JP2014510727A5 - - Google Patents
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- JP2014510727A5 JP2014510727A5 JP2013557870A JP2013557870A JP2014510727A5 JP 2014510727 A5 JP2014510727 A5 JP 2014510727A5 JP 2013557870 A JP2013557870 A JP 2013557870A JP 2013557870 A JP2013557870 A JP 2013557870A JP 2014510727 A5 JP2014510727 A5 JP 2014510727A5
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- JP
- Japan
- Prior art keywords
- cancer
- composition
- alkyl
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- item
- 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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- 150000001875 compounds Chemical class 0.000 claims description 112
- 125000000217 alkyl group Chemical group 0.000 claims description 79
- 229910052736 halogen Inorganic materials 0.000 claims description 46
- 150000002367 halogens Chemical class 0.000 claims description 46
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 39
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 30
- 239000000203 mixture Substances 0.000 claims description 22
- 229910052739 hydrogen Inorganic materials 0.000 claims description 21
- 201000011510 cancer Diseases 0.000 claims description 20
- 229910052760 oxygen Inorganic materials 0.000 claims description 17
- 239000001301 oxygen Substances 0.000 claims description 16
- MYMOFIZGZYHOMD-UHFFFAOYSA-N oxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims description 16
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 15
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 11
- 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 10
- -1 R 22 is H Chemical compound 0.000 claims description 9
- 229910052799 carbon Inorganic materials 0.000 claims description 9
- 206010047461 Viral infection Diseases 0.000 claims description 7
- 208000001756 Virus Disease Diseases 0.000 claims description 7
- 230000017613 viral reproduction Effects 0.000 claims description 7
- 125000001188 haloalkyl group Chemical group 0.000 claims description 5
- 150000003839 salts Chemical class 0.000 claims description 5
- 239000011780 sodium chloride Substances 0.000 claims description 5
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 4
- 102100008329 FASN Human genes 0.000 claims description 4
- 101710008102 FASN Proteins 0.000 claims description 4
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 4
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims description 4
- 208000005176 Hepatitis C Diseases 0.000 claims description 3
- 239000001257 hydrogen Substances 0.000 claims description 3
- 125000004435 hydrogen atoms Chemical class [H]* 0.000 claims description 3
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000000546 pharmaceutic aid Substances 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 210000001672 Ovary Anatomy 0.000 claims 2
- 210000001185 Bone Marrow Anatomy 0.000 claims 1
- 210000000988 Bone and Bones Anatomy 0.000 claims 1
- 210000004556 Brain Anatomy 0.000 claims 1
- 210000000481 Breast Anatomy 0.000 claims 1
- 210000001072 Colon Anatomy 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 210000003238 Esophagus Anatomy 0.000 claims 1
- 210000001508 Eye Anatomy 0.000 claims 1
- 210000002216 Heart Anatomy 0.000 claims 1
- 210000003734 Kidney Anatomy 0.000 claims 1
- 210000004185 Liver Anatomy 0.000 claims 1
- 210000004072 Lung Anatomy 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 210000001165 Lymph Nodes Anatomy 0.000 claims 1
- 210000002027 Muscle, Skeletal Anatomy 0.000 claims 1
- 210000002464 Muscle, Smooth, Vascular Anatomy 0.000 claims 1
- 206010061306 Nasopharyngeal cancer Diseases 0.000 claims 1
- 210000001989 Nasopharynx Anatomy 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010031096 Oropharyngeal cancer Diseases 0.000 claims 1
- 210000003300 Oropharynx Anatomy 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 210000000496 Pancreas Anatomy 0.000 claims 1
- 210000002307 Prostate Anatomy 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 206010038038 Rectal cancer Diseases 0.000 claims 1
- 210000000664 Rectum Anatomy 0.000 claims 1
- 210000003079 Salivary Glands Anatomy 0.000 claims 1
- 206010061934 Salivary gland cancer Diseases 0.000 claims 1
- 210000000278 Spinal Cord Anatomy 0.000 claims 1
- 210000002784 Stomach Anatomy 0.000 claims 1
- 210000001550 Testis Anatomy 0.000 claims 1
- 210000001685 Thyroid Gland Anatomy 0.000 claims 1
- 210000000626 Ureter Anatomy 0.000 claims 1
- 210000003932 Urinary Bladder Anatomy 0.000 claims 1
- 201000005216 brain cancer Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 201000010453 lymph node cancer Diseases 0.000 claims 1
- 201000006958 oropharynx cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 210000001519 tissues Anatomy 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 4
- 125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 0 *C(CC1)(CCN1C(c1cc(C2=*I=C(*)N2)c(*)cc1*)=O)c1cc(*)c(*)c(*)c1 Chemical compound *C(CC1)(CCN1C(c1cc(C2=*I=C(*)N2)c(*)cc1*)=O)c1cc(*)c(*)c(*)c1 0.000 description 1
- 230000000840 anti-viral Effects 0.000 description 1
- 125000005418 aryl aryl group Chemical group 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 1
- 125000001072 heteroaryl group Chemical group 0.000 description 1
- 125000005842 heteroatoms Chemical group 0.000 description 1
- 125000000623 heterocyclic group Chemical group 0.000 description 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- WYURNTSHIVDZCO-UHFFFAOYSA-N tetrahydrofuran Substances C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161450482P | 2011-03-08 | 2011-03-08 | |
| US201161450561P | 2011-03-08 | 2011-03-08 | |
| US61/450,482 | 2011-03-08 | ||
| US61/450,561 | 2011-03-08 | ||
| US201161508611P | 2011-07-16 | 2011-07-16 | |
| US61/508,611 | 2011-07-16 | ||
| US201261585642P | 2012-01-11 | 2012-01-11 | |
| US61/585,642 | 2012-01-11 | ||
| PCT/US2012/028309 WO2012122391A1 (en) | 2011-03-08 | 2012-03-08 | Heterocyclic modulators of lipid synthesis |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016018610A Division JP6061437B2 (ja) | 2011-03-08 | 2016-02-03 | 脂質合成の複素環式モジュレーター |
| JP2016018611A Division JP2016074742A (ja) | 2011-03-08 | 2016-02-03 | 脂質合成の複素環式モジュレーター |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014510727A JP2014510727A (ja) | 2014-05-01 |
| JP2014510727A5 true JP2014510727A5 (US20040106767A1-20040603-C00005.png) | 2015-04-30 |
| JP5973473B2 JP5973473B2 (ja) | 2016-08-23 |
Family
ID=48221725
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013557870A Active JP5973473B2 (ja) | 2011-03-08 | 2012-03-08 | 脂質合成の複素環式モジュレーター |
| JP2016018610A Active JP6061437B2 (ja) | 2011-03-08 | 2016-02-03 | 脂質合成の複素環式モジュレーター |
| JP2016018611A Pending JP2016074742A (ja) | 2011-03-08 | 2016-02-03 | 脂質合成の複素環式モジュレーター |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016018610A Active JP6061437B2 (ja) | 2011-03-08 | 2016-02-03 | 脂質合成の複素環式モジュレーター |
| JP2016018611A Pending JP2016074742A (ja) | 2011-03-08 | 2016-02-03 | 脂質合成の複素環式モジュレーター |
Country Status (21)
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20170119786A1 (en) | 2011-03-08 | 2017-05-04 | 3-V Biosciences, Inc. | Heterocyclic modulators of lipid synthesis |
| US8871790B2 (en) | 2011-03-08 | 2014-10-28 | 3-V Biosciences, Inc. | Heterocyclic modulators of lipid synthesis |
| 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 |
| AR092211A1 (es) * | 2012-09-24 | 2015-04-08 | Merck Patent Ges Mit Beschränkter Haftung | Derivados de hidropirrolopirrol |
| EA201591220A1 (ru) | 2012-12-27 | 2016-01-29 | Дрексел Юниверсити | Новые противовирусные агенты против инфекции вирусом гепатита в |
| BR112015019208A2 (pt) * | 2013-02-14 | 2017-07-18 | Galderma Res & Dev | processo de síntese |
| WO2014135495A1 (en) * | 2013-03-06 | 2014-09-12 | F. Hoffmann-La Roche Ag | Antiviral compounds |
| DK2968316T3 (da) | 2013-03-13 | 2019-10-07 | Forma Therapeutics Inc | 2-hydroxy-1-{4-[(4-phenylphenyl)carbonyl]piperazin-1-yl}ethan-1-on-derivater og relaterede forbindelser som fedtsyresyntase (fasn)-inhibitorer til behandlingen af cancer |
| CA2934251C (en) * | 2013-12-20 | 2024-01-02 | 3-V Biosciences, Inc. | A combination of heterocyclic modulators of lipid synthesis and chemotherapeutic drugs in treatment of cancer |
| NZ721780A (en) | 2014-01-07 | 2022-01-28 | Sagimet Biosciences Inc | Heterocyclic modulators of lipid synthesis for use against cancer and viral infections |
| CN104774204A (zh) * | 2014-01-15 | 2015-07-15 | 鲁南贝特制药有限公司 | 一种制备奈韦拉平及其中间体的方法 |
| 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 |
| WO2016025816A1 (en) * | 2014-08-15 | 2016-02-18 | 3-V Biosciences, Inc. | Fatty acid synthase inhibitor for use in the treatment of drug resistant cancer |
| WO2016149271A1 (en) * | 2015-03-19 | 2016-09-22 | 3-V Biosciences, Inc. | Heterocyclic modulators of lipid synthesis |
| 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 |
| AU2016280255A1 (en) | 2015-06-18 | 2018-02-08 | Cephalon, Inc. | 1, 4-substituted piperidine derivatives |
| US10919875B2 (en) | 2015-06-18 | 2021-02-16 | 89Bio Ltd | Substituted 4-benzyl and 4-benzoyl piperidine derivatives |
| JP6855481B2 (ja) * | 2015-09-04 | 2021-04-07 | ポリ・エムディー・エス.アール.エル.Poli Md S.R.L. | ヒトパピローマウイルス皮膚感染の治療のためのアセチルサリチル酸を含む組成物および医用デバイス |
| CA3043308A1 (en) * | 2016-11-11 | 2018-05-17 | 3-V Biosciences, Inc. | Heterocyclic modulators of lipid synthesis |
| 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 |
| TWI767148B (zh) | 2018-10-10 | 2022-06-11 | 美商弗瑪治療公司 | 抑制脂肪酸合成酶(fasn) |
| US10793554B2 (en) | 2018-10-29 | 2020-10-06 | Forma Therapeutics, Inc. | Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone |
| WO2021229533A1 (en) * | 2020-05-14 | 2021-11-18 | Palani Llc | A fatty acid based composition for treatment and/or prevention of enveloped-virus related infections |
| CN114469945A (zh) * | 2020-10-28 | 2022-05-13 | 歌礼生物科技（杭州）有限公司 | 脂肪酸合酶抑制剂的用途和药物组合物 |
| CN113584044A (zh) * | 2021-08-28 | 2021-11-02 | 青岛农业大学 | 一种牙鲆socs3基因及其真核表达载体、表达系统和异源表达方法 |
| WO2024069574A1 (en) * | 2022-10-01 | 2024-04-04 | Assia Chemical Industries Ltd. | Solid state forms of denifanstat |
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| US4906474A (en) | 1983-03-22 | 1990-03-06 | Massachusetts Institute Of Technology | Bioerodible polyanhydrides for controlled drug delivery |
| US4789734A (en) | 1985-08-06 | 1988-12-06 | La Jolla Cancer Research Foundation | Vitronectin specific cell receptor derived from mammalian mesenchymal tissue |
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| AU610083B2 (en) | 1986-08-18 | 1991-05-16 | Clinical Technologies Associates, Inc. | Delivery systems for pharmacological agents |
| US6024983A (en) | 1986-10-24 | 2000-02-15 | Southern Research Institute | Composition for delivering bioactive agents for immune response and its preparation |
| US5075109A (en) | 1986-10-24 | 1991-12-24 | Southern Research Institute | Method of potentiating an immune response |
| US5001139A (en) | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US4992445A (en) | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
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| EP1959951B1 (en) * | 2005-12-01 | 2009-12-23 | F. Hoffmann-la Roche AG | Heteroaryl substituted piperidine derivatives as l-cpt1 inhibitors |
| EP2061479A4 (en) * | 2006-09-05 | 2010-08-04 | Bipar Sciences Inc | FETTIC ACID SYNTHESIS INHIBITED BY PARP HEMMER AND TREATMENT PROCEDURES THEREWITH |
| WO2008059214A1 (en) * | 2006-11-13 | 2008-05-22 | Astrazeneca Ab | Bisamlde derivatives and use thereof as fatty acid synthase inhibitors |
| TW200831092A (en) * | 2006-12-21 | 2008-08-01 | Astrazeneca Ab | Therapeutic agents |
| WO2008075077A1 (en) * | 2006-12-21 | 2008-06-26 | Astrazeneca Ab | Piperidine derivatives for the treatment of obesity |
| TW200833663A (en) * | 2006-12-21 | 2008-08-16 | Astrazeneca Ab | Therapeutic agents |
-
2012
- 2012-03-08 SI SI201230912A patent/SI2683244T1/sl unknown
- 2012-03-08 PT PT127549699T patent/PT2683244T/pt unknown
- 2012-03-08 AU AU2012225390A patent/AU2012225390B2/en active Active
- 2012-03-08 PL PL12754969T patent/PL2683244T3/pl unknown
- 2012-03-08 EA EA201391290A patent/EA031193B1/ru unknown
- 2012-03-08 DK DK12754969.9T patent/DK2683244T3/en active
- 2012-03-08 JP JP2013557870A patent/JP5973473B2/ja active Active
- 2012-03-08 EP EP12754969.9A patent/EP2683244B1/en active Active
- 2012-03-08 HU HUE12754969A patent/HUE032459T2/en unknown
- 2012-03-08 BR BR122015005122-3A patent/BR122015005122B1/pt active IP Right Grant
- 2012-03-08 MX MX2016009579A patent/MX369388B/es unknown
- 2012-03-08 EP EP17153778.0A patent/EP3190108B1/en active Active
- 2012-03-08 LT LTEP12754969.9T patent/LT2683244T/lt unknown
- 2012-03-08 CN CN201510354353.6A patent/CN105001225B/zh active Active
- 2012-03-08 BR BR112013022761A patent/BR112013022761B8/pt active IP Right Grant
- 2012-03-08 BR BR122015005121-5A patent/BR122015005121B1/pt active IP Right Grant
- 2012-03-08 ES ES12754969.9T patent/ES2624131T3/es active Active
- 2012-03-08 WO PCT/US2012/028309 patent/WO2012122391A1/en active Application Filing
- 2012-03-08 KR KR1020187017297A patent/KR101968058B1/ko active IP Right Grant
- 2012-03-08 CA CA2829082A patent/CA2829082C/en active Active
- 2012-03-08 CN CN201280020832.9A patent/CN103561576B/zh active Active
- 2012-03-08 KR KR1020137026499A patent/KR101930106B1/ko active IP Right Grant
- 2012-03-08 ES ES17153778T patent/ES2883274T3/es active Active
- 2012-03-08 MX MX2013010170A patent/MX342287B/es active IP Right Grant
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2013
- 2013-09-03 IL IL228276A patent/IL228276A/en active IP Right Grant
- 2013-09-04 ZA ZA2013/06655A patent/ZA201306655B/en unknown
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2016
- 2016-02-03 JP JP2016018610A patent/JP6061437B2/ja active Active
- 2016-02-03 JP JP2016018611A patent/JP2016074742A/ja active Pending
- 2016-04-11 HK HK16104111.8A patent/HK1216310A1/zh unknown
- 2016-09-13 IL IL247804A patent/IL247804B/en active IP Right Grant
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2017
- 2017-03-28 HR HRP20170500TT patent/HRP20170500T1/hr unknown
