PATENT CLAIM ANALYSIS

Application Number: 16228324
Application Type: Utility
Filing Date: 2018-12
Publication Date: 2019-07
Patent Classification: ["514", "255050"]

Abstract:
The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.

Claim (Index 2):
The compound of  claim 1 , wherein the compound is Formula I: or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or isomer thereof, wherein: A is 5- to 12-membered monocyclic or polycyclic heterocycloalkyl, aryl, or heteroaryl; Y 1  is \u2014S\u2014 or a direct bond; Y 2  is \u2014NR a \u2014, \u2014(CR a 2 ) m \u2014, \u2014C(O)\u2014, \u2014C(R a ) 2 NH\u2014, \u2014(CR a 2 ) m O\u2014, \u2014C(O)N(R a )\u2014, \u2014N(R a )C(O)\u2014, \u2014S(O) 2 N(R a )\u2014, \u2014N(R a )S(O) 2 \u2014, \u2014N(R a )C(O)N(R a )\u2014, \u2014N(R a )C(S)N(R a )\u2014, \u2014C(O)O\u2014, \u2014OC(O)\u2014, \u2014OC(O)N(R a )\u2014, \u2014N(R a )C(O)O\u2014, \u2014C(O)N(R a )O\u2014, \u2014N(R a )C(S)\u2014, \u2014C(S)N(R a )\u2014, or \u2014OC(O)O\u2014; wherein the bond on the left side of Y 2 , as drawn, is bound to the pyrazine ring and the bond on the right side of the Y 2  moiety is bound to R 3 ; R 1  is independently, at each occurrence, \u2014H, -D, \u2014C 1 -C 6 alkyl, \u2014C 2 -C 6 alkenyl, \u2014C 4 -C 8 cycloalkenyl, \u2014C 2 -C 6 alkynyl, \u2014C 3 -C 8 cycloalkyl, \u2014OH, halogen, \u2014NO 2 , \u2014CN, \u2014NR 5 R 6 , \u2014SR 5 , \u2014S(O) 2 NR 5 R 6 , \u2014S(O) 2 R 5 , \u2014NR 5 S(O) 2 NR 5 R 6 , \u2014NR 5 S(O) 2 R 6 , \u2014S(O)NR 5 R 6 , \u2014S(O)R 5 , \u2014NR 5 S(O)NR 5 R 6 , \u2014NR 5 S(O)R 6 , \u2014C(O)R 5 , or \u2014CO 2 R 5 , wherein each alkyl, alkenyl, cycloalkenyl, alkynyl, or cycloalkyl is optionally substituted with one or more \u2014OH, \u2014NO 2 , oxo, \u2014CN, \u2014R 5 , \u2014OR 5 , \u2014NR 5 R 6 , \u2014SR 5 , \u2014S(O) 2 NR 5 R 6 , \u2014S(O) 2 R 5 , \u2014NR 5 S(O) 2 NR 5 R 6 , \u2014NR 5 S(O) 2 R 6 , \u2014S(O)NR 5 R 6 , \u2014S(O)R 5 , \u2014NR 5 S(O)NR 5 R 6 , \u2014NR 5 S(O)R 6 , heterocycle, aryl, or heteroaryl; R 2  is independently \u2014OH, \u2014CN, \u2014C 1 -C 6 alkyl, \u2014C 2 -C 6 alkenyl, \u2014C 4 -C 8 cycloalkenyl, \u2014C 2 -C 6 alkynyl, \u2014C 3 -C 8 cycloalkyl, aryl, heterocyclyl containing 1-5 heteroatoms selected from the group consisting of N, S, P, and O, or heteroaryl containing 1-5 heteroatoms selected from the group consisting of N, S, P, and O; wherein each alkyl, alkenyl, cycloalkenyl, alkynyl, cycloalkyl, heterocyclyl, or heteroaryl is optionally substituted with one or more \u2014OH, halogen, \u2014NO 2 , oxo, \u2014CN, \u2014R 5 , \u2014OR 5 , \u2014NR 5 R 6 , \u2014SR 5 , \u2014S(O) 2 NR 5 R 6 , \u2014S(O) 2 R 5 , \u2014NR 5 \u2014NR 5 S(O) 2 R 6 , \u2014S(O)NR 5 R 6 , \u2014S(O)R 5 , \u2014NR 5 S(O)NR 5 R 6 , \u2014NR 5 S(O)R 6 , heterocycle, aryl, or heteroaryl; and wherein the heterocyclyl or heteroaryl is not attached via a nitrogen atom; R a  is independently, at each occurrence, \u2014H, -D, \u2014OH, \u2014C 3 -C 8 cycloalkyl, or \u2014C 1 -C 6 alkyl, wherein each alkyl or cycloalkyl is optionally substituted with one or more \u2014NH 2 , wherein 2 R a , together with the carbon atom to which they are both attached, can combine to form a 3- to 8-membered cycloalkyl; R b  is independently, at each occurrence, \u2014H, -D, \u2014C 1 -C 6 alkyl, \u2014C 3 -C 8 cycloalkyl, \u2014C 2 -C 6 alkenyl, or heterocyclyl containing 1-5 heteroatoms selected from the group consisting of N, S, P, and O; wherein each alkyl, cycloalkyl, alkenyl, or heterocycle is optionally substituted with one or more \u2014OH, halogen, \u2014NO 2 , oxo, \u2014CN, \u2014R 5 , \u2014OR 5 , \u2014NR 5 R 6 , \u2014SR 5 , \u2014S(O) 2 NR 5 R 6 , \u2014S(O) 2 R 5 , \u2014NR 5 S(O) 2 NR 5 R 6 , \u2014NR 5 S(O) 2 R 6 , \u2014S(O)NR 5 R 6 , \u2014S(O)R 5 , \u2014NR 5 S(O)NR 5 R 6 , \u2014NR 5 S(O)R 6 , heterocycle, aryl, or heteroaryl; R 3  is independently \u2014C 1 -C 6 alkyl or a 3- to 12-membered monocyclic or polycyclic heterocycle, wherein each alkyl or heterocycle is optionally substituted with one or more \u2014C 1 -C 6 alkyl, \u2014OH, or \u2014NH 2 ; or R 3  can combine with R a  to form a 3- to 12-membered monocyclic or polycyclic heterocycle or a 5- to 12-membered spiroheterocycle, wherein each heterocycle or spiroheterocycle is optionally substituted with \u2014C 1 -C 6 alkyl, \u2014OH, or \u2014NH 2 ; R 4  is independently \u2014H, -D, or \u2014C 1 -C 6 alkyl, wherein each alkyl is optionally substituted with one or more \u2014OH, \u2014NH 2 , halogen, or oxo; or R a  and R 4 , together with the atom or atoms to which they are attached, can combine to form a monocyclic or polycyclic C 3 -C 12 cycloalkyl or a monocyclic or polycyclic 3- to 12-membered heterocycle, wherein the cycloalkyl or heterocycle is optionally substituted with oxo; R 5  is independently \u2014H, -D, \u2014C 1 -C 6 alkyl, \u2014C 2 -C 6 alkenyl, \u2014C 4 -C 8 cycloalkenyl, \u2014C 2 -C 6 alkynyl, \u2014C 3 -C 8 cycloalkyl, a monocyclic or polycyclic 3- to 12-membered heterocycle, \u2014OR 7 , \u2014SR 7 , \u2014NR 7 R 8 , \u2014NO 2 , or \u2014CN; R 6  is independently \u2014H, -D, \u2014C 1 -C 6 alkyl, \u2014C 2 -C 6 alkenyl, \u2014C 4 -C 8 cycloalkenyl, \u2014C 2 -C 6 alkynyl, \u2014C 3 -C 8 cycloalkyl, a monocyclic or polycyclic 3- to 12-membered heterocycle, \u2014OR 7 , \u2014SR 7 , halogen, \u2014NR 7 R 8 , \u2014NO 2 , or \u2014CN; R 7  and R 8  are independently, at each occurrence, \u2014H, -D, \u2014C 1 -C 6 alkyl, \u2014C 2 -C 6 alkenyl, \u2014C 4 -C 8 cycloalkenyl, \u2014C 2 -C 6 alkynyl, \u2014C 3 -C 8 cycloalkyl, or a monocyclic or polycyclic 3- to 12-membered heterocycle, wherein each alkyl, alkenyl, cycloalkenyl, alkynyl, cycloalkyl, or heterocycle is optionally substituted with one or more \u2014OH, \u2014SH, \u2014NH 2 , \u2014NO 2 , or \u2014CN; m is independently, at each occurrence, 1, 2, 3, 4, 5 or 6; and n is independently, at each occurrence, 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 98.0
- Lexical Diversity: 1.125
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['16186490', '13352864', '14344628', '14670422', '14670421']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8100176951184463
- 35 USC 102 Novelty (BERT): 0.5375660207587649
- Combined Prediction Score: 0.7827725276824783
- Mean Citation Score: 355.792522
- Max Citation Score: 365.5356
- Similarity Product: 279.55420172896385

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