AR063367A1 - Derivados de metastina y sus usos - Google Patents
Derivados de metastina y sus usosInfo
- Publication number
- AR063367A1 AR063367A1 ARP070104699A ARP070104699A AR063367A1 AR 063367 A1 AR063367 A1 AR 063367A1 AR P070104699 A ARP070104699 A AR P070104699A AR P070104699 A ARP070104699 A AR P070104699A AR 063367 A1 AR063367 A1 AR 063367A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- optionally substituted
- alkyl
- atoms
- aromatic
- Prior art date
Links
- 125000004432 carbon atom Chemical group C* 0.000 abstract 18
- 125000001424 substituent group Chemical group 0.000 abstract 13
- 229910052760 oxygen Inorganic materials 0.000 abstract 11
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 9
- 125000003118 aryl group Chemical group 0.000 abstract 9
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 7
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 7
- 230000000694 effects Effects 0.000 abstract 7
- 125000005842 heteroatom Chemical group 0.000 abstract 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 7
- 229910052757 nitrogen Inorganic materials 0.000 abstract 7
- 125000004434 sulfur atom Chemical group 0.000 abstract 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 6
- 125000004122 cyclic group Chemical group 0.000 abstract 5
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 4
- 150000001413 amino acids Chemical class 0.000 abstract 4
- 125000002029 aromatic hydrocarbon group Chemical group 0.000 abstract 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- KAHDONZOCXSKII-NJVVDGNHSA-N kisspeptin Chemical class C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC=CC=1)C(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H]1N(CCC1)C(=O)[C@H]1N(CCC1)C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)C1=CN=CN1 KAHDONZOCXSKII-NJVVDGNHSA-N 0.000 abstract 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 4
- 239000001301 oxygen Chemical group 0.000 abstract 4
- 229910052698 phosphorus Inorganic materials 0.000 abstract 4
- 230000028327 secretion Effects 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 206010027476 Metastases Diseases 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 125000003277 amino group Chemical group 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 230000005907 cancer growth Effects 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000006165 cyclic alkyl group Chemical group 0.000 abstract 2
- 239000003163 gonadal steroid hormone Substances 0.000 abstract 2
- 230000001456 gonadotroph Effects 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 239000005556 hormone Substances 0.000 abstract 2
- 229940088597 hormone Drugs 0.000 abstract 2
- 230000009401 metastasis Effects 0.000 abstract 2
- 125000003837 (C1-C20) alkyl group Chemical group 0.000 abstract 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000005915 C6-C14 aryl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 102000013599 Kisspeptins Human genes 0.000 abstract 1
- 108010012048 Kisspeptins Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000000539 amino acid group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 230000004071 biological effect Effects 0.000 abstract 1
- 239000008280 blood Substances 0.000 abstract 1
- 210000004369 blood Anatomy 0.000 abstract 1
- 210000004899 c-terminal region Anatomy 0.000 abstract 1
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 abstract 1
- 239000000470 constituent Substances 0.000 abstract 1
- 230000001747 exhibiting effect Effects 0.000 abstract 1
- 238000001879 gelation Methods 0.000 abstract 1
- -1 glyoxyloyl Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000004936 stimulating effect Effects 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 125000005750 substituted cyclic group Chemical group 0.000 abstract 1
- 125000000213 sulfino group Chemical group [H]OS(*)=O 0.000 abstract 1
- 125000003396 thiol group Chemical group [H]S* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
- C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
- C07K14/4702—Regulators; Modulating activity
- C07K14/4703—Inhibitors; Suppressors
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- C—CHEMISTRY; METALLURGY
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- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
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- A61K38/1703—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
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- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
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| WO2004063221A1 (ja) | 2002-12-26 | 2004-07-29 | Takeda Pharmaceutical Company Limited | メタスチン誘導体およびその用途 |
| PE20091567A1 (es) * | 2004-06-25 | 2009-11-03 | Takeda Pharmaceutical | Derivados de metastina en el tratamiento del cancer |
| US20090093615A1 (en) * | 2005-12-22 | 2009-04-09 | 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 |
| US8404643B2 (en) | 2005-12-22 | 2013-03-26 | Takeda Pharmaceutical Company Limited | Metastin derivatives and use thereof |
| TWI386417B (zh) | 2005-12-22 | 2013-02-21 | Takeda Pharmaceutical | 轉移抑素衍生物及其用途 |
| 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 |
| TWI404726B (zh) | 2006-10-25 | 2013-08-11 | Takeda Pharmaceutical | 腫瘤轉移抑制素衍生物及其用途 |
| US8110639B2 (en) * | 2006-11-17 | 2012-02-07 | Solvay Advanced Polymers, L.L.C. | Transparent and flame retardant polysulfone compositions |
| US20110118172A1 (en) * | 2008-04-24 | 2011-05-19 | Takeda Pharmaceutical Company Limited | Metastin derivative and use thereof |
| EP2275433B1 (en) * | 2008-04-30 | 2017-06-07 | Kyoto University | Metastin derivative and use thereof |
| ES2617657T3 (es) | 2008-07-30 | 2017-06-19 | Takeda Pharmaceutical Company Limited | Derivado de metastina y uso del mismo |
| WO2010137022A1 (en) * | 2009-05-27 | 2010-12-02 | Yeda Research And Development Co. Ltd | Gpr54 agonists or antagonists for treatment of diseases presenting behavioral abnormalities |
| KR20130097088A (ko) * | 2010-06-25 | 2013-09-02 | 다케다 야쿠힌 고교 가부시키가이샤 | 서방성 제제 |
| EP2755690B1 (en) | 2011-08-04 | 2020-04-01 | Merck Sharp & Dohme B.V. | Kisspeptide-pentasaccharide conjugates |
| US10202418B2 (en) | 2013-06-12 | 2019-02-12 | Merck Patent Gmbh | Hydroxy-ethylene derivatives for the treatment of arthrosis |
| WO2015112703A1 (en) * | 2014-01-22 | 2015-07-30 | The Johns Hopkins University | Compositions and methods for treating diabetes |
| 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 |
| EP3253774B1 (en) * | 2015-02-08 | 2018-11-21 | Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. | Peptides for the treatment of malignant proliferative diseases |
| JP7215755B2 (ja) * | 2017-07-05 | 2023-01-31 | エックスディーシーエクスプローラー （シャンハイ） カンパニー リミテッド | ペプチド類化合物、その使用及びそれを含む組成物 |
| 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 |
| CA3179884A1 (en) * | 2020-04-08 | 2021-10-14 | Rutgers, The State University Of New Jersey | Modified kisspeptin receptor agonists for fatty liver disease |
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| AU2005249373A1 (en) | 2004-04-23 | 2005-12-15 | Laboratoires Serono Sa | Use of GPCR54 ligands for the treatment of infertility |
| PE20091567A1 (es) | 2004-06-25 | 2009-11-03 | Takeda Pharmaceutical | Derivados de metastina en el tratamiento del cancer |
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| US8404643B2 (en) | 2005-12-22 | 2013-03-26 | 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 |
| US20090099334A1 (en) * | 2005-12-22 | 2009-04-16 | Takeda Pharmaceutical Company Limited | Metastin derivatives and use thereof |
| CN101443356A (zh) | 2006-03-20 | 2009-05-27 | 默克公司 | 神经介肽u受体激动剂及其用途 |
| JP2009536611A (ja) * | 2006-03-28 | 2009-10-15 | バイオファルミカ リミテッド | ホルモン依存性障害の処置のための作用物質及びその使用 |
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| WO2010033224A1 (en) | 2008-09-19 | 2010-03-25 | Nektar Therapeutics | Polymer conjugates of kiss1 peptides |
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