HRP20181036T1 - 2,6-supstituirani derivati purina i njihova upotreba u liječenju proliferativnih poremećaja - Google Patents
2,6-supstituirani derivati purina i njihova upotreba u liječenju proliferativnih poremećaja Download PDFInfo
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
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- 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
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- 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
- A61K31/52—Purines, e.g. adenine
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
-
- 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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- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (22)
1. Spoj formule (Ia):
,
naznačen time što
R1 je C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, 4-6-eročlani heterocikloalkil ili 4-6-eročlani heteroaril, gdje C1-C6 alkil može biti supstituiran s jednim, dva ili tri supstituenta, koje se bira iz skupine koju čine halogen, hidroksi, te C1-C3 alkoksi, gdje dodatno svaki od C3-C6 cikloalkila, 4-6-eročlanog heterocikloalkila, te 4-6-eročlanog heteroarila može neovisno biti supstituiran s jednim, dva ili tri supstituenta, koje se bira iz skupine koju čine C1-C3 alkil, hidroksi, te C1-C3 alkoksi;
prsten A je C6-C10 aril ili 5-12-eročlani heteroaril;
svaki od R2 i R5 je neovisno odsutan, vodik, halogen, cijano, difluormetil, trifluormetil, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C1-C6 alkoksi, -N(R10)(R11), C3-C5 cikloalkil ili 4-6-eročlani heterocikloalkil, gdje C1-C6 alkil može biti supstituiran s jednim, dva ili tri supstituenta, koje se bira iz skupine koju čine halogen, hidroksi, C1-C6 alkoksi, te -N(R12)(R13);
R3 je odsutan, vodik, halogen, C1-C6 alkil, C2-C6 alkinil, C1-C6 alkoksi, C3-C7 cikloalkil ili 3-7-eročlani heterocikloalkil, gdje svaki od C1-C6 alkila i C1-C6 alkoksi može biti supstituiran s jednom, dvije ili tri skupine R14, te gdje dodatno svaki od C3-C7 cikloalkila i 3-7-eročlanog heterocikloalkila može biti supstituiran s jednom, dvije ili tri skupine R15;
R4 je odsutan, vodik, halogen, C1-C6 alkil ili C3-C6 cikloalkil, gdje se R2 i R3 ili R3 i R4 može kombinirati kako bi tvorili C5-C7 cikloalkilni prsten ili 5-7-eročlani heterocikloalkilni prsten, gdje dodatno svaki od C5-C7 cikloalkilnog prstena i 5-7-eročlanog heterocikloalkilnog prstena može neovisno biti supstituiran s jednom, dvije ili tri skupine R14;
svaki od R6 i R8 je neovisno vodik, halogen, cijano, hidroksi, difluormetil, trifluormetil, C1-C3 alkil, C1-C3 alkoksi ili C3-C5 cikloalkil, gdje C1-C3 alkil može biti supstituiran s hidroksi, difluormetilom, trifluormetilom, C1-C3 alkoksi ili C3-C5 cikloalkilom;
R7 je
G je -NR18-;
R12 i R13 je svaki od neovisno vodik ili C1-C3 alkil;
R10 i R11 je svaki od neovisno vodik ili C1-C6 alkil; ili se R10 i R11, zajedno s dušikom na kojeg su vezani, može kombinirati kako bi tvorili 4-7-eročlani heterocikloalkilni prsten, kada je svaki od R10 i R11 C1-C3 alkil, gdje dobiveni 4-7-eročlani heterocikloalkilni prsten može biti supstituiran s jednom, dvije, tri ili četiri skupine R15;
svaki R14 je neovisno halogen, cijano, C1-C3 alkil, hidroksi, C1-C6 alkoksi, -N(R19)(R20), -CON(R21)(R22) ili 3-7-eročlani heterocikloalkil, gdje 3-7-eročlani heterocikloalkil može biti supstituiran s jednom, dvije, tri ili četiri skupine R15;
svaki R15 je neovisno halogen, C1-C3 alkil, hidroksi, C1-C6 alkoksi, -NH2, -NHCH3 ili -N(CH3)2;
svaki od R16 i R17 je neovisno vodik ili C1-C6 alkil, gdje C1-C6 alkil može biti supstituiran s -N(R23)(R24), uz uvjet da R16 i R17 mogu tvoriti C3-C5 cikloalkilni prsten;
R18 je vodik ili C1-C3 alkil;
svaki R19, R20, R21, R22, R23, te R24 je neovisno vodik ili C1-C3 alkil;
n je 0, 1 ili 2; i
p je 0, 1 ili 2; ili
njegova farmaceutski prihvatljiva sol.
2. Spoj ili sol u skladu s patentnim zahtjevom 1, naznačen time što je R1 C1-C6 alkil ili C3-C6 cikloalkil, gdje C1-C6 alkil može biti supstituiran s hidroksi, te gdje dodatno C3-C6 cikloalkil može biti supstituiran s C1-C3 alkilom.
3. Spoj ili sol u skladu s patentnim zahtjevom 1 ili 2, naznačen time što je R1 metil, etil, izopropil ili tert-butil.
4. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time što je R2 vodik, metil, difluormetil ili metoksi.
5. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time što je R5 vodik, C1-C6 alkil ili C1-C6 alkoksi.
6. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time što je R5 vodik, metil ili metoksi.
7. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time što je R3 C1-C6 alkil ili 3-7-eročlani heterocikloalkil, gdje C1-C6 alkil može biti supstituiran s jednom ili dvije skupine R14, te gdje dodatno 3-7-eročlani heterocikloalkil može biti supstituiran s C1-C3 alkilom.
8. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time što je R3 metil.
9. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-8, naznačen time što ima formulu (IIIa):
,
ili njegova farmaceutski prihvatljiva sol,
naznačen time što
svaki od R2 i R5 je neovisno vodik, halogen, cijano, difluormetil, trifluormetil, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C1-C6 alkoksi, -N(R10)(R11), C3-C5 cikloalkil ili 4-6-eročlani heterocikloalkil, gdje C1-C6 alkil može biti supstituiran s jednim, dva ili tri supstituenta, koje se bira iz skupine koju čine halogen, hidroksi, C1-C6 alkoksi, te -N(R12)(R13),
uz uvjet da je najmanje jedan od R2 i R5 vodik; i
R3 je vodik, halogen, C1-C6 alkil, C2-C6 alkinil, C1-C6 alkoksi, C3-C7 cikloalkil ili 3-7-eročlani heterocikloalkil, gdje svaki od C1-C6 alkila i C1-C6 alkoksi može biti supstituiran s jednom, dvije ili tri skupine R14, te gdje dodatno svaki od C3-C7 cikloalkila i 3-7-eročlanog heterocikloalkila može biti supstituiran s jednom, dvije ili tri skupine R15.
10. Spoj ili sol u skladu s patentnim zahtjevom 1 ili 9, naznačen time što je n 0.
11. Spoj ili sol u skladu s patentnim zahtjevom 1 ili 9, naznačen time što je n 1.
12. Spoj ili sol u skladu s patentnim zahtjevom 1 ili 9, naznačen time što p je 1.
13. Spoj ili sol u skladu s patentnim zahtjevom 1 ili 9, naznačen time što je n 1 i p je 1.
14. Spoj ili sol u skladu s patentnim zahtjevom 1 ili 9, naznačen time što je svaki od R6 i R8 neovisno vodik, halogen, C1-C3 alkil ili C1-C3 alkoksi.
15. Spoj ili sol u skladu s patentnim zahtjevom 1 ili 9, naznačen time što je R6 vodik, fluor, metil ili metoksi.
16. Spoj ili sol u skladu s patentnim zahtjevom 1 ili 9, naznačen time što je R6 fluor.
17. Spoj ili sol u skladu s patentnim zahtjevom 1 ili 9, naznačen time što je R8 vodik, fluor ili metil.
18. Spoj u skladu s patentnim zahtjevom 9, ili s bilo kojim od patentnih zahtjeva 14 do 17 kao ovisnih o patentnom zahtjevu 9, naznačen time što ima formulu (IIIb):
,
ili njegova farmaceutski prihvatljiva sol.
19. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je
,
ili njegova farmaceutski prihvatljiva sol.
20. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, ili njegovu farmaceutski prihvatljivu sol, kao i farmaceutski prihvatljivu podlogu ili razrjeđivač.
21. Kombinacija spoja u skladu s bilo kojim od patentnih zahtjeva 1-19, ili njegove farmaceutski prihvatljive soli, s protutumorskim sredstvom, naznačena time što je namijenjena liječenju raka.
22. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-19, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u liječenju abnormalnog staničnog rasta kod sisavca.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361907322P | 2013-11-21 | 2013-11-21 | |
| EP14806447.0A EP3071570B1 (en) | 2013-11-21 | 2014-11-10 | 2,6-substituted purine derivatives and their use in the treatment of proliferative disorders |
| PCT/IB2014/065935 WO2015075598A1 (en) | 2013-11-21 | 2014-11-10 | 2,6-substituted purine derivatives and their use in the treatment of proliferative disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20181036T1 true HRP20181036T1 (hr) | 2018-08-24 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20181036TT HRP20181036T1 (hr) | 2013-11-21 | 2014-11-10 | 2,6-supstituirani derivati purina i njihova upotreba u liječenju proliferativnih poremećaja |
Country Status (39)
| Country | Link |
|---|---|
| US (1) | US9290496B2 (hr) |
| EP (1) | EP3071570B1 (hr) |
| JP (2) | JP6166845B2 (hr) |
| KR (1) | KR101919672B1 (hr) |
| CN (1) | CN105916853B (hr) |
| AP (1) | AP2016009219A0 (hr) |
| AR (1) | AR098492A1 (hr) |
| AU (1) | AU2014351433B2 (hr) |
| CA (1) | CA2931034C (hr) |
| CL (1) | CL2016001151A1 (hr) |
| CR (1) | CR20160236A (hr) |
| CU (1) | CU24402B1 (hr) |
| CY (1) | CY1120478T1 (hr) |
| DK (1) | DK3071570T3 (hr) |
| DO (1) | DOP2016000115A (hr) |
| EA (1) | EA029842B1 (hr) |
| ES (1) | ES2681799T3 (hr) |
| GE (1) | GEP20186878B (hr) |
| GT (1) | GT201600091A (hr) |
| HR (1) | HRP20181036T1 (hr) |
| HU (1) | HUE039858T2 (hr) |
| IL (1) | IL245698B (hr) |
| LT (1) | LT3071570T (hr) |
| MA (1) | MA39043B1 (hr) |
| MD (1) | MD20160053A2 (hr) |
| MX (1) | MX2016006397A (hr) |
| MY (1) | MY184433A (hr) |
| NI (1) | NI201600072A (hr) |
| PE (1) | PE20160885A1 (hr) |
| PH (1) | PH12016500911A1 (hr) |
| PL (1) | PL3071570T3 (hr) |
| PT (1) | PT3071570T (hr) |
| RS (1) | RS57537B1 (hr) |
| SI (1) | SI3071570T1 (hr) |
| TN (1) | TN2016000188A1 (hr) |
| TW (1) | TWI538913B (hr) |
| UA (1) | UA115388C2 (hr) |
| UY (1) | UY35845A (hr) |
| WO (1) | WO2015075598A1 (hr) |
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| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| JP6458039B2 (ja) | 2013-09-18 | 2019-01-23 | 北京韓美薬品有限公司 | Ｂｔｋ及び／又はｊａｋ３キナーゼの活性を抑制する化合物 |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| RU2017139771A (ru) * | 2015-05-12 | 2019-06-13 | Зено Роялтис Энд Майлстоунс, Ллс | Бициклические соединения |
| CN109937039A (zh) * | 2016-09-30 | 2019-06-25 | 斯坦福国际研究院 | 用于癌症治疗的双重clk/cdk1抑制剂 |
| EP3541389A1 (en) | 2016-11-16 | 2019-09-25 | Pfizer Inc | Combination of an egfr t790m inhibitor and a cdk inhibitor for the treatment of non-small cell lung cancer |
| BR112019012682A2 (pt) | 2016-12-23 | 2019-12-17 | Arvinas Operations Inc | moléculas quiméricas visando a proteólise de egfr e métodos associados de uso |
| EP3592740B1 (en) | 2017-03-10 | 2022-02-09 | Pfizer Inc. | Cyclic substituted imidazo[4,5-c]quinoline derivatives |
| KR102582626B1 (ko) | 2017-03-10 | 2023-09-22 | 화이자 인코포레이티드 | Lrrk2 억제제로서의 신규 이미다조[4,5-c]퀴놀린 유도체 |
| EP3814354B1 (en) * | 2018-06-22 | 2023-11-08 | The Royal Institution for the Advancement of Learning / McGill University | Purine compounds and method for the treatment of cancer |
| WO2020175968A1 (ko) * | 2019-02-28 | 2020-09-03 | 주식회사 보로노이 | N을 포함하는 헤테로아릴 유도체 및 이를 유효성분으로 포함하는 약학적 조성물 |
| AU2021276206B2 (en) * | 2020-05-20 | 2024-12-12 | Tyk Medicines, Inc. | Compound used as RET kinase inhibitor and application thereof |
| US12115157B2 (en) | 2021-09-14 | 2024-10-15 | Boehringer Ingelheim International Gmbh | 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives and the use thereof as medicament |
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