The invention provides compositions or pharmaceutical compositions of novel high penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. For example, HPCs of NSAIA have demonstrated indications such as treating hair loss and bold. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

The invention provides compositions or pharmaceutical compositions of novel high penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. For example, HPCs of NSAIA have demonstrated indications such as treating hair loss and bold. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

The present invention features a compound of formula I:

##STR00001##

or a pharmaceutically acceptable salt thereof, where R.sub.1, R.sub.2, R.sub.3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.

The present invention features a compound of formula I:

##STR00001##

or a pharmaceutically acceptable salt thereof, where R.sub.1, R.sub.2, R.sub.3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.

A process for preparing and purifying a compound of Formula I is provided:

##STR00001##

thereof, wherein the subscript m is an integer of from 0 to 3; each R.sup.a is independently selected from the group consisting of (C.sub.3-C.sub.8)cycloalkyl, (C.sub.1-C.sub.4)haloalkyl, halogen, —OH, —OR.sup.1, —SH, —SR.sup.1, —S(O)R.sup.1, —S(O).sub.2R.sup.1, —SO.sub.2NH.sub.2, —C(O)NH.sub.2, —C(O)NHR.sup.1, —C(O)N(R.sup.1).sub.2, —C(O)R.sup.1, —C(O)H, —CO.sub.2H, —CO.sub.2R.sup.1, —NO.sub.2, —NH.sub.2, —NHR.sup.1, —N(R.sup.1).sub.2, wherein each R.sup.1 is independently (C.sub.1-C.sub.8)alkyl; L is a linking group selected from the group consisting of a bond or CH.sub.2; Q.sup.a, Q.sup.b, and Q.sup.c are each members independently selected from the group consisting of N, S, O and C(R.sup.q) wherein each R.sup.q is independently selected from the group consisting of H, C.sub.1-8 alkyl, halo and phenyl, and the ring having Q.sup.a, Q.sup.b, Q.sup.c and Y as ring vertices is a five-membered ring having two double bonds; and
Y is selected from the group consisting of C and N.

A process for preparing and purifying a compound of Formula I is provided:

##STR00001##

thereof, wherein the subscript m is an integer of from 0 to 3; each R.sup.a is independently selected from the group consisting of (C.sub.3-C.sub.8)cycloalkyl, (C.sub.1-C.sub.4)haloalkyl, halogen, —OH, —OR.sup.1, —SH, —SR.sup.1, —S(O)R.sup.1, —S(O).sub.2R.sup.1, —SO.sub.2NH.sub.2, —C(O)NH.sub.2, —C(O)NHR.sup.1, —C(O)N(R.sup.1).sub.2, —C(O)R.sup.1, —C(O)H, —CO.sub.2H, —CO.sub.2R.sup.1, —NO.sub.2, —NH.sub.2, —NHR.sup.1, —N(R.sup.1).sub.2, wherein each R.sup.1 is independently (C.sub.1-C.sub.8)alkyl; L is a linking group selected from the group consisting of a bond or CH.sub.2; Q.sup.a, Q.sup.b, and Q.sup.c are each members independently selected from the group consisting of N, S, O and C(R.sup.q) wherein each R.sup.q is independently selected from the group consisting of H, C.sub.1-8 alkyl, halo and phenyl, and the ring having Q.sup.a, Q.sup.b, Q.sup.c and Y as ring vertices is a five-membered ring having two double bonds; and
Y is selected from the group consisting of C and N.

A nitrogen-containing ring derivative regulator, a preparation method therefor and use thereof. In particular, the present invention relates to a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and use thereof as a G protein-coupled receptor regulator in the treatment or prevention of central nervous system diseases and/or mental diseases.

##STR00001##

The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I) and to the use of compounds of Formula (I) for controlling weeds, in particular in crops of useful plants.

##STR00001##

Disclosed in the present invention are a substituted nitrogen heterocyclic compound and anesthetic action thereof. Specifically provided a chemical compound as shown in formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, a prodrug thereof, a metabolite thereof or a deuterated derivative thereof. The substituted nitrogen heterocyclic compound provided in the present application has good central nervous system inhibition effects, capable of generating sedative, hypnotic and/or general anesthetic effects, and capable of controlling status epilepticus; said substituted nitrogen heterocyclic compound is also characterized by rapid onset of action and rapid recovery, while maintaining positive anesthetic activity; in addition, said substituted nitrogen heterocyclic compound has almost no inhibitory effect on adrenocortical function, low side effects, and resolves technical difficulties in the art. The present invention provides a new selection for clinical screening and/or preparation of sedative, hypnotic and/or general anesthetic drugs and drugs controlling status epilepticus.

Disclosed in the present invention are a substituted nitrogen heterocyclic compound and anesthetic action thereof. Specifically provided a chemical compound as shown in formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, a prodrug thereof, a metabolite thereof or a deuterated derivative thereof. The substituted nitrogen heterocyclic compound provided in the present application has good central nervous system inhibition effects, capable of generating sedative, hypnotic and/or general anesthetic effects, and capable of controlling status epilepticus; said substituted nitrogen heterocyclic compound is also characterized by rapid onset of action and rapid recovery, while maintaining positive anesthetic activity; in addition, said substituted nitrogen heterocyclic compound has almost no inhibitory effect on adrenocortical function, low side effects, and resolves technical difficulties in the art. The present invention provides a new selection for clinical screening and/or preparation of sedative, hypnotic and/or general anesthetic drugs and drugs controlling status epilepticus.