HRP20230859T1 - Kruti oblici soli tartarata 3-((1r,3r)-1-(2,6-difluoro-4-((1-(3-fluoropropil)azetidin-3-il)amino)fenil)-3-metil-1,3,4,9-tetrahidro-2hpirido[3,4-b]indol-2-il)-2,2-difluoropropan-1-ol, postupak njihove proizvodnje i postupci njihove primjene u liječenju raka - Google Patents
Kruti oblici soli tartarata 3-((1r,3r)-1-(2,6-difluoro-4-((1-(3-fluoropropil)azetidin-3-il)amino)fenil)-3-metil-1,3,4,9-tetrahidro-2hpirido[3,4-b]indol-2-il)-2,2-difluoropropan-1-ol, postupak njihove proizvodnje i postupci njihove primjene u liječenju raka Download PDFInfo
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- HRP20230859T1 HRP20230859T1 HRP20230859TT HRP20230859T HRP20230859T1 HR P20230859 T1 HRP20230859 T1 HR P20230859T1 HR P20230859T T HRP20230859T T HR P20230859TT HR P20230859 T HRP20230859 T HR P20230859T HR P20230859 T1 HRP20230859 T1 HR P20230859T1
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- 238000000034 method Methods 0.000 title claims 13
- 239000007787 solid Substances 0.000 title claims 8
- 206010028980 Neoplasm Diseases 0.000 title claims 4
- GQCXHIKRWBIQMD-AKJBCIBTSA-N 3-[(1R,3R)-1-[2,6-difluoro-4-[[1-(3-fluoropropyl)azetidin-3-yl]amino]phenyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl]-2,2-difluoropropan-1-ol Chemical compound FC1=C(C(=CC(=C1)NC1CN(C1)CCCF)F)[C@H]1N([C@@H](CC2=C1NC1=CC=CC=C21)C)CC(CO)(F)F GQCXHIKRWBIQMD-AKJBCIBTSA-N 0.000 title 1
- 150000003892 tartrate salts Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 23
- 238000000634 powder X-ray diffraction Methods 0.000 claims 16
- 239000000825 pharmaceutical preparation Substances 0.000 claims 7
- 206010006187 Breast cancer Diseases 0.000 claims 5
- 208000026310 Breast neoplasm Diseases 0.000 claims 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 238000001953 recrystallisation Methods 0.000 claims 2
- 206010055113 Breast cancer metastatic Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 208000027706 hormone receptor-positive breast cancer Diseases 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 239000000543 intermediate Substances 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims 1
- 208000036907 triple-positive breast carcinoma Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Claims (22)
1. Spoj B, naznačen time, da ima strukturu:
[image]
2. Kristalni oblik, naznačen time, da sadrži Spoj B prema patentnom zahtjevu 1,
[image]
koji ima uzorak rendgenske difrakcije na prahu s vrhovima na 19,32, 20,26, 21,63, 23,28 ili 24,81 ±θ,1° 2θ (±0,1°2θ).
3. Kristalni oblik prema patentnom zahtjevu 2, naznačen time, da kristalni oblik Spoja B ima uzorak rendgenske difrakcije na prahu s jednim, dva, tri, četiri, pet, šest, sedam, osam, devet, deset, jedanaest, dvanaest, trinaest, četrnaest, petnaest, šesnaest, sedamnaest, osamnaest, devetnaest ili dvadeset, karakterističnih vrhova rendgenske difrakcije na prahu odabranih između:
[image]
4. Kristalni oblik prema patentnom zahtjevu 2, naznačen time, da kristalni oblik Spoja B ima uzorak rendgenske difrakcije na prahu uglavnom kao što je prikazano na SL. 1.
5. Kristalni oblik koji sadrži Spoj B prema patentnom zahtjevu 1,
[image]
naznačen time, da ima uzorak rendgenske difrakcije na prahu koji sadrži vrhove na 11,49, 12,54, 19,16, 19,42 ili 24,67 ±θ,1° 2θ (±0,1°2θ).
6. Kristalni oblik prema patentnom zahtjevu 5, naznačen time, da kristalni oblik Spoja B ima uzorak rendgenske difrakcije na prahu s jednim, dva, tri, četiri, pet, šest, sedam, osam, devet, deset, jedanaest, dvanaest, trinaest, četrnaest, petnaest, šesnaest, sedamnaest, osamnaest, devetnaest ili dvadeset, karakterističnih vrhova rendgenske difrakcije na prahu odabranih između:
[image]
7. Kristalni oblik prema patentnom zahtjevu 5, naznačen time, da kristalni oblik Spoja B ima uzorak rendgenske difrakcije na prahu uglavnom kao što je prikazano na SL. 4.
8. Kristalni oblik koji sadrži Spoj B prema patentnom zahtjevu 1,
[image]
naznačen time, da ima uzorak rendgenske difrakcije na prahu koji sadrži vrhove na 11,31, 15,70, 16,54, 19,10 ili 22,76 ±0,1° 2θ.
9. Kristalni oblik prema patentnom zahtjevu 8, naznačen time, da kristalni oblik Spoja B ima uzorak rendgenske difrakcije na prahu s jednim, dva, tri, četiri, pet, šest, sedam, osam, devet, deset, jedanaest, dvanaest, trinaest, četrnaest, petnaest, šesnaest, sedamnaest, osamnaest, devetnaest ili dvadeset, karakterističnih vrhova rendgenske difrakcije na prahu odabranih između:
[image]
10. Kristalni oblik prema patentnom zahtjevu 8, naznačen time, da kristalni oblik Spoja B ima uzorak rendgenske difrakcije na prahu uglavnom kao što je prikazano na SL. 12.
11. Kristalni oblik koji sadrži Spoj B prema patentnom zahtjevu 1,
[image]
naznačen time, da ima uzorak rendgenske difrakcije na prahu koji sadrži vrhove na 12,52, 15,90, 19,66, 20,65 ili 24,99 ±0,1° 2θ.
12. Kristalni oblik prema patentnom zahtjevu 11, naznačen time, da kristalni oblik Spoja B ima uzorak rendgenske difrakcije na prahu s jednim, dva, tri, četiri, pet, šest, sedam, osam, devet, deset, jedanaest, dvanaest, trinaest, četrnaest, petnaest, šesnaest, sedamnaest, osamnaest, devetnaest ili dvadeset, karakterističnih vrhova rendgenske difrakcije na prahu odabranih između:
[image]
13. Kristalni oblik prema patentnom zahtjevu 11, naznačen time, da kristalni oblik Spoja B ima uzorak rendgenske difrakcije na prahu uglavnom kao što je prikazano na SL. 16.
14. Farmaceutski pripravak, naznačen time, da sadrži spoj prema patentnom zahtjevu 1 i/ili kruti oblik prema patentnom zahtjevu 7 i najmanje jedan farmaceutski prihvatljiv ekscipijent.
15. Spoj prema patentnom zahtjevu 1, kruti oblik prema patentnom zahtjevu 7 ili farmaceutski pripravak prema patentnom zahtjevu 14, naznačen time, da je za primjenu u postupku za liječenje raka pluća, raka jajnika, raka endometrija, raka prostate, raka maternice ili raka dojke kod pacijenta koji ima navedeni rak, gdje navedeni postupak podrazumijeva davanje pacijentu s rakom učinkovite količine spoja prema patentnom zahtjevu 1, krutog oblika prema patentnom zahtjevu 7 ili farmaceutskog pripravka prema patentnom zahtjevu 14.
16. Spoj prema patentnom zahtjevu 1, kruti oblik prema patentnom zahtjevu 7 ili farmaceutski pripravak prema patentnom zahtjevu 14, naznačen time, da je za primjenu u postupku za liječenje raka dojke kod pacijenta s rakom dojke, gdje navedeni postupak podrazumijeva davanje pacijentu s rakom učinkovite količine spoja prema patentnom zahtjevu 1, krutog oblika prema patentnom zahtjevu 7 ili farmaceutskog pripravka prema patentnom zahtjevu 14, pri čemu ovaj rak dojke je rak dojke pozitivan na hormonske receptore, HER2-pozitivan rak dojke ili trostruko negativan rak dojke.
17. Spoj, kruti oblik ili farmaceutski pripravak za primjenu prema patentnom zahtjevu 16, naznačen time, da ovaj rak dojke je metastatski rak dojke.
18. Spoj, kruti oblik ili farmaceutski pripravak za primjenu prema bilo kojem od patentnih zahtjeva 16 do 17, naznačen time, da je pacijent prethodno bio liječen jednim ili višebrojnim sredstvima protiv raka ili terapijom zračenjem.
19. Postupak za proizvodnju Spoja B,
[image]
naznačen time, da se postupak sastoji od sljedećih koraka:
[image]
20. Postupak prema patentnom zahtjevu 19, naznačen time, da postupak nadalje uključuje rekristalizaciju Spoja B u metanolu i etanolu;
[image]
21. Postupak prema patentnom zahtjevu 19, naznačen time, da postupak nadalje uključuje rekristalizaciju Spoja B u MTBE, vodi, NaOH i etanolu;
[image]
22. Postupak prema bilo kojem od patentnih zahtjeva 19 do 21, naznačen time, da se indolil intermedijeri sintetiziraju prema sljedećim koracima:
[image]
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862687930P | 2018-06-21 | 2018-06-21 | |
US201862719896P | 2018-08-20 | 2018-08-20 | |
EP19745335.0A EP3810283B1 (en) | 2018-06-21 | 2019-06-17 | Solid forms of the tartrate salt of 3-((1r,3r)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2h-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, process for their preparation and methods of their use in treating cancers |
PCT/US2019/037492 WO2019245974A1 (en) | 2018-06-21 | 2019-06-17 | Solid forms of 3-((1r,3r)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2h-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol and processes for preparing fused tricyclic compounds comprising a substituted phenyl or pyridinyl moiety, including methods of their use |
Publications (1)
Publication Number | Publication Date |
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HRP20230859T1 true HRP20230859T1 (hr) | 2023-11-10 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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HRP20230859TT HRP20230859T1 (hr) | 2018-06-21 | 2019-06-17 | Kruti oblici soli tartarata 3-((1r,3r)-1-(2,6-difluoro-4-((1-(3-fluoropropil)azetidin-3-il)amino)fenil)-3-metil-1,3,4,9-tetrahidro-2hpirido[3,4-b]indol-2-il)-2,2-difluoropropan-1-ol, postupak njihove proizvodnje i postupci njihove primjene u liječenju raka |
Country Status (29)
Country | Link |
---|---|
US (2) | US10954234B2 (hr) |
EP (2) | EP3810283B1 (hr) |
JP (4) | JP6916969B1 (hr) |
KR (2) | KR20230117761A (hr) |
CN (2) | CN117946107A (hr) |
AU (3) | AU2019290545B2 (hr) |
BR (1) | BR112020024073A2 (hr) |
CA (1) | CA3098203A1 (hr) |
CL (1) | CL2020003022A1 (hr) |
CO (1) | CO2020014604A2 (hr) |
CR (2) | CR20230409A (hr) |
DK (1) | DK3810283T3 (hr) |
ES (1) | ES2951829T3 (hr) |
FI (1) | FI3810283T3 (hr) |
HR (1) | HRP20230859T1 (hr) |
HU (1) | HUE064542T2 (hr) |
IL (1) | IL278063A (hr) |
LT (1) | LT3810283T (hr) |
MX (3) | MX2020011531A (hr) |
PE (1) | PE20211207A1 (hr) |
PH (1) | PH12020500676A1 (hr) |
PL (1) | PL3810283T3 (hr) |
PT (1) | PT3810283T (hr) |
RS (1) | RS64429B1 (hr) |
SG (1) | SG11202012171SA (hr) |
SI (1) | SI3810283T1 (hr) |
TW (1) | TW202016098A (hr) |
UA (1) | UA128114C2 (hr) |
WO (1) | WO2019245974A1 (hr) |
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SG11202012171SA (en) | 2018-06-21 | 2021-01-28 | Hoffmann La Roche | Solid forms of 3-((1r,3r)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2h-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol and processes for preparing fused tricyclic compounds comprising a substituted phenyl or pyridinyl moiety, including methods of their use |
JP2023525022A (ja) * | 2020-05-07 | 2023-06-14 | リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー | 組み合わせ |
US11918561B2 (en) | 2020-05-12 | 2024-03-05 | Genentech, Inc. | Treatment of breast cancer using combination therapies comprising GDC-9545 and a CDK4/6 inhibitor |
CN115836068A (zh) * | 2020-05-15 | 2023-03-21 | 先声药业有限公司 | 吡咯烷类化合物及其应用 |
EP4174059A1 (en) | 2020-06-28 | 2023-05-03 | Medshine Discovery Inc. | Indazole-fused cyclic compound |
MX2022015880A (es) * | 2020-06-30 | 2023-02-27 | Genentech Inc | Procesos para elaborar compuestos serd tricíclicos que tienen un resto sustituido de fenilo o piridinilo. |
WO2022140744A1 (en) * | 2020-12-23 | 2022-06-30 | Recurium Ip Holdings, Llc | Estrogen receptor modulators |
TW202237099A (zh) * | 2021-02-16 | 2022-10-01 | 美商建南德克公司 | 使用包含gdc-9545及帕他色替之組合療法治療乳癌 |
JP2024506348A (ja) * | 2021-02-16 | 2024-02-13 | ジェネンテック, インコーポレイテッド | Gdc-9545とアベマシクリブ又はリボシクリブとを含む併用療法を使用する乳がんの治療 |
CN117813288A (zh) | 2021-07-15 | 2024-04-02 | 西藏海思科制药有限公司 | 芳氨基衍生物雌激素受体调节剂及其用途 |
CN114656444A (zh) * | 2022-03-04 | 2022-06-24 | 河北松辰医药科技有限公司 | 一种2,2-二氟-1,3-丙基磺酸内酯的合成方法 |
TW202400141A (zh) | 2022-04-28 | 2024-01-01 | 瑞士商赫孚孟拉羅股份公司 | 3-((1r,3r)-1-(2,6-二氟-4-((1-(3-氟丙基)四氫吖唉-3-基)胺基)苯基)-3-甲基-1,3,4,9-四氫-2h-吡啶并[3,4-b]吲哚-2-基)-2,2-二氟丙-1-醇酒石酸鹽之固體形式 |
CN115872996B (zh) * | 2023-02-21 | 2023-05-05 | 山东绿叶制药有限公司 | 一种雌激素受体降解剂化合物及其制备方法和应用 |
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