Claims for Patent: 8,691,866

Summary for Patent: 8,691,866

Title:	HIF inhibitors and use thereof
Abstract:	The present invention is directed to HIF inhibitors and methods of preventing cell proliferation, reducing inflammation, and treating an angiogenic disease or disorders.
Inventor(s):	Iliopoulos; Othon (Cambridge, MA), Zimmer; Michael (Arlington, MA)
Assignee:	The General Hospital Corporation (Boston, MA)
Application Number:	13/139,058
Patent Claims:	1. A method of reducing inflammation or treating a cancer with increased HIF levels or activity in the pentose phosphate (hexose monophosophate, HMP shunt) in a subject in need thereof, comprising administrating to said subject an effective amount of an HIF inhibitor, wherein said inhibitor is 3-(2,5-diethoxyphenyl)-1-(2-thienyl)-2-propen-1-one, having the following structure: ##STR00024## or methyl 3-{2-[cyano(methylsulfonyl)methylene]hydrazino}thiophene-2-carboxylate, having the following structure: ##STR00025## 2. The method of claim 1, comprising pulsed or sustained release administration of said HIF inhibitor, wherein pulse administration is administration of a single therapeutic dose in 5-30 individual pulse doses. 3. The method of claim 2, wherein interval between individual pulse doses is 24 hours or greater. 4. The method of claim 2, wherein administration of a single therapeutic dose occurs in about 5 to about 10 pulses. 5. The method of claim 1, comprising pulsed or sustained release administration of said HIF inhibitor, wherein pulse administration is administration of a single therapeutic dose in greater than 20 pulses. 6. The method of claim 1, comprising co-administering a second therapeutic agent selected from the group consisting of an antibody, antibiotic, anti-inflammatory, anti-oxidant, analgesic, radioisotope, noscapine, paclitaxel, nocodazole, buslfulan, lomustine (CCNU), caboplatinum, cisplatinum, cytoxan, daunorubicin, dacarbazine (DTIC), 5-fluorouracil (5-FU), fludarabine, hydroxyurea, idarubicin, ifosfamide, methotrexrate, mithramycin, mitomycin, mitoxantrone, nitrogen mustard, vinblastine, vincristine, CPT-11, cladribine, vinorebne tartrate, rituximab, STI-571, docetaxel, temozolomide, topotecan, capecitaine, ibritumomab tiuxetan, and any combination thereof. 7. The method of claim 1, wherein said cancer is renal cell, colon, breast, prostate, glioblastoma multiform, or endometrial. 8. The method of claim 7, wherein said cancer comprises a VHL gene mutation.

Details for Patent 8,691,866

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997		2039-03-29
Idec Pharmaceuticals Corp.	RITUXAN	rituximab	Injection	103737	02/19/2002		2039-03-29
Acrotech Biopharma Llc	ZEVALIN	ibritumomab tiuxetan	Injection	125019	02/19/2002		2039-03-29
Genentech, Inc.	RITUXAN HYCELA	rituximab and hyaluronidase human	Injection	761064	06/22/2017		2039-03-29