JP2013526541A5 - - Google Patents
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- JP2013526541A5 JP2013526541A5 JP2013510300A JP2013510300A JP2013526541A5 JP 2013526541 A5 JP2013526541 A5 JP 2013526541A5 JP 2013510300 A JP2013510300 A JP 2013510300A JP 2013510300 A JP2013510300 A JP 2013510300A JP 2013526541 A5 JP2013526541 A5 JP 2013526541A5
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- Prior art keywords
- alkyl
- compound according
- aliphatic
- cancer
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Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2743134A1 (en) | 2008-11-10 | 2010-05-14 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| PT3354650T (pt) | 2008-12-19 | 2022-06-20 | Vertex Pharma | Compostos úteis como inibidores da cinase atr |
| EP2569287B1 (en) | 2010-05-12 | 2014-07-09 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| CA2798760A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | 2-aminopyridine derivatives useful as inhibitors of atr kinase |
| US9630956B2 (en) | 2010-05-12 | 2017-04-25 | 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 |
| US8962631B2 (en) | 2010-05-12 | 2015-02-24 | 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 |
| CA2803802A1 (en) | 2010-06-23 | 2011-12-29 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
| CA2832100A1 (en) | 2011-04-05 | 2012-10-11 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of tra kinase |
| 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 |
| JP2014522818A (ja) | 2011-06-22 | 2014-09-08 | 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 |
| CN103946221B (zh) * | 2011-09-16 | 2016-08-03 | 诺华股份有限公司 | 用于治疗囊性纤维化的杂环化合物 |
| JP6162126B2 (ja) | 2011-09-30 | 2017-08-23 | 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阻害剤による膵臓癌及び非小細胞肺癌の治療 |
| KR20140084112A (ko) | 2011-09-30 | 2014-07-04 | 버텍스 파마슈티칼스 인코포레이티드 | Ａｔｒ 키나제의 억제제로서 유용한 화합물 |
| US8853217B2 (en) | 2011-09-30 | 2014-10-07 | 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 |
| HUE046429T2 (hu) | 2011-09-30 | 2020-03-30 | Vertex Pharma | ATR kináz inhibítoraként használható vegyületek elõállítására szolgáló eljárás |
| EP2776422A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | 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 |
| WO2013071085A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Pyrazine 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 |
| WO2013071094A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| HK1205028A1 (en) | 2012-04-05 | 2015-12-11 | 沃泰克斯药物股份有限公司 | Compounds useful as inhibitors of atr kinase and combination therapies thereof |
| US20140085316A1 (en) * | 2012-09-25 | 2014-03-27 | Avaya Inc. | Follow me notification and widgets |
| US8999632B2 (en) | 2012-10-04 | 2015-04-07 | 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 |
| BR112015007312A2 (pt) | 2012-12-03 | 2017-08-08 | Hoffmann La Roche | composto, composição farmacêutica, utilização de um composto, método para o tratamento de câncer e invenção |
| US9340546B2 (en) | 2012-12-07 | 2016-05-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| RU2644769C2 (ru) | 2013-01-23 | 2018-02-14 | Астразенека Аб | Химические соединения |
| US9663519B2 (en) | 2013-03-15 | 2017-05-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| 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 |
| CN107074863B (zh) | 2014-06-05 | 2019-12-03 | 沃泰克斯药物股份有限公司 | Atr激酶抑制剂的制备方法及其不同的固体形式 |
| CA2950780C (en) | 2014-06-17 | 2023-05-16 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of chk1 and atr 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 |
| PL3330259T3 (pl) | 2015-07-27 | 2021-02-08 | Chong Kun Dang Pharmaceutical Corp. | Związek pochodna amidowa 1,3,4-oksadiazolu jako inhibitor deacetylazy histonowej 6 i kompozycja farmaceutyczna go zawierająca |
| ES2935932T3 (es) | 2015-07-27 | 2023-03-13 | Chong Kun Dang Pharmaceutical Corp | Compuestos de derivados de 1,3,4-oxadiazolsulfonamida como inhibidor de histona desacetilasa 6, y la composición farmacéutica que comprende los mismos |
| US10464911B2 (en) | 2015-07-27 | 2019-11-05 | Chong Kun Dang Pharmaceutical Corp. | 1,3,4-oxadiazole sulfamide derivative compounds as histone deacetylase 6 inhibitor, and the pharmaceutical composition comprising the same |
| EP3331864B1 (en) | 2015-08-04 | 2021-11-03 | Chong Kun Dang Pharmaceutical Corp. | 1,3,4-oxadiazole derivative compounds as histone deacetylase 6 inhibitor, and the pharmaceutical composition comprising the same |
| HK1258570A1 (zh) | 2015-09-30 | 2019-11-15 | Vertex Pharmaceuticals Inc. | 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法 |
| MX384527B (es) | 2015-10-12 | 2025-03-14 | Chong Kun Dang Pharmaceutical Corp | Compuestos derivados de oxadiazolamina como inhibidores de histona desacetilasa 6, y la composición farmacéutica que comprende los mismos |
| FI3936153T3 (fi) | 2016-01-11 | 2024-11-21 | Celator Pharmaceuticals Inc | Ataksia-teleangiektasia ja rad3 liitännäisen proteiinin (atr) estäminen |
| 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 |
| 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 |
| EP3575301A4 (en) | 2017-03-16 | 2020-08-05 | Jiangsu Hengrui Medicine Co., Ltd. | HETEROARYL [4,3-C] PYRIMIDINE-5-AMINE DERIVATIVE, PROCESS FOR PREPARATION AND MEDICAL USES |
| WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
| EP3661560B1 (en) | 2017-08-04 | 2025-02-26 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and pd-1/pd-l1 inhibitors |
| EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
| WO2019110586A1 (en) | 2017-12-08 | 2019-06-13 | Bayer Aktiengesellschaft | Predictive markers for atr kinase inhibitors |
| KR102316234B1 (ko) | 2018-07-26 | 2021-10-22 | 주식회사 종근당 | 히스톤 탈아세틸화효소 6 억제제로서의 1,3,4-옥사다이아졸 유도체 화합물 및 이를 포함하는 약제학적 조성물 |
| MX2021003263A (es) | 2018-09-26 | 2021-05-12 | Merck Patent Gmbh | Combinacion de un antagonista de proteina de muerte programada 1 (pd-1), un inhibidor de ataxia telangiectasia y proteina relacionada con rad3 (atr) y un agente de platino para el tratamiento de cancer. |
| CN113164447A (zh) | 2018-10-15 | 2021-07-23 | 默克专利股份公司 | 利用dna烷化剂和atr抑制剂的组合疗法 |
| CA3116230A1 (en) | 2018-10-16 | 2020-04-23 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds |
| AU2020284606B2 (en) | 2019-05-31 | 2023-01-19 | Chong Kun Dang Pharmaceutical Corp. | 1,3,4-oxadiazole homophthalimide derivative compounds as histone deacetylase 6 inhibitor, and the pharmaceutical composition comprising the same |
| CN113354631B (zh) * | 2021-06-01 | 2022-11-18 | 江苏大学 | 一种1,3,4-噁二唑衍生物及其制备方法和用途 |
| WO2025231259A1 (en) | 2024-05-01 | 2025-11-06 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor m1 |
Family Cites Families (218)
| 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 |
| JPS62270623A (ja) | 1985-12-07 | 1987-11-25 | Daicel Chem Ind Ltd | ビス（４−アミノフエニル）ピラジンおよびその製法、ならびにポリイミドおよびその製法 |
| JPS63208520A (ja) | 1987-02-26 | 1988-08-30 | Terumo Corp | ピラジン誘導体を含有する血小板凝集抑制剤 |
| US5329012A (en) | 1987-10-29 | 1994-07-12 | The Research Foundation Of State University Of New York | Bis(acyloxmethyl)imidazole compounds |
| JPH0272370A (ja) | 1988-09-07 | 1990-03-12 | Konica Corp | 電子写真感光体 |
| JPH0272372A (ja) | 1988-09-07 | 1990-03-12 | Konica Corp | 電子写真感光体 |
| JPH0374370A (ja) | 1989-08-16 | 1991-03-28 | Terumo Corp | ピラジン誘導体およびこれを含有する血小板凝集抑制剤または抗炎症剤 |
| 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 |
| US5572248A (en) | 1994-09-19 | 1996-11-05 | Teleport Corporation | Teleconferencing method and system for providing face-to-face, non-animated teleconference environment |
| CA2253910A1 (en) | 1996-05-11 | 1997-11-20 | King's College London | Pyrazines |
| JP4026876B2 (ja) | 1996-09-05 | 2007-12-26 | 日本食品化工株式会社 | 発光性シクロデキストリン誘導体及びその製造方法 |
| 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 |
| WO1999044609A1 (en) | 1998-03-03 | 1999-09-10 | Merck & Co., Inc. | FUSED PIPERIDINE SUBSTITUTED ARYLSULFONAMIDES AS β3-AGONISTS |
| DE19826671A1 (de) | 1998-06-16 | 1999-12-23 | Hoechst Schering Agrevo Gmbh | 1,3-Oxazolin- und 1,3-Thiazolin-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel |
| AU748816B2 (en) | 1998-07-16 | 2002-06-13 | Shionogi & Co., Ltd. | Pyrimidine derivatives exhibiting antitumor activity |
| US7023913B1 (en) | 2000-06-14 | 2006-04-04 | Monroe David A | Digital security multimedia sensor |
| ATE330968T1 (de) | 1999-02-05 | 2006-07-15 | Debiopharm Sa | Cyclosporin-derivate und verfahren zu deren herstellung |
| US6738073B2 (en) | 1999-05-12 | 2004-05-18 | Imove, Inc. | Camera system with both a wide angle view and a high resolution view |
| US6479504B1 (en) | 1999-06-16 | 2002-11-12 | The University Of Iowa Research Foundation | Antagonism of immunostimulatory CpG-oligonucleotides by 4-aminoquinolines and other weak bases |
| US7015954B1 (en) | 1999-08-09 | 2006-03-21 | Fuji Xerox Co., Ltd. | Automatic video system using multiple cameras |
| US6660753B2 (en) | 1999-08-19 | 2003-12-09 | Nps Pharmaceuticals, Inc. | Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
| CN1272328C (zh) | 1999-12-17 | 2006-08-30 | 希龙公司 | 糖元合成酶激酶3的基于吡嗪的抑制剂 |
| US6849660B1 (en) | 2000-08-01 | 2005-02-01 | Isis Pharmaceuticals, Inc. | Antimicrobial biaryl compounds |
| JP2002072370A (ja) | 2000-08-29 | 2002-03-12 | Fuji Photo Optical Co Ltd | ペーパーマガジン及び写真焼付装置 |
| JP2002072372A (ja) | 2000-09-04 | 2002-03-12 | Fuji Photo Film Co Ltd | 画像形成用シート体の切断装置 |
| US6829391B2 (en) | 2000-09-08 | 2004-12-07 | Siemens Corporate Research, Inc. | Adaptive resolution system and method for providing efficient low bit rate transmission of image data for distributed applications |
| EP1217000A1 (en) | 2000-12-23 | 2002-06-26 | Aventis Pharma Deutschland GmbH | Inhibitors of factor Xa and factor VIIa |
| US8085293B2 (en) | 2001-03-14 | 2011-12-27 | Koninklijke Philips Electronics N.V. | Self adjusting stereo camera system |
| US6759657B2 (en) | 2001-03-27 | 2004-07-06 | Kabushiki Kaisha Toshiba | Infrared sensor |
| JPWO2002080899A1 (ja) | 2001-03-30 | 2005-01-06 | エーザイ株式会社 | 消化器疾患治療剤 |
| US6469002B1 (en) | 2001-04-19 | 2002-10-22 | Millennium Pharmaceuticals, Inc. | Imidazolidine compounds |
| US6858600B2 (en) | 2001-05-08 | 2005-02-22 | Yale University | Proteomimetic compounds and methods |
| SE0102439D0 (sv) | 2001-07-05 | 2001-07-05 | Astrazeneca Ab | New compounds |
| SE0102438D0 (sv) | 2001-07-05 | 2001-07-05 | Astrazeneca Ab | New compounds |
| JP2003074370A (ja) | 2001-09-05 | 2003-03-12 | Suzuki Motor Corp | エンジンのベルト保護装置 |
| USRE40794E1 (en) | 2001-09-26 | 2009-06-23 | Merck & Co., Inc. | Crystalline forms of carbapenem antibiotics and methods of preparation |
| GB0124939D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| ATE447561T1 (de) | 2001-11-21 | 2009-11-15 | Pharmacia & Upjohn Co Llc | Substituierte aryl 1,4-pyrazin derivate |
| US6992087B2 (en) | 2001-11-21 | 2006-01-31 | Pfizer Inc | Substituted aryl 1,4-pyrazine derivatives |
| US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
| ES2437391T3 (es) | 2002-02-06 | 2014-01-10 | Vertex Pharmaceuticals, Inc. | Compuestos de heteroarilo útiles como inhibidores de GSK-3 |
| MXPA04007775A (es) | 2002-03-13 | 2004-10-15 | Janssen Pharmaceutica Nv | Derivados de sulfonilo como novedosos inhibidores de la histona desacetilasa. |
| GB0206860D0 (en) | 2002-03-22 | 2002-05-01 | Glaxo Group Ltd | Compounds |
| TWI319387B (en) | 2002-04-05 | 2010-01-11 | Astrazeneca Ab | Benzamide derivatives |
| US7043079B2 (en) | 2002-04-25 | 2006-05-09 | Microsoft Corporation | “Don't care” pixel interpolation |
| GB0209715D0 (en) | 2002-04-27 | 2002-06-05 | Astrazeneca Ab | Chemical compounds |
| AU2003234464B2 (en) | 2002-05-03 | 2009-06-04 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| US7704995B2 (en) | 2002-05-03 | 2010-04-27 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| JP4414881B2 (ja) | 2002-05-31 | 2010-02-10 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ピラゾール化合物およびこれを含んでなる医薬組成物 |
| AU2003249369A1 (en) | 2002-06-21 | 2004-01-06 | Cellular Genomics, Inc. | Certain amino-substituted monocycles as kinase modulators |
| WO2004000820A2 (en) | 2002-06-21 | 2003-12-31 | Cellular Genomics, Inc. | Certain aromatic monocycles as kinase modulators |
| WO2004033431A2 (en) | 2002-10-04 | 2004-04-22 | Arena Pharmaceuticals, Inc. | Hydroxypyrazoles for use against metabolic-related disorders |
| US20040075741A1 (en) | 2002-10-17 | 2004-04-22 | Berkey Thomas F. | Multiple camera image multiplexer |
| US7385626B2 (en) | 2002-10-21 | 2008-06-10 | Sarnoff Corporation | Method and system for performing surveillance |
| US20040100560A1 (en) | 2002-11-22 | 2004-05-27 | Stavely Donald J. | Tracking digital zoom in a digital video camera |
| SE0203754D0 (sv) | 2002-12-17 | 2002-12-17 | Astrazeneca Ab | New compounds |
| SE0203752D0 (sv) | 2002-12-17 | 2002-12-17 | Astrazeneca Ab | New compounds |
| DK2476667T3 (da) | 2003-02-26 | 2014-09-15 | Sugen Inc | Aminoheteroaryl-forbindelser som proteinkinase-inhibitorer |
| US7684624B2 (en) | 2003-03-03 | 2010-03-23 | Smart Technologies Ulc | System and method for capturing images of a target area on which information is recorded |
| CA2517720A1 (en) | 2003-03-11 | 2004-09-23 | Pfizer Products Inc. | Pyrazine compounds as transforming growth factor (tgf) inhibitors |
| EP1606266A4 (en) | 2003-03-21 | 2008-06-25 | Smithkline Beecham Corp | CHEMICAL COMPOUNDS |
| CN1791580A (zh) | 2003-03-24 | 2006-06-21 | 麦克公司 | 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 |
| GB2400514B (en) | 2003-04-11 | 2006-07-26 | Hewlett Packard Development Co | Image capture method |
| CN1788008A (zh) | 2003-05-15 | 2006-06-14 | 麦克公司 | 作为s1p受体激动剂的3－(2－氨基－1－氮杂环基)－5－芳基－1,2,4－噁二唑 |
| WO2004103991A1 (en) | 2003-05-20 | 2004-12-02 | 'chemical Diversity Research Institute', Ltd. | 2-substituted piperidines, focused library and a pharmaceutical compound |
| US20050123902A1 (en) | 2003-05-21 | 2005-06-09 | President And Fellows Of Harvard College | Human papillomavirus inhibitors |
| PE20050206A1 (es) | 2003-05-26 | 2005-03-26 | Schering Ag | Composicion farmaceutica que contiene un inhibidor de histona deacetilasa |
| US7986339B2 (en) | 2003-06-12 | 2011-07-26 | Redflex Traffic Systems Pty Ltd | Automated traffic violation monitoring and reporting system with combined video and still-image data |
| JP2005020227A (ja) | 2003-06-25 | 2005-01-20 | Pfu Ltd | 画像圧縮装置 |
| AR045595A1 (es) | 2003-09-04 | 2005-11-02 | Vertex Pharma | Composiciones utiles como inhibidores de proteinas quinasas |
| US7807696B2 (en) | 2003-10-07 | 2010-10-05 | The Feinstein Institute For Medical Research | Isoxazole and isothiazole compounds useful in the treatment of inflammation |
| US20050116968A1 (en) | 2003-12-02 | 2005-06-02 | John Barrus | Multi-capability display |
| EP1694670A1 (en) | 2003-12-16 | 2006-08-30 | GPC Biotech AG | Pyrazine derivatives as effective compounds against infectious diseases |
| AU2005215379A1 (en) | 2004-02-12 | 2005-09-01 | Merck & Co., Inc. | Bipyridyl amides as modulators of metabotropic glutamate receptor-5 |
| US20050276765A1 (en) | 2004-06-10 | 2005-12-15 | Paul Nghiem | Preventing skin damage |
| WO2005123672A2 (en) | 2004-06-14 | 2005-12-29 | Takeda San Diego, Inc. | Kinase inhibitors |
| BRPI0513899A (pt) | 2004-07-27 | 2008-05-20 | Sgx Pharmaceuticals Inc | moduladores de cinase heterocìclica de anel fundido |
| US7626021B2 (en) | 2004-07-27 | 2009-12-01 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
| MX2007001986A (es) | 2004-08-26 | 2007-05-10 | Pfizer | Compuestos de aminoheteroarilo como inhibidores de proteina quinasa. |
| ES2341351T3 (es) | 2004-08-26 | 2010-06-18 | Pfizer, Inc. | Compuestos de aminoheteroarilo enantiomericamente puros como inhibidores de proteina cinasas. |
| US7730406B2 (en) | 2004-10-20 | 2010-06-01 | Hewlett-Packard Development Company, L.P. | Image processing system and method |
| DE602005015742D1 (de) | 2004-10-22 | 2009-09-10 | Janssen Pharmaceutica Nv | Aromatische amide als hemmer der c-fms-kinase |
| EP1828144A2 (en) | 2004-11-12 | 2007-09-05 | OSI Pharmaceuticals, Inc. | Integrin antagonists useful as anticancer agents |
| AU2005309616A1 (en) | 2004-11-22 | 2006-06-01 | Vertex Pharmaceuticals Incorporated | Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases |
| JP4810669B2 (ja) | 2004-11-25 | 2011-11-09 | コニカミノルタホールディングス株式会社 | 有機エレクトロルミネッセンス素子、表示装置及び照明装置 |
| GB0428235D0 (en) | 2004-12-23 | 2005-01-26 | Glaxo Group Ltd | Novel compounds |
| AU2005322338B2 (en) | 2004-12-27 | 2011-06-09 | Alcon, Inc. | Aminopyrazine analogs for treating glaucoma and other rho kinase-mediated diseases |
| 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 |
| GB0501999D0 (en) | 2005-02-01 | 2005-03-09 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| WO2006088837A2 (en) | 2005-02-16 | 2006-08-24 | Schering Corporation | Heterocyclic substituted piperazines with cxcr3 antagonist activity |
| WO2006114180A1 (de) | 2005-04-25 | 2006-11-02 | Merck Patent Gmbh | Neuartige aza-heterozyklen als kinase-inhibitoren |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| AU2006258101A1 (en) | 2005-06-09 | 2006-12-21 | Merck Sharp & Dohme Corp. | Inhibitors of checkpoint kinases |
| CA2617413A1 (en) | 2005-08-02 | 2007-02-08 | Lexicon Pharmaceuticals, Inc. | 2-aminoaryl pyridines as protein kinases inhibitors |
| WO2007015632A1 (en) | 2005-08-04 | 2007-02-08 | Cgk Co., Ltd. | Atm and atr inhibitor |
| US7394926B2 (en) | 2005-09-30 | 2008-07-01 | Mitutoyo Corporation | Magnified machine vision user interface |
| US7806604B2 (en) | 2005-10-20 | 2010-10-05 | Honeywell International Inc. | Face detection and tracking in a wide field of view |
| TW200736260A (en) | 2005-11-10 | 2007-10-01 | Smithkline Beecham Corp | Inhibitors of Akt activity |
| EP1959951B1 (en) | 2005-12-01 | 2009-12-23 | F. Hoffmann-la Roche AG | Heteroaryl substituted piperidine derivatives as l-cpt1 inhibitors |
| US7871982B2 (en) | 2005-12-09 | 2011-01-18 | Meiji Seika Kaisha, Ltd. | Lincomycin derivatives and antimicrobial agents comprising the same as active ingredient |
| BRPI0620668A2 (pt) | 2005-12-14 | 2011-11-22 | Du Pont | composto da fórmula 1, composição que compreende composto, composição de controle de pragas invertebradas, composição de pulverização, composição de isca, dispositivo de armadilha, métodos de controle de pragas invertebradas, método de controle de baratas, formigas ou cupins e método de proteção de sementes contra pragas invertebradas |
| US7655662B2 (en) | 2005-12-22 | 2010-02-02 | Alcon Research, Ltd. | (Indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)-pyrazines for treating glaucoma and controlling intraocular pressure |
| PE20070978A1 (es) | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
| 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 |
| CN101479255B (zh) | 2006-03-22 | 2013-05-01 | 沃泰克斯药物股份有限公司 | 用于治疗增殖性病症的c-MET蛋白激酶抑制剂 |
| US7574131B2 (en) | 2006-03-29 | 2009-08-11 | Sunvision Scientific Inc. | Object detection system and method |
| MX2008012658A (es) | 2006-03-31 | 2008-12-16 | Schering Corp | Inhibidores de cinasa. |
| US7629346B2 (en) | 2006-06-19 | 2009-12-08 | Hoffmann-La Roche Inc. | Pyrazinecarboxamide derivatives as CB1 antagonists |
| CA2655857C (en) | 2006-06-22 | 2014-12-02 | Mallinckrodt Inc. | Pyrazine derivatives with extended conjugation and uses thereof |
| WO2007147874A1 (en) | 2006-06-22 | 2007-12-27 | Biovitrum Ab (Publ) | Pyridine and pyrazine derivatives as mnk kinase inhibitors |
| EP1900727A1 (en) | 2006-08-30 | 2008-03-19 | Cellzome Ag | Aminopyridine derivatives as kinase inhibitors |
| WO2008037477A1 (en) | 2006-09-29 | 2008-04-03 | Novartis Ag | Pyrazolopyrimidines as p13k lipid kinase inhibitors |
| GB0619342D0 (en) | 2006-09-30 | 2006-11-08 | Vernalis R&D Ltd | New chemical compounds |
| JP2010505789A (ja) | 2006-10-04 | 2010-02-25 | エフ．ホフマン−ラ ロシュ アーゲー | Ｈｄｌ−コレステロール上昇剤としての３−ピリジンカルボキサミド及び２−ピラジンカルボキサミド誘導体 |
| EP2090577B1 (en) | 2006-10-19 | 2017-04-05 | Signal Pharmaceuticals, LLC | Heteroaryl compounds, compositions thereof, and their use as protein kinase inhibitors |
| US8148361B2 (en) | 2006-11-10 | 2012-04-03 | Bristol-Myers Squibb Company | Kinase inhibitors |
| US20080132698A1 (en) | 2006-11-30 | 2008-06-05 | University Of Ottawa | Use of N-oxide compounds in coupling reactions |
| US20090062273A1 (en) | 2006-12-15 | 2009-03-05 | Ingo Hartung | 3-H-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same. |
| US7687522B2 (en) | 2006-12-20 | 2010-03-30 | Amgen Inc. | Substituted pyridines and pyrimidines and their use in treatment of cancer |
| GB0625659D0 (en) | 2006-12-21 | 2007-01-31 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| PE20081581A1 (es) | 2006-12-21 | 2008-11-12 | Plexxikon Inc | COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA |
| WO2008103277A2 (en) | 2007-02-16 | 2008-08-28 | Amgen Inc. | Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors |
| AU2008221263B2 (en) | 2007-03-01 | 2012-02-23 | Novartis Ag | Pim kinase inhibitors and methods of their use |
| JP2008260691A (ja) | 2007-04-10 | 2008-10-30 | Bayer Cropscience Ag | 殺虫性アリールイソオキサゾリン誘導体 |
| KR20090130064A (ko) | 2007-04-10 | 2009-12-17 | 바이엘 크롭사이언스 아게 | 살충성 아릴 이속사졸린 유도체 |
| PE20090288A1 (es) | 2007-05-10 | 2009-04-03 | Smithkline Beecham Corp | Derivados de quinoxalina como inhibidores de la pi3 quinasa |
| PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| UY31137A1 (es) | 2007-06-14 | 2009-01-05 | Smithkline Beecham Corp | Derivados de quinazolina como inhibidores de la pi3 quinasa |
| EP2012409A2 (en) | 2007-06-19 | 2009-01-07 | Hitachi, Ltd. | Rotating electrical machine |
| JP2009027904A (ja) | 2007-06-19 | 2009-02-05 | Hitachi Ltd | 回転電機 |
| EP2157090A4 (en) | 2007-06-21 | 2011-09-07 | Taisho Pharmaceutical Co Ltd | PYRAZINAMIDE COMPOUND |
| AU2008268494A1 (en) | 2007-06-26 | 2008-12-31 | Lexicon Pharmaceuticals, Inc. | Methods of treating serotonin-mediated diseases and disorders |
| US8461189B2 (en) | 2007-06-27 | 2013-06-11 | Merck Sharp & Dohme Corp. | Pyridyl derivatives as histone deacetylase inhibitors |
| GB0713259D0 (en) | 2007-07-09 | 2007-08-15 | Astrazeneca Ab | Pyrazine derivatives 954 |
| CN101801958B (zh) | 2007-07-19 | 2014-01-29 | 默沙东公司 | 作为蛋白质激酶抑制剂的杂环酰胺化合物 |
| ES2551095T3 (es) | 2007-07-19 | 2015-11-16 | Lundbeck, H., A/S | Amidas heterocíclicas de 5 miembros y compuestos relacionados |
| AP2010005167A0 (en) | 2007-08-01 | 2010-02-28 | Pfizer | 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 |
| AR068509A1 (es) | 2007-09-19 | 2009-11-18 | Jerini Ag | Antagosnistas del receptor de bradiquinina b1 |
| EP2215085B1 (en) * | 2007-10-25 | 2011-09-07 | AstraZeneca AB | Pyridine and pyrazine derivatives useful in the treatment of cell proliferative disorders |
| EP2265270A1 (en) | 2008-02-04 | 2010-12-29 | OSI Pharmaceuticals, Inc. | 2-aminopyridine kinase inhibitors |
| DK2250172T3 (da) | 2008-02-25 | 2012-01-16 | Hoffmann La Roche | Pyrrolopyrazinkinaseinhibitorer |
| ATE517107T1 (de) | 2008-02-25 | 2011-08-15 | Hoffmann La Roche | Pyrrolopyrazinkinaseinhibitoren |
| CA2713710A1 (en) | 2008-02-25 | 2009-09-03 | F. Hoffmann-La Roche Ag | Pyrrolopyrazine kinase inhibitors |
| CN101952296B (zh) | 2008-02-25 | 2013-08-21 | 霍夫曼-拉罗奇有限公司 | 吡咯并吡嗪激酶抑制剂 |
| TW200940537A (en) | 2008-02-26 | 2009-10-01 | Astrazeneca Ab | Heterocyclic urea derivatives and methods of use thereof |
| US20110003859A1 (en) | 2008-02-29 | 2011-01-06 | Array Biopharma Inc. | N- (6-aminopyridin-3-yl) -3- (sulfonamido) benzamide derivatives as b-raf inhibitors for the treatment of cancer |
| US8268834B2 (en) | 2008-03-19 | 2012-09-18 | Novartis Ag | Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme |
| US8110576B2 (en) | 2008-06-10 | 2012-02-07 | Plexxikon Inc. | Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications |
| 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 |
| ES2466565T3 (es) | 2008-08-06 | 2014-06-10 | Biomarin Pharmaceutical Inc. | Inhibidores dihidropiridoftalazinona de poli(ADP-ribosa)polimerasa (PARP) |
| CA2731368C (en) | 2008-08-06 | 2013-05-14 | Pfizer Inc. | 6 substituted 2-heterocyclylamino pyrazine compounds as chk-1 inhibitors |
| JP2010077286A (ja) | 2008-09-26 | 2010-04-08 | Aica Kogyo Co Ltd | シリコーン樹脂組成物および粘着フィルム |
| JP2012506381A (ja) | 2008-10-21 | 2012-03-15 | 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 | ｃ−ＭＥＴタンパク質キナーゼ阻害剤 |
| CA2743134A1 (en) | 2008-11-10 | 2010-05-14 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP3037421A3 (en) | 2008-11-25 | 2016-11-30 | University Of Rochester | Mlk inhibitors and methods of use |
| ES2464458T3 (es) | 2008-12-05 | 2014-06-02 | F. Hoffmann-La Roche Ag | Pirrolopirazinil-ureas como inhibidores de quinasas |
| PT3354650T (pt) | 2008-12-19 | 2022-06-20 | Vertex Pharma | Compostos úteis como inibidores da cinase atr |
| TW201028410A (en) | 2008-12-22 | 2010-08-01 | Astrazeneca Ab | Chemical compounds 610 |
| CA2748099C (en) | 2008-12-22 | 2017-02-28 | Array Biopharma Inc. | 7-phenoxychroman carboxylic acid derivatives |
| US8541424B2 (en) | 2008-12-23 | 2013-09-24 | Abbott Laboratories | Anti-viral compounds |
| TW201036946A (en) | 2009-01-30 | 2010-10-16 | Toyama Chemical Co Ltd | N-acylanthranilic acid derivative or salt thereof |
| JP5353279B2 (ja) | 2009-02-06 | 2013-11-27 | Ｊｎｃ株式会社 | セレンテラミド又はその類縁体の製造方法 |
| US8063032B2 (en) | 2009-02-11 | 2011-11-22 | 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 |
| EP2411007A4 (en) | 2009-03-27 | 2012-12-05 | Uab Research Foundation | MODULATION OF IRES-MEDIATED TRANSLATION |
| AU2010272769B2 (en) | 2009-07-13 | 2013-09-19 | T&W Engineering A/S | A hearing aid adapted for detecting brain waves and a method for adapting such a hearing aid |
| 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 |
| WO2011017513A1 (en) | 2009-08-07 | 2011-02-10 | Dow Agrosciences Llc | Pesticidal compositions |
| JP2011042639A (ja) | 2009-08-24 | 2011-03-03 | Kowa Co | ビフェニルピラジン化合物及びこれを有効成分として含有するエリスロポエチン産生促進剤 |
| 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 |
| DE102009043260A1 (de) | 2009-09-28 | 2011-04-28 | Merck Patent Gmbh | Pyridinyl-imidazolonderivate |
| IL295518B2 (en) | 2009-10-06 | 2023-11-01 | Millennium Pharm Inc | Heterocyclic compounds useful as pdk1 inhibitors |
| PL2526090T3 (pl) | 2010-01-18 | 2016-04-29 | Medicines For Malaria Venture Mmv | Nowe środki przeciwmalaryczne |
| US8518945B2 (en) | 2010-03-22 | 2013-08-27 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
| CN102933563A (zh) | 2010-04-08 | 2013-02-13 | Ah美国42有限责任公司 | 作为杀虫剂和杀螨剂的取代的3,5-二苯基异噁唑啉衍生物 |
| US20130030237A1 (en) | 2010-04-15 | 2013-01-31 | Charles Theuer | Potentiation of anti-cancer activity through combination therapy with ber pathway inhibitors |
| EP2566858A2 (en) | 2010-05-04 | 2013-03-13 | Pfizer Inc. | Heterocyclic derivatives as alk inhibitors |
| US8962631B2 (en) | 2010-05-12 | 2015-02-24 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| CA2798760A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | 2-aminopyridine derivatives useful as inhibitors of atr kinase |
| US9630956B2 (en) | 2010-05-12 | 2017-04-25 | 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 |
| EP2569287B1 (en) | 2010-05-12 | 2014-07-09 | Vertex Pharmaceuticals Inc. | 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 |
| RU2012152354A (ru) | 2010-05-20 | 2014-06-27 | Ф. Хоффманн-Ля Рош Аг | Производные пирролопиразина в качестве ингибиторов syk и jak |
| JP2013529204A (ja) | 2010-05-20 | 2013-07-18 | エフ．ホフマン−ラ ロシュ アーゲー | ピロロ［２，３−ｂ］ピラジン−７−カルボキサミド誘導体とＪＡＫ及びＳＹＫ及び阻害剤としてのそれらの使用 |
| CA2803802A1 (en) | 2010-06-23 | 2011-12-29 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
| 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 |
| EP2407478A1 (en) | 2010-07-14 | 2012-01-18 | GENETADI Biotech, S.L. | New cyclotetrapeptides with pro-angiogenic properties |
| JP5782238B2 (ja) | 2010-07-30 | 2015-09-24 | ルネサスエレクトロニクス株式会社 | 電圧検出回路及びその制御方法 |
| US8440652B2 (en) | 2011-03-04 | 2013-05-14 | Lexicon Pharmaceuticals, Inc. | MST1 kinase inhibitors and methods of their use |
| WO2012121939A2 (en) | 2011-03-04 | 2012-09-13 | Locus Pharmaceuticals, Inc. | Aminopyrazine compounds |
| CA2832100A1 (en) | 2011-04-05 | 2012-10-11 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of tra kinase |
| JP2014513728A (ja) | 2011-05-17 | 2014-06-05 | プリンシピア バイオファーマ インコーポレイテッド | チロシンキナーゼ阻害剤としてのアザインドール誘導体 |
| WO2012178123A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| JP2014522818A (ja) | 2011-06-22 | 2014-09-08 | 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 |
| EP2723746A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| HUE046429T2 (hu) | 2011-09-30 | 2020-03-30 | Vertex Pharma | ATR kináz inhibítoraként használható vegyületek elõállítására szolgáló eljárás |
| KR20140084112A (ko) | 2011-09-30 | 2014-07-04 | 버텍스 파마슈티칼스 인코포레이티드 | Ａｔｒ 키나제의 억제제로서 유용한 화합물 |
| JP6162126B2 (ja) | 2011-09-30 | 2017-08-23 | 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阻害剤による膵臓癌及び非小細胞肺癌の治療 |
| WO2013049719A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| 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 |
| US8846917B2 (en) | 2011-11-09 | 2014-09-30 | 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 |
| HK1205028A1 (en) | 2012-04-05 | 2015-12-11 | 沃泰克斯药物股份有限公司 | Compounds useful as inhibitors of atr kinase and combination therapies 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 |
| US8999632B2 (en) | 2012-10-04 | 2015-04-07 | 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 |
| JP6096005B2 (ja) | 2013-02-26 | 2017-03-15 | リンテック株式会社 | シート剥離装置および剥離方法 |
-
2011
- 2011-05-12 US US13/106,476 patent/US9630956B2/en not_active Expired - Fee Related
- 2011-05-12 SG SG2012083176A patent/SG185524A1/en unknown
- 2011-05-12 KR KR1020127032379A patent/KR20130066633A/ko not_active Withdrawn
- 2011-05-12 MX MX2012013081A patent/MX2012013081A/es active IP Right Grant
- 2011-05-12 AU AU2011253025A patent/AU2011253025A1/en not_active Abandoned
- 2011-05-12 NZ NZ603477A patent/NZ603477A/en not_active IP Right Cessation
- 2011-05-12 WO PCT/US2011/036246 patent/WO2011143426A1/en not_active Ceased
- 2011-05-12 CA CA2798763A patent/CA2798763A1/en not_active Abandoned
- 2011-05-12 EP EP11720956A patent/EP2569313A1/en not_active Withdrawn
- 2011-05-12 RU RU2012153675/04A patent/RU2012153675A/ru not_active Application Discontinuation
- 2011-05-12 JP JP2013510300A patent/JP5836367B2/ja not_active Expired - Fee Related
- 2011-05-12 CN CN2011800303808A patent/CN103228651A/zh active Pending
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- 2012-11-11 IL IL222968A patent/IL222968A0/en unknown
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