A61K31/433

Aryl hydrocarbon receptor modulators
11547698 · 2023-01-10 · ·

The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts, ##STR00001## R′ is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3, ##STR00002##
two R.sub.a is independently H, or two R.sub.a together form ═O or ═N—W.sub.3—R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring, or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and C═N, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is R.sub.c connected with C or R.sub.N connected with N.

Aryl hydrocarbon receptor modulators
11547698 · 2023-01-10 · ·

The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts, ##STR00001## R′ is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3, ##STR00002##
two R.sub.a is independently H, or two R.sub.a together form ═O or ═N—W.sub.3—R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring, or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and C═N, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is R.sub.c connected with C or R.sub.N connected with N.

COMPOUNDS FOR TREATING CORONAVIRUS INFECTION
20220387354 · 2022-12-08 · ·

Described herein are compounds of Formula I:

##STR00001##

wherein R.sub.1-R.sub.6 are as described herein, for use in the treatment of a coronavirus infection; a method of inhibiting a coronavirus 3CL protease, by contacting the 3CL protease with a compound of Formula I; as well as methods pharmaceutical composition comprising a compound of Formula I and at least one phospholipid, wherein a weight ratio of the phospholipid(s) to the compound in the composition is in a range of from 10:1 to 1:10. Further described herein is a method of treating a coronavirus infection in a subject in need thereof, by administering to the subject at least one compound that exhibits at least two of: inhibition of an activity of a 3CL protease of the coronavirus; inhibition of inflammation in the subject; and inhibition of autophagy in the subject.

COMPOUNDS FOR TREATING CORONAVIRUS INFECTION
20220387354 · 2022-12-08 · ·

Described herein are compounds of Formula I:

##STR00001##

wherein R.sub.1-R.sub.6 are as described herein, for use in the treatment of a coronavirus infection; a method of inhibiting a coronavirus 3CL protease, by contacting the 3CL protease with a compound of Formula I; as well as methods pharmaceutical composition comprising a compound of Formula I and at least one phospholipid, wherein a weight ratio of the phospholipid(s) to the compound in the composition is in a range of from 10:1 to 1:10. Further described herein is a method of treating a coronavirus infection in a subject in need thereof, by administering to the subject at least one compound that exhibits at least two of: inhibition of an activity of a 3CL protease of the coronavirus; inhibition of inflammation in the subject; and inhibition of autophagy in the subject.

METHOD OF TREATING RNA REPEAT MEDIATED DISEASES WITH RNA REPEAT BINDING COMPOUND
20220387399 · 2022-12-08 · ·

The use of 2,4-disubstituted thiadiazolidinone (TDZD) compounds, such as Tideglusib (4-Benzyl-2-naphthalen-1-yl-[1,2,4]thiadiazolidine-3,5-dione), in methods of inhibiting RNA molecules comprising abnormal trinucleotide repeats (such as CUG) in their sequences is provided. Such methods include methods of inhibiting RNA molecules having abnormal repeat sequences, as well as methods of treating and/or preventing diseases associated with the presence of RNA molecules having abnormal repeat sequences, such as myotonic dystrophy type 1 (DM1).

METHOD OF TREATING RNA REPEAT MEDIATED DISEASES WITH RNA REPEAT BINDING COMPOUND
20220387399 · 2022-12-08 · ·

The use of 2,4-disubstituted thiadiazolidinone (TDZD) compounds, such as Tideglusib (4-Benzyl-2-naphthalen-1-yl-[1,2,4]thiadiazolidine-3,5-dione), in methods of inhibiting RNA molecules comprising abnormal trinucleotide repeats (such as CUG) in their sequences is provided. Such methods include methods of inhibiting RNA molecules having abnormal repeat sequences, as well as methods of treating and/or preventing diseases associated with the presence of RNA molecules having abnormal repeat sequences, such as myotonic dystrophy type 1 (DM1).

COMPOSITIONS AND METHODS BASED ON HIV GP120 MUTANTS

Compositions and methods based on the use of mutated HIV-1 gp120 polypeptides having amino acid substitutions at positions 61, 105, 108, 375, 474, 475 and 476 are described. These mutated HIV-1 gp120 polypeptides, which make the HIV env protein more amenable to adopt specific conformations when contacted with gp120 ligands, may be useful as vaccines or tools to identify and characterize agents modulating HIV infection.

COMPOSITIONS AND METHODS BASED ON HIV GP120 MUTANTS

Compositions and methods based on the use of mutated HIV-1 gp120 polypeptides having amino acid substitutions at positions 61, 105, 108, 375, 474, 475 and 476 are described. These mutated HIV-1 gp120 polypeptides, which make the HIV env protein more amenable to adopt specific conformations when contacted with gp120 ligands, may be useful as vaccines or tools to identify and characterize agents modulating HIV infection.

1,2,4-oxadiazole derivatives as immunomodulators

The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I) ##STR00001## In the formula Q is O, R.sub.1 is the side chain of Ser, R.sub.2 is —CO-Thr, R.sub.3 is the side chain of Asn or Glu, and R.sub.4, R.sub.5 and R.sub.6 are each H.

1,2,4-oxadiazole derivatives as immunomodulators

The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I) ##STR00001## In the formula Q is O, R.sub.1 is the side chain of Ser, R.sub.2 is —CO-Thr, R.sub.3 is the side chain of Asn or Glu, and R.sub.4, R.sub.5 and R.sub.6 are each H.