Patents Assigned to Hoechst-Roussel Pharmaceuticals Inc.
  • Patent number: 5550130
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 27, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5550253
    Abstract: There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl, with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 27, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: R. Richard L. Hamer, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5550254
    Abstract: There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl,with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 27, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: R. Richard L. Hamer, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5550247
    Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.
    Type: Grant
    Filed: April 20, 1995
    Date of Patent: August 27, 1996
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Harner, Brian S. Freed, Gregory H. Merriman
  • Patent number: 5547977
    Abstract: There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl, with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.
    Type: Grant
    Filed: October 16, 1992
    Date of Patent: August 20, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Richard L. Hamer, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5543427
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: August 24, 1994
    Date of Patent: August 6, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
  • Patent number: 5541340
    Abstract: There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl,with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 30, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Richard L. Hamer, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5541216
    Abstract: There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl,with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.
    Type: Grant
    Filed: October 28, 1992
    Date of Patent: July 30, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Richard L. Hamer, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5534636
    Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.
    Type: Grant
    Filed: April 21, 1995
    Date of Patent: July 9, 1996
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
  • Patent number: 5534640
    Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.
    Type: Grant
    Filed: April 21, 1995
    Date of Patent: July 9, 1996
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
  • Patent number: 5519062
    Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.
    Type: Grant
    Filed: May 23, 1994
    Date of Patent: May 21, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
  • Patent number: 5504084
    Abstract: Pharmaceutical for the treatment of skin disordersA compound of the formula I or II ##STR1## and physiologically tolerable salts of compound of the formula II are suitable for treatment of psoriasis.
    Type: Grant
    Filed: March 23, 1994
    Date of Patent: April 2, 1996
    Assignees: Hoechst Aktiengesellschaft, Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Robert R. Bartlett, Klaus U. Weithmann, Ellen S. Kurtz
  • Patent number: 5502203
    Abstract: Novel 9-aminotetrahydroacridines and related compounds, intermediates and processes for the preparation thereof, and a method of relieving memory dysfunction are disclosed.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: March 26, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer
  • Patent number: 5500423
    Abstract: Novel 5,6-dihydro-4H-imidazo[4,5,1-ij]quinolines, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: September 9, 1994
    Date of Patent: March 19, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, Brian S. Freed
  • Patent number: 5488063
    Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.
    Type: Grant
    Filed: May 23, 1994
    Date of Patent: January 30, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Harmer, Brian S. Freed, Gregory H. Merriman
  • Patent number: 5488061
    Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.
    Type: Grant
    Filed: May 23, 1994
    Date of Patent: January 30, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Harmer, Brian S. Freed, Gregory H. Merriman
  • Patent number: 5482970
    Abstract: Novel compositions comprising an antiandrogenic compound of the formula ##STR1## wherein R is COR.sub.1 wherein R.sub.1 is loweralkyl and a vehicle comprising a metabolism modulator and a polar organic solvent, and a method of controlling the membrane permeation and metabolism of the compound thereof are disclosed.
    Type: Grant
    Filed: September 17, 1993
    Date of Patent: January 9, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Kwon H. Kim, Barry Koplowitz, Norman L. Henderson
  • Patent number: 5464846
    Abstract: This application is a continuation-in-part of pending U.S. patent application Ser. No. 388,437, filed Aug. 2, 1989.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 or 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.
    Type: Grant
    Filed: May 13, 1994
    Date of Patent: November 7, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Richard C. Effland, David G. Wettlaufer
  • Patent number: 5459274
    Abstract: The synthesis of memory enhancing, analgetic, and antidepressant N-alkyl-N-pyridinyl-1H-indol-1-amines is described.
    Type: Grant
    Filed: May 13, 1994
    Date of Patent: October 17, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Thomas B. Lee, Keith E. Goehring
  • Patent number: 5455245
    Abstract: This invention relates to compounds of the formula ##STR1## where R.sub.1 -R.sub.6, X and Y are as defined in the specification, which are useful for the treatment of various memory dysfunctions characterized by a cholinergic deficit and thus may be indicated in the treatment of Alzheimer's disease.
    Type: Grant
    Filed: May 25, 1994
    Date of Patent: October 3, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Larry Davis, Gordon E. Olsen