HRP20241237T1 - Derivati n-(piridinil)acetamida kao inhibitori p300/cbp hat i postupci za njihovu upotrebu - Google Patents
Derivati n-(piridinil)acetamida kao inhibitori p300/cbp hat i postupci za njihovu upotrebu Download PDFInfo
- Publication number
- HRP20241237T1 HRP20241237T1 HRP20241237TT HRP20241237T HRP20241237T1 HR P20241237 T1 HRP20241237 T1 HR P20241237T1 HR P20241237T T HRP20241237T T HR P20241237TT HR P20241237 T HRP20241237 T HR P20241237T HR P20241237 T1 HRP20241237 T1 HR P20241237T1
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- Croatia
- Prior art keywords
- image
- compound according
- halo
- 4alkyl
- 6alkyl
- Prior art date
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- 239000003112 inhibitor Substances 0.000 title 1
- QROKOTBWFZITJZ-UHFFFAOYSA-N n-pyridin-2-ylacetamide Chemical class CC(=O)NC1=CC=CC=N1 QROKOTBWFZITJZ-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 18
- 125000005843 halogen group Chemical group 0.000 claims 12
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 3
- -1 haloC1-3alkoxy Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 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
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 1
- 229910006074 SO2NH2 Inorganic materials 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000016097 disease of metabolism Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 208000019622 heart disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000000160 oxazolidinyl group Chemical group 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (15)
1. Spoj koji ima Formulu I:
[image]
ili njegova farmaceutski prihvatljiva sol, naznačen time što
R1, R3, i R4 su svaki neovisno vodik ili C1-4alkil;
R2 je fenil ili pirazolil, od kojih je svaki izborno supstituiran s halo ili C1-4alkilom;
R5 je C1-6alkil supstituiran s 4- do 6-članim heterociklilom ili 5- do 6-članim heteroarilm, pri čemu su svaki navedeni 4- do 6-člani heterociklil ili 5- do 6-člani heteroaril izborno supstituirani s 1 do 3 skupine odabrane od Rd; ili R5 je 4- do 6-člani heterociklil ili 5- do 6-člani heteroaril, pri čemu su svaki navedeni 4- do 6-člani heterociklil ili 5- do 6-člani heteroaril izborno supstituirani s 1 do 3 skupine odabrane od Rd;
Ra, ako je prisutan, je C1-3alkil, C1-3alkoksi, halo(C1-3alkil), haloC1-3alkoksi, ili halo;
Rb je halo, cijano, ili -SO2NH2;
svaki Rd je neovisno halo, CN, okso, NO2, C1-6alkil, C2-6alkenil, C1-6alkoksi, halo(C1-6alkoksi), halo(C1-6alkil), -C1-6alkilORe, -C(O)Rf, -C(O)OR, -C1-6alkilC(O)ORe, -C(O)N(Re)2, -C(O)NReC1-6alkilORe, -OC1-6alkilN(Re)2, -C1-6alkilC(O)N(Re)2, -C1-6alkilN(Re)2, -N(Re)2, -C(O)NReC1-6alkilN(Re)2, -NReC1-6alkilN(Re)2, -NReC1-6alkilORe, -SORe, -S(O)2Re, -SON(Re)2, -SO2N(Re)2, -O(C3-C6)cikloalkil, -O-C1-4alkilaril, -C1-6alkil(C3-C6)cikloalkil, -C1-6alkilaril, -C1-6alkilheteroaril, -C1-6alkilheterociklil, (C3-C6)cikloalkil, heterociklil, heteroaril, ili aril, pri čemu su svaki navedeni (C3-C6)cikloalkil, heterociklil, aril, i heteroaril sami i u vezi sa -O(C3-C6)cikloalkil, -C1-6alkil(C3-C6)cikloalkil, -C1-6alkilaril, -C1-6alkilheteroaril, i -C1-6alkilheterociklil izborno supstituirani s 1 do 3 skupine odabrane između halo, C1-6alkil, C1-6haloalkil, C1-6alkoksi, C1-6haloalkoksi, -N(Re)2, -C(O)Rf, i -C1-6alkilORe;
svaki Re je neovisno vodik, halo(C1-4alkil), ili C1-4alkil;
svaki Rf je neovisno vodik, halo(C1-4alkil), C1-4alkil, ili
(C3-C4)cikloalkil;
q je 0 ili 1; i
p je 1,
pri čemu:
pojam aril odnosi se na aromatski karbociklički sustav s jednim prstenom ili sustav s dva kondenzirana prstena koji sadrži 6 do 10 atoma ugljika;
pojam heteroaril korišten sam za sebe ili kao dio većeg ostatka odnosi se na 5 do 12-člani aromatski radikal koji sadrži 1 do 4 heteroatoma odabrana između N, O, i S; i
pojam heterociklil odnosi se na 4 do 12-člani zasićeni ili djelomično nezasićeni heterociklički prsten koji sadrži 1 do 4 heteroatoma neovisno odabrana između N, O, i S.
2. Spoj prema zahtjevu 1 naznačen time što spoj ima Formulu V:
[image]
ili njegova farmaceutski prihvatljiva sol.
3. Spoj prema zahtjevu 1 ili 2, naznačen time što spoj ima Formulu VI ili VII:
[image]
ili njegova farmaceutski prihvatljiva sol.
4. Spoj prema bilo kojem od zahtjeva 1 do 3, naznačen time što soj ima Formulu VIII, IX, X, ili XI:
[image]
[image]
ili njegova farmaceutski prihvatljiva sol.
5. Spoj prema bilo kojem od zahtjeva 1 do 4, naznačen time što R2 je fenil.
6. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time što Rb je cijano.
7. Spoj prema bilo kojem od zahtjeva 1 do 6, naznačen time što R5 je C1-4alkil supstituiran s pirazolilom ili oksazolidinilom, od kojih je svaki izborno supstituiran s 1 do 3 skupine odabrane od Rd; ili R5 je piperidinil, azetidinil, heksahidropirimidinil, tetrahidrofuranil, tetrahidropiranil, oksetanil, pirazolil, pirolidinil, ili pirimidinil, od kojih je svaki izborno supstituiran s 1 do 3 skupine odabrane od Rd.
8. Spoj prema bilo kojem od zahtjeva 1 do 7, naznačen time što je Rd odabran između halo, okso, C1-4alkil, C1-4alkoksi, halo(C1-4alkil), -C1-4alkilORe, -C(O)Rf, -C(O)N(Re)2, -C1-6alkilC(O)N(Re)2, i -S(O)2Re.
9. Spoj prema bilo kojem od zahtjeva 1 do 8, naznačen time što je Rd odabran od C1-6alkila, -C(O)Rf, i okso.
10. Spoj prema bilo kojem od zahtjeva 1 do 8, naznačen time što Re je vodik ili C1-3alkil.
11. Spoj prema bilo kojem od zahtjeva 1 do 10, naznačen time što Rf je ciklopropil ili C1-4alkil.
12. Spoj prema bilo kojem od zahtjeva 1 do 11, naznačen time što R5 je
[image]
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13. Spoj prema zahtjevu 1, naznačen time što je spoj odabran između
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ili njegova farmaceutski prihvatljiva sol.
14. Farmaceutski pripravak, naznačen time što sadrži spoj prema bilo kojem od zahtjeva 1 do 13, ili njegovu farmaceutski prihvatljivu sol; i farmaceutski prihvatljiv nosač.
15. Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, ili pripravak prema zahtjevu 14, za upotrebu u liječenju poremećaja posredovanog sa CBP i/ili EP300 odabranog od raka, srčane bolesti, metaboličke bolesti, fibrozne bolesti, upalne bolesti i virusne infekcije.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962811143P | 2019-02-27 | 2019-02-27 | |
| US201962879852P | 2019-07-29 | 2019-07-29 | |
| PCT/US2020/019786 WO2020176558A1 (en) | 2019-02-27 | 2020-02-26 | P300/cbp hat inhibitors and methods for their use |
| EP20714389.2A EP3930838B1 (en) | 2019-02-27 | 2020-02-26 | N-(pyridinyl)acetamide derivatives as p300/cbp hat inhibitors and methods for their use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20241237T1 true HRP20241237T1 (hr) | 2024-12-06 |
Family
ID=70005771
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20241237TT HRP20241237T1 (hr) | 2019-02-27 | 2020-02-26 | Derivati n-(piridinil)acetamida kao inhibitori p300/cbp hat i postupci za njihovu upotrebu |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20220135538A1 (hr) |
| EP (1) | EP3930838B1 (hr) |
| JP (1) | JP7638880B2 (hr) |
| CN (1) | CN113727756B (hr) |
| AU (1) | AU2020227742A1 (hr) |
| CA (1) | CA3131383A1 (hr) |
| DK (1) | DK3930838T3 (hr) |
| ES (1) | ES2989353T3 (hr) |
| FI (1) | FI3930838T3 (hr) |
| HR (1) | HRP20241237T1 (hr) |
| HU (1) | HUE068415T2 (hr) |
| LT (1) | LT3930838T (hr) |
| PL (1) | PL3930838T3 (hr) |
| PT (1) | PT3930838T (hr) |
| RS (1) | RS65998B1 (hr) |
| SI (1) | SI3930838T1 (hr) |
| SM (1) | SMT202400386T1 (hr) |
| TW (1) | TWI850342B (hr) |
| WO (1) | WO2020176558A1 (hr) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20240122941A1 (en) * | 2020-12-25 | 2024-04-18 | National Cancer Center | Therapy based on synthetic lethality in swi/snf complex-dysfunction cancer |
| WO2025169375A1 (ja) | 2024-02-07 | 2025-08-14 | 住友ファーマ株式会社 | ４員環構造で置換された３級アミド誘導体 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112014014767A2 (pt) | 2011-12-16 | 2017-06-13 | Olema Pharmaceuticals Inc | novos compostos de benzopirano, composições e usos dos mesmos |
| US20160235716A1 (en) | 2014-09-18 | 2016-08-18 | Abbvie Inc. | Spirocyclic hat inhibitors and methods for their use |
| CN107108512B (zh) | 2014-10-10 | 2021-05-04 | 基因泰克公司 | 治疗性化合物及其用途 |
| EP3632915A1 (en) * | 2014-11-27 | 2020-04-08 | Genentech, Inc. | 4,5,6,7-tetrahydro-1 h-pyrazolo[4,3-c]pyridin-3-amine compounds as cbp and/or ep300 inhibitors |
| EP3302468A4 (en) * | 2015-06-01 | 2019-02-06 | The Scripps Research Institute | SMALL MOLECULAR ANALOGS OF NEMO BINDING PEPTIDE |
| WO2017205536A2 (en) * | 2016-05-24 | 2017-11-30 | Genentech, Inc. | Therapeutic compounds and uses thereof |
| MA45146A (fr) * | 2016-05-24 | 2021-03-24 | Constellation Pharmaceuticals Inc | Dérivés de pyrazolopyridine pour le traitement du cancer |
| EP3643703A4 (en) | 2017-06-21 | 2020-12-23 | Daiichi Sankyo Co., Ltd. | EP300 / CREBBP INHIBITOR |
| UY37866A (es) * | 2017-09-07 | 2019-03-29 | Glaxosmithkline Ip Dev Ltd | Nuevos compuestos derivados de benzoimidazol sustituidos que reducen la proteína myc (c-myc) en las células e inhiben la histona acetiltransferasa de p300/cbp. |
| AU2019220662B2 (en) * | 2018-02-16 | 2024-06-13 | Constellation Pharmaceuticals, Inc. | P300/CBP HAT inhibitors |
-
2020
- 2020-02-26 HR HRP20241237TT patent/HRP20241237T1/hr unknown
- 2020-02-26 CA CA3131383A patent/CA3131383A1/en active Pending
- 2020-02-26 EP EP20714389.2A patent/EP3930838B1/en active Active
- 2020-02-26 WO PCT/US2020/019786 patent/WO2020176558A1/en not_active Ceased
- 2020-02-26 JP JP2021550155A patent/JP7638880B2/ja active Active
- 2020-02-26 RS RS20241084A patent/RS65998B1/sr unknown
- 2020-02-26 SM SM20240386T patent/SMT202400386T1/it unknown
- 2020-02-26 US US17/434,102 patent/US20220135538A1/en not_active Abandoned
- 2020-02-26 TW TW109106273A patent/TWI850342B/zh active
- 2020-02-26 FI FIEP20714389.2T patent/FI3930838T3/fi active
- 2020-02-26 HU HUE20714389A patent/HUE068415T2/hu unknown
- 2020-02-26 ES ES20714389T patent/ES2989353T3/es active Active
- 2020-02-26 PL PL20714389.2T patent/PL3930838T3/pl unknown
- 2020-02-26 AU AU2020227742A patent/AU2020227742A1/en not_active Abandoned
- 2020-02-26 CN CN202080031338.7A patent/CN113727756B/zh active Active
- 2020-02-26 DK DK20714389.2T patent/DK3930838T3/da active
- 2020-02-26 PT PT207143892T patent/PT3930838T/pt unknown
- 2020-02-26 SI SI202030496T patent/SI3930838T1/sl unknown
- 2020-02-26 LT LTEPPCT/US2020/019786T patent/LT3930838T/lt unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PT3930838T (pt) | 2024-10-04 |
| JP2022522349A (ja) | 2022-04-18 |
| FI3930838T3 (fi) | 2024-10-14 |
| EP3930838A1 (en) | 2022-01-05 |
| HUE068415T2 (hu) | 2024-12-28 |
| LT3930838T (lt) | 2024-09-10 |
| CN113727756A (zh) | 2021-11-30 |
| JP7638880B2 (ja) | 2025-03-04 |
| DK3930838T3 (da) | 2024-10-07 |
| SMT202400386T1 (it) | 2024-11-15 |
| US20220135538A1 (en) | 2022-05-05 |
| EP3930838B1 (en) | 2024-07-10 |
| WO2020176558A1 (en) | 2020-09-03 |
| CA3131383A1 (en) | 2020-09-03 |
| PL3930838T3 (pl) | 2024-12-02 |
| TW202045492A (zh) | 2020-12-16 |
| CN113727756B (zh) | 2024-07-02 |
| TWI850342B (zh) | 2024-08-01 |
| AU2020227742A1 (en) | 2021-09-16 |
| SI3930838T1 (sl) | 2024-10-30 |
| RS65998B1 (sr) | 2024-10-31 |
| ES2989353T3 (es) | 2024-11-26 |
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