PATENT CLAIM ANALYSIS

Application Number: 16045518
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2019-01
Patent Classification: ["544", "284000"]

Abstract:
The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.

Claim (Index 51):
A method for inhibiting cancer Osaka thyroid (Cot) comprising administering, to a human patient in need thereof, an effective amount of a compound of Formula I: wherein R 1  is C 1-9  alkyl, C 3-15  cycloalkyl, heterocyclyl, heteroaryl, or C 6-10  aryl; wherein each C 1-9  alkyl, C 3-15  cycloalkyl, heterocyclyl, heteroaryl, and C 6-10  aryl may be optionally substituted with one to four Z 1 ; R 2  is hydrogen, \u2014C(O)\u2014R 7 , \u2014C(O)O\u2014R 7 , \u2014C(O)N(R 7 ) 2 , or C 1-9  alkyl; R 3  is heterocyclyl or heteroaryl;\n wherein each heterocyclyl or heteroaryl is optionally substituted with one to four Z 3 ; \n R 4  is aryl, heterocyclyl, or heteroaryl;\n wherein each aryl, heterocyclyl, or heteroaryl is optionally substituted with one to four Z 4 ; \n R 5  is hydrogen, halo, cyano, \u2014NO 2 , \u2014O\u2014R 7 , \u2014N(R 8 )(R 9 ), \u2014S(O)\u2014R 7 , \u2014S(O) 2 R 7 , \u2014S(O) 2 N(R 7 ) 2 , \u2014C(O)R 7 , OC(O)\u2014R 7 , \u2014C(O)O\u2014R 7 , \u2014OC(O)O\u2014R 7 , \u2014OC(O)N(R 10 )(R 11 ), \u2014C(O)N(R 7 ) 2 , \u2014N(R 7 )C(O)(R 7 ), C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-9  alkylthio, C 1-6  haloalkyl, C 3-15  cycloalkyl, aryl, heterocyclyl, or heteroaryl;\n wherein each C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-9  alkylthio, C 1-6  haloalkyl, C 3-15  cycloalkyl, aryl, heterocyclyl, and heteroaryl may be optionally substituted with one to four Z 5 ; \n R 6  is hydrogen, \u2014C(O)\u2014R 7 , \u2014C(O)O\u2014R 7 , \u2014C(O)N(R 7 ) 2 , C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  haloalkyl, C 3-15  cycloalkyl, aryl, heterocyclyl, or heteroaryl;\n wherein each C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  haloalkyl, C 3-15  cycloalkyl, aryl, heterocyclyl, and heteroaryl may be optionally substituted with one to four Z 6 ; \n each R 7  is independently hydrogen, C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  haloalkyl, C 3-15  cycloalkyl, aryl, heterocyclyl, or heteroaryl;\n wherein each C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  haloalkyl, C 3-15  cycloalkyl, aryl, heterocyclyl, and heteroaryl may be optionally substituted with one to four Z 7 ; \n R 8  and R 9  at each occurrence are independently hydrogen, \u2014S(O) 2 R 10 , \u2014C(O)\u2014R 10 , \u2014C(O)O\u2014R 10 , \u2014C(O)N(R 10 )(R 11 ), C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  haloalkyl, C 3-15  cycloalkyl, aryl, heterocyclyl, or heteroaryl;\n wherein each C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  haloalkyl, C 3-15  cycloalkyl, aryl, heterocyclyl, or heteroaryl may be optionally substituted with one to four Z 8 ; \n R 10  and R 11  at each occurrence are independently hydrogen, C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  haloalkyl, C 3-15  cycloalkyl, aryl, heterocyclyl, or heteroaryl,\n wherein each C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  haloalkyl, C 3-15  cycloalkyl, aryl, heterocyclyl, and heteroaryl optionally is substituted with one to four Z 1b ; \n each Z 1 , Z 3 , Z 4 , Z 5 , Z 6 , Z 7  and Z 8  is independently hydrogen, oxo, halo, \u2014NO 2 , \u2014N 3 , cyano, thioxo, C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 3-15  cycloalkyl, C 1-8  haloalkyl, aryl, heteroaryl, heterocyclyl, \u2014O\u2014R 12 , \u2014C(O)\u2014R 12 , \u2014C(O)O\u2014R 12 , \u2014C(O)\u2014N(R 13 )(R 14 ), \u2014N(R 13 )(R 14 ), \u2014N(R 13 ) 2 (R 14 ) + , \u2014N(R 12 )C(O)\u2014R 12 , \u2014N(R 12 )C(O)O\u2014R 12 , \u2014N(R 12 )C(O)N(R(R 13 )(R 14 ), \u2014N(R 12 )S(O) 2 (R 12 ), \u2014NR 12 S(O) 2 N(R 13 )(R 14 ), \u2014NR 12 S(O) 2 O(R 12 ), \u2014OC(O)R 12 , \u2014OC(O)\u2014N(R 13 )(R 14 ), \u2014P(O)(OR 12 ) 2 , \u2014OP( 12 )(OR 12 ) 2 , \u2014CH 2 P(O)(OR 12 ) 2 , \u2014OCH 2 P(O)(OR 1 ) 2 , \u2014C(O)OCH 2 P(O)(O)R 12 ) 2 , \u2014P(O)(R 12 )(OR 12 ), \u2014OP(O)(R 12 )(OR 12 ), \u2014CH 2 P(O)(R 12 )(OR 12 ), OCH 2 P(O)(R 12 )(OR 12 ), \u2014C(O)OCH 2 P(O)(R 12 )(OR 12 ), \u2014P(O)(N(R 12 ) 2 ) 2 , \u2014OP(O)(N(R 12 ) 2 ) 2 , \u2014CH 2 P(O)(N(R 12 ) 2 ) 2 , \u2014OCH 2 P(O)(N(R 12 ) 2 ) 2 , \u2014C(O)OCH 2 P(O)(N(R 12 ) 2 ) 2 , \u2014P(O)(N(R 12 ) 2 )(OR 12 ), \u2014OP(O)(N(R 12 ) 2 )(OR 12 ), \u2014CH 2 P(O)(N(R 12 ) 2 )(OR 12 ), \u2014OCH 2 P(O)(N(R 12 ) 2 )(OR 12 ), C(O)OCH 2 P(O)(N(R 12 ) 2 )(OR 12 ), \u2014P(O)(R 12 )(N(R 12 ) 2 ), \u2014OP(O)(R 12 )(N(R 12 ) 2 ), \u2014CH 2 P(O)(R 12 )(N(R 12 ) 2 ), \u2014OCH 2 P(O)(R 12 )(N(R 12 ) 2 ), \u2014C(O)OCH 2 P(O)(R 12 )(N(R 12 ) 2 ), \u2014Si(R 12 ) 3 , \u2014S\u2014R 12 , \u2014S(O)R 12 , \u2014S(O)(NH)R 12 , \u2014S(O) 2 R 12  or \u2014S(O) 2 N(R 13 )(R 14 );\n wherein any alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with one to four Z 1a  groups; \n each Z 1a  is independently oxo, halo, thioxo, \u2014NO 2 , cyano, \u2014N 3 , C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 3-15  cycloalkyl, C 1-8  haloalkyl, aryl, heteroaryl, heterocyclyl, \u2014O\u2014R 12 , \u2014C(O)R 12 , \u2014C(O)O\u2014R 12 , \u2014C(O)N(R 13 )(R 14 ), \u2014N(R 13 )(R 14 ), \u2014N(R 13 ) 2 (R 14 ) + , \u2014N(R 12 )\u2014C(O)R 12 , \u2014N(R 12 )C(O)O(R 12 ), \u2014N(R 12 )C(O)N(R 13 )(R 14 ), \u2014N(R 12 )S(O) 2 (R 12 ), \u2014N(R 12 )S(O) 2 \u2014N(R 13 )(R 14 ), \u2014N(R 12 )S(O) 2 O(R 12 ), \u2014OC(O)R 12 , \u2014OC(O)OR 12 , \u2014OC(O)\u2014N(R 13 )(R 14 ), \u2014Si(R 12 ) 3 , \u2014S\u2014R 12 , \u2014S(O)R 12 , \u2014S(O)(NH)R 12 , \u2014S(O) 2 R 12  or \u2014S(O) 2 N(R 13 )(R 14 );\n wherein any alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with one to four Z 1b  groups; \n each R 12  is independently hydrogen, C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 3-15  cycloalkyl, aryl, heteroaryl or heterocyclyl,\n wherein any alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with one to four Z 1b  groups; \n R 13  and R 14  at each occurrence are each independently hydrogen, C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 3-15  cycloalkyl, aryl, heteroaryl or heterocyclyl;\n wherein any alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with one to four Z 1b  groups, or R 13  and R 14  together with the nitrogen to which they are attached form a heterocyclyl, wherein said heterocyclyl is optionally substituted with one to four Z 1b  groups; \n each Z 1b  is independently oxo, thioxo, hydroxy, halo, \u2014NO 2 , \u2014N 3 , cyano, C 1-9  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 3-15  cycloalkyl, C 1-8  haloalkyl, aryl, heteroaryl, heterocyclyl, \u2014O(C 1-9  alkyl), \u2014O(C 2-6  alkenyl), \u2014O(C 2-6  alkynyl), \u2014O(C 3-15  cycloalkyl), \u2014O(C 1-8  haloalkyl), \u2014O(aryl), \u2014O(heteroaryl), \u2014O(heterocyclyl), \u2014NH 2 , \u2014NH(C 1-9  alkyl), \u2014NH(C 2-6  alkenyl), \u2014NH(C 2-6  alkynyl), \u2014NH(C 3-15  cycloalkyl), \u2014NH(C 1-8  haloalkyl), \u2014NH(aryl), \u2014NH(heteroaryl), \u2014NH(heterocyclyl), \u2014N(C 1-9  alkyl) 2 , \u2014N(C 3-15  cycloalkyl) 2 , \u2014N(C 2-6  alkenyl) 2 , \u2014N(C 2-6  alkynyl) 2 , \u2014N(C 3-15  cycloalkyl) 2 , \u2014N(C 1-8  haloalkyl) 2 , \u2014N(aryl) 2 , \u2014N(heteroaryl) 2 , \u2014N(heterocyclyl) 2 , \u2014N(C 1-9  alkyl)(C 3-15  cycloalkyl), \u2014N(C 1-9  alkyl)(C 2-6  alkenyl), \u2014N(C 1-9  alkyl)(C 2-6  alkynyl), \u2014N(C 1-9  alkyl)(C 3-15  cycloalkyl), \u2014N(C 1-9  alkyl)(C 1-8  haloalkyl), \u2014N(C 1-9  alkyl)(aryl), \u2014N(C 1-9  alkyl)(heteroaryl), \u2014N(C 1-9  alkyl)(heterocyclyl), \u2014C(O)(C 1-9  alkyl), \u2014C(O)(C 2-6  alkenyl), \u2014C(O)(C 2-6  alkynyl), \u2014C(O)(C 3-15  cycloalkyl), \u2014C(O)(C 1-8  haloalkyl), \u2014C(O)(aryl), \u2014C(O)(heteroaryl), \u2014C(O)(heterocyclyl), \u2014C(O)O(C 1-9  alkyl), \u2014C(O)O(C 2-6  alkenyl), \u2014C(O)O(C 2-6  alkynyl), \u2014C(O)O(C 3-15  cycloalkyl), \u2014C(O)O(C 1-8  haloalkyl), \u2014C(O)O(aryl), \u2014C(O)O(heteroaryl), \u2014C(O)O(heterocyclyl), \u2014C(O)NH 2 , \u2014C(O)NH(C 1-9  alkyl), \u2014C(O)NH(C 2-6  alkenyl), \u2014C(O)NH(C 2-6  alkynyl), \u2014C(O)NH(C 3-15  cycloalkyl), \u2014C(O)NH(C 1-8  haloalkyl), \u2014C(O)NH(aryl), \u2014C(O)NH(heteroaryl), \u2014C(O)NH(heterocyclyl), \u2014C(O)N(C 1-9  alkyl) 2 , \u2014C(O)N(C 3-15  cycloalkyl) 2 , \u2014C(O)N(C 2-6  alkenyl) 2 , \u2014C(O)N(C 2-6  alkynyl) 2 , \u2014C(O)N(C 3-15  cycloalkyl) 2 , \u2014C(O)N(C 1-8  haloalkyl) 2 , \u2014C(O)N(aryl) 2 , \u2014C(O)N(heteroaryl) 2 , \u2014C(O)N(heterocyclyl) 2 , \u2014NHC(O)(C 1-9  alkyl), \u2014NHC(O)(C 2-6  alkenyl), \u2014NHC(O)(C 2-6  alkynyl), \u2014NHC(O)(C 3-15  cycloalkyl), \u2014NHC(O)(C 1-8  haloalkyl), \u2014NHC(O)(aryl), \u2014NHC(O)(heteroaryl), \u2014NHC(O)(heterocyclyl), \u2014NHC(O)O(C 1-9  alkyl), \u2014NHC(O)O(C 2-6  alkenyl), \u2014NHC(O)O(C 2-6  alkynyl), \u2014NHC(O)O(C 3-15  cycloalkyl), \u2014NHC(O)O(C 1-8  haloalkyl), \u2014NHC(O)O(aryl), \u2014NHC(O)O(heteroaryl), \u2014NHC(O)O(heterocyclyl), \u2014NHC(O)NH(C 1-9  alkyl), \u2014NHC(O)NH(C 2-6  alkenyl), \u2014NHC(O)NH(C 2-6  alkynyl), \u2014NHC(O)NH(C 3-15  cycloalkyl), \u2014NHC(O)NH(C 1-8  haloalkyl), \u2014NHC(O)NH(aryl), \u2014NHC(O)NH(heteroaryl), \u2014NHC(O)NH(heterocyclyl), \u2014SH, \u2014S(C 1-9  alkyl), \u2014S(C 2-6  alkenyl), \u2014S(C 2-6  alkynyl), \u2014S(C 3-15  cycloalkyl), \u2014S(C 1-8  haloalkyl), \u2014S(aryl), \u2014S(heteroaryl), \u2014S(heterocyclyl), \u2014NHS(O)(C 1-9  alkyl), \u2014N(C 1-9  alkyl)(S(O)(C 1-9  alkyl), \u2014S(O)N(C 1-9  alkyl) 2 , \u2014S(O)(C 1-9  alkyl), \u2014S(O)(NH)(C 1-9  alkyl), \u2014S(O)(C 2-6  alkenyl), \u2014S(O)(C 2-6  alkynyl), \u2014S(O)(C 3-15  cycloalkyl), \u2014S(O)(C 1-8  haloalkyl), \u2014S(O)(aryl), \u2014S(O)(heteroaryl), \u2014S(O)(heterocyclyl), \u2014S(O) 2 (C 1-9  alkyl), \u2014S(O) 2 (C 2-6  alkenyl), \u2014S(O) 2 (C 2-6  alkynyl), \u2014S(O) 2 (C 3-15  cycloalkyl), \u2014S(O) 2 (C 1-8  haloalkyl), \u2014S(O) 2 (aryl), \u2014S(O) 2 (heteroaryl), \u2014S(O) 2 (heterocyclyl), \u2014S(O) 2 NH(C 1-9  alkyl), or \u2014S(O) 2 N(C 1-9  alkyl) 2 ;\n wherein any alkyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl is optionally substituted with one to four halo, C 1-9  alkyl, C 1-8  haloalkyl, \u2014OH, \u2014NH 2 , \u2014NH(C 1-9  alkyl), \u2014NH(C 3-15  cycloalkyl), \u2014NH(C 1-8  haloalkyl), \u2014NH(aryl), \u2014NH(heteroaryl), \u2014NH(heterocyclyl), \u2014N(C 1-9  alkyl) 2 , \u2014N(C 3-15  cycloalkyl) 2 , \u2014NHC(O)(C 3-15  cycloalkyl), \u2014NHC(O)(C 1-8  haloalkyl), \u2014NHC(O)(aryl), \u2014NHC(O)(heteroaryl), \u2014NHC(O)(heterocyclyl), \u2014NHC(O)O(C 1-9  alkyl), \u2014NHC(O)O(C 2-6  alkynyl), \u2014NHC(O)O(C 3-15  cycloalkyl), \u2014NHC(O)O(C 1-8  haloalkyl), \u2014NHC(O)O(aryl), \u2014NHC(O)O(heteroaryl), \u2014NHC(O)O(heterocyclyl), \u2014NHC(O)NH(C 1-9  alkyl), \u2014S(O)(NH)(C 1-9  alkyl), S(O) 2 (C 1-9  alkyl), \u2014S(O) 2 (C 3-15  cycloalkyl), \u2014S(O) 2 (C 1-8  haloalkyl), \u2014S(O) 2 (aryl), \u2014S(O) 2 (heteroaryl), \u2014S(O) 2 (heterocyclyl), \u2014S(O) 2 NH(C 1-9  alkyl), \u2014S(O) 2 N(C 1-9  alkyl) 2 , \u2014O(C 3-15  cycloalkyl), \u2014O(C 1-8  haloalkyl), \u2014O(aryl), \u2014O(heteroaryl), \u2014O(heterocyclyl), or \u2014O(C 1-9  alkyl); \n m is 0, 1, or 2; or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers, or deuterated analog thereof.

Metadata:
- Claim Count in Document: 11.0
- Percentile: 95.0
- Lexical Diversity: 1.1
- Patent Class: 544.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15634314', '15199779', '15697755', '13066616', '13878654']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8280436482682236
- 35 USC 102 Novelty (BERT): 0.5634066640403573
- Combined Prediction Score: 0.801579949845437
- Mean Citation Score: 451.13848600000006
- Max Citation Score: 479.00513
- Similarity Product: 362.80521210693536

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