PATENT CLAIM ANALYSIS

Application Number: 15772893
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-11
Patent Classification: ["514", "082000"]

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

Claim (Index 1):
A compound selected from the group consisting of:\n i) a compound of formula (I): wherein in formula (I):\n each occurrence of R 1  is independently selected from the group consisting of hydrogen and alkyl; \n R 2  is selected from the group consisting of hydrogen, alkyl, \u2014OR 8 , \u2014N(R 8 )(R 9 ), and halogen; \n each occurrence of R 3  and R 4  is independently selected from the group consisting of alkyl, haloalkyl, heteroalkyl, halogen, \u2014CN, \u2014NO 2 , \u2014OR 16 , \u2014SR 16 , \u2014S(\u2550O)R 16 , \u2014S(\u2550O) 2 R 16 , \u2014NHS(\u2550O) 2 R 16 , \u2014C(\u2550O)R 16 , \u2014OC(\u2550O)R 16 , \u2014CO 2 R 16 , \u2014OCO 2 R 16 , \u2014CH(R 16 ) 2 , \u2014N(R 16 ) 2 , \u2014C(\u2550O)N(R 16 ) 2 , \u2014OC(\u2550O)N(R 16 ) 2 , \u2014NHC(\u2550O)NH(R 16 ), \u2014NHC(\u2550O)R 16 , \u2014NHC(\u2550O)OR 16 , \u2014C(OH)(R 16 ) 2 , and \u2014C(NH 2 )(R 16 ) 2 , wherein the alkyl, haloalkyl, or heteroalkyl is optionally substituted; \n R 5 , R 6 , R 8  and R 9  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 L 1  and L 2  are each independently selected from the group consisting of a bond, alkyl, aryl, cycloalkyl, alkylaryl, alkylcycloalkyl, alkylaryl, and arylalkyl wherein the alkyl, aryl, cycloalkyl, alkylaryl, alkylaryl, arylalkyl or alkylcycloalkyl 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 Y is selected from the group consisting of \u2014PO(OR 10 )(OR 11 ), \u2014PO(R 10 )(OR 11 ), \u2014CO 2 R 10 , and \u2014SO 3 R 10 ; \n R 10  and R 11  are each independently selected from the group consisting of hydrogen and alkyl; \n Z 1  is selected from the group consisting of a bond, CH 2  and NR 12 ; \n A is selected from the group consisting of a bond, CH 2 , C(\u2550O), C(\u2550NR 13 ), and C(\u2550S); \n Z 2  is selected from the group consisting of a bond, CH 2 , NR 14 , S, and O; \n Z 3  is selected from the group consisting of a bond, CH 2 , NR 7 , S, and O \n Z 4  is selected from the group consisting of O, NR 15 , and S; \n R 7 , R 12 , R 13 , R 14 , and R 15  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 each occurrence of R 16  is 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 n is an integer from 0 to 10; \n x is an integer from 0 to 4; and \n z is an integer from 0 to 2; and \n ii) a compound of formula (II): wherein in formula (II):\n each occurrence of R 1  is independently selected from the group consisting of hydrogen and alkyl; \n R 2  is selected from the group consisting of hydrogen, alkyl, \u2014OR 8 , \u2014N(R 8 )(R 9 ), and halogen; \n each occurrence of R 3  and R 4  is independently selected from the group consisting of alkyl, haloalkyl, heteroalkyl, halogen, \u2014CN, \u2014NO 2 , \u2014OR 16 , \u2014SR 16 , \u2014S(\u2550O)R 16 , \u2014S(\u2550O) 2 R 16 , \u2014NHS(\u2550O) 2 R 16 , \u2014C(\u2550O)R 16 , \u2014OC(\u2550O)R 16 , \u2014CO 2 R 16 , \u2014OCO 2 R 16 , \u2014CH(R 16 ) 2 , \u2014N(R 16 ) 2 , \u2014C(\u2550O)N(R 16 ) 2 , \u2014OC(\u2550O)N(R 16 ) 2 , \u2014NHC(\u2550O)NH(R 16 ), \u2014NHC(\u2550O)R 16 , \u2014NHC(\u2550O)OR 16 , \u2014C(OH)(R 16 ) 2 , and \u2014C(NH 2 )(R 16 ) 2 , wherein the alkyl, haloalkyl, or heteroalkyl is optionally substituted; \n R 5 , R 6 , R 8  and R 9  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 L 1  and L 2  are each independently selected from the group consisting of a bond, alkyl, aryl, cycloalkyl, alkylaryl, alkylcycloalkyl, alkylaryl, and arylalkyl wherein the alkyl, aryl, cycloalkyl, alkylaryl, alkylaryl, arylalkyl or alkylcycloalkyl 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 Y is selected from the group consisting of \u2014PO(OR 10 )(OR 11 ), \u2014PO(R 10 )(OR 11 ), \u2014CO 2 R 10 , and \u2014SO 3 R 10 ; \n R 10  and R 11  are each independently selected from the group consisting of hydrogen and alkyl; \n Z 1  is selected from the group consisting of a bond, CH 2  and NR 12 ; \n A and B are each independently selected from the group consisting of a bond, CH 2 , C(\u2550O), C(\u2550NR 13 ), and C(\u2550S); \n Z 2  is selected from the group consisting of a bond, CH 2 , NR 14 , S, and O; \n Z 3  is selected from the group consisting of a bond, CH 2 , NR 7 , S, and O \n Z 4  is selected from the group consisting of O, NR 15 , and S; \n R 7 , R 12 , R 14 , and R 15  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 each occurrence of R 13  and R 16  is 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 n is an integer from 0 to 10; \n x is an integer from 0 to 4; and \n z is an integer from 0 to 2; or \n a pharmaceutically acceptable salt thereof; or an isomer thereof; or a mixture of isomers thereof.

Metadata:
- Claim Count in Document: 47.0
- Percentile: 93.0
- Lexical Diversity: 1.30952
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['13646143', '12588882', '14620700', '15621665', '10576228']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8034026209545365
- 35 USC 102 Novelty (BERT): 0.5251936058669224
- Combined Prediction Score: 0.7755817194457751
- Mean Citation Score: 322.2473619999999
- Max Citation Score: 323.93375
- Similarity Product: 243.17328077703712

Labels:
- Claim Label 101: 1
- Claim Label 102: 0
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 0
- Label 101 Adjusted: 1

Dataset: test