WO2000066590A3 - Tetracyclic progesterone receptor modulator compounds and methods - Google Patents

Tetracyclic progesterone receptor modulator compounds and methods Download PDF

Info

Publication number
WO2000066590A3
WO2000066590A3 PCT/US2000/011750 US0011750W WO0066590A3 WO 2000066590 A3 WO2000066590 A3 WO 2000066590A3 US 0011750 W US0011750 W US 0011750W WO 0066590 A3 WO0066590 A3 WO 0066590A3
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
progesterone receptor
methods
receptor modulator
tetracyclic
Prior art date
Application number
PCT/US2000/011750
Other languages
French (fr)
Other versions
WO2000066590A2 (en
Inventor
Lin Zhi
Todd K Jones
Keith B Marschke
Christopher M Tegley
Andrew Fensome
Puwen Zhang
Jay E Wrobel
James P Edwards
Original Assignee
Ligand Pharm Inc
American Home Prod
Lin Zhi
Todd K Jones
Keith B Marschke
Christopher M Tegley
Andrew Fensome
Puwen Zhang
Jay E Wrobel
James P Edwards
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
Priority claimed from US09/552,353 external-priority patent/US6358947B1/en
Application filed by Ligand Pharm Inc, American Home Prod, Lin Zhi, Todd K Jones, Keith B Marschke, Christopher M Tegley, Andrew Fensome, Puwen Zhang, Jay E Wrobel, James P Edwards filed Critical Ligand Pharm Inc
Priority to JP2000615620A priority Critical patent/JP2002543204A/en
Priority to AU45018/00A priority patent/AU4501800A/en
Priority to EP00926495A priority patent/EP1175422A2/en
Priority to CA002371273A priority patent/CA2371273A1/en
Priority to MXPA01011294A priority patent/MXPA01011294A/en
Publication of WO2000066590A2 publication Critical patent/WO2000066590A2/en
Publication of WO2000066590A3 publication Critical patent/WO2000066590A3/en
Priority to HK02104861.6A priority patent/HK1043788A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32Antioestrogens

Abstract

Nonsteroidal compounds that are high affinity, high selectivity modulators for progesterone receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring progesterone receptor agonist, partial agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the progesterone receptor modulator compounds.
PCT/US2000/011750 1999-05-04 2000-05-01 Tetracyclic progesterone receptor modulator compounds and methods WO2000066590A2 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
JP2000615620A JP2002543204A (en) 1999-05-04 2000-05-01 Tetracyclic progesterone receptor modulatory compounds and methods
AU45018/00A AU4501800A (en) 1999-05-04 2000-05-01 Tetracyclic progesterone receptor modulator compounds and methods
EP00926495A EP1175422A2 (en) 1999-05-04 2000-05-01 Tetracyclic progesterone receptor modulator compounds and methods
CA002371273A CA2371273A1 (en) 1999-05-04 2000-05-01 Tetracyclic progesterone receptor modulator compounds and methods
MXPA01011294A MXPA01011294A (en) 1999-05-04 2000-05-01 Tetracyclic progesterone receptor modulator compounds and methods.
HK02104861.6A HK1043788A1 (en) 1999-05-04 2002-06-28 Tetracyclic progesterone receptor modulator compounds and methods

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US30461499A 1999-05-04 1999-05-04
US09/552,353 2000-04-19
US09/552,353 US6358947B1 (en) 1999-05-04 2000-04-19 Tetracyclic progesterone receptor modulator compounds and methods
US60/183,044 2000-04-19

Publications (2)

Publication Number Publication Date
WO2000066590A2 WO2000066590A2 (en) 2000-11-09
WO2000066590A3 true WO2000066590A3 (en) 2001-02-08

Family

ID=26974128

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/011750 WO2000066590A2 (en) 1999-05-04 2000-05-01 Tetracyclic progesterone receptor modulator compounds and methods

Country Status (6)

Country Link
EP (1) EP1175422A2 (en)
CN (1) CN1353717A (en)
AU (1) AU4501800A (en)
CA (1) CA2371273A1 (en)
HK (1) HK1043788A1 (en)
WO (1) WO2000066590A2 (en)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2295050T3 (en) * 1999-08-31 2008-04-16 Bayer Schering Pharma Aktiengesellschaft MESOPROGESTINES FOR THE TREATMENT AND PREVENTION OF BENEFIT DEPENDENT GYNECOLOGICAL DISORDERS OF HORMONES.
CN1384748A (en) * 1999-08-31 2002-12-11 耶拿制药两合公司 Mesoprogestins (progesterone receptor modulators) as component of female contraceptives
US8193252B1 (en) 1999-08-31 2012-06-05 Bayer Pharma AG Mesoprogestins (progesterone receptor modulators) for the treatment and prevention of benign hormone dependent gynecological disorders
HK1055058A2 (en) 2002-10-11 2003-12-05 Ligand Pharm Inc 5-CYCLOALKENYL 5H-CHROMENO[3,4-f]QUINOLINE DERIVATIVES AS SELECTIVE PROGESTERONE RECEPTOR MODULATOR COMPOUNDS
AR040783A1 (en) 2002-10-11 2005-04-20 Ligand Pharm Inc 5- (1 ', 1'-CYCLOAQUIL / ALQUENIL) METHYLIDEN-1,2-DIHYDRO-5-H-CHROMENE [3,4- F] CHIINOLINES AS SELECTING MODULATING COMPOUNDS OF PROGESTERONE RECEPTORS
GB0316290D0 (en) 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
US8519158B2 (en) 2004-03-12 2013-08-27 Ligand Pharmaceuticals Incorporated Androgen receptor modulator compounds and methods
PE20060272A1 (en) 2004-05-24 2006-05-22 Glaxo Group Ltd (2R, 3R, 4S, 5R, 2'R, 3'R, 4'S, 5'S) -2.2 '- {TRANS-1,4-CYCLOHEXANODIYLBIS- [IMINO (2 - {[2- (1-METHYL- 1H-IMIDAZOL-4-IL) ETHYL] AMINO} -9H-PURIN-6,9-DIYL)]} BIS [5- (2-ETHYL-2H-TETRAZOLE-5-IL) TETRAHYDRO-3,4-FURANODIOL] AS AN A2A AGONIST
TWI307630B (en) 2004-07-01 2009-03-21 Glaxo Group Ltd Immunoglobulins
EP1841780B1 (en) 2005-01-10 2011-07-27 Glaxo Group Limited Androstane 17-alpha-carbonate derivatives for use in the treatment of allergic and inflammatory conditions
PE20100741A1 (en) 2005-03-25 2010-11-25 Glaxo Group Ltd COMPOUNDS DERIVED FROM 3,4-DIHYDROPYRIMIDE [4,5-d] PYRIMIDIN-2 (1H) -ONE AS KINASE INHIBITORS p38
TWI389690B (en) 2005-03-25 2013-03-21 Glaxo Group Ltd Novel compounds
DE102005030294A1 (en) * 2005-06-24 2007-01-04 Schering Ag Nonsteroidal progesterone receptor modulators
GB0514809D0 (en) 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
TW200730498A (en) 2005-12-20 2007-08-16 Glaxo Group Ltd Compounds
US7943651B2 (en) 2006-04-20 2011-05-17 Glaxo Group Limited Compounds
GB0611587D0 (en) 2006-06-12 2006-07-19 Glaxo Group Ltd Novel compounds
MX2010012814A (en) 2008-05-23 2010-12-20 Amira Pharmaceuticals Inc 5-lipoxygenase-activating protein inhibitor.
ES2383246T3 (en) 2008-06-05 2012-06-19 Glaxo Group Limited 4-amino-indazoles
ES2566339T3 (en) 2008-06-05 2016-04-12 Glaxo Group Limited 4-Carboxamide indazole derivatives useful as PI3-kinase inhibitors
WO2010094643A1 (en) 2009-02-17 2010-08-26 Glaxo Group Limited Quinoline derivatives and their uses for rhinitis and urticaria
WO2010102958A1 (en) 2009-03-09 2010-09-16 Glaxo Group Limited 4-oxadiazol-2 -yl- indazoles as inhibitors of p13 kinases
EP2406249A1 (en) 2009-03-10 2012-01-18 Glaxo Group Limited Indole derivatives as ikk2 inhibitors
WO2010106016A1 (en) 2009-03-17 2010-09-23 Glaxo Group Limited Pyrimidine derivatives used as itk inhibitors
EP2408458A1 (en) 2009-03-19 2012-01-25 Merck Sharp&Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF SIGNAL TRANSDUCER AND ACTIVATOR OF TRANSCRIPTION 6 (STAT6) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
EP2408915A2 (en) 2009-03-19 2012-01-25 Merck Sharp&Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GATA BINDING PROTEIN 3 (GATA3) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
MX2011009724A (en) 2009-03-19 2011-10-14 Merck Sharp & Dohme RNA INTERFERENCE MEDIATED INHIBITION OF BTB AND CNC HOMOLOGY 1, BASIC LEUCINE ZIPPER TRANSCRIPTION FACTOR 1 (BACH 1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) SEQUENCE LISTING.
EP2408916A2 (en) 2009-03-19 2012-01-25 Merck Sharp&Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF CONNECTIVE TISSUE GROWTH FACTOR (CTGF) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
WO2010111464A1 (en) 2009-03-27 2010-09-30 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF APOPTOSIS SIGNAL-REGULATING KINASE 1 (ASK1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
EP2411520A2 (en) 2009-03-27 2012-02-01 Merck Sharp&Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF THE THYMIC STROMAL LYMPHOPOIETIN (TSLP) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
US20120004281A1 (en) 2009-03-27 2012-01-05 Merck Sharp & Dohme Corp RNA Interference Mediated Inhibition of the Nerve Growth Factor Beta Chain (NGFB) Gene Expression Using Short Interfering Nucleic Acid (siNA)
WO2010111471A2 (en) 2009-03-27 2010-09-30 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF SIGNAL TRANSDUCER AND ACTIVATOR OF TRANSCRIPTION 1 (STAT1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
US20100273744A1 (en) 2009-04-24 2010-10-28 Paul Martin Gore Compounds
WO2010122088A1 (en) 2009-04-24 2010-10-28 Glaxo Group Limited Pyrazole and triazole carboxamides as crac channel inhibitors
BRPI1016219B8 (en) 2009-04-30 2021-05-25 Glaxo Group Ltd indazole compound substituted with oxazole, and pharmaceutical composition
WO2011067364A1 (en) 2009-12-03 2011-06-09 Glaxo Group Limited Novel compounds
WO2011067366A1 (en) 2009-12-03 2011-06-09 Glaxo Group Limited Indazole derivatives as pi 3 - kinase inhibitors
JP2013512879A (en) 2009-12-03 2013-04-18 グラクソ グループ リミテッド Benzpyrazole derivatives as inhibitors of PI3 kinase
EP2512438B1 (en) 2009-12-16 2017-01-25 3M Innovative Properties Company Formulations and methods for controlling mdi particle size delivery
WO2011110575A1 (en) 2010-03-11 2011-09-15 Glaxo Group Limited Derivatives of 2-[2-(benzo- or pyrido-) thiazolylamino]-6-aminopyridine, useful in the treatment of respiratoric, allergic or inflammatory diseases
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
ES2602972T3 (en) 2010-09-08 2017-02-23 Glaxosmithkline Intellectual Property Development Limited Indazole derivatives for use in the treatment of influenza virus infection
PL2614058T3 (en) 2010-09-08 2015-12-31 Glaxosmithkline Ip Dev Ltd POLYMORPHS AND SALTS OF N-[5-[4-(5-{[(2R,6S)-2,6-DIMETHYL-4-MORPHOLINYL]METHYL}-& xA;1,3-OXAZOL-2-YL)-1H-INDAZOL-6-YL]-2-(METHYLOXY)-3-PYRIDINYL]METHANESULFONAMIDE
WO2012035055A1 (en) 2010-09-17 2012-03-22 Glaxo Group Limited Novel compounds
WO2012052459A1 (en) 2010-10-21 2012-04-26 Glaxo Group Limited Pyrazole compounds acting against allergic, inflammatory and immune disorders
ES2532213T3 (en) 2010-10-21 2015-03-25 Glaxo Group Limited Pyrazole compounds that act against allergic, immune and inflammatory conditions
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
GB201104153D0 (en) 2011-03-11 2011-04-27 Glaxo Group Ltd Novel compounds
EP2683716A1 (en) 2011-03-11 2014-01-15 Glaxo Group Limited Pyrido[3,4-b]pyrazine derivatives as syk inhibitors
KR20160060100A (en) 2013-09-22 2016-05-27 칼리토르 사이언시즈, 엘엘씨 Substituted aminopyrimidine compounds and methods of use
KR20160062178A (en) 2013-10-17 2016-06-01 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 Pi3k inhibitor for treatment of respiratory disease
WO2015055690A1 (en) 2013-10-17 2015-04-23 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
EP3122730B1 (en) 2014-03-28 2020-03-25 Calitor Sciences, LLC Substituted heteroaryl compounds and methods of use
WO2015173701A2 (en) 2014-05-12 2015-11-19 Glaxosmithkline Intellectual Property (No. 2) Limited Pharmaceutical compositions for treating infectious diseases
EP3347097B1 (en) 2015-09-11 2021-02-24 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine derivatives as modulators of the kinases jak, flt3 and aurora
GB201602527D0 (en) 2016-02-12 2016-03-30 Glaxosmithkline Ip Dev Ltd Chemical compounds
JP2019524792A (en) 2016-08-08 2019-09-05 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited Compound
GB201706102D0 (en) 2017-04-18 2017-05-31 Glaxosmithkline Ip Dev Ltd Chemical compounds
GB201712081D0 (en) 2017-07-27 2017-09-13 Glaxosmithkline Ip Dev Ltd Chemical compounds
WO2019099311A1 (en) 2017-11-19 2019-05-23 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
EP4125919A1 (en) 2020-03-26 2023-02-08 GlaxoSmithKline Intellectual Property Development Limited Cathepsin inhibitors for preventing or treating viral infections

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996019458A2 (en) * 1994-12-22 1996-06-27 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
US5688808A (en) * 1994-12-22 1997-11-18 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996019458A2 (en) * 1994-12-22 1996-06-27 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
US5688808A (en) * 1994-12-22 1997-11-18 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
US5693646A (en) * 1994-12-22 1997-12-02 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
US5693647A (en) * 1994-12-22 1997-12-02 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods

Also Published As

Publication number Publication date
CN1353717A (en) 2002-06-12
WO2000066590A2 (en) 2000-11-09
HK1043788A1 (en) 2002-09-27
EP1175422A2 (en) 2002-01-30
CA2371273A1 (en) 2000-11-09
AU4501800A (en) 2000-11-17

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