PATENT CLAIM ANALYSIS

Application Number: 15942333
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-10
Patent Classification: ["514", "211080"]

Abstract:
Isoquinoline compounds and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibitng HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the isoquinoline compounds.

Claim (Index 1):
A compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein,\n R 1  is hydrogen, halogen, cyano, C 1-6  alkyl, C 3-7  cycloalkyl, C 1-6  haloalkyl, C 1-6  hydroxyalkyl, hydroxyl, C 1-6  alkoxyl, optionally substituted amino or optionally substituted acylamino; \n R 2  is (a), (b), (c), (d), (e), (f), (g) or (h):\n (a) a 5-10 membered heteroaryl or 5-10 membered heterocyclyl, having 1-4 heteroatoms selected from O, S, and N; and optionally substituted with one, two, three, four or five substituents; or \n (b) a C 6-10  aryl optionally substituted with one, two, three, four or five substituents; or \n (c) hydrogen, halogen, cyano, \u2014NR b C(O)R a , \u2014NR b SO 2 R a , \u2014SO 2 NR a R b ; or \u2014SO 2 R a ; \n \n wherein each R a  is independently C 1-6  alkyl, and R b  is independently hydrogen or C 1-6  alkyl; or R a  and R b  are taken together with the atom(s) to which they are attached to form an optionally substituted 5-10 membered heterocyclyl; or\n (d) \u2014OR a1  or \u2014(C 1-6  alkylene)-OR a1 ; wherein each R a1  is independently C 1-6  alkyl optionally substituted with C 6-10  aryl; 5-10 membered heteroaryl; or 5-10 membered heterocyclyl; wherein the C 6-10  aryl, 5-10 membered heteroaryl, and 5-10 membered heterocyclyl are optionally substituted; or \n (e) a C 1-6  alkyl, C 2-6  alkenyl, or C 2-6  alkynyl, each optionally substituted with one to five substituents; or \n (f) a C 3-8  cycloalkyl optionally substituted with one to five substituents; \n (g) \u2014C(O)NR a2 R b2  or NR a2 (CO)R b2 , wherein each R a2  is independently hydrogen or C 1-6  alkyl, and R b2  is hydrogen, C 1-6  alkyl, C 6-10  aryl, 5-10 membered heteroaryl or 5-10 membered heterocyclyl; or R a2  and R b2  are taken together with the atom(s) to which they are attached to form an optionally substituted 5-10 membered heterocyclyl; wherein the C 1-6  alkyl, C 6-10  aryl, 5-10 membered heteroaryl and 5-10 membered heterocyclyl are optionally substituted; or \n (h) 5-10 membered heteroaryl fused with a ring selected from the group consisting of 5 or 6 membered heteroaryl, 5-10 membered heterocyclyl, C 6-10  aryl and C 3-7  cycloalkyl, wherein the 5-10 membered heteroaryl of R 2  and the fused ring are optionally substituted with one to four substituents; \n \n R 3  is hydrogen, cyano, halogen, optionally substituted C 1-6  alkyl, optionally substituted C 2-9  heterocyclyl, or optionally substituted C 1-6  alkoxy; and \n R 4  is A-C(O)\u2014 or D; \n A is C 1-6  alkyl, C 3-7  cycloalkyl, C 2-9  heteroaryl, C 2-9  heterocyclyl, \u2014NHR g  or \u2014OR h ; wherein the C 1-6  alkyl, C 3-7  cycloalkyl, 7 C 2-9  heteroaryl and C 2-9  heterocyclyl of A are optionally substituted independently with one, two, three, four or five substituents; \n R g  and R h  are independently C 1-6  alkyl, C 2-6  alkenyl, C 3-7  cycloalkyl, C 6-10  aryl, C 2-9  heteroaryl, or C 2-9  heterocyclyl; wherein the C 1-6  alkyl, C 2-6  alkenyl, C 3-7  cycloalkyl, C 6-10  aryl, C 2-9  heteroaryl and C 2-9  heterocyclyl of R g  and R h  are optionally substituted independently with one, two, three, four or five substituents; and \n D is hydrogen, a C 6-10  aryl, or a 5-10 membered heteroaryl having 1-4 heteroatoms selected from O, S, and N; or a 5-10 membered heteroaryl fused with a ring selected from the group consisting of 5- or 6-membered heteroaryl, 5-10 membered heterocyclyl, C 6  aryl and C 3-8  cycloalkyl; wherein the 5-10 membered heteroaryl of D and the fused ring are optionally substituted with one, two, three, four or five substituents; \n provided that the compound is other than compounds selected from the group consisting of N-(8-amino-3-isoquinolinyl)-N\u2032-ethyl-urea, 5-[(8-amino-3-isoquinolinyl)amino]-2-pyrazinecarbonitrile, and 5-[(8-amino-3-isoquinolinyl)amino]-3-[(1R)-2-(dimethylamino)-1-methylethoxy]-2-pyrazinecarbonitrile, and pharmaceutically acceptable salts thereof.

Metadata:
- Claim Count in Document: 104.0
- Percentile: 90.0
- Lexical Diversity: 1.71429
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15942321', '15698788', '13266976', '15852639', '14428546']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8067469421221503
- 35 USC 102 Novelty (BERT): 0.5304334058721827
- Combined Prediction Score: 0.7791155884971536
- Mean Citation Score: 281.45004400000005
- Max Citation Score: 362.283
- Similarity Product: 302.1170482973457

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

Dataset: test