US2019292178A9PendingUtilityA9
Host targeted inhibitors of dengue virus and other viruses
Assignee: DANA FARBER CANCER INST INCPriority: Apr 11, 2012Filed: Jan 26, 2018Published: Sep 26, 2019
Est. expiryApr 11, 2032(~5.7 yrs left)· nominal 20-yr term from priority
C07D 519/00C07D 471/04
51
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Claims
Abstract
The inventive compounds, pharmaceutical compositions thereof, and kits including the inventive compounds are useful for the prevention and treatment of infectious diseases caused by viruses, for example, by Flaviviridae virus (e.g., Dengue virus (DENV)), Kunjin virus, Japanese encephalitis virus, vesicular stomatitis virus (VSV), herpes simplex virus 1 (HSV-1), human cytomegalovirus (HCMV), poliovirus, Junin virus, Ebola virus, Marburg virus (MARV), Lassa fever virus (LASV), Venezuelan equine encephalitis virus (VEEV), or Rift Valley Fever virus (RVFV).
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A compound of Formula (I):
or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof;
wherein:
Ring A is heteroaryl;
each instance of R A is independently selected from the group consisting of hydrogen, halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, —OR A1 , —N(R A1 ) 2 , —SR A1 , —CN, —C(═NR A1 )R A1 , —C(═NR A1 )OR A1 , —C(═NR A1 )SR A1 , —C(═NR A1 )N(R A1 ) 2 , —C(═O)NR A1 —, —NR A1 C(═O)—, —C(═O)R A1 , —C(═S)R A1 , —C(═S)OR A1 , —C(═S)SR A1 , —C(═S)N(R A1 ) 2 , —NO 2 , —N 3 , —N(R A1 ) 3 + F − , —N(R A1 ) 3 + Cl − , —N(R A1 ) 3 + Br − , —N(R A1 ) 3 + I − , —N(OR A1 )R A1 , —NR A1 C(═O)R A1 , —NR A1 C(═O)OR A1 , —NR A1 C(═O)SR A1 , —NR A1 C(═O)N(R A1 ) 2 , —NR A1 C(═S)R A1 , —NR A1 C(═S)OR A1 , —NR A1 C(═S)SR A1 , —NR A1 C(═S)N(R A1 ) 2 , —NR A1 C(═NR A1 )R A1 , —NR A1 C(═NR A1 )OR A1 , —NR A1 C(═NR A1 )SR A1 , —NR A1 C(═NR A1 )N(R A1 ) 2 , —NR A1 S(═O) 2 R A1 , —NR A1 S(═O) 2 OR A1 , —NR A1 S(═O) 2 SR A1 , —NR A1 S(═O) 2 N(R A1 ) 2 , —NR A1 S(═O)R A1 , —NR A1 S(═O)OR A1 , —NR A1 S(═O)SR A1 , —NR A1 S(═O)N(R A1 ) 2 , —NR A1 P(═O), —NR A1 P(═O) 2 , —NR A1 P(═O)(R A1 ) 2 , —NR A1 P(═O)R A1 (OR A1 ), —NR A1 P(═O)(OR A1 ) 2 , —OC(═O)R A1 , —OC(═O)OR A1 , —OC(═O)SR A1 , —OC(═O)N(R A1 ) 2 , —OC(═NR A1 )R A1 , —OC(═NR A1 )OR A1 , —OC(═NR A1 )N(R A1 ) 2 , —OC(═S)R A1 , —OC(═S)OR A1 , —OC(═S)SR A1 , —OC(═S)N(R A1 ) 2 , —ON(R A1 ) 2 , —OS(═O)R A1 , —OS(═O)OR A1 , —OS(═O)SR A1 , —OS(═O)N(R A1 ) 2 , —OS(═O) 2 R A1 , —OS(═O) 2 OR A1 , —OS(═O) 2 SR A1 , —OS(═O) 2 N(R A1 ) 2 , —OP(═O) 2 , —OP(═O)(R A1 ) 2 , —OP(═O)R A1 (OR A1 ), —OP(═O)(OR A1 ) 2 , —OP(═O), —OP(R A1 ) 2 , —OPR A1 (OR A1 ), —OP(OR A1 ) 2 , —OSi(R A1 ) 3 , —OSi(R A1 ) 2 OR A1 , —OSi(R A1 )(OR A1 ) 2 , —OSi(OR A1 ) 3 , —SSR A1 , —S(═O)R A1 , —S(═O)OR A1 , —S(═O)N(R A1 ) 2 , —S(═O) 2 R A1 , —S(═O) 2 OR A1 , —S(═O) 2 N(R A1 ) 2 , —SC(═O)R A1 , —SC(═O)OR A1 , —SC(═O)SR A1 , —SC(═O)N(R A1 ) 2 , —SC(═S)R A1 , —SC(═S)OR A1 , —SC(═S)SR A1 , —SC(═S)N(R A1 ) 2 , —P(R A1 ) 2 , —PR A1 (OR A1 ), —P(OR A1 ) 2 , —P(═O), —P(═O)(R A1 ) 2 , —P(═O)(OR A1 ) 2 , —P(═O)R A1 (OR A1 ), —P(═O) 2 , —B(R A1 ) 2 , —B(OR A1 ) 2 , —BR A1 (OR A1 ), —Si(R A1 ) 3 , —Si(R A1 ) 2 OR A1 , —SiR A1 (OR A1 ) 2 , and —Si(OR A ) 3 , wherein each occurrence of R A1 is independently selected from the group consisting of hydrogen, optionally substituted acyl, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, a nitrogen protecting group when attached to a nitrogen atom, an oxygen protecting group when attached to an oxygen atom, a sulfur protecting group when attached to a sulfur atom, or two R A1 groups are joined to form an optionally substituted heterocyclic ring;
k is 0, 1, 2, 3, 4, or 5;
Ring C is a carbocyclic, heterocyclic, aryl, or heteroaryl ring;
each instance of R C is independently selected from the group consisting of hydrogen, halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, —OR C1 , —N(R C1 ) 2 , —SR C1 , —CN, —C(═NR C1 )R C1 , —C(═NR C1 )OR C1 , —C(═NR C1 )SR C1 , —C(═NR C1 )N(R C1 ) 2 , —C(═O)R C1 , —C(═S)R C1 , —C(═S)OR C1 , —C(═S)SR C1 , —C(═S)N(R C1 ) 2 , —NO 2 , —N 3 , —N(R C1 ) 3 + F − , —N(R C1 ) 3 + Cl − , —N(R C1 ) 3 + Br − , —N(R C1 ) 3 + I − , —N(OR C1 )R C1 , —NR C1 C(═O)R C1 , —NR C1 C(═O)OR C1 , —NR C1 C(═O)SR C1 , —NR C1 C(═O)N(R C1 ) 2 , —NR C1 C(═S)R C1 , —NR C1 C(═S)OR C1 , —NR C1 C(═S)SR C1 , —NR C1 C(═S)N(R C1 ) 2 , —NR C1 C(═NR)R C1 , —NR C1 C(═NR C1 )OR C1 , —NR C1 C(═NR C1 )SR C1 , —NR C1 C(═NR C1 )N(R C1 ) 2 , —NR C1 S(═O) 2 R C1 , —NR C1 S(═O) 2 OR C1 , —NR C1 S(═O) 2 SR C1 , —NR C1 S(═O) 2 N(R C1 ) 2 , —NR C1 S(═O)R C1 , —NR C1 S(═O)OR C1 , —NR C1 S(═O)SR C1 , —NR C1 S(═O)N(R C1 ) 2 , —NR C1 P(═O), —NR C1 P(═O) 2 , —NR C1 P(═O)(R C1 ) 2 , —NR C1 P(═O)R C1 (OR C1 ), —NR C1 P(═O)(OR C1 ) 2 , —OC(═O)R C1 , —OC(═O)OR C1 , —OC(═O)SR C1 , —OC(═O)N(R C1 ) 2 , —OC(═NR C1 )R C1 , —OC(═NR C1 )OR C1 , —OC(═NR C1 )N(R C1 ) 2 , —OC(═S)R C1 , —OC(═S)OR C1 , —OC(═S)SR C1 , —OC(═S)N(R C1 ) 2 , —ON(R C1 ) 2 , —OS(═O)R C1 , —OS(═O)OR C1 , —OS(═O)SR C1 , —OS(═O)N(R C1 ) 2 , —OS(═O) 2 R C1 , —OS(═O) 2 OR C1 , —OS(═O) 2 SR C1 , —OS(═O) 2 N(R C1 ) 2 , —OP(═O) 2 , —OP(═O)(R C1 ) 2 , —OP(═O)R C1 (OR C1 ), —OP(═O)(OR C1 ) 2 , —OP(═O), —OP(R C1 ) 2 , —OPR C1 (OR C1 ), —OP(OR C1 ) 2 , —OSi(R C1 ) 3 , —OSi(R C1 ) 2 OR C1 , —OSi(R C1 )(OR C1 ) 2 , —OSi(OR C1 ) 3 , —SSR C1 , —S(═O)R C1 , —S(═O)OR C1 , —S(═O)N(R C1 ) 2 , —S(═O) 2 R C1 , —S(═O) 2 OR C1 , —S(═O) 2 N(R C1 ) 2 , —SC(═O)R C1 , —SC(═O)OR C1 , —SC(═O)SR C1 , —SC(═O)N(R C1 ) 2 , —SC(═S)R C1 , —SC(═S)OR C1 , —SC(═S)SR C1 , —SC(═S)N(R C1 ) 2 , —P(R C1 ) 2 , —PR C1 (OR C1 ), —P(OR C1 ) 2 , —P(═O), —P(═O)(R C1 ) 2 , —P(═O)(OR C1 ) 2 , —P(═O)R C1 (OR C1 ), —P(═O) 2 , —B(R C1 ) 2 , —B(OR C1 ) 2 , —BR C1 (OR C1 ), —Si(R C1 ) 3 , —Si(R C1 ) 2 OR C1 , —SiR C1 (OR C1 ) 2 , and —Si(OR C1 ) 3 , wherein each occurrence of R C1 is independently selected from the group consisting of hydrogen, optionally substituted acyl, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, a nitrogen protecting group when attached to a nitrogen atom, an oxygen protecting group when attached to an oxygen atom, a sulfur protecting group when attached to a sulfur atom, or two R C1 groups are joined to form an optionally substituted heterocyclic ring or optionally substituted heteroaryl ring;
n is 0, 1, 2, 3, or 4;
L is a bond or an optionally substituted, branched or unbranched C 1-6 hydrocarbon chain;
R D is any one of Formulae (i-1)-(i-43):
wherein:
each instance of R D1 is independently hydrogen, halogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —CN, —NO 2 , —OR D1a , —N(R D1a ) 2 , —SR D1a , —CH 2 OR D1a , —CH 2 N(R D1a ) 2 , —CH 2 SR D1a , —C(═O)R D1a , —C(═O)OR D1a , —C(═O)SR D1a , —C(═O)N(R D1a ) 2 , —C(═S)R D1a , —C(═S)OR D1a , —C(═S)SR D1a , —C(═S)N(R D1a ) 2 , —C(═NR D1a )R D1a , —C(═NR D1a )OR D1a , —C(═NR D1a )SR D1a , or —C(═NR D1a )N(R D1a ) 2 , wherein each occurrence of R D1a is independently hydrogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, or two R D1a groups are joined to form an substituted or unsubstituted heterocyclic ring;
each instance of R D2 is independently hydrogen, halogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —CN, —NO 2 , —OR D2a , —N(R D2a ) 2 , —SR D2a , —CH 2 OR D2a CH 2 N(R D2a ) 2 , —CH 2 SR D2a , —C(═O)R D2a , —C(═O)OR D2a , —C(═O)SR D2a , —C(═O)N(R D2a ) 2 , —C(═S)R D2a , —C(═S)OR D2a , —C(═S)SR D2a , —C(═S)N(R D2a ) 2 , —C(═NR D2a )R D2a , —C(═NR D2a )OR D2a , —C(═NR D2a )SR D2a , and —C(═NR D2a )N(R D2a ) 2 , wherein each occurrence of R D2a is independently hydrogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, or two R D2a groups are joined to form an substituted or unsubstituted heterocyclic ring;
each instance of R D3 is independently hydrogen, halogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR D3a , —N(R D3a ) 2 , —SR D3a , —CH 2 OR D3a , —CH 2 N(R D3a ) 2 , —CH 2 SR D3a , —C(═O)R D3a , —C(═O)OR D3a , —C(═O)SR D3a , —C(═O)N(R D3a ) 2 , —C(═S)R D3a , —C(═S)OR D3a , —C(═S)SR D3a , —C(═S)N(R D3a ) 2 , —C(═NR D3a )R D3a , —C(═NR D3a )OR D3a , —C(═NR D3a )SR D3a , or —C(═NR D3a )N(R D3a ) 2 wherein each occurrence of R D3a is independently hydrogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, or two R D3a groups are joined to form an substituted or unsubstituted heterocyclic ring;
optionally R D1 and R D3 , or R D2 and R D3 , or R D1 and R D2 are joined to form an substituted or unsubstituted carbocyclic or substituted or unsubstituted heterocyclic ring;
R D4 is a leaving group selected from the group consisting of —Br, —Cl, —I, and —OS(═O) w R D4a , wherein w is 1 or 2, and R D4a is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
each instance of X 1 is independently a bond, —C(═O)—, —SO 2 —, —NR D5 —, optionally substituted alkylene, or optionally substituted heteroarylene, wherein R D5 is hydrogen, C 1-6 alkyl, or a nitrogen protecting group;
each instance of Y is independently O, S, or NR D6 , wherein R D6 is hydrogen, C 1-6 alkyl, or a nitrogen protecting group; and
each instance of z and z 1 is independently 0, 1, 2, 3, 4, 5, or 6, as valency permits.
2 . A compound of Formula (II):
or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof;
wherein:
Ring A is aryl, arylalkenyl, or heteroaryl;
each instance of R A is independently selected from the group consisting of hydrogen, halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, —OR A1 , —N(R A1 ) 2 , —SR A1 , —CN, —C(═NR A1 )R A1 , —C(═NR A1 )OR A1 , —C(═NR A1 )SR A1 , —C(═NR A1 )N(R A1 ) 2 , —C(═O)NR A1 —, —NR A1 C(═O)—, —C(═O)R A1 , —C(═S)R A1 , —C(═S)OR A1 , —C(═S)SR A1 , —C(═S)N(R A1 ) 2 , —NO 2 , —N 3 , —N(R A1 ) 3 + F − , —N(R A1 ) 3 + Cl − , —N(R A1 ) 3 + Br − , —N(R A1 ) 3 + I − , —N(OR A1 )R A1 , —NR A1 C(═O)R A1 , —NR A1 C(═O)OR A1 , —NR A1 C(═O)SR A1 , —NR A1 C(═O)N(R A1 ) 2 , —NR A1 C(═S)R A1 , —NR A1 C(═S)OR A1 , —NR A1 C(═S)SR A1 , —NR A1 C(═S)N(R A1 ) 2 , —NR A1 C(═NR A1 )R A1 , —NR A1 C(═NR A1 )OR A1 , —NR A1 C(═NR A1 )SR A1 , —NR A1 C(═NR A1 )N(R A1 ) 2 , —NR A1 S(═O) 2 R A1 , —NR A1 S(═O) 2 OR A1 , —NR A1 S(═O) 2 SR A1 , —NR A1 S(═O) 2 N(R A1 ) 2 , —NR A1 S(═O)R A1 , —NR A1 S(═O)OR A1 , —NR A1 S(═O)SR A1 , —NR A1 S(═O)N(R A1 ) 2 , —NR A1 P(═O), —NR A1 P(═O) 2 , —NR A1 P(═O)(R A1 ) 2 , —NR A1 P(═O)R A1 (OR A1 ), —NR A1 P(═O)(OR A1 ) 2 , —OC(═O)R A1 , —OC(═O)OR A1 , —OC(═O)SR A1 , —OC(═O)N(R A1 ) 2 , —OC(═NR A1 )R A1 , —OC(═NR A1 )OR A1 , —OC(═NR A1 )N(R A1 ) 2 , —OC(═S)R A1 , —OC(═S)OR A1 , —OC(═S)SR A1 , —OC(═S)N(R A1 ) 2 , —ON(R A1 ) 2 , —OS(═O)R A1 , —OS(═O)OR A1 , —OS(═O)SR A1 , —OS(═O)N(R A1 ) 2 , —OS(═O) 2 R A1 , —OS(═O) 2 OR A1 , —OS(═O) 2 SR A1 , —OS(═O) 2 N(R A1 ) 2 , —OP(═O) 2 , —OP(═O)(R A1 ) 2 , —OP(═O)R A1 (OR A1 ), —OP(═O)(OR A1 ) 2 , —OP(═O), —OP(R A1 ) 2 , —OPR A1 (OR A1 ), —OP(OR A1 ) 2 , —OSi(R A1 ) 3 , —OSi(R A1 ) 2 OR A1 , —OSi(R A1 )(OR A1 ) 2 , —OSi(OR A1 ) 3 , —SSR A1 , —S(═O)R A1 , —S(═O)OR A1 , —S(═O)N(R A1 ) 2 , —S(═O) 2 R A1 , —S(═O) 2 OR A1 , —S(═O) 2 N(R A1 ) 2 , —SC(═O)R A1 , —SC(═O)OR A1 , —SC(═O)SR A1 , —SC(═O)N(R A1 ) 2 , —SC(═S)R A1 , —SC(═S)OR A1 , —SC(═S)SR A1 , —SC(═S)N(R A1 ) 2 , —P(R A1 ) 2 , —PR A1 (OR A1 ), —P(OR A1 ) 2 , —P(═O), —P(═O)(R A1 ) 2 , —P(═O)(OR A1 ) 2 , —P(═O)R A1 (OR A1 ), —P(═O) 2 , —B(R A1 ) 2 , —B(OR A1 ) 2 , —BR A1 (OR A1 ), —Si(R A1 ) 3 , —Si(R A1 ) 2 OR A1 , —SiR A1 (OR A1 ) 2 , and —Si(OR A1 ) 3 , wherein each occurrence of R A1 is independently selected from the group consisting of hydrogen, optionally substituted acyl, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, a nitrogen protecting group when attached to a nitrogen atom, an oxygen protecting group when attached to an oxygen atom, a sulfur protecting group when attached to a sulfur atom, or two R A1 groups are joined to form an optionally substituted heterocyclic ring;
k is 0, 1, 2, 3, 4, or 5;
Ring C is a carbocyclic, heterocyclic, aryl, or heteroaryl ring;
each instance of R j1 , R j2 , R j3 , and R C is independently selected from the group consisting of hydrogen, halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, —OR C1 , —N(R C1 ) 2 , —SR C1 , —CN, —C(═NR C1 )R C1 , —C(═NR C1 )OR C1 , —C(═NR C1 )SR C1 , —C(═NR C1 )N(R C1 ) 2 , —C(═O)R C1 , —C(═S)R C1 , —C(═S)OR C1 , —C(═S)SR C1 , —C(═S)N(R C1 ) 2 , —NO 2 , —N 3 , —N(R C1 ) 3 + F − , —N(R C1 ) 3 + Cl − , —N(R C1 ) 3 + Br − , —N(R C1 ) 3 + F − , —N(OR C1 )R C1 , —NR C1 C(═O)R C1 , —NR C1 C(═O)OR C1 , —NR C1 C(═O)SR C1 , —NR C1 C(═O)N(R C1 ) 2 , —NR C1 C(═S)R C1 , —NR C1 C(═S)OR C1 , —NR C1 C(═S)SR C1 , —NR C1 C(═S)N(R C1 ) 2 , —NR C1 C(═NR C1 )R C1 , —NR C1 C(═NR C1 )OR C1 , —NR C1 C(═NR C1 )SR C1 , —NR C1 C(═NR C1 )N(R C1 ) 2 , —NR C1 S(═O) 2 R C1 , —NR C1 S(═O) 2 OR C1 , —NR C1 S(═O) 2 SR C1 , —NR C1 S(═O) 2 N(R C1 ) 2 , —NR C1 S(═O)R C1 , —NR C1 S(═O)OR C1 , —NR C1 S(═O)SR C1 , —NR C1 S(═O)N(R C1 ) 2 , —NR C1 P(═O), —NR C1 P(═O) 2 , —NR C1 P(═O)(R C1 ) 2 , —NR C1 P(═O)R C1 (OR C1 ), —NR C1 P(═O)(OR 1 ) 2 , —OC(═O)R C1 , —OC(═O)OR C1 , —OC(═O)SR C1 , —OC(═O)N(R C1 ) 2 , —OC(═NR C1 )R C1 , —OC(═NR C1 )OR C1 , —OC(═NR C1 )N(R C1 ) 2 , —OC(═S)R C1 , —OC(═S)OR C1 , —OC(═S)SR C1 , —OC(═S)N(R C1 ) 2 , —ON(R C1 ) 2 , —OS(═O)R C1 , —OS(═O)OR C1 , —OS(═O)SR C1 , —OS(═O)N(R C1 ) 2 , —OS(═O) 2 R C1 , —OS(═O) 2 OR C1 , —OS(═O) 2 SR C1 , —OS(═O) 2 N(R C1 ) 2 , —OP(═O) 2 , —OP(═O)(R C1 ) 2 , —OP(═O)R C1 (OR C1 ), —OP(═O)(OR C1 ) 2 , —OP(═O), —OP(R C1 ) 2 , —OPR C1 (OR C1 ), —OP(OR C1 ) 2 , —OSi(R C1 ) 3 , —OSi(R C1 ) 2 OR C1 , —OSi(R C1 )(OR C1 ) 2 , —OSi(OR C1 ) 3 , —SSR C1 , —S(═O)R C1 , —S(═O)OR C1 , —S(═O)N(R C1 ) 2 , —S(═O) 2 R C1 , —S(═O) 2 OR C1 , —S(═O) 2 N(R C1 ) 2 , —SC(═O)R C1 , —SC(═O)OR C1 , —SC(═O)SR C1 , —SC(═O)N(R C1 ) 2 , —SC(═S)R C1 , —SC(═S)OR C1 , —SC(═S)SR C1 , —SC(═S)N(R C1 ) 2 , —P(R C1 ) 2 , —PR C1 (OR C1 ), —P(OR C1 ) 2 , —P(═O), —P(═O)(R C1 ) 2 , —P(═O)(OR C1 ) 2 , —P(═O)R C1 (OR C1 ), —P(═O) 2 , —B(R C1 ) 2 , —B(OR C1 ) 2 , —BR C1 (OR C1 ), —Si(R C1 ) 3 , —Si(R C1 ) 2 OR C1 , —SiR C1 (OR C1 ) 2 , and —Si(OR C1 ) 3 , wherein each occurrence of R C d is independently selected from the group consisting of hydrogen, optionally substituted acyl, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, a nitrogen protecting group when attached to a nitrogen atom, an oxygen protecting group when attached to an oxygen atom, a sulfur protecting group when attached to a sulfur atom, or two R C1 groups are joined to form an optionally substituted heterocyclic ring or optionally substituted heteroaryl ring;
n is 0, 1, 2, 3, or 4;
L is a bond or an optionally substituted, branched or unbranched C 1-6 hydrocarbon chain;
R D is any one of Formulae (i-1)-(i-43):
wherein:
each instance of R D1 is independently hydrogen, halogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —CN, —NO 2 , —OR D1a , —N(R D1a ) 2 , —SR D1a , —CH 2 OR D1a , —CH 2 N(R D1a ) 2 , —CH 2 SR D1a , —C(═O)R D1a , —C(═O)OR D1a , —C(═O)SR D1a , —C(═O)N(R D1a ) 2 , —C(═S)R D1a , —C(═S)OR D1a , —C(═S)SR D1a , —C(═S)N(R D1a ) 2 , —C(═NR D1a )R D1a , —C(═NR D1a )OR D1a , —C(═NR D1a )SR D1 , or —C(═NR D1a )N(R D1a ) 2 , wherein each occurrence of R D1a is independently hydrogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, or two R D1a , groups are joined to form an substituted or unsubstituted heterocyclic ring;
each instance of R D2 is independently hydrogen, halogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —CN, —NO 2 , —OR D2a , —N(R D2a ) 2 , —SR D2a , —CH 2 OR D2a , —CH 2 N(R D2a ) 2 , —CH 2 SR D2a , —C(═O)R D2a , —C(═O)OR D2a , —C(═O)SR D2a , —C(═O)N(R D2a ) 2 , —C(═S)R D2a , —C(═S)OR D2a , —C(═S)SR D2a , —C(═S)N(R D2a ) 2 , —C(═NR D2a )R D2a , —C(═NR D2a )OR D2a , —C(═NR D2a )SR D2a , and —C(═NR D2a )N(R D2a ) 2 , wherein each occurrence of R D2a is independently hydrogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, or two R D2a groups are joined to form an substituted or unsubstituted heterocyclic ring;
each instance of R D3 is independently hydrogen, halogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR D3a , —N(R D3a ) 2 , —SR D3a , —CH 2 OR D3a , —CH 2 N(R D3a ) 2 , —CH 2 SR D3a , —C(═O)R D3a , —C(═O)OR D3a , —C(═O)SR D3a , —C(═O)N(R D3a ) 2 , —C(═S)R D3a , —C(═S)OR D3a , —C(═S)SR D3a , —C(═S)N(R D3a ) 2 , —C(═NR D3a )R D3a , —C(═NR D3a )OR D3a , —C(═NR D3a )SR D3a , or —C(═NR D3a )N(R D3a ) 2 wherein each occurrence of R D3a is independently hydrogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, or two R D3a groups are joined to form an substituted or unsubstituted heterocyclic ring;
optionally R D1 and R D3 , or R D2 and R D3 , or R D1 and R D2 are joined to form an substituted or unsubstituted carbocyclic or substituted or unsubstituted heterocyclic ring;
R D4 is a leaving group selected from the group consisting of —Br, —Cl, —I, and —OS(═O) w R D4a , wherein w is 1 or 2, and R D4a is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
each instance of X 1 is independently a bond, —C(═O)—, —SO 2 —, —NR D5 —, optionally substituted alkylene, or optionally substituted heteroarylene, wherein R D5 is hydrogen, C 1-6 alkyl, or a nitrogen protecting group;
each instance of Y is independently O, S, or NR D6 , wherein R D6 is hydrogen, C 1-6 alkyl, or a nitrogen protecting group; and
each instance of z and z 1 is independently 0, 1, 2, 3, 4, 5, or 6, as valency permits.
3 . A compound of Formula (III):
or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof;
wherein:
Ring A is aryl, arylalkenyl, or heteroaryl;
each instance of R A is independently selected from the group consisting of hydrogen, halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, —OR A1 , —N(R A1 ) 2 , —SR A1 , —CN, —C(═NR A1 )R A1 , —C(═NR A1 )OR A1 , —C(═NR A1 )SR A1 , —C(═NR A1 )N(R A1 ) 2 , —C(═O)NR A1 —, —NR A1 C(═O)—, —C(═O)R A1 , —C(═S)R A1 , —C(═S)OR A1 , —C(═S)SR A1 , —C(═S)N(R A1 ) 2 , —NO 2 , —N 3 , —N(R A1 ) 3 +F—, —N(R A1 ) 3 + Cl − , —N(R A1 ) 3 + Br − , —N(R A1 ) 3 + I − , —N(OR A1 )R A1 , —NR A1 C(═O)R A1 , —NR A1 C(═O)OR A1 , —NR A1 C(═O)SR A1 , —NR A1 C(═O)N(R A1 ) 2 , —NR A1 C(═S)R A1 , —NR A1 C(═S)OR A1 , —NR A1 C(═S)SR A1 , —NR A1 C(═S)N(R A1 ) 2 , —NR A1 C(═NR A1 )R A1 , —NR A1 C(═NR A1 )OR A1 , —NR A1 C(═NR A1 )SR A1 , —NR A1 C(═NR A1 )N(R A1 ) 2 , —NR A1 S(═O) 2 R A1 , —NR A1 S(═O) 2 OR A1 , —NR A1 S(═O) 2 SR A1 , —NR A1 S(═O) 2 N(R A1 ) 2 , —NR A1 S(═O)R A1 , —NR A1 S(═O)OR A1 , —NR A1 S(═O)SR A1 , —NR A1 S(═O)N(R A1 ) 2 , —NR A1 P(═O), —NR A1 P(═O) 2 , —NR A1 P(═O)(R A1 ) 2 , —NR A1 P(═O)R A1 (OR A1 ), —NR A1 P(═O)(OR A1 ) 2 , —OC(═O)R A1 , —OC(═O)OR A1 , —OC(═O)SR A1 , —OC(═O)N(R A1 ) 2 , —OC(═NR A1 )R A1 , —OC(═NR A1 )OR A1 , —OC(═NR A1 )N(R A1 ) 2 , —OC(═S)R A1 , —OC(═S)OR A1 , —OC(═S)SR A1 , —OC(═S)N(R A1 ) 2 , —ON(R A1 ) 2 , —OS(═O)R A1 , —OS(═O)OR A1 , —OS(═O)SR A1 , —OS(═O)N(R A1 ) 2 , —OS(═O) 2 R A1 , —OS(═O) 2 OR A1 , —OS(═O) 2 SR A1 , —OS(═O) 2 N(R A1 ) 2 , —OP(═O) 2 , —OP(═O)(R A1 ) 2 , —OP(═O)R A1 (OR A1 ), —OP(═O)(OR A1 ) 2 , —OP(═O), —OP(R A1 ) 2 , —OPR A1 (OR A1 ), —OP(OR A1 ) 2 , —OSi(R A1 ) 3 , —OSi(R A1 ) 2 OR A1 , —OSi(R A1 )(OR A1 ) 2 , —OSi(OR A1 ) 3 , —SSR A1 , —S(═O)R A1 , —S(═O)OR A1 , —S(═O)N(R A1 ) 2 , —S(═O) 2 R A1 , —S(═O) 2 OR A , —S(═O) 2 N(R A1 ) 2 , —SC(═O)R A1 , —SC(═O)OR A1 , —SC(═O)SR A1 , —SC(═O)N(R A1 ) 2 , —SC(═S)R A1 , —SC(═S)OR A1 , —SC(═S)SR A1 , —SC(═S)N(R A1 ) 2 , —P(R A1 ) 2 , —PR A1 (OR A1 ), —P(OR A1 ) 2 , —P(═O), —P(═O)(R A1 ) 2 , —P(═O)(OR A1 ) 2 , —P(═O)R A1 (OR A1 ), —P(═O) 2 , —B(R A1 ) 2 , —B(OR A1 ) 2 , —BR A1 (OR A1 ), —Si(R A1 ) 3 , —Si(R A1 ) 2 OR A1 , —SiR A1 (OR A1 ) 2 , and —Si(OR A1 ) 3 , wherein each occurrence of R A1 is independently selected from the group consisting of hydrogen, optionally substituted acyl, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, a nitrogen protecting group when attached to a nitrogen atom, an oxygen protecting group when attached to an oxygen atom, a sulfur protecting group when attached to a sulfur atom, or two R A1 groups are joined to form an optionally substituted heterocyclic ring;
k is 0, 1, 2, 3, 4, or 5;
Ring C is a carbocyclic, heterocyclic, aryl, or heteroaryl ring;
each instance of R C is independently selected from the group consisting of hydrogen, halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, —OR C1 , —N(R C1 ) 2 , —SR C1 , —CN, —C(═NR C1 )R C1 , —C(═NR C1 )OR q , —C(═NR C1 )SR C1 , —C(═NR C1 )N(R C1 ) 2 , —C(═O)R C1 , —C(═S)R C1 , —C(═S)OR C1 , —C(═S)SR C1 , —C(═S)N(R C1 ) 2 , —NO 2 , —N 3 , —N(R C1 ) 3 + F − , —N(R C1 ) 3 + Cl − , —N(R C1 ) 3 + Br − , —N(R C1 ) 3 + I − , —N(OR C1 )R C1 , —NR C1 C(═O)R C1 , —NR C1 C(═O)OR C1 , —NR C1 C(═O)SR C1 , —NR C1 C(═O)N(R C1 ) 2 , —NR C1 C(═S)R C1 , —NR C1 C(═S)OR C1 , —NR C1 C(═S)SR C1 , —NR C1 C(═S)N(R C1 ) 2 , —NR C1 C(═NR)R C1 , —NR C1 C(═NR C1 )OR C1 , —NR C1 C(═NR C1 )SR C1 , —NR C1 C(═NR C1 )N(R C1 ) 2 , —NR C1 S(═O) 2 R C1 , —NR C1 S(═O) 2 OR C1 , —NR C1 S(═O) 2 SR C1 , —NR C1 S(═O) 2 N(R C1 ) 2 , —NR C1 S(═O)R C1 , —NR C1 S(═O)OR C1 , —NR C1 S(═O)SR C1 , —NR C1 S(═O)N(R C1 ) 2 , —NR C1 P(═O), —NR C1 P(═O) 2 , —NR C1 P(═O)(R C1 ) 2 , —NR C1 P(═O)R C1 (OR C1 ), —NR C1 P(═O)(OR C1 ) 2 , —OC(═O)R C1 , —OC(═O)OR C1 , —OC(═O)SR C1 , —OC(═O)N(R C1 ) 2 , —OC(═NR C1 )R C1 , —OC(═NR C1 )OR C1 , —OC(═NR C1 )N(R C1 ) 2 , —OC(═S)R C1 , —OC(═S)OR C1 , —OC(═S)SR C1 , —OC(═S)N(R C1 ) 2 , —ON(R C1 ) 2 , —OS(═O)R C1 , —OS(═O)OR C1 , —OS(═O)SR C1 , —OS(═O)N(R C1 ) 2 , —OS(═O) 2 R C1 , —OS(═O) 2 OR C1 , —OS(═O) 2 SR C1 , —OS(═O) 2 N(R C1 ) 2 , —OP(═O) 2 , —OP(═O)(R C1 ) 2 , —OP(═O)R C1 (OR C1 ), —OP(═O)(OR C1 ) 2 , —OP(═O), —OP(R C1 ) 2 , —OPR C1 (OR C1 ), —OP(OR C1 ) 2 , —OSi(R C1 ) 3 , —OSi(R C1 ) 2 OR C1 , —OSi(R C1 )(OR C1 ) 2 , —OSi(OR C1 ) 3 , —SSR C1 , —S(═O)R C1 , —S(═O)OR C1 , —S(═O)N(R C1 ) 2 , —S(═O) 2 R C1 , —S(═O) 2 OR C1 , —S(═O) 2 N(R C1 ) 2 , —SC(═O)R C1 , —SC(═O)OR C1 , —SC(═O)SR C1 , —SC(═O)N(R C1 ) 2 , —SC(═S)R C1 , —SC(═S)OR C1 , —SC(═S)SR C1 , —SC(═S)N(R C1 ) 2 , —P(R C1 ) 2 , —PR C1 (OR C1 ), —P(OR C1 ) 2 , —P(═O), —P(═O)(R C1 ) 2 , —P(═O)(OR C1 ) 2 , —P(═O)R C1 (OR C1 ), —P(═O) 2 , —B(R C1 ) 2 , —B(OR C1 ) 2 , —BR C1 (OR C1 ), —Si(R C1 ) 3 , —Si(R C1 ) 2 OR C1 , —SiR C1 (OR C1 ) 2 , and —Si(OR C1 ) 3 , wherein each occurrence of R C1 is independently selected from the group consisting of hydrogen, optionally substituted acyl, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, a nitrogen protecting group when attached to a nitrogen atom, an oxygen protecting group when attached to an oxygen atom, a sulfur protecting group when attached to a sulfur atom, or two R C1 groups are joined to form an optionally substituted heterocyclic ring or optionally substituted heteroaryl ring;
R q is independently hydrogen, halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, or a nitrogen protecting group;
n is 0, 1, 2, 3, or 4;
L is a bond or an optionally substituted, branched or unbranched C 1-6 hydrocarbon chain;
R D is any one of Formulae (i-1)-(i-43):
wherein:
each instance of R D1 is independently hydrogen, halogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —CN, —NO 2 , —OR D1a , —N(R D1a ) 2 , —SR D1a , —CH 2 OR D1a , —CH 2 N(R D1a ) 2 , —CH 2 SR D1a , —C(═O)R D1a , —C(═O)OR D1a , —C(═O)SR D1a , —C(═O)N(R D1a ) 2 , —C(═S)R D1a , —C(═S)OR D1a , —C(═S)SR D1a , —C(═S)N(R D1a ) 2 , —C(═NR D1a )R D1a , —C(═NR D1a )OR D1a C(═NR D1a )SR D1a , or —C(═NR D1a )N(R D1a ) 2 , wherein each occurrence of R D1a is independently hydrogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, or two R D1a groups are joined to form an substituted or unsubstituted heterocyclic ring;
each instance of R D2 is independently hydrogen, halogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —CN, —NO 2 , —OR D2a , —N(R D2a ) 2 , —SR D2a , —CH 2 OR D2a CH 2 N(R D2a ) 2 , —CH 2 SR D2a , —C(═O)R D2a , —C(═O)OR D2a , —C(═O)SR D2a , —C(═O)N(R D2a ) 2 , —C(═S)R D2a , —C(═S)OR D2a , —C(═S)SR D2a , —C(═S)N(R D2a ) 2 , —C(═NR D2a )R D2a , —C(═NR D2a )OR D2a , —C(═NR D2a )SR D2a , and —C(═NR D2a )N(R D2a ) 2 , wherein each occurrence of R D2a is independently hydrogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl, or two R D2a groups are joined to form an substituted or unsubstituted heterocyclic ring;
each instance of R D3 is independently hydrogen, halogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR D3a , —N(R D3a ) 2 , —SR D3a , —CH 2 OR D3a , —CH 2 N(R D3a ) 2 , —CH 2 SR D3a , —C(═O)R D3a , —C(═O)OR D3a , —C(═O)SR D3a , —C(═O)N(R D3a ) 2 , —C(═S)R D3a , —C(═S)OR D3a , —C(═S)SR D3a , —C(═S)N(R D3a ) 2 , —C(═NR D3a )R D3a , —C(═NR D3a )OR D3a , —C(═NR D3a )SR D3a , or —C(═NR D3a )N(R D3a ) 2 wherein each occurrence of R D3a is independently hydrogen, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, or two R D3a groups are joined to form an substituted or unsubstituted heterocyclic ring;
optionally R D1 and R D3 , or R D2 and R D3 , or R D1 and R D2 are joined to form an substituted or unsubstituted carbocyclic or substituted or unsubstituted heterocyclic ring;
R D4 is a leaving group selected from the group consisting of —Br, —Cl, —I, and —OS(═O) w R D4a , wherein w is 1 or 2, and R D4a is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
each instance of X 1 is independently a bond, —C(═O)—, —SO 2 —, —NR D5 —, optionally substituted alkylene, or optionally substituted heteroarylene, wherein R D5 is hydrogen, C 1-6 alkyl, or a nitrogen protecting group;
each instance of Y is independently O, S, or NR D6 , wherein R D6 is hydrogen, C 1-6 alkyl, or a nitrogen protecting group; and
each instance of z and z 1 is independently 0, 1, 2, 3, 4, 5, or 6, as valency permits.
4 . (canceled)
5 . The compound of claim 1 , wherein Ring A is a 5-membered or 6-membered, monocyclic heteroaryl ring.
6 . The compound of claim 5 , wherein
is of formula:
7 . (canceled)
8 . The compound of claim 5 , wherein
is of formula:
9 . (canceled)
10 . The compound of claim 1 , wherein
is one of the following formulae:
11 - 12 . (canceled)
13 . The compound of claim 1 , wherein Ring C is aryl.
14 . (canceled)
15 . The compound of claim 1 , wherein Ring C is indoline.
16 . (canceled)
17 . The compound of claim 1 , wherein L is a bond or —CH 2 —.
18 . (canceled)
19 . The compound of claim 1 , wherein R D is of formula:
20 . (canceled)
21 . The compound of claim 1 , wherein R D is of formula:
22 - 25 . (canceled)
26 . The compound of claim 1 , wherein the compound is of formula:
or a pharmaceutically acceptable salt thereof.
27 - 31 . (canceled)
32 . The compound of claim 1 , wherein the compound is of formula:
or a pharmaceutically acceptable salt thereof.
33 - 41 . (canceled)
42 . The compound of claim 1 , wherein the compound is of formula:
or a pharmaceutically acceptable salt thereof.
43 - 48 . (canceled)
49 . A pharmaceutical composition comprising a therapeutically or prophylactically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof, and optionally a pharmaceutically acceptable excipient.
50 . A method of treating or preventing an infectious disease in a subject suffering therefrom, the method comprising:
administering to the subject a therapeutically or prophylactically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof.
51 - 58 . (canceled)
59 . A method of preventing a viral infection in a subject who was or may be exposed to a virus, the method comprising:
administering to the subject a prophylactically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof.
60 - 69 . (canceled)
70 . A kit for treating or preventing an infectious disease, the kit comprising:
a first container comprising a compound of claim 1 , or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof; and instructions for administering the compound, or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof, to a subject to treat or prevent the infectious disease.
71 . The compound of claim 1 , wherein the compound is of the formula:
or a pharmaceutically acceptable salt thereof.Join the waitlist — get patent alerts
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