Patent classifications
C07D277/28
DICARBOXYLIC ACID BISAMIDE DERIVATIVES, USE THEREOF, PHARMACEUTICAL COMPOSITION BASED THEREON AND METHODS FOR PRODUCING DICARBOXYLIC ACID BISAMIDE DERIVATIVES
The present invention relates to novel biologically active compounds, in particular dicarboxylic acid bisamide derivatives of general formula I:
##STR00001##
or pharmaceutically acceptable salts thereof, which are able to form complexes with or chelate metal ions. The invention also relates to the use of said compounds as an agent for the prevention and/or treatment of cardiovascular, viral, cancer, neurodegenerative and inflammatory diseases, diabetes, age-related diseases, diseases caused by microbial toxins, alcoholism and alcoholic cirrhosis, anaemia, porphyria cutanea tarda, and transition metal salt poisoning. The present invention also relates to novel methods for preparing dicarboxylic acid bisamide derivatives of general formula I.
THIAZOLOXIME AND OXAZOLOXIME DERIVATIVES AS REACTIVATORS OF ORGANOPHOSPHOROUS NERVE AGENT (OPNA)-INHIBITED HUMAN ACETYLCHOLINESTERASE FOR THE TREATMENT OF NERVOUS AND/OR RESPIRATORY FAILURE AFTER INTOXICATION WITH OPNA
The present invention relates to a compound of formula (I). It also relates to a pharmaceutical composition comprising at least one compound of formula (I) and at least one pharmaceutically acceptable support. Finally, it relates to the compounds of formula (I) for use in a method of medical treatment, preferably in the treatment of a nervous and/or respiratory failure due to intoxication with at least one organo-phosphorous nerve agent (OPNA); in the treatment of neurological diseases such as Alzheimer's disease; and/or in the treatment of cancer. The compounds act as reactivators of OPNA-inhibited hAChE (human acetylcholinesterase).
##STR00001##
THIAZOLOXIME AND OXAZOLOXIME DERIVATIVES AS REACTIVATORS OF ORGANOPHOSPHOROUS NERVE AGENT (OPNA)-INHIBITED HUMAN ACETYLCHOLINESTERASE FOR THE TREATMENT OF NERVOUS AND/OR RESPIRATORY FAILURE AFTER INTOXICATION WITH OPNA
The present invention relates to a compound of formula (I). It also relates to a pharmaceutical composition comprising at least one compound of formula (I) and at least one pharmaceutically acceptable support. Finally, it relates to the compounds of formula (I) for use in a method of medical treatment, preferably in the treatment of a nervous and/or respiratory failure due to intoxication with at least one organo-phosphorous nerve agent (OPNA); in the treatment of neurological diseases such as Alzheimer's disease; and/or in the treatment of cancer. The compounds act as reactivators of OPNA-inhibited hAChE (human acetylcholinesterase).
##STR00001##
HUMAN PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE
The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis.
HUMAN PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE
The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis.
Anticancer indenes, indanes, azaindenes, azaindanes, pharmaceutical compositions and uses
Disclosed are compounds for medical uses, for example, compounds of formula Ia, ##STR00001##
wherein A.sub.1, A.sub.2, A.sub.3, A.sub.4, A.sub.5, A.sub.6, A.sub.7, R.sub.6, R.sub.7 and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.
Anticancer indenes, indanes, azaindenes, azaindanes, pharmaceutical compositions and uses
Disclosed are compounds for medical uses, for example, compounds of formula Ia, ##STR00001##
wherein A.sub.1, A.sub.2, A.sub.3, A.sub.4, A.sub.5, A.sub.6, A.sub.7, R.sub.6, R.sub.7 and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.
NOVEL PERIPHERAL CANNABINOID-1 RECEPTOR ANTAGONISTS
The technology disclosed herein concerns compounds capable of binding to CB1Rs in the periphery and not in the CNS.
USE OF STROBILURIN TYPE COMPOUNDS FOR COMBATING PHYTOPATHOGENIC FUNGI CONTAINING AN AMINO ACID SUBSTITUTION F129L IN THE MITOCHONDRIAL CYTOCHROME B PROTEIN CONFERRING RESISTANCE TO QO INHIBITORS II
- Andreas Koch ,
- Marcus Fehr ,
- Vanessa Tegge ,
- Chandan Dey ,
- Manojkumar Poonoth ,
- Sarang Kulkarni ,
- Ronan Le Vezouet ,
- Christian Harald Winter ,
- Georg Christoph Rudolf ,
- Rakesh Rath ,
- Smriti Khanna ,
- lan Robert Craig ,
- Wassilios Grammenos ,
- Thomas Grote ,
- Gerd Stammler ,
- Tobias Mentzel ,
- Egon Haden ,
- Joachim Rheinheimer
The present invention relates to the use of strobilurin type compounds of formula I and the N-oxides and the salts thereof for combating phytopathogenic fungi containing an amino acid substitution F129L in the mitochondrial cytochrome b protein (also referred to as F129L mutation in the mitochondrial cytochrome b gene) conferring resistance to Qo inhibitors, and to methods for combating such fungi. The invention also relates to novel compounds, processes for preparing these compounds, to compositions comprising at least one such compound, and to seeds coated with at least one such compound.
USE OF STROBILURIN TYPE COMPOUNDS FOR COMBATING PHYTOPATHOGENIC FUNGI CONTAINING AN AMINO ACID SUBSTITUTION F129L IN THE MITOCHONDRIAL CYTOCHROME B PROTEIN CONFERRING RESISTANCE TO QO INHIBITORS II
- Andreas Koch ,
- Marcus Fehr ,
- Vanessa Tegge ,
- Chandan Dey ,
- Manojkumar Poonoth ,
- Sarang Kulkarni ,
- Ronan Le Vezouet ,
- Christian Harald Winter ,
- Georg Christoph Rudolf ,
- Rakesh Rath ,
- Smriti Khanna ,
- lan Robert Craig ,
- Wassilios Grammenos ,
- Thomas Grote ,
- Gerd Stammler ,
- Tobias Mentzel ,
- Egon Haden ,
- Joachim Rheinheimer
The present invention relates to the use of strobilurin type compounds of formula I and the N-oxides and the salts thereof for combating phytopathogenic fungi containing an amino acid substitution F129L in the mitochondrial cytochrome b protein (also referred to as F129L mutation in the mitochondrial cytochrome b gene) conferring resistance to Qo inhibitors, and to methods for combating such fungi. The invention also relates to novel compounds, processes for preparing these compounds, to compositions comprising at least one such compound, and to seeds coated with at least one such compound.