C=o Bonded Directly To The Hetero Ring (x Is Chalcogen) Patents (Class 514/448)
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Patent number: 6492412Abstract: 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: June 29, 2001Date of Patent: December 10, 2002Assignee: Pfizer, Inc.Inventors: Kimberly O. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L. Rosati, David D. Thompson
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Patent number: 6492362Abstract: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: September 15, 2000Date of Patent: December 10, 2002Assignee: Axys Pharmaceuticals, Inc.Inventors: Michael Graupe, John O. Link, John W. Patterson, Sheila Zipfel
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Patent number: 6482846Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: August 30, 2001Date of Patent: November 19, 2002Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6482849Abstract: 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: June 23, 1998Date of Patent: November 19, 2002Assignees: 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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Patent number: 6476023Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions. Also disclosed are processes of making such compounds.Type: GrantFiled: November 20, 2000Date of Patent: November 5, 2002Assignee: Boehringen Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Eugene R. Hickey, John R. Regan
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Patent number: 6472433Abstract: This invention relates to the use of enantiomerically pure R-NSAIDs for the treatment of inflammation. Preferably, the R-NSAID used is R-flurbiprofen and is administered in a dose of at least 5 milligrams per kilogram of body weight per day. The anti-inflammatory action of R-NSAIDs is due to their ability to interfere with the biosynthesis of COX-2 by inhibiting COX-2 mRNA synthesis, rather than by just blocking the action of the enzyme itself. In order to effect the inhibition of COX-2 mRNA synthesis, the R-NSAID must be present at relatively high doses. Because the R-NSAID is selective in its action, that is, it does not inhibit either COX-1 mRNA synthesis or the COX-1 enzyme itself, it can be administered in the required high doses because the tissue protective effects of prostaglandins made through the COX-1 pathway are not interfered with.Type: GrantFiled: March 1, 2001Date of Patent: October 29, 2002Assignee: Loma Linda University Medical CenterInventor: William J. Wechter
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Patent number: 6465445Abstract: Novel methods for the medical treatment and/or inhibition of the development of osteoporosis, breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure: and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3&bgr;,17&bgr;-diol and compounds converted in vivo to one of the foregoing presursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursor is disclosed for the medical treatment and/or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.Type: GrantFiled: June 11, 1998Date of Patent: October 15, 2002Assignee: Endorecherche, Inc.Inventor: Fernand Labrie
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Publication number: 20020137750Abstract: There are provided novel compounds of formula (I) 1Type: ApplicationFiled: February 27, 2001Publication date: September 26, 2002Inventors: D.W. Chen Deborah, James R. Empfield, James E. Macdonald, Kenneth C. Mattes, Robert Murray, Eifion Phillips, Hans Schmitthenner
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Patent number: 6455520Abstract: The invention concerns amide derivatives of formula (I) wherein R3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R1 and R2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R4 is a basic group such as amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, di-[(1-6C)alkyl]amino-(1-6C)alkyl, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, heteroaryl, heteroaryloxy, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; and Q2 is a group such as heteroaryl, heteroaryloxy or heteroaryl-(1-6C)alkoxy which is optionally substituted; 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: GrantFiled: March 23, 2001Date of Patent: September 24, 2002Assignee: Astra Zeneca ABInventors: Dearg S Brown, George R Brown
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Publication number: 20020132833Abstract: This invention provides novel compounds that are effective as inhibitors of caspase and cellular apoptosis. The invention also provides methods for using the compounds to treat caspase-mediated diseases in mammals.Type: ApplicationFiled: April 3, 2001Publication date: September 19, 2002Inventors: Julian M.C. Golec, Paul Charifson, Guy Brenchley
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Patent number: 6448290Abstract: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is —COR1, —CH═CH—COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4). The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.Type: GrantFiled: June 18, 1999Date of Patent: September 10, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Yuuki Nagao
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Patent number: 6441023Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflmatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.Type: GrantFiled: July 3, 2001Date of Patent: August 27, 2002Assignee: American Home Products CorporationInventors: Aranapakam Mudumbai Venkatesan, Jannie Lea Baker, Jeremy Ian Levin
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Patent number: 6436993Abstract: In accordance with the present invention, it has been discovered that retinoic acid receptor (RAR) antagonists are capable of modulating processes mediated by other members of the steroid/thyroid hormone receptor superfamily, including permissive receptors such as PPARs (e.g., PPAR&agr;, PPAR&dgr; and PPAR&ggr;). Indeed, it has been discovered that RAR antagonists, in combination with agonists for members of the steroid/thyroid hormone receptor superfamily, are capable of inducing and/or enhancing processes mediated by such members.Type: GrantFiled: July 13, 1999Date of Patent: August 20, 2002Assignee: The Salk Institute for Biological StudiesInventors: Ronald M. Evans, Peter J. Tontonoz, Laszlo Nagy
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Patent number: 6429317Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.Type: GrantFiled: September 5, 2000Date of Patent: August 6, 2002Assignee: Eli Lilly and CompanyInventors: Sean P. Hollinshead, Michael A. Staszak, John S. Ward, Joseph W. Wilson, Bret E. Huff, Philip F. Hughes, Jose S. Mendoza, Charles H. Mitch
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Publication number: 20020103238Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: ApplicationFiled: March 12, 2002Publication date: August 1, 2002Inventors: Robert H. Chen, Min A. Xiang
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Patent number: 6426355Abstract: Compounds having the formula: wherein R1-R5, X and G are described herein and which are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.Type: GrantFiled: September 27, 2000Date of Patent: July 30, 2002Assignee: American Home ProductsInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Thomas Jones, Stanley Lang, Adma Ross, Eugene A. Terefenko, Bryan O'Hara
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Patent number: 6407100Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.Type: GrantFiled: September 1, 1993Date of Patent: June 18, 2002Assignee: Bayer AktiengesellschaftInventors: Hans Peter Isenring, Bettina Weiss
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Patent number: 6403615Abstract: This invention provides methods which are useful for the inhibition of the various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of formula I:Type: GrantFiled: September 29, 2000Date of Patent: June 11, 2002Assignee: Eli Lilly and CompanyInventor: George Joseph Cullinan
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Patent number: 6403810Abstract: This invention relates to new retinoic acid receptor selective retinoid agonists, to pharmaceutical compositions containing such compounds, and to the use of such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, for the treatment of emphysema and related pulmonary diseases.Type: GrantFiled: June 15, 2001Date of Patent: June 11, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Jean-Marc Lapierre
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Patent number: 6395719Abstract: The present invention is directed to increasing levels of acetylcholine by the administration of 2-aryl-3-aroylbenzo[b]thiophenes.Type: GrantFiled: November 14, 2000Date of Patent: May 28, 2002Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Michele Annette Glinn, Steven Marc Paul, Xin Wu
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Patent number: 6395769Abstract: This invention provides methods which are useful for the inhibition of the various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of formula I:Type: GrantFiled: May 12, 2000Date of Patent: May 28, 2002Assignee: Eli Lilly and CompanyInventor: George Joseph Cullinan
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Patent number: 6391912Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups and G, V, W, X, Y and Z are each as defined in the description, to processes and intermediates for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: June 29, 2001Date of Patent: May 21, 2002Assignee: Bayer AktiengesellschaftInventors: Hermann Hagemann, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Alan Graff, Wolfram Andersch
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Patent number: 6376502Abstract: 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: February 22, 2000Date of Patent: April 23, 2002Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
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Patent number: 6372779Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:Type: GrantFiled: December 28, 1998Date of Patent: April 16, 2002Assignee: Ortho Pharmaceutical CorporationInventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
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Patent number: 6365623Abstract: Active acne and acneiform scars are treated by topical application of a composition containing lipoic acid and/or a lipoic acid derivative such as dihydrolipoic acid, a lipoic or dihydrolipoic acid ester, a lipoic or dihydrolipoic acid amide, a lipoic or dihydrolipoic acid salt, and mixtures of any of these to reduce erythema, pore size, and scarring. Topical application of lipoic acid and/or a lipoic acid derivatives are advantageously used with at least one adjunct ingredient such as a retinoid, an antibiotic, or benzoyl peroxide conventionally used for acne, alone or in combination with dimethylaminoalcohol, an &agr;-hydroxy acid such as glycolic acid, a tyrosine, tocotrienol, and/or a fatty acid ester of ascorbic acid. One preferred embodiment contains a combination of lipoic acid, an &agr;-hydroxy acid, and dimethylaminoalcohol.Type: GrantFiled: December 30, 1999Date of Patent: April 2, 2002Inventor: Nicholas V. Perricone
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Patent number: 6355634Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.Type: GrantFiled: June 7, 1995Date of Patent: March 12, 2002Assignee: Bayer AktiengesellschaftInventors: Hans Peter Isenring, Bettina Weiss
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Patent number: 6353003Abstract: The current invention relates to a method for decreasing levels of homocysteine and/or C-reactive protein in humans comprising administering to a mammal in need thereof an effective amount of a compound of formula I: or a pharmaceutical salt or solvate thereof.Type: GrantFiled: May 3, 1999Date of Patent: March 5, 2002Assignee: Eli Lilly and CompanyInventor: Pamela Wang Anderson
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Patent number: 6350761Abstract: This invention is directed to benzenamine derivatives of formula (I): wherein A, W, m, n, R1, R2, R3, R4, R5 and R6 are defined herein. These compounds are useful as anti-coagulants.Type: GrantFiled: July 24, 2000Date of Patent: February 26, 2002Assignee: Berlex Laboratories, Inc.Inventors: William J. Guilford, Steven T. Sakata, Kenneth J. Shaw, Shung Wu, Wei Xu, Zuchun Zhao
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Publication number: 20020019438Abstract: This invention relates to new retinoic acid receptor selective retinoid agonists, to pharmaceutical compositions containing such compounds, and to the use of such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, for the treatment of emphysema and related pulmonary diseases.Type: ApplicationFiled: June 15, 2001Publication date: February 14, 2002Inventors: Michael Klaus, Jean-Marc Lapierre
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Publication number: 20020016322Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.Type: ApplicationFiled: August 27, 2001Publication date: February 7, 2002Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang
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Publication number: 20020002192Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: ApplicationFiled: March 9, 2001Publication date: January 3, 2002Inventors: Robert H. Chen, Min A Xiang
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Publication number: 20020002168Abstract: A compound of the formula 1Type: ApplicationFiled: May 22, 2001Publication date: January 3, 2002Inventor: Harry R. Howard
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Patent number: 6333337Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.Type: GrantFiled: January 13, 1999Date of Patent: December 25, 2001Assignee: ICAgen, Inc.Inventors: Michael F. Gross, Neil A. Castle
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Patent number: 6331640Abstract: A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.Type: GrantFiled: September 29, 1999Date of Patent: December 18, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
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Patent number: 6323234Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; composition comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: March 3, 2000Date of Patent: November 27, 2001Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6316467Abstract: 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: November 16, 1998Date of Patent: November 13, 2001Assignee: American Home Products CorporationInventor: Thomas J. Commons
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Patent number: 6316503Abstract: The invention provides compounds, compositions and methods for modulating the effects of LXR in a cell. The compounds and compositions are useful both as diagnostic indicators of LXR function and as pharmacologically active agents. The compounds and compositions find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.Type: GrantFiled: March 14, 2000Date of Patent: November 13, 2001Assignee: Tularik Inc.Inventors: Leping Li, Julio C. Medina, Kevin Lustig, Bei Shan, Hirohiko Hasegawa, Serena T. Cutler, Jiwen Liu, Liusheng Zhu
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Patent number: 6313159Abstract: The present invention relates to metabotropic glutamate receptor ligand derivatives and methods of using the same to inhibit NAALADase enzyme activity, to effect neuronal activities, to inhibit angiogenesis, and to treat glutamate abnormalities, compulsive disorders, pain, diabetic neuropathy, and prostate diseases, as well as pharmaceutical compositions comprising the same.Type: GrantFiled: August 20, 1999Date of Patent: November 6, 2001Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Barbara S. Slusher
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Patent number: 6307092Abstract: The present invention provides a novel compound represented by the general formula I: wherein R is H or COR3; R1 is H, R2, phenyl, or COR3, wherein R2 is C1-C5 lower alkyl and R3 is R2 or phenyl; Z is CH2 or O; Y is OH, OCOR3 or ═O; x is 0 or 1; and X is C1-C5 n-alkyl, C3-C7 cycloalkyl, phenyl, furanyl, thienyl or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR42, CO2R4 and OR4 wherein R4 is hydrogen or C1-C5 alkyl and dotted lines represent the presence or absence of a double bond and wavy lines represent a cis or trans bond. These novel compounds are especially useful for treating elevated intraocular pressure (ocular hypertension) and glaucoma.Type: GrantFiled: May 8, 2001Date of Patent: October 23, 2001Assignee: Allergan Sales, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
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Patent number: 6303602Abstract: A compound of the following formula: or a salt thereof, wherein A is hydrogen, halo, hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, furanyl or thienyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.Type: GrantFiled: January 26, 2001Date of Patent: October 16, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
Patent number: 6297260Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.Type: GrantFiled: October 29, 1999Date of Patent: October 2, 2001Assignee: NitroMed, Inc.Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang -
Patent number: 6297381Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions. Also disclosed are processes of making such compounds.Type: GrantFiled: February 14, 2000Date of Patent: October 2, 2001Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Eugene R. Hickey, John R. Regan
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Publication number: 20010016595Abstract: The present invention provides a method of treating a neurodegenerative disease and in particular Alzheimers disease which comprises administering to a human in need thereof a therapeutically effective amount of a non-steroid COX-II inhibitor.Type: ApplicationFiled: February 28, 2001Publication date: August 23, 2001Applicant: Merck Frosst Canada Inc./Merck Frosst Canada & Co.Inventors: Yves Ducharme, Jacques Yves Gauthier, Petpiboon Prasit, Yves Leblanc, Zhaoyin Wang, Serge Leger, Michel Therien
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Patent number: 6274590Abstract: A class of 3,4-diaryl substituted thiophene, derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: wherein Y is S; wherein X is one or two substituents selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: September 14, 2000Date of Patent: August 14, 2001Assignee: G. D. Searle & Co.Inventors: John J. Talley, Stephen R Bertenshaw, Paul W Collins, Thomas D. Penning, David B. Reitz, Roland S Rogers
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Patent number: 6274620Abstract: The present invention comprises compounds that are effective inhibitors of integrins, particularly &agr;v&bgr;3 and &agr;v&bgr;5 integrins. Particularly, the compounds are of formula I and pharmaceutically acceptable salts thereof wherein X,Y1 W, R1 to R5, A and B are defined according to the disclosure herein.Type: GrantFiled: June 7, 2000Date of Patent: August 14, 2001Assignee: BioChem Pharma Inc.Inventors: Denis Labrecque, Giorgio Attardo, Monica Bubenik, Laval Chan, Sylvie Charron, Réal Denis, Guy Falardeau, Serge Lamothe, Patrice Préville, Boulos Zacharie
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Patent number: 6271247Abstract: Compounds of formula (I): R—NH—A—CO—NH—NH—(W)n—Z (I) wherein: n is 0 or 1, W represents —CO— or S(O)r wherein r is 0, 1 or 2, Z represents a group selected from aryl, arylalkyl, heteroaryl and heteroarylalkyl, each optionally substituted, R represents a grouping selected from: Z1—T—CO—, Z1—O—T—CO—, Z1—T—O—CO—, Z1—T—S(O)q— wherein Z1, T and q are as defined in the description, A represents alkylene, alkenylene or alkynylene each having from 3 to 8 carbon atoms, alkylenecycloalkylene, cycloalkylenealkylene, alkylenecycloalkylenealkylene, alkylenearylene, arylenealkylene, alkylenearylenealkylene a grouping wherein B1 is as defined in the description, or A forms with the adjacent nitrogen atom a grouping as defined in the description. Medicinal products containing the same are useful as Neuropeptide Y receptors ligands.Type: GrantFiled: June 23, 2000Date of Patent: August 7, 2001Assignee: Adir et CompagnieInventors: Antonio Monge Vega, Ignacio Aldana Moraza, Daniel-Henri Caignard, Jacques Duhault, Jean Boutin, Odile Dellazuana
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Patent number: 6262079Abstract: A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): wherein Z is C═O or a covalent bond; Y is H or O(C1-C4)alkyl, R1 and R2 are individually (C1-C4)allyl or together with N are a saturated heterocyclic group, R3 is ethyl or chloroethyl, R4 is H or together with R3 is —CH2—CH2— or —S—, R5 is I, O(C1-C4)alkyl or H and R6 is I, O(C1-C4)alkyl or H with the proviso that when R4F R5, and R6 are H, R3 is not ethyl; or a pharmaceutically acceptable salt thereof, effective to activate or stimulate production of TGF-beta to treat and/or prevent conditions such as atherosclerosis, thrombosis, myocardial infarction, and stroke is provided. Useful compounds include idoxifene and salts thereof. Further provided is a method for identifying a compound that is a TGF-beta activator or production stimulator is provided. Another embodiment of the invention is an assay or kit to determine TGF-beta in vitro.Type: GrantFiled: May 6, 1999Date of Patent: July 17, 2001Assignee: NeoRx CorporationInventors: David J. Grainger, James C. Metcalfe, Lawrence L. Kunz, Robert W. Schroff, Peter L. Weissberg
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Patent number: 6262055Abstract: Sulfur-containing heteroaryl dioxo-butyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: June 1, 1999Date of Patent: July 17, 2001Assignee: Merck & Co., Inc.Inventors: Steven D. Young, John S. Wai, Mark W. Embrey, Thorsten E. Fisher
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Patent number: 6251920Abstract: A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): wherein Z is C═O or a covalent bond; Y is H or O(C1-C4)alkyl, R1 and R2 are individually (C1-C4)alkyl or together with N are a saturated heterocyclic group, R3 is ethyl or chloroethyl, R4 is H or together with R3 is —CH2—CH2— or —S—, R5 is I, O(C1-C4)alkyl or H and R6 is I, O(C1-C4)alkyl or H with the proviso that when R4, R5, and R6 are H, R3 is not ethyl; or a pharmaceutically acceptable salt thereof, effective to activate or stimulate production of TGF-beta to treat and/or prevent conditions such as atherosclerosis, thrombosis, myocardial infarction, and stroke is provided. Useful compounds include idoxifene and salts thereof. Further provided is a method for identifying a compound that is a TGF-beta activator or production stimulator is provided. Another embodiment of the invention is an assay or kit to determine TGF-beta in vitro.Type: GrantFiled: May 21, 1998Date of Patent: June 26, 2001Assignee: NeoRx CorporationInventors: David J. Grainger, James C. Metcalfe, Peter L. Weissberg
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Patent number: 6248783Abstract: The present invention provides a novel compound represented by the general formula I; wherein R is H or COR3; R1 is H, R2, phenyl, or COR3, wherein R2 is C1-C5 lower alkyl and R3 is R2 or phenyl; Z is CH2 or O; Y is OH or OCOR3; x is 0 or 1; and X is C1-C5 n-alkyl, C3-C7 cycloalkyl, phenyl, furanyl, thienyl or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR42, CO2R4 and OR4 wherein R4 is hydrogen or C1-C5 alkyl and dotted lines represent the presence or absence of a double bond and wavy lines represent a cis or trans bond. These novel compounds are especially useful for treating elevated intraocular pressure (ocular hypertension) and glaucoma.Type: GrantFiled: September 20, 2000Date of Patent: June 19, 2001Assignee: Allergan Sales, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner