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Last Updated: March 29, 2024

Claims for Patent: 9,266,903


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Summary for Patent: 9,266,903
Title:Polymorphs of 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazole-5-yl)-5,6-dihydrobenzo[F]- imidazo [1,2-D][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide, methods of production, and pharmaceutical uses thereof
Abstract: The present invention relates to crystalline polymorphs of (2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]- imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide (GDC-0032, taselisib), methods of use, and processes of preparing thereof.
Inventor(s): Stults; Jeffrey (El Granada, CA)
Assignee: Genentech, Inc. (South San Francisco, CA)
Application Number:14/570,019
Patent Claims:1. A crystalline, mono-methanolate polymorph of (2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]- imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide designated the Form A polymorph that exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2-theta at approximately 10.1, 11.2, 14.0, 18.3, 20.2, and 22.0.

2. The Form A polymorph of claim 1 characterized by the X-ray powder diffraction pattern shown in FIG. 2.

3. A crystalline, isoamyl alcohol polymorph of (2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]- imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide designated the Form C polymorph that exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2-theta at approximately 6.2, 14.1, 17.2, 18.3, 21.9, and 26.7.

4. The Form C polymorph of claim 3 characterized by the X-ray powder diffraction pattern shown in FIG. 13.

5. A crystalline, mono-hydrate polymorph of (2-(4-(2-(1-isopropyl-3-methyl-1-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]i- midazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide designated the Form D polymorph that exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2-theta at approximately 12.2, 17.5, 17.7, 18.3, 20.1, 21.3, 22.8, and 26.0.

6. The Form D polymorph of claim 5 characterized by the X-ray powder diffraction pattern shown in FIG. 14.

7. A pharmaceutical composition comprising a therapeutically effective amount of the crystalline, isoamyl alcohol polymorph of claim 3, and a pharmaceutically acceptable carrier, glidant, diluent, or excipient.

8. The pharmaceutical composition of claim 7 in the form of a tablet.

9. The pharmaceutical composition of claim 7 wherein the therapeutically effective amount is from 1 to 100 mg.

10. A method of therapeutic treatment a hyperproliferative disorder in a mammal comprising administering the pharmaceutical composition of claim 7 wherein the hyperproliferative disorder is selected from the group consisting of multiple myeloma, lymphoma, leukemia, prostate cancer, breast cancer, hepatocellular carcinoma, lung cancer, pancreatic cancer, and colorectal cancer.

11. The method of claim 10 wherein the therapeutically effective amount is from 1 mg to 100 mg.

12. The method of claim 10 further comprising administering a chemotherapeutic agent selected from the group consisting of 5-fluorouracil, docetaxel, eribulin, gemcitabine, cobimetinib, 5-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-ca- rboxamide, paclitaxel, tamoxifen, fulvestrant, dexamethasone, pertuzumab, trastuzumab emtansine, trastuzumab and letrozole.

Details for Patent 9,266,903

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 09/25/1998 ⤷  Try a Trial 2039-02-26
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 02/10/2017 ⤷  Try a Trial 2039-02-26
Genentech, Inc. PERJETA pertuzumab Injection 125409 06/08/2012 ⤷  Try a Trial 2039-02-26
Genentech, Inc. HERCEPTIN HYLECTA trastuzumab and hyaluronidase-oysk Injection 761106 02/28/2019 ⤷  Try a Trial 2039-02-26
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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