PATENT CLAIM ANALYSIS

Application Number: 16006520
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2018-10
Patent Classification: ["514", "063000"]

Abstract:
Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R 12  or R 13  on the A group is an alkyne (R 32 ) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

Claim (Index 1):
A compound of Formula: or a pharmaceutically acceptable salt thereof, wherein:\n R 1 , R 2 , R 2\u2032 , and R 3  are independently chosen from hydrogen, halogen, and C 1 -C 6 alkyl; \n R 4  is chosen from \u2014CHO, \u2014CONH 2 , C 2 -C 6 alkanoyl, hydrogen, \u2014SO 2 NH 2 , \u2014C(CH 2 ) 2 F, \u2014CH(CF 3 )NH 2 , C 1 -C 6 alkyl, \u2014C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl), \u2014C(O)C 0 -C 2 alkyl(C 3 -C 7 cycloalkyl), \n R 5  and R 6  are independently chosen from hydrogen \u2014CHO, \u2014C(O)NH 2 , \u2014C(O)NH(CH 3 ), and C 2 -C 6 alkanoyl; R 8  and R 8\u2032  are hydrogen; one of R 12  and R 13  is chosen from R 31  and the other of R 12  and R 13  is chosen from R 32 : R 31  is chosen from hydrogen, halogen, hydroxyl, nitro, cyano, amino, \u2014COOH, C 1 -C 2 haloalkyl, C 1 -C 2 haloalkoxy, C 1 -C 6 alkyl, \u2014C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl), C 2 -C 6 alkenyl, C 2 -C 6 alkanoyl, C 1 -C 6 alkoxy, C 2 -C 6 alkenyloxy, \u2014C(O)OR 9 , C 1 -C 6 thioalkyl, \u2014C 0 -C 4 alkylNR 9 R 10 , \u2014C(O)NR 9 R 10 , \u2014SO 2 R 9 , \u2014SO 2 NR 9 R 10 , \u2014OC(O)R 9 , and \u2014C(NR 9 )NR 9 R 10 ; R 9  and R 10  are independently chosen at each occurrence from hydrogen and C 1 -C 6 alkyl; R 32  is R 11  and R 14  are hydrogen; R 30  is independently chosen at each occurrence from hydrogen, (phenyl)C 0 -C 4 alkyl, and (5- or 6-membered unsaturated or aromatic heterocycle)C 0 -C 4 alkyl having 1, 2, or 3 heteroatoms independently chosen from N, O, and S; L is R 17  is hydrogen; R 18  and R 18\u2032  are hydrogen; m is 0, 1, 2, or 3; B is \u2014(C 0 -C 4 alkyl)(aryl); \u2014(C 0 -C 4 alkyl)(heteroaryl); or \u2014(C 0 -C 4 alkyl)(biphenyl) each of which B is unsubstituted or substituted with one or more substituents independently chosen from R 33  and R 34 , and 0 or 1 substituents chosen from R 36 ; R 33  is independently chosen from halogen, hydroxyl, \u2014COOH, cyano, C 1 -C 6 alkyl, C 2 -C 6 alkanoyl, C 1 -C 6 alkoxy, \u2014C 0 -C 4 alkylNR 9 R 10 , \u2014SO 2 R 9 , C 1 -C 2 haloalkyl, and C 1 -C 2 haloalkoxy; R 34  is independently chosen from nitro, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, and C 1 -C 6 thioalkyl; and R 36  is independently chosen from (phenyl)C 0 -C 2 alkyl, (phenyl)C 1 -C 2 alkoxy, phenoxy, and 6-membered heteroaryl containing 1, 2, or 3 heteroatoms independently chosen from N, O, B, and S, each of which R 36  is unsubstituted or substituted with one or more substituents independently chosen from halogen, hydroxyl, nitro, cyano, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkanoyl, C 1 -C 6 alkoxy, (mono- and di-C 1 -C 6 alkylamino)C 0 -C 4 alkyl, C 1 -C 6 alkylester, \u2014C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl), \u2014SO 2 R 9 , C 1 -C 2 haloalkyl, and C 1 -C 2 haloalkoxy.

Metadata:
- Claim Count in Document: 1.0
- Percentile: 94.0
- Lexical Diversity: 1.6
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['14631090', '14630959', '15676411', '14631683', '15245712']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8348456016137084
- 35 USC 102 Novelty (BERT): 0.5594384909926087
- Combined Prediction Score: 0.8073048905515984
- Mean Citation Score: 398.378724
- Max Citation Score: 426.23492000000016
- Similarity Product: 327.8668476912595

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