CN101048407A - 双环杂芳基pde4b抑制剂 - Google Patents

双环杂芳基pde4b抑制剂 Download PDF

Info

Publication number
CN101048407A
CN101048407A CNA200580036980XA CN200580036980A CN101048407A CN 101048407 A CN101048407 A CN 101048407A CN A200580036980X A CNA200580036980X A CN A200580036980XA CN 200580036980 A CN200580036980 A CN 200580036980A CN 101048407 A CN101048407 A CN 101048407A
Authority
CN
China
Prior art keywords
optionally substituted
compound
pde4b
replaces
alkynyl
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.)
Pending
Application number
CNA200580036980XA
Other languages
English (en)
Chinese (zh)
Inventor
P·L·易卜拉欣
R·E·布雷默
S·J·吉勒特
H·丘
M·内斯皮
S·马莫
C·张
D·R·阿尔蒂
B·李
R·L·朱克曼
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 CN101048407A publication Critical patent/CN101048407A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06—Antiabortive agents; Labour repressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • 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
    • C07D401/12—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 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
    • C07D405/02—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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Spectroscopy & Molecular Physics (AREA)
  • Physics & Mathematics (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Theoretical Computer Science (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Medical Informatics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Evolutionary Biology (AREA)
  • Biotechnology (AREA)
  • Computing Systems (AREA)
  • Biophysics (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
CNA200580036980XA 2004-09-03 2005-09-02 双环杂芳基pde4b抑制剂 Pending CN101048407A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US60740704P 2004-09-03 2004-09-03
US60/607,407 2004-09-03

Publications (1)

Publication Number Publication Date
CN101048407A true CN101048407A (zh) 2007-10-03

Family

ID=36000749

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA200580036980XA Pending CN101048407A (zh) 2004-09-03 2005-09-02 双环杂芳基pde4b抑制剂

Country Status (7)

Country Link
US (1) US7605168B2 (enExample)
EP (1) EP1786813A2 (enExample)
JP (1) JP2008512380A (enExample)
CN (1) CN101048407A (enExample)
AU (1) AU2005279795A1 (enExample)
CA (1) CA2583428A1 (enExample)
WO (1) WO2006026754A2 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103748076A (zh) * 2011-02-11 2014-04-23 默沙东公司 RORγT抑制剂
CN113754796A (zh) * 2021-10-18 2021-12-07 中国石油大学(华东) 一种萘修饰交联的β-环糊精凝胶、制备方法及应用
WO2024153112A1 (zh) * 2023-01-17 2024-07-25 瑞石生物医药有限公司 Pde4抑制剂、其制备方法及其在医药上的应用

Families Citing this family (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6663602B2 (en) 2000-06-16 2003-12-16 Novo Nordisk A/S Injection device
CA2584760C (en) 2004-10-21 2013-12-24 Novo Nordisk A/S Dial-down mechanism for wind-up pen
EP2354139A1 (en) * 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
US7579360B2 (en) 2005-06-09 2009-08-25 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
US7572807B2 (en) 2005-06-09 2009-08-11 Bristol-Myers Squibb Company Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
ATE523595T1 (de) 2005-06-24 2011-09-15 Bayer Bioscience Nv Verfahren zur veränderung der reaktivität von pflanzenzellwänden
DE102006012617A1 (de) * 2006-03-20 2007-09-27 Merck Patent Gmbh 4-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate
ES2389866T3 (es) 2006-05-18 2012-11-02 Novo Nordisk A/S Dispositivo de inyección con medio de bloqueo de modo
US8097699B2 (en) 2006-08-30 2012-01-17 Rsr Limited Crystal structure of thyroid stimulating hormone receptor
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
GB0702456D0 (en) 2007-02-08 2007-03-21 Astrazeneca Ab New combination
CA2695004C (en) 2007-07-17 2016-01-19 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
US8119658B2 (en) 2007-10-01 2012-02-21 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
WO2009067597A1 (en) * 2007-11-21 2009-05-28 Decode Genetics Ehf 4- (or 5-) substituted catechol derivatives
CN101965208B (zh) 2007-12-20 2013-04-17 阿斯利康(瑞典)有限公司 用于在气流中夹带粉末的方法和分配器
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
TW201036957A (en) 2009-02-20 2010-10-16 Astrazeneca Ab Novel salt 628
RU2536826C2 (ru) 2009-07-01 2014-12-27 Астразенека Аб Устройство раздачи и способ увеличения порошкообразного средства в поток воздуха
KR20120097512A (ko) 2009-11-18 2012-09-04 플렉시콘, 인코퍼레이티드 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증
WO2011073662A1 (en) 2009-12-17 2011-06-23 Astrazeneca Ab Combination of a benzoxazinone and a further agent for treating respiratory diseases
EP2516438A4 (en) 2009-12-23 2013-06-12 Plexxikon Inc COMPOUNDS AND METHODS FOR KINASE MODULATION AND DISPLAYS THEREFOR
MX2012008906A (es) 2010-02-10 2012-08-15 Astrazeneca Uk Ltd Proceso para proporcionar un cartucho relleno para un inhalador.
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
JO3131B1 (ar) 2010-04-27 2017-09-20 Glaxosmithkline Llc مركبات كيميائية
US8673922B2 (en) 2010-07-15 2014-03-18 Bristol-Myers Squibb Company Azaindazole compounds
KR20130036287A (ko) 2010-07-21 2013-04-11 아스트라제네카 아베 흡입기
BR112013001342A2 (pt) 2010-07-21 2016-05-17 Astrazeneca Ab dispositivo
TR201816421T4 (tr) 2011-02-07 2018-11-21 Plexxikon Inc Kinaz modülasyonu için bileşikler ve metotlar ve bunların endikasyonları.
RU2631487C2 (ru) 2011-05-17 2017-09-22 Плексксикон Инк. Модуляция киназ и показания к её применению
ES2624984T3 (es) * 2011-07-15 2017-07-18 Viiv Healthcare Uk Limited Derivados de ácido 2-(pirrolo[2,3-b]piridin-5-il)-2-(t-butoxi)-acético como inhibidores de la replicación del VIH para el tratamiento del SIDA
GB201115874D0 (en) 2011-09-14 2011-10-26 Astrazeneca Ab Inhaler
MX2014007375A (es) 2011-12-29 2014-08-22 Novo Nordisk As Jeringa autoinyectora de cuerda basada en resorte de torsion con mecanismo dosificador giratorio de aumento/disminucion.
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
EP2836240B1 (en) * 2012-04-10 2019-03-13 Georgia State University Research Foundation, Inc. Compositions and methods for treating otitis media and other conditions with inhibitors of cyld
WO2014026329A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof
WO2014026330A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 3-AMINOCYCLOALKYL COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
WO2014026327A1 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof
AU2013312477B2 (en) 2012-09-06 2018-05-31 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
SG11201504754QA (en) 2012-12-21 2015-07-30 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
EP2958915B1 (en) 2013-02-19 2017-07-05 Pfizer Inc Azabenzimidazole compounds as inhibitors of pde4 isozymes for the treatment of cns and other disorders
PT2970265T (pt) 2013-03-15 2018-10-23 Plexxikon Inc Compostos heterocíclicos e suas utilizações
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
WO2014194127A1 (en) 2013-05-30 2014-12-04 Plexxikon Inc. Compounds for kinase modulation, and indications therefor
US9771369B2 (en) 2014-03-04 2017-09-26 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
JP6713982B2 (ja) 2014-07-24 2020-06-24 ファイザー・インク ピラゾロピリミジン化合物
MD20170011A2 (ro) 2014-08-06 2017-08-31 Pfizer Inc. Compuşi imidazopiridazinici
EP3194392B1 (en) 2014-09-15 2020-01-01 Plexxikon, Inc. Heterocyclic compounds and uses thereof
US10221142B2 (en) 2015-02-11 2019-03-05 Merck Sharp & Dohme Corp. Substituted pyrazole compounds as RORgammaT inhibitors and uses thereof
US10160755B2 (en) 2015-04-08 2018-12-25 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2016179415A1 (en) 2015-05-06 2016-11-10 Plexxikon Inc. Solid forms of a compound modulating kinases
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
WO2017019804A2 (en) 2015-07-28 2017-02-02 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
EP4071149A3 (en) 2015-09-21 2023-01-25 Opna Immuno Oncology, SA Heterocyclic compounds and uses thereof
EP3368516B1 (en) 2015-10-27 2020-07-15 Merck Sharp & Dohme Corp. SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
CA3002853A1 (en) 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof
US10287272B2 (en) 2015-10-27 2019-05-14 Merck Sharp & Dohme Corp. Substituted indazole compounds as RORgammaT inhibitors and uses thereof
BR112018011475A2 (pt) 2015-12-07 2018-12-04 Plexxikon Inc compostos e métodos para modulação de quinase e indicação para a mesma
EP3430005B1 (en) 2016-03-16 2021-12-08 Plexxikon Inc. Compounds and methods for kinase modulation and indications therefore
US10513509B2 (en) 2016-05-26 2019-12-24 Recurium Ip Holdings, Llc EGFR inhibitor compounds
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
US10703757B2 (en) 2016-12-23 2020-07-07 Plexxikon Inc. Compounds and methods for CDK8 modulation and indications therefor
US10577366B2 (en) 2017-03-20 2020-03-03 Plexxikon Inc. Crystalline forms of a compound that inhibits bromodomain
WO2018226846A1 (en) 2017-06-07 2018-12-13 Plexxikon Inc. Compounds and methods for kinase modulation
TWI805599B (zh) 2017-07-25 2023-06-21 美商第一三共公司 激酶調節化合物之調配物
AU2018348241B2 (en) 2017-10-13 2023-01-12 Opna Bio SA Solid forms of a compound for modulating kinases
CA3080197C (en) 2017-10-27 2023-12-19 Plexxikon Inc. Formulations of a compound modulating kinases
CN112119072A (zh) 2018-03-20 2020-12-22 普莱希科公司 用于ido和tdo调节的化合物和方法，以及其适应症
AU2020271836B2 (en) 2019-04-09 2025-11-13 Opna Bio SA Condensed azines for EP300 or CBP modulation and indications therefor
US12509444B2 (en) 2019-12-06 2025-12-30 Plexxikon Inc. Compounds and methods for CD73 modulation and indications therefor
WO2021216898A1 (en) 2020-04-23 2021-10-28 Plexxikon Inc. Compounds and methods for cd73 modulation and indications therefor
JP2023524465A (ja) 2020-04-29 2023-06-12 プレキシコン インコーポレイティド 複素環式化合物の合成
AU2021327375A1 (en) 2020-08-21 2023-03-16 Opna Bio SA Combinational drug anticancer therapies
CN116370640A (zh) * 2023-04-26 2023-07-04 中国医学科学院基础医学研究所 Pde4b抑制剂在制备预防和/或治疗肺动脉高压的药物中的应用

Family Cites Families (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US587707A (en) * 1897-08-10 Tension device for sewing-machine binders
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
US5688655A (en) 1988-02-10 1997-11-18 Ict Pharmaceuticals, Inc. Method of screening for protein inhibitors and activators
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
US4861891A (en) * 1988-08-31 1989-08-29 Pfizer Inc. Antidepressant N-substituted nicotinamide compounds
JP3082204B2 (ja) * 1988-09-01 2000-08-28 ホワイトヘッド・インスティチュート・フォー・バイオメディカル・リサーチ 両栄養性および環境栄養性宿主域を持つ組換え体レトロウイルス
US5703055A (en) * 1989-03-21 1997-12-30 Wisconsin Alumni Research Foundation Generation of antibodies through lipid mediated DNA delivery
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
US5744101A (en) * 1989-06-07 1998-04-28 Affymax Technologies N.V. Photolabile nucleoside protecting groups
US5527681A (en) * 1989-06-07 1996-06-18 Affymax Technologies N.V. Immobilized molecular synthesis of systematically substituted compounds
US5800992A (en) * 1989-06-07 1998-09-01 Fodor; Stephen P.A. Method of detecting nucleic acids
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
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
DE69434998T2 (de) * 1993-05-27 2008-03-13 Aventis Pharmaceuticals Inc. Topologisch getrennte, kodierende Festphasen-Bibliotheken
US5840485A (en) * 1993-05-27 1998-11-24 Selectide Corporation Topologically segregated, encoded solid phase libraries
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
JP2928079B2 (ja) * 1994-02-14 1999-07-28 永信薬品工業股▲ふん▼有限公司 １−（置換ベンジル）−３−（置換アリール）縮合ピラゾール類、その製造法及びその用途
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
US5763198A (en) * 1994-07-22 1998-06-09 Sugen, Inc. Screening assays for compounds
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
US5837815A (en) 1994-12-15 1998-11-17 Sugen, Inc. PYK2 related polypeptide products
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
US5747276A (en) * 1995-09-15 1998-05-05 The Scripps Research Institute Screening methods for the identification of novel antibiotics
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
US5922557A (en) * 1997-01-09 1999-07-13 Merck & Co., Inc. System for stably expressing a high-affinity camp phosphodiesterase and use thereof
US6294330B1 (en) * 1997-01-31 2001-09-25 Odyssey Pharmaceuticals Inc. Protein fragment complementation assays for the detection of biological or drug interactions
EP0972071A4 (en) * 1997-03-07 2004-04-21 Tropix Inc TEST ARRANGEMENT FOR PROTEAS INHIBITORS
JP2000510481A (ja) 1997-04-04 2000-08-15 ファイザー・プロダクツ・インク ニコチンアミド誘導体
CA2238283C (en) * 1997-05-30 2002-08-20 Cell Pathways, Inc. Method for identifying compounds for inhibition of neoplastic lesions, pharmaceutical compositions from such compounds and uses of such compounds and compositions for treating neoplastic lesions
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
CA2300940A1 (en) 1997-08-15 1999-02-25 Hyseq, Inc. Methods and compositions for detection or quantification of nucleic acid species
AU733589B2 (en) * 1997-09-11 2001-05-17 Bioventures, Inc. Method of making high density arrays
US6178384B1 (en) * 1997-09-29 2001-01-23 The Trustees Of Columbia University In The City Of New York Method and apparatus for selecting a molecule based on conformational free energy
US6465178B2 (en) * 1997-09-30 2002-10-15 Surmodics, Inc. Target molecule attachment to surfaces
MA24682A1 (fr) 1997-10-23 1999-07-01 Smithkline Beecham Corp Formes polymorphes nouvelles de cipamfylline, procede pour leur preparation et compositions les contenant
AU738792B2 (en) 1997-10-27 2001-09-27 Agouron Pharmaceuticals, Inc. 4-aminothiazole derivatives, their preparation and their use as inhibitors of cyclin-dependent kinases
US6537749B2 (en) 1998-04-03 2003-03-25 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
US6288234B1 (en) * 1998-06-08 2001-09-11 Advanced Medicine, Inc. Multibinding inhibitors of microsomal triglyceride transferase protein
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
US20020009764A1 (en) * 1999-10-08 2002-01-24 W. Joseph Thompson Methods for identifying compounds for inhibition of neoplastic lesions, and pharmaceutical compositions containing such compounds
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
PE20010306A1 (es) * 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
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
US6387942B2 (en) * 2000-06-19 2002-05-14 Yung Shin Pharmaceutical Ind. Co. Ltd Method of treating disorders related to protease-activated receptors-induced cell activation
US20020165237A1 (en) * 2000-08-11 2002-11-07 Fryburg David Albert Treatment of the insulin resistance syndrome
TWI262920B (en) * 2000-10-27 2006-10-01 Elbion Ag New 7-azaindoles, their use as inhibitors of phosphodiesterase 4, and a method for synthesizing them
EP1341783A1 (en) * 2000-11-21 2003-09-10 Smithkline Beecham Plc Isoquinoline derivatives useful in the treatment of cns disorders
US6774134B2 (en) * 2000-12-20 2004-08-10 Bristol-Myers Squibb Company Heterocyclic substituted 2-methyl-benzimidazole antiviral agents
CA2436551A1 (en) * 2001-01-31 2002-08-08 Pfizer Products Inc. Thiazolyl-, oxazolyl-, pyrrolyl-, and imidazolyl-acid amide derivatives useful as inhibitors of pde4 isozymes
GB0111186D0 (en) * 2001-05-08 2001-06-27 Smithkline Beecham Plc Novel compounds
FR2828693B1 (fr) * 2001-08-14 2004-06-18 Exonhit Therapeutics Sa Nouvelle cible moleculaire de la neurotoxicite
GB0319037D0 (en) * 2003-08-13 2003-09-17 Glaxo Group Ltd 7-Azaindole Derivatives

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103748076A (zh) * 2011-02-11 2014-04-23 默沙东公司 RORγT抑制剂
CN113754796A (zh) * 2021-10-18 2021-12-07 中国石油大学(华东) 一种萘修饰交联的β-环糊精凝胶、制备方法及应用
WO2024153112A1 (zh) * 2023-01-17 2024-07-25 瑞石生物医药有限公司 Pde4抑制剂、其制备方法及其在医药上的应用

Also Published As

Publication number Publication date
US7605168B2 (en) 2009-10-20
WO2006026754A9 (en) 2006-04-20
WO2006026754B1 (en) 2007-02-22
WO2006026754A2 (en) 2006-03-09
AU2005279795A1 (en) 2006-03-09
WO2006026754A3 (en) 2007-01-11
JP2008512380A (ja) 2008-04-24
EP1786813A2 (en) 2007-05-23
US20060100218A1 (en) 2006-05-11
CA2583428A1 (en) 2006-03-09

Similar Documents

Publication Publication Date Title
CN101048407A (zh) 双环杂芳基pde4b抑制剂
CN1925855A (zh) 开发Ret调节剂的化合物和方法
AU733890B2 (en) Crystal structures of a protein tyrosine kinase
WO2004004652A2 (en) Mitotic kinesin binding site
WO2004078923A2 (en) Pyk2 crystal structure and uses
JP7336178B2 (ja) 治療における使用のための新規のＴＮＦα構造
WO1998007835A9 (en) Crystal structures of a protein tyrosine kinase
CA2503905A1 (en) Crystal structure of pim-1 kinase
US20050079548A1 (en) Ligand development using PDE4B crystal structures
AU2014361662A1 (en) Systems and methods of selecting compounds with reduced risk of cardiotoxicity
CN1788084A (zh) 人冠状病毒229e主蛋白酶的晶体结构及其在开发sars抑制剂中的用途
WO2009055509A9 (en) Cholesterol consensus motif of membrane proteins
US7662581B1 (en) Eg5 co-crystals
AU6960696A (en) Crystalline zap family proteins
WO2001085748A2 (en) Designing modulators for glycosyltransferases
CN101792745B (zh) 流感病毒聚合酶亚基pa氨基端多肽的表达纯化及pa氨基端多肽的晶体结构
WO2008037688A2 (en) Crystalline forms of pkc alpha kinase, methods of making such crystals, and uses thereof
CN1701122A (zh) Pim－1激酶的晶体结构
WO2016201566A1 (en) Systems and methods of selecting compounds with reduced risk of cardiotoxicity using herg models
KR101421089B1 (ko) 대장암에 특이적인 항암 활성을 갖는 신규 펩타이드, 이를 포함하는 ｎｄｒｇ２ 결정체 및 이의 용도
WO2009076621A1 (en) High resolution structures of acidic mammalian chitinases and uses thereof
WO2012037150A1 (en) Crystal structures of o-glcnac transferase and uses thereof
US20060134768A1 (en) Erbb4 co-crystal
JP2005137361A (ja) ペプチジルアルギニンデイミナーゼ４又はその変異体タンパク質の結晶、ペプチジルアルギニンデイミナーゼ４変異体タンパク質及びその複合体
CN101142235A (zh) 雌激素受体结构

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Open date: 20071003