Patent classifications
A61K31/504
INHIBITION OF RIP KINASES FOR TREATING NEURODEGENERATIVE DISORDERS
Provided herein are compositions comprising a RIPK2 inhibitor and methods of using the RIPK2 inhibitor for treating or preventing neurodegenerative diseases or disorders. Also provided herein are methods of screening or identifying therapeutic agents useful for treating or preventing neurodegenerative diseases or disorders.
SMALL MOLECULE INHIBITORS OF THE NUCLEAR TRANSLOCATION OF ANDROGEN RECEPTOR FOR THE TREATMENT OF CASTRATION-RESISTANT PROSTATE CANCER
A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I:
R.sup.20—(Z).sub.b—(Y).sub.c—(R.sup.21).sub.a—(X).sub.d—R.sup.22—R.sup.23
wherein R.sup.20 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, S(═O), S(═O)(═O)—, or NR.sup.10, wherein R.sup.10 is H or alkyl; R.sup.21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, cycloalkenediyl, substituted cycloalkenediyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)—, —S(═O)(═O)—, or —N(H)C(═O)—; R.sup.22 includes at least one divalent amino radical; R.sup.23 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.
SMALL MOLECULE INHIBITORS OF THE NUCLEAR TRANSLOCATION OF ANDROGEN RECEPTOR FOR THE TREATMENT OF CASTRATION-RESISTANT PROSTATE CANCER
A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I:
R.sup.20—(Z).sub.b—(Y).sub.c—(R.sup.21).sub.a—(X).sub.d—R.sup.22—R.sup.23
wherein R.sup.20 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, S(═O), S(═O)(═O)—, or NR.sup.10, wherein R.sup.10 is H or alkyl; R.sup.21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, cycloalkenediyl, substituted cycloalkenediyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)—, —S(═O)(═O)—, or —N(H)C(═O)—; R.sup.22 includes at least one divalent amino radical; R.sup.23 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.
3-beta-hydroxy-5-alpha-pregnan-20-one for use in medical treatment
The present invention provides the steroid compound 3beta-hydroxy-5alpha-pregnan-20-one for use in treatment of Tourette's syndrome, obsessive compulsive disorder and/or gambling disorder, as well as methods for treating said disorders and pharmaceutical compositions for use in treatment of said disorders.
Small molecule inhibitors of the nuclear translocation of androgen receptor for the treatment of castration-resistant prostate cancer
A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I:
R.sup.20—(Z).sub.b—(Y).sub.c—(R.sup.21).sub.a—(X).sub.d—R.sup.22—R.sup.23
wherein R.sup.20 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, S(═O), —S(═O)(═O)—, or NR.sup.10, wherein R.sup.10 is H or alkyl; R.sup.21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, cycloalkenediyl, substituted cycloalkenediyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)—, —S(═O)(═O)—, or —N(H)C(═O)—; R.sup.22 includes at least one divalent amino radical; R.sup.23 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.
Small molecule inhibitors of the nuclear translocation of androgen receptor for the treatment of castration-resistant prostate cancer
A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I:
R.sup.20—(Z).sub.b—(Y).sub.c—(R.sup.21).sub.a—(X).sub.d—R.sup.22—R.sup.23
wherein R.sup.20 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, S(═O), —S(═O)(═O)—, or NR.sup.10, wherein R.sup.10 is H or alkyl; R.sup.21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, cycloalkenediyl, substituted cycloalkenediyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)—, —S(═O)(═O)—, or —N(H)C(═O)—; R.sup.22 includes at least one divalent amino radical; R.sup.23 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.
PHARMACEUTICAL COMPOSITION
[Problem to be solved]
The present invention addresses the problem of providing a pharmaceutical composition for the prevention and/or treatment of diseases related to pulmonary fibrosis.
[Solution]
Provided is a pharmaceutical composition for the prevention and/or treatment of diseases involving pulmonary fibrosis, in which the active ingredient is 3-[2-(5-{[1-(5-ethoxypyrimidin-2-yl)-2-isopropyl-6-oxo-4-propyl-1,6-dihydropyrimidin-5-yl]methyl}pyridin-2-yl)phenyl]-1,2,4-oxadiazol-5(4H)-one, or a salt thereof, or a solvate of these.
PHARMACEUTICAL COMPOSITION
[Problem to be solved]
The present invention addresses the problem of providing a pharmaceutical composition for the prevention and/or treatment of diseases related to pulmonary fibrosis.
[Solution]
Provided is a pharmaceutical composition for the prevention and/or treatment of diseases involving pulmonary fibrosis, in which the active ingredient is 3-[2-(5-{[1-(5-ethoxypyrimidin-2-yl)-2-isopropyl-6-oxo-4-propyl-1,6-dihydropyrimidin-5-yl]methyl}pyridin-2-yl)phenyl]-1,2,4-oxadiazol-5(4H)-one, or a salt thereof, or a solvate of these.
COMPOUNDS THAT PARTICIPATE IN COOPERATIVE BINDING AND USES THEREOF
The disclosure features macrocyclic compounds, alone and in combination with other therapeutic agents, as well as pharmaceutical compositions and protein complexes thereof, capable of modulating biological processes including RAS and RAS-RAF inhibition, and their uses in the treatment of cancers.
COMPOUNDS THAT PARTICIPATE IN COOPERATIVE BINDING AND USES THEREOF
The disclosure features macrocyclic compounds, alone and in combination with other therapeutic agents, as well as pharmaceutical compositions and protein complexes thereof, capable of modulating biological processes including RAS and RAS-RAF inhibition, and their uses in the treatment of cancers.