JP2012504639A5 - - Google Patents

Download PDF

Info

Publication number
JP2012504639A5
JP2012504639A5 JP2011530218A JP2011530218A JP2012504639A5 JP 2012504639 A5 JP2012504639 A5 JP 2012504639A5 JP 2011530218 A JP2011530218 A JP 2011530218A JP 2011530218 A JP2011530218 A JP 2011530218A JP 2012504639 A5 JP2012504639 A5 JP 2012504639A5
Authority
JP
Japan
Prior art keywords
alkyl
haloalkyl
independently selected
alkynyl
alkenyl
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.)
Withdrawn
Application number
JP2011530218A
Other languages
English (en)
Japanese (ja)
Other versions
JP2012504639A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2009/059203 external-priority patent/WO2010039939A1/en
Publication of JP2012504639A publication Critical patent/JP2012504639A/ja
Publication of JP2012504639A5 publication Critical patent/JP2012504639A5/ja
Withdrawn legal-status Critical Current

Links

JP2011530218A 2008-10-02 2009-10-01 ドライアイおよび他の目に関連する疾患を治療するためのヤヌスキナーゼ阻害剤 Withdrawn JP2012504639A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US10224208P 2008-10-02 2008-10-02
US61/102,242 2008-10-02
PCT/US2009/059203 WO2010039939A1 (en) 2008-10-02 2009-10-01 Janus kinase inhibitors for treatment of dry eye and other eye related diseases

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2015042933A Division JP2015127332A (ja) 2008-10-02 2015-03-04 ドライアイおよび他の目に関連する疾患を治療するためのヤヌスキナーゼ阻害剤

Publications (2)

Publication Number Publication Date
JP2012504639A JP2012504639A (ja) 2012-02-23
JP2012504639A5 true JP2012504639A5 (https=) 2013-02-07

Family

ID=41572626

Family Applications (5)

Application Number Title Priority Date Filing Date
JP2011530218A Withdrawn JP2012504639A (ja) 2008-10-02 2009-10-01 ドライアイおよび他の目に関連する疾患を治療するためのヤヌスキナーゼ阻害剤
JP2015042933A Pending JP2015127332A (ja) 2008-10-02 2015-03-04 ドライアイおよび他の目に関連する疾患を治療するためのヤヌスキナーゼ阻害剤
JP2017000685A Pending JP2017057231A (ja) 2008-10-02 2017-01-05 ドライアイおよび他の目に関連する疾患を治療するためのヤヌスキナーゼ阻害剤
JP2017246134A Pending JP2018044012A (ja) 2008-10-02 2017-12-22 ドライアイおよび他の目に関連する疾患を治療するためのヤヌスキナーゼ阻害剤
JP2020002245A Pending JP2020050682A (ja) 2008-10-02 2020-01-09 ドライアイおよび他の目に関連する疾患を治療するためのヤヌスキナーゼ阻害剤

Family Applications After (4)

Application Number Title Priority Date Filing Date
JP2015042933A Pending JP2015127332A (ja) 2008-10-02 2015-03-04 ドライアイおよび他の目に関連する疾患を治療するためのヤヌスキナーゼ阻害剤
JP2017000685A Pending JP2017057231A (ja) 2008-10-02 2017-01-05 ドライアイおよび他の目に関連する疾患を治療するためのヤヌスキナーゼ阻害剤
JP2017246134A Pending JP2018044012A (ja) 2008-10-02 2017-12-22 ドライアイおよび他の目に関連する疾患を治療するためのヤヌスキナーゼ阻害剤
JP2020002245A Pending JP2020050682A (ja) 2008-10-02 2020-01-09 ドライアイおよび他の目に関連する疾患を治療するためのヤヌスキナーゼ阻害剤

Country Status (18)

Country Link
US (4) US20100113416A1 (https=)
EP (2) EP3042655A1 (https=)
JP (5) JP2012504639A (https=)
AR (2) AR073530A1 (https=)
CA (2) CA3064247A1 (https=)
CL (1) CL2009001884A1 (https=)
CY (1) CY1117317T1 (https=)
DK (1) DK2349260T3 (https=)
ES (1) ES2564203T3 (https=)
HR (1) HRP20160330T1 (https=)
HU (1) HUE028499T2 (https=)
PL (1) PL2349260T3 (https=)
PT (1) PT2349260E (https=)
RS (1) RS54651B1 (https=)
SI (1) SI2349260T1 (https=)
SM (1) SMT201600080B (https=)
TW (2) TWI643622B (https=)
WO (1) WO2010039939A1 (https=)

Families Citing this family (126)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005105814A1 (en) * 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
EP2455382B1 (en) 2005-12-13 2016-10-26 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
UA96457C2 (ru) 2006-08-03 2011-11-10 Нитек Фарма Аг Лечение ревматоидного артрита глюкокортикоидами с отсроченным высвобождением
AU2007322033B2 (en) 2006-11-20 2013-07-11 President And Fellows Of Harvard College Methods, compositions, and kits for treating pain and pruritis
EP3070090B1 (en) 2007-06-13 2018-12-12 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
WO2009064835A1 (en) * 2007-11-16 2009-05-22 Incyte Corporation 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
CA3121743A1 (en) 2009-01-15 2010-07-22 Incyte Holdings Corporation Processes for preparing jak inhibitors and related intermediate compounds
AU2010207740B2 (en) * 2009-01-26 2016-06-16 Nitec Pharma Ag Delayed-release glucocorticoid treatment of asthma
JP5775070B2 (ja) * 2009-05-22 2015-09-09 インサイト・コーポレイションIncyte Corporation ヤヌスキナーゼ阻害剤としてのピラゾール−4−イル−ピロロ[2,3−d]ピリミジンおよびピロール−3−イル−ピロロ[2,3−d]ピリミジンのN−(ヘテロ)アリール−ピロリジン誘導体
SG176111A1 (en) * 2009-05-22 2011-12-29 Incyte Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
JP6205133B2 (ja) 2009-07-10 2017-09-27 プレジデント アンド フェローズ オブ ハーバード カレッジ 抗炎症剤としての恒久的に荷電したナトリウムおよびカルシウムチャンネルブロッカー
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
KR101921850B1 (ko) * 2009-10-09 2018-11-23 인사이트 홀딩스 코포레이션 3-(4-(7H-피롤로〔2,3-d〕피리미딘-4-일)-1H-피라졸-1-일)-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체
US9242987B2 (en) 2009-10-20 2016-01-26 Cellzome Limited Heterocyclyl pyrazolopyrimidine analogues as JAK inhibitors
PT3354652T (pt) * 2010-03-10 2020-07-20 Incyte Holdings Corp Derivados de piperidin-4-ilazetidina como inibidores de jak1
BR112012027803A2 (pt) 2010-04-30 2016-08-09 Cellzome Ltd compostos de pirazol como inibidores de jak
RS54824B1 (sr) 2010-05-21 2016-10-31 Incyte Holdings Corp Topikalna formulacija za inhibiciju jak-a
AU2011258005A1 (en) * 2010-05-28 2013-01-17 Biocryst Pharmaceuticals, Inc. Heterocyclic compounds as Janus kinase inhibitors
EP2588105A1 (en) 2010-07-01 2013-05-08 Cellzome Limited Triazolopyridines as tyk2 inhibitors
US9040545B2 (en) 2010-08-20 2015-05-26 Cellzome Limited Heterocyclyl pyrazolopyrimidine analogues as selective JAK inhibitors
AU2011328237A1 (en) 2010-11-09 2013-05-23 Cellzome Limited Pyridine compounds and aza analogues thereof as TYK2 inhibitors
WO2012068440A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
EA036970B1 (ru) * 2010-11-19 2021-01-21 Инсайт Холдингс Корпорейшн Применение {1-{1-[3-фтор-2-(трифтометил)изоникотиноил] пиперидин-4-ил}-3-[4-(7h-пирроло[2,3-d]пиримидин-4-ил)-1н-пиразол-1-ил]азетидин-3-ил}ацетонитрила для лечения заболеваний, связанных с активностью jak1
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
CA2827673C (en) 2011-02-18 2020-10-27 Novartis Pharma Ag Mtor/jak inhibitor combination therapy
WO2012127506A1 (en) 2011-03-22 2012-09-27 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
WO2012143320A1 (en) 2011-04-18 2012-10-26 Cellzome Limited (7h-pyrrolo[2,3-d]pyrimidin-2-yl)amine compounds as jak3 inhibitors
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
KR20140058543A (ko) 2011-07-08 2014-05-14 노파르티스 아게 신규 피롤로 피리미딘 유도체
CN103781780B (zh) 2011-07-28 2015-11-25 赛尔佐姆有限公司 作为jak抑制剂的杂环基嘧啶类似物
WO2013017479A1 (en) 2011-07-29 2013-02-07 Cellzome Limited Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors
WO2013017480A1 (en) 2011-07-29 2013-02-07 Cellzome Limited Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors
EP2741747A1 (en) 2011-08-10 2014-06-18 Novartis Pharma AG JAK P13K/mTOR COMBINATION THERAPY
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
WO2013041605A1 (en) 2011-09-20 2013-03-28 Cellzome Limited Pyrazolo[4,3-c]pyridine derivatives as kinase inhibitors
CN103957910A (zh) * 2011-10-21 2014-07-30 葛兰素史克有限责任公司 增加先天免疫反应的化合物和方法
CN104169272A (zh) 2011-12-23 2014-11-26 赛尔佐姆有限公司 作为激酶抑制剂的嘧啶-2,4-二胺衍生物
WO2013108644A1 (ja) * 2012-01-20 2013-07-25 京都府公立大学法人 レバミピドのアレルギー性結膜炎治療剤
US20130310340A1 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
EP2855451B1 (en) 2012-05-24 2017-10-04 Cellzome Limited Heterocyclyl pyrimidine analogues as tyk2 inhibitors
IN2015DN02008A (https=) 2012-09-21 2015-08-14 Advinus Therapeutics Ltd
CN104918945B (zh) 2012-11-01 2018-01-05 因赛特公司 作为jak抑制剂的三环稠合噻吩衍生物
CN113384546A (zh) 2012-11-15 2021-09-14 因赛特公司 鲁索利替尼的缓释剂型
US10130632B2 (en) 2012-11-27 2018-11-20 Beth Israel Deaconess Medical Center, Inc. Methods for treating renal disease
EP2951590A1 (en) 2013-02-04 2015-12-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
WO2014138168A1 (en) 2013-03-06 2014-09-12 Incyte Corporation Processes and intermediates for making a jak inhibitor
SMT201900223T1 (it) 2013-05-17 2019-07-11 Incyte Corp Sale di bipirazolo come inibitore di jak
SG10201801069QA (en) 2013-08-07 2018-03-28 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
US9289494B2 (en) 2013-11-20 2016-03-22 RestorTears, LLC Method of treating ocular disorders with compounds found in Harderian gland secretions
PH12020552277A1 (en) 2014-04-08 2023-07-17 Incyte Holdings Corp Treatment of b-cell malignancies by a combination jak and pi3k inhibitor
CN106687462A (zh) 2014-04-30 2017-05-17 因赛特公司 Jak1抑制剂的制备方法以及其新形式
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
CN105777754B (zh) 2014-12-16 2019-07-26 北京赛林泰医药技术有限公司 吡咯并嘧啶化合物
CN105924444B (zh) * 2015-03-11 2019-06-18 苏州晶云药物科技股份有限公司 Jak抑制剂的晶型及其制备方法
AU2016301282B2 (en) 2015-08-03 2022-03-17 Children's Medical Center Corporation Charged ion channel blockers and methods for use
CN106554363B (zh) * 2015-09-28 2019-03-05 正大天晴药业集团股份有限公司 一种Baricitinib中间体的制备方法
HK1252685A1 (zh) 2015-11-03 2019-05-31 Theravance Biopharma R&D Ip, Llc 用於治疗呼吸疾病的jak激酶抑制剂化合物
WO2017097224A1 (zh) * 2015-12-11 2017-06-15 四川科伦博泰生物医药股份有限公司 氮杂环丁烷衍生物、其制备方法及用途
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
WO2017114461A1 (zh) * 2015-12-31 2017-07-06 正大天晴药业集团股份有限公司 一种芦可替尼的合成工艺
CN107573348B (zh) * 2016-01-29 2019-09-03 上海宣创生物科技有限公司 巴瑞克替尼三氟乙酸盐b晶型及其制备方法
CN107573349A (zh) * 2016-02-01 2018-01-12 上海宣创生物科技有限公司 巴瑞克替尼磷酸盐h晶型及其制备方法
CN107200742A (zh) * 2016-03-18 2017-09-26 罗欣生物科技(上海)有限公司 一种巴瑞克替尼磷酸盐晶体及其制备方法
CN107759600A (zh) * 2016-06-16 2018-03-06 正大天晴药业集团股份有限公司 作为jak抑制剂的吡咯并嘧啶化合物的结晶
TW201811795A (zh) 2016-08-24 2018-04-01 美商亞闊股份有限公司 胺基-吡咯并嘧啶酮化合物及其用途
CN110072523A (zh) * 2016-09-07 2019-07-30 格利亚有限责任公司 通过脑神经的药理皮肤激活来治疗与神经退行性病症相关的症状
WO2018056268A1 (ja) * 2016-09-20 2018-03-29 参天製薬株式会社 炎症性眼疾患の治療及び/又は予防剤
WO2018056269A1 (ja) * 2016-09-20 2018-03-29 参天製薬株式会社 Jak阻害剤を含有する点眼剤
CZ2016816A3 (cs) 2016-12-21 2018-07-04 Zentiva, K.S. Krystalické formy 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrilu s kyselinou fosforečnou a způsob jejich přípravy
JP7112755B2 (ja) * 2017-01-23 2022-08-04 シャンハイ ロングウッド バイオファーマシューティカルズ カンパニー リミテッド Jak酵素阻害剤及びその製造方法と用途
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
WO2018189335A1 (en) 2017-04-13 2018-10-18 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma
ES2937823T3 (es) * 2017-06-07 2023-03-31 Sichuan Kelun Biotech Biopharmaceutical Co Ltd Forma sólida del derivado de azetidina y método de preparación del mismo y uso del mismo
US10759865B2 (en) * 2017-08-22 2020-09-01 Eyal Levit Treatment of diabetes mellitus
US20220143075A1 (en) * 2017-09-25 2022-05-12 Surface Ophthalmics, Inc. Ophthalmic pharmaceutical compositions and methods for treating ocular surface disease
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
EP3710431A4 (en) 2017-11-03 2021-07-07 Aclaris Therapeutics, Inc. SUBSTITUTED PYRROLOPYRIMIDINE-BASED JAK INHIBITORS AND THEIR MANUFACTURING AND USE PROCEDURES
CN109867676B (zh) * 2017-12-01 2020-10-30 北京普祺医药科技有限公司 一种吡咯并嘧啶衍生的化合物、药物组合物以及其用途
CN109867675B (zh) * 2017-12-01 2021-01-19 北京普祺医药科技有限公司 一种吡咯并嘧啶衍生的化合物、药物组合物以及其用途
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
EA202091830A1 (ru) 2018-01-30 2020-12-29 Инсайт Корпорейшн Способы и промежуточные соединения для получения ингибитора jak
IL311485B1 (en) 2018-02-16 2026-01-01 Incyte Corp JAK1 pathway inhibitors for the treatment of cytokine-related disorders
WO2019191679A1 (en) 2018-03-30 2019-10-03 Incyte Corporation Biomarkers for inflammatory skin disease
MD3773593T2 (ro) 2018-03-30 2024-10-31 Incyte Corp Tratament hidradenitei supurative utilizând inhibitori ai JAK
CA3097025A1 (en) 2018-04-13 2019-10-17 Incyte Corporation Biomarkers for graft-versus-host disease
IT201800005599A1 (it) * 2018-05-22 2019-11-22 Lente a contatto morbida
CA3101323A1 (en) 2018-06-01 2019-12-05 Incyte Corporation Dosing regimen for the treatment of pi3k related disorders
WO2020033955A1 (en) 2018-08-10 2020-02-13 Aclaris Therapeutics, Inc. Pyrrolopyrimidine itk inhibitors
BR112021007877A2 (pt) 2018-10-26 2021-08-03 Viramal Limited composição em gel mucoadesiva
CA3117969A1 (en) 2018-10-31 2020-05-07 Incyte Corporation Combination therapy for treatment of hematological diseases
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
EP3659583B1 (en) 2018-11-30 2023-06-07 Viramal Limited A method of preparing a gelling agent, the gelling agent obtained thereby, and the use of said gelling agent
CN111320633B (zh) * 2018-12-14 2022-09-27 中国医药研究开发中心有限公司 吡咯/咪唑并六元杂芳环类化合物及其制备方法和医药用途
CN113508114B (zh) * 2019-02-27 2024-03-26 四川科伦博泰生物医药股份有限公司 以氮杂环丁烷衍生物为活性成分的口服药物组合物、其制备方法及用途
US10786485B1 (en) 2019-03-11 2020-09-29 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US10780083B1 (en) 2019-03-11 2020-09-22 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
AU2020234961C1 (en) 2019-03-11 2025-08-14 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
BR112021017809A2 (pt) 2019-03-11 2021-11-23 Nocion Therapeutics Inc Bloqueadores de canais iônicos substituídos por éster e métodos para uso
CN113811305A (zh) 2019-03-11 2021-12-17 诺西恩医疗公司 带电的离子通道阻滞剂及其使用方法
WO2020223728A1 (en) 2019-05-02 2020-11-05 Aclaris Therapeutics, Inc. Substituted pyrrolopyridines as jak inhibitors
CN110028509B (zh) * 2019-05-27 2020-10-09 上海勋和医药科技有限公司 作为选择性jak2抑制剂的吡咯并嘧啶类化合物、其合成方法及用途
EP4041204A1 (en) 2019-10-10 2022-08-17 Incyte Corporation Biomarkers for graft-versus-host disease
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
WO2021091585A1 (en) 2019-11-06 2021-05-14 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
WO2021091586A1 (en) 2019-11-06 2021-05-14 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
CN115038443A (zh) 2019-11-22 2022-09-09 因西特公司 包含alk2抑制剂和jak2抑制剂的组合疗法
US11332446B2 (en) 2020-03-11 2022-05-17 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US12162851B2 (en) 2020-03-11 2024-12-10 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
FI4157831T3 (fi) 2020-06-02 2024-12-02 Incyte Corp Menetelmiä jak1-estäjän valmistamiseksi
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
AU2021318236A1 (en) * 2020-07-30 2023-03-09 Rohto Pharmaceutical Co., Ltd. Aqueous composition
CA3192099A1 (en) 2020-08-18 2022-02-24 Incyte Corporation Process and intermediates for preparing a jak inhibitor
CR20230130A (es) 2020-08-18 2023-07-13 Incyte Corp Proceso e intermedios para preparar un inhibidor de jak1
CN114085224A (zh) * 2020-08-25 2022-02-25 北京普祺医药科技有限公司 一种吡咯并嘧啶化合物的制备方法
WO2022125670A1 (en) 2020-12-08 2022-06-16 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
CN118420621A (zh) * 2021-02-07 2024-08-02 南京知和医药科技有限公司 一种磺酰胺类多环化合物及其制备方法与用途
CN118459504A (zh) * 2021-02-26 2024-08-09 南京知和医药科技有限公司 一种巴瑞替尼衍生物及其制备方法与用途
RS67455B1 (sr) 2021-05-03 2025-12-31 Incyte Corp Inhibitori jak1 puta za lečenje prurigo nodularisa
TW202317550A (zh) 2021-06-25 2023-05-01 美商施萬生物製藥研發 Ip有限責任公司 作為jak抑制劑之咪唑吲唑化合物
CN118317946A (zh) 2021-07-12 2024-07-09 因赛特公司 用于制备巴瑞替尼的方法和中间体
JP2025014078A (ja) * 2021-11-30 2025-01-29 興和株式会社 新規ニコチンアミド化合物及びその用途
EP4489858A4 (en) * 2022-03-07 2026-01-21 Harrow Ip Llc Extended-release pharmaceutical compositions for the treatment of eye conditions
KR20240069235A (ko) 2022-11-11 2024-05-20 주식회사 다운컴퍼니 디지털 에이전시 기반의 그로스 해킹 테스팅 플랫폼

Family Cites Families (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2985589A (en) * 1957-05-22 1961-05-23 Universal Oil Prod Co Continuous sorption process employing fixed bed of sorbent and moving inlets and outlets
DE3220113A1 (de) * 1982-05-28 1983-12-01 Basf Ag, 6700 Ludwigshafen Difluormethoxiphenylthiophosphorsaeureester
US4402832A (en) * 1982-08-12 1983-09-06 Uop Inc. High efficiency continuous separation process
US4548990A (en) 1983-08-15 1985-10-22 Ciba-Geigy Corporation Crosslinked, porous polymers for controlled drug delivery
US4498991A (en) * 1984-06-18 1985-02-12 Uop Inc. Serial flow continuous separation process
IT1258781B (it) * 1992-01-16 1996-02-29 Zambon Spa Composizione farmaceutica oftalmica contenente n-acetilcisteina e polivinilalcol
US5521184A (en) * 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
US5856326A (en) * 1995-03-29 1999-01-05 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5630943A (en) * 1995-11-30 1997-05-20 Merck Patent Gesellschaft Mit Beschrankter Haftung Discontinuous countercurrent chromatographic process and apparatus
US6060038A (en) * 1997-05-15 2000-05-09 Merck & Co., Inc. Radiolabeled farnesyl-protein transferase inhibitors
CA2295620A1 (en) * 1997-08-11 1999-02-18 Boehringer Ingelheim Pharmaceuticals, Inc. 5,6-heteroaryl-dipyrido¬2,3-b:3',2'-f|azepines and their use in the prevention or treatment of hiv infection
US6232320B1 (en) * 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
PA8474101A1 (es) * 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
ATE459616T1 (de) 1998-08-11 2010-03-15 Novartis Ag Isochinoline derivate mit angiogenesis-hemmender wirkung
FR2785196B1 (fr) * 1998-10-29 2000-12-15 Inst Francais Du Petrole Procede et dispositif de separation avec des zones chromatographiques a longueur variable
US6375839B1 (en) * 1998-10-29 2002-04-23 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic zones
US6413419B1 (en) * 1998-10-29 2002-07-02 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
US6217895B1 (en) * 1999-03-22 2001-04-17 Control Delivery Systems Method for treating and/or preventing retinal diseases with sustained release corticosteroids
US6239113B1 (en) * 1999-03-31 2001-05-29 Insite Vision, Incorporated Topical treatment or prevention of ocular infections
OA12514A (en) * 1999-12-24 2006-05-29 Aventis Pharma Ltd Azaindoles.
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7235551B2 (en) * 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
EP1142566B1 (fr) * 2000-04-07 2003-10-01 Laboratoire Medidom S.A. Formulations ophtalmiques à base de ciclosporine, d'acide hyaluronique et du polysorbate
US7498304B2 (en) * 2000-06-16 2009-03-03 Curis, Inc. Angiogenesis-modulating compositions and uses
US6335342B1 (en) * 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
ES2344831T3 (es) * 2000-06-23 2010-09-08 Mitsubishi Tanabe Pharma Corporation Potenciadores de un efecto antitumoral.
WO2002055496A1 (en) * 2001-01-15 2002-07-18 Glaxo Group Limited Aryl piperidine and piperazine derivatives as inducers of ldl-receptor expression
AU2002308748A1 (en) * 2001-05-16 2002-11-25 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
EP1414443B1 (en) * 2001-08-01 2006-11-15 Merck & Co., Inc. BENZIMIDAZO 4,5-f|ISOQUINOLINONE DERIVATIVES
IL160915A0 (en) 2001-09-19 2004-08-31 Aventis Pharma Sa Indolizines inhibiting kinase proteins
ES2269793T3 (es) 2001-10-30 2007-04-01 Novartis Ag Derivados de estaurospina como inhibidores de la actividad de tirosina quinasa receptora flt3.
EP1460059A4 (en) * 2001-11-30 2005-01-05 Teijin Ltd PROCESS FOR PRODUCING 5- (3-CYANOPHENYL) -3-FORMYLBENZOIC ACID COMPOUND
US6995144B2 (en) * 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
TW200403058A (en) * 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
AU2003237121A1 (en) * 2002-04-26 2003-11-10 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
WO2003094888A1 (en) * 2002-05-07 2003-11-20 Control Delivery Systems, Inc. Processes for forming a drug delivery device
DE60317198T2 (de) * 2002-05-23 2008-12-04 Cytopia Research Pty. Ltd., Richmond Proteinkinaseinhibitoren
TW200406374A (en) 2002-05-29 2004-05-01 Novartis Ag Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
US20060004010A1 (en) * 2002-07-10 2006-01-05 Hiromu Habashita Ccr4 antagonist and medical use thereof
CA2497977A1 (en) * 2002-09-20 2004-04-01 Alcon, Inc. Use of cytokine synthesis inhibitors for the treatment of dry eye disorders
US20040204404A1 (en) * 2002-09-30 2004-10-14 Robert Zelle Human N-type calcium channel blockers
CL2003002353A1 (es) 2002-11-15 2005-02-04 Vertex Pharma Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
UY28126A1 (es) * 2002-12-24 2004-06-30 Alcon Inc Uso de glucocorticoides selectivos para la superficie ocular en el tratamiento de la sequedad ocular
JP2006518381A (ja) * 2003-02-07 2006-08-10 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
US7183941B2 (en) * 2003-07-30 2007-02-27 Lear Corporation Bus-based appliance remote control
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
CN1870997B (zh) * 2003-10-24 2011-05-04 参天制药株式会社 角膜结膜病变的治疗剂
MXPA06007076A (es) * 2003-12-19 2006-08-31 Pharmacopeia Drug Discovery Tiadiazoles como ligandos del receptor cxc y cc-quimiocina.
WO2005067546A2 (en) * 2004-01-13 2005-07-28 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
WO2005105814A1 (en) * 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
EP1760071A4 (en) * 2004-06-23 2008-03-05 Ono Pharmaceutical Co COMPOUND WITH S1P RECEPTOR BINDING ABILITY AND USE THEREOF
DE102004038530B3 (de) * 2004-08-07 2006-01-05 Universität Mannheim Verfahren und Vorrichtung zur Herstellung einer optischen Verbindung zwischen einem optoelektronischen Bauelement und einem Lichtwellenleiter
WO2006040036A1 (en) * 2004-10-13 2006-04-20 F. Hoffmann-La Roche Ag Disubstituted pyrazolobenzodiazepines useful as inhibitors for cdk2 and angiogesis, and for the treatment of breast, colon, lung and prostate cancer
US7517870B2 (en) * 2004-12-03 2009-04-14 Fondazione Telethon Use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/or reversing ocular diseases related with ocular neovascularization
WO2006065916A1 (en) * 2004-12-14 2006-06-22 Alcon, Inc. Method of treating dry eye disorders using 13(s)-hode and its analogs
AR054416A1 (es) * 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
CA2596830A1 (en) * 2005-02-03 2006-09-14 Vertex Pharmaceuticals Incorporated Pyrrolopyrimidines useful as inhibitors of protein kinase
WO2006127587A1 (en) * 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
WO2006133426A2 (en) * 2005-06-08 2006-12-14 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
EP2251341A1 (en) * 2005-07-14 2010-11-17 Astellas Pharma Inc. Heterocyclic Janus kinase 3 inhibitors
EP2270014A1 (en) * 2005-09-22 2011-01-05 Incyte Corporation Azepine inhibitors of janus kinases
CN103626742B (zh) * 2005-11-01 2017-04-26 塔格根公司 激酶的联-芳基间-嘧啶抑制剂
WO2007062459A1 (en) * 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
EP2455382B1 (en) * 2005-12-13 2016-10-26 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
SI1962830T1 (sl) * 2005-12-23 2013-07-31 Glaxosmithkline Llc Azaindolni inhibitorji kinaz Aurora
US20070208053A1 (en) * 2006-01-19 2007-09-06 Arnold Lee D Fused heterobicyclic kinase inhibitors
WO2007090141A2 (en) * 2006-02-01 2007-08-09 Smithkline Beecham Corporation Pyrrolo [2, 3, b] pyridine derivatives useful as raf kinase inhibitors
KR20090008217A (ko) * 2006-03-10 2009-01-21 오노 야꾸힝 고교 가부시키가이샤 질소 함유 복소환 유도체 및 이들을 유효 성분으로 하는 약제
MX2008012738A (es) * 2006-04-03 2009-02-06 Astellas Pharma Inc Heterocompuesto.
JP2009532475A (ja) * 2006-04-05 2009-09-10 バーテックス ファーマシューティカルズ インコーポレイテッド ヤヌスキナーゼの阻害剤として有用なデアザプリン
US7691811B2 (en) * 2006-05-25 2010-04-06 Bodor Nicholas S Transporter-enhanced corticosteroid activity and methods and compositions for treating dry eye
EP2044061A2 (en) * 2006-07-20 2009-04-08 Mehmet Kahraman Benzothiophene inhibitors of rho kinase
US8492378B2 (en) * 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
JP5252404B2 (ja) * 2006-08-16 2013-07-31 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ピラジン化合物、その使用及び調製方法
TW200837064A (en) * 2006-10-04 2008-09-16 Pharmacopeia Inc 8-substituted 2-(benzimidazolyl)purine derivatives for immunosuppression
BRPI0718029A2 (pt) * 2006-11-06 2013-11-26 Supergen Inc Derivados de imidazo(1,2-b)piridazina e pirazolo(1,5-a)pirimidina e seu uso como inibidores da proteína cinase
US20080119496A1 (en) * 2006-11-16 2008-05-22 Pharmacopeia Drug Discovery, Inc. 7-Substituted Purine Derivatives for Immunosuppression
US20080132259A1 (en) * 2006-12-05 2008-06-05 Eric Vin System and method of providing access to instant messaging services via a wireless network
SG177221A1 (en) * 2006-12-15 2012-01-30 Abbott Lab Novel oxadiazole compounds
WO2008079292A1 (en) * 2006-12-20 2008-07-03 Amgen Inc. Heterocyclic compounds and their use in treating inflammation, angiogenesis and cancer
EP2121692B1 (en) * 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
CL2008001709A1 (es) * 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
US8541426B2 (en) * 2007-07-11 2013-09-24 Pfizer Inc. Pharmaceutical compositions and methods of treating dry eye disorders
BRPI0815042A2 (pt) * 2007-08-01 2015-02-10 Pfizer Compostos de pirazol
WO2009049028A1 (en) * 2007-10-09 2009-04-16 Targegen Inc. Pyrrolopyrimidine compounds and their use as janus kinase modulators
CN101977923B (zh) * 2008-01-18 2014-10-08 捷克有机化学和生物化学研究院 抑制细胞生长的7-脱氮嘌呤核苷
US8158616B2 (en) * 2008-03-11 2012-04-17 Incyte Corporation Azetidine and cyclobutane derivatives as JAK inhibitors
CA3121743A1 (en) * 2009-01-15 2010-07-22 Incyte Holdings Corporation Processes for preparing jak inhibitors and related intermediate compounds
SG176111A1 (en) * 2009-05-22 2011-12-29 Incyte Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
WO2010135731A1 (en) * 2009-05-22 2010-11-25 Kaufman Herbert E Preparations and methods for ameliorating or reducing presbyopia
JP5775070B2 (ja) * 2009-05-22 2015-09-09 インサイト・コーポレイションIncyte Corporation ヤヌスキナーゼ阻害剤としてのピラゾール−4−イル−ピロロ[2,3−d]ピリミジンおよびピロール−3−イル−ピロロ[2,3−d]ピリミジンのN−(ヘテロ)アリール−ピロリジン誘導体
AR078012A1 (es) * 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
KR101921850B1 (ko) * 2009-10-09 2018-11-23 인사이트 홀딩스 코포레이션 3-(4-(7H-피롤로〔2,3-d〕피리미딘-4-일)-1H-피라졸-1-일)-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체
EP2536729A1 (en) * 2010-02-18 2012-12-26 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
PT3354652T (pt) * 2010-03-10 2020-07-20 Incyte Holdings Corp Derivados de piperidin-4-ilazetidina como inibidores de jak1

Similar Documents

Publication Publication Date Title
JP2012504639A5 (https=)
AU2002334635B2 (en) Inhibitors of glycogen synthase kinase-3 (GSK-3) for treating glaucoma
AU2008322595B2 (en) Method of treating arthritis
MXPA03000407A (es) Formulacion oftalmica de una droga selectiva para la inhibicion de cicloxigenasa-2.
WO2022093818A1 (en) Ocular implant containing an active agent
JP2017043614A5 (https=)
JP7097181B2 (ja) 増殖性硝子体網膜症用メトトレキサート
US20220125791A1 (en) Novel devices
CN103249400B (zh) 用于治疗青光眼和高眼压症的腺苷a1激动剂
CN118119390A (zh) 用于延长释放克罗卡林疗法的组合物和方法
JP2024041947A (ja) 眼圧下降増強剤
JP2004503601A (ja) 眼のcox−2媒介疾患の処置及び予防におけるcox−2阻害剤の使用法
CN106604730A (zh) 角膜厚度调节剂
US10537579B2 (en) Rejection reaction suppressant
EP3606514A1 (en) Methods of preventing or treating ophthalmic diseases
JP2011144111A (ja) 軸性近視の予防または治療剤
US7589107B2 (en) Amelioration of vitrectomy-induced cataracts
US20070203190A1 (en) Hydroxylamines and derivatives for the inhibition of complement activation
CN119730855A (zh) 甾体化合物在制备预防和/或治疗眼科疾病药物中的应用
EP4284507A1 (en) Methods of treating ocular fibrotic pathologies
JP2013534251A (ja) 角膜混濁を治療するためのep2またはep4アゴニスト
ES2628321T3 (es) Mejora del resultado de una trabeculectomía
WO2023034466A1 (en) Cgrp antagonists for treating psoriasis
CN101389336A (zh) 用于抑制补体激活的羟胺类和衍生物
JP2009527565A (ja) 補体活性化を阻害するヒドロキシルアミンおよび誘導体