Patents Represented by Attorney Jerome Rosenstock
  • Patent number: 4812450
    Abstract: This invention relates to spiro-[(piperidine-, pyrrolidine-, or -hexahyroazepinyl substituted) pyrrolo[2,1-c][1,4]-benzoxazepines] having the following formula ##STR1## wherein R is hydrogen, lower alkyl, arylloweralkyl, acyl, lower alkenyl, lower alkynyl, and loweralkylbenzisoxazole; X is hydrogen, halogen, loweralkoxy, and trifluoromethyl; Y is hydrogen; 2' or 3' acyl, formyl, carbinol of the formula ##STR2## wherein R.sub.1 and R.sub.2 are the same or different and are independently hydrogen, loweralkyl, arylloweralkyl, aryl, loweralkenyl, lower alkynyl and lower alkylbenzisoxazole; loweralkyl, loweralkenyl and halogen; and n is an integer of 1 to 3. The compounds of this invention display utility as analgesic and antihypertensive agents.
    Type: Grant
    Filed: July 30, 1987
    Date of Patent: March 14, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples
  • Patent number: 4794181
    Abstract: The invention relates to 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines of the formula ##STR1## wherein Y is the same of different and is hydrogen and lower alkoxy; X is hydrogen, halogen, lower alkyl, lower alkoxy, CF.sub.3, NO.sub.2, CN and NH.sub.2 ; R is hydrogen, lower alkyl, cycloalkyllower alkyl, ##STR2## Ar lower alkyl of the formula ##STR3## where Z is hydrogen, lower alkyl, lower alkoxy, halogen CF.sub.3, NO.sub.2 and NH.sub.2 ; Aryloxy lower alkyl of the formula ##STR4## where Z is as previously defined; and an alkylene amine of the formula ##STR5## where R.sub.1 and R.sub.2 are the same or different and are hydrogen and lower alkyl, n is an integer of 1 or 2; and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: January 16, 1986
    Date of Patent: December 27, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Larry Davis
  • Patent number: 4758668
    Abstract: Novel 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles, intermediates and processes for the preparation thereof, and methods for treating pyschoses, treating depression, alleviating pain, treating convulsions and treating hypertension utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: September 30, 1987
    Date of Patent: July 19, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Joseph T. Strupczewski
  • Patent number: 4751238
    Abstract: This invention relates to substituted alkyl amine derivatives of 6,11-dihydro-11-oxodibenz[b,e]oxepins of the formula: ##STR1## where X is hydrogen, halogen, lower alkoxy, lower alkyl, nitro, hydroxyl and CF.sub.3 ; R is H, and lower alkyl, R.sub.1 is CH.sub.3 SO.sub.3 and ##STR2## where R.sub.2 and R.sub.3 are the same of different and are hydrogen, lower alkyl, mesyl (CH.sub.3 SO.sub.2 --), and cycloalkyl loweralkyl; ##STR3## and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: June 18, 1986
    Date of Patent: June 14, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Lawrence L. Martin, Linda L. Setescak
  • Patent number: 4710573
    Abstract: Novel 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles, intermediates and processes for the preparation thereof, and methods for treating psychoses, treating depression, alleviating pain, treating convulsions and treating hypertension utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: March 19, 1987
    Date of Patent: December 1, 1987
    Assignee: Hoechst Roussel Pharmaceuticals, Inc.
    Inventor: Joseph T. Strupczewski
  • Patent number: 4670447
    Abstract: Novel 3-(piperidinyl- and 3-(pyrrolidinyl)-1H-indazoles, intermediates and processes for the preparation thereof, and methods for treating psychoses, treating depression, alleviating pain, treating convulsions and treating hypertension utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: December 19, 1985
    Date of Patent: June 2, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Joseph T. Strupczewski
  • Patent number: 4668690
    Abstract: This invention relates to 1,2,3,4,4a,9b-hexahydro-4a-aminoalkyldibenzofurans of the formula ##STR1## where X is hydrogen, loweralkyl, F and Cl; R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl, loweralkoxyloweralkyl, aryloxyloweralkyl, cycloalkylloweralkyl and heteroarylloweralkyl: R.sub.2 is hydrogen, lower alkyl or R.sub.1 and R.sub.2 taken together with the N ring atom constitute a saturated or unsaturated heterocyclic ring having 5 or 6 members; R.sub.3 is hydrogen, lower alkyl; n is an interger of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and where applicable the stereo, optical and geometrical isomers of the foregoing.
    Type: Grant
    Filed: December 30, 1985
    Date of Patent: May 26, 1987
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventor: Gregory M. Shutske
  • Patent number: 4645737
    Abstract: A method for the determination of anti-treponemal antibody in a test sample comprises contacting a substrate for the anti-treponemal antibody with sample; treating the contacted substrate with labeled antihuman Ig antibody selected from (a) a mixture comprising enzyme labeled antihuman Ig antibody and fluorescent labeled antihuman Ig antibody, (b) antihuman Ig antibody labeled with an enzyme and a fluorescent label, and (c) fluorescent labeled antihuman Ig antibody to which enzyme labeled antibody against the animal species from which the antibody used in the fluorescent labeled antibody was derived is added subsequently, and (d) enzyme labeled antihuman Ig antibody to which fluorescent labeled antibody against the animal species from which the antibody used in the enzyme labeled antibody was derived is subsequently added; determining the enzyme activity of the treated substrate; and determining the immunofluorescent patterns in substrates exhibiting enzyme activity.
    Type: Grant
    Filed: March 5, 1984
    Date of Patent: February 24, 1987
    Assignee: American Hoechst Corporation
    Inventors: Stephen R. Coates, Walter L. Binder
  • Patent number: 4594435
    Abstract: 2'-substituted-spiro[benzofuran-2(3H),1'-cycloalkanes] and methods of preparing same are described. On the aromatic portion of the benzofuran ring, there may be a substituent or substituents including halogen, amino, lower-alkyl-substituted amino, lower alkyl, lower alkoxy, hydroxy and nitro. The substituents at the 2-position of the cycloalkane ring are --(CH.sub.2).sub.n NR.sup.1 R.sup.2 where n is 0, 1 or 2 and R.sup.1 and R.sup.2 are each independently hydrogen and alkyl or 1-3 carbons. These compounds are useful as antidepressants and analgesics.Various other compounds which are useful as intermediates for preparing the aforementioned compounds and methods for preparing same are also described.
    Type: Grant
    Filed: February 28, 1985
    Date of Patent: June 10, 1986
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Michael C. Jones, deceased
  • Patent number: 4585779
    Abstract: cis-4a-Aryl-1,2,3,4,4a,9b-hexahydro-benzofuro[3,2-c]pyridines and methods of preparing same are described. On the nitrogen atom there may be a substituent including loweralkyl, loweralkenyl, phenylloweralkyl, hydrogen cyanoloweralkyl, phenylcarbonylloweralkyl, phenoxyloweralkyl and cycloalkylloweralkyl. The 4a-aryl group may be a phenyl, mono-halogen substituted phenyl, tolyl, methoxyphenyl, hydroxyphenyl, or furyl. These compounds are useful as analgesic and anticonvulsant agents.3-o-Fluorophenyl-1-methyl-4-aryl-4-piperidinols which are useful as intermediates for preparing the aforementioned compounds and methods for preparing same are also described.
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: April 29, 1986
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Solomon S. Klioze
  • Patent number: 4578394
    Abstract: This invention relates to 1,4 dihydropyridines having the following formula ##STR1## wherein R is loweralkyl or Arloweralkyl; R.sub.1, R.sub.2 and R.sub.3 may be the same or different and are hydrogen, loweralkyl or halogen; X is hydrogen, NH.sub.2, ##STR2## and R.sub.4 is hydrogen or loweralkyl. The compounds of this invention display utility in the treatment of Alzheimer's disease and related cognitive disorders characterized by centrally deficient cholinergic function.
    Type: Grant
    Filed: December 10, 1984
    Date of Patent: March 25, 1986
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Allen, Richard C. Effland, Joseph T. Klein
  • Patent number: 4576960
    Abstract: This invention relates to 6,11-dihydro-11-oxo-dibenz[b, e]oxepin derivatives of the formula ##STR1## where Y is hydrogen, alkyl, alkoxy, halogen and trifluoromethyl, n is 0, 1, 2 or 3; R.sub.9 is hydrogen and alkyl; R is ##STR2## where Hal is a halogen; ##STR3## where R.sub.10 is hydrogen, alkyl and benzyl of the formula ##STR4## where Z is hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, and amino; where n is 0, 1, 2 or 3; p is 1 or 2; q is 0, 1 or 2; R.sub.1 to R.sub.7 are the same or different and are hydrogen and alkyl; and R.sub.8 is hydrogen, alkyl and phenyl; and R.sub.9 is hydrogen and alkyl, and where appropriate pharmaceutically acceptable acid or base addition salts thereof.
    Type: Grant
    Filed: April 4, 1983
    Date of Patent: March 18, 1986
    Assignee: Hoechst Roussel Pharmaceuticals Incorporated
    Inventors: Lawrence L. Martin, Linda L. Setescak
  • Patent number: 4551474
    Abstract: This invention relates to 4-aryloxy-1,2,3,4-tetrahydroisoquinolines of the formula ##STR1## where Y is hydrogen and alkoxy; X is hydrogen, cyano, benzoyl, trifluoromethyl, phenyl, halogen, alkyl alkoxy and nitro; R is hydrogen and alkyl; R.sub.1 is hydrogen, alkyl, aralkyl, ##STR2## and CO.sub.2 R.sub.4 where R.sub.1 is aryl and alkyl; R.sub.2 and R.sub.3 are the same or differnt and are hydrogen and alkyl or R.sub.2 and R.sub.3 are fused together to form a pyrrolidino or a piperidino ring substituent; and m is an integer of 1 or 2; n is an integer of 2 or 3; and a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: August 9, 1984
    Date of Patent: November 5, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Larry Davis, Joseph T. Klein
  • Patent number: 4544745
    Abstract: Cis-4a-aryl, 1, 2, 3, 4, 4A, 9B-hexahydro-benzofuro-[3,2-C]- pyridines, useful as analgesic and anticonvulsant agents are described.
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: October 1, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Solomon S. Klioze
  • Patent number: 4532333
    Abstract: The invention relates to 1-(aminoalkylphenyl and aminoalkylbenzyl)indoles and indolines of the formula: ##STR1## where R.sub.1 and R.sub.2 are the same or different and are hydrogen, lower alkyl, cycloalkyl and acyl of the formula ##STR2## where R.sub.3 is lower alkyl, lower alkoxy, cycloalkyl, phenyl of the formula ##STR3## and Ar lower alkyl of the formula -lower alkylene ##STR4## X is hydrogen, halogen, lower alkoxy, Ar lower alkoxy of the formula ##STR5## lower alkylene --O--; m and p are independently integers of 0 and 1 and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: August 6, 1984
    Date of Patent: July 30, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, James M. Fortunato
  • Patent number: 4526891
    Abstract: This invention relates to compounds of the formula: ##STR1## where X is hydrogen, halogen, lower alkoxy, lower alkyl, nitro, hydroxyl and CF.sub.3 ; R is H, and lower alkyl, R.sub.1 is CH.sub.3 SO.sub.3 and ##STR2## where R.sub.2 and R.sub.3 are the same or different and are hydrogen, lower alkyl, mesyl (CH.sub.3 SO.sub.
    Type: Grant
    Filed: March 10, 1983
    Date of Patent: July 2, 1985
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Linda L. Setescak
  • Patent number: 4517311
    Abstract: 2'-Substituted-spiro[benzofuran-2(3H),1'-cycloalkanes] and methods of praparing same are described. On the aromatic portion of the benzofuran ring, there may be a substituent or substituents including halogen, amino, lower-alkyl-substituted amino, lower alkyl, lower alkoxy, hydroxy and nitro. The substituents at the 2-position of the cycloalkane ring are --(CH.sub.2).sub.n NR.sup.1 R.sup.2 where n is 0, 1 or 2 and R.sup.1 and R.sup.2 are each independently hydrogen and alkyl of 1-3 carbons. These compounds are useful as antidepressants and analgesics.Various other compounds which are useful as intermediates for preparing the aforementioned compounds and methods for preparing same are also described.
    Type: Grant
    Filed: September 13, 1982
    Date of Patent: May 14, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, Michael C. Jones, deceased, by Herbert Jones, administrator
  • Patent number: 4515946
    Abstract: This invention relates to 6,11-dihydro-11-oxo-dibenz[b,e]oxepin derivatives of the formula ##STR1## where Y is alkyl, alkoxy, halogen or trifluoromethyl, n is 0, 1, 2 or 3; R is ##STR2## where Hal is a halogen; ##STR3## where n is 0, 1, 2 or 3; p is 1 or 2; q is 0, 1, or 2; R.sup.1 to R.sup.7 are the same or different and are hydrogen and alkyl and R.sup.8 is hydrogen, alkyl and phenyl; and R.sup.9 is alkyl and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: December 23, 1981
    Date of Patent: May 7, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Linda L. Setescak
  • Patent number: 4514411
    Abstract: This invention relates to substituted 4,10-dihydro-10-oxothieno benzoxepins of the formula, ##STR1## where R is hydrogen and lower alkyl; R.sub.1 is ##STR2## where R.sub.2 is hydrogen, lower alkyl and benzyl of the formula ##STR3## where X is hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl, nitro, and amino; ##STR4## where R.sub.3 and R.sub.4 are the same or different and are hydrogen and lower alkyl; ##STR5## where R.sub.5 and R.sub.6 are the same or different and are lower alkyl; and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: August 10, 1984
    Date of Patent: April 30, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Linda L. Setescak
  • Patent number: 4487934
    Abstract: A method of preparing substituted acylbenzenes is disclosed. The method comprises reacting selected acylhalides or equivalents with a selected poly-substituted benzene in the presence of an acylating catalyst comprising a perfluoro sulfonic acid polymer.
    Type: Grant
    Filed: June 6, 1980
    Date of Patent: December 11, 1984
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Linda L. Setescak