Claims for Patent: 9,133,162

Summary for Patent: 9,133,162

Title:	Substituted quinoline compounds and methods of use
Abstract:	The present invention provides novel substituted quinoline compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
Inventor(s):	Xi; Ning (Newbury Park, CA)
Assignee:	SUNSHINE LAKE PHARMA CO., LTD. (Dongguan, Guangdong, CN) CALITOR SCIENCES, LLC (Newbury Park, CA)
Application Number:	13/400,586
Patent Claims:	1. A compound of Formula (I): ##STR00052## or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, wherein: R.sup.1 is hydroxy C.sub.2-6 alkoxy; R.sup.2 is H, alkoxy, or hydroxyalkoxy; R.sup.3 is H or F; R.sup.4 is H, F, Cl, Br, I, CN, alkyl, haloalkyl, heterocyclyl, heterocyclylalkyl, cycloalkyl, or cycloalkylalkyl; and X is CH or N, wherein at least one of R.sup.1 and R.sup.2 is hydroxyalkoxy. 2. The compound according to claim 1, wherein R.sup.3 is H or F; R.sup.2 is H or methoxy; and R.sup.4 is H, F, Cl, Br, I, CN, C.sub.1-3 haloalkyl, C.sub.2-5 heterocyclyl, C.sub.2-5 heterocyclyl C.sub.1-3 alkyl, C.sub.3-6 cycloalkyl, or C.sub.3-6 cycloalkyl C.sub.1-3 alkyl. 3. The compound according to claim 1, wherein R.sup.2 is H or methoxy; R.sup.3 is H or F; R.sup.4 is H or F; and X is CH. 4. The compound according to claim 1, wherein R.sup.2 is H; R.sup.3 is H or F; R.sup.4 is H; and X is CH. 5. The compound of claim 1 having one of the following structures: ##STR00053## ##STR00054## ##STR00055## or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. 6. A pharmaceutical composition comprising the compound according to claim 1 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 atherosclerosis, an agent for treating lung fibrosis, and combinations thereof. 8. The pharmaceutical composition according to claim 7, wherein the additional therapeutic agent is adriamycin, rapamycin, temsirolimus, everolimus, ixabepilone, gemcitabin, cyclophosphamide, dexamethasone, etoposide, fluorouracil, afatinib, alisertib, amuvatinib, axitinib, bosutinib, brivanib, cabozantinib, cediranib, crenolanib, crizotinib, dabrafenib, dacomitinib, dasatinib, danusertib, dovitinib, erlotinib, foretinib, ganetespib, gefitinib, ibrutinib, imatinib, iniparib, lapatinib, lenvatinib, linifanib, linsitinib, masitinib, momelotinib, motesanib, neratinib, niraparib, nilotinib, oprozomib, olaparib, pazopanib, pictilisib, ponatinib, quizartinib, regorafenib, rigosertib, rucaparib, ruxolitinib, saracatinib, saridegib, sorafenib, sunitinib, tasocitinib, telatinib, tivantinib, tivozanib, tofacitinib, trametinib, vandetanib, veliparib, vemurafenib, vismodegib, volasertib, an interferon, carboplatin, topotecan, taxol, vinblastine, vincristine, temozolomide, tositumomab, trabedectin, belimumab, bevacizumab, brentuximab, cetuximab, gemtuzumab, ipilimumab, ofatumumab, panitumumab, ranibizumab, rituximab, tositumomab, trastuzumab or a combination thereof.

Details for Patent 9,133,162

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997		2031-02-28
Idec Pharmaceuticals Corp.	RITUXAN	rituximab	Injection	103737	02/19/2002		2031-02-28
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	09/25/1998		2031-02-28
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	02/10/2017		2031-02-28
Glaxosmithkline Llc	BEXXAR	tositumomab and iodine i-131 tositumomab	Injection	125011	06/27/2003		2031-02-28
Eli Lilly And Company	ERBITUX	cetuximab	Injection	125084	02/12/2004		2031-02-28