JP2020505356A5 - - Google Patents
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- JP2020505356A5 JP2020505356A5 JP2019538620A JP2019538620A JP2020505356A5 JP 2020505356 A5 JP2020505356 A5 JP 2020505356A5 JP 2019538620 A JP2019538620 A JP 2019538620A JP 2019538620 A JP2019538620 A JP 2019538620A JP 2020505356 A5 JP2020505356 A5 JP 2020505356A5
- Authority
- JP
- Japan
- Prior art keywords
- hydroxy
- cyano
- nitro
- amino
- 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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- -1 hydroxy, amino Chemical group 0.000 claims description 61
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 33
- 150000001875 compounds Chemical class 0.000 claims description 31
- 229910052739 hydrogen Inorganic materials 0.000 claims description 30
- 125000000217 alkyl group Chemical group 0.000 claims description 29
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 25
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 25
- 125000003545 alkoxy group Chemical group 0.000 claims description 20
- 208000035475 disorder Diseases 0.000 claims description 20
- 125000000623 heterocyclic group Chemical group 0.000 claims description 18
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims description 14
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 14
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 14
- 239000008194 pharmaceutical composition Substances 0.000 claims description 14
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 14
- 201000010099 disease Diseases 0.000 claims description 13
- 102000000452 Acetyl-CoA carboxylase Human genes 0.000 claims description 12
- 108010016219 Acetyl-CoA carboxylase Proteins 0.000 claims description 12
- 108010018763 Biotin carboxylase Proteins 0.000 claims description 12
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims description 12
- 125000004122 cyclic group Chemical group 0.000 claims description 10
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 9
- 125000002541 furyl group Chemical group 0.000 claims description 8
- 125000002883 imidazolyl group Chemical group 0.000 claims description 8
- 125000001624 naphthyl group Chemical group 0.000 claims description 8
- 230000001613 neoplastic effect Effects 0.000 claims description 8
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims description 8
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims description 8
- 125000002971 oxazolyl group Chemical group 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 8
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 8
- 125000000335 thiazolyl group Chemical group 0.000 claims description 8
- 125000001544 thienyl group Chemical group 0.000 claims description 8
- 125000001425 triazolyl group Chemical group 0.000 claims description 8
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 7
- 206010028980 Neoplasm Diseases 0.000 claims description 7
- 201000011510 cancer Diseases 0.000 claims description 7
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims description 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 6
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims description 6
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 6
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- 125000004076 pyridyl group Chemical group 0.000 claims description 6
- 125000001424 substituent group Chemical group 0.000 claims description 6
- 125000004205 trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims description 6
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 5
- 125000006642 (C1-C6) cyanoalkyl group Chemical group 0.000 claims description 4
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 4
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 4
- 206010014733 Endometrial cancer Diseases 0.000 claims description 4
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 4
- 206010022489 Insulin Resistance Diseases 0.000 claims description 4
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 4
- 208000001145 Metabolic Syndrome Diseases 0.000 claims description 4
- 150000001204 N-oxides Chemical class 0.000 claims description 4
- 206010029098 Neoplasm skin Diseases 0.000 claims description 4
- 208000008589 Obesity Diseases 0.000 claims description 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 4
- 206010060862 Prostate cancer Diseases 0.000 claims description 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 4
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 4
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 4
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 4
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims description 4
- 125000004966 cyanoalkyl group Chemical group 0.000 claims description 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 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 4
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 4
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 4
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 4
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 4
- 125000002632 imidazolidinyl group Chemical group 0.000 claims description 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- 208000030159 metabolic disease Diseases 0.000 claims description 4
- 239000002207 metabolite Substances 0.000 claims description 4
- 125000002757 morpholinyl group Chemical group 0.000 claims description 4
- 235000020824 obesity Nutrition 0.000 claims description 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 4
- 125000004193 piperazinyl group Chemical group 0.000 claims description 4
- 125000005936 piperidyl group Chemical group 0.000 claims description 4
- 239000000651 prodrug Substances 0.000 claims description 4
- 229940002612 prodrug Drugs 0.000 claims description 4
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims description 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 4
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 239000012453 solvate Substances 0.000 claims description 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 4
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 4
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 3
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims description 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 2
- 125000001731 2-cyanoethyl group Chemical group [H]C([H])(*)C([H])([H])C#N 0.000 claims description 2
- 125000004777 2-fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 229920006395 saturated elastomer Polymers 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- 238000000034 method Methods 0.000 description 4
- 239000003814 drug Substances 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710052275.3 | 2017-01-22 | ||
| CN201710052275 | 2017-01-22 | ||
| PCT/CN2018/073581 WO2018133858A1 (en) | 2017-01-22 | 2018-01-22 | Thienopyrimidine derivative and use thereof in medicine |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020505356A JP2020505356A (ja) | 2020-02-20 |
| JP2020505356A5 true JP2020505356A5 (https=) | 2021-02-18 |
| JP7046959B2 JP7046959B2 (ja) | 2022-04-04 |
Family
ID=62908330
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019538620A Active JP7046959B2 (ja) | 2017-01-22 | 2018-01-22 | チエノピリミジン誘導体及び医薬におけるその使用 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10759812B2 (https=) |
| EP (1) | EP3571205B1 (https=) |
| JP (1) | JP7046959B2 (https=) |
| KR (1) | KR102577824B1 (https=) |
| CN (1) | CN108341830B (https=) |
| AU (1) | AU2018209006B2 (https=) |
| CA (1) | CA3049816A1 (https=) |
| WO (1) | WO2018133858A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN119977993A (zh) | 2016-03-02 | 2025-05-13 | 吉利德阿波罗公司 | 噻吩并嘧啶二酮acc抑制剂的固体形式及其制备方法 |
| EP4273132A3 (en) | 2017-03-03 | 2024-01-10 | Gilead Sciences, Inc. | Processes for preparing acc inhibitors and solid forms thereof |
| PT3600309T (pt) | 2017-03-28 | 2022-10-03 | Gilead Sciences Inc | Combinações terapêuticas para o tratamento de doenças hepáticas |
| WO2019020041A1 (zh) * | 2017-07-26 | 2019-01-31 | 南京圣和药业股份有限公司 | 作为acc抑制剂的化合物及其应用 |
| EP3758706A4 (en) | 2018-02-28 | 2021-11-24 | The Regents Of The University Of Colorado | WEE1 KINASE INHIBITORS AND METHODS OF TREATING CANCER USING THEREOF |
| 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 |
| CN111848678A (zh) * | 2019-04-30 | 2020-10-30 | 正大天晴药业集团股份有限公司 | 含磷类噻吩并嘧啶衍生物 |
| EP3995498A4 (en) * | 2019-07-02 | 2023-03-01 | Sunshine Lake Pharma Co., Ltd. | THIENOPYRIMIDI DERIVATIVES WITH STEREO CONFIGURATION AND THEIR USE IN MEDICINE |
| AR119594A1 (es) | 2019-08-09 | 2021-12-29 | Gilead Sciences Inc | Derivados de tienopirimidina como inhibidores acc y usos de los mismos |
| WO2022111517A1 (zh) * | 2020-11-24 | 2022-06-02 | 正大天晴药业集团股份有限公司 | 氘修饰的噻吩并吡啶酮化合物 |
| TW202233632A (zh) * | 2021-02-07 | 2022-09-01 | 大陸商正大天晴藥業集團股份有限公司 | 噻吩并嘧啶衍生物 |
| CN117126174B (zh) * | 2022-05-26 | 2025-12-05 | 广东东阳光药业股份有限公司 | 噻吩并嘧啶类化合物的共晶及其用途 |
| TW202400151A (zh) * | 2022-05-26 | 2024-01-01 | 大陸商廣東東陽光藥業股份有限公司 | 噻吩並嘧啶類化合物的晶型及其用途 |
| CN117126175B (zh) * | 2022-05-26 | 2025-12-05 | 广东东阳光药业股份有限公司 | 噻吩并嘧啶类化合物的共晶及其用途 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19644228A1 (de) | 1996-10-24 | 1998-04-30 | Merck Patent Gmbh | Thienopyrimidine |
| CA2644996A1 (en) | 2006-03-02 | 2007-09-13 | Cv Therapeutics, Inc. | A2a adenosine receptor antagonists |
| LT2776038T (lt) * | 2011-11-11 | 2018-04-25 | Gilead Apollo, Llc | Acc inhibitoriai ir jų panaudojimas |
| EA201591959A1 (ru) | 2013-05-10 | 2016-03-31 | Нимбус Аполло, Инк. | Ингибиторы акк и их применение |
| CA2911818A1 (en) | 2013-05-10 | 2014-11-13 | Nimbus Apollo, Inc. | Acc inhibitors and uses thereof |
| AU2014262547A1 (en) | 2013-05-10 | 2015-11-26 | Gilead Apollo, Llc | ACC inhibitors and uses thereof |
| WO2015003881A1 (en) | 2013-07-08 | 2015-01-15 | Syngenta Participations Ag | Microbiocidal heterobicyclic derivatives |
| WO2015007451A1 (en) * | 2013-07-15 | 2015-01-22 | Syngenta Participations Ag | Microbiocidal heterobicyclic derivatives |
| EP3034501A1 (en) * | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Hydroxy containing FXR (NR1H4) modulating compounds |
| JP2018501276A (ja) * | 2015-01-09 | 2018-01-18 | ギリアド アポロ， エルエルシー | 非アルコール性脂肪肝疾患の処置のためのａｃｃ阻害剤併用療法 |
| AR106472A1 (es) | 2015-10-26 | 2018-01-17 | Gilead Apollo Llc | Inhibidores de acc y usos de los mismos |
| HUE053175T2 (hu) | 2015-11-25 | 2021-06-28 | Gilead Apollo Llc | ACC-gátló észterek és azok alkalmazása |
| BR112018009212B1 (pt) | 2015-11-25 | 2022-06-14 | Gilead Apollo, Llc | Método para controlar patógenos fúngicos agrícolas |
| CA3004796C (en) | 2015-11-25 | 2023-11-14 | Gilead Apollo, Llc | Pyrazole acc inhibitors and uses thereof |
| EP3380479B1 (en) | 2015-11-25 | 2022-12-07 | Gilead Apollo, LLC | Triazole acc inhibitors and uses thereof |
| WO2017147161A1 (en) | 2016-02-23 | 2017-08-31 | Raju Mohan | Treatment of dermatological disorders or conditions |
| CN107698603B (zh) | 2016-08-09 | 2022-04-08 | 南京红云生物科技有限公司 | 噻吩并嘧啶类化合物、其制备方法、药用组合物及其应用 |
| CN110431144B (zh) | 2017-03-24 | 2022-08-05 | 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 |
| WO2018171698A1 (zh) | 2017-03-24 | 2018-09-27 | 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 |
| WO2018228369A1 (zh) | 2017-06-15 | 2018-12-20 | 浙江海正药业股份有限公司 | 杂芳基并嘧啶酮类衍生物、其制备方法及其在医药上用途 |
-
2018
- 2018-01-22 CN CN201810057305.4A patent/CN108341830B/zh active Active
- 2018-01-22 EP EP18741820.7A patent/EP3571205B1/en active Active
- 2018-01-22 KR KR1020197024406A patent/KR102577824B1/ko active Active
- 2018-01-22 WO PCT/CN2018/073581 patent/WO2018133858A1/en not_active Ceased
- 2018-01-22 US US16/476,290 patent/US10759812B2/en active Active
- 2018-01-22 CA CA3049816A patent/CA3049816A1/en active Pending
- 2018-01-22 AU AU2018209006A patent/AU2018209006B2/en active Active
- 2018-01-22 JP JP2019538620A patent/JP7046959B2/ja active Active
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