Alpha helix mimetics and methods relating thereto

A compound having the following general formula (II):

• wherein
• is single bond or double bond;
• A is —CHR7—,
• wherein
• R7 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted cycloalkylalkyl or optionally substituted heterocycloalkylalkyl;
• B is optionally substituted 3-, 4-, 5-, 6- or 7- membered saturated or unsaturated monocyclic carbocyclic ring formed together with G and Y, or is optionally substituted 4-, 5-, 6- or 7 membered saturated or unsaturated heterocyclic ring formed together with G and Y and the hetero atom is selected from S, N and O and the number of hetero atoms is an integer of 1-3;
• G and Y are independently carbon atom or nitrogen atom;
• R1 is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted cycloalkylalkyl or optionally substituted heterocycloalkylalkyl;
• R2 is —W21—W22—Rb—R20,
• wherein
• W21 is —(CO)—or —(SO2)—,
• W22 is bond, —O—, —NH—or optionally substituted lower alkylene,
• Rb is bond or optionally substituted alkylene, and
• R20 is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl or optionally substituted heterocycloalkyl;
• R3 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl;
• R91 is selected from optionally substituted alkyl, linker and solid support;
• and
• R92 is selected from optionally substituted alkyl, linker and solid support;
• with the proviso that
• when B is benzene, and R21 is W21—W22—Rb—R20, wherein W21 is —(CO)—, W22 is —NH—, and Rb is bond, then R20 should not be optionally substituted phenyl;
• or a salt thereof.

A process for preparing a compound having the following general formula (I):

• wherein
• is single bond or double bond;
• A is —CHR7—,
• wherein
• R7 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted cycloalkylalkyl or optionally substituted heterocycloalkylalkyl;
• B is optionally substituted 3-, 4-, 5-, 6- or 7- membered saturated or unsaturated monocyclic carbocyclic ring formed together with G and Y, or is optionally substituted 4-, 5-, 6- or 7 membered saturated or unsaturated heterocyclic ring formed together with G and Y and the hetero atom is selected from S, N and O and the number of hetero atoms is an integer of 1-3;
• G and Y are independently carbon atom or nitrogen atom;
• R1 is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted cycloalkylalkyl or optionally substituted heterocycloalkylalkyl;
• R2 is —W21—W22—Rb—R20,
• wherein
• W21 is —(CO)—or —(SO2)—,
• W22 is bond, —O—, —NH— or optionally substituted lower alkylene,
• Rb is bond or optionally substituted alkylene, and
• R20 is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl or optionally substituted heterocycloalkyl;
• and
• R3 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl;
• with the proviso that
• when B is benzene, and R2 is —W21—W22—Rb—R20, wherein W21 is —(CO)—, W22 is —NH—, and Rb is bond, then R20 should not be optionally substituted phenyl;
• or a salt thereof, which comprises reacting a compound having the following general formula (II):
• wherein
• R91 is selected from optionally substituted alkyl, linker and solid support;
• R92 is selected from optionally substituted alkyl, linker and solid support;
• and
• the other symbols are as defined above, or a salt thereof, with an acid.