JP2010507565A5 - - Google Patents
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- JP2010507565A5 JP2010507565A5 JP2009518179A JP2009518179A JP2010507565A5 JP 2010507565 A5 JP2010507565 A5 JP 2010507565A5 JP 2009518179 A JP2009518179 A JP 2009518179A JP 2009518179 A JP2009518179 A JP 2009518179A JP 2010507565 A5 JP2010507565 A5 JP 2010507565A5
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- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 30
- 125000001424 substituent group Chemical group 0.000 claims 23
- 125000004432 carbon atom Chemical group C* 0.000 claims 22
- 229910052757 nitrogen Inorganic materials 0.000 claims 21
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 21
- 229910052799 carbon Inorganic materials 0.000 claims 19
- 150000001721 carbon Chemical group 0.000 claims 19
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 19
- 229910052717 sulfur Inorganic materials 0.000 claims 19
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 16
- -1 glyoxyloyl group Chemical group 0.000 claims 16
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 15
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 14
- 239000003814 drug Substances 0.000 claims 14
- 125000005842 heteroatom Chemical group 0.000 claims 14
- 125000004430 oxygen atom Chemical group O* 0.000 claims 14
- 125000004434 sulfur atom Chemical group 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 13
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 11
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 11
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 9
- 125000002029 aromatic hydrocarbon group Chemical group 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 8
- 125000003277 amino group Chemical group 0.000 claims 7
- 239000003795 chemical substances by application Substances 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 6
- GZYFIMLSHBLMKF-UHFFFAOYSA-N ALBIZZIINE Chemical compound OC(=O)C(N)CNC(N)=O GZYFIMLSHBLMKF-UHFFFAOYSA-N 0.000 claims 6
- 125000006165 cyclic alkyl group Chemical group 0.000 claims 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- SENJXOPIZNYLHU-UHFFFAOYSA-N L-leucyl-L-arginine Natural products CC(C)CC(N)C(=O)NC(C(O)=O)CCCN=C(N)N SENJXOPIZNYLHU-UHFFFAOYSA-N 0.000 claims 4
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 4
- SENJXOPIZNYLHU-IUCAKERBSA-N Leu-Arg Chemical compound CC(C)C[C@H](N)C(=O)N[C@H](C(O)=O)CCCN=C(N)N SENJXOPIZNYLHU-IUCAKERBSA-N 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 4
- 108010000761 leucylarginine Proteins 0.000 claims 4
- 229910052698 phosphorus Inorganic materials 0.000 claims 4
- 230000000069 prophylactic effect Effects 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims 3
- OUYCCCASQSFEME-MRVPVSSYSA-N D-tyrosine Chemical compound OC(=O)[C@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-MRVPVSSYSA-N 0.000 claims 3
- 150000001413 amino acids Chemical group 0.000 claims 3
- 229960001230 asparagine Drugs 0.000 claims 3
- 235000009582 asparagine Nutrition 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000001589 carboacyl group Chemical group 0.000 claims 3
- OGNSCSPNOLGXSM-UHFFFAOYSA-N 2,4-diaminobutyric acid Chemical compound NCCC(N)C(O)=O OGNSCSPNOLGXSM-UHFFFAOYSA-N 0.000 claims 2
- QNAYBMKLOCPYGJ-UWTATZPHSA-N D-alanine Chemical compound C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 claims 2
- ROHFNLRQFUQHCH-RXMQYKEDSA-N D-leucine Chemical compound CC(C)C[C@@H](N)C(O)=O ROHFNLRQFUQHCH-RXMQYKEDSA-N 0.000 claims 2
- KDXKERNSBIXSRK-RXMQYKEDSA-N D-lysine Chemical compound NCCCC[C@@H](N)C(O)=O KDXKERNSBIXSRK-RXMQYKEDSA-N 0.000 claims 2
- COLNVLDHVKWLRT-MRVPVSSYSA-N D-phenylalanine Chemical compound OC(=O)[C@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-MRVPVSSYSA-N 0.000 claims 2
- QIVBCDIJIAJPQS-SECBINFHSA-N D-tryptophane Chemical compound C1=CC=C2C(C[C@@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-SECBINFHSA-N 0.000 claims 2
- NSTUFLGQJCOCDL-UWVGGRQHSA-N Gly-Leu-Arg Chemical compound NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(O)=O)CCCN=C(N)N NSTUFLGQJCOCDL-UWVGGRQHSA-N 0.000 claims 2
- 102000006771 Gonadotropins Human genes 0.000 claims 2
- 108010086677 Gonadotropins Proteins 0.000 claims 2
- UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 230000003828 downregulation Effects 0.000 claims 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 2
- 125000000350 glycoloyl group Chemical group O=C([*])C([H])([H])O[H] 0.000 claims 2
- 239000003163 gonadal steroid hormone Substances 0.000 claims 2
- 239000002622 gonadotropin Substances 0.000 claims 2
- 239000005556 hormone Substances 0.000 claims 2
- 229940088597 hormone Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 230000028327 secretion Effects 0.000 claims 2
- DFZVZEMNPGABKO-SSDOTTSWSA-N (2r)-2-amino-3-pyridin-3-ylpropanoic acid Chemical compound OC(=O)[C@H](N)CC1=CC=CN=C1 DFZVZEMNPGABKO-SSDOTTSWSA-N 0.000 claims 1
- PDRJLZDUOULRHE-SSDOTTSWSA-N (2r)-2-azaniumyl-3-pyridin-2-ylpropanoate Chemical compound OC(=O)[C@H](N)CC1=CC=CC=N1 PDRJLZDUOULRHE-SSDOTTSWSA-N 0.000 claims 1
- FQFVANSXYKWQOT-SSDOTTSWSA-N (2r)-2-azaniumyl-3-pyridin-4-ylpropanoate Chemical compound OC(=O)[C@H](N)CC1=CC=NC=C1 FQFVANSXYKWQOT-SSDOTTSWSA-N 0.000 claims 1
- RWLSBXBFZHDHHX-VIFPVBQESA-N (2s)-2-(naphthalen-2-ylamino)propanoic acid Chemical compound C1=CC=CC2=CC(N[C@@H](C)C(O)=O)=CC=C21 RWLSBXBFZHDHHX-VIFPVBQESA-N 0.000 claims 1
- SAAQPSNNIOGFSQ-LURJTMIESA-N (2s)-2-(pyridin-4-ylamino)propanoic acid Chemical compound OC(=O)[C@H](C)NC1=CC=NC=C1 SAAQPSNNIOGFSQ-LURJTMIESA-N 0.000 claims 1
- 125000003837 (C1-C20) alkyl group Chemical group 0.000 claims 1
- RFRJUFFMYCMGHN-UHFFFAOYSA-N 2,2-diamino-4-oxobutanoic acid Chemical compound OC(=O)C(N)(N)CC=O RFRJUFFMYCMGHN-UHFFFAOYSA-N 0.000 claims 1
- ZIPUIDBGTLUSKQ-UHFFFAOYSA-N 2,2-diamino-4-oxopentanoic acid Chemical compound CC(=O)CC(N)(N)C(O)=O ZIPUIDBGTLUSKQ-UHFFFAOYSA-N 0.000 claims 1
- WTOFYLAWDLQMBZ-UHFFFAOYSA-N 2-azaniumyl-3-thiophen-2-ylpropanoate Chemical compound OC(=O)C(N)CC1=CC=CS1 WTOFYLAWDLQMBZ-UHFFFAOYSA-N 0.000 claims 1
- PECYZEOJVXMISF-UWTATZPHSA-N 3-amino-D-alanine Chemical compound NC[C@@H](N)C(O)=O PECYZEOJVXMISF-UWTATZPHSA-N 0.000 claims 1
- XWHHYOYVRVGJJY-QMMMGPOBSA-N 4-fluoro-L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(F)C=C1 XWHHYOYVRVGJJY-QMMMGPOBSA-N 0.000 claims 1
- 206010000234 Abortion spontaneous Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 206010004272 Benign hydatidiform mole Diseases 0.000 claims 1
- 125000005915 C6-C14 aryl group Chemical group 0.000 claims 1
- 208000006332 Choriocarcinoma Diseases 0.000 claims 1
- CKLJMWTZIZZHCS-UHFFFAOYSA-N D-OH-Asp Natural products OC(=O)C(N)CC(O)=O CKLJMWTZIZZHCS-UHFFFAOYSA-N 0.000 claims 1
- MTCFGRXMJLQNBG-UWTATZPHSA-N D-Serine Chemical compound OC[C@@H](N)C(O)=O MTCFGRXMJLQNBG-UWTATZPHSA-N 0.000 claims 1
- 125000002237 D-aspartyl group Chemical group [H]OC(=O)[C@]([H])(N([H])[H])C([H])([H])C(*)=O 0.000 claims 1
- ZDXPYRJPNDTMRX-GSVOUGTGSA-N D-glutamine Chemical compound OC(=O)[C@H](N)CCC(N)=O ZDXPYRJPNDTMRX-GSVOUGTGSA-N 0.000 claims 1
- HNDVDQJCIGZPNO-RXMQYKEDSA-N D-histidine Chemical compound OC(=O)[C@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-RXMQYKEDSA-N 0.000 claims 1
- AYFVYJQAPQTCCC-STHAYSLISA-N D-threonine Chemical compound C[C@H](O)[C@@H](N)C(O)=O AYFVYJQAPQTCCC-STHAYSLISA-N 0.000 claims 1
- 125000002849 D-tyrosine group Chemical group [H]N([H])[C@@]([H])(C(=O)[*])C([H])([H])C1=C([H])C([H])=C(O[H])C([H])=C1[H] 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 208000006937 Hydatidiform mole Diseases 0.000 claims 1
- 102100034845 KiSS-1 receptor Human genes 0.000 claims 1
- 101710104293 KiSS-1 receptor Proteins 0.000 claims 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 1
- 125000000510 L-tryptophano group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C(C([H])([H])[C@@]([H])(C(O[H])=O)N([H])[*])C2=C1[H] 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 206010046798 Uterine leiomyoma Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000000539 amino acid group Chemical group 0.000 claims 1
- 239000002257 antimetastatic agent Substances 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 229940000635 beta-alanine Drugs 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- 230000005907 cancer growth Effects 0.000 claims 1
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 206010016165 failure to thrive Diseases 0.000 claims 1
- 230000004578 fetal growth Effects 0.000 claims 1
- 201000007116 gestational trophoblastic neoplasm Diseases 0.000 claims 1
- 208000018914 glucose metabolism disease Diseases 0.000 claims 1
- 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 claims 1
- 230000002710 gonadal effect Effects 0.000 claims 1
- 239000003966 growth inhibitor Substances 0.000 claims 1
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 claims 1
- 125000003651 hexanedioyl group Chemical group C(CCCCC(=O)*)(=O)* 0.000 claims 1
- 239000000411 inducer Substances 0.000 claims 1
- 230000006698 induction Effects 0.000 claims 1
- 208000000509 infertility Diseases 0.000 claims 1
- 230000036512 infertility Effects 0.000 claims 1
- 231100000535 infertility Toxicity 0.000 claims 1
- 208000037805 labour Diseases 0.000 claims 1
- 201000010260 leiomyoma Diseases 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- 208000015994 miscarriage Diseases 0.000 claims 1
- 230000016087 ovulation Effects 0.000 claims 1
- 230000003169 placental effect Effects 0.000 claims 1
- 208000006155 precocious puberty Diseases 0.000 claims 1
- 235000018102 proteins Nutrition 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 208000000995 spontaneous abortion Diseases 0.000 claims 1
- 125000000213 sulfino group Chemical group [H]OS(*)=O 0.000 claims 1
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 1
- 125000001493 tyrosinyl group Chemical group [H]OC1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2006290536 | 2006-10-25 | ||
| JP2007021387 | 2007-01-31 | ||
| JP2007221911 | 2007-08-28 | ||
| PCT/JP2007/071169 WO2008050897A1 (en) | 2006-10-25 | 2007-10-24 | Metastin derivatives and use thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013004011A Division JP5686825B2 (ja) | 2006-10-25 | 2013-01-11 | メタスチン誘導体およびその用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010507565A JP2010507565A (ja) | 2010-03-11 |
| JP2010507565A5 true JP2010507565A5 (enExample) | 2010-12-09 |
Family
ID=38925530
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009518179A Pending JP2010507565A (ja) | 2006-10-25 | 2007-10-24 | メタスチン誘導体およびその用途 |
| JP2013004011A Expired - Fee Related JP5686825B2 (ja) | 2006-10-25 | 2013-01-11 | メタスチン誘導体およびその用途 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013004011A Expired - Fee Related JP5686825B2 (ja) | 2006-10-25 | 2013-01-11 | メタスチン誘導体およびその用途 |
Country Status (33)
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2511858A1 (en) | 2002-12-26 | 2004-07-29 | Takeda Pharmaceutical Company Limited | Metastin derivative and use thereof |
| US7625869B2 (en) * | 2004-06-25 | 2009-12-01 | Takeda Pharmaceutical Company Limited | Metastin derivatives and use thereof |
| US20090093615A1 (en) * | 2005-12-22 | 2009-04-09 | Takeda Pharmaceutical Company Limited | Metastin derivatives and use thereof |
| AR058584A1 (es) | 2005-12-22 | 2008-02-13 | Takeda Pharmaceutical | Derivados de metastina y uso de los mismos |
| US8404643B2 (en) | 2005-12-22 | 2013-03-26 | Takeda Pharmaceutical Company Limited | Metastin derivatives and use thereof |
| US20090099334A1 (en) * | 2005-12-22 | 2009-04-16 | Takeda Pharmaceutical Company Limited | Metastin derivatives and use thereof |
| WO2007125619A1 (ja) * | 2006-04-26 | 2007-11-08 | Kyoto University | Ｇｐｒ５４アゴニスト活性を有する新規化合物 |
| JO3048B1 (ar) | 2006-10-25 | 2016-09-05 | Takeda Pharmaceuticals Co | مشتقات متاستين واستخدامها |
| US8110639B2 (en) * | 2006-11-17 | 2012-02-07 | Solvay Advanced Polymers, L.L.C. | Transparent and flame retardant polysulfone compositions |
| EP2277900A4 (en) * | 2008-04-24 | 2011-08-03 | Takeda Pharmaceutical | METASTINE DERIVATIVE AND ITS USE |
| WO2009139298A1 (ja) * | 2008-04-30 | 2009-11-19 | 国立大学法人京都大学 | メタスチン誘導体およびその用途 |
| WO2010013762A1 (ja) | 2008-07-30 | 2010-02-04 | 武田薬品工業株式会社 | メタスチン誘導体およびその用途 |
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| EP2755690B1 (en) | 2011-08-04 | 2020-04-01 | Merck Sharp & Dohme B.V. | Kisspeptide-pentasaccharide conjugates |
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| JP6253146B2 (ja) * | 2014-02-04 | 2017-12-27 | 国立大学法人山口大学 | 新規なペプチド誘導体及びこれを含有する医薬 |
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| TWI795462B (zh) * | 2017-11-17 | 2023-03-11 | 日商鹽野義製藥股份有限公司 | 光安定性及溶出性優異的醫藥製劑 |
| EP4132559A4 (en) * | 2020-04-08 | 2024-06-12 | Rutgers, the State University of New Jersey | MODIFIED KISSPEPTIN RECEPTOR AGONISTS FOR FATTY LIVER STEATOSIS |
| WO2025217074A1 (en) | 2024-04-08 | 2025-10-16 | Radionetics Oncology, Inc. | Kisspeptin receptor (kiss1r) targeted therapeutics and uses thereof |
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