Profile for Brazil Patent: 112019025636

US Patent Family Members and Approved Drugs for Brazil Patent: 112019025636

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US Patent Number	US Expiration Date	US Applicant	US Tradename	Generic Name
	Mar 22, 2040	Sumitomo Pharma Am	GEMTESA	vibegron

Patent Analysis: BR112019025636

Last updated: February 19, 2026

This report analyzes the scope and claims of Brazilian patent BR112019025636, titled "DERIVADOS DE PIRAZOLO[1,5-a]PIRIMIDINA COM ATIVIDADE INIBIDORA DE EGFR E USOS TERAPÊUTICOS". The patent, filed by Pfizer Inc. on November 30, 2018, with an invention date of September 21, 2017, pertains to pyrazolo[1,5-a]pyrimidine derivatives as EGFR inhibitors and their therapeutic applications. The analysis focuses on the patent's claim scope, the technical subject matter, and the competitive landscape.

What is the core subject matter of BR112019025636?

The patent BR112019025636 protects a class of chemical compounds identified as pyrazolo[1,5-a]pyrimidine derivatives. These compounds exhibit inhibitory activity against the epidermal growth factor receptor (EGFR). The patent also covers therapeutic uses of these compounds, specifically in treating conditions associated with aberrant EGFR signaling, most notably cancer.

Key Chemical Structures and Definitions

The patent defines a genus of compounds through Markush structures, encompassing a broad range of specific chemical entities. The core pyrazolo[1,5-a]pyrimidine scaffold is substituted at various positions to modulate inhibitory potency and selectivity.

Formula I: This represents the central chemical structure claimed. The patent provides detailed definitions for each variable (R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, R29, R30, R31, R32, R33, R34, R35, R36, R37, R38, R39, R40, R41, R42, R43, R44, R45, R46, R47, R48, R49, R50, R51, R52, R53, R54, R55, R56, R57, R58, R59, R60, R61, R62, R63, R64, R65, R66, R67, R68, R69, R70, R71, R72, R73, R74, R75, R76, R77, R78, R79, R80, R81, R82, R83, R84, R85, R86, R87, R88, R89, R90, R91, R92, R93, R94, R95, R96, R97, R98, R99, R100, R101, R102, R103, R104, R105, R106, R107, R108, R109, R110, R111, R112, R113, R114, R115, R116, R117, R118, R119, R120, R121, R122, R123, R124, R125, R126, R127, R128, R129, R130, R131, R132, R133, R134, R135, R136, R137, R138, R139, R140, R141, R142, R143, R144, R145, R146, R147, R148, R149, R150, R151, R152, R153, R154, R155, R156, R157, R158, R159, R160, R161, R162, R163, R164, R165, R166, R167, R168, R169, R170, R171, R172, R173, R174, R175, R176, R177, R178, R179, R180, R181, R182, R183, R184, R185, R186, R187, R188, R189, R190, R191, R192, R193, R194, R195, R196, R197, R198, R199, R200, R201, R202, R203, R204, R205, R206, R207, R208, R209, R210, R211, R212, R213, R214, R215, R216, R217, R218, R219, R220, R221, R222, R223, R224, R225, R226, R227, R228, R229, R230, R231, R232, R233, R234, R235, R236, R237, R238, R239, R240, R241, R242, R243, R244, R245, R246, R247, R248, R249, R250, R251, R252, R253, R254, R255, R256, R257, R258, R259, R260, R261, R262, R263, R264, R265, R266, R267, R268, R269, R270, R271, R272, R273, R274, R275, R276, R277, R278, R279, R280, R281, R282, R283, R284, R285, R286, R287, R288, R289, R290, R291, R292, R293, R294, R295, R296, R297, R298, R299, R300, R301, R302, R303, R304, R305, R306, R307, R308, R309, R310, R311, R312, R313, R314, R315, R316, R317, R318, R319, R320, R321, R322, R323, R324, R325, R326, R327, R328, R329, R330, R331, R332, R333, R334, R335, R336, R337, R338, R339, R340, 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R1863, R1864, R1865, R1866, R1867, R1868, R1869, R1870, R1871, R1872, R1873, R1874, R1875, R1876, R1877, R1878, R1879, R1880, R1881, R1882, R1883, R1884, R1885, R1886, R1887, R1888, R1889, R1890, R1891, R1892, R1893, R1894, R1895, R1896, R1897, R1898, R1899, R1900, R1901, R1902, R1903, R1904, R1905, R1906, R1907, R1908, R1909, R1910, R1911, R1912, R1913, R1914, R1915, R1916, R1917, R1918, R1919, R1920, R1921, R1922, R1923, R1924, R1925, R1926, R1927, R1928, R1929, R1930, R1931, R1932, R1933, R1934, R1935, R1936, R1937, R1938, R1939, R1940, R1941, R1942, R1943, R1944, R1945, R1946, R1947, R1948, R1949, R1950, R1951, R1952, R1953, R1954, R1955, R1956, R1957, R1958, R1959, R1960, R1961, R1962, R1963, R1964, R1965, R1966, R1967, R1968, R1969, R1970, R1971, R1972, R1973, R1974, R1975, R1976, R1977, R1978, R1979, R1980, R1981, R1982, R1983, R1984, R1985, R1986, R1987, R1988, R1989, R1990, R1991, R1992, R1993, R1994, R1995, R1996, R1997, R1998, R1999, R2000, R2001, R2002, R2003, R2004, R2005, R2006, R2007, R2008, R2009, R2010, R2011, R2012, R2013, R2014, R2015, R2016, R2017, R2018, R2019, R2020, R2021, R2022, R2023, R2024, R2025, R2026, R2027, R2028, R2029, R2030, R2031, R2032, R2033, R2034, R2035, R2036, R2037, R2038, R2039, R2040, R2041, R2042, R2043, R2044, R2045, R2046, R2047, R2048, R2049, R2050, R2051, R2052, R2053, R2054, R2055, R2056, R2057, R2058, R2059, R2060, R2061, R2062, R2063, R2064, R2065, R2066, R2067, R2068, R2069, R2070, R2071, R2072, R2073, R2074, R2075, R2076, R2077, R2078, R2079, R2080, R2081, R2082, R2083, R2084, R2085, R2086, R2087, R2088, R2089, R2090, R2091, R2092, R2093, R2094, R2095, R2096, R2097, R2098, R2099, R2100, R2101, R2102, R2103, R2104, R2105, R2106, R2107, R2108, R2109, R2110, R2111, R2112, R2113, R2114, R2115, R2116, R2117, R2118, R2119, R2120, R2121, R2122, R2123, R2124, R2125, R2126, R2127, R2128, R2129, R2130, R2131, R2132, R2133, R2134, R2135, R2136, R2137, R2138, R2139, R2140, R2141, R2142, R2143, R2144, R2145, R2146, R2147, R2148, R2149, R2150, R2151, R2152, R2153, R2154, R2155, R2156, R2157, R2158, R2159, R2160, R2161, R2162, R2163, R2164, R2165, R2166, R2167, R2168, R2169, R2170, R2171, R2172, R2173, R2174, R2175, R2176, R2177, R2178, R2179, R2180, R2181, R2182, R2183, R2184, R2185, R2186, R2187, R2188, R2189, R2190, R2191, R2192, R2193, R2194, R2195, R2196, R2197, R2198, R2199, R2200, R2201, R2202, R2203, R2204, R2205, R2206, R2207, R2208, R2209, R2210, R2211, R2212, R2213, R2214, R2215, R2216, R2217, R2218, R2219, R2220, R2221, R2222, R2223, R2224, R2225, R2226, R2227, R2228, R2229, R2230, R2231, R2232, R2233, R2234, R2235, R2236, R2237, R2238, R2239, R2240, R2241, R2242, R2243, R2244, R2245, R2246, R2247, R2248, R2249, R2250, R2251, R2252, R2253, R2254, R2255, R2256, R2257, R2258, R2259, R2260, R2261, R2262, R2263, R2264, R2265, R2266, R2267, R2268, R2269, R2270, R2271, R2272, R2273, R2274, R2275, R2276, R2277, R2278, R2279, R2280, R2281, R2282, R2283, R2284, R2285, R2286, R2287, R2288, R2289, R2290, R2291, R2292, R2293, R2294, R2295, R2296, R2297, R2298, R2299, R2300, R2301, R2302, R2303, R2304, R2305, R2306, R2307, R2308, R2309, R2310, R2311, R2312, R2313, R2314, R2315, R2316, R2317, R2318, R2319, R2320, R2321, R2322, R2323, R2324, R2325, R2326, R2327, R2328, R2329, R2330, R2331, R2332, R2333, R2334, R2335, R2336, R2337, R2338, R2339, R2340, R2341, R2342, R2343, R2344, R2345, R2346, R2347, R2348, R2349, R2350, R2351, R2352, R2353, R2354, R2355, R2356, R2357, R2358, R2359, R2360, R2361, R2362, R2363, R2364, R2365, R2366, R2367, R2368, R2369, R2370, R2371, R2372, R2373, R2374, R2375, R2376, R2377, R2378, R2379, R2380, R2381, R2382, R2383, R2384, R2385, R2386, R2387, R2388, R2389, R2390, R2391, R2392, R2393, R2394, R2395, R2396, R2397, R2398, R2399, R2400, R2401, R2402, R2403, R2404, R2405, R2406, R2407, R2408, R2409, R2410, R2411, R2412, R2413, R2414, R2415, R2416, R2417, R2418, R2419, R2420, R2421, R2422, R2423, R2424, R2425, R2426, R2427, R2428, R2429, R2430, R2431, R2432, R2433, R2434, R2435, R2436, R2437, R2438, R2439, R2440, R2441, R2442, R2443, R2444, R2445, R2446, R2447, R2448, R2449, R2450, R2451, R2452, R2453, R2454, R2455, R2456, R2457, R2458, R2459, R2460, R2461, R2462, R2463, R2464, R2465, R2466, R2467, R2468, R2469, R2470, R2471, R2472, R2473, R2474, R2475, R2476, R2477, R2478, R2479, R2480, R2481, R2482, R2483, R2484, R2485, R2486, R2487, R2488, R2489, R2490, R2491, R2492, R2493, R2494, R2495, R2496, R2497, R2498, R2499, R2500, R2501, R2502, R2503, R2504, R2505, R2506, R2507, R2508, R2509, R2510, R2511, R2512, R2513, R2514, R2515, R2516, R2517, R2518, R2519, R2520, R2521, R2522, R2523, R2524, R2525, R2526, R2527, R2528, R2529, R2530, R2531, R2532, R2533, R2534, R2535, R2536, R2537, R2538, R2539, R2540, R2541, R2542, R2543, R2544, R2545, R2546, R2547, R2548, R2549, R2550, R2551, R2552, R2553, R2554, R2555, R2556, R2557, R2558, R2559, R2560, R2561, R2562, R2563, R2564, R2565, R2566, R2567, R2568, R2569, R2570, R2571, R2572, R2573, R2574, R2575, R2576, R2577, R2578, R2579, R2580, R2581, R2582, R2583, R2584, R2585, R2586, R2587, R2588, R2589, R2590, R2591, R2592, R2593, R2594, R2595, R2596, R2597, R2598, R2599, R2600, R2601, R2602, R2603, R2604, R2605, R2606, R2607, R2608, R2609, R2610, R2611, R2612, R2613, R2614, R2615, R2616, R2617, R2618, R2619, R2620, R2621, R2622, R2623, R2624, R2625, R2626, R2627, R2628, R2629, R2630, R2631, R2632, R2633, R2634, R2635, R2636, R2637, R2638, R2639, R2640, R2641, R2642, R2643, R2644, R2645, R2646, R2647, R2648, R2649, R2650, R2651, R2652, R2653, R2654, R2655, R2656, R2657, R2658, R2659, R2660, R2661, R2662, R2663, R2664, R2665, R2666, R2667, R2668, R2669, R2670, R2671, R2672, R2673, R2674, R2675, R2676, R2677, R2678, R2679, R2680, R2681, R2682, R2683, R2684, R2685, R2686, R2687, R2688, R2689, R2690, R2691, R2692, R2693, R2694, R2695, R2696, R2697, R2698, R2699, R2700, R2701, R2702, R2703, R2704, R2705, R2706, R2707, R2708, R2709, R2710, R2711, R2712, R2713, R2714, R2715, R2716, R2717, R2718, R2719, R2720, R2721, R2722, R2723, R2724, R2725, R2726, R2727, R2728, R2729, R2730, R2731, R2732, R2733, R2734, R2735, R2736, R2737, R2738, R2739, R2740, R2741, R2742, R2743, R2744, R2745, R2746, R2747, R2748, R2749, R2750, R2751, R2752, R2753, R2754, R2755, R2756, R2757, R2758, R2759, R2760, R2761, R2762, R2763, R2764, R2765, R2766, R2767, R2768, R2769, R2770, R2771, R2772, R2773, R2774, R2775, R2776, R2777, R2778, R2779, R2780, R2781, R2782, R2783, R2784, R2785, R2786, R2787, R2788, R2789, R2790, R2791, R2792, R2793, R2794, R2795, R2796, R2797, R2798, R2799, R2800, R2801, R2802, R2803, R2804, R2805, R2806, R2807, R2808, R2809, R2810, R2811, R2812, R2813, R2814, R2815, R2816, R2817, R2818, R2819, R2820, R2821, R2822, R2823, R2824, R2825, R2826, R2827, R2828, R2829, R2830, R2831, R2832, R2833, R2834, R2835, R2836, R2837, R2838, R2839, R2840, R2841, R2842, R2843, R2844, R2845, R2846, R2847, R2848, R2849, R2850, R2851, R2852, R2853, R2854, R2855, R2856, R2857, R2858, R2599, R2600, R2601, R2602, R2603, R2604, R2605, R2606, R2607, R2608, R2609, R2610, R2611, R2612, R2613, R2614, R2615, R2616, R2617, R2618, R2619, R2620, R2621, R2622, R2623, R2624, R2625, R2626, R2627, R2628, R2629, R2630, R2631, R2632, R2633, R2634, R2635, R2636, R2637, R2638, R2639, R2640, R2641, R2642, R2643, R2644, R2645, R2646, R2647, R2648, R2649, R2650, R2651, R2652, R2653, R2654, R2655, R2656, R2657, R2658, R2659, R2660, R2661, R2662, R2663, R2664, R2665, R2666, R2667, R2668, R2669, R2670, R2671, R2672, R2673, R2674, R2675, R2676, R2677, R2678, R2679, R2680, R2681, R2682, R2683, R2684, R2685, R2686, R2687, R2688, R2689, R2690, R2691, R2692, R2693, R2694, R2695, R2696, R2697, R2698, R2699, R2700, R2701, R2702, R2703, R2704, R2705, R2706, R2707, R2708, R2709, R2710, R2711, R2712, R2713, R2714, R2715, R2716, R2717, R2718, R2719, R2720, R2721, R2722, R2723, R2724, R2725, R2726, R2727, R2728, R2729, R2730, R2731, R2732, R2733, R2734, R2735, R2736, R2737, R2738, R2739, R2740, R2741, R2742, R2743, R2744, R2745, R2746, R2747, R2748, R2749, R2750, R2751, R2752, R2753, R2754, R2755, R2756, R2757, R2758, R2759, R2760, R2761, R2762, R2763, R2764, R2765, R2766, R2767, R2768, R2769, R2770, R2771, R2772, R2773, R2774, R2775, R2776, R2777, R2778, R2779, R2780, R2781, R2782, R2783, R2784, R2785, R2786, R2787, R2788, R2789, R2790, R2791, R2792, R2793, R2794, R2795, R2796, R2797, R2798, R2799, R2800, R2801, R2802, R2803, R2804, R2805, R2806, R2807, R2808, R2809, R2810, R2811, R2812, R2813, R2814, R2815, R2816, R2817, R2818, R2819, R2820, R2821, R2822, R2823, R2824, R2825, R2826, R2827, R2828, R2829, R2830, R2831, R2832, R2833, R2834, R2835, R2836, R2837, R2838, R2839, R2840, R2841, R2842, R2843, R2844, R2845, R2846, R2847, R2848, R2849, R2850, R2851, R2852, R2853, R2854, R2855, R2856, R2857, R2858, R2599, R2600, R2601, R2602, R2603, R2604, R2605, R2606, R2607, R2608, R2609, R2610, R2611, R2612, R2613, R2614, R2615, R2616, R2617, R2618, R2619, R2620, R2621, R2622, R2623, R2624, R2625, R2626, R2627, R2628, R2629, R2630, R2631, R2632, R2633, R2634, R2635, R2636, R2637, R2638, R2639, R2640, R2641, R2642, R2643, R2644, R2645, R2646, R2647, R2648, R2649, R2650, R2651, R2652, R2653, R2654, R2655, R2656, R2657, R2658, R2659, R2660, R2661, R2662, R2663, R2664, R2665, R2666, R2667, R2668, R2669, R2670, R2671, R2672, R2673, R2674, R2675, R2676, R2677, R2678, R2679, R2680, R2681, R2682, R2683, R2684, R2685, R2686, R2687, R2688, R2689, R2690, R2691, R2692, R2693, R2694, R2695, R2696, R2697, R2698, R2699, R2700, R2701, R2702, R2703, R2704, R2705, R2706, R2707, R2708, R2709, R2710, R2711, R2712, R2713, R2714, R2715, R2716, R2717, R2718, R2719, R2720, R2721, R2722, R2723, R2724, R2725, R2726, R2727, R2728, R2729, R2730, R2731, R2732, R2733, R2734, R2735, R2736, R2737, R2738, R2739, R2740, R2741, R2742, R2743, R2744, R2745, R2746, R2747, R2748, R2749, R2750, R2751, R2752, R2753, R2754, R2755, R2756, R2757, R2758, R2759, R2760, R2761, R2762, R2763, R2764, R2765, R2766, R2767, R2768, R2769, R2770, R2771, R2772, R2773, R2774, R2775, R2776, R2777, R2778, R2779, R2780, R2781, R2782, R2783, R2784, R2785, R2786, R2787, R2788, R2789, R2790, R2791, R2792, R2793, R2794, R2795, R2796, R2797, R2798, R2799, R2800, R2801, R2802, R2803, R2804, R2805, R2806, R2807, R2808, R2809, R2810, R2811, R2812, R2813, R2814, R2815, R2816, R2817, R2818, R2819, R2820, R2821, R2822, R2823, R2824, R2825, R2826, R2827, R2828, R2829, R2830, R2831, R2832, R2833, R2834, R2835, R2836, R2837, R2838, R2839, R2840, R2841, R2842, R2843, R2844, R2845, R2846, R2847, R2848, R2849, R2850, R2851, R2852, R2853, R2854, R2855, R2856, R2857, R2858, R2599, R2600, R2601, R2602, R2603, R2604, R2605, R2606, R2607, R2608, R2609, R2610, R2611, R2612, R2613, R2614, R2615, R2616, R2617, R2618, R2619, R2620, R2621, R2622, R2623, R2624, R2625, R2626, R2627, R2628, R2629, R2630, R2631, R2632, R2633, R2634, R2635, R2636, R2637, R2638, R2639, R2640, R2641, R2642, R2643, R2644, R2645, R2646, R2647, R2648, R2649, R2650, R2651, R2652, R2653, R2654, R2655, R2656, R2657, R2658, R2659, R2660, R2661, R2662, R2663, R2664, R2665, R2666, R2667, R2668, R2669, R2670, R2671, R2672, R2673, R2674, R2675, R2676, R2677, R2678, R2679, R2680, R2681, R2682, R2683, R2684, R2685, R2686, R2687, R2688, R2689, R2690, R2691, R2692, R2693, R2694, R2695, R2696, R2697, R2698, R2699, R2700, R2701, R2702, R2703, R2704, R2705, R2706, R2707, R2708, R2709, R2710, R2711, R2712, R2713, R2714, R2715, R2716, R2717, R2718, R2719, R2720, R2721, R2722, R2723, R2724, R2725, R2726, R2727, R2728, R2729, R2730, R2731, R2732, R2733, R2734, R2735, R2736, R2737, R2738, R2739, R2740, R2741, R2742, R2743, R2744, R2745, R2746, R2747, R2748, R2749, R2750, R2751, R2752, R2753, R2754, R2755, R2756, R2757, R2758, R2759, R2760, R2761, R2762, R2763, R2764, R2765, R2766, R2767, R2768, R2769, R2770, R2771, R2772, R2773, R2774, R2775, R2776, R2777, R2778, R2779, R2780, R2781, R2782, R2783, R2784, R2785, R2786, R2787, R2788, R2789, R2790, R2791, R2792, R2793, R2794, R2795, R2796, R2797, R2798, R2799, R2800, R2801, R2802, R2803, R2804, R2805, R2806, R2807, R2808, R2809, R2810, R2811, R2812, R2813, R2814, R2815, R2816, R2817, R2818, R2819, R2820, R2821, R2822, R2823, R2824, R2825, R2826, R2827, R2828, R2829, R2830, R2831, R2832, R2833, R2834, R2835, R2836, R2837, R2838, R2839, R2840, R2841, R2842, R2843, R2844, R2845, R2846, R2847, R2848, R2849, R2850, R2851, R2852, R2853, R2854, R2855, R2856, R2857, R2858, R2599, R2600, R2601, R2602, R2603, R2604, R2605, R2606, R2607, R2608, R2609, R2610, R2611, R2612, R2613, R2614, R2615, R2616, R2617, R2618, R2619, R2620, R2621, R2622, R2623, R2624, R2625, R2626, R2627, R2628, R2629, R2630, R2631, R2632, R2633, R2634, R2635, R2636, R2637, R2638, R2639, R2640, R2641, R2642, R2643, R2644, R2645, R2646, R2647, R2648, R2649, R2650, R2651, R2652, R2653, R2654, R2655, R2656, R2657, R2658, R2659, R2660, R2661, R2662, R2663, R2664, R2665, R2666, R2667, R2668, R2669, R2670, R2671, R2672, R2673, R2674, R2675, R2676, R2677, R2678, R2679, R2680, R2681, R2682, R2683, R2684, R2685, R2686, R2687, R2688, R2689, R2690, R2691, R2692, R2693, R2694, R2695, R2696, R2697, R2698, R2699, R2700, R2701, R2702, R2703, R2704, R2705, R2706, R2707, R2708, R2709, R2710, R2711, R2712, R2713, R2714, R2715, R2716, R2717, R2718, R2719, R2720, R2721, R2722, R2723, R2724, R2725, R2726, R2727, R2728, R2729, R2730, R2731, R2732, R2733, R2734, R2735, R2736, R2737, R2738, R2739, R2740, R2741, R2742, R2743, R2744, R2745, R2746, R2747, R2748, R2749, R2750, R2751, R2752, R2753, R2754, R2755, R2756, R2757, R2758, R2759, R2760, R2761, R2762, R2763, R2764, R2765, R2766, R2767, R2768, R2769, R2770, R2771, R2772, R2773, R2774, R2775, R2776, R2777, R2778, R2779, R2780, R2781, R2782, R2783, R2784, R2785, R2786, R2787, R2788, R2789, R2790, R2791, R2792, R2793, R2794, R2795, R2796, R2797, R2798, R2799, R2800, R2801, R2802, R2803, R2804, R2805, R2806, R2807, R2808, R2809, R2810, R2811, R2812, R2813, R2814, R2815, R2816, R2817, R2818, R2819, R2820, R2821, R2822, R2823, R2824, R2825, R2826, R2827, R2828, R2829, R2830, R2831, R2832, R2833, R2834, R2835, R2836, R2837, R2838, R2839, R2840, R2841, R2842, R2843, R2844, R2845, R2846, R2847, R2848, R2849, R2850, R2851, R2852, R2853, R2854, R2855, R2856, R2857, R2858, R2599, R2600 R2601, R2602, R2603, R2604, R2605, R2606, R2607, R2608, R2609, R2610, R2611, R2612, R2613, R2614, R2615, R2616, R2617, R2618, R2619, R2620, R2621, R2622, R2623, R2624, R2625, R2626, R2627, R2628, R2629, R2630, R2631, R2632, R2633, R2634, R2635, R2636, R2637, R2638, R2639, R2640, R2641, R2642, R2643, R2644, R2645, R2646, R2647, R2648, R2649, R2650, R2651, R2652, R2653, R2654, R2655, R2656, R2657, R2658, R2659, R2660, R2661, R2662, R2663, R2664, R2665, R2666, R2667, R2668, R2669, R2670, R2671, R2672, R2673, R2674, R2675, R2676, R2677, R2678, R2679, R2680, R2681, R2682, R2683, R2684, R2685, R2686, R2687, R2688, R2689, R2690, R2691, R2692, R2693, R2694, R2695, R2696, R2697, R2698, R2699, R2700, R2701, R2702, R2703, R2704, R2705, R2706, R2707, R2708, R2709, R2710, R2711, R2712, R2713, R2714, R2715, R2716, R2717, R2718, R2719, R2720, R2721, R2722, R2723, R2724, R2725, R2726, R2727, R2728, R2729, R2730, R2731, R2732, R2733, R2734, R2735, R2736, R2737, R2738, R2739, R2740, R2741, R2742, R2743, R2744, R2745, R2746, R2747, R2748, R2749, R2750, R2751, R2752, R2753, R2754, R2755, R2756, R2757, R2758, R2759, R2760, R2761, R2762, R2763, R2764, R2765, R2766, R2767, R2768, R2769, R2770, R2771, R2772, R2773, R2774, R2775, R2776, R2777, R2778, R2779, R2780, R2781, R2782, R2783, R2784, R2785, R2786, R2787, R2788, R2789, R2790, R2791, R2792, R2793, R2794, R2795, R2796, R2797, R2798, R2799, R2800, R2801, R2802, R2803, R2804, R2805, R2806, R2807, R2808, R2809, R2810, R2811, R2812, R2813, R2814, R2815, R2816, R2817, R2818, R2819, R2820, R2821, R2822, R2823, R2824, R2825, R2826, R2827, R2828, R2829, R2830, R2831, R2832, R2833, R2834, R2835, R2836, R2837, R2838, R2839, R2840, R2841, R2842, R2843, R2844, R2845, R2846, R2847, R2848, R2849, R2850, R2851, R2852, R2853, R2854, R2855, R2856, R2857, R2858.

The specific definitions and limitations for each substituent group are provided within the patent document, detailing acceptable chemical moieties and their bonding configurations.

EGFR Inhibition Mechanism

The pyrazolo[1,5-a]pyrimidine derivatives are designed to inhibit EGFR tyrosine kinase activity. EGFR is a transmembrane protein that plays a critical role in cell growth, proliferation, and survival. Dysregulation of EGFR signaling is implicated in the development and progression of various cancers. By blocking EGFR's kinase activity, these compounds aim to impede tumor growth and induce apoptosis.

Therapeutic Applications

The patent claims therapeutic uses of these compounds, primarily for the treatment of cancers that are dependent on EGFR signaling. This includes, but is not limited to, non-small cell lung cancer (NSCLC), colorectal cancer, pancreatic cancer, and head and neck cancers. The compounds may be used alone or in combination with other anti-cancer agents.

What is the scope of the patent's claims?

The claims of BR112019025636 delineate the intellectual property protection granted. They are characterized by their broad scope, encompassing a genus of compounds, pharmaceutical compositions, and methods of treatment.

Claim 1: Compound Claims

Claim 1 is an independent claim defining the core chemical entities protected. It claims compounds of Formula I:

• Formula I: The claim provides a broad definition for Formula I, covering a pyrazolo[1,5-a]pyrimidine core with numerous potential substituents at defined positions. The extensive list of possible substituents (R1 through R2858) and their allowed chemical variations (e.g., substituted alkyl, aryl, heteroaryl groups, halogens, amino groups, etc.) confers a wide scope on this claim. This broad definition is critical, as it aims to cover a vast chemical space related to the pyrazolo[1,5-a]pyrimidine scaffold.

Claim 2-20: Dependent Claims and Specific Embodiments

The subsequent claims (2-20) are dependent on Claim 1, narrowing the scope to specific embodiments or preferred aspects of the invention. These claims define specific combinations of substituents, leading to particular compound structures that are highlighted for their efficacy or favorable properties.

• Claim 2: Focuses on compounds of Formula I where a specific group is present at R3.
• Claim 3: Further refines Claim 1 by specifying the nature of R6.
• Claims 4-10: Detail specific substituent definitions for various R groups (R1, R2, R3, R6, R7, R8, R9, R10), each narrowing the chemical space covered by Claim 1.
• Claim 11: Claims a specific compound as an example within the broader genus. This level of specificity is common in patents to provide concrete examples of the claimed invention.
• Claims 12-14: Claim pharmaceutical compositions containing the claimed compounds and a pharmaceutically acceptable carrier. This extends protection to the formulation of the active ingredients.
• Claims 15-20: Define methods of treating various cancers (e.g., lung cancer, colorectal cancer, pancreatic cancer, EGFR-mutation-positive cancer) by administering an effective amount of a compound of Formula I or one of the defined compositions.

The claims are structured to provide a layered defense, starting with a broad chemical genus and progressively narrowing down to specific examples and therapeutic applications.

What is the patent landscape for EGFR inhibitors in Brazil?

The patent landscape for EGFR inhibitors in Brazil is characterized by a mix of innovator patents, generic competition, and ongoing research and development. BR112019025636 adds to the existing body of intellectual property in this therapeutic area.

Key Players and Technologies

• Innovator Companies: Major pharmaceutical companies, including Pfizer Inc., AstraZeneca, Novartis, Roche, and others, hold patents on various EGFR inhibitors. These patents typically cover specific chemical entities, formulations, and methods of use.
• Generic Competition: As patents expire, generic versions of established EGFR inhibitors enter the market. This can significantly impact pricing and market dynamics. Brazil has a well-established generic pharmaceutical industry.
• Research and Development: Ongoing research focuses on developing next-generation EGFR inhibitors with improved efficacy, reduced resistance, and better safety profiles. This includes targeting specific EGFR mutations and developing combination therapies.

Patentability Considerations for BR112019025636 in Brazil

The patentability of BR112019025636 would have been assessed by the Brazilian National Institute of Industrial Property (INPI) based on criteria such as novelty, inventive step, and industrial applicability.

• Novelty: The claimed pyrazolo[1,5-a]pyrimidine derivatives must not have been previously disclosed in the prior art.
• Inventive Step: The invention must not be obvious to a person skilled in the art, considering the existing knowledge in the field of EGFR inhibitors. The specific structural modifications and demonstrated biological activity would be crucial in establishing inventive step.
• Industrial Applicability: The invention must be capable of being made or used in any kind of industry. This is generally met by pharmaceutical compounds and their therapeutic applications.

Potential for Freedom-to-Operate Issues

Companies looking to develop or market EGFR inhibitors in Brazil would need to conduct thorough freedom-to-operate (FTO) analyses to ensure their products do not infringe on existing patents, including BR112019025636. This involves:

• Claim Mapping: Comparing the claims of BR112019025636 with the structure and intended use of a competitor's product.
• Prior Art Analysis: Evaluating the validity of the patent's claims based on existing scientific literature and patents.

The broad definition of Formula I in Claim 1 suggests a wide potential scope, necessitating careful FTO assessments for any compound that falls within its structural parameters.

What are the implications of this patent for the pharmaceutical market?

The grant of BR112019025636 has several implications for the pharmaceutical market, particularly in the oncology sector.

Market Exclusivity and Competition

• Market Exclusivity: The patent grants Pfizer Inc. a period of market exclusivity for the claimed compounds and their uses in Brazil. This exclusivity period is typically 20 years from the filing date, subject to patent term extensions in certain circumstances.
• Competitive Landscape: During the patent term, other companies are generally precluded from making, using, selling, or importing the patented compounds or products for which the patent is granted. This protects Pfizer's investment in R&D and allows for potential market leadership.
• Generic Entry: Upon patent expiry, generic manufacturers can seek regulatory approval to market bioequivalent versions of the drugs, leading to increased competition and potentially lower prices.

R&D and Investment Decisions

• Pipeline Development: The patent signals Pfizer's ongoing interest and investment in the field of EGFR inhibitors. This may influence R&D strategies of competitors, potentially leading to the development of alternative targets or different chemical classes of inhibitors to circumvent the patent.
• Investment Strategy: Investors analyzing the oncology market would consider the patent landscape, including patents like BR112019025636, when making decisions regarding R&D funding, acquisitions, or partnerships. The strength and breadth of the claims are critical factors in assessing the commercial potential and longevity of the protected technology.

Therapeutic Advancements

• Treatment Options: The patent aims to expand treatment options for cancer patients by introducing novel EGFR inhibitors. If successful, these compounds could offer improved therapeutic outcomes compared to existing treatments.
• Resistance Mechanisms: The development of new inhibitors is also driven by the need to overcome resistance mechanisms that emerge with current therapies. The specific design of these pyrazolo[1,5-a]pyrimidine derivatives may offer advantages in addressing such resistance.

The broad scope of the compound claims in BR112019025636, coupled with its defined therapeutic uses, positions it as a significant patent in the Brazilian oncology market. Companies operating in this space must carefully assess its claims and potential impact on their R&D and commercial strategies.

Key Takeaways

• Patent Scope: BR112019025636 broadly protects pyrazolo[1,5-a]pyrimidine derivatives as EGFR inhibitors, encompassing a wide chemical genus and specific therapeutic applications in cancer treatment.
• Claim Structure: The patent features a strong independent claim (Claim 1) defining the core compound structure with extensive substituent variations, supported by dependent claims for specific embodiments and pharmaceutical compositions.
• Market Impact: The patent grants Pfizer Inc. market exclusivity for these EGFR inhibitors in Brazil, influencing competitive dynamics, R&D strategies, and investment decisions within the oncology pharmaceutical sector.
• Freedom-to-Operate: Companies seeking to enter the Brazilian EGFR inhibitor market must conduct thorough FTO analyses to navigate the patent's broad claim scope.

Frequently Asked Questions

• What specific types of cancer are targeted by the compounds claimed in BR112019025636? The patent claims methods for treating various cancers, including but not limited to, non-small cell lung cancer (NSCLC), colorectal cancer, pancreatic cancer, and head and neck cancers. The core indication is cancer associated with aberrant EGFR signaling.
• Does BR112019025636 cover all pyrazolo[1,5-a]pyrimidine derivatives, or are there specific limitations? The patent covers compounds of Formula I as defined in Claim 1, which includes a broad pyrazolo[1,5-a]pyrimidine scaffold with extensive possibilities for substituents. While broad, the specific definitions of the variables (R1-R2858) and their allowed chemical groups define the precise scope of coverage.
• What is the expected expiration date of patent BR112019025636 in Brazil? The patent was filed on November 30, 2018. Under Brazilian patent law, patents are generally granted for 20 years from the filing date. Therefore, the patent is expected to expire around November 30, 2038, though potential extensions for pharmaceutical products may apply.
• Are there any approved drugs on the market in Brazil that are directly covered by the claims of BR112019025636? As of the current analysis, it is not possible to definitively state whether any specific approved drugs in Brazil are directly covered by BR112019025636 without a detailed claim mapping exercise against approved drug structures and their claims. However, the patent is likely related to the development of novel EGFR inhibitors.
• What actions could a competitor take if they wish to develop a similar compound in Brazil before the patent's expiration? A competitor could explore developing compounds that fall outside the scope of the patent's claims, seek a license from Pfizer Inc., or challenge the validity of the patent through legal proceedings, although the latter is complex and resource-intensive.

Citations

[1] Pfizer Inc. (2019). DERIVADOS DE PIRAZOLO[1,5-a]PIRIMIDINA COM ATIVIDADE INIBIDORA DE EGFR E USOS TERAPÊUTICOS. Brazilian Patent BR112019025636.