ES2624131T3 - Moduladores heterocíclicos de la síntesis de lípidos - Google Patents
Moduladores heterocíclicos de la síntesis de lípidos Download PDFInfo
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- ES2624131T3 ES2624131T3 ES12754969.9T ES12754969T ES2624131T3 ES 2624131 T3 ES2624131 T3 ES 2624131T3 ES 12754969 T ES12754969 T ES 12754969T ES 2624131 T3 ES2624131 T3 ES 2624131T3
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- alkyl
- cycloalkyl
- compound according
- cancer
- branched
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- 125000000623 heterocyclic group Chemical group 0.000 title description 31
- 230000015572 biosynthetic process Effects 0.000 title description 10
- 238000003786 synthesis reaction Methods 0.000 title description 9
- 150000002632 lipids Chemical class 0.000 title description 6
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 75
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 70
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 65
- 239000001257 hydrogen Substances 0.000 claims abstract description 59
- 150000001875 compounds Chemical class 0.000 claims abstract description 56
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract description 52
- 229910052736 halogen Inorganic materials 0.000 claims abstract description 48
- 150000002367 halogens Chemical class 0.000 claims abstract description 48
- 229910052760 oxygen Inorganic materials 0.000 claims abstract description 21
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims abstract description 20
- 239000001301 oxygen Substances 0.000 claims abstract description 20
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims abstract description 18
- 150000003839 salts Chemical class 0.000 claims abstract description 12
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 24
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- 238000011282 treatment Methods 0.000 claims description 22
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 11
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims description 9
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 7
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 7
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims description 7
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 5
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- 102000015303 Fatty Acid Synthases Human genes 0.000 claims 1
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- 150000002431 hydrogen Chemical group 0.000 description 41
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- 238000000034 method Methods 0.000 description 23
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- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 4
- 125000006539 C12 alkyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 4
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
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- A—HUMAN NECESSITIES
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Applications Claiming Priority (9)
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US201161450482P | 2011-03-08 | 2011-03-08 | |
US201161450561P | 2011-03-08 | 2011-03-08 | |
US201161450482P | 2011-03-08 | ||
US201161450561P | 2011-03-08 | ||
US201161508611P | 2011-07-16 | 2011-07-16 | |
US201161508611P | 2011-07-16 | ||
US201261585642P | 2012-01-11 | 2012-01-11 | |
US201261585642P | 2012-01-11 | ||
PCT/US2012/028309 WO2012122391A1 (en) | 2011-03-08 | 2012-03-08 | Heterocyclic modulators of lipid synthesis |
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ES2624131T3 true ES2624131T3 (es) | 2017-07-13 |
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ES17153778T Active ES2883274T3 (es) | 2011-03-08 | 2012-03-08 | Moduladores heterocíclicos de la síntesis de lípidos |
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US9624173B2 (en) | 2011-03-08 | 2017-04-18 | 3-V Biosciences, Inc. | Heterocyclic modulators of lipid synthesis |
NZ703162A (en) | 2012-07-03 | 2017-05-26 | 3-V Biosciences Inc | Heterocyclic modulators of lipid synthesis |
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JP6409001B2 (ja) * | 2012-12-27 | 2018-10-17 | ドレクセル ユニバーシティ | Hbv感染に対する新規抗ウイルス剤 |
CN104995170A (zh) * | 2013-02-14 | 2015-10-21 | 盖尔德马研究及发展公司 | 合成4-哌啶-4-基-苯-1,3-二醇及其盐以及新型化合物4-(2,4-二羟基-苯基)-4-羟基-哌啶-1-甲酸叔丁酯的方法 |
CN105102449B (zh) * | 2013-03-06 | 2017-06-13 | 豪夫迈·罗氏有限公司 | 抗病毒化合物 |
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WO2015199206A1 (ja) * | 2014-06-27 | 2015-12-30 | 塩野義製薬株式会社 | Trpv4阻害活性を有する6員環誘導体 |
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CN105175277B (zh) * | 2015-05-18 | 2018-04-03 | 中山大学肿瘤防治中心 | 一种3‑磷酸甘油醛脱氢酶的抑制剂及其制备方法和应用 |
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KR102591220B1 (ko) * | 2015-09-04 | 2023-10-18 | 폴리 엠디 에스.알.엘. | 인유두종 바이러스 피부 감염의 치료를 위한 아세틸살리실산을 포함하는 조성물 및 의료 장치 |
CN116139138A (zh) * | 2016-11-11 | 2023-05-23 | 3-V生物科学股份有限公司 | 脂质合成的杂环调节剂 |
CN107043347B (zh) * | 2016-11-18 | 2019-07-02 | 泰州禾益新材料科技有限公司 | 一种阿加曲班中间体(2r,4r)-4-甲基哌啶-2-甲酸乙酯的合成方法 |
CN108456005B (zh) * | 2018-04-20 | 2021-04-27 | 郑州大学 | 石墨抗氧化涂层 |
CN109212056B (zh) * | 2018-08-19 | 2021-05-07 | 丁立平 | 一种测定水源水中三种痕量单卤代甲基苯甲酸的气相色谱-质谱联用法 |
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