Provided are a long-acting prodrug of Entecavir, preparation method and use thereof, wherein the prodrug of Entecavir has a structure of formula I. The prodrug of Entecavir can be released slowly, sustainably and steady, and converted to active compound of Entecavir to achieve a long-acting effect.

This invention is directed to synthetic co-crystals of anhydrous guanine and at least one additional material, wherein the co-crystals have a high refraction index and therefore, provide products with pearlescence or whiteness with high coverage. The invention is further directed to a process for the preparation of anhydrous guanine and of the co crystals.

This invention is directed to synthetic co-crystals of anhydrous guanine and at least one additional material, wherein the co-crystals have a high refraction index and therefore, provide products with pearlescence or whiteness with high coverage. The invention is further directed to a process for the preparation of anhydrous guanine and of the co crystals.

Provided are a novel compound having an antagonistic activity for the P2X.sub.7 receptor, and a pharmaceutical composition having an antagonistic activity for the P2X.sub.7 receptor. A compound represented by Formula (I):

##STR00001##

wherein Z.sup.1 is C(R.sup.4) or the like; R.sup.4 is a hydrogen atom or the like; Z.sup.2 is C(R.sup.5a)(R.sup.5a′) or the like; the dashed line represents the presence or absence of a bond; when the dashed line represents the presence of a bond, then R.sup.5a′ is absent; R.sup.5a and R.sup.5a′ are each independently a hydrogen atom or the like; Ring Q is a substituted or unsubstituted 5-membered non-aromatic heterocycle or the like; Y.sup.1 is O or the like; R.sup.2a is a group represented by the formula: —(C(R.sup.2a′)(R.sup.2b′)).sub.n—R.sup.1; R.sup.2b is a hydrogen atom or the like; R.sup.2a′ and R.sup.2b′ is each independently a hydrogen atom or the like; R.sup.1 is substituted or unsubstituted aromatic carbocyclyl or the like; X is N(R.sup.7a) or the like; R.sup.7a is a hydrogen atom or the like; R.sup.3 is substituted or unsubstituted aromatic carbocyclyl or the like; n is an integer from 0 to 4; and m is an integer from 0 to 4, or a pharmaceutically acceptable salt thereof.

Provided are a novel compound having an antagonistic activity for the P2X.sub.7 receptor, and a pharmaceutical composition having an antagonistic activity for the P2X.sub.7 receptor. A compound represented by Formula (I):

##STR00001##

wherein Z.sup.1 is C(R.sup.4) or the like; R.sup.4 is a hydrogen atom or the like; Z.sup.2 is C(R.sup.5a)(R.sup.5a′) or the like; the dashed line represents the presence or absence of a bond; when the dashed line represents the presence of a bond, then R.sup.5a′ is absent; R.sup.5a and R.sup.5a′ are each independently a hydrogen atom or the like; Ring Q is a substituted or unsubstituted 5-membered non-aromatic heterocycle or the like; Y.sup.1 is O or the like; R.sup.2a is a group represented by the formula: —(C(R.sup.2a′)(R.sup.2b′)).sub.n—R.sup.1; R.sup.2b is a hydrogen atom or the like; R.sup.2a′ and R.sup.2b′ is each independently a hydrogen atom or the like; R.sup.1 is substituted or unsubstituted aromatic carbocyclyl or the like; X is N(R.sup.7a) or the like; R.sup.7a is a hydrogen atom or the like; R.sup.3 is substituted or unsubstituted aromatic carbocyclyl or the like; n is an integer from 0 to 4; and m is an integer from 0 to 4, or a pharmaceutically acceptable salt thereof.

The present invention is generally directed to novel fluorophores and their use in imaging methods. In one case, the present invention provides a compound according to the structure shown in FIG. 20A. In another case, the present invention provides a method of imaging one or more cellular structures within one or more cells using a compound of the structure shown in FIG. 20A.

The present invention is generally directed to novel fluorophores and their use in imaging methods. In one case, the present invention provides a compound according to the structure shown in FIG. 20A. In another case, the present invention provides a method of imaging one or more cellular structures within one or more cells using a compound of the structure shown in FIG. 20A.

The present invention relates to an alkoxyphenyl derivative capable of synthesizing an oligonucleotide by a quicker liquid phase synthesis method than in the prior art, a protected nucleoside and a protected nucleotide to which the alkoxyphenyl derivative is bonded, a method for producing an oligonucleotide using the same, and a method for selectively removing the alkoxyphenyl derivative moiety and the like. A compound represented by the general formula (1) or a derivative thereof:

##STR00001##

(In the formula, R each independently represents an optionally substituted alkyl group having 10 to 40 carbons. m represents an integer between 1 and 5. When m is 2 or more, a plurality of ROs may be the same or different. X represents O, S, NH, or NR.sup.N. n represents an integer from 1 to 4. R.sup.N represents an optionally substituted alkyl group having 1 to 6 carbons.)

The present invention provides a method for obtaining a specifically-shaped crystal (specifically, spherocrystal) of a compound with good reproducibility. This method for producing a specifically-shaped crystal (specifically spherocrystal) of a compound comprises: (1) a step for preparing a supersaturated solution of a compound having a degree of supersaturation equal to or higher than a critical degree of supersaturation; and (2) a step for precipitating a specifically-shaped crystal (specifically spherocrystal) of a compound from the supersaturated solution.

To provide a chiral reagent or a salt thereof. The chiral reagent has following chemical formula (I). In the formula (I), G.sup.1 and G.sup.2 are independently a hydrogen atom, a nitro group (—NO.sub.2), a halogen atom, a cyano group (—CN), a group of formula (II) or (III), or both G.sup.1 and G.sup.2 taken together to form a group of formula (IV). ##STR00001##