PATENT CLAIM ANALYSIS

Application Number: 15860894
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-05
Patent Classification: ["514", "210210"]

Abstract:
Provided herein are compounds of the Formula I: or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X 1 , X 2 , X 3 , X 4 , Ring D, E, R a , R b , n and m 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 RET-associated diseases and disorders.

Claim (Index 1):
A method for treating a RET-associated cancer, the method comprising:\n (a) detecting 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 Formula I or a pharmaceutically acceptable salt or solvate thereof: and pharmaceutically acceptable salts and solvates thereof, wherein: X 1 , X 2 , X 3  and X 4  are independently CH or N, wherein zero, one or two of X 1 , X 2 , X 3  and X 4  is N; A is CN; B is: (b) C1-C6 alkyl optionally substituted with 1-3 fluoros, (c) hydroxyC2-C6 alkyl- wherein the alkyl portion is optionally substituted with a C3-C6 cycloalkylidene ring, or (i) (hetCyc a )C1-C3 alkyl-; hetCyc a  is a 4-6 membered heterocyclic ring having 1-2 ring heteroatoms independently selected from N and O and optionally substituted with one or more substituents independently selected from OH, C1-C6 alkyl (optionally substituted with 1-3 fluoros), hydroxyC1-C6 alkyl, halogen, (C1-C6 alkyl)C(\u2550O)\u2014, C1-C6 alkoxy, oxo, and (C1-C6 alkoxy)C(\u2550O)\u2014; Ring D is a saturated monocyclic 4-7 membered heterocyclic ring having one ring heteroatom which is nitrogen; each R a  is independently C1-C6 alkyl (optionally substituted with 1-3 fluoros); R b  is (a) hydroxy; n is 0 or 1; m is 0 or 1; E is: (e) hetAr 2 C1-C6 alkyl-, (h) hetAr 2 \u2014O\u2014, (k) R 3 C(\u2550O)NR g \u2014 where R g  is H or C1-C6 alkyl, (l) Ar 1 C(\u2550O)NR g \u2014 where R g  is H or C1-C6 alkyl, or (m) hetAr 2 C(\u2550O)NR g (CH 2 ) p \u2014 where p is 0 or 1 and R g  is H or C1-C6 alkyl; Ar 1  is phenyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, C1-C6 alkyl (optionally substituted with 1-3 fluoros), C1-C6 alkoxy (optionally substituted with 1-3 fluoros), (C1-C6 alkoxy)C1-C6 alkyl- (optionally substituted with 1-3 fluoros), C3-C6 cycloalkyl, hydroxyC1-C6 alkyl, (C1-C6 alkyl)SO 2 \u2014, R e R f N\u2014 and (R e R f N)C1-C6 alkyl- where each R e  and R f  is independently H or C1-C6 alkyl; hetAr 2  is a 5-6 membered heteroaryl ring having 1-3 ring heteroatoms independently selected from N, O and S, or a 9-10 membered bicyclic heteroaryl having 1-2 ring nitrogen atoms, wherein hetAr 2  is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, C1-C6 alkyl (optionally substituted with 1-3 fluoros), C1-C6 alkoxy (optionally substituted with 1-3 fluoros), (C1-C6 alkoxy)C1-C6 alkyl- (optionally substituted with 1-3 fluoros) and hydroxyC1-C6 alkoxy-; R 3  is C1-C6 alkyl (optionally substituted with 1-3 fluoros), hydroxyC1-C6 alkyl-, C1-C6 alkoxy, C3-C6 cycloalkyl, (C3-C6 cycloalkyl)CH 2 \u2014, (C3-C6 cycloalkyl)O\u2014, (C3-C6 cycloalkyl)CH 2 O\u2014, hetCyc 7 O\u2014, Ph-O\u2014, or (C1-C6 alkoxy)C1-C6 alkyl-; wherein each of said C3-C6 cycloalkyl moieties is optionally substituted with C1-C6 alkyl (optionally substituted with 1-3 fluoros), C1-C6 alkoxy, OH, or R\u2032R\u2033N\u2014 where R\u2032 and R\u2033 are independently hydrogen or C1-C6 alkyl; and hetCyc 7  is a 5-7 membered heterocyclic ring having 1-3 ring heteroatoms independently selected from N, O and S.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 86.0
- Lexical Diversity: 1.6
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15861244', '15860808', '15860852', '15858929', '15858240']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8190321104473408
- 35 USC 102 Novelty (BERT): 0.6511002257810066
- Combined Prediction Score: 0.8022389219807073
- Mean Citation Score: 599.3505399999998
- Max Citation Score: 612.18823
- Similarity Product: 606.8591922226882

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