PATENT CLAIM ANALYSIS

Application Number: 15772910
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-11
Patent Classification: ["540", "467000"]

Abstract:
The present invention provides compositions and methods for providing controllable local delivery of a conjugate of bortezomib (Btz) and a bisphosphonate to promote bone formation. In certain embodiments, the invention is used as a treatment for a subject with diseases and disorders characterized by bone loss.

Claim (Index 29):
A method of killing cancer cells of bone, bone marrow and bone surrounding tissues in a subject, the method comprising administering a therapeutically effective amount of a composition comprising at least one compound of formula (I): wherein in formula (I): each occurrence of R 1  is independently selected from the group consisting of hydrogen and alkyl; R 2  is selected from the group consisting of hydrogen, alkyl, \u2014OR 13 , \u2014N(R 13 )(R 14 ), and halogen; R 3  is selected from the group consisting of hydrogen and alkyl, wherein the alkyl group is optionally substituted with one to four substituents selected from the group consisting of hydroxyl, alkoxy, alkenyl, cycloalkyl, aryl, heteroaryl, halo, cyano and amino; R 4  is selected from the group consisting of hydrogen, alkyl, aryl, and alkylaryl wherein the alkyl, aryl, or alkylaryl group is optionally substituted with one to four substituents selected from the group consisting of hydroxyl, alkoxy, alkenyl, cycloalkyl, aryl, heteroaryl, halo, cyano and amino; L 1  is selected from the group consisting of alkyl, aryl, cycloalkyl, alkylaryl, alkylcycloalkyl, and alkyl-Z 4 C(O)NR 10 , wherein the alkyl, aryl, cycloalkyl, alkylaryl, or alkylcycloalkyl group is optionally substituted with one to four substituents selected from the group consisting of alkyl, hydroxyl, alkoxy, alkenyl, cycloalkyl, aryl, heteroaryl, halo, cyano and amino; L 2  is aryl or an alkyl chain of C 1 -C 6  alkyl, wherein any carbon atom in the alkyl chain is optionally substituted with one to two substituents selected from the group consisting of alkyl, cycloalkyl, and carbonyl; L 3  is aryl or an alkyl chain of C 1 -C 6  alkyl, wherein any carbon atom in the alkyl chain is optionally substituted with one to two substituents selected from the group consisting of alkyl, cycloalkyl, and carbonyl; Y is selected from the group consisting of \u2014PO(OR 8 )(OR 9 ), \u2014PO(R 9 )(OR 8 ), \u2014CO 2 R 8 , and \u2014SO 3 R 8 ; Z 1  is selected from the group consisting of CH 2  and NR 6 ; A is selected from the group consisting of CH 2 , C(\u2550O), C(\u2550NR 7 ), and C(\u2550S); Z 2  is selected from the group consisting of CH 2 , NR 11 , S, and O; Z 3  is selected from the group consisting of N, CR 12 , and phenyl; Z 4  is selected from the group consisting of CH 2  and O; Z 5  is selected from the group consisting of aryl, alkyl, OR 18 , and wherein the aryl or alkyl group is optionally substituted with one to four substituents selected from the group consisting of alkyl, hydroxyl, alkoxy, alkenyl, cycloalkyl, aryl, heteroaryl, halo, cyano and amino;\n each occurrence of R 5  is independently selected from the group consisting of, alkyl, fluoroalkyl, heteroalkyl, aryl, F, Cl, Br, I, \u2014CN, \u2014NO 2 , \u2014OR 17 , \u2014SR 17 , \u2014S(\u2550O)R 17 , \u2014S(\u2550O) 2 R 17 , \u2014NHS(\u2550O) 2 R 17 , \u2014C(\u2550O)R 17 , \u2014OC(\u2550O)R 17 , \u2014CO 2 R 17 , \u2014OCO 2 R 17 , \u2014CH(R 17 ) 2 , \u2014N(R 17 ) 2 , \u2014C(\u2550O)N(R 17 ) 2 , \u2014OC(\u2550O)N(R 17 ) 2 , \u2014NHC(\u2550O)NH(R 17 ), \u2014NHC(\u2550O)R 17 , \u2014NHC(\u2550O)OR 17 , \u2014C(OH)(R 17 ) 2 , and \u2014C(NH 2 )(R 17 ) 2 ; \n X 1  is selected from the group consisting of CR 15  and N; \n X 2  is selected from the group consisting of CR 16  and N; \n R 6  and R 7  are each independently selected from the group consisting of hydrogen and alkyl, wherein the alkyl group is optionally substituted with one to four substituents selected from the group consisting of hydroxyl, alkoxy, alkenyl, cycloalkyl, aryl, heteroaryl, halo, cyano and amino; \n R 8 , R 9 , and R 10  are each independently selected from the group consisting of hydrogen and alkyl; \n R 11 , R 12 , R 13 , and R 14  are each independently selected from the group consisting of hydrogen and alkyl, wherein the alkyl group is optionally substituted with one to four substituents selected from the group consisting of hydroxyl, alkoxy, alkenyl, cycloalkyl, aryl, heteroaryl, halo, cyano and amino; \n R 15  and R 16  are each independently selected form the group consisting of hydrogen, alkyl, fluoroalkyl, heteroalkyl, aryl, F, Cl, Br, I, \u2014CN, \u2014NO 2 , \u2014OR 17 , \u2014SR 17 , \u2014S(\u2550O)R 17 , \u2014S(\u2550O) 2 R 17 , \u2014NHS(\u2550O) 2 R 17 , \u2014C(\u2550O)R 17 , \u2014OC(\u2550O)R 17 , \u2014CO 2 R 17 , \u2014OCO 2 R 17 , \u2014CH(R 17 ) 2 , \u2014N(R 17 ) 2 , \u2014C(\u2550O)N(R 17 ) 2 , \u2014OC(\u2550O)N(R 17 ) 2 , \u2014NHC(\u2550O)NH(R 17 ), \u2014NHC(\u2550O)R 17 , \u2014NHC(\u2550O)OR 17 , \u2014C(OH)(R 17 ) 2 , and \u2014C(NH 2 )(R 17 ) 2 ; \n each occurrence of R 17  is selected from the group consisting of hydrogen and alkyl; \n R 18  is selected from the group consisting of alkyl, aryl, and arylalkyl; \n n is an integer from 0 to 10; and \n z is an integer from 0 to 2; or \n a pharmaceutically acceptable salt thereof, an isomer thereof, or a mixture of isomers thereof.

Metadata:
- Claim Count in Document: 33.0
- Percentile: 93.0
- Lexical Diversity: 1.2439
- Patent Class: 540.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15772893', '15094733', '14378089', '10576228', '15951585']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.6895450582944129
- 35 USC 102 Novelty (BERT): 0.5345571632981987
- Combined Prediction Score: 0.6740462687947915
- Mean Citation Score: 295.387648
- Max Citation Score: 362.4084
- Similarity Product: 271.3699984787464

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