The Nitrogen Is Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 549/452)
  • Patent number: 9126967
    Abstract: A process for the production of dioxolane compounds of formula (I): wherein R1 and R2 independently represent hydrogen or an alkyl chain from 1 to 10 carbon atoms; R3 and R4 independently represent hydrogen, an alkyl chain from 1 to 5 carbon atoms, or an alkyl chain from 1 to 5 carbon atoms which is endowed with one or more hydroxyl groups, such process comprising a reaction between crude glycerol and an aldehyde or a ketone, with a molar ratio of aldehyde:glycerol or ketone:glycerol from 3:1 to 20:1.
    Type: Grant
    Filed: September 30, 2011
    Date of Patent: September 8, 2015
    Assignee: RHODIA POLIAMIDA E ESPECIALIDADES LTDA
    Inventors: Edson Rodrigues, Arthur Malheiro
  • Patent number: 9035070
    Abstract: The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: May 19, 2015
    Assignee: ESTEVE QUÍMICA, S.A.
    Inventors: Martí Bartra Sanmarti, Ramon Berenguer Maimo, Jorge Medrano Ruperez, Jorge Garcia Gomez, Javier Ariza Piquer
  • Patent number: 8969559
    Abstract: Disclosed herein are ketal amide compounds. The ketal amide compounds are synthesized by the reaction of ketal acids or ketal esters with amine functional compounds. Also disclosed are methodologies useful to make the ketal amide compounds. Also disclosed herein are formulations and articles containing the ketal amide compounds.
    Type: Grant
    Filed: February 10, 2012
    Date of Patent: March 3, 2015
    Assignee: Segetis, Inc.
    Inventors: Sergey Selifonov, Adam E. Goetz, Marc D. Scholten, Ning Zhou
  • Patent number: 8877945
    Abstract: The present invention provides redox drug derivatives. In particular, 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 1-ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, (3R,4R,5S)-4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylic acid ethyl ester, (3S)-3-(aminomethyl)-5-methylhexanoic acid, (3S)-1-[2-(2,3-dihydro-5-benzofuranyl)ethyl]-?-?-diphenyl-3-pyrrolidineacetamide, (1S,2S,3S,4R)-3-[(1S)-1-acetamido-2-ethyl-butyl]-4-(diaminomethylideneamino)-2-hydroxy-cyclopentane-1-carboxylic acid and (2R,3R,4S)-4-[(diaminomethylidene)amino]-3-acetamido-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid redox derivatives.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: November 4, 2014
    Assignee: Redx Pharma Limited
    Inventors: Derek Lindsay, Peter Jackson
  • Publication number: 20140100374
    Abstract: Industrial synthesis process for the compound of formula (I):
    Type: Application
    Filed: December 11, 2013
    Publication date: April 10, 2014
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Nicolas ROBERT, Jean-Michel Lerestif, Jean-Pierre Lecouve, Marina Gaillard, Loic Meunier, Philippe Letellier, Mathieu Boiret
  • Publication number: 20140100353
    Abstract: The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I employing an aldehyde acetal intermediate, wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.
    Type: Application
    Filed: October 1, 2013
    Publication date: April 10, 2014
    Applicant: NOVARTIS AG
    Inventors: Murat ACEMOGLU, Heribert HELLSTERN, Bernard RISS, Christian SPRECHER
  • Patent number: 8530465
    Abstract: The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.
    Type: Grant
    Filed: August 1, 2012
    Date of Patent: September 10, 2013
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Chia-Chung Lee
  • Publication number: 20130184472
    Abstract: The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.
    Type: Application
    Filed: July 28, 2011
    Publication date: July 18, 2013
    Applicant: ESTEVE QUIMICA, S.A.
    Inventors: Martí Bartra Sanmartí, Ramon Berenguer Maimo, Jorge Medrano Ruperez, Jorge Garcia Gomez, Javier Ariza Piquer
  • Publication number: 20130102641
    Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.
    Type: Application
    Filed: December 13, 2012
    Publication date: April 25, 2013
    Applicant: XENOPORT, INC.
    Inventor: XENOPORT, INC.
  • Publication number: 20130053564
    Abstract: Disclosed herein are ketal amide compounds. The ketal amide compounds are synthesized by the reaction of ketal acids or ketal esters with amine functional compounds. Also disclosed are methodologies useful to make the ketal amide compounds. Also disclosed herein are formulations and articles containing the ketal amide compounds.
    Type: Application
    Filed: February 10, 2012
    Publication date: February 28, 2013
    Applicant: SEGETIS, INC.
    Inventors: Sergey SELIFONOV, Adam E. GOETZ, Marc D. SCHOLTEN, Ning ZHOU
  • Patent number: 8304415
    Abstract: A series of novel 1,2-disubstituted amido-anthraquinone derivatives, and the preparation method and application of said derivatives. Said application includes said derivatives with therapeutically effective amount being prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.
    Type: Grant
    Filed: February 25, 2010
    Date of Patent: November 6, 2012
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Chia-Chung Lee
  • Publication number: 20120271049
    Abstract: A process for preparing phenyl iso(thio)cyanates of the formula I in which a compound of the formula II or its HCl adduct is reacted with a phosgenating agent where W is oxygen or sulfur and Ar and A are as defined in claim 1 is described. Moreover, the invention relates to the use of the phenyl iso(thio)cyanates for preparing crop protection agents.
    Type: Application
    Filed: June 28, 2012
    Publication date: October 25, 2012
    Applicant: BASF AKTIENGESELLSCHAFT
    Inventors: Gerhard Hamprecht, Michael Puhl, Bernd Wolf, Norbert Götz, Michael Keil, Robert Reinhard, Ingo Sagasser, Werner Seitz
  • Publication number: 20120196947
    Abstract: The present disclosure relates to the preparation of ketal compounds from glycerol and levulinic acid and esters, and uses thereof, in particular the manufacture of polyurethanes.
    Type: Application
    Filed: April 12, 2012
    Publication date: August 2, 2012
    Applicant: SEGETIS, INC.
    Inventor: Sergey SELIFONOV
  • Publication number: 20120077974
    Abstract: The present invention provides redox drug derivatives. In particular, 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 1-ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, (3R,4R,5S)-4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylic acid ethyl ester, (3S)-3-(aminomethyl)-5-methylhexanoic acid, (3S)-1-[2-(2,3-dihydro-5-benzofuranyl)ethyl]-?-?-diphenyl-3-pyrrolidineacetamide, (1S,2S,3S,4R)-3-[(1S)-1-acetamido-2-ethyl-butyl]-4-(diaminomethylideneamino)-2-hydroxy-cyclopentane-1-carboxylic acid and (2R,3R,4S)-4-[(diaminomethylidene)amino]-3-acetamido-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid redox derivatives.
    Type: Application
    Filed: May 17, 2010
    Publication date: March 29, 2012
    Inventors: Derek Lindsay, Peter Jackson
  • Publication number: 20120022100
    Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
    Type: Application
    Filed: September 28, 2011
    Publication date: January 26, 2012
    Inventors: Juergen Klaus Maibaum, Daniel K. Baeschlin, Holger Sellner
  • Publication number: 20110275797
    Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.
    Type: Application
    Filed: January 29, 2010
    Publication date: November 10, 2011
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
  • Publication number: 20110136902
    Abstract: There provided a 12-membered-ring macrolactam derivative having antitumor activity: A compound represented by Formula (1) or a salt thereof. In this Formula, R1 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkylcarbonyl group or a C6-14 arylcarbonyl group; R2 is a hydrogen atom or a C1-6 alkyl group; R3 is a hydrogen atom or a hydroxyl group; R4 is a hydrogen atom or a hydroxyl group; R5 is a hydrogen atom or a C1-6 alkyl group; R6 is a hydrogen atom or a hydroxyl group; and R7 is an acetyl group or the like.
    Type: Application
    Filed: February 15, 2011
    Publication date: June 9, 2011
    Inventors: Masayuki MIYANO, Daisuke ITO, Norio MURAI
  • Publication number: 20110105522
    Abstract: The application discloses ketoconazole derivatives that are antagonists of the human pregnane X receptor (PXR), methods of preparing the derivatives, uses of the derivatives with drug therapy, and methods of inhibiting tumor cell proliferation and multidrug resistance using inhibitors of PXR.
    Type: Application
    Filed: January 27, 2009
    Publication date: May 5, 2011
    Inventors: Sridhar Mani, Bhaskar C. Das
  • Patent number: 7750049
    Abstract: The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-carboxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl. R2 is te/t-butyl or trifluoromethyl; R3 is independently selected from hydrogen, carboxy, cyano, alkyl or hydroxyalkyl, The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, hemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: July 6, 2010
    Assignee: Pharmeste S.R.L.
    Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti, Francesca Fruttarolo, Maria Giovanna Pavani, Marcello Trevisani
  • Publication number: 20100069625
    Abstract: Disclosed is a method for preparing 2?-deoxy-2?,2?-difluorocytidine of Formula I comprising, preparing an optically pure 3R-hydroxypropane amide compound of Formula VIII from an optical ester compound of Formula IX using an optically active chiral amine, preparing an optically pure D-erythro-2,2-difluoro-2-deoxy-1-oxoribose compound of Formula V from the compound of Formula VIII, glycosylating the compound of Formula V with a nucleobase to prepare the 2?-deoxy-2?,2?-difluorocytidine of Formula I as a ?-nucleoside. With the present invention, it is possible to prepare an optically pure compound of Formula I in a high purity and a high yield. In the Formulae, R1 and R2 are protecting groups and are each independently benzoyl, 4-methylbenzoyl, 3-methylbenzoyl, 4-cyanobenzoyl, 3-cyanobenzoyl, 4-propylbenzoyl, 2-ethoxybenzoyl, 4-t-butylbenzoyl, 1-naphthoyl or 2-naphthoyl, R3, R4 and R7 are each independently C1-C3 alkyl, R5 is methyl or ethyl, R6 is hydrogen, methyl or methoxy.
    Type: Application
    Filed: March 20, 2008
    Publication date: March 18, 2010
    Applicant: DONGWOO SYNTECH CO., LTD
    Inventors: Su-Jin Park, Chun-Rim Oh, Young-Deuck Kim
  • Publication number: 20090240015
    Abstract: The present invention provides compounds having in their molecule a structure contributing to high hydrophilicity, and having high photopolymerizability, as well as polymers of such compounds, and a method for producing the compound. The compounds are diol (meth)acrylate having a urethane bond represented by the formula (1), and cyclic ketal (meth)acrylate having a urethane bond represented by the formula (2): (R1: H, —CH3; R2: —(CH2)n-; R3: —(CH2)m-; n: 1-4; m: 1-8; (AO): C2-C4 oxyalkylene group; x: 0-1000; R4, R5: H, —CH3, —C2H5).
    Type: Application
    Filed: June 4, 2009
    Publication date: September 24, 2009
    Applicant: NOF Corporation
    Inventors: Eui-chul Kang, Atsuhiko Ogura, Shingo Kataoka, Takashi Iwata
  • Publication number: 20090176786
    Abstract: The present invention relates to a benzoylurea compound represented by formula (I): wherein, X and Y represent a fluorine atom or a chlorine atom, R1 represents a lower alkyl group or the like, R2 represents a lower alkyl group, R3 represents a halogen atom or the like, R4 represents an alkylthio group optionally substituted with one or more of halogen atoms, or a salt thereof, and use thereof for controlling pests and the like.
    Type: Application
    Filed: October 16, 2006
    Publication date: July 9, 2009
    Inventors: Masato Konobe, Shigeyuki Itoh, Norihisa Sakamoto, Araki Tomohiro, Yoshitomo Tohyama
  • Publication number: 20090105237
    Abstract: A method of conferring a cooling effect on the skin or mucous membranes by applying thereto at least one compound of the Formula I: (a) wherein B is selected from H, CH3, C2H5, OCH3, OC2H5; and OH; and (b) wherein A is a moiety of the formula —CO-D, wherein D is selected from the following moieties: (i) —NR1R2, wherein R1 and R2 are independently selected from H and C1-C8 straight or branched-chain aliphatic, alkoxyalkyl, hydroxyalkyl, araliphatic and cycloalkyl groups, or R1 and R2 together with the nitrogen atom to which they are attached form part of an optionally-substituted, five- or six-membered heterocyclic ring; (ii) —NHCH2COOCH2CH3, —NHCH2CONH2, —NHCH2CH2OCH3, —NHCH2CH2OH, —NHCH2CH(OH)CH2OH and (iii) a moiety selected from the group consisting of: The compounds are useful for providing cooling effects in a variety of products, such as foodstuffs, confectionery, tobacco products, beverages, cosmetics, dentifrices, medicinal preparations, mouthwashes and toiletries.
    Type: Application
    Filed: May 24, 2006
    Publication date: April 23, 2009
    Inventors: Karen Ann Bell, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack
  • Publication number: 20090082328
    Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 9, 2008
    Publication date: March 26, 2009
    Inventors: Yingfu Li, Joachim Rudolph, Jacques P. Dumas, Daniel Auclair, Mario Lobell, Marion Hitchcock, Ingo Hartung, Marcus Koppitz, Dominic Brittain, Florian Puehler, Kirstin Petersen, Judith Guenther
  • Publication number: 20090076062
    Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
    Type: Application
    Filed: September 13, 2007
    Publication date: March 19, 2009
    Inventors: Juergen Klaus Maibaum, Daniel Kaspar Baeschlin, Holger Sellner
  • Patent number: 6812352
    Abstract: Multidentate phosphite ligands are disclosed for use in reactions such as hydrocyanation and isomerization. The catalyst compositions made therefrom and the various catalytic processes which employ such multidentate phosphite ligands are also disclosed. In particular, the ligands have heteroatom-containing substituents on the carbon attached to the ortho position of the terminal phenol group.
    Type: Grant
    Filed: April 9, 2002
    Date of Patent: November 2, 2004
    Assignee: Invista North America S.a.r.l.
    Inventors: Kristina Ann Kreutzer, Wilson Tam, J. Michael Garner, John Ronald Boyles
  • Patent number: 6812229
    Abstract: It is to provide a novel fungicide having high controlling effects on plant diseases particularly on wheat powdery mildew and cucumber gray mold, without ill effects on crops. A carbamate derivative represented by the general formula [I] {wherein X is a halogen atom, a C1-C6 alkyl group or the like, n is 0 or an integer of from 1 to 4, R1 is a C1-C6 alkyl group, R2 is a hydrogen atom, a C1-C6 alkyl group or the like, R3 is a hydrogen atom or a C1-C6 alkyl group, G is an oxygen atom, a sulfur atom or the like, Y is a hydrogen atom, a C1-C10 alkyl group, C2-C10 alkenyl group or the like, and Q is a hydrogen atom, a C1-C6 haloalkyl group, a phenyl group or the like} and an agricultural/horticultural fungicide containing the same as the active ingredient.
    Type: Grant
    Filed: February 5, 2002
    Date of Patent: November 2, 2004
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Masami Ozaki, Shunichiro Fukumoto, Ryuji Tamai, Kazuhiro Ikegaya, Norihisa Yonekura, Takahiro Kawashima, Junetsu Sakai, Norimichi Muramatsu, Makikazu Takagaki, Kouzou Nagayama
  • Patent number: 6787559
    Abstract: This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Grant
    Filed: October 9, 2002
    Date of Patent: September 7, 2004
    Assignee: Syntex (U.S.A.) LLC.
    Inventors: Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
  • Patent number: 6492394
    Abstract: A compound of the Formula (I): wherein Z, R1, R, and Ar2 are as defined in the specification. This invention also relates to sulfonamide compounds of the Formula (I) that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use, and methods for preparing the compounds.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: December 10, 2002
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
  • Patent number: 6452000
    Abstract: The present invention concerns an improved process for the preparation of asymmetric cyclic ureas as well as intermediates in the preparation of asymmetric cyclic ureas. In the process, a diamine of formula (I-a) is selectively monoacylated to give an asymmetric monoacylated diamine which can be converted into asymmetric intermediates. The asymmetric intermediates can be further alkylated, cyclized, and/or modified to give compounds which are useful as HIV protease inhibitors for the treatment of HIV infection. The invention allows for scalable preparation of a wide variety of asymmetrical cyclic ureas.
    Type: Grant
    Filed: March 7, 2001
    Date of Patent: September 17, 2002
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Benjamin R. P. Stone, Luigi Anzalone, Joseph M. Fortunak, Gregory D. Harris, Ioannis I. Valvis, Robert E. Waltermire
  • Patent number: 6414158
    Abstract: The invention relates to novel carbazate intermediates of formula (II), and to a process for their preparation, and their usefulness in the preparation of (1,3,4) oxadiazine derivatives useful as pesticides, in particular as anthelminthicides, insecticides, acaricides, and nematicides.
    Type: Grant
    Filed: July 6, 2000
    Date of Patent: July 2, 2002
    Assignee: Bayer AKtiengesellschaft
    Inventors: Hubert Dyker, Andrew Plant, Jürgen Scherkenbeck, Christoph Erdelen, Achim Harder
  • Publication number: 20020002307
    Abstract: The instant invention provides a process for the selective N-formylation of N-hydroxylamines.
    Type: Application
    Filed: March 30, 2001
    Publication date: January 3, 2002
    Inventors: David R. Hill, Chi-Nung Hsiao, Ravi Kurukulasuriya, Steve Wittenberger
  • Patent number: 6262084
    Abstract: A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions thereof; and the use of the compounds either as above, or in formulations for the control or prevention of diseases states in which &agr;4&bgr;1 is involved.
    Type: Grant
    Filed: October 14, 1999
    Date of Patent: July 17, 2001
    Assignee: Texas Biotechnology Corporation
    Inventors: Ronald J. Biediger, Vanessa O. Grabbe, George W. Holland, Jamal Kassir, Karin M. Keller, Timothy P. Kogan, Shuqun Lin, Robert V. Market, Bore G. Raju, Ian L. Scott, Chengde Wu
  • Patent number: 6235753
    Abstract: Inhibitors of the Production of s-CD23 and the secretion of TNF are provided.
    Type: Grant
    Filed: January 21, 1999
    Date of Patent: May 22, 2001
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Stuart Bailey, Andrew Faller, David Glynn Smith, Derek Richard Buckle
  • Patent number: 6222052
    Abstract: A process is disclosed for preparing an (S)-2-amino-&ohgr;-oxoalkanoic acid derivative in which the corresponding aldehyde is converted into the corresponding acetal-protected aldehyde, the acetal-protected aldehyde is converted into the corresponding aminonitrile, the aminonitrile is converted into the corresponding amino acid amide, the amino acid amide is subjected to an enzymatic, enantioselective hydrolysis in which the (R)-enantiomer of the amino acid amide remains and the (S)-enantiomer is converted into the (S)-amino acid, and the (S)-amino acid is isolated. Preferably, the reaction mixture obtained after the conversion of the aminonitrile into the amino acid amide is treated with a benzaldehyde to form the Schiff base of the amino acid amide. The Schiff base is separated out and is converted into the free amino acid amide.
    Type: Grant
    Filed: August 18, 2000
    Date of Patent: April 24, 2001
    Assignee: DSM N.V.
    Inventors: Wilhelmus H. J. Boesten, Quirinus B. Broxterman, Marcus J. M. Plaum
  • Patent number: 6177576
    Abstract: A novel composition for supplementing the human diet having a polyol-derived pyruvate (2-keto-propionic-acid) moeity as a component.
    Type: Grant
    Filed: August 5, 1998
    Date of Patent: January 23, 2001
    Inventor: Michael J. Arnold
  • Patent number: 6166227
    Abstract: The glycinamide of the formula (I) ##STR1## is reacted with the dioxolane of the formula (II) ##STR2## wherein L is a leaving group such as iodo, bromo, alkylsulfonyloxy, or arylsulfonyloxy to give the dioxolane of the formula (III) ##STR3## Treatment of (III) gives the dioxolane pentanoic acid IV ##STR4## which can be converted to (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester.
    Type: Grant
    Filed: July 8, 1999
    Date of Patent: December 26, 2000
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Jollie D. Godfrey, Jr., David R. Kronenthal, Mark D. Schwinden
  • Patent number: 6096773
    Abstract: A method for the inhibition of the binding of .alpha..sub.4 .beta..sub.1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which .alpha..sub.4 .beta..sub.1 is involved.
    Type: Grant
    Filed: April 15, 1999
    Date of Patent: August 1, 2000
    Assignee: Texas Biotechnology Corporation, Inc.
    Inventors: Ian L. Scott, Bore G. Raju, Ronald J. Biediger, Vanessa O. Grabbe, Jamal Kassir, Karin M. Keller, Timothy P. Kogan, deceased, Shuqun Lin, Robert V. Market
  • Patent number: 6084131
    Abstract: A process for the preparation of protected dihydroxypropyl trialkylammonium salts, particularly in chiral form is described. In particular, a process for the preparation of (2,2-dimethyl-1,3-dioxolan-4-ylmethyl)trialkylammonium salts, particularly in chiral form is described. Furthermore, a process is described wherein the (2,2-dimethyl-1,3-dioxolan-4ylmethyl)trialkylammonium salts is a 2,2-dimethyl-1,3-dioxolan-4-ylmethyl trimethylammonium salt, preferably in chiral form. The protected dihydroxypropyl trialkylammonium salts lead to L-carnitine (9) when in chiral form (5).
    Type: Grant
    Filed: May 27, 1999
    Date of Patent: July 4, 2000
    Assignee: Board of Trustees operating Michigan State University
    Inventors: Rawle I. Hollingsworth, Guijun Wang
  • Patent number: 6011174
    Abstract: The present invention relates to a compound of the formula (I), or its pharmaceutically acceptable salt or ester: ##STR1## wherein Ar.sup.1 is an aryl group or a heteroaromatic ring group; Ar is a group of the formula ##STR2## each of Ar.sup.2 and Ar.sup.3 is an aryl group or a heteroaromatic ring group; Cy is an aryl group, a heteroaromatic ring group or an aliphatic ring group which may contain one or two oxygen atoms; A.sup.1 is a C.sub.1-4 chain hydrocarbon group; m is an integer of from 1 to 6; each of n and p is an integer of from 0 to 3; Q.sup.1 is a single bond, a group of the formula --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S-- or --SCH.sub.2 --, or a C.sub.1-6 chain hydrocarbon group; Q.sup.2 is a single bond or a group of the formula --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.n --W--(CH.sub.2).sub.p --; Q.sup.3 is a single bond, an oxygen atom, a sulfur atom, a methylene group, a vinylene group or a group of the formula --CO--, --NH--, --COO--, --OCO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.
    Type: Grant
    Filed: August 4, 1998
    Date of Patent: January 4, 2000
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
  • Patent number: 5990158
    Abstract: New therapeutic agents of carboxylic acid derivatives are disclosed, which are represented by the compounds of the following formula (I) or its pharmaceutically acceptable salts, ##STR1## These compounds are useful as a matrix metalloproteinases (MMPs) inhibitors.
    Type: Grant
    Filed: November 3, 1997
    Date of Patent: November 23, 1999
    Assignee: Kotobuki Seiyaku Co., Ltd.
    Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Takashi Yanagisawa, Atsushi Noda, Yoshinori Kobayashi
  • Patent number: 5981511
    Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: March 5, 1997
    Date of Patent: November 9, 1999
    Assignee: G.D. Searle & Co.
    Inventors: Rolando E. Gapud, Timothy J. Hagen, Ann E. Hallinan, Donald W. Hansen, Jr., Robert E. Manning, Suzanne Metz, Barnett S. Pitzele, Foe S. Tjoeng, Mihaly V. Toth, R. Keith Webber
  • Patent number: 5962704
    Abstract: A method for producing an amide derivative of the formula ?XV! ##STR1## wherein each symbol is as defined in the specification, and an enantiomer thereof, a novel intermediate useful for producing said compound and a production method thereof. The production method of the present invention is extremely easy and simple as compared to the conventional methods, and enables effective production of compound ?XV! at high yields, which includes compound ?XVI! having an HIV protease inhibitory action. In addition, the novel intermediates of the present invention are extremely useful as intermediates for producing not only the aforementioned compound ?XVI! but also compounds useful as X-ray contrast media.
    Type: Grant
    Filed: March 25, 1998
    Date of Patent: October 5, 1999
    Assignees: Japan Tobacco Inc., Agouron Pharmaceuticals, Inc.
    Inventors: Takashi Inaba, Yasuki Yamada
  • Patent number: 5945408
    Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: August 8, 1996
    Date of Patent: August 31, 1999
    Assignee: G.D. Searle & Co.
    Inventors: R. Keith Webber, Foe S. Tjoeng, Robert E. Manning
  • Patent number: 5834498
    Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives 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, solid triangles are used to indicate .beta. configuration, dashed bonds represent a double bond, or a single bond, R is a substituted heteroaryl radical, 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.O or represents 2 hydrogen radicals. Certain of the compounds represented by Formula I comprise another aspect of the present invention.
    Type: Grant
    Filed: October 7, 1996
    Date of Patent: November 10, 1998
    Assignee: Allergan
    Inventor: Robert M. Burk
  • Patent number: 5801258
    Abstract: The amide derivative of the present invention is one represented by the following general formula (I) and the dermatologic preparation of the present invention is one containing said amide derivative. ##STR1## wherein R.sup.1 represents a straight-chain or branched, saturated or unsaturated hydrocarbon group carrying 10 to 40 carbon atoms; R.sup.2 represents a straight-chain or branched, saturated or unsaturated hydrocarbon group carrying 3 to 39 carbon atoms; R.sup.3 represents a group containing at least one group represented by the formula: ##STR2## wherein R.sup.4 and R.sup.5 each represents a hydrogen atom or a straight-chain or branched or cyclic, saturated or unsaturated hydrocarbon group, or R.sup.4 and R.sup.
    Type: Grant
    Filed: May 5, 1997
    Date of Patent: September 1, 1998
    Assignee: Kao Corporation
    Inventors: Yukihiro Ohashi, Akira Kawamata, Yukihiro Yada, Kazuhiko Higuchi, Kazue Tsukahara, Genji Imokawa
  • Patent number: 5753707
    Abstract: An amide derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents a C.sub.1-40 hydrocarbon; R.sup.2 represents a C.sub.1-6 alkylene; R.sup.3 represents H, OH or alkoxyl; R.sup.4 represents a C.sub.1-39 hydrocarbon; R.sup.5 represents ##STR2## with the proviso that when R.sup.5 represents ##STR3## R.sup.3 does not represent OH; and a composition of the amide derivative for topical application to human skin. The composition improves the barrier function of the stratum corneum, providing improvement and prevention of dermatitis, skin roughness, or similar disorders.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: May 19, 1998
    Assignee: Kao Corporation
    Inventors: Masahide Hoshino, Hiroshi Kusuoku, Tadashi Hase, Atsuko Otsuka, Ichiro Tokimitsu, Akira Yamamuro, Yoshiya Sugai, Koji Yoshino, Youichi Arai, Shinichi Meguro
  • Patent number: 5744569
    Abstract: In one-component and two-component polyurethane coating compositions comprising at least one reactive component capable of reacting with polyisocyanates, the reactive component is a compound A) containing an isocyanate group, a urethane, thiourethane or urea group and two capped isocyanate-reactive groups.
    Type: Grant
    Filed: June 28, 1996
    Date of Patent: April 28, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Bruchmann, Hans Renz, Gunter Mohrhardt
  • Patent number: 5739374
    Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: February 14, 1997
    Date of Patent: April 14, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5723646
    Abstract: There are described new amino acid amide derivatives, some of which are known, of the formula (I) ##STR1## in which R.sup.1 to R.sup.8 have the meaning given in the description, and a process for their preparation. The amino acid amide derivatives of the formula (I) are used for the preparation of pesticides.
    Type: Grant
    Filed: January 16, 1992
    Date of Patent: March 3, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Thomas Seitz, Heinz-Wilhelm Dehne