Patents Represented by Attorney Arthur G. Seifert
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Patent number: 5177078Abstract: Compounds of formula ##STR1## where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups,R is hydrogen or lower alkyl,R.sup.1 is an aryl or heteroaryl radical,R.sup.2 is a mono- or bicyclic heterocyclic radical,R.sup.3 is hydrogen, lower alkyl or hydroxy andR.sup.4 is a aryl or heteroaryl radical,and their pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents which may be used, for example, for the treatment of CNS--disorders such as anxiety.Type: GrantFiled: September 30, 1991Date of Patent: January 5, 1993Assignee: John Wyeth & Brother LimitedInventors: Terence J. Ward, Graham J. Warrellow
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Patent number: 5169845Abstract: Piperazine derivative of formula ##STR1## and the pharmaceutically acceptable acid addition salts, where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups, m is 0, 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is aryl or a mono- or bicyclic heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is a heteroaryl radical, R.sup.4 is hydrogen, lower alkyl or aryl, and R.sup.5 is hydrogen, lower alkyl, cycloalkyl, cycloalkyl(lower)alkyl, aryl, or aryl(lower)alkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom are 5--HT.sub.1A -binding agents and may be used, for example, as anxiolytics.Type: GrantFiled: September 30, 1991Date of Patent: December 8, 1992Assignee: John Wyeth & Brother LimitedInventors: Ian A. Cliffe, Graham J. Warrellow
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Patent number: 5164385Abstract: Azetidine derivatives of formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula R is hydrogen or one or more specified substituents. The compounds have hypotensive activity. Some are also 5-HT.sub.1A agonists.Type: GrantFiled: September 9, 1991Date of Patent: November 17, 1992Assignee: John Wyeth & Brother, Ltd.Inventors: Ian A. Cliffe, Alan C. White
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Patent number: 5086073Abstract: The invention concerns compounds having formula: ##STR1## or a salt thereof, wherein E represents hydrogen, lower alkyl or a group Ar.sup.1 --A.sup.1 ; Ar and Ar.sup.1 are the same or different aryl groups (including heteroaryl) which are optionally substituted, e.g. by one or more substituents commonly used in pharmaceutical chemistry; A and A.sup.1 are the same or different alkylene groups having one or two carbon atoms linking Ar or Ar.sup.1 to N and optionally substituted by lower alkyl and/or optionally substituted aryl, B is an alkylene group of 3 or 4 carbon atoms, which may be substituted by lower alkyl; D.sup.1 represents halogen, CH.sub.3, CR.sup.1 R.sup.2 NH.sub.2, SO.sub.3 H or SO.sub.2 NR.sup.6 R.sup.7 where R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl and R.sup.6 and R.sup.7 are each hydrogen, lower alkyl or aralkyl of 7 to 12 carbon atoms or R.sup.6 and R.sup.Type: GrantFiled: May 30, 1990Date of Patent: February 4, 1992Assignee: John Wyeth & Brother LimitedInventors: John F. White, Michael C. Warren, Christine Ennis
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Patent number: 5082843Abstract: Novel ethers of formula ##STR1## their heteroaromatic N-oxides, and the pharmaceutically acceptable acid additions of the compounds of formula (I) and their N-oxides possess 5-HT.sub.3 -antagonistic activity. In the formula ##STR2## represents an optionally substituted heteroaryl group containing a hetero atom X and -B represents a saturated azabicyclic ring such as quinuclidyl or tropanyl.Type: GrantFiled: October 30, 1990Date of Patent: January 21, 1992Assignee: John Wyeth and Brother LimitedInventor: Ian A. Cliffe
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Patent number: 5068342Abstract: Disclosed herein are 1- or 2-thio, thiomethylene, and sulfonylnaphthalene derivatives of formulas I and II ##STR1## or a pharmaceutically acceptable cationic salt thereof, wherein n is 0 or 1R.sub.5 is hydrogen, bromo, chloro, trifluoromethyl or difluoroethyl;R.sub.6 is hydrogen, hydroxy, methoxy or ethoxy; andR.sub.7 is hydrogen or R.sub.7 and R.sub.6 are both methyl or ethyl carbonate,provided that, when S(O).sub.2 is in the 2 position of the naphthalene ring, R.sub.5, R.sub.6 and R.sub.7 are each hydrogen. The disclosed compounds possess blood-glucose lowering actions and are useful in the treatment of diabetes mellitus.Type: GrantFiled: October 12, 1990Date of Patent: November 26, 1991Assignee: American Home Products CorporationInventors: Arie Zask, Ivo Jirkovsky
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Patent number: 5064842Abstract: The invention concerns compounds of formula ##STR1## or salts thereof; wherein:.alpha. and .beta. together represent a bond and additionally when B is an electron withdrawing group .alpha. can also represent OH and .beta. can represent hydrogen;Ar is an optionally substituted aryl or heteroaryl radical;R represents hydrogen or an optionally substituted alkyl or aralkyl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optioanlly substituted aryl or heteroaryl;A represents a group of formula --XR.sup.3 wherein X is a group of formula --(CHR.sup.6).sub.p --Y--(CHR.sup.7).sub.q -- in which formula: Y represents --O--, --S--, NR.sup.8 or a direct bond, p and q each represent 0, 1 or 2 R.sup.6, R.sup.7 and R.sup.Type: GrantFiled: June 25, 1990Date of Patent: November 12, 1991Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, Terence J. Ward, Albert Opalko
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Patent number: 5043466Abstract: The preparation of compounds having the formula I ##STR1## where R.sup.1 is --CN, --CO--N(CH.sub.3).sub.2 or --CS--N(CH.sub.3).sub.2 and R.sup.2 is hydrogen, methyl or a removable protecting group is carried out by condensing a compound having the formula ##STR2## where M is lithium, sodium, potassium or halomagnesium and R.sup.3 is methyl or a removable protecting group in a solvent comprising 80-100% of one or more hydrocarbons and 0-20% of one or more ethers.The solvent enables less inconvenient reaction temperatures to be used and higher yields to be obtained. Compounds (I) are new per se where R.sup.1 is --CS--N(CH.sub.3).sub.2. Compounds (I) are chemical intermediates for preparing N,N-dimethyl-2-(1-hydroxycyclohexyl)-2-(4-hydroxyphenyl or 4-methoxyphenyl) ethylamine and pharmaceutically acceptable salts thereof. These end products are antidepressants.Type: GrantFiled: January 26, 1990Date of Patent: August 27, 1991Assignee: John Wyeth & Bro., LimitedInventor: Robin G. Shepard
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Patent number: 5000975Abstract: Disclosed herein are all vegetable oil fat compositions having a randomized palmitic acid oil as the sole palmitic acid oil. The novel all vegetable oil fat compositions are particularly for use in human infant nutritional products and combine a lauric acid oil, an oleic acid oil and a linoleic acid oil with the randomized palmitic acid oil. Sunflower oleic oil and canola (LEAR) oil may be used as oleic acids oils. For preterm or low birth weight infants, medium-chain triglycerides (MCTs) are also included in the all vegetable oil fat compositions of the invention.Type: GrantFiled: December 29, 1988Date of Patent: March 19, 1991Assignee: American Home Products CorporationInventor: Rudolph M. Tomarelli
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Patent number: 4997948Abstract: Disclosed herein are 1- or 2-thio, thiomethylene, and sulfonylnaphthalene derivatives of formulas I and II ##STR1## or a pharmaceutically acceptable catonic salt thereof, wherein n is 0 or 1R.sub.5 is hydrogen, bromo, chloro, trifluoromethyl or difluoroethyl;R.sub.6 is hydrogen, hydroxy, methoxy or ethoxy; andR.sub.7 is hydrogen or R.sub.7 and R.sub.6 are both methyl or ethyl carbonate,provided that, when S(O).sub.2 is in the 2 position of the naphthalene ring, R.sub.5, R.sub.6 and R.sub.7 are each hydrogen. The disclosed compounds possess blood-glucose lowering actions and are useful in the treatment of diabetes mellitus.Type: GrantFiled: October 27, 1989Date of Patent: March 5, 1991Assignee: American Home ProductsInventors: Arie Zask, Ivo Jirkovsky
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Patent number: 4997839Abstract: Novel ethers of formula ##STR1## their heteroaromatic N-oxides, and the pharmaceutically acceptable acid additions of the compounds of formula (I) and their N-oxides possess 5-HT.sub.3 -antagonistic activity. In the formula ##STR2## represents an optionally substituted heteroaryl group containing a hetero atom X and -B represents a saturated azabicyclic ring such as quinuclidyl or tropanyl.Type: GrantFiled: March 22, 1990Date of Patent: March 5, 1991Assignee: John Wyeth & Brother LimitedInventor: Ian A. Cliffe
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Patent number: 4985438Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6 ; and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substitutent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: October 19, 1988Date of Patent: January 15, 1991Assignee: John Wyeth & Brother, LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 4983617Abstract: The invention concerns a new stable crystal form of anhydrous, crystalline 1,4-dihydro-2-(imidazol-1-ylmethyl)-6-methyl-4-(3-nitrophenyl)pyridine)-3, 5-dicarboxylic acid 3-ethyl 5-methyl diester hydrochloride, "having a melting point greater than about 215.degree. C., an infra red spectrum (nujolmull) having sharp peaks at 3195 cm.sup.-1, 3100 cm.sup.-1, 2735 cm.sup.-1 and 2625 cm.sup.-1 and an x-ray powder diffraction pattern with specific peaks occurring at 2.theta.=12.3.degree. and 44.5.degree..Type: GrantFiled: December 12, 1988Date of Patent: January 8, 1991Assignee: John Wyeth and Brothers LimitedInventors: Gerald Bradley, Geoffrey P. R. Carr, Albert Opalko, Richard J. Yarwood
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Patent number: 4959375Abstract: Piperidine derivatives of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein A represents an aromatic radical selected from ##STR2## wherein R.sup.3 is hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy or halogen; X.sup.1 -X.sup.2 represents CH.sub.2 --CH, NR.sup.4 --CH, O--CH, S--CH, CH.sub.2 --N, O--N, S--N, NR.sup.4 --N, CH--NR.sup.4 or N--NR.sup.4 [where R.sup.4 is hydrogen, (C.sub.1-4)alkyl, phenyl or phenyl(C.sub.1-4)alkyl] or ##STR3## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen, halogen, trifluoromethyl, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, hydroxy, nitro, amino, (C.sub.1-4)alkylamino, di(C.sub.1-4)alkyl-amino, (C.sub.2-4)alkanoylamino, mercapto or (C.sub.1-4)alkylthio and R.sup.1 and R.sup.2 are independently hydrogen, (C.sub.1-4)alkyl or (C.sub.1-4)alkylphenyl or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached represent pyrrolidino or piperidino possess 5-HT.sub.3 -antagonistic activity.Type: GrantFiled: February 21, 1989Date of Patent: September 25, 1990Assignee: John Wyeth & Brothers LimitedInventor: Terence J. Ward
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Patent number: 4955481Abstract: Packaging for a course of tablets comprises a base for a blister pack and a cover flap. Rub-off indicators are provided on the inner surface of the flap to permit indication of one of a range of alternatives related to the course. The indicators may be color keyed to particular doses of the course. A method of using such a pack is also disclosed.Type: GrantFiled: July 3, 1986Date of Patent: September 11, 1990Assignee: American Home Products Corp.Inventors: Michael V. Novinski, Thomas J. Patton
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Patent number: 4935515Abstract: Disclosed herein are novel 1,2,3,4,5,6-hexahydro[1,3,6]triazocino[1,2-a]benzimidazole of Formulas I and II: ##STR1## wherein R.sup.1 may be phenyl, m- or p-nitrophenyl, m- or p-methylsulfonylaminophenyl, napthtyl, naphthyl mono-substituted by nitro or methylsulfonylamino, benzofurazanyl, 2-pyrimidinyl, 2- or 4-pyridinyl, 2- or 4-naphthyridinyl, pyrazinyl, isoquinolinyl, or quinolinyl;R.sup.2 may be hydrogen; C.sub.1 -C.sub.8 alkyl; phenyl(C.sub.1 -C.sub.4)alkyl or substituted-phenyl(C.sub.1 -C.sub.4)alkyl, in which phenyl may have one to three substituents selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluorine, chlorine or bromine; phenyl or substituted-phenyl in which the phenyl substituents are the same as for substituted-phenyl (C.sub.1 -C.sub.4)alkyl; 2- or 4-pyrimidinyl; pyrazinyl; imidazolyl; C.sub.1 -C.sub.4 alkanoyl; halo or dihalo-(C.sub.1 -C.sub.4)alkanoyl, in which halo is fluoro or chloro; benzoyl or benzoyl substituted on the phenyl ring by one or two C.sub.1 -C.sub.Type: GrantFiled: November 6, 1989Date of Patent: June 19, 1990Assignee: American Home Products CorporationInventors: Michael W. Winkley, James L. Diebold
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Patent number: 4929625Abstract: Novel ethers of formula ##STR1## their heteroaromatic N-oxides, and the pharmaceutically acceptable acid additions of the compounds of formula (I) and their N-oxides possess 5-HT.sub.3 -antagonistic activity. In the formula ##STR2## represents an optionally substituted heteroaryl group containing a hetero atom X and --B represents a saturated azabicyclic ring such as quinuclidyl or tropanyl.Type: GrantFiled: August 1, 1988Date of Patent: May 29, 1990Assignee: John Wyeth and Brothers LimitedInventor: Ian A. Cliffe
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Patent number: 4921860Abstract: Pyridyl ethers of formula ##STR1## [where R is hydrogen, or 1 to 4 hydroxy, alkyl, alkoxy, amino, alkylamino, dialkylamino, halogen, trifluoromethyl, phenyl, halophenyl, alkyphenyl, alkoxyphenyl, carboxy, carboxamide, nitro, thiol or alkylthio substituents and B is quinuclidyl or tyopanyl] are useful for the treatment of conditions which respond to antagonism of 5 - HT.sub.3 receptors e.g. the treatment of migraine, emesis, anxiety, gastro-intestinal disorders and psychotic disorders.Type: GrantFiled: August 1, 1988Date of Patent: May 1, 1990Assignee: John Wyeth and Brother, LimitedInventor: Ian A. Cliffe
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Patent number: 4900750Abstract: This invention concerns compounds of formula ##STR1## or salts thereof, wherein: Ar is an optionally substituted aryl radical;R represents hydrogen or an optionally substituted alkyl, aralkyl, or aryl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optionally substituted aryl;A and B independently represent a group of formula --XR.sup.3 whereinX is a group of formula --(CHR.sup.6).sub.p Y(CHR.sup.7).sub.q --whereinY represents --O--, --S--, --NR.sup.8 -- or a direct bond; p and q each represent 0, 1 or 2 providing that p and q do not both represent O when Y is a direct bond; and R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or alkyl; and R.sup.Type: GrantFiled: August 3, 1987Date of Patent: February 13, 1990Assignee: John Wyeth & Brother, LimitedInventors: John L. Archibald, Terence J. Ward, Albert Opalko
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Patent number: 4889808Abstract: Disclosed herein is a method of enhancing the production of tissue plasminogen activator (t-PA) and single chain urokinase plasminogen activator (SCU-PA) by normal human lung diploid fibroblast cells in a serum-free medium. The method comprises the addition of heparin (or low molecular weight heparin) and an endothelial cell growth factor to the culture medium.Type: GrantFiled: September 17, 1986Date of Patent: December 26, 1989Assignee: American Home ProductsInventor: Ruth Rappaport