. The methods include delivery of a stent coated with a hypoestoxide, hypoestoxide derivative or hypoestoxide agonist compound to a vessel. The methods further include the administration of a chemotherapeutic agent in combination with delivery of a stent coated with a hypoestoxide, hypoestoxide derivative or hypoestoxide agonist compound to a vessel. The chemotherapeutic agent may be coated on the stent or administered systemically.
    Type: Grant
    Filed: June 23, 2004
    Date of Patent: June 12, 2007
    Assignee: Immune Modulation, Inc.
    Inventors: Emeka J. Nchekwube, Emmanuel A. Ojo-Amaize, Howard B. Cottam
  • Patent number: 7192939
    Abstract: The present invention relates to the novel isolated 12–30 strain of Pestalotiopsis microspora capable of producing novel antioxidant and antimycotic agents. The present invention also relates to the novel isolated 3,5,7 trisubstituted isobenzofuranone and derivatives thereof, methods of isolating the novel isobenzofuranone from cultures P. microspora 12–30, and to novel uses of the compound as an antioxidant and antimycotic agent. The present invention further relates to a novel 1,5,7 trisubstituted 1,3-dihydroisobenzofuran and derivatives thereof, methods of isolating this novel compound from cultures of Pestalotiopsis microspora 12–30, and to uses thereof.
    Type: Grant
    Filed: January 30, 2003
    Date of Patent: March 20, 2007
    Assignee: Montana State University
    Inventors: Gary Strobel, Eugene Ford, James K. Harper
  • Patent number: 7192905
    Abstract: Combination of a cytochrome P450 monooxygenase inducer with an organophosphate pesticide (insecticide or acaracide) provides effective control of ticks and flies, particularly against organophosphate-resistant strains of the ticks and flies. In use, a pesticidally effective amount of a composition of the cytochrome P450 monooxygenase inducer and organophosphate pesticide is applied to the locus of the targeted tick or fly.
    Type: Grant
    Filed: June 20, 2003
    Date of Patent: March 20, 2007
    Assignee: The United States of America as represented by the Secretary of Agriculture
    Inventors: Andrew Y. Li, John Allen Miller
  • Patent number: 7144867
    Abstract: The present invention relates to new classes of anti-cancer compounds. In particular, the present invention provides glycoside compounds as anti-cancer agent, alone, or in combination with other anti-cancer agents or therapies.
    Type: Grant
    Filed: January 27, 2005
    Date of Patent: December 5, 2006
    Assignees: Northwestern University, Coastside Bio Resources
    Inventors: Thomas E. Adrian, Peter D. Collin
  • Patent number: 7138486
    Abstract: Derivatives of glucagon-like peptide I (GLP-1) and especially GLP-1 (7-37) have been found to have insulinotropic activity. The invention pertains to a composition comprising an acid addition salt of GLP-I (7-37) and to a composition comprising a carboxylate salt of GLP-I (7-37). The invention also pertains to method of treating type II diabetes mellitus by providing derivatives of GLP-I (7-37) to the patient.
    Type: Grant
    Filed: June 21, 2004
    Date of Patent: November 21, 2006
    Assignee: The General Hospital Corporation
    Inventors: Joel F. Habener, Svetlana Mojsov
  • Patent number: 7122525
    Abstract: The invention features a method of delivering a drug to a diseased cell by linking the drug to a rifamycin derivative, compositions that include drug-rifamycin conjugates of the invention, and methods for treating disease using those compositions.
    Type: Grant
    Filed: November 21, 2002
    Date of Patent: October 17, 2006
    Assignee: ActivBiotics, Inc.
    Inventors: Arthur F. Michaelis, Hawkins V. Maulding, Chalom Sayada, Congxiang Zha
  • Patent number: 7084134
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 1, 2003
    Date of Patent: August 1, 2006
    Assignee: Merk & Co., Inc.
    Inventors: James C. Barrow, Philippe G. Nantermet, Harold G. Selnick
  • Patent number: 7060290
    Abstract: Disclosed are compounds of general formula (I) that function as prodrugs, thereby increasing bioavailabilities of the linked therapeutic agents, wherein the LINKER is (i) substituted or unsubstituted alkyl, (ii) substituted or unsubstituted alkenyl, (iii) substituted or unsubstituted alkanoyl, (iv) substituted or unsubstituted alkenoyl wherein the double bond is cis, and (v) (ortho or para) carbonyl-substituted aryl; and wherein the subtituent is each an independent group or linked together thereby forming a ring; and wherein X is one or more substituted or unsubstituted group containing one or more O, N, or S atom and wherein the substituent is each an independent group or linked together thereby forming a ring; and wherein the therapeutic agent is an alcohol-containing water-insoluble steroids or another alcohol containing compounds and methods to prepare such compounds.
    Type: Grant
    Filed: February 16, 2000
    Date of Patent: June 13, 2006
    Assignee: Supergen, Inc.
    Inventors: Bruce H. Morimoto, Peter L. Barker
  • Patent number: 7056499
    Abstract: The present invention relates to a treating method for hair growth inhibition, which comprises administering (A) the extract of a plant of the family Juniperus or a malt. In addition, the present invention relates to a dermatologic composition for external use, which comprises (B) an elastase inhibitor or neutral endopeptidase inhibitor, and the above-described component (A) and/or (C) at least one proteolytic enzyme selected from the group consisting of papain, trypsin, chymotrypsin, pepsin, bromelain, ficin and pancreatin.
    Type: Grant
    Filed: February 8, 2002
    Date of Patent: June 6, 2006
    Assignee: Kao Corporation
    Inventors: Naoko Tsuji, Shigeru Moriwaki, Atsushi Ohuchi, Yasuto Suzuki
  • Patent number: 7019024
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: March 28, 2006
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Patent number: 6974806
    Abstract: The present invention provides a lipid-rich plaque regressing agent comprising a compound represented by Formula: in which ring A is a cyclic hydrocarbon or the like; ring B is a heterocyclic ring or the like; each of X and Y is —NR1— (in which R1 is a hydrocarbon or the like); D is a C1-3 alkylene group or the like; E is —NH— or the like; G is a bond or the like; and Ar is an aryl or the like; D may be taken together with a constituent atom of the ring B to form a ring, and R4 may be taken together with a constituent atom of the ring B to form a ring.
    Type: Grant
    Filed: July 13, 2001
    Date of Patent: December 13, 2005
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Zen-ichi Terashita, Masahira Nakamura, Shogo Marui, Masaki Ogino
  • Patent number: 6858209
    Abstract: Means for detection of bacteria of the genus Taylorella and biological applications thereof are described. In particular, the detection of T. equigenitalis and the treatment or prevention of infections caused by bacteria of this species are disclosed. Monoclonal antibodies which recognize an epitope of a bacterium of the species T. equigenitalis are disclosed. These monoclonal antibodies may be used to detect T. equigenitalis with certainty and by means of a single test.
    Type: Grant
    Filed: April 11, 1997
    Date of Patent: February 22, 2005
    Assignee: Conseil General de l'Orne
    Inventors: Frédéric Klein, Dragos Gradinaru
  • Patent number: 6858593
    Abstract: There is provided a crystalline chemical composition comprising a compound of formula (I) in which the crystal lattice is stabilized by the presence of a guest molecule, characterized in the crystalline composition is of space group P212121 having unit cell dimensions of about 7.6±0.6 ?, 12.7±0.7 ?, and 33±3 ? when determined at 120 K.
    Type: Grant
    Filed: July 22, 2002
    Date of Patent: February 22, 2005
    Assignee: Smithkline Beecham Corporation
    Inventors: Keith Biggadike, Olga Chetina, Steven John Coote, Andrew Craig, Victor Jacewicz, Michael J. Millan, John F. Seager, Andrew L. Theophilus
  • Patent number: 6849708
    Abstract: Derivatives of glucagon-like peptide I (GLP-1) and especially GLP-1(7-36) have been found to have insulinotropic activity. The invention pertains to the use of GLP-1(7-36) for the treatment of type II diabetes mellitus.
    Type: Grant
    Filed: August 10, 2000
    Date of Patent: February 1, 2005
    Assignee: The General Hospital Corporation
    Inventor: Joel F. Habener
  • Publication number: 20040265396
    Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.
    Type: Application
    Filed: September 30, 2003
    Publication date: December 30, 2004
    Inventor: Mickey L. Peshoff
  • Publication number: 20040258728
    Abstract: Methods of treating a host suffering from restenosis are provided. The methods include delivery of a stent coated with a hypoestoxide, hypoestoxide derivative or hypoestoxide agonist compound to a vessel. The methods further include the administration of a chemotherapeutic agent in combination with delivery of a stent coated with a hypoestoxide, hypoestoxide derivative or hypoestoxide agonist compound to a vessel. The chemotherapeutic agent may be coated on the stent or administered systemically.
    Type: Application
    Filed: June 23, 2004
    Publication date: December 23, 2004
    Applicant: Paraquest Medivice, Inc.
    Inventors: Emeka J. Nchekwube, Emmanuel A. Ojo-Amaize, Howard B. Cottam
  • Publication number: 20040254149
    Abstract: The present invention pertains to the use of a compounds for the manufacture of a medicament for use in the treatment of a proliferative condition, wherein the compounds have the following formula: 1
    Type: Application
    Filed: April 2, 2004
    Publication date: December 16, 2004
    Inventors: Gerard Andrew Potter, Paul Crispin Butler
  • Publication number: 20040253318
    Abstract: There is provided a method for preventing, alleviating symptoms or treating a skin condition comprising topically administering to the skin of a subject a cosmetic or pharmaceutical topical formulation comprising an effective skin-penetrating amount of one or more phosphate derivatives of one or more electron transfer agents.
    Type: Application
    Filed: August 5, 2004
    Publication date: December 16, 2004
    Inventors: Simon Michael West, Robert J. Verdicchio, David Kannar, Otto H. Mills Jr.
  • Publication number: 20040242544
    Abstract: Novel derivatives of ascorbic acid and compositions comprising them are provided. The novel derivatives are of the following general formula (I): where R1 is a C2-C22 saturated or unsaturated fatty acid residues, amino acid residues, or a C1-C17 alkyl ; R2 is a group of the following formula (II) wherein R5 or R6 are the same or different and represent hydrogen, a C1-C4 alkyl, or R5 is C1-C4 alkyl group and R6 is a metal cation or ammonium cation; R3 or R4 are the same or different and represent hydrogen, C2-C22 saturated or unsaturated fatty acid residues, amino acid residues, or a C1-C17 alkyl.
    Type: Application
    Filed: July 15, 2004
    Publication date: December 2, 2004
    Inventors: Vladimir Babtsov, Yury Shapiro, Emma Kvitnitsky, Valery Belakhov
  • Publication number: 20040228884
    Abstract: This invention relates to a novel ion-pair delivery system useful for cosmetic, pharmaceutical, and topical nutraceutical applications in which the functional performance and consumer aesthetics of an electron donor composition and an electron acceptor composition, or a proton donor composition and a proton acceptor composition, are synergistically enhanced when such compositions are combined in an ion-pair mode. During ion-pair bonding process, the electron donor composition or the proton acceptor composition become positively charged and the electron acceptor composition or proton donor composition become negatively charged and thus bind together in an ionic manner. Such ion-pair compositions release their electronically bound components in their original state when such compositions are absorbed into skin and reach physiological pH conditions.
    Type: Application
    Filed: May 15, 2003
    Publication date: November 18, 2004
    Inventor: Shyam K. Gupta
  • Publication number: 20040176309
    Abstract: The invention relates to Siglec inhibitors that have an increased affinity for the receptor molecule. The Siglec inhibitors provided by the invention are preferably selective of a given Siglec molecule. The invention further relates to a method for producing Siglec inhibitors and to a method for increasing the binding selectivity for a given Siglec molecule. The invention also relates to pharmaceutical compositions that contain the Siglec inhibitors and to medical indications for the Siglec inhibitors.
    Type: Application
    Filed: February 13, 2004
    Publication date: September 9, 2004
    Inventors: Sorge Kelm, Reinhard Brossmer
  • Patent number: 6780430
    Abstract: Disclosed herein is a stabilization method of nano-sized emulsion by using lecithin and tocopheryl derivatives represented by the following formula (I) and (Wherein, R1, R2 and R3 are H or methyl group, and at least one position selected from the group consisting of the R1, R2 and R3 positions are methyl group; and, A is CH2—CH(CH3)— or CH═C(CH3)—) and an external application for skin containing the stabilized nano-sized emulsion.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: August 24, 2004
    Assignee: Pacific Corporation
    Inventors: Byung Hee Yoo, Joung Soo Kim, Byung Young Kang, Kil Joong Kim, Sang Hoon Han
  • Publication number: 20040157800
    Abstract: Novel L-carnitine and lower alkanoyl L-carnitine ascorbyl derivatives and topically applicable cosmetic compositions comprising same as active ingredients. The cosmetic compositions are particularly suitable for preventing and treating the anaesthetic consequences of localized adiposity and the cascade of dysmetabolic events linked thereto.
    Type: Application
    Filed: April 19, 2004
    Publication date: August 12, 2004
    Inventors: Antonietta Buononato, Emanuela Veggetti
  • Publication number: 20040156923
    Abstract: Provided is a nutraceutical composition including a glucosamine based component. The composition is effective to improve fertility in mammals, including humans and stallions. A method for improving fertility in a mammal using glucosamine based nutraceutical composition is also provided.
    Type: Application
    Filed: October 23, 2003
    Publication date: August 12, 2004
    Inventors: David F. Davenport, J. Eric Martin
  • Patent number: 6774142
    Abstract: 3-Deoxyflavonoid compounds and methods for inhibiting T-cell activity and treating diseases and disorders (e.g., autoimmune disorders, inflammatory disorders, diabetes, ALS, MS, rheumatoid arthritis, etc.). In some cases the efficacy and/or duration of action of luteolin and/or other 3-dioxyflavinoid compounds may be increased by administering such compounds along with Rutin, a Rutin congener and/or a Rutin derivative. Also, in some cases, first pass metabolism of luteolin or other 3-deoxyflavinoids may be avoided by administering such compounds by parenteral routes (e.g., sublingual, buccal, intranasal, injection, etc.).
    Type: Grant
    Filed: September 6, 2002
    Date of Patent: August 10, 2004
    Inventors: Thomas P. Lahey, Vithal J. Rajadhyasksha
  • Publication number: 20040106581
    Abstract: The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia), 1
    Type: Application
    Filed: July 1, 2003
    Publication date: June 3, 2004
    Inventors: Bansi Lal, Kalpana Joshi, Sanjeev Kulkarni, Malcolm Mascarenhas, Shrikant Kamble, Maggie Joyce Rathos, Rajendrakumar Joshi
  • Publication number: 20040102386
    Abstract: 3-Deoxyflavonoid compounds and methods for inhibiting T-cell activity and treating diseases and disorders (e.g., autoimmune disorders, inflammatory disorders, diabetes, ALS, MS, rheumatoid arthritis, etc.). In some cases the efficacy and/or duration of action of luteolin and/or other 3-deoxyflavonoid compounds may be increased by administering such compounds along with Rutin, a Rutin congener and/or a Rutin derivative. Also, in some cases, first pass metabolism of luteolin or other 3-deoxyflavonoids may be avoided by administering such compounds by parenteral routes (e.g., routes wherein absorption occurs at sites other than the stomach or intestinal mucosa, such as sublingual, buccal, intranasal, injection, etc.).
    Type: Application
    Filed: August 29, 2003
    Publication date: May 27, 2004
    Inventors: Thomas Lahey, Vithal J. Rajadhyaksha
  • Publication number: 20040087553
    Abstract: Methods for treatment and prophylaxis of hyperlipidemias, including hypertriglyceridemia and hypercholesterolemia, are provided. The methods include administering to a host a therapeutically or prophylactically effective amount of a diterpene compound, such as a hypoestoxide.
    Type: Application
    Filed: October 28, 2003
    Publication date: May 6, 2004
    Applicant: Paraquest, Inc.
    Inventors: Emeka J. Nchekwube, Emmanuel A. Ojo-Amaize, Howard B. Cottam
  • Publication number: 20040029837
    Abstract: The invention relates to oxazine derivatives by means of which a broad spectrum of material to be examined can be marked and identified using fluorescence techniques.
    Type: Application
    Filed: July 14, 2003
    Publication date: February 12, 2004
    Inventors: Joachim Fries, Eloisa Lopez-Calle, Karl-Heinz Drexhage
  • Publication number: 20040006049
    Abstract: Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.
    Type: Application
    Filed: March 10, 2003
    Publication date: January 8, 2004
    Applicant: SLIL Biomedical Corporation
    Inventors: Benjamin Frydman, Laurence J. Marton
  • Patent number: 6656927
    Abstract: A compound represented by the general formula (I) or a salt thereof, wherein R represents a group represented by the following formula (A), (B) or (C) wherein R1 and R2 independently represent a C1-6 alkyl group, R3 represents an amino group, a mono(C1-6 alkyl)amino group, a di(C1-6 alkyl)amino group or a C1-6 alkoxy group and X-represents an anion, and n represents an integer of 2 to 5. The compound or a salt is useful as a ligand of inositol-1,4,5-trisphosphate (IP3) receptor.
    Type: Grant
    Filed: November 30, 2001
    Date of Patent: December 2, 2003
    Assignees: Daiichi Pharmaceutical., Ltd.
    Inventors: Tetsuo Nagano, Kazuya Kikuchi, Takanari Inoue, Masamitsu Iino, Kenzo Hirose
  • Publication number: 20030212009
    Abstract: Isoflavones are modified by esterification at one or more of the C4′, C5, C6, and C7 positions to promote bioavailability, and especially to enhance solubility over the corresponding unesterified isoflavones. Preferred modifications produce a carboxylic acid hemiester or a phosphate ester which is biologically hydrolysable. Preferred starting isoflavones are genistin and daidzin, and still more preferably comprises an aglycone form such as genistein or daidzein. Esterified isoflavones may be employed therapeutically or prophylactically for a variety of conditions, provided as a dietary supplement, or added to natural or processed food-stuffs. Further preferred uses include incorporation of contemplated compounds into topical formulations, and especially cosmetic topical formulations.
    Type: Application
    Filed: February 20, 2003
    Publication date: November 13, 2003
    Inventors: Sheldon S. Hendler, Jan Zielinski
  • Patent number: 6645951
    Abstract: The present invention provides novel benzopyran compounds, pharmaceutically acceptable salts thereof and stereoisomers thereof where the benzopyran compounds of the invention are compounds according to Formula I: The present invention further provides pharmaceutical compositions which possess anti-estrogenic activity and comprise at least one benzopyran compound of the invention and a method of treating breast cancer by administration of an effective amount of a benzopyran compound provided by the present invention.
    Type: Grant
    Filed: July 16, 2001
    Date of Patent: November 11, 2003
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Jae Chon Jo, Hyun Suk Lim, Jong Min Kim, Ju Su Kim, Kazumi Morikawa, Yoshitake Kanbe, Myung Hwa Kim, Masahiro Nishimoto
  • Patent number: 6642216
    Abstract: Compounds of the formula wherein X in each of formulas (1) and (2) represents a substituted or unsubstituted alkylene, alkenylene, or alkynylene linker of 2-6C; Y is of the formula  or a stereoisomer thereof, wherein R1 is substituted or unsubstituted alkyl; each R2 is independently H, hydroxy, alkoxy (1-6C) or lower alkyl (1-4C); R3 is H, hydroxy, or alkoxy (1-6C); or Y is of the formula  wherein each n is 1, Z is N, K comprises a substituted or unsubstituted aromatic carbocyclic or heterocyclic ring system which may optionally be spaced from the linkage position shown in formula (7) by a linker of 1-2C, or in formula (7), Z may be spaced from the carbon bonded to X by ═CR6— wherein R6 is H or linear, branded or cyclic alkyl (1-6C), R5 is H or linear, branched or cyclic alkyl, and R′ represents a cation, H or a substituted or unsubstituted alkyl group of 1-6C, promote bone formation and are thus useful in treating oste
    Type: Grant
    Filed: May 3, 2001
    Date of Patent: November 4, 2003
    Assignees: ZymoGenetics Corporation, OsteoScreen, Inc.
    Inventors: Shirley R. Gasper, Robert R. West, Theresa Martinez, Kirk G. Robbins, Patricia A. McKernan, Nand Baindur, Virender M. Labroo, Gregory R. Mundy
  • Publication number: 20030199014
    Abstract: In vitro methods for qualitative screening and/or quantitative determination of the functional activity of components of the Protein C anticoagulant pathway of blood coagulation are described. The methods entail measuring the conversion rate of a substrate by an enzyme, the activity of which is related to the Protein C anticoagulant activity, in a blood sample of a human comprising coagulation factors and said substrate, after at least partial activation of coagulation through the intrinsic, extrinsic or common pathway and triggering coagulation by adding calcium ions; and comparing said conversion rate with the conversion rate of a normal human blood sample determined in the same way. The methods include the addition of additional metal ions to the sample to enhance activity, sensitivity and resolution. Kits and reagents for use in the methods are also provided.
    Type: Application
    Filed: December 30, 2002
    Publication date: October 23, 2003
    Inventors: Bert Steffen Rosen, Christina Maria Yvonne Hall
  • Publication number: 20030181423
    Abstract: A polybifunctional reagent having a polymeric backbone, one or more pendent photoreactive moieties, and two or more pendent bioactive groups. The reagent can be activated to form a bulk material or can be brought into contact with the surface of a previously formed biomaterial and activated to form a coating. The pendent bioactive groups function by promoting the attachment of specific molecules or cells to the bulk material or coated surface. Bioactive groups can include proteins, peptides, carbohydrates, nucleic acids and other molecules that are capable of binding noncovalently to specific and complimentary portions of molecules or cells.
    Type: Application
    Filed: February 3, 2003
    Publication date: September 25, 2003
    Inventors: David L. Clapper, Melvin J. Swanson, Sheau-Ping Hu, Richard A. Amos, Terrence P. Everson
  • Publication number: 20030176324
    Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.
    Type: Application
    Filed: July 29, 2002
    Publication date: September 18, 2003
    Applicant: University of Kansas
    Inventors: Valentino J. Stella, Jan J. Zygmunt, Ingrid Gunda Georg, Muhammad S. Safadi
  • Publication number: 20030171336
    Abstract: A packaging cell line capable of complementing recombinant adenoviruses based on serotypes from subgroup B, preferably adenovirus type 35. The cell line is preferably derived from primary, diploid human cells transformed by adenovirus E1 sequences either operatively linked on one or two DNA molecules, the sequences operatively linked to regulatory sequences enabling transcription and translation of encoded proteins. Also, a cell line derived from PER.C6 that expresses functional Ad35 E1B sequences. The Ad35-E1B sequences are driven by the E1B promoter and terminated by a heterologous poly-adenylation signal. The new cell lines are useful for producing recombinant adenoviruses. The cell lines can be used to produce human recombinant therapeutic proteins such as human antibodies. In addition, the cell lines are useful for producing human viruses other than adenovirus such as influenza, herpes simplex, rotavirus, and measles.
    Type: Application
    Filed: June 4, 2002
    Publication date: September 11, 2003
    Inventors: Ronald Vogels, Menzo Havenga, Majid Mehtali
  • Publication number: 20030157201
    Abstract: The present invention relates to a highly potent herbal composition for improving overall mental performance in children, adults and mentally deficient people characterized by using extracted active plant materials from Brahmi herb and at least one of the herbs from Acorus calamus and Celestrus paniculatus oil.
    Type: Application
    Filed: January 16, 2003
    Publication date: August 21, 2003
    Inventors: Maharaj Krishen Pandita, Govind Prashad Dubey