JP2016501244A5 - - Google Patents
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- JP2016501244A5 JP2016501244A5 JP2015545859A JP2015545859A JP2016501244A5 JP 2016501244 A5 JP2016501244 A5 JP 2016501244A5 JP 2015545859 A JP2015545859 A JP 2015545859A JP 2015545859 A JP2015545859 A JP 2015545859A JP 2016501244 A5 JP2016501244 A5 JP 2016501244A5
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- Prior art keywords
- membered
- ring
- nitrogen
- sulfur
- oxygen
- Prior art date
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Families Citing this family (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2376485B1 (en) | 2008-12-19 | 2017-12-06 | Vertex Pharmaceuticals Incorporated | Pyrazine derivatives useful as inhibitors of atr kinase |
| EP2723746A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| KR102056586B1 (ko) | 2011-09-30 | 2019-12-18 | 버텍스 파마슈티칼스 인코포레이티드 | Ａｔｒ 억제제를 이용한 췌장암 및 비소세포 폐암의 치료 |
| BR112014007721B1 (pt) | 2011-09-30 | 2022-11-01 | Vertex Pharmaceuticals Incorporated | Processos para preparar compostos úteis como inibidores de atr quinase |
| AU2013243291B2 (en) | 2012-04-05 | 2018-02-01 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase and combination therapies thereof |
| LT3486245T (lt) | 2012-12-07 | 2021-08-25 | Vertex Pharmaceuticals Incorporated | 2-amino-n-(piperidin-1-il-piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamidas, kaip atr kinazės inhibitorius |
| US9278950B2 (en) | 2013-01-14 | 2016-03-08 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| AU2014207691B2 (en) | 2013-01-15 | 2018-08-30 | Incyte Holdings Corporation | Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors |
| EP2970288A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2014143241A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| JP2016512815A (ja) | 2013-03-15 | 2016-05-09 | 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縮合ピラゾロピリミジン誘導体 |
| WO2015027124A1 (en) | 2013-08-23 | 2015-02-26 | Incyte Corporation | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
| CA2932757C (en) * | 2013-12-06 | 2023-10-31 | 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 |
| AU2015271030B2 (en) * | 2014-06-05 | 2019-05-16 | Vertex Pharmaceuticals Incorporated | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo [1,5-a] pyrimidin-3-carboxamide compound useful as ATR kinase inhibitor, the preparation of said compound and different solid forms thereof |
| LT3157566T (lt) * | 2014-06-17 | 2019-08-12 | Vertex Pharmaceuticals Incorporated | Vėžio gydymo būdas, panaudojant chk1 ir atr inhibitorių derinį |
| WO2016010897A1 (en) * | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| TWI700283B (zh) | 2014-08-04 | 2020-08-01 | 德商拜耳製藥公司 | ２-(嗎啉-４-基)-１,７-萘啶 |
| CN107108581B (zh) * | 2014-08-21 | 2020-06-23 | 百时美施贵宝公司 | 作为强效rock抑制剂的回接苯甲酰胺衍生物 |
| IL252053B2 (en) | 2014-11-06 | 2024-04-01 | Lysosomal Therapeutics Inc | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| US20170333435A1 (en) | 2014-11-06 | 2017-11-23 | Lysosomal Therapeutics Inc. | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| CA2966581A1 (en) | 2014-11-06 | 2016-05-12 | Lysosomal Therapeutics Inc. | Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders |
| WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | Incyte Corporation | Pyridineamine compounds useful as pim kinase inhibitors |
| AR105967A1 (es) | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
| WO2017059357A1 (en) * | 2015-09-30 | 2017-04-06 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of dna damaging agents and atr inhibitors |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| IL260469B2 (en) * | 2016-01-08 | 2025-10-01 | The Institute Of Cancer Res Royal Cancer Hospital | Inhibitors of ataxia telangiectasia and rad3-related protein kinase (atr) mutations for use in cancer treatment methods |
| JP6918829B2 (ja) | 2016-01-11 | 2021-08-11 | メリマック ファーマシューティカルズ インコーポレーティッド | 血管拡張性失調症及びＲａｄ３関連タンパク質（ＡＴＲ）の阻害 |
| CN109071456A (zh) * | 2016-02-16 | 2018-12-21 | 麻省理工学院 | 作为myc调节剂的max结合剂及其用途 |
| CA3020305A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| MX2018012211A (es) | 2016-04-06 | 2019-03-28 | Lysosomal Therapeutics Inc | Compuestos de pirazol[1,5-a]pirimidinil carboxamida y su uso en el tratamiento de trastornos médicos. |
| EP3440081A4 (en) | 2016-04-06 | 2019-09-18 | Lysosomal Therapeutics Inc. | PYRROLO [1,2-A] PYRIMIDINYL-CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDER |
| WO2017192931A1 (en) | 2016-05-05 | 2017-11-09 | Lysosomal Therapeutics Inc. | SUBSTITUTED IMDAZO[1,2-α]PYRIDINES, SUBSTITUTED IMIDAZO[1,2-α]PYRAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| EP3452481A4 (en) | 2016-05-05 | 2020-02-26 | Lysosomal Therapeutics Inc. | IMIDAZO [1,2-B] SUBSTITUTED PYRIDAZINES, IMIDAZO [1,5-B] SUBSTITUTED PYRIDAZINES, RELATED COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL CONDITIONS |
| CN109890829B (zh) * | 2016-11-02 | 2022-07-15 | 豪夫迈·罗氏有限公司 | 作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物 |
| TW201840319A (zh) | 2017-02-24 | 2018-11-16 | 德商拜耳廠股份有限公司 | Atr激酶抑制劑與鐳-223鹽之組合 |
| JOP20190197A1 (ar) | 2017-02-24 | 2019-08-22 | Bayer Pharma AG | مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر |
| WO2018153972A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and antiandrogens |
| CN106946890A (zh) * | 2017-04-26 | 2017-07-14 | 中国药科大学 | 吡啶类irak4抑制剂、其制备方法及应用 |
| WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
| US10421765B2 (en) | 2017-05-26 | 2019-09-24 | Board Of Regents, The University Of Texas System | Tetrahydropyrido[4,3-d]pyrimidine inhibitors of ATR kinase |
| HRP20240368T1 (hr) | 2017-07-13 | 2024-08-30 | Board Of Regents, The University Of Texas System | Heterociklički inhibitori atr kinaze |
| DK3658557T3 (da) | 2017-07-28 | 2024-07-29 | Takeda Pharmaceuticals Co | Tyk2-inhibitorer og anvendelser deraf |
| US11690911B2 (en) | 2017-08-04 | 2023-07-04 | Bayer Aktiengesellschaft | Combination of ATR kinase inhibitors and PD-1/PD-L1 inhibitors |
| EP3668839B1 (en) | 2017-08-17 | 2023-04-12 | Board of Regents, The University of Texas System | Heterocyclic inhibitors of atr kinase |
| EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
| CN107935918A (zh) * | 2017-11-15 | 2018-04-20 | 山东潍坊润丰化工股份有限公司 | 一种百草枯的制备方法 |
| CN111417408B (zh) * | 2017-11-30 | 2024-04-23 | 思进公司 | 药物接头化合物的制备方法 |
| CA3084863A1 (en) | 2017-12-08 | 2019-06-13 | Bayer Aktiengesellschaft | Predictive markers for atr kinase inhibitors |
| US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| WO2019133711A1 (en) * | 2017-12-29 | 2019-07-04 | Vertex Pharmaceuticals Incorporated | Methods of cancer treatment using an atr inhibitor |
| WO2019178590A1 (en) | 2018-03-16 | 2019-09-19 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of atr kinase |
| CA3114024A1 (en) * | 2018-09-26 | 2020-04-02 | Merck Patent Gmbh | Combination of a pd-1 antagonist, an atr inhibitor and a platinating agent for the treatment of cancer |
| US20210369705A1 (en) | 2018-10-15 | 2021-12-02 | Merck Patent Gmbh | Combination therapy utilizing dna alkylating agents and atr inhibitors |
| CA3116230A1 (en) | 2018-10-16 | 2020-04-23 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds |
| CN112142744A (zh) | 2019-06-28 | 2020-12-29 | 上海瑛派药业有限公司 | 取代的稠合杂芳双环化合物作为激酶抑制剂及其应用 |
| WO2021178832A2 (en) * | 2020-03-06 | 2021-09-10 | The Henry M. Jackson Foundation For The Advancement Of Military Medicine, Inc. | Dna damage repair genes in cancer |
| WO2021187605A1 (ja) * | 2020-03-19 | 2021-09-23 | 田辺三菱製薬株式会社 | 含窒素複素環αシアノカルボニル化合物 |
| IL299179A (en) * | 2020-06-18 | 2023-02-01 | Merck Patent Gmbh | Atr inhibitors for use in treatment of viral infections |
| WO2022002243A1 (zh) * | 2020-07-02 | 2022-01-06 | 江苏恒瑞医药股份有限公司 | 咪唑并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| KR20230039675A (ko) * | 2020-07-13 | 2023-03-21 | 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 | Atr 키나제 억제제로 사용되는 피라졸로피리미딘 화합물 |
| CA3225945A1 (en) * | 2021-07-16 | 2023-01-19 | Tuan Trang | Sulfamoyl benzene derivatives and uses thereof |
| US20250042873A1 (en) * | 2021-08-24 | 2025-02-06 | The Johns Hopkins University | Compositions and methods for treating proteotoxicity-associated diseases |
| CN116283960A (zh) | 2021-12-21 | 2023-06-23 | 上海安诺达生物科技有限公司 | 取代的稠杂环化合物及其制备方法与应用 |
| WO2023116865A1 (zh) * | 2021-12-23 | 2023-06-29 | 优领医药科技（上海）有限公司 | 含吡唑类衍生物、其药学上可接受的盐及其制备方法和应用 |
| CN115322143B (zh) * | 2022-07-21 | 2023-07-14 | 安徽德诺医药股份有限公司 | 一种4-哌啶甲酸叔丁酯盐酸盐的制备方法 |
| US20250084085A1 (en) | 2023-08-01 | 2025-03-13 | Principia Biopharma Inc. | Process of making 2-[(3r)-2-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4[4-(oxetan-3-yl)piperazin-1-yl]-pent-2-enenitrile and solvate forms thereof |
Family Cites Families (265)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4309430A (en) | 1980-06-27 | 1982-01-05 | Merck & Co., Inc. | Pyrazinyl-1,2,4-oxadiazole-5-ones, for treatment of edema, and processes for preparing same |
| US5329012A (en) | 1987-10-29 | 1994-07-12 | The Research Foundation Of State University Of New York | Bis(acyloxmethyl)imidazole compounds |
| JP2597917B2 (ja) | 1990-04-26 | 1997-04-09 | 富士写真フイルム株式会社 | 新規な色素形成カプラー及びそれを用いたハロゲン化銀カラー写真感光材料 |
| JPH11506428A (ja) | 1995-05-09 | 1999-06-08 | ビーエーエスエフ アクチェンゲゼルシャフト | ピラゾロ［１，５ａ］ピリミジン、その製造方法およびその用途 |
| CA2253910A1 (en) | 1996-05-11 | 1997-11-20 | King's College London | Pyrazines |
| US6191131B1 (en) | 1997-07-23 | 2001-02-20 | Dupont Pharmaceuticals Company | Azolo triazines and pyrimidines |
| HU228962B1 (en) | 1996-07-24 | 2013-07-29 | Bristol Myers Squibb Pharma Co | Azolo triazines, pharmaceutical compositions containing them and use of the compounds |
| US6060478A (en) | 1996-07-24 | 2000-05-09 | Dupont Pharmaceuticals | Azolo triazines and pyrimidines |
| JPH10218881A (ja) | 1997-02-03 | 1998-08-18 | Pola Chem Ind Inc | 新規なピロロピラゾロピリミジン誘導体 |
| GB2323861B (en) | 1997-02-05 | 2001-06-20 | Sector Exhibiting Systems | Artificial wall structure |
| JP2002241379A (ja) | 1997-03-21 | 2002-08-28 | Dainippon Pharmaceut Co Ltd | ３−オキサジアゾリルキノキサリン誘導体 |
| US6235741B1 (en) | 1997-05-30 | 2001-05-22 | Merck & Co., Inc. | Angiogenesis inhibitors |
| WO1998054093A1 (en) | 1997-05-30 | 1998-12-03 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
| JP3910365B2 (ja) | 1998-07-16 | 2007-04-25 | 塩野義製薬株式会社 | 抗腫瘍活性を有するピリミジン誘導体 |
| US6245759B1 (en) | 1999-03-11 | 2001-06-12 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| US6660753B2 (en) | 1999-08-19 | 2003-12-09 | Nps Pharmaceuticals, Inc. | Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
| JP2001302666A (ja) | 1999-09-21 | 2001-10-31 | Nissan Chem Ind Ltd | アゾール縮合ヘテロ環アニライド化合物及び除草剤 |
| MY125533A (en) | 1999-12-06 | 2006-08-30 | Bristol Myers Squibb Co | Heterocyclic dihydropyrimidine compounds |
| US6608063B2 (en) | 1999-12-17 | 2003-08-19 | Chiron Corporation | Pyrazine based inhibitors of glycogen synthase kinase 3 |
| AU2001264932A1 (en) | 2000-05-26 | 2001-12-11 | Neurogen Corporation | Oxo-imidazopyrimidine-carboxamides and their use as gaba brain receptor ligands |
| US20020041880A1 (en) | 2000-07-05 | 2002-04-11 | Defeo-Jones Deborah | Method of treating cancer |
| US6849660B1 (en) | 2000-08-01 | 2005-02-01 | Isis Pharmaceuticals, Inc. | Antimicrobial biaryl compounds |
| US7067520B2 (en) | 2000-11-17 | 2006-06-27 | Ishihara Sangyo Kaisha, Ltd. | Preventive or therapeutic medicines for diabetes containing fused-heterocyclic compounds or their salts |
| EP1217000A1 (en) | 2000-12-23 | 2002-06-26 | Aventis Pharma Deutschland GmbH | Inhibitors of factor Xa and factor VIIa |
| US6420637B1 (en) | 2001-01-29 | 2002-07-16 | Asgrow Seed Company L.L.C. | Plants and seeds of corn variety I389972 |
| GB0103926D0 (en) | 2001-02-17 | 2001-04-04 | Astrazeneca Ab | Chemical compounds |
| WO2002089738A2 (en) | 2001-05-08 | 2002-11-14 | Yale University | Proteomimetic compounds and methods |
| US20030114467A1 (en) | 2001-06-21 | 2003-06-19 | Shakespeare William C. | Novel pyrazolo- and pyrrolo-pyrimidines and uses thereof |
| SE0102439D0 (sv) | 2001-07-05 | 2001-07-05 | Astrazeneca Ab | New compounds |
| SE0102438D0 (sv) | 2001-07-05 | 2001-07-05 | Astrazeneca Ab | New compounds |
| EP1506196B1 (en) | 2001-11-01 | 2012-01-18 | Icagen, Inc. | Pyrazolopyrimidines as sodium channel inhibitors |
| ES2333586T3 (es) | 2001-11-21 | 2010-02-24 | PHARMACIA & UPJOHN COMPANY LLC | Derivados de aril 1,4-pirazina sustituidos. |
| US6992087B2 (en) | 2001-11-21 | 2006-01-31 | Pfizer Inc | Substituted aryl 1,4-pyrazine derivatives |
| ES2437391T3 (es) | 2002-02-06 | 2014-01-10 | Vertex Pharmaceuticals, Inc. | Compuestos de heteroarilo útiles como inhibidores de GSK-3 |
| JP4725946B2 (ja) | 2002-03-13 | 2011-07-13 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ヒストンデアセチラーゼの新規な阻害剤としてのスルホニル誘導体 |
| GB0206860D0 (en) | 2002-03-22 | 2002-05-01 | Glaxo Group Ltd | Compounds |
| TWI319387B (en) | 2002-04-05 | 2010-01-11 | Astrazeneca Ab | Benzamide derivatives |
| BR0309475A (pt) * | 2002-04-23 | 2005-03-01 | Shionogi & Co | Derivados de pirazolo-[1,5-a]-pirimidina e inibidores de nad(p)h oxidase que contêm os mesmos |
| GB0209715D0 (en) | 2002-04-27 | 2002-06-05 | Astrazeneca Ab | Chemical compounds |
| US7704995B2 (en) | 2002-05-03 | 2010-04-27 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| CA2484209C (en) | 2002-05-03 | 2013-06-11 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| TW200406385A (en) | 2002-05-31 | 2004-05-01 | Eisai Co Ltd | Pyrazole compound and pharmaceutical composition containing the same |
| US7449488B2 (en) | 2002-06-04 | 2008-11-11 | Schering Corporation | Pyrazolopyrimidines as protein kinase inhibitors |
| ATE389656T1 (de) | 2002-06-04 | 2008-04-15 | Neogenesis Pharmaceuticals Inc | Pyrazolo(1,5-a)pyrimidin-verbindungen als antivirale agentien |
| AU2003249369A1 (en) | 2002-06-21 | 2004-01-06 | Cellular Genomics, Inc. | Certain amino-substituted monocycles as kinase modulators |
| ATE362474T1 (de) | 2002-09-04 | 2007-06-15 | Schering Corp | Pyrazolo(1,5-a)pyrimidine als hemmstoffe cyclin- abhängiger kinasen |
| CA2497440C (en) | 2002-09-04 | 2011-03-22 | Schering Corporation | Pyrazolopyrimidines as cyclin-dependent kinase inhibitors |
| EP1534710B1 (en) | 2002-09-04 | 2007-10-24 | Schering Corporation | Pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| US7205308B2 (en) | 2002-09-04 | 2007-04-17 | Schering Corporation | Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors |
| US8580782B2 (en) | 2002-09-04 | 2013-11-12 | Merck Sharp & Dohme Corp. | Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors |
| US7563798B2 (en) | 2002-09-04 | 2009-07-21 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| US7601724B2 (en) | 2002-09-04 | 2009-10-13 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| ATE364608T1 (de) | 2002-09-04 | 2007-07-15 | Schering Corp | Pyrazolopyrimidine als hemmstoffe cyclin- abhängiger kinasen |
| US7196092B2 (en) | 2002-09-04 | 2007-03-27 | Schering Corporation | N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| US7196078B2 (en) | 2002-09-04 | 2007-03-27 | Schering Corpoartion | Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| US7119200B2 (en) | 2002-09-04 | 2006-10-10 | Schering Corporation | Pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| US8673924B2 (en) | 2002-09-04 | 2014-03-18 | Merck Sharp & Dohme Corp. | Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors |
| AU2003282679A1 (en) | 2002-10-04 | 2004-05-04 | Arena Pharmaceuticals, Inc. | Hydroxypyrazoles for use against metabolic-related disorders |
| WO2004052315A2 (en) | 2002-12-11 | 2004-06-24 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| SE0203752D0 (sv) | 2002-12-17 | 2002-12-17 | Astrazeneca Ab | New compounds |
| SE0203754D0 (sv) | 2002-12-17 | 2002-12-17 | Astrazeneca Ab | New compounds |
| MXPA05009063A (es) | 2003-02-26 | 2005-12-12 | Sugen Inc | Compuestos de aminoheteroarilo como inhibidores de proteina cinasa. |
| KR20050115252A (ko) | 2003-02-28 | 2005-12-07 | 데이진 화-마 가부시키가이샤 | 피라졸로[1,5-ａ]피리미딘 유도체 |
| EP1606267B1 (en) | 2003-03-11 | 2008-07-30 | Pfizer Products Inc. | Pyrazine compounds as transforming growth factor (tgf) inhibitors |
| US7459454B2 (en) | 2003-03-21 | 2008-12-02 | Smithkline Beecham Corporation | Aminopyrazine derivatives and compositions |
| CN101468965A (zh) | 2003-03-24 | 2009-07-01 | 默克公司 | 联芳基取代的6元杂环钠通道阻滞剂 |
| GB2400101A (en) | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
| WO2004103279A2 (en) | 2003-05-15 | 2004-12-02 | Merck & Co., Inc. | 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists |
| TWI339206B (en) | 2003-09-04 | 2011-03-21 | Vertex Pharma | Compositions useful as inhibitors of protein kinases |
| BRPI0414533A (pt) | 2003-09-18 | 2006-11-07 | Conforma Therapeutics Corp | composto, composição farmacêutica, e, métodos para inibir um hsp90 e para tratar um indivìduo tendo um distúrbio mediado por hsp90 |
| US7807696B2 (en) | 2003-10-07 | 2010-10-05 | The Feinstein Institute For Medical Research | Isoxazole and isothiazole compounds useful in the treatment of inflammation |
| CN1905873A (zh) | 2003-11-19 | 2007-01-31 | 阵列生物制药公司 | Mek的杂环抑制剂及其使用方法 |
| DE10356579A1 (de) | 2003-12-04 | 2005-07-07 | Merck Patent Gmbh | Aminderivate |
| EP1715867A4 (en) | 2004-02-12 | 2009-04-15 | Merck & Co Inc | BIPYRIDYLAMIDE AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5 |
| US20070197389A1 (en) | 2004-02-25 | 2007-08-23 | Anja Schwogler | Azolopyrimidine compounds and use thereof for combating parasitic fungi |
| CA2563699C (en) | 2004-04-23 | 2014-03-25 | Exelixis, Inc. | Kinase modulators and method of use |
| WO2005123672A2 (en) | 2004-06-14 | 2005-12-29 | Takeda San Diego, Inc. | Kinase inhibitors |
| US7626021B2 (en) | 2004-07-27 | 2009-12-01 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
| JP2008508304A (ja) | 2004-07-27 | 2008-03-21 | エスジーエックス ファーマシューティカルズ、インコーポレイテッド | 縮合環ヘテロ環キナーゼ調節因子 |
| KR20070090172A (ko) | 2004-11-04 | 2007-09-05 | 버텍스 파마슈티칼스 인코포레이티드 | 단백질 키나아제의 억제제로서 유용한피라졸로[1,5-ａ]피리미딘 |
| US8003806B2 (en) | 2004-11-12 | 2011-08-23 | OSI Pharmaceuticals, LLC | Integrin antagonists useful as anticancer agents |
| AU2005309566A1 (en) | 2004-11-22 | 2006-06-01 | Vertex Pharmaceuticals Incorporated | Bicyclic inhibitors or Rho kinase |
| GB0428235D0 (en) | 2004-12-23 | 2005-01-26 | Glaxo Group Ltd | Novel compounds |
| JP2008525453A (ja) | 2004-12-27 | 2008-07-17 | アルコン，インコーポレイティド | 緑内障と、ｒｈｏキナーゼを媒介とした他の疾患および症状を治療するためのアミノピラジン・アナログ |
| US7635699B2 (en) | 2004-12-29 | 2009-12-22 | Bristol-Myers Squibb Company | Azolopyrimidine-based inhibitors of dipeptidyl peptidase IV and methods |
| GB0500492D0 (en) | 2005-01-11 | 2005-02-16 | Cyclacel Ltd | Compound |
| US7622583B2 (en) | 2005-01-14 | 2009-11-24 | Chemocentryx, Inc. | Heteroaryl sulfonamides and CCR2 |
| US20060156482A1 (en) | 2005-01-14 | 2006-07-20 | The Procter & Gamble Company | Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof |
| GB0501999D0 (en) | 2005-02-01 | 2005-03-09 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| CN101163692B (zh) | 2005-02-16 | 2012-01-18 | 先灵公司 | 具有cxcr3拮抗活性的杂环取代的哌嗪 |
| DE102005007534A1 (de) | 2005-02-17 | 2006-08-31 | Bayer Cropscience Ag | Pyrazolopyrimidine |
| CA2605738C (en) | 2005-04-25 | 2013-10-01 | Merck Patent Gesellschaft Mit Beschraenkter Haftung | Novel azaheterocyclic compounds as kinase inhibitors |
| EA013525B1 (ru) | 2005-05-20 | 2010-06-30 | Алантос-Фармасьютикалз Холдинг, Инк. | Гетеробициклические ингибиторы металлопротеазы и их применение |
| US20070155737A1 (en) | 2005-05-20 | 2007-07-05 | Alantos Pharmaceuticals, Inc. | Heterobicyclic metalloprotease inhibitors |
| US20070155738A1 (en) | 2005-05-20 | 2007-07-05 | Alantos Pharmaceuticals, Inc. | Heterobicyclic metalloprotease inhibitors |
| WO2007015632A1 (en) | 2005-08-04 | 2007-02-08 | Cgk Co., Ltd. | Atm and atr inhibitor |
| CN101321759A (zh) | 2005-10-06 | 2008-12-10 | 先灵公司 | 作为蛋白激酶抑制剂的吡唑并嘧啶化合物 |
| RU2008117298A (ru) | 2005-10-06 | 2009-11-20 | Шеринг Корпорейшн (US) | Пиразолопиримидины как ингибиторы протеинкиназ |
| US20070082900A1 (en) | 2005-10-06 | 2007-04-12 | Schering Corporation | Methods for inhibiting protein kinases |
| JP5102212B2 (ja) * | 2005-10-06 | 2012-12-19 | メルク・シャープ・アンド・ドーム・コーポレーション | プロテインキナーゼインヒビターとしてのピラゾロピリミジン |
| CA2626789A1 (en) | 2005-10-21 | 2007-04-26 | Exelixis, Inc. | Pyrimidinones as casein kinase ii (ck2) modulators |
| US8188097B2 (en) | 2005-10-21 | 2012-05-29 | Mitsubishi Tanabe Pharma Corporation | Pyrazolo[1,5-A]pyrimidine compounds |
| TW200736260A (en) | 2005-11-10 | 2007-10-01 | Smithkline Beecham Corp | Inhibitors of Akt activity |
| RU2396269C2 (ru) | 2005-12-01 | 2010-08-10 | Ф.Хоффманн-Ля Рош Аг | Производные гетероарилзамещенного пиперидина в качестве ингибиторов печеночной карнитин пальмитоилтрансферазы (l-cpt1) |
| US7871982B2 (en) | 2005-12-09 | 2011-01-18 | Meiji Seika Kaisha, Ltd. | Lincomycin derivatives and antimicrobial agents comprising the same as active ingredient |
| ZA200804497B (en) | 2005-12-22 | 2009-10-28 | Alcon Res Ltd | (Indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)-pyrazines for treating rho kinase-mediated diseases and conditions |
| ITMI20060311A1 (it) | 2006-02-21 | 2007-08-22 | Btsr Int Spa | Dispositivo perfezionato di alimentazione di filo o filatio ad una macchina tessile e metodo per attuare tale alimentazione |
| GB0603684D0 (en) | 2006-02-23 | 2006-04-05 | Novartis Ag | Organic compounds |
| WO2007096764A2 (en) | 2006-02-27 | 2007-08-30 | Glenmark Pharmaceuticals S.A. | Bicyclic heteroaryl derivatives as cannabinoid receptor modulators |
| TW200800203A (en) | 2006-03-08 | 2008-01-01 | Astrazeneca Ab | New use |
| NZ571933A (en) | 2006-03-22 | 2011-06-30 | Vertex Pharma | C-Met protein kinase inhibitors for the treatment of proliferative disorders |
| WO2007126841A2 (en) | 2006-03-29 | 2007-11-08 | Foldrx Pharmaceuticals, Inc. | Inhibition of alpha-synuclein toxicity |
| US7700601B2 (en) | 2006-03-31 | 2010-04-20 | Schering Corporation | Substituted indazoles of formula 1.0 that are kinase inhibitors |
| JP2009538304A (ja) | 2006-05-22 | 2009-11-05 | シェーリング コーポレイション | ＣＤＫ阻害剤としてのピラゾロ［１，５−ａ］ピリミジン |
| RU2009101911A (ru) | 2006-06-22 | 2010-07-27 | Биовитрум Аб (Пабл) (Se) | Производные пиридина и пиразина в качестве ингибиторов mnk-киназы |
| WO2007149478A2 (en) | 2006-06-22 | 2007-12-27 | Mallinckrodt Inc. | Pyrazine derivatives with extended conjugation and uses thereof |
| AR061793A1 (es) | 2006-07-05 | 2008-09-24 | Mitsubishi Tanabe Pharma Corp | Compuesto de pirazolo[1,5-a] pirimidina y composicion farmaceutica |
| US8217177B2 (en) | 2006-07-14 | 2012-07-10 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| PE20080403A1 (es) | 2006-07-14 | 2008-04-25 | Amgen Inc | Derivados heterociclicos fusionados y metodos de uso |
| US8198448B2 (en) | 2006-07-14 | 2012-06-12 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| KR20090073121A (ko) | 2006-09-29 | 2009-07-02 | 노파르티스 아게 | Ｐｉ3ｋ 지질 키나제 억제제로서의 피라졸로피리미딘 |
| GB0619342D0 (en) | 2006-09-30 | 2006-11-08 | Vernalis R&D Ltd | New chemical compounds |
| EP2074096B1 (en) | 2006-10-04 | 2012-06-27 | F. Hoffmann-La Roche AG | 3-pyridinecarboxamide and 2-pyrazinecarboxamide derivatives as hdl-cholesterol raising agents |
| MX337906B (es) | 2006-10-19 | 2016-03-28 | Signal Pharm Llc | Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas. |
| JP5244118B2 (ja) | 2006-11-10 | 2013-07-24 | ブリストル−マイヤーズ スクイブ カンパニー | 新規キナーゼ阻害剤 |
| US20080176870A1 (en) | 2006-11-20 | 2008-07-24 | Bert Nolte | Heterobicyclic metalloprotease inhibitors |
| CL2007003627A1 (es) | 2006-12-15 | 2008-07-25 | Bayer Schering Pharma Ag | Compuestos derivados de 3-h-pirazolopiridinas; metodo de preparacion; composicion farmaceutica; y uso para el tratamiento de enfermedades de crecimiento vascular desregulado tal como leucemia mielogena aguda, retinopatia, artritis reumatoide, psorias |
| CA2672438A1 (en) | 2006-12-20 | 2008-07-03 | Amgen Inc. | Substituted heterocycles and methods of use |
| PE20121126A1 (es) | 2006-12-21 | 2012-08-24 | Plexxikon Inc | Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa |
| GB0625659D0 (en) | 2006-12-21 | 2007-01-31 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| JP2010519204A (ja) | 2007-02-16 | 2010-06-03 | アムジエン・インコーポレーテツド | 窒素含有複素環ケトン類およびそれらのｃ−Ｍｅｔ阻害薬としての使用 |
| CA2679659C (en) | 2007-03-01 | 2016-01-19 | Novartis Ag | Pim kinase inhibitors and methods of their use |
| WO2008122375A2 (en) | 2007-04-10 | 2008-10-16 | Bayer Cropscience Ag | Insecticidal aryl isoxazoline derivatives |
| US20100234386A1 (en) | 2007-05-10 | 2010-09-16 | Chaudhari Amita | Quinoxaline derivatives as pi3 kinase inhibitors |
| PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| EP2014661A1 (de) | 2007-06-13 | 2009-01-14 | Bayer CropScience AG | Heterocyclisch substituierte Heterocyclyl-carbonsäurederivate |
| UY31137A1 (es) | 2007-06-14 | 2009-01-05 | Smithkline Beecham Corp | Derivados de quinazolina como inhibidores de la pi3 quinasa |
| WO2008156174A1 (ja) | 2007-06-21 | 2008-12-24 | Taisho Pharmaceutical Co., Ltd. | ピラジンアミド化合物 |
| MX2009013990A (es) | 2007-06-26 | 2010-03-30 | Lexicon Pharmaceuticals Inc | Metodos para tratar enfermedades y trastornos mediados por serotonina. |
| US20090012103A1 (en) | 2007-07-05 | 2009-01-08 | Matthew Abelman | Substituted heterocyclic compounds |
| WO2009006580A1 (en) | 2007-07-05 | 2009-01-08 | Cv Therapeutics, Inc. | Optionally condensed dihydropyridine, dihydropyrimidine and dihydropyrane derivatives acting as late sodium channel blockers |
| GB0713259D0 (en) | 2007-07-09 | 2007-08-15 | Astrazeneca Ab | Pyrazine derivatives 954 |
| EP2178865B1 (en) | 2007-07-19 | 2015-08-19 | Lundbeck, H., A/S | 5-membered heterocyclic amides and related compounds |
| NZ582708A (en) | 2007-07-19 | 2012-04-27 | Schering Corp | Heterocyclic amide compounds as protein kinase inhibitors |
| WO2009017954A1 (en) | 2007-08-01 | 2009-02-05 | Phenomix Corporation | Inhibitors of jak2 kinase |
| WO2009016460A2 (en) | 2007-08-01 | 2009-02-05 | Pfizer Inc. | Pyrazole compounds and their use as raf inhibitors |
| WO2009024825A1 (en) | 2007-08-21 | 2009-02-26 | Astrazeneca Ab | 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors |
| EP2203436A1 (en) | 2007-09-17 | 2010-07-07 | Neurosearch A/S | Pyrazine derivatives and their use as potassium channel modulators |
| JP2011500778A (ja) | 2007-10-25 | 2011-01-06 | アストラゼネカ・アクチエボラーグ | ピリジン及びピラジン誘導体−０８３ |
| CA2706946A1 (en) | 2007-11-28 | 2009-06-04 | Schering Corporation | 2-fluoropyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| WO2009075790A1 (en) | 2007-12-07 | 2009-06-18 | Alantos Pharmaceuticals Holding, Inc. | Metalloprotease inhibitors for intra-articular application |
| AU2008343173A1 (en) | 2007-12-19 | 2009-07-09 | Aj Park | Pyrazolo [1,5-a] pyrimidines useful as JAK2 inhibitors |
| KR101660050B1 (ko) | 2008-01-04 | 2016-09-26 | 인텔리카인, 엘엘씨 | 특정 화학 물질, 조성물 및 방법 |
| EP2085398A1 (en) | 2008-02-01 | 2009-08-05 | Merz Pharma GmbH & Co. KGaA | Pyrazolopyrimidines, a process for their preparation and their use as medicine |
| RU2010139284A (ru) | 2008-02-25 | 2012-04-10 | Ф.Хоффманн-Ля Рош Аг (Ch) | Пирролопиразины в качестве ингибиторов киназ |
| PT2247592E (pt) | 2008-02-25 | 2011-11-03 | Hoffmann La Roche | Inibidores de pirrolpirazina-cinase |
| JP5529049B2 (ja) | 2008-02-25 | 2014-06-25 | エフ．ホフマン−ラ ロシュ アーゲー | ピロロピラジンキナーゼ阻害剤 |
| ATE517107T1 (de) | 2008-02-25 | 2011-08-15 | Hoffmann La Roche | Pyrrolopyrazinkinaseinhibitoren |
| TW200940537A (en) | 2008-02-26 | 2009-10-01 | Astrazeneca Ab | Heterocyclic urea derivatives and methods of use thereof |
| AU2009226024B2 (en) | 2008-03-20 | 2012-07-12 | Amgen Inc. | Aurora kinase modulators and method of use |
| WO2009152087A1 (en) | 2008-06-10 | 2009-12-17 | Plexxikon, Inc. | Bicyclic heteroaryl compounds and methods for kinase modulation, and indications therefor |
| EP3009436B1 (en) | 2008-07-08 | 2019-06-05 | Intellikine, LLC | Kinase inhibitors and methods of use |
| GB0814364D0 (en) | 2008-08-05 | 2008-09-10 | Eisai London Res Lab Ltd | Diazaindole derivatives and their use in the inhibition of c-Jun N-terminal kinase |
| US8455477B2 (en) | 2008-08-05 | 2013-06-04 | Merck Sharp & Dohme Corp. | Therapeutic compounds |
| CN102223798A (zh) | 2008-09-24 | 2011-10-19 | 巴斯夫欧洲公司 | 用于防治无脊椎动物害虫的吡唑化合物 |
| WO2010048131A1 (en) | 2008-10-21 | 2010-04-29 | Vertex Pharmaceuticals Incorporated | C-met protein kinase inhibitors |
| MX2011004494A (es) | 2008-10-31 | 2011-05-24 | Genentech Inc | Compuestos de pirazolopirimidina inhibidores de jak y metodos. |
| EP2370424A1 (en) | 2008-11-10 | 2011-10-05 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2010059836A1 (en) | 2008-11-20 | 2010-05-27 | Decode Genetics Ehf | Substituted aza-bridged bicyclics for cardiovascular and cns disease |
| AU2009324894B2 (en) | 2008-11-25 | 2015-04-09 | University Of Rochester | MLK inhibitors and methods of use |
| KR101361858B1 (ko) | 2008-12-05 | 2014-02-12 | 에프. 호프만-라 로슈 아게 | 피롤로피라지닐 우레아 키나아제 저해제 |
| EP2376485B1 (en) * | 2008-12-19 | 2017-12-06 | Vertex Pharmaceuticals Incorporated | Pyrazine derivatives useful as inhibitors of atr kinase |
| RU2505540C2 (ru) | 2008-12-23 | 2014-01-27 | Эббви Инк. | Антивирусные соединения |
| WO2010086040A1 (en) | 2009-01-29 | 2010-08-05 | Biomarin Iga, Ltd. | Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy |
| EP2385036A4 (en) | 2009-01-30 | 2012-08-08 | Toyama Chemical Co Ltd | N-ACYL-ANTHRANILIC ACID DERIVATIVE OR SALT THEREOF |
| US20100204265A1 (en) | 2009-02-09 | 2010-08-12 | Genelabs Technologies, Inc. | Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections |
| AU2010214101A1 (en) | 2009-02-11 | 2011-09-01 | Sunovion Pharmaceuticals Inc. | Histamine H3 inverse agonists and antagonists and methods of use thereof |
| CN101537007A (zh) | 2009-03-18 | 2009-09-23 | 中国医学科学院血液病医院（血液学研究所） | N-(噻吩-2)吡唑并[1,5-a]嘧啶-3-甲酰胺类化合物在制备抗恶性肿瘤药物方面的应用 |
| US20120065247A1 (en) | 2009-03-27 | 2012-03-15 | Discoverybiomed, Inc. | Modulating ires-mediated translation |
| UA110324C2 (en) | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| JP2012533551A (ja) | 2009-07-15 | 2012-12-27 | アボット・ラボラトリーズ | ピロロピラジン系キナーゼ阻害薬 |
| NZ598220A (en) | 2009-08-17 | 2014-02-28 | Intellikine Llc | Heterocyclic compounds and uses thereof |
| WO2011025706A2 (en) | 2009-08-26 | 2011-03-03 | Schering Corporation | Heterocyclic amide compounds as protein kinase inhibitors |
| CN101671336B (zh) | 2009-09-23 | 2013-11-13 | 辽宁利锋科技开发有限公司 | 芳杂环并嘧啶衍生物和类似物及其制备方法和用途 |
| BR112012013508A2 (pt) | 2009-12-04 | 2019-09-24 | Cylene Pharmaceuticals Inc | pirazolopirimidinas e heterociclos relacionados como inibidores de ck2 |
| GB2550698B (en) | 2009-12-22 | 2018-04-11 | Intel Corp | Method and Apparatus to provide secure application execution |
| KR101732212B1 (ko) | 2010-03-18 | 2017-05-02 | 재단법인 한국파스퇴르연구소 | 항감염성 화합물 |
| US8518945B2 (en) | 2010-03-22 | 2013-08-27 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
| WO2011121096A1 (en) | 2010-03-31 | 2011-10-06 | Dkfz Deutsches Krebsforschungszentrum | PYRAZOL[1,5-a]PYRIMIDINE DERIVATIVES AS WNT PATHWAY ANTAGONISTS |
| JP2013523805A (ja) | 2010-04-08 | 2013-06-17 | ゾエティス・エルエルシー | 殺虫剤および殺ダニ剤としての置換３，５−ジフェニル−イソオキサゾリン誘導体 |
| US20130030237A1 (en) | 2010-04-15 | 2013-01-31 | Charles Theuer | Potentiation of anti-cancer activity through combination therapy with ber pathway inhibitors |
| CN102947272A (zh) | 2010-05-12 | 2013-02-27 | 沃泰克斯药物股份有限公司 | 用作atr激酶抑制剂的2-氨基吡啶衍生物 |
| US9630956B2 (en) | 2010-05-12 | 2017-04-25 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2011143425A2 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US9062008B2 (en) | 2010-05-12 | 2015-06-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| JP2013526539A (ja) | 2010-05-12 | 2013-06-24 | 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 | Ａｔｒキナーゼ阻害剤として有用なピラジン |
| JP2013526538A (ja) | 2010-05-12 | 2013-06-24 | 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 | Ａｔｒキナーゼ阻害剤として有用な化合物 |
| EP2571881A1 (en) | 2010-05-20 | 2013-03-27 | F.Hoffmann-La Roche Ag | Pyrrolopyrazine derivatives as syk and jak inhibitors |
| MX2012013378A (es) | 2010-05-20 | 2013-01-24 | Hoffmann La Roche | Derivados de pirrolo [2, 3-b] pirazina-7-carboxamida y sus uso como inhibidores de cinasa janus (jak) y cinasa tirosina del brazo (syk). |
| CA2803802A1 (en) | 2010-06-23 | 2011-12-29 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
| CN102958933B (zh) | 2010-06-24 | 2016-02-03 | 吉里德科学公司 | 作为抗病毒药的吡唑并[1,5-a]嘧啶类 |
| CN102311396B (zh) | 2010-07-05 | 2015-01-07 | 暨南大学 | 一种吡嗪类衍生物和其制备方法及在制药中的应用 |
| RU2604062C2 (ru) | 2010-07-13 | 2016-12-10 | Ф.Хоффманн-Ля Рош Аг | ПРОИЗВОДНЫЕ ПИРАЗОЛО[1,5-a]ПИРИМИДИНА И ТИЕНО[3,2-b]ПИРИМИДИНА В КАЧЕСТВЕ МОДУЛЯТОРОВ IRAK-4 |
| EP2407478A1 (en) | 2010-07-14 | 2012-01-18 | GENETADI Biotech, S.L. | New cyclotetrapeptides with pro-angiogenic properties |
| WO2012022045A1 (en) | 2010-08-20 | 2012-02-23 | Hutchison Medipharma Limited | Pyrrolopyrimidine compounds and uses thereof |
| EP2608669B1 (en) | 2010-08-23 | 2016-06-22 | Merck Sharp & Dohme Corp. | NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS |
| US8609669B2 (en) | 2010-11-16 | 2013-12-17 | Abbvie Inc. | Potassium channel modulators |
| MX343669B (es) | 2010-11-16 | 2016-11-16 | Array Biopharma Inc | Combinacion de inhibidores de la cinasa de control 1 inhibidores de la cinasa wee 1. |
| EP3366688B1 (en) | 2010-12-08 | 2022-02-09 | The U.S.A. as represented by the Secretary, Department of Health and Human Services | Substituted pyrazolopyrimidines as glucocerebrosidase activators |
| CA2825098C (en) | 2011-01-27 | 2020-03-10 | Universite De Montreal | Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators |
| MX2013011450A (es) | 2011-04-05 | 2014-02-03 | Vertex Pharma | Compuestos de aminopirazina utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr). |
| JP6005134B2 (ja) | 2011-04-21 | 2016-10-12 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | フルオロアルキル置換ピラゾロピリジンおよびその使用 |
| US9029389B2 (en) | 2011-04-21 | 2015-05-12 | Institut Pasteur Korea | Anti-inflammation compounds |
| EP2710006A1 (en) | 2011-05-17 | 2014-03-26 | Principia Biopharma Inc. | Azaindole derivatives as tyrosine kinase inhibitors |
| EP2723746A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| WO2012178123A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2012177997A1 (en) | 2011-06-22 | 2012-12-27 | The General Hospital Corporation | Treatment of proteinopathies |
| WO2012178124A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| KR20140048968A (ko) | 2011-07-13 | 2014-04-24 | 파마시클릭스, 인코포레이티드 | 브루톤형 티로신 키나제의 억제제 |
| WO2013052263A2 (en) | 2011-09-16 | 2013-04-11 | Microbiotix, Inc. | Antifungal compounds |
| KR102056586B1 (ko) | 2011-09-30 | 2019-12-18 | 버텍스 파마슈티칼스 인코포레이티드 | Ａｔｒ 억제제를 이용한 췌장암 및 비소세포 폐암의 치료 |
| CA2850564A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| BR112014007721B1 (pt) | 2011-09-30 | 2022-11-01 | Vertex Pharmaceuticals Incorporated | Processos para preparar compostos úteis como inibidores de atr quinase |
| WO2013049720A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2013049719A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| JP6073343B2 (ja) | 2011-10-20 | 2017-02-01 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ | サーチュイン調節因子としての置換された二環式アザ複素環およびアナログ |
| WO2013071094A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2013071085A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| EP2776422A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2013071088A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2013071093A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| US9193725B2 (en) | 2012-03-14 | 2015-11-24 | Bristol-Meyers Squibb Company | Cyclic hydrazine derivatives as HIV attachment inhibitors |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| KR20160046693A (ko) | 2012-04-02 | 2016-04-29 | 싸이토키네틱스, 인코포레이티드 | 횡격막 기능을 향상시키는 방법들 |
| AU2013243291B2 (en) | 2012-04-05 | 2018-02-01 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase and combination therapies thereof |
| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CN103373996A (zh) | 2012-04-20 | 2013-10-30 | 山东亨利医药科技有限责任公司 | 作为crth2受体拮抗剂的二并环衍生物 |
| KR102341637B1 (ko) | 2012-05-15 | 2021-12-21 | 캔써 리서치 테크놀로지 리미티드 | 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도 |
| CN104507481B (zh) | 2012-05-23 | 2017-08-04 | 萨维拉制药有限公司 | 用于治疗、改善或预防病毒疾病的7‑氧代‑4,7‑二氢‑吡唑并[1,5‑a]嘧啶衍生物 |
| CN104334563B (zh) | 2012-05-23 | 2017-03-08 | 萨维拉制药有限公司 | 7‑氧代‑噻唑并吡啶碳酸衍生物和它们在治疗、改善或预防病毒疾病中的用途 |
| WO2014011911A2 (en) | 2012-07-11 | 2014-01-16 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| WO2014015523A1 (en) | 2012-07-27 | 2014-01-30 | Hutchison Medipharma Limited | Novel heteroaryl and heterocycle compounds, compositions and methods |
| CN104619699A (zh) | 2012-08-06 | 2015-05-13 | 萨维拉制药有限公司 | 二羟基嘧啶碳酸衍生物以及它们在治疗、改善或预防病毒疾病中的用途 |
| EP2895472B1 (en) | 2012-08-09 | 2016-11-23 | VIIV Healthcare UK (No.5) Limited | Tricyclic alkene derivatives as HIV attachment inhibitors |
| EP2895475B1 (en) | 2012-08-09 | 2016-11-09 | VIIV Healthcare UK (No.5) Limited | Tricyclic amidine derivatives as hiv attachment inhibitors |
| US9505752B2 (en) | 2012-08-09 | 2016-11-29 | Viiv Healthcare Uk (No. 5) Limited | Piperidine amide derivatives as HIV attachment inhibitors |
| CN104718206B (zh) | 2012-08-17 | 2017-03-08 | 拜尔农作物科学股份公司 | 作为杀虫剂和杀螨剂的氮杂吲哚甲酰胺和氮杂吲哚硫代甲酰胺 |
| BR112015002950A2 (pt) | 2012-08-24 | 2017-08-08 | Hoffmann La Roche | novos derivados de bicíclico-piridina |
| WO2014035140A2 (en) | 2012-08-30 | 2014-03-06 | Kainos Medicine, Inc. | Compounds and compositions for modulating histone methyltransferase activity |
| US9475816B2 (en) | 2012-09-07 | 2016-10-25 | Takeda Pharmaceutical Company Limited | Substituted-1,4-dihydropyrazolo[4,3-b]indoles |
| WO2014042433A2 (en) | 2012-09-14 | 2014-03-20 | Kainos Medicine, Inc. | Compounds and compositions for modulating adenosine a3 receptor activity |
| TW201412740A (zh) | 2012-09-20 | 2014-04-01 | Bayer Pharma AG | 經取代之吡咯并嘧啶胺基苯并噻唑酮 |
| EP2897618B1 (en) | 2012-09-24 | 2021-11-17 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| US8999632B2 (en) | 2012-10-04 | 2015-04-07 | Vertex Pharmaceuticals Incorporated | Method for measuring ATR inhibition mediated increases in DNA damage |
| EP2909214B1 (en) | 2012-10-22 | 2020-07-22 | City of Hope | Etp derivatives |
| WO2014066552A1 (en) | 2012-10-24 | 2014-05-01 | Becton, Dickinson And Company | Hydroxamate substituted azaindoline-cyanine dyes and bioconjugates of the same |
| LT3486245T (lt) | 2012-12-07 | 2021-08-25 | Vertex Pharmaceuticals Incorporated | 2-amino-n-(piperidin-1-il-piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamidas, kaip atr kinazės inhibitorius |
| EP2970288A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| JP2016512815A (ja) | 2013-03-15 | 2016-05-09 | 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縮合ピラゾロピリミジン誘導体 |
| WO2014143241A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| CA2932757C (en) | 2013-12-06 | 2023-10-31 | 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 |
| US20150158868A1 (en) | 2013-12-06 | 2015-06-11 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| AU2015271030B2 (en) | 2014-06-05 | 2019-05-16 | Vertex Pharmaceuticals Incorporated | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo [1,5-a] pyrimidin-3-carboxamide compound useful as ATR kinase inhibitor, the preparation of said compound and different solid forms thereof |
| LT3157566T (lt) | 2014-06-17 | 2019-08-12 | Vertex Pharmaceuticals Incorporated | Vėžio gydymo būdas, panaudojant chk1 ir atr inhibitorių derinį |
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