HRP20200186T1 - Radioaktivno obilježeni derivati 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-karboksamid spojeva koji se koriste kao inhibitori atr kinaze, priprava navedenih spojeva i njihovi različiti čvrsti oblici - Google Patents
Radioaktivno obilježeni derivati 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-karboksamid spojeva koji se koriste kao inhibitori atr kinaze, priprava navedenih spojeva i njihovi različiti čvrsti oblici Download PDFInfo
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- HRP20200186T1 HRP20200186T1 HRP20200186TT HRP20200186T HRP20200186T1 HR P20200186 T1 HRP20200186 T1 HR P20200186T1 HR P20200186T T HRP20200186T T HR P20200186TT HR P20200186 T HRP20200186 T HR P20200186T HR P20200186 T1 HRP20200186 T1 HR P20200186T1
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- 150000001875 compounds Chemical class 0.000 title claims 20
- 239000007787 solid Substances 0.000 title claims 5
- 229940125775 ATR kinase inhibitor Drugs 0.000 title 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 15
- 229910052805 deuterium Inorganic materials 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 238000000034 method Methods 0.000 claims 10
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical group [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims 5
- 238000006243 chemical reaction Methods 0.000 claims 5
- 239000003054 catalyst Substances 0.000 claims 4
- 239000002904 solvent Substances 0.000 claims 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 3
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical group CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims 3
- 239000002585 base Substances 0.000 claims 3
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 claims 2
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 238000002441 X-ray diffraction Methods 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- RDOXTESZEPMUJZ-UHFFFAOYSA-N anisole Chemical compound COC1=CC=CC=C1 RDOXTESZEPMUJZ-UHFFFAOYSA-N 0.000 claims 2
- ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 claims 2
- 229910052751 metal Inorganic materials 0.000 claims 2
- 239000002184 metal Substances 0.000 claims 2
- 150000007530 organic bases Chemical class 0.000 claims 2
- 229910052763 palladium Inorganic materials 0.000 claims 2
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- LWIHDJKSTIGBAC-UHFFFAOYSA-K tripotassium phosphate Chemical compound [K+].[K+].[K+].[O-]P([O-])([O-])=O LWIHDJKSTIGBAC-UHFFFAOYSA-K 0.000 claims 2
- KZPYGQFFRCFCPP-UHFFFAOYSA-N 1,1'-bis(diphenylphosphino)ferrocene Chemical compound [Fe+2].C1=CC=C[C-]1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=C[C-]1P(C=1C=CC=CC=1)C1=CC=CC=C1 KZPYGQFFRCFCPP-UHFFFAOYSA-N 0.000 claims 1
- XTHFKEDIFFGKHM-UHFFFAOYSA-N Dimethoxyethane Chemical group COCCOC XTHFKEDIFFGKHM-UHFFFAOYSA-N 0.000 claims 1
- 229910002666 PdCl2 Inorganic materials 0.000 claims 1
- YNHIGQDRGKUECZ-UHFFFAOYSA-L PdCl2(PPh3)2 Substances [Cl-].[Cl-].[Pd+2].C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 YNHIGQDRGKUECZ-UHFFFAOYSA-L 0.000 claims 1
- 238000010976 amide bond formation reaction Methods 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 238000004132 cross linking Methods 0.000 claims 1
- 238000006880 cross-coupling reaction Methods 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 230000026030 halogenation Effects 0.000 claims 1
- 238000005658 halogenation reaction Methods 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- UZKWTJUDCOPSNM-UHFFFAOYSA-N methoxybenzene Substances CCCCOC=C UZKWTJUDCOPSNM-UHFFFAOYSA-N 0.000 claims 1
- PIBWKRNGBLPSSY-UHFFFAOYSA-L palladium(II) chloride Chemical compound Cl[Pd]Cl PIBWKRNGBLPSSY-UHFFFAOYSA-L 0.000 claims 1
- 229910000027 potassium carbonate Inorganic materials 0.000 claims 1
- 235000015320 potassium carbonate Nutrition 0.000 claims 1
- 229910000160 potassium phosphate Inorganic materials 0.000 claims 1
- 235000011009 potassium phosphates Nutrition 0.000 claims 1
- LPNYRYFBWFDTMA-UHFFFAOYSA-N potassium tert-butoxide Chemical compound [K+].CC(C)(C)[O-] LPNYRYFBWFDTMA-UHFFFAOYSA-N 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229910000029 sodium carbonate Inorganic materials 0.000 claims 1
- 235000017550 sodium carbonate Nutrition 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D401/14—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 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Claims (17)
1. Spoj formule I-A:
[image]
ili njegova farmaceutski prihvatljiva sol, naznačen time, da:
svaki Y1, Y2, Y3, Y4, Y5, Y6, i Y7 je neovisno vodik ili deuterij;
pod uvjetom da barem jedan od Y1, Y2, Y3, Y4, Y5, Y6, i Y7 predstavlja deuterij;
svaki od X1, X2 i X4 je neovisno 12C ili 13C; i
X3 je neovisno -12C(O)- ili -13C(O)-.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da su
a) Y1, Y2, Y3 i Y4 neovisno deuterij ili vodik; i Y5, Y6, i Y7 su deuterij;
b) Y1, Y2 su neovisno deuterij ili vodik; i Y3, Y4, Y5, Y6, i Y7 su deuterij;
c) Y1, Y2, Y5, Y6, i Y7 su neovisno deuterij ili vodik; a Y3 i Y4 su deuterij; ili
d) Y1, Y3 i Y4 su neovisno deuterij ili vodik; a Y2, Y5, Y6, i Y7 su deuterij.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da su
a) Y1, Y2, Y3, Y4, Y5, Y6, i Y7 vodik; i X4 je 13C;
b) Y1, Y2, Y3, Y4, Y5, Y6, i Y7 vodik; i X1 i X4 je 13C;
c) Y1, Y3, Y4, Y5, Y6, i Y7 vodik; Y2 je deuterij; i X4 je 13C;
d) Y1, Y2, Y3 i Y4 vodik; Y5, Y6, i Y7 su deuterij; i X1 je 13C;
e) Y1, Y3, Y4, Y5, Y6, i Y7 vodik; Y2 je deuterij; i X1 je 13C;; ili
f) Y1, Y2, Y3, Y5, Y6 i Y7 su vodik; Y4 je deuterij; i X1 je 13C.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da su
a) Y1, Y2, Y3, Y4, Y5, Y6, i Y7 vodik; i X3 je -13C(O)-; ili
b) Y1 je vodik; Y2, Y3, Y4, Y5, Y6, i Y7 su deuterij; X2 je 13C; i X3 je -13C(O)-.
5. Postupak dobivanja spoja formule I-1:
[image]
naznačen time, da obuhvaća korak reakcije spoja formule 6b:
[image]
sa spojem formule 11:
[image]
pod uvjetima pogodnim za formiranje amidne veze; po želji nadalje obuhvaćajući korak pripreme spoja formule 11:
[image]
reakcijom spoja formule 9:
[image]
pri čemu je X halogen, sa spojem formule 10:
[image]
pod pogodnim metalnim kataliziranim uvjetima umrežavanja, da se dobije adukt koji sadržava zaštićenu amino skupinu;
i
podvrgavanje dobivenog adukta uvjetima pogodnim za uklanjanje zaštite; po želji nadalje obuhvaćajući korak pripreme spoja formule 9:
[image]
reakcijom spoja formule 8:
[image]
pod pogodnim uvjetima halogeniranja; i opcijski nadalje obuhvaća korak pripreme spoja formule 8:
[image]
reakcijom spoja formule 7:
[image]
pod pogodnim uvjetima za stvaranje zaštićene aminske skupine.
6. Čvrsti oblik spoja formule I-1:
[image]
naznačen time, da je oblik Spoja I-1 bezvodna slobodna baza.
7. Čvrsti oblik u skladu s patentnim zahtjevom 6, pri čemu je oblik bezvodna baza kristalnog spoja I-1, naznačen time, da čvrsti oblik karakterizira jedan ili više vrhova izraženih u 2-theta +/- 0,2 u 9,9, 12,8, 15,4, 17,0, 23,1 , 27,8, 29,0 i 30,1 stupnjeva u difrakcijskom dijagramu rendgenskih zraka dobivenom korištenjem K-alfa zračenja Cu.
8. Čvrsti oblik u skladu s patentnim zahtjevom 7, naznačen time, da ima difrakcijski dijagram rendgenskih zraka dobivenom korištenjem K-alfa zračenja Cu, koji sadržava vrhove izražene u 2-theta +/- 0,2 pri
Kut (2-theta +/- 0,2) Intenzitet (%)
8.704 35.67
9.8727 100
12.7565 34.37
15.4224 31.96
16.9295 29.04
17.4518 6.14
18.6901 21.74
20.5734 9.04
21.2755 9.98
21.7139 5.54
23.0565 29.6
24.3907 14.96
25.9089 3.38
27.8453 28.56
28.9558 17.14
30.1162 9.76
31.7775 6.85
32.2508 2.88
33.04 3.17
33.7887 4.71
36.5878 2.64
37.6243 0.33
9. Postupak u skladu s patentnim zahtjevom 5, naznačen time, da se korak reakcije spoja formule 6b sa spojem formule 11 odvija u prisutnosti otapala i organske baze.
10. Postupak u skladu s patentnim zahtjevom 9, naznačen time, da je otapalo odabrano između NMP, DMF ili anizola.
11. Postupak u skladu s patentnim zahtjevom 9, naznačen time, da je organska baza alifatski amin.
12. Postupak u skladu s patentnim zahtjevom 11, naznačen time, da je alifatični amin odabran između trietilamina ili DIPEA.
13. Postupak u skladu s patentnim zahtjevom 5, naznačen time, da prikladni uvjeti unakrsnog spajanja kataliziranog metalom uključuju metalni katalizator, pogodno otapalo i pogodnu bazu.
14. Postupak u skladu s patentnim zahtjevom 13, naznačen time, da je metalni katalizator paladijski katalizator.
15. Postupak u skladu s patentnim zahtjevom 14, naznačen time, da se paladij katalizator bira između PdCl2(PPh3)2, Pd(Ph3)4 i PdCl2(dppf).
16. Postupak u skladu s patentnim zahtjevom 13, naznačen time, da se pogodna baza bira između kalijevog fosfata, K2CO3, tBuOK i Na2CO3.
17. Postupak u skladu s patentnim zahtjevom 13, naznačen time, da je pogodno otapalo odabrano između DME, tetrahidrofurana, toluena i etanola.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462008277P | 2014-06-05 | 2014-06-05 | |
PCT/US2015/032879 WO2015187451A1 (en) | 2014-06-05 | 2015-05-28 | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
EP15745265.7A EP3152212B9 (en) | 2014-06-05 | 2015-05-28 | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20200186T1 true HRP20200186T1 (hr) | 2020-05-29 |
Family
ID=53773488
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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HRP20200186TT HRP20200186T1 (hr) | 2014-06-05 | 2020-02-05 | Radioaktivno obilježeni derivati 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-karboksamid spojeva koji se koriste kao inhibitori atr kinaze, priprava navedenih spojeva i njihovi različiti čvrsti oblici |
Country Status (22)
Country | Link |
---|---|
US (3) | US9670215B2 (hr) |
EP (1) | EP3152212B9 (hr) |
JP (2) | JP6568111B2 (hr) |
KR (1) | KR102575125B1 (hr) |
CN (2) | CN110590787A (hr) |
AU (2) | AU2015271030B2 (hr) |
BR (1) | BR112016028273B1 (hr) |
CA (1) | CA2950587C (hr) |
DK (1) | DK3152212T3 (hr) |
ES (1) | ES2777608T3 (hr) |
HR (1) | HRP20200186T1 (hr) |
IL (1) | IL249361B (hr) |
LT (1) | LT3152212T (hr) |
MX (2) | MX2016015874A (hr) |
PL (1) | PL3152212T3 (hr) |
PT (1) | PT3152212T (hr) |
RS (1) | RS60013B1 (hr) |
RU (2) | RU2020110358A (hr) |
SG (2) | SG11201610197XA (hr) |
SI (1) | SI3152212T1 (hr) |
WO (1) | WO2015187451A1 (hr) |
ZA (1) | ZA201700035B (hr) |
Families Citing this family (25)
Publication number | Priority date | Publication date | Assignee | Title |
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CA3013000C (en) | 2008-12-19 | 2022-12-13 | Vertex Pharmaceuticals Incorporated | Pyrazine derivatives useful as inhibitors of atr kinase |
WO2013049726A2 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Processes for making compounds useful as inhibitors of atr kinase |
CA2850491C (en) | 2011-09-30 | 2020-10-27 | Vertex Pharmaceuticals Incorporated | Treating pancreatic cancer and non-small cell lung cancer with atr inhibiors |
MX358818B (es) | 2012-04-05 | 2018-09-05 | Vertex Pharma | Compuestos utiles como inhibidores de cinasa ataxia telangiectasia mutada y rad3 relacionados (atr) y terapias de combinacion de estos. |
ES2946360T3 (es) | 2012-12-07 | 2023-07-17 | Vertex Pharma | Pirazolo[1,5-a]pirimidinas útiles como inhibidores de ATR quinasa para el tratamiento de enfermedades de cáncer |
WO2014143240A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
RU2687276C2 (ru) * | 2013-12-06 | 2019-05-13 | Вертекс Фармасьютикалз Инкорпорейтед | Соединения, пригодные для использования в качестве ингибиторов atr киназы |
LT3152212T (lt) | 2014-06-05 | 2020-05-11 | Vertex Pharmaceuticals Inc. | Radioaktyviai žymėti 2-amino-6-fluor-n-[5-fluor-piridin-il]- pirazolo[1,5-a]pirimidin-3-karboksamido junginio dariniai, naudingi kaip atr kinazės inhibitoriai, minėto junginio gamybos būdas ir jo skirtingos kietos formos |
SG11201610500WA (en) | 2014-06-17 | 2017-01-27 | Vertex Pharma | Method for treating cancer using a combination of chk1 and atr inhibitors |
CA3000684A1 (en) | 2015-09-30 | 2017-04-06 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of dna damaging agents and atr inhibitors |
EP3399983A1 (en) * | 2016-01-08 | 2018-11-14 | The Institute of Cancer Research: Royal Cancer Hospital | Inhibitors of ataxia-telangiectasia mutated and rad3-related protein kinase (atr) for use in methods of treating cancer |
JOP20190197A1 (ar) | 2017-02-24 | 2019-08-22 | Bayer Pharma AG | مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر |
WO2018153969A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with radium-223 salt |
WO2018153972A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and antiandrogens |
WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
EP3630116B1 (en) | 2017-05-26 | 2024-05-01 | The Board Of Regents Of The University Of Texas System | Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase |
LT3651768T (lt) | 2017-07-13 | 2024-04-25 | Board Of Regents, The University Of Texas System | Heterocikliniai atr kinazės inhibitoriai |
CA3071760A1 (en) | 2017-08-04 | 2019-02-07 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and pd-1/pd-l1 inhibitors |
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