PATENT CLAIM ANALYSIS

Application Number: 16272788
Application Type: Utility
Filing Date: 2019-02
Publication Date: 2019-06
Patent Classification: ["546", "245000"]

Abstract:
The disclosed subject matter provides certain polymorphic forms of Compound (I) as well as pharmaceutical compositions comprising Compound (I) or such polymorphic forms, and methods of using or making such compounds and pharmaceutical compositions. It has now been discovered that Compound (I) can exist in multiple crystalline forms (polymorphs). One particular crystalline form, Form II, has been found to be more thermodynamically stable and, thus, likely more suitable for bulk preparation and handling than other polymorphic forms. Efficient and economic methods have been developed to prepare Compound (I) and Form II in high purity on a large scale. In animal studies, Form II has demonstrated safety and efficacy in treating depressive disorders and, when micronized, improved absorption compared to non-micronized Form II.

Claim (Index 14):
A method of preparing Form II of Compound I comprising: (i) reacting Compound (8) with triflic anhydride to yield a triflate; (ii) reacting the triflate with ammonia to yield Compound (9) (iii) reacting the Compound (9) with 2-chloropyrimidine to yield a crude form of Compound I; (iv) purifying said crudeform of Compound I by dissolving the crude form of Compound I in ethyl acetate at a temperature above 35\u00b0 C., followed by partially or completely replacing the ethyl acetate with heptane; (v) collecting the purified Form I of Compound I; and (vi) heating Form I of Compound I in its solid form to a temperature above 50\u00b0 C. to obtain Form II of Compound I.

Metadata:
- Claim Count in Document: 41.0
- Percentile: 99.0
- Lexical Diversity: 1.70588
- Patent Class: 546.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15538015', '14604334', '13990632', '16301027', '15740719']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7268905791326515
- 35 USC 102 Novelty (BERT): 0.4978900186625171
- Combined Prediction Score: 0.703990523085638
- Mean Citation Score: 213.96425
- Max Citation Score: 243.34459
- Similarity Product: 184.71979366764305

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