BR112015012530A2 - ligantes de receptor da neurotensina - Google Patents
ligantes de receptor da neurotensinaInfo
- Publication number
- BR112015012530A2 BR112015012530A2 BR112015012530A BR112015012530A BR112015012530A2 BR 112015012530 A2 BR112015012530 A2 BR 112015012530A2 BR 112015012530 A BR112015012530 A BR 112015012530A BR 112015012530 A BR112015012530 A BR 112015012530A BR 112015012530 A2 BR112015012530 A2 BR 112015012530A2
- Authority
- BR
- Brazil
- Prior art keywords
- group
- hydrogen
- alkyl
- receptor ligands
- amino
- Prior art date
Links
- 102000017922 Neurotensin receptor Human genes 0.000 title abstract 2
- 108060003370 Neurotensin receptor Proteins 0.000 title abstract 2
- 239000003446 ligand Substances 0.000 title abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000001118 alkylidene group Chemical group 0.000 abstract 2
- WAMWSIDTKSNDCU-ZETCQYMHSA-N (2s)-2-azaniumyl-2-cyclohexylacetate Chemical compound OC(=O)[C@@H](N)C1CCCCC1 WAMWSIDTKSNDCU-ZETCQYMHSA-N 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- WQMQRNCPZFUGID-UHFFFAOYSA-N 2-azaniumyladamantane-2-carboxylate Chemical compound C1C(C2)CC3CC1C(C(O)=O)(N)C2C3 WQMQRNCPZFUGID-UHFFFAOYSA-N 0.000 abstract 1
- FHJXLSAWYORMMX-UHFFFAOYSA-N 9-aminobicyclo[3.3.1]nonane-9-carboxylic acid Chemical compound C1CCC2CCCC1C2(N)C(O)=O FHJXLSAWYORMMX-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004981 cycloalkylmethyl group Chemical group 0.000 abstract 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- 239000012636 effector Substances 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/0474—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
- A61K51/0482—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group chelates from cyclic ligands, e.g. DOTA
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Physics & Mathematics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Optics & Photonics (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Abstract
resumo patente de invenção: "ligantes de receptor da neurotensina". a presente invenção refere-se a um composto da fórmula (i) em que r1 é selecionado do grupo que consiste em hidrogênio, metila e ciclopropilmetila; aa-cooh é um aminoácido selecionado do grupo que consiste em ácido 2-amino-2-adamantano carboxílico, ciclo-hexilglicina e ácido 9-amino-biciclo[3,3,1]nonano-9-carboxílico; r2 é selecionado do grupo que consiste em (c1-c6)alquila, (c3-c8)cicloalquila, (c3-c8)cicloalquilmetila, halogênio, nitro e trifluorometila; alk é (c2-c5)alquilideno; r3, r4 e r5 são cada e independentemente selecionados do grupo que consiste em hidrogênio e (c1-c4)alquila com a condição de que um de r3, r4 e r5 é da fórmula (ii) em que alk´ é (c2-c5)alquilideno; r6 é selecionado do grupo que consiste em hidrogênio e (c1-c4)alquila; e r7 é selecionado do grupo que consiste em h e um grupamento efetor; ou um sal, um solvato ou um hidrato farmacologicamente aceitável do mesmo.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12008208.6 | 2012-12-07 | ||
| EP12008208.6A EP2740726A1 (en) | 2012-12-07 | 2012-12-07 | Neurotensin receptor ligands |
| PCT/EP2013/003700 WO2014086499A1 (en) | 2012-12-07 | 2013-12-06 | Neurotensin receptor ligands |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112015012530A2 true BR112015012530A2 (pt) | 2017-09-12 |
| BR112015012530B1 BR112015012530B1 (pt) | 2022-07-19 |
Family
ID=47355771
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112015012530-1A BR112015012530B1 (pt) | 2012-12-07 | 2013-12-06 | Compostos ligantes de receptor da neurotensina, composição e kit que os compreendem |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US10961199B2 (pt) |
| EP (3) | EP2740726A1 (pt) |
| JP (2) | JP6576828B2 (pt) |
| KR (1) | KR102290803B1 (pt) |
| CN (2) | CN104837819B9 (pt) |
| AU (1) | AU2013354422B2 (pt) |
| BR (1) | BR112015012530B1 (pt) |
| CA (1) | CA2893605C (pt) |
| DK (2) | DK2928870T3 (pt) |
| ES (2) | ES2941629T3 (pt) |
| FI (1) | FI3712131T3 (pt) |
| HK (1) | HK1210148A1 (pt) |
| HU (2) | HUE050388T2 (pt) |
| IL (1) | IL239080B (pt) |
| MX (1) | MX370354B (pt) |
| PL (2) | PL3712131T3 (pt) |
| PT (2) | PT2928870T (pt) |
| RU (1) | RU2671970C2 (pt) |
| SG (2) | SG10201704564QA (pt) |
| WO (1) | WO2014086499A1 (pt) |
| ZA (1) | ZA201503446B (pt) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2954934A1 (en) * | 2014-06-11 | 2015-12-16 | 3B Pharmaceuticals GmbH | Conjugate comprising a neurotensin receptor ligand and use thereof |
| EP2954933A1 (en) * | 2014-06-10 | 2015-12-16 | 3B Pharmaceuticals GmbH | Conjugate comprising a neurotensin receptor ligand |
| EP3154638A1 (en) | 2014-06-10 | 2017-04-19 | 3B Pharmaceuticals GmbH | Conjugate comprising a neurotensin receptor ligand and use thereof |
| BR112018010535A2 (pt) | 2015-11-24 | 2018-11-13 | Transfert Plus Sec | compostos peptídicos e conjugados peptídicos para o tratamento de câncer por quimioterapia com mediação por um receptor |
| EP3279197A1 (en) | 2016-08-03 | 2018-02-07 | Friedrich-Alexander-Universität Erlangen-Nürnberg | Diagnosis, treatment and prevention of neurotensin receptor-related conditions |
| MA46952A (fr) | 2016-12-01 | 2019-10-09 | Regeneron Pharma | Anticorps anti-pd-l1 radiomarqués pour imagerie immuno-pet |
| CN118557758A (zh) | 2017-02-10 | 2024-08-30 | 瑞泽恩制药公司 | 用于免疫-pet成像的放射性标记的抗-lag3抗体 |
| JP7304846B2 (ja) | 2017-07-24 | 2023-07-07 | リジェネロン・ファーマシューティカルズ・インコーポレイテッド | 抗ｃｄ８抗体およびその使用 |
| US20220273831A1 (en) * | 2019-07-08 | 2022-09-01 | 3B Pharmaceuticals Gmbh | Compounds comprising a fibroblast activation protein ligand and use thereof |
| CN111875667B (zh) * | 2020-07-16 | 2021-12-21 | 南方科技大学 | 有机金属螯合物及其制备方法与应用、探针 |
| IL301868A (en) * | 2020-10-22 | 2023-06-01 | Nihon Mediphysics Co Ltd | A method for preparing a radioactive zirconium complex |
| KR20240007257A (ko) * | 2021-05-13 | 2024-01-16 | 더 제너럴 하스피탈 코포레이션 | 알데히드의 생체내 검출을 위한 분자 프로브 |
| EP4355377A1 (en) * | 2021-06-16 | 2024-04-24 | Fusion Pharmaceuticals Inc. | Combination comprising a neurotensin receptor binding compound, gemcitabine and nab-paclitaxel |
| WO2022261770A1 (en) * | 2021-06-16 | 2022-12-22 | Fusion Pharmaceuticals Inc. | Combination comprising a neurotensin receptor binding compound and folfirinox |
| AU2023211720A1 (en) * | 2022-01-28 | 2024-08-15 | Fusion Pharmaceuticals Inc. | Ntsr1-targeted radiopharmaceuticals and checkpoint inhibitor combination therapy |
| WO2023158802A1 (en) * | 2022-02-18 | 2023-08-24 | Full-Life Technologies U.S. Inc. | Compounds and radioligands for targeting neurotensin receptor and uses thereof |
| WO2023215778A1 (en) * | 2022-05-03 | 2023-11-09 | The University Of North Carolina At Chapel Hill | Development of ntsr targeted agents for imaging and therapy applications |
| US12091454B2 (en) | 2022-12-28 | 2024-09-17 | Development Center For Biotechnology | Humanized anti-human neurotensin receptor 1 antibodies and their uses |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4110321A (en) | 1976-07-12 | 1978-08-29 | Folkers Karl | Synthetic tridecapeptide [Gln4 ]-neurotensin having hormonal activity |
| US4425269A (en) | 1982-06-07 | 1984-01-10 | Merck & Co., Inc. | Metabolically protected analogs of neurotensin |
| US4439359A (en) | 1982-07-02 | 1984-03-27 | Merck & Co., Inc. | Cyclic octapeptide analogs of neurotensin |
| US4885363A (en) | 1987-04-24 | 1989-12-05 | E. R. Squibb & Sons, Inc. | 1-substituted-1,4,7-triscarboxymethyl-1,4,7,10-tetraazacyclododecane and analogs |
| US5021556A (en) | 1987-07-22 | 1991-06-04 | Neorx Corporation | Method of radiolabeling chelating compounds comprising sulfur atoms with metal radionuclides |
| US5075099A (en) | 1988-05-31 | 1991-12-24 | Neorx Corporation | Metal radionuclide chelating compounds for improved chelation kinetics |
| US5364613A (en) | 1989-04-07 | 1994-11-15 | Sieving Paul F | Polychelants containing macrocyclic chelant moieties |
| FR2665898B1 (fr) | 1990-08-20 | 1994-03-11 | Sanofi | Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| US5367080A (en) | 1990-11-08 | 1994-11-22 | Sterling Winthrop Inc. | Complexing agents and targeting radioactive immunoreagents useful in therapeutic and diagnostic imaging compositions and methods |
| US5965107A (en) | 1992-03-13 | 1999-10-12 | Diatide, Inc. | Technetium-99m labeled peptides for imaging |
| CA2086453A1 (en) | 1992-12-30 | 1994-07-01 | Mcgill University | Marker for neurotensin receptor |
| US5407916A (en) | 1993-02-16 | 1995-04-18 | Warner-Lambert Company | Neurotensin mimetics as central nervous system agents |
| FR2711140B1 (fr) * | 1993-10-12 | 1996-01-05 | Sanofi Sa | 1-Naphtylpyrazole-3-carboxamides substitués actifs sur la neurotensine, leur préparation, les compositions pharmaceutiques en contenant. |
| JPH11514329A (ja) | 1994-02-18 | 1999-12-07 | マリンクロット・メディカル・インコーポレイテッド | 標識化ペプチド化合物 |
| US6054557A (en) | 1995-04-04 | 2000-04-25 | Advanced Bioconcept (1994) Ltd. | Fluorescent peptides |
| EP0820466A2 (en) | 1995-04-04 | 1998-01-28 | Advanced Bioconcept Inc. | Fluorescent peptides |
| FR2732967B1 (fr) | 1995-04-11 | 1997-07-04 | Sanofi Sa | 1-phenylpyrazole-3-carboxamides substitues, actifs sur la neurotensine, leur preparation, les compositions pharmaceutiques en contenant |
| AU6352296A (en) | 1995-07-20 | 1997-02-18 | Advanced Bioconcept, Inc. | Cell sorting with fluorescent peptides |
| CA2279530C (en) | 1997-02-03 | 2009-04-28 | Mallinckrodt Inc. | A method for the detection and localization of ductal exocrine pancreas tumours |
| US5886142A (en) | 1997-05-20 | 1999-03-23 | Thomas Jefferson University | Radiolabeled thrombus imaging agents |
| WO1999052539A1 (en) | 1998-04-10 | 1999-10-21 | Mayo Foundation For Medical Education And Research | Neo-tryptophan |
| CA2374270A1 (en) | 1999-06-24 | 2000-12-28 | Ananthachari Srinivasan | Labeled neurotensin derivatives |
| EP2338525A3 (en) * | 2003-07-09 | 2011-08-03 | California Pacific Medical Center | Remote detection of substance delivery to cells |
| US20060062729A1 (en) * | 2004-09-09 | 2006-03-23 | Carraway Robert E | Enhanced ligand binding to neurotensin receptors |
| US20100111858A1 (en) * | 2007-01-19 | 2010-05-06 | Howard Carol P | Diangostic and Therapeutic Cyclooxygenase-2 Binding Ligands |
| EP2100900A1 (en) | 2008-03-07 | 2009-09-16 | Universitätsspital Basel | Bombesin analog peptide antagonist conjugates |
| EP2334642B1 (en) * | 2008-09-16 | 2014-01-01 | The Regents Of The University Of California | Simplified one-pot synthesis of [18f]sfb for radiolabeling |
| CA2745524C (en) | 2008-12-05 | 2020-06-09 | Angiochem Inc. | Conjugates of neurotensin or neurotensin analogs and uses thereof |
| EP2374003B1 (en) * | 2009-01-07 | 2015-03-11 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment, the prognostic assessment and the detection of breast cancer |
| WO2011006985A1 (en) | 2009-07-16 | 2011-01-20 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Neurotensin analogues for radioisotope targeting to neurotensin receptor-positive tumors |
| WO2011156557A2 (en) * | 2010-06-11 | 2011-12-15 | Thomas James B | Compounds active at the neurotensin receptor |
-
2012
- 2012-12-07 EP EP12008208.6A patent/EP2740726A1/en not_active Withdrawn
-
2013
- 2013-12-06 CN CN201380063364.8A patent/CN104837819B9/zh active Active
- 2013-12-06 HU HUE13814827A patent/HUE050388T2/hu unknown
- 2013-12-06 BR BR112015012530-1A patent/BR112015012530B1/pt active IP Right Grant
- 2013-12-06 PL PL20166422.4T patent/PL3712131T3/pl unknown
- 2013-12-06 CA CA2893605A patent/CA2893605C/en active Active
- 2013-12-06 FI FIEP20166422.4T patent/FI3712131T3/fi active
- 2013-12-06 PT PT138148275T patent/PT2928870T/pt unknown
- 2013-12-06 JP JP2015545697A patent/JP6576828B2/ja active Active
- 2013-12-06 DK DK13814827.5T patent/DK2928870T3/da active
- 2013-12-06 KR KR1020157018171A patent/KR102290803B1/ko active IP Right Grant
- 2013-12-06 SG SG10201704564QA patent/SG10201704564QA/en unknown
- 2013-12-06 EP EP20166422.4A patent/EP3712131B1/en active Active
- 2013-12-06 PL PL13814827T patent/PL2928870T3/pl unknown
- 2013-12-06 ES ES20166422T patent/ES2941629T3/es active Active
- 2013-12-06 AU AU2013354422A patent/AU2013354422B2/en active Active
- 2013-12-06 SG SG11201503880YA patent/SG11201503880YA/en unknown
- 2013-12-06 EP EP13814827.5A patent/EP2928870B1/en active Active
- 2013-12-06 DK DK20166422.4T patent/DK3712131T3/da active
- 2013-12-06 HU HUE20166422A patent/HUE061839T2/hu unknown
- 2013-12-06 ES ES13814827T patent/ES2795923T3/es active Active
- 2013-12-06 WO PCT/EP2013/003700 patent/WO2014086499A1/en active Application Filing
- 2013-12-06 CN CN201811305966.0A patent/CN109320502B/zh active Active
- 2013-12-06 PT PT201664224T patent/PT3712131T/pt unknown
- 2013-12-06 US US14/650,437 patent/US10961199B2/en active Active
- 2013-12-06 MX MX2015007193A patent/MX370354B/es active IP Right Grant
- 2013-12-06 RU RU2015127086A patent/RU2671970C2/ru active
-
2015
- 2015-05-18 ZA ZA2015/03446A patent/ZA201503446B/en unknown
- 2015-05-28 IL IL239080A patent/IL239080B/en active IP Right Grant
- 2015-11-03 HK HK15110838.8A patent/HK1210148A1/xx unknown
-
2019
- 2019-08-21 JP JP2019150947A patent/JP7042776B2/ja active Active
-
2020
- 2020-12-04 US US17/112,258 patent/US20210087149A1/en active Pending
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| BR112014030651A2 (pt) | inibidor de jak1 e jak2 |
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