Patents Represented by Attorney Ralph R. Palo
  • Patent number: 5332732
    Abstract: Compounds of the general formula I ##STR1## wherein A is N; Ar is aryl, substituted aryl or benzofuranyl, wherein the substituents are selected from C.sub.1 -C.sub.8 alkoxy; B is CO or CH.sub.2 and HET is selected from any of piperizine, piperidine, hexahydroazepine, morpholine, thiomorpholine or pyrrolidine, which may be substituted with one of more oxo groups are disclosed as novel antipsychotic agents. Pharmaceutical compositions and methods of treating convulsions employing such compounds of formula I are also disclosed.
    Type: Grant
    Filed: September 11, 1992
    Date of Patent: July 26, 1994
    Assignee: McNeilab, Inc.
    Inventors: Malcolm K. Scott, Allen B. Reitz, Frank J. Villani, Jr., C. Royce Rasmussen
  • Patent number: 5326765
    Abstract: Novel 2,2,4-trialkyl-1,2-dihydroquinazoline-3-oxides and their synthesis are described. These compounds possess cardiotonic activity, and are useful for the treatment of heart failure.
    Type: Grant
    Filed: November 6, 1991
    Date of Patent: July 5, 1994
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Donald W. Combs, Robert Falotico, Victor Bandurco
  • Patent number: 5315012
    Abstract: Compounds of the general formula I: ##STR1## are disclosed as useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia and atherosclerosis. Novel intermediate compounds used to make the compound of formula I are also disclosed.
    Type: Grant
    Filed: September 9, 1993
    Date of Patent: May 24, 1994
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Peter J. Connolly, Michael P. Wachter
  • Patent number: 5314885
    Abstract: Compounds of the general formula I ##STR1## are disclosed as novel antipsychotic agents. Pharmaceutical compositions and methods of treating convulsions employing such compounds of formula I are also disclosed.
    Type: Grant
    Filed: September 11, 1992
    Date of Patent: May 24, 1994
    Assignee: McNeilab, Inc.
    Inventors: Malcolm K. Scott, Allen B. Reitz, Cynthia A. Maryanoff, Frank J. Villani, Jr.
  • Patent number: 5290948
    Abstract: A process for converting 1,4- and 1,5-dicarbonyl sugars to pyrrolidine and piperidine amino sugars. Novel compounds resulting from this process are also described.
    Type: Grant
    Filed: September 17, 1990
    Date of Patent: March 1, 1994
    Assignee: McNeilab, Inc.
    Inventors: Allen B. Reitz, Ellen W. Baxter, Bruce E. Maryanoff
  • Patent number: 5260458
    Abstract: The invention provides a process for preparing 1,5-diaryl pyrazole anti-inflammatory agents. A 6-aryl-4,6-dioxohexanoic acid is treated with acetic anhydride or acetyl chloride to produce an enol lactone, which is added to methylhydroxylamine to generate the dione hydroxamic acid. This dione hydroxamic acid is then treated with 4-methoxyphenylhydrazine hydrochloride to yield the 1,5-diaryl pyrazole. Novel intermediate compounds in the synthetic pathway are also disclosed.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: November 9, 1993
    Assignee: Ortho Pharmaceutical Corporation
    Inventor: William V. Murray
  • Patent number: 5258402
    Abstract: Imidate derivatives of sulfamates having the following formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and X are as herein defined have been found to be useful prodrug and exhibit anticonvulsant activity when converted to the active agent upon administration to a mammal and are thus useful in the treatment of conditions such as epilepsy. Further, the present invention encompasses pharmaceutical compositions containing a compound of formula (I) as well as methods for their use.
    Type: Grant
    Filed: June 11, 1992
    Date of Patent: November 2, 1993
    Assignee: McNeil-PPC, Inc.
    Inventor: Bruce E. Maryanoff
  • Patent number: 5252753
    Abstract: A process for producing a compound of formula I: ##STR1## comprising reacting 5-(2-fluorophenyl)-1H-tetrazole with a Grignard reagent to produce the desired product is disclosed. Novel compounds produced by this process for use as intermediates in making certain angiotension II antagonists are also disclosed.
    Type: Grant
    Filed: November 1, 1991
    Date of Patent: October 12, 1993
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Ronald Russell, William V. Murray
  • Patent number: 5250561
    Abstract: Compounds of the general formula I: ##STR1## are disclosed as useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia and atherosclerosis. Novel intermediate compounds used to make the compound of formula I are also disclosed.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: October 5, 1993
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Peter J. Connolly, Michael P. Wachter
  • Patent number: 5242940
    Abstract: N-1 and C-5 heterocyclic pyrazoles, a method of their preparation, compositions containing the same and methods of their use are disclosed. The pyrazoles are useful in alleviating inflammatory and cardiovascular disorders in mammals.
    Type: Grant
    Filed: December 17, 1991
    Date of Patent: September 7, 1993
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Michael P. Wachter, William V. Murray
  • Patent number: 5242942
    Abstract: Compounds of the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n and p are as herein defined; exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Compounds of this class are also useful for the treatment of glaucoma, peptic ulcers, hypertension, congestive heart failure and other types of edema. Furthermore, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and novel intermediates are disclosed.
    Type: Grant
    Filed: April 28, 1992
    Date of Patent: September 7, 1993
    Assignee: McNeilab, Inc.
    Inventors: Michael J. Costanzo, Bruce E. Maryanoff
  • Patent number: 5223541
    Abstract: This invention relates to a tramadol N-oxide material, enantiomers and compositions thereof and their use. The tramadol N-oxide material and compositions thereof are pharmacologically useful in treating pain, diarrhea and tussive conditions. The tramadol N-oxide is also subject to less side-effects as compared to pure opiate based compositions, such as abuse liability, tolerance, constipation and respiratory depression. Furthermore, the tramadol N-oxide material when administered orally exhibits analgesia for a longer duration than an equi-analgesic amount of tramadol.
    Type: Grant
    Filed: September 13, 1991
    Date of Patent: June 29, 1993
    Assignee: McNeilab, Inc.
    Inventors: Cynthia A. Maryanoff, Robert B. Raffa, Frank J. Villani
  • Patent number: 5134155
    Abstract: Compounds of the general formula I: ##STR1## are disclosed as useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia and atherosclerosis. Novel intermediate compounds used to make the compound of formula I are also disclosed.
    Type: Grant
    Filed: August 8, 1991
    Date of Patent: July 28, 1992
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Peter J. Connolly, Michael P. Wachter
  • Patent number: 5117054
    Abstract: The invention provides a process for preparing 1,5-diaryl pyrazole anti-inflammatory agents. A 6-aryl-4,6-dioxohexanoic acid is treated with acetic anhydride or acetyl chloride to produce an enol lactone, which is added to methylhydroxylamine to generate the dione hydroxamic acid. This dione hydroxamic acid is then treated with 4-methoxyphenylhydrazine hydrochloride to yield the 1,5-diaryl pyrazole. Novel intermediate compounds in the synthetic pathway are also disclosed.
    Type: Grant
    Filed: September 26, 1991
    Date of Patent: May 26, 1992
    Assignee: Ortho Pharmaceutical Corporation
    Inventor: William V. Murray
  • Patent number: 4960798
    Abstract: Acetylene compounds of the formula (I): ##STR1## wherein Y, R.sub.1, R.sub.2 R.sub.3, and R.sub.4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The compounds possess anti-hypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.
    Type: Grant
    Filed: January 26, 1990
    Date of Patent: October 2, 1990
    Assignee: McNeilab, Inc.
    Inventor: John R. Carson