A61P9/10

USE OF SENICAPOC FOR TREATMENT OF STROKE
20230045322 · 2023-02-09 ·

Neuroinflammation mediated by microglia and infiltrating peripheral immune cells is a major component of stroke pathophysiology. The calcium activated potassium channel K.sub.Ca3.1 is expressed selectively in the injured CNS by microglia, and K.sub.Ca3.1 function has been implicated in proinflammatory activation of microglia. K.sub.Ca3.1 is further implicated in the pathophysiology of ischemia/reperfusion (stroke) related brain injury. Senicapoc, an investigational drug with a proven safety profile and shown to cross the blood-brain barrier, is a potent and selective K.sub.Ca3.1 inhibitor that intervenes in the inflammation cascade that follows ischemia/reperfusion, and is a potential treatment for stroke.

USE OF SENICAPOC FOR TREATMENT OF STROKE
20230045322 · 2023-02-09 ·

Neuroinflammation mediated by microglia and infiltrating peripheral immune cells is a major component of stroke pathophysiology. The calcium activated potassium channel K.sub.Ca3.1 is expressed selectively in the injured CNS by microglia, and K.sub.Ca3.1 function has been implicated in proinflammatory activation of microglia. K.sub.Ca3.1 is further implicated in the pathophysiology of ischemia/reperfusion (stroke) related brain injury. Senicapoc, an investigational drug with a proven safety profile and shown to cross the blood-brain barrier, is a potent and selective K.sub.Ca3.1 inhibitor that intervenes in the inflammation cascade that follows ischemia/reperfusion, and is a potential treatment for stroke.

Bile acid synthesis promoter, composition for promoting bile acid synthesis and food composition for promoting bile acid synthesis

[Problem] To provide a novel medicine that is capable of promoting cholesterol metabolism to thereby treat, ameliorate or prevent various symptoms associated with increase in blood cholesterol level. [Solution] The present inventors newly found that arctigenin has an effect of promoting the conversion of cholesterol into bile acid. The present invention provides a bile acid synthesis promoter, a composition for promoting bile acid synthesis and a food composition for promoting bile acid synthesis each comprising arctigenin and/or arctiin as active ingredient(s).

Purine diones as Wnt pathway modulators

The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.

Methods for treating disorders or diseases associated with hyperlipidemia and hypercholesterolemia while minimizing side-effects

The present invention provides methods and compositions for treating hyperlipidemia and/or hypercholesterolemia comprising administering to the subject an effective amount of an MTP inhibitor to inhibit hyperlipidemia and/or hypercholesterolemia in said subject, wherein said administration comprises an escalating series of doses of the MTP inhibitor. In some embodiments the method comprises administering at least three step-wise, increasing dosages of the MTP inhibitor to the subject. In some embodiments, the method further comprises the administration of one or more other lipid modifying compounds.

N-acylethanolamide derivatives and uses thereof
11547681 · 2023-01-10 · ·

The present disclosure provides certain N-Acylethanolamide derivatives, and uses relating thereto.

GLP-1 derivatives and uses thereof
11572398 · 2023-02-07 · ·

The invention relates to a derivative of a GLP-1 analogue of a general Formula I, which derivative comprises a side chain attached to a Lys residue at position 34, 35, 36, 37, or 38 of the GLP-1 analogue, which side chain comprises a Branched linker, a 1.sup.st and a 2.sup.nd Protractor selected from C18 diacid, C20 diacid, and sulfonic acid C16, and at least one Linker element-1 incorporating ethylene glycol units. Linker element-1 may be incorporated in an optional Pre-linker, and/or in a 1.sup.st or 2.sup.nd Post-linker. The invention also relates to novel GLP-1 analogues, novel side chain intermediate products and their manufacture and use to prepare derivatives of biologically active peptides and proteins, as well as pharmaceutical compositions and medical uses of the analogues and derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.

Compositions of microbiota and methods related thereto

Methods and compositions are provided for treating weight related conditions and metabolic disorders by altering microbiota in a subject. One aspect provides methods and compositions to alter microbiota in a subject by administering to the subject a composition that includes a substantially purified microbiota from phyla such as Bacteroidetes, Proteobacteria, Firmicutes and Verrucomicrobia or orders such as Bacteroidales, Verrucomicrobiales, Clostridiales and Enterobacteriales or genera such as Alistipes, Clostridium, Escherichia, and Akkermansia. Another aspect includes a pharmaceutical composition for altering microbiota that includes a therapeutically effective amount of substantially purified microbiota and a pharmaceutically acceptable carrier. Yet another aspect includes methods for treating a disorder, such as obesity, in a subject in need of such treatment by changing relative abundance of microbiota in a gastrointestinal tract of the subject without or in addition to a surgical procedure.

Acid addition salts of piperazine derivatives

The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and, in particular, as glycosidase inhibitors.

Therapeutic use of a Fraximus augustifolia extract

The present invention relates to extracts from Fraxinus angustifolia samara, processes for providing such extracts, and methods and uses of the extracts obtained. In particular, the present invention relates to the use of such extracts in reversing obesity-related and/or metabolic syndrome-related gut microbiota dysbiosis treatment, treating or preventing hepatic steatosis, non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH), and modulating and/or adjusting gut microbiota.