CN101801957A - 吡啶酮gpr119g蛋白偶联受体激动剂 - Google Patents
吡啶酮gpr119g蛋白偶联受体激动剂 Download PDFInfo
- Publication number
- CN101801957A CN101801957A CN200880108168A CN200880108168A CN101801957A CN 101801957 A CN101801957 A CN 101801957A CN 200880108168 A CN200880108168 A CN 200880108168A CN 200880108168 A CN200880108168 A CN 200880108168A CN 101801957 A CN101801957 A CN 101801957A
- Authority
- CN
- China
- Prior art keywords
- alkyl
- heterocyclic radical
- cycloalkyl
- aryl
- thiazolinyl
- Prior art date
- 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.)
- Pending
Links
- 229940080349 GPR agonist Drugs 0.000 title description 2
- LVWZTYCIRDMTEY-UHFFFAOYSA-N metamizole Chemical compound O=C1C(N(CS(O)(=O)=O)C)=C(C)N(C)N1C1=CC=CC=C1 LVWZTYCIRDMTEY-UHFFFAOYSA-N 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 94
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 23
- 201000010099 disease Diseases 0.000 claims abstract description 18
- 102000004169 proteins and genes Human genes 0.000 claims abstract description 10
- 108090000623 proteins and genes Proteins 0.000 claims abstract description 10
- 238000002560 therapeutic procedure Methods 0.000 claims abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 948
- 125000003118 aryl group Chemical group 0.000 claims description 909
- 125000000217 alkyl group Chemical group 0.000 claims description 807
- 125000002769 thiazolinyl group Chemical group 0.000 claims description 556
- 125000000304 alkynyl group Chemical group 0.000 claims description 522
- 125000001072 heteroaryl group Chemical group 0.000 claims description 516
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 412
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 378
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 326
- 229910052736 halogen Inorganic materials 0.000 claims description 326
- 150000002367 halogens Chemical class 0.000 claims description 326
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 280
- 125000001188 haloalkyl group Chemical group 0.000 claims description 279
- 229910052739 hydrogen Inorganic materials 0.000 claims description 260
- 239000001257 hydrogen Substances 0.000 claims description 260
- 150000002431 hydrogen Chemical class 0.000 claims description 240
- 125000003545 alkoxy group Chemical group 0.000 claims description 70
- 229910052717 sulfur Inorganic materials 0.000 claims description 64
- 206010012601 diabetes mellitus Diseases 0.000 claims description 32
- 229910052799 carbon Inorganic materials 0.000 claims description 23
- 229910052757 nitrogen Inorganic materials 0.000 claims description 23
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 20
- 239000008103 glucose Substances 0.000 claims description 20
- 108090001061 Insulin Proteins 0.000 claims description 17
- 239000003814 drug Substances 0.000 claims description 15
- 208000008589 Obesity Diseases 0.000 claims description 14
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims description 14
- 235000020824 obesity Nutrition 0.000 claims description 13
- 239000008194 pharmaceutical composition Substances 0.000 claims description 9
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 8
- 208000011580 syndromic disease Diseases 0.000 claims description 8
- 229940125396 insulin Drugs 0.000 claims description 7
- 238000000034 method Methods 0.000 claims description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
- 201000001421 hyperglycemia Diseases 0.000 claims description 6
- 150000002632 lipids Chemical class 0.000 claims description 5
- 230000004060 metabolic process Effects 0.000 claims description 5
- 230000001105 regulatory effect Effects 0.000 claims description 5
- 150000003839 salts Chemical class 0.000 claims description 5
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 claims description 4
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims description 4
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims description 4
- 206010020772 Hypertension Diseases 0.000 claims description 4
- 208000006011 Stroke Diseases 0.000 claims description 4
- 238000011161 development Methods 0.000 claims description 4
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims description 4
- 201000008980 hyperinsulinism Diseases 0.000 claims description 4
- 201000001320 Atherosclerosis Diseases 0.000 claims description 3
- 206010008190 Cerebrovascular accident Diseases 0.000 claims description 3
- 206010019280 Heart failures Diseases 0.000 claims description 3
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 206010033645 Pancreatitis Diseases 0.000 claims description 3
- 208000017442 Retinal disease Diseases 0.000 claims description 3
- 206010038923 Retinopathy Diseases 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- 208000010877 cognitive disease Diseases 0.000 claims description 3
- 208000035475 disorder Diseases 0.000 claims description 3
- 208000006575 hypertriglyceridemia Diseases 0.000 claims description 3
- 208000028867 ischemia Diseases 0.000 claims description 3
- 201000001119 neuropathy Diseases 0.000 claims description 3
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 3
- 230000002265 prevention Effects 0.000 claims description 3
- 208000037803 restenosis Diseases 0.000 claims description 3
- 239000012453 solvate Substances 0.000 claims description 3
- 230000002792 vascular Effects 0.000 claims description 3
- 208000020084 Bone disease Diseases 0.000 claims description 2
- 206010012289 Dementia Diseases 0.000 claims description 2
- 208000010412 Glaucoma Diseases 0.000 claims description 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims description 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims description 2
- 206010049287 Lipodystrophy acquired Diseases 0.000 claims description 2
- 108091005804 Peptidases Proteins 0.000 claims description 2
- 239000004365 Protease Substances 0.000 claims description 2
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 230000006999 cognitive decline Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 201000005577 familial hyperlipidemia Diseases 0.000 claims description 2
- 230000004217 heart function Effects 0.000 claims description 2
- 239000003112 inhibitor Substances 0.000 claims description 2
- 208000006132 lipodystrophy Diseases 0.000 claims description 2
- 208000031225 myocardial ischemia Diseases 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 230000007823 neuropathy Effects 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 230000029663 wound healing Effects 0.000 claims description 2
- 102100023915 Insulin Human genes 0.000 claims 1
- 208000005764 Peripheral Arterial Disease Diseases 0.000 claims 1
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 1
- 230000000879 anti-atherosclerotic effect Effects 0.000 claims 1
- 229940127003 anti-diabetic drug Drugs 0.000 claims 1
- 230000000326 anti-hypercholesterolaemic effect Effects 0.000 claims 1
- 230000003579 anti-obesity Effects 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 239000002220 antihypertensive agent Substances 0.000 claims 1
- 229940127088 antihypertensive drug Drugs 0.000 claims 1
- 239000003524 antilipemic agent Substances 0.000 claims 1
- 239000002830 appetite depressant Substances 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 230000003750 conditioning effect Effects 0.000 abstract 4
- -1 heterocyclic radical Chemical class 0.000 description 565
- 229920000728 polyester Polymers 0.000 description 208
- 102000004877 Insulin Human genes 0.000 description 16
- 210000000227 basophil cell of anterior lobe of hypophysis Anatomy 0.000 description 15
- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 description 12
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 description 12
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 description 11
- 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 0.000 description 11
- 230000003914 insulin secretion Effects 0.000 description 10
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 9
- 210000004027 cell Anatomy 0.000 description 8
- 210000002381 plasma Anatomy 0.000 description 7
- RYCNUMLMNKHWPZ-SNVBAGLBSA-N 1-acetyl-sn-glycero-3-phosphocholine Chemical compound CC(=O)OC[C@@H](O)COP([O-])(=O)OCC[N+](C)(C)C RYCNUMLMNKHWPZ-SNVBAGLBSA-N 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 102000005962 receptors Human genes 0.000 description 5
- 108020003175 receptors Proteins 0.000 description 5
- 230000006907 apoptotic process Effects 0.000 description 4
- 210000004369 blood Anatomy 0.000 description 4
- 239000008280 blood Substances 0.000 description 4
- 230000037396 body weight Effects 0.000 description 4
- 208000029078 coronary artery disease Diseases 0.000 description 4
- 230000008878 coupling Effects 0.000 description 4
- 238000010168 coupling process Methods 0.000 description 4
- 238000005859 coupling reaction Methods 0.000 description 4
- 230000001419 dependent effect Effects 0.000 description 4
- 208000024172 Cardiovascular disease Diseases 0.000 description 3
- 230000018109 developmental process Effects 0.000 description 3
- 230000002641 glycemic effect Effects 0.000 description 3
- 229940088597 hormone Drugs 0.000 description 3
- 239000005556 hormone Substances 0.000 description 3
- 210000003734 kidney Anatomy 0.000 description 3
- 230000004044 response Effects 0.000 description 3
- 230000000630 rising effect Effects 0.000 description 3
- 206010052895 Coronary artery insufficiency Diseases 0.000 description 2
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 description 2
- 102400000322 Glucagon-like peptide 1 Human genes 0.000 description 2
- 101800000224 Glucagon-like peptide 1 Proteins 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 101100069093 Mus musculus Gpr119 gene Proteins 0.000 description 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 description 2
- 239000012190 activator Substances 0.000 description 2
- 230000003915 cell function Effects 0.000 description 2
- 230000008859 change Effects 0.000 description 2
- 230000002526 effect on cardiovascular system Effects 0.000 description 2
- 235000013305 food Nutrition 0.000 description 2
- 230000037406 food intake Effects 0.000 description 2
- 230000006377 glucose transport Effects 0.000 description 2
- 210000000496 pancreas Anatomy 0.000 description 2
- 210000001525 retina Anatomy 0.000 description 2
- 150000003384 small molecules Chemical class 0.000 description 2
- 238000005728 strengthening Methods 0.000 description 2
- 231100000419 toxicity Toxicity 0.000 description 2
- 230000001988 toxicity Effects 0.000 description 2
- SYOKIDBDQMKNDQ-XWTIBIIYSA-N vildagliptin Chemical compound C1C(O)(C2)CC(C3)CC1CC32NCC(=O)N1CCC[C@H]1C#N SYOKIDBDQMKNDQ-XWTIBIIYSA-N 0.000 description 2
- 229960001254 vildagliptin Drugs 0.000 description 2
- 210000002237 B-cell of pancreatic islet Anatomy 0.000 description 1
- 102100039705 Beta-2 adrenergic receptor Human genes 0.000 description 1
- 208000002177 Cataract Diseases 0.000 description 1
- 208000028698 Cognitive impairment Diseases 0.000 description 1
- 102100025892 Complement C1q tumor necrosis factor-related protein 1 Human genes 0.000 description 1
- 208000002249 Diabetes Complications Diseases 0.000 description 1
- 206010012655 Diabetic complications Diseases 0.000 description 1
- 208000032928 Dyslipidaemia Diseases 0.000 description 1
- 108091006027 G proteins Proteins 0.000 description 1
- 102000030782 GTP binding Human genes 0.000 description 1
- 108091000058 GTP-Binding Proteins 0.000 description 1
- 108010004460 Gastric Inhibitory Polypeptide Proteins 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 101000611338 Homo sapiens Rhodopsin Proteins 0.000 description 1
- 208000009164 Islet Cell Adenoma Diseases 0.000 description 1
- 208000017170 Lipid metabolism disease Diseases 0.000 description 1
- 208000028389 Nerve injury Diseases 0.000 description 1
- 206010033307 Overweight Diseases 0.000 description 1
- 102000004257 Potassium Channel Human genes 0.000 description 1
- 102000004330 Rhodopsin Human genes 0.000 description 1
- 108090000820 Rhodopsin Proteins 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 230000001594 aberrant effect Effects 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 229960001667 alogliptin Drugs 0.000 description 1
- ZSBOMTDTBDDKMP-OAHLLOKOSA-N alogliptin Chemical compound C=1C=CC=C(C#N)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 ZSBOMTDTBDDKMP-OAHLLOKOSA-N 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 230000033115 angiogenesis Effects 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 230000002567 autonomic effect Effects 0.000 description 1
- 210000003403 autonomic nervous system Anatomy 0.000 description 1
- 239000002585 base Substances 0.000 description 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 description 1
- 108010014499 beta-2 Adrenergic Receptors Proteins 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 235000019577 caloric intake Nutrition 0.000 description 1
- 230000003130 cardiopathic effect Effects 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 230000019522 cellular metabolic process Effects 0.000 description 1
- 208000026106 cerebrovascular disease Diseases 0.000 description 1
- 210000000349 chromosome Anatomy 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 230000034994 death Effects 0.000 description 1
- 230000006735 deficit Effects 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- 238000007599 discharging Methods 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 239000000446 fuel Substances 0.000 description 1
- 208000020694 gallbladder disease Diseases 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 230000005802 health problem Effects 0.000 description 1
- 230000001639 hypophagic effect Effects 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 206010022498 insulinoma Diseases 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 206010025482 malaise Diseases 0.000 description 1
- 230000028161 membrane depolarization Effects 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000009456 molecular mechanism Effects 0.000 description 1
- 230000008764 nerve damage Effects 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 230000002981 neuropathic effect Effects 0.000 description 1
- 125000002811 oleoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])/C([H])=C([H])\C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 238000007410 oral glucose tolerance test Methods 0.000 description 1
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 description 1
- 239000004025 pancreas hormone Substances 0.000 description 1
- 208000021255 pancreatic insulinoma Diseases 0.000 description 1
- 210000001428 peripheral nervous system Anatomy 0.000 description 1
- 108020001213 potassium channel Proteins 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 230000022558 protein metabolic process Effects 0.000 description 1
- 208000017443 reproductive system disease Diseases 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- QGJUIPDUBHWZPV-SGTAVMJGSA-N saxagliptin Chemical compound C1C(C2)CC(C3)CC2(O)CC13[C@H](N)C(=O)N1[C@H](C#N)C[C@@H]2C[C@@H]21 QGJUIPDUBHWZPV-SGTAVMJGSA-N 0.000 description 1
- 229960004937 saxagliptin Drugs 0.000 description 1
- 108010033693 saxagliptin Proteins 0.000 description 1
- 230000020341 sensory perception of pain Effects 0.000 description 1
- 229960004034 sitagliptin Drugs 0.000 description 1
- MFFMDFFZMYYVKS-SECBINFHSA-N sitagliptin Chemical compound C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F MFFMDFFZMYYVKS-SECBINFHSA-N 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 208000035408 type 1 diabetes mellitus 1 Diseases 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/04—Artificial tears; Irrigation solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Endocrinology (AREA)
- Ophthalmology & Optometry (AREA)
- Neurosurgery (AREA)
- Communicable Diseases (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Oncology (AREA)
- Psychiatry (AREA)
- Virology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Molecular Biology (AREA)
- Hospice & Palliative Care (AREA)
- AIDS & HIV (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Vascular Medicine (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US95016207P | 2007-07-17 | 2007-07-17 | |
US60/950,162 | 2007-07-17 | ||
PCT/US2008/070101 WO2009012275A1 (en) | 2007-07-17 | 2008-07-16 | Pyridone gpr119 g protein-coupled receptor agonists |
Publications (1)
Publication Number | Publication Date |
---|---|
CN101801957A true CN101801957A (zh) | 2010-08-11 |
Family
ID=39864683
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN200880108168A Pending CN101801957A (zh) | 2007-07-17 | 2008-07-16 | 吡啶酮gpr119g蛋白偶联受体激动剂 |
CN201310495045.6A Pending CN103550218A (zh) | 2007-07-17 | 2008-07-16 | 用于调节gpr119 g蛋白偶联受体的方法及所选化合物 |
CN2008801081672A Expired - Fee Related CN101801956B (zh) | 2007-07-17 | 2008-07-16 | 用于调节gpr119 g蛋白偶联受体的方法及所选化合物 |
Family Applications After (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201310495045.6A Pending CN103550218A (zh) | 2007-07-17 | 2008-07-16 | 用于调节gpr119 g蛋白偶联受体的方法及所选化合物 |
CN2008801081672A Expired - Fee Related CN101801956B (zh) | 2007-07-17 | 2008-07-16 | 用于调节gpr119 g蛋白偶联受体的方法及所选化合物 |
Country Status (27)
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN115504927A (zh) * | 2022-08-15 | 2022-12-23 | 广西中医药大学 | 4-甲基-2-对甲苯基-6-羰基吡啶-3-甲酸及其制备方法和用途 |
Families Citing this family (50)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8158652B2 (en) * | 2004-12-01 | 2012-04-17 | Msd K.K. | Substituted pyridone derivative |
WO2008137435A1 (en) | 2007-05-04 | 2008-11-13 | Bristol-Myers Squibb Company | [6,6] and [6,7]-bicyclic gpr119 g protein-coupled receptor agonists |
KR20100051814A (ko) * | 2007-07-17 | 2010-05-18 | 브리스톨-마이어스 스큅 컴퍼니 | Gpr119 g 단백질-커플링된 수용체의 조절 방법 및 선택된 화합물 |
EP2146210A1 (en) | 2008-04-07 | 2010-01-20 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY |
JP5627574B2 (ja) | 2008-06-03 | 2014-11-19 | インターミューン, インコーポレイテッド | 炎症性および線維性疾患を治療するための化合物および方法 |
JP2011528365A (ja) * | 2008-07-16 | 2011-11-17 | シェーリング コーポレイション | Gpr119モジュレーターとしての二環式ヘテロ環誘導体およびそれらの使用方法 |
WO2010009208A1 (en) * | 2008-07-16 | 2010-01-21 | Schering Corporation | Bicyclic heterocycle derivatives and methods of use thereof |
TW201006821A (en) * | 2008-07-16 | 2010-02-16 | Bristol Myers Squibb Co | Pyridone and pyridazone analogues as GPR119 modulators |
GB0904287D0 (en) | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
CA2754523A1 (en) * | 2009-03-20 | 2010-09-23 | Pfizer Inc. | 3-oxa-7-azabicyclo[3.3.1]nonanes |
KR20120046188A (ko) | 2009-06-24 | 2012-05-09 | 뉴로크린 바이오사이언시즈 인코퍼레이티드 | 신규 화합물, 약제학적 조성물 및 이에 관련된 방법 |
WO2010149685A1 (en) | 2009-06-24 | 2010-12-29 | Boehringer Ingelheim International Gmbh | New compounds, pharmaceutical composition and methods relating thereto |
WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
WO2011113947A1 (en) | 2010-03-18 | 2011-09-22 | Boehringer Ingelheim International Gmbh | Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions |
US8415367B2 (en) | 2010-04-08 | 2013-04-09 | Bristol-Myers Squibb Company | Pyrimidinylpiperidinyloxypyridinone analogues as GPR119 modulators |
US8729084B2 (en) | 2010-05-06 | 2014-05-20 | Bristol-Myers Squibb Company | Benzofuranyl analogues as GPR119 modulators |
BR112012028445A2 (pt) | 2010-05-06 | 2016-07-19 | Bristol Myers Squibb Co | compostos de heteroarila bicíclica como moduladores de gpr119 |
US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
SG188547A1 (en) | 2010-10-08 | 2013-04-30 | Cadila Healthcare Ltd | Novel gpr 119 agonists |
JP5848775B2 (ja) | 2010-12-06 | 2016-01-27 | コンフルエンス・ライフ・サイエンシズ,インコーポレーテッド | 置換ピリジノンピリジニル化合物 |
US9359300B2 (en) | 2010-12-06 | 2016-06-07 | Confluence Life Sciences, Inc. | Methyl/difluorophenyl-methoxy substituted pyridinone-pyridinyl compounds, methyl-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds, and methyl-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds |
WO2012123449A1 (en) * | 2011-03-14 | 2012-09-20 | Boehringer Ingelheim International Gmbh | N- cyclopropyl - n- piperidinylbenzamides as gpr119 modulators |
EP2718279B1 (en) | 2011-06-09 | 2016-08-10 | Rhizen Pharmaceuticals SA | Novel compounds as modulators of gpr-119 |
WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
EP2760862B1 (en) | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
US9174965B2 (en) | 2012-05-16 | 2015-11-03 | Bristol-Myers Squibb Company | Pyrimidinylpiperidinyloxypyridone analogues as GPR119 modulators |
EP2872127A1 (en) | 2012-07-11 | 2015-05-20 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
PT2921489T (pt) * | 2012-11-13 | 2017-12-01 | Nissan Chemical Ind Ltd | Composto de 2-piridona |
CN102993088A (zh) * | 2012-12-31 | 2013-03-27 | 东华大学 | 一种4-羟基-2-吡啶酮的制备方法 |
TW201444849A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
TW201444821A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代之哌啶化合物及其作為食慾素受體調節劑之用途 |
TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途 |
KR102653785B1 (ko) | 2013-06-07 | 2024-04-01 | 어클라리스 쎄라퓨틱스, 인코포레이티드 | 메틸/플루오로-피리디닐-메톡시 치환된 피리디논-피리디닐 화합물 및 플루오로-피리미디닐-메톡시 치환된 피리디논-피리디닐 화합물 |
WO2014202505A1 (de) | 2013-06-20 | 2014-12-24 | Bayer Cropscience Ag | Arylsulfid- und arylsulfoxid-derivate als akarizide und insektizide |
ES2761571T3 (es) | 2013-06-20 | 2020-05-20 | Bayer Cropscience Ag | Derivados de arilsulfuro y arilsulfóxido como acaricidas e insecticidas |
WO2015004028A1 (de) | 2013-07-08 | 2015-01-15 | Bayer Cropscience Ag | Sechsgliedrige c-n-verknüpfte arylsulfid- und arylsulfoxid- derivate als schädlingsbekämpfungsmittel |
KR102373700B1 (ko) | 2014-04-02 | 2022-03-11 | 인터뮨, 인크. | 항섬유성 피리디논 |
EP2929883A1 (en) | 2014-04-08 | 2015-10-14 | Institut Pasteur | Pyrazole derivatives as dihydroorotate dehydrogenase (DHODH) inhibitors |
EP3191468B1 (en) | 2014-09-11 | 2018-12-12 | Janssen Pharmaceutica NV | Substituted 2-azabicycles and their use as orexin receptor modulators |
WO2016130652A1 (en) | 2015-02-10 | 2016-08-18 | Vanderbilt University | Negative allosteric modulators of metabotropic glutamate receptor 3 |
JP6578116B2 (ja) * | 2015-03-25 | 2019-09-18 | 公益財団法人相模中央化学研究所 | 一置換(フルオロアルキル)エチレン類及びその製造方法 |
US10865194B2 (en) | 2017-11-03 | 2020-12-15 | Fondazione Istituto Italiano Di Tecnologia | Therapeutically active bicyclic-sulphonamides and pharmaceutical compositions |
US11844801B2 (en) | 2020-03-27 | 2023-12-19 | Aclaris Therapeutics, Inc. | Oral compositions of MK2 pathway inhibitor for treatment of immune conditions |
EP4153589A4 (en) | 2020-05-19 | 2024-06-12 | Kallyope, Inc. | AMPK ACTIVATORS |
CN116390925A (zh) | 2020-06-26 | 2023-07-04 | 卡尔优普公司 | Ampk活化剂 |
WO2022081573A1 (en) * | 2020-10-12 | 2022-04-21 | University Of Tennessee Research Foundation | Transient receptor potential canonical 3 inhibitors and methods of use thereof |
Family Cites Families (39)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3826643A (en) | 1967-08-07 | 1974-07-30 | American Cyanamid Co | Method of controlling undesirable plant species using 3-nitropyridines |
US5776983A (en) | 1993-12-21 | 1998-07-07 | Bristol-Myers Squibb Company | Catecholamine surrogates useful as β3 agonists |
US5488064A (en) | 1994-05-02 | 1996-01-30 | Bristol-Myers Squibb Company | Benzo 1,3 dioxole derivatives |
US5612359A (en) | 1994-08-26 | 1997-03-18 | Bristol-Myers Squibb Company | Substituted biphenyl isoxazole sulfonamides |
US5491134A (en) | 1994-09-16 | 1996-02-13 | Bristol-Myers Squibb Company | Sulfonic, phosphonic or phosphiniic acid β3 agonist derivatives |
US5541204A (en) | 1994-12-02 | 1996-07-30 | Bristol-Myers Squibb Company | Aryloxypropanolamine β 3 adrenergic agonists |
US5620997A (en) | 1995-05-31 | 1997-04-15 | Warner-Lambert Company | Isothiazolones |
AU6966696A (en) | 1995-10-05 | 1997-04-28 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
US5770615A (en) | 1996-04-04 | 1998-06-23 | Bristol-Myers Squibb Company | Catecholamine surrogates useful as β3 agonists |
US6566384B1 (en) | 1996-08-07 | 2003-05-20 | Darwin Discovery Ltd. | Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity |
TW536540B (en) | 1997-01-30 | 2003-06-11 | Bristol Myers Squibb Co | Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe |
UA57811C2 (uk) | 1997-11-21 | 2003-07-15 | Пфайзер Продактс Інк. | Фармацевтична композиція, що містить інгібітор альдозоредуктази та інгібітор глікогенфосфорилази (варіанти), комплект, який її включає, та способи лікування ссавців зі станом інсулінорезистентності |
IL140622A0 (en) | 1998-07-06 | 2002-02-10 | Bristol Myers Squibb Co | Biphenyl sufonamide derivatives, pharmaceutical compositions containing the same and methods for the preparation thereof |
AU3127900A (en) | 1998-12-23 | 2000-07-31 | Du Pont Pharmaceuticals Company | Thrombin or factor xa inhibitors |
US6586418B2 (en) | 2000-06-29 | 2003-07-01 | Bristol-Myers Squibb Company | Thrombin or factor Xa inhibitors |
EP1338651B9 (en) | 2000-12-01 | 2007-05-09 | Astellas Pharma Inc. | Method of screening remedy for diabetes |
ES2421511T3 (es) | 2001-12-21 | 2013-09-03 | X Ceptor Therapeutics Inc | Moduladores de LXR |
US7482366B2 (en) | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
OA12771A (en) * | 2002-02-14 | 2006-07-04 | Pharmacia Corp | Substituted pyridinones as modulators of P38 map kinase. |
US8293751B2 (en) | 2003-01-14 | 2012-10-23 | Arena Pharmaceuticals, Inc. | 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia |
PL378295A1 (pl) | 2003-02-24 | 2006-03-20 | Arena Pharmaceuticals, Inc. | Podstawione pochodne arylowe i heteroarylowe jako modulatory metabolizmu glukozy oraz profilaktyka i leczenie zaburzeń tego metabolizmu |
SE0301010D0 (sv) | 2003-04-07 | 2003-04-07 | Astrazeneca Ab | Novel compounds |
US7003597B2 (en) * | 2003-07-09 | 2006-02-21 | International Business Machines Corporation | Dynamic reallocation of data stored in buffers based on packet size |
UA86943C2 (ru) * | 2003-07-11 | 2009-06-10 | Арена Фармасьютикалз, Инк. | Тризамещенные производные арилов и гетероарилов как модуляторы метаболизма и профилактика и лечение связанных с ними нарушений |
AR045047A1 (es) * | 2003-07-11 | 2005-10-12 | Arena Pharm Inc | Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos |
WO2005007658A2 (en) * | 2003-07-14 | 2005-01-27 | Arena Pharmaceuticals, Inc. | Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
WO2005025504A2 (en) | 2003-09-12 | 2005-03-24 | Kemia, Inc. | Modulators of calcitonin and amylin activity |
WO2005085200A1 (ja) * | 2004-03-05 | 2005-09-15 | Banyu Pharmaceutical Co., Ltd. | ピリドン誘導体 |
EP2060266B1 (en) | 2004-03-17 | 2011-08-10 | 7TM Pharma A/S | Y4 selective receptor agonist PP2-36 for therapeutic interventions |
DK1756096T3 (da) | 2004-05-03 | 2009-10-26 | Hoffmann La Roche | Indolylderivater som lever-X-receptormodulatorer |
JP2008501698A (ja) | 2004-06-04 | 2008-01-24 | アリーナ ファーマシューティカルズ, インコーポレイテッド | 代謝の調節因子としての置換アリールおよびヘテロアリール誘導体ならびにそれらに関連する疾患の予防および処置 |
WO2006067532A1 (en) | 2004-12-24 | 2006-06-29 | Prosidion Ltd | G-protein coupled receptor agonists |
MY148521A (en) | 2005-01-10 | 2013-04-30 | Arena Pharm Inc | Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto |
US20060292073A1 (en) | 2005-06-23 | 2006-12-28 | Emory University | Stereoselective Synthesis of Amino Acid Analogs for Tumor Imaging |
US20090325924A1 (en) * | 2005-06-30 | 2009-12-31 | Stuart Edward | GPCR Agonists |
EP1907384A2 (en) | 2005-06-30 | 2008-04-09 | Prosidion Limited | Gpcr agonists |
EP2152707B1 (en) | 2007-05-04 | 2012-06-20 | Bristol-Myers Squibb Company | [6,5]-bicyclic gpr119 g protein-coupled receptor agonists |
WO2008137435A1 (en) | 2007-05-04 | 2008-11-13 | Bristol-Myers Squibb Company | [6,6] and [6,7]-bicyclic gpr119 g protein-coupled receptor agonists |
KR20100051814A (ko) * | 2007-07-17 | 2010-05-18 | 브리스톨-마이어스 스큅 컴퍼니 | Gpr119 g 단백질-커플링된 수용체의 조절 방법 및 선택된 화합물 |
-
2008
- 2008-07-16 KR KR1020107003333A patent/KR20100051814A/ko not_active Application Discontinuation
- 2008-07-16 ES ES08781867T patent/ES2371515T3/es active Active
- 2008-07-16 DK DK08781868.8T patent/DK2173737T3/da active
- 2008-07-16 PT PT08781867T patent/PT2170864E/pt unknown
- 2008-07-16 TW TW097127046A patent/TW200904440A/zh unknown
- 2008-07-16 PE PE2008001196A patent/PE20090888A1/es not_active Application Discontinuation
- 2008-07-16 AU AU2008276057A patent/AU2008276057B2/en not_active Ceased
- 2008-07-16 PL PL08781868T patent/PL2173737T3/pl unknown
- 2008-07-16 SI SI200830592T patent/SI2173737T1/sl unknown
- 2008-07-16 NZ NZ582664A patent/NZ582664A/en not_active IP Right Cessation
- 2008-07-16 EP EP08781868A patent/EP2173737B1/en not_active Not-in-force
- 2008-07-16 CA CA2693444A patent/CA2693444A1/en not_active Abandoned
- 2008-07-16 BR BRPI0814428-1A2A patent/BRPI0814428A2/pt not_active IP Right Cessation
- 2008-07-16 KR KR1020107003332A patent/KR20100045471A/ko not_active Application Discontinuation
- 2008-07-16 US US12/173,856 patent/US8003796B2/en active Active
- 2008-07-16 WO PCT/US2008/070103 patent/WO2009012277A1/en active Application Filing
- 2008-07-16 WO PCT/US2008/070101 patent/WO2009012275A1/en active Application Filing
- 2008-07-16 BR BRPI0815097A patent/BRPI0815097A2/pt not_active IP Right Cessation
- 2008-07-16 US US12/173,864 patent/US7928230B2/en active Active
- 2008-07-16 DK DK08781867.0T patent/DK2170864T3/da active
- 2008-07-16 CA CA2693439A patent/CA2693439A1/en not_active Abandoned
- 2008-07-16 AR ARP080103061A patent/AR067569A1/es not_active Application Discontinuation
- 2008-07-16 PT PT08781868T patent/PT2173737E/pt unknown
- 2008-07-16 PL PL08781867T patent/PL2170864T3/pl unknown
- 2008-07-16 NZ NZ582661A patent/NZ582661A/en not_active IP Right Cessation
- 2008-07-16 CN CN200880108168A patent/CN101801957A/zh active Pending
- 2008-07-16 JP JP2010517122A patent/JP5318867B2/ja not_active Expired - Fee Related
- 2008-07-16 CN CN201310495045.6A patent/CN103550218A/zh active Pending
- 2008-07-16 ES ES08781868T patent/ES2378914T3/es active Active
- 2008-07-16 EP EP08781867A patent/EP2170864B1/en not_active Not-in-force
- 2008-07-16 PE PE2008001197A patent/PE20090449A1/es not_active Application Discontinuation
- 2008-07-16 AT AT08781868T patent/ATE540945T1/de active
- 2008-07-16 AU AU2008276055A patent/AU2008276055B2/en not_active Ceased
- 2008-07-16 AR ARP080103060A patent/AR067568A1/es unknown
- 2008-07-16 TW TW097127045A patent/TW200904439A/zh unknown
- 2008-07-16 EA EA201000211A patent/EA016595B1/ru not_active IP Right Cessation
- 2008-07-16 EA EA201000210A patent/EA018709B1/ru not_active IP Right Cessation
- 2008-07-16 SI SI200830464T patent/SI2170864T1/sl unknown
- 2008-07-16 CN CN2008801081672A patent/CN101801956B/zh not_active Expired - Fee Related
- 2008-07-16 AT AT08781867T patent/ATE524460T1/de active
- 2008-07-16 JP JP2010517123A patent/JP5301539B2/ja not_active Expired - Fee Related
- 2008-07-17 CL CL200802110A patent/CL2008002110A1/es unknown
- 2008-07-17 CL CL200802111A patent/CL2008002111A1/es unknown
-
2010
- 2010-01-08 ZA ZA2010/00151A patent/ZA201000151B/en unknown
- 2010-01-15 ZA ZA2010/00326A patent/ZA201000326B/en unknown
- 2010-01-15 CO CO10003756A patent/CO6160315A2/es unknown
- 2010-04-15 HK HK10103702.1A patent/HK1136298A1/xx not_active IP Right Cessation
- 2010-10-05 HK HK10109487.9A patent/HK1143136A1/xx not_active IP Right Cessation
-
2011
- 2011-03-07 US US13/041,564 patent/US8178561B2/en active Active
- 2011-06-14 US US13/159,497 patent/US8232404B2/en active Active
- 2011-11-02 HR HR20110806T patent/HRP20110806T1/hr unknown
- 2011-12-14 CY CY20111101241T patent/CY1112151T1/el unknown
-
2012
- 2012-03-07 HR HR20120221T patent/HRP20120221T1/hr unknown
- 2012-04-09 CY CY20121100343T patent/CY1112751T1/el unknown
- 2012-04-24 US US13/454,789 patent/US20120232048A1/en not_active Abandoned
- 2012-06-12 US US13/494,489 patent/US8513424B2/en active Active
-
2013
- 2013-07-10 JP JP2013144778A patent/JP2013237680A/ja not_active Withdrawn
- 2013-08-26 IL IL228120A patent/IL228120A0/en unknown
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN115504927A (zh) * | 2022-08-15 | 2022-12-23 | 广西中医药大学 | 4-甲基-2-对甲苯基-6-羰基吡啶-3-甲酸及其制备方法和用途 |
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CN101801957A (zh) | 吡啶酮gpr119g蛋白偶联受体激动剂 | |
US8372837B2 (en) | Pyridone and pyridazone analogues as GPR119 modulators | |
US8314095B2 (en) | [6,6] and [6,7]-bicyclic GPR119 G protein-coupled receptor agonists | |
KR102151288B1 (ko) | [오르토 바이 (헤테로 )아릴]-[2-(메타 바이 (헤테로 )아릴)-피롤리딘-1-일]-메타논 유도체인 오렉신 수용체 안타고니스트 | |
CN102971311B (zh) | 作为gpr119调节剂的二环杂芳基化合物 | |
CN101668759A (zh) | [6,5]-双环gpr119g蛋白-偶合受体激动剂 | |
CN103619817A (zh) | 新颖的二环含氮杂芳基tgr5受体调节剂 | |
CN102933576A (zh) | 作为gpr119调节剂的嘧啶基哌啶基氧基吡啶酮类似物 | |
EP2850073B1 (en) | Pyrimidinylpiperidinyloxypyridone analogues as gpr119 modulators |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
C06 | Publication | ||
PB01 | Publication | ||
C10 | Entry into substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
AD01 | Patent right deemed abandoned |
Effective date of abandoning: 20100811 |
|
C20 | Patent right or utility model deemed to be abandoned or is abandoned |