HRP20200673T1 - Makrociklički inhibitori mcl1 za liječenje raka - Google Patents
Makrociklički inhibitori mcl1 za liječenje raka Download PDFInfo
- Publication number
- HRP20200673T1 HRP20200673T1 HRP20200673TT HRP20200673T HRP20200673T1 HR P20200673 T1 HRP20200673 T1 HR P20200673T1 HR P20200673T T HRP20200673T T HR P20200673TT HR P20200673 T HRP20200673 T HR P20200673T HR P20200673 T1 HRP20200673 T1 HR P20200673T1
- Authority
- HR
- Croatia
- Prior art keywords
- solid form
- compound
- pharmaceutically acceptable
- acceptable salt
- cancer
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title claims 7
- 201000011510 cancer Diseases 0.000 title claims 5
- 102100026539 Induced myeloid leukemia cell differentiation protein Mcl-1 Human genes 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 101150094281 mcl1 gene Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 17
- 239000007787 solid Substances 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 10
- 238000000634 powder X-ray diffraction Methods 0.000 claims 3
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 2
- 230000002489 hematologic effect Effects 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 239000012752 auxiliary agent Substances 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 238000000354 decomposition reaction Methods 0.000 claims 1
- 238000004807 desolvation Methods 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000008018 melting Effects 0.000 claims 1
- 238000002844 melting Methods 0.000 claims 1
- 150000004682 monohydrates Chemical class 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 238000001757 thermogravimetry curve Methods 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D497/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
- C07D497/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D515/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (24)
1. Spoj naznačen time što je 17-kloro-5,13,14,22-tetrametil-28-oksa-2,9-ditia-5,6,12,13,22-pentaazaheptaciklo[27.7.1.14,7.011,15.016,21.020,24.030,35]oktatriakonta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridekaen-23-karboksilna kiselina (Formula I)
[image]
ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema patentnom zahtjevu 1.
3. Farmaceutski prihvatljiva sol spoja prema patentnom zahtjevu 1.
4. Spoj prema patentnom zahtjevu 1, naznačen time što spoj Formule I ima strukturu (Ra)-17-kloro-5,13,14,22-tetrametil-28-oksa-2,9-ditia-5,6,12,13,22-pentaazaheptaciklo[27.7.1.14,7.011,15.016,21.020,24.030,35]oktatriakonta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridekaen-23-karboksilna kiselina (Formula II)
[image]
ili njegova farmaceutski prihvatljiva sol.
5. Spoj prema patentnom zahtjevu 4.
6. Farmaceutski prihvatljiva sol spoja prema patentnom zahtjevu 4.
7. Spoj prema patentnom zahtjevu 1, naznačen time što spoj Formule I ima strukturu (Sa)-17-kloro-5,13,14,22-tetrametil-28-oksa-2,9-ditia-5,6,12,13,22-pentaazaheptaciklo[27.7.1.14,7.011,15.016,21.020,24.030,35]oktatriakonta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridekaen-23-karboksilna kiselina (Formula III)
[image]
ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema patentnom zahtjevu 7.
9. Farmaceutski prihvatljiva sol spoja prema patentnom zahtjevu 7.
10. Spoj, ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od patentnih zahtjeva 1-9, naznačen time što je u kristalnom obliku.
11. Kruti oblik (Ra)-17-kloro-5,13,14,22-tetrametil-28-oksa-2,9-ditia-5,6,12,13,22-pentaazaheptaciklo[27.7.1.14,7.011,15.016,21.020,24.030,35]oktatriakonta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridekaen-23-karboksilna kiselina (Formula II)
[image]
ili njegova farmaceutski prihvatljiva sol.
12. Kruti oblik prema patentnom zahtjevu 11, naznačen time što kruti oblik je Oblik A monohidrata (Ra)-17-kloro-5,13,14,22-tetrametil-28-oksa-2,9-ditia-5,6,12,13,22-pentaazaheptaciklo[27.7.1.14,7.011,15.016,21.020,24.030,35]oktatriakonta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridekaen-23-karboksilne kiseline koji ima XRPD uzorak koji obuhvaća najmanje jedan vrh izražen kao 2Θ (±0.2°) odabran od 5,4°, 7,0°, 8,4°, 10,7°, 12,5°, 13,1°, 14,4°, 15,1°, 15,6°, 17,1° i 18,2°.
13. Kruti oblik prema patentnom zahtjevu 12, naznačen time što kruti oblik ima XRPD uzorak koji obuhvaća najmanje jedan vrh izražen kao 2θ (±0.2°) odabran od 7,0°, 8,4° i 12,5°.
14. Kruti oblik prema patentnom zahtjevu 12, naznačen time što kruti oblik ima XRPD uzorak uglavnom sličan kao na Slici 1.
15. Kruti oblik prema patentnom zahtjevu 12, naznačen time što kruti oblik ima DSC termogram koji obuhvaća endotermu s nastupom desolvacije na oko 121 °C i maksimumom na oko 152 °C.
16. Kruti oblik prema patentnom zahtjevu 12, naznačen time što kruti oblik ima DSC termogram koji obuhvaća endotermu s nastupom taljenja/ raspadanja na oko 181 °C i maksimumom na oko 194 °C.
17. Kruti oblik prema patentnom zahtjevu 12, naznačen time što kruti oblik ima DSC uzorak uglavnom sličan Slici 2.
18. Kruti oblik prema patentnom zahtjevu 12, naznačen time što kruti oblik ima TGA termogram koji pokazuje gubitak mase od oko 4% pri zagrijavanju od oko 25 °C do oko 160 °C.
19. Kruti oblik prema patentnom zahtjevu 12, naznačen time što kruti oblik ima TGA uzorak uglavnom sličan kao na Slici 2.
20. Farmaceutski pripravak naznačen time što sadrži spoj prema bilo kojem od zahtjeva 1-11, ili njegova farmaceutski prihvatljiva sol i farmaceutski pomoćno sredstvo, nosač ili razrjeđivač.
21. A spoj prema bilo kojem od zahtjeva 1-19, ili njegova farmaceutski prihvatljiva sol, naznačen time što je za upotrebu u liječenju raka.
22. Spoj za uporabu prema patentnom zahtjevu 21, naznačen time što rak je hematološki karcinom ili solidni tumor.
23. Spoj za uporabu prema patentnom zahtjevu 22, naznačen time što je hematološki karcinom odabran od akutne mijeloidne leukemije, multiplog mijeloma, limfoma plaštenih stanica, kronične limfocitne leukemije, difuznog velikog B staničnog limfoma, Burkittovog limfoma i folikularnog limfoma.
24. Spoj za uporabu prema patentnom zahtjevu 22, naznačen time što je solidni tumor odabran od karcinoma pluća ne-malih stanica, karcinoma pluća malih stanica, raka dojke, neuroblastoma, raka prostate, melanoma, raka gušterače, raka maternice, raka endometrija i raka debelog crijeva.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662326156P | 2016-04-22 | 2016-04-22 | |
| EP17720720.6A EP3445767B1 (en) | 2016-04-22 | 2017-04-21 | Macrocyclic mcl1 inhibitors for treating cancer |
| PCT/EP2017/059511 WO2017182625A1 (en) | 2016-04-22 | 2017-04-21 | Macrocyclic mcl1 inhibitors for treating cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20200673T1 true HRP20200673T1 (hr) | 2020-07-10 |
Family
ID=58664658
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20200673TT HRP20200673T1 (hr) | 2016-04-22 | 2020-04-28 | Makrociklički inhibitori mcl1 za liječenje raka |
Country Status (37)
| Country | Link |
|---|---|
| US (4) | US9840518B2 (hr) |
| EP (1) | EP3445767B1 (hr) |
| JP (1) | JP6894449B2 (hr) |
| KR (1) | KR102388208B1 (hr) |
| CN (1) | CN109071566B (hr) |
| AR (1) | AR108301A1 (hr) |
| AU (1) | AU2017252222B2 (hr) |
| BR (1) | BR112018070677B1 (hr) |
| CA (1) | CA3020378A1 (hr) |
| CL (1) | CL2018002410A1 (hr) |
| CO (1) | CO2018008759A2 (hr) |
| CR (1) | CR20180499A (hr) |
| CY (1) | CY1123186T1 (hr) |
| DK (1) | DK3445767T3 (hr) |
| DO (1) | DOP2018000222A (hr) |
| EA (1) | EA036551B1 (hr) |
| ES (1) | ES2791319T3 (hr) |
| HR (1) | HRP20200673T1 (hr) |
| HU (1) | HUE049591T2 (hr) |
| IL (1) | IL262237B (hr) |
| LT (1) | LT3445767T (hr) |
| MA (1) | MA44721B1 (hr) |
| ME (1) | ME03729B (hr) |
| MX (1) | MX2018012711A (hr) |
| NI (1) | NI201800093A (hr) |
| PE (1) | PE20181803A1 (hr) |
| PH (1) | PH12018502227A1 (hr) |
| PL (1) | PL3445767T3 (hr) |
| PT (1) | PT3445767T (hr) |
| RS (1) | RS60257B1 (hr) |
| SG (1) | SG11201805838UA (hr) |
| SI (1) | SI3445767T1 (hr) |
| SV (1) | SV2018005742A (hr) |
| TN (1) | TN2018000319A1 (hr) |
| TW (1) | TWI742074B (hr) |
| WO (1) | WO2017182625A1 (hr) |
| ZA (1) | ZA201807766B (hr) |
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| EP3782636B1 (en) | 2016-02-04 | 2024-05-15 | The Johns Hopkins University | Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof |
| US11708391B2 (en) | 2016-02-04 | 2023-07-25 | The Johns Hopkins University | Rapaglutins, novel inhibitors of GLUT and use thereof |
| US11066416B2 (en) | 2016-02-04 | 2021-07-20 | The Johns Hopkins University | Rapafucin derivative compounds and methods of use thereof |
| CO2018008759A2 (es) | 2016-04-22 | 2018-09-20 | Astrazeneca Ab | Inhibidores de mcl-1 y métodos de uso de los mismos |
| EP3458459B1 (en) | 2016-05-19 | 2022-04-27 | Bayer Aktiengesellschaft | Macrocyclic indole derivatives |
| TW201904976A (zh) * | 2017-03-31 | 2019-02-01 | 瑞典商阿斯特捷利康公司 | Ｍｃｌ-１抑制劑及其使用方法 |
| TWI781996B (zh) | 2017-03-31 | 2022-11-01 | 瑞典商阿斯特捷利康公司 | 合成ｍｃｌ-１抑制劑之方法 |
| BR112020003180A2 (pt) | 2017-08-15 | 2020-09-15 | AbbVie Deutschland GmbH & Co. KG | inibidores macrocíclicos de mcl-1 e métodos de uso |
| WO2019035899A1 (en) * | 2017-08-15 | 2019-02-21 | Abbvie Inc. | MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE |
| EP3710450A1 (en) * | 2017-11-17 | 2020-09-23 | Bayer Aktiengesellschaft | Macrocyclic chlorine substituted indole derivatives |
| US11401278B2 (en) | 2017-11-17 | 2022-08-02 | The Broad Institute, Inc. | Macrocyclic indole derivatives |
| EP3710449B1 (en) * | 2017-11-17 | 2022-07-06 | The Broad Institute, Inc. | Macrocyclic fluorine substituted indole derivatives as mcl-1 inhibitors, for use in the treatment of cancer |
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| TW202106693A (zh) * | 2019-04-30 | 2021-02-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 吲哚類大環衍生物、其製備方法及其在醫藥上的應用 |
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| EP4008324A1 (en) | 2020-12-07 | 2022-06-08 | Cellestia Biotech AG | Combinations comprising an inhibitor of an anti-apoptotic protein, such as bcl-2, bcl-xl, bclw or mcl-1, and a notch signaling pathway inhibitor for treating cancer |
| AU2021403616A1 (en) | 2020-12-17 | 2023-08-03 | Janssen Pharmaceutica Nv | Branched macrocyclic 4-(pyrazol-5-yl)-indole derivatives as inhibitors of mcl-1 |
| MX2023009475A (es) | 2021-02-12 | 2023-08-22 | Janssen Pharmaceutica Nv | Derivados macrociclicos 1,3-con puente 6-cloro-7-pirazol-4-il-1h-i ndol-2-carboxilato y 6-cloro-7-pirimidina-5-il-1h-indol-2-carboxil ato como inhibidores de mcl-1 para el tratamiento del cancer. |
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