JP2013533279A5 - - Google Patents
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- JP2013533279A5 JP2013533279A5 JP2013521136A JP2013521136A JP2013533279A5 JP 2013533279 A5 JP2013533279 A5 JP 2013533279A5 JP 2013521136 A JP2013521136 A JP 2013521136A JP 2013521136 A JP2013521136 A JP 2013521136A JP 2013533279 A5 JP2013533279 A5 JP 2013533279A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- alkyl
- independently
- 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.)
- Granted
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- 150000003839 salts Chemical class 0.000 claims description 134
- 150000001875 compounds Chemical class 0.000 claims description 128
- -1 cyano, carboxy, formyl Chemical group 0.000 claims description 102
- 125000000217 alkyl group Chemical group 0.000 claims description 81
- 125000004432 carbon atom Chemical group C* 0.000 claims description 51
- 229910052799 carbon Inorganic materials 0.000 claims description 42
- 229910052739 hydrogen Inorganic materials 0.000 claims description 38
- 239000001257 hydrogen Substances 0.000 claims description 38
- 125000003545 alkoxy group Chemical group 0.000 claims description 30
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 29
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 25
- 229910052757 nitrogen Inorganic materials 0.000 claims description 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 18
- 125000004193 piperazinyl group Chemical group 0.000 claims description 15
- 125000003282 alkyl amino group Chemical group 0.000 claims description 14
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 13
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 10
- 125000004076 pyridyl group Chemical group 0.000 claims description 7
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims description 5
- 125000003386 piperidinyl group Chemical group 0.000 claims description 5
- 125000003003 spiro group Chemical group 0.000 claims description 5
- 125000003342 alkenyl group Chemical group 0.000 claims description 4
- 125000000304 alkynyl group Chemical group 0.000 claims description 3
- 125000005843 halogen group Chemical group 0.000 claims 28
- 125000000623 heterocyclic group Chemical group 0.000 claims 27
- 150000001721 carbon Chemical group 0.000 claims 24
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 22
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 20
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 19
- 239000003814 drug Substances 0.000 claims 16
- 150000002431 hydrogen Chemical class 0.000 claims 16
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 15
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 13
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 12
- 208000035475 disorder Diseases 0.000 claims 11
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 11
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 9
- 206010022489 Insulin Resistance Diseases 0.000 claims 9
- 201000010099 disease Diseases 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 125000002757 morpholinyl group Chemical group 0.000 claims 9
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 9
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 7
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 208000002705 Glucose Intolerance Diseases 0.000 claims 6
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 6
- 208000008589 Obesity Diseases 0.000 claims 6
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 6
- 239000004480 active ingredient Substances 0.000 claims 6
- 125000004423 acyloxy group Chemical group 0.000 claims 6
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 6
- 206010012601 diabetes mellitus Diseases 0.000 claims 6
- 235000020824 obesity Nutrition 0.000 claims 6
- 201000009104 prediabetes syndrome Diseases 0.000 claims 6
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 5
- 125000003725 azepanyl group Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 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 5
- 125000003226 pyrazolyl group Chemical group 0.000 claims 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 4
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 4
- 102000000452 Acetyl-CoA carboxylase Human genes 0.000 claims 4
- 108010016219 Acetyl-CoA carboxylase Proteins 0.000 claims 4
- 108010018763 Biotin carboxylase Proteins 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 4
- 125000001589 carboacyl group Chemical group 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 4
- 206010006895 Cachexia Diseases 0.000 claims 3
- 208000002249 Diabetes Complications Diseases 0.000 claims 3
- 206010012655 Diabetic complications Diseases 0.000 claims 3
- 208000032928 Dyslipidaemia Diseases 0.000 claims 3
- 208000030814 Eating disease Diseases 0.000 claims 3
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 3
- 206010020772 Hypertension Diseases 0.000 claims 3
- 201000001431 Hyperuricemia Diseases 0.000 claims 3
- 102000016267 Leptin Human genes 0.000 claims 3
- 108010092277 Leptin Proteins 0.000 claims 3
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 3
- 206010033307 Overweight Diseases 0.000 claims 3
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 3
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 3
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 3
- 235000014632 disordered eating Nutrition 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 230000005764 inhibitory process Effects 0.000 claims 3
- NRYBAZVQPHGZNS-ZSOCWYAHSA-N leptin Chemical compound O=C([C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(C)C)CCSC)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CS)C(O)=O NRYBAZVQPHGZNS-ZSOCWYAHSA-N 0.000 claims 3
- 229940039781 leptin Drugs 0.000 claims 3
- 239000003446 ligand Substances 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 201000005665 thrombophilia Diseases 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 claims 2
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 2
- IGERFAHWSHDDHX-UHFFFAOYSA-N 1,3-dioxanyl Chemical group [CH]1OCCCO1 IGERFAHWSHDDHX-UHFFFAOYSA-N 0.000 claims 2
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000003542 3-methylbutan-2-yl group Chemical group [H]C([H])([H])C([H])(*)C([H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 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 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical group CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims 2
- 125000005278 alkyl sulfonyloxy group Chemical group 0.000 claims 2
- 125000001769 aryl amino group Chemical group 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 208000019425 cirrhosis of liver Diseases 0.000 claims 2
- 125000006622 cycloheptylmethyl group Chemical group 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 claims 2
- 125000003566 oxetanyl group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 2
- 125000006513 pyridinyl methyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims 1
- 125000000530 1-propynyl group Chemical group [H]C([H])([H])C#C* 0.000 claims 1
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 claims 1
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims 1
- 229940123208 Biguanide Drugs 0.000 claims 1
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 1
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 102100025101 GATA-type zinc finger protein 1 Human genes 0.000 claims 1
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 101000684208 Homo sapiens Prolyl endopeptidase FAP Proteins 0.000 claims 1
- 229940122199 Insulin secretagogue Drugs 0.000 claims 1
- 229940122355 Insulin sensitizer Drugs 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 claims 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 claims 1
- 102000018692 Sulfonylurea Receptors Human genes 0.000 claims 1
- 108010091821 Sulfonylurea Receptors Proteins 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 229960001138 acetylsalicylic acid Drugs 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 125000005153 alkyl sulfamoyl group Chemical group 0.000 claims 1
- 125000005422 alkyl sulfonamido group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000005281 alkyl ureido group Chemical group 0.000 claims 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000005605 benzo group Chemical group 0.000 claims 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 1
- 230000037396 body weight Effects 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 201000003278 cryoglobulinemia Diseases 0.000 claims 1
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 229940125753 fibrate Drugs 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 125000003104 hexanoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 150000002440 hydroxy compounds Chemical class 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000004026 insulin derivative Substances 0.000 claims 1
- 230000002473 insulinotropic effect Effects 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000005929 isobutyloxycarbonyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])OC(*)=O 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 229960003512 nicotinic acid Drugs 0.000 claims 1
- 235000001968 nicotinic acid Nutrition 0.000 claims 1
- 239000011664 nicotinic acid Substances 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000006514 pyridin-2-ylmethyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000002112 pyrrolidino group Chemical group [*]N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004550 quinolin-6-yl group Chemical group N1=CC=CC2=CC(=CC=C12)* 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 150000003254 radicals Chemical class 0.000 claims 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 239000004059 squalene synthase inhibitor Substances 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 description 3
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36882010P | 2010-07-29 | 2010-07-29 | |
| US61/368,820 | 2010-07-29 | ||
| PCT/EP2011/062933 WO2012013716A1 (en) | 2010-07-29 | 2011-07-27 | Bicyclic acetyl-coa carboxylase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013533279A JP2013533279A (ja) | 2013-08-22 |
| JP2013533279A5 true JP2013533279A5 (OSRAM) | 2014-08-28 |
| JP5998133B2 JP5998133B2 (ja) | 2016-09-28 |
Family
ID=44532808
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013521136A Expired - Fee Related JP5998133B2 (ja) | 2010-07-29 | 2011-07-27 | 二環式アセチル−coaカルボキシラーゼ阻害剤およびそれらの使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US8697739B2 (OSRAM) |
| EP (1) | EP2598486B1 (OSRAM) |
| JP (1) | JP5998133B2 (OSRAM) |
| CN (1) | CN103339111B (OSRAM) |
| AR (1) | AR082391A1 (OSRAM) |
| ES (1) | ES2641833T3 (OSRAM) |
| TW (1) | TW201206907A (OSRAM) |
| UY (1) | UY33536A (OSRAM) |
| WO (1) | WO2012013716A1 (OSRAM) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101218226A (zh) * | 2005-05-16 | 2008-07-09 | 沃泰克斯药物股份有限公司 | 作为离子通道调控剂的二环衍生物 |
| WO2012124744A1 (ja) * | 2011-03-14 | 2012-09-20 | 大正製薬株式会社 | 含窒素縮合複素環化合物 |
| JPWO2013061962A1 (ja) | 2011-10-24 | 2015-04-02 | 武田薬品工業株式会社 | 二環性化合物 |
| HK1221420A1 (zh) | 2013-05-10 | 2017-06-02 | Gilead Apollo, Inc. | Acc抑制剂和其用途 |
| JP6434498B2 (ja) * | 2013-05-10 | 2018-12-05 | ギリアド アポロ, エルエルシー | Acc阻害剤及びその使用 |
| WO2015036892A1 (en) | 2013-09-12 | 2015-03-19 | Pfizer Inc. | Use of acetyl-coa carboxylase inhibitors for treating acne vulgaris |
| MA41179A (fr) | 2014-12-19 | 2017-10-24 | Cancer Research Tech Ltd | Composés inhibiteurs de parg |
| WO2016126973A1 (en) * | 2015-02-05 | 2016-08-11 | Dermira Inc. | Synthetic process for preparing 2-((2-ethoxy-2-oxoethyl)(methyl)amino)-2-oxoethyl 5-tetradecyloxy)furan-2-carboxylate |
| EP3287441B1 (en) | 2015-04-20 | 2021-06-09 | Takeda Pharmaceutical Company Limited | Acylated 4-aminopiperidines as inhibitors of serine palmitoyltransferase |
| PL3330259T3 (pl) | 2015-07-27 | 2021-02-08 | Chong Kun Dang Pharmaceutical Corp. | Związek pochodna amidowa 1,3,4-oksadiazolu jako inhibitor deacetylazy histonowej 6 i kompozycja farmaceutyczna go zawierająca |
| KR101799005B1 (ko) | 2015-07-27 | 2017-11-17 | 주식회사 종근당 | 히스톤 탈아세틸화효소 6 억제제로서의 1,3,4-옥사다이아졸 설프아마이드 유도체 화합물 및 이를 포함하는 약제학적 조성물 |
| NZ739026A (en) | 2015-07-27 | 2019-03-29 | Chong Kun Dang Pharmaceutical Corp | 1,3,4-oxadiazole sulfonamide derivative compounds as histone deacetylase 6 inhibitor, and the pharmaceutical composition comprising the same |
| BR112018002304B1 (pt) | 2015-08-04 | 2023-12-19 | Chong Kun Dang Pharmaceutical Corp | Compostos de derivado de 1,3,4-oxadiazol como inibidor de histona desacetilase 6 e a composição farmacêutica que compreende os mesmos |
| CN105130893B (zh) * | 2015-09-08 | 2018-04-10 | 大连理工大学 | 一种1‑苄基‑6‑甲氧羰甲基四氢异喹啉衍生物、制备方法及其抗血小板聚集的应用 |
| WO2017065473A1 (en) | 2015-10-12 | 2017-04-20 | Chong Kun Dang Pharmaceutical Corp. | Oxadiazole amine derivative compounds as histone deacetylase 6 inhibitor, and the pharmaceutical composition comprising the same |
| US20170266157A1 (en) * | 2016-03-21 | 2017-09-21 | David Weinstein | Methods for wound healing and scar prevention |
| US10653678B2 (en) | 2016-04-11 | 2020-05-19 | Genfit | Methods of treatment for cholestatic and fibrotic diseases |
| ES2839453T3 (es) | 2016-04-11 | 2021-07-05 | Genfit | Métodos para el tratamiento de enfermedades colestásicas y fibróticas |
| JP6921100B2 (ja) | 2016-10-18 | 2021-08-18 | 武田薬品工業株式会社 | 複素環化合物 |
| US11572347B2 (en) | 2017-10-20 | 2023-02-07 | The Regents Of The University Of California | Orally available sEH/PDE4 dual inhibitors |
| CA3079819C (en) | 2017-11-06 | 2023-03-14 | Acelot, Inc. | Small molecule drugs and related methods for treatment of diseases related to a.beta.42 oligomer formation |
| CN110041253B (zh) * | 2018-01-17 | 2022-03-29 | 上海翰森生物医药科技有限公司 | 吡啶类n-氧化衍生物及其制备方法和应用 |
| KR102316234B1 (ko) | 2018-07-26 | 2021-10-22 | 주식회사 종근당 | 히스톤 탈아세틸화효소 6 억제제로서의 1,3,4-옥사다이아졸 유도체 화합물 및 이를 포함하는 약제학적 조성물 |
| CA3112414A1 (en) * | 2018-09-18 | 2020-03-26 | Metacrine, Inc. | Farnesoid x receptor agonists for the treatment of disease |
| WO2020097398A1 (en) | 2018-11-07 | 2020-05-14 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| WO2020198478A1 (en) | 2019-03-28 | 2020-10-01 | Zoetis Services Llc | Serotonin 5-ht2b inhibitory compounds |
| CN109836385B (zh) * | 2019-04-04 | 2021-12-17 | 上海翰森生物医药科技有限公司 | 四氢喹啉类n-氧化衍生物及其制备方法和应用 |
| MX2021014315A (es) | 2019-05-31 | 2022-01-04 | Chong Kun Dang Pharmaceutical Corp | Compuestos derivados de 1,3,4-oxadiazol homoftalimida como inhibidores de histona desacetilasa 6, y la composicion farmaceutica que comprende los mismos. |
| WO2021087077A1 (en) * | 2019-10-29 | 2021-05-06 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of autophagy and histone deactylases and uses thereof |
| CA3181537A1 (en) | 2020-05-06 | 2021-11-11 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| CN112370455A (zh) * | 2020-10-19 | 2021-02-19 | 济南大学 | 一种磺酰胺衍生物作为α-葡萄糖苷酶抑制剂及其应用 |
| CN117321048A (zh) * | 2020-12-16 | 2023-12-29 | 艾福姆德尤股份有限公司 | 用于治疗与sting活性有关的疾病的化合物和组合物 |
| WO2022140527A1 (en) | 2020-12-23 | 2022-06-30 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| TW202325289A (zh) | 2021-11-09 | 2023-07-01 | 美商雅捷可斯治療公司 | Jak2抑制劑之形式及組合物 |
| TW202334139A (zh) | 2021-11-09 | 2023-09-01 | 美商雅捷可斯治療公司 | 作為jak2抑制劑之6-雜芳氧基苯并咪唑及氮雜苯并咪唑 |
| CN116354903B (zh) * | 2021-12-28 | 2025-09-09 | 南京药石科技股份有限公司 | 一种6-苯并噻唑磺酰氯的制备方法 |
| CN116966185A (zh) * | 2022-03-02 | 2023-10-31 | 中南大学湘雅三医院 | 特拉匹韦在制备malt1抑制剂、抗malt1依赖性肿瘤的药物中的应用及抗肿瘤药物 |
| TW202345809A (zh) | 2022-03-23 | 2023-12-01 | 美商愛德亞生物科學公司 | 作為parg抑制劑之經哌取代的吲唑化合物 |
Family Cites Families (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB284425A (en) | 1926-11-22 | 1928-02-02 | James Last | Improvements in and relating to sand or like moulds for making castings |
| JPS5612114B2 (OSRAM) | 1974-06-07 | 1981-03-18 | ||
| US4231938A (en) | 1979-06-15 | 1980-11-04 | Merck & Co., Inc. | Hypocholesteremic fermentation products and process of preparation |
| DK149080C (da) | 1980-06-06 | 1986-07-28 | Sankyo Co | Fremgangsmaade til fremstilling af derivater af ml-236b-carboxylsyre |
| US4450171A (en) | 1980-08-05 | 1984-05-22 | Merck & Co., Inc. | Antihypercholesterolemic compounds |
| US4448784A (en) | 1982-04-12 | 1984-05-15 | Hoechst-Roussel Pharmaceuticals, Inc. | 1-(Aminoalkylphenyl and aminoalkylbenzyl)-indoles and indolines and analgesic method of use thereof |
| US4499289A (en) | 1982-12-03 | 1985-02-12 | G. D. Searle & Co. | Octahydronapthalenes |
| CA1327360C (en) | 1983-11-14 | 1994-03-01 | William F. Hoffman | Oxo-analogs of mevinolin-like antihypercholesterolemic agents |
| US4613610A (en) | 1984-06-22 | 1986-09-23 | Sandoz Pharmaceuticals Corp. | Cholesterol biosynthesis inhibiting pyrazole analogs of mevalonolactone and its derivatives |
| US4686237A (en) | 1984-07-24 | 1987-08-11 | Sandoz Pharmaceuticals Corp. | Erythro-(E)-7-[3'-C1-3 alkyl-1'-(3",5"-dimethylphenyl)naphth-2'-yl]-3,5-dihydroxyhept-6-enoic acids and derivatives thereof |
| US4647576A (en) | 1984-09-24 | 1987-03-03 | Warner-Lambert Company | Trans-6-[2-(substitutedpyrrol-1-yl)alkyl]-pyran-2-one inhibitors of cholesterol synthesis |
| ATE60571T1 (de) | 1984-12-04 | 1991-02-15 | Sandoz Ag | Inden-analoga von mevalonolakton und ihre derivate. |
| US4668794A (en) | 1985-05-22 | 1987-05-26 | Sandoz Pharm. Corp. | Intermediate imidazole acrolein analogs |
| WO1987002662A2 (en) | 1985-10-25 | 1987-05-07 | Sandoz Ag | Heterocyclic analogs of mevalonolactone and derivatives thereof, processes for their production and their use as pharmaceuticals |
| FR2596393B1 (fr) | 1986-04-01 | 1988-06-03 | Sanofi Sa | Derives de l'acide hydroxy-3 dihydroxyoxophosphorio-4 butanoique, leur procede de preparation, leur application comme medicament et les compositions les renfermant |
| IL86464A (en) | 1987-05-22 | 1993-06-10 | Squibb & Sons Inc | 4-phosphinyl-3- hydroxybutanoic acid derivatives useful as cholesterol biosynthesis inhibitors and pharmaceutical compositions containing the same |
| US5506219A (en) | 1988-08-29 | 1996-04-09 | E. R. Squibb & Sons, Inc. | Pyridine anchors for HMG-CoA reductase inhibitors |
| US5753675A (en) | 1989-03-03 | 1998-05-19 | Novartis Pharmaceuticals Corporation | Quinoline analogs of mevalonolactone and derivatives thereof |
| HUT64023A (en) | 1991-03-22 | 1993-11-29 | Sandoz Ag | Process for producing aminoguanidine derivatives and pharmaceutical compositions comprising such compounds |
| TW225528B (OSRAM) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| 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 |
| 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 |
| JP3216457B2 (ja) * | 1994-12-28 | 2001-10-09 | 富士レビオ株式会社 | アミド誘導体 |
| CA2240024A1 (en) | 1995-12-13 | 1997-06-19 | The Regents Of The University Of California | Nuclear receptor ligands and ligand binding domains |
| US5770615A (en) | 1996-04-04 | 1998-06-23 | Bristol-Myers Squibb Company | Catecholamine surrogates useful as β3 agonists |
| GB9713739D0 (en) | 1997-06-27 | 1997-09-03 | Karobio Ab | Thyroid receptor ligands |
| KR20010083092A (ko) | 1998-07-06 | 2001-08-31 | 스티븐 비. 데이비스 | 이중 안지오텐신 엔도텔린 수용체 길항제로서의 비페닐술폰아미드 |
| CO5150173A1 (es) | 1998-12-10 | 2002-04-29 | Novartis Ag | Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv |
| DE10139416A1 (de) * | 2001-08-17 | 2003-03-06 | Aventis Pharma Gmbh | Aminoalkyl substituierte aromatische Bicyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| TW200303742A (en) | 2001-11-21 | 2003-09-16 | Novartis Ag | Organic compounds |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| US20050069522A1 (en) | 2002-08-12 | 2005-03-31 | Richard Colonno | Combination pharmaceutical agents as inhibitors of HCV replication |
| CN1753897A (zh) | 2002-11-22 | 2006-03-29 | 日本烟草产业株式会社 | 稠合双环含氮杂环 |
| US20040185559A1 (en) | 2003-03-21 | 2004-09-23 | Isis Pharmaceuticals Inc. | Modulation of diacylglycerol acyltransferase 1 expression |
| EP2316827B1 (en) | 2003-07-30 | 2016-01-27 | Xenon Pharmaceuticals Inc. | Piperazine derivatives and their use as therapeutic agents |
| US7300932B2 (en) | 2003-08-07 | 2007-11-27 | Japan Tobacco Inc. | Pyrrolo[1,2-b]pyridazine derivatives |
| GB0325192D0 (en) | 2003-10-29 | 2003-12-03 | Astrazeneca Ab | Method of use |
| WO2005108370A1 (ja) * | 2004-04-16 | 2005-11-17 | Ajinomoto Co., Inc. | ベンゼン化合物 |
| US20080261952A1 (en) * | 2004-08-16 | 2008-10-23 | Jason Bloxham | Aryl Urea Derivatives for Treating Obesity |
| AR051596A1 (es) | 2004-10-26 | 2007-01-24 | Irm Llc | Compuestos heterociclicos condensados nitrogenados como inhibidores de la actividad del receptor canabinoide 1; composiciones farmaceuticas que los contienen y su empleo en la preparacion de medicamentos para el tratamiento de trastornos alimentarios |
| EP2009011A1 (en) * | 2006-04-14 | 2008-12-31 | Takeda Pharmaceutical Company Limited | Nitrogen-containing heterocyclic compound |
| US20090197916A1 (en) | 2007-01-29 | 2009-08-06 | Arete Therapeutics, Inc | Soluble epoxide hydrolase inhibitors for treatment of metabolic syndrome and related disorders |
| US20090005375A1 (en) * | 2007-03-30 | 2009-01-01 | Edcon Chang | Acetyl coenzyme a carboxylase inhibitors |
| PE20091309A1 (es) | 2007-12-21 | 2009-09-30 | Astrazeneca Ab | Derivados de ciclohexilo como inhibidores de acetil coenzima a carboxilasa |
| JP2009173567A (ja) * | 2008-01-23 | 2009-08-06 | Lion Corp | Ppar抑制剤並びに骨形成促進剤及び骨粗鬆症の治療薬 |
| WO2010065799A2 (en) | 2008-12-04 | 2010-06-10 | Palatin Technologies, Inc. | Amine substituted piperidine melanocortin receptor-specific compounds |
| WO2010065801A1 (en) | 2008-12-04 | 2010-06-10 | Palatin Technologies, Inc. | Amine substituted piperazine melanocortin receptor-specific compounds |
| WO2010065802A2 (en) | 2008-12-04 | 2010-06-10 | Palatin Technologies, Inc. | Substituted pyrrolidine or imidazolidine melanocortin receptor-specific compounds |
| WO2010065800A1 (en) | 2008-12-04 | 2010-06-10 | Palatin Technologies, Inc. | Hydrazine substituted piperidine melanocortin receptor-specific compounds |
| KR20110135972A (ko) | 2009-03-19 | 2011-12-20 | 시오노기세이야쿠가부시키가이샤 | Npy y5 수용체 길항제를 함유하는 고형 제제 |
| WO2011039735A2 (en) | 2009-10-02 | 2011-04-07 | Consiglio Nazionale Delle Ricerche | Compounds with ddx3 inhibitory activity and uses thereof |
-
2011
- 2011-07-25 US US13/189,760 patent/US8697739B2/en not_active Expired - Fee Related
- 2011-07-27 EP EP11741554.7A patent/EP2598486B1/en not_active Not-in-force
- 2011-07-27 CN CN201180035809.2A patent/CN103339111B/zh not_active Expired - Fee Related
- 2011-07-27 ES ES11741554.7T patent/ES2641833T3/es active Active
- 2011-07-27 JP JP2013521136A patent/JP5998133B2/ja not_active Expired - Fee Related
- 2011-07-27 WO PCT/EP2011/062933 patent/WO2012013716A1/en not_active Ceased
- 2011-07-27 AR ARP110102709A patent/AR082391A1/es unknown
- 2011-07-28 UY UY0001033536A patent/UY33536A/es not_active Application Discontinuation
- 2011-07-28 TW TW100126860A patent/TW201206907A/zh unknown
-
2014
- 2014-02-24 US US14/188,647 patent/US9789118B2/en not_active Expired - Fee Related
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