The Additional Hetero Ring Is Six-membered Patents (Class 546/280.1)
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Patent number: 6881742Abstract: Novel benzamidoxime derivatives, processes and intermediates for their preparation and their use as fungicides are described. In the context of the present invention, benzamidoxime derivatives are compounds of the formula I where: A is an aryl or hetaryl radical; Y is a straight-chain or branched C1-C4-alkylene group, where one carbon can be replaced by oxygen, nitrogen or sulfur or by a cyclopropyl group; Rn1 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-alkoxyalkoxy; R2 is unsubstituted or substituted phenyl-C1-C6-alkyl, thienyl-C1-C4-alkyl, or pyrazolyl-C1-C4-alkyl, Rp3 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-alkoxyalkoxy, C1-C6-alkylcarbonyl; n is 0-5; p is, depending on the number of free valencies, 0-4.Type: GrantFiled: October 5, 2000Date of Patent: April 19, 2005Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Karl Eicken, Ingo Rose, Thomas Grote, Eberhard Ammermann, John-Bryan Speakman, Siegfried Strathmann, Gisela Lorenz
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Patent number: 6858732Abstract: Benzodioxino-naphtho[1,2-b]pyran compounds having particularly advantageous photochromic properties, such as, high sensitivity/coloration, two distinct absorption bands in the 430-500 nm range and 520-620 nm range of the visible spectrum may be generally described as a naphthopyran having a central nucleus of the formula: wherein F is a 1,4-benzodioxine ring with its 2,3 positions fused to the i, j, or k faces; and R1 and R2 are the atoms or groups providing photochromic properties to the naphthopyran.Type: GrantFiled: March 1, 2002Date of Patent: February 22, 2005Assignee: Vision-Ease Lens, Inc.Inventors: Xuzhi Qin, J. Thomas Ippoliti
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Patent number: 6750233Abstract: 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: GrantFiled: September 17, 2001Date of Patent: June 15, 2004Assignee: Pharmacia CorporationInventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Yvette M. Fobian, John N. Freskos, Daniel P. Getman, Joseph J. McDonald, Susan L. Hockerman, Susan C. Howard, Steve A. Kolodziej, Hui Li, Deborah A. Mischke, Joseph G. Rico, Nathan W. Stehle, Michael B. Tollefson, William F. Vernier, Clara I. Villamil
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Publication number: 20040097729Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as herbicides.Type: ApplicationFiled: December 6, 2002Publication date: May 20, 2004Inventors: Andrew Edmunds, Alain De Mesmaeker, Christoph Luthy, Jurgen Schaetzer
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Publication number: 20040097733Abstract: Compounds of the formula 1Type: ApplicationFiled: July 2, 2003Publication date: May 20, 2004Inventors: Richard L. Beard, Thong Vu, Diana F. Colon, Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Publication number: 20040082601Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1Type: ApplicationFiled: October 21, 2003Publication date: April 29, 2004Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, Richard Cordova, Kevin Pan, Joseph Meschino
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Patent number: 6696470Abstract: A compound of the formula: and its pharmaceutically effective salts, wherein R1 and R2 are independently selected from the following: (a) hydrogen, halo, R5—, C2-6 alkenyl, C2-6 alkynyl, hydroxy-R5—, R5—O—R5—, or the like; (b) Ar—, Ar—R5—, Ar—C2-6 alkenyl, Ar—C2-6 alkynyl, Ar—O—, Ar—O—R5— or the like; (c) R5—C(O)—, —NO2, cyano, NH2—C(O)—, R5—NH—C(O)—, (R5)2—N—C(O)—, Ar—C(O)— or the like; and (d) R5—C(O)—NH—, Ar—C(O)—NH— or the like; wherein Ar is optionally substituted aryl or heteroaryl such as phenyl and pyridyl; and wherein R5 is optionally halo-substituted C1-6 alkyl; R3 is selected from the following: (e) cyano, formyl, tetrazolyl, triazolyl, imidazolyl, oxazolyl, thiazolyl, R5—C(O)—, C2-6 alkenyl-C(O)—, C2-6 alkynyl-C(O)—, R5—C(O)—R5—, or theType: GrantFiled: July 30, 2001Date of Patent: February 24, 2004Assignee: Pfizer Inc.Inventors: Akiyoshi Kawai, Makoto Kawai
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Publication number: 20030225077Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are and pharmaceutical compositions containing, intermediate compounds and processes of making such compounds.Type: ApplicationFiled: April 28, 2003Publication date: December 4, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John R. Proudfoot, Alan D. Swinamer
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Patent number: 6645951Abstract: The present invention provides novel benzopyran compounds, pharmaceutically acceptable salts thereof and stereoisomers thereof where the benzopyran compounds of the invention are compounds according to Formula I: The present invention further provides pharmaceutical compositions which possess anti-estrogenic activity and comprise at least one benzopyran compound of the invention and a method of treating breast cancer by administration of an effective amount of a benzopyran compound provided by the present invention.Type: GrantFiled: July 16, 2001Date of Patent: November 11, 2003Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Jae Chon Jo, Hyun Suk Lim, Jong Min Kim, Ju Su Kim, Kazumi Morikawa, Yoshitake Kanbe, Myung Hwa Kim, Masahiro Nishimoto
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Publication number: 20030203927Abstract: Heterocyclic-substituted tricyclics of the formula 1Type: ApplicationFiled: October 16, 2002Publication date: October 30, 2003Applicant: Schering CorporationInventors: Samuel Chackalamannil, Mariappan V. Chelliah, Martin C. Clasby, Yan Xia
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Publication number: 20030166932Abstract: Compounds of the formula 1Type: ApplicationFiled: January 4, 2002Publication date: September 4, 2003Inventors: Richard L. Beard, Thong Vu, Diana F. Colon, Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Publication number: 20030158413Abstract: The present invention relates to an amide compound of the formula 1Type: ApplicationFiled: October 21, 2002Publication date: August 21, 2003Inventors: Shinichi Takanashi, Yoichiro Naito, Hiroshi Tanaka, Masayoshi Uehata, Koshiro Katayama
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Publication number: 20030130515Abstract: Compounds of the formula 1Type: ApplicationFiled: January 2, 2003Publication date: July 10, 2003Inventors: Vidyasagar Vuligonda, Alan T. Johnson, Roshantha A. Chandraratna
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Publication number: 20030078441Abstract: The invention provides photochromic bis-naphthopyran compounds as well as methods for their manufacture and their use. The bis-naphthopyran compounds of the invention exhibit a wide range of color, i.e., from pink to purple to blue gray, upon activation by a source of UV light. Additionally, the bis-naphthopyran compounds of the present invention exhibit broad coloration ability, fast response as to both color change on activation and return to original color, and good fatigue-resistance.Type: ApplicationFiled: September 4, 2001Publication date: April 24, 2003Inventors: Weili Zhao, Erick M. Carreira
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Publication number: 20030050306Abstract: A heteroaryl derivative having the formula (I) 1Type: ApplicationFiled: June 25, 2002Publication date: March 13, 2003Applicant: H. Lundbeck A/SInventors: Thomas Ruhland, Christian Krog-Jensen, Ivan Mikkelsen, Mario Rottlander, Gitte Mikkelsen, Ejner Knud Moltzen, Kim Andersen
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Patent number: 6495568Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diType: GrantFiled: October 12, 2001Date of Patent: December 17, 2002Assignee: Warner-Lambert CompanyInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Patent number: 6495576Abstract: Compounds of formula (I) may be useful in treating diseases prevented by or ameliorated with potassium channel openers.Type: GrantFiled: January 14, 2002Date of Patent: December 17, 2002Assignee: Abbott LaboratoriesInventors: Michael E. Kort, Robert J. Gregg, William A. Carroll, Arturo Perez Medrano, Jürgen Dinges, Fatima Z. Basha
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Patent number: 6489344Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.Type: GrantFiled: June 18, 1999Date of Patent: December 3, 2002Assignee: Chiron CorporationInventors: John M. Nuss, Stephen D. Harrison, David B. Ring, Rustum S. Boyce, Sean P. Brown, Dane A. Goff, Kirk W. Johnson, Keith B. Pfister, Savithri Ramurthy, Paul A. Renhowe, Lynn Seely, Sharadha Subramanian, Allan S. Wagman, Xiaohui A. Zhou
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Patent number: 6458950Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):Type: GrantFiled: August 3, 2000Date of Patent: October 1, 2002Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Koji Ishikura
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Patent number: 6458789Abstract: The present invention relates to novel 2-aminopyridine derivative compounds of the following formula: wherein R1 to R5 have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminopyridine derivative compounds.Type: GrantFiled: September 29, 1999Date of Patent: October 1, 2002Assignee: Lion Bioscience AGInventors: Behrouz Forood, Brenton T. Flatt, Christophe Chassaing, Alan K. Katritzky
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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: 6432880Abstract: 2-Phenylpyridines I an their salts, wherein R1 to R17, X1-X3 are as defined in the specification. The compounds are useful as herbicides, desiccants and defoliants.Type: GrantFiled: July 5, 2001Date of Patent: August 13, 2002Assignee: BASF AktiengesellschaftInventors: Olaf Menke, Markus Menges, Ingo Sagasser, Gerhard Hamprecht, Robert Reinhard, Cyrill Zagar, Karl-Otto Westphalen, Martina Otten, Helmut Walter
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Publication number: 20020103217Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1Type: ApplicationFiled: January 8, 2002Publication date: August 1, 2002Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, Richard Cordova, Kevin Pan, Joseph Meschino
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Patent number: 6420375Abstract: To provide a novel compound of the formula: [wherein A1 ix a 5 or 6-membered ring which may be substituted by a group not containing a cyclic group, A2 is an aromatic ring which may be substituted, X is a divalent group, Y is a nitrogen atom or a methine group, Z is an ethenylene which may be substituted or ethynylene, R is a heterocyclic group which may be substituted, provided that 3,4-dihydro-6-[3-(1H-imidazol-1-yl)-1-propenyl]-2(1H)-quinolone and 2-[3-[5-ethyl-6-methyl-2-(benzyloxy)-3-pyridyl]-1-propenyl]benzoxazole are excluded.], or a salt thereof which has steroid C17,20-lyase inhibitory activity, and is useful for preventing and treating mammals suffering from, for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.Type: GrantFiled: August 18, 1999Date of Patent: July 16, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Tetsuya Aono, Fumio Itoh, Tomohiro Kaku, Masuo Yamaoka
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Publication number: 20020091150Abstract: The present invention is a compound of formula 1Type: ApplicationFiled: December 10, 2001Publication date: July 11, 2002Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jurgen Wichmann, Thomas Johannes Woltering
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Publication number: 20020082419Abstract: Compounds of Formula 1 1Type: ApplicationFiled: November 5, 2001Publication date: June 27, 2002Applicant: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 6387931Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diType: GrantFiled: October 12, 2001Date of Patent: May 14, 2002Assignee: Pfizer INCInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Patent number: 6384045Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.Type: GrantFiled: June 24, 1999Date of Patent: May 7, 2002Assignee: Kansas State University Research FoundationInventors: Duy H. Hua, Jean-Pierre Perchellet
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Patent number: 6362183Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: March 26, 2002Assignee: G. D. Searle & CompanyInventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
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Patent number: 6340676Abstract: This invention provides compounds of Formula I having the structure wherein B and D are each, independently, hydrogen, halogen, —CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms; R1 is hydrogen, alkyl of 1-6 carbon atoms, —CH(R2)W, —C(CH3)2CO2R3, 5-thiazolidine-2,4-dione, —CH(R4)CH2CO2R3, —COR3, or —PO3(R3)2; R2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, —CH2(1H-imidazol-4-yl), —CH2(3-1H-indolyl), —CH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), —CH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), or —CH2(3-pyridyl); W is —CO R3, —CONH2, —CONHOH, —CN, CONH(CH2)2CN, 5-tetrazole, or —PO3(R3)2; R3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl; R4 is hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: April 20, 2001Date of Patent: January 22, 2002Assignee: American Home Products CorporationInventors: Jay E. Wrobel, Zenan Li
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Patent number: 6211379Abstract: The present application relates to a process for preparing compounds of the formula (I) in which R1, A, X and Z are each as defined in the description by reacting compounds of the formula (II) in which A and X are each as defined in the description with compounds of the formula (III) in which Z, R1 and M1 are each as defined in the description.Type: GrantFiled: January 20, 2000Date of Patent: April 3, 2001Assignee: Bayer AktiengesellschaftInventors: Hermann Seifert, Reinhard Lantzsch, Werner Lindner, Klaus Jelich
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Patent number: 6211385Abstract: Compounds of Formula 1 where the symbols have the meaning disclosed in the specification are prepared by reaction of a compound of Formula 2 with an organometal reagent R—M to provide a compound of Formula 3 that is reacted with the reagent X3—Y(R2)—A—B in the presence of a catalyst to provide the compounds of Formula 1.Type: GrantFiled: January 27, 2000Date of Patent: April 3, 2001Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna