Some of the successful targets explored for the new investigational agents described in the U.S. patents approved in 2000 through 2004
| Therapeutic Target | No. of U.S. Patents | Targeted Diseases | |
|---|---|---|---|
| Protein | Subgroup | ||
| Adrenergic receptors (63) | α-Adrenergic receptor | 1 | Nasal congestion, glaucoma, asthma, migraine, diarrhea |
| α1-Adrenergic receptor | 4 | Congestive heart failure, hypertension, benign prostatic hyperplasia, eye disorders | |
| α1D-Adrenergic receptor | 5 | Benign prostatic hyperplasia, peripheral vascular disease, congestive heart failure, hypertension | |
| α1B-Adrenergic receptor | 3 | CNS disorders, anxiety, sleep disorders, schizophrenia, hypertension, sexual dysfunction | |
| α2-Adrenergic receptor | 8 | Nasal congestion, glaucoma, asthma, migraine, diarrhea | |
| α2C-Adrenergic receptor | 1 | Mental illnesses | |
| β-Adrenergic receptor | 6 | Airway inflammatory disorders, asthma, obstructive lung disease, ocular hypertension, glaucoma | |
| β2-Adrenergic receptor | 5 | Pulmonary disorders, asthma, chronic bronchitis, emphysema, neurological disorders, cardiac disorders | |
| β3-adrenergic receptor | 30 | Metabolic disorders, atherosclerosis, gastrointestinal disorders, type 2 diabetes | |
| HIV protease (58) | Retroviral infection, viral infections (HIV),viral infections (EHV) | ||
| Serotonin receptors (43) | 5-HT receptor | 1 | Headaches |
| 5-HT 1 receptor | 7 | Depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain | |
| 5-HT 1A receptor | 4 | Mood disorders, pain, neuronal disorders | |
| 5-HT 1B receptor | 4 | Migraine, depression, psychological disorders | |
| 5-HT 1D receptor | 6 | Depression, psychological disorders | |
| 5-HT 1F receptor | 2 | Headaches | |
| 5-HT 2 receptor | 3 | Cardiovascular disorders, CNS disorders, gastrointestinal disorders, glaucoma | |
| 5-HT 2A receptor | 5 | Psychotic disorders, schizophrenia, sleep-disordered breathing, sleep apnea syndrome | |
| 5-HT 2B receptor | 2 | Irritable bowel syndrome | |
| 5-HT 2C receptor | 6 | Obesity, obsessive-compulsive disorder, depression | |
| 5-HT 3 receptor | 8 | Gastrointestinal motility disorders, headache, anxiety, depression, psychosis, rheumatoid disease | |
| 5-HT 6 receptor | 2 | Hyperactivity disorders, attention deficit hyperactivity disorder | |
| 5-HT 7 receptor | 4 | CNS disorders, aforementioned disorders, disorders of the bladder, urinary retention | |
| Factor Xa (47) | Thrombotic disorders, coronary artery, cerebrovascular disease, inflammatory diseases, cancers | ||
| Substance P receptor (39) | Asthma, cough, bronchospasm, depression, emesis, inflammatory diseases, gastrointestinal disorders | ||
| Tyrosine kinases (39) | Tyrosine-protein kinase | 28 | Cancers, atherosclerosis, restenosis, endometriosis, psoriasis |
| Tyrosine-protein kinase Src | 5 | Immune diseases, cancers, atheroscelerosis, graft rejection, rheumatoid arthritis | |
| Tyrosine-protein kinase JAK3 | 3 | Allergic disorders | |
| Tyrosine-protein kinase SYK | 1 | Inflammatory diseases, obstructive airways disease | |
| Tyrosine-protein kinase BTK | 2 | Cancers, immune diseases | |
| Cyclooxygenase 2 (38) | Alzheimer's disease, osteoporosis, glaucoma, inflammation, asthma, cancers, heart diseases | ||
| Thrombin (36) | Blood coagulation, cardiovascular disorders, thrombosis, ischemia, stroke, restenosis, inflammation | ||
| NMDA receptor (27) | NMDA receptor | 14 | CNS disorders, inflammatory diseases, allergic diseases, depression, drug abuse |
| NMDA receptor NR2B | 13 | Pain, migraine, depression, anxiety, schizophrenia, Parkinson's disease, stroke | |
| Opioid receptors (25) | Opioid receptor | 4 | Eating disorders, narcotic dependence, alcoholism, pain, drug dependence |
| μ-Type opioid receptor | 2 | Constipation, vomiting and/or nausea, pain, anxiety | |
| δ-Type opioid receptor | 3 | CNS disorders, peripheral nervous system diseases, pain | |
| κ-Type opioid receptor | 16 | Depression, headaches, inflammation, arthritis, stroke, functional bowel disease, abdominal pain, pruritus | |
| Inducible NOS (24) | CNS disorders, inflammation, shock, immune disorders, disorders of gastrointestinal motility | ||
| Muscarinic receptors (22) | Muscarinic receptor | 10 | Cognitive disorders, Alzheimer's disease, neurologic, psychiatric disorders, pain |
| M1 receptor | 3 | Cognitive disorders, Alzheimer's disease, glaucoma | |
| M2 receptor | 8 | Cognitive disorders, Alzheimer's disease, smooth muscle disorders | |
| M3 receptor | 5 | Smooth muscle disorders | |
| M4 receptor | 4 | Mental disorders, Parkinson's disease, glaucoma | |
| Adenosine receptors (22) | Adenosine receptor | 1 | Cardiac and circulatory disorders, CNS disorders, respiratory disorders |
| Adenosine A1 receptor | 6 | Allergic disorders, CNS disorders, asthma | |
| Adenosine A2a receptor | 10 | CNS disorders, Parkinson's disease | |
| Adenosine A2b receptor | 3 | Airway diseases, asthma, inflammation, diabetes mellitus | |
| Adenosine A3 receptor | 6 | Bronchus disorders, inflammation, allergosis | |
| HIV reverse transcriptase (20) | Viral infections (HIV) | ||
| PDE5 (19) | Cardiovascular and cerebrovascular disorders, disorders of urogenital system, erectile dysfunction | ||
| Histamine receptors (16) | Histamine H1 receptor | 8 | Allergy, rhinitis, congestion, inflammation, CNS diseases, respiratory disorders, viral infections |
| Histamine H2 receptor | 6 | Dry eye, duodenal ulcer, gastroesophogeal reflux disease, gastrointestinal disorders | |
| Histamine H3 receptor | 5 | Allergy, congestion, inflammation, CNS-related diseases | |
| Tumor necrosis factor (16) | Inflammatory diseases, allergic diseases, cytokine-induced toxicity, muscular disorders | ||
| Serotonin reuptake (16) | CNS-related diseases, anxiety | ||
| Gonadotropin-releasing hormone receptor (16) | Sex-hormone-related disorders, steroid-dependent tumors, prostate cancer | ||
| Endothelin receptors (15) | Endothelin receptor | 11 | Angina, pulmonary hypertension, Raynaud's disease, migraine, blood vessel disorders, renal diseases |
| Endothelin A receptor | 4 | Hypertension, acute myocardial infarction, Raynaud's syndrome, atherosclerosis, asthma, prostate cancer | |
| Endothelin B receptor | 2 | Hypertension, acute myocardial infarction, stroke, benign prostate hypertrophy, atherosclerosis, asthma | |
| HMG-CoA reductase (13) | Atherosclerosis, lipid disorders, hypercholesterolemia, hypertriglyceridemia, combined hyperlipidemia | ||
| Gastric H+/K+-ATPase (12) | Bacterial infections, gastric acid-related diseases, nasal disorders, bronchus disorders, osteoporosis | ||
| U-plasminogen activator (12) | Angiogenic disorders, arthritis, inflammation, osteoporotic, cancers, lymphomas, chronic dermal ulcers | ||
| LHRH receptor (12) | Hormone-dependent tumors, hormone-influenced disorders, benign prostate hyperplasia, endometriosis | ||
| LHRH (12) | Hormone-dependent tumors, hormone-influenced disorders, benign prostate hyperplasia, endometriosis | ||
| RARs (11) | Retinoic acid receptor | 5 | Acne, psoriasis, rheumatoid arthritis, viral infections |
| RAR-α | 1 | Systemic erythematosus, glomerulonephritis, lupus nephritis, autoimmune anemia | |
| RAR-γ | 5 | Emphysema and associated pulmonary diseases, dermatological disorders, epithelial lesions, tumors | |
| PPARs (10) | PPAR-α | 4 | Abnormality of lipid metabolism, type 2 diabetes |
| PPAR-γ | 5 | Diabetes, obesity, metabolic syndrome, cardiovascular diseases, dyslipidemia, cancers | |
| PPAR-δ | 2 | Dyslipidemia, syndrome X, cardiovascular diseases, diabetes, obesity, anorexia bulimia | |
| Glycogen synthase kinase-3 (9) | Cancers, diabetes, Alzheimer's disease | ||
| Prostanoid FP receptor (9) | Bone disorders, glaucoma, ocular hypertension | ||
| Calcium channel (9) | Cardiovascular disorders, angina, hypertension, ischemia | ||
| 5-Lipoxygenase (8) | Asthma, atherosclerosis, cancers | ||
| Glycoprotein IIb/IIIa receptor (8) | Cancers, osteoporosis, arteriosclerosis, restenosis, ophthalmia | ||
| DNA topoisomerases (7) | DNA topoisomerase I | 3 | Cancers |
| DNA topoisomerase II | 6 | Bacterial infections, cancers | |
| Angiotensin-converting enzyme (7) | Diabetic complications, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy | ||
| Glucocorticoid receptor (7) | Cocaine addiction, depression, Alzheimer's disease, aforementioned diseases, Diabetes | ||
| Serine protease (7) | Cardiovascular disorders, thrombosis, asthma | ||
| Angiotensin II receptor (7) | AT1 | 6 | Acute myocardial infarction, cancers, hypertension, QT dispersion |
| AT2 | 6 | Acute myocardial infarction, cancers, hypertension, QT dispersion, wounds healing | |
| Estrogen receptors (6) | Estrogen receptor | 2 | Breast cancer, inflammatory diseases, sepsis, viral infections, cardiovascular diseases |
| Estrogen receptor a | 4 | Uterine cancer, adjuvant breast cancer, prostate cancer, benign prostatic hyperplasia, ovarian cancers | |
| Tryptase (6) | Cardiovascular disorders, inflammatory diseases, cancers | ||
| Dopamine receptors (5) | Dopamine receptor | 2 | Cancers, Parkinson's disease |
| D2 dopamine receptor | 2 | Fibromyalgia, musculoskeletal pain symptoms associated with fibromyalgia | |
| D3 dopamine receptor | 2 | Fibromyalgia, musculoskeletal pain symptoms associated with fibromyalgia | |
| D4 dopamine receptor | 1 | Central nervous system disorders, psychotic disorders, schizophrenia | |
| Interleukin-1 receptor (5) | IL-1R | 4 | Hypotension, tachycardia, lung edema, renal failure |
| IL-1R-a | 1 | Allergic rhinitis, allergic asthma, allergic Inflammatory diseases | |
| Neuraminidase (5) | Influenza A, influenza B, viral infections, bacterial infections | ||
| Histone deacetylase (5) | Cancers, hematological disorders, metabolic disorders, cystic fibrosis, adrenoleukodystrophy | ||
CNS, central nervous system; NOS, nitric-oxide synthase; LHRH, luteinizing hormone-releasing hormone; RAR, retinoic acid receptor; PPAR; peroxisome proliferator-activated receptor; IL-1R, interleukin-1 receptor