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 10):
A method of  claim 1 , wherein the PDE1 inhibitor is compound of Formula IX: wherein\n (i) Q is \u2014C(\u2550S)\u2014, \u2014C(\u2550N(R 6 ))\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\n H, \n C 1-6 alkyl (e.g., isopropyl, isobutyl, 2-methylbutyl or 2,2-dimethylpropyl) wherein said alkyl group is optionally substituted with one or more halo (e.g., fluoro) or hydroxy (e.g., hydroxyC 1-6 alkyl, for example 1-hydroxyprop-2-yl or 3-hydroxy-2-methylpropyl), \n haloC 1-6 alkyl (e.g., trifluoromethyl or 2,2,2-trifluoroethyl), \n N(R 14 )(R 15 )\u2014C 1-6 alkyl (e.g., 2-(dimethylamino)ethyl or 2-aminopropyl), \n arylC 0-6 alkyl (e.g., phenyl or benzyl), wherein said aryl is optionally substituted with one or more C 1-6 alkoxy, for example, C 1-6 alkoxyarylC 0-6 alkyl (e.g., 4-methoxybenzyl), \n heteroarylC 0-6 alkyl (e.g., pyridinylmethyl), wherein said heteroaryl is optionally substituted with one or more C 1-6 alkoxy (e.g., C 1-6 alkoxyheteroarylC 1-6 alkyl); \n G-J wherein G is a single bond or C 1-6 alkylene (e.g., methylene) and J is C 3-8 cycloalkyl or heteroC 3-8 cycloalkyl (e.g., oxetan-2-yl, pyrrolidin-3-yl, pyrrolidin-2-yl) wherein the cycloalkyl and heterocycloalkyl group are optionally substituted with one or more C 1-6 alkyl or amino, for example,\n \u2014C 0-4 alkyl-C 3-8 cycloalkyl (e.g., \u2014C 0-4 alkyl-cyclopentyl, \u2014C 0-4 alkyl-cyclohexyl or \u2014C 0-4 alkyl-cyclopropyl), wherein said cycloalkyl is optionally substituted with one or more C 1-6 alkyl or amino (for example, 2-aminocyclopentyl or 2-aminocyclohexyl), \n \u2014C 0-4 alkyl-C 3-8 heterocycloalkyl (e.g., \u2014C 0-4 alkyl-pyrrolidinyl, for example, \u2014C 0-4 alkylpyrrolidin-3-yl) wherein said heterocycloalkyl is optionally substituted with C 1-6 alkyl (e.g., methyl), for example, 1-methylpyrrolidin-3-yl, 1-methyl-pyrrolindin-2-yl, 1-methyl-pyrrolindin-2-yl-methyl or 1-methyl-pyrrolindin-3-yl-methyl); \n \n \n (iv) R 3  is\n 4) -D-E-F wherein:\n D is a single bond, C 1-6 alkylene (e.g., methylene), or arylC 1-6 alkylene (e.g., benzylene or \u2014CH 2 C 6 H 4 \u2014); \n E is\n a single bond, \n C 1-4 alkylene (e.g., methylene, ethynylene, prop-2-yn-1-ylene), \n C 0-4 alkylarylene (e.g., phenylene or \u2014C 6 H 4 \u2014, -benzylene- or \u2014CH 2 C 6 H 4 \u2014), wherein the arylene group is optionally substituted with halo (e.g., Cl or F), \n heteroarylene (e.g., pyridinylene or pyrimidinylene), \n aminoC 1-6 alkylene (e.g., \u2014CH 2 N(H)\u2014), \n 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 \n F is\n H, \n halo (e.g., F, Br, Cl), \n C 1-6 alkyl (e.g., isopropyl or isobutyl), \n haloC 1-6 alkyl (e.g., trifluoromethyl), \n aryl (e.g., phenyl), \n C 3-8 cycloalkyl optionally containing one or more atom selected from a group consisting of N, S or O (e.g., cyclopentyl, cyclohexyl, piperidinyl, pyrrolidinyl, tetrahydro-2H-pyran-4-yl, or morpholinyl), and optionally substituted with one or more 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-methylpiperidin-2-yl, 1-ethylpiperidin-2-yl, \n heteroaryl (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), alkyloxadiazolyl (e.g., 5-methyl-1,2,4-oxadiazol), wherein said heteroaryl is optionally substituted with one or more C 1-6 alkyl, halo (e.g., fluoro) or haloC 1-6 alkyl; \n C 1-6 alkoxy, \n \u2014O-haloC 1-6 alkyl (e.g., \u2014O\u2014CF 3 ), \n C 1-6 alkylsulfonyl (for example, methylsulfonyl or \u2014S(O) 2 CH 3 ), \n \u2014C(O)\u2014R 13 , wherein 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; \n \u2014N(R 14 )(R 15 ); \n \n or \n \n 5) a substituted heteroarylC 1-6 aklyl, e.g., substituted with haloC 1-6 alkyl;\n or \n \n 6) attached to one of the nitrogens on the pyrazolo portion of Formula I and is a moiety of Formula A \n \n wherein:\n X, Y and Z are, independently, N or C, \n R 8 , R 9 , R 11  and R 12  are independently H or halogen (e.g., Cl or F); and \n R 10  is \n \u2003halogen (e.g., fluoro or chloro), \n \u2003C 1-6 alkyl, \n \u2003C 3-8 cycloalkyl, \n \u2003heteroC 3-8 cycloalkyl (e.g., pyrrolidinyl or piperidinyl), \n \u2003haloC 1-6 alkyl (e.g., trifluoromethyl), \n \u2003aryl (e.g., phenyl) or heteroaryl (e.g., pyridyl, (for example, pyrid-2-yl) or e.g., thiadiazolyl (for example, 1,2,3-thiadiazol-4-yl), diazolyl, triazolyl (e.g., 1,2,4-triazol-1-yl), tetrazolyl (e.g., tetrazol-5-yl), alkyloxadiazolyl (e.g., 5-methyl-1,2,4-oxadiazol), pyrazolyl (e.g., pyrazol-1-yl), \n \u2003wherein said 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), \n \u2003C 1-6 alkyl sulfonyl (e.g., methyl sulfonyl), \n \u2003arylcarbonyl (e.g., benzoyl), \n \u2003heteroarylcarbonyl, \n \u2003C 1-6 alkoxycarbonyl, (e.g., methoxycarbonyl), \n \u2003Aminocarbonyl, \n \u2003\u2014N(R 14 )(R 15 ); \n \u2003preferably R 10  is phenyl, pyridyl, piperidinyl or pyrrolidinyl optionally substituted with the substituents previously defined, e.g. optionally substituted with halo or alkyl; \n provided that when X, Y or X is nitrogen, R 8 , R 9  or R 10 , respectively, is not present; \n (v) R 4  and R 5  are independently:\n H, \n C 1-6 alkyl (e.g., methyl, isopropyl, isobutyl, n-propyl), \n C 3-8 cycloalkyl (e.g., cyclopentyl or cyclohexyl), \n C 3-8 heterocycloalkyl (e.g., pyrrolidinyl (for example pyrrolidin-3-yl or pyrrolidin-1-yl), piperidinyl (for example, piperidin-1-yl), morpholinyl), \n \u2014C 0-6 alkylaryl (e.g., phenyl or benzyl) or \n \u2014C 0-6 alkylheteroaryl (e.g., pyrid-4-yl, pyrid-2-yl or pyrazol-3-yl) \n wherein said aryl or heteroaryl is optionally substituted with one or more 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); \n (vi) R 6  is H, C 1-6 alkyl (e.g., methyl or ethyl) or C 3-8 cycloalkyl; (vii) R 14  and R 15  are independently H or C 1-6 alkyl, 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): 0.8048895550744455
- 35 USC 102 Novelty (BERT): 0.5555688952015111
- Combined Prediction Score: 0.7799574890871521
- Mean Citation Score: 348.187806
- Max Citation Score: 492.94012
- Similarity Product: 406.5429943205594

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