Provided is a method for biocatalytic synthesis of Sitagliptin and intermediates thereof, in particular, provided are compounds of Formula (I) and Formula (II), or pharmaceutically acceptable salts thereof, a polypeptide capable of catalyzing conversion of a compound of Formula (I) to a compound of Formula (II), a nucleic acid encoding the polypeptide, a vector and a cell comprising the nucleic acid. In addition, also provided are a method for producing a compound of Formula (II) and Sitagliptin by using the polypeptide and the compound of Formula (I), and a method for preparing the polypeptide.

The present invention provides bumetanide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide analogs and methods for their use. These analogs are believed useful for the treatment and/or prophylaxis of conditions that involve the Na.sup.+K.sup.+Cl.sup.− co-transporter or GABA.sub.A receptor.

The present invention provides bumetanide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide analogs and methods for their use. These analogs are believed useful for the treatment and/or prophylaxis of conditions that involve the Na.sup.+K.sup.+Cl.sup.− co-transporter or GABA.sub.A receptor.

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:

X-A-Y-L-R  (I)

which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:

X-A-Y-L-R  (I)

which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Provided is a method for biocatalytic synthesis of Sitagliptin and intermediates thereof, in particular, provided are compounds of Formula (I) and Formula (II), or pharmaceutically acceptable salts thereof, a polypeptide capable of catalyzing conversion of a compound of Formula (I) to a compound of Formula (II), a nucleic acid encoding the polypeptide, a vector and a cell comprising the nucleic acid. In addition, also provided are a method for producing a compound of Formula (II) and Sitagliptin by using the polypeptide and the compound of Formula (I), and a method for preparing the polypeptide.

The present invention relates to a novel FXR agonist having a pyrazine structure, a preparation method therefor and the use thereof, and in particular relates to a compound as represented by the following general formula (I), or a hydrate, a solvate or a pharmaceutically acceptable salt thereof or a resolved single isomer thereof, which has the effect of treating non-alcoholic fatty liver disease.

##STR00001##

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:
X-A-Y-L-R(I)
which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:
X-A-Y-L-R(I)
which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

The present invention provides compounds of formula (I): ##STR00001##
wherein
A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are independently of one another CH, CR.sup.5, or nitrogen;
B.sup.1-B.sup.2-B.sup.3-B.sup.4 is CH.sub.2CNCH.sub.2, CH.sub.2NCH.sub.2CH.sub.2, CH.sub.2CCHO or CHCCH.sub.2O;
G.sup.1 is oxygen or sulfur;
L is a single bond or C.sub.1-C.sub.8alkylene;
R.sup.1 is hydrogen, C.sub.1-C.sub.8alkyl, C.sub.1-C.sub.8alkylcarbonyl-, C.sub.1-C.sub.8alkoxy, C.sub.2-C.sub.8alkenyl, C.sub.2-C.sub.8alkynyl, C.sub.1-C.sub.8alkoxy-C.sub.1-C.sub.8alkyl, aryl or aryl substituted by one to three R.sup.6, or R.sup.1 is heterocyclyl or heterocyclyl substituted by one to three R.sup.6 or C.sub.1-C.sub.8alkoxycarbonyl-;
R.sup.2 is hydrogen, C.sub.1-C.sub.8haloalkyl or C.sub.1-C.sub.8alkyl;
R.sup.3 is C.sub.1-C.sub.8haloalkyl;
R.sup.4 is aryl or aryl substituted by one to three R.sup.6, or R.sup.4 is heterocyclyl or heterocyclyl substituted by one to three R.sup.6;
Y.sup.1 is CR.sup.7R.sup.8, CO or CS;
Y.sup.2, Y.sup.3 and Y.sup.4 are independently CR.sup.7R.sup.8, CO, CS, NR.sup.9, O, S, SO or SO.sub.2;
wherein at least two adjacent ring atoms in the ring formed by Y.sup.1, Y.sup.2, Y.sup.3 and Y.sup.4 are heteroatoms;
each R.sup.7 and R.sup.8 is independently hydrogen, halogen, C.sub.1-C.sub.8alkyl, or C.sub.1-C.sub.8haloalkyl;
and R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.