AU2006247315A1 - 4, 6-diamino-[1,7] naphthyridine-3-carbonitrile inhibitors of Tpl2 kinase and methods of making and using the same - Google Patents
4, 6-diamino-[1,7] naphthyridine-3-carbonitrile inhibitors of Tpl2 kinase and methods of making and using the same Download PDFInfo
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- AU2006247315A1 AU2006247315A1 AU2006247315A AU2006247315A AU2006247315A1 AU 2006247315 A1 AU2006247315 A1 AU 2006247315A1 AU 2006247315 A AU2006247315 A AU 2006247315A AU 2006247315 A AU2006247315 A AU 2006247315A AU 2006247315 A1 AU2006247315 A1 AU 2006247315A1
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- Australia
- Prior art keywords
- alkyl
- naphthyridine
- carbonitrile
- compound according
- mmol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
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- 238000000034 method Methods 0.000 title claims description 126
- 239000003112 inhibitor Substances 0.000 title description 4
- DMNOLIMFCNADKN-UHFFFAOYSA-N 4,6-diamino-1,7-naphthyridine-3-carbonitrile Chemical compound N#CC1=CN=C2C=NC(N)=CC2=C1N DMNOLIMFCNADKN-UHFFFAOYSA-N 0.000 title description 2
- NMEUKWOOQOHUNA-UHFFFAOYSA-N 4-(3-chloro-4-fluoroanilino)-6-(pyridin-3-ylmethylamino)-1,7-naphthyridine-3-carbonitrile Chemical compound C1=C(Cl)C(F)=CC=C1NC(C1=C2)=C(C#N)C=NC1=CN=C2NCC1=CC=CN=C1 NMEUKWOOQOHUNA-UHFFFAOYSA-N 0.000 title description 2
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- 229940083575 sodium dodecyl sulfate Drugs 0.000 description 1
- 239000011775 sodium fluoride Substances 0.000 description 1
- 235000013024 sodium fluoride Nutrition 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 238000002798 spectrophotometry method Methods 0.000 description 1
- 125000003003 spiro group Chemical group 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- HKSZLNNOFSGOKW-FYTWVXJKSA-N staurosporine Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@@H](NC)[C@@H](OC)[C@]4(C)O1 HKSZLNNOFSGOKW-FYTWVXJKSA-N 0.000 description 1
- CGPUWJWCVCFERF-UHFFFAOYSA-N staurosporine Natural products C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1C1CC(NC)C(OC)C4(OC)O1 CGPUWJWCVCFERF-UHFFFAOYSA-N 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 238000000967 suction filtration Methods 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 239000002511 suppository base Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- QSYTWBKZNNEKPN-UHFFFAOYSA-N tert-butyl 4-(2-aminoethyl)piperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCN(CCN)CC1 QSYTWBKZNNEKPN-UHFFFAOYSA-N 0.000 description 1
- SIPFWMSOIPIUHS-UHFFFAOYSA-N tert-butyl 4-[2-[[4-(4-benzylanilino)-3-cyano-1,7-naphthyridin-6-yl]amino]ethyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCN1CCNC(N=CC1=NC=C2C#N)=CC1=C2NC(C=C1)=CC=C1CC1=CC=CC=C1 SIPFWMSOIPIUHS-UHFFFAOYSA-N 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 150000003536 tetrazoles Chemical group 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- HPGGPRDJHPYFRM-UHFFFAOYSA-J tin(iv) chloride Chemical compound Cl[Sn](Cl)(Cl)Cl HPGGPRDJHPYFRM-UHFFFAOYSA-J 0.000 description 1
- 125000003944 tolyl group Chemical group 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 238000000844 transformation Methods 0.000 description 1
- 150000003852 triazoles Chemical class 0.000 description 1
- IMFACGCPASFAPR-UHFFFAOYSA-N tributylamine Chemical group CCCCN(CCCC)CCCC IMFACGCPASFAPR-UHFFFAOYSA-N 0.000 description 1
- IHIXIJGXTJIKRB-UHFFFAOYSA-N trisodium vanadate Chemical compound [Na+].[Na+].[Na+].[O-][V]([O-])([O-])=O IHIXIJGXTJIKRB-UHFFFAOYSA-N 0.000 description 1
- UJMBCXLDXJUMFB-UHFFFAOYSA-K trisodium;5-oxo-1-(4-sulfonatophenyl)-4-[(4-sulfonatophenyl)diazenyl]-4h-pyrazole-3-carboxylate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)C1=NN(C=2C=CC(=CC=2)S([O-])(=O)=O)C(=O)C1N=NC1=CC=C(S([O-])(=O)=O)C=C1 UJMBCXLDXJUMFB-UHFFFAOYSA-K 0.000 description 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
- 241000701447 unidentified baculovirus Species 0.000 description 1
- 238000011144 upstream manufacturing Methods 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/582—Recycling of unreacted starting or intermediate materials
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US68204405P | 2005-05-18 | 2005-05-18 | |
| US60/682,044 | 2005-05-18 | ||
| PCT/US2006/018996 WO2006124944A1 (en) | 2005-05-18 | 2006-05-17 | 4, 6-diamino-[1,7] naphthyridine-3-carbonitrile inhibitors of tpl2 kinase and methods of making and using the same |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU2006247315A1 true AU2006247315A1 (en) | 2006-11-23 |
Family
ID=36972841
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2006247315A Abandoned AU2006247315A1 (en) | 2005-05-18 | 2006-05-17 | 4, 6-diamino-[1,7] naphthyridine-3-carbonitrile inhibitors of Tpl2 kinase and methods of making and using the same |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US7432279B2 (en:Method) |
| EP (1) | EP1881981A1 (en:Method) |
| JP (1) | JP2008540667A (en:Method) |
| CN (1) | CN101223170A (en:Method) |
| AU (1) | AU2006247315A1 (en:Method) |
| BR (1) | BRPI0611521A2 (en:Method) |
| CA (1) | CA2608362A1 (en:Method) |
| MX (1) | MX2007014258A (en:Method) |
| WO (1) | WO2006124944A1 (en:Method) |
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| AU2011235069B2 (en) * | 2010-04-02 | 2016-03-17 | Senomyx, Inc. | Sweet flavor modifier |
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| AU2011344270A1 (en) | 2010-12-17 | 2013-07-18 | F. Hoffmann-La Roche Ag | Substituted 6,6-fused nitrogenous heterocyclic compounds and uses thereof |
| MY179876A (en) | 2011-08-12 | 2020-11-18 | Firmenich Incorporated | Sweet flavor modifier |
| CN102408426B (zh) * | 2011-09-14 | 2013-07-10 | 湖南有色凯铂生物药业有限公司 | 取代的芳香脲类化合物及其作为抗癌药物的应用 |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118675D0 (en) * | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| EP2911655A1 (en) | 2012-10-24 | 2015-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Tpl2 kinase inhibitors for preventing or treating diabetes and for promoting -cell survival |
| WO2014204261A1 (ko) * | 2013-06-21 | 2014-12-24 | 사회복지법인 삼성생명공익재단 | Tpl2의 발현억제제 또는 활성억제제를 유효성분으로 포함하는 신세포암의 예방 또는 치료용 약학적 조성물 |
| RU2715893C2 (ru) | 2014-03-26 | 2020-03-04 | Астекс Терапьютикс Лтд | Комбинации ингибитора fgfr и ингибитора igf1r |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| SMT202100115T1 (it) | 2014-03-26 | 2021-05-07 | Astex Therapeutics Ltd | Combinazioni di inibitori di fgfr e cmet per il trattamento del cancro |
| AU2015343463A1 (en) | 2014-11-07 | 2017-06-15 | Senomyx, Inc. | Substituted 4-amino-5-(cyclohexyloxy)quinoline-3-carboxylic acids as sweet flavor modifiers |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| PT3319955T (pt) | 2015-07-06 | 2021-01-05 | Gilead Sciences Inc | 6-amino-quinolino-3-carbonitrilos como moduladores de cot |
| EP3456717B1 (en) | 2015-07-06 | 2021-03-17 | Gilead Sciences, Inc. | 4,6-diamino-quinoline-3-carbonitrile derivative as cancer osaka thyroid (cot) modulator for treating inflammatory disease |
| WO2017050865A1 (en) | 2015-09-23 | 2017-03-30 | Janssen Pharmaceutica Nv | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| HRP20201157T1 (hr) | 2015-09-23 | 2020-11-13 | Janssen Pharmaceutica N.V. | Triciklički heterocikli za liječenje raka |
| ES2800339T3 (es) | 2016-06-30 | 2020-12-29 | Gilead Sciences Inc | 4,6-diaminoquinazolinas como moduladores de cuna y métodos de uso de los mismos |
| TWI770527B (zh) | 2019-06-14 | 2022-07-11 | 美商基利科學股份有限公司 | Cot 調節劑及其使用方法 |
| CR20210687A (es) | 2019-06-25 | 2022-03-03 | Gilead Sciences Inc | PROTEÍNAS DE FUSIÓN FLT3L-Fc Y MÉTODOS DE USO |
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| PT4081305T (pt) | 2019-12-24 | 2024-12-04 | Gilead Sciences Inc | Compostos moduladores da diacilglicerol quinase |
| CA3169451A1 (en) | 2020-02-14 | 2021-08-19 | Jounce Therapeutics, Inc. | Antibodies and fusion proteins that bind to ccr8 and uses thereof |
| WO2021179274A1 (en) * | 2020-03-13 | 2021-09-16 | Suzhou Zanrong Pharma Ltd. | ErbB RECEPTOR INHIBITORS AS ANTI-TUMOR AGENTS |
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| TW202302145A (zh) | 2021-04-14 | 2023-01-16 | 美商基利科學股份有限公司 | ＣＤ４７／ＳＩＲＰα結合及ＮＥＤＤ８活化酶Ｅ１調節次單元之共抑制以用於治療癌症 |
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| WO2024215754A1 (en) | 2023-04-11 | 2024-10-17 | Gilead Sciences, Inc. | Kras modulating compounds |
| WO2024220917A1 (en) | 2023-04-21 | 2024-10-24 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| US20250042922A1 (en) | 2023-06-30 | 2025-02-06 | Gilead Sciences, Inc. | Kras modulating compounds |
| US20250100998A1 (en) | 2023-07-26 | 2025-03-27 | Gilead Sciences, Inc. | Parp7 inhibitors |
| US20250066328A1 (en) | 2023-07-26 | 2025-02-27 | Gilead Sciences, Inc. | Parp7 inhibitors |
| US20250101042A1 (en) | 2023-09-08 | 2025-03-27 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| WO2025054530A1 (en) | 2023-09-08 | 2025-03-13 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds |
| US20250154172A1 (en) | 2023-11-03 | 2025-05-15 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| US20250230168A1 (en) | 2023-12-22 | 2025-07-17 | Gilead Sciences, Inc. | Azaspiro wrn inhibitors |
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| CN100408576C (zh) * | 1999-04-21 | 2008-08-06 | 惠氏控股有限公司 | 取代的3-氰基-[1.7],[1.5]和[1.8]-二氮杂萘酪氨酸激酶抑制剂 |
| US6548496B2 (en) | 1999-04-21 | 2003-04-15 | American Cyanamid Company | Substituted 3-cyano-[1.7], [1.5], and [1.8] naphthyridine inhibitors of tyrosine kinases |
| US6355636B1 (en) * | 1999-04-21 | 2002-03-12 | American Cyanamid Company | Substituted 3-cyano-[1.7],[1.5], and [1.8] naphthyridine inhibitors of tyrosine kinases |
| US6521618B2 (en) | 2000-03-28 | 2003-02-18 | Wyeth | 3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors |
-
2006
- 2006-05-17 CN CNA2006800261965A patent/CN101223170A/zh active Pending
- 2006-05-17 CA CA002608362A patent/CA2608362A1/en not_active Abandoned
- 2006-05-17 AU AU2006247315A patent/AU2006247315A1/en not_active Abandoned
- 2006-05-17 WO PCT/US2006/018996 patent/WO2006124944A1/en active Application Filing
- 2006-05-17 MX MX2007014258A patent/MX2007014258A/es active IP Right Grant
- 2006-05-17 JP JP2008512451A patent/JP2008540667A/ja not_active Withdrawn
- 2006-05-17 EP EP06759971A patent/EP1881981A1/en not_active Withdrawn
- 2006-05-17 BR BRPI0611521-7A patent/BRPI0611521A2/pt not_active Application Discontinuation
- 2006-05-18 US US11/436,328 patent/US7432279B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US7432279B2 (en) | 2008-10-07 |
| CA2608362A1 (en) | 2006-11-23 |
| US20060276498A1 (en) | 2006-12-07 |
| JP2008540667A (ja) | 2008-11-20 |
| EP1881981A1 (en) | 2008-01-30 |
| BRPI0611521A2 (pt) | 2010-09-14 |
| WO2006124944A1 (en) | 2006-11-23 |
| CN101223170A (zh) | 2008-07-16 |
| MX2007014258A (es) | 2008-01-22 |
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