Patent classifications
A61P5/28
Selective androgen receptor degrader (SARD) ligands and methods of use thereof
This invention provides novel 3-amino propanamide selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other 5 hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
Selective androgen receptor degrader (SARD) ligands and methods of use thereof
This invention provides novel 3-amino propanamide selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other 5 hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
PARTICULAR PYRIDINEDICARBOXYLIC ACID DERIVATIVE/ANTIOXIDANT COMBINATION
The invention relates to a cosmetic composition comprising one or more pyridinedicarboxylic acid derivatives of general formula (I) or a salt thereof and one or more antioxidants chosen from flavone heterosides, polyhydroxylated stilbenes, pyrimidinecarboxylic acid derivatives and ascorbic acid esters.
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METHODS FOR PREPARING ANTIBODY DRUG CONJUGATES
The subject matter described herein is directed to methods of preparing certain antibody-drug conjugates (ADCs) wherein the antibody is linked to the drug through a linker, wherein the drug contains a heteroaryl group having a secondary nitrogen, and the linker is attached to the drug via the secondary nitrogen. The resulting conjugates are useful in treating various diseases and conditions.
ANDROGEN RECEPTOR PROTEIN DEGRADERS
The present disclosure provides compounds represented by Formula I: A-L-B.sup.1 and the salts or solvates thereof, wherein A, L, and B1 are as defined in the specification. Compounds having Formula I are androgen receptor degraders useful for the treatment of cancer and other diseases.
Methods for preparing antibody drug conjugates
The subject matter described herein is directed to methods of preparing certain antibody-drug conjugates (ADCs) wherein the antibody is linked to the drug through a linker, wherein the drug contains a heteroaryl group having a secondary nitrogen, and the linker is attached to the drug via the secondary nitrogen. The resulting conjugates are useful in treating various diseases and conditions.
Anti-androgens for the treatment of non-metastatic castrate-resistant prostate cancer
Described herein are methods of treating non-metastatic castrate-resistant prostate cancer with anti-androgens.
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.
PROGNOSTIC PATHWAYS FOR HIGH RISK SEPSIS PATIENTS
The present invention relates to means and methods that can be used—based on a blood sample of a subject having sepsis, a subject suspected to have sepsis or a subject at risk to develop sepsis, to diagnose the subject with sepsis. The methods can further be used for making a prediction, e.g. whether the subject is likely to develop sepsis, or whether the subject has a high mortality risk as a result of sepsis. The invention further provides for compounds for use in the treatment or prevention of sepsis.
ENZYMATIC PROCESS FOR OBTAINING 17 ALPHA-MONOESTERS OF CORTEXOLONE AND/OR ITS 9,11-DEHYDRODERIVATIVES
The present invention refers to a new enzymatic process for obtaining 17α-monoesters of cortexolone and/or its 9, 11-dehydroderivatives starting from the corresponding 17α,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone-17α-propionate and 9,11-dehydro-cortexolone 17α-butanoate.