CN110709402A - 杂芳基并嘧啶酮类衍生物、其制备方法及其在医药上用途 - Google Patents
杂芳基并嘧啶酮类衍生物、其制备方法及其在医药上用途 Download PDFInfo
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- CN110709402A CN110709402A CN201880030204.6A CN201880030204A CN110709402A CN 110709402 A CN110709402 A CN 110709402A CN 201880030204 A CN201880030204 A CN 201880030204A CN 110709402 A CN110709402 A CN 110709402A
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- heteroaryl
- cycloalkyl
- aryl
- heterocyclyl
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- RLWYQPWCTNGHEF-UHFFFAOYSA-N ethyl 3-aminocyclobutane-1-carboxylate Chemical compound CCOC(=O)C1CC(N)C1 RLWYQPWCTNGHEF-UHFFFAOYSA-N 0.000 description 1
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- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 125000004491 isohexyl group Chemical group C(CCC(C)C)* 0.000 description 1
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 description 1
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
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- 125000000842 isoxazolyl group Chemical group 0.000 description 1
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- OYHQOLUKZRVURQ-IXWMQOLASA-N linoleic acid Natural products CCCCC\C=C/C\C=C\CCCCCCCC(O)=O OYHQOLUKZRVURQ-IXWMQOLASA-N 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 1
- 229910001629 magnesium chloride Inorganic materials 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
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- 235000011090 malic acid Nutrition 0.000 description 1
- LTYOQGRJFJAKNA-VFLPNFFSSA-N malonyl-coa Chemical compound O[C@@H]1[C@H](OP(O)(O)=O)[C@@H](COP(O)(=O)OP(O)(=O)OCC(C)(C)C(O)C(=O)NCCC(=O)NCCSC(=O)CC(O)=O)O[C@H]1N1C2=NC=NC(N)=C2N=C1 LTYOQGRJFJAKNA-VFLPNFFSSA-N 0.000 description 1
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- 229960002510 mandelic acid Drugs 0.000 description 1
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- 239000002184 metal Substances 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- GBMDVOWEEQVZKZ-UHFFFAOYSA-N methanol;hydrate Chemical compound O.OC GBMDVOWEEQVZKZ-UHFFFAOYSA-N 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 210000003470 mitochondria Anatomy 0.000 description 1
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- 238000012986 modification Methods 0.000 description 1
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- 125000002757 morpholinyl group Chemical group 0.000 description 1
- 210000004165 myocardium Anatomy 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 description 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 230000001613 neoplastic effect Effects 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 238000000655 nuclear magnetic resonance spectrum Methods 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
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- 125000005476 oxopyrrolidinyl group Chemical group 0.000 description 1
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- 229940049954 penicillin Drugs 0.000 description 1
- 125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000000865 phosphorylative effect Effects 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical compound C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 description 1
- 230000004962 physiological condition Effects 0.000 description 1
- IWELDVXSEVIIGI-UHFFFAOYSA-N piperazin-2-one Chemical compound O=C1CNCCN1 IWELDVXSEVIIGI-UHFFFAOYSA-N 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- TYJJADVDDVDEDZ-UHFFFAOYSA-M potassium hydrogencarbonate Chemical compound [K+].OC([O-])=O TYJJADVDDVDEDZ-UHFFFAOYSA-M 0.000 description 1
- YCYVPVNGUXMWMP-UHFFFAOYSA-M potassium;acetate;hydrate Chemical compound O.[K+].CC([O-])=O YCYVPVNGUXMWMP-UHFFFAOYSA-M 0.000 description 1
- BYTCDABWEGFPLT-UHFFFAOYSA-L potassium;sodium;dihydroxide Chemical compound [OH-].[OH-].[Na+].[K+] BYTCDABWEGFPLT-UHFFFAOYSA-L 0.000 description 1
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- 229940002612 prodrug Drugs 0.000 description 1
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- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
本发明涉及式(I)所示的杂芳基并嘧啶酮类衍生物、其制备方法及其作为治疗剂的用途,特别是作为乙酰辅酶A羧化酶(ACC)抑制剂的用途,其中式(I)中的各取代基的定义与说明书中的定义相同。
Description
PCT国内申请,说明书已公开。
Claims (19)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
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CN2017104500236 | 2017-06-15 | ||
PCT/CN2018/090804 WO2018228369A1 (zh) | 2017-06-15 | 2018-06-12 | 杂芳基并嘧啶酮类衍生物、其制备方法及其在医药上用途 |
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KR102577824B1 (ko) | 2017-01-22 | 2023-09-13 | 선샤인 레이크 파르마 컴퍼니 리미티드 | 티에노피리미딘 유도체 및 의약에서 이의 용도 |
JP7067725B2 (ja) * | 2017-07-17 | 2022-05-16 | ナンジン ルイジエ ファーマテック カンパニー, リミテッド | Acc阻害剤としての新規な化合物およびそれらの使用 |
CN110959007B (zh) * | 2017-07-26 | 2022-07-01 | 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 |
CN111808077B (zh) * | 2019-04-12 | 2023-05-02 | 浙江海正药业股份有限公司 | 哌嗪酰胺衍生物,其制备方法及其在医药上的用途 |
CN116745299A (zh) * | 2021-02-07 | 2023-09-12 | 正大天晴药业集团股份有限公司 | 噻吩并嘧啶衍生物 |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2013071169A1 (en) * | 2011-11-11 | 2013-05-16 | Nimbus Apollo, Inc. | Acc inhibitors and uses thereof |
CN104470931A (zh) * | 2012-05-21 | 2015-03-25 | 拜耳医药股份有限公司 | 取代的苯并噻吩并嘧啶 |
US20160229865A1 (en) * | 2013-09-18 | 2016-08-11 | Beijing Hanmi Pharmaceutical Co., Ltd. | Compound inhibiting activities of btk and/or jak3 kinases |
Family Cites Families (2)
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AR106472A1 (es) * | 2015-10-26 | 2018-01-17 | Gilead Apollo Llc | Inhibidores de acc y usos de los mismos |
CN108349995B (zh) * | 2015-11-25 | 2021-08-03 | 吉利德阿波罗公司 | 吡唑acc抑制剂及其用途 |
-
2018
- 2018-06-12 WO PCT/CN2018/090804 patent/WO2018228369A1/zh active Application Filing
- 2018-06-12 CN CN201880030204.6A patent/CN110709402B/zh active Active
- 2018-06-13 TW TW107120292A patent/TW201904974A/zh unknown
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Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2013071169A1 (en) * | 2011-11-11 | 2013-05-16 | Nimbus Apollo, Inc. | Acc inhibitors and uses thereof |
CN104105485A (zh) * | 2011-11-11 | 2014-10-15 | 尼普斯阿波罗有限公司 | Acc抑制剂和其用途 |
CN104470931A (zh) * | 2012-05-21 | 2015-03-25 | 拜耳医药股份有限公司 | 取代的苯并噻吩并嘧啶 |
US20160229865A1 (en) * | 2013-09-18 | 2016-08-11 | Beijing Hanmi Pharmaceutical Co., Ltd. | Compound inhibiting activities of btk and/or jak3 kinases |
Non-Patent Citations (1)
Title |
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COLUMBUS, OHIO, US REGISTRY[ONLINE]: "STN检索报告", 《STN REGISTRY》 * |
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