Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly To The Nitrogen By Nonionic Bonding Patents (Class 548/139)
  • Patent number: 6225323
    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: August 11, 1998
    Date of Patent: May 1, 2001
    Assignee: Joseph Koziak
    Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
  • Patent number: 6150385
    Abstract: The present invention presents novel 1,3,4-thiadiazole derivatives of formula I ##STR1## which have useful antiviral activity against herpes virus, cytomegalovirus (CMV).
    Type: Grant
    Filed: March 16, 1999
    Date of Patent: November 21, 2000
    Assignee: Pharmacia & Upjohn Company
    Inventors: Suvit Thaisrivongs, Steven Ronald Turner
  • Patent number: 5977373
    Abstract: The present invention provides thiadiazolyl and oxadiazolyl phenyl oxzolidinone compounds of formula I ##STR1## wherein Q is thiadiazolyl or oxadiazolyl; wherein X.sup.1 and X.sup.2 are independently hydrogen, fluorine or chlorine; andwherein R.sup.1 is, for example, --COCH.sub.3 or --COCH.sub.2 CH.sub.3.These compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive and gram-negative aerobic bacteria.
    Type: Grant
    Filed: July 8, 1998
    Date of Patent: November 2, 1999
    Assignee: Pharmacia & Upjohn Company
    Inventors: Robert C. Gadwood, Lisa Marie Thomasco, David John Anderson
  • 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: 5965738
    Abstract: Described is a process for producing an N-biphenyl-methylthiadiazoline derivative (7) in accordance with the reaction formula described below. According to the process of the present invention, it is possible to produce a compound (7) advantageously from the industrial viewpoint.
    Type: Grant
    Filed: March 20, 1997
    Date of Patent: October 12, 1999
    Assignee: Wakunaga Seiyaku Kabushiki Kaisha
    Inventors: Satoshi Inoue, Nobuya Sakae, Masaharu Yokomoto, Kouji Nishimura, Terukage Hirata
  • Patent number: 5912353
    Abstract: The present invention relates to a process for producing a tetrazolylated biphenylmethane derivatives (6) or salts thereof in accordance with the below-described reaction scheme wherein R.sup.1 represents an alkyl; R.sup.2 represents H, etc.; Z represents a halogen, etc.; and A represents a cycloalkene, etc. According to the above process, a tetrazolylated biphenylmethane derivative can be industrially and advantageously produced with short steps.
    Type: Grant
    Filed: December 23, 1997
    Date of Patent: June 15, 1999
    Assignee: Wakunaga Seiyaku Kabushiki Kaisha
    Inventors: Satoshi Inoue, Kouji Nishimura, Masaharu Yokomoto, Nobuya Sakae, Terukage Hirata
  • Patent number: 5912258
    Abstract: A thiadiazoleamide derivative or a salt thereof expressed by the following Formula 1: ##STR1## wherein each of R.sub.1 and R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylamino group or an alkenyloxy group; wherein when either R.sub.1 or R.sub.2 is a hydrogen atom, the other is not a hydrogen atom; R.sub.3 represents a lower alkyl group, an aryl group, a pyridyl group or --N(R.sub.4)R.sub.5, wherein R.sub.4 and R.sub.5 represent lower alkyl groups or together represent a saturated heterocyclic ring having 4-8 members; wherein when R.sub.1 or R.sub.2 is a lower alkoxy group, R.sub.3 is --N(R.sub.4)R.sub.5 or a pyridyl group; and n represents an integer of 1-3. The derivatives have anti-ulcer effect to be available for preventing or curing ulcers in mammals.
    Type: Grant
    Filed: September 21, 1998
    Date of Patent: June 15, 1999
    Assignee: Shiseido Co., Ltd.
    Inventors: Chikao Nishino, Fumitaka Sato, Tomohiro Uetake, Hirotada Fukunishi, Nao Kojima
  • Patent number: 5847149
    Abstract: Thiadiazole derivatives of the formula (I)X-B-A.sup.1 -(M.sup.1 -A.sup.2 -).sub.m (M.sup.2 -A.sup.3).sub.n -R.sup.1(I )in which the symbols and indices have the following meanings:X is Cl, Br or I;B is 1,3,4-thiadiazole-2,5-diyl;A.sup.1, A.sup.2 and A.sup.3 are identical or different and are substituted or unsubstituted 1,4-phenylene, pyrazine-2,5-diyl, pyridazine-3,6-diyl, pyridine-2,5-diyl, pyrimidine-2,5-diyl, trans-1,4-cyclohexylene, 1,3,4-thiadiazole-2,5-diyl, 1,3-dioxane-2,5-diyl, 1,3-dithiane-2,5-diyl, 1,3-thiazole-2,4-diyl, 1,3-thiazole-2,5-diyl, thiophene-2,4-diyl, thiophene-2,5-diyl, piperazine-1,4-diyl, piperazine-2,5-diyl, naphthalene-2,6-diyl, bicyclo?2.2.2!octane-1,4-diyl, or 1,3-dioxaborinane-2,5-diyl;M.sup.1 and M.sup.2 are identical or different and are --CO--O--, --O--CO--, --O--CO--O--, --O--CS--O--, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C-- or a single bond;R.sup.
    Type: Grant
    Filed: July 16, 1996
    Date of Patent: December 8, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Robert Walter Fuss, Javier Manero, Hubert Schlosser, Rainer Wingen
  • Patent number: 5830869
    Abstract: The present invention provides novel thiadiazole amide derivatives represented by formula I ##STR1## The compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, predominantly stromelysins, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthritis, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis, periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, inflammation and other diseases related to connective tissue degradation.
    Type: Grant
    Filed: June 18, 1997
    Date of Patent: November 3, 1998
    Inventors: Mark Allen Mitchell, Heinrich Josef Schostarez, Linda Louise Maggiora, Thomas J. Lindberg
  • Patent number: 5747514
    Abstract: The present invention relates to therapeutically active hydroxamic acid and carboxylic acid derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to the use of such compounds in medicine. In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation, and in addition are inhibitors of the release of tumor necrosis factor from cells.
    Type: Grant
    Filed: July 19, 1996
    Date of Patent: May 5, 1998
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Raymond Paul Beckett, Mark Whittaker, Andrew Miller, Fionna Mitchell Martin
  • Patent number: 5677282
    Abstract: Amino acid amides of 5-amino-1,3,4-thiadiazole-2-thione are disclosed. These compounds inhibit matrix metalloproteinase enzymes and cartilage degradation. Methods of treating diseases caused by over-activity of matrix metalloproteinases, such as osteoarthritis and rheumatoid arthritis, are also disclosed.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 14, 1997
    Assignee: Proscript, Inc.
    Inventors: Jozef Oleksyszyn, Alan R. Jacobson
  • Patent number: 5627198
    Abstract: The invention relates to heterocyclic amides of the formula ##STR1## in which the radicals A, Z, A.sub.1, R.sub.1, R.sub.2 and R.sub.3 are as defined in the description, to a process for the preparation of these amides and to their use as active substances for the curing and amelioration of disorders and diseases which can be treated by exerting influence on potassium channels.
    Type: Grant
    Filed: December 4, 1995
    Date of Patent: May 6, 1997
    Assignee: Hafslund Nycomed Pharma Aktiengesellschaft
    Inventors: Peter Esch, Robertson Towart, Franz Rovenszky
  • Patent number: 5538991
    Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.
    Type: Grant
    Filed: September 14, 1994
    Date of Patent: July 23, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Linda L. Chang, William J. Greenlee
  • Patent number: 5516442
    Abstract: A rust and corrosion inhibiting marine diesel engine lubricating oil additive is provided which comprises a mixture of:(a) an oligomeric polythiocyclic imide represented by the formula ##STR1## wherein R and R.sup.1 each are a (C.sub.1 -C.sub.50) saturated or unsaturated aliphatic group and n is an integer of 0 to 5; an oligomeric amine represented byR"--NH.sub.2where R" is dodecyl or a (C.sub.12 -C.sub.
    Type: Grant
    Filed: August 11, 1995
    Date of Patent: May 14, 1996
    Assignee: Texaco Inc.
    Inventors: Joseph M. Russo, Rodney L. Sung, Benjamin J. Kaufman, Thomas F. Derosa
  • Patent number: 5512588
    Abstract: This invention relates to furylthiazole derivatives represented by the following formula: ##STR1## wherein each symbol is as defined in the specification and pharmaceutically acceptable salts thereof which have antiulcer activity, H.sub.2 -receptor antagonism and antimicrobial activity, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of ulcer and infectious diseases in human being or animals.
    Type: Grant
    Filed: January 28, 1994
    Date of Patent: April 30, 1996
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hisashi Takasugi, Yousuke Katsura, Yoshikazu Inoue, Tetsuo Tomishi
  • Patent number: 5457122
    Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.
    Type: Grant
    Filed: July 13, 1993
    Date of Patent: October 10, 1995
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
  • Patent number: 5412117
    Abstract: Benzopyran derivatives represented by formula (I): ##STR1## wherein X represents =O, =S, =N-Z (Z represents a lower alkyl group, etc.), or =CHNO.sub.2 ; Y represents a substituted amino group, an alkoxy group, an alkylthio group, etc., and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 each represent a hydrogen atom, a lower alkyl group, etc., are disclosed. The benzopyran derivatives exhibit K.sup.+ channel activating activities and are widely applicable as antiasthmatics, antiepileptics, and the like.
    Type: Grant
    Filed: January 26, 1993
    Date of Patent: May 2, 1995
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroshi Koga, Hiroyuki Nabata
  • Patent number: 5401853
    Abstract: Thiadiazole derivatives of general formula (I) ##STR1## wherein R.sub.1 is selected from the class consisting of: C.sub.1 -C.sub.10 linear or branched alkyl, benzyl, optionally substituted at the aromatic ring with one or more groups selected on their turn from the class consisting of : C.sub.1 -C.sub.20 linear or branched alkyl residues , nitro groups, halogen atoms, C.sub.1 -C.sub.20 linear or branched alkoxy, hydroxy and C.sub.2 -C.sub.20 linear or branched acyloxy groups, R.sub.2 is selected from H, C.sub.2 -C.sub.10 alkanoyl, cycloalkanoyl wherein this ring has from 3 to 10 carbon atoms, aroyl, and R.sub.3 is selected from H and C.sub.1 -C.sub.10 alkyl, for the treatment of depressive states and anxiety, a process for their preparation and relative pharmaceutical compositions containing them as the active ingredient.
    Type: Grant
    Filed: July 9, 1993
    Date of Patent: March 28, 1995
    Assignee: Laboratorio Farmaceutico C.T. S.r.l.
    Inventors: Mario Brufani, Antonella Loche, Vincenzo Perlini, Donato Pocar
  • Patent number: 5350856
    Abstract: This invention relates to a process for producing a compound of the formula ##STR1## comprising reacting a compound having the formula ##STR2## with cyanogen chloride or cyanogen bromide.
    Type: Grant
    Filed: January 10, 1990
    Date of Patent: September 27, 1994
    Assignee: ICI Americas Inc.
    Inventor: Raymond A. Felix
  • Patent number: 5344927
    Abstract: A tetrahydrobenzimidazole derivative represented by formula (I): ##STR1## wherein Het represents a heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxy group, a nitro group, a hydroxyl group, a lower alkoxycarbonyl group, and a halogen atom; and X represents a single bond or --NH-- which is bonded to the carbon atom or nitrogen atom of the heterocyclic ring, or a pharmaceutically acceptable salt thereof.The compound of formula (I) and a salt thereof exhibits antagonism against 5-HT.sub.3 receptor.
    Type: Grant
    Filed: March 30, 1993
    Date of Patent: September 6, 1994
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Mitsuaki Ohta, Tokuo Koide, Takeshi Suzuki, Akira Matsuhisa, Keiji Miyata, Junya Ohmori, Isao Yanagisawa
  • Patent number: 5312926
    Abstract: Indonaphthol thermal transfer dyes have the formula ##STR1## where X is nitrogen or the radical CH,R.sup.1 and R.sup.2 are each independently of the other C.sub.1 -C.sub.6 -alkyl, which may be substituted, C.sub.1 -C.sub.6 -monooxaalkyl or -dioxaalkyl or allyl,R.sup.3 and R.sup.4 are each independently of the other hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -alkanoylamino, andR.sup.5 is five-membered hetaryl which is not benzofused and has two or more hetero atoms,with the proviso that R.sup.1 and R.sup.2 are not both unsubstituted C.sub.1 -C.sub.6 -alkyl at one and the same time.
    Type: Grant
    Filed: March 29, 1991
    Date of Patent: May 17, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Volker Bach, Karl-Heinz Etzbach, Ruediger Sens
  • Patent number: 5288735
    Abstract: Method of treating glaucoma in a mammal, comprising administering to the mammal an effective amount of an active water-soluble carbonic anhydrase inhibitor having the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is selected from the group consisting of H, --OH, --CN and --OCH.sub.3, R.sup.2 is methyl or a lower alkyl having from two to about 5 carbon atoms, R.sup.3 is selected from the group consisting of NHCHR.sup.4 --, R.sup.5 NHCHR.sup.4 --, R.sup.5 NHCHR.sup.4 --, ##STR2## R.sup.4 is selected from lower alkyl having from one to about five carbon atoms, or a naturally occurring amino acid side-chain, and R.sup.5 is selected from the group consisting of H, CH.sub.3 --, HCO--, CH.sub.3 CO-- and X--CH.sub.2 CO-- wherein X is a halogen atom and stereoisomers thereof.
    Type: Grant
    Filed: June 15, 1992
    Date of Patent: February 22, 1994
    Inventors: Seymour F. Trager, G. Michael Blackburn
  • Patent number: 5242937
    Abstract: The present invention is directed to a compound of the formula: ##STR1## or pharmaceutically acceptable salts thereof which are useful in the treatment of glaucoma and in the assessment of corneal function.
    Type: Grant
    Filed: March 19, 1990
    Date of Patent: September 7, 1993
    Assignee: Research Corporation Technologies, Inc.
    Inventor: William M. Pierce, Jr.
  • Patent number: 5225424
    Abstract: N-[5-(aminosulfonyl)-3-methyl-1,3,4-thiadiazol-2(3H)ylidene] -2-acetyloxyacetamide, commonly referred to as acetylhydroxymethazolamide and is a water soluble pharmacologically active carbonic anhydrase inhibitor.
    Type: Grant
    Filed: October 21, 1992
    Date of Patent: July 6, 1993
    Assignee: University of Iowa Research Foundation
    Inventors: Ronald D. Schoenwald, Charles F. Barfknecht
  • Patent number: 5223616
    Abstract: A heterocyclic compound which is useful for dyeing or printing hydrophobic fiber materials and which has the following formula (I), ##STR1##wherein A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are each hydrogen, halogen, alkyl, alkoxy or alkenyl, X.sub.1 is --O-- or the like, R.sub.1 is a methylene or the like, X.sub.2 is a direct linkage or a divalent group of --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## in which R.sub.3 is a hydrogen atom or a C.sub.1-4 alkyl group, ##STR3## in which R.sub.3 is as defined above, T and u are each independently hydrogen or a C.sub.1-4 alkyl, l is O or an integer of 1 to 3, Q is an unsubstituted or substituted 5-, 6- or 7-membered saturated or unsaturated heterocyclic residue, Y is hydrogen, C.sub.1-4 alkyl, a C.sub.1-4 alkoxy group or the like.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: June 29, 1993
    Assignee: Sumitomo Chemical Company, Ltd.
    Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
  • Patent number: 5176739
    Abstract: Dicarboximides of the formulae Ia, Ib and Ic ##STR1## where X is oxygen or sulfur, R.sup.1 is hydrogen, halogen, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, haloalkoxy, haloalkylthio, alkylsulfonyl, haloalkylsulfonyl, phenyl, phenylalkyl, phenoxy or phenylthio, a 5-membered or 6-membered saturated or aromatic heterocyclic radical containing one or two hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen, where the stated organic radicals may be further substituted, andR.sup.2 is hydrogen, hydroxyl, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, di-C.sub.1 -C.sub.
    Type: Grant
    Filed: June 21, 1991
    Date of Patent: January 5, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Volker Maywald, Klaus Ditrich, Thomas Kuekenhoehner, Gerhard Hamprecht, Wolfgang Freund, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
  • Patent number: 5158950
    Abstract: 2-(1,3-Dithiol-2-ylidene)-2-[N-(substituted) carbamoly] acetate esters and salts thereof, having potent therapeutic or prophylactic effect for hepatic disorder, are provided. Processes for their preparation and intermediates in their preparation also are disclosed.
    Type: Grant
    Filed: May 23, 1990
    Date of Patent: October 27, 1992
    Assignee: Yuhan Corporation, Ltd.
    Inventors: Choong S. Kim, Jeong S. Chae, Young R. Choi, Jong W. Lee, Joung K. Yoo
  • Patent number: 5157044
    Abstract: Analogs are prepared of the carbonic anhydrase inhibitors methazolamide, and dichlorphenamide. The analogs link a cleavable functional group to the pharmacologically active carbonic anhydrase inhibitor resulting in compounds of improved corneal permeability, which are non-irritable to the eye and which are effective topically to inhibit intraocular pressure.
    Type: Grant
    Filed: June 11, 1990
    Date of Patent: October 20, 1992
    Assignee: University of Iowa Research Foundation
    Inventors: Ronald D. Schoenwald, Charles F. Barfknecht
  • Patent number: 5155122
    Abstract: The present invention is novel compounds which are 3,5-di-tertiary-butyl-4-hydroxyphenyl substituted 1,2,4- and 1,3,4-thiadazoles and oxadiazoles, and 1,2,4-triazoles, and pharmaceutically acceptable additions and base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are now found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever, and the like.
    Type: Grant
    Filed: August 23, 1991
    Date of Patent: October 13, 1992
    Assignee: Warner-Lambert Company
    Inventors: David T. Connor, Daniel L. Flynn, Catherine R. Kostlan, Michael D. Mullican, Gary P. Shrum, Paul C. Unangst, Michael W. Wilson
  • Patent number: 5103007
    Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.
    Type: Grant
    Filed: October 27, 1989
    Date of Patent: April 7, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
  • Patent number: 5081245
    Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.
    Type: Grant
    Filed: August 18, 1989
    Date of Patent: January 14, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
  • Patent number: 4975446
    Abstract: Method and formulation useful in treatment of glaucoma in a mammal wherein an effective amount of an active water soluble carbonic anhydrase inhibitor is administered, said inhibitor being a compound having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is selected from the group consisting of H, --OH, --CN and --OCH.sub.3 ; R.sup.2 is hydrogen or a lower alkyl having from one to about 5 carbon atoms; R.sup.3 is selected from the group consisting of HNHCHR.sup.4 --, R.sup.5 NHCHR.sup.4 --, R.sup.5 NHCHR.sup.4, CONHCR.sup.4 --, R.sup.5 NHCH.sub.2 CHR.sup.4 --, ##STR2## R.sup.4 is selected from lower alkyl having from one to about 5 carbon atoms; or a naturally occurring amino acid side chain; and R.sub.5 is selected from the group consisting of H, CH.sub.3 --, HCO--, CH.sub.3 CO-- and XCH.sub.2 CO-- wherein X is a halogen atom; and stereoisomers thereof.
    Type: Grant
    Filed: May 2, 1989
    Date of Patent: December 4, 1990
    Inventors: Seymour F. Trager, G. Michael Blackburn
  • Patent number: 4948891
    Abstract: Compounds of the formula ##STR1## where Het is a heterocyclic group, n is an integer of 0 to 2 and R.sup.1 is hydrogen or lower alkyl are protease inhibitors useful as anti-plasmin and anti-thrombin agents.
    Type: Grant
    Filed: August 9, 1989
    Date of Patent: August 14, 1990
    Assignee: Pfizer Inc.
    Inventors: Rodney C. Schnur, Anton F. J. Fliri
  • Patent number: 4912224
    Abstract: An antibacterial 7beta-(carboxyalkenoyl)amino-3-cephem-4-carboxylic acid represented by the following formula: ##STR1## (wherein R is aryl or a heterocyclic group;R.sup.1 is hydrogen or halogen;R.sup.2 is a single bond, alkylene, or thiaalkylene;R.sup.3 is a hydrogen atom or carboxy modifying group;R.sup.4 is hydrogen or methoxy;R.sup.5 is hydrogen or a 3-substituent of cephalosporins;R.sup.6 is a hydrogen atom or carboxy modifying group; andX is oxygen, sulfur, or sulfinyl)a pharmaceutical composition containing the same, and a method for treating a bacterial infection with the same.
    Type: Grant
    Filed: December 9, 1987
    Date of Patent: March 27, 1990
    Assignee: Shionogi & Co., Ltd.
    Inventor: Yoshio Hamashima
  • Patent number: 4911745
    Abstract: Novel herbicides are 3-(substituted) phenyl-2-(substituted imino)-1,3,4-dihydrothiadiazoles. Also disclosed are intermediates for such compounds, and processes for producing the herbicidal compounds and their intermediates.
    Type: Grant
    Filed: July 8, 1988
    Date of Patent: March 27, 1990
    Assignee: ICI Americas Inc.
    Inventor: Raymond A. Felix
  • Patent number: 4874864
    Abstract: Compounds of the formula ##STR1## where HET is a heterocyclic group, n is an integer of 0 to 2 and R.sup.1 is hydrogen or lower alkyl are protease inhibitors use as anti-plasmin and anti-thrombin agents.
    Type: Grant
    Filed: May 24, 1988
    Date of Patent: October 17, 1989
    Assignee: Pfizer Inc.
    Inventors: Rodney C. Schnur, Anton F. J. Fliri
  • Patent number: 4855310
    Abstract: Novel heterocyclic compounds shown by the general formula ##STR1## or the pharmaceutically acceptable salts thereof useful as medicament in particular as antagonist of slow reacting substance of anaphylaxis (SRS-A).
    Type: Grant
    Filed: March 25, 1988
    Date of Patent: August 8, 1989
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Murase, Toshiyasu Mase, Hiromu Hara, Kenichi Tomioka
  • Patent number: 4845230
    Abstract: Herbicidally active novel 2,5-dihydropyrroles of the formula ##STR1## wherein R.sup.1 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, R.sup.2 and R.sup.3 each represent an alkyl group having 1 to 4 carbon atoms or a haloalkyl group having 1 to 4 carbon atoms or together may form a C.sub.2 -C.sub.6 alkylene group which may be substituted by halogen, and R represents a hydroxy group, a mercapto group, a halogen atom, an amino group or a group of the formula --O--W in which W represents an alkylcarbonyl, a halogenoalkylcarbonyl, an alkoxycarbonyl or a halogenoalkoxycarbonyl group each having 1 to 4 carbon atoms in the alkyl group, an alkylsulfonyl or a halogenoalkylsulfonyl group each having 1 to 4 carbon atoms in the alkyl group or a di-C.sub.1 -C.sub.4 -alkylamino sulfonyl group.
    Type: Grant
    Filed: November 22, 1988
    Date of Patent: July 4, 1989
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Shigeki Yagi, Hiroshi Miyauchi
  • Patent number: 4828604
    Abstract: Herbicidally active novel 2,5-dihydropyrroles of the formula ##STR1## wherein R.sup.1 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, R.sup.2 and R.sup.3 each represent an alkyl group having 1 to 4 carbon atoms or a haloalkyl group having 1 to 4 carbon atoms or together may form a C.sub.2 -C.sub.6 alkylene group which may be substituted by halogen, and R represents a hydroxy group, a mercapto group, a halogen atom, an amino group or a group of the formula --O--W in which W represents an alkylcarbonyl, a halogenoalkylcarbonyl, an alkoxycarbonyl or a halogenoalkoxycarbonyl group each having 1 to 4 carbon atoms in the alkyl group, an alkylsulfonyl or a halogenoalkylsulfonyl group each having 1 to 4 carbon atoms in the alkyl group or a di-C.sub.1 -C.sub.4 -alkylamino sulfonyl group.
    Type: Grant
    Filed: March 9, 1988
    Date of Patent: May 9, 1989
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Shigeki Yagi, Hiroshi Miyauchi
  • Patent number: 4803211
    Abstract: This invention relates to novel heterocyclic compounds structurally characterized by containing a specific heterocyclic group and by the presence of --CH.sub.2 --S-- directly bound to the specific heterocyclic group. These heterocyclic compounds are useful as medicines, particularly as antagonists of SRS-A (slow reacting substance of anaphylaxis).
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: February 7, 1989
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Toshiyasu Mase, Ryuji Tsuzuki, Hiromu Hara, Kiyoshi Murase, Kenichi Tomioka
  • Patent number: 4801718
    Abstract: N-Aryl benzamides wherein the aryl group is a nitrogen containing heterocycle are useful as selective herbicidal agents. Compositions containing the novel benzamides and a herbicidal method of selective weed control are disclosed.
    Type: Grant
    Filed: December 5, 1985
    Date of Patent: January 31, 1989
    Assignee: Eli Lilly and Company
    Inventor: Kenneth W. Burow, Jr.
  • Patent number: 4746745
    Abstract: Process and composition for reducing intraocular pressure and reducing aqueous humor formation by applying topically to the cornea an effective amount of an aqueous solution of a caronic anhydrase inhibitor comprising a sulfonamide having the following properties:a. sufficiently soluble in water to form at least a 3 mM solution at pH 8.2 or a pKa of not greater than 7.3;b. ether partition coefficient of at least 1.0;c. chloroform partition coefficient of at least 0.01;d. dissociation constant against carbonic anhydrase of not more than 3.times.10.sup.-8 molar;e. first order rate constant for penetration of the sulfonamide through a living rabbit cornea of at least 0.005 hr.sup.-1 ;f. not injurious to the cornea; andg. stable in aqueous solution and in contact with the cornea.
    Type: Grant
    Filed: June 19, 1986
    Date of Patent: May 24, 1988
    Inventor: Thomas H. Maren
  • Patent number: 4742060
    Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.
    Type: Grant
    Filed: January 21, 1986
    Date of Patent: May 3, 1988
    Assignee: Nihon Tokushu Noyaku Seizo K. K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
  • Patent number: 4739083
    Abstract: A new process for preparing a pyrone-3-carboxamide compound of the formula (IV): ##STR1## wherein R.sub.1 is aryl or heterocyclic group optionally substituted, R.sub.2 is alkyl, aralkyl or like group, comprising reacting a compound of the formula (I) or (I'): ##STR2## wherein R.sub.3 is dialkylamino group and n is 0 to 6, and R.sub.1 and R.sub.2 are as above,with a compound of the formula (II): ##STR3## wherein R.sub.4 and R.sub.5 are hydrogen atom, alkyl or like group, or reacting a compound of the formula (III): ##STR4## wherein R.sub.6 is alkyl, aryl or like group, and R.sub.1 and R.sub.2 are as above,with a compound of the formula (II) or diketene in the presence of a tertiary organic base.
    Type: Grant
    Filed: January 2, 1986
    Date of Patent: April 19, 1988
    Assignee: Daicel Chemical Industries Ltd.
    Inventors: Yoichiro Ueda, Yukihisa Goto, Kazuhisa Masamoto
  • Patent number: 4703125
    Abstract: A carbonyl compound of the formula ##STR1## in which R.sup.1 denotes hydrogen, aryl, substituted aryl or a straight-chain or cyclic, saturated or unsaturated aliphatic hydrocarbon radical, which is optionally interrupted by O, S, N, N-alkyl, N-aryl or N-aralkyl, and which is optionally substituted by hydroxyl, alkoxy, alkyl, trifluoromethyl, halogen, phenyl, alkoxycarbonyl or dialkylamino, the two alkyl radicals together with the nitrogen atom optionally forming a 5 to 7-membered ring, which optionally contains a heteroatom from the group comprising O, S, NH or N-alkyl and these aforementioned alkyl and phenyl radicals in turn optionally being substituted by halogen, trifluoromethyl, alkyl, aryl, aralkyl, alkoxy, alkylmercapto or SO.sub.2 -alkyl,R.sup.2 represents the radical CXR.sup.8, R.sup.8 having the meaning indicated for R.sup.1 and being identical to or different from R.sup.1, and X representing oxygen, sulphur or the radical NR.sup.9 R.sup.10, R.sup.9 and R.sup.
    Type: Grant
    Filed: July 1, 1986
    Date of Patent: October 27, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Axel Ingendoh, Horst Meyer, Bernward Garthoff
  • Patent number: 4695571
    Abstract: Tricyclic oxindole carboxamides, prepared by (a) reaction of an isocyanate with the basic ring system or (b) ammonolysis of a corresponding alkyl ester, are non-steroidal antiinflammatory agents useful in the treatment of rheumatoid arthritis.
    Type: Grant
    Filed: April 2, 1986
    Date of Patent: September 22, 1987
    Assignee: Pfizer Inc.
    Inventor: Lawrence S. Melvin
  • Patent number: 4686224
    Abstract: Ketone containing 1-substituted oxindole-3-carboxamides as antiinflammatory agents prepared by reaction of the 1-substituted oxindole with an isocyanate or by aminolysis of the corresponding alkyl oxindole-3-carboxylate.
    Type: Grant
    Filed: August 6, 1985
    Date of Patent: August 11, 1987
    Assignee: Pfizer Inc.
    Inventor: Lawrence S. Melvin, Jr.
  • Patent number: 4639526
    Abstract: 2-(alkyl, alkenyl and alkylmercapto)-5-[N-(alkanoyl, chloroalkanoyl, alkoxycarbonyl, phenoxy carbonyl, N'-[alkyl and alkenyl]-aminocarbonyl and N'-alkyl-N'-[alkyl and alkenyl]-aminocarbonyl)-amino]-1,3,4-thiadiazoles, i.e. 2-(alkyl, alkenyl and alkylmercapto)-5-[N-(alkanoylamino, chloroalkanoylamino, alkoxycarbonylamino, phenoxycarbonylamino, N'-[alkyl and alkenyl]-ureido and N'-alkyl-N'-[alkyl and alkenyl]-ureido)]-1,3,4-thiadiazoles, which possess herbicidal properties, and which may be produced by conventional methods.
    Type: Grant
    Filed: August 29, 1968
    Date of Patent: January 27, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Carl Metzger, Ludwig Eue, Helmuth Hack
  • Patent number: 4568752
    Abstract: Recording material for color photography, which contains, in at least one silver halide emulsion layer, at least one yellow coupler of the formula ##STR1## in which R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are alkyl, cycloalkyl or aryl, X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are radicals detachable during the coupling reaction and Y.sub.1 and Y.sub.2 are halogen, alkyl, alkoxy, alkylmercapto, --CN, --COOH, carbalkoxy, --NH.sub.2, --NHR.sub.5, --NR.sub.5 R.sub.6 or --NHCOR.sub.5, in which R.sub.5 and R.sub.6 are alkyl or phenyl, Z is a divalent bridge member and r is 1 or 2.Photographic colored images with excellent spectral absorption characteristics and good resistance to light, heat and moisture are obtained by exposing the recording material image-wise and developing.
    Type: Grant
    Filed: December 10, 1984
    Date of Patent: February 4, 1986
    Assignee: Ciba-Geigy AG
    Inventor: Mario Fryberg
  • Patent number: 4518414
    Abstract: Thiadiazole derivatives of the formula ##STR1## where R.sup.1, A, X, Y, Z, m and n have the meanings given in the description, are used for controlling undesirable plant growth.
    Type: Grant
    Filed: January 11, 1983
    Date of Patent: May 21, 1985
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulrich Schirmer, Peter Plath, Bruno Wuerzer