BRPI0611521A2 - inibidores de 4,6-diamino-[1,7]naftiridina-3-carbonitrila de quìnase tpl2 e métodos de fabricação e uso dos mesmos - Google Patents
inibidores de 4,6-diamino-[1,7]naftiridina-3-carbonitrila de quìnase tpl2 e métodos de fabricação e uso dos mesmos Download PDFInfo
- Publication number
- BRPI0611521A2 BRPI0611521A2 BRPI0611521-7A BRPI0611521A BRPI0611521A2 BR PI0611521 A2 BRPI0611521 A2 BR PI0611521A2 BR PI0611521 A BRPI0611521 A BR PI0611521A BR PI0611521 A2 BRPI0611521 A2 BR PI0611521A2
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- compound according
- naphthyridine
- carbonitrile
- mmol
- Prior art date
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- 238000000034 method Methods 0.000 title claims abstract description 129
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- LZXXNPOYQCLXRS-UHFFFAOYSA-N methyl 4-aminobenzoate Chemical compound COC(=O)C1=CC=C(N)C=C1 LZXXNPOYQCLXRS-UHFFFAOYSA-N 0.000 description 1
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- 239000010452 phosphate Substances 0.000 description 1
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- 230000026731 phosphorylation Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 description 1
- XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical compound C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 description 1
- XUWHAWMETYGRKB-UHFFFAOYSA-N piperidin-2-one Chemical compound O=C1CCCCN1 XUWHAWMETYGRKB-UHFFFAOYSA-N 0.000 description 1
- 239000013612 plasmid Substances 0.000 description 1
- 229920001993 poloxamer 188 Polymers 0.000 description 1
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- 125000003367 polycyclic group Chemical group 0.000 description 1
- 229920005862 polyol Polymers 0.000 description 1
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- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 description 1
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- 229920000136 polysorbate Polymers 0.000 description 1
- 229920006316 polyvinylpyrrolidine Polymers 0.000 description 1
- 238000010837 poor prognosis Methods 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- DMTUQTRZIMTUQV-UHFFFAOYSA-N potassium;ethenylideneazanide Chemical compound [K+].[CH2-]C#N DMTUQTRZIMTUQV-UHFFFAOYSA-N 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 230000000770 proinflammatory effect Effects 0.000 description 1
- 239000003380 propellant Substances 0.000 description 1
- 125000004368 propenyl group Chemical group C(=CC)* 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 description 1
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- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 description 1
- USPWKWBDZOARPV-UHFFFAOYSA-N pyrazolidine Chemical compound C1CNNC1 USPWKWBDZOARPV-UHFFFAOYSA-N 0.000 description 1
- DNXIASIHZYFFRO-UHFFFAOYSA-N pyrazoline Chemical compound C1CN=NC1 DNXIASIHZYFFRO-UHFFFAOYSA-N 0.000 description 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 description 1
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical compound OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 description 1
- ILVXOBCQQYKLDS-UHFFFAOYSA-N pyridine N-oxide Chemical compound [O-][N+]1=CC=CC=C1 ILVXOBCQQYKLDS-UHFFFAOYSA-N 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
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- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 235000011083 sodium citrates Nutrition 0.000 description 1
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- 238000002798 spectrophotometry method Methods 0.000 description 1
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- 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
- 239000007929 subcutaneous injection Substances 0.000 description 1
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- 125000001424 substituent group Chemical group 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
- DYHSDKLCOJIUFX-UHFFFAOYSA-N tert-butoxycarbonyl anhydride Chemical compound CC(C)(C)OC(=O)OC(=O)OC(C)(C)C DYHSDKLCOJIUFX-UHFFFAOYSA-N 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
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(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 class 0.000 description 1
- 101150054171 thf1 gene Proteins 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
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
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- 125000005270 trialkylamine group Chemical group 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
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
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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 |
|---|---|
| BRPI0611521A2 true BRPI0611521A2 (pt) | 2010-09-14 |
Family
ID=36972841
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0611521-7A BRPI0611521A2 (pt) | 2005-05-18 | 2006-05-17 | inibidores de 4,6-diamino-[1,7]naftiridina-3-carbonitrila de quìnase tpl2 e métodos de fabricação e uso dos mesmos |
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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| PE20171345A1 (es) | 2010-04-02 | 2017-09-13 | Senomyx Inc | Modificador del sabor dulce |
| 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 |
| CN103261167B (zh) * | 2010-12-17 | 2016-05-04 | 霍夫曼-拉罗奇有限公司 | 取代的6，6-稠合含氮杂环化合物及其用途 |
| MX336378B (es) | 2011-08-12 | 2016-01-15 | Senomyx Inc | Modificador del sabor dulce. |
| 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 |
| GB201118675D0 (en) * | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| 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 |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| IN2015DN03795A (en:Method) | 2012-10-24 | 2015-10-02 | Inserm Inst Nat De La Santé Et De La Rech Médicale | |
| WO2014204261A1 (ko) * | 2013-06-21 | 2014-12-24 | 사회복지법인 삼성생명공익재단 | Tpl2의 발현억제제 또는 활성억제제를 유효성분으로 포함하는 신세포암의 예방 또는 치료용 약학적 조성물 |
| CA2943687C (en) | 2014-03-26 | 2024-02-13 | Astex Therapeutics Ltd | Combinations of an fgfr inhibitor and an igf1r inhibitor |
| PT3122358T (pt) | 2014-03-26 | 2021-03-04 | Astex Therapeutics Ltd | Combinações de inibidores do fgfr e cmet para o tratamento do cancro |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| US11339128B2 (en) | 2014-11-07 | 2022-05-24 | Firmenich Incorporated | 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 |
| NZ738538A (en) | 2015-07-06 | 2019-06-28 | Gilead Sciences Inc | 6-amino-quinoline-3-carbonitrils as cot modulators |
| KR20240008398A (ko) | 2015-07-06 | 2024-01-18 | 길리애드 사이언시즈, 인코포레이티드 | Cot 조정제 및 그의 사용 방법 |
| KR102703498B1 (ko) | 2015-09-23 | 2024-09-04 | 얀센 파마슈티카 엔브이 | 신규 화합물 |
| RU2747644C2 (ru) | 2015-09-23 | 2021-05-11 | Янссен Фармацевтика Нв | Бигетероарил-замещенные 1,4-бензодиазепины и пути их применения для лечения рака |
| AU2017289158C1 (en) | 2016-06-30 | 2020-07-23 | Gilead Sciences, Inc. | 4,6-diaminoquinazolines as Cot modulators and methods of use thereof |
| 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 |
| JP7295283B2 (ja) | 2019-06-25 | 2023-06-20 | ギリアード サイエンシーズ， インコーポレイテッド | Ｆｌｔ３ｌ－ｆｃ融合タンパク質及び使用方法 |
| CN118178645A (zh) | 2019-10-18 | 2024-06-14 | 四十七公司 | 用于治疗骨髓增生异常综合征和急性髓系白血病的联合疗法 |
| KR20220091576A (ko) | 2019-10-31 | 2022-06-30 | 포티 세븐, 인코포레이티드 | 혈액암의 항-cd47 및 항-cd20 기반 치료 |
| TWI778443B (zh) | 2019-11-12 | 2022-09-21 | 美商基利科學股份有限公司 | Mcl1抑制劑 |
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| 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 |
| 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 |
| CZ20013660A3 (cs) * | 1999-04-21 | 2002-01-16 | American Cyanamid Company | Substituované 3-kyano-(1,7),(1,5) a (1,8)-naftyridinové inhibitory tyrosinových kináz |
| 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 |
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2006
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- 2006-05-17 BR BRPI0611521-7A patent/BRPI0611521A2/pt not_active Application Discontinuation
- 2006-05-17 EP EP06759971A patent/EP1881981A1/en not_active Withdrawn
- 2006-05-17 CN CNA2006800261965A patent/CN101223170A/zh active Pending
- 2006-05-17 AU AU2006247315A patent/AU2006247315A1/en not_active Abandoned
- 2006-05-17 MX MX2007014258A patent/MX2007014258A/es active IP Right Grant
- 2006-05-17 CA CA002608362A patent/CA2608362A1/en not_active Abandoned
- 2006-05-17 JP JP2008512451A patent/JP2008540667A/ja not_active Withdrawn
- 2006-05-18 US US11/436,328 patent/US7432279B2/en not_active Expired - Fee Related
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| CN101223170A (zh) | 2008-07-16 |
| WO2006124944A1 (en) | 2006-11-23 |
| JP2008540667A (ja) | 2008-11-20 |
| US20060276498A1 (en) | 2006-12-07 |
| AU2006247315A1 (en) | 2006-11-23 |
| US7432279B2 (en) | 2008-10-07 |
| EP1881981A1 (en) | 2008-01-30 |
| CA2608362A1 (en) | 2006-11-23 |
| MX2007014258A (es) | 2008-01-22 |
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