PATENT CLAIM ANALYSIS

Application Number: 16219589
Application Type: Utility
Filing Date: 2018-12
Publication Date: 2019-06
Patent Classification: ["514", "210180"]

Abstract:
The subject matter generally relates to methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.

Claim (Index 11):
A method of  claim 1 , wherein the PDE1 inhibitor is compound of Formula X, e.g.: Formula X-A Formula X-B wherein\n (i) Q is \u2014C(\u2550S)\u2014, \u2014C(\u2550O)\u2014, \u2014C(\u2550N(R 7 ))\u2014 or \u2014C(R 14 )(R 15 )\u2014; \n (ii) R 1  is H or C 1-6 alkyl (e.g., methyl or ethyl); \n (iii) R 2  is H, C 1-6 alkyl (e.g., isopropyl, isobutyl, 2-methylbutyl, 2,2-dimethylpropyl) wherein said alkyl group is optionally substituted with halo (e.g., fluoro) or hydroxy (e.g., 1-hydroxypropan-2-yl, 3-hydroxy-2-methylpropyl), for example, R 2  may be a trifluoromethyl or 2,2,2-trifluoroethyl, N(R 14 )(R 15 )\u2014C 1-6 alkyl (e.g., 2-(dimethylamino)ethyl or 2-aminopropyl), arylC 1-6 alkyl (e.g., phenyl or benzyl), heteroaryl C 1-6 alkyl (e.g., pyridinylmethyl), C 1-6 alkoxyaryl-C 1-6 alkyl (e.g., 4-methoxybenzyl); -G-J wherein:\n G is a single bond or, alkylene (e.g., methylene); J is cycloalkyl or heterocycloalkyl (e.g., oxetan-2-yl, pyrolyin-3-yl, pyrolyin-2-yl) optionally substituted with one or more C 1-6 alkyl (e.g., (1-methylpyrolidin-2-yl)), amino (e.g., \u2014NH 2 ), for example, -G-J may be \u2014C 0-4 alkyl-C 3-8 cycloalkyl (e.g., cyclopentyl, cyclohexyl or cyclopropylmethyl) optionally substituted with one or more C 1-6 alkyl, amino (e.g., \u2014NH 2 ), for example, 2-aminocyclopentyl or 2-aminocyclohexyl, wherein said cycloalkyl optionally contains one or more heteroatom selected from N and O (e.g., pyrrolidinyl, for example, pyrrolidin-3-yl or pyrrolidin-2-yl, 1-methyl-pyrrolindin-2-yl, 1-methyl-pyrrolindin-3-yl, 1-methyl-pyrrolindin-2-yl-methyl or 1-methyl-pyrrolindin-3-yl-methyl); \n \n (iv) R 3  is\n 1) -D-E-F wherein: \n D is a single bond, C 1-6 alkylene (e.g., methylene), or arylalkylene (e.g., p-benzylene or \u2014CH 2 C 6 H 4 \u2014); \n E is a single bond, \n C 1-6 alkylene (e.g., methylene) C 2-6 alkynylene (e.g., ethynylene, prop-2-yn-1-ylene), ethynylene, prop-2-yn-1-ylene), \u2014Co -4 alkylarylene (e.g., phenylene or \u2014C 6 H 4 \u2014, -benzyle{acute over (\u03b7)}\u03b5- or \u2014CH 2 C 6 H 4 \u2014), wherein the arylene group is optionally substituted with halo (e.g., Cl or F), heteroarylene (e.g., pyridinylene or pyrimidinylene), aminoC 1-6 alkylene (e.g., \u2014CH 2 N(H)\u2014), amino (e.g., \u2014N(H)\u2014); \n C 3-8 cycloalkylene optionally containing one or more heteroatom selected from N or O (e.g., piperidinylene), \n F is \n H, \n halo (e.g., F, Br, Cl), C 1-6 alkyl (e.g., isopropyl or isobutyl), haloC 1-6 alkyl (e.g., trifluoromethyl), \n aryl (e.g., phenyl), \n C 3-8 cycloalkyl optionally containing at least one atom selected from a group consisting of N or O (e.g., cyclopentyl, N cyclohexyl, piperidinyl, pyrrolidinyl, tetrahydro-2H-pyran-4-yl, or morpholinyl), said cycloalkyl is optionally substituted with C 1-6 alkyl (e.g., methyl or isopropyl), for example, 1-methylpyrrolidin-2-yl, pyrrolidin-1-yl, pyrrolidin-2-yl, piperidin-2-yl, 1-methyrpiperidin-2-yl, 1-ethylpiperidin-2-yl, heteroaryl optionally substituted with C 1-6 alkyl, (e.g., pyridyl, (for example, pyrid-2-yl), pyrimidinyl (for example, pyrimidin-2-yl), thiadiazolyl (for example, 1,2,3-thiadiazol-4-yl), diazolyl (e.g., pyrazolyl (for example, pyrazol-1-yl) or imidazolyl (for example, imidazol-1-yl, 4-methylimidazolyl, 1-methylimidazol-2-yl,), triazolyl (e.g., 1,2,4-triazol-1-yl), tetrazolyl (e.g., tetrazol-5-yl), alkoxadiazolyl (e.g., 5-methyl-1,2,4-oxadiazol), pyrazolyl (e.g., pyrazol-1-yl), wherein said \n heteroaryl is optionally substituted with halo (e.g., fluoro) or haloC 1-6 alkyl, for example, 6-fluoropyrid-2-yl; amino (e.g., \u2014NH 2 ), C 1-6 alkoxy, \u2014O-haloC 1-6 alkyl (e.g., \u2014O\u2014CF 3 ), C 1-6 alkylsulfonyl (for example, methylsulfonyl or \u2014S(O) 2 CH 3 ), \n \u2014C(O)\u2014R 13 , \n \u2014N(R 14 )(R 5 ); or \n \n 2) a substituted heteroarylaklyl, e.g., substituted with haloalkyl; or \n 3) attached to the nitrogen on the pyrrolo portion of Formula I and is a moiety of Formula A \n wherein X, Y and Z are, independently, N or C, and R 8 , R 9 , R 11  and R 12  are independently H or halogen (e.g., Cl or F); and R 10  is halogen, C 1-6 alkyl, C 1-6 alkoxy (e.g., methoxy), C 3-8 cycloalkyl, heteroC 3-8 cycloalkyl (e.g., pyrrolidinyl) haloC 1-6 alkyl (e.g., trifluoromethyl), aryl (e.g., phenyl), heteroaryl (e.g., pyridyl, (for example, pyrid-2-yl) or e.g., thiadiazolyl (for example, 1,2,3-thiadiazol-4-yl), diazolyl (e.g., imidazolyl or pyrazolyl), triazolyl (e.g., 1,2,4-triazol-1-yl), tetrazolyl (e.g., tetrazol-5-yl), alkoxadiazolyl (e.g., 5-methyl-1,2,4-oxadiazol), pyrazolyl (e.g., pyrazol-1-yl), C 1-6 alkyl sulfonyl (e.g., methyl sulfonyl), arylcarbonyl (e.g., benzoyl), heteroarylcarbonyl, alkoxycarbonyl, (e.g., methoxycarbonyl), aminocarbonyl; wherein the aryl, heteroaryl, cycloalkyl or heterocycloalkyl is optionally substituted with one or more C 1-6 alkyl (e.g., methyl), halogen (e.g., chloro or fluoro), haloC 1-6 alkyl (e.g., trifluoromethyl), hydroxy, carboxy, \u2014SH, or an additional aryl or heteroaryl (e.g., biphenyl or pyridylphenyl) preferably R 10  is phenyl or pyridyl, e.g., 2-pyridyl optionally substituted with the substituents previously defined; provided that when X, Y or X is nitrogen, R 8 , R 9  or R 10 , respectively, is not present; (v) R 4  and R 5  are independently H, C 1-6 alkyl (e.g., methyl, isopropyl), C 3-8 cycloalkyl (e.g., cyclopentyl), C 3-8 heterocycloalkyl (e.g., pyrrolidin-3-yl), aryl (e.g., phenyl) or heteroaryl (e.g., pyrid-4-yl, pyrid-2-yl or pyrazol-3-yl) wherein said aryl or heteroaryl is optionally substituted with halo (e.g., 4-fluorophenyl), hydroxy (e.g., 4-hydroxyphenyl), C 1-6 alkyl, C 1-6 alkoxy or another aryl group (e.g., biphenyl-4-ylmethyl); (vi) R 6  is H, C 1-6 alkyl (e.g., methyl), hydroxy, C 1-6 alkoxy, aryloxy, \u2014N(R 16 )(R 17 ), oxo (e.g., =0), or C 3-8 Cycloalkyl; (vii) R 7  is H, C 1-6 alkyl (e.g., methyl) or C 3-8 cycloalkyl wherein said cycloalkyl is optionally substituted with one or more oxo (e.g., 2,5-dioxopyrrolidin-1-yl); (viii) R 13  is \u2014N(R 14 )(R 15 ), C 1-6 alkyl (e.g., methyl), \u2014OC 1-6 alkyl (e.g., \u2014OCH 3 ), haloC 1-6 alkyl (trifluoromethyl), aryl (e.g., phenyl), or heteroaryl; and (ix) R 14  and R 15  are independently H or C 1-6 alkyl; (x) R 16  and R 17  are independently H, C 1-6 alkyl, aryl (e.g., phenyl), heteroaryl, wherein said aryl or heteroaryl is optionally substituted with halo (e.g., fluoro), C 1-6 alkoxy (e.g., methoxy); in free or salt form.

Metadata:
- Claim Count in Document: 2.0
- Percentile: 98.0
- Lexical Diversity: 1.54545
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14777448', '15406346', '14767489', '15709258', '14820323']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8049575987154317
- 35 USC 102 Novelty (BERT): 0.5553196652654214
- Combined Prediction Score: 0.7799938053704307
- Mean Citation Score: 348.187806
- Max Citation Score: 492.94012
- Similarity Product: 405.2202970195197

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