Plural Oxygens Bonded Directly To The Oxazine Ring 3,1-benzoxazine-2,4- Diones (including Hydrogenated) Patents (Class 544/94)
  • Patent number: 9301529
    Abstract: The present invention discloses a polysubstituted pyridyl pyrazolecarboxamide and its preparation method and use. The structure of the polysubstituted pyridyl pyrazolecarboxamide of the present invention is shown in the following General Formula I. The polysubstituted pyridyl pyrazolecarboxamide has the following advantages such as good insecticidal effect, low production cost; and it may be used in control of agriculture, forest or health pests, especially of resistant pests. For its preparation method, the yield is high, the number of steps is small, and the operation is simple.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: April 5, 2016
    Assignee: ZHAOQING ZHENGE BIOLOGICAL TECHNOLOGY CO., LTD
    Inventors: Boli Wang, Yong Zhao, Daohang He, Weiwen Li
  • Patent number: 9018203
    Abstract: The present invention provides a pharmaceutical composition of salicylanilide-derived small molecules include: (a) a compound which structure is selected from formula I or formula II: (b) a pharmaceutically acceptable salt and excipient. The present invention also provides the synthesis method of the pharmaceutical composition and the application thereof.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: April 28, 2015
    Assignee: National Defense Medical Center
    Inventors: Deh-Ming Chang, Hsu-Shan Huang, Chun-Liang Chen, Chia-Chung Lee
  • Patent number: 8975255
    Abstract: The present invention provides a biphenyl benzamide-derived derivatives, which structure is selected from formula I or formula II: and the synthesis and the application thereof.
    Type: Grant
    Filed: August 9, 2012
    Date of Patent: March 10, 2015
    Assignee: National Defense Medical Center
    Inventors: Deh-Ming Chang, Hsu-Shan Huang, Chia-Chung Lee, Chun-Liang Chen
  • Publication number: 20130338151
    Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
    Type: Application
    Filed: October 21, 2010
    Publication date: December 19, 2013
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Publication number: 20130302378
    Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.
    Type: Application
    Filed: July 8, 2013
    Publication date: November 14, 2013
    Inventors: Viswajanani J. SATTIGERI, Venkata P. PALLE, Manoj Kumar KHERA, Ranadheer REDDY, Manoj Kumar TIWARI, Ajay SONI, Abdul Rehman Abdul RAUF, Sony JOSEPH, Arpita MUSIB, Sunanda G. DASTIDAR, Punit Kumar SRIVASTAVA
  • Publication number: 20130281412
    Abstract: The present invention provides a pharmaceutical composition of salicylanilide-derived small molecules include: (a) a compound which structure is selected from formula I or formula II: (b) a pharmaceutically acceptable salt and excipient. The present invention also provides the synthesis method of the pharmaceutical composition and the application thereof.
    Type: Application
    Filed: September 11, 2012
    Publication date: October 24, 2013
    Inventors: Deh-Ming CHANG, Hsu-Shan Huang, Chun-Liang Chen, Chia-Chung Lee
  • Patent number: 8557982
    Abstract: The present invention relates to compounds of general formula (I) as tublin polymerization inhibitors and methods for preparing such compounds.
    Type: Grant
    Filed: August 13, 2012
    Date of Patent: October 15, 2013
    Assignee: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
  • Publication number: 20130253179
    Abstract: The present invention relates to a process of functionalising at least one ribonucleic acid (RNA) molecule which comprises the following steps: a) having at least: a binding molecule constituted by an isatoic anhydride or a derivative thereof, a group of interest, and a binding arm linking the binding molecule with the group of interest, b) reacting the anhydride function of the binding molecule with at least one hydroxyl group in: position 2? of the ribose of one of the RNA nucleotides, and/or position(s) 2? and/or 3? of the ribose of the nucleotide at the 3? terminal end of the RNA, and c) obtaining an anthranilate linking, via the binding arm, the RNA to the group of interest. The invention also relates to a functionalising reagent able to be used in such processes, a functionalised biological RNA molecule capable of being obtained by these processes and a kit for detecting a target RNA molecule comprising such a reagent.
    Type: Application
    Filed: December 5, 2011
    Publication date: September 26, 2013
    Inventors: Arnaud Burr, Ali Laayoun, Alain Laurent
  • Patent number: 8461385
    Abstract: The present invention relates to a method of preparing N-substituted salicylamides or derivatives thereof, and their salts, hydrates and solvates. In particular, the present invention relates to a method of preparing N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC) and its corresponding disodium monohydrate.
    Type: Grant
    Filed: December 14, 2005
    Date of Patent: June 11, 2013
    Assignee: Novartis AG
    Inventors: Bernhard Riss, Ulrich Meier
  • Publication number: 20120270863
    Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
    Type: Application
    Filed: October 21, 2010
    Publication date: October 25, 2012
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Publication number: 20120202782
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or dysregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).
    Type: Application
    Filed: April 12, 2012
    Publication date: August 9, 2012
    Applicant: IRM LLC
    Inventors: Badry Bursulaya, Dai Cheng, Jiqing Jiang, Donald S. Karanewsky, Yi Liu, Shifeng Pan, Yongqin Wan, Xia Wang, Yun Feng Xie, Yang Yang
  • Patent number: 8222405
    Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: July 17, 2012
    Assignee: Ajinomoto Co., Inc.
    Inventors: Shingo Makino, Tatsuya Okuzumi, Toshihiko Yoshimura, Yuko Satake, Nobuyasu Suzuki, Hiroyuki Izawa, Kazuyuki Sagi, Akira Chiba, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
  • Publication number: 20120108576
    Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.
    Type: Application
    Filed: November 30, 2011
    Publication date: May 3, 2012
    Applicant: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande
  • Patent number: 8153844
    Abstract: Disclosed is a method for preparing a compound of Formula 1 by contacting compound of Formula 2 with R1—NH2 in the presence of a carboxylic acid and a method for preparing a compound of Formula 2 by contacting a compound of Formula 4 with phosphorus tribromide. wherein R1 is H, C1-C4 alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R2 is CH3 or Cl; R3 is C1-C6 alkyl or C3-C6 alkenyl, each optionally substituted with up to 3 halogen and up to 1 phenyl; and X is Cl or Br. Also disclosed is a method for preparing a compound of Formula 5 wherein R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 that is characterized by preparing the compound of Formula 1 by the method above.
    Type: Grant
    Filed: June 27, 2007
    Date of Patent: April 10, 2012
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Richard F. Davis, Rafael Shapiro, Eric G. Taylor
  • Publication number: 20110313154
    Abstract: A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3? which is a group corresponding to R3 is protected.
    Type: Application
    Filed: August 26, 2011
    Publication date: December 22, 2011
    Applicant: AJINOMOTO CO., INC.
    Inventors: Noriyasu KATAOKA, Kotaro OKADO, Tatsuhiro YAMADA, Koichi FUJITA, Tamotsu SUZUKI, Tatsuya OKUZUMI, Masayuki SUGIKI, Akinori TATARA
  • Patent number: 8026335
    Abstract: The present invention provides a baked resin product that exhibits an excellent heat resistance and an electronic device that incorporates this baked resin product. The present invention provides a baked resin product obtained by baking a resin composition that contains a main chain-type aromatic benzoxazine structure, wherein the baked resin product has a peak measured by 13C-NMR at 58±2 ppm and a half width of this peak of 4 to 10 ppm. The present invention also provides a method of producing a baked resin product, comprising baking a resin composition that contains a main chain-type aromatic benzoxazine structure at 270° C. to 350° C. The present invention further provides an electronic device that incorporates this baked resin product.
    Type: Grant
    Filed: May 1, 2007
    Date of Patent: September 27, 2011
    Assignee: Sekisui Chemical Co., Ltd.
    Inventors: Yoshinori Chiku, Yuji Eguchi, Kazuo Doyama
  • Patent number: 7994270
    Abstract: The present invention provides a method for producing a thermosetting resin having a benzoxazine ring, comprising the step of: reacting a bifunctional phenol compound, a diamine compound, and an aldehyde compound in a mixed solvent of an aromatic nonpolar solvent and an alcohol.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: August 9, 2011
    Assignee: Sekisui Chemical Co., Ltd
    Inventors: Tomoaki Katagiri, Yuji Eguchi
  • Publication number: 20110092700
    Abstract: The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N? etc., Y3 and Y4 are selected from —CH? etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.
    Type: Application
    Filed: December 3, 2010
    Publication date: April 21, 2011
    Inventors: Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
  • Patent number: 7915406
    Abstract: The invention relates to a method for preparing a benzoxazinone comprising reacting an isatoic anhydride with an acylating compound in the presence of an N-alkyl imidazole, to a method for preparing a photo-stabilised composition, comprising adding a benzoxazinone and to the use of a benzoxazinone as a light-absorber or as a stabiliser for a light-sensitive compound.
    Type: Grant
    Filed: January 5, 2007
    Date of Patent: March 29, 2011
    Assignee: Temsa International Inc.
    Inventor: Asim Kumar Sarkar
  • Publication number: 20110065918
    Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.
    Type: Application
    Filed: November 22, 2010
    Publication date: March 17, 2011
    Applicant: Ajinomoto Co., Inc.
    Inventors: Shingo MAKINO, Tatsuya Okuzumi, Toshihiko Yoshimura, Yuko Satake, Nobuyasu Suzuki, Hiroyuki Izawa, Kazuyuki Sagi, Akira Chiba, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
  • Publication number: 20110009626
    Abstract: The present invention relates to an adenosine A3 receptor ligand of the general formula (VI?), (VII?) and (VIII?) and their preparation.
    Type: Application
    Filed: August 11, 2010
    Publication date: January 13, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Peter ARANYI, Sandor BATORI, Geza TIMARI, Kinga BOER, Zoltan KAPUI, Endre MIKUS, Katalin URBAN-SZABO, Katalin GERBER, Judit VARGANE SZEREDI, Michel FINET
  • Publication number: 20100184748
    Abstract: The invention provides a novel class of compounds of formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or dysregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).
    Type: Application
    Filed: June 12, 2008
    Publication date: July 22, 2010
    Applicant: IRM LLC
    Inventors: Badry Bursulaya, Dai Cheng, Jiqing Jiang, Donald S. Karanewsky, Yi Liu, Shifeng Pan, Yongqin Wan, Xia Wang, Yun Feng Xie, Yang Yang
  • Publication number: 20100004233
    Abstract: The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N? etc., Y3 and Y4 are selected from —CH? etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.
    Type: Application
    Filed: February 9, 2007
    Publication date: January 7, 2010
    Inventors: Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
  • Publication number: 20090318688
    Abstract: A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3? which is a group corresponding to R3 is protected.
    Type: Application
    Filed: May 22, 2009
    Publication date: December 24, 2009
    Applicant: AJINOMOTO CO., INC.
    Inventors: Noriyasu KATAOKA, Kotaro OKADO, Tatsuhiro YAMADA, Koichi FUJITA, Tamotsu SUZUKI, Tatsuya OKUZUMI, Masayuki SUGIKI, Akinori TATARA
  • Publication number: 20090306372
    Abstract: Disclosed is a method for preparing a compound of Formula 1 by contacting compound of Formula 2 with R1—NH2 in the presence of a carboxylic acid and a method for preparing a compound of Formula 2 by contacting a compound of Formula 4 with phosphorus tribromide. wherein R1 is H, C1-C4 alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R2 is CH3 or Cl; R3 is C1-C6 alkyl or C3-C6 alkenyl, each optionally substituted with up to 3 halogen and up to 1 phenyl; and X is Cl or Br. Also disclosed is a method for preparing a compound of Formula 5 wherein R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 that is characterized by preparing the compound of Formula 1 by the method above.
    Type: Application
    Filed: June 27, 2007
    Publication date: December 10, 2009
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Richard F. Davis, Rafael Shapiro, Eric G. Taylor
  • Publication number: 20090253811
    Abstract: The present invention relates to a method of preparing N-substituted salicylamides or derivatives thereof, and their salts, hydrates and solvates. In particular, the present invention relates to a method of preparing N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC) and its corresponding disodium monohydrate.
    Type: Application
    Filed: December 14, 2005
    Publication date: October 8, 2009
    Inventors: Bernhard Riss, Ulrich Meier
  • Publication number: 20090247745
    Abstract: The present invention relates to an adenosine A3 receptor ligand of the general formula (I), within those preferably to the antagonists, including a salt, solvate or isomer (tautomer, desmotrop, and optically active isomer) thereof, to a pharmaceutical composition containing the ligand, to the use of the ligand, to its preparation, and intermediates of the ligand of the general formula (II?), (III?), (IV?), (V?), (VI?), (VII?), (VIII?) and (XIII?) and their preparation.
    Type: Application
    Filed: June 15, 2009
    Publication date: October 1, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Peter ARANYI, Sandor BATORI, Geza TIMARI, Kinga BOER, Zoltan KAPUI, Endre MIKUS, Katalin URBAN-SZABO, Katalin GERBER, Judit VARGANE SZEREDI, Michel FINET
  • Patent number: 7495096
    Abstract: Processes for the production of a compound of the following formula (I) by converting a compound of formula (II) with 2-pyrrolidone used in excess relative to compound (II) and processes for the production of a compound of formula (III). The latter process includes preparing compound (I); a reduction reaction which yields compound (III) in salt form; and liberating compound (III) from the salt.
    Type: Grant
    Filed: January 22, 2004
    Date of Patent: February 24, 2009
    Assignee: HF Arzneimittelforschung GmbH
    Inventors: Joachim Moormann, Hans-Rainer Hoffmann, Rudolf Matusch
  • Publication number: 20080146544
    Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.
    Type: Application
    Filed: February 25, 2008
    Publication date: June 19, 2008
    Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
  • Patent number: 7339057
    Abstract: A method for preparing a fused oxazinone is disclosed in which (1) a carboxylic acid is contacted with a sulfonyl chloride in the presence of an optionally substituted pyridine compound, the nominal mole ratio of sulfonyl chloride to carboxylic acid being from about 0.75 to 1.5; (2) the mixture prepared in (1) is contacted with an ortho-amino aromatic carboxylic acid in the presence of an optionally substituted pyridine compound, the nominal mole ratio of the ortho-amino aromatic carboxylic acid to carboxylic acid charged in (1) being from about 0.8 to 1.2; and (3) additional sulfonyl chloride is added to the mixture prepared in (2), the nominal mole ratio of additional sulfonyl chloride added in (3) to carboxylic acid charged in (1) being at least about 0.5.
    Type: Grant
    Filed: July 29, 2003
    Date of Patent: March 4, 2008
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Eric Deguyon Taylor
  • Patent number: 7276601
    Abstract: A method for preparing a fused oxazinone is disclosed in which a carboxylic acid is contacted with a sulfonyl chloride and an isatoic anhydride in the presence of a tertiary amine, the nominal mole ratio of said sulfonyl chloride to said carboxylic acid being from about 1.0 to 1.5 and the nominal mole ratio of said isatoic anhydride to said carboxylic acid is from about 0.8 to 1.2.
    Type: Grant
    Filed: June 10, 2004
    Date of Patent: October 2, 2007
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Eric DeGuyon Taylor
  • Patent number: 7169776
    Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.
    Type: Grant
    Filed: January 19, 2005
    Date of Patent: January 30, 2007
    Assignee: Emisphere Technologies, Inc.
    Inventors: Joseph N. Bernadino, Doris C. O'Toole, William E. Bay
  • Publication number: 20040092502
    Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) 1
    Type: Application
    Filed: December 19, 2001
    Publication date: May 13, 2004
    Inventors: John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
  • Patent number: 6624161
    Abstract: The use of a compound comprising formula (I): or a salt, ester, amide or prodrug therof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality, e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them. In formula (I) A is a 6-membered aromatic or heteroaromatic ring; and R1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups.
    Type: Grant
    Filed: July 6, 2001
    Date of Patent: September 23, 2003
    Assignee: Alizyme Therapeutics Limited
    Inventors: Harold Francis Hodson, Robert Downham, Timothy John Mitchell, Beverley Jane Carr, Christopher Robert Dunk, Richard Michael John Palmer
  • Patent number: 6541629
    Abstract: The present invention relates to polymer conjugates having the formula: wherein T is a heterocyclic unit which is capable of inhibiting one or more proteolytic enzymes; L is a linking group; [Poly] is a polymeric unit, i indicates the number of said heterocyclic units which comprise said conjugate and has the value of from 1 to 100; z is 0 or 1, said polymer conjugates suitable for use in preventing skin irritation resulting from exposure of the skin to body fluids, inter alia, feces, menstrual fluid. The conjugates of the present invention are useful in diapers, dressings, sanitary napkins, and the like.
    Type: Grant
    Filed: September 8, 2000
    Date of Patent: April 1, 2003
    Assignee: The Procter & Gamble Company
    Inventors: Scott Edward Osborne, Todd Laurence Underiner
  • Patent number: 6504028
    Abstract: The present invention relates to a process for forming polymer conjugates which are useful as enzyme inhibitors. The process of the present invention comprises the steps of: a) reacting a polymer or copolymer alcohol to form a chloroformate; b) combining a substituted or unsubstituted anthranilic acid comprising an enzyme interaction attenuating unit; and a base catalyst wherein the base catalyst is a supported base catalyst, to form a substrate reactive admixture; and c) adding to said chloroformate formed in step (a) said substrate reactive admixture formed in step (b) to form a benzoxazin-4-one conjugate.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: January 7, 2003
    Assignee: The Procter & Gamble Co.
    Inventors: Renae Dianna Fossum, Todd Laurence Underiner
  • Patent number: 6399798
    Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide (hereinafter referred to as a “protected/activated salicylamide”). The method comprises the steps of (a) alkylating the protected/activated salicylamide with an alkylating agent to form a protected/activated alkylated salicylamide, and (b) deprotecting and deactivating the protected/activated alkylated salicylamide, simultaneously or in any order, to form the alkylated salicylamide. The alkylated salicylamides prepared by this method are suitable for use in compositions for delivering active agents via oral or other routes of administration to animals.
    Type: Grant
    Filed: August 3, 2001
    Date of Patent: June 4, 2002
    Assignee: Emisphere Technologies, Inc.
    Inventors: David Gschneidner, Joseph N. Bernadino, William E. Bay
  • Publication number: 20020028934
    Abstract: The present invention relates to a process for forming polymer conjugates which are useful as enzyme inhibitors.
    Type: Application
    Filed: June 26, 2001
    Publication date: March 7, 2002
    Inventors: Renae Dianna Fossum, Todd Laurence Underiner
  • Patent number: 6133259
    Abstract: Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.
    Type: Grant
    Filed: November 9, 1998
    Date of Patent: October 17, 2000
    Assignee: University of Pittsburgh
    Inventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
  • Patent number: 5981749
    Abstract: A process for producing isatoic anhydrides of the formula (II): ##STR1## which comprises reacting an anthranilic acid of formula (I): ##STR2## or a salt thereof with phosgene using a mixed solvent of water and an organic solvent miscible with water and inert to the reaction;conducting the reaction in the coexistence of an alkylpyridinium salt in an aqueous solvent; orusing a mixed solvent of water and a specific amount of an organic solvent substantially immiscible with water and inert to the reaction.
    Type: Grant
    Filed: June 5, 1998
    Date of Patent: November 9, 1999
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Shinji Nishii, Masashi Komatsu, Hiroshi Ueda
  • Patent number: 5973145
    Abstract: A process for producing isatoic anhydrides of the formula (II): ##STR1## which comprises reacting an anthranilic acid of formula (I): ##STR2## or a salt thereof with phosgene using a mixed solvent of water and an organic solvent miscible with water and inert to the reaction;conducting the reaction in the coexistence of an alkylpyridinium salt in an aqueous solvent; orusing a mixed solvent of water and a specific amount of an organic solvent substantially immiscible with water and inert to the reaction.
    Type: Grant
    Filed: June 5, 1998
    Date of Patent: October 26, 1999
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Shinji Nishii, Masashi Komatsu, Hiroshi Ueda
  • Patent number: 5795984
    Abstract: A process for producing isatoic anhydrides of the formula (II): ##STR1## which comprises reacting an anthranilic acid of formula (I): ##STR2## or a salt thereof with phosgene using a mixed solvent of water and an organic solvent miscible with water and inert to the reaction; conducting the reaction in the coexistence of an alkylpyridinium salt in an aqueous solvent; or using a mixed solvent of water and a specific amount of an organic solvent substantially immiscible with water and inert to the reaction.
    Type: Grant
    Filed: December 26, 1996
    Date of Patent: August 18, 1998
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Shinji Nishii, Masashi Komatsu, Hiroshi Ueda
  • Patent number: 5767121
    Abstract: There is disclosed a pharmaceutical composition for providing antiinflammatory, antipyretic, analgesic, antiallergic, immunosuppressing or immunomodulating activity which comprises a pyridine derivative of the formula (I): ##STR1## wherein R is an optionally substituted pyridine ring, X is a oxygen atom or --S(O).sub.n --, wherein n is 0, 1 or 2, A is a bivalent C.sub.1-15 hydrocarbon residue whose branched moiety may have a substituent, Y is an oxygen or sulfur atom, R.sub.3 is a hydrogen atom or an optionally substituted hydrocarbon residue, R.sub.4 is an optionally substituted hydrocarbon residue or an optionally substituted monocyclic or bicyclic heterocyclic group, R.sub.3 and R.sub.4 may be joined together with the carbamoyl group or the thiocarbamoyl group to which they are attached to form an optionally substituted heterocyclic group, or R.sub.3 or R.sub.
    Type: Grant
    Filed: September 20, 1996
    Date of Patent: June 16, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Muneo Takatani, Taketoshi Saijo, Kiminori Tomimatsu
  • Patent number: 5731441
    Abstract: The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino,carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.
    Type: Grant
    Filed: October 29, 1996
    Date of Patent: March 24, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
  • Patent number: 5604227
    Abstract: The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.
    Type: Grant
    Filed: April 13, 1995
    Date of Patent: February 18, 1997
    Assignee: Imperial Chemical Industries PLC
    Inventors: Thomas M. Bare, Richard B. Sparks
  • Patent number: 5599647
    Abstract: Toning agents are provided for use in thermographic and photothermographic materials, either on their own or in combination with at least one other toning agent, with improved compatibility with hydrophobic media as shown by reduced crystallization and reduced diffusion through the material, which properties enabling an improved imaging performance to be achieved and in particular a more neutral image tone after storage.
    Type: Grant
    Filed: June 20, 1996
    Date of Patent: February 4, 1997
    Assignee: Agfa-Gevaert N.V.
    Inventors: Geert Defieuw, Marcel Monbaliu, Jean-Marie Dewanckele
  • Patent number: 5599814
    Abstract: The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.
    Type: Grant
    Filed: April 24, 1995
    Date of Patent: February 4, 1997
    Assignee: Imperial Chemical Industries, PLC
    Inventors: Thomas M. Bare, Richard B. Sparks
  • Patent number: 5597922
    Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a compound which has high binding to the glycine receptor.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: January 28, 1997
    Assignees: State of Oregon, Acting by and through the Oregon State Board of Higher Education, Acting for and on Behalf of the Oregon Health Sciences University and the University of Oregon, Acea Pharmaceuticals, Inc., The Regents of the University of California
    Inventors: Sui X. Cai, John F. W. Keana, Eckard Weber
  • Patent number: 5342942
    Abstract: Pyrazolo[5,1-b]quinazoline compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds, and methods for treating neurodegenerative disorders, tumors of neuronal origin, inflammation, allergy, and pain, and methods for screening compounds that interact with the neurotrophic receptors using said compositions are disclosed.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: August 30, 1994
    Assignee: Warner-Lambert Company
    Inventors: Juan C. Jaen, Bradley W. Caprathe
  • Patent number: 5292735
    Abstract: The cyclic amide derivative is defined by the formula (I) or a salt thereof: R1--(CH2)n-z in which R1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R3 being hydrogen or a lower alkyl, R4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R2 and R4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.
    Type: Grant
    Filed: June 14, 1991
    Date of Patent: March 8, 1994
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Masahiro Yonaga, Norio Karibe, Youichi Iimura, Satoshi Nagato, Atsushi Sasaki, Yoshiharu Yamanishi, Hiroo Ogura, Takashi Kosasa, Kumi Uchikoshi, Kiyomi Yamatsu