Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly To The Nitrogen By Nonionic Bonding Patents (Class 548/139)
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Patent number: 6225323Abstract: 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: GrantFiled: August 11, 1998Date of Patent: May 1, 2001Assignee: Joseph KoziakInventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
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Patent number: 6150385Abstract: 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: GrantFiled: March 16, 1999Date of Patent: November 21, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Suvit Thaisrivongs, Steven Ronald Turner
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Patent number: 5977373Abstract: 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: GrantFiled: July 8, 1998Date of Patent: November 2, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Robert C. Gadwood, Lisa Marie Thomasco, David John Anderson
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Patent number: 5977149Abstract: 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: GrantFiled: January 14, 1998Date of Patent: November 2, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
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Patent number: 5965738Abstract: 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: GrantFiled: March 20, 1997Date of Patent: October 12, 1999Assignee: Wakunaga Seiyaku Kabushiki KaishaInventors: Satoshi Inoue, Nobuya Sakae, Masaharu Yokomoto, Kouji Nishimura, Terukage Hirata
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Patent number: 5912353Abstract: 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: GrantFiled: December 23, 1997Date of Patent: June 15, 1999Assignee: Wakunaga Seiyaku Kabushiki KaishaInventors: Satoshi Inoue, Kouji Nishimura, Masaharu Yokomoto, Nobuya Sakae, Terukage Hirata
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Patent number: 5912258Abstract: 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: GrantFiled: September 21, 1998Date of Patent: June 15, 1999Assignee: Shiseido Co., Ltd.Inventors: Chikao Nishino, Fumitaka Sato, Tomohiro Uetake, Hirotada Fukunishi, Nao Kojima
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Patent number: 5847149Abstract: 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: GrantFiled: July 16, 1996Date of Patent: December 8, 1998Assignee: Hoechst AktiengesellschaftInventors: Robert Walter Fuss, Javier Manero, Hubert Schlosser, Rainer Wingen
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Patent number: 5830869Abstract: 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: GrantFiled: June 18, 1997Date of Patent: November 3, 1998Inventors: Mark Allen Mitchell, Heinrich Josef Schostarez, Linda Louise Maggiora, Thomas J. Lindberg
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Patent number: 5747514Abstract: 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: GrantFiled: July 19, 1996Date of Patent: May 5, 1998Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Mark Whittaker, Andrew Miller, Fionna Mitchell Martin
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Patent number: 5677282Abstract: 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: GrantFiled: June 7, 1995Date of Patent: October 14, 1997Assignee: Proscript, Inc.Inventors: Jozef Oleksyszyn, Alan R. Jacobson
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Patent number: 5627198Abstract: 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: GrantFiled: December 4, 1995Date of Patent: May 6, 1997Assignee: Hafslund Nycomed Pharma AktiengesellschaftInventors: Peter Esch, Robertson Towart, Franz Rovenszky
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Patent number: 5538991Abstract: 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: GrantFiled: September 14, 1994Date of Patent: July 23, 1996Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Linda L. Chang, William J. Greenlee
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Patent number: 5516442Abstract: 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: GrantFiled: August 11, 1995Date of Patent: May 14, 1996Assignee: Texaco Inc.Inventors: Joseph M. Russo, Rodney L. Sung, Benjamin J. Kaufman, Thomas F. Derosa
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Patent number: 5512588Abstract: 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: GrantFiled: January 28, 1994Date of Patent: April 30, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hisashi Takasugi, Yousuke Katsura, Yoshikazu Inoue, Tetsuo Tomishi
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Patent number: 5457122Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: July 13, 1993Date of Patent: October 10, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5412117Abstract: 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: GrantFiled: January 26, 1993Date of Patent: May 2, 1995Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Koga, Hiroyuki Nabata
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Patent number: 5401853Abstract: 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: GrantFiled: July 9, 1993Date of Patent: March 28, 1995Assignee: Laboratorio Farmaceutico C.T. S.r.l.Inventors: Mario Brufani, Antonella Loche, Vincenzo Perlini, Donato Pocar
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Patent number: 5350856Abstract: 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: GrantFiled: January 10, 1990Date of Patent: September 27, 1994Assignee: ICI Americas Inc.Inventor: Raymond A. Felix
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Patent number: 5344927Abstract: 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: GrantFiled: March 30, 1993Date of Patent: September 6, 1994Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Mitsuaki Ohta, Tokuo Koide, Takeshi Suzuki, Akira Matsuhisa, Keiji Miyata, Junya Ohmori, Isao Yanagisawa
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Patent number: 5312926Abstract: 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: GrantFiled: March 29, 1991Date of Patent: May 17, 1994Assignee: BASF AktiengesellschaftInventors: Volker Bach, Karl-Heinz Etzbach, Ruediger Sens
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Patent number: 5288735Abstract: 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: GrantFiled: June 15, 1992Date of Patent: February 22, 1994Inventors: Seymour F. Trager, G. Michael Blackburn
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Patent number: 5242937Abstract: 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: GrantFiled: March 19, 1990Date of Patent: September 7, 1993Assignee: Research Corporation Technologies, Inc.Inventor: William M. Pierce, Jr.
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Patent number: 5225424Abstract: 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: GrantFiled: October 21, 1992Date of Patent: July 6, 1993Assignee: University of Iowa Research FoundationInventors: Ronald D. Schoenwald, Charles F. Barfknecht
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Patent number: 5223616Abstract: 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: GrantFiled: November 4, 1991Date of Patent: June 29, 1993Assignee: Sumitomo Chemical Company, Ltd.Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
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Patent number: 5176739Abstract: 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: GrantFiled: June 21, 1991Date of Patent: January 5, 1993Assignee: BASF AktiengesellschaftInventors: Volker Maywald, Klaus Ditrich, Thomas Kuekenhoehner, Gerhard Hamprecht, Wolfgang Freund, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 5158950Abstract: 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: GrantFiled: May 23, 1990Date of Patent: October 27, 1992Assignee: Yuhan Corporation, Ltd.Inventors: Choong S. Kim, Jeong S. Chae, Young R. Choi, Jong W. Lee, Joung K. Yoo
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Patent number: 5157044Abstract: 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: GrantFiled: June 11, 1990Date of Patent: October 20, 1992Assignee: University of Iowa Research FoundationInventors: Ronald D. Schoenwald, Charles F. Barfknecht
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Patent number: 5155122Abstract: 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: GrantFiled: August 23, 1991Date of Patent: October 13, 1992Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn, Catherine R. Kostlan, Michael D. Mullican, Gary P. Shrum, Paul C. Unangst, Michael W. Wilson
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Patent number: 5103007Abstract: 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: GrantFiled: October 27, 1989Date of Patent: April 7, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
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Patent number: 5081245Abstract: 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: GrantFiled: August 18, 1989Date of Patent: January 14, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
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Patent number: 4975446Abstract: 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: GrantFiled: May 2, 1989Date of Patent: December 4, 1990Inventors: Seymour F. Trager, G. Michael Blackburn
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Patent number: 4948891Abstract: 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: GrantFiled: August 9, 1989Date of Patent: August 14, 1990Assignee: Pfizer Inc.Inventors: Rodney C. Schnur, Anton F. J. Fliri
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Patent number: 4912224Abstract: 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: GrantFiled: December 9, 1987Date of Patent: March 27, 1990Assignee: Shionogi & Co., Ltd.Inventor: Yoshio Hamashima
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Patent number: 4911745Abstract: 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: GrantFiled: July 8, 1988Date of Patent: March 27, 1990Assignee: ICI Americas Inc.Inventor: Raymond A. Felix
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Patent number: 4874864Abstract: 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: GrantFiled: May 24, 1988Date of Patent: October 17, 1989Assignee: Pfizer Inc.Inventors: Rodney C. Schnur, Anton F. J. Fliri
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Patent number: 4855310Abstract: 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: GrantFiled: March 25, 1988Date of Patent: August 8, 1989Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kiyoshi Murase, Toshiyasu Mase, Hiromu Hara, Kenichi Tomioka
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Patent number: 4845230Abstract: 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: GrantFiled: November 22, 1988Date of Patent: July 4, 1989Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Shigeki Yagi, Hiroshi Miyauchi
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Patent number: 4828604Abstract: 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: GrantFiled: March 9, 1988Date of Patent: May 9, 1989Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Shigeki Yagi, Hiroshi Miyauchi
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Patent number: 4803211Abstract: 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: GrantFiled: July 14, 1986Date of Patent: February 7, 1989Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Toshiyasu Mase, Ryuji Tsuzuki, Hiromu Hara, Kiyoshi Murase, Kenichi Tomioka
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Patent number: 4801718Abstract: 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: GrantFiled: December 5, 1985Date of Patent: January 31, 1989Assignee: Eli Lilly and CompanyInventor: Kenneth W. Burow, Jr.
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Patent number: 4746745Abstract: 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: GrantFiled: June 19, 1986Date of Patent: May 24, 1988Inventor: Thomas H. Maren
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Patent number: 4742060Abstract: 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: GrantFiled: January 21, 1986Date of Patent: May 3, 1988Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
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Patent number: 4739083Abstract: 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: GrantFiled: January 2, 1986Date of Patent: April 19, 1988Assignee: Daicel Chemical Industries Ltd.Inventors: Yoichiro Ueda, Yukihisa Goto, Kazuhisa Masamoto
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Patent number: 4703125Abstract: 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: GrantFiled: July 1, 1986Date of Patent: October 27, 1987Assignee: Bayer AktiengesellschaftInventors: Axel Ingendoh, Horst Meyer, Bernward Garthoff
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Patent number: 4695571Abstract: 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: GrantFiled: April 2, 1986Date of Patent: September 22, 1987Assignee: Pfizer Inc.Inventor: Lawrence S. Melvin
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Patent number: 4686224Abstract: 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: GrantFiled: August 6, 1985Date of Patent: August 11, 1987Assignee: Pfizer Inc.Inventor: Lawrence S. Melvin, Jr.
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Patent number: 4639526Abstract: 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: GrantFiled: August 29, 1968Date of Patent: January 27, 1987Assignee: Bayer AktiengesellschaftInventors: Carl Metzger, Ludwig Eue, Helmuth Hack
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Patent number: 4568752Abstract: 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: GrantFiled: December 10, 1984Date of Patent: February 4, 1986Assignee: Ciba-Geigy AGInventor: Mario Fryberg
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Patent number: 4518414Abstract: 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: GrantFiled: January 11, 1983Date of Patent: May 21, 1985Assignee: BASF AktiengesellschaftInventors: Ulrich Schirmer, Peter Plath, Bruno Wuerzer