JP2014533281A5 - - Google Patents
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- JP2014533281A5 JP2014533281A5 JP2014541351A JP2014541351A JP2014533281A5 JP 2014533281 A5 JP2014533281 A5 JP 2014533281A5 JP 2014541351 A JP2014541351 A JP 2014541351A JP 2014541351 A JP2014541351 A JP 2014541351A JP 2014533281 A5 JP2014533281 A5 JP 2014533281A5
- Authority
- JP
- Japan
- Prior art keywords
- membered
- ring
- sulfur
- oxygen
- nitrogen
- 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.)
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 86
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 64
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 64
- 125000005842 heteroatom Chemical group 0.000 claims description 64
- 229910052757 nitrogen Inorganic materials 0.000 claims description 64
- 229910052760 oxygen Inorganic materials 0.000 claims description 64
- 239000001301 oxygen Substances 0.000 claims description 64
- 229910052717 sulfur Inorganic materials 0.000 claims description 62
- 239000011593 sulfur Substances 0.000 claims description 62
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 42
- 229920006395 saturated elastomer Polymers 0.000 claims description 32
- 229910052736 halogen Inorganic materials 0.000 claims description 30
- 150000002367 halogens Chemical class 0.000 claims description 30
- 229910052739 hydrogen Inorganic materials 0.000 claims description 30
- 239000001257 hydrogen Substances 0.000 claims description 30
- 150000001875 compounds Chemical class 0.000 claims description 26
- 125000001931 aliphatic group Chemical group 0.000 claims description 24
- 125000002950 monocyclic group Chemical group 0.000 claims description 22
- 150000003839 salts Chemical class 0.000 claims description 21
- 125000000623 heterocyclic group Chemical group 0.000 claims description 20
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 20
- 239000000203 mixture Substances 0.000 claims description 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 13
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 8
- 125000001047 cyclobutenyl group Chemical group C1(=CCC1)* 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 150000002431 hydrogen Chemical class 0.000 claims description 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 8
- 208000030159 metabolic disease Diseases 0.000 claims description 8
- 125000003566 oxetanyl group Chemical group 0.000 claims description 8
- 208000008589 Obesity Diseases 0.000 claims description 6
- 125000000217 alkyl group Chemical group 0.000 claims description 6
- 230000002401 inhibitory effect Effects 0.000 claims description 6
- 235000020824 obesity Nutrition 0.000 claims description 6
- 208000035143 Bacterial infection Diseases 0.000 claims description 4
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 4
- 206010017533 Fungal infection Diseases 0.000 claims description 4
- 208000031888 Mycoses Diseases 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 208000030852 Parasitic disease Diseases 0.000 claims description 4
- 208000022362 bacterial infectious disease Diseases 0.000 claims description 4
- 239000012472 biological sample Substances 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 125000002837 carbocyclic group Chemical group 0.000 claims description 4
- 229910052805 deuterium Inorganic materials 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 230000002538 fungal effect Effects 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
- 230000003071 parasitic effect Effects 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 208000011580 syndromic disease Diseases 0.000 claims description 4
- 208000008020 Cohen syndrome Diseases 0.000 claims description 2
- 208000032928 Dyslipidaemia 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
- 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
- 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
- 125000005605 benzo group Chemical group 0.000 claims description 2
- 125000002619 bicyclic 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
- 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
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- 229940125396 insulin Drugs 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 125000002971 oxazolyl 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
- 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
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 2
- 150000001467 thiazolidinediones Chemical class 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 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 description 6
- 108010016219 Acetyl-CoA carboxylase Proteins 0.000 description 6
- 108010018763 Biotin carboxylase Proteins 0.000 description 6
- 0 C*CCC(C)N(C(C(C(*)=C(C)*1)=C1N1*)=O)C1=O Chemical compound C*CCC(C)N(C(C(C(*)=C(C)*1)=C1N1*)=O)C1=O 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161559023P | 2011-11-11 | 2011-11-11 | |
| US61/559,023 | 2011-11-11 | ||
| US201261615092P | 2012-03-23 | 2012-03-23 | |
| US61/615,092 | 2012-03-23 | ||
| US201261651878P | 2012-05-25 | 2012-05-25 | |
| US61/651,878 | 2012-05-25 | ||
| US201261675513P | 2012-07-25 | 2012-07-25 | |
| US61/675,513 | 2012-07-25 | ||
| PCT/US2012/064528 WO2013071169A1 (en) | 2011-11-11 | 2012-11-09 | Acc inhibitors and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017051746A Division JP6276442B2 (ja) | 2011-11-11 | 2017-03-16 | Acc阻害剤およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014533281A JP2014533281A (ja) | 2014-12-11 |
| JP2014533281A5 true JP2014533281A5 (enExample) | 2015-12-24 |
| JP6114297B2 JP6114297B2 (ja) | 2017-04-12 |
Family
ID=48281206
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014541351A Active JP6114297B2 (ja) | 2011-11-11 | 2012-11-09 | Acc阻害剤およびその使用 |
| JP2017051746A Active JP6276442B2 (ja) | 2011-11-11 | 2017-03-16 | Acc阻害剤およびその使用 |
| JP2018002648A Active JP6543358B2 (ja) | 2011-11-11 | 2018-01-11 | Acc阻害剤およびその使用 |
| JP2019111246A Active JP6756014B2 (ja) | 2011-11-11 | 2019-06-14 | Acc阻害剤およびその使用 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017051746A Active JP6276442B2 (ja) | 2011-11-11 | 2017-03-16 | Acc阻害剤およびその使用 |
| JP2018002648A Active JP6543358B2 (ja) | 2011-11-11 | 2018-01-11 | Acc阻害剤およびその使用 |
| JP2019111246A Active JP6756014B2 (ja) | 2011-11-11 | 2019-06-14 | Acc阻害剤およびその使用 |
Country Status (26)
| Country | Link |
|---|---|
| US (5) | US8969557B2 (enExample) |
| EP (3) | EP3329919B1 (enExample) |
| JP (4) | JP6114297B2 (enExample) |
| KR (3) | KR102060290B1 (enExample) |
| CN (3) | CN109970760B (enExample) |
| AU (3) | AU2012335088B2 (enExample) |
| BR (2) | BR112014011351B1 (enExample) |
| CA (1) | CA2855372C (enExample) |
| CL (1) | CL2014001241A1 (enExample) |
| CY (2) | CY1120224T1 (enExample) |
| DK (2) | DK3329919T3 (enExample) |
| EA (2) | EA030264B1 (enExample) |
| ES (3) | ES2665580T3 (enExample) |
| HR (2) | HRP20180534T1 (enExample) |
| HU (2) | HUE037444T2 (enExample) |
| LT (2) | LT2776038T (enExample) |
| MX (3) | MX370976B (enExample) |
| PL (3) | PL2776038T3 (enExample) |
| PT (2) | PT3329919T (enExample) |
| RS (1) | RS57157B1 (enExample) |
| SI (2) | SI2776038T1 (enExample) |
| SM (1) | SMT201800191T1 (enExample) |
| TW (4) | TWI655193B (enExample) |
| UA (2) | UA114901C2 (enExample) |
| WO (1) | WO2013071169A1 (enExample) |
| ZA (3) | ZA201403633B (enExample) |
Families Citing this family (123)
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| TWI625121B (zh) | 2009-07-13 | 2018-06-01 | 基利科學股份有限公司 | 調節細胞凋亡信號之激酶的抑制劑 |
| EP2386555A1 (en) | 2010-05-13 | 2011-11-16 | Almirall, S.A. | New cyclohexylamine derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activities |
| EP2592078A1 (en) | 2011-11-11 | 2013-05-15 | Almirall, S.A. | New cyclohexylamine derivatives having beta2 adrenergic agonist and M3 muscarinic antagonist activities |
| RS57157B1 (sr) | 2011-11-11 | 2018-07-31 | Gilead Apollo Llc | Acc inhibitori i njihove primene |
| PL2861611T3 (pl) | 2012-05-25 | 2017-08-31 | Janssen Sciences Ireland Uc | Nukleozydy uracylowe spirooksetanu |
| US8859774B2 (en) | 2012-05-25 | 2014-10-14 | Corcept Therapeutics, Inc. | Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
| US12226412B2 (en) | 2012-05-25 | 2025-02-18 | Corcept Therapeutics, Inc. | Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
| BR112015013628A2 (pt) | 2012-12-18 | 2017-07-11 | Almirall Sa | derivados de carbamato de ciclo-hexila e quinuclidinila tendo atividades agonista adrenérgica de beta2 e antagonista muscarínica de m3 |
| TWI643853B (zh) | 2013-02-27 | 2018-12-11 | 阿爾米雷爾有限公司 | 同時具有β2腎上腺素受體促效劑和M3毒蕈鹼受體拮抗劑活性之2-氨基-1-羥乙基-8-羥基喹啉-2(1H)-酮衍生物之鹽類 |
| EP2994138A4 (en) * | 2013-05-10 | 2016-12-28 | Nimbus Apollo Inc | ACC-HEMMER AND USES THEREOF |
| EP2994139B1 (en) | 2013-05-10 | 2019-04-10 | Gilead Apollo, LLC | Acc inhibitors and uses thereof |
| JP6417403B2 (ja) * | 2013-05-10 | 2018-11-07 | ギリアド アポロ, エルエルシー | Acc阻害剤及びその使用 |
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| WO2015003879A1 (en) * | 2013-07-08 | 2015-01-15 | Syngenta Participations Ag | Microbiocidal heterobicylic derivatives |
| WO2015003881A1 (en) * | 2013-07-08 | 2015-01-15 | Syngenta Participations Ag | Microbiocidal heterobicyclic derivatives |
| WO2015007453A1 (en) * | 2013-07-15 | 2015-01-22 | Syngenta Participations Ag | Microbiocidal heterobicyclic derivatives |
| WO2015007451A1 (en) | 2013-07-15 | 2015-01-22 | Syngenta Participations Ag | Microbiocidal heterobicyclic derivatives |
| WO2015010832A1 (en) * | 2013-07-22 | 2015-01-29 | Syngenta Participations Ag | Microbiocidal heterocyclic derivatives |
| TW201517906A (zh) | 2013-07-25 | 2015-05-16 | Almirall Sa | 含有maba化合物和皮質類固醇之組合 |
| TWI641373B (zh) | 2013-07-25 | 2018-11-21 | 阿爾米雷爾有限公司 | 具有蕈毒鹼受體拮抗劑和β2腎上腺素受體促效劑二者之活性的2-胺基-1-羥乙基-8-羥基喹啉-2(1H)-酮衍生物之鹽 |
| BR112016004118A2 (pt) | 2013-09-12 | 2017-10-17 | Pfizer | uso de inibidores da acetil-coa carboxilase para tratamento de acne vulgar |
| MX2016004250A (es) | 2013-10-07 | 2016-07-12 | Bayer Pharma AG | Tienouracilcarboxamidas ciclicas y usos de las mismas. |
| WO2015056782A1 (ja) | 2013-10-17 | 2015-04-23 | 塩野義製薬株式会社 | 新規アルキレン誘導体 |
| SI3064498T1 (sl) * | 2013-10-30 | 2019-11-29 | Shanghai hengrui pharmaceutical co ltd | Derivati pirazolopirimidona ali pirolotriazona, postopki priprave le-teh in farmacevtske uporabe le-teh |
| MY175865A (en) | 2013-12-19 | 2020-07-14 | Novartis Ag | [1,2,4]triazolo[1,5-a]pyrimidine derivatives as protozoan proteasome inhibitors for the treatment of parasitic diseases such as leishmaniasis |
| JP6573968B2 (ja) * | 2014-08-11 | 2019-09-11 | ハイドラ バイオサイエンシズ インコーポレイテッドHydra Biosciences,Inc. | TRPC5調節因子としての、精神神経障害の処置のためのチエノおよびフロ[2,3−d]ピリミジン−2,4[1H,3H]−ジオン誘導体 |
| TW201617343A (zh) | 2014-09-26 | 2016-05-16 | 阿爾米雷爾有限公司 | 具有β2腎上腺素促效劑及M3蕈毒拮抗劑活性之新穎雙環衍生物 |
| CN105779463B (zh) * | 2014-12-25 | 2019-08-09 | 深圳华大生命科学研究院 | Vps13b基因突变体及其应用 |
| EA201892625A1 (ru) | 2015-01-09 | 2019-07-31 | Джилид Аполло, Ллс | КОМБИНИРОВАННАЯ ТЕРАПИЯ С ПРИМЕНЕНИЕМ ИНГИБИТОРА АЦЕТИЛ-КоА-КАРБОКСИЛАЗЫ (ACC) ДЛЯ ЛЕЧЕНИЯ НЕАЛКОГОЛЬНОЙ ЖИРОВОЙ БОЛЕЗНИ ПЕЧЕНИ |
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