JP2005507918A5 - - Google Patents
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- Publication number
- JP2005507918A5 JP2005507918A5 JP2003537622A JP2003537622A JP2005507918A5 JP 2005507918 A5 JP2005507918 A5 JP 2005507918A5 JP 2003537622 A JP2003537622 A JP 2003537622A JP 2003537622 A JP2003537622 A JP 2003537622A JP 2005507918 A5 JP2005507918 A5 JP 2005507918A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- aryl
- cycloalkyl
- moieties
- 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 76
- 125000000217 alkyl group Chemical group 0.000 claims 67
- 125000003118 aryl group Chemical group 0.000 claims 43
- 125000000753 cycloalkyl group Chemical group 0.000 claims 37
- 239000008194 pharmaceutical composition Substances 0.000 claims 27
- 125000003545 alkoxy group Chemical group 0.000 claims 21
- 150000003839 salts Chemical class 0.000 claims 20
- 125000004438 haloalkoxy group Chemical group 0.000 claims 16
- 125000001188 haloalkyl group Chemical group 0.000 claims 16
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 150000002367 halogens Chemical class 0.000 claims 16
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 15
- 125000003710 aryl alkyl group Chemical group 0.000 claims 12
- 239000012453 solvate Substances 0.000 claims 12
- 208000008589 Obesity Diseases 0.000 claims 10
- 239000000556 agonist Substances 0.000 claims 10
- 235000020824 obesity Nutrition 0.000 claims 10
- 239000002830 appetite depressant Substances 0.000 claims 8
- 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 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 125000002947 alkylene group Chemical group 0.000 claims 7
- 239000003937 drug carrier Substances 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
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- -1 3-cyanophenyl Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 102000004877 Insulin Human genes 0.000 claims 4
- 108090001061 Insulin Proteins 0.000 claims 4
- 239000005557 antagonist Substances 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 230000003054 hormonal effect Effects 0.000 claims 4
- 229940125396 insulin Drugs 0.000 claims 4
- 208000030159 metabolic disease Diseases 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 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 4
- 210000001685 thyroid gland Anatomy 0.000 claims 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 4
- 239000003112 inhibitor Substances 0.000 claims 3
- 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 2
- 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 2
- 208000032841 Bulimia Diseases 0.000 claims 2
- 206010006550 Bulimia nervosa Diseases 0.000 claims 2
- RKWGIWYCVPQPMF-UHFFFAOYSA-N Chloropropamide Chemical compound CCCNC(=O)NS(=O)(=O)C1=CC=C(Cl)C=C1 RKWGIWYCVPQPMF-UHFFFAOYSA-N 0.000 claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 206010022489 Insulin Resistance Diseases 0.000 claims 2
- 102000000536 PPAR gamma Human genes 0.000 claims 2
- 108010016731 PPAR gamma Proteins 0.000 claims 2
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 claims 2
- 229940100389 Sulfonylurea Drugs 0.000 claims 2
- 229960002632 acarbose Drugs 0.000 claims 2
- 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 2
- 229960001761 chlorpropamide Drugs 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 229960004580 glibenclamide Drugs 0.000 claims 2
- 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 2
- 230000002608 insulinlike Effects 0.000 claims 2
- 239000003446 ligand Substances 0.000 claims 2
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 2
- 229960003105 metformin Drugs 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 239000000137 peptide hydrolase inhibitor Substances 0.000 claims 2
- 229960005095 pioglitazone Drugs 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 239000003801 protein tyrosine phosphatase 1B inhibitor Substances 0.000 claims 2
- 230000001225 therapeutic effect Effects 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 229960001641 troglitazone Drugs 0.000 claims 2
- 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 2
- 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 2
- 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
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 229940118148 Aldose reductase inhibitor Drugs 0.000 claims 1
- 102000007390 Glycogen Phosphorylase Human genes 0.000 claims 1
- 108010046163 Glycogen Phosphorylase Proteins 0.000 claims 1
- 108010009384 L-Iditol 2-Dehydrogenase Proteins 0.000 claims 1
- 108090000854 Oxidoreductases Proteins 0.000 claims 1
- 102000004316 Oxidoreductases Human genes 0.000 claims 1
- 102100026974 Sorbitol dehydrogenase Human genes 0.000 claims 1
- 229940123659 Sorbitol dehydrogenase inhibitor Drugs 0.000 claims 1
- 239000003288 aldose reductase inhibitor Substances 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- MNQZXJOMYWMBOU-UHFFFAOYSA-N glyceraldehyde Chemical compound OCC(O)C=O MNQZXJOMYWMBOU-UHFFFAOYSA-N 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 0 N*(*C(CN(CCc(cc1)ccc1-c1cc(C#N)ccc1)C(CCN(CC1)C[C@]1O)=O)=O)c1cc(Cl)cc(Cl)c1 Chemical compound N*(*C(CN(CCc(cc1)ccc1-c1cc(C#N)ccc1)C(CCN(CC1)C[C@]1O)=O)=O)c1cc(Cl)cc(Cl)c1 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34306501P | 2001-10-25 | 2001-10-25 | |
| PCT/US2002/033869 WO2003035055A1 (en) | 2001-10-25 | 2002-10-23 | Mch antagonists for the treatment of obesity |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010031848A Division JP2010155848A (ja) | 2001-10-25 | 2010-02-16 | 肥満治療用のｍｃｈアンタゴニスト |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005507918A JP2005507918A (ja) | 2005-03-24 |
| JP2005507918A5 true JP2005507918A5 (enExample) | 2006-01-05 |
| JP4643141B2 JP4643141B2 (ja) | 2011-03-02 |
Family
ID=23344534
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003537622A Expired - Fee Related JP4643141B2 (ja) | 2001-10-25 | 2002-10-23 | 肥満治療用のｍｃｈアンタゴニスト |
| JP2010031848A Withdrawn JP2010155848A (ja) | 2001-10-25 | 2010-02-16 | 肥満治療用のｍｃｈアンタゴニスト |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010031848A Withdrawn JP2010155848A (ja) | 2001-10-25 | 2010-02-16 | 肥満治療用のｍｃｈアンタゴニスト |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US7045636B2 (enExample) |
| EP (1) | EP1443922A1 (enExample) |
| JP (2) | JP4643141B2 (enExample) |
| KR (1) | KR20040047935A (enExample) |
| CN (1) | CN100548291C (enExample) |
| AR (1) | AR036939A1 (enExample) |
| AU (1) | AU2002337956B2 (enExample) |
| CA (1) | CA2464130C (enExample) |
| HU (1) | HUP0401656A3 (enExample) |
| IL (1) | IL161041A0 (enExample) |
| MX (1) | MXPA04003858A (enExample) |
| WO (1) | WO2003035055A1 (enExample) |
| ZA (1) | ZA200403087B (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1450801A4 (en) * | 2001-11-27 | 2010-10-27 | Merck Sharp & Dohme | 2-aminoquinoline CONNECTIONS |
| US20050009815A1 (en) * | 2001-11-27 | 2005-01-13 | Devita Robert J. | 4-Aminoquinoline compounds |
| US7351719B2 (en) * | 2002-10-31 | 2008-04-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Amide compounds having MCH-antagonistic activity and medicaments comprising these compounds |
| DE10250743A1 (de) * | 2002-10-31 | 2004-05-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Amid-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
| US7727998B2 (en) * | 2003-02-10 | 2010-06-01 | Banyu Pharmaceutical Co., Ltd. | Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient |
| US7304065B2 (en) | 2003-10-01 | 2007-12-04 | The Procter & Gamble Company | Melanin concentrating hormone antagonists |
| US7592373B2 (en) | 2003-12-23 | 2009-09-22 | Boehringer Ingelheim International Gmbh | Amide compounds with MCH antagonistic activity and medicaments comprising these compounds |
| EP2305352A1 (en) | 2004-04-02 | 2011-04-06 | Merck Sharp & Dohme Corp. | 5-alpha-reductase inhibitors for use in the treatment of men with metabolic and anthropometric disorders |
| DE102004017934A1 (de) | 2004-04-14 | 2005-11-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
| US7524862B2 (en) | 2004-04-14 | 2009-04-28 | Boehringer Ingelheim International Gmbh | Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds |
| TW200630337A (en) * | 2004-10-14 | 2006-09-01 | Euro Celtique Sa | Piperidinyl compounds and the use thereof |
| EP1867341A4 (en) * | 2005-03-29 | 2009-07-29 | Banyu Pharma Co Ltd | THERAPEUTIC AGENT FOR NON-ALCOHOLIC FATBERS AND SCREENING METHODS FOR A DRUG-RELATED BIO-TREATMENT FOR THE TREATMENT OR PREVENTION OF NON-ALCOHOLIC FATERS |
| US7678363B2 (en) | 2005-08-26 | 2010-03-16 | Braincells Inc | Methods of treating psychiatric conditions comprising administration of muscarinic agents in combination with SSRIs |
| EP2258358A3 (en) | 2005-08-26 | 2011-09-07 | Braincells, Inc. | Neurogenesis with acetylcholinesterase inhibitor |
| EP2377530A3 (en) | 2005-10-21 | 2012-06-20 | Braincells, Inc. | Modulation of neurogenesis by PDE inhibition |
| EP1942879A1 (en) | 2005-10-31 | 2008-07-16 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
| US20100216734A1 (en) | 2006-03-08 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis by nootropic agents |
| US8247442B2 (en) * | 2006-03-29 | 2012-08-21 | Purdue Pharma L.P. | Benzenesulfonamide compounds and their use |
| US8791264B2 (en) * | 2006-04-13 | 2014-07-29 | Purdue Pharma L.P. | Benzenesulfonamide compounds and their use as blockers of calcium channels |
| WO2007118854A1 (en) * | 2006-04-13 | 2007-10-25 | Euro-Celtique S.A. | Benzenesulfonamide compounds and the use thereof |
| US7858611B2 (en) * | 2006-05-09 | 2010-12-28 | Braincells Inc. | Neurogenesis by modulating angiotensin |
| WO2007134136A2 (en) | 2006-05-09 | 2007-11-22 | Braincells, Inc. | Neurogenesis by modulating angiotensin |
| AU2007292848A1 (en) | 2006-09-08 | 2008-03-13 | Braincells, Inc. | Combinations containing a 4-acylaminopyridine derivative |
| US20100184806A1 (en) | 2006-09-19 | 2010-07-22 | Braincells, Inc. | Modulation of neurogenesis by ppar agents |
| US20080167363A1 (en) * | 2006-12-28 | 2008-07-10 | Braincells, Inc | Modulation of Neurogenesis By Melatoninergic Agents |
| US20080171750A1 (en) * | 2007-01-11 | 2008-07-17 | Braincells, Inc. | Modulation Of Neurogenesis With Use of Modafinil |
| US8244197B2 (en) * | 2007-03-29 | 2012-08-14 | Panasonic Corporation | Receiving device and electronic equipment using the same |
| US8399486B2 (en) * | 2007-04-09 | 2013-03-19 | Purdue Pharma L.P. | Benzenesulfonyl compounds and the use thereof |
| WO2009040659A2 (en) * | 2007-09-28 | 2009-04-02 | Purdue Pharma L.P. | Benzenesulfonamide compounds and the use thereof |
| EP2288345B1 (en) | 2008-04-18 | 2015-06-10 | University College Dublin National University Of Ireland, Dublin | Psycho-pharmaceuticals |
| US20100216805A1 (en) | 2009-02-25 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis using d-cycloserine combinations |
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 |
| US6245746B1 (en) * | 1998-01-23 | 2001-06-12 | Microcide Pharmaceuticals, Inc. | Efflux pump inhibitors |
| WO2001021169A1 (en) * | 1999-09-20 | 2001-03-29 | Takeda Chemical Industries, Ltd. | Mch antagonists |
| US20030022891A1 (en) * | 2000-12-01 | 2003-01-30 | Anandan Palani | MCH antagonists and their use in the treatment of obesity |
| JP4280073B2 (ja) * | 2001-04-12 | 2009-06-17 | ファーマコペイア ドラッグ ディスカバリー， インコーポレイテッド | Ｍｃｈアンタゴニストとして使用されるアリールピペリジンおよびビアリールピペリジン |
-
2002
- 2002-10-23 AR ARP020104004A patent/AR036939A1/es unknown
- 2002-10-23 CA CA2464130A patent/CA2464130C/en not_active Expired - Fee Related
- 2002-10-23 US US10/278,468 patent/US7045636B2/en not_active Expired - Fee Related
- 2002-10-23 CN CNB028210697A patent/CN100548291C/zh not_active Expired - Fee Related
- 2002-10-23 EP EP02773861A patent/EP1443922A1/en not_active Withdrawn
- 2002-10-23 WO PCT/US2002/033869 patent/WO2003035055A1/en not_active Ceased
- 2002-10-23 JP JP2003537622A patent/JP4643141B2/ja not_active Expired - Fee Related
- 2002-10-23 MX MXPA04003858A patent/MXPA04003858A/es active IP Right Grant
- 2002-10-23 HU HU0401656A patent/HUP0401656A3/hu unknown
- 2002-10-23 KR KR10-2004-7005832A patent/KR20040047935A/ko not_active Withdrawn
- 2002-10-23 AU AU2002337956A patent/AU2002337956B2/en not_active Ceased
- 2002-10-23 IL IL16104102A patent/IL161041A0/xx unknown
-
2004
- 2004-04-22 ZA ZA200403087A patent/ZA200403087B/en unknown
-
2010
- 2010-02-16 JP JP2010031848A patent/JP2010155848A/ja not_active Withdrawn
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