S Of S-x-c Attached Directly To A Benzene Ring Patents (Class 514/518)
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Patent number: 7402704Abstract: Aryl sulfone compounds of formula I and II are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:Type: GrantFiled: April 14, 2005Date of Patent: July 22, 2008Assignee: Amgen Inc.Inventors: Pingchen Fan, Hiroyuki Goto, Xiao He, Makoto Kakutani, Marc Labelle, Dustin L. McMinn, Jay P. Powers, Yosup Rew, Daqing Sun, Xuelei Yan
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Patent number: 7390833Abstract: The present invention relates to methods of treating ADAMTS-5-associated diseases and particularly osteoarthritis comprising administering an agent capable of modulating ADMATS-5 activity to a subject afflicted with the disease. The agent is preferably a biaryl sulfonamide compound. The invention is based, in part, on the discovery that transgenic animals that do not express functional ADAMTS-5 show a reduction in the degree of osteoarthritis after the induction of osteoarthritis as compared to WT animals. Furthermore, the ADAMTS-5 transgenic animals have reduced aggrecanase activity in articular tissue as compared to WT animals. These animals are good models for ADAMTS-5-associated diseases, and for screening of drugs useful in the treatment and/or prevention of these diseases. There are no other animal models in which the deletion of the activity of a single gene is capable of abrogating the course of osteoarthritis.Type: GrantFiled: November 8, 2004Date of Patent: June 24, 2008Assignee: WyethInventors: Elisabeth A. Morris, Sonya Glasson, Jason Shaoyun Xiang
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Patent number: 7351427Abstract: Pharmaceutically acceptable liposome-encapsulated busulphan formulations for parenteral administration are provided, as well as such formulations furthermore comprising glutathione and/or at least one glutathione precursor and a process for manufacture of the preparations. The formulations are stable, have improved biodistribution and significantly reduced side effects over those produced by oral administration or parenteral administration of free drug. The formulations are useful as part of stem cell and/or bone marrow transplant conditioning regimens. A method of treatment of a mammal by use of such formulations.Type: GrantFiled: April 30, 2003Date of Patent: April 1, 2008Assignee: Busulipo ABInventors: Zuzana Hassan, Moustapha Hassan
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Patent number: 7250440Abstract: This invention provides estrogen receptor modulators of formula I, having the structure where R1, R2, R3, and R4 are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 9, 2004Date of Patent: July 31, 2007Assignee: WyethInventors: Richard Eric Mewshaw, Stephen Marc Bowen, Eric Steven Manas
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Patent number: 7199155Abstract: Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-?, such as rheumatoid arthritis, graft rejection, cachexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease or HIV infection.Type: GrantFiled: December 19, 2003Date of Patent: April 3, 2007Assignee: Wyeth Holdings CorporationInventors: Jeremy Ian Levin, Mila Ti Du
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Patent number: 7041844Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.Type: GrantFiled: November 18, 2002Date of Patent: May 9, 2006Assignee: The University Of Tennessee Research CorporationInventors: Duane D. Miller, Leonid I. Kirkovsky, James T. Dalton, Arnab Mukherjee
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 7026339Abstract: The present invention relates to compounds, process for their synthesis, compositions and methods for the treatment and prevention of hepatitis C virus (HCV) infection. In particular, the present invention provides novel compounds, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment or prevention of HCV infection. The present invention also provides processes and intermediates for the synthesis of these compounds.Type: GrantFiled: November 3, 2004Date of Patent: April 11, 2006Inventors: Fan Yang, Bo Zhang, Nancy Anne Wicnienski, Jeffrey Allen Pfefferkorn, Meredith L. Greene, Ke Chen, Richard A. Nugent, Matthew Todd Reding, Robert Charles Kelly, Mark A. Mitchell, Lee A. Funk, Richard Frederick Heier, III, Rebecca Merry Anderson
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Publication number: 20040259813Abstract: Compositions of matter and methods wherein chalcone and flavone derivatives are administered to human or veterinary patients for the treatment of bladder or urinary tract cancer. Compounds of the invention include 2′-hydroxy-4,4′,6′-trimethoxychalcone (Flavokawain A).Type: ApplicationFiled: April 1, 2004Publication date: December 23, 2004Applicant: The Regents of the University of CaliforniaInventors: Xiolin Zi, Anne R. Simoneau
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Publication number: 20040161393Abstract: The present invention provides a method of treating sebaceous gland disorders comprising administering to a patient in need of said treatment an effective amount of a compound named [(2,4,6-triisopropyl-phenyl)-acetyl]-sulfamic acid 2,6-diisopropyl-phenyl ester or a pharmaceutically acceptable salt thereof. Particularly, methods of treating sebaceous gland disorders are provided wherein said disorders are selected from seborrhea, acnes, perioral dermatitis, rosacea, and corticosteroid-induced acneiform lesions. The present invention provides methods of treating acnes such as, for example, chloracne, ciliaris acne, cystic acne, keratosa acne, vulgaris acne, senile acne, and medicinal acne.Type: ApplicationFiled: February 6, 2004Publication date: August 19, 2004Inventor: Reynold Homan
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Patent number: 6777200Abstract: This invention provides novel compounds derived from a marine sponge, Adocia sp., that specifically modulat kinesin activity by targeting the kinesin motor domain and mimicking the activity a microtubule. The compounds act as potent anti-mitogens are useful in a wide variety of in vitro and in vivo applications.Type: GrantFiled: November 27, 2002Date of Patent: August 17, 2004Assignee: The Regents of the University of CaliforniaInventors: Lawrence S. B. Goldstein, David John Faulkner, Roman Sakowicz, Michael S. Berdelis, Christine L. Blackburn, Cordula Hopmann
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Publication number: 20040157919Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.Type: ApplicationFiled: November 14, 2003Publication date: August 12, 2004Inventors: Yong-Qian Wu, Sergei Belyakov, Gregory S. Hamilton, David Limburg, Joseph P. Steiner, Mark Vaal, Ling Wei, Douglas Wilkinson
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Publication number: 20040132810Abstract: The present invention includes a method for making a formulation for treating mucosal discontinuities, comprising: providing phenolic compounds and treating the purified phenolic compounds with sulfuric acid to make sulfonic acids and sulfonate salts. The present invention also includes formulations prepared by the method.Type: ApplicationFiled: May 21, 2003Publication date: July 8, 2004Inventor: Michael Basara
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Publication number: 20040127524Abstract: Hydroxamic acids having the formula 1Type: ApplicationFiled: December 19, 2003Publication date: July 1, 2004Applicant: Wyeth Holdings CorporationInventors: Jeremy Ian Levin, Mila Ti Du
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Publication number: 20040097583Abstract: Inhibitors of the cellular sodium/hydrogen exchangers show an inhibiting effect on the secretion of von-Willebrand factor and/or increased expression of P-selectin. These inhibitors can therefore be employed for the treatment of thrombotic and inflammatory disorders.Type: ApplicationFiled: February 7, 2003Publication date: May 20, 2004Inventors: Hans-Jochen Lang, Stefan Werner Schneider, Hans Oberleithner, Andre Niemeyer
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Publication number: 20040087650Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: ApplicationFiled: September 25, 2003Publication date: May 6, 2004Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jeffrey O. Saunders, Daniel Elbaum, Perry M. Novak, Douglas Naegele, Randy S. Bethiel, Steven M. Ronkin, Michael C. Badia, Catharine Frank, Dean P. Stamos, William Walters, David Pearlman
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Publication number: 20040087659Abstract: The invention relates to urea- and urethane-substituted acylureas and to their physiologically tolerated salts and physiologically functional derivatives.Type: ApplicationFiled: July 11, 2003Publication date: May 6, 2004Inventors: Elisabeth Defossa, Dieter Kadereit, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Karl Schoenafinger
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Patent number: 6730783Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: April 22, 2003Date of Patent: May 4, 2004Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan
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Publication number: 20040082611Abstract: Described in the present invention are a sulfonyl derivative represented by the following formula (I):Type: ApplicationFiled: October 9, 2003Publication date: April 29, 2004Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Syozo Kobayashi, Satoshi Komoriya, Noriyasu Haginoya, Masanori Suzuki, Toshiharu Yoshino, Takayasu Nagahara, Tsutomu Nagata, Haruhiko Horino, Masayuki Ito, Akiyoshi Mochizuki
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Publication number: 20040052864Abstract: Compositions and methods are provided for treating diseases associated with abnormal cell proliferation such as cancer by storing inherent tumor-suppressing functions of neoplastic cells through DNA hypomethylation. The method comprises: delivering to a patient suffering from cancer a therapeutically effective amount of a DNA methylation inhibitor such as decitabine, in combination with an effective amount of an anti-neoplastic agent whose activity as an anti-neoplastic agent in vivo is adversely affected by aberrant DNA methylation. The anti-neoplastic agent can be an alkylating agent, an antibiotic agent, an antimetabolic agent, a retinoid, a hormonal agent, a plant-derived agent, an anti-angiogenesis agent and a biologic agent such as monoclonal antibody and interferon.Type: ApplicationFiled: July 3, 2003Publication date: March 18, 2004Applicant: SuperGen, Inc.Inventors: Joseph Rubinfeld, Lucy Chang, Jorge DiMartino
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Publication number: 20030228268Abstract: The present invention relates to a cosmetic and/or dermatological composition more particularly intended for artificially tanning and/or browning the skin and comprising, in a cosmetically acceptable support, at least one derivative or a mixture of derivatives of 1,7-bisphenyl heptane-3,5-dione of particular structure and at least one self-tanning agent.Type: ApplicationFiled: March 28, 2003Publication date: December 11, 2003Applicant: SOCIETE L'OREAL S.A.Inventor: Didier Candau
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Patent number: 6638931Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: November 28, 2000Date of Patent: October 28, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
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Patent number: 6617360Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1 and R2 are independently H or methyl (for example N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl amine hydrochloride optionally in the form of its monohydrate) is used for reducing Insulin resistance in humans in whom Impaired Glucose Tolerance and Non-Insulin Dependent Diabetes Mellitus have not presented.Type: GrantFiled: October 30, 2000Date of Patent: September 9, 2003Assignee: Knoll AktiengesellschaftInventors: Clifford James Bailey, Robert Brian Jones, Helen Christine Jackson
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Publication number: 20030166732Abstract: The invention relates to the use of ambroxol and the pharmacologically acceptable salts thereof for preparing a pharmaceutical composition for the treatment of painful conditions in the oral and pharyngeal cavity.Type: ApplicationFiled: February 27, 2003Publication date: September 4, 2003Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Anke Esperester, Uwe Pschorn, Jean-Michel Vix
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Publication number: 20030162817Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.Type: ApplicationFiled: October 11, 2002Publication date: August 28, 2003Applicant: Tularik Inc.Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
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Patent number: 6608054Abstract: The present invention relates to novel pharmaceutical compositions based on anticholinergics and endothelin antagonists, processes for preparing them and their use in the treatment of respiratory tract diseases.Type: GrantFiled: March 18, 2002Date of Patent: August 19, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Christopher J. M. Meade, Michel Pairet, Michael P. Pieper
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Publication number: 20030095992Abstract: A method for modifying at least one non-ester-containing parent compound, and the compounds produced using such method, which compounds are deployed to temporarily incapacitate at least one subject are disclosed. The modified compounds are rapidly metabolized to inactive and non-toxic metabolites when exposure to the modified compounds is halted.Type: ApplicationFiled: November 18, 2002Publication date: May 22, 2003Inventor: Paul W. Erhardt
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Patent number: 6562859Abstract: A method of using a ureido derivative of a poly-4-amino-2-carboxy-1-methyl pyrrole or a pharmaceutically acceptable salt thereof to inhibit inflammation, particularly non-TNF-&agr; dependent inflammation, in a mammal.Type: GrantFiled: August 4, 2000Date of Patent: May 13, 2003Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: O. M. Zack Howard, Joost J. Oppenheim, William J. Murphy, Edward A. Sausville
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Publication number: 20030083380Abstract: A composition comprising an amphoteric or pseudo-amphoteric agent and a polyhydroxy alpha hydroxyacid existing as a free acid, lactone, or salt, and isomeric or non-isomeric forms thereof is provided. The amphoteric or pseudo-amphoteric agent can be selected from amino acids, dipeptides, aminoaldonic acid, aminouronic acid, lauryl aminoproplyglycine, aminoaldaric acid, neuraminic acid desulfated heparin, deacetylated hyaluronic acid, hyalobiuronic acid, chondrosine, deacetylated chondroitin, creatine, creatinine, hydroxyproline, homocysteine, homocystine, homoserine, ornithine, citrulline, phosphatidylserine, and sphingomyelin. The composition may contain other additives, including cosmetic or pharmaceutical agents for topical treatment of dermatological disorders.Type: ApplicationFiled: December 6, 2000Publication date: May 1, 2003Inventors: Ruey J. Yu, Eugene J. Van Scott
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Patent number: 6555540Abstract: This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or said prodrug and a selective COX-2 inhibitor, a prodrug thereof or a pharmaceutically acceptable salt of said selective COX-2 inhibitor or said prodrug. This invention further relates to methods of using those pharmaceutical compositions for the treatment of diabetic complications such as diabetic neuropathy, diabetic nephropathy, diabetic retinopathy and diabetic cardiomyopathy.Type: GrantFiled: June 23, 2000Date of Patent: April 29, 2003Assignee: Pfizer IncInventor: Banavara L. Mylari
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Publication number: 20030073671Abstract: Novel non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.Type: ApplicationFiled: July 31, 2002Publication date: April 17, 2003Inventor: Timothy Mark Willson
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Publication number: 20030060457Abstract: The invention relates to the identification of cdk inhibitors as inhibitors of gene expression, replication and reactivation in pathogenic agents.Type: ApplicationFiled: December 6, 2000Publication date: March 27, 2003Inventors: Priscilla A. Schaffer, Luis M. Schang
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Patent number: 6525091Abstract: Substituted diarylureas, pharmaceutical compositions containing them, and their use for stimulating Fas-mediated apoptosis. The compounds, as single stereoisomers or mixtures of stereoisomers, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them, are useful in methods of treating autoimmune diseases, infectious diseases, and malignancies.Type: GrantFiled: February 22, 2002Date of Patent: February 25, 2003Assignee: Telik, Inc.Inventors: Louise Robinson, Hugo O. Villar
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Patent number: 6521663Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.Type: GrantFiled: October 5, 2001Date of Patent: February 18, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Wenxi Pan, Tianbao Lu, Thomas P. Markotan, Bruce E. Tomczuk
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Patent number: 6518310Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: March 16, 2001Date of Patent: February 11, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
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Patent number: 6489134Abstract: This invention provides novel compounds derived from a marine sponge, Adocia sp., that specifically modulat kinesin activity by targeting the kinesin motor domain and mimicking the activity a microtubule. The compounds act as potent anti-mitogens are useful in a wide variety of in vitro and in vivo applications.Type: GrantFiled: November 28, 2000Date of Patent: December 3, 2002Assignee: The Regents of the University of CaliforniaInventors: Lawrence S.B. Goldstein, David John Faulkner, Roman Sakowicz, Michael S. Berdelis, Christine L. Blackburn, Cordula Hopmann
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Publication number: 20020165275Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.Type: ApplicationFiled: January 25, 2002Publication date: November 7, 2002Inventors: Yong-Qian Wu, Sergei Belyakov, Gregory S. Hamilton, David Limburg, Joseph P. Steiner, Mark Vaal, Ling Wei, Douglas Wilkinson
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Publication number: 20020143036Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: ApplicationFiled: October 5, 2001Publication date: October 3, 2002Applicant: Tularik Inc.Inventors: John A Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
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Patent number: 6448251Abstract: A composition and method for treating both superficial and subdermal inflammation is taught by treating an inflamed skin area, muscle, or bone joint, with a therapeutically effective amount of a skin-compatible ester of a zwitterionic aminosulphonic acid (ZASA-Ester) of the formula. ROCH2—CH2—N N—CH2CH2 SO3M wherein M is an alkali metal, like sodium, and R is a naturally occurring, straight-chain, saturated or unsaturated, aliphatic acid moiety, selected from one of the groups consisting of alkanes, alkenes, and alkadienes, each having a hydrocarbon chain of from one to twenty carbon atoms. The resulting HEPES esters are represented by the acetic acid ester as an exemplary alkane, the oleic acid ester as a exemplary alkene, and the linoleic acid ester as an exemplary alkadiene, the esters of which form fatty acids in nature. The most useful of which are the acetic oleic (cis isomer), linoleic, palmitic, and stearic moieties; they occur naturally as glycerides, i.e., esters of glycerol.Type: GrantFiled: July 27, 2000Date of Patent: September 10, 2002Inventors: Peter T. Pugliese, Peter M. Pugliese
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Patent number: 6440938Abstract: The present invention relates to the use of an inhibitor of cysteine proteinase activity in conjunction with an inhibitor of any serine proteinase activity other than trypsin for the manufacture of a medicament for the prevention or treatment of a condition in which an allergen traverses an epithelial barrier such as asthma. Also included in the invention are formulations and kits containing serine and cysteine proteinase inhibitors and their use in the prevention or treatment of conditions in which an allergen traverses an epithelial barrier.Type: GrantFiled: August 10, 2000Date of Patent: August 27, 2002Assignee: The Victoria University of ManchesterInventors: David R. Garrod, Clive Robinson
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Patent number: 6432427Abstract: Cosmetic methods and compositions containing selected substituted sulfonamide aromatic compounds. The inventive compositions provide control of sebum secretion from sebocytes, improved oil control and improved feel, and prevent shine and stickiness.Type: GrantFiled: June 1, 2001Date of Patent: August 13, 2002Assignee: Unilever Hope & Personal Care USA, division of Conopco, Inc.Inventors: John Steven Bajor, David Joseph Pocalyko
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Patent number: 6414020Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: May 9, 2001Date of Patent: July 2, 2002Assignee: 3- Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Patent number: 6403643Abstract: A method for the use of 2,5-dihydroxybenzenesulfonic derivatives for normalizing endothelial function is disclosed. Preferred 2,5-dihydroxybenzenesulfonic derivatives are calcium dobesilate, ethamsylate and persilate.Type: GrantFiled: July 26, 2000Date of Patent: June 11, 2002Assignee: Laboratories del Dr. Esteve, S.A.Inventor: Jose Esteve-Soler
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Publication number: 20020061927Abstract: Methods of treating a person suffering from HIV protease inhibitor-induced metabolic disorders such as lipodystrophy, hypertriglyceridemia, insulin resistance, hyperglycemia, diabetes and ketoacidosis, comprise treatment with an insulin receptor activating compound, optionally in conjunction with insulin. In general, any insulin receptor activating compound is suitable for the practice of the invention; and preferred compounds are disclosed.Type: ApplicationFiled: October 11, 2001Publication date: May 23, 2002Inventors: Prasad V.V.S.V. Manchem, Robert T. Lum, Steven R. Schow
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Publication number: 20020040043Abstract: There is provided compounds of formula I, 1Type: ApplicationFiled: April 23, 2001Publication date: April 4, 2002Inventor: Thomas Antonsson
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Patent number: 6365625Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.Type: GrantFiled: September 17, 1999Date of Patent: April 2, 2002Assignee: Procept, Inc.Inventors: Shyam K. Singh, Raymond J. Patch, Peter V. Pallai, Edith A. Neidhardt, Gerard P. Palace, Kevin J. Willis, Theresa M. Sampo, Kevin W. McDonald, Zhan Shi
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Patent number: 6337327Abstract: The invention relates to pharmaceutical compositions comprising an aldose reductase inhibitor and an ACE inhibitor, and their use in the treatment of diabetic complications such as diabetic neuropathy, diabetic retinopathy and diabetic nephropathy.Type: GrantFiled: January 7, 2000Date of Patent: January 8, 2002Assignee: Zeneca LimitedInventors: David Patrick Tuffin, Frank Carey, Mary Anne Cotter, Norman Eugene Cameron
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Patent number: 6316484Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: August 7, 2000Date of Patent: November 13, 2001Assignee: Tularik Inc.Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
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Patent number: 6306858Abstract: Methods for treating muscular inflammation comprise applying to an inflamed area a therapeutically effective amount of a skin-compatible ester of a zwitterionic aminosulphonic acid of the formula wherein M is an alkali metal and R is a straight chain aliphatic acid moiety. Compositions for treating inflammation comprising a therapeutically effective amount of a skin-compatible component comprising an ester, ether, urethane, amide or urea of at least one compound selected from a specified group. Additional methods for treating inflammation comprise applying to an inflamed area a therapeutically effective amount of a skin-compatible component comprising an ester, ether, urethane, amide or urea of at least one compound selected from a specified group.Type: GrantFiled: May 26, 2000Date of Patent: October 23, 2001Inventors: Peter T. Pugliese, Peter M. Pugliese
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Patent number: 6255517Abstract: The present invention relates to a thymol derivative represented by following Chemical Formula 1, pharmaceutically acceptable salts or esters thereof, and anti-cancer agents comprising the same as an active ingredient.Type: GrantFiled: October 14, 1999Date of Patent: July 3, 2001Inventors: Ok Pyo Zee, Young Hoon Jung, Kang Ro Lee, Hyung In Moon, Hyung Geun Baek, Min Jung Lee, Dae Keun Kim