Patent classifications
A61P5/28
Deuterated compounds and uses thereof
An anthraquinone compound of formula I (such as the compounds of formulae II to X) and processes for making the same are provided. Pharmaceutical compositions for use in the treatment of cancer, optionally in combination with an agent capable of reducing the level of oxygenation of a tumour, are also provided. Additionally, an option for combination with chemotherapeutic and radiotherapeutic modalities to enhance overall tumour cell kill is provided. Methods for the detection of cellular hypoxia, both in vivo and in vitro, are additionally provided. ##STR00001##
PHARMACEUTICAL COMPOSITIONS AND COMBINATIONS COMPRISING INHIBITORS OF THE ANDROGEN RECEPTOR AND USES THEREOF
The present disclosure generally relates to pharmaceutical compositions and combinations comprising an androgen receptor N-terminal domain inhibitor or an inhibitor and a second therapeutically active agent, such as an CDK4/6 inhibitor, a Pin1 inhibitor (inhibitor of peptidyl-prolyl cis/trans isomerases), or an antiandrogen. In particular, the present disclosure relates to pharmaceutical compositions and combinations useful for treatment of various cancers, for example breast cancer and prostate cancer. Further, the present disclosure relates administering an androgen receptor N-terminal domain inhibitor in combination with radiation therapy for treatment of various cancers.
SUBSTITUTED PYRAZOLE COMPOUNDS, COMPOSITIONS CONTAINING SAME, AND USE THEREOF
The present invention provides substituted pyrazole compounds, compositions containing same, and use thereof. The substituted pyrazole compounds comprise a compound represented by formula (I) or a tautomer, stereoisomer, prodrug, crystalline form, pharmaceutically acceptable salt, hydrate, or solvate thereof. The compound represented by formula (I) can serve as a tissue selective androgen receptor modulator (SARM), particularly serving as a drug for treating prostate cancer and other AR-dependent conditions and diseases in which AR antagonism is desired.
SYNTHETIC ANTIBODY MIMETIC COMPOUNDS (SYAMS) TARGETING CANCER, ESPECIALLY PROSTATE CANCER
The present invention relates to compounds which function as antibody mimetic compounds. These compounds are bifuinctional/multifuinctional compounds which contain at least one cancer cell binding moiety which selectively binds to prostate specific membrane antigen (PSMA) and a FC receptor binding moiety which modulates an FC immune receptor, preferably a FcγRI receptor. Compounds according to the present invention bind selectively to cancer cells which upregulate PSMA and through that interaction, place the Fc receptor binding moiety of the compound in proximity to a Fc receptor, preferably a FcγRI receptor, which can modulate (preferably, upregulate) a humoral response in a patient to cancer cells. Through this biological action of the compounds according to the present invention, cancer cells, including metastatic cancer cells, especially prostate cancer cells can be immune regulated, resulting in the favorable therapy of cancer in a patient. Methods of using these compounds to treat cancer and/or reduce the likelihood of metastatis of cancer are additional aspects of the present invention.
NUTRACEUTICAL FORMULATION FOR POLYCYSTIC OVARY SYNDROME
Nutraceutical food supplement for treatment of young women in post-puberty age suffering from polycystic ovary syndrome with symptoms like irregular menstruation cycles, insulin resistant diabetes, infertility, hair loss, acne and weight gain is provided. Formulations having myo-inositol and its D-chiro isomer along with plant proteins, a carbohydrate (inulin) and other plant fibres; along with well-defined proportions of vitamins (A, B.sub.1 to 6; B.sub.12 and C); several minerals like Ca, Cr, Fe, K, Mg, Mn, Na and Zn and essential amino acids like L-Glutamine, L-Lysine, and L-Taurine are provided.
NUTRACEUTICAL FORMULATION FOR POLYCYSTIC OVARY SYNDROME
Nutraceutical food supplement for treatment of young women in post-puberty age suffering from polycystic ovary syndrome with symptoms like irregular menstruation cycles, insulin resistant diabetes, infertility, hair loss, acne and weight gain is provided. Formulations having myo-inositol and its D-chiro isomer along with plant proteins, a carbohydrate (inulin) and other plant fibres; along with well-defined proportions of vitamins (A, B.sub.1 to 6; B.sub.12 and C); several minerals like Ca, Cr, Fe, K, Mg, Mn, Na and Zn and essential amino acids like L-Glutamine, L-Lysine, and L-Taurine are provided.
Indazole-3-carboxamides and their use as WNT/B-catenin signaling pathway inhibitors
Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
Modified Mullerian inhibiting substance (MIS) proteins and uses thereof for the treatment of diseases
The present invention relates to modified recombinant human MIS protein which has improved cleavage and increased bioactivity and increased potency as compared to wild-type human MIS protein. Other aspects of the invention relate to methods to prevent and treat cancers, such as cancers that express the MIS receptor type II (MISRII) by administering to a subject a composition comprising a recombinant human MIS protein. Another aspect of the present invention relates to methods to lower plasma androgen levels in a subject, and/or for the treatment of a subject with a disease characterized by excess androgen. Another aspect provides pharmaceutical compositions and kits and methods for use comprising a recombinant human MIS protein. Another aspect of the present invention relates to methods to decrease the dose of a chemotherapeutic agent by administering the chemotherapeutic agent with the recombinant MIS protein that lowers the effective dose of the chemotherapeutic agent.
Modified Mullerian inhibiting substance (MIS) proteins and uses thereof for the treatment of diseases
The present invention relates to modified recombinant human MIS protein which has improved cleavage and increased bioactivity and increased potency as compared to wild-type human MIS protein. Other aspects of the invention relate to methods to prevent and treat cancers, such as cancers that express the MIS receptor type II (MISRII) by administering to a subject a composition comprising a recombinant human MIS protein. Another aspect of the present invention relates to methods to lower plasma androgen levels in a subject, and/or for the treatment of a subject with a disease characterized by excess androgen. Another aspect provides pharmaceutical compositions and kits and methods for use comprising a recombinant human MIS protein. Another aspect of the present invention relates to methods to decrease the dose of a chemotherapeutic agent by administering the chemotherapeutic agent with the recombinant MIS protein that lowers the effective dose of the chemotherapeutic agent.
Development of a standardized and effect-optimized herbal extract of <i>Wedelia chinensis </i>and its use for treating disease
A composition including a standardized Wedelia chinensis extract and a method of treating an androgen-stimulated disorder with such a composition. Also provided are a method for qualifying a standardized preparation of a Wedelia chinensis extract for treating an androgen-stimulated disorder and a method for treating said disorder with a thus qualified preparation.