BR112012015721A2 - modificação covalente de proteínas dirigida por ligante - Google Patents

modificação covalente de proteínas dirigida por ligante

Info

Publication number
BR112012015721A2
BR112012015721A2 BR112012015721A BR112012015721A BR112012015721A2 BR 112012015721 A2 BR112012015721 A2 BR 112012015721A2 BR 112012015721 A BR112012015721 A BR 112012015721A BR 112012015721 A BR112012015721 A BR 112012015721A BR 112012015721 A2 BR112012015721 A2 BR 112012015721A2
Authority
BR
Brazil
Prior art keywords
protein modification
covalent ligand
driven protein
driven
covalent
Prior art date
Application number
BR112012015721A
Other languages
English (en)
Inventor
Medikonda Aravind
F Jewell Charles
Niu Deqiang
Singh Juswinder
Lee Kwangho
Qiao Lixin
C Petter Russell
Zhu Zhendong
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 BR112012015721A2 publication Critical patent/BR112012015721A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—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
    • 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—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
    • 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
    • C07D239/48—Two nitrogen atoms
    • C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/503—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from viruses
    • C12N9/506—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from viruses derived from RNA viruses
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/93—Ligases (6)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/25—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving enzymes not classifiable in groups C12Q1/26 - C12Q1/66
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
    • 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21—Serine endopeptidases (3.4.21)
    • C12Y304/21098—Hepacivirin (3.4.21.98)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y603/00—Ligases forming carbon-nitrogen bonds (6.3)
    • C12Y603/02—Acid—amino-acid ligases (peptide synthases)(6.3.2)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16B—BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B15/00—ICT specially adapted for analysing two-dimensional or three-dimensional molecular structures, e.g. structural or functional relations or structure alignment
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16B—BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B15/00—ICT specially adapted for analysing two-dimensional or three-dimensional molecular structures, e.g. structural or functional relations or structure alignment
    • G16B15/30—Drug targeting using structural data; Docking or binding prediction
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16C—COMPUTATIONAL CHEMISTRY; CHEMOINFORMATICS; COMPUTATIONAL MATERIALS SCIENCE
    • G16C20/00—Chemoinformatics, i.e. ICT specially adapted for the handling of physicochemical or structural data of chemical particles, elements, compounds or mixtures
    • G16C20/50—Molecular design, e.g. of drugs

Abstract

modificação covalente de proteínas dirigida por ligante a presente invenção se refere a inibidores de enzima. mais especificamente, a presente invenção se refere a modificação covalente de proteínas dirigida por ligante; a método de desenho do mesmo; formulação farmacêutica contendo o mesmo e a métodos de uso.
BR112012015721A 2009-12-30 2010-12-30 modificação covalente de proteínas dirigida por ligante BR112012015721A2 (pt)

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
BR112012015721A2 true BR112012015721A2 (pt) 2017-09-26

Family

ID=44226810

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012015721A BR112012015721A2 (pt) 2009-12-30 2010-12-30 modificação covalente de proteínas dirigida por ligante

Country Status (13)

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

Families Citing this family (88)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101820848B (zh) 2007-10-11 2015-06-10 加利福尼亚大学董事会 抑制n-酰基乙醇胺水解性酸酰胺酶的组合物和方法
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
AU2009248923B2 (en) 2008-05-21 2015-01-29 Takeda Pharmaceutical Company Limited Phosphorous derivatives as kinase inhibitors
CN105574346A (zh) * 2008-09-05 2016-05-11 新基阿维罗米克斯研究公司 多肽偶联物与不可逆抑制剂的设计方法和检测方法
IN2012DN02534A (pt) 2009-09-16 2015-08-28 Avila Therapeutics Inc
MX2012007684A (es) 2009-12-30 2012-10-05 Avila Therapeutics Inc Modificacion covalente ligando dirigida de proteina.
KR101884010B1 (ko) 2011-05-04 2018-07-31 어리어드 파마슈티칼스, 인코포레이티드 Egfr-유도된 암의 세포 증식을 억제하는 화합물
WO2012170867A1 (en) 2011-06-09 2012-12-13 Rhizen Pharmaceuticals Sa Novel compounds as modulators of gpr-119
HUE036017T2 (hu) 2011-09-29 2018-06-28 Ono Pharmaceutical Co Fenil származék
JP6266528B2 (ja) 2011-11-22 2018-01-24 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア Ｎ−アシルエタノールアミン酸アミダーゼ（ｎａａａ）の阻害剤としての二置換ベータ−ラクトン
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
CA3113959A1 (en) * 2012-09-26 2014-04-03 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
WO2014143659A1 (en) 2013-03-15 2014-09-18 Araxes Pharma Llc Irreversible covalent inhibitors of the gtpase k-ras g12c
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de 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
BR112015024897A2 (pt) 2013-03-26 2017-07-18 Ono Pharmaceutical Co derivado de fenila
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
MX2016004360A (es) * 2013-10-10 2016-08-19 Araxes Pharma Llc Inhibidores de kras g12c.
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
CN117886738A (zh) * 2013-12-27 2024-04-16 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
US10300074B2 (en) * 2014-06-04 2019-05-28 Sanford Burnham Prebys Medical Discovery 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
WO2016049524A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
KR20180005178A (ko) 2015-04-10 2018-01-15 아락세스 파마 엘엘씨 치환된 퀴나졸린 화합물 및 이의 사용방법
WO2016168540A1 (en) * 2015-04-15 2016-10-20 Araxes Pharma Llc Fused-tricyclic inhibitors of kras and methods of use thereof
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058915A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356339A1 (en) 2015-09-28 2018-08-08 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
EP3356354A1 (en) 2015-09-28 2018-08-08 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
EP3364977A4 (en) 2015-10-19 2019-09-04 Araxes Pharma LLC PROCESS FOR SCREENING INHIBITORS OF RAS
EP3377481A1 (en) 2015-11-16 2018-09-26 Araxes Pharma LLC 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US10590084B2 (en) 2016-03-09 2020-03-17 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
JP7039489B2 (ja) 2016-05-18 2022-03-22 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤
US11292801B2 (en) 2016-07-05 2022-04-05 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
SG10201912574WA (en) 2016-09-28 2020-02-27 Blade Therapeutics Inc Calpain modulators and therapeutic uses thereof
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
CN110312711A (zh) 2016-10-07 2019-10-08 亚瑞克西斯制药公司 作为ras抑制剂的杂环化合物及其使用方法
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
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法
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
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
WO2018140512A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
SG10202113146UA (en) 2017-05-25 2021-12-30 Araxes Pharma Llc Covalent inhibitors of kras
CN110831933A (zh) 2017-05-25 2020-02-21 亚瑞克西斯制药公司 喹唑啉衍生物作为突变kras、hras或nras的调节剂
JP2020521741A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
KR20200081417A (ko) 2017-11-01 2020-07-07 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 아폽토시스 억제제 단백질을 표적화하는 신규 작용제
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
KR20200100632A (ko) 2017-11-15 2020-08-26 미라티 테라퓨틱스, 인크. Ｋｒａｓ ｇ12ｃ 억제제
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
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
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
JP2022518591A (ja) * 2019-01-29 2022-03-15 博瑞生物医薬（蘇州）股▲分▼有限公司 複素環式化合物であるベンゾピリドンおよびその使用
US11547759B2 (en) 2019-01-30 2023-01-10 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
JP2022523916A (ja) 2019-01-30 2022-04-27 モンテリノ・セラピューティクス・インコーポレイテッド アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法
PL3966207T3 (pl) 2019-05-10 2024-03-04 Deciphera Pharmaceuticals, Llc Fenyloaminopirymidynoamidowe inhibitory autofagii i sposoby ich zastosowania
SG11202112171XA (en) 2019-05-10 2021-12-30 Deciphera Pharmaceuticals Llc Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
US20220241765A1 (en) * 2019-05-24 2022-08-04 Glytech, Inc. Novel artificial protein catalyst
JP2022536540A (ja) 2019-06-17 2022-08-17 デシフェラ・ファーマシューティカルズ，エルエルシー アミノピリミジンアミドオートファジー阻害剤およびその使用方法
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
MX2022002465A (es) 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
WO2021055749A1 (en) * 2019-09-19 2021-03-25 Totus Medicines Inc. Therapeutic conjugates
CA3152025A1 (en) 2019-09-24 2021-04-01 David BRIERE Combination therapies
AU2020378643A1 (en) 2019-11-08 2022-06-02 Coave Therapeutics Modified adeno-associated virus vectors and delivery thereof into the central nervous system
CN115210238A (zh) * 2019-11-28 2022-10-18 拜耳公司 作为用于免疫激活的DGKα抑制剂的取代的氨基喹诺酮类
IL294048A (en) 2019-12-20 2022-08-01 Mirati Therapeutics Inc sos1 inhibitors
EP4132921A4 (en) * 2020-04-09 2024-03-27 Purdue Research Foundation PI3 KINASE INHIBITORS AND THEIR USES
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
KR20230107584A (ko) * 2020-11-06 2023-07-17 코브 테라퓨틱스 락탐-변형된 아데노-관련 바이러스 벡터
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
WO2023165581A1 (zh) * 2022-03-03 2023-09-07 四川汇宇制药股份有限公司 一种吡啶类衍生物及其用途

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
US5516931A (en) 1982-02-01 1996-05-14 Northeastern University Release tag compounds producing ketone signal groups
US5650270A (en) 1982-02-01 1997-07-22 Northeastern University Molecular analytical release tags and their use in chemical analysis
US4709016A (en) 1982-02-01 1987-11-24 Northeastern University Molecular analytical release tags and their use in chemical analysis
US4650750A (en) 1982-02-01 1987-03-17 Giese Roger W Method of chemical analysis employing molecular release tag compounds
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
US5856116A (en) 1994-06-17 1999-01-05 Vertex Pharmaceuticals, Incorporated Crystal structure and mutants of interleukin-1 beta converting enzyme
US5756466A (en) 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
BR9708640B1 (pt) 1996-04-12 2013-06-11 inibidores irreversÍveis de tirosina-cinases e composiÇço farmacÊutica compreendendo os mesmo.
EP0914605B1 (en) 1996-07-25 2007-05-30 Biogen Idec MA Inc. Molecular model for vla-4 inhibitors
US6686350B1 (en) 1996-07-25 2004-02-03 Biogen, Inc. Cell adhesion inhibitors
CA2274249A1 (en) 1996-12-06 1998-06-11 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1.beta. converting enzyme
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
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
US6919178B2 (en) 2000-11-21 2005-07-19 Sunesis Pharmaceuticals, Inc. Extended tethering approach for rapid identification of ligands
AU6059099A (en) 1998-09-25 2000-04-17 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
BR9915487A (pt) 1998-11-19 2001-07-31 Warner Lambert Co N-[4-(3-cloro-4-flúor-fenilamino) - 7 - (3-morfolin-4-il-propóxi)-quinazolin-6-il]-acrilamida, um inibidor irreversìvel de tirosina quinases
CA2375229A1 (en) 1999-06-17 2000-12-28 Source Precision Medicine, Inc. Method and compounds 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
EP1207864A2 (en) 2000-02-05 2002-05-29 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of erk
US6384051B1 (en) 2000-03-13 2002-05-07 American Cyanamid Company Method of treating or inhibiting colonic polyps
US7427689B2 (en) 2000-07-28 2008-09-23 Georgetown University ErbB-2 selective small molecule kinase inhibitors
EP1345922B1 (en) 2000-12-21 2006-05-31 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
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
RU2295518C2 (ru) 2001-11-21 2007-03-20 Сьюнесис Фармасьютикалс, Инк. Способ нахождения лигандов
AU2003202914A1 (en) 2002-01-07 2003-07-24 Sequoia Pharmaceuticals Broad spectrum inhibitors
WO2003081210A2 (en) 2002-03-21 2003-10-02 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
BR0316680A (pt) * 2002-11-28 2005-10-18 Schering Ag Pirimidinas inibidoras de chk, pdk e akt, sua produção e uso como agentes farmacêuticos
PE20040945A1 (es) 2003-02-05 2004-12-14 Warner Lambert Co Preparacion de quinazolinas substituidas
WO2004072261A2 (en) 2003-02-11 2004-08-26 Immusol Incorporated Sirna libraries optimized for predetermined protein families
US7557129B2 (en) 2003-02-28 2009-07-07 Bayer Healthcare Llc Cyanopyridine derivatives useful in the treatment of cancer and other disorders
JP4594925B2 (ja) 2003-02-28 2010-12-08 ニッポネックス インコーポレイテッド 増殖亢進性、血管新生性及び炎症性疾患の治療に有用な２−オキソ−１，３，５−パーヒドロトリアザピン誘導体
CA2516627A1 (en) 2003-02-28 2004-09-16 Bayer Pharmaceuticals Corporation Substituted pyridine derivatives useful in the treatment of cancer and other disorders
WO2004087059A2 (en) 2003-03-26 2004-10-14 The University Of Texas Covalent attachment of ligands to nucleophilic proteins guided by non-covalent binding
WO2005000197A2 (en) 2003-04-11 2005-01-06 The Regents Of The University Of California Selective serine/threonine kinase inhibitors
US8748601B2 (en) 2003-04-11 2014-06-10 The Regents Of The University Of California Selective serine/threonine kinase inhibitors
PL1626714T3 (pl) 2003-05-20 2007-12-31 Bayer Healthcare Llc Diarylowe pochodne mocznika do schorzeń, w których pośredniczy PDGFR
KR20060054412A (ko) 2003-08-01 2006-05-22 와이어쓰 홀딩스 코포레이션 암 치료 및 억제용 표피 성장인자 수용체 키나제 억제제와세포독성제의 배합물 용도
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
EP1670422A4 (en) 2003-09-17 2007-08-01 Sunesis Pharmaceuticals Inc IDENTIFICATION OF KINASE INHIBITORS
US8187874B2 (en) 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
CN1960728A (zh) * 2004-01-16 2007-05-09 密歇根大学董事会 构象受限的smac模拟物及其应用
CN1972925A (zh) 2004-01-30 2007-05-30 默克专利有限公司 双芳基脲类衍生物
US20080268460A1 (en) 2004-05-20 2008-10-30 Wyeth Assays to Identify Irreversibly Binding Inhibitors of Receptor Tyrosine Kinases
WO2005115145A2 (en) 2004-05-20 2005-12-08 Wyeth Quinone substituted quinazoline and quinoline kinase inhibitors
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
WO2006036941A2 (en) 2004-09-27 2006-04-06 Kosan Biosciences Incorporated Specific kinase inhibitors
MX2007004248A (es) 2004-10-13 2007-06-12 Merck Patent Gmbh Derivados heterociclicos de bisarilurea sustituidos como inhibidores de cinasa.
CN113952338A (zh) 2005-02-03 2022-01-21 综合医院公司 治疗吉非替尼耐药性癌症的方法
KR20080002826A (ko) 2005-04-14 2008-01-04 와이어쓰 게피티니브 내성 환자에서의 표피 성장 인자 수용체（ｅｇｆｒ） 키나제 억제제의 용도
TW200716132A (en) 2005-05-03 2007-05-01 Smithkline Beecham Corp Novel chemical compounds
GB0509224D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Inhibitors of intracellular enzymatic activity
EP3530290A1 (en) 2005-05-05 2019-08-28 GlaxoSmithKline Intellectual Property Development Limited Alpha aminoacid ester-drug conjugates hydrolysable by carboxylesterase
EP1888065A2 (en) 2005-05-27 2008-02-20 Bayer HealthCare AG Combination therapy comprising diaryl ureas for treating diseases
EP1951684B1 (en) 2005-11-01 2016-07-13 TargeGen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
CN103145702A (zh) 2005-11-03 2013-06-12 顶点医药品公司 用作激酶抑制剂的氨基嘧啶
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
AU2007254179B2 (en) 2006-05-18 2013-03-21 Pharmacyclics Llc Intracellular kinase inhibitors
NZ601278A (en) 2006-09-22 2013-09-27 Pharmacyclics Inc Inhibitors of Bruton's tyrosine kinase
WO2008049123A2 (en) 2006-10-19 2008-04-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine derivatives as inhibitors of jak kinases for the treatment of autoimmune diseases
EP2091918B1 (en) 2006-12-08 2014-08-27 Irm Llc Compounds and compositions as protein kinase inhibitors
CA2670645A1 (en) 2006-12-19 2008-07-03 Genentech, Inc. Pyrimidine kinase inhibitors
WO2008092199A1 (en) 2007-01-31 2008-08-07 Cytopia Research Pty Ltd Thiopyrimidine-based compounds and uses thereof
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
US7982036B2 (en) 2007-10-19 2011-07-19 Avila Therapeutics, Inc. 4,6-disubstitued pyrimidines useful as kinase inhibitors
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
TW201518507A (zh) * 2007-12-21 2015-05-16 Celgene Avilomics Res Inc Ｈｃｖ蛋白酶抑制劑及其用途（二）
US8309685B2 (en) 2007-12-21 2012-11-13 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
US8778877B2 (en) 2007-12-21 2014-07-15 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
US8293705B2 (en) 2007-12-21 2012-10-23 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
KR20110025224A (ko) 2008-06-27 2011-03-09 아빌라 테라퓨틱스, 인크. 헤테로아릴 화합물 및 이의 용도
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8188137B2 (en) 2008-08-15 2012-05-29 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
CN105574346A (zh) 2008-09-05 2016-05-11 新基阿维罗米克斯研究公司 多肽偶联物与不可逆抑制剂的设计方法和检测方法
US8603737B2 (en) 2008-09-19 2013-12-10 Celgene Avilomics Research, Inc. Methods for identifying HCV protease inhibitors
SG179085A1 (en) 2009-09-09 2012-04-27 Avila Therapeutics Inc Pi3 kinase inhibitors and uses thereof
IN2012DN02534A (pt) 2009-09-16 2015-08-28 Avila Therapeutics Inc
MX2012007684A (es) 2009-12-30 2012-10-05 Avila Therapeutics Inc Modificacion covalente ligando dirigida de proteina.
WO2012021444A1 (en) 2010-08-10 2012-02-16 Avila Therapeutics, Inc. Besylate salt of a btk inhibitor

Also Published As

Publication number Publication date
AU2010339456A1 (en) 2012-07-05
CN102812167A (zh) 2012-12-05
EP2519664A1 (en) 2012-11-07
US20110269244A1 (en) 2011-11-03
RU2012132473A (ru) 2014-02-10
KR20130067487A (ko) 2013-06-25
JP2016195596A (ja) 2016-11-24
MX2012007684A (es) 2012-10-05
WO2011082285A1 (en) 2011-07-07
EP2519664A4 (en) 2014-03-12
AU2016244281A1 (en) 2016-11-03
CA2785738A1 (en) 2011-07-07
US11542492B2 (en) 2023-01-03
US20170218353A1 (en) 2017-08-03
JP2013516422A (ja) 2013-05-13
SG181965A1 (en) 2012-08-30
TW201134825A (en) 2011-10-16

Similar Documents

Publication Publication Date Title
BR112012015721A2 (pt) modificação covalente de proteínas dirigida por ligante
CY1123208T1 (el) Κυκλικα παραγωγα εστερων βορονικου οξεος, μεθοδος για την παρασκευη και θεραπευτικες χρησεις αυτων
CY1118454T1 (el) Πρωτοτυποι αναστολεις πυρρολιου της αναγωγασης s-νιτροζογλουταθειονης ως θεραπευτικοι παραγοντες
UY34342A (es) ?derivados de pirrolopirimidina y purina?.
MX2019002979A (es) Formulaciones de anticuerpos.
WO2012062810A3 (en) Cell culture medium and process for protein expression, said medium and process comprising a pam inhibitor
UY34350A (es) Derivados de pirazolquinolinona, su preparación y su uso terapéutico.
ECSP10010295A (es) Formulacion de anticuerpo
CL2013003145A1 (es) Formulación farmacéutica que comprende mezcla de anticuerpo anti-alfa4beta7, un antioxidante o quelante y al menos un aminoácido libre.
EA201391285A1 (ru) Производные тетрагидрохинолина, полезные в качестве ингибиторов бромодомена
EA201290980A1 (ru) Производные 1-амино-2-циклопропилэтилбороновой кислоты
CL2011002194A1 (es) Formulacion que comprende anticuerpo en un regulador de histidina-arginina ph 4.5 a 6.5; articulo de manufactura que comprende dicha formulacion; metodo para estabilizar un anticuerpo en una formulacion farmaceutica acuosa.
BR112013030472A2 (pt) formulação farmacêutica, artigo de fabricação e método
CO6440530A2 (es) Formulaciones de caldo de fermentación
BR112014010631A2 (pt) inibidores de pak para o tratamento da síndrome do x frágil
CL2012003075A1 (es) Composicion farmaceutica en solucion de pazopanib, estable y para uso oftalmico; metodo para la preparacion de dicha solucion.
EA200970247A1 (ru) Способ получения оптического активного n-защищенного 3-аминопирролидина или оптически активного n-защищенного 3-аминопиперидина и соответствующих кетонов путем оптического разделения рацемических смесей аминов с использованием бактериальной омега-трансаминазы
SMT201400114B (it) Derivati di 2-arilimidazolo come inibitori dell'enzima pde10a
EA201490450A1 (ru) Новые ингибиторы ферментов
MX347795B (es) Formulaciones liquidas de st-246 y metodos.
CL2012003523A1 (es) Método para la preparación de una composición farmacéutica que contiene un portador de oxígeno termoestable; composicion farmaceutica que contiene un portador de oxigeno altamente purificado y termoestable.
CR20140128A (es) Inhibidores de la enzima activadora de nedd 8
BR112014014319A2 (pt) composições de cuidado oral
EA201200616A1 (ru) Производные 2-оксо-1-пирролидинилимидазотиадиазола
GB2496356A (en) Pharmaceutical composition and method of inhibiting of production or amplifying elimination of P24 protein

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]
B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]
B25B Requested transfer of rights rejected

Owner name: AVILA THERAPEUTICS, INC. (US)

B350 Update of information on the portal [chapter 15.35 patent gazette]