JP7167021B2 - アルブミン結合ｐｓｍａ阻害剤 - Google Patents
アルブミン結合ｐｓｍａ阻害剤 Download PDFInfo
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- JP7167021B2 JP7167021B2 JP2019527426A JP2019527426A JP7167021B2 JP 7167021 B2 JP7167021 B2 JP 7167021B2 JP 2019527426 A JP2019527426 A JP 2019527426A JP 2019527426 A JP2019527426 A JP 2019527426A JP 7167021 B2 JP7167021 B2 JP 7167021B2
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- 125000003136 n-heptyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- 125000005963 oxadiazolidinyl group Chemical group 0.000 description 1
- 125000005882 oxadiazolinyl group Chemical group 0.000 description 1
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- 125000005968 oxazolinyl group Chemical group 0.000 description 1
- 125000006503 p-nitrobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1[N+]([O-])=O)C([H])([H])* 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 125000006245 phosphate protecting group Chemical group 0.000 description 1
- 239000004038 photonic crystal Substances 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 229960005235 piperonyl butoxide Drugs 0.000 description 1
- 125000004591 piperonyl group Chemical group C(C1=CC=2OCOC2C=C1)* 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 description 1
- 125000003072 pyrazolidinyl group Chemical group 0.000 description 1
- 125000002755 pyrazolinyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 125000001422 pyrrolinyl group Chemical group 0.000 description 1
- 238000000163 radioactive labelling Methods 0.000 description 1
- 239000012217 radiopharmaceutical Substances 0.000 description 1
- 229940121896 radiopharmaceutical Drugs 0.000 description 1
- 230000002799 radiopharmaceutical effect Effects 0.000 description 1
- 230000003439 radiotherapeutic effect Effects 0.000 description 1
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 description 1
- 229910052707 ruthenium Inorganic materials 0.000 description 1
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 description 1
- 229960002930 sirolimus Drugs 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 238000012706 support-vector machine Methods 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000005958 tetrahydrothienyl group Chemical group 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 125000005304 thiadiazolidinyl group Chemical group 0.000 description 1
- 125000005305 thiadiazolinyl group Chemical group 0.000 description 1
- 125000001984 thiazolidinyl group Chemical group 0.000 description 1
- 125000002769 thiazolinyl group Chemical group 0.000 description 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 125000005455 trithianyl group Chemical group 0.000 description 1
- 230000008728 vascular permeability Effects 0.000 description 1
- 210000005166 vasculature Anatomy 0.000 description 1
- 229960005080 warfarin Drugs 0.000 description 1
- PJVWKTKQMONHTI-UHFFFAOYSA-N warfarin Chemical compound OC=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=CC=C1 PJVWKTKQMONHTI-UHFFFAOYSA-N 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K49/00—Preparations for testing in vivo
- A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
- A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
- A61K49/10—Organic compounds
- A61K49/101—Organic compounds the carrier being a complex-forming compound able to form MRI-active complexes with paramagnetic metals
- A61K49/106—Organic compounds the carrier being a complex-forming compound able to form MRI-active complexes with paramagnetic metals the complex-forming compound being cyclic, e.g. DOTA
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D225/00—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom
- C07D225/04—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D225/08—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with two six-membered rings
-
- 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
- A61K51/0402—Organic compounds carboxylic acid carriers, fatty acids
-
- 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
- A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
- A61K51/081—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins the protein being an albumin, e.g. human serum albumin [HSA], bovine serum albumin [BSA], ovalbumin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Optics & Photonics (AREA)
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- Radiology & Medical Imaging (AREA)
- Molecular Biology (AREA)
- Urology & Nephrology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| US201662425810P | 2016-11-23 | 2016-11-23 | |
| US62/425,810 | 2016-11-23 | ||
| PCT/US2017/063182 WO2018098390A1 (en) | 2016-11-23 | 2017-11-24 | Albumin-binding psma inhibitors |
Publications (3)
| Publication Number | Publication Date |
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| JP2019535754A JP2019535754A (ja) | 2019-12-12 |
| JP2019535754A5 JP2019535754A5 (enExample) | 2021-01-07 |
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| EP (1) | EP3544960A1 (enExample) |
| JP (1) | JP7167021B2 (enExample) |
| CN (1) | CN109982998A (enExample) |
| BR (1) | BR112019010206A2 (enExample) |
| CA (1) | CA3043619A1 (enExample) |
| MX (1) | MX2019005742A (enExample) |
| WO (1) | WO2018098390A1 (enExample) |
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| KR102884167B1 (ko) * | 2017-10-22 | 2025-11-12 | 프로빈셜 헬스 서비시즈 오쏘리티 | 전립선 특이적 막 항원-발현 암의 진단 또는 치료를 위한 신규한 라디오메탈-결합 화합물 |
| US20210276971A1 (en) * | 2018-06-20 | 2021-09-09 | The Research Foundation For The State University Of New York | Triazamacrocycle-derived chelator compositions for coordination of imaging and therapy metal ions and methods of using same |
| EP3880253A1 (en) * | 2018-11-14 | 2021-09-22 | Noria Therapeutics, Inc. | Thioamide-containing compositions and methods of use thereof |
| WO2020108753A1 (en) * | 2018-11-28 | 2020-06-04 | ITM Isotopen Technologien München AG | Novel tumor antigen binding agents and uses thereof |
| CA3136979A1 (en) | 2019-04-17 | 2020-10-22 | Provincial Health Services Authority | Radiolabelled compounds for diagnosis or treatment of prostate-spe cific membrane antigen-expressing cancer |
| CN119431260A (zh) | 2019-06-21 | 2025-02-14 | 省卫生服务机构 | 靶向前列腺特异性膜抗原的放射性标记化合物 |
| CN115210240A (zh) | 2020-03-04 | 2022-10-18 | 日本医事物理股份有限公司 | 化合物及放射性标记化合物 |
| KR20230027004A (ko) * | 2020-05-06 | 2023-02-27 | 코넬 유니버시티 | 구리-함유 테라그노스틱 화합물 및 사용 방법 |
| KR20230117581A (ko) * | 2020-12-04 | 2023-08-08 | 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 | 펩티드 수용체 방사성 핵종 요법 |
| WO2022126275A1 (en) * | 2020-12-16 | 2022-06-23 | The University Of British Columbia | Radiolabeled compounds targeting the prostate-specific membrane antigen |
| CN114685599A (zh) * | 2020-12-30 | 2022-07-01 | 南京江原安迪科正电子研究发展有限公司 | 一种psma靶向抑制剂及放射性核素标记的psma靶向抑制剂、制备方法和用途 |
| WO2022186311A1 (ja) * | 2021-03-04 | 2022-09-09 | 日本メジフィジックス株式会社 | 化合物及び放射性標識化合物 |
| EP4486756A1 (en) * | 2022-03-04 | 2025-01-08 | Provincial Health Services Authority | Radiolabeled compounds targeting the prostate-specific membrane antigen |
| WO2024126687A1 (en) * | 2022-12-16 | 2024-06-20 | Silence Therapeutics Gmbh | Nucleic acids conjugated to an albumin binding moiety |
| KR20250148672A (ko) * | 2023-02-16 | 2025-10-14 | 노로이 바이오사이언스 씨오., 엘티디. | Psma 표적 방사성 약물 및 그 합성과 응용 |
| CN116217505B (zh) * | 2023-03-17 | 2024-10-01 | 南京医科大学 | 用于诊断或治疗表达前列腺特异性膜抗原癌症的新型标记靶向剂 |
Citations (6)
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| WO2010108125A2 (en) | 2009-03-19 | 2010-09-23 | The Johns Hopkins University | Psma-targeting compounds and uses thereof |
| WO2013028664A1 (en) | 2011-08-22 | 2013-02-28 | Siemens Medical Solutions Usa, Inc. | Psma imaging agents |
| JP2014524419A (ja) | 2011-08-05 | 2014-09-22 | モレキュラー インサイト ファーマシューティカルズ | 放射標識された前立腺特異的膜抗原阻害剤 |
| WO2016030329A1 (en) | 2014-08-24 | 2016-03-03 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Method for the production of 18f-labeled active esters and their application exemplified by the preparation of a psma-specific pet-tracer |
| JP2018531243A (ja) | 2015-09-30 | 2018-10-25 | ドイチェス クレブスフォルシュンクスツェントルム | 前立腺特異的膜抗原（ｐｓｍａ）の１８ｆ−タグ付加インヒビターおよび前立腺癌についての画像化剤としてのその使用 |
| JP2019535727A (ja) | 2016-11-18 | 2019-12-12 | エービーエックス・アドヴァンスド・バイオケミカル・コンパウンズ・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | ラジオフッ素化のための前駆体 |
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|---|---|---|---|---|
| GB0621973D0 (en) * | 2006-11-03 | 2006-12-13 | Philogen Spa | Binding molecules and uses thereof |
| WO2015069932A1 (en) * | 2013-11-06 | 2015-05-14 | Solstice Biologics, Ltd. | Polynucleotide constructs having disulfide groups |
| EP3069147A4 (en) * | 2013-11-14 | 2017-10-11 | Endocyte, Inc. | Compounds for positron emission tomography |
| KR20250057132A (ko) * | 2016-03-22 | 2025-04-28 | 더 존스 홉킨스 유니버시티 | 전립선 암의 내부방사선요법을 위한 전립선-특이적 막 항원 표적화된 고-친화성 제제 |
| EP3474903B1 (en) * | 2016-06-23 | 2025-01-22 | Cornell University | Double targeted constructs to affect tumor kill |
-
2017
- 2017-11-24 BR BR112019010206A patent/BR112019010206A2/pt not_active Application Discontinuation
- 2017-11-24 WO PCT/US2017/063182 patent/WO2018098390A1/en not_active Ceased
- 2017-11-24 MX MX2019005742A patent/MX2019005742A/es unknown
- 2017-11-24 CN CN201780071927.6A patent/CN109982998A/zh active Pending
- 2017-11-24 JP JP2019527426A patent/JP7167021B2/ja active Active
- 2017-11-24 EP EP17821755.0A patent/EP3544960A1/en not_active Withdrawn
- 2017-11-24 US US16/349,756 patent/US11147889B2/en active Active
- 2017-11-24 CA CA3043619A patent/CA3043619A1/en active Pending
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| WO2010108125A2 (en) | 2009-03-19 | 2010-09-23 | The Johns Hopkins University | Psma-targeting compounds and uses thereof |
| JP2014524419A (ja) | 2011-08-05 | 2014-09-22 | モレキュラー インサイト ファーマシューティカルズ | 放射標識された前立腺特異的膜抗原阻害剤 |
| WO2013028664A1 (en) | 2011-08-22 | 2013-02-28 | Siemens Medical Solutions Usa, Inc. | Psma imaging agents |
| WO2016030329A1 (en) | 2014-08-24 | 2016-03-03 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Method for the production of 18f-labeled active esters and their application exemplified by the preparation of a psma-specific pet-tracer |
| JP2018531243A (ja) | 2015-09-30 | 2018-10-25 | ドイチェス クレブスフォルシュンクスツェントルム | 前立腺特異的膜抗原（ｐｓｍａ）の１８ｆ−タグ付加インヒビターおよび前立腺癌についての画像化剤としてのその使用 |
| JP2019535727A (ja) | 2016-11-18 | 2019-12-12 | エービーエックス・アドヴァンスド・バイオケミカル・コンパウンズ・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | ラジオフッ素化のための前駆体 |
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| Shallal, Hassan M. et al.，Heterobivalent Agents Targeting PSMA and Integrin-αvβ3，Bioconjugate Chemistry ，2014年，25(2)，393-405 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3544960A1 (en) | 2019-10-02 |
| JP2019535754A (ja) | 2019-12-12 |
| CA3043619A1 (en) | 2018-05-31 |
| BR112019010206A2 (pt) | 2019-09-03 |
| US20200061218A1 (en) | 2020-02-27 |
| WO2018098390A1 (en) | 2018-05-31 |
| MX2019005742A (es) | 2019-09-13 |
| US11147889B2 (en) | 2021-10-19 |
| CN109982998A (zh) | 2019-07-05 |
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