JP6317319B2 - 上皮成長因子受容体キナーゼ阻害剤の固体形態 - Google Patents
上皮成長因子受容体キナーゼ阻害剤の固体形態 Download PDFInfo
- Publication number
- JP6317319B2 JP6317319B2 JP2015500563A JP2015500563A JP6317319B2 JP 6317319 B2 JP6317319 B2 JP 6317319B2 JP 2015500563 A JP2015500563 A JP 2015500563A JP 2015500563 A JP2015500563 A JP 2015500563A JP 6317319 B2 JP6317319 B2 JP 6317319B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- solid form
- diffraction pattern
- solid
- peak
- 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.)
- Expired - Fee Related
Links
- HUFOZJXAKZVRNJ-UHFFFAOYSA-N CC(N(CC1)CCN1c(cc1)cc(OC)c1Nc1nc(Nc2cccc(NC(C=C)=O)c2)c(C(F)(F)F)cn1)=O Chemical compound CC(N(CC1)CCN1c(cc1)cc(OC)c1Nc1nc(Nc2cccc(NC(C=C)=O)c2)c(C(F)(F)F)cn1)=O HUFOZJXAKZVRNJ-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261611376P | 2012-03-15 | 2012-03-15 | |
| US61/611,376 | 2012-03-15 | ||
| PCT/US2013/030982 WO2013138495A1 (en) | 2012-03-15 | 2013-03-13 | Solid forms of an epidermal growth factor receptor kinase inhibitor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017222779A Division JP2018024713A (ja) | 2012-03-15 | 2017-11-20 | 上皮成長因子受容体キナーゼ阻害剤の固体形態 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015514060A JP2015514060A (ja) | 2015-05-18 |
| JP2015514060A5 JP2015514060A5 (enExample) | 2016-04-14 |
| JP6317319B2 true JP6317319B2 (ja) | 2018-04-25 |
Family
ID=49161778
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015500563A Expired - Fee Related JP6317319B2 (ja) | 2012-03-15 | 2013-03-13 | 上皮成長因子受容体キナーゼ阻害剤の固体形態 |
| JP2017222779A Withdrawn JP2018024713A (ja) | 2012-03-15 | 2017-11-20 | 上皮成長因子受容体キナーゼ阻害剤の固体形態 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017222779A Withdrawn JP2018024713A (ja) | 2012-03-15 | 2017-11-20 | 上皮成長因子受容体キナーゼ阻害剤の固体形態 |
Country Status (17)
| Country | Link |
|---|---|
| US (5) | US9056839B2 (enExample) |
| EP (1) | EP2825041B1 (enExample) |
| JP (2) | JP6317319B2 (enExample) |
| KR (1) | KR102081042B1 (enExample) |
| CN (2) | CN104302178B (enExample) |
| AU (2) | AU2016203338A1 (enExample) |
| BR (1) | BR112014022789B1 (enExample) |
| CA (1) | CA2866852C (enExample) |
| ES (1) | ES2880109T3 (enExample) |
| IL (1) | IL234425B (enExample) |
| IN (1) | IN2014DN07401A (enExample) |
| MX (1) | MX356753B (enExample) |
| MY (1) | MY169233A (enExample) |
| RU (1) | RU2673077C2 (enExample) |
| SG (2) | SG11201405691WA (enExample) |
| WO (1) | WO2013138495A1 (enExample) |
| ZA (1) | ZA201407441B (enExample) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| SG10201508958WA (en) | 2010-11-01 | 2015-11-27 | Celgene Avilomics Res Inc | Heterocyclic Compounds And Uses Thereof |
| CA2866857C (en) | 2012-03-15 | 2021-03-09 | Celgene Avilomics Research, Inc. | Salts of an epidermal growth factor receptor kinase inhibitor |
| JP6317319B2 (ja) * | 2012-03-15 | 2018-04-25 | セルジーン シーエーアール エルエルシー | 上皮成長因子受容体キナーゼ阻害剤の固体形態 |
| US9561228B2 (en) | 2013-02-08 | 2017-02-07 | Celgene Avilomics Research, Inc. | ERK inhibitors and uses thereof |
| WO2014182593A1 (en) * | 2013-05-06 | 2014-11-13 | Clovis Oncology, Inc. | Salts of an epidermal growth factor receptor kinase inhibitor |
| JP6453864B2 (ja) | 2013-10-02 | 2019-01-16 | スリーエム イノベイティブ プロパティズ カンパニー | ポリアクリレート感圧性プライマーと、ポリアクリレート成分を含む接着剤と、を含む物品 |
| CN105593275B (zh) | 2013-10-02 | 2020-10-30 | 3M创新有限公司 | 包括具有含氮聚合物的聚丙烯酸酯底漆的制品和方法 |
| NO2718543T3 (enExample) | 2014-02-04 | 2018-01-06 | ||
| US10005760B2 (en) | 2014-08-13 | 2018-06-26 | Celgene Car Llc | Forms and compositions of an ERK inhibitor |
| WO2016029002A2 (en) * | 2014-08-22 | 2016-02-25 | Clovis Oncology, Inc. | Growth factor receptor inhibitors |
| CN106999493A (zh) * | 2014-12-12 | 2017-08-01 | 默克专利股份公司 | 具有抗癌活性的6‑氧代‑1,6‑二氢‑哒嗪衍生物与egfr抑制剂的组合 |
| CN104961688A (zh) * | 2014-12-25 | 2015-10-07 | 苏州晶云药物科技有限公司 | 一种表皮生长因子受体激酶抑制剂的磷酸盐及其制备方法 |
| WO2016101912A1 (zh) * | 2014-12-25 | 2016-06-30 | 苏州晶云药物科技有限公司 | 一种表皮生长因子受体激酶抑制剂的盐的晶型及其制备方法 |
| US10494373B2 (en) * | 2015-04-29 | 2019-12-03 | Guangdong Zhongsheng Pharmaceutical Co., Ltd | Fused-ring or tricyclic aryl pyrimidine compound used as kinase inhibitor |
| CN106146406A (zh) * | 2016-02-23 | 2016-11-23 | 深圳市塔吉瑞生物医药有限公司 | 一种取代的二氨基嘧啶类化合物及包含该化合物的组合物及其用途 |
| CN107663208B (zh) * | 2016-07-27 | 2021-10-15 | 南京圣和药业股份有限公司 | 一种新型egfr激酶抑制剂的药用盐及其制备方法与用途 |
| CN107663207B (zh) * | 2016-07-27 | 2021-07-30 | 南京圣和药业股份有限公司 | 一种egfr激酶抑制剂的甲磺酸盐结晶及制备方法 |
| CN107955019B (zh) * | 2016-10-17 | 2021-09-14 | 广东众生药业股份有限公司 | 一种egfr抑制剂的盐型、晶型及其制备方法 |
| CN108299419B (zh) * | 2017-01-11 | 2022-04-26 | 南京圣和药业股份有限公司 | 一种新型egfr激酶抑制剂的几种新晶型及其制备方法 |
| EP3942045A1 (en) | 2019-03-21 | 2022-01-26 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| US12523663B2 (en) | 2019-06-04 | 2026-01-13 | Inserm (Institut National De La Santé Et De La Rescherche Médicale) | Use of CD9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
Family Cites Families (165)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1062357A (en) * | 1965-03-23 | 1967-03-22 | Pfizer & Co C | Quinazolone derivatives |
| US4337341A (en) * | 1976-11-02 | 1982-06-29 | Eli Lilly And Company | 4a-Aryl-octahydro-1H-2-pyrindines |
| GB8608335D0 (en) | 1986-04-04 | 1986-05-08 | Pfizer Ltd | Pharmaceutically acceptable salts |
| JPH0741461A (ja) | 1993-05-27 | 1995-02-10 | Eisai Co Ltd | スルホン酸エステル誘導体 |
| DE69630214T2 (de) | 1995-03-10 | 2004-07-15 | Berlex Laboratories, Inc., Richmond | Benzamidin-derivate, deren herstellung und deren verwendung als anti-koagulantien |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9619284D0 (en) | 1996-09-16 | 1996-10-30 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9622363D0 (en) | 1996-10-28 | 1997-01-08 | Celltech Therapeutics Ltd | Chemical compounds |
| AU1507199A (en) | 1997-12-15 | 1999-07-05 | Yamanouchi Pharmaceutical Co., Ltd. | Novel pyrimidine-5-carboxamide derivatives |
| US6303652B1 (en) | 1998-08-21 | 2001-10-16 | Hughes Institute | BTK inhibitors and methods for their identification and use |
| DE69933680T2 (de) | 1998-08-29 | 2007-08-23 | Astrazeneca Ab | Pyrimidine verbindungen |
| JP3635238B2 (ja) | 1998-11-10 | 2005-04-06 | 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 | Hivの複製を阻害するピリミジン類 |
| US6262088B1 (en) | 1998-11-19 | 2001-07-17 | Berlex Laboratories, Inc. | Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants |
| US6127376A (en) | 1998-12-04 | 2000-10-03 | Berlex Laboratories, Inc. | Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants |
| GB9828511D0 (en) | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| US6495558B1 (en) | 1999-01-22 | 2002-12-17 | Amgen Inc. | Kinase inhibitors |
| AU2871900A (en) | 1999-02-04 | 2000-08-25 | Millennium Pharmaceuticals, Inc. | G-protein coupled heptahelical receptor binding compounds and methods of use thereof |
| GB9914258D0 (en) | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| HRP20010969B1 (en) | 1999-06-29 | 2005-04-30 | Egis Gy�Gyszergy�R Rt. | Novel piperazinylalkylthiopyrimidine derivatives, |
| ATE449764T1 (de) | 1999-12-28 | 2009-12-15 | Pharmacopeia Inc | Cytokine, insbesondere tnf-alpha, hemmer |
| HUP0301117A3 (en) | 2000-02-17 | 2004-01-28 | Amgen Inc Thousand Oaks | Imidazole derivatives kinase inhibitors, their use, process for their preparation and pharmaceutical compositions containing them |
| GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004888D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| US7034019B2 (en) | 2000-05-08 | 2006-04-25 | Janssen Pharmaceutica N.V. | Prodrugs of HIV replication inhibiting pyrimidines |
| GB0016877D0 (en) | 2000-07-11 | 2000-08-30 | Astrazeneca Ab | Chemical compounds |
| CA2417500C (en) | 2000-07-28 | 2008-11-18 | Georgetown University Medical Center | Erbb-2 selective small molecule kinase inhibitors |
| US6908906B2 (en) * | 2001-02-09 | 2005-06-21 | Sankyo Company, Limited | Crystalline forms of pyrimidine nucleoside derivative |
| JP3748536B2 (ja) * | 2001-02-09 | 2006-02-22 | 三共株式会社 | ピリミジンヌクレオシド誘導体の結晶 |
| US6881737B2 (en) | 2001-04-11 | 2005-04-19 | Amgen Inc. | Substituted triazinyl acrylamide derivatives and methods of use |
| JO3429B1 (ar) | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | مشتقات برميدينات مثبطة فيروس الايدز |
| US6939874B2 (en) | 2001-08-22 | 2005-09-06 | Amgen Inc. | Substituted pyrimidinyl derivatives and methods of use |
| WO2003030909A1 (en) | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
| MXPA04004178A (es) | 2001-11-01 | 2004-09-06 | Janssen Pharmaceutica Nv | Heteroarilaminas como inhibidores de glucogeno cintasa cinasa 3beta. |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| WO2003066601A1 (en) | 2002-02-08 | 2003-08-14 | Smithkline Beecham Corporation | Pyrimidine compounds |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| JP2005534286A (ja) | 2002-03-21 | 2005-11-17 | サネシス ファーマシューティカルズ, インコーポレイテッド | キナーゼインヒビターの同定 |
| US20040002395A1 (en) | 2002-06-27 | 2004-01-01 | Poynor Raymond L. | Bridge weight for metal wood golf club |
| BR0313059B8 (pt) | 2002-07-29 | 2021-07-27 | Rigel Pharmaceuticals | composto, e, composição farmacêutica |
| CA2439440A1 (en) | 2002-09-05 | 2004-03-05 | Emory University | Treatment of tuberous sclerosis associated neoplasms |
| AU2002951853A0 (en) | 2002-10-04 | 2002-10-24 | Commonwealth Scientific And Industrial Research Organisation | Crystal structure of erbb2 and uses thereof |
| UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| PL227577B1 (pl) | 2003-02-07 | 2017-12-29 | Janssen Pharmaceutica Nv | Zastosowanie pochodnych pirymidyny do wytwarzania leku do zapobiegania zakażeniu wirusem HIV oraz kompozycja farmaceutyczna |
| DE602004021472D1 (en) | 2003-02-20 | 2009-07-23 | Smithkline Beecham Corp | Pyrimiidinverbindungen |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| US20050014753A1 (en) | 2003-04-04 | 2005-01-20 | Irm Llc | Novel compounds and compositions as protein kinase inhibitors |
| US20050043233A1 (en) | 2003-04-29 | 2005-02-24 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis |
| US7504396B2 (en) | 2003-06-24 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| CN102358738A (zh) | 2003-07-30 | 2012-02-22 | 里格尔药品股份有限公司 | 2,4-嘧啶二胺化合物及其预防和治疗自体免疫疾病的用途 |
| EP1663242B1 (en) | 2003-08-07 | 2011-04-27 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents |
| TWI378923B (en) | 2003-08-15 | 2012-12-11 | Novartis Ag | Pyrimidine derivatives |
| GB0321710D0 (en) | 2003-09-16 | 2003-10-15 | Novartis Ag | Organic compounds |
| BRPI0414544A (pt) | 2003-09-18 | 2006-11-07 | Novartis Ag | 2,4-di-(fenilamino) pirimidinas úteis no tratamento de transtornos proliferativos |
| JP2007514775A (ja) | 2003-12-19 | 2007-06-07 | ライジェル ファーマシューティカルズ, インコーポレイテッド | 1−(2,4−ピリミジンジアミノ)−2−シクロペンタンカルボキサイミド合成中間体の立体異性体および立体異性体混合物 |
| US20080207613A1 (en) | 2004-01-12 | 2008-08-28 | Cytopia Research Pty Ltd | Selective Kinase Inhibitors |
| CA2553729A1 (en) | 2004-01-16 | 2005-08-04 | Wyeth | Quinoline intermediates of receptor tyrosine kinase inhibitors and the synthesis thereof |
| WO2005092836A1 (en) | 2004-03-15 | 2005-10-06 | Eli Lilly And Company | Opioid receptor antagonists |
| WO2005105988A2 (en) | 2004-04-28 | 2005-11-10 | Vertex Pharmaceuticals Incorporated | Crystal structure of human jak3 kinase domain complex and binding pockets thereof |
| US7754714B2 (en) | 2004-05-18 | 2010-07-13 | Rigel Pharmaceuticals, Inc. | Cycloalkyl substituted pyrimidinediamine compounds and their uses |
| EP1598343A1 (de) | 2004-05-19 | 2005-11-23 | Boehringer Ingelheim International GmbH | 2-Arylaminopyrimidine als PLK Inhibitoren |
| EP3042964A1 (en) | 2004-06-04 | 2016-07-13 | Genentech, Inc. | Egfr mutations |
| US7521457B2 (en) | 2004-08-20 | 2009-04-21 | Boehringer Ingelheim International Gmbh | Pyrimidines as PLK inhibitors |
| GB0419161D0 (en) | 2004-08-27 | 2004-09-29 | Novartis Ag | Organic compounds |
| CA2581623A1 (en) | 2004-09-23 | 2006-03-30 | Reddy Us Therapeutics, Inc. | Novel pyridine compounds, process for their preparation and compositions containing them |
| US7531548B2 (en) | 2004-09-30 | 2009-05-12 | Tibotec Pharmaceuticals Ltd | HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines |
| EP1799652A1 (en) | 2004-10-13 | 2007-06-27 | Wyeth | N-benzenesulfonyl substituted anilino-pyrimidine analogs |
| EP1805208A2 (en) | 2004-10-20 | 2007-07-11 | Proteolix, Inc. | Labeled compounds for proteasome inhibition |
| WO2006053109A1 (en) | 2004-11-10 | 2006-05-18 | Synta Pharmaceuticals Corp. | Heteroaryl compounds |
| GB2420559B (en) | 2004-11-15 | 2008-08-06 | Rigel Pharmaceuticals Inc | Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses |
| JP5095409B2 (ja) | 2004-11-24 | 2012-12-12 | ライジェル ファーマシューティカルズ, インコーポレイテッド | スピロ2,4−ピリミジンジアミン化合物およびその使用 |
| MY169441A (en) | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
| CA2590110C (en) | 2004-12-30 | 2014-06-03 | Exelixis, Inc. | Kinase modulators and method of use |
| EP1856053A1 (en) | 2005-01-14 | 2007-11-21 | Millennium Pharmaceuticals, Inc. | Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity |
| JP4801096B2 (ja) | 2005-01-19 | 2011-10-26 | ライジェル ファーマシューティカルズ, インコーポレイテッド | 2,4−ピリミジンジアミン化合物のプロドラッグおよびそれらの使用 |
| EP2505591A1 (en) | 2005-02-11 | 2012-10-03 | Memorial Sloan-Kettering Cancer Center | Methods and compositions for detecting a drug resistant EGFR mutant |
| US20060247250A1 (en) | 2005-03-16 | 2006-11-02 | Targegen, Inc. | Pyrimidine inhibitors of kinases |
| DE102005016634A1 (de) | 2005-04-12 | 2006-10-19 | Merck Patent Gmbh | Neuartige Aza-Hetercyclen als Kinase-Inhibitoren |
| US20060270694A1 (en) | 2005-05-03 | 2006-11-30 | Rigel Pharmaceuticals, Inc. | JAK kinase inhibitors and their uses |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| WO2006128129A2 (en) | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating cancer |
| WO2006128172A2 (en) | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating b cell regulated autoimmune disorders |
| WO2006129100A1 (en) | 2005-06-03 | 2006-12-07 | Glaxo Group Limited | Novel compounds |
| EP1904457B1 (en) | 2005-06-08 | 2017-09-06 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| WO2007048064A2 (en) | 2005-10-21 | 2007-04-26 | Exelixis, Inc. | Amino-pyrimidines as casein kinase ii (ck2) modulators |
| US7528143B2 (en) | 2005-11-01 | 2009-05-05 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
| KR20080053954A (ko) | 2005-11-03 | 2008-06-16 | 아이알엠 엘엘씨 | 단백질 키나제 억제제 |
| US7713987B2 (en) | 2005-12-06 | 2010-05-11 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2,4-diamines and their uses |
| WO2007120339A1 (en) | 2005-12-19 | 2007-10-25 | Genentech, Inc. | Pyrimidine kinase inhibitors |
| TW200736232A (en) | 2006-01-26 | 2007-10-01 | Astrazeneca Ab | Pyrimidine derivatives |
| KR20080110998A (ko) | 2006-01-30 | 2008-12-22 | 엑셀리시스, 인코포레이티드 | Jak2 조절자로서 4아릴2아미노피리미딘 또는 4아릴2아미노알킬피리미딘 및 이들을 포함하는 약제학적 조성물 |
| JP4653842B2 (ja) | 2006-02-17 | 2011-03-16 | ライジェル ファーマシューティカルズ, インコーポレイテッド | 自己免疫疾患を治療または予防するための2,4−ピリミジンジアミン化合物 |
| JP2009528295A (ja) | 2006-02-24 | 2009-08-06 | ライジェル ファーマシューティカルズ, インコーポレイテッド | Jak経路の阻害のための組成物および方法 |
| EP2004632B1 (en) | 2006-03-30 | 2014-03-12 | Janssen R&D Ireland | Hiv inhibiting 5-amido substituted pyrimidines |
| CA2645959C (en) | 2006-03-30 | 2016-05-17 | Tibotec Pharmaceuticals Ltd. | Hiv inhibiting 5-(hydroxymethylene and aminomethylene) substituted pyrimidines |
| GB0608386D0 (en) | 2006-04-27 | 2006-06-07 | Senexis Ltd | Compounds |
| DE102006027156A1 (de) | 2006-06-08 | 2007-12-13 | Bayer Schering Pharma Ag | Sulfimide als Proteinkinaseinhibitoren |
| EP2043651A2 (en) | 2006-07-05 | 2009-04-08 | Exelixis, Inc. | Methods of using igf1r and abl kinase modulators |
| CA2657260A1 (en) | 2006-07-21 | 2008-01-24 | Novartis Ag | 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors |
| DE102006041382A1 (de) | 2006-08-29 | 2008-03-20 | Bayer Schering Pharma Ag | Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren |
| PL2526933T3 (pl) | 2006-09-22 | 2015-08-31 | Pharmacyclics Llc | Inhibitory kinazy tyrozynowej Brutona |
| ATE497496T1 (de) | 2006-10-19 | 2011-02-15 | Rigel Pharmaceuticals Inc | 2,4-pyridimediamon-derivate als hemmer von jak- kinasen zur behandlung von autoimmunerkrankungen |
| ES2403546T3 (es) | 2006-11-03 | 2013-05-20 | Pharmacyclics, Inc. | Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización |
| ES2380551T3 (es) | 2006-11-21 | 2012-05-16 | Rigel Pharmaceuticals, Inc. | Sales de profármaco de compuestos de 2,4-pirimidindiamina y sus usos |
| WO2008073687A2 (en) | 2006-12-08 | 2008-06-19 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| AU2007337088A1 (en) | 2006-12-19 | 2008-07-03 | Genentech, Inc. | Pyrimidine kinase inhibitors |
| EP1939185A1 (de) | 2006-12-20 | 2008-07-02 | Bayer Schering Pharma Aktiengesellschaft | Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs |
| CN106045965A (zh) | 2006-12-29 | 2016-10-26 | 爱尔兰詹森科学公司 | 抑制hiv的5,6‑取代的嘧啶类化合物 |
| US9006243B2 (en) | 2006-12-29 | 2015-04-14 | Janssen R&D Ireland | HIV inhibiting 6-substituted pyrimidines |
| TW200902010A (en) | 2007-01-26 | 2009-01-16 | Smithkline Beecham Corp | Anthranilamide inhibitors of aurora kinase |
| ES2702362T3 (es) | 2007-01-31 | 2019-02-28 | Ym Biosciences Australia Pty | Compuestos a base de tiopirimidina y usos de los mismos |
| JP4221470B2 (ja) | 2007-02-01 | 2009-02-12 | トヨタ自動車株式会社 | 電動車両制御装置及び電動車両制御方法 |
| DE102007010801A1 (de) | 2007-03-02 | 2008-09-04 | Bayer Cropscience Ag | Diaminopyrimidine als Fungizide |
| CN101686675A (zh) | 2007-03-20 | 2010-03-31 | 史密丝克莱恩比彻姆公司 | 化合物 |
| CN101677554A (zh) | 2007-03-20 | 2010-03-24 | 史密丝克莱恩比彻姆公司 | 化合物 |
| US7947698B2 (en) | 2007-03-23 | 2011-05-24 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| US7834024B2 (en) | 2007-03-26 | 2010-11-16 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| US20120065201A1 (en) | 2007-03-28 | 2012-03-15 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
| US20120101113A1 (en) | 2007-03-28 | 2012-04-26 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
| EP2152079A4 (en) | 2007-06-04 | 2011-03-09 | Avila Therapeutics Inc | HETEROCYCLIC COMPOUNDS AND USES THEREOF |
| CN101903357A (zh) | 2007-07-17 | 2010-12-01 | 里格尔药品股份有限公司 | 作为pkc抑制剂的环状胺取代的嘧啶二胺 |
| WO2009017838A2 (en) | 2007-08-01 | 2009-02-05 | Exelixis, Inc. | Combinations of jak-2 inhibitors and other agents |
| US20090088371A1 (en) | 2007-08-28 | 2009-04-02 | Rigel Pharmaceuticals, Inc. | Combination therapy with syk kinase inhibitor |
| WO2009032668A2 (en) | 2007-08-28 | 2009-03-12 | Irm Llc | 2 -biphenylamino-4 -aminopyrimidine derivatives as kinase inhibitors |
| WO2009032703A1 (en) | 2007-08-28 | 2009-03-12 | Irm Llc | 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors |
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| US7982036B2 (en) | 2007-10-19 | 2011-07-19 | Avila Therapeutics, Inc. | 4,6-disubstitued pyrimidines useful as kinase inhibitors |
| WO2009080638A2 (en) | 2007-12-20 | 2009-07-02 | Cellzome Limited | Sulfamides as zap-70 inhibitors |
| HRP20170050T1 (hr) | 2008-02-22 | 2017-03-10 | Rigel Pharmaceuticals, Inc. | Uporaba 2,4-pirimidindiamina za liječenje ateroskleroze |
| WO2009112490A1 (en) | 2008-03-11 | 2009-09-17 | Cellzome Limited | Sulfonamides as zap-70 inhibitors |
| US8205348B2 (en) | 2008-03-19 | 2012-06-26 | Zashiki-Warashi Manufacturing Inc. | Tile spacer and holder therefor |
| CL2009000600A1 (es) | 2008-03-20 | 2010-05-07 | Bayer Cropscience Ag | Uso de compuestos de diaminopirimidina como agentes fitosanitarios; compuestos de diaminopirimidina; su procedimiento de preparacion; agente que los contiene; procedimiento para la preparacion de dicho agente; y procedimiento para combatir plagas de animales y/u hongos dañinos patogenos de plantas. |
| WO2009127642A2 (en) | 2008-04-15 | 2009-10-22 | Cellzome Limited | Use of lrrk2 inhibitors for neurodegenerative diseases |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| CA2722326A1 (en) | 2008-04-24 | 2009-10-29 | Incyte Corporation | Macrocyclic compounds and their use as kinase inhibitors |
| EP2300013B2 (en) | 2008-05-21 | 2024-11-13 | Takeda Pharmaceutical Company Limited | Phosphorous derivatives as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| NZ603525A (en) | 2008-06-27 | 2015-02-27 | Celgene Avilomics Res Inc | Pyrimidine based compound and uses thereof |
| CA2730930C (en) | 2008-07-16 | 2015-01-13 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors |
| BRPI0918078A2 (pt) | 2008-09-03 | 2016-06-14 | Bayer Cropscience Ag | compostos de anilinopirimidinas substituídas com alcóxi e alquiltio e agentes para controlar fungos nocivos fitopatogênicos, processo para produção dos mesmos, bem como seus usos |
| WO2010077740A2 (en) | 2008-12-09 | 2010-07-08 | Cytokine Pharmasciences, Inc. | Novel antiviral compounds, compositions, and methods of use |
| WO2010081679A2 (en) | 2009-01-15 | 2010-07-22 | F. Hoffmann-La Roche Ag | Antibodies against human epo receptor |
| EP2414337B1 (en) | 2009-04-03 | 2013-05-01 | Cellzome GmbH | Methods for the identification of kinase interacting molecules and for the purification of kinase proteins |
| JP5918693B2 (ja) * | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Egfr阻害剤及び疾患の治療方法 |
| JP5364159B2 (ja) | 2009-05-08 | 2013-12-11 | アステラス製薬株式会社 | ジアミノへテロ環カルボキサミド化合物 |
| EP2443095A1 (en) | 2009-06-18 | 2012-04-25 | Cellzome Limited | Sulfonamides and sulfamides as zap-70 inhibitors |
| US7741330B1 (en) | 2009-10-12 | 2010-06-22 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase |
| US20110207736A1 (en) | 2009-12-23 | 2011-08-25 | Gatekeeper Pharmaceuticals, Inc. | Compounds that modulate egfr activity and methods for treating or preventing conditions therewith |
| WO2011140338A1 (en) | 2010-05-05 | 2011-11-10 | Gatekeeper Pharmaceuticals, Inc. | Compounds that modulate egfr activity and methods for treating or preventing conditions therewith |
| US20120071497A1 (en) | 2010-06-03 | 2012-03-22 | Pharmacyclics, Inc. | Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase |
| NZ772688A (en) | 2010-06-03 | 2022-09-30 | Pharmacyclics Llc | The use of inhibitors of bruton’s tyrosine kinase (btk) |
| WO2011153553A2 (en) | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
| CN105566229A (zh) * | 2010-08-10 | 2016-05-11 | 西建阿维拉米斯研究公司 | Btk抑制剂的苯磺酸盐及其用途和制备方法 |
| US9238629B2 (en) | 2010-11-01 | 2016-01-19 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| US20130317029A1 (en) | 2010-11-01 | 2013-11-28 | Portola Pharmaceuticals, Inc. | Oxypyrimidines as syk modulators |
| SG10201508958WA (en) | 2010-11-01 | 2015-11-27 | Celgene Avilomics Res Inc | Heterocyclic Compounds And Uses Thereof |
| EP2637502B1 (en) | 2010-11-10 | 2018-01-10 | Celgene CAR LLC | Mutant-selective egfr inhibitors and uses thereof |
| CN102558149A (zh) | 2010-12-29 | 2012-07-11 | 中国医学科学院药物研究所 | 嘧啶衍生物、及其制法和药物组合物与用途 |
| EP2704572B1 (en) | 2011-05-04 | 2015-12-30 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| HUE048834T2 (hu) | 2011-05-17 | 2020-08-28 | Univ California | Kináz inhibitorok |
| CN103159742B (zh) | 2011-12-16 | 2015-08-12 | 北京韩美药品有限公司 | 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用 |
| CA2866857C (en) | 2012-03-15 | 2021-03-09 | Celgene Avilomics Research, Inc. | Salts of an epidermal growth factor receptor kinase inhibitor |
| JP6317319B2 (ja) | 2012-03-15 | 2018-04-25 | セルジーン シーエーアール エルエルシー | 上皮成長因子受容体キナーゼ阻害剤の固体形態 |
| EP2914263A4 (en) | 2012-11-02 | 2016-04-27 | Pharmacyclics Inc | ADJUVANT THERAPY WITH TEC FAMILY KINASE INHIBITOR |
-
2013
- 2013-03-13 JP JP2015500563A patent/JP6317319B2/ja not_active Expired - Fee Related
- 2013-03-13 US US13/801,060 patent/US9056839B2/en active Active
- 2013-03-13 WO PCT/US2013/030982 patent/WO2013138495A1/en not_active Ceased
- 2013-03-13 CN CN201380023923.2A patent/CN104302178B/zh not_active Expired - Fee Related
- 2013-03-13 KR KR1020147028834A patent/KR102081042B1/ko not_active Expired - Fee Related
- 2013-03-13 SG SG11201405691WA patent/SG11201405691WA/en unknown
- 2013-03-13 MY MYPI2014002631A patent/MY169233A/en unknown
- 2013-03-13 CN CN201810628108.3A patent/CN108658873B/zh not_active Expired - Fee Related
- 2013-03-13 BR BR112014022789-6A patent/BR112014022789B1/pt not_active IP Right Cessation
- 2013-03-13 EP EP13760923.6A patent/EP2825041B1/en active Active
- 2013-03-13 CA CA2866852A patent/CA2866852C/en active Active
- 2013-03-13 MX MX2014010849A patent/MX356753B/es active IP Right Grant
- 2013-03-13 SG SG10201700804XA patent/SG10201700804XA/en unknown
- 2013-03-13 ES ES13760923T patent/ES2880109T3/es active Active
- 2013-03-13 RU RU2014136896A patent/RU2673077C2/ru active
-
2014
- 2014-09-02 IL IL234425A patent/IL234425B/en active IP Right Grant
- 2014-09-03 IN IN7401DEN2014 patent/IN2014DN07401A/en unknown
- 2014-10-14 ZA ZA2014/07441A patent/ZA201407441B/en unknown
-
2015
- 2015-06-09 US US14/734,279 patent/US9539255B2/en active Active
-
2016
- 2016-05-23 AU AU2016203338A patent/AU2016203338A1/en not_active Abandoned
-
2017
- 2017-01-09 US US15/401,663 patent/US10004741B2/en active Active
- 2017-11-20 JP JP2017222779A patent/JP2018024713A/ja not_active Withdrawn
-
2018
- 2018-03-16 AU AU2018201897A patent/AU2018201897B2/en not_active Ceased
- 2018-06-22 US US16/015,645 patent/US10946016B2/en active Active
-
2021
- 2021-03-12 US US17/200,019 patent/US20220062280A1/en not_active Abandoned
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US10946016B2 (en) | Solid forms of an epidermal growth factor receptor kinase inhibitor | |
| JP6676602B2 (ja) | 上皮成長因子受容体キナーゼ阻害剤の塩 | |
| HK1205431B (en) | Solid forms of an epidermal growth factor receptor kinase inhibitor |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20160224 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20160224 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20160808 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20160824 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20161122 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20170123 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20170223 |
|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20170719 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20171120 |
|
| A711 | Notification of change in applicant |
Free format text: JAPANESE INTERMEDIATE CODE: A712 Effective date: 20171221 |
|
| A911 | Transfer to examiner for re-examination before appeal (zenchi) |
Free format text: JAPANESE INTERMEDIATE CODE: A911 Effective date: 20180115 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20180223 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20180326 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20180329 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6317319 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| RD04 | Notification of resignation of power of attorney |
Free format text: JAPANESE INTERMEDIATE CODE: R3D04 |
|
| RD02 | Notification of acceptance of power of attorney |
Free format text: JAPANESE INTERMEDIATE CODE: R3D02 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| S111 | Request for change of ownership or part of ownership |
Free format text: JAPANESE INTERMEDIATE CODE: R313113 |
|
| R350 | Written notification of registration of transfer |
Free format text: JAPANESE INTERMEDIATE CODE: R350 |
|
| LAPS | Cancellation because of no payment of annual fees |