Abstract: The present invention relates to a transgenic non-human animal embryo lacking native presenilin 1 and a transgenic non-human animal having only a non-native presenilin 1. The transgenic animals and cells derived therefrom can be used in the study of the expression pattern, activity and modulators of presenilin 1, in the study of the role of presenilin 1 in Alzheimer's Disease and in the study of disorders of the central nervous system.
Type:
Grant
Filed:
May 14, 1998
Date of Patent:
September 17, 2002
Assignees:
Merck & Co., Inc., Johns Hopkins University
Inventors:
Hui Zheng, Ping Jiang, Su Qian, Leonardus H. T. Van Der Ploeg, Philip Chun-Ying Wong, Sangram S. Sisodia
Abstract: A substituted triazolopyridazine derivative, its use in cognition enhancement therapy, compositions containing it and processes for its manufacture.
Type:
Grant
Filed:
July 24, 2000
Date of Patent:
September 10, 2002
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street
Abstract: To provide an ultraviolet absorbent having high UV shieldability, especially UV-A shieldability, high transparency and good dispersibility.
An ultraviolet absorbent, which comprises a flaky substrate coated with ultra-fin zinc oxide particles having a mean particle size of not larger than 100 nm, and which is optionally treated with an organic silicone compound; and a method for producing the ultraviolet absorbent, which comprises calcining particles as coated with basic zinc carbonate in the presence of a complex-forming agent.
Abstract: The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof:
wherein X is CH2, O or S. The compounds inhibit gamma secretase without affecting Notch signalling, and hence find use in the treatment or prevention of Alzheimer's disease.
Abstract: The invention relates to a method for disubstituting carboxylic acid amides on the geminal carbonyl-C-atom using at least one grignard reagent in the presence of a metal alcoholate compound used as a catalyst and in the presence of another organometallic compound used as a co-catalyst.
Type:
Grant
Filed:
February 23, 2001
Date of Patent:
September 10, 2002
Assignee:
Merck Patent Gesellschaft mit beschraenkter Haftung
Abstract: The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme.
The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.
Type:
Grant
Filed:
December 21, 2000
Date of Patent:
September 10, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Yves Leblanc, Claude Dufresne, Jacques Yves Gauthier, Robert Young
Abstract: The present invention relates to fluoro-&agr;,&ohgr;-bis[(fluoroalkyl)fluorophosphorano)]alkanes, to a process for their preparation, and to their use as intermediates.
Type:
Application
Filed:
February 28, 2002
Publication date:
September 5, 2002
Applicant:
MERCK KGAA
Inventors:
Michael Schmidt, Andreas Kuhner, Nikolai Ignatyev, Peter Sartori
Abstract: Fluoroalkylphosphate salts of Formula I, described herein, are suitable for use, alone or in mixtures with, e.g., other salts, in electrolytes, primary batteries, secondary batteries, capacitors, supercapacitors or galvanic cells.
Type:
Application
Filed:
February 25, 2002
Publication date:
September 5, 2002
Applicant:
Merck Patent GmbH
Inventors:
Michael Schmidt, Andreas Kuh ner, Nikolai Ignatyev, Peter Sartori
Abstract: Compounds represented by formula I:
as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also included. The compounds are active against the caspase-3 enzyme, and thus are useful to treat fin caspase-3 mediated diseases and conditions.
Type:
Grant
Filed:
July 19, 2000
Date of Patent:
September 3, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Yongxin Han, Andre Giroux, Robert Zamboni, Daniel J. McKay, Christopher I. Bayly, Erich L. Grimm, John Colucci
Abstract: A compound of formula I, or a salt or prodrug thereof:
wherein:
Z represents C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, aryl, C3-7 heterocycloalkyl, heteroaryl or di(C1-6)alkylamino, any of which groups may be optionally substituted;
R1 represents an optionally substituted five-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or
R1 represents an optionally substituted six-membered heteroaromatic ring selected from pyrazine, pyrimidine and pyridazine; and
R2 represents cyano(C1-6)alkyl, hydroxy(C1-6)alkyl, C3-7 cycloalkyl(C1-6)alkyl, propargyl, C3-7 heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; its use in treating anxiety and pharmaceutical compositions comprising it; a subclass of compounds which are useful in enhancing cognition, such as Alzheimer's Disease, is also disclosed.
Type:
Grant
Filed:
August 27, 1998
Date of Patent:
September 3, 2002
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Tamara Ladduwahetty, Kevin John Merchant, Francine Sternfeld, Leslie Joseph Street
Abstract: The present invention relates to 2,6-di-tert-butylphenols of the formula I
in which
R, A1 A2, Z1, Z2 m and n are as defined herein, and their use as stabilizers or antioxidants.
Type:
Grant
Filed:
October 10, 1997
Date of Patent:
September 3, 2002
Assignee:
Merck Patent Gesellschaft Mit Beschraenkter Haftung
Abstract: Amine salts of 3-(2-methyl-pyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-nonanoic acid are potent antagonists of the integrin &agr;v&bgr;3 receptor and are useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salts as well as pharmaceutical compositions containing the salts and methods of using the salts. Also disclosed are 3(R)- and 3(S)-(2-methylpyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid in the form of a zwitterion trihydrate.
Type:
Grant
Filed:
November 29, 2001
Date of Patent:
September 3, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Guy R. Humphrey, Marjorie See Waters, Wei Xu
Abstract: Acetylene derivatives of the formula I
in which
R, A1, A2, Z1, Z2, Z3, L1, L2, L3, Y, m and n are as defined herein
are suitable as components of liquid-crystalline media.
Abstract: The invention relates to a plastic part having lustrous pigments and filler particles. Moldings of this plastic part exhibit a pronounced glitter effect.
Type:
Application
Filed:
February 11, 2002
Publication date:
August 29, 2002
Applicant:
Merck Patent GmbH
Inventors:
Hans-Jurgen Brehm, Manfred Kieser, Emil Aust
Abstract: Polymorphic, amorphous and hydrated forms of the title compound having the following structure:
are disclosed. The compound is a potent and selective cyclooxygenase-2 (COX-2) inhibitor.
Abstract: The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemothera-peutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
Type:
Grant
Filed:
September 7, 2000
Date of Patent:
August 27, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Ian M. Bell, Douglas C. Beshore, Steven N. Gallicchio, C. Blair Zartman