- ISOQUINOLINOPYRROLOPYRIDINONES ACTIVE AS KINASE INHIBITORS
-
Heteroarylpyridinone derivatives represented by formula (I) wherein R1, R2, R3, R4, R5, and X are as defined in the specification, compositions thereof, and methods of use thereof. Particularly, there are described isoquinolinoyrrolopyridinones, pharmaceutical compositions comprising them and their use as therapeutic agents in the treatment of cancer and cell proliferation disorders.
- -
-
Page/Page column 23
(2008/12/07)
-
- N-substituted pyrrolopyridinones active as kinase inhibitors
-
Compounds represented by formula (I) wherein A, R1, R2, R3, R4, R5, and R6 are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
- -
-
Page/Page column 18
(2010/11/27)
-
- Novel compounds that inhibit dipeptidyl peptidase (DPP-IV) and neprilysin (NEP) and/or angiotensin converting enzyme (ACE)
-
This invention relates to novel compounds, compositions containing the compounds, that inhibit dipeptidyl peptidase (especially DPP-IV) and neprilysin (NEP, neutral endopeptidase) as well as dipeptidyl peptidase (especially DPP-IV) and angiotensin converting enzyme (ACE) and/or dipeptidyl Peptidase (especially DPP-IV) and vasopeptidases (especially ACE and NEP). These compounds and pharmaceutical compositions thereof are useful for the treatment as well as the prevention of type 2 diabetes mellitus.
- -
-
Page/Page column 12
(2010/10/20)
-
- PYRIDYLPYRROLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
-
Pyridylpyrrole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treat
- -
-
Page/Page column 24-25; 41
(2010/02/10)
-
- PYRIMIDYLPYRROLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
-
Pyrimidylpyrrole derivatives of formula (1) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be
- -
-
Page/Page column 32
(2010/02/10)
-
- Process for producing threo-3-amino-2-hydroxybutanoyl-aminoacetic acids, as well as novel intermediated therefor and process for producing them
-
A process for producing threo-3-amino-2-hydroxybutanoylaminoacetic acids comprises the steps of allowing to react a starting compound represented by the general formula: STR1 wherein R1 represents a naphthyl or a group of the formula: STR2 in which R6 and R7 represent individually hydrogen, halogen, amino or a protected amino, hydroxy or a protected hydroxy, a lower alkoxy or a lower alkyl and R2 represents a protected amino, with a starting compound represented by the general formula: STR3 wherein R3 represents hydrogen or an ester residue, to obtain threo-3-protected amino-2-hydroxy-4-oxobutanoic acid or its ester represented by the general formula: STR4 wherein R1, R2 and R3 have the same meanings as above, and then reducing the same into threo-3-protected amino-2-hydroxybutanoic acid or its ester represented by the general formula: STR5 wherein R1, R2 and R3 have the same meanings as above, and further converting the above compound into 3-amino-2-hydroxybutanoic acid represented by the general formula: STR6 wherein R2 ' represents amino or a protected amino, thereafter condensing the same, in a conventional manner for forming a peptide coupling, with a compound represented by the general formula: STR7 wherein R4 represents an alkyl having 3-4 carbon atom or 3-guanidinopropyl, while previously protecting as required those groups not relevant to the reaction, and removing the protecting groups for the functional groups to produce threo-3-amino-2-hydroxybutanoylaminoacetic acids represented by the general formula: STR8 wherein R1 and R4 have the same meanings as above. This invention also provides the compounds represented by the general formula (III) as novel intermediates for the above aimed compounds and a process for producing the intermediates.
- -
-
-