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 |
|---|---|---|---|---|
| AU2002352878B2 (en) | 2001-11-27 | 2007-11-22 | Merck Sharp & Dohme Corp. | 2-Aminoquinoline compounds |
| EP1595867A4 (en) | 2003-02-10 | 2008-05-21 | Banyu Pharma Co Ltd | PIPERIDINE DERIVATIVES AS AN ACTIVE ANTAGONIST AT THE RECIPE OF MELANIN CONCENTRATING HORMONE |
| DE602004013427T2 (de) * | 2003-02-28 | 2009-06-04 | Schering Corp. | Biaryltetrahydroisochinolin-piperidine als selektive mch-rezeptor-antagonisten zur behandlung von adipositas und verwandten erkrankungen |
| US7354925B2 (en) | 2004-03-29 | 2008-04-08 | Pfizer Inc. | Alpha aryl or heteroaryl methyl beta piperidino propanamide compounds as ORL1-receptor antagonists |
| TW200630337A (en) * | 2004-10-14 | 2006-09-01 | Euro Celtique Sa | Piperidinyl compounds and the use thereof |
| WO2006104136A1 (ja) * | 2005-03-29 | 2006-10-05 | Banyu Pharmaceutical Co., Ltd. | 非アルコール性脂肪性肝疾患の治療剤、及び非アルコール性脂肪性肝疾患の治療又は予防のための薬剤の候補化合物のスクリーニング方法 |
| WO2007110449A1 (en) * | 2006-03-29 | 2007-10-04 | Euro-Celtique S.A. | Benzenesulfonamide compounds and their use |
| WO2007118854A1 (en) * | 2006-04-13 | 2007-10-25 | Euro-Celtique S.A. | Benzenesulfonamide compounds and the use thereof |
| US8791264B2 (en) * | 2006-04-13 | 2014-07-29 | Purdue Pharma L.P. | Benzenesulfonamide compounds and their use as blockers of calcium channels |
| US20090247560A1 (en) * | 2006-09-28 | 2009-10-01 | Banyu Pharmaceutical Co., Ltd. | Diaryl ketimine derivative |
| WO2008124118A1 (en) * | 2007-04-09 | 2008-10-16 | Purdue Pharma L.P. | Benzenesulfonyl compounds and the use therof |
| WO2009040659A2 (en) * | 2007-09-28 | 2009-04-02 | 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 |
| US9090084B2 (en) | 2010-05-21 | 2015-07-28 | Hewlett-Packard Development Company, L.P. | Fluid ejection device including recirculation system |
| JP2017535545A (ja) * | 2014-11-21 | 2017-11-30 | ラボラトリオス・デル・デエレ・エステベ・エセ・ア | 疼痛に対する多様な活性を有するスピロ−イソキノリン−１，４’−ピペリジン化合物 |
| 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 |
| JP2003527444A (ja) | 2000-03-23 | 2003-09-16 | メルク エンド カムパニー インコーポレーテッド | メラノコルチン受容体アゴニストとして作用するスピロピペリジン誘導体 |
| 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 US US10/607,051 patent/US7109207B2/en not_active Expired - Fee Related
- 2003-06-26 AU AU2003258957A patent/AU2003258957A1/en not_active Abandoned
- 2003-06-26 DE DE60307289T patent/DE60307289T2/de not_active Expired - Lifetime
- 2003-06-26 TW TW092117445A patent/TW200401777A/zh unknown
- 2003-06-26 AR ARP030102294A patent/AR040344A1/es unknown
- 2003-06-26 AT AT03762050T patent/ATE334983T1/de not_active IP Right Cessation
- 2003-06-26 EP EP03762050A patent/EP1532147B1/en not_active Expired - Lifetime
- 2003-06-26 WO PCT/US2003/020088 patent/WO2004002987A1/en not_active Ceased
- 2003-06-26 PE PE2003000647A patent/PE20040749A1/es not_active Application Discontinuation
- 2003-06-26 CA CA2490531A patent/CA2490531C/en not_active Expired - Fee Related
- 2003-06-26 ES ES03762050T patent/ES2266861T3/es not_active Expired - Lifetime
- 2003-06-26 JP JP2004517838A patent/JP4522853B2/ja not_active Expired - Fee Related
- 2003-06-26 MX MXPA05000185A patent/MXPA05000185A/es active IP Right Grant
- 2003-06-26 CN CNB038151936A patent/CN100374440C/zh not_active Expired - Fee Related
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