Salts of potassium ATP channel openers and uses thereof
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/549
C07D-085/22
C07D-085/00
출원번호
UP-0391990
(2009-02-24)
등록번호
US-7572789
(2009-08-25)
발명자
/ 주소
Cowen, Neil M.
Kashkin, Kenneth B.
Yamout, Khaled A.
출원인 / 주소
Essentialis, Inc.
대리인 / 주소
Foley & Lardner LLP
인용정보
피인용 횟수 :
31인용 특허 :
23
초록▼
Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP cha
Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.
대표청구항▼
That which is claimed is: 1. A salt comprising: a KATP channel opener selected from the group consisting of Formula III and Formula IV, and a counter ion as shown below wherein: R1 is selected from the group consisting of hydrogen, lower alkyl, substituted lower alkyl, and cycloalkyl provided ho
That which is claimed is: 1. A salt comprising: a KATP channel opener selected from the group consisting of Formula III and Formula IV, and a counter ion as shown below wherein: R1 is selected from the group consisting of hydrogen, lower alkyl, substituted lower alkyl, and cycloalkyl provided however that when R1 is a substituted lower alkyl, then the substituent does not include an amino group; R2a is hydrogen; R2b is hydrogen; R3 is selected from the group consisting of hydrogen, halogen, lower alkyl, substituted lower alkyl, cycloalkyl and substituted cycloalkyl provided however that when R3 is a substituted lower alkyl, then the substituent does not include an amino group; R4 is selected from the group consisting of hydrogen, halogen, lower alkyl, substituted lower alkyl, cycloalkyl and substituted cycloalkyl provided however that when R4 is a substituted lower alkyl, then the substituent does not include an amino group. 2. The salt according to claim 1 wherein said KATP channel opener is diazoxide. 3. The salt according to claim 1 wherein said KATP channel opener is diazoxide and said counter ion is choline. 4. The salt according to claim 1 wherein said KATP channel opener is diazoxide and said counter ion is hexamethyl hexamethylene diammonium. 5. A pharmaceutical formulation comprising the salt of claim 1 and at least one pharmaceutically acceptable excipient. 6. The formulation according to claim 5 wherein the pharmaceutical formulation is an oral dosage form. 7. The formulation according to claim 6 which is an enteric coated formulation. 8. The formulation according to claim 7 wherein the enteric coating is selected from the group consisting of: (a) a compression coating on a tablet, (b) a thin film on a tablet, and (c) a coating on microparticles wherein the microparticles can be further encapsulated. 9. The formulation according to claim 6 wherein the formulation is a sustained release formulation. 10. The formulation according to claim 9 wherein the period of release is 8-24 hours following administration. 11. The formulation according to claim 9 wherein the formulation comprises a component selected from the group consisting of: (a) a pH sensitive polymeric coating, (b) a hydrogel, (c) a film coating that controls the rate of diffusion of the salt from a coated matrix, (d) n erodable matrix that controls rate of salt release, (e) polymer coated pellets, granules or microparticles of salt which can be further encapsulated or compressed into a tablet, (f) an osmotic pump system containing the salt, (g) a compression coated tablet form of the salt, and (h) combinations thereof. 12. The formulation according to claim 5 for a single administration that contains between 10 and 2000 mg of the salt. 13. The formulation according to claim 5 for a single administration that contains between 300 and 500 mg of the salt. 14. The formulation according to claim 9 wherein the period of release is 2-30 hours following administration.
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