CN105073751B - 作为酪蛋白激酶1δ/ε抑制剂的新的取代的咪唑 - Google Patents
作为酪蛋白激酶1δ/ε抑制剂的新的取代的咪唑 Download PDFInfo
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- CN105073751B CN105073751B CN201380073382.4A CN201380073382A CN105073751B CN 105073751 B CN105073751 B CN 105073751B CN 201380073382 A CN201380073382 A CN 201380073382A CN 105073751 B CN105073751 B CN 105073751B
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- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 description 1
- WFWLQNSHRPWKFK-ZCFIWIBFSA-N tegafur Chemical compound O=C1NC(=O)C(F)=CN1[C@@H]1OCCC1 WFWLQNSHRPWKFK-ZCFIWIBFSA-N 0.000 description 1
- 229960001674 tegafur Drugs 0.000 description 1
- MHSKRLJMQQNJNC-UHFFFAOYSA-N terephthalamide Chemical compound NC(=O)C1=CC=C(C(N)=O)C=C1 MHSKRLJMQQNJNC-UHFFFAOYSA-N 0.000 description 1
- 229950003046 tesevatinib Drugs 0.000 description 1
- HVXKQKFEHMGHSL-QKDCVEJESA-N tesevatinib Chemical compound N1=CN=C2C=C(OC[C@@H]3C[C@@H]4CN(C)C[C@@H]4C3)C(OC)=CC2=C1NC1=CC=C(Cl)C(Cl)=C1F HVXKQKFEHMGHSL-QKDCVEJESA-N 0.000 description 1
- BPEWUONYVDABNZ-DZBHQSCQSA-N testolactone Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(OC(=O)CC4)[C@@H]4[C@@H]3CCC2=C1 BPEWUONYVDABNZ-DZBHQSCQSA-N 0.000 description 1
- 229960005353 testolactone Drugs 0.000 description 1
- 229960003604 testosterone Drugs 0.000 description 1
- WHRNULOCNSKMGB-UHFFFAOYSA-N tetrahydrofuran thf Chemical compound C1CCOC1.C1CCOC1 WHRNULOCNSKMGB-UHFFFAOYSA-N 0.000 description 1
- 125000003698 tetramethyl group Chemical group [H]C([H])([H])* 0.000 description 1
- VXKWYPOMXBVZSJ-UHFFFAOYSA-N tetramethyltin Chemical compound C[Sn](C)(C)C VXKWYPOMXBVZSJ-UHFFFAOYSA-N 0.000 description 1
- WROMPOXWARCANT-UHFFFAOYSA-N tfa trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C(F)(F)F WROMPOXWARCANT-UHFFFAOYSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- GVIJJXMXTUZIOD-UHFFFAOYSA-N thianthrene Chemical group C1=CC=C2SC3=CC=CC=C3SC2=C1 GVIJJXMXTUZIOD-UHFFFAOYSA-N 0.000 description 1
- 125000003396 thiol group Chemical group [H]S* 0.000 description 1
- 229930192474 thiophene Natural products 0.000 description 1
- 208000013066 thyroid gland cancer Diseases 0.000 description 1
- 208000013076 thyroid tumor Diseases 0.000 description 1
- 229960003087 tioguanine Drugs 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 150000003852 triazoles Chemical class 0.000 description 1
- IMFACGCPASFAPR-UHFFFAOYSA-N tributylamine Chemical compound CCCCN(CCCC)CCCC IMFACGCPASFAPR-UHFFFAOYSA-N 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 125000006168 tricyclic group Chemical group 0.000 description 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
- NOYPYLRCIDNJJB-UHFFFAOYSA-N trimetrexate Chemical compound COC1=C(OC)C(OC)=CC(NCC=2C(=C3C(N)=NC(N)=NC3=CC=2)C)=C1 NOYPYLRCIDNJJB-UHFFFAOYSA-N 0.000 description 1
- 229960001099 trimetrexate Drugs 0.000 description 1
- RIOQSEWOXXDEQQ-UHFFFAOYSA-N triphenylphosphine Chemical compound C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 RIOQSEWOXXDEQQ-UHFFFAOYSA-N 0.000 description 1
- UCPYLLCMEDAXFR-UHFFFAOYSA-N triphosgene Chemical compound ClC(Cl)(Cl)OC(=O)OC(Cl)(Cl)Cl UCPYLLCMEDAXFR-UHFFFAOYSA-N 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- 230000004565 tumor cell growth Effects 0.000 description 1
- 102000003390 tumor necrosis factor Human genes 0.000 description 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 description 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 description 1
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 description 1
- 102000009816 urokinase plasminogen activator receptor activity proteins Human genes 0.000 description 1
- 108040001269 urokinase plasminogen activator receptor activity proteins Proteins 0.000 description 1
- UHTHHESEBZOYNR-UHFFFAOYSA-N vandetanib Chemical compound COC1=CC(C(/N=CN2)=N/C=3C(=CC(Br)=CC=3)F)=C2C=C1OCC1CCN(C)CC1 UHTHHESEBZOYNR-UHFFFAOYSA-N 0.000 description 1
- 229960000241 vandetanib Drugs 0.000 description 1
- 239000002525 vasculotropin inhibitor Substances 0.000 description 1
- 229950000578 vatalanib Drugs 0.000 description 1
- YCOYDOIWSSHVCK-UHFFFAOYSA-N vatalanib Chemical compound C1=CC(Cl)=CC=C1NC(C1=CC=CC=C11)=NN=C1CC1=CC=NC=C1 YCOYDOIWSSHVCK-UHFFFAOYSA-N 0.000 description 1
- 229940099039 velcade Drugs 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 229940033942 zoladex Drugs 0.000 description 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261740564P | 2012-12-21 | 2012-12-21 | |
| US61/740564 | 2012-12-21 | ||
| PCT/US2013/076795 WO2014100533A1 (en) | 2012-12-21 | 2013-12-20 | NOVEL SUBSTITUTED IMIDAZOLES AS CASEIN KINASE 1 δ/ε INHIBITORS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105073751A CN105073751A (zh) | 2015-11-18 |
| CN105073751B true CN105073751B (zh) | 2018-11-30 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380073382.4A Expired - Fee Related CN105073751B (zh) | 2012-12-21 | 2013-12-20 | 作为酪蛋白激酶1δ/ε抑制剂的新的取代的咪唑 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US9556179B2 (enExample) |
| EP (1) | EP2935271B1 (enExample) |
| JP (1) | JP6267231B2 (enExample) |
| CN (1) | CN105073751B (enExample) |
| WO (1) | WO2014100533A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
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| JP6283688B2 (ja) | 2012-12-21 | 2018-02-21 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | カゼインキナーゼ１ｄ／ｅ阻害剤としての新規なピラゾール置換のイミダゾピラジン |
| EP3157925B1 (en) | 2014-06-19 | 2019-12-18 | Bristol-Myers Squibb Company | Imidazo-pyridazine derivatives as casein kinase 1 delta/epsilon inhibitors |
| ES2895626T3 (es) | 2014-11-21 | 2022-02-22 | Rigel Pharmaceuticals Inc | Derivados de imidazol condensados como inhibidores de TGF-beta |
| EP3265454B1 (en) * | 2015-03-02 | 2020-02-26 | Rigel Pharmaceuticals, Inc. | Tgf-beta inhibitors |
| EP4591936A3 (en) | 2015-03-23 | 2025-10-15 | Tianli Biotech Pty Ltd | Treatment of respiratory diseases |
| CA2994027C (en) | 2015-07-31 | 2023-10-10 | Merck Patent Gmbh | Bicyclic heterocyclic derivatives |
| JP7177495B2 (ja) * | 2016-09-21 | 2022-11-24 | ベクタス・バイオシステムズ・リミテッド | 高血圧症及び／又は線維症を処置するための組成物 |
| WO2018224455A1 (en) | 2017-06-07 | 2018-12-13 | Basf Se | Substituted cyclopropyl derivatives |
| ES2918448T3 (es) * | 2018-03-29 | 2022-07-15 | Univ Masarykova | 4-(1H-Imidazol-5-il)-1H-pirrolo [2,3-b]piridinas para su uso en el tratamiento de leucemias, linfomas y tumores sólidos |
| AU2019336540B2 (en) * | 2018-09-09 | 2025-02-13 | Qanatpharma Ag | Use of casein kinase 1 inhibitors for treating vascular diseases |
| WO2020093098A1 (en) | 2018-11-07 | 2020-05-14 | The University Of Melbourne | Novel compounds for the treatment of respiratory diseases |
| US11795160B2 (en) | 2019-02-22 | 2023-10-24 | Insilico Medicine Ip Limited | Kinase inhibitors |
| US11530199B2 (en) | 2021-02-24 | 2022-12-20 | Insilico Medicine Ip Limited | Analogs for the treatment of disease |
| WO2025231117A1 (en) * | 2024-05-01 | 2025-11-06 | Nimbus Salacia, Inc. | Sik2 modulators and uses thereof |
| WO2025231112A1 (en) * | 2024-05-01 | 2025-11-06 | Nimbus Salacia, Inc. | Sik2 modulators and uses thereof |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003249977A1 (en) * | 2002-07-05 | 2004-01-23 | Axxima Pharmaceuticals Ag | Imidazole compounds for the treatment of hepatitis c virus infections |
| US20070078136A1 (en) | 2005-09-22 | 2007-04-05 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
| JPWO2008016131A1 (ja) * | 2006-08-04 | 2009-12-24 | 武田薬品工業株式会社 | 縮合複素環化合物 |
| EP2170337A4 (en) * | 2007-06-28 | 2013-12-18 | Abbvie Inc | NEW TRIAZOLOPYRIDAZINE |
| FR2918986B1 (fr) * | 2007-07-19 | 2009-09-04 | Sanofi Aventis Sa | Derives de 6-cycloamino-3-(pyridazin-4-yl)imidazo[1,2-b]- pyridazine, leur preparation et leur application en therapeutique |
| CA2710194C (en) | 2007-12-19 | 2014-04-22 | Amgen Inc. | Inhibitors of p13 kinase |
| WO2009137081A2 (en) | 2008-05-07 | 2009-11-12 | Massachusetts Institute Of Technology | Small molecule inhibitors of plasmodium falciparum dihydroorotate dehydrogenase |
| TWI501965B (zh) | 2008-06-20 | 2015-10-01 | Lundbeck & Co As H | 作為ｐｄｅ１０ａ酵素抑制劑之新穎苯基咪唑衍生物 |
| FR2940284B1 (fr) | 2008-12-19 | 2011-02-18 | Sanofi Aventis | Derives de 6-cycloamino-2,3-di-pyridinyl-imidazo°1,2-b!- pyridazine,leur preparation et leur application en therapeutique |
| FR2940285A1 (fr) * | 2008-12-19 | 2010-06-25 | Sanofi Aventis | Derives de 6-cycloamino-2-thienyl-3-(pyridin-4-yl)imidazo °1,2-b!-pyridazine et 6-cycloamino-2-furanyl-3- (pyridin-4-yl)imidazo°1,2-b!-pyridazine, leur preparation et leur application en therapeutique |
| US20100204265A1 (en) | 2009-02-09 | 2010-08-12 | Genelabs Technologies, Inc. | Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections |
| UA107791C2 (en) | 2009-05-05 | 2015-02-25 | Dow Agrosciences Llc | Pesticidal compositions |
| EP2493876B1 (en) | 2009-10-28 | 2014-02-12 | Pfizer Inc | Imidazole derivatives as casein kinase inhibitors |
| JP6283688B2 (ja) | 2012-12-21 | 2018-02-21 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | カゼインキナーゼ１ｄ／ｅ阻害剤としての新規なピラゾール置換のイミダゾピラジン |
-
2013
- 2013-12-20 EP EP13818937.8A patent/EP2935271B1/en not_active Not-in-force
- 2013-12-20 CN CN201380073382.4A patent/CN105073751B/zh not_active Expired - Fee Related
- 2013-12-20 US US14/653,895 patent/US9556179B2/en active Active
- 2013-12-20 WO PCT/US2013/076795 patent/WO2014100533A1/en not_active Ceased
- 2013-12-20 JP JP2015549756A patent/JP6267231B2/ja not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US9556179B2 (en) | 2017-01-31 |
| JP2016507502A (ja) | 2016-03-10 |
| JP6267231B2 (ja) | 2018-01-24 |
| EP2935271A1 (en) | 2015-10-28 |
| EP2935271B1 (en) | 2017-10-25 |
| WO2014100533A1 (en) | 2014-06-26 |
| US20150344481A1 (en) | 2015-12-03 |
| CN105073751A (zh) | 2015-11-18 |
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