Nebulizer formulations of dehydroepiandrosterone and methods of treating asthma or chronic obstructive pulmonary disease using compositions thereof
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/56
A61K-031/566
A61K-031/568
A61K-031/5685
C07J-069/00
출원번호
US-0462901
(2003-06-17)
등록번호
US-7405207
(2008-07-29)
발명자
/ 주소
Leonard,Sherry A.
Johnson,Keith A.
출원인 / 주소
Epigenesis Pharmaceuticals, Inc.
대리인 / 주소
Halluin,Albert P.
인용정보
피인용 횟수 :
4인용 특허 :
38
초록▼
This invention relates to a sealed container containing a powder formulation comprising a dehydroepiandrosterone, its analogue(s) or salt(s) by itself or with a pharmaceutically or veterinarily acceptable carrier or diluent, and having a particle size of about 0.1 μm to about 100 μm. The f
This invention relates to a sealed container containing a powder formulation comprising a dehydroepiandrosterone, its analogue(s) or salt(s) by itself or with a pharmaceutically or veterinarily acceptable carrier or diluent, and having a particle size of about 0.1 μm to about 100 μm. The formulation can be used to treat or prevent asthma, chronic obstructive pulmonary disease, lung inflammation, and other respiratory diseases or conditions. The formulation may be prepared by jet milling, and may be delivered through the respiratory tract or other routes using a nebulizer. The sealed container is provided in a device and/or a therapeutic kit.
대표청구항▼
What is claimed is: 1. A pharmaceutical composition comprising an agent, wherein the agent comprises a compound as described by chemical formula (I), (II), (III), (IV) or (V), or a pharmaceutically or veterinarily acceptable salt thereof, in an anhydrous form thereof; wherein the broken line repr
What is claimed is: 1. A pharmaceutical composition comprising an agent, wherein the agent comprises a compound as described by chemical formula (I), (II), (III), (IV) or (V), or a pharmaceutically or veterinarily acceptable salt thereof, in an anhydrous form thereof; wherein the broken line represents a single or a double bond; wherein R is hydrogen or a halogen; the H at position 5 is present in the alpha or beta configuration or the compound of formula (I) comprises either isomer or a racemic mixture of both configurations; and R1 is hydrogen or a multivalent inorganic or organic dicarboxylate acid covalent bound to the compound of chemical formula (I); wherein R1, R2, R3, R4, R6, R7, R8, R9, R10, R11, R12, R13, R14 and R19 are independently H, OH, halogen, C1-10 alkyl or C1-10 alkoxy; R5 is H, OH, halogen, C1-10 alkyl, C1-10 alkoxy or OSO2R20; R15 is (1) H, halogen, C1-10 alkyl or C1-10 alkoxy when R16 is C(O)OR21 or (2) H, halogen, OH or C1-10 alkyl when R16 is H, halogen, OH or C1-10 alkyl or (3) H, halogen, C1-10 alkyl, C1-10 alkenyl, C1-10 alkynyl, formyl, C1-10 alkanoyl or epoxy when R16 is OH; or R15 and R16 taken together are ═O; R17 and R18 are independently (1) H, OH, halogen, C1-10 alkyl or C1-10 alkoxy when R16 is H, OH, halogen, C1-10 alkyl or--C(O)OR21 or (2) H, (C1-10 alkyl)n amino, (C1-10 alkyl)n amino-C1-10 alkyl, C1-10 alkoxy, hydroxy-C1-10 alkyl, C1-10 alkoxy-C1-10 alkyl, (halogen)m-C1-10 alkyl, C1-10 alkanoyl, formyl, C1-10 carbalkoxy or C1-10 alkanoyloxy when R15 and R16 taken together are ═O; or R17 and R18 taken together are ═O or taken together with the carbon to which they are attached form a 3-6 member ring containing 0 or 1 oxygen atoms; or R15 and R17 taken together with the carbons to which they are attached form an epoxide ring; [R20 is OH, pharmaceutically acceptable ester or pharmaceutically acceptable ether; R21 is H, (halogen)m -C1-10 alkyl or C1-10 alkyl]; n is 0, 1 or 2; and m is 1, 2 or 3, with the proviso that (a) R3 is not H, OH or halogen when R1, R2, R4, R6, R7, R9, R10, R12, R13, R14, R17 and R19 are H and R5 is OH or C1-10 alkoxy and R8 is H, OH or halogen and R11 is H or OH and R18 is H, halogen or methyl and R15 is H and R16 is OH; (b) R3 is not H, OH or halogen when R1, R2, R4, R6, R7, R9, R10, R12, R13, and R14 [and R19 ] are H and R5 is OH or C1-10 alkoxy and R8 is H, OH or halogen and R11 is H or OH and R18 is H, halogen or methyl and R15 and R16 taken together are ═O; (c) R5 is not H, halogen, C1-10 alkoxy or OSO2R20 when R1, R2, R3, R4, R6, R7, R8, R9, R10, R12, R13, R14 and R17 are H and R11 is H, halogen, OH or C1-10 alkoxy and R18 is H or halogen and R15 and R16 taken together are ═O; and (d) R5 is not H, halogen, C1-10 alkoxy or OSO2R20 when R1, R2, R3, R4, R6, R7, R8, R9, R10, R12, R13, R14 and R17 are H and R11 is H, halogen, OH or C1-10 alkoxy and R18 is H or halogen and R15 is H and R16 is H, OH or halogen; wherein R is A--CH(OH)--C(O)--and A is hydrogen or a C1-C22 alkyl or alkenyl group wherein the C1-C22 alkyl or alkenyl group is not subsitutued or substituted with one or more C1-C4 alkyl groups, phenyls, halogens or hydroxyl groups, said phenyl is not substituted or substituted with one or more halogen HO or CH3O; wherein said dry powder pharmaceutical composition is particles of respirable or inhalable size. 2. The pharmaceutical composition of claim 1, wherein the multivalent inorganic acid is SO2OM, phosphate or carbonate, wherein M is selected from the group consisting of H, Na, sulphatide, and phosphatide wherein R2 and R3, which may be the same or different, are straight or branched (C1-C14) alkyl or glucuronide wherein the multivalent organic dicarboxylic acid is succinate, maleate, or fumarate. 3. The pharmaceutical composition of claim 1, wherein powder pharmaceutical composition further comprises a pharmaceutically or veterinarily acceptable excipient. 4. The pharmaceutical composition of claim 3, wherein said excipient is one selected from human protein, bovine serum albumin, gelatin, immunoglobulins, galactose, D-mannose, sorbose, trehalose, sucrose, cyclodextrins, raffinose, maltodextrins, dextrans, monosodium glutamate, glycine, alanine, arginine or histidine, tryptophan, tyrosine, leucine, phenylalanine, betaine, magnesium sulfate, magnesium stearate, glycerin, erythritol, glycerol, arabitol, xylitol, sorbitol, mannitol, propylene glycbl, polyethylene glycol, pluronics, surfactants, and a mixture thereof. 5. The pharmaceutical composition of claim 1, wherein the agent comprises a compound as described by chemical formula (II): 6. The pharmaceutical composition of claim 1, wherein said powder pharmaceutical composition is deliverable using a nebulizer, a dry powder inhaler, an insufflator, or an aerosol or spray generator. 7. The pharmaceutical composition of claim 1, wherein said powder pharmaceutical composition is produced by jet-milling. 8. The pharmaceutical composition of claim 1, wherein greater than 80% of the particles are about 0.1 μm to about 100 μm in diameter. 9. The pharmaceutical composition of claim 8, wherein greater than 80% of the particles are about 0.1 μm to about 50 μm. 10. The pharmaceutical composition of claim 9, wherein greater than 80% of the particles are about 0.1 μm to about 10 μm. 11. The pharmaceutical composition of claim 10, wherein greater than 90% of the particles are about 0.1 μm to about 5 μm. 12. The pharmaceutical composition of claim 1, further comprising a therapeutic agent selected from inhibitors of the adenosine A1 receptor, inhibitors of the adenosine A2b receptor, inhibitors of the adenosine A3 receptor, adenosine A2a receptor stimulating agents, anti-inflammatory agents, anti-bacterial agents, anti-sepsis agents, kidney activity maintenance or restoration agents, and agents for treatment of pulmonary vasoconstriction, inflammation, allergies, asthma, impeded respiration, respiratory distress syndrome, pain, cystic fibrosis (CF), pulmonary hypertension, pulmonary vasoconstriction, emphysema, chronic obstructive pulmonary disease (COPD), allergic rhinitis (AR), SARS, and lung cancer. 13. A sealed container comprising the composition of claim 1, wherein said sealed container is vacuum sealed. 14. A kit comprising the sealed container of claim 13 and a second sealed container containing a pharmaceutically acceptable propellant for the pharmaceutical composition. 15. The kit of claim 14, further comprising a nebulizer. 16. A method for treatment of asthma, comprising administering to a subject in need of such treatment a therapeutically effective amount of the powder pharmaceutical composition from the sealed container of claim 13. 17. A method for treatment of chronic obstructive pulmonary disease, comprising administering to a subject in need of such treatment a therapeutically effective amount of the powder pharmaceutical composition from the sealed container of claim 13. 18. A method of reducing or depleting adenosine in a subject's tissue, comprising administering to a subject in need of such treatment a therapeutically effective amount of the powder pharmaceutical composition from the sealed container of claim 13 to reduce or deplete adenosine levels in the subject's tissue. 19. The method of claim 18, wherein subject suffers from airway inflammation, allergy, asthma, impeded respiration, cystic fibrosis, Chronic Obstructive Pulmonary Diseases, allergic rhinitis, Acute Respiratory Distress Syndrome, microbial infection, SARS, pulmonary hypertension, lung inflammation, bronchitis, airway obstruction, or bronchoconstriction. 20. A method for treatment of a disorder or condition associated with high levels of, or sensitivity to, adenosine in a subject's tissue, comprising administering to a subject in need of such treatment a therapeutically effective amount of the powder pharmaceutical composition from the sealed container of claim 1 to reduce adenosine levels in the subject's tissue and prevent or treat the disorder. 21. The method of claim 20, wherein the disorder or condition is airway inflammation, allergy, asthma, impeded respiration, cystic fibrosis, Chronic Obstructive Pulmonary Diseases, allergic rhinitis, Acute Respiratory Distress Syndrome, microbial infection, SARS, pulmonary hypertension, lung inflammation, bronchitis, airway obstruction, or bronchoconstriction.
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