JP2004534850A5 - - Google Patents
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- Publication number
- JP2004534850A5 JP2004534850A5 JP2003512363A JP2003512363A JP2004534850A5 JP 2004534850 A5 JP2004534850 A5 JP 2004534850A5 JP 2003512363 A JP2003512363 A JP 2003512363A JP 2003512363 A JP2003512363 A JP 2003512363A JP 2004534850 A5 JP2004534850 A5 JP 2004534850A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- compound
- phe
- optionally substituted
- phenylalanyl
- 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.)
- Withdrawn
Links
- 150000001875 compounds Chemical class 0.000 claims 11
- COLNVLDHVKWLRT-MRVPVSSYSA-N D-phenylalanine Chemical compound OC(=O)[C@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-MRVPVSSYSA-N 0.000 claims 2
- 125000001711 D-phenylalanine group Chemical group [H]N([H])[C@@]([H])(C(=O)[*])C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 125000002059 L-arginyl group Chemical group O=C([*])[C@](N([H])[H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])C(=N[H])N([H])[H] 0.000 claims 1
- 125000002066 L-histidyl group Chemical group [H]N1C([H])=NC(C([H])([H])[C@](C(=O)[*])([H])N([H])[H])=C1[H] 0.000 claims 1
- -1 L-tryptophanyl Chemical group 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
Claims (12)
- 式(I)：
ＨisはＬ-ヒスチジルであり；
Ｄ-Ｐhe(Ｘ)は、パラ位が場合によりＦ、Ｃl、Ｂr、Ｍe及びＯＭeから選択される基で置換されていてもよいＤ-フェニルアラニルであり；
ＡrgはＬ-アルギニルであり；
Ｗは、Ｌ-トリプトファニル又は２-ナフチル-Ｌ-アラニルであり；
ＹとＺの一方は-Ｃ(Ｏ)-であって、他方は-ＮＨ-であり；
ｍは１〜４であり；
ｎは１〜４であるが、但し、ｎ＋ｍは４〜６である]
で表される化合物又はその塩。 - Ｚが-Ｃ(Ｏ)-であって、Ｙが-ＮＨ-である、請求項１に記載の化合物。
- ｍが２である、請求項２に記載の化合物。
- ｎが２〜３である、請求項２に記載の化合物。
- ｍが２であり且つｎが２である、請求項２に記載の化合物。
- Ｄ-Ｐhe(Ｘ)が、パラ位が場合により塩素で置換されていてもよいＤ-フェニルアラニルである、請求項２に記載の化合物。
- Ｙが-Ｃ(Ｏ)-であって、Ｚが-ＮＨ-である、請求項１に記載の化合物。
- ｍが２であり且つｎが２である、請求項７に記載の化合物。
- 下記から選択される請求項１に記載の化合物。
- 下記から選択される請求項１に記載の化合物。
- ヒトにおける肥満を予防又は治療するための医薬の製造における請求項１に記載の化合物の使用。
- 請求項１に記載の化合物及び製薬上許容される担体を含む医薬組成物。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30495801P | 2001-07-12 | 2001-07-12 | |
| PCT/US2002/021443 WO2003006604A2 (en) | 2001-07-12 | 2002-07-08 | Cyclic peptides as potent and selective melanocortin-4 receptor agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004534850A JP2004534850A (ja) | 2004-11-18 |
| JP2004534850A5 true JP2004534850A5 (ja) | 2005-12-22 |
Family
ID=23178678
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003512363A Withdrawn JP2004534850A (ja) | 2001-07-12 | 2002-07-08 | 強力な選択的メラノコルチン−４受容体アゴニストとしての環状ペプチド |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US6960646B2 (ja) |
| EP (1) | EP1409521A2 (ja) |
| JP (1) | JP2004534850A (ja) |
| CA (1) | CA2453027A1 (ja) |
| WO (1) | WO2003006604A2 (ja) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7176279B2 (en) | 2000-06-28 | 2007-02-13 | Palatin Technologies, Inc. | Cyclic peptide compositions and methods for treatment of sexual dysfunction |
| CA2453515A1 (en) | 2001-07-11 | 2003-01-23 | Palatin Technologies, Inc. | Linear and cyclic melanocortin receptor-specific peptides |
| US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| MXPA05011830A (es) | 2003-05-09 | 2006-01-26 | Novo Nordisk As | Peptidos para uso en el tratamiento de la obesidad. |
| WO2005000339A2 (en) * | 2003-06-19 | 2005-01-06 | Eli Lilly And Company | Melanocortin receptor 4(mc4) agonists and their uses |
| EP1644022A1 (en) * | 2003-06-19 | 2006-04-12 | Eli Lilly And Company | Uses of melanocortin-3 receptor (mc3r) agonist peptides |
| WO2005060985A1 (en) * | 2003-12-10 | 2005-07-07 | Merck & Co., Inc. | Inhibition of voluntary ethanol consumption with selective melanocortin 4-receptor agonists |
| WO2005102377A1 (en) * | 2004-03-29 | 2005-11-03 | Eli Lilly And Company | Uses of melanocortin-4 receptor (mc4r) agonist peptides administered by continuous infusion |
| 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 |
| CA2609951A1 (en) * | 2005-05-31 | 2006-12-07 | Yissum Research Development Company Of The Hebrew University Of Jerusale M | Backbone cyclized melanocortin stimulating hormone (.alpha.s) analogs |
| US20070021433A1 (en) | 2005-06-03 | 2007-01-25 | Jian-Qiang Fan | Pharmacological chaperones for treating obesity |
| JP5546451B2 (ja) | 2007-06-04 | 2014-07-09 | シナジー ファーマシューティカルズ インコーポレイテッド | 胃腸の障害、炎症、癌および他の障害の処置に有用なグアニル酸シクラーゼのアゴニスト |
| US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
| AU2009256157B2 (en) | 2008-06-04 | 2014-12-18 | Bausch Health Ireland Limited | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
| NZ590254A (en) | 2008-06-09 | 2012-07-27 | Palatin Technologies Inc | Melanocortin receptor-specific cyclic peptides for treatment of sexual dysfunction |
| WO2010009319A2 (en) | 2008-07-16 | 2010-01-21 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders |
| 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 |
| EP2440572B1 (en) | 2009-06-08 | 2017-04-05 | Palatin Technologies, Inc. | Lactam-bridged melanocortin receptor-specific peptides |
| CN105037502A (zh) | 2009-06-08 | 2015-11-11 | 帕拉丁科技公司 | 黑皮质素受体特异性肽 |
| UY32690A (es) | 2009-06-08 | 2011-01-31 | Astrazeneca Ab | Péptidos específicos para receptores de melanocortina |
| EP2504351A4 (en) | 2009-11-23 | 2013-10-30 | Palatin Technologies Inc | MELANOCORTIN-1 RECEPTOR-SPECIFIC LINEAR PEPTIDE |
| CN102725305B (zh) | 2009-11-23 | 2016-08-24 | 帕拉丁科技公司 | 黑皮质素-1受体特异性环肽 |
| EP2538784B1 (en) | 2010-02-25 | 2015-09-09 | Merck Sharp & Dohme Corp. | Benzimidazole derivatives useful anti-diabetic agents |
| US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
| EP2677869B1 (en) | 2011-02-25 | 2017-11-08 | Merck Sharp & Dohme Corp. | Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents |
| RU2015106909A (ru) | 2012-08-02 | 2016-09-27 | Мерк Шарп И Доум Корп. | Антидиабетические трициклические соединения |
| CA2898482A1 (en) | 2013-02-22 | 2014-08-28 | Linda L. Brockunier | Antidiabetic bicyclic compounds |
| WO2014139388A1 (en) | 2013-03-14 | 2014-09-18 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| CA2905435A1 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Compositions useful for the treatment of gastrointestinal disorders |
| WO2014151206A1 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase and their uses |
| US10011637B2 (en) | 2013-06-05 | 2018-07-03 | Synergy Pharmaceuticals, Inc. | Ultra-pure agonists of guanylate cyclase C, method of making and using same |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| US10899793B2 (en) | 2016-05-27 | 2021-01-26 | Regents Of The University Of Minnesota | Melanocortin ligands and methods of use thereof |
| US11124541B2 (en) | 2016-10-18 | 2021-09-21 | Regents Of The University Of Minnesota | Chimeric melanocortin ligands and methods of use thereof |
| EP3551176A4 (en) | 2016-12-06 | 2020-06-24 | Merck Sharp & Dohme Corp. | ANTIDIABETIC HETEROCYCLIC COMPOUNDS |
| EP3558298A4 (en) | 2016-12-20 | 2020-08-05 | Merck Sharp & Dohme Corp. | ANTIDIABETIC SPIROCHROMAN COMPOUNDS |
| US11332499B2 (en) | 2018-08-16 | 2022-05-17 | Regents Of The University Of Minnesota | Cyclic peptides and methods of use thereof |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5622860A (en) * | 1994-02-17 | 1997-04-22 | The Regents Of The University Of Michigan | Genes encoding melanocortin receptors |
| US6054556A (en) * | 1995-04-10 | 2000-04-25 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Melanocortin receptor antagonists and agonists |
| CA2251520C (en) * | 1997-10-31 | 2003-12-30 | Atsushi Ohta | Pipe connector connection checking assembly |
| HUP0303078A3 (en) * | 2000-08-30 | 2012-02-28 | Hoffmann La Roche | Cyclic peptidies process for their preparation pharmaceutical compositions containing them and their use |
-
2002
- 2002-07-08 WO PCT/US2002/021443 patent/WO2003006604A2/en not_active Application Discontinuation
- 2002-07-08 CA CA002453027A patent/CA2453027A1/en not_active Abandoned
- 2002-07-08 US US10/483,309 patent/US6960646B2/en not_active Expired - Fee Related
- 2002-07-08 JP JP2003512363A patent/JP2004534850A/ja not_active Withdrawn
- 2002-07-08 EP EP02748099A patent/EP1409521A2/en not_active Withdrawn
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