Abstract:
The disclosure relates to selective small molecule dual activators of human constitutive androstane receptor (hCAR) and nuclear factor erythroid 2-related factor 2 (Nrf2), pharmaceutical compositions thereof, and use thereof for the treatment of hematologic malignancies and other cancers. The small molecule dual hCAR and Nrf2 activators in combination with CPA based chemotherapy regimen provides a synergistic effect to help promote cytoxicity of the cyclophosphamide (CPA) based and doxorubicin (DOX) based anticancer treatments including CHOP regimen (CPA, doxorubicin, vincristine, and prednisone) while reducing cardiotixocity associated with DOX.
Abstract:
A compound comprises a donor and an acceptor, wherein at least one donor ( "D" ) and at least one acceptor ( "A" ) may be arranged in an order of D-A; D-A-D; A-D-A; D-D-A-D-D; A-A-D-A-A; D-A-D-A-D; and A-D-A-D-A. The compound may be selected from the group consisting of: MTPE-TP, MTPE-TT, TPE-TPA-TT, PTZ-BT-TPA, NPB-TQ, TPE-TQ-A, MTPE-BTSe, DCDPP-2TPA, DCDPP-2TPA4M, DCDP-2TPA, DCDP-2TPA4M, TTS, ROpen-DTE-TPECM, and RClosed-DTE-TPECM. The compound may be used as a probe and may be functionalized with special targeted groups to image biological species. As non-limiting examples, the compound may be used in cellular cytoplasms or tissue imaging, blood vessel imaging, in vivo fluorescence imaging, brain vascular imaging, sentinel lymph node mapping, and tumor imaging, and the compound may be used as a photoacoustic agent.
Abstract:
The present invention relates to a novel process for the preparation of polymorphic forms of clopidogrel hydrogen sulfate, namely methyl (+)-(S)-α-(o-chlorophenyl)-6,7-dihydrotliieno [3,2-c] pyridine-5(4H)-acetate hydrogen sulfate of formula (I). Particularly the present invention relates to the process for the preparation of form (I) and amorphous clopidogrel hydrogen sulfate.
Abstract:
The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Abstract:
Provided are chemical entities chosen from compounds of Formula (I) and pharmaceutically or cosmetically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof. The chemical entities modulate TRPV1 and are useful in the treatment of at least one disease or disorder modulated by TRPV1 activity.
Abstract:
The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.
Abstract:
Compositions and methods for treating cancer, including hematologic cancers such as multiple myeloma, are disclosed. In some embodiments, chaetocin, chaetomin, or gliotoxin can be used to treat or ameliorate one or more symptoms or disorders associated with multiple myeloma.
Abstract:
The invention relates to compounds having progestogenic activity and to their use. The invention discloses a compound having the general formula (I) wherein Y, Y', X and X' are independently selected from the group consisting of O, S and N; R 1 is selected from the group consisting of optionally substituted C 1-8 alkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 2-6 alkynyl, optionally substituted C 1-6 alkoxy, optionally substituted C1-6 thioalkyl, optionally substituted C4-10 aryl, optionally substituted C 6-11 alkylaryl, optionally substituted C 1-6 alkylamino, optionally substituted C 1-6 alkylcarbonyl, optionally substituted C 1-6 alkylsulfonamino, optionally substituted (C 1 -C 6 )alkylsulfinyl, optionally substituted C 1-6 alkylcarbonylamino, optionally substituted hetero(C 5 -C 10 )aryl, hydroxyl, halogen, cyano, nitro, amino, formyl, and thiol; R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are independently selected from the group consisting of hydrogen, optionally substituted C 1-8 alkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 2-6 alkynyl, optionally substituted C 1-6 alkoxy, optionally substituted C 1-6 thioalkyl, optionally substituted C 5-10 aryl, optionally substituted C 6-11 alkylaryl, optionally substituted C 1-6 alkylamino, optionally substituted C 1-6 alkylcarbonyl, optionally substituted C 1-6 alkylsulfonamino, optionally substituted (C 1 -C 6 )alkylsulfinyl, optionally substituted C 1-6 alkylcarbonylamino, optionally substituted hetero(C 5 -C 10 )aryl, hydroxyl, halogen, cyano, nitro, amino, formyl, and thiol; ---- indicates an optional double bond.
Abstract:
Compounds of formula I, that modulate DCAF15 and induce RBM39 protein degradation, pharmaceutical compositions containing these compounds, and methods of using these compounds for treating diseases associated with RBM39 protein activity and DCAF15 modulation are described herein.