C07C233/87

Anti-tumor compound and the medical use thereof

The invention disclose a compound of formula (I), wherein, R.sub.1 is selected from H or C1-C6 hydrocarbon group, NH.sub.2, OH, O(CH.sub.2).sub.nCH.sub.3 (n=0, 1 or 2), N(CH.sub.3).sub.2, or CH.sub.2N(CH.sub.3).sub.2, R.sub.2 is selected from an amino acid ##STR00001##
or an hydroxy acid ##STR00002##
or OH (R.sub.1, R.sub.2 are not CH.sub.3 and OH at the same time), wherein X, Y are ##STR00003##
H, CH.sub.3, CH.sub.2OH, CH(OH)CH.sub.3, CH.sub.2SH, CH(CH.sub.3).sub.2, CH.sub.2CH(CH.sub.3).sub.2, CH(CH.sub.3)CH.sub.2CH.sub.3, CH.sub.2CH.sub.2SCH.sub.3, CH.sub.2COOH, CH.sub.2CONH.sub.2, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2NH.sub.2, or CH.sub.2CH.sub.2CONH.sub.2, R.sub.3-R.sub.5 are H or C1-C6 hydrocarbon group. The compound has a low toxicity, can significantly inhibit the migration and invasion of tumor cells in vitro, and can inhibit tumor metastasis in vivo in mice at low concentration, while showing notable sensitizing effect on cytotoxic anti-tumor drugs such as Paclitaxel etc. ##STR00004##

Compounds and methods for inducing chondrogenesis

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

Compounds and methods for inducing chondrogenesis

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

COMPOSITIONS COMPRISING AN INTEGRIN INHIBITOR AND AGENTS WHICH INTERACT WITH A CHEMOKINE AND METHODS OF USE THEREOF

The present disclosure provides therapeutic agents including those of the formula:

##STR00001##

wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such therapeutic agents. Methods of using the therapeutic agents are also provided. The present disclosure further provides combinations of a VLA-4 inhibitor and an agent which interacts with a chemokine receptor, and methods of use thereof. In some embodiments, the disclosed combinations may be used in a method of mobilizing hematopoietic stem cells. In some embodiments, the disclosed methods may be used in the treatment of a condition which requires the collection of hematopoietic stem cells for transfusions or in chemotherapy. The present disclosure further provides methods of treating a patient comprising administering an agent which interacts with a chemokine such as G-CSF, plerixafor, or Gro- and VLA-4 inhibitors.

COMPOSITIONS COMPRISING AN INTEGRIN INHIBITOR AND AGENTS WHICH INTERACT WITH A CHEMOKINE AND METHODS OF USE THEREOF

The present disclosure provides therapeutic agents including those of the formula:

##STR00001##

wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such therapeutic agents. Methods of using the therapeutic agents are also provided. The present disclosure further provides combinations of a VLA-4 inhibitor and an agent which interacts with a chemokine receptor, and methods of use thereof. In some embodiments, the disclosed combinations may be used in a method of mobilizing hematopoietic stem cells. In some embodiments, the disclosed methods may be used in the treatment of a condition which requires the collection of hematopoietic stem cells for transfusions or in chemotherapy. The present disclosure further provides methods of treating a patient comprising administering an agent which interacts with a chemokine such as G-CSF, plerixafor, or Gro- and VLA-4 inhibitors.

Taxanes compounds, preparation method therefor, and uses thereof

The present invention provides taxanes compounds with a formula (I) or formula (II) structure, a method for preparing the compounds, as well as the use of the compositions containing the compounds, pharmaceutically acceptable salts and solvates thereof as active ingredients in manufacturing oral antitumor medicaments, ##STR00001## In formula (I), R.sub.1 is COR.sub.6, COOR.sub.6 or CONR.sub.7aR.sub.7b; R.sub.2 is a C1-C6 alkyl, a C1-C6 alkenyl, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; R.sub.3 is OR.sub.6, OCOOR.sub.6, OCOSR.sub.6 or OCONR.sub.7aR.sub.7b; R.sub.4 is OR.sub.6, OCOOR.sub.6, OCOSR.sub.6, OCONR.sub.7aR.sub.7b or H; wherein, R.sub.6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; R.sub.7a and R.sub.7b are respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group. In formula (II), R.sub.1 is COR.sub.6 or COOR.sub.6; R.sub.2 is an aromatic group; R.sub.3 is OR.sub.6; wherein, R.sub.6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group.

Taxanes compounds, preparation method therefor, and uses thereof

The present invention provides taxanes compounds with a formula (I) or formula (II) structure, a method for preparing the compounds, as well as the use of the compositions containing the compounds, pharmaceutically acceptable salts and solvates thereof as active ingredients in manufacturing oral antitumor medicaments, ##STR00001## In formula (I), R.sub.1 is COR.sub.6, COOR.sub.6 or CONR.sub.7aR.sub.7b; R.sub.2 is a C1-C6 alkyl, a C1-C6 alkenyl, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; R.sub.3 is OR.sub.6, OCOOR.sub.6, OCOSR.sub.6 or OCONR.sub.7aR.sub.7b; R.sub.4 is OR.sub.6, OCOOR.sub.6, OCOSR.sub.6, OCONR.sub.7aR.sub.7b or H; wherein, R.sub.6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; R.sub.7a and R.sub.7b are respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group. In formula (II), R.sub.1 is COR.sub.6 or COOR.sub.6; R.sub.2 is an aromatic group; R.sub.3 is OR.sub.6; wherein, R.sub.6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group.

Mitochondrial aldehyde dehydrogenase-2 modulators and methods of use thereof

The present disclosure provides compounds of formula (I) that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity, and methods of preparing these compounds.

Mitochondrial aldehyde dehydrogenase-2 modulators and methods of use thereof

The present disclosure provides compounds of formula (I) that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity, and methods of preparing these compounds.

PPAR AGONISTS AND METHODS OF USE THEREOF

Provided herein are deuterated compounds and compositions useful in increasing PPAR activity. The compounds have a formula

##STR00001##

where L.sup.5 comprises at least one deuterium. Exemplary species include

##STR00002##

The compounds and compositions provided herein are useful for the treatment of PPAR related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).