The present invention relates to a sacubitril intermediate and a preparation method thereof. The sacubitril intermediate disclosed herein can be prepared by a deprotection reaction of a compound. In addition, the intermediate can be used as a raw material to synthesize sacubitril.

The present invention relates to a sacubitril intermediate and a preparation method thereof. The sacubitril intermediate disclosed herein can be prepared by a deprotection reaction of a compound. In addition, the intermediate can be used as a raw material to synthesize sacubitril.

Useful processes of preparation and intermediates useful for the preparation of Compound 1, a selective estrogen receptor alpha (ERα) modulator/degrader (SERM/SERD), having utility for the treatment of ER+ cancers including breast cancer are described.

Useful processes of preparation and intermediates useful for the preparation of Compound 1, a selective estrogen receptor alpha (ERα) modulator/degrader (SERM/SERD), having utility for the treatment of ER+ cancers including breast cancer are described.

This invention provides a compound having the structure

##STR00001##

wherein α, β, X, Y, and R.sub.1-R.sub.11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF.sub.K-B activation in a population of cells.

This invention provides a compound having the structure

##STR00001##

wherein α, β, X, Y, and R.sub.1-R.sub.11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF.sub.K-B activation in a population of cells.

The invention generally concerns a novel class of CB 1 receptor binding molecules and uses thereof.

Provided herein are novel ortho-Phthalaldehyde (OPA) containing linkers (OPA-L) and the use of OPA-L for the preparation of Antibody-drug conjugate (ADC) via the formation of Phthalimidine through the reaction of primary amine on antibody (e.g., residue of Lysine) and ortho-Phthalaldehyde. The advantage of this OPA-L is high reactivity and can be applied in different types of antibodies to form stably-linked conjugates. The use of OPA-L for the preparation of ADC is advantageous for mild and wide condition of conjugation, for instance, low percentage of organic solvent required, wide range of pH and temperature can be used.

Provided herein are novel ortho-Phthalaldehyde (OPA) containing linkers (OPA-L) and the use of OPA-L for the preparation of Antibody-drug conjugate (ADC) via the formation of Phthalimidine through the reaction of primary amine on antibody (e.g., residue of Lysine) and ortho-Phthalaldehyde. The advantage of this OPA-L is high reactivity and can be applied in different types of antibodies to form stably-linked conjugates. The use of OPA-L for the preparation of ADC is advantageous for mild and wide condition of conjugation, for instance, low percentage of organic solvent required, wide range of pH and temperature can be used.

Provided are a compound represented by formula (I) or a salt thereof, a nerve growth promoter containing the compound or a salt thereof as an active ingredient, a pharmaceutical composition containing the compound or a salt thereof, a therapeutic agent for neurodegenerative diseases containing the compound or a salt thereof as an active ingredient, a therapeutic agent for amyotrophic lateral sclerosis containing the compound or a salt thereof as an active ingredient, a therapeutic agent for pain containing the compound or a salt thereof as an active ingredient, and a therapeutic agent for lower urinary tract dysfunction containing the compound or a salt thereof as an active ingredient.