The present disclosure relates to prodrugs, double prodrugs, derivatives and analogues of 3-(methylamino)-2-((methylamino)methyl)propane-1-thiol. Their use as radio- and chemo-protectors is also described.

The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

Pharmaceutical compositions of the invention comprise functionalized bicyclic carboxamide useful as pregenomic RNA encapsidation inhibitors, useful for the treatment of Hepatitis B virus (HBV) infection.

Object of the present invention is an improved process for the preparation of cyclopropyldiketopiperazines and thereof key intermediates.

Object of the present invention is an improved process for the preparation of cyclopropyldiketopiperazines and thereof key intermediates.

According to the present invention, as a monomer which is unlikely to be crystallized in a curable composition for manufacturing an optical member and which enables manufacture of a cured product having a high level of moisture-heat resistance, a compound represented by General Formula (A) is provided. ##STR00001## In the formula, Ar.sup.11 and Ar.sup.12 each independently represent an aryl group or a heteroaryl group; X.sup.1, Y.sup.1, X.sup.2, Y.sup.2, Z.sup.1, and Z.sup.2 each independently represent a nitrogen atom or a carbon atom, or the like; Ar.sup.13 and Ar.sup.14 each independently represent an arylene group or a heteroarylene group, where at least one of Ar.sup.13 or Ar.sup.14 is a group other than a phenylene group; R.sup.3 to R.sup.6 each independently represent a substituent, q and r each independently are an integer of 0 to 4, and v and w each independently are an integer of 0 or more; L.sup.1 and L.sup.2 each independently represent a single bond, an oxygen atom, an ester bond, or the like; R.sup.11 and R.sup.12 each independently represent a divalent linking group containing a branched alkylene group; and R.sup.21 and R.sup.22 each independently represent a hydrogen atom or a methyl group.

According to the present invention, as a monomer which is unlikely to be crystallized in a curable composition for manufacturing an optical member and which enables manufacture of a cured product having a high level of moisture-heat resistance, a compound represented by General Formula (A) is provided. ##STR00001## In the formula, Ar.sup.11 and Ar.sup.12 each independently represent an aryl group or a heteroaryl group; X.sup.1, Y.sup.1, X.sup.2, Y.sup.2, Z.sup.1, and Z.sup.2 each independently represent a nitrogen atom or a carbon atom, or the like; Ar.sup.13 and Ar.sup.14 each independently represent an arylene group or a heteroarylene group, where at least one of Ar.sup.13 or Ar.sup.14 is a group other than a phenylene group; R.sup.3 to R.sup.6 each independently represent a substituent, q and r each independently are an integer of 0 to 4, and v and w each independently are an integer of 0 or more; L.sup.1 and L.sup.2 each independently represent a single bond, an oxygen atom, an ester bond, or the like; R.sup.11 and R.sup.12 each independently represent a divalent linking group containing a branched alkylene group; and R.sup.21 and R.sup.22 each independently represent a hydrogen atom or a methyl group.

Provided are a compound represented by the following General Formula (A1-1), a method for producing the same, and the use of the compound:

##STR00001##

wherein R.sup.5 and R.sup.6 represent a hydrogen atom or an alkyl group, L.sup.1 and L.sup.2 represent an alkylene group having 1 to 6 carbon atoms, Sp.sup.a and Sp.sup.b represent a single bond or a divalent linking group, R.sup.11 and R.sup.21 represent a substituent, and v1 and w1 are an integer of 0 to 4. Further provided that a structure represented by (R.sup.11).sub.v1-benzen ring/cyclopentadiene skeleton/naphthalene ring-(R.sup.21).sub.w1 is not line-symmetrical, where “/” represents that two rings described on left and right sides of the structure are fused.

The present invention relates to compounds of formula I: in which A.sup.1-A.sup.7 and R.sup.1 to R.sup.5 are defined herein, for use in the treatment of a condition or disease which is alleviated by the activation of retinoic acid receptors (RAR). The invention also relates to pharmaceutical compounds comprising such compounds, and related methods of treatment. In an aspect, the invention relates to a method of screening compounds for therapeutic potential in the treatment of a condition or disease which is alleviated by the activation of retinoic acid receptors (RAR). Aspects of the invention relate to novel compounds of formula I in which at least one of A.sup.1 to A.sup.3 is or at least one of A.sup.4 is CR.sup.12 or A.sup.5 is CR.sup.13 in which R.sup.12/R.sup.13 is halogen.