Double Bonded Divalent Chalcogen Containing Patents (Class 544/54)
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Patent number: 7314932Abstract: Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrite groups, are provided.Type: GrantFiled: April 7, 2005Date of Patent: January 1, 2008Assignee: WyethInventor: Bogdan Kazimierz Wilk
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Patent number: 7223754Abstract: The invention relates to methods of using Cav2.2 subunit calcium channel modulators, particularly thiazolidinone, oxazolidinone, and imidazolone derivatives, to treat lower urinary tract and related disorders.Type: GrantFiled: November 17, 2004Date of Patent: May 29, 2007Assignee: Dynogen Pharmaceuticals, Inc.Inventors: Matthew Oliver Fraser, Karl Bruce Thor, Edward C. Burgard
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Patent number: 7183275Abstract: The present invention relates to 2-imino-1,3-thiazine derivatives, in specific, 2-imino-1,3-thiazine derivatives having a selective antagonistic activity or agonistic activity to a cannabinoid type 2 receptor and their pharmaceutical use.Type: GrantFiled: October 26, 2004Date of Patent: February 27, 2007Assignee: Shionogi Co., Ltd.Inventors: Koji Hanasaki, Takami Murashi, Hiroyuki Kai
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Patent number: 7166590Abstract: A compound of the formula (I): [wherein R1 is (substituted) alkyl, alkoxy, phenyl, hetero ring etc.; A is bond, CO, SO2; R2 is H, (substituted) alkyl etc.; D is alkylene etc.; E is COO, OCO, O, S, SO, SO2 etc.; R3 is (substituted) alkyl, carbocyclic ring, hetero ring; J is O, NR16 (R16 is H, substituted alkyl); R4 is (substituted) alkyl, carbocyclic ring, hetero ring.] or non-toxic salt thereof, and an N-type calcium channel blocker comprising it as an active ingredient. The compounds of the formula (I) possess an inhibitory action on N-type calcium channel, so they are useful as agent for the prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis or epilepsy etc. or agent for the treatment of pain.Type: GrantFiled: May 28, 2002Date of Patent: January 23, 2007Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Masashi Kato
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Patent number: 7094778Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: October 14, 2003Date of Patent: August 22, 2006Assignee: Syntex (U.S.A.) LLCInventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, III, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
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Patent number: 7015217Abstract: The present application describes novel cyclic sulfone derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof. In formula I, A is selected from —COR5, —CO2H, —CO2R6, —C(O)NHOH, —C(O)NHOR5, —C(O)NHOR6, —NHRa, —N(OH)COR5, —N(OH)CHO, —SH, —CH2SH, —S(O)(?NH)Ra, —S(?NH)2Ra, —SC(O)Ra, —PO(OH)2, and —PO(OH)NHRa; B is a thiomorpholine ring; X is absent or is CR3R4; and Ua, Xa, Ya, Za, R1, R2, Rb, and q are defined in the present specification.Type: GrantFiled: October 7, 2002Date of Patent: March 21, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, Chu-Biao Xue
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Patent number: 6936606Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases.Type: GrantFiled: September 27, 2002Date of Patent: August 30, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel
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Patent number: 6818640Abstract: It is found out that compounds represented by general formula (I) bind selectively to cannabinoid 2 receptor (CB2R) and thus exhibit CB2R antagonism or CB2R agonis wherein R1 represents optionally substituted alkylene; R2 represents hydrogen, alkyl, a group represented by the formula —C(═R5)—R6 (wherein R5 represents O or S; and R6 represents alkyl, alkoxy, alkylthio, etc.) or a group represented by the formula SO2R7 (wherein R7 represents allyl, etc.); m is an integer of from 0 to 2; and A represents optionally substituted aryl, etc.Type: GrantFiled: February 26, 2002Date of Patent: November 16, 2004Assignee: Shionogi & Co., Ltd.Inventors: Koji Hanasaki, Takami Murashi, Hiroyuki Kai
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Patent number: 6794406Abstract: The invention relates to new indole derivatives, processes for their preparation, and their use in medicaments.Type: GrantFiled: December 21, 2001Date of Patent: September 21, 2004Assignee: Bayer AktiengesellschaftInventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Hilmar Bischoff, Axel Kretschmer, Verena Vöhringer, Christiane Faeste
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Patent number: 6787522Abstract: Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n—(ALK)m— wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, anType: GrantFiled: April 30, 2002Date of Patent: September 7, 2004Assignee: British Biotech PharmaceuticalsInventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
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Patent number: 6673804Abstract: A compound of the formula (I) or a pharmacologically acceptable salt, ester or other derivative thereof: R1 is H or NHOH. R2 is H, optionally substituted alkyl, cycloalkyl or a group —AR6. A is an alkylene which may be optionally interrupted by O, —S(O)m— or —N(R9). R6 is a group (II), (III), (IV) X is O, S, —N(R10)—, —C(R11)(R12)—. Y is O, CO, —S(O)n—, —N(R10)—, —C(R11)(R12)—. Each of R7 and R8 is H, alkyl, COOH, optionally substituted alkyl, etc. Each of R9, R10, R11, and R12 is H, alkyl, etc. Each of m and n is 0 to 2. R3 is H, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted alkynyl. R4 is optionally substituted (hetero)arylene. R5 is optionally substituted alkyl, optionally substituted (hetero)aryl. These compounds have matrixmetalloproteinase—13 inhibitory activity and aglycanase inhibitory activity.Type: GrantFiled: October 2, 2000Date of Patent: January 6, 2004Assignee: Sankyo Company, LimitedInventors: Tomio Kimura, Shoujiro Miyazaki, Keiji Ueda, Kazuhiko Tanzawa, Shigeru Ushiyama, Wataru Takasaki
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Patent number: 6670359Abstract: The present invention relates to new new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.Type: GrantFiled: November 1, 2002Date of Patent: December 30, 2003Assignee: AstraZeneca ABInventors: Stefan Berg, Martin Nylöf, Svante Ross, Seth-Olov Thorberg
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Publication number: 20030232984Abstract: The method of this invention prepares acylated cyclic compounds by contacting phenyl esters as acylating agents with cyclic compounds in the presence of a cyanide or fluoride catalyst.Type: ApplicationFiled: March 24, 2003Publication date: December 18, 2003Inventor: Paul Walter Wojtkowski
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Patent number: 6656911Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: April 18, 2002Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W Spruce
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Patent number: 6642180Abstract: The present invention relates to novel biphenyl-substituted cyclic ketoenols of the formula (I) in which W represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or halogenoalkoxy, CKE represents one of the groups in which A, B, D, L, M, Q1, Q2, Q3, Q4, Q5 and Q6 are as defined in the description, to preparation and to their use as pesticides and herbicides.Type: GrantFiled: January 25, 2002Date of Patent: November 4, 2003Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht
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Publication number: 20030176418Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.Type: ApplicationFiled: December 23, 2002Publication date: September 18, 2003Inventors: Niels Skjaerbaek, Kristian Norup Koch, Bo Lennart Mikael Friberg, Bo-Ragnar Tolf
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Publication number: 20030171219Abstract: The invention relates to new phenyl-substituted cyclic ketoenols of the formula (I) 1Type: ApplicationFiled: September 19, 2002Publication date: September 11, 2003Inventors: Folker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Alan Graff, Norbert Mencke, Andreas Turberg, Peter Dahmen
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Publication number: 20030171368Abstract: The disclosure is directed to compounds of the formula (I) 1Type: ApplicationFiled: February 6, 2002Publication date: September 11, 2003Inventors: Werner Seitz, Andreas Kling, Herve Geneste, Thomas Subkowski, Claudia Graef, Wilfried Hornberger
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Patent number: 6605608Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.Type: GrantFiled: December 22, 2000Date of Patent: August 12, 2003Assignee: Ono Pharmaceutical Co., LtdInventors: Takuya Seko, Masashi Kato
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Publication number: 20030144504Abstract: The present invention relates to new compounds of the formula (I) 1Type: ApplicationFiled: July 18, 2002Publication date: July 31, 2003Inventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Michael Ruther, Arno Widdig, Peter Dahmen, Markus Dollinger, Christoph Erdelen, Hans-Joachim Santel, Ulrike Wachendorff-Neumann, Alan Graff, Wolfram Andersch
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Publication number: 20030109521Abstract: This invention relates aryl substituted thiazolidinones of Formula I: 1Type: ApplicationFiled: July 16, 2002Publication date: June 12, 2003Applicant: Euro-Celtique, S.A.Inventors: Qun Sun, Donald J. Kyle
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Patent number: 6559155Abstract: Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA2 and thereof use in treating inter alia atherosclerosis, in which: R1 is COOH or a salt thereof, COOR10, CONR11R12, CN or CH2OH; R2 is a mono- or bicyclic aromatic ring system or a mono- or bicyclic heteroaromatic ring system; R3 is C1-20alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-5alkyl, C1-10alkoxyC1-10alkyl, or an aromatic or heteroaromatic ring system; W is SO2 or a bond; X is O or S; and Y is a group of the formula A1—A2—A3 in which A1 and A3 each represent a bond or a straight chain or branched alkylene group, said alkylene group(s) containing a total of 1 to 10 carbon atoms and A2 represents a bond or O, S, SO, SO2, CO, C═CH2, CONH, NHCO, CR15R16, CH═CH or C═C, providing that when A2 is O, S, SO, SO2 or CONH, A3 contains at least two carbon atoms linking the A2 group and the CH2 group in formula (I).Type: GrantFiled: February 21, 2001Date of Patent: May 6, 2003Assignee: SmithKline Beecham p.l.c.Inventors: Colin Andrew Leach, Stephen Allan Smith
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Publication number: 20030045432Abstract: The present invention relates to new compounds of the formula (I) 1Type: ApplicationFiled: December 11, 2001Publication date: March 6, 2003Inventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Norbert Lui, Michael Ruther, Arno Widdig, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Peter Dahmen, Norbert Mencke, Andreas Turberg
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Patent number: 6485868Abstract: The invention relates to an electrolyte for an electrochemical device. This electrolyte includes an ionic metal complex represented by the general formula (1): wherein M is an element of groups 3-15 of the periodic table; Aa+ represents a metal ion, onium ion or proton; X1 represents O, S or NR5R6; each of R1 and R2 independently represents H, a halogen, a C1-C10 alkyl group or C1-C10 halogenated alkyl group; R3 represents a C1-C10 alkylene group, C1-C10 halogenated alkylene group, C4-C20 aryl group or C4-C20 halogenated aryl group; R4 represents a halogen, C1-C10 alkyl group, C1-C10 halogenated alkyl group, C4-C20 aryl group, C4-C20 halogenated aryl group or X2R7; X2 represents O, S or NR5R6; each of R5 and R6 represents H or a C1-C10 alkyl group; and R7 represents a C1-C10 alkyl group, C1-C10 halogenated alkyl group, C4-C20 aryl group or C4-C20 halogenated aryl group. The electrolyte has high heat resistance and hydrolysis resistance as compared with conventional electrolytes.Type: GrantFiled: July 25, 2000Date of Patent: November 26, 2002Assignee: Central Glass Company, LimitedInventors: Shoichi Tsujioka, Hironari Takase, Mikihiro Takahashi
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Patent number: 6469000Abstract: Disclosed are compounds which are inhibitors of metalloproteases having the following structure: where Ar, W, X, Y, Z, R1 and R2 have the meanings described in the specification and optical isomers, diastereomers, and enantiomers thereof or a pharmaceutically-acceptable salt, or biohydrolyzable amides, esters, or imides thereof. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by unwanted metalloprotease activity using these compounds or pharmaceutical compositions.Type: GrantFiled: August 29, 2000Date of Patent: October 22, 2002Assignee: The Procter & Gamble Co.Inventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Neil Gregory Almstead, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo
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Publication number: 20020123491Abstract: Compound represented by the structural formula 1Type: ApplicationFiled: December 14, 2000Publication date: September 5, 2002Inventors: Neng-Yang Shih, Ho-Jane Shue, Gregory A. Reichard, Sunil Paliwal, David J. Blythin, John J. Piwinski, Dong Xiao, Xiao Chen
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Patent number: 6410482Abstract: (Het)Arylsulfonylureas having an imino function, their preparation, and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which A is a (hetero)aromatic or heterocyclic bridge linked to the group SO2 by a direct bond, or via O, S, NH, CH2 or via alkylated NH or alkylated methylene, B is a group having an imino-containing fragment N═C—N, N═C—S, N═C—O or N═C—C which is linked to A by one of the nitrogen atoms of the fragment, R═H or an aliphatic radical, W═O or S and X, Y and Z are as defined in claim 1 are suitable as herbicides and plant growth regulators. The preparation is carried out for example similarly to known processes via novel intermediates of the formula (XII) (cf.Type: GrantFiled: May 13, 1997Date of Patent: June 25, 2002Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6407232Abstract: The invention relates an ionic metal complex represented by the general formula (1): wherein M is an element of groups 3-15 of the periodic table; Aa+ represents a metal ion, onium ion or proton; X1 represents O, S or NR5R6; each of R1 and R2 independently represents H, a halogen, a C1-C10 alkyl group or C1-C10 halogenated alkyl group; R3 represents a C1-C10 alkylene group, C1-C10 halogenated alkylene group, C4-C20 aryl group or C4-C20 halogenated aryl group; R4 represents a halogen, C1-C10 alkyl group, C1-C10 halogenated alkyl group, C4-C20 aryl group, C4-C20 halogenated aryl group or X2R7; X2 represents O, S or NR5R6; each of R5 and R6 represents H or a C1-C10 alkyl group; and R7 represents a C1-C10 alkyl group, C1-C10 halogenated alkyl group, C4-C20 aryl group or C4-C20 halogenated aryl group. The ionic metal complex can be used as a supporting electrolyte for electrochemical devices, a polymerization catalyst of polyolefins and so forth, or a catalyst for organic synthesis.Type: GrantFiled: July 25, 2000Date of Patent: June 18, 2002Assignee: Central Glass Company, LimitedInventors: Shoichi Tsujioka, Hironari Takase, Mikihiro Takahashi
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Patent number: 6395730Abstract: Certain thiazolidinone and metathiazanone compounds, as described, are useful as potassium channel inhibitors and are especially useful for the treatment of cardiac arrhythmias and other diseases, conditions and disorders.Type: GrantFiled: October 13, 2000Date of Patent: May 28, 2002Assignees: Icagen, Inc., Eli Lilly and CompanyInventors: Michael F. Gross, Neil A. Castle, Jose S. Mendoza
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Patent number: 6365587Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-1 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.Type: GrantFiled: May 13, 1999Date of Patent: April 2, 2002Inventors: Matthew E. Voss, Carl P. Decicco, Ruth R. Wexler
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Publication number: 20020022575Abstract: The present invention relates to new compounds of the formula (I) 1Type: ApplicationFiled: April 20, 2001Publication date: February 21, 2002Inventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Michael Ruther, Arno Widdig, Peter Dahmen, Markus Dollinger, Christoph Erdelen, Hans-Joachim Santel, Ulrike Wachendorff-Neumann, Alan Graff, Wolfram Andersch
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Publication number: 20020004503Abstract: A compound of the formula: 1Type: ApplicationFiled: April 18, 2001Publication date: January 10, 2002Inventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
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Patent number: 6268311Abstract: 1-Amino-3-benzyluracils I (X=oxygen, sulfur; R1=C1-C4-haloalkyl; R2=H, halogen; R3, R7=H, CN, SCN, halogen, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-haloalkylthio; R4=H, CN, SCN, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C1-C4-haloalkylthio, C1-C6-alkylaminocarbonyl; R5=H, CN, NO2, halogen, OH, C1-C4-alkoxy, NH2, C1-C6-alkyl-amino; R6=H, CN, NO2, halogen, OH, C1-C4-alkoxy, NH2, C1-C6-alkyl-amino, CHO) and their salts are used as herbicides and for the desiccation/defoliation of plants.Type: GrantFiled: March 17, 1998Date of Patent: July 31, 2001Assignee: BASF AktiengesellschaftInventors: Olaf Menke, Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schäfer, Cyrill Zagar, Norbert Götz, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
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Patent number: 6217848Abstract: Dye-peptide conjugates useful for diagnostic imaging and therapy are disclosed. The dye-peptide conjugates include several cyanine dyes with a variety of bis- and tetrakis(carboxylic acid) homologues. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350-1300 nm, the exact range being dependent upon the particular dye. Use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The molecules of the invention are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities and for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.Type: GrantFiled: June 4, 1999Date of Patent: April 17, 2001Assignee: Mallinckrodt Inc.Inventors: Samuel Achilefu, Richard Bradley Dorshow, Joseph Edward Bugaj, Raghavan Rajagopalan
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Patent number: 6172060Abstract: Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.Type: GrantFiled: February 10, 1999Date of Patent: January 9, 2001Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada
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Patent number: 6156794Abstract: A method of using a compound of formula (I) wherein R.sup.1, R.sup.2, R.sup.3, X and n have any of the meanings defined in the specification, to antagonize glutamate binding, or to treat glutamate-related disorders is provided. Novel compounds, intermediates and pharmaceutical compositions are also provided.Type: GrantFiled: September 13, 1999Date of Patent: December 5, 2000Inventors: Morris Faiman, John V. Schloss, Jang-Yen Wu
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Patent number: 6114327Abstract: The present application provides a series of benzimidazole compounds of formula I: ##STR1## which inhibit the growth of picornaviruses, such as rhinoviruses (bovine and human), enteroviruses such as polioviruses, coxsackieviruses of the A and B groups, or echo virus, cardioviruses such as encephalomyocarditis (EMC), apthoviruses such as foot and mouth disease virus, and flaviviruses such as hepatitis C virus and bovine viral diarrhea virus.Such compounds are also useful as intermediates for preparing additional benzimidazole antiviral compounds.Type: GrantFiled: October 22, 1999Date of Patent: September 5, 2000Assignee: Eli Lilly and CompanyInventors: Steven Eugene Dunlap, Louis Nickolaus Jungheim, Mark Joseph Tebbe, Gilbert Thomas Voy, John Arnold Werner
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Patent number: 6048824Abstract: Compounds of formula (I), wherein A is an unsubstituted or substituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical wherein a ring nitrogen atom may have been replaced by a group ##STR2## R.sub.1 is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.3 is hydrogen, an unsubstituted or substituted C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl group, or C(.dbd.O)--R.sub.5, R.sub.5 is C.sub.1 -C.sub.4 alkyl C.sub.1 -C.sub.4 alkoxy, an unsubstituted or substituted phenyl, phenoxy or benzyloxy group, or N(R.sub.6).sub.2, each R.sub.6, independently of the other, is hydrogen, C.sub.1 -C.sub.4 alkyl or unsubstituted or substituted phenyl, X is CH--NO.sub.2, N--CN or N--NO.sub.2 and n is from 1 to 3, in free form or in salt form, and, where appropriate, tautomers of those compounds and the salts thereof, can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: November 22, 1995Date of Patent: April 11, 2000Assignee: Novartis CorporationInventors: Peter Maienfisch, Jozef Gonda, Olivier Jacob, Laurenz Gsell
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Patent number: 6048999Abstract: This invention provides sweetener blends comprising N-[N-(3,3-dimethylbutyl)-L-.alpha.-aspartyl]-L-phenylalanine 1-methyl ester and another sweetener. The sweetener blends of this invention exhibit isobole synergy.Type: GrantFiled: January 25, 1999Date of Patent: April 11, 2000Assignee: The NutraSweet CompanyInventors: Laurie L. Pajor, Kernon M. Gibes
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Patent number: 6008223Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: January 20, 1998Date of Patent: December 28, 1999Assignee: Zeneca LimitedInventors: Peter R. Bernstein, Scott C. Miller
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Patent number: 5965565Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: December 11, 1997Date of Patent: October 12, 1999Assignee: Merck & Co., Inc.Inventors: Meng H. Chen, Zhijian Lu, Ravi Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang, Mu Tsu Wu
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Patent number: 5861380Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.Type: GrantFiled: December 6, 1996Date of Patent: January 19, 1999Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5854241Abstract: Disclosed are pyrido?3,2,1-i,j!?3,1!benzoxazine compounds of the formula (I): ##STR1## wherein z represents a radical having the formula: ##STR2## wherein B represents --CH.sub.2 --, --O-- or a direct bond; and the other variables in formula (I) and Z are as described herein. The compounds have antibacterial properties and also disclosed are antibacterial compositions containing them and methods of using them to prevent or combat bacterial infections. Methods for preparing the compounds are also disclosed.Type: GrantFiled: January 3, 1997Date of Patent: December 29, 1998Assignee: Bayer AktiengesellschaftInventors: Werner Hallenbach, Thomas Himmler, Thomas Jaetsch, Burkhard Mielke, Klaus Dieter Bremm, Rainer Endermann, Franz Pirro, Michael Stegemann, Heinz-Georg Wetzstein
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Patent number: 5847115Abstract: There is disclosed an azetidinone compound of the formula ?I!: ##STR1## wherein Ring B is a benzene ring which may have substituent(s), R.sup.1 is a hydroxy-substituted lower alkyl group which may have substituent(s), X is oxygen atom and the like, Y is oxygen atom and the like, and Z is a methylene group which may have substituent(s), which is useful as a synthetic intermediate of the 1 .beta.-methylcarbapenem-type antibacterial agent.Type: GrantFiled: November 1, 1996Date of Patent: December 8, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tameo Iwasaki, Kazuhiko Kondo
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Patent number: 5840732Abstract: This invention provides a new condensed imidazole compound possessing inhibitory activity of adhesion molecule expression.This invention also provides a therapeutic and prophylactic agent for diabetic nephritis and/or autoimmune disease and an immunosuppressor for organ transplantation.Type: GrantFiled: December 6, 1996Date of Patent: November 24, 1998Assignee: Takeda Chemical Industries Ltd.Inventors: Muneo Takatani, Hitoshi Ikeda, Kyoko Iida, Hidenori Abe
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Patent number: 5789404Abstract: 3-Substituted 1-arylindole compounds are provided having general formula (I) ##STR1## wherein Ar is an optionally substituted aryl group; X represents a divalent hydrocarbon group, methyleneoxy or -thioxo; R.sup.1 -R.sup.4 are hydrogen or other substituents; R.sup.5 is hydrogen, alkyl, alkenyl, etc.; R.sup.6 and R.sup.7 are independently hydrogen, alkyl, alkenyl, etc.; R.sup.8 is alkyl, alkenyl or R.sup.8 represents a group of formula 1a or 1b; wherein n is an integer from 2-8; W is O or S; U is N or CH; Z is (CH.sub.2).sub.m, m being 2 or 3, 1,2-phenylene optionally substituted with halogen or trifluoromethyl, CH.dbd.CH, COCH.sub.2 or CSCH.sub.2 ; V is O, S, CH.sub.2 or NR.sup.10, wherein R.sup.10 is hydrogen, alkyl, alkenyl, cycloalkyl, etc.; U.sup.1 is O, S, CH.sub.2 or a group NR.sup.11, wherein R.sup.11 is hydrogen, alkyl, alkenyl, etc.; and V.sup.1 is NR.sup.12 R.sup.13, OR.sup.14, SR.sup.15 or CR.sup.16 R.sup.17 R.sup.18, where R.sup.12 -R.sup.18 are as the R.sup.10 substituents; R.sup.Type: GrantFiled: August 12, 1996Date of Patent: August 4, 1998Assignee: H. Lundbeck A/SInventors: Kim Andersen, Jens Kristian Perregaard
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Patent number: 5760033Abstract: A compound represented by the chemical formula ?1!: ##STR1## wherein Z is oxygen or sulfur, Y is halogen, optionally substituted alkyl, optionally substituted alkoxycarbonyl, optionally substituted alkoxy, S(O).sub.p r.sup.1 wherein p denotes an integer from 0 to 2, r.sup.1 is optionally substituted alkyl, nitro, cyano or optionally substituted amino, m denotes an integer from 1 to 3, R.sub.1, R.sub.2 and R.sub.4 are same or different one another and each independently hydrogen, optionally substituted alkyl or optionally substituted phenyl, R.sub.3 is alkyl, alkenyl, aralkyl, cycloalkyl, phenyl, naphthyl, pyridyl, furyl or thienyl, those which substituents can be further optionally substituted by halogen, hydroxy, optionally substituted alkyl or the like, and a chemical agent for controlling pests.Type: GrantFiled: August 25, 1995Date of Patent: June 2, 1998Inventors: Yasuo Yamada, Takashi Kishimoto, Michihiko Matsuda, Renpei Hatano, Takao Iwasa, Makio Yano
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Patent number: 5739130Abstract: Heterotricyclic derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino,R.sup.2 is hydroxy, protected hydroxy, halogen, amino or protected amino,R.sup.3 is hydrogen or an organic group,R.sup.4 is hydrogen or lower alkyl,R.sup.8 is hydrogen or lower alkyl, and--Z-- is --O-- or a group of the formula: ##STR2## (in which n is 0, 1 or 2), and pharmaceutically acceptable salts thereof which are useful as a medicament.Type: GrantFiled: September 4, 1996Date of Patent: April 14, 1998Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Kiyoshi Tsuji, Katsuya Nakamura, Glen W. Spears
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Patent number: 5686454Abstract: The invention is directed to a series of novel compounds of the formula ##STR1## where Y is carbonyl or sulfonyl; R.sup.7 and R.sup.8 are alkyl, or R.sup.7 and R.sup.8, together with the carbon to which they are attached, form a C.sub.3-6 carbocyclic ring; R.sup.9 and R.sup.10 are each independently selected from hydrogen, hydroxyl, oximido, methyl, carboxyl, carboxyalkyl, unsubstituted or substituted alkoxycarbonyl, alkylcarbonyloxyalkyl, cyanoalkyl, hydroxyalkyl or unsubstituted amino; R.sup.11 is hydrogen, oxo, --N(R.sup.12)--CO--R.sup.13 or --CO--N(R.sup.14)--R.sup.15 ; R.sup.12 is hydrogen or unsubstituted or substituted alkyl; R.sup.13 is alkoxyl, unsubstituted or substituted heterocyclic rings selected from ##STR2## or unsubstituted or substituted alkyl; and R.sup.14 and R.sup.15 are each independently selected from hydrogen or unsubstituted or substituted alkyl. The Y moiety cannot be bonded to the camphor ring at the 3 or 6 positions.Type: GrantFiled: January 16, 1996Date of Patent: November 11, 1997Assignee: Merck & Co., Inc.Inventors: Mark G. Bock, Doug W. Hobbs
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Patent number: RE39130Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally substituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: June 6, 1994Date of Patent: June 13, 2006Assignee: Bayer Cropscience K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori