PATENT CLAIM ANALYSIS

Application Number: 15905427
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-06
Patent Classification: ["514", "210000"]

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 of Factor D described herein reduce the excessive activation of complement.

Claim (Index 1):
A method for the treatment of a disorder mediated by complement factor D, comprising administering an effective amount to a host in need thereof a compound of the formula or a pharmaceutically acceptable salt thereof, wherein:\n Q 1  is C(R 1 R 1\u2032 ); \n Q 2  is C(R 2 R 2\u2032 ); \n Q 3  is C(R 3 R 3\u2032 ); \n X 1  is N and X 2  is CH; \n R 1 , R 1\u2032 , R 2 , R 2\u2032 , R 3 , and R 3\u2032  are independently chosen from hydrogen, halogen, hydroxyl, nitro, cyano, amino, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 1 -C 6 alkoxy, C 2 -C 6 alkanoyl, C 1 -C 6 thioalkyl, hydroxyC 1 -C 6 alkyl, aminoC 1 -C 6 alkyl, \u2014C 0 -C 4 alkylNR 9 R 10 , \u2014C(O)OR 9 , \u2014OC(O)R 9 , \u2014NR 9 C(O)R 10 , \u2014C(O)NR 9 R 10 , \u2014OC(O)NR 9 R 10 , \u2014NR 9 C(O)OR 10 , C 1 -C 2 haloalkyl, and C 1 -C 2 haloalkoxy; \n R 9  and R 10  are independently chosen 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); \n or R 1  and R 2  are linked to form a 3- to 6-membered carbocyclic or aryl ring; \n or R 2  and R 3  are linked to form a 3- to 6-membered carbocyclic ring; \n or R 1  and R 1\u2032 , R 2  and R 2\u2032  or R 3  and R 3\u2032  are linked to form a 3- to 6-membered carbocyclic spiro ring; \n or R 1  and R 1\u2032 , R 2  and R 2\u2032  or R 3  and R 3\u2032  are linked to form a 3- to 6-membered heterocyclic spiro ring; \n each of which ring may be unsubstituted or substituted with 1 or more substituents independently selected from halogen, hydroxyl, cyano, \u2014COOH, C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 1 -C 4 alkoxy, C 2 -C 4 alkanoyl, hydroxyC 1 -C 4 alkyl, (mono- and di-C 1 -C 4 alkylamino)C 0 -C 4 alkyl, \u2014C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl), \u2014O\u2014C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl), C 1 -C 2 haloalkyl, and C 1 -C 2 haloalkoxy; \n or R 1  and R 1\u2032  or R 2  and R 2\u2032  are linked to form a carbonyl group; \n A is a group selected from: \n 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, 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, and 5- to 6-membered heteroaryl; R 8  and R 8\u2032  are independently selected from hydrogen, halogen, hydroxyl, C 1 -C 6 alkyl, \u2014C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl), C 1 -C 6 alkoxy, and (C 1 -C 4 alkylamino)C 0 -C 2 alkyl; or R 8  and R 8\u2032  are taken together to form an oxo group; or R 8  and R 8\u2032  are taken together with the carbon that they are bonded to form a 3-membered carbocyclic ring; 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 ; wherein no more than 2 of X 11 , X 12 , X 13 , and X 14  are N; one of R 12  and R 13  is selected from R 31  and the other of R 12  and R 13  is selected from R 32 ; wherein when A is an indole or indazole and X 12  is N then X 13  is CR 32 ; wherein when A is an indole or indazole and X 13  is N then X 12  is CR 32 ; R 31  is selected 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 , each of which R 31  other than hydrogen, halogen, hydroxyl, nitro, cyano, C 1 -C 2 haloalkyl, and C 1 -C 2 haloalkoxy is unsubstituted or substituted with one or more substituents independently selected from halogen, hydroxyl, nitro, cyano, amino, \u2014COOH, \u2014CONH 2  C 1 -C 2 haloalkyl, and C 1 -C 2 haloalkoxy, and each of which R 31  is also optionally substituted with one substituent selected from phenyl and 4- to 7-membered heterocycle containing 1, 2, or 3 heteroatoms independently selected from N, O, and S; which phenyl or 4- to 7-membered heterocycle is unsubstituted or substituted with one or more substituents independently selected 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), C 1 -C 2 haloalkyl, and C 1 -C 2 haloalkoxy; R 32  is selected from NR 37 R 38 , NR 9 SO 2 R 38 , or N(SO 2 R 9 )CH 2 C(O)R 39 ; R 37  is selected at each occurrence from aryl, heteroaryl, heterocycle, 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)(heteroalkyl), \u2014S(O)(heteroalkyl), \u2014S(O)(O)(aryl), \u2014S(O)(aryl), \u2014S(O)(O)(heteroaryl), \u2014S(O)(heteroaryl), (4- to 7-membered heterocycloalkyl)C 0 -C 4 alkyl having 1, 2, or 3 heteroatoms independently selected from N, O, and S, and (5- or 6-membered saturated or partially unsaturated heterocycle)C 0 -C 4 alkyl having 1, 2, or 3 heteroatoms independently selected from N, O, and S, each of which groups can be optionally substituted with 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, hydroxyC 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, or C 1 -C 2 haloalkoxy; R 38  is selected 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 selected 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 selected from N, O, and S, each of which groups can be optionally substituted with 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, hydroxyC 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, or C 1 -C 2 haloalkoxy; R 39  is a proline amide optionally substituted with 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, hydroxyC 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, or C 1 -C 2 haloalkoxy; R 11  and R 14  are independently selected 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 alkenyl(aryl), C 2 -C 6 alkenyl(cycloalkyl), C 2 -C 6 alkenyl(heterocycle), C 2 -C 6 alkenyl(heteroaryl), C 2 -C 6 alkynyl, C 2 -C 6 alkynyl(aryl), C 2 -C 6 alkynyl(cycloalkyl), C 2 -C 6 alkynyl(heterocycle), C 2 -C 6 alkynyl(heteroaryl), 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; R 21  and R 22  are independently selected 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 selected 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 selected from N, O, and S; R 23  is independently selected from (C 3 -C 7 cycloalkyl)C 0 -C 4 alkyl, (aryl)C 0 -C 4 alkyl, (4- to 7-membered heterocycloalkyl)C 0 -C 4 alkyl having 1, 2, or 3 heteroatoms independently selected 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 selected 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; L is selected from the formulas R 17  is hydrogen, C 1 -C 6 alkyl, or \u2014C 0 -C 4 alkyl(C 3 -C 7 cycloalkyl); R 18  and R 18\u2032  are independently selected from hydrogen, halogen, hydroxymethyl, and methyl; 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), and B is unsubstituted or substituted with one or more substituents independently selected from R 33  and R 34 , and 0 or 1 substituents selected from R 35  and R 36 ; R 33  is independently selected 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 selected 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)NR 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 selected 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 selected from naphthyl, naphthyloxy, indanyl, (4- to 7-membered heterocycloalkyl)C 0 -C 4 alkyl containing 1 or 2 heteroatoms selected from N, O, and S, and bicyclic heterocycle containing 1, 2, or 3 heteroatoms independently selected 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 selected 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; R 36  is independently selected 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 selected from N, O, B, and S, each of which R 36  is unsubstituted or substituted with one or more substituents independently selected 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: 8.0
- Percentile: 88.0
- Lexical Diversity: 1.31915
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15247410', '15247440', '15247424', '15247429', '15905524']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8244110117189584
- 35 USC 102 Novelty (BERT): 0.6398526597397938
- Combined Prediction Score: 0.8059551765210419
- Mean Citation Score: 530.856136
- Max Citation Score: 600.47015
- Similarity Product: 591.6266703414441

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

Dataset: test