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
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
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
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
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
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
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.
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
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.
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.
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
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
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
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
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).
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
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
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
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