JP2005508886A5 - - Google Patents
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- Publication number
- JP2005508886A5 JP2005508886A5 JP2003519107A JP2003519107A JP2005508886A5 JP 2005508886 A5 JP2005508886 A5 JP 2005508886A5 JP 2003519107 A JP2003519107 A JP 2003519107A JP 2003519107 A JP2003519107 A JP 2003519107A JP 2005508886 A5 JP2005508886 A5 JP 2005508886A5
- Authority
- JP
- Japan
- Prior art keywords
- somatostatin
- group
- pharmaceutical composition
- radioisotope
- treatment
- 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.)
- Ceased
Links
- NHXLMOGPVYXJNR-ATOGVRKGSA-N somatostatin Chemical class C([C@H]1C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)NC(=O)CNC(=O)[C@H](C)N)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 NHXLMOGPVYXJNR-ATOGVRKGSA-N 0.000 claims description 21
- 108050001286 Somatostatin Receptor Proteins 0.000 claims description 8
- 102000011096 Somatostatin receptor Human genes 0.000 claims description 8
- 239000002738 chelating agent Substances 0.000 claims description 8
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims description 7
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims description 6
- BKQQPCDQZZTLSE-UHFFFAOYSA-N 2-amino-3-naphthalen-1-ylpropanoic acid;hydrochloride Chemical compound Cl.C1=CC=C2C(CC(N)C(O)=O)=CC=CC2=C1 BKQQPCDQZZTLSE-UHFFFAOYSA-N 0.000 claims description 5
- -1 DOTAGA Chemical compound 0.000 claims description 5
- 229940024606 amino acid Drugs 0.000 claims description 5
- 235000001014 amino acid Nutrition 0.000 claims description 5
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 claims description 4
- WTOFYLAWDLQMBZ-UHFFFAOYSA-N 2-azaniumyl-3-thiophen-2-ylpropanoate Chemical compound OC(=O)C(N)CC1=CC=CS1 WTOFYLAWDLQMBZ-UHFFFAOYSA-N 0.000 claims description 4
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 4
- 125000005647 linker group Chemical group 0.000 claims description 4
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims description 4
- 239000004475 Arginine Substances 0.000 claims description 3
- 150000001413 amino acids Chemical group 0.000 claims description 3
- 235000009697 arginine Nutrition 0.000 claims description 3
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims description 3
- 150000001875 compounds Chemical class 0.000 claims description 3
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims description 3
- JHALWMSZGCVVEM-UHFFFAOYSA-N 2-[4,7-bis(carboxymethyl)-1,4,7-triazonan-1-yl]acetic acid Chemical compound OC(=O)CN1CCN(CC(O)=O)CCN(CC(O)=O)CC1 JHALWMSZGCVVEM-UHFFFAOYSA-N 0.000 claims description 2
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims description 2
- 229930182847 D-glutamic acid Natural products 0.000 claims description 2
- 125000004077 D-glutamic acid group Chemical group [H]N([H])[C@@]([H])(C(=O)[*])C([H])([H])C([H])([H])C(N([H])[H])=O 0.000 claims description 2
- OGNSCSPNOLGXSM-VKHMYHEASA-N L-2,4-diaminobutyric acid Chemical compound NCC[C@H](N)C(O)=O OGNSCSPNOLGXSM-VKHMYHEASA-N 0.000 claims description 2
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims description 2
- RHGKLRLOHDJJDR-BYPYZUCNSA-N L-citrulline Chemical compound NC(=O)NCCC[C@H]([NH3+])C([O-])=O RHGKLRLOHDJJDR-BYPYZUCNSA-N 0.000 claims description 2
- QPCDCPDFJACHGM-UHFFFAOYSA-N N,N-bis{2-[bis(carboxymethyl)amino]ethyl}glycine Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(=O)O)CCN(CC(O)=O)CC(O)=O QPCDCPDFJACHGM-UHFFFAOYSA-N 0.000 claims description 2
- RHGKLRLOHDJJDR-UHFFFAOYSA-N Ndelta-carbamoyl-DL-ornithine Natural products OC(=O)C(N)CCCNC(N)=O RHGKLRLOHDJJDR-UHFFFAOYSA-N 0.000 claims description 2
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims description 2
- WDLRUFUQRNWCPK-UHFFFAOYSA-N Tetraxetan Chemical compound OC(=O)CN1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1 WDLRUFUQRNWCPK-UHFFFAOYSA-N 0.000 claims description 2
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims description 2
- 239000004473 Threonine Substances 0.000 claims description 2
- 229960003121 arginine Drugs 0.000 claims description 2
- 235000009582 asparagine Nutrition 0.000 claims description 2
- 229960001230 asparagine Drugs 0.000 claims description 2
- 229960002685 biotin Drugs 0.000 claims description 2
- 235000020958 biotin Nutrition 0.000 claims description 2
- 239000011616 biotin Substances 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 150000001728 carbonyl compounds Chemical class 0.000 claims description 2
- 229960002173 citrulline Drugs 0.000 claims description 2
- 235000013477 citrulline Nutrition 0.000 claims description 2
- 229960002989 glutamic acid Drugs 0.000 claims description 2
- 230000026030 halogenation Effects 0.000 claims description 2
- 238000005658 halogenation reaction Methods 0.000 claims description 2
- 230000007935 neutral effect Effects 0.000 claims description 2
- 239000003973 paint Substances 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 125000000467 secondary amino group Chemical group [H]N([*:1])[*:2] 0.000 claims description 2
- 125000000341 threoninyl group Chemical group [H]OC([H])(C([H])([H])[H])C([H])(N([H])[H])C(*)=O 0.000 claims description 2
- 229960004441 tyrosine Drugs 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 239000002184 metal Substances 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- 229940075620 somatostatin analogue Drugs 0.000 claims 5
- 238000003745 diagnosis Methods 0.000 claims 4
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 3
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 230000002018 overexpression Effects 0.000 claims 3
- WJJGAKCAAJOICV-JTQLQIEISA-N (2s)-2-(dimethylamino)-3-(4-hydroxyphenyl)propanoic acid Chemical compound CN(C)[C@H](C(O)=O)CC1=CC=C(O)C=C1 WJJGAKCAAJOICV-JTQLQIEISA-N 0.000 claims 2
- 239000004472 Lysine Substances 0.000 claims 2
- UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 claims 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 2
- 150000002994 phenylalanines Chemical class 0.000 claims 2
- FSYKKLYZXJSNPZ-UHFFFAOYSA-N sarcosine Chemical compound C[NH2+]CC([O-])=O FSYKKLYZXJSNPZ-UHFFFAOYSA-N 0.000 claims 2
- 230000001225 therapeutic effect Effects 0.000 claims 2
- RTBFRGCFXZNCOE-UHFFFAOYSA-N 1-methylsulfonylpiperidin-4-one Chemical compound CS(=O)(=O)N1CCC(=O)CC1 RTBFRGCFXZNCOE-UHFFFAOYSA-N 0.000 claims 1
- COLNVLDHVKWLRT-MRVPVSSYSA-N D-phenylalanine Chemical compound OC(=O)[C@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-MRVPVSSYSA-N 0.000 claims 1
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-Ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 claims 1
- UBQYURCVBFRUQT-UHFFFAOYSA-N N-benzoyl-Ferrioxamine B Chemical compound CC(=O)N(O)CCCCCNC(=O)CCC(=O)N(O)CCCCCNC(=O)CCC(=O)N(O)CCCCCN UBQYURCVBFRUQT-UHFFFAOYSA-N 0.000 claims 1
- AHLPHDHHMVZTML-UHFFFAOYSA-N Orn-delta-NH2 Natural products NCCCC(N)C(O)=O AHLPHDHHMVZTML-UHFFFAOYSA-N 0.000 claims 1
- UTJLXEIPEHZYQJ-UHFFFAOYSA-N Ornithine Natural products OC(=O)C(C)CCCN UTJLXEIPEHZYQJ-UHFFFAOYSA-N 0.000 claims 1
- 108010077895 Sarcosine Proteins 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- JFCQEDHGNNZCLN-UHFFFAOYSA-N anhydrous glutaric acid Natural products OC(=O)CCCC(O)=O JFCQEDHGNNZCLN-UHFFFAOYSA-N 0.000 claims 1
- 125000000637 arginyl group Chemical group N[C@@H](CCCNC(N)=N)C(=O)* 0.000 claims 1
- 229940000635 beta-alanine Drugs 0.000 claims 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims 1
- 229960000958 deferoxamine Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- FKRKTHDSSJWJJP-UHFFFAOYSA-N hydrazine;pyridine-3-carboxamide Chemical compound NN.NC(=O)C1=CC=CN=C1 FKRKTHDSSJWJJP-UHFFFAOYSA-N 0.000 claims 1
- 229960003646 lysine Drugs 0.000 claims 1
- 229960003104 ornithine Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 235000019260 propionic acid Nutrition 0.000 claims 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 claims 1
- 229940043230 sarcosine Drugs 0.000 claims 1
- 150000003668 tyrosines Chemical class 0.000 claims 1
- KOUZWQLNUJWNIA-UHFFFAOYSA-N 2-hydrazinylpyridine-3-carboxamide Chemical compound NNC1=NC=CC=C1C(N)=O KOUZWQLNUJWNIA-UHFFFAOYSA-N 0.000 description 1
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 description 1
- 230000008878 coupling Effects 0.000 description 1
- 238000010168 coupling process Methods 0.000 description 1
- 238000005859 coupling reaction Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01203033A EP1283216A1 (en) | 2001-08-10 | 2001-08-10 | Somatostatin analogues binding to all somatostatin receptor subtypes and their use |
| PCT/EP2002/009004 WO2003014158A1 (en) | 2001-08-10 | 2002-08-07 | Somatostatin analogues and their use somatostatin analogues binding to all somatostatin receptor and their use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005508886A JP2005508886A (ja) | 2005-04-07 |
| JP2005508886A5 true JP2005508886A5 (https=) | 2009-06-04 |
Family
ID=8180776
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003519107A Ceased JP2005508886A (ja) | 2001-08-10 | 2002-08-07 | ソマトスタチン類似体とそれらの使用、全てのソマトスタチンレセプターと結合するソマトスタチン類似体およびそれらの使用 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US7192570B2 (https=) |
| EP (2) | EP1283216A1 (https=) |
| JP (1) | JP2005508886A (https=) |
| AT (1) | ATE328005T1 (https=) |
| AU (1) | AU2002333396B2 (https=) |
| CA (1) | CA2456881A1 (https=) |
| CY (1) | CY1105177T1 (https=) |
| DE (1) | DE60211917T2 (https=) |
| DK (1) | DK1419178T3 (https=) |
| ES (1) | ES2266616T3 (https=) |
| PT (1) | PT1419178E (https=) |
| WO (1) | WO2003014158A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1283216A1 (en) | 2001-08-10 | 2003-02-12 | Mallinckrodt Inc. | Somatostatin analogues binding to all somatostatin receptor subtypes and their use |
| NZ542371A (en) * | 2003-03-19 | 2008-10-31 | Universitatsspital Basel | Radiolabeled conjugates based on substance P and the uses thereof |
| JP2009511565A (ja) * | 2005-10-14 | 2009-03-19 | スティフティング カトリーケ ユニフェルスィテイト | １つ以上の部位特異的に結合体化されたヒドラジノニコチンアミド（ｈｙｎｉｃ）部分を介して標識されたインターロイキン−８、ならびに感染および炎症の診断におけるその使用 |
| US8691761B2 (en) * | 2006-10-16 | 2014-04-08 | Jean E. F. Rivier | Somatostatin receptor 2 antagonists |
| CA2666642C (en) | 2006-10-16 | 2015-11-17 | The Salk Institute For Biological Studies | Receptor(sstr2)-selective somatostatin antagonists |
| WO2009012288A2 (en) | 2007-07-17 | 2009-01-22 | Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Trifunctional imaging agent for monoclonal antibody tumor-targeted imaging |
| US9782565B2 (en) | 2008-10-01 | 2017-10-10 | Covidien Lp | Endoscopic ultrasound-guided biliary access system |
| US9186128B2 (en) | 2008-10-01 | 2015-11-17 | Covidien Lp | Needle biopsy device |
| US9332973B2 (en) | 2008-10-01 | 2016-05-10 | Covidien Lp | Needle biopsy device with exchangeable needle and integrated needle protection |
| US11298113B2 (en) | 2008-10-01 | 2022-04-12 | Covidien Lp | Device for needle biopsy with integrated needle protection |
| US8968210B2 (en) | 2008-10-01 | 2015-03-03 | Covidien LLP | Device for needle biopsy with integrated needle protection |
| GB0903496D0 (en) * | 2009-02-27 | 2009-04-08 | Cambridge Entpr Ltd | Methods for identification |
| ES2351569B8 (es) | 2009-05-07 | 2012-06-20 | Bcn Peptides S.A. | Ligandos peptídicos de receptores de somatostatina. |
| GB0922369D0 (en) * | 2009-12-22 | 2010-02-03 | Hammersmith Imanet Ltd | Labelled biotin conjugates |
| CN104768565B (zh) * | 2012-11-01 | 2017-04-26 | 益普生制药股份有限公司 | 促生长素抑制素类似物及其二聚体 |
| TWI523863B (zh) | 2012-11-01 | 2016-03-01 | 艾普森藥品公司 | 體抑素－多巴胺嵌合體類似物 |
| JP6410339B2 (ja) * | 2013-03-25 | 2018-10-24 | 国立大学法人千葉大学 | 放射性核種標識オクトレオチド誘導体 |
| AU2017217271C1 (en) | 2016-02-09 | 2021-08-05 | Cdrd Ventures Inc. | Somatostatin receptor antagonist compounds and methods of using the same |
| DK3568205T3 (da) | 2017-01-12 | 2023-10-09 | Radiomedix Inc | Behandling af cancerceller, der overeksprimerer somatostatinreceptorer ved at anvende radioisotop-chelaterede ocreotid-derivater |
| CN108440664A (zh) * | 2018-03-27 | 2018-08-24 | 上海欣科医药有限公司 | 一种用于癌症检测的生长抑素类似物及其制备方法和应用 |
| CN112538103B (zh) * | 2020-12-28 | 2022-10-25 | 合肥科生景肽生物科技有限公司 | 制备生长激素释放抑制素的方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5819669B2 (ja) * | 1978-10-28 | 1983-04-19 | 白井松新薬株式会社 | 新規生理活性ペプチド化合物及びその製造法 |
| US5620675A (en) * | 1992-06-23 | 1997-04-15 | Diatech, Inc. | Radioactive peptides |
| US6051206A (en) * | 1994-06-03 | 2000-04-18 | Diatide, Inc | Radiolabeled somatostatin-derived peptides for imaging and therapeutic uses |
| US6355613B1 (en) * | 1996-07-31 | 2002-03-12 | Peptor Limited | Conformationally constrained backbone cyclized somatostatin analogs |
| US6180082B1 (en) * | 1997-11-24 | 2001-01-30 | Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College | Method to enhance tissue accumulation of radiolabeled compounds |
| US6358491B1 (en) * | 1999-08-27 | 2002-03-19 | Berlex Laboratories, Inc. | Somatostatin analogs |
| EP1086947A1 (en) * | 1999-09-01 | 2001-03-28 | Pfizer Products Inc. | Somatostatin antagonists and agonists that act at the SST subtype 2 receptor |
| EP1283216A1 (en) | 2001-08-10 | 2003-02-12 | Mallinckrodt Inc. | Somatostatin analogues binding to all somatostatin receptor subtypes and their use |
-
2001
- 2001-08-10 EP EP01203033A patent/EP1283216A1/en not_active Withdrawn
-
2002
- 2002-08-07 US US10/486,310 patent/US7192570B2/en not_active Expired - Fee Related
- 2002-08-07 DE DE60211917T patent/DE60211917T2/de not_active Expired - Lifetime
- 2002-08-07 PT PT02794598T patent/PT1419178E/pt unknown
- 2002-08-07 EP EP02794598A patent/EP1419178B1/en not_active Expired - Lifetime
- 2002-08-07 WO PCT/EP2002/009004 patent/WO2003014158A1/en not_active Ceased
- 2002-08-07 AT AT02794598T patent/ATE328005T1/de not_active IP Right Cessation
- 2002-08-07 AU AU2002333396A patent/AU2002333396B2/en not_active Ceased
- 2002-08-07 ES ES02794598T patent/ES2266616T3/es not_active Expired - Lifetime
- 2002-08-07 JP JP2003519107A patent/JP2005508886A/ja not_active Ceased
- 2002-08-07 DK DK02794598T patent/DK1419178T3/da active
- 2002-08-07 CA CA002456881A patent/CA2456881A1/en not_active Abandoned
-
2006
- 2006-08-29 CY CY20061101213T patent/CY1105177T1/el unknown
-
2007
- 2007-03-08 US US11/683,734 patent/US7541018B2/en not_active Expired - Fee Related
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