ME02855B - KONDENZOVANI TETRA ILl PENTA-CIKLIČNI DIHIDRODIAZEPINOKARBAZOLONI KAO PARP INHIBITORI - Google Patents
KONDENZOVANI TETRA ILl PENTA-CIKLIČNI DIHIDRODIAZEPINOKARBAZOLONI KAO PARP INHIBITORIInfo
- Publication number
- ME02855B ME02855B MEP-2017-278A MEP28617A ME02855B ME 02855 B ME02855 B ME 02855B ME P28617 A MEP28617 A ME P28617A ME 02855 B ME02855 B ME 02855B
- Authority
- ME
- Montenegro
- Prior art keywords
- alkyl
- heterocyclyl
- heteroaryl
- cycloalkyl
- aryl
- Prior art date
Links
- 239000012661 PARP inhibitor Substances 0.000 title 1
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims 40
- 125000003118 aryl group Chemical group 0.000 claims 39
- 125000000753 cycloalkyl group Chemical group 0.000 claims 39
- 125000001072 heteroaryl group Chemical group 0.000 claims 39
- 125000000623 heterocyclic group Chemical group 0.000 claims 39
- 125000003342 alkenyl group Chemical group 0.000 claims 36
- 125000000304 alkynyl group Chemical group 0.000 claims 36
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 16
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 8
- 125000004429 atom Chemical group 0.000 claims 7
- 229920006395 saturated elastomer Polymers 0.000 claims 7
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 102000012338 Poly(ADP-ribose) Polymerases Human genes 0.000 claims 2
- 108010061844 Poly(ADP-ribose) Polymerases Proteins 0.000 claims 2
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
Classifications
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- 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
- C07D487/06—Peri-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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/16—Peri-condensed systems
-
- 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
- C07D471/22—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 systems contains four or more hetero rings
-
- 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
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Claims (12)
1. Jedinjenje odabrano od jedinjenja Formule (I): ili njegovog stereoizomera, ili njegove farmaceutski prihvatljive soli, pri čemu: RN se bira od vodonika, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12; X se bira iz grupe koja obuhvata C, N, O, i S; m i n, koji mogu da budu isti ili različiti, nezavisno broj 0, 1, 2, ili 3; t je je broj od 0, 1, 2, ili 3; R1, u svakom slučaju, je nezavisno odabran od halogena, CN, NO2, OR9, NR9R10, NR9COR10, NR9SO2R10, CONR9R10, COOR9, SO2R9, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12; R2 se bira od vodonika, COR9, CONR9R10, CO2R9, SO2R9, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12; R3, R4, R5, R6, R7 i R8, koji mogu da budu isti ili različiti, su svaki nezavisno odabrani od vodonika, halogena, -NR9R10, -OR9, okso, -COR9, -CO2R9, -CONR9R10,-NR9CONR10R11, -NR9CO2R10, -NR9SO2R10, -SO2R9, alkil, alkenil, cikloalkil, aril, heterociklil, alkinil, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, aril, heterociklil, i heteroaril je nezavisno pociono supstituisan sa najmanje jednim supstituentom R12, ili (R3 i R4), i/ili (R4 i R5), i/ili (R5 i R6), i/ili (R6 i R7), i/ili (R7 i R8), zajedno sa atom(ima) za koje su vezani, obrazuju 3-do 8-člane zasićene, delimično ili u potpunosti nezasićen prsten koji ima 0, 1 ili 2 heteroatoma koji su nezavisno odabrani od -NR13-, -O-, -S-, -SO-ili -SO2-, i pomenuti prsten je opciono supstituisan sa najmanje jednim supstituentom R12, pod uslovom da kada X je O, R5 i R6 su odsutni, kada X je N, R6 je odsutan, kada X je S, R5 i R6 su odsutni, ili najmanje R5 i R6 je okso, kada jedan od R3 i R4 je okso, drugi je odsutan, kada jedan od R7 i R8 je okso, drugi je odsutan, kada X je C i kada jedna od R5 i R6 je okso, drugi je odsutan; R9, R10, i R11, koji mogu da budu isti ili različiti, pri čemu se svaki bira od vodonika, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12; R12 se bira od CN, halogena, haloalkil, NO2, -NR’R", -OR’, oxo, -COR’, -CO2R’,-CONR’R", -NR’CONR"R"’, -NR’CO2R", -NR’SO2R", -SO2R’, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu R’, R", i R’’’ se nezavisno biraju od vodonika, haloalkila, alkil, arilalkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, ili (R’ i R"), i/ili (R" i R’’’) zajedno sa atom(ima) za koje su vezani, obrazuju 3-do 8 člani zasićeni, delimično ili potpuno nezasićeni prsten koji ima od 0, 1 ili 2 dodatna heteroatoma koji su nezavisno odabrani od -NR13-, -O-, -S-, -SO-i SO2-. R13 je odabran od vodonika, alkil, cikloalkil, aril, heteroaril, i heterociklila.
2. Jedinjenje prema Zahtevu 1, koje je odabrano od jedinjenja Formule (II): ili njegovog stereoizomera, ili njegove farmaceutski prihvatljive soli, pri čemu: RN je odabran od vodonika, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12; m i n, koji mogu da budu isti ili različiti, nezavisno broj 0, 1, 2, ili 3; t je broj od 0, 1, 2, ili 3; R1, u svakom slučaju, je nezavisno odabran od halogena, CN, NO2, OR9, NR9R10, NR9COR10, NR9SO2R10, CONR9R10, COOR9, SO2R9, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12; R2 se bira od vodonika, COR9, CONR9R10, CO2R9, SO2R9, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12; R3, R4, R5, R6, R7 i R8, koji mogu da budu isti ili različiti, pri čemu se svaki nezavisno bira od vodonika, halogena, -NR9R10, -OR9, okso, -COR9, -CO2R9, -CONR9R10,-NR9CONR10R11, -NR9CO2R10, -NR9SO2R10, -SO2R9, alkil, alkenil, cikloalkil, aril, heterociklil, alkinil, i heteroarila, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, aril, heterociklil, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12, ili (R3 i R4), i/ili (R4 i R5), i/ili (R5 i R6), i/ili (R6 i R7), i/ili (R7 i R8), zajedno sa atom(ima) to za koje su vezani, obrazuju 3-do 8-člani zasićeni, delimično ili u potpunosti nezasićeni prsten koji ima 0, 1 ili 2 heteroatoma koji su nezavisno odabrani od -NR13-, -O-, -S-, -SO-i -SO2-, i pomenuti prsten je opciono supstituisan sa najmanje jednim supstituentom R12, pod uslovom da kada jedan od R3 i R4 je okso, drugi je odsutan, kada jedan od R7 i R8 je okso, drugi je odsutan, i kada jedna od R5 i R6 je okso, drugi je odsutan; R9, R10, i R11, koji mogu da budu isti ili različiti, su svaki odabrani od vodonika, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12; R12 je odabran od CN, halogena, haloalkil, NO2, -NR’R", -OR’, okso, -COR’, -CO2R’,-CONR’R", -NR’CONR"R"’, -NR’CO2R", -NR’SO2R", -SO2R’, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu R’, R", i R’’’ su nezavisno odabrani od hidrogen, haloalkil, alkil, arilalkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, ili (R’ i R"), i/ili (R" i R’’’) zajedno sa atom(ima) za koje su vezani, obrazuju 3-do 8-člani zasićen, delimično il u potpunosti nezasićen prsten koji ima 0, 1 ili 2 dodatna heteroatoma koji su nezavisno odabrani od -NR13-, -O-, -S-, -SO-ili -SO2-. R13 se bira od vodonika, alkil, cikloalkil, aril, heteroaril, i heterociklil.
3. Jedinjenje prema Zahtevu 1, koje je odabrano od jedinjenja frmule (III): ili njegovog stereoizomera, ili njegove farmaceutski prihvatljive soli, pri čemu: RN se bira od vodonika, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12; m i n, koji mogu da budu isti ili različiti, nezavisno broj 0, 1, 2, ili 3; t je broj od 0, 1, 2, ili 3; R1, u svakom slučaju, je nezavisno odabran od halogena, CN, NO2, OR9, NR9R10, NR9COR10, NR9SO2R10, CONR9R10, COOR9, SO2R9, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12; R2 se bira od vodonika, COR9, CONR9R10, CO2R9, SO2R9, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12; R3, R4, R5, R7 i R8, koji mogu da budu isti ili različiti, su svaki nezavisno odabrani vodonika, halogena, -NR9R10, -OR9, okso, -COR9, -CO2R9, -CONR9R10, -NR9CONR10R11,-NR9CO2R10, -NR9SO2R10, -SO2R9, alkil, alkenil, cikloalkil, aril, heterociklil, alkinil, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, aril, heterociklil, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12, ili (R3 i R4), i/ili (R4 i R5), i/ili (R5 i R7), i/ili (R7 i R8), zajedno sa atom(ima) za koje su vezani, obrazuju 3-do 8-člani zasićeni, delimično ili u potpunosti nezasićeni prsten koji ima 0, 1 ili 2 heteroatoma koji su nezavisno odabrani od -NR13-, -O-, -S-, -SO-, i -SO2-, i pomenuti prsten je opciono supstituisan sa najmanje jednim supstituentom R12, pod uslovom da kada jedan od R3 i R4 je okso, drugi je odsutan, i kada jedna od R7 i R8 je okso, drugi je odsutan; R9, R10, i R11, koji mogu da budu isti ili različiti, se svaki biraju od vodonika, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu svaki od alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril je nezavisno opciono supstituisan sa najmanje jednim supstituentom R12; R12 se bira od CN, halogena, haloalkil, NO2, -NR’R", -OR’, okso, -COR’, -CO2R’,-CONR’R", -NR’CONR"R"’, -NR’CO2R", -NR’SO2R", -SO2R’, alkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, pri čemu R’, R", i R’’’ su nezavisno odabrani od, haloalkil, alkil, arilalkil, alkenil, alkinil, cikloalkil, heterociklil, aril, i heteroaril, ili (R’ i R"), i/ili (R" i R’’’) zajedno sa atom(ima) za koje su vezani, obrazuju 3-do 8-člani zasićeni, delimični ili u potpunosti nezasićeni prsten kojiima 0, 1 ili 2 dodatna heteroatoma koji su nezavisno odabrani od -NR13-, -O-, -S-, -SO-ili -SO2-; i R13 se bira od vodonika, alkil, cikloalkil, aril, heteroaril, i heterociklil.
4. Jedinjenje prema Zahtevu 3, pri čemu m i n su zajedno broj 1.
5. Jedinjenje prema Zahtevu 3, pri čemu t je 1, i R1 je halogen ili alkil.
6. Jedinjenje prema Zahtevu 3, pri je čemu R2 vodonik.
7. Jedinjenje prema Zahtevu 3, pri čemu R4 i R5, zajedno sa atomom(ima) za koji(e) su vezani, obrazuju 5-člani zasićeni prsten koji ima jedan heteroatom azota.
8. Jedinjenje prema bilo kom od prethodnih zahteva koje se bira od sledećih jedinjenja: ili njihovih stereoizomera, ili njihove farmaceutski prihvatljive soli.
9. Jedinjenje prema bilo kom prethodnom zahtevu koje je ili njegov stereoizomer, ili njegova farmaceutski prihvatljiva so.
10. Farmaceutska kompozicija koja sadrži najmanje jedan farmaceutski prihvatljivi nosač i kao aktivni sastojak terapeutski efikasnu količinu jedinjenja prema bilo kom od zahteva 1-9 ili njegov stereoizomer, ili njegovu farmaceutski prihvatljivu so.
11. Jedinjenje prema bilo kom od zahteva 1-9 ili njegov stereoizomer, ili njegova farmaceutski prihvatljiva so za upotebu u lečenju kancera koji reaguje na inhibiciju Poli(ADP-riboza) polimeraze.
12. Jedinjenje prema bilo kom od zahteva 1-9 ili njegov stereoizomer, ili njegova farmaceutski prihvatljiva so za upotebu u lečenju najmanje jedne bolesti koja reaguje na inhibiciju Poli(ADP-riboza) polimeraze.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2011/085148 WO2013097225A1 (en) | 2011-12-31 | 2011-12-31 | Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors |
| EP11878508.8A EP2797921B1 (en) | 2011-12-31 | 2011-12-31 | Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02855B true ME02855B (me) | 2018-04-20 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2017-278A ME02855B (me) | 2011-12-31 | 2011-12-31 | KONDENZOVANI TETRA ILl PENTA-CIKLIČNI DIHIDRODIAZEPINOKARBAZOLONI KAO PARP INHIBITORI |
Country Status (29)
| Country | Link |
|---|---|
| US (4) | US9260440B2 (me) |
| EP (2) | EP2797921B1 (me) |
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| EP2822656B1 (en) | 2012-03-07 | 2016-10-19 | Institute of Cancer Research: Royal Cancer Hospital (The) | 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use |
| US9611223B2 (en) | 2013-09-11 | 2017-04-04 | Institute Of Cancer Research: Royal Cancer Hospital (The) | 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use |
| CN107922425B (zh) * | 2015-08-25 | 2021-06-01 | 百济神州有限公司 | 制备parp抑制剂、结晶形式的方法及其用途 |
| CA3017388C (en) * | 2016-04-01 | 2024-03-12 | Zeno Royalties & Milestones, LLC | Estrogen receptor modulators |
| US11202782B2 (en) | 2016-09-27 | 2021-12-21 | Beigene, Ltd. | Treatment cancers using a combination comprising PARP inhibitors |
| US10899763B2 (en) | 2017-02-28 | 2021-01-26 | Beigene, Ltd. | Crystalline forms of salts of fused penta-cyclic dihydrodiazepinocarbazolones, and uses thereof |
| CN106883232B (zh) * | 2017-03-31 | 2019-01-22 | 苏州康润医药有限公司 | 一种氮杂非那烯-3-酮的衍生物及其制备方法与应用 |
| WO2019015561A1 (en) * | 2017-07-17 | 2019-01-24 | Beigene, Ltd. | TREATMENT OF CANCERS USING A COMBINATION COMPRISING INHIBITORS OF PARP, TEMOZOLOMIDE AND / OR RADIOTHERAPY |
| AU2019275722A1 (en) * | 2018-06-01 | 2020-11-12 | Beigene, Ltd. | Maintenance therapy of a PARP inhibitor in treating gastric cancer |
| CN111171031B (zh) * | 2019-05-10 | 2021-04-09 | 百济神州(苏州)生物科技有限公司 | 一种含parp抑制剂倍半水合物产物的制备方法 |
| CN113402502B (zh) * | 2019-05-16 | 2022-10-14 | 百济神州(苏州)生物科技有限公司 | 一种parp抑制剂中间体制备的物料组合体系 |
| WO2020239097A1 (zh) | 2019-05-31 | 2020-12-03 | 百济神州有限公司 | 一种parp抑制剂微丸制剂及其制备工艺 |
| US11278532B2 (en) | 2019-08-06 | 2022-03-22 | Recurium Ip Holdings, Llc | Estrogen receptor modulators for treating mutants |
| WO2021046014A1 (en) | 2019-09-03 | 2021-03-11 | Teva Czech Industries S.R.O | Solid state forms of pamiparib and process for preparation thereof |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| TW202530228A (zh) | 2023-10-12 | 2025-08-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025217307A1 (en) | 2024-04-09 | 2025-10-16 | Revolution Medicines, Inc. | Methods for predicting response to a ras(on) inhibitor and combination therapies |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
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| RU2409361C2 (ru) | 2006-04-04 | 2011-01-20 | Пфайзер Продактс Инк. | КОМБИНИРОВАННАЯ ТЕРАПИЯ (2R,Z)-2-АМИНО-2-ЦИКЛОГЕКСИЛ-N-(5-(1-МЕТИЛ-1Н-ПИРАЗОЛ-4-ИЛ)-1-ОКСО-2,6-ДИГИДРО-1Н-[1,2]ДИАЗЕПИНО[4,5,6-cd]ИНДОЛ-8-ИЛ)АЦЕТАМИДОМ |
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| US9637488B2 (en) | 2015-01-29 | 2017-05-02 | Fuqiang Ruan | Heterocyclic compounds as inhibitors of class I PI3KS |
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| US11202782B2 (en) | 2016-09-27 | 2021-12-21 | Beigene, Ltd. | Treatment cancers using a combination comprising PARP inhibitors |
| US10899763B2 (en) | 2017-02-28 | 2021-01-26 | Beigene, Ltd. | Crystalline forms of salts of fused penta-cyclic dihydrodiazepinocarbazolones, and uses thereof |
| WO2019015561A1 (en) | 2017-07-17 | 2019-01-24 | Beigene, Ltd. | TREATMENT OF CANCERS USING A COMBINATION COMPRISING INHIBITORS OF PARP, TEMOZOLOMIDE AND / OR RADIOTHERAPY |
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