Novel methods of synthesis of ethylenedicysteine-sugar conjugates and therapeutic and diagnostic applications of such conjugates are disclosed. Methods of synthesizing these conjugates in high purity are also presented as using starting materials such as thiazolidine carboxylic acid. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these conjugates prepared herein, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

This disclosure provides functional templates that direct Pd to functionalize multiple CH bonds in polycyclic aza-arenes such as quinolines and related heterocycles at locations that are difficult to isolate and reach for substitution. Herein disclosed are two conceptually distinct directing templates (T) that enable site-selective C6 and C7-H activation of polycyclic aza-arenes. These catalytic pyridine-based templates recruit the aza-arene substrate through N-coordination, enabling the directing arm to deliver the catalyst and precisely activate remote and adjacent C6 or C7-H bond (FIG. 1d). In parallel, we discovered that the use of a simple and readily prepared template chaperone (TC) can turn over the directing template, allowing it to be used catalytically for the first time. Notably, chiral recognition is vital in the granular discrimination between competing C3 and C7-H bonds when the differentiation via distance and geometry is insufficient. Thus, precise recognition of a directing template's distance, geometry and chirality now enables the iterative CH editing of quinoline and related pharmacophores at any desired site and order. The methods disclosed herein can also be used for diverse and late-stage modification of heterocycle-based drug molecules and pharmacophores.

A method for preparing high-purity granatin A: by means of a combination of low-temperature liquid phase chromatography and an isomerization conversion purification method, using pomegranate peel extract as a source material, granatin A of over 98% purity can be acquired, and can be used as a standard product for quality control of pomegranate peel, pomegranate flower, or other medicinal material with granatin A as the active ingredient.

A method for preparing high-purity granatin A: by means of a combination of low-temperature liquid phase chromatography and an isomerization conversion purification method, using pomegranate peel extract as a source material, granatin A of over 98% purity can be acquired, and can be used as a standard product for quality control of pomegranate peel, pomegranate flower, or other medicinal material with granatin A as the active ingredient.

Disclosed are a compound having a neuroprotective effect, a preparation method therefor and a use thereof. Specifically, the compound has the structure shown by formula I, the definition of each group and substituent being as described in the description. Further disclosed are a preparation method for the compound and a use thereof for neuroprotection. ##STR00001##

Disclosed are a compound having a neuroprotective effect, a preparation method therefor and a use thereof. Specifically, the compound has the structure shown by formula I, the definition of each group and substituent being as described in the description. Further disclosed are a preparation method for the compound and a use thereof for neuroprotection. ##STR00001##

The present invention relates to aromatic ring or heteroaromatic ring derivatives, a preparation method therefor and applications thereof in medicine. Specifically, the present invention relates to aromatic ring or heteroaromatic ring derivatives represented by general formula (I), a preparation method therefor and pharmaceutically acceptable salts thereof, as well as a use thereof as therapeutic agents, especially uses as angiotensin II type 2 receptor (AT.sub.2R) antagonists, wherein the definition of each substituent in the general formula (I) is the same as the definition thereof in the description.

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt thereof, or an N-oxide thereof), which are positive allosteric modulators of one or more GABA-A receptors, e.g., which are peripherally restricted, positive allosteric modulators of one or more GABA-A receptors: e.g., which are positive allosteric modulators of one or more GABA-A receptors and which selectively target the peripheral nervous system and organs of the body, and which do not substantially pass through the blood-brain barrier. Said compounds are useful e.g., for the treatment of systemic diseases of the body. e.g., diseases in which modulation of one or more peripherally restricted GABA-A receptors is beneficial (e.g., diseases or disorders which are mediated by GABA-A neuronal activity. This disclosure also features pharmaceutical compositions containing the chemical entities described herein as well as methods of using same for the treatment of systemic diseases of the body.

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt thereof, or an N-oxide thereof), which are positive allosteric modulators of one or more GABA-A receptors, e.g., which are peripherally restricted, positive allosteric modulators of one or more GABA-A receptors: e.g., which are positive allosteric modulators of one or more GABA-A receptors and which selectively target the peripheral nervous system and organs of the body, and which do not substantially pass through the blood-brain barrier. Said compounds are useful e.g., for the treatment of systemic diseases of the body. e.g., diseases in which modulation of one or more peripherally restricted GABA-A receptors is beneficial (e.g., diseases or disorders which are mediated by GABA-A neuronal activity. This disclosure also features pharmaceutical compositions containing the chemical entities described herein as well as methods of using same for the treatment of systemic diseases of the body.