TWI500620B - 新穎三環化合物 - Google Patents

新穎三環化合物 Download PDF

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Publication number
TWI500620B
TWI500620B TW099141754A TW99141754A TWI500620B TW I500620 B TWI500620 B TW I500620B TW 099141754 A TW099141754 A TW 099141754A TW 99141754 A TW99141754 A TW 99141754A TW I500620 B TWI500620 B TW I500620B
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TW
Taiwan
Prior art keywords
pyrrolo
optionally substituted
imidazo
pyrazin
alkyl
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TW099141754A
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English (en)
Chinese (zh)
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TW201125869A (en
Inventor
Neil Wishart
Anna M Ericsson
Michael Friedman
Nathan S Josephsohn
Kent D Stewart
Lu Wang
Maria A Argiriadi
Bryan A Fiamengo
Dawn M George
Jeffrey W Voss
Kevin R Woller
David J Calderwood
Kristine E Frank
Eric R Goedken
Michael J Morytko
Grier A Wallace
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Abbvie Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44070404&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TWI500620(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Abbvie Inc filed Critical Abbvie Inc
Publication of TW201125869A publication Critical patent/TW201125869A/zh
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    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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Families Citing this family (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS54560B1 (sr) * 2008-06-10 2016-06-30 Abbvie Inc. Triciklična jedinjenja
EP2420502A4 (en) * 2009-04-14 2012-12-19 Astellas Pharma Inc CONDENSED PYRROLOPYRIDINE DERIVATIVE
RU2012127368A (ru) * 2009-12-01 2014-01-10 Эбботт Лэборетриз Новые трициклические соединения
CN102711476B (zh) * 2009-12-01 2014-12-03 Abbvie公司 新的三环化合物
EP2523957A1 (en) 2010-01-12 2012-11-21 F. Hoffmann-La Roche AG Tricyclic heterocyclic compounds, compositions and methods of use thereof
WO2012127506A1 (en) 2011-03-22 2012-09-27 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
KR101649610B1 (ko) 2011-04-21 2016-08-19 오리제니스 게엠베하 키나아제 억제제로서의 헤테로사이클릭 화합물
WO2013007765A1 (en) * 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Fused tricyclic compounds for use as inhibitors of janus kinases
US9216999B2 (en) * 2011-08-12 2015-12-22 Nissan Chemical Industries, Ltd. Substituted pyrrolo[2,3-h][1,6]naphthyridines and compositions thereof as JAK inhibitors
WO2013043826A1 (en) 2011-09-21 2013-03-28 Abbvie Inc. Tricyclic compounds useful as protein kinase inhibitors
CN102516146B (zh) * 2011-11-24 2013-10-02 爱斯特(成都)生物制药有限公司 5位为氮的四元氮杂螺环衍生物及其制备方法和用途
JP2015529242A (ja) * 2012-09-21 2015-10-05 アドヴィヌス セラピューティクス リミテッドAdvinus Therapeutics Limited 置換された縮合三環式化合物、組成物およびその医薬用途
US10000482B2 (en) 2012-10-19 2018-06-19 Origenis Gmbh Kinase inhibitors
ES2755130T3 (es) 2013-02-08 2020-04-21 Nissan Chemical Corp Compuesto de pirrolopiridina tricíclico, e inhibidor de JAK
SI3290421T1 (sl) 2013-02-22 2019-03-29 Pfizer Inc. Kombinacija derivatov pirolo (2,3-D)pirimidina z enim ali več dodatnimi sredstvi za zaviranje z janusom povezane kinaze (JAK)
IL240830B (en) 2013-02-28 2022-08-01 Teewinot Tech Limited Processes for chemical engineering and the device for the synthesis of compounds
WO2015023675A2 (en) 2013-08-12 2015-02-19 Pharmaceutical Manufacturing Research Services, Inc. Extruded immediate release abuse deterrent pill
CA2926361A1 (en) * 2013-10-24 2015-04-30 Abbvie Inc. Jak1 selective inhibitor and uses thereof
US9492444B2 (en) 2013-12-17 2016-11-15 Pharmaceutical Manufacturing Research Services, Inc. Extruded extended release abuse deterrent pill
US10172797B2 (en) 2013-12-17 2019-01-08 Pharmaceutical Manufacturing Research Services, Inc. Extruded extended release abuse deterrent pill
US10246455B2 (en) * 2014-04-11 2019-04-02 Taipei Medical University Histone deacetylase inhibitors
MX374105B (es) 2014-05-14 2025-03-05 Nissan Chemical Ind Ltd Compuestos azatricíclicos como inhibidores de tirosinas quinasas (jak) y el uso de los mismos en el tratamiento de enfermedades autoinmunes, inflamatorias y alérgicas.
AU2015290098B2 (en) 2014-07-17 2018-11-01 Pharmaceutical Manufacturing Research Services, Inc. Immediate release abuse deterrent liquid fill dosage form
WO2016024185A1 (en) 2014-08-12 2016-02-18 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase
BR112017003966A2 (pt) 2014-08-25 2018-10-23 Full Spectrum Laboratories Ltd aparelhos e métodos para a produção simultânea de compostos canabinoides
AU2015336065A1 (en) 2014-10-20 2017-05-04 Pharmaceutical Manufacturing Research Services, Inc. Extended release abuse deterrent liquid fill dosage form
US11512092B2 (en) 2015-10-16 2022-11-29 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US10550126B2 (en) 2015-10-16 2020-02-04 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11524964B2 (en) 2015-10-16 2022-12-13 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
RU2018117889A (ru) * 2015-10-16 2019-11-20 Эббви Инк. СПОСОБЫ ПОЛУЧЕНИЯ (3S,4R)-3-ЭТИЛ-4-(3H-ИМИДАЗО[1,2-a]ПИРРОЛО[2,3-e]-ПИРАЗИН-8-ИЛ)-N-(2,2,2-ТРИФТОРЭТИЛ)ПИРРОЛИДИН-1-КАРБОКСАМИДА И ЕГО ТВЕРДОФАЗНЫХ ФОРМ
US20250250277A1 (en) * 2015-10-16 2025-08-07 Abbvie Inc. PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF
US11365198B2 (en) 2015-10-16 2022-06-21 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US12365689B2 (en) 2015-10-16 2025-07-22 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11773106B2 (en) 2015-10-16 2023-10-03 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
KR102758609B1 (ko) 2016-01-14 2025-01-22 주식회사 한독 A3 아데노신 수용체 길항 화합물, 그의 제조 방법 및 그의 의학적 용도
EP3433615A1 (en) 2016-03-21 2019-01-30 Institut National de la Sante et de la Recherche Medicale (INSERM) Methods for diagnosis and treatment of solar lentigo
JOP20190144A1 (ar) 2016-12-16 2019-06-16 Janssen Pharmaceutica Nv إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز
PL3555097T3 (pl) 2016-12-16 2022-10-17 Janssen Pharmaceutica Nv Związki imidazo[4,5-d]pirolo[2,3-b]pirydynowe jako inhibitory kinaz janusowych
US11564922B2 (en) 2017-03-09 2023-01-31 Abbvie Inc. Methods of treating crohn's disease and ulcerative colitis
US20190046527A1 (en) 2017-03-09 2019-02-14 Abbvie Inc. Methods of treating crohn's disease and ulcerative colitis
WO2018167283A1 (en) 2017-03-17 2018-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling
US10364245B2 (en) 2017-06-07 2019-07-30 Chiesi Farmaceutici S.P.A. Kinase inhibitors
CN109535164B (zh) * 2017-09-21 2022-01-18 上海华汇拓医药科技有限公司 Jak激酶抑制剂及其制备方法和在医药领域的应用
UY38144A (es) 2018-03-12 2019-10-31 Abbvie Inc Inhibidores de la señalización mediada por tirosina cinasa
KR20210018264A (ko) 2018-05-04 2021-02-17 인사이트 코포레이션 Fgfr 억제제의 염
TW202016110A (zh) 2018-06-15 2020-05-01 比利時商健生藥品公司 Jak激酶家族之小分子抑制劑
WO2020043033A2 (zh) * 2018-08-31 2020-03-05 苏州鹏旭医药科技有限公司 一种乌帕替尼及其中间体的合成方法
CN110872250B (zh) * 2018-08-31 2023-01-10 苏州鹏旭医药科技有限公司 两种化合物及其制备方法和在合成乌西替尼中的用途
KR102841141B1 (ko) 2018-11-01 2025-07-31 링크 파마슈티컬스 컴퍼니 리미티드 트리사이클릭 야누스 키나제 1 억제제 및 이의 조성물 및 방법
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
CN111217819B (zh) * 2018-11-27 2021-05-14 杭州科巢生物科技有限公司 乌帕替尼的合成方法
EP3891151A1 (en) 2018-12-05 2021-10-13 LEK Pharmaceuticals d.d. Crystalline phosphate salt of selective jak1 inhibitor upadacitinib
WO2020115213A1 (en) 2018-12-07 2020-06-11 Lek Pharmaceuticals D.D. Solvate of a selective jak1 inhibitor
CN109761885B (zh) * 2019-02-21 2020-06-26 北京悦康科创医药科技股份有限公司 一种阿加曲班异构体杂质的拆分方法
CN112888692A (zh) * 2019-03-01 2021-06-01 苏州科睿思制药有限公司 一种Upadacitinib的晶型及其制备方法和用途
IL285999B1 (en) 2019-03-05 2025-09-01 Incyte Corp JAK1 inhibitor pathway for the treatment of chronic lung allograft dysfunction
JP7248256B2 (ja) 2019-03-14 2023-03-29 上海華匯拓医薬科技有限公司 Jakキナーゼ阻害剤及びその調製方法、並びにその医薬分野での使用
WO2020202183A1 (en) 2019-03-29 2020-10-08 Mylan Laboratories Limited The process for the preparation of upadacitinib and its intermediates
CN111909160B (zh) * 2019-05-09 2024-05-28 苏州鹏旭医药科技有限公司 一种乌帕替尼盐类化合物及其制备方法
EP4006028B1 (en) * 2019-07-26 2025-07-02 Zhuhai Yufan Biotechnologies Co., Ltd Irak4 kinase inhibitor and preparation method therefor
CN110938048B (zh) * 2019-12-02 2023-03-28 四川大学 路易酸催化的插入反应高效合成二氢呋喃衍生物
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
WO2021123288A1 (en) 2019-12-19 2021-06-24 Crystal Pharma, S.A.U. Process and intermediates for the preparation of upadacitinib
CN111007184B (zh) * 2019-12-30 2023-05-16 天津天士力圣特制药有限公司 一种4-甲基哌嗪-1-甲酰氯盐酸盐含量的检测方法
WO2021176473A1 (en) 2020-03-05 2021-09-10 Mylan Laboratories Limited A process for the preparation of upadacitinib and its intermediates
US11718622B2 (en) 2020-03-16 2023-08-08 Exelixis Inc. Heterocyclic adenosine receptor antagonists
EP4138561A1 (en) * 2020-04-24 2023-03-01 Kansas Soybean Commission One-step synthesis of soybean polyols
CN114206877B (zh) * 2020-06-05 2024-04-19 苏州科睿思制药有限公司 一种乌帕替尼的晶型及其制备方法和用途
EP4180435A1 (en) 2020-07-08 2023-05-17 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystal form of upadacitinib, preparation method therefor, and use thereof
WO2022044037A1 (en) 2020-08-24 2022-03-03 Mylan Laboratories Limited An improved process for the preparation of upadacitinib intermediate
WO2022054005A1 (en) * 2020-09-14 2022-03-17 Galderma Holding SA Novel jak inhibitor compounds, method for synthesizing same and use thereof
CA3190745A1 (en) * 2020-10-08 2022-04-14 Dhananjay G. Sathe Substituted tricyclic compounds
CN112578034B (zh) * 2020-11-04 2022-02-11 广东众生睿创生物科技有限公司 一种手性胺小分子及其盐的质量控制方法
CN114790208B (zh) * 2021-01-26 2024-06-07 珠海宇繁生物科技有限责任公司 一种irak4激酶抑制剂及其制备方法
BR112023018286A2 (pt) 2021-03-11 2023-10-31 Janssen Pharmaceutica Nv Lorpucitinib para uso no tratamento de distúrbios mediados por jak
WO2022217257A1 (en) * 2021-04-07 2022-10-13 Abbvie Inc. Cocrystals of upadacitinib
CN113200967B (zh) * 2021-05-07 2022-05-24 中国人民解放军陆军军医大学 吲哚苯醌类化合物、其制备方法及其应用
AU2022271927B2 (en) * 2021-05-13 2025-07-10 Innovstone Therapeutics Limited Compound having anti-tumor activity and use thereof
CN113603693B (zh) * 2021-07-13 2022-08-26 陕西丽彩药业有限公司 一种2-溴-5-对甲苯磺酰基-5H-吡咯并[2,3-b]吡嗪的制备方法
CN114380837B (zh) * 2021-12-27 2023-06-30 上海邈金医药科技有限公司 一种具有Janus激酶抑制活性的化合物、包括该化合物的组合物及其应用
EP4215196A1 (en) 2022-01-24 2023-07-26 Abivax Combination of 8-chloro-n-(4-(trifluoromethoxy)phenyl)quinolin-2-amine and its derivatives with a jak inhibitor
US12487299B2 (en) 2022-06-20 2025-12-02 Shanghai United Imaging Healthcare Co., Ltd. Magnetic resonance imaging devices and radiation therapy systems including the magnetic resonance imaging devices
CN116836171B (zh) * 2023-06-30 2024-06-04 凌科药业(杭州)有限公司 一种磺酰胺类化合物及其应用
WO2025102268A1 (en) * 2023-11-15 2025-05-22 Lynk Pharmaceuticals Co. Ltd. Solid state forms, pharmaceutical compositions, preparation methods and use thereof
CN117285537B (zh) * 2023-11-27 2024-02-06 中节能万润股份有限公司 一种乌帕替尼的制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007077949A1 (en) * 2005-12-28 2007-07-12 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
EP2123651A1 (en) * 2007-01-12 2009-11-25 Astellas Pharma Inc. Condensed pyridine compound
TW201002720A (en) * 2008-06-10 2010-01-16 Abbott Lab Novel tricyclic compounds
TW201102389A (en) * 2009-04-14 2011-01-16 Astellas Pharma Inc Fused pyrroloprydine derivatives

Family Cites Families (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB716327A (en) 1951-09-05 1954-10-06 Ici Ltd New heterocyclic compounds
US3663559A (en) 1969-12-03 1972-05-16 Union Carbide Corp Preparation of oxo-furo-pyridines from furylvinyl isocyanates
ZA737247B (en) 1972-09-29 1975-04-30 Ayerst Mckenna & Harrison Rapamycin and process of preparation
US4053474A (en) * 1976-04-21 1977-10-11 E. R. Squibb & Sons, Inc. Pyrazolo[4,3-e][1,2,4]triazolo[4,3-c]pyrimidine
US5605690A (en) 1989-09-05 1997-02-25 Immunex Corporation Methods of lowering active TNF-α levels in mammals using tumor necrosis factor receptor
US5270316A (en) 1989-10-20 1993-12-14 Kyowa Hakko Kogyo Co., Ltd. Condensed purine derivatives
CA2073500C (en) 1990-01-11 2008-03-25 Phillip Dan Cook Compositions and methods for detecting and modulating rna activity and gene expression
US6262241B1 (en) 1990-08-13 2001-07-17 Isis Pharmaceuticals, Inc. Compound for detecting and modulating RNA activity and gene expression
ES2099245T3 (es) 1990-11-26 1997-05-16 Robert R Recker Tratamiento de la osteoporosis usando factor de liberacion de hormona de crecimiento (grf) en combinacion con hormona paratiroidea (pth).
EP1857554A1 (en) 1991-03-18 2007-11-21 New York University Monoclonal and chimeric antibodies specific for human tumor necrosis factor
JP3147902B2 (ja) 1991-06-14 2001-03-19 ファルマシア・アンド・アップジョン・カンパニー イミダゾ〔1,5−a〕キノキサリン
US5212310A (en) 1991-12-19 1993-05-18 Neurogen Corporation Certain aryl fused imidazopyrimidines; a new class of GABA brain receptor ligands
US5266698A (en) 1992-04-30 1993-11-30 Neurogen Corporation Certain aryl and cycloalkyl fused imidazopyrazinediones; a new class of GABA brain receptor ligands
US5306819A (en) 1992-08-27 1994-04-26 Neurogen Corporation Certain aryl a cycloalkyl fused imidazopyrazinols; and new class of GABA brain receptor ligands
EP1005870B1 (en) 1992-11-13 2009-01-21 Biogen Idec Inc. Therapeutic application of chimeric antibodies to human B lymphocyte restricted differentiation antigen for treatment of B cell lymphoma
HUT72640A (en) 1993-02-26 1996-05-28 Schering Corp 2-benzyl-polycyclic guanine derivatives, pharmaceutical compositions containing them and process for preparing them
US5733905A (en) 1993-07-29 1998-03-31 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
US5736540A (en) 1993-07-29 1998-04-07 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
IL112248A0 (en) * 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
US5547975A (en) 1994-09-20 1996-08-20 Talley; John J. Benzopyranopyrazolyl derivatives for the treatment of inflammation
RU2158127C2 (ru) 1994-12-23 2000-10-27 Варнер-Ламберт Компани Способы ингибирования тирозинкиназы рецептора эпидермального фактора роста, азотсодержащие трициклические соединения, фармацевтическая композиция, предназначенная для введения ингибитора тирозинкиназы рецептора эпидермального фактора роста, например, erb-b2, erb-b3 или erb-b4, и противозачаточная композиция
US5521173A (en) 1995-01-17 1996-05-28 American Home Products Corporation Tricyclic benzazepine vasopressin antagonists
US5753648A (en) 1995-01-17 1998-05-19 American Cyanamid Company Tricyclic benzazepine vasopressin antagonists
US5763137A (en) 1995-08-04 1998-06-09 Agfa-Gevaert, N.V. Method for making a lithographic printing plate
US6090382A (en) 1996-02-09 2000-07-18 Basf Aktiengesellschaft Human antibodies that bind human TNFα
ATE430149T1 (de) 1998-03-04 2009-05-15 Bristol Myers Squibb Co Heterocyclen substituierte imidazopyrazine als protein- tyrosin-kinase-inhibitoren
US6448253B1 (en) * 1998-09-16 2002-09-10 King Pharmaceuticals Research And Development, Inc. Adenosine A3 receptor modulators
CO5271670A1 (es) 1999-10-29 2003-04-30 Pfizer Prod Inc Antagonistas del factor de liberacion de corticitropina y composiciones relacionadas
JP4100865B2 (ja) * 1999-12-13 2008-06-11 エーザイ・アール・アンド・ディー・マネジメント株式会社 三環式縮合異項環化合物、その製造法およびその医薬
TWI271406B (en) 1999-12-13 2007-01-21 Eisai Co Ltd Tricyclic condensed heterocyclic compounds, preparation method of the same and pharmaceuticals comprising the same
JP2004505942A (ja) 2000-08-07 2004-02-26 ニューロゲン コーポレイション Gabaa受容体の配位子としての複素環式化合物
GB0115393D0 (en) 2001-06-23 2001-08-15 Aventis Pharma Ltd Chemical compounds
GB0124299D0 (en) 2001-10-10 2001-11-28 Astrazeneca Ab Crystal structure of enzyme and uses thereof
ATE353013T1 (de) 2002-02-19 2007-02-15 Pfizer Italia Srl Trizyklische pyrazolderivate, verfahren zu ihrer herstellung und ihre verwendung als antitumor mittel
TW200400034A (en) 2002-05-20 2004-01-01 Bristol Myers Squibb Co Pyrazolo-pyrimidine aniline compounds useful as kinase inhibitors
ATE477251T1 (de) * 2002-08-23 2010-08-15 Novartis Vaccines & Diagnostic Pyrrolverbindungen als glykogen synthase kinase 3 inhibitoren
MXPA05007503A (es) * 2003-01-17 2005-09-21 Warner Lambert Co Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular.
US7176214B2 (en) 2003-05-21 2007-02-13 Bristol-Myers Squibb Company Imidazo-fused oxazolo[4,5-β]pyridine and imidazo-fused thiazolo[4,5-β]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
TW200524864A (en) * 2003-11-10 2005-08-01 Wyeth Corp Sulfonyltetrahydro-3H-benzo(E)indole-8-amine compounds as 5-hydroxytryptamine-6 ligands
MXPA06013250A (es) * 2004-05-14 2007-02-28 Abbott Lab Inhibidores de quinasa como agentes terapeuticos.
PE20060526A1 (es) * 2004-06-15 2006-07-13 Schering Corp Compuestos triciclicos como antagonistas de mglur1
WO2006010567A1 (de) 2004-07-23 2006-02-02 Curacyte Discovery Gmbh INHIBITOREN DER PHOSPHODIESTERASE 4 UND TNFα-FREISETZUNG
CN101098872B (zh) 2004-11-22 2012-09-05 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吡咯并吡嗪和吡唑并吡嗪
CA2594425A1 (en) * 2005-01-14 2006-07-20 Janssen Pharmaceutica N.V. 5-membered annelated heterocyclic pyrimidines as kinase inhibitors
EP1844048B1 (en) * 2005-01-14 2010-05-26 Janssen Pharmaceutica N.V. Pyrazolopyrimidines as cell cycle kinase inhibitors
US20060183758A1 (en) 2005-02-17 2006-08-17 Cb Research And Development, Inc. Method for synthesis of AZA-annelated pyrroles, thiophenes, and furans
JP2008538119A (ja) * 2005-04-01 2008-10-09 コーリー ファーマシューティカル グループ,インコーポレーテッド ピラゾロ[3,4−c]キノリン類、ピラゾロ[3,4−c]ナフチリジン類、これらの類似体、および方法
US7737279B2 (en) * 2005-05-10 2010-06-15 Bristol-Myers Squibb Company 1,6-dihydro-1,3,5,6-tetraaza-as-indacene based tricyclic compounds and pharmaceutical compositions comprising same
US7593820B2 (en) 2005-05-12 2009-09-22 Cytopia Research Pty Ltd Crystal structure of human Janus Kinase 2 (JAK2) and uses thereof
EP1910358A2 (en) * 2005-07-14 2008-04-16 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
CN101223168A (zh) * 2005-07-14 2008-07-16 安斯泰来制药株式会社 Janus激酶3的杂环类抑制剂
ES2481402T3 (es) 2005-07-21 2014-07-30 Ardea Biosciences, Inc. Inhibidores de N-(arilamino)sulfonamida de MEK
JP5016601B2 (ja) * 2005-08-16 2012-09-05 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
EP1937683A4 (en) 2005-09-23 2010-08-25 Coley Pharm Group Inc PROCESS FOR 1H-IMIDAZO [4,5-C] PYRIDINES AND ANALOGUE THEREOF
US7776865B2 (en) * 2005-10-06 2010-08-17 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
WO2007061764A2 (en) 2005-11-22 2007-05-31 Merck & Co., Inc. Tricyclic compounds useful as inhibitors of kinases
TW201307354A (zh) * 2005-12-29 2013-02-16 Abbott Lab 蛋白質激酶抑制劑
JP5242419B2 (ja) * 2006-02-15 2013-07-24 アボット・ラボラトリーズ ピラゾロキノロン類は強力なparp阻害薬である
ATE522518T1 (de) 2006-05-31 2011-09-15 Takeda San Diego Inc Indazol- und isoindolderivate als glucokinaseaktivierende stoffe
US7629346B2 (en) 2006-06-19 2009-12-08 Hoffmann-La Roche Inc. Pyrazinecarboxamide derivatives as CB1 antagonists
US20080090834A1 (en) 2006-07-06 2008-04-17 Pfizer Inc Selective azole pde10a inhibitor compounds
US8063225B2 (en) 2006-08-14 2011-11-22 Chembridge Corporation Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders
CN101553224A (zh) * 2006-10-06 2009-10-07 艾博特公司 新型咪唑并噻唑和咪唑并唑
US20110281821A9 (en) * 2007-01-30 2011-11-17 Biogen Idec Ma Inc. Modulators of Mitotic Kinases
WO2008112695A2 (en) 2007-03-12 2008-09-18 Irm Llc Pyrazolo [3,4-d] pyrimidines and 1, 2, 5, 6-tetraaza- as- indacenes as protein kinase inhibitors for cancer treatment
US7691869B2 (en) * 2007-03-30 2010-04-06 King Pharmaceuticals Research And Development, Inc. Pyrrolotriazolopyrimidine derivatives, pharmaceutical compositions containing them and methods of treating conditions and diseases mediated by the adenosine A2A receptor activity
CN101641447A (zh) 2007-04-04 2010-02-03 霍夫曼-拉罗奇有限公司 乙酰氧基酮的微生物还原
US8188083B2 (en) * 2007-06-28 2012-05-29 Abbott Laboratories Triazolopyridazines
EP2175885B1 (en) 2007-07-30 2016-10-12 Ardea Biosciences, Inc. Combinations of mek inhibitors and raf kinase inhibitors and uses thereof
PE20091485A1 (es) * 2008-02-06 2009-10-26 Novartis Ag DERIVADOS DE PIRROLO-[2,3-d]-PIRIMIDINA COMO INHIBIDORES DE CINASAS
RU2503676C2 (ru) 2008-02-25 2014-01-10 Ф.Хоффманн-Ля Рош Аг Пирролопиразиновые ингибиторы киназы
EP2250172B1 (en) 2008-02-25 2011-08-31 F. Hoffmann-La Roche AG Pyrrolopyrazine kinase inhibitors
ATE517107T1 (de) 2008-02-25 2011-08-15 Hoffmann La Roche Pyrrolopyrazinkinaseinhibitoren
WO2009108827A1 (en) 2008-02-29 2009-09-03 Wyeth Fused tricyclic pyrazolo[1, 5-a]pyrimidines, methods for preparation and uses thereof
WO2010003133A2 (en) * 2008-07-03 2010-01-07 Exelixis Inc. Cdk modulators
US8361962B2 (en) * 2009-07-27 2013-01-29 Roche Palo Alto Llc Tricyclic inhibitors of JAK
CN102711476B (zh) * 2009-12-01 2014-12-03 Abbvie公司 新的三环化合物
RU2012127368A (ru) * 2009-12-01 2014-01-10 Эбботт Лэборетриз Новые трициклические соединения
US8637529B2 (en) 2010-06-11 2014-01-28 AbbYie Inc. Pyrazolo[3,4-d]pyrimidine compounds
US20120330012A1 (en) 2011-04-29 2012-12-27 Abbott Laboratories Novel Tricyclic Compounds
WO2013043826A1 (en) 2011-09-21 2013-03-28 Abbvie Inc. Tricyclic compounds useful as protein kinase inhibitors
CA2926361A1 (en) 2013-10-24 2015-04-30 Abbvie Inc. Jak1 selective inhibitor and uses thereof
RU2018117889A (ru) 2015-10-16 2019-11-20 Эббви Инк. СПОСОБЫ ПОЛУЧЕНИЯ (3S,4R)-3-ЭТИЛ-4-(3H-ИМИДАЗО[1,2-a]ПИРРОЛО[2,3-e]-ПИРАЗИН-8-ИЛ)-N-(2,2,2-ТРИФТОРЭТИЛ)ПИРРОЛИДИН-1-КАРБОКСАМИДА И ЕГО ТВЕРДОФАЗНЫХ ФОРМ

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007077949A1 (en) * 2005-12-28 2007-07-12 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
EP2123651A1 (en) * 2007-01-12 2009-11-25 Astellas Pharma Inc. Condensed pyridine compound
TW201002720A (en) * 2008-06-10 2010-01-16 Abbott Lab Novel tricyclic compounds
TW201102389A (en) * 2009-04-14 2011-01-16 Astellas Pharma Inc Fused pyrroloprydine derivatives

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