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Last Updated: April 26, 2024

Claims for Patent: 7,767,669


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Summary for Patent: 7,767,669
Title:Small molecule PI 3-kinase inhibitors and methods of their use
Abstract: Compounds having formula I are provided where the variables have the values described herein. ##STR00001## Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and combinations with other agents. A method of treating a patient comprises administering a pharmaceutical formulation according to the invention to a patient in need thereof.
Inventor(s): Nuss; John M. (Danville, CA), Pecchi; Sabina (Oakland, CA), Renhowe; Paul A. (Danville, CA)
Assignee: Novartis AG (Basel, CH)
Application Number:12/188,984
Patent Claims:1. A compound having the formula: ##STR00244## or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, wherein R.sub.1 is H; R.sub.2 is selected from the group consisting of substituted aryl and substituted heteroaryl, where said substituted heteroaryl is selected from the group consisting of a substituted pyridyl, a substituted pyrazinyl, a substituted pyrimidinyl, a substituted pyrrolyl, a substituted pyrazolyl, a substituted indazolyl, a substituted quinolinyl, and a substituted isoquinolinyl; X is a direct bond; Y is substituted or unsubstituted heterocyclyl; and W is substituted and or unsubstituted morpholinyl.

2. The compound of claim 1, wherein said substituted aryl is a substituted phenyl.

3. The compound of claim 1, wherein said substituted aryl is hydroxy phenyl.

4. The compound of claim 1, wherein said substituted heteroaryl is a substituted pyridyl.

5. The compound of claim 1, wherein said unsubstituted heterocyclyl is selected from the group consisting of morpholinyl, pyrrolidinyl, imidazolidinyl, piperazinyl, piperidinyl, and diazepanyl.

6. The compound of claim 1, wherein said unsubstituted heterocyclyl is morpholinyl.

7. The compound of claim 1, wherein W is unsubstituted morpholinyl.

8. A composition, comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

9. The composition of claim 8 further comprising at least one additional agent for the treatment of breast cancer.

10. The composition of claim 9, wherein the at least one additional agent for the treatment of breast cancer is selected from the group consisting of irinotecan, topotecan, gemcitabine, imatinib mesylate, herceptin, 5-fluorouracil, leucovorin, carboplatin, cisplatin, taxanes, tezacitabine, cyclophosphamide, vinca alkaloids, imatinib, anthracyclines, rituximab, tamoxifen, CPT 11, and trastuzumab.

11. A method for treating breast cancer comprising administering to a subject in need of such treatment an effective amount of a compound of claim 1.

12. The method of claim 11 further comprising administering to said subject at least one additional agent for the treatment of breast cancer.

13. The method of claim 12, wherein the at least one additional agent for the treatment of breast cancer is selected form the group consisting of irinotecan, topotecan, gemcitabine, imatinib mesylate, herceptin, 5-fluorouracil, leucovorin, carboplatin, cisplatin, taxanes, tezacitabine, cyclophosphamide, vinca alkaloids, imatinib, anthracyclines, rituximab, tamoxifen, CPT 11, and trastuzumab.

Details for Patent 7,767,669

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Genentech, Inc. RITUXAN rituximab Injection 103705 11/26/1997 ⤷  Try a Trial 2022-11-21
Idec Pharmaceuticals Corp. RITUXAN rituximab Injection 103737 02/19/2002 ⤷  Try a Trial 2022-11-21
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 09/25/1998 ⤷  Try a Trial 2022-11-21
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 02/10/2017 ⤷  Try a Trial 2022-11-21
Genentech, Inc. RITUXAN HYCELA rituximab and hyaluronidase human Injection 761064 06/22/2017 ⤷  Try a Trial 2022-11-21
Genentech, Inc. HERCEPTIN HYLECTA trastuzumab and hyaluronidase-oysk Injection 761106 02/28/2019 ⤷  Try a Trial 2022-11-21
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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