JP2004530656A5 - - Google Patents
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- Publication number
- JP2004530656A5 JP2004530656A5 JP2002567241A JP2002567241A JP2004530656A5 JP 2004530656 A5 JP2004530656 A5 JP 2004530656A5 JP 2002567241 A JP2002567241 A JP 2002567241A JP 2002567241 A JP2002567241 A JP 2002567241A JP 2004530656 A5 JP2004530656 A5 JP 2004530656A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- phenyl
- substituted
- heteroaryl
- group
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 46
- 125000001072 heteroaryl group Chemical group 0.000 claims 26
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 15
- 239000001257 hydrogen Substances 0.000 claims 15
- 125000001624 naphthyl group Chemical group 0.000 claims 15
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- -1 (1) pyridinyl Chemical group 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 125000002950 monocyclic group Chemical group 0.000 claims 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000001544 thienyl group Chemical group 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 claims 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000004618 benzofuryl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 125000005956 isoquinolyl group Chemical group 0.000 claims 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000005493 quinolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000006704 (C5-C6) cycloalkyl group Chemical group 0.000 claims 1
- ZOOGRGPOEVQQDX-UUOKFMHZSA-N 3',5'-cyclic GMP Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-UUOKFMHZSA-N 0.000 claims 1
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 229940122355 Insulin sensitizer Drugs 0.000 claims 1
- 101710151321 Melanostatin Proteins 0.000 claims 1
- 102400000064 Neuropeptide Y Human genes 0.000 claims 1
- 102000019280 Pancreatic lipases Human genes 0.000 claims 1
- 108050006759 Pancreatic lipases Proteins 0.000 claims 1
- 229940099471 Phosphodiesterase inhibitor Drugs 0.000 claims 1
- 229940100389 Sulfonylurea Drugs 0.000 claims 1
- 239000000670 adrenergic alpha-2 receptor antagonist Substances 0.000 claims 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 230000003579 anti-obesity Effects 0.000 claims 1
- 239000003555 cannabinoid 1 receptor antagonist Substances 0.000 claims 1
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- ZOOGRGPOEVQQDX-UHFFFAOYSA-N cyclic GMP Natural products O1C2COP(O)(=O)OC2C(O)C1N1C=NC2=C1NC(N)=NC2=O ZOOGRGPOEVQQDX-UHFFFAOYSA-N 0.000 claims 1
- 239000003136 dopamine receptor stimulating agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000002608 insulinlike Effects 0.000 claims 1
- 229940125425 inverse agonist Drugs 0.000 claims 1
- HWYHDWGGACRVEH-UHFFFAOYSA-N n-methyl-n-(4-pyrrolidin-1-ylbut-2-ynyl)acetamide Chemical group CC(=O)N(C)CC#CCN1CCCC1 HWYHDWGGACRVEH-UHFFFAOYSA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- URPYMXQQVHTUDU-OFGSCBOVSA-N nucleopeptide y Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(N)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CC=1C=CC(O)=CC=1)C1=CC=C(O)C=C1 URPYMXQQVHTUDU-OFGSCBOVSA-N 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 229940116369 pancreatic lipase Drugs 0.000 claims 1
- 239000002571 phosphodiesterase inhibitor Substances 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 239000002469 receptor inverse agonist Substances 0.000 claims 1
- 239000000952 serotonin receptor agonist Substances 0.000 claims 1
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 229940126158 β3 adrenergic receptor agonist Drugs 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27225901P | 2001-02-28 | 2001-02-28 | |
| PCT/US2002/008002 WO2002067869A2 (en) | 2001-02-28 | 2002-02-25 | Acylated piperidine derivatives as melanocortin-4 receptor agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004530656A JP2004530656A (ja) | 2004-10-07 |
| JP2004530656A5 true JP2004530656A5 (enExample) | 2005-12-22 |
| JP4316238B2 JP4316238B2 (ja) | 2009-08-19 |
Family
ID=23039067
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002567241A Expired - Fee Related JP4316238B2 (ja) | 2001-02-28 | 2002-02-25 | メラノコルチン−４受容体作動薬としてのアシル化ピペリジン誘導体 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US7012084B2 (enExample) |
| EP (1) | EP1385506B1 (enExample) |
| JP (1) | JP4316238B2 (enExample) |
| AT (1) | ATE430565T1 (enExample) |
| AU (1) | AU2002250343B2 (enExample) |
| CA (1) | CA2439119A1 (enExample) |
| DE (1) | DE60232238D1 (enExample) |
| WO (1) | WO2002067869A2 (enExample) |
Families Citing this family (75)
| Publication number | Priority date | Publication date | Assignee | Title |
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| JP4323169B2 (ja) | 2001-02-28 | 2009-09-02 | 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−４受容体作働薬としてのアシル化ピペリジン誘導体 |
| JP4104983B2 (ja) | 2001-02-28 | 2008-06-18 | 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−４受容体作動薬としてのアシル化ピペリジン誘導体 |
| ATE411021T1 (de) | 2001-07-18 | 2008-10-15 | Merck & Co Inc | Überbrückte piperidinderivate als melanocortin- rezeptor-agonisten |
| US6977264B2 (en) | 2001-07-25 | 2005-12-20 | Amgen Inc. | Substituted piperidines and methods of use |
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| US7354923B2 (en) | 2001-08-10 | 2008-04-08 | Palatin Technologies, Inc. | Piperazine melanocortin-specific compounds |
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| US6458790B2 (en) | 2000-03-23 | 2002-10-01 | Merck & Co., Inc. | Substituted piperidines as melanocortin receptor agonists |
| 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 |
| EP1289526A4 (en) | 2000-05-30 | 2005-03-16 | Merck & Co Inc | MELANOCORTIN RECEPTOR AGONISTS |
| US6511994B2 (en) * | 2000-10-11 | 2003-01-28 | Merck & Co., Inc. | Modulators of CCR5 chemokine receptor activity |
| JP4104983B2 (ja) | 2001-02-28 | 2008-06-18 | 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−４受容体作動薬としてのアシル化ピペリジン誘導体 |
| JP4323169B2 (ja) * | 2001-02-28 | 2009-09-02 | 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−４受容体作働薬としてのアシル化ピペリジン誘導体 |
-
2002
- 2002-02-25 AT AT02719251T patent/ATE430565T1/de not_active IP Right Cessation
- 2002-02-25 AU AU2002250343A patent/AU2002250343B2/en not_active Ceased
- 2002-02-25 EP EP02719251A patent/EP1385506B1/en not_active Expired - Lifetime
- 2002-02-25 CA CA002439119A patent/CA2439119A1/en not_active Abandoned
- 2002-02-25 JP JP2002567241A patent/JP4316238B2/ja not_active Expired - Fee Related
- 2002-02-25 WO PCT/US2002/008002 patent/WO2002067869A2/en not_active Ceased
- 2002-02-25 DE DE60232238T patent/DE60232238D1/de not_active Expired - Lifetime
- 2002-02-25 US US10/468,517 patent/US7012084B2/en not_active Expired - Fee Related
-
2005
- 2005-09-30 US US11/239,770 patent/US7700778B2/en not_active Expired - Fee Related
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