# US 2019/0167675 A1 · Methods and compositions for appetite control and weight management > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2019/0167675 A1 - Document ID: US20190167675A1 - Status: Published application - Kind: A1 - Application number: 16/323,455 - Filed: 2016-08-09 - Published: 2019-06-06 - Earliest claimed: 2016-08-09 - Assignees: Shanghai Yao Yuan Biotechnology Co., Ltd. - Applicants: Shanghai Yao Yuan Biotechnology Co., Ltd. - Inventors: Jieqing FAN; Yan LIU; Cong XU - Web page: https://patentgrep.com/patent/US20190167675A1 ## CPC - A61K 31/4965: Non-condensed pyrazines - A61K 31/519: ortho- or peri-condensed with heterocyclic rings - A61P 3/04: Anorexiants; Antiobesity agents - G01N 33/6872: {Intracellular protein regulatory factors and their receptors, e.g. including ion channels} - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q) ## Abstract The present invention provides methods and compositions for modulation of appetite, or for treatment of an appetite disorder or a metabolic disorder such as obesity or overweight, comprising a DEG/ENaC receptor modulator. The present invention also provides methods for identifying an agent for appetite modulation and/or weight management. ## Claims ### Claim 1 (canceled) ### Claim 2 A method of regulating appetite, or treating or preventing an appetite disorder or a metabolic disorder, in a subject, comprising administering to the subject a therapeutically effective amount of a modulator capable of modulating the activity of a DEG/ENaC receptor. ### Claim 3 (depends on 2) The method according to claim 2, wherein the DEG/ENaC receptor is amiloride-sensitive. ### Claim 4 (canceled) ### Claim 5 (canceled) ### Claim 6 (depends on 2) The method according to claim 2, wherein the modulator is an inhibitor, and the appetite is suppressed to induce a reduced food intake and/or loss of body weight. ### Claim 7 (depends on 6) The method according to claim 6, wherein the modulator induces fat loss in the subject. ### Claim 8 (depends on 2) The method according to claim 2, wherein the modulator is an activator, and the appetite is stimulated to induce an increase in food intake and/or gain of body weight. ### Claim 9 (depends on 2) The method according to claim 2, wherein the modulator is administrated before or during food consumption. ### Claim 10 (depends on 2) The method according to claim 2, wherein the modulator interacts with a DEG/ENaC receptor in gastrointestinal tract. ### Claim 11 (depends on 6) The method according to claim 6, wherein the modulator comprises an inhibitor capable of inhibiting both an ENaC channel and an ASIC channel. ### Claim 12 (depends on 6) The method according to claim 6, wherein the modulator comprises amiloride or amiloride analog, or a compound of the following structural formula where X is halogen, R1-R8 is selected independently from H, alkyl having 1-12 carbons, arylalkyl having 7-13 carbons, aryl, or heteroaryl, wherein the alkyl portion of each alkyl or arylalkyl substituent is optionally and independently further substituted one or more times by halogen, hydroxy, alkoxy having 1-6 carbons, aryl, heteroaryl, amino, alkylamino having 1-6 carbons, dialkylaminio having 2-12 carbons, carboxylic acid, or an ester formally derived from carboxylic acid and an alcohol having 1-6 carbons, and wherein the aromatic portion of each aryl, arylalkyl, or heteroaryl substituent is optionally and independently further substituted one or more times by halogen, alkyl having 1-6 carbons, amino, alkylamino having 1-6 carbons, dialkylamino having 2-12 carbons, carboxylic acid, or an ester formally derived from carboxylic acid and an alcohol having 1-6 carbons. ### Claim 13 (depends on 12) The method according to claim 12, wherein the modulator is a compound of the following structural formula wherein R1, R2, R7 and R8 are independently H, alkyl having 1-6 carbons, or arylalkyl having 7-13 carbons. ### Claim 14 (depends on 6) The method according to claim 6, wherein the modulator comprises amiloride analog, selected from the group consisting of benzamil, phenamil, EIPA, bepridil, KB-R7943, 5-(N-methyl-N-isobutyl)-amiloride, 5-(N,N-hexamethylene)-amiloride, 5-(N,N-dimenthyl)amiloride hydrochloride, P552-02 and NVP-QBE170. ### Claim 15 (depends on 12) The method according to claim 12, wherein the modulator is administered in an amount of about 0.01-3 mg/kg body weight/day. ### Claim 16 (depends on 6) The method according to claim 6, wherein the DEG/ENac inhibitor comprises at least one selected from the groups consisting of Triamterene, A317567, A317567 analogs, P301, P365, GS-9411/P680, Aromatic diamidines, and any analog or derivative thereof, and any combination. ### Claim 17 (depends on 8) The method according to claim 8, wherein the DEG/ENac activator is selected from the groups consisting of compound S3969, N,N,N-trimethyl-2-((4-methyl-2-((4-methyl-1H-indol-3-yl)thio)pentanoyl)oxy)ethanaminium iodide and N-(2-hydroxyethyl)-4-methyl-2-((4-methyl-1H-indol-3-yl)thio) pentanamide, GMQ, AP301, and any analog or derivative thereof, and any combination. ### Claim 18 (depends on 2) The method according to claim 2, wherein the modulator comprises an ASIC-targeting modulator. ### Claim 19 (depends on 2) The method according to claim 2, wherein the DEG/ENac modulator modulates the level of expression or activity in gastrointestinal tract of a DEG/ENaC receptor. ### Claim 20 (depends on 19) The method according to claim 19, wherein the modulation is a decrease in the level of expression or activity, and the modulator is selected from the group consisting of catalytic and inhibitory oligonucleotide molecules targeted against the gene(s) encoding a DEG/ENaC receptor, and inhibitors of DEG/ENaC receptor transcription or translation. ### Claim 21 (canceled) ### Claim 22 A method for identifying an agent for appetite modulation and/or weight management, said method comprising the steps of: providing an assay to determine modulation of expression or activity of an DEG/ENaC receptor; introducing to said assay a compound suspected of being an DEG/ENaC modulator; and determining whether DEG/ENaC modulation occurs, wherein the agent that modulates the level of expression or activity of the DEG/ENaC ion channel is a candidate for modulation of appetite or management of weight. ### Claim 23 (depends on 22) A method according to claim 22, said method comprising the steps of: (i) contacting said agent with a DEG/ENaC receptor, and (ii) detecting any change in the activity of said DEG/ENaC receptor. ### Claim 24 (canceled) ### Claim 25 A pharmaceutical composition for modulation of appetite, or for treatment of an appetite disorder or a metabolic disorder, comprising: a DEG/ENaC receptor modulator and a pharmaceutically acceptable carrier.