Abstract: The invention concerns benzimidazole derivatives of the general formula (I) in which the radicals R1, R2, R3, X1 and A can have the meanings assigned to them in the specification, their prodrugs, processes for their production as well as the use of the benzimidazole derivatives as medicines, especially as medicines that have trypsin-inhibiting action.
Type:
Grant
Filed:
September 9, 2002
Date of Patent:
February 15, 2005
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Pascale Pouzet, Christoph Hoenke, Claudia Heine, Ralf Anderskewitz, Horst Dollinger, Herbert Nar, Hans Michael Jennewein, Bernd Disse
Abstract: Novel 6,7-disubstituted-5,8-quinolinedione derivatives of general formula (I) or the process for the preparation thereof, wherein R1 is C1-C20 alkylmercapto or phenylamino substituted by up to 3 groups selected from halogen, aceto; R2 is halogen, thiocyano or C1-C20 alkylmercapto, are useful as an antifungal agent.
Abstract: The invention concerns chiral amino acid, is preparation method, and the use of said chiral amino acid as intermediate for the synthesis of chiral organic compounds.
Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.
Abstract: The present invention provides an acrylophosphate derivatives of the formula (I)
wherein n≧1; Ar is
or
The acrylophosphate derivatives of formula (I) have high char residue test results by TGA.
Type:
Grant
Filed:
December 10, 2002
Date of Patent:
June 22, 2004
Assignee:
Chung Shan Institute of Science & Technology
Abstract: The present invention relates to novel trifluorobutenes of the formula (I)
wherein
R1 represents hydrogen; halogen; alkyl that is unsubstituted or substituted with halogen, hydroxy, alkoxy, alkylthio, alkylcarbonyloxy, haloalkylcarbonyloxy, or cyano; alkylsulfonyloxy; or phenyl that is unsubstituted or substituted with halogen, alkyl, haloalkyl, alkoxy, alkylthio, alkylsulfonyl, haloalkoxy, haloalkylthio, phenyl, phenoxy, cyano, or nitro;
R2 represents hydrogen; halogen; alkyl that is unsubstituted or substituted with alkoxy or halogen; or alkoxycarbonyl; and
n represents 0, 1 or 2,
with the proviso that if R1 represents alkyl, then R2 does not represent halogen. The invention also relates to processes for their preparation and their use as nematicides.
Abstract: The present invention provides a compound represented by the general formula I;
wherein A, Ar, X, Z, n, x, y, R and R3 are as defined in the specification.
Type:
Grant
Filed:
June 2, 2003
Date of Patent:
May 11, 2004
Assignee:
Allergan, Inc.
Inventors:
David W. Old, Thang D. Dinh, Robert M. Burk