Double Bond Between Ring Members Of The Hetero Ring Patents (Class 549/479)
  • Publication number: 20100221186
    Abstract: Cardiovascular tissue mRNA expression profiles in monkeys treated with coxibs was analyzed. Genomic data indicated that the animals showing vasculitis exhibit a specific mRNA expression pattern. The pattern includes gene expression changes involved in blood and endothelial cell (EC) activation, interaction of blood cells with EC, activation of INF? pathway, and release of pro-inflammatory cytokines and chemo-attractants. These results provide direct evidence of minimal vasculitis together with corresponding genomic signature and peripheral biomarkers for minimal vasculatis. These results also suggest that treatment might triggers/aggravate a clinically latent cardiovascular disorder in the context of an endothelium tropic viral infection and/or an autoimmune vascular disorder. The histopathological examination revealed marginal vascular changes consistent with the genomic findings.
    Type: Application
    Filed: March 10, 2006
    Publication date: September 2, 2010
    Inventors: Hueseyin Firat, Julie Boisclair, Olivier Grenet, Perentes Elias, Martin M. Schumacher
  • Publication number: 20100218415
    Abstract: Accordingly, the current invention provides a method for the manufacture of an ether of 5-hydroxymethylfurfural by reacting a hexose-containing starting material with a higher alcohol in the presence of an acid catalyst, and at a temperature in the range of from 125 to 250 degrees Centigrade.
    Type: Application
    Filed: September 5, 2008
    Publication date: September 2, 2010
    Applicant: FURANIX TECHNOLOGIES B.V.
    Inventors: Gerardus Johannes Maria Gruter, Leo Ernest Manzer
  • Publication number: 20100204480
    Abstract: The present invention relates to a process for preparing 4-aminobut-2-enolides and also corresponding intermediates and starting compounds which are passed through or used in the process according to the invention.
    Type: Application
    Filed: September 5, 2008
    Publication date: August 12, 2010
    Applicant: BAYER CROPSCIENCE
    Inventors: Norbert Lui, Jens-Dietmar Heinrich
  • Publication number: 20100197781
    Abstract: The present invention provides an antimalarial compound 3-[2-(2-Hydroxymethyl-1, 4a, 5-trimethyl-7-oxo-1,2,3,4,4a, 7 8, 8a-octahydronaphthalen-1-yl)-ethyl]-5H-furan-2-one of the formula 1 given below or pharmaceutically acceptable derivatives thereof, isolated from Gomphostema niveum and also provides a method for the extraction thereof as well as methods for the treatment of malaria using said compound.
    Type: Application
    Filed: August 30, 2006
    Publication date: August 5, 2010
    Inventors: Mahabir Prashad Kaushik, Duraipandian Thavaselvam, Manisha Nivsarkar, Badri Narayan Acharya, Subramaniam Prasanna, Krishnamurthy Sekhar
  • Publication number: 20100184974
    Abstract: The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein R2 may be, for example, 2-pyridyl-CH2—, 3-pyridyl-CH2—, 4-pyridyl-CH2—, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R2a—CO)—, R2a being selected from the group consisting of piperonyl, 2-pyranzinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONR5R6, CH2OH or CH2OR7.
    Type: Application
    Filed: September 20, 2007
    Publication date: July 22, 2010
    Applicant: Ambrilia Biopharma Inc.
    Inventors: Brent Richard Stranix, Jean-Francois Lavallee, Nicolas LeBerre, Valerie Perron, Dominik Herbart, Guy Milot, Chandra Panchal
  • Publication number: 20100120905
    Abstract: A method for inhibiting the growth of a microorganism using an effective amount of one or more of the following synthetic brominated furanones: (i) 4-bromo-5Z-(bromomethylene)-3-methylfuran-2-one; (ii) 3-(dibromomethyl)-5-(dibromomethylene)furan-2-one; (iii) 3-(bromomethyl)-5-(dibromomethylene)furan-2-one; (iv) 4-bromo-3-(bromomethyl)-5Z-(bromomethylene)furan-2-one; or (v) 4-bromo-5-(dibromomethyl)-3-methylfuran-2(5H)-one. The brominated furanones inhibit the growth of both fungi and bacteria, including the fungal species Candida albicans, Gloeophyllum trabeum, Chaetomium globosum, and Trametes versicolor and the bacterial species Pseudomonas aeruginosa. The brominated furanones can be used topically or internally to treat human infections, and can be used to treat other objects, such as wood building supplies, to prevent fungal rot.
    Type: Application
    Filed: November 13, 2009
    Publication date: May 13, 2010
    Applicant: SYRACUSE UNIVERSITY
    Inventors: Yan-Yeung Luk, Dacheng Ren
  • Publication number: 20100105714
    Abstract: The invention features compounds of the general Formula (I): (formula should be inserted here) Compounds of Formula (I) possess unexpectedly high affinity for Alk5 and/or Alk4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders.
    Type: Application
    Filed: January 30, 2008
    Publication date: April 29, 2010
    Applicant: Biogen Idec MA Inc.
    Inventors: Lihong Sun, Wen-Cherng Lee, Paul Lyne
  • Publication number: 20100041708
    Abstract: An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.
    Type: Application
    Filed: October 21, 2009
    Publication date: February 18, 2010
    Applicant: ONO PHARMACEUTICAL Co., Ltd.
    Inventors: Atsushi NAGANAWA, Tetsuji Saito, Kaoru Kobayashi, Takayuki Maruyama, Yoshihiko Nakai, Shinsuke Hashimoto
  • Publication number: 20100029752
    Abstract: A pharmaceutical composition containing a pharmaceutical diluent and a compound of formula II: wherein: R8?H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, —C(O)R4, where R4 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms, or —OH, —OR7 or —NR7, where R7 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms; R9=—OR5, —NR5, —NH—NH—R5 where R5 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl, optionally containing halogen atoms; R10?H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, or —CH2C(O)R6, where R6 is OR7 and NR7, where R7?H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl and can optionally contain halogen atoms. Also included in the invention are methods of using the pharmaceutical compositions and the chemical compounds used in the compositions.
    Type: Application
    Filed: July 26, 2006
    Publication date: February 4, 2010
    Inventors: Francis P. Kuhajda, Craig A. Townsend, Susan M. Medghalchi, Jill M. McFadden
  • Publication number: 20100022594
    Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's disease and Down's syndrome are described.
    Type: Application
    Filed: October 9, 2009
    Publication date: January 28, 2010
    Applicants: Wyeth, ArQule, Inc.
    Inventors: Anthony F. Kreft, Derek Cecil Cole, Kevin R. Woller, Joseph R. Stock, George Diamantidis, Dennis M. Kubrak, Kristina M. Kutterer, William J. Moore, David S. Casebier
  • Publication number: 20090281337
    Abstract: A pyridazine compound represented by formula (1): has an excellent plant disease controlling effect.
    Type: Application
    Filed: July 13, 2009
    Publication date: November 12, 2009
    Inventors: Hiroshi Morishita, Akio Manabe
  • Publication number: 20090269323
    Abstract: The present invention relates to a non-amphiphile-based water-in-water emulsion composition. The non-amphiphile-based water-in-water emulsion composition includes a water-soluble polymer, a non-amphiphilic lyotropic mesogen encapsulated by the water-soluble polymer; and water. In one embodiment, the non-amphiphilic lyotropic mesogen includes, without limitation, a lyotropic chromonic liquid crystal, and more specifically disodium cromoglycate (DSCG). In another embodiment, the water-soluble polymer can include, without limitation, a polyacrylamide, a polyol, a polyvinylpyrrolidone, a polysaccharide, or a water-soluble fluoride-bearing polymer. The present invention also relates to a porous hydrogel made with the use of the non-amphiphile-based water-in-water emulsion. The present invention further relates to using the emulsion and hydrogel for various applications.
    Type: Application
    Filed: September 18, 2008
    Publication date: October 29, 2009
    Applicant: Syracuse University Technology Transfer and Industrial Development Office
    Inventors: Yan-Yeung LUK, Karen A. SIMON, Dacheng REN
  • Publication number: 20090232935
    Abstract: The invention relates to new derivatives of 2-methyl-3-furanthiol which are useful as flavoring ingredients to confer meaty, juicy taste to a large variety of edible consumer products, chewing gums and oral care products, without imparting thereto undesirable off-notes typical of prior known furanthiol derivatives.
    Type: Application
    Filed: July 31, 2007
    Publication date: September 17, 2009
    Inventors: Alain Chaintreau, Christian Starkenmann, Sabine Rochat, Francois Benzi
  • Patent number: 7572910
    Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.
    Type: Grant
    Filed: October 18, 2004
    Date of Patent: August 11, 2009
    Assignee: Pfizer, Inc.
    Inventor: Banavara L. Mylari
  • Publication number: 20090192151
    Abstract: Disclosed herein are compounds useful in treating glaucoma, inflammatory bowel disease, the stimulation of hair growth, and the stimulation of the conversion of vellus hair to terminal hair. The compounds themselves are herein.
    Type: Application
    Filed: January 14, 2009
    Publication date: July 30, 2009
    Inventors: David W. Old, Danny T. Dinh
  • Publication number: 20090124664
    Abstract: The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
    Type: Application
    Filed: November 24, 2006
    Publication date: May 14, 2009
    Inventors: Marcello Allegretti, Alessio Moriconi, Andrea Aramini, Maria Candida Cesta, Andrea Beccari, Riccardo Bertini
  • Patent number: 7528157
    Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: May 5, 2009
    Assignee: Asterand UK Limited
    Inventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
  • Publication number: 20090093641
    Abstract: The subject invention pertains to pentafluorosulfanyl (—SF5) substituted compounds and methods of their synthesis. The subject invention provides convenient methods to incorporate the —SF5 substituent into compounds such as heterocycles and alkynes.
    Type: Application
    Filed: March 13, 2007
    Publication date: April 9, 2009
    Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
    Inventors: William R. Dolbier, JR., Akira Mitani
  • Publication number: 20080287532
    Abstract: The present invention relates to oxacyclopentene-2 derivatives as compounds possessing antiinflammatory, neuroprotective, immunomodulatory and cardiovascular activities in mammals.
    Type: Application
    Filed: May 18, 2007
    Publication date: November 20, 2008
    Inventors: Joseph Schwarz, Michael Weisspapir
  • Publication number: 20080167373
    Abstract: The present invention relates to the side chain functionalization of fimbrolides (halogenated 3-alkyl-5-methylene-2(5H)-furanones) and their synthetic analogues, that yields fimbrolides substituted with a halogen, an oxygen or a nitrogen functionality in the alkyl chain, especially fimbrolide alcohols, caboxylate and sulfinate and sulfonate esters, ethers, aldehydes, ketones, acids, amides, nitro derivatives, hydrophobic, hydrophilic and fluorophilic alkyl derivatives and polymers.
    Type: Application
    Filed: March 19, 2008
    Publication date: July 10, 2008
    Applicant: Unisearch Limited, A.C.N.
    Inventors: Roger Read, Naresh Kumar
  • Publication number: 20080139825
    Abstract: There is provided a process for efficiently producing an anti form of an optically active ?-hydroxy-?-aminocarboxylic acid derivative that is useful as an intermediate for pharmaceuticals and agrochemicals. The process for producing optically active ?-hydroxy-?-aminocarboxylic acid derivative of formula (2) or (3) therein R1 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, R2 is substituted or unsubstituted C1-20, alkyl group, or substituted or unsubstituted C4-12 aromatic group, comprising subjecting an ?-aminoacyl acetic acid ester compound of formula (1) wherein R1 and R2 have the same meaning as the above, to hydrogenation by catalytic asymmetric hydrogenation in the presence of an acid by using as a catalyst a rhodium complex containing as a ligand an optically active compound of formula (4), (4?) or (5) characterized in that the hydrogenation is conducted in the presence of an acetic acid salt.
    Type: Application
    Filed: January 12, 2006
    Publication date: June 12, 2008
    Applicant: Nissan Chemical Industrial, Ltd.
    Inventors: Yasumasa Hamada, Kazuishi Makino
  • Publication number: 20080139622
    Abstract: This invention relates to a compound of the following formula: wherein R1, R2, R3, G, and Z are defined herein. It also relates to is methods of treating autoimmune disease, cancer, and atherosclerosis with such a compound.
    Type: Application
    Filed: December 11, 2007
    Publication date: June 12, 2008
    Applicant: Hutchison Medipharma Limited
    Inventors: Tao Wang, Weihan Zhang, Xiaoqiang Yan, Weiguo Su, Jifeng Duan, Yu Cai
  • Patent number: 7365196
    Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: April 29, 2008
    Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.
    Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
  • Patent number: 7208528
    Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinational polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.
    Type: Grant
    Filed: September 15, 1999
    Date of Patent: April 24, 2007
    Assignee: MediQuest Therapeutics, Inc.
    Inventors: Nicolaas M. J. Vermeulin, Christine L. O'Day, Heather K. Webb, Mark R. Burns, Donald E. Bergstrom
  • Patent number: 7192978
    Abstract: New pyrrolidinium derivatives having the chemical structure of general formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors.
    Type: Grant
    Filed: April 11, 2003
    Date of Patent: March 20, 2007
    Assignee: Almirall Prodesfarma AG
    Inventors: Maria Prat Quinones, Maria Dolors Fernandez Forner
  • Patent number: 7160923
    Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinatiorial polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.
    Type: Grant
    Filed: November 14, 2000
    Date of Patent: January 9, 2007
    Assignee: MediQuest Therapeutics, Inc.
    Inventors: Nicolaas M. J. Vermeulin, Christine L. O'Day, Heather K. Webb, Mark R. Burns, Donald E. Bergstrom
  • Patent number: 7132001
    Abstract: The object of the present patent application are 3-aminophenol derivatives of formula (I) or the physiologically compatible, water-soluble salts thereof and colorants based on a developer-coupler combination containing these compounds.
    Type: Grant
    Filed: January 8, 2003
    Date of Patent: November 7, 2006
    Assignee: Wella AG
    Inventors: Gisela Umbricht, Franco Jose Rosato, Hans-Juergen Braun
  • Patent number: 7128764
    Abstract: The object of the present patent application are 3-aminophenol derivatives of formula (I) or the physiologically tolerated, water-soluble salts thereof wherein R denotes a heterocyclic aromatic 5-membered ring of formula (Ia) and colorants based on a developer-coupler combination and containing these compounds.
    Type: Grant
    Filed: April 24, 2002
    Date of Patent: October 31, 2006
    Assignee: Wella AG
    Inventors: Cècile Pasquier, Patrick Wyss, Hans-Juergen Braun
  • Patent number: 7122061
    Abstract: The present invention has for an object compounds of formula (I) and colorants containing these 4-aminobiphenyl-3-ol derivatives of general formula (I) for dyeing keratin fibers, particularly hair, wherein R1 and R2 independently of each other denote hydrogen, a halogen atom, a cyano group, a hydroxyl group, a C1–C4-alkoxy group, a C2–C4-hydroxyalkoxy group, a C1–C6-alkyl group, a nitro group, a trifluoromethyl group, a —C(O)H group, a —C(O)CH3 group, a —C(O)CF3 group, an —Si(CH3)3 group or a C1–6-hydroxyalkyl group or R1 and R2 together form an —O—CH2—O— bridge.
    Type: Grant
    Filed: May 13, 2003
    Date of Patent: October 17, 2006
    Assignee: Wella AG
    Inventors: Laurent Chassot, Hans-Juergen Braun
  • Patent number: 7019024
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: March 28, 2006
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Patent number: 6960688
    Abstract: The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R1 is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described.
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: November 1, 2005
    Assignee: AstraZeneca AB
    Inventors: Roger J Butlin, Thorsten Nowak, Jeremy N Burrows, Michael H Block
  • Patent number: 6878742
    Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof.
    Type: Grant
    Filed: June 5, 2003
    Date of Patent: April 12, 2005
    Assignees: Wyeth, ArQule, Inc.
    Inventors: Anthony F. Kreft, Derek C. Cole, Kevin R. Woller, Joseph R. Stock, George Diamantidis, Dennis M. Kubrak, Kristina M. Kutterer, William J. Moore, David S. Casebier
  • Patent number: 6849660
    Abstract: Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1? is —C(O)NR5R5?, —C(O)—Q—NR5R5?, —CH2NR5R5? or —S(O)2NR5R5? and the other is H or R3. One of R2 and R2? is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5? or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5? is H or R5 and R5? together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide.
    Type: Grant
    Filed: August 1, 2000
    Date of Patent: February 1, 2005
    Assignee: ISIS Pharmaceuticals, Inc.
    Inventors: Elizabeth Jefferson, Eric Swayze
  • Patent number: 6844452
    Abstract: A process for the co-production of a diol product (e.g. butane-1,4-diol) and a cyclic ether (e.g. tetrahydrofuran) by hydrogenation of an aliphatic diester or lactone feedstock (e.g. dimethyl or diethyl maleate), which contains a minor amount of acidic material, such as the corresponding monoester. The process utilizes a plurality of hydrogenation zones connected in series, each containing a charge of a granular ester hydrogenation catalyst. The catalyst in the first hydrogenation zone is tolerant of a minor amount of acidic material, while the catalyst in the second hydrogenation zone provides enhanced yields of cyclic ethers compared to the catalyst of the first hydrogenation zone. The catalyst in a third hydrogenation zone exhibits low selectivity towards conversion of the diester to at least one by product (e.g. 2-4?-hydroxybutoxy-tetrahydrofuran).
    Type: Grant
    Filed: December 12, 2000
    Date of Patent: January 18, 2005
    Assignee: Davy Process Technology Ltd.
    Inventors: Michael Anthony Wood, Paul Willett, Robert Wild, Stephen William Colley
  • Patent number: 6840965
    Abstract: The object of the invention are p-aminophenol derivatives of general formula (I) or physiologically tolerated, water-soluble salts thereof and oxidative coloring preparations based on a developer-coupler combination containing at least one p-aminophenol derivative of formula (I).
    Type: Grant
    Filed: March 9, 2001
    Date of Patent: January 11, 2005
    Assignee: Wella Aktiengesellschaft
    Inventors: Laurent Chassot, Hans-Juergen Braun
  • Patent number: 6824805
    Abstract: This invention pertains to a method for flavoring an ingestible composition with a flavoring agent, furfuryl propyl disulfide, in organoleptically purified form, unaccompanied by substances of natural origin present in cooked beef and onions. The flavoring agent may be used in a wide variety of ingestible vehicles to augment or enhance the aroma or taste of foodstuffs, particularly roasted nut, roasted meat, beef broth, black pepper, onion, fine herbs, omelet, and cooked onion omelet flavored foodstuffs. The present invention also pertains to an ingestible composition comprising an ingestible vehicle and an organoleptically effective amount of the purified flavoring agent. The present invention also pertains to furfuryl propyl disulfide represented by the formula, (2-Furan-CH2SSCH2CH2CH3), in purified form, unaccompanied by substances of natural origin present in cooked beef and onions, and to methods for preparing furfuryl propyl disulfide.
    Type: Grant
    Filed: January 4, 2002
    Date of Patent: November 30, 2004
    Assignee: Bush Boake Allen Ltd.
    Inventors: Ronald Louis Belanger, Benjamin Owen Isaac, Anne-Dominique Fortineau
  • Publication number: 20040230066
    Abstract: Citalopram can be industrially and economically produced and at a high yield by reacting a compound of the following formula [VI] with 3-(dimethylamino)propyl chloride in the presence of at least one of N,N,N′,N′-tetramethylethylenediamine and 1,3-dimethyl-2-imidazolidinone and a condensing agent. The compound of the following formula [III], which is a key compound for the production of citalopram, can be easily produced by subjecting the compound of the following formula [II] to reduction and cyclization.
    Type: Application
    Filed: June 14, 2004
    Publication date: November 18, 2004
    Applicant: Sumika Fine Chemicals Co., Ltd.
    Inventors: Tetsuya Ikemoto, Wei-Guo Gao, Masami Igi
  • Patent number: 6790866
    Abstract: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is —COR1, —CH═CH—COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4). The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.
    Type: Grant
    Filed: July 30, 2002
    Date of Patent: September 14, 2004
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Shuichi Ohuchida, Yuuki Nagao
  • Patent number: 6770764
    Abstract: A compound of the formula (I) wherein R1 is a protecting group for N&agr;, R2 is a protecting group for NG, and R3 is aryl, and wherein the compound of formula (I) is a trypsin substrate such that trypsin cleaves the O—C single bond, which liberates R3—OH; a diagnostic device comprising same; a method for preparing the diagnostic device; and a method of using the diagnostic device to detect levels of urinary trypsin inhibitor in a biological sample; and a diagnostic kit for detecting levels of urinary trypsin inhibitor in a biological sample.
    Type: Grant
    Filed: April 30, 2001
    Date of Patent: August 3, 2004
    Assignee: Bayer Corporation
    Inventors: Paul F. Corey, Steven W. Felman, Gary E. Rehm, Michael J. Pugia
  • Patent number: 6720433
    Abstract: Ethylamine derivatives that function as a motilin receptor antagonist and are useful as medicines are represented by the general formula (1): wherein R1 represents a phenyl group or the like, R2 represents a hydrogen atom and the like, R3 represents a hydrogen atom and the like, R4 represents a hydrogen atom and the like, R5 represents an alkyl group and the like, R7 represents a hydrogen atom and the like and R8 represents a heterocyclic ring and the like; or a hydrate or pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 3, 2003
    Date of Patent: April 13, 2004
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroharu Matsuoka, Tsutomu Sato
  • Patent number: 6696472
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenoxy-N-phenyl aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: February 24, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6673784
    Abstract: A class of compounds is described which can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula II wherein each of R1, R2, and R3 is independently selected from hydrido, halo, and nitro; wherein R8 is selected from haloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted arylalkoxy and optionally substituted aryloxyalkyl; where Y is selected from fluoroalkyl, and wherein R9 alkylamino; or a pharmaceutically-acceptable salt or tautomer thereof.
    Type: Grant
    Filed: November 14, 2000
    Date of Patent: January 6, 2004
    Assignee: G. D. Searle & Co.
    Inventors: Daniel L. Flynn, Jeffery Zablocki, Kenneth Williams, Susan L. Hockerman
  • Patent number: 6627652
    Abstract: Process of treatment of mammals, including humans to treat diseases or conditions of the type which are normally treated with retinoid-like compounds is disclosed, with pharmaceutical compositions containing an active compound which is a selective agonist of the RXR retinoid receptor sites in preference to the RAR retinoid receptor sites. A compound is defined to be a selective agonist of the RXR receptor site if the compound is at least approximately ten times more effective as an agonist in the RXR receptor sites than in the RAR receptor sites.
    Type: Grant
    Filed: April 20, 1995
    Date of Patent: September 30, 2003
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 6586630
    Abstract: The object of the present invention is to provide ethylamine derivatives that function as a motilin receptor antagonist and that are useful as medicines. The invention provides compounds represented by the general formula (1): wherein R1 represents a phenyl group or the like, R2 represents a hydrogen atom and the like, R3 represents a hydrogen atom and the like, R4 represents a hydrogen atom and the like, R5 represents an alkyl group and the like, R7 represents a hydrogen atom and the like and R8 represents a heterocyclic ring and the like; or a hydrate or pharmaceutically acceptable salt thereof and a medicine which comprises the above compound or a hydrate or pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 21, 2001
    Date of Patent: July 1, 2003
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroharu Matsuoka, Tsutomu Sato
  • Patent number: 6573398
    Abstract: New secondary amines are described which are prepared from inexpensive, commercially available raw materials, are stable at room temperature, and are reactive toward electrophiles. The secondary amines are prepared by the addition of one or more primary amines with one or more male (amide/ester) and fumar (amide/ester) Michael receptors. The above amines can be used as coreactants with aliphatic polyisocyanates for polyurea coatings. The novel secondary amines are also described as particularly useful as part of a two-part liquid pavement marking composition for pavement markings.
    Type: Grant
    Filed: July 22, 2002
    Date of Patent: June 3, 2003
    Assignee: 3M Innovative Properties Company
    Inventors: Richard G. Hansen, Dean M. Moren, Mark D. Purgett
  • Patent number: 6545154
    Abstract: The invention relates to a process for preparing N-(5-amino-2-cyano-4-fluoro-phenyl)-sulphonamides in which, in a first step, 2-amino-4,5-difluoro-benzonitrile is reacted with sulphonyl halides in the presence of an acid acceptor and in the presence of a diluent at temperatures between 0° C. and 150° C. and, in a second step, the N-(2-cyano-4,5-difluoro-phenyl)-sulphonamides and/or N-(2-cyano-4,5-difluoro-phenyl)-sulphonimides obtained in the first step are as pure substances or as mixtures with ammonia in the presence of a diluent reacted at a temperature between 100° C. and 200° C. The invention furthermore relates to novel intermediates of the process.
    Type: Grant
    Filed: September 5, 2001
    Date of Patent: April 8, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Achim Hupperts, Mark Wilhelm Drewes, David Erdman, Reinhard Lantzsch
  • Patent number: 6492416
    Abstract: The present invention provides a novel class of 4,5-diaryl-3(2H)-furanone derivatives, which inhibit strongly and selectively COX-2 over COX-1. They are useful to treat inflammation, inflammation-associated disorders, and COX-2 mediated diseases.
    Type: Grant
    Filed: November 27, 2001
    Date of Patent: December 10, 2002
    Assignee: Pacific Corporation
    Inventors: Song Seok Shin, Min-Soo Noh, Young Joo Byun, Jin Kyu Choi, Jin Kwan Kim, Kyung Min Lim, Ji Young Kim, Young Hoon Choi, Jun-Yong Ha, Ki-Wha Lee, Joo Hyun Moh, Yeon Su Jeong, Shin Chung, Yung Hyup Joo, Chang Hoon Lee, Seon Hwa Kang, Young-Ho Park, Jung Bum Yi
  • Patent number: 6485886
    Abstract: New oxime derivatives of formula (I) or. (II), wherein m is 0 or 1; R1 inter alia is phenyl, naphthyl, anthracyl, phenanthryl or a heteroaryl radical; R′1 is for example C2-C12alkylene, phenylene, naphthylene; R2 is CN; R3 is C2-C6haloalkanoyl, halobenzoyl, a phosphoryl or an organosilyl group; R4, R5, R10 and R11 inter alia are hydrogen, C1-C6alkyl, C1-C6alkoxy; R6 inter alia is hydrogen phenyl, C1-C12alkyl; R7 and R8 inter alia are hydrogen, C1-C12alkyl; or R7 and R8, together with the nitrogen atom to which they are bonded, form a 5-, 6 or 7-membered ring; R9 is for example C1-C12alkyl; and A inter alia is S, O, NR7a; are useful as latent acids, especially in photoresist applications.
    Type: Grant
    Filed: April 24, 2001
    Date of Patent: November 26, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Hitoshi Yamato, Toshikage Asakura, Jean-Luc Birbaum, Kurt Dietliker
  • Patent number: 6482859
    Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are ea
    Type: Grant
    Filed: February 4, 2000
    Date of Patent: November 19, 2002
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Martin Zeller, André Jeanguenat
  • Patent number: RE39530
    Abstract: 3-amino-3-arylpropan-1-ol compounds corresponding to the formula I in which R1 to R5, A and X have the meanings according to claim 1, and their preparation and use as medicaments.
    Type: Grant
    Filed: September 11, 2003
    Date of Patent: March 27, 2007
    Assignee: Gruenenthal GmbH
    Inventors: Bernd Sundermann, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Helmut Buschmann