PL411864A1 - Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy P13 - Google Patents
Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy P13Info
- Publication number
- PL411864A1 PL411864A1 PL411864A PL41186415A PL411864A1 PL 411864 A1 PL411864 A1 PL 411864A1 PL 411864 A PL411864 A PL 411864A PL 41186415 A PL41186415 A PL 41186415A PL 411864 A1 PL411864 A1 PL 411864A1
- Authority
- PL
- Poland
- Prior art keywords
- compound
- pyrazolo
- morpholin
- pyrimidine
- kinase
- Prior art date
Links
- 108091000080 Phosphotransferase Proteins 0.000 title abstract 2
- 102000020233 phosphotransferase Human genes 0.000 title abstract 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 abstract 1
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical group F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 abstract 1
- 108010081348 HRT1 protein Hairy Chemical group 0.000 abstract 1
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000001708 Protein Isoforms Human genes 0.000 abstract 1
- 108010029485 Protein Isoforms Proteins 0.000 abstract 1
- 229940124639 Selective inhibitor Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 208000026278 immune system disease Diseases 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- 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
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Ujawniono związek o wzorze ogólnym (I), w którym Y oznacza -CH2- lub >C=O; R1 oznacza grupę wybraną z grup A1, A2 i A3 zdefiniowanych w opisie; R2 oznacza grupę wybraną z grup B1, B2, B3 i B4 zdefiniowanych w opisie; R3 oznacza H, halogen, lub C1-C4 alkil; R4 oznacza C1-C4 alkil, C3-C4-cykloalkil, C1-C4 alkil podstawiony przez C1-C4 alkoksyl, lub CHF2; jego dopuszczalne farmaceutycznie sole, oraz kompozycja farmaceutyczna zawierająca związek o wzorze (I). Związek jest selektywnym inhibitorem izoformy delta kinazy PI3 i znajduje zastosowanie jako lek w leczeniu chorób układu immunologicznego, chorób o podłożu zapalnym i nowotworów.
Priority Applications (19)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PL411864A PL236355B1 (pl) | 2015-04-02 | 2015-04-02 | Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3 |
| PCT/IB2016/051792 WO2016157091A1 (en) | 2015-04-02 | 2016-03-30 | 7-(morpholin-4-yl)pyrazole[1,5-a]pyrimidine derivatives which are useful for the treatment of immune or inflammatory diseases or cancer |
| HRP20192195TT HRP20192195T1 (hr) | 2015-04-02 | 2016-03-30 | Derivati 7-(morfolin-4-il)pirazol[1,5-a]pirimidina koji su korisni za liječenje imunoloških ili upalnih oboljenja ili karcinoma |
| DK16714019.3T DK3277687T3 (da) | 2015-04-02 | 2016-03-30 | 7-(Morpholin-4-yl)pyrazol[1,5-a]pyrimidinderivater, som kan anvendes til behandling af immunsygdomme eller inflammatoriske sygdomme eller cancer |
| ES16714019T ES2765642T3 (es) | 2015-04-02 | 2016-03-30 | Derivados de 7-(morfolin-4-il)pirazol[1,5-a]pirimidina que son útiles para el tratamiento de enfermedades inmunitarias o inflamatorias o cáncer |
| PT167140193T PT3277687T (pt) | 2015-04-02 | 2016-03-30 | Derivados de 7-(morfolin-4-il)pirazole[1,5-a]pirimidina que são úteis para o tratamento de doenças imunitárias ou inflamatórias ou cancro |
| EA201792087A EA032826B1 (ru) | 2015-04-02 | 2016-03-30 | ПРОИЗВОДНЫЕ 7-(МОРФОЛИН-4-ИЛ)ПИРАЗОЛО[1,5-a]ПИРИМИДИНА, ПРИГОДНЫЕ ДЛЯ ЛЕЧЕНИЯ ИММУННЫХ ИЛИ ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙ ИЛИ РАКА |
| HUE16714019A HUE047822T2 (hu) | 2015-04-02 | 2016-03-30 | Immun- vagy gyulladásos betegségek és rák kezelésére alkalmas 7-(morfolin-4-il)pirazol[1,5-a]pirimidin-származékok |
| EP16714019.3A EP3277687B1 (en) | 2015-04-02 | 2016-03-30 | 7-(morpholin-4-yl)pyrazole[1,5-a]pyrimidine derivatives which are useful for the treatment of immune or inflammatory diseases or cancer |
| KR1020177031214A KR102559190B1 (ko) | 2015-04-02 | 2016-03-30 | 면역성 또는 염증성 질환 또는 암의 치료를 위해 유용한 7-(모르폴린-4-일)피라졸[1,5-a]피리미딘 유도체 |
| CN201680017259.4A CN107743489B (zh) | 2015-04-02 | 2016-03-30 | 治疗免疫疾病、炎性疾病或癌症的7-(吗啉-4-基)吡唑并[1,5-a]嘧啶衍生物 |
| SI201630560T SI3277687T1 (sl) | 2015-04-02 | 2016-03-30 | 7-(morfolin-4-IL)pirazol(1,5-A)pirimidinski derivati, ki so uporabni za zdravljenje imunskih ali vnetnih bolezni ali raka |
| US15/562,537 US10138247B2 (en) | 2015-04-02 | 2016-03-30 | 7-(morpholin-4-yl)pyrazole[1,5-A]pyrimidine derivatives as PI3 kinase inhibitors |
| JP2017551627A JP6665201B2 (ja) | 2015-04-02 | 2016-03-30 | 免疫もしくは炎症性の疾患またはがんの処置に有用な7−(モルホリン−4−イル)ピラゾール[1,5−a]ピリミジン誘導体 |
| CA2978828A CA2978828A1 (en) | 2015-04-02 | 2016-03-30 | 7-(morpholin-4-yl)pyrazole[1,5-a]pyrimidine derivatives which are useful for the treatment of immune or inflammatory diseases or cancer |
| AU2016241568A AU2016241568B2 (en) | 2015-04-02 | 2016-03-30 | 7-(morpholin-4-yl)pyrazole[1,5-a]pyrimidine derivatives which are useful for the treatment of immune or inflammatory diseases or cancer |
| MX2017011423A MX2017011423A (es) | 2015-04-02 | 2016-03-30 | Derivados de 7-(morfolin-4-il)pirazolo[1,5-a]pirimidina que son utiles para el tratamiento de enfermedades inmunes o inflamatorias o cancer. |
| BR112017020131-3A BR112017020131B1 (pt) | 2015-04-02 | 2016-03-30 | Composto, seu uso e composição farmacêutica |
| PL16714019T PL3277687T3 (pl) | 2015-04-02 | 2016-03-30 | Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-a]pirymidyny użyteczne do leczenia chorób immunologicznych lub zapalnych lub nowotworów |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PL411864A PL236355B1 (pl) | 2015-04-02 | 2015-04-02 | Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| PL411864A1 true PL411864A1 (pl) | 2016-10-10 |
| PL236355B1 PL236355B1 (pl) | 2021-01-11 |
Family
ID=55650626
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PL411864A PL236355B1 (pl) | 2015-04-02 | 2015-04-02 | Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3 |
| PL16714019T PL3277687T3 (pl) | 2015-04-02 | 2016-03-30 | Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-a]pirymidyny użyteczne do leczenia chorób immunologicznych lub zapalnych lub nowotworów |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PL16714019T PL3277687T3 (pl) | 2015-04-02 | 2016-03-30 | Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-a]pirymidyny użyteczne do leczenia chorób immunologicznych lub zapalnych lub nowotworów |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US10138247B2 (pl) |
| EP (1) | EP3277687B1 (pl) |
| JP (1) | JP6665201B2 (pl) |
| KR (1) | KR102559190B1 (pl) |
| CN (1) | CN107743489B (pl) |
| AU (1) | AU2016241568B2 (pl) |
| BR (1) | BR112017020131B1 (pl) |
| CA (1) | CA2978828A1 (pl) |
| DK (1) | DK3277687T3 (pl) |
| EA (1) | EA032826B1 (pl) |
| ES (1) | ES2765642T3 (pl) |
| HR (1) | HRP20192195T1 (pl) |
| HU (1) | HUE047822T2 (pl) |
| MX (1) | MX2017011423A (pl) |
| PL (2) | PL236355B1 (pl) |
| PT (1) | PT3277687T (pl) |
| SI (1) | SI3277687T1 (pl) |
| WO (1) | WO2016157091A1 (pl) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3167339A1 (en) | 2020-01-13 | 2021-07-22 | Verge Analytics, Inc. | Substituted pyrazolo-pyrimidines and uses thereof |
| TWI908894B (zh) * | 2020-09-28 | 2025-12-21 | 南韓商福斯特生物股份有限公司 | 作為造血前驅細胞激酶1(hpk1)抑制劑的吲唑及其用途 |
| EP4229063A4 (en) * | 2020-10-19 | 2024-12-25 | TME Therapeutics LLC | NOVEL PIKFYVE INHIBITORS AND METHODS OF USE THEREOF |
| CN114957261B (zh) * | 2022-05-17 | 2023-06-23 | 重庆文理学院 | 一种具有抗头颈癌作用的化合物及其制备方法和应用 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997029109A1 (en) * | 1996-02-07 | 1997-08-14 | Janssen Pharmaceutica N.V. | Pyrazolopyrimidines as crf receptor antagonists |
| WO2005062882A2 (en) | 2003-12-23 | 2005-07-14 | Activbiotics, Inc | Rifamycin analogs and uses thereof |
| CN101115755B (zh) * | 2005-02-11 | 2013-01-16 | 弗·哈夫曼-拉罗切有限公司 | 作为mglur2拮抗剂的吡唑并-嘧啶衍生物 |
| UA96458C2 (ru) * | 2006-09-20 | 2011-11-10 | Эли Лилли Энд Компани | Тиазолпиразолопиримидиновые соединения как антагонисты рецептора crf1 |
| EP2215090B1 (en) | 2007-10-26 | 2015-03-04 | F. Hoffmann-La Roche AG | Purine derivatives useful as pi3 kinase inhibitors |
| BRPI0908529A2 (pt) | 2008-02-26 | 2015-09-29 | Novartis Ag | composto orgânicos |
| US8158624B2 (en) * | 2008-05-30 | 2012-04-17 | Genetech, Inc. | Purine PI3K inhibitor compounds and methods of use |
| CA2742550A1 (en) * | 2008-10-03 | 2010-04-08 | Merck Serono S.A. | 4-morpholino-pyrido[3,2-d]pyrimidines |
| WO2010074284A1 (ja) * | 2008-12-26 | 2010-07-01 | 味の素株式会社 | ピラゾロピリミジン化合物 |
| NZ596185A (en) * | 2009-04-16 | 2013-01-25 | Ct Nac Investigaciones Oncologicas Cnio | Imidazopyrazines for use as kinase inhibitors |
| SG175708A1 (en) * | 2009-05-27 | 2011-12-29 | Genentech Inc | Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use |
| EP2451811A1 (en) | 2009-05-27 | 2012-05-16 | F. Hoffmann-La Roche AG | Bicyclic indole-pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use |
| GB0912745D0 (en) | 2009-07-22 | 2009-08-26 | Wolfson Microelectronics Plc | Improvements relating to DC-DC converters |
| CN102762565A (zh) | 2010-02-22 | 2012-10-31 | 弗·哈夫曼-拉罗切有限公司 | 吡啶并[3,2-d]嘧啶PI3δ抑制剂化合物及使用方法 |
| MX336711B (es) | 2010-03-04 | 2016-01-28 | Merck Sharp & Dohme | Inhibidores de catecol o-metil transferasa y su uso en el tratamiento de transtornos psicoticos. |
| US9096605B2 (en) * | 2011-08-24 | 2015-08-04 | Glaxosmithkline Llc | Pyrazolopyrimidine derivatives as PI3 kinase inhibitors |
-
2015
- 2015-04-02 PL PL411864A patent/PL236355B1/pl unknown
-
2016
- 2016-03-30 AU AU2016241568A patent/AU2016241568B2/en not_active Ceased
- 2016-03-30 DK DK16714019.3T patent/DK3277687T3/da active
- 2016-03-30 MX MX2017011423A patent/MX2017011423A/es active IP Right Grant
- 2016-03-30 SI SI201630560T patent/SI3277687T1/sl unknown
- 2016-03-30 KR KR1020177031214A patent/KR102559190B1/ko active Active
- 2016-03-30 ES ES16714019T patent/ES2765642T3/es active Active
- 2016-03-30 CA CA2978828A patent/CA2978828A1/en active Pending
- 2016-03-30 EP EP16714019.3A patent/EP3277687B1/en active Active
- 2016-03-30 JP JP2017551627A patent/JP6665201B2/ja not_active Expired - Fee Related
- 2016-03-30 PL PL16714019T patent/PL3277687T3/pl unknown
- 2016-03-30 CN CN201680017259.4A patent/CN107743489B/zh not_active Expired - Fee Related
- 2016-03-30 PT PT167140193T patent/PT3277687T/pt unknown
- 2016-03-30 EA EA201792087A patent/EA032826B1/ru not_active IP Right Cessation
- 2016-03-30 WO PCT/IB2016/051792 patent/WO2016157091A1/en not_active Ceased
- 2016-03-30 HR HRP20192195TT patent/HRP20192195T1/hr unknown
- 2016-03-30 HU HUE16714019A patent/HUE047822T2/hu unknown
- 2016-03-30 BR BR112017020131-3A patent/BR112017020131B1/pt not_active IP Right Cessation
- 2016-03-30 US US15/562,537 patent/US10138247B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| KR20170132275A (ko) | 2017-12-01 |
| MX2017011423A (es) | 2018-05-17 |
| EA032826B1 (ru) | 2019-07-31 |
| DK3277687T3 (da) | 2019-12-16 |
| PT3277687T (pt) | 2020-01-10 |
| BR112017020131A2 (pt) | 2018-05-29 |
| ES2765642T3 (es) | 2020-06-10 |
| EA201792087A1 (ru) | 2018-03-30 |
| EP3277687A1 (en) | 2018-02-07 |
| PL236355B1 (pl) | 2021-01-11 |
| AU2016241568B2 (en) | 2019-09-26 |
| PL3277687T3 (pl) | 2020-09-21 |
| AU2016241568A1 (en) | 2017-10-19 |
| CN107743489B (zh) | 2021-05-04 |
| JP6665201B2 (ja) | 2020-03-13 |
| HUE047822T2 (hu) | 2020-05-28 |
| EP3277687B1 (en) | 2019-10-30 |
| KR102559190B1 (ko) | 2023-07-25 |
| US10138247B2 (en) | 2018-11-27 |
| WO2016157091A1 (en) | 2016-10-06 |
| SI3277687T1 (sl) | 2020-02-28 |
| CA2978828A1 (en) | 2016-10-06 |
| BR112017020131B1 (pt) | 2023-02-28 |
| US20180111939A1 (en) | 2018-04-26 |
| JP2018510192A (ja) | 2018-04-12 |
| CN107743489A (zh) | 2018-02-27 |
| HRP20192195T1 (hr) | 2020-03-06 |
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