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 2):
A method of  claim 1 , wherein the PDE1 inhibitor is compound of Formula II: wherein\n (i) Q is C(\u2550O), C(\u2550S), C(\u2550N(R 20 )) or CH 2 ; \n (ii) L is a single bond, \u2014N(H)\u2014, \u2014CH 2 \u2014, \u2014S\u2014, \u2014S(O)\u2014 or \u2014S(O 2 )\u2014; \n (iii) R 1  is H or C 1-4  alkyl (e.g., methyl); \n (iv) R 4  is H or C 1-6  alkyl (e.g., methyl or isopropyl) and R 2  and R 3  are, independently,\n H \n C 1-6 alkyl (e.g., methyl, 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), \n aryl, \n heteroaryl, \n (optionally hetero)arylalkoxy, \n (optionally hetero)arylC 1-6 alkyl; or \n R 2  and R 3  together form a 3- to 6-membered ring; \n \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 or \n (v) R 5  is\n g) -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\n H, \n aryl (e.g., phenyl), \n heteroaryl (e.g., pyridyl, diazolyl, triazolyl, for example, pyrid-2-yl, imidazol-1-yl, 1,2,4-triazol-1-yl), \n halo (e.g., F, Br, Cl), \n haloC 1-4 alkyl (e.g., trifluoromethyl), \n \u2014C(O)\u2014R 15 , \n \u2014N(R 16 )(R 17 ), or \n 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 \n wherein D, E and F are independently and optionally substituted with one or more halo (e.g., F, Cl or Br), C 1-4 alkyl (e.g., methyl), haloC 1-4 alkyl (e.g., trifluoromethyl), C 1-4 alkoxy (e.g., methoxy), hydroxy, C 1-4 carboxy, or an additional aryl or heteroaryl (e.g., biphenyl or pyridylphenyl), \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), or F is aryl, e.g., phenyl, substituted with one or more halo (e.g., 4-fluorophenyl) 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); or \n \n h) a substituted heteroarylalkyl, e.g., substituted with haloC 1-4 alkyl; \n i) attached to the nitrogen on the pyrrolo portion of Formula II-A or II-B 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 haloC 1-4 alkyl (e.g., trifluoromethyl) \n C 1-4 alkoxy (e.g. methoxy), \n C 3-7 cycloalkyl, \n heteroC 3-7 cycloalkyl (e.g., pyrrolidinyl or piperidinyl), \n C 1-4 haloalkyl (e.g., trifluoromethyl), \n aryl (e.g., phenyl), \n heteroaryl (e.g., pyridyl (for example pyrid-2-yl or pyrid-4-yl), or thiadiazolyl (e.g., 1,2,3-thiadiazol-4-yl)), diazolyl (e.g., imidazol-1-yl), triazolyl (e.g., 1,2,4-triazol-1-yl), tetrazolyl, \n arylcarbonyl (e.g., benzoyl), \n alkylsulfonyl (e.g., methylsulfonyl), \n heteroarylcarbonyl, or \n alkoxycarbonyl; \n wherein the aryl, heteroaryl, cycloalkyl or heterocycloalkyl is independently, optionally substituted with one or more C 1-4 alkyl (e.g., methyl), halogen (e.g., chloro or fluoro), haloC 1-4 alkyl (e.g., trifluoromethyl), hydroxy, C 1-4 carboxy, \u2014SH or an additional aryl, heteroaryl (e.g., biphenyl or pyridylphenyl) or C 3-8 cycloalkyl, preferably R 10  is phenyl, pyridyl, piperidinyl or pyrrolidinyl optionally substituted with the substituents previously defined, e.g. optionally substituted with halo or alkyl 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 (e.g., methyl, ethyl, n-propyl, isobutyl), \n C 3-7 cycloalkyl (e.g., cyclopentyl or cyclohexyl), \n heteroC 3-7 cycloalkyl (e.g., pyrrolidinyl, piperidinyl, morpholinyl), \n aryl (e.g., phenyl), \n heteroaryl (e.g., 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 and heteroaryl are optionally substituted with one or more C 1-4 alkyl (e.g., methyl), halogen (e.g., chloro or fluoro), haloC 1-4 alkyl (e.g., trifluoromethyl), hydroxy, C 1-4 carboxy, or an additional aryl, heteroaryl (e.g., biphenyl or pyridylphenyl) or C 3-8 cycloalkyl; \n (vii) R 7  is H, C 1-6 alkyl (e.g., methyl or ethyl), halogen (e.g., Cl), \u2014N(R 18 )(R 19 ), hydroxy or C 1-6 alkoxy; (viii) n=0 or 1; (ix) 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, (optionally hetero)arylC 1-4 alkyl or R 14  can form a bridge with R 2  or R 4 ; (x) R 15  is C 1-4 alkyl, haloC 1-4 alkyl, \u2014OH or \u2014OC 1-4 alkyl (e.g., \u2014OCH 3 ) (xi) R 16  and R 17  are independently H or C 1-4 alkyl; (xii) R 18  and R 19  are independently\n H, \n C 1-4 alky (e.g., methyl, ethyl, n-propyl, isobutyl), \n C 3-8 cycloalky (e.g., cyclohexyl or cyclopenyl), \n heteroC 3-8 cycloalky (e.g., pyrrolidinyl, piperidinyl, morpholinyl), \n aryl (e.g., phenyl) or \n heteroaryl (e.g., pyridyl), \n wherein said aryl and heteroaryl are optionally substituted with one or more\n halo (e.g., fluorophenyl, e.g., 4-fluorophenyl), \n hydroxy (e.g., hydroxyphenyl, e.g., 4-hydroxyphenyl or 2-hydroxyphenyl), \n C 1-4 alkyl (e.g., methyl), \n haloC 1-4 alkyl (e.g., trifluoromethyl), \n C 1-4 carboxy, or \n an additional aryl, heteroaryl (e.g., biphenyl or pyridylphenyl) or C 3-8 cycloalkyl, \n \n (xiii) R 20  is H, C 1-4 alkyl or C 3-7 cycloalkyl; 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): 0.8068594588701794
- 35 USC 102 Novelty (BERT): 0.5483110023059281
- Combined Prediction Score: 0.7810046132137543
- Mean Citation Score: 348.187806
- Max Citation Score: 492.94012
- Similarity Product: 368.0775300396776

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