PATENT CLAIM ANALYSIS

Application Number: 16072291
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2018-12
Patent Classification: ["514", "146000"]

Abstract:
The present invention is directed to novel cytotoxic tubulysin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.

Claim (Index 5):
A compound of formula (III):\n (AB)-(L-P) b \u2003\u2003(III) or a pharmaceutically acceptable salt thereof, wherein: L is the linker moiety L 1 -L 2 -L 3 , where L is bound to P through R 6 ; P is a radical of formula: W is selected from: where:\n m is 1-3; \n n is 1-2; and \n p is 1-4; \n R 1  is selected from hydrogen, C 1 -C 8  alkyl and C 1 -C 8  haloalkyl; R 2  is selected from hydrogen, C 1 -C 8  alkyl and C 1 -C 8  haloalkyl; each R 3A  and R 3B  is independently selected from C 1 -C 8  alkyl, C 1 -C 8  haloalkyl, C 3 -C 8  carbocyclyl, C 1 -C 10  heterocyclyl, aryl, heteroaralkyl, halogen and aralkyl; or R 3A  and R 3B  taken together are selected from C 2 -C 8  alkylene and C 1 -C 8  heteroalkylene; R 5  is selected from hydrogen, C 1 -C 8  alkyl, C 1 -C 8  haloalkyl, C 3 -C 8  carbocyclyl, C 3 -C 8  heterocyclyl, aryl, heteroaralkyl, aralkyl, where R 5  is optionally substituted with \u2014(C(R) 2 ) m NR 1 R 2 ; R 6  is selected from \u2014OC(O)N(*)R 7 , \u2014O\u2014, \u2014NR\u2014, \u2014N(*)C(O)R 7 , \u2014N(*)C(O)OR 7 , \u2014N(*)C(O)NR 7 R 8 , \u2014N(*)SO 2 R and \u2014N(*)SO 2 NR 7 R 8 , where * is a bond to L, and where R 7  and R 8  are each independently selected from hydrogen, C 1 -C 8  alkyl, C 3 -C 8  carbocyclyl, C 3 -C 8  heterocyclyl, aryl, heteroaralkyl and aralkyl; or R 7  and R 8 , together with the nitrogen to which they are joined form C 3 -C 10  heterocyclyl, and where one or more of R 7  and R 8  are optionally substituted with one or more substituents selected from halogen, NR 2 , CN, OH and OC 1 -C 8  alkyl;\n Z is N or CR 2 ; \n Y is selected from aryl, C 3 -C 8  heterocyclyl and C 5 -C 14  heteroaryl, where Y is optionally substituted with one or more R 11 , or \n Y is selected from: \n where\n d is 1-5; \n q is 1-3; and \n each R 11  is independently selected from hydrogen, C 1 -C 5  alkyl, C 1 -C 8  haloalkyl, halogen, \u2014CN, \u2014OH, \u2014(C(R) 2 ) t ONRR, \u2014(C(R) 2 ) t \u2014NRR, (C(R) 2 ) t \u2014C(O)R, (C(R) 2 ) t \u2014CONR 8 R 9 , \u2014(C(R) 2 ) t C(O)NRNRR, \u2014(C(R) 2 ) t C(O)N(R)OH, \u2014(C(R) 2 ) t SH, \u2014(C(R) 2 ) t \u2014N(R)\u2014C(O)R, \n \u2014(C(R) 2 ) t N(R)\u2014C(O)OR, \u2014(C(R) 2 ) t N(R)\u2014SO 2 R, \u2014(C(R) 2 ) t N(R)C(O)NR 8 R 9 , \u2014(C(R) 2 ) t SO 2 NR 8 R 9 , and \u2014(C(R) 2 ) t N(R)SO 2 NR 8 R 9 , where each t is independently 0-3; and \n X is selected from hydrogen, \u2014C(O)OR, C 1 -C 6  alkyl, C 6 -C 14  aryl, C 5 -C 14  heteroaryl, C 3 -C 6  carbocyclyl, C 3 -C 8  heterocyclyl, \u2014C 1 -C 6  alkyl-C 6 -C 14  aryl, and \u2014C 1 -C 6 alkyl-C 5 -C 14 heteroaryl, where X is optionally substituted with 1-3 substituents independently selected from, halogen, \u2014OH, \u2014C(O)OR, \u2014CON(R)OH, \u2014ONR 2 , \u2014NR 8 R 9 , \u2014COR, \u2014CONR 2 , \u2014CONRNRR, \u2014SH, \u2014N(R)\u2014COR, \u2014N(R)\u2014C(O)OR, \u2014N(R)\u2014SO 2 R, \u2014N(R)\u2014CONR 8 R 9 , \u2014SO 2 \u2014NR 8 R 9 , \u2014N(R)\u2014SO 2  NR 8 R 9 , \u2014P(O)(OR) 2 , and \u2014S(O)(OR) 2 , where each R is independently hydrogen, C 1 -C 8  alkyl or C 1 -C 8  haloalkyl; L 1  is selected from: a bond to AB, \u2014NR 2 -(bond to AB) and; L 2  is L 2A -L 2B -L 2C  or L 2C -L 2B -L 2A , where:\n L 2A  comprises one or more components selected from: \u2014C(O)\u2014C 1 -C 6 alkyl-, \u2014C 1 -C 6 alkyl(OCH 2 CH 2 ) 1-6 \u2014, \u2014C(O)\u2014C 1 -C 6 alkyl-NRC(O)C 1 -C 6 alkyl-, \u2014C 1 -C 6 alkyl(OCH 2 CH 2 ) 1-6 \u2014 NRC(O)C 1 -C 6 alkyl-, \u2014C(O)\u2014, and \u2014C(O)\u2014O\u2014C 1 -C 6 alkyl-S\u2014, or L 2A  is absent; \n L 2B  is AA 0-aa , where AA is a natural or non-natural amino acid and aa is 12; and \n L 2C  is selected from -PABA- and -PABC-, or L 2C  is absent; and \n L 3  is \u2014CR 2 NR\u2014, or L 3  is absent; and b is 1-20.

Metadata:
- Claim Count in Document: 7.0
- Percentile: 95.0
- Lexical Diversity: 1.17857
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['14793942', '13670612', '14322262', '14069057', '15280563']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.771219313072833
- 35 USC 102 Novelty (BERT): 0.5316928795226806
- Combined Prediction Score: 0.7472666697178177
- Mean Citation Score: 318.400396
- Max Citation Score: 330.31903
- Similarity Product: 233.11560314195515

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