JP2019507160A5 - - Google Patents
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- JP2019507160A5 JP2019507160A5 JP2018545600A JP2018545600A JP2019507160A5 JP 2019507160 A5 JP2019507160 A5 JP 2019507160A5 JP 2018545600 A JP2018545600 A JP 2018545600A JP 2018545600 A JP2018545600 A JP 2018545600A JP 2019507160 A5 JP2019507160 A5 JP 2019507160A5
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- compound
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- acyl
- under conditions
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 128
- 229940125904 compound 1 Drugs 0.000 claims description 52
- 238000000034 method Methods 0.000 claims description 28
- 125000002252 acyl group Chemical group 0.000 claims description 20
- 125000001931 aliphatic group Chemical group 0.000 claims description 20
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 239000001257 hydrogen Substances 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 13
- 229910052736 halogen Inorganic materials 0.000 claims description 10
- 150000002367 halogens Chemical class 0.000 claims description 10
- 229910052760 oxygen Inorganic materials 0.000 claims description 10
- 239000001301 oxygen Chemical group 0.000 claims description 10
- 239000013078 crystal Substances 0.000 claims description 9
- -1 cyclic anhydride Chemical class 0.000 claims description 8
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims description 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 125000005842 heteroatom Chemical group 0.000 claims description 6
- 238000004519 manufacturing process Methods 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 6
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 229910052717 sulfur Chemical group 0.000 claims description 6
- 239000011593 sulfur Chemical group 0.000 claims description 6
- AICOOMRHRUFYCM-ZRRPKQBOSA-N oxazine, 1 Chemical compound C([C@@H]1[C@H](C(C[C@]2(C)[C@@H]([C@H](C)N(C)C)[C@H](O)C[C@]21C)=O)CC1=CC2)C[C@H]1[C@@]1(C)[C@H]2N=C(C(C)C)OC1 AICOOMRHRUFYCM-ZRRPKQBOSA-N 0.000 claims description 5
- 108090001060 Lipase Proteins 0.000 claims description 4
- 102000004882 Lipase Human genes 0.000 claims description 4
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims description 4
- 239000002253 acid Substances 0.000 claims description 4
- 239000002671 adjuvant Substances 0.000 claims description 4
- 150000003842 bromide salts Chemical class 0.000 claims description 4
- 125000001246 bromo group Chemical group Br* 0.000 claims description 4
- 239000003153 chemical reaction reagent Substances 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 230000003301 hydrolyzing effect Effects 0.000 claims description 4
- FALRKNHUBBKYCC-UHFFFAOYSA-N 2-(chloromethyl)pyridine-3-carbonitrile Chemical group ClCC1=NC=CC=C1C#N FALRKNHUBBKYCC-UHFFFAOYSA-N 0.000 claims description 2
- 208000002874 Acne Vulgaris Diseases 0.000 claims description 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical group [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 2
- 108010031797 Candida antarctica lipase B Proteins 0.000 claims description 2
- 229940126062 Compound A Drugs 0.000 claims description 2
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical group C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical group [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims description 2
- KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical group [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 claims description 2
- 206010000496 acne Diseases 0.000 claims description 2
- 239000003054 catalyst Substances 0.000 claims description 2
- ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical group OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 claims description 2
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 2
- 150000002596 lactones Chemical class 0.000 claims description 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims description 2
- 229910052763 palladium Inorganic materials 0.000 claims description 2
- 125000004193 piperazinyl group Chemical group 0.000 claims description 2
- 239000000843 powder Substances 0.000 claims description 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 2
- 230000005855 radiation Effects 0.000 claims description 2
- 239000012453 solvate Substances 0.000 claims description 2
- 229940014800 succinic anhydride Drugs 0.000 claims description 2
- 125000002730 succinyl group Chemical group C(CCC(=O)*)(=O)* 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 5
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims 1
- MRHCVYVBPDWKKW-UHFFFAOYSA-N CC(C)(C(O)=O)N(C(N(CC(c(cccc1)c1OC)OC1CCOCC1)c1c2c(C)c(-c3ncc[o]3)[s]1)O)C2=O Chemical compound CC(C)(C(O)=O)N(C(N(CC(c(cccc1)c1OC)OC1CCOCC1)c1c2c(C)c(-c3ncc[o]3)[s]1)O)C2=O MRHCVYVBPDWKKW-UHFFFAOYSA-N 0.000 description 1
- 0 CC(C)(C(O)=O)N(C(c1c(N2CC(c(cccc3)c3OC)OC3CCOCC3)[s]c(-c3ncc[o]3)c1C)=*)C2=O Chemical compound CC(C)(C(O)=O)N(C(c1c(N2CC(c(cccc3)c3OC)OC3CCOCC3)[s]c(-c3ncc[o]3)c1C)=*)C2=O 0.000 description 1
- NFBQJHOKTSYEDJ-QHCPKHFHSA-N CC(C)(C)OC(C(C)(C)N(C(c1c(N2C[C@@H](c3ccccc3OC)OC3CCOCC3)[s]c(-c3ncc[o]3)c1C)=O)C2=O)=O Chemical compound CC(C)(C)OC(C(C)(C)N(C(c1c(N2C[C@@H](c3ccccc3OC)OC3CCOCC3)[s]c(-c3ncc[o]3)c1C)=O)C2=O)=O NFBQJHOKTSYEDJ-QHCPKHFHSA-N 0.000 description 1
- KDOOPURHOFZIIO-UHFFFAOYSA-N COc1c(C(COC(CCC(O)=O)=O)OC2CCOCC2)cccc1 Chemical compound COc1c(C(COC(CCC(O)=O)=O)OC2CCOCC2)cccc1 KDOOPURHOFZIIO-UHFFFAOYSA-N 0.000 description 1
- CEEBLZHSAZJAFU-AWEZNQCLSA-N COc1c([C@H](CC(F)(F)F)OC2CCOCC2)cccc1 Chemical compound COc1c([C@H](CC(F)(F)F)OC2CCOCC2)cccc1 CEEBLZHSAZJAFU-AWEZNQCLSA-N 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021147802A JP7184988B2 (ja) | 2016-03-02 | 2021-09-10 | チエノピリミジンジオンａｃｃ阻害剤の固体形態およびその生成のための方法 |
| JP2022187472A JP7356564B2 (ja) | 2016-03-02 | 2022-11-24 | チエノピリミジンジオンａｃｃ阻害剤の固体形態およびその生成のための方法 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662302755P | 2016-03-02 | 2016-03-02 | |
| US62/302,755 | 2016-03-02 | ||
| US201662303237P | 2016-03-03 | 2016-03-03 | |
| US62/303,237 | 2016-03-03 | ||
| PCT/US2017/020271 WO2017151816A1 (en) | 2016-03-02 | 2017-03-01 | Solid forms of a thienopyrimidinedione acc inhibitor and methods for production thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021147802A Division JP7184988B2 (ja) | 2016-03-02 | 2021-09-10 | チエノピリミジンジオンａｃｃ阻害剤の固体形態およびその生成のための方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019507160A JP2019507160A (ja) | 2019-03-14 |
| JP2019507160A5 true JP2019507160A5 (enExample) | 2020-03-19 |
| JP6944462B2 JP6944462B2 (ja) | 2021-10-06 |
Family
ID=58347936
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018545600A Active JP6944462B2 (ja) | 2016-03-02 | 2017-03-01 | チエノピリミジンジオンａｃｃ阻害剤の固体形態およびその生成のための方法 |
| JP2021147802A Active JP7184988B2 (ja) | 2016-03-02 | 2021-09-10 | チエノピリミジンジオンａｃｃ阻害剤の固体形態およびその生成のための方法 |
| JP2022187472A Active JP7356564B2 (ja) | 2016-03-02 | 2022-11-24 | チエノピリミジンジオンａｃｃ阻害剤の固体形態およびその生成のための方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021147802A Active JP7184988B2 (ja) | 2016-03-02 | 2021-09-10 | チエノピリミジンジオンａｃｃ阻害剤の固体形態およびその生成のための方法 |
| JP2022187472A Active JP7356564B2 (ja) | 2016-03-02 | 2022-11-24 | チエノピリミジンジオンａｃｃ阻害剤の固体形態およびその生成のための方法 |
Country Status (15)
| Country | Link |
|---|---|
| US (4) | US10183951B2 (enExample) |
| EP (2) | EP4364795A3 (enExample) |
| JP (3) | JP6944462B2 (enExample) |
| KR (3) | KR102700008B1 (enExample) |
| CN (3) | CN108699078A (enExample) |
| AU (3) | AU2017226267B2 (enExample) |
| BR (1) | BR112018067408A2 (enExample) |
| CA (4) | CA3155220C (enExample) |
| ES (1) | ES2972487T3 (enExample) |
| IL (1) | IL261255A (enExample) |
| MX (1) | MX2018010427A (enExample) |
| PL (1) | PL3423456T3 (enExample) |
| SG (1) | SG11201807077RA (enExample) |
| TW (3) | TWI818828B (enExample) |
| WO (1) | WO2017151816A1 (enExample) |
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| MX370976B (es) | 2011-11-11 | 2020-01-10 | Gilead Apollo Llc | Inhibidores de acetil coa carboxilasa (acc) y usos de los mismos. |
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| 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 |
| US20170166582A1 (en) | 2015-11-25 | 2017-06-15 | Gilead Apollo, Llc | Pyrazole acc inhibitors and uses thereof |
| CN108347939B (zh) | 2015-11-25 | 2021-09-28 | 吉利德阿波罗公司 | 含有2,4-二氧代-1,4-二氢噻吩并[2,3-d]嘧啶的衍生物的杀真菌组合物 |
| CA3155220C (en) | 2016-03-02 | 2024-01-16 | Gilead Apollo, Llc | Solid forms of a thienopyrimidinedione acc inhibitor and methods for production thereof |
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| WO2019015583A1 (en) * | 2017-07-17 | 2019-01-24 | Nanjing Ruijie Pharmatech Co., Ltd. | NOVEL 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 |
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| CN109810085B (zh) * | 2019-04-19 | 2019-07-19 | 上海皓元生物医药科技有限公司 | Acc抑制剂及其中间体的制备方法 |
| TWI915558B (zh) | 2019-06-14 | 2026-02-21 | 美商基利科學股份有限公司 | Cot 調節劑及其使用方法 |
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| JP2022548617A (ja) | 2019-09-19 | 2022-11-21 | ノバルティス アーゲー | Ｆｘｒアゴニストを含む処置 |
| CN112574253B (zh) * | 2019-09-29 | 2021-08-27 | 上海喀露蓝科技有限公司 | 磷酸或磷酸酯类衍生物、其制备方法及其在医药上的用途 |
| CN110746439B (zh) * | 2019-10-18 | 2020-10-30 | 南京瑞捷医药科技有限公司 | 一种噻吩并嘧啶二酮化合物的制备方法 |
| CN112778325A (zh) * | 2019-11-07 | 2021-05-11 | 南京瑞捷医药科技有限公司 | 一种acc抑制剂及其用途 |
| CN114728168B (zh) | 2019-11-15 | 2024-04-09 | 吉利德科学公司 | 三唑氨基甲酸酯吡啶基磺酰胺作为lpa受体拮抗剂及其用途 |
| CN114787166B (zh) * | 2019-12-05 | 2023-09-19 | 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 |
| WO2021110135A1 (zh) * | 2019-12-05 | 2021-06-10 | 漳州片仔癀药业股份有限公司 | 作为acc1和acc2抑制剂的晶型及其制备方法和应用 |
| CA3175541A1 (en) | 2020-03-30 | 2021-10-07 | Gilead Sciences, Inc. | Solid forms of (s)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1h-1,2,3-triazol-4-yl)2-methyl-1-oxo-1,2- dihydroisoquinolin-5-yl)methyl)))amino)8-chloro-(neopentylamino)quinoline-3-carb onitrile a cot inhibitor compound |
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| CA3209240A1 (en) * | 2021-02-22 | 2022-08-25 | Samuel D. Waksal | Rock2 inhibitor for the treatment of viral infection |
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