Provided herein are processes, compounds and compositions for making (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid. Also provided herein a pharmaceutical compositions containing (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid.

Provided herein are processes, compounds and compositions for making (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid. Also provided herein a pharmaceutical compositions containing (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid.

Herein described are deuterated catecholamine derivatives of the general Formula I

##STR00001##

wherein, R.sub.1 is deuterium, R.sub.2, and R.sub.3 are independently selected from hydrogen and deuterium and wherein at least one of R.sub.2 and R.sub.3 has a deuterium enrichment in the range from 0.02 mol % to 100 mol % deuterium, and wherein the deuterium enrichment of R.sub.2 and R.sub.3 is different from each other and that the difference between the deuterium enrichment of R.sub.2 and R.sub.3 is at least 5 percentage points, R.sub.4 is hydrogen, deuterium, C.sub.1 to C.sub.6-alkyl or C.sub.5 to C.sub.6-cycloalkyl, deuterated C.sub.1 to C.sub.6-alkyl or C.sub.5 to C.sub.6-cycloalkyl, or a group that is easily hydrolytically or enzymatically cleavable under physiological conditions, as well as their physiologically acceptable salts and their stereoisomers, enantiomers or diastereomers in optically pure form. The compounds can easily be prepared by mixing deuterated and non-deuterated compounds in a predefined ratio. The compounds show anti-Parkinson effect at lower doses and show lower side effects.

Herein described are deuterated catecholamine derivatives of the general Formula I

##STR00001##

wherein, R.sub.1 is deuterium, R.sub.2, and R.sub.3 are independently selected from hydrogen and deuterium and wherein at least one of R.sub.2 and R.sub.3 has a deuterium enrichment in the range from 0.02 mol % to 100 mol % deuterium, and wherein the deuterium enrichment of R.sub.2 and R.sub.3 is different from each other and that the difference between the deuterium enrichment of R.sub.2 and R.sub.3 is at least 5 percentage points, R.sub.4 is hydrogen, deuterium, C.sub.1 to C.sub.6-alkyl or C.sub.5 to C.sub.6-cycloalkyl, deuterated C.sub.1 to C.sub.6-alkyl or C.sub.5 to C.sub.6-cycloalkyl, or a group that is easily hydrolytically or enzymatically cleavable under physiological conditions, as well as their physiologically acceptable salts and their stereoisomers, enantiomers or diastereomers in optically pure form. The compounds can easily be prepared by mixing deuterated and non-deuterated compounds in a predefined ratio. The compounds show anti-Parkinson effect at lower doses and show lower side effects.

Disclosed in the present invention are an aromatic vinyl or aromatic ethyl derivative, a preparation method therefor, an intermediate, a pharmaceutical composition, and an application. The aromatic vinyl or aromatic ethyl derivative in the present invention is as represented by general formula (I). The aromatic vinyl or aromatic ethyl derivative in the present invention has an obvious inhibitory effect on PD-1/PD-L1, is a very effective small-molecule PD-1/PD-L1 inhibitor, and can effectively alleviate or treat relevant diseases such as cancer.

##STR00001##

Disclosed in the present invention are an aromatic vinyl or aromatic ethyl derivative, a preparation method therefor, an intermediate, a pharmaceutical composition, and an application. The aromatic vinyl or aromatic ethyl derivative in the present invention is as represented by general formula (I). The aromatic vinyl or aromatic ethyl derivative in the present invention has an obvious inhibitory effect on PD-1/PD-L1, is a very effective small-molecule PD-1/PD-L1 inhibitor, and can effectively alleviate or treat relevant diseases such as cancer.

##STR00001##

The present invention relates to a conjugate salt of N,N-dimethylglycine with metal and organic acid, and a preparation method and use thereof. The conjugate salt of N,N-dimethylglycine with metal and organic acid has a following structural formula: [(CH.sub.3).sub.2NCH.sub.2COO].sub.nM.[Organic acid], wherein, n is 1 or 2; M is selected from an alkali metal ion or a divalent metal ion; the organic acid is selected from an organic polyacid, a C.sub.2-C.sub.18 linear fatty acid or an aromatic acid. The conjugate salt of N,N-dimethylglycine with metal and organic acid is a conjugate acid salt formed by introducing another organic acid with a hydrophobic group into the salt of N,N-dimethylglycine and a metal ion, so as to modify the hygroscopicity of N,N-dimethylglycine by decreasing the affinity of the salt toward water molecules in the air, or decreasing the affinity or attraction of molecular aggregates formed through crystalline behavior of the salt toward water molecules in the air.

The invention relates to a process for the preparation of one or more intermediate chemical compounds useful in the preparation of non-ionic contrast agents wherein the process is carried out continuously using one or more flow procedures.

The invention relates to a process for the preparation of one or more intermediate chemical compounds useful in the preparation of non-ionic contrast agents wherein the process is carried out continuously using one or more flow procedures.

The invention relates to a process for the preparation of one or more intermediate chemical compounds useful in the preparation of non-ionic contrast agents wherein the process is carried out continuously using one or more flow procedures.