PATENT CLAIM ANALYSIS

Application Number: 16117203
Application Type: Utility
Filing Date: 2018-08
Publication Date: 2019-01
Patent Classification: ["546", "294000"]

Abstract:
The present invention provides for compounds of formula (I) wherein Y 1 , Y 2 , R 1 , R 2 , R 3 , A 1 , A 2 , A 3 , and A 4 , have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

Claim (Index 27):
A method for treating a disease or condition in a subject comprising administering a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein\n R 1  is C 1 -C 3  alkyl or C 1 -C 3  haloalkyl; \n R 2  is H; \n R 3  is \u2014O\u2014C 1 -C 6  alkyl, \u2014OCD 2 CH 3 , or \u2014OCD 2 CD 3 ; \n Y 1  is N or CR 4 , wherein R 4  is H, C 1 -C 3  alkyl, or C 1 -C 3  haloalkyl; \n A 2  is CR 5 , and A 1 , A 3 , and A 4  are CR 6 ; or \n A 2  is CR 5 , A 1  and A 3  are CR 6 , and A 4  is N; \n R 5  is \u2014N(R 5d )\u2014C 1 -C 6  alkylenyl-R 5a , \u2014N(R 5d )C(O)\u2014C 1 -C 6  alkylenyl-R 5b , \u2014N(R 5d )SO 2 \u2014C 1 -C 6  alkylenyl-R 5c , \u2014N(R 5d )C(O)N(R 5d )-G 1 , \u2014N(R 5d )C(O)N(R 5d )\u2014C 1 -C 6  alkylenyl-R 5a , \u2014N(R 5d )SO 2 N(R d )\u2014C 1 -C 6  alkylenyl-R a , \u2014C(O)N(R 5d )\u2014C 1 -C 6  alkylenyl-R 5a , or \u2014SO 2 N(R 5d )\u2014C 1 -C 6  alkylenyl-R 5a ,\n wherein \n R 5a , at each occurrence, is independently G 1 , \u2014OR 5aa , \u2014OC(O)R 5dd , \u2014SR 5aa , \u2014S(O)R 5aa , \u2014SO 2 R 5aa , \u2014SO 2 NR 5bb R 5cc , \u2014NR 5bb R 5cc , \u2014NR 5bb C(O)R 5dd , \u2014NR 5bb SO 2 R 5dd , \u2014NR 5bb C(O)OR 5dd , \u2014NR 5bb C(O)NR 5bb R 5cc , \u2014NR 5bb SO 2 NR 5bb R 5cc , \u2014C(O)R 5aa , \u2014C(O)OR 5aa  or \u2014C(O)NR 5bb R 5cc , \n R 5b  is G 1 , \u2014OR 5aa , \u2014OC(O)R 5dd , \u2014SR 5aa , \u2014S(O)R 5aa , \u2014SO 2 R 5aa , \u2014SO 2 NR 5bb R 5cc , \u2014N(R 5bb )(G 1 ), \u2014NR 5bb (C 1 -C 6  alkylenyl)-G 1 , \u2014NR 5bb C(O)R 5dd , \u2014NR 5bb SO 2 R 5dd , \u2014NR 5bb C(O)OG 1 , \u2014NR 5bb C(O)O\u2014(C 1 -C 6  alkylenyl)-G 1 , \u2014NR 5bb C(O)NR 5bb R 5cc , \u2014NR 5bb SO 2 NR 5bb R 5cc , \u2014C(O)R 5a , \u2014C(O)OR 5aa  or \u2014C(O)NR 5bb R 5cc , \n R 5c  is \u2014OR 5aa , \u2014OC(O)R 5dd , \u2014SR 5aa , \u2014S(O)R 5a , \u2014SO 2 R 5aa , \u2014SO 2 NR 5bb R 5cc , \u2014NR 5bb R 5cc , \u2014NR 5bb C(O)R 5dd , \u2014NR 5bb SO 2 R 5dd , \u2014NR 5bb C(O)OR 5dd , \u2014NR 5bb C(O)NR 5bb R 5cc , \u2014NR 5bb SO 2 NR 5bb R 5cc , \u2014C(O)R 5aa , \u2014C(O)OG 1 , \u2014C(O)O\u2014(C 1 -C 6  alkylenyl)-G 1 , or \u2014C(O)NR 5bb R 5cc , \n R 5d , at each occurrence, is independently H, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 1 -C 6  haloalkyl, G 1 , \u2014OR 5aa , \u2014OC(O)R 5dd , \u2014SR 5aa , \u2014S(O)R 5aa , \u2014SO 2 R 5aa , \u2014SO 2 NR 5bb R 5cc , \u2014NR 5bb R 5cc , \u2014NR 5bb C(O)R 5dd , \u2014NR 5bb SO 2 R 5dd , \u2014NR 5bb C(O)OR 5dd , \u2014NR 5bb C(O)NR 5bb R 5cc , \u2014NR 5bb SO 2 NR 5bb R 5cc , \u2014C(O)R 5aa , \u2014C(O)OR 5aa , \u2014C(O)NR 5bb R 5cc , \u2014(C 1 -C 6  alkylenyl)-G 1 , \u2014(C 1 -C 6  alkylenyl)-OR 5aa , \u2014(C 1 -C 6  alkylenyl)-OC(O)R 5dd , \u2014(C 1 -C 6  alkylenyl)-SR 5aa , \u2014(C 1 -C 6  alkylenyl)-S(O)R 5aa , \u2014(C 1 -C 6  alkylenyl)-SO 2 R 5aa , \u2014(C 1 -C 6  alkylenyl)-SO 2 NR 5bb R 5cc , \u2014(C 1 -C 6  alkylenyl)-NR 5bb R 5cc , \u2014(C 1 -C 6  alkylenyl)-NR 5bb C(O)R 5dd , \u2014(C 1 -C 6  alkylenyl)-NR 5bb SO 2 R 5dd , \u2014(C 1 -C 6  alkylenyl)-NR 5bb C(O)OR 5dd , \u2014(C 1 -C 6  alkylenyl)-NR 5bb C(O)NR 5bb R 5cc , \u2014(C 1 -C 6  alkylenyl)-NR 5bb SO 2 NR 5bb R 5cc , \u2014(C 1 -C 6  alkylenyl)-C(O)R 5aa , \u2014(C 1 -C 6  alkylenyl)OC(O)OR 5aa , or \u2014(C 1 -C 6  alkylenyl)OC(O)NR 5bb R 5cc ; \n \n R 6  is H, C 1 -C 6  alkyl, halogen, C 1 -C 6  haloalkyl, or \u2014CN; \n R 5aa , R 5bb , and R 5cc , at each occurrence, are each independently H, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 1 -C 6  haloalkyl, G 1 , or \u2014(C 1 -C 6  alkylenyl)-G 1 ; \n R 5dd , at each occurrence, is independently C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 1 -C 6  haloalkyl, G 1 , or \u2014(C 1 -C 6  alkylenyl)-G 1 ; \n G 1 , at each occurrence, is independently aryl, heteroaryl, heterocycle, cycloalkyl, or cycloalkenyl, each of which is optionally substituted with 1, 2, 3, 4, or 5 R 1g  groups, \n Y 2  is -L-G 2 ; wherein\n L is O or N(R x ) wherein R x  is H or C 1 -C 6  alkyl; \n G 2  is aryl, heteroaryl, heterocycle, cycloalkyl, or cycloalkenyl, each of which is optionally substituted with 1, 2, 3, 4, or 5 R 2g  groups; \n \n R 1g  and R 2g , at each occurrence, are each independently oxo, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, halogen, C 1 -C 6  haloalkyl, \u2014CN, NO 2 , \u2014OR z1 , \u2014OC(O)R z2 , \u2014OC(O)NR z3 R z4 , \u2014SR z1 , \u2014S(O) 2 R z1 , \u2014S(O) 2 NR z3 R z4 , \u2014C(O)R z1 , \u2014C(O)OR z1 , \u2014C(O)NR z3 R z4 , \u2014NR z3 R z4 , \u2014N(R z3 )C(O)R z2 , \u2014N(R z3 )S(O) 2 R z2 , \u2014N(R z3 )C(O)O(R z2 ), \u2014N(R z3 )C(O)NR z3 R z4 , \u2014N(R z3 )S(O) 2 NR z3 R z4 , G 3 , \u2014(C 1 -C 6  alkylenyl)-CN, \u2014(C 1 -C 6  alkylenyl)-OR z1 , \u2014(C 1 -C 6  alkylenyl)-OC(O)R z2 , \u2014(C 1 -C 6  alkylenyl)-OC(O)NR z3 R z4 , \u2014(C 1 -C 6  alkylenyl)-S(O) 2 R z1 , \u2014(C 1 -C 6  alkylenyl)-S(O) 2 NR z3 R z4 , \u2014(C 1 -C 6  alkylenyl)-C(O)R z1 , \u2014(C 1 -C 6  alkylenyl)-C(O)OR z1 , \u2014(C 1 -C 6  alkylenyl)-C(O)NR z3 R z4 , \u2014(C 1 -C 6  alkylenyl)-NR z3 R z4 , \u2014(C 1 -C 6  alkylenyl)-N(R z3 )C(O)R z2 , \u2014(C 1 -C 6  alkylenyl)-N(R z3 )S(O) 2 R z2 , \u2014(C 1 -C 6  alkylenyl)-N(R z3 )C(O)O(R z2 ), \u2014(C 1 -C 6  alkylenyl)-N(R z3 )C(O)NR z3 R z4 , \u2014(C 1 -C 6  alkylenyl)-N(R z3 )S(O) 2 NR z3 R z4 , \u2014(C 1 -C 6  alkylenyl)-CN, or \u2014(C 1 -C 6  alkylenyl)-G 3 ; \n R z1 , R z3 , and R z4 , at each occurrence, are each independently H, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 1 -C 6  haloalkyl, G 3 , or \u2014C 1 -C 6  alkylenyl-G 3 ; \n R z2 , at each occurrence, is independently C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, C 1 -C 6  haloalkyl, G 3 , or \u2014C 1 -C 6  alkylenyl-G 3 ; \n G 3  is aryl, heteroaryl, heterocycle, cycloalkyl, or cycloalkenyl, each of which is optionally substituted with 1, 2, 3, 4, or 5 R 3g  groups, \n R 3g , at each occurrence, is independently oxo, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, halogen, C 1 -C 6  haloalkyl, \u2014CN, NO 2 , \u2014OR a , \u2014OC(O)R b , \u2014OC(O)NR c R d , \u2014SR a , \u2014S(O) 2 R a , \u2014S(O) 2 NR c R d , \u2014C(O)R a \u2014C(O)OR a , \u2014C(O)NR c R d , \u2014NR c R d , \u2014N(R c )C(O)R b , \u2014N(R c )S(O) 2 R b , \u2014N(R c )C(O)O(R b ), \u2014N(R c )C(O)NR c R d , \u2014N(R c )S(O) 2 NR c R d , \u2014(C 1 -C 6  alkylenyl)-CN, \u2014(C 1 -C 6  alkylenyl)-OR a , \u2014(C 1 -C 6  alkylenyl)-OC(O)R b , \u2014(C 1 -C 6  alkylenyl)-OC(O)NR c R d , \u2014(C 1 -C 6  alkylenyl)-S(O) 2 R a , \u2014(C 1 -C 6  alkylenyl)-S(O) 2 NR c R d , \u2014(C 1 -C 6  alkylenyl)-C(O)R a , \u2014(C 1 -C 6  alkylenyl)-C(O)OR a , \u2014(C 1 -C 6  alkylenyl)-C(O)NR c R d , \u2014(C 1 -C 6  alkylenyl)-NR c R d , \u2014(C 1 -C 6  alkylenyl)-N(R c )C(O)R b , \u2014(C 1 -C 6  alkylenyl)-N(R c )S(O) 2 R b , \u2014(C 1 -C 6  alkylenyl)-N(R c )C(O)O(R b ), \u2014(C 1 -C 6  alkylenyl)-N(R c )C(O)NR c R d , \u2014(C 1 -C 6  alkylenyl)-N(R c )S(O) 2 NR c R d , or \u2014(C 1 -C 6  alkylenyl)-CN, \n R a , R c , and R d , at each occurrence, are each independently H, C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, or C 1 -C 6  haloalkyl, and \n R b , at each occurrence, is independently C 1 -C 6  alkyl, C 2 -C 6  alkenyl, C 2 -C 6  alkynyl, or C 1 -C 6  haloalkyl,\n wherein said disease or condition is selected from the group consisting of Addison's disease, acute gout, ankylosing spondylitis, asthma, atherosclerosis, Behcet's disease, bullous skin diseases, cardiac myopathy, chronic obstructive pulmonary disease (COPD), Crohn's disease, dermatitis, eczema, giant cell arteritis, glomerulonephritis, heart failure, hepatitis, hypophysitis, inflammatory bowel disease), Kawasaki disease, lupus nephritis, multiple sclerosis, myocarditis, myositis, nephritis, organ transplant rejection, osteoarthritis, pancreatitis, pericarditis, Polyarteritis nodosa, pneumonitis, primary biliary cirrhosis, psoriasis, psoriatic arthritis, rheumatoid arthritis, scleritis, sclerosing cholangitis, sepsis systemic lupus erythematosus, Takayasu's Arteritis, toxic shock, thyroiditis, type I diabetes, ulcerative colitis, uveitis, vitiligo, vasculitis, and Wegener's granulomatosis.

Metadata:
- Claim Count in Document: 20.0
- Percentile: 96.0
- Lexical Diversity: 1.79245
- Patent Class: 546.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['14564352', '15216855', '14206028', '14774866', '14203651']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.84599064068665
- 35 USC 102 Novelty (BERT): 0.6420686749592297
- Combined Prediction Score: 0.8255984441139079
- Mean Citation Score: 536.555558
- Max Citation Score: 663.77985
- Similarity Product: 581.1769394570142

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