PATENT CLAIM ANALYSIS

Application Number: 15758045
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-09
Patent Classification: ["514", "229800"]

Abstract:
A genus of arylsulfonamide derivatives of heterocyclic constrained tricyclic compounds is disclosed. The compounds are of the following genus: The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a therapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.

Claim (Index 1):
A compound of formula I: wherein:\n D is selected from a direct bond, \u2014O\u2014, \u2014CH 2 O\u2014, \u2014OCH 2 \u2014, \u2014C(\u2550O)NR D \u2014, and \u2014N(R D )C(\u2550O)\u2014; \n R D  is selected from hydrogen and (C 1 -C 6 )alkyl; \n T is a benzene ring or a five- or six-membered heteroaromatic ring; \n U is a benzene ring or a five- or six-membered heteroaromatic ring; \n X 1 , X 2 , X 3 , and X 4  are independently selected in each instance from hydrogen, halogen, nitro, cyano, (C 1 -C 6 )alkyl, (C 1 -C 6 )haloalkyl, (C 1 -C 6 )haloalkoxy, (C 1 -C 6 )haloalkylthio, \u2014NR 1 R 2 , \u2014C(O)R 1 , \u2014OC(O)R 1 , \u2014C(O)NR 1 R 2 , \u2014C(O)OR 1 , \u2014SO 2 R 1 , and \u2014SO 2 NR 1 R 2 ; \n R 1  and R 2  are independently selected in each instance from the group consisting of hydrogen and (C 1 -C 6 )alkyl; \n Q is selected from \u2014O\u2014, S(O) n \u2014, and \u2014NR\u2014; \n n is zero, 1 or 2; \n R is selected from hydrogen, optionally substituted (C 1 -C 6 )alkyl, (C 3 -C 7 )cycloalkyl, aryl, or heteroaryl; \u2014SO 2 R 3 ; \u2014SO 2 N(R 3 R 4 ); \u2014C(\u2550O)R 5 ; \u2014C(\u2550O)OR 5 ; or \u2014C(\u2550O)N(R 3 R 4 ); wherein said substituents on the (C 1 -C 6 )alkyl, (C 3 -C 7 )cycloalkyl, aryl, or heteroaryl are selected from the group consisting of hydroxy, halogen, cyano, nitro, amino, (C 1 -C 4 )alkylamino, (C 1 -C 4 )dialkylamino, (C 1 -C 4 )acylamino, (C 1 -C 4 )alkylsulfonyl, (C 1 -C 4 )alkylthio, (C 1 -C 4 )alkyl, (C 3 -C 7 )cycloalkyl, (C 1 -C 4 )haloalkyl, (C 1 -C 4 )haloalkoxy, and (C 1 -C 4 )alkoxy; \n R 3  and R 4  are independently selected in each instance from hydrogen, (C 1 -C 6 )alkyl, aryl, and arylalkyl, wherein said aryl or the aryl of the arylalkyl is optionally substituted with hydroxy, halogen, cyano, nitro, amino, (C 1 -C 4 )alkylamino, (C 1 -C 4 )dialkylamino, (C 1 -C 4 )acylamino, (C 1 -C 4 )alkylsulfonyl, (C 1 -C 4 )alkylthio, (C 1 -C 4 )alkyl, (C 1 -C 4 )haloalkyl, (C 1 -C 4 )haloalkoxy, or (C 1 -C 4 )alkoxy; \n R 5  is selected from hydrogen, optionally substituted (C 1 -C 4 )alkyl, or optionally substituted aryl, wherein said optional substituents are selected from the group consisting of (C 1 -C 3 )alkyl, OR 1 , NH 2 , NHMe, N(Me) 2 , and heterocycle; \n Y is selected from hydrogen or hydroxyl; \n V is selected from phenyl, a six-membered heteroaromatic ring, furan, and thiophene; \n Z 1  and Z 2  are independently selected in each instance from the group consisting of hydrogen, halogen, nitro, cyano, azide, (C 1 -C 6 )alkyl, (C 1 -C 6 )haloalkyl, (C 1 -C 6 )haloalkoxy, \u2014(C 1 -C 6 )haloalkylthio, \u2014NR 1 R 2 , \u2014NR 1 C(O)R 2 , \u2014NR 1 C(O)OR 6 , \u2014C(O)R 1 , \u2014OC(O)R 1 , \u2014C(O)NR 1 R 2 , \u2014C(O)OR 1 , \u2014SO 2 R 1 , and \u2014SO 2 NR 1 R 2 ; and \n R 6  is (C 1 -C 8 )hydrocarbon.

Metadata:
- Claim Count in Document: 46.0
- Percentile: 90.0
- Lexical Diversity: 1.42105
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15758038', '15124891', '15750388', '12041860', '11862690']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8287182760226419
- 35 USC 102 Novelty (BERT): 0.5521317903166701
- Combined Prediction Score: 0.8010596274520447
- Mean Citation Score: 340.52525
- Max Citation Score: 418.73618
- Similarity Product: 370.5963906448936

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

Dataset: test