WO2003053368A3 - Chalcone derivatives and their use to treat diseases - Google Patents

Chalcone derivatives and their use to treat diseases Download PDF

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Publication number
WO2003053368A3
WO2003053368A3 PCT/US2002/041336 US0241336W WO03053368A3 WO 2003053368 A3 WO2003053368 A3 WO 2003053368A3 US 0241336 W US0241336 W US 0241336W WO 03053368 A3 WO03053368 A3 WO 03053368A3
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WIPO (PCT)
Prior art keywords
treat diseases
chalcone derivatives
compounds
chalcone
derivatives
Prior art date
Application number
PCT/US2002/041336
Other languages
French (fr)
Other versions
WO2003053368A2 (en
Inventor
Liming Ni
Kimberly J Worsencroft
M David Weingarten
Charles Q Meng
James A Sikorski
Original Assignee
Atherogenics Inc
Liming Ni
Kimberly J Worsencroft
M David Weingarten
Charles Q Meng
James A Sikorski
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.)
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Publication date
Application filed by Atherogenics Inc, Liming Ni, Kimberly J Worsencroft, M David Weingarten, Charles Q Meng, James A Sikorski filed Critical Atherogenics Inc
Priority to CA002470931A priority Critical patent/CA2470931A1/en
Priority to IL16253302A priority patent/IL162533A0/en
Priority to UA20040705876A priority patent/UA81617C2/en
Priority to JP2003554128A priority patent/JP2005516941A/en
Priority to HU0500165A priority patent/HUP0500165A2/en
Priority to EP02796045A priority patent/EP1465854A4/en
Priority to MXPA04005864A priority patent/MXPA04005864A/en
Priority to BR0215240-1A priority patent/BR0215240A/en
Priority to AU2002360763A priority patent/AU2002360763A1/en
Publication of WO2003053368A2 publication Critical patent/WO2003053368A2/en
Publication of WO2003053368A3 publication Critical patent/WO2003053368A3/en

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    • 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
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Abstract

The invention relates to compounds, pharmaceutical compositions and use of compounds of the general formula (I), or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.
PCT/US2002/041336 2001-12-19 2002-12-19 Chalcone derivatives and their use to treat diseases WO2003053368A2 (en)

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CA002470931A CA2470931A1 (en) 2001-12-19 2002-12-19 Chalcone derivatives and their use to treat diseases
IL16253302A IL162533A0 (en) 2001-12-19 2002-12-19 Chalcone derivatives and their use to treat diseases
UA20040705876A UA81617C2 (en) 2001-12-19 2002-12-19 Chalcone derivatives and their use
JP2003554128A JP2005516941A (en) 2001-12-19 2002-12-19 Chalcone derivatives and their use for treating diseases
HU0500165A HUP0500165A2 (en) 2001-12-19 2002-12-19 Chalcone derivatives and their use to treat diseases
EP02796045A EP1465854A4 (en) 2001-12-19 2002-12-19 Chalcone derivatives and their use to treat diseases
MXPA04005864A MXPA04005864A (en) 2001-12-19 2002-12-19 Chalcone derivatives and their use to treat diseases.
BR0215240-1A BR0215240A (en) 2001-12-19 2002-12-19 Calcium derivatives and their use in treating diseases
AU2002360763A AU2002360763A1 (en) 2001-12-19 2002-12-19 Chalcone derivatives and their use to treat diseases

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8940756B2 (en) 2012-06-07 2015-01-27 Deciphera Pharmaceuticals, Llc Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
US9447071B2 (en) 2014-02-07 2016-09-20 Global Blood Therapeutics, Inc. Crystalline polymorphs of the free base of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde

Families Citing this family (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1596240A (en) 2001-12-19 2005-03-16 阿特罗吉尼克斯公司 Chalcone derivatives and their use to treat diseases
EP1988397B8 (en) 2002-12-19 2012-02-15 The Scripps Research Institute Compositions and uses for stabilising transthyretin and inhibiting transthyretin misfolding
AU2003303239A1 (en) * 2002-12-19 2004-07-14 Atherogenics, Inc. Process of making chalcone derivatives
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
US7279576B2 (en) 2002-12-31 2007-10-09 Deciphera Pharmaceuticals, Llc Anti-cancer medicaments
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
WO2004108094A2 (en) * 2003-06-06 2004-12-16 Atherogenics, Inc. Sulfonamide-substituted chalcone derivatives and their use to treat diseases
US7504401B2 (en) 2003-08-29 2009-03-17 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
WO2005112913A1 (en) 2004-05-20 2005-12-01 The Scripps Research Institute Transthyretin stabilization
WO2006004903A2 (en) * 2004-06-28 2006-01-12 Atherogenics, Inc. 1,2-bis-(substituted-phenyl)-2-propen-1-ones and pharmaceutical compositions thereof
US7772271B2 (en) 2004-07-14 2010-08-10 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7868037B2 (en) 2004-07-14 2011-01-11 Ptc Therapeutics, Inc. Methods for treating hepatitis C
WO2006019831A1 (en) 2004-07-14 2006-02-23 Ptc Therapeutics, Inc. Methods for treating hepatitis c
JP2008507518A (en) 2004-07-22 2008-03-13 ピーティーシー セラピューティクス，インコーポレーテッド Thienopyridine for treating hepatitis C
EP1846388A4 (en) 2005-01-25 2011-12-07 Synta Pharmaceuticals Corp Thiophene compounds for inflammation and immune-related uses
JP2006316027A (en) * 2005-05-16 2006-11-24 Mitsui Chemicals Inc 1, 3-dialkyl-2-imidazolidinone and method for purifying the same
CN100336797C (en) * 2005-08-19 2007-09-12 浙江大学 Tetra substituted chalcone derivative and preparing method and use
US20080280891A1 (en) * 2006-06-27 2008-11-13 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
CN101600683B (en) 2006-07-05 2013-06-12 法博太科制药有限公司 Therapeutic compounds
WO2008034016A2 (en) * 2006-09-15 2008-03-20 Foldrx Pharmaceuticals, Inc. Assays for detecting native-state proteins and identifying compounds that modulate the stability of native-state proteins
CN101611016B (en) * 2006-10-17 2012-01-25 斯蒂菲尔实验室公司 Talarazole metabolites
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
SI2091948T1 (en) 2006-11-30 2012-07-31 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
US20100160450A1 (en) * 2007-01-31 2010-06-24 Eric Kuhrts Methods of reducing 15-f2t-isop levels in mammals
EP2481408A3 (en) 2007-03-01 2013-01-09 Probiodrug AG New use of glutaminyl cyclase inhibitors
DK2142514T3 (en) 2007-04-18 2015-03-23 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
WO2009079692A1 (en) * 2007-12-21 2009-07-02 Fibrotech Therapeutics Pty Ltd Halogenated analogues of anti-fibrotic agents
US8993556B2 (en) 2009-04-21 2015-03-31 Nerviano Medical Sciences S.R.L. Resorcinol derivatives as HSP90 inhibitors
WO2011009826A2 (en) 2009-07-21 2011-01-27 ADAMED Sp.z o.o. Novel chalcone derivatives with cytotoxic activity
AU2010294214B2 (en) 2009-09-11 2015-05-07 Vivoryon Therapeutics N.V. Heterocylcic derivatives as inhibitors of glutaminyl cyclase
US9062076B2 (en) 2009-10-22 2015-06-23 Fibrotech Therapeutics Pty Ltd Fused ring analogues of anti-fibrotic agents
US8889874B2 (en) 2010-01-12 2014-11-18 Council Of Scientific And Industrial Research Imidazolone-chalcone derivatives as potential anticancer agent and process for the preparation thereof
JP6026284B2 (en) 2010-03-03 2016-11-16 プロビオドルグ エージー Inhibitors of glutaminyl cyclase
AU2011226074B2 (en) 2010-03-10 2015-01-22 Vivoryon Therapeutics N.V. Heterocyclic inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5)
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
JP6050264B2 (en) 2011-03-16 2016-12-21 プロビオドルグ エージー Benzimidazole derivatives as inhibitors of glutaminyl cyclase
WO2013019978A1 (en) * 2011-08-03 2013-02-07 State Of Oregon Acting By And Through The State Board Of Higher Education On Behalf Of Portland State University Fluorescence detection of cysteine and homocysteine
JP5869677B2 (en) 2011-09-16 2016-02-24 ファイザー・インク Solid form of transthyretin dissociation inhibitor
ES2790358T3 (en) 2011-12-28 2020-10-27 Global Blood Therapeutics Inc Substituted Heteroaryl Aldehyde Compounds and Methods for Their Use in Increasing Tissue Oxygenation
PT3738434T (en) 2011-12-28 2023-11-13 Global Blood Therapeutics Inc Intermediates to obtain substituted benzaldehyde compounds and methods for their use in increasing tissue oxygenation
WO2014086697A1 (en) * 2012-12-06 2014-06-12 F. Hoffmann-La Roche Ag Substituted thiazole compounds
PE20160078A1 (en) 2013-03-15 2016-03-02 Global Blood Therapeutics Inc COMPOUNDS AND THEIR USES TO MODULATE HEMOGLOBIN
US10100043B2 (en) 2013-03-15 2018-10-16 Global Blood Therapeutics, Inc. Substituted aldehyde compounds and methods for their use in increasing tissue oxygenation
US9604999B2 (en) 2013-03-15 2017-03-28 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US20140274961A1 (en) 2013-03-15 2014-09-18 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US8952171B2 (en) 2013-03-15 2015-02-10 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US9422279B2 (en) 2013-03-15 2016-08-23 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
CN105073728A (en) 2013-03-15 2015-11-18 全球血液疗法股份有限公司 Compounds and uses thereof for the modulation of hemoglobin
US9458139B2 (en) 2013-03-15 2016-10-04 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
EA033555B1 (en) 2013-03-15 2019-10-31 Global Blood Therapeutics Inc Pharmaceutical compositions for treating sickle cell disorder
US10266551B2 (en) 2013-03-15 2019-04-23 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
EA201992707A1 (en) 2013-11-18 2020-06-30 Глобал Блад Терапьютикс, Инк. COMPOUNDS AND THEIR APPLICATIONS FOR HEMOGLOBIN MODULATION
CN103755541B (en) * 2014-02-19 2015-09-02 厦门大学 One class chalcone derivative and its production and use
MA41841A (en) 2015-03-30 2018-02-06 Global Blood Therapeutics Inc ALDEHYDE COMPOUNDS FOR THE TREATMENT OF PULMONARY FIBROSIS, HYPOXIA, AND AUTOIMMUNE AND CONNECTIVE TISSUE DISEASES
US11020382B2 (en) 2015-12-04 2021-06-01 Global Blood Therapeutics, Inc. Dosing regimens for 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde
AR108435A1 (en) 2016-05-12 2018-08-22 Global Blood Therapeutics Inc PROCESS TO SYNTHETIZE 2-HYDROXI-6 - ((2- (1-ISOPROPIL-1H-PIRAZOL-5-IL) -PIRIDIN-3-IL) METOXI) BENZALDEHYDE
CN106279082B (en) * 2016-08-02 2019-02-01 浙江大学 Substituted furans chalcone derivative and preparation method thereof
TWI778983B (en) 2016-10-12 2022-10-01 美商全球血液治療公司 Tablets comprising 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde
MX2019009235A (en) 2017-02-03 2019-12-11 Certa Therapeutics Pty Ltd Anti-fibrotic compounds.
PL232667B1 (en) * 2017-07-31 2019-07-31 Univ Przyrodniczy We Wroclawiu 3'-Amino-4-carboxychalcone and method for obtaining 3'-amino-4-carboxychalcone
PL232668B1 (en) * 2017-07-31 2019-07-31 Univ Przyrodniczy We Wroclawiu 2'-Amino-4-carboxychalcone and method for obtaining 2'-amino-4-carboxychalcone
PL3461819T3 (en) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitors of glutaminyl cyclase
CN108440278B (en) * 2018-03-07 2021-01-12 中国计量大学 Dicarboxy chalcone compound and its application in preparing anti-inflammatory medicine
ES2966707T3 (en) 2018-10-01 2024-04-23 Global Blood Therapeutics Inc Hemoglobin modulators for the treatment of sickle cell disease
CN109705017B (en) * 2019-01-22 2022-09-20 中美（河南）荷美尔肿瘤研究院 Application of chalcone indole derivative in preparation of antitumor drugs
CN109651226B (en) * 2019-01-22 2022-06-07 中美（河南）荷美尔肿瘤研究院 Chalcone indole derivative, preparation method and application thereof
MX2022001863A (en) 2019-08-12 2022-05-30 Deciphera Pharmaceuticals Llc Ripretinib for treating gastrointestinal stromal tumors.
TW202122082A (en) 2019-08-12 2021-06-16 美商迪賽孚爾製藥有限公司 Methods of treating gastrointestinal stromal tumors
LT4084778T (en) 2019-12-30 2024-01-25 Deciphera Pharmaceuticals, Llc Amorphous kinase inhibitor formulations and methods of use thereof
IL293864A (en) 2019-12-30 2022-08-01 Deciphera Pharmaceuticals Llc Compositions of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea
CN114105753B (en) * 2021-09-17 2024-02-20 温州医科大学 Fisetin derivative and application thereof in preparation of anti-inflammatory drugs
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6462075B1 (en) * 1999-12-23 2002-10-08 The University Of Georgia Research Foundation, Inc. Chalcone and its analogs as agents for the inhibition of angiogensis and related disease states

Family Cites Families (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE787838R (en) 1971-08-25 1973-02-22 Delalande Sa NEW DERIVATIVES OF CINNAMOYL-5 BENZOFURANNE, THEIR PROCESS FOR PREPARATION AND THEIR USE IN THERAPEUTICS
FR2175634A1 (en) 1972-03-16 1973-10-26 Delalande Sa Carboxymethoxybenzofurans derivs - analgesic antiinflammatory hypotensive activity etc
FR2217001B2 (en) 1973-02-12 1976-03-12 Delalande Sa
JPS5297950A (en) 1976-02-13 1977-08-17 Taisho Pharmaceut Co Ltd Chalconeether derivatives
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
DE3415033C2 (en) * 1983-04-20 1986-04-03 Hitachi Chemical Co., Ltd. 4'-Azidobenzal-2-methoxyacetophenone, process for its preparation and photosensitive composition containing it
JPS6310720A (en) 1986-07-01 1988-01-18 Nippon Kayaku Co Ltd 5-lipoxygenase inhibitor and anti-allergic agent
DE3627673A1 (en) 1986-08-14 1988-02-25 Bayer Ag METHOD FOR PRODUCING OPTICALLY ACTIVE 2-HYDROXYETHYL AZOL DERIVATIVES
US4794205A (en) 1986-12-10 1988-12-27 Hoechst Celanese Corporation Method for producing alkenylthiophenols and their esters
US4904697A (en) 1987-04-09 1990-02-27 Merrell Dow Pharmaceuticals Inc. Controlling the growth of certain tumor tissue with chalcone derivatives
EP0307762A1 (en) 1987-09-16 1989-03-22 F. Hoffmann-La Roche Ag Acrylic-acid amides and their use as fungicides
US5217999A (en) 1987-12-24 1993-06-08 Yissum Research Development Company Of The Hebrew University Of Jerusalem Styryl compounds which inhibit EGF receptor protein tyrosine kinase
KR0139296B1 (en) * 1988-11-21 1998-05-15 가와무라 시게꾸니 Chalcone derivatives and process for producing the same
FR2663633B1 (en) * 1990-06-22 1994-06-17 Adir NEW CHALCONES, THEIR PREPARATION PROCESS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.
US5155250A (en) 1990-07-05 1992-10-13 Merrell Dow Pharmaceuticals Inc. 2,6-di-alkyl-4-silyl-phenols as antiatheroscerotic agents
ZA917369B (en) 1990-09-20 1992-06-24 Merrell Dow Pharma Calcium uptake inhibitors
JPH04217621A (en) 1990-10-01 1992-08-07 Shiseido Co Ltd Cosmetic
US6159988A (en) 1992-01-16 2000-12-12 Hoeschst Aktiengesellschaft Arylcycloalkyl derivatives, their production and their use
JPH0692950A (en) 1992-09-16 1994-04-05 Kanegafuchi Chem Ind Co Ltd Production of epoxy compound
JPH06116206A (en) 1992-10-02 1994-04-26 Morinaga Milk Ind Co Ltd Chalcone derivative and its use
US5807884A (en) 1992-10-30 1998-09-15 Emory University Treatment for atherosclerosis and other cardiovascular and inflammatory diseases
US5380747A (en) 1992-10-30 1995-01-10 Emory University Treatment for atherosclerosis and other cardiovascular and inflammatory diseases
US5783596A (en) 1992-10-30 1998-07-21 Emory University Treatment for atherosclerosis and other cardiovascular and inflammatory diseases
US5631365A (en) 1993-09-21 1997-05-20 Schering Corporation Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
PT1468692E (en) 1993-12-10 2006-09-29 Aventis Inc USE OF 2,6-DIALQUIL-4-SILYPHENOLS FOR THE TREATMENT OF XANTOMA
FR2713635B1 (en) 1993-12-15 1996-01-05 Cird Galderma New bi-aromatic propynyl compounds, pharmaceutical and cosmetic compositions containing them and uses.
JPH07330814A (en) 1994-06-06 1995-12-19 Hitachi Chem Co Ltd Photoinitiator, photosensitive composition, photosensitive material and production of relief pattern
JP3304093B2 (en) 1994-09-13 2002-07-22 モンサント カンパニー Novel benzothiepines with inhibitory activity on ileal bile acid transport and taurocholate absorption
IT1271301B (en) 1994-12-20 1997-05-27 Indena Spa NATURAL AND SYNTHETIC CALCONES AND THEIR ESTERS WITH ANTI-PROLIFERATIVE ACTIVITY IN CANCER OF THE UTERUS, OVARIAN AND BREAST AND FORMULATIONS CONTAINING THEM
DE4446329A1 (en) 1994-12-23 1996-06-27 Basf Ag Salts of aromatic hydroxyl compounds and their use as brighteners
KR960022486A (en) 1994-12-29 1996-07-18 김준웅 New Thiazolidin-4-one Derivatives
DE19500838A1 (en) 1995-01-13 1996-07-18 Basf Ag Process for the preparation of 3,5-diarylpyrazoles
JP3145410B2 (en) 1995-04-13 2001-03-12 大鵬薬品工業株式会社 Novel 4,6-diarylpyrimidine derivatives and salts thereof
US5792787A (en) 1995-06-07 1998-08-11 Emory University Treatment for atherosclerosis and other cardiovascular and inflammatory diseases
AU6966696A (en) 1995-10-05 1997-04-28 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
CN1110494C (en) 1996-03-11 2003-06-04 G·D·瑟尔公司 Novel benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
US5608095A (en) 1996-04-30 1997-03-04 Hoechst Marion Roussel, Inc. Alkyl-4-silyl-phenols and esters thereof as antiatherosclerotic agents
JP3895404B2 (en) 1996-05-17 2007-03-22 興和株式会社 Chalcone derivative and pharmaceutical containing the same
HRP970330B1 (en) 1996-07-08 2004-06-30 Bayer Ag Cycloalkano pyridines
AR008789A1 (en) 1996-07-31 2000-02-23 Bayer Corp PIRIDINES AND SUBSTITUTED BIPHENYLS
DE19648793A1 (en) 1996-11-26 1998-05-28 Basf Ag New benzamides and their application
JP2894445B2 (en) 1997-02-12 1999-05-24 日本たばこ産業株式会社 Compounds effective as CETP activity inhibitors
WO1998040375A2 (en) 1997-03-11 1998-09-17 G.D. Searle & Co. COMBINATION OF ILEAL BILE ACID TRANSPORT INHIBITING BENZOTHIEPINES AND HMG Co-A REDUCTASE INHIBITORS
NZ528906A (en) 1997-05-14 2005-06-24 Atherogenics Inc Compounds and methods for the inhibition of the expression of VCAM-1
US6423740B1 (en) 1997-06-19 2002-07-23 Indena S.P.A. Chalcones having antiproliferative activity
AU7908098A (en) 1997-06-26 1999-01-19 Statens Serum Institut Biologically active 1,3-bis-aromatic-prop-2-en-1-ones, 1,3-bis-aromatic-propan-1-ones, and 1,3-bis-aromatic-prop-2-yn-1-ones
DE19741051A1 (en) 1997-09-18 1999-03-25 Bayer Ag New tetrahydroquinoline derivatives useful in treatment of raised lipid levels and arteriosclerosis
MA24643A1 (en) 1997-09-18 1999-04-01 Bayer Ag SUBSTITUTED TETRAHYDRO-NAPHTHALENES AND SIMILAR COMPOUNDS
DE19741399A1 (en) 1997-09-19 1999-03-25 Bayer Ag New tetrahydroquinoline derivatives useful in treatment of elevated lipid levels and arteriosclerosis
US6197786B1 (en) 1998-09-17 2001-03-06 Pfizer Inc 4-Carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines
GT199900147A (en) 1998-09-17 1999-09-06 1, 2, 3, 4- TETRAHIDROQUINOLINAS 2-SUBSTITUTED 4-AMINO SUBSTITUTED.
US6147089A (en) 1998-09-17 2000-11-14 Pfizer Inc. Annulated 4-carboxyamino-2-methyl-1,2,3,4,-tetrahydroquinolines
US6147090A (en) 1998-09-17 2000-11-14 Pfizer Inc. 4-carboxyamino-2-methyl-1,2,3,4,-tetrahydroquinolines
PT1115693E (en) 1998-09-25 2007-08-02 Monsanto Co Substituted polycyclic aryl and heteroaryl $i(tertiary)-heteroalkylamines useful for inhibiting cholesteryl ester transfer protein activity
JP2002525350A (en) 1998-09-25 2002-08-13 モンサント カンパニー Substituted N-aliphatic-N-aromatic tertiary heteroalkylamines effective for inhibiting cholesterol ester transfer protein activity
BR9916564A (en) 1998-12-23 2002-01-29 Searle Llc Combinations for cardiovascular indications
EP1159264A2 (en) 1999-02-11 2001-12-05 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa
US6677350B1 (en) * 1999-09-22 2004-01-13 Advanced Life Sciences, Inc. Beta-fluoroethyl thiourea compounds and use
HN2000000203A (en) 1999-11-30 2001-06-13 Pfizer Prod Inc PROCEDURE FOR OBTAINING 1,2,3,4-TETRAHYDROQUINOLINS 4-CARBOXYAMIN-2-SUBSTITUTED.
GB0007401D0 (en) * 2000-03-27 2000-05-17 Cancer Res Campaign Tech Substituted chalcones as therapeeutic compounds
WO2001098291A2 (en) 2000-06-20 2001-12-27 Atherogenics, Inc. 1,3-bis-(substituted-phenyl)-2-propen-1-ones and their use to treat vcam-1 mediated disorders
EP1343502A2 (en) 2000-11-17 2003-09-17 Idenix (Cayman) Limited Methods for inhibiting the transmission of hiv using topically applied substituted 6-benzyl-4-oxopyrimidines
ATE356635T1 (en) * 2001-11-15 2007-04-15 Pantarhei Bioscience Bv METHOD FOR PREVENTING OR TREATING BENIGUS GYNECOLOGICAL DISORDERS
US7202247B2 (en) 2001-12-19 2007-04-10 Atherogenics, Inc. 1,3-bis-(substituted-phenyl)-2-propyn-1-ones and their use to treat disorders
CN1596240A (en) 2001-12-19 2005-03-16 阿特罗吉尼克斯公司 Chalcone derivatives and their use to treat diseases
AU2003303239A1 (en) 2002-12-19 2004-07-14 Atherogenics, Inc. Process of making chalcone derivatives

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6462075B1 (en) * 1999-12-23 2002-10-08 The University Of Georgia Research Foundation, Inc. Chalcone and its analogs as agents for the inhibition of angiogensis and related disease states

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8940756B2 (en) 2012-06-07 2015-01-27 Deciphera Pharmaceuticals, Llc Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
US9447071B2 (en) 2014-02-07 2016-09-20 Global Blood Therapeutics, Inc. Crystalline polymorphs of the free base of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde

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