CO2018007052A2 - Compuestos y metodos para modulación de la quinasa, e indicaciones de los mismos - Google Patents

Compuestos y metodos para modulación de la quinasa, e indicaciones de los mismos

Info

Publication number
CO2018007052A2
CO2018007052A2 CONC2018/0007052A CO2018007052A CO2018007052A2 CO 2018007052 A2 CO2018007052 A2 CO 2018007052A2 CO 2018007052 A CO2018007052 A CO 2018007052A CO 2018007052 A2 CO2018007052 A2 CO 2018007052A2
Authority
CO
Colombia
Prior art keywords
compounds
indications
methods
kinase modulation
kinase
Prior art date
Application number
CONC2018/0007052A
Other languages
English (en)
Inventor
Wayne Spevak
Katrina Chan
Guoxian Wu
Jeffrey Wu
Ken Dong
Todd Ewing
Jack Lin
Ying Zhang
Prabha N Ibrahim
Original Assignee
Plexxikon 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 Plexxikon Inc filed Critical Plexxikon Inc
Publication of CO2018007052A2 publication Critical patent/CO2018007052A2/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)

Abstract

Se divulgan compuestos de Fórmula I, o una sal aceptable para uso farmacéutico, un solvato, un tautómero, un isómero o un análogo deuterado de los mismos, donde Z2, Z3, y Z5 son como se describen en la presente, composiciones de los mismos, y usos de los mismos.
CONC2018/0007052A 2015-12-07 2018-07-05 Compuestos y metodos para modulación de la quinasa, e indicaciones de los mismos CO2018007052A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562264180P 2015-12-07 2015-12-07
PCT/US2016/065179 WO2017100201A1 (en) 2015-12-07 2016-12-06 Compounds and methods for kinase modulation, and indications therefor

Publications (1)

Publication Number Publication Date
CO2018007052A2 true CO2018007052A2 (es) 2018-07-19

Family

ID=57796966

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2018/0007052A CO2018007052A2 (es) 2015-12-07 2018-07-05 Compuestos y metodos para modulación de la quinasa, e indicaciones de los mismos

Country Status (16)

Country Link
US (1) US9938273B2 (es)
EP (1) EP3386980B1 (es)
JP (1) JP6862468B2 (es)
KR (1) KR20180086247A (es)
CN (1) CN108368110A (es)
AU (1) AU2016367147B2 (es)
BR (1) BR112018011475A2 (es)
CA (1) CA3007462C (es)
CO (1) CO2018007052A2 (es)
ES (1) ES2899581T3 (es)
IL (1) IL259803A (es)
MX (1) MX2018006856A (es)
PH (1) PH12018501179A1 (es)
RU (1) RU2018123825A (es)
SG (1) SG11201804711RA (es)
WO (1) WO2017100201A1 (es)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009012283A1 (en) 2007-07-17 2009-01-22 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
PT2672967T (pt) 2011-02-07 2018-12-07 Plexxikon Inc Compostos e métodos de modulação da quinase e suas indicações
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
AU2013312477B2 (en) 2012-09-06 2018-05-31 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
PL2935248T3 (pl) 2012-12-21 2018-07-31 Plexxikon Inc Związki i sposoby modulacji kinaz i wskazania dla nich
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
TWI634111B (zh) 2013-03-15 2018-09-01 普雷辛肯公司 雜環化合物及其用途
BR112015028845A2 (pt) 2013-05-30 2017-07-25 Plexxikon Inc compostos para a modulação da quinase e indicações da mesma
HUE050506T2 (hu) 2015-05-06 2020-12-28 Plexxikon Inc Kinázokat moduláló vegyület szilárd formái
CN107531706A (zh) 2015-05-06 2018-01-02 普莱希科公司 调节激酶的1H‑吡咯并[2,3‑b]吡啶衍生物的合成
HUE050936T2 (hu) 2015-05-22 2021-01-28 Plexxikon Inc Heterociklusos vegyületek szintézise
US10829484B2 (en) 2015-07-28 2020-11-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
AU2016328619B2 (en) 2015-09-21 2020-07-16 Opna Bio SA Heterocyclic compounds and uses thereof
WO2017156071A1 (en) 2016-03-09 2017-09-14 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
WO2018009417A1 (en) 2016-07-05 2018-01-11 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
TW201815766A (zh) 2016-09-22 2018-05-01 美商普雷辛肯公司 用於ido及tdo調節之化合物及方法以及其適應症
KR20190063473A (ko) 2016-09-28 2019-06-07 블레이드 테라퓨틱스, 인크. 칼페인 조정자 및 그 치료학적 용도
AU2017395023B2 (en) 2016-12-23 2022-04-07 Plexxikon Inc. Compounds and methods for CDK8 modulation and indications therefor
WO2018134254A1 (en) 2017-01-17 2018-07-26 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
JP2020511467A (ja) 2017-03-20 2020-04-16 プレキシコン インコーポレーテッドPlexxikon Inc. ブロモドメインを阻害する4−(1−(1,1−ジ(ピリジン−2−イル)エチル)−6−(3,5−ジメチルイソオキサゾール−4−イル)−1H−ピロロ[3,2−b]ピリジン−3−イル)安息香酸の結晶形
WO2018226846A1 (en) * 2017-06-07 2018-12-13 Plexxikon Inc. Compounds and methods for kinase modulation
WO2019018562A1 (en) 2017-07-19 2019-01-24 Ideaya Biosciences, Inc. AMIDO COMPOUND AS MODULATORS OF AHR
WO2019023198A1 (en) 2017-07-25 2019-01-31 Plexxikon Inc. FORMULATION OF A COMPOUND MODULATING KINASES
RU2739489C2 (ru) * 2018-03-06 2020-12-24 Закрытое Акционерное Общество "Биокад" Новые гетероциклические соединения как ингибиторы CDK8/19
BR112020002674A2 (pt) * 2017-08-07 2020-07-28 Joint Stock Company Biocad compostos heterocíclicos inovadores como inibidores de cdk8/19
JP2020536917A (ja) 2017-10-13 2020-12-17 プレキシコン インコーポレーテッドPlexxikon Inc. キナーゼを調節するための化合物の固体形態
BR112020007972A2 (pt) 2017-10-27 2020-10-20 Plexxikon, Inc. formulações de composto que modula quinases
WO2019183145A1 (en) 2018-03-20 2019-09-26 Plexxikon Inc. Compounds and methods for ido and tdo modulation, and indications therefor
CN110833548A (zh) * 2018-08-15 2020-02-25 广西梧州制药(集团)股份有限公司 吡唑并嘧啶衍生物在治疗肝肺综合征的用途
CN111434661B (zh) * 2019-01-11 2023-09-12 爱科诺生物医药(香港)有限公司 具有细胞坏死抑制活性的芳香杂环化合物及其应用
KR20220018475A (ko) 2019-04-09 2022-02-15 플렉시콘 인코퍼레이티드 Ep300 또는 cbp 조절 및 이의 표시를 위한 응축 아진
MX2022006059A (es) * 2019-11-25 2022-09-12 Gain Therapeutics Sa Compuestos de arilo y heteroarilo, y usos terapeuticos de los mismos en condiciones asociadas con la alteracion de la actividad de galactocerebrosidasa.
WO2021118924A2 (en) 2019-12-12 2021-06-17 Ting Therapeutics Llc Compositions and methods for the prevention and treatment of hearing loss
US11807626B2 (en) 2020-04-23 2023-11-07 Opna Bio SA Compounds and methods for CD73 modulation and indications therefor
WO2022013225A1 (en) 2020-07-13 2022-01-20 Precirix N.V. Antibody fragment against folr1
AU2021327375A1 (en) 2020-08-21 2023-03-16 Opna Bio SA Combinational drug anticancer therapies
CN114230565B (zh) * 2020-09-09 2023-10-27 成都奥睿药业有限公司 5-取代吲哚3-酰胺衍生物及其制备方法和用途
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
WO2023213801A1 (en) 2022-05-02 2023-11-09 Precirix N.V. Pre-targeting
WO2023240140A1 (en) * 2022-06-08 2023-12-14 Blossomhill Therapeutics, Inc. Indazole macrocycles and their use
WO2023245329A1 (en) * 2022-06-20 2023-12-28 Biofront Ltd Multi-kinase inhibitors, compositions thereof, and methods of using the same

Family Cites Families (125)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US878589A (en) 1907-01-19 1908-02-11 Rail Joint Co Reinforced angle-bar for rail-joints.
GB1573212A (en) 1976-04-15 1980-08-20 Technicon Instr Immunoassay for gentamicin
US4568649A (en) 1983-02-22 1986-02-04 Immunex Corporation Immediate ligand detection assay
US4626513A (en) 1983-11-10 1986-12-02 Massachusetts General Hospital Method and apparatus for ligand detection
ATE56096T1 (de) 1984-03-15 1990-09-15 Immunex Corp Test zur sofortigen feststellung von liganden, testsatz und seine herstellung.
US6054270A (en) 1988-05-03 2000-04-25 Oxford Gene Technology Limited Analying polynucleotide sequences
US5700637A (en) 1988-05-03 1997-12-23 Isis Innovation Limited Apparatus and method for analyzing polynucleotide sequences and method of generating oligonucleotide arrays
US5658775A (en) 1988-05-17 1997-08-19 Sloan-Kettering Institute For Cancer Research Double copy retroviral vector
WO1990002806A1 (en) 1988-09-01 1990-03-22 Whitehead Institute For Biomedical Research Recombinant retroviruses with amphotropic and ecotropic host ranges
US5703055A (en) 1989-03-21 1997-12-30 Wisconsin Alumni Research Foundation Generation of antibodies through lipid mediated DNA delivery
US5527681A (en) 1989-06-07 1996-06-18 Affymax Technologies N.V. Immobilized molecular synthesis of systematically substituted compounds
US5744101A (en) 1989-06-07 1998-04-28 Affymax Technologies N.V. Photolabile nucleoside protecting groups
US5800992A (en) 1989-06-07 1998-09-01 Fodor; Stephen P.A. Method of detecting nucleic acids
US5143854A (en) 1989-06-07 1992-09-01 Affymax Technologies N.V. Large scale photolithographic solid phase synthesis of polypeptides and receptor binding screening thereof
AU7906691A (en) 1990-05-23 1991-12-10 United States of America, as represented by the Secretary, U.S. Department of Commerce, The Adeno-associated virus (aav)-based eucaryotic vectors
JPH06509578A (ja) 1991-07-26 1994-10-27 ユニバーシティ・オブ・ロチェスター 悪性細胞利用による癌治療法
US5632957A (en) 1993-11-01 1997-05-27 Nanogen Molecular biological diagnostic systems including electrodes
JPH05236997A (ja) 1992-02-28 1993-09-17 Hitachi Ltd ポリヌクレオチド捕捉用チップ
US5631236A (en) 1993-08-26 1997-05-20 Baylor College Of Medicine Gene therapy for solid tumors, using a DNA sequence encoding HSV-Tk or VZV-Tk
US5426039A (en) 1993-09-08 1995-06-20 Bio-Rad Laboratories, Inc. Direct molecular cloning of primer extended DNA containing an alkane diol
US6045996A (en) 1993-10-26 2000-04-04 Affymetrix, Inc. Hybridization assays on oligonucleotide arrays
US5965452A (en) 1996-07-09 1999-10-12 Nanogen, Inc. Multiplexed active biologic array
US6468742B2 (en) 1993-11-01 2002-10-22 Nanogen, Inc. Methods for determination of single nucleic acid polymorphisms using bioelectronic microchip
US5807522A (en) 1994-06-17 1998-09-15 The Board Of Trustees Of The Leland Stanford Junior University Methods for fabricating microarrays of biological samples
US5556752A (en) 1994-10-24 1996-09-17 Affymetrix, Inc. Surface-bound, unimolecular, double-stranded DNA
US5830645A (en) 1994-12-09 1998-11-03 The Regents Of The University Of California Comparative fluorescence hybridization to nucleic acid arrays
US5959098A (en) 1996-04-17 1999-09-28 Affymetrix, Inc. Substrate preparation process
US6117681A (en) 1995-03-29 2000-09-12 Bavarian Nordic Research Inst. A/S Pseudotyped retroviral particles
US6110456A (en) 1995-06-07 2000-08-29 Yale University Oral delivery or adeno-associated viral vectors
US5856174A (en) 1995-06-29 1999-01-05 Affymetrix, Inc. Integrated nucleic acid diagnostic device
US5866411A (en) 1995-09-08 1999-02-02 Pedersen; Finn Skou Retroviral vector, a replication system for said vector and avian or mammalian cells transfected with said vector
US5721118A (en) 1995-10-31 1998-02-24 The Regents Of The University Of California, San Diego Mammalian artificial chromosomes and methods of using same
US6022963A (en) 1995-12-15 2000-02-08 Affymetrix, Inc. Synthesis of oligonucleotide arrays using photocleavable protecting groups
US6013440A (en) 1996-03-11 2000-01-11 Affymetrix, Inc. Nucleic acid affinity columns
US6025155A (en) 1996-04-10 2000-02-15 Chromos Molecular Systems, Inc. Artificial chromosomes, uses thereof and methods for preparing artificial chromosomes
US6057100A (en) 1996-06-07 2000-05-02 Eos Biotechnology, Inc. Oligonucleotide arrays
US6846630B2 (en) 1996-10-18 2005-01-25 Takara Shuzo Co., Ltd. Nucleic acid encoding receptor type protein kinase
US6096718A (en) 1997-06-05 2000-08-01 Gene Targeting Corp. Tissue specific adenovirus vectors for breast cancer treatment
US6826296B2 (en) 1997-07-25 2004-11-30 Affymetrix, Inc. Method and system for providing a probe array chip design database
CN1273609A (zh) 1997-08-15 2000-11-15 希斯克有限公司 检测或量化核酸物类的方法和组合物
AU733589B2 (en) 1997-09-11 2001-05-17 Bioventures, Inc. Method of making high density arrays
US6465178B2 (en) 1997-09-30 2002-10-15 Surmodics, Inc. Target molecule attachment to surfaces
ATE340870T1 (de) 1998-04-03 2006-10-15 Compound Therapeutics Inc Adressierbare protein arrays
US6048695A (en) 1998-05-04 2000-04-11 Baylor College Of Medicine Chemically modified nucleic acids and methods for coupling nucleic acids to solid support
EP1086950B1 (en) * 1998-05-26 2010-09-29 Chugai Seiyaku Kabushiki Kaisha Heterocyclic indole derivatives and mono- or diazaindole derivatives
US6113913A (en) 1998-06-26 2000-09-05 Genvec, Inc. Recombinant adenovirus
US6277628B1 (en) 1998-10-02 2001-08-21 Incyte Genomics, Inc. Linear microarrays
US6277489B1 (en) 1998-12-04 2001-08-21 The Regents Of The University Of California Support for high performance affinity chromatography and other uses
US6221653B1 (en) 1999-04-27 2001-04-24 Agilent Technologies, Inc. Method of performing array-based hybridization assays using thermal inkjet deposition of sample fluids
US6653151B2 (en) 1999-07-30 2003-11-25 Large Scale Proteomics Corporation Dry deposition of materials for microarrays using matrix displacement
US20010008765A1 (en) 1999-12-06 2001-07-19 Fuji Photo Film Co., Ltd. DNA chip and reactive solid carrier
CZ301750B6 (cs) 1999-12-24 2010-06-09 Aventis Pharma Limited Bicyklický pyrrolový derivát, jeho použití pri výrobe léciva, farmaceutická kompozice tento derivát obsahující a pro použití pri lécení
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
US20040171062A1 (en) 2002-02-28 2004-09-02 Plexxikon, Inc. Methods for the design of molecular scaffolds and ligands
US20040142864A1 (en) 2002-09-16 2004-07-22 Plexxikon, Inc. Crystal structure of PIM-1 kinase
US20050048573A1 (en) 2003-02-03 2005-03-03 Plexxikon, Inc. PDE5A crystal structure and uses
EP1627045A2 (en) 2003-02-28 2006-02-22 Plexxikon, Inc. Pyk2 crystal structure and uses
US20050079548A1 (en) 2003-07-07 2005-04-14 Plexxikon, Inc. Ligand development using PDE4B crystal structures
RU2356889C2 (ru) 2003-07-17 2009-05-27 Плекссикон, Инк. Соединения, являющиеся активными по отношению к рецепторам, активируемым пролифератором пероксисом
US7348338B2 (en) 2003-07-17 2008-03-25 Plexxikon, Inc. PPAR active compounds
US20050164300A1 (en) 2003-09-15 2005-07-28 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
US7517970B2 (en) 2003-12-19 2009-04-14 Plexxikon, Inc. Nucleic acids encoding kinase and phosphatase enzymes, expression vectors and cells containing same
US20070066641A1 (en) 2003-12-19 2007-03-22 Prabha Ibrahim Compounds and methods for development of RET modulators
PT1696920E (pt) 2003-12-19 2015-01-14 Plexxikon Inc Compostos e métodos para o desenvolvimento de moduladores de ret
JP2008503446A (ja) 2004-05-06 2008-02-07 プレキシコン,インコーポレーテッド Pde4b阻害剤及びその使用
TW200616632A (en) 2004-06-17 2006-06-01 Plexxikon Inc Compounds modulating c-kit activity and uses therefor
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
JP2008508303A (ja) * 2004-07-27 2008-03-21 エスジーエックス ファーマシューティカルズ、インコーポレイテッド ピロロ−ピリジンキナーゼモジュレーター
US7605168B2 (en) 2004-09-03 2009-10-20 Plexxikon, Inc. PDE4B inhibitors
AU2005311826A1 (en) 2004-11-30 2006-06-08 Plexxikon, Inc. Indole derivatives for use as PPAR active compounds
CA2588953A1 (en) 2004-11-30 2006-06-08 Plexxikon, Inc. Ppar active compounds
US20060160135A1 (en) 2004-12-08 2006-07-20 Weiru Wang SF-1 and LRH-1 modulator development
AU2006272951A1 (en) 2005-05-17 2007-02-01 Plexxikon, Inc. Pyrrol (2,3-b) pyridine derivatives protein kinase inhibitors
MY153898A (en) 2005-06-22 2015-04-15 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
EP1940767A2 (en) 2005-09-07 2008-07-09 Plexxikon, Inc. Pparactive compounds
KR20080047591A (ko) 2005-09-07 2008-05-29 플렉시콘, 인코퍼레이티드 Ppar 조절인자로서 사용하기 위한 1,3-이치환된 인돌유도체
US20080234349A1 (en) 2005-09-07 2008-09-25 Jack Lin PPAR active compounds
ATE532788T1 (de) * 2006-04-26 2011-11-15 Hoffmann La Roche Pharmazeutische verbindungen
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
BRPI0720695A2 (pt) 2006-12-21 2014-02-18 Plexxikon Inc Compostos e métodos para modulação de cinase, e indicações para estes
WO2008079909A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
PE20081581A1 (es) 2006-12-21 2008-11-12 Plexxikon Inc COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA
PE20090159A1 (es) 2007-03-08 2009-02-21 Plexxikon Inc COMPUESTOS DERIVADOS DE ACIDO INDOL-PROPIONICO COMO MODULADORES PPARs
BRPI0808196A2 (pt) 2007-03-08 2014-07-08 Plexxikon Inc Compostos ativos de ppar
WO2009012283A1 (en) 2007-07-17 2009-01-22 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US8158636B2 (en) 2008-05-19 2012-04-17 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
PE20091846A1 (es) 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
US8110576B2 (en) 2008-06-10 2012-02-07 Plexxikon Inc. Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications
CN104530052A (zh) 2008-06-10 2015-04-22 普莱希科公司 用于激酶调节的5h-吡咯[2,3-b]吡嗪衍生物和其适应症
US8785489B2 (en) 2008-10-17 2014-07-22 Boehringer Ingelheim International Gmbh Heteroaryl substituted indole compounds useful as MMP-13 inhibitors
WO2010104973A1 (en) 2009-03-11 2010-09-16 Plexxikon, Inc. Pyrrolo [2, 3-b] pyridine derivatives for the inhibition of raf kinases
AR075812A1 (es) 2009-03-11 2011-04-27 Plexxikon Inc Derivados de pirrol[2,3-b]piridina como inhibidores de raf quinasa
WO2010111527A1 (en) 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use
MX349923B (es) 2009-04-03 2017-08-21 Hoffmann La Roche Composiciones del ácido propano-1-sulfónico {3-[5-(4-cloro-fenil)- 1h-pirrolo [2,3-b]-piridina-3-carbonil]-2,4-difluoro-fenil]-amida y el uso de las mismas.
CA2761009A1 (en) 2009-05-04 2010-11-11 Plexxikon, Inc. Compounds and methods for inhibition of renin, and indications therefor
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
ES2633317T3 (es) 2009-11-06 2017-09-20 Plexxikon, Inc. Compuestos y métodos para la modulación de quinasas, e indicaciones para ello
AU2010321883A1 (en) 2009-11-18 2012-05-31 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
KR20120112623A (ko) 2009-12-23 2012-10-11 플렉시콘, 인코퍼레이티드 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증
TWI510487B (zh) 2010-04-21 2015-12-01 Plexxikon Inc 用於激酶調節的化合物和方法及其適應症
US8642606B2 (en) 2010-09-29 2014-02-04 Plexxikon Inc. ZAP-70 active compounds
PT2672967T (pt) 2011-02-07 2018-12-07 Plexxikon Inc Compostos e métodos de modulação da quinase e suas indicações
AR085279A1 (es) 2011-02-21 2013-09-18 Plexxikon Inc Formas solidas de {3-[5-(4-cloro-fenil)-1h-pirrolo[2,3-b]piridina-3-carbonil]-2,4-difluor-fenil}-amida del acido propano-1-sulfonico
KR20140032430A (ko) 2011-05-17 2014-03-14 플렉시콘, 인코퍼레이티드 키나제 조절 및 그에 대한 적응증
DE102011111400A1 (de) * 2011-08-23 2013-02-28 Merck Patent Gmbh Bicyclische heteroaromatische Verbindungen
US20130158049A1 (en) 2011-12-20 2013-06-20 Hoffmann-La Roche Inc. 7-azaindole inhibitors of crac
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
AU2013312477B2 (en) 2012-09-06 2018-05-31 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
EP2738172A1 (en) 2012-11-28 2014-06-04 Almirall, S.A. New bicyclic compounds as crac channel modulators
PL2935248T3 (pl) 2012-12-21 2018-07-31 Plexxikon Inc Związki i sposoby modulacji kinaz i wskazania dla nich
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
TWI634111B (zh) 2013-03-15 2018-09-01 普雷辛肯公司 雜環化合物及其用途
BR112015028845A2 (pt) 2013-05-30 2017-07-25 Plexxikon Inc compostos para a modulação da quinase e indicações da mesma
WO2015134536A1 (en) 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
EA201691777A1 (ru) * 2014-03-21 2016-12-30 Бристол-Маерс Сквибб Компани Содержащие цианогруппу соединения азабензофурана для лечения гепатита с
WO2016044067A1 (en) 2014-09-15 2016-03-24 Plexxikon Inc. Heterocyclic compounds and uses thereof
WO2016164641A1 (en) 2015-04-08 2016-10-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CN107531706A (zh) 2015-05-06 2018-01-02 普莱希科公司 调节激酶的1H‑吡咯并[2,3‑b]吡啶衍生物的合成
HUE050506T2 (hu) 2015-05-06 2020-12-28 Plexxikon Inc Kinázokat moduláló vegyület szilárd formái
TWI812581B (zh) 2015-05-22 2023-08-21 美商普雷辛肯公司 激酶調節及其適應症
HUE050936T2 (hu) 2015-05-22 2021-01-28 Plexxikon Inc Heterociklusos vegyületek szintézise
US10829484B2 (en) 2015-07-28 2020-11-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
AU2016328619B2 (en) 2015-09-21 2020-07-16 Opna Bio SA Heterocyclic compounds and uses thereof
AU2017232610B2 (en) 2016-03-16 2021-07-22 Plexxikon Inc. Compounds and methods for kinase modulation and indications therefore

Also Published As

Publication number Publication date
US20170158690A1 (en) 2017-06-08
PH12018501179A1 (en) 2019-02-04
MX2018006856A (es) 2018-08-01
AU2016367147A1 (en) 2018-07-05
US9938273B2 (en) 2018-04-10
ES2899581T3 (es) 2022-03-14
JP6862468B2 (ja) 2021-04-21
BR112018011475A2 (pt) 2018-12-04
CN108368110A (zh) 2018-08-03
IL259803A (en) 2018-07-31
AU2016367147B2 (en) 2021-04-08
KR20180086247A (ko) 2018-07-30
CA3007462A1 (en) 2017-06-15
SG11201804711RA (en) 2018-07-30
WO2017100201A1 (en) 2017-06-15
JP2018537533A (ja) 2018-12-20
RU2018123825A (ru) 2020-01-15
EP3386980B1 (en) 2021-10-13
EP3386980A1 (en) 2018-10-17
CA3007462C (en) 2023-10-24

Similar Documents

Publication Publication Date Title
CO2018007052A2 (es) Compuestos y metodos para modulación de la quinasa, e indicaciones de los mismos
CL2018000730A1 (es) Compuestos heterocíclicos y usos de los mismos
WO2017019804A3 (en) Compounds and methods for kinase modulation, and indications therefor
CO2018005369A2 (es) Inhibidores triazol de acc y usos de los mismos
CL2017001050A1 (es) Nuevos compuestos de metil-quinolina útiles para inhibir la sintasa-1 de prostaglandina microsomal e2
NI201700095A (es) Derivados de nucleósidos sustituidos útiles como agentes antineoplásicos
CO2017006214A2 (es) Derivados de quinazolina utilizados para tratar el vih
DOP2018000268A (es) Derivados de carbonucleósidos sustituidos útiles como agentes antineoplásicos
BR112019005595A2 (pt) compostos e métodos para modulação de ido e tdo, e indicações para os mesmos
SV2017005405A (es) Compuestos y composiciones como inhibidores de quinasa raf
ECSP15043696A (es) Compuestos de heteroarilo y sus usos
NI201500119A (es) Compuestos de heteroarilo y sus usos
CR20150487A (es) Compuestos de biaril-amida como inhibidores de cinasa
CR20150371A (es) Inhibidores de prmt5 y sus usos
NI201900077A (es) Inhibidores selectivos de jak1
CO2020015747A2 (es) Analogos de rapamicina y usos de los mismos
GT201700190A (es) Desacetoxitubulisina h y análogos de esta
ECSP17069696A (es) Compuestos novedosos
ECSP18003372A (es) Compuestos tricíclicos y su uso como inhibidores de la fosfodiesterasa
CO2020004977A2 (es) Compuestos bicíclicos para su uso como inhibidores de la ripi quinasa
CU24434B1 (es) Compuestos derivados de n-(1,5-dimetil-3-oxo-2,3-dihidro-1h-pirazol-4-il)-4-metil-5-isoxazol-3-carboxamida activos como inhibidores selectivos de smurf-1
ECSP19013196A (es) Derivado de triazolopirazinona útil como un inhibidor de pde1 humana
ECSP18056196A (es) Derivados de indano
BR112019008606A2 (pt) inibidores de interações de mtor-deptor e métodos de uso dos mesmos
UY36464A (es) Compuestos de quinazolina