PATENT CLAIM ANALYSIS

Application Number: 16170487
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-02
Patent Classification: ["514", "167000"]

Abstract:
This present disclosure is directed to novel prodrugs of activated vitamin D 3  compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.

Claim (Index 9):
A method for treating diseases which benefit from an increase in the levels of 1\u03b1,25-dihydroxyvitamin D 3 , or for treating diseases which benefit from an inhibition of the catabolism of 1\u03b1,25-dihydroxyvitamin D 3 , or for treating one or more diseases detected from the group consisting of the catabolism of 1\u03b1,25-dihydroxyvitamin D 3 , or for treating breast cancer, lung cancer, prostate cancer, colon cancer, colorectal cancer, kidney cancer, head and neck cancer, pancreatic cancer, skin cancer, Kaposi's sarcoma, leukemia, and psoriasis, or for inhibiting CPY24 activity in a cell or animal, or for increasing the levels of 1\u03b1,25-dihydroxyvitamin D 3  in a cell or animal, or for inhibiting catabolism of 1\u03b1,25-dihydroxyvitamin D 3  in a cell or animal in need thereof an effective amount of a compound:\n having Formula II, or a pharmaceutically acceptable salt, solvate, or hydrate thereof: wherein each   independently is a single bond or a double bond; R 1  is selected from the group consisting of OH, OC 1-6 alkyl, and halo; R 2  and R 3  are each independently H or halo, or together form \u2550CH 2 ; R 4  is C 1-6 alkyl; R 5  and R 6  are each independently H, halo, C 1-4 alkyl, or can be taken, together with the carbon atom to which they are bound, to form a C 3-6 cycloalkyl ring, with the proviso that when   between carbon-23 and carbon-24 is a double bond, then R 5  is absent; R 7  is selected from the group consisting of H, C 1-6 alkyl, C 2-6 alkenyl, aryl and heteroaryl, with C 1-6 alkyl and C 2-6 alkenyl being unsubstituted or substituted with 1 to 4 groups independently selected from C 1-4 alkyl, C 2-4 alkenyl, OC 1-4 alkyl, OC 2-4 alkenyl, OH, halo, NH 2 , NHC 1-4  alkyl, NHC 2-4  alkenyl, N(C 1-4  alkyl)(C 1-4  alkyl), N(C 2-4  alkenyl)(C 1-4  alkyl), and with aryl and heteroaryl being unsubstituted or substituted with 1 to 5 groups independently selected from C 1-4 alkyl, C 2-4 alkenyl, OC 1-4 alkyl, OC 2-4 alkenyl, OH, CF 3 , OCF 3 , halo, SH, SC 1-4 alkyl, SC 2-4 alkenyl NH 2 , NHC 1-4 alkyl, NHC 2-4 alkenyl, N(C 1-4 alkyl)(C 1-4 alkyl), N(C 2-4 alkenyl)(C 1-4 alkyl)CN, C(O)OH, C(O)OC 1-4 alkyl, C(O)OC 2-4 alkenyl, C(O)NHC 1-4 alkyl, C(O)NHC 2-4 alkenyl, NHC(O)C 1-4 alkyl, NHC(O)C 2-4 alkenyl, OC(O)C 1-4 alkyl, OC(O)C 2-4 alkenyl, SOC 1-4 alkyl, SOC 2-4 alkenyl, SO 2 C 1-4 alkyl, SO 2 C 2-4 alkenyl, SO 2 NHC 1-4 alkyl, SO 2 NHC 2-4 alkenyl and SO 2 NH 2 ; and R 8  is selected from the group consisting of C 1-6 alkyl, C 2-6 alkenyl, cyclo(C 3 -C 6 )alkyl, cyclo(C 5 -C 6 )alkenyl, aryl, heteroaryl, aryl-C 1-6 alkyl, aryl-C 2-6 alkenyl, heteroaryl-C 1-6 alkyl, and heteroaryl-C 2-6 alkenyl with C 1-6 alkyl and C 2-6 alkenyl being unsubstituted or substituted with 1-4 groups independently selected from C 1-4 alkyl, C 2-4 alkenyl, OC 1-4 alkyl, OC 2-4 alkenyl, OH, halo, NH 2 , NHC 1-4 alkyl, NHC 2-4 alkenyl, N(C 1-4 alkyl)(C 1-4 alkyl), and N(C 2-4 alkenyl)(C 1-4 alkyl), and with cyclo(C 3 -C 6 )alkyl, cyclo(C 5 -C 6 )alkenyl aryl, heteroaryl, aryl-C 1-6 alkyl, aryl-C 2-6 alkenyl, heteroaryl-C 1-6 alkyl, heteroaryl-C 2-6 alkenyl being unsubstituted or substituted with 1-5 groups independently selected from C 1-4 alkyl, C 2-4 alkenyl, OC 1-4 alkyl, OC 2-4 alkenyl, OH, CF 3 , OCF 3 , halo, SH, SC 1-4 alkyl, SC 2-4 alkenyl, NH 2 , NHC 1-4 alkyl, NHC 2-4 alkenyl, N(C 1-4 alkyl)(C 1-4 alkyl), N(C 2-4 alkenyl)(C 1-4 alkyl), CN, C(O)OH, C(O)OC 1-4 alkyl, C(O)OC 2-4 alkenyl, C(O)NHC 1-4 alkyl, C(O)NHC 2-4 alkenyl, NHC(O)C 1-4 alkyl, NHC(O)C 2-4 alkenyl, OC(O)C 1-4 alkyl, OC(O)C 2-4 alkenyl, SOC 1-4 alkyl, SOC 2-4 alkenyl SO 2 C 1-4 alkyl, SO 2 C 2-4 alkenyl, SO 2 NHC 1-4 alkyl, SO 2 NHC 2-4 alkenyl and SO 2 NH 2 .

Metadata:
- Claim Count in Document: 22.0
- Percentile: 97.0
- Lexical Diversity: 1.55556
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['13521980', '10270158', '10612302', '11912395', '10738248']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8080809118251118
- 35 USC 102 Novelty (BERT): 0.6833194610599165
- Combined Prediction Score: 0.7956047667485923
- Mean Citation Score: 476.151318
- Max Citation Score: 735.80597
- Similarity Product: 656.9147441317928

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