PATENT CLAIM ANALYSIS

Application Number: 15956385
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-10
Patent Classification: ["424", "499000"]

Abstract:
The disclosure provides a sustained release injectable neurosteroid formulation comprising neurosteroid particles having a D50 of less than 10 microns, the neurosteroid particles comprising a neurosteroid of Formula I: or a pharmaceutically acceptable salt thereof, wherein:   is a double or single bond and the variables, e.g., R 1 , R 2 , R 3 , R 4 , R 4a , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , and R 10a  are described herein. The formulation comprises neurosteroid particles comprising the neurosteroid and a polymeric surface stabilizer and provides an effective plasma concentration of the neurosteroid at steady state for at least 48 hours, and in some embodiments for at least 4 weeks. The sustained release injectable neurosteroid formulation can formulated for intramuscular or subcutaneous administration. The disclosure provides a method of treating a patient having seizures, anxiety, agitation, depression (including post-partum depression), schizophrenia, post-traumatic stress disorder, or tremors by administering the sustained release neurosteroid formulation to the patient. In certain embodiments the neurosteroid is ganaxolone.

Claim (Index 1):
A sustained release injectable neurosteroid formulation comprising neurosteroid particles having a D50 of less than 10 microns, the neurosteroid particles comprising\n a) a neurosteroid of Formula I: or a pharmaceutically acceptable salt thereof, wherein:  is a double or single bond; X is O, S, or NR 11 ; R 1  is hydrogen, hydroxyl, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted aryl, or optionally substituted arylalkyl; R 4  is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, or optionally substituted (cycloalkyl)alkyl, or \u2014OR 40 , where R 40  is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, or optionally substituted (cycloalkyl)alkyl, or optionally substituted C 3 -C 6 carbocycle; R 4a  is hydrogen or R 4  and R 4a  are taken together to form an oxo (\u2550O) group; R 2 , R 3 , R 5 , and R 6 , are each independently hydrogen, hydroxyl, halogen, optionally substituted alkyl, optionally substituted cycloalkyl, or optionally substituted (cycloalkyl)alkyl, or optionally substituted heteroalkyl; R 7  is hydrogen, halogen, optionally substituted alkyl, optionally substituted C 3 -C 6 carbocycle, optionally substituted (C 3 -C 6 carbocycle)alkyl or \u2014OR 70  where R 70  is hydrogen, optionally substituted alkyl, optionally substituted C 3 -C 6 carbocycle, or optionally substituted (C 3 -C 6 carbocycle)alkyl; R 8  is hydrogen, optionally substituted alkyl or optionally substituted C 3 -C 6 carbocycle, and R 9  is hydroxyl; or R 8  and R 9  are taken together to form an oxo group; R 10  is hydrogen, halogen, hydroxyl, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted C 3 -C 6 carbocyle, or optionally substituted (C 3 -C 6 carbocycle)alkyl, and R 10a  is hydrogen, halogen, or optionally substituted alkyl, provided that if   is a double bond R 10a  is absent; each alkyl is a C 1 -C 10 alkyl and optionally contains one or more single bonds replaced by a double or triple bond; each heteroalkyl group is an alkyl group in which one or more methyl group is replaced by an independently chosen \u2014O\u2014, \u2014S\u2014, \u2014N(R 11 )\u2014, \u2014S(\u2550O)\u2014 or \u2014S(\u2550O) 2 \u2014, where R 11  is independently chosen at each occurrence and is hydrogen, alkyl, or alkyl in which one or more methylene group is replaced by \u2014O\u2014, \u2014S\u2014, \u2014NH, or \u2014N-alkyl; and b) at least one polymeric surface stabilizer; wherein the formulation provides an effective plasma concentration of the compound at steady state for at least 48 hours.

Metadata:
- Claim Count in Document: 50.0
- Percentile: 91.0
- Lexical Diversity: 2.0102
- Patent Class: 424.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15700314', '14772726', '11587906', '12041038', '12320539']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.696795940694589
- 35 USC 102 Novelty (BERT): 0.5017507845516136
- Combined Prediction Score: 0.6772914250802915
- Mean Citation Score: 207.997362
- Max Citation Score: 269.98532
- Similarity Product: 207.49623030911445

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

Dataset: test