Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.

The present disclosure provides a benzene fused heterocyclic derivative of Formula (I): is a single or double bond; n is an integer of 0 or 1; A is CH.sub.2, CH(OH), or C(O); G is C or N; X is CH.sub.2, O, or C(O); Y is alkyl, aryl, or heterocyclic alkyl optionally substituted with at least one substituent independently selected from a group consisting of: H, halogen, alkyl, alkyl substituted with at least one halogen, aryl, aryl substituted with at least one halogen, NR.sub.y1R.sub.y2, OR.sub.y1, R.sub.y1C(O)R.sub.y3, C(O)R.sub.y1, C(O)OR.sub.y2, C(O)OR.sub.y2Ry3, NR.sub.y1C(O)R.sub.y2, NR.sub.y1C(O)NR.sub.y2R.sub.y3, NR.sub.y1C(O)OR.sub.y2R.sub.y3, NR.sub.y1C(O)R.sub.y2OR.sub.y3, C(O)NR.sub.y1(R.sub.y2R.sub.y3), C(O)NR.sub.y1(R.sub.y2OR.sub.y1), OR.sub.y2R.sub.y3, and OR.sub.y2OR.sub.y3, wherein each of R.sub.y1 and R.sub.y2 is independently selected from a group consisting of H, oxygen, alkyl, and aryl, and R.sub.y3 is aryl optionally substituted with at least one halogen; Z is NR.sub.z1R.sub.z2, NR.sub.z1R.sub.z3, OR.sub.z1, OR.sub.z1R.sub.z3, C(O)R.sub.z1R.sub.z3, C(O)OR.sub.z1R.sub.z3, NR.sub.z1C(O)R.sub.z2R.sub.z3, NR.sub.z1C(O)OR.sub.z2R.sub.z3, C(O)NR.sub.z1R.sub.z3, or OR.sub.z2OR.sub.z3, wherein each of R.sub.z1 and R.sub.z2 is independently selected from a group consisting of H, oxygen, alkyl and aryl, and R.sub.z3 is aryl optionally substituted with at least one substituent independently selected from a group consisting of halogen, OH, R.sub.zaCOOR.sub.zb, OR.sub.zaCOOR.sub.zb, R.sub.zaSO.sub.2R.sub.zb, R.sub.zaSO.sub.2NR.sub.zbR.sub.zcR.sub.zd, R.sub.zaC(O)R.sub.zbR.sub.zc, R.sub.zaC(O)NR.sub.zbR.sub.zcR.sub.zd, RZ.sub.aC(O)NR.sub.zbSO.sub.2R.sub.zc, wherein Rza is nil or alkyl, R.sub.zb is H or alkyl, each of R.sub.zb and R.sub.zc is independently selected from a group consisting of H, OH, alkyl, aryl, alkoxyl, or NR.sub.zbR.sub.zc is a nitrogen-containing heterocyclic alkyl ring, R.sub.zd is nil or a sulfonyl alkyl group.

##STR00001##

The present disclosure provides a benzene fused heterocyclic derivative of Formula (I): is a single or double bond; n is an integer of 0 or 1; A is CH.sub.2, CH(OH), or C(O); G is C or N; X is CH.sub.2, O, or C(O); Y is alkyl, aryl, or heterocyclic alkyl optionally substituted with at least one substituent independently selected from a group consisting of: H, halogen, alkyl, alkyl substituted with at least one halogen, aryl, aryl substituted with at least one halogen, NR.sub.y1R.sub.y2, OR.sub.y1, R.sub.y1C(O)R.sub.y3, C(O)R.sub.y1, C(O)OR.sub.y2, C(O)OR.sub.y2Ry3, NR.sub.y1C(O)R.sub.y2, NR.sub.y1C(O)NR.sub.y2R.sub.y3, NR.sub.y1C(O)OR.sub.y2R.sub.y3, NR.sub.y1C(O)R.sub.y2OR.sub.y3, C(O)NR.sub.y1(R.sub.y2R.sub.y3), C(O)NR.sub.y1(R.sub.y2OR.sub.y1), OR.sub.y2R.sub.y3, and OR.sub.y2OR.sub.y3, wherein each of R.sub.y1 and R.sub.y2 is independently selected from a group consisting of H, oxygen, alkyl, and aryl, and R.sub.y3 is aryl optionally substituted with at least one halogen; Z is NR.sub.z1R.sub.z2, NR.sub.z1R.sub.z3, OR.sub.z1, OR.sub.z1R.sub.z3, C(O)R.sub.z1R.sub.z3, C(O)OR.sub.z1R.sub.z3, NR.sub.z1C(O)R.sub.z2R.sub.z3, NR.sub.z1C(O)OR.sub.z2R.sub.z3, C(O)NR.sub.z1R.sub.z3, or OR.sub.z2OR.sub.z3, wherein each of R.sub.z1 and R.sub.z2 is independently selected from a group consisting of H, oxygen, alkyl and aryl, and R.sub.z3 is aryl optionally substituted with at least one substituent independently selected from a group consisting of halogen, OH, R.sub.zaCOOR.sub.zb, OR.sub.zaCOOR.sub.zb, R.sub.zaSO.sub.2R.sub.zb, R.sub.zaSO.sub.2NR.sub.zbR.sub.zcR.sub.zd, R.sub.zaC(O)R.sub.zbR.sub.zc, R.sub.zaC(O)NR.sub.zbR.sub.zcR.sub.zd, RZ.sub.aC(O)NR.sub.zbSO.sub.2R.sub.zc, wherein Rza is nil or alkyl, R.sub.zb is H or alkyl, each of R.sub.zb and R.sub.zc is independently selected from a group consisting of H, OH, alkyl, aryl, alkoxyl, or NR.sub.zbR.sub.zc is a nitrogen-containing heterocyclic alkyl ring, R.sub.zd is nil or a sulfonyl alkyl group.

##STR00001##

The present invention provides a pharmaceutical composition for treating or preventing a cognitive disease or disorder, comprising a compound represented by Formula (I), an enantiomer thereof a diastereomer thereof, or a pharmaceutically acceptable salt thereof.

The present invention provides a pharmaceutical composition for treating or preventing a cognitive disease or disorder, comprising a compound represented by Formula (I), an enantiomer thereof a diastereomer thereof, or a pharmaceutically acceptable salt thereof.

An object of the present invention is to provide a composition capable of forming a film having a high refractive index and excellent exterior characteristics. Another object of the present invention is to provide a film, a lens, and a solid-state imaging element in which the composition is used. Still another object of the present invention is to provide novel compounds.

The composition according to an embodiment of the present invention contains a compound represented by General Formula (I), a solvent, and a resin, in which a solubility of the compound represented by General Formula (I) in the solvent is less than 0.5% by mass at 25 C., and a maximum absorption wavelength of the compound represented by General Formula (I) at a wavelength range of 300 to 800 nm is equal to or shorter than 450 nm.

AB-C).sub.n (I)

Disclosed are small molecule PLK inhibitors that can target the polo box domain (PBD). Inhibitors can have an atomic mass of about 1000 Da or less and a general structure of

##STR00001##

For instance, the inhibitors can include an alkyl benzamido benzoic acid core structure.

Disclosed are small molecule PLK inhibitors that can target the polo box domain (PBD). Inhibitors can have an atomic mass of about 1000 Da or less and a general structure of

##STR00001##

For instance, the inhibitors can include an alkyl benzamido benzoic acid core structure.

Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K activity, including compounds that selectively inhibit PI3K activity. Methods of using PI3K inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K inhibitory compounds to inhibit PI3K-mediated processes in vitro and in vivo.

The present invention is directed to benzamide-containing compounds of formula I

##STR00001##

or pharmaceutically acceptable salts thereof which inhibit the P2X.sub.7 receptor, and their use in the treatment of depression.