HRP20231369T1 - Inhibitori lsd1 i njihova medicinska upotreba - Google Patents
Inhibitori lsd1 i njihova medicinska upotreba Download PDFInfo
- Publication number
- HRP20231369T1 HRP20231369T1 HRP20231369TT HRP20231369T HRP20231369T1 HR P20231369 T1 HRP20231369 T1 HR P20231369T1 HR P20231369T T HRP20231369T T HR P20231369TT HR P20231369 T HRP20231369 T HR P20231369T HR P20231369 T1 HRP20231369 T1 HR P20231369T1
- Authority
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- Croatia
- Prior art keywords
- image
- alkyl
- pharmaceutically acceptable
- acceptable salt
- compound
- Prior art date
Links
- 229940123628 Lysine (K)-specific demethylase 1A inhibitor Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 13
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000001475 halogen functional group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 229910006074 SO2NH2 Inorganic materials 0.000 claims 2
- 208000029052 T-cell acute lymphoblastic leukemia Diseases 0.000 claims 2
- 201000011176 T-cell adult acute lymphocytic leukemia Diseases 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 claims 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- ROSDSFDQCJNGOL-UHFFFAOYSA-N Dimethylamine Chemical compound CNC ROSDSFDQCJNGOL-UHFFFAOYSA-N 0.000 claims 1
- 208000031886 HIV Infections Diseases 0.000 claims 1
- 208000037357 HIV infectious disease Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 241000700584 Simplexvirus Species 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 230000007419 viral reactivation Effects 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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/12—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring 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
- A61K31/435—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
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
-
- 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
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/20—Spiro-condensed ring systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (12)
1. Spoj formule:
[image]
pri čemu je stereokemijska konfiguracija oko ciklopropilnog prstena 1R,2S,
ili njegova farmaceutski prihvatljiva sol, naznačen time što
n je 1 ili 2;
m je 1 ili 2;
o je o ili 1;
q je o, 1, 2, ili 3;
R1 je vodik ili (C1-C6)alkil;
R2 je vodik ili (C1-C6)alkil izborno supstituiran s OH ili (C1-C6)alkoksi;
R3 i R4, ako su prisutni, svaki je neovisno odabran od vodika, halo, OH, i (C1-C6)alkila;
R5 je odabran od NH2, -NH(SO2)(C1-C6)alkil, -NH(SO2)(C1-C6)alkilO(C1-C6)alkil, -NHC(O)(C1-C6)alkil, -NH(SO2)(C3-C6)cikloalkil, OH, -O(C1-C6)alkil, - SO2NH2, -C(O)NH2, -C(O)NH(C1-C6)alkil, -C(O)N[(C1-C6)alkil]2, -C(O)NH(SO2)(C1-C6)alkil, -C(O)NH(C1-C6)alkil(SO2)(C1-C6)alkil, -C(O)NH(SO2)(C3-C6)cikloalkil, - C(O)NH(C1-C6)alkilOH, -C(O)NH(C1-C6)alkilO(C1-C6)alkil, i (C1-C4)alkil supstituiran s OH; i
R6, ako je prisutan, odabran je od (C1-C6)alkil, halo(C1-C6)alkil, (C1-C6)alkoksi, halo(C1-C6)alkoksi, halo, i cijano;
pod uvjetom da spoj nema formulu:
[image]
ili njegova sol.
2. Spoj prema zahtjevu 1, naznačen time što je spoj formule:
[image]
ili njegova farmaceutski prihvatljiva sol.
3. Spoj prema bilo kojem zahtjevu 1, naznačen time što spoj ima formulu:
[image]
ili njegova farmaceutski prihvatljiva sol.
4. Spoj prema bilo kojem od zahtjeva 1 do 3 ili njegova farmaceutski prihvatljiva sol, naznačen time što R2 je vodik, metil, ili hidroksi(C1-C4)alkil.
5. Spoj prema zahtjevu 1, naznačen time što spoj ima formulu:
[image]
ili njegova farmaceutski prihvatljiva sol.
6. Spoj prema bilo kojem od zahtjeva 1 do 5 ili njegova farmaceutski prihvatljiva sol, naznačen time što R5 je NH2, -NH(SO2)(C1-C4)alkil, -NH(SO2)(C1-C4)alkilO(C1-C4)alkil, - NHC(O)(C1-C4)alkil, -NH(SO2)(C3-C6)cikloalkil, OH, -SO2NH2, -C(O)NH2, - C(O)NH(C1-C4)alkil, -C(O)NH(SO2)(C1-C4)alkil, -C(O)NH(C1-C4)alkil(SO2)(C1-C4)alkil, -C(O)NH(C1-C4)alkilOH, ili (C1-C2)alkil supstituiran sa OH.
7. Spoj prema bilo kojem od zahtjeva 1 do 6 ili njegova farmaceutski prihvatljiva sol, naznačen time što R5 je -NH(SO2)CH3, -NH(SO2)(CH2)2OCH3, -NH(SO2)CH(CH3)2, -NH(SO2)CH2CH3, - NHC(O)CH3, -NH(SO2)ciklopropil,-C(O)NH(SO2)CH3, - C(O)NH(CH3)2, -C(O)NHCH(CH3)2, -C(O)NHCH2CH3, -C(O)NH(CH2)2(SO2)CH3, - C(O)NH(CH2)2OH, ili -CH2OH.
8. Spoj prema zahtjevu 1, naznačen time što je spoj formule odabran od
[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]
[image]
[image]
i
[image]
ili njihova farmaceutski prihvatljiva sol.
9. Spoj prema zahtjevu 1, naznačen time što spoj ima formulu
[image]
ili njegova farmaceutski prihvatljiva sol.
10. Spoj prema zahtjevu 1, naznačen time što spoj ima formulu
[image]
ili njegova farmaceutski prihvatljiva sol.
11. Farmaceutski pripravak, naznačen time što sadrži učinkovitu količinu spoja prema bilo kojem od zahtjeva 1 do 10, ili njegovu farmaceutski prihvatljivu sol; i farmaceutski prihvatljiv nosač.
12. Spoj prema bilo kojem od zahtjeva 1 do 10, ili njegova farmaceutski prihvatljiva sol, ili pripravak prema zahtjevu 11 za upotrebu u liječenju bolesti ili stanja odabranog između CML (kronična mijeloična leukemija), T-ALL (T akutna limfoblastična leukemija), neuroblastoma, raka dojke, raka prostate, reaktivacije virusa herpes simplex i HIV infekcije.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662413162P | 2016-10-26 | 2016-10-26 | |
US201662413166P | 2016-10-26 | 2016-10-26 | |
PCT/US2017/058405 WO2018081343A1 (en) | 2016-10-26 | 2017-10-26 | Lsd1 inhibitors and medical uses thereof |
EP17797805.3A EP3532459B1 (en) | 2016-10-26 | 2017-10-26 | Lsd1 inhibitors and medical uses thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20231369T1 true HRP20231369T1 (hr) | 2024-02-16 |
Family
ID=60320993
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20231369TT HRP20231369T1 (hr) | 2016-10-26 | 2017-10-26 | Inhibitori lsd1 i njihova medicinska upotreba |
Country Status (17)
Country | Link |
---|---|
US (3) | US10517849B2 (hr) |
EP (1) | EP3532459B1 (hr) |
JP (1) | JP7142633B2 (hr) |
CN (1) | CN109863137B (hr) |
AU (1) | AU2017348100B2 (hr) |
CA (1) | CA3039793A1 (hr) |
DK (1) | DK3532459T3 (hr) |
ES (1) | ES2961499T3 (hr) |
FI (1) | FI3532459T3 (hr) |
HR (1) | HRP20231369T1 (hr) |
HU (1) | HUE063848T2 (hr) |
LT (1) | LT3532459T (hr) |
PT (1) | PT3532459T (hr) |
RS (1) | RS64889B1 (hr) |
SI (1) | SI3532459T1 (hr) |
TW (1) | TWI753037B (hr) |
WO (1) | WO2018081343A1 (hr) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FI3532459T3 (fi) | 2016-10-26 | 2023-10-23 | Constellation Pharmaceuticals Inc | Lsd1-estäjiä ja niiden lääkinnällisiä käyttöjä |
WO2019025588A1 (en) | 2017-08-03 | 2019-02-07 | Oryzon Genomics, S.A. | METHODS OF TREATING ALTERATIONS IN BEHAVIOR |
WO2020052649A1 (zh) | 2018-09-13 | 2020-03-19 | 南京明德新药研发有限公司 | 作为lsd1抑制剂的环丙胺类化合物及其应用 |
EP3941465A1 (en) | 2019-03-20 | 2022-01-26 | Oryzon Genomics, S.A. | Methods of treating attention deficit hyperactivity disorder using kdm1a inhibitors such as the compound vafidemstat |
AU2020242302A1 (en) | 2019-03-20 | 2021-09-16 | Oryzon Genomics, S.A. | Methods of treating borderline personality disorder |
CN114341366A (zh) | 2019-07-05 | 2022-04-12 | 奥莱松基因组股份有限公司 | 用于使用kdm1a抑制剂个体化治疗小细胞肺癌的生物标志物和方法 |
AU2022254484A1 (en) | 2021-04-08 | 2023-11-09 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors for treating myeloid cancers |
WO2023217784A1 (en) | 2022-05-09 | 2023-11-16 | Oryzon Genomics, S.A. | Methods of treating nf1-mutant tumors using lsd1 inhibitors |
WO2023217758A1 (en) | 2022-05-09 | 2023-11-16 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
WO2024110649A1 (en) | 2022-11-24 | 2024-05-30 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors and menin inhibitors for treating cancer |
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2017
- 2017-10-26 FI FIEP17797805.3T patent/FI3532459T3/fi active
- 2017-10-26 WO PCT/US2017/058405 patent/WO2018081343A1/en active Application Filing
- 2017-10-26 ES ES17797805T patent/ES2961499T3/es active Active
- 2017-10-26 HU HUE17797805A patent/HUE063848T2/hu unknown
- 2017-10-26 US US16/345,011 patent/US10517849B2/en active Active
- 2017-10-26 RS RS20231023A patent/RS64889B1/sr unknown
- 2017-10-26 SI SI201731432T patent/SI3532459T1/sl unknown
- 2017-10-26 EP EP17797805.3A patent/EP3532459B1/en active Active
- 2017-10-26 CN CN201780065306.7A patent/CN109863137B/zh active Active
- 2017-10-26 CA CA3039793A patent/CA3039793A1/en active Pending
- 2017-10-26 TW TW106136856A patent/TWI753037B/zh active
- 2017-10-26 JP JP2019522808A patent/JP7142633B2/ja active Active
- 2017-10-26 HR HRP20231369TT patent/HRP20231369T1/hr unknown
- 2017-10-26 DK DK17797805.3T patent/DK3532459T3/da active
- 2017-10-26 LT LTEPPCT/US2017/058405T patent/LT3532459T/lt unknown
- 2017-10-26 AU AU2017348100A patent/AU2017348100B2/en active Active
- 2017-10-26 PT PT177978053T patent/PT3532459T/pt unknown
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PT3532459T (pt) | 2023-11-10 |
CN109863137B (zh) | 2022-12-16 |
CA3039793A1 (en) | 2018-05-03 |
TW201821406A (zh) | 2018-06-16 |
RS64889B1 (sr) | 2023-12-29 |
AU2017348100B2 (en) | 2021-08-26 |
LT3532459T (lt) | 2023-11-10 |
WO2018081343A1 (en) | 2018-05-03 |
ES2961499T3 (es) | 2024-03-12 |
DK3532459T3 (da) | 2023-10-30 |
TWI753037B (zh) | 2022-01-21 |
CN109863137A (zh) | 2019-06-07 |
FI3532459T3 (fi) | 2023-10-23 |
US20220079917A1 (en) | 2022-03-17 |
US20190274998A1 (en) | 2019-09-12 |
US11013718B2 (en) | 2021-05-25 |
JP7142633B2 (ja) | 2022-09-27 |
HUE063848T2 (hu) | 2024-02-28 |
EP3532459A1 (en) | 2019-09-04 |
JP2019537584A (ja) | 2019-12-26 |
US11547695B2 (en) | 2023-01-10 |
US10517849B2 (en) | 2019-12-31 |
AU2017348100A1 (en) | 2019-05-02 |
SI3532459T1 (sl) | 2024-03-29 |
EP3532459B1 (en) | 2023-08-02 |
US20200306223A1 (en) | 2020-10-01 |
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