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 5):
A method of  claim 1 , wherein the PDE1 inhibitor is compound of Formula IV: wherein\n (i) Q is C(\u2550S), C(\u2550N(R 20 )) or CH 2 ; \n (ii) L is a single bond, \u2014N(H)\u2014, \u2014CH 2 \u2014; \n (iii) R 1  is H or C 1-4  alkyl (e.g., methyl or ethyl); \n (iv) R 4  is H or C 1-6  alkyl (e.g., methyl, isopropyl) and R 2  and R 3  are, independently, H or C 1-6 alkyl (e.g., methyl or isopropyl) optionally substituted with halo or hydroxy (e.g., R 2  and R 3  are both methyl, or R 2  is H and R 3  is methyl, ethyl, isopropyl or hydroxyethyl), aryl, heteroaryl, (optionally hetero)arylalkoxy, or (optionally hetero)arylC 1-6 alkyl;\n or \n R 2  is H and R 3  and R 4  together form a di-, tri- or tetramethylene bridge (pref. wherein the R 3  and R 4  together have the cis configuration, e.g., where the carbons carrying R 3  and R 4  have the R and S configurations, respectively); \n \n (v) R 5  is\n d) -D-E-F, wherein:\n D is C 1-4 alkylene (e.g., methylene, ethylene or prop-2-yn-1-ylene); \n E is a single bond, C 2-4 alkynylene (e.g., \u2014C\u2261C\u2014), arylene (e.g., phenylene) or heteroarylene (e.g., pyridylene); \n F is H, aryl (e.g., phenyl), heteroaryl (e.g., pyridyl, diazolyl, triazolyl, for example, pyrid-2-yl, imidazol-1-yl, 1,2,4-triazol-1-yl), halo (e.g., F, Br, Cl), haloC 1-4 alkyl (e.g., trifluoromethyl), \u2014C(O)\u2014R 15 , \u2014N(R 16 )(R 17 ), \u2014S(O) 2 R 21  or C 3-7 cycloalkyl optionally containing at least one atom selected from a group consisting of N or O (e.g., cyclopentyl, cyclohexyl, pyrrolidinyl (e.g., pyrrolidin-3-yl), tetrahydro-2H-pyran-4-yl, or morpholinyl); \n wherein D, E and F are independently and optionally substituted with one or more:\n halo (e.g., F, Cl or Br), \n C 1-4 alkyl (e.g., methyl), \n \n haloC 1-4 alkyl (e.g., trifluoromethyl), \n for example, F is heteroaryl, e.g., pyridyl substituted with one or more halo (e.g., 6-fluoropyrid-2-yl, 5-fluoropyrid-2-yl, 6-fluoropyrid-2-yl, 3-fluoropyrid-2-yl, 4-fluoropyrid-2-yl, 4,6-dichloropyrid-2-yl), haloC 1-4 alkyl (e.g., 5-trifluoromethylpyrid-2-yl) or C 1-4 alkyl (e.g., 5-methylpyrid-2-yl), \n or F is aryl, e.g., phenyl, substituted with one or more halo (e.g., 4-fluorophenyl) \n or F is a C 3-7 heterocycloalkyl (e.g., pyrrolidinyl) optionally substituted with a C 1-6 alkyl (e.g., 1-methylpyrrolidin-3-yl); \n or \n \n e) a substituted heteroarylalkyl, e.g., substituted with haloalkyl; \n f) attached to one of the nitrogens on the pyrazolo portion of Formula IV and is a moiety of Formula A \n \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:\n halogen, \n C 1-4 alkyl, \n C 3-7 cycloalkyl, \n C 1-4 haloalkyl (e.g., trifluoromethyl), \n aryl (e.g., phenyl), \n heteroaryl (e.g., pyridyl (for example pyrid-2-yl), or \n thiadiazolyl (e.g., 1,2,3-thiadiazol-4-yl)), diazolyl, triazolyl, tetrazolyl, \n arylcarbonyl (e.g., benzoyl), \n alkylsulfonyl (e.g., methylsulfonyl), \n heteroarylcarbonyl, or \n alkoxycarbonyl; \n provided that when X, Y, or Z is nitrogen, R 8 , R 9 , or R 10 , respectively, is not present; (vi) R 6  is\n H, \n C 1-4 alkyl, \n C 3-7 cycloalkyl (e.g., cyclopentyl), \n aryl (e.g., phenyl), \n heteroaryl (e.g., pyridyl, for example, pyrid-4-yl), \n arylC 1-4 alkyl (e.g., benzyl), \n arylamino (e.g., phenylamino), \n heteroarylamino, \n N,N-diC 1-4 alkylamino, \n N,N-diarylamino, \n N-aryl-N-(arylC 1-4 alkyl)amino (e.g., N-phenyl-N-(1,1\u2032-biphen-4-ylmethyl)amino), or \n \u2014N(R 18 )(R 19 ); \n wherein the aryl or heteroaryl is optionally substituted with one or more halo (e.g., F, Cl), hydroxy or C 1-6 alkoxy, for example, R 6  is 4-hydroxyphenyl or 4-fluorophenyl, \n (vii) n=0 or 1; (viii) when n=1, A is \u2014C(R 13 R 14 )\u2014, wherein R 13  and R 14 , are, independently, H or C 1-4 alkyl, aryl, heteroaryl, (optionally hetero)arylC 1-4 alkoxy or (optionally hetero)arylC 1-4 alkyl; (ix) R 15  is C 1-4 alkyl, haloC 1-4 alkyl, \u2014OH or \u2014OC 1-4 alkyl (e.g., \u2014OCH 3 ) (x) R 16  and R 17  are independently H or C 1-4 alkyl; (xi) R 18  and R 19  are independently H, C 1-4 alky or aryl (e.g., phenyl) wherein said aryl is optionally substituted with one or more halo (e.g., fluorophenyl, e.g., 4-fluorophenyl) or hydroxy (e.g., hydroxyphenyl, e.g., 4-hydroxyphenyl or 2-hydroxyphenyl) (xii) R 20  is H, C 1-4 alkyl (e.g., methyl) or C 3-7 cycloalkyl, (xiii) R 21  is 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): 0.8079904743519867
- 35 USC 102 Novelty (BERT): 0.5441089360622329
- Combined Prediction Score: 0.7816023205230114
- Mean Citation Score: 348.187806
- Max Citation Score: 492.94012
- Similarity Product: 345.857990026064

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