Patent classifications
C07C335/40
Therapeutic compounds
The invention provides methods for producing analgesia in an animal comprising administering to the animal a compound of the formula Ia, Ib, Ic, and Id: ##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables A, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.x, L, X, Y, and Z have the meaning as described herein.
Hydrosoluble hydroxybisphosphonic derivatives of doxorubicin
The invention relates to hydrosoluble hydroxybisphosphonic derivatives of doxorubicin of formula (I) and the pharmaceutically acceptable salts thereof. The invention also relates to the use of said compounds as a drug, especially in the treatment of a bone tumour. The invention further relates to the pharmaceutical compositions comprising such compounds, the methods for the synthesis thereof and synthesis intermediates. ##STR00001##
Hydrosoluble hydroxybisphosphonic derivatives of doxorubicin
The invention relates to hydrosoluble hydroxybisphosphonic derivatives of doxorubicin of formula (I) and the pharmaceutically acceptable salts thereof. The invention also relates to the use of said compounds as a drug, especially in the treatment of a bone tumour. The invention further relates to the pharmaceutical compositions comprising such compounds, the methods for the synthesis thereof and synthesis intermediates. ##STR00001##
THERAPEUTIC COMPOUNDS
The invention provides compounds of formula Ia, Ib, Ic, and Id:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables A, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.x, L, X, Y, and Z have the meaning as described herein. The compounds are useful for reducing endoplasmic reticulum stress and for producing analgesia in an animal.
Chemical Activators of Nicotinamide Mononucleotide adenylyltransferase 2 (NMNAT2) and Uses Thereof
The present disclosure relates to novel NMNAT2 activators, semicarbazones and thiosemicarbazones, to processes for preparing them, to pharmaceutical preparations comprising them, to the method by administering the novel semicarbazones and thiosemicarbazones for the treatment and/or prevention of diseases and to the use thereof for the production of a medicament for the treatment and/or prevention of diseases, especially neurodegenerative and age-associated diseases or conditions associated with NAD loss. The present disclosure also provides a method for high throughput screening of NMNAT2 activators.
Chemical Activators of Nicotinamide Mononucleotide adenylyltransferase 2 (NMNAT2) and Uses Thereof
The present disclosure relates to novel NMNAT2 activators, semicarbazones and thiosemicarbazones, to processes for preparing them, to pharmaceutical preparations comprising them, to the method by administering the novel semicarbazones and thiosemicarbazones for the treatment and/or prevention of diseases and to the use thereof for the production of a medicament for the treatment and/or prevention of diseases, especially neurodegenerative and age-associated diseases or conditions associated with NAD loss. The present disclosure also provides a method for high throughput screening of NMNAT2 activators.
CELLULOSE SYNTHASE INHIBITORS AS A NEW CLASS OF HERBICIDE AND NON-GMO CROPS THAT ARE RESISTANT TO THE HERBICIDE
Using chemical genetic screening, we discovered a small molecule Cellulosin (aka endosidin20 or ES20) that causes cell swollen and inhibits plant growth, but does not disrupt global vesicle trafficking. By doing mutant screening, we obtained multiple alleles of Arabidopsis thaliana that are resistant to Cellulosin inhibition in growth. Those mutated amino acid residues are conserved across plant species. Cellulosin targets a group of cellulose synthases (CesAs) of Arabidopsis thaliana by binding to a conserved domain essential for the catalytic activity of CesA. Cellulosin may target and inhibit all subtypes of CesAs in plants. The present invention relates to Cellulosin, a cellulose synthase inhibitor, its analogs or derivatives as a broad-spectrum herbicide. The mutated genes, their protein products and a cell or a plant having those mutated genes or expressing those protein products are within the scope of this disclosure.
CELLULOSE SYNTHASE INHIBITORS AS A NEW CLASS OF HERBICIDE AND NON-GMO CROPS THAT ARE RESISTANT TO THE HERBICIDE
Using chemical genetic screening, we discovered a small molecule Cellulosin (aka endosidin20 or ES20) that causes cell swollen and inhibits plant growth, but does not disrupt global vesicle trafficking. By doing mutant screening, we obtained multiple alleles of Arabidopsis thaliana that are resistant to Cellulosin inhibition in growth. Those mutated amino acid residues are conserved across plant species. Cellulosin targets a group of cellulose synthases (CesAs) of Arabidopsis thaliana by binding to a conserved domain essential for the catalytic activity of CesA. Cellulosin may target and inhibit all subtypes of CesAs in plants. The present invention relates to Cellulosin, a cellulose synthase inhibitor, its analogs or derivatives as a broad-spectrum herbicide. The mutated genes, their protein products and a cell or a plant having those mutated genes or expressing those protein products are within the scope of this disclosure.
CELLULOSE SYNTHASE INHIBITORS AS A NEW CLASS OF HERBICIDE AND NON-GMO CROPS THAT ARE RESISTANT TO THE HERBICIDE
Using chemical genetic screening, we discovered a small molecule Cellulosin (aka endosidin20 or ES20) that causes cell swollen and inhibits plant growth, but does not disrupt global vesicle trafficking. By doing mutant screening, we obtained multiple alleles of Arabidopsis thaliana that are resistant to Cellulosin inhibition in growth. Those mutated amino acid residues are conserved across plant species. Cellulosin targets a group of cellulose synthases (CesAs) of Arabidopsis thaliana by binding to a conserved domain essential for the catalytic activity of CesA. Cellulosin may target and inhibit all subtypes of CesAs in plants. The present invention relates to Cellulosin, a cellulose synthase inhibitor, its analogs or derivatives as a broad-spectrum herbicide. The mutated genes, their protein products and a cell or a plant having those mutated genes or expressing those protein products are within the scope of this disclosure.
CELLULOSE SYNTHASE INHIBITORS AS A NEW CLASS OF HERBICIDE AND NON-GMO CROPS THAT ARE RESISTANT TO THE HERBICIDE
Using chemical genetic screening, we discovered a small molecule Cellulosin (aka endosidin20 or ES20) that causes cell swollen and inhibits plant growth, but does not disrupt global vesicle trafficking. By doing mutant screening, we obtained multiple alleles of Arabidopsis thaliana that are resistant to Cellulosin inhibition in growth. Those mutated amino acid residues are conserved across plant species. Cellulosin targets a group of cellulose synthases (CesAs) of Arabidopsis thaliana by binding to a conserved domain essential for the catalytic activity of CesA. Cellulosin may target and inhibit all subtypes of CesAs in plants. The present invention relates to Cellulosin, a cellulose synthase inhibitor, its analogs or derivatives as a broad-spectrum herbicide. The mutated genes, their protein products and a cell or a plant having those mutated genes or expressing those protein products are within the scope of this disclosure.