CN103732597B - 三环杂环化合物和jak抑制剂 - Google Patents

三环杂环化合物和jak抑制剂 Download PDF

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Publication number
CN103732597B
CN103732597B CN201280039516.6A CN201280039516A CN103732597B CN 103732597 B CN103732597 B CN 103732597B CN 201280039516 A CN201280039516 A CN 201280039516A CN 103732597 B CN103732597 B CN 103732597B
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group
alkyl
unsubstituted
phenyl
aromatic heterocyclic
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CN103732597A (zh
Inventor
林圭史
渡边恒夫
外山公二
加门淳司
南昌孝
宇仁巳由纪
奈须麻莉子
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Misao Kusano
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Nissan Chemical Corp
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
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    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14—Ortho-condensed systems

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  • Urology & Nephrology (AREA)
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  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201280039516.6A 2011-08-12 2012-08-10 三环杂环化合物和jak抑制剂 Expired - Fee Related CN103732597B (zh)

Priority Applications (1)

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CN201510345134.1A CN105001226B (zh) 2011-08-12 2012-08-10 三环杂环化合物和jak抑制剂

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
JP2011-177270 2011-08-12
JP2011177270 2011-08-12
JP2011-177289 2011-08-12
JP2011177289 2011-08-12
JP2012097073 2012-04-20
JP2012-097073 2012-04-20
JP2012-103517 2012-04-27
JP2012103517 2012-04-27
JP2012103516 2012-04-27
JP2012-103516 2012-04-27
PCT/JP2012/070876 WO2013024895A1 (en) 2011-08-12 2012-08-10 Tricyclic heterocyclic compounds and jak inhibitors

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US (2) US9216999B2 (cg-RX-API-DMAC7.html)
EP (2) EP3112370A1 (cg-RX-API-DMAC7.html)
JP (2) JP6123804B2 (cg-RX-API-DMAC7.html)
KR (1) KR102021159B1 (cg-RX-API-DMAC7.html)
CN (2) CN103732597B (cg-RX-API-DMAC7.html)
AU (1) AU2012295802B2 (cg-RX-API-DMAC7.html)
BR (1) BR112014002472A2 (cg-RX-API-DMAC7.html)
CA (1) CA2841458C (cg-RX-API-DMAC7.html)
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Families Citing this family (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7960139B2 (en) 2007-03-23 2011-06-14 Academia Sinica Alkynyl sugar analogs for the labeling and visualization of glycoconjugates in cells
JP5986745B2 (ja) 2008-07-15 2016-09-06 アカデミア シニカＡｃａｄｅｍｉａ Ｓｉｎｉｃａ Ｐｔｆｅ様のアルミニウム・コート・ガラススライド上のグリカンアレイおよび関連する方法
US11377485B2 (en) 2009-12-02 2022-07-05 Academia Sinica Methods for modifying human antibodies by glycan engineering
US10087236B2 (en) 2009-12-02 2018-10-02 Academia Sinica Methods for modifying human antibodies by glycan engineering
WO2011130332A1 (en) 2010-04-12 2011-10-20 Academia Sinica Glycan arrays for high throughput screening of viruses
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
AU2012295802B2 (en) * 2011-08-12 2017-03-30 Nissan Chemical Industries, Ltd. Tricyclic heterocyclic compounds and JAK inhibitors
BR112014030812B1 (pt) 2012-06-13 2022-11-08 Incyte Holdings Corporation Compostos tricíclicos substituídos como inibidores de fgfr, seus usos, composição farmacêutica e método para inibir uma enzima fgfr
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9914956B2 (en) 2012-08-18 2018-03-13 Academia Sinica Cell-permeable probes for identification and imaging of sialidases
CA2883168A1 (en) 2012-08-21 2014-02-27 Academia Sinica Benzocyclooctyne compounds and uses thereof
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
ES2755130T3 (es) * 2013-02-08 2020-04-21 Nissan Chemical Corp Compuesto de pirrolopiridina tricíclico, e inhibidor de JAK
JP6506248B2 (ja) 2013-03-14 2019-04-24 ゾーン・ロイヤリティズ・アンド・マイルストーンズ・エルエルシー 二環式鎮痛化合物
ME03015B (me) 2013-04-19 2018-10-20 Incyte Holdings Corp Biciklični heterocikli kao fgfr inhibitori
WO2014210397A1 (en) 2013-06-26 2014-12-31 Academia Sinica Rm2 antigens and use thereof
WO2014210564A1 (en) 2013-06-27 2014-12-31 Academia Sinica Glycan conjugates and use thereof
KR102298172B1 (ko) 2013-09-06 2021-09-06 아카데미아 시니카 변화된 글리코실 그룹을 갖는 당지질을 사용한 인간 iNKT 세포 활성화
CN108947867A (zh) 2013-12-12 2018-12-07 卡利拉制药公司 双环烷基化合物及合成
CA2937123A1 (en) 2014-01-16 2015-07-23 Academia Sinica Compositions and methods for treatment and detection of cancers
US10150818B2 (en) 2014-01-16 2018-12-11 Academia Sinica Compositions and methods for treatment and detection of cancers
CA2942144C (en) 2014-03-07 2023-08-22 Kalyra Pharmaceuticals, Inc. Propellane derivates and synthesis
TWI797430B (zh) 2014-03-27 2023-04-01 中央研究院 反應性標記化合物及其用途
EP2924026A1 (en) 2014-03-28 2015-09-30 Novartis Tiergesundheit AG Aminosulfonylmethylcyclohexanes as JAK inhibitors
WO2015174376A1 (ja) * 2014-05-14 2015-11-19 日産化学工業株式会社 ３環性化合物及びｊａｋ阻害剤
AU2015267045B2 (en) 2014-05-27 2021-02-25 Academia Sinica Anti-HER2 glycoantibodies and uses thereof
FI3149045T3 (fi) 2014-05-27 2023-03-20 Academia Sinica Koostumuksia ja menetelmiä, jotka liittyvät yleisglykoformeihin vasta-aineiden parannettua tehokkuutta varten
US10118969B2 (en) 2014-05-27 2018-11-06 Academia Sinica Compositions and methods relating to universal glycoforms for enhanced antibody efficacy
US20150344585A1 (en) 2014-05-27 2015-12-03 Academia Sinica Anti-cd20 glycoantibodies and uses thereof
US11332523B2 (en) 2014-05-28 2022-05-17 Academia Sinica Anti-TNF-alpha glycoantibodies and uses thereof
TWI745275B (zh) 2014-09-08 2021-11-11 中央研究院 使用醣脂激活人類ｉＮＫＴ細胞
CN106999451B (zh) * 2014-09-17 2021-04-02 里科瑞尔姆Ip控股有限责任公司 双环化合物
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US10495645B2 (en) 2015-01-16 2019-12-03 Academia Sinica Cancer markers and methods of use thereof
US9975965B2 (en) 2015-01-16 2018-05-22 Academia Sinica Compositions and methods for treatment and detection of cancers
AU2015378564A1 (en) 2015-01-24 2017-07-13 Academia Sinica Novel glycan conjugates and methods of use thereof
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CR20170390A (es) 2015-02-20 2017-10-23 Incyte Holdings Corp Heterociclos biciclicos como inhibidores de fgfr
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
JP2019515876A (ja) 2016-03-08 2019-06-13 アカデミア シニカＡｃａｄｅｍｉａ Ｓｉｎｉｃａ Ｎ−グリカンおよびそのアレイのモジュール合成のための方法
TWI764917B (zh) 2016-08-22 2022-05-21 醣基生醫股份有限公司 抗體、結合片段及使用方法
PT3509591T (pt) * 2016-10-03 2021-12-27 Highlightll Pharmaceutical Hainan Co Ltd Novos inibidores seletivos da jak1 e usos dos mesmos
WO2018213140A1 (en) 2017-05-15 2018-11-22 Zeno Royalties & Milestones, LLC Analgesic compounds
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3656806B1 (en) 2017-07-20 2024-08-21 Mitsubishi Chemical Corporation Sheet molding compound, fiber-reinforced composite material, and method for producing fiber-reinforced composite material
US10800775B2 (en) 2017-11-03 2020-10-13 Aclaris Therapeutics, Inc. Pyrazolyl pyrrolo[2,3-b]pyrmidine-5-carboxylate analogs and methods of making the same
US10981906B2 (en) * 2017-11-03 2021-04-20 Aclaris Therapeutics, Inc. Substituted pyrrolopyridine JAK inhibitors and methods of making and using the same
KR102034538B1 (ko) * 2017-11-28 2019-10-21 주식회사한국파마 Jak 저해제 화합물, 및 이의 제조방법
SG11202010636VA (en) 2018-05-04 2020-11-27 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
WO2020033955A1 (en) 2018-08-10 2020-02-13 Aclaris Therapeutics, Inc. Pyrrolopyrimidine itk inhibitors
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
CN113727975A (zh) 2019-05-02 2021-11-30 阿克拉瑞斯治疗股份有限公司 作为jak抑制剂的被取代的吡咯并吡啶
EP3969458A4 (en) * 2019-05-13 2023-05-17 Borah, Inc. CHEMICAL COMPOUNDS
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
KR102228442B1 (ko) * 2019-08-14 2021-03-16 (주)호모미미쿠스 도식을 이용한 아이디에이션 플랫폼 장치 및 방법
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AU2021276066A1 (en) * 2020-05-20 2022-12-08 Bayer Aktiengesellschaft Process of preparing butyl-(5S)-5-({2-(4-(butoxycarbonyl)phenyl)ethyl}(2-(2-{(3-chloro-4'-(trifluoromethyl)(biphenyl)-4-yl)methoxy}phenyl)ethyl)amino)-5,6,7,8-tetrahydroquinoline-2-carboxylate
AU2021329303A1 (en) 2020-08-18 2023-04-06 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
AU2021329301A1 (en) 2020-08-18 2023-04-13 Incyte Corporation Process and intermediates for preparing a JAK1 inhibitor
CN114591351B (zh) * 2020-12-03 2023-12-05 成都科岭源医药技术有限公司 一种多环化合物及其制备方法和用途
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
TW202313611A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之三環雜環
US12071439B2 (en) 2021-07-12 2024-08-27 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
WO2023126436A1 (en) 2021-12-29 2023-07-06 Bayer Aktiengesellschaft Process for preparing (5s)-{[2-(4-carboxyphenyl)ethyl] |2-(2-{|3-chloro-4'-(trifluoromethyl)biphenyl-4- yl]methoxy}phenyl)ethyl]aminol-5,6,7,8-tetrahydroquinoline-2-carboxylic acid and its crystalline forms for use as pharmaceutically active compound
TW202342034A (zh) 2021-12-29 2023-11-01 德商拜耳廠股份有限公司 心肺病症之治療
AU2023235233A1 (en) 2022-03-14 2024-09-12 Slap Pharmaceuticals Llc Multicyclic compounds
CN116554057B (zh) * 2023-05-05 2023-12-15 杭州安道药业有限公司 降低促红细胞生长素（epo）生成的化合物及其用途
CN117586285B (zh) * 2024-01-19 2024-04-05 英矽智能科技(上海)有限公司 三并环类化合物

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101351466A (zh) * 2005-12-28 2009-01-21 安斯泰来制药株式会社 Janus激酶3的杂环抑制剂
CN101437822A (zh) * 2006-05-11 2009-05-20 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
WO2010044885A2 (en) * 2008-10-17 2010-04-22 Whitehead Institute For Biomedical Research Soluble mtor complexes and modulators thereof
WO2010119875A1 (ja) * 2009-04-14 2010-10-21 アステラス製薬株式会社 縮合ピロロピリジン誘導体
WO2011068899A1 (en) * 2009-12-01 2011-06-09 Abbott Laboratories Novel tricyclic compounds
CN102118968A (zh) * 2008-06-10 2011-07-06 雅培制药有限公司 新的三环化合物
WO2011086053A1 (en) * 2010-01-12 2011-07-21 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof
WO2012085176A1 (en) * 2010-12-23 2012-06-28 F. Hoffmann-La Roche Ag Tricyclic pyrazinone compounds, compositions and methods of use thereof as janus kinase inhibitors

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001042246A2 (en) * 1999-12-10 2001-06-14 Pfizer Products Inc. PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS
CN101213783B (zh) * 2005-06-29 2011-08-31 Nxp股份有限公司 采用自适应参考频率校正的同步方案
KR20080026654A (ko) 2005-07-14 2008-03-25 아스텔라스세이야쿠 가부시키가이샤 헤테로시클릭 야누스 키나제 3 억제제
JP5287253B2 (ja) 2007-01-12 2013-09-11 アステラス製薬株式会社 縮合ピリジン化合物
US8361962B2 (en) * 2009-07-27 2013-01-29 Roche Palo Alto Llc Tricyclic inhibitors of JAK
CN102574860A (zh) 2009-10-15 2012-07-11 辉瑞大药厂 吡咯并[2,3-d]嘧啶化合物
TWI500620B (zh) 2009-12-01 2015-09-21 Abbvie Inc 新穎三環化合物
EP2513114B1 (en) 2009-12-18 2014-04-02 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine compounds
CN201663335U (zh) * 2010-01-04 2010-12-01 飞利浦(中国)投资有限公司 一种插接站及包含该插接站的多媒体系统
CN102399233B (zh) * 2010-09-15 2014-08-13 山东轩竹医药科技有限公司 PI3K和mTOR双重抑制剂类化合物
US20120330012A1 (en) * 2011-04-29 2012-12-27 Abbott Laboratories Novel Tricyclic Compounds
WO2013007765A1 (en) * 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Fused tricyclic compounds for use as inhibitors of janus kinases
AU2012295802B2 (en) * 2011-08-12 2017-03-30 Nissan Chemical Industries, Ltd. Tricyclic heterocyclic compounds and JAK inhibitors

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101351466A (zh) * 2005-12-28 2009-01-21 安斯泰来制药株式会社 Janus激酶3的杂环抑制剂
CN101437822A (zh) * 2006-05-11 2009-05-20 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
CN102118968A (zh) * 2008-06-10 2011-07-06 雅培制药有限公司 新的三环化合物
WO2010044885A2 (en) * 2008-10-17 2010-04-22 Whitehead Institute For Biomedical Research Soluble mtor complexes and modulators thereof
WO2010119875A1 (ja) * 2009-04-14 2010-10-21 アステラス製薬株式会社 縮合ピロロピリジン誘導体
WO2011068899A1 (en) * 2009-12-01 2011-06-09 Abbott Laboratories Novel tricyclic compounds
WO2011086053A1 (en) * 2010-01-12 2011-07-21 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof
WO2012085176A1 (en) * 2010-12-23 2012-06-28 F. Hoffmann-La Roche Ag Tricyclic pyrazinone compounds, compositions and methods of use thereof as janus kinase inhibitors

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