PATENT CLAIM ANALYSIS

Application Number: 15999117
Application Type: Utility
Filing Date: 2018-08
Publication Date: 2019-02
Patent Classification: ["424", "001890"]

Abstract:
Provided herein are monoacylglycerol lipase (MGLL) occupancy probes comprising a MGLL inhibitor containing a positron emission tomography (PET) tracer radionuclide. Also provided are methods of assessing MGLL enzyme occupancy of a MGLL inhibitor using the radiolabeled occupancy probes described herein.

Claim (Index 7):
The radiolabeled MGLL occupancy probe of  claim 6 , wherein the MGLL inhibitor has the structure of Formula (Ia): wherein p is 0, 1, or 2; R d  is selected from the group consisting of: H and C 1-6 alkyl; L 3  is a bond, \u2014CH 2 \u2014, \u2014S(O) 2 \u2014, or \u2014C(O)\u2014; R 7  is selected from the group consisting of: H, phenyl, naphthyl, mono or bicyclic heteroaryl, and mono or bicyclic heterocyclyl, wherein the heteroaryl or the heterocyclyl has 1, 2 or 3 heteroatoms independently selected from O, S, and N; wherein R 7  is optionally substituted by one, two, three, or four moieties independently selected from R h ; R a  and R b  may be independently selected, for each occurrence, from the group consisting of hydrogen and C 1-3 alkyl; wherein C 1-3 alkyl may optionally be substituted by one or more substituents selected from halogen, cyano, oxo, hydroxyl, heterocycle, and phenyl; or R a  and R b , when they occur together with the nitrogen to which they are attached, form a 4-6 membered heterocyclic ring or a 9-10 membered bicyclic heterocycle or spirocyclic ring, which may have an additional heteroatom selected from O, S, and N; wherein the 4-6 membered heterocyclic ring or 9-10 membered bicyclic heterocycle or spirocycle may optionally be substituted by one or more substituents selected from the group consisting of halogen, cyano, oxo, C 1-6 alkyl, C 1-6 haloalkyl, \u2014S(O) w \u2014C 1-6 alkyl (where w is 0, 1, or 2), hydroxyl, \u2014C(O)\u2014C 1-6 alkyl, \u2014NH 2 , and \u2014NH\u2014C(O)\u2014C 1-6 alkyl; R c  is selected from the group consisting of halogen, cyano, hydroxyl, nitro, C 1-6 alkyl (optionally substituted by one, two, or three halogens, cyano, or hydroxyl), C 2-6 alkenyl (optionally substituted by one, two, or three halogens), C 2-6 alkynyl (optionally substituted by one, two, or three halogens), C 3-6 cycloalkyl, C 1-6 alkoxy (optionally substituted by one, two, or three halogens), R a R b N\u2014, R a R b N\u2014SO 2 \u2014, R a R b N\u2014C(O)\u2014, R a \u2014C(O)\u2014NR a \u2014, R a \u2014C(O)\u2014, R a \u2014S(O) w \u2014NR b \u2014 (wherein w is 0, 1, or 2), and R a \u2014S(O) w \u2014 (wherein w is 0, 1, or 2); and R h  is selected from the group consisting of: halogen, phenyl (optionally substituted by one, two, or three moieties each independently selected from R c ), phenyloxy (optionally substituted by one, two, or three moieties each independently selected from R c ), hydroxyl, cyano, C 1-6 alkyl (optionally substituted by cyano, hydroxyl, or one, two, or three halogens), C 2-6 alkenyl (optionally substituted by cyano, hydroxyl, or one, two, or three halogens), C 2-6 alkynyl (optionally substituted by cyano, hydroxyl, or one, two, or three halogens), C 1-6  alkoxy (optionally substituted by cyano, hydroxyl, or one, two, or three halogens), R a R b N\u2014, R a \u2014C(O)NR a \u2014, R a R b N\u2014SO 2 \u2014, R a R b N\u2014C(O)\u2014, R a \u2014S(O) w \u2014 (wherein w is 0, 1, or 2), R a \u2014SO 2 \u2014NR b \u2014, heteroaryl (optionally substituted by one, two, or three moieties each independently selected from R c , and connected to R 7  through a carbon or heteroatom), heterocycle (optionally substituted by one, two, or three moieties each independently selected from R c , and connected to R 7  through a carbon or heteroatom), and heteroaryloxy (optionally substituted by one, two, or three moieties each independently selected from R c ), or two adjacent R h  groups, along with the carbons to which they are attached, can be taken together to form a 5- or 6-member heterocyclic or heteroaryl ring optionally substituted with 0, 1 or 2 halogens selected from F or Cl and which may have one or two additional heteroatoms selected from O, S, and N; or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof.

Metadata:
- Claim Count in Document: 53.0
- Percentile: 96.0
- Lexical Diversity: 1.48387
- Patent Class: 424.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['13043956', '13479826', '14003547', '14764426', '13391402']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7697826509956889
- 35 USC 102 Novelty (BERT): 0.5085448129831085
- Combined Prediction Score: 0.7436588671944309
- Mean Citation Score: 262.048626
- Max Citation Score: 265.28232
- Similarity Product: 172.67114110160355

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