Claims for Patent: 8,071,795

Summary for Patent: 8,071,795

Title:	HIF inhibitors
Abstract:	HIF-1 inhibitors and methods of use thereof are provided.
Inventor(s):	Van Meir; Erwin G (Tucker, GA), Nicolaou; Kyriacos (La Jolla, CA)
Assignee:	Emory University (Atlanta, GA) Scripps Research Institute (LaJolla, CA)
Application Number:	11/997,809
Patent Claims:	1. A pharmaceutical composition comprising, a compound selected from one or more of the following: ##STR00001## wherein X is selected from at least one of the following groups: ##STR00002## wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, and R18, are each independently selected from the following groups: H, OH, a branched or unbranched C.sub.1-12 alkyl group, an alkenyl group, an alkoxy group, an aryl group, a heterocycle group, an imidazole group, a substituted imidazole group, an alkyl substituted aryl group, a halogen substituted an aryl group, a halogen group, an amine group, NO.sub.2, and an acyl group; wherein R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, R29, R30, R31, R32, R33, R34, R35, R36, R37, R38, R39, R40, R41, R42, R43, R44, R45, R46, R47, R48, R49, R50, and R51 are each independently selected from the following groups: H, OH, a branched or unbranched C.sub.1-12 alkyl group, an alkenyl group, an alkoxy group, an aryl group, a heterocycle group, an imidazole group, a substituted imidazole group, an alkyl substituted aryl group, a halogen substituted aryl group, a halogen group, an amine group, NO.sub.2, and an acyl group; or a pharmaceutically acceptable salt thereof. 2. A pharmaceutical composition comprising, one or more compounds selected from the following: ##STR00003## ##STR00004## ##STR00005## wherein R52, R53, R54, R55, R56, R57, R58, R59, R60, R61, R62, R63, R64, R65, R66, R67, R68, R69, R70, R71, R72, R73, R74, R75, R76, R77, R78, R79, R80, R81, R82, R83, R84, R85, R86, R87, R88, R89, R90, R91, R92, R93, R94, R95, R96, R97, R98, R99, R100, R101, R102, R103, R104, R105, R106, R107, R108, R109, R110, R11, R112, R113, R114, R115, R116, R117, R118, R119, R120, R121, R122, R123, R124, R125, R126, R127, R128, R129, R130, R131, R132, R133, R134, R135, R136, R137, R138, R139, R140, R141, R142, R143, R144, R145, R146, R147, R148, R149, R150, R151, R152, R153, R154, R155, R156, R157, R158, R159, R160, R161, R162, and R163, are each independently selected from the following groups: H, OH, a branched or unbranched C.sub.1-12 alkyl group, an alkenyl group, an alkoxy group, an aryl group, a heterocycle group, an imidazole group, a substituted imidazole group, an alkyl substituted aryl group, a halogen substituted aryl group, a halogen group, an amine group, NO.sub.2, and an acyl group; or a pharmaceutically acceptable salt thereof. 3. The pharmaceutical composition of claim 1, further comprising a second therapeutic compound. 4. The pharmaceutical composition of claim 3, wherein the second therapeutic compound is an antibody, antibiotic, anti-inflammatory, anti-oxidant, analgesic, radioisotope, noscapine, paclitaxel, nocodazole, vinca alkaloids, adriamycin, alkeran, Ara-C, BiCNU, busulfan, CCNU, carboplatinum, cisplatinum, cytoxan, daunorubicin, DTIC, 5-FU, fludarabine, hydrea, idarubicin, ifosfamide, methotrexate, mithramycin, mitomycin, mitoxantrone, nitrogen mustard, velban, vincristine, VP-16, gemcitabine, herceptin, irinotecan, camptosar, CPT-11, leustatin, navelbine, rituxan, STI-571, taxotere, temozolomide, topotecan, hycamtin, xeloda, capecitabine, zevelin, and combinations thereof. 5. The pharmaceutical composition of claim 2, further comprising a second therapeutic compound. 6. The pharmaceutical composition of claim 5, wherein the second therapeutic compound is an antibody, antibiotic, anti-inflammatory, anti-oxidant, analgesic, radioisotope, noscapine, paclitaxel, nocodazole, vinca alkaloids, adriamycin, alkeran, Ara-C, BiCNU, busulfan, CCNU, carboplatinum, cisplatinum, cytoxan, daunorubicin, DTIC, 5-FU, fludarabine, hydrea, idarubicin, ifosfamide, methotrexate, mithramycin, mitomycin, mitoxantrone, nitrogen mustard, velban, vincristine, VP-16, gemcitabine, herceptin, irinotecan, camptosar, CPT-11, leustatin, navelbine, rituxan, STI-571, taxotere, temozolomide, topotecan, hycamtin, xeloda, capecitabine, zevelin, and combinations thereof. 7. A method of modulating HIF activity in a cell comprising: contacting the cell with a HIF inhibiting amount of the compositions of claim 2. 8. A method of treating cancer or a tumor in a host comprising administering to the host a HIF inhibiting amount of the compositions of claim 2 wherein the cancer or tumor is selected from the group consisting of cervical, ovarian, colon, breast, gastric, lung, skin, ovarian, pancreatic, prostate, and renal cancer. 9. A pharmaceutical composition of claim 1, wherein the compound of Formula B is N-cyclohexyl-N-((2,2-dimethyl-2H-chromen-6-yl)methyl)-2,4-dimethoxybenzen- esulfonamide or salt thereof. 10. A pharmaceutical composition of claim 1, wherein the compound of Formula C is N-((2,2-dimethyl-2H-chromen-6-yl)methyl)-N-isobutyl-3,4-dimethoxybenzenes- ulfonamide or salt thereof. 11. A pharmaceutical composition of claim 1, wherein the compound of Formula D is N-((2,2-dimethyl-2H-chromen-6-yl)methyl)-3,4-dimethoxy-N-phenylbenzenesul- fonamide or salt thereof.

Details for Patent 8,071,795

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997		2025-08-25
Idec Pharmaceuticals Corp.	RITUXAN	rituximab	Injection	103737	02/19/2002		2025-08-25
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	09/25/1998		2025-08-25