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

双环杂芳基pde4b抑制剂 Download PDF

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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
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China
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optionally substituted
compound
pde4b
replaces
alkynyl
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CNA200580036980XA
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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
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Plexxikon Inc
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Plexxikon Inc
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    • 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
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    • 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
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    • C07—ORGANIC CHEMISTRY
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    • 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
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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

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CNA200580036980XA Pending CN101048407A (zh) 2004-09-03 2005-09-02 双环杂芳基pde4b抑制剂

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

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 (72)

* 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
DE602005016952D1 (de) 2004-10-21 2009-11-12 Novo Nordisk As Wählmechanismus für einen drehstift
US8921376B2 (en) * 2005-05-20 2014-12-30 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
MX2008000097A (es) 2005-06-24 2008-03-19 Bayer Bioscience Nv Metodos para alterar la reactividad de las paredes de las celulas vegetales.
DE102006012617A1 (de) * 2006-03-20 2007-09-27 Merck Patent Gmbh 4-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate
AU2007253481B2 (en) 2006-05-18 2013-01-17 Novo Nordisk A/S An injection device with mode locking means
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
BRPI0814423B1 (pt) 2007-07-17 2022-04-19 Plexxikon, Inc Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos
US8119658B2 (en) 2007-10-01 2012-02-21 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
US8877816B2 (en) * 2007-11-21 2014-11-04 Decode Genetics Ehf 4-(or 5-) substituted catechol derivatives
BRPI0821648A2 (pt) 2007-12-20 2015-06-16 Astrazeneca Ab Método e dispositivo para pó desagregante
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
AU2010266754B2 (en) 2009-07-01 2013-12-05 Astrazeneca Ab Dispenser and method for entraining powder in an airflow
MX2012005827A (es) 2009-11-18 2012-06-19 Plexxikon Inc Compuestos y metodos para la modulacion de cinasas, e indicaciones para ello.
WO2011073662A1 (en) 2009-12-17 2011-06-23 Astrazeneca Ab Combination of a benzoxazinone and a further agent for treating respiratory diseases
WO2011079133A2 (en) 2009-12-23 2011-06-30 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
JP2013519413A (ja) 2010-02-10 2013-05-30 アストラゼネカ・ユーケイ・リミテッド 充填された吸入器用キャニスターを提供する方法
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 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
JP2013534539A (ja) 2010-07-15 2013-09-05 ブリストル−マイヤーズ スクイブ カンパニー アザインダゾール化合物
EP2595683B1 (en) 2010-07-21 2015-03-04 AstraZeneca AB Inhaler
EP2595684B1 (en) 2010-07-21 2015-03-04 AstraZeneca AB Inhaler
CN103517710B (zh) 2011-02-07 2017-05-31 普莱希科公司 用于激酶调节的化合物
SG194847A1 (en) 2011-05-17 2013-12-30 Plexxikon Inc Kinase modulation and indications therefor
WO2013012649A1 (en) 2011-07-15 2013-01-24 Glaxosmithkline Llc Azaindole compounds and methods for treating hiv
GB201115874D0 (en) 2011-09-14 2011-10-26 Astrazeneca Ab Inhaler
JP6069351B2 (ja) 2011-12-29 2017-02-01 ノボ・ノルデイスク・エー／エス ダイアルアップ／ダイアルダウン投与機構を有するねじりバネ式ねじ巻き自動注射器
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
HK1207573A1 (en) 2012-04-10 2016-02-05 Georgia State University Research Foundation, Inc. Compositions and methods for treating otitis media and other conditions with inhibitors of cyld
WO2014026327A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof
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
CN104981247A (zh) 2012-09-06 2015-10-14 普莱希科公司 用于激酶调节的化合物和方法及其适应症
US9676748B2 (en) 2012-12-21 2017-06-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
MD20150071A2 (ro) 2013-02-19 2016-02-29 Pfizer Inc. Compuşi azabenzimidazolici ca inhibitori ai PDE4 izoenzimelor pentru tratamentul tulburărilor SNC şi altor afecţiuni
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
RU2015149937A (ru) 2013-05-30 2017-07-06 Плексксикон Инк. Соединения для модулирования киназы и показания к их применению
WO2015134536A1 (en) 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US10131669B2 (en) 2014-07-24 2018-11-20 Pfizer Inc. Pyrazolopyrimidine compounds
HUE044040T2 (hu) 2014-08-06 2019-09-30 Pfizer Imidazopiridazin vegyületek
ES2774177T3 (es) 2014-09-15 2020-07-17 Plexxikon Inc Compuestos heterocíclicos y usos de estos
JP2018510135A (ja) 2015-02-11 2018-04-12 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． ＲＯＲγＴ阻害剤としての置換ピラゾール化合物及びその使用
WO2016164641A1 (en) * 2015-04-08 2016-10-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
EP3581573B1 (en) 2015-05-06 2022-07-06 Plexxikon Inc. Synthesis of a compound that modulates kinases
SG10201912355TA (en) 2015-05-06 2020-02-27 Plexxikon Inc Solid forms of a compound modulating kinases
WO2017019804A2 (en) 2015-07-28 2017-02-02 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CN108137585B (zh) 2015-09-21 2021-10-22 普莱希科公司 杂环化合物及其应用
AU2016344115A1 (en) 2015-10-27 2018-05-10 Merck Sharp & Dohme Corp. Substituted indazole compounds as rorgammat inhibitors and uses thereof
EP3368535B1 (en) 2015-10-27 2020-12-02 Merck Sharp & Dohme Corp. Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof
JP2018531957A (ja) 2015-10-27 2018-11-01 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． ＲＯＲγＴ阻害薬としての置換二環式ピラゾール化合物及びその使用
SG11201804711RA (en) 2015-12-07 2018-07-30 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
AU2017232610B2 (en) 2016-03-16 2021-07-22 Plexxikon Inc. Compounds and methods for kinase modulation and indications therefore
CN109311858B (zh) 2016-05-26 2021-12-03 里科瑞尔姆Ip控股有限责任公司 Egfr抑制剂化合物
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
WO2018136202A2 (en) 2016-12-23 2018-07-26 Plexxikon Inc. Compounds and methods for cdk8 modulation and indications therefor
WO2018175311A1 (en) 2017-03-20 2018-09-27 Plexxikon Inc. Crystalline forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1h- pyrrolo[3,2-b]pyridin-3-yl)benzoic acid that inhibits bromodomain
WO2018226846A1 (en) 2017-06-07 2018-12-13 Plexxikon Inc. Compounds and methods for kinase modulation
CA3070505C (en) 2017-07-25 2023-09-26 Plexxikon Inc. Formulations of a compound modulating kinases
EP3694855A1 (en) 2017-10-13 2020-08-19 Plexxikon Inc. Solid forms of a compound for modulating kinases
CN112165958A (zh) 2017-10-27 2021-01-01 普莱希科公司 调制激酶的化合物的制剂
EP3768666A1 (en) 2018-03-20 2021-01-27 Plexxikon Inc. Compounds and methods for ido and tdo modulation, and indications therefor
TW202104221A (zh) 2019-04-09 2021-02-01 美商普雷辛肯公司 用於ep300或cbp調節及其適應症之化合物及方法
AU2021261383A1 (en) 2020-04-23 2022-11-17 Opna Bio SA Compounds and methods for CD73 modulation and indications therefor
CN115605460A (zh) 2020-04-29 2023-01-13 普莱希科公司（Us） 杂环化合物的合成
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
US5527681A (en) * 1989-06-07 1996-06-18 Affymax Technologies N.V. Immobilized molecular synthesis of systematically substituted compounds
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
US5800992A (en) * 1989-06-07 1998-09-01 Fodor; Stephen P.A. Method of detecting nucleic acids
US5744101A (en) * 1989-06-07 1998-04-28 Affymax Technologies N.V. Photolabile nucleoside protecting groups
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
WO1993002556A1 (en) * 1991-07-26 1993-02-18 University Of Rochester 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
AU686186B2 (en) * 1993-05-27 1998-02-05 Aventisub Ii Inc. Topologically segregated, encoded solid phase libraries
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
CN1254335A (zh) 1997-04-04 2000-05-24 辉瑞产品公司 烟酰胺衍生物
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
JP2001514906A (ja) 1997-08-15 2001-09-18 ハイセック，インコーポレーテッド 核酸種を検出または定量するための方法および組成物
CN100367023C (zh) * 1997-09-11 2008-02-06 生物风险公司 制备高密度阵列的方法
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
CN1158269C (zh) 1997-10-27 2004-07-21 阿古龙制药公司 作为cdk抑制剂的取代的4-氨基-噻唑-2-基化合物
WO1999051773A1 (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
EP1085846A2 (en) * 1998-06-08 2001-03-28 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
US6849644B2 (en) * 2000-11-21 2005-02-01 Smithkline Beecham P.L.C. 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
PL365443A1 (en) * 2001-01-31 2005-01-10 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

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