The Sulfur Is Bonded Directly To The Aryl Ring Or Ring System Patents (Class 564/341)
  • Patent number: 5756068
    Abstract: 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: Grant
    Filed: August 27, 1996
    Date of Patent: May 26, 1998
    Assignee: The Governors of the University of Alberta
    Inventor: Kowichi Jimbow
  • Patent number: 5674909
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: October 7, 1997
    Assignee: Zambon Group
    Inventors: Stefania Montanari, Paolo Cavalleri, Cristina Fraire, Gian Carlo Grancini, Mauro Napoletano, Francesco Santangelo
  • Patent number: 5650541
    Abstract: 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: Grant
    Filed: January 11, 1996
    Date of Patent: July 22, 1997
    Assignee: Alcon Laboratories, Inc.
    Inventor: Jesse A. May
  • Patent number: 5616803
    Abstract: A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of the substituents are herein defined.
    Type: Grant
    Filed: October 6, 1995
    Date of Patent: April 1, 1997
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Takashi Nomoto, Masahiro Hayashi, Jun Shibata, Yoshikazu Iwasawa, Morihiro Mitsuya, Yoshiaki Iida, Katsumasa Nonoshita, Yasufumi Nagata
  • Patent number: 5482964
    Abstract: 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: Grant
    Filed: October 11, 1994
    Date of Patent: January 9, 1996
    Assignee: Warner-Lambert Company
    Inventor: Sheryl J. Hays
  • Patent number: 5182401
    Abstract: 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: Grant
    Filed: May 2, 1991
    Date of Patent: January 26, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventor: Klaus Grohe
  • Patent number: 5124334
    Abstract: 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: Grant
    Filed: July 28, 1989
    Date of Patent: June 23, 1992
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventor: Wendell W. Wilkerson
  • Patent number: 5117061
    Abstract: 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: Grant
    Filed: May 12, 1986
    Date of Patent: May 26, 1992
    Assignee: Ethyl Corporation
    Inventor: Kju H. Shin
  • Patent number: 5023378
    Abstract: 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: Grant
    Filed: October 6, 1989
    Date of Patent: June 11, 1991
    Assignee: Glaxo Group Limited
    Inventors: Michael D. Dowle, David Middlemiss, Harry Finch, Alan Naylor, Lawrence H. C. Lunts
  • Patent number: 5021429
    Abstract: 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: Grant
    Filed: December 22, 1986
    Date of Patent: June 4, 1991
    Assignee: Allen & Hansburys Limited
    Inventor: Michael Martin-Smith
  • Patent number: 5008430
    Abstract: 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: Grant
    Filed: April 10, 1989
    Date of Patent: April 16, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerhard Heywang, Friedrich Jonas
  • Patent number: 4959366
    Abstract: 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: Grant
    Filed: April 29, 1987
    Date of Patent: September 25, 1990
    Assignee: Pfizer Inc.
    Inventors: Peter E. Cross, Geoffrey N. Thomas, John E. Arrowsmith
  • Patent number: 4945181
    Abstract: 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: Grant
    Filed: December 1, 1986
    Date of Patent: July 31, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Helmut Dick, Wolf-Dietrich Gradel, Mathias Weber
  • Patent number: 4927970
    Abstract: 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: Grant
    Filed: April 11, 1988
    Date of Patent: May 22, 1990
    Assignee: Bristol-Myers Company
    Inventors: James L. Douglas, Guy Fabre, Claude Demosthene
  • Patent number: 4921980
    Abstract: 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: Grant
    Filed: May 22, 1987
    Date of Patent: May 1, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Milos Rusek
  • Patent number: 4902710
    Abstract: 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: Grant
    Filed: December 14, 1988
    Date of Patent: February 20, 1990
    Assignee: Eli Lilly and Company
    Inventors: Bennie J. Foster, David C. Hunden, Edward R. Lavagnino
  • Patent number: 4902799
    Abstract: 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: Grant
    Filed: June 4, 1987
    Date of Patent: February 20, 1990
    Assignee: Maggioni-Winthrop S.p.A.
    Inventors: Giampaolo Picciola, Mario Riva, Franco Ravenna, Piergiorgio Gentili
  • Patent number: 4898944
    Abstract: 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: Grant
    Filed: October 27, 1988
    Date of Patent: February 6, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gunther Schwaiger, Hartmut Springer, Walter Helmling
  • Patent number: 4883804
    Abstract: 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: Grant
    Filed: November 19, 1986
    Date of Patent: November 28, 1989
    Assignee: Fisons plc
    Inventors: Francis Ince, Brian Springthorpe, John Dixon
  • Patent number: 4857663
    Abstract: 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: Grant
    Filed: November 16, 1988
    Date of Patent: August 15, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Eugene R. Wagner, Donald P. Matthews, Charlotte L. Barney
  • Patent number: 4829089
    Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.
    Type: Grant
    Filed: July 22, 1988
    Date of Patent: May 9, 1989
    Assignee: American Cyanamid Company
    Inventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
  • Patent number: 4808625
    Abstract: 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: Grant
    Filed: August 28, 1987
    Date of Patent: February 28, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4803221
    Abstract: 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: Grant
    Filed: August 28, 1987
    Date of Patent: February 7, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4803225
    Abstract: 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: Grant
    Filed: December 2, 1987
    Date of Patent: February 7, 1989
    Assignee: Fisons, plc
    Inventors: John Dixon, Francis Ince
  • Patent number: 4803222
    Abstract: 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: Grant
    Filed: August 28, 1987
    Date of Patent: February 7, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4799934
    Abstract: 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: Grant
    Filed: October 30, 1987
    Date of Patent: January 24, 1989
    Assignee: Clairol Incorporated
    Inventors: Mu-Ill Lim, James S. Anderson
  • Patent number: 4772405
    Abstract: 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: Grant
    Filed: August 14, 1986
    Date of Patent: September 20, 1988
    Assignee: Ciba-Geigy Corporation
    Inventor: Hermann O. Wirth
  • Patent number: 4760377
    Abstract: 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: Grant
    Filed: March 29, 1985
    Date of Patent: July 26, 1988
    Assignee: Giordano Associates, Inc.
    Inventor: Philip C. Jackson
  • Patent number: 4720587
    Abstract: 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: Grant
    Filed: October 17, 1984
    Date of Patent: January 19, 1988
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4720586
    Abstract: 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: Grant
    Filed: October 18, 1984
    Date of Patent: January 19, 1988
    Assignee: Fisons, plc
    Inventors: John Dixon, Francis Ince
  • Patent number: 4719055
    Abstract: 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: Grant
    Filed: October 10, 1984
    Date of Patent: January 12, 1988
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4719049
    Abstract: 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: Grant
    Filed: October 17, 1984
    Date of Patent: January 12, 1988
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4719046
    Abstract: 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: Grant
    Filed: October 18, 1984
    Date of Patent: January 12, 1988
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4699928
    Abstract: 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: Grant
    Filed: November 6, 1986
    Date of Patent: October 13, 1987
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Ian A. McDonald
  • Patent number: 4686309
    Abstract: 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: Grant
    Filed: February 15, 1985
    Date of Patent: August 11, 1987
    Assignee: Rhone-Poulenc Sante
    Inventors: Jean-Claude Barriere, Jean-Pierre Corbet, Claude Cotrel, Daniel Farge, Jean-Marc Paris
  • Patent number: 4670470
    Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.
    Type: Grant
    Filed: August 29, 1985
    Date of Patent: June 2, 1987
    Assignee: Merck & Co., Inc.
    Inventor: Raymond A. Firestone
  • Patent number: 4588719
    Abstract: 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: Grant
    Filed: October 24, 1984
    Date of Patent: May 13, 1986
    Assignee: William H. Rorer, Inc.
    Inventors: William L. Studt, Donald E. Kuhla, Henry F. Campbell
  • Patent number: 4558071
    Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.
    Type: Grant
    Filed: February 25, 1983
    Date of Patent: December 10, 1985
    Assignee: Merck & Co., Inc.
    Inventor: Raymond A. Firestone
  • Patent number: 4537621
    Abstract: 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: Grant
    Filed: March 31, 1983
    Date of Patent: August 27, 1985
    Assignee: BASF Aktiengesellschaft
    Inventors: Adolf Parg, Hans Ziegler, Bruno Wuerzer
  • Patent number: 4534908
    Abstract: 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: Grant
    Filed: September 26, 1983
    Date of Patent: August 13, 1985
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hermann Fuchs, Klaus Filzinger
  • Patent number: 4529556
    Abstract: 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: Grant
    Filed: August 19, 1983
    Date of Patent: July 16, 1985
    Assignee: The Dow Chemical Company
    Inventor: Kenneth J. Bruza
  • Patent number: 4526893
    Abstract: 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: Grant
    Filed: December 16, 1983
    Date of Patent: July 2, 1985
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Toshihiro Takahashi, Noriyoshi Sueda, Masahiro Tsuji, Yoshiyuki Tahara, Hiroyasu Koyama, Yoshikuni Suzuki, Masao Nagase, Toshiji Sugai
  • Patent number: 4526973
    Abstract: 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: Grant
    Filed: June 9, 1982
    Date of Patent: July 2, 1985
    Assignee: Bristol-Myers Company
    Inventors: Aldo A. Algieri, Ronnie R. Crenshaw
  • Patent number: 4522943
    Abstract: 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: Grant
    Filed: April 21, 1982
    Date of Patent: June 11, 1985
    Assignee: Bristol-Myers Company
    Inventors: Aldo A. Algieri, Ronnie R. Crenshaw
  • Patent number: 4507500
    Abstract: 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: Grant
    Filed: July 7, 1981
    Date of Patent: March 26, 1985
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Shigenobu Nakayama, Eiichi Noda, Yoshiaki Noguchi, Isamu Yamamoto, Noboru Kawasaki
  • Patent number: 4415591
    Abstract: 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: Grant
    Filed: June 4, 1981
    Date of Patent: November 15, 1983
    Assignee: Georgia Tech Research Institute
    Inventors: Sheldon W. May, Robert S. Phillips, Heath H. Herman, Patricia W. Mueller
  • Patent number: 4388475
    Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.
    Type: Grant
    Filed: May 7, 1980
    Date of Patent: June 14, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Raymond A. Firestone
  • Patent number: 4364956
    Abstract: 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: Grant
    Filed: September 17, 1981
    Date of Patent: December 21, 1982
    Assignee: Lilly Industries Limited
    Inventors: Barry P. Clark, William J. Ross, Alec Todd
  • Patent number: 4339393
    Abstract: 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: Grant
    Filed: April 4, 1980
    Date of Patent: July 13, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Christian Luthi, Hans R. Meyer, Kurt Weber
  • Patent number: 4327214
    Abstract: 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: Grant
    Filed: September 12, 1980
    Date of Patent: April 27, 1982
    Assignee: BASF Aktiengesellschaft
    Inventors: Costin Rentzea, Hubert Sauter, Johann Jung