PATENT CLAIM ANALYSIS

Application Number: 15746338
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-07
Patent Classification: ["544", "037000"]

Abstract:
The present invention pertains generally to the field of chemical synthesis, and more particularly to methods of chemical synthesis which include the step of preparing a substituted 10H-phenothiazine-3,7-diamine compound of Formula (1) by a step of selective alkylation by reductive amination, in which the corresponding unsubstituted diamine of Formula (4) is reacted with aldehyde/ketone, under reductive amination conditions. The present invention also relates to such methods which incorporate additional subsequent and/or preceding steps, for example, to prepare compounds of Formulae (2) and (3) from compounds of Formula (1), and to prepare compounds of Formula (4) from, for example, compounds of Formulae (5), (6), (7), (8), and (9). Compounds of Formula (1), Formula (2), and Formula (3) are useful, for example, in the treatment of diseases of protein aggregation, such as Alzheimer's disease.

Claim (Index 73):
A method according to  claim 72 , wherein:\n R 1A  is \u2014CH(R 1AX )(R 1AY ); and R 1B  is independently \u2014H or \u2014CH(R 1BX )(R 1BY ); or R 1A  and R 1B , taken together, form \u2014CH 2 \u2014R 1AB \u2014CH 2 \u2014; wherein:\n R 1AX  is independently \u2014H, C 1-10 alkyl, C 3-6 cycloalkyl, or C 6-10 carboaryl; and \n R 1AY  is independently \u2014H, C 1-10 alkyl, C 3-6 cycloalkyl, or C 6-10  carboaryl; or \n R 1AX  and R 1AY , taken together, form C 4-6 alkylene; \n and wherein:\n R 1BX  is independently \u2014H, C 1-10 alkyl, C 3-6 cycloalkyl, or C 6-10 carboaryl; and \n R 1BY  is independently \u2014H, C 1-10 alkyl, C 3-6 cycloalkyl, or C 6-10  carboaryl; or \n R 1BX  and R 1BY , taken together, form C 4-6 alkylene; \n and wherein:\n R 1AB  is C 2-4 alkylene; \n and wherein:\n R 2A  is \u2014CH(R 2AX )(R 2AY ); and \n R 2B  is independently \u2014H or \u2014CH(R 2BX )(R 2BY ); or \n R 2A  and R 2B , taken together, form \u2014CH 2 \u2014R 2AB \u2014CH 2 \u2014; \n wherein:\n R 2AX  is independently \u2014H, C 1-10 alkyl, C 3-6 cycloalkyl, or C 6-10  carboaryl; and \n R 2AY  is independently \u2014H, C 1-10 alkyl, C 3-6 cycloalkyl, or C 6-10  carboaryl; or \n R 2AX  and R 2AY , taken together, form C 4-6 alkylene; \n and wherein:\n R 2BX  is independently \u2014H, C 1-10 alkyl, C 3-6 cycloalkyl, or C 6-10 carboaryl; and \n R 2BY  is independently \u2014H, C 1-10 alkyl, C 3-6 cycloalkyl, or C 6-10  carboaryl; or \n R 2BX  and R 2BY , taken together, form C 4-6 alkylene; \n and wherein:\n R 2AB  is C 2-4 alkylene; \n wherein: if (a):\n R 1A  is \u2014CH(R 1AX )(R 1AY ); and \n R 1B  is independently \u2014H or \u2014CH(R 1BX )(R 1BY ); \n R 2A  is \u2014CH(R 2AX )(R 2AY ); and \n R 2B  is independently \u2014H or \u2014CH(R 2BX )(R 2BY ); \n then the aldehyde/ketone comprises:\n R 1AX \u2014C(\u2550O)\u2014R 1AY , and \n R 2AX \u2014C(\u2550O)\u2014R 2AY ; \n and further if R 1B  is other than \u2014H, then the aldehyde/ketone further comprises:\n R 1BX \u2014C(\u2550O)\u2014R 1BY , \n and further if R 2B  is other than \u2014H, then the aldehyde/ketone further comprises:\n R 2BX \u2014C(\u2550O)\u2014R 2BY ; \n and if (b):\n R 1A  and R 1B , taken together, form \u2014CH 2 \u2014R 1AB \u2014CH 2 \u2014; and \n R 2A  and R 2B , taken together, form \u2014CH 2 \u2014R 2AB \u2014CH 2 \u2014; \n then the aldehyde/ketone comprises:\n (O\u2550)CH\u2014R 1AB \u2014CH(\u2550O); and \n (O\u2550)CH\u2014R 2AB \u2014CH(\u2550O).

Metadata:
- Claim Count in Document: 68.0
- Percentile: 86.0
- Lexical Diversity: 2.32051
- Patent Class: 544.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['14410952', '13063525', '13984841', '15056610', '13241887']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7276550358088293
- 35 USC 102 Novelty (BERT): 0.5130737463536277
- Combined Prediction Score: 0.706196906863309
- Mean Citation Score: 219.46046
- Max Citation Score: 265.7381
- Similarity Product: 182.9734448441208

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