HRP20191396T1 - Imidazolonilkinolini i njihova uporaba kao inhibotora atm kinaze - Google Patents
Imidazolonilkinolini i njihova uporaba kao inhibotora atm kinaze Download PDFInfo
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- HRP20191396T1 HRP20191396T1 HRP20191396T HRP20191396T1 HR P20191396 T1 HRP20191396 T1 HR P20191396T1 HR P20191396 T HRP20191396 T HR P20191396T HR P20191396 T1 HRP20191396 T1 HR P20191396T1
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- pyrazol
- tautomer
- stereoisomer
- solvate
- salt
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- VFEDRRNHLBGPNN-UHFFFAOYSA-N nimustine Chemical compound CC1=NC=C(CNC(=O)N(CCCl)N=O)C(N)=N1 VFEDRRNHLBGPNN-UHFFFAOYSA-N 0.000 claims 2
- PCHKPVIQAHNQLW-CQSZACIVSA-N niraparib Chemical compound N1=C2C(C(=O)N)=CC=CC2=CN1C(C=C1)=CC=C1[C@@H]1CCCNC1 PCHKPVIQAHNQLW-CQSZACIVSA-N 0.000 claims 2
- FAQDUNYVKQKNLD-UHFFFAOYSA-N olaparib Chemical compound FC1=CC=C(CC2=C3[CH]C=CC=C3C(=O)N=N2)C=C1C(=O)N(CC1)CCN1C(=O)C1CC1 FAQDUNYVKQKNLD-UHFFFAOYSA-N 0.000 claims 2
- 229960000572 olaparib Drugs 0.000 claims 2
- 229960001756 oxaliplatin Drugs 0.000 claims 2
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims 2
- 229950000755 palifosfamide Drugs 0.000 claims 2
- 229950003180 peplomycin Drugs 0.000 claims 2
- QIMGFXOHTOXMQP-GFAGFCTOSA-N peplomycin Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCCN[C@@H](C)C=1C=CC=CC=1)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1NC=NC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C QIMGFXOHTOXMQP-GFAGFCTOSA-N 0.000 claims 2
- 229950005566 picoplatin Drugs 0.000 claims 2
- IIMIOEBMYPRQGU-UHFFFAOYSA-L picoplatin Chemical compound N.[Cl-].[Cl-].[Pt+2].CC1=CC=CC=N1 IIMIOEBMYPRQGU-UHFFFAOYSA-L 0.000 claims 2
- NJBFOOCLYDNZJN-UHFFFAOYSA-N pipobroman Chemical compound BrCCC(=O)N1CCN(C(=O)CCBr)CC1 NJBFOOCLYDNZJN-UHFFFAOYSA-N 0.000 claims 2
- 229960000952 pipobroman Drugs 0.000 claims 2
- 229960001221 pirarubicin Drugs 0.000 claims 2
- 229960004403 pixantrone Drugs 0.000 claims 2
- PEZPMAYDXJQYRV-UHFFFAOYSA-N pixantrone Chemical compound O=C1C2=CN=CC=C2C(=O)C2=C1C(NCCN)=CC=C2NCCN PEZPMAYDXJQYRV-UHFFFAOYSA-N 0.000 claims 2
- 150000003058 platinum compounds Chemical class 0.000 claims 2
- 229960003171 plicamycin Drugs 0.000 claims 2
- CPTBDICYNRMXFX-UHFFFAOYSA-N procarbazine Chemical compound CNNCC1=CC=C(C(=O)NC(C)C)C=C1 CPTBDICYNRMXFX-UHFFFAOYSA-N 0.000 claims 2
- 229960000624 procarbazine Drugs 0.000 claims 2
- 229960002185 ranimustine Drugs 0.000 claims 2
- BMKDZUISNHGIBY-UHFFFAOYSA-N razoxane Chemical compound C1C(=O)NC(=O)CN1C(C)CN1CC(=O)NC(=O)C1 BMKDZUISNHGIBY-UHFFFAOYSA-N 0.000 claims 2
- 229960000460 razoxane Drugs 0.000 claims 2
- 229960003452 romidepsin Drugs 0.000 claims 2
- OHRURASPPZQGQM-GCCNXGTGSA-N romidepsin Chemical compound O1C(=O)[C@H](C(C)C)NC(=O)C(=C/C)/NC(=O)[C@H]2CSSCC\C=C\[C@@H]1CC(=O)N[C@H](C(C)C)C(=O)N2 OHRURASPPZQGQM-GCCNXGTGSA-N 0.000 claims 2
- OHRURASPPZQGQM-UHFFFAOYSA-N romidepsin Natural products O1C(=O)C(C(C)C)NC(=O)C(=CC)NC(=O)C2CSSCCC=CC1CC(=O)NC(C(C)C)C(=O)N2 OHRURASPPZQGQM-UHFFFAOYSA-N 0.000 claims 2
- 108010091666 romidepsin Proteins 0.000 claims 2
- HMABYWSNWIZPAG-UHFFFAOYSA-N rucaparib Chemical compound C1=CC(CNC)=CC=C1C(N1)=C2CCNC(=O)C3=C2C1=CC(F)=C3 HMABYWSNWIZPAG-UHFFFAOYSA-N 0.000 claims 2
- 229950004707 rucaparib Drugs 0.000 claims 2
- 229960005399 satraplatin Drugs 0.000 claims 2
- 190014017285 satraplatin Chemical compound 0.000 claims 2
- 229960001052 streptozocin Drugs 0.000 claims 2
- ZSJLQEPLLKMAKR-GKHCUFPYSA-N streptozocin Chemical compound O=NN(C)C(=O)N[C@H]1[C@@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O ZSJLQEPLLKMAKR-GKHCUFPYSA-N 0.000 claims 2
- 229950004550 talazoparib Drugs 0.000 claims 2
- 229960004964 temozolomide Drugs 0.000 claims 2
- 229960001196 thiotepa Drugs 0.000 claims 2
- 229940044693 topoisomerase inhibitor Drugs 0.000 claims 2
- 229960000303 topotecan Drugs 0.000 claims 2
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims 2
- PKVRCIRHQMSYJX-AIFWHQITSA-N trabectedin Chemical compound C([C@@]1(C(OC2)=O)NCCC3=C1C=C(C(=C3)O)OC)S[C@@H]1C3=C(OC(C)=O)C(C)=C4OCOC4=C3[C@H]2N2[C@@H](O)[C@H](CC=3C4=C(O)C(OC)=C(C)C=3)N(C)[C@H]4[C@@H]21 PKVRCIRHQMSYJX-AIFWHQITSA-N 0.000 claims 2
- 229960000977 trabectedin Drugs 0.000 claims 2
- 229960003181 treosulfan Drugs 0.000 claims 2
- 229960000875 trofosfamide Drugs 0.000 claims 2
- UMKFEPPTGMDVMI-UHFFFAOYSA-N trofosfamide Chemical compound ClCCN(CCCl)P1(=O)OCCCN1CCCl UMKFEPPTGMDVMI-UHFFFAOYSA-N 0.000 claims 2
- 229960001055 uracil mustard Drugs 0.000 claims 2
- 229960000653 valrubicin Drugs 0.000 claims 2
- ZOCKGBMQLCSHFP-KQRAQHLDSA-N valrubicin Chemical compound O([C@H]1C[C@](CC2=C(O)C=3C(=O)C4=CC=CC(OC)=C4C(=O)C=3C(O)=C21)(O)C(=O)COC(=O)CCCC)[C@H]1C[C@H](NC(=O)C(F)(F)F)[C@H](O)[C@H](C)O1 ZOCKGBMQLCSHFP-KQRAQHLDSA-N 0.000 claims 2
- 229950011257 veliparib Drugs 0.000 claims 2
- JNAHVYVRKWKWKQ-CYBMUJFWSA-N veliparib Chemical compound N=1C2=CC=CC(C(N)=O)=C2NC=1[C@@]1(C)CCCN1 JNAHVYVRKWKWKQ-CYBMUJFWSA-N 0.000 claims 2
- 229950009268 zinostatin Drugs 0.000 claims 2
- 229960000641 zorubicin Drugs 0.000 claims 2
- FBTUMDXHSRTGRV-ALTNURHMSA-N zorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(\C)=N\NC(=O)C=1C=CC=CC=1)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 FBTUMDXHSRTGRV-ALTNURHMSA-N 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 201000003741 Gastrointestinal carcinoma Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 206010024305 Leukaemia monocytic Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 210000000981 epithelium Anatomy 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 208000035474 group of disease Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 210000000987 immune system Anatomy 0.000 claims 1
- 201000002313 intestinal cancer Diseases 0.000 claims 1
- 210000000936 intestine Anatomy 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000000867 larynx Anatomy 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 201000005249 lung adenocarcinoma Diseases 0.000 claims 1
- 210000004324 lymphatic system Anatomy 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000006894 monocytic leukemia Diseases 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 210000003932 urinary bladder Anatomy 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
- A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
-
- 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
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (15)
1. Spoj s formulom (IV)
gdje
Het1 je pirazolil, koji može biti nesupstituiran ili mono-, di- ili trisupstituiran, neovisno jedan od drugoga sa Hal ili A,
A u svakom slučaju neovisno označava nerazgranati ili razgranati alkil koji ima 1, 2, 3, 4, 5 ili 6 C atoma, gdje, međusobno neovisno, 1, 2, 3, 4, ili 5 H atoma mogu biti zamijenjeni s Hal,
Hal predstavlja F, Cl, Br ili I,
HET je odabran od: 3-difluorometoksi-5-fluoropiridin-4-il, 3-fluoro-5-metoksipiridin-4-il, 3-fluoro-5-fluorometoksipiridin-4-il, 3-fluoro-5-(trideuteriometoksi)piridin-4-il,
i/ili njihovog farmaceutski upotrebljivog derivata, soli, solvata, tautomera, stereoizomera.
2. Spoj s formulom (IV) prema zahtjevu 1, naznačen time što je Het1 odabran iz niza koji sadrži: 1H-pirazol-4-il, 2H-pirazol-3-il, 1H-pirazol-3-il, 1-metil-1H-pirazol-4-il, 3-metil-1H-pirazol-4-il, 5-metil-1H-pirazol-3-il, 4-metil-1H-pirazol-3-il, 1-fluorometil-1H-pirazol-4-il, 1-difluorometil-1H-pirazol-4-il, 1,3-dimetil-1H-pirazol-4-il, 1-etil-1H-pirazol-4-il, 1-etil-3-metil-1H-pirazolil, 3-fluoro-1-metil-1H-pirazol-4-il,
i/ili njihov farmaceutski upotrebljiv derivat, sol, solvat, tautomer, stereoizomer.
3. Spoj prema zahtjevu 1, naznačen time što je odabran od
i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer, stereoizomer.
4. Spoj prema jednom od zahtjeva 1 do 3 i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer ili stereoizomer, naznačen time što je za uporabu kao lijek.
5. Spoj prema jednom od zahtjeva 1 do 3 i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer ili stereoizomer, naznačen time što je za uporabu u liječenju raka, tumora i/ili metastaza.
6. Spoj prema jednom od zahtjeva 1 do 3 i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer, stereoizomer, naznačen time što je za uporabu u liječenju raka, tumora i/ili metastaza u kombinaciji s radioterapijom.
7. Spoj prema jednom od zahtjeva 1 do 3 i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer, stereoizomer naznačen time što je za uporabu u liječenju raka, tumora i/ili metastaza u kombinaciji s najmanje jednim antikancerogenim sredstvom.
8. Spoj i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer, stereoizomer za uporabu prema jednom od patentnih zahtjeva 5 do 7 naznačen time što je tumor odabran iz skupine bolesti skvamoznog epitela, mjehura, želuca, bubrega, glave, vrata, jednjaka, grlića maternice, štitnjače, crijeva, kosti, jetre, mozga, prostate, urogenitalnog trakta, limfnog sustava, grkljana, pluća, kože, krvi i imunološkog sustava, i/ili rak je odabran iz skupine koju čine monocitna leukemija, adenokarcinom pluća, karcinom pluća malih stanica, rak gušterače, glioblastom, karcinom crijeva, karcinom dojke, akutna mijeloična leukemija, kronična mijeloična leukemija, akutna limfatična leukemija, kronična limfatična leukemija, Hodgkinov limfom i ne-Hodgkinov limfom.
9. Farmaceutski pripravak naznačen time što sadrži učinkovitu količinu najmanje jednog spoja prema jednom od zahtjeva 1 do 3 i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer ili stereoizomer, po izboru zajedno s najmanje jednom farmaceutski podnošljivom pomoćnom tvari.
10. Farmaceutski pripravak prema zahtjevu 9, naznačen time što nadalje sadrži najmanje jedno antikancerogeno sredstvo.
11. Komplet naznačen time što sadrži zasebna pakiranja
(a) učinkovite količine spoja prema jednom od zahtjeva 1 do 3 i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer ili stereoizomer, i
(b) učinkovite količine daljnjeg antikancernog sredstva.
12. Farmaceutski pripravak prema zahtjevu 10, naznačen time što je najmanje jedno antikancerogeno sredstvo odabrano od sredstava za alkiliranje, spojeva platine, inhibitora topoizomeraze, inhibitora poli-(ADP-riboza)-polimeraze (PARP), inhibitora ATR (ataksija telangiektazija i Rad3 povezanih), antikancerogenih antibiotika i alfa emitera.
13. Farmaceutski pripravak prema zahtjevu 10, naznačen time što je najmanje jedno antikancerogeno sredstvo odabrano iz skupa koji sadrži altretamin, bendamustin, busulfan, karmustin, klorambucil, klormetin, ciklofosfamid, dakarbazin, ifosfamid, improsulfan tozilat, lomustin, melfalan, mitobronitol, mitolaktol, nimustin, ranimustin, temozolomid, tiotepa, treosulfan, mekloretamin, karbokvon, apazikuon, fotemustin, glufosfamid, palifosfamid, pipobroman, trofosfamid, uramustin; karboplatin, cisplatin, eptaplatin, miriplatin hidrat, oksaliplatin, lobaplatin, nedaplatin, pikoplatin, satraplatin; etopozid, irinotekan, razoksan, sobuzoksan, topotekan, kamptotecin, doksorubicin, amsakrin; talazoparib, olaparib, veliparib, rukaparib, CEP 9722, MK4827, BGB-290; VE-822, AZ20, AZD6738; amrubicin, bisantren, decitabin, mitoksantron, prokarbazin, trabektedin, klofarabin, amsakrin, brostalicin, piksantron, laromustin; bleomicin, daktinomicin, doksorubicin, epirubicin, idarubicin, levamizol, miltefozin, mitomicin C, romidepsin, streptozocin, valrubicin, zinostatin, zorubicin, daunurobicin, plikamicin, aklarubicin, peplomicin, pirarubicin.
14. Komplet prema zahtjevu 11, naznačen time što je daljnje antikancerogeno sredstvo odabrano od sredstava za alkiliranje, spojeva platine, inhibitora topoizomeraze, inhibitora poli-(ADP-riboza)-polimeraze (PARP), inhibitora ATR (ataksija telangiektazija i Rad3 povezanih), antikancerogenih antibiotika i alfa emitera.
15. Komplet prema zahtjevu 11, naznačen time što je najmanje jedno antikancerogeno sredstvo odabrano iz skupa koji sadrži altretamin, bendamustin, busulfan, karmustin, klorambucil, klormetin, ciklofosfamid, dakarbazin, ifosfamid, improsulfan tozilat, lomustin, melfalan, mitobronitol, mitolaktol, nimustin, ranimustin, temozolomid, tiotepa, treosulfan, mekloretamin, karbokvon, apazikuon, fotemustin, glufosfamid, palifosfamid, pipobroman, trofosfamid, uramustin; karboplatin, cisplatin, eptaplatin, miriplatin hidrat, oksaliplatin, lobaplatin, nedaplatin, pikoplatin, satraplatin; etopozid, irinotekan, razoksan, sobuzoksan, topotekan, kamptotecin, doksorubicin, amsakrin; talazoparib, olaparib, veliparib, rukaparib, CEP 9722, MK4827, BGB-290; VE-822, AZ20, AZD6738; amrubicin, bisantren, decitabin, mitoksantron, prokarbazin, trabektedin, klofarabin, amsakrin, brostalicin, piksantron, laromustin; bleomicin, daktinomicin, doksorubicin, epirubicin, idarubicin, levamizol, miltefozin, mitomicin C, romidepsin, streptozocin, valrubicin, zinostatin, zorubicin, daunurobicin, plikamicin, aklarubicin, peplomicin, pirarubicin.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15000968 | 2015-04-02 | ||
| EP16717560.3A EP3277681B1 (de) | 2015-04-02 | 2016-03-31 | Imidazolonylchinoline und deren verwendung als atm kinase inhibitoren |
| PCT/EP2016/000542 WO2016155884A1 (de) | 2015-04-02 | 2016-03-31 | Imidazolonylchinoline und deren verwendung als atm kinase inhibitoren |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20191396T1 true HRP20191396T1 (hr) | 2019-11-01 |
Family
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| Application Number | Title | Priority Date | Filing Date |
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| CN110312717B (zh) * | 2017-02-27 | 2022-04-12 | 上海瑛派药业有限公司 | 取代的稠合杂芳三环化合物作为激酶抑制剂及其应用 |
| JOP20190209A1 (ar) * | 2017-03-16 | 2019-09-12 | Astrazeneca Ab | مركبات إيميدازو [ 4، 5-c ] كينولين-2-أون ديوترومية واستخدامها في علاج السرطان |
| AU2019208024A1 (en) | 2018-01-12 | 2020-08-13 | Prolynx Llc | Protocol for minimizing toxicity of combination dosages and imaging agent for verification |
| CA3093499A1 (en) * | 2018-03-14 | 2019-09-19 | Merck Patent Gmbh | Compounds and uses thereof to treat tumors in a subject |
| KR20200143367A (ko) | 2018-04-12 | 2020-12-23 | 바이엘 악티엔게젤샤프트 | 살충제로서의 ｎ-（시클로프로필메틸）-５-（메틸술포닐）-ｎ-｛１-［１-（피리미딘-２-일）-１ｈ-１,２,４-트리아졸-５-일］에틸｝벤즈아미드 유도체 및 상응하는 피리딘-카르복스아미드 유도체 |
| WO2019201283A1 (en) * | 2018-04-20 | 2019-10-24 | Xrad Therapeutics, Inc. | Dual atm and dna-pk inhibitors for use in anti-tumor therapy |
| CN110386932A (zh) * | 2018-04-20 | 2019-10-29 | 艾科思莱德制药公司 | 用于抗肿瘤疗法中的双重atm和dna-pk抑制剂 |
| GB201814487D0 (en) * | 2018-09-06 | 2018-10-24 | Cycle Pharmaceuticals Ltd | Cancer |
| CN109045042A (zh) * | 2018-09-21 | 2018-12-21 | 上海交通大学医学院附属上海儿童医学中心 | Atm抑制剂在制备抑制急性淋巴细胞性白血病复发的药物中的应用 |
| CN112771045B (zh) * | 2018-09-30 | 2022-04-19 | 南京明德新药研发有限公司 | 喹啉并吡咯烷-2-酮类衍生物及其应用 |
| AU2020247451A1 (en) | 2019-03-27 | 2021-11-18 | Merck Patent Gmbh | Imidazolonylquinoline compounds and therapeutic uses thereof |
| BR112022001067A2 (pt) * | 2019-07-30 | 2022-05-24 | Xrad Therapeutics Inc | Inibidores duplos de atm e dna-pk para uso em terapia antitumoral |
| WO2021084124A1 (en) | 2019-11-01 | 2021-05-06 | Ares Trading S.A. | COMBINED INHIBITION OF PD-1, TGFβ AND ATM TOGETHER WITH RADIOTHERAPY FOR THE TREATMENT OF CANCER |
| EP4069366A1 (en) * | 2019-12-04 | 2022-10-12 | CHDI Foundation, Inc. | Atm kinase inhibitors and compositions and methods of use thereof |
| CN115003672A (zh) * | 2020-01-09 | 2022-09-02 | 南京明德新药研发有限公司 | 喹啉并咪唑类化合物及其应用 |
| WO2021197339A1 (zh) * | 2020-03-30 | 2021-10-07 | 南京明德新药研发有限公司 | 作为atm抑制剂的喹啉并吡咯烷-2-酮类化合物的晶型及其应用 |
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