PATENT CLAIM ANALYSIS

Application Number: 15750704
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-08
Patent Classification: ["514", "211150"]

Abstract:
FGFR and VEGFR inhibitors are provided, and compounds represented by formula (1) or formula (II) as FGFR and VEGFR inhibitors, pharmaceutically acceptable salts or tautomers thereof are specifically disclosed.

Claim (Index 1):
A compound represented by formula (I) or formula (II), a pharmaceutically acceptable salt or a tautomer thereof, wherein, one of R 1  and R 2  is selected from the group consisting of F, Cl, Br, I, CN, OH and NH 2 , the other is selected from the group consisting of H, F, Cl, Br, I, CN, OH and NH 2 ; B 1  is selected from the group consisting of wherein, 0 to 2 of T 11-15  are selected from N and the rest are selected from C(R); 0 to 2 of T 16-18  are selected from N and the rest are selected from C(R); D 11  is selected from the group consisting of \u2014C(R)(R)\u2014, \u2014C(\u2550O)N(R)\u2014, \u2014N(R)\u2014, \u2014C(\u2550NR)\u2014, \u2014S(\u2550O) 2 N(R)\u2014, \u2014S(\u2550O)N(R)\u2014, \u2014O\u2014, \u2014S\u2014, \u2014C(\u2550O)O\u2014, \u2014C(\u2550O)\u2014, \u2014C(\u2550S)\u2014, \u2014S(\u2550O)\u2014, \u2014S(\u2550O) 2 \u2014 or \u2014N(R)C(\u2550O)N(R)\u2014; T 41  is selected from N or C(R); D 41  is selected from the group consisting of \u2014C(R)(R)\u2014, \u2014C(\u2550O)N(R)\u2014, \u2014N(R)\u2014, \u2014C(\u2550NR)\u2014, \u2014S(\u2550O) 2 N(R)\u2014, \u2014S(\u2550O)N(R)\u2014, \u2014O\u2014, \u2014S\u2014, \u2014C(\u2550O)O\u2014, \u2014C(\u2550O)\u2014, \u2014C(\u2550S)\u2014, \u2014S(\u2550O)\u2014, \u2014S(\u2550O) 2 \u2014 or \u2014N(R)C(\u2550O)N(R)\u2014; 0 to 2 of D 42-45  are each independently selected from the group consisting of a single bond, \u2014[C(R)(R)] 1-3 \u2014, \u2014C(\u2550O)N(R)\u2014, \u2014N(R)\u2014, \u2014C(\u2550NR)\u2014, \u2014S(\u2550O) 2 N(R)\u2014, \u2014S(\u2550O)N(R)\u2014, \u2014O\u2014, \u2014S\u2014, \u2014C(\u2550O)O\u2014, \u2014C(\u2550O)\u2014, \u2014C(\u2550S)\u2014, \u2014S(\u2550O)\u2014, \u2014S(\u2550O) 2 \u2014 or \u2014N(R)C(\u2550O)N(R)\u2014, the rest are selected \u2014C(R)(R)\u2014; optionally, any two of D 41-45  are connected to the same atom or atom group to form a 3-6 membered ring; L 1  and L 3  are each independently selected from the group consisting of \u2014(CRR) 0-3 \u2014, \u2014(CRR) 0-3 \u2014C(\u2550O)N(R)\u2014(CRR) 0-3 \u2014, \u2014(CRR) 0-3 \u2014N(R)\u2014(CRR) 0-3 \u2014, \u2014(CRR) 0-3 \u2014C(\u2550NR)\u2014(CRR) 0-3 \u2014, \u2014(CRR) 0-3 \u2014S(\u2550O) 2 N(R)\u2014(CRR) 0-3 \u2014, \u2014(CRR) 0-3 \u2014S(\u2550O)N(R)\u2014(CRR) 0-3 \u2014, \u2014(CRR) 0-3 \u2014O\u2014(CRR) 0-3 \u2014, \u2014(CRR) 0-3 \u2014S\u2014(CRR) 0-3 \u2014, \u2014(CRR) 0-3 \u2014C(\u2550O)O\u2014(CRR) 0-3 \u2014, \u2014(CRR) 0-3 \u2014C(\u2550O)\u2014(CRR) 0-3 \u2014, \u2014(CRR) 0-3 \u2014C(\u2550S)\u2014(CRR) 0-3 \u2014, \u2014(CRR) 0-3 \u2014S(\u2550O)\u2014(CRR) 0-3 \u2014, \u2014(CRR) 0-3 \u2014S(\u2550O) 2 \u2014(CRR) 0-3 \u2014 or \u2014(CRR) 0-3 \u2014N(R)C(\u2550O)N(R)\u2014(CRR) 0-3 \u2014; B 2  is selected from a 5- to 10-membered aryl or heteroaryl which is optionally substituted with R; B 4  is selected from a 5- to 6-membered aryl or heteroaryl and a 5- to 6-membered cycloalkyl or heterocycloalkyl, each of which is optionally substituted with R; T 31-34  are each independently selected from N or C(R); optionally, any two of T 31-34  are connected to the same atom or atom group to form a 3-6 membered ring; n is 0 or 1, and when n is 0, the defined structural unit represents a single bond for linkage; R is selected from the group consisting of H, F, Cl, Br, I, CN, OH, SH, NH 2 , CHO, COOH, C(\u2550O)NH 2 , S(\u2550O)NH 2 , S(\u2550O) 2 NH 2 , or selected from a C 1-12  alkyl or heteroalkyl, a C 3-12  cyclocarbyl or heterocyclocarbyl, and a C 1-12  alkyl or heteroalkyl substituted with a C 3-12  cyclocarbyl or heterocyclocarbyl; and the C 1-12  alkyl or heteroalkyl and the C 3-12  cyclocarbyl or heterocyclocarbyl is optionally substituted with R\u2032; R\u2032 is selected from the group consisting of F, Cl, Br, I, CN, OH, SH, NH 2 , CHO, COOH, C(\u2550O)NH 2 , S(\u2550O)NH 2 , S(\u2550O) 2 NH 2 , \u2550NH, \u2550O, \u2550S, or selected from the group optionally substituted with R\u2033 consisting of NHC(\u2550O)CH 3 , a C 1-12  alkyl, a C 1-12  alkylamino, N,N-di(C 1-12  alkyl)amino, a C 1-12  alkoxy, a C 1-12  alkanoyl, a C 1-12  alkoxycarbonyl, a C 1-12  alkylsulfonyl, a C 1-12  alkylsulfinyl, a 3- to 12-membered cycloalkyl, a 3- to 12-membered cycloalkylamino, a 3- to 12-membered heterocycloalkylamino, a 3- to 12-membered cycloalkyloxy, a 3- to 12-membered cycloalkylcarbonyl, a 3- to 12-membered cycloalkyloxycarbonyl, a 3- to 12-membered cycloalkylsulfonyl, a 3- to 12-cycloalkylsulfinyl, a 5- to 12-membered aryl or heteroaryl, a 5 to 12-membered aralkyl or heteroaralkyl; R\u2033 is selected from the group consisting of F, Cl, Br, I, CN, OH, N(CH 3 ) 2 , NH(CH 3 ), NH 2 , CHO, COOH, C(\u2550O)NH 2 , S(\u2550O)NH 2 , S(\u2550O) 2 NH 2 , \u2550NH, \u2550O, \u2550S, trihalomethyl, dihalomethyl, monohalomethyl, aminomethyl, hydroxymethyl, methyl, methoxy, formyl, methoxycarbonyl, methanesulfonyl, methylsulfinyl; \u201chetero\u201d represents a heteroatom or a heteroatom group selected from the group consisting of \u2014C(\u2550O)N(R)\u2014, \u2014N(R)\u2014, \u2014C(\u2550NR)\u2014, \u2014S(\u2550O) 2 N(R)\u2014, \u2014S(\u2550O)N(R)\u2014, \u2014O\u2014, \u2014S\u2014, \u2550O, \u2550S, \u2014C(\u2550O)O\u2014, \u2014C(\u2550O)\u2014, \u2014C(\u2550S)\u2014, \u2014S(\u2550O)\u2014, \u2014S(\u2550O) 2 \u2014 and/or \u2014N(R)C(\u2550O)N(R)\u2014; in each of the above cases, the number of R, R\u2032, R\u2033, heteroatoms or heteroatom groups is independently selected from 0, 1, 2 or 3; and the compound represented by formula (I) does not include

Metadata:
- Claim Count in Document: 4.0
- Percentile: 88.0
- Lexical Diversity: 1.44
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15548776', '16470111', '15812142', '15314599', '16317510']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.829093247661096
- 35 USC 102 Novelty (BERT): 0.5228628588429379
- Combined Prediction Score: 0.7984702087792803
- Mean Citation Score: 329.67529
- Max Citation Score: 341.71124
- Similarity Product: 269.6420757174253

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