(WO2020163612) Formulations of cannabidiol derivatives and their use as modulators of cannabinoid receptor type 2 (cb2) 机翻标题: 暂无翻译,请尝试点击翻译按钮。

源语言标题
(WO2020163612) Formulations of cannabidiol derivatives and their use as modulators of cannabinoid receptor type 2 (cb2)
公开号/公开日
WO2020/163612 / 2020-08-13
申请号/申请日
WOUS2020/017035 / 2020-02-06
发明人
ROLLAND ALAINBLANCO EDUARDO MUNOZ;
申请人
EMERALD HEALTH PHARMACEUTICALS;
主分类号
IPC分类号
A61K-031/133 C07C-225/28
摘要
(WO2020/163612) Compositions, comprising the cannabidiol derivatives of Formula (I) in pharmaceutical formulations displaying increased bioavailability and solubility are described. Cannabidiol derivatives of Formula (I) and compositions comprising the same for use in the treatment of various conditions, and diseases, including diseases associated with demyelination.
机翻摘要
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地址
代理人
(WO2020163612) NGUYEN, Quang D. et al. ([US])
代理机构
;
优先权号
2019US-62801756 2019US-62870546
主权利要求
(WO2020/163612)  CLAMS e claim: 1. A composition comprising at least one compound of Formula (11, or a derivative thereof.  wherein R is the nitrogen atom of a group independently selected from a linear or branched alkyiamkie, an aryl amine* an arylalkylaraiiie, a heteroaryla ine, a   hetemarylalkylam e, a linear or branche aikers iamihe, a, linear or branched aJkynyiamine, or NIL,   solithiiiaed in a pharmaceutical vehicle,   wherein the pharmaceutical vehicle is selected from the group consisting of aqueous boilers, solvents co-solvents, ig/dodextrin complexes, lipid vehicles, and any combination thereof 2. The composition of claim. 1 , wherein the composition is a liquid formulation. 3. The composition of claim I, wherein the composition is a suspension formulation,  4 The composition of claim 3, wherein the formulation Is a naoostispension formulation. 5. The composition of claim 1, wherein the composition i an emulsion formdlatl ,  6 The composition of claim L wherein the composition is a dry powder formalaii7 Tiie composition of claim 5, wherein fee powd r k compressed intis a tablet  S. Tiie composition of claim I , where in the composition k: a solution, a g , a lotion, a paste, a» ointment, as emoBieaf, a liposome, a nanosphere, a skin tonic, a month wash* an ora! rinse, a mousse, spray, a pack, a capsule* a granule, a patch, aft occlusive skin agent, or an   combination thereof  0. The composition of claim 1 * wherein said compound of Formula (I) is selected from the group consisting of;     (11%   9!     cm      10. The composition of clai m 1 , wherein the pharmaceutical vehicle is selected fr m the group consisting of aqueous buffers, solvents, ccksolveats, cyclodextrin complexes, lipid vehicles, and any combination thereof, and further comprising at least on stabilker, emulsifier, polymer, and any combinatio thereof  1 L The composition of claim 10, wherein the aqueous buffer is selected from the group consisting of aqueous HCI, aqueous citrate-lid buffer, aqueous NaOfl aqueous citrate-MaOH buffer, aqueous phosphate buffer, aqueous KCl aqueous horafe-KCbHaOH buffer, PBS buffer, and any combination ihereof  1.2. The composition of claim 10, wherein the solvent is selected from the group consisting of acetone, ethyl acetate acetonitrile, pentane, hexane, heptane, methanol, ethanol, isopropyl alcohol, dimethyl sulfoxide (DMSO), water, chloroform, dichloromethane, diethyl ether, PEG400, Transeutoi (diethy!ene glyeomonoethyl ether), MCT 70, Labrasol (PEG-8   eaprylie/eaprie glycerides), Labrafil M1 44CS (PEG 5 Oleate), propylene glycol, Transeutoi P, PEC1400, propylene glycol, glycerol, Captex 300, Tween 85, Cremophor EL, Malsine 35-1, atsiue CC, Caproul M€M, mafee oil, and any combination thereof.  13 The composition of claim 10, wherein the co-sol vent is selected from the group consisting of acetone, ethyl acetate, acetonitrile, pentane, hexane, heptane, methanol, ethanol, isopropyl alcohol, dimethyl sulfoxide (DMSO), water, chloroform, d ehlofomefhane, diethyl ether, PEG400, Transeutoi (diethyiene glyeornoiioethyl ether), MCT 70, Eabrasol (PEG-8 eapryiic/capric glycerides), Labrafil M1944CS (PEG 5 Oleate), propy lene glycol, Tfansc tiol P,FEG40O, propyleae glycol, glycerol, Capex 300, Tween 05, C mqpbor EL, Maisiac 354, arin €€, Capmul MCM, make ail, and any combination thereof,  14, The composition of claim 10, wherein the cyeiodextrin complexes is selected Drops the group consisting of raethyElEcyelodexirin, etl yfy-cyelodextriti, HP^p-cydodexirin, HR-g- cyclodextrin., SBE-p-eycJodexirin, a-cydodextfin, ymYeladextrin,6-0-glueosyEpmycIodex.trin, and any combination thereof  15, The composition of claim 10, wherein the stabilizer is selected from the group consisting of Pharmaeo&t 603, SLS, Nisso BPC-SSL, Koliiphor, PVF K.30, PVF VA 64, and any combination thereof  36, The composition of claim 1 , wherein the polymer is selected from the group consisting of HFMG-AS-MG, MPMC-AS4X , HFMC-AS4KT MPMC, I1PMC-P-55S, BPMC-P-SO, methyl eellalose, BEG, HPC, Hudragn L I 00. End git E100, PEG i.OOM, PEG 6000, PVF VA64, PVF KBQ, TPGS, Kollieoat IR, Carbopol 980MF, Povocoat MP, Soluplos, Snreteric, Flnronic F~ 68  17. The composition of claim 10» wherein live antioxidant is selected from th group consisting of Vitamin A, Vitamin C* Vitamin £, Cocnxyine 016, manganese,, iodide, melatonin;, alphu-caroteixe, astaxanth i, beta-carotene, eantbaxanthlih etyptmianthM, lutein, lycopene, zeaxanthm, polyphenol antioxidant, flavonokl, ilav-ones, apigenin, lateoiin, laagerU , flavonoi, isotha etin, koempferoi, mytieetin, pfronndxocyanidit, quercetin, .flavanone, erio ktyol, hesperetm, isa ge », f!avasol, eatechio, gailocaisehln, gaUatfc esters, epicafe t ,   epigaliocatechin, theaflavln, thearuMgin, isof!avbne pliytoestrogen, daidzein, ge stein, glycitein, stilbeaoid, resveratrol, pterostilbene, anthoeyanin, cyani ih, delph idin, aividtu, pelargomdin,. peonidm, peinnidm, chicoric acid, cafXeic acid, chlorogenie acid, ferutic acid, cinnamic acid, ellagie acid, ellagitannin, gallic acid, gailotannio, rosniarlnic acid, salicylic acid, cureamin, ilavonolignan, sMymarin, xant ones, eiigenoL capsaicin, iiimbin, citric acid, oxalic acid, phytic acid, n-acety!cysidae, R«aipha Hpotc acid, and any combination thereof  18. Tlie composition of claim !¾ wherein the lipid vehicle is selecte fiiam the group eonsisiing of Ca iex 300, Tween 85, Cremophor EL, Maisine 35-1, Maisine CC, Caprnnl M€M,com oil anti any combination thereof.  19. The composition of clai 10, wherein the lipid vehicle is an oil,  20. The compositio of claim 10, wherein the lipid vehicle is an oil mixture comprising at least two oils.  21: , The competition of claim 20, wherein the oil mixtur Is a mixture of Mu me CC and name oil  22. The composition of claim 21 , wherein the mixture of Mai sins CC and maize oil comprises 50 Maisine CC: 50 maize oil v/v.  23. The formulation of claim 2, wherein the pharmaceutical vehicle is an oil.  24. The formulation of claim 2, wherein the pharmaceutical vehicle is an oil mixture.  25. The formulation of claim 24, wherein the oil mixture is a mixture of Maisine€€ and roalze oil,  26. The fermnlaiioa of claim 25, wherein the mixture of Maisine CC and maize oil comprises 50 Maisine CC: 50 maize oil v/v.  27. A method of treating a condition or disease responsive to the modulation of the  Cannabinoid Receptor Type 2 (CBs) activity in a subject in need thereof, wherein the method comprises administering to the subject a therapeutically effective amount of the compound of Formula (I), or a formulation thereof to a subject iu need thereof or a derivative thereof  wherein R is tlie nitrogen atom of a group independently selected femi a linear or branched alkylamme, an arylamine, an aryialkykniine, a heteroaryiamme, a   heteroaryia!fcyktnine, a linear o branched aSfcenybaoh a linear or branched alkynylannne, or Nila  28 The method of claim 27, wherein sai d compound of Formula (1) or a formulation thereof is independently selected from the group consisting oh  mu      2 The method of claim 27, wherein said compound of Formula (I) selectively binds the-  Camtabmoid Receptor Type 2 (CBif  30- The method of claim 27» herein II binds: the Carmabmold Receptor Type 2 iCBef  3 ! The method of claim 27, wherein the condition or disease responsive to the modulation of the Camtahinoid Receptor Type 2 (CBa) activity is selected from the group consisting of autoimmune disease, demye!mating disease, Inflammatory-related disorder, and any combination thereof  32. The method of claim 27, wherein the condition or disease responsive to the modulation of the Catmabinoi Receptor Type 2 (C¾) acti vity Is selected from the group consisting of systemic sclerosis, myehnoci lic disorder, multiple sclerosis, neuromyelitis optica, central nervous system neuropathy, central pontine myel olysis, myelopathy, leukoericephalopaihy, leukodystrophy, peripheral neuropathy, Guiilaln-Barre syndrome, anti-MAG peripheral neuropathy, Charcoi-Marie-Tooih disease, progressive inflammatory neuropathy, and any combination thereof  33. The method of claim 27, wherein the condition or disease responsive to the modulation of the Canoahmok! Receptor Type 2 (CBa) acti vity Is multiple sclerosis,  34. The method of claim 27, wherein said compound of Formula (I) or a formulation thereof is admin stered orally.  35. Tile method of claim 2% Wherein i compound of Formula {1} or a formulation thereof is administered topically  36. The method of claim 27, wherein said compound of Formula (I) or a. formulation thereof is administered via intramuscular injection,  37 The method of claim 27, wherein said compound of Formula (I) or a formulation thereof is administered via intravenous infection,  38. The method of claim 27, wherein said compound of formula (I) or a formulation thereof is administered with food or drink.  39. The method of claim 27, wherein said compound of formula (I) or a formulation thereof is administered in combination with another therapeutic agent,  40. A liqui d formulation, comprisin g compound of Formula (VIII). or a derivative thereof, solubilized in a pharmaceutical vehicle, wherein the plmonaeeutical vehicle is 50 ; 50 v/v Maisine CG ; maiae oil mixture.    41. A method of treating a m ultiple sclerosis or systemic sclerosis responsive to the modulation of the CBz receptor activity in a subj ect In need thereof wherein the methodcomprises administering to the Subject a thenipentieally effecti ve amount of the compound of Formula (YJ1I) or a formulation thereof or a derivative thereof     (V!U),  42. A method of treating a condition or disease associated with deffiyel atkm in a subject in need thereof wherein the method comprises administering to the subject a therapeutically effective amount of the compound of Formula (I), or a formulation thereof to a subject i need thereof or a derivative thereof  wherein R is the nitrogen atom of a group independently selected from a linear or branched a!k ia ine, as aryl amine, an arylalky!amine., a heteroaryiamjnm a   heteroarylafkyiamine, a linear or branched alkei¾¾rmnes a linear or branched alfeyuylamine, orN¾  43 , The method of claim 4% wherein said compound of Formula (I) or a formulation drereof is independently selected from the group consisting of      44. lie method of elate 42, wherein die subject: farthe lias a condition or disease responsive to the nioduiadm of the Camiabinold Receptor Type 2 (CBt) activity,45, The ethod of ata 42, wherein the condition or disease associated with demyelination is selected from the group consisting of an inmione disease, demyetaatin disease, inSam atory^rekited disorder, and any doarbiiiatios ther of  46 The method of ata 42, where!» the condition or disease associated with demyelination i selected from the group eo dstmg of systemic sclerosis, myelinoeiastic disorder, multiple sclerosis, nenremyefltis optica, central nervoos system neuropathy, central pontine myelinolysis, myelopathy, leokoencephalopathy , leukodystrophy, peripheral neuropathy , Gulf lam-Barre syndrome, anti-MAG peripheral neuropathy, Charcot- Marie -Tooth disease, progressive inflammatory neuropathy, and any combination thereof  47 The method of clai 42 , wherein the condition or disease associated with demyelination is multiple sclerosis.  48 A method of fe-Tayeiinatlon in a subject in need thereof wherein the method comprises administering to the sul¾eet a iherapeutically effective amount of the compound of Formula (I), or a formulation thereof to a subject in need thereof or a derivative thereof  wherein is the nitrogen atom of a group independently selected fh i a linear or ranched aikylamlne, an aryl amine, an twylaikylantae, a heteroarylamme, a   hetemaryialfcylaotae, a linear or branched alkenylamine, a linear or branched alkyuyiaurine, or fc.  3. The method of claim 48, where!» said cosipouftd ef Fomiute (I) or a Ibrsmtlatio» thereof !r epe«de»iiy selected .¾¾«·» the group e-oissist g of:      50. T le method of claim 48, wteeia the subect lias a condition or disease selected tom die group consisting of a condition or disease respon ive io d e modulation of die Carmahinokl Receptor Type 2 (CBe) activity, a conditio» or disease associated wibi demyelinatlon, and any combination thereof.51 The method of c laim 48, wherein the subject has a conditio or disease selected from the group consisting of autoimoiuae disease, demyelinating disease, inflarnmaiory-reiated disorder, and any combination thereof  52. The method of claim 48, wherein the subject has a condition or disease selected from the group consisting of systemic sclerosis, myeHnoelastic disorder, ronitlp!e sclerosis, neuro yeiids o ttea, central nervous system neuropathy, central pontine myebnolysls, myelopathy, leukoencepl iopathy, leukodystrophy, peripheral neuropathy, GubialmBarre syndrome, ants- MAG peripheral neuropathy, Charcot-Marie-T oth disease, progressive inflammatory neuropathy, and any combination thereof  S3 , The method of claim 48, wherein the subject has multiple sclerosis.  ! 10
法律状态
PENDING
专利类型码
A1
国别省市代码
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