Claims for Patent: 7,714,139

Summary for Patent: 7,714,139

Title:	IDO inhibitors and methods of use
Abstract:	Compounds, compositions and methods for the treatment of malignancy are disclosed.
Inventor(s):	Prendergast; George C. (Bala Cynwyd, PA), Muller; Alexander J. (Media, PA), Duhadaway; James B. (Wilmington, DE), Malachowski; William (Collegeville, PA)
Assignee:	Lankenau Institute for Medcial Research (Wynnewood, PA)
Application Number:	10/550,444
Patent Claims:	1. A compound having indoleamine 2,3 dioxygenase (IDO) inhibitory activity, said compound having the: ##STR00017## wherein R.sub.1 is H or lower alkyl; R.sub.2 and R.sub.3 are joined together and represent part of a ring which is fused to the pyrrole moiety of formula (I) and which is selected from the group of: ##STR00018## (ii) wherein R.sub.E is a hydrocarbyl or alkyl-Q, Q representing a substituent of the formula: ##STR00019## the compound of formula (I) being a brassilexin derivative when R.sub.2 and R.sub.3 joined together represent (i), and an N-substituted brassilexin derivative when R.sub.2 and R.sub.3 joined together represent (ii); X, Y, and Z may be the same or different and are selected from the group consisting of H, halogen, NO.sub.2, and hydrocarbyl; or Y may also be isothiocyanate. 2. A pharmaceutical composition comprising an effective amount of the compound of claim 1 and a pharmaceutically acceptable carrier medium. 3. A pharmaceutical composition comprising an effective amount of at least one indoleamine 2,3-dioxygenase (IDO) inhibitor and at least one signal transduction inhibitor (STI) in a pharmaceutically acceptable carrier medium, wherein said at least one IDO inhibitor is compounds having the formula: ##STR00020## wherein R.sub.1 is H or lower alkyl; R.sub.2 and R.sub.3 are joined together and represent part of a ring which is fused to the pyrrole moiety of formula (I) and which is selected from the group of: ##STR00021## wherein R.sub.E is a hydrocarbyl or alkyl-Q, Q representing a substituent of the formula: ##STR00022## the compound of formula (I) being a brassilexin derivative when R.sub.2 and R.sub.3 joined together represent (i) and an N-substituted brassilexin derivative when R.sub.2 and R.sub.3 joined together represent (ii); X, Y, and Z may be the same or different and are selected from the group consisting of H, halogen, NO.sub.2, and hydrocarbyl; or Y may also be isothiocyanate. 4. The pharmaceutical composition of claim 3, wherein said at least one STI is selected from the group consisting of ber/abi kinase inhibitors, epidermal growth factor (EGF) receptor inhibitors, her-2/neu receptor inhibitors, farnesyl transferase inhibitors (FTIs), inhibitors of Akt family kinases or the Akt pathway, and cell cycle kinase inhibitors. 5. The pharmaceutical composition of claim 4, wherein said at least one STI is selected from the group consisting of STI 571, 551-774, C225, ABX-EGF, trastuzumab, L-744,832, rapamycin, LY294002, flavopiridal, and UNC-01. 6. The pharmaceutical composition of claim 5, wherein said at least one STI is L-744,832. 7. A pharmaceutical composition comprising an effective amount of at least one indoleamine 2,3-dioxygenase (IDO) inhibitor and at least one chemotherapeutic agent in a pharmaceutically acceptable carrier medium, wherein said at least one IDO inhibitor is selected from the group of compounds having the formula: ##STR00023## wherein R.sub.1 is H or lower alkyl; R.sub.2 and R.sub.3 are joined together and represent part of a ring which is fused to the pyrrole moiety of formula (I) and which is selected from the group of: ##STR00024## wherein R.sub.E is a hydrocarbyl or alkyl-Q, Q representing a substituent of the formula: ##STR00025## the compound of formula (I) being a brassilexin derivative when R.sub.2 and R.sub.3 joined together represent (i), and an N-substituted brassilexin derivative when R.sub.2 and R.sub.3 joined together represent (ii); X, Y, and Z may be the same or different and are selected from the group consisting of H, halogen, NO.sub.2, and hydrocarbyl; or Y may also be isothiocyanate. 8. The pharmaceutical composition of claim 7, wherein said at least one chemotherapeutic agent is selected from the group consisting of paclitaxel TAXOL.RTM., cisplatin, docetaxol, carboplatin, vincristine, vinbiastine, methotrexate, cyclophosphamide, CPT-11, 5-fluorouracil (5-FU), gemcitabine, estramustine, carmustine, adriamycin (doxorubicin), etoposide, arsenic trioxide, irinotecan, and epothilone derivatives. 9. The pharmaceutical composition of claim 4, wherein said at least one chemotherapeutic agent is paclitaxel.

Details for Patent 7,714,139

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	09/25/1998		2039-02-26
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	02/10/2017		2039-02-26
Genentech, Inc.	HERCEPTIN HYLECTA	trastuzumab and hyaluronidase-oysk	Injection	761106	02/28/2019		2039-02-26