PATENT CLAIM ANALYSIS

Application Number: 16219735
Application Type: Utility
Filing Date: 2018-12
Publication Date: 2019-08
Patent Classification: ["514", "080000"]

Abstract:
The present disclosure provides MAT2A inhibitor compounds that are useful as therapeutic agents for treating malignancies, and wherein the compounds conform to general formula (IA): wherein R A , R B , R C , R D , and R E  are defined herein.

Claim (Index 46):
A method for:\n treating a disease or condition in a subject suffering therefrom, wherein the disease or condition is mediated by the overexpression of MAT2A, or treating a cancer characterized by a reduction or absence of methylthioadenosine phosphorylase (MTAP) gene expression, the absence of the MTAP gene, or reduced function of MTAP protein, comprising administering to the subject an effective amount of\n a compound according to formula IA or a pharmaceutically acceptable salt thereof: \n wherein\n R A  is selected from the group consisting of H, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 1 -C 6 -alkoxy, C 3 -C 14 -carbocycle, (C 3 -C 14 -carbocyclo)-C 1 -C 6 -alkyl-, 3- to 14-membered heterocycle or heterocyclo-C 1 -C 6 -alkyl- (wherein 1 to 4 heterocycle ring members are heteroatoms selected from N, O, and S), (3- to 14-membered heterocyclo)oxy-, C 6 -C 14 -aryl, (C 6 -C 14 -aryl)-C 1 -C 6 -alkyl-, C 6 -C 14 -aryloxy-, \u2014(CH 2 ) 0-6 NR 1 (CH 2 ) 0-6 C(O)R 2 , NR 1 R 2 , C(O)NR 1 R 2 , NR 1 C(NR 2 )NR 1 R 2 , NR 1 C(NR 2 )(\u2550NR 1 ), SR 1 , \u2014CN, and \u2014OH;\n wherein each alkyl, alkenyl, alkoxy, aryl, and heterocycle is optionally substituted with one or more substituents selected from the group consisting of R 1 , OR 1 , halo, \u2014N\u2550N\u2014R 1 , NR 1 R 2 , \u2014(C 1 -C 6 -alkyl)NR 1 R 2 , \u2014C(O)OR 1 , \u2014C(O)NR 1 R 2 , \u2014OC(O)R 1 , \u2014CN, \u2014OP(O)(OR 1 ) 1-2 , and oxo; \n \n R B  is selected from the group consisting of H, C 2 -C 6 -alkenyl, and C 1 -C 6 -alkyl, wherein R B  is optionally substituted by one or more R 1 ; \n R C , R D , and R E  are independently selected from the group consisting of C 3 -C 14 -carbocycle, C 6 -C 14 -aryl, and 3- to 14-membered heterocycle (wherein 1 to 4 heterocycle ring members are heteroatoms selected from N, O, and S), \n wherein R C , R D , and R E  are optionally substituted with one or more substituents selected from the group consisting of R 1 , \u2014OR 1 , halo, \u2014NR 1 R 2 , \u2014(C 1 -C 6 -alkyl)-NR 1 R 2 , \u2014C(O)OR 1 , \u2014C(O)NR 1 R 2 , \u2014NO 2 , \u2014CN, and oxo; and \n R 1  and R 2  are independently selected from the group consisting of H, D ( 2 H), \u2014CN, \u2014OH, C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, NH 2 , \u2014S(O) 0-2 \u2014(C 1 -C 6 -alkyl), \u2014S(O) 0-2 \u2014(C 6 -C 14 -aryl), \u2014C(O)(C 1 -C 6 -alkyl), \u2014C(O)(C 3 -C 14 -carbocyclo), \u2014C 3 -C 14 -carbocycle, C 6 -C 14 -aryl, 3- to 14-membered heterocycle or heterocyclo(C 1 -C 6 -alkyl)- (wherein 1 to 4 heterocycle ring members are heteroatoms selected from N, O, and S),\n wherein each alkyl, alkoxy, alkenyl, alkynyl, aryl, carbocycle, and heterocycle moiety of R 1  and R 2  is optionally substituted with one or more substituents selected from the group consisting of hydroxy, halo, \u2014NH 2 , \u2014NHC(O)(OC 1 -C 6 -alkyl), \u2014NO 2 , \u2014CN, oxo, \u2014C(O)OH, \u2014C(O)O(C 1 -C 6 -alkyl), \u2014C 1 -C 6 -alkyl(C 1 -C 6 -alkoxy), \u2014C(O)NH 2 , C 1 -C 6 -alkyl, \u2014C(O)C 1 -C 6 -alkyl, \u2014OC 1 -C 6 -alkyl, \u2014Si(C 1 -C 6 -alkyl) 3 , C 6 -C 14 -aryl, \u2014(C 1 -C 6 -alkyl)(C 6 -C 14 -aryl), 3- to 14-membered heterocycle or heterocyclo(C 1 -C 6 -alkyl)- (wherein 1 to 4 heterocycle ring members are heteroatoms selected from N, O, and S), and \u2014O(C 6 -C 14 -aryl),\n wherein each alkyl, aryl, and heterocyclo in R 1  and R 2  is optionally substituted with one or more substituents selected from the group consisting of hydroxy, \u2014OC 1 -C 6 -alkyl, halo, \u2014NH 2 , \u2014(C 1 -C 6 -alkyl)NH 2 , \u2014C(O)OH, CN, and oxo; \n \n \n or\n a compound of formula (I) or a pharmaceutically acceptable salt thereof: \n wherein:\n ring A and ring B are independently a carbocycle or a heterocycle each optionally substituted with one or more substituents selected from the group consisting of hydroxy, halogen, amino, carboxy, CN, oxo, alkyl, alkoxy and alkylamino wherein said alkyl, alkoxy and alkylamino are optionally substituted with hydroxy, halogen, amino, carboxy, CN and oxo; \n ring C is a carbocycle or a heterocycle each optionally substituted with one or more substituents selected from the group consisting of hydroxy, halogen, amino, carboxy, CN, oxo, alkyl, alkoxy and alkylamino wherein said alkyl, alkoxy and alkylamino are optionally substituted with hydroxy, halogen, amino, carboxy, CN and oxo; and \n R 1  is H or alkyl, a carbocycle or a heterocycle each optionally substituted with one or more substituents selected from the group consisting of hydroxy, halogen, amino, NO 2 , CN, oxo, carboxy, alkoxycarbonyl, alkoxyalkyl, aminocarbonyl, alkyl, acyl, alkoxy, alkylamino aryl, aralkyl, heteroaryl, heteroaralkyl, aryloxy, aralkoxy, heteroaryloxy and heteroaralkoxy wherein said alkyl, alkoxy, alkylamino, alkoxycarbonyl, alkoxyalkyl, aminocarbonyl, aryl, aralkyl, heteroaryl, heteroaralkyl, aryloxy, aralkoxy, heteroaryloxy and heteroaralkoxy are optionally substituted with hydroxy, halogen, amino, alkylamino, carboxy, CN or oxo.

Metadata:
- Claim Count in Document: 110.0
- Percentile: 98.0
- Lexical Diversity: 1.32432
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15691408', '14305393', '11487884', '12669843', '14982127']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7697805403979948
- 35 USC 102 Novelty (BERT): 0.5739301699271694
- Combined Prediction Score: 0.7501955033509122
- Mean Citation Score: 379.887276
- Max Citation Score: 539.0189
- Similarity Product: 335.3458557941497

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