Plural Nitrogens In The Hetero Ring Patents (Class 540/489)
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Patent number: 9447118Abstract: The problem to be solved is to provide a method for efficiently producing compounds (1) and (1a) that are important intermediate compounds in the production of FXa inhibitors (X) and (X-a). The solutions thereto are a method for producing a compound represented by the formula (8d) using a stereoselective intramolecular cyclization reaction, and a method for producing a compound (1f) or a salt thereof, or a hydrate thereof, which is characterized by desulfonylation of the compound (8d). In each formula, R4a represents a C1-C6 alkyl group, a benzyl group, etc.Type: GrantFiled: July 21, 2015Date of Patent: September 20, 2016Assignee: Daiichi Sankyo Company, LimitedInventors: Yoshitaka Nakamura, Makoto Michida, Takeshi Kaneda
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Publication number: 20140350243Abstract: The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices.Type: ApplicationFiled: August 7, 2014Publication date: November 27, 2014Applicant: Merch Patent GmbHInventors: Amir Hossain Parham, Christof Pflumm, Teresa Mujica-Fernaud
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Publication number: 20140302988Abstract: The invention relates to novel compounds of the formula (I) in which X, Y and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions comprising, firstly, the 1,2,4-triazolyl-substituted ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, 1,2,4-triazolyl-substituted ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.Type: ApplicationFiled: August 10, 2012Publication date: October 9, 2014Applicant: Bayer Intellectual Property GMBHInventors: Wolfgang Gienckle, Stefan Lehr, Reiner Fischer, David Stephen Lindell, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Angela Becker, Arnd Voerste, Ulrich D.I. Goergens
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Patent number: 8809318Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.Type: GrantFiled: November 11, 2009Date of Patent: August 19, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Zhaoning Zhu, William J. Greenlee, Hongmei Li, Monica L. Vicarel, Jun Qin, Pawan Kumar Dhondi, Xianhai Huang, Anandan Palani, Xiaoxiang Liu, Zhong-Yue Sun, Hubert B. Josien, Ruo Xu, David James Cole, Duane A. Burnett, Chad E. Bennett, Troy McCracken, Malcolm MacCoss
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Publication number: 20140220122Abstract: The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo.Type: ApplicationFiled: April 7, 2014Publication date: August 7, 2014Applicant: BHI Limited PartnershipInventors: Xianqi KONG, Mohamed ATFANI, Benoit BACHAND, Abderrahim BOUZIDE, Stephane CIBLAT, Sophie LEVESQUE, David MIGNEAULT, Isabelle VALADE, Xinfu WU, Daniel DELORME
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Publication number: 20140142299Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: ApplicationFiled: January 23, 2014Publication date: May 22, 2014Applicant: G1 Therapeutics, Inc.Inventors: Francis X. Tavares, Jay C. Strum
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Patent number: 8318719Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-II: wherein, variables Q1, Q2, R, X, Y1, Y2, Y2?, Y3, Y4, Y5, m, and p are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-II and at least one carrier, diluent or excipient.Type: GrantFiled: April 23, 2010Date of Patent: November 27, 2012Assignee: Roche Palo Alto LLCInventors: Nolan James Dewdney, Ronald Charles Hawley, Rama Kondru, Yingjie Lai, Yan Lou
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Publication number: 20120183954Abstract: Chemically reactive dyes that are intramolecularly crosslinked with a water-soluble bridge, their bioconjugates and their uses are described. Reactive fluorescent dyes that have a water-soluble bridge are superior to those of conjugates of spectrally non-crosslinked dyes or the dyes that are crosslinked with a hydrophobic bridge. The invention includes reactive fluorescent dyes, their biological conjugates and uses.Type: ApplicationFiled: July 12, 2011Publication date: July 19, 2012Applicants: AAT BIOQUEST, INC., BECTON, DICKINSON AND COMPANYInventors: Zhenjun Diwu, Qinglin Meng, Jinfang Liao, Haitao Guo, Timothy Dubrovsky, Barnaby Abrams
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Publication number: 20120088770Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a chemical library relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.Type: ApplicationFiled: May 7, 2010Publication date: April 12, 2012Applicant: Prism BioLab CorporationInventors: Takenao Odagami, Yiji Kogami, Hiroyuki Kouji
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Patent number: 8071586Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y1, Y2, Y3, R3, R4, R5, R6, R7, R8, R9, R10, m, n and p are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.Type: GrantFiled: July 8, 2009Date of Patent: December 6, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
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Publication number: 20100189762Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, including various ocular diseases, and parasitic infections. Representative triphenyl methane analogs include triphenyl methane analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.Type: ApplicationFiled: December 21, 2009Publication date: July 29, 2010Applicant: EMORY UNIVERSITYInventor: Jack L. Arbiser
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Patent number: 7759354Abstract: The present application provides compounds of the Formula: and stereoisomers, tautomers, or pharmaceutically acceptable salts and solvates thereof, wherein U, W, R, R1, R2, R3 and R4 in each formula (when present) are as defined in the specification, and pharmaceutical compositions comprising such compounds. Also disclosed are methods of using such compounds and compositions to inhibit aspartyl protease, and to treat a variety of disease and indications including (but not limited) to cardiovascular disease and cognitive and neurodegenerative disease. The compounds of the present invention are disclosed for use alone or in combination with one or more additional active ingredients such as cholinesterase inhibitors and a muscarinic m1 agonist and/or m2 antagonists.Type: GrantFiled: June 12, 2006Date of Patent: July 20, 2010Assignee: Schering CorporationInventors: Zhaoning Zhu, Brian McKittrick, Andrew Stamford, Ying Huang, Elizabeth M. Smith
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Patent number: 7727982Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compound and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: July 17, 2006Date of Patent: June 1, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Publication number: 20100016282Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y1, Y2, Y3, R3, R4, R5, R6, R7, R8, R9, R10, m, n and p are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.Type: ApplicationFiled: July 8, 2009Publication date: January 21, 2010Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
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Publication number: 20090258856Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: June 23, 2009Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Norbert HAUEL, Elke LANGKOPF, Frank HIMMELSBACH, Iris KAUFFMANN-HEFNER, Mohammad TADAYYON, Michael MARK
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Publication number: 20090194407Abstract: A method and system for disposal of furfural wastewater, wherein raw crop material is transported into a hydrolysis reactor after crushed and mixed with acid to be hydrolyzed to form raw furfural liquid, and then said raw furfural liquid is transported into a distillation column to be distilled, during which furfural wastewater is discharged from said distillation column. Firstly said furfural wastewater is transported into a wastewater evaporation system to be heated it into wastewater vapor which is then transported back into said hydrolysis reactor to form recycle of said furfural wastewater. Wastewater vapor residues generated therein can be utilized directly to combust in boiler, mix with acid, or prepare end product acetate. The system for disposal of furfural wastewater comprises at least a wastewater evaporation system connecting with a heat resource which is one of steam, electricity, coal, oil, gas, plant straws or wastewater vapor residues.Type: ApplicationFiled: November 8, 2006Publication date: August 6, 2009Applicant: JINAN SHENGQUAN GROUP SHAREHOLDINGS CO., LTD.Inventors: Yilin Tang, Chengzhen Jiang, Shaofeng Gao, Dongsheng Lv, Zujiang Shen, Xuanwei Suo
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Patent number: 7566707Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: June 10, 2004Date of Patent: July 28, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Norbert Hauel, Elke Langkopf, Frank Himmelsbach, Iris Kauffmann-Hefner, Mohammad Tadayyon, Michael Mark
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Patent number: 7560451Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W, R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.Type: GrantFiled: October 30, 2006Date of Patent: July 14, 2009Assignee: Schering CorporationInventors: Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
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Publication number: 20090093457Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: December 10, 2008Publication date: April 9, 2009Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
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Patent number: 7125888Abstract: The present invention relates to imidazopyridine compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: GrantFiled: April 28, 2003Date of Patent: October 24, 2006Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Mark E. Fraley, Zhicai Wu
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Patent number: 7015321Abstract: A practical and high-yielding method for the efficient, one-step synthesis of diverse classes of N,N?-differentiated sulfamides employs a wide range of amino alcohols and simple amines using Burgess-type reagents. This methodology extends the application and availability of sulfamides within the fields of chemical biology, medicinal chemistry, asymmetric synthesis, and supramolecular chemistry.Type: GrantFiled: October 14, 2003Date of Patent: March 21, 2006Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Deborah Longbottom, Scott A. Snyder, Xianhai Huang
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Patent number: 6949538Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: July 17, 2003Date of Patent: September 27, 2005Assignees: Cytokinetics, Inc., Smithkline Beecham CorporationInventors: Andrew McDonald, Gustave Bergnes, David J. Morgans, Jr., Dashyant Dhanak, Steven David Knight
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Patent number: 6921759Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: October 10, 2001Date of Patent: July 26, 2005Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, Robert P. Gomez, Steven D. Young, Melissa Egbertson, John S. Wai, Linghang Zhuang, Mark Embrey, Jeffrey Y. Melamed, H. Marie Langford, James P. Guare, Thorsten E. Fisher, Samson M. Jolly, Michelle S. Kuo, Debra S. Perlow, Jennifer J. Bennett, Timothy W. Funk
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Patent number: 6900222Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is aType: GrantFiled: May 23, 2000Date of Patent: May 31, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 6867298Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate.Type: GrantFiled: May 8, 2003Date of Patent: March 15, 2005Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Artis Klapars, Jon C. Antilla, Gabriel E. Job, Martina Wolter, Fuk Y. Kwong, Gero Nordmann, Edward J. Hennessy
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Publication number: 20040186091Abstract: A compound of formula (I), 1Type: ApplicationFiled: February 18, 2004Publication date: September 23, 2004Applicant: Pfizer IncInventors: Justin Stephen Bryans, Patrick Stephen Johnson, Thomas Ryckmans, Alan Stobie
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Patent number: 6686350Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.Type: GrantFiled: January 25, 1999Date of Patent: February 3, 2004Assignee: Biogen, Inc.Inventors: Zhongli Zheng, Carol L. Ensinger, Steven P. Adams
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Patent number: 6624157Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof wherein: r, s and t are 0 or 1; m=0, 1, 2; p is 0, 1 or 2; X is selected from the group consisting of oxygen, hydrogen or R1, R2, R3; Y is selected from the group consisting of CHR9, SO2, CO, CO2, O, NR10, SO2NR11 and CONR12; R6, R7, R9, R10, R11, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, and R28 are selected from the group consisting of hydrogen, lower alkyl or substituted alkyl; R4, R5 are selected from the group consisting of hydrogen, halo, nitro, cyano and U-R13; R12 is selected from the group consisting of hydrogen, lower alkyl, aryl, substituted alkyl or aryl; U is selected from the group consisting of sulfur, oxygen, NR14, CO, SO, SO2, CO2, NR15CO2, NR16CONR17, NR19SO2, NR19SO2NR20, SO2NR2Type: GrantFiled: January 26, 2001Date of Patent: September 23, 2003Assignee: Bristol-Myers Squibb CompanyInventor: Charles Z. Ding
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Patent number: 6503898Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: wherein R22 and R23 are allyl.Type: GrantFiled: July 10, 1998Date of Patent: January 7, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Yuk-Sun Lam, Prabhakar Kondaji Jadhav, Charles Joseph Eyermann, Carl Nicholas Hodge, George Vincent De Lucca, James David Rodgers
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Patent number: 6416922Abstract: The present invention related to an azomethine dye precursor represented by the following general formula (1) and the image-forming material and image-forming method using the azomethine dye precursor: wherein Ar represents an aryl group or a heterocyclic group which may each have a substituent; X represents a bivalent group linking a carbon atom and a nitrogen atom; and Cp represent a coupler residue which may or may not form a ring.Type: GrantFiled: January 29, 2001Date of Patent: July 9, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Hiroshi Sato, Masatoshi Yumoto, Yoshimitsu Arai, Hirotaka Matsumoto
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Patent number: 6156746Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula ##STR1## and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof.The compounds of formula I are useful in the treatment of a variety of cancers. In addition, the formula I compounds may also be useful in the treatment of diseases other than cancer.Type: GrantFiled: July 15, 1999Date of Patent: December 5, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Katerina Leftheris, John T. Hunt, Charles Z. Ding
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Patent number: 6100252Type: GrantFiled: December 8, 1998Date of Patent: August 8, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Yoshiyuki Inada
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Patent number: 5932570Abstract: The present invention relates to compounds of formulae I and II: ##STR1## or pharmaceutically acceptable salt forms or prodrugs thereof, which are useful as inhibitors of HIV protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: November 7, 1997Date of Patent: August 3, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: James David Rodgers, Robert Frank Kaltenbach, III
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Patent number: 5753642Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.Type: GrantFiled: June 6, 1995Date of Patent: May 19, 1998Assignee: Rohm and Haas CompanyInventors: Enrique Luis Michelotti, Anne Ritchie Egan, Ronald Ross, Jr., Willie Joe Wilson
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Patent number: 5670497Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating vital infection.Type: GrantFiled: January 11, 1996Date of Patent: September 23, 1997Assignee: Ciba-Geigy CorporationInventors: Guido Bold, Shripad S. Bhagwat, Alexander Fassler, Marc Lang
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Patent number: 5646276Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents.Type: GrantFiled: June 19, 1996Date of Patent: July 8, 1997Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl
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Patent number: 5610294Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: ##STR1## wherein R.sup.22 and R.sup.23 are allyl.Type: GrantFiled: February 16, 1994Date of Patent: March 11, 1997Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Patrick Y. Lam, Prabhakar K. Jadhav, Charles J. Eyermann, Carl N. Hodge, George V. De Lucca, James D. Rodgers
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Patent number: 5523469Abstract: This invention relates to levogyral isomers of alkylammonium (amino-3 phenyl)-1 ethanesulphonate derivatives of formula (I) in which R+ denotes a tetraalkylammonium or trialkylphenylalkylammonium residue. The invention also concerns the preparation and use of said derivatives.Type: GrantFiled: March 10, 1995Date of Patent: June 4, 1996Assignee: Rhone-Poulenc Rorer S.A.Inventor: Claude Guyon
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Patent number: 5496943Abstract: Disclosed is a novel heterocyclic compound selected from the group consisting of the compounds [IV] to [VII], [IX] and [X]. The heterocyclic compound is useful for reactive materials in chemical industry. A process for producing the heterocyclic compound is also disclosed.Type: GrantFiled: March 13, 1992Date of Patent: March 5, 1996Assignee: Nippon Paint Co., Ltd.Inventors: Otohiko Tsuge, Taizo Hatta, Satoshi Urano, Noriyuki Tsuboniwa, Ryuzo Mizuguchi
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Patent number: 5340807Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6 alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 --O, CH.sub.2 --(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.Type: GrantFiled: December 11, 1992Date of Patent: August 23, 1994Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
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Patent number: 5238936Abstract: The compounds are trisubstituted triazines and pyrimidines useful for the suppressing the resistance of tumour cells to anti-cancer agents and for suppressing the resistance of parasites to anti-parasitic agents.A compound disclosed is 2,4-diallylamino-6-{4-[(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl) methylamino]piperidin-1-yl}-1,3,5-triazine.Type: GrantFiled: March 6, 1992Date of Patent: August 24, 1993Assignee: Adir et CompagnieInventors: Gilbert Regnier, Alain Dhainaut, Ghanem Atassi, Alain Pierre, Stephane Leonce
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Patent number: 5149823Abstract: A novel class of sulfonamoyl-substituted 1,6-diaza[4.4]spirodilactams, having a sulfonamoyl substituent on the hydrocarbyl group attached to each spiro ring nitrogen atom, is useful for the preparation of polymers, including polyamides and as latent curing agents for epoxy resins.Type: GrantFiled: August 9, 1990Date of Patent: September 22, 1992Assignee: Shell Oil CompanyInventor: Pen-Chung Wang
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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Patent number: 4939251Abstract: Novel 1-azaspiro[4.4] lactams are produced by reaction of at least one hydroxy-containing primary amino compound with a 4-ketodiacid compound or a 1,6-dioxaspiro[4.4]lactone. Molar excesses of amion compound result in production of spirodilactams, while limited molar quantities of amino compound results in production of a spirolactam-lactone which reacts further with hydroxy-containing primary amino compound or with hydroxy-free primary amino compound to produce a spirodilactam. Certain of the spirolactams are useful as precursors for glycidyloxy derivatives which react with epoxy curing agents to form insoluble thermoset resins while others are useful as curing agents and yet others are converted to glycidyloxy derivatives useful as reactive diluents in epoxy resin applications.Type: GrantFiled: September 16, 1988Date of Patent: July 3, 1990Assignee: Shell Oil CompanyInventor: Pen C. Wang
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Patent number: 4895942Abstract: Novel epoxyalkoxy-containing [4.4] spirodilactams having ring nitrogen atoms in the 1- and the 6- ring positions and having a substituent on each ring nitrogen atom, at least one of which substituents contains an epoxyalkyl moiety. Such epoxy compounds are produced by reaction of a 1-halo-2,3-epoxyalkane and the corresponding hydroxy-containing spirodilactam followed by treatment with strong base.Type: GrantFiled: September 16, 1988Date of Patent: January 23, 1990Assignee: Shell Oil CompanyInventor: Pen C. Wang
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Patent number: 4748160Abstract: There are described compounds of formula I,ZCHRCON(--N.dbd.CR.sub.4 R.sub.5)CHR.sub.6 (CH.sub.2).sub.n COY Iwhere the substituents are defined in the disclosure.There are also described methods for making the compounds, formulations containing them and their use, e.g. as antihypertensives.Type: GrantFiled: November 14, 1985Date of Patent: May 31, 1988Assignee: Fisons plcInventors: Colin Bennion, David P. Marriott, Anthony R. Cook, David H. Robinson
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Patent number: 4709027Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or lower alkyl, or R.sup.1 and R.sup.2 taken together represent ##STR2## A is O or NR.sup.3 ; B is --(CH.sub.2).sub.n --, ##STR3## R.sup.3 is hydrogen or lower alkyl; R.sup.4 is hydrogen, lower alkyl, aryl of 6-12 carbon atoms or halo;R.sup.5 is unsubstituted or substituted phenyl, 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl or 3-pyridazinyl, where the substituents are selected from the group lower alkyl, lower alkoxy, halo, cyano, nitro and trifluoromethyl;Z is --(CH.sub.2).sub.n -- or vinylene;X is lower alkylene, vinylene or O;m is 2-5;n is 1-3;o is 1-5;and the pharmaceutically acceptable salts thereof and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.Type: GrantFiled: June 25, 1986Date of Patent: November 24, 1987Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Guy A. Schiehser
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Patent number: 4680052Abstract: The invention relates to new benzodisultams of the general formula (I) ##STR1## in which R.sup.1 represents an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aralkyl and aryl,R.sup.2 represents hydrogen or an optionally substituted radical from the series comprising alkyl, alkemyl, alkinyl and aralkyl, andR.sup.3 represents an optionally substituted and/or optionally fused six-membered aromatic heterocyclic radical which contains at least one nitrogen atom,a process for their preparation and their use as herbicides.Type: GrantFiled: August 23, 1985Date of Patent: July 14, 1987Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Diehr, Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Theodor Pfister, Uwe Priesnitz, Hans-Jochem Riebel, Wolfgang Roy, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: RE37781Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: wherein R22 and R23 are allyl.Type: GrantFiled: March 10, 1999Date of Patent: July 2, 2002Assignee: DuPont Pharmaceuticals CompanyInventors: Patrick Y. Lam, Prabhakar K. Jadhav, Charles J. Eyermann, Carl N. Hodge, George V. De Lucca, James D. Rodgers