JP2003522184A5 - - Google Patents
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- JP2003522184A5 JP2003522184A5 JP2001557901A JP2001557901A JP2003522184A5 JP 2003522184 A5 JP2003522184 A5 JP 2003522184A5 JP 2001557901 A JP2001557901 A JP 2001557901A JP 2001557901 A JP2001557901 A JP 2001557901A JP 2003522184 A5 JP2003522184 A5 JP 2003522184A5
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- Prior art keywords
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- peptide
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- 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.)
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- 108090000765 processed proteins & peptides Proteins 0.000 description 43
- 150000001875 compounds Chemical class 0.000 description 20
- 108020003175 receptors Proteins 0.000 description 16
- 102000005962 receptors Human genes 0.000 description 16
- FSYKKLYZXJSNPZ-UHFFFAOYSA-N sarcosine Chemical compound C[NH2+]CC([O-])=O FSYKKLYZXJSNPZ-UHFFFAOYSA-N 0.000 description 12
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- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 description 10
- 239000004475 Arginine Substances 0.000 description 9
- 229960003121 arginine Drugs 0.000 description 9
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 9
- 150000003839 salts Chemical class 0.000 description 9
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 8
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 7
- LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-norleucine Chemical compound CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 description 7
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- 108010077895 Sarcosine Proteins 0.000 description 6
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- 125000006239 protecting group Chemical group 0.000 description 6
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- ONIBWKKTOPOVIA-SCSAIBSYSA-N D-Proline Chemical compound OC(=O)[C@H]1CCCN1 ONIBWKKTOPOVIA-SCSAIBSYSA-N 0.000 description 5
- LRQKBLKVPFOOQJ-RXMQYKEDSA-N D-norleucine Chemical compound CCCC[C@@H](N)C(O)=O LRQKBLKVPFOOQJ-RXMQYKEDSA-N 0.000 description 5
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 description 5
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 description 4
- BVAUMRCGVHUWOZ-ZETCQYMHSA-N (2s)-2-(cyclohexylazaniumyl)propanoate Chemical compound OC(=O)[C@H](C)NC1CCCCC1 BVAUMRCGVHUWOZ-ZETCQYMHSA-N 0.000 description 4
- 239000004471 Glycine Substances 0.000 description 4
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 description 4
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 description 4
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 description 4
- 102000029828 Melanin-concentrating hormone receptor Human genes 0.000 description 4
- 108010047068 Melanin-concentrating hormone receptor Proteins 0.000 description 4
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 description 4
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 4
- 150000001413 amino acids Chemical class 0.000 description 4
- 229960000310 isoleucine Drugs 0.000 description 4
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 229960001153 serine Drugs 0.000 description 4
- 150000008574 D-amino acids Chemical class 0.000 description 3
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 description 3
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 description 3
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 description 3
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 3
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 3
- 239000004472 Lysine Substances 0.000 description 3
- 229940024606 amino acid Drugs 0.000 description 3
- 125000003277 amino group Chemical group 0.000 description 3
- 210000004899 c-terminal region Anatomy 0.000 description 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 3
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 3
- 229960002885 histidine Drugs 0.000 description 3
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 description 3
- 235000008729 phenylalanine Nutrition 0.000 description 3
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 3
- FPDYKABXINADKS-LURJTMIESA-N (2s)-2-(methylazaniumyl)hexanoate Chemical compound CCCC[C@H](NC)C(O)=O FPDYKABXINADKS-LURJTMIESA-N 0.000 description 2
- LJRDOKAZOAKLDU-UDXJMMFXSA-N (2s,3s,4r,5r,6r)-5-amino-2-(aminomethyl)-6-[(2r,3s,4r,5s)-5-[(1r,2r,3s,5r,6s)-3,5-diamino-2-[(2s,3r,4r,5s,6r)-3-amino-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6-hydroxycyclohexyl]oxy-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl]oxyoxane-3,4-diol;sulfuric ac Chemical compound OS(O)(=O)=O.N[C@@H]1[C@@H](O)[C@H](O)[C@H](CN)O[C@@H]1O[C@H]1[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](N)C[C@@H](N)[C@@H]2O)O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)N)O[C@@H]1CO LJRDOKAZOAKLDU-UDXJMMFXSA-N 0.000 description 2
- XWHHYOYVRVGJJY-UHFFFAOYSA-N 4-fluorophenylalanine Chemical compound OC(=O)C(N)CC1=CC=C(F)C=C1 XWHHYOYVRVGJJY-UHFFFAOYSA-N 0.000 description 2
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 description 2
- DCXYFEDJOCDNAF-UWTATZPHSA-N D-Asparagine Chemical compound OC(=O)[C@H](N)CC(N)=O DCXYFEDJOCDNAF-UWTATZPHSA-N 0.000 description 2
- XUJNEKJLAYXESH-UWTATZPHSA-N D-Cysteine Chemical compound SC[C@@H](N)C(O)=O XUJNEKJLAYXESH-UWTATZPHSA-N 0.000 description 2
- MTCFGRXMJLQNBG-UWTATZPHSA-N D-Serine Chemical compound OC[C@@H](N)C(O)=O MTCFGRXMJLQNBG-UWTATZPHSA-N 0.000 description 2
- ODKSFYDXXFIFQN-SCSAIBSYSA-N D-arginine Chemical compound OC(=O)[C@H](N)CCCNC(N)=N ODKSFYDXXFIFQN-SCSAIBSYSA-N 0.000 description 2
- 229930195710 D‐cysteine Natural products 0.000 description 2
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 description 2
- FFFHZYDWPBMWHY-VKHMYHEASA-N L-homocysteine Chemical compound OC(=O)[C@@H](N)CCS FFFHZYDWPBMWHY-VKHMYHEASA-N 0.000 description 2
- MRAUNPAHJZDYCK-BYPYZUCNSA-N L-nitroarginine Chemical compound OC(=O)[C@@H](N)CCCNC(=N)N[N+]([O-])=O MRAUNPAHJZDYCK-BYPYZUCNSA-N 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 235000001014 amino acid Nutrition 0.000 description 2
- 229960001230 asparagine Drugs 0.000 description 2
- 235000009582 asparagine Nutrition 0.000 description 2
- -1 aspartic Chemical compound 0.000 description 2
- 229940021745 d- arginine Drugs 0.000 description 2
- 229940021746 d- serine Drugs 0.000 description 2
- 229960001639 penicillamine Drugs 0.000 description 2
- VKBLQCDGTHFOLS-NSHDSACASA-N (2s)-2-(4-benzoylanilino)propanoic acid Chemical compound C1=CC(N[C@@H](C)C(O)=O)=CC=C1C(=O)C1=CC=CC=C1 VKBLQCDGTHFOLS-NSHDSACASA-N 0.000 description 1
- ROHFNLRQFUQHCH-RXMQYKEDSA-N D-leucine Chemical compound CC(C)C[C@@H](N)C(O)=O ROHFNLRQFUQHCH-RXMQYKEDSA-N 0.000 description 1
- RHGKLRLOHDJJDR-BYPYZUCNSA-N L-citrulline Chemical compound NC(=O)NCCC[C@H]([NH3+])C([O-])=O RHGKLRLOHDJJDR-BYPYZUCNSA-N 0.000 description 1
- QEFRNWWLZKMPFJ-ZXPFJRLXSA-N L-methionine (R)-S-oxide Chemical compound C[S@@](=O)CC[C@H]([NH3+])C([O-])=O QEFRNWWLZKMPFJ-ZXPFJRLXSA-N 0.000 description 1
- UCUNFLYVYCGDHP-BYPYZUCNSA-N L-methionine sulfone Chemical compound CS(=O)(=O)CC[C@H](N)C(O)=O UCUNFLYVYCGDHP-BYPYZUCNSA-N 0.000 description 1
- QEFRNWWLZKMPFJ-UHFFFAOYSA-N L-methionine sulphoxide Natural products CS(=O)CCC(N)C(O)=O QEFRNWWLZKMPFJ-UHFFFAOYSA-N 0.000 description 1
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 description 1
- RHGKLRLOHDJJDR-UHFFFAOYSA-N Ndelta-carbamoyl-DL-ornithine Natural products OC(=O)C(N)CCCNC(N)=O RHGKLRLOHDJJDR-UHFFFAOYSA-N 0.000 description 1
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 235000013477 citrulline Nutrition 0.000 description 1
- 229960002173 citrulline Drugs 0.000 description 1
- UKUBCVAQGIZRHL-UHFFFAOYSA-N delta-Guanidinovaleric acid Chemical compound NC(N)=NCCCCC(O)=O UKUBCVAQGIZRHL-UHFFFAOYSA-N 0.000 description 1
- 229960003692 gamma aminobutyric acid Drugs 0.000 description 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 1
- 229960003646 lysine Drugs 0.000 description 1
- 150000002994 phenylalanines Chemical class 0.000 description 1
- 230000002285 radioactive effect Effects 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17996700P | 2000-02-03 | 2000-02-03 | |
| US60/179,967 | 2000-02-03 | ||
| PCT/US2001/003293 WO2001057070A1 (en) | 2000-02-03 | 2001-02-01 | Melanin-concentrating hormone analogs |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2003522184A JP2003522184A (ja) | 2003-07-22 |
| JP2003522184A5 true JP2003522184A5 (https=) | 2008-02-14 |
Family
ID=22658736
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001557901A Withdrawn JP2003522184A (ja) | 2000-02-03 | 2001-02-01 | メラニン濃縮ホルモン類似体 |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP1255770A4 (https=) |
| JP (1) | JP2003522184A (https=) |
| CA (1) | CA2399509A1 (https=) |
| WO (1) | WO2001057070A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6221613B1 (en) | 1998-12-31 | 2001-04-24 | Synaptic Pharmaceutical Corporation | DNA encoding a human melanin concentrating hormone receptor (MCH1) and uses thereof |
| EP1298439B1 (en) * | 2000-07-05 | 2010-11-24 | Takeda Pharmaceutical Company Limited | Method for screening mch receptor antagonist/agonist |
| JP4780365B2 (ja) * | 2000-07-05 | 2011-09-28 | 武田薬品工業株式会社 | Ｍｃｈ受容体アンタゴニスト・アゴニストのスクリーニング方法 |
| EP1485405A4 (en) * | 2001-05-31 | 2005-09-21 | Merck & Co Inc | MELANIN CONCENTRATING HORMONE ANALOG |
| JP2004537581A (ja) | 2001-08-08 | 2004-12-16 | メルク エンド カムパニー インコーポレーテッド | メラニン濃縮ホルモン拮抗物質 |
| EP1495046A2 (en) * | 2002-01-09 | 2005-01-12 | Merck & Co., Inc. | Selective melanin concentrating hormone type 1 receptor agonists |
| EP2751291B1 (en) * | 2011-09-01 | 2018-08-15 | University of Southern California | Methods for preparing high throughput peptidomimetics, orally bioavailable drugs and compositions containing same |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5049655A (en) * | 1989-03-22 | 1991-09-17 | The Salk Institute For Biological Studies | Melanin-concentrating hormones |
| US5849708A (en) * | 1995-06-06 | 1998-12-15 | Joslin Diabetes Center, Inc. | Promotion of eating behavior |
-
2001
- 2001-02-01 EP EP01906868A patent/EP1255770A4/en not_active Withdrawn
- 2001-02-01 WO PCT/US2001/003293 patent/WO2001057070A1/en not_active Ceased
- 2001-02-01 CA CA002399509A patent/CA2399509A1/en not_active Abandoned
- 2001-02-01 JP JP2001557901A patent/JP2003522184A/ja not_active Withdrawn
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