JP2015535851A5 - - Google Patents
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- Publication number
- JP2015535851A5 JP2015535851A5 JP2015535840A JP2015535840A JP2015535851A5 JP 2015535851 A5 JP2015535851 A5 JP 2015535851A5 JP 2015535840 A JP2015535840 A JP 2015535840A JP 2015535840 A JP2015535840 A JP 2015535840A JP 2015535851 A5 JP2015535851 A5 JP 2015535851A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- halogen
- independently selected
- compound
- 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.)
- Granted
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- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 72
- 229910052739 hydrogen Inorganic materials 0.000 claims description 66
- 239000001257 hydrogen Substances 0.000 claims description 66
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 42
- 150000002367 halogens Chemical class 0.000 claims description 37
- 229910052736 halogen Inorganic materials 0.000 claims description 34
- 150000001875 compounds Chemical class 0.000 claims description 28
- 150000002431 hydrogen Chemical class 0.000 claims description 24
- 125000000623 heterocyclic group Chemical group 0.000 claims description 22
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 18
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 15
- 125000006685 (C1-C6) polyhaloalkyl group Chemical group 0.000 claims description 15
- 241000124008 Mammalia Species 0.000 claims description 15
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 14
- 229910052799 carbon Inorganic materials 0.000 claims description 14
- 150000003973 alkyl amines Chemical class 0.000 claims description 12
- 125000004966 cyanoalkyl group Chemical group 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 9
- 208000027866 inflammatory disease Diseases 0.000 claims description 8
- 230000010261 cell growth Effects 0.000 claims description 7
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims description 6
- 102000001253 Protein Kinase Human genes 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- 125000001475 halogen functional group Chemical group 0.000 claims description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 6
- 108060006633 protein kinase Proteins 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 239000012453 solvate Substances 0.000 claims description 6
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims description 4
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 230000002917 arthritic effect Effects 0.000 claims description 4
- 206010003246 arthritis Diseases 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000037824 growth disorder Diseases 0.000 claims description 4
- 230000004663 cell proliferation Effects 0.000 claims description 3
- NOIXNOMHHWGUTG-UHFFFAOYSA-N 2-[[4-[4-pyridin-4-yl-1-(2,2,2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinoline Chemical group C=1C=C(OCC=2N=C3C=CC=CC3=CC=2)C=CC=1C1=NN(CC(F)(F)F)C=C1C1=CC=NC=C1 NOIXNOMHHWGUTG-UHFFFAOYSA-N 0.000 claims description 2
- 208000003950 B-cell lymphoma Diseases 0.000 claims description 2
- 208000028564 B-cell non-Hodgkin lymphoma Diseases 0.000 claims description 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims description 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims description 2
- 102100029823 Tyrosine-protein kinase BTK Human genes 0.000 claims description 2
- 101710086214 Tyrosine-protein kinase BTK Proteins 0.000 claims description 2
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims description 2
- 230000004064 dysfunction Effects 0.000 claims description 2
- 230000002757 inflammatory effect Effects 0.000 claims description 2
- 210000004698 lymphocyte Anatomy 0.000 claims description 2
- 201000008482 osteoarthritis Diseases 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 16
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 125000006684 polyhaloalkyl group Polymers 0.000 claims 3
- 238000000034 method Methods 0.000 description 14
- 0 CC(C1C2C(C3)C3C2)C1C1C*CC1 Chemical compound CC(C1C2C(C3)C3C2)C1C1C*CC1 0.000 description 5
- 125000006698 (C1-C3) dialkylamino group Chemical group 0.000 description 3
- 125000005700 haloalkyleneoxy group Chemical group 0.000 description 3
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261709534P | 2012-10-04 | 2012-10-04 | |
| US61/709,534 | 2012-10-04 | ||
| PCT/US2013/063555 WO2014055934A2 (en) | 2012-10-04 | 2013-10-04 | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015535851A JP2015535851A (ja) | 2015-12-17 |
| JP2015535851A5 true JP2015535851A5 (enExample) | 2016-11-24 |
| JP6313772B2 JP6313772B2 (ja) | 2018-04-18 |
Family
ID=50435583
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015535840A Expired - Fee Related JP6313772B2 (ja) | 2012-10-04 | 2013-10-04 | チロシン受容体キナーゼｂｔｋ阻害剤である置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9296703B2 (enExample) |
| EP (1) | EP2903971B1 (enExample) |
| JP (1) | JP6313772B2 (enExample) |
| KR (1) | KR20150067298A (enExample) |
| CN (1) | CN104822663B (enExample) |
| CA (1) | CA2887465A1 (enExample) |
| WO (1) | WO2014055934A2 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6147727B2 (ja) | 2011-04-01 | 2017-06-14 | ユニヴァーシティー オブ ユタ リサーチ ファウンデーション | チロシン受容体キナーゼｂｔｋ阻害剤としての置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体 |
| CA2887465A1 (en) | 2012-10-04 | 2014-04-10 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| JP6401169B2 (ja) | 2012-10-04 | 2018-10-03 | ユニヴァーシティー オブ ユタ リサーチ ファウンデーション | チロシン受容体キナーゼｂｔｋ阻害剤としての置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体 |
| KR102327917B1 (ko) | 2016-07-07 | 2021-11-17 | 주식회사 대웅제약 | 신규한 4-아미노피라졸로[3,4-d]피리미디닐아자바이사이클로 유도체 및 이를 포함하는 약학 조성물 |
| WO2019013562A1 (ko) | 2017-07-12 | 2019-01-17 | 주식회사 대웅제약 | 신규한 1h-피라졸로피리딘 유도체 및 이를 포함하는 약학 조성물 |
| KR102384924B1 (ko) | 2017-07-12 | 2022-04-08 | 주식회사 대웅제약 | 신규한 1h-피라졸로피리딘 유도체 및 이를 포함하는 약학 조성물 |
| KR102613433B1 (ko) | 2017-10-11 | 2023-12-13 | 주식회사 대웅제약 | 신규한 페닐피리딘 유도체 및 이를 포함하는 약학 조성물 |
| KR102328682B1 (ko) | 2018-08-27 | 2021-11-18 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| WO2020045941A1 (ko) | 2018-08-27 | 2020-03-05 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| JOP20220199A1 (ar) | 2020-02-26 | 2023-01-30 | Daewoong Pharmaceutical Co Ltd | طريقة لتحضير مشتقات أمين حلقي غير متجانس |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9924862D0 (en) | 1999-10-20 | 1999-12-22 | Celltech Therapeutics Ltd | Chemical compounds |
| JP2007500179A (ja) * | 2003-07-30 | 2007-01-11 | サイクラセル・リミテッド | キナーゼ阻害剤としての２−アミノフェニル−４−フェニルピリミジン |
| ATE499364T1 (de) | 2004-04-09 | 2011-03-15 | Merck Sharp & Dohme | Hemmer der akt aktivität |
| DK1951684T3 (en) | 2005-11-01 | 2016-10-24 | Targegen Inc | BIARYLMETAPYRIMIDIN kinase inhibitors |
| US8133900B2 (en) | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
| WO2007089768A2 (en) | 2006-01-30 | 2007-08-09 | Exelixis, Inc. | 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as jak-2 modulators and pharmaceutical compositions containing them |
| EA017269B1 (ru) | 2007-05-04 | 2012-11-30 | Айрм Ллк | ПРОИЗВОДНЫЕ ПИРИМИДИНА И СОДЕРЖАЩИЕ ИХ КОМПОЗИЦИИ КАК ИНГИБИТОРЫ КИНАЗЫ c-kit И PDGFR |
| WO2009032861A1 (en) * | 2007-09-04 | 2009-03-12 | The Scripps Research Institute | Substituted pyrimidinyl-amines as protein kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8426428B2 (en) | 2008-12-05 | 2013-04-23 | Principia Biopharma, Inc. | EGFR kinase knockdown via electrophilically enhanced inhibitors |
| CN102356075B (zh) | 2009-01-23 | 2015-06-10 | 里格尔药品股份有限公司 | 抑制jak途径的组合物和方法 |
| TW201041892A (en) | 2009-02-09 | 2010-12-01 | Supergen Inc | Pyrrolopyrimidinyl Axl kinase inhibitors |
| US9908884B2 (en) * | 2009-05-05 | 2018-03-06 | Dana-Farber Cancer Institute, Inc. | EGFR inhibitors and methods of treating disorders |
| US7741330B1 (en) | 2009-10-12 | 2010-06-22 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase |
| PT2693881T (pt) | 2011-04-01 | 2019-12-09 | Univ Utah Res Found | Análogos de n-fenilpirimidin-2-amina substituídos como inibidores da axl cinase |
| JP6147727B2 (ja) * | 2011-04-01 | 2017-06-14 | ユニヴァーシティー オブ ユタ リサーチ ファウンデーション | チロシン受容体キナーゼｂｔｋ阻害剤としての置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体 |
| SG10201604682VA (en) * | 2011-06-10 | 2016-07-28 | Merck Patent Gmbh | Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity |
| LT2734522T (lt) * | 2011-07-19 | 2019-02-11 | Merck Sharp & Dohme B.V. | 4-imidazopiridazin-1-il-benzamidai ir 4-imidazotriazin-1-il-benzamidai kaip btk-inhibitoriai |
| AU2012285988B2 (en) * | 2011-07-19 | 2017-05-25 | Merck Sharp & Dohme B.V. | 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides Btk-inhibitors |
| US8993756B2 (en) | 2011-12-06 | 2015-03-31 | Merck Sharp & Dohme Corp. | Pyrrolopyrimidines as janus kinase inhibitors |
| JP6401169B2 (ja) | 2012-10-04 | 2018-10-03 | ユニヴァーシティー オブ ユタ リサーチ ファウンデーション | チロシン受容体キナーゼｂｔｋ阻害剤としての置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体 |
| CA2887465A1 (en) | 2012-10-04 | 2014-04-10 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
-
2013
- 2013-10-04 CA CA 2887465 patent/CA2887465A1/en not_active Abandoned
- 2013-10-04 US US14/433,580 patent/US9296703B2/en not_active Expired - Fee Related
- 2013-10-04 WO PCT/US2013/063555 patent/WO2014055934A2/en not_active Ceased
- 2013-10-04 JP JP2015535840A patent/JP6313772B2/ja not_active Expired - Fee Related
- 2013-10-04 KR KR1020157011754A patent/KR20150067298A/ko not_active Withdrawn
- 2013-10-04 CN CN201380063031.5A patent/CN104822663B/zh not_active Expired - Fee Related
- 2013-10-04 EP EP13844062.3A patent/EP2903971B1/en not_active Not-in-force