Polycyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 548/207)
-
Patent number: 5094683Abstract: Herbicidal sulphonylaminocarbonyltriazolinones of the formula ##STR1## in which R.sup.1 represents hydrogen, hydroxyl or amino, or represents an optionally substituted radical from the series comprising alkyl, alkenyl, akinyl, cycloalkyl, aralkyl, aryl, alkoxy, alkenyloxy, alkylamino and dialkylamino,R.sup.2 represents hydrogen hydroxyl, mercapto or amino, or represents an optionally substituted radical from the series comprising alkyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, alkoxy, alkylamino and dialkylamino, andR.sup.3 represents an optionally substituted radical from the series comprising alkyl, aralkyl, aryl and heteroaryl, and salts thereof. Intermediates of the formula ##STR2## in which A.sup.1 represents in each case optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy or dialkylamino andA.sup.2 represents hydrogen, or represents in each case optionally substituted alkyl, cycloalkyl, aralkyl, aryl or alkoxy,provided that both A.sup.1 and A.sup.Type: GrantFiled: April 29, 1991Date of Patent: March 10, 1992Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Klaus-Helmut Muller, Michael Schwamborn, Peter Babczinski, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
-
Patent number: 5055585Abstract: Novel aminoketones useful as central muscle relaxants and their preparation processes are disclosed. The disclosed processes are novel processes which do not use any heavy metal in view of the facts that their products are will be used as drugs and which require no complex purification step such as liberation of the aminoketones from their hydrochlorides or the like.Type: GrantFiled: January 31, 1991Date of Patent: October 8, 1991Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Akira Matsubara, Kazuya Sakai, Hideki Tanada, Hironori Komatsu
-
Patent number: 5047554Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.Type: GrantFiled: January 31, 1990Date of Patent: September 10, 1991Assignee: Pfizer Inc.Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
-
Patent number: 5037841Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n denotes a number from 1 to 19, andB denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.Type: GrantFiled: April 12, 1989Date of Patent: August 6, 1991Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Peter-Rudolf Seidel, Jorg Traber, Thomas Glaser
-
Patent number: 5030643Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: July 14, 1989Date of Patent: July 9, 1991Assignee: ICI Americas Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying Kwong Yee
-
Patent number: 5021438Abstract: Novel compounds having an affinity for 5-hydroxytryptamine receptors of the formula ##STR1## in which R.sup.1 stands for H, alkyl, aralkyl or heteroarylalkyl,X stands for H, OCH.sub.3, OH, SCH.sub.3, halogen, CN or CONH.sub.2,Y stands for a straight-chain or branched, saturated or unsaturated alkylene chain having up to 6 carbon atomsandZ stands for a group of the formula ##STR2## --OR.sup.4, --SO.sub.m R.sup.5, --COOR.sup.6 or CONR.sup.7 R.sup.8 or salts thereof.Type: GrantFiled: March 15, 1989Date of Patent: June 4, 1991Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber
-
Patent number: 5003074Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl or aryl, m and n are 0 or 1, and A is a divalent organic radical which, with (CR.sup.1 R.sup.2).sub.m NF--SO.sub.2 (CR.sup.3 R.sup.4).sub.n groups, forms a 5- to 8-membered ring, are admirably suitable fluorinating agents for fluorinating carbon atoms, especially as stereospecific fluorinating agents, when the compounds contain a chiral carbon atom and are in optically active form. The compounds of formula I are prepared by reacting the corresponding silated sulfonamides, wherein the NF group is replaced by an N-SiR.sup.7 R.sup.8 R.sup.9 group and R.sup.7, R.sup.8 R.sup.9 are each independently C.sub.1 -C.sub.12 alkyl, cyclopentyl, cyclohexyl, benzyl or phenyl, with a fluorinating agent.Type: GrantFiled: September 28, 1988Date of Patent: March 26, 1991Assignee: Ciba-Geigy CorporationInventors: Thomas Allmendinger, Edmond Differding, Robert W. Lang
-
Patent number: 4994512Abstract: Disclosed are poly-methine compounds having the formula: ##STR1## wherein R.sup.1 is an unsubstituted or substituted alkoxycarbonyl, cycloalkoxycarbonyl or aryloxycarbonyl radical; an unsubstituted or substituted carbamoyl radical; or an unsubstituted or substituted alkylsulfonyl, cycloalkylsulfonyl or arylsulfonyl radical, or an unsubstituted or substituted aryl radical;R.sup.2 is an unsubstituted or substituted alkyl, cycloalkyl or aryl radical;R.sup.3 is hydrogen, alkyl, --OR.sup.2 or halogen; andL is an organic linking group bonded by non-oxo carbon atoms to the oxygen atoms adjacent to L. Also disclosed are admixtures of about 100 to 10,000 ppm of at least one of the poly-methine compounds and certain condensation polymers. The resulting polymer compositions are useful to protect substrates or materials susceptible to degradation by ultraviolet light.Type: GrantFiled: May 1, 1989Date of Patent: February 19, 1991Assignee: Eastman Kodak CompanyInventors: Max A. Weaver, Clarence A. Coates, Wayne P. Pruett, Samuel D. Hilbert
-
Patent number: 4968679Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: May 22, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
-
Patent number: 4960901Abstract: A thermal imaging method is provided which comprises heating imagewise a di- or triarylmethane compound possessing within its di- or triarylmethane structure an aryl group substituted in the ortho position to the meso carbon atom with a moiety ring-closed on the meso carbon atom directly through a nitrogen atom, which nitrogen atom is also bound to a group with a masked acyl substituent that undergoes fragmentation upon heating to liberate the acyl group for effecting intramolecular acylation of said nitrogen atom to form a new group in the ortho position whereby the di- or triarylmethane compound is rendered colored in an imagewise pattern corresponding to said imagewise heating.Type: GrantFiled: October 29, 1987Date of Patent: October 2, 1990Assignee: Polaroid CorporationInventors: Alan L. Borror, Ernest W. Ellis
-
Patent number: 4957931Abstract: Disclosed are 1,2-benzisoxazole and 1,2-benzisothiazole derivatives represented by formula I ##STR1## wherein X represents oxygen or sulfur; Z represents carbon (CH) so as to complete the imidazol-1-yl ring radical or Z represents nitrogen (N) so as to complete the 1,2,4-triazol-l-yl ring radical; R.sub.1 represents hydrogen, lower alkenyl, lower alkynyl, aryl-lower alkyl or lower alkyl; R.sub.2 represents hydrogen, lower alkenyl, lower alkynyl, aryl-lower alkyl or lower alkyl; or R.sub.1 and R.sub.2 combined represent lower alkylene; or R.sub.1 combined with R.sub.5 located on the Z-carbon atom of the imidazolyl radical represents C.sub.2 -C.sub.4 -alkylene; R.sub.3 and R.sub.4 independently represent hydrogen, lower alkyl, cycloalkyl, halogen, trifluoromethyl, cyano, nitro, amino, hydroxy, lower alkanoyloxy, carbocyclic aroyloxy, lower alkoxy, or carbocyclic aryl; or R.sub.3 and R.sub.4, together when located on adjacent carbon atoms, represent lower alkylenedioxy; or R.sub.3 and R.sub.Type: GrantFiled: June 9, 1989Date of Patent: September 18, 1990Assignee: Ciba-Geigy CorporationInventor: Robert M. Bowman
-
Patent number: 4904811Abstract: A Z compound, substantially free of the E-isomers, of the formula ##STR1## in which Q represents Cl or OM,M represents hydrogen or an alkali metal atom,R represents optionally substituted cycloalkyl or the ##STR2## group, R.sup.1 represents hydrogen or alkyl, andX represents hydrogen, alkyl, alkenyl, alkinyl, cyano, optionally substituted cycloalkyl, optionally substituted aryl, or an optionally substituted heterocyclic ring which is optionally fused to a benzene ring.The compounds wherein Q is Cl are produced by reacting the compounds wherein Q is--OM with a chlorinating agent. The products are intermediates for fungicides.Type: GrantFiled: July 10, 1987Date of Patent: February 27, 1990Assignee: Bayer AktiengesellschaftInventor: Winfried Lunkenheimer
-
Patent number: 4900739Abstract: This invention relates to novel spirosuccinimide derivatives, to the processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.Type: GrantFiled: October 20, 1988Date of Patent: February 13, 1990Assignee: American Home Products Corp.Inventor: Jay E. Wroel
-
Patent number: 4873262Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: December 15, 1987Date of Patent: October 10, 1989Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
-
Patent number: 4868188Abstract: Novel 4-(benzisothiazol-3-yl)phenoxyacetic acid 1',1'-dioxides of the formula ##STR1## where X is hydrogen, halogen or loweralkyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 and R.sub.3 are each independently Cl, Br or CH.sub.3, and related compounds, methods for preparing same and methods of treatment by administering compositions containing such a compound are described. These compounds are useful as diuretics.Type: GrantFiled: November 3, 1982Date of Patent: September 19, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventor: Gregory M. Shutske
-
Patent number: 4859692Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: April 16, 1986Date of Patent: August 22, 1989Assignee: ICI Americas Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying Kwong Yee
-
Patent number: 4826976Abstract: This invention relates to a color-shifted dye compounds containing at least one thermally unstable carbamate moiety which are useful in thermal imaging. These compounds may be represented by the formula [M--(X).sub.q ].sub.p D wherein M is a carbamate moiety; X is --N.dbd., --SO.sub.2 -- or --CH.sub.2 --; D taken with X and M represents the radical of a color-shifted organic dye, said carbamate moiety M comprising a tert-alkoxycarbonyl group, ##STR1## wherein R' is halomethyl or alkyl.Type: GrantFiled: December 18, 1987Date of Patent: May 2, 1989Assignee: Polaroid CorporationInventors: Alan L. Borror, Ernest W. Ellis, Donald A. McGowan
-
Substituted pyrazolin-5-ones, composition containing them, and method of combating fungi or bacteria
Patent number: 4767775Abstract: Microbicidal substituted pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl or dialkylaminocarbonylalkyl, or represent in each case optionally substituted oxiranylalkyl, aralkyl, heterocyclyl or aryl andHet represents an optionally substituted heterocyclic radical.Intermediates therefor of the formula ##STR2## in which R is alkyl, are also disclosed.Type: GrantFiled: July 24, 1986Date of Patent: August 30, 1988Assignee: Bayer AktiengesellschaftInventors: Klaus Jelich, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke -
Patent number: 4738709Abstract: This invention relates to herbicidally active substituted benzisoxazole (or benzisothiazole) compounds and to the use of such compounds to control the growth of noxious plants, i.e., weeds.Type: GrantFiled: November 26, 1985Date of Patent: April 19, 1988Assignee: PPG Industries, Inc.Inventor: Donald R. Nielsen
-
Patent number: 4723020Abstract: The present invention relates to new chromogenic amino acid esters and peptide esters of hydroxybenzo(iso)thiazoles and hydroxybenzopyrazoles, processes for their preparation and the use of the new esters as substrates for the analytical detection of esterolytic and/or proteolytic enzymes, for example in body fluids, the esters being incorporated into test agents, in particular test strips, in a suitable manner. The new esters are preferably used for the detection of leukocytes, in particular in urine.Type: GrantFiled: March 11, 1985Date of Patent: February 2, 1988Assignee: Miles Laboratories, Inc.Inventors: Herbert Hugl, Eugen Schnabel
-
Patent number: 4720449Abstract: A thermal imaging method is provided which comprises heating imagewise a di- or triarylmethane compound possessing within its di- or triarylmethane structure an aryl group substituted in the ortho position to the meso carbon atom with a moiety ring-closed on the meso carbon atom directly through a nitrogen atom, which nitrogen atom is also bound to a group with a masked acyl substituent that undergoes fragmentation upon heating to liberate the acyl group for effecting intramolecular acylation of said nitrogen atom to form a new group in the ortho position whereby the di- or triarylmethane compound is rendered colored in an imagewise pattern corresponding to said imagewise heating.Type: GrantFiled: May 14, 1986Date of Patent: January 19, 1988Assignee: Polaroid CorporationInventors: Alan L. Borror, Ernest W. Ellis
-
Patent number: 4703044Abstract: The invention provides novel imidazoquinolines, processes for their preparation and pharmaceutical compositions containing them. The compounds have Formula I ##STR1## wherein A is a C.sub.1 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,B is a C.sub.2 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,R.sup.1 and R.sup.2 are the same or different and are hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxyalkyl, C.sub.1-6 hydroxyalkyl, hydroxy, halogen, nitro, carboxy, carboxylic lower alkyl ester, carbamoyl, carbamoyloxy, cyano, loweralkanoyl, lower alkanoylamino or trifluoromethyl, Het is a heterocyclic group chosen from imidazolyl, imidazolinyl, benzimidazolyl, thiazolyl, thiazolinyl, quinolyl, piperidyl, pryidyl, benzothiazoly and pyrimidyl, any of which heterocyclic groups may be substituted, and x is 0 or 1, and pharmaceutically acceptable salts thereof.The compounds are anti-ulcer/anti-secretory agents.Type: GrantFiled: December 11, 1985Date of Patent: October 27, 1987Assignee: John Wyeth & Brother LimitedInventor: Roger Crossley
-
Patent number: 4673746Abstract: Novel 1,2-benzisoxazoloxyacetic acids and related compounds, methods for preparing same and methods of treatment by administering compositions containing such a compound are described. These compounds are useful as diuretic, uricosuric and antihypertensive agents.Type: GrantFiled: October 27, 1980Date of Patent: June 16, 1987Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Gregory M. Shutske, Linda L. Setescak, Richard C. Allen
-
Patent number: 4667041Abstract: A process for the preparation of a 3-hydrazino-1, 2-benzisothiazole 1,1-dioxide of the formula ##STR1## in which R.sup.1 and R.sup.2 each independently is hydrogen, alkyl, halogen, amino, hydroxyl or carboxyl, andR.sup.3 and R.sup.4 each independently is hydrogen, alkyl, cycloalkyl or aryl,comprising reacting a 3-keto-2H,3H-1,2-benzisothiazole 1,1-dioxide of the formula ##STR2## with a hydrazine of the formula ##STR3## in a molar ratio of 1:1 to 1:50, in an inert solvent, at a temperature between 75.degree. C. and 200.degree. C. and for a reaction time of 15 to 40 hours. The products, some of which are known, are fungicidally active and can also be used as intermediates.Type: GrantFiled: February 28, 1985Date of Patent: May 19, 1987Assignee: Bayer AktiengesellschaftInventors: Herbert Salzburg, Manfred Hajek, Gerd Hanssler
-
Patent number: 4666930Abstract: Compounds of the formula ##STR1## in which R.sup.1 is alkyl, cycloalkyl, aryl or hydrogen,R.sup.2 is --CO--R.sup.3,R.sup.3 is alkyl, alkenyl or cycloalkyl, or is phenyl which is optionally substituted, or is alkoxy or benzyl, or is phenoxy which is optionally substituted, or is phenoxymethyl, alkylamino, cycloalkylamino or phenylamino, orR.sup.1 and R.sup.2 together are a ##STR2## group, R.sup.4 and R.sup.5 each independently is hydrogen, alkyl, cycloalkenyl or phenylalkenyl, or is phenyl which is optionally substituted by alkyl, halogen and/or alkoxy, or is furyl, orR.sup.4 and R.sup.5 together are alkylene having 4 to 6 carbon atoms,are fungicidally active. Those compounds wherein R.sup.3 is alkylamino, cycloalkylamino or phenylamino, with the exception of the compound in which R.sup.1 is hydrogen and R.sup.6 is phenylamino, are new.Type: GrantFiled: March 1, 1985Date of Patent: May 19, 1987Assignee: Bayer AktiengesellschaftInventors: Herbert Salzburg, Manfred Hajek, Gerd Hanssler
-
Patent number: 4656273Abstract: There is described a novel process for producing sulfonylureas of formula I ##STR1## wherein R.sub.1 is hydrogen or alkyl,R.sub.2 is ##STR2## E is .dbd.N-- or .dbd.CH--, R.sub.3 is alkyl, alkoxy or halogen,R.sub.4 is alkyl, cycloalkyl, alkoxy, halogen, alkoxy-alkyl, halo-alkyl or halo-alkoxy,R.sub.5 is hydrogen or alkyl,T is a substituted phenyl group ##STR3## Y is hydrogen or halogen, X is hydrogen, halogen, alkyl, halo-alkyl, alkenyl, halo-alkenyl, alkynyl, alkoxy, halo-alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halo-alkylthio, alkylsulfonyloxy, phenylsulfonyloxy, phenylsulfonyloxy mono- or polysubstituted by alkyl, or is di-alkylsulfamoyl, andA is a bridge member which has 3 or 4 atoms and which contains 1 or 2 hetero atoms, selected from the group consisting of oxygen, sulfur and nitrogen,the said process comprising reacting a silfonamide of the formula IIT--SO.sub.2 --NH.sub.Type: GrantFiled: December 16, 1985Date of Patent: April 7, 1987Assignee: Ciba-Geigy CorporationInventor: Werner Topfl
-
Patent number: 4634716Abstract: Compounds of the formula: ##STR1## where R.sup.3 is ##STR2## where n is 1-3 and the R.sup.a 's and R.sup.b 's are independently hydrogen or loweralkyl; and pharmaceutically acceptable salts thereof; are inhibitors or angiotensin I converting enzyme useful as antihypertensive agents.Type: GrantFiled: May 16, 1983Date of Patent: January 6, 1987Assignee: Merck & Co., Inc.Inventors: William H. Parsons, David Taub
-
Patent number: 4589910Abstract: A 4'-(Benzisothiazol-5-yloxy)-phenylureas of the formula ##STR1## where R.sup.1 and R.sup.2 are each a saturated straight-chain or branched aliphatic radical of 1 to 10 carbon atoms, an unsaturated straight-chain or branched aliphatic radical of 3 to 10 carbon atoms, or an araliphatic or aromatic radical which may be substituted by 1, 2 or 3 C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, cyano, halogen, nitro, monofluoromethyl or trifluoromethyl groups, or are each alkoxy of 1 to 6 carbon atoms, R.sup.2 may furthermore be hydrogen, or R.sup.1 and R.sup.2, together with the nitrogen atom, may be members of a 5-membered or 6-membered ring which may contain further nitrogen and/or oxygen atoms as heteroatoms, and X is hydrogen, trifluoromethyl or chlorine, processes for their preparation, and herbicides containing ureas of the formula I as active ingredients.Type: GrantFiled: April 30, 1985Date of Patent: May 20, 1986Assignee: BASF AktiengesellschaftInventors: Helmut Hagen, Hans Ziegler, Bruno Wuerzer
-
Patent number: 4495352Abstract: 1-Aryloxy-3-[(3-indolyl)-tert.-butyl]amino-2-propanols having a heterocyclic aryl-attached substituent or aryl-fused heterocyclic ring are antihypertensive agents having vasodilator and adrenergic .beta.-receptor blocking action.Type: GrantFiled: December 3, 1981Date of Patent: January 22, 1985Assignee: Mead Johnson & CompanyInventors: William E. Kreighbaum, William T. Comer
-
Patent number: 4409389Abstract: Disclosed is a novel process and product involving the manufacture in advantageously high yields of imidazole compounds corresponding to the general formula: ##STR1## wherein a preferred embodiment of the process comprises contacting a diamine salt of the formula ##STR2## with a biscarbonyl compound of the structure ##STR3## in an acid medium, wherein R, R.sub.1 and R.sub.2 each represents hydrogen or any group which does not hinder the cyclization reaction or lead to degradation of the reactants or imidazole products, and A.sup.- is an anion equivalent such as that of mineral acids, sulfonic acids and carboxylic acids.Type: GrantFiled: May 10, 1982Date of Patent: October 11, 1983Assignee: Eastman Kodak CompanyInventors: Michael Bellas, John Duvall
-
Patent number: 4398028Abstract: The present invention concerns compounds of formula ##STR1## wherein X is O, S or NH; n is 1 or 2 and A is a 5-membered heterocyclic ring, wherein the bicyclic system may be substituted. The compounds are useful as myotonolytic and anti-hypertensive agents.Type: GrantFiled: June 24, 1981Date of Patent: August 9, 1983Assignee: Sandoz Ltd.Inventor: Peter Neumann
-
Patent number: 4379157Abstract: The invention relates to new sulphonyl compounds of the general formula ##STR1## wherein X is a halogen atom, a phenoxy group, or an alkyl group or alkoxy group having 1-4 carbon atoms and substituted, if desired, with halogen;R.sub.1 is a cyano group, andR.sub.2 is an amino group which, if desired, may be substituted with halogen, with one or two alkenyl groups or alkynyl groups having 2-6 carbon atoms or with one or two alkyl groups having 1-6 carbon atoms, which alkyl groups, together with the nitrogen atom to which they are bound, may form a saturated heterocyclic ring, which ring may also contain a second hetero atom selected from the group consisting of nitrogen, oxygen and sulphur, or which alkyl groups may be substituted with an alkoxy group, having 1-4 carbon atoms, or with a dialkylamino group having 2-6 carbon atoms the alkyl groups of which, together with the nitrogen atom to which they are bound, may form a saturated heterocyclic ring;or whereinR.sub.1 and R.sub.Type: GrantFiled: January 19, 1981Date of Patent: April 5, 1983Assignee: Duphar International Research B.V.Inventors: Roelof van Hes, Arnoldus C. Grosscurt, Wouter Balk
-
Patent number: 4343944Abstract: An indolinospiropyrane compound of the formula ##STR1## wherein R.sub.1 represents alkyl which has at most 12 carbon atoms and is unsubstituted or substituted by halogen, hydroxyl, cyano, lower alkoxy or lower alkyl-carbonyloxy, or cycloalkyl, phenyl or benzyl or phenyl or benzyl which are substituted by halogen, nitro, lower alkyl or lower alkoxy,R.sub.2 represents hydrogen, alkyl which has at most 12 carbon atoms and is unsubstituted or substituted by halogen, hydroxyl, cyano, lower alkoxy or lower alkyl-carbonyloxy, or cycloalkyl or benzyl which is unsubstituted or substituted by halogen, nitro, lower alkyl or lower alkoxy, orR.sub.1 and R.sub.Type: GrantFiled: December 5, 1980Date of Patent: August 10, 1982Assignee: Ciba-Geigy CorporationInventor: Peter Burri
-
Patent number: 4314943Abstract: 1-Aryloxy-3-[(3-indolyl)-tert.-butyl]amino-2-propanols having a heterocyclic aryl-attached substituent or aryl-fused heterocyclic ring are antihypertensive agents having vasodilator and adrenergic .beta.-receptor blocking action.Type: GrantFiled: February 13, 1979Date of Patent: February 9, 1982Assignee: Mead Johnson & CompanyInventors: William E. Kreighbaum, William T. Comer
-
Patent number: 4311839Abstract: In one aspect, this invention relates to a method of synthesizing certain 3-(4'-OP-carbocyclic aryl)-3-(carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxides (and -2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxides) by reacting (a) a 3-(4'-OP-carbocyclic aryl)-benz[d]isothiazole-1,1-dioxide wherein P is a protecting group or a 3-(4'-OP-carbocyclic aryl)-naphtho[1,8-de]-1,2-thiazine-1,1-dioxide wherein P is a protecting group and (b) a carbocyclic aryllithium compound to give (c) the corresponding 3-(4'-OP-carbocyclic aryl)-3-(carbocyclic aryl)-2,3-dihydrobenz[d]-isothiazole-1,1-dioxide or the corresponding 3-(4'-OP-carbocyclic aryl)-3-(carbocyclic aryl)-2,3-dihydronaphtho-[1,8-de]-1,2-thiazine-1,1-dioxide.Type: GrantFiled: December 22, 1980Date of Patent: January 19, 1982Assignee: Polaroid CorporationInventors: Alan L. Borror, Louis Cincotta, James W. Foley, Marcis M. Kampe
-
Patent number: 4311847Abstract: The present invention is concerned with novel xanthene compounds of the formula ##STR1## wherein R' is alkyl and n is 0 or 1, which compounds are useful in photographic products and processes.Type: GrantFiled: October 6, 1980Date of Patent: January 19, 1982Assignee: Polaroid CorporationInventors: Richard L. Cournoyer, James W. Foley
-
Patent number: 4310673Abstract: The present invention is concerned with novel xanthene compounds of the formula ##STR1## wherein R is hydrogen or alkyl, which compounds are useful in photographic products and processes.Type: GrantFiled: October 6, 1980Date of Patent: January 12, 1982Assignee: Polaroid CorporationInventors: James W. Foley, Louis Locatell, Jr., Charles M. Zepp
-
Patent number: 4307017Abstract: The present invention is concerned with novel xanthene compounds of the formulae ##STR1## and ##STR2## wherein each R.sup.1 the same or different is alkyl or benzyl; each R.sup.2 the same or different is an electron-withdrawing group having a positive sigma value greater than 0.6; R.sup.3 is hydrogen or alkyl; R.sup.4 is alkyl; and n is 0 or 1, said R.sup.2 group being ortho, meta or para to said N atom. The subject compounds are useful as light-screening dyes in photographic products and processes.Type: GrantFiled: October 6, 1980Date of Patent: December 22, 1981Assignee: Polaroid CorporationInventors: Richard L. Cournoyer, James W. Foley
-
Patent number: 4290955Abstract: In one embodiment, the present invention is concerned with novel xanthene compounds of the formula ##STR1## wherein each R.sup.1 the same or different is hydrogen or alkyl, each R.sup.2 the same or different is alkyl or phenyl, R.sup.3 is phenyl or alkyl, Y is an electron-withdrawing group and A is an anion. In another embodiment, the present invention is concerned with photographic products and processes employing these xanthene compounds.Type: GrantFiled: May 30, 1980Date of Patent: September 22, 1981Assignee: Polaroid CorporationInventors: Louis Cincotta, James W. Foley
-
Patent number: 4290950Abstract: In one embodiment, the present invention is concerned with novel xanthene compounds of the formula ##STR1## wherein X is ##STR2## wherein R' is alkyl, Y is an electron-withdrawing group and n is 0 or 1. In another embodiment, the present invention is concerned with photographic products and processes employing these xanthene compounds.Type: GrantFiled: May 30, 1980Date of Patent: September 22, 1981Assignee: Polaroid CorporationInventors: Richard L. Cournoyer, James W. Foley
-
Patent number: 4290951Abstract: In one embodiment, the present invention is concerned with novel xanthene compounds of the formula ##STR1## wherein X is ##STR2## wherein R' is alkyl; Y is an electron-withdrawing group and A is an anion. In another embodiment, the present invention is concerned with photographic products and processes employing these xanthene compounds.Type: GrantFiled: May 30, 1980Date of Patent: September 22, 1981Assignee: Polaroid CorporationInventors: James W. Foley, Louis Locatell, Jr., Charles M. Zepp
-
Patent number: 4283538Abstract: In one embodiment, the present invention is concerned with novel triarylmethane compounds possessing in their triaryl structure a 4'-oxo-1'-naphthylidene (or a 4'-oxo-1'-phenylidene) moiety and a phenyl moiety substituted in the ortho-position to the central carbon atom with the group ##STR1## wherein R is an alkyl group or a phenyl group, unsubstituted or substituted with a solubilizing group; R' is selected from ##STR2## wherein R" is methyl, unsubstituted or substituted with one or two halo groups or substituted with a phenyl, alkoxy or phenoxy group and ##STR3## wherein Y is an electron-withdrawing group; and R and R' taken with said ##STR4## represents ##STR5## In another embodiment the present invention is concerned with a method of synthesizing the aforementioned compounds by reacting, e.g., a 2-R'-3-(4'-hydroxy-1'-phenyl/naphthyl)-3-(phenyl/naphthyl)-2,3-dihydrobenz [d]isothiazole-1,1-dioxide with an alkylation reagent in the presence of base.Type: GrantFiled: December 26, 1979Date of Patent: August 11, 1981Assignee: Polaroid CorporationInventor: James W. Foley
-
Patent number: 4283537Abstract: In one embodiment, the present invention is concerned with 3,3-disubstituted sulfam(na)phthaleins wherein one of the 3-substituents is derived from a perhalomethylcarbinol-substituted phenol or 1-naphthol useful as intermediates in the preparation of certain N-acylated sulfam(na)phthalein compounds, which compounds find utility, e.g., as pH-sensitive indicator dyes or photographic light-screening dyes.In another embodiment, the present invention is concerned with a method of synthesizing said sulfam(na)phthalein intermediates by reacting certain 3-substituted-benz[d]isothiazole-1,1-dioxides (or 3-substituted-naphtho[1,8-de]-1,2-thiazine-1,1-dioxides) and a 4-OLi-naphthyllithium compound or a 4-OLi-phenyllithium compound substituted in the 3-position with a lithiated perhalomethylcarbinol group.Type: GrantFiled: November 2, 1978Date of Patent: August 11, 1981Assignee: Polaroid CorporationInventors: Louis Cincotta, James W. Foley
-
Patent number: 4277477Abstract: Novel 1,2-benzisothiazoles and a process for the manufacture of 1,2-benzisothiazoles by reacting o-haloaryl ketones with ammonia and elementary sulfur. The compounds are starting materials for the manufacture of dyes, crop protection agents and drugs.Type: GrantFiled: October 2, 1979Date of Patent: July 7, 1981Assignee: BASF AktiengesellschaftInventors: Helmut Hagen, Rolf-Dieter Kohler, Juergen Markert
-
Patent number: 4268300Abstract: New and valuable polycyclic compounds which contain nitrogen-containing rings and have a strong action on plants, agents for influencing plant growth containing these compounds, and a method of influencing plant growth with these compounds.Type: GrantFiled: January 16, 1980Date of Patent: May 19, 1981Assignee: BASF AktiengesellschaftInventors: Rolf Platz, Werner Fuchs, Norbert Rieber, Ulf-Rainer Samel, Johann Jung, Bruno Wuerzer
-
Patent number: 4259498Abstract: This invention relates to certain 3,3,-di(4'-OP-carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxides (and-2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxides) and to the preparation thereof by reacting (a) at least 2 equivalents of (i) a 4'-OP-carbocyclic aryllithium compound wherein P is a protecting group compatible with organometallic reagents or (ii) a 4'-OP-carbocyclic arylMgE compound wherein P is a protecting group compatible with organometallic reagents and E is chloro, bromo or iodo and (b) 1 equivalent of a compound selected from a 3-chlorobenz[d]isothiazole-1,1-dioxide and a 3-chloronaphtho[1,8-de]-1,2-thiazine-1,1-dioxide to give the corresponding 3,3-di(4'-OP-carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxide or the corresponding 3,3-di(4'-OP-carbocyclic aryl)-2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxide, which compounds are useful in the synthesis of phenol and 1-naphthol sulfam(na)-phthaleins employed, for example, as photographic optical filter agents and filter agentType: GrantFiled: October 12, 1979Date of Patent: March 31, 1981Assignee: Polaroid CorporationInventors: Stanley M. Bloom, Alan L. Borror, James W. Foley
-
Patent number: 4259493Abstract: The present invention is concerned with novel 3,3-disubstituted-sulfam(na)phthaleins wherein one of the 3-substituents is derived from a 1-naphthol or a phenol substituted in the 2-position with a perhalomethylcarbinol group and wherein the N atom of the sulfam(na)phthalein ring is substituted with ##STR1## wherein R is alkyl or aryl or with ##STR2## wherein Y is hydrogen or an electron-withdrawing group, which compounds find utility, e.g., as pH-sensitive indicator dyes or as photographic light-screening dyes.Type: GrantFiled: November 2, 1978Date of Patent: March 31, 1981Assignee: Polaroid CorporationInventor: James W. Foley
-
Patent number: 4255578Abstract: The present invention is concerned with a method of synthesizing certain ##STR1## 3-disubstituted sulfam(na)phthalein compounds useful as pH-sensitive indicator dyes and with intermediates useful in the preparation of said compounds. The subject method comprises (1) reacting (a) a 3,3-disubstituted sulfam(na)phthalein wherein one of the 3-substituents is a 4'-hydroxy-1'-phenyl moiety or a 4'-hydroxy-1'-naphthyl moiety substituted in the 3'-position with a perhalomethylcarbinol group and (b) an acid halide, ##STR2## wherein R is alkyl or aryl to give (c) an acylated intermediate wherein the N atom of the sulfam(na)phthalein ring and the 4'-hydroxy and carbinol hydroxy groups are acylated with ##STR3## and (2) treating said compound (c) with alkali to selectively remove said ##STR4## from said hydroxy groups and yield the ##STR5## product. The intermediates of the present invention are the acylated compounds (c).Type: GrantFiled: November 2, 1978Date of Patent: March 10, 1981Assignee: Polaroid CorporationInventors: Louis Cincotta, James W. Foley
-
Patent number: 4253865Abstract: Compounds of the formula: ##STR1## wherein R is haloalkyl, haloalkenyl or halogenated aryl; R.sup.1 and R.sup.2 are hydrogen, alkyl or are joined to form a cyclopentyl or cyclohexyl ring; X is hydrogen, halo, alkyl, haloalkyl, alkoxy, nitro or cyano; and n=1 to 5 have fungicidal and bactericidal activity.Type: GrantFiled: September 6, 1979Date of Patent: March 3, 1981Assignee: Chevron Research CompanyInventor: David C. K. Chan
-
Patent number: 4252957Abstract: Heterocyclylcarbonyl derivatives of urea having the formula ##STR1## wherein R is a heterocyclyl group; and R.sub.1 and R.sub.2 when taken together with the nitrogen to which they are attached are morpholino, thiomorpholino or a 6-8 membered nitrogen containing heterocyclic ring; methods for their preparation and use as agents for dissolving gallstones.Type: GrantFiled: September 14, 1979Date of Patent: February 24, 1981Assignee: Pfizer Inc.Inventor: Gerald F. Holland