JP2016520131A5 - - Google Patents
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- JP2016520131A5 JP2016520131A5 JP2016516830A JP2016516830A JP2016520131A5 JP 2016520131 A5 JP2016520131 A5 JP 2016520131A5 JP 2016516830 A JP2016516830 A JP 2016516830A JP 2016516830 A JP2016516830 A JP 2016516830A JP 2016520131 A5 JP2016520131 A5 JP 2016520131A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- compound according
- alkyl
- heteroaryl
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims 15
- -1 substituted Chemical class 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- KDDQRKBRJSGMQE-UHFFFAOYSA-N 4-thiazolyl Chemical group [C]1=CSC=N1 KDDQRKBRJSGMQE-UHFFFAOYSA-N 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- CWDWFSXUQODZGW-UHFFFAOYSA-N 5-thiazolyl Chemical group [C]1=CN=CS1 CWDWFSXUQODZGW-UHFFFAOYSA-N 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010027480 Metastatic malignant melanoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000021039 metastatic melanoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- SNVLJLYUUXKWOJ-UHFFFAOYSA-N methylidenecarbene Chemical compound C=[C] SNVLJLYUUXKWOJ-UHFFFAOYSA-N 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 0 Cc(c(C**)c1F)ccc1N(*)S(*)(=O)=O Chemical compound Cc(c(C**)c1F)ccc1N(*)S(*)(=O)=O 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361829190P | 2013-05-30 | 2013-05-30 | |
| US61/829,190 | 2013-05-30 | ||
| PCT/US2014/040076 WO2014194127A1 (en) | 2013-05-30 | 2014-05-29 | Compounds for kinase modulation, and indications therefor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016520131A JP2016520131A (ja) | 2016-07-11 |
| JP2016520131A5 true JP2016520131A5 (OSRAM) | 2017-07-06 |
Family
ID=51023140
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016516830A Pending JP2016520131A (ja) | 2013-05-30 | 2014-05-29 | キナーゼ調節のための化合物、およびその適応 |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US9873700B2 (OSRAM) |
| EP (1) | EP3004060B1 (OSRAM) |
| JP (1) | JP2016520131A (OSRAM) |
| KR (1) | KR20160013028A (OSRAM) |
| CN (1) | CN105228983A (OSRAM) |
| AR (1) | AR096450A1 (OSRAM) |
| AU (1) | AU2014274093B2 (OSRAM) |
| BR (1) | BR112015028845A2 (OSRAM) |
| CA (1) | CA2912568A1 (OSRAM) |
| HK (1) | HK1219732A1 (OSRAM) |
| IL (1) | IL242587A0 (OSRAM) |
| MX (1) | MX2015015966A (OSRAM) |
| PH (1) | PH12015502610A1 (OSRAM) |
| RU (1) | RU2015149937A (OSRAM) |
| SG (1) | SG11201509338QA (OSRAM) |
| TW (1) | TW201533028A (OSRAM) |
| UY (1) | UY35596A (OSRAM) |
| WO (1) | WO2014194127A1 (OSRAM) |
Families Citing this family (100)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| BRPI0814423B1 (pt) | 2007-07-17 | 2022-04-19 | Plexxikon, Inc | Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos |
| WO2009143018A2 (en) | 2008-05-19 | 2009-11-26 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| EP2501236B1 (en) | 2009-11-18 | 2017-03-29 | Plexxikon Inc. | N-[2-fluoro-3-(4-amino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonyl)-phenyl]-4-benzenesulfonamide derivatives as Raf protein kinase modulators for the treatment of cancer |
| MX2012007429A (es) | 2009-12-23 | 2012-07-23 | Plexxikon Inc | Compuestos y metodos para la modulacion de quinasa e indicaciones de la misma. |
| TWI619713B (zh) | 2010-04-21 | 2018-04-01 | 普雷辛肯公司 | 用於激酶調節的化合物和方法及其適應症 |
| AU2012214762B2 (en) | 2011-02-07 | 2015-08-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CA2836474A1 (en) | 2011-05-17 | 2012-11-22 | Plexxikon Inc. | Kinase modulation and indications therefor |
| US9358235B2 (en) | 2012-03-19 | 2016-06-07 | Plexxikon Inc. | Kinase modulation, and indications therefor |
| RU2637948C2 (ru) * | 2012-05-03 | 2017-12-08 | Дженентек, Инк. | Производные пиразоламинопиримидина в качестве модуляторов обогащенной лейциновыми повторами киназы 2 (lrrk2) для применения при лечении болезни паркинсона |
| US9150570B2 (en) * | 2012-05-31 | 2015-10-06 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
| WO2014039714A2 (en) | 2012-09-06 | 2014-03-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| EP2912065A4 (en) | 2012-10-25 | 2016-10-19 | True North Therapeutics Inc | ANTI COMPLEMENT C1S ANTIBODIES AND USES THEREOF |
| BR112015014752B1 (pt) | 2012-12-21 | 2022-07-05 | Plexxikon, Inc | Compostos e seus uso para modulação de cinase |
| US20140303121A1 (en) | 2013-03-15 | 2014-10-09 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| RU2680100C9 (ru) | 2013-03-15 | 2019-04-18 | Плексксикон Инк. | Гетероциклические соединения и их применения |
| CA2912568A1 (en) | 2013-05-30 | 2014-12-04 | Plexxikon Inc. | Compounds for kinase modulation, and indications therefor |
| WO2015134536A1 (en) | 2014-03-04 | 2015-09-11 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| US9856259B2 (en) | 2014-09-15 | 2018-01-02 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| EP3265454B1 (en) * | 2015-03-02 | 2020-02-26 | Rigel Pharmaceuticals, Inc. | Tgf-beta inhibitors |
| US10160755B2 (en) | 2015-04-08 | 2018-12-25 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CN104829613B (zh) * | 2015-04-13 | 2020-06-09 | 赤峰蒙广生物科技有限公司 | 二芳基取代的吡唑并环类衍生物、其制备方法及其在医药领域的应用 |
| DK3292123T3 (da) | 2015-05-06 | 2020-08-17 | Plexxikon Inc | Faste former af en forbindelse, der modulerer kinaser |
| US9745298B2 (en) | 2015-05-06 | 2017-08-29 | Plexxikon Inc. | Synthesis of a compound that modulates kinases |
| BR112017025045A2 (pt) * | 2015-05-22 | 2018-08-07 | Plexxikon Inc | plx-8394 ou plx-7904 para uso no tratamento de doenças relacionadas a braf-v600 |
| TWI658042B (zh) * | 2015-05-22 | 2019-05-01 | 美商普雷辛肯公司 | 雜環化合物的合成 |
| DK3322706T3 (da) | 2015-07-16 | 2021-02-01 | Array Biopharma Inc | Substituerede pyrazolo[1,5-a]pyridin-forbindelser som ret-kinaseinhibitorer |
| US10829484B2 (en) | 2015-07-28 | 2020-11-10 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CA3129180A1 (en) | 2015-09-21 | 2017-03-30 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| JP2018534296A (ja) | 2015-10-26 | 2018-11-22 | ロクソ オンコロジー， インコーポレイテッドＬｏｘｏ Ｏｎｃｏｌｏｇｙ， Ｉｎｃ． | Ｔｒｋ阻害薬耐性がんにおける点変異およびそれに関連する方法 |
| MX2018006856A (es) | 2015-12-07 | 2018-08-01 | Plexxikon Inc | Compuestos y metodos para modulacion de la quinasa, e indicaciones de los mismos. |
| US9630968B1 (en) | 2015-12-23 | 2017-04-25 | Arqule, Inc. | Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof |
| JP6921846B6 (ja) | 2016-03-16 | 2021-09-15 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | キナーゼ調節およびその適応症のための化合物および方法 |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| RS65988B1 (sr) | 2016-04-04 | 2024-10-31 | Loxo Oncology Inc | Postupak lečenja pedijatrijskih karcinoma |
| MX386416B (es) | 2016-04-04 | 2025-03-18 | Loxo Oncology Inc | Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida. |
| HUE063877T2 (hu) | 2016-05-18 | 2024-02-28 | Loxo Oncology Inc | (S)-N-(5-((R)-2-(2,5-dlfluorofenil)pirolidin-1-il)plrazolo[1,5-A]pirimidin-3-il) -3-hidroxipirolidin-1-karboxamid elõállítása |
| CN109311894B (zh) * | 2016-06-21 | 2022-03-22 | 内尔维阿诺医学科学有限公司 | 作为激酶抑制剂的n-(取代的-苯基)-磺酰胺衍生物 |
| CN107722013B (zh) * | 2016-08-11 | 2021-01-12 | 中国科学院上海药物研究所 | 去氮嘌呤类化合物及其药物组合物、制备方法和用途 |
| RU2019108280A (ru) * | 2016-08-24 | 2020-09-25 | Аркьюл, Инк. | Аминопирролопиримидиноновые соединения и способы их применения |
| TW201815766A (zh) | 2016-09-22 | 2018-05-01 | 美商普雷辛肯公司 | 用於ｉｄｏ及ｔｄｏ調節之化合物及方法以及其適應症 |
| US20190263796A1 (en) | 2016-09-23 | 2019-08-29 | Cellipse | Lim kinase inhibitors, pharmaceutical composition and method of use in limk-mediated diseases |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| CA3047580A1 (en) | 2016-12-23 | 2018-07-26 | Plexxikon Inc. | Compounds and methods for cdk8 modulation and indications therefor |
| WO2018134254A1 (en) | 2017-01-17 | 2018-07-26 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| CA3049136C (en) | 2017-01-18 | 2022-06-14 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| AU2018237047A1 (en) | 2017-03-20 | 2019-10-17 | Plexxikon Inc. | Crystalline forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1H- pyrrolo[3,2-b]pyridin-3-yl)benzoic acid that inhibits bromodomain |
| US10428067B2 (en) | 2017-06-07 | 2019-10-01 | Plexxikon Inc. | Compounds and methods for kinase modulation |
| BR112019028235B1 (pt) | 2017-07-25 | 2024-04-30 | Plexxikon, Inc. | Composições e seus métodos de preparação |
| BR112020001935A2 (pt) * | 2017-07-29 | 2020-07-28 | Lutris Pharma Ltd | novos inibidores de braf e uso destes para o tratamento de reações cutâneas |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| US10717735B2 (en) | 2017-10-13 | 2020-07-21 | Plexxikon Inc. | Solid forms of a compound for modulating kinases |
| TWI803530B (zh) | 2017-10-27 | 2023-06-01 | 美商普雷辛肯公司 | 調節激酶之化合物之調配物 |
| CA3087354C (en) | 2018-01-18 | 2023-01-03 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| CA3087578C (en) | 2018-01-18 | 2023-08-08 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| WO2019142128A1 (en) * | 2018-01-18 | 2019-07-25 | Integral Biosciences Private Limited | Dual inhibitors of alk5 and p38α map kinase |
| SG11202007143UA (en) | 2018-01-31 | 2020-08-28 | Heparegenix Gmbh | Protein kinase mkk4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| WO2019183145A1 (en) | 2018-03-20 | 2019-09-26 | Plexxikon Inc. | Compounds and methods for ido and tdo modulation, and indications therefor |
| EP3810139A1 (en) | 2018-06-21 | 2021-04-28 | HepaRegeniX GmbH | Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| AU2019303986B2 (en) | 2018-07-16 | 2024-02-22 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| KR102545594B1 (ko) | 2018-07-31 | 2023-06-21 | 록쏘 온콜로지, 인코포레이티드 | (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의 분무-건조된 분산물 및 제제 |
| TWI811428B (zh) | 2018-08-21 | 2023-08-11 | 日商杏林製藥股份有限公司 | 雙環雜芳香環衍生物 |
| CN112996794A (zh) | 2018-09-10 | 2021-06-18 | 阿雷生物药品公司 | 作为ret激酶抑制剂的稠合杂环化合物 |
| BR112021010690A2 (pt) | 2018-12-03 | 2021-08-24 | Boehringer Ingelheim International Gmbh | Compostos heteroaromáticos como inibidores de vanina |
| WO2020124397A1 (en) | 2018-12-19 | 2020-06-25 | Inventisbio Shanghai Ltd. | C-terminal src kinase inhibitors |
| EP3898626A1 (en) | 2018-12-19 | 2021-10-27 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
| JP2022515197A (ja) | 2018-12-19 | 2022-02-17 | アレイ バイオファーマ インコーポレイテッド | がんを治療するためのｆｇｆｒ阻害剤としての７－（（３，５－ジメトキシフェニル）アミノ）キノキサリン誘導体 |
| BR112021019957A2 (pt) | 2019-04-09 | 2021-12-07 | Plexxikon Inc | Azinas condensadas para modulação de ep300 ou cbp e indicações da mesma |
| US20220235049A1 (en) * | 2019-05-31 | 2022-07-28 | Fochon Pharmaceuticals, Ltd. | SUBSTITUTED PYRROLO [2, 3-b] PYRIDINE AND PYRAZOLO [3,4-b] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS |
| AU2020311940A1 (en) | 2019-07-11 | 2022-02-03 | ESCAPE Bio, Inc. | Indazoles and azaindazoles as LRRK2 inhibitors |
| NZ785221A (en) | 2019-07-29 | 2025-08-29 | Heparegenix Gmbh | Heteroaryl-substituted pyrazolo-pyridine protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| WO2021113492A1 (en) | 2019-12-06 | 2021-06-10 | Schrödinger, Inc. | Cyclic compounds and methods of using same |
| EP4483882A3 (en) | 2019-12-10 | 2025-03-05 | F. Hoffmann-La Roche AG | New methylquinazolinone derivatives |
| WO2021134004A1 (en) | 2019-12-27 | 2021-07-01 | Schrodinger, Inc. | Cyclic compounds and methods of using same |
| JP7639008B2 (ja) | 2020-01-15 | 2025-03-04 | ヘパリジェニックス ゲーエムベーハー | 肝再生促進又は肝細胞死の抑制もしくは防止のためのプロテインキナーゼ阻害剤 |
| TW202206422A (zh) | 2020-04-23 | 2022-02-16 | 美商普雷辛肯公司 | 用於ｃｄ７３調節之化合物及方法及其適應症 |
| AU2021263383A1 (en) | 2020-04-29 | 2022-11-24 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
| US20230303551A1 (en) * | 2020-08-13 | 2023-09-28 | Albert Einstein College Of Medicine | N-cyclyl-sulfonamides useful for inhibiting raf |
| WO2022040512A1 (en) | 2020-08-21 | 2022-02-24 | Plexxikon Inc. | Combinational drug anticancer therapies |
| JP2023541047A (ja) | 2020-09-10 | 2023-09-27 | シュレーディンガー， インコーポレイテッド | がんの治療のための複素環式ペリ縮環ｃｄｃ７キナーゼ阻害剤 |
| US20240148732A1 (en) | 2021-01-26 | 2024-05-09 | Schrödinger, Inc. | Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders |
| CN112574200B (zh) * | 2021-02-26 | 2021-06-11 | 安润医药科技（苏州）有限公司 | Btk和/或btk的突变体c481s的小分子抑制剂 |
| CN113018415B (zh) * | 2021-03-17 | 2022-07-01 | 遵义医科大学 | 一种药物组合及其应用 |
| TW202300150A (zh) | 2021-03-18 | 2023-01-01 | 美商薛定諤公司 | 環狀化合物及其使用方法 |
| EP4352051A1 (en) * | 2021-06-09 | 2024-04-17 | F. Hoffmann-La Roche AG | New solid forms of (3r)-n-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide |
| CN113941001B (zh) * | 2021-12-09 | 2023-09-08 | 宁夏医科大学 | Craf抑制剂在制备抗肿瘤的药物中的应用 |
| US12331026B2 (en) | 2022-03-28 | 2025-06-17 | Nikang Therapeutics, Inc. | Sulfonamido derivatives as cyclin-dependent kinase 2 inhibitors |
| WO2023213965A1 (en) * | 2022-05-05 | 2023-11-09 | University Of Dundee | Inhibitors of cdk8 and cdk19 |
| WO2023240024A1 (en) * | 2022-06-08 | 2023-12-14 | Nikang Therapeutics, Inc. | Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors |
| WO2025026377A1 (en) * | 2023-08-02 | 2025-02-06 | Insilico Medicine Ip Limited | Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp1) inhibitors and uses thereof |
| WO2025059027A1 (en) | 2023-09-11 | 2025-03-20 | Schrödinger, Inc. | Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors |
| WO2025229494A1 (en) * | 2024-04-29 | 2025-11-06 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| CN119899194B (zh) * | 2025-03-31 | 2025-06-24 | 浙江省人民医院 | 双环杂芳基类braf负变构调节剂及其制备方法与应用 |
Family Cites Families (81)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040171062A1 (en) | 2002-02-28 | 2004-09-02 | Plexxikon, Inc. | Methods for the design of molecular scaffolds and ligands |
| KR20140070676A (ko) | 2002-09-06 | 2014-06-10 | 인설트 테라페틱스, 인코퍼레이티드 | 공유결합된 치료제 전달을 위한 사이클로덱스트린-기초 중합체 |
| US20040142864A1 (en) | 2002-09-16 | 2004-07-22 | Plexxikon, Inc. | Crystal structure of PIM-1 kinase |
| US20050048573A1 (en) | 2003-02-03 | 2005-03-03 | Plexxikon, Inc. | PDE5A crystal structure and uses |
| US20050170431A1 (en) | 2003-02-28 | 2005-08-04 | Plexxikon, Inc. | PYK2 crystal structure and uses |
| US20050079548A1 (en) | 2003-07-07 | 2005-04-14 | Plexxikon, Inc. | Ligand development using PDE4B crystal structures |
| US7348338B2 (en) | 2003-07-17 | 2008-03-25 | Plexxikon, Inc. | PPAR active compounds |
| AU2004259738B2 (en) | 2003-07-17 | 2011-11-17 | Plexxikon, Inc. | PPAR active compounds |
| WO2005028624A2 (en) | 2003-09-15 | 2005-03-31 | Plexxikon, Inc. | Molecular scaffolds for kinase ligand development |
| DK1696920T3 (en) | 2003-12-19 | 2015-01-19 | Plexxikon Inc | RELATIONS AND PROCEDURES FOR THE DEVELOPMENT OF LAW MODULATORS |
| US7517970B2 (en) | 2003-12-19 | 2009-04-14 | Plexxikon, Inc. | Nucleic acids encoding kinase and phosphatase enzymes, expression vectors and cells containing same |
| US20070066641A1 (en) | 2003-12-19 | 2007-03-22 | Prabha Ibrahim | Compounds and methods for development of RET modulators |
| EP1742627A4 (en) | 2004-05-06 | 2009-08-26 | Plexxikon Inc | PDE4B HEMMER AND ITS USE |
| US7498342B2 (en) | 2004-06-17 | 2009-03-03 | Plexxikon, Inc. | Compounds modulating c-kit activity |
| WO2006009797A1 (en) | 2004-06-17 | 2006-01-26 | Plexxikon, Inc. | Azaindoles modulating c-kit activity and uses therefor |
| CN101048407A (zh) | 2004-09-03 | 2007-10-03 | 普莱希科公司 | 双环杂芳基pde4b抑制剂 |
| JP2008521829A (ja) | 2004-11-30 | 2008-06-26 | プレキシコン，インコーポレーテッド | Ｐｐａｒ活性化合物 |
| AU2005311826A1 (en) | 2004-11-30 | 2006-06-08 | Plexxikon, Inc. | Indole derivatives for use as PPAR active compounds |
| US20060160135A1 (en) | 2004-12-08 | 2006-07-20 | Weiru Wang | SF-1 and LRH-1 modulator development |
| MX2007014377A (es) | 2005-05-17 | 2008-02-06 | Plexxikon Inc | Inhibidores de proteina cinasa de derivados de pirrol (2,3-b) piridina. |
| WO2007002433A1 (en) | 2005-06-22 | 2007-01-04 | Plexxikon, Inc. | Pyrrolo [2, 3-b] pyridine derivatives as protein kinase inhibitors |
| RU2008108221A (ru) | 2005-09-07 | 2009-10-20 | Плекссикон, Инк. (Us) | Соединения, активные в отношении ppar (рецепторов активаторов пролиферации пероксисом) |
| JP2009509932A (ja) | 2005-09-07 | 2009-03-12 | プレキシコン，インコーポレーテッド | Ｐｐａｒ活性化合物 |
| SG165362A1 (en) | 2005-09-07 | 2010-10-28 | Plexxikon Inc | Ppar active compounds |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| PE20121126A1 (es) | 2006-12-21 | 2012-08-24 | Plexxikon Inc | Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa |
| CA2673736A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| WO2008079909A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
| PE20090159A1 (es) | 2007-03-08 | 2009-02-21 | Plexxikon Inc | COMPUESTOS DERIVADOS DE ACIDO INDOL-PROPIONICO COMO MODULADORES PPARs |
| EP2121591A2 (en) | 2007-03-08 | 2009-11-25 | Plexxikon, Inc. | Ppar active compounds |
| BRPI0814423B1 (pt) | 2007-07-17 | 2022-04-19 | Plexxikon, Inc | Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos |
| KR20100122505A (ko) * | 2008-02-29 | 2010-11-22 | 어레이 바이오파마 인크. | Ｒａｆ 저해물질 화합물 및 이들의 이용 방법 |
| WO2009111279A1 (en) * | 2008-02-29 | 2009-09-11 | Array Biopharma Inc. | Pyrazole [3, 4-b] pyridine raf inhibitors |
| UA103319C2 (en) * | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
| PE20091846A1 (es) | 2008-05-19 | 2009-12-16 | Plexxikon Inc | DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS |
| WO2009143018A2 (en) | 2008-05-19 | 2009-11-26 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| 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 |
| JP5767965B2 (ja) | 2008-06-10 | 2015-08-26 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | キナーゼを調節する５ｈ−ピロロ［２，３−ｂ］ピラジン誘導体、およびその適応症 |
| RU2011141123A (ru) * | 2009-03-11 | 2013-04-20 | Плексксикон, Инк. | ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-b]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ RAF-КИНАЗ |
| WO2010104973A1 (en) | 2009-03-11 | 2010-09-16 | Plexxikon, Inc. | Pyrrolo [2, 3-b] pyridine derivatives for the inhibition of raf kinases |
| WO2010111527A1 (en) | 2009-03-26 | 2010-09-30 | Plexxikon, Inc. | Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use |
| MX2011008303A (es) | 2009-04-03 | 2011-11-29 | Plexxikon Inc | Composiciones del acido propano-1-sulfonico {3-[5-(4-cloro-fenil)- 1h-pirrolo [2,3-b]-piridina-3-carbonil]-2,4-difluoro-fenil}-amida y el uso de las mismas. |
| WO2010129467A1 (en) | 2009-05-04 | 2010-11-11 | Plexxikon, Inc. | Compounds and methods for inhibition of renin, and indications therefor |
| TW201041888A (en) | 2009-05-06 | 2010-12-01 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| JP2013503188A (ja) * | 2009-08-28 | 2013-01-31 | アレイ バイオファーマ、インコーポレイテッド | Ｒａｆ阻害化合物およびその使用方法 |
| US8242260B2 (en) * | 2009-08-28 | 2012-08-14 | Novartis Ag | Compounds and compositions as protein kinase inhibitors |
| US20120157451A1 (en) * | 2009-08-28 | 2012-06-21 | Genentech, Inc | Raf inhibitor compounds and methods of use thereof |
| WO2011025938A2 (en) | 2009-08-28 | 2011-03-03 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
| JO3002B1 (ar) | 2009-08-28 | 2016-09-05 | Irm Llc | مركبات و تركيبات كمثبطات كيناز بروتين |
| BR112012012156A2 (pt) | 2009-11-06 | 2015-09-08 | Plexxikon Inc | compostos e métodos para modulação de cinase, e indicações para esta |
| EP2498608A4 (en) | 2009-11-10 | 2013-04-24 | Glaxosmithkline Llc | BENZOLSULFONAMIDE THIAZOL AND OXAZOLE COMPOUNDS |
| EP2501236B1 (en) | 2009-11-18 | 2017-03-29 | Plexxikon Inc. | N-[2-fluoro-3-(4-amino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonyl)-phenyl]-4-benzenesulfonamide derivatives as Raf protein kinase modulators for the treatment of cancer |
| MX2012007429A (es) | 2009-12-23 | 2012-07-23 | Plexxikon Inc | Compuestos y metodos para la modulacion de quinasa e indicaciones de la misma. |
| TWI619713B (zh) | 2010-04-21 | 2018-04-01 | 普雷辛肯公司 | 用於激酶調節的化合物和方法及其適應症 |
| US8642606B2 (en) | 2010-09-29 | 2014-02-04 | Plexxikon Inc. | ZAP-70 active compounds |
| AU2012214762B2 (en) | 2011-02-07 | 2015-08-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| TWI558702B (zh) | 2011-02-21 | 2016-11-21 | 普雷辛肯公司 | 醫藥活性物質的固態形式 |
| CA2836474A1 (en) | 2011-05-17 | 2012-11-22 | Plexxikon Inc. | Kinase modulation and indications therefor |
| WO2013043935A1 (en) * | 2011-09-21 | 2013-03-28 | Neupharma, Inc. | Certain chemical entites, compositions, and methods |
| US9358235B2 (en) | 2012-03-19 | 2016-06-07 | Plexxikon Inc. | Kinase modulation, and indications therefor |
| US9150570B2 (en) | 2012-05-31 | 2015-10-06 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
| WO2014039714A2 (en) | 2012-09-06 | 2014-03-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| BR112015014752B1 (pt) | 2012-12-21 | 2022-07-05 | Plexxikon, Inc | Compostos e seus uso para modulação de cinase |
| US20140303121A1 (en) | 2013-03-15 | 2014-10-09 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| RU2680100C9 (ru) | 2013-03-15 | 2019-04-18 | Плексксикон Инк. | Гетероциклические соединения и их применения |
| CA2912568A1 (en) | 2013-05-30 | 2014-12-04 | Plexxikon Inc. | Compounds for kinase modulation, and indications therefor |
| WO2015134536A1 (en) | 2014-03-04 | 2015-09-11 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| US9856259B2 (en) | 2014-09-15 | 2018-01-02 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| US10160755B2 (en) | 2015-04-08 | 2018-12-25 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| DK3292123T3 (da) | 2015-05-06 | 2020-08-17 | Plexxikon Inc | Faste former af en forbindelse, der modulerer kinaser |
| US9745298B2 (en) | 2015-05-06 | 2017-08-29 | Plexxikon Inc. | Synthesis of a compound that modulates kinases |
| BR112017025045A2 (pt) | 2015-05-22 | 2018-08-07 | Plexxikon Inc | plx-8394 ou plx-7904 para uso no tratamento de doenças relacionadas a braf-v600 |
| TWI658042B (zh) | 2015-05-22 | 2019-05-01 | 美商普雷辛肯公司 | 雜環化合物的合成 |
| US10829484B2 (en) | 2015-07-28 | 2020-11-10 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CA3129180A1 (en) | 2015-09-21 | 2017-03-30 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| MX2018006856A (es) | 2015-12-07 | 2018-08-01 | Plexxikon Inc | Compuestos y metodos para modulacion de la quinasa, e indicaciones de los mismos. |
| JP6921846B6 (ja) | 2016-03-16 | 2021-09-15 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | キナーゼ調節およびその適応症のための化合物および方法 |
| TW201815766A (zh) | 2016-09-22 | 2018-05-01 | 美商普雷辛肯公司 | 用於ｉｄｏ及ｔｄｏ調節之化合物及方法以及其適應症 |
| CA3047580A1 (en) | 2016-12-23 | 2018-07-26 | Plexxikon Inc. | Compounds and methods for cdk8 modulation and indications therefor |
| AU2018237047A1 (en) | 2017-03-20 | 2019-10-17 | Plexxikon Inc. | Crystalline forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1H- pyrrolo[3,2-b]pyridin-3-yl)benzoic acid that inhibits bromodomain |
| US10428067B2 (en) | 2017-06-07 | 2019-10-01 | Plexxikon Inc. | Compounds and methods for kinase modulation |
-
2014
- 2014-05-29 CA CA2912568A patent/CA2912568A1/en not_active Abandoned
- 2014-05-29 JP JP2016516830A patent/JP2016520131A/ja active Pending
- 2014-05-29 AU AU2014274093A patent/AU2014274093B2/en not_active Ceased
- 2014-05-29 TW TW103118934A patent/TW201533028A/zh unknown
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- 2014-05-29 MX MX2015015966A patent/MX2015015966A/es unknown
- 2014-05-29 WO PCT/US2014/040076 patent/WO2014194127A1/en not_active Ceased
- 2014-05-29 RU RU2015149937A patent/RU2015149937A/ru unknown
- 2014-05-29 CN CN201480029525.6A patent/CN105228983A/zh active Pending
- 2014-05-29 BR BR112015028845A patent/BR112015028845A2/pt not_active IP Right Cessation
- 2014-05-29 HK HK16107741.9A patent/HK1219732A1/zh unknown
- 2014-05-29 KR KR1020157033201A patent/KR20160013028A/ko not_active Withdrawn
- 2014-05-29 US US14/290,786 patent/US9873700B2/en active Active
- 2014-05-29 SG SG11201509338QA patent/SG11201509338QA/en unknown
- 2014-05-30 UY UY0001035596A patent/UY35596A/es not_active Application Discontinuation
- 2014-05-30 AR ARP140102152A patent/AR096450A1/es unknown
-
2015
- 2015-11-12 IL IL242587A patent/IL242587A0/en unknown
- 2015-11-23 PH PH12015502610A patent/PH12015502610A1/en unknown
-
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- 2017-12-11 US US15/838,268 patent/US10421761B2/en active Active
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