PATENT CLAIM ANALYSIS

Application Number: 15765232
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-10
Patent Classification: ["548", "400000"]

Abstract:
Disclosed are compounds based on dolastatins, drug-conjugates, methods of preparing drug-conjugates, and uses thereof. Also disclosed are pharmaceutical compositions and methods of treatment. The compounds and drug-conjugates disclosed herein can be used to treat diseases such as bladder cancer, breast cancer, colon cancer, rectal cancer, endometrial cancer, kidney cancer, lung cancer, melanoma, non-Hodgkin lymphoma, glioblastoma, pancreatic cancer, prostate cancer, and thyroid cancer.

Claim (Index 5):
A compound having the structure of Formula II: or pharmaceutically acceptable salts or solvates thereof, wherein: R 1  is selected from the group consisting of hydrogen, deuterium, an optionally substituted C 1 -C 6  alkyl, an optionally substituted C 3 -C 7  cycloalkyl, an optionally substituted aryl, and an optionally substituted heteroaryl; R 2  is selected from the group consisting of R D , an optionally substituted C 1 -C 6  alkyl, an optionally substituted C 3 -C 7  cycloalkyl, an optionally substituted aryl, and an optionally substituted heteroaryl; R 3  is selected from the group consisting of hydrogen, deuterium, and optionally substituted C 1 -C 6  alkyl, an optionally substituted hydroxyl, an optionally substituted C 1 -C 6  alkoxy, an optionally substituted C 3 -C 7  cycloalkyl, an optionally substituted aryl, and an optionally substituted heteroaryl; R 4  is an optionally substituted C 1 -C 6  alkyl; R 5  is hydrogen, deuterium or an optionally substituted C 1 -C 6  alkyl; R 6  is hydrogen, deuterium or an optionally substituted C 1 -C 6  alkyl; X 1  and X 2  are each independently selected from the group consisting of hydrogen, deuterium, an optionally substituted C 1 -C 6  alkyl, an optionally substituted aryl, an optionally substituted heteroaryl, halogen, \u2014CN, \u2014N 3 , \u2014COOR B , \u2014NR A R B , \u2014OR B , and \u2014SR B , where at least one of X 1  and X 2  is selected from the group consisting of an optionally substituted aryl, an optionally substituted heteroaryl, halogen, \u2014CN, \u2014N 3 , \u2014COOR B , \u2014NR A R B , \u2014OR B , and \u2014SR B  when R 5  is methyl; R A  is selected from the group consisting of hydrogen, deuterium, an optionally substituted C 1 -C 6  alkyl, an optionally substituted C 3 -C 7  cycloalkyl, an optionally substituted aryl, and an optionally substituted heteroaryl; R B  is selected from the group consisting of hydrogen, R 1A -L 1 -, R 3A -L 1 -, R 4A -L 1 -, Mc-L 1 -, Mal-L 3 -L 1 -, R 1A -Mal-L 3 -L 1 -Val-Cit-PAB\u2014C(O)\u2014 or Mal-L 3 -L 1 -Val-Cit-PAB\u2014C(O)\u2014; R 7  is an optionally substituted C 1 -C 6  alkyl, an optionally substituted heteroaryl, or \u2014C(\u2550O)R C ; R C  is selected from the group consisting of an optionally substituted C 1 -C 6  alkyl, optionally substituted C 1 -C 6  alkoxy, an optionally substituted C 3 -C 7  cycloalkyl, an optionally substituted aryl, and an optionally substituted heteroaryl, and hydroxyl; and R 8  is hydrogen, deuterium, \u2014OR D , or \u2014SR D ; R D  is selected from the group consisting of hydrogen, R 1A -L 1 -, R 3A -L 1 -, R 4A -L 1 -, Mc-L 1 -, Mal-L 3 -L 1 -, R 1A -Mal-L 3 -L 1 -Val-Cit-PAB\u2014C(O)\u2014 and Mal-L 3 -L 1 -Val-Cit-PAB\u2014C(O)\u2014; R 3A  is R 4A  is a conjugation moiety; R 1A  is a conjugated targeting moiety; L 1  is a linker or a bond; and L 3  is an alkanoyl.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 90.0
- Lexical Diversity: 1.77778
- Patent Class: 548.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14401318', '14843520', '15581749', '15557703', '13513982']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7976708318996099
- 35 USC 102 Novelty (BERT): 0.5061191385303113
- Combined Prediction Score: 0.76851566256268
- Mean Citation Score: 295.580128
- Max Citation Score: 303.1212
- Similarity Product: 249.6950825054168

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