JP2011505345A5 - - Google Patents
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- Publication number
- JP2011505345A5 JP2011505345A5 JP2010535349A JP2010535349A JP2011505345A5 JP 2011505345 A5 JP2011505345 A5 JP 2011505345A5 JP 2010535349 A JP2010535349 A JP 2010535349A JP 2010535349 A JP2010535349 A JP 2010535349A JP 2011505345 A5 JP2011505345 A5 JP 2011505345A5
- Authority
- JP
- Japan
- Prior art keywords
- phe
- group
- compound according
- cyclo
- carbamoyl
- 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
- 150000001875 compounds Chemical class 0.000 claims 18
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 11
- -1 methyloxy groups Chemical group 0.000 claims 11
- KAFHLONDOVSENM-HNNXBMFYSA-N O-Benzyl-L-tyrosine Chemical compound C1=CC(C[C@H](N)C(O)=O)=CC=C1OCC1=CC=CC=C1 KAFHLONDOVSENM-HNNXBMFYSA-N 0.000 claims 10
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 9
- QXRNAOYBCYVZCD-BQBZGAKWSA-N Ala-Lys Chemical class C[C@H](N)C(=O)N[C@H](C(O)=O)CCCCN QXRNAOYBCYVZCD-BQBZGAKWSA-N 0.000 claims 7
- 125000000266 alpha-aminoacyl group Chemical group 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000000524 functional group Chemical group 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 206010012735 Diarrhoea Diseases 0.000 claims 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 239000013522 chelant Substances 0.000 claims 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical group C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 239000002184 metal Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 1
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 208000030507 AIDS Diseases 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical group CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- 206010000599 Acromegaly Diseases 0.000 claims 1
- 125000001433 C-terminal amino-acid group Chemical group 0.000 claims 1
- 208000000668 Chronic Pancreatitis Diseases 0.000 claims 1
- 208000006784 Cutaneous Fistula Diseases 0.000 claims 1
- 108010069514 Cyclic Peptides Proteins 0.000 claims 1
- 102000001189 Cyclic Peptides Human genes 0.000 claims 1
- 208000002699 Digestive System Neoplasms Diseases 0.000 claims 1
- 208000012671 Gastrointestinal haemorrhages Diseases 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- 208000001344 Macular Edema Diseases 0.000 claims 1
- 206010025415 Macular oedema Diseases 0.000 claims 1
- 229910002651 NO3 Inorganic materials 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 206010033647 Pancreatitis acute Diseases 0.000 claims 1
- 206010033649 Pancreatitis chronic Diseases 0.000 claims 1
- 208000031481 Pathologic Constriction Diseases 0.000 claims 1
- 206010038934 Retinopathy proliferative Diseases 0.000 claims 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 1
- 208000009311 VIPoma Diseases 0.000 claims 1
- 208000024248 Vascular System injury Diseases 0.000 claims 1
- 208000012339 Vascular injury Diseases 0.000 claims 1
- 206010053648 Vascular occlusion Diseases 0.000 claims 1
- 201000003229 acute pancreatitis Diseases 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 claims 1
- 235000008206 alpha-amino acids Nutrition 0.000 claims 1
- 150000001413 amino acids Chemical group 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 125000005427 anthranyl group Chemical group 0.000 claims 1
- 229940009098 aspartate Drugs 0.000 claims 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 1
- 239000004305 biphenyl Chemical group 0.000 claims 1
- 235000010290 biphenyl Nutrition 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 150000001768 cations Chemical class 0.000 claims 1
- 239000002738 chelating agent Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 230000002596 correlated effect Effects 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical group C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 1
- 125000003983 fluorenyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3CC12)* 0.000 claims 1
- 230000030136 gastric emptying Effects 0.000 claims 1
- 208000030304 gastrointestinal bleeding Diseases 0.000 claims 1
- 239000003629 gastrointestinal hormone Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 1
- 230000000968 intestinal effect Effects 0.000 claims 1
- 150000002500 ions Chemical class 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 201000010230 macular retinal edema Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 201000011116 pancreatic cholera Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229920001467 poly(styrenesulfonates) Polymers 0.000 claims 1
- 208000030761 polycystic kidney disease Diseases 0.000 claims 1
- 229920000193 polymethacrylate Polymers 0.000 claims 1
- 229960002796 polystyrene sulfonate Drugs 0.000 claims 1
- 239000011970 polystyrene sulfonate Substances 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 230000003248 secreting effect Effects 0.000 claims 1
- 208000037804 stenosis Diseases 0.000 claims 1
- 230000036262 stenosis Effects 0.000 claims 1
- 125000005504 styryl group Chemical group 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 208000021331 vascular occlusion disease Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ITMI2007A002266 | 2007-12-03 | ||
| ITMI20072266 ITMI20072266A1 (it) | 2007-12-03 | 2007-12-03 | Nuovi analoghi non selettivi di somatostatina |
| EP07425778A EP2067786A1 (en) | 2007-12-07 | 2007-12-07 | Novel non selective analogs of somatostatin |
| EP07425778.3 | 2007-12-07 | ||
| PCT/EP2008/066081 WO2009071460A2 (en) | 2007-12-03 | 2008-11-24 | New non-selective somatostatin analogues |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011505345A JP2011505345A (ja) | 2011-02-24 |
| JP2011505345A5 true JP2011505345A5 (https=) | 2011-08-04 |
| JP5331817B2 JP5331817B2 (ja) | 2013-10-30 |
Family
ID=40667736
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010535349A Active JP5331817B2 (ja) | 2007-12-03 | 2008-11-24 | 新規な非選択的ソマトスタチン類似体 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8937152B2 (https=) |
| EP (1) | EP2225271B1 (https=) |
| JP (1) | JP5331817B2 (https=) |
| KR (1) | KR101500528B1 (https=) |
| CN (1) | CN101883785B (https=) |
| BR (1) | BRPI0818978B8 (https=) |
| CA (1) | CA2702940C (https=) |
| CY (1) | CY1114490T1 (https=) |
| DK (1) | DK2225271T3 (https=) |
| ES (1) | ES2431573T3 (https=) |
| HR (1) | HRP20130948T1 (https=) |
| PL (1) | PL2225271T3 (https=) |
| PT (1) | PT2225271E (https=) |
| SI (1) | SI2225271T1 (https=) |
| WO (1) | WO2009071460A2 (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8592377B2 (en) | 2007-03-28 | 2013-11-26 | President And Fellows Of Harvard College | Stitched polypeptides |
| US8937152B2 (en) * | 2007-12-03 | 2015-01-20 | Italfarmaco Spa | Non-selective somatostatin analogues |
| ES2711526T3 (es) | 2010-08-13 | 2019-05-06 | Aileron Therapeutics Inc | Macrociclos peptidomiméticos |
| BR112014004936A2 (pt) * | 2011-09-04 | 2017-04-04 | Glytech Inc | polipeptídeo glicosilado e composição de drogas contendo referido polipeptídeo |
| TW201806968A (zh) | 2011-10-18 | 2018-03-01 | 艾利倫治療公司 | 擬肽巨環化合物 |
| EP2819688A4 (en) | 2012-02-15 | 2015-10-28 | Aileron Therapeutics Inc | TRIAZOL AND THIOETHER-COUPLED PEPTIDOMIMETIC MACROCYCLES |
| BR112014020103A2 (pt) | 2012-02-15 | 2018-10-09 | Aileron Therapeutics, Inc. | macrociclos peptidomiméticos |
| WO2014071241A1 (en) | 2012-11-01 | 2014-05-08 | Aileron Therapeutics, Inc. | Disubstituted amino acids and methods of preparation and use thereof |
| JP6869720B2 (ja) * | 2013-06-13 | 2021-05-12 | アンチセンス セラピューティクス リミテッド | 併用療法 |
| CN103467575B (zh) * | 2013-08-22 | 2016-03-02 | 深圳翰宇药业股份有限公司 | 一种帕西瑞肽的制备方法 |
| CN103641894B (zh) * | 2013-12-06 | 2015-10-28 | 深圳翰宇药业股份有限公司 | 一种治疗库欣病的多肽药物的制备方法 |
| EP3197478A4 (en) | 2014-09-24 | 2018-05-30 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| CN104447962B (zh) * | 2014-12-29 | 2018-07-17 | 成都圣诺生物科技股份有限公司 | 一种合成帕瑞肽的方法 |
| WO2016154058A1 (en) | 2015-03-20 | 2016-09-29 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| WO2020064693A1 (en) * | 2018-09-25 | 2020-04-02 | Advanced Accelerator Applications (Italy) Srl | Combination therapy |
| GB201816637D0 (en) * | 2018-10-12 | 2018-11-28 | Heptares Therapeutics Ltd | Selective somatostatin receptor agonists |
| IL305248A (en) * | 2021-03-04 | 2023-10-01 | Starget Pharma Ltd | Structurally constrained peptide ligands for the somatostatin-3 receptor, their derivatives, and their uses |
| IT202100032615A1 (it) | 2021-12-24 | 2023-06-24 | Italfarmaco Spa | Uso di un agonista della somatostatina nel trattamento di tumori che esprimono SSTR3 |
| CN119708199A (zh) * | 2023-09-27 | 2025-03-28 | 钱杭江医药科技(嘉兴)有限公司 | 生长抑素肽类类似物、螯合物及其应用 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY147327A (en) * | 1995-06-29 | 2012-11-30 | Novartis Ag | Somatostatin peptides |
| GB0018891D0 (en) * | 2000-08-01 | 2000-09-20 | Novartis Ag | Organic compounds |
| US6365380B2 (en) * | 2000-02-23 | 2002-04-02 | Pcbu Services, Inc. | Method for stereoselectively inverting a chiral center of a chemical compound using an enzyme and a metal catalyst |
| CA2476324A1 (en) * | 2002-03-12 | 2003-09-25 | The Procter & Gamble Company | Cosmetic composition comprising double coated pigment and a gelling agent |
| GB0206415D0 (en) | 2002-03-19 | 2002-05-01 | Glaxo Group Ltd | Deracemisation of amines |
| GB0300095D0 (en) * | 2003-01-03 | 2003-02-05 | Novartis Ag | Organic compounds |
| AR044852A1 (es) * | 2003-06-24 | 2005-10-05 | Novartis Ag | Una composicion farmaceutica para la administracion parenteral que comprende un analogo de somatostatina |
| JP2007501775A (ja) * | 2003-08-07 | 2007-02-01 | ノバルティス アクチエンゲゼルシャフト | 免疫抑制剤としてのヒストンデアセチラーゼ阻害剤 |
| GB0318682D0 (en) | 2003-08-08 | 2003-09-10 | Novartis Ag | Organic compounds |
| EP1522311A1 (fr) * | 2003-10-10 | 2005-04-13 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Utilisation de la somatostine ou d'un de ses analogues pour préparer un médicament destiné à réguler la réserve folliculaire ovarienne chez la femme non ménopausée |
| JP2007518702A (ja) * | 2003-11-25 | 2007-07-12 | ノバルティス アクチエンゲゼルシャフト | ソマトスタチン類似体処置の効力についてのバイオマーカー |
| ITFI20040057A1 (it) * | 2004-03-10 | 2004-06-10 | Mauro Giuntini | Analoghi della somatostatina |
| GB0428151D0 (en) | 2004-12-22 | 2005-01-26 | Novartis Ag | Organic compounds |
| US7824663B2 (en) * | 2005-03-10 | 2010-11-02 | Kokyu Alcohol Kogyo Co., Ltd. | Lip gloss composition |
| ES2383303T3 (es) * | 2005-11-10 | 2012-06-20 | Chemi S.P.A. | Formulaciones de inhibidores de la liberación prolongada de la hormona del crecimiento análogos de la somatostatina |
| US8937152B2 (en) * | 2007-12-03 | 2015-01-20 | Italfarmaco Spa | Non-selective somatostatin analogues |
-
2008
- 2008-11-24 US US12/734,475 patent/US8937152B2/en active Active
- 2008-11-24 DK DK08856519.7T patent/DK2225271T3/da active
- 2008-11-24 EP EP08856519.7A patent/EP2225271B1/en active Active
- 2008-11-24 CA CA2702940A patent/CA2702940C/en active Active
- 2008-11-24 KR KR1020107010880A patent/KR101500528B1/ko active Active
- 2008-11-24 CN CN200880118937.1A patent/CN101883785B/zh active Active
- 2008-11-24 PL PL08856519T patent/PL2225271T3/pl unknown
- 2008-11-24 ES ES08856519T patent/ES2431573T3/es active Active
- 2008-11-24 SI SI200831046T patent/SI2225271T1/sl unknown
- 2008-11-24 WO PCT/EP2008/066081 patent/WO2009071460A2/en not_active Ceased
- 2008-11-24 PT PT88565197T patent/PT2225271E/pt unknown
- 2008-11-24 BR BRPI0818978A patent/BRPI0818978B8/pt active IP Right Grant
- 2008-11-24 HR HRP20130948AT patent/HRP20130948T1/hr unknown
- 2008-11-24 JP JP2010535349A patent/JP5331817B2/ja active Active
-
2013
- 2013-10-10 CY CY20131100895T patent/CY1114490T1/el unknown
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