The Sulfur Is Bonded Directly To The Aryl Ring Or Ring System Patents (Class 564/341)
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Patent number: 5756068Abstract: Compounds useful in radioimaging and radiochemotherapy as it particularly relates to the treatment and location of malignant melanomas and other pigmenting disorders, as well as novel acyl derivatives of phenolic thioester amines and their use in compositions for blocking melanin synthesis in human or animal melanocyte cells.Type: GrantFiled: August 27, 1996Date of Patent: May 26, 1998Assignee: The Governors of the University of AlbertaInventor: Kowichi Jimbow
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Patent number: 5674909Abstract: Compounds of formula ##STR1## wherein R, R', R", R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, X, Y, m, n and p have the meanings reported in the description;and their pharmaceutically acceptable salts are described.The compounds of formula I are useful in the treatment of arterial hypertension and congestive heart failure, of renal failure, of peripheral arteriopathies, of cerebrovascular insufficiencies and of ischemic cardiopathy.Type: GrantFiled: June 6, 1995Date of Patent: October 7, 1997Assignee: Zambon GroupInventors: Stefania Montanari, Paolo Cavalleri, Cristina Fraire, Gian Carlo Grancini, Mauro Napoletano, Francesco Santangelo
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Patent number: 5650541Abstract: Compounds structurally related to ethacrynic acid are described. The compounds are useful for controlling intraocular pressure. Unlike ethacrynic acid, the compounds of the present invention are capable of effectively penetrating the cornea. Methods of controlling intraocular pressure via topical application of one or more of the compounds to the eye and topical ophthalmic compositions useful in the treatment of glaucoma are also described.Type: GrantFiled: January 11, 1996Date of Patent: July 22, 1997Assignee: Alcon Laboratories, Inc.Inventor: Jesse A. May
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Patent number: 5616803Abstract: A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of the substituents are herein defined.Type: GrantFiled: October 6, 1995Date of Patent: April 1, 1997Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Nomoto, Masahiro Hayashi, Jun Shibata, Yoshikazu Iwasawa, Morihiro Mitsuya, Yoshiaki Iida, Katsumasa Nonoshita, Yasufumi Nagata
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Patent number: 5482964Abstract: Substituted phenoxyhydroxy amines and derivatives thereof are described as well as methods for the preparation and pharmaceutical compositions of same, which are central nervous system agents useful in the treatment of neurological disorders including traumatic brain surgery, stroke, migraine, acute and chronic pain, epilepsy, Parkinson's disease, Alzheimer's disease, amyotropic lateral sclerosis, multiple sclerosis, psychosis, and depression.Type: GrantFiled: October 11, 1994Date of Patent: January 9, 1996Assignee: Warner-Lambert CompanyInventor: Sheryl J. Hays
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Patent number: 5182401Abstract: A process for the preparation of a 3-amino-2-(het)aroyl-acrylic acid derivative fo the formula ##STR1## in which Y represents a nitrile, or an ester group, --COOR.sub.1, or an acetyl group, whereR.sup.1 denotes C.sub.1 -C.sub.4 -alkyl, andR denotes optionally substituted alkyl, cyclopropyl, alkoxy, phenyl or amino,A represents nitrogen or C--R.sub.2, whereR.sub.2 denotes hydrogen, methyl, halogen, nitro, methoxy or cyano,X.sub.1 and X.sub.2 are identical or different and denote halogen, andX.sub.3 denotes hydrogen, halogen or nitro andX.sub.4 denotes halogen, nitro, methoxy or methylthio, which comprises reacting a 3-dialkylamino-2-(het)aroyl-acrylic acid derivative of the formula ##STR2## in which R.sub.3 and R.sub.4 are the same or different and represent an alkyl group having 1 to 4 carbon atoms, or, together with the nitrogen atom to which they are bonded, form a ring,with a primary amine of the formula R--NH.sub.2 in the presence of at least one equivalent of an acid HX in a solvent or in excess acid.Type: GrantFiled: May 2, 1991Date of Patent: January 26, 1993Assignee: Bayer AktiengesellschaftInventor: Klaus Grohe
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Patent number: 5124334Abstract: The invention relates to benylalcohol phospholipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylalcohol phospholipase A.sub.2 inhibitor.Type: GrantFiled: July 28, 1989Date of Patent: June 23, 1992Assignee: Du Pont Merck Pharmaceutical CompanyInventor: Wendell W. Wilkerson
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Patent number: 5117061Abstract: Novel anilines of the 2,6-dialkyl-4-dialkylaminomethylaniline type are prepared by reacting a secondary amine and an aldehyde with a primary aniline reactant having a free para position and substituents in both ortho positions in the presence of an acid catalyst, the amounts of amine and acid employed being at least equimolar with respect to the amount of aldehyde, and the reaction being conducted by adding the primary aniline reactant to a preformed mixture of the secondary amine, aldehyde, and acid.Type: GrantFiled: May 12, 1986Date of Patent: May 26, 1992Assignee: Ethyl CorporationInventor: Kju H. Shin
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Patent number: 5023378Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable acid addition salts, metabolically labile esters and solvates thereof in whichR.sup.1 represents a halogen atom or a methyl, ethyl, n-propyl or n-butyl group;R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each represent hydrogen atoms or one or two of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent a methy or ethyl group;X represents a C.sub.4-7 alkylene chain optionally substituted by one or more C.sub.1-4 alkyl or hydroxyl groups; or optionally containing one or two double or triple bonds; or optionally interrupted by an oxygen or sulphur atom, or by a sulphone (--SO.sub.2 --) or urea (--NHCONH--) group; andY represents a phenyl ring optionally carrying one to three substituents selected from hydroxyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, amino, carboxamido, C.sub.1-4 alkylsulphonylamino and nitro groups and halogen atoms with the proviso that when X is a C.sub.Type: GrantFiled: October 6, 1989Date of Patent: June 11, 1991Assignee: Glaxo Group LimitedInventors: Michael D. Dowle, David Middlemiss, Harry Finch, Alan Naylor, Lawrence H. C. Lunts
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Patent number: 5021429Abstract: Compounds of the general formula: ##STR1## and physiologically acceptable salts, and hydrates, N-oxides and bioprecursors of such compounds and such salts in whichR.sub.1 and R.sub.2, which may be the same or different, represent hydrogen or lower alkyl, cycloalkyl, aralkyl or lower alkenyl groups, or lower alkyl groups interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl; or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached form a heterocyclic ring which may contain the hetero functions --O-- and ##STR3## R.sub.3 represents hydrogen, lower alkyl, alkenyl or alkoxyalkyl; X represents --O--, --S-- or --CH.sub.2 -- or ##STR4## where R.sub.5 is hydrogen or lower alkyl; Y represents .dbd.S, .dbd.O, .dbd.NR.sub.6 or .dbd.CHR.sub.7 ;in which R.sub.6 represents hydrogen, nitro, cyano, lower alkyl, aryl, arylsulphonyl or lower alkylsulphonyl; R.sub.Type: GrantFiled: December 22, 1986Date of Patent: June 4, 1991Assignee: Allen & Hansburys LimitedInventor: Michael Martin-Smith
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Patent number: 5008430Abstract: The invention relates to mercaptopyrenes of the formula ##STR1## in which n denotes a whole number from 3 to 10 andR stands for a substitute or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl or aryl radicalto a process for its preparation, its use for the preparation of CT complexes and to the CT complexes obtained.Type: GrantFiled: April 10, 1989Date of Patent: April 16, 1991Assignee: Bayer AktiengesellschaftInventors: Gerhard Heywang, Friedrich Jonas
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Patent number: 4959366Abstract: A series of [N-alkyl-N-(nitro-, alkylsulphonamido, or amino-phenalkyl)amino]-alkyl, alkoxy or alkylthio phenyl derivatives having utility as anti-arrhythmic agents.Type: GrantFiled: April 29, 1987Date of Patent: September 25, 1990Assignee: Pfizer Inc.Inventors: Peter E. Cross, Geoffrey N. Thomas, John E. Arrowsmith
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Patent number: 4945181Abstract: The present invention provides a process for the preparation of thamphenicol (I) from D,L-threo-1-(p-methylsulphonylphenyl)-2-aminopropane-1, 3-diol hydrochloride (V) and intermediates thereof. The process comprises conversion to a corresponding benzal compound followed by hydrolysis to D,L-threo-aminodiol.Type: GrantFiled: December 1, 1986Date of Patent: July 31, 1990Assignee: Boehringer Mannheim GmbHInventors: Helmut Dick, Wolf-Dietrich Gradel, Mathias Weber
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Patent number: 4927970Abstract: The present invention relates to novel intermediates of the formula ##STR1## wherein R is lower alkyl or cyclohexyl, and X is hydroxy or a conventional leaving group, and the use thereof in a process for the preparation of certain histamine H.sub.2 -antagonists.Type: GrantFiled: April 11, 1988Date of Patent: May 22, 1990Assignee: Bristol-Myers CompanyInventors: James L. Douglas, Guy Fabre, Claude Demosthene
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Patent number: 4921980Abstract: A process for the preparation of N-alkylanilines is described, the most essential feature of which comprises reacting corresponding anilines at 150.degree. to 300.degree.C. with corresponding alcohols in the presence of a catalyst consisting of silica gel as carrier, of 0.2 to 10% of platinum and of 0.05 to 3% of a compound of a metal of the groups Ia and/or IIa of the Periodic Table, with the catalyst additionally containing at least one compound of an element of the groups Ib, IVa, IVb, Vb, VIIb and VIII in such an amount that the atomic ratio of platinum to the sum of these elements is 1 to 6.Type: GrantFiled: May 22, 1987Date of Patent: May 1, 1990Assignee: Ciba-Geigy CorporationInventor: Milos Rusek
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Patent number: 4902710Abstract: The present invention provides propanamines, substituted at the 3-position of the propanamine chain with a thio, sulfinyl or sulfonyl moiety, which are capable of selectively inhibiting the uptake of serotonin and norepinephrine.Type: GrantFiled: December 14, 1988Date of Patent: February 20, 1990Assignee: Eli Lilly and CompanyInventors: Bennie J. Foster, David C. Hunden, Edward R. Lavagnino
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Patent number: 4902799Abstract: Novel bicyclic alkoxy- and alkylthio-substituted aminoalcohols of formula (I). The compounds show anti-hypertensive, platelet aggregation inhibiting, hypolipemic, antianoxic, spasmolytic, antithrombotic, calcium antagonizing and neuroleptic activity.Type: GrantFiled: June 4, 1987Date of Patent: February 20, 1990Assignee: Maggioni-Winthrop S.p.A.Inventors: Giampaolo Picciola, Mario Riva, Franco Ravenna, Piergiorgio Gentili
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Patent number: 4898944Abstract: Precursors for the preparation of fiber-reactive triphendioxazine dyestuffs correspond to the general formulas: ##STR1## in which Y' is a vinyl, a beta-hydroxyethyl or an ethyl group which contains in the beta-position a substituent which can be eliminated by an alkali;T is an optionally substituted alkyl (e.g.Type: GrantFiled: October 27, 1988Date of Patent: February 6, 1990Assignee: Hoechst AktiengesellschaftInventors: Gunther Schwaiger, Hartmut Springer, Walter Helmling
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Patent number: 4883804Abstract: There are described compounds of formula I, ##STR1## in which X represents a C2 to 8 alkylene chain optionally interrupted by a double bond or by S(O).sub.n, wherein n is 0, 1 or 2;Y represents O or NH,l and m each independently represent 2, 3 or 4,R.sub.10 represents phenyl substituted by one or more substituents R.sub.23, which may be the same or different; or R.sub.10 represents pyridyl, a saturated carbocyclic group, alkyl C 1 to 6 or hydrogen,R.sub.15 represents hydrogen or together with R.sub.23 forms a (CH.sub.2).sub.p chain, wherein p represents 0, 1 or 2;R.sub.20, R.sub.21, R.sub.22 and R.sub.23, which may be the same or different, independently represent hydrogen, alkyl C 1 to 6, NHR.sub.25, SH, NO.sub.2, halogen, CF.sub.3, SO.sub.2 R.sub.30, CH.sub.2 OH or OH, wherein R.sub.25 represents hydrogen, alkyl C 1 to 6, alkanoyl C 1 to 6 or SO.sub.2 alkyl C 1 to 6, and R.sub.30 represents alkyl C 1 to 6 or NH.sub.Type: GrantFiled: November 19, 1986Date of Patent: November 28, 1989Assignee: Fisons plcInventors: Francis Ince, Brian Springthorpe, John Dixon
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Patent number: 4857663Abstract: N-(3-Dialkylamino-2-propenylidene)-N-alkylalkanaminium salts substituted in the 2-position with an ether or thioether and having the formula ##STR1## are active as hypoglycemic agents.Type: GrantFiled: November 16, 1988Date of Patent: August 15, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Eugene R. Wagner, Donald P. Matthews, Charlotte L. Barney
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Patent number: 4829089Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.Type: GrantFiled: July 22, 1988Date of Patent: May 9, 1989Assignee: American Cyanamid CompanyInventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
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Patent number: 4808625Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a phenanthrene or substituted phenanthrene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five-or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: August 28, 1987Date of Patent: February 28, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4803225Abstract: There are provided compounds of formula I, ##STR1## and pharmaceutically acceptable derivatives thereof. There are also described the use of the compounds of formula I as pharmaceuticals, methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.Type: GrantFiled: December 2, 1987Date of Patent: February 7, 1989Assignee: Fisons, plcInventors: John Dixon, Francis Ince
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Patent number: 4803221Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is an anthracene or substituted anthracene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: August 28, 1987Date of Patent: February 7, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4803222Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fluoranthene or substituted fluoranthene ring system; R.sup.1 contains not more than eight carbon carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl;--C--C-- is a five- or six-membered saturated carbocyclic ring;R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: August 28, 1987Date of Patent: February 7, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4799934Abstract: Novel sulfur containing nitroamino benzene dyes of formula: ##STR1## and salts thereof wherein (a) R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of alkyl, hydroxyalkyl, polyhydroxyalky, aminoalkyl, monoalkylamioalkyl and dialkylaminoalkyl,wherein(b) n is 0, 1 or 2, and wherein(c) the group ##STR2## occupies a position that is meta or para to the group-NHR.sub.1 ; a process for synthesizing these compounds and their use as direct dyeing hair dyes are being disclosed.Type: GrantFiled: October 30, 1987Date of Patent: January 24, 1989Assignee: Clairol IncorporatedInventors: Mu-Ill Lim, James S. Anderson
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Patent number: 4772405Abstract: The invention relates to compositions comprising a lubricant or a hydraulic fluid and at least one compound of formula I ##STR1## wherein X is --S--, --O--, --CO--O--, --CH.sub.2 -- or --NR.sup.5 --, where R.sup.5 is hydrogen or C.sub.1 --C.sub.8 alkyl, n is 0, 1, 2 or 3, R.sup.1 and R.sup.2 are each independently of the other hydrogen or C.sub.1 -C.sub.12 alkyl, R.sup.3 is hydrogen or methyl, and R.sup.4 is C.sub.1 -C.sub.22 alkyl, C.sub.5 -C.sub.8 cycloalkyl, aryl or aryl which is substituted by one or two C.sub.1 -C.sub.8 alkyl radicals, or is C.sub.7 -C.sub.12 aralkyl or the group ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and n have the given meanings. The sulfur-containing phenol derivatives of formula I are particularly suitable antiwear, extreme pressure and antioxidant additives for mineral and synthetic lubricants and for hydraulic fluids.The invention further relates to novel phenol derivatives of formula I which are suitable additives for lubricants, hydraulics and elastomers.Type: GrantFiled: August 14, 1986Date of Patent: September 20, 1988Assignee: Ciba-Geigy CorporationInventor: Hermann O. Wirth
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Patent number: 4760377Abstract: Disclosed is a decompaction system for reading compacted paralled data from a memory and providing in real time uncompacted serial data therefrom. The decompaction system is especially suited to be utilized in pin electronics automatic test equipment for real time testing of units such as integrated circuits, circuit boards, etc. The decompaction system includes a separate channel for each pin of the unit under test (UUT) and is capable of decoding a number of types of compacted parallel data and providing serail data to each pin of the UUT in the most prevalently used test patterns. The data is compacted by software algorithms according to these patterns, stored in a memory and retrieved and decoded by the decompaction system during real-time testing of the UUT. In a specific embodiment, compacted parallel data is stored in 16-bit words in a separate memory for each channel, and is decompacted into serial data sequences of from 8 to 4096 bits per channel for each access of the respective memory.Type: GrantFiled: March 29, 1985Date of Patent: July 26, 1988Assignee: Giordano Associates, Inc.Inventor: Philip C. Jackson
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Patent number: 4720587Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fluoranthene or substituted fluoranthene ring system; R.sup.1 contains not more than eight carbon carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: October 17, 1984Date of Patent: January 19, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4720586Abstract: There are provided compounds of formula I, ##STR1## in which R.sub.1 represents OH,R.sub.2 and R.sub.3, which may be the same or different, each independently represent hydrogen, fluorine, chlorine, bromine, alkyl C1 to 6, nitro, nitrile, (CH.sub.2).sub.p R.sub.9 or SR.sub.9,W represents a single bond, a 1,2; 1,3; or 1,4-disubstituted benzene ring; a --CH.dbd.CH--group or a 1,4-cyclohexanediyl group;X respresents NH, O, S, SO.sub.2, CO, CH.sub.2, CONH or --COO;Y represents (CH.sub.2)q, CO, CS, SO.sub.2 and R.sub.20 represents hydrogen,or Y represents CR.sub.15 R.sub.16 CR.sub.17 R.sub.18,wherein the carbon atom bearing R.sub.15 and R.sub.16 is adjacent to X and in whichR.sub.15 and R.sub.18, together with the carbon atom to which they are attached form a carbonyl group, and R.sub.15, R.sub.16 and R.sub.20 each represent hydrogen, orR.sub.15 and R.sub.20 together form a chain --CH.sub.2 --, and R.sub.16, R.sub.17 and R.sub.18 each represent hydrogen, orR.sub.15, R.sub.16, R.sub.17 and R.sub.Type: GrantFiled: October 18, 1984Date of Patent: January 19, 1988Assignee: Fisons, plcInventors: John Dixon, Francis Ince
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Patent number: 4719049Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is an anthracene or substituted anthracene ring system; R.sup.1 contains not more than eight carbon carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl;--C--C-- is a five- or six-membered saturated carbocyclic ring;R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: October 17, 1984Date of Patent: January 12, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4719046Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a chrysene or substituted chrysene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl, ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: October 18, 1984Date of Patent: January 12, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4719055Abstract: The present invention relates to compounds of formula (1)ArCH.sub.2 R.sup.1 (1)or a monomethyl ether thereof (the compound of formula (1) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a phenanthrene or substituted phenanthrene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: October 10, 1984Date of Patent: January 12, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4699928Abstract: Fluoroallylamine derivatives of the following Formula I are novel MAO-inhibitors and at low dose levels selectively inhibit MAO-B: ##STR1## wherein: R.sub.1 and R.sub.2 independently represent hydrogen, chlorine or fluroine;R.sub.3 represents hydrogen or (C.sub.1 -C.sub.4)alkyl; andX represents oxygen or sulfur.They are useful for the treatment of depression and, co-administered with L-dopa, in the treatment of Parkinsonism.Type: GrantFiled: November 6, 1986Date of Patent: October 13, 1987Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Ian A. McDonald
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Patent number: 4686309Abstract: The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl, either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl, or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and (i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.Type: GrantFiled: February 15, 1985Date of Patent: August 11, 1987Assignee: Rhone-Poulenc SanteInventors: Jean-Claude Barriere, Jean-Pierre Corbet, Claude Cotrel, Daniel Farge, Jean-Marc Paris
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Patent number: 4670470Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.Type: GrantFiled: August 29, 1985Date of Patent: June 2, 1987Assignee: Merck & Co., Inc.Inventor: Raymond A. Firestone
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Patent number: 4588719Abstract: A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: October 24, 1984Date of Patent: May 13, 1986Assignee: William H. Rorer, Inc.Inventors: William L. Studt, Donald E. Kuhla, Henry F. Campbell
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Patent number: 4558071Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.Type: GrantFiled: February 25, 1983Date of Patent: December 10, 1985Assignee: Merck & Co., Inc.Inventor: Raymond A. Firestone
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Patent number: 4537621Abstract: Diphenyl ethers of the formula ##STR1## where Z.sup.1, Z.sup.2, and Z.sup.3 and R have the meanings given in the description, are used for controlling undesirable plant growth.Type: GrantFiled: March 31, 1983Date of Patent: August 27, 1985Assignee: BASF AktiengesellschaftInventors: Adolf Parg, Hans Ziegler, Bruno Wuerzer
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Patent number: 4534908Abstract: Water-soluble disazo compounds of the formula (1) ##STR1## and diamino compounds serving as starting compounds (tetrazo components), of the formula (4) ##STR2## in which the formulae moieties occurring twice, namely Z, K and X, in each case have a meaning identical to one another and the groups Z are bonded to the two benzene nuclei in each case in the ortho- or in each case in the para-position relative to the ethylenedioxy substituent, and the azo groups or amino groups and the groups Z in the benzene nuclei are in each case bonded in the meta-position relative to one another and K is the radical of a coupling component containing a sulfato, carboxy or sulfo group, X denotes a hydrogen atom or a fiber-reactive group and Z is a group of the formula --SO.sub.2 --CH.dbd.CH.sub.2 or --SO.sub.2 --CH.sub.2 --CH.sub.2 --Y in which Y denotes a radical which can be eliminated in aqueous medium under alkaline or acidic conditions or the hydroxy group.Type: GrantFiled: September 26, 1983Date of Patent: August 13, 1985Assignee: Hoechst AktiengesellschaftInventors: Hermann Fuchs, Klaus Filzinger
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Patent number: 4529556Abstract: The invention bis((aryl)vinyl)benzenes wherein the aryl and benzene moieties may be substituted, and the vinyl carbon alpha to the central benzene ring may be further substituted with an aliphatic group.Type: GrantFiled: August 19, 1983Date of Patent: July 16, 1985Assignee: The Dow Chemical CompanyInventor: Kenneth J. Bruza
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Patent number: 4526973Abstract: Certain 1-(substituted amino)-2-(amino or substituted amino)cyclobutene-3,4-diones of the general formula ##STR1## are potent histamine H.sub.2 -antagonists useful in the treatment of peptic ulcers. A preferred compound, 1-amino-2-[3-(3-piperidinomethylphenoxy)propylamino]cyclobutene-3,4-dione, is prepared by treating an intermediate, 1-methoxy-2-[3-(3-piperidinomethylphenoxy)propylamino]cyclobutene-3,4-dion e, with ammonia.Type: GrantFiled: June 9, 1982Date of Patent: July 2, 1985Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4526893Abstract: Compounds of the structure ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are as herein defined, effective as .beta.-blockers and hypotensive agents, are described.Type: GrantFiled: December 16, 1983Date of Patent: July 2, 1985Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Toshihiro Takahashi, Noriyoshi Sueda, Masahiro Tsuji, Yoshiyuki Tahara, Hiroyasu Koyama, Yoshikuni Suzuki, Masao Nagase, Toshiji Sugai
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Patent number: 4522943Abstract: Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.Type: GrantFiled: April 21, 1982Date of Patent: June 11, 1985Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4507500Abstract: A process for producing 2-mercaptoethylamine hydrohalides of the general formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are identical or different, and each represents a hydrogen atom, a lower alkyl group, a hydroxy-substituted lower alkyl group or a phenyl group, and X represents a halogen atom,which comprises reacting a 2-mercaptothiazoline of the general formula ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined above, with a 2-halogenoethylamine hydrohalide of the general formula ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and X are as defined above, in the presence of water.Type: GrantFiled: July 7, 1981Date of Patent: March 26, 1985Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Shigenobu Nakayama, Eiichi Noda, Yoshiaki Noguchi, Isamu Yamamoto, Noboru Kawasaki
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Patent number: 4415591Abstract: Hypertension in mammals can be treated by administering an effective amount of an aminoalkyl phenyl sulfide having the formula ##STR1## wherein (C.sub.n H.sub.2n)=a linear or branched alkyl chain of 10 carbons or less (n=1-10);R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5,=H, OH, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, F, Cl, Br, or I;R.sub.6 R.sub.7 =H, C.sub.1 -C.sub.4 -alkyl;and the pharmaceutically acceptable salts thereof. The hypotensive potential of the compounds may be evaluated by oxygenation with dopamine-beta-hydroxylase.Type: GrantFiled: June 4, 1981Date of Patent: November 15, 1983Assignee: Georgia Tech Research InstituteInventors: Sheldon W. May, Robert S. Phillips, Heath H. Herman, Patricia W. Mueller
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Patent number: 4388475Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.Type: GrantFiled: May 7, 1980Date of Patent: June 14, 1983Assignee: Merck & Co., Inc.Inventor: Raymond A. Firestone
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Patent number: 4364956Abstract: Compounds are described of the formula ##STR1## in which R.sup.1 is COOR.sup.5, CONHR.sup.5, cyano, 5-tetrazolyl or 5-tetrazolylaminocarbonyl, where R.sup.5 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is a group of the formulaR.sup.6 --(Z).sub.m --where m is O or 1, Z is O, S, SO, SO.sub.2 or CO, and R.sup.6 phenyl optionally substituted by one or more group selected from halogen, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, C.sub.1-4 alkoxy, benzyloxy, hydroxy, nitro, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, amino and NHR.sup.7 where R.sup.7 is C.sub.2-6 acyl; and R.sup.4 is hydrogen, C.sub.1-6 alkyl or halogen; and salts thereof. These compounds have pharmaceutical properties and in particular are useful in the treatment of immediate hypersensitivity conditions such as asthma.Type: GrantFiled: September 17, 1981Date of Patent: December 21, 1982Assignee: Lilly Industries LimitedInventors: Barry P. Clark, William J. Ross, Alec Todd
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Patent number: 4339393Abstract: The distyrylbiphenyls of the formula ##STR1## in which X and X' independently of one another are a direct bond, oxygen, sulfur, --O--C.sub.1--3 --alkylene--CON(R.sub.4)--, --CON(R.sub.4)--,--O--C.sub.1--3 --alkylene--COO--, OCO or --COO--, with the proviso that if n+n'=O, X and X' may not be --CON(R.sub.4)--or O--C.sub.1--3 --alkylene--CON(R.sub.4)--, and if n+n'=2 and X and X' are --CON(R.sub.4)--or --COO--, A.crclbar. may not be a phosphite or phosphonate anion, and Y and Y' independently of one another are C.sub.1--20 --alkylene, R.sub.1 and R.sub.1' independently of one another are unsubstituted or substituted C.sub.1--8 --alkyl or C.sub.3--4 --alkenyl, or R.sub.1 together with R.sub.2, or R.sub.1' together with R.sub.2', is a heterocyclic ring, R.sub.2 and R.sub.2' independently of one another are unsubstituted or substituted C.sub.1--8 --alkyl or C.sub.3--4 -- alkenyl, or R.sub.2 together with R.sub.1, or R.sub.2' together with R.sub.1', is a heterocyclic ring, or R.sub.1 and R.sub.2, or R.sub.1' and R.Type: GrantFiled: April 4, 1980Date of Patent: July 13, 1982Assignee: Ciba-Geigy CorporationInventors: Christian Luthi, Hans R. Meyer, Kurt Weber
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Patent number: 4327214Abstract: Substituted alkylammonium salts of the formula ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are hydrogen, C.sub.1-4 -alkyl, fluorine, chlorine or bromine, X is oxygen or sulfur, n denotes one of the integers 2, 3 and 4, A denotes quinuclidine or pyrrolizidine, or --NR.sup.4 R.sup.5 R.sup.6, R.sup.4, R.sup.5 and R.sup.6 denoting C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.2-6 -alkynyl which are unsubstituted or substituted by halogen, cyano or C.sub.1-4 -alkoxy, or R.sup.5 and R.sup.6, as alkylene groups, may be part of an unsubstituted or C.sub.1-2 -alkyl-substituted 5- or 6-membered heterocycle with 1 to 3 heteroatoms in the ring, and Z is the anion of any non-phytotoxic acid HZ, the manufacture of such compounds, agents for regulating plant growth containing these compounds, and the use thereof for regulating plant growth.Type: GrantFiled: September 12, 1980Date of Patent: April 27, 1982Assignee: BASF AktiengesellschaftInventors: Costin Rentzea, Hubert Sauter, Johann Jung