Patent classifications
C07D239/38
Hetroarylamine compounds for modulating the hedgehog pathway and preparing method and uses thereof
The present invention provides a compound of formula (1): ##STR00001##
wherein X, Y, Z.sub.1, Z.sub.2, R.sub.1, R.sub.2, A, B, p and q are as disclosed in the specification. A pharmaceutical composition and a method for modulating the Hedgehog pathway are also provided. The present invention rurthe r provides a process for preparing the compound.
Hetroarylamine compounds for modulating the hedgehog pathway and preparing method and uses thereof
The present invention provides a compound of formula (1): ##STR00001##
wherein X, Y, Z.sub.1, Z.sub.2, R.sub.1, R.sub.2, A, B, p and q are as disclosed in the specification. A pharmaceutical composition and a method for modulating the Hedgehog pathway are also provided. The present invention rurthe r provides a process for preparing the compound.
Heat shock protein binding compounds, compositions, and methods for making and using same
The present subject matter relates to a compound represented by the general formula (I) or (I) or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).
Heat shock protein binding compounds, compositions, and methods for making and using same
The present subject matter relates to a compound represented by the general formula (I) or (I) or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).
SULFONYLUREAS AND SULFONYLTHIOUREAS AS NLRP3 INHIBITORS
The present invention relates to compounds of formula (I):
##STR00001##
wherein Q is O or S, R.sup.1 is a 6-membered heteroaryl group containing at least one nitrogen atom in the 6-membered ring structure, wherein R.sup.1 may optionally be substituted, and R.sup.2 is a cyclic group substituted at the -position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
SULFONYLUREAS AND SULFONYLTHIOUREAS AS NLRP3 INHIBITORS
The present invention relates to compounds of formula (I):
##STR00001##
wherein Q is O or S, R.sup.1 is a 6-membered heteroaryl group containing at least one nitrogen atom in the 6-membered ring structure, wherein R.sup.1 may optionally be substituted, and R.sup.2 is a cyclic group substituted at the -position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
Ketone inhibitors of lysine gingipain
The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
Ketone inhibitors of lysine gingipain
The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
IDO/TDO Inhibitor
A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, an aliphatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, an aliphatic ring and a heterocyclic ring; X, R.sup.1 and R.sup.2 represent a substituent on a ring atom constituting ring A; m represents an integer of 0 to 6; X represents, for example, a halogen atom; and R.sup.1 and R.sup.2 are the same or different and are selected from, for example, the group consisting of groups of formula (a) or formula (b); and in the following formula (a) and formula (b), Y is selected from the group consisting of O, S, and Se, Z is selected from the group consisting of O, S, and Se, n represents an integer of 1 to 8, r represents an integer of 1 to 8, s represents an integer of 1 to 8, R.sup.4 represents, for example, C(NH)HN.sub.2, and R.sup.6 represents, for example, a substituted or unsubstituted aryl group].
##STR00001##
INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE
The present disclosure discloses compounds capable of modulating the activity of -amino--carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD.sup.+ biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.