HRP20230537T1 - Supstituirani derivati tieno[2,3-d]pirimidina kao inhibitori za menin-mll i postupci za uporabu - Google Patents
Supstituirani derivati tieno[2,3-d]pirimidina kao inhibitori za menin-mll i postupci za uporabu Download PDFInfo
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- HRP20230537T1 HRP20230537T1 HRP20230537TT HRP20230537T HRP20230537T1 HR P20230537 T1 HRP20230537 T1 HR P20230537T1 HR P20230537T T HRP20230537T T HR P20230537TT HR P20230537 T HRP20230537 T HR P20230537T HR P20230537 T1 HRP20230537 T1 HR P20230537T1
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- 239000003112 inhibitor Substances 0.000 title 1
- DDWBRNXDKNIQDY-UHFFFAOYSA-N thieno[2,3-d]pyrimidine Chemical class N1=CN=C2SC=CC2=C1 DDWBRNXDKNIQDY-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 27
- 150000003839 salts Chemical class 0.000 claims 6
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 1
- 125000003837 (C1-C20) alkyl group Chemical group 0.000 claims 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000006649 (C2-C20) alkynyl group Chemical group 0.000 claims 1
- 125000006593 (C2-C3) alkynyl group Chemical group 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 1
- 125000003358 C2-C20 alkenyl group Chemical group 0.000 claims 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
Classifications
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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
- A61K31/535—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- 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
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
- C07D295/205—Radicals derived from carbonic acid
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Claims (18)
1. Spoj, naznačen time, da ima Formulu (II-A):
[image]
ili njegova farmaceutski prihvatljiva sol, gdje:
C se bira od piperidinila i piperazinila;
L2 je -CH2-;
L3 je -CH2CH(R56)-, i R56 je metil;
R1 je C1-3 haloalkil;
R2 se bira od sljedećih: halogen, -OR52, -N(R52)2, -CN, C1-3 alkil, C1-3 alkil-OR52, C1-3 alkil-N(R52)2, C1-3 haloalkil, C2-3 alkenil, i C2-3 alkinil;
R3 se bira od sljedećih: vodik, halogen, -OH, -N(R52)2, -CN, -C(O)OR52, C1-3 alkil, i C1-3 haloalkil;
svaki RA i RB se kod svakog pojavljivanja neovisno bira od sljedećih: halogen, -CN, -OR52, -N(R52)2, -NR53R54, -C(O)R52, -C(O)OR52, -OC(O)R52, -NR52C(O)R52, -C(O)N(R52)2, -C(O)NR53R54, =O, C1-10 alkil, C2-10 alkenil, i C2-10 alkinil;
RC se bira od sljedećih: -C(O)R52, -S(=O)R52, -S(=O)2R52, -S(=O)2N(R52)2, -S(=O)2NR53R54, -NR52S(=O)2R52, =O, C1-3 alkil, i C1-3 haloalkil, ili dvije skupine RC koje su vezane s različitim atomima, mogu zajedno tvoriti C1-3 most;
svaki m i p je neovisno cijeli broj od 0 do 6;
n je cijeli broj od 1 do 4;
R51 se bira od sljedećih: vodik i C1-6 alkil;
R52 se kod svakog pojavljivanja neovisno bira od sljedećih: vodik; i C1-20 alkil, C2-20 alkenil, C2-20 alkinil, 1-člani do 6-člani heteroalkil, C3-12 karbocikl, i 3-člani do 12-člani heterocikl, od kojih je svaki opcionalno supstituiran sa sljedećima: halogen, -CN, -NO2, -NH2, -NHCH3, -NHCH2CH3, =O, -OH, -OCH3, -OCH2CH3, C3-12 karbocikl, ili 3-člani do 6-člani heterocikl; i
R53 i R54 se uzimaju zajedno s dušikovim atomom s kojim su vezani, za tvorbu heterocikla.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da m je 0 i n je cijeli broj od 1 do 3.
3. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time, da se L3 bira od sljedećih:
[image]
i
[image]
4. Spoj prema bilo kojem od patentnih zahtjeva 1 do 2, naznačen time, da L3 je
[image]
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 2, naznačen time, da L3 je
[image]
6. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj ima strukturu Formule (II-C):
[image]
ili njegova farmaceutski prihvatljiva sol.
7. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj ima strukturu Formule (II-C):
[image]
8. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj ima strukturu Formule (II-F), ili (II-H):
[image]
ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj ima strukturu Formule (II-F), ili (II-H):
[image]
10. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj ima strukturu Formule (II-F):
[image]
ili njegova farmaceutski prihvatljiva sol.
11. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj ima strukturu Formule (II-F):
[image]
12. Spoj prema patentnom zahtjevu 1, naznačen time, da se spoj bira iz skupine koju čine:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
i
[image]
ili njegova farmaceutski prihvatljiva sol.
13. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj je:
[image]
ili njegova farmaceutski prihvatljiva sol.
14. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj je:
[image]
15. Farmaceutski pripravak, naznačen time, da sadrži spoj prema bilo kojem od prethodnih patentnih zahtjeva, i farmaceutski prihvatljiv nosač.
16. Spoj prema bilo kojem od patentnih zahtjeva 1 do 14, naznačen time, da je za uporabu u liječenju bolesti ili stanja.
17. Spoj za uporabu prema patentnom zahtjevu 16, naznačen time, da bolest ili stanje je leukemija, hematološka malignost, rak solidnih tumora, rak prostate, rak dojke, rak jetre, rak mozga, ili dijabetes.
18. Spoj za uporabu prema patentnom zahtjevu 17, naznačen time, da bolest ili stanje je leukemija.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662309372P | 2016-03-16 | 2016-03-16 | |
| US201662334369P | 2016-05-10 | 2016-05-10 | |
| US201662431389P | 2016-12-07 | 2016-12-07 | |
| US201762446640P | 2017-01-16 | 2017-01-16 | |
| PCT/US2017/022564 WO2017161028A1 (en) | 2016-03-16 | 2017-03-15 | Substituted inhibitors of menin-mll and methods of use |
| EP17767462.9A EP3429591B1 (en) | 2016-03-16 | 2017-03-15 | Substituted thieno[2,3-d]pyrimidine derivatives as inhibitors of menin-mll and methods of use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20230537T1 true HRP20230537T1 (hr) | 2023-08-04 |
Family
ID=59851028
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20230537TT HRP20230537T1 (hr) | 2016-03-16 | 2017-03-15 | Supstituirani derivati tieno[2,3-d]pirimidina kao inhibitori za menin-mll i postupci za uporabu |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US10781218B2 (hr) |
| EP (2) | EP3429591B1 (hr) |
| JP (3) | JP6919977B2 (hr) |
| KR (1) | KR102419531B1 (hr) |
| CN (2) | CN109152784B (hr) |
| AU (1) | AU2017232516B2 (hr) |
| BR (1) | BR112018068703B1 (hr) |
| CA (1) | CA3015847A1 (hr) |
| CY (1) | CY1126066T1 (hr) |
| DK (1) | DK3429591T3 (hr) |
| ES (1) | ES2947636T3 (hr) |
| FI (1) | FI3429591T3 (hr) |
| HK (1) | HK1259232A1 (hr) |
| HR (1) | HRP20230537T1 (hr) |
| HU (1) | HUE061989T2 (hr) |
| IL (1) | IL261606B (hr) |
| LT (1) | LT3429591T (hr) |
| MD (1) | MD3429591T2 (hr) |
| MX (1) | MX2018011105A (hr) |
| PH (1) | PH12018501952A1 (hr) |
| PL (1) | PL3429591T3 (hr) |
| PT (1) | PT3429591T (hr) |
| RS (1) | RS64261B1 (hr) |
| SG (1) | SG11201807982UA (hr) |
| SI (1) | SI3429591T1 (hr) |
| TW (1) | TWI747889B (hr) |
| WO (1) | WO2017161028A1 (hr) |
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| EA202092627A1 (ru) | 2013-11-18 | 2021-09-30 | Глобал Блад Терапьютикс, Инк. | Соединения и их применения для модуляции гемоглобина |
| US10246464B2 (en) | 2014-09-09 | 2019-04-02 | The Regents Of The University Of Michigan | Thienopyrimidine and thienopyridine compounds and methods of use thereof |
| TWI703150B (zh) | 2015-06-04 | 2020-09-01 | 美商庫拉腫瘤技術股份有限公司 | 用於抑制ｍｅｎｉｎ及ｍｌｌ蛋白之交互作用的方法及組合物 |
| WO2016197027A1 (en) | 2015-06-04 | 2016-12-08 | Kura Oncology, Inc. | Methods and compositions for inhibiting the interaction of menin with mll proteins |
| GB201516504D0 (en) | 2015-09-17 | 2015-11-04 | Astrazeneca Ab | Imadazo(4,5-c)quinolin-2-one Compounds and their use in treating cancer |
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