A61P13/02

N-PYRIDINYL ACETAMIDE DERIVATIVES AS WNT SIGNALLING PATHWAY INHIBITORS

Disclosed are compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition, the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example, in treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment.

Soluble C5aR antagonists

Compounds are provided to modulate the C5a receptor. The compounds have the following Formula (I): ##STR00001## including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2 and R.sup.3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Use of angiogenin or angiogenin agonists for treating diseases and disorders

The invention provides a method of treating a disorder characterized by elevated or dysregulated myostatin, disorders where the interaction between follistatin and angiogenin can be used to improve function in tissues, neurological diseases or disorders, spinal injuries or diseases, bone diseases or disorders, diseases involving glucose homeostasis, wound healing, neuroprotection, nervous system functional support or managing metabolic diseases, the method comprising administering an effective amount of angiogenin or an angiogenin agonist. Compositions and neutraceuticals comprising angiogenin are also provided.

Biologically active macrolides, compositions, and uses thereof

The present invention provides a compound of the formula (I) or (II), wherein R.sup.1 is H, alkyl, alkenyl or aryl, R.sup.2 is H, alkyl or aryl, R.sup.3 is H, a alkyl, alkenyl or aryl, R.sup.4 and R.sup.4-R.sup.8 are independently R.sup.10, C(O)R.sup.10 or SO.sub.2R.sup.10, wherein R.sup.10 is H, alkyl, alkenyl or aryl, and R.sup.9 is R.sup.9a, C(O)R.sup.9a or SO.sub.2R.sup.9a, wherein R.sup.9a is H, alkyl, alkenyl or aryl. R.sup.9a can be unsubstituted or substituted with one or more oxo(═O), OR.sup.9b, OC(O)R.sup.9b, OSO.sub.2R.sup.9b, NHR.sup.9b, NHC(O)R.sup.9b and NHSO.sub.2R.sup.9b groups. R.sup.9b is H, alkyl, alkenyl, or aryl. R.sup.9b can be unsubstituted or substituted with one or more groups such as oxo(═O), OR.sup.9c, CO.sub.2R.sup.9c, CO.sub.2R.sup.9c and OC(O)R.sup.9c. R.sup.9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer. ##STR00001##

Bicyclic acetyl-CoA carboxylase inhibitors and uses thereof

The present invention provides compounds of formula (IV); ##STR00001##
or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (IV), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.

Crystallized oxalate decarboxylase and methods of use

Oxalate decarboxylase crystals, including stabilized crystals, such as cross-linked crystals of oxalate decarboxylase, are disclosed. Methods to treat a disorder associated with elevated oxalate concentration using oxalate decarboxylase crystals are also disclosed. Additionally disclosed are methods of producing protein crystals.

Microrna compounds and methods for modulating MIR-21 activity
09790496 · 2017-10-17 · ·

Described herein are compositions and methods for the inhibition of miR-21 activity. The compositions have certain nucleoside modification patterns that yield potent inhibitors of miR-21 activity. The compositions may be used to inhibit miR-21, and also to treat diseases associated with abnormal expression of miR-21, such as fibrosis and cancer.

Steroid derivative FXR agonist

The present invention relates to a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt thereof, and relates to applications thereof in the preparation of drugs for treating FXR related diseases. ##STR00001##

Heteroaryl compounds as IRAK inhibitors and uses thereof

The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.

2-AMINOTHIAZOLE DERIVATIVE OR SALT THEREOF

A compound which is useful as an active ingredient for a pharmaceutical composition for treating urine storage dysfunction, voiding dysfunction, lower urinary tract dysfunction, and the like. The present inventors have found that a 2-aminothiazole derivative has an excellent muscarinic M.sub.3 receptor-positive allosteric modulator activity and is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic M.sub.3 receptor, thereby completing the present invention. 2-aminothiazole derivative or a salt thereof of the present invention is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic M.sub.3 receptor, for example voiding dysfunction such as underactive bladder.