The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 549/498)
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Publication number: 20100210524Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, wherein W, X, Y, Z, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15 and R16 are as defined in the specification. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.Type: ApplicationFiled: July 21, 2008Publication date: August 19, 2010Inventors: Theresa Apelqvist, Joakim Löfstedt, Thomas Norin, Mattias Wennerstål, Xiongyu Wu, Lars Hagberg
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Publication number: 20100111888Abstract: Disclosed are compounds having the ability to modulate, namely to improve, enhance and or modify fragrance compositions due to their ability to inhibit cytochrome P450 enzymes, e.g. CYP2A13 and CYP2B6.Type: ApplicationFiled: March 20, 2008Publication date: May 6, 2010Applicant: GIVAUDAN SAInventors: Boris Schilling, Thierry Granier, Georg Frater, Andreas Hanhart
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Publication number: 20100113460Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.Type: ApplicationFiled: March 20, 2008Publication date: May 6, 2010Applicant: Givaudan SAInventors: Boris Schilling, Wolf D. Woggon, Antoinette Chougnet, Thierry Granier, Georg Frater, Andreas Hanhart
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Patent number: 7579484Abstract: The invention relates to monoalkylaminoketones of the formula (I), in which R1 and R2 have the meanings indicated.Type: GrantFiled: August 1, 2003Date of Patent: August 25, 2009Assignee: Merck Patent GmbHInventors: Kai Fabian, Claus-Peter Niesert, Joachim Kralik, Karl-Heinz Glüsenkamp
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Publication number: 20090062516Abstract: Lignin polymers having distinctive properties, including a generally high molecular weight and generally homogeneous size distribution, as well as preservation of native reactive side groups, are isolated by solvent extraction of plant materials. Methods for isolation of lignin polymers, and for use of the isolated lignin polymers are disclosed. Compositions containing lignin isolated from plant materials, such as carbon fiber composites, resins, adhesive binders and coatings, polyurethane-based foams, rubbers and elastomers, plastics, films, paints, nutritional supplements, food and beverage additives are disclosed. Xylose and xylose derivatives, furfural, fermentable sugars, cellulose and hemi-cellulose products may be used directly or further processed. The lignin polymers and other plant-derived products disclosed herein may be produced in abundance at low cost, and may be used as substitutes for feedstocks originating from fossil fuel or petrochemical sources in the manufacture of various products.Type: ApplicationFiled: September 2, 2008Publication date: March 5, 2009Applicant: BIOJOULE LIMITEDInventors: Helene BELANGER, Ross L. PRESTIDGE, Tony James LOUGH, James D. WATSON
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Publication number: 20080145901Abstract: The present invention provides novel methods for preparing a key intermediate, 3,5-di-O-acyl-2-fluoro-2-C-methyl-D-ribono-?-lactone (2), for the preparation of 1-(2-deoxy-2-fluoro-2-C-methyl-?-D-ribofuranosyl)cytosine (1), which is a potent and selective anti-hepatitis C virus agent.Type: ApplicationFiled: December 11, 2007Publication date: June 19, 2008Inventors: Miall Cedilote, Thomas Cleary, Hans Iding, Pingsheng Zhang
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Publication number: 20080090900Abstract: This invention describes a new antibiotic, hereinafter designated as bushrin, having the formula C16H16O2, which is 7-(3-furyl)-3,7-dimethyl-7,8-dihydro-1-naphthalenol, its production method by fermentation, and the methods related to its recovery, concentration and purification from the crude solutions. The invention includes within its scope the agent in dilute form, as a crude concentrate, and in pure form. The invention also relates to the use of the compound according to the invention in antimicrobial compositions and as antiseptics or disinfectants.Type: ApplicationFiled: October 12, 2006Publication date: April 17, 2008Applicant: University of KarachiInventors: Nuzhat Ahmed, Bushra Uzair, Viqar Uddin Ahmad, Farzana Kousar
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Patent number: 7312181Abstract: The present invention provides compounds of Formula I: wherein Ar1 is aryl or heteroaryl, Ar2 is aryl or heteroaryl, and R is a suitable organic group. Herbicidal composition comprising such active compounds, and methods for controlling undesirable plants by applying such compounds, are also described.Type: GrantFiled: March 22, 2006Date of Patent: December 25, 2007Assignee: Cropsolution, Inc.Inventors: Shy-Fuh Lee, Vivian Du, Richard Anderson
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Publication number: 20070232813Abstract: The present invention is generally directed to the use of L-proline and certain derivatives thereof to catalyze the asymmetric self-condensation of ?,?-unsaturated aldehydes to form homodimer and heterodimer cyclohexadienals. Reaction conditions are mild and yet amenable to a variety of different substrates yielding molecules with complex scaffolds from simple precursors. This approach allows for diversification and synthesis of this structural class of compounds in sufficient quantity, purity and enantioselectivity for, e.g., biological investigations and use as fluorescent probes, anti-cancer agents, anti-bacterial agents, and/or anti-fungal agents. The present invention is also generally directed to the cyclohexadienals produced.Type: ApplicationFiled: March 28, 2007Publication date: October 4, 2007Inventors: Coran M. H. Watanabe, Bennie John Bench
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Publication number: 20070197806Abstract: A carbonyl compound represented by following Formula (1): wherein R1 represents hydrogen atom or an organic group; and R2 represents hydrogen atom or an organic group having a carbon atom at a bonding site with the carbonyl group in Formula (1), wherein R1 and R2 may be combined to form a ring with adjacent two carbon atoms, or an equivalent thereof is reacted with an unsaturated compound represented by following Formula (2): wherein each of R3, R4, and R5 represents hydrogen atom, a halogen atom, hydroxyl group, or an organic group and wherein R3 and R4 may be combined to form a ring with adjacent two carbon atoms, or a precursor thereof, to yield a furan compound represented by following Formula (3): wherein R3? represents R3, R5 or hydrogen atom; and R1, R2, R3, R4, are R5 are as defined above.Type: ApplicationFiled: February 22, 2007Publication date: August 23, 2007Inventors: Yasutaka Ishii, Tatsuya Nakano, Takahiro Iwahama
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Patent number: 7202247Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: December 19, 2002Date of Patent: April 10, 2007Assignee: AtheroGenics, Inc.Inventors: James A. Sikorski, Charles Q. Meng, M. David Weingarten
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Patent number: 7196089Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): ?wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.Type: GrantFiled: January 29, 2004Date of Patent: March 27, 2007Assignee: Asterand UK LimitedInventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
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Patent number: 7135574Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein the substituents are as defined in claim 1, by conversion of a compound of formula II reaction of that compound with a compound of formula IV X—C(O)—Q,??(IV) wherein X is a leaving group, to form a compound of formula V and treatment of that compound in the presence of a base with catalytic amounts of cyanide ions.Type: GrantFiled: February 11, 2005Date of Patent: November 14, 2006Assignee: Syngenta Crop Protection, Inc.Inventors: Hermann Schneider, Christoph Lüthy, Andrew Edmunds
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Publication number: 20040248943Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: July 8, 2002Publication date: December 9, 2004Applicant: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
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Publication number: 20040198933Abstract: Photoiniferters for controlled radical polymerizations are described. The photoiniferters have an azlactone or ring-opened azlactone moiety to provide telechelic (co)polymers.Type: ApplicationFiled: April 12, 2004Publication date: October 7, 2004Applicant: 3M Innovative Properties CompanyInventors: Michael S. Wendland, Kevin M. Lewandowski, Duane D. Fansler, Babu N. Gaddam, Steven M. Heilmann
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Patent number: 6762198Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where J, M, Q, T, W, X, Z, R1, R2, R3, R4, R4′, R5, R6, R6′, R7, m, and n have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also disclosed are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.Type: GrantFiled: March 25, 2003Date of Patent: July 13, 2004Assignee: The Procter & Gamble CompanyInventors: Menyan Cheng, Neil Gregory Almstead, Michael George Natchus, Stanislaw Pikul, Biswanath De
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Patent number: 6753391Abstract: Chain transfer agents for controlled radical polymerizations (RAFT) are described. The chain transfer agents have an azlactone or ring-opened azlactone moiety to provide telechelic (co)polymers.Type: GrantFiled: May 5, 2003Date of Patent: June 22, 2004Assignee: 3M Innovative Properties CompanyInventors: Kevin M. Lewandowski, Duane D. Fansler, Michael S. Wendland, Babu N. Gaddam, Steven M. Heilmann
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Patent number: 6747104Abstract: Photoiniferters for controlled radical polymerizations are described. The photoiniferters have an azlactone or ring-opened azlactone moiety to provide telechelic (co)polymers.Type: GrantFiled: March 21, 2003Date of Patent: June 8, 2004Assignee: 3M Innovative Properties CompanyInventors: Michael S. Wendland, Kevin M. Lewandowski, Duane D. Fansler, Babu N. Gaddam, Steven M. Heilmann
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Patent number: 6720425Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: December 9, 2002Date of Patent: April 13, 2004Assignee: Allergan, Inc.Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Publication number: 20040049037Abstract: This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.Type: ApplicationFiled: July 3, 2003Publication date: March 11, 2004Inventors: Colin M. Tice, Enrique L. Michelotti, Robert E. Hormann
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Patent number: 6620841Abstract: A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORA wherein RA is hydrogen or ester residue, —CONRBRC wherein RB and RC each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.Type: GrantFiled: June 7, 2001Date of Patent: September 16, 2003Assignee: Shionogi & Co., Ltd.Inventors: Toshio Fujishita, Tomokazu Yoshinaga, Akihiko Sato
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Patent number: 6566381Abstract: Heterocyclic substituted compounds having the general structure: which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.Type: GrantFiled: March 1, 2000Date of Patent: May 20, 2003Assignee: The Procter & Gamble CompanyInventors: Menyan Cheng, Neil Gregory Almstead, Michael George Natchus, Stanislaw Pikul, Biswanath De
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Patent number: 6559100Abstract: Substituted 2-benzoylcyclohexane-1,3-diones of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR3, —OCOR3, —OSO2R3, —S(O)nR3, —SO2OR3, —SO2N(R3)2, —NR3SO2R3 or —NR3COR3; R3 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl or phenyl-C1-C6-alkyl; where the abovementioned alkyl radicals may be partially or fully halogenated and/or may carry one to three of the following groups: hydroxyl, mercapto, amino, cyano, R3, —OR3, —SR3, —N(R3)2, ═NOR3, —OCOR3, —SCOR3, —NR3COR3, —CO2R3, —COSR3, —CON(R3)2, C1-C4-alkyliminooxy, C1-C4-alkoxyamino, C1-C4-alkylcarbonyl, C1-C4-alkoxy-C2-C6-alkoxycarbonyl, C1-C4-alkylsulfonyl, heterocyclyl, heterocyclyloxy, phenyl, benzyl, hetaryl, phenoxy, benzyloxy and hetaryloxy, where the eight last mentioned radicType: GrantFiled: February 7, 2000Date of Patent: May 6, 2003Assignee: BASF AktiengesellschaftInventors: Stefan Engel, Joachim Rheinheimer, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Matthias Witschel, Martina Otten, Helmut Walter, Karl-Otto Westphalen
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Patent number: 6555690Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: May 8, 2002Date of Patent: April 29, 2003Assignee: Allergan, Inc.Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Publication number: 20030073722Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: July 8, 2002Publication date: April 17, 2003Applicant: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
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Patent number: 6515137Abstract: Acid addition salts of imidazolidinones are provided as catalysts for transforming a functional group within a first reactant by reaction with a second reactant. Exemplary first reactants are &agr;,&bgr;-unsaturated carbonyl compounds such as &agr;,&bgr;-unsaturated ketones and &agr;,&bgr;-unsaturated aldehydes. Chiral imidazolidinone salts can be used to catalyze enantioselective reactions, such that a chiral product is obtained from a chiral or achiral starting material in enantiomerically pure form.Type: GrantFiled: July 30, 2001Date of Patent: February 4, 2003Assignee: The Regents of the University of CaliforniaInventors: David W. C. MacMillan, Kateri A. Ahrendt
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Patent number: 6420392Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.Type: GrantFiled: October 9, 1996Date of Patent: July 16, 2002Assignee: Millennium Pharmaceuticals, Inc.Inventors: Tesfaye Biftu, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, T Y Shen
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Publication number: 20020082440Abstract: This invention relates to a method of preparing a compound type where at least one of R′ or R″ is a carboxyl group (I) by treating a compound of formula (II) with a Group I(a) or Group II(a) metal halide, with an aprotic dipolar amide-based solvent and water.Type: ApplicationFiled: November 8, 2001Publication date: June 27, 2002Applicant: SmithKline Beecham CorporationInventors: Kevin Webb, Wilford Mendelson, Jianhao Chen
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Patent number: 6376429Abstract: Benzoylcyclohexanediones of the formula (I), process for their preparation and their use as herbicides and plant growth regulators are described. In this formula (I), R11, R2, R3, R4, R5, R6 and R7 are various radicals, L is an alkylene chain, and Y and Z are a monoatomic bridge element.Type: GrantFiled: October 7, 1999Date of Patent: April 23, 2002Assignee: Hoechst Schering AgrEvo GmbHInventors: Andreas Van Almsick, Lothar Willms, Thomas Auler, Hermann Bieringer, Christopher Rosinger
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Publication number: 20020010337Abstract: The invention relates to novel stilbene compounds having the general formula (I): 1Type: ApplicationFiled: February 21, 2001Publication date: January 24, 2002Inventors: Jean-Michel Bernardon, Bruno Charpentier
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Patent number: 6316630Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.Type: GrantFiled: June 6, 2000Date of Patent: November 13, 2001Assignee: Sloan Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, DongFang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J Sorensen, Aaron Balog, Kenneth A. Savin
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Patent number: 6277833Abstract: Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.Type: GrantFiled: September 24, 1998Date of Patent: August 21, 2001Assignee: Bayer AktiengesellschaftInventors: Rolf Angerbauer, Peter Fey, Walter Hübsch, Thomas Philipps, Hilmar Bischoff, Hans-Peter Krause, Jörg Petersen von Gehr, Delf Schmidt
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Patent number: 6258822Abstract: Compounds having the formula are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions and a method of inhibiting urokinase in a mammal.Type: GrantFiled: August 6, 1998Date of Patent: July 10, 2001Assignee: Abbott LaboratoriesInventors: Andrew G. Geyer, William J. McClellan, Todd W. Rockway, Kent D. Stewart, Moshe Weitzberg, Michael D. Wendt
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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: 6204388Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.Type: GrantFiled: February 24, 1999Date of Patent: March 20, 2001Assignee: Sloan-Kettering Institute For Cancer ResearchInventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, DongFang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J Sorensen, Aaron Balog, Kenneth A. Savin, Scott Kuduk, Christina Harris, Xiu-Guo Zhang, Joseph R. Bertino
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Patent number: 6201013Abstract: Compounds of the formula: are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simples viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses −6 and −7, and Kaposi herpes virus.Type: GrantFiled: November 22, 1999Date of Patent: March 13, 2001Assignee: American Home Products CorporationInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Thomas Jones, Stanley Lang, Adma Ross, Eugene A. Terefenko, Bryan O'Hara
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Patent number: 6191292Abstract: The invention relates to precursors of the A-ring of vitamin D, of the formula (I): in which A, R, R1 and R2 are as defined in the specification. The invention also relates to a method of preparing compounds (I) comprising the enzymatic asymmetrization of 3,5-dihydroxybenzoic acid derivatives, as well as intermediates of preparation of said compounds.Type: GrantFiled: December 8, 1999Date of Patent: February 20, 2001Assignee: Laboratoire TheramexInventors: Jean-Claude Pascal, Maurits Vandewalle, Philippe Maillos, Pierre De Clercq
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Patent number: 6160129Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The compounds used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate .alpha. configuration; the solid triangle is used to indicate .beta. configuration; dashed bonds represent a double bond, or a single bond; R is a substituted heteroaryl radical having at least two pendant substituents selected from the group consisting of C.sub.1 to C.sub.6 alkyl; halogen; trifluoromethyl; COR.sup.1 ; COCF.sub.3 ; SO.sub.2 NR.sup.1 ; NO.sub.2 and CN or at least one cyano group; R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2 ; Y is .dbd.Type: GrantFiled: February 1, 1999Date of Patent: December 12, 2000Assignee: Allergan Sales, Inc.Inventor: Robert M. Burk
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Patent number: 6153759Abstract: Heterocyclic substituted benzoyl derivatives of the formula ##STR1## where Z is a 5-membered or 6-membered heterocyclic, saturated or unsaturated radical containing one to three hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen, useful as intermediates for herbicidal compounds.Type: GrantFiled: January 7, 1999Date of Patent: November 28, 2000Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Franz Rohl, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
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Patent number: 6153770Abstract: The invention relates to new furfurylthioalkanes of the formula ##STR1## wherein n can be zero or 1R represents the methyl or ethyl radical if n is 0, and represents hydrogen or the methyl radical if n is 1, andR' represents methyl or ethyl,a process for their preparation and their use as aroma substances.Type: GrantFiled: June 5, 1997Date of Patent: November 28, 2000Assignee: Haarmann & ReimerInventors: Heinz-Jurgen Bertram, Peter Werkhoff, Matthias Guntert
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Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 6040274Abstract: 2- Aroylcyclohexanediones I ##STR1## where X, Y=O or S;Ar=phenyl or heteroaryl in each case having 1-4 substituents: halogen, cyano, nitro, --N.dbd.N--Ph, C.sub.1 -C.sub.4 -alkoxycarbonyl, --N(R.sup.9)--COR.sup.10, --N(R.sup.9)--SO.sub.2 --R.sup.11, --SO.sub.2 --N(R.sup.9)R.sup.10, --S(O).sub.m --R.sup.8 or opt. subst. C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl or C.sub.1 -C.sub.4 -haloalkoxy;two adjacent C atoms of the phenyl or heteroaryl ring can also be bridged by means of a chain --C(R.sup.12).dbd.C(R.sup.13)--C(R.sup.14).dbd.C(R.sup.15)--, --Z.sup.1 --C(R.sup.12).dbd.N--, --Z.sup.1 --N.dbd.C(R.sup.12)--, --Z.sub.1 --C(R.sup.12).dbd.C(R.sup.13)--, --Z.sup.1 --C(R.sup.12).dbd.C(R.sup.13)--C(R.sup.14,R.sup.15)--, --Z.sup.1 --C (R.sup.12,R.sup.13)--C(R.sup.14,R.sup.15)--, --Z.sup.1 --C(R.sup.12,R.sup.13)--C(R.sup.14 R.sup.15)--Z.sup.2 --, --C(R.sup.12,R.sup.13)--Z.sup.1 --C(R.sup.14,R.sup.15)--C(R.sup.16,R.sup.17)--, --Z.sup.1 --N(R.sup.20)--Z.sup.2 --, --Z.sup.1 --Z.sup.Type: GrantFiled: March 18, 1997Date of Patent: March 21, 2000Assignee: BASF AktiengesellschaftInventors: Jurgen Kast, Marcus Vossen, Wolfgang von Deyn, Stefan Engel, Regina Luise Hill, Uwe Kardorff, Martina Otten, Peter Plath, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
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Patent number: 6004903Abstract: Benzoyl derivatives of the formula I ##STR1## where Z is a 5-membered or 6-membered heterocyclic, saturated or unsaturated radical containing one to three hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen,Q is a cyclohexane-1, 3-dione ring bonded in the 2-position and of the formula II, ##STR2## or conventional agricultural salts of the compounds I.Type: GrantFiled: August 14, 1997Date of Patent: December 21, 1999Assignee: Basf AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Franz Rohl, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
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Patent number: 5952316Abstract: 2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients.The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.Type: GrantFiled: August 14, 1997Date of Patent: September 14, 1999Assignees: Yoshitomi Pharmaceutical Industries, Ltd., Taito Co., Ltd.Inventors: Tetsuro Fujita, Shigeo Sasaki, Masahiko Yoneta, Tadashi Mishina, Kunitomo Adachi, Kenji Chiba
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Patent number: 5939268Abstract: This invention features methods of synthesizing combinatorial libraries of chemical compounds, and combinatorial libraries of chemical compounds formed by the methods of this invention. Specifically, Diels-Alder chemistry is utilized to generate libraries of diverse molecules which are easily differentially functionalized with various chemical moities and in one aspect are configured to act as non-hydrolyzable peptidomimetics.Type: GrantFiled: July 26, 1994Date of Patent: August 17, 1999Assignee: The Scripps Research InstituteInventor: Dale L. Boger
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Patent number: 5912388Abstract: A process for preparing an aldehyde or ketone comprising reacting a primary or secondary alcohol with oxygen in the presence of a base, a catalytic amount of a copper salt and a suitable lignad under anhydrous conditions.Type: GrantFiled: November 12, 1997Date of Patent: June 15, 1999Assignee: Zeneca LimitedInventors: Christopher John Urch, Istvan Ettienne Marko, Masao Tuskazaki, Paul Richard Giles, Stephen Martin Brown
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Patent number: 5856323Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: June 7, 1995Date of Patent: January 5, 1999Assignee: CytoMed, Inc.Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5780629Abstract: The invention relates to chiral compounds containing at least one divalent or polyvalent chiral group, at least one polymerizable group, at least one spacer and at least one mesogenic group, and to their use as polymerizable, chiral dopes for the preparation of cholesteric networks. The novel compounds are suitable for use in electro-optical displays or as chiral dopes for nematic or cholesteric liquid crystals in order to produce layers which reflect in colors.Type: GrantFiled: June 6, 1996Date of Patent: July 14, 1998Assignee: BASF AktiengesellschaftInventors: Karl-Heinz Etzbach, Paul Delavier, Karl Siemensmeyer, Gerhard Wagenblast, Lothar Laupichler, Volkmar Vill
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Patent number: 5767141Abstract: Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseasesPropane derivatives of the formula I ##STR1## in which the radicals have the meanings stated in the description, a process for the preparation of these compounds, their use as pharmaceuticals, and pharmaceutical products are described. Also described are novel intermediates for preparing the compounds of the formula I.Type: GrantFiled: March 8, 1995Date of Patent: June 16, 1998Assignee: Hoechst AktiengesellschaftInventors: Gerrit Schubert, Horst Hemmerle, Peter Below, Andreas Herling, Hans-Jorg Burger
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Patent number: 5723681Abstract: The present invention relates to novel 3,3-(disubstituted)cyclohexan-1-ol dimers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).Type: GrantFiled: June 23, 1997Date of Patent: March 3, 1998Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski