PATENT CLAIM ANALYSIS

Application Number: 15890436
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-06
Patent Classification: ["544", "236000"]

Abstract:
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

Claim (Index 1):
A compound of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt thereof, wherein:\n M is N; \n L is selected from \u2014CR 4 R 4 C(O)\u2014, \u2014OC(O)\u2014, \u2014NR 6 C(O)\u2014, and \u2014NR 6 \u2014; \n R 1  is selected from NR 5 R 5 , C 3-10  carbocycle and 4- to 15-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p ; wherein said carbocycle and heterocycle are substituted with 1-4 R 7 ; \n R 2 , at each occurrence, is independently selected from halogen, C 1-6  alkyl, C 1-4  alkoxy, C 1-4  alkylthio, C 1-4  haloalkyl, \u2014OH, \u2014CH 2 OH, \u2014OCH 2 F, \u2014OCHF 2 , \u2014OCF 3 , CN, \u2014NH 2 , \u2014NH(C 1-4  alkyl), \u2014N(C 1-4  alkyl) 2 , \u2014CO 2 H, \u2014CH 2 CO 2 H, \u2014CO 2 (C 1-4  alkyl), \u2014CO(C 1-4  alkyl), \u2014CH 2 NH 2 , \u2014CONH 2 , \u2014CONH(C 1-4  alkyl), \u2014CON(C 1-4  alkyl) 2 , \u2014OCH 2 CO 2 H, \u2014NHCO(C 1-4  alkyl), \u2014NHCO 2 (C 1-4  alkyl), \u2014NHSO 2 (C 1-4  alkyl), \u2014SO 2 NH 2 , \u2014C(\u2550NH)NH 2 , carbocycle, and heterocycle, wherein said alkyl, alkoxy, alkylthio, haloalkyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ; \n R 3 , at each occurrence, is independently selected from halogen, C 1-6  alkyl, C 1-4  alkoxy, C 1-4  alkylthio, C 1-4  haloalkyl, \u2014CH 2 OH, \u2014OCH 2 F, \u2014OCHF 2 , \u2014OCF 3 , CN, \u2014NH 2 , \u2014NH(C 1-4  alkyl), \u2014N(C 1-4  alkyl) 2 , \u2014CO 2 H, \u2014CH 2 CO 2 H, \u2014CO 2 (C 1-4  alkyl), \u2014CO(C 1-4  alkyl), \u2014CH 2 NH 2 , \u2014CONH 2 , \u2014CONH(C 1-4  alkyl), \u2014CON(C 1-4  alkyl) 2 , \u2014OCH 2 CO 2 H, \u2014NHCO(C 1-4  alkyl), \u2014NHCO 2 (C 1-4  alkyl), \u2014NHSO 2 (C 1-4  alkyl), \u2014SO 2 NH 2 , \u2014C(\u2550NH)NH 2 , carbocycle, and heterocycle, wherein said alkyl, alkoxy, alkylthio, haloalkyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ; \n R 4 , at each occurrence, is independently selected from H, OH, NH 2 , CH 2 NH 2 , C 1-4  haloalkyl, OCH 2 F, OCHF 2 , OCF 3 , \u2014NH(C 1-4  alkyl), \u2014N(C 1-4  alkyl) 2 , C 1-4  alkoxy, CH 2 OH, CH 2 O(C 1-4  alkyl), CH 2 CO 2 H, CH 2 CO 2 (C 1-4  alkyl), C 1-4  alkyl, carbocycle, and heterocycle, wherein said alkyl, alkoxy, haloalkyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ; \n R 5 , at each occurrence, is independently selected from H, C 1-4  alkyl, \u2014(CR 6 R 6 ) n \u2014C 3-10  carbocycle and \u2014(CR 6 R 6 ) n -4-10 membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p , wherein said alkyl, carbocycle and heterocycle are substituted with 1-4 R 7 ; \n alternatively, R 5  and R 5  are taken together with the nitrogen atom to which they are attached to form 4- to 15-membered heterocycle substituted with 1-4 R 7 ; \n R 6 , at each occurrence, is independently selected from H and C 1-4  alkyl; \n R 7 , at each occurrence, is independently selected from H, \u2550O, NO 2 , halogen, C 1-4  alkyl, C 1-4  alkoxy, CN, OH, CF 3 , \u2014(CH 2 ) n \u2014CO 2 H, \u2014(CH 2 ) n \u2014CO 2 (C 1-4  alkyl), \u2014(CH 2 ) n \u2014NR 8 R 8 , \u2014NHCO(C 1-4  alkyl), \u2014NHCOCF 3 , \u2014NHCO 2 (C 1-4  alkyl), \u2014NHCO 2 (CH 2 ) 2 O (C 1-4  alkyl), \u2014NHCO 2 (CH 2 ) 3 O (C 1-4  alkyl), \u2014NHCO 2 (CH 2 ) 2 OH, \u2014NHCO 2 (CH 2 ) 2 NH 2 , \u2014NHCO 2 (CH 2 ) 2 N(C 1-4  alkyl) 2 , \u2014NHCO 2 CH 2 CO 2 H, \u2014CH 2 NHCO 2 (C 1-4  alkyl), \u2014NHC(O)NR 8 R 8 , \u2014NHSO 2 (C 1-4  alkyl), \u2014SO 2 NH 2 , \u2014SO 2 NH(C 1-4  alkyl), \u2014SO 2 N(C 1-4  alkyl) 2 , \u2014SO 2 NH(CH 2 ) 2 OH, \u2014SO 2 NH(CH 2 ) 2 O (C 1-4  alkyl), \u2014(CH 2 ) n \u2014CONR 8 R 8 , \u2014O(CH 2 ) n -carbocycle, \u2014O(CH 2 ) n -heterocycle, \u2014NHCO-carbocycle, \u2014NHCO-heterocycle, \u2014(CH 2 ) n -carbocycle, and \u2014(CH 2 ) n -heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NR 8 , O, and S(O) p , wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ; \n R 8 , at each occurrence, is independently selected from H, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, \u2014(CH 2 ) n \u2014C(O)C 1-4 alkyl, \u2014(CH 2 ) n \u2014C(O)carbocycle, \u2014(CH 2 ) n \u2014C(O)heterocycle, \u2014(CH 2 ) n \u2014C(O)NR a R a , \u2014(CH 2 ) n \u2014C(O)O-alkyl, \u2014(CH 2 ) n \u2014C(O)O-carbocycle, \u2014(CH 2 ) n \u2014C(O)O-heterocycle, \u2014(CH 2 ) n \u2014SO 2 alkyl, \u2014(CH 2 ) n  SO 2 carbocycle, \u2014(CH 2 ) n \u2014SO 2 heterocycle, \u2014(CH 2 ) n \u2014SO 2 NR a R a , \u2014(CH 2 ) n -carbocycle, and \u2014(CH 2 ) n -heterocycle, wherein said alkyl, alkenyl, alkynyl, carbocycle, and heterocycle are substituted with 0-4 R 9 ; \n alternatively, R 8  and R 8  are taken together with the nitrogen atom to which they are attached to form 4- to 10-membered heterocycle substituted with 0-4 R 9 ; \n R 9 , at each occurrence, is independently selected from halogen, OH, NO 2 , CHF 2 , CF 3 , C 1-4  alkyl, C 1-4  alkoxy, CH 2 OH, CO(C 1-4  alkyl), CO 2 H, CO 2 (C 1-4  alkyl), \u2014(CH 2 ) n NR a R a , \u2014(CH 2 ) n CONR a R a , \u2014O(CH 2 ) n carbocycle, \u2014O(CH 2 ) n heterocycle, \u2014O(CH 2 ) n NR a R a , \u2014(CR 10 R 10 ) n -4-10 membered heterocycle, wherein said alkyl, alkoxyl, carbocycle, and heterocycle are substituted with 0-4 R b ; \n R 10  is selected from H and C 1-4  alkyl; \n R a , at each occurrence, is independently selected from H, C 1-4  alkyl, \u2014(CH 2 ) n OH, CO(C 1-4  alkyl), COCF 3 , CO 2 (C 1-4  alkyl), \u2014CONH 2 , \u2014CONH\u2014C 1-4  alkylene-CO 2 (C 1-4  alkyl), C 1-4  alkylene-CO 2 (C 1-4  alkyl), R c , CO 2 R c , and CONHR c ; alternatively, R a  and R a  are taken together with the nitrogen atom to which they are attached to form 4- to 10-membered heterocycle, wherein said alkyl, alkylene, and heterocycle are substituted with 0-4 R b ; \n R b , at each occurrence, is independently selected from \u2550O, OH, halogen, C 1-4  alkyl, C 1-4  alkoxy, OCF 3 , NH 2 , NO 2 , N(C 1-4  alkyl) 2 , CO(C 1-4  alkyl), CO(C 1-4  haloalkyl), CO 2 (C 1-4  alkyl), CONH 2 , \u2014CONH(C 1-4  alkyl), \u2014CON(C 1-4  alkyl) 2 , \u2014CONH\u2014C 1-4  alkylene-O(C 1-4  alkyl), \u2014CONH\u2014C 1-4  alkylene-N(C 1-4  alkyl) 2 , \u2014CONH\u2014C 1-4  alkylene-N (C 1-4  alkyl) 2 , \u2014C 1-4  alkylene-O\u2014P(O)(OH) 2 , \u2014NHCO 2 (C 1-4  alkyl), \u2014R c , COR c , CO 2 R c , and CONHR c ; \n R c , at each occurrence, is independently selected from \u2014(CH 2 ) n \u2014C 3-6  cycloalkyl, \u2014(CH 2 ) n -phenyl, and \u2014(CH 2 ) n -5- to 6-membered heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NH, N(C 1-4  alkyl), O, and S(O) p ; wherein each ring moiety is substituted with 0-2 R d ; \n R d , at each occurrence, is independently selected from \u2550O, halogen, \u2014OH, C 1-4  alkyl, NH 2 , NH(C 1-4  alkyl), N(C 1-4  alkyl) 2 , C 1-4  alkoxy, and \u2014NHCO(C 1-4  alkyl), and heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of: N, NH, N(C 1-4  alkyl), O, and S(O) p ; \n n, at each occurrence, is independently selected from 0, 1, 2, 3, and 4; \n p, at each occurrence, is independently selected from 0, 1, and 2; \n provided\n when L is NHC(O), R 1  is other than \n wherein X is N or a substituted or unsubstituted carbon atom;\n when L is NR 6 , R 1  is heterocycle substituted with 1-4 R 7 ;

Metadata:
- Claim Count in Document: 32.0
- Percentile: 88.0
- Lexical Diversity: 1.30909
- Patent Class: 544.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14759495', '14157564', '14797414', '16067619', '15503419']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8114803900048508
- 35 USC 102 Novelty (BERT): 0.6374426808715803
- Combined Prediction Score: 0.7940766190915238
- Mean Citation Score: 541.344386
- Max Citation Score: 598.7151
- Similarity Product: 575.3909559817673

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