JP2016519659A5 - - Google Patents

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Publication number

JP2016519659A5

JP2016519659A5 JP2016502225A JP2016502225A JP2016519659A5 JP 2016519659 A5 JP2016519659 A5 JP 2016519659A5 JP 2016502225 A JP2016502225 A JP 2016502225A JP 2016502225 A JP2016502225 A JP 2016502225A JP 2016519659 A5 JP2016519659 A5 JP 2016519659A5

Authority

JP

Japan

Prior art keywords

optionally substituted

use according

independently

alkyl

compound

Prior art date

2014-03-13

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Links

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• 125000000547 substituted alkyl group Chemical group 0.000 claims 46
• 150000001875 compounds Chemical class 0.000 claims 35
• 150000001204 N-oxides Chemical class 0.000 claims 31
• 150000002148 esters Chemical class 0.000 claims 31
• 239000002207 metabolite Substances 0.000 claims 31
• 239000000651 prodrug Substances 0.000 claims 31
• 229940002612 prodrug Drugs 0.000 claims 31
• 150000003839 salts Chemical class 0.000 claims 31
• 239000012453 solvate Substances 0.000 claims 31
• 229910052739 hydrogen Inorganic materials 0.000 claims 30
• 125000001475 halogen functional group Chemical group 0.000 claims 25
• 125000005415 substituted alkoxy group Chemical group 0.000 claims 25
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 19
• 125000000217 alkyl group Chemical group 0.000 claims 12
• 125000004104 aryloxy group Chemical group 0.000 claims 11
• 206010003246 arthritis Diseases 0.000 claims 9
• 125000001072 heteroaryl group Chemical group 0.000 claims 9
• KIWSYRHAAPLJFJ-DNZSEPECSA-N n-[(e,2z)-4-ethyl-2-hydroxyimino-5-nitrohex-3-enyl]pyridine-3-carboxamide Chemical compound [O-][N+](=O)C(C)C(/CC)=C/C(=N/O)/CNC(=O)C1=CC=CN=C1 KIWSYRHAAPLJFJ-DNZSEPECSA-N 0.000 claims 9
• 125000003710 aryl alkyl group Chemical group 0.000 claims 8
• 210000001612 chondrocyte Anatomy 0.000 claims 7
• 230000004069 differentiation Effects 0.000 claims 7
• 125000001188 haloalkyl group Chemical group 0.000 claims 7
• 238000004519 manufacturing process Methods 0.000 claims 7
• 210000002901 mesenchymal stem cell Anatomy 0.000 claims 7
• -1 polymorph Substances 0.000 claims 7
• 230000006378 damage Effects 0.000 claims 6
• 210000001503 joint Anatomy 0.000 claims 6
• GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims 4
• 101150065749 Churc1 gene Proteins 0.000 claims 4
• 102100038239 Protein Churchill Human genes 0.000 claims 4
• 125000000623 heterocyclic group Chemical group 0.000 claims 4
• 239000000203 mixture Substances 0.000 claims 4
• 125000003107 substituted aryl group Chemical group 0.000 claims 4
• 238000006467 substitution reaction Methods 0.000 claims 4
• 101100294102 Caenorhabditis elegans nhr-2 gene Proteins 0.000 claims 3
• 206010060820 Joint injury Diseases 0.000 claims 3
• 238000009472 formulation Methods 0.000 claims 3
• 239000001257 hydrogen Substances 0.000 claims 3
• 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 3
• 239000008194 pharmaceutical composition Substances 0.000 claims 3
• 102100025668 Angiopoietin-related protein 3 Human genes 0.000 claims 2
• 101000693085 Homo sapiens Angiopoietin-related protein 3 Proteins 0.000 claims 2
• 241000124008 Mammalia Species 0.000 claims 2
• 125000003118 aryl group Chemical group 0.000 claims 2
• 230000001939 inductive effect Effects 0.000 claims 2
• 239000003112 inhibitor Substances 0.000 claims 2
• LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 2
• KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims 1
• 102100022544 Bone morphogenetic protein 7 Human genes 0.000 claims 1
• 102000011727 Caspases Human genes 0.000 claims 1
• 108010076667 Caspases Proteins 0.000 claims 1
• 102000008186 Collagen Human genes 0.000 claims 1
• 108010035532 Collagen Proteins 0.000 claims 1
• 102100035323 Fibroblast growth factor 18 Human genes 0.000 claims 1
• 244000068988 Glycine max Species 0.000 claims 1
• 235000010469 Glycine max Nutrition 0.000 claims 1
• 101000899361 Homo sapiens Bone morphogenetic protein 7 Proteins 0.000 claims 1
• 101000878128 Homo sapiens Fibroblast growth factor 18 Proteins 0.000 claims 1
• 102100029438 Nitric oxide synthase, inducible Human genes 0.000 claims 1
• 101710089543 Nitric oxide synthase, inducible Proteins 0.000 claims 1
• 244000025272 Persea americana Species 0.000 claims 1
• 235000008673 Persea americana Nutrition 0.000 claims 1
• 108010009736 Protein Hydrolysates Proteins 0.000 claims 1
• QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 claims 1
• 125000002877 alkyl aryl group Chemical group 0.000 claims 1
• 125000005360 alkyl sulfoxide group Chemical group 0.000 claims 1
• 125000005012 alkyl thioether group Chemical group 0.000 claims 1
• 229940035676 analgesics Drugs 0.000 claims 1
• 239000000730 antalgic agent Substances 0.000 claims 1
• 125000005362 aryl sulfone group Chemical group 0.000 claims 1
• 125000005361 aryl sulfoxide group Chemical group 0.000 claims 1
• 150000004832 aryl thioethers Chemical class 0.000 claims 1
• BBBFJLBPOGFECG-VJVYQDLKSA-N calcitonin Chemical compound N([C@H](C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(N)=O)C(C)C)C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 BBBFJLBPOGFECG-VJVYQDLKSA-N 0.000 claims 1
• 229960003773 calcitonin (salmon synthetic) Drugs 0.000 claims 1
• 230000002648 chondrogenic effect Effects 0.000 claims 1
• 229920001436 collagen Polymers 0.000 claims 1
• 125000000753 cycloalkyl group Chemical group 0.000 claims 1
• 125000005265 dialkylamine group Chemical group 0.000 claims 1
• 229920002674 hyaluronan Polymers 0.000 claims 1
• 229960003160 hyaluronic acid Drugs 0.000 claims 1
• 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
• 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 1
• 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
• 125000003373 pyrazinyl group Chemical group 0.000 claims 1
• 125000002098 pyridazinyl group Chemical group 0.000 claims 1
• 125000004076 pyridyl group Chemical group 0.000 claims 1
• 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
• 108010068072 salmon calcitonin Proteins 0.000 claims 1
• 208000024891 symptom Diseases 0.000 claims 1
• QYSXJUFSXHHAJI-YRZJJWOYSA-N vitamin D3 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-YRZJJWOYSA-N 0.000 claims 1
• 235000005282 vitamin D3 Nutrition 0.000 claims 1
• 239000011647 vitamin D3 Substances 0.000 claims 1
• 229940021056 vitamin d3 Drugs 0.000 claims 1