Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/329)
  • Publication number: 20030229093
    Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.
    Type: Application
    Filed: January 29, 2003
    Publication date: December 11, 2003
    Applicant: Tularik Inc.
    Inventors: Xian Yun Jiao, Frank Kayser, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
  • Patent number: 6660728
    Abstract: The present invention relates to thienyl substituted acylguanidine derivatives, such as compounds of formula (I) in which R1, R2, R4, R6, A, B and D have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the present invention are valuable pharmaceutical active compounds. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts. They are suitable, for example, for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of thienyl substituted acylguanidines, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Grant
    Filed: November 14, 2002
    Date of Patent: December 9, 2003
    Assignees: Aventis Pharma Deutschland GmbH, Genentech, Inc.
    Inventors: Karl-Heinz Scheunemann, Jochen Knolle, Amuschirwan Peyman, David William Will, Denis Carniato, Jean-Francois Gourvest, Thomas Gadek, Robert McDowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson
  • Publication number: 20030225088
    Abstract: The invention relates to substituted aromatic polycyclic 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.
    Type: Application
    Filed: September 26, 2002
    Publication date: December 4, 2003
    Applicant: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Mark A. Massa, Jane L. Wang, Deborah A. Mischke, Barry L. Parnas, Melvin L. Rueppel
  • Patent number: 6656958
    Abstract: The present invention is directed to a series of substituted pyridine compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions containing these compounds. Preferred compounds are 3′-(5′- and/or 6′-substituted) pyridyl ethers.
    Type: Grant
    Filed: February 1, 2001
    Date of Patent: December 2, 2003
    Assignee: Abbott Laboratories
    Inventors: Nan-Horng Lin, Liming Dong
  • Patent number: 6657065
    Abstract: The present invention relates to methods of making quinoline amides of Formula I below, which are microsomal triglyceride transfer protein inhibitors and can be used as medicines. The present invention also relates to compounds that are used to make quinoline amides of Formula I and methods of making these compounds.
    Type: Grant
    Filed: April 23, 2002
    Date of Patent: December 2, 2003
    Assignee: Pfizer Inc
    Inventors: Norma J. Tom, David C. Whritenour
  • Publication number: 20030216393
    Abstract: Substituted 1-aminobutane-3-ol compounds, methods for producing them, pharmaceutical compounds containing them, and the use of substituted 1-aminobutane-3-ol compounds for producing pharmaceutical compounds.
    Type: Application
    Filed: March 28, 2003
    Publication date: November 20, 2003
    Applicant: Gruenenthal GmbH
    Inventors: Helmut Buschmann, Corinna Maul, Bernd Sundermann, Utz-Peter Jagusch, Michael Haurand, Boris Chizh
  • Patent number: 6649616
    Abstract: The present invention relates to substituted phenylcyclohexanecarboxamides of the formula (I) to processes for their preparation and to their use in medicaments, in particular for the prevention and/or treatment of cardiovascular disorders.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: November 18, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Erwin Bischoff, Thomas Krahn, Stephan-Nicholas Müller, Holger Paulsen, Joachim Schuhmacher, Henning Steinhagen, Wolfgang Thielemann
  • Patent number: 6649633
    Abstract: This application is directed to compounds useful as inhibitors at PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis and chronic obstructuive pulmonary disease, of the formula: where j is 0 or 1 provided that when j is 0, n must be 2; k is 0 or 1; m is 0, 1, or 2; n is 1 or 2; W1 is —O—; or —S(═O)t—, where t is 0, 1, or 2; Y is —C(R1a); Q1 is phenyl or substituted phenyl; Q2 is biphenyl or substituted biphenyl; and the remaining variables are defined as set forth in the specification. This application is also directed to pharmaceutical compositions comprising those compounds and to methods of treating diseases regulated by the activation and degranulation of eosinophils, in particular asthma, chronic bronchitis and chronic obstructive pulmonary disease.
    Type: Grant
    Filed: January 31, 2002
    Date of Patent: November 18, 2003
    Assignee: Pfizer Inc
    Inventors: Robert J. Chambers, Anthony Marfat, Thomas V. Magee
  • Publication number: 20030203906
    Abstract: The present invention relates to novel substituted diamine derivatives for the formula 1
    Type: Application
    Filed: November 8, 2002
    Publication date: October 30, 2003
    Inventors: Sigmong G. Johnson, Ralph A. Rivero
  • Patent number: 6638940
    Abstract: Compounds of formula are described, wherein R1 and R2 are for example, independently of each other, halogen, C1-C6-alkyl, C3-C6-cycloalkyl, halogen-C1-C6-alkyl, halogen-C3-C6-cycloalkyl, C2-C4-alkenyl, C2-C4-alkinyl, halogen-C2-C4-alkenyl and halogen-C2-C4-alkinyl; R3 is hydrogen, OH, halogen, C1-C6-alkoxy, or —O—C(═O)—C1-C6-alkyl; R4 is for example phenyl, benzyl, phenoxy or benzyloxy, which is substituted by substituents selected from the group consisting of halogen, cyano, NO2, C1-C6-alkyl, C3-C8-cycloalkyl, C3-C8-cyclalkyl-C1-C6-alkyl, halogen-C1-C6-alkyl, C1-C6-alkoxy, C3-C8-cycloalkoxy, C3-C8-cycloalkoxy-C1-C6-alkyl, C3-C8-cycloalkoxy-C1-C6-alkoxy, halogen-C1-C6-alkoxy, C2-C4-alkenyl, C2-C4-alkinyl, halogen-C2-C4-alkenyl, halogen-C2-C4-alkinyl, C2-C6-alkenyloxy, C2-C6-alkinyloxy, halogen-C2-C6-alkenyloxy, halogen-C2-C6-alkenyloxy, —NR6—C(═O)—O—C1-C6-alkyl, —NR6—C(═O)—O-halogen-C1-C6-alkyl, —C(R7)═N&
    Type: Grant
    Filed: February 25, 2002
    Date of Patent: October 28, 2003
    Assignee: Syngenta Crop Protection, Inc.
    Inventor: Stephan Trah
  • Patent number: 6638962
    Abstract: Compound of formula (I): wherein: X represents a bond or alkylene, CO, S(O)n, —S(O)n—A1—, —CO—A1—, —A—S(O)n—A′1— or —A1—CO—A′1—, Y represents aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, R1, R2, R3 and R4 each independently of the others represent hydrogen or aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, or R1, R2, R3 and R4, taken in pairs, together form a bond, or form a fused benzene ring or a fused aromatic or partially unsaturated heterocycle, T represents —CH(R5)—, —N(R5)— or —N(R5)CO—, V represents hydrogen or unsubstituted or substituted aryl or heteroaryl, A2 represents [C(R6)(R′6)]p, R7 and R8 are as defined in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing t
    Type: Grant
    Filed: January 16, 2002
    Date of Patent: October 28, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Patrick Casara, Thierry Le Diguarher, Gilbert Dorey, John Hickman, Alain Pierre, Gordon Tucker, Nicolas Guilbaud
  • Patent number: 6635641
    Abstract: Amide compounds represented by the formula: wherein: R1 is a moiety represented by the formula  where X is selected from the group consisting of CH2, O, S, and NH; and Y is selected from the group consisting of CH2, O, and S, provided that at least one of X and Y is CH2, or X and Y together with the bond there-between form a cyclopropyl; are described. These compounds and pharmaceutical compositions containing them modulate and/or inhibit the activity of certain protein kinases and are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation.
    Type: Grant
    Filed: January 19, 2001
    Date of Patent: October 21, 2003
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Steven Lee Bender, Dilip Bhumralkar, Michael Raymond Collins, Stephen James Cripps, Judith Gail Deal, Lei Jia, Mitchell David Nambu, Cynthia Louise Palmer, Zhengwei Peng, Michael David Varney
  • Patent number: 6632823
    Abstract: In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: October 14, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Jean-Michel Vernier, Nicholas D. P. Cosford, Ian A. McDonald
  • Publication number: 20030191306
    Abstract: The invention relates to substituted N-Aliphatic-N-Aromatic 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, dyslipidemia, and other coronary artery disease.
    Type: Application
    Filed: December 16, 2002
    Publication date: October 9, 2003
    Applicant: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Deborah A. Mischke, Emily J. Reinhard, Barry L. Parnas, Melvin L. Rueppel
  • Publication number: 20030191316
    Abstract: This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); 1
    Type: Application
    Filed: January 10, 2003
    Publication date: October 9, 2003
    Inventors: Yoshio Ogino, Hideki Kurihara, Kenji Matsuda, Tomoshige Numazawa, Norikazu Otake, Kazuhito Noguchi
  • Publication number: 20030187033
    Abstract: The present invention is related to anthranilamides of formula I, 1
    Type: Application
    Filed: April 26, 2002
    Publication date: October 2, 2003
    Inventors: Joachim Brendel, Bernard Pirard, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
  • Publication number: 20030186985
    Abstract: To provide a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the prevention or treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.
    Type: Application
    Filed: December 27, 2002
    Publication date: October 2, 2003
    Inventors: Yu Momose, Hiroyuki Odaka, Hiroshi Imoto, Hiroyuki Kimura, Junichi Sakamoto
  • Publication number: 20030181489
    Abstract: In one aspect, the present invention concerns the use of certain quaternary ammonium compounds as active ingredient in the manufacture of a medicament for use in the treatment and/or prevention of cough in warm-blooded animals, including humans, such as compounds of formula Y—J—E An− (I), wherein J is independently selected from a group represented by one of formulae (II), (III) and (IV).
    Type: Application
    Filed: February 14, 2003
    Publication date: September 25, 2003
    Inventors: Lewis Siu Leung Choi, Gregory N Beatch, Clive Page
  • Publication number: 20030181726
    Abstract: This invention relates to new aminoalcohol derivatives or salts thereof represented by the following formula [I]: 1
    Type: Application
    Filed: March 4, 2003
    Publication date: September 25, 2003
    Applicant: Fujisawa Pharmaceutical Co. Ltd.
    Inventors: Kiyoshi Taniguchi, Naoaki Fujii, Minoru Sakurai, Yasuyo Tomishima, Hisashi Takasugi
  • Publication number: 20030181491
    Abstract: The present invention is directed to C2-disubstituted indan-1-ol systems of the Formula I, 1
    Type: Application
    Filed: August 29, 2002
    Publication date: September 25, 2003
    Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
  • Publication number: 20030176707
    Abstract: A novel process is provided for the preparation of 2,5-di-(3′-aminopropyl)pyridine which is useful in the synthesis of &agr;v&bgr;3 integrin receptor antagonists. Also provided are useful intermediates obtained from the process.
    Type: Application
    Filed: January 29, 2003
    Publication date: September 18, 2003
    Inventor: Philip J. Pye
  • Publication number: 20030171592
    Abstract: A process for producing an optically active amino alcohol is provided that includes a step in which a nitro ketone or a cyano ketone is reacted with a hydrogen-donating organic or inorganic compound in the presence of a transition metal compound catalyst having an optically active nitrogen-containing compound as an asymmetric ligand to give an optically active nitro alcohol or an optically active cyano alcohol, and a step in which the above optically active alcohol is further reduced to efficiently produce an optically active amino alcohol.
    Type: Application
    Filed: October 31, 2002
    Publication date: September 11, 2003
    Inventors: Masahito Watanabe, Kunihiko Murata, Takao Ikariya
  • Publication number: 20030171410
    Abstract: Compounds of formula (I) and salts thereof as phytopathogenic fungicides wherein A1 is substituted 2-pyridyl; A2 is optionally substituted phenyl; L is —(C═O)—, —SO2— or —(C═S)—; R1 is hydrogen, optionally substituted alkyl or acyl; and R2 is hydrogen or optionally substituted alkyl are useful phytopathogenic fungicides.
    Type: Application
    Filed: November 25, 2002
    Publication date: September 11, 2003
    Applicant: Aventis CropScience UK Limited
    Inventors: Brian Anthony Moloney, David Hardy, Elizabeth Anne Saville-Stones
  • Publication number: 20030171341
    Abstract: Compounds of formula 1 modulate the activity of Rho C: 1
    Type: Application
    Filed: November 19, 2002
    Publication date: September 11, 2003
    Inventors: Dongxu Sun, Edward L. Perkins, Stuart Tugendreich
  • Publication number: 20030158152
    Abstract: The present invention refers to synthetic protease inhibitors having an axis of symmetry C2 or pseudo-C2 characterised by possessing, in the central portion: (1) preferably, a dihydroxyethylene function, which is isosteric with a peptidic bond; (2) a peptidemimetic bridge between the two nitrogens of the main chain and (3) radicals capable of mimetising amino acids. These new protease inhibitors are a base for the preparation of anti-viral formulations capable of inhibiting HIV virus proliferation.
    Type: Application
    Filed: November 15, 2002
    Publication date: August 21, 2003
    Inventors: Emerson Poley Pecanha, Luciana J.O. Figueiredo, Vera Bongertz, Octavio Augusto Ceva Antunes, Amilcar Tanuri, Rodrigo de Moraes Brindeiro
  • Publication number: 20030153609
    Abstract: The present invention is directed C2-disubstituted indan-1-ones of the Formula I, 1
    Type: Application
    Filed: August 29, 2002
    Publication date: August 14, 2003
    Applicant: Aventis Pharma Dutschlan GmbH.
    Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
  • Publication number: 20030149005
    Abstract: The present invention provides novel C24-aryl sulfone analogs of 1&agr;,25-dihydroxy vitamin D3, compositions comprising these compounds and methods of using these compounds as selective inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseases which benefit from a modulation of the levels of 1&agr;,25-dihydroxy vitamin D3, for example, cell-proliferative disorders.
    Type: Application
    Filed: August 22, 2002
    Publication date: August 7, 2003
    Inventors: Gary H. Posner, Kenneth R. Crawford, Hong Woon Yang, Jay A. White, Glenville Jones, Byung-Chul Suh, HeungBae Jeon, Mark Hatcher
  • Patent number: 6603011
    Abstract: Patients susceptible to or suffering from central nervous system disorders are treated by administering effective amounts of aryl substituted aliphatic amine compounds, aryl substituted olefinic amine compounds or aryl substituted acetylenic amine compounds. A representative compound is (E)-N-methyl-5-(3-pyridinyl)-4-penten-2-amine.
    Type: Grant
    Filed: August 21, 2000
    Date of Patent: August 5, 2003
    Assignee: Targacept, Inc.
    Inventors: William Scott Caldwell, Gary Maurice Dull, Grayland Page Dobson
  • Publication number: 20030144526
    Abstract: A novel calcium receptor active compound having the formula is provided:
    Type: Application
    Filed: December 19, 2002
    Publication date: July 31, 2003
    Applicant: NPS Pharmaceuticals, Inc.
    Inventors: Teruyuki Sakai, Atsuya Takami, Rika Nagao
  • Publication number: 20030144514
    Abstract: Non-symmetrical ligands of formula (I); 1
    Type: Application
    Filed: December 16, 2002
    Publication date: July 31, 2003
    Inventors: Eric Johannes Maria De Boer, Henderikus Hyacinthus Deuling, Harry Van Der Heijden, Nicolaas Meijboom, Aart Bartus Van Oort, Arie Van Zon
  • Publication number: 20030144542
    Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.
    Type: Application
    Filed: November 28, 2001
    Publication date: July 31, 2003
    Inventors: Gunnar J. Hanson, John S. Baran
  • Publication number: 20030144217
    Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
    Type: Application
    Filed: August 21, 2002
    Publication date: July 31, 2003
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Roger D. Tung, Michael R. Hale, Christopher T. Baker, Andrew Spaltenstein, Eric S. Furfine, Istvan Kaldor, Wieslaw M. Kazmierski
  • Publication number: 20030144525
    Abstract: The present invention relates to compounds of formulae 1
    Type: Application
    Filed: October 21, 2002
    Publication date: July 31, 2003
    Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Emmanuel Pinard, Rene Wyler
  • Publication number: 20030139418
    Abstract: Compounds of the formula I; 1
    Type: Application
    Filed: October 31, 2002
    Publication date: July 24, 2003
    Inventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
  • Publication number: 20030139457
    Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.
    Type: Application
    Filed: September 17, 2002
    Publication date: July 24, 2003
    Applicant: Curis, Inc.
    Inventors: Anthony David Baxter, Edward Andrew Boyd, Maria Frank-Kamenetsky, Oivin Guicherit, Jeffery Porter, Stephen Price, Lee Rubin, John Harry Alexander Stibbard
  • Publication number: 20030138664
    Abstract: A light emitting device material comprising a compound represented by the following formula (I): 1
    Type: Application
    Filed: December 3, 2002
    Publication date: July 24, 2003
    Applicant: FUJI PHOTO FILM CO., LTD.
    Inventor: Kazumi Nii
  • Publication number: 20030134148
    Abstract: Disclosed is a novel methine compound, for examples, which is represented by the following formula (I): 1
    Type: Application
    Filed: November 8, 2002
    Publication date: July 17, 2003
    Applicant: FUJI PHOTO FILM CO., LTD.
    Inventors: Hisashi Okada, Terukazu Yanagi
  • Publication number: 20030135052
    Abstract: Disclosed is a method for preparing tertiary amine compounds from primary amines and nitrites in the presence of hydrogen gas and a metal catalyst, or metal-containing catalyst composition, at a temperature from about 50° C. to about 200° C. and at a pressure from about 100 psig to 1500 psig. The primary amines and the nitrites used in the process may be diamines and/or dinitriles, or may be combinations of primary amines and/or nitrites. Also disclosed are novel tertiary amine compounds made by the described method.
    Type: Application
    Filed: November 13, 2001
    Publication date: July 17, 2003
    Inventors: Kelley Moran Whittle, Alan Martin Allgeier, THOMAS PAPIN GANNETT, DAVID PAGE HIGLEY
  • Publication number: 20030135066
    Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.
    Type: Application
    Filed: November 28, 2001
    Publication date: July 17, 2003
    Inventors: Gunnar J. Hanson, Baran S. John
  • Patent number: 6593340
    Abstract: The present invention relates to N-propargylphentermine and its derivatives and the neuroprotective and anti-depressant activity of such compounds as well as therapeutic methods for such compounds.
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: July 15, 2003
    Assignee: CV Technologies, Inc.
    Inventors: Brian D. Sloley, Liana Urichuk, Lei Ling, Glen Baker, Ronald Coutts, Jacqueline Shan
  • Publication number: 20030130522
    Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.
    Type: Application
    Filed: November 28, 2001
    Publication date: July 10, 2003
    Inventors: Gunnar J. Hanson, John S. Baran
  • Publication number: 20030125563
    Abstract: One aspect of the present invention relates to methods for the transition-metal-catalyzed asymmetric 1,4-addition of a nucleophile, e.g., hydride, to cyclic and acyclic enoates and enones. In certain embodiments of the methods of the present invention, the transition metal catalyst consists essentially of copper and an asymmetric bidentate bisphosphine ligand.
    Type: Application
    Filed: October 15, 2002
    Publication date: July 3, 2003
    Inventors: Stephen L. Buchwald, Daniel H. Appella, Yasunori Moritani, Ryo Shintani, Valdas Jurkauskas
  • Publication number: 20030125328
    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.
    Type: Application
    Filed: May 23, 2002
    Publication date: July 3, 2003
    Applicant: G.D. Searle & Co.
    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
  • Publication number: 20030119877
    Abstract: A compound of the formula (I), wherein R1 is hydrogen, halogen, carbymoyl, cyano, formuly, or lower alkyl optionally substituted with halogen, amino or a protected amino, R2 is hydrogen, halogen, cyano or lower alkoxy, R3 is phenyl or pyridyl, each of which is substituted with lower alkoxy, and R4 is lower alkoxy; provided that either R1 or R2 is hydrogen, then the other is other than hydrogen, or its salts, which are useful as a medicament.
    Type: Application
    Filed: August 16, 2002
    Publication date: June 26, 2003
    Inventors: Junya Ishida, Hirofumi Yamamoto, Nobukiyo Konishi, Masataka Morita, Katsuya Nakamura, Susumu Miyata, Takehiro Ochi, Yoshiaki Morita, Eiji Yoshimi, Kanae Kuroda
  • Publication number: 20030119721
    Abstract: A class of compounds is described which can be used for the treatment of viral infections.
    Type: Application
    Filed: November 25, 2002
    Publication date: June 26, 2003
    Applicant: G. D. Searle & Co., Corporate Patent Department
    Inventors: Daniel L. Flynn, Jeffery Zablocki, Kenneth Williams, Susan L. Hockerman
  • Patent number: 6583182
    Abstract: This invention involves synthesis and use of a class of compounds with chelation affinity and selectivity for first transition series elements. Administration of the free or conjugated compound, or physiological salts of the free or conjugated compound, results in decrease in the in vivo bioavailability of first transition series elements and/or removal from the body of first transition series elements and elements with similar chemical properties. These characteristics make such compounds useful in the management of diseases associated with a bodily excess of first transition series elements and elements with similar chemical properties. This invention demonstrates that such compounds inhibit mammalian, bacterial, and fungal cell replication and are therefore useful in the treatment of neoplasia, infection, inflammation, immune reponse, and in termination of pregnancy.
    Type: Grant
    Filed: November 30, 2001
    Date of Patent: June 24, 2003
    Assignee: Chelator LLC
    Inventors: Harry S Winchell, Joseph Y Klein, Elliot D Simhon, Rosa L Cyjon, Ofer Klein, Haim Zaklad
  • Publication number: 20030114499
    Abstract: This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them.
    Type: Application
    Filed: June 12, 2002
    Publication date: June 19, 2003
    Inventors: Joachim Brendel, Thomas Bohme, Stefan Peukert, Heinz-Werner Kleemann
  • Publication number: 20030109459
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: April 5, 2002
    Publication date: June 12, 2003
    Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achytharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
  • Publication number: 20030109560
    Abstract: Novel compounds of general formula (I), the use of these compounds as medicaments, pharmaceuticaly compositions comprising the compounds and methods of treatment employing these compounds and compostiones. The present compounds may be useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). The compounds exert their effects by modulating the PPAR&ggr; response in a partial agonist manner.
    Type: Application
    Filed: July 29, 2002
    Publication date: June 12, 2003
    Inventors: Lone Jeppesen, Paul Stanley Bury, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
  • Publication number: 20030109758
    Abstract: The present invention relates to a continuous process for the selective hydrogenation of olefinically unsaturated carbonyl compounds to give unsaturated alcohols in particular of citral to give a mixture of geraniol and nerol, in a reactor containing a liquid phase, in which at least one catalyst is suspended, and which can additionally contain a gas phase, wherein the liquid phase and, if present, the gas phase are passed through a device in the reactor having openings or channels.
    Type: Application
    Filed: December 4, 2002
    Publication date: June 12, 2003
    Inventors: Hans-Georg Gobbel, Till Gerlach, Frank Funke, Klaus Ebel, Signe Unverricht, Gerd Kaibel