Abstract: The present invention relates to a method of providing an antihistaminic effect in a hepatically impaired patient in need thereof comprising administering to said patient an effective antihistaminic amount of a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or hydroxy;R.sub.2 is hydrogen;or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;n is an integer of from 1 to 5;R.sub.3 is --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched;each of A and B is hydrogen or hydroxy with the proviso that at least one of A or B is hydrogen;or a pharmaceutically acceptable salt and individual isomers thereof.
Type:
Grant
Filed:
March 2, 1995
Date of Patent:
March 14, 2000
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
James K. Woodward, Richard A. Okerholm, Mark G. Eller, Bruce E. McNutt
Abstract: The invention provides a pharmaceutical composition in solid unit dosage form, comprising, a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof; and, b) at least one inert ingredient.
Type:
Grant
Filed:
October 3, 1997
Date of Patent:
January 5, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Thomas T. Ortyl, Paul F. Skultety, Kristen C. Mitchell, Deepak S. Phadke, Faraneh Attarchi, Marguerite L. Pierce, Aaron W. Schoeneman, Joseph M. Schnitz
Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
December 15, 1998
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
H. Michael Kolb, Joseph P. Burkhart, Michel J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin
Abstract: This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
Abstract: This invention relates to certain polyamine derivatives, to the methods and intermediates useful for their preparation, and to their use in treating diseases caused by infestation with a variety of parasitic protozoa.
Type:
Grant
Filed:
March 15, 1994
Date of Patent:
May 19, 1998
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
David M. Stemerick, Alan J. Bitonti, Michael L. Edwards, Peter P. McCann, Albert Sjoerdsma
Abstract: The present invention relates to a method for the treatment of patients suffering from certain neoplastic disease states which comprises administering a therapeutically effective amount of a compound of the formula: ##STR1## wherein m is an integer 6 to 9, Z is a saturated (C.sub.2 -C.sub.6) alkylene moiety, each R group independently is hydrogen, methyl, ethyl, or n-propyl except that both R groups cannot be hydrogen when Z is a straight chain; or a pharmaceutically acceptable acid addition salt thereof. Said treatment can optionally comprise conjunctive therapy with a polyamine oxidase inhibitor. The invention also relates to certain novel polyamine derivatives.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
August 5, 1997
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Nellikunja J. Prakash, David M. Stemerick, Michael L. Edwards
Abstract: This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
Type:
Grant
Filed:
December 22, 1994
Date of Patent:
April 1, 1997
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Michael L. Edwards, Donald P. Matthews, James R. McCarthy
Abstract: .alpha.-Fluoromethyl- or .alpha.-difluoromethylornithine, and certain derivatives thereof, can be used alone or in combination with cytotoxic agents for the treatment of neoplastic diseases.
Type:
Grant
Filed:
March 14, 1995
Date of Patent:
March 25, 1997
Assignee:
Marion Merrell et Compagnie C/O Merrell Pharmaceuticals Inc.
Abstract: This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
Type:
Grant
Filed:
November 1, 1994
Date of Patent:
March 4, 1997
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Donald P. Matthews, Alan J. Bitonti, Michael L. Edwards, James R. McCarthy
Abstract: The present invention provides novel aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake.
Abstract: This invention relates to certain 2,6-di-alkyl-4-silyl-phenols which are useful as inhibitors of LDL lipid peroxidation and as antiatherosclerotic agents.
Abstract: The present invention relates to novel triaryl-ethylene derivatives that are useful as anti-neoplastic agents, antiatherosclerotic agents, and hypocholesterolemic agents.
Type:
Grant
Filed:
June 15, 1994
Date of Patent:
June 11, 1996
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Donald P. Matthews, Alan J. Bitonti, William A. Van Sickle, Donald A. Kaplan
Abstract: This invention relates to certain aristeromycin/adenosine derivatives which are useful in inhibiting AdoMet-dependent transmethylation and in the treatment of patients afflicted with neoplastic or viral disease states.
Type:
Grant
Filed:
November 1, 1994
Date of Patent:
May 28, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Esa T. Jarvi, James R. McCarthy, Nellikunja J. Prakash
Abstract: The present invention relates to 4-amino-.DELTA..sup.4 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4-azido steroid with triphenylphosphine in an aqueous inert solvent with heating.
Type:
Grant
Filed:
February 25, 1994
Date of Patent:
July 25, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Philip M. Weintraub, Joseph P. Burkhart, Thomas R. Blohm
Abstract: This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
Type:
Grant
Filed:
August 27, 1993
Date of Patent:
January 3, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
James R. McCarthy, Michael L. Edwards, Donald P. Matthews
Abstract: The present invention relates to 4-amino-.DELTA..sup.4 -steroids which are inhibitors of 5.alpha.-reductase. The compounds are useful for treating DHT-mediated diseases.
Type:
Grant
Filed:
December 20, 1992
Date of Patent:
June 7, 1994
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Philip M. Weintraub, Joseph P. Burkhart, Thomas R. Blohm
Abstract: The present invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering to said patient an effective immunosuppressive amount of certain 5'-amine substituted adenosine analogs.