An incretin analogue, a preparation method therefor, and the use thereof. The incretin analogue has a GLP-1R/GIPR/GCGR agonist activity, is a triple agonist, and can be used for lowering blood glucose, reducing fat and reducing weight.

An incretin analogue, a preparation method therefor, and the use thereof. The incretin analogue has a GLP-1R/GIPR/GCGR agonist activity, is a triple agonist, and can be used for lowering blood glucose, reducing fat and reducing weight.

The present invention provides parenteral pharmaceutical compositions comprising therapeutically effective amounts of semaglutide or pharmaceutically acceptable salts thereof, the parenteral pharmaceutical compositions are formulated in depot form and provide low-burst release and a continued release profile. The present invention further provides methods of use of the parenteral pharmaceutical compositions for treating type-2 diabetes mellitus, obesity, and Parkinson's disease.

The present invention provides parenteral pharmaceutical compositions comprising therapeutically effective amounts of semaglutide or pharmaceutically acceptable salts thereof, the parenteral pharmaceutical compositions are formulated in depot form and provide low-burst release and a continued release profile. The present invention further provides methods of use of the parenteral pharmaceutical compositions for treating type-2 diabetes mellitus, obesity, and Parkinson's disease.

A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CB.sub.1 receptor mediating scaffold conjugated to (ii) a second therapeutic scaffold.

Compositions and methods of treating hyperglycemia in a subject having such a condition are disclosed. An inhibitor compound which causes activity of Cullin RING E3 ligases (CRL) to be reduced is administered to the subject, wherein blood glucose concentration is decreased. In at least certain embodiments insulin secretion and insulin sensitization in the subject are increased. Inhibition of CRL activity, e.g., by decreasing cullin neddylation by inhibiting NEDD8-activating enzyme (NAE), or decreasing cullin activity, e.g., by inhibiting expression of cullins, is shown herein to delay IRS protein turnover in liver cells and muscle cells, thereby increasing cellular response to insulin and decreasing blood glucose. Thus, inhibition of CRLs, for example by inhibiting neddylation, is an effective method to treat hyperglycemia and insulin resistance, and to increase insulin secretion in patients with hyperglycemia, for example due to type-2 diabetes.

Methods of treating anti-inflammatory conditions through the use of boron-containing small molecules are disclosed.

The invention relates to compounds of formula ##STR00001##
wherein R, R.sup.1, R.sup.2, X, and Y are as defined herein and to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease 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.

The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) ##STR00001##
and also the preparation and use of the crystalline polymorph I of (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I).