JP2016526024A5 - - Google Patents
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- Publication number
- JP2016526024A5 JP2016526024A5 JP2016513082A JP2016513082A JP2016526024A5 JP 2016526024 A5 JP2016526024 A5 JP 2016526024A5 JP 2016513082 A JP2016513082 A JP 2016513082A JP 2016513082 A JP2016513082 A JP 2016513082A JP 2016526024 A5 JP2016526024 A5 JP 2016526024A5
- Authority
- JP
- Japan
- Prior art keywords
- sulfur
- oxygen
- nitrogen
- membered
- compound
- 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
Links
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 29
- 229910052757 nitrogen Inorganic materials 0.000 claims description 24
- 229910052760 oxygen Inorganic materials 0.000 claims description 24
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 23
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 23
- 239000001301 oxygen Substances 0.000 claims description 23
- 229910052717 sulfur Chemical group 0.000 claims description 23
- 239000011593 sulfur Chemical group 0.000 claims description 22
- 150000001875 compounds Chemical class 0.000 claims description 20
- 125000005842 heteroatom Chemical group 0.000 claims description 18
- 239000000203 mixture Substances 0.000 claims description 18
- 229920006395 saturated elastomer Polymers 0.000 claims description 14
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 13
- 229910052736 halogen Inorganic materials 0.000 claims description 12
- 150000002367 halogens Chemical class 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 9
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 239000001257 hydrogen Substances 0.000 claims description 8
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims description 7
- 150000003839 salts Chemical class 0.000 claims description 7
- 208000008589 Obesity Diseases 0.000 claims description 6
- 230000002401 inhibitory effect Effects 0.000 claims description 6
- 208000030159 metabolic disease Diseases 0.000 claims description 6
- 125000001620 monocyclic carbocycle group Chemical group 0.000 claims description 6
- 235000020824 obesity Nutrition 0.000 claims description 6
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- 125000001931 aliphatic group Chemical group 0.000 claims description 4
- 229910052805 deuterium Inorganic materials 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 150000002431 hydrogen Chemical class 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
- 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
- 125000001072 heteroaryl group Chemical group 0.000 claims description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 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
- 208000022362 bacterial infectious disease Diseases 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
- 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
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 description 10
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 description 2
- 229910052799 carbon Inorganic materials 0.000 description 2
- 125000001183 hydrocarbyl group Chemical group 0.000 description 2
- 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
- 125000003118 aryl group Chemical group 0.000 description 1
- 125000005605 benzo group Chemical group 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 125000002619 bicyclic 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 |
|---|---|---|---|
| US201361821824P | 2013-05-10 | 2013-05-10 | |
| US61/821,824 | 2013-05-10 | ||
| PCT/US2014/037360 WO2014182943A1 (en) | 2013-05-10 | 2014-05-08 | Acc inhibitors and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016526024A JP2016526024A (ja) | 2016-09-01 |
| JP2016526024A5 true JP2016526024A5 (OSRAM) | 2017-07-06 |
| JP6417401B2 JP6417401B2 (ja) | 2018-11-07 |
Family
ID=51867752
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016513082A Active JP6417401B2 (ja) | 2013-05-10 | 2014-05-08 | Ａｃｃ阻害剤及びその使用 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9988399B2 (OSRAM) |
| EP (1) | EP2994138A4 (OSRAM) |
| JP (1) | JP6417401B2 (OSRAM) |
| KR (1) | KR20160007598A (OSRAM) |
| CN (1) | CN105358152A (OSRAM) |
| AR (1) | AR096241A1 (OSRAM) |
| AU (1) | AU2014262636A1 (OSRAM) |
| BR (1) | BR112015028171A8 (OSRAM) |
| CA (1) | CA2911926A1 (OSRAM) |
| CL (1) | CL2015003314A1 (OSRAM) |
| EA (1) | EA201591959A1 (OSRAM) |
| HK (2) | HK1221659A1 (OSRAM) |
| MX (1) | MX2015015417A (OSRAM) |
| WO (1) | WO2014182943A1 (OSRAM) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102033806B1 (ko) * | 2011-11-11 | 2019-10-17 | 길리어드 아폴로, 엘엘씨 | Ａｃｃ 억제제 및 이의 용도 |
| HK1221411A1 (zh) | 2013-05-10 | 2017-06-02 | Gilead Apollo, Inc. | Acc抑制剂和其用途 |
| WO2014182950A1 (en) | 2013-05-10 | 2014-11-13 | Nimbus Apollo, Inc. | Acc inhibitors and uses thereof |
| KR20160005365A (ko) | 2013-05-10 | 2016-01-14 | 님버스 아폴로, 인코포레이티드 | Acc 억제제 및 이의 용도 |
| US10150728B2 (en) | 2013-10-17 | 2018-12-11 | Shionogi & Co., Ltd. | Alkylene derivatives |
| BR112017014341A2 (pt) | 2015-01-09 | 2018-03-27 | Gilead Apollo, Llc | método e sistema para tratamento, estabilização, ou redução da gravidade ou progressão de uma doença de fígado gorduroso não alcoólica, e, composição. |
| UY36586A (es) | 2015-03-26 | 2016-10-31 | Bayer Pharma AG | Heterociclilmetiltienouracilos y uso de los mismos |
| AR106472A1 (es) * | 2015-10-26 | 2018-01-17 | Gilead Apollo Llc | Inhibidores de acc y usos de los mismos |
| EP3380478B1 (en) | 2015-11-25 | 2020-12-23 | Gilead Apollo, LLC | Ester acc inhibitors and uses thereof |
| BR112018010453B1 (pt) * | 2015-11-25 | 2022-06-14 | Gilead Apollo, Llc | Compostos triazólicos inibindores de acetil coa carboxilase (acc) |
| EA201890913A1 (ru) * | 2015-11-25 | 2018-11-30 | Джилид Аполло, Ллс | Пиразоловые соединения в качестве ингибиторов акк и их применение |
| KR20180086191A (ko) | 2015-11-25 | 2018-07-30 | 길리어드 아폴로, 엘엘씨 | 2,4-디옥소-1,4-디히드로티에노[2,3-d]피리미딘 유도체를 함유하는 살진균 조성물 |
| AU2017226267B2 (en) | 2016-03-02 | 2021-06-24 | Gilead Apollo, Llc | Solid forms of a thienopyrimidinedione ACC inhibitor and methods for production thereof |
| WO2018041771A1 (de) | 2016-09-02 | 2018-03-08 | Bayer Pharma Aktiengesellschaft | (1-methylcyclopropyl)methyl-substituierte thienouracile und ihre verwendung |
| MX2019003351A (es) | 2016-09-23 | 2019-08-05 | Bayer Ag | Tienouracilos n3-ciclicamente sustituidos y uso de los mismos. |
| CN108341830B (zh) | 2017-01-22 | 2021-03-02 | 广东东阳光药业有限公司 | 噻吩并嘧啶衍生物及其在药物中的应用 |
| CN110431143B (zh) * | 2017-03-24 | 2022-08-12 | 浙江海正药业股份有限公司 | 杂芳基并嘧啶酮类衍生物及其制备方法和用途 |
| WO2018171699A1 (zh) | 2017-03-24 | 2018-09-27 | 浙江海正药业股份有限公司 | 氰基取代的杂芳基并嘧啶酮类衍生物及其制备方法和用途 |
| EP4122464B1 (en) | 2017-03-28 | 2024-05-15 | Gilead Sciences, Inc. | Therapeutic combinations for treating liver diseases |
| ES2986922T3 (es) * | 2018-06-05 | 2024-11-13 | Medshine Discovery Inc | Derivado de tieno[2,3-c]piridazin-4(1H)-ona y aplicación del mismo |
| KR20210093947A (ko) * | 2018-11-20 | 2021-07-28 | 더 내셔널 인스티튜츠 오브 파마슈티컬 리서치 앤드 디벨롭먼트 (엔아이피) | 스피로 화합물 및 이의 의학적 용도 |
| WO2020197926A1 (en) * | 2019-03-22 | 2020-10-01 | Kallyope, Inc. | Gpcr combination therapies |
| CN113924303B (zh) | 2019-07-02 | 2023-10-20 | 广东东阳光药业股份有限公司 | 具有立体构型的噻吩并嘧啶衍生物及其在药物中的应用 |
| AR119594A1 (es) | 2019-08-09 | 2021-12-29 | Gilead Sciences Inc | Derivados de tienopirimidina como inhibidores acc y usos de los mismos |
| WO2021110138A1 (zh) * | 2019-12-05 | 2021-06-10 | 漳州片仔癀药业股份有限公司 | 噻吩并[2,3-c]哒嗪-4(1H)-酮类化合物的晶型及其制备方法和应用 |
| ES2965380T3 (es) * | 2019-12-05 | 2024-04-15 | Zhangzhou Pien Tze Huang Pharm | Forma cristalina como inhibidor de ACC1 y ACC2, y método de preparación de la misma y uso de la misma |
| US11478533B2 (en) | 2020-04-27 | 2022-10-25 | Novo Nordisk A/S | Semaglutide for use in medicine |
| CN111793566B (zh) * | 2020-07-31 | 2021-11-16 | 南京林业大学 | 一种杉木内生真菌及其生物防治应用 |
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| GEP20166474B (en) * | 2011-04-22 | 2016-05-10 | Pfizer | Pyrazolospiroketone derivatives for use as acetyl-coa carboxylase inhibitors |
| JPWO2013035827A1 (ja) | 2011-09-09 | 2015-03-23 | 塩野義製薬株式会社 | 新規オレフィン誘導体 |
| US20130116241A1 (en) | 2011-11-09 | 2013-05-09 | Abbvie Inc. | Novel inhibitor compounds of phosphodiesterase type 10a |
| KR102033806B1 (ko) * | 2011-11-11 | 2019-10-17 | 길리어드 아폴로, 엘엘씨 | Ａｃｃ 억제제 및 이의 용도 |
| KR20160005365A (ko) | 2013-05-10 | 2016-01-14 | 님버스 아폴로, 인코포레이티드 | Acc 억제제 및 이의 용도 |
| WO2014182950A1 (en) * | 2013-05-10 | 2014-11-13 | Nimbus Apollo, Inc. | Acc inhibitors and uses thereof |
| HK1221411A1 (zh) | 2013-05-10 | 2017-06-02 | Gilead Apollo, Inc. | Acc抑制剂和其用途 |
-
2014
- 2014-05-08 EA EA201591959A patent/EA201591959A1/ru unknown
- 2014-05-08 MX MX2015015417A patent/MX2015015417A/es unknown
- 2014-05-08 KR KR1020157035041A patent/KR20160007598A/ko not_active Withdrawn
- 2014-05-08 EP EP14795076.0A patent/EP2994138A4/en not_active Withdrawn
- 2014-05-08 JP JP2016513082A patent/JP6417401B2/ja active Active
- 2014-05-08 AU AU2014262636A patent/AU2014262636A1/en not_active Abandoned
- 2014-05-08 US US14/890,308 patent/US9988399B2/en active Active
- 2014-05-08 CN CN201480036133.2A patent/CN105358152A/zh active Pending
- 2014-05-08 HK HK16109917.3A patent/HK1221659A1/zh unknown
- 2014-05-08 HK HK16109586.3A patent/HK1221410A1/zh unknown
- 2014-05-08 CA CA2911926A patent/CA2911926A1/en not_active Abandoned
- 2014-05-08 BR BR112015028171A patent/BR112015028171A8/pt not_active Application Discontinuation
- 2014-05-08 WO PCT/US2014/037360 patent/WO2014182943A1/en not_active Ceased
- 2014-05-09 AR ARP140101888A patent/AR096241A1/es unknown
-
2015
- 2015-11-10 CL CL2015003314A patent/CL2015003314A1/es unknown
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