Chalcogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/441)
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Patent number: 5948813Abstract: A method for suppressing the rejection of allogeneic transplants in a mammal, including a human, comprising administering to said mammal an effective amount of the compound of the formula ##STR1## wherein n, A, B, R.sup.1 and R.sup.2 are as defined above, or the pharmaceutically acceptable salt thereof.Type: GrantFiled: October 14, 1997Date of Patent: September 7, 1999Assignee: Pfizer Inc.Inventors: Henry J. Showell, Elora J. Weringer
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Patent number: 5874252Abstract: EBI 3 polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing EBI 3 polypeptides and polynucleotides in the design of protocols for the treatment of infections such as bacterial, fungal, protozoan and viral infections, particularly infections caused by HIV-1 or HIV-2; pain; cancers; anorexia; bulimia; asthma; Parkinson's disease; acute heart failure; hypotension; hypertension; urinary retention; osteoporosis; angina pectoris; myocardial infarction; ulcers; astma; allergies; benign prostatic hypertrophy; and psychotic and neurological disorders, including anxiety, schizophrenia, manic depression, delirium, dementia, severe mental retardation and dysldnesias, such as Huntington's disease or Gilles dela Tourett's syndrome, among others and diagnostic assays for such conditions.Type: GrantFiled: July 29, 1997Date of Patent: February 23, 1999Assignee: Smithkline Beecham CorporationInventor: Yuan Zhu
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Patent number: 5798379Abstract: UCS1025 compounds represented by the following formula (I): ##STR1## wherein R represents hydrogen or hydroxyl group, or tautomers or pharmacologically acceptable salts thereof.Type: GrantFiled: December 18, 1997Date of Patent: August 25, 1998Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tamio Mizukami, Harumi Ogawa, Ryuichiro Nakai, Akira Asai, Yoshinori Yamashita, Katsuhiko Ando, Tsutomu Agatsuma, Shiro Akinaga, Kozo Ouchi, Hideki Kawasaki
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Patent number: 5750560Abstract: The present invention relates to therapeutic compositions based on compounds chosen from the formulae: ##STR1## in which: X is chosen from .dbd.S, .dbd.O, .dbd.SO, .dbd.N--OH, .dbd.N--R.sub.5, .dbd.N--NH--CONH.sub.2, .dbd.N--NH--CSNH.sub.2 and ##STR2## A is chosen from the >C.dbd.N--OH group, a group of formula >C.dbd.N--OR.sub.3, a C.dbd.O group, a group C.dbd.N--R.sub.4 and a CHOH group,and their pharmaceutically acceptable salts.These compositions may be used as free-radical trapping agents.Type: GrantFiled: November 27, 1995Date of Patent: May 12, 1998Assignee: Laboratoires De Therapeutique ModerneInventors: Marie-Odile Christen, Jean-Louis Burgot
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Patent number: 5747505Abstract: The heterocyclic aryl-, alkyl- and cycloalklacetamides are prepared by reacting the appropriately substituted acetic acids with amines, if appropriate in complexed form. The heterocyclic aryl-, alkyl- and cycloalkylacetamides can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.Type: GrantFiled: September 20, 1996Date of Patent: May 5, 1998Assignee: Bayer AktiengesellschaftInventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
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Patent number: 5728710Abstract: Rapamycin derivatives; pharmaceutical compositions comprising such rapamycin derivatives and pharmaceutically acceptable carriers or diluents; and methods of using such derivatives to inhibit pathogenic fungi growth inhibition, inhibit immunosuppression or treat carcinogenic tumors are disclosed.Type: GrantFiled: March 16, 1995Date of Patent: March 17, 1998Assignee: SmithKline Beecham CorporationInventor: Juan Ignacio Luengo
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Patent number: 5703114Abstract: Disclosed is the use of compositions employing a 4,5-dicyano-1,3-dithiole-2-one (or thione) compound corresponding to the formula: ##STR1## wherein Z is oxygen or sulfur as the active antimicrobial and marine antifouling agent.Type: GrantFiled: July 10, 1996Date of Patent: December 30, 1997Assignee: The Dow Chemical CompanyInventors: Ravi B. Shankar, Duane R. Romer, R. Garth Pews
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Patent number: 5691338Abstract: This invention provides a method of inhibiting the replication of a reverse transcriptase-dependent virus in cells which comprises contacting infected cells with an effective amount of a 1,2-dithiole-3-thione. A composition for inhibiting reverse transcriptase-dependent viral replication of cells comprising an effective amount of a 1,2-dithiole-3-thione and a physiologically acceptable carrier is also provided.Type: GrantFiled: June 7, 1995Date of Patent: November 25, 1997Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Hans J. Prochaska, Bruce Polsky
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Patent number: 5661176Abstract: Disclosed are (2-one (or thione)-1,3-dithiole-4,5-diyl)bis(thiomethylthiocyanate) compounds corresponding to the formula: ##STR1## wherein Z is oxygen or sulfur, compositions containing said compounds and their use as antimicrobial and marine antifouling agents.Type: GrantFiled: July 10, 1996Date of Patent: August 26, 1997Assignee: The Dow Chemical CompanyInventors: Duane R. Romer, Weishi W. Wu, Ravi B. Shankar, R. Garth Pews
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Patent number: 5631277Abstract: Disclosed is (2-thione-1,3-dithiole 4,5-diyl) bis(thiocyanate), its preparation and its use as an antimicrobial and marine antifouling agent.Type: GrantFiled: July 10, 1996Date of Patent: May 20, 1997Assignee: The Dow Chemical CompanyInventors: Duane R. Romer, Weishi W. Wu, Ravi B. Shankar, R. Garth Pews
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Patent number: 5618835Abstract: A compound having the structure: ##STR1## pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: April 8, 1997Assignee: The Procter & Gamble CompanyInventors: Laurence I. Wu, John M. Janusz
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Patent number: 5531989Abstract: A composition for restoring and maintaining gastrointestinal health comprises 40-60% by weight of an immunoglobulin composition comprising concentrated immunologically active immunoglobulins and 40-60% by weight of soluble dietary fiber selected from inulin, fructo-oligosaccharides, pectin, guar gum, and mixtures thereof. The immunoglobulin and fiber-containing composition can optionally contain one or more of a beneficial human intestinal microorganism, components of a non-immune natural defense system, an iron-sequestering molecule, and gluconic acid. Preferred beneficial human intestinal microorganisms include lactobacilli and bifidobacteria. The immunologically active immunoglobulins are preferably purified from bovine milk, milk products, or whey. Methods of use are also described.Type: GrantFiled: May 9, 1995Date of Patent: July 2, 1996Assignee: Metagenics, Inc.Inventor: Stephen M. Paul
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Patent number: 5470871Abstract: The present invention relates to therapeutic compositions based on compounds chosen from the formulae: ##STR1## in which: X is chosen from .dbd.S, .dbd.O, .dbd.SO, .dbd.N--OH, .dbd.N--R.sub.5, .dbd.N--NH--CONH.sub.2, .dbd.N--NH--CSNH.sub.2 and ##STR2## A is chosen from the ##STR3## group, a group of formula ##STR4## a C.dbd.O group, a group C.dbd.N--R.sub.4 and a CHOH group, and their pharmaceutically acceptable salts.These compositions may be used as free-radical trapping agents.Type: GrantFiled: December 27, 1993Date of Patent: November 28, 1995Assignee: Laboratoires de Therapeutique ModerneInventors: Marie-Odile Christen, Jean-Louis Burgot
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Patent number: 5434151Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: August 24, 1992Date of Patent: July 18, 1995Assignee: CytoMed, Inc.Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5387594Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: August 4, 1992Date of Patent: February 7, 1995Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, William R. Pilgrim
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Patent number: 5288750Type: GrantFiled: January 31, 1991Date of Patent: February 22, 1994Assignee: Orion-yhtyma OyInventors: Pentti Pohto, Paivi A. Aho, Reijo J. Backstrom, Erkki J. Honkanen, Inge-Britt Y. Linden, Erkki A. O. Nissinen
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Patent number: 5198489Abstract: Thermoplastic compositions useful for producing metallic moldings containA) 40-65% by volume of a sinterable pulverulent metal or of a pulverulent metal alloy or of a mixture thereof,B) 35-60% by volume of a mixture ofB1) 85-100% by weight of a polyoxymethylene homopolymer or copolymer andB2) 0-15% by weight of a polymer homogeneously dissolved in B1) or dispersed therein with an average particle size of less than 1 .mu.m,C) 0-5% by volume of a dispersant.Type: GrantFiled: February 28, 1991Date of Patent: March 30, 1993Assignee: BASF AktiengesellschaftInventors: Hans-Josef Sterzel, Johan H. H. ter Maat
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Patent number: 5134158Abstract: A bactericidal composition and method for inhibiting and controlling the growth of the capsulated, facultative bacterium, Klebsiella pneumoniae, are disclosed. The composition comprises an amount, effective for the intended purpose of 3-iodo-2-propynylbutyl carbamate and 3,4-dichloro-1,2-dithiol-3-one. The method comprises administering between about 0.1 to about 200 parts of this combined treatment (based on one million parts of the desired aqueous system) to the particular water containing system for which treatment is desired.Type: GrantFiled: October 15, 1991Date of Patent: July 28, 1992Assignee: Betz Laboratories, Inc.Inventors: Wilson K. Whitekettle, Deborah K. Donofrio
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Patent number: 5128133Abstract: An industrial microbicidal/microbistatic composition which comprises (1) 4,5-dichloro-1,2-dithiol-3-one and (2) N-dodecylguanidine hydrochloride or N-dodecylguanidine acetate and a method of killing or inhibiting the growth of microbe or controlling slime formation using said composition.Type: GrantFiled: November 21, 1990Date of Patent: July 7, 1992Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Yasuhiro Hidaka, Masanobu Takahashi, Toshio Sato
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Patent number: 5118672Abstract: This invention provides compounds and pharmaceutical compositions that include compounds of the formula: ##STR1## in which A, B, and C are hydrogen, halogen, or azido; D is hydrogen, halogen, azido, or OH; A and B or C and D can be replaced with a double bond; R is an aldohexose, aldohexosamine, or N-acetyl aldohexosamine, W is O or S; X is O, S, or CH.sub.2 ; Y is a purine or pyrimidine base, Z is C, S, or O, and wherein when Z is S or O, A and C are not present. The compounds of this inverntion have enhanced pharmaceutical or biological activity or increased intracellular absorption compared to the corresponding parent nucleoside as a function of the 5'-diphosphohexose moiety. Many of these compounds have antiviral, including anti-HIV, activity. Others have antibacterial activity. In one embodiment, the invention is a method to treat HIV infection and opportunistic infections concomitantly.Type: GrantFiled: July 11, 1990Date of Patent: June 2, 1992Assignees: University of Georgia Research Foundation, Emory University, UAB Research FoundationInventors: Raymond F. Schinazi, Jean-Pierre Sommadossi, Chung K. Chu, William M. Shafer
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Patent number: 5096920Abstract: The use of 5-phenyl-3H-1,2-dithiol-3-thion-S-oxides which are optionally substituted in the phenyl ring as active substances in hepato-protective medicaments and new 5-phenyl-3H-1,2-dithiol-3-thion-S-oxides which are substituted in the phenyl ring are described.Type: GrantFiled: May 26, 1989Date of Patent: March 17, 1992Assignee: Kali-Chemie Pharma GmbHInventors: Dominique Biard, Marie-Odile Christen, Patrick Dansette, Daniel Jasserand, Daniel Mansuy, Amor Sassi
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Patent number: 5093357Abstract: A bactericidal composition and method for inhibiting and controlling the growth of the capsulated, facultative bacterium, Klebsiella pneumoniae, are disclosed. The composition comprises an amount, effective for the intended purpose of diiodomethyl-p-tolylsulfone and 3,4-dichloro-1,2-dithiol-3-one. The method comprises administering between about 0.1 to about 200 parts of this combined treatment (based on one million parts of the desired aqueous system) to the particular water containing system for which treatment is desired.Type: GrantFiled: March 25, 1991Date of Patent: March 3, 1992Assignee: Betz Laboratories, Inc.Inventors: Wilson Whitekettle, Deborah K. Donofrio
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Patent number: 5084470Abstract: A germicidal composition includes 3-isothiazolone compound of the general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a halogen atom and R.sup.Type: GrantFiled: October 25, 1990Date of Patent: January 28, 1992Assignee: Somar CorporationInventors: Susumu Mitsui, Shigeru Kurose, Ryoji Funatsu
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Patent number: 5026723Abstract: A microbicidal/microbistatic synergistic composition for industrial use comprising a specific nitrobromopropane derivative and 4,5-dichloro-1,2-dithiol-3-one and an industrial method of killing or inhibiting the growth of microorganisms using the same compounds, which are useful of microbicidal/microbistatic treatment in various industrial media.Type: GrantFiled: April 14, 1989Date of Patent: June 25, 1991Assignee: Katayama Chemical, Inc.Inventors: Sakae Katayama, Yosuke Ito, Hidenori Hirashima
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Patent number: 5015660Abstract: A microbicidal/microbistatic composition for industrial use which contains 4,5-dichloro-1,2-dithiol-3-one and bromonitrostyrene and a method of killing or inhibiting the growth of microorganisms or controlling slime formation using the composition.Type: GrantFiled: November 20, 1989Date of Patent: May 14, 1991Assignee: Yoshitami Pharmaceutical Industries, Ltd.Inventors: Yasuhiro Hidaka, Toshio Sato, Masanobu Takahashi
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Patent number: 5001143Abstract: A pharmaceutical composition for prophylactic and preventive of ketosis of livestocks which contains a dithia derivative represented by the general formula (I), ##STR1## wherein R and R' may be the same or different and are each individually a lower alkyl group, n is an integer of 0, 1 or 2; and A is a group of the formula, --CH.sub.2 --, ##STR2## (wherein M is a hydrogen atom or a salt-forming residue), --CH.dbd.CH--, --CH.sub.2 --CH.sub.Type: GrantFiled: August 28, 1989Date of Patent: March 19, 1991Assignee: Nihon Nohyaku Co., Ltd.Inventors: Akio Hokazono, Masahiro Shimosako, Tatsuyoshi Sugimoto, Takehiro Shimada, Masahiro Hayashi
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Patent number: 4987148Abstract: A biocidal composition which comprises 4,5-dichloro-1,2-dithiol-3-one and N-methyl-2-pyrrolidone in a proportion by weight of 70:30 to 10:90 is described.Type: GrantFiled: October 19, 1989Date of Patent: January 22, 1991Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Yasuhiro Hidaka, Masato Magami, Takeshi Inoue, Sumio Nakane
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Patent number: 4942172Abstract: A method of curing or alleviating hepatic disease comprising administrating to the patient 1,3-dithiole-2-thione or 1,3-dithiolane-2-thione is disclosed. Adminstration of the compound can be made in various dosing forms, including tablets, granules, powders, capsules, suspensions, injections, and suppositories. Normal dosing amount can be determined from the range of 0.01 to 50 mg/kg/day for oral administration, and 0.002 to 10 mg/kg/day for injection or other forms of administration.Type: GrantFiled: May 20, 1988Date of Patent: July 17, 1990Assignee: SS Pharmaceutical Co., Ltd.Inventors: Hitoshi Nakazawa, Mari Ohtsuka, Hideaki Matsuda, Tatsuhiko Katori, Kazuhiko Irinoda
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Patent number: 4910217Abstract: A curing agent for fat necrosis which contains a dithia derivative represented by the general formula ##STR1## wherein R and R.sup.1 may be either the same or different and denote a lower alkyl group; n denotes an integer of 0, 1 or 2; and A denotes --CH.sub.2 --, ##STR2## M being H or a salt-forming rest, --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, or ##STR3## and a method for curing said disease using the said curing agent.Type: GrantFiled: December 24, 1986Date of Patent: March 20, 1990Assignee: Nihon Nohyaku Co., Ltd.Inventors: Matazaemon Uchida, Masakazu Shibayama, Isao Nishino, Harutaka Kimura
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Patent number: 4879306Abstract: A composition killing or inhibiting the growth of microorganisms is described and which contains a mixture of 4,5-dichloro-1,2-dithiol-3-one and dibromonitrilopropionamide. The combination leads to a marked synergistic action of the two active substance components in the control of microorganisms. The composition is suitable for use in a large number of industrial systems.Type: GrantFiled: September 27, 1985Date of Patent: November 7, 1989Assignee: Grace Service Chemicals GmbHInventors: Wolf-Dieter Henkels, Marion Balzer
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Patent number: 4853411Abstract: A method of treating an aqueous or non-aqueous dfsystem is disclosed which comprises adding to the system a thiolan of the formula ##STR1## wherein each of X and Y, which may be the same or different, represents fluorine, chlorine or bromine, in combination with a sulphone of the formula: ##STR2## in which R.sub.1 represents an optionally halogenated alkyl radical or an optionally substituted aryl radical, R.sub.2 represents a cyano or amidocarbonyl radical and X represents a halogen atom.Type: GrantFiled: December 11, 1987Date of Patent: August 1, 1989Assignee: W.R. Grace & Co.-Conn.Inventors: Douglas Clarkson, Richard P. Clifford
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Patent number: 4818765Abstract: The invention relates to the use of ketenethioacetals of the formula ##STR1## in which R.sub.1 represents aryl or heteroaryl, R.sub.2 represents hydrogen, an optionally substituted hydrocarbon radical, heteroaryl, an acyl radical, a group of the formula --S(O).sub.m --R.sub.a, wherein m is 0, 1, or 2 and R.sub.a is an optionally substituted hydrocarbon radical; or optionally functionally modified sulpho, A represents an optionally substituted bivalent aliphatic hydrocarbon radical and n is 0 or 1, and pharmaceutically acceptable salts of such compounds that contain a salt-forming group, for the treatment of liver diseases, respiratory tract diseases and vascular diseases pharmaceutical preparations containing compounds of the formula I and novel compounds of the formula I. The compounds have liver-protecting and immunomodulating properties.Type: GrantFiled: February 11, 1987Date of Patent: April 4, 1989Assignee: Ciba-Geigy CorporationInventors: Andrr J. Weith, Philippe M. Narbel
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Patent number: 4801586Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X and Y, each, may represent sulfur, oxygen or two hydrogen atoms, A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having 1-4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkylformyl; m is 3-7; q is 2m-2x, wherein x equals the number of double bonds in the lactam ring and may be 1, 2 or 3, and R is CH.sub.3, ##STR2## wherein R" is H or halogen.Type: GrantFiled: October 7, 1986Date of Patent: January 31, 1989Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 4760078Abstract: A novel 1,2-dithiol-3-thione derivative which has an immunomodulating property, which is expressed by the formula (I): ##STR1## wherein R denotes hydrogen, halogen, lower alkoxy group, lower alkyl group, amino group, lower alkyl-substituted amino group or lower alkoxycarbonyl group.Type: GrantFiled: March 5, 1987Date of Patent: July 26, 1988Assignee: Mitsui Toatsu Chemicals Inc.Inventors: Itaru Yamamoto, Akira Matsubara, Kanji Tomiya, Osamu Mizuno, Mitsuhiro Sakaguchi, Mikio Kumakura
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Patent number: 4755535Abstract: This invention provides compositions comprising a physiologically-active agent and an azacycloalkene having at least one double bond in the ring and of the general formula ##STR1## wherein X and Y, each, may represent sulfur, oxygen or two hydrogen atoms, A is a straight or branched chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having 1-4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkylformyl; m is 3-7; q is 2m-2x, wherein x equals the number of double bonds in the lactam ring and may be 1, 2 or 3; and R is --CH.sub.3, ##STR2## wherein R" is H or halogen in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.Type: GrantFiled: April 23, 1986Date of Patent: July 5, 1988Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 4647577Abstract: This invention relates to microbicidal/microbistatic compositions for industrial use which comprise 4,5-dichloro-1,2-dithiol-3-one and a haloacetic acid ester and an industrial method of killing and/or inhibiting microbes by using the aforementioned compositions.Type: GrantFiled: December 20, 1985Date of Patent: March 3, 1987Assignees: Katayama Chemical Works Co., Ltd., Yoshitomi Pharmaceutical Ind., Ltd.Inventors: Osamu Umekawa, Sakae Katayama
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Patent number: 4564627Abstract: Feed compositions containing a dithia derivative represented by the general formula: ##STR1## wherein R and R' are same or different lower alkyl groups, n is an integer of 0, 1 or 2, and A is --CH.sub.2 --. ##STR2## (wherein M is hydrogen or a salt-forming residue), --CH.dbd.CH--, --CH.sub.2 --CH.sub.2 --, ##STR3## are useful for improving meat qualities of livestock, poultry and fish as well as for strengthening the eggshell of poultry.Type: GrantFiled: August 16, 1983Date of Patent: January 14, 1986Assignee: Nihon Nohyaku Co., Ltd.Inventors: Akio Hokazono, Tatsuyoshi Sugimoto