ES2554375T3 - Inhibidores de las MLK y métodos de uso - Google Patents
Inhibidores de las MLK y métodos de uso Download PDFInfo
- Publication number
- ES2554375T3 ES2554375T3 ES09832359.5T ES09832359T ES2554375T3 ES 2554375 T3 ES2554375 T3 ES 2554375T3 ES 09832359 T ES09832359 T ES 09832359T ES 2554375 T3 ES2554375 T3 ES 2554375T3
- Authority
- ES
- Spain
- Prior art keywords
- pyrazin
- indol
- imidazo
- pyrrolo
- trimethoxyphenyl
- 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.)
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Classifications
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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- 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
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- 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
- C07D471/10—Spiro-condensed systems
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Vascular Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11795008P | 2008-11-25 | 2008-11-25 | |
| US117950P | 2008-11-25 | ||
| US14877809P | 2009-01-30 | 2009-01-30 | |
| US14875509P | 2009-01-30 | 2009-01-30 | |
| US148778P | 2009-01-30 | ||
| US148755P | 2009-01-30 | ||
| PCT/US2009/065878 WO2010068483A2 (en) | 2008-11-25 | 2009-11-25 | Mlk inhibitors and methods of use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2554375T3 true ES2554375T3 (es) | 2015-12-18 |
Family
ID=42243278
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES09832359.5T Active ES2554375T3 (es) | 2008-11-25 | 2009-11-25 | Inhibidores de las MLK y métodos de uso |
Country Status (8)
| Country | Link |
|---|---|
| US (4) | US8877772B2 (enExample) |
| EP (2) | EP2379561B1 (enExample) |
| JP (2) | JP5930278B2 (enExample) |
| CN (1) | CN102264743B (enExample) |
| AU (1) | AU2009324894B2 (enExample) |
| CA (1) | CA2744498C (enExample) |
| ES (1) | ES2554375T3 (enExample) |
| WO (1) | WO2010068483A2 (enExample) |
Families Citing this family (113)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8227603B2 (en) | 2006-08-01 | 2012-07-24 | Cytokinetics, Inc. | Modulating skeletal muscle |
| US8299248B2 (en) | 2006-08-02 | 2012-10-30 | Cytokinetics, Incorporated | Certain 1H-imidazo[4,5-b]pyrazin-2(3H)-ones and 1H-imidazo[4,5-b]pyrazin-2-ols and methods for their use |
| EP2666777A1 (en) | 2006-08-02 | 2013-11-27 | Cytokinetics, Inc. | Certain chemical entities having an imidazo<4,5-b>pyrazin-2(3H)-one core, compositions and methods |
| NZ576278A (en) | 2006-10-19 | 2011-12-22 | Signal Pharm Llc | Heteroaryl compounds, compositions thereof, and their use as protein kinase inhibitors |
| US7998976B2 (en) | 2008-02-04 | 2011-08-16 | Cytokinetics, Inc. | Certain chemical entities, compositions and methods |
| MX2010008518A (es) | 2008-02-04 | 2010-11-10 | Cytokinetics Inc | Ciertas entidades quimicas, composiciones y metodos. |
| BRPI0917540A2 (pt) | 2008-08-05 | 2015-11-17 | Daiichi Sankyo Co Ltd | composto, sal farmacologicamente aceitavél, composição farmacêutica, e, uso de um composto ou sal farmacologicamente aceitável |
| MX2011004953A (es) | 2008-11-10 | 2011-12-14 | Vertex Pharma | Compuestos utiles como inhibidores de cinasa atr. |
| CN102264743B (zh) * | 2008-11-25 | 2015-02-11 | 罗彻斯特大学 | Mlk抑制剂及其使用方法 |
| ES2921576T3 (es) | 2008-12-19 | 2022-08-29 | Vertex Pharma | Compuestos útiles como inhibidores de la quinasa ATR |
| KR20120091240A (ko) | 2009-10-26 | 2012-08-17 | 시그날 파마소티칼 엘엘씨 | 헤테로아릴 화합물의 합성 및 정제 방법 |
| EP2569313A1 (en) | 2010-05-12 | 2013-03-20 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US8969356B2 (en) | 2010-05-12 | 2015-03-03 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| EP2569286B1 (en) | 2010-05-12 | 2014-08-20 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| NZ603478A (en) | 2010-05-12 | 2014-09-26 | Vertex Pharma | 2 -aminopyridine derivatives useful as inhibitors of atr kinase |
| US9334244B2 (en) | 2010-05-12 | 2016-05-10 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2011143419A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Pyrazines useful as inhibitors of atr kinase |
| NZ603644A (en) * | 2010-05-24 | 2014-10-31 | Univ Rochester | Bicyclic heteroaryl kinase inhibitors and methods of use |
| EP2585468A1 (en) * | 2010-06-23 | 2013-05-01 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
| DE102010049877A1 (de) | 2010-11-01 | 2012-05-03 | Merck Patent Gmbh | 7-((1,2,3)Triazol-4-yl)-pyrrolo(2,3) pyrazinderivate |
| EP2487159A1 (en) * | 2011-02-11 | 2012-08-15 | MSD Oss B.V. | RorgammaT inhibitors |
| AU2012240030A1 (en) | 2011-04-05 | 2013-10-24 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of TRA kinase |
| WO2012178123A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2723747A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| US9309250B2 (en) | 2011-06-22 | 2016-04-12 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors |
| WO2013010015A2 (en) | 2011-07-13 | 2013-01-17 | Cytokinetics, Inc. | Combination als therapy |
| RU2018108589A (ru) | 2011-09-30 | 2019-02-25 | Вертекс Фармасьютикалз Инкорпорейтед | Лечение рака поджелудочной железы и немелкоклеточного рака легкого ингибиторами atr |
| CA2850564A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP3878851A1 (en) | 2011-09-30 | 2021-09-15 | Vertex Pharmaceuticals Incorporated | Process for making compounds useful as inhibitors of atr kinase |
| WO2013049720A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US8765751B2 (en) | 2011-09-30 | 2014-07-01 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| EP3466423B1 (en) * | 2011-10-19 | 2021-07-28 | Signal Pharmaceuticals, LLC | Treatment of cancer with tor kinase inhibitors |
| JP2015502925A (ja) | 2011-11-09 | 2015-01-29 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Atrキナーゼの阻害剤として有用なピラジン化合物 |
| EP2776429A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2013071090A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2776420A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| US8846917B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| BR112014013332B1 (pt) | 2011-12-02 | 2022-09-06 | Signal Pharmaceuticals, Llc | Composições farmacêuticas de 7-(6-(2-hidroxi-propan-2-il)piridin-3-il)-1-((trans)-4- metoxicicloexil)-3,4-diidropirazino [2,3-b]pirazin-2(1h)-ona, uma forma sólida dessa e métodos de seu uso |
| KR102064626B1 (ko) | 2012-02-24 | 2020-01-09 | 시그날 파마소티칼 엘엘씨 | Tor 키나제 억제자 복합 치료법을 사용한 비소세포 폐암의 치료 방법 |
| CN102627646A (zh) * | 2012-03-19 | 2012-08-08 | 苏州四同医药科技有限公司 | 一种3-碘-5-溴-4,7-二氮杂吲哚的制备方法 |
| PT2833973T (pt) | 2012-04-05 | 2017-12-21 | Vertex Pharma | Compostos úteis como inibidores da cinase atr e terapias de combinação dos mesmos |
| WO2014026329A1 (en) | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof |
| WO2014026330A1 (en) | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | 3-AMINOCYCLOALKYL COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF |
| WO2014026327A1 (en) | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof |
| WO2014055756A1 (en) | 2012-10-04 | 2014-04-10 | Vertex Pharmaceuticals Incorporated | Method for measuring atr inhibition mediated increases in dna damage |
| EP2909202A1 (en) | 2012-10-16 | 2015-08-26 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
| EP2925319B1 (en) * | 2012-11-30 | 2019-01-09 | University Of Rochester | Mixed lineage kinase inhibitors for hiv/aids therapies |
| WO2014089379A1 (en) | 2012-12-07 | 2014-06-12 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US9260426B2 (en) | 2012-12-14 | 2016-02-16 | Arrien Pharmaceuticals Llc | Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors |
| WO2014096965A2 (en) | 2012-12-21 | 2014-06-26 | Rvx Therapeutics Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| US9346812B2 (en) | 2013-01-16 | 2016-05-24 | Signal Pharmaceuticals, Llc | Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith |
| JP2016510764A (ja) * | 2013-03-07 | 2016-04-11 | カリフィア バイオ, インク.Califia Bio, Inc. | 混合系キナーゼ阻害剤および治療法 |
| US9663519B2 (en) | 2013-03-15 | 2017-05-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| JP6382945B2 (ja) | 2013-04-17 | 2018-08-29 | シグナル ファーマシューティカルズ,エルエルシー | ジヒドロピラジノ−ピラジンによる癌治療 |
| MX368286B (es) | 2013-04-17 | 2019-09-27 | Signal Pharm Llc | Terapia de combinacion que comprende un inhibidor de tor cinasa y un compuesto de quinazolinona 5-sustituida para tratar cancer. |
| CN105339008A (zh) | 2013-04-17 | 2016-02-17 | 西格诺药品有限公司 | 用于治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯酰胺的组合疗法 |
| MX393164B (es) | 2013-04-17 | 2025-03-21 | Signal Pharm Llc | Formulaciones farmacéuticas, proceso, formas sólidas y métodos de uso relacionados con 1-etil-7-(2-metil-6-(1h-1,2,4-triazol-3-ii)piridin-3-ii)-3,4-dihidropirazino[2,3-b]pirazin-2(1h)-ona. |
| BR112015026257B1 (pt) | 2013-04-17 | 2022-12-20 | Signal Pharmaceuticals, Llc | Uso de um composto dihidropirazino-pirazina e enzalutamida, composição farmacêutica que os compreende, e kit |
| EP2986321A1 (en) | 2013-04-17 | 2016-02-24 | Signal Pharmaceuticals, LLC | Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer |
| HK1221150A1 (zh) | 2013-04-17 | 2017-05-26 | 西格诺药品有限公司 | 用二氢吡嗪并-吡嗪类对癌症的治疗 |
| WO2014181813A1 (ja) * | 2013-05-10 | 2014-11-13 | 武田薬品工業株式会社 | 複素環化合物 |
| NZ629486A (en) | 2013-05-29 | 2017-11-24 | Signal Pharm Llc | Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use |
| WO2015004533A2 (en) | 2013-06-21 | 2015-01-15 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| SG11201510409QA (en) | 2013-06-21 | 2016-01-28 | Zenith Epigenetics Corp | Novel bicyclic bromodomain inhibitors |
| WO2015015318A2 (en) | 2013-07-31 | 2015-02-05 | Zenith Epigenetics Corp. | Novel quinazolinones as bromodomain inhibitors |
| WO2015085132A1 (en) | 2013-12-06 | 2015-06-11 | Vertex Pharmaceuticals Incorporated | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
| NZ714742A (en) | 2014-04-16 | 2017-04-28 | Signal Pharm Llc | Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use |
| WO2015160868A1 (en) | 2014-04-16 | 2015-10-22 | Signal Pharmaceuticals, Llc | Methods for treating cancer using tor kinase inhibitor combination therapy |
| EP3131551A4 (en) | 2014-04-16 | 2017-09-20 | Signal Pharmaceuticals, LLC | SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF |
| US9718824B2 (en) | 2014-04-16 | 2017-08-01 | Signal Pharmaceuticals, Llc | Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, and a coformer, compositions and methods of use thereof |
| HRP20200186T1 (hr) | 2014-06-05 | 2020-05-29 | Vertex Pharmaceuticals Inc. | Radioaktivno obilježeni derivati 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-karboksamid spojeva koji se koriste kao inhibitori atr kinaze, priprava navedenih spojeva i njihovi različiti čvrsti oblici |
| JP6936007B2 (ja) | 2014-06-17 | 2021-09-15 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Chk1阻害剤とatr阻害剤との組み合わせを使用してがんを処置する方法 |
| NZ629796A (en) | 2014-07-14 | 2015-12-24 | Signal Pharm Llc | Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use |
| AU2015289929A1 (en) | 2014-07-14 | 2017-03-02 | Signal Pharmaceuticals, Llc | Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof |
| PT3180329T (pt) | 2014-08-15 | 2020-06-08 | Janssen Pharmaceuticals Inc | Triazóis como inibidores do recetor nr2b |
| HUE049278T2 (hu) | 2014-08-15 | 2020-09-28 | Janssen Pharmaceuticals Inc | Pirazolok |
| EP3227280B1 (en) | 2014-12-01 | 2019-04-24 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| JP2017537946A (ja) | 2014-12-11 | 2017-12-21 | ゼニス・エピジェネティクス・リミテッドZenith Epigenetics Ltd. | ブロモドメイン阻害剤としての置換複素環 |
| HK1245247A1 (zh) | 2014-12-17 | 2018-08-24 | 恒翼生物医药科技(上海)有限公司 | 溴结构域的抑制剂 |
| CA2975997A1 (en) | 2015-02-11 | 2016-08-18 | Merck Sharp & Dohme Corp. | Substituted pyrazole compounds as rorgammat inhibitors and uses thereof |
| WO2016164641A1 (en) * | 2015-04-08 | 2016-10-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| LT3319963T (lt) | 2015-07-09 | 2020-03-25 | Janssen Pharmaceutica Nv | Pakeistieji 4-azaindolai ir jų, kaip glun2b receptoriaus moduliatorių, panaudojimas |
| EP3355926B1 (en) | 2015-09-30 | 2025-12-24 | Vertex Pharmaceuticals Inc. | Combination of dna damaging agents and atr inhibitors for use in a method for treating cancer using |
| JP2018531958A (ja) | 2015-10-27 | 2018-11-01 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | RORγT阻害薬としてのヘテロアリール置換安息香酸及びその使用 |
| AU2016344111A1 (en) | 2015-10-27 | 2018-05-10 | Merck Sharp & Dohme Corp. | Substituted bicyclic pyrazole compounds as RORgammaT inhibitors and uses thereof |
| CA3002850A1 (en) | 2015-10-27 | 2017-05-04 | Merck Sharp & Dohme Corp. | Substituted indazole compounds as rorgammat inhibitors and uses thereof |
| CA3014314A1 (en) | 2016-02-10 | 2017-08-17 | Janssen Pharmaceutica Nv | Substituted 1,2,3-triazoles as nr2b-selective nmda modulators |
| TW201819376A (zh) | 2016-10-06 | 2018-06-01 | 比利時商健生藥品公司 | 經取代之1H-咪唑並[4,5-b]吡啶-2(3H)-酮及其作為GLUN2B受體調節劑之用途 |
| US11447503B2 (en) | 2019-06-14 | 2022-09-20 | Janssen Pharmaceutica Nv | Pyridine carbamates and their use as GLUN2B receptor modulators |
| IL271491B2 (en) | 2017-06-22 | 2023-09-01 | Celgene Corp | Treatment of carcinoma of the liver characterized by hepatitis b virus infection |
| AU2019226571A1 (en) | 2018-03-01 | 2020-10-01 | The Trustees Of Columbia University In The City Of New York | Compounds, compositions, and methods for suppressing toxic endoplasmic reticulum stress |
| WO2019193516A2 (en) | 2018-04-04 | 2019-10-10 | Janssen Pharmaceutica Nv | Substituted pyridine and pyrimidines and their use as glun2b receptor modulators |
| JP7486478B2 (ja) * | 2018-09-19 | 2024-05-17 | エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト | スピロ環状2,3-ジヒドロ-7-アザインドール化合物およびその使用 |
| WO2020236890A1 (en) * | 2019-05-20 | 2020-11-26 | Mayo Foundation For Medical Education And Research | Treating chronic liver disease |
| EP3983075A1 (en) | 2019-06-14 | 2022-04-20 | Janssen Pharmaceutica NV | Substituted pyrazolo-pyridine amides and their use as glun2b receptor modulators |
| US11459336B2 (en) | 2019-06-14 | 2022-10-04 | Janssen Pharmaceutica Nv | Pyrazine carbamates and their use as GluN2B receptor modulators |
| PH12021552839A1 (en) | 2019-06-14 | 2022-10-03 | Janssen Pharmaceutica Nv | Substituted pyrazolo-pyridine amides and their use as glun2b receptor modulators |
| KR20220024403A (ko) | 2019-06-14 | 2022-03-03 | 얀센 파마슈티카 엔.브이. | 치환된 피라졸로-피라진 및 이들의 glun2b 수용체 조절제로서의 용도 |
| BR112021025141A2 (pt) | 2019-06-14 | 2022-01-25 | Janssen Pharmaceutica Nv | Pirazolo-piridinas heteroaromáticas substituídas e seu uso como moduladores do receptor glun2b |
| CN113993583A (zh) | 2019-06-14 | 2022-01-28 | 詹森药业有限公司 | 取代的吡唑并[4,3-b]吡啶及其作为GLUN2B受体调节剂的用途 |
| EP4023647B1 (en) * | 2019-08-30 | 2025-04-09 | TSD Life Sciences Co., Ltd. | Imidazopyridine derivative and pharmaceutical composition comprising same as active ingredient |
| WO2021163683A1 (en) | 2020-02-14 | 2021-08-19 | President And Fellows Of Harvard College | Inhibitors of nicotinamide n-methyltransferase, compositions and uses thereof |
| US20230183215A1 (en) * | 2020-05-21 | 2023-06-15 | Stemsynergy Therapeutics, Inc. | Notch Inhibitors and Uses Thereof |
| WO2023050323A1 (en) * | 2021-09-30 | 2023-04-06 | Citrix Systems, Inc. | Automated transfer of peripheral device operations |
| US11661409B1 (en) * | 2022-01-31 | 2023-05-30 | Pioneura Corporation | Acid addition salts, compositions, and methods of treating |
| US11479541B1 (en) | 2022-01-31 | 2022-10-25 | Pioneura Corporation | Acid addition salts, compositions, and methods of treating thereof |
| WO2023207911A1 (zh) * | 2022-04-24 | 2023-11-02 | 上海医药集团股份有限公司 | 一种双环杂环化合物、药物组合物和应用 |
| CN117050075A (zh) * | 2022-05-05 | 2023-11-14 | 中国药科大学 | 一类联芳环类bet抑制剂及合成方法与用途 |
| CN117447392B (zh) * | 2023-09-13 | 2024-11-26 | 广州大学 | 一种荧光材料及其制备方法和应用 |
Family Cites Families (78)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4933438A (en) | 1984-02-29 | 1990-06-12 | University Of Florida | Brain-specific analogues of centrally acting amines |
| US6150354A (en) | 1987-01-15 | 2000-11-21 | Bonnie Davis | Compounds for the treatment of Alzheimer's disease |
| US5133974A (en) | 1989-05-05 | 1992-07-28 | Kv Pharmaceutical Company | Extended release pharmaceutical formulations |
| DE69229781T2 (de) | 1991-05-14 | 2000-01-05 | Ernir Snorrason | Behandlung des ermüdungssyndroms mit cholinesteraseinhibitoren |
| IT1250421B (it) | 1991-05-30 | 1995-04-07 | Recordati Chem Pharm | Composizione farmaceutica a rilascio controllato con proprieta' bio-adesive. |
| US6537579B1 (en) | 1993-02-22 | 2003-03-25 | American Bioscience, Inc. | Compositions and methods for administration of pharmacologically active compounds |
| FR2710265B1 (fr) | 1993-09-22 | 1995-10-20 | Adir | Composition pharmaceutique bioadhésive pour la libération contrôlée de principes actifs. |
| US5618819A (en) | 1994-07-07 | 1997-04-08 | Adir Et Compagnie | 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-(3H)-one compounds |
| US6548084B2 (en) | 1995-07-20 | 2003-04-15 | Smithkline Beecham Plc | Controlled release compositions |
| US6245347B1 (en) | 1995-07-28 | 2001-06-12 | Zars, Inc. | Methods and apparatus for improved administration of pharmaceutically active compounds |
| DE19541260A1 (de) | 1995-11-06 | 1997-05-07 | Lohmann Therapie Syst Lts | Therapeutische Zubereitung zur transdermalen Applikation von Wirkstoffen durch die Haut |
| US6512010B1 (en) | 1996-07-15 | 2003-01-28 | Alza Corporation | Formulations for the administration of fluoxetine |
| DE69819351D1 (de) | 1997-09-11 | 2003-12-04 | Nycomed Danmark As Roskilde | Aus mehreren einzeleinheiten zusammengesetzte arzneimittel mit nicht-steroidalen wirkstoffen (nsaids) |
| US6624200B2 (en) | 1998-08-25 | 2003-09-23 | Columbia Laboratories, Inc. | Bioadhesive progressive hydration tablets |
| US6607751B1 (en) | 1997-10-10 | 2003-08-19 | Intellipharamaceutics Corp. | Controlled release delivery device for pharmaceutical agents incorporating microbial polysaccharide gum |
| GB9721437D0 (en) | 1997-10-10 | 1997-12-10 | Glaxo Group Ltd | Heteroaromatic compounds and their use in medicine |
| US6403597B1 (en) | 1997-10-28 | 2002-06-11 | Vivus, Inc. | Administration of phosphodiesterase inhibitors for the treatment of premature ejaculation |
| US6248864B1 (en) | 1997-12-31 | 2001-06-19 | Adherex Technologies, Inc. | Compounds and methods and modulating tissue permeability |
| US6613358B2 (en) | 1998-03-18 | 2003-09-02 | Theodore W. Randolph | Sustained-release composition including amorphous polymer |
| US6312717B1 (en) | 1998-07-07 | 2001-11-06 | Bristol-Myers Squibb Company | Method for treatment of anxiety and depression |
| US20020009478A1 (en) | 1998-08-24 | 2002-01-24 | Douglas Joseph Dobrozsi | Oral liquid mucoadhesive compositions |
| SE9802864D0 (sv) | 1998-08-27 | 1998-08-27 | Pharmacia & Upjohn Ab | Transdermally administered tolterodine as antimuscarinic agent for the treatment of overactive bladder |
| EP1121104B1 (en) | 1998-10-01 | 2005-01-12 | Novartis AG | New controlled release oral formulations for rivastigmine |
| US6248363B1 (en) | 1999-11-23 | 2001-06-19 | Lipocine, Inc. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| US6498176B1 (en) | 1999-03-04 | 2002-12-24 | Smithklinebeecham Corporation | 3-(anilinomethylene) oxindoles as protein tyrosine kinase and protein serine/threonine kinase inhibitors |
| GB9904995D0 (en) | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Substituted aza-oxindole derivatives |
| US6624171B1 (en) | 1999-03-04 | 2003-09-23 | Smithkline Beecham Corporation | Substituted aza-oxindole derivatives |
| GB9904933D0 (en) | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Compounds |
| FR2792527B1 (fr) | 1999-04-22 | 2004-08-13 | Ethypharm Lab Prod Ethiques | Microgranules de ketoprofene, procede de preparation et compositions pharmaceutiques |
| US6541020B1 (en) | 1999-07-09 | 2003-04-01 | Trimeris, Inc. | Methods and compositions for administration of therapeutic reagents |
| CZ2002203A3 (cs) | 1999-07-21 | 2002-08-14 | Astrazeneca Ab | Spirooxindolové deriváty |
| US6562375B1 (en) | 1999-08-04 | 2003-05-13 | Yamanouchi Pharmaceuticals, Co., Ltd. | Stable pharmaceutical composition for oral use |
| WO2001015668A1 (en) | 1999-09-02 | 2001-03-08 | Nostrum Pharmaceuticals, Inc. | Controlled release pellet formulation |
| US6544548B1 (en) | 1999-09-13 | 2003-04-08 | Keraplast Technologies, Ltd. | Keratin-based powders and hydrogel for pharmaceutical applications |
| US6080736A (en) | 1999-10-27 | 2000-06-27 | Janus Pharmaceuticals, Inc. | Methods and compositions for treating and preventing anxiety and anxiety disorders using optically pure (R) tofisopam |
| US6461631B1 (en) | 1999-11-16 | 2002-10-08 | Atrix Laboratories, Inc. | Biodegradable polymer composition |
| WO2001047501A1 (en) | 1999-12-29 | 2001-07-05 | Nanodelivery, Inc. | Drug delivery system exhibiting permeability control |
| US6589549B2 (en) | 2000-04-27 | 2003-07-08 | Macromed, Incorporated | Bioactive agent delivering system comprised of microparticles within a biodegradable to improve release profiles |
| US6524621B2 (en) | 2000-05-01 | 2003-02-25 | Aeropharm Technology Inc. | Core formulation |
| US6482440B2 (en) | 2000-09-21 | 2002-11-19 | Phase 2 Discovery, Inc. | Long acting antidepressant microparticles |
| US6524615B2 (en) | 2001-02-21 | 2003-02-25 | Kos Pharmaceuticals, Incorporated | Controlled release pharmaceutical composition |
| CA2439263C (en) | 2001-03-02 | 2012-10-23 | Frank Becker | Three hybrid assay system |
| US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
| EP2295433A3 (en) * | 2003-03-06 | 2011-07-06 | Eisai R&D Management Co., Ltd. | JNK inhibitors |
| GB2400101A (en) * | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
| US7250417B2 (en) * | 2003-07-02 | 2007-07-31 | Sugen Inc. | Arylmethyl triazolo- and imidazopyrazines as c-Met inhibitors |
| AR045595A1 (es) * | 2003-09-04 | 2005-11-02 | Vertex Pharma | Composiciones utiles como inhibidores de proteinas quinasas |
| NZ584499A (en) * | 2004-03-30 | 2011-08-26 | Vertex Pharma | Azaindoles Useful as Inhibitors of Jak and Other Protein Kinases |
| US20060011139A1 (en) | 2004-07-16 | 2006-01-19 | Applied Materials, Inc. | Heated substrate support for chemical vapor deposition |
| US7709645B2 (en) * | 2004-07-27 | 2010-05-04 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| US7361763B2 (en) | 2004-07-27 | 2008-04-22 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| US7361764B2 (en) * | 2004-07-27 | 2008-04-22 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| CN101027302B (zh) * | 2004-07-27 | 2011-05-11 | Sgx药物公司 | 吡咯并吡啶激酶调节剂 |
| US7626021B2 (en) | 2004-07-27 | 2009-12-01 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
| EP1796467A4 (en) | 2004-09-24 | 2009-07-01 | Janssen Pharmaceutica Nv | INHIBITORS IMIDAZO {4,5-B} PYRAZINONE PROTEIN KINASES |
| AU2005302707A1 (en) | 2004-10-27 | 2006-05-11 | Janssen Pharmaceutica N.V. | Pyridine imidazoles and aza-indoles as progesterone receptor modulators |
| US20090233955A1 (en) | 2004-12-08 | 2009-09-17 | Frazee James S | 1H-Pyrrolo[2,3-B]Pyridnes |
| US7763616B2 (en) | 2005-02-16 | 2010-07-27 | Schering Corporation | Piperazine-piperidines with CXCR3 antagonist activity |
| PL2395004T3 (pl) * | 2005-06-22 | 2016-08-31 | Plexxikon Inc | Pochodne pirolo[2,3-b]pirydyny jako inhibitory kinazy białkowej |
| JP2007108926A (ja) | 2005-10-12 | 2007-04-26 | Denso Corp | 運転支援装置及びプログラム |
| JP2009518042A (ja) | 2005-12-08 | 2009-05-07 | アイアールエム・リミテッド・ライアビリティ・カンパニー | Hiv感染を阻止する方法および組成物 |
| ATE477331T1 (de) | 2006-05-05 | 2010-08-15 | George Mason Intellectual Prop | Verfahren zum nachweis einer hiv-infektion |
| EP2029593A1 (en) * | 2006-05-22 | 2009-03-04 | AstraZeneca AB | Indole derivatives |
| US7732447B2 (en) | 2006-06-22 | 2010-06-08 | Cephalon, Inc. | Fused [d]pyridazin-7-ones |
| EP2666777A1 (en) | 2006-08-02 | 2013-11-27 | Cytokinetics, Inc. | Certain chemical entities having an imidazo<4,5-b>pyrazin-2(3H)-one core, compositions and methods |
| NZ576278A (en) * | 2006-10-19 | 2011-12-22 | Signal Pharm Llc | Heteroaryl compounds, compositions thereof, and their use as protein kinase inhibitors |
| GB0706168D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| EP2078020A4 (en) | 2007-04-10 | 2011-10-19 | Sgx Pharmaceuticals Inc | HETEROCYCLIC MODULATORS WITH FUSED CYCLES FOR KINASES |
| CN101663302B (zh) | 2007-04-18 | 2013-07-24 | 橘生药品工业株式会社 | 含氮稠环衍生物、包含所述含氮稠环衍生物的药物组合物及其医药用途 |
| JP2011500806A (ja) | 2007-10-25 | 2011-01-06 | メルク・シャープ・エンド・ドーム・コーポレイション | 治療用化合物 |
| MX2010008198A (es) | 2008-02-25 | 2010-08-23 | Hoffmann La Roche | Inhibidores de cinasa de pirrolopirazina. |
| BRPI0917540A2 (pt) * | 2008-08-05 | 2015-11-17 | Daiichi Sankyo Co Ltd | composto, sal farmacologicamente aceitavél, composição farmacêutica, e, uso de um composto ou sal farmacologicamente aceitável |
| EP2356116A1 (en) * | 2008-11-20 | 2011-08-17 | OSI Pharmaceuticals, Inc. | Substituted pyrroloý2,3-b¨-pyridines and-pyrazines |
| CN102264743B (zh) * | 2008-11-25 | 2015-02-11 | 罗彻斯特大学 | Mlk抑制剂及其使用方法 |
| WO2010068899A1 (en) | 2008-12-12 | 2010-06-17 | Creighton University | Nanoparticles comprising combinations of antiretroviral agents and use thereof |
| NZ603644A (en) | 2010-05-24 | 2014-10-31 | Univ Rochester | Bicyclic heteroaryl kinase inhibitors and methods of use |
| JP2013542945A (ja) | 2010-11-02 | 2013-11-28 | ボード オブ リージェンツ オブ ザ ユニバーシティ オブ ネブラスカ | 治療を送達するための組成物および方法 |
| EP2925319B1 (en) | 2012-11-30 | 2019-01-09 | University Of Rochester | Mixed lineage kinase inhibitors for hiv/aids therapies |
-
2009
- 2009-11-25 CN CN200980152665.1A patent/CN102264743B/zh active Active
- 2009-11-25 EP EP09832359.5A patent/EP2379561B1/en active Active
- 2009-11-25 ES ES09832359.5T patent/ES2554375T3/es active Active
- 2009-11-25 WO PCT/US2009/065878 patent/WO2010068483A2/en not_active Ceased
- 2009-11-25 AU AU2009324894A patent/AU2009324894B2/en active Active
- 2009-11-25 JP JP2011537733A patent/JP5930278B2/ja active Active
- 2009-11-25 CA CA2744498A patent/CA2744498C/en active Active
- 2009-11-25 EP EP15186751.2A patent/EP3037421A3/en not_active Withdrawn
- 2009-11-25 US US13/131,193 patent/US8877772B2/en active Active
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2014
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- 2014-11-14 JP JP2014232195A patent/JP5873544B2/ja active Active
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Also Published As
| Publication number | Publication date |
|---|---|
| US20150105401A1 (en) | 2015-04-16 |
| EP2379561B1 (en) | 2015-11-04 |
| CN102264743B (zh) | 2015-02-11 |
| US9814704B2 (en) | 2017-11-14 |
| CN102264743A (zh) | 2011-11-30 |
| US8877772B2 (en) | 2014-11-04 |
| CA2744498A1 (en) | 2010-06-17 |
| AU2009324894A1 (en) | 2011-11-24 |
| US9181247B2 (en) | 2015-11-10 |
| JP5873544B2 (ja) | 2016-03-01 |
| EP2379561A4 (en) | 2012-10-03 |
| EP3037421A3 (en) | 2016-11-30 |
| US20120053175A1 (en) | 2012-03-01 |
| JP2012509903A (ja) | 2012-04-26 |
| WO2010068483A3 (en) | 2010-09-30 |
| US20160024087A1 (en) | 2016-01-28 |
| US20160317509A1 (en) | 2016-11-03 |
| JP2015052009A (ja) | 2015-03-19 |
| AU2009324894B2 (en) | 2015-04-09 |
| CA2744498C (en) | 2017-10-24 |
| WO2010068483A2 (en) | 2010-06-17 |
| JP5930278B2 (ja) | 2016-06-08 |
| EP3037421A1 (en) | 2016-06-29 |
| EP2379561A2 (en) | 2011-10-26 |
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