HRP20140807T1 - Derivati pirolo[2,3-d]pirimidina kao inhibitori protein kinaze b - Google Patents
Derivati pirolo[2,3-d]pirimidina kao inhibitori protein kinaze b Download PDFInfo
- Publication number
- HRP20140807T1 HRP20140807T1 HRP20140807AT HRP20140807T HRP20140807T1 HR P20140807 T1 HRP20140807 T1 HR P20140807T1 HR P20140807A T HRP20140807A T HR P20140807AT HR P20140807 T HRP20140807 T HR P20140807T HR P20140807 T1 HRP20140807 T1 HR P20140807T1
- Authority
- HR
- Croatia
- Prior art keywords
- cancer
- pharmaceutically acceptable
- acceptable salt
- compound according
- treatment
- Prior art date
Links
- JJTNLWSCFYERCK-UHFFFAOYSA-N 7h-pyrrolo[2,3-d]pyrimidine Chemical class N1=CN=C2NC=CC2=C1 JJTNLWSCFYERCK-UHFFFAOYSA-N 0.000 title 1
- 239000003197 protein kinase B inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 13
- 206010028980 Neoplasm Diseases 0.000 claims 9
- 201000011510 cancer Diseases 0.000 claims 9
- 206010006187 Breast cancer Diseases 0.000 claims 6
- 208000026310 Breast neoplasm Diseases 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 3
- 206010017758 gastric cancer Diseases 0.000 claims 3
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 3
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 3
- 201000002528 pancreatic cancer Diseases 0.000 claims 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 3
- 201000011549 stomach cancer Diseases 0.000 claims 3
- JDUBGYFRJFOXQC-KRWDZBQOSA-N 4-amino-n-[(1s)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide Chemical compound C1([C@H](CCO)NC(=O)C2(CCN(CC2)C=2C=3C=CNC=3N=CN=2)N)=CC=C(Cl)C=C1 JDUBGYFRJFOXQC-KRWDZBQOSA-N 0.000 claims 2
- ZRDYBUCARNESOB-ZDUSSCGKSA-N 4-amino-n-[(1s)-1-(4-chlorophenyl)-3-hydroxypropyl]piperidine-4-carboxamide Chemical compound N([C@@H](CCO)C=1C=CC(Cl)=CC=1)C(=O)C1(N)CCNCC1 ZRDYBUCARNESOB-ZDUSSCGKSA-N 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- JGNACDMQJLVKIU-VIFPVBQESA-N (3s)-3-amino-3-(4-chlorophenyl)propan-1-ol Chemical compound OCC[C@H](N)C1=CC=C(Cl)C=C1 JGNACDMQJLVKIU-VIFPVBQESA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- QIGUQECRLHBCDL-FQEVSTJZSA-N tert-butyl n-[4-[[(1s)-1-(4-chlorophenyl)-3-hydroxypropyl]carbamoyl]-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-yl]carbamate Chemical compound C1([C@H](CCO)NC(=O)C2(CCN(CC2)C=2C=3C=CNC=3N=CN=2)NC(=O)OC(C)(C)C)=CC=C(Cl)C=C1 QIGUQECRLHBCDL-FQEVSTJZSA-N 0.000 claims 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed 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
- A61K31/495—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
-
- 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
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Claims (19)
1. Spoj naznačen time da je: (S)-4-amino-N-(1-(4-klorofenil)-3-hidroksipropil)-1-(7H-pirolo[2,3-d]pirimidin-4-il)piperidin-4-karboksamid:
[image]
ili njegova farmaceutski prihvatljiva sol.
2. Farmaceutski pripravak naznačen time da sadrži spoj prema zahtjevu 1, ili njegovu farmaceutski prihvatljivu sol, zajedno s farmaceutski prihvatljivim razrjeđivačem ili nosačem.
3. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za uporabu kao lijek.
4. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za uporabu za liječenje raka.
5. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za uporabu za liječenje raka, gdje je rak odabran od raka dojke, ne-Hodgkinovog limfoma, raka gušterače, hepatocelularnog karcinoma, raka želuca, raka prostate i raka pluća.
6. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za uporabu za liječenje raka dojke.
7. Uporaba spoja prema zahtjevu 1, ili njegove farmaceutski prihvatljive soli, naznačena time da je za pripravu lijeka za liječenje raka.
8. Uporaba spoja prema zahtjevu 1, ili njegove farmaceutski prihvatljive soli, naznačena time da je za pripravu lijeka za liječenje raka, gdje je rak odabran od raka dojke, ne-Hodgkinovog limfoma, raka gušterače, hepatocelularnog karcinoma, raka želuca, raka prostate i raka pluća.
9. Uporaba spoja prema zahtjevu 1, ili njegove farmaceutski prihvatljive soli, naznačena time da je za pripravu lijeka za liječenje raka dojke.
10. Spoj: (S)-4-amino-N-(1-(4-klorofenil)-3-hidroksipropil)-1-(7H-pirolo[2,3-d]pirimidin-4-il)piperidin-4-karboksamid, kako je zatraženo u zahtjevu 1.
11. Spoj prema zahtjevu 10 naznačen time da je za uporabu kod liječenja raka.
12. Spoj prema zahtjevu 10 naznačen time da je za uporabu kod liječenja raka gdje je rak odabran od raka dojke, ne-Hodgkinovog limfoma, raka gušterače, hepatocelularnog karcinoma, raka želuca, raka prostate i raka pluća.
13. Spoj prema zahtjevu 10 naznačen time da je za uporabu kod liječenja raka dojke.
14. Postupak za pripravu spoja prema zahtjevu 1, ili njegove farmaceutski prihvatljive soli, naznačen time da postupak sadrži reakciju kiseline Formule (II) i (S)-3-amino-3-(4-klorofenil)propan-1-ola:
[image]
pri čemu P1 predstavlja pogodnu zaštitnu skupinu; te nakon toga, ako je potrebno:
uklanjanje zaštitne skupine; i/ili
tvorbu njegove farmaceutski prihvatljive soli.
15. Postupak prema zahtjevu 14, naznačen time da P1 predstavlja tert-butoksikarbonil zaštitnu skupinu.
16. Spoj: (S)-tert-butil4-(1-(4-klorofenil)-3-hidroksipropilkarbamoil)-1-(7H-pirolo[2,3-d]pirimidin-4-il)piperidin-4-ilkarbamat:
[image]
17. Postupak za pripravu spoja prema zahtjevu 1, ili njegove farmaceutski prihvatljive soli, naznačen time da postupak sadrži reakciju (S)-4-amino-N-(1-(4-klorofenil)-3-hidroksipropil)piperidin-4-karboksamida sa bicikličkim heterociklom sa Formulom (V):
[image]
pri čemu L1 predstavlja pogodnu odlazeću skupinu; te nakon toga ako je potrebno, tvorbu njegove farmaceutski prihvatljive soli.
18. Postupak prema zahtjevu 17, naznačen time da L1 je klor.
19. Spoj: (S)-4-amino-N-(1-(4-klorofenil)-3-hidroksipropil)piperidin-4-karboksamid:
[image]
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97919207P | 2007-10-11 | 2007-10-11 | |
| US4786208P | 2008-04-25 | 2008-04-25 | |
| PCT/GB2008/050925 WO2009047563A1 (en) | 2007-10-11 | 2008-10-09 | Pyrrolo [2, 3 -d] pyrimidin derivatives as protein kinase b inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20140807T1 true HRP20140807T1 (hr) | 2014-11-21 |
Family
ID=40251789
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20140807AT HRP20140807T1 (hr) | 2007-10-11 | 2014-08-26 | Derivati pirolo[2,3-d]pirimidina kao inhibitori protein kinaze b |
Country Status (38)
| Country | Link |
|---|---|
| US (8) | US8101623B2 (hr) |
| EP (1) | EP2201012B1 (hr) |
| JP (2) | JP4705695B2 (hr) |
| KR (1) | KR101494734B1 (hr) |
| CN (1) | CN101861321B (hr) |
| AR (1) | AR068846A1 (hr) |
| AU (1) | AU2008309383B2 (hr) |
| BR (1) | BRPI0818533B8 (hr) |
| CA (1) | CA2701057C (hr) |
| CL (1) | CL2008003023A1 (hr) |
| CO (1) | CO6270328A2 (hr) |
| CR (1) | CR11359A (hr) |
| CU (1) | CU23886B1 (hr) |
| CY (1) | CY1116929T1 (hr) |
| DK (1) | DK2201012T3 (hr) |
| DO (1) | DOP2010000103A (hr) |
| EA (1) | EA018512B1 (hr) |
| ES (1) | ES2522365T3 (hr) |
| GT (1) | GT201000082A (hr) |
| HK (1) | HK1143154A1 (hr) |
| HN (1) | HN2010000653A (hr) |
| HR (1) | HRP20140807T1 (hr) |
| IL (1) | IL204721A (hr) |
| ME (1) | ME01999B (hr) |
| MX (1) | MX2010003927A (hr) |
| MY (1) | MY150059A (hr) |
| NI (1) | NI201000050A (hr) |
| NZ (1) | NZ585261A (hr) |
| PE (2) | PE20130152A1 (hr) |
| PL (1) | PL2201012T3 (hr) |
| PT (1) | PT2201012E (hr) |
| RS (1) | RS53552B1 (hr) |
| SA (1) | SA08290625B1 (hr) |
| SI (1) | SI2201012T1 (hr) |
| TW (1) | TWI453021B (hr) |
| UY (1) | UY31384A1 (hr) |
| WO (1) | WO2009047563A1 (hr) |
| ZA (1) | ZA201002318B (hr) |
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| JP6100700B2 (ja) | 2011-01-11 | 2017-03-22 | ノバルティス アーゲー | 組合せ |
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| PL2785349T5 (pl) * | 2011-11-30 | 2023-01-30 | Astrazeneca Ab | Kombinacja do leczenia nowotworu |
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| EP2815749A1 (en) | 2013-06-20 | 2014-12-24 | IP Gesellschaft für Management mbH | Solid form of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione having specified X-ray diffraction pattern |
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| US9695168B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors |
| US9695167B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors |
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| JP7427363B2 (ja) | 2015-08-12 | 2024-02-05 | インサイト・ホールディングス・コーポレイション | Ｌｓｄ１阻害剤の塩 |
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