PATENT CLAIM ANALYSIS

Application Number: 15961553
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-10
Patent Classification: ["544", "280000"]

Abstract:
Disclosed are chemical entities of formula I: wherein X, Y, Z, R 1 , R 3 , R 4 , R 5  and R 6  are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of formula I, and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of formula I.

Claim (Index 21):
A chemical entity selected from the group consisting of: TABLE 1.C   compound X R 1 C-1\u2002 H H C-2\u2002 F H C-3\u2002 Cl H C-4\u2002 CH 3 H C-5\u2002 CF 3 H C-6\u2002 CF 2 H H C-7\u2002 CH 2 F H C-8\u2002 CH 2 CH 3 H C-9\u2002 cyclopropyl H C-10 CH 3 O H C-11 CF 3 O H C-12 CHF 2 O H C-13 SCH 3 H C-14 CN H C-15 F F C-16 Cl F C-17 CH 3 F C-18 CF 3 F C-19 CF 2 H F C-20 CH 2 F F C-21 CH 2 CH 3 F C-22 cyclopropyl F C-23 F Cl C-24 Cl Cl C-25 CH 3 Cl C-26 CF 3 Cl C-27 cyclopropyl Cl C-28 F CH 3 C-29 Cl CH 3 C-30 CH 3 CH 3 C-31 CF 3 CH 3 C-32 cyclopropyl CH 3 TABLE 2.C   compound X R 1 R 4 R 5 C-33 CF 3 H CH 3 H C-34 Cl H CH 3 H C-35 CH 3 H CH 3 H C-36 CF 3 H Cl H C-37 Cl H Cl H C-38 CH 3 H Cl H C-39 CF 3 F CH 3 H C-40 Cl F CH 3 H C-41 CH 3 F CH 3 H C-42 CF 3 F Cl H C-43 Cl F Cl H C-44 CH 3 F Cl H C-45 CF 3 H H CH 3 C-46 Cl H H CH 3 C-47 CH 3 H H CH 3 TABLE 3.C   compound X R 2 R 3 C-48 F F H C-49 Cl F H C-50 CH 3 F H C-51 CF 3 F H C-52 F CH 3 H C-53 Cl CH 3 H C-54 CH 3 CH 3 H C-55 CF 3 CH 3 H C-56 F Cl H C-57 Cl Cl H C-58 CH 3 Cl H C-59 CF 3 Cl F C-60 F H F C-61 Cl H F C-62 CH 3 H F C-63 CF 3 H Cl C-64 F H Cl C-65 Cl H Cl C-66 CH 3 H Cl C-67 CF 3 H CH 3 C-68 F H CH 3 C-69 Cl H CH 3 C-70 CH 3 H CH 3 TABLE 4.C   compound X R 1 R 6 C-71 F H CH 3 C-72 Cl H CH 3 C-73 CH 3 H CH 3 C-74 CF 3 H CH 3 C-75 CF 2 H H CH 3 C-76 CH 2 F H CH 3 C-77 OCF 3 H CH 3 C-78 OCF 2 H H CH 3 C-79 CH 2 CH 3 H CH 3 C-80 cyclopropyl H CH 3 C-81 F H F C-82 Cl H F C-83 CH 3 H F C-84 CF 3 H F C-85 CF 2 H H F C-86 CH 2 F H F C-87 OCF 3 H F C-88 OCF 2 H H F C-89 CH 2 CH 3 H F C-90 cyclopropyl H F C-91 F F CH 3 C-92 Cl F CH 3 C-93 CH 3 F CH 3 C-94 CF 3 F CH 3 C-95 F F F C-96 Cl F F C-97 CH 3 F F C-98 CF 3 F F TABLE 5.C   compound X R 1 R 6 C-99\u2002 F H CH 3 C-100 Cl H CH 3 C-101 CH 3 H CH 3 C-102 CF 3 H CH 3 C-103 CF 2 H H CH 3 C-104 CH 2 F H CH 3 C-105 OCF 3 H CH 3 C-106 OCF 2 H H CH 3 C-107 CH 2 CH 3 H CH 3 C-108 cyclopropyl H CH 3 C-109 F H F C-110 Cl H F C-111 CH 3 H F C-112 CF 3 H F C-113 CF 2 H H F C-114 CH 2 F H F C-115 OCF 3 H F C-116 OCF 2 H H F C-117 CH 2 CH 3 H F C-118 cyclopropyl H F C-119 F F CH 3 C-120 Cl F CH 3 C-121 CH 3 F CH 3 C-122 CF 3 F CH 3 C-123 F F F C-124 Cl F F C-125 CH 3 F F C-126 CF 3 F F TABLE 6.C   compound X R 1 R 2 R 3 C-127 CF 3 H H H C-128 CH 3 H H H C-129 F H H H C-130 Cl H H H C-131 OCH 3 H H H C-132 OCF 3 H H H C-133 SCH 3 H H H C-134 CH 2 CH 3 H H H C-135 cyclopropyl H H H C-136 CF 3 F H H C-137 CF 3 H F H C-138 CF 3 H H F C-139 H CF 3 H H C-140 H H CF 3 H C-141 H H H CF 3 TABLE 7.C   compound X R 4 R 6 C-142 CF 3 CH 3 H C-143 CH 3 CH 3 H C-144 CF 3 H F C-145 CH 3 H F C-146 CH 2 CH 3 H F C-147 SCH 3 H F C-148 cyclopropyl H F C-149 OCF 3 H F C-150 OCH 3 H F C-151 CF 3 H CH 3 C-152 CH 3 H CH 3 C-153 CH 2 CH 3 H CH 3 C-154 SCH 3 H CH 3 C-155 cyclopropyl H CH 3 C-156 OCF 3 H CH 3 C-157 OCH 3 H CH 3 TABLE 8.C   compound X R 4 R 6 C-158 CF 3 Cl H C-159 CH 3 Cl H C-160 CF 3 H F C-161 CH 3 H F C-162 CH 2 CH 3 H F C-163 SCH 3 H F C-164 cyclopropyl H F C-165 OCF 3 H F C-166 OCH 3 H F C-167 CF 3 H CH 3 C-168 CH 3 H CH 3 C-169 CH 2 CH 3 H CH 3 C-170 SCH 3 H CH 3 C-171 cyclopropyl H CH 3 C-172 OCF 3 H CH 3 C-173 OCH 3 H CH 3 TABLE 9.C   compound X R 1 C-174 H H C-175 F H C-176 Cl H C-177 CH 3 H C-178 CF 3 H C-179 CF 2 H H C-180 CH 2 F H C-181 CH 2 CH 3 H C-182 cyclopropyl H C-183 CH 3 O H C-184 CF 3 O H C-185 CHF 2 O H C-186 SCH 3 H C-187 CN H C-188 F F C-189 Cl F C-190 CH 3 F C-191 CF 3 F C-192 CF 2 H F C-193 CH 2 F F C-194 CH 2 CH 3 F C-195 cyclopropyl F C-196 F Cl C-197 Cl Cl C-198 CH 3 Cl C-199 CF 3 Cl C-200 cyclopropyl Cl C-201 F CH 3 C-202 Cl CH 3 C-203 CH 3 CH 3 C-204 CF 3 CH 3 C-205 cyclopropyl CH 3 TABLE 10.C   compound X R 2 R 3 C-206 F F H C-207 Cl F H C-208 CH 3 F H C-209 CF 3 F H C-210 F CH 3 H C-211 Cl CH 3 H C-212 CH 3 CH 3 H C-213 CF 3 CH 3 H C-214 F Cl H C-215 Cl Cl H C-216 CH 3 Cl H C-217 CF 3 Cl F C-218 F H F C-219 Cl H F C-220 CH 3 H F C-221 CF 3 H Cl C-222 F H Cl C-223 Cl H Cl C-224 CH 3 H Cl C-225 CF 3 H CH 3 C-226 F H CH 3 C-227 Cl H CH 3 C-228 CH 3 H CH 3 TABLE 11.C   compound X R 4 C-229 CF 3 H C-230 CH 3 H C-231 Cl H C-232 F H C-233 CF 2 H H C-234 OCF 3 H C-235 OCF 2 H H C-236 CH 2 CH 3 H C-237 cyclopropyl H C-238 isopropyl H C-239 CF 3 CH 3 C-240 CH 3 CH 3 C-241 CH 2 CH 3 CH 3 C-242 cyclopropyl CH 3 C-243 isopropyl CH 3 C-244 OCF 3 CH 3 or a pharmaceutically acceptable salt thereof.

Metadata:
- Claim Count in Document: 11.0
- Percentile: 91.0
- Lexical Diversity: 1.72549
- Patent Class: 544.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15428321', '15315812', '14855010', '15548594', '15578460']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.799864449513608
- 35 USC 102 Novelty (BERT): 0.5454871979158349
- Combined Prediction Score: 0.7744267243538308
- Mean Citation Score: 370.752534
- Max Citation Score: 397.77426
- Similarity Product: 332.64899385087494

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 1
- Label 101 Adjusted: 1

Dataset: test