The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 549/446)
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Patent number: 10584108Abstract: The invention provides compounds that are useful for treating or preventing cancer.Type: GrantFiled: May 9, 2016Date of Patent: March 10, 2020Assignee: Kuality Herbceutics LLCInventor: Chengguo Xing
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Patent number: 9530658Abstract: A method for processing a substrate in a process chamber is provided. A plurality of cycles is provided to process the substrate, wherein each cycle comprises the steps of providing a flow of a first process gas into the process chamber, stopping the flow of the first process gas into the process chamber, providing a flow of a first transition gas into the process chamber, wherein the first transition gas neutralizes a component of the first process gas, stopping the flow of the first transition gas into the process chamber, providing a flow of a second process gas into the process chamber, stopping the second process gas into the process chamber, and maintaining a continuous plasma during the cycle.Type: GrantFiled: August 12, 2015Date of Patent: December 27, 2016Assignee: Lam Research CorporationInventors: Wonchul Lee, Qian Fu
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Patent number: 8633242Abstract: The present invention relates to benzylidene indanones of general formula 1. The compounds exhibited tubulin polymerisation inhibition. A series of compounds 2-benzylidene 3-(3,4,5-trimethoxyphenyl) indanones having general formula 1 were synthesized from gallic acid through a chemical process. 2-(3,4-Methylenedioxybenzylidine), 3-(3,4,5-trimethoxyphenyl), 4,5,6-trimethoxyindanone (8), a representative compound of this series possessing the molecular formula C29H28O9, was synthesized from gallic acid and exhibits potent anticancer activity. Compound 8 was evaluated for acute oral activity in Swiss albino mice and found to be safe up to 300 mg/kg body weight. The anticancer activity of the compounds has been determined, in order to obtain new potent and cost effective molecules using an in vitro cytotoxicity assay.Type: GrantFiled: September 20, 2012Date of Patent: January 21, 2014Assignee: Council of Scientific and Industrial ResearchInventors: Arvind Singh Negi, Ayyampudur Palanisamy Prakasham, Ajit Kumar Saxena, Suaib Luqman, Debabrata Chanda, Tandeep Kaur, Atul Gupta
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Publication number: 20130217895Abstract: The present invention provides a catalyst used for manufacturing an optically active carbonyl compound by selective asymmetric hydrogenation of an ?, ?-unsaturated carbonyl compound, which is insoluble in a reaction mixture, and a method for manufacturing the corresponding optically active carbonyl compound. Particularly, the invention provides a catalyst for obtaining an optically active citronellal useful as a flavor or fragrance, by selective asymmetric hydrogenation of citral, geranial or neral. The invention relates to a catalyst for asymmetric hydrogenation of an ?, ?-unsaturated carbonyl compound, which comprises: a powder of at least one metal selected from metals belonging to Group 8 to Group 10 of the Periodic Table, or a metal-supported substance in which the at least one metal is supported on a support; an optically active cyclic nitrogen-containing compound; and an acid, and also relates to a method for manufacturing an optically active carbonyl compound using the same.Type: ApplicationFiled: November 29, 2011Publication date: August 22, 2013Applicant: TAKASAGO INTERNATIONAL CORPORATIONInventors: Shinya Yamada, Hironori Maeda, Yoji Hori
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Publication number: 20130165507Abstract: The invention relates to novel guanidine derivatives in the cinnamic series of general formula (I): The invention also relates to the process for preparing said guanidine derivatives and also to synthetic intermediates. Finally, the invention relates to the use of the guanidine derivatives for the preparation of compositions with anti-glycation properties, especially in cosmetology.Type: ApplicationFiled: September 6, 2011Publication date: June 27, 2013Applicant: PRODUITS CHIMIQUES AUXILIAIRES ET DE SYNTHESEInventors: Sylvain Rault, Jean Charles Lancelot, Peggy Suzanne, Anne-Sophie Voisin-Chiret, Regis Pecquet, Jean-Christophe Joseph
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Patent number: 8450508Abstract: The present invention relates to [1] a method for keeping a quality of 2-methyl-3-(3,4-methylenedioxyphenyl)propanal useful as a perfume, which comprises incorporating from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene in the 2-methyl-3-(3,4-methylenedioxyphenyl)propanal; [2] a process for producing 2-methyl-3-(3,4-methylenedioxyphenyl)propanal having a content range from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene; and [3]2-methyl-3-(3,4-methylenedioxyphenylpropanal having a content range from 50 to 3000 ppm of of 1-acetyl-3,4-methylenedioxybenzene.Type: GrantFiled: October 18, 2012Date of Patent: May 28, 2013Assignee: Ube Industries, Ltd.Inventors: Takashi Doi, Yoshihiro Yoshida, Eiji Sajiki, Satoru Fujitsu
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Publication number: 20130079396Abstract: The present invention relates to benzylidene indanones of general formula 1. The compounds exhibited tubulin polymerisation inhibition. A series of compounds 2-benzylidene 3-(3,4,5-trimethoxyphenyl) indanones having general formulae 1 were synthesized from gallic acid through a chemical process. 2-(3,4-Methylenedioxybenzylidine), 3-(3,4,5-trimethoxyphenyl), 4,5,6-trimethoxyindanone (8), a representative compound of this series possessing the molecular formulae C29H28O9, was synthesized from gallic acid and exhibits potent anticancer activity. Compound 8 was evaluated for acute oral activity in Swiss albino mice and found to be safe up to 300 mg/kg body weight. The anticancer activity of the compounds has been determined, in order to obtain new potent and cost effective molecules using an in vitro cytotoxicity assay.Type: ApplicationFiled: September 20, 2012Publication date: March 28, 2013Applicant: Council of Scientific and Industrial ResearchInventor: Council of Scientific and Industrial Research
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Publication number: 20130046101Abstract: The present invention relates to [1] a method for keeping a quality of 2-methyl-3-(3,4-methylenedioxyphenyl)propanal useful as a perfume, which comprises incorporating from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene in the 2-methyl-3-(3,4-methylenedioxyphenyl)propanal; [2] a process for producing 2-methyl-3-(3,4-methylenedioxyphenyl)propanal having a content range from to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene; and [3]2-methyl-3-(3,4-methylenedioxyphenylpropanal having a content range from 50 to 3000 ppm of of 1-acetyl-3,4-methylenedioxybenzene.Type: ApplicationFiled: October 18, 2012Publication date: February 21, 2013Inventors: Takashi DOI, Yoshihiro Yoshida, Eiji Sajiki, Satoru Fujitsu
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Patent number: 8344166Abstract: The present invention relates to [1] a method for keeping a quality of 2-methyl-3-(3,4-methylenedioxyphenyl)propanal useful as a perfume, which comprises incorporating from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene in the 2-methyl-3-(3,4-methylenedioxyphenyl)propanal; [2] a process for producing 2-methyl-3-(3,4-methylenedioxyphenyl)propanal having a content range from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene; and [3] 2-methyl-3-(3,4-methylenedioxyphenyl)propanal having a content range from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene.Type: GrantFiled: August 22, 2011Date of Patent: January 1, 2013Assignee: Ube Industries, Ltd.Inventors: Takashi Doi, Yoshihiro Yoshida, Eiji Sajiki, Satoru Fujitsu
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Publication number: 20120277252Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alkyl groups, and optionally having hydroxyl and/or alkoxyl groups substituents.Type: ApplicationFiled: July 6, 2012Publication date: November 1, 2012Inventors: Helen E. Blackwell, Matthew D. Bowman, Jennifer C. O'Neill, Joseph R. Stringer
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Patent number: 8168809Abstract: Disclosed are: (1) a method for producing 2-methyl-3-(3,4-methylenedioxyphenyl)propanal, which comprises the step of providing a reaction mixture containing 1-acetoxy-2-methyl-3-(3,4-methylenedioxyphenyl)-1-propene by a process for reacting 1,2-methylenedioxybenzene with 2-methyl-3,3-diacetoxypropene or a process for reacting 1,2-methylenedioxybenzene, methacrolein and acetic anhydride with one another; subjecting the reaction mixture to hydrolysis or transesterification with an alcohol to provide a reaction mixture containing 2-methyl-3-(3,4-methylenedioxyphenyl)propanal; and purifying by distilling the reaction mixture, wherein a high boiling point compound contained in the reaction mixture is removed by a specific procedure; and (2) 2-methyl-3-(3,4-methylenedioxyphenyl)-propanal produced by the method, which has an acetic acid content of a less than 40 ppm, is useful as a perfume, and has a high purity.Type: GrantFiled: February 14, 2008Date of Patent: May 1, 2012Assignee: Ube Industries, Ltd.Inventors: Takashi Doi, Yoshihiro Yoshida, Eiji Sajiki, Satoru Fujitsu
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Patent number: 8088820Abstract: This invention provides a method for treating or preventing malaria in a subject. The method includes administering to the subject an effective amount of a substituted tetracycline compound, such that malaria is treated or prevented. In one aspect, the invention relates to pharmaceutical compositions which include an effective amount of a tetracycline compound to treat malaria in a subject and a pharmaceutically acceptable carrier. The substituted tetracycline compounds of the invention can be used to in combination with one or more anti-malarial compounds or can be used to treat or prevent malaria which is resistant to one or more other anti-malarial compounds.Type: GrantFiled: October 24, 2003Date of Patent: January 3, 2012Assignee: Paratek Pharmaceuticals, Inc.Inventors: Michael Draper, Mark L. Nelson
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Patent number: 8039649Abstract: The present invention relates to [1] a method for keeping a quality of 2-methyl-3-(3,4-methylenedioxyphenyl)propanal useful as a perfume, which comprises incorporating from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene in the 2-methyl-3-(3,4-methylenedioxyphenyl)propanal; [2] a process for producing 2-methyl-3-(3,4-methylenedioxyphenyl)propanal having a content range from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene; and [3] 2-methyl-3-(3,4-methylenedioxyphenyl)propanal having a content range from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene.Type: GrantFiled: March 6, 2008Date of Patent: October 18, 2011Assignee: UBE Industries, Ltd.Inventors: Takashi Doi, Yoshihiro Yoshida, Eiji Sajiki, Satoru Fujitsu
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Publication number: 20110190325Abstract: Embodiments of the present invention provide compounds (such as Formula (I) compounds, Formula (II) compounds, and various embodiments thereof). Compositions comprising those compounds are also provided. Methods for their preparation are included. Also, uses of the compounds are included, such as administering and treating diseases (e.g., cancer and infections).Type: ApplicationFiled: August 14, 2009Publication date: August 4, 2011Inventors: Gerald B. Hammond, Jose C. Aponte, Robert H. Gilman, Michel Henri Auguste Sauvain, Abraham Caisberg
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Patent number: 7893282Abstract: 7-substituted fused ring tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted fused ring tetracycline compounds are described.Type: GrantFiled: October 10, 2007Date of Patent: February 22, 2011Assignee: Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Laura Honeyman
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Publication number: 20100316631Abstract: The present disclosure describes the design and synthesis of a novel class of water soluble curcumin-based compounds. These water soluble curcumin-based compounds are shown to provide superior cell killing activity and exhibit increased and cell internalization solubility in aqueous solutions as compared to the free (unconjugated) curcumin. The present disclosure provides compositions for the treatment or prevention of a variety of disease states or conditions, such as but not limited to, cancer, other cell hyperproliferative disorders and chronic inflammatory conditions, said compositions comprising a water soluble curcumin-based compound.Type: ApplicationFiled: October 19, 2007Publication date: December 16, 2010Applicant: THE UAB RESEARCH FOUNDATIONInventor: Ahmad Safavy
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Patent number: 7728154Abstract: 1-aryl-3,4-dihydro-1H-naphthalene-2-one is prepared by isomerizing an epoxy compound represented by the following general formula, wherein a is an integer of 0 to 5, b is an integer of 0 to 4, and R1 to R6 are hydrogen atoms or substituents such as alkyl groups, in an organic solvent in the presence of magnesium sulfate. This process makes it possible to prepare the 1-aryl-3,4-dihydro-1H-naphthalene-2-one safely and in a high yield without using highly explosive compounds such as lithium perchlorate.Type: GrantFiled: February 6, 2008Date of Patent: June 1, 2010Assignee: Tokuyama CorporationInventors: Junji Takenaka, Nobumasa Kuwashima, Toshiaki Takahashi
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Publication number: 20100029541Abstract: The present invention relates to [1] a method for keeping a quality of 2-methyl-3-(3,4-methylenedioxyphenyl)propanal useful as a perfume, which comprises incorporating from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene in the 2-methyl-3-(3,4-methylenedioxyphenyl)propanal; [2] a process for producing 2-methyl-3-(3,4-methylenedioxyphenyl)propanal having a content range from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene; and [3] 2-methyl-3-(3,4-methylenedioxyphenyl)propanal having a content range from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene.Type: ApplicationFiled: March 6, 2008Publication date: February 4, 2010Applicant: UBE Industries, Ltd.Inventors: Takashi Doi, Yoshihiro Yoshida, Eiji Sajiki, Satoru Fujitsu
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Publication number: 20080200697Abstract: 1-aryl-3,4-dihydro-1H-naphthalene-2-one is prepared by isomerizing an epoxy compound represented by the following general formula, wherein a is an integer of 0 to 5, b is an integer of 0 to 4, and R1 to R6 are hydrogen atoms or substituents such as alkyl groups, in an organic solvent in the presence of magnesium sulfate. This process makes it possible to prepare the 1-aryl-3,4-dihydro-1H-naphthalene-2-one safely and in a high yield without using highly explosive compounds such as lithium perchlorate.Type: ApplicationFiled: February 6, 2008Publication date: August 21, 2008Applicant: Tokuyama CorporationInventors: Junji Takenaka, Nobumasa Kuwashima, Toshiaki Takahashi
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Patent number: 7109327Abstract: The invention relates to a method for the synthesis of galanthamifle, the derivatives and analogues thereof of formula (1) where R1=a hydrogen atom.Type: GrantFiled: June 14, 2002Date of Patent: September 19, 2006Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Claude Thal, Catherine Guillou, Jean-Luc Beunard, Emmanuel Gras, Pierre Potier
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Patent number: 6867310Abstract: The present invention provides transition-metal-catalyst-based methods for the arylation and vinylation of activated methyl, methylene, and methine carbons with aryl halides, vinyl halides, and the like. The methods of the invention provide several improvements over existing methods, including the ability to synthesize efficiently and under mild conditions ?-aryl and ?-vinyl products from a wide range of starting materials, including ketones, esters, hydrazones, and imines. Furthermore, the methods of the invention may be used in an asymmetric sense, i.e. to produce enantiomerically-enriched chiral ?-aryl and ?-vinyl products.Type: GrantFiled: January 27, 1999Date of Patent: March 15, 2005Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, John P. Wolfe, Jens Ahman, Malisa Troutman, Michael Palucki, Ken Kamikawa, Andre Chieffi
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Patent number: 6864282Abstract: 9,11-Cycloendoperoxide derivatives of biologically active prostaglandin analogs, and particularly of the ocular hypotensive drugs Bimatoprost, Latanaprost, Unoprostone, Travoprost and prostaglandin H2 1-ethanolamide or of structurally closely related analogs, are pro-drugs which hydrolyze under physiological conditions to provide prostaglandin analogues that are capable of providing sustained ocular and other in vivo concentrations of the respective drugs. The compounds of the invention have the formula shown below where the variables have the meaning defined in the specification.Type: GrantFiled: August 5, 2002Date of Patent: March 8, 2005Assignee: Allergan, Inc.Inventors: Kah-Hiing John Ling, Wu Yang, Jinsong Ni, Haiqing Yuan, Diane D. S. Tang-Liu
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Patent number: 6686482Abstract: The present invention is to provide a process for producing piperonal which comprises continuous three steps of: (A) an addition reaction step wherein 1,2-methylenedioxybenzene and glyoxylic acid are reacted to form 3,4-methylenedioxymandelic acid in the presence of a strong acid, (B) an extraction step wherein an organic solvent is then added to a reaction mixture and the mixture is neutralized with a base to extract 3,4-methylenedioxymandelic acid in an organic solvent layer, and separating the organic solvent layer and an aqueous layer, and (C) an oxidation reaction step wherein the aqueous layer is removed and the organic solvent layer is concentrated, and then, nitric acid is added to a concentrate, and the 3,4-methylenedioxymandelic acid and nitric acid are reacted to form piperonal.Type: GrantFiled: July 30, 2002Date of Patent: February 3, 2004Assignee: Ube Industries, Ltd.Inventors: Katsumasa Harada, Masashi Shirai, Koji Shiba, Toshio Furuya
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Patent number: 6677456Abstract: This invention is to provide a novel taxol derivative useful as an antitumor compound having respective substituent groups, represented by the following formula (I) which can be orally administeredType: GrantFiled: March 6, 2002Date of Patent: January 13, 2004Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Tsunehiko Soga, Kouichi Uoto, Yasuyuki Takeda
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Patent number: 6642270Abstract: 7-substituted fused ring tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted fused ring tetracycline compounds are described.Type: GrantFiled: May 10, 2001Date of Patent: November 4, 2003Assignee: Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Laura McIntyre
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Publication number: 20030158427Abstract: A process for preparing compounds of the formula I 1Type: ApplicationFiled: January 6, 2003Publication date: August 21, 2003Inventors: Hansgeorg Ernst, Klaus Henrich
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Publication number: 20020133009Abstract: The present invention relates to a method for opening potassium channels in mammalian cells by administering to a mammal effective amounts of potassium channel-opening keto compounds as described herein.Type: ApplicationFiled: March 4, 2002Publication date: September 19, 2002Inventors: George N. Lambrou, Anna Ottlecz, Christine Percicot, Michael Wiederholt
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Patent number: 6444615Abstract: This invention relates to 1-substituted-phenyl-3-substituted-2-thioxo-4,5-imidazolidinediones and 2,4,5-imidazolidinetriones which have activity as herbicides, to compositions which contain these compounds and to methods of use of these compounds. In particular, the present invention pertains to 2-thioxo-4,5-imidazolidinediones or 2,4,5-imidazolidinetriones wherein a 2,4,5,6-tetrasubstituted phenyl ring is linked to the heterocyclic ring.Type: GrantFiled: April 18, 2000Date of Patent: September 3, 2002Assignee: Dow AgroSciences LLCInventors: Bin Li, Ying Man, Zongjian Zhang, Adam Chi-Tung Hsu
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Publication number: 20020016361Abstract: The present invention relates to beta-amino acid nitrile derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are cysteine protease inhibitors useful for the treatment of diseases associated with cysteine proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.Type: ApplicationFiled: June 1, 2001Publication date: February 7, 2002Inventors: Tobias Gabriel, Michael Pech, Rosa Maria Rodriguez Sarmiento
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Publication number: 20020002177Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: ApplicationFiled: July 10, 2001Publication date: January 3, 2002Applicant: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 6310080Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: December 1, 1999Date of Patent: October 30, 2001Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 6077849Abstract: Compounds of formula I: ##STR1## as well as tautomers, pharmaceutically acceptable salts, hydrates, prodrugs and reduced forms are disclosed. The compounds are useful for the treatment and prevention of diabetes mellitus, and in particular, for the treatment or prevention of hyperglycemia in diabetic patients.Type: GrantFiled: March 29, 1999Date of Patent: June 20, 2000Assignee: Merck & Co., Inc.Inventors: Kun Liu, Harold B. Wood, Anthony B. Jones, Bei Zhang
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Patent number: 5814657Abstract: Compounds of the formula ##STR1## wherein the variables are defined as in the specification, are capable of lowering introaocular pressure in the eye of a mammal.Type: GrantFiled: November 21, 1997Date of Patent: September 29, 1998Assignee: AllerganInventors: Robert M. Burk, David F. Woodward
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Patent number: 5500407Abstract: Triazolo pyrimidines of the formula ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 haloalkyl; and R.sub.2 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkylthio, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkylthio, halogen, amino, C.sub.1 -C.sub.4 alkylamino or C.sub.1 -C.sub.4 dialkylamino, have pre- and postemergence herbicidal properties. Their preparation use thereof as herbicides are described.Type: GrantFiled: November 21, 1994Date of Patent: March 19, 1996Assignee: Ciba-Geigy CorporationInventor: Hermann Rempfler
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Patent number: 5493032Abstract: The reaction of 2,2-difluorobenzo-1,3-dioxole with (a) an alkali metal or an alkali metal compound and then (b) a compound R.sup.1 -Z.sup.1 in which Z.sup.Type: GrantFiled: March 6, 1995Date of Patent: February 20, 1996Assignee: Ciba-Geigy CorporationInventors: Peter Ackermann, Hans-Ruedi Kanel, Bruno Schaub
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Patent number: 5480908Abstract: The invention is antiobesity/antidiabetes beta-3 agonists of the formula: ##STR1## wherein Ar, X, R.sub.2, R.sub.3, Y and n are as defined in the specification.Type: GrantFiled: December 13, 1993Date of Patent: January 2, 1996Assignee: American Cyanamid CompanyInventors: Joseph W. Epstein, Gary H. Birnberg, Minu D. Dutia, Thomas H. Claus, Elwood E. Largis
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Patent number: 5420273Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.6 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.Type: GrantFiled: December 23, 1993Date of Patent: May 30, 1995Assignee: Hoffman-La Roche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
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Patent number: 5369127Abstract: Compounds of the formula ##STR1## where W is (CH.sub.2).sub.n where n is 1 or 2, or n is O and W represents lower alkyl groups attached to each oxygen;m is an integer between 1 and 8;R.sub.1 is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.4, CONR.sub.5 R.sub.6, CONR.sub.5 SO.sub.2 R.sub.7, CH.sub.2 OH, CH.sub.2 OR.sub.7, CH.sub.2 O--COR.sub.7, CH.sub.2 O--CONR.sub.5, R.sub.7, CH.sub.2 OCOOR.sub.7, CH.sub.2 NH.sub.2, CH.sub.2 NR.sub.5 R.sub.6, CH.sub.2 NR.sub.5 COR.sub.7, CHO, CH(OR.sub.8).sub.2, CHOR.sub.9 O, --COR.sub.10, CR.sub.10 (OR.sub.8).sub.2, or CR.sub.10 OR.sub.9 O, where R.sub.4 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.4 is phenyl or lower alkylphenyl, R.sub.5 and R.sub.6 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.7 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.8 is lower alkyl, and R.sub.Type: GrantFiled: April 21, 1993Date of Patent: November 29, 1994Assignee: Allergan, Inc.Inventors: Robert M. Burk, David F. Woodward
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Patent number: 5352678Abstract: Certain piperazinyl- and piperidinyl-substituted cyclohexanes have anti-ischemic properties.Type: GrantFiled: June 25, 1993Date of Patent: October 4, 1994Assignee: Bristol-Myers Squibb Co.Inventors: Ronald J. Mattson, John D. Catt
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Patent number: 5320833Abstract: Arylpolyenecarboxylic acids and their derivatives of the formula I ##STR1## where Ar is phenyl, biphenylyl or naphthyl, each of which can be substituted by one to three C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, hydroxyl or phenoxy groups, or amino groups which can be mono- or di-substituted by C.sub.1 -C.sub.4 -alkyl groups, or one methylenedioxy group, it being possible for the substituents to be identical or different,R.sup.1 is hydrogen, an alkali metal or ammonium cation, C.sub.1 -C.sub.20 -alkyl or C.sub.2 -C.sub.20 -alkenyl,R.sup.2 is C.sub.1 -C.sub.8 -alkyl,R.sup.3 to R.sup.7 are each hydrogen or C.sub.1 -C.sub.4 -alkyl, andn is 0 or 1are used as sunscreen agents in cosmetic preparations.Type: GrantFiled: September 23, 1991Date of Patent: June 14, 1994Assignee: BASF AktiengesellschaftInventors: Gabriele Deckers, Rainer Becker, Bernd Wenderoth, Norbert Goetz, Karin Sperling-Vietmeier
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Patent number: 5270301Abstract: The present invention relates to certain fluoro-amide derivatives, as described herein, which are human leukocyte elastase (HLE) inhibitors making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated, including treatment of tissue degenerative diseases such as pulmonary emphysema. The invention also includes intermediates useful in the synthesis of these fluoro-amide derivatives, processes for preparing them, pharmaceutical compositions containing such peptide derivatives and methods for their use.Type: GrantFiled: May 7, 1990Date of Patent: December 14, 1993Assignee: ICI Americas Inc.Inventor: Donald J. Wolanin
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Patent number: 5194628Abstract: The reaction of 2,2-difluorobenzo-1,3-dioxole with (a) an alkali metal or an alkali metal compound and then (b) a compound R.sup.1 -Z.sup.1 l in which Z.sup.1 is a leaving group, or with an aldehyde produces compounds of formula I ##STR1## wherein R.sup.1 l is --OH, --SH, --CHO, --CN, --COOH, --B(OH).sub.2, --COX, with X being Cl or Br, or is --COOR.sup.2, --SiR.sub.3.sup.2 or --B(OR.sup.2).sub.2, with R.sup.2 being a C.sub.1 -C.sub.12 alcohol moiety without the hydroxy group, wherein R.sup.1 is further --C.sub.n H.sub.2n COOR.sup.2, with n being an integer from 1 to 4, or linear or branched C.sub.1 -C.sub.12 hydroxyalkyl which is unsubstituted or is substituted by --F, --CN, C.sub.1 -C.sub.6 alkoxy, phenyl, fluorophenyl, C.sub.1 -C.sub.4 alkoxy-phenyl, C.sub.1 -C.sub.4 alkylthio-phenyl, C.sub.1 -C.sub.4 alkyl-phenyl, C.sub.1 -C.sub.4 fluoroalkyl-phenyl, nitrophenyl or by cyanophenyl, or wherein R.sup.1 is a benzyl alcohol which is unsubstituted or is substituted by F, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.Type: GrantFiled: September 14, 1990Date of Patent: March 16, 1993Assignee: Ciba-Geigy CorporationInventors: Peter Ackermann, Hans-Ruedi Kanel, Bruno Schaub
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Patent number: 5015777Abstract: A process for the preparation of aromatic beta-diketones by the reaction of an acetophenone and a molar excess of an alphatic ester or an ester of benzoic acid in the presence of sodium alkoxide condensation agent in an aromatic hydrocarbon solvent. Also disclosed is a method of recycling the solvent and excess ester reactant after separation of the aromatic beta-diketone product.Type: GrantFiled: November 2, 1989Date of Patent: May 14, 1991Assignee: Witco CorporationInventors: Daniel R. Chisolm, Richard A. Weiss, Leonid Rozov
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Patent number: 4929741Abstract: Propiolophenone derivatives of the formula ##STR1## wherein R.sup.6 is hydrogen, lower alkyl or a group of the formula ##STR2## as well as corresponding hydroxy compounds of the formula ##STR3## wherein R.sup.6' is hydrogen, lower alkyl, a group of formula (a), (b), (c), (d) or (e) or a group of the formula--C(R.sup.14)(R.sup.15)OR.sup.16' (f'):exhibit mucosa-protective and/or gastric acid secretion-inhibiting properties, such that they can be used for the control or prevention of illnesses of the gastrointestinal tract, especially against gastric ulcers and/or duodenal ulcers.Type: GrantFiled: March 17, 1988Date of Patent: May 29, 1990Assignee: Hoffman-La Roche Inc.Inventors: Albert Fischli, Eva-Maria Gutknecht, Daniel Obrecht
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Patent number: 4822905Abstract: Compounds having the structural formula ##STR1## wherein R.sub.1, R.sub.2 R.sub.3, R.sub.4 and R.sup.5 are the same or different and are selected from the group consisting of hydrogen, chlorine, bromine, iodine, nitro, alkyl having from 1 to 4 carbon atoms, alkoxy having from 1 to 4 carbon atoms, trifluoromethyl, trifluoromethoxy, cyano, alkylsulfonyl, and alkylthio having from 1 to 4 carbon atoms, and wherein R.sub.2 and R.sub.3 or R.sub.3 and R.sub.4 together can be methylene or ethylenedioxy.Type: GrantFiled: June 9, 1986Date of Patent: April 18, 1989Assignee: Stauffer Chemical CompanyInventors: David L. Lee, Donald R. James, William J. Michaely
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Patent number: 4797415Abstract: A new series of benzofuran and benzothiophene derivatives are disclosed. These compounds have a structure which can be obtained by substituting the third position of 2-lower alkyl-benzofuran or 2-lower alkyl-benzothiophene with a substituted benzene derivative, itaconic acid derivative or a substituted phenoxymethyl tetrazole derivative. They are useful as diuretics without side effects of elevating serum uric acid levels and can be used in the treatment of hyperuricemia.Type: GrantFiled: July 28, 1986Date of Patent: January 10, 1989Assignee: Kotobuki Seiyaku Company LimitedInventors: Tsuyoshi Tomiyama, Akira Tomiyama, Koichi Kubota
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Patent number: 4617392Abstract: 4-Alkyl-5,6-, 6,7-methylenedioxy-2-1[H]-quinazolinones are prepared from 2,3-methylenedioxyacetophenones. The 4-alkyl-5,6-, 6,7-methylenedioxy-2-1[H]-quinazolinones are active as cardiotonic agents.Type: GrantFiled: September 29, 1983Date of Patent: October 14, 1986Assignee: Ortho Pharmaceutical CorporationInventors: Victor T. Bandurco, Stanley C. Bell, Donald W. Combs, Robert Falotico
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Patent number: 4544766Abstract: This invention relates to a process for preparing an aryl acetic acid derivative represented by the formulaAr--CH.sub.2 COY).sub.ncomprising hydrolyzing in an alkaline substance a dichloroethenyl compound represented by the formulaAr--CH.dbd.CCl.sub.2).sub.n.Type: GrantFiled: February 26, 1982Date of Patent: October 1, 1985Assignee: Otsuka Kagaku Yakuhin Kabushiki KaishaInventor: Tatsuya Shono
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Patent number: 4435585Abstract: There is disclosed a novel process for preparing a number of cinnamaldehyde derivatives. These cinnamaldehyde derivatives can be reduced to dihydrocinnamaldehyde derivatives, a number of which are commercially important in the preparation of fragrances. The invention is also directed to a number of novel intermediates and their preparation.Type: GrantFiled: November 17, 1981Date of Patent: March 6, 1984Assignee: Givaudan CorporationInventors: Yvo Crameri, Paul A. Ochsner, Peter Schudel
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Patent number: RE41366Abstract: The invention relates to a method for the synthesis of galanthamine, the derivatives and analogues thereof of formula (1) where R1=a hydrogen atom, R2=a hydroxy group, R1 and R2 together form ?O, R3, R4, and R5 independently=a hydrogen atom, a hydroxy group or a (C1-C2)alkoxy group, R6?H, (C1-C12)alkyl, (CH2)nNR7R8, or —(CH2)nN+R7R8R9 where n=1 to 12, Z=two hydrogen atoms, or an oxygen atom and X=an oxygen, sulphur or nitrogen atom, or a —SO, —SO2, or —NR6 group where R6 is as defined above or is an amine protecting group.Type: GrantFiled: June 14, 2002Date of Patent: June 1, 2010Assignee: Centre National del la Recherche Scientifique (CNRS)Inventors: Claude Thal, Catherine Guillou, Jean-Luc Beunard, Emmanuel Gras, Pierre Potier