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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
Authority
WO
WIPO (PCT)
Prior art keywords
tgf
inhibitors
improvement
lung function
methods
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.)
Ceased
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
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.)
Scios LLC
Original Assignee
Scios LLC
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 LLC filed Critical Scios LLC
Priority to AU2003256783A priority Critical patent/AU2003256783A1/en
Priority to CA002494367A priority patent/CA2494367A1/en
Priority to EP03771821A priority patent/EP1575506A4/en
Publication of WO2004010929A2 publication Critical patent/WO2004010929A2/en
Anticipated expiration legal-status Critical
Publication of WO2004010929A3 publication Critical patent/WO2004010929A3/en
Ceased legal-status Critical Current

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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 Ceased WO2004010929A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
AU2003256783A AU2003256783A1 (en) 2002-07-25 2003-07-23 METHODS FOR IMPROVEMENT OF LUNG FUNCTION USING TGF-Beta INHIBITORS
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

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 Ceased 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)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10214519B2 (en) 2016-09-23 2019-02-26 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
US10227350B2 (en) 2016-09-23 2019-03-12 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
US10479770B2 (en) 2016-09-23 2019-11-19 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors

Families Citing this family (27)

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CA2506978A1 (en) * 2002-11-22 2004-06-10 Scios, Inc. Method for counteracting a pathologic change in the b-adrenergic pathway
ATE398125T1 (en) 2003-03-12 2008-07-15 Millennium Pharm Inc QUINAZOLINE DERIVATIVES AS TGF BETA INHIBITORS
DE602004004553T2 (en) 2003-09-19 2007-10-25 Astrazeneca Ab quinazoline derivatives
US8232278B2 (en) 2005-06-24 2012-07-31 Gilead Sciences, Inc. Pyrido(3,2-D)pyrimidines and pharmaceutical compositions useful for treating hepatitis C
JP5602365B2 (en) * 2005-10-25 2014-10-08 ザ・ジョンズ・ホプキンス・ユニバーシティ Methods and compositions for treating Marfan syndrome and related diseases.
US8338435B2 (en) 2006-07-20 2012-12-25 Gilead Sciences, Inc. Substituted pyrido(3,2-D) pyrimidines and pharmaceutical compositions for treating viral infections
HUE035575T2 (en) 2006-10-03 2018-05-28 Genzyme Corp Use of TGF beta 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
WO2010002998A1 (en) 2008-07-03 2010-01-07 Gilead Sciences, Inc. 2,4,6-TRISUBSTITUTED PYRIDO (3,2-d) PYRIMIDINES USEFUL FOR TREATING VIRAL INFECTIONS
JP2012513464A (en) 2008-12-23 2012-06-14 ザ トラスティーズ オブ コロンビア ユニヴァーシティ イン ザ シティ オブ ニューヨーク Phosphodiesterase inhibitors and uses thereof
EA201300052A1 (en) 2010-06-28 2013-06-28 Мерк Патент Гмбх [1,8] NAPHTHYRID DERIVATIVES
US8609672B2 (en) 2010-08-27 2013-12-17 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
KR20140022829A (en) 2011-03-09 2014-02-25 메르크 파텐트 게엠베하 Pyrido [2, 3 - b] pyrazine derivatives and their therapeutical uses
EP2737083A1 (en) 2011-07-27 2014-06-04 INSERM (Institut National de la Santé et de la Recherche Scientifique) Methods for diagnosing and treating myhre syndrome
BR112014009789A2 (en) 2011-10-26 2017-04-25 Seattle Children's Res Inst cysteamine in the treatment of fibrotic disease
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
RS63581B1 (en) 2017-10-05 2022-10-31 Fulcrum Therapeutics Inc P38 KINASE INHIBITORS REDUCE THE EXPRESSION OF DUX4 AND DOWNSTREAM GENES TO TREAT FSHD
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
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
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
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
WO2020201362A2 (en) 2019-04-02 2020-10-08 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
IL306100A (en) 2021-04-13 2023-11-01 Nuvalent Inc Amino-substituted heterocycles for treating cancers with egfr mutations

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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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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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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10214519B2 (en) 2016-09-23 2019-02-26 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
US10227350B2 (en) 2016-09-23 2019-03-12 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
US10479770B2 (en) 2016-09-23 2019-11-19 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors

Also Published As

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

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