Methods of synthesizing compounds using CO.sub.2 as a directing group for CH functionalization, and compounds made thereby, are described.

Methods of synthesizing compounds using CO.sub.2 as a directing group for CH functionalization, and compounds made thereby, are described.

The present invention relates to the compounds of formula (I) below:

##STR00001##

wherein: X represents an oxygen atom, a sulfur atom, a nitrogen atom or a CH radical, The bond XY and Y are absent if X represents an oxygen or sulfur atom, the bond XY and Y are present if X represents a nitrogen atom or a CH radical, When present, Y represents a group R if X represents a nitrogen atom, a hydrogen atom or a group NR.sup.1R.sup.2 if X represents a CH radical, (Het)Ar is an aromatic ring selected from the group consisting of aryl and heteroaryl groups, R.sup.3, R.sup.4, R.sup.5, R.sup.6 represent, independently of one another, a hydrogen atom, a halogen atom, a NR.sup.12R.sup.13, a SR.sup.14 group, a OR.sup.14 group or a CF.sub.3 group, When Y is NR.sup.1R.sup.2, the groups NR.sup.1R.sup.2 and (Het)Ar are in the cis-conformation,
or a pharmaceutically acceptable salt thereof,
for use in the treatment of proliferative diseases, infectious diseases, allergies, inflammation and/or asthma.

Provided are a long-acting prodrug of Rasagiline, which has application in the treatment of Central Nervous System diseases such as Parkinson's disease, preparation method and use thereof. The long-acting prodrug of Rasagiline has a structure of formula (I), wherein T is absent, or T is selected from

##STR00001##

each of R.sub.1 and R.sub.2 is independently selected from H, D, and alkyl; W is absent, or W is selected from (CH.sub.2).sub.n, wherein n is an integer selected from 1 to 15; X is absent, or X is selected from (CH.sub.2).sub.m, wherein m is an integer selected from 1 to 10; Y is absent, or Y is selected from C(O)NH, NHC(O); R.sub.3 is selected from substituted or unsubstituted C.sub.1-C.sub.30 alkyl, substituted or unsubstituted C.sub.2-C.sub.30 alkenyl, substituted or unsubstituted C.sub.2-C.sub.30 alkynyl, substituted or unsubstituted C.sub.3-C.sub.30 cycloalkyl, cholane aliphatic group, R.sup.3aC(O)OR.sup.3b, R.sup.3aOC(O)R.sup.3b, R.sup.3aC(O)NHR.sup.3b, R.sup.3aNHC(O)R.sup.3b, R.sup.3aS(O).sub.1-2OR.sup.3b and R.sup.3aOS(O).sub.1-2R.sup.3b.

##STR00002##

Aspects of the present disclosure include G6PD-modulating agents and methods for modulating a glucose-6-phosphate dehydrogenase (G6PD) in a sample using such agents. A G6PD-modulating agent can be dimeric and include two terminal carbocyclic or heterocyclic groups connected via a linker. In some instances, the agent includes a diamino-containing linker. In certain cases, the agent includes two amino substituents. Also provided are methods for treating a subject for a G6PD deficiency-associated condition, that include administering to a subject an effective amount of a G6PD-modulating agent to selectively activate a mutant G6PD and treat the subject. Kits and compositions for practicing the subject methods are also provided.

Aspects of the present disclosure include G6PD-modulating agents and methods for modulating a glucose-6-phosphate dehydrogenase (G6PD) in a sample using such agents. A G6PD-modulating agent can be dimeric and include two terminal carbocyclic or heterocyclic groups connected via a linker. In some instances, the agent includes a diamino-containing linker. In certain cases, the agent includes two amino substituents. Also provided are methods for treating a subject for a G6PD deficiency-associated condition, that include administering to a subject an effective amount of a G6PD-modulating agent to selectively activate a mutant G6PD and treat the subject. Kits and compositions for practicing the subject methods are also provided.

The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C disorders, including diseases and disorders mediated by GPCRs.

The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C disorders, including diseases and disorders mediated by GPCRs.

Bifunctional molecules having first and second alpha-synuclein binding agents coupled by a linker are disclosed. The bifunctional molecules have potential utility in the diagnosis, treatment and/or prophylaxis of disorders in which alpha-synuclein is implicated, including Parkinson's disease. Methods of making and using the bifunctional molecules are disclosed.

This invention relates to, in part, compositions and methods that are useful for, inter alia, the treatment of various diseases, including those linked to binding at a serotonin receptor in the GI tract.