PATENT CLAIM ANALYSIS

Application Number: 15775871
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-11
Patent Classification: ["514", "080000"]

Abstract:
The present invention relates to Spirocyclic Pyridotriazine Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R 1 , R 2  and R 16  are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Pyridotriazine Derivative, and methods of using the Spirocyclic Pyridotriazine Derivatives for treating or preventing HIV infection in a subject.

Claim (Index 1):
A compound having the formula: or a pharmaceutically acceptable salt or prodrug thereof, wherein:\n A is \u2014NHC(O)\u2014 or 5 or 6-membered monocyclic heteroaryl; \n B is 3 to 8-membered heterocycloalkyl, which may be optionally substituted with one or more groups, each independently selected from R 6 ; \n X is C 1 -C 3  alkylene; \n Y is \u2014CH 2 \u2014, \u2014CH(R 6 )\u2014 or \u2014N(R 3 )\u2014; \n R is H or benzyl; \n R 1  is selected from hours, C 1 -C 6  alkyl, C 3 -C 7  cycloalkyl, \u2014(C 1 -C 4  alkylene)-O\u2014(C 1 -C 6  alkyl), \u2014(C 1 -C 4  alkylene)\u2014S\u2014(C 1 -C 6  alkyl), \u2014(C 1 -C 4  alkylene)\u2014SO 2 \u2014(C 1 -C 6  alkyl), \u2014(C 1 -C 4  alkylene)\u2014N\u2014(C 1 -C 6  alkyl) 2 , \u2014(C 1 -C 6  alkylene) m \u2014Z\u2014(C 1 -C 3  alkylene) m R 11 , C 1 -C 6  haloalkyl, C 1 -C 6  hydroxyalkyl, phenyl, 3 to 8-membered monocyclic heterocycloalkyl and 5 or 6-membered monocyclic heteroaryl; \n R 2  represents up to 3 optional substitutents, each independently selected from halo, C 1 -C 6  alkyl, \u2014O\u2014(C 1 -C 6  alkyl) and C 1 -C 6  haloalkyl; \n R 3  is selected from H, C 1 -C 6  alkyl, \u2014SO 2 R 4 , \u2014C(O)R 4 , \u2014(C 1 -C 6  alkylene) p \u2014C(O)N(R 5 ) 2 , \u2014(C 2 -C 4  alkylene)\u2014O\u2014(C 1 -C 6  alkyl), \u2014(C 2 -C 4  alkylene)\u2014S\u2014(C 1 -C 6  alkyl), \u2014(C 2 -C 4  alkylene)\u2014SO 2 \u2014(C 1 -C 6  alkyl), \u2014(C 2 -C 4  alkylene)\u2014N\u2014(C 1 -C 6  alkyl) 2 , \u2014(C 1 -C 6  alkylene) m \u2014Z\u2014(C 1 -C 3  alkylene) m \u2014R 11 , C 3 -C 7  cycloalkyl, phenyl, 4 to 8-membered monocyclic heterocycloalkyl or 6-membered monocyclic heteroaryl and 8 to 10-membered bicyclic heteroaryl; \n each occurrence of R 4  is independently selected from H, C 1 -C 6  alkyl, C 1 -C 6  haloalkyl, C 3 -C 7  cycloalkyl, phenyl, 3 to 8-membered monocyclic heterocycloalkyl or 6-membered monocyclic heteroaryl and 8 to 10-membered bicyclic heteroaryl, wherein said C 3 -C 7  cycloalkyl group, said phenyl group, said 3 to 8-membered monocyclic heteroaryl group, said 6-membered monocyclic heteroaryl group and said 8 to 10-membered bicyclic heteroaryl group may be optionally substituted with one or more groups, each independently selected from R 6 ; \n each occurrence of R 5  is independently selected from hours, C 1 -C 6  alkyl, C 3 -C 7  cycloalkyl, \u2014(C 1 -C 6  alkylene)\u2014N(R 7 ) 2 , C 1 -C 6  haloalkyl, \u2014C(O)O(C 1 -C 6  alkyl), \u2014(C 1 -C 6  alkylene) m \u2014Z\u2014(C 1 -C 3  alkylene) m \u2014R 11 , \u2014(C 1 -C 6  alkylene) p \u2014R 8  and \u2014(C 1 -C 6  alkylene)\u2014O\u2014(C 1 -C 6  alkyl); \n each occurrence of R 6  is independently selected from halo, C 1 -C 6  alkyl, C 1 -C 6  haloalkyl, \u2014(C 1 -C 6  alkylene) m \u2014Z\u2014(C 1 -C 3  alkylene) m \u2014R 11 , \u2014N(R 20 ) 2 , 3 to 8-membered monocyclic heterocycloalkyl, 6 to 10-membered bicyclic heterocycloalkyl, \u2014O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 6 -C 10  aryl), \u2014O\u2014(C 1 -C 6  alkylene)\u2014O\u2014(C 1 -C 6  alkyl), \u2014O\u2014(C 1 -C 6  haloalkyl), \u2014O\u2014(C 1 -C 6  alkylene)\u2014O\u2014(C 1 -C 6  alkylene)\u2014O\u2014(C 1 -C 6  alkyl), \u2014S(O) 2 (C 1 -C 6  alkyl), \u2014NHS(O) 2 \u2014(C 1 -C 6  alkyl), \u2014S(O) 2 NH\u2014(C 1 -C 6  alkyl), \u2014OC(O)\u2014(C 1 -C 6  haloalkyl), \u2014(C 1 -C 6  alkylene) p \u2014C(O)O\u2014(C 1 -C 6  alkyl), \u2014(C 1 -C 6  alkylene) p \u2014C(O)\u2014(C 1 -C 6  alkyl), \u2014(C 1 -C 6  alkylene) p \u2014C(O)N(R 7 ) 2 , C 1 -C 6  hydroxyalkyl, \u2014P(O)(OR 9 ) 2 , and \u2014CN; \n each occurrence of R 7  is independently selected from hours, C 1 -C 6  alkyl, C 3 -C 7  cycloalkyl, C 1 -C 6  haloalkyl, \u2014C(O)O(C 1 -C 6  alkyl), \u2014(C 1 -C 6  alkylene) m \u2014Z\u2014(C 1 -C 3  alkylene) m \u2014R 11 , \u2014(C 1 -C 6  alkylene) p \u2014R 8  and \u2014(C 1 -C 6  alkylene)\u2014O\u2014(C 1 -C 6  alkyl); \n each occurrence of R 8  is independently selected from hours, C 1 -C 6  alkyl, C 3 -C 7  cycloalkyl, 5 or 6-membered monocyclic heteroaryl and 3 to 8-membered monocyclic heterocycloalkyl; \n each occurrence of R 9  is independently selected from hours, C 1 -C 6  alkyl and \u2014(C 1 -C 6  alkylene) m \u2014Z\u2014(C 1 -C 3  alkylene) m \u2014R 11 ; \n R 10  is selected from hours, C 1 -C 6  alkyl, C 3 -C 7  cycloalkyl and \u2014(C 1 -C 4  alkylene)\u2014O\u2014(C 1 -C 6  alkyl); \n each occurrence of R 11  is independently selected from \u2014P(O)(\u2014OR 18 ) 2 , \n each occurrence of R 12  is independently selected from hours, C 1 -C 6  alkyl, C 3 -C 7  cycloalkyl, phenyl or benzyl, wherein said C 1 -C 6  alkyl may be optionally substituted with a group selected from halo, \u2014OR 16 , \u2014SR 16 , guanidino, \u2014N(R 16 ) 2 , \u2014C(O)OR 16 , \u2014C(O)N(R 16 ) 2 , \u2014NHC(O)R 16 , 5- or 6-membered monocyclic heteroaryl and 9- or 10-membered bicyclic heteroaryl, and wherein said phenyl group and said benzyl group may be optionally substituted with up to 2 groups, each independently selected from C 1 -C 6  alkyl, halo and \u2014OR 16 ;\n each occurrence of R 13  is independently selected from hours, C 1 -C 6  alkyl, C 3 -C 7  cycloalkyl, phenyl or benzyl, wherein said C 1 -C 6  alkyl may be optionally substituted with a group selected from halo, \u2014OR 16 , \u2014SR 16 , guanidino, \u2014N(R 16 ) 2 , \u2014C(O)OR 16 , \u2014C(O)N(R 16 ) 2 , \u2014NHC(O)R 16 , 5- or 6-membered monocyclic heteroaryl and 9- or 10-membered bicyclic heteroaryl, and wherein said phenyl group and said benzyl group may be optionally substituted with up to 2 groups, each independently selected from C 1 -C 6  alkyl, halo and \u2014OR 16 ; \n each occurrence of R 14  is independently selected from hours, C 1 -C 20  alkyl, C 2 -C 20  alkenyl, \u2014(C 1 -C 3  alkylene) m \u2014(C 3 -C 7  cycloalkyl), \u2014(C 1 -C 3  alkylene) m \u2014(C 6 -C 10  aryl) or \u2014(C 1 -C 3  alkylene) m -adamantyl, wherein said C 1 -C 20  alkyl group, said C 2 -C 20  alkenyl group, said C 6 -C 10  aryl group and said adamantyl group may be optionally substituted with up to three groups, each independently selected from halo, \u2014OR 16 , \u2014C(O)OR 16 , CN, NO 2 , C 1 -C 6  haloalkyl, C 1 -C 6  hydroxyalkyl, C 3 -C 7  cycloalkyl, C 6 -C 10  aryl, 5- or 6-membered monocyclic heteroaryl, 9- or 10-membered bicyclic heteroaryl, \u2014N(R 16 ) 2 , \u2014C(O)N(R 16 ) 2 \u2014SR 16 , \u2014S(O)R 16 , \u2014S(O) 2 R 16 , \u2014S(O) 2 N(R 16 ) 2 , \u2014NHC(O)R 16 , \u2014NHC(O)OR 16  and \u2014NHC(O)N(R 16 ) 2 ; \n R 15  is hours, C 6 -C 10  aryl, 5- or 6-membered monocyclic heteroaryl or 9- or 10-membered bicyclic heteroaryl, wherein said C 6 -C 10  aryl group, said 5- or 6-membered monocyclic heteroaryl group and said 9- or 10-membered bicyclic heteroaryl group may be optionally substituted with R 17 ; \n each occurrence of R 16  is independently hours, C 1 -C 10  alkyl, C 1 -C 6  haloalkyl, C 1 -C 6  hydroxyalkyl, \u2014(C 1 -C 3  alkylene) m  \u2014(C 3 -C 7  cycloalkyl), \u2014(C 1 -C 3  alkylene) m \u2014(C 6 -C 10  aryl), \u2014(C 1 -C 3  alkylene) m -(4 to 7-membered heterocycloalkyl), \u2014(C 1 -C 3  alkylene) m -(5- or 6-membered monocyclic heteroaryl) or \u2014(C 1 -C 3  alkylene) m -(9- or 10-membered bicyclic heteroaryl), wherein said C 3 -C 7  cycloalkyl group, said C 6 -C 10  aryl group, said 4 to 7-membered heterocycloalkyl group, said -5- or 6-membered monocyclic heteroaryl group or said 9- or 10-membered bicyclic heteroaryl group may be optionally substituted with R 17 ; \n R 17  represents from one to five substituent groups, each independently selected from C 1 -C 6  alkyl, halo, \u2014OR 19 , \u2014SR 19 , C l -C 6  haloalkyl, C 1 -C 6  hydroxyalkyl, \u2014O\u2014(C 1 -C 6  haloalkyl), \u2014CN, \u2014NO 2 , \u2014N(R 19 ) 2 , \u2014C(O)OR 19 , \u2014C(O)N(R 19 ) 2  and \u2014NHC(O)R 19 ; \n each occurence of R 18  is independently selected from hours, C 1 -C 6  alkyl, C 6 -C 10  aryl, \u2014(C 1 -C 6  alkylene)\u2014O\u2014(C 1 -C 20  alkyl), \u2014(C 1 -C 6  alkylene)\u2014O\u2014C(O)\u2014R 16 , and \u2014(C 1 -C 6  alkylene)\u2014O\u2014C(O)\u2014O\u2014R 16 ; \n each occurrence of R 19  is independently hours, C 1 -C 10  alkyl, C 1 -C 6  haloalkyl, C 1 -C 6  hydroxyalkyl, \u2014(C 1 -C 3  alkylene) m \u2014(C 3 -C 7  cycloalkyl), \u2014(C 1 -C 3  alkylene) m \u2014(C 6 -C 10  aryl), \u2014(C 1 -C 3  alkylene) m -(4 to 7-membered heterocycloalkyl), \u2014(C 1 -C 3  alkylene) m -(5- or 6-membered monocyclic heteroaryl) or \u2014(C 1 -C 3  alkylene) m -(9- or 10-membered bicyclic heteroaryl); \n each occurence of R 20  is independently selected from hours, C 1 -C 6  alkyl and \u2014(C 1 -C 6  alkylene) m \u2014Z\u2014(C 1 -C 3  alkylene) m \u2014R 11 ; \n each occurrence of Z is independently selected from a bond, \u2014O\u2014 or \u2014N(R 9 )\u2014; \n each occurrence of m is independently 0 or 1; \n n is 1 or 2; and \n each occurrence of p is independently 0 or 1, \n such that at least one occurrence of R 11  must be present in the compound of formula (I), \n and provided that the compound of formula (I) is other than:

Metadata:
- Claim Count in Document: 8.0
- Percentile: 93.0
- Lexical Diversity: 1.42308
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15775966', '16061369', '15105376', '15560896', '15575433']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8095503027253421
- 35 USC 102 Novelty (BERT): 0.5951235635718978
- Combined Prediction Score: 0.7881076288099977
- Mean Citation Score: 452.614154
- Max Citation Score: 491.0582
- Similarity Product: 464.3792464010477

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

Dataset: test