Patents Represented by Attorney, Agent or Law Firm David L. Rose
  • Patent number: 6080876
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: September 17, 1998
    Date of Patent: June 27, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Ilias Dorziotis, Ioannis Houpis, Kan K. Eng
  • Patent number: 6077849
    Abstract: Compounds of formula I: ##STR1## as well as tautomers, pharmaceutically acceptable salts, hydrates, prodrugs and reduced forms are disclosed. The compounds are useful for the treatment and prevention of diabetes mellitus, and in particular, for the treatment or prevention of hyperglycemia in diabetic patients.
    Type: Grant
    Filed: March 29, 1999
    Date of Patent: June 20, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Kun Liu, Harold B. Wood, Anthony B. Jones, Bei Zhang
  • Patent number: 6071928
    Abstract: The present invention relates to compounds of formula (I), wherein R is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, which groups are optionally substituted by hydroxy, C.sub.1-4 alkoxy or NR.sup.a R.sup.b, where R.sup.a and R.sup.b each independently repesent hydrogen or C.sub.1-4 alkyl; or R is C.sub.1-4 alkyl substituted by Ar, and optionally further substituted by one or both of R.sup.4 and R.sup.5 ; R.sup.1, R.sup.2 and R.sup.3 represent a variety of substituents; R.sup.9 and R.sup.10 are each hydrogen, halogen, C.sub.1-6 alkyl, CH.sub.2 OR.sup.c, oxo, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b where R.sup.c represents hydrogen, C.sub.1-6 alkyl or phenyl; X is --CH.sub.2, or --CH.sub.2 CH.sub.2 --; Y is --CH--, --CH.sub.2 --, --CH.sub.2 CH-- or --CH.sub.2 CH.sub.2 --, with the proviso that the sum total of carbon atoms in X+Y is 2 or 3; and when Y is --CH-- or --CH.sub.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: June 6, 2000
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Neil Roy Curtis, Ian Thomas Huscroft, Janusz Jozef Kulagowski, Christopher John Swain
  • Patent number: 6071954
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: March 13, 1998
    Date of Patent: June 6, 2000
    Assignee: Merk Frosst Canada, Inc.
    Inventors: Yves LeBlanc, Patrick Roy, Serge Leger, Erich Grimm, Zhaoyin Wang
  • Patent number: 6071927
    Abstract: The present invention relates to certain spiro-piperdine derivatives which are tachykinnin antagonists and are useful, for example, in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: June 6, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Patent number: 6071936
    Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: May 17, 1999
    Date of Patent: June 6, 2000
    Assignee: Merck Frosst Canada & Co.
    Inventors: Daniel Dube, Rejean Fortin, Richard Friesen, Zhaoyin Wang, Jacques Yves Gauthier
  • Patent number: 6071909
    Abstract: The present patent application discloses compounds having formula (I) ##STR1## or a pharmaceutically acceptable salt thereof or an oxide thereof, wherein R.sup.3 is (II), ##STR2## wherein A, B and D each is CH, or one or two of A, B and D is N and the others are CH; R.sub.11 is phenyl, benzimidazolyl, or monocyclic heteroaryl all of which may be substituted one or more times with substituents selected from alkyl, alkoxy, phenyl, halogen, CF.sub.3, amino, nitro, cyano, acyl, acylamino, phenyl and monocyclic heteroaryl; and one of R.sup.6 and R.sup.7 is hydrogen and the other is furanyl or isoxazolyl each of which may be substituted one or more times with substituents selected from halogen, alkyl, alkoxy and phenyl. The compounds are useful for the treatment of various central nervous system disorders such as epilepsy and other convulsive disorders, anxiety, sleep disorders and memory disorders.
    Type: Grant
    Filed: July 20, 1999
    Date of Patent: June 6, 2000
    Assignee: Merck Sharpe & Dohme Ltd.
    Inventors: Timothy Harrison, Timothy Jason Sparey, Martin Richard Teall
  • Patent number: 6069163
    Abstract: Azapeptide acids of Formula I are antagonists of VLA-4 and/or .alpha..sub.4 .beta..sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
    Type: Grant
    Filed: October 16, 1998
    Date of Patent: May 30, 2000
    Assignee: Merck & Co., Inc.
    Inventor: Stephen E. Delaszlo
  • Patent number: 6068987
    Abstract: Histone deacetylase inhibition provides a target for identifying potential antiprotozoal compounds. Histone deacetylase inhibitors are useful as therapeutic agents against protozoal infections.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: May 30, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Paula M. Dulski, Robert W. Myers, Anne M. Gurnett, Sandra J. Rattray, Dennis M. Schmatz
  • Patent number: 6063811
    Abstract: This application relates to a method of treating a disease susceptible to treatment with a non-steroidal anti-inflammatory drug by administering to a patient once daily an effective amount of 3-phenyl-4-(4-methylsulfonyl)phenyl)-2-(5H)-furanone.
    Type: Grant
    Filed: March 8, 1999
    Date of Patent: May 16, 2000
    Assignees: Merck & Co., Inc., Merch Frosst Canada & Co.
    Inventors: Bruno Hancock, Conrad Winters, Barry Gertz, Elliot Ehrich
  • Patent number: 6063950
    Abstract: The present invention is directed to a process for the preparation of titanocene dichloride (Cp.sub.2 TiCl.sub.2) from the titanocene dimer (Cp.sub.2 TiMe).sub.2 O), which is produced as a by-product from employing the reagent dimethyl titanocene (Cp.sub.2 Ti(CH.sub.3).sub.2) in the methylenation of carbonyl compounds, such as esters and lactones.
    Type: Grant
    Filed: October 28, 1999
    Date of Patent: May 16, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark Huffman, Joseph Payack
  • Patent number: 6063783
    Abstract: A class of substituted 7,8-ring fused 1,2,4-triazolo[4,3-b]pyridazine derivatives as shown in Formula I, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and a substituted alkoxy moiety at the 6-position, are selective ligands for GABA.sub.A receptors, in particular having high affinity for the .alpha.2 and/or .alpha.3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of pain.
    Type: Grant
    Filed: December 10, 1998
    Date of Patent: May 16, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Raymond George Hill
  • Patent number: 6063796
    Abstract: This invention relates to somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. Compounds of the formula: ##STR1## including pharmaceutically acceptable salts and hydrates thereof are disclosed. These compounds are useful in the treatment of diabetes, cancer, acromegaly, restenosis, depression, irritable bowel syndrome, pain and diabetic retinopathy. Many of the compounds are also orally active.
    Type: Grant
    Filed: April 1, 1998
    Date of Patent: May 16, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lihu Yang, Arthur A. Patchett, Alexander Pasternak, Scott Berk, Meng Hsin Chen, David Johnston, Kevin Chapman, Ravi Nargund, James R. Tata, Liangqin Guo
  • Patent number: 6060469
    Abstract: The present invention relates to compounds of formula (I), ##STR1## wherein R.sup.1 represents halogen, hydroxy, C.sub.1-6 alkyl group optionally substituted by one or three fluorine atoms, C.sub.1-6 alkoxy group optionally substituted by one to three fluorine atoms, or C.sub.1-6 alkylthio optionally substituted by one to three fluorine atoms; R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or when R.sup.2 is adjacent to R.sup.1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R.sup.3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; m is 0-3 and n is 0-3, with the proviso that the sum total of m+n is 2 or 3; p is zero or 1; q is 1 or 2; and when m is 1 and n is 1 or 2, the broken line represents an optional double bond; R.sup.4, R.sup.5, R.sup.6, R.sup.9 and R.sup.
    Type: Grant
    Filed: May 18, 1998
    Date of Patent: May 9, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Timothy Harrison, Christopher John Swain, Brian John Williams
  • Patent number: 6057338
    Abstract: This invention relates to somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. Compounds of the formula: ##STR1## including pharmaceutically acceptable salts and hydrates thereof are disclosed. These compounds are useful in the treatment of diabetes, cancer, acromegaly, restenosis, depression, irritable bowel syndrome, pain and diabetic retinopathy. Many of the compounds are also orally active.
    Type: Grant
    Filed: April 1, 1998
    Date of Patent: May 2, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lihu Yang, Arthur A. Patchett, Alexander Pasternak, Scott Berk
  • Patent number: 6057319
    Abstract: The invention encompasses the novel compound of formula (I) useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of formula (I).
    Type: Grant
    Filed: October 2, 1998
    Date of Patent: May 2, 2000
    Assignee: Merck Frosst Canada & Co.
    Inventors: Cameron Black, Serge Leger, Petpiboon Prasit, Zhaoyin Wang, Pierre Hamel, Yongxin Han, Gregory Hughes
  • Patent number: 6054434
    Abstract: 8a-Azalides are useful in the treatment and prevention of bacterial respiratory and enteric infections in livestock animals, particularly in cattle and swine.
    Type: Grant
    Filed: September 9, 1998
    Date of Patent: April 25, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Helmut Kropp, Daniel O. Farrington, Jeffrey N. Clark, Ronald W. Ratcliffe, Robert D. Wilkening
  • Patent number: 6054469
    Abstract: Compounds having formula I, or salts or prodrugs thereof: ##STR1## are selective agonists of the 5-HT.sub.1D.alpha. receptor and are useful in the treatment of migraine and associated conditions.
    Type: Grant
    Filed: April 29, 1998
    Date of Patent: April 25, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Sylvie Bourrain, Angus Murray MacLeod, Graham Andrew Showell
  • Patent number: 6054456
    Abstract: The present invention provides a compound of formula I, or a pharmaceutically acceptable salt thereof: ##STR1## wherein Z, E, Q, T, U, V and L are as defined herein; processes for its preparation and its use in the treatment of conditions for which the administration of an agonist selective for the 5-HT.sub.1D.alpha. receptor subtype is indicated, such as migraine.
    Type: Grant
    Filed: May 26, 1998
    Date of Patent: April 25, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Tamara Ladduwahetty, Angus Murray MacLeod, Michael Rowley
  • Patent number: 6054455
    Abstract: A tachykinin receptor antagonist, in particular a neurokinin-1 receptor antagonist, is useful for the treatment or prevention of chronic nonbacterial prostatitis and/or prostatodynia.
    Type: Grant
    Filed: May 17, 1999
    Date of Patent: April 25, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Harry A. Guess, Joanne Waldstreicher, Jay Dee Pearson