SG11201805380YA - Urea-based prostate specific membrane antigen (psma) inhibitors for imaging and therapy - Google Patents
Urea-based prostate specific membrane antigen (psma) inhibitors for imaging and therapyInfo
- Publication number
- SG11201805380YA SG11201805380YA SG11201805380YA SG11201805380YA SG11201805380YA SG 11201805380Y A SG11201805380Y A SG 11201805380YA SG 11201805380Y A SG11201805380Y A SG 11201805380YA SG 11201805380Y A SG11201805380Y A SG 11201805380YA SG 11201805380Y A SG11201805380Y A SG 11201805380YA
- Authority
- SG
- Singapore
- Prior art keywords
- international
- pennsylvania
- formula
- psma
- philadelphia
- Prior art date
Links
Classifications
-
- 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
- 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
- A61K51/0478—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 complexes from non-cyclic ligands, e.g. EDTA, MAG3
-
- 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
- A61K51/0491—Sugars, nucleosides, nucleotides, oligonucleotides, nucleic acids, e.g. DNA, RNA, nucleic acid aptamers
-
- 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
- A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Optics & Photonics (AREA)
- Epidemiology (AREA)
- Physics & Mathematics (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Crystallography & Structural Chemistry (AREA)
- Urology & Nephrology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyridine Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
- Nuclear Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 6 July 2017 (06.07.2017) WIPOIPCT (10) International Publication Number WO 2017/116994 A1 (51) International Patent Classification: G01N33/60 (2006.01) C12Q 1/37{2006.01) G01N33/68 (2006.01) (21) International Application Number: PCT/US2016/068327 (22) International Filing Date: 22 December 2016 (22.12.2016) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/273,786 31 December 2015 (31.12.2015) US 15/385,490 20 December 2016 (20.12.2016) US (71) Applicant: FIVE ELEVEN PHARMA INC. [US/US]; 3700 Market St. Suite 305, Philadelphia, Pennsylvania 19104 (US). (72) Inventors: KUNG, Hank F.; 232 N. Highland Road, Springfield, Pennsylvania 19064 (US). PLOESSL, Karl; 1525 Delaware Ave. #3, Wilmington, Delaware 19806 (US). CHOI, Seok Rye; 52 Andrew Court, Aston, Pennsylvania 19014 (US). ZHA, Zhihao; 221 S. 44th Street, Apt. 2-F, Philadelphia, Pennsylvania 19104 (US). WU, Zehui; 503S 41st Street, Apt. 302, Philadelphia, Pennsylvania 19104 (US). (74) Agents: COVERT, John M. et al.; Sterne, Kessler, Gold stein & Fox PLLC, 1100 New York Avenue, NW, Wash ington, District of Columbia 20005 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available)'. AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available)'. ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3)) — before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h)) •t 0\ 0\ o CJ (54) Title: UREA-BASED PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITORS FOR IMAGING AND THER APY (57) : The present invention relates to compounds according to Formula I and Formula IV. These compounds display very good binding affinities to the PSMA binding sites. They can be labeled with [68Ga]GaC13 with high yields and excellent radiochem - ical purity. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or Formula IV, or a pharmaceutically acceptable salt thereof.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562273786P | 2015-12-31 | 2015-12-31 | |
| US15/385,490 US10688200B2 (en) | 2015-12-31 | 2016-12-20 | Urea-based prostate specific membrane antigen (PSMA) inhibitors for imaging and therapy |
| PCT/US2016/068327 WO2017116994A1 (en) | 2015-12-31 | 2016-12-22 | Urea-based prostate specific membrane antigen (psma) inhibitors for imaging and therapy |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201805380YA true SG11201805380YA (en) | 2018-07-30 |
Family
ID=59225798
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201805380YA SG11201805380YA (en) | 2015-12-31 | 2016-12-22 | Urea-based prostate specific membrane antigen (psma) inhibitors for imaging and therapy |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US10688200B2 (en) |
| EP (1) | EP3397968B1 (en) |
| JP (1) | JP6850027B2 (en) |
| KR (1) | KR20180098373A (en) |
| CN (1) | CN108541302B (en) |
| AU (2) | AU2016380151A1 (en) |
| CA (1) | CA3010295C (en) |
| DK (1) | DK3397968T3 (en) |
| EA (1) | EA201891544A1 (en) |
| HK (1) | HK1255215A1 (en) |
| IL (1) | IL260342A (en) |
| MX (1) | MX2018008168A (en) |
| SG (1) | SG11201805380YA (en) |
| WO (1) | WO2017116994A1 (en) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9951324B2 (en) | 2010-02-25 | 2018-04-24 | Purdue Research Foundation | PSMA binding ligand-linker conjugates and methods for using |
| MX2016005013A (en) | 2013-10-18 | 2017-02-28 | Deutsches Krebsforsch | Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer. |
| US10688200B2 (en) | 2015-12-31 | 2020-06-23 | Five Eleven Pharma Inc. | Urea-based prostate specific membrane antigen (PSMA) inhibitors for imaging and therapy |
| PT3925952T (en) * | 2016-03-22 | 2023-12-13 | Univ Johns Hopkins | Prostate-specific membrane antigen targeted high-affinity agents for endoradiotherapy of prostate cancer |
| WO2018204477A1 (en) | 2017-05-02 | 2018-11-08 | Cornell University | Methods and reagents for tumor targeting with greater efficacy and less toxicity |
| US11478558B2 (en) * | 2017-05-30 | 2022-10-25 | The Johns Hopkins University | Prostate-specific membrane antigen targeted high-affinity agents for endoradiotherapy of prostate cancer |
| IL274072B1 (en) | 2017-12-11 | 2024-07-01 | Univ Muenchen Tech | Psma ligands for imaging and endoradiotherapy |
| US20190184040A1 (en) * | 2017-12-15 | 2019-06-20 | Wisconsin Alumni Research Foundation | Targeted Macrocyclic Agents for Dual Modality PET and MRI Imaging of Cancer |
| MX2018003175A (en) * | 2018-03-14 | 2019-09-16 | Instituto Nac De Investigaciones Nucleares | 177lu-dota-hynic-ipsma as a therapeutic radiopharmaceutical targeting prostate-specific membrane antigen. |
| CN109438517B (en) * | 2018-12-27 | 2021-01-08 | 北京久杰净化工程技术有限公司 | Complex of bifunctional linking agent coordinated with carbonyl metal core and preparation method thereof |
| KR20220004125A (en) * | 2019-04-26 | 2022-01-11 | 파이브 일레븐 파마 인크. | Prostate-specific membrane antigen (PSMA) inhibitors as diagnostic and radionuclide therapeutics |
| WO2020252598A1 (en) | 2019-06-21 | 2020-12-24 | Provincial Health Services Authority | Radiolabeled compounds targeting the prostate-specific membrane antigen |
| CN115380117A (en) * | 2020-02-18 | 2022-11-22 | 恩多塞特公司 | Methods of treating PSMA-expressing cancers |
| AU2021352915A1 (en) * | 2020-10-01 | 2023-06-08 | Cornell University | Methods and compositions for increasing uptake, internalization, and/or retention of small molecule ligands |
| CN112358422B (en) * | 2020-10-16 | 2023-06-23 | 中国辐射防护研究院 | Preparation method of novel chelating agent NBED |
| US20240158420A1 (en) * | 2021-03-17 | 2024-05-16 | Five Eleven Pharma, Inc | [18f]a1f labeled psma targeting molecular probe and preparation method therefor |
| CN113372285B (en) * | 2021-05-28 | 2024-06-18 | 西南医科大学附属医院 | Prostate specific membrane antigen inhibitor, radionuclide marker, preparation method and application thereof |
| CN114436905A (en) * | 2022-01-24 | 2022-05-06 | 攀枝花学院 | Purification method of 3-aldehyde-4-hydroxy methyl phenylacetate |
| CN116514735A (en) * | 2022-01-30 | 2023-08-01 | 晶核生物医药科技(南京)有限公司 | Peptide urea derivative, pharmaceutical composition containing same and application of peptide urea derivative |
| CN114874122A (en) * | 2022-05-31 | 2022-08-09 | 南京航空航天大学 | Novel small molecule inhibitor and preparation method and application thereof |
| WO2024021556A1 (en) * | 2023-02-02 | 2024-02-01 | 北京师范大学 | Radioactive metal complex targeting prostate specific membrane antigen and labeling ligand thereof |
| CN116507630A (en) * | 2023-02-14 | 2023-07-28 | 北京师范大学 | PSMA targeted radioactive metal complex containing nitro aromatic heterocyclic group and preparation thereof |
| CN118496299A (en) * | 2023-02-16 | 2024-08-16 | 无锡诺宇医药科技有限公司 | PSMA targeted radioactive diagnosis and treatment integrated medicine and synthesis and application thereof |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI1472541T1 (en) | 2002-01-10 | 2010-12-31 | Univ Johns Hopkins | Imaging agents and methods of imaging naaladase of psma |
| US8338565B2 (en) | 2008-08-20 | 2012-12-25 | Ensemble Therapeutics Corporation | Macrocyclic compounds for inhibition of tumor necrosis factor alpha |
| CN107325127B (en) * | 2011-06-15 | 2020-09-01 | 癌靶技术有限责任公司 | Chelated PSMA inhibitors |
| WO2013022797A1 (en) | 2011-08-05 | 2013-02-14 | Molecular Insight Pharmaceuticals | Radiolabeled prostate specific membrane antigen inhibitors |
| CN104203942B (en) * | 2011-11-30 | 2017-04-12 | 约翰霍普金斯大学 | Homomultivalent and heteromultivalent inhibitors of prostate specific membrane antigen (PMSA) and uses thereof |
| US9636413B2 (en) * | 2012-11-15 | 2017-05-02 | Endocyte, Inc. | Conjugates for treating diseases caused by PSMA expressing cells |
| WO2014110372A1 (en) * | 2013-01-14 | 2014-07-17 | Molecular Insight Pharmaceuticals | Triazine based radiopharmaceuticals and radioimaging agents |
| US10406246B2 (en) | 2013-10-17 | 2019-09-10 | Deutsches Kresbsforschungszentrum | Double-labeled probe for molecular imaging and use thereof |
| EP2862857A1 (en) * | 2013-10-18 | 2015-04-22 | Deutsches Krebsforschungszentrum | Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer |
| MX2016005013A (en) * | 2013-10-18 | 2017-02-28 | Deutsches Krebsforsch | Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer. |
| KR102457827B1 (en) * | 2013-11-14 | 2022-10-24 | 엔도사이트, 인코포레이티드 | Compounds for positron emission tomography |
| CA3215134A1 (en) * | 2014-05-06 | 2015-11-12 | The Johns Hopkins University | Metal/radiometal-labeled psma inhibitors for psma-targeted imaging and radiotherapy |
| US10688200B2 (en) | 2015-12-31 | 2020-06-23 | Five Eleven Pharma Inc. | Urea-based prostate specific membrane antigen (PSMA) inhibitors for imaging and therapy |
-
2016
- 2016-12-20 US US15/385,490 patent/US10688200B2/en active Active - Reinstated
- 2016-12-22 JP JP2018534552A patent/JP6850027B2/en active Active
- 2016-12-22 AU AU2016380151A patent/AU2016380151A1/en not_active Abandoned
- 2016-12-22 WO PCT/US2016/068327 patent/WO2017116994A1/en active Application Filing
- 2016-12-22 MX MX2018008168A patent/MX2018008168A/en unknown
- 2016-12-22 EA EA201891544A patent/EA201891544A1/en unknown
- 2016-12-22 SG SG11201805380YA patent/SG11201805380YA/en unknown
- 2016-12-22 KR KR1020187021593A patent/KR20180098373A/en not_active Application Discontinuation
- 2016-12-22 DK DK16882430.8T patent/DK3397968T3/en active
- 2016-12-22 CA CA3010295A patent/CA3010295C/en active Active
- 2016-12-22 EP EP16882430.8A patent/EP3397968B1/en active Active
- 2016-12-22 CN CN201680079844.7A patent/CN108541302B/en active Active
-
2018
- 2018-06-28 IL IL260342A patent/IL260342A/en unknown
- 2018-11-09 HK HK18114343.5A patent/HK1255215A1/en unknown
-
2023
- 2023-06-13 AU AU2023203682A patent/AU2023203682A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| DK3397968T3 (en) | 2021-11-01 |
| CA3010295C (en) | 2023-09-26 |
| EP3397968A4 (en) | 2019-11-27 |
| US10688200B2 (en) | 2020-06-23 |
| IL260342A (en) | 2018-08-30 |
| CN108541302B (en) | 2023-02-14 |
| EP3397968B1 (en) | 2021-09-29 |
| US20170189568A1 (en) | 2017-07-06 |
| AU2016380151A1 (en) | 2018-07-19 |
| CA3010295A1 (en) | 2017-07-06 |
| HK1255215A1 (en) | 2019-08-09 |
| JP6850027B2 (en) | 2021-03-31 |
| JP2019508374A (en) | 2019-03-28 |
| WO2017116994A1 (en) | 2017-07-06 |
| CN108541302A (en) | 2018-09-14 |
| EP3397968A1 (en) | 2018-11-07 |
| MX2018008168A (en) | 2019-02-20 |
| AU2023203682A1 (en) | 2023-07-06 |
| KR20180098373A (en) | 2018-09-03 |
| EA201891544A1 (en) | 2018-11-30 |
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