Patents Represented by Attorney William H. Nicholson
  • Patent number: 5759842
    Abstract: Natural products such as equisetin and derivatives are described. These compounds are useful in the inhibition of HIV integrase.
    Type: Grant
    Filed: October 24, 1996
    Date of Patent: June 2, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Anne W. Dombrowski, Jeffrey C. Hastings, Daria Jean Hazuda, Jon David Polishook, Sheo Bux Singh
  • Patent number: 5760046
    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
  • Patent number: 5756480
    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
  • Patent number: 5753641
    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.
    Type: Grant
    Filed: April 25, 1995
    Date of Patent: May 19, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Glenn J. Gormley, Elizabeth Stoner
  • Patent number: 5741795
    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
  • Patent number: 5739137
    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
  • Patent number: 5710275
    Abstract: Described are new 7.beta.-substituted 4-aza-5.alpha.-androstan-3-ones and related compounds as 5.alpha.-reductase inhibitors.
    Type: Grant
    Filed: April 3, 1995
    Date of Patent: January 20, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Raman K. Bakshi, Gary H. Rasmusson, Richard L. Tolman, Gool F. Patel, Georgianna S. Harris, Donald W. Graham, Bruce E. Witzel
  • Patent number: 5693643
    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
  • Patent number: 5693805
    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
  • Patent number: 5599809
    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.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: February 4, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Gerard J. Hickey, Douglas J. Pettibone
  • Patent number: 5268378
    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
  • Patent number: 5266583
    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.
    Type: Grant
    Filed: September 1, 1992
    Date of Patent: November 30, 1993
    Assignee: Merck & Co., Inc.
    Inventor: Masakatsu Ohtawa
  • Patent number: 5264447
    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.
    Type: Grant
    Filed: September 1, 1992
    Date of Patent: November 23, 1993
    Assignee: Merck & Co., Inc.
    Inventor: Masakatsu Ohtawa
  • Patent number: 5264439
    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
  • Patent number: 5260322
    Abstract: A pharmaceutical composition comprising a non-peptide type angiotension II receptor antagonist is useful for the treatment of hyperuricemia.
    Type: Grant
    Filed: October 1, 1991
    Date of Patent: November 9, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Mitsuyosi Nakasima, Ikuo Ohta, Mitsutaka Kanamaru, Kazuo Kamei
  • Patent number: 5260293
    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
  • Patent number: 5260285
    Abstract: Novel substituted imidazopyridazines of formula (I) which are useful as angiotensin II antagonists, are disclosed.
    Type: Grant
    Filed: November 25, 1991
    Date of Patent: November 9, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, William J. Greenlee, Prasun K. Chakravarty, Malcolm MacCoss, Arthur A. Patchett, Thomas F. Walsh
  • Patent number: 5250558
    Abstract: Substituted triazolinone, triazolinethione, and triazolinimine compounds of formula (I) are as neurotensin II antagonists.
    Type: Grant
    Filed: January 28, 1992
    Date of Patent: October 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, Richard W. Ransom
  • Patent number: 5250521
    Abstract: Novel substituted pyrazolopyrimidines of formula (I) which are useful as angiotensin II antagonists, are disclosed.
    Type: Grant
    Filed: November 25, 1991
    Date of Patent: October 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, William J. Greenlee, Prasun K. Chakravarty, Malcolm MacCoss, Arthur A. Patchett, Thomas F. Walsh
  • Patent number: 5240938
    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