Abstract: The instant invention involves a method of treating and/or reversing androgenic alopecia and promoting hair growth, and methods of treating acne vulgaris, seborrhea, and female hirsutism, by administering to a patient in need of such treatment a 5.alpha.-reductase 2 inhibitor, such as finasteride, in a dosage amount under 5 mgs/day.
Type:
Grant
Filed:
February 14, 1996
Date of Patent:
June 2, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Glenn J. Gormley, Keith D. Kaufman, Elizabeth Stoner, Joanne Waldstreicher
Abstract: The invention concerns the treatment of hyperandrogenic conditions in humans by the formation of a novel mechanism-based irreversible inhibitor of human 5.alpha.-reductase enzymes from 3-oxo-4-oxa end 4-thiasteroids having a 1,2-double bond and the pyridine-nucleotide cofactor of the 5.alpha.-reductase enzyme, NADPH. The invention further relates to the isolated inhibitor-cofactor complex.
Type:
Grant
Filed:
October 24, 1996
Date of Patent:
May 26, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Herb G. Bull, Georgianna Harris, Robert W. Myers
Abstract: Disclosed is an improved treatment for men with benign prostatic hyperplasia (BPH), involving combination therapy of a 5.alpha.-reductase inhibitor, e.g. a 17.beta.-substituted 4-azasteroid, a 17.beta.-substituted non-azasteroid, 17.beta.-acyl-3-carboxy-androst-3,5-diene, benzoylaminophenoxybutanoic acid derivative, fused benz(thio)amide or cinnamoylamide derivative, aromatic 1,2-diethers or thioethers, aromatic ortho acylaminophenoxy alkanoic acids, ortho thioalkylacylaminophenoxy alkanoic acids, pharmaceutically acceptable salts and esters thereof, and particularly finasteride, in combination with an .alpha..sub.1 -adrenergic receptor blocker, i.e., terazosin. The combination provides therapy at the molecular level for the underlying cause of the disease as well as providing symptomatic relief. Pharmaceutical compositions useful for treatment are also disclosed.
Abstract: Compounds of the formula I ##STR1## are inhibitors of 5.alpha.-reductase, and are useful for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, prostatic carcinoma, prostatitis and benign prostatic hyperplasia.
Type:
Grant
Filed:
October 17, 1996
Date of Patent:
April 21, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Susan D. Aster, Donald W. Graham, Derek J. Von Langen
Abstract: Compounds of formula (I) are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
Type:
Grant
Filed:
February 28, 1996
Date of Patent:
April 14, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek Von Langen
Abstract: A process for the manufacture of oxytocin receptor antagonists of the following formula (I) ##STR1## and their crystalline salts is disclosed.
Type:
Grant
Filed:
September 12, 1995
Date of Patent:
December 2, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Anthony M. DeMarco, Edward J.J. Grabowski, Guo-Jie Ho, David J. Mathre, Khateeta M. Emerson, Richard F. Shuman, Paul Sohar
Abstract: Compounds of formula (I) wherein X is (a) or (b), R is Het as defined in the description. These compounds are oxytocin and vasopressin antagonists useful in the treatment of preterm labor, dysmenorrhea, and for the stoppage of labor preparatory to Cesarean delivery.
Type:
Grant
Filed:
August 15, 1995
Date of Patent:
December 2, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Kevin Gilbert, Peter D. Williams, Ben E. Evans, Doug W. Hobbs, Daniel F. Veber
Abstract: Oxytocin receptor antagonists of the formula ##STR1## wherein R.sup.12 is hydrogen, alkoxycarbonyl or unsubstituted of substituted alkyl; R.sup.13 is hydrogen, alkoxyl, aralkoxyl, alkoxycarbonyl, alkoxycarbonylamino, unsubstituted or substituted cycloalkyl, unsubstituted or substituted phenyl, unsubstituted or substituted amino, unsubstituted or substituted rings of the formulae ##STR2## unsubstituted or substituted alkyl, and the pharmaceutically acceptable salts thereof, are useful for increasing fertility rates, embryonic survival and overall reproductive efficiency in farm animals.
Abstract: A class of 2,4-dioxo-1,2,3,4-tetrahydroquinoline derivatives, substituted at the 3-position by a range of carbonyl-containing substituents or by a five- or six-membered heteroaromatic moiety, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA antagonist.
Type:
Grant
Filed:
January 22, 1992
Date of Patent:
December 7, 1993
Assignee:
Merck Sharp & Dohme, Limited
Inventors:
Raymond Baker, Paul D. Leeson, Michael Rowley, Graeme I. Sevenson
Abstract: A human urinary metabolite of Losartan has been isolated and identified as structure I. ##STR1## This compound is an active angiotensin II receptor antagonist useful in the treatment of hypertension and congestive heart failure.
Abstract: A human urinary metabolite of Losartan has been isolated and identified as Structure I: ##STR1## This compound is an active angiotensin II receptor antagonist useful in the treatment of hypertension and congestive heart failure.
Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.
Type:
Grant
Filed:
August 13, 1991
Date of Patent:
November 23, 1993
Assignee:
Merck & Co., Inc.
Inventors:
William J. Greenlee, David Hangauer, Arthur A. Patchett, Thomas F. Walsh, Kenneth J. Fitch, Daljit S. Dhanoa, Ralph A. Rivero
Abstract: The present invention provides pyrazines, pyridazines or pyrimidines, or salts or prodrugs thereof, substituted on one of the ring carbon atoms thereof with a non-aromatic azacyclic or azabicyclic ring system; and independently substituted on each of the other ring carbon atoms with a substituent of low lipophilicity or a hydrocarbon substituent; which compounds stimulate central muscarinic acetylcholine receptors and therefore are useful in the treatment of neurological and mental illnesses.
Type:
Grant
Filed:
October 10, 1991
Date of Patent:
November 9, 1993
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Raymond Baker, Leslie J. Street, John Saunders
Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.
Type:
Grant
Filed:
August 13, 1991
Date of Patent:
August 31, 1993
Assignee:
Merck & Co., Inc.
Inventors:
William J. Greenlee, Arthur A. Patchett, David Hangauer, Thomas F. Walsh, Kenneth J. Fitch, Ralph A. Rivero, Daljit S. Dhanoa