Patents Represented by Attorney William J. Stein
  • Patent number: 4650907
    Abstract: Novel nonaromatic fluoroallylamines are potent MAO inhibitors and at low dose selectively inhibit MAO-B. They are useful in the treatment of depression and coadministered with L-dopa, in the treatment of Parkinsonism.
    Type: Grant
    Filed: December 5, 1985
    Date of Patent: March 17, 1987
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Philippe Bey, Michael G. Palfreyman, Ian A. McDonald
  • Patent number: 4621145
    Abstract: 4-Amino-5-hexenoic acid is prepared by:(a) reacting 5-oxo-2-pyrrolidine-acetonitrile with hydrogen and dimethylamine in the presence of a palladium catalyst to form N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]ethylamine;(b) oxidizing N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]-ethylamine to produce the corresponding N-oxide derivative;(c) pyrolysis of the N-oxide derivative to form 5-vinyl-2-pyrrolidinone;(d) optionally, separating N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]ethylamine by-product from the 5-vinyl-2-pyrrolidinone product; and(e) hydrolyzing 5-vinyl-2-pyrrolidinone to form 4-amino-5-hexenoic acid.
    Type: Grant
    Filed: November 29, 1983
    Date of Patent: November 4, 1986
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Wolfgang Frieben, Fritz Gerhart
  • Patent number: 4612312
    Abstract: Glutarimide derivatives of the formula which are useful antihypertensive and antianxiety agents ##STR1## wherein R.sub.1 and R.sub.2 each independently represent hydrogen, a 1 to 4 carbon alkyl, a 1 to 4 carbon alkoxy, halogen, nitro, hydroxy, SO.sub.3 H, SO.sub.2 NH.sub.2, and when R.sub.1 and R.sub.2 are taken together, form a fused phenyl group at the 1,2- or 3,4- positions, with the proviso that when R.sub.1 and R.sub.2 are identical they each represent a hydrogen, a 1 to 4 carbon alkyl, a 1 to 4 carbon alkoxy, hydroxy or a halogen group; A and B independently represent an oxo, a thio or an imino group having the formula --N(R.sub.6)-- wherein the R.sub.6 group is hydrogen or a 1 to 4 carbon alkyl group; R.sub.3 is a hydrogen, a 1 to 4 carbon alkyl or hydroxyethyl group; n is an integer of from 2 to 5; and R.sub.4 and R.sub.5 represent methyl groups or when taken together form a cyclopentane or cyclohexane ring; its enantiomers; and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: June 13, 1985
    Date of Patent: September 16, 1986
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Marcel Hibert, Maurice W. Gittos
  • Patent number: 4612318
    Abstract: The present invention refers to a new class of pyrazolopyridines having analgetic, anxiolytic, antiinflammatory and CNS-depressant activity. It is described a process for producing the compounds as well as pharmaceutical compositions containing them.
    Type: Grant
    Filed: September 19, 1983
    Date of Patent: September 16, 1986
    Assignee: Gruppo Lepetit S.p.A.
    Inventor: Giorgio Winters
  • Patent number: 4595697
    Abstract: Glycine, sarcosine, or N,N-dimethylglycine exerts a synergistic effect upon gamma-vinyl GABA for the treatment of seizure disorders, in particular epilepsy.
    Type: Grant
    Filed: February 27, 1985
    Date of Patent: June 17, 1986
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Nikolaus Seiler, Shakir Sarhan
  • Patent number: 4594348
    Abstract: The present invention is directed to a new pharmacological use of some known naphthoimidazole derivatives. More particularly, the compounds of the invention are 2-[2-(4-phenyl-1-piperazinyl)ethyl]-1H-naphtho[1,2-d]imidazoles of formula ##STR1## wherein R is selected from methyl and 1-methylethyl and R.sup.1 is selected from hydrogen, chloro, methoxy and trifluoromethyl and the pharmaceutically acceptable acid addition salts thereof and possess antihypertensive activity.
    Type: Grant
    Filed: February 6, 1985
    Date of Patent: June 10, 1986
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Emilio Toja, Domenico Barone, Emiliana Baldoli
  • Patent number: 4594187
    Abstract: The present invention is directed to a chemical process for preparing the antibiotic substance denominated antibiotic L 17054 and its pharmaceutically acceptable salts by selectively hydrolyzing teicoplanin or a factor or component thereof with a concentrated strong organic acid.
    Type: Grant
    Filed: December 11, 1984
    Date of Patent: June 10, 1986
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Paolo Strazzolini, Adriano Malabarba, Bruno Cavalleri
  • Patent number: 4585866
    Abstract: Migraine is treated with a tropyl benzoate derivative of the following general formula: ##STR1## wherein: R.sub.1 represents C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen;R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen; andR.sub.3 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen, provided that R.sub.3 is hydrogen when R.sub.2 is hydrogen, or a pharmaceutically acceptable salt thereof.Additionally, some novel tropyl benzoate derivatives are disclosed.
    Type: Grant
    Filed: December 13, 1984
    Date of Patent: April 29, 1986
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: John R. Fozard, Maurice W. Gittos
  • Patent number: 4576746
    Abstract: New .beta.-lactam acetic acid derivatives I ##STR1## wherein R represents alkyl, alkyl substituted with amino, protected amino, mono- or di-alkylamino, hydroxy, protected hydroxy or alkoxy, and alkenyl, and their salts are useful as intermediates for preparing 1-azabicyclo [3.2.0]hept-2-ene antibiotics II ##STR2## The process for preparing the .beta.-lactam acetic acid derivatives I as well as the overall process which starting from the acids I leads to the antibiotics II are also claimed.
    Type: Grant
    Filed: March 4, 1982
    Date of Patent: March 18, 1986
    Assignee: Gruppo Lepetit, S.p.A.
    Inventors: Duccio Favara, Amedeo Omodei-Sale', Pietro Consonni
  • Patent number: 4563465
    Abstract: Migraine is treated with a tropyl benzoate derivative of the following general formula: ##STR1## wherein: R.sub.1 represents C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen;R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen; andR.sub.3 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen, provided that R.sub.3 is hydrogen when R.sub.2 is hydrogen, or a pharmaceutically acceptable salt thereof.Additionally, some novel tropyl benzoate derivatives are disclosed.
    Type: Grant
    Filed: December 13, 1984
    Date of Patent: January 7, 1986
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: John R. Fozard, Maurice W. Gittos
  • Patent number: 4560795
    Abstract: Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein Y is F.sub.2 CH--, F.sub.3 C--, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR2## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; each of R.sub.a and R.sub.b can be the same or different and is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR3## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.
    Type: Grant
    Filed: February 6, 1984
    Date of Patent: December 24, 1985
    Assignee: Merrell Dow France et Cie.
    Inventors: Philippe Bey, Michel Jung
  • Patent number: 4551550
    Abstract: 1. A compound of the formula:H.sub.2 C.dbd.C.dbd.CHCH.sub.2 NHCH.sub.2 --Z--CH.sub.2 NHRwherein:Z is --CH.sub.2 CH.sub.2 -- or trans-CH.dbd.CH--,R is H, CH.sub.3 --, CH.sub.3 CH.sub.2, CH.sub.3 (CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 NH.sub.2, --(CH.sub.2).sub.3 NHCOCH.sub.3, --CH.sub.2 CH.dbd.CH.sub.2, or --CH.sub.2 CH.dbd.C.dbd.CH.sub.2,or a pharmaceutically acceptable acid addition salt thereof are inhibitors of polyamine oxidase.
    Type: Grant
    Filed: December 17, 1984
    Date of Patent: November 5, 1985
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Philippe Bey
  • Patent number: 4547521
    Abstract: The present invention is directed to new 16-methoxy-16-methyl prostaglandin E.sub.1 derivatives of the following general formula ##STR1## wherein R stands for a (C.sub.1-4) alkyl group or a non-toxic pharmaceutically acceptable cation, to a process for preparing them and to their use as gastroprotective agents.
    Type: Grant
    Filed: November 18, 1983
    Date of Patent: October 15, 1985
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Umberto Guzzi, Romeo Ciabatti
  • Patent number: 4542018
    Abstract: The invention refers to an individual antibiotic substance selected from the group consisting of Teichomycin A.sub.2 factor 1, Teichomycin A.sub.2 factor 2, Teichomycin A.sub.2 factor 3, Teichomycin A.sub.2 factor 4 and Teichomycin A.sub.2 factor 5 in substantially pure form, and to the method of producing them by recovery from Teichomycin A.sub.2, a known antibiotic substance, by means of high-efficiency chromatographic methods. The single pure Teichomycin A.sub.2 factor 1, Teichomycin A.sub.2 factor 2, Teichomycin A.sub.2 factor 3, Teichomycin A.sub.2 factor 4 and Teichomycin A.sub.2 factor 5 are biologically distinguishable from Teichomycin A.sub.2 in that they have a higher degree of antibiotic activity against susceptible microorganisms.
    Type: Grant
    Filed: June 7, 1983
    Date of Patent: September 17, 1985
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Angelo Borghi, Rosa Pallanza, Carolina Coronelli, Giovanni Cassani
  • Patent number: 4540582
    Abstract: Glycine, sarcosine, or N,N-dimethylglycine exerts a synergistic effect upon gamma-vinyl GABA for the treatment of seizure disorders, in particular epilepsy.
    Type: Grant
    Filed: March 28, 1984
    Date of Patent: September 10, 1985
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Nikolaus Seiler, Shakir Sarhan
  • Patent number: 4535090
    Abstract: 3,5-diphenyl-1H-1,2,4-triazoles with contragestational activity of the following formula ##STR1## wherein R may be located on one or the other of the two adjacent nitrogen atoms and may represent hydrogen or a group R.sub.5 CO-- wherein R.sub.5 is an aliphatic saturated or unsaturated hydrocarbyl containing from 1 to 20 carbon atoms, R.sub.1, R.sub.2 and R.sub.3, each independently are selected from hydrogen, lower alkyl and lower alkoxy or R.sub.2 and R.sub.3 together may represent a methylenedioxy group, and R.sub.4 is an aliphatic saturated or unsaturated hydrocarbyl group of from 1 to 20 carbons, with the proviso that when R is hydrogen or an R.sub.5 CO-- group wherein R.sub.5 contains 4 or less carbon atoms, R.sub.4 must contain 5 or more carbons.These compounds have proven to be highly effective in terminating pregnancy in several animal species after a single parenteral injection.
    Type: Grant
    Filed: October 15, 1982
    Date of Patent: August 13, 1985
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Giulio Galliani, Amedeo Omodei-Sale, Pietro Consonni, Alessandro Assandri
  • Patent number: 4530927
    Abstract: New isoxazole[5,4-b]pyridines having antiinflammatory, CNS-depressant and cardiovascular activity.
    Type: Grant
    Filed: March 28, 1983
    Date of Patent: July 23, 1985
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Giorgio Winters, Alberto Sala
  • Patent number: 4529733
    Abstract: Novel 1,4-dihydropyridine derivatives have the following general Formula: ##STR1## and are calcium antagonists, useful for treating cardiovascular diseases.
    Type: Grant
    Filed: March 22, 1984
    Date of Patent: July 16, 1985
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Maurice W. Gittos, Michael Spedding
  • Patent number: 4528297
    Abstract: New 3-azetidinylethyl-1-phenyl-2-imidazolidinones with neuroleptic activity, their use and methods for their preparation. The azetidinyl group bears alkyl substituents in position 3 and the phenyl group bears halogenated substituents in position 3 and hydroxy group or acylated hydroxy groups in position 4 and/or 6.
    Type: Grant
    Filed: March 4, 1983
    Date of Patent: July 9, 1985
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Luigi Fontanella, Edoardo Martinelli, Alessandro Assandri
  • Patent number: RE31980
    Abstract: Novel compounds of the following general formula are useful pharmacologic agents: ##STR1## R is .[.selected from.]. hydrogen.[., alkylcarbonyl wherein the alkyl moiety contains from 1 to 4 carbon atoms, alkoxycarbonyl wherein the alkoxy moiety contains from 1 to 4 carbon atoms and may be straight or branched, and ##STR2## wherein R.sub.10 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl.].; R.sub.2 is .[.selected from.]. hydroxy.[., a straight or branched alkoxy group of from 1 to 8 carbon atoms, a lower alkylamino group wherein the alkyl moiety contains from 1 to 4 carbon atoms, and ##STR3## wherein R.sub.4 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl, and p-hydroxybenzyl.].; R.sub.3 is .[.selected from.]. hydrogen.[., chlorine, bromine, and iodine.].; [A] is .[.selected from.]. ##STR4## .[.and --CH.dbd.CH--.]. wherein R.sub.1 is .[.selected from.]. hydrogen.[.
    Type: Grant
    Filed: January 14, 1983
    Date of Patent: September 3, 1985
    Assignee: Merrell Toraude et Compagnie
    Inventors: Brian W. Metcalf, Michel Jung