Abstract: Certain endo-9-lower-alkyl 9-azabicyclo[3.3.1]nonane-3-amines are valuable intermediates for the preparation of 2-methoxy-4-amino-5-halo-N-[9-lower-alkyl]-azabicyclo[3.3.1]nonanylbenzami des wherein said final products possess useful pharmacological activity, such as ability to regulate gastro-intestinal function, anti-emetic activity and CNS activity.
Abstract: A monocyclic .beta.-lactam antibiotic having a formamido substituent at the 3S-position, including compounds of the formula (I): ##STR1## and salts thereof wherein R is --SO.sub.3 H; --PO(OH)Y wherein Y is C.sub.1-6 alkoxy, hydroxy, aryloxy, C.sub.1-6 alkyl or aryl; ##STR2## wherein Z represents C.sub.1-6 alkyl or aryl; ##STR3## wherein Z.sup.1 and Z.sup.2 may be the same or different and each represents hydrogen, C.sub.1-6 alkyl, aryl, amino or C.sub.1-6 alkoxy, or Z.sup.1 and Z.sup.2 together form the residue of a heterocyclic ring; --OSO.sub.3 H; or ##STR4## where X is hydrogen or hydroxy; R.sup.1 is an amino, protected amino or carboxylic acylamino group, and R.sup.2 and R.sup.3 are independently selected from hydrogen or a hydrocarbon group of 1 to 18 carbon atoms.
Type:
Grant
Filed:
March 3, 1986
Date of Patent:
November 3, 1987
Assignee:
Beecham Group p.l.c.
Inventors:
Roger J. Ponsford, Michael J. Pearson, Stephen C. Finch
Abstract: A compound of formula (I): ##STR1## or a salt thereof, in which Y is a group--O(CH.sub.2).sub.m CH<, --(CH.sub.2).sub.m CH<, or --CH.dbd.C< wherem is an integer of from 1 to 5,n is an integer of from 4 to 12,each of R.sup.1 and R.sup.2, which may be the same or different, represents hydrogen or C.sub.1-6 alkyl,X represents a double or triple bond, and each of A and B represents hydrogen when X is a double bond, or both A and B are absent when X is a triple bond,is useful in treating allergic diseases.
Abstract: A compound of formula (XXII): ##STR1## or a compound of formula (XXIII): ##STR2## wherein in formula (XXIII), j.sup.1 -1 is 1 to 4; and Q.sub.6 and Q.sub.7 are on the same carbon atom; and wherein, in formulae (XXII) and (XXIII), Q.sub.6 is NH.sub.2 and Q.sub.7 is H, and either p is 0 to 2 and q is 1; or p is 1 and q is 0 to 3; and one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl --C.sub.1-3 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen; and the other of R.sub.5 and R.sub.6 is hydrogen or C.sub.1-6 alkyl.
Abstract: A process for preparing 3-thienyl malonic acid, comprising treatment of a 3-thienyl cyanoacetate of formula (III): ##STR1## where R.sup.1 represents an aryl or alkyl group, with at least a molar excess of an alkali metal hydroxide.
Abstract: Compounds of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl,C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, C.sub.1-6 alkyl-thiolmethyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.2 is nitro, cyano or C.
Abstract: A compound of formula I ##STR1## or a salt or ester thereof. Processes for the preparation of these compounds and the use of these compounds in the preparation of further bicyclic compounds are also disclosed.
Abstract: A monocyclic .beta.-lactam antibiotic having a formamido substitutent at the 3S-position, including compounds of the formula (I): ##STR1## and salts thereof wherein R is --SO.sub.3 H; --PO(OH)Y wherein Y is C.sub.1-6 alkoxy, hydroxy, aryloxy, C.sub.1-6 alkyl or aryl; ##STR2## wherein Z represents C.sub.1-6 alkyl or aryl; ##STR3## wherein Z.sup.1 and Z.sup.2 may be the same or different and each represents hydrogen, C.sub.1-6 alkyl, aryl, amino or C.sub.1-6 alkoxy, or Z.sup.1 and Z.sup.2 together form the residue of a heterocyclic ring; --OSO.sub.3 H; or ##STR4## where X is hydrogen or hydroxy; R.sup.1 is an amino, protected amino or carboxylic acylamino group, and R.sup.2 and R.sup.3 are independently selected from hydrogen or a hydrocarbon group of 1 to 18 carbon atoms.
Type:
Grant
Filed:
December 7, 1984
Date of Patent:
July 7, 1987
Assignee:
Beecham Group p.l.c.
Inventors:
Roger J. Ponsford, Michael J. Pearson, Stephen C. Finch
Abstract: A container (1) for dispensing viscous liquids consists of a hollow, resilient oval body (2) having a valve cap (6), and a hook-shaped support (7) slidably attached to the body (2). The support (7) may be fully extended and the hook (9) used to suspend the container (1) from a shower rail. Liquid may then be obtained from the container (1) by squeezing the body (2).
Abstract: Compounds of formula (I) ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkylthiocarbonyl, C.sub.1-6 alkoxythiocarbonyl, C.sub.1-6 alkylthiocarbonyloxy, C.sub.1-6 alkylthiolmethyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.
Abstract: A fibrinolytically active protein conjugate comprising at least one optionally blocked fibrinolytic enzyme linked by way of a site other than the catalytic site responsible for fibrinolytic activity to at least one human protein.Processes from making the conjugates and pharmaceutical compositions containing them are also described.
Type:
Grant
Filed:
January 9, 1985
Date of Patent:
June 16, 1987
Assignee:
Beecham Group p.l.c.
Inventors:
Harry Ferres, Richard A. G. Smith, Andrew J. Garman
Abstract: A compound of formula (I) or a salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl;R.sub.2 is hydrogen or C.sub.1-6 alkyl;R.sub.3 is C.sub.2-10 alkenyl or C.sub.1-10 alkyl substituted by hydroxy, C.sub.1-4 alkoxy, thiol, C.sub.1-4 alkylthio or NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are independently hydrogen or C.sub.1-6 alkyl or together are C.sub.3-6 polymethylene;R.sub.4 and R.sub.5 are independently hydrogen or C.sub.1-4 alkyl; andR.sub.6 is hydrogen; or C.sub.1-4 alkyl or benzyl attached at nitrogen atom 1 or 2;having anti-inflammatory and/or anti-allergy activity.
Abstract: An anti-perspirant composition includes 30% by weight of an anti-perspirant agent, aluminium chlorhydrate, 68.5% by weight of ethanol and 1.5% by weight of a long chain fatty acid, myristic acid.The presence of the fatty acid counteracts the reduction in efficacy caused by the high concentration of ethanol.
Abstract: Compounds of formula (I): ##STR1## or a salt thereof, in which W is phenyl optionally substituted by halogen or trifluoromethyl, or a benzofuran-2-yl group,R.sup.1 is hydrogen or methyl,R.sup.2 is carboxyl or a group O--Z--CO.sub.2 H or an ester or amide thereof; a group O--E--NR.sup.3 R.sup.4 or a group O--E--OR.sup.5,wherein R.sup.3, R.sup.4 and R.sup.5 each represents hydrogen or C.sub.1-6 alkyl, Z is a C.sub.1-6 straight or branched alkylene chain, n is 1 or 2, a is 2 or 3, and E is a C.sub.2-7 straight or branched alkylene chain with at least two carbon atoms separating the two heteroatoms in the group R.sup.2 ; a process for the production of such compounds and their use in medicine as anti-hyperglycaemic and/or anti-obesity agents.
Abstract: Pharmaceutical compositions with comprise a compound of the formula (I): ##STR1## wherein X is a chlorine or bromine atom or a methoxyl, methylthio or alkyl group of 1-4 carbon atoms; Y is a --CHR.sub.1 --CH.sub.2 -- or --CR.sub.1 .dbd.CH-- group where R.sub.1 is a hydrogen atom or a methyl group and A is a CHOH or CO group, and a pharmaceutically acceptable carrier selected from the group of creams, ointments, lotions, gels, aerosols, sprays, liniments and gel sticks. The compositions possess systemic anti-inflammatory activity when administered topically.
Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolyzable ester thereof: ##STR1## R is phenyl, substituted phenyl, C.sub.3-6 cycloalkyl cyclohexenyl, cyclohexadienyl, or a 5- or 6-membered heterocyclic ring containing up to three hetero-atoms slected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen, substituted amino or C.sub.1-6 alkoxy; Q represents acetoxy, carbamoyloxy, heterocyclylthio group, or a nitrogen containing heterocyclic group bonded via nitrogen; R.sup.1 is hydrogen or a C.sub.1-6 alkyl group and R.sup.2 is an optionally substituted 5- or 6-membered heterocyclic group containing one or two heteroatoms; or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form an optionally substituted five- or six-membered heterocyclic group containing one or two nitrogen heteroatoms; a process for the preparation of such compounds and pharmaceutical compositions comprising them.
Abstract: A compound of formula (I): ##STR1## in which R is optionally substituted phenyl; C.sub.3-8 cycloalkyl; C.sub.5-8 cycloalkenyl; C.sub.1-8 alkyl which may be straight or branched; C.sub.2-8 alkenyl which may be straight or branched; 5- or 6- membered heterocyclyl; or optionally substituted phenyl C.sub.1-4 alkyl, each of Y and Z, which may be the same or different, is oxygen or sulphur; and X is --CH.sub.2 -- or oxygen, a process for the preparation of such compounds and their use in human and veterinary medicine.
Abstract: The compounds of the formula (II): ##STR1## and their pharmaceutically acceptable salts wherein R.sub.1 is a hydrogen, fluorine or chlorine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R.sub.2 is a hydrogen, fluorine or chlorine atom or a hydroxyl group; R.sub.3 is a hydrogen or chlorine atom or a hydroxyl group; R.sub.4 is a carboxylic acid group or a salt, ester or amide thereof; R.sub.5 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R.sub.6 is a hydrogen atom or a methyl, or propyl group; X is an oxygen atom or a bond; and Y is an alkylene group of up to 6 carbon atoms or a bond have been found to possess anti-obesity and/or anti-hyperglycaemic activity.