PATENT CLAIM ANALYSIS

Application Number: 15777499
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-11
Patent Classification: ["540", "460000"]

Abstract:
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

Claim (Index 2):
A compound of Formula (I\u2032): wherein:\n R 1  and R 2  are each independently H, \u2014(C 1 -C 6 )alkyl, \u2014(C 1 -C 6 )alkyl-OR 23 , \u2014CH 2 CH(OH)CH 2 NH 2 , \u2014CH 2 CH(heterocycloalkyl)CH 2 NH 2 , \u2014CH 2 C(O)NH 2 , \u2014CH 2 C(O)N(H)CH 2 CN, \u2014(C 1 -C 6 )alkyl-C(O)OR 23 , \u2014(C 1 -C 6 )alkyl-NR 21 R 22 , \u2014(C 1 -C 6 )alkyl-C(O)NR 25 R 26 , \u2014(C 1 -C 6 )alkyl-N(R 23 )C(O)(C 1 -C 6 )alkylNR 21 R 22 , \u2014(C 1 -C 6 )alkyl-C(O)N(R 23 )(C 1 -C 6 )alkyl, \u2014(C 1 -C 6 )alkyl-C(O)N(R 23 )(C 1 -C 6 )alkyl-heterocycloalkyl, (C 1 -C 6 )heteroalkyl or optionally substituted heterocycloalkyl; \n R 3  is H, or \u2014(C 1 -C 6 )alkyl; \n R 4  is H, \u2014(C 1 -C 6 )alkyl, \u2014(C 1 -C 6 )alkyl-OH, \u2014(C 3 -C 6 )cycloalkyl, or \u2014C(O)NH 2 ; or R 3  and R 4  are combined to form a heterocycloalkyl ring; \n R 5  is H, or \u2014(C 1 -C 6 )alkyl; or R 4  and R 5  and the carbon atom to which that are attached form a cyclopropyl ring; \n R 6 , R 7 , and R are each independently H, fluoro, hydroxyl, amino, optionally substituted alkyl or heteroalkyl or \u2014(C 1 -C 6 )alkyl; \n R 9  is H, \u2014(C 1 -C 6 )alkyl, \u2014(C 1 -C 6 )haloalkyl, or \u2014(C 3 -C 6 )cycloalkyl; \n R 10  is H, \u2014(C 1 -C 6 )alkyl, \u2014(C 1 -C 6 )haloalkyl, or \u2014(C 3 -C 6 )cycloalkyl; \n or R 9  and R 10  are combined to form a heterocycloalkyl or cycloalkyl ring \n R 11  and R 12  are each independently H, \u2014NH 2 , \u2014(C 1 -C 6 )alkyl, \u2014(C 1 -C 6 )alkyl-OR 23 , \u2014(C 1 -C 6 )alkyl-SR 23 , \u2014(C 1 -C 6 )alkyl-C(O)OR 23 , \u2014(C 1 -C 6 )alkyl-NR 21 R 22 , \u2014(C 1 -C 6 )alkyl-CN, \u2014(C 1 -C 6 )alkyl-C(O)NR 25 R 26 , \u2014(C 1 -C 6 )heteroalkyl-CO 2 H, \u2014(C 1 -C 6 )alkyl-S(O)\u2014(C 1 -C 6 )alkyl, \u2014(C 1 -C 6 )alkyl-N(H)CH\u2550NH, \u2014(C 1 -C 6 )alkyl-C(NH 2 )\u2550NH, \u2014(C 1 -C 6 )alkyl-N(H)C(NH)NH 2 , \u2014(C 1 -C 6 )alkyl-N(H)SO 2 NR 25 R 26 , \u2014(C 1 -C 6 )alkyl-N(H)\u2014C(O)NR 25 R 26 , (C 1 -C 6 )alkyl-heterocycloalkyl, optionally substituted \u2014(C 1 -C 6 )alkyl-N(H)heterocycloalkyl, or \u2014(C 1 -C 6 )alkyl-heteroaryl; or R 11  and R 18  are combined to form an optionally substituted heterocycloalkyl ring, and R 12  is H; \n R 15 , R 16 , R 17 , and R 18  are each independently H, \u2014(C 1 -C 6 )alkyl, \u2014(C 3 -C 6 )cycloalkyl, \u2014(C 1 -C 6 )alkyl-OR 23 , \u2014(C 1 -C 6 )alkyl-C(O)OR 23 , or \u2014(C 1 -C 6 )alkyl-NR 21 R 22 ; \n X is optionally substituted \u2014(C 1 -C 6 )alkyl-, \u2014(C 2 -C 6 )alkenyl-, \u2014(C 2 -C 6 )alkynyl, \u2014(C 3 -C 7 )cycloalkyl-, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, \u2014O\u2014(C 1 -C 6 )alkyl-, \u2014N(R 24 )(C 1 -C 6 )alkyl-, \u2014N(R 24 )(C 6 -C 1 )aryl-, or \u2014SO 2 (C 1 -C 6 )alkyl-; \n Y is a bond, optionally substituted \u2014(C 1 -C 6 )alkyl-, \u2014(C 2 -C 6 )alkenyl-, \u2014(C 2 -C 6 )alkynyl, \u2014(C 1 -C 6 )alkyl-N(R 24 )(C 1 -C 6 )alkyl-, \u2014O\u2014(C 1 -C 6 )alkyl-, \u2014O(C 1 -C 6 )aryl-, \u2014N(R 24 )(C 1 -C 6 )alkyl-, \u2014N(R 24 )SO 2 (C 1 -C 6 )alkyl-, \u2014N(R 24 )C(O)(C 1 -C 6 )alkyl-, \u2014C(O)(C 1 -C 6 )alkyl-, \u2014S(C 1 -C 6 )alkyl-, \u2014SO 2 (C 1 -C 6 )alkyl-, \u2014C(O)NH(C 1 -C 6 )alkyl-, \u2014(C 3 -C 7 )cycloalkyl-, optionally substituted \u2014C(O)N(R 24 )aryl-, optionally substituted \u2014N(R 24 )C(O)aryl-, optionally substituted \u2014N(R 24 )SO 2 aryl-, optionally substituted aryl, or optionally substituted heteroaryl; \n Z is H, halogen, \u2014NH 2 , \u2014CN, \u2014CF 3 , \u2014CO 2 H, \u2014(C 1 -C 12 )alkyl, \u2014(C 2 -C 12 )alkenyl, \u2014(C 2 -C 12 )alkynyl, \u2014C(O)NR 25 R 26 , \u2014O\u2014(C 1 -C 12 )alkyl, \u2014N(R 24 )(C 1 -C 12 )alkyl, \u2014N(R 24 )C(O)(C 1 -C 12 )alkyl, optionally substituted \u2014(C 3 -C 7 )cycloalkyl, \u2014(C 1 -C 6 )alkyl-heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; \n each R 21  and R 22  is independently H, \u2014(C 1 -C 6 )alkyl, \u2014(C 1 -C 6 )heteroalkyl, \u2014(C 1 -C 6 )alkyl-CO 2 H, \u2014C(O)(C 1 -C 6 )alkyl, \u2014C(O)O(C 1 -C 6 )alkyl, \u2014C(O)O(C 1 -C 6 )haloalkyl, \u2014C(\u2550NH)(C 1 -C 6 )alkyl, \u2014C(\u2550NH)N(R 31 ) 2 , \u2014C(O)N(R 31 ) 2 , or \u2014SO 2 N(R 31 ) 2 ; or R 21  and R 22  and the nitrogen atom to which that are attached form a heterocycloalkyl ring; \n each R 31  is independently H or \u2014(C 1 -C 6 )alkyl; or two R 31  and the nitrogen atom to which that are attached form a heterocycloalkyl ring; \n each R 23  is independently H or \u2014(C 1 -C 6 )alkyl; \n each R 24  is independently H or \u2014(C 1 -C 6 )alkyl; \n each R 25  and R 26  is independently H or optionally substituted \u2014(C 1 -C 6 )alkyl; or R 25  and R 26  and the nitrogen atom to which that are attached form a heterocycloalkyl ring; \n each R 27  is independently halogen, \u2014NR 23 R 24 , \u2014NC(O)R 23 , \u2014NC(O)NR 23 R 24 ), nitro, hydroxyl, optionally substituted \u2014(C 1 -C 6 )alkyl, optionally substituted \u2014(C 1 -C 6 )heteroalkyl, \u2014(C 1 -C 6 )alkoxy, \u2014C(O)(C 1 -C 6 )alkyl, or \u2014S(O) 2 (C 1 -C 6 )alkyl; \n each R 28  is independently halogen, \u2014NR 23 R 24 , \u2014NC(O)R 23 , \u2014NC(O)NR 23 R 24 ), nitro, hydroxyl, optionally substituted \u2014(C 1 -C 6 )alkyl, optionally substituted \u2014(C 1 -C 6 )heteroalkyl, \u2014(C 1 -C 6 )alkoxy, \u2014C(O)(C 1 -C 6 )alkyl, or \u2014S(O) 2 (C 1 -C 6 )alkyl; \n p is 0, 1, or 2; and \n q is 0, 1, or 2; \n or a pharmaceutically acceptable salt, solvate, or prodrug thereof.

Metadata:
- Claim Count in Document: 59.0
- Percentile: 93.0
- Lexical Diversity: 1.29545
- Patent Class: 540.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15312614', '14086908', '15777201', '13460524', '15950683']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7336495225874834
- 35 USC 102 Novelty (BERT): 0.5390498850742007
- Combined Prediction Score: 0.7141895588361552
- Mean Citation Score: 342.3761140000001
- Max Citation Score: 371.89584
- Similarity Product: 260.2113067910385

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 0
- Claim Label 112: 0
- Combined Label: 1
- Label 101 Adjusted: 1

Dataset: test