DK3083631T3 - Wnt-vejsmodulatorer - Google Patents
Wnt-vejsmodulatorer Download PDFInfo
- Publication number
- DK3083631T3 DK3083631T3 DK14870867.0T DK14870867T DK3083631T3 DK 3083631 T3 DK3083631 T3 DK 3083631T3 DK 14870867 T DK14870867 T DK 14870867T DK 3083631 T3 DK3083631 T3 DK 3083631T3
- Authority
- DK
- Denmark
- Prior art keywords
- methyl
- compound
- synthesis
- pyrimidin
- nmr
- Prior art date
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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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- 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
- A61P27/02—Ophthalmic agents
-
- 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
- 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
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Ophthalmology & Optometry (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Dermatology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (15)
1. Forbindelse med formlen (I)
eller et farmaceutisk acceptabelt salt, solvat eller en farmaceutisk acceptabel polymorf deraf, herunder alle tautomerer og stereoisomerer deraf, hvor Ri betegner H; eventuelt substitueret alkyl (hvor de eventuelle substituenter indbefatter en eller flere substituenter, der hver er uafhængigt valgt blandt Ci-6alkoxy, NH2, -NHCi-3alkyl og -N (Ci-3alkyl)2); -C(0)0alkyl; halogenalkyl; halogenalkoxy; eller -alkylaryl; hver R2 uafhængigt betegner H; eventuelt substitueret alkyl (hvor de eventuelle substituenter indbefatter en eller flere substituenter, der hver er uafhængigt valgt blandt Ci-6alkoxy, NH2, -NHCi-3alkyl og -N (Ci-3alkyl) 2) ; -alkylaryl; eventuelt substitueret carbocyclyl (hvor de eventuelle substituenter indbefatter en eller flere substituenter, der hver er uafhængigt valgt blandt Ci-6alkyl, Ci-6alkoxy, Ci-6halogenalkyl, Ci-6halogenalkoxy og halogen); eventuelt substitueret heterocyclyl (hvor de eventuelle substituenter indbefatter en eller flere substituenter, der hver er uafhængigt valgt blandt Ci-6alkyl, Ci-6alkoxy, -C (0) 0Ci-6alkyl, -C (0) Ci-6alkyl og -C (0) NHCi-6alkyl) ; - NHalkyl; -N(alkyl)2; amino; hydroxyl; alkoxy eller halogen; n betegner 0, 1 eller 2; R3 betegner H eller alkyl; R4 betegner H eller alkyl; R5 betegner H eller alkyl; W og X betegner hver uafhængigt C=0; C=S eller CH2; Y betegner aryl eller 6-leddet monocyklisk heteroaryl; og Z betegner aryl eller heteroaryl.
2. Forbindelse ifølge krav 1, hvor Ri betegner H, methyl, ethyl, -C(0)0Me, CF3 eller OMe.
3. Forbindelse ifølge krav 1 eller krav 2, hvor hver R2 uafhængigt betegner H eller alkyl.
4. Forbindelse ifølge et hvilket som helst af kravene 1 til 3, hvor W og X hver betegner C=0.
5. Forbindelse ifølge et hvilket som helst af kravene 1 til 4, hvor Y betegner monocyklisk heteroaryl, der omfatter en, to eller tre ring-heteroatomer, herunder et eller to nitrogenatomer.
6. Forbindelse ifølge et hvilket som helst af kravene 1 til 4, hvor Y betegner phenyl.
7. Forbindelse ifølge et hvilket som helst af kravene 1 til 6, hvor Y er ikke-substitueret.
8. Forbindelse ifølge krav 1, der er en af følgende forbindelser:
9. Forbindelse ifølge krav 1, som er 4-(2-methyl-6,7-dihydropyrazolo[1,5-a]pyrimidin-4(5H)-yl)-4-oxo-N-(6-(pyridin-3-yl)pyridazin-3-yl)butanamid
eller
10. Forbindelse ifølge et hvilket som helst af kravene 1 til 9 til anvendelse som lægemiddel.
11. Farmaceutisk sammensætning, som omfatter en forbindelse ifølge et hvilket som helst af kravene 1 til 10 i kombination med et eller flere farmaceutisk acceptable adjuvanser eller fortyndingsmidler eller en eller flere farmaceutisk acceptable bærere.
12. Forbindelse ifølge et hvilket som helst af kravene 1 til 10 til anvendelse ved modulering af WNT-vejen.
13. Forbindelse ifølge et hvilket som helst af kravene 1 til 10 til anvendelse ved behandling af en sygdom eller tilstand forbundet med aktiviteten af WNT-vejen.
14. Forbindelse til anvendelse ifølge krav 13, hvor sygdommen eller tilstanden er valgt fra gruppen bestående af cancer, såsom cervixcancer, coloncancer, brystcancer, blærecancer, hoved og hals-cancer, gastrisk cancer, lungecancer, prostatacancer, thyreoideacancer, ikke-småcellet lungecancer, kronisk lymfatisk leukæmi, mesothelioma, melanoma, pancreas-adenocarcinom, basalcellecarcinom, osteosarcom, hepatocellulær carcinom, Wilms tumor eller medulloblastom; fibrose, såsom lungefibrose, leverfibrose, hudfibrose eller nyrefibrose; stamcelle- og diabetisk retinopati; reumatoid artrit; psoriasis; og myokardieinfarkt.
15. Fremgangsmåde til fremstilling af en forbindelse ifølge et hvilket som helst af kravene 1 til 10, hvor W og X hver betegner C=0, hvilken fremgangsmåde omfatter omsætning af en forbindelse med formlen (II)
hvor Ri, R2, R2, n, R3 og R4 er som defineret i et hvilket som helst af kravene 1 til 10, med en forbindelse med formlen (III)
eller et beskyttet derivat deraf, hvor R5, Y og Z er som defineret i et hvilket som helst af kravene 1 til 10.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1322333.4A GB201322333D0 (en) | 2013-12-17 | 2013-12-17 | WNT pathway modulators |
| PCT/SG2014/000602 WO2015094119A1 (en) | 2013-12-17 | 2014-12-17 | Wnt pathway modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK3083631T3 true DK3083631T3 (da) | 2018-09-24 |
Family
ID=50031066
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK14870867.0T DK3083631T3 (da) | 2013-12-17 | 2014-12-17 | Wnt-vejsmodulatorer |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US10189842B2 (da) |
| EP (1) | EP3083631B1 (da) |
| JP (1) | JP6452703B2 (da) |
| KR (1) | KR102383739B1 (da) |
| CN (1) | CN105992767B (da) |
| AU (1) | AU2014367284B2 (da) |
| BR (1) | BR112016013640A8 (da) |
| CA (1) | CA2933683A1 (da) |
| DK (1) | DK3083631T3 (da) |
| ES (1) | ES2687493T3 (da) |
| GB (1) | GB201322333D0 (da) |
| SG (1) | SG11201604839XA (da) |
| WO (1) | WO2015094119A1 (da) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201322333D0 (en) | 2013-12-17 | 2014-01-29 | Agency Science Tech & Res | WNT pathway modulators |
| GB201414730D0 (en) * | 2014-08-19 | 2014-10-01 | Tpp Global Dev Ltd | Pharmaceutical compound |
| DK3204381T3 (da) * | 2014-10-08 | 2022-07-25 | Redx Pharma Plc | N-pyridinylacetamidderivater som wnt-signaleringsbanehæmmere |
| WO2016167372A1 (ja) * | 2015-04-14 | 2016-10-20 | 国立大学法人京都大学 | 大脳皮質ニューロンの誘導方法 |
| TWI804545B (zh) * | 2018-03-23 | 2023-06-11 | 法商史坦普醫藥簡式股份公司 | 化合物 |
| WO2019180244A1 (en) * | 2018-03-23 | 2019-09-26 | Step Pharma S.A.S. | Aminopyrimidine derivatives as ctps1 inhibitors |
| JP7428692B2 (ja) * | 2018-03-23 | 2024-02-06 | ステップ ファーマ エス．エー．エス | Ｃｔｐｓ１阻害剤としてのアミノピリミジン誘導体 |
| EA202191104A1 (ru) | 2018-10-23 | 2021-07-19 | Степ Фарма С.А.С. | Производные аминопиридина/пиразина в качестве ингибиторов ctps1 |
| CN111620874B (zh) * | 2019-02-28 | 2022-11-15 | 汇瀚医疗科技有限公司 | 取代5,6-双杂环氨基化合物作为wnt信号通路抑制剂及其治疗应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070219183A1 (en) * | 2006-03-17 | 2007-09-20 | Wyeth | Dihydropyrazolo[1,5-A]pyrimidine and dihydroimidazo[1,5-A]pyrimidine derivatives and methods of use thereof |
| EP1918291A1 (en) * | 2006-10-30 | 2008-05-07 | Novartis AG | 3-Aminocarbonyl-substituted fused pyrazolo-derivatives as protein kinase modulators |
| CN101906105B (zh) * | 2009-06-08 | 2013-01-16 | 河北医科大学 | 吡唑并[1，5-a]嘧啶酮衍生物及其药物组合物以及其用途 |
| WO2011121096A1 (en) * | 2010-03-31 | 2011-10-06 | Dkfz Deutsches Krebsforschungszentrum | PYRAZOL[1,5-a]PYRIMIDINE DERIVATIVES AS WNT PATHWAY ANTAGONISTS |
| WO2011156632A2 (en) * | 2010-06-09 | 2011-12-15 | Georgetown University | Compositions and methods of treatment for tumors in the nervous system |
| CN104080773B (zh) | 2012-01-28 | 2016-12-28 | 默克专利股份公司 | 氮杂环化合物 |
| PH12017500997A1 (en) * | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
| US20150157633A1 (en) | 2012-05-11 | 2015-06-11 | The Board Of Regents Of The University Of Texas System | Wnt protein signalling inhibitors |
| GB201322333D0 (en) | 2013-12-17 | 2014-01-29 | Agency Science Tech & Res | WNT pathway modulators |
-
2013
- 2013-12-17 GB GBGB1322333.4A patent/GB201322333D0/en not_active Ceased
-
2014
- 2014-12-17 JP JP2016540531A patent/JP6452703B2/ja active Active
- 2014-12-17 ES ES14870867.0T patent/ES2687493T3/es active Active
- 2014-12-17 SG SG11201604839XA patent/SG11201604839XA/en unknown
- 2014-12-17 CA CA2933683A patent/CA2933683A1/en not_active Abandoned
- 2014-12-17 KR KR1020167019109A patent/KR102383739B1/ko active IP Right Grant
- 2014-12-17 BR BR112016013640A patent/BR112016013640A8/pt not_active IP Right Cessation
- 2014-12-17 WO PCT/SG2014/000602 patent/WO2015094119A1/en active Application Filing
- 2014-12-17 US US15/105,224 patent/US10189842B2/en active Active
- 2014-12-17 AU AU2014367284A patent/AU2014367284B2/en active Active
- 2014-12-17 DK DK14870867.0T patent/DK3083631T3/da active
- 2014-12-17 CN CN201480075676.5A patent/CN105992767B/zh active Active
- 2014-12-17 EP EP14870867.0A patent/EP3083631B1/en active Active
-
2018
- 2018-12-19 US US16/226,398 patent/US10870653B2/en active Active
-
2020
- 2020-10-29 US US17/084,507 patent/US11434245B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US20170240550A9 (en) | 2017-08-24 |
| US10870653B2 (en) | 2020-12-22 |
| US20190185478A1 (en) | 2019-06-20 |
| SG11201604839XA (en) | 2016-07-28 |
| US10189842B2 (en) | 2019-01-29 |
| JP6452703B2 (ja) | 2019-01-16 |
| AU2014367284A1 (en) | 2016-06-30 |
| EP3083631B1 (en) | 2018-06-13 |
| KR20160124083A (ko) | 2016-10-26 |
| BR112016013640A8 (pt) | 2020-05-19 |
| WO2015094119A1 (en) | 2015-06-25 |
| ES2687493T3 (es) | 2018-10-25 |
| KR102383739B1 (ko) | 2022-04-05 |
| EP3083631A4 (en) | 2017-05-31 |
| US20210047336A1 (en) | 2021-02-18 |
| EP3083631A1 (en) | 2016-10-26 |
| CN105992767B (zh) | 2019-06-21 |
| AU2014367284B2 (en) | 2019-01-17 |
| US11434245B2 (en) | 2022-09-06 |
| US20180093988A9 (en) | 2018-04-05 |
| US20160311829A1 (en) | 2016-10-27 |
| CA2933683A1 (en) | 2015-06-25 |
| BR112016013640A2 (da) | 2017-08-08 |
| GB201322333D0 (en) | 2014-01-29 |
| JP2016540803A (ja) | 2016-12-28 |
| CN105992767A (zh) | 2016-10-05 |
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