PATENT CLAIM ANALYSIS

Application Number: 16035771
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2019-01
Patent Classification: ["424", "452000"]

Abstract:
Embodiments of the disclosure relate generally to formulations, methods, kits, and dosage forms for improved stability of an active pharmaceutical ingredient, wherein the active ingredient comprises a compound of the formula: wherein X is N, Y is H or optionally substituted C 1 -C 6  alkyl; R 4  is morpholine optionally substituted with by C 1 -C 6  alkyl; R 7  is C 1 -C 6  alkyl optionally substituted by one or more F; R 8′  is halogen; and R 6  is wherein R 10  is H, C 1 -C 6  alkyl, halogen, CN or CF 3 ; R 12  is H or halogen; R 13  is H, halogen or C 1 -C 6  alkyl; and R 17  is H, C 1 -C 6  alkyl, (C 1 -C 6  alkyl)-NH 2 ; and, pharmaceutically acceptable salts and free bases thereof, wherein the active ingredient remains in substantially amorphous form after storage of the pharmaceutical formulation for a predetermined time and conditions. In one embodiment the formulations, methods, kits and dosage forms comprising the active pharmaceutical ingredient with improved stability can be used in the treatment of a condition characterized by the dysregulation of one of both of the RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways.

Claim (Index 30):
A dosage form comprising a pharmaceutical formulation and additional excipients, wherein the pharmaceutical formulation comprises about 400 mg total of a stabilizing polymer/active ingredient mixture comprising about 300 to 390 mg of hydroxypropylmethyl cellulose acetate succinate and about 10 to 100 mg of an active ingredient in substantially amorphous form, about 250 mg particulate mannitol, about 10 mg colloidal silicon dioxide; and the additional excipients comprise about 100 mg mannitol, about 30 mg of microcrystalline cellulose, about 40 mg crospovidone, about 10 mg magnesium stearate, wherein the active ingredient is the free base of N-(3-(2-(6-amino-4-(trifluoromethyl)pyridin-3-yl)-4-morpholinopyrido[3,2-d]pyrimidin-6-yl)-2-fluorophenyl)-3-fluoropropane-1-sulfonamide, and wherein the active ingredient remains in substantially amorphous form after storage of the dosage form for a predetermined time and conditions.

Metadata:
- Claim Count in Document: 35.0
- Percentile: 95.0
- Lexical Diversity: 2.41053
- Patent Class: 424.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15581330', '15290788', '14783903', '16073355', '13957470']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7579426910241241
- 35 USC 102 Novelty (BERT): 0.5370536662522085
- Combined Prediction Score: 0.7358537885469326
- Mean Citation Score: 334.927828
- Max Citation Score: 392.866
- Similarity Product: 240.39745754814143

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