PATENT CLAIM ANALYSIS

Application Number: 16220184
Application Type: Utility
Filing Date: 2018-12
Publication Date: 2019-04
Patent Classification: ["514", "253000"]

Abstract:
Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, 7-aza- and 4,7-diaza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.

Claim (Index 1):
A method of treating cardiometabolic diseases comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein\n each R 1  is independently halogen, \u2014CN, \u2014C 1-3 alkyl, or \u2014OC 1-3 alkyl, wherein the alkyl of C 1-3 alkyl and OC 1-3 alkyl is substituted with 0 to 3 F atoms; \n m is 0, 1, 2, or 3; \n each R 2  is independently F, Cl, or \u2014CN; \n p is 0, 1 or 2; \n each R 3  is independently F, \u2014OH, \u2014CN, \u2014C 1-3 alkyl, \u2014OC 1-3 alkyl, or \u2014C 3-4 cycloalkyl, or 2 R 3 s may together cyclize to form \u2014C 3-4 spirocycloalkyl, wherein the alkyl of C 1-3 alkyl and OC 1-3 alkyl, cycloalkyl, or spirocycloalkyl may be substituted as valency allows with 0 to 3 F atoms and with 0 to 1 \u2014OH; \n q is 0, 1, or 2; \n Y is CH or N; \n R 4  is \u2014C 1-3 alkyl, \u2014C 0-3 alkylene-C 3-6 cycloalkyl, \u2014C 0-3 alkylene-R 5 , or \u2014C 1-3 alkylene-R 6 , \n wherein said alkyl may be substituted as valency allows with 0 to 3 substituents independently selected from 0 to 3 F atoms and 0 to 1 substituent selected from \u2014C 0-1 alkylene-CN, \u2014C 0-1 alkylene-OR O , and \u2014N(R N ) 2 , and wherein said alkylene and cycloalkyl may be independently substituted as valency allows with 0 to 2 substituents independently selected from 0 to 2 F atoms and 0 to 1 substituent selected from \u2014C 0-1 alkylene-CN, \u2014C 0-1 alkylene-OR O , and \u2014N(R N ) 2 ;\n R 5  is a 4- to 6-membered heterocycloalkyl, wherein said heterocycloalkyl may be substituted with 0 to 2 substituents as valency allows independently selected from: \n 0 to 1 oxo (\u2550O), \n 0 to 1 \u2014CN, \n 0 to 2 F atoms, and \n 0 to 2 substituents independently selected from \u2014C 1-3 alkyl and \u2014OC 1-3 alkyl, wherein the alkyl of C 1-3 alkyl and OC 1-3 alkyl may be substituted with 0 to 3 substituents as valency allows independently selected from:\n 0 to 3 F atoms, \n 0 to 1 \u2014CN, and \n 0 to 1 \u2014OR O ; \n \n R 6  is a 5- to 6-membered heteroaryl, wherein said heteroaryl may be substituted with 0 to 2 substituents as valency allows independently selected from: \n 0 to 2 halogens, \n 0 to 1 substituent selected from \u2014OR O  and \u2014N(R N ) 2 , and \n 0 to 2 \u2014C 1-3 alkyl, wherein the alkyl may be substituted with 0 to 3 substituents as valency allows independently selected from:\n 0 to 3 F atoms, and \n 0 to 1 \u2014OR O ; \n \n each R O  is independently H, or \u2014C 1-3 alkyl, wherein C 1-3 alkyl may be substituted with 0 to 3 F atoms; \n each R N  is independently H, or \u2014C 1-3 alkyl; \n Z 1  is CH or N; \n Z 2  and Z 3  are each independently \u2014CR Z  or N, provided that when Z 1  or Z 3  is N, Z 2  is \u2014CR Z ; and \n each R Z  is independently H, F, Cl, or \u2014CH 3 ; and\n wherein the disease is T1D, T2DM, pre-diabetes, idiopathic T1D, LADA, EOD, YOAD, MODY, malnutrition-related diabetes, gestational diabetes, hyperglycemia, insulin resistance, hepatic insulin resistance, impaired glucose tolerance, diabetic neuropathy, diabetic nephropathy, kidney disease, diabetic retinopathy, adipocyte dysfunction, visceral adipose deposition, sleep apnea, obesity, eating disorders, weight gain from use of other agents, excessive sugar craving, dyslipidemia, hyperinsulinemia, NAFLD, NASH, fibrosis, cirrhosis, hepatocellular carcinoma, cardiovascular disease, atherosclerosis, coronary artery disease, peripheral vascular disease, hypertension, endothelial dysfunction, impaired vascular compliance, congestive heart failure, myocardial infarction, stroke, hemorrhagic stroke, ischemic stroke, traumatic brain injury, pulmonary hypertension, restenosis after angioplasty, intermittent claudication, post-prandial lipemia, metabolic acidosis, ketosis, arthritis, osteoporosis, Parkinson's Disease, left ventricular hypertrophy, peripheral arterial disease, macular degeneration, cataract, glomerulosclerosis, chronic renal failure, metabolic syndrome, syndrome X, premenstrual syndrome, angina pectoris, thrombosis, atherosclerosis, transient ischemic attacks, vascular restenosis, impaired glucose metabolism, conditions of impaired fasting plasma glucose, hyperuricemia, gout, erectile dysfunction, skin and connective tissue disorders, psoriasis, foot ulcerations, ulcerative colitis, hyper apo B lipoproteinemia, Alzheimer's Disease, schizophrenia, impaired cognition, inflammatory bowel disease, short bowel syndrome, Crohn's disease, colitis, irritable bowel syndrome, treatment of Polycystic Ovary Syndrome and treatment of addiction.

Metadata:
- Claim Count in Document: 15.0
- Percentile: 98.0
- Lexical Diversity: 1.26667
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15839901', '11801841', '15381295', '15328908', '14418147']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7545186077304195
- 35 USC 102 Novelty (BERT): 0.579046615419668
- Combined Prediction Score: 0.7369714084993444
- Mean Citation Score: 361.559926
- Max Citation Score: 478.28885
- Similarity Product: 394.2299755174458

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