IP Library Granted Patent US 8,217,035
Granted Patent B2
US 8,217,035 · App. 12/161,537 · Granted Jul 10, 2012

Pyrimidine derivatives used as PI-3-kinase inhibitors

Assignee: Novartis AG
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Quick Facts
Patent No.
US 8,217,035
App. No.
12/161,537
Granted
Jul 10, 2012
Kind
B2
Abstract

Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.

Claims (8)

1. The compound 4-(trifluoromethyl)-5-(2,6-dimorpholinopyrimidin-4-yl)pyridin-2-amine, of structure:

or a pharmaceutically acceptable salt thereof.

2. A composition, comprising a pharmaceutically acceptable carrier and an amount of a compound of claim 1 effective to inhibit PI3-K activity in a human or animal subject when administered thereto.

3. The composition of claim 2 further comprising at least one agent for the treatment of cancer.

4. The composition of claim 3 , wherein the at least one agent for the treatment of cancer is vatalanib, imatinib, erlotinib, lapatinib, pertuzumab, trastuzumab, capecitabine, gemcitabine, irinotecan, paclitaxel, cisplatin, carboplatin, fulvestrant, dexamethasone, bevacizumab, docetaxel or gefitinib.

5. A method for treating ovarian cancer in a human or animal subject having ovarian cancer, comprising administering to the human or animal subject a composition comprising an amount of a compound of claim 1 effective to inhibit PI3-K activity in the human or animal subject.

6. The method of claim 5 further comprising administering to the human or animal subject at least one agent for the treatment of cancer.

7. The method of claim 6 , wherein the at least one agent for the treatment of cancer is vatalanib, imatinib, erlotinib, lapatinib, pertuzumab, trastuzumab, capecitabine, gemcitabine, irinotecan, paclitaxel, cisplatin, carboplatin, fulvestrant, dexamethasone, bevacizumab, docetaxel or gefitinib.

Assignments (5)
CORRECTIVE ASSIGNMENT TO CORRECT THE 5TH INVENTORS LAST NAME TO BARTULIS PREVIOUSLY RECORDED ON REEL 023249 FRAME 0244. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Oct 18, 2022
From: BURGER, MATTHEW; NI, ZHI-JIE; PECCHI, SABINA; ATALLAH, GORDANA; BARTULIS, SARAH; FRAZIER, KELLY; SMITH, AARON; VERHAGEN, JOELLE; ZHANG, YANCHEN; WAGMAN, ALLAN S.; NG, SIMON; PFISTER, KEITH; POON, DANIEL; LOUIE, ALICIA; PICK, TERESA; BARSANTI, PAUL; IWANOWICZ, EDWIN; FANTL, WENDY; HENDRICKSON, TOM; KNAPP, MARK; MERRITT, HANNE; VOLIVA, CHARLES; WIESMANN, MARION; XIN, XIAOHUA
To: CHIRON CORPORATION
Reel/Frame 061701/0697 →
CORRECTIVE ASSIGNMENT TO CORRECT THE THE MISSPELLING OF INVENTOR KNAPP'S LAST NAME IN THE RECORDATION COVER SHEET FROM <KANPP> TO <KNAPP> PREVIOUSLY RECORDED ON REEL 023038 FRAME 0099. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT OF THEIR APPLICATION NO. 12/161,537, FILED JULY 18, 2008, TO CHIRON CORPORATION. Recorded Sep 17, 2009
From: BURGER, MATTHEW; NI, ZHI-JIE; PECCHI, SABINA; ATALLAH, GORDANA; BARTULLIS, SARAH; FRAZIER, KELLY; SMITH, AARON; VERHAGEN, JOELLE; ZHANG, YANCHEN; WAGMAN, ALLAN S.; NG, SIMON; PFISTER, KEITH; POON, DANIEL; LOUIE, ALICIA; PICK, TERESA; BARSANTI, PAUL; IWANOWICZ, EDWIN; FANTL, WENDY; HENDRICKSON, TOM; KNAPP, MARK; MERRITT, HANNE; VOLIVA, CHARLES; WIESMANN, MARION; XIN, XIAOHUA
To: CHIRON CORPORATION
Reel/Frame 023249/0244 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 31, 2009
From: BURGER, MATTHEW; NI, ZHI-JIE; PECCHI, SABINA; ATALLAH, GORDANA; BARTULLIS, SARAH; FRAZIER, KELLY; SMITH, AARON; VERHAGEN, JOELLE; ZHANG, YANCHEN; WAGMAN, ALLAN S.; NG, SIMON; PFISTER, KEITH; POON, DANIEL; LOUIE, ALICIA; PICK, TERESA; BARSANTI, PAUL; IWANOWICZ, EDWIN; FANTL, WENDY; HENDRICKSON, TOM; KANPP, MARK; MERRITT, HANNE; VOLIVA, CHARLES; WIESMANN, MARION; XIN, XIAOHUA
To: CHIRON CORPORATION
Reel/Frame 023038/0099 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 31, 2009
From: NOVARTIS VACCINES AND DIAGNOSTICS INC.
To: NOVARTIS AG
Reel/Frame 023038/0547 →
MERGER AND NAME CHANGE Recorded Jul 31, 2009
From: CHIRON CORPORATION
To: NOVARTIS VACCINES AND DIAGNOSTICS, INC.
Reel/Frame 023042/0806 →
Continuity (2)
Provisional Application 60760789 · Jan 20, 2006
Related Publication 20100249126A1 · Sep 30, 2010