PATENT CLAIM ANALYSIS

Application Number: 15923285
Application Type: Utility
Filing Date: 2018-03
Publication Date: 2018-07
Patent Classification: ["514", "210210"]

Abstract:
The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds and the uses of such compounds for the treatment of D1-mediated (or D1-associated) disorders including cognitive and motivational impairments and negative symptoms associated with illnesses such as schizophrenia, depression, bipolar disorder, Parkinson's disease, Mild cognitive impairment (MCI), Alzheimer's disease, lupus, Huntington's disease, Parkinson's, dyskinesia, ADHD, post-traumatic stress disorder, autism spectrum disorder, treatment-resistant depression, major depressive disorder (MDD), drug dependence, Tourette's syndrome, tardive dyskinesias as well as impairments associated with age, chronic stress, sleep deprivation, combat, chronic fatigue; endocrine or metabolic diseases such as hyperglycemia, dislipidemia, diabetes, obesity, and sepsis; and cardiovascular disorder such as hypertension.

Claim (Index 1):
A compound of Formula I: or an N-oxide thereof, or a pharmaceutically acceptable salt of said compound or said N-oxide, wherein: X 1  is O or S; Y 1  is O, S, or NR N ; Q 1  is an N-containing 5- to 10-membered heterocycloalkyl, an N-containing 5- to 10-membered heteroaryl, or phenyl, wherein the heterocycloalkyl or heteroaryl is optionally substituted with 1, 2, 3, 4, or 5 independently selected R 7 ; and the phenyl is optionally substituted with 1, 2, 3, 4, or 5 independently selected R 7a ; R T1  and R T2  are each independently selected from the group consisting of H, C 1-3  alkyl, C 1-3  fluoroalkyl, cyclopropyl, fluorocyclopropyl, C 1-3  alkoxy, C 1-3  haloalkoxy, \u2014C(\u2550O)\u2014O\u2014(C 1-3  alkyl), and \u2014C(\u2550O)OH; R 1  is selected from the group consisting of H, F, \u2014C(\u2550O)OH, \u2014C(\u2550O)\u2014O\u2014(C 1-3  alkyl), C 1-3  alkyl, C 1-3  fluoroalkyl, C 3-6  cycloalkyl, and C 3-6  fluorocycloalkyl, wherein said C 3-6  cycloalkyl is optionally substituted with 1, 2, 3, 4, or 5 substituents each independently selected from halo, C 1-4  alkyl, C 1-4  haloalkyl, C 1-4  alkoxy, and C 1-4  haloalkoxy; R 2  is selected from the group consisting of H, halogen, \u2014CN, \u2014OH, C(\u2550O)OH, C(\u2550O)\u2014O\u2014(C 1-3  alkyl), C 1-3  alkoxy, C 1-3  haloalkoxy, \u2014N(R 8 )(R 9 ), C 1-3  alkyl, C 1-3  fluoroalkyl, C 3-6  cycloalkyl, C 3-6  fluorocycloalkyl, C 2-6  alkenyl, and C 2-6  alkynyl, wherein said C 3-6  cycloalkyl is optionally substituted with 1, 2, 3, 4, or 5 substituents each independently selected from halo, C 1-4  alkyl, C 1-4  haloalkyl, C 1-4  alkoxy, and C 1-4  haloalkoxy; R 3  and R 4  are each independently selected from the group consisting of H, C 1-6  alkyl, C 1-6  haloalkyl, C 1-6  alkoxy, C 1-6  haloalkoxy, \u2014CN, C 3-6  cycloalkyl, \u2014C(\u2550O)OH, C(\u2550O)\u2014O\u2014(C 1-4  alkyl), and halogen, wherein each of said C 1-6  alkyl and C 3-6  cycloalkyl is optionally substituted with 1, 2, 3, 4, or 5 substituents each independently selected from halo, \u2014OH, \u2014CN, C 1-4  alkyl, C 1-4  haloalkyl, C 1-4  alkoxy, and C 1-4  haloalkoxy; R 5  and R 6  are each independently selected from the group consisting of H, halogen, \u2014OH, \u2014NO 2 , \u2014CN, C 1-6  alkyl, C 1-6  haloalkyl, C 1-6  haloalkoxy, C 2-6  alkenyl, C 2-6  alkynyl, C 3-7  cycloalkyl, a 4- to 10-membered heterocycloalkyl, \u2014N(R 8 )(R 9 ), \u2014N(R 10 )(C(\u2550O)R 11 ), \u2014C(\u2550O)\u2014N(R 8 )(R 9 ), \u2014C(\u2550O)\u2014R 12 , \u2014C(\u2550O)\u2014OR 12 , and \u2014OR 13 , wherein each of said C 1-6  alkyl, C 3-7  cycloalkyl, and heterocycloalkyl is optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of halogen, \u2014CN, \u2014OH, C 1-3  alkyl, C 1-3  alkoxy, C 1-3  haloalkyl, C 1-3  haloalkoxy, C 3-6  cycloalkyl, \u2014N(R 14 )(R 15 ), \u2014N(R 16 )(C(\u2550O)R 17 ), \u2014C(\u2550O)\u2014OR 18 , \u2014C(\u2550O)H, \u2014C(\u2550O)R 18 , \u2014C(\u2550O)N(R 14 )(R 15 ), and \u2014OR 19 ; or R 5  and R 3  together with the two carbon atoms to which they are attached form a fused N-containing 5- or 6-membered heteroaryl, a fused N-containing 5- or 6-membered heterocycloalkyl, a fused 5- or 6-membered cycloalkyl, or a fused benzene ring, each optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of halo, \u2014CN, \u2014OH, C 1-3  alkyl, C 1-3  alkoxy, C 1-3  haloalkyl, and C 1-3  haloalkoxy; R 7  and R 7a  are each independently selected from the group consisting of halogen, \u2014OH, \u2014CN, \u2014NO 2 , oxo, C 1-6  alkyl, C 1-6  haloalkyl, C 1-6  hydroxylalkyl, C 1-6  alkoxy, C 1-6  haloalkoxy, C 3-7  cycloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 6-10  aryl, a 4- to 10-membered heterocycloalkyl, a 5- to 10-membered heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl, heteroarylalkyl, heteroarylalkenyl, \u2014CH\u2550N\u2014O\u2014(C 1-3  alkyl), \u2014N(R 14 )(R 15 ), \u2014N(R 16 )(C(\u2550O)R 17 ), \u2014S(\u2550O) 2 N(R 14 )(R 15 ), \u2014C(\u2550O)N(R 14 )(R 15 ), \u2014C(\u2550O)\u2014R 12 , \u2014C(\u2550O)\u2014OR 18 , and \u2014OR 19 , wherein each of said C 1-6  alkyl, C 3-7  cycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl, heteroarylalkyl, heteroarylalkenyl, C 6- aryl, heterocycloalkyl and heteroaryl is optionally substituted with 1, 2, 3, or 4 substituents each independently selected from the group consisting of halogen, OH, \u2014CN, \u2014NO 2 , C 1-4  alkyl, C 1-4  hydroxylalkyl, C 1-4  alkoxy, \u2014N(R 14 )(R 15 ), \u2014S\u2014(C 1-3  alkyl), \u2014S(\u2550O) 2 \u2014(C 1-4  alkyl), aryloxy, arylalkyloxy optionally substituted with 1 or 2 C 1-4  alkyl, oxo, \u2014C(\u2550O)H, \u2014C(\u2550O)\u2014C 1-4  alkyl, \u2014C(\u2550O)O\u2014C 1-4  alkyl, \u2014C(\u2550O)NH 2 , \u2014NHC(\u2550O)H, \u2014NHC(\u2550O)\u2014(C 1-4  alkyl), C 3-7  cycloalkyl, a 5- or 6-membered heteroaryl, C 1-4  haloalkyl, and C 1-4  haloalkoxy; or two adjacent R 7a  together with the two carbon atoms to which they are attached form a fused 5- or 6-membered cycloalkyl, a fused 5- or 6-membered heterocycloalkyl, or a fused benzene ring, each optionally substituted with 1, 2, 3, or 4 R 7b , wherein each R 7b  is independently selected from the group consisting of halo, \u2014CN, \u2014NO 2 , \u2014NH 2 , \u2014NH(C 1-4  alkyl), \u2014N(C 1-4  alkyl) 2 , azetidin-1-yl, pyrrolidin-1-yl, pyridin-1-yl, OH, oxo, C 1-4  alkyl, C 1-4  alkoxy, C 1-4  hydroxylalkyl, C 1-4  haloalkyl, and C 1-4  haloalkoxy; R 8  and R 9  are each independently selected from the group consisting of H, C 1-6  alkyl, C 1-6  haloalkyl, C 3-10  cycloalkyl, a 4- to 10-membered heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl, and heteroarylalkyl, wherein each of said C 1-6  alkyl, C 3-10  cycloalkyl, 4- to 10-membered heterocycloalkyl, cycloalkylalkyl, arylalkyl, and heteroarylalkyl is optionally substituted with 1, 2, 3, or 4 substituents each independently selected from the group consisting of \u2014OH, \u2014CN, C 1-3  alkyl, C 3-7  cycloalkyl, C 1-3  hydroxylalkyl, \u2014S\u2014C 1-3  alkyl, \u2014C(\u2550O)H, \u2014C(\u2550O)\u2014C 1-3  alkyl, \u2014C(\u2550O)\u2014O\u2014C 1-3  alkyl, \u2014C(\u2550O)\u2014NH 2 , \u2014C(\u2550O)\u2014N(C 1-3  alkyl) 2 , C 1-3  haloalkyl, C 1-3  alkoxy, and C 1-3  haloalkoxy; or R 8  and R 9  together with the N atom to which they are attached form a 4- to 10-membered heterocycloalkyl or heteroaryl optionally substituted with 1, 2, 3, or 4 substituents each independently selected from the group consisting of halogen, \u2014OH, oxo, \u2014C(\u2550O)H, \u2014C(\u2550O)OH, \u2014C(\u2550O)\u2014C 1-3  alkyl, \u2014C(\u2550O)\u2014NH 2 , \u2014C(\u2550O)\u2014N(C 1-3  alkyl) 2 , \u2014CN, C 1-3  alkyl, C 1-3  alkoxy, C 1-3  hydroxylalkyl, C 1-3  haloalkyl, and C 1-3  haloalkoxy; R 10  is selected from the group consisting of H, C 1-3  alkyl, and C 3-7  cycloalkyl; R 11  is selected from the group consisting of C 1-6  alkyl, C 3-7  cycloalkyl, a 4- to 14-membered heterocycloalkyl, C 6-10  aryl, a 5- to 10-membered heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl, and heteroarylalkyl, each optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of halogen, \u2014CF 3 , \u2014CN, \u2014OH, oxo, \u2014S\u2014C 1-3  alkyl, C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 3-7  cycloalkyl, C 1-6  alkoxy, and C 1-6  haloalkoxy; R 12  is H or is selected from the group consisting of C 1-10  alkyl, C 3-7  cycloalkyl, a 4- to 14-membered heterocycloalkyl, C 6-10  aryl, a 5- to 10-membered heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl, and heteroarylalkyl, each optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of halogen, \u2014CF 3 , \u2014CN, \u2014OH, \u2014C(\u2550O)OH, C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 3-7  cycloalkyl, C 1-6  alkoxy, and C 1-6  haloalkoxy; R 13  is selected from the group consisting of C 1-10  alkyl, C 1-6  haloalkyl, C 3-7  cycloalkyl, a 4- to 14-membered heterocycloalkyl, C 6-10  aryl, a 5- to 10-membered heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl, and heteroarylalkyl, each optionally substituted with 1, 2, 3, or 4 substituents each independently selected from the group consisting of halogen, \u2014N(R 14 )(R 15 ), \u2014C(\u2550O)N(R 14 )(R 15 ), \u2014N(R 16 )(C(\u2550O)R 17 ), \u2014C(\u2550O)H, \u2014C(\u2550O)N(R 16 )(OR 18 ), \u2014C(\u2550O)\u2014R 18 , \u2014C(\u2550O)\u2014OR 18 , \u2014O\u2014C(\u2550O)R 18 , \u2014CF 3 , \u2014CN, \u2014OH, \u2014O\u2014(C 1-6  hydroxylalkyl), C 1-6  alkyl, oxo, C 1-6  hydroxylalkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 3-7  cycloalkyl, C 1-6  alkoxy, and C 1-6  haloalkoxy; R 14  and R 15  are each independently selected from the group consisting of H, C 1-6  alkyl, C 2-6  alkenyl, C 3-10  cycloalkyl, a 4- to 14-membered heterocycloalkyl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl, and heteroarylalkyl, wherein each of said C 1-6  alkyl, C 3-7  cycloalkyl, cycloalkylalkyl, arylalkyl, and heteroarylalkyl is optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of \u2014OH, \u2014CN, oxo, \u2014NHC(\u2550O)\u2014(C 1-3  alkyl), \u2014C(\u2550O)N(C 1-3  alkyl) 2 , \u2014O\u2014(C 1-6  hydroxylalkyl), \u2014S(\u2550O) 2 \u2014C 1-3  alkyl, \u2014S\u2014C 1-3  alkyl, C 1-3  alkyl, C 3-7  cycloalkyl, C 1-3  hydroxylalkyl, a 5- to 10-membered heteroaryl, C 1-3  alkoxy, C 1-3  haloalkyl, and C 1-3  haloalkoxy; or R 14  and R 15  together with the N atom to which they are attached form a 4- to 10-membered heterocycloalkyl or 5- to 10-membered heteroaryl optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of halogen, oxo, \u2014OH, C 1-3  alkyl, C 1-3  alkoxy, C 1-3  haloalkyl, C 1-3  haloalkoxy, C 1-3  hydroxylalkyl, C 2-4  alkoxyalkyl, oxo, a 5- to 6-membered heteroaryl, \u2014NH 2 , \u2014N(C 1-3  alkyl) 2 , \u2014S(\u2550O) 2 \u2014C 1-3  alkyl, \u2014S\u2014C 1-3  alkyl, \u2014C(\u2550O)H, \u2014C(\u2550O)OH, \u2014C(\u2550O)NH 2 , and \u2014C(\u2550O)\u2014C 1-3  alkyl; R 16  is selected from the group consisting of H, C 1-3  alkyl, and C 3-7  cycloalkyl; R 17  is selected from the group consisting of C 1-6  alkyl, C 3-7  cycloalkyl, a 4- to 14-membered heterocycloalkyl, C 6-10  aryl, a 5- to 10-membered heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl, and heteroarylalkyl, each optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of halogen, \u2014CF 3 , \u2014CN, \u2014OH, C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 3-7  cycloalkyl, C 1-6  alkoxy, and C 1-6  haloalkoxy; R 18  is H or is selected from the group consisting of C 1-6  alkyl, C 3-7  cycloalkyl, a 4- to 14-membered heterocycloalkyl, C 6-10  aryl, a 5- to 10-membered heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl, and heteroarylalkyl, each optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of halogen, \u2014CF 3 , \u2014CN, \u2014OH, C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 3-7  cycloalkyl, C 1-6  alkoxy, and C 1-6  haloalkoxy; R 19  is selected from the group consisting of C 1-6  alkyl, C 1-6  haloalkyl, C 3-7  cycloalkyl, a 4- to 14-membered heterocycloalkyl, C 6-10  aryl, a 5- to 10-membered heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl, and heteroarylalkyl, each optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of halogen, \u2014N(R 14 )(R 15 ), \u2014C(\u2550O)N(R 14 )(R 15 ), \u2014N(R 16 )(C(\u2550O)R 17 ), \u2014C(\u2550O)\u2014R 18 , \u2014C(\u2550O)\u2014OR 18 , \u2014CF 3 , \u2014CN, \u2014OH, C 1-6  alkyl, C 1-6  haloalkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 3-7  cycloalkyl, C 1-6  alkoxy, and C 1-6  haloalkoxy; and R N  is selected from the group consisting of H, C 1-6  alkyl, C 3-6  cycloalkyl, C 3-6  fluorocycloalkyl, heteroarylalkyl, and arylalkyl, wherein each of said C 3-6  cycloalkyl, heteroarylalkyl, and arylalkyl is optionally substituted with 1, 2, 3, 4, or 5 substituents each independently selected from halo, C 1-4  alkyl, C 1-4  haloalkyl, C 1-4  alkoxy, and C 1-4  haloalkoxy.

Metadata:
- Claim Count in Document: 32.0
- Percentile: 90.0
- Lexical Diversity: 1.87097
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14820611', '15305384', '14819541', '15305372', '14694039']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8232451606580913
- 35 USC 102 Novelty (BERT): 0.5713070913851535
- Combined Prediction Score: 0.7980513537307975
- Mean Citation Score: 437.003564
- Max Citation Score: 460.4846
- Similarity Product: 382.63139938232905

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