JP2005535641A5 - - Google Patents
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- Publication number
- JP2005535641A5 JP2005535641A5 JP2004517838A JP2004517838A JP2005535641A5 JP 2005535641 A5 JP2005535641 A5 JP 2005535641A5 JP 2004517838 A JP2004517838 A JP 2004517838A JP 2004517838 A JP2004517838 A JP 2004517838A JP 2005535641 A5 JP2005535641 A5 JP 2005535641A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutical composition
- hydrogen
- alkyl
- pharmaceutically acceptable
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 53
- 239000008194 pharmaceutical composition Substances 0.000 claims 21
- 229910052739 hydrogen Inorganic materials 0.000 claims 15
- 239000001257 hydrogen Substances 0.000 claims 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 11
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 208000030814 Eating disease Diseases 0.000 claims 6
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 6
- 235000014632 disordered eating Nutrition 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- -1 -CF 3 Chemical group 0.000 claims 4
- 239000002830 appetite depressant Substances 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 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 4
- 208000008589 Obesity Diseases 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 3
- 208000030159 metabolic disease Diseases 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims 2
- 229940126062 Compound A Drugs 0.000 claims 2
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 239000005557 antagonist Substances 0.000 claims 2
- 239000000883 anti-obesity agent Substances 0.000 claims 2
- 229940125710 antiobesity agent Drugs 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- HYAFETHFCAUJAY-UHFFFAOYSA-N pioglitazone Chemical compound N1=CC(CC)=CC=C1CCOC(C=C1)=CC=C1CC1C(=O)NC(=O)S1 HYAFETHFCAUJAY-UHFFFAOYSA-N 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 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 compound 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
- ROJNYKZWTOHRNU-UHFFFAOYSA-N 2-chloro-4,5-difluoro-n-[[2-methoxy-5-(methylcarbamoylamino)phenyl]carbamoyl]benzamide Chemical compound CNC(=O)NC1=CC=C(OC)C(NC(=O)NC(=O)C=2C(=CC(F)=C(F)C=2)Cl)=C1 ROJNYKZWTOHRNU-UHFFFAOYSA-N 0.000 claims 1
- SXKBTDJJEQQEGE-UHFFFAOYSA-N 3-(3,5-dibromo-4-hydroxy-benzoyl)-2-ethyl-benzofuran-6-sulfonic acid [4-(thiazol-2-ylsulfamoyl)-phenyl]-amide Chemical compound CCC=1OC2=CC(S(=O)(=O)NC=3C=CC(=CC=3)S(=O)(=O)NC=3SC=CN=3)=CC=C2C=1C(=O)C1=CC(Br)=C(O)C(Br)=C1 SXKBTDJJEQQEGE-UHFFFAOYSA-N 0.000 claims 1
- 229940118148 Aldose reductase inhibitor Drugs 0.000 claims 1
- 208000032841 Bulimia Diseases 0.000 claims 1
- 206010006550 Bulimia nervosa Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- RKWGIWYCVPQPMF-UHFFFAOYSA-N Chloropropamide Chemical compound CCCNC(=O)NS(=O)(=O)C1=CC=C(Cl)C=C1 RKWGIWYCVPQPMF-UHFFFAOYSA-N 0.000 claims 1
- QTQMRBZOBKYXCG-MHZLTWQESA-N GW 1929 Chemical compound N([C@@H](CC1=CC=C(C=C1)OCCN(C)C=1N=CC=CC=1)C(O)=O)C1=CC=CC=C1C(=O)C1=CC=CC=C1 QTQMRBZOBKYXCG-MHZLTWQESA-N 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 claims 1
- 229940123659 Sorbitol dehydrogenase inhibitor Drugs 0.000 claims 1
- 229940100389 Sulfonylurea Drugs 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
- 239000003288 aldose reductase inhibitor Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 229960001761 chlorpropamide Drugs 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 150000002222 fluorine compounds Chemical class 0.000 claims 1
- 229960004580 glibenclamide Drugs 0.000 claims 1
- ZNNLBTZKUZBEKO-UHFFFAOYSA-N glyburide Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZNNLBTZKUZBEKO-UHFFFAOYSA-N 0.000 claims 1
- MNQZXJOMYWMBOU-UHFFFAOYSA-N glyceraldehyde Chemical compound OCC(O)C=O MNQZXJOMYWMBOU-UHFFFAOYSA-N 0.000 claims 1
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 1
- 229960003105 metformin Drugs 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical group [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 claims 1
- 229960005095 pioglitazone Drugs 0.000 claims 1
- 239000003801 protein tyrosine phosphatase 1B inhibitor Substances 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- GXPHKUHSUJUWKP-UHFFFAOYSA-N troglitazone Chemical compound C1CC=2C(C)=C(O)C(C)=C(C)C=2OC1(C)COC(C=C1)=CC=C1CC1SC(=O)NC1=O GXPHKUHSUJUWKP-UHFFFAOYSA-N 0.000 claims 1
- 229960001641 troglitazone Drugs 0.000 claims 1
- GXPHKUHSUJUWKP-NTKDMRAZSA-N troglitazone Natural products C([C@@]1(OC=2C(C)=C(C(=C(C)C=2CC1)O)C)C)OC(C=C1)=CC=C1C[C@H]1SC(=O)NC1=O GXPHKUHSUJUWKP-NTKDMRAZSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39181302P | 2002-06-27 | 2002-06-27 | |
| PCT/US2003/020088 WO2004002987A1 (en) | 2002-06-27 | 2003-06-26 | Spirosubstituted piperidines as selective melanin concentrating hormone receptor antagonists for the treatment of obesity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005535641A JP2005535641A (ja) | 2005-11-24 |
| JP2005535641A5 true JP2005535641A5 (https=) | 2006-07-20 |
| JP4522853B2 JP4522853B2 (ja) | 2010-08-11 |
Family
ID=30000757
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004517838A Expired - Fee Related JP4522853B2 (ja) | 2002-06-27 | 2003-06-26 | 肥満の処置のための選択的メラニン濃縮ホルモンレセプターアンタゴニストとしてのスピロ置換ピペリジン |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US7109207B2 (https=) |
| EP (1) | EP1532147B1 (https=) |
| JP (1) | JP4522853B2 (https=) |
| CN (1) | CN100374440C (https=) |
| AR (1) | AR040344A1 (https=) |
| AT (1) | ATE334983T1 (https=) |
| AU (1) | AU2003258957A1 (https=) |
| CA (1) | CA2490531C (https=) |
| DE (1) | DE60307289T2 (https=) |
| ES (1) | ES2266861T3 (https=) |
| MX (1) | MXPA05000185A (https=) |
| PE (1) | PE20040749A1 (https=) |
| TW (1) | TW200401777A (https=) |
| WO (1) | WO2004002987A1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2468015A1 (en) | 2001-11-27 | 2003-06-05 | Merck & Co., Inc. | 2-aminoquinoline compounds |
| US7727998B2 (en) | 2003-02-10 | 2010-06-01 | Banyu Pharmaceutical Co., Ltd. | Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient |
| ES2305735T3 (es) * | 2003-02-28 | 2008-11-01 | Schering Corporation | Biariltetrahidroisoquinolin-piperidinas como antagonistas del receptor de mch selectivos, para el tratamiento de obesidad y trastornos relacionados. |
| CA2563164A1 (en) | 2004-03-29 | 2005-10-06 | Pfizer Inc. | Alpha aryl or heteroaryl methyl beta piperidino propanoic acid compounds as orl1-receptor antagonists |
| TW200630337A (en) * | 2004-10-14 | 2006-09-01 | Euro Celtique Sa | Piperidinyl compounds and the use thereof |
| US20100184648A1 (en) * | 2005-03-29 | 2010-07-22 | Akira Gomori | Therapeutic agent for non-alcoholic fatty liver disease, and screening method for drug candidate compound for treatment or prevention of non-alcoholic fatty liver disease |
| WO2007110449A1 (en) * | 2006-03-29 | 2007-10-04 | Euro-Celtique S.A. | Benzenesulfonamide compounds and their use |
| US8937181B2 (en) * | 2006-04-13 | 2015-01-20 | Purdue Pharma L.P. | Benzenesulfonamide compounds and the use thereof |
| TW200815353A (en) * | 2006-04-13 | 2008-04-01 | Euro Celtique Sa | Benzenesulfonamide compounds and their use |
| AU2007301126A1 (en) * | 2006-09-28 | 2008-04-03 | Banyu Pharmaceutical Co., Ltd. | Diaryl ketimine derivative |
| US8399486B2 (en) * | 2007-04-09 | 2013-03-19 | Purdue Pharma L.P. | Benzenesulfonyl compounds and the use thereof |
| US8765736B2 (en) * | 2007-09-28 | 2014-07-01 | Purdue Pharma L.P. | Benzenesulfonamide compounds and the use thereof |
| US9963739B2 (en) | 2010-05-21 | 2018-05-08 | Hewlett-Packard Development Company, L.P. | Polymerase chain reaction systems |
| WO2011146069A1 (en) | 2010-05-21 | 2011-11-24 | Hewlett-Packard Development Company, L.P. | Fluid ejection device including recirculation system |
| TW201632522A (zh) * | 2014-11-21 | 2016-09-16 | 伊史帝夫博士實驗室股份有限公司 | 針對疼痛具有多模式活性的螺－異喹啉－１，４’－哌啶化合物 |
| CN107312056B (zh) * | 2017-08-24 | 2019-10-25 | 广西师范学院 | 2-(3’-羟基-17’-孕甾烷基)-5-氟苯并咪唑的合成方法 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5908830A (en) | 1996-10-31 | 1999-06-01 | Merck & Co., Inc. | Combination therapy for the treatment of diabetes and obesity |
| TWI279402B (en) * | 1999-08-20 | 2007-04-21 | Banyu Pharma Co Ltd | Spiro compounds having NPY antagonistic activities and agents containing the same |
| CA2381111A1 (en) * | 1999-08-26 | 2001-03-01 | Leah M. Giupponi | Npy antagonists: spiroisoquinolinone derivatives |
| EP1268000A4 (en) * | 2000-03-23 | 2004-12-29 | Merck & Co Inc | SPIROPIPERID DERIVATIVES AS MELANOCORTIN RECEPTOR AGONISTS |
| EP1299362A4 (en) * | 2000-07-05 | 2004-11-03 | Synaptic Pharma Corp | SELECTIVE RECEPTOR ANTAGONISTS OF MELANINE CONCENTRATING HORMON-1 (MCH1) AND THEIR USE |
-
2003
- 2003-06-26 CA CA2490531A patent/CA2490531C/en not_active Expired - Fee Related
- 2003-06-26 AT AT03762050T patent/ATE334983T1/de not_active IP Right Cessation
- 2003-06-26 MX MXPA05000185A patent/MXPA05000185A/es active IP Right Grant
- 2003-06-26 AR ARP030102294A patent/AR040344A1/es unknown
- 2003-06-26 EP EP03762050A patent/EP1532147B1/en not_active Expired - Lifetime
- 2003-06-26 CN CNB038151936A patent/CN100374440C/zh not_active Expired - Fee Related
- 2003-06-26 DE DE60307289T patent/DE60307289T2/de not_active Expired - Lifetime
- 2003-06-26 AU AU2003258957A patent/AU2003258957A1/en not_active Abandoned
- 2003-06-26 WO PCT/US2003/020088 patent/WO2004002987A1/en not_active Ceased
- 2003-06-26 US US10/607,051 patent/US7109207B2/en not_active Expired - Fee Related
- 2003-06-26 ES ES03762050T patent/ES2266861T3/es not_active Expired - Lifetime
- 2003-06-26 PE PE2003000647A patent/PE20040749A1/es not_active Application Discontinuation
- 2003-06-26 TW TW092117445A patent/TW200401777A/zh unknown
- 2003-06-26 JP JP2004517838A patent/JP4522853B2/ja not_active Expired - Fee Related