The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

A compound of formula (I) ##STR00001##
wherein X is 0, C=0 or S; Y is N or CH; R.sub.2 and R.sub.4 are each independently H, —(CH.sub.2).sub.pCOOH, —(CH.sub.2).sub.pCON(R.sup.5).sub.2 or —(CH.sub.2).sub.pCOOC.sub.1-6alkyl; or R.sub.2 and R.sub.4 together form a 6-membered phenyl ring fused to the five membered ring; each R.sub.1 is independently selected from H, halo (e.g. fluoro or chloro), C.sub.6-10aryl, C.sub.7-12arylalkyl, C.sub.2-12 alkenyl; OC.sub.1-12 alkyl, OC.sub.2-12 alkenyl or a C.sub.1-12 alkyl group; each R.sup.5 is H or C.sub.1-6 alkyl; each p is 0 to 3; n is 1 to 4; or a salt, ester, solvate, N-oxide, or prodrug thereof, e.g. a salt thereof.

A compound of formula (I) ##STR00001##
wherein X is 0, C=0 or S; Y is N or CH; R.sub.2 and R.sub.4 are each independently H, —(CH.sub.2).sub.pCOOH, —(CH.sub.2).sub.pCON(R.sup.5).sub.2 or —(CH.sub.2).sub.pCOOC.sub.1-6alkyl; or R.sub.2 and R.sub.4 together form a 6-membered phenyl ring fused to the five membered ring; each R.sub.1 is independently selected from H, halo (e.g. fluoro or chloro), C.sub.6-10aryl, C.sub.7-12arylalkyl, C.sub.2-12 alkenyl; OC.sub.1-12 alkyl, OC.sub.2-12 alkenyl or a C.sub.1-12 alkyl group; each R.sup.5 is H or C.sub.1-6 alkyl; each p is 0 to 3; n is 1 to 4; or a salt, ester, solvate, N-oxide, or prodrug thereof, e.g. a salt thereof.

The present invention relates to novel 2-[thiophen-2-yl)formamido]-N-(phenyl)-2-methylpropanamides of formula A ##STR00001##
and pharmaceutically acceptable salts thereof, wherein R.sup.1 to R.sup.3 are as defined herein. The invention also relates to processes for the preparation of these compound, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions in which inhibition of the indoleamine 2,3-dioxygenase 1 (IDO1) enzyme may be beneficial.

The present invention relates to novel 2-[thiophen-2-yl)formamido]-N-(phenyl)-2-methylpropanamides of formula A ##STR00001##
and pharmaceutically acceptable salts thereof, wherein R.sup.1 to R.sup.3 are as defined herein. The invention also relates to processes for the preparation of these compound, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions in which inhibition of the indoleamine 2,3-dioxygenase 1 (IDO1) enzyme may be beneficial.

Provided herein are novel synthetic compounds having the structure of formula (1),

##STR00001##

wherein X is a substituted or unsubstituted aromatic or heteroaromatic mono- or polycyclic ring system; and Y is substituted or unsubstituted C.sup.5-C.sup.10 alkyl or alkenyl group, or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions. The compounds and pharmaceutical compositions are useful for inhibiting growth of a bacterium.

Provided herein are novel synthetic compounds having the structure of formula (1),

##STR00001##

wherein X is a substituted or unsubstituted aromatic or heteroaromatic mono- or polycyclic ring system; and Y is substituted or unsubstituted C.sup.5-C.sup.10 alkyl or alkenyl group, or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions. The compounds and pharmaceutical compositions are useful for inhibiting growth of a bacterium.

Compositions and methods based on the use of mutated HIV-1 gp120 polypeptides having amino acid substitutions at positions 61, 105, 108, 375, 474, 475 and 476 are described. These mutated HIV-1 gp120 polypeptides, which make the HIV env protein more amenable to adopt specific conformations when contacted with gp120 ligands, may be useful as vaccines or tools to identify and characterize agents modulating HIV infection.

Compositions and methods based on the use of mutated HIV-1 gp120 polypeptides having amino acid substitutions at positions 61, 105, 108, 375, 474, 475 and 476 are described. These mutated HIV-1 gp120 polypeptides, which make the HIV env protein more amenable to adopt specific conformations when contacted with gp120 ligands, may be useful as vaccines or tools to identify and characterize agents modulating HIV infection.