PATENT CLAIM ANALYSIS

Application Number: 15887214
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-08
Patent Classification: ["546", "160000"]

Abstract:
Disclosed are compounds of Formula (I) or a salt thereof, wherein: A is CR 1  or N; B is CR 3  or N; D is CR 4  or N; L 1  is —(CR 7 R 7 ) m —; L 2  is —(CR 7 R 7 ) n —; and X, Z, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6  are define herein. Also disclosed are methods of using such compounds as modulators of TNFα, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Claim (Index 3):
The compound according to  claim 1  or a salt thereof, wherein:\n X is a bond or \u2014NR 8 \u2014; \n L 1  is a bond or \u2014CH 2 ; \n L 2  is a bond, \u2014CH 2 \u2014, \u2014CH(CH 3 )\u2014, \u2014C(CH 3 ) 2 \u2014, \u2014CH(CH 2 F)\u2014, \u2014CH(CHF 2 )\u2014, \u2014CH(CF 3 )\u2014, \u2014CH(CH 2 CH 3 )\u2014, \u2014CH(CH 2 CH 2 F)\u2014, \u2014CH(CH 2 CHF 2 )\u2014, \u2014CH(CH 2 CF 3 )\u2014, \u2014CH(CH 2 CH 2 OH)\u2014, \u2014CH(CH 2 N(CH 3 ) 2 )\u2014, \u2014CH(C(CH 3 ) 2 OH)\u2014, \u2014CH(CH 2 CH\u2550CH 2 )\u2014, \u2014CH(CH 3 )CH 2 \u2014, \u2014CH(cyclopropyl)-, \u2014CH(CH(CH 3 ) 2 )\u2014, \u2014CH(C(CH 3 ) 2 F)\u2014, \u2014CH(CH 3 )CH 2 CH 2 \u2014, \u2014CH(CH 3 )CH 2 C(OH)(phenyl)-, cyclopropyl, or cyclobutyl; \n Z is a cyclic group selected from C 3-6  cycloalkyl, cyclopentenyl, phenyl, furanyl, imidazolyl, indolinyl, isoquinolinyl, isothiazolyl, isoxazolyl, oxazolyl, piperidinyl, pyrazinyl, pyrazolyl, pyridinyl, pyrimidinyl, thiazolyl, and thiophenyl, wherein said cyclic group is substituted with zero to 3 R a ; \n R 1  is H or F; \n R 2  is:\n (i) H, F, Cl, or Br; or \n (ii) dihydropyridinonyl, phenyl, piperidinyl, pyrazinyl, pyrazolyl, pyridinyl, or pyrimidinyl, each substituted with zero to 3 R 1a ; \n \n R 3  is H, F, or Cl; \n R 4  is H, F, or Cl; \n R 5  is H, \u2014OH, \u2014CH 3 , \u2014CH 2 OH, \u2014CH 2 NH 2 , \u2014CH 2 N 3 , \u2014C(O)OH, \u2014C(O)NH(CH 3 ), \u2014C(O)N(CH 3 ) 2 , \u2014C(O)OCH 2 CH 3 , \u2014CH 2 NH(dimethylphenyl), \u2014C(O)NH(pyridinyl), \u2014C(O)NH(phenyl), or \u2014CH 2 O(pyridinyl); \n R 8  is H, \u2014CH 3 , or \u2014CH 2 CH 3 ; \n each R 1a  is independently F, \u2014CN, \u2014CH 3 , \u2014CH 2 CH 3 , \u2014CH 2 OH, \u2014C(CH 3 ) 2 OH, \u2014CH(OH)CH 2 OH, \u2014CH(CH 3 )(OH)CH 2 OH, \u2014C(CH 2 F) 2 OH, \u2014C(CH 3 ) 2 NHC(O)CH 3 , \u2014C(O)NH 2 , \u2014C(O)NHCH 2 CH 2 CH 2 CH 2 NH 2 , \u2014C(O)NHCH 3 , \u2014C(O)OH, \u2014CH(C(O)OCH 3 )CH 2 NH 2 , \u2014CH(CH 2 OH)NHC(O)CH 3 , \u2014CH(NH 2 )CH 2 OH, \u2014CH(NH 2 )CH 2 C(O)OH, \u2014CH 2 CH(NH 2 )C(O)OH, \u2014CH 2 NH(CH 2 CH 3 ), \u2014CH 2 NHC(O)CH 3 , \u2014CH 2 NHC(O)NH 2 , \u2014CH(OH)CH 2 NH(CH 3 ), \u2014NH(CH 3 ), \u2014NHCH 2 CH 2 OH, \u2014NHCH 2 CH(OH)CH 2 OH, \u2014NHCH 2 C(CH 3 ) 2 OH, \u2014NHCH(CH 2 OH) 2 , \u2014NHCH 2 C(O)NH 2 , \u2014NHCH 2 C(O)OH, \u2014NHCH(CH 3 )C(O)NH 2 , \u2014NHCH 2 CH(OH)CH 2 OH, \u2014N(CH 3 )C(O)CH\u2550CH 2 , \u2014OCH 2 CH 3 , \u2014S(O) 2 CH 3 , \u2014S(O) 2 NH(CH 3 ), \u2014CH 2 (azetidinyl), \u2014CH 2 (piperazinyl), \u2014CH 2 (butoxycarbonyl piperazinyl), \u2014CH(OH)(cyclopropyl), \u2014CH(OH)CH 2 (morpholinyl), \u2014CH(OH)CH 2 (carboxypyrrolidinyl), \u2014NH(carbamoylcyclopropyl), C 3-6  cycloalkyl substituted with 1 to 2 substituents independently selected from \u2014OH, \u2014NH 2 , \u2014NHC(O)NH 2 , \u2014NHC(O)CH 3 , \u2014NHCH 2 CH 2 OH, \u2014NHS(O) 2 CH 3 , \u2014CH 2 OH, \u2014C(O)OH, and \u2014C(O)CH 3 ; hydroxybutanonyl, hydroxypyrrolidinyl, carboxypyrrolidinyl, methoxycarbonylpyrrolidinyl, hydroxypropylpyrrolidinyl, hydroxypyranyl, hydroxyoxetanyl, hydroxymethylmorpholinyl, dioxohydroxytetrahydrothiopyranyl, piperidinyl substituted with 1 to 2 substituents independently selected from \u2014NH 2 , \u2014C(O)OH, \u2014CH 2 C(O)OH, \u2014C(CH 3 ) 2 OH, and \u2014C(O)OCH 2 CH 3 ; piperazinyl substituted with zero or 1 substituent selected from \u2014CH 2 OH, \u2014CH 2 CN, \u2014CH 2 C(O)OH, \u2014CH 2 C(O)OCH 3 , \u2014CH 2 C(O)NH 2 , \u2014CH 2 C(O)NHCH 3 , \u2014CH(C(O)OCH 3 )CH 2 NHC(O)CH 3 , \u2014CH(C(O)OH)CH 2 NH 2 , \u2014CH 2 C(O)NHS(O) 2 CH 3 , \u2014CH 2 C(O)NHCH 2 C(O)OH, \u2014CH(C(O)OH)CH 2 NHC(O)CH 3 , \u2014CH(C(O)OH)CH 2 NHC(O)OC(CH 3 ) 3 , \u2014C(O)OH, \u2014C(O)CH(CH 3 )OH, \u2014C(O)CH(NH 2 )CH 2 C(O)OH, \u2014C(O)CH(NH 2 )CH 2 OH, \u2014C(O)CH 2 CH 2 C(O)OH, \u2014C(O)CH\u2550CH 2 , \u2014C(O)C\u2261CH, \u2014CH 2 (tetrazolyl), and pyrrolidinonyl; piperazinonyl, carboxymethylpiperazinonyl, morpholinyl, dioxothiomorpholinyl, carboxy-azabicyclo[3.2.1]octanyl, or pyridinyl; \n each R a  is independently F, Cl, Br, \u2014CN, \u2014OH, \u2014CH 3 , \u2014CH 2 CH 3 , \u2014CH\u2550CH 2 , \u2014C\u2261C(phenyl), \u2014CF 3 , \u2014CH 2 OH, \u2014CH 2 CH 2 OH, \u2014CH(CH 3 )OH, \u2014CH 2 CH 2 CH 2 OH, \u2014C(CH 3 ) 2 OH, \u2014CH(OH)CH 2 OH, \u2014CH 2 CH(OH)CH 2 OH, \u2014C(CH 3 )(OH)CH 2 OH, \u2014CH(OH)CH(CH 3 )CH 2 CH(CH 3 ) 2 , \u2014CH 2 NH 2 , \u2014CH(NH 2 )CH 2 OH, \u2014CH(NH 2 )CH(CH 3 )CH 2 CH 2 CH 3 , \u2014CH 2 C(O)NH 2 , \u2014CH 2 CH 2 C(O)NH 2 , \u2014CH 2 (phenyl), \u2014C(O)CH 3 , \u2014C(O)NH 2 , \u2014C(O)NH(CH 3 ), \u2014C(O)NH(CH 2 CH 3 ), \u2014C(O)N(CH 3 ) 2 , \u2014C(O)CH(CH 3 )CH 2 CH 2 CH 3 , \u2014C(O)(pyrazolyl), \u2014C(O)(pyridinyl), \u2014C(O)NH(phenyl), \u2014C(O)OH, \u2014CH 2 C(O)OH, \u2014CH 2 CH 2 C(O)OH, \u2014C(O)OCH 3 , \u2014C(O)OC(CH 3 ) 3 , \u2014CH\u2550NOH, \u2014OCHF 2 , \u2014OCH 3 , \u2014OCF 3 , \u2014OCH 2 CH 2 OH, \u2014OCH 2 CH 2 CH 2 OH, \u2014OCH 2 C(O)OH, \u2014OCH\u2550CH 2 , \u2014NH 2 , \u2014NHC(O)OC(CH 3 ) 3 , \u2014NHCH(CH 3 )CH 2 CH(CH 3 )CH 3 , \u2014S(O)CH 3 , \u2014S(O) 2 NH 2 , \u2014S(O) 2 CH 2 CH 2 C(O)OCH 3 , S(O) 2 (methylpyrazolyl), oxazolidinonyl, cyclopentenyl, imidazolidine-2,4-dionyl, imidazolinonyl, methylimidazolyl, indolyl, morpholinonyl, morpholinyl, pyrazinyl, pyridazinyl, methylpyridazinyl, dimethoxypyridazinyl, pyrrolidinonyl, pyrrolidinyl, pyrrolo[2,3-b]pyridinyl, tetrahydropyridinyl, tetrazolyl, methyltetrazolyl, thiazolyl, triazolyl, methyltriazolyl, phenyl substituted with zero to 2 substituents independently selected from F, Cl, \u2014CN, \u2014CH 3 , \u2014NH 2 , \u2014OCH 3 , and \u2014OC(O)C(CH 3 ) 3 ; pyrazolyl substituted with zero to 2 substituents independently selected from \u2014CH 3 , \u2014CH 2 CH 3 , \u2014CHF 2 , \u2014CF 3 , \u2014C(O)OH, \u2014CH 2 C(O)OH, \u2014CH 2 C(CH 3 ) 2 OH, \u2014CH 2 (phenyl), and \u2014CH 2 CH 2 (morpholinyl); pyridinyl substituted with zero to 2 substituents independently selected from \u2014CN, \u2014CH 3 , \u2014CH 2 CH 3 , \u2014OCH 3 , \u2014NH 2 , \u2014NH(CH 3 ), \u2014N(CH 3 ) 2 , and \u2014C(O)(morpholinyl); or pyrimidinyl substituted with zero to 1 substituent selected from \u2014CH 3 , \u2014C(CH 3 ) 2 OH, \u2014OCH 3 , \u2014NH 2 , \u2014N(CH 3 ) 2 , cyclopropyl, and morpholinyl.

Metadata:
- Claim Count in Document: 3.0
- Percentile: 88.0
- Lexical Diversity: 2.06897
- Patent Class: 546.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15749611', '15558692', '15558708', '15558724', '14588470']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8450798260421137
- 35 USC 102 Novelty (BERT): 0.552306930172486
- Combined Prediction Score: 0.815802536455151
- Mean Citation Score: 430.14112400000016
- Max Citation Score: 456.6969
- Similarity Product: 311.34429167012576

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

Dataset: test