PATENT CLAIM ANALYSIS

Application Number: 15942321
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-10
Patent Classification: ["514", "210020"]

Abstract:
Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

Claim (Index 14):
The compound of  claim 13 , wherein A is:\n i. (C 3-7  cycloalkyl)(C 1-6  alkyl) j - or (C 2-9  heterocyclyl)(C 1-6  alkyl) j -, wherein, j is 1 or 0; and wherein said cycloalkyl or heterocyclyl can be optionally substituted with one, two, three or four of R, wherein R, in each instance, is independently selected from the group consisting of branched or linear C 1-6  alkyl, halogen, cyano, cyano(C 1-6  alkyl)-, \u2014CF 3 , \u2014CHF 2 , hydroxy(C 1-6  alkyl), halo(C 1-6  alkyl), hydroxyl, (C 1-6  alkyl)-O\u2014(C 1-6  alkyl)-, \u2014(C 1-6  alkyl)-NHC(O)\u2014(C 1-6  alkyl), amino, \u2014NR\u2032C(O)R\u2033, acetyl, di(C 1-6  alkyl)amino, mono(C 1-6  alkyl)amino, amino(C 1-6  alkyl), C 1-6  alkoxy, CH 3 CO 2 \u2014(C 1-6  alkyl)-, \u2014NR\u2032SO 2 R\u2033, \u2014SO 2 R\u2032, \u2014SO 2 NR\u2032R\u2033, \u2014C(O)NR\u2032R\u2033, \u2014NR\u2032C(O)R\u2033, optionally substituted C 2-9  heteroaryl, optionally substituted C 2-9  heterocyclyl, optionally substituted C 6-10  aryl, optionally substituted C 3-9  cycloalkyl-C(O)\u2014, and NR e R f \u2014C(O)\u2014(C 1-6  alkyl) k -,\n wherein said C 2-9  heteroaryl, C 2-9  heterocyclyl, and C 6-10  aryl can be optionally substituted with C 1-6  alkyl or (C 1-6  alkyl)-O\u2014(C 1-6  alkyl)-, wherein said (C 1-6  alkyl)-O\u2014(C 1-6  alkyl)- may be optionally substituted with amino, \n wherein, in each instance, R\u2032 and R\u2033 are independently H or C 1-6  alkyl, \n wherein R e  and R f  are each independently selected from the group consisting of hydrogen and branched or linear C 1-6  alkyl, or R e  and R f  together with the nitrogen to which each is bound can form a C 3-7  cycloalkyl, which can be optionally substituted with branched or linear C 1-6  alkyl, C 3-4  cycloalkyl, halogen, cyano, \u2014CF 3 , \u2014CHF 2 , or hydroxyl; \n and k is 1 or 0; \n or, said cycloalkyl or heterocyclyl together with two of R form a bicyclic or spiro ring, wherein two of R attached to different carbons are taken together with the carbon to which each is attached to form a bicyclic, or two of R 5  attached to the same carbon are taken together with the carbon to which each is attached to form a spiro ring, wherein said bicyclic or spiro rings may be substituted with one, two, three or four of R 5  as described above; \n ii. \u2014NR g R h , wherein\n R g  is H or branched or linear C 1-6  alkyl, wherein said alkyl can be optionally substituted with one to four substituents independently selected from the group consisting of hydroxyl, halogen, cyano, amino, di(C 1-6  alkyl)amino, mono(C 1-6  alkyl)amino; \u2014CHF 2 , and \u2014CF 3 ; \n R h  is selected from the group consisting of:\n a. branched or linear C 1-6  alkyl, wherein said alkyl can be optionally substituted with hydroxyl, halogen, cyano, amino, di(C 1-6  alkyl)amino, mono(C 1-6  alkyl)amino, \u2014CHF 2 , \u2014CF 3 , or NR e\u2032 R f\u2032 \u2014C(O)\u2014, wherein R e\u2032  and R f\u2032  are each independently hydrogen or branched or linear C 1-6  alkyl; \n and, \n b. (C 3-7  cycloalkyl)(C 1-6  alkyl) m -, (C 2-9  heteroaryl)(C 1-6  alkyl) m -, (C 6-10  aryl)(C 1-6  alkyl) m - or (C 2-9  heterocyclyl)(C 1-6  alkyl) m -, wherein, m is 1 or 0; and wherein said cycloalkyl, heteroaryl, aryl or heterocyclyl can be optionally substituted with one or two of R 5\u2032 , \n wherein R 5\u2032 , in each instance, is independently selected from the group consisting of branched or linear C 1-6  alkyl, halogen, cyano, cyano(C 1-6  alkyl)-, \u2014CF 3 , \u2014CHF 2 , hydroxy(C 1-6  alkyl), halo(C 1-6  alkyl), hydroxyl, C 1-6  alkoxy, amino, amino(C 1-6  alkyl), and NR i R j \u2014C(O)\u2014(C 1-6  alkyl) k\u2032 -, \n \n wherein R i  and R j  are independently selected from the group consisting of hydrogen and branched or linear C 1-6  alkyl, and k\u2032 is 1 or 0; \n iii. R 9 \u2014(C 1-6  alkyl)-, wherein R 9  is selected from the group consisting of hydroxyl, halogen, \u2014CHF 2 , \u2014CF 3 , cyano, C 1-6  alkoxy, \u2014NR o R p , NR o\u2032 R p\u2032 \u2014C(O)\u2014; wherein R o , R p , R o\u2032  and R p\u2032  are each independently hydrogen or branched or linear C 1-6  alkyl; iv. B\u2014(C 1-6  alkyl) t -, wherein, B is C 3-9  heteroaryl or C 3-7  heterocyclyl, wherein, said heteroaryl or heterocyclyl has 1-3 heteroatoms selected from O, S and N; and wherein said heteroaryl or heterocyclyl can be optionally substituted with one, two or three of R 10 , R 10\u2032  and R 10\u2033 , each of which is independently selected from the group consisting of:\n a. branched or linear C 1-6  alkyl or C 3-4  cycloalkyl, wherein said alkyl or cycloalkyl can be optionally substituted with hydroxyl, halogen, \u2014CHF 2 , \u2014CF 3 , amino, di(C 1-6  alkyl)amino, mono(C 1-6  alkyl)amino, cyano, \u2014C(O)NR q R r  or \u2014NR q C(O)R r , wherein R q  and R r  are independently H or C 1-6  alkyl; \n b. C 3-7  cycloalkyl; \n c. C 3-7  heterocyclyl; \n d. hydroxyl; \n e. halogen; \n f. \u2014CHF 2 ; \n g. \u2014CF 3 ; \n h. amino; \n i. di(C 1-6  alkyl)amino; \n j. mono(C 1-6  alkyl)amino; \n k. cyano; \n l. \u2014C(O)NR s R t , wherein R s  and R t  are independently H or C 1-6  alkyl; and \n m. \u2014NR s C(O)R t , wherein R s  and R t  are independently H or C 1-6  alkyl; \n and, t is 1 or 0; \n v. (C 6-10  aryl) q\u2032 -(C 1-6  alkyl) n -O\u2014 or (C 2-7  heterocyclyl)-O\u2014, wherein, said aryl or heterocyclyl can be optionally substituted with one, two or three of R 11 , R 12  and R 13 , each of which is selected from the group consisting of branched or linear C 1-6  alkyl, hydroxyl, halogen, \u2014CHF 2 , \u2014CF 3 , cyano, C 1-6  alkoxy, acetyl, and NR u R v \u2014; wherein R u  and R v  are each independently H or branched or linear C 1-6  alkyl; wherein, if present, a sulfur embedded in said heterocyclyl taken together with one oxygen can form a sulfoxide, or taken together with two oxygens can form a sulfone; and, n is 1 or 0, q\u2032 is 1 or 0, provided that one of n and q\u2032 is 1; or vi. branched or linear C 1-6  alkyl, C 1-6  alkenyl, C 1-6  alkenylene, wherein said alkyl, alkenyl, and alkenylene, can be optionally substituted with hydroxyl, halogen, \u2014CHF 2 , \u2014CF 3 , amino, di(C 1-6  alkyl)amino, mono(C 1-6  alkyl)amino, cyano, C 3-7  cycloalkyl, C 1-6  alkoxy, \u2014SO 2 R\u2032, \u2014SO 2 NR\u2032R\u2033, \u2014C(O)NR\u2032R\u2033, or \u2014NR\u2032C(O)R\u2033, wherein R\u2032 and R\u2033 are independently H or C 1-6  alkyl.

Metadata:
- Claim Count in Document: 140.0
- Percentile: 90.0
- Lexical Diversity: 1.83333
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['12530648', '13102720', '15281923', '13266976', '15852639']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7857474163791655
- 35 USC 102 Novelty (BERT): 0.5061792348644538
- Combined Prediction Score: 0.7577905982276942
- Mean Citation Score: 269.39763800000003
- Max Citation Score: 276.27457000000004
- Similarity Product: 226.1498162106693

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