C07C237/04

AMINOMETHYL-FUNCTIONALIZED DENATONIUM DERIVATIVES, THEIR PREPARATION AND USE

The present invention is directed to compounds of the general formula (I) and salts thereof

##STR00001##

wherein X.sup. is halide, pseudohalide, sulphate, benzoate, acetate, trifluoroacetate, hydroxide, saccharinate or capsaicinate; R.sup.10 is hydrogen or C1-C10-alkyl; and R.sup.1-R.sup.9 independently are hydrogen, halogen, C1-C5-alkyl, C1-C4-alkoxy, C1-C20-alkoxycarbonyl. The invention is furthermore directed to a method for the preparation of these compounds. The compounds can be used as bitter substances in medicine, pharmaceutics and/or diagnostics. They can furthermore be used for the coupling to proteins and peptides by means of forming a peptide bond between the amino-group of the compounds of the present invention and a carboxyl-group of the protein or peptide.

AMINOMETHYL-FUNCTIONALIZED DENATONIUM DERIVATIVES, THEIR PREPARATION AND USE

The present invention is directed to compounds of the general formula (I) and salts thereof

##STR00001##

wherein X.sup. is halide, pseudohalide, sulphate, benzoate, acetate, trifluoroacetate, hydroxide, saccharinate or capsaicinate; R.sup.10 is hydrogen or C1-C10-alkyl; and R.sup.1-R.sup.9 independently are hydrogen, halogen, C1-C5-alkyl, C1-C4-alkoxy, C1-C20-alkoxycarbonyl. The invention is furthermore directed to a method for the preparation of these compounds. The compounds can be used as bitter substances in medicine, pharmaceutics and/or diagnostics. They can furthermore be used for the coupling to proteins and peptides by means of forming a peptide bond between the amino-group of the compounds of the present invention and a carboxyl-group of the protein or peptide.

CHARGED ION CHANNEL BLOCKERS AND METHODS FOR USE
20210061763 · 2021-03-04 ·

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof:

##STR00001##

The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.

CHARGED ION CHANNEL BLOCKERS AND METHODS FOR USE
20210061763 · 2021-03-04 ·

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof:

##STR00001##

The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.

KETAMINE DERIVATIVES AND COMPOSITIONS THEREOF

Ketamine derivatives and pharmaceutical compositions thereof are disclosed. When administered orally the ketamine derivatives provide increased bioavailability of ketamine in the systemic circulation. The ketamine derivatives can be used to treat neurological diseases, psychological diseases and pain.

Solid Support
20210207288 · 2021-07-08 ·

A solid support for use in non-aqueous DNA-conjugated molecule reactions, wherein the support comprises a solid body formed from a plurality of polyethylene glycol units, wherein the solid body includes at least one cationic moiety.

Linker Containing Arylnitro, Antibody-Drug Conjugate Containing Linker and Use of Linker

The present application relates to a linker containing arylnitro, an antibody-drug conjugate the linker and use of the linker, as well as a pharmaceutical composition comprising the antibody-drug conjugate and use of the antibody-drug conjugate for treatment and/or prevention of a disease.

##STR00001##

Linker Containing Arylnitro, Antibody-Drug Conjugate Containing Linker and Use of Linker

The present application relates to a linker containing arylnitro, an antibody-drug conjugate the linker and use of the linker, as well as a pharmaceutical composition comprising the antibody-drug conjugate and use of the antibody-drug conjugate for treatment and/or prevention of a disease.

##STR00001##

Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds

Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.

Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds

Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.