Chalcogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding (e.g., 4-hydroxy -3-pyrrolidinemethanol, Etc.) Patents (Class 548/556)
-
Patent number: 4913721Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.Type: GrantFiled: October 31, 1988Date of Patent: April 3, 1990Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey
-
Patent number: 4906634Abstract: Novel N-[4-(aminosubstituted)phenyl]methanesulfonamides and their use as cardiovascular agents, especially as antiarrhythmic agents are described. Pharmaceutical formulations containing such compounds are also discussed.Type: GrantFiled: March 8, 1988Date of Patent: March 6, 1990Assignee: Schering A.G.Inventors: Stanley S. Greenberg, William C. Lumma, Jr., Klaus Nickisch, Ronald A. Wohl
-
Patent number: 4904679Abstract: Pyrrolophenylalkanolamines of the formula ##STR1## R.sup.1 and R.sup.2 represent hydrogen or various radicals, R.sup.3 represents hydrogen, acyl or trialkylsilyl,R.sup.4 represents hydrogen or alkyl,R.sup.5 represents hydrogen, or, together with R.sup.3, represents ##STR2## wherein R.sup.7 represents hydrogen or alkyl, andR.sup.6 represents branched or cyfclic alkyl, which is optionally substituted,and salts thereof promote the yield of animals. Many new intermediates are also shown.Type: GrantFiled: April 22, 1988Date of Patent: February 27, 1990Assignee: Bayer AktiengesellschaftInventors: Hartmund Wollweber, Jurgen Stoltefuss, Friedrich Berschauer, Ann de Jong, Martin Scheer
-
Patent number: 4895847Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halogen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].Type: GrantFiled: September 21, 1988Date of Patent: January 23, 1990Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
-
Patent number: 4894388Abstract: The specificity of glycosidase inhibitory activity of the novel 1,4-dideoxy-1,4-imino-L-allitol is substantially changed by substituting the ring nitrogen with an alkyl or benzyl substituent.Type: GrantFiled: December 22, 1988Date of Patent: January 16, 1990Assignee: Monsanto CompanyInventor: George W. J. Fleet
-
Patent number: 4876268Abstract: Acylated derivatives of 1,4-dideoxy-1,4-imino-L-arabinitol and their N-alkyl and N-hydroxyalkyl derivatives in which all the free hydroxyl groups are acylated with acyl groups having from one to six carbon atoms and in which the N-alkyl substituents in the N-alkyl and N-hydroxyalkyl derivatives contain from one to fourteen carbon atoms are disclosed.Type: GrantFiled: November 3, 1988Date of Patent: October 24, 1989Assignee: G. D. Searle & Co.Inventors: Francis J. Koszyk, Richard A. Partis, Richard A. Mueller
-
Patent number: 4827019Abstract: Photographic coupler solvents comprising aromatic carboxylic esters such as phthalates and isophthalates having bulky or branched ester substituents are described for incorporation in photographic emulsions and elements. The solvents are preferably employed in the cyan layer to protect the cyan dye against ferrous ion reduction. The solvents also provide improvements in yellow dye stability to light, cyan dye stability in the dark and magenta dye stability to heat and light.Type: GrantFiled: January 12, 1987Date of Patent: May 2, 1989Assignee: Eastman Kodak CompanyInventor: Sundaram Krishnamurthy
-
Patent number: 4802913Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.Type: GrantFiled: August 5, 1986Date of Patent: February 7, 1989Assignee: Imperial Chemical Industries PLCInventors: John Clough, Christopher R. A. Godfrey
-
Patent number: 4792556Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.Type: GrantFiled: April 28, 1986Date of Patent: December 20, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: D. V. K. Murthy, Michael C. Venuti, John M. Young
-
Patent number: 4766233Abstract: Herbicidal utility for 2-aryl-1,2,4-triazine-3,5(2H,4H)-diones and sulfur analogs is disclosed and exemplified. Many of the disclosed compounds are novel. Methods for preparing the herbicidal compounds and intermediates therefor are also disclosed.Type: GrantFiled: December 12, 1985Date of Patent: August 23, 1988Assignee: FMC CorporationInventor: John W. Lyga
-
Patent number: 4766110Abstract: Novel inhibitors of angiotensin converting enzyme are disclosed which have the general formula ##STR1## wherein R.sub.1 and/or R.sub.3 form complex amides and imides thereof, R.sub.4 and R.sub.5 form with --N--C-- a 4-6 membered ring structure as described and the other R substituents are selected from a variety of disclosed groups.Type: GrantFiled: October 31, 1986Date of Patent: August 23, 1988Inventors: James W. Ryan, Alfred Chung
-
Patent number: 4731369Abstract: Amides and esters of 2-[N-(hydroxypiperidinoalkyl) and (hydroxypyrrolidinoalkyl) aminosulfonyl]-6-nitrobenzoic acids are disclosed to have activity in increasing the sensitivity of hypoxic tumor cells to therapeutic radiation. Also disclosed are methods of preparing such compounds, pharmaceutical compositions including such compounds and methods of treating patients in need of therapeutic radiation with effective amounts of such compounds.Type: GrantFiled: June 26, 1987Date of Patent: March 15, 1988Assignee: Merck & Co. Inc.Inventors: Edward L. Engelhardt, Walfred S. Saari
-
Patent number: 4721722Abstract: A new class of anti-spasmodic compounds having two branch chains and containing quaternary nitrogen is provided. The compounds have the general formula: ##STR1## wherein R.sub.1 and R.sub.2 are defined hereinbelow and m is an integer from 0 to 3.Type: GrantFiled: July 12, 1985Date of Patent: January 26, 1988Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
-
Patent number: 4716236Abstract: A method for preparing an ester having the structure ##STR1## in which A is an acid residue; R, same or different is H, lower alkyl, aryl, or in which both R together form a ring structure and R' is H, lower alkyl or aryl. The method comprises combining a first compound having the structure ##STR2## and a second compound which is an acyl halide corresponding to A, said combining being performed in the presence of an organic acid.Type: GrantFiled: December 5, 1985Date of Patent: December 29, 1987Assignee: Miles Laboratories, Inc.Inventors: Frederick E. Ward, Kin F. Yip
-
Patent number: 4665174Abstract: A process for preparing cyclopentenone derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or lower alkenyl, R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted ar(lower)alkyl and A is the residue of a nucleophilic agent from which a hydrogen atom is excluded, which comprises reacting a 3-hydroxy-4-cyclopentenone compound of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above with a nucleophilic agent of the formulaA--H (III)wherein A is as defined above.The cyclopentenone derivatives of the formula (I) are useful as pharmaceuticals, agricultural chemicals, perfumes and as intermediates for the preparation of agricultural chemicals, pharmaceuticals and perfumes.Type: GrantFiled: May 11, 1982Date of Patent: May 12, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Masayoshi Minai, Tadashi Katsura
-
Patent number: 4636505Abstract: Acylanilides of the formula ##STR1## wherein R.sup.1 and R.sup.2, the same or different, each is cyano, carbamoyl, nitro, halogeno, perfluoroalkyl or other defined substituents;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or alkyl, or is joined to R.sup.5 ;R.sup.5 is hydrogen, hydroxy, alkoxy or acyloxy or is joined to R.sup.4 ;R.sup.6 is alkyl or halogenoalkyl, or has the formula --A.sup.3 --R.sup.8 or --A.sup.4 --X.sup.2 --A.sup.5 --R.sup.9 ;A.sup.1 and A.sup.4, the same or different, each is alkylene;A.sup.2, A.sup.3 and A.sup.5, the same or different, each is a direct link or alkylene;X.sup.1 and X.sup.2, the same or different, each is oxygen, sulphur, sulphinyl, sulphonyl, imino or alkylimino;R.sup.7 and R.sup.9, the same or different, each is alkyl, alkenyl, hydroxyalkyl, cycloalkyl, phenyl optionally substituted, naphthyl or heterocyclic optionally substituted;and R.sup.8 is phenyl, naphthyl or heterocyclic as defined above for R.sup.7 or R.sup.Type: GrantFiled: July 15, 1983Date of Patent: January 13, 1987Assignee: Imperial Chemical Industries PLCInventor: Howard Tucker
-
Patent number: 4602023Abstract: The present invention provides various novel diphenic acid monoamide compounds, novel pharmaceutical compositions and methods of use thereof, as well as novel methods of synthesis therefor. The novel diphenic acid monoamides of the present invention are leukotriene antagonists, 5-lipoxygenase inhibitors, and mediator release inhibitors providing activity useful for treating asthma, allergies, cardiovascular diseases, migraines, and immunoinflammatory conditions.Type: GrantFiled: June 3, 1985Date of Patent: July 22, 1986Assignee: Warner-Lambert CompanyInventors: John S. Kiely, Suchin Huang
-
Patent number: 4550107Abstract: Disclosed are novel condensed diazepinones of formula I ##STR1## wherein B is a fused ring selected from ##STR2## X is --CH-- or, when B is ortho-phenylene, X can also be nitrogen; A.sub.1 is C.sub.1 -C.sub.2 alkylene; A.sub.2 is C.sub.1 -C.sub.2 when it is in the 2-position relative to the saturated heterocyclic ring nitrogen or a single bond or methylene when it is in the 3- or 4-position; R.sub.1 is C.sub.1 -C.sub.3 alkyl; R.sub.2 is C.sub.1 -C.sub.7 alkyl, optionally hydroxy-substituted on at least one of its second to seventh carbon, or C.sub.3 -C.sub.7 cycloalkyl, optionally hydroxy substituted, or C.sub.3 -C.sub.7 cycloalkylmethyl; or R.sub.1 and R.sub.2 can, together with the nitrogen therebetween, be a 4- to 7-membered saturated monocyclic, heterocyclic ring which can optionally include an oxygen or N--CH.sub.3 ; R.sub.3 is hydrogen, chlorine, or methyl; R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.5 is hydrogen, chlorine or C.sub.1 -C.sub.Type: GrantFiled: March 14, 1985Date of Patent: October 29, 1985Assignee: Dr. Karl Thomae GmbHInventors: Wolfhard Engel, Gunter Trummlitz, Wolfgang Eberlein, Gerhard Mihm, Gunther Schmidt, Rudolf Hammer, Antonio Giachetti
-
Patent number: 4539408Abstract: Quaternary sulfoalkyl or sulfoalkenyl salts of tertiary amine bases are prepared by reacting the tertiary amine bases at elevated temperatures with a hydroxy alkane sulfonic acid or a hydroxyalkene sulphonic acid.Type: GrantFiled: April 28, 1978Date of Patent: September 3, 1985Assignee: Agfa-Gevaert AktiengesellschaftInventors: Helmut Kampfer, Marie Hase, Max Glass
-
Patent number: 4508724Abstract: Novel aryloxymethylpyrrolidinols and piperidinols are provided of the formula: ##STR1## wherein R.sup.1 is hydrogen, loweralkyl and phenylloweralkyl; R.sup.2 is hydrogen, loweralkyl and acyl; R.sup.3 is phenyl, naphthyl, 4-indanyl and 5-indanyl; m is 2 or 3 and n is 1 or 2; and the pharmaceutically acceptable salts thereof, having antiarrhythmic, antidepressant and antihypertensive activity.Type: GrantFiled: February 3, 1984Date of Patent: April 2, 1985Assignee: A. H. Robins Company, Inc.Inventors: Chandler R. Taylor, Jr., Harold F. Stauffer, Jr.
-
Patent number: 4499273Abstract: There are disclosed new organic peroxides having two peroxy functional groups and containing in their molecule an atom of salified aminic nitrogen, having the general formula: ##STR1## in which: R.sub.1, R.sub.2 are each an alkyl radical having 1 to 8 carbon atoms, optionally aryl-substituted, preferably a tertiary alkyl group such as t.butyl, t.amyl, t.octyl and cumyl;R.sub.3 is a hydrogen, an alkyl radical having 1 to 8 carbon atoms, a cycloalkyl having 5-6 carbon atoms in the ring, an aryl, an arylalkyl optionally halogen, alkoxy-, carboalkoxy-, alkyl-, mono- or poly-substituted;R.sub.4 is the methylene, ethylene or trimethylene radical, optionally halogen-, alkoxy-, carboalkoxy-, aryl-, alkyl-, mono- or poly-substituted;R.sub.Type: GrantFiled: December 21, 1982Date of Patent: February 12, 1985Inventors: Alberto Fontana, Renzo Fontanelli, Egeo Sacrini, Osvaldo Cicchetti
-
Patent number: 4473394Abstract: This invention relates to pyrrole sulfonamides which are useful as herbicides. Typical of the pyrrole sulfonamides of the instant application in N-[(4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocarbonyl]-2,5-dimethyl-1H-p yrrole-3-sulfonamide.Type: GrantFiled: September 27, 1982Date of Patent: September 25, 1984Assignee: E. I. DuPont De Nemours & CompanyInventors: John C. Budzinski, George Levitt
-
Patent number: 4466981Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are lower alkoxy or lower alkylthio;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, halo, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and n is 0, 1 or 2; andW is alkyl of one to seven carbon atoms.Type: GrantFiled: October 27, 1982Date of Patent: August 21, 1984Assignee: Syntex (U.S.A.) Inc.Inventors: Gordon H. Jones, Michael C. Venuti, Young, John M.
-
Patent number: 4458090Abstract: Novel .gamma.-lactone derivatives are provided. These lactone derivatives, when reacted with hydrogen halide in alcohol, yield .gamma.-halogeno-.delta.-unsaturated carboxylic acid esters. This ring-opening process is useful for the purpose of increasing the yield of pyrethrin analogs which are of value as insecticides and agricultural chemicals. Thus, the .gamma.-lactone derivatives by-produced in the production process for dihalogenovinyl chrysanthemumates are caused to undergo ring-opening reaction to yield the corresponding .gamma.-halogeno-.delta.-unsaturated carboxylic acid esters which are important intermediates for said pyrethrin analogs.Type: GrantFiled: October 15, 1981Date of Patent: July 3, 1984Assignee: Kuraray Co., Ltd.Inventors: Mori Fumio, Omura Yoshiaki, Nishida Takashi, Itoi Kazuo
-
Patent number: 4419363Abstract: Novel 1-aryloxy-3-amidoamidoalkylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart diseases. Representative of the compounds disclosed is 1-(o-cyanophenoxy)-3-.beta.-(2-thenamidoacetamido)ethylaminopropan-2-ol.Type: GrantFiled: June 4, 1982Date of Patent: December 6, 1983Assignee: Imperial Chemical Industries PLCInventor: Leslie H. Smith
-
Patent number: 4414219Abstract: Novel azacycloalkanes, azacycloalkenes and derivatives thereof and methods of preparing same are described. These compounds are useful as antidepressants, anticonvulsants, tranquilizers and analgetics.Type: GrantFiled: August 1, 1980Date of Patent: November 8, 1983Assignee: American Hoechst CorporationInventors: Lawrence L. Martin, Helen H. Ong, Vernon B. Anderson, Charles A. Crichlow
-
Patent number: 4383112Abstract: Chiral Schiff bases according to the general formula: ##STR1## and transition metal complexes thereof, wherein C.sup.* is an asymmetric carbon atom, R.sup.1 and R.sup.2, which may be the same or different are alkyl, aralkyl, aryl or alkaryl, R.sup.3 is hydrogen, alkyl, aralkyl, aryl or alkaryl, R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or lower alkyl or, where n is 1, may with the cyclic ring to which CR.sup.4 R.sup.Type: GrantFiled: July 8, 1980Date of Patent: May 10, 1983Assignee: Imperial Chemical Industries LimitedInventors: Dale A. Laidler, David J. Milner
-
Patent number: 4368067Abstract: Pyrrole sulfonamides are useful as agricultural chemicals.Type: GrantFiled: March 25, 1981Date of Patent: January 11, 1983Assignee: E. I. Du Pont de Nemours and CompanyInventors: John C. Budzinski, George Levitt