Abstract: A method for the treatment and/or prophylaxis of congestive heart failure, angina, occlusive peripheral vascular disease or cerebral vascular disease in mammals, such as humans, which method comprises administering to the mammal in need of such treatment and/or prophylaxis an effective and/or prophylactic amount of a compound of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, and X are set forth in the specification herein.
Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is a hydrogen atom or a C.sub.1-6 alkyl group, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are selected from hydrogen, hydroxyl, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy and C.sub.1-4 alkanoyl; G is a hydrogen atom or a hydroxyl group, and m and n are independently integers of from 1 to 3, with the proviso that when G is a hydroxyl grup, m or n is 1;is useful in the treatment of asthma.
Abstract: A pharmaceutical composition for topical administration consisting of two liquid phases designed to be admixed in situ or prior to use. The first phase contains a dissolved drug, and is preferably saturated in the drug, while the second phase is a chemically or physically different liquid from that in the first phase and contains no drug, but is miscible with the first phase. The two liquids are selected so that, on admixture of suitable volumes of the phases, the resultant drug concentration exceeds the saturated drug solubility in the resultant mixture. This produces a liquid mixture supersaturated in drug, which has been found to increase the rate of drug penetration into the skin. The two liquid phases may be gels, and the drug may be hydrocortisone.
Abstract: A topical composition for application to skin affected by acne containing from 0.05 to 2% by weight of Octopirox together with a non-irritant topically acceptable carrier. The composition is particularly useful for treating acne vulgaris.
Type:
Grant
Filed:
October 2, 1986
Date of Patent:
August 9, 1988
Assignee:
Beecham Group p.l.c.
Inventors:
Peter J. Edwards, Carol A. Jeffryes, Fiona M. Swain
Abstract: 2,2-Dimethyl-3,4-dihydro-2H-benzo[b]pyran-3-ols bearing an amino group in the 4-position and a cyano group in the benzo ring, their salts, esters and ethers, demonstrate excellent vasodilatory activity. The compounds, of which trans-2,2-dimethyl-4-isopropylamino-6-cyano-3,4-dihydro-2H-benzo[b]pyran-3 -ol is a representative embodiment, can be prepared from the corresponding 3,4-epoxy derivative upon treatment with an amine.
Abstract: A compound of the general formula I: ##STR1## or a salt or solvate thereof, in which, R.sup.1 represents hydrogen or a lower alkyl group,R.sup.2 represents hydrogen, a lower alkyl group, or ##STR2## R.sup.3 represents hydrogen, a lower alkyl group, or ##STR3## R.sup.4 represents a lower alkyl group substituted by one or more fluorine atoms,R.sup.5 represents hydrogen, halogen or lower alkyl, andR.sup.6 represents a lower alkyl or a substituted or unsubstituted carbocyclic aryl group. The compounds are useful as inhibitors of 5-lipoxygenase.
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.
Abstract: A fibrinolytically active hybrid protein which comprises one chain of a 2-chain protease linked to a chain of a different 2-chain protease, or to the same chain of the same protease, at least one of the chains in the hybrid protein being derived from a fibrinolytically active protease, such that the hybrid protein has a catalytic site essential for fibrinolytic activity which is optionally blocked by a removable blocking group.
Abstract: Compounds of the general formula I ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl or together are a group X which is C.sub.3-6 polymethylene optionally in which one carbon atom is replaced by O, S or NR.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl;R.sub.3 is a mono- or fused bi-cyclic heteroaromatic group having up to ten atoms in the aromatic ring(s), not more than four of which are selected from nitrogen, oxygen or sulphur, optionally C-substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl or cyano; or is phenyl or naphthyl, optionally substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl, carboxyl, C.sub.1-6 alkoxycarbonyl, cyano, CONR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X; NR.sub.9 R.sub.
Type:
Grant
Filed:
October 18, 1985
Date of Patent:
May 17, 1988
Assignee:
Beecham Group p.l.c.
Inventors:
Roger E. Markwell, Stephen A. Smith, David J. Hunter
Abstract: An antibacterially active 9,11-O-methylene derivative of 9-dihydroerythromycin wherein the methylene group is optionally substituted by one or two hydrocarbon groups. In particular, compounds of formula I and their pharmaceutically acceptable esters and acid addition salts: ##STR1## wherein: R.sup.1 and R.sup.2 are each H, optionally substituted hydrocarbon, or optionally substituted 5 or 6-membered O or S heterocyclyl, orR.sup.1 +R.sup.2 is optionally substituted divalent hydrocarbon,R.sup.3 is H or OH;R.sup.4 is H, F or OH;R.sup.5 and R.sup.6 are each H of CH.sub.3 ;one of R.sup.7 and R.sup.8 is H, OH, alkoxy, alkanoyloxy optionally substituted NH.sub.2, or R.sup.9 --SO.sub.2 --O--, and the other of R.sup.7 and R.sup.8 is H, orR.sup.7 +R.sup.8 is oxo, oxime or substituted oxime; and R.sup.9 is organic.
Abstract: A derivative of a fibrinolytic enzyme in which the catalytic site on the enzyme which is responsible for fibrinolytic activity is blocked by a human protein attached thereto by way of a reversible linking group.
Abstract: A method for the treatment and/or prophylaxis of incontinence in mammals, which method comprises administering to the mammal in need of said treatment an effective amount of a compound of formula (I): ##STR1## wherein R.sub.1 -R.sub.8 and X are as set forth herein.
Type:
Grant
Filed:
May 27, 1986
Date of Patent:
April 19, 1988
Assignee:
Beecham Group p.l.c.
Inventors:
Thomas C. Hamilton, Robin E. Buckingham
Abstract: Peptides comprising, in sequence, units selected from the amino acid residues 11 to 23 of vasoactive intestinal peptide (VIP) and consisting at least of the amino acid residues 15 to 20, or an analogue thereof wherein one or more of the amino acid residues is replaced by an equivalent other amino acid, or a pharmaceutically acceptable salt thereof; having pharmacological activity, a process for their preparation and their use as pharmaceuticals.
Type:
Grant
Filed:
October 31, 1985
Date of Patent:
April 12, 1988
Assignee:
Beecham Group p.l.c.
Inventors:
Eric A. Watts, Gordon Wootton, Christine Summers
Abstract: Compounds of formula (I): ##STR1## in which R.sub.1 is hydrogen or C.sub.1-6 alkyl;R.sub.2 is hydrogen or a group --CO.sub.2 R.sub.3 where R.sub.3 is hydrogen or C.sub.1-6 alkyl;n is an integer of from 2 to 12;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; and ##STR2## represents an aromatic heterocyclic ring, are disclosed as inhibitors of 5-lipoxygenase.
Abstract: A derivative of a fibrinolytic enzyme in which the catalytic site on the enzyme which is responsible for fibrinolytic activity is blocked by a human protein attached thereto by way of a reversible linking group.
Abstract: A method of treatment of migraine, cluster headaches and trigeminal neuralgia, radiation or cytotoxic agent induced nausea and vomiting and/or cardiac arrhythmia in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is C.sub.1-6 alkyl;R.sub.2 is amino or C.sub.1-7 acylamino;R.sub.3 is halo;one of R.sub.4 and R.sub.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-3 alkyl, which phenyl moieties may be substituted by one or more substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen;the other of R.sub.4 and R.sub.5 is hydrogen or C.sub.1-6 alkyl;p is 0 to 2; andq is 0 to 3.
Abstract: The invention provides crystalline paroxetine hydrochloride hemihydrate, processes for its preparation, compositions containing the same and its therapeutic use as an anti-depressant.
Type:
Grant
Filed:
October 23, 1986
Date of Patent:
January 26, 1988
Assignee:
Beecham Group p.l.c.
Inventors:
Roger D. Barnes, Marian W. Wood-Kaczmar, Alan D. Curzons, Ian R. Lynch, John E. Richardson, Philip C. Buxton
Abstract: A method of treatment of emesis, anxiety and/or IBS in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or (II) or a pharmaceutically acceptable salt thereof:Ar--Co--Y--Z (I)wherein Ar is a group of formula (a): ##STR1## wherein: R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-4 alkoxy, hydroxy, amino optionally substituted by one or two C.sub.1-4 alkyl groups, thiol, C.sub.1-4 alkylthio; X is CH.sub.2, NR.sub.3, --O-- or --S-- wherein R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.3-5 alkenyl, phenyl or phenyl C.sub.1-4 alkyl; or Ar is a group of formula (b): ##STR2## wherein R.sub.4 to R.sub.7 are independently hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, amino optionally substituted by one or two C.sub.1-4 alkyl, by C.sub.1-4 alkanoylamino or pyrrolyl, one of R.sub.4 to R.sub.
Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is C.sub.1-6 alkyl;R.sub.2 is amino or C.sub.1-7 acylamino;R.sub.3 is halo or C.sub.1-6 alkythio;R.sub.4 and R.sub.5 are independently selected from hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-4 alkyl any of which phenyl moieties may be substituted by one or two of halo, CF.sub.3, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.6 is C.sub.1-7 alkyl, --(CH.sub.2).sub.s R.sub.7, s being 0 to 2 andR.sub.7 being C.sub.3-8 cycloalky, --(CH.sub.2).sub.t R.sub.8, t being 1 or 2 andR.sub.8 being thienyl or phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy and C.sub.1-4 alkyl optionally substituted by hydroxy, C.sub.