Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 548/217)
-
Patent number: 6224644Abstract: A cyanine dye having the formula wherein R1-R8 are each independently selected from a group consisting of hydrogen, C1-C6 alkyl group, and C0-C4 alkyl group having a hydrophilic substituent thereon. R11 and R12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.Type: GrantFiled: November 24, 1999Date of Patent: May 1, 2001Assignee: NEN Life Science Products, Inc.Inventors: Malcolm Harry Randall, Philip Richard Buzby, Thomas Joseph Erickson, Joseph David Trometer, Joseph John Miller, Jr., David George Ahern, Mark Norman Bobrow
-
Patent number: 6225331Abstract: This invention involves compounds having the following structure: as described in the claims; and enantiomers, optical isomers, stereoisomers, diastereomers, tautomers, addition salts, biohydrolyzable amides and esters thereof, as well as pharmaceutical compositions comprising such novel compounds. The invention also relates to the use of such compounds for preventing or treating disorders modulated by alpha-2 adrenoceptors.Type: GrantFiled: August 9, 1999Date of Patent: May 1, 2001Assignee: The Procter & Gamble CompanyInventors: Thomas Lee Cupps, Sophie Eva Bogdan, Raymond Todd Henry, Russell James Sheldon, William Lee Seibel, Jeffrey Joseph Ares
-
Patent number: 6221604Abstract: The invention provides compositions electron-deficient nitrogen heterocycle-substituted fluorescein dyes and methods in which the dyes are conjugated to substrates and used as detection labels in molecular biology experiments. The electron-deficient nitrogen heterocycles include pyridine, quinoline, pyrazine, and the like. Substrates include polynucleotides, nucleosides, nucleotides, peptides, proteins, carbohydrates, and ligands.Type: GrantFiled: February 7, 2000Date of Patent: April 24, 2001Assignee: PE CorporationInventors: Krishna G. Upadhya, Steven M. Menchen, Weiguo Zhen
-
Patent number: 6218135Abstract: The present invention has its objects to provide a compound not only which is easy to handle, thermally stable, and high in emission efficiency, but also which can show high emission efficiency without coexisting enhancer in the system even in a protic solvent. The present invention is related to a 1,2-dioxetane derivative of general formula (I). [wherein R1, R2, R3, R4 and R5 each independently represents hydrogen, alkyl or aryl; a pair of R2 and R3 and a pair of R4 and R5 may respectively be joined to each other to form a cycloalkyl group.Type: GrantFiled: March 15, 1999Date of Patent: April 17, 2001Inventors: Masakatsu Matsumoto, Nobuko Watanabe
-
Patent number: 6211215Abstract: Heterocyclic compounds represented by the general formula (I) wherein R stands for an optionally substituted aromatic heterocyclic group; X stands for oxygen atom, an optionally oxidated sulfur atom, —C(═O)— or —CH(OH)—; Y stands for CH or N; m denotes an integer of 0 to 10: n denotes an integer of 1 to 5: cyclic group stands for an optionally substituted aromatic azole group; and ring A is optionally further substituted, or salts thereof. The compound (I) possesses action of inhibiting tyrosine kinase and useful as antitumor agents.Type: GrantFiled: November 18, 1998Date of Patent: April 3, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Yu Momose, Etsuya Matsutani
-
Patent number: 6204389Abstract: A cyanine dye having the formula wherein R1--R8 are each independently selected from a group consisting of hydrogen, C1-C6 alkyl group, and C0-C4 alkyl group having a hydrophilic substituent thereon. R11 and R12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.Type: GrantFiled: November 24, 1999Date of Patent: March 20, 2001Assignee: NEN Life Science Products, Inc.Inventors: Malcolm Harry Randall, Philip Richard Buzby, Thomas Joseph Erickson, Joseph David Trometer, Joseph John Miller, Jr., David George Ahern, Mark Norman Bobrow
-
Patent number: 6204279Abstract: Compounds are described which have efflux pump inhibitor activity. Also described are methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.Type: GrantFiled: June 3, 1998Date of Patent: March 20, 2001Assignee: Microcide Pharmaceuticals, Inc.Inventors: Roger Leger, Ving J. Lee, Miles She
-
Patent number: 6201125Abstract: Disclosed is a process for preparing 2,5-dicarbonamido phenol compounds comprising a step employing a 2-alkyl-6-nitro-benzoxazole to form a 2-alkyl-6-amino-benzoxazole in which the 2-alkyl group is unbranched at the &agr; carbon. It also provides intermediate compounds useful in the process. The process provides a simple and safe way to prepare 2,5-dicarbonamido phenol compounds in good yield.Type: GrantFiled: December 28, 1999Date of Patent: March 13, 2001Assignee: Eastman Kodak CompanyInventor: William J. Begley
-
Patent number: 6201126Abstract: Compounds of the formula (I) in which A represents N or a cyanomethylene radical, B represents S, O or NH and R1, R2, R3 and x have the meaning given in the description, are highly suitable for dyeing and printing high-molecular-weight materials, in particular automotive cover fabrics.Type: GrantFiled: June 2, 1997Date of Patent: March 13, 2001Assignee: Bayer AktiengesellschaftInventor: Manfred Lorenz
-
Patent number: 6197956Abstract: A cyanine dye having the formula wherein R1-R8 are each independently selected from a group consisting of hydrogen, C1-C6 alkyl group, and C0-C4 alkyl group having a hydrophilic substituent thereon. R11 and R12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.Type: GrantFiled: November 24, 1999Date of Patent: March 6, 2001Assignee: NEN Life Science Products, Inc.Inventors: Malcolm Harry Randall, Philip Richard Buzby, Thomas Joseph Erickson, Joseph David Trometer, Joseph John Miller, Jr., David George Ahern, Mark Norman Bobrow
-
Patent number: 6197750Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: GrantFiled: October 22, 1998Date of Patent: March 6, 2001Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Robert J. Ternansky
-
Patent number: 6190580Abstract: Photochromic diaryl-2H-naphthopyran structures, which dye photochromically well at room temperature, lighten up quickly when incorporated into ophthalmic lenses, possess longevity, and due to their special structure, have a reduced tendency of the molecules to migrate in plastics.Type: GrantFiled: November 23, 1999Date of Patent: February 20, 2001Assignee: Optische Werke G. RodenstockInventors: Manfred Melzig, Herbert Zinner
-
Patent number: 6177572Abstract: Methods for preparing benzoxazoles and benzothiazoles on solid supports. Substituted benzothiazoles and benzoxazoles, libraries of the compounds, and methods of using the compounds are also disclosed.Type: GrantFiled: August 20, 1997Date of Patent: January 23, 2001Assignee: Sepracor, Inc.Inventor: Fengjiang Wang
-
Patent number: 6169085Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: October 4, 1999Date of Patent: January 2, 2001Assignee: G. D. Searle & CompanyInventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
-
Patent number: 6159995Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
-
Patent number: 6156937Abstract: Fluoropolyethers having functional groups, consisting of randomly distributed sequences of perfluoropolyoxyalkylene units selected from: ##STR1## where X is F or CF.sub.3 T, T', T"=a perfluoroalkyl group containing from 1 to 3 carbon atoms and one or two atoms of Cl, Br or I;R, R'=halogen atoms;Y=a functional group;o, q=numbers, zero included, such that o+q=1-20;n=a number ranging from 1 to 15;m/n=a number ranging from 0.01 to 0.5;p=a number ranging from 1 to 20;s/p=a number ranging from 0.5 to 2; andz/o+p=a number ranging from 0.01 to 0.05.Type: GrantFiled: January 20, 1998Date of Patent: December 5, 2000Assignee: Ausimont S.p.A.Inventors: Giuseppe Marchionni, Piero Gavezotti, Ezio Strepparola
-
Patent number: 6156772Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: May 14, 1999Date of Patent: December 5, 2000Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Thomas F. Walsh, Feroze Ujjainwalla, Matthew J. Wyvratt, Jr.
-
Patent number: 6143747Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.Type: GrantFiled: February 26, 1998Date of Patent: November 7, 2000Assignee: G. D. Searle & Co.Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
-
Patent number: 6140506Abstract: The present invention produces novel cis-oxazolidinone compound which is racemic form or optically active form, of a formula (1) ##STR1## wherein R represents C.sub.1 -C.sub.6 alkyl group, C.sub.2 -C.sub.6 alkenyl group, C.sub.1 -C.sub.6 alkoxyl group, C.sub.1 -C.sub.6 alkylamino group, aryl group or halogen atom, and oxazolidinone ring is at cis-configuration, comprising reacting cis-1,2-indene epoxide of a formula (3) ##STR2## form, with sulfonyl isocyanate compound of a formula (4) ##STR3## in the presence of metal halide catalyst. Further, cis-1-amino-2-indanol is produced by hydrolyzing the oxazolidinone compound. The latter compound is useful as an intermediate of HIV-drug.Type: GrantFiled: December 30, 1998Date of Patent: October 31, 2000Assignee: Nissan Chemical Industries, Ltd.Inventors: Akio Baba, Kenji Suzuki, Yoshinobu Yanagawa, Yoko Ohkuni, Takashi Oda, Masao Shimada, Masami Kozawa
-
Patent number: 6140051Abstract: Dibenzazole compounds having the general structure: ##STR1## wherein; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 are independently H or a substituent which aids in solubility of the compound or which provides a linker arm for linking the compound to another moiety; Y is H or a cleavable moiety; X is a hydrogen, halogen, CF.sub.3, or SO.sub.3 H; V and W are oxygen or sulfur; Z is --C.dbd.C--, --C.tbd.C-- or an aromatic ring moiety; and n is 0, 1, or 2. When n=0 at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 is a substituent which aids in solubility of the compound or which provides a linker arm for linking the compound to another moiety or X is a halogen, CF.sub.3 or SO.sub.3 H. These compounds are highly fluorescent and can be easily detected using a fluorometer. Derivatives in which the Y group is a substituent other than H contain a fluorescence inhibiting chemical moiety that upon removal restores the fluorescence of the compound.Type: GrantFiled: July 17, 1998Date of Patent: October 31, 2000Assignee: Promega Biosciences, Inc.Inventors: Lauren R. Brown, Cheng Xu
-
Patent number: 6136831Abstract: The purpose is to provide anti-inflammatory agents which have potent pharmacological actions and exert a selective inhibitory activity on COX-2, thereby being expected to reduce adverse effects such as disorders in gastric mucosa. The present invention encompasses a compound of the formula (1): wherein R.sup.1 is hydrogen or halogen, R.sup.2 and R.sup.3 are each independently hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy or lower alkanoyloxy, R.sup.4 is lower haloalkyl or lower alkyl, X is sulfur, oxygen or NH, and Y is lower alkylthio, lower alkylsulfonyl or sulfamoyl, which exerts superior anti-inflammatory activity, and highly inhibits COX-2 induced in inflamed sites, with less inhibitory action on COX-1 present in stomach, kidney, etc. Pharmaceutical agents comprising the compound of the present invention are provided as selective COX-2 inhibitors, and anti-inflammatory agents rarely accompanying adverse actions including attacks on gastric mucosa.Type: GrantFiled: October 7, 1999Date of Patent: October 24, 2000Assignee: Grelan Pharmaceutical Co., Ltd.Inventors: Tomoji Aotsuka, Nagatoshi Wagatsuma, Hideo Kato, Naoki Ashizawa
-
Patent number: 6124277Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.Type: GrantFiled: March 11, 1999Date of Patent: September 26, 2000Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
-
Patent number: 6114350Abstract: A cyanine dye having the formula ##STR1## wherein R.sub.1 -R.sub.8 are each independently selected from a group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl group, and C.sub.0 -C.sub.4 alkyl group having a hydrophilic substituent thereon. R.sub.11 and R.sub.12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.Type: GrantFiled: April 19, 1999Date of Patent: September 5, 2000Assignee: NEN Life Science Products, Inc.Inventors: Malcolm Harry Randall, Philip Richard Buzby, Thomas Joseph Erickson, Joseph David Trometer, Joseph John Miller, Jr., David George Ahern, Mark Norman Bobrow
-
Patent number: 6114329Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof:X--CO--CH.sub.2 --Z (I)whereinX is a monocyclic or polycyclic aromatic group,Z is of a linear, cyclic or bicyclic, aromatic or aliphatic moiety containing a nitrogen atom;and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: January 26, 1998Date of Patent: September 5, 2000Assignee: SmithKline Beecham plcInventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
-
Patent number: 6110952Abstract: This invention relateds to compounds of formula I, (2-imidazolinylamino)benzoxazoles. The compounds have been found to be alpha-2 adrenocepto agonists and are useful for treatment of disorders modulated by alpha-2 adrenoceptors.Type: GrantFiled: August 9, 1999Date of Patent: August 29, 2000Assignee: The Procter & Gamble CompanyInventors: Raymond Todd Henry, Russell James Sheldon, William Lee Seibel
-
Patent number: 6093830Abstract: The invention relates to a novel non-catalytic enantioselective resolution process for the separation of enantiomer of arylpropionic acid drugs from the racemic mixture, which comprises dissolving the racemic mixture of the said drug an organic solvent, reacting this solution with an aqueous phase containing an ionic surfactant with or without a suitable co-surfactant, and an electrolyte in microemulsion/micellar/biphasic medium, reacting this mixture with an appropriate chiral amine at a temperature in the range of 0 to 70 degrees Celsius to obtain a diastereomeric salt, acid hydrolysing the diastereomeric salt to result in the pure enantiomer of the drug which is extracted by known methods.Type: GrantFiled: March 15, 1999Date of Patent: July 25, 2000Assignee: Council of Scientific and Industrial ResearchInventors: Nirmal Kishor Yadav, Bhaskar Dattatraya Kulkarni, Ramdas Bhagvan Khomane
-
Patent number: 6083961Abstract: This invention relates to a heterocyclic compound of the formula: ##STR1## wherein a group of the formula: ##STR2## is a group of the formula: ##STR3## etc., X is O, S or N--R.sup.5,R.sup.1 is lower alkyl, etc.,R.sup.5 is hydrogen, lower alkyl, etc.,R.sup.2 is hydrogen, halogen, lower alkyl, etc.,R.sup.3 is halogen, lower alkyl, etc.,R.sup.4 is amino optionally having suitable substituent(s), andA is lower alkylene,and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.Type: GrantFiled: February 3, 1997Date of Patent: July 4, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Hiroshi Kayakiri, Shigeki Satoh, Yoshito Abe, Yuki Sawada, Takayuki Inoue, Hirokazu Tanaka
-
Patent number: 6080868Abstract: The invention provides an asymmetric cyanine dye compound having the structure ##STR1## including substituted forms thereof, wherein, at least one of R.sub.1 and R.sub.2 is linking group, X is O, S, or Se, and n ranges from 0 to 2. The invention further provides reporter-quencher dye pairs comprising the asymmetric cyanine dyes, dye-labeled polynucleotides incorporating the asymmetric cyanine dyes, and hybridization detection methods utilizing the dye-labeled polynucleotides.Type: GrantFiled: January 23, 1998Date of Patent: June 27, 2000Assignee: The Perkin-Elmer CorporationInventors: Linda G. Lee, Ronald J. Graham, Khairuzzaman B. Mullah, Francis T. Haxo
-
Patent number: 6077864Abstract: A compound of the formula ##STR1## wherein n, X, Y and Ar are as defined herein, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.Type: GrantFiled: June 17, 1999Date of Patent: June 20, 2000Assignee: Pfizer Inc.Inventors: Laurence Edward Burgess, James Patrick Rizzi
-
Patent number: 6063795Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: May 10, 1999Date of Patent: May 16, 2000Assignee: G.D. Searle & CompanyInventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
-
Patent number: 6060493Abstract: A compound of the general formula I ##STR1## where the indices and the substituents have the following meanings: R.sup.1 is C(CO.sub.2 CH.sub.3).dbd.CHOCH.sub.3, C(CO.sub.2 CH.sub.3).dbd.NOCH.sub.3, N(OCH.sub.3)CO.sub.2 CH.sub.3 and C(CONHCH.sub.3).dbd.NOCH.sub.3 ;R.sup.2 is cyano, halogen, C.sub.1 -C.sub.4 -alkyl and C.sub.1 -C.sub.4 -alkoxy;m is 0 or 1;R.sup.3 is cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl and C.sub.1 -C.sub.4 -alkoxy;n is 0, 1, 2 or 3, it being possible for the substituents R.sup.3 to be different from each other when n is 2 or 3;R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl and phenyl;X and Y are C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino or a C.sub.1 -C.sub.Type: GrantFiled: April 20, 1998Date of Patent: May 9, 2000Assignee: BASF AktiengesellschaftInventors: Hubert Sauter, Wassilios Grammenos, Bernd Muller, Klaus Oberdorf, Norbert Gotz, Franz Rohl, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
-
Patent number: 6036890Abstract: Photochromic diaryl-2H-naphthopyran structures, which dye photochromically well at room temperature, lighten up quickly when incorporated into ophthalmic lenses, possess longevity, and due to their spacial structures, have a reduced tendency of the molecules to migrate in plastics.Type: GrantFiled: July 31, 1998Date of Patent: March 14, 2000Assignee: Optische Werke G. RodenstockInventors: Manfred Melzig, Herbert Zinner
-
Patent number: 6037473Abstract: The invention relates to N-substituted benzazoles, processes for their preparation and their use as UV absorbers.Type: GrantFiled: April 23, 1999Date of Patent: March 14, 2000Assignee: Haarmann & Reimer GmbHInventors: Erich Dilk, Roland Langner, William Johncock
-
Patent number: 6034246Abstract: There are disclosed herein 2-phenylbenzazole compounds having a 3'-substituent and a 4'-NR.sup.2 R.sup.6 substituent in the phenyl group where R.sup.5 and R.sup.6 are each hydrogen or alkyl, or where the $'-NR.sup.5 R.sup.6 substituent is N-acyl (or N-benzoyl). There are also disclosed 2-phenylbenzazole compounds in the form of 4'-N sulphamate salts. Such compounds exhibit significant selective cytotoxic activity in respect of tumor cells and provide potentially useful chemotherapeutic agents for selective treatment of a range of cancers.Type: GrantFiled: August 28, 1997Date of Patent: March 7, 2000Assignee: Cancer Research Campaign Technology LimitedInventors: Malcolm Francis Graham Stevens, Dong-Fang Shi, Tracey Dawn Bradshaw, Samantha Wrigley
-
Patent number: 6030619Abstract: Molecular mimetics of unique epitopes of Neisseria meningitidis serogroup B ("MenB") are disclosed. Compositions containing such molecular mimetics can be used to prevent MenB or E. coli K1 disease without the risk of evoking autoantibody responses.Type: GrantFiled: August 26, 1998Date of Patent: February 29, 2000Assignee: Chiron CorporationInventors: Dan M. Granoff, Gregory R. Moe
-
Patent number: 6025177Abstract: Processes for preparing a single enantiomer of an .alpha.,.alpha.-disubstituted-.alpha.-hydroxy acetic acid, especially cyclohexylphenylglycolic acid (CHPGA), is disclosed. The processes employ cyclic 1,2-aminoalcohols as chiral auxiliaries by forming diastereomeric esters of aminoalcohols or diastereomeric amides of oxazolidines. ##STR1## Intermediates useful in the process are also disclosed.Type: GrantFiled: February 9, 1999Date of Patent: February 15, 2000Assignee: Sepracor Inc.Inventors: Chris Hugh Senanayake, Roger P. Bakale, Qun Kevin Fang, Paul Timothy Grover, Donald L. Heefner, Richard F. Rossi, Stephen Alan Wald
-
Patent number: 6015827Abstract: Benzoxazole carboxamides are disclosed which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. Representative of the compounds are 2-methyl, 2-t-butyl, 2-phenyl or 2-(4-methoxyphenyl) benzoxazole-4-carboxamide.Type: GrantFiled: April 8, 1998Date of Patent: January 18, 2000Assignee: Newcastle University Ventures LimitedInventors: Roger John Griffin, Alan Hilary Calvert, Nicola Jane Curtin, David Richard Newell, Bernard Thomas Golding
-
Patent number: 6015824Abstract: The present invention relates to the use of pyrrolidine and piperidine derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 are, independently from each other, hydrogen, lower alkoxy, hydroxy, halogen, --CONH.sub.2 or --C(O)O-lower alkyl; or taken together are --O--CH.sub.2 O;R.sup.3 and R.sup.4 are, independently from each other, hydrogen, lower alkoxy, benzyloxy, halogen, hydroxy, --CONH.sub.2 or --SCH.sub.3 ; or taken together are --O--CH.sub.2 --O--;Y is --CH(OH)--, --(CH.sub.2).sub.n --, --C(O)-- or --CH(lower alkoxy)--; andm, n and p are 1 or 2;and to their pharmaceutically acceptable addition salts for the treatment of diseases caused by over activation of NMDA receptor subtypes.Type: GrantFiled: January 20, 1999Date of Patent: January 18, 2000Assignee: Hoffmann-La Roche AGInventors: Alexander Alanine, Bernd Buttelmann, Marie-Paule Heitz Neidhart, Emmanuel Pinard, Rene Wyler
-
Patent number: 6013830Abstract: Processes for preparing a single enantiomer of an .alpha.,.alpha.-disubstituted-.alpha.-hydroxy acetic acid, especially cyclohexylphenylglycolic acid (CHPGA), is disclosed. The processes employ cyclic 1,2-aminoalcohols as chiral auxiliaries by forming diastereomeric esters of aminoalcohols or diastereomeric amides of oxazolidines. ##STR1## Intermediates useful in the process are also disclosed.Type: GrantFiled: March 30, 1998Date of Patent: January 11, 2000Assignee: Sepracor Inc.Inventors: Chris Hugh Senanayake, Roger P. Bakale, Qun Kevin Fang, Paul Timothy Grover, Donald L. Heefner, Richard F. Rossi, Stephen Alan Wald
-
Patent number: 6011033Abstract: This invention relates to a phenylene derivative represented by the following formula (1) or a salt thereof and also to a medicine containing it as an effective ingredient. ##STR1## wherein R.sup.1 represents H or halogen; A represents --CH.dbd.CH--, --CH.dbd.N--, --N(R.sup.2)--, --O-- or --S--; W represents --CH.dbd.CH-- or --CH.sub.2 O--; X represents --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 N(R.sup.3)--, --CH.dbd.N--, --COO-- or --CONH--; Y represents ##STR2## B.sup.1 represents --C(R.sup.7)(R.sup.8)(CH.sub.2).sub.l --, --S(O).sub.m (CH.sub.2).sub.n -- or --CH.dbd.C(R.sup.9)--; B.sup.2 represents --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --; Z.sup.1 and Z.sup.2 each represents O or S; etc. The phenylene derivative or salt thereof has antileukotrienic action and antihistaminic action and is useful as a medicine such as an asthma preventive or curative.Type: GrantFiled: November 13, 1998Date of Patent: January 4, 2000Assignee: Kowa Co., Ltd.Inventors: Henk Timmerman, Mingqiang Zhang, Kazuhiro Onogi, Masahiro Tamura, Tsutomu Toma, Yasushi Wada
-
Patent number: 6004536Abstract: The present invention relates to a family of cyanine dyes possessing lipophilic alkyl chains and either one or more reactive functional groups, bromo or chloro, or phenyl, sulfophenyl or polysulfophenyl substituents or combinations thereof. The dyes of the invention are useful for staining membranes in cells or isolated from cells, and are well-retained therein. Additionally, the reactive dyes of the invention are useful for preparing dye-conjugates, thereby conferring the membrane staining ability of the subject dye onto the resulting dye-conjugate.Type: GrantFiled: August 14, 1996Date of Patent: December 21, 1999Assignee: Molecular Probes, Inc.Inventors: Wai-Yee Leung, Richard P. Haugland, Fei Mao
-
Patent number: 5994379Abstract: The present invention relates to inhibitors of COX-2, compositions which contain such compounds and methods of use. The compounds are represented by formula I: ##STR1## and include pharmaceutically acceptable salts and esters thereof.Type: GrantFiled: February 9, 1999Date of Patent: November 30, 1999Assignee: Merck Frosst Canada, Inc.Inventors: Christopher I. Bayly, Cameron Black, Nathalie Ouimet, David Percival, Serge Leger, Marc Ouellet
-
Patent number: 5985870Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: December 19, 1997Date of Patent: November 16, 1999Assignee: G.D. Searle & Co.Inventors: Daniel P Getman, Gary A. Decrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
-
Patent number: 5981759Abstract: An intermediate in the synthesis of indinavir is prepared by iodohydroxylating an allyl acetonide by hypoiodous acid generated in situ from sodium hypochlorite and sodium iodide.Type: GrantFiled: June 17, 1998Date of Patent: November 9, 1999Assignee: Merck & Co., Inc.Inventors: Yongku Sun, Frank P. Gortsema, Carl Leblond, Kai Rossen
-
Patent number: 5981559Abstract: An azole derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, having both of a leukotriene antagonistic effect and a thromboxane A2 antagonistic effect and being useful in preventing or treating allergic diseases, ischemic heart diseases or ischemic brain diseases, and a medicinal composition containing the same as the active ingredient, wherein R.sup.1 and R.sup.2 may be the same or different and represent each hydrogen, cycloalkyl, etc., or R.sup.1 and R.sup.2 together with (a) may form a fused ring (b) or (c) which may be substituted by optionally substituted lower alkyl, amino, etc.; R.sup.3, R.sup.6, R.sup.7, R.sup.8 may be the same or different and represent each hydrogen, amino, etc.; R.sup.4 represents cyano, tetrazolyl, --COOR.sup.9, etc.; R.sup.5 represents hydrogen or lower alkyl; D represents optionally substituted lower alkylene; X and Z may be the same or different and represent each oxygen or sulfur; Y represents --N.dbd. or --CH.dbd.Type: GrantFiled: August 15, 1997Date of Patent: November 9, 1999Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriko Nagaoka, Masaki Yokota, Hiroaki Akane, Yasuhito Arakida, Yasuo Isomura
-
Patent number: 5962656Abstract: A photographic element comprising a support having situated thereon at least one silver halide emulsion layer, the layer containing a photographic coupler represented by the formulaCOUP--T.sup.1 --T.sup.2 --(T.sup.3).sub.b --PUGwhereinCOUP is a coupler moiety having a coupling site to which T.sup.1 is attached;T.sup.1 and T3 are timing or linking groups;T.sup.2 is an indazole timing or linking group which, after release from T.sup.1, functions by electron transfer down a conjugated chain to release T.sup.3 or PUG, and which is represented by the formula: ##STR1## wherein ** denotes the point of attachment to T.sup.1 and *** denotes the point of attachment to T.sup.3 or PUG;R.sup.1 and R.sup.2 are independently selected from hydrogen, or an aliphatic, carbocyclic, or heterocyclic group, or may be bonded together to form a 5, 6, or 7 membered ring;V is independently a substituent group as further defined;q is 0, 1, 2, 3 or 4;b is 0 or 1; andPUG is a photographically useful group.Type: GrantFiled: June 10, 1997Date of Patent: October 5, 1999Assignee: Eastman Kodak CompanyInventors: William James Begley, Teh Hsuan Chen, Donald Singleton, Jr., Frank Dino Coms
-
Patent number: 5962504Abstract: Compounds of formula I: ##STR1## wherein R.sub.1 and R.sub.2 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are PKC activators and are useful for treating diseases, such as, for example, cancer. Also disclosed are pharmaceutical compositions comprising compounds of formula I, processes for preparing compounds of formula I, and intermediates useful for preparing compounds of formula I.Type: GrantFiled: September 8, 1998Date of Patent: October 5, 1999Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Shaomeng Wang, Lixin Qiao
-
Patent number: 5942535Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid group and for the prevention of allergically induced diseases.Type: GrantFiled: March 28, 1997Date of Patent: August 24, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
-
Patent number: 5939415Abstract: The present invention relates to heterocyclic compounds with the formula ##STR1## in which R.sup.1 to R.sup.7, B, a, and X have the meanings indicated in the specification. These compounds can be used for the treatment of diseases of the rheumatic variety and for the prevention of allergically-induced diseases.Type: GrantFiled: March 28, 1997Date of Patent: August 17, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
-
Patent number: 5932740Abstract: Disclosed is a novel near-infrared absorbing dye of formula: ##STR1## wherein X.sup.1, X.sup.2 independently represents --CR.sup.8 R.sup.9 --, --S--, --Se--, --NR.sup.10 --, --CH.dbd.CH-- or --O--;n is an integer of 2 or 3;R.sup.1 and R.sup.2 independently represent alkyl of 1 to 10 carbons or substituted alkyl of 1 to 10 carbons;R.sup.3 represents a ring chosen from a set consisting of aryl, substituted aryl, and a heterocyclic ring of a type present in photographic emulsions;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently represent hydrogen, alkyl of 1-10 carbons, substituted alkyl of 1-10 carbons, R.sup.4 and R.sup.5 taken together or R.sup.6 and R.sup.7 taken together can represent atoms necessary to form a 5 or 6-membered aliphatic ring, an aromatic six-membered ring, an aromatic 10-membered ring, a substituted aromatic six-member ring or a substituted aromatic 10-member ring;R.sup.8, R.sup.Type: GrantFiled: January 23, 1998Date of Patent: August 3, 1999Assignee: Sterling Diagnostic Imaging, Inc.Inventors: Dietrich Max Fabricius, Gregory Charles Weed