Two Double Bonds Between Ring Members Of The Five-membered Hetero Ring (e.g., Pyrrole, Etc.) Patents (Class 514/427)
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Patent number: 6620843Abstract: Water soluble triptolide prodrugs are used as anticancer agents, and are found to be more effective in vivo, at lower doses, in reducing tumor size than the widely used chemotherapeutic agents 5-fluorouracil and irinotecan.Type: GrantFiled: January 19, 2001Date of Patent: September 16, 2003Assignee: PharmagenesisInventors: John M. Fidler, Ke Li
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Patent number: 6608050Abstract: The present invention relates to a pharmaceutically acceptable dosage form of water insoluble porphyrins, particularly metal containing porphyrins such as tin porphyrin, which can be complexed with a lipid, reconstituted from a lyophilizate and administrated to a patient in the treatment of cancer and other diseases.Type: GrantFiled: October 4, 2001Date of Patent: August 19, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Mathew Cherian, Shireesh Prakash Apte
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Patent number: 6608095Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 orType: GrantFiled: April 24, 2001Date of Patent: August 19, 2003Assignee: Pfizer Inc.Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
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Patent number: 6605619Abstract: The instant invention is directed to the use of a biologically compatible composition, containing an effective amount of a metal-independent nitroxide compound which is preferably represented by the formula wherein R1 is —CH3; R2 is —C2H5, —C3H7, —C4H9, —C5H11, —C6H13, —CH2—CH(CH3)2, —CHCH3C2H5, or —(CH2)7—CH3, or wherein R1 and R2 together form spirocyclopentane, spirocyclohexane, spirocycloheptane, spirocyclooctane, 5-cholestane, or norbornane, R3 is —O. or —OH, or a physiologically acceptable salt thereof, and a pharmaceutically acceptable carrier, as antioxidants capable of protecting cells, tissues, organs, and whole organisms against the deleterious effects of harmful free radical species generated during oxidative stress.Type: GrantFiled: June 7, 1995Date of Patent: August 12, 2003Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: James B. Mitchell, Amran Samuni, William G. Degraff, Stephen Hahn
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Patent number: 6605634Abstract: The present invention comprises a new class of novel aryl and heteroaryl substituted fused pyrrole compounds useful for the prophylaxis and treatment of diseases or conditions, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. In particular, the compounds of the invention are useful for the prophylaxis and treatment of diseases or conditions involving inflammation. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of inflammation and other maladies, such as pain and diabetes, using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: June 18, 2002Date of Patent: August 12, 2003Assignee: Amgen, Inc.Inventors: Jeffery A. Zablocki, Eugene Tarlton, Jr., James P. Rizzi, Nathan B. Mantlo
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Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
Patent number: 6593347Abstract: 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: August 27, 2001Date of Patent: July 15, 2003Assignee: 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: 6593345Abstract: The instant invention provides novel substituted naphthyl compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.Type: GrantFiled: August 27, 1997Date of Patent: July 15, 2003Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones, Alan David Palkowitz
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Patent number: 6583182Abstract: This invention involves synthesis and use of a class of compounds with chelation affinity and selectivity for first transition series elements. Administration of the free or conjugated compound, or physiological salts of the free or conjugated compound, results in decrease in the in vivo bioavailability of first transition series elements and/or removal from the body of first transition series elements and elements with similar chemical properties. These characteristics make such compounds useful in the management of diseases associated with a bodily excess of first transition series elements and elements with similar chemical properties. This invention demonstrates that such compounds inhibit mammalian, bacterial, and fungal cell replication and are therefore useful in the treatment of neoplasia, infection, inflammation, immune reponse, and in termination of pregnancy.Type: GrantFiled: November 30, 2001Date of Patent: June 24, 2003Assignee: Chelator LLCInventors: Harry S Winchell, Joseph Y Klein, Elliot D Simhon, Rosa L Cyjon, Ofer Klein, Haim Zaklad
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Patent number: 6566346Abstract: There are provided an oral skin improving agent that exhibits good skin improving effects when orally ingested, suppresses problems of discoloration and generation of unpleasant odor during storage, and has excellent storage stability; a food composition for improving skin containing this skin improving agent; and a skin improving method. The oral skin improving agent contains as a principal component refined hyaluronic acid having a purity of at least 90%, preferably at least 95%, and an average molecular weight in a range of 750,000 to 1,200,000, preferably 800,000 to 1,000,000. A person's skin can be improved by having the person ingest the oral skin improving agent such that the ingestion amount thereof is at least 5 mg per day.Type: GrantFiled: March 11, 2002Date of Patent: May 20, 2003Assignee: Q.P. CorporationInventors: Osami Kajimoto, Wakako Sakamoto, Wataru Odanaka, Kazuya Yoshida
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Patent number: 6538016Abstract: The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl, C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR12R13 wherein R12 and R13 are each independently of the other hydrogen or C1-C6-alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; R4, R5, R6 and R7 are each independently hydrogen or C1-C4alType: GrantFiled: June 1, 2001Date of Patent: March 25, 2003Assignee: Syngenta Participations AGInventors: Martin Zeller, André Jeanguenat, Clemens Lamberth
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Patent number: 6531472Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, X and Y have the meanings defined in the specification. The compounds have histone deacetylase (HDAC) inhibitory activity which is useful in cancer treatment. Also provided is a process for making a compound of formula I by reacting a compound of formula III with a compound of formula IV wherein A is a displaceable group and PG is a protecting group.Type: GrantFiled: December 4, 2001Date of Patent: March 11, 2003Assignee: Hoffman-La Roche Inc.Inventors: Guy Georges, Adelbert Grossmann, Tim Sattelkau, Wolfgang Schaefer, Ulrich Tibes
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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: 6514510Abstract: An insecticidal and miticidal composition comprising as active ingredients 4-bromo-2-(4-chloro-phenyl)-1-(ethoxymethyl)-5-(trifluoromethyl)pyrrole-3-carbonitrile and a pyrethroid insecticidal ingredient(s). This insecticidal and miticidal composition is effective against pests and mites which are resistant against the insecticidal and miticidal agents on the market.Type: GrantFiled: March 25, 1999Date of Patent: February 4, 2003Assignee: BASF AktiengesellschaftInventor: Toshiki Fukuchi
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Patent number: 6512002Abstract: This invention relates to methods and pharmaceutical compositions useful in the treatment of conditions that are responsive to the elevation of testosterone levels in the body and the use of estrogen agonists/antagonists for the manufacture of medicaments for the treatment of conditions that are responsive to the elevation of testosterone levels in the body. The compositions are comprised of an estrogen agonist/antagonist and a pharmaceutically acceptable vehicle, carrier or diluent. These compositions are effective in treating male subject sexual dysfunction and timidity in female subjects including post-menopausal women and are effective in increasing libido in female subjects including post-menopausal women. In the case of male subject sexual dysfunction, the compositions may also include a compound which is an elevator of cyclic guanosine 3′,5′-monophosphate (cGMP).Type: GrantFiled: January 10, 2001Date of Patent: January 28, 2003Assignee: Pfizer Inc.Inventors: Andrew G. Lee, Wesley W. Day, David D. Thompson
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Publication number: 20030018057Abstract: Novel thiol derivatives of formula I 1Type: ApplicationFiled: June 13, 2002Publication date: January 23, 2003Inventors: Cynthia Anne Fink, Faribroz Firooznia
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Patent number: 6492413Abstract: A class of 3,4-diaryl substituted thiophene, furan and pyrrole 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 selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent 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 at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: March 20, 2000Date of Patent: December 10, 2002Assignee: 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: 6489348Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2 I in which A, R1 and R2 are as defined in the description, and b) compounds of the formula II, their N-oxide or one of their salts where the substituents R12 to R18 are as defined in the description, and/or c) compounds of the formula III where the substituents X1 to X5 and R19 to R22 are as defined in the description, in a synergistically effective amount.Type: GrantFiled: September 24, 2001Date of Patent: December 3, 2002Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6482859Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eaType: GrantFiled: February 4, 2000Date of Patent: November 19, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: Martin Zeller, André Jeanguenat
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Patent number: 6479532Abstract: This invention relates to an antimycotic composition comprising pyrrolnitrin and at least one member selected from the group consisting of lanoconazole, butenafine or a salt thereof, and an allylamine-series antimycotic agent as active ingredients, which composition has a potent antimycotic action as compared with its component drugs used each independently and is not only of great use in the treatment of dermatophytosis such as tinea, tinea imbricata, tinea favosa, tinea profunda, etc. and fungal infections such as candidiasis of cutaneous mucosa, candidiasis profunda, etc. but also useful from the standpoint of alleviation of side effects and improvement in the patient's compliance.Type: GrantFiled: October 15, 2001Date of Patent: November 12, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Toshiaki Kamimura, Tsuguo Yabuta, Saburo Obata
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Patent number: 6479493Abstract: Substituted condensation products of -benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of type I diabetes.Type: GrantFiled: August 23, 2001Date of Patent: November 12, 2002Assignee: Cell Pathways, Inc.Inventors: Clark M. Whitehead, Keith A. Earle, Hector W. Alila, W. Joseph Thompson
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Patent number: 6479485Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: August 7, 2001Date of Patent: November 12, 2002Assignee: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
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Patent number: 6479537Abstract: The present invention provides methods for synergistic control of ectoparasitic arthropods with a synergistically effective amount of a combination of the macrocyclic lactone moxidectin and an arylpyrrole compound. Also provided are methods of protecting animals from infestation and attack by ectoparasites with said combination. The present invention also provides synergistic insecticidal compositions comprising as essential active ingredients the macrocyclic lactone moxidectin and an arylpyrrole compound.Type: GrantFiled: November 21, 2001Date of Patent: November 12, 2002Assignee: American Cyanamid CompanyInventors: Kathleen Heaney, Mary E. Doscher, Douglas Rugg
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Patent number: 6465471Abstract: Compounds of formula (1) are described: in which Het is a heteroaromatic group, Alk1 is an optionally substituted aliphatic or heteroaliphatic chain and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: July 1, 1999Date of Patent: October 15, 2002Assignee: Celltech Therapeutics LimitedInventors: Graham John Warrellow, John Clifford Head, John Robert Porter, Sarah Catherine Archibald
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Patent number: 6462024Abstract: Inhibitors of the sodium-hydrogen exchanger are used for the production of a medicament for decreasing the undesired effects in human and in veterinary medicine which originate from substances which cause damage to the heart when administered acutely or chronically.Type: GrantFiled: July 11, 2000Date of Patent: October 8, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Hans Jochen Lang, Hartmut RĂ¼tten, Holger Heitsch, Wolfgang Linz, Bernward Schölkens
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Patent number: 6458803Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: November 23, 2001Date of Patent: October 1, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6455574Abstract: This invention relates to pharmaceutical combinations of amlodipine or a pharmaceutically acceptable acid addition salt thereof and atorvastatin or a pharmaceutically acceptable salt thereof, kits containing such combinations and methods of using such combinations to treat subjects suffering from angina pectoris, atherosclerosis, combined hypertension and hyperlipidemia and to treat subjects presenting with symptoms of cardiac risk, including humans. This invention also relates to additive and synergistic combinations of amlodipine and atorvastatin whereby those synergistic combinations are useful in treating subjects suffering from angina pectoris, atherosclerosis, combined hypertension and hyperlipidemia and those subjects presenting with symptoms of cardiac risk, including humans.Type: GrantFiled: February 25, 2000Date of Patent: September 24, 2002Assignee: Pfizer Inc.Inventor: Jan Buch
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Patent number: 6451824Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: September 17, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
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Publication number: 20020119994Abstract: The invention relates to novel compounds having formula (I) 1Type: ApplicationFiled: November 26, 2001Publication date: August 29, 2002Applicant: GENENTECH, INCInventors: Daniel J. Burdick, Mark S. Stanley, David Oare, Mark E. Reynolds, Thomas R. Gadek, James C. Marsters
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Patent number: 6441237Abstract: The present patent application relates to new substituted 3-phenoxy- or 3-phenylalkyloxy-2-phenyl-propylamines of general formula 1, processes for preparing them and their use as pharmaceutical compositions.Type: GrantFiled: February 18, 2000Date of Patent: August 27, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Werner Stransky, Matthias Grauert, Adrian Carter, Thomas Weiser, Wolf-Dietrich Bechtel, Helmut Ensinger, Ralf Richard H. Lotz, Rainer Palluk, Uwe Pschorn
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Patent number: 6436999Abstract: Diacyl-substituted guanidines of the formula I are described where X(1) and X(2) are as defined herein. The compounds are suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventitive manner the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.Type: GrantFiled: April 18, 1997Date of Patent: August 20, 2002Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
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Publication number: 20020111376Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist and an arylpyrrole insecticide.Type: ApplicationFiled: January 29, 2002Publication date: August 15, 2002Applicant: Intellectual Property Department BASF AktiengesellschaftInventors: Michael Frank Treacy, Raymond Frank Borysewicz, Paul E. Rensner
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Patent number: 6432965Abstract: The invention relates to novel fungicidal compositions having a synergistically increased action, wherein component a) is a thieno[2,3-d]pyrimidin-4-one of formula I wherein R1 is halogen, R2 is C1-C5alkyl, —CH2-cyclopropyl and R3 is C1-C5alkyl, —CH2-cyclopropyl; in association with b) either an anilinopyrimidine fungicide (II), or an azole fungicide (III), or a morpholine fungicide (IV), or a strobilurin compound (V), or a pyrrole compound (VI), or a phenylamide (VII), or a dithiocarbamate fungicide selected from mancozeb, maneb, metiram and zineb, or a copper compound selected from copper hydroxide, coopper oxychloride, copper sulfate and oxine-copper, or a phthalimide compound (VIII), or prochloraz, or triflumizole, or pyrifenox, or acibenzolar-S-methyl, or chlorothalonil, or cymoxanil, or dimethomorph, or famoxadone, or fenhexamide, or fenarimol, or fluazinam, or fosetyl-aluminium, orquinoxyfen, or fenpropidine, or spiroxamine, or carbendazime, or thlabendazole, orType: GrantFiled: September 15, 2000Date of Patent: August 13, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: Kaspar MĂ¼ller, Gertrude Knauf-Beiter, Dietrich Hermann, Harald Walter
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Patent number: 6433002Abstract: A compound of formula (I): compositions containing them and methods of use to control pests.Type: GrantFiled: April 12, 2001Date of Patent: August 13, 2002Assignee: Rhone-Poulenc Inc.Inventors: Jamin Huang, Scot Kevin Huber
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Publication number: 20020103202Abstract: The present application describes heteroaryl-phenyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of factor Xa.Type: ApplicationFiled: June 22, 2001Publication date: August 1, 2002Inventors: Donald J.P. Pinto, Mimi L. Quan, Francis J. Woerner
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Patent number: 6420427Abstract: An aminobutyric acid derivative of the formula (I): (wherein all symbols are as defined in the specification) and salt thereof. salt thereof. The compounds of the formula (I) possess an inhibitory activity on matrix metalloproteinase and are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cells, autoimmune disease (e.g. Crohn's disease, Sjogren's syndrome), disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, aorta aneurysm, endometriosis.Type: GrantFiled: April 7, 2000Date of Patent: July 16, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kanji Takahashi, Tsuneyuki Sugiura
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Patent number: 6417371Abstract: The present invention relates to a process process for the preparation of the compound of the formula I where the compound of the formula III is reacted with oxalyl chloride and the product obtained is treated with hydrazine and an alkali metal hydroxide in the aqueous phase at elevated temperature, after treatment is complete a three-phase system is produced by addition of an ether and the compound of the formula I is obtained by acidifying the middle phase. The invention moreover relates to a polymorph of the compound of the formula I.Type: GrantFiled: January 26, 2001Date of Patent: July 9, 2002Assignee: Merckle GmbHInventors: Thomas Kammermeier, Stefan Laufer, Philipp Merckle, Hans-Guenter Striegel
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Patent number: 6414005Abstract: Compounds represented by the general formula (1): [wherein R1 is typically an aminoalkyl group; R2 is typically a hydrogen atom, a lower alkyl group, R3 or SR4 (where R4 is typically a lower alkyl group); Ar is typically a 5-membered aromatic heterocyclic group] have an NOS inhibiting activity and are useful as therapeutics of cerebrovascular diseases and other pharmaceuticals.Type: GrantFiled: May 4, 2000Date of Patent: July 2, 2002Assignee: Chugai Seiyaku Kabushiki KaishaInventor: Toshihiko Makino
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Patent number: 6413973Abstract: The invention relates to novel fungicidal compositions having synergistically increased action, wherein component a) is a pyrimidin-4-one of formula i in association with b) either an anilinopyrimidine fungicide (II), or an azole fungicide (III), or a morpholine fungicide (IV), or a strobilurin compound (V), or a pyrrole compound (VI), or a phenylamide (VII), or a dithiocarbamate fungicide selected from mancozeb, maneb, metiram and zineb, or a copper compound selected from copper hydroxide, copper oxychloride, copper sulfate and oxine-copper, or a phthalimide compound (VIII), or prochloraz, or triflumizole, or pyrifenox, or acibenzolar-S-methyl, or chlorothalonil, or cymoxanil, or dimethomorph, or famoxadone, or fenhexamide, or fluazinam, or fosetyl-aluminium, or quinoxyfen, or spiroxamine, or carbendazime, or thiabendazole, or ethirimol, or triazoxide, or guazatine.Type: GrantFiled: August 31, 2000Date of Patent: July 2, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: Harald Walter, Kaspar MĂ¼ller, Gertrude Knauf-Beiter, Dietrich Hermann
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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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Publication number: 20020068760Abstract: The invention relates to an insecticidal and miticidal composition which contains as active ingredients chlorfenapyr in combination with one or more organophosphoric acid ester-type compounds and to a method for controlling insecticidal or miticidal pests which have acquired resistance to commercial insecticidal and miticidal agents.Type: ApplicationFiled: September 28, 2001Publication date: June 6, 2002Applicant: American Cyanamid Company Intellectual Property DepartmentInventor: Toshiki Fukuchi
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Patent number: 6395724Abstract: Disclosed are multibinding compounds which inhibit cyclooxygenase-2 (COX-2), an enzyme which catalyzes the first committed step in the biosynthesis of prostaglandins. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to COX-2. The multibinding compounds of this invention are useful in the treatment inflammation, pain, fever and the like.Type: GrantFiled: June 7, 1999Date of Patent: May 28, 2002Assignee: Advanced Medicine, Inc.Inventors: J. Kevin Judice, Deborah L. Higgins, John H. Griffin
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Publication number: 20020058691Abstract: A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders.Type: ApplicationFiled: March 20, 2000Publication date: May 16, 2002Inventors: JOHN J. TALLEY, Stephen R. Bertenshaw, Paul W. Collins, Thomas D. Penning, David B. Reitz, Ronald S. Rogers
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Patent number: 6384052Abstract: Trisubstituted pyrroles are useful in the control of coccidiosis in poultry.Type: GrantFiled: November 10, 2000Date of Patent: May 7, 2002Assignee: Merck & Co., Inc.Inventors: Tesfaye Bitfu, Danqing D. Feng
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Patent number: 6355669Abstract: The present invention provides a therapeutic or prophylactic agent as a substitute for conventional steroids or immunosuppressive agents to treat or prevent systemic erythematosus, glomerulonephritis, lupus nephritis, idiopathic thrombocytopenic purpura or autoimmune anemia.Type: GrantFiled: April 18, 2000Date of Patent: March 12, 2002Assignee: Eisai Co., Ltd.Inventors: Toshihiko Yamauchi, Akira Ishibashi, Naoki Tokuhara, Mitsuo Nagai
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Patent number: 6355810Abstract: Disclosed are multibinding compounds which inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-COA reductase), the rate limiting enzyme in cholesterol biosynthesis. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to HMG-CoA reductase and the distance between ligands is at least 10 Å. The multibinding compounds of this invention are useful in the treatment and prevention of hypercholesterolemia, hyperlipidemia, atherosclerosis and the like.Type: GrantFiled: June 4, 1999Date of Patent: March 12, 2002Assignee: Advanced Medicine, Inc.Inventors: John H. Griffin, Michael R. Leadbetter, Donald E. Schmidt, Jr.
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Patent number: 6353016Abstract: The invention is directed to a pharmaceutical composition comprising a pyrrole derivative of the following formula [1] or its pharmaceutically acceptable salt as an active ingredient. (wherein R1 represents hydrogen or alkoxycarbonylamino; R2 represents alkyl, aryl which may be substituted, a aromatic heterocyclyl which may be substituted, unsubstituted amino, monoalkyl-substituted amino, dialkyl-substituted amino, or cyclic amino which may be substituted; R3 represents cyano or carbamoyl; R4 represents hydrogen or alkyl; E represents alkylene; q represents 0 or 1; A represents methyl, aryl which may be substituted, or a aromatic heterocyclyl which may be substituted). This pharmaceutical composition is useful as a potassium channel activator.Type: GrantFiled: June 29, 2000Date of Patent: March 5, 2002Assignee: Nippon Shinyaku Co., Ltd.Inventors: Mitsushi Tanaka, Masami Tsuda, Ayatsugu Nakamura
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Patent number: 6348476Abstract: Pharmaceutical combination preparation of an inhibitor of the sodium/hydrogen exchanger and a medicament for the treatment of cardiovascular diseases. These combinations of an NHE inhibitor can comprise one or more therapeutically active compounds having cardiovascular activity. The combination of the cardioprotective properties with known therapies of cardiovascular diseases leads on the one hand to an improvement of the quality of the treatment and on the other hand in a large number of combinations to an additive or potentiated increase of the cardiovascular effects of the individual active compounds alone.Type: GrantFiled: July 5, 2000Date of Patent: February 19, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Wolfgang Scholz, Udo Albus
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Patent number: 6342518Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist and an arylpyrrole insecticide. Also provided are methods for synergistic insect control and crop protection.Type: GrantFiled: March 9, 2000Date of Patent: January 29, 2002Assignee: BASF AktiengesellschaftInventors: Michael Frank Treacy, Raymond Frank Borysewicz, Paul E. Rensner
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Patent number: 6342624Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of a disorder mediated by inhibiting plasma renin activity.Type: GrantFiled: January 6, 2000Date of Patent: January 29, 2002Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran