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Last Updated: April 25, 2024

Claims for Patent: 9,920,033

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Summary for Patent: 9,920,033

Title:	Crystalline form of a substituted quinoline compound and pharmaceutical compositions thereof
Abstract:	The present invention relates to a crystalline form of N-(3-fluoro-4-((7-(2-hydroxy-2-methylpropoxy)quinolin-4-yl)oxy)phenyl)-1,- 5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide p-toluenesulfonate, the process for preparing the crystalline form thereof, and the pharmaceutical compositions comprising the crystalline form thereof. This invention also relates to a method of using such a crystalline form and pharmaceutical compositions comprising the crystalline form thereof in the treatment of hyperproliferative diseases in mammals, especially in humans.
Inventor(s):	Xi; Ning (Newbury Park, CA), Sun; Mingming (Guangdong, CN)
Assignee:	Calitor Sciences, LLC (Newbury Park, CA) Sunshine Lake Pharma Co., LTD. (Dongguan, Guangdong, CN)
Application Number:	15/350,013
Patent Claims:	1. A crystalline form of a compound of formula (I): ##STR00003## wherein the crystalline form is form A having: a) an X-ray powder diffraction pattern comprising peaks, in terms of 2.theta., at about 8.29.degree., about 9.53.degree., about 11.11.degree., about 16.99.degree., about 18.75.degree. and about 23.66.degree.; or b) an X-ray powder diffraction pattern comprising peaks, in terms of 2.theta., at 8.29.degree..+-.0.2.degree., 9.53.degree..+-.0.2.degree., 11.11.degree..+-.0.2.degree., 16.99.degree..+-.0.2.degree., 18.75.degree..+-.0.2.degree. and 23.66.degree..+-.0.2.degree.; or c) unit cell parameters substantially equal to the following: (i) unit cell dimensions: a=8.7430 .ANG., b=12.8275 .ANG., c=16.1281 .ANG., a=96.689.degree., .beta.=95.737.degree., .gamma.=99.649.degree.; (ii) space group: P-1; (iii) volume: 1757.82 .ANG..sup.3; (iv) Z: 2; and (v) calculated density: 1.377 g/cm.sup.3. 2. The crystalline form of claim 1 having an X-ray powder diffraction pattern comprising peaks, in terms of 2.theta., at about 8.29.degree., about 9.53.degree., about 11.11.degree., about 15.28.degree., about 16.99.degree., about 18.75.degree., about 19.14.degree., about 19.98.degree., about 20.42.degree., about 21.77.degree., about 22.02.degree. and about 23.66.degree., or at 8.29.degree..+-.0.2.degree., 9.53.degree..+-.0.2.degree., 11.11.degree..+-.0.2.degree., 15.28.degree..+-.0.2.degree., 16.99.degree..+-.0.2.degree. 18.75.degree..+-.0.2.degree. 19.14.degree..+-.0.2.degree. 19.98.degree..+-.0.2.degree. 20.42.degree..+-.0.2.degree. 21.77.degree..+-.0.2.degree., 22.02.degree..+-.0.2.degree. and 23.66.degree..+-.0.2.degree.. 3. The crystalline form of claim 1, wherein the X-ray powder diffraction pattern comprising peaks, in terms of 2.theta., at about 8.29.degree., about 9.53.degree., about 11.11.degree., about 12.67.degree., about 14.04.degree., about 15.28.degree., about 15.82.degree., about 16.99.degree., about 18.75.degree., about 19.14.degree., about 19.98.degree., about 20.42.degree., about 21.77.degree., about 22.02.degree., about 22.45.degree., about 22.65.degree., about 23.66.degree., about 26.85.degree., about 27.94.degree. and about 28.34.degree., or at 8.29.degree..+-.0.2.degree., 9.53.degree..+-.0.2.degree., 11.11.degree..+-.0.2.degree., 12.67.degree..+-.0.2.degree., 14.04.degree..+-.0.2.degree., 15.28.degree..+-.0.2.degree., 15.82.degree..+-.0.2.degree., 16.99.degree..+-.0.2.degree., 18.75.degree..+-.0.2.degree. 19.14.degree..+-.0.2.degree. 19.98.degree..+-.0.2.degree. 20.42.degree..+-.0.2.degree. 21.77.degree..+-.0.2.degree. 22.02.degree..+-.0.2.degree. 22.45.degree..+-.0.2.degree., 22.65.degree..+-.0.2.degree., 23.66.degree..+-.0.2.degree., 26.85.degree..+-.0.2.degree., 27.94.degree..+-.0.2.degree. and 28.34.degree..+-.0.2.degree.. 4. The crystalline form of claim 1, wherein the X-ray powder diffraction pattern is substantially in accordance with that shown in FIG. 2. 5. The crystalline form of claim 1, wherein the crystalline form is substantially pure. 6. A pharmaceutical composition comprising the crystalline form of claim 1 and a pharmaceutically acceptable excipient, carrier, vehicle or a combination thereof. 7. The pharmaceutical composition of claim 6 further comprising a therapeutic agent. 8. The pharmaceutical composition of claim 7, wherein the therapeutic agent is melphalan, cyclophosphamide, ifosfamide, busulfan, carmustine, lomustine, streptozocin, cisplatin, carboplatin, oxaliplatin, dacarbazine, temozolomide, procarbazine, methotrexate, fluorouracil, cytarabine, gemcitabine, mercaptopurine, fludarabine, vinblastine, vincristine, vinorelbine, paclitaxel, docetaxel, topotecan, irinotecan, etoposide, trabectedin, dactinomycin, doxorubicin, epirubicin, daunorubicin, mitoxantrone, bleomycin, mitomycin, ixabepilone, tamoxifen, flutamide, gonadorelin analogues, megestrol, prednisone, dexamethasone, methylprednisolone, thalidomide, interferon alfa, leucovorin, sirolimus, temsirolimus, everolimus, afatinib, alisertib, amuvatinib, apatinib, axitinib, bosutinib, bortezomib, brivanib, cediranib, cabozantinib, crenolanib, crizotinib, dabrafenib, dacomitinib, danusertib, dasatinib, dovitinib, erlotinib, foretinib, ganetespib, gefitinib, ibrutinib, icotinib, imatinib, iniparib, lapatinib, lenvatinib, linifanib, linsitinib, masitinib, momelotinib, neratinib, nilotinib, niraparib, oprozomib, olaparib, pazopanib, pegaptanib, pictilisib, ponatinib, quizartinib, radotinib, regorafenib, rigosertib, rucaparib, ruxolitinib, saracatinib, saridegib, sorafenib, sunitinib, tasocitinib, telatinib, tivantinib, tivozanib, tofacitinib, trametinib, vandetanib, veliparib, vemurafenib, vismodegib, volasertib, alemtuzumab, bevacizumab, brentuximabvedotin, catumaxomab, cetuximab, denosumab, gemtuzumab, ipilimumab, nimotuzumab, ofatumumab, panitumumab, ramucirumab, rituximab, tositumomab, trastuzumab, idelalisib, duvelisib, gilteritinib, buparlisib, taselisib, copanlisib, voxtalisib, pilaralisib, sonolisib, perifosine, alectinib, ibrutinib, pertuzumab, nintedanib, cobimetinib, temsirolimus, sirolimus, pixantrone or a combination thereof. 9. A method of treating or lessening the severity of a proliferative disorder in a patient by administering to the patient with the crystalline form of claim 1, wherein the proliferative disorder is gastric cancer, gastric adenocarcinoma, kidney cancer, renal cell carcinoma, liver cancer, hepatocellular carcinoma or lung cancer thereof. 10. A method of treating or lessening the severity of a proliferative disorder in a patient by administering to the patient with the pharmaceutical composition of claim 6, wherein the proliferative disorder is gastric cancer, gastric adenocarcinoma, kidney cancer, renal cell carcinoma, liver cancer, hepatocellular carcinoma or lung cancer thereof.

Details for Patent 9,920,033

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Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997	⤷ Try a Trial	2035-11-14
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	09/25/1998	⤷ Try a Trial	2035-11-14
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	02/10/2017	⤷ Try a Trial	2035-11-14
>Applicant	>Tradename	>Biologic Ingredient	>Dosage Form	>BLA	>Approval Date	>Patent No.	>Expiredate

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