PATENT CLAIM ANALYSIS

Application Number: 16148647
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-01
Patent Classification: ["546", "221000"]

Abstract:
The compound of the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P 2  antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P 2 -mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.

Claim (Index 1):
A method of preparing a compound of formula (I-A): wherein R 1  is (1) a C1-8 alkyl group which may be substituted with 1 to 5 R 21  groups, (2) a C2-8 alkenyl group which may be substituted with 1 to 5 R 21  groups, (3) a C2-8 alkynyl group which may be substituted with 1 to 5 R 21  groups, (4) a C3-7 carbocycle which may be substituted with 1 to 5 substituents selected from the group consisting of a C1-4 alkyl group, a C1-4 haloalkyl group, a C1-4 alkoxy group and a halogen atom, or (5) \u2014CONR 31 R 32 ; R 21  is (1) a halogen atom, (2) \u2014OR 22  (wherein, R 22  is (1) a hydrogen atom, (2) a C1-4 alkyl group or (3) a C1-4 haloalkyl group), (3) \u2014NR 23 R 24  (wherein, R 23  and R 24  each independently are (1) a hydrogen atom or (2) a C1-4 alkyl group) or (4) an oxo group; R 31  and R 32  each independently are (1) a hydrogen atom or (2) a C1-4 alkyl group; R 3  and R 4  each independently are (1) a halogen atom, (2) a C1-4 alkyl group, (3) a C1-4 haloalkyl group, (4) a C1-4 alkoxy group, (5) a hydroxy group, (6) -L-CONR 6 R 7 , (7) -L-SO 2 R 8  or (8) -L-COOR 9 ; R 5  is (1) a halogen atom, (2) a C1-4 alkyl group or (3) a C1-4 haloalkyl group; L is (1) a bond, (2) a group represented by the formula: wherein A is (1) a bond or (2) an oxygen atom; R 12  and R 13  each independently are (1) a hydrogen atom, (2) a C1-4 alkyl group, (3) a hydroxy group or (4) NH 2  or (5) R 12  and R 13  together with the carbon atom to which they are attached may form a C3-7 carbocycle; and the arrow on the right hand side binds to \u2014CONR 6 R 7 , \u2014SO 2 R 8  or \u2014COOR 9 , (3) a C2-4 alkenylene group, (4) a \u2014O\u2014C2-4 alkenylene group, (5) an oxygen atom or (6) a nitrogen atom which may be substituted with a C1-4 alkyl group; R 6  and R 7  each independently are (1) a hydrogen atom, (2) a C1-4 alkyl group, (3) a C1-4 haloalkyl group, (4) a hydroxy group, (5) \u2014CONR 15 R 16 , (6) \u2014SO 2 NR 15 R 16 , (7) \u2014COR 17  or (8) \u2014SO 2 R 17 , or R 6  and R 7  together with the nitrogen atom to which they are attached may form a 4- to 7-membered nitrogen-containing saturated heterocycle that may be substituted with a hydroxy group; R 8  is (1) a C1-4 alkyl group, (2) a C1-4 haloalkyl group or (3) NR 10 R 11 ; R 9  is (1) a hydrogen atom or (2) a C1-8 alkyl group; R 10  and R 11  each independently are (1) a hydrogen atom, (2) a C1-4 alkyl group, (3) \u2014CONR 15 R 16 , (4) \u2014SO 2 NR 15 R 16 , (5) \u2014COR 17  or (6) \u2014SO 2 R 17 ; the ring 1 and the ring 2 each independently are a 5- to 7-membered cyclic group; R 15  and R 16  each independently are (1) a hydrogen atom, (2) a C1-4 alkyl group or (3) a 5- to 7-membered cyclic group; R 17  is (1) a C1-4 alkyl group or (2) a 5- to 7-membered cyclic group; n is an integer of 1 to 2; m is an integer of 1 to 2; p is an integer of 0 to 5; q is an integer of 0 to 5; r is an integer of 0 to 4; t is an integer of 1 to 4; when p is 2 or more, a plurality of R 3  groups may be the same or different; when q is 2 or more, a plurality of R 4  groups may be the same or different; when r is 2 or more, a plurality of R 5  groups may be the same or different; and when t is 2 or more, a plurality of R 12  and R 13  groups may be respectively the same or different, or a salt thereof, wherein the method comprises:\n reacting a compound of formula (E): \n wherein T is a protecting group of the amino group and the other symbols have the same definitions as above, in the presence of a base with a compound of formula (V) wherein all symbols have the same definitions as above, in an organic solvent.

Metadata:
- Claim Count in Document: 32.0
- Percentile: 97.0
- Lexical Diversity: 1.32143
- Patent Class: 546.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15089690', '14592100', '15784376', '14347178', '14780152']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8166503636057508
- 35 USC 102 Novelty (BERT): 0.567990163404944
- Combined Prediction Score: 0.7917843435856702
- Mean Citation Score: 379.053078
- Max Citation Score: 439.05518
- Similarity Product: 427.9624080175663

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