PATENT CLAIM ANALYSIS

Application Number: 16246832
Application Type: Utility
Filing Date: 2019-01
Publication Date: 2019-05
Patent Classification: ["514", "214020"]

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 amino substituent (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, optionally in a pharmaceutically acceptable carrier, wherein:\n the \n ring is q is 0, 1, 2, or 3; r is 1, 2, or 3; A is a group selected from: 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), and \u2014C(O)C 0 -C 2 alkyl(C 3 -C 7 cycloalkyl); R 5  and R 6  are independently selected from \u2014CHO, \u2014C(O)NH 2 , \u2014C(O)NH(CH 3 ), C 2 -C 6 alkanoyl, hydrogen, hydroxyl, halogen, cyano, nitro, \u2014COOH, \u2014SO 2 NH 2 , vinyl, C 1 -C 6 alkyl (including methyl), C 2 -C 6 alkenyl, C 1 -C 6 alkoxy, \u2014C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl), \u2014C(O)C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl), \u2014P(O)(OR 9 ) 2 , \u2014OC(O)R 9 , \u2014C(O)OR 9 , \u2014C(O)N(CH 2 CH 2 R 9 )(R 10 ), \u2014NR 9 C(O)R 10 , phenyl, or 5- to 6-membered heteroaryl; R 7  is hydrogen, C 1 -C 6 alkyl, or \u2014C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl). R 8  and R 8\u2032  are hydrogen; R 9  and R 10  are independently chosen at each occurrence from hydrogen, C 1 -C 6 alkyl, (C 3 -C 7 cycloalkyl)C 0 -C 4 alkyl, \u2014C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl), and \u2014O\u2014C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl); X 11  is N or CR 11 ; X 12  is N or CR 12 ; X 13  is N or CR 13 ; X 14  is N or CR 14 , and wherein no more than two of X 11 , X 12 , X 13 , and X 14  are N; R 11  and R 14  are independently chosen at each occurrence from hydrogen, halogen, hydroxyl, nitro, cyano, \u2014O(PO)(OR 9 ) 2 , \u2014(PO)(OR 9 ) 2 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 2 -C 6 alkanoyl, C 1 -C 6 alkoxy, C 1 -C 6 thioalkyl, \u2014C 0 -C 4 alkyl(mono- and di-C 1 -C 6 alkylamino), \u2014C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl), \u2014C 0 -C 4 alkoxy(C 3 -C 7 cycloalkyl), C 1 -C 2 haloalkyl, and C 1 -C 2 haloalkoxy; 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 32  is NR 9 SO 2 R 38  or NR 37 R 38 ; R 37  is selected from aryl, heteroaryl, hetercycle, alkynyl, hydroxyl, C 1 -C 6 alkoxy, (C 3 -C 7 cycloalkyl)C 0 -C 4 alkyl, (aryl)C 0 -C 4 alkyl, (heterocycle)C 0 -C 4 alkyl, (heteroaryl)C 0 -C 4 alkyl, \u2014C 1 -C 4 alkylOC(O)OC 1 -C 6 alkyl, \u2014C 1 -C 4 alkylOC(O)C 1 -C 6 alkyl, \u2014C 1 -C 4 alkylC(O)OC 1 -C 6 alkyl, \u2014S(O)(O)(alkyl), \u2014S(O)(alkyl), \u2014S(O)(O)(aryl), \u2014S(O)(aryl), \u2014S(O)(O)(heteroaryl), and \u2014S(O)(heteroaryl), each of which R 37  groups can be optionally substituted with one or more substituents independently chosen from halogen, hydroxyl, amino, cyano, \u2014CHO, \u2014COOH, \u2014CONH 2 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, \u2014C 1 -C 6 alkoxy, C 2 -C 6 alkanoyl, C 1 -C 6 alkylester, (mono- and di-C 1 -C 6 alkylamino)C 0 -C 2 alkyl, C 1 -C 2 haloalkyl, hydoxyC 1 -C 6 alkyl, ester, carbamate, urea, sulfonamide, \u2014C 1 -C 6 alkyl(heterocyclo), C 1 -C 6 alkyl(heteroaryl), \u2014C 1 -C 6 alkyl(C 3 -C 7 cycloalkyl), O\u2014C 1 -C 6 alkyl(C 3 -C 7 cycloalkyl), B(OH) 2 , phosphate, phosphonate and C 1 -C 2 haloalkoxy; R 38  is chosen at each occurrence from hydrogen, hydroxyl, cyano, amino, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, (C 3 -C 7 cycloalkyl)C 0 -C 4 alkyl, (phenyl)C 0 -C 4 alkyl, \u2014C 1 -C 4 alkylOC(O)OC 1 -C 6 alkyl, \u2014C 1 -C 4 alkylOC(O)C 1 -C 6 alkyl, \u2014C 1 -C 4 alkylC(O)OC 1 -C 6 alkyl, (4- to 7-membered heterocycloalkyl)C 0 -C 4 alkyl having 1, 2, or 3 heteroatoms independently chosen from N, O, and S, 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, each of which R 38  groups can be optionally substituted with one or more substituents independently chosen from halogen, hydroxyl, amino, cyano, \u2014CHO, \u2014COOH, \u2014CONH 2 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, \u2014C 1 -C 6 alkoxy, C 2 -C 6 alkanoyl, C 1 -C 6 alkylester, (mono- and di-C 1 -C 6 alkylamino)C 0 -C 2 alkyl, C 1 -C 2 haloalkyl, hydoxyC 1 -C 6 alkyl, ester, carbamate, urea, sulfonamide, \u2014C 1 -C 6 alkyl(heterocyclo), C 1 -C 6 alkyl(heteroaryl), \u2014C 1 -C 6 alkyl(C 3 -C 7 cycloalkyl), O\u2014C 1 -C 6 alkyl(C 3 -C 7 cycloalkyl), B(OH) 2 , phosphate, phosphonate and C 1 -C 2 haloalkoxy; R 21  and R 22  are independently chosen at each occurrence from hydrogen, hydroxyl, cyano, amino, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, (C 3 -C 7 cycloalkyl)C 0 -C 4 alkyl, (phenyl)C 0 -C 4 alkyl, \u2014C 1 -C 4 alkylOC(O)OC 1 -C 6 alkyl, \u2014C 1 -C 4 alkylOC(O)C 1 -C 6 alkyl, \u2014C 1 -C 4 alkylC(O)OC 1 -C 6 alkyl, (4- to 7-membered heterocycloalkyl)C 0 -C 4 alkyl having 1, 2, or 3 heteroatoms independently chosen from N, O, and S, 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; R 23  is independently chosen at each occurrence from C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, (aryl)C 0 -C 4 alkyl, (C 3 -C 7 cycloalkyl)C 0 -C 4 alkyl, (phenyl)C 0 -C 4 alkyl, (4- to 7-membered heterocycloalkyl)C 0 -C 4 alkyl having 1, 2, or 3 heteroatoms independently chosen from N, O, and S, 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; R 24  and R 25  are taken together with the nitrogen to which they are attached to form a 4- to 7-membered monocyclic heterocycloalkyl group, or a 6- to 10-membered bicyclic heterocyclic group having fused, spiro, or bridged rings, and each R 24  and R 25  can be optionally substituted; L is R 17  is hydrogen; R 18  and R 18\u2032  are independently chosen from hydrogen, halogen, hydroxymethyl, and methyl; m is 0, 1, 2, or 3; B is a monocyclic or bicyclic carbocyclic; a monocyclic or bicyclic carbocyclic-oxy group; a monocyclic, bicyclic, or tricyclic heterocyclic group having 1, 2, 3, or 4 heteroatoms independently selected from N, O, and S and from 4 to 7 ring atoms per ring; C 2 -C 6 alkenyl; C 2 -C 6 alkynyl; \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 35  and 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, C 1 -C 6 thioalkyl, -JC 3 -C 7 cycloalkyl, \u2014B(OH) 2 , -JC(O)NR 9 R 23 , -JOSO 2 OR 21 , \u2014C(O)(CH 2 ) 1-4 S(O)R 21 , \u2014O(CH 2 ) 1-4 S(O)NR 21 R 22 , -JOP(O)(OR 21 )(OR 22 ), -JP(O)(OR 21 )(OR 22 ), -JOP(O)(OR 21 )R 22 , -JP(O)(OR 21 )R 22 , -JOP(O)R 21 R 22 , -JP(O)R 21 R 22 , -JSP(O)(OR 21 )(OR 22 ), -JSP(O)(OR 21 )(R 22 ), -JSP(O)(R 21 )(R 22 ), -JNR 9 P(O)(NHR 21 )(NHR 22 ) -JNR 9 P(O)(OR 21 )(NHR 22 ), -JNR 9 P(O)(OR 21 )(OR 22 ), -JC(S)R 21 , -JNR 21 SO 2 R 22 , -JNR 9 S(O)NR 10 R 22 , -JNR 9 SO 2 NR 10 R 22 , -JSO 2 NR 9 COR 22 , -JSO 2 NR 9 CONR 21 R 22 , -JNR 21 SO 2 R 22 , -JC(O)NR 21 SO 2 R 22 , -JC(NH 2 )NR 22 , -JC(NH 2 )NR 9 S(O) 2 R 22 , -JOC(O)NR 21 R 22 , -JNR 21 C(O)OR 22 , -JNR 21 OC(O)R 22 , \u2014(CH 2 ) 1-4 C(O)NR 21 R 22 , -JC(O)R 24 R 25 , -JNR 9 C(O)R 21 , -JC(O)R 21 , -JNR 9 C(O)NR 10 R 22 , \u2014CCR 21 , \u2014(CH 2 ) 1-4 OC(O)R 21 , and -JC(O)OR 23 ; each of which R 34  may be unsubstituted or substituted with one or more substituents independently chosen from halogen, hydroxyl, nitro, cyano, amino, oxo, \u2014B(OH) 2 , \u2014Si(CH 3 ) 3 , \u2014COOH, \u2014CONH 2 , \u2014P(O)(OH) 2 , C 1 -C 6 alkyl, \u2014C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl), C 1 -C 6 alkoxy, \u2014C 0 -C 2 alkyl(mono- and di-C 1 -C 4 alkylamino), C 1 -C 6 alkylester, C 1 -C 4 alkylamino, C 1 -C 4 hydroxylalkyl, C 1 -C 2 haloalkyl, and C 1 -C 2 haloalkoxy; R 35  is independently chosen from naphthyl, naphthyloxy, indanyl, (4- to 7-membered heterocycloalkyl)C 0 -C 4 alkyl containing 1 or 2 heteroatoms chosen from N, O, and S, and bicyclic heterocycle containing 1, 2, or 3 heteroatoms independently chosen from N, O, and S, and containing 4- to 7-ring atoms in each ring; each of which R 35  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; and R 36  is independently chosen from tetrazolyl, (phenyl)C 0 -C 2 alkyl, (phenyl)C 1 -C 2 alkoxy, phenoxy, and 5- or 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 , \u2014OSi(CH 3 ) 2 C(CH 3 ) 3 , \u2014Si(CH 3 ) 2 C(CH 3 ) 3 , C 1 -C 2 haloalkyl, and C 1 -C 2 haloalkoxy; and J is independently selected at each occurrence from a covalent bond, C 1 -C 4 alkylene, \u2014OC 1 -C 4 alkylene, C 2 -C 4 alkenylene, and C 2 -C 4 alkynylene.

Metadata:
- Claim Count in Document: 47.0
- Percentile: 99.0
- Lexical Diversity: 1.59259
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['14631312', '15463701', '14630959', '16164632', '14631625']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8103971384127943
- 35 USC 102 Novelty (BERT): 0.5688319442142163
- Combined Prediction Score: 0.7862406189929365
- Mean Citation Score: 461.2075
- Max Citation Score: 468.40335
- Similarity Product: 339.99425038563606

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