HRP20240793T1 - Modulatori enzima koji modificiraju metil, njihovi pripravci i upotreba - Google Patents
Modulatori enzima koji modificiraju metil, njihovi pripravci i upotreba Download PDFInfo
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- HRP20240793T1 HRP20240793T1 HRP20240793TT HRP20240793T HRP20240793T1 HR P20240793 T1 HRP20240793 T1 HR P20240793T1 HR P20240793T T HRP20240793T T HR P20240793TT HR P20240793 T HRP20240793 T HR P20240793T HR P20240793 T1 HRP20240793 T1 HR P20240793T1
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- alkyl
- compound according
- halo
- pharmaceutically acceptable
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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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
-
- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Pyridine Compounds (AREA)
Claims (15)
1. Spoj formule IV ili VI:
[image]
ili
[image]
ili njegova farmaceutski prihvatljiva sol, naznačen time što:
R1 je -SCH3 ili klor;
X je CH;
Ra je vodik, (C1-C4)alkil, ili halo(C1-C4)alkil;
Rb je (C1-C4)alkil, halo(C1-C4)alkil, ili 4-7 pri čemu je navedeni heterociklil izborno supstituiran s 1 do 3 skupine odabrane iz niza koji sadrži halo, (C1-C4)alkil, halo(C1-C4)alkil, (C1-C4)alkoksi, i halo(C1-C4)alkoksi; ili
Ra i Rb zajedno s atomom dušika na koji su oni vezani tvore 4-7 člani heterociklil po izboru supstituiran s 1 do 3 skupine odabrane iz niza koji sadrži halo, (C1-C4)alkil, halo(C1-C4)alkil, i -ORc;
Rc je (C1-C4)alkil, halo(C1-C4)alkil, ili (C3-C7)cikloalkil;
R6 je halo(C1-C4)alkil.
2. Spoj prema zahtjevu 1, naznačen time što spoj ima formulu:
[image]
ili njegova farmaceutski prihvatljiva sol.
3. Spoj prema bilo kojem od zahtjeva 1 ili 2, naznačen time što Rb je (C1-C4)alkil ili oksetanil, pri čemu je navedeni oksetanil izborno supstituiran s halo(C1-C4)alkilom; ili Ra i Rb zajedno s atomom dušika na koji su oni vezani tvore azetidinil izborno supstituiran s halo ili -ORc.
4. Spoj prema bilo kojem od zahtjeva 1 do 3, naznačen time što Ra je vodik ili metil; i Rb je metil ili oksetanil, pri čemu je navedeni oksetanil izborno supstituiran s -CH2F ili - CF3.
5. Spoj prema bilo kojem od zahtjeva 1 do 4, naznačen time što Ra i Rb zajedno s atomom dušika na koji su oni vezani tvore azetidinil izborno supstituiran s 1 do 2 fluora ili -ORc; i Rc je -CH3, -CHF2, ili ciklopropil.
6. Spoj prema zahtjevu 1, naznačen time što spoj ima formulu:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
ili
[image]
ili njegova farmaceutski prihvatljiva sol.
7. Spoj prema bilo kojem od zahtjeva 1 do 6, naznačen time što skupina
[image]
i NRaRb su orijentirani trans oko cikloheksila.
8. Spoj prema bilo kojem od zahtjeva 1 do 6, naznačen time što skupina
[image]
i NRaRb su orijentirani cis oko cikloheksila.
9. Spoj prema bilo kojem od zahtjeva 1 do 8, naznačen time što stereokemijska konfiguracija kiralnog središta 1,3-dioksolanila je R.
10. Spoj prema bilo kojem od zahtjeva 1 do 8, stereokemijska konfiguracija kiralnog središta 1,3-dioksolanila je S.
11. Spoj prema zahtjevu 1, naznačen time što spoj ima formulu:
[image]
ili njegova farmaceutski prihvatljiva sol.
12. Spoj prema zahtjevu 11, naznačen time što spoj ima formulu:
[image]
ili njegova farmaceutski prihvatljiva sol.
13. Farmaceutski pripravak naznačen time što sadrži spoj prema bilo kojem od zahtjeva 1 do 12, ili njegovu farmaceutski prihvatljivu sol; i farmaceutski prihvatljiv nosač.
14. Spoj prema bilo kojem od zahtjeva 1 do 12, ili njegova farmaceutski prihvatljiva sol, za upotrebu u liječenju raka kod subjekta.
15. Spoj za upotrebu prema zahtjevu 14, naznačen time što je rak odabran između raka dojke, raka prostate, raka debelog crijeva, karcinoma bubrežnih stanica, multiformnog glioblastoma, raka mokraćnog mjehura, melanoma, raka bronha, limfoma, kolangiosarkoma, multiplog mijeloma, raka pluća, raka jajnika, i raka jetre.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862659408P | 2018-04-18 | 2018-04-18 | |
EP19722363.9A EP3781561B1 (en) | 2018-04-18 | 2019-04-17 | Modulators of methyl modifying enzymes, compositions and uses thereof |
PCT/US2019/027932 WO2019204490A1 (en) | 2018-04-18 | 2019-04-17 | Modulators of methyl modifying enzymes, compositions and uses thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20240793T1 true HRP20240793T1 (hr) | 2024-09-13 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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HRP20240793TT HRP20240793T1 (hr) | 2018-04-18 | 2019-04-17 | Modulatori enzima koji modificiraju metil, njihovi pripravci i upotreba |
Country Status (34)
Country | Link |
---|---|
US (3) | US10689371B2 (hr) |
EP (2) | EP3781561B1 (hr) |
JP (2) | JP7256823B2 (hr) |
KR (2) | KR102798145B1 (hr) |
CN (2) | CN111989325B (hr) |
AR (1) | AR114793A1 (hr) |
AU (1) | AU2019255310B2 (hr) |
BR (1) | BR112020021194A2 (hr) |
CA (1) | CA3098428A1 (hr) |
CL (1) | CL2020002698A1 (hr) |
CO (1) | CO2020014217A2 (hr) |
CR (1) | CR20200553A (hr) |
DK (1) | DK3781561T3 (hr) |
EA (1) | EA202092490A1 (hr) |
ES (1) | ES2983344T3 (hr) |
FI (1) | FI3781561T3 (hr) |
HR (1) | HRP20240793T1 (hr) |
HU (1) | HUE066783T2 (hr) |
IL (1) | IL278013B2 (hr) |
LT (1) | LT3781561T (hr) |
MA (1) | MA52288B1 (hr) |
MD (1) | MD3781561T2 (hr) |
MX (1) | MX2020010999A (hr) |
PE (1) | PE20201448A1 (hr) |
PH (1) | PH12020551578A1 (hr) |
PL (1) | PL3781561T3 (hr) |
PT (1) | PT3781561T (hr) |
RS (1) | RS65621B1 (hr) |
SG (1) | SG11202009438UA (hr) |
SI (1) | SI3781561T1 (hr) |
SM (1) | SMT202400233T1 (hr) |
TW (1) | TWI828677B (hr) |
UA (1) | UA127357C2 (hr) |
WO (1) | WO2019204490A1 (hr) |
Families Citing this family (18)
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SG11202009438UA (en) | 2018-04-18 | 2020-11-27 | Constellation Pharmaceuticals Inc | Modulators of methyl modifying enzymes, compositions and uses thereof |
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KR102689665B1 (ko) | 2019-02-19 | 2024-07-31 | 한미약품 주식회사 | 신규한 헤테로트리시클릭 유도체 화합물 및 이의 용도 |
KR20220041130A (ko) * | 2019-07-24 | 2022-03-31 | 콘스텔레이션 파마슈티칼스, 인크. | 암 치료를 위한 병용 요법에서의 ezh2 억제 |
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