Claims for Patent: 9,789,193

Summary for Patent: 9,789,193

Title:	Compositions for treating cancer and methods for making the same
Abstract:	Described herein are compositions and methods relating to chemotherapeutic agent conjugates and the treatment of cancer.
Inventor(s):	Sengupta; Shiladitya (Waltham, MA), Kulkarni; Ashish (Waltham, MA), Rao; Poornima (Waltham, MA), Roy; Bhaskar (Belmont, MA)
Assignee:	THE BRIGHAM AND WOMEN\'S HOSPITAL, INC. (Boston, MA)
Application Number:	14/406,938
Patent Claims:	1. A composition comprising a conjugate, the conjugate comprising a chemotherapeutic agent conjugated to cholesterol, wherein conjugate is of Formula (III): ##STR00013## 2. The composition of claim 1, wherein the composition further comprises a lipid in addition to the conjugate. 3. The composition of claim 2, wherein the lipid is a lipid conjugated with polyethylene glycol (PEG). 4. The composition of claim 3, wherein the PEG conjugated lipid is selected from the group consisting of: PEG conjugated diacylglycerols and dialkylglycerols; PEG-conjugated phosphatidylethanolamine and phosphatidic acid; PEG conjugated ceramides; PEG conjugated dialkylamines; PEG conjugated 1,2-diacyloxypropan-3-amines; 1,2-distearoyl-sn-glycem-3-phosphoethanolamine-N-[amino(polyethylene glycol)-2000] (DSPE-PEG2000); and any combinations thereof. 5. The composition of any of claim 1 or 2-4, wherein the composition further comprises a phospholipid. 6. The composition of claim 5, wherein the phospholipid is selected from the group consisting of: phosphatidyl cholines; phosphatidyl cholines with acyl groups having 6 to 22 carbon atoms; phosphatidyl ethanolamines; phosphatidyl inositols; phosphatidic acids; phosphatidyl serines; sphingomyelin; phosphatidyl glycerols; phosphatidylcholine; phosphatidylglycerol; lecithin; .beta.,.gamma.-dipalmitoyl-.alpha.-lecithin; sphingomyelin; phosphatidylserine; phosphatidic acid; N-(2,3-di(9-(Z)-octadecenyloxy))-prop-1-yl-N,N,N-trimethylammonium chloride; phosphatidylethanolamine; lysolecithin; lysophosphatidylethanolamine; phosphatidylinositol; cephalin; cardiolipin; cerebrosides; dicetylphosphate; dioleoylphosphatidylcholine; dipalmitoylphosphatidylcholine; dipalmitoylphosphatidylglycerol; dioleoylphosphatidylglycerol; palmitoyl-oleoyl-phosphatidylcholine; di-stearoyl-phosphatidylcholine; stearoyl-palmitoyl-phosphatidylcholine; di-palmitoyl-phosphatidylethanolamine; di-stearoyl-phosphatidylethanolamine; di-myrstoyl-phosphatidylserine; di-oleyl-phosphatidylcholine; dimyristoyl phosphatidyl choline (DMPC); dioleoylphosphatidylethanolamine (DOPE); palmitoyloleoylphosphatidylcholine (POPC); egg phosphatidylcholine (EPC); distearoylphosphatidylcholine (DSPC); dioleoylphosphatidylcholine (DOPC); dipalmitoylphosphatidylcholine (DPPC); dioleoylphosphatidylglycerol (DOPG); dipalmitoylphosphatidylglycerol (DPPG); -phosphatidylethanolamine (POPE); dioleoyl-phosphatidylethanolamine 4-(N-maleimidomethyl)-cyclohexane-1-carboxylate (DOPE-mal); L-a-phosphatidylcholine; and any combinations thereof. 7. The composition of any of claim 1 or 2-6, further comprising a targeting agent. 8. The composition of claim 7, wherein the targeting agent is selected from the group consisting of: peptides; polypeptides; proteins; enzymes; peptidomimetics; glycoproteins; antibodies (monoclonal or polyclonal) and portions and fragments thereof; lectins; nucleosides; nucleotides; nucleoside and nucleotide analogues; nucleic acids; monosaccharides; disaccharides; trisaccharides; oligosaccharides; polysaccharides; lipopolysaccharides; vitamins; steroids; hormones; cofactors; receptors; receptor ligands; and iRGD (amino acid sequence CRGDKGPDC (SEQ ID NO: 1. 9. The composition of any of claim 1 or 2-8, wherein the composition further comprises an anticancer agent in addition to the conjugate. 10. The composition of claim 9, wherein the anticancer agent is selected from the group consisting of: a platinum compound, paclitaxel; carboplatin; bortezomib; vorinostat; rituximab; temozolomide; rapamycin; an alkylating agent; cyclosphosphamide; an alkyl sulfonate; busulfan; improsulfan; piposulfan; an aziridine; an ethylenimine; a methylamelamine; an acetogenin; a camptothecin; a cryptophycin; a nitrogen mustard; a nitrosurea; an antibiotic; a enediyne antibiotic; a bisphosphonate; doxorubicin; a mitomycin; an anti-metabolite; a folic acid analogue; a purine analog; a pyrimidine analog; an androgen; an anti-adrenal; an epothilone; a maytansinoid; a trichothecene; gemcitabine; 6-thioguanine; mercaptopurine; methotrexate; vinblastine; etoposide; ifosfamide; mitoxantrone; vincristine; vinorelbine; novantrone; teniposide; edatrexate; daunomycin; aminopterin; xeloda; ibandronate; irinotecan; a topoisomerase inhibitor; a retinoid; capecitabine; combretastatin; leucovorin; lapatinib; erlotinib; and a compound having the structure of formula (IV): ##STR00014## 11. The composition of any of claim 1 or 2-10, wherein the composition comprises the conjugate, a PEG conjugated lipid, and a phospholipid. 12. The composition of claim 11, wherein the PEG conjugated lipid is DSPE-PEG2000 and the phospholipid is phosphatidylcholine.

Details for Patent 9,789,193

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997		2032-06-15
Genentech, Inc.	RITUXAN HYCELA	rituximab and hyaluronidase human	Injection	761064	06/22/2017		2032-06-15