The Additional Hetero Ring Contains Sulfur As The Only Ring Hetero Atom [e.g., 5-(2-thienyl) Hydantoin, Etc.] Patents (Class 548/315.1)
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Patent number: 6458963Abstract: The present invention relates to a process for preparing eprosartan, an angiotensin II receptor antagonist useful in the treatment of hypertension, congestive heart failure, and renal failure. The process for preparing eprosartan consists of three stages. These stages are: (Stage†1) the regioselective protection of 2-n-butyl-4-formylimidazole; (Stage†2) the reaction between the product from Stage 1 and (2-thienylmethyl)-propanedioic acid, mono-C1-4alkyl ester; and (Stage†3) quaternary salt formation, followed by a basic work-up and an acidification. The efficiency of this synthetic sequence is particularly is particularly useful for the large-scale production of eprosartan.Type: GrantFiled: August 14, 2001Date of Patent: October 1, 2002Assignee: SMithKline Beecham CorporationInventors: Richard T. Matsuoka, Peng Liu
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Publication number: 20020137943Abstract: This invention relates to (E)-&agr;-[2-n-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazol-5-yl]methylene-2-thiophenepropionic acid arginyl charge-neutralization-complex, a process for its production, compositions containing the compound and methods of using the compound to block angiotensin II receptors and to treat hypertension, congestive heart failure and renal failure.Type: ApplicationFiled: December 12, 2001Publication date: September 26, 2002Inventors: Nageswara R. Palepu, Gopadi M. Venkatesh
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Patent number: 6448286Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: July 28, 1998Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Patent number: 6440899Abstract: Cyclohexenonedioxothiochromanoyl derivatives of the formula I where X is oxygen, sulfur, S═O, S(═O)2, CR4R5, C═O or C═NR6, the other substituents are as defined in the specification, and and agriculturally useful salts thereof; processes for preparing the cyclohexenonedioxotheiochromanoyl derivatives; compositions comprising them, and the use of these derivatives or of compositions comprising them for controling undesirable piants.Type: GrantFiled: October 30, 2000Date of Patent: August 27, 2002Assignee: BASF AktiengesellschaftInventors: Matthias Witschel, Klaus Langemann, Wolfgang von Deyn, Ulf Misslitz, Ernst Baumann, Stefan Engel, Guido Mayer, Ulf Neidlein, Oliver Wagner, Roland Götz, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Patent number: 6436967Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2. The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelling associated with inflammation also produce severe side effects, including life threatening ulcers. The recent discovery of an inducible enzyme associated with inflammation (“prostaglandin G/H synthase II” or “cyclooxygenase-2 (COX-2)”) provides a viable target of inhibition which more effectively reduces inflammation and produces fewer and less drastic side effects.Type: GrantFiled: September 14, 2000Date of Patent: August 20, 2002Assignee: Pharmacia CorporationInventors: John J Talley, James W Malecha, Stephen Bertenshaw, Matthew J Graneto, Jeffery Carter, Jinglin Li, Srinivasan Nagarajan, David L Brown, Donald J Rogier, Jr., Thomas D Penning, Ish K Khanna, Xiangdong Xu, Richard M Weier
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Patent number: 6429222Abstract: The invention relates to novel 1-(p-thienylbenzy)imidazoles of formula (I) where the radicals R(1) to R(6), X, and Y have the meaning indicated in the description, which are potent agonists of angiotensin (1-7) receptors and owing to the production and release of the vasorelaxant, antithrombotic, and cardioprotective messengers cyclic 3′,5′-guanosine monophosphate (cGMP) and nitrogen monoxide (NO) associated with the stimulation of these receptors on endothelial cells are valuable pharmaceuticals for the treatment and prophylaxis of high blood pressure, cardiac hypertrophy, cardiac insufficiency, coronary heart diseases such as angina pectoris, cardiac infarct, vascular restenosis after angioplasty, cardiomyopathies, endothelial dysfunction or endothelial damage, e.g., as a result of arteriosclerotic processes or diabetes mellitus, and also of arterial and venous thromboses.Type: GrantFiled: March 16, 2001Date of Patent: August 6, 2002Inventors: Holger Heitsch, Gabriele Wiemer
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Patent number: 6420412Abstract: The invention relates to (E)-&agr;-[2-n-butyl-1-[(4-carboxyphenyl)methyl]-1-H-imidazol-5-yl]methylene-2-thiopheneproprionic acid monomethanesulfonate dihydrate, a process for its production, compositions containing the compound and methods of using the compound to block angiotensin II receptors and to treat hypertension, congestive heart failure and renal failure.Type: GrantFiled: March 15, 2001Date of Patent: July 16, 2002Assignee: SmithKline Beecham CorporationInventors: Nageswara R. Palepu, Gopadi M. Venkatesh, Sarma Duddu
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Patent number: 6410582Abstract: The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromatic group, N-methyl-substituted, that contains from one to three nitrogen atoms. They have analgesic activity in mammals, including humans. The compounds (I) can be obtained, for example, by reaction of a derivative of hydroxy-thienylazol (IV) with a derivative of a suitable N-(ethyl)amine. The compounds (IV) are useful intermediates in the synthesis of the compounds (I). The compounds (I) have an application in human and/or veterinary medicine.Type: GrantFiled: October 12, 2000Date of Patent: June 25, 2002Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Ramon Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
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Patent number: 6376497Abstract: An antifungal compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: X is CH or N; Y is O, R1 and R2 are each independently F or Cl; R3 is a thiophenyl, naphthyl, or phenyl group, the phenyl group being optionally substituted with one or more substituents selected from the group consisting of C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, methylenedioxy and halogen; and R4 is H or trifluoromethyl.Type: GrantFiled: July 6, 2001Date of Patent: April 23, 2002Assignee: Korea Research Institute of Chemical TechnologyInventors: Bum-Tae Kim, Sun-Young Han, Chwang-Siek Pak
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Patent number: 6369225Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 9, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6358955Abstract: Disclosed are compounds of the formula: wherein R1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R3 and R4 are organic or inorganic substituents which may together form ring structures; m is zero, one or two; and R5 and R6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.Type: GrantFiled: February 4, 2000Date of Patent: March 19, 2002Assignee: Neurogen CorporationInventors: Andrew Thurkauf, Raymond F. Horvath, Jun Yuan, John M. Peterson
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Patent number: 6344564Abstract: Fungicidal 2-imidazolin-5-ones and 2-imidazoline-5-thiones, processes for their preparation, fungicidal compositions containing them, and methods of using them to treat or prevent fungal disease in crops.Type: GrantFiled: October 14, 1999Date of Patent: February 5, 2002Assignee: Rhone-Poulenc, Inc.Inventors: Guy Lacroix, Raymond Peignier, Regis Pepin, Jean-Philippe Bascou, Gilbert Emeric, Joseph Perez, Fabrice Pinard, Christian Schmitz, Alain Gadras
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Publication number: 20010044531Abstract: Nucleic acid labeling compounds containing heterocyclic derivatives are disclosed. The heterocyclic derivative containing compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.Type: ApplicationFiled: February 9, 2001Publication date: November 22, 2001Inventors: Glenn McGall, Anthony D. Barone
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Publication number: 20010039287Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.Type: ApplicationFiled: February 24, 1999Publication date: November 8, 2001Inventors: THOMAS E BARTA, DANIEL P BECKER, TERRI L BOEHM, GARY A DECRESCENZO, CLARA I WILLAMI1, JOSEPH J MCDONALD, JOHN N FRESKOS, DANIEL P GETMAN, GUNNAR J HANSON
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Patent number: 6313164Abstract: Compounds of the formula (I): wherein one of m and n is 0, and the other is 0, 1 or 2; k is 0 or 1 to 12; R1 is hydrogen, a substituent which is an aryl or a heterocyclic, or an optionally substituted alkyl group; A is a single bond, an oxygen atom, a carbonyl group or a group of the formula —N(R2)CO—, —N(R2)CS—, —N(R2)SO2—, —CON(R2)N(R3)CO—, —CON(R2)CO—, —CON(R2)CS—, —CON(R2)SO2—, —O—CO—, —ON(R2)CO—, —ON(R2)SO2—, —O—CON(R2)N(R3)CO—, —O—CON(R2)CO—, —O—CON(R2)SO2—, —CO—O—, —CO—CO—, —CO—CON(R2)N(R3)CO—, —CO—CON(R2)CO—, —CO—CON(R2)SO2—, —N(R2)O—, —N(R2)COCO—, —N(R2)N(R3)CO—, —N(R2)N(R3)SO2—, —N(R2)CON(R3)N(R4)CO—, —N(R2)CON(R3)CO—, —N(R2)CON(R3)SO2&mdasType: GrantFiled: July 15, 1999Date of Patent: November 6, 2001Assignee: Sankyo Company, LimitedInventors: Takashi Fujita, Tomihisa Yokoyama
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Patent number: 6306892Abstract: The present invention is directed to compound of the formula I: wherein R1, R2, R3, R4, R 5, X, Y, and are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.Type: GrantFiled: June 21, 2000Date of Patent: October 23, 2001Assignees: Agouron Pharmaceuticals, Inc., Syntex Inc.Inventors: Steven L. Bender, Arlindo L. Castelhano, Wesley K. M. Chong, Melwyn A. Abreo, Roland J. Billedeau, Jian Jeffrey Chen, Judith G. Deal
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Publication number: 20010031877Abstract: The invention relates to (E)-&agr;-[2-n-butyl-1-[(4-carboxyphenyl)methyl]-1-H-imidazol-5-yl]methylene-2-thiopheneproprionic acid monomethanesulfonate dihydrate, a process for its production, compositions containing the compound and methods of using the compound to block angiotensin II receptors and to treat hypertension, congestive heart failure and renal failure.Type: ApplicationFiled: March 15, 2001Publication date: October 18, 2001Applicant: SmithKline Beecham CorporationInventors: Nageswara R. Palepu, Gopadi M. Venkatesh, Sarma Duddu
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Patent number: 6294675Abstract: This invention relates to a process for preparing eprosartan.Type: GrantFiled: July 27, 1999Date of Patent: September 25, 2001Assignee: SmithKline Beecham CorporationInventors: Richard T. Matsuoka, Peng Liu
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Publication number: 20010018449Abstract: The invention relates to novel 1-(p-thienylbenzyl)imidazoles of formula (I) 1Type: ApplicationFiled: March 16, 2001Publication date: August 30, 2001Applicant: Aventis Pharma Deutschland GmbHInventors: Holger Heitsch, Gabriele Wiemer
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Patent number: 6265422Abstract: The present invention provides compounds of Formula I The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula I.Type: GrantFiled: April 28, 2000Date of Patent: July 24, 2001Assignee: Warner-Lambert CompanyInventors: Jack Bikker, Ellen Myra Dobrusin, Annette Marian Doherty, Matthew Drowns, James Stanley Kaltenbronn, Juergen Kleinschroth, Dennis Joseph McNamara, John Quin, III, Joseph Thomas Repine, Marcin Stasiak
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Patent number: 6262102Abstract: This invention relates to (E)-&agr;-[2-n-butyl-1-[(4-carboxyphenyl)methyl]-1) H-imidazol-5-yl]methylene-2-thiophenepropionic acid monomethanfesulfonate monohydrate, compositions containing the compound and methods of using the compound to block angiotensin II receptors and to treat hypertension, congestive heart failure and renal failure.Type: GrantFiled: December 8, 1999Date of Patent: July 17, 2001Assignee: SmithKline Beecham CorporationInventors: Sarma Duddu, Nageswara R Palepu, Gopadi M Venkatesh
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Publication number: 20010006975Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: January 8, 2001Publication date: July 5, 2001Applicant: BAYER CORPORATION and ONYX PHARMACEUTICALS West Haven, CT and Richmond, CA, respectivelyInventors: Jill E. Wood, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Patent number: 6242474Abstract: Novel aromatic ring derivatives represented by formula (I) or their pharmaceutical acceptable salts are provided. wherein Nu represents a 5- or 6-membered aromatic ring; ch1 and ch2 each represents a cross-linking group; and A represents an aromatic ring. These compounds have blood sugar-depressing activity or PDE 5 inhibitory activity and are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin-resistance, polycystic ovary syndrome, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, hypertension, stenocardia, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, autoimmune diseases, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, nephritis, cachexia, pancreatitis, restenosis after PTCA, etc.Type: GrantFiled: March 21, 2000Date of Patent: June 5, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Noritsugu Yamasaki, Takafumi Imoto, Takahiro Hiramura, Osamu Onomura, Masahiro Nishikawa, Hiroshi Kayakiri, Yoshito Abe, Hitoshi Hamashima, Hitoshi Sawada
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Patent number: 6228848Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.Type: GrantFiled: November 22, 1999Date of Patent: May 8, 2001Assignee: Allergan, Inc.Inventors: Elliott S. Klein, Alan T. Johnson, Andrew M. Standeven, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Sunil Nagpal, Vidyasagar Vuligonda, Min Teng, Roshantha A. Chandraratna
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Patent number: 6187799Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: GrantFiled: May 22, 1998Date of Patent: February 13, 2001Assignees: Onyx Pharmaceuticals, Bayer CorporationInventors: Jill E Wood, Hanno Wild, Daniel H Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Patent number: 6172237Abstract: This invention relates to a process for preparing eprosartan by reacting 4-[(2-n-butyl-5-formyl-1H-imidazol-1-yl)methyl]benzoic acid or the bisulfite addition compound of 4-[(2-n-butyl-5-formyl-1H-imidazol-1-yl)methyl]benzoic acid with (2-thienylmethyl)propanedioic acid, mono-ethyl ester.Type: GrantFiled: July 27, 1999Date of Patent: January 9, 2001Assignee: SmithKline Beecham CorporationInventors: Clifford S. Labaw, Joseph Robert Flisak, Li Liu
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Patent number: RE37303Abstract: A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as in the specification having antagonist properties to histamine H3-receptors.Type: GrantFiled: April 6, 2000Date of Patent: July 31, 2001Assignees: Institut National del la Sante et de la Recherche Medicale, Societe Civile BioprojetInventors: Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Jeanne-Marie Lecomte, Charon R. Ganellin, Abdellatif Fkyerat, Wasyl Tertiuk, Walter Schunack, Ralph Lipp, Holger Stark, Katja Purand