Patent classifications
C07C217/12
IONIZABLE LIPIDS FOR NUCLEIC ACID DELIVERY
The present document describes compounds, or pharmaceutically acceptable salt thereof, of a core formula (I) where R.sub.1 features an amine group, particularly useful in the formulation of lipid particles including nucleic acid therapeutic agents, or proteins, or both, and for delivery of nucleic acid and protein therapeutics to cells in vivo or ex vivo, including anticancer and vaccine applications.
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Phenalene-1-one-containing photosensitizer composition, phenalene-1-one compound and the use thereof
A phenalene-1-one compound, a photosensitizer composition including the phenalene-1-one compound, an article including the phenalene-1-one compound and/or photosensitizer composition and the use thereof.
PHENALENE-1-ONE-CONTAINING PHOTOSENSITIZER COMPOSITION, PHENALENE-1-ONE COMPOUND AND THE USE THEREOF
A phenalene-1-one compound, a photosensitizer composition including the phenalene-1-one compound, an article including the phenalene-1-one compound and/or photosensitizer composition and the use thereof.
Monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and preparation method and application thereof
The invention discloses a monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and a preparation method and application thereof. The amphiphilic hypocrellin derivative substituted by a group containing PEG, a quaternary ammonium salt or the like prepared according to the invention has an obvious red shift in its absorption spectrum and a significantly enhanced molar extinction coefficient, compared with the parent hypocrellin, can efficiently produce singlet state oxygen and other reactive oxygen species under photosensitive conditions; has different amphiphilicities and increased biocompatibility with cells or tissues by regulating its hydrophilicity and hydrophobicity; can meet the requirements of different clinical drugs, and solves the requirements of different drug delivery methods for different drug hydrophilicity and lipophilicity. Under identical conditions, the amphiphilic hypocrellin derivative photosensitizer according to the invention has higher ability to photodynamically inactivate tumor cells than the first and second generation commercial photosensitizers.
Monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and preparation method and application thereof
The invention discloses a monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and a preparation method and application thereof. The amphiphilic hypocrellin derivative substituted by a group containing PEG, a quaternary ammonium salt or the like prepared according to the invention has an obvious red shift in its absorption spectrum and a significantly enhanced molar extinction coefficient, compared with the parent hypocrellin, can efficiently produce singlet state oxygen and other reactive oxygen species under photosensitive conditions; has different amphiphilicities and increased biocompatibility with cells or tissues by regulating its hydrophilicity and hydrophobicity; can meet the requirements of different clinical drugs, and solves the requirements of different drug delivery methods for different drug hydrophilicity and lipophilicity. Under identical conditions, the amphiphilic hypocrellin derivative photosensitizer according to the invention has higher ability to photodynamically inactivate tumor cells than the first and second generation commercial photosensitizers.
PHENALENE-1-ONE-CONTAINING PHOTOSENSITIZER COMPOSITION, PHENALENE-1-ONE COMPOUND AND THE USE THEREOF
A phenalene-1-one compound, a photosensitizer composition including the phenalene-1-one compound, an article including the phenalene-1-one compound and/or photosensitizer composition and the use thereof.
Phenalene-1-one-containing photosensitizer composition, phenalene-1-one compound and the use thereof
A phenalene-1-one compound, a photosensitizer composition including the phenalene-1-one compound, an article including the phenalene-1-one compound and/or photosensitizer composition and the use thereof.
CATIONIC LIPID
The present invention provides novel cationic lipids having excellent encapsulation and delivery stability of nucleic acid medicines. Provided is a compound represented by Formula (I) or a pharmacologically acceptable salt thereof. In the Formula (I), R.sup.1 is a substituted or unsubstituted formula: (CH.sub.2).sub.aL.sub.1(CH.sub.2).sub.bCH.sub.3; R.sup.2 is a substituted or unsubstituted C5-C20 alkyl group or a substituted or unsubstituted formula: (CH.sub.2).sub.cL.sub.2(CH.sub.2).sub.aCH.sub.3; L.sup.1 and L.sup.2 are each independently C(?O)O, OC(?O), or OC(?O)O; a, b, c, and d are each independently an integer of at least 1, and the total of a and b and the total of c and d are each an integer of 5 to 25; R.sup.3 to R.sup.7 are each independently a hydrogen atom, a substituted or unsubstituted C.sup.1-C.sup.6 alkyl group, or the like; R.sup.8, R.sup.9, and R.sup.10 are each a hydrogen atom; the constituent atoms in the Formula (I) may form a ring; Z is OC(?O), C(?O)O, OC(?O)O, or the like; and X is O or S.
POLYETHERAMINES BASED ON 1,3-DIALCOHOLS
Described herein is an etheramine mixture including at least 90% by weight, based on the total weight of the etheramine mixture, of an amine of Formula (I) and/or (II),
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wherein R.sub.1-R.sub.12 are independently selected from H, alkyl, cycloalkyl, aryl, alkylaryl, or arylalkyl, wherein at least one of R.sub.1-R.sub.6 and at least one of R.sub.7-R.sub.12 is different from H, wherein A.sub.1-A.sub.9 are independently selected from linear or branched alkanediyl groups having 2 to 18 carbon atoms,
wherein Z.sub.1-Z.sub.4 are independently selected from OH and linear OCH.sub.2CH.sub.2CH.sub.2NH.sub.2, wherein the degree of amination of each of the etheramines of Formula (I) and Formula (II) is at least 50%, and wherein the sum of x+y is in the range of from 2 to 200, wherein x1 and y1; and x.sub.1+y.sub.1 is in the range of from 2 to 200, wherein x.sub.11 and y.sub.11.
POLYETHERAMINES BASED ON 1,3-DIALCOHOLS
Described herein is an etheramine mixture including at least 90% by weight, based on the total weight of the etheramine mixture, of an amine of Formula (I) and/or (II),
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wherein R.sub.1-R.sub.12 are independently selected from H, alkyl, cycloalkyl, aryl, alkylaryl, or arylalkyl, wherein at least one of R.sub.1-R.sub.6 and at least one of R.sub.7-R.sub.12 is different from H, wherein A.sub.1-A.sub.9 are independently selected from linear or branched alkanediyl groups having 2 to 18 carbon atoms,
wherein Z.sub.1-Z.sub.4 are independently selected from OH and linear OCH.sub.2CH.sub.2CH.sub.2NH.sub.2, wherein the degree of amination of each of the etheramines of Formula (I) and Formula (II) is at least 50%, and wherein the sum of x+y is in the range of from 2 to 200, wherein x1 and y1; and x.sub.1+y.sub.1 is in the range of from 2 to 200, wherein x.sub.11 and y.sub.11.