PATENT CLAIM ANALYSIS

Application Number: 15941063
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-09
Patent Classification: ["544", "281000"]

Abstract:
Certain pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds that inhibit cycline dependent kinase (CDK) (e.g., CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8, CDK9, CDK10, CDK11, CDK12, CDK13, etc.) are disclosed. Pharmaceutical compositions comprising these compounds, and the use of these compounds and compositions to inhibit CDK; to treat disorders associated with CDK such as those arising from an inappropriate activity, mutation, overexpression, or upstream pathway activation of CDK; or disorders that are ameliorated by the inhibition of CDK; proliferative disorders; cancer; viral infections; neurodegenerative disorders; ischaemia; renal diseases; and cardiovascular disorders are also disclosed. Optionally, the treatment further comprises simultaneous or sequential treatment with a further active agent, e.g., an aromatase inhibitor, an anti-estrogen, a Her2 blocker, a cytotoxic chemotherapeutic agent, etc.

Claim (Index 117):
A method of treatment of breast cancer, comprising administering to a subject in need of treatment a therapeutically-effective amount of a compound of the following formula: or a pharmaceutically acceptable salt thereof; wherein:\n \u2014R 5X  is -LX-Q; \n *L 5X - is independently a covalent single bond or -L 5XA -; \n -L 5XA - is independently linear or branched saturated C 1-6 alkylene, and is optionally substituted with one or more groups selected from \u2014OH and \u2014OR L5X , wherein each \u2014R L5X  is independently linear or branched saturated C 1-6 alkyl or saturated C 3-6 cycloalkyl; \n -Q is pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, or diazepanyl, wherein the point of attachment is via a ring carbon atom, and is substituted with \u201cn\u201d groups -J, and is substituted with \u201cm\u201d groups \u2014R Q ; \n \u201cn\u201d is 1, 2, or 3; \n \u201cm\u201d is 0, 1, 2, or 3; \n each -J is independently \u2014OH, \u2014OR J , -L J -OH, or -L J -OR J ; \n each \u2014R J  is independently linear or branched saturated C 1-6 alkyl or saturated C 3-6 cycloalkyl; \n each -L J - is independently linear or branched saturated C 1-6 alkylene; \n each \u2014R Q  is independently \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014R QA , \u2014CF 3 , \u2014OCF 3 , \u2014NH 2 , \u2014NHR QA , \u2014NR QA 2 , pyrrolidino, piperidino, morpholino, piperazino, N\u2014(R QA )-piperazino, \u2014SH, \u2014SR QA , or \u2014CN; \n each \u2014R QA  is independently linear or branched saturated C 1-6 alkyl or saturated C 3-6 cycloalkyl; \n \u2014R 5Y  is independently \u2014H or \u2014R 5YA ; \n \u2014R 5YA  is independently linear or branched saturated C 1-6 alkyl; \n \u2014R 7  is independently \u2014R 7X  or \u2014C(\u2550O)R 7X ; \n each \u2014R 7X  is independently:\n \u2014R 7A , \u2014R 7B , \u2014R 7C , \u2014R 7D , \u2014R 7E , \n -L 7 -R 7B , -L 7 -R 7C , -L 7 -R 7D , or -L 7 -R 7E ; \n \n each -L 7 - is independently linear or branched saturated C 1-6 alkylene; \n each \u2014R 7A  is independently linear or branched saturated C 1-6 alkyl, and is optionally substituted with one or more substituents \u2014W 1 ; \n each \u2014R 7B  is saturated C 3-6 cycloalkyl, and is optionally substituted with one or more substituents \u2014W 2 ; \n each \u2014R 7C  is non-aromatic C 3-7 heterocyclyl, and is optionally substituted with one or more substituents \u2014W 2 ; \n each \u2014R 7D  is phenyl or naphthyl, and is optionally substituted with one or more substituents \u2014W 3 ; \n each \u2014R 7E  is C 5-12 heteroaryl, and is optionally substituted with one or more substituents \u2014W 3 ; \n each \u2014W 1  is independently: \n \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014CF 3 , \u2014OH, \u2014OR W1 , \u2014OCF 3 , \u2014NH 2 , \u2014NHR W1 , \u2014NR W1 2 , pyrrolidino, piperidino, morpholino, piperazino, N\u2014(R W1 )-piperazino, \u2014C(\u2550O)OH, \u2014C(\u2550O)OR W1 , \u2014C(\u2550O)NH 2 , \u2014C(\u2550O)NHR W1 , \u2014C(\u2550O)NR W1 2 , \u2014C(\u2550O)-pyrrolidino, \u2014C(\u2550O)-piperidino, \u2014C(\u2550O)-morpholino, \u2014C(\u2550O)-piperazino, \u2014C(\u2550O)\u2014N\u2014(R W1 )-piperazino, \u2014S(\u2550O)R W1 , \u2014S(\u2550O) 2 R W1 , \u2014S(\u2550O) 2 NH 2 , \u2014S(\u2550O) 2 NHR W1 , \u2014S(\u2550O) 2 NR W1 2 , \u2014S(\u2550O) 2 pyrrolidino, \u2014S(\u2550O) 2 -piperidino, \u2014S(\u2550O) 2 -morpholino, \u2014S(\u2550O) 2 -piperazino, \u2014S(\u2550O) 2 \u2014N\u2014(R W1 )-piperazino, \u2014CN, or \u2014NO 2 ; \n wherein each \u2014R W1  is independently linear or branched saturated C 1-6 alkyl, phenyl, or \u2014CH 2 -phenyl, wherein each phenyl is optionally substituted with one or more groups selected from \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014R W11 , \u2014CF 3 , \u2014OH, \u2014OR W11 , and \u2014OCF 3 , wherein each \u2014R W11  is independently linear or branched saturated C 1-6 alkyl; \n each \u2014W 2  is independently: \n \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014R W2 , \u2014CF 3 , \u2014OH, \u2014OR W2 , \u2014OCF 3 , \u2014NH 2 , \u2014NHR W2 , \u2014NR W2 2 , pyrrolidino, piperidino, morpholino, piperazino, N\u2014(R W2 )-piperazino, \u2014C(\u2550O)OH, \u2014C(\u2550O)OR W2 , \u2014C(\u2550O)NH 2 , \u2014C(\u2550O)NHR W2 , \u2014C(\u2550O)NR W2 2 , \u2014C(\u2550O)-pyrrolidino, \u2014C(\u2550O)-piperidino, \u2014C(\u2550O)-morpholino, \u2014C(\u2550O)-piperazino, \u2014C(\u2550O)\u2014N\u2014(R W2 )-piperazino, \u2014S(\u2550O)R W2 , \u2014S(\u2550O) 2 R W2 , \u2014S(\u2550O) 2 NH 2 , \u2014S(\u2550O) 2 NHR W2 , \u2014S(\u2550O) 2 NR W2 2 , \u2014S(\u2550O) 2 pyrrolidino, \u2014S(\u2550O) 2 -piperidino, \u2014S(\u2550O) 2 -morpholino, \u2014S(\u2550O) 2 -piperazino, \u2014S(\u2550O) 2 \u2014N\u2014(R W2 )-piperazino, \u2014CN, or \u2014NO 2 ; \n wherein each \u2014R W2  is independently linear or branched saturated C 1-6 alkyl, phenyl, or \u2014CH 2 -phenyl, wherein each phenyl is optionally substituted with one or more groups selected from \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014R W22 , \u2014CF 3 , \u2014OH, \u2014OR W22 , and \u2014OCF 3 , wherein each \u2014R W22  is independently linear or branched saturated C 1-6 alkyl; \n each \u2014W 3  is independently: \n \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014R W3 , \u2014CF 3 , \u2014OH, \u2014OR W3 , \u2014OCF 3 , \u2014NH 2 , \u2014NHR W3 , \u2014NR W3 2 , pyrrolidino, piperidino, morpholino, piperazino, N\u2014(R W3 )-piperazino, \u2014C(\u2550O)OH, \u2014C(\u2550O)OR W3 , \u2014C(\u2550O)NH 2 , \u2014C(\u2550O)NHR W3 , \u2014C(\u2550O)NR W3 2 , \u2014C(\u2550O)-pyrrolidino, \u2014C(\u2550O)-piperidino, \u2014C(\u2550O)-morpholino, \u2014C(\u2550O)-piperazino, \u2014C(\u2550O)\u2014N\u2014(R W3 )-piperazino, \u2014S(\u2550O)R W3 , \u2014S(\u2550O) 2 R W3 , \u2014S(\u2550O) 2 NH 2 , \u2014S(\u2550O) 2 NHR W3 , \u2014S(\u2550O) 2 NR W3 2 , \u2014S(\u2550O) 2 pyrrolidino, \u2014S(\u2550O) 2 -piperidino, \u2014S(\u2550O) 2 -morpholino, \u2014S(\u2550O) 2 -piperazino, \u2014S(\u2550O) 2 \u2014N\u2014(R W3 )-piperazino, \u2014CN, or \u2014NO 2 ; \n wherein each \u2014R W3  is independently linear or branched saturated C 1-6 alkyl, phenyl, or \u2014CH 2 -phenyl, wherein each phenyl is optionally substituted with one or more groups selected from \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014R W33 , \u2014CF 3 , \u2014OH, \u2014OR W33 , and \u2014OCF 3 , wherein each \u2014R W33  is independently linear or branched saturated C 1-6 alkyl; \n \u2014R 3  is independently \u2014R 3A  or \u2014R 3B ; \n \u2014R 3A  is independently linear or branched saturated C 1-6 alkyl; \n \u2014R 3B  is independently saturated C 3-7 cycloalkyl; \n \u2014R 2  is independently \u2014H or \u2014R 2A ; \n \u2014R 2A  is independently \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014R 2AA , \u2014CF 3 , \u2014OH, \u2014OR 2AA , \u2014OCF 3 , \u2014NH 2 , \u2014NHR 2AA , \u2014NR 2AA 2 , pyrrolidino, piperidino, morpholino, piperazino, N\u2014(R 2AA )-piperazino, \u2014SH, \u2014SR 2AA , or \u2014CN; \n each \u2014R 2AA  is independently linear or branched saturated C 1-6 alkyl; \n \u2014R 6  is independently \u2014H or \u2014R 6A ; \n \u2014R 6A  is independently \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014R 6AA , \u2014CF 3 , \u2014OH, \u2014OR 6AA , \u2014OCF 3 , \u2014NH 2 , \u2014NHR 6AA , \u2014NR 6AA 2 , pyrrolidino, piperidino, morpholino, piperazino, N\u2014(R 6AA )-piperazino, \u2014SH, \u2014SR 6AA , or \u2014CN; and \n each \u2014R 6AA  is independently linear or branched saturated C 1-6 alkyl.

Metadata:
- Claim Count in Document: 11.0
- Percentile: 90.0
- Lexical Diversity: 1.8
- Patent Class: 544.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15117982', '12631373', '13773052', '12843494', '13060154']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7382288355503315
- 35 USC 102 Novelty (BERT): 0.6489870415341521
- Combined Prediction Score: 0.7293046561487136
- Mean Citation Score: 400.453204
- Max Citation Score: 741.6448
- Similarity Product: 561.0927100013732

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