Patent classifications
C07D317/32
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.
ROR gamma (RORγ) modulators
Compounds according to Formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof wherein: A.sub.1 is NR.sub.1 or CR.sub.1, with R.sub.1 being H or methyl, with methyl, if present, optionally being substituted with one or more F; the cyclopropyl moiety can be optionally substituted with one or more methyl and one or more F; A.sub.2-A.sub.5 are N or CR.sub.2-CR.sub.5, respectively, with the proviso that no more than two of the four positions A in A.sub.2-A.sub.5 can be simultaneously N; R.sub.2-R.sub.5 are independently H, halogen, amino, C(1-3)alkoxy, (di)C(1-3)alkylamino or C(1-6)alkyl; R.sub.6 and R.sub.7 are independently H, F, methyl, ethyl, hydroxyl or methoxy or R.sub.2 and R.sub.3 together is carbonyl, all alkyl groups, if present, optionally being substituted with one or more F; R.sub.8 is H or C(1-6)alkyl; R.sub.9 is selected from the group consisting of Formula II, III, IV and V ##STR00002## The compounds can be used as inhibitors of ROR and are useful for the treatment of ROR mediated diseases.
Anthracycline Derivatives For Treating Tumor Diseases
The invention relates to anthracycline derivative compounds for treating tumor diseases, and related methods, compositions, and kits.
Anthracycline Derivatives For Treating Tumor Diseases
The invention relates to anthracycline derivative compounds for treating tumor diseases, and related methods, compositions, and kits.
MANUFACTURING METHOD OF 1,4-DIOXANE DERIVATIVE, 1,4-DIOXANE DERIVATIVE, COMPOSITION CONTAINING 1,4-DIOXANE DERIVATIVE, AND MANUFACTURING METHOD OF (1,3-DIOXOLANE)-2- CARBOXYLIC ACID DERIVATIVE, (1,3-DIOXOLANE)-2-CARBOXYLIC ACID DERIVATIVE, AND COMPOSITION CONTAINING (1,3-DIOXOLANE)-2-CARBOXYLIC ACID DERIVATIVE
The manufacturing method of the 1,4-dioxane derivative represented by Formula (2) and/or Formula (10) includes reacting water, an inorganic base, and a fluoroalkene oxide represented by Formula (1). The manufacturing method of the (1,3-dioxolane)-2-carboxylic acid derivative includes manufacturing the 1,4-dioxane derivative represented by Formula (2) and/or Formula (10) by the above manufacturing method and a manufacturing method of the (1,3-dioxolane)-2-carboxylic acid derivative includes manufacturing the 1,4-dioxane derivative represented by Formula (2) and/or Formula (10) comprising ring reduction under heating. In Formula (1), R represents a fluorine atom or a fluoroalkyl group. In Formula (2) and in Formula (10), R represents a fluorine atom or a fluoroalkyl group, two R's present are the same as or different from each other, and M.sup.+ represents a counter cation.
##STR00001##
MANUFACTURING METHOD OF 1,4-DIOXANE DERIVATIVE, 1,4-DIOXANE DERIVATIVE, COMPOSITION CONTAINING 1,4-DIOXANE DERIVATIVE, AND MANUFACTURING METHOD OF (1,3-DIOXOLANE)-2- CARBOXYLIC ACID DERIVATIVE, (1,3-DIOXOLANE)-2-CARBOXYLIC ACID DERIVATIVE, AND COMPOSITION CONTAINING (1,3-DIOXOLANE)-2-CARBOXYLIC ACID DERIVATIVE
The manufacturing method of the 1,4-dioxane derivative represented by Formula (2) and/or Formula (10) includes reacting water, an inorganic base, and a fluoroalkene oxide represented by Formula (1). The manufacturing method of the (1,3-dioxolane)-2-carboxylic acid derivative includes manufacturing the 1,4-dioxane derivative represented by Formula (2) and/or Formula (10) by the above manufacturing method and a manufacturing method of the (1,3-dioxolane)-2-carboxylic acid derivative includes manufacturing the 1,4-dioxane derivative represented by Formula (2) and/or Formula (10) comprising ring reduction under heating. In Formula (1), R represents a fluorine atom or a fluoroalkyl group. In Formula (2) and in Formula (10), R represents a fluorine atom or a fluoroalkyl group, two R's present are the same as or different from each other, and M.sup.+ represents a counter cation.
##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.
Anthracycline derivatives for treating tumor diseases
The invention relates to anthracycline derivative compounds for treating tumor diseases, and related methods, compositions, and kits. ##STR00001##
Anthracycline derivatives for treating tumor diseases
The invention relates to anthracycline derivative compounds for treating tumor diseases, and related methods, compositions, and kits. ##STR00001##
PEG lipids and uses thereof
The present disclosure in part provides compounds (i.e., PEG lipids) which are useful in pharmaceutical compositions, cosmetic compositions, and drug delivery systems, e.g, for use in lipid nanoparticle (LNP) formulations. The present disclosure also provides LNP formulations comprising PEG lipids described herein, and methods of using the same. For example, the LNPs provided herein are useful for the delivery of an agent (e.g, therapeutic agent) to a subject. The PEG lipids and LNPs provided herein, in certain embodiments, exhibit increased PEG shedding compared to existing PEG lipids and LNP formulations.