C=o Bonded Directly To The Six-membered Hetero Ring Patents (Class 514/354)
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Patent number: 6605624Abstract: A class of substituted pyridines that are useful for inhibiting the activity of cholesteryl ester transfer protein, and have the structural formula (IA), wherein R2, R3, R4, R5, and R6 are defined in the claims.Type: GrantFiled: December 11, 2000Date of Patent: August 12, 2003Assignee: Pharmacia CorporationInventors: Len F. Lee, Kevin C. Glenn, Daniel T. Connolly, David G. Corley, Daniel L. Flynn, Ashton T. Hamme, Shridhar G. Hegde, Michele A. Melton, Roger J. Schilling, James A. Sikorski, Nancy N. Wall, Jeffery A. Zablocki
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Patent number: 6605625Abstract: Ortho, meta-substituted bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters. Compounds of the invention include compounds of the formula I in which: A1, A2, A3, A4, A5, A6, A7 and A8 independently of one another are chosen from nitrogen, CH and CR(5), at least four of these groups being CH, and wherein all other variables are as defined here.Type: GrantFiled: November 29, 2001Date of Patent: August 12, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleemann
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Publication number: 20030144276Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): 1Type: ApplicationFiled: January 6, 2003Publication date: July 31, 2003Applicant: Eisai Co. Ltd.Inventors: Kouichi Kikuchi, Katsuya Tagami, Hiroyuki Yoshimura, Shigeki Hibi, Mitsuo Nagai, Shinya Abe, Makoto Okita, Takayuki Hida, Seiko Higashi, Naoki Tokuhara, Seiichi Kobayashi
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Patent number: 6599890Abstract: A compound of the formula wherein R1, R2 R3, R4 R5, R6, R7, R8, R9 and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.Type: GrantFiled: November 8, 2000Date of Patent: July 29, 2003Assignee: Pfizer IncInventors: Kim F. McClure, Mark C. Noe, Michael A. Letavic, Louis S. Chupak
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Publication number: 20030139370Abstract: Compositions are provided, which comprise at least one nucleoside analogue inhibitor, pharmaceutically acceptable salts, solvates, or prodrugs thereof and fusaric acid, derivatives, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising the above compositions are also provided that optionally further include another therapeutically effective compound, such as a carrier. Systemic and topical preparations comprising the above compositions are also provided as well as methods of treating viral diseases by the administration of the above antiviral agents to a patient.Type: ApplicationFiled: December 3, 2002Publication date: July 24, 2003Inventors: Michael G. Douglas, Avinash N. Amin
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Patent number: 6596752Abstract: The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.Type: GrantFiled: July 12, 2002Date of Patent: July 22, 2003Assignees: Tanabe Seiyaku Co., Ltd., Pharmacia & Upjohn CompanyInventors: Thomas J. Lobl, Bradley R. Teegarden, Alexander Polinsky, Gilbert M. Rishton, Masafumi Yamagishi, Steven Tanis, Jed F. Fisher, Edward W. Thomas, Robert A. Chrusciel
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Publication number: 20030133966Abstract: Non-absorbent articles are disclosed. The non-absorbent articles include an effective amount of an aromatic inhibitory compound to substantially inhibit the production of exotoxins by Gram positive bacteria.Type: ApplicationFiled: October 2, 2001Publication date: July 17, 2003Applicant: Kimberly-Clark Worldwide, Inc.Inventors: Rae Ellen Syverson, Richard A. Proctor
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Publication number: 20030130320Abstract: Phenylalanine derivatives of the following formulae and analogues thereof have an antagonistic activity to &agr;4 integrin. They are used as therapeutic agents for various diseases concerning &agr;4 integrin.Type: ApplicationFiled: September 23, 2002Publication date: July 10, 2003Applicant: AJINOMOTO CO. INCInventors: Nobuyasu Suzuki, Toshihiko Yoshimura, Hiroyuki Izawa, Shingo Makino, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
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Publication number: 20030129212Abstract: A compound of formula 1Type: ApplicationFiled: October 15, 2002Publication date: July 10, 2003Inventor: Andreas Herrmann
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Publication number: 20030125360Abstract: The present invention is directed to carbocyclic hydrazino compounds that function as inhibitors of copper-containg amine oxidases commonly known as semicarbazide-sensitive amine oxidases (SSAO), including the human SSAO known as Vascular Adhesion Protein-I (VAP-1). These SSAO inhibitors have therapeutic utility as drugs to treat conditions and diseases including, but not limited to, a number of inflammatory conditions and diseases (in particular chronic inflammatory conditions such as chronic arthritis, inflammatory bowel diseases, and chronic skin dermatoses), diseases related to carbohydrate metabolism and to aberrations in adipocyte differentiation or function and smooth muscle cell function, and vascular diseases.Type: ApplicationFiled: July 12, 2001Publication date: July 3, 2003Applicant: Biotie Therapies Corp.Inventors: David John Smith, Ferenc Fulop, Marjo Pihlavisto, Laszlo Lazar, Sakari Alaranta, Petri Vainio, Zsolt Szakonyi
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Publication number: 20030119877Abstract: A compound of the formula (I), wherein R1 is hydrogen, halogen, carbymoyl, cyano, formuly, or lower alkyl optionally substituted with halogen, amino or a protected amino, R2 is hydrogen, halogen, cyano or lower alkoxy, R3 is phenyl or pyridyl, each of which is substituted with lower alkoxy, and R4 is lower alkoxy; provided that either R1 or R2 is hydrogen, then the other is other than hydrogen, or its salts, which are useful as a medicament.Type: ApplicationFiled: August 16, 2002Publication date: June 26, 2003Inventors: Junya Ishida, Hirofumi Yamamoto, Nobukiyo Konishi, Masataka Morita, Katsuya Nakamura, Susumu Miyata, Takehiro Ochi, Yoshiaki Morita, Eiji Yoshimi, Kanae Kuroda
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Patent number: 6579891Abstract: An antiproliferative, antiinflammatory, antiinfective, immunization agent of a metal ion chelating agent such as picolinic acid or derivatives thereof, and methods of using the same. The agents chelate metals in metal containing protein complexes and enzymes required for growth, replication or inflammatory response. The preparations can be administered systemically or for topical use. The preparations have antineoplastic, antiviral, antiinflammatory, analgesic antiangiogenic and antiproliferative effects and are used in the treatment of warts, psoriasis, acne, skin cancers, sunburn, inflammatory responses, untoward angiogenesis and other diseases and in the prevention of sexually transmitted diseases such as genital warts, herpes and AIDS.Type: GrantFiled: September 8, 2000Date of Patent: June 17, 2003Assignee: Novactyl, Inc.Inventor: Jose A. Fernandez-Pol
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Publication number: 20030105142Abstract: The invention concerns amide derivatives of formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q1 is heteroaryl which is optionally substituted with 1, 2, 3, or 4 substituents such as hydroxy, halogeno, trifluoromethyl, (1-6C)alkyl, (1-6C)alkoxy, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, amino-(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, heteroaryl and heterocyclyl; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and Q2 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: July 11, 2002Publication date: June 5, 2003Applicant: ASTRAZENECA ABInventors: Dearg S. Brown, George R. Brown
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Patent number: 6572848Abstract: Agonists of chlorine/potassium channel receptor, for example taurine, gamma-aminobutyric acid (GABA), isoguvacin, isonipecotic acid, 4,5,6,7-tetrahydroisoxazolo-(5,4-c)pyrid-3(2H)-one, a benzodiazepine, steroids, and cromakalim, pinacidil, nicorandil and minoxidil, are well suited for treating sensitive human skin and are especially useful for treating/eliminating skin itching, pruritus, tautness, tingling and/or erythema.Type: GrantFiled: April 28, 2000Date of Patent: June 3, 2003Assignee: Societe L'Oreal S.A.Inventors: Lionel Breton, Olivier De Lacharriere, Isabelle Nonotte
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Patent number: 6569864Abstract: Compositions and kits comprising acyclovir and fusaric acid are provided.Type: GrantFiled: July 11, 2001Date of Patent: May 27, 2003Assignee: Novactyl, Inc.Inventors: Michael G. Douglas, Avinash N. Amin
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Publication number: 20030096847Abstract: Amide compounds of the formula: 1Type: ApplicationFiled: November 1, 2002Publication date: May 22, 2003Applicant: Fujisawa Pharmaceutical Co. Ltd.Inventors: Akira Yamada, Satoshi Aoki
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Patent number: 6566375Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.Type: GrantFiled: April 26, 2001Date of Patent: May 20, 2003Assignee: WyethInventor: Thomas J. Commons
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Publication number: 20030092744Abstract: The invention discloses novel compounds of the pyridinium series useful for the management of diabetes and aging-related vascular complications, including kidney disease, nerve damage, atherosclerosis, retinopathy, dermatological disorders and discoloration of teeth, by breaking preformed AGE, of the general formula I, or pharmaceutically acceptable salts thereof, 1Type: ApplicationFiled: August 9, 2002Publication date: May 15, 2003Applicant: TORRENT PHARMACEUTICALS LTD.Inventor: Alangudi Sankaranarayanan
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Patent number: 6562848Abstract: This invention relates generally to bis-amino acid sulfonamides containing substituted benzyl amines of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as assay standards or reagents, and intermediates and processes for making the same.Type: GrantFiled: September 18, 2002Date of Patent: May 13, 2003Assignee: Bristol-Myers Squibb CompanyInventor: Robert F. Kaltenbach
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Patent number: 6559186Abstract: Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an &agr;-1-adrenergic antagonist, &agr;-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.Type: GrantFiled: August 5, 1994Date of Patent: May 6, 2003Assignee: Arc 1, Inc.Inventor: James N. Campbell
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Patent number: 6548521Abstract: Compositions and methods for treating a patient infected with a metazoan parasite by inhibiting the enzymatic action of the metazoan parasite protease, wherein there is employed at least one compound of formula I A—X—B wherein A is a substituted or unsubstituted homoaromatic or heteroaromatic ring system comprising one to three rings which binds to at least one of the S2, S1 and S1′ subsites; B is a substituted or unsubstituted homoaromatic or heteroaromatic ring system comprising one to three rings which binds to at least one of the S1′, S1 and S2 subsites; and X is —C═C—C(═O)—. These compositions and methods have particular utility in the treatment of schistosomiasis, malaria, and other infectious diseases.Type: GrantFiled: July 28, 2000Date of Patent: April 15, 2003Assignee: The Regents of the University of CaliforniaInventors: Fred Ehrenkranz Cohen, James Hobson McKerrow, Christine Sun Ring, Philip Jon Rosenthal, George Lommel Kenyon, Zhe Li
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Publication number: 20030069284Abstract: Aryl- and heteroaryl-substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed.Type: ApplicationFiled: March 1, 2002Publication date: April 10, 2003Inventors: Kathleen S. Keegan, Edward A. Kesicki, John Joseph Gaudino, Adam Wade Cook, Scott Douglas Cowen, Laurence Edward Burgess
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Publication number: 20030064977Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: ApplicationFiled: March 8, 2002Publication date: April 3, 2003Applicant: Vertex Pharmaceuticals, Inc.Inventors: Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti
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Publication number: 20030065011Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I.Type: ApplicationFiled: October 30, 2001Publication date: April 3, 2003Applicant: Merck Frosst Canada & Co.Inventors: Daniel Dube, Rejean Fortin, Richard Friesen, Zhaoyin Wang, Jacques Yves Gauthier
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Patent number: 6541505Abstract: This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.Type: GrantFiled: June 30, 2000Date of Patent: April 1, 2003Assignee: Aventis Pharmaceuticals Inc.Inventors: William P. Dankulich, Daniel G. McGarry, Christopher Burns, Timothy F. Gallagher, Francis A. Volz
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Publication number: 20030060491Abstract: The invention relates to novel bicyclic aromatic compounds which have the general formula (I): 1Type: ApplicationFiled: September 24, 2002Publication date: March 27, 2003Inventor: Jean-Michel Bernardon
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Patent number: 6537991Abstract: The invention provides methods for treating and preventing neuropathic pain which comprise the administration of an effective amount of an antagonist of the pain-enhancing effects of E-type prostaglandins, for example, EP1-typo prostaglandin receptor antagonists, to warm-blooded animals including humans in need of such treatment. The invention also provides pharmaceutical compositions for such prevention and treatment of neuropathic pain.Type: GrantFiled: November 15, 2001Date of Patent: March 25, 2003Assignee: AstraZeneca ABInventors: John S Shaw, William Bastain
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Patent number: 6534513Abstract: Phenylalkanoic acid derivatives of formula (1) are described: wherein Ar1 is an aromatic or heteroaromatic group; L1 is a covalent bond or a linker atom or group; A is an optionally substituted aliphatic, heteroaliphatic, cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha 4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: September 29, 1999Date of Patent: March 18, 2003Assignee: Celltech R&D LimitedInventors: John Robert Porter, Graham John Warrellow, Sarah Catherine Archibald, John Clifford Head
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Patent number: 6534536Abstract: Alkylsulfonamido heterocyclic thrombin inhibitors are provided which have the structure wherein G is wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; R is hydrogen, hydroxyalkyl, aminoalkyl, alkyl, cycloalkyl, amidoalkyl, arylalkyl, alkenyl, aryl, alkynyl, arylalkoxyalkyl, or an amino acid side chain; R1 and R2 are independently hydrogen, lower alkyl, cycloalkyl, aryl, hydroxy, alkoxy, oxo, thioketal, thioalkyl, thioaryl, amino or alkylamino; or R1 and R2 can be taken together with the carbons to which they are attached to form a cycloalkyl, aryl or heteroaryl ring.Type: GrantFiled: March 16, 1994Date of Patent: March 18, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Spencer D. Kimball, Jagabandhu Das, Wan Fang Lau
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Publication number: 20030049212Abstract: The present invention relates to a topical skin care composition having improved aesthetics containing a skin care active wherein the skin care active is soluble in a tacky solvent and wherein the dermatologically acceptable delivery system contains a tacky solvent in combination with a silicone elastomer and a carrier for the elastomer. The present invention also relates to methods of using such compositions to regulate the condition of mammalian skin while retaining good aesthetics.Type: ApplicationFiled: April 25, 2002Publication date: March 13, 2003Applicant: The Procter & Gamble CompanyInventors: Larry Richard Robinson, Robert Bao Kim Ha, Jorge Max Sunkel, Michael Lee Vatter
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Patent number: 6531485Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: December 16, 1999Date of Patent: March 11, 2003Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Paul A. DaSilva-Jardine
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Publication number: 20030045461Abstract: This invention is directed to the use of novel methods and nitroxide compositions having high redox activity to treat diseases and conditions related to free radicals. The compositions and methods described include pro-drug forms of nitroxide that enhance the therapeutic effect through their ability to penetrate readily into skin cells and remain sequestered within the cells. The formulations and methods described herein result in a significant accumulation of nitroxides in the skin cells, thus achieving a targeted delivery of a therapeutic or diagnostic dose. Applications using the novel compositions and methods described herein include use as improved imaging agents and as improved topical agents for treating conditions of the skin, including aging of the skin, wrinkles caused by sun-exposure, skin cancer, burns, psoriasis and alopecia, among others.Type: ApplicationFiled: September 6, 2001Publication date: March 6, 2003Inventors: Jen-Chang Hsia, Li Ma
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Patent number: 6528531Abstract: Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.Type: GrantFiled: November 10, 2000Date of Patent: March 4, 2003Assignee: Merck & Co., Inc.Inventors: Tesfaye Bitfu, Danqing D. Feng, Gui-Bai Liang, Mitree M. Ponpipom, Xiaoxia Qian, Michael H. Fisher, Matthew J. Wyvratt, Robert L. Bugianesi
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Patent number: 6525099Abstract: The present invention provides certain N-substituted sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: GrantFiled: January 23, 2001Date of Patent: February 25, 2003Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6521626Abstract: Compounds of formula (1): wherein R1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain; L1 is a linker atom or group; r and s is each zero or an integer 1; R2 and R3, which may be the same or different, is each a hydrogen or halogen atom or a straight or branched alkyl, haloalkyl, alkoxy, haloalkoxy, hydroxyl or nitro group; Alk2 is a straight or branched alkylene chain; m is zero or an integer 1; R4 is a hydrogen atom or a methyl group; R5 is a hydrogen atom or a straight or branched alkyl group; R6 is a group —(CH2)tR7 in which t is zero or the integer 1 and R7 is an optionally substituted polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates and hydrates theType: GrantFiled: March 23, 1999Date of Patent: February 18, 2003Assignee: Celltech R&D LimitedInventors: Sarah Catherine Archibald, John Clifford Head, Graham John Warrellow, John Robert Porter
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Patent number: 6521643Abstract: A compound of formula (I) wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NOS(nitric oxide synthasey)-mediated diseases such as adult respiratory distress syndrome, myocarditis, synovitis, septic shock, insulin-ependent diabetes mellitus, ulcerative colitis, cerebral infarction, rheumatoid arthritis, osteoarthritis, osteoporosis, systemic lupus erythematosus, rejection by organ transplantation, asthma, pain, ulcer, and the like in human being and animals.Type: GrantFiled: August 17, 2001Date of Patent: February 18, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaki Tomishima, Kazuhiko Take
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Publication number: 20030032660Abstract: Novel compounds of the pyridinium series useful for the management of diabetes and aging-related vascular and neurovascular complications, including kidney disease, nerve damage, atherosclerosis, retinopathy, inflammatory disorders, immunological disorders, oxidative stress, dermatological disorders and discoloration of teeth, by breaking preformed AGE, of the general formula I, or pharmaceutically acceptable salts thereof, 1Type: ApplicationFiled: August 28, 2001Publication date: February 13, 2003Applicant: TORRENT PHARMACEUTICALS LTD.Inventor: Alangudi Sankaranarayanan
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Patent number: 6514999Abstract: With an agent for preparing a medication for treating the symptoms of Parkinson's disease, one obtains more effective treatment of the symptoms of said disease compared to classical treatment by a combination of effective substances comprising a substance increasing dopamine concentration in the synaptic cleft of the neurons of the brain along with a local anesthetic of the anilide group.Type: GrantFiled: August 8, 2001Date of Patent: February 4, 2003Inventor: Lothar Saiger
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Patent number: 6515134Abstract: It is an objective to produce intermediates of optically active beta-3 adrenaline receptor agonists from readily available raw materials in a safe, efficient and industrially advantageous manner. A substituted acetylpyridine derivative represented by the general formula (9) is reduced by enantioselective reduction to produce an optically active hydroxyethyl derivative represented by the general formula (10) (wherein * represents an asymmetric carbon atom), and it is further derivatized to an intermediate of an optically active beta-3 adrenaline receptor agonist, such as an optically active dihydroxyethylpyridine derivative represented by the general formula (14) or an optically active oxirane derivative represented by the general formula (16).Type: GrantFiled: November 7, 2001Date of Patent: February 4, 2003Assignee: Kaneka CorporationInventors: Susumu Amano, Naoaki Taoka, Masaru Mitsuda, Kenji Inoue
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Patent number: 6511990Abstract: The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.Type: GrantFiled: August 24, 2000Date of Patent: January 28, 2003Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New YorkInventors: Ronald Breslow, Sandro Belvedere, Leland Gershell, Thomas A. Miller, Paul A. Marks, Victoria M. Richon, Richard A. Rifkind
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Patent number: 6511988Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: GrantFiled: August 10, 2001Date of Patent: January 28, 2003Assignee: Isotechnika Inc.Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
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Publication number: 20030013746Abstract: The instant invention provides compositions and methods for modeling post-Amadori AGE formation and the identification and characterization of effective inhibitors of post-Amadori AGE formation, and such identified inhibitor compositions.Type: ApplicationFiled: August 8, 2002Publication date: January 16, 2003Applicant: University of Kansas Medical Center.Inventors: Billy G. Hudson, Parvin Todd, Raja Gabriel Khalifah, Aaron Ashley Booth
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Patent number: 6506780Abstract: This invention relates to a series of substituted benzophenone and sulfone compounds of the formula I wherein ring A, Z, Y, R and X are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.Type: GrantFiled: July 2, 2001Date of Patent: January 14, 2003Assignee: Pfizer Inc.Inventor: John A. Lowe, III
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Publication number: 20030008895Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: ApplicationFiled: December 16, 1999Publication date: January 9, 2003Inventors: KIMBERLY O CAMERON, PAUL A. DASILVA-JARDINE
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Patent number: 6503948Abstract: A method for treating an organ donor prior to harvesting organ to reduce graft rejection in a recipient. An amount effective to reduce graft rejection of at least one compound selected from the group consisting of compounds having formulas I, II, III, IV, V, VI, and VII is administered to the organ donor: wherein Y is X is F or Cl; and the remaining groups are as defined in the specification.Type: GrantFiled: April 17, 2002Date of Patent: January 7, 2003Assignee: Southern Research InstituteInventors: Herbert M. Blatter, Donald R. Kahn, James R. Piper, John A. Secrist, III, Robert F. Struck, Carroll Temple
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Publication number: 20030004189Abstract: Disclosed are nicotinanilide-N-oxide compounds, methods for their production, pharmaceutical compositions which include these compounds, and methods for their use in various therapies.Type: ApplicationFiled: December 12, 2001Publication date: January 2, 2003Applicant: Darwin Discovery Ltd.Inventors: Neil S. Cutshall, Kraig M. Yager
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Publication number: 20020198207Abstract: Compounds of the formula 1Type: ApplicationFiled: May 22, 2002Publication date: December 26, 2002Inventors: John Charles Kath, Matthew Frank Brown, Christopher Stanley Poss
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Publication number: 20020198156Abstract: The present invention provides methods for the asymmetric synthesis of (S,S,R)-(−)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: 1Type: ApplicationFiled: March 19, 2002Publication date: December 26, 2002Inventors: William G. Bornmann, Francis Sirotnak, Howard Scher, Ephraim Vidal, Christopher Borella, David Scheinberg
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Publication number: 20020198240Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: ApplicationFiled: April 29, 2002Publication date: December 26, 2002Inventors: James A. Shayman, Norman S. Radin
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Publication number: 20020193412Abstract: There is disclosed a genus of compounds and pharmaceutical compositions that are protective for mitigating damage associated with tissue ischemia, particularly stroke (CNS ischemia), and ischemia of the myocardium. The present invention further provides a method for treating tissue damage caused by ischemia. Lastly, the present invention provides a method for treating tissue damage caused by providing a compound that inhibits the cytotoxic activity of 3-aminopropanal.Type: ApplicationFiled: May 7, 2002Publication date: December 19, 2002Inventors: Kevin J. Tracey, Yousef Al-Abed, Svetlana Ivanova, Richard J. Bucala