WO2004037792A3 - Benzo (f) quinolinone variants as nuclear hormone receptor ligands - Google Patents

Benzo (f) quinolinone variants as nuclear hormone receptor ligands Download PDF

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Publication number
WO2004037792A3
WO2004037792A3 PCT/EP2003/010108 EP0310108W WO2004037792A3 WO 2004037792 A3 WO2004037792 A3 WO 2004037792A3 EP 0310108 W EP0310108 W EP 0310108W WO 2004037792 A3 WO2004037792 A3 WO 2004037792A3
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WO
WIPO (PCT)
Prior art keywords
nuclear hormone
receptor
cancers
disorders
prostate
Prior art date
Application number
PCT/EP2003/010108
Other languages
French (fr)
Other versions
WO2004037792A2 (en
Inventor
Marcus Ruda
David Wensbo
Original Assignee
Karobio Ab
Marcus Ruda
David Wensbo
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 Karobio Ab, Marcus Ruda, David Wensbo filed Critical Karobio Ab
Priority to AU2003293305A priority Critical patent/AU2003293305A1/en
Publication of WO2004037792A2 publication Critical patent/WO2004037792A2/en
Publication of WO2004037792A3 publication Critical patent/WO2004037792A3/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/10—Aza-phenanthrenes

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as nuclear hormone receptor modulators. The compounds of the instant invention are ligands for nuclear hormone receptors and as such may be useful for treatment or prevention of a variety of conditions related to nuclear hormone functioning including proliferative diseases, cancers, benign prostate hyperplasia, adenomas and neoplasisms of the prostate, benign or malignant tumor cells containing the androgen receptor, cardiovascular diseases, angiogenic conditions or disorders, hirsutism, acne, hyperpilosity, inflammation, immune modulation, seborrhea, endometriosis, polycycstic ovary syndrome, androgen alopecia, hypogonadism, osteoporosis, suppressing spermatogenesis, libido, cachexia, anorexia, cancers expressing the estrogen receptor, prostate cancer, breast cancer, endometrial cancer, incontinence, hot flashes, vaginal dryness, menopause, contraception, pregnancy termination, cancers containing the progesterone e receptor, endometriosis, cachexia, menopause fibrosis, labor induction, autoimmune diseases, impairment of cognitive functioning, cerebral degenerative disorders, Alzheimer's disease, psychotic disorders, type-II diabetes, congestive heart failure, disregulation of cholesterol or lipid homeostasis, and/or obesity. A compound having the general formula I or II:
PCT/EP2003/010108 2002-09-27 2003-09-10 Benzo (f) quinolinone variants as nuclear hormone receptor ligands WO2004037792A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003293305A AU2003293305A1 (en) 2002-09-27 2003-09-10 Benzo (f) quinolinone variants as nuclear hormone receptor ligands

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0222516A GB0222516D0 (en) 2002-09-27 2002-09-27 Novel compounds
GB0222516.7 2002-09-27

Publications (2)

Publication Number Publication Date
WO2004037792A2 WO2004037792A2 (en) 2004-05-06
WO2004037792A3 true WO2004037792A3 (en) 2004-09-02

Family

ID=9944918

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2003/010108 WO2004037792A2 (en) 2002-09-27 2003-09-10 Benzo (f) quinolinone variants as nuclear hormone receptor ligands

Country Status (3)

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AU (1) AU2003293305A1 (en)
GB (1) GB0222516D0 (en)
WO (1) WO2004037792A2 (en)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI366565B (en) 2007-06-06 2012-06-21 Otsuka Pharma Co Ltd Quinolone compound and pharmaceutical composition
TWI472525B (en) 2008-12-05 2015-02-11 Otsuka Pharma Co Ltd Quinolone compound and pharmaceutical composition
CA2888210C (en) 2012-10-16 2021-02-09 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of ror-gamma-t
AU2013331505A1 (en) 2012-10-16 2015-04-30 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of ROR-gamma-t
WO2014062655A1 (en) 2012-10-16 2014-04-24 Janssen Pharmaceutica Nv HETEROARYL LINKED QUINOLINYL MODULATORS OF RORyt
US9284308B2 (en) 2013-10-15 2016-03-15 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of RORγt
JP6423423B2 (en) 2013-10-15 2018-11-14 ヤンセン ファーマシューティカ エヌ．ベー． Rorγt alkyl-linked quinolinyl modulator
EP3057422B1 (en) 2013-10-15 2019-05-15 Janssen Pharmaceutica NV Quinolinyl modulators of ror(gamma)t
AU2013403330A1 (en) * 2013-10-15 2016-04-21 Janssen Pharmaceutica Nv Heteroaryl linked quinolinyl modulators of RORYt
US9328095B2 (en) 2013-10-15 2016-05-03 Janssen Pharmaceutica Nv Heteroaryl linked quinolinyl modulators of RORgammat
US10555941B2 (en) 2013-10-15 2020-02-11 Janssen Pharmaceutica Nv Alkyl linked quinolinyl modulators of RORγt
US9403816B2 (en) 2013-10-15 2016-08-02 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of RORγt
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
CN109721536B (en) * 2017-10-27 2020-11-24 广东东阳光药业有限公司 Phenyl-substituted fused tricyclic compounds and application thereof
CN108218770A (en) * 2018-02-28 2018-06-29 南京波普生物医药研发有限公司 The preparation method of the chloro- 7,8- dihydros -6H- quinoline -5- ketone of 2-

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0102046A1 (en) * 1982-08-26 1984-03-07 Schering Corporation Tricyclic lactams, method for making them, pharmaceutical compositions containing them
EP0531026A1 (en) * 1991-08-21 1993-03-10 Eli Lilly And Company Hexahydrobenzo[f]quinolinones as 5-alpha-reductase inhibitors
US5629007A (en) * 1995-03-21 1997-05-13 Eli Lilly And Company Method of preventing prostatic cancer development
US5670514A (en) * 1995-05-10 1997-09-23 Eli Lilly And Company Compositions for inhibiting bone loss
US5670512A (en) * 1991-08-21 1997-09-23 Eli Lilly And Company Benzo F! quinolinones
US5696133A (en) * 1994-12-22 1997-12-09 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0102046A1 (en) * 1982-08-26 1984-03-07 Schering Corporation Tricyclic lactams, method for making them, pharmaceutical compositions containing them
EP0531026A1 (en) * 1991-08-21 1993-03-10 Eli Lilly And Company Hexahydrobenzo[f]quinolinones as 5-alpha-reductase inhibitors
US5670512A (en) * 1991-08-21 1997-09-23 Eli Lilly And Company Benzo F! quinolinones
US5696133A (en) * 1994-12-22 1997-12-09 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
US5629007A (en) * 1995-03-21 1997-05-13 Eli Lilly And Company Method of preventing prostatic cancer development
US5670514A (en) * 1995-05-10 1997-09-23 Eli Lilly And Company Compositions for inhibiting bone loss

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ANTONIO GUARNA ET AL: "Benzo(c)quinolizin-3-ones: A Novel Class of Potent and Selective Nonsteroidal Inhibitors of Human Steroid 5x-Reductase 1", J. MED. CHEM., vol. 43, 2000, pages 3718 - 3735, XP002284578 *

Also Published As

Publication number Publication date
WO2004037792A2 (en) 2004-05-06
AU2003293305A1 (en) 2004-05-13
AU2003293305A8 (en) 2004-05-13
GB0222516D0 (en) 2002-11-06

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