JP2006515611A5 - - Google Patents
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- Publication number
- JP2006515611A5 JP2006515611A5 JP2006500522A JP2006500522A JP2006515611A5 JP 2006515611 A5 JP2006515611 A5 JP 2006515611A5 JP 2006500522 A JP2006500522 A JP 2006500522A JP 2006500522 A JP2006500522 A JP 2006500522A JP 2006515611 A5 JP2006515611 A5 JP 2006515611A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- phenyl
- agonist
- inhibitors
- alkenyl
- 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.)
- Abandoned
Links
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 18
- 239000000556 agonist Substances 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 239000003814 drug Substances 0.000 claims 9
- 239000003112 inhibitor Substances 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- -1 SO-phenyl Inorganic materials 0.000 claims 3
- 239000005557 antagonist Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- 125000006375 C2-C10 alkynyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 102000018997 Growth Hormone Human genes 0.000 claims 2
- 108010051696 Growth Hormone Proteins 0.000 claims 2
- 229940127470 Lipase Inhibitors Drugs 0.000 claims 2
- 239000000637 Melanocyte-Stimulating Hormone Substances 0.000 claims 2
- 108010007013 Melanocyte-Stimulating Hormones Proteins 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 239000003613 bile acid Substances 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 239000000122 growth hormone Substances 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 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
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- YYGNTYWPHWGJRM-UHFFFAOYSA-N (6E,10E,14E,18E)-2,6,10,15,19,23-hexamethyltetracosa-2,6,10,14,18,22-hexaene Chemical compound CC(C)=CCCC(C)=CCCC(C)=CCCC=C(C)CCC=C(C)CCC=C(C)C YYGNTYWPHWGJRM-UHFFFAOYSA-N 0.000 claims 1
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- KWTSXDURSIMDCE-QMMMGPOBSA-N (S)-amphetamine Chemical compound C[C@H](N)CC1=CC=CC=C1 KWTSXDURSIMDCE-QMMMGPOBSA-N 0.000 claims 1
- SWLAMJPTOQZTAE-UHFFFAOYSA-N 4-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]benzoic acid Chemical class COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(C(O)=O)C=C1 SWLAMJPTOQZTAE-UHFFFAOYSA-N 0.000 claims 1
- 102000004146 ATP citrate synthases Human genes 0.000 claims 1
- 108090000662 ATP citrate synthases Proteins 0.000 claims 1
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 claims 1
- 229940122816 Amylase inhibitor Drugs 0.000 claims 1
- 229940123208 Biguanide Drugs 0.000 claims 1
- 102000013585 Bombesin Human genes 0.000 claims 1
- 108010051479 Bombesin Proteins 0.000 claims 1
- 102000019432 Galanin Human genes 0.000 claims 1
- 101800002068 Galanin Proteins 0.000 claims 1
- 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 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 102000000853 LDL receptors Human genes 0.000 claims 1
- 108010001831 LDL receptors Proteins 0.000 claims 1
- 102000016267 Leptin Human genes 0.000 claims 1
- 108010092277 Leptin Proteins 0.000 claims 1
- 102000004882 Lipase Human genes 0.000 claims 1
- 239000004367 Lipase Substances 0.000 claims 1
- 108090001060 Lipase Proteins 0.000 claims 1
- 229940086609 Lipase inhibitor Drugs 0.000 claims 1
- 108010013563 Lipoprotein Lipase Proteins 0.000 claims 1
- 102100022119 Lipoprotein lipase Human genes 0.000 claims 1
- 102000057248 Lipoprotein(a) Human genes 0.000 claims 1
- 108010033266 Lipoprotein(a) Proteins 0.000 claims 1
- 102000002512 Orexin Human genes 0.000 claims 1
- 102000023984 PPAR alpha Human genes 0.000 claims 1
- 108010028924 PPAR alpha Proteins 0.000 claims 1
- 102000000536 PPAR gamma Human genes 0.000 claims 1
- 108010016731 PPAR gamma Proteins 0.000 claims 1
- 229940124754 PPAR-alpha/gamma agonist Drugs 0.000 claims 1
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 claims 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 claims 1
- 102000004257 Potassium Channel Human genes 0.000 claims 1
- 229940100389 Sulfonylurea Drugs 0.000 claims 1
- BHEOSNUKNHRBNM-UHFFFAOYSA-N Tetramethylsqualene Natural products CC(=C)C(C)CCC(=C)C(C)CCC(C)=CCCC=C(C)CCC(C)C(=C)CCC(C)C(C)=C BHEOSNUKNHRBNM-UHFFFAOYSA-N 0.000 claims 1
- 229940123464 Thiazolidinedione Drugs 0.000 claims 1
- 102100031241 Thioredoxin reductase 2, mitochondrial Human genes 0.000 claims 1
- 108010071769 Thyroid Hormone Receptors beta Proteins 0.000 claims 1
- 102000008219 Uncoupling Protein 2 Human genes 0.000 claims 1
- 108010021111 Uncoupling Protein 2 Proteins 0.000 claims 1
- 102000008200 Uncoupling Protein 3 Human genes 0.000 claims 1
- 108010021098 Uncoupling Protein 3 Proteins 0.000 claims 1
- 102000005630 Urocortins Human genes 0.000 claims 1
- 108010059705 Urocortins Proteins 0.000 claims 1
- 239000006096 absorbing agent Substances 0.000 claims 1
- 238000010521 absorption reaction Methods 0.000 claims 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 claims 1
- 229940025084 amphetamine Drugs 0.000 claims 1
- 239000003392 amylase inhibitor Substances 0.000 claims 1
- 229940125708 antidiabetic agent Drugs 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 210000000227 basophil cell of anterior lobe of hypophysis Anatomy 0.000 claims 1
- 229940125388 beta agonist Drugs 0.000 claims 1
- 150000004283 biguanides Chemical class 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- DNDCVAGJPBKION-DOPDSADYSA-N bombesin Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC=1NC2=CC=CC=C2C=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1NC(=O)CC1)C(C)C)C1=CN=CN1 DNDCVAGJPBKION-DOPDSADYSA-N 0.000 claims 1
- OZVBMTJYIDMWIL-AYFBDAFISA-N bromocriptine Chemical compound C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@]2(C(=O)N3[C@H](C(N4CCC[C@H]4[C@]3(O)O2)=O)CC(C)C)C(C)C)C2)=C3C2=C(Br)NC3=C1 OZVBMTJYIDMWIL-AYFBDAFISA-N 0.000 claims 1
- 229960002802 bromocriptine Drugs 0.000 claims 1
- 230000023852 carbohydrate metabolic process Effects 0.000 claims 1
- 235000021256 carbohydrate metabolism Nutrition 0.000 claims 1
- 230000001906 cholesterol absorption Effects 0.000 claims 1
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N dodecahydrosqualene Natural products CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000002532 enzyme inhibitor Substances 0.000 claims 1
- 229940125753 fibrate Drugs 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 230000002218 hypoglycaemic effect Effects 0.000 claims 1
- 239000000411 inducer Substances 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 229940039781 leptin Drugs 0.000 claims 1
- 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 1
- 235000019421 lipase Nutrition 0.000 claims 1
- 230000037356 lipid metabolism Effects 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 239000002697 lyase inhibitor Substances 0.000 claims 1
- 229950004994 meglitinide Drugs 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- SLZIZIJTGAYEKK-CIJSCKBQSA-N molport-023-220-247 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)CN)[C@@H](C)O)C1=CNC=N1 SLZIZIJTGAYEKK-CIJSCKBQSA-N 0.000 claims 1
- 239000002658 neuropeptide Y receptor agonist Substances 0.000 claims 1
- 230000002474 noradrenergic effect Effects 0.000 claims 1
- 108060005714 orexin Proteins 0.000 claims 1
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 108020001213 potassium channel Proteins 0.000 claims 1
- 230000000862 serotonergic effect Effects 0.000 claims 1
- 239000000952 serotonin receptor agonist Substances 0.000 claims 1
- 239000003772 serotonin uptake inhibitor Substances 0.000 claims 1
- 229940031439 squalene Drugs 0.000 claims 1
- TUHBEKDERLKLEC-UHFFFAOYSA-N squalene Natural products CC(=CCCC(=CCCC(=CCCC=C(/C)CCC=C(/C)CC=C(C)C)C)C)C TUHBEKDERLKLEC-UHFFFAOYSA-N 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 150000001467 thiazolidinediones Chemical class 0.000 claims 1
- 239000000777 urocortin Substances 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10301788A DE10301788B4 (de) | 2003-01-20 | 2003-01-20 | Pharmazeutische Verwendung von Pyrimido[5,4-e][1,2,4]triazin-5,7-dionen |
| PCT/EP2004/000040 WO2004065387A1 (de) | 2003-01-20 | 2004-01-07 | PYRIMIDO[5,4-e][1,2,4]TRIAZIN-5,7-DIONE, VERFAHREN ZU DEREN HERSTELLUNG UND DEREN VERWENDUNG |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006515611A JP2006515611A (ja) | 2006-06-01 |
| JP2006515611A5 true JP2006515611A5 (https=) | 2007-02-22 |
Family
ID=32602696
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006500522A Abandoned JP2006515611A (ja) | 2003-01-20 | 2004-01-07 | ピリミド［５，４−ｅ］［１，２，４］トリアジン−５，７−ジオン、その製造方法及び使用 |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP1587806B1 (https=) |
| JP (1) | JP2006515611A (https=) |
| AT (1) | ATE414086T1 (https=) |
| AU (1) | AU2004205351A1 (https=) |
| BR (1) | BRPI0406828A (https=) |
| CA (1) | CA2513285A1 (https=) |
| DE (2) | DE10301788B4 (https=) |
| MX (1) | MXPA05007201A (https=) |
| WO (1) | WO2004065387A1 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010047982A1 (en) | 2008-10-22 | 2010-04-29 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| JP5557845B2 (ja) | 2008-10-31 | 2014-07-23 | メルク・シャープ・アンド・ドーム・コーポレーション | 糖尿病用剤として有用な新規環状ベンゾイミダゾール誘導体 |
| BRPI0923373B8 (pt) * | 2008-12-12 | 2021-05-25 | Merck Patent Gmbh | composições farmacêuticas compreendendo uma combinação de insulina com derivados de triazina, e uso da dita combinação |
| WO2010072807A2 (en) | 2008-12-23 | 2010-07-01 | Fondation Jerome Lejeune | Inhibitors of cystathionine beta synthase to reduce the neurotoxic overproduction of endogenous hydrogen sulfide |
| US8895596B2 (en) | 2010-02-25 | 2014-11-25 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| BR112013021236B1 (pt) | 2011-02-25 | 2021-05-25 | Merck Sharp & Dohme Corp | composto derivado de benzimidazol, e, composição |
| US9527875B2 (en) | 2012-08-02 | 2016-12-27 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| RU2015140066A (ru) | 2013-02-22 | 2017-03-30 | Мерк Шарп И Доум Корп. | Противодиабетические бициклические соединения |
| WO2014139388A1 (en) | 2013-03-14 | 2014-09-18 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| US11072602B2 (en) | 2016-12-06 | 2021-07-27 | Merck Sharp & Dohme Corp. | Antidiabetic heterocyclic compounds |
| WO2018118670A1 (en) | 2016-12-20 | 2018-06-28 | Merck Sharp & Dohme Corp. | Antidiabetic spirochroman compounds |
| EP4613274A1 (en) | 2024-03-06 | 2025-09-10 | Freie Universität Berlin | Senolytic compounds |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH09255681A (ja) * | 1996-03-25 | 1997-09-30 | Taisho Pharmaceut Co Ltd | 抗腫瘍剤 |
| GB0022079D0 (en) * | 2000-09-08 | 2000-10-25 | Inst Of Molecul & Cell Biology | Novel protein tyrosine phosphatase inhibitor |
-
2003
- 2003-01-20 DE DE10301788A patent/DE10301788B4/de not_active Expired - Fee Related
-
2004
- 2004-01-07 AT AT04700447T patent/ATE414086T1/de not_active IP Right Cessation
- 2004-01-07 MX MXPA05007201A patent/MXPA05007201A/es active IP Right Grant
- 2004-01-07 BR BR0406828-9A patent/BRPI0406828A/pt not_active IP Right Cessation
- 2004-01-07 WO PCT/EP2004/000040 patent/WO2004065387A1/de not_active Ceased
- 2004-01-07 EP EP04700447A patent/EP1587806B1/de not_active Expired - Lifetime
- 2004-01-07 JP JP2006500522A patent/JP2006515611A/ja not_active Abandoned
- 2004-01-07 AU AU2004205351A patent/AU2004205351A1/en not_active Abandoned
- 2004-01-07 CA CA002513285A patent/CA2513285A1/en not_active Abandoned
- 2004-01-07 DE DE502004008447T patent/DE502004008447D1/de not_active Expired - Lifetime
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