PATENT CLAIM ANALYSIS

Application Number: 16172312
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-05
Patent Classification: ["514", "314000"]

Abstract:
The present disclosure is concerned with oxadiazole and thiadiazole analogs that are capable of inhibiting TGF-β and methods of treating cancers such as, for example, multiple myeloma and a hematologic malignancy, and methods of treating fibrotic conditions using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Claim (Index 19):
A method for inhibiting TGF-\u03b2 activity in a subject, the method comprising the step of administering to the subject an effective amount of at least one compound having a structure represented by a formula: wherein n is selected from 1, 2, 3, and 4; wherein q is selected from 0 and 1; wherein X is selected from O and S; wherein R 1  is selected from C1-C8 alkyl and Cy 1 ;\n wherein Cy 1 , when present, is selected from C3-C8 cycloalkyl and aryl and is substituted with 0-4 non-hydrogen groups independently selected from halogen, \u2014NH 2 , C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, C1-C4 alkylamino, and (C1-C4)(C1-C4) dialkylamino; \n wherein R 2  is selected from hydrogen, C1-C4 alkyl, and amine protecting group; wherein R 3  is selected from NR 20a R 20b , NHCOR 21 , and Ar 1 ;\n wherein each of R 20a  and R 20b , when present, is independently selected from hydrogen, C1-C4 alkyl, Cy 2 , and amine protecting group;\n wherein Cy 2 , when present, is selected from C3-C8 cycloalkyl and aryl and is substituted with 0-4 non-hydrogen groups independently selected from halogen, \u2014NH 2 , C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, C1-C4 alkylamino, and (C1-C4)(C1-C4) dialkylamino; \n \n wherein R 21 , when present, is selected from C1-C4 alkyl, cycloalkyl, and heterocycloalkyl and is substituted with 0-4 non-hydrogen groups independently selected from halogen, \u2014NH 2 , C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, C1-C4 alkylamino, and (C1-C4)(C1-C4) dialkylamino; \n wherein Ar 1 , when present, is selected from aryl and heteroaryl and is substituted with 1-4 non-hydrogen groups independently selected from halogen, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, \u2014(CH 2 ) m NH 2 , \u2014(CH 2 ) m (C1-C4 alkylamino), and \u2014(CH 2 ) m [(C1-C4)(C1-C4) dialkylamino], provided that Ar 1 , when present, is substituted with at least one non-hydrogen group selected from \u2014(CH 2 ) m NH 2  and \u2014(CH 2 ) m (C1-C4 alkylamino);\n wherein m is selected from 0 and 1; \n \n wherein each of R 4a  and R 4b  is independently selected from hydrogen and C1-C4 alkyl; or wherein each of R 4a  and R 4b  are optionally covalently bonded together and, together with the intermediate atoms, comprise a 3- to 7-membered cycloalkyl substituted with 0-4 non-hydrogen groups independently selected from halogen, \u2014NH 2 , C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, C1-C4 alkylamino, and (C1-C4)(C1-C4) dialkylamino; wherein each of R 5a  and R 5b  is independently selected from hydrogen, C1-C4 alkyl, and Cy 3 ;\n wherein Cy 3 , when present, is selected from C3-C8 cycloalkyl and aryl and is substituted with 0-4 non-hydrogen groups independently selected from halogen, \u2014NH 2 , C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, C1-C4 alkylamino, and (C1-C4)(C1-C4) dialkylamino; \n wherein R 6  is selected from C1-C4 alkyl and Cy 4 ; and\n wherein Cy 4 , when present, is selected from C3-C8 cycloalkyl, C2-C7 heterocycloalkyl, aryl, and heteroaryl and is substituted with 0-4 non-hydrogen groups independently selected from halogen, \u2014NH 2 , C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, C1-C4 alkoxyhaloalkyl, C1-C4 alkylamino, and (C1-C4)(C1-C4) dialkylamino, \n or a pharmaceutically acceptable salt thereof, thereby inhibiting TGF-\u03b2 activity in the subject.

Metadata:
- Claim Count in Document: 17.0
- Percentile: 97.0
- Lexical Diversity: 1.41176
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15892302', '14913266', '14380659', '13974858', '15039763']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8117834358231442
- 35 USC 102 Novelty (BERT): 0.5818044696130451
- Combined Prediction Score: 0.7887855392021343
- Mean Citation Score: 518.051642
- Max Citation Score: 573.8161
- Similarity Product: 363.5527095333457

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