WO2004010929A3 - METHODS FOR IMPROVEMENT OF LUNG FUNCTION USING TGF-β INHIBITORS - Google Patents

METHODS FOR IMPROVEMENT OF LUNG FUNCTION USING TGF-β INHIBITORS Download PDF

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Publication number
WO2004010929A3
WO2004010929A3 PCT/US2003/023240 US0323240W WO2004010929A3 WO 2004010929 A3 WO2004010929 A3 WO 2004010929A3 US 0323240 W US0323240 W US 0323240W WO 2004010929 A3 WO2004010929 A3 WO 2004010929A3
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WO
WIPO (PCT)
Prior art keywords
tgf
inhibitors
improvement
lung function
methods
Prior art date
Application number
PCT/US2003/023240
Other languages
French (fr)
Other versions
WO2004010929A2 (en
Inventor
Zhihe Li
David Y Liu
Jing Ying Ma
Andrew Protter
George F Schreiner
Thomas-Toan Tran
Original Assignee
Scios Inc
Zhihe Li
David Y Liu
Jing Ying Ma
Andrew Protter
George F Schreiner
Thomas-Toan Tran
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 Scios Inc, Zhihe Li, David Y Liu, Jing Ying Ma, Andrew Protter, George F Schreiner, Thomas-Toan Tran filed Critical Scios Inc
Priority to CA002494367A priority Critical patent/CA2494367A1/en
Priority to EP03771821A priority patent/EP1575506A4/en
Priority to AU2003256783A priority patent/AU2003256783A1/en
Publication of WO2004010929A2 publication Critical patent/WO2004010929A2/en
Publication of WO2004010929A3 publication Critical patent/WO2004010929A3/en

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    • 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
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • 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
    • 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
    • A61K31/495—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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • 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

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

The invention concerns methods for improvement of lung function by administering non-peptide small molecule inhibitors of TGF-β specifically binding to the type I TGF-β receptor (TGFβ-R1). Preferably, the inhibitors are quinazoline derivatives.
PCT/US2003/023240 2002-07-25 2003-07-23 METHODS FOR IMPROVEMENT OF LUNG FUNCTION USING TGF-β INHIBITORS WO2004010929A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CA002494367A CA2494367A1 (en) 2002-07-25 2003-07-23 Methods for improvement of lung function using tgf-.beta. inhibitors
EP03771821A EP1575506A4 (en) 2002-07-25 2003-07-23 Methods for improvement of lung function using tgf-beta inhibitors
AU2003256783A AU2003256783A1 (en) 2002-07-25 2003-07-23 METHODS FOR IMPROVEMENT OF LUNG FUNCTION USING TGF-Beta INHIBITORS

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39936902P 2002-07-25 2002-07-25
US60/399,369 2002-07-25

Publications (2)

Publication Number Publication Date
WO2004010929A2 WO2004010929A2 (en) 2004-02-05
WO2004010929A3 true WO2004010929A3 (en) 2005-12-01

Family

ID=31188573

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/023240 WO2004010929A2 (en) 2002-07-25 2003-07-23 METHODS FOR IMPROVEMENT OF LUNG FUNCTION USING TGF-β INHIBITORS

Country Status (4)

Country Link
EP (1) EP1575506A4 (en)
AU (1) AU2003256783A1 (en)
CA (1) CA2494367A1 (en)
WO (1) WO2004010929A2 (en)

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US20040127575A1 (en) * 2002-11-22 2004-07-01 Feng Ying Method for counteracting a pathologic change in the beta-adrenergic pathway
WO2004081009A1 (en) 2003-03-12 2004-09-23 Millennium Pharmaceuticals, Inc. Quinazoline derivatives as tgf-beta inhibitors
NZ545913A (en) 2003-09-19 2009-01-31 Astrazeneca Ab Quinazoline derivatives
EP1899332A1 (en) 2005-06-24 2008-03-19 Gilead Sciences, Inc. Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for treating hepatitis c.
WO2007050793A2 (en) * 2005-10-25 2007-05-03 The Johns Hopkins University Methods and compositions for the treatment of marfan syndrome and associated disorders
US8338435B2 (en) 2006-07-20 2012-12-25 Gilead Sciences, Inc. Substituted pyrido(3,2-D) pyrimidines and pharmaceutical compositions for treating viral infections
US8642034B2 (en) 2006-10-03 2014-02-04 Genzyme Corporation Use of TGF-β antagonists to treat infants at risk of developing bronchopulmonary dysplasia
WO2008071605A2 (en) * 2006-12-15 2008-06-19 F. Hoffmann-La Roche Ag Methods of treating inflammatory diseases
TW200840584A (en) 2006-12-26 2008-10-16 Gilead Sciences Inc Pyrido(3,2-d)pyrimidines useful for treating viral infections
US8536187B2 (en) 2008-07-03 2013-09-17 Gilead Sciences, Inc. 2,4,6-trisubstituted pyrido(3,2-d)pyrimidines useful for treating viral infections
EP2379076B1 (en) 2008-12-23 2014-11-12 The Trustees of Columbia University in the City of New York Phosphodiesterase inhibitors and uses thereof
SG186855A1 (en) 2010-06-28 2013-02-28 Merck Patent Gmbh 2,4- diaryl - substituted [1,8] naphthyridines as kinase inhibitors for use against cancer
US8609672B2 (en) 2010-08-27 2013-12-17 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
MX2013010163A (en) 2011-03-09 2013-10-30 Merck Patent Gmbh Pyrido [2, 3 - b] pyrazine derivatives and their therapeutical uses.
US20140308275A1 (en) 2011-07-27 2014-10-16 Inserm (Institut National De La Sante Et De La Recherche Medicale Methods for diagnosing and treating myhre syndrome
CA2853484C (en) 2011-10-26 2018-08-21 Seattle Children's Research Institute Cysteamine in the treatment of fibrotic disease
TW201815787A (en) 2016-09-23 2018-05-01 美商基利科學股份有限公司 Phosphatidylinositol 3-kinase inhibitors
TW201825465A (en) 2016-09-23 2018-07-16 美商基利科學股份有限公司 Phosphatidylinositol 3-kinase inhibitors
TW201813963A (en) 2016-09-23 2018-04-16 美商基利科學股份有限公司 Phosphatidylinositol 3-kinase inhibitors
ES2927715T3 (en) 2017-10-05 2022-11-10 Fulcrum Therapeutics Inc p38 kinase inhibitors reduce the expression of dux4 and the genes that follow it for the treatment of FSHD
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
CN108912061B (en) * 2018-06-14 2021-03-19 温州医科大学 Synthetic method of quinazoline inflammation inhibition compound
CN109053597B (en) * 2018-06-14 2021-03-19 温州医科大学附属第二医院、温州医科大学附属育英儿童医院 Inflammation inhibiting compound and preparation method thereof
CN108912059B (en) * 2018-06-14 2021-03-02 温州医科大学附属第一医院 Synthetic method of nitrogenous heterocyclic inflammation inhibiting compound
CN108727283B (en) * 2018-06-14 2021-03-02 温州医科大学附属第一医院 Synthesis method of benzenesulfonyl amide anti-inflammatory compound
CN108912060B (en) * 2018-06-14 2021-03-19 温州医科大学 Quinazoline anti-inflammatory compound and synthesis method thereof
CN108727282B (en) * 2018-06-14 2021-03-02 温州医科大学附属第一医院 Benzene sulfonyl amino-containing anti-inflammatory compound and synthesis method thereof
EP3947737A2 (en) 2019-04-02 2022-02-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
CN112568188B (en) * 2021-02-24 2021-05-25 澎立生物医药技术（上海）有限公司 Method for preparing Brown Norway rat pulmonary fibrosis model

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US6476031B1 (en) * 1998-08-28 2002-11-05 Scios, Inc. Quinazoline derivatives as medicaments
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US20040038856A1 (en) * 2002-05-17 2004-02-26 Sarvajit Chakravarty Treatment of fibroproliferative disorders using TGF-beta inhibitors
US20040127575A1 (en) * 2002-11-22 2004-07-01 Feng Ying Method for counteracting a pathologic change in the beta-adrenergic pathway

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US4366189A (en) * 1979-12-21 1982-12-28 Ciba-Geigy Corporation 4-Heterocyclyl-4'-vinylstilbenes
US6476031B1 (en) * 1998-08-28 2002-11-05 Scios, Inc. Quinazoline derivatives as medicaments
US20030166633A1 (en) * 2000-02-21 2003-09-04 Gaster Laramie Mary Pyridinylimidazoles
US20040038856A1 (en) * 2002-05-17 2004-02-26 Sarvajit Chakravarty Treatment of fibroproliferative disorders using TGF-beta inhibitors
US20040127575A1 (en) * 2002-11-22 2004-07-01 Feng Ying Method for counteracting a pathologic change in the beta-adrenergic pathway

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See also references of EP1575506A4 *

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Publication number Publication date
AU2003256783A1 (en) 2004-02-16
WO2004010929A2 (en) 2004-02-05
CA2494367A1 (en) 2004-02-05
EP1575506A2 (en) 2005-09-21
EP1575506A4 (en) 2008-04-23

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