PATENT CLAIM ANALYSIS

Application Number: 15937475
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-08
Patent Classification: ["548", "373100"]

Abstract:
There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.

Claim (Index 19):
A pharmaceutical composition comprising a pharmaceutically acceptable excipient in combination with a compound according to  claim 1  or a compound as set forth below:\n Compound 36, 1-(5-{[(4-fluorophenyl)methyl]amino}-3-phenyl-1H-pyrazol-1-yl)-2,2-dimethylpropan-1-one; \n Compound 37, 1-(5-{[(4-fluorophenyl)methyl]amino}-3-(pyridin-3-yl)-1H-pyrazol-1-yl)-2,2-dimethylpropan-1-one; \n Compound 38, 1-(5-{[(4-fluorophenyl)methyl]amino}-4-methyl-3-phenyl-1H-pyrazol-1-yl)-2,2-dimethylpropan-1-one; \n Compound 39, 1-(5-{[(4-fluorophenyl)methyl]amino}-3-(pyridin-2-yl)-1H-pyrazol-1-yl)-2,2-dimethylpropan-1-one; \n Compound 40, 1-(5-{[(4-fluorophenyl)methyl]amino}-3-(pyridin-2-yl)-1H-pyrazol-1-yl)propan-1-one; \n Compound 41, 1-[(2-chlorophenyl)carbonyl]-N-[(4-fluorophenyl)methyl]-3-(pyridin-2-yl)-1H-pyrazol-5-amine; \n Compound 74, 1-(5-{[(4-fluorophenyl)methyl]amino}-3-(pyridin-3-yl)-1H-pyrazol-1-yl)propan-1-one; \n Compound 84, 1-(5-{[(4-fluorophenyl)methyl]amino}-3-phenyl-1H-pyrazol-1-yl)propan-1-one; \n Compound 85, 1-(5-{[(4-fluorophenyl)methyl]amino}-4-methyl-3-phenyl-1H-pyrazol-1-yl)propan-1-one; \n Compound 103, 1-[(2-amino-4-methoxyphenyl)carbonyl]-N-benzyl-3-(2-fluorophenyl)-1H-pyrazol-5-amine; \n Compound 105, 1-[(2-amino-4-methoxyphenyl)carbonyl]-N-benzyl-3-(pyridin-2-yl)-1H-pyrazol-5-amine; \n Compound 106, 1-[(2-amino-4-methylphenyl)carbonyl]-N-benzyl-3-(2-fluorophenyl)-1H-pyrazol-5-amine; \n Compound 108, 1-[(2-amino-4-methylphenyl)carbonyl]-N-benzyl-3-(pyridin-2-yl)-1H-pyrazol-5-amine; \n Compound 114, 1-[(2-chlorophenyl)carbonyl]-N-[(4-fluorophenyl)methyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 116, 1-[(2-methoxyphenyl)carbonyl]-3-(pyridin-2-yl)-N-(thiophen-2-ylmethyl)-1H-pyrazol-5-amine; \n Compound 118, 1-[(2-methoxyphenyl)carbonyl]-3-(pyridin-2-yl)-N-(thiophen-3-ylmethyl)-1H-pyrazol-5-amine; \n Compound 133, 1-[5-(benzylamino)-3-(2-fluorophenyl)-1H-pyrazol-1-yl]-2,2-dimethylpropan-1-one; \n Compound 134, 1-[5-(benzylamino)-3-(2-fluorophenyl)-1H-pyrazol-1-yl]-3-methylbutan-1-one; \n Compound 143, 1-[5-(benzylamino)-3-(pyridin-2-yl)-1H-pyrazol-1-yl]-2,2-dimethylpropan-1-one; \n Compound 144, 1-[5-(benzylamino)-3-(pyridin-2-yl)-1H-pyrazol-1-yl]-3-methylbutan-1-one; \n Compound 165, 1-{5-[(furan-2-ylmethyl)amino]-3-(pyridin-2-yl)-1H-pyrazol-1-yl}-2,2-dimethylpropan-1-one; \n Compound 166, 1-{5-[(furan-3-ylmethyl)amino]-3-(pyridin-2-yl)-1H-pyrazol-1-yl}-2,2-dimethylpropan-1-one; \n Compound 167, 2,2-dimethyl-1-[3-(pyridin-2-yl)-5-[(thiophen-2-ylmethyl)amino]-1H-pyrazol-1-yl]propan-1-one; \n Compound 168, 2,2-dimethyl-1-[3-(pyridin-2-yl)-5-[(thiophen-3-ylmethyl)amino]-1H-pyrazol-1-yl]propan-1-one; \n Compound 201, N-(furan-2-ylmethyl)-1-[(2-methoxyphenyl)carbonyl]-3-(pyridin-2-yl)-1H-pyrazol-5-amine; \n Compound 202, N-(furan-3-ylmethyl)-1-[(2-methoxyphenyl)carbonyl]-3-(pyridin-2-yl)-1H-pyrazol-5-amine; \n Compound 208, N-[(4-fluorophenyl)methyl]-1-[(2-methoxyphenyl)carbonyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 234, N-benzyl-1-[(2,4-dimethoxyphenyl)carbonyl]-3-(2-fluorophenyl)-1H-pyrazol-5-amine; \n Compound 236, N-benzyl-1-[(2,4-dimethoxyphenyl)carbonyl]-3-(pyridin-2-yl)-1H-pyrazol-5-amine; \n Compound 241, N-benzyl-1-[(2-bromophenyl)carbonyl]-3-(pyridin-2-yl)-1H-pyrazol-5-amine; \n Compound 242, N-benzyl-1-[(2-chlorophenyl)carbonyl]-3-(2-fluorophenyl)-1H-pyrazol-5-amine; \n Compound 244, N-benzyl-1-[(2-chlorophenyl)carbonyl]-3-(pyridin-2-yl)-1H-pyrazol-5-amine; \n Compound 247, N-benzyl-1-[(2-ethylphenyl)carbonyl]-3-(pyridin-2-yl)-1H-pyrazol-5-amine; \n Compound 251, N-benzyl-1-[(2-fluorophenyl)carbonyl]-3-(pyridin-2-yl)-1H-pyrazol-5-amine; \n Compound 256, N-benzyl-1-[(2-methoxyphenyl)carbonyl]-3-(pyridin-2-yl)-1H-pyrazol-5-amine; \n Compound 260, N-benzyl-1-[(2-methylphenyl)carbonyl]-3-(pyridin-2-yl)-1H-pyrazol-5-amine; \n Compound 276, N-benzyl-1-{[2-(propan-2-yl)phenyl]carbonyl}-3-(pyridin-2-yl)-1 H-pyrazol-5-amine; \n Compound 277, N-benzyl-3-(2-fluorophenyl)-1-[(2-fluorophenyl)carbonyl]-1H-pyrazol-5-amine; \n Compound 278, N-benzyl-3-(2-fluorophenyl)-1-[(2-methoxyphenyl)carbonyl]-1H-pyrazol-5-amine; \n Compound 418, 1-[5-(benzylamino)-3-(pyridin-3-yl)-1H-pyrazol-1-yl]-2-methylpropan-1-one; \n Compound 419, 1-[5-(benzylamino)-3-(pyridin-3-yl)-1H-pyrazol-1-yl]-2-phenylethan-1-one; \n Compound 420, 1-[5-(benzylamino)-3-(pyridin-3-yl)-1H-pyrazol-1-yl]-3-methylbutan-1-one; \n Compound 421, 1-[5-(benzylamino)-3-(pyridin-3-yl)-1H-pyrazol-1-yl]-3-phenylpropan-1-one; \n Compound 422, 1-[5-(benzylamino)-3-(pyridin-3-yl)-1H-pyrazol-1-yl]butan-1-one; \n Compound 423, 1-[5-(benzylamino)-3-(pyridin-3-yl)-1H-pyrazol-1-yl]ethan-1-one; \n Compound 424, 1-[5-(benzylamino)-3-(pyridin-3-yl)-1H-pyrazol-1-yl]propan-1-one; \n Compound 436, 1-[5-(benzylamino)-3-phenyl-1H-pyrazol-1-yl]-2-methylpropan-1-one; \n Compound 437, 1-[5-(benzylamino)-3-phenyl-1H-pyrazol-1-yl]-2-phenylethan-1-one; \n Compound 438, 1-[5-(benzylamino)-3-phenyl-1H-pyrazol-1-yl]-3-methylbutan-1-one; \n Compound 439, 1-[5-(benzylamino)-3-phenyl-1H-pyrazol-1-yl]-3-phenylpropan-1-one; \n Compound 440, 1-[5-(benzylamino)-3-phenyl-1H-pyrazol-1-yl]butan-1-one; \n Compound 441, 1-[5-(benzylamino)-3-phenyl-1H-pyrazol-1-yl]ethan-1-one; \n Compound 442, 1-[5-(benzylamino)-3-phenyl-1H-pyrazol-1-yl]propan-1-one; \n Compound 460, 1-benzoyl-3-(pyridin-3-yl)-N-(pyridin-3-ylmethyl)-1H-pyrazol-5-amine; \n Compound 461, 1-benzoyl-3-(pyridin-3-yl)-N-(pyridin-3-ylmethyl)-1H-pyrazol-5-amine; \n Compound 463, 1-benzoyl-3-(pyridin-3-yl)-N-(pyridin-4-ylmethyl)-1H-pyrazol-5-amine; \n Compound 464, 1-benzoyl-3-(pyridin-3-yl)-N-(pyridin-4-ylmethyl)-1H-pyrazol-5-amine; \n Compound 470, 1-benzoyl-3-phenyl-N-(pyridin-2-ylmethyl)-1H-pyrazol-5-amine; \n Compound 471, 1-benzoyl-3-phenyl-N-(pyridin-2-ylmethyl)-1H-pyrazol-5-amine; \n Compound 474, 1-benzoyl-3-phenyl-N-(pyridin-3-ylmethyl)-1H-pyrazol-5-amine; \n Compound 475, 1-benzoyl-3-phenyl-N-(pyridin-3-ylmethyl)-1H-pyrazol-5-amine; \n Compound 476, 1-benzoyl-3-phenyl-N-(pyridin-4-ylmethyl)-1H-pyrazol-5-amine; \n Compound 477, 1-benzoyl-3-phenyl-N-(pyridin-4-ylmethyl)-1H-pyrazol-5-amine; \n Compound 479, 1-benzoyl-N-(pyridin-2-ylmethyl)-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 480, 1-benzoyl-N-(pyridin-2-ylmethyl)-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 491, 1-benzoyl-N-[(2-chlorophenyl)methyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 495, 1-benzoyl-N-[(2-chlorophenyl)methyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 497, 1-benzoyl-N-[(2-fluorophenyl)methyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 500, 1-benzoyl-N-[(2-fluorophenyl)methyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 502, 1-benzoyl-N-[(2-methoxyphenyl)methyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 506, 1-benzoyl-N-[(2-methoxyphenyl)methyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 508, 1-benzoyl-N-[(2-methylphenyl)methyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 512, 1-benzoyl-N-[(2-methylphenyl)methyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 514, 1-benzoyl-N-[(3-chlorophenyl)methyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 518, 1-benzoyl-N-[(3-chlorophenyl)methyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 520, 1-benzoyl-N-[(3-fluorophenyl)methyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 523, 1-benzoyl-N-[(3-fluorophenyl)methyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 526, 1-benzoyl-N-[(3-methoxyphenyl)methyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 530, 1-benzoyl-N-[(3-methoxyphenyl)methyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 533, 1-benzoyl-N-[(3-methylphenyl)methyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 537, 1-benzoyl-N-[(3-methylphenyl)methyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 538, 1-benzoyl-N-[(4-chlorophenyl)methyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 541, 1-benzoyl-N-[(4-chlorophenyl)methyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 542, 1-benzoyl-N-[(4-fluorophenyl)methyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 544, 1-benzoyl-N-[(4-fluorophenyl)methyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 545, 1-benzoyl-N-[(4-methoxyphenyl)methyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 547, 1-benzoyl-N-[(4-methoxyphenyl)methyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 549, 1-benzoyl-N-[(4-methylphenyl)methyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 553, 1-benzoyl-N-[(4-methylphenyl)methyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 560, 1-benzoyl-N-benzyl-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 561, 1-benzoyl-N-benzyl-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 562, 1-benzoyl-N-benzyl-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 563, 1-benzoyl-N-benzyl-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 564, 1-benzoyl-N-benzyl-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 565, 1-benzoyl-N-benzyl-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 572, 1-benzoyl-N-benzyl-3-phenyl-1H-pyrazol-5-amine; \n Compound 573, 1-benzoyl-N-benzyl-3-phenyl-1H-pyrazol-5-amine; \n Compound 574, 1-benzoyl-N-benzyl-3-phenyl-1H-pyrazol-5-amine; \n Compound 575, 1-benzoyl-N-benzyl-3-phenyl-1H-pyrazol-5-amine; \n Compound 576, 1-benzoyl-N-benzyl-3-phenyl-1H-pyrazol-5-amine; \n Compound 577, 1-benzoyl-N-benzyl-3-phenyl-1H-pyrazol-5-amine; \n Compound 581, 1-benzoyl-N-{[2-(dimethylamino)phenyl]methyl}-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 585, 1-benzoyl-N-{[2-(dimethylamino)phenyl]methyl}-3-phenyl-1H-pyrazol-5-amine; \n Compound 589, 1-benzoyl-N-{[3-(dimethylamino)phenyl]methyl}-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 593, 1-benzoyl-N-{[3-(dimethylamino)phenyl]methyl}-3-phenyl-1H-pyrazol-5-amine; \n Compound 596, 1-benzoyl-N-{[4-(dimethylamino)phenyl]methyl}-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 599, 1-benzoyl-N-{[4-(dimethylamino)phenyl]methyl}-3-phenyl-1H-pyrazol-5-amine; \n Compound 602, 2-({[1-benzoyl-3-(pyridin-3-yl)-1H-pyrazol-5-yl]amino}methyl)benzonitrile; \n Compound 606, 2-{[(1-benzoyl-3-phenyl-1H-pyrazol-5-yl)amino]methyl}benzonitrile; \n Compound 609, 2-{[5-(benzylamino)-3-(pyridin-3-yl)-1H-pyrazol-1-yl]carbonyl}benzonitrile; \n Compound 613, 2-{[5-(benzylamino)-3-phenyl-1H-pyrazol-1-yl]carbonyl}benzonitrile; \n Compound 617, 3-({[1-benzoyl-3-(pyridin-3-yl)-1H-pyrazol-5-yl]amino}methyl)benzonitrile; \n Compound 621, 3-{[(1-benzoyl-3-phenyl-1H-pyrazol-5-yl)amino]methyl}benzonitrile; \n Compound 625, 3-{[5-(benzylamino)-3-(pyridin-3-yl)-1H-pyrazol-1-yl]carbonyl}benzonitrile; \n Compound 629, 3-{[5-(benzylamino)-3-phenyl-1H-pyrazol-1-yl]carbonyl}benzonitrile; \n Compound 633, 4-({[1-benzoyl-3-(pyridin-3-yl)-1H-pyrazol-5-yl]amino}methyl)benzonitrile; \n Compound 637, 4-{[(1-benzoyl-3-phenyl-1H-pyrazol-5-yl)amino]methyl}benzonitrile; \n Compound 641, 4-{[5-(benzylamino)-3-(pyridin-3-yl)-1H-pyrazol-1-yl]carbonyl}benzonitrile; \n Compound 645, 4-{[5-(benzylamino)-3-phenyl-1H-pyrazol-1-yl]carbonyl}benzonitrile; \n Compound 648, N-benzyl-1-[(2-chlorophenyl)carbonyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 650, N-benzyl-1-[(2-chlorophenyl)carbonyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 652, N-benzyl-1-[(2-fluorophenyl)carbonyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 655, N-benzyl-1-[(2-fluorophenyl)carbonyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 656, N-benzyl-1-[(2-methoxyphenyl)carbonyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 657, N-benzyl-1-[(2-methoxyphenyl)carbonyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 658, N-benzyl-1-[(2-methylphenyl)carbonyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 662, N-benzyl-1-[(2-methylphenyl)carbonyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 664, N-benzyl-1-[(3-chlorophenyl)carbonyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 668, N-benzyl-1-[(3-chlorophenyl)carbonyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 670, N-benzyl-1-[(3-fluorophenyl)carbonyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 673, N-benzyl-1-[(3-fluorophenyl)carbonyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 674, N-benzyl-1-[(3-methoxyphenyl)carbonyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 678, N-benzyl-1-[(3-methoxyphenyl)carbonyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 680, N-benzyl-1-[(3-methylphenyl)carbonyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 684, N-benzyl-1-[(3-methylphenyl)carbonyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 686, N-benzyl-1-[(4-chlorophenyl)carbonyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 689, N-benzyl-1-[(4-chlorophenyl)carbonyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 690, N-benzyl-1-[(4-fluorophenyl)carbonyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 692, N-benzyl-1-[(4-fluorophenyl)carbonyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 693, N-benzyl-1-[(4-methoxyphenyl)carbonyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 697, N-benzyl-1-[(4-methoxyphenyl)carbonyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 699, N-benzyl-1-[(4-methylphenyl)carbonyl]-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 702, N-benzyl-1-[(4-methylphenyl)carbonyl]-3-phenyl-1H-pyrazol-5-amine; \n Compound 714, N-benzyl-1-{[2-(dimethylamino)phenyl]carbonyl}-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 718, N-benzyl-1-{[2-(dimethylamino)phenyl]carbonyl}-3-phenyl-1H-pyrazol-5-amine; \n Compound 722, N-benzyl-1-{[3-(dimethylamino)phenyl]carbonyl}-3-(pyridin-3-yl)-1H-pyrazol-5-amine; \n Compound 726, N-benzyl-1-{[3-(dimethylamino)phenyl]carbonyl}-3-phenyl-1H-pyrazol-5-amine; \n Compound 730, N-benzyl-1-{[4-(dimethylamino)phenyl]carbonyl}-3-(pyridin-3-yl)-1H-pyrazol-5-amine; and \n Compound 734, N-benzyl-1-{[4-(dimethylamino)phenyl]carbonyl}-3-phenyl-1H-pyrazol-5-amine.

Metadata:
- Claim Count in Document: 9.0
- Percentile: 90.0
- Lexical Diversity: 1.60526
- Patent Class: 548.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['13630201', '14776612', '15605566', '15811220', '14776641']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7978884269738863
- 35 USC 102 Novelty (BERT): 0.5801058472647487
- Combined Prediction Score: 0.7761101690029726
- Mean Citation Score: 464.241458
- Max Citation Score: 486.57462
- Similarity Product: 433.2359452487647

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