Abstract: Supertwist liquid crystal displays with outstanding properties are obtained when the nematic liquid crystal mixture contains at least one compound of the formula (I): ##STR1## where the variables are as defined in the disclosure.
Type:
Grant
Filed:
December 1, 1997
Date of Patent:
January 25, 2000
Assignee:
Merck Patent Gesellschaft mit Beschrankter Haftung
Inventors:
Volker Reiffenrath, Bernhard Rieger, Michael Junge, Martina Schmidt, Christine Pfister
Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
Abstract: An efficient method for the preparation of key intermediate, in the synthesis of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one, a reverse transcriptase inhibitor is achieved using a chiral addition reaction to the 4-chloro-2-trifluoromethylketoaniline with an organozinc complex to give the desired alcohol. This instant method has broad applicability in the chiral addition to any prochiral ketone.
Type:
Grant
Filed:
May 11, 1998
Date of Patent:
January 18, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Cheng Yi Chen, Lushi Tan, Richard D. Tillyer
Abstract: Disclosed are methods for inhibiting bone resorption in mammals while minimizing the occurrence of or potential for adverse gastrointestinal effects. Also disclosed are pharmaceutical compositions and kits for caring out the therapeutic methods disclosed herein.
Type:
Grant
Filed:
August 14, 1998
Date of Patent:
January 18, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Anastasia G. Daifotis, A. John Yates, Arthur C. Santora, II
Abstract: Disclosed are spiro-substituted azacycles of formula I are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula I are shown to be neurokinin antagonists.
Type:
Grant
Filed:
December 4, 1997
Date of Patent:
January 11, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Yuan-Ching P. Chiang, Patrick T. Dunn, Hiroo Koyama
Abstract: The invention relates to copolymers made from mono-reactive liquid and/or di-reactive liquid crystals which can be photopolymerized to form copolymers and to novel reactive liquid crystal compound having a nematic phase. Preferentially the reactive liquid crystal is polymerized while in the liquid crystal phase to produce an oriented birefringent polymer film. To do this, the reactive liquid crystal, in its nematic or smectic phase is aligned (by well known techniques such as rubbed polyimide, etc.) and the thin film containing a small amount of photoinitiator, is subjected to ultraviolet light whereupon it polymerizes into a thin, aligned polymer film.
Type:
Grant
Filed:
December 8, 1997
Date of Patent:
January 11, 2000
Assignee:
Merck Patent Gesellschaft mit Beschrankter Haftung
Inventors:
Owain Llyr Parri, Ian Bonny, Ian Victor E. Hassall, Mark John Goulding, Simon Greenfield, Emma Jane Brown, David Coates
Abstract: An interactive computer assisted method reviews, and analyzes, a patient who needs one or more medications using a computer and a user associated therewith. The method includes the steps of pre-selecting patients to obtain a preliminary set of patients eligible for the interactive computer assisted method responsive to first predetermined criteria, and filtering the preliminary set of patients to identify and form a secondary set of patients from the preliminary set of patients having a greater likelihood of benefiting from the interactive computer assisted method responsive to second predetermined criteria. The method also includes the steps of enrolling a patient from the secondary set of patients, and communicating with the patient to obtain information to assist the user in determining whether therapy and/or medication issues are relevant.
Type:
Grant
Filed:
April 2, 1998
Date of Patent:
January 11, 2000
Assignee:
Merck-Medco Managed Care, LLC
Inventors:
J. Russel Teagarden, Michael Clotz, David Angaran, Charlotte Kenreigh
Abstract: The present invention is directed spiro-substituted azacycles of formula I: (wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, k, l and m are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
Type:
Grant
Filed:
December 12, 1997
Date of Patent:
January 11, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Sander G. Mills, Malcolm Maccoss, Martin S. Springer
Abstract: The invention relates to a liquid material in the form of cholesteric polymer network, wherein the polymerized material is obtainable by copolymerization of a compound (a) having at least two polymerizable functional groups and a chiral polymerizable compound (b), which is a terpinoid and to novel polymerizable terpinoids.
Type:
Grant
Filed:
May 23, 1997
Date of Patent:
January 4, 2000
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Abstract: Thiazole substituted benzenesulfonamides are .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for decreasing gut motility are also disclosed.
Type:
Grant
Filed:
January 15, 1998
Date of Patent:
January 4, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Robert J. Mathvink, Emma R. Parmee, Samuel Tolman, Ann E. Weber
Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## for example: ##STR2##
Type:
Grant
Filed:
September 3, 1998
Date of Patent:
January 4, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Bruce D. Dorsey, Philip E. Sanderson, Terry A. Lyle
Abstract: A process of welding plastic vials and closure suitable for sterile filling operations is disclosed. Following a mechanical seal, a heated die is used to fuse the container and closure into a hermetic seal capable of use in the pharmaceutical industry.
Abstract: Compounds of formula I: ##STR1## as well as pharmaceutically acceptable salts thereof are disclosed. R.sup.2 is H and R.sup.3 is C1-3 alkyl, or R.sup.2 and R.sup.3 taken in combination represent C.sub.1-3 alkylidene. Pharmaceutical compositions and methods of treatment are also included. The compounds are useful against methicillin resistant staphylococci (MRSA).
Type:
Grant
Filed:
October 8, 1998
Date of Patent:
December 28, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Ronald W. Ratcliffe, Timothy A. Blizzard
Abstract: Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR .alpha., .delta. and/or .gamma. mediated diseases, disorders and conditions.
Type:
Grant
Filed:
December 17, 1998
Date of Patent:
December 28, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Soumya P. Sahoo, Richard L. Tolman, Wei Han, Jeffrey Bergman, Conrad Santini, Victoria K. Lombardo, Ranjit Desai, Julia K. Boueres, Dominick F. Gratale
Abstract: Disclosed is a method for treating and preventing bone loss in patients by administering a formulation of anhydrous alendronate sodium. Also described is a pharmaceutical doage form of said anhydrous alendronate sodium, being anhydrous 4-amino-1-hydroxy-butylidene-1,1-bisphosphonic acid, monosodium salt, in a pharmaceutically acceptable excipient.
Type:
Grant
Filed:
August 13, 1998
Date of Patent:
December 28, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Gerald S. Brenner, Drazen Ostovic, Earl R. Oberholtzer, Jr., J. Eric Thies
Abstract: The invention relates to a linear UV polarizer based on a polymerized mesogen obtained by curing with actinic radiation or heat of a polymerizable composition comprising:a) a liquid crystalline component A composed of one or more achiral mesogenic compounds having at least one polymerizable end group optionally linked via a spacer group to a mesogenic core,b) a dichroic component B that absorbs light in the UV region, with an absorption maximum of from 320 to 440 nm, andc) a photoinitiator or thermal initiator component C.
Type:
Grant
Filed:
July 3, 1997
Date of Patent:
December 28, 1999
Assignee:
Merck Patent Gesellschaft mit Beschrankter Haftung
Inventors:
David Coates, Emma Jolliffe, Patrick Nolan
Abstract: The object of the present invention is to provide a preparation for local administration to permit selective delivery of an effective amount of sodium alendronate to the bone site where bone resorption is accentuated.
Abstract: A trans-activation assay for leptin is described. Leptin response elements are located proximal to a promoter, and the promoter region is operatively linked to a reporter gene. When leptin binds with the receptor, the reporter gene is transcribed.
Type:
Grant
Filed:
April 21, 1997
Date of Patent:
December 28, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Charles I. Rosenblum, Leonardus H. T. Van Der Ploeg, Sajjad A. Qureshi, Doris F. Cully, John W. Hess, Michael R. Tota, Fang Chen
Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##
Type:
Grant
Filed:
November 4, 1998
Date of Patent:
January 4, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Edward S. Inamine, Otto D. Hensens, David R. Houck, Ta J. Lee, Robert L. Smith, Wasyl Halczenko, George D. Hartman, Gerald E. Stokker
Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formula (II): ##STR1##
Type:
Grant
Filed:
November 4, 1998
Date of Patent:
January 18, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Robert L. Smith, Wasyl Halczenko, George D. Hartman, Gerald E. Stokker, Edward S. Inamine, Otto D. Hensens, David R. Houck, Ta Jyh Lee