Abstract: Compounds of formula (I): are found to be selective inhibitors of cathepsin B, and hence useful in treating a variety of pathological conditions.
Type:
Application
Filed:
September 24, 2007
Publication date:
February 25, 2010
Applicant:
MERCK FROSST CANADA LTD, Merk & Co., Inc.
Inventors:
Jacques Yves Gauthier, Vouy-Linh Truong
Abstract: The present invention features truncated MCH analogs active at the MCH receptor. The truncated MCH analogs are optionally modified peptide derivatives of mammalian MCH. The analogs can bind to the MCH receptor and, preferably, bring about signal transduction. MCH analogs have a variety of different uses including being used as a research tool and being used therapeutically.
Abstract: Provided are methods of identifying inhibitors of ?-secretase that employ modified ?-secretase substrates. The modified ?-secretase substrates have ?-secretase cleavage sites that are altered from wild type. The amino acid sequences of the altered ?-secretase cleavage sites contain different amino acids in at least one of the positions P2-P1-P1?-P2? of the ?-secretase cleavage site. Many of the modified ?-secretase substrates are more efficient substrates for ?-secretase than are corresponding substrates having wild-type sequences, that is, these modified substrates are more susceptible to enzymatic breakdown by ?-secretase. Recombinant polynucleotide molecules encoding the modified ?-secretase substrates are provided. Antibodies that recognize cleavage products of the modified ?-secretase substrates are provided. Stable cell lines expressing the modified ?-secretase substrates are provided. Transgenic animals expressing the modified ?-secretase substrates are provided.
Type:
Grant
Filed:
April 30, 2003
Date of Patent:
March 27, 2007
Assignee:
Merk & Co., Inc.
Inventors:
Daria Jean Hazuda, Elizabeth Chen Dodson, Ming-Tain Lai, Min Xu, Xiao-Ping Shi, Adam J. Simon, Guoxin Wu, Yueming Li, Bruce Register
Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
May 1, 2003
Date of Patent:
August 1, 2006
Assignee:
Merk & Co., Inc.
Inventors:
James C. Barrow, Philippe G. Nantermet, Harold G. Selnick
Abstract: The invention provides a method, system, and computer program device for allowing users to preview and/or choose one or more slides and slidekits to be incorporated into a professional presentation. Intended users include physicians and other healthcare providers. Slidekits are displayed by medical categories to which they are assigned. Each slidekit includes a series of interrelated slides concerning a particular medical topic. Each slide may include lecture notes, in addition to a thumbnail image, full image display, title, and/or brief description. Slides and/or slidekits may be downloaded to the user's remote computer, for further incorporation into a presentation, printed by the user, or stored in the user's folder. The user's folder also may be used to store other folders and/or bookmarks to internal or external pages. Optionally, the user's right to access the slidekits and/or external sites is verified.
Type:
Application
Filed:
March 18, 2003
Publication date:
December 4, 2003
Applicant:
Merk & Co., Inc.
Inventors:
Susan Schramm-Apple, Sean Dippold, Melanie Kittrell, Keith Bauer, Lori Moore
Abstract: Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).
Type:
Application
Filed:
September 21, 2001
Publication date:
August 22, 2002
Applicant:
Merk & Co., Inc.
Inventors:
Victor M. Garsky, Dong-Mei Feng, Defeo-Jones Deborah
Abstract: The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit farnesyl-protein transferase. Furthermore, these CAAX analogues differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.