KR20100051814A - Gpr119 g 단백질-커플링된 수용체의 조절 방법 및 선택된 화합물 - Google Patents
Gpr119 g 단백질-커플링된 수용체의 조절 방법 및 선택된 화합물 Download PDFInfo
- Publication number
- KR20100051814A KR20100051814A KR1020107003333A KR20107003333A KR20100051814A KR 20100051814 A KR20100051814 A KR 20100051814A KR 1020107003333 A KR1020107003333 A KR 1020107003333A KR 20107003333 A KR20107003333 A KR 20107003333A KR 20100051814 A KR20100051814 A KR 20100051814A
- Authority
- KR
- South Korea
- Prior art keywords
- cycloalkyl
- aryl
- alkyl
- heteroaryl
- heterocyclyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims abstract description 109
- 238000000034 method Methods 0.000 title claims abstract description 62
- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 title description 10
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 title description 10
- 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 0.000 claims abstract description 62
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 claims abstract description 61
- 230000000694 effects Effects 0.000 claims abstract description 49
- 239000003814 drug Substances 0.000 claims abstract description 16
- 229940124597 therapeutic agent Drugs 0.000 claims abstract description 16
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 784
- 125000003118 aryl group Chemical group 0.000 claims description 727
- 125000000217 alkyl group Chemical group 0.000 claims description 718
- 125000001072 heteroaryl group Chemical group 0.000 claims description 672
- 125000000623 heterocyclic group Chemical group 0.000 claims description 604
- 125000003342 alkenyl group Chemical group 0.000 claims description 427
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 396
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 396
- 125000000304 alkynyl group Chemical group 0.000 claims description 384
- 125000005843 halogen group Chemical group 0.000 claims description 295
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 293
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 261
- 229910052739 hydrogen Inorganic materials 0.000 claims description 260
- 239000001257 hydrogen Substances 0.000 claims description 260
- 125000001188 haloalkyl group Chemical group 0.000 claims description 244
- 150000002431 hydrogen Chemical class 0.000 claims description 232
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 191
- -1 —NH 2 Chemical group 0.000 claims description 183
- 125000003545 alkoxy group Chemical group 0.000 claims description 76
- 229910052717 sulfur Inorganic materials 0.000 claims description 72
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 28
- 229910052799 carbon Inorganic materials 0.000 claims description 25
- 229910052757 nitrogen Inorganic materials 0.000 claims description 24
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 15
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 10
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 6
- 125000005842 heteroatom Chemical group 0.000 claims description 6
- 229910052760 oxygen Inorganic materials 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 claims description 5
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims description 5
- 239000003112 inhibitor Substances 0.000 claims description 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 229920000728 polyester Polymers 0.000 description 203
- 206010012601 diabetes mellitus Diseases 0.000 description 37
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 31
- 208000008589 Obesity Diseases 0.000 description 20
- 201000010099 disease Diseases 0.000 description 20
- 235000020824 obesity Nutrition 0.000 description 19
- 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 description 18
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 18
- 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 description 17
- 239000008103 glucose Substances 0.000 description 17
- 210000000227 basophil cell of anterior lobe of hypophysis Anatomy 0.000 description 16
- 208000035475 disorder Diseases 0.000 description 11
- 230000003914 insulin secretion Effects 0.000 description 11
- 201000001421 hyperglycemia Diseases 0.000 description 10
- 208000032928 Dyslipidaemia Diseases 0.000 description 9
- 206010020772 Hypertension Diseases 0.000 description 9
- 102000004877 Insulin Human genes 0.000 description 9
- 108090001061 Insulin Proteins 0.000 description 9
- 208000017170 Lipid metabolism disease Diseases 0.000 description 9
- 238000011161 development Methods 0.000 description 9
- 229940125396 insulin Drugs 0.000 description 9
- 238000011282 treatment Methods 0.000 description 9
- 210000004027 cell Anatomy 0.000 description 8
- 206010022489 Insulin Resistance Diseases 0.000 description 7
- 208000001145 Metabolic Syndrome Diseases 0.000 description 6
- 208000017169 kidney disease Diseases 0.000 description 6
- 208000031225 myocardial ischemia Diseases 0.000 description 6
- 208000028698 Cognitive impairment Diseases 0.000 description 5
- 208000006011 Stroke Diseases 0.000 description 5
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 description 5
- 208000010877 cognitive disease Diseases 0.000 description 5
- 150000002632 lipids Chemical class 0.000 description 5
- 230000009467 reduction Effects 0.000 description 5
- 230000002792 vascular Effects 0.000 description 5
- 201000001320 Atherosclerosis Diseases 0.000 description 4
- 208000024172 Cardiovascular disease Diseases 0.000 description 4
- 208000010412 Glaucoma Diseases 0.000 description 4
- 206010060378 Hyperinsulinaemia Diseases 0.000 description 4
- 206010028980 Neoplasm Diseases 0.000 description 4
- 210000004369 blood Anatomy 0.000 description 4
- 239000008280 blood Substances 0.000 description 4
- 201000011510 cancer Diseases 0.000 description 4
- 230000001419 dependent effect Effects 0.000 description 4
- 230000003451 hyperinsulinaemic effect Effects 0.000 description 4
- 201000008980 hyperinsulinism Diseases 0.000 description 4
- 208000015181 infectious disease Diseases 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 239000008194 pharmaceutical composition Substances 0.000 description 4
- 102000005962 receptors Human genes 0.000 description 4
- 108020003175 receptors Proteins 0.000 description 4
- 230000004044 response Effects 0.000 description 4
- 208000011580 syndromic disease Diseases 0.000 description 4
- 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 3
- 208000020084 Bone disease Diseases 0.000 description 3
- 206010012289 Dementia Diseases 0.000 description 3
- 208000002705 Glucose Intolerance Diseases 0.000 description 3
- 108010010369 HIV Protease Proteins 0.000 description 3
- 241000282412 Homo Species 0.000 description 3
- 208000035150 Hypercholesterolemia Diseases 0.000 description 3
- 208000031226 Hyperlipidaemia Diseases 0.000 description 3
- 102000007330 LDL Lipoproteins Human genes 0.000 description 3
- 206010033645 Pancreatitis Diseases 0.000 description 3
- 208000017442 Retinal disease Diseases 0.000 description 3
- 206010038923 Retinopathy Diseases 0.000 description 3
- 230000002159 abnormal effect Effects 0.000 description 3
- 230000006907 apoptotic process Effects 0.000 description 3
- 239000002775 capsule Substances 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 208000029078 coronary artery disease Diseases 0.000 description 3
- 230000003111 delayed effect Effects 0.000 description 3
- 239000003937 drug carrier Substances 0.000 description 3
- 230000004217 heart function Effects 0.000 description 3
- 208000006575 hypertriglyceridemia Diseases 0.000 description 3
- 230000001965 increasing effect Effects 0.000 description 3
- 230000004770 neurodegeneration Effects 0.000 description 3
- 208000015122 neurodegenerative disease Diseases 0.000 description 3
- 201000001119 neuropathy Diseases 0.000 description 3
- 230000007823 neuropathy Effects 0.000 description 3
- 208000033808 peripheral neuropathy Diseases 0.000 description 3
- 201000009104 prediabetes syndrome Diseases 0.000 description 3
- 208000037803 restenosis Diseases 0.000 description 3
- 230000029663 wound healing Effects 0.000 description 3
- 108700028369 Alleles Proteins 0.000 description 2
- 206010052895 Coronary artery insufficiency Diseases 0.000 description 2
- 101800000224 Glucagon-like peptide 1 Proteins 0.000 description 2
- 102400000322 Glucagon-like peptide 1 Human genes 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
- 206010019280 Heart failures Diseases 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 description 2
- 230000005856 abnormality Effects 0.000 description 2
- 230000004913 activation Effects 0.000 description 2
- 239000012190 activator Substances 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 239000000556 agonist Substances 0.000 description 2
- 230000002567 autonomic effect Effects 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 230000002526 effect on cardiovascular system Effects 0.000 description 2
- 230000002708 enhancing effect Effects 0.000 description 2
- 235000019197 fats Nutrition 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 230000006870 function Effects 0.000 description 2
- 230000002641 glycemic effect Effects 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 229940088597 hormone Drugs 0.000 description 2
- 239000005556 hormone Substances 0.000 description 2
- 239000007972 injectable composition Substances 0.000 description 2
- 210000003734 kidney Anatomy 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 210000000496 pancreas Anatomy 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 239000012453 solvate Substances 0.000 description 2
- 241000894007 species Species 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 239000003981 vehicle Substances 0.000 description 2
- 208000011732 Abnormal glucose homeostasis Diseases 0.000 description 1
- 206010003211 Arteriosclerosis coronary artery Diseases 0.000 description 1
- 210000002237 B-cell of pancreatic islet Anatomy 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- 208000002177 Cataract Diseases 0.000 description 1
- 241000282693 Cercopithecidae Species 0.000 description 1
- 102100025892 Complement C1q tumor necrosis factor-related protein 1 Human genes 0.000 description 1
- IVOMOUWHDPKRLL-KQYNXXCUSA-N Cyclic adenosine monophosphate Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-KQYNXXCUSA-N 0.000 description 1
- 208000002249 Diabetes Complications 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
- 101000611338 Homo sapiens Rhodopsin Proteins 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241000699666 Mus <mouse, genus> Species 0.000 description 1
- 101100069093 Mus musculus Gpr119 gene Proteins 0.000 description 1
- 208000028389 Nerve injury Diseases 0.000 description 1
- 206010033307 Overweight Diseases 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- 102000004257 Potassium Channel Human genes 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- IVOMOUWHDPKRLL-UHFFFAOYSA-N UNPD107823 Natural products O1C2COP(O)(=O)OC2C(O)C1N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-UHFFFAOYSA-N 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000001154 acute effect Effects 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
- 238000010171 animal model Methods 0.000 description 1
- 229940125708 antidiabetic agent Drugs 0.000 description 1
- 239000003472 antidiabetic agent Substances 0.000 description 1
- 239000003524 antilipemic agent Substances 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 239000011324 bead Substances 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 description 1
- 102000016966 beta-2 Adrenergic Receptors Human genes 0.000 description 1
- 108010014499 beta-2 Adrenergic Receptors Proteins 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 235000019577 caloric intake Nutrition 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 235000014633 carbohydrates Nutrition 0.000 description 1
- 230000030833 cell death Effects 0.000 description 1
- 230000019522 cellular metabolic process Effects 0.000 description 1
- 210000000349 chromosome Anatomy 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 208000026758 coronary atherosclerosis Diseases 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 229940095074 cyclic amp Drugs 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
- 230000029087 digestion Effects 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000003028 elevating effect Effects 0.000 description 1
- 208000030533 eye disease Diseases 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 235000012631 food intake Nutrition 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- 239000000446 fuel Substances 0.000 description 1
- 208000020694 gallbladder disease Diseases 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 208000035474 group of disease Diseases 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 230000005802 health problem Effects 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 230000003054 hormonal effect Effects 0.000 description 1
- 102000056352 human GPR119 Human genes 0.000 description 1
- 230000001639 hypophagic effect Effects 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 230000004941 influx Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 230000009456 molecular mechanism Effects 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 230000008764 nerve damage Effects 0.000 description 1
- 210000000653 nervous system Anatomy 0.000 description 1
- 230000002981 neuropathic effect Effects 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- BOWVQLFMWHZBEF-KTKRTIGZSA-N oleoyl ethanolamide Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)NCCO BOWVQLFMWHZBEF-KTKRTIGZSA-N 0.000 description 1
- 238000007410 oral glucose tolerance test Methods 0.000 description 1
- 238000012261 overproduction Methods 0.000 description 1
- 125000001715 oxadiazolyl group Chemical group 0.000 description 1
- 230000008506 pathogenesis Effects 0.000 description 1
- 125000001151 peptidyl group Chemical group 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 239000008024 pharmaceutical diluent Substances 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 108020001213 potassium channel Proteins 0.000 description 1
- 230000003823 potassium efflux Effects 0.000 description 1
- 230000022558 protein metabolic process Effects 0.000 description 1
- 235000018102 proteins Nutrition 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 208000017443 reproductive system disease Diseases 0.000 description 1
- 210000001525 retina Anatomy 0.000 description 1
- 230000002207 retinal effect Effects 0.000 description 1
- 229960004937 saxagliptin Drugs 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
- 108010033693 saxagliptin Proteins 0.000 description 1
- 238000007789 sealing Methods 0.000 description 1
- 230000000276 sedentary effect 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
- 150000003384 small molecules Chemical class 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 208000035408 type 1 diabetes mellitus 1 Diseases 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 229960001254 vildagliptin Drugs 0.000 description 1
- SYOKIDBDQMKNDQ-XWTIBIIYSA-N vildagliptin Chemical compound C1C(O)(C2)CC(C3)CC1CC32NCC(=O)N1CCC[C@H]1C#N SYOKIDBDQMKNDQ-XWTIBIIYSA-N 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 230000004580 weight loss Effects 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)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Ophthalmology & Optometry (AREA)
- Endocrinology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- Emergency Medicine (AREA)
- Virology (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- AIDS & HIV (AREA)
- Vascular Medicine (AREA)
- Molecular Biology (AREA)
- Orthopedic Medicine & Surgery (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US95016207P | 2007-07-17 | 2007-07-17 | |
US60/950,162 | 2007-07-17 |
Publications (1)
Publication Number | Publication Date |
---|---|
KR20100051814A true KR20100051814A (ko) | 2010-05-18 |
Family
ID=39864683
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1020107003332A KR20100045471A (ko) | 2007-07-17 | 2008-07-16 | 피리돈 gpr119 g 단백질-커플링된 수용체 효능제 |
KR1020107003333A KR20100051814A (ko) | 2007-07-17 | 2008-07-16 | Gpr119 g 단백질-커플링된 수용체의 조절 방법 및 선택된 화합물 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1020107003332A KR20100045471A (ko) | 2007-07-17 | 2008-07-16 | 피리돈 gpr119 g 단백질-커플링된 수용체 효능제 |
Country Status (27)
Families Citing this family (51)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2005310467B2 (en) * | 2004-12-01 | 2011-06-23 | Msd K.K. | Substituted pyridone derivative |
EP2144902B1 (en) | 2007-05-04 | 2012-05-16 | Bristol-Myers Squibb Company | [6,6]and [6,7]-bicyclic gpr119 g protein-coupled receptor agonists |
EP2170864B1 (en) * | 2007-07-17 | 2011-09-14 | Bristol-Myers Squibb Company | Pyridone gpr119 g protein-coupled receptor agonists |
EP2108960A1 (en) | 2008-04-07 | 2009-10-14 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY |
US8304413B2 (en) | 2008-06-03 | 2012-11-06 | Intermune, Inc. | Compounds and methods for treating inflammatory and fibrotic disorders |
TW201006821A (en) * | 2008-07-16 | 2010-02-16 | Bristol Myers Squibb Co | Pyridone and pyridazone analogues as GPR119 modulators |
CA2730606A1 (en) | 2008-07-16 | 2010-01-21 | Schering Corporation | Bicyclic heterocycle derivatives and methods of use thereof |
WO2010009195A1 (en) * | 2008-07-16 | 2010-01-21 | Schering Corporation | Bicyclic heterocycle derivatives and use thereof as gpr119 modulators |
GB0904287D0 (en) | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
EP2408780A2 (en) * | 2009-03-20 | 2012-01-25 | Pfizer Inc. | 3-oxa-7-azabicycloý3.3.1¨nonanes |
WO2010149685A1 (en) | 2009-06-24 | 2010-12-29 | Boehringer Ingelheim International Gmbh | New compounds, pharmaceutical composition and methods relating thereto |
NZ596445A (en) | 2009-06-24 | 2013-04-26 | Boehringer Ingelheim Int | 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 |
EP2547339A1 (en) | 2010-03-18 | 2013-01-23 | 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 |
EP2566862B1 (en) | 2010-05-06 | 2015-09-16 | 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 |
TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
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 |
EA022501B1 (ru) | 2010-10-08 | 2016-01-29 | Кадила Хелзкэр Лимитед | Агонисты gpr 119 |
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 |
DK2648516T3 (da) | 2010-12-06 | 2019-01-02 | Aclaris Therapeutics Inc | Substituerede pyridinon-pyridinylforbindelser |
WO2012123449A1 (en) * | 2011-03-14 | 2012-09-20 | Boehringer Ingelheim International Gmbh | N- cyclopropyl - n- piperidinylbenzamides as gpr119 modulators |
WO2012170867A1 (en) | 2011-06-09 | 2012-12-13 | 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 |
WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
WO2013173198A1 (en) | 2012-05-16 | 2013-11-21 | Bristol-Myers Squibb Company | Pyrimidinylpiperidinyloxypyridone analogues as gpr119 modulators |
AU2013290100A1 (en) | 2012-07-11 | 2015-01-29 | 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 |
IN2015DN03869A (US07928230-20110419-C00056.png) * | 2012-11-13 | 2015-10-02 | Taisho Pharmaceutical Co Ltd | |
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 |
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 |
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 |
DK3003039T3 (da) | 2013-06-07 | 2021-05-25 | Aclaris Therapeutics Inc | Methyl/fluor-pyridinyl-metoxy-substituerede pyridinon-pyridinyl-forbindelser og fluor-pyrimidinyl-metoxy-substituerede pyridinon-pyridinyl-forbindelser |
ES2761571T3 (es) | 2013-06-20 | 2020-05-20 | Bayer Cropscience Ag | Derivados de arilsulfuro y arilsulfóxido como acaricidas e insecticidas |
US9981928B2 (en) | 2013-06-20 | 2018-05-29 | Bayer Cropscience Aktiengesellschaft | Aryl sulfide derivatives and aryl sulfoxide derivatives as acaricides and insecticides |
EP3019481B1 (de) | 2013-07-08 | 2019-03-06 | Bayer CropScience Aktiengesellschaft | Sechsgliedrige c-n-verknüpfte arylsulfid- und arylsulfoxid- derivate als schädlingsbekämpfungsmittel |
CA2943363A1 (en) | 2014-04-02 | 2015-10-08 | Intermune, Inc. | Anti-fibrotic pyridinones |
EP2929883A1 (en) | 2014-04-08 | 2015-10-14 | Institut Pasteur | Pyrazole derivatives as dihydroorotate dehydrogenase (DHODH) inhibitors |
US9611262B2 (en) | 2014-09-11 | 2017-04-04 | 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 |
EP4132524A1 (en) | 2020-03-27 | 2023-02-15 | Aclaris Therapeutics, Inc. | Oral compositions of mk2 pathway inhibitor for treatment of immune conditions |
UY39222A (es) | 2020-05-19 | 2021-11-30 | Kallyope Inc | Activadores de la ampk |
EP4172162A4 (en) | 2020-06-26 | 2024-08-07 | Kallyope Inc | AMPK ACTIVATORS |
WO2022081573A1 (en) * | 2020-10-12 | 2022-04-21 | University Of Tennessee Research Foundation | Transient receptor potential canonical 3 inhibitors and methods of use thereof |
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 |
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 |
AU767456B2 (en) | 1998-07-06 | 2003-11-13 | Bristol-Myers Squibb Company | Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists |
CA2320730A1 (en) | 1998-12-23 | 2000-07-06 | Renhua Li | Thrombin or factor xa inhibitors |
US6586418B2 (en) | 2000-06-29 | 2003-07-01 | Bristol-Myers Squibb Company | Thrombin or factor Xa inhibitors |
ES2280435T3 (es) | 2000-12-01 | 2007-09-16 | Astellas Pharma Inc. | Metodo de exploracion de remedios para la diabetes. |
US7482366B2 (en) * | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
AU2002351412B2 (en) * | 2001-12-21 | 2010-05-20 | Exelixis Patent Company Llc | Modulators of LXR |
JP4164031B2 (ja) * | 2002-02-14 | 2008-10-08 | ファルマシア コーポレーション | P38mapキナーゼのモジュレータとしての置換されたピリジノン |
ATE374766T1 (de) | 2003-01-14 | 2007-10-15 | Arena Pharm Inc | 1,2,3-trisubstituierte aryl- und heteroarylderivate als modulatoren des metabolismus zur vorbeugung und behandlung von metabolismus-bedingten krankheiten wie diabetes oder hyperglykämie |
EP1606282B1 (en) | 2003-02-24 | 2008-11-12 | Arena Pharmaceuticals, Inc. | Phenyl- and pyridylpipereidinye-derivatives as modulators of glucose metabolism |
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 |
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 |
CN100509798C (zh) * | 2003-07-11 | 2009-07-08 | 艾尼纳制药公司 | 作为新陈代谢调节剂的三取代芳基和杂芳基衍生物以及预防和治疗与其相关之病症 |
AU2004257267B2 (en) * | 2003-07-14 | 2009-12-03 | Arena Pharmaceuticals,Inc | Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
US20070088163A1 (en) | 2003-09-12 | 2007-04-19 | Kemia, Inc. | Modulators of calcitonin and amylin activity |
EP1741703A4 (en) * | 2004-03-05 | 2009-11-25 | Banyu Pharma Co Ltd | PYRIDONE DERIVATIVE |
EP2060266B1 (en) | 2004-03-17 | 2011-08-10 | 7TM Pharma A/S | Y4 selective receptor agonist PP2-36 for therapeutic interventions |
KR100893449B1 (ko) * | 2004-05-03 | 2009-04-17 | 에프. 호프만-라 로슈 아게 | 간-x-수용체 조절제로서의 인돌일 유도체 |
PT1756084E (pt) | 2004-06-04 | 2009-02-17 | Arena Pharm Inc | Composto seleccionado de compostos de fórmula (i) e seus sais, solvatos, hidratos e n-óxidos farmaceuticamente aceitáveis |
JP5065908B2 (ja) | 2004-12-24 | 2012-11-07 | プロシディオン・リミテッド | Gタンパク質結合受容体作動薬 |
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 |
JP5349960B2 (ja) * | 2005-06-23 | 2013-11-20 | エモリー ユニバーシティー | 腫瘍画像化のためのアミノ酸類似体の立体選択的合成 |
JP5114395B2 (ja) * | 2005-06-30 | 2013-01-09 | プロシディオン・リミテッド | Gpcrアゴニスト |
JP2008545008A (ja) | 2005-06-30 | 2008-12-11 | プロシディオン・リミテッド | Gpcrアゴニスト |
JP2010526146A (ja) | 2007-05-04 | 2010-07-29 | ブリストル−マイヤーズ スクイブ カンパニー | [6,5]−二環式gpr119gタンパク質結合受容体アゴニスト |
EP2144902B1 (en) | 2007-05-04 | 2012-05-16 | Bristol-Myers Squibb Company | [6,6]and [6,7]-bicyclic gpr119 g protein-coupled receptor agonists |
EP2170864B1 (en) * | 2007-07-17 | 2011-09-14 | Bristol-Myers Squibb Company | Pyridone gpr119 g protein-coupled receptor agonists |
-
2008
- 2008-07-16 EP EP08781867A patent/EP2170864B1/en not_active Not-in-force
- 2008-07-16 AU AU2008276057A patent/AU2008276057B2/en not_active Ceased
- 2008-07-16 US US12/173,856 patent/US8003796B2/en active Active
- 2008-07-16 CA CA2693439A patent/CA2693439A1/en not_active Abandoned
- 2008-07-16 SI SI200830592T patent/SI2173737T1/sl unknown
- 2008-07-16 BR BRPI0815097A patent/BRPI0815097A2/pt not_active IP Right Cessation
- 2008-07-16 NZ NZ582664A patent/NZ582664A/en not_active IP Right Cessation
- 2008-07-16 AU AU2008276055A patent/AU2008276055B2/en not_active Ceased
- 2008-07-16 EA EA201000210A patent/EA018709B1/ru not_active IP Right Cessation
- 2008-07-16 PE PE2008001197A patent/PE20090449A1/es not_active Application Discontinuation
- 2008-07-16 JP JP2010517123A patent/JP5301539B2/ja not_active Expired - Fee Related
- 2008-07-16 TW TW097127046A patent/TW200904440A/zh unknown
- 2008-07-16 US US12/173,864 patent/US7928230B2/en active Active
- 2008-07-16 EA EA201000211A patent/EA016595B1/ru not_active IP Right Cessation
- 2008-07-16 JP JP2010517122A patent/JP5318867B2/ja not_active Expired - Fee Related
- 2008-07-16 AT AT08781867T patent/ATE524460T1/de active
- 2008-07-16 CN CN2008801081672A patent/CN101801956B/zh not_active Expired - Fee Related
- 2008-07-16 NZ NZ582661A patent/NZ582661A/en not_active IP Right Cessation
- 2008-07-16 CN CN201310495045.6A patent/CN103550218A/zh active Pending
- 2008-07-16 PL PL08781868T patent/PL2173737T3/pl unknown
- 2008-07-16 PE PE2008001196A patent/PE20090888A1/es not_active Application Discontinuation
- 2008-07-16 AT AT08781868T patent/ATE540945T1/de active
- 2008-07-16 ES ES08781868T patent/ES2378914T3/es active Active
- 2008-07-16 EP EP08781868A patent/EP2173737B1/en not_active Not-in-force
- 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 PT PT08781868T patent/PT2173737E/pt unknown
- 2008-07-16 KR KR1020107003332A patent/KR20100045471A/ko not_active Application Discontinuation
- 2008-07-16 CA CA2693444A patent/CA2693444A1/en not_active Abandoned
- 2008-07-16 DK DK08781867.0T patent/DK2170864T3/da active
- 2008-07-16 SI SI200830464T patent/SI2170864T1/sl unknown
- 2008-07-16 BR BRPI0814428-1A2A patent/BRPI0814428A2/pt not_active IP Right Cessation
- 2008-07-16 AR ARP080103061A patent/AR067569A1/es not_active Application Discontinuation
- 2008-07-16 CN CN200880108168A patent/CN101801957A/zh active Pending
- 2008-07-16 KR KR1020107003333A patent/KR20100051814A/ko not_active Application Discontinuation
- 2008-07-16 TW TW097127045A patent/TW200904439A/zh unknown
- 2008-07-16 DK DK08781868.8T patent/DK2173737T3/da active
- 2008-07-16 PT PT08781867T patent/PT2170864E/pt unknown
- 2008-07-16 PL PL08781867T patent/PL2170864T3/pl unknown
- 2008-07-16 ES ES08781867T patent/ES2371515T3/es active Active
- 2008-07-16 AR ARP080103060A patent/AR067568A1/es unknown
- 2008-07-17 CL CL200802111A patent/CL2008002111A1/es unknown
- 2008-07-17 CL CL200802110A patent/CL2008002110A1/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
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP5301539B2 (ja) | Gpr119gタンパク質共役受容体の調節方法および選択された化合物 | |
US8372837B2 (en) | Pyridone and pyridazone analogues as GPR119 modulators | |
US8476283B2 (en) | [6,5]—bicyclic GPR119 G protein-coupled receptor agonists | |
US8513265B2 (en) | [6,6] and [6,7]-bicyclic GPR119 G protein-coupled receptor agonists | |
US8729084B2 (en) | Benzofuranyl analogues as GPR119 modulators | |
JP2013525489A (ja) | Gpr119修飾因子としての二環式ヘテロアリール類似体 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
WITN | Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid |