MX2012007684A - Modificacion covalente ligando dirigida de proteina. - Google Patents

Modificacion covalente ligando dirigida de proteina.

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Publication number
MX2012007684A
MX2012007684A MX2012007684A MX2012007684A MX2012007684A MX 2012007684 A MX2012007684 A MX 2012007684A MX 2012007684 A MX2012007684 A MX 2012007684A MX 2012007684 A MX2012007684 A MX 2012007684A MX 2012007684 A MX2012007684 A MX 2012007684A
Authority
MX
Mexico
Prior art keywords
ligand
covalent modification
protein
directed covalent
directed
Prior art date
Application number
MX2012007684A
Other languages
English (en)
Inventor
Deqiang Niu
Juswinder Singh
Lixin Qiao
Russell C Petter
Zhendong Zhu
Charles F Jewell
Kwangho Lee
Aravind Prasad Medikonda
Original Assignee
Avila Therapeutics Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Avila Therapeutics Inc filed Critical Avila Therapeutics Inc
Publication of MX2012007684A publication Critical patent/MX2012007684A/es

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    • C12N9/96—Stabilising an enzyme by forming an adduct or a composition; Forming enzyme conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
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    • C12Y207/11—Protein-serine/threonine kinases (2.7.11)
    • C12Y207/11001—Non-specific serine/threonine protein kinase (2.7.11.1), i.e. casein kinase or checkpoint kinase
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    • C12Y304/21—Serine endopeptidases (3.4.21)
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    • C12Y603/02—Acid—amino-acid ligases (peptide synthases)(6.3.2)
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Abstract

La presente invención se relaciona con inhibidores de enzima. De manera más especial, la presente invención se relaciona a modificación covalente dirigida a ligando de proteínas; método del mismo diseño; formulación farmacéutica de la misma; y método de uso.
MX2012007684A 2009-12-30 2010-12-30 Modificacion covalente ligando dirigida de proteina. MX2012007684A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US33504309P 2009-12-30 2009-12-30
PCT/US2010/062473 WO2011082285A1 (en) 2009-12-30 2010-12-30 Ligand-directed covalent modification of protein

Publications (1)

Publication Number Publication Date
MX2012007684A true MX2012007684A (es) 2012-10-05

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Application Number Title Priority Date Filing Date
MX2012007684A MX2012007684A (es) 2009-12-30 2010-12-30 Modificacion covalente ligando dirigida de proteina.

Country Status (13)

Country Link
US (2) US20110269244A1 (es)
EP (1) EP2519664A4 (es)
JP (2) JP2013516422A (es)
KR (1) KR20130067487A (es)
CN (1) CN102812167A (es)
AU (2) AU2010339456A1 (es)
BR (1) BR112012015721A2 (es)
CA (1) CA2785738A1 (es)
MX (1) MX2012007684A (es)
RU (1) RU2012132473A (es)
SG (1) SG181965A1 (es)
TW (1) TW201134825A (es)
WO (1) WO2011082285A1 (es)

Families Citing this family (104)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100311711A1 (en) 2007-10-11 2010-12-09 The Regents Of The University Of California Inhibitors of NAAA and Methods Thereof
MX2010012703A (es) 2008-05-21 2010-12-21 Ariad Pharma Inc Derivados fosforosos como inhibidores de cinasa.
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
MY156789A (en) * 2008-09-05 2016-03-31 Celgene Avilomics Res Inc Algorithm for designing irreversible inhibitors
IN2012DN02534A (es) 2009-09-16 2015-08-28 Avila Therapeutics Inc
US20110269244A1 (en) 2009-12-30 2011-11-03 Petter Russell C Ligand-directed covalent modification of protein
BR112013027734A2 (pt) 2011-05-04 2017-08-08 Ariad Pharma Inc compostos para a inibição de proliferação celular em cânceres impulsionados pelo egfr, método e composição farmacêutica
WO2012170867A1 (en) * 2011-06-09 2012-12-13 Rhizen Pharmaceuticals Sa Novel compounds as modulators of gpr-119
KR101972619B1 (ko) 2011-09-29 2019-04-25 오노 야꾸힝 고교 가부시키가이샤 페닐 유도체
CA2856522C (en) * 2011-11-22 2020-10-27 The Regents Of The University Of California Disubstituted beta-lactones as inhibitors of n-acylethanolamine acid amidase (naaa)
AU2013204563B2 (en) 2012-05-05 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
US9617309B2 (en) * 2012-09-26 2017-04-11 President And Fellows Of Harvard College Proline-locked stapled peptides and uses thereof
CN103788071A (zh) * 2012-11-01 2014-05-14 中国人民解放军第二军医大学 N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途
US9493510B2 (en) 2013-01-10 2016-11-15 Noliva Therapeutics Llc Peptidomimetic compounds
EP3391898A3 (en) 2013-03-13 2019-02-13 President and Fellows of Harvard College Stapled and stitched polypeptides and uses thereof
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
WO2014144547A2 (en) 2013-03-15 2014-09-18 The Regents Of The University Of California Amide derivatives of lactam based n-acylethanolamine acid amidase (naaa) inhibitors
WO2014144836A2 (en) 2013-03-15 2014-09-18 The Regents Of The University Of California Carbamate derivatives of lactam based n-acylethanolamine acid amidase (naaa) inhibitors
WO2014143659A1 (en) 2013-03-15 2014-09-18 Araxes Pharma Llc Irreversible covalent inhibitors of the gtpase k-ras g12c
CA2907964A1 (en) 2013-03-26 2014-10-02 Ono Pharmaceutical Co., Ltd. Phenyl derivative
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
EP3636639A1 (en) * 2013-10-10 2020-04-15 Araxes Pharma LLC Inhibitors of kras g12c
CN111499562B (zh) * 2013-12-27 2023-12-26 株式会社Api 5-羟基哌啶-2-甲酸的制造方法
US10441654B2 (en) 2014-01-24 2019-10-15 Children's Hospital Of Eastern Ontario Research Institute Inc. SMC combination therapy for the treatment of cancer
CA2950911C (en) * 2014-06-04 2023-10-10 Sanford-Burnham Medical Research Institute Use of inhibitor of apoptosis protein (iap) antagonists in hiv therapy
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
JP2017528498A (ja) 2014-09-25 2017-09-28 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質のインヒビター
ES2898765T3 (es) * 2015-04-10 2022-03-08 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356353A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
US10414757B2 (en) 2015-11-16 2019-09-17 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
EP3426674A4 (en) 2016-03-09 2019-08-14 Blade Therapeutics, Inc. CYCLIC KETO AMID COMPOUNDS AS CALPAIN MODULATORS AND METHOD FOR THE PRODUCTION AND USE THEREOF
WO2017172979A1 (en) 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
SG11201810171SA (en) 2016-05-18 2018-12-28 Mirati Therapeutics Inc Kras g12c inhibitors
WO2018009417A1 (en) 2016-07-05 2018-01-11 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
KR20190063473A (ko) 2016-09-28 2019-06-07 블레이드 테라퓨틱스, 인크. 칼페인 조정자 및 그 치료학적 용도
WO2018064510A1 (en) 2016-09-29 2018-04-05 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
CN107314979A (zh) * 2016-10-09 2017-11-03 河南理工大学 一种基于罗丹明6g的铜离子传感器、制备及应用
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
WO2018140600A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused hetero-hetero bicyclic compounds and methods of use thereof
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
KR20200010306A (ko) 2017-05-25 2020-01-30 아락세스 파마 엘엘씨 Kras의 공유적 억제제
CN110869357A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 化合物及其用于治疗癌症的使用方法
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
WO2019087696A1 (ja) * 2017-11-01 2019-05-09 富士フイルム株式会社 経口医薬組成物
CA3080943A1 (en) 2017-11-01 2019-05-09 The Regents Of The University Of California Novel agents targeting inhibitor of apoptosis proteins
PT3710439T (pt) 2017-11-15 2023-05-15 Array Biopharma Inc Inibidores de kras g12c
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
US10696638B2 (en) 2017-12-26 2020-06-30 Industrial Technology Research Institute Compounds for inhibiting AGC kinase and pharmaceutical compositions comprising the same
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
CA3107168A1 (en) 2018-08-01 2020-02-06 Araxes Pharma Llc Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
CA3111980A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
JP2022500385A (ja) 2018-09-10 2022-01-04 ミラティ セラピューティクス， インコーポレイテッド 組み合わせ療法
EP3849537B1 (en) 2018-09-10 2024-10-23 Mirati Therapeutics, Inc. Combination therapies
IL281344B2 (en) 2018-09-10 2025-09-01 Mirati Therapeutics Inc Combination of adagrasib and cetuximab for cancer treatment
EP3854786B1 (en) * 2018-09-21 2026-02-18 UBE Corporation Method for producing amino acid derivatives
CN110963991A (zh) * 2018-09-28 2020-04-07 嘉兴学院 一种pi3k抑制剂及其制备方法和应用
CA3112129A1 (en) 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies
CN109721522A (zh) * 2018-12-29 2019-05-07 常州吉恩药业有限公司 一种高品质n-叔丁氧羰基-l-焦谷氨酸苄酯工业化生产方法
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
US20220064141A1 (en) * 2019-01-29 2022-03-03 Brightgene Bio-Medical Technology Co., Ltd. Benzopyridone heterocyclic compound and use thereof
US11098025B2 (en) 2019-01-30 2021-08-24 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
US11547759B2 (en) 2019-01-30 2023-01-10 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
AU2020274011B2 (en) 2019-05-10 2024-02-15 Deciphera Pharmaceuticals, Llc Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
RS65019B1 (sr) 2019-05-10 2024-01-31 Deciphera Pharmaceuticals Llc Fenilaminopirimidin amidni inhibitori autofagije i postupci njihove primene
TW202110482A (zh) * 2019-05-24 2021-03-16 日商糖鎖工學研究所股份有限公司 新穎的人工蛋白質觸媒
CN119241444A (zh) 2019-06-17 2025-01-03 德西费拉制药有限责任公司 氨基嘧啶酰胺自噬抑制剂及其使用方法
CN110256322B (zh) * 2019-06-27 2023-12-15 济南大学 一种合成阿维巴坦关键中间体及其重结晶工艺
AU2020337938B2 (en) 2019-08-29 2025-09-25 Array Biopharma Inc. KRas G12D inhibitors
WO2021055749A1 (en) * 2019-09-19 2021-03-25 Totus Medicines Inc. Therapeutic conjugates
MX2022003537A (es) 2019-09-24 2022-07-11 Mirati Therapeutics Inc Terapias de combinacion.
CA3160619A1 (en) 2019-11-08 2021-05-14 Coave Therapeutics Modified adeno-associated virus vectors and delivery thereof into the central nervous system
US20230064809A1 (en) * 2019-11-28 2023-03-02 Bayer Aktiengesellschaft Substituted aminoquinolones as dgkalpha inhibitors for immune activation
WO2021105117A1 (en) 2019-11-28 2021-06-03 Bayer Aktiengesellschaft Substituted aminoquinolones as dgkalpha inhibitors for immune activation
EP4076418A4 (en) 2019-12-20 2024-01-24 Mirati Therapeutics, Inc. Sos1 inhibitors
US20230158153A1 (en) * 2020-04-09 2023-05-25 Purdue Research Foundation Pi3 kinase inhibitors and uses thereof
CN111665351B (zh) * 2020-06-20 2021-12-03 江南大学 一种快速、特异性测定rna含量的方法
AU2021340716A1 (en) 2020-09-11 2023-03-30 Mirati Therapeutics, Inc. Crystalline forms of a KRas G12C inhibitor
WO2022096681A1 (en) * 2020-11-06 2022-05-12 Coave Therapeutics Lactam-modified adeno-associated virus vectors
CN116802279A (zh) 2020-11-06 2023-09-22 科亚韦治疗公司 内酰胺修饰的腺相关病毒载体
AU2021401232A1 (en) 2020-12-15 2023-06-22 Mirati Therapeutics, Inc. Azaquinazoline pan-kras inhibitors
US11999753B2 (en) 2020-12-16 2024-06-04 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-KRas inhibitors
US11981672B2 (en) 2021-09-13 2024-05-14 Montelino Therapeutics Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
WO2023070114A2 (en) * 2021-10-22 2023-04-27 Terremoto Biosciences, Inc. Reversible lysine covalent modifiers of egfr and uses thereof
CN114105848B (zh) * 2021-11-24 2024-01-12 四川同晟生物医药有限公司 一种顺式-d-羟脯氨酸衍生物的制备方法
CN118632843A (zh) * 2022-03-03 2024-09-10 四川汇宇制药股份有限公司 一种吡啶类衍生物及其用途
WO2024081302A1 (en) * 2022-10-14 2024-04-18 Purdue Research Foundation Ligand-directed covalent modification of amino acid side chains using cyclic imine mannich electrophiles
WO2024109233A1 (zh) * 2022-11-22 2024-05-30 四川汇宇制药股份有限公司 一种嘧啶并芳环化合物及其制备方法和用途

Family Cites Families (98)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3710795A (en) 1970-09-29 1973-01-16 Alza Corp Drug-delivery device with stretched, rate-controlling membrane
US4650750A (en) 1982-02-01 1987-03-17 Giese Roger W Method of chemical analysis employing molecular release tag compounds
US5516931A (en) 1982-02-01 1996-05-14 Northeastern University Release tag compounds producing ketone signal groups
US4709016A (en) 1982-02-01 1987-11-24 Northeastern University Molecular analytical release tags and their use in chemical analysis
US5650270A (en) 1982-02-01 1997-07-22 Northeastern University Molecular analytical release tags and their use in chemical analysis
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
US5756466A (en) 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5856116A (en) 1994-06-17 1999-01-05 Vertex Pharmaceuticals, Incorporated Crystal structure and mutants of interleukin-1 beta converting enzyme
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
HU228446B1 (en) 1996-04-12 2013-03-28 Warner Lambert Co Kinazoline derivatives as irreversible inhibitors of protein-kinase, pharmaceutical compositions containing these compounds and use thereof
US6686350B1 (en) 1996-07-25 2004-02-03 Biogen, Inc. Cell adhesion inhibitors
ES2285735T3 (es) 1996-07-25 2007-11-16 Biogen Idec Inc Modelo molecular para inhibidores de vla-4.
ATE290545T1 (de) 1996-12-06 2005-03-15 Vertex Pharma Inhibitoren des interleukin-1beta konvertierenden enzyms
US6002008A (en) 1997-04-03 1999-12-14 American Cyanamid Company Substituted 3-cyano quinolines
ZA986732B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
US6251912B1 (en) 1997-08-01 2001-06-26 American Cyanamid Company Substituted quinazoline derivatives
US6162613A (en) 1998-02-18 2000-12-19 Vertex Pharmaceuticals, Inc. Methods for designing inhibitors of serine/threonine-kinases and tyrosine kinases
US7383135B1 (en) 1998-05-04 2008-06-03 Vertex Pharmaceuticals Incorporated Methods of designing inhibitors for JNK kinases
US6919178B2 (en) 2000-11-21 2005-07-19 Sunesis Pharmaceuticals, Inc. Extended tethering approach for rapid identification of ligands
US6335155B1 (en) 1998-06-26 2002-01-01 Sunesis Pharmaceuticals, Inc. Methods for rapidly identifying small organic molecule ligands for binding to biological target molecules
EP1115847A1 (en) 1998-09-25 2001-07-18 Children's Medical Center Corporation Short peptides which selectively modulate the activity of protein kinases
US6288082B1 (en) 1998-09-29 2001-09-11 American Cyanamid Company Substituted 3-cyanoquinolines
EP1131304B1 (en) 1998-11-19 2002-12-04 Warner-Lambert Company N- 4-(3-chloro-4-fluoro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide, an irreversible inhibitor of tyrosine kinases
US6569876B1 (en) 1999-06-17 2003-05-27 John C. Cheronis Method and structure for inhibiting activity of serine elastases
US6420364B1 (en) 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
AU2001236720A1 (en) 2000-02-05 2001-08-14 Bemis, Guy Compositions useful as inhibitors of erk
US6384051B1 (en) 2000-03-13 2002-05-07 American Cyanamid Company Method of treating or inhibiting colonic polyps
CA2417500C (en) 2000-07-28 2008-11-18 Georgetown University Medical Center Erbb-2 selective small molecule kinase inhibitors
HUP0400639A3 (en) 2000-12-21 2010-03-29 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them
US7235576B1 (en) 2001-01-12 2007-06-26 Bayer Pharmaceuticals Corporation Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
IL144583A0 (en) 2001-07-26 2002-05-23 Peptor Ltd Chimeric protein kinase inhibitors
IL161409A0 (en) 2001-11-21 2004-09-27 Sunesis Pharmaceuticals Inc Methods for ligand discovery
CA2472580A1 (en) 2002-01-07 2003-07-17 Sequoia Pharmaceuticals Broad spectrum inhibitors
US7202033B2 (en) 2002-03-21 2007-04-10 Sunesis Pharmaceuticals, Inc. Identification of kinase inhibitors
GB0213186D0 (en) * 2002-06-08 2002-07-17 Univ Dundee Methods
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
EP1375517A1 (en) * 2002-06-21 2004-01-02 Smithkline Beecham Corporation Structure of a glucocorticoid receptor ligand binding domain comprising an expanded binding pocket and methods employing same
GB0221169D0 (en) * 2002-09-12 2002-10-23 Univ Bath Crystal
EA200500721A1 (ru) * 2002-11-28 2005-12-29 Шеринг Акциенгезельшафт Пиримидины, ингибирующие chk, pdk и акт, их получение и применение в качестве лекарственных средств
PE20040945A1 (es) 2003-02-05 2004-12-14 Warner Lambert Co Preparacion de quinazolinas substituidas
CA2515688A1 (en) 2003-02-11 2004-08-26 Immusol Incorporated Sirna libraries optimized for predetermined protein families
JP4927533B2 (ja) 2003-02-28 2012-05-09 ニッポネックス インコーポレイテッド 癌その他の疾患の治療に有用な置換ピリジン誘導体
ATE489379T1 (de) 2003-02-28 2010-12-15 Bayer Healthcare Llc 2-oxo-1,3,5-perhydrotriazapinderivate, die sich zur behandlung von hyperproliferativen, angiogenen und entzündlichen erkrankungen eignen
UY28213A1 (es) 2003-02-28 2004-09-30 Bayer Pharmaceuticals Corp Nuevos derivados de cianopiridina útiles en el tratamiento de cáncer y otros trastornos.
EP1610808A4 (en) 2003-03-26 2011-04-06 Sudhir Paul COVALENT BINDING OF LIGANDS TO NUCLEOPHILIC PROTEINS UNDER GUIDANCE BY NONCOVALENT BINDING
WO2007038613A2 (en) 2005-09-26 2007-04-05 The Regents Of The University Of California Selective serine/threonine kinase inhibitors
US7687506B2 (en) 2003-04-11 2010-03-30 The Regents Of The University Of California Selective serine/threonine kinase inhibitors
WO2004113274A2 (en) 2003-05-20 2004-12-29 Bayer Pharmaceuticals Corporation Diaryl ureas with kinase inhibiting activity
EP1648516A2 (en) 2003-08-01 2006-04-26 Wyeth Holdings Corporation Use of combination of an epidermal growth factor receptor kinase inhibitor and cytotoxic agents for treatment and inhibition of cancer
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
WO2005034840A2 (en) 2003-09-17 2005-04-21 Sunesis Pharmaceuticals, Inc. Identification of kinase inhibitors
WO2005043118A2 (en) 2003-10-27 2005-05-12 Vertex Pharmaceuticals Incorporated Drug discovery method
US7932382B2 (en) * 2004-01-16 2011-04-26 The Regents Of The University Of Michigan Conformationally constrained Smac mimetics and the uses thereof
AU2005211448A1 (en) 2004-01-30 2005-08-18 Merck Patent Gmbh Bisarylurea derivatives
WO2005115145A2 (en) 2004-05-20 2005-12-08 Wyeth Quinone substituted quinazoline and quinoline kinase inhibitors
US20080268460A1 (en) 2004-05-20 2008-10-30 Wyeth Assays to Identify Irreversibly Binding Inhibitors of Receptor Tyrosine Kinases
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
US20060079494A1 (en) 2004-09-27 2006-04-13 Santi Daniel V Specific kinase inhibitors
JP5089392B2 (ja) 2004-10-13 2012-12-05 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング キナーゼ阻害剤としての複素環式置換ビスアリール尿素誘導体
ZA200706804B (en) 2005-02-03 2008-10-29 Gen Hospital Corp Method for treating gefitinib resistant cancer
KR20080002826A (ko) 2005-04-14 2008-01-04 와이어쓰 게피티니브 내성 환자에서의 표피 성장 인자 수용체（ｅｇｆｒ） 키나제 억제제의 용도
AR053602A1 (es) 2005-05-03 2007-05-09 Smithkline Beecham Corp Compuesto de 2- arilamino -4-oxo-1,3-tiazol-5(4h)- substituido, composicion farmaceutica que lo comprende, proceso para prepararla y uso del compuesto para preparar un medicamento
GB0509224D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Inhibitors of intracellular enzymatic activity
CA2607020C (en) 2005-05-05 2015-01-13 Chroma Therapeutics Ltd. Alpha amino acid ester-drug conjugates hydrolysable by carboxylesterases
WO2006125539A2 (en) 2005-05-27 2006-11-30 Bayer Healthcare Ag Combination therapy comprising diaryl ureas for treating diseases
NZ567851A (en) 2005-11-01 2011-09-30 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
TW200734327A (en) 2005-11-03 2007-09-16 Vertex Pharma Aminopyrimidines useful as kinase inhibitors
WO2007062459A1 (en) 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
JP2009520038A (ja) 2005-12-19 2009-05-21 ジェネンテック・インコーポレーテッド ピリミジンキナーゼインヒビター
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
CA2647271A1 (en) 2006-04-07 2007-10-18 Modpro Ab Binder for c-reactive protein
CN101054380B (zh) 2006-04-13 2011-07-20 沈阳药科大学 用作细胞周期依赖性蛋白激酶抑制剂的吡唑并嘧啶类衍生物
US7601852B2 (en) 2006-05-11 2009-10-13 Kosan Biosciences Incorporated Macrocyclic kinase inhibitors
US8604031B2 (en) 2006-05-18 2013-12-10 Mannkind Corporation Intracellular kinase inhibitors
EA018573B1 (ru) 2006-09-22 2013-09-30 Фармасайкликс, Инк. Ингибиторы тирозинкиназы брутона
US8193197B2 (en) 2006-10-19 2012-06-05 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
ME00811B (me) 2006-12-08 2012-03-20 Novartis Ag JEDINJENJA l KOMPOZICIJE KAO INHIBITORI PROTEIN KINAZE
EP2099771A1 (en) 2006-12-19 2009-09-16 Genentech, Inc. Pyrimidine kinase inhibitors
PT2114900T (pt) 2007-01-31 2019-01-17 Ym Biosciences Australia Pty Compostos à base de tiopirimidina e as suas utilizações
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
EP2152079A4 (en) 2007-06-04 2011-03-09 Avila Therapeutics Inc HETEROCYCLIC COMPOUNDS AND USES THEREOF
WO2009030890A1 (en) 2007-09-03 2009-03-12 University Court Of The University Of Dundee Pyrimidine compounds for the treatment of cancer, septic shock and/or primary open angle glaucoma
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
EP2214486A4 (en) 2007-10-19 2011-03-09 Avila Therapeutics Inc HETEROARYL COMPOUNDS AND ITS USES
US8293705B2 (en) 2007-12-21 2012-10-23 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
US8309685B2 (en) 2007-12-21 2012-11-13 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
TWI487522B (zh) 2007-12-21 2015-06-11 賽基艾維洛米斯研究股份有限公司 Ｈｃｖ蛋白酶抑制劑及其用途（一）
TW200932255A (en) * 2007-12-21 2009-08-01 Avila Therapeutics Inc HCV protease inhibitors and uses thereof
EP2244721A4 (en) 2008-01-14 2017-01-18 Bayer Intellectual Property GmbH Sulfone substituted 2,3-dihydroimidazo ý1,2-c¨quinazoline derivatives useful for treating hyper-proliferative disorders and diseases with angiogenesis
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
SG10201510696RA (en) 2008-06-27 2016-01-28 Celgene Avilomics Res Inc Heteroaryl compounds and uses thereof
US8188137B2 (en) 2008-08-15 2012-05-29 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
MY156789A (en) 2008-09-05 2016-03-31 Celgene Avilomics Res Inc Algorithm for designing irreversible inhibitors
US8603737B2 (en) 2008-09-19 2013-12-10 Celgene Avilomics Research, Inc. Methods for identifying HCV protease inhibitors
WO2011031896A2 (en) 2009-09-09 2011-03-17 Avila Therapeutics, Inc. Pi3 kinase inhibitors and uses thereof
IN2012DN02534A (es) 2009-09-16 2015-08-28 Avila Therapeutics Inc
US20110269244A1 (en) 2009-12-30 2011-11-03 Petter Russell C Ligand-directed covalent modification of protein
MY160734A (en) 2010-08-10 2017-03-15 Celgene Avilomics Res Inc Besylate salt of a btk inhibitor

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JP2016195596A (ja) 2016-11-24
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AU2010339456A1 (en) 2012-07-05
WO2011082285A1 (en) 2011-07-07
KR20130067487A (ko) 2013-06-25
TW201134825A (en) 2011-10-16
SG181965A1 (en) 2012-08-30
CA2785738A1 (en) 2011-07-07
EP2519664A4 (en) 2014-03-12
US11542492B2 (en) 2023-01-03
JP2013516422A (ja) 2013-05-13
US20110269244A1 (en) 2011-11-03
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CN102812167A (zh) 2012-12-05
EP2519664A1 (en) 2012-11-07

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