PATENT CLAIM ANALYSIS

Application Number: 15872642
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-07
Patent Classification: ["548", "400000"]

Abstract:
Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.

Claim (Index 104):
A method of preparing an antibody drug conjugate of Formula II:\n (T)-(L)-(D)\u2003\u2003 II \n wherein (T) is a targeting moiety, (L) is a linker, and (D) is a compound of Formula I: wherein:\n R 1  is selected from: amino-C 1 -C 6  alkyl, amino-aryl, amino-C 3 -C 7  cycloalkyl, amino-heterocyclyl and heterocyclyl, each optionally substituted with one or more substituents selected from aryl, aryl-C 1 -C 6  alkyl, C 1 -C 6  alkyl, C 1 -C 6  alkylthio, carboxyl, carboxamide, C 3 -C 7  cycloalkyl, C 3 -C 7  cycloalkyl-C 1 -C 6  alkyl, guanidino, halo, C 1 -C 6  haloalkyl, heterocyclyl, heterocyclyl-C 1 -C 6  alkyl, hydroxyl and thio; or \n R 1  is R a R b NCH(R c )\u2014; \n R a  is selected from: H and C 1 -C 6  alkyl; \n R b  is C 1 -C 6  alkyl; \n R c  is R d -C(CH 3 ) 2 \u2014; \n R d  is selected from: H, aryl, C 3 -C 7  cycloalkyl and heteroaryl, each of which is optionally substituted with one or more substituents selected from: C 1 -C 4  acylthio, C 2 -C 4  alkenyl, C 1 -C 4  alkyl, C 1 -C 4  alkylamino, C 1 -C 4  alkyloxy, amino, amino-C 1 -C 4  alkyl, halo, C 1 -C 4  haloalkyl, hydroxyl, hydroxy-C 1 -C 4  alkyl and thio, wherein C 2 -C 4  alkenyl, C 1 -C 4  alkylamino and C 1 -C 4  alkyloxy are further optionally substituted with one substituent selected from C 1 -C 4  alkylaryl, hydroxyl and thio; or \n R b  and R c  taken together with the atoms to which they are each bonded form a heterocyclyldiyl; \n R 2  is selected from: C 2 -C 6  alkyl, aryl, aryl-C 1 -C 6  alkyl, C 4 -C 7  cycloalkyl, C 3 -C 7  cycloalkyl-C 1 -C 6  alkyl, heteroaryl, heteroaryl-C 1 -C 6  alkyl and heterocyclyl, each optionally substituted with one or more substituents selected from: C 1 -C 6  alkoxy, C 1 -C 6  alkoxycarbonyl, C 1 -C 6  alkyl, C 1 -C 6  alkylamino, amino, amino-C 1 -C 6  alkyl, amino-aryl, amino-C 3 -C 7  cycloalkyl, aryl, carboxamide, carboxyl, cyano, C 1 -C 6  haloacyl, C 1 -C 6  haloalkyl, C 1 -C 6  haloalkoxy, halo, hydroxyl, nitro, thio and thio-C 1 -C 6  alkyl, and \n X is absent, \n the method comprising:\n (i) deprotecting the precursor according to  claim 74  to provide a compound of Formula I, \n (ii) conjugating the compound of Formula I to (L).

Metadata:
- Claim Count in Document: 85.0
- Percentile: 86.0
- Lexical Diversity: 1.86364
- Patent Class: 548.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14857733', '15512030', '15108258', '14213504', '14776654']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.735252098641061
- 35 USC 102 Novelty (BERT): 0.5693354531320268
- Combined Prediction Score: 0.7186604340901577
- Mean Citation Score: 385.776854
- Max Citation Score: 519.564
- Similarity Product: 465.15634365820887

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