Patents Assigned to Hoechst Roussel Pharmaceuticals Incorporated
  • Patent number: 5155226
    Abstract: A method of preparing 9-amino-1,2,3,4-tetrahydroacridine by the reaction of 2-aminobenzonitrile and cyclohexanone with p-toluenesulfonic acid monohydrate in xylenes is disclosed.
    Type: Grant
    Filed: February 19, 1991
    Date of Patent: October 13, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Thomas B. K. Lee, Keith E. Goehring
  • Patent number: 5153193
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters R.sub.1 and R.sub.2 are as defined in the specification, which compounds are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.
    Type: Grant
    Filed: October 1, 1991
    Date of Patent: October 6, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Denise M. Flanagan, Lawrence L. Martin
  • Patent number: 5149813
    Abstract: There are described compounds of the formula, ##STR1## where X is hydrogen, loweralkyl, loweralkoxy or halogen;R when present is hydrogen, loweralkyl or arylloweralkyl;R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; andR.sub.2 when present is hydrogen or loweralkyl;which compounds are useful for alleviating various memory dysfunctions characterized by a decreased cholinergic function such Alzheimer's disease.
    Type: Grant
    Filed: March 27, 1992
    Date of Patent: September 22, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Lawrence L. Martin, Joseph F. Payack, Helen H. Ong
  • Patent number: 5145844
    Abstract: Novel hydroxy-,alkoxy-and benzyloxy-substituted phospholipids, a process for the preparation thereof, and methods for treating pain, phospholipase A.sub.2 mediated inflammation and similar conditions utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: March 5, 1991
    Date of Patent: September 8, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: John J. Tegeler, Kirk D. Shoger
  • Patent number: 5145866
    Abstract: A method of treating anxiety with the aid of R(+)-3-amino-1-hydroxypyrrolidin-2-one of the formula ##STR1## is disclosed.
    Type: Grant
    Filed: April 22, 1991
    Date of Patent: September 8, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Robert W. Dunn, Roy Corbett
  • Patent number: 5145965
    Abstract: Novel 2,6-methanopyrrolo-3-benzazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: March 11, 1991
    Date of Patent: September 8, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Allen, David G. Wettlaufer
  • Patent number: 5134236
    Abstract: Novel 1-phenyl-3-(1-piperazinyl)-1H-indazoles, intermediates and processes for the preparation thereof, and methods for alleviating pain, treating convulsions, and treating depression utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: September 28, 1990
    Date of Patent: July 28, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventor: Joseph T. Strupczewski
  • Patent number: 5114936
    Abstract: This invention relates to 6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-ones and -ols of the formula ##STR1## wherein X is (Y) ##STR2## or loweralkyl; Y is hydrogen, halogen, loweralkyl, loweralkoxy, trifluoromethyl, nitro or amino; R is H when the bond between the oxygen atom and the carbon atom in question is a single bond; otherwise the dotted line signifies part of a double bond to the oxygen atom; R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl or arylloweralkyl, or R.sub.2 and R.sub.3 taken together with the nitogen atom form an optionally substituted heterocycle selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, imidazol-1-yl, 1-piperazinyl, said substituents being hydrogen or loweralkyl; 4-substituted-1-piperazinyl of the formula ##STR3## where R.sub.
    Type: Grant
    Filed: April 26, 1991
    Date of Patent: May 19, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: David G. Wettlaufer, Gregory M. Shutske, Peter A. Nemoto
  • Patent number: 5109011
    Abstract: This invention relates to p-acylaminophenoxycarbamates having the formula ##STR1## where R.sub.1 and R.sub.2 are each independently hydrogen, loweralkyl, aryl and arylloweralkyl; R.sub.3 is hydrogen, loweralkyl, aryllowerallkyl; R.sub.4 is hydrogen, loweralkyl, formyl, alkylcarbonyl, arylloweralkyl, phenylcarbonyl, arylloweralkylcarbonyl, substituted phenylcarbonyl, pyridylcarbonyl, and substituted pyridylcarbonyl with the proviso that if R.sub.4 contains a carbonyl group directly attached to the oxygen of the N-O moiety, R.sub.3 cannot by hydrogen; or R.sub.3 and R.sub.4 taken together form a heterocyclic ring selected from the group consisting of imidazole or loweralkylimidazole; X is hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; and p is an integer selected from 0 and 1; the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and stereoisomers and racemic mixtures thereof.
    Type: Grant
    Filed: July 30, 1990
    Date of Patent: April 28, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Allen, Raymond W. Kosley, Jr., Bettina Spahl
  • Patent number: 5081117
    Abstract: This invention relates to 4- and 6-carbamates related to physostigmine of the formula ##STR1## where R.sub.1 is alkyl, cycloalkyl, bicycloalkyl, aryl or arylloweralkyl; R.sub.2 is hydrogen or alkyl or the group --NR.sub.1 R.sub.2 taken together forms a monocyclic or bicyclic ring of 5 to 12 carbons; m is 0,1, or 2; each X is independently hydrogen, halogen, loweralkyl, nitro or amino; and the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. This invention also relates to novel intermediates useful in the preparation of the 4- and 6-carbamates. The compounds of this invention display utility for alleviating various memory dysfunctions characterized by a decreased cholinergic function, such as Alzheimer's disease.
    Type: Grant
    Filed: November 3, 1989
    Date of Patent: January 14, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Edward J. Glamkowski, Barbara E. Kurys
  • Patent number: 5078280
    Abstract: An improvement in a mechanic's creeper whereby a Z-shaped shelf member with a powerful magnet is attached to an edge of the creeper. The shelf member with its magnet holds tools in such a way that the tools can be readily accessible to the mechanic.
    Type: Grant
    Filed: March 22, 1991
    Date of Patent: January 7, 1992
    Assignee: Hoechst-Roussel Pharmaceutical Incorporated
    Inventor: Ryan C. Nordeen
  • Patent number: 5077405
    Abstract: This invention relates to 3-(1-substituted-4-piperazinyl)-1H-indazoles having the following formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, arylloweralkyl, acyl, cycloalkylloweralkylene, and phenylsulfonyl; and R.sub.2 is hydrogen, lower alkyl, hydroxyloweralkyl of the formula -(loweralkylene)-OH, arylloweralkyl, acyl, cycloalkylloweralkylene, ##STR2## where Z is selected from hydrogen, halogen, loweralkoxy, CF.sub.3, NO.sub.2, and NH.sub.2 ; ##STR3## where Z is as defined above; ##STR4## where Z is as defined above; ##STR5## where R.sub.3 and R.sub.4 are each independently hydrogen and loweralkyl; ##STR6## where Z is as defined above; ##STR7## where R' and R" are each independently hydrogen and loweralkyl; X is hydrogen, loweralkyl, hydroxyl, halogen, loweralkoxy, CF.sub.3, NO.sub.2 and amino; n is an integer of 1 to 4, with the further proviso that R.sub.2 is not loweralkyl when R.sub.
    Type: Grant
    Filed: May 21, 1990
    Date of Patent: December 31, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
  • Patent number: 5055476
    Abstract: This invention relates to 3-(1,2-benzisoxazol-3-yl)-4-pyridinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, arylalkyl or acyl; R.sub.2 is hydrogen, loweralkyl or arylalkyl, X is hydrogen, halogen, nitro or amino; or the pharmaceutically acceptable addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention are useful as analgesics, for alleviating various memory dysfunctions characterized by a decreased cholinergic function, as cognition enhancers in the treatment of senile dementia such as Alzheimer's disease and as topical antiinflammatory agents for the treatment of various dermatoses.
    Type: Grant
    Filed: August 13, 1990
    Date of Patent: October 8, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Joseph T. Klein
  • Patent number: 5053513
    Abstract: A method of reducing a carbonyl containing acridine of the formula ##STR1## where n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, trifluoromethyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl and R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl, is disclosed.
    Type: Grant
    Filed: March 29, 1990
    Date of Patent: October 1, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Thomas B. K. Lee, George E. Lee, George S. K. Wong, Donna M. Borek, Keith E. Goehring
  • Patent number: 5053511
    Abstract: This invention relates to 1,3-dihydro-1-(pyridinylamino)-2H-indol-2-ones of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; or R.sub.2 and R.sub.3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl cycloalkane or heterocycloalkyl selected from the group consisting of piperidine and tetrahydropyran; X and Y are independently hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m and n are independently integers of 1 to 3, the pharmaceutically acceptable acid addition salts thereof and, where applicable the optical, geometrical and stereoisomers and racemic mixtures thereof. The compounds of this invention display utility as analgesics, anticonvulsants, for enhancing memory and for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: June 11, 1990
    Date of Patent: October 1, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, David G. Wettlaufer
  • Patent number: 5051430
    Abstract: This invention relates to 3-(1H-indazol-3-yl)-4-pyridinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, arylalkyl or acyl; R.sub.2 is hydrogen, loweralkyl or arylalkyl; R.sub.3 is hydrogen, loweralkyl or aryl and X is hydrogen, halogen, nitro or amino or the pharmaceutically acceptable addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention are useful as analgesics and as topical antiinflammatory agents for the treatment of various dermatoses.
    Type: Grant
    Filed: September 10, 1990
    Date of Patent: September 24, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Joseph T. Klein
  • Patent number: 5041445
    Abstract: This invention relates to 3-[1-thiazolidinylbutyl-4-piperazinyl]-1H-indazoles of the formula ##STR1## where R.sub.1 and R.sub.2 are each independently hydrogen or loweralkyl or R.sub.1 and R.sub.2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane or cycloheptane ring; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane or cycloheptane ring; R.sub.5 is hydrogen, loweralkyl, alkanoyl or aroyl; X is hydrogen, halogen, loweralkyl or alkoxy; m is an integer of 1 to 3, the pharmaceutically acceptable acid addition salts thereof and where applicable, the optical, geometrical and stereoisomers and racemic mixtures thereof. The compounds of this invention are useful as antipsychotic agents.
    Type: Grant
    Filed: May 21, 1990
    Date of Patent: August 20, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Nicholas J. Hrib, Joseph T. Strupczewski, John G. Jurcak, Kenneth Bordeau
  • Patent number: 5037985
    Abstract: Novel 2,6-methanopyrrolo-3-benzazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: February 22, 1990
    Date of Patent: August 6, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Allen, David G. Wettlaufer
  • Patent number: 5036152
    Abstract: Novel alkoxycarbonylalkylphospholipids, alkylaminocarbonylalkylphospholipids, processes for the preparation thereof, and methods for treating inflammation utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: September 5, 1989
    Date of Patent: July 30, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Nicholas J. Hrib, Kirk D. Shoger, John J. Tegeler
  • Patent number: 5034392
    Abstract: This invention relates to compounds of the formula ##STR1## where R.sub.1 and R.sub.2 are independently hydrogen or loweralkyl or R.sub.1 and R.sub.2 taken together with the carbon atom to which they are attached form a spiro-fused cycloalkane of 5 to 8 carbons; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a spiro-fused cycloalkane of 5 to 8 carbons; R.sub.5 and R.sub.6 taken together with the nitrogen atom to which they are attached are ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, amino, cyano, trifluoromethyl or methoxy; and m is 0, 1 or 2; the pharmaceutically acceptable acid addition salts thereof and where applicable the optical and geometrical isomers and racemic mixtures thereof. The compounds of this invention are useful as analgesic and antihypertensive agents.
    Type: Grant
    Filed: April 16, 1990
    Date of Patent: July 23, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventor: Nicholas J. Hrib