PATENT CLAIM ANALYSIS

Application Number: 15948716
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-08
Patent Classification: ["424", "450000"]

Abstract:
Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.

Claim (Index 22):
A compound having the formula: or a pharmaceutically acceptable salt thereof, wherein D is a drug selected from the group consisting of: tacrolimus, cyclosporine, and azathioprine; wherein Z is a Liposome Solubilization Unit of formula IIA: wherein [S] is a \u201cspacer\u201d comprising:\n (a) a chain of the type (CH 2 ) n , where n may range from 1 to 10, or \n (b) a derivative of the above (CH 2 ) n  where one or more H atoms are replaced by: a linear, branched, or cyclic alkyl group containing from 1 to 10 C atoms, a heteroatom such as N, O, S, Si, which may be further connected to H atoms; or to heteroatoms such as N, O, S; or to linear, branched, or cyclic alkyl groups containing from 1 to 10 C atoms and facultatively incorporating one or more halogen atoms, a halogen atom; or \n (c) a derivative of the above (CH 2 ) n  where one or more CH 2  groups are replaced by: a heteroatom such as N, O, S, Si, which may be further connected to H atoms; or to heteroatoms such as N, O, S; or to linear, branched, or cyclic alkyl groups containing from 1 to 10 C atoms and facultatively incorporating one or more halogen atoms, a ring structure consisting of 3 to 10 carbon atoms and facultatively incorporating one of more heteroatoms such as N, O, S, Si, or halogen, as well as multiple bonds among pairs of atoms; or \n (d) a derivative of the above (CH 2 ) n  where one or more pairs of adjacent C atoms share a double bond of E- or Z-geometry, or a triple bond; and \n wherein [N] is a Solubilization Domain of any of the following:\n (a) [N] is of the general formula III: \n wherein R and R\u2032 together with the nitrogen atom to which they are attached form a heterocyclic ring having four to five carbon atoms, which may comprise one of multiple rings within a ring system; or\n (b) [N] is selected from the group consisting of: \n wherein:\n A is selected from the group consisting of: carbonyl, methylene, and NR\u2014C\u2550O, where R is H or C 1 -C 5  alkyl; \n R 1  and R 2  are independently selected from the group consisting of: linear or branched C 1 -C 30  alkyl, C 2 -C 30  alkenyl, and C 2 -C 30  alkynyl; and \n R 3  and R 4  are independently selected from the group consisting of: H; C 1 -C 10  alkyl, C 2 -C 10  alkenyl, C 2 -C 10  alkynyl, each optionally substituted with halo; and cycloalkyl, heterocyclyl, aryl, and heteroaryl, each optionally substituted with halo; or \n R 3  and R 4  together with the nitrogen atom to which they are attached form a heterocyclic ring having four to five carbon atoms, which may comprise one of multiple rings within a ring system; or \n (c) [N] is selected from the group consisting of:

Metadata:
- Claim Count in Document: 62.0
- Percentile: 91.0
- Lexical Diversity: 1.61194
- Patent Class: 424.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14302537', '13866873', '13467021', '12993482', '13866913']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8253456806117245
- 35 USC 102 Novelty (BERT): 0.6577285404568675
- Combined Prediction Score: 0.8085839665962389
- Mean Citation Score: 683.52984
- Max Citation Score: 799.9733
- Similarity Product: 589.6554599730491

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

Dataset: test