PATENT CLAIM ANALYSIS

Application Number: 15771487
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-11
Patent Classification: ["514", "217060"]

Abstract:
To provide a compound having an inhibitory activity for an androgen receptor. A fused pyrimidine compound represented by the following formula (I) or a pharmaceutically acceptable thereof (in the formula, X, Y, Z, R 1 , and R 2  are as defined in the specification).

Claim (Index 1):
A fused pyrimidine compound represented by formula (I): wherein, in the formula, X represents a cyano group or a nitro group; Y represents a halogen atom, a halogeno-C 1-3  alkyl group, a C 1-3  alkoxy group, or a C 1-3  alkyl group; Z represents a hydrogen atom, a halogen atom, or a C 1-3  alkyl group; R 1  represents a C 6-14  aryl group which is substituted with Ra and may be substituted simultaneously with Rb or a 5- or 6-membered heteroaryl group which is substituted with Ra and may be substituted simultaneously with Rb, wherein the Ra and Rb may be bonded to each other to form a fused ring together with the C 6-14  aryl group or the heteroaryl group; and R 2  represents a hydrogen atom, a C 1-3  alkyl group, or a cyano group, wherein Ra represents a phenyl group, a hydroxy-C 1-6  alkyl group, a hydroxy-C 3-7  cycloalkyl group, a hydroxy-heterocycloalkyl group, a C 1-6  alkoxy group which may be substituted with Rc, an amino-C 1-6  alkyl group which may be substituted with Rf, a halogeno-C 1-3  alkoxy group, a C 3-7  cycloalkylaminosulfonyl group, a C 1-3  alkylsulfonyl group, a 3- to 7-membered monocyclic heterocycloalkylsulfonyl group, a C 1-3  alkoxycarbonylamino group which may be substituted with a halogen, a C 1-3  alkylcarbonylamino group which may be substituted with a halogen, a 3- to 7-membered monocyclic heterocycloalkanecarbonyl group substituted with a hydroxy-C 1-6  alkyl group, a bicyclic heterocycloalkyl group, or \u2014(CH 2 ) n \u2014C(\u2550O)\u2014NRdRe; Rb represents a hydrogen atom, a halogen atom, a C 1-3  alkyl group which may be substituted with a halogen atom, or a C 1-4  alkoxy group which may be y substituted with a halogen atom; Rc represents a pyrazolyl group, triazolyl group, or tetrazolyl group which may be substituted or a piperazinyl group which may be substituted with Rf, Rd and Re each independently represent a hydrogen atom, a C 1-3  alkyl group, a C 2-6  alkynyl group, a C 1-6  alkoxy group, a C 3-7  cycloalkyl group, a halogeno-C 1-3  alkyl group, a hydroxy-C 1-6  alkyl group, a hydroxy-C 3-7  cycloalkyl group, a hydroxy-C 3-7  cycloalkyl-C 1-6  alkyl group, a C 1-4  alkoxy group, or a C 1-6  alkyl group substituted with Rg, or NRdRe of the \u2014(CH 2 ) n \u2014C(\u2550O)\u2014NRdRe may form a ring; Rf represents a C 1-6  alkyl group, a C 1-6  alkylcarbonyl group, a C 1-6  alkylsulfonyl group, a C 1-6  alkoxycarbonyl group, or a C 1-6  alkylaminocarbonyl group; Rg represents a C 1-6  alkylpyrazolyl group, a halogeno-C 1-3  alkylthiazolyl group, an oxadiazolyl group, a halogeno-C 1-3  alkyloxadiazolyl group, or a C 1-6  alkoxycarbonylamino group; and n represents an integer of from 0 to 3, provided that: if X is a cyano group, Y is a halogen atom or a halogeno-C 1-3  alkyl group, R 2  is a hydrogen atom, Z is a hydrogen atom, R 1  is a C 6-14  aryl group which is substituted with Ra and may be substituted simultaneously with Rb or a 5- or 6-membered heteroaryl group which is substituted with Ra and may be substituted simultaneously with Rb, and Rb is a hydrogen atom, a halogen atom, or a C 1-3  alkyl group which may be substituted with a halogen atom, then Ra is a hydroxy-heterocycloalkyl group, a C 1-6  alkoxy group which may be substituted with Rc, wherein Rc represents a piperazinyl group which may be substituted with C 1-6  alkyl, C 1-6  alkylcarbonyl, C 1-6  alkoxycarbonyl, or C 1-6  alkylaminocarbonyl, an amino-C 1-6  alkyl group which may be substituted with Rf, wherein Rf is as described above, a halogeno-C 1-3  alkoxy group, a C 1-3  alkylsulfonyl group, a bicyclic cycloheteroalkyl group, or (CH 2 ) n \u2014C(\u2550O)\u2014NRdRe, wherein n, Rd, and Re are as described above, provided that if either one of Rd and Re is a halogeno-C 1-3  alkyl group, a hydroxy-C 1-6  alkyl group, a hydroxy-C 3-7  cycloalkyl group, a hydroxy-C 3-7  cycloalkyl-C 1-6  alkyl group, or a C 1-6  alkyl group substituted with C 1-6  alkylpyrazolyl, halogeno-C 1-3  alkylthiazolyl, oxadiazolyl, or halogeno-C 1-3  alkyloxadiazolyl, then the other is not a hydrogen atom, or a pharmaceutically acceptable salt thereof.

Metadata:
- Claim Count in Document: 38.0
- Percentile: 91.0
- Lexical Diversity: 1.375
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15203059', '15893804', '15023894', '13394525', '13796928']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8335524906649661
- 35 USC 102 Novelty (BERT): 0.6002809405384869
- Combined Prediction Score: 0.8102253356523181
- Mean Citation Score: 457.957174
- Max Citation Score: 524.8892
- Similarity Product: 481.6236442993164

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

Dataset: test