Abstract: A hypoxia contrast medium including nitroimidazole-amino acid chelate with a positively charged radioactive nuclide, a preparation method and use thereof. The contrast medium can be used in imaging cerebral thrombosis, tumors or other diseases such as ulceration, thrombosis, and so on.
Abstract: A diagnostic agent for infectious diseases which is capable of distinguishing among different kinds of bacterial species and which allows simple and non-invasive measurement and/or imaging in a short period of time is provided; and a screening method for a therapeutic agent for infectious diseases caused by microorganisms are provided. A diagnostic agent for infectious diseases caused by nitroimidazole susceptible microorganisms, containing an imidazole derivative or a fused imidazole derivative having at least one nitro group on an imidazole ring, or a labeled form thereof as an active ingredient is provided.
Abstract: The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side-effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.
Type:
Application
Filed:
October 5, 2011
Publication date:
August 9, 2012
Inventors:
Richard Franklin, Martin Quibell, Robert G. Tyson, Bernard T. Golding
Abstract: A hypoxia contrast medium including nitroimidazole-amino acid chelate with a positively charged radioactive nuclide, a preparation method and use thereof. The contrast medium can be used in imaging cerebral thrombosis, tumors or other diseases such as ulceration, thrombosis, and so on.
Abstract: This invention is directed to a class of compounds (Formula I) including hydroxyalkanoyl amino pyrazoles, hydroxyalkanoyl amino thiadiazoles, hydroxyalkanoyl amino acid esters, hydroxyalkanoyl amino acid amides, hydroxyalkanoyl amino alcohols, hydroxyalkanoyl amino ketoes, hydroxyalkanoyl amino hydantoins, hydroxyalkanoyl anilines, and hydroxyalkanoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting &bgr;-amyloid peptide release and/or synthesis, a method for inhibiting &ggr;-secretase activity and a method for treating neurological disorders associated with &bgr;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.
Type:
Application
Filed:
January 31, 2003
Publication date:
January 8, 2004
Inventors:
Jay S. Tung, Ashley C. Guinn, Gene Thorsett, Mike A. Pleiss
Abstract: The invention describes novel compounds of the formula I which are biologically active as ligands of integrin &agr;v&bgr;3
X—Y—Z—R1—CH2—R2(R4)—CH2—CO—R5
in which X, Y, Z, R1, R2, R4 and R5 are as defined in claim 1, and their physiologically acceptable salts and solvates.
Type:
Grant
Filed:
June 21, 2002
Date of Patent:
November 11, 2003
Assignee:
Merck Patent GmbH
Inventors:
Alfred Jonczyk, Oliver Schadt, Simon Goodman
Abstract: The invention provides a processes for the preparation of a compound of Formula I, or a salt thereof
wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH2, O, or NH; and B′ is a base customary in nucleotide chemistry. The processes include reacting a compound of Formula (II)
with a compound of Formula (III)
a compound of Formula (V)
B′—CH2—CO—R2 (V),
a monohaloacetic acid derivative in a suitable solvent with an auxiliary base, or a compound of Formula (VII)
B′—CH2—CO—R3 (VII),
and converting the resulting compounds to that of Formula I.
Type:
Grant
Filed:
February 18, 2000
Date of Patent:
October 15, 2002
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Gerhard Breipohl, Eugen Uhlmann, Jochen Knolle
Abstract: Five-membered heterocycles having biphenylsulfonyl substitution, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the formula I
in which the symbols have the meanings indicated in the claims, have outstanding antiarrhythmic properties and exhibit a cardioprotective component. They can preventively inhibit or greatly decrease the pathophysiological processes in the formation of ischemically induced damage, in particular in the elicitation of ischemically induced cardiac arrhythmias. Moreover, they have a potent inhibitory action on the proliferation of cells.
Type:
Grant
Filed:
January 21, 1998
Date of Patent:
January 1, 2002
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Sabine Faber, Hans-Willi Jansen
Abstract: The hetero-linked phenylglycinolamides are prepared by reaction of the corresponding hetero-linked phenylacetic acids with appropriate phenylglycinols. The hetero-linked phenylglycinolamides are suitable as active compounds in medicaments.
Type:
Grant
Filed:
December 4, 1998
Date of Patent:
February 20, 2001
Assignee:
Bayer Aktiengesellschaft
Inventors:
Siegfried Goldmann, Ulrich Müller, Richard Connell, Hilmar Bischoff, Dirk Denzer, Rudi Grützmann, Martin Beuck