PATENT CLAIM ANALYSIS

Application Number: 16067158
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2019-01
Patent Classification: ["514", "063000"]

Abstract:
The present invention discloses a nitrogen-containing fused heterocyclic compound, as well as a preparation method, intermediate, composition and application thereof. The nitrogen-containing fused heterocyclic compound of the present invention as represented by formula (I), as well as the pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, metabolite or drug precursor thereof, exhibit a high selectivity and a high inhibitory activity with respect to CDK4 and CDK6 at a molecular level, an excellent inhibitory activity with respect to breast cancer cells at a cellular level, and significant inhibition of tumor cell proliferation associated with cyclin-dependent kinase activity at an animal level. The invention also exhibits a good stability with respect to human or mouse liver microsomes without significant inhibition of metabolic enzymes, good in vivo absorption in mice and rats, a high bioavailability and good druggability.

Claim (Index 2):
The nitrogen-containing fused heterocyclic compound, the pharmaceutically acceptable salt, the enantiomer, the diastereomer, the tautomer, the solvate, the metabolite or the drug precursor thereof according to  claim 1 , wherein the C 2 -C 20  alkenyl contained in the term \u201csubstituted or unsubstituted C 2 -C 20  alkenyl\u201d and the term \u201cC 2 -C 20  alkenyl\u201d is independently C 2 -C 12  alkenyl;\n and/or, the C 2 -C 20  alkynyl contained in the term \u201csubstituted or unsubstituted C 2 -C 20  alkynyl\u201d and the term \u201cC 2 -C 20  alkynyl\u201d is independently C 2 -C 12  alkynyl; \n and/or, the C 1 -C 20  alkyl contained in the term \u201csubstituted or unsubstituted C 1 -C 20  alkyl\u201d, the term \u201cC 1 -C 20 alkyl\u201d and the term \u201cC 1 -C 20  alkyl mono-substituted, di-substituted or unsubstituted amino\u201d is independently C 1 -C 12  alkyl; \n and/or, the C 1 -C 20  alkylthio contained in the term \u201csubstituted or unsubstituted C 1 -C 20  alkylthio\u201d and \u201cC 1 -C 20  alkylthio\u201d is independently C 1 -C 12  alkylthio; \n and/or, the C 1 -C 20  alkoxy contained in the term \u201csubstituted or unsubstituted C 1 -C 20  alkoxy\u201d and the term \u201cC 1 -C 20  alkoxy\u201d is independently C 1 -C 12  alkoxy; \n and/or, the \u201cC 1 -C 20  silyl\u201d is independently \u201cC 1 -C 12  silyl\u201d; \n and/or, the C 3 -C 12  cycloalkyl contained in the term \u201csubstituted or unsubstituted C 3 -C 12  cycloalkyl\u201d is independently C 3 -C 8  cycloalkyl; \n and/or, the C 1 -C 9  heterocycloalkyl in the \u201csubstituted or unsubstituted C 1 -C 9  heterocycloalkyl\u201d is independently C 3 -C 8  heterocycloalkyl having the heteroatom selected from the group consisting of boron, silicon, oxygen, sulfur, selenium, nitrogen and phosphorus and the number of the heteroatom is 1 to 4; \n and/or, the C 1 -C 9  heteroaryl contained in the term \u201csubstituted or unsubstituted C 1 -C 9  heteroaryl\u201d is independently C 1 -C 6  heteroaryl; \n and/or, the C 3 -C 12  aryl contained in the term \u201csubstituted or unsubstituted C 3 -C 12  aryl\u201d is independently C 6 -C 10  aryl.

Metadata:
- Claim Count in Document: 1.0
- Percentile: 94.0
- Lexical Diversity: 1.8
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['12723137', '14132877', '14883720', '10572958', '15612670']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.840531685858968
- 35 USC 102 Novelty (BERT): 0.5332712291829999
- Combined Prediction Score: 0.8098056401913712
- Mean Citation Score: 369.647188
- Max Citation Score: 375.8492
- Similarity Product: 245.72044354639053

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

Dataset: test