HRP20170288T1 - DERIVATI PIRIMIDOOKSAZOCINA KAO INHIBITORI mTOR - Google Patents
DERIVATI PIRIMIDOOKSAZOCINA KAO INHIBITORI mTOR Download PDFInfo
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- HRP20170288T1 HRP20170288T1 HRP20170288TT HRP20170288T HRP20170288T1 HR P20170288 T1 HRP20170288 T1 HR P20170288T1 HR P20170288T T HRP20170288T T HR P20170288TT HR P20170288 T HRP20170288 T HR P20170288T HR P20170288 T1 HRP20170288 T1 HR P20170288T1
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- ZHKMLTCNJQHQMU-UHFFFAOYSA-N 2H-pyrimido[4,5-g]oxazocine Chemical class O1NC=CC=CC2=C1C=NC=N2 ZHKMLTCNJQHQMU-UHFFFAOYSA-N 0.000 title 1
- 229940124302 mTOR inhibitor Drugs 0.000 title 1
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 26
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 6
- 239000002253 acid Substances 0.000 claims 5
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010053185 Glycogen storage disease type II Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000030852 Parasitic disease Diseases 0.000 claims 1
- 238000006069 Suzuki reaction reaction Methods 0.000 claims 1
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 1
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 1
- 230000032683 aging Effects 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 201000004502 glycogen storage disease II Diseases 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 208000026278 immune system disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000000269 nucleophilic effect Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 210000002345 respiratory system Anatomy 0.000 claims 1
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
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- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
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- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
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- A—HUMAN NECESSITIES
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- A61P35/00—Antineoplastic agents
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
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- 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
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (16)
1. Spoj prema formuli (I):
[image]
naznačen time da:
- svaki od radikala R1 neovisno predstavlja skupinu (C1-C6)-alkil, gdje se podrazumijeva da dvije skupine R1 koje nose dva različita atoma ugljika iz morfolinil prstena mogu biti spojene zajedno tako da s morfolinil prstenom, tvore bicikličku heterocikličku strukturu,
- R2 i R3 neovisno predstavljaju:
- H, ili
- skupinu (C1-C6) alkil,
- R4 predstavlja:
- H,
- skupinu (C1-C6)-alkil, proizvoljno supstituiranu sa hidroksilnom skupinom,
- skupinu (C1-C6)-alkoksi,
- skupinu -L1-R10, u kojoj:
- L1 predstavlja skupinu (C1-C6)-alkilen,
- R10 predstavlja skupinu odabranu od -COOR11, -CO-R12, -OR13, -CONR14R15 i heterocikal s 5- ili 6-atoma proizvoljno supstituiran sa skupinom -R16, -COOR17, -CO-R18, -OR19 ili -NR20R21, ili
- heterocikal s 5- ili 6-atoma proizvoljno supstituiran sa skupinom -R22, -COOR23, -CO-R24, -OR25 ili -CONR26R27,
- G1 predstavlja dvovalentni fenil ili heteroarilni radikal s 5- do 6-atoma, proizvoljno supstituiran s 1 do 4 skupina R5 neovisno odabranih od halogenog atoma, skupine -OR30 i skupine -(C1-C6)-alkil proizvoljno supstituirane s hidroksilom,
- X1 predstavlja skupinu -O- ili -NR40-,
- X2 predstavlja jednostruku vezu ili skupinu -CONR50-, -CONR51-O-, -COO-, -CO- ili -SO2-,
- R6 predstavlja:
- H,
- skupinu -L2-R7, u kojoj:
- -L2- predstavlja skupinu (C1-C6)-alkilen ili (C3-C6)-cikloalkilen,
- R7 predstavlja skupinu odabranu od:
- H,
- OR60,
- atoma halogena,
- skupine (C1-C6)-haloalkil,
- heterocikla s 5- do 6-atoma proizvoljno supstituiranog s jednom ili više skupina koje su odabrane od skupine (C1-C6)-alkil, skupine (C1-C6)-alkoksi i skupine =O, ili
- skupine -G2-X3-G3, u kojoj:
- X3 predstavlja jednostruku vezu ili skupinu -O-, -CO- ili -CH2-,
- G2 predstavlja jednostruku vezu ili dvovalentni ciklički radikal s 5- do 6-atoma proizvoljno supstituiran s jednom ili više skupina R80,
- G3 predstavlja prsten s 4- do 8-atoma proizvoljno supstituiran s jednom ili više skupina R81,
- ili -G2-X3-G3 zajedno tvore kondenziranu bicikličku skupinu s 7- do 10-atoma,
- svaki radikal R80 i svaki radikal R81 je neovisno odabran od:
- atoma halogena,
- skupine -COOR70, -CO-R71, -OR72, -NR73R74, -CONR75R76, -CN ili -S(O)p-R77,
- skupine (C1-C6)-alkil proizvoljno supstituirane s jednom ili više skupina R100 i/ili proizvoljno prekinute s jednim ili više kisikovih atoma,
- skupinu (C1-C6)-alkoksi proizvoljno supstituiranu s jednom ili više skupina R101 i/ili proizvoljno prekinute s jednim ili više kisikovih atoma,
- n predstavlja 0, 1 ili 2,
- m predstavlja 0 ili 1,
- p predstavlja 0, 1 ili 2,
- R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, R30, R40, R50, R51, R60, R70, R71, R72, R73, R74, R75, R76 i R77 neovisno predstavljaju H ili skupinu (C1-C6)-alkil proizvoljno supstituiranu sa skupinom R90 i/ili proizvoljno prekinute s jednim ili više kisikovih atoma,
- R90 predstavlja skupinu -OR91 ili -NR92R93,
- R91, R92 i R93 neovisno predstavljaju H ili skupinu (C1-C6)-alkil,
- R100 i R101 su neovisno odabrani od halogenog atoma i hidroksila u obliku baze ili u obliku kisele adicijske soli.
2. Spoj prema zahtjevu 1 prema formuli (II) odabran od:
[image]
naznačen time da su n, R1, R4, G1, X1, X2 i R6 kako je definirano u zahtjevu 1,
u obliku baze ili u obliku kisele adicijske soli.
3. Spoj prema zahtjevu 1 ili 2, naznačen time da R4 predstavlja:
- H,
- skupinu (C1-C6)-alkil, proizvoljno supstituiranu s hidroksilnom skupinom,
- skupinu -L1-R10, u kojoj:
- L1 predstavlja skupinu (C1-C6)-alkilen,
- R10 predstavlja skupinu odabranu od -COOR11, -OR13, -CONR14R15 i heterocikal s 5- ili 6-atoma proizvoljno supstituiran sa skupinom -COOR17 ili -CO-R18, ili
- heterocikal s 5- ili 6-atoma proizvoljno supstituiran sa skupinom -R22,
- R11, R13, R14, R15, R17, R18 i R22 su kako je definirano u zahtjevu 1.
4. Spoj prema bilo kojem od zahtjeva 1 do 3, naznačen time da G1 predstavlja dvovalentan fenilni ili piridil radikal proizvoljno supstituiran sa skupinom R5 odabranom od halogenih atoma.
5. Spoj prema bilo kojem od zahtjeva 1 do 4, naznačen time da X1 predstavlja skupinu -NR40-, u kojoj R40 je kako je definirano u zahtjevu 1.
6. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time da X2 predstavlja -CONR50- ili -COO-.
7. Spoj prema bilo kojem od zahtjeva 1 do 6, prema formuli (III) ispod:
[image]
naznačen time da:
- R4 predstavlja skupinu (C1-C6)-alkil,
- R'5 i R"5 predstavljaju -H ili -F, pri čemu se podrazumijeva da kada jedan od radikala R'5 i R"5 predstavlja -F, tada drugi predstavlja -H,
- X2 predstavlja -CONR50- ili -COO-,
- R6 predstavlja:
- skupinu -L2-R7, u kojoj:
- -L2- predstavlja skupinu (C1-C6)-alkilen ili (C3-C6)-cikloalkilen,
- R7 predstavlja skupinu odabranu od:
- H, ili
- OR60,
- skupinu -G2-X3-G3, u kojoj:
- X3 predstavlja jednostruku vezu ili skupinu -O-,
- G2 predstavlja jednostruku vezu ciklički dvovalentan radikal s 6 atoma,
- G3 predstavlja prsten s 4- do 8-atoma proizvoljno supstituiran sa jednom ili više skupina R81,
- n, R1, R50, R60 i R81 su kako je definirano u zahtjevu 1,
u obliku baze ili u obliku kisele adicijske soli.
8. Spoj prema bilo kojem od zahtjeva 1 do 7, naznačen time da R4 predstavlja metilnu skupinu ili etilnu skupinu.
9. Spoj prema zahtjevu 7 ili 8, naznačen time da je odabran od slijedećih spojeva:
[image]
[image]
[image]
[image]
u obliku baze ili u obliku kisele adicijske soli.
10. Postupak za pripremanje spoja s formulom (I) prema bilo kojem od zahtjeva 1 do 9, naznačen time da sadrži korak m) ispod:
m) cijepljenje skupine -X2-R6 na spoj s formulom (XLII) ispod:
[image]
u kojoj R1, n, m, R2, R3, R4, G1 i X1 su kako je definirano u zahtjevu 1,
da se dobije spoj s formulom (I).
11. Postupak za pripremanje spoja s formulom (I) prema bilo kojem od zahtjeva 1 do 9, u kojoj X1 predstavlja -NR40- i X2 predstavlja -CONR50-, naznačen time da sadrži korak ispod:
n) Suzukijevu reakciju spoja s formulom (XXXV):
[image]
u kojoj n, R1, m, R2, R3 i R4 su kako je definirano u zahtjevu 1 i LG5 je odlazeća skupina, sa spojem s formulom R6R50N-(C=O)-NR40-G1-R300, u kojoj su G1, R6, R50 i R40 kako je definirano u zahtjevu 1 i R300 je boronična kiselina ili radikal estera,
da se dobije spoj s formulom (I) u kojoj X1 predstavlja -NR40- i X2 predstavlja -CONR50-.
12. Postupak za pripremanje spoja s formulom (I) prema bilo kojem od zahtjeva 1 do 9, naznačen time da sadrži korak q) ispod:
q) nukleofilni napad spoja s formulom (CI) ispod:
[image]
u kojoj n i R1 su kako je definirano u zahtjevu 1,
na spoju s formulom (LII) ispod:
[image]
u kojoj su m, R2, R3, R4, G1, X1, X2 i R6 kako je definirano u zahtjevu 1,
da se dobije spoj s formulom (I).
13. Lijek, naznačen time da sadrži spoj prema bilo kojem od zahtjeva 1 do 9 ili farmaceutski prihvatljivu kiselu adicijsku sol navedenog spoja.
14. Farmaceutski pripravak, naznačen time da sadrži spoj prema bilo kojem od zahtjeva 1 do 9, farmaceutski prihvatljivu sol navedenog spoja, te također barem jedno farmaceutski prihvatljivo pomoćno sredstvo.
15. Spoj s formulom (I) prema bilo kojem od zahtjeva 1 do 9, naznačen time da je za uporabu za liječenje ili prevenciju patološkog stanja koje zahtijeva inhibiciju kinaze mTOR.
16. Spoj s formulom (I) prema zahtjevu 15, naznačen time da je za uporabu za liječenje ili sprječavanje karcinoma, upalnih i imunoloških bolesti, dijabetesa, pretilosti, opstruktivnih bolesti dišnih puteva, fibroze, Pompeove bolesti, kardiovaskularnih bolesti, bolesti povezanih sa starenjem, epilepsija ili parazitskih bolesti.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR1250768A FR2986232B1 (fr) | 2012-01-26 | 2012-01-26 | Derives heterocycliques bicycliques, leur preparation et leur application en therapeutique |
| EP13712331.1A EP2807172B1 (en) | 2012-01-26 | 2013-01-25 | Pyrimidooxazocine derivatives as mtor-inhibitors |
| PCT/IB2013/050656 WO2013111106A1 (en) | 2012-01-26 | 2013-01-25 | Pyrimidooxazocine derivatives as mtor - inhibitors |
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| Publication Number | Publication Date |
|---|---|
| HRP20170288T1 true HRP20170288T1 (hr) | 2017-04-21 |
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| HRP20170288TT HRP20170288T1 (hr) | 2012-01-26 | 2017-02-21 | DERIVATI PIRIMIDOOKSAZOCINA KAO INHIBITORI mTOR |
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| US (1) | US9120812B2 (hr) |
| EP (1) | EP2807172B1 (hr) |
| JP (1) | JP6068508B2 (hr) |
| KR (1) | KR20140125389A (hr) |
| CN (1) | CN104203958B (hr) |
| AR (1) | AR089782A1 (hr) |
| AU (1) | AU2013213261B2 (hr) |
| BR (1) | BR112014018226A8 (hr) |
| CA (1) | CA2862747A1 (hr) |
| CY (1) | CY1118852T1 (hr) |
| DK (1) | DK2807172T3 (hr) |
| ES (1) | ES2617880T3 (hr) |
| FR (1) | FR2986232B1 (hr) |
| HR (1) | HRP20170288T1 (hr) |
| HU (1) | HUE031917T2 (hr) |
| IL (1) | IL233774A (hr) |
| LT (1) | LT2807172T (hr) |
| MX (1) | MX348841B (hr) |
| PL (1) | PL2807172T3 (hr) |
| PT (1) | PT2807172T (hr) |
| RU (1) | RU2627269C2 (hr) |
| SG (1) | SG11201404325VA (hr) |
| SI (1) | SI2807172T1 (hr) |
| TW (1) | TWI572608B (hr) |
| UY (1) | UY34594A (hr) |
| WO (1) | WO2013111106A1 (hr) |
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| MX2016004964A (es) * | 2013-10-16 | 2016-07-11 | Shanghai Yingli Pharm Co Ltd | Compuesto heterociclico fusionado, metodo de preparacion del mismo, composicion farmaceutica, y usos del mismo. |
| WO2016050201A1 (zh) * | 2014-09-29 | 2016-04-07 | 山东轩竹医药科技有限公司 | 高选择性取代嘧啶类pi3k抑制剂 |
| US10307707B2 (en) * | 2017-05-17 | 2019-06-04 | Thomas P. Daly | 1-amino-2-methyl-2-propanol derivatives |
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| MXPA04006571A (es) * | 2002-01-18 | 2004-10-04 | Kyorin Seiyaku Kk | Derivado de pirimidina biciclica fusionada. |
| AU2003293006A1 (en) * | 2002-11-22 | 2004-06-18 | Japan Tobacco Inc. | Fused bicyclic nitrogen-containing heterocycles |
| AU2009314544C1 (en) * | 2008-11-11 | 2015-11-12 | Xcovery Holding Company Llc | PI3K/mTOR kinase inhibitors |
| US8637499B2 (en) * | 2009-05-26 | 2014-01-28 | Exelixis, Inc. | Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture |
| JP2013529212A (ja) * | 2010-05-19 | 2013-07-18 | エクスカバリー ホールディング カンパニー，エルエルシー | ｍＴＯＲ選択的キナーゼ阻害剤 |
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