PATENT CLAIM ANALYSIS

Application Number: 15860781
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-07
Patent Classification: ["544", "331000"]

Abstract:
Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X 1 , X 2 , X 3  and X 4  have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.

Claim (Index 1):
A method for treating a RET-associated cancer, the method comprising:\n (a) detecting a dysregulation of a RET gene, a RET kinase, or the expression or activity or level of any of the same in a sample from a patient; and (b) administering to the patient a therapeutically effective amount of a compound having the Formula I or a pharmaceutically acceptable salt or solvate thereof: wherein:\n X 1  is CH or N; \n X 2  is CH or N; \n X 3  is CH or N; \n X 4  is CH or N; \n wherein one or two of X 1 , X 2 , X 3  and X 4  is N; \n A is CN; \n B is hetAr 1 ; \n hetAr 1  is a 5-membered heteroaryl ring having 1-3 ring nitrogen atoms, wherein said heteroaryl ring is optionally substituted with one or more substituents independently selected from the group consisting of halogen, C1-C6 alkyl, hydroxyC1-C6 alkyl, fluoroC1-C6 alkyl, difluoroC1-C6 alkyl, trifluoroC1-C6 alkyl, cyanoC1-C6 alkyl, (C1-C6 alkoxy)C1-C6 alkyl, (C1-C4 alkoxy)CH 2 C(\u2550O)\u2014, (C1-C4 alkoxy)C(\u2550O)C1-C3 alkyl, C3-C6 cycloalkyl, (R a R b N)C1-C6 alkyl, (R a R b N)C(\u2550O)C1-C6 alkyl, (C1-C6 alkylSO 2 )C1-C6 alkyl, and 4-methoxybenzyl; \n R a  and R b  are independently H or C1-C6 alkyl; \n D is hetCyc 1 ; \n hetCyc 1  is a 4-6 membered heterocyclic ring having 1-2 ring nitrogen atoms, wherein said heterocyclic ring is optionally substituted with one or more substituents independently selected from the group consisting of C1-C3 alkyl, fluoroC1-C3 alkyl, difluoroC1-C3 alkyl, trifluoroC1-C3 alkyl and OH, or said heterocyclic ring is substituted with a C3-C6 cycloalkylidene ring, or said heterocyclic ring is substituted with an oxo group; \n E is \n (w) Ar 2 C(\u2550O)\u2014, \n (x) Ar 2 C1-C6 alkyl-, \n (z) Ar 2 (C1-C3 alkyl)C(\u2550O)\u2014 wherein said alkyl portion is optionally substituted with one or two groups independently selected from the group consisting of OH, C1-C6 alkyl (optionally substituted with 1-3 fluoros), hydroxyC1-C6 alkyl, C1-C6 alkoxy and R e R f N\u2014, where R e  and R f  are independently H or C1-C6 alkyl, or R e  and R f  together with the nitrogen to which they are attached form a 5-6 membered azacyclic ring optionally having an additional ring heteroatom selected from N and O, \n (cc) hetAr 2 (C1-C3 alkyl)C(\u2550O)\u2014, wherein said alkyl portion is optionally substituted with one or two groups independently selected from the group consisting of OH, C1-C6 alkyl, hydroxyC1-C6 alkyl, C1-C6 alkoxy and R e R f N\u2014, wherein R e  and R f  are independently H or C1-C6 alkyl or R e  and R f  together with the nitrogen to which they are attached form a 5-6 membered azacyclic ring optionally having an additional ring heteroatom selected from N and O, \n (dd) R 1 R 2 NC(\u2550O)\u2014, or \n (oo) hetAr 2 C1-C6 alkyl-; \n Ar 2  is phenyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkoxy (optionally substituted with 1-3 fluoros), fluoroC1-C6 alkyl, difluoroC1-C6 alkyl, trifluoroC1-C6 alkyl, CN, a 5-6 membered heterocyclic ring having 1-2 ring heteroatoms independently selected from N and O, and R i R j N\u2014 wherein R i  and R j  are independently H or C1-C6 alkyl; \n hetAr 2  is a 5-6 membered heteroaryl ring having 1-3 ring heteroatoms independently selected from N, O and S and optionally substituted with one or more substituents independently selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkoxy (optionally substituted with 1-3 fluoros), fluoroC1-C6 alkyl, difluoroC1-C6 alkyl, trifluoroC1-C6 alkyl, hydroxyC1-C6 alkyl, (C3-C6)cycloalkyl, (C1-C6 alkoxy)C1-C6 alkyl, CN, OH, and R\u2032R\u2033N\u2014, wherein R\u2032 and R\u2033 are independently H or C1-C3 alkyl; \n R 1  is H, C1-C6 alkyl or (C1-C6 alkoxy)C1-C6 alkyl; and \n R 2  is H, C1-C6 alkyl (optionally substituted with 1-3 fluoros), (C1-C6 alkoxy)C1-C6 alkyl (optionally substituted with 1-3 fluoros), hydroxyC1-C6 alkyl (optionally substituted with 1-3 fluoros), C1-C6 alkoxy (optionally substituted with 1-3 fluoros), (C1-C6 alkoxy)C(\u2550O), hydroxyC1-C6 alkoxy or (3-6C cycloalkyl)CH 2 O.

Metadata:
- Claim Count in Document: 77.0
- Percentile: 86.0
- Lexical Diversity: 1.63462
- Patent Class: 544.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15860849', '15858658', '15860852', '15860808', '15860894']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8325951038226911
- 35 USC 102 Novelty (BERT): 0.6282623923359223
- Combined Prediction Score: 0.8121618326740142
- Mean Citation Score: 555.9032100000002
- Max Citation Score: 590.9769
- Similarity Product: 548.8116267715216

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