PATENT CLAIM ANALYSIS

Application Number: 15747218
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-08
Patent Classification: ["514", "249000"]

Abstract:
Disclosed is a compound of Formula (I) or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein one R 3  is H and the other R 3  is an aryl group substituted with zero to 3 R 3a ; and R 1 , R 2 , and R 3a  are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors for the inhibition or prevention of platelet aggregation, and the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder. Also disclosed are methods of using such compounds for the treatment of human papillomavirus. Additionally, pharmaceutical compositions comprising at least one compound of Formula (I) are disclosed.

Claim (Index 9):
A method for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder, comprising the steps of administering to a patient in need thereof a therapeutically effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein:\n one R 1  is H and the other R 1  is F, Cl, \u2014OH, C 1-4  alkyl, C 1-4  fluoroalkyl, C 2-4  alkenyl, C 2-4  alkynyl, C 3-7  cycloalkyl, C 3-7  fluorocycloalkyl, C 1-3  alkoxy, C 1-3  fluoroalkoxy, C 2-4  hydroxyalkoxy, C 3-6  cycloalkoxy, (C 1-3  alkoxy)-(C 1-3  alkylene), (C 1-3  alkoxy)-(C 1-3  fluoroalkylene), (C 1-3  deuteroalkoxy)-(C 1-3  deuteroalkylene), (C 1-3  fluoroalkoxy)-(C 1-3  alkylene), \u2014(CH 2 ) 1-3 O(phenyl), \u2014(CH 2 ) 1-3 NR a R a , \u2014C(O)O(C 1-6  alkyl), \u2014C(O)NR a R a , \u2014C(O)NR b R b , \u2014NH 2 , \u2014NH(C 1-6  alkyl), \u2014N(C 1-4  alkyl) 2 , azetidin-1-yl, pyrrolidin-1-yl, furanyl, pyranyl, piperidin-1-yl, morpholin-4-yl, piperazin-1-yl, \u2014S(O) 2 (C 1-4  alkyl), \u2014S(O) 2 NR a R a , or C 1-3  alkylthio; \n one R 2  is H and the other R 2  is H, F, Cl, Br, \u2014OH, \u2014CN, C 1-4  alkyl, C 1-4  fluoroalkyl, C 1-4  hydroxyalkyl, C 1-3  aminoalkyl, C 2-4  alkenyl, C 2-4  alkynyl, C 3-7  cycloalkyl, C 3-7  fluorocycloalkyl, C 1-6  alkoxy, C 1-3  fluoroalkoxy, C 1-3  alkylthio, (C 1-3  alkoxy)-(C 1-3  alkylene), (C 1-3  fluoroalkoxy)-(C 1-3  alkylene), \u2014C(O)NH 2 , \u2014C(O)NH(C 1-6  alkyl), \u2014C(O)N(C 1-6  alkyl) 2 , \u2014C(O)NR b R b , \u2014C(O)O(C 1-6  alkyl), \u2014CH(OH)(C 3-6  cycloalkyl), \u2014CH(OH)phenyl), \u2014S(O) 2 (C 1-3  alkyl), \u2014S(O) 2 NR a R a , or a cyclic group selected from phenyl, 5- to 6-membered heteroaryl, and 5- to 7-membered heterocycle, wherein said cyclic group is substituted with zero to 5 substituents independently selected from F, Cl, C 1-3  alkoxy, and \u2014CN; \n one R 3  is H and the other R 3  is an aryl group substituted with zero to 3 R 3a ; \n R 3a , at each occurrence, is independently: \n (i) H, F, Cl, Br, \u2014CN, \u2014OH, C 1-3  alkyl, C 1-3  fluoroalkyl, C 1-6  hydroxyalkyl, C 1-6  alkoxy, C 1-3  fluoroalkoxy, C 3-6  cycloalkyl, C 3-6  fluorocycloalkyl, 3- to 6-membered heterocyclyl, \u2014CH(OH)(C 3-6  cycloalkyl), \u2014CH(OH)(aryl), \u2014CH(OH)(heteroaryl), (C 1-3  alkoxy)-(C 1-3  alkylene), \u2014(CH 2 ) 1-3 NR a R a , \u2014(CH 2 ) 1-4 NHS(O) 2 (aryl), \u2014O(CH 2 ) 1-3 (aryl), \u2014O(CH 2 ) 1-3 (thiazolyl), \u2014O(C 1-6  hydroxyalkyl), (C 1-3  alkoxy)-(C 1-6  alkoxy), \u2014O(CH 2 ) 1-4 O(aryl), \u2014O(CH 2 ) 1-4 O(CH 2 ) 1-3 (aryl), \u2014O(CH 2 ) 1-4 NR a R a , \u2014O(CH 2 ) 1-4 NHS(O) 2 (C 1-3  alkyl), \u2014O(CH 2 ) 1-4 NHS(O) 2 (aryl), \u2014O(CH 2 ) 1-4 C(O)OH, \u2014O(CH 2 ) 1-4 C(O)O(C 1-6  alkyl), \u2014O(CH 2 ) 1-4 C(O)NR a (CH 2 ) 0-3 (aryl), \u2014O(CH 2 ) 1-4 C(O)(morpholinyl), \u2014O(CH 2 ) 1-4 OC(O)O(C 1-3  alkyl), \u2014O(CH 2 ) 1-3 CHR a OC(O)NR a (CH 2 ) 1-4 C(O)NR a R a , \u2014O(CH 2 ) 1-4 OC(O)NR a (heteroaryl), \u2014O(imidazolyl substituted with aryl), \u2014C(O)OH, \u2014C(O)O(C 1-6  alkyl), \u2014NR a C(O)(furanyl), \u2014NR a C(O)(pyranyl), \u2014NR a C(O)O(C 1-6  alkyl), \u2014NR a C(O)O(CH 2 ) 1-4 (aryl), \u2014O(CH 2 ) 1-4 NR a C(O)O(C 1-6  alkyl), \u2014O(CH 2 ) 1-4 NR a C(O)O(CH 2 ) 1-4 (pyranyl), \u2014O(CH 2 ) 1-4 NR a C(O)O(CH 2 ) 1-4 (aryl), or \u2014O(CH 2 ) 1-4  NR a C(O)O(CH 2 ) 1-4 (furanyl), wherein each of said aryl or heteroaryl is substituted with zero to 5 substituents independently selected from F, Cl, \u2014CN, C 1-3  alkyl, C 1-3  fluoroalkyl, C 1-4  hydroxyalkyl, C 1-3  alkoxy, \u2014OCF 3 , \u2014OCHF 2 , \u2014NH 2 , \u2014NH(C 1-6  alkyl), \u2014N(C 1-6  alkyl) 2 , C 1-3  hydroxyalkoxy, \u2014CONR c R c , and \u2014S(O) 2 NR c R c ; (ii) \u2014O(CH 2 ) 1-4 NR a S(O) 2 R w , wherein R w  is aryl or heteroaryl substituted with zero to 2 substituents independently selected from F, Cl, \u2014CN, C 1-3  alkyl, C 1-3  alkoxy, \u2014OCF 3 , \u2014OCHF 2 , and C 1-3  fluoroalkyl; or (iii) \u2014O(CH 2 ) 1-4 OC(O)NR a R x , \u2014OCH(R d )(CH 2 ) 1-3 OC(O)NR a R x , \u2014O(CH 2 ) 1-4 CH(R d )OC(O)NR a R x , or \u2014OCH(R d )CH(R d )(CH 2 ) 0-2 OC(O)NR a R a , wherein R x  is selected from H, C 1-4  alkyl, C 1-4  fluoroalkyl, aryl, pyrrolyl, pyrazolyl, thiazolyl, heteroaryl, pyridazinyl, pyrimidinyl, oxadiazolyl, thiadiazolyl, indolyl, pyrrolo[2,3-b]pyridinyl, benzo[d]oxazol-2(3H)-onyl, and \u2014CH 2 (heteroaryl), each aryl, pyrrolyl, pyrazolyl, thiazolyl, heteroaryl, pyridazinyl, pyrimidinyl, oxadiazolyl, thiadiazolyl, indolyl, pyrrolo[2,3-b]pyridinyl, benzo[d]oxazol-2(3H)-onyl, and heteroaryl substituted with zero to 2 substituents independently selected from F, \u2014Cl, \u2014CN, C 1-3  alkyl, C 1-3  fluoroalkyl, C 1-6  hydroxyalkyl, C 1-6  hydroxyalkoxy, C 1-3  alkoxy, \u2014C(O)O(C 1-3  alkyl), \u2014C(O)NH 2 , \u2014C(O)NH(C 1-6  alkyl), \u2014C(O)N(C 1-6  alkyl) 2 , \u2014C(O)NR a (C 1-6  hydroxyalkyl), \u2014C(O)NR a R a , \u2014C(O)NR b R b , \u2014S(O) 2 NR a R a , and methyl triazolyl:\n R a , at each occurrence, is independently H or \u2014CH 3 ; \n two R b  along with the nitrogen atom to which they are attached form a 4- to 7-membered heterocyclo ring; \n R c , at each occurrence, is independently C 1-3  alkyl or C 1-3  hydroxyalkyl or two R c  along with the nitrogen atom to which they are attached form a monocyclic or a bicyclic heterocyclyl; and \n R d , at each occurrence, is independently C 1-6  alkyl, fluoroalkyl, C 1-6  hydroxyalkyl, (C 1-3  alkoxy)-(C 1-3  alkylene), (C 1-2  fluoroalkyl)-O\u2014(C 1-2  alkylene), (C 3-6  cycloalkyl)-(C 0-2  alkylene), aryl(C 1-2  alkylene), heteroaryl(C 1-2  alkylene), aryl-O\u2014(C 1-2  alkylene), or heteroaryl-O\u2014(C 1-2  alkylene); \n wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart or in the peripheral circulation.

Metadata:
- Claim Count in Document: 18.0
- Percentile: 86.0
- Lexical Diversity: 1.86957
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14747037', '14746908', '15549257', '15549307', '14396807']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7771001374030717
- 35 USC 102 Novelty (BERT): 0.5169751172390743
- Combined Prediction Score: 0.751087635386672
- Mean Citation Score: 293.59795
- Max Citation Score: 300.1764
- Similarity Product: 197.91364499065875

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