PATENT CLAIM ANALYSIS

Application Number: 16036670
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2019-05
Patent Classification: ["514", "050000"]

Abstract:
Compounds, compositions, and methods of treatment and prevention of HIV infection are disclosed. The compounds are pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidine JAK inhibitors. Combinations of these JAK inhibitors and additional antiretroviral compounds, such as NRTI, NNRTI, integrase inhibitors, entry inhibitors, protease inhibitors, and the like, are also disclosed. In one embodiment, the combinations include a combination of adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, optionally in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog. This combination has the potential to eliminate the presence of HIV in an infected patient.

Claim (Index 1):
A method for treating an HIV infection, comprising administering to a patient in need thereof an effective antiviral amount of a compound of Formula B: including pharmaceutically acceptable salt forms or prodrugs thereof, wherein:\n A 1  and A 2  are independently selected from C and N; \n T, U, and V are independently selected from O, S, N, CR 5 , and NR 6 ; \n wherein the 5-membered ring formed by A 1 , A 2 , U, T, and V is aromatic; \n X is N or CR 4 ; \n Y is C 1-8  alkylene, C 2-8  alkenylene, C 2-8  alkynylene, (CR 11 R 12 ) p \u2014(C 3-10  cycloalkylene)-(CR 11 R 12 ) q , (CR 11 R 12 ) p -(arylene)-(CR 11 R 12 ) q , (CR 11 R 12 ) p \u2014(C 1-10  heterocycloalkylene)-(CR 11 R 12 ) q , (CR 11 R 12 ) p -(heteroarylene)-(CR 11 R 12 ) q , (CR 11 R 12 ) p O(CR 11 R 12 ) q , (CR 11 R 12 ) p S(CR 11 R 12 ) q , (CR 11 R 12 ) p C(O)(CR 11 R 12 ) q , (CR 11 R 12 ) p C(O)NR c (CR 11 R 12 ) q , (CR 11 R 12 ) p C(O)O(CR 11 R 12 ) q , (CR 11 R 12 ) p OC(O)(CR 11 R 12 ) q , (CR 11 R 12 ) p OC(O)NR c (CR 11 R 12 ) q , (CR 11 R 12 ) p NR c (CR 11 R 12 ) q  (CR 11 R 12 ) p NR c C(O)NR d (CR 11 R 12 ) q , (CR 11 R 12 ) p S(O)(CR 11 R 12 ) q , (CR 11 R 12 ) p S(O)NR c (CR 11 R 12 ) q , (CR 11 R 12 ) p S(O) 2 (CR 11 R 12 ) q , or (CR 11 R 12 ) p S(O) 2 NR(CR 11 R 12 ) q , wherein said C 1-8  alkylene, C 2-8  alkenylene, C 2-8  alkynylene, cycloalkylene, arylene, heterocycloalkylene, or heteroarylene, is optionally substituted with 1, 2, or 3 substituents independently selected from -D 1 -D 2 -D 3 -D 4 ; \n Z is H, halo, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, C 1-4  haloalkyl, halosulfanyl, C 1-4  hydroxyalkyl, C 1-4  cyanoalkyl, \u2550C\u2014R i , \u2550N\u2014R i , Cy 1 , CN, NO 2 , OR a , SR a , C(O)R b , C(O)NR c R d , C(O)OR a , OC(O)R b , OC(O)NR c R d , NR c R d , NR c C(O)R b , NR c C(O)NR c R d , NR c C(O)OR a , C(\u2550NR i )NR c R d , NR c C(\u2550NR i )NR c R d , S(O)R b , S(O)NR c R d , S(O) 2 R b , NR c S(O) 2 R b , C(\u2550NOH)R b , C(\u2550NO(C 1-6 alkyl)R b , and S(O) 2 NR c R d , wherein said C 1-8  alkyl, C 2-8  alkenyl, or C 2-8  alkynyl, is optionally substituted with 1, 2, 3, 4, 5, or 6 substituents independently selected from halo, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, C 1-4  haloalkyl, halosulfanyl, C 1-4  hydroxyalkyl, C 1-4  cyanoalkyl, Cy 1 , CN, N 2 , OR a , SR a , C(O)R b , C(O)NR c R d , C(O)OR a , OC(O)R b , OC(O)NR c R d , NR c R d , NR c C(O)R b , NR c C(O)NR c R d , NR c C(O)OR a , C(\u2550NR i )NR c R d , NR c C(\u2550NR i )NR c R d , S(O)R b , S(O)NR c R d , S(O) 2 R b , NR c S(O) 2 R b , C(\u2550NOH)R b , C(\u2550NO(C 1-6  alkyl))R b , and S(O) 2 NR c R d ; \n wherein when Z is H, n is 1; \n or the \u2014(Y) n \u2014Z moiety is taken together with i) A 2  to which the moiety is attached, ii) R 5  or R 6  of either T or V, and iii) the C or N atom to which the R 5  or R 6  of either T or V is attached to form a 4- to 20-membered aryl, cycloalkyl, heteroaryl, or heterocycloalkyl ring fused to the 5-membered ring formed by A 1  A2, U, T, and V, wherein said 4- to 20-membered aryl, cycloalkyl, heteroaryl, or heterocycloalkyl ring is optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from \u2014(W) m -Q; \n W is C 1-8  alkylenyl, C 2-8  alkenylenyl, C 2-8  alkynylenyl, O, S, C(O), C(O)NR c , C(O)O, OC(O), OC(O)NR c\u2032 , NR c\u2032 , NR c\u2032 C(O)NR d\u2032 , S(O), S(O)NR c\u2032 , S(O) 2 , or S(O) 2 NR c\u2032 ; \n Q is H, halo, CN, NO 2 , C 1-8  alkyl, C 2-8  alkenyl, C 2-8  alkynyl, C 1-8  haloalkyl, halosulfanyl, aryl, cycloalkyl, heteroaryl, or heterocycloalkyl, wherein said C 1-8  alkyl, C 2-s  alkenyl, C 2-8  alkynyl, C 1l s haloalkyl, aryl, cycloalkyl, heteroaryl, or heterocycloalkyl is optionally substituted with 1, 2, 3 or 4 substituents independently selected from halo, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, C 1-4  haloalkyl, halosulfanyl, C 1-4  hydroxyalkyl, C 1-4  cyanoalkyl, Cy 2 , CN, NO 2 , OR a\u2032 , SR a\u2032 , C(O)R b\u2032 , C(O)NR c\u2032 R d\u2032 , C(O)OR a\u2032 , OC(O)R b\u2032 , OC(O)NR c\u2032 R d\u2032 , NR c\u2032 R d\u2032 , NR c\u2032 C(O)R b\u2032 , NR c\u2032 C(O)N R c\u2032 R d\u2032 , N R c\u2032 C(O)OR a\u2032 , S(O)R b\u2032 , S(O)N R c\u2032 R d\u2032 , S(O) 2 R b\u2032 , NR c\u2032 S(O) 2 R b\u2032 , and S(O) 2 N R c\u2032 R d\u2032 ; \n Cy 1  and Cy 2  are independently selected from aryl, heteroaryl, cycloalkyl, and heterocycloalkyl, each optionally substituted by 1, 2, 3, 4 or 5 substituents independently selected from halo, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, C 1-4  haloalkyl, halosulfanyl, C 1-4  hydroxyalkyl, C 1-4  cyanoalkyl, CN, NO 2 , OR a\u2033 , SR a\u2033 , C(O)R b\u2033 , C(O)NR c\u2033 R d\u2033 , C(O)OR a\u2033 , OC(O)R b\u2033 , OC(O)N R c\u2033 R d\u2033 , NR c\u2033 R d\u2033 , NR c\u2033 C(O)R b\u2033 , NR c\u2033 C(O)OR a\u2033 , NR c\u2033 S(O)R b\u2033 , NR c\u2033 S(O) 2 R b\u2033 , S(O)R b\u2033 , S(O)NR c\u2033 R d\u2033 , S(O) 2 R b\u2033 , and S(O) 2 NR c\u2033 R d\u2033 ; \n R 1 , R 2 , R 3 , and R 4  are independently selected from H, halo, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, C 1-4  haloalkyl, halosulfanyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, CN, NO 2 , OR 7 , SR 7 , C(O)R 8 , C(O)NR 9 R 10 , C(O)OR 7 OC(O)R 8 , OC(O)NR 9 R 10 , NR 9 R 10 , NR 9 C(O)R 8 , NR c C(O)OR 7 , S(O)R 8 , S(O)NR 9 R 10 , S(O) 2 R 8 , NR 9 S(O) 2 R 8 , and S(O) 2 NR 9 R 10 ; \n R 5  is H, halo, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, C 1-4  haloalkyl, halosulfanyl, CN, NO 2 , OR 7 , SR 7 , C(O)R 8 , C(O)NR 9 R 10 , C(O)OR 7 , OC(O)R 8 , OC(O)NR 9 R 10 , NR 9 R 10 , NR 9 C(O)R 8 , NR 9 C(O)OR 7 , S(O)R 8 , S(O)NR 9 R 10 , S(O) 2 R 8 , NR 9 S(O) 2 R 8 , or S(O) 2 NR 9 R 10 ; \n R 6  is H, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, C 1-4  haloalkyl, OR 7 , C(O)R 8 , C(O)NR 9 R 10 , C(O)OR 7 , S(O)R 8 , S(O)NR 9 R 10 , S(O) 2 R 8 , or S(O) 2 NR 9 R 10 ; \n R 7  is H, C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocycloalkylalkyl; \n R 8  is H, C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocycloalkylalkyl; \n R 9  and R 10  are independently selected from H, C 1-10  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  alkylcarbonyl, arylcarbonyl, C 1-6  alkylsulfonyl, arylsulfonyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl and heterocycloalkylalkyl; \n or R 9  and R 10  together with the N atom to which they are attached form a 4-, 5-, 6- or 7-membered heterocycloalkyl group; \n R 11  and R 12  are independently selected from H and -E 1 -E 2 -E 3 -E 4 ; \n D 1  and E 1  are independently absent or independently selected from C 1-6  alkylene, C 2-6  alkenylene, C 2-6  alkynylene, arylene, cycloalkylene, heteroarylene, and heterocycloalkylene, wherein each of the C 1-6  alkylene, C 2-6  alkenylene, C 2-6  alkynylene, arylene, cycloalkylene, heteroarylene, and heterocycloalkylene is optionally substituted by 1, 2 or 3 substituents independently selected from halo, CN, NO 2 , N 3 , SCN, OH, C 1-6  alkyl, C 1-6  haloalkyl, C 2-8  alkoxyalkyl, C 1-6  alkoxy, C 1-6  haloalkoxy, amino, C 1-6  alkylamino, and C 2-8  dialkylamino; \n D 2  and E 2  are independently absent or independently selected from C 1-6  alkylene, C 2-6  alkenylene, C 2-6  alkynylene, (C 1-6  alkylene) r -O\u2014(C 1-6  alkylene) s , (C 1-6  alkylene) r -S\u2014(C 1-6  alkylene) s , (C 1-6  alkylene) r -NR c \u2014(C 1-6  alkylene) s , (C 1-6  alkylene) r -CO\u2014(C 1-6  alkylene) s , (C 1-6  alkylene) r -COO\u2014(C 1-6  alkylene) s , (C 1-6  alkylene) r -CONR c \u2014(C 1-6  alkylene) s , (C 1-6  alkylene) r -SO\u2014(C 1-6  alkylene) s , (C 1-6  alkylene) r -SO 2 \u2014(C 1-6  alkylene) s , (C 1-6  alkylene) r -SONR c \u2014(C 1-6  alkylene) s , and (C 1-6  alkylene) r -NR c CONR f \u2014(C 1-6  alkylene) s , wherein each of the C 1-6  alkylene, C 2-6  alkenylene, and C 2-6  alkynylene is optionally substituted by 1, 2 or 3 substituents independently selected from halo, CN, NO 2 , N 3 , SCN, OH, C 1-6  alkyl, C 1-6  haloalkyl, C 2-8  alkoxyalkyl, C 1-6  alkoxy, C 1-6  haloalkoxy, amino, C 1-6  alkylamino, and C 2-8  dialkylamino; \n D 3  and E 3  are independently absent or independently selected from C 1-6  alkylene, C 2-6  alkenylene, C 2-6  alkynylene, arylene, cycloalkylene, heteroarylene, and heterocycloalkylene, wherein each of the C 1-6  alkylene, C 2-6  alkenylene, C 2-6  alkynylene, arylene, cycloalkylene, heteroarylene, and heterocycloalkylene is optionally substituted by 1, 2 or 3 substituents independently selected from halo, CN, NO 2 , N 3 , SCN, OH, C 1-6  alkyl, C 1-6  haloalkyl, C 2-8  alkoxyalkyl, C 1-6  alkoxy, C 1-6  haloalkoxy, amino, C 1-6  alkylamino, and C 2-8  dialkylamino; \n E 4  and E 4  are independently selected from H, halo, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, C 1-4  haloalkyl, halosulfanyl, C 1-4  hydroxyalkyl, C 1-4  cyanoalkyl, Cy 1 , CN, NO 2 , OR a , SR a , C(O)R b , C(O)NR c R a , C(O)OR a , OC(O)R b OC(O)NR c R d  NR c R d , NR c C(O)R b , NR c C(O)NR c R d , NR c C(O)OR a , C(\u2550NR i )NR c R d , NR c C(\u2550NR i )NR c R d , S(O)R b , S(O)NR c R d , S(O) 2 R b , NR c S(O) 2 R b , C(\u2550NOH)R b , C(\u2550NO(C 1-6  alkyl)R b , and S(O) 2 NR c R d , wherein said C 1-8  alkyl, C 2-8  alkenyl, or C 2-8  alkynyl, is optionally substituted with 1, 2, 3, 4, 5, or 6 substituents independently selected from halo, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, C 1-4  haloalkyl, halosulfanyl, C 1-4  hydroxyalkyl, C 1-4  cyanoalkyl, Cy 1 , CN, NO 2 , OR a , SR a , C(O)R b , C(O)NR c R d , C(O)OR a , OC(O)R b , OC(O)NR c R d , NR c R d , NR c C(O)R b , NR c C(O)NR c R d , NR c C(O)OR a , C(\u2550NR i )NR c R d , NR c C(\u2550NR i )NR c R d , S(O)R b , S(O)NR c R d , S(O) 2 R b , NR c S(O) 2 R b , C(\u2550NOH)R b , C(\u2550NO(C 1-6  alkyl))R b , and S(O) 2 NR c R d ; \n R a  is H, Cy 1 , \u2014(C 1-6  alkyl)-Cy 1 , C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, wherein said C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, or C 2-6  alkynyl is optionally substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, halo, C 1-6  alkyl, C 1-6  haloalkyl, halosulfanyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl and heterocycloalkyl; \n R b  is H, Cy 1 , \u2014(C 1-6  alkyl)-Cy 1 , C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, wherein said C 1-6  alkyl, C 1-61-6  haloalkyl, C 2-6  alkenyl, or C 2-6  alkynyl is optionally substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, halo, C 1-6  alkyl, C 1-6  haloalkyl, C 1-6  haloalkyl, halosulfanyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl and heterocycloalkyl; \n R a \u2032 and R a \u2033 are independently selected from H, C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl and heterocycloalkylalkyl, wherein said C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocycloalkylalkyl is optionally substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, halo, C 1-6  alkyl, C 1-6  haloalkyl, halosulfanyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl and heterocycloalkyl; \n R b\u2032  and R b\u2033  are independently selected from H, C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl and heterocycloalkylalkyl, wherein said C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocycloalkylalkyl is optionally substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, halo, C 1-6  alkyl, C 1-6  haloalkyl, C 1-6  haloalkyl, halosulfanyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl and heterocycloalkyl; \n R c  and R d  are independently selected from H, Cy 1 , \u2014(C 1-6  alkyl)-Cy 1 , C 1-10  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, wherein said C 1-10  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, or C 2-6  alkynyl, is optionally substituted with 1, 2, or 3 substituents independently selected from Cy 1 , \u2014(C 1-6  alkyl)-Cy 1 , OH, CN, amino, halo, C 1-6  alkyl, C 1-6  haloalkyl, C 1-6  haloalkyl, and halosulfanyl; \n or R c  and R d  together with the N atom to which they are attached form a 4-, 5-, 6- or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from Cy 1 , \u2014(C 1-6  alkyl)-Cy 1 , OH, CN, amino, halo, C 1-6  alkyl, C 1-6  haloalkyl, C 1-6  haloalkyl, and halosulfanyl; \n R c \u2032 and R d \u2032 are independently selected from H, C 1-10  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl and heterocycloalkylalkyl, wherein said C 1-10  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocycloalkylalkyl is optionally substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, halo, C 1-6  alkyl, C 1-6  haloalkyl, C 1-6  haloalkyl, halosulfanyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl and heterocycloalkyl; \n or R c \u2032 and R d \u2032 together with the N atom to which they are attached form a 4-, 5-, 6- or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, halo, C 1-6  alkyl, C 1-6  haloalkyl, C 1-6  haloalkyl, halosulfanyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl and heterocycloalkyl; \n R c \u2033 and R d \u2033 are independently selected from H, C 1-10  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl and heterocycloalkylalkyl, wherein said C 1-10  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocycloalkylalkyl is optionally substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, halo, C 1-6  alkyl, C 1-6  haloalkyl, halosulfanyl, C 1-6  haloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl and heterocycloalkyl; \n or R c \u2033 and R d \u2033 together with the N atom to which they are attached form a 4-, 5-, 6- or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, halo, C 1-6  alkyl, C 1-6  haloalkyl, C 1-6  haloalkyl, halosulfanyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl and heterocycloalkyl; \n R i  is H, CN, NO 2 , or C 1-6  alkyl; \n R e  and R f  are independently selected from H and C 1-6  alkyl; \n R i  is H, CN, or NO 2 ; \n m is 0 or 1; \n n is 0 or 1; \n p is 0, 1,2,3,4,5, or 6; \n q is 0, 1, 2, 3, 4, 5 or 6; \n r is 0 or 1; and \n s is 0 or 1.

Metadata:
- Claim Count in Document: 65.0
- Percentile: 95.0
- Lexical Diversity: 1.7027
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14360905', '14808860', '13293828', '14512262', '12784916']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7194160170081821
- 35 USC 102 Novelty (BERT): 0.636034868128416
- Combined Prediction Score: 0.7110779021202055
- Mean Citation Score: 448.166796
- Max Citation Score: 695.8886
- Similarity Product: 518.1731675338149

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