Patent classifications
A61K31/403
N-CYANO-7-AZANORBORNANE DERIVATIVES AND USES THEREOF
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
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Role Of Novel Carbazole Linked 1, 2, 3- Triazole Analogs in Alleviating Methylglyoxal-Mediated Late Diabetic Vascular Complications
The present intervention identifies the antiglycating inhibitors from a series of carbazole-linked 1,2,3 triazole derivatives through in vitro MGO-mediated glycating BSA model. Derivatives 12, and 13 established a remarkable antiglycation activity at the receptor level in human monocytes. These compounds were found non-toxic, and possess the potential to halt AGE-RAGE/ROS- mediated NF- kB-dependent COX-2, and its proinflammatory product, PGE.sub.2, production in monocytes. Hence, carbazole-linked 1,2,3 triazole derivatives provide treatment modalities to delay or prevent the onset of late diabetic micro- and macro-vascular complications in diabetic patients.
Role Of Novel Carbazole Linked 1, 2, 3- Triazole Analogs in Alleviating Methylglyoxal-Mediated Late Diabetic Vascular Complications
The present intervention identifies the antiglycating inhibitors from a series of carbazole-linked 1,2,3 triazole derivatives through in vitro MGO-mediated glycating BSA model. Derivatives 12, and 13 established a remarkable antiglycation activity at the receptor level in human monocytes. These compounds were found non-toxic, and possess the potential to halt AGE-RAGE/ROS- mediated NF- kB-dependent COX-2, and its proinflammatory product, PGE.sub.2, production in monocytes. Hence, carbazole-linked 1,2,3 triazole derivatives provide treatment modalities to delay or prevent the onset of late diabetic micro- and macro-vascular complications in diabetic patients.
METHOD FOR TREATMENT OF PANCREATITIS
A composition for preventing and/or treating pancreatitis and a method of prevention and/or treatment of pancreatitis are disclosed. The composition include an aryl ethene compound, a pharmaceutically acceptable salt thereof, or a solvate thereof, as an active ingredient. Also disclosed is a use of the aryl ethene compound, a pharmaceutically acceptable salt thereof, or a solvate thereof, in manufacturing a medicament for preventing and/or treating pancreatitis or for treating one or more symptoms of pancreatitis in a patient. The method of prevention and/or treatment of pancreatitis includes administering the aryl ethene compound, an isomer, a pharmaceutically acceptable salt thereof, or a solvate thereof, in an effective amount to a subject in need thereof.
METHOD FOR TREATMENT OF PANCREATITIS
A composition for preventing and/or treating pancreatitis and a method of prevention and/or treatment of pancreatitis are disclosed. The composition include an aryl ethene compound, a pharmaceutically acceptable salt thereof, or a solvate thereof, as an active ingredient. Also disclosed is a use of the aryl ethene compound, a pharmaceutically acceptable salt thereof, or a solvate thereof, in manufacturing a medicament for preventing and/or treating pancreatitis or for treating one or more symptoms of pancreatitis in a patient. The method of prevention and/or treatment of pancreatitis includes administering the aryl ethene compound, an isomer, a pharmaceutically acceptable salt thereof, or a solvate thereof, in an effective amount to a subject in need thereof.
Dual antagonist of PGD.SUB.2./DPr2 and Thromboxane A.SUB.2./TPr receptors and use for treatment of maladaptive immune response or thrombotic diathesis
The present invention relates to a pharmaceutical composition for treatment of a disease or condition characterized by or associated with stimulation of both DPr2 and TPr signaling, said composition comprising an effective amount of a dual receptor antagonist of DPr.sub.2 for prostaglandin D.sub.2 and TPr for thromboxane A.sub.2 and a pharmaceutically acceptable carrier.
Dual antagonist of PGD.SUB.2./DPr2 and Thromboxane A.SUB.2./TPr receptors and use for treatment of maladaptive immune response or thrombotic diathesis
The present invention relates to a pharmaceutical composition for treatment of a disease or condition characterized by or associated with stimulation of both DPr2 and TPr signaling, said composition comprising an effective amount of a dual receptor antagonist of DPr.sub.2 for prostaglandin D.sub.2 and TPr for thromboxane A.sub.2 and a pharmaceutically acceptable carrier.
1,5-DISUBSTITUTED 1,2,3-TRIAZOLES ARE INHIBITORS OF RAC/CDC42 GTPASES
Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.
SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/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 indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.