PATENT CLAIM ANALYSIS

Application Number: 15757816
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-12
Patent Classification: ["514", "302000"]

Abstract:
The present invention relates to compounds of general formula I wherein the groups R, R 1 , R 2 , m and n are defined as in claim  1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.

Claim (Index 1):
A compound of formula I wherein R is selected from the group consisting of\n H, F, Cl, Br, I, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-6 -cycloalkyl, NC\u2014, HNR N \u2014C(\u2550O)\u2014, C 1-4 -alkyl-NR N \u2014C(\u2550O)\u2014, C 3-6 -cycloalkyl-NR N \u2014C(\u2550O)\u2014, heterocyclyl-NR N \u2014C(\u2550O)\u2014, heteroaryl-NR N \u2014C(\u2550O)\u2014, HOOC\u2014, C 1-4 -alkyl-O\u2014C(\u2550O)\u2014, O 2 N\u2014, HR N N\u2014, C 1-4 -alkyl-R N N\u2014, C 1-4 -alkyl-C(\u2550O)NR N \u2014, C 3-6 -cycloalkyl-C(\u2550O)NR N \u2014, heterocyclyl-C(\u2550O)NR N \u2014, heteroaryl-C(\u2550O)NR N \u2014, C 1-4 -alkyl-S(\u2550O) 2 NR N \u2014, C 3-6 -cycloalkyl-S(\u2550O) 2 NR N \u2014, heterocyclyl-S(\u2550O) 2 NR N \u2014, heteroaryl-S(\u2550O) 2 NR N \u2014, HO\u2014, C 1-6 -alkyl-O\u2014, HOOC\u2014C 1-3 -alkyl-O\u2014, heterocyclyl-C 1-3 -alkyl-O\u2014, phenyl C 1-3  alkyl O, C 3-6 -cycloalkyl-O\u2014, heterocyclyl-O\u2014, heteroaryl-O\u2014, C 1-4 -alkyl-S\u2014, C 3-6 -cycloalkyl-S\u2014, heterocyclyl-S\u2014, C 1-4 -alkyl-S(\u2550O)\u2014, C 3-6 -cycloalkyl-S(\u2550O)\u2014, heterocyclyl-S(\u2550O)\u2014, C 1-4 -alkyl-S(\u2550O) 2 \u2014C 3-6 -cycloalkyl-S(\u2550O) 2 \u2014, heterocyclyl-S(\u2550O) 2 \u2014, phenyl-S(\u2550O) 2 \u2014, heteroaryl-S(\u2550O) 2 \u2014, HNR N \u2014S(\u2550O) 2 \u2014, C 1-4 -alkyl-NR N \u2014S(\u2550O) 2 \u2014, heterocyclyl, phenyl, and heteroaryl, \n wherein each alkyl, cycloalkyl, and heterocyclyl group or sub-group within the groups forming R is optionally substituted with 1 or more F atoms and optionally substituted with 1 to 3 groups independently selected from the group consisting of Cl, C 1-3 -alkyl, NC\u2014, (R N ) 2 N\u2014, HO\u2014, C 1-3- alkyl-O\u2014, and C 1-3 -alkyl-S(\u2550O) 2 \u2014; and \n wherein each phenyl and heteroaryl group or sub-group within the groups forming R is optionally substituted with 1 to 5 substituents independently selected from the group consisting of F, Cl, C 1-3 -alkyl, HF 2 C\u2014, F 3 C\u2014, NC\u2014, (R N ) 2 N\u2014, HO\u2014, C 1-3 -alkyl-O\u2014, F 3 C\u2014O\u2014, and C 1-3 -alkyl-S(\u2550O) 2 \u2014; \n wherein each heterocyclyl group or sub-group within the groups forming R is selected from the group consisting of\n a cyclobutyl group wherein 1 CH 2  group is replaced by \u2014NR N \u2014 or \u2014O\u2014; \n a C 5-6 -cycloalkyl group wherein 1 CH 2  group is replaced by \u2014C(\u2550O)\u2014, \u2014NR N \u2014, \u2014O\u2014 or \u2014S(\u2550O) 2 \u2014 and/or 1 CH group is replaced by N; \n a C 5-6 -cycloalkyl group wherein 1 CH 2  group is replaced by \u2014NR N \u2014 or \u2014O\u2014, a second CH 2  group is replaced by \u2014NR N \u2014, \u2014C(\u2550O)\u2014 or \u2014S(\u2550O) 2 \u2014 and/or 1 CH group is replaced by N; and \n a C 5-6 -cycloalkyl group wherein 2 CH 2  groups are replaced by \u2014NR N \u2014 or 1 CH 2  group by \u2014NR N \u2014 and the other by \u2014O\u2014 and a third CH 2  group is replaced by \u2014C(\u2550O)\u2014 or \u2014S(\u2550O) 2 \u2014 and/or 1 CH group is replaced by N; \n \n wherein each heteroaryl group or sub-group within the groups forming R is selected from the group consisting of\n tetrazolyl and a 5- or 6-membered heteroaromatic ring which contains 1, 2, or 3 heteroatoms independently of each other selected from the group consisting of \u2550N\u2014, \u2014NR N \u2014, \n \u2014O\u2014, and \u2014S\u2014, wherein in heteroaromatic groups containing a \u2014HC\u2550N\u2014 unit this group is optionally replaced by \u2014NR N \u2014C(\u2550O)\u2014; \n \n wherein in heteroaryl and heterocyclyl rings with one or more NH groups, each of said NH groups is replaced by NR N , \n R 1  is selected from the group consisting of H, F, Cl, C 1-4 -alkyl, C 3-6 -cycloalkyl-, HO\u2014C 1-4 -alkyl, C 1-4 -alkyl-O\u2014C 1-4 -alkyl, NC\u2014, HO\u2014, C 1-4 -alkyl-O\u2014, C 3-6- cycloalkyl-O\u2014, C 1-4 -alkyl-S\u2014, C 1-4 -alkyl-S(O)\u2014, and C 1-4 -alkyl-S(O) 2 \u2014,\n wherein any alkyl and cycloalkyl group or sub-group within the groups forming R 1  is optionally substituted with 1 or more F atoms, and wherein multiple R 1  may be identical or different if m is 2, 3 or 4; \n m is an integer selected from the group consisting of 1, 2, 3, and 4; R 2  is H, F, Cl, C 1-4 -alkyl, NC\u2014, or C 1-4 -alkyloxy,\n wherein any alkyl group or sub-group within the groups forming R 2  is optionally substituted with 1 or more F atoms, and wherein multiple R 2  may be identical or different if n is 2 or 3; \n n is an integer selected from the group consisting of 1, 2, and 3; R N  is independently of each other selected from the group consisting of H, C 1-4 -alkyl, HO\u2014(C 1-4 -alkyl)-H 2 C\u2014, C 1-3 -alkyl-O\u2014C 1-4 -alkyl-, C 1-4 -alkyl-C(\u2550O)\u2014, C 1-4 -alkyl-NH\u2014C(\u2550O)\u2014, C 1-4 -alkyl-N(C 1-4 -alkyl)-C(\u2550O)\u2014, C 1-4 -alkyl-O\u2014C(\u2550O)\u2014, and C 1-4 -alkyl-S(\u2550O) 2 \u2014,\n wherein each alkyl group or sub-group within the groups forming R N  is optionally substituted with 1 or more F atoms; \n wherein in any definition mentioned hereinbefore and if not specified otherwise, any alkyl group or sub-group may be straight-chained or branched, or a salt thereof.

Metadata:
- Claim Count in Document: 26.0
- Percentile: 90.0
- Lexical Diversity: 1.70175
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15225038', '16484124', '15818790', '13803237', '15876237']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8179664945257652
- 35 USC 102 Novelty (BERT): 0.5502636183233535
- Combined Prediction Score: 0.7911962069055241
- Mean Citation Score: 390.195968
- Max Citation Score: 394.82303
- Similarity Product: 388.12557434210953

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