C07C2602/50

Hepatitis B antiviral agents

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.

C-glycoside derivative

The present invention involves a compound represented by general formula (I), a derivative thereof and a use thereof: ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c and X are defined as in the description.

TETRACYCLINE COMPOUNDS

The present invention is directed to a compound represented by Structural Formula (I):

##STR00001##

or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein.

Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.

Process for preparing spirogalbanone
10227280 · 2019-03-12 · ·

A method of making spirogalbanone includes the steps of: (a) subjecting ethynylspirodecanol to a Rupe rearrangement to give a compound of the formula I ##STR00001## (b) converting the compound of (a) to a C1-C4 alkyl acetal; (c) subjecting the acetal to a trans-acetalization reaction with allyl alcohol in the presence of a mild acid catalyst; (d) heating the product of (c) in the presence of an acid catalyst to give an allylenolether; and (e) subjecting the product of (d) to a Claisen rearrangement to give spirogalbanone. The method affords an easier and more efficient method of preparation.

Cyclopropanation of substituted alkenes

Disclosed is a cyclopropanation process comprising the step of reacting an alkene compound having at least one carbon-carbon double bond with at least one dihaloalkane. The reaction is carried out in the presence of (i) particulate metal Zn, (ii) catalytically effective amount of particulate metal Cu or a salt thereof, (iii) at least one haloalkylsilane, and (iv) at least one solvent.

ANALGESIC COMPOUNDS

Disclosed herein are compounds of Formula (I), methods of synthesizing compounds of Formula (I), and methods of using compounds of Formula (I) as an analgesic.

##STR00001##

HEPATITIS B ANTIVIRAL AGENTS

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.

Process For Preparing Spirogalbanone
20190055181 · 2019-02-21 ·

A method of making spirogalbanone includes the steps of: (a) subjecting ethynylspirodecanol to a Rupe rearrangement to give a compound of the formula I

##STR00001## (b) converting the compound of (a) to a C1-C4 alkyl acetal; (c) subjecting the acetal to a trans-acetalisation reaction with allyl alcohol in the presence of a mild acid catalyst; (d) heating the product of (c) in the presence of an acid catalyst to give an allylenolether; and (e) subjecting the product of (d) to a Claisen rearrangement to give spirogalbanone.

The method affords an easier and more efficient method of preparation.

COMPOUNDS

A compound of the formula (I)

##STR00001##

in which, independently, R.sub.1 is selected from H and methyl; R.sub.2 is selected from H, and methyl; R.sub.3 is selected from H, methyl and ethyl; R.sub.4 is selected from H, methyl and ethyl; or R.sub.3 and R.sub.4 together form a ring in which n is 1 or 2.

The compounds have the characteristic desirable odour qualities of the Damascone molecules, but lack their disadvantageous skin sensitization effects.

SUBSTITUTED CYCLOPENTYL- AND CYCLOHEXYL-DERIVATIVES USEFUL FOR PERFUMERY
20180346412 · 2018-12-06 ·

The present invention refers to substituted cyclopentyl- and cyclohexyl-derivatives of formula (I)

##STR00001## wherein n, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the same meaning as given in the description.

The invention further refers to fragrance compositions and fragranced articles comprising them.