JP2010532383A5 - - Google Patents
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- JP2010532383A5 JP2010532383A5 JP2010515241A JP2010515241A JP2010532383A5 JP 2010532383 A5 JP2010532383 A5 JP 2010532383A5 JP 2010515241 A JP2010515241 A JP 2010515241A JP 2010515241 A JP2010515241 A JP 2010515241A JP 2010532383 A5 JP2010532383 A5 JP 2010532383A5
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- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- cycloalkyl
- group
- hydrogen
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 90
- 229910052739 hydrogen Inorganic materials 0.000 claims 48
- 239000001257 hydrogen Substances 0.000 claims 48
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 36
- 125000003277 amino group Chemical group 0.000 claims 30
- 125000000753 cycloalkyl group Chemical group 0.000 claims 30
- 125000001424 substituent group Chemical group 0.000 claims 30
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 24
- 150000002431 hydrogen Chemical class 0.000 claims 24
- 239000000203 mixture Substances 0.000 claims 21
- 238000009472 formulation Methods 0.000 claims 19
- 125000003545 alkoxy group Chemical group 0.000 claims 18
- 125000004429 atom Chemical group 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 16
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 12
- 150000001450 anions Chemical class 0.000 claims 12
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 12
- 150000002367 halogens Chemical class 0.000 claims 12
- FCTRVTQZOUKUIV-MCDZGGTQSA-M potassium;[[[(2r,3s,4r,5r)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate Chemical compound [K+].C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP(O)(=O)OP(O)(=O)OP(O)([O-])=O)[C@@H](O)[C@H]1O FCTRVTQZOUKUIV-MCDZGGTQSA-M 0.000 claims 9
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 claims 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 6
- 229910052783 alkali metal Inorganic materials 0.000 claims 6
- 150000001340 alkali metals Chemical class 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- -1 atom halogen Chemical class 0.000 claims 6
- 239000008280 blood Substances 0.000 claims 6
- 210000004369 blood Anatomy 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 150000001768 cations Chemical class 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 238000004519 manufacturing process Methods 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 229920006395 saturated elastomer Polymers 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 239000011593 sulfur Substances 0.000 claims 6
- 150000003512 tertiary amines Chemical class 0.000 claims 6
- 125000000524 functional group Chemical group 0.000 claims 5
- 239000003472 antidiabetic agent Substances 0.000 claims 4
- 229940125708 antidiabetic agent Drugs 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- YASAKCUCGLMORW-UHFFFAOYSA-N Rosiglitazone Chemical compound C=1C=CC=NC=1N(C)CCOC(C=C1)=CC=C1CC1SC(=O)NC1=O YASAKCUCGLMORW-UHFFFAOYSA-N 0.000 claims 2
- 239000003098 androgen Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
- 230000003914 insulin secretion Effects 0.000 claims 2
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- XUFXOAAUWZOOIT-SXARVLRPSA-N (2R,3R,4R,5S,6R)-5-[[(2R,3R,4R,5S,6R)-5-[[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-1-cyclohex-2-enyl]amino]-2-oxanyl]oxy]-3,4-dihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy]-6-(hydroxymethyl)oxane-2,3,4-triol Chemical group O([C@H]1O[C@H](CO)[C@H]([C@@H]([C@H]1O)O)O[C@H]1O[C@@H]([C@H]([C@H](O)[C@H]1O)N[C@@H]1[C@@H]([C@@H](O)[C@H](O)C(CO)=C1)O)C)[C@@H]1[C@@H](CO)O[C@@H](O)[C@H](O)[C@H]1O XUFXOAAUWZOOIT-SXARVLRPSA-N 0.000 claims 1
- YLLWQNAEYILHLV-UHFFFAOYSA-N 7-chloro-3-methyl-1$l^{6},2,4-benzothiadiazin-2-ide 1,1-dioxide;2-hydroxyethyl(trimethyl)azanium Chemical group C[N+](C)(C)CCO.C1=C(Cl)C=C2S(=O)(=O)[N-]C(C)=NC2=C1 YLLWQNAEYILHLV-UHFFFAOYSA-N 0.000 claims 1
- LBXCUWNYHJDGKP-UHFFFAOYSA-N 7-chloro-3-methyl-2h-1,2,4-benzothiadiazine Chemical compound C1=C(Cl)C=C2SNC(C)=NC2=C1 LBXCUWNYHJDGKP-UHFFFAOYSA-N 0.000 claims 1
- 206010061666 Autonomic neuropathy Diseases 0.000 claims 1
- FAEKWTJYAYMJKF-QHCPKHFHSA-N GlucoNorm Chemical compound C1=C(C(O)=O)C(OCC)=CC(CC(=O)N[C@@H](CC(C)C)C=2C(=CC=CC=2)N2CCCCC2)=C1 FAEKWTJYAYMJKF-QHCPKHFHSA-N 0.000 claims 1
- 208000013016 Hypoglycemia Diseases 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- IBAQFPQHRJAVAV-ULAWRXDQSA-N Miglitol Chemical compound OCCN1C[C@H](O)[C@@H](O)[C@H](O)[C@H]1CO IBAQFPQHRJAVAV-ULAWRXDQSA-N 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 229960002632 acarbose Drugs 0.000 claims 1
- XUFXOAAUWZOOIT-UHFFFAOYSA-N acarviostatin I01 Natural products OC1C(O)C(NC2C(C(O)C(O)C(CO)=C2)O)C(C)OC1OC(C(C1O)O)C(CO)OC1OC1C(CO)OC(O)C(O)C1O XUFXOAAUWZOOIT-UHFFFAOYSA-N 0.000 claims 1
- 239000012190 activator Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 229940125753 fibrate Drugs 0.000 claims 1
- 230000002218 hypoglycaemic effect Effects 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 229960001110 miglitol Drugs 0.000 claims 1
- 229960000698 nateglinide Drugs 0.000 claims 1
- OELFLUMRDSZNSF-BRWVUGGUSA-N nateglinide Chemical compound C1C[C@@H](C(C)C)CC[C@@H]1C(=O)N[C@@H](C(O)=O)CC1=CC=CC=C1 OELFLUMRDSZNSF-BRWVUGGUSA-N 0.000 claims 1
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229960002354 repaglinide Drugs 0.000 claims 1
- 229960004586 rosiglitazone Drugs 0.000 claims 1
- 239000004059 squalene synthase inhibitor Substances 0.000 claims 1
- 230000004936 stimulating effect Effects 0.000 claims 1
- 108090000721 thyroid hormone receptors Proteins 0.000 claims 1
- 102000004217 thyroid hormone receptors Human genes 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 0 CC=[S@]1N(*)C(*)=Nc2cc(*)c(*)cc12 Chemical compound CC=[S@]1N(*)C(*)=Nc2cc(*)c(*)cc12 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94762807P | 2007-07-02 | 2007-07-02 | |
| US94920707P | 2007-07-11 | 2007-07-11 | |
| US95085407P | 2007-07-19 | 2007-07-19 | |
| US98625107P | 2007-11-07 | 2007-11-07 | |
| PCT/US2008/068936 WO2009006483A1 (en) | 2007-07-02 | 2008-07-01 | Salts of potassium atp channel openers and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010532383A JP2010532383A (ja) | 2010-10-07 |
| JP2010532383A5 true JP2010532383A5 (enExample) | 2011-08-18 |
Family
ID=40226526
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010515241A Pending JP2010532383A (ja) | 2007-07-02 | 2008-07-01 | カリウムａｔｐチャネル開口薬の塩およびその使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US20090062264A1 (enExample) |
| EP (1) | EP2170341A4 (enExample) |
| JP (1) | JP2010532383A (enExample) |
| CN (1) | CN101795691A (enExample) |
| AU (1) | AU2008272923A1 (enExample) |
| CA (1) | CA2692160A1 (enExample) |
| WO (1) | WO2009006483A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008510835A (ja) * | 2004-08-25 | 2008-04-10 | エッセンシャリス，インク． | カリウムａｔｐチャンネル開放因子の製剤処方、及びその使用 |
| US9757384B2 (en) | 2005-04-06 | 2017-09-12 | Essentialis, Inc. | Methods for treating subjects with Prader-Willi syndrome or Smith-Magenis syndrome |
| WO2007081521A2 (en) * | 2006-01-05 | 2007-07-19 | Essentialis, Inc. | Salts of potassium atp channel openers and uses thereof |
| EP2343075A1 (en) * | 2010-01-04 | 2011-07-13 | Neurotec Pharma, S.L. | Diazoxide for use in the treatment a central nervous system (CNS) autoimmune demyelinating disease |
| CN103298469A (zh) | 2010-08-31 | 2013-09-11 | 首尔大学校产学协力财团 | PPARδ激动剂的胎儿重编程的用途 |
| WO2013130411A1 (en) * | 2012-02-27 | 2013-09-06 | Essentialis, Inc. | Salts of potassium atp channel openers and uses thereof |
| US20140364367A1 (en) * | 2013-06-08 | 2014-12-11 | Sedogen, Llc | Methods of treating prader willi syndrome and conditions associated with low basal metabolic rate or hyperphagia using a katp channel opener |
| WO2016007921A1 (en) * | 2014-07-10 | 2016-01-14 | Rhodel Island Hospital | Treating arrhythmia with mitochondrial-targeted antioxidants |
| KR102323613B1 (ko) | 2014-11-14 | 2021-11-09 | 에센셜리스 인코포레이티드 | 프라더-윌리 증후군 또는 스미스-마제니스 증후군을 가지는 대상체를 치료하는 방법 |
| US10964950B2 (en) | 2015-03-26 | 2021-03-30 | Taiheiyo Cement Corporation | Secondary battery positive-electrode active material and method for producing same |
| WO2017058869A1 (en) | 2015-09-29 | 2017-04-06 | Acorda Therapeutics, Inc. | Sustained release compositions of 4-aminopyridine |
| CN106518804A (zh) * | 2016-07-31 | 2017-03-22 | 北京梅尔森医药技术开发有限公司 | 一种二氮嗪新晶型及其制备方法 |
| CN115551811B (zh) * | 2020-05-08 | 2024-08-20 | 夏普株式会社 | 含有量子点的水溶液的处理方法 |
| CN115877018A (zh) * | 2022-08-05 | 2023-03-31 | 四川大学华西医院 | 一种孔蛋白在制备检测去氢表雄酮硫酸酯的试剂盒中的应用 |
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| WO2004078113A2 (en) * | 2003-03-04 | 2004-09-16 | Pharmacia Corporation | Treatment and prevention of obesity with cox-2 inhibitors alone or in combination with weight-loss agents |
| WO2004093895A1 (en) * | 2003-04-22 | 2004-11-04 | Pharmacia Corporation | Compositions of a cyclooxygenase-2 selective inhibitor and a potassium ion channel modulator for the treatment of pain, inflammation or inflammation mediated disorders |
| US7378414B2 (en) * | 2003-08-25 | 2008-05-27 | Abbott Laboratories | Anti-infective agents |
| WO2005025511A2 (en) * | 2003-09-10 | 2005-03-24 | Cedars-Sinai Medical Center | Potassium channel mediated delivery of agents through the blood-brain barrier |
| WO2006000607A1 (es) * | 2004-06-23 | 2006-01-05 | Neurotec Pharma, S.L. | Uso de activadores de los canales de katp (kco), en particular el diazóxido, en el tratamiento de la inflamación crónica de snc asociada a algunas efermedades |
| JP2008510835A (ja) * | 2004-08-25 | 2008-04-10 | エッセンシャリス，インク． | カリウムａｔｐチャンネル開放因子の製剤処方、及びその使用 |
| FR2877338B1 (fr) * | 2004-11-03 | 2007-01-26 | Servier Lab | Nouveaux derives de benzothiadiazine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US20060263805A1 (en) * | 2005-03-16 | 2006-11-23 | Andre Terzic | Diagnosing and treating potassium channel defects |
| WO2007081521A2 (en) * | 2006-01-05 | 2007-07-19 | Essentialis, Inc. | Salts of potassium atp channel openers and uses thereof |
| US20070254863A1 (en) * | 2006-04-27 | 2007-11-01 | Jochen Antel | Use of CBx cannabinoid receptor modulators as potassium channel modulators |
-
2008
- 2008-07-01 CN CN200880105223A patent/CN101795691A/zh active Pending
- 2008-07-01 WO PCT/US2008/068936 patent/WO2009006483A1/en not_active Ceased
- 2008-07-01 CA CA002692160A patent/CA2692160A1/en not_active Abandoned
- 2008-07-01 US US12/166,251 patent/US20090062264A1/en not_active Abandoned
- 2008-07-01 AU AU2008272923A patent/AU2008272923A1/en not_active Abandoned
- 2008-07-01 EP EP08772317A patent/EP2170341A4/en not_active Withdrawn
- 2008-07-01 JP JP2010515241A patent/JP2010532383A/ja active Pending
-
2012
- 2012-07-06 US US13/543,665 patent/US20130040942A1/en not_active Abandoned
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