WO2005032481A3 - Quinazoline derivatives as medicaments - Google Patents

Quinazoline derivatives as medicaments Download PDF

Info

Publication number
WO2005032481A3
WO2005032481A3 PCT/US2004/032430 US2004032430W WO2005032481A3 WO 2005032481 A3 WO2005032481 A3 WO 2005032481A3 US 2004032430 W US2004032430 W US 2004032430W WO 2005032481 A3 WO2005032481 A3 WO 2005032481A3
Authority
WO
WIPO (PCT)
Prior art keywords
halide
independently
quinazoline derivatives
halo
alkyl
Prior art date
Application number
PCT/US2004/032430
Other languages
French (fr)
Other versions
WO2005032481A2 (en
Inventor
Sundeep Dugar
Sarvajit Chakravarty
Alison Murphy
Glen Mcenroe
Aurelia Conte
John J Perumattam
Original Assignee
Scios Inc
Sundeep Dugar
Sarvajit Chakravarty
Alison Murphy
Glen Mcenroe
Aurelia Conte
John J Perumattam
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, Sundeep Dugar, Sarvajit Chakravarty, Alison Murphy, Glen Mcenroe, Aurelia Conte, John J Perumattam filed Critical Scios Inc
Publication of WO2005032481A2 publication Critical patent/WO2005032481A2/en
Publication of WO2005032481A3 publication Critical patent/WO2005032481A3/en

Links

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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/06—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
    • C07D475/10—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with an aromatic or hetero-aromatic ring directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Abstract

Quinazoline derivatives have the formula (I) or the pharmaceutically acceptable salts thereof; wherein each of Z5, Z6, Z7 and Z8 is N or CH and wherein one or two Z5, Z6, Z7 and Z8 are N and wherein two adjacent Z positions cannot be N; wherein m and n are each independently 0-3; wherein R1 is independently OH, SH, NH2, OR, SR, NHR, halo or R-halide; wherein two adjacent R1 groups may be joined to form an aliphatic hetero cycle ring of 5-6 members; wherein R2 is independently R, halo, R-halide, OR-halide, NH2, CONH2 or CONHR; wherein R is optionally substituted C1-C12 alkyl, C1-C12 alkenyl, C1-C12 alkynyl, or aryl C1-C12 alkyl, containing 0-4 heteroatoms in place of a carbon in the carbon backbone, where the optional substituents are =O, =N, or OH; and wherein R3 is H or CH3. Such compounds are useful in pharmaceutical compositions and methods of treating conditions characterized by enhanced TGFβ activity.
PCT/US2004/032430 2003-09-30 2004-09-30 Quinazoline derivatives as medicaments WO2005032481A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US50791003P 2003-09-30 2003-09-30
US60/507,910 2003-09-30

Publications (2)

Publication Number Publication Date
WO2005032481A2 WO2005032481A2 (en) 2005-04-14
WO2005032481A3 true WO2005032481A3 (en) 2005-06-16

Family

ID=34421686

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/032430 WO2005032481A2 (en) 2003-09-30 2004-09-30 Quinazoline derivatives as medicaments

Country Status (2)

Country Link
US (2) US7232824B2 (en)
WO (1) WO2005032481A2 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7101165B2 (en) 2016-08-15 2022-07-14 ニューファーマ， インコーポレイテッド Specific chemical entities, compositions, and methods
JP7273723B2 (en) 2016-12-20 2023-05-15 オリゴメリックス インコーポレイテッド Novel quinazolinones that inhibit the formation of tau oligomers and methods of use thereof

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2491943B1 (en) 2003-02-04 2018-10-10 Cornell Research Foundation, Inc. Methods for preventing mitochondrial permeability transition
CA2524258C (en) 2003-05-01 2012-08-07 Cornell Research Foundation, Inc. Carrier complexes comprising cationic peptides for delivering molecules to cells
CA2551524A1 (en) * 2003-12-24 2005-07-21 Scios, Inc. Treatment of malignant gliomas with tgf-beta inhibitors
JP4931604B2 (en) * 2004-01-23 2012-05-16 コーネル リサーチ ファウンデイション インコーポレイテッド Methods for reducing oxidative damage
TW200626157A (en) 2004-09-30 2006-08-01 Tibotec Pharm Ltd HCV inhibiting bi-cyclic pyrimidines
CA2583259C (en) * 2004-10-08 2011-08-02 Astellas Pharma Inc. Aromatic ring fused pyrimidine derivative
MX2007011850A (en) 2005-03-25 2007-10-03 Tibotec Pharm Ltd Heterobicylic inhibitors of hcv.
CN101189234B (en) * 2005-03-25 2011-08-17 泰博特克药品有限公司 Heterobicyclic inhibitors of HCV
AR054122A1 (en) * 2005-05-12 2007-06-06 Tibotec Pharm Ltd PIRIDO [2,3-D] USEFUL PYRIMIDES AS HCV INHIBITORS, AND METHODS FOR THE PREPARATION OF THE SAME
AR056347A1 (en) * 2005-05-12 2007-10-03 Tibotec Pharm Ltd USE OF PTERIDINE COMPOUNDS TO MANUFACTURE PHARMACEUTICAL MEDICINES AND COMPOSITIONS
CA2947335A1 (en) 2005-09-16 2007-03-29 Cornell Research Foundation, Inc. Methods for reducing cd36 expression
AU2014203126B2 (en) * 2005-09-16 2016-03-10 Cornell Research Foundation, Inc. Methods for reducing cd36 expression
WO2007081517A2 (en) 2005-12-21 2007-07-19 Abbott Laboratories Anti-viral compounds
WO2007076034A2 (en) * 2005-12-21 2007-07-05 Abbott Laboratories Anti-viral compounds
ES2647472T3 (en) 2006-10-03 2017-12-21 Genzyme Corporation Antibodies against TGF-BETA for use in the treatment of infants at risk of developing bronchopulmonary dysplasia
EP2094276A4 (en) 2006-12-20 2011-01-05 Abbott Lab Anti-viral compounds
CA2713150C (en) 2008-02-07 2016-01-05 Cornell University Methods for preventing or treating insulin resistance
CN106975070A (en) 2008-02-26 2017-07-25 康奈尔大学 Method for preventing and treating acute injury of kidney
CN103933542A (en) 2009-03-20 2014-07-23 通用医疗公司以马萨诸塞州通用医疗公司名义经营 Methods For The Prevention And Treatment Of Burn Injuries And Secondary Complications
JP5909182B2 (en) * 2009-08-12 2016-04-26 コーネル ユニヴァーシティー Methods for preventing or treating metabolic syndrome
EP3318264A1 (en) 2009-08-24 2018-05-09 Stealth Peptides International, Inc. Methods ans compositions for preventing or treating opthalmic conditions
EP2944317A1 (en) * 2009-10-05 2015-11-18 Cornell University Methods for the prevention or treatment of heart failure
AU2011379972B2 (en) 2011-10-26 2016-05-12 Seattle Children's Research Institute Cysteamine in the treatment of fibrotic disease
HUE043465T2 (en) 2013-08-23 2019-08-28 Neupharma Inc Certain chemical entities, compositions, and methods
PL3089971T3 (en) 2014-01-01 2021-01-25 Medivation Technologies Llc Compounds and methods of use
CN107001358A (en) * 2014-10-29 2017-08-01 东亚St株式会社 Adjust the new pyridine hepyramine compound of istone lysine demethylase (KDM) catalytic activity
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
LT3691620T (en) 2017-10-05 2022-09-26 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce dux4 and downstream gene expression for the treatment of fshd
CN109265457A (en) * 2018-11-01 2019-01-25 中国药科大学 A kind of new method using oxidation aromatisation building pyridopyrimidine dione skeleton
US20220177978A1 (en) 2019-04-02 2022-06-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6476031B1 (en) * 1998-08-28 2002-11-05 Scios, Inc. Quinazoline derivatives as medicaments
WO2003097615A1 (en) * 2002-05-17 2003-11-27 Scios, Inc. TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-β INHIBITORS
WO2004047818A2 (en) * 2002-11-22 2004-06-10 Scios, Inc. USE OF TFG-β INHIBITORSTO COUNTERACT PATHOLOGIC CHANGES IN THE LEVEL OR FUNCTION OF STEROID/THYROID RECEPTORS

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1175875A (en) 1983-02-25 1984-10-09 Office Specialty Division Of Hollanding Inc. Anti-tip blocking device
US5034393A (en) 1989-07-27 1991-07-23 Dowelanco Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives
US5480883A (en) * 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5721237A (en) 1991-05-10 1998-02-24 Rhone-Poulenc Rorer Pharmaceuticals Inc. Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
US5430148A (en) 1992-03-31 1995-07-04 Agouron Pharmaceuticals, Inc. Antiproliferative quinazolines
EP0634169B1 (en) 1993-06-29 2000-01-05 Takeda Chemical Industries, Ltd. Quinoline or quinazoline derivatives and their use in the manufacture of a medicament for the treatment of osteoporosis
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
US5658903A (en) 1995-06-07 1997-08-19 Smithkline Beecham Corporation Imidazole compounds, compositions and use
USH2007H1 (en) 1996-01-19 2001-12-04 Fmc Corporation Insecticidal N-heterocyclylalkyl-or N-[(polycyclyl)alkyl]-N′substituted piperazines
JP2001506230A (en) 1996-08-09 2001-05-15 スミスクライン・ビーチャム・コーポレイション New piperazine-containing compounds
WO1998007425A1 (en) 1996-08-21 1998-02-26 Smithkline Beecham Corporation Imidazole compounds, compositions and use
US6251912B1 (en) 1997-08-01 2001-06-26 American Cyanamid Company Substituted quinazoline derivatives
US6355678B1 (en) 1998-06-29 2002-03-12 Parker Hughes Institute Inhibitors of the EGF-receptor tyrosine kinase and methods for their use

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6476031B1 (en) * 1998-08-28 2002-11-05 Scios, Inc. Quinazoline derivatives as medicaments
WO2003097615A1 (en) * 2002-05-17 2003-11-27 Scios, Inc. TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-β INHIBITORS
WO2004047818A2 (en) * 2002-11-22 2004-06-10 Scios, Inc. USE OF TFG-β INHIBITORSTO COUNTERACT PATHOLOGIC CHANGES IN THE LEVEL OR FUNCTION OF STEROID/THYROID RECEPTORS

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7101165B2 (en) 2016-08-15 2022-07-14 ニューファーマ， インコーポレイテッド Specific chemical entities, compositions, and methods
JP7273723B2 (en) 2016-12-20 2023-05-15 オリゴメリックス インコーポレイテッド Novel quinazolinones that inhibit the formation of tau oligomers and methods of use thereof

Also Published As

Publication number Publication date
WO2005032481A2 (en) 2005-04-14
US7232824B2 (en) 2007-06-19
US20050096333A1 (en) 2005-05-05
US20070293500A1 (en) 2007-12-20

Similar Documents

Publication Publication Date Title
WO2005032481A3 (en) Quinazoline derivatives as medicaments
HK1068334A1 (en) Derivatives of triazolyl-imidazopyridine and of the triazolylpurines useful as ligands of the adenosine a2a receptor and their use as medicaments
EG24928A (en) Heterocyclic inhibitors of mek and methods of use thereof
EA200100486A1 (en) DERIVATIVES 2-UREIDOTHIAOSOL, THE WAY OF THEIR RECEPTION AND APPLICATION OF THE SPECIFIED SUBSTANCES AS ANTI-TUMOR MEDICINE
HUP0400246A2 (en) 1,2,4-trioxolane antimalarial pharmaceutical compositions and process for their preparation and use
MY127066A (en) Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors.
HUP0300743A2 (en) Heteroaryl derivatives and use thereof as medicaments
RU2005137032A (en) USE OF OXAZOLIDINO-QUINOLINE HYBRID ANTIBIOTICS FOR TREATMENT OF SIBERIAN ULCER AND OTHER INFECTIONS
GB0411056D0 (en) Organic compounds
CY1105047T1 (en) PYRIDOPYRIMIDINONE COMPOUNDS, THEIR METHOD OF PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
NZ592766A (en) 1,4-dihydropyridine-fused heterocycles, process for preparing the same, use and compositions containing them
TW200503712A (en) (2-carboxamido)(3-amino)thiophene compounds
WO2005040345A3 (en) 4-azole substituted imidazole compositions useful as inhibitors or c-met receptor tyrosine kinase
MY138051A (en) Compounds and processes
HUP0402602A2 (en) Method for preparing echinocandin derivatives, their use, pharmaceutical compositions comprising thereof and their intermediates
DK0732332T3 (en) Substituted benzothienylpiperazines, their use as drugs and their methods of preparation
EA200300272A1 (en) NEW HINAZOLIN DERIVATIVES, METHOD OF THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
DE602005015223D1 (en) 3 - (((4-PHENYL) -Piperazine-1-YL) -ALKYL) -3-ALKYL-1,3-DIHYDRO-2H-INDOL-2-ON DERIVATIVES AND RELATED COMPOUNDS FOR THE TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM
ZA979328B (en) Process for the preparation of n-[2-(dimethylamino)ethyl[acridine-4-carboxamide
CA2453991A1 (en) New antitumoral derivatives of et-743
IL159792A0 (en) Variolin derivatives and pharmaceutical compositions containing the same
NZ334951A (en) Process for the preparation of n-[2-(dimethylamino)ethyl]acridine-4-carboxamide
NZ505110A (en) Neuroprotective agents
WO2003007935A3 (en) Use of a class of antiviral compounds for production of an agent for the treatment or prevention of a viral infection in the respiratory tract
TH60263A (en) 1,4-diazabycloid derivatives [3.2.2] nonane-phenylisoxazole, such preparations and therapeutic use.

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BW BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE EG ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NA NI NO NZ OM PG PH PL PT RO RU SC SD SE SG SK SL SY TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): BW GH GM KE LS MW MZ NA SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LU MC NL PL PT RO SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DPEN Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed from 20040101)
122 Ep: pct application non-entry in european phase