Patent classifications
A61K31/504
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.dR.sup.22R.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.
Autotaxin inhibitors
The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.
Autotaxin inhibitors
The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.
Autotaxin inhibitors
The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.
NOVEL MACROCYCLIC AMINOPYRAZOLE COMPOUNDS AS CDK2 INHIBITORS
The present disclosure relates to a compound of Formula (I), a tautomer, a stereoisomer or a mixture of stereoisomers, a pharmaceutically acceptable salt, a hydrate, or a deuterated derivative thereof and their use in, e.g., treating a disease or disorder associated with CDK2. The present disclosure also relates to pharmaceutical compositions containing such compounds, and their use in treating or preventing a disease or disorder associated with CDK2.
NOVEL MACROCYCLIC AMINOPYRAZOLE COMPOUNDS AS CDK2 INHIBITORS
The present disclosure relates to a compound of Formula (I), a tautomer, a stereoisomer or a mixture of stereoisomers, a pharmaceutically acceptable salt, a hydrate, or a deuterated derivative thereof and their use in, e.g., treating a disease or disorder associated with CDK2. The present disclosure also relates to pharmaceutical compositions containing such compounds, and their use in treating or preventing a disease or disorder associated with CDK2.
NLRP3 INFLAMMASOME INHIBITOR AND APPLICATION THEREOF
The present invention belongs to the technical field of medicines, relates to an NLRP3 inflammasome inhibitor and use thereof, and particularly relates to a compound of general formula (I), or a pharmaceutically acceptable salt, a stereoisomer or a tautomer thereof, wherein each group is defined in the specification. Researches show that the compound of general formula (I), or pharmaceutically acceptable salt, the stereoisomer or the tautomer thereof has relatively high biological activity on NLRP3 inflammasomes and has an important clinical development value for the treatment of NLRP3-associated diseases.
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CRYSTALLINE FORMS OF RAS INHIBITORS, COMPOSITIONS CONTAINING THE SAME, AND METHODS OF USE THEREOF
The disclosure features crystalline forms of Ras inhibitors, pharmaceutical compositions thereof, and their uses in the treatment of cancers.
CRYSTALLINE FORMS OF RAS INHIBITORS, COMPOSITIONS CONTAINING THE SAME, AND METHODS OF USE THEREOF
The disclosure features crystalline forms of Ras inhibitors, pharmaceutical compositions thereof, and their uses in the treatment of cancers.
AUTOTAXIN INHIBITORS
The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.