HRP20240124T1 - Inhibitori za ret za uporabu u liječenju raka koji ima ret alteraciju - Google Patents
Inhibitori za ret za uporabu u liječenju raka koji ima ret alteraciju Download PDFInfo
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- HRP20240124T1 HRP20240124T1 HRP20240124TT HRP20240124T HRP20240124T1 HR P20240124 T1 HRP20240124 T1 HR P20240124T1 HR P20240124T T HRP20240124T T HR P20240124TT HR P20240124 T HRP20240124 T HR P20240124T HR P20240124 T1 HRP20240124 T1 HR P20240124T1
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- cancer
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- thyroid cancer
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- 201000011510 cancer Diseases 0.000 title claims 17
- 230000004075 alteration Effects 0.000 title claims 3
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Classifications
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
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- 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
- A61P35/04—Antineoplastic agents specific for metastasis
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- Pharmacology & Pharmacy (AREA)
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- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- General Chemical & Material Sciences (AREA)
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- Oncology (AREA)
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- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Claims (14)
1. Spoj, naznačen time, da je za uporabu u liječenju raka koji je RET (engl. rearranged during transfection)-promijenjen kod pojedinca kojemu je to potrebno, koja obuhvaća davanje pojedincu 300 mg ili 400 mg Spoja 1 ili njegove farmaceutski prihvatljive soli jednom dnevno, pri čemu Spoj 1 je:
[image]
gdje RET alteracija sadrži RET mutaciju ili RET fuziju, i pri čemu se rak koji je RET-promijenjen bira od raka pluća ne-malih stanica (NSCLC) i raka štitnjače.
2. Spoj, naznačen time, da je za uporabu u liječenju raka koji je RET (engl. rearranged during transfection)-promijenjen kod pojedinca kojemu je to potrebno, koja obuhvaća davanje pojedincu 400 mg Spoja 1 ili njegove farmaceutski prihvatljive soli jednom dnevno, pri čemu Spoj 1 je:
[image]
gdje RET alteracija sadrži RET mutaciju ili RET fuziju, i pritom se rak koji je RET-promijenjen bira iz skupine koju čine rak gušterače, rak pluća, kolorektalni rak, rak glave i vrata, hepatobilijarni rak i sarkom.
3. Spoj za uporabu prema patentnom zahtjevu 2, naznačen time, da:
(i) rak pluća se bira od raka pluća malih stanica (SCLC), adenokarcinoma pluća, raka pluća ne-malih stanica (NSCLC), karcinoma plućnih stanica bronhiola, i mezotelioma; i
(ii) rak glave i vrata se bira od raka žlijezde slinovnice i raka štitnjače, prvenstveno gdje se rak štitnjače bira od diferenciranog raka štitnjače (DTC), medularnog raka štitnjače (MTC) i anaplastičnog raka štitnjače, prvenstveno gdje se diferencirani rak štitnjače bira od papilarnog raka štitnjače (PTC) i folikularnog raka štitnjače.
4. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da:
(i) RET-promijenjeni rak sadrži RET fuziju;
(ii) RET-promijenjeni rak je RET fuzijski rak ne-malih stanica pluća (NSCLC); ili
(iii) RET-promijenjeni rak je RET fuzijski rak štitnjače odabran od papilarnog raka štitnjače (PTC), metastatskog papilarnog raka štitnjače, karcinoma tiroidne žlijezde, medularnog raka štitnjače (MTC), difuzne sklerozirajuće varijante papilarnog raka štitnjače i sporadičnog medularnog raka štitnjače.
5. Spoj za uporabu prema patentnom zahtjevu 4, naznačen time, da se RET fuzija bira iz skupine koju čine CLIP1, PIBF1, BCR, FGFRIOP, CEP55, CUX1, MPRIP, CCDC6, KIF5B, PTClex9, NCOA4, TRIM33, ERC1, MBD1, RAB61P2, PRKAR1A, TRIM24, KTN1, GOLGA5, HOOK3, KIAA1468, TRIM27, AKAP13, FKBP15, SPECC1L, TBL1XR1, ACBD5, KIAA1217, i MYH13, poželjno gdje se RET fuzija bira od CCDC6, KIF5B, TRIM33, TRIM24, i NCOA4; ili MPRIP, KIF5B, CCDC6, NCOA4, TRIM33, i KIAA1217; ili ERC1, GOLGA5, MYH13, PTClex9, MBD1, RAB61P2, PRKAR1A, TRIM24, KTN1, HOOK3, TRIM27, AKAP13, FKBP15, SPECC1L, TBL1XR1, ACBD5, CCDC6, NCOA4, TRIM33, KIAA1468, KIF5B, i KIAA1217.
6. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da RET-promijenjeni rak sadrži:
(i) RET mutaciju, opcionalno pritom RET mutacija je točkasta mutacija ili rezistencijska mutacija; ili
(ii) RET mutantni rak štitnjače odabran od papilarnog karcinoma štitnjače (PTC), medularnog raka štitnjače (MTC), metastatskog papilarnog raka štitnjače, difuzne sklerozirajuće varijante papilarnog raka štitnjače, karcinoma tiroidne žlijezde i sporadičnog medularnog raka štitnjače, gdje prvenstveno rak je medularni rak štitnjače (MTC).
7. Spoj za uporabu prema patentnom zahtjevu 6, naznačen time, da RET-promijenjeni rak je RET mutantni rak štitnjače, i pri čemu RET mutant je sporadičan ili pri čemu RET mutant je nasljedan.
8. Spoj za uporabu prema patentnom zahtjevu 6, naznačen time, da RET mutacija ili RET mutant je V804L, V804M, V804E, M918T, C609Y, C609S, C609G, C609R, C609F, C609W, C611R, C611S, C611G, C611Y, C611F, C611W, C618S, C618Y, C618R, C618G, C618F, C618W, C620S, C620W, C620R, C620G, C620L, C620Y, C620F, C630A, C630R, C630S, C630Y, C630F, C634W, C634Y, C634S, C634F, C634G, C634L, C634A, C634T, L790F, R844W, R844Q, R844L, A883F, A883S, A883T, K666E, K666M, ili K666N.
9. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 1 do 8, naznačen time, da rak je metastatski i odabran je od metastatskog papilarnog raka štitnjače (PTC) i metastatskog raka pluća ne-malih stanica (NSCLC).
10. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 2 do 8, naznačen time, da rak je metastatski i radi se o metastatskom raku debelog crijeva.
11. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 1 do 10, naznačen time, da je pojedinac prethodno bio tretiran s kemoterapijom, opcionalno gdje je prethodna kemoterapija odabrana od cisplatina i karboplatina.
12. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 1 i 4 do 11, naznačen time, da se pojedincu daje 300 mg Spoja 1 jednom dnevno.
13. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 1 i 4 do 11, naznačen time, da se pojedincu daje 400 mg Spoja 1 jednom dnevno.
14. Spoj za uporabu prema patentnom zahtjevu 1, naznačen time, da:
(i) RET-promijenjeni rak je RET mutantni rak štitnjače odabran od papilarnog karcinoma štitnjače (PTC), medularnog raka štitnjače (MTC), metastatskog papilarnog raka štitnjače, difuzne sklerozirajuće varijante papilarnog raka štitnjače, karcinoma tiroidne žlijezde i sporadičnog medularnog raka štitnjače; i pojedincu se oralno daje 300 mg ili 400 mg Spoja 1 jednom dnevno; ili
(ii) RET-promijenjeni rak je RET fuzijski rak ne-malih stanica pluća (NSCLC); i pojedincu se oralno daje 300 mg ili 400 mg Spoja 1 jednom dnevno; ili
(iii) RET-promijenjeni rak je RET fuzijski rak štitnjače odabran od papilarnog raka štitnjače (PTC), metastatskog papilarnog raka štitnjače, karcinoma tiroidne žlijezde, medularnog raka štitnjače (MTC), difuzne sklerozirajuće varijante papilarnog raka štitnjače i sporadičnog medularnog raka štitnjače; i pojedincu se oralno daje 300 mg ili 400 mg Spoja 1 jednom dnevno.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862652284P | 2018-04-03 | 2018-04-03 | |
| US201862656297P | 2018-04-11 | 2018-04-11 | |
| US201862657605P | 2018-04-13 | 2018-04-13 | |
| US201862741683P | 2018-10-05 | 2018-10-05 | |
| PCT/US2019/025655 WO2019195471A1 (en) | 2018-04-03 | 2019-04-03 | Ret inhibitor for use in treating cancer having a ret alteration |
| EP19718531.7A EP3773589B1 (en) | 2018-04-03 | 2019-04-03 | Ret inhibitor for use in treating cancer having a ret alteration |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20240124T1 true HRP20240124T1 (hr) | 2024-04-12 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20240124TT HRP20240124T1 (hr) | 2018-04-03 | 2019-04-03 | Inhibitori za ret za uporabu u liječenju raka koji ima ret alteraciju |
Country Status (25)
| Country | Link |
|---|---|
| US (4) | US20210100795A1 (hr) |
| EP (2) | EP3773589B1 (hr) |
| JP (3) | JP7422084B2 (hr) |
| KR (1) | KR20200139749A (hr) |
| AU (1) | AU2019247766A1 (hr) |
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| WO2016127074A1 (en) | 2015-02-06 | 2016-08-11 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as ret inhibitors |
| CN111423416B (zh) | 2015-11-02 | 2023-05-26 | 缆图药品公司 | Ret的抑制剂 |
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| US11666570B2 (en) * | 2019-07-11 | 2023-06-06 | The Board Of Trustees Of The Leland Stanford Junior University | Diagnosis and regulation of epidermal differentiation and cancer cell activity |
| US11946935B2 (en) * | 2020-08-25 | 2024-04-02 | Regents Of The University Of Minnesota | Circulating tumor markers for meningiomas |
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