Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/336)
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Patent number: 5079361Abstract: Cross-linking reagents which are highly specific for sulphydryl groups and react with thiols at an excellent rate. The essential feature of the reagents is at least one vinyl group conjugated with an armoatic nitrogen heterocycle. Particular examples include vinyl pyridines, vinyl pyrimidines and vinyl triazines.Type: GrantFiled: September 9, 1988Date of Patent: January 7, 1992Assignee: Celltech LimitedInventors: Rikki P. Alexander, Michael A. W. Eaton, Thomas A. Millican, Richard C. D. Titmas
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Patent number: 5047535Abstract: The invention relates to novel compounds which are suited for the production of multilayer films which have piezoelectric, and pyroelectric properties, and which provide second harmonic generation. The novel compounds are amphiphilic and it is possible to prepare from same polar single-layer and multi-layer films by depositing them on a substrate. When such substrate is a solid support, polar Z-type Langmuir-Blodgett films are obtained. Upon compression of films of such compounds, at an air/water interface, stable Langmuir monolayers are formed.Type: GrantFiled: August 5, 1987Date of Patent: September 10, 1991Assignee: Yeda Research and Development Company LimitedInventors: Meir Lahav, Leslie Leiserowitz, Jacob Sagiv, Ronit Popovitz-Biro, Karlheinz Hill, Ehud Landau
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Patent number: 5041452Abstract: Novel diamides having a nitrogen-containing heterocyclic moiety such as pyridyl are disclosed that are useful for improving feed utilization efficiency of ruminants and for improving lactation of lactating ruminants.Type: GrantFiled: September 28, 1989Date of Patent: August 20, 1991Assignee: Eastman Kodak CompanyInventor: Alan W. White
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Patent number: 5037827Abstract: A glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor.Type: GrantFiled: June 29, 1989Date of Patent: August 6, 1991Assignee: Eisai Co., Ltd.Inventors: Kazuo Okano, Osamu Asano, Naoyuki Shimomura, Tetsuya Kawahara, Shinya Abe, Shuhei Miyazawa, Mitsuaki Miyamoto, Hiroyuki Yoshimura, Koukichi Harada, Junsaku Nagaoka, Tsutomu Kawata, Tsutomu Yoshimura, Hiromasa Suzuki, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
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Patent number: 5036157Abstract: Novel compounds of formula (I)Ar--(L--Ar').sub.q --(X).sub.k --(Y).sub.p --Q (I)wherein:k, p and q are independently 0 or 1;Ar represents either:(i) naphthyl, tetrahydronaphthyl, pyridyl or(ii) phenyl, optionally substituted,L is selected from --(CH.sub.2).sub.r -- (where r is 1-4), --O--, --CH.sub.2 O--, --CH.sub.2 S--, --OCH.sub.2 --, --CONH--, --NHCO--, --CO-- and --CH.sub.2 NH--, and,Ar' represents phenylene, thienylene or pyridylene optionally substituted,X represents oxygen, sulphur or carbonyl,Y is C.sub.1-10 alkylene or C.sub.1-10 alkenylene;Q represents a non-cyclic moiety selected from groups of formula ##STR1## in which one of m and n is 0 and the other is 1, R.sup.1 and R.sup.2 is selected from hydrogen, C.sub.1-4 alkyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, C.sub.5-7 cycloalkylamino, C.sub.5-7 cycloalkyl (C.sub.1-4 alkyl) amino, anilino, N-C.sub.Type: GrantFiled: March 10, 1987Date of Patent: July 30, 1991Assignee: Burroughs Wellcome Co.Inventors: Geoffrey Kneen, William P. Jackson, Peter J. Islip, Peter J. Wates
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Patent number: 5030654Abstract: A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6-membered carbocycyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3.4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: May 19, 1989Date of Patent: July 9, 1991Assignee: Pfizer Inc.Inventors: Ian T. Barnish, John C. Danilewicz, Keith James, Gillian M. R. Samuels, Nicholas K. Terrett, Michael T. Williams, Martin J. Wythes
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Patent number: 5025017Abstract: Seco-mevinic acid derivatives are provided which has the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## R is H, alkali metal or lower alkyl, R.sup.1 is H, lower alkyl, aryl, lower alkoxy, cycloalkyl, heteroaryl, aralkyl, heteroaralkyl or heterocyclic; R.sup.2 is lower alkyl, cycloalkyl or aralkyl, and X is O or NR.sup.5 wherein R.sup.5 is H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis. New intermediates for preparing the above seco-mevinic acid derivatives are also provided.Type: GrantFiled: September 28, 1989Date of Patent: June 18, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Donald S. Karanewsky
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Patent number: 5013861Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as intermediates in the preparation of pharmaceutically active products.Type: GrantFiled: October 6, 1986Date of Patent: May 7, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Harold N. Weller, III, Eric M. Gordon
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Patent number: 5010097Abstract: Novel compounds of the formula (I), a process for their preparation and their use as collagenase inhibitors are described: ##STR1## in which, R.sub.1 is hydrogen, alkyl, or optionally substituted aryl;R.sub.2 is hydrogen, or acyl such as ##STR2## where Z is optionally substituted aryl; R.sub.3 is C.sub.3-6 alkyl;R.sub.4 is hydrogen, alkyl, --CH.sub.2 --R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl, or a group ##STR3## where R.sub.11 is hydrogen, alkyl, or --CH.sub.2 --Ph where Ph is optionally substituted phenyl, and R.sub.12 is hydrogen or alkyl; andR.sub.5 is hydrogen, alkyl, or a group ##STR4## where R.sub.13 is hydrogen, or alkyl, and R.sub.14 is hydroxy, alkoxy, or --NR.sub.6 R.sub.7, where each of R.sub.6 and R.sub.7 is hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom in the ring or an optional further nitrogen atom optionally substituted by alkyl.Type: GrantFiled: December 20, 1988Date of Patent: April 23, 1991Assignee: Beecham PharmaceuticalsInventors: Roger E. Markwell, Stephen A. Smith, Ian Hughes, Laramie M. Gaster
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Patent number: 5010091Abstract: 2,4-dihalogeno-6-pyridylethanolphenylisopropylamines for shifting the protein-fat ratio of animals in favor of protein, of the formula ##STR1## in which Hal are identical or different and represent fluorine, chlorine or bromine,X represents a direct bond or --CH.sub.2 -- andY represents phenyl, which is substituted by OH, C.sub.1-4 -alkoxy, C.sub.1-4 -alkoxy-C.sub.1-4 -alkoxy, carboxyl, aminocarbonyl, C.sub.1-4 -alkoxycarbonyl, hydroxy-C.sub.1-4 -alkoxy, C.sub.1-4 -alkoxycarbonyl-C.sub.1-4 -alkoxy or phenyl-C.sub.1-4 -alkoxy,or their physiologically tolerated salts.Type: GrantFiled: February 8, 1990Date of Patent: April 23, 1991Assignee: Bayer AktiengesellschaftInventors: Hans Lindel, Werner Hallenbach, Friedrich Berschauer, Heinrich Greife, Gernot Klotz
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Patent number: 5008276Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.Type: GrantFiled: October 17, 1988Date of Patent: April 16, 1991Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
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Patent number: 5001156Abstract: Lipophilic quaternary ammonium salicylate, characterized in that it corresponds to the formula: ##STR1## in which: (i) R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote an alkyl or alkylcycloalkyl radical, optionally substituted or interrupted;(ii) R.sub.3 and/or R.sub.4 denote(s) a group:R.sub.8 [OC.sub.2 H.sub.3 R.sub.7 ].sub.n [OCH.sub.2 CHOH--CH.sub.2 ].sub.pin which 0.ltoreq.n.ltoreq.4 and p denotes 0 or 1; R.sub.8 denotes H or an alkyl, alkenyl, alkylcycloalkyl or alkylaryl radical;(iii) R.sub.4 denotes an alkylphenyl radical;(iv), (v) R.sub.1 and R.sub.2 can form a saturated or unsaturated aromatic or non-aromatic heterocycle;(vi) R.sub.1, R.sub.2 and R.sub.3 form polycyclic derivatives with the nitrogen atoms; R.sub.5 denotes a group corresponding to the formula: ##STR2## in which n is an integer varying between 0 and 10.Type: GrantFiled: December 1, 1987Date of Patent: March 19, 1991Assignee: L'OrealInventors: Michel Philippe, Henri Sebag, Michel Hocquaux, Bernard Jacquet, Jean P. Laugier
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Patent number: 4978384Abstract: There are disclosed novel 2,6-substituted-3,5-pyridinedicarboxylic acids, esters, salts, amides, halides, and cyano compounds useful as herbicides, and as intermediates which provide herbicides.Type: GrantFiled: May 1, 1989Date of Patent: December 18, 1990Assignee: Monsanto CompanyInventor: Len F. Lee
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Patent number: 4977170Abstract: Novel isoprenoidamine compounds (I) which show antiulcer activity are provided.Type: GrantFiled: May 3, 1989Date of Patent: December 11, 1990Assignee: Shionogi & Co., Ltd.Inventors: Saichi Matsumoto, Masami Doteuchi, Takuji Mizui, Kentaro Hirai
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Patent number: 4963688Abstract: A dihydropyridine.revreaction.pyridinium salt type of redox, or chemical, delivery system for the site-specific and/or site-enhanced delivery of a radionuclide to the brain is provided. A chelating agent capable of chelating with a radionuclide and having a reactive hydroxyl, carboxyl, amino, amide or imide group is coupled to a carrier moiety comprising a dihydropyridine.revreaction.pyridinium salt nucleus and then complexed with a radionuclide to provide a new radiopharmaceutical that, in its lipoidal dihydropyridine form, penetrates the blood-brain barrier ("BBB") and allows increased levels of radionuclide concentration in the brain, particularly since oxidation of the dihydropyridine carrier moiety in vivo to the ionic pyridinium salt retards elimination from the brain while elimination from the general circulation is accelerated.This radionuclide delivery system is well suited for use in scintigraphy and similar radiographic techniques.Type: GrantFiled: August 21, 1987Date of Patent: October 16, 1990Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 4963682Abstract: A dihydropyridine.rarw..fwdarw. pyridinium salt type of redox, or chemical, delivery system for the site-specific and/or site-enhanced delivery of a radionuclide to the brain is provided. A chelating agent capable of chelating with a radionuclide and having a primary, secondary or tertiary amino function can be converted to the corresponding analogue in which said function is replaced with a dihydropyridine.rarw. .fwdarw. pyridinium salt redox system and then complexed with a radionuclide to provide a new radiopharmaceutical that, in its lipoidal dihydropyridine form, penetrates the blood-brain barrier ("BBB") and allows increased levels of radionuclide concentration in the brain, particularly since oxidation of the dihydropyridine moiety in vivo to the ionic pyridinium salt retards elimination from the brain while elimination from the general circulation is accelerated.This radionuclide delivery system is well suited for use in scintigraphy and similar radiographic techniques.Type: GrantFiled: August 21, 1987Date of Patent: October 16, 1990Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 4933339Abstract: 2,3 and 4-(2-cyano-2-arylethyl)pyridines of the formula: ##STR1## wherein R is a hydrogen, alkyl, cycloalkyl, haloalkyl, alkenyl including dialkenyl, haloalkenyl, akynyl including alkynylalkenyl, alkoxyalkyl, halo(alkoxyalkyl), optionally substituted phenyl, phenylalkyl, phen(c.sub.2 -C.sub.4)alkenyl, phenoxyalkyl, a heterocyclic group selected from pyridyl, pyrimidyl, pyrazinyl and furyl or a heterocycloalkyl group wherein the heterocycle is pyridyl, pyrimidyl, pyrazinyl, morpholinyl, pyrrolyl, tetrahydrofuryl, furyl, pyrazolyl or dioxalyl; and Ar is an optionally substituted phenyl or naphthyl group, are new compounds which are fungicidally active, particularly against phytopathogenic fungi.Type: GrantFiled: April 7, 1988Date of Patent: June 12, 1990Assignee: Rohm and Haas CompanyInventor: Ashok K. Sharma
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Patent number: 4902699Abstract: Compounds useful in the treatment of patients suffering from senile dementia, Alzheimer's disease or memory defects, of the formula ##STR1## in which R represents hydrogen or a linear, branched or cyclic alkyl, alkenyl, or alkynyl, containing up to 8 carbon atoms, or the radical ##STR2## in which R.sub.1 represents a linear or branched, alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, a linear or branched, saturated or unsaturated, alkoxy containing up to 8 carbon atoms, or aryl containing up to 14 carbon atoms, or the radical ##STR3## in which R.sub.2 represents a linear or branched alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, aryl containing up to 14 carbon atoms, possibly substituted, or aralkyl containing up to 18 carbon atoms, possibly substituted, and R' represents a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, as well as their addition salts with organic or mineral acids.Type: GrantFiled: August 22, 1988Date of Patent: February 20, 1990Assignee: Roussel UclafInventors: Emilio Toja, Carla Bonetti, Fernando Barzaghi, Giulio Galliani
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Patent number: 4895834Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin associated hypertension, hyperaldosternoism, and congestive heart failure. Processes for preparing the peptides, compositions containing them and methods of using them are included. Also included is a diagnostic test using the compounds to determine the presence of renin-associated hypertension or hyperaldosteronism.Type: GrantFiled: November 2, 1987Date of Patent: January 23, 1990Assignee: Warner-Lambert CompanyInventors: James P. Hudspeth, James S. Kaltenbronn, Joseph T. Repine, William H. Roark, Michael A. Stier
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Patent number: 4895951Abstract: Novel diamides having a nitrogen-containing heterocyclic moiety such as pyridyl are disclosed that are useful for improving feed utilization efficiency of ruminants and for improving lactation of lactating ruminants.Type: GrantFiled: January 17, 1989Date of Patent: January 23, 1990Assignee: Eastman Kodak CompanyInventor: Alan W. White
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Patent number: 4889865Abstract: Mono, di and tri-esters of 1,8-dihydroxy-10-phenyl-9-anthrone or -9-anthranol have the formula ##STR1## wherein p is 0 or 1,(a) when p=0, t=1 and R.sub.2 represents hydrogen or --COR.sub.3,(b) when p=1, t=0 and R.sub.1 and R.sub.2 each independently represent hydrogen or --COR.sub.3,R.sub.3 represents linear or branched alkyl having 1-17 carbon atoms, cycloalkyl, phenyl or phenyl substituted by lower alkyl, lower alkoxy, halogen, a nitro function, --CF.sub.3 or a hydroxyl function, and mixtures of said esters. These esters are prepared by reacting 1,8-dihydroxy-10-phenyl-9-anthrone with an activated form of an acid. The esters are useful in human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: February 21, 1989Date of Patent: December 26, 1989Assignee: Centre International de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Gerard Lang, Jean Maignan, Serge Restle, Christopher Hensby, Michel Colin
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Patent number: 4876343Abstract: An improved process for the preparation of statine, the phenyl analog of statine, the cyclohexyl analog of statine and derivatives thereof is described, as well as other valuable intermediates used in the process.Type: GrantFiled: June 15, 1988Date of Patent: October 24, 1989Assignee: Warner-Lambert CompanyInventors: John C. Hodges, Sylvester Klutchko
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Patent number: 4863939Abstract: The growth of livestock is promoted by the new compounds of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, halogen, halogenoalkyl, hydroxyl, cyano, alkoxycarbonyl, aminocarbonyl, mono- and dialkylaminocarbonyl, alkoxy, halogenoalkoxy, halogenoalkylthio or NHSO.sub.2 -alkyl,R.sup.2 represents hydrogen, hydroxyl, alkoxy or the --NR.sup.11 R.sup.12 radical,R.sup.3 represents the radicals mentioned in the case of R.sup.1R.sup.4 represents hydroxyl, acyloxy or alkoxy,R.sup.5 represents hydrogen or alkyl,R.sup.6 represents hydrogen or alkyl,R.sup.7 represents hydrogen or alkyl,R.sup.8 represents hydrogen or alkyl,X represents C.sub.1 -C.sub.10 -alkylene or a direct bond,Y represents oxygen or a direct bond,R.sup.9 represents hydrogen, C.sub.1 -C.sub.10 -alkyl which is optionally substituted by hydroxyl, alkoxy, acyloxy or the --NR.sup.13 R.sup.14 radical, or represents the COR.sup.15 radical or the O--Z--R.sup.16 radical,Z represents C.sub.1 -C.sub.10 -alkylene, C.sub.1 -C.sub.Type: GrantFiled: July 30, 1987Date of Patent: September 5, 1989Assignee: Bayer AktiengesellschaftInventors: Hans Lindel, Werner Hallenbach, Friedrich Berschauer, Anno de Jong, Martin Scheer
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Patent number: 4863936Abstract: Various substituted aminoalkylamino-2-pyridine derivatives are disclosed which are useful as histamine H.sub.1 -antagonists.Type: GrantFiled: October 21, 1986Date of Patent: September 5, 1989Assignee: Smith Kline & French Laboratories LimitedInventor: George S. Sach
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Patent number: 4855213Abstract: Polymethine dyes are disclosed containing an acidic electron accepting terminal nucleus comprised of an isocyano group. The dyes are useful as spectral sensitizers in ultravioilet responsive imaging compositions.Type: GrantFiled: April 20, 1988Date of Patent: August 8, 1989Assignee: Eastman Kodak CompanyInventor: Margaret E. Logan
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Patent number: 4841059Abstract: Antibacterially active new 1,8-bridged 4-quinolone-3-carboxylic acid derivatives of the formula ##STR1## in which Y is carboxyl or a derivative thereofR.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2 and X.sup.5 are H or various radicals,Z is O, NH, substituted NH, ##STR2## m and n are 0 or 1, andA, B, D, and E are CH or substituted C or up to three of them are N,and physiologically acceptable salts thereof. Novel intermediates are described as well as processes for making the intermediates and end products.Type: GrantFiled: October 15, 1987Date of Patent: June 20, 1989Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
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Patent number: 4829053Abstract: New aminoacid derivatives of the formula IX--Z--NR.sup.2 --CHR.sup.3 --CR.sup.4 --(CHR.sup.5).sub.n --CO--E--NR.sup.6 --(CHR.sup.7).sub.s --D Iwherein X, Z, R.sup.2, R.sup.3, R.sup.4, R.sup.5, E, R.sup.6, R.sup.7, D, n and s have the meanings defined herein and their salts, inhibit the activity of human plasma renin.Type: GrantFiled: July 31, 1987Date of Patent: May 9, 1989Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Peter Raddatz, Joachim Gante, Claus J. Schmitges, Klaus Otto Minck, Johannes Sombroek, Gunter Holzemann
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Patent number: 4826531Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur; A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 or --S(O).sub.n R.sup.3 groups; any two of the groups A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.Type: GrantFiled: April 17, 1987Date of Patent: May 2, 1989Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Paul DeFraine, Christopher R. A. Godfrey, Patrick J. Crowley, Kenneth Anderton
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Patent number: 4820691Abstract: Compounds of the formula ##STR1## are disclosed. These compounds interevene in the conversion of angiotensin to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.Type: GrantFiled: June 24, 1987Date of Patent: April 11, 1989Assignee: E. R. Squibb & Sons, Inc.Inventor: Dinesh V. Patel
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Patent number: 4812442Abstract: Enzyme tripeptides of the formula: ##STR1## and analogs thereof which inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these problems employing the novel tripeptides.Type: GrantFiled: May 4, 1987Date of Patent: March 14, 1989Assignee: Merck & Co., Inc.Inventors: Joshua S. Boger, Ben E. Evans, Mark G. Bock
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Patent number: 4808750Abstract: Novel fluorophenoxyphenoxypropionates and derivatives thereof possess herbicidal activity selectively in the presence of broadleaf crops. Preemergent and postemergent applications are contemplated.Type: GrantFiled: July 14, 1986Date of Patent: February 28, 1989Assignee: The Dow Chemical CompanyInventors: Richard B. Rogers, B. Clifford Gerwick, III
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Patent number: 4794121Abstract: Alkylcarboxamides of pyridylalkylamines, useful in human and verterinary medicine, correspond to the general formula I: ##STR1## wherein n=0 or 1,R.sub.3 represents an alkyl group of C.sub.1 to C.sub.3 or a hydrogen atom,R.sub.1 represents a hydrogen atom,R.sub.2 represents a group: ##STR2## in which: X and Y are different,X and Y each represent a linear or branched saturated or unsaturated hydrocarbon chain comprising from 1 to 16 carbon atoms;X and Y together determine a saturated or unsaturated cyclic radical substituted or not comprising from 3 to 12 carbon atoms.Type: GrantFiled: September 18, 1986Date of Patent: December 27, 1988Assignee: PanmedicaInventors: Claude Laruelle, Marcel Lepant, Bernard Raynier
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Patent number: 4782074Abstract: The substituted heteroaryl compounds of this invention are good fungicides. In particular, they possess especially good activity against Bean Powdery Mildew.Type: GrantFiled: March 30, 1987Date of Patent: November 1, 1988Assignee: Chevron Research CompanyInventor: David M. Spatz
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Patent number: 4772713Abstract: Disclosed are compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently are H or C.sub.1-8 -alkyl or together are C.sub.2-7 -alkylene forming a ring with the connecting N-atom; X is CN, halo, C.sub.6-10 -arylsulfonyl, C.sub.6-10 -arylsulfinyloxy, C.sub.6-10 -aryloxy, C.sub.6-10 -arylthio or C.sub.1-8 -alkylsulfonyloxy or nitro, and Y is the anion of an acid having a pK.sub.a of about 3 or less.These compounds are intermediates in the preparation of 4-substituted pyridines.Type: GrantFiled: May 21, 1987Date of Patent: September 20, 1988Assignee: Nepera, Inc.Inventor: Laurence J. Nummy
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Patent number: 4766132Abstract: Compounds of formula: ##STR1## and stereoisomers thereof, wherein R.sup.1 is unsubstituted or substituted aryl or heteroaryl; R.sup.2 is H, alkyl, alkenyl or alkynyl; X is O, NH, or S; R.sup.3 being alkyl, alkenyl, alkynyl or COR.sup.4 where R.sup.4 has an R.sup.3 value, when X is O; R.sup.3 being --CO-- alkyl when X is NH; and R.sup.3 being alkyl, alkenyl or CSNR.sup.5 R.sup.6 where R.sup.5 and R.sup.6, which may be the same or different, are H, alkyl, alkenyl or, together with the adjacent N atom, constitute a ring, when X is S; or XR.sup.3 together represent --CN; and salts and metal complexes thereof, have fungicidal and plant growth regulating activity.Type: GrantFiled: January 29, 1986Date of Patent: August 23, 1988Assignee: Imperial Chemical Industries PLCInventor: Ian T. Kay
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Patent number: 4731373Abstract: Glycerine derivatives of the formula ##STR1## wherein the residues R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description,and their hydrates, which inhibit blood platelet activating factor (PAF), are descried.Type: GrantFiled: December 10, 1984Date of Patent: March 15, 1988Assignee: Hoffman-La Roche Inc.Inventors: Richard Barner, Kasper Burri, Jean-Marie Cassal, Paul Hadvary, Georges Hirth, Klaus Muller
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Patent number: 4719288Abstract: Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, X.sub.1 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to X.sub.2, X.sub.2 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to X.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl, aryl-lower alkyl or aryl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents alkyl, cycloalkyl, aryl-lower alkyl or aryl, and R.sub.6 represents free or substituted amino or substituted hydroxy, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.Type: GrantFiled: June 2, 1986Date of Patent: January 12, 1988Assignee: Ciba-Geigy CorporationInventors: Walter Fuhrer, Peter Buhlmayer, Vittorio Rasetti, Bernhard Riniker
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Patent number: 4716175Abstract: Certain substituted amides of saturated fatty acids are potent inhibitors of the enzyme acyl-CoA:cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol.Type: GrantFiled: February 24, 1987Date of Patent: December 29, 1987Assignee: Warner-Lambert CompanyInventors: Milton L. Hoefle, Ann Holmes, Bruce D. Roth
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Patent number: 4710508Abstract: Certain O-substituted 1-(1,2,3,6-tetrahydro-1-methyl-3-pyridinyl)ketone oximes and O-substituted 1-(1,2,3,6-tetrahydro-4-pyridinyl)ketone oximes are useful as analgesic agents or agents for the treatment or amelioration of the symptoms of cerebral insufficiency characterized by decreased central acetylcholine production or release.Pharmaceutical compositions containing the compounds and methods of using the compositions in a pharmaceutical method are also disclosed.Type: GrantFiled: December 8, 1986Date of Patent: December 1, 1987Assignee: Warner-Lambert CompanyInventors: Stephen C. Bergmeier, David A. Downs, Walter H. Moos, David W. Moreland, Haile Tecle
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Patent number: 4698354Abstract: 3-carbamoyl-(3'-picolyl)-4-methoxy-1-benzamide of formula ##STR1## is a pharmaceutical agent for the prevention and treatment of thromboelmbolic disorders due to increased blood platelet aggregation.Type: GrantFiled: October 8, 1986Date of Patent: October 6, 1987Assignee: Societa Italo-Brittanica L. Manetti-H. Roberts & Co.Inventors: Massimo De Regis, Emanuela Mannucci
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Patent number: 4692450Abstract: Polycyclic salts of the formulaA.sup.- XN.sup.+ CH.sub.2 --(Y).sub.n --(CH.sub.2).sub.p --(Z).sub.q --L--(T).sub.r --M IwhereinA.sup.- is the anion of a strong organic or inorganic acid;XN.sup.+ is pyridinium, pyrimidinium, thiazolium or imidazolium substituted by R.sup.1, R.sup.2 and R.sup.3 ;n, q and r individually are the integer 1 or 0 and p is an integer from 1 to 15;Y is CH.sub.2, C(H,OH) or C(O);Z is O, S, CH.sub.2, C(O), NQ.sup.1, SO.sub.2, C(O)O, OC(O), C(O)N(Q.sup.1) or N(Q.sup.1)C(O);L is p-phenylene substituted by R.sup.4 ; andM is phenyl substituted by R.sup.5 and R.sup.6,T has one of the meanings given above, for Z or is C(CH.sub.3).sub.2, C.sub.2 H.sub.4, C(Q.sup.2).dbd.C(Q.sup.3), C.tbd.C, CH.sub.2 C(O), C(O)CH.sub.2, CH.sub.2 O or OCH.sub.2,R.sup.1 is a group Ar, Ar--C.sub.1-4 -alkyl, ArO or Arc(O),Ar is phenyl substituted by R.sup.7, R.sup.8 and R.sup.9 ;R.sup.2 and R.sup.3 individually are H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.6 H.sub.Type: GrantFiled: January 10, 1986Date of Patent: September 8, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Jean-Marie Cassal, Albrecht Edenhofer, Henri Ramuz
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Patent number: 4647668Abstract: Disopyramide immunogens, antibodies prepared therefrom, labeled conjugates, synthetic intermediates, and the use of such antibodies and labeled conjugates in immunoassays for determining disopyramide. The immunogens comprise disopyramide coupled by an ether linkage at a selected singular position on its phenyl ring to an immunogenic carrier material. Likewise, the labeled conjugates and synthetic intermediates are phenyl ether derivatives of disopyramide or precursors thereof. The antibody and labeled conjugates are particularly useful in homogeneous nonradioisotopic immunoassays for measuring disopyramide in biological fluids such as serum.Type: GrantFiled: May 20, 1985Date of Patent: March 3, 1987Assignee: Miles Laboratories, Inc.Inventors: Robert T. Buckler, Stephan G. Thompson
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Patent number: 4616088Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.Type: GrantFiled: December 14, 1984Date of Patent: October 7, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Denis E. Ryono, Edward W. Petrillo, Jr.
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Patent number: 4562257Abstract: The invention provides a process for the preparation of substituted and unsubstituted 2-carbamoyl nicotinic and 3-quinolinecarboxylic acids.Type: GrantFiled: November 7, 1983Date of Patent: December 31, 1985Assignee: American Cyanamid CompanyInventor: David V. Petrocine
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Patent number: 4556649Abstract: Insecticidally active novel substituted malonic acid diamide insecticides of the formula ##STR1## wherein R.sup.1 represents aryl or heteroaryl, each of which can optionally be substituted,R.sup.2 represents hydrogen or trialkylsilyl, and represents alkyl, cycloalkyl, alkenyl, alkinyl, aralkyl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, alkylsulphenyl, arylsulphenyl, alkylsulphonyl, arylsulphonyl, alkylaminosulphonyl, dialkylaminosulphonyl, arylaminosulphonyl or arylalkylaminosulphonyl, each of which can optionally be substituted, and represents radicals of the formula--CO--NR.sup.5 R.sup.6whereinR.sup.5 and R.sup.6 independently of one another represent hydrogen, alkyl, cycloalkyl, aryl, alkylaminocarbonyl, arylaminocarbonyl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, alkylsulphonyl or arylsulphonyl, it being possible for these radicals to be optionally substituted,R.sup.3 represents hydrogen or the radical R.sup.4,R.sup.7 and R.sup.Type: GrantFiled: December 21, 1984Date of Patent: December 3, 1985Assignee: Bayer AktiengesellschaftInventors: Herbert Salzburg, Rudolf Fauss, Kurt Findeisen, Bernhard Homeyer
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Patent number: 4551460Abstract: Pyrido[2,1-b]quinazoline derivatives of the formulas ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as hereinafter set forth, are described. The compounds of formulas I and II are useful as agents for the treatment of allergic conditions as well as for the treatment of vascular disorders involving thrombosis.Type: GrantFiled: March 2, 1983Date of Patent: November 5, 1985Assignee: Hoffmann-La Roche Inc.Inventor: Jefferson W. Tilley
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Patent number: 4503232Abstract: The invention provides a novel method for the preparation of an .alpha.-ketoamide imine having a characteristic structure expressed by the formula ##STR1## in which R is a group such as an alkyl, aryl or the like group, in a one-step reaction in which a halogen-containing organic compound reacts with a primary amine and carbon monoxide in the presence of a carbonylation catalyst. The product compound is useful as an intermediate for the synthesis of various kinds of organic compounds including medicines and agricultural chemicals.Type: GrantFiled: September 24, 1982Date of Patent: March 5, 1985Assignee: Agency of Industrial Science & TechnologyInventors: Toshiaki Kobayashi, Masato Tanaka
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Patent number: 4501746Abstract: Novel N,N-disubstituted carboxamide derivatives useful as herbicides, fungicides and aquatic plant growth regulators.Type: GrantFiled: September 15, 1982Date of Patent: February 26, 1985Assignee: Eli Lilly and CompanyInventor: Eriks V. Krumkalns
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Patent number: 4460480Abstract: The present invention relates to novel oligomers of the formula R.sub.f --E--S--M.sub.1 ].sub.x [M.sub.2 ].sub.y H, and mixutes thereof, wherein R.sub.f is a perfluoroalkyl group, E is a linkage group, --M.sub.1 -- represents a hydrophilic monomer unit, --M.sub.2 -- represents a hydrophobic monomer unit, x and y represent the number of monomer units present in the novel oligomers. The sum of x and y is between 4 and 500 and x/(x+y) is between 1 and 0.5. The novel oligomers are useful as additives in protein foam type fire fighting compositions improving foam expansion, foam drainage and extinguishing times and reducing flammability of hydrocarbon contaminated protein foams. The novel oligomers are further useful as surface tension depressants providing improved wetting, spreading and leveling properties in aqueous systems.Type: GrantFiled: March 13, 1980Date of Patent: July 17, 1984Assignee: Ciba-Geigy CorporationInventors: Eduard K. Kleiner, Thomas W. Cooke, Robert A. Falk
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Patent number: 4435330Abstract: Amphoteric branched sulfatobetaines of the formula ##STR1## wherein R.sub.f is perfluoroalkyl or perfluoroxyperfluoroalkyl; R.sub.1 is a direct bond or a divalent connecting group; R.sub.2, R.sub.3, and R.sub.4 are independently hydrogen or lower alkyl; R.sub.5, R.sub.6 and R.sub.7 are independently lower alkyl, and R.sub.6 may additionally represent aralkyl, and R.sub.6 and R.sub.7 taken together with the nitrogen to which they are attached may also represent piperidino or morpholino and R.sub.5, R.sub.6 and R.sub.7 taken together may also represent pyridyl, acridyl or quinolyl and salts thereof, their preparation and use as surfactants are disclosed.Type: GrantFiled: December 29, 1982Date of Patent: March 6, 1984Assignee: Ciba-Geigy CorporationInventor: Robert A. Falk