TWI335913B - Diaminotriazoles useful as inhibitors of protein kinases - Google Patents

Diaminotriazoles useful as inhibitors of protein kinases Download PDF

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TWI335913B
TWI335913B TW092132032A TW92132032A TWI335913B TW I335913 B TWI335913 B TW I335913B TW 092132032 A TW092132032 A TW 092132032A TW 92132032 A TW92132032 A TW 92132032A TW I335913 B TWI335913 B TW I335913B
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Taiwan
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doc
compound
phenyl
zry
group
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TW092132032A
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TW200413334A (en
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C Pierce Albert
Arnost Michael
J Davies Robert
J Forster Cornelia
Galullo Vincent
Grey Ronald
Ledeboer Mark
Tian Shi-Kai
Xu Jinwang
Binch Hayley
Henkel Greg
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Vertex Pharma
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI743484B (zh) * 2018-06-04 2021-10-21 瑞士商Ａｃ免疫公司 用於治療、改善或預防與tau聚集物相關之病症的新穎化合物

Families Citing this family (287)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
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
MXPA05012281A (es) 2003-05-14 2006-05-19 Torreypines Therapeutics Inc Compuestos y uso de los mismos en la modulacion beta amiloide.
CN100434428C (zh) 2003-05-23 2008-11-19 巴斯利尔药物股份公司 呋咱并苯并咪唑类化合物
RS53109B (sr) 2003-07-30 2014-06-30 Rigel Pharmaceuticals Inc. Jedinjenja 2,4 pirimidindiamina za upotrebu u tretmanu ili prevenciji autoimunih bolesti
AU2005212218A1 (en) * 2004-02-11 2005-08-25 Janssen Pharmaceutica, N.V. Process for the preparation of substituted triazole compounds
US20070167505A1 (en) * 2004-02-11 2007-07-19 Basilea Pharmaceutica Ag Substituted benzimidazoles and their use for inducing apoptosis
DK1791830T3 (da) 2004-09-17 2011-04-18 Vertex Pharma Diaminotriazol-forbindelser der er nyttige som protein-kinase-inhibitorer
AU2012205127B2 (en) * 2004-09-17 2014-10-30 Vertex Pharmaceuticals Incorporated Diaminotriazole Compounds Useful as Protein Kinase Inhibitors
KR20070061907A (ko) 2004-10-08 2007-06-14 얀센 파마슈티카 엔.브이. 1,2,4-트리아졸일아미노아릴(헤테로아릴)설폰아미드 유도체
MX2007004551A (es) 2004-10-18 2007-05-23 Amgen Inc Compuestos tiadiazol y metodos de uso.
DE602005024293D1 (de) * 2004-10-21 2010-12-02 Vertex Pharma Triazole als hemmer von proteinkinasen
JP2008520612A (ja) * 2004-11-24 2008-06-19 ノバルティス アクチエンゲゼルシャフト ＪＡＫ阻害剤およびＢｃｒ−Ａｂｌ、Ｆｌｔ−３、ＦＡＫまたはＲＡＦキナーゼ阻害剤のうち少なくとも１個の組合せ
WO2006122150A1 (en) 2005-05-10 2006-11-16 Incyte Corporation Modulators of indoleamine 2,3-dioxygenase and methods of using the same
MX286273B (es) 2005-06-08 2011-05-04 Rigel Pharmaceuticals Inc Composiciones y metodos para inhibicion de la via jak.
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7825244B2 (en) 2005-06-10 2010-11-02 Janssen Pharmaceutica Nv Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
US20060281788A1 (en) 2005-06-10 2006-12-14 Baumann Christian A Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor
US8071768B2 (en) 2005-06-10 2011-12-06 Janssen Pharmaceutica, N.V. Alkylquinoline and alkylquinazoline kinase modulators
WO2006135915A2 (en) 2005-06-13 2006-12-21 Rigel Pharmaceuticals, Inc. Methods and compositions for treating degenerative bone disorders
DE602005000514T2 (de) * 2005-06-17 2007-10-25 Magneti Marelli Powertrain S.P.A. Brennstoffeinspritzventil
CN101291927A (zh) * 2005-07-26 2008-10-22 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的苯并咪唑
US7884119B2 (en) * 2005-09-07 2011-02-08 Rigel Pharmaceuticals, Inc. Triazole derivatives useful as Axl inhibitors
EP1926735A1 (en) 2005-09-22 2008-06-04 Incyte Corporation Tetracyclic inhibitors of janus kinases
JP2009511628A (ja) 2005-10-18 2009-03-19 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｆｌｔ３キナーゼの阻害方法
PT1966202E (pt) 2005-12-13 2012-01-03 Incyte Corp Pirrolo[2,3-b] pirimidinas e pirrolo[2,3-b]piridinas substituídas com heteroarilo como inibidores de janus quinase
BRPI0706621A2 (pt) 2006-01-18 2011-04-05 Amgen Inc composto, composição farmacêutica, métodos para tratar um distúrbio mediado por quinase em um mamìfero e para tratar um distúrbio relacionado com a proliferação em um mamìfero, e , uso do composto
CA2642229C (en) 2006-02-24 2015-05-12 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US8697716B2 (en) 2006-04-20 2014-04-15 Janssen Pharmaceutica Nv Method of inhibiting C-KIT kinase
WO2007124322A1 (en) 2006-04-20 2007-11-01 Janssen Pharmaceutica N.V. Inhibitors of c-fms kinase
SI2021335T1 (sl) 2006-04-20 2011-09-30 Janssen Pharmaceutica Nv Heterocikliäśne spojine kot zaviralci c-fms kinaze
WO2008011557A2 (en) * 2006-07-20 2008-01-24 Borchardt Allen J Heteroaryl inhibitors of rho kinase
CN103739595A (zh) 2006-10-02 2014-04-23 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
JP5161233B2 (ja) 2006-10-19 2013-03-13 ライジェル ファーマシューティカルズ， インコーポレイテッド 自己免疫疾患の処置のためのｊａｋキナーゼの阻害剤としての２，４−ピリミジンアミン誘導体
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
JP5567837B2 (ja) * 2006-12-29 2014-08-06 ライジェル ファーマシューティカルズ， インコーポレイテッド Ａｘｌインヒビターとして有用なＮ３−ヘテロアリール置換トリアゾールおよびＮ５−ヘテロアリール置換トリアゾール
WO2008083367A2 (en) 2006-12-29 2008-07-10 Rigel Pharmaceuticals, Inc. Polycyclic heteroaryl substituted triazoles useful as axl inhibitors
AU2014200824B2 (en) * 2006-12-29 2016-12-15 Rigel Pharmaceuticals, Inc. Substituted triazoles useful as Axl inhibitors
CA2710230C (en) 2006-12-29 2016-02-23 Rigel Pharmaceuticals, Inc. Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
AU2016259396B2 (en) * 2006-12-29 2018-11-08 Rigel Pharmaceuticals, Inc. Substituted triazoles useful as Axl inhibitors
AU2014200825B2 (en) * 2006-12-29 2016-05-26 Rigel Pharmaceuticals, Inc. N3-heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles useful as Axl inhibitors
EP2079736B1 (en) * 2006-12-29 2017-10-18 Rigel Pharmaceuticals, Inc. Substituted triazoles useful as axl inhibitors
CA2710043C (en) 2006-12-29 2016-02-09 Rigel Pharmaceuticals, Inc. Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors
CN101778825A (zh) * 2007-03-22 2010-07-14 沃泰克斯药物股份有限公司 适用作詹纳斯激酶抑制剂的n-杂环类化合物
RS53245B2 (sr) 2007-06-13 2022-10-31 Incyte Holdings Corp Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila
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.
CN101707863A (zh) * 2007-06-15 2010-05-12 Irm责任有限公司 蛋白激酶抑制剂及其使用方法
WO2009011880A2 (en) * 2007-07-17 2009-01-22 Amgen Inc. Heterocyclic modulators of pkb
CA2693473A1 (en) 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of pkb
HRP20160949T1 (hr) 2007-09-10 2016-10-07 Boston Biomedical, Inc. Novi sastavi i metode za liječenje karcinoma
WO2009042677A2 (en) * 2007-09-24 2009-04-02 Farjo Rafal A Stat3 inhibiting compositions and methods
JO3240B1 (ar) 2007-10-17 2018-03-08 Janssen Pharmaceutica Nv c-fms مثبطات كيناز
ES2424023T3 (es) * 2007-10-18 2013-09-26 Janssen Pharmaceutica N.V. 1,2,4-triazoles trisustituidos
JO2784B1 (en) * 2007-10-18 2014-03-15 شركة جانسين فارماسوتيكا ان. في 5,3,1 - Triazole substitute derivative
WO2009054864A1 (en) * 2007-10-26 2009-04-30 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors
EP2902495B1 (en) * 2007-11-09 2019-12-25 The Salk Institute for Biological Studies Use of tam receptor activators as immunosuppressors
US8008013B2 (en) * 2007-11-16 2011-08-30 Oklahoma Medical Research Foundation Predicting and diagnosing patients with autoimmune disease
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
JP5711537B2 (ja) 2008-02-15 2015-05-07 ライジェル ファーマシューティカルズ， インコーポレイテッド ピリミジン−２−アミン化合物およびｊａｋキナーゼの阻害剤としてのその使用
BRPI0909040B8 (pt) 2008-03-11 2021-05-25 Incyte Holdings Corp derivados de azetidina e ciclobutano, seus usos, e composição
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
JP2011518219A (ja) 2008-04-22 2011-06-23 ポートラ ファーマシューティカルズ， インコーポレイテッド タンパク質キナーゼの阻害剤
EP2274288A2 (en) 2008-04-24 2011-01-19 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
US20100048557A1 (en) 2008-06-20 2010-02-25 Bing-Yan Zhu Triazolopyridine JAK Inhibitor Compounds and Methods
BRPI0909945A2 (pt) * 2008-06-20 2015-07-28 Genentech Inc "composto, composição farmacêutica, método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak2 quinase em um paciente, kit para o tratamento de uma doença ou distúrbio responsivo à inibição da jak quinase"
MX2011000235A (es) 2008-07-08 2011-02-23 Incyte Corp 1,2,5-oxadiazoles como inhibidores de indolamina 2,3-dioxigenasa.
JP5592884B2 (ja) 2008-07-09 2014-09-17 ライジェル ファーマシューティカルズ， インコーポレイテッド Ａｘｌ阻害剤として有用な多環式ヘテロアリール置換トリアゾール
WO2010005879A1 (en) 2008-07-09 2010-01-14 Rigel Pharmaceuticals, Inc. Bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
PL2325181T3 (pl) * 2008-07-10 2017-09-29 General Incorporated Association Pharma Valley Project Supporting Organization Inhibitor STAT3 zawierający jako składnik aktywny pochodną chinolinokarboksyamidu
TWI453207B (zh) * 2008-09-08 2014-09-21 Signal Pharm Llc 胺基三唑并吡啶，其組合物及使用其之治療方法
KR20110060894A (ko) * 2008-09-18 2011-06-08 아스테라스 세이야쿠 가부시키가이샤 복소환 카르복사미드 화합물
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
CN108042560A (zh) * 2008-12-04 2018-05-18 库尔纳公司 通过抑制针对沉默调节蛋白1的天然反义转录物来治疗沉默调节蛋白1相关的疾病
TWI469979B (zh) * 2008-12-24 2015-01-21 Bial Portela & Ca Sa 脂肪酸醯胺水解酶(faah)抑制劑、以及其藥學組成物與用途
CN102281875B (zh) * 2009-01-16 2017-09-22 里格尔药品股份有限公司 预防、治疗或应对转移癌的使用axl抑制剂的组合疗法
US8765727B2 (en) 2009-01-23 2014-07-01 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
AU2010223919B2 (en) 2009-03-13 2016-03-31 Les Laboratoires Servier Methods and compositions for cell-proliferation-related disorders
TW201100429A (en) 2009-05-22 2011-01-01 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
PL2432472T3 (pl) 2009-05-22 2020-03-31 Incyte Holdings Corporation 3-[4-(7H-Pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo]oktano- lub heptano-nitryle jako inhibitory JAK
JP5095035B2 (ja) * 2009-06-09 2012-12-12 アクテリオン ファーマシューティカルズ リミテッド フッ素化アミノトリアゾール誘導体
ME01838B (me) 2009-06-29 2014-12-20 Lncyte Holdings Corp Pirimidinoni kao inhibitori pi3k
NZ597379A (en) 2009-06-29 2014-04-30 Agios Pharmaceuticals Inc Therapeutic compounds and compositions
WO2011017178A1 (en) * 2009-07-28 2011-02-10 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
ES2435491T3 (es) 2009-10-09 2013-12-19 Incyte Corporation Derivados de hidroxilo, ceto y glucurónido de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo
EP3064595B1 (en) 2009-10-21 2019-02-27 Agios Pharmaceuticals, Inc. Methods for cell-proliferation-related disorders
US8759359B2 (en) 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
TW201130842A (en) 2009-12-18 2011-09-16 Incyte Corp Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors
WO2011083124A1 (en) 2010-01-05 2011-07-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Flt3 receptor antagonists for the treatment or the prevention of pain disorders
ES2539170T3 (es) 2010-01-12 2015-06-26 Ab Science Inhibidores de quinasas de oxazol
US8883785B2 (en) * 2010-01-25 2014-11-11 Chdi Foundation, Inc. Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
CN102844317B (zh) 2010-02-18 2015-06-03 因西特公司 作为Janus激酶抑制剂的环丁烷和甲基环丁烷衍生物
MX354212B (es) 2010-03-10 2018-02-19 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
CA2793527A1 (en) 2010-03-19 2011-09-22 Boston Biomedical, Inc. Use of naphthofuran derivatives in the treatment of cancer
DK3108750T3 (en) * 2010-03-19 2018-10-22 1Globe Biomedical Co Ltd NEW RELATIONS AND COMPOSITIONS TARGETED FOR CANCER STAM CELLS
JP6065183B2 (ja) * 2010-03-24 2017-01-25 アミテック セラピューティック ソリューションズ，インク． キナーゼ阻害に役立つ複素環式化合物
CA2796311A1 (en) 2010-04-14 2011-10-20 Incyte Corporation Fused derivatives as pi3k.delta. inhibitors
EA202091303A3 (ru) 2010-05-21 2021-05-31 Инсайт Холдингс Корпорейшн Композиция ингибитора jak для местного применения
WO2011163195A1 (en) 2010-06-21 2011-12-29 Incyte Corporation Fused pyrrole derivatives as pi3k inhibitors
JP2012102090A (ja) * 2010-10-15 2012-05-31 Sumitomo Chemical Co Ltd ピリミジン化合物およびその有害生物防除用途
WO2012061428A2 (en) 2010-11-01 2012-05-10 Portola Pharmaceuticals, Inc. Nicotinamides as jak kinase modulators
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
WO2012068440A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
JP5961187B2 (ja) 2010-12-20 2016-08-02 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｐｉ３ｋ阻害剤としてのｎ−（１−（置換フェニル）エチル）−９ｈ−プリン−６−アミン
EP2675451B9 (en) 2011-02-18 2017-07-26 Novartis Pharma AG mTOR/JAK INHIBITOR COMBINATION THERAPY
AU2012243226A1 (en) * 2011-03-01 2013-09-26 Npharmakon, Llc Use of N-(4-methoxyphenyl)-1-phenyl-1H-pyrazol-3-amine and related compounds
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
PH12017501176B1 (en) 2011-05-03 2023-03-08 Agios Pharmaceuticals Inc Pyruvate kinase activators for use in therapy
CN102827073A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
CN102827170A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
HK1198579A1 (en) 2011-08-10 2015-04-30 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
MY166890A (en) 2011-08-30 2018-07-24 Chdi Foundation Inc Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
US9428464B2 (en) 2011-08-30 2016-08-30 Chdi Foundation, Inc. Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
SI3513793T1 (sl) 2011-09-02 2021-07-30 Incyte Holdings Corporation Heterociklilamini kot zaviralci PI3K
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
WO2013049591A2 (en) * 2011-09-29 2013-04-04 Verseon Corporation Dual inhibitor compounds and methods of use thereof
CA2856301C (en) 2011-11-23 2020-10-06 Portola Pharmaceuticals, Inc. Pyrazine kinase inhibitors
AU2013207289B2 (en) 2012-01-06 2017-09-21 Les Laboratoires Servier Therapeutically active compounds and their methods of use
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
WO2013122575A2 (en) * 2012-02-14 2013-08-22 Grl Small molecule having antiviral properties
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
AU2013258107B2 (en) 2012-05-08 2017-06-22 Bayer Pharma Aktiengesellschaft Method for the preparation of triazole compounds
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
SI2861595T1 (sl) 2012-06-13 2017-04-26 Incyte Holdings Corporation Substituirane triciklične spojine kot inhibitorji fgfr
US20140010783A1 (en) * 2012-07-06 2014-01-09 Hoffmann-La Roche Inc. Antiviral compounds
US20150148292A1 (en) * 2012-07-09 2015-05-28 Emory University Bone morphogenetic protein pathway activation, compositions for ossification, and methods related thereto
JOP20180012A1 (ar) 2012-08-07 2019-01-30 Janssen Pharmaceutica Nv عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد
ES2608628T3 (es) 2012-08-07 2017-04-12 Janssen Pharmaceutica Nv Procedimiento para la preparacion de derivados de ester heterociclicos
KR101738063B1 (ko) 2012-09-21 2017-05-19 아로그 파마슈티칼스, 인코퍼레이티드 구조적으로 활성인 인산화된 ｆｌｔ３ 키나제의 억제 방법
EP2903970A4 (en) 2012-10-08 2016-11-30 Portola Pharm Inc SUBSTITUTED PYRIMIDINYL KINASE INHIBITORS
WO2014062511A1 (en) 2012-10-15 2014-04-24 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions
BR112015009942A2 (pt) 2012-11-01 2017-07-11 Incyte Corp derivados de tiofeno fundidos tricíclicos como inibidores de jak
NZ708157A (en) 2012-11-15 2019-07-26 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
BR112015016282A2 (pt) 2013-01-07 2017-07-11 Arog Pharmaceuticals Inc crenolanibe para tratamento de distúrbios proliferativos de flt3 mutado
TWI687220B (zh) 2013-03-01 2020-03-11 美商英塞特控股公司 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途
US9896433B2 (en) * 2013-03-05 2018-02-20 Hoffmann-La Roche Inc. Antiviral compounds
MX2015011125A (es) * 2013-03-05 2015-11-11 Hoffmann La Roche Compuestos antivirales.
EP2964635B1 (en) 2013-03-06 2018-05-02 F.Hoffmann-La Roche Ag Antiviral compounds
TWI634121B (zh) 2013-03-06 2018-09-01 英塞特控股公司 用於製備ｊａｋ抑制劑之方法及中間物
WO2014169078A2 (en) 2013-04-09 2014-10-16 Boston Biomedical, Inc. Methods for treating cancer
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
WO2014186706A1 (en) 2013-05-17 2014-11-20 Incyte Corporation Bipyrazole derivatives as jak inhibitors
WO2015003360A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
EP3019490B1 (en) 2013-07-11 2020-06-03 Agios Pharmaceuticals, Inc. N,6-bis(aryl or heteroaryl)-1,3,5-triazine-2,4-diamine compounds as idh2 mutants inhibitors for the treatment of cancer
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
WO2015003355A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
CA2917671A1 (en) * 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. 2,4-or 4,6-diaminopyrimidine compounds as idh2 mutants inhibitors for the treatment of cancer
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
MX394928B (es) 2013-08-07 2025-03-24 Incyte Holdings Corp Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1).
CN105555313A (zh) 2013-08-20 2016-05-04 因赛特公司 在c-反应蛋白水平较高的实体肿瘤患者中的存活益处
US10463658B2 (en) 2013-10-25 2019-11-05 Videra Pharmaceuticals, Llc Method of inhibiting FLT3 kinase
SG11201607083VA (en) 2014-02-28 2016-09-29 Incyte Corp Jak1 inhibitors for the treatment of myelodysplastic syndromes
KR20220070066A (ko) 2014-03-14 2022-05-27 아지오스 파마슈티컬스 아이엔씨. 치료적으로 활성인 화합물의 약제학적 조성물
HRP20201887T1 (hr) 2014-04-08 2021-02-05 Incyte Corporation LIJEČENJE B-STANIČNIH MALIGNITETA S KOMBINACIJOM INHIBITORA JAK i PI3K
SG11201609016VA (en) 2014-04-30 2016-11-29 Incyte Corp Processes of preparing a jak1 inhibitor and new forms thereto
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
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
JP2017520610A (ja) 2014-07-17 2017-07-27 シーエイチディーアイ ファウンデーション，インコーポレーテッド Ｈｉｖ関連障害を治療するための方法及び組成物
US10065937B2 (en) 2014-07-31 2018-09-04 Inserm (Institut National De La Sante Et De La Recherche Medicale) FLT3 receptor antagonists
US9586949B2 (en) 2015-02-09 2017-03-07 Incyte Corporation Aza-heteroaryl compounds as PI3K-gamma inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
SG10201913036RA (en) 2015-02-20 2020-02-27 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
MA41607B1 (fr) 2015-02-27 2021-01-29 Incyte Corp Sels d'un inhibiteur de pi3k et procédés de préparation de ces sels
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016183062A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Salts of (s)-7-(1-(9h-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5h-thiazolo[3,2-a]pyrimidin-5-one
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
SI3307271T1 (sl) 2015-06-11 2023-11-30 Agios Pharmaceuticals, Inc. Postopki za uporabo aktivatorjev piruvat kinaze
PT3362065T (pt) 2015-10-15 2024-06-21 Servier Lab Terapia de combinação compreendendo ivosidenib, citarabina e daunorubicina ou idarubicina para o tratamento de leucemia mielóide aguda
US10653710B2 (en) 2015-10-15 2020-05-19 Agios Pharmaceuticals, Inc. Combination therapy for treating malignancies
AR106595A1 (es) 2015-11-06 2018-01-31 Incyte Corp COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g
EP3792256B1 (en) 2016-01-05 2024-10-23 Incyte Corporation Pyridine compounds as pi3k-gamma inhibitors
EP3241830A1 (de) 2016-05-04 2017-11-08 Bayer CropScience Aktiengesellschaft Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel
EP3254698A1 (en) 2016-06-08 2017-12-13 Universite De Montpellier Flt3 receptor inhibitor at low dosage for the treatment of neuropathic pain
TW201803871A (zh) 2016-06-24 2018-02-01 英塞特公司 作為ＰＩ３Ｋ-γ抑制劑之雜環化合物
CA3030581C (en) * 2016-07-18 2021-05-25 National Institute Of Biological Sciences, Beijing Apoptosis inhibitors
AU2017353925A1 (en) 2016-11-02 2018-09-27 Arog Pharmaceuticals, Inc. Crenolanib for treating FLT3 mutated proliferative disorders associated mutations
CA3045306A1 (en) 2016-11-29 2018-06-07 Boston Biomedical, Inc. Naphthofuran derivatives, preparation, and methods of use thereof
RU2629360C1 (ru) * 2016-12-08 2017-08-29 Федеральное государственное бюджетное образовательное учреждение высшего образования "Московский технологический университет" НОВЫЕ 1-β-D-РИБОФУРАНОЗИЛ-3-(5-ЗАМЕЩЕННЫЕ-1,2,4-ОКСАДИАЗОЛ-3-ИЛ)-1,2,4-ТРИАЗОЛЫ, ОБЛАДАЮЩИЕ ПРОТИВОВИРУСНЫМИ СВОЙСТВАМИ, И СПОСОБ ИХ ПОЛУЧЕНИЯ
JP2020520923A (ja) 2017-05-17 2020-07-16 ボストン バイオメディカル， インコーポレイテッド がんを処置するための方法
WO2018211018A1 (en) 2017-05-17 2018-11-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Flt3 inhibitors for improving pain treatments by opioids
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
WO2019057649A1 (en) 2017-09-19 2019-03-28 INSERM (Institut National de la Santé et de la Recherche Médicale) METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF ACUTE MYELOID LEUKEMIA
MX2020003862A (es) 2017-10-18 2020-08-13 Incyte Corp Derivados condensados de imidazol sustituidos por grupos hidroxi terciarios como inhibidores de fosfoinositido 3-cinasas gamma (pi3k-gamma).
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
US11306079B2 (en) 2017-12-21 2022-04-19 Incyte Corporation 3-(5-amino-pyrazin-2-yl)-benzenesulfonamide derivatives and related compounds as PI3K-gamma kinase inhibitors
GB201801226D0 (en) * 2018-01-25 2018-03-14 Redx Pharma Plc Modulators of Rho-associated protein kinase
WO2019152374A1 (en) 2018-01-30 2019-08-08 Incyte Corporation Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
WO2019161098A1 (en) 2018-02-16 2019-08-22 Incyte Corporation Jak1 pathway inhibitors for the treatment of cytokine-related disorders
AU2019227607C1 (en) 2018-02-27 2023-07-20 Incyte Corporation Imidazopyrimidines and triazolopyrimidines as A2A / A2B inhibitors
WO2019226213A2 (en) 2018-03-08 2019-11-28 Incyte Corporation AMINOPYRAZINE DIOL COMPOUNDS AS PI3K-y INHIBITORS
US11584961B2 (en) 2018-03-30 2023-02-21 Incyte Corporation Biomarkers for inflammatory skin disease
HUE067471T2 (hu) 2018-03-30 2024-10-28 Incyte Corp Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával
US11220510B2 (en) 2018-04-09 2022-01-11 Incyte Corporation Pyrrole tricyclic compounds as A2A / A2B inhibitors
DK3784661T3 (da) 2018-04-25 2024-02-12 Bayer Ag Hidtil ukendte heteroaryl-triazol- og heteroaryl-tetrazol-forbindelser som pesticider
PL3788047T3 (pl) 2018-05-04 2025-04-14 Incyte Corporation Stałe postacie inhibitora fgfr i sposoby ich otrzymywania
KR20210018264A (ko) 2018-05-04 2021-02-17 인사이트 코포레이션 Fgfr 억제제의 염
MA52940A (fr) 2018-05-18 2021-04-28 Incyte Corp Dérivés de pyrimidine fusionnés utilisés en tant qu'inhibiteurs de a2a/a2b
ES2929415T3 (es) 2018-05-25 2022-11-29 Incyte Corp Compuestos heterocíclicos tricíclicos como activadores de STING
BR112020024427A2 (pt) 2018-06-01 2021-03-23 Incyte Corporation regime de dosagem para o tratamento de distúrbios relacionados a pi3k
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
CA3105721A1 (en) 2018-07-05 2020-01-09 Incyte Corporation Fused pyrazine derivatives as a2a / a2b inhibitors
WO2020028565A1 (en) 2018-07-31 2020-02-06 Incyte Corporation Tricyclic heteraryl compounds as sting activators
US10875872B2 (en) 2018-07-31 2020-12-29 Incyte Corporation Heteroaryl amide compounds as sting activators
WO2020036133A1 (ja) * 2018-08-17 2020-02-20 クミアイ化学工業株式会社 ３－（１ｈ－１，２，４－トリアゾール－１－イル）安息香酸アミド誘導体及び有害生物防除剤
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US11078204B2 (en) 2018-11-13 2021-08-03 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
WO2020102216A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Substituted heterocyclic derivatives as pi3k inhibitors
WO2020102150A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
US11596692B1 (en) 2018-11-21 2023-03-07 Incyte Corporation PD-L1/STING conjugates and methods of use
US12129267B2 (en) 2019-01-07 2024-10-29 Incyte Corporation Heteroaryl amide compounds as sting activators
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
EP3923949A1 (en) 2019-02-15 2021-12-22 Incyte Corporation Cyclin-dependent kinase 2 biomarkers and uses thereof
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
US11919904B2 (en) 2019-03-29 2024-03-05 Incyte Corporation Sulfonylamide compounds as CDK2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
MA56215A (fr) 2019-06-10 2022-04-20 Incyte Corp Traitement topique du vitiligo par un inhibiteur de jak
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN118496198A (zh) 2019-07-23 2024-08-16 拜耳公司 作为农药的新的杂芳基-三唑化合物
PH12022550166A1 (en) 2019-07-23 2022-11-14 Bayer Ag Novel heteroaryl-triazole compounds as pesticides
EP4007602A1 (en) 2019-08-01 2022-06-08 Incyte Corporation A dosing regimen for an ido inhibitor
PH12022550361A1 (en) 2019-08-14 2023-02-27 Incyte Corp Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
TW202115082A (zh) 2019-08-26 2021-04-16 美商英塞特公司 作為ａ２ａ／ａ２ｂ抑制劑之三唑并嘧啶
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7693656B2 (ja) 2019-10-11 2025-06-17 インサイト・コーポレイション Ｃｄｋ２阻害剤としての二環式アミン
CR20220169A (es) 2019-10-14 2022-10-27 Incyte Corp Heterociclos bicíclicos como inhibidores de fgfr
US11992490B2 (en) 2019-10-16 2024-05-28 Incyte Corporation Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
JP7518900B2 (ja) 2019-10-16 2024-07-18 インサイト・コーポレイション 皮膚エリテマトーデス及び扁平苔癬（ｌｐ）の治療のためのｊａｋ１阻害剤の使用
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JP7720840B2 (ja) 2019-12-04 2025-08-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式複素環
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AU2021230385A1 (en) 2020-03-06 2022-09-22 Incyte Corporation Combination therapy comprising AXL/MER and PD-1/PD-L1 inhibitors
PH12022552739A1 (en) 2020-04-16 2024-03-25 Incyte Corp Fused tricyclic kras inhibitors
GB202006382D0 (en) 2020-04-30 2020-06-17 Spermatech As Use
US11739102B2 (en) 2020-05-13 2023-08-29 Incyte Corporation Fused pyrimidine compounds as KRAS inhibitors
JP2023528868A (ja) 2020-06-02 2023-07-06 インサイト・コーポレイション Ｊａｋ１阻害剤の調製プロセス
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US11713310B2 (en) 2020-07-20 2023-08-01 Arog Pharmaceuticals, Inc. Crystal forms of crenolanib and methods of use thereof
WO2022047093A1 (en) 2020-08-28 2022-03-03 Incyte Corporation Vinyl imidazole compounds as inhibitors of kras
US20230364095A1 (en) 2020-09-16 2023-11-16 Incyte Corporation Topical treatment of vitiligo
WO2022072783A1 (en) 2020-10-02 2022-04-07 Incyte Corporation Bicyclic dione compounds as inhibitors of kras
WO2022090547A1 (en) 2020-10-30 2022-05-05 Dsm Ip Assets B.V. Production of carotenoids by fermentation
US11969420B2 (en) 2020-10-30 2024-04-30 Arog Pharmaceuticals, Inc. Combination therapy of crenolanib and apoptosis pathway agents for the treatment of proliferative disorders
JP2023552452A (ja) 2020-12-08 2023-12-15 インサイト・コーポレイション 白斑治療用のｊａｋ１経路阻害薬
WO2022155941A1 (en) 2021-01-25 2022-07-28 Qilu Regor Therapeutics Inc. Cdk2 inhibitors
WO2022206888A1 (en) 2021-03-31 2022-10-06 Qilu Regor Therapeutics Inc. Cdk2 inhibitors and use thereof
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法
US12268667B2 (en) 2021-05-03 2025-04-08 Incyte Corporation JAK1 pathway inhibitors for the treatment of prurigo nodularis
EP4352060A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
WO2023283213A1 (en) 2021-07-07 2023-01-12 Incyte Corporation Tricyclic compounds as inhibitors of kras
US20230114765A1 (en) 2021-07-14 2023-04-13 Incyte Corporation Tricyclic compounds as inhibitors of kras
US12441742B2 (en) 2021-08-31 2025-10-14 Incyte Corporation Naphthyridine compounds as inhibitors of KRAS
US12030883B2 (en) 2021-09-21 2024-07-09 Incyte Corporation Hetero-tricyclic compounds as inhibitors of KRAS
JP2024537824A (ja) 2021-10-01 2024-10-16 インサイト・コーポレイション ピラゾロキノリンｋｒａｓ阻害剤
WO2023064458A1 (en) * 2021-10-13 2023-04-20 Yale University Selective jak2 inhibitors and methods of use
MX2024004444A (es) 2021-10-14 2024-05-08 Incyte Corp Compuestos de quinolina como inhibidores de la proteina del virus de sarcoma de rata kirsten (kras).
US20230226040A1 (en) 2021-11-22 2023-07-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a kras inhibitor
TW202329937A (zh) 2021-12-03 2023-08-01 美商英塞特公司 雙環胺ｃｋ１２抑制劑
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
US20230192722A1 (en) 2021-12-22 2023-06-22 Incyte Corporation Salts and solid forms of an fgfr inhibitor and processes of preparing thereof
WO2023168686A1 (en) 2022-03-11 2023-09-14 Qilu Regor Therapeutics Inc. Substituted cyclopentanes as cdk2 inhibitors
TW202341982A (zh) 2021-12-24 2023-11-01 大陸商上海齊魯銳格醫藥研發有限公司 Ｃｄｋ２抑制劑及其用途
US20230279004A1 (en) 2022-03-07 2023-09-07 Incyte Corporation Solid forms, salts, and processes of preparation of a cdk2 inhibitor
EP4540252A1 (en) 2022-06-14 2025-04-23 Incyte Corporation Solid forms of a jak inhibitor and process of preparing the same
US20250353842A1 (en) 2022-06-22 2025-11-20 Incyte Corporation Bicyclic amine cdk12 inhibitors
WO2024015731A1 (en) 2022-07-11 2024-01-18 Incyte Corporation Fused tricyclic compounds as inhibitors of kras g12v mutants
US20240058343A1 (en) 2022-08-05 2024-02-22 Incyte Corporation Treatment of urticaria using jak inhibitors
WO2024051667A1 (zh) * 2022-09-05 2024-03-14 南京正大天晴制药有限公司 具有axl抑制活性的取代三唑化合物
US20240368156A1 (en) 2023-04-18 2024-11-07 Incyte Corporation 2-azabicyclo[2.2.1]heptane kras inhibitors
WO2024220532A1 (en) 2023-04-18 2024-10-24 Incyte Corporation Pyrrolidine kras inhibitors
CN121039109A (zh) * 2023-04-18 2025-11-28 国家科学研究中心 3,5-二氨基三唑衍生物及其用于治疗眼部疾病的用途
WO2024254245A1 (en) 2023-06-09 2024-12-12 Incyte Corporation Bicyclic amines as cdk2 inhibitors
WO2025080695A1 (en) * 2023-10-10 2025-04-17 Collaborations Pharmaceuticals, Inc. 1-sulfonyl-3-amino-1h-1,2,4-triazoles as yellow fever virus inhibitors
US20250163079A1 (en) 2023-11-01 2025-05-22 Incyte Corporation Kras inhibitors
WO2025129002A1 (en) 2023-12-13 2025-06-19 Incyte Corporation Bicyclooctane kras inhibitors

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK113716B (da) * 1960-07-30 1969-04-21 Takeda Chemical Industries Ltd Fremgangsmåde til fremstilling af 1-[pyrimidinyl-(2)]-guanazolforbindelser eller salte deraf.
AU5775198A (en) * 1997-01-14 1998-08-03 Egis Gyogyszergyar Rt. 2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives having an effect on the c.n.s. and the heart
JP2001522853A (ja) * 1997-11-11 2001-11-20 ファイザー・プロダクツ・インク 抗癌剤として有用なチエノピリミジンおよびチエノピリジン誘導体
JP2002510033A (ja) * 1998-01-12 2002-04-02 ザ・サルク・インスティチュート 二重微小ｄｎａを有する細胞を処理するための組成物およびその処理方法
US6599910B1 (en) 1998-08-20 2003-07-29 Smithkline Beecham Corporation Substituted triazole compounds
EP1126843A4 (en) * 1998-10-29 2005-06-15 Bristol Myers Squibb Co AMINO-CELL DERIVATIVE COMPOUNDS INHIBITORS OF ENZYME IMPDH
US6596747B2 (en) * 1998-10-29 2003-07-22 Bristol-Myers Squibb Company Compounds derived from an amine nucleus and pharmaceutical compositions comprising same
AU782878B2 (en) * 2000-02-05 2005-09-08 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of erk
DE60120494T2 (de) * 2000-12-22 2006-12-21 Ortho-Mcneil Pharmaceutical, Inc. Substituieten triazoldiamin derivaten und ihre verwendung als kinase inhibitoren
DE10123586A1 (de) * 2001-05-08 2002-11-28 Schering Ag 3,5-Diamino-1,2,4-triazole als Kinase Inhibitoren
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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI743484B (zh) * 2018-06-04 2021-10-21 瑞士商Ａｃ免疫公司 用於治療、改善或預防與tau聚集物相關之病症的新穎化合物

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