PATENT CLAIM ANALYSIS

Application Number: 15767795
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-10
Patent Classification: ["514", "248000"]

Abstract:
The present invention provides compounds of Formula I: wherein Y, AA, W, R 3′  R 2 , R 4 , R 5 , R 6 , R 7 , X 1 , X 2 , X 3 , X 4  and X 5  are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug or esters or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.

Claim (Index 1):
A compound of Formula I: or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein: the dashed lines represent double-bonds with the proviso that only one of the two dashed line double bonds exists at the same time; X 1  is O and X 2  is \u2550N\u2014 or CR 1a ; or X 2  is S and X 1  is \u2550N\u2014 or CR 1a ; or X 1  is \u2550N\u2014 and X 2  is O or NR 1b ; or X 1  is NR 1b  and X 2  is CR 1a ; or X 1  is CR 1a  and X 2  is NR 1b ; X 3 , X 4 , and X 5  are independently selected from CR 1d  and \u2550N\u2014; R 1a  is selected from the group consisting of H, halo, cyano, C 1 -C 3  alkyl, C 3 -C 5  cycloalkyl, halo-C 1 -C 2 alkyl, and C 1 -C 3  alkoxy; R 1b  is selected from the group consisting of H, C 1 -C 3  alkyl, C 3 -C 5  cycloalkyl, and halo-C 1 -C 2 alkyl; R 1d  is selected from the group consisting of H, C 1 -C 4  alkyl, C 2 -C 4  alkenyl, C 2 -C 4  alkynyl, C 1 -C 4  alkoxy, C 1 -C 4  alkylthio, halo, OH, CN, OCF 3 , OCHF 2 , OCH 2 F, C 1 -C 2 -alkoxy-C 1 -C 2 -alkoxy, halo-C 1 -C 3 -alkyl, halo-C 1-2 -alkoxy, halo-C 1-2 -alkylthio, benzyloxy substituted (on the phenyl of said benzyl) by 0 to 3 groups independently selected from the group consisting of halo, C 1 -C 4  alkoxy, C 1 -C 4  alkyl, cyclopropyl, CF 3 , OCF 3 , 5- or 6-membered heteroaryl, OH, OCHF 2 , di-C 1 -C 4 -alkylamino, and cyano, and \u2014(CH 2 ) n -phenyl substituted by 0 to 3 groups independently selected from the group consisting of halo, C 1 -C 4  alkoxy, C 1 -C 4  alkyl, cyclopropyl, CF 3 , OCF 3 , 5- or 6-membered heteroaryl, OH, OCHF 2 , di-C 1 -C 4 -alkylamino, and cyano; n is 1 or 2; Y is S, O or \u2014CR 1e \u2550CR 1f \u2014; R 1e  is independently at each occurrence selected from the group consisting of H, halo, cyano, C 1 -C 3  alkyl, C 3 -C 5  cycloalkyl, halo-C 1 -C 2  alkyl, C 1 -C 3  alkoxy, and halo-C 1 -C 3  alkoxy; R 1f  is independently at each occurrence selected from the group consisting of H, halo, cyano, C 1 -C 3  alkyl, C 3 -C 5  cycloalkyl, halo-C 1 -C 2  alkyl, C 1 -C 3  alkoxy, and halo-C 1 -C 3  alkoxy; R 2  is H, halo, C 1 -C 3  alkyl, halo-C 1 -C 2  alkyl, C 1 -C 3  alkoxy, halo-C 1 -C 3  alkoxy, CN or C 3 -C 5  cycloalkyl; R 3  is selected from the group consisting of C 1-4  alkyl, C 1-4  alkoxy, C 1-4  alkylthio, C 1-2  haloalkyl, C 1-2  haloalkoxy, C 1-2  haloalkylthio, C 3-4  cycloalkyl, halo-C 3-4  cycloalkyl, C 1-4  alkylamino, di-C 1-4  alkylamino, (C 1-2  alkoxy) C 1-2  alkyl, halo(C 1-2  alkoxy) C 1-2  alkyl, C 2-3  alkenyl, C 2-3  alkynyl, tetrahydrofuran-2-yl, and halo; W is O or S; R 4  and R 5  are independently selected from H, C 1 -C 6  alkyl, C 1 -C 4  fluoroalkyl, and C 1 -C 4  hydroxyalkyl, or R 4  and R 5  can be taken together with the carbon to which they are attached to form a C 3 -C 7  cycloalkyl ring; is a 4-8 membered saturated heterocyclic ring containing 1-3 ring atoms which may be the same or different, each being independently selected from the group consisting of N, O and S, wherein said ring may be optionally fused to a C 6 -C 10  aryl or a 5-6 membered heteroaryl ring, further wherein said ring AA and optional fused ring may be unsubstituted or independently substituted with 0-1 R 6 , 0-4 R 7  or both 0-1 R 6  and 0-4 R 7  substituents;\n R 6  is selected from the group consisting of C 6 -C 10  aryl, 5-10 membered heteroaryl, 4-8 membered saturated heterocyclic ring, or C 3 -C 8  cycloalkyl ring, wherein each of said C 6 -C 10  aryl, 5-10 membered heteroaryl, 4-8 membered saturated heterocyclic ring, or C 3 -C 8  cycloalkyl ring, can be substituted with 0-4 R 7a  substituents; \n R 7  is independently selected at each occurrence from the group consisting of halo, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, halo C 1 -C 4  alkyl, halo C 1 -C 4  alkoxy, C 1 -C 4  alkylthio, halo C 1 -C 4  alkylthio, hydroxy, hydroxy C 1 -C 4  alkyl, hydroxy C 1 -C 4  alkoxy, (C 1 -C 6  alkyl)carboxy-, carboxy, \u2014C(O)Oalkyl, \u2014C(O)NH 2 , \u2014C(O)NHalkyl, \u2014C(O)N-dialkyl, \u2014NH 2 , (alkyl)amino-, (dialkyl)amino-, \u2014NH-carboxy-C 1 -C 6  alkyl, nitro, cyano, oxo, (haloaryl)alkyl-, C 3 -C 6  cycloalkyl, \u2014S(O)-alkyl, \u2014S(O)-aryl, \u2014S(O)-heteroaryl, \u2014S(O 2 )alkyl, \u2014S(O 2 )aryl, \u2014S(O 2 )heteroaryl, \u2014S(O 2 )NH 2 , \u2014S(O 2 )NHalkyl, \u2014S(O 2 )N-dialkyl, or if two R 7  substituents are attached to the same carbon atom, they may be taken together with the carbon atom to which they are attached to form a C 3 -C 6  cycloalkyl group or a 3-6 membered heterocyclic ring, or if two R 7  substituents are attached to adjacent carbon atoms, they may be taken together with the carbon atoms to which they are attached to form a C 3 -C 6  cycloalkyl group or a 3-6 membered heterocyclic ring; and \n R 7a  is independently selected at each occurrence from the group consisting of halo, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, halo C 1 -C 4  alkyl, halo C 1 -C 4  alkoxy, C 1 -C 4  alkylthio, halo C 1 -C 4  alkylthio, hydroxy, hydroxy C 1 -C 4  alkyl, hydroxy C 1 -C 4  alkoxy, (C 1 -C 6  alkyl)carboxy-, carboxy, \u2014C(O)Oalkyl, \u2014C(O)NH 2 , \u2014C(O)NHalkyl, \u2014C(O)N-dialkyl, \u2014NH 2 , (alkyl)amino-, (dialkyl)amino-, \u2014NHC(O)O\u2014C 1 -C 6  alkyl, \u2014NHC(O)-halo C 1 -C 6  alkyl, nitro, cyano, oxo, C 3 -C 6  cycloalkyl, \u2014S(O)\u2014 alkyl, \u2014S(O)-aryl, \u2014S(O)-heteroaryl, \u2014S(O 2 )alkyl, \u2014S(O 2 )aryl, \u2014S(O 2 )heteroaryl, \u2014S(O 2 )NH 2 , \u2014S(O 2 )NHalkyl, \u2014S(O 2 )N-dialkyl, aryl C 1 -C 4  alkoxy, \u2014C(O)aryl, \u2014C(O)\u2014C 1 -C 6  alkyl, or if two R 7a  substituents are attached to the same carbon atom, they may be taken together with the carbon atom to which they are attached to form a C 3 -C 6  cycloalkyl group or a 3-6 membered heterocyclic ring, or if two R 7a  substituents are attached to adjacent carbon atoms, they may be taken together with the carbon atoms to which they are attached to form a C 3 -C 6  cycloalkyl group or a 3-6 membered heterocyclic ring.

Metadata:
- Claim Count in Document: 22.0
- Percentile: 91.0
- Lexical Diversity: 1.71186
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15549307', '15549257', '14396831', '15593534', '14396807']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8466313559657416
- 35 USC 102 Novelty (BERT): 0.5510453950789274
- Combined Prediction Score: 0.8170727598770602
- Mean Citation Score: 404.92014600000016
- Max Citation Score: 412.2366
- Similarity Product: 398.6478329293728

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

Dataset: test