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Last Updated: April 19, 2024

Claims for Patent: 9,181,277


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Summary for Patent: 9,181,277
Title:Aminoquinazoline derivatives and their salts and methods of use
Abstract: The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
Inventor(s): Zhang; Jiancun (San Mateo, CA), Zhang; Yingjun (Dongguan, CN), Zhang; Weihong (Dongguan, CN), Liu; Bing (Dongguan, CN), Zhang; Jiquan (Dongguan, CN), Liu; Jinlei (Dongguan, CN), Zhang; Lu (Dongguan, CN)
Assignee: SUNSHINE LAKE PHARMA CO., LTD. (Dongguan, Guangdong, CN)
Application Number:14/346,741
Patent Claims:1. A compound having formula (III) ##STR00297## wherein each of X.sup.9, X.sup.10 and X.sup.11 is independently CR.sup.eR.sup.f, NR.sup.e, O or S, with the proviso that at least one of X.sup.9, X.sup.10 and X.sup.11 is CR.sup.eR.sup.f; D is a bond, methylene or ethylene; each of R.sup.e and R.sup.f is independently H, C.sub.1-6 alkyl, C.sub.1-6 alkylacyl, C.sub.3-8 cycloalkyl, C.sub.6-10 aryl-C.sub.1-6-alkyl, or C.sub.1-6 haloalkyl; and n is 1 or 2.

2. A compound having one of the following structures: ##STR00298## ##STR00299## ##STR00300## ##STR00301## ##STR00302## ##STR00303## ##STR00304## ##STR00305## ##STR00306## ##STR00307## ##STR00308## ##STR00309## ##STR00310## ##STR00311## ##STR00312## ##STR00313## ##STR00314## ##STR00315## ##STR00316## or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, or a pharmaceutically acceptable salt thereof.

3. A pharmaceutical composition comprising the compound according to claim 1 and a pharmaceutically acceptable carrier, excipient, diluent, adjuvant, vehicle or a combination thereof.

4. The pharmaceutical composition according to claim 3 further comprising a therapeutic agent selected from a chemotherapeutic agent, an anti-proliferative agent, an agent for treating non-small cell lung cancer or epidermoid carcinoma, or a combination thereof.

5. The pharmaceutical composition according to claim 4, wherein the therapeutic agent is adriamycin, rapamycin, temsirolimus, everolimus, ixabepilone, gemcitabine, cyclophosphamide, dexamethasone, etoposide, fluorouracil, imatinibmesylate, dasatinib, nilotinib, erlotinib, lapatinib, gefitinib, sorafenib, sunitinib, an interferon, carboplatin, topotecan, taxol, vinblastine, vincristine, temozolomide, tositumomab, trabectedin, bevacizumab, trastuzumab, cetuximab, panitumumab or a combination thereof.

6. A pharmaceutical composition comprising the compound according to claim 2 and a pharmaceutically acceptable carrier, excipient, diluent, adjuvant, vehicle or a combination thereof.

7. The pharmaceutical composition according to claim 6 further comprising a therapeutic agent selected from a chemotherapeutic agent, an anti-proliferative agent, an agent for treating non-small cell lung cancer or epidermoid carcinoma, or a combination thereof.

8. The pharmaceutical composition according to claim 7, wherein the therapeutic agent is adriamycin, rapamycin, temsirolimus, everolimus, ixabepilone, gemcitabine, cyclophosphamide, dexamethasone, etoposide, fluorouracil, imatinibmesylate, dasatinib, nilotinib, erlotinib, lapatinib, gefitinib, sorafenib, sunitinib, an interferon, carboplatin, topotecan, taxol, vinblastine, vincristine, temozolomide, tositumomab, trabectedin, bevacizumab, trastuzumab, cetuximab, panitumumab or a combination thereof.

Details for Patent 9,181,277

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 2031-11-14
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 02/10/2017 ⤷  Try a Trial 2031-11-14
Glaxosmithkline Llc BEXXAR tositumomab and iodine i-131 tositumomab Injection 125011 06/27/2003 ⤷  Try a Trial 2031-11-14
Eli Lilly And Company ERBITUX cetuximab Injection 125084 02/12/2004 ⤷  Try a Trial 2031-11-14
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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