1,3,4-thiadiazoles (including Hydrogenated) Patents (Class 548/136)
  • Publication number: 20040214870
    Abstract: The present invention is directed to compounds of formula (I), 1
    Type: Application
    Filed: February 4, 2004
    Publication date: October 28, 2004
    Inventors: Zhili Xin, Gang Liu, Zhonghua Pei, Bruce G. Szczepankiewicz, Michael D. Serby, Hongyu Zhao
  • Publication number: 20040214036
    Abstract: Compounds and compositions are provided that can be used as electron transport agents in organic electronic devices such as organic electroluminescent devices. The compounds are non-polymeric and have an aromatic core conjugated to end capping groups. The aromatic core contains a phenylene group arylene or naphthalene group arylene having a pendant heteroaryl group that includes a —C═N— unit.
    Type: Application
    Filed: April 15, 2003
    Publication date: October 28, 2004
    Applicant: 3M Innovative Properties Company
    Inventors: James G. Bentsen, Nicholas P. Goplen, Yingbo Li, Ralph R. Roberts
  • Patent number: 6809113
    Abstract: Compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection; pharmaceutical compositions comprising these compounds; and the use of these compounds and compositions in the prevention or treatment of such diseases.
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: October 26, 2004
    Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co.
    Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
  • Patent number: 6797723
    Abstract: The invention relates to novel heterocycle substituted diphenyl leukotriene B4 (LTB4) antagonists, to compositions containing such compounds, and to methods of using such compounds for treatment of inflammatory diseases.
    Type: Grant
    Filed: April 24, 2002
    Date of Patent: September 28, 2004
    Assignee: Eli Lilly and Company
    Inventors: Jason Scott Sawyer, Douglas Wade Beight, Edward C R Smith, William Thomas McMillen
  • Patent number: 6794518
    Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: September 21, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Milind Rajopadhye, Thomas D. Harris, Edward H. Cheesman
  • Patent number: 6780995
    Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.
    Type: Grant
    Filed: November 25, 2002
    Date of Patent: August 24, 2004
    Assignee: Isotechnika Inc.
    Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
  • Patent number: 6777418
    Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.
    Type: Grant
    Filed: October 1, 2001
    Date of Patent: August 17, 2004
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Jean-Marc Lapierre, David Mark Rotstein, Eric Brian Sjogren
  • Patent number: 6746731
    Abstract: The active-matrix display contains a chiral smectic liquid-crystal mixture comprising at least one compound of the formula (I) R1—(A1—M1)a—(A2—M2)b—A3—X—B1—(B2)c—R2  (I). where the symbols are as defined in the description.
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: June 8, 2004
    Assignee: Clariant GmbH
    Inventors: Toshiaki Nonaka, Hans-Rolf Dübal, Rainer Wingen
  • Patent number: 6743817
    Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.
    Type: Grant
    Filed: September 6, 2001
    Date of Patent: June 1, 2004
    Assignee: Neurogen Corporation
    Inventors: George Maynard, LingHong Xie, Stanislaw Rachwal
  • Patent number: 6743811
    Abstract: Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.
    Type: Grant
    Filed: June 27, 2002
    Date of Patent: June 1, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Robert C. Gadwood
  • Patent number: 6740647
    Abstract: Novel five-membered heterocyclic amidines, their preparation and use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and kininogenases such as kallikrein. Pharmaceutical compositions which contain the compounds as active ingredients, and use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory agents.
    Type: Grant
    Filed: June 21, 2000
    Date of Patent: May 25, 2004
    Assignee: Abbott GmbH & Co., KG
    Inventors: Dorit Baucke, Udo Lange, Helmut Mack, Werner Seitz, Hans Wolfgang Höffken, Wilfried Hornberger
  • Publication number: 20040097732
    Abstract: PDF inhibitors and novel methods for their use are provided.
    Type: Application
    Filed: August 28, 2003
    Publication date: May 20, 2004
    Inventors: Kelly M Aubart, Jia-Ning Xiang, Siegfried B Christensen, XIangmin Liao, Maxwell D Cummings
  • Publication number: 20040092747
    Abstract: Amide compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
    Type: Application
    Filed: July 17, 2003
    Publication date: May 13, 2004
    Inventors: Steven Lee Bender, Dilip Bhumaralkar, Michael Raymond Collins, Stephen James Cripps, Judith Gail Deal, Lei Jia, Mitchell David Nambu, Cynthia Louise Palmer, Zhengwei Peng, Michael David Varney
  • Publication number: 20040063673
    Abstract: This invention provides compounds defined by Formula I
    Type: Application
    Filed: August 5, 2003
    Publication date: April 1, 2004
    Inventor: Adam Richard Johnson
  • Publication number: 20040063669
    Abstract: The present invention relates to novel aryl-substituted S(O)m cycles of the formula (I) 1
    Type: Application
    Filed: June 13, 2003
    Publication date: April 1, 2004
    Inventors: Reiner Fischer, Oliver Kretschik, Thomas Schenke, Ralf-Ingo Schenkel, Jurgen Wiedemann, Christoph Erdelen, Peter Losel, Mark Wilhelm Drewes, Dieter Feucht, Wolfram Andersch
  • Patent number: 6713628
    Abstract: There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.N-carboxyanhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.
    Type: Grant
    Filed: November 18, 2002
    Date of Patent: March 30, 2004
    Assignee: Kaneka Corporation
    Inventors: Yasuyoshi Ueda, Koichi Kinoshita, Tadashi Moroshima, Yoshifumi Yanagida, Yoshihide Fuse
  • Patent number: 6706743
    Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.
    Type: Grant
    Filed: March 5, 2003
    Date of Patent: March 16, 2004
    Assignee: Pfizer Inc
    Inventors: Robert F. Day, Jennifer A. Lafontaine
  • Patent number: 6696475
    Abstract: The present invention discloses compounds having the formula wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: February 24, 2004
    Assignee: NeuroSearch A/S
    Inventors: Bjarne H. Dahl, Palle Christophersen
  • Patent number: 6696110
    Abstract: Liquid crystal mixtures comprising at least one of the compounds of formula (I) containing a heterocyclic five-membered ring and with a carbon-carbon double bond in the termninal group are new. RJ=CnH2n+1CH=CHCmH2mZ1; n=1-5; m=0-5; and q=0, 1 or 2; A1 and A2=2,5-disubstituted furan, 2,5-disubstituted thiophene, 2,5-disubstituted oxazole, 2,5-disubstituted thiazole, 2,5-disubstituted 1,3,4-oxadiazole, 2,5-disubstituted 1,3,4-thiadiazole, 1,4-disubstituted benzene, 2,5-disubstituted pyrimidine, 2,5-disubstituted pyridine, 2,6-disubstituted naphthalene; laterally substituted 1,4-disubstituted benzene, laterally substituted 2,5-disubstituted pyrimidine, laterally substituted 2,5-disubstituted pyridine or laterally substituted 2,6-disubstituted naphthalene (lateral substituents=F, Cl, Br or CN); A3=any A1 or 1,4-disubstituted bicyclo(2.2.
    Type: Grant
    Filed: November 26, 2001
    Date of Patent: February 24, 2004
    Assignee: Qinetiq Limited
    Inventors: Rachel P Tuffin, Steven M Kelly, Neil L Campbell, Warren L Duffy, Janine H Wild
  • Patent number: 6686065
    Abstract: Organic materials based on [5] helicenes or dibenzofluorenes are shown to have excellent properties for use in electroluminescent devices, including high stability and efficiency and low excimer formation. The materials may advantageously be adapted to have hole transport or electron transport capabilities in addition to emissive properties.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: February 3, 2004
    Assignee: Canon Kabushiki Kaisha
    Inventor: Jian Ping Chen
  • Publication number: 20040019218
    Abstract: The present invention is directed to a novel process for preparing heteroaryl and unsaturated heterocycloalkylmagnesium reagents that are useful in the synthesis of a variety of pharmaceuticals, in particular certain cysteine protease inhibitors.
    Type: Application
    Filed: April 16, 2003
    Publication date: January 29, 2004
    Applicants: AXYS PHARMACEUTICALS, INC., AVENTIS PHARMACEUTICALS, INC.
    Inventors: Jiayao Li, John O. Link, Colette Colladant
  • Publication number: 20040010011
    Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: 1
    Type: Application
    Filed: February 20, 2003
    Publication date: January 15, 2004
    Inventors: Jean-Louis Assens, Claude Bernhart, Frederique Cabanel-Haudricourt, Dino Nisato
  • Patent number: 6677360
    Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.
    Type: Grant
    Filed: April 6, 2001
    Date of Patent: January 13, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
  • Publication number: 20040006093
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Application
    Filed: March 7, 2003
    Publication date: January 8, 2004
    Inventors: Eugene D. Thorsett, Christopher M. Semko, Michael A. Pleiss, Anthony Kreft, Andrei W. Konradi, Francine S. Grant, Reinhardt Bernhard Baudy, Dimitrios Sarantakis
  • Publication number: 20030229054
    Abstract: Novel amines of formulas 1A and 1B 1
    Type: Application
    Filed: February 14, 2003
    Publication date: December 11, 2003
    Inventors: Thomas Richard Belliotti, Justin Stephen Bryans, Thomas Capiris, David Christopher Horwell, Clare Octavia Kneen, David Juergen Wustrow
  • Publication number: 20030225053
    Abstract: Disclosed are amide compounds of formula(I): 1
    Type: Application
    Filed: April 10, 2003
    Publication date: December 4, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Kevin Chungeng Qian, Gregory Paul Roth, Christopher Ronald Sarko, Alan David Swinamer, Zhaoming Xiong
  • Patent number: 6657064
    Abstract: A novel bicyclic imidazo-5-yl-amine derivative of Formula I, wherein X denotes CR5, N or S, and Y in the case where X denotes S, denotes CR6 or N and in all other cases denotes N, and methods for preparation thereof are disclosed. Also disclosed are methods for treating pain using the compound of Formula I, and pharmaceutical compositions comprising the compound of Formula I.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: December 2, 2003
    Assignee: Gruenenthal GmbH
    Inventors: Matthias Gerlach, Corinna Maul
  • Patent number: 6656911
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.
    Type: Grant
    Filed: April 18, 2002
    Date of Patent: December 2, 2003
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W Spruce
  • Patent number: 6656910
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: December 2, 2003
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Publication number: 20030208073
    Abstract: The invention relates to novel substituted N-aryl nitrogen-containing heterocyclic compounds of the general formula (I) 1
    Type: Application
    Filed: January 29, 2003
    Publication date: November 6, 2003
    Inventors: Karl-Heinz Linker, Kurt Findeisen, Otto Schallner, Andreas Lender, Hans-Joachim Santel, Markus Dollinger, Akihiko Yanagi, Toshio Goto
  • Publication number: 20030207913
    Abstract: The invention provides compounds of Formula I:
    Type: Application
    Filed: November 6, 2002
    Publication date: November 6, 2003
    Inventors: David W. Piotrowski, Jason K. Myers, Bruce N. Rogers, Eric Jon Jacobsen, Alice L. Bodnar, Vincent E. Groppi, Daniel Patrick Walker, Brad A. Acker
  • Publication number: 20030207869
    Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) 1
    Type: Application
    Filed: May 6, 2003
    Publication date: November 6, 2003
    Inventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
  • Publication number: 20030207823
    Abstract: The present invention relates to novel imaging probes and methods for using the probes in diagnostic imaging processes and other imaging processes to determine physiological functions.
    Type: Application
    Filed: April 11, 2003
    Publication date: November 6, 2003
    Inventor: Manssur Yalpani
  • Patent number: 6642180
    Abstract: The present invention relates to novel biphenyl-substituted cyclic ketoenols of the formula (I) in which W represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or halogenoalkoxy, CKE represents one of the groups  in which A, B, D, L, M, Q1, Q2, Q3, Q4, Q5 and Q6 are as defined in the description, to preparation and to their use as pesticides and herbicides.
    Type: Grant
    Filed: January 25, 2002
    Date of Patent: November 4, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht
  • Patent number: 6632775
    Abstract: A herbicidal composition, comprising: (a) at least one arylthiadiazole having the formula (I):  wherein: R represents linear or branched C1-C6 alkyl or haloalkyl; or C3-C5 cycloalkyl or halocycloalkyl; said alkyl, haloalkyl, cycloalkyl or halocycloalkyl being optionally substituted with linear or branched C1-C3 alkyl; X represents halogen; Y represents halogen; linear or branched C1-C4 alkyl or haloalkyl; linear or branched C1-C4 alkoxyl or haloalkoxyl; R1 represents hydrogen or methyl; and (b) one or more herbicidal compounds.
    Type: Grant
    Filed: December 3, 1999
    Date of Patent: October 14, 2003
    Assignee: Isagro Ricerca S.r.L.
    Inventors: Franco Bettarini, Ernesto Signorini, Piero La Porta, Sergio Massimini, Domenico Portoso
  • Publication number: 20030166645
    Abstract: The invention relates to nitrofuran-containing compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making the compounds, and methods for identifying compounds with desired biological activity.
    Type: Application
    Filed: June 25, 2002
    Publication date: September 4, 2003
    Inventors: Paul J. Ala, Jacob J. Clement, Andrew S. Magee, Scott T. Moe, Manuel A. Navia, Aloka Roy
  • Publication number: 20030158194
    Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.
    Type: Application
    Filed: December 10, 2002
    Publication date: August 21, 2003
    Inventor: Pascal Druzgala
  • Patent number: 6608175
    Abstract: Certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases, are prepared in various embodiments using Grignard reagents and alkyllithium reagents and various aldehydes to make oxadiazole, thiadiazole and triazole peptoid alcohols, which are then oxidized to the desired keto products.
    Type: Grant
    Filed: November 16, 2001
    Date of Patent: August 19, 2003
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Patent number: 6605630
    Abstract: The invention concerns a compound of the formula (I): wherein, for example: T is of the formula (IA), (IB), or (IC); R1 is of the formula —NHC(═O)Rb wherein Rb is (1-4C)alkyl; R2 and R3 are hydrogen or fluoro; >A—B— is >C═CH— (but not when T is (IA)) or >CH—CH2—; wherein when T is of the formula (IA) or (IB); R6 is, for example, (1-4C)alkyl; R5 is hydrogen, R10CO—, R10SO2— or R10CS— wherein R10 is, for example, optionally substituted phenyl, or (1-10C)alkyl, or when T is of the formula (IA), (IB); or (IC): R5 and R6 are linked to give a 5- or 6-membered ring which is fused to the ring shown in (IA), (IB), or (IC) so as to give an optionally substituted bicyclic ring; and pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them, and their use as antibacterial agents.
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: August 12, 2003
    Assignee: Syngenta Limited
    Inventor: Michael Barry Gravestock
  • Patent number: 6605631
    Abstract: Compounds of the general formula I where the index and the substituents have the following meanings: n is 0 or 1 to 4; X is O or S; Y is a five-membered heteroaromatic ring; R1 is nitro; cyano; halogen; alkyl; haloalkyl; alkoxy; haloalkoxy; alkylthio; phenyl or phenoxy; R2 is hydrogen; alkyl, alkenyl or alkynyl; or a saturatedy,or unsaturated ring which, in addition to carbon atoms, can also contain hetero atoms as ring members are described.
    Type: Grant
    Filed: September 30, 1999
    Date of Patent: August 12, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Kirstgen, Wassilios Grammenos, Herbert Bayer, Reinhard Doetzer, Hartmann Koenig, Klaus Oberdorf, Hubert Sauter, Horst Wingert, Gisela Lorenz, Eberhard Ammermann, Volker Harries
  • Patent number: 6603013
    Abstract: The present invention relates to a process wherein heterogeneous finely-dispersed palladium catalysts are used in a cross-coupling reaction of alkenyl halides and aryl or heteroaryl boronic acids in the presence of base in an aprotic solvent to produce aryl- or heteroaryl-olefin compounds of Formula I:
    Type: Grant
    Filed: July 16, 2001
    Date of Patent: August 5, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Yongkui Sun, Carl LeBlond, John R. Sowa, Jr.
  • Patent number: 6602827
    Abstract: The invention relates to novel 5-chlorodifluoromethyl-1,3,4-thiadiazol-2-yl-oxyacetanilides of the general formula (I) in which n represents the number 0, 1, 2 or 3, R represents straight-chain or branched alkyl having 1 to 4 carbon atoms, and X represents nitro, cyano, halogen or represents in each case optionally cyano-, halogen- or C1-C4-alkoxy-substituted alkyl, alkoxy, alkylthio, alkylsulphinyl or alkylsulphonyl having in each case 1 to 4 carbon atoms, except for the compounds N-methyl-5-chlorodifluoromethyl-1,3,4-thiadiazol-2-yl-oxyacetanilide, N-ethyl-5-chlorodifluoromethyl-1,3,4-thiadiazol-2-yl-oxyacetanilide, 4-chloro-N-methyl-(5-chlorodifluoromethyl-1,3,4-thiadiazol-2-yl)-oxyacetanilide and 3-trifluoromethyl-N-methyl-(5-chlorodifluoromethyl-1,3,4-thiadiazol-2-yl)-oxyacetanilide, N-i-propyl-5-chlorodifluoromethyl-1,3,4-thiadiazol-2-yl-oxyacetanilide, and 4-fluoro-N-methyl-(5-chlorodifluoromethyl-1,3,4-thiadiazol-2-yl)-oxyacetanilide and 4-fluoro-N-ethyl-(5-chlorodifluoromethyl-1
    Type: Grant
    Filed: January 24, 2002
    Date of Patent: August 5, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Jochem Riebel, Heinz Förster, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Patent number: 6589914
    Abstract: The dihalopropene compounds of the general formula (I) have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.
    Type: Grant
    Filed: March 4, 2002
    Date of Patent: July 8, 2003
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
  • Publication number: 20030109705
    Abstract: Accordingly, the present invention provides a compound of Formula I, or tautomers or isomers thereof, 1
    Type: Application
    Filed: February 27, 2002
    Publication date: June 12, 2003
    Inventor: Jonas Grina
  • Publication number: 20030105279
    Abstract: The present invention is directed to protected amino acid halide monomers and oligomers, and to their use in the efficient sythesis of polyamides. The present invention is further directed to the use of &agr;-haloenamine reagents, which may optionally be immobilized, for the preparation of the amino acid halides.
    Type: Application
    Filed: August 30, 2002
    Publication date: June 5, 2003
    Applicant: Pharmacia Corporation
    Inventor: Dennis P. Phillion
  • Publication number: 20030100558
    Abstract: The present invention relates to 4-aryl triazoles having the formula: 1
    Type: Application
    Filed: April 24, 2002
    Publication date: May 29, 2003
    Inventors: Joshua Spector Tullis, John Charles Van Rens, Michael Philip Clark, Benjamin Eric Blass, Michael George Natchus, Biswanath De
  • Patent number: 6569876
    Abstract: The present invention is directed to novel inhibitors and methods for inhibiting serine elastases. These compounds and methods achieve a novel approach to enzyme inhibition; namely, balanced inhibition of a plurality of serine elastases. Balanced inhibition of a plurality of elastases offers a novel approach to therapeutic treatment of diseases that involve abnormal activities of a plurality of elastases resulting in pathological changes such as occur in inflammatory and vascular conditions. These pathological changes are not limited to the breakdown of elastin but may include the processing of other proteins by serine elastases which in turn results in adverse effects. The opportunity of targeting a plurality of enzymes using single inhibitor offers therapeutic advantages over administering multiple therapeutic against where each agent has a single specificity for an individual target enzyme.
    Type: Grant
    Filed: June 19, 2000
    Date of Patent: May 27, 2003
    Inventor: John C. Cheronis
  • Patent number: 6562816
    Abstract: The invention provides compounds of Formula I: compounds of the Formula I: wherein R1, R2, R4, R6, X, and W are defined herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which &agr;7 is known to be involved.
    Type: Grant
    Filed: August 14, 2002
    Date of Patent: May 13, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventors: Donn G. Wishka, Jason K. Myers, Bruce N. Rogers, Eric Jon Jacobsen, David W. Piotrowski, Jeffrey W. Corbett, Alice L. Bodnar, Vincent E. Groppi, Jr.
  • Patent number: 6559100
    Abstract: Substituted 2-benzoylcyclohexane-1,3-diones of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR3, —OCOR3, —OSO2R3, —S(O)nR3, —SO2OR3, —SO2N(R3)2, —NR3SO2R3 or —NR3COR3; R3 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl or phenyl-C1-C6-alkyl; where the abovementioned alkyl radicals may be partially or fully halogenated and/or may carry one to three of the following groups: hydroxyl, mercapto, amino, cyano, R3, —OR3, —SR3, —N(R3)2, ═NOR3, —OCOR3, —SCOR3, —NR3COR3, —CO2R3, —COSR3, —CON(R3)2, C1-C4-alkyliminooxy, C1-C4-alkoxyamino, C1-C4-alkylcarbonyl, C1-C4-alkoxy-C2-C6-alkoxycarbonyl, C1-C4-alkylsulfonyl, heterocyclyl, heterocyclyloxy, phenyl, benzyl, hetaryl, phenoxy, benzyloxy and hetaryloxy, where the eight last mentioned radic
    Type: Grant
    Filed: February 7, 2000
    Date of Patent: May 6, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Stefan Engel, Joachim Rheinheimer, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Matthias Witschel, Martina Otten, Helmut Walter, Karl-Otto Westphalen
  • Publication number: 20030069290
    Abstract: The invention provides compounds of Formula I: compounds of the Formula I: 1
    Type: Application
    Filed: August 14, 2002
    Publication date: April 10, 2003
    Inventors: Donn G. Wishka, Jason K. Myers, Bruce N. Rogers, Eric Jon Jacobsen, David W. Piotrowski, Jeffrey W. Corbett, Alice L. Bodnar, Vincent E. Groppi,