JP2017513824A5 - - Google Patents

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Publication number: JP2017513824A5
Authority: JP; Japan
Prior art keywords: obese; item; ether; alkyl; pharmaceutical formulation
Prior art date: 2015-03-26
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

Application number

JP2016558721A

Other languages

English (en)

Japanese (ja)

Other versions

JP2017513824A (ja

Filing date

2015-03-26

Publication date

2018-05-10

2015-03-26 Application filed filed Critical

2015-03-26 Priority claimed from PCT/US2015/022746 external-priority patent/WO2015148802A1/en

2017-06-01 Publication of JP2017513824A publication Critical patent/JP2017513824A/ja

2018-05-10 Publication of JP2017513824A5 publication Critical patent/JP2017513824A5/ja

Status Pending legal-status Critical Current

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

JP2016558721A 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 Pending JP2017513824A (ja)

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 (2)	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 (2)
EP (1)	EP3122347B1 (2)
JP (1)	JP2017513824A (2)
CN (2)	CN117357538A (2)
AU (2)	AU2015235979B2 (2)
BR (1)	BR112016021985B1 (2)
CA (2)	CA3044998A1 (2)
ES (1)	ES2813424T3 (2)
RU (1)	RU2706239C2 (2)
WO (1)	WO2015148802A1 (2)

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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
JP7034078B2 (ja) *	2015-10-23	2022-03-11	イーアールエックスファーマシューティカルズインコーポレイテッド	セラストロールの類似体
US10053693B2 (en)	2016-01-19	2018-08-21	Mubin I. Syed	Method for controlling obesity using minimally invasive means
AU2017285486B2 (en)	2016-06-15	2023-04-27	Targa Biomedical	Reagents, compositions and methods for improving viability and function of cells, tissues and organs
JP2019523245A (ja)	2016-07-04	2019-08-22	厦▲門▼大学	オーファン核内受容体Ｎｕｒ７７のリガンド及びその使用
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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

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WO2008063513A2 (en) *	2006-11-13	2008-05-29	Trustees Of Columbia University In The City Of New York	Selective proteasome inhibitors for treating diabetes
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2015
- 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 RU RU2016141567A patent/RU2706239C2/ru active
- 2015-03-26 AU AU2015235979A patent/AU2015235979B2/en active Active
- 2015-03-26 JP JP2016558721A patent/JP2017513824A/ja active Pending
- 2015-03-26 CA CA2944030A patent/CA2944030C/en active Active
- 2015-03-26 WO PCT/US2015/022746 patent/WO2015148802A1/en not_active Ceased
- 2015-03-26 US US14/669,787 patent/US20150274634A1/en not_active Abandoned
- 2015-03-26 BR BR112016021985-6A patent/BR112016021985B1/pt active IP Right Grant
- 2015-03-26 ES ES15715606T patent/ES2813424T3/es active Active
- 2015-03-26 CN CN201580027586.3A patent/CN107073016A/zh active Pending
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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