PATENT CLAIM ANALYSIS

Application Number: 16279291
Application Type: Utility
Filing Date: 2019-02
Publication Date: 2019-06
Patent Classification: ["514", "258100"]

Abstract:
Disclosed are a condensed-ring pyrimidylamino derivative, a preparation method therefor, and an intermediate, a pharmaceutical composition and applications thereof. The method for preparing the condensed-ring pyrimidylamino derivative comprises: in a solvent, in the presence of a palladium-containing catalyst, allowing a compound represented by formula I-a and a compound represented by formula I-b′ to have a coupling reaction, and then preparing a compound represented by formula I by means of a deprotection reaction. Also disclosed applications of the condensed-ring pyrimidylamino derivative in the preparation of drugs for preventing, relieving and/or treating tumors or diseases caused by an anaplastic lymphoma kinase. The condensed-ring pyrimidylamino derivative of the present invention has an obvious restraint effect on the anaplastic lymphoma kinase.

Claim (Index 1):
A condensed-ring pyrimidylamino derivative having a structure of formula II-2, a tautomer, a mesomer, a racemate, a stereoisomer, a pharmaceutically acceptable salt or a prodrug thereof: wherein, V is a chemical bond or \u2014CONH\u2014; ring A is an aromatic ring or a heteroaromatic ring; R 1  is selected from hydrogen atom, hydroxyl, a halogen, an alkyl, a sulfonyl, an alkoxy, formyl, amino, an amide or a heteroaryl, or the two adjacent R 1 (s) and the two atoms on the ring A connected to them form a 5- to 7-membered heterocyclic ring together; in the heterocyclic ring, the heteroatom(s) is(are) oxygen and/or nitrogen, the number of the heteroatom(s) is 1 to 4, and the number of carbon atom(s) is 1 to 6; where, in R 1 , the alkyl, the alkoxy, the formyl, the amino, the sulfonyl or the heteroaryl are optionally independently substituted by a substituent selected from the group consisting of a halogen, a C 1-10  alkyl, hydroxy, amino, a C 1-10  alkoxy, a C 1-4  sulfonyl and a heterocycloalkyl having 3 to 8 carbon atoms in which the heteroatom is oxygen and/or nitrogen and the number of the heteroatom(s) is 1 to 4; the heterocyclic ring is further substituted by a substituent selected from the group consisting of a C 1-4  alkyl; R 2  is selected from an amide or a heterocycloalkyl which is piperidinyl; where, in R 2 , the heterocycloalkyl which is piperidinyl is optionally substituted by a substituent selected from the group consisting of: hydroxy, a C 1-4  alkyl and a C 1-4  acyl; or R 2  is ring B is an aromatic ring or a heteroaromatic ring, the heteroaromatic ring is a heteroaromatic ring having 2 to 3 carbon atoms in which the heteroatom is nitrogen atom and the number of the heteroatom(s) is 1 or 2; m is 1 or 2; when the ring B is an aromatic ring, m is 2, the two adjacent R 3 (s) together with the carbon atom on the ring B to which they are attached to form a 5- to 7-membered heterocyclyl; the heterocyclyl is a heterocyclyl wherein the heteroatom is selected from the group consisting of oxygen, nitrogen and sulfur, the number of the heteroatoms is 1 to 4, and the number of carbon atoms is 2 to 6; when the ring B is a heteroaromatic ring, m is 1 or 2, R 3  is selected from the group consisting of a hydrogen atom, a hydroxyl, a halogen, an alkyl and an alkoxy, or the two adjacent R 3 (s) together with the carbon atom on the ring B to which they are attached to form a 5- to 7-membered heterocyclyl; the heterocyclyl is a heterocyclyl wherein the heteroatom is selected from the group consisting of oxygen, nitrogen and sulfur, the number of the heteroatoms is 1 to 4, and the number of carbon atoms is 2 to 6; where in R 3 , the hydroxyl, the alkyl or the alkoxy is optionally independently substituted by a substituent selected from the group consisting of a halogen, a C 1-4  alkyl, hydroxy, amino, a C 1-4  alkoxy, a C 1-4  sulfonyl and an amide; and the heterocyclyl is optionally substituted by a substituent selected from the group consisting of a C 1-4  alkyl; R 4  is selected from hydrogen atom, a halogen or an alkyl; n is 1 or 2; and the amide is

Metadata:
- Claim Count in Document: 44.0
- Percentile: 99.0
- Lexical Diversity: 1.95455
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15568999', '15985848', '15559181', '15746254', '15025618']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7922919440696082
- 35 USC 102 Novelty (BERT): 0.5861685060061739
- Combined Prediction Score: 0.7716796002632648
- Mean Citation Score: 351.83731
- Max Citation Score: 477.65143
- Similarity Product: 439.4650037315864

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