ME02356B - Inhibitor bromodomena benzodiazepina - Google Patents
Inhibitor bromodomena benzodiazepinaInfo
- Publication number
- ME02356B ME02356B MEP-2016-52A MEP5216A ME02356B ME 02356 B ME02356 B ME 02356B ME P5216 A MEP5216 A ME P5216A ME 02356 B ME02356 B ME 02356B
- Authority
- ME
- Montenegro
- Prior art keywords
- 6alkyl
- compound
- pharmaceutically acceptable
- acceptable salt
- halo
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 5
- -1 carbocyclylC1-4alkyl Chemical group 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 125000004452 carbocyclyl group Chemical group 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 2
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 230000002440 hepatic effect Effects 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000000926 neurological effect Effects 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 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
- C07D487/04—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
- A61K31/55—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
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
-
- 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
- A61P37/02—Immunomodulators
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (10)
1. Jedinjenje formule (Ic) ili njegova farmaceutski prihvatljiva sogde R1 je C1-3alkil;R2 je -NR2aR2a’ ili -OR2b;gde jedan od R2a ili R2’a je H, i R2b ili drugi od R2a ili R2’a je izabran od C1-6alkil, haloC1-6alkil, R2cR2’cN-C1-6alkil, karbociklil, karbociklilC1-4alkil, heterociklil i heterociklilC1-4alkil,gde je bilo koja karbociklil ili heterociklil grupa opciono supstituisana sa jednom ili više grupa izabranih od halogena, C1-6alkil, haloC1-6alkil, C1-6alkoksi, haloC1-6alkoksi, karbonil, -CO-karbociklil, azido, nitro i cijano,gde -CO-karbocikl grupa može biti dalje opciono supstituisansa sa jednom ili više grupa izabranih od halogena, C1-6alkil, haloC1-6alkil, C1-6alkoksi, haloC1-6alkoksi, azido, nitro i cijano;ili dve susedne grupe na bilo kom od karbociklil ili heterociklil grupa zajedno sa atomom koji ih povezuje obrazuju 5- ili 6-člani prsten koji može sadržati 1 ili 2 heteroatoma nezavisno izabrana od O, S i N;ili R2a i R2’a zajedno sa N-atomom za koji su vezani obrazuju 5-, 6- ili 7-člani prsten koji može opciono sadržati 1 ili 2 heteroatoma nezavisno izabrana od O, S i N; gde 5-, 6- ili 7-člani prsten može biti dalje opciono supstituisan sa C1-6alkil;R2c i R2’c su nezavisno H i C1-6alkil;svaki R3 je nezavisno izabran od H, hidroksi, halo, C1-6alkil, halo C1-6alkil, C1-6alkoksi, halo C1-6alkoksi, nitro, cijano, CF3, -OCF3 i -COOR5;R4 je hidroksi, halo, C1-6alkil, halo C1-6alkil, C1-6alkoksi, halo C1-6alkoksi, nitro, cijano, CF3, -OCF3; -COOR5 ili-OS(O)2C1-4alkil;R5 je C1-3alkil; in je ceo broj od 1 do 5 za upotrebu u lečenju kancera.
2. Jedinjenje ili njegova farmaceutski prihvatljiva so za upotrebu prema zahtevu 1, gde R4 predstavlja hidroksil ili C1-6alkoksi.
3. Jedinjenje ili njegova farmaceutski prihvatljiva so za upotrebu prema zahtevu 1, gde je jedinjenje formule (Ib) pri čemu su R1, R2 i R3 i n kao što je definisano u patentnom zahtevu 1.
4. Jedinjenje ili njegova farmaceutski prihvatljiva so za upotrebu prema bilo kom od patentnih zahteva 1-3, gde je R1 metil.
5. Jedinjenje ili njegova farmaceutski prihvatljiva so za upotrebu prema bilo kom od patentnih zahteva 1-4, gde je n jednako 1.
6. Jedinjenje ili njegova farmaceutski prihvatljiva so za upotrebu prema bilo kom od patentnih zahteva 1-5, gde je R3 3-fluoro, 4-hloro, 4-fluoro, 4-metoksi ili 4-CF3.
7. Jedinjenje ili njegova farmaceutski prihvatljiva so za upotrebu prema bilo kom od patentnih zahteva 1-6, koje je S-enantiomer.
8. Jedinjenje ili njegova farmaceutski prihvatljiva so za upotrebu prema bilo kom od patentnih zahteva 1-7, gde je kancer izabran od hematoloških, epitelijalnih karcinoma uključujući pluća, grudi i creva, mezenhimalne, hepatične, renalne i neurološke tumore.
9. Upotreba jedinjenja ili njihove farmaceutski prihvatljive soli kao što je definisano prema bilo kom od patentnih zahteva 1-7, u proizvodnji leka za lečenje kancera.
10. Farmaceutska kompozicija koja sadrži jedinjenje formule (Ic) ili njegovu farmaceutski prihvatljvu so kao što je definisano prema bilo kom od patentnih zahteva 1-7 i jedan ili više farmaceutski prihvatljivih nosača, razblaživača ili ekscipijenata za upotrebu u lečenju kancera.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0919433A GB0919433D0 (en) | 2009-11-05 | 2009-11-05 | Novel compounds |
| GBGB1010509.6A GB201010509D0 (en) | 2010-06-22 | 2010-06-22 | Novel compounds |
| PCT/EP2010/061518 WO2011054553A1 (en) | 2009-11-05 | 2010-08-06 | Benzodiazepine bromodomain inhibitor |
| GBGB1014231.3A GB201014231D0 (en) | 2010-08-25 | 2010-08-25 | Novel compounds |
| PCT/EP2010/066697 WO2011054845A1 (en) | 2009-11-05 | 2010-11-03 | Benzodiazepine bromodomain inhibitor |
| EP10773325.5A EP2496582B1 (en) | 2009-11-05 | 2010-11-03 | Benzodiazepine bromodomain inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02356B true ME02356B (me) | 2016-06-20 |
Family
ID=43969589
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2016-52A ME02356B (me) | 2009-11-05 | 2010-11-03 | Inhibitor bromodomena benzodiazepina |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US9102677B2 (me) |
| EP (2) | EP2496582B1 (me) |
| JP (3) | JP5702396B2 (me) |
| KR (1) | KR20120097508A (me) |
| CN (1) | CN102781943B (me) |
| AU (1) | AU2010317096B2 (me) |
| BR (1) | BR112012010705A2 (me) |
| CA (1) | CA2779423C (me) |
| CY (1) | CY1117424T1 (me) |
| DK (1) | DK2496582T3 (me) |
| EA (1) | EA023441B1 (me) |
| ES (2) | ES2654423T3 (me) |
| HK (1) | HK1221221A1 (me) |
| HR (1) | HRP20160253T1 (me) |
| HU (1) | HUE026967T2 (me) |
| IL (2) | IL219253A (me) |
| ME (1) | ME02356B (me) |
| MX (1) | MX341212B (me) |
| PL (1) | PL2496582T3 (me) |
| RS (1) | RS54645B1 (me) |
| SI (1) | SI2496582T1 (me) |
| SM (1) | SMT201600104B (me) |
| WO (1) | WO2011054845A1 (me) |
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| KR20120097508A (ko) * | 2009-11-05 | 2012-09-04 | 글락소스미스클라인 엘엘씨 | 벤조디아제핀 브로모도메인 억제제 |
| JP5715241B2 (ja) * | 2010-05-14 | 2015-05-07 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | 新生物、炎症性疾患、およびその他の障害を治療するための組成物および方法 |
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| MX373121B (es) | 2010-05-14 | 2020-04-30 | Dana Farber Cancer Inst Inc | Composiciones y metodos para el tratamiento de leucemia. |
| EP2450039A1 (en) | 2010-11-08 | 2012-05-09 | PAION UK Ltd. | Dosing regimen for sedation with CNS 7056 (Remimazolam) |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
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| AR094963A1 (es) | 2013-03-04 | 2015-09-09 | Ono Pharmaceutical Co | Reacción de oxidación excelente en el índice de conversión |
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