http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-079745-A1
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_cf32b60391b469c41e86c353437f5751 |
classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J31-006 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K2300-00 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J43-003 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J41-0055 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J31-006 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-1272 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-7088 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-127 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
filingDate | 2010-12-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2012-02-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | AR-079745-A1 |
titleOfInvention | LIPIDS, LIPID COMPOSITIONS, TREATMENT METHOD AND KIT |
abstract | Claim 1: A composition comprising at least one cationic lipid, at least one auxiliary lipid and at least one furtive lipid, for the delivery of a biologically active agent, wherein the biologically active agent is to be delivered to a selected tissue or cell. from: a) a liver or liver cells, wherein the composition has a cationic lipid with a pKa of approximately 6.2 or greater; b) a tumor or a tumor cell, wherein the composition has a cationic lipid with a pKa of approximately 6.2 or less; c) a liver or liver cells, wherein the composition has a cationic lipid with a pKa of about 5.1 to about 7.4; and d) a tumor or a tumor cell, wherein the composition has a cationic lipid with a pKa of about 5.0 to about 6.7. Claim 2: A compound of the formula (1) or a pharmaceutically acceptable salt or derivative thereof wherein R1 and R2 together with the nitrogen atom with which they are attached, form a C3-20 heterocycloalkyl group, hetero- optionally substituted C3-20 cycloalkenyl, C3-20 heterocycloalkynyl or C5-20 heteroaryl; a is absent or is optionally substituted C1-4 alkylene; b is absent or is optionally substituted C1-4 alkylene; c is absent or is optionally substituted C1-4 alkylene; X1 is O or S; X2 is O or S; Y1 is C10-30 alkenyl, C10-30 alkynyl, C10-30 hetero-alkenyl, or optionally substituted C10-30 hetero alkynyl; L is absent or is - (La) d- (Lb) e- (Lc) f-, where La is C1-15 alkylene, C1-15 alkenylene, C1-15 alkynylene, C1-15 hetero-alkylene, hetero- optionally substituted C1-15 alkenylene or C1-15 hetero-alkynylene; Lb is optionally substituted C6-14 arylene or C5-13 heteroarylene; Lc is C1-15 alkylene, C1-15 alkenylene, C1-15 alkynylene, C1-15 hetero-alkylene, C1-15 hetero-alkenylene or optionally substituted C1-15 hetero-alkynylene; d is 0 or 1; e is 0 or 1; and f is 0 or 1; and Y2 is an optionally substituted steroid. Claim 4: A furtive lipid of the formula (11) or a pharmaceutically acceptable salt or derivative thereof, wherein Z is a hydrophilic head group component selected from PEG and poly (oxazoline) based polymers, poly- (ethylene oxide), poly- (vinyl alcohol), poly (glycerol), poly- (N-vinyl-pyrrolidone), poly- [N- (2-hydroxy-propyl) -methacrylamide] and poly- (amino acid) s , wherein the polymer can be linear or branched, and where the polymer can be optionally substituted; where Z is polymerized by n subunits; n is a degree of polymerization averaged between 10 and 200 units of Z, where n is optimized for different types of polymers; L1 is an optionally substituted C1-10 alkylene or C1-10 hetero-alkylene linker, which includes zero, one, two or more of an ether (for example, -O-), ester (for example, -C (O) O-), succinate (for example, -O (O) C-CH2-CH2-C (O) O-)), carbamate (for example, -OC (O) -NR'-), carbonate (for example, -OC (O) O-), ketone (for example, -CC (O) -C-), carbonyl (for example, -C (O) -), urea (for example, -NRC (O) NR'- ), amine (for example, -NR'-), amide (for example, -C (O) NR'-), imine (for example, -C (NR ') -), thioether (for example, -S- ), xanthate (for example, -OC (S) S-), and phosphodiester (for example, -OP (O) 2O-); any of which may be substituted by zero, one or more Z groups; wherein R 'is independently selected from H, -NH-, -O-, -S-, a phosphate, or an optionally substituted C1-10 alkylene; X1 and X2 are independently selected from a carbon atom, or a heteroatom selected from -NH-, -O-, -S- or a phosphate; A1 and A2 are independently selected from a C6-30 alkyl, C6-30 alkenyl and C6-30 alkynyl, wherein A1 and A2 may be the same or different, or where A1 and A2, together with the carbon atom with which are attached, form an optionally substituted steroid. Claim 15: The composition of claims 13 or 14, wherein the biologically active agent is selected from the group consisting of antibodies, cholesterol, hormones, antivirals, peptides, polypeptides, proteins, nucleoproteins, chemotherapeutic products, low weight drugs. molecular, vitamins, co-factors, nucleosides, nucleoside derivatives, nucleotides, oligonucleotides, enzymatic nucleic acids, anti-sense nucleic acids, triplex-forming oligonucleotides, 2,5-A antisense chimeras, allozymes, aptamers, grandfather RNA molecules and analogs thereof, and small nucleic acid molecules, such as an RNA interference agent (RNAi), short interference nucleic acid (siAN), short interference RNA (siRNA), double stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA). Claim 20: The method of claim 19, wherein the disease or condition is a cancer, a liver disease, or a disease that responds to treatment with an RNAi construct. |
priorityDate | 2009-12-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 46.