JP2016520065A5 - - Google Patents
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- JP2016520065A5 JP2016520065A5 JP2016513086A JP2016513086A JP2016520065A5 JP 2016520065 A5 JP2016520065 A5 JP 2016520065A5 JP 2016513086 A JP2016513086 A JP 2016513086A JP 2016513086 A JP2016513086 A JP 2016513086A JP 2016520065 A5 JP2016520065 A5 JP 2016520065A5
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- Prior art keywords
- membered
- sulfur
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- oxygen
- nitrogen
- Prior art date
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 31
- 229910052757 nitrogen Inorganic materials 0.000 claims description 26
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 22
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 22
- 229910052760 oxygen Inorganic materials 0.000 claims description 22
- 239000001301 oxygen Substances 0.000 claims description 22
- 229910052717 sulfur Inorganic materials 0.000 claims description 22
- 239000011593 sulfur Substances 0.000 claims description 22
- 150000001875 compounds Chemical class 0.000 claims description 20
- 125000005842 heteroatom Chemical group 0.000 claims description 19
- 239000000203 mixture Substances 0.000 claims description 19
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 13
- 229920006395 saturated elastomer Polymers 0.000 claims description 13
- 229910052739 hydrogen Inorganic materials 0.000 claims description 12
- 239000001257 hydrogen Substances 0.000 claims description 12
- 229910052736 halogen Inorganic materials 0.000 claims description 11
- 150000002367 halogens Chemical class 0.000 claims description 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 9
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims description 7
- 150000003839 salts Chemical class 0.000 claims description 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- 208000008589 Obesity Diseases 0.000 claims description 6
- 150000002431 hydrogen Chemical class 0.000 claims description 6
- 208000030159 metabolic disease Diseases 0.000 claims description 6
- 235000020824 obesity Nutrition 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 5
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 4
- 125000001931 aliphatic group Chemical group 0.000 claims description 4
- 125000002619 bicyclic group Chemical group 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 229910052805 deuterium Inorganic materials 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 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 4
- 125000001620 monocyclic carbocycle group Chemical group 0.000 claims description 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 3
- 125000004429 atom Chemical group 0.000 claims description 3
- 239000012472 biological sample Substances 0.000 claims description 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 3
- 208000035143 Bacterial infection Diseases 0.000 claims description 2
- 208000008020 Cohen syndrome Diseases 0.000 claims description 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 2
- 206010017533 Fungal infection Diseases 0.000 claims description 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims description 2
- 102000004877 Insulin Human genes 0.000 claims description 2
- 108090001061 Insulin Proteins 0.000 claims description 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 2
- 208000012708 MOMO syndrome Diseases 0.000 claims description 2
- 208000031888 Mycoses Diseases 0.000 claims description 2
- 208000030852 Parasitic disease Diseases 0.000 claims description 2
- CXOFVDLJLONNDW-UHFFFAOYSA-N Phenytoin Chemical compound N1C(=O)NC(=O)C1(C=1C=CC=CC=1)C1=CC=CC=C1 CXOFVDLJLONNDW-UHFFFAOYSA-N 0.000 claims description 2
- 201000010769 Prader-Willi syndrome Diseases 0.000 claims description 2
- 229940100389 Sulfonylurea Drugs 0.000 claims description 2
- 229940123464 Thiazolidinedione Drugs 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 229940125681 anticonvulsant agent Drugs 0.000 claims description 2
- 239000001961 anticonvulsive agent Substances 0.000 claims description 2
- 239000000935 antidepressant agent Substances 0.000 claims description 2
- 229940005513 antidepressants Drugs 0.000 claims description 2
- 239000000164 antipsychotic agent Substances 0.000 claims description 2
- 229940005529 antipsychotics Drugs 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 208000022362 bacterial infectious disease Diseases 0.000 claims description 2
- 125000005605 benzo group Chemical group 0.000 claims description 2
- 229940124558 contraceptive agent Drugs 0.000 claims description 2
- 239000003433 contraceptive agent Substances 0.000 claims description 2
- 125000001047 cyclobutenyl group Chemical group C1(=CCC1)* 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 230000003054 hormonal effect Effects 0.000 claims description 2
- 229940125396 insulin Drugs 0.000 claims description 2
- 125000003566 oxetanyl group Chemical group 0.000 claims description 2
- 229960002036 phenytoin Drugs 0.000 claims description 2
- FIADGNVRKBPQEU-UHFFFAOYSA-N pizotifen Chemical compound C1CN(C)CCC1=C1C2=CC=CC=C2CCC2=C1C=CS2 FIADGNVRKBPQEU-UHFFFAOYSA-N 0.000 claims description 2
- 229960004572 pizotifen Drugs 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- AEQFSUDEHCCHBT-UHFFFAOYSA-M sodium valproate Chemical compound [Na+].CCCC(C([O-])=O)CCC AEQFSUDEHCCHBT-UHFFFAOYSA-M 0.000 claims description 2
- 150000003431 steroids Chemical class 0.000 claims description 2
- 208000024891 symptom Diseases 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 150000001467 thiazolidinediones Chemical class 0.000 claims description 2
- 229940102566 valproate Drugs 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 102000000452 Acetyl-CoA carboxylase Human genes 0.000 claims 1
- 108010016219 Acetyl-CoA carboxylase Proteins 0.000 claims 1
- 108010018763 Biotin carboxylase Proteins 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 10
- 125000001183 hydrocarbyl group Chemical group 0.000 description 2
- KDLCGRKHKVMFHR-DEOSSOPVSA-N CC(C)(C(N)=O)N(C(c(cc(cc1)-c2ncc[o]2)c1N1C[C@@H](c2cc(F)ccc2OC)OC2CCOCC2)=O)C1=O Chemical compound CC(C)(C(N)=O)N(C(c(cc(cc1)-c2ncc[o]2)c1N1C[C@@H](c2cc(F)ccc2OC)OC2CCOCC2)=O)C1=O KDLCGRKHKVMFHR-DEOSSOPVSA-N 0.000 description 1
- IVABDSKSJOSSRT-DEOSSOPVSA-N CC(C)(C(O)=O)N(C(c(cc(cc1)-c2ncc[o]2)c1N1C[C@@H](c2cc(F)ccc2OC)OC2CCOCC2)=O)C1=O Chemical compound CC(C)(C(O)=O)N(C(c(cc(cc1)-c2ncc[o]2)c1N1C[C@@H](c2cc(F)ccc2OC)OC2CCOCC2)=O)C1=O IVABDSKSJOSSRT-DEOSSOPVSA-N 0.000 description 1
- RHVOBHXRHOANLT-QFIPXVFZSA-N CC(C)(C(O)=O)N(C(c(cc(cc1)Br)c1N1C[C@@H](c2cc(F)ccc2OC)OC2CCOCC2)=O)C1=O Chemical compound CC(C)(C(O)=O)N(C(c(cc(cc1)Br)c1N1C[C@@H](c2cc(F)ccc2OC)OC2CCOCC2)=O)C1=O RHVOBHXRHOANLT-QFIPXVFZSA-N 0.000 description 1
- SOEUICFXQSKRNO-UHFFFAOYSA-N CC(C)(C(O)=O)N(C(c1nc(C(F)(F)F)ccc1N1CC(/C=[O]/C2CCOCC2)c2ccccc2OC)=O)C1=O Chemical compound CC(C)(C(O)=O)N(C(c1nc(C(F)(F)F)ccc1N1CC(/C=[O]/C2CCOCC2)c2ccccc2OC)=O)C1=O SOEUICFXQSKRNO-UHFFFAOYSA-N 0.000 description 1
- QPRWHLAQHYQMQZ-UHFFFAOYSA-N CC(C)(C(O)=O)N(C(c1nc(C2CCC2)ccc1N1CC(/C=[O]/C2CCOCC2)c2ccccc2OC)=O)C1=O Chemical compound CC(C)(C(O)=O)N(C(c1nc(C2CCC2)ccc1N1CC(/C=[O]/C2CCOCC2)c2ccccc2OC)=O)C1=O QPRWHLAQHYQMQZ-UHFFFAOYSA-N 0.000 description 1
- PYXUHQFFTOKVQG-UHFFFAOYSA-N CC(C)/[O]=C(/CN(c(ccc(-c1ncc[o]1)c1)c1C(N1C(C)(C)C(O)=O)=O)C1=O)\c1ccccc1OC Chemical compound CC(C)/[O]=C(/CN(c(ccc(-c1ncc[o]1)c1)c1C(N1C(C)(C)C(O)=O)=O)C1=O)\c1ccccc1OC PYXUHQFFTOKVQG-UHFFFAOYSA-N 0.000 description 1
- FEABGNJLMRLXKO-UHFFFAOYSA-N COc1ccccc1CCN(c(cc1)c(C(N2CC(O)=O)=S)nc1-c1ncc[o]1)C2=S Chemical compound COc1ccccc1CCN(c(cc1)c(C(N2CC(O)=O)=S)nc1-c1ncc[o]1)C2=S FEABGNJLMRLXKO-UHFFFAOYSA-N 0.000 description 1
- UCRIFBCDWXVRAR-UHFFFAOYSA-N COc1ccccc1CCN(c(cc1)c(C(N2CCc3ncc[o]3)=O)nc1-c1ncc[o]1)C2=O Chemical compound COc1ccccc1CCN(c(cc1)c(C(N2CCc3ncc[o]3)=O)nc1-c1ncc[o]1)C2=O UCRIFBCDWXVRAR-UHFFFAOYSA-N 0.000 description 1
- QDKRWQAYFXFZNL-UHFFFAOYSA-N COc1ccccc1CCN(c1c(C(N2CC(O)=O)=O)nc(-c3ncc[o]3)nn1)C2=O Chemical compound COc1ccccc1CCN(c1c(C(N2CC(O)=O)=O)nc(-c3ncc[o]3)nn1)C2=O QDKRWQAYFXFZNL-UHFFFAOYSA-N 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 229940121373 acetyl-coa carboxylase inhibitor Drugs 0.000 description 1
- 230000002293 adipogenic effect Effects 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361821831P | 2013-05-10 | 2013-05-10 | |
| US61/821,831 | 2013-05-10 | ||
| PCT/US2014/037370 WO2014182951A1 (en) | 2013-05-10 | 2014-05-08 | Acc inhibitors and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016520065A JP2016520065A (ja) | 2016-07-11 |
| JP2016520065A5 true JP2016520065A5 (cg-RX-API-DMAC7.html) | 2017-07-06 |
| JP6417403B2 JP6417403B2 (ja) | 2018-11-07 |
Family
ID=51867755
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016513086A Active JP6417403B2 (ja) | 2013-05-10 | 2014-05-08 | Ａｃｃ阻害剤及びその使用 |
Country Status (14)
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9988399B2 (en) | 2013-05-10 | 2018-06-05 | Gilead Apollo, Llc | Bicyclic compounds as ACC inhibitors and uses thereof |
| HK1221660A1 (zh) | 2013-05-10 | 2017-06-09 | Gilead Apollo, Llc | Acc抑制剂和其用途 |
| WO2014182945A1 (en) | 2013-05-10 | 2014-11-13 | Nimbus Apollo, Inc. | Acc inhibitors and uses thereof |
| JPWO2015056782A1 (ja) | 2013-10-17 | 2017-03-09 | 塩野義製薬株式会社 | 新規アルキレン誘導体 |
| CN107106873A (zh) | 2015-01-09 | 2017-08-29 | 吉利德阿波罗公司 | 用于治疗非酒精性脂肪肝病的acc抑制剂组合治疗 |
| AR106472A1 (es) | 2015-10-26 | 2018-01-17 | Gilead Apollo Llc | Inhibidores de acc y usos de los mismos |
| WO2017091617A1 (en) | 2015-11-25 | 2017-06-01 | Gilead Apollo, Llc | Triazole acc inhibitors and uses thereof |
| HUE053175T2 (hu) | 2015-11-25 | 2021-06-28 | Gilead Apollo Llc | ACC-gátló észterek és azok alkalmazása |
| MX2018006285A (es) | 2015-11-25 | 2018-09-07 | Gilead Apollo Llc | Composiciones fungicidas que contienen derivados de 2,4-dioxido-1,4-dihidrotieno[2,3-d] pirimidina. |
| KR20180082556A (ko) * | 2015-11-25 | 2018-07-18 | 길리어드 아폴로, 엘엘씨 | 피라졸 acc 억제제 및 그의 용도 |
| AU2018209006B2 (en) | 2017-01-22 | 2021-04-22 | Sunshine Lake Pharma Co., Ltd. | Thienopyrimidine derivative and use thereof in medicine |
| US10995099B2 (en) * | 2017-07-17 | 2021-05-04 | Nanjing Ruijie Pharmatech Co., Ltd. | Compounds and their uses as ACC inhibitors |
| KR20190036705A (ko) | 2017-09-28 | 2019-04-05 | 한미약품 주식회사 | (2r)-2-(2-메톡시페닐)-2-(옥산-4-일옥시)에탄-1-올 화합물의 신규 제조방법 및 이에 사용되는 중간체 |
| CN110950884B (zh) * | 2018-09-27 | 2024-03-26 | 上海翰森生物医药科技有限公司 | 含二并环类衍生物抑制剂、其制备方法和应用 |
| CN110343650B (zh) * | 2019-05-28 | 2020-12-29 | 浙江工业大学 | 一种产两性霉素b的重组结节链霉菌及其应用 |
| JP7374233B2 (ja) | 2019-07-02 | 2023-11-06 | ▲広▼▲東▼▲東▼▲陽▼光▲薬▼▲業▼有限公司 | 立体配置を有するチエノピリミジン誘導体及び薬物におけるその応用 |
| AR119594A1 (es) | 2019-08-09 | 2021-12-29 | Gilead Sciences Inc | Derivados de tienopirimidina como inhibidores acc y usos de los mismos |
| US11478533B2 (en) | 2020-04-27 | 2022-10-25 | Novo Nordisk A/S | Semaglutide for use in medicine |
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| FR2985185B1 (fr) * | 2012-01-04 | 2013-12-27 | Sanofi Sa | Utilisation en therapeutique de derives d'imidazopyridine |
| WO2014182945A1 (en) | 2013-05-10 | 2014-11-13 | Nimbus Apollo, Inc. | Acc inhibitors and uses thereof |
| US9988399B2 (en) | 2013-05-10 | 2018-06-05 | Gilead Apollo, Llc | Bicyclic compounds as ACC inhibitors and uses thereof |
| HK1221660A1 (zh) | 2013-05-10 | 2017-06-09 | Gilead Apollo, Llc | Acc抑制剂和其用途 |
-
2014
- 2014-05-08 CA CA2911822A patent/CA2911822A1/en not_active Abandoned
- 2014-05-08 HK HK16109662.0A patent/HK1221420A1/zh unknown
- 2014-05-08 CN CN201480036146.XA patent/CN105358155A/zh active Pending
- 2014-05-08 KR KR1020157035038A patent/KR20160005365A/ko not_active Withdrawn
- 2014-05-08 US US14/890,358 patent/US10208044B2/en active Active
- 2014-05-08 MX MX2015015416A patent/MX2015015416A/es unknown
- 2014-05-08 HK HK16109920.8A patent/HK1221662A1/zh unknown
- 2014-05-08 EA EA201591962A patent/EA201591962A1/ru unknown
- 2014-05-08 WO PCT/US2014/037370 patent/WO2014182951A1/en not_active Ceased
- 2014-05-08 EP EP14795147.9A patent/EP2994141A4/en not_active Withdrawn
- 2014-05-08 AU AU2014262547A patent/AU2014262547A1/en not_active Abandoned
- 2014-05-08 BR BR112015028214A patent/BR112015028214A2/pt not_active Application Discontinuation
- 2014-05-08 JP JP2016513086A patent/JP6417403B2/ja active Active
-
2015
- 2015-11-10 CL CL2015003317A patent/CL2015003317A1/es unknown
- 2015-11-12 ZA ZA2015/08355A patent/ZA201508355B/en unknown
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