AU2017395023B2 - Compounds and methods for CDK8 modulation and indications therefor - Google Patents

Compounds and methods for CDK8 modulation and indications therefor Download PDF

Info

Publication number
AU2017395023B2
AU2017395023B2 AU2017395023A AU2017395023A AU2017395023B2 AU 2017395023 B2 AU2017395023 B2 AU 2017395023B2 AU 2017395023 A AU2017395023 A AU 2017395023A AU 2017395023 A AU2017395023 A AU 2017395023A AU 2017395023 B2 AU2017395023 B2 AU 2017395023B2
Authority
AU
Australia
Prior art keywords
alkyl
alkylene
heterocycloalkyl
cancer
membered
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
AU2017395023A
Other languages
English (en)
Other versions
AU2017395023A1 (en
Inventor
Aaron ALBERS
John BUELL
Elizabeth A. Burton
Phuongly Pham
Hannah POWERS
Songyuan Shi
Wayne Spevak
Guoxian Wu
Jeffrey Wu
Jiazhong Zhang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Plexxikon Inc
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 AU2017395023A1 publication Critical patent/AU2017395023A1/en
Application granted granted Critical
Publication of AU2017395023B2 publication Critical patent/AU2017395023B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Steroid Compounds (AREA)
AU2017395023A 2016-12-23 2017-12-21 Compounds and methods for CDK8 modulation and indications therefor Active AU2017395023B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662438682P 2016-12-23 2016-12-23
US62/438,682 2016-12-23
PCT/US2017/068045 WO2018136202A2 (en) 2016-12-23 2017-12-21 Compounds and methods for cdk8 modulation and indications therefor

Publications (2)

Publication Number Publication Date
AU2017395023A1 AU2017395023A1 (en) 2019-07-11
AU2017395023B2 true AU2017395023B2 (en) 2022-04-07

Family

ID=62152611

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017395023A Active AU2017395023B2 (en) 2016-12-23 2017-12-21 Compounds and methods for CDK8 modulation and indications therefor

Country Status (5)

Country Link
US (1) US10703757B2 (https=)
EP (1) EP3558991A2 (https=)
JP (1) JP7193460B2 (https=)
AU (1) AU2017395023B2 (https=)
WO (1) WO2018136202A2 (https=)

Families Citing this family (34)

* 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
US9624213B2 (en) 2011-02-07 2017-04-18 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
DK2970265T3 (en) 2013-03-15 2018-10-01 Plexxikon Inc HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
CN105228983A (zh) 2013-05-30 2016-01-06 普莱希科公司 用于激酶调节的化合物及其适应症
JP6530826B2 (ja) 2015-05-06 2019-06-12 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼを修飾する１ｈ−ピロロ［２，３−ｂ］ピリジン誘導体の合成
LT3292123T (lt) 2015-05-06 2020-12-28 Plexxikon Inc. Junginio, moduliuojančio kinazes, kietos formos
WO2016191295A1 (en) 2015-05-22 2016-12-01 Plexxikon Inc. Solid forms of a compound for modulating kinases
ES2913048T3 (es) 2015-09-21 2022-05-31 Opna Immuno Oncology Sa Compuestos heterocíclicos y usos de estos
CN109071546B (zh) 2016-02-24 2021-03-02 辉瑞大药厂 作为jak抑制剂的吡唑并[1,5-a]吡嗪-4-基衍生物
EP3558991A2 (en) 2016-12-23 2019-10-30 Plexxikon Inc. Compounds and methods for cdk8 modulation and indications therefor
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
WO2018175746A1 (en) 2017-03-24 2018-09-27 Kura Oncology, Inc. Methods for treating hematological malignancies and ewing's sarcoma
WO2018226846A1 (en) 2017-06-07 2018-12-13 Plexxikon Inc. Compounds and methods for kinase modulation
AU2018307910B2 (en) 2017-07-25 2024-07-25 Daiichi Sankyo Company, Limited Formulations of a compound modulating kinases
WO2019034973A1 (en) 2017-08-14 2019-02-21 Pfizer Inc. PYRAZOLO [1,5-A] PYRAZIN-4-YL AND RELATED DERIVATIVES
US10717735B2 (en) 2017-10-13 2020-07-21 Plexxikon Inc. Solid forms of a compound for modulating kinases
AU2018354423B2 (en) 2017-10-27 2024-11-07 Plexxikon Inc. Formulations of a compound modulating kinases
WO2019126731A1 (en) 2017-12-22 2019-06-27 Petra Pharma Corporation Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
EP3768666A1 (en) 2018-03-20 2021-01-27 Plexxikon Inc. Compounds and methods for ido and tdo modulation, and indications therefor
JP2022503792A (ja) * 2018-09-26 2022-01-12 クラ オンコロジー，インク． メニン阻害剤を用いた血液悪性腫瘍の処置
WO2020071550A1 (ja) * 2018-10-04 2020-04-09 京都薬品工業株式会社 Ｃｄｋ８阻害剤およびその用途
WO2020081689A1 (en) 2018-10-16 2020-04-23 Dana-Farber Cancer Institute, Inc. Azaindole inhibitors of wild-type and mutant forms of lrrk2
SG11202110714VA (en) 2019-04-09 2021-10-28 Plexxikon Inc Condensed azines for ep300 or cbp modulation and indications therefor
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
EP4065111A4 (en) 2019-11-26 2023-09-20 Dana-Farber Cancer Institute, Inc. Potent and selective azaindole inhibitors of cdk8 and cdk19
US12509444B2 (en) 2019-12-06 2025-12-30 Plexxikon Inc. Compounds and methods for CD73 modulation and indications therefor
US11807626B2 (en) 2020-04-23 2023-11-07 Opna Bio SA Compounds and methods for CD73 modulation and indications therefor
TW202227068A (zh) 2020-08-21 2022-07-16 美商普雷辛肯公司 組合藥物療法
WO2022257894A1 (zh) * 2021-06-07 2022-12-15 贝达药业股份有限公司 P300抑制剂及其在医药上的应用
WO2023078337A1 (en) * 2021-11-04 2023-05-11 Insilico Medicine Ip Limited Cdk8/19 dual inhibitors and methods of use
CN115772170B (zh) * 2021-12-03 2025-05-16 徐诺药业(南京)有限公司 一种吡唑并[1,5-a]吡啶衍生物及其制备方法和应用
EP4519258A1 (en) * 2022-05-05 2025-03-12 University of Dundee Inhibitors of cdk8 and cdk19
WO2025261366A1 (zh) * 2024-06-18 2025-12-26 南京正大天晴制药有限公司 一种五元并六元杂环化合物及用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015050505A1 (en) * 2013-10-03 2015-04-09 Agency For Science, Technology And Research Bicyclic alkyne derivatives and uses thereof
WO2015100117A1 (en) * 2013-12-26 2015-07-02 Cephalon, Inc. Pyrazolo[1,5-a]pyridine derivatives and methods of their use

Family Cites Families (126)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1016075A (en) 1911-10-18 1912-01-30 George Kowalsky Feed-bag.
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
EP0154734B1 (en) 1984-03-15 1990-08-29 Immunex Corporation Immediate ligand detection assay, a test kit and its formation
US5700637A (en) 1988-05-03 1997-12-23 Isis Innovation Limited Apparatus and method for analyzing polynucleotide sequences and method of generating oligonucleotide arrays
US6054270A (en) 1988-05-03 2000-04-25 Oxford Gene Technology Limited Analying polynucleotide sequences
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
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
US5527681A (en) 1989-06-07 1996-06-18 Affymax Technologies N.V. Immobilized molecular synthesis of systematically substituted compounds
WO1991018088A1 (en) 1990-05-23 1991-11-28 The United States Of America, Represented By The Secretary, United States Department Of Commerce Adeno-associated virus (aav)-based eucaryotic vectors
CA2113990A1 (en) 1991-07-26 1993-02-18 Frederick L. Moolten Cancer therapy utilizing malignant cells
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
US6468742B2 (en) 1993-11-01 2002-10-22 Nanogen, Inc. Methods for determination of single nucleic acid polymorphisms using bioelectronic microchip
US5965452A (en) 1996-07-09 1999-10-12 Nanogen, Inc. Multiplexed active biologic array
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
WO1997016533A1 (en) 1995-10-31 1997-05-09 The Regents Of The University Of California 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
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
EP1012335A4 (en) 1997-08-15 2004-06-09 Hyseq Inc EXPERIENCE AND COMPOSITIONS FOR DETECTING OR QUANTIFYING NUCLEIC ACID SPECIES
IL134702A (en) 1997-09-11 2004-03-28 Bioventures Inc High density arrays and methods of making the same
US6465178B2 (en) 1997-09-30 2002-10-15 Surmodics, Inc. Target molecule attachment to surfaces
CA2323638A1 (en) 1998-04-03 1999-10-14 Phylos, Inc. Addressable 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
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
US20040171062A1 (en) 2002-02-28 2004-09-02 Plexxikon, Inc. Methods for the design of molecular scaffolds and ligands
ES2377318T3 (es) 2002-09-06 2012-03-26 Cerulean Pharma Inc. Polímeros a base de ciclodextrina para el suministro de los agentes terapéuticos enlazados covalentemente a ellos
AU2003272548A1 (en) 2002-09-16 2004-04-30 Plexxikon, Inc. Crystal structure of pim-1 kinase
US20050048573A1 (en) 2003-02-03 2005-03-03 Plexxikon, Inc. PDE5A crystal structure and uses
JP2007524374A (ja) 2003-02-28 2007-08-30 プレキシコン，インコーポレーテッド Ｐｙｋ２結晶構造および使用
US20050079548A1 (en) 2003-07-07 2005-04-14 Plexxikon, Inc. Ligand development using PDE4B crystal structures
US7348338B2 (en) 2003-07-17 2008-03-25 Plexxikon, Inc. PPAR active compounds
CA2532403A1 (en) 2003-07-17 2005-02-03 James Arnold Ppar active compounds
WO2005028624A2 (en) 2003-09-15 2005-03-31 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
US20070066641A1 (en) 2003-12-19 2007-03-22 Prabha Ibrahim Compounds and methods for development of RET modulators
US7517970B2 (en) 2003-12-19 2009-04-14 Plexxikon, Inc. Nucleic acids encoding kinase and phosphatase enzymes, expression vectors and cells containing same
CN1925855B (zh) 2003-12-19 2010-06-16 普莱希科公司 开发Ret调节剂的化合物和方法
EP1742627A4 (en) 2004-05-06 2009-08-26 Plexxikon Inc PDE4B HEMMER AND ITS USE
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
JP2008503473A (ja) 2004-06-17 2008-02-07 プレキシコン，インコーポレーテッド Ｃ−ｋｉｔ活性を調節する化合物
WO2006026754A2 (en) 2004-09-03 2006-03-09 Plexxikon, Inc. Bicyclic heteroaryl pde4b inhibitors
JP4935357B2 (ja) * 2004-11-08 2012-05-23 Ｍｓｄ株式会社 新規縮環イミダゾール誘導体
JP2008521831A (ja) 2004-11-30 2008-06-26 プレキシコン，インコーポレーテッド Ｐｐａｒ活性化合物
JP2008521829A (ja) 2004-11-30 2008-06-26 プレキシコン，インコーポレーテッド Ｐｐａｒ活性化合物
US20060160135A1 (en) 2004-12-08 2006-07-20 Weiru Wang SF-1 and LRH-1 modulator development
US7846941B2 (en) 2005-05-17 2010-12-07 Plexxikon, Inc. Compounds modulating c-kit and c-fms activity and uses therefor
UA95244C2 (ru) 2005-06-22 2011-07-25 Плексикон, Инк. Соединения и способ модулирования активности киназ, и показания для их применения
BRPI0615948A2 (pt) 2005-09-07 2011-05-31 Plexxikon Inc composto ativo de ppar, sua composição, seu kit e seu uso
JP2009509932A (ja) 2005-09-07 2009-03-12 プレキシコン，インコーポレーテッド Ｐｐａｒ活性化合物
WO2007030559A2 (en) 2005-09-07 2007-03-15 Plexxikon, Inc. 1, 3-disubstituted indole derivatives for use as ppar modulators
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
JP2010514695A (ja) 2006-12-21 2010-05-06 プレキシコン，インコーポレーテッド キナーゼ調節のための化合物および方法およびそのための適応症
WO2008079909A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
FR2912744B1 (fr) * 2007-02-16 2012-09-07 Centre Nat Rech Scient Composes pyrrolo°2,3-b!pyridine,composes azaindoles utiles dans la synthese de ces composes pyrrolo°2,3-b!pyridine, leurs procedes de fabrication et leurs utilisations.
PE20090159A1 (es) 2007-03-08 2009-02-21 Plexxikon Inc COMPUESTOS DERIVADOS DE ACIDO INDOL-PROPIONICO COMO MODULADORES PPARs
EP2121591A2 (en) 2007-03-08 2009-11-25 Plexxikon, Inc. Ppar active compounds
WO2009012283A1 (en) 2007-07-17 2009-01-22 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2009143018A2 (en) 2008-05-19 2009-11-26 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
JP5767965B2 (ja) 2008-06-10 2015-08-26 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５ｈ−ピロロ［２，３−ｂ］ピラジン誘導体、およびその適応症
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
US20110201599A1 (en) * 2008-07-03 2011-08-18 Exelixis, Inc. CDK Modulators
WO2010104945A1 (en) 2009-03-11 2010-09-16 Plexxikon, Inc. Pyrrolo [2, 3-b] pyridine derivatives for the inhibition of raf kinases
AU2010224184A1 (en) 2009-03-11 2011-09-29 Plexxikon, Inc. Pyrrolo [2, 3-b] pyridine derivatives for the inhibition of Raf kinases
WO2010111527A1 (en) 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use
MY172424A (en) 2009-04-03 2019-11-25 Hoffmann La Roche Propane- i-sulfonic acid {3- (4-chloro-phenyl)-1h-pyrrolo [2, 3-b] pyridine-3-carconyl] -2, 4-difluoro-phenyl} -amide compositions and uses thereof
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
CN106220623A (zh) 2009-11-06 2016-12-14 普莱希科公司 用于激酶调节的化合物和方法及其适应症
ES2627911T3 (es) 2009-11-18 2017-08-01 Plexxikon, Inc. Derivados de N-[2-fluoro-3-(4-amino-7H-pirrolo[2,3-d]pirimidin-5-carbonil)-fenil]-4-bencenosulfonamida como moduladores de la proteína quinasa Raf para el tratamiento del cáncer
BR112012015745A2 (pt) 2009-12-23 2016-05-17 Plexxikon Inc compostos e métodos para a modulação de quinase, e indicações dos mesmos
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
US9624213B2 (en) 2011-02-07 2017-04-18 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
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
JP6113151B2 (ja) 2011-05-17 2017-04-12 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼ調節およびその適応症
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
EP2892534B8 (en) 2012-09-06 2021-09-15 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US9260426B2 (en) * 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
MX365640B (es) 2012-12-21 2019-06-10 Plexxikon Inc Compuestos y metodos para la modulacion de quinasas y sus indicaciones.
MX2015010700A (es) 2013-02-21 2017-01-23 Calitor Sciences Llc Compuestos heteroaromaticos como moduladores de la p13 cinasa.
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
DK2970265T3 (en) 2013-03-15 2018-10-01 Plexxikon Inc HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
CN105228983A (zh) 2013-05-30 2016-01-06 普莱希科公司 用于激酶调节的化合物及其适应症
US9771369B2 (en) 2014-03-04 2017-09-26 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
ES2774177T3 (es) 2014-09-15 2020-07-17 Plexxikon Inc Compuestos heterocíclicos y usos de estos
WO2016101119A1 (en) 2014-12-23 2016-06-30 Merck Sharp & Dohme Corp. Fused heteroaryl derivatives as orexin receptor antagonists
JP6530826B2 (ja) 2015-05-06 2019-06-12 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼを修飾する１ｈ−ピロロ［２，３−ｂ］ピリジン誘導体の合成
LT3292123T (lt) 2015-05-06 2020-12-28 Plexxikon Inc. Junginio, moduliuojančio kinazes, kietos formos
US9814714B2 (en) 2015-05-22 2017-11-14 Plexxikon Inc. Kinase modulation, and indications therefor
WO2016191295A1 (en) 2015-05-22 2016-12-01 Plexxikon Inc. Solid forms of a compound for modulating kinases
US10829484B2 (en) 2015-07-28 2020-11-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
ES2913048T3 (es) 2015-09-21 2022-05-31 Opna Immuno Oncology Sa Compuestos heterocíclicos y usos de estos
MX2018006856A (es) 2015-12-07 2018-08-01 Plexxikon Inc Compuestos y metodos para modulacion de la quinasa, e indicaciones de los mismos.
ES2904615T3 (es) 2016-03-16 2022-04-05 Plexxikon Inc Compuestos y métodos para la modulación de quinasas e indicaciones al respecto
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
EP3558991A2 (en) 2016-12-23 2019-10-30 Plexxikon Inc. Compounds and methods for cdk8 modulation and indications therefor
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
AU2018307910B2 (en) 2017-07-25 2024-07-25 Daiichi Sankyo Company, Limited Formulations of a compound modulating kinases

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015050505A1 (en) * 2013-10-03 2015-04-09 Agency For Science, Technology And Research Bicyclic alkyne derivatives and uses thereof
WO2015100117A1 (en) * 2013-12-26 2015-07-02 Cephalon, Inc. Pyrazolo[1,5-a]pyridine derivatives and methods of their use

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Yasuyoshi, M. et al. "Acid-catalyzed reactions of 3-(α-hydroxybenzyl)pyrazolo[1,5-a]pyridines", Journal of Heterocyclic Chemistry (1988), 25(1), 327-31 *

Also Published As

Publication number Publication date
EP3558991A2 (en) 2019-10-30
US10703757B2 (en) 2020-07-07
JP7193460B2 (ja) 2022-12-20
CA3047580A1 (en) 2018-07-26
AU2017395023A1 (en) 2019-07-11
US20180215763A1 (en) 2018-08-02
JP2020504727A (ja) 2020-02-13
WO2018136202A2 (en) 2018-07-26
WO2018136202A3 (en) 2018-10-04

Similar Documents

Publication Publication Date Title
AU2017395023B2 (en) Compounds and methods for CDK8 modulation and indications therefor
AU2017331345B2 (en) Compounds and methods for IDO and TDO modulation, and indications therefor
AU2016367147B2 (en) Compounds and methods for kinase modulation, and indications therefor
AU2017232610B2 (en) Compounds and methods for kinase modulation and indications therefore
ES2664985T3 (es) Compuestos y métodos para modulación de quinasa, e indicaciones de los mismos
WO2017019804A2 (en) Compounds and methods for kinase modulation, and indications therefor
WO2018226846A1 (en) Compounds and methods for kinase modulation
WO2021202900A1 (en) 1,6-naphthyridine compounds and methods for csk modulation and indications therefor
CA3047580C (en) Compounds and methods for cdk8 modulation and indications therefor
HK1213877B (en) Compounds and methods for kinase modulation, and indications therefor

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)