Chalcogen Bonded Directly To Ring Carbon Of The Thiadiazole Ring Patents (Class 548/129)
  • Publication number: 20040135117
    Abstract: Dichroic dyes, dichroic dye compositions, and liquid crystal composition and liquid crystal display element containing the dichroic dyes. The dichroic dye has increased solubility and stability.
    Type: Application
    Filed: May 23, 2003
    Publication date: July 15, 2004
    Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTE
    Inventors: Shih-Hsien Liu, Yang-Chu Lin, Woan-Shiow Tzeng, Jie-Hwa Ma, Kung-Lung Cheng, Long-Li Lai
  • Publication number: 20030220315
    Abstract: Alkenyldiarylmethane (ADAM) compounds have been found effective as anti-HIV agents. Novel ADAM compounds, their pharmaceutical formulations and a method of using same to treat viral infections are described.
    Type: Application
    Filed: May 27, 2003
    Publication date: November 27, 2003
    Inventors: Mark S. Cushman, Agustin Casimiro-Garcia, William G. Rice
  • Patent number: 6544931
    Abstract: The invention relates to novel substituted heteroaryloxyacetanilides of the general formula (I), in which n, R, X, and Z are to intermediates for their preparation and to their use as herbicides.
    Type: Grant
    Filed: January 16, 2002
    Date of Patent: April 8, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus-Helmut Müller, Lothar Rohe, Joachim Kluth, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Patent number: 6521650
    Abstract: Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.
    Type: Grant
    Filed: April 4, 2000
    Date of Patent: February 18, 2003
    Assignee: Pfizer, Inc.
    Inventors: Thomas Richard Belliotti, Justin Stephen Bryans, Thomas Capiris, David Christopher Horwell, Clare Octavia Kneen, David Juergen Wustrow
  • Patent number: 6518289
    Abstract: Novel amines of formulas (1), (1C), (1F), (1G) and (1H) or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A′ is a bridged ring selected from (1), (2), (3), (4), (5) wherein is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, especially irritable bowel syndrome.
    Type: Grant
    Filed: April 3, 2000
    Date of Patent: February 11, 2003
    Assignee: Pfizer, Inc.
    Inventors: Justin Stephen Bryans, Thomas Capiris, David Christopher Horwell, Clare Octavia Kneen, David Juergen Wustrow
  • Patent number: 6503934
    Abstract: Compounds of the formula (I): are suitable for the preparation of pharmaceuticals for prophylaxis and treatment of all those diseases where an increased concentration of interleukin-1&bgr; participates in their course, for example septic shock, leukemia, hepatitis, muscular degeneration, HIV infections or degenerative joint diseases (such as osteoarthrosis, spondylosis, chondrolysis following joint trauma or prolonged immobilization of joints following meniscus or patella injuries, or torn ligaments), diseases of the connective tissue (such as collagenosis, periodontal diseases, or wound-healing disturbances), and chronic diseases of the locomotor system (such as inflammatory or immunologically or metabolism-related acute and chronic arthritis, arthropathies, rheumatoid arthritis, myalgias and disturbances in bone metabolism).
    Type: Grant
    Filed: February 9, 2001
    Date of Patent: January 7, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Klaus-Ulrich Weithmann, Swen Hölder
  • Patent number: 6500944
    Abstract: The invention relates to the chemical synthesis of oligonucleotides and to chemical entities useful in such synthesis. More particularly, the invention relates to sulfurization of the internucleotide linkages of oligonucleotides. The invention provides a process to synthesize new sulfur transfer reagents and a process for their use in sulfurizing oligonucleotides. The sulfur transfer reagents according to the invention are inexpensive to make, stable in storage and in solution, and highly efficient in sulfurization.
    Type: Grant
    Filed: July 16, 1997
    Date of Patent: December 31, 2002
    Assignee: Avecia Biotechnology, Inc.
    Inventors: Saroj K. Roy, Jin-Yan Tang
  • Patent number: 6495551
    Abstract: The invention concerns compounds of formula (I), wherein, for example, R1 is of the formula —NHC(═O)Ra wherein Ra is (1-4C)alkyl; R2 and R3 are independently hydrogen or fluoro; R5 and R6 are, for example, hydrogen; R4 is —X—Y—Het.; wherein, for example, X is a direct bond and Y is —(CH2)m— or —CONH—(CH2)m—; or X is —(CH2)n— and Y is —S(O)p—(CH2)m—; or X is —CH2O—or —CH2NH— and Y is —CO—(CH2)m—; wherein n is 1, 2 or 3; m is 0, 1, 2 or 3 and p is 0, 1 or 2; wherein Het. is a heterocyclic ring, unsaturated or saturated, optionally substituted by, for example, (1-4C)alkyl, halo, cyano, nitro or amino; pharmaceutically acceptable salts and in vivo hydrolysable ester thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.
    Type: Grant
    Filed: May 25, 2000
    Date of Patent: December 17, 2002
    Inventors: Michael John Betts, Michael Lingard Swain
  • Publication number: 20020165398
    Abstract: The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like.
    Type: Application
    Filed: April 19, 2002
    Publication date: November 7, 2002
    Inventors: Lone Jeppesen, Henrik Sune Andersen, Ole Hvilsted Olsen, Luke Milburn Judge, Daniel Dale Holsworth, Farid Bakir, Frank Urban Axe, Yu Ge
  • Patent number: 6342245
    Abstract: The present invention is concerned with novel pharmaceutical compositions of lipid lowering agents which can be administered to a mammal suffering from hyperlipidemia, obesitas or atherosclerosis, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising a lipid lowering agent and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.
    Type: Grant
    Filed: April 24, 2000
    Date of Patent: January 29, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Lieven Baert, Geert Verreck
  • Publication number: 20020010326
    Abstract: In our research, 3-phenyl-1,2,4-dithiazoline-5-one is found to be a potential sulfur-transfer reagent. The efficiency and optimization of this new sulfur-transfer reagent was investigated by solid-phase syntheses of dinucleotide phosphorothioate and 25 mer oligonucleotide phosphorothioates at 1 &mgr;mol and 200 &mgr;mol scales. The results show that 3-phenyl-1,2,4-dithiazoline-5-one is a highly efficient sulfurizing reagent, and greater than 99.8% sulfur transfer efficiency can be achieved. In contrast to EDITH or Beaucage reagent, this novel sulfur-transfer reagent is highly stable in storage and in solution, highly soluble in CH3CN solvent, and can be synthesized at a low cost because of the single step reaction. Due to these advantages, 3-phenyl-1,2,4-dithiazoline-5-one can be considered as a better alternative to EDITH or Beaucage reagent, especially in large-scale preparation of oligonucleotide phosphorothioates.
    Type: Application
    Filed: July 16, 1997
    Publication date: January 24, 2002
    Inventors: SAROJ K. ROY, JIN YAN TANG
  • Patent number: 6323315
    Abstract: The present invention provides compounds of the formula where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocylic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or —C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: November 27, 2001
    Assignees: BASF Aktiengesellschaft, Arizona Board of Regents
    Inventors: George R. Pettit, Jayaram K. Srirangam, Michael D. Williams, Kieran P. M. Durkin, Teresa Barlozzari, Andreas Kling, Bernd Janssen, Andreas Haupt
  • Patent number: 6306855
    Abstract: The invention relates to novel fluoromethoximino compounds, to a process for their preparation and to their use as pesticides, and also to novel intermediates and to a plurality of processes for their preparation.
    Type: Grant
    Filed: December 2, 1999
    Date of Patent: October 23, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Albrecht Marhold, Uwe Stelzer, Reinhard Lantzsch, Ralf Tiemann, Klaus Stenzel, Astrid Mauler-Machnik, Stefan Dutzmann, Martin Kugler, Hans-Ulrich Buschhaus
  • Patent number: 6218412
    Abstract: Compounds of the formula (I): are suitable for the preparation of pharmaceuticals for prophylaxis and treatment of all those diseases where an increased concentration of interleukin-1&bgr; participates in their course, for example septic shock, leukemia, hepatitis, muscular degeneration, HIV infections or degenerative joint diseases (such as osteoarthrosis, spondylosis, chondrolysis following joint trauma or prolonged immobilization of joints following meniscus or patella injuries, or torn ligaments), diseases of the connective tissue (such as collagenosis, periodontal diseases, or wound-healing disturbances), and chronic diseases of the locomotor system (such as inflammatory or immunologically or metabolism-related acute and chronic arthritis, arthropathies, rheumatoid arthritis, myalgias and disturbances in bone metabolism).
    Type: Grant
    Filed: October 14, 1999
    Date of Patent: April 17, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Klaus-Ulrich Weithmann, Swen Hölder
  • Patent number: 6114537
    Abstract: Thiols are trapped, and converted to disulfide compounds, by a process of reacting them with compounds containing a 1,2,4-thiadiazole ring structure carrying a substituent at position 3 of the thiadiazole ring, and being unsubstituted at position N-2. The process is useful pharmacologically, in inhibiting certain thiol-containing enzymes such as H.sup.+ /K.sup.+ -ATPase (the proton pump), and industrially, in selective removal of thiol compounds from gas or liquid mixtures.
    Type: Grant
    Filed: February 21, 1997
    Date of Patent: September 5, 2000
    Assignee: Apotex Inc.
    Inventors: Khashayar Karimian, Tim F. Tam, Denis Desilets, Sue Lee, Tullio Cappelletto, Wanren Li
  • Patent number: 6096895
    Abstract: Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful as fungicides ##STR1## In said formula, E is a ring system selected from certain 5- to 12-membered monocyclic and fused bicyclic aromatic heterocyclic ring systems, or an optionally substituted naphthalene ring as defined in the disclosure;A is O; S; N; NR.sup.5 ; or CR.sup.14 ;G is C or N; provided that when G is C, then A is O, S or NR.sup.5 and the floating double bond is attached to G; and when G is N, then A is N or CR.sup.14 and the floating double bond is attached to A;W is O; S; NH; N(C.sub.1 -C.sub.6 alkyl); or NO(C.sub.1 -C.sub.6 alkyl);X is OR.sup.1 ; S(O).sub.m R.sup.1 ; or halogen;R.sup.1 is C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl; C.sub.2 -C.sub.6 alkenyl; C.sub.2 -C.sub.6 haloalkenyl; C.sub.2 -C.sub.6 alkynyl; C.sub.2 -C.sub.6 haloalkynyl; C.sub.3 -C.sub.6 cycloalkyl; C.sub.2 -C.sub.4 alkylcarbonyl; or C.sub.2 -C.sub.4 alkoxycarbonyl;R.sup.2 is H; C.sub.1 -C.sub.6 alkyl; C.
    Type: Grant
    Filed: November 13, 1997
    Date of Patent: August 1, 2000
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Richard James Brown, Dilon Jancey Daniel, Deborah Ann Frasier, Michael Henry Howard, Jr., Gerard Michael Koether, Morris Padgett Rorer
  • Patent number: 6031107
    Abstract: The invention relates to new fluoromethoxyacrylic acid derivatives, a process for their preparation and their use as pesticides, as well as to new intermediates and a plurality of processes for their preparation.It has already been disclosed that certain fluoromethoxyacrylic acid derivatives which are similar in constitution to the compounds described below have fungicidal properties (compare, for example, WO 9517376). The fungicidal action of these compounds, however, is unsatisfactory in many cases.
    Type: Grant
    Filed: April 16, 1998
    Date of Patent: February 29, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Albrecht Marhold, Uwe Stelzer, Ralf Tiemann, Klaus Stenzel, Stefan Dutzmann
  • Patent number: 6022868
    Abstract: Disclosed are compounds of formula (I) selected from the following ##STR1## wherein Y is ##STR2## and wherein A, B, C, D, R, k, m, n, o, p, s, t and u are as defined in the specification. These compounds are useful in treating diseases in the central nervous system related to malfunctioning of the nicotinic cholinergic system.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: February 8, 2000
    Assignee: Novo Nordisk Als
    Inventors: Preben Houlberg Olesen, John Bondo Hansen
  • Patent number: 5981556
    Abstract: 1,3-diazolino and 1,3-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: July 22, 1997
    Date of Patent: November 9, 1999
    Assignee: G.D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Arija A. Bergmanis, Timothy J. Hagen, E. Ann Hallinan, Steven W. Kramer, Suzanne Metz, Karen B. Peterson, Barnett S. Pitzele, Foe S. Tjoeng, Mihaly V. Toth, Mahima Trivedi, R. Keith Webber, Sofya Tsymbalov, Rolando E. Gapud
  • Patent number: 5977123
    Abstract: The invention relates to novel oximether and acrylic acid derivatives of the formula (I) ##STR1## in which Z, G, Ar, E, R.sup.1 and R.sup.2 have the meanings as given in the specification, to processes for their preparation and to their use as fungicides.
    Type: Grant
    Filed: January 9, 1998
    Date of Patent: November 2, 1999
    Assignee: Bayer Aktiengesellscgaft
    Inventors: Peter Gerdes, Herbert Gayer, Ulrich Heinemann, Ralf Tiemann, Klaus Stenzel, Stefan Dutzmann
  • Patent number: 5977149
    Abstract: Cyclic amides of Formula (I) which are useful as fungicides wherein: A is O; S; N; NR.sup.5 ;or CR.sup.14--, G is C or N; W is O or S; X is OR.sup.1, S(O).sub.m R.sup.1 or halogen; R.sup.1, R.sup.2, and R.sup.5 are independently, in part, C.sub.1 -C.sub.6 alkyl; Y is, in part, --O--; --S(O).sub.n --,--CHR.sup.6 O--; or --CHR.sup.6 O--N.dbd.C(R.sup.7)--; Z is, in part, optionally substituted cycloalkyl, phenyl, pyridinyl, pyrimidinyl, or naphthyl; and R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.14, m, and n are defined in the disclosure, are disclosed.
    Type: Grant
    Filed: January 14, 1998
    Date of Patent: November 2, 1999
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
  • Patent number: 5972978
    Abstract: The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.
    Type: Grant
    Filed: February 19, 1999
    Date of Patent: October 26, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
  • Patent number: 5958957
    Abstract: The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 --A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.
    Type: Grant
    Filed: April 16, 1997
    Date of Patent: September 28, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
  • Patent number: 5958958
    Abstract: 1,2,4-oxa-diazolino and 1,2,4-oxa-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: January 14, 1999
    Date of Patent: September 28, 1999
    Assignee: G.D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Arija A. Bergmanis, Timothy J. Hagen, E. Ann Hallinan, Steven W. Kramer, Suzanne Metz, Karen B. Peterson, Barnett S. Pitzele, Foe S. Tjoeng, Mihaly V. Toth, Mahima Trivedi, R. Keith Webber, Sofya Tsymbalov, Rolando E. Gapud
  • Patent number: 5929075
    Abstract: The present invention provides novel compounds of formula ##STR1## the N-oxides, the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof, wherein A and B taken together form a bivalent radical of formula:--N.dbd.CH-- (a), --CH.dbd.N-- (b), --CH.sub.2 --CH.sub.2 -- (c), --CH.dbd.CH-- (d), --C(.dbd.O)--CH.sub.2 -- (e), --CH.sub.2 --C(.dbd.O)-- (f); R.sup.1 is hydrogen, C.sub.1-6 alkyl, or halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-6 cycloalkyl or C.sub.1-8 alkyl substituted with hydroxy, oxo, C.sub.3-6 cycloalkyl or aryl. Het is five- or six-membered optionally substituted heterocyclic ring. The use as a medicine, especially as a lipid lowering agent is disclosed as well as pharmaceutical compositions and processes for preparing compounds and compositions.
    Type: Grant
    Filed: April 9, 1997
    Date of Patent: July 27, 1999
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Heeres, Leo Jacobus Jozef Backx, Robert Jozef Maria Hendrickx, Luc Alfons Leo Van der Eycken, Didier Robert Guy Gabriel de Chaffoy de Courcelles
  • Patent number: 5883111
    Type: Grant
    Filed: July 22, 1996
    Date of Patent: March 16, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takehiko Naka, Yoshiyuki Inada
  • Patent number: 5852168
    Abstract: The present invention provides a method for sulfurizing a phosphorus-containing compound, such as a trivalent phosphorus compound, using a disulfide-containing five-membered heterocycle.
    Type: Grant
    Filed: April 30, 1996
    Date of Patent: December 22, 1998
    Assignees: Regents of the University of Minesota, The Board of Supervisors of LA State University
    Inventors: George Barany, Robert P. Hammer, Karin Musier-Forsyth, Qinghong Xu, Lin Chen
  • Patent number: 5849216
    Abstract: Compounds of the formula (I)R.sup.1 --(A.sup.1).sub.a (--M.sup.1).sub.b --(--A.sup.2).sub.c (--M.sup.2).sub.d (--A.sup.3).sub.e (--M.sup.3).sub.f (--A.sup.4).sub.g --H(I)in which the symbols and indices have the following meanings:R.sup.1 is B or a straight-chain or branched alkyl radical having 1 to 22 carbon atoms (with or without an asymmetrical carbon atom) in which, in addition, it is possible for one or two non-adjacent --CH.sub.2 -- groups to be replaced by --O--, --S--, --CO--, --CO--O--, --O--CO--, --CO--S--, --S--CO--, --O--CO--O--, --CH.dbd.CH--, --C.tbd.C--, .DELTA. or --Si(CH.sub.3).sub.2 --, and in which, in addition, one or more hydrogen atoms of the alkyl radical may be substituted by F, Cl, Br or CN, or is a chiral group, for example an epoxide, a dioxolane or a cyclic lactone,--(A.sup.1).sub.a (--M.sup.1).sub.b --(--A.sup.2).sub.c (--M.sup.2).sub.d (--A.sup.3).sub.e (--M.sup.3).sub.f (--A.sup.4).sub.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: December 15, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerd Illian, Anke Kaltbeitzel, Rainer Wingen, Hubert Schlosser
  • Patent number: 5834468
    Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.
    Type: Grant
    Filed: July 2, 1996
    Date of Patent: November 10, 1998
    Assignee: Zeneca Limited
    Inventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
  • Patent number: 5827800
    Abstract: The invention relates to novel alkyl sulphinyl and alkyl sulphonyl-1,2,4-thiadiazolyloxy acetamides of formula (I) ##STR1## in which n is the numbers 1 or 2,R.sup.1 is hydrogen or possibly substituted alkyl, alkenyl, alkinyl or aralkyl,R.sup.2 is possibly substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, alkoxy, alkenyloxy or alkinyloxy, orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are bound form a possibly substituted, saturated or unsaturated nitrogen heterocycle which may contain other hetero atoms and to which a benzo group may be annellated, andR.sup.3 is possibly substituted alkyl, aryl or arylalkyl,and also processes and novel intermediate products for producing the novel compounds and their use as herbicides.
    Type: Grant
    Filed: October 25, 1996
    Date of Patent: October 27, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz Forster, Hans-Joachim Santel, Markus Dollinger
  • Patent number: 5736555
    Type: Grant
    Filed: July 22, 1996
    Date of Patent: April 7, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takehiko Naka, Yoshiyuki Inada
  • Patent number: 5736561
    Abstract: This invention relates to a method for the prophylaxis or treatment of vascular hypertropy in a mammal by administering a pharmaceutically effective amount of a compound represented by the formula (I): ##STR1## wherein ring W is a nitrogen-containing heterocyclic ring residue which may be substituted; R.sup.1 is hydrogen or an optionally substituted hydrocarbon residue which optionally binds through a hetero-atom; R.sup.3 represents a group capable of forming an anion or a group capable of changing thereto; X shows that the phenylene and phenyl groups bind to each other directly or through a spacer having an atomic length of two or less; n denotes 1 or 2; a and b forming the heterocyclic ring residue are independently one or two optionally substituted carbon or hetero atoms; c is an optionally substituted carbon or hetero atom; provided that, when the ring W is a condensed ring, R.sup.
    Type: Grant
    Filed: January 18, 1996
    Date of Patent: April 7, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventor: Kohei Nishikawa
  • Patent number: 5728737
    Abstract: The present invention relates to novel N-alkoxy-arnidine derivatives of the formula (I), to a process for their preparation and to their use as pesticides. In addition, the invention also relates to novel intermediates and to a process for their preparation.
    Type: Grant
    Filed: January 23, 1997
    Date of Patent: March 17, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Bernd-Wieland Kruger, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
  • Patent number: 5703065
    Abstract: The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein A, W, P, R.sup.3, Q and R.sup.1 are as defined herein. The compounds of formula I, and pharmaceutically acceptable salts thereof, are substance P antagonists and as such are useful in the treament of various inflammatory and central nervous system disorders.
    Type: Grant
    Filed: May 7, 1996
    Date of Patent: December 30, 1997
    Assignee: Pfizer Inc.
    Inventor: Harry R. Howard, Jr.
  • Patent number: 5686621
    Abstract: Substituted hydrindanes and their use in controlling angiogenesis-dependent diseases in warm blooded animals are disclosed.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 11, 1997
    Assignee: Alcon Laboratories, Inc.
    Inventors: Abbot F. Clark, Raymond E. Conrow
  • Patent number: 5674894
    Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.
    Type: Grant
    Filed: May 15, 1995
    Date of Patent: October 7, 1997
    Assignee: G.D. Searle & Co.
    Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
  • Patent number: 5650419
    Abstract: Described herein are compounds of the formula; ##STR1## wherein: Thi is a unsubstituted or substituted thiadiazolyl;Y is an alkylene bridge of 3-9 carbon atoms;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxylcarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.3 is alkoxycarbonyl, substituted or unsubstituted phenyl, alkyltetrazolyl or a substituted or unsubstituted imidazolyl, dihydroimidazolyl, pyrazolyl, furyl, thiazolyl or thienyl or a pharmaceutically acceptable salt thereof are effective antipicornaviral agents.
    Type: Grant
    Filed: August 30, 1996
    Date of Patent: July 22, 1997
    Assignee: Sanofi, S.A.
    Inventors: David J. Aldous, Thomas R. Bailey, Guy Dominic Diana, Theodore J. Nitz
  • Patent number: 5641796
    Abstract: Antihyperglycemic compounds selected from the group consisting of C-substituted pentacycloazoles and N-alkyl-substituted pentacycloazoles.
    Type: Grant
    Filed: November 1, 1994
    Date of Patent: June 24, 1997
    Assignee: Eli Lilly and Company
    Inventors: Samuel J. Dominianni, Lora L. Fitch, Klaus K. Schmiegel
  • Patent number: 5622971
    Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: April 22, 1997
    Assignee: Abbott Laboratories
    Inventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen
  • Patent number: 5596012
    Abstract: Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula ##STR1## wherein: L is --O--, --S--, --SO--or --SO.sub.2 --;m and n are each independently 0 or 1;R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substituted heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl; R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; andR.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: January 21, 1997
    Assignee: Sterling winthrop Inc.
    Inventors: Richard P. Dunlap, Neil W. Boaz, Albert J. Mura, Dennis J. Hlasta, Ranjit C. Desai, Chakrapani Subramanyam, Lee H. Latimer, Eric P. Lodge
  • Patent number: 5583141
    Type: Grant
    Filed: August 16, 1994
    Date of Patent: December 10, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takehiko Naka, Yoshiyuki Inada
  • Patent number: 5569655
    Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: October 29, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
  • Patent number: 5567725
    Abstract: Cyclohexanol esters of the formula I ##STR1## are described in which the radicals have the given meaning. The compounds are pharmacologically active and may therefore be used as pharmaceuticals, in particular for treating diabetes and other diseases which are characterized by an elevated secretion of glucose from the liver or by an elevated activity of the glucose-6-phosphatase system.
    Type: Grant
    Filed: February 14, 1995
    Date of Patent: October 22, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Horst Hemmerle, Gerrit Schubert, Peter Below, Andreas Herling, Hans-J org Burger
  • Patent number: 5547967
    Abstract: 3-(Phenylalkylaminoalkylozy)-heteroaryl compounds having heart rate lowering and/or anti-ischemic effects, methods for their preparation and pharmaceutical compositions containing them are described. The compounds correspond to the general formula I ##STR1## or to the general formula XXXI ##STR2## in which the substituents have the meanings given the specification.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 20, 1996
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Wolfgang Kehrbach, Michael Mlinaric, Dieter Ziegler, Reinhard Brueckner, Willi Bielenberg
  • Patent number: 5523312
    Abstract: Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: September 27, 1994
    Date of Patent: June 4, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Gee-Hong Kuo, Theodore J. Nitz, Michael Reuman
  • Patent number: 5521186
    Abstract: The present invention provides novel compounds of formula ##STR1## the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof, wherein A and B taken together form a bivalent radical of formula: --N.dbd.CH-- (a), --CH.dbd.N-- (b), --CH.sub.2 --CH.sub.2 -- (c), --CH.dbd.CH-- (d) --C(.dbd.O)--CH.sub.2 -- (e), --CH.sub.2 --C(.dbd.O)-- (f); R.sup.1 is hydrogen, C.sub.1-6 alkyl, or halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-6 cycloalkyl or C.sub.1-8 alkyl substituted with hydroxy, oxo, C.sub.3-6 cycloalkyl or aryl. Het is five- or six-membered optionally substituted heterocyclic ring. The use as a medicine, especially as a lipid lowering agent is disclosed as well as pharmaceutical compositions and processes for preparing compounds and compositions.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: May 28, 1996
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Leo J. J. Backx, Robert J. M. Hendrickx, Luc A. L. Van Der Eycken, Didier R. G. G. De Chaffoy De Courcelles
  • Patent number: 5500427
    Abstract: The present invention relates to a compounds represented by the following formula or salts thereof. ##STR1## The above compounds have strong angiotensin II antagonistic action, antihypertensive action and action on central nervous system, which are useful for the treatment of circulatory diseases such as hypertension, heart diseases, cerebral apoplexy, nephritis, atherosclerosis or Alzheimer's disease and senile dementia, and for agents of improving cerebral function.
    Type: Grant
    Filed: September 14, 1993
    Date of Patent: March 19, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Keiji Kubo, Yoshiyuki Inada, Takehiko Naka
  • Patent number: 5494925
    Abstract: 2-Heterocyclyloxymethyl and 2-heterocyclylthiomethyL-1,2,5-thiadiazolidin-3-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
    Type: Grant
    Filed: December 2, 1994
    Date of Patent: February 27, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: John J. Court, Ranjit C. Desai, Dennis J. Hlasta
  • Patent number: 5482966
    Abstract: The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: January 9, 1996
    Assignees: Zeneca Limited, Zeneca Pharma S.A.
    Inventors: Thomas G. C. Bird, Patrick Ple
  • Patent number: 5481013
    Abstract: Compounds of the formula ##STR1## in which A is oxygen, sulfur or --NR.sub.1 --;B is C.sub.2 -C.sub.6 alkylene,D-E is --O--E, --S--E, --O--CH.sub.2 --E, --O--C(.dbd.O)--E, --O--C(.dbd.O)--O--E, --O--C(.dbd.O)--N(H)--E or --O--C(.dbd.S)--N(H)--E;E is phenyl; phenyl which is substituted by one to three substituents; a five-membered aromatic heterocycle having one to three hetero atoms; a five-membered aromatic heterocycle which has one to three hetero atoms and which is substituted by one or two substituents; a six-membered aromatic heterocycle which has one to three nitrogen atoms; or a six-membered aromatic heterocycle which has one to three nitrogen atoms and which is substituted by one or two substituents;L is halogen or methyl;X is fluorine;Y is chlorine or fluorine;Z is hydrogen, fluorine or methyl;m is the number zero, one, two, three, four or five;n is the number zero, one or two andR.sub.1 is hydrogen, C.sub.1 -C.sub.
    Type: Grant
    Filed: June 23, 1993
    Date of Patent: January 2, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Maienfisch, Thomas Pitterna, Manfred Boger