JP2017513824A5 - - Google Patents
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- JP2017513824A5 JP2017513824A5 JP2016558721A JP2016558721A JP2017513824A5 JP 2017513824 A5 JP2017513824 A5 JP 2017513824A5 JP 2016558721 A JP2016558721 A JP 2016558721A JP 2016558721 A JP2016558721 A JP 2016558721A JP 2017513824 A5 JP2017513824 A5 JP 2017513824A5
- Authority
- JP
- Japan
- Prior art keywords
- obese
- item
- ether
- alkyl
- pharmaceutical formulation
- 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.)
- Pending
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims description 24
- 150000001875 compounds Chemical class 0.000 claims description 17
- 210000000577 adipose tissue Anatomy 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 6
- 230000004580 weight loss Effects 0.000 claims description 6
- NRYBAZVQPHGZNS-ZSOCWYAHSA-N leptin Chemical compound O=C([C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(C)C)CCSC)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CS)C(O)=O NRYBAZVQPHGZNS-ZSOCWYAHSA-N 0.000 claims description 5
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 4
- 102000016267 Leptin Human genes 0.000 claims description 3
- 108010092277 Leptin Proteins 0.000 claims description 3
- 235000021316 daily nutritional intake Nutrition 0.000 claims description 3
- 230000001939 inductive effect Effects 0.000 claims description 3
- 229940039781 leptin Drugs 0.000 claims description 3
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 66
- 125000000217 alkyl group Chemical group 0.000 description 47
- 125000003118 aryl group Chemical group 0.000 description 43
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical group NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 description 42
- 229910052736 halogen Inorganic materials 0.000 description 35
- 150000002367 halogens Chemical class 0.000 description 35
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 35
- 150000003568 thioethers Chemical class 0.000 description 34
- IOVCWXUNBOPUCH-UHFFFAOYSA-M Nitrite anion Chemical compound [O-]N=O IOVCWXUNBOPUCH-UHFFFAOYSA-M 0.000 description 33
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 33
- 239000004202 carbamide Substances 0.000 description 33
- 125000004093 cyano group Chemical group *C#N 0.000 description 33
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 31
- 150000002148 esters Chemical class 0.000 description 30
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 28
- 150000001408 amides Chemical class 0.000 description 26
- 150000001412 amines Chemical class 0.000 description 26
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 26
- 125000001424 substituent group Chemical group 0.000 description 26
- BYUYRWRYAISPPF-UHFFFAOYSA-N cyclobutyloxycyclobutane Chemical compound C1CCC1OC1CCC1 BYUYRWRYAISPPF-UHFFFAOYSA-N 0.000 description 24
- 125000001072 heteroaryl group Chemical group 0.000 description 22
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 22
- 125000000753 cycloalkyl group Chemical group 0.000 description 21
- 125000000304 alkynyl group Chemical group 0.000 description 19
- 125000003342 alkenyl group Chemical group 0.000 description 18
- 125000002877 alkyl aryl group Chemical group 0.000 description 18
- -1 -CONHR 7 ) Chemical class 0.000 description 16
- 239000001257 hydrogen Substances 0.000 description 15
- 229910052739 hydrogen Inorganic materials 0.000 description 15
- 238000009472 formulation Methods 0.000 description 11
- 238000000034 method Methods 0.000 description 11
- 239000000203 mixture Substances 0.000 description 11
- 229910052760 oxygen Inorganic materials 0.000 description 11
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 10
- 239000001301 oxygen Substances 0.000 description 10
- 150000003334 secondary amides Chemical class 0.000 description 10
- 150000003511 tertiary amides Chemical class 0.000 description 10
- 206010007134 Candida infections Diseases 0.000 description 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 9
- 150000003140 primary amides Chemical class 0.000 description 9
- 150000003141 primary amines Chemical class 0.000 description 9
- 150000003335 secondary amines Chemical class 0.000 description 9
- 125000000213 sulfino group Chemical group [H]OS(*)=O 0.000 description 9
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 description 9
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 9
- 150000003512 tertiary amines Chemical class 0.000 description 9
- 150000003573 thiols Chemical class 0.000 description 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 6
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
- 230000014101 glucose homeostasis Effects 0.000 description 6
- 150000002431 hydrogen Chemical class 0.000 description 6
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 5
- 239000008103 glucose Substances 0.000 description 5
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 description 5
- 239000000651 prodrug Substances 0.000 description 5
- 229940002612 prodrug Drugs 0.000 description 5
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 4
- 150000002500 ions Chemical class 0.000 description 4
- 229910052757 nitrogen Inorganic materials 0.000 description 4
- 239000008280 blood Substances 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 235000012631 food intake Nutrition 0.000 description 3
- 230000037406 food intake Effects 0.000 description 3
- 125000003831 tetrazolyl group Chemical group 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 239000003472 antidiabetic agent Substances 0.000 description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 2
- 125000003700 epoxy group Chemical group 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- PNIYSYOGEMDKHK-YMEFGNJHSA-N CC(CC[C@](C)(C1)N)(CC2)[C@@H]1[C@](C)(CC[C@]13C)[C@@]2(C)C1=CC=C(C(C)=C1O)C3=CC1=O Chemical compound CC(CC[C@](C)(C1)N)(CC2)[C@@H]1[C@](C)(CC[C@]13C)[C@@]2(C)C1=CC=C(C(C)=C1O)C3=CC1=O PNIYSYOGEMDKHK-YMEFGNJHSA-N 0.000 description 1
- JWEBHSFTHNSVMT-MRHSIXBGSA-N C[C@@](CC[C@](C)(C1)C(O)=O)(CC2)[C@@H]1[C@](C)(CC[C@@]1(C)c(c3c4C)cc(O)c4O)[C@@]2(C)C1=CC3C#N Chemical compound C[C@@](CC[C@](C)(C1)C(O)=O)(CC2)[C@@H]1[C@](C)(CC[C@@]1(C)c(c3c4C)cc(O)c4O)[C@@]2(C)C1=CC3C#N JWEBHSFTHNSVMT-MRHSIXBGSA-N 0.000 description 1
- GOUYEWVPSKOUQK-YDTDWPKOSA-N C[C@@](CC[C@](C)(C1)C(O)=O)(CC2)[C@@H]1[C@](C)(CC[C@@]1(C)c(cc3O)c4c(C)c3O)[C@@]2(C)C1=CC4C#C Chemical compound C[C@@](CC[C@](C)(C1)C(O)=O)(CC2)[C@@H]1[C@](C)(CC[C@@]1(C)c(cc3O)c4c(C)c3O)[C@@]2(C)C1=CC4C#C GOUYEWVPSKOUQK-YDTDWPKOSA-N 0.000 description 1
- GHXOQAKCUGHNOV-DGFGRELFSA-N C[C@@](CC[C@](C)(C1)C(O)=O)(CC2)[C@@H]1[C@](C)(CC[C@@]1(C)c3c4)[C@@]2(C)C1=CC(CC=C)c3c(C)c(O)c4O Chemical compound C[C@@](CC[C@](C)(C1)C(O)=O)(CC2)[C@@H]1[C@](C)(CC[C@@]1(C)c3c4)[C@@]2(C)C1=CC(CC=C)c3c(C)c(O)c4O GHXOQAKCUGHNOV-DGFGRELFSA-N 0.000 description 1
- 0 C[C@@](CC[C@](C)(C1)C(O)=O)(CC2)[C@@]1[C@](C)(CC[C@]13C)[C@@]2(C)C1=CC(*)c(c(C)c1O)c3cc1O Chemical compound C[C@@](CC[C@](C)(C1)C(O)=O)(CC2)[C@@]1[C@](C)(CC[C@]13C)[C@@]2(C)C1=CC(*)c(c(C)c1O)c3cc1O 0.000 description 1
- TXANSOGODOQSJK-JJWQIEBTSA-N C[C@@](CC[C@](C)(C1)c2n[nH]nn2)(CC2)[C@@H]1[C@](C)(CC[C@]13C)[C@@]2(C)C1=CC=C(C(C)=C1O)C3=CC1=O Chemical compound C[C@@](CC[C@](C)(C1)c2n[nH]nn2)(CC2)[C@@H]1[C@](C)(CC[C@]13C)[C@@]2(C)C1=CC=C(C(C)=C1O)C3=CC1=O TXANSOGODOQSJK-JJWQIEBTSA-N 0.000 description 1
- GYUVZGGERRSPQY-UHKCKZGUSA-N C[C@@](CO)(CC[C@]1(C)CC2)C[C@H]1[C@](C)(CC[C@]13C)[C@@]2(C)C1=CC=C(C(C)=C1O)C3=CC1=O Chemical compound C[C@@](CO)(CC[C@]1(C)CC2)C[C@H]1[C@](C)(CC[C@]13C)[C@@]2(C)C1=CC=C(C(C)=C1O)C3=CC1=O GYUVZGGERRSPQY-UHKCKZGUSA-N 0.000 description 1
- 230000003178 anti-diabetic effect Effects 0.000 description 1
- 229940125708 antidiabetic agent Drugs 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 238000011282 treatment Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461970839P | 2014-03-26 | 2014-03-26 | |
| US61/970,839 | 2014-03-26 | ||
| PCT/US2015/022746 WO2015148802A1 (en) | 2014-03-26 | 2015-03-26 | Celastrol and derivatives for the treatment of obesity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017513824A JP2017513824A (ja) | 2017-06-01 |
| JP2017513824A5 true JP2017513824A5 (enExample) | 2018-05-10 |
Family
ID=52823863
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016558721A Pending JP2017513824A (ja) | 2014-03-26 | 2015-03-26 | 肥満の処置のためのセラストロールおよび誘導体 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US20150274634A1 (enExample) |
| EP (1) | EP3122347B1 (enExample) |
| JP (1) | JP2017513824A (enExample) |
| CN (2) | CN107073016A (enExample) |
| AU (2) | AU2015235979B2 (enExample) |
| BR (1) | BR112016021985B1 (enExample) |
| CA (2) | CA2944030C (enExample) |
| ES (1) | ES2813424T3 (enExample) |
| RU (1) | RU2706239C2 (enExample) |
| WO (1) | WO2015148802A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2209911B1 (en) | 2007-10-19 | 2013-10-16 | The Trustees of Columbia University in the City of New York | Dna sequencing with non-fluorescent nucleotide reversible terminators and cleavable label modified nucleotide terminators and a deoxyinosine analogue with a reversible terminator group |
| US20170209408A1 (en) * | 2014-04-03 | 2017-07-27 | The Children's Medical Center Corporation | Hsp90 inhibitors for the treatment of obesity and methods of use thereof |
| CN119241632A (zh) * | 2015-10-23 | 2025-01-03 | Erx制药股份有限公司 | 雷公藤红素的类似物 |
| US10053693B2 (en) | 2016-01-19 | 2018-08-21 | Mubin I. Syed | Method for controlling obesity using minimally invasive means |
| CN109803664A (zh) | 2016-06-15 | 2019-05-24 | 尚特·德扎尔基西安 | 用于改善细胞、组织和器官的活力和功能的试剂、组合物和方法 |
| WO2018006801A1 (zh) * | 2016-07-04 | 2018-01-11 | 厦门大学 | 孤儿核受体Nur77的配体及其用途 |
| CN106243181A (zh) * | 2016-07-29 | 2016-12-21 | 合肥中科玛卡生物技术有限公司 | 一种从苦瓜中提取雷公藤红素的方法 |
| WO2018026810A1 (en) * | 2016-08-03 | 2018-02-08 | Vanderbilt University | Treatment methods using celastrol |
| CN111821308B (zh) * | 2019-04-15 | 2021-10-08 | 中国科学院上海药物研究所 | 雷藤舒在制备用于治疗非酒精性脂肪性肝病的药物中的应用 |
| CN115023431B (zh) * | 2019-09-12 | 2024-02-02 | 藤济(厦门)生物医药科技有限公司 | 三萜类化合物，其药物组合物和在治疗核受体亚家族4组成员1所介导疾病中的用途 |
| CN117860904B (zh) * | 2024-01-10 | 2025-02-18 | 四川大学 | 一种四面体框架核酸-雷公藤红素复合物及其制备方法和应用 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5650167A (en) * | 1995-11-16 | 1997-07-22 | Dawa Incorporated | Method and composition for treating hepatitis B |
| WO2004037180A2 (en) * | 2002-10-21 | 2004-05-06 | Metaproteomics, Llc | Compositions that treat or inhibit pathological conditions associated with inflammatory response |
| CN101272795B (zh) * | 2005-09-30 | 2013-04-03 | 森永乳业株式会社 | 胰岛素抵抗改善剂 |
| US20100240581A1 (en) * | 2006-11-13 | 2010-09-23 | The Trustees Of Columbia University In The City Of New York | Selective proteasome inhibitors for treating diabetes |
| US8641155B2 (en) * | 2007-07-26 | 2014-02-04 | David Lee | Modular furniture system |
| US7776894B2 (en) * | 2007-08-17 | 2010-08-17 | Burnham Institute For Medical Research | Compositions and methods for inhibiting growth and metastasis of melanoma |
| CN101434635B (zh) * | 2007-11-16 | 2012-05-16 | 上海华拓医药科技发展股份有限公司 | 一类具抗肿瘤活性的水溶性酚性三萜化合物及其制备方法 |
| WO2009100037A1 (en) * | 2008-02-01 | 2009-08-13 | The Scripps Research Institute | Methods for treating a condition characterized by dysfunction in protein homeostasis |
| WO2010119674A1 (ja) * | 2009-04-17 | 2010-10-21 | 国立大学法人広島大学 | レプチン抵抗性を改善および／または予防するための薬学的組成物、並びにその使用 |
| WO2012024893A1 (en) * | 2010-08-23 | 2012-03-01 | Suzhou Neupharma Co., Ltd. | Certain chemical entities, compositions, and methods |
| MX336247B (es) * | 2012-01-20 | 2016-01-13 | Actelion Pharmaceuticals Ltd | Derivados de amida heterociclicos como antagonistas del receptor p2x7. |
| CN104812898B (zh) * | 2012-05-25 | 2018-01-30 | 博格有限责任公司 | 通过调节热休克蛋白质(HSP)90‑β治疗代谢综合征的方法 |
| CN111529535A (zh) * | 2012-09-27 | 2020-08-14 | 儿童医学中心公司 | 用于治疗肥胖症的化合物和其使用方法 |
| CN103524592B (zh) * | 2013-09-27 | 2015-08-05 | 安徽医科大学 | 一种雷公藤红素衍生物、该衍生物的生物盐及其制备方法与用途 |
-
2015
- 2015-03-26 CA CA2944030A patent/CA2944030C/en active Active
- 2015-03-26 AU AU2015235979A patent/AU2015235979B2/en active Active
- 2015-03-26 RU RU2016141567A patent/RU2706239C2/ru active
- 2015-03-26 CN CN201580027586.3A patent/CN107073016A/zh active Pending
- 2015-03-26 ES ES15715606T patent/ES2813424T3/es active Active
- 2015-03-26 WO PCT/US2015/022746 patent/WO2015148802A1/en not_active Ceased
- 2015-03-26 JP JP2016558721A patent/JP2017513824A/ja active Pending
- 2015-03-26 BR BR112016021985-6A patent/BR112016021985B1/pt active IP Right Grant
- 2015-03-26 CA CA3044998A patent/CA3044998A1/en not_active Abandoned
- 2015-03-26 EP EP15715606.8A patent/EP3122347B1/en active Active
- 2015-03-26 CN CN202311282376.1A patent/CN117357538A/zh active Pending
- 2015-03-26 US US14/669,787 patent/US20150274634A1/en not_active Abandoned
-
2018
- 2018-02-21 US US15/901,401 patent/US20180194709A1/en not_active Abandoned
- 2018-10-30 US US16/175,613 patent/US20190062254A1/en not_active Abandoned
-
2019
- 2019-04-15 AU AU2019202601A patent/AU2019202601A1/en not_active Abandoned
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