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Last Updated: March 29, 2024

Claims for Patent: 7,855,204


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Summary for Patent: 7,855,204
Title:Derivatives of gefitinib
Abstract: This invention relates to novel quinazoline derivatives, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by inhibiting cell surface tyrosine receptor kinases.
Inventor(s): Tung; Roger (Lexington, MA)
Assignee: Concert Pharmaceuticals Inc. (Lexington, MA)
Application Number:12/358,238
Patent Claims:1. A compound of the formula A ##STR00014## or a pharmaceutically acceptable salt thereof, wherein the compound is selected from any one of the compounds depicted in the following Table: TABLE-US-00004 TABLE Cmpd Y.sup.1 = Y.sup.2 Y.sup.3 = Y.sup.4 Y.sup.5 = Y.sup.6 Y.sup.7 = Y.sup.8 R.sup.1 R.sup.2 R.sup.3 101 D D D D CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 F 102 H H H H CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 F 104 H H H H CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 F 108 D D D D CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 H 109 H H H H CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 H 110 D D D D CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 H 111 H H H H CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 H 112 D D D D CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 H 113 H H H H CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 H 114 D D D D CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 H 115 D D D D CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 OH 116 H H H H CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 OH 117 D D D D CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 OH 118 H H H H CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 OH 119 D D D D CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 OH 120 H H H H CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 OH 121 D D D D CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 OH 122 D D D D CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 OCD.sub.3 123 H H H H CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 OCD.sub.3 124 D D D D CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 OCD.sub.3 125 H H H H CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 OCD.sub.3 126 D D D D CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 OCD.sub.3 127 H H H H CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 OCD.sub.3 128 D D D D CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 OCD.sub.3 129 D D D D CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 OCH.sub.3 130 H H H H CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 OCH.sub.3 131 D D D D CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 OCH.sub.3 132 H H H H CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 OCH.sub.3 133 D D D D CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 OCH.sub.3 134 H H H H CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 OCH.sub.3 135 D D D D CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 OCD.sub.3 136 D D D D CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 Cl 137 H H H H CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 Cl 138 D D D D CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 Cl 139 H H H H CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 Cl 140 D D D D CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 Cl 141 H H H H CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 Cl 142 D D D D CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 Cl 143 D D D D CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 Br 144 H H H H CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 Br 145 D D D D CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 Br 146 H H H H CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 Br 147 D D D D CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 Br 148 H H H H CD.sub.3 CD.sub.2CD.sub.2CD.sub.2 Br 149 D D D D CD.sub.3 CH.sub.2CH.sub.2CH.sub.2 Br.

2. The compound of claim 1, wherein any atom not designated as deuterium is present at its natural isotopic abundance.

3. A pyrogen-free pharmaceutical composition comprising as a first therapeutic agent a compound of claim 1 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.

4. The composition of claim 3, further comprising a second therapeutic agent useful in the treatment of a patient suffering from non-small cell lung cancer.

5. The composition of claim 4, wherein the second therapeutic agent is selected from anastrozole, cediranib, bexarotene, calcitriol, capecitabine, carboplatin, cefixime, celecoxib, canertinib, cisplatin, dexamethasone, docetaxel, cetuximab, etoposide, everolimus, fluorouracil, fulvestrant, gemcitabine, irinotecan, leucovorin, loperamide, oxaliplatin, paclitaxel, PEG-interferon alpha, pemetrexed, raltitrexed, simvastatin, sirolimus, sunitinib, tamoxifen, temozolomide, topotecan, trastuzumab, and vinorelbine.

6. A method of treating a patient suffering from, or susceptible to, non-small cell lung cancer comprising the step of administering to the patient in need thereof a composition of claim 3.

7. The method of claim 6, wherein the patient is a smoker.

8. The method of claim 6, wherein the patient is a non-smoker.

9. The method of claim 6, further comprising the additional step of co-administering to the patient in need thereof a second therapeutic agent useful in the treatment of non-small cell lung cancer.

10. The method of claim 9, wherein the second therapeutic agent is selected from AZD2171, bexarotene, carboplatin, celecoxib, cisplatin, docetaxel, cetuximab, everolimus, fulvestrant, gemcitabine, paclitaxel, pemetrexed, simvastatin, sirolimus, and vinorelbine.

Details for Patent 7,855,204

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 2028-01-22
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 02/10/2017 ⤷  Try a Trial 2028-01-22
Eli Lilly And Company ERBITUX cetuximab Injection 125084 02/12/2004 ⤷  Try a Trial 2028-01-22
Eli Lilly And Company ERBITUX cetuximab Injection 125084 03/28/2007 ⤷  Try a Trial 2028-01-22
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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