DE69728893D1 - N-aryl substituierte tetrahydrochinoline ligande für retinoidrezeptoren mit agonist, antagonist oder inverser agonist wirkung - Google Patents

N-aryl substituierte tetrahydrochinoline ligande für retinoidrezeptoren mit agonist, antagonist oder inverser agonist wirkung

Info

Publication number
DE69728893D1
DE69728893D1 DE69728893T DE69728893T DE69728893D1 DE 69728893 D1 DE69728893 D1 DE 69728893D1 DE 69728893 T DE69728893 T DE 69728893T DE 69728893 T DE69728893 T DE 69728893T DE 69728893 D1 DE69728893 D1 DE 69728893D1
Authority
DE
Germany
Prior art keywords
agonist
antagonist
aryl substituted
retinoid receptors
substituted tetrahydroquinoline
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.)
Expired - Fee Related
Application number
DE69728893T
Other languages
English (en)
Other versions
DE69728893T2 (de
Inventor
L Beard
Min Teng
F Colon
T Duong
A Chandraratna
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.)
Allergan Inc
Original Assignee
Allergan Inc
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 Allergan Inc filed Critical Allergan Inc
Publication of DE69728893D1 publication Critical patent/DE69728893D1/de
Application granted granted Critical
Publication of DE69728893T2 publication Critical patent/DE69728893T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/06—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms having only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/18—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
DE69728893T 1996-11-05 1997-10-29 N-aryl substituierte tetrahydrochinoline ligande für retinoidrezeptoren mit agonist, antagonist oder inverser agonist wirkung Expired - Fee Related DE69728893T2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/744,210 US5739338A (en) 1996-11-05 1996-11-05 N-aryl substituted tetrahydroquinolines having retinoid agonist, retinoid antagonist or retinoid inverse agonist type biological activity
PCT/US1997/019915 WO1998019999A1 (en) 1996-11-05 1997-10-29 N-aryl substituted tetrahydroquinolines ligands for retinoid receptors having agonist, antagonist or inverse agonist type activity

Publications (2)

Publication Number Publication Date
DE69728893D1 true DE69728893D1 (de) 2004-06-03
DE69728893T2 DE69728893T2 (de) 2005-04-21

Family

ID=24991892

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69728893T Expired - Fee Related DE69728893T2 (de) 1996-11-05 1997-10-29 N-aryl substituierte tetrahydrochinoline ligande für retinoidrezeptoren mit agonist, antagonist oder inverser agonist wirkung

Country Status (9)

Country Link
US (1) US5739338A (de)
EP (1) EP0937045B1 (de)
JP (1) JP2001504458A (de)
AT (1) ATE265436T1 (de)
AU (1) AU729997B2 (de)
CA (1) CA2270893C (de)
DE (1) DE69728893T2 (de)
ES (1) ES2219760T3 (de)
WO (1) WO1998019999A1 (de)

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6008204A (en) 1995-09-01 1999-12-28 Allergan Sales, Inc. Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
US5958954A (en) 1995-09-01 1999-09-28 Allergan Sales, Inc. Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
US5952345A (en) 1995-09-01 1999-09-14 Allergan Sales, Inc. Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
US6555690B2 (en) 1996-06-21 2003-04-29 Allergan, Inc. Alkyl or aryl substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity
US5773594A (en) 1996-06-21 1998-06-30 Allergan Alkyl or aryl substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity
US5763635A (en) 1996-06-21 1998-06-09 Allergan Tetrahydronaphthalene derivatives substituted in the 8 position with alkyhidene groups having retinoid and/or retinoid antagonist-like biological activity
US5728846A (en) * 1996-12-12 1998-03-17 Allergan Benzo 1,2-g!-chrom-3-ene and benzo 1,2-g!-thiochrom-3-ene derivatives
AU4583599A (en) 1998-06-25 2000-01-10 Sepracor, Inc. Di- and tetra-hydroquinoline-indole antimicrobial agents, uses and compositions related thereto
US6048873A (en) * 1998-10-01 2000-04-11 Allergan Sales, Inc. Tetrahdroquinolin-2-one 6 or 7-yl, tetrahdroquinilin-2-thione 6 or 7-yl pentadienoic acid and related derivatives having retinoid-like biological activity
WO2000061233A2 (en) * 1999-04-14 2000-10-19 Allergan Sales, Inc. Methods and compositions for the treatment and prevention of lung disease involving a specific rar-gamma agonist
AU4222400A (en) * 1999-04-14 2000-11-14 Allergan Sales, Inc. Methods and compositions for the treatment and prevention of lung disease
AU4225500A (en) * 1999-04-14 2000-11-14 Allergan Sales, Inc. Methods and compositions for the treatment and prevention of lung disease
US6869959B1 (en) 1999-04-28 2005-03-22 Institute Of Medicinal Molecular Design Inc. Heterocyclic carboxylic acid derivatives
US7268148B2 (en) * 1999-05-20 2007-09-11 Regents Of The University Of Michigan Compositions and methods for use against acne-induced inflammation and dermal matrix-degrading enzymes
US20040235950A1 (en) * 1999-05-20 2004-11-25 Voorhees John J. Compositions and methods for use against acne-induced inflammation and dermal matrix-degrading enzymes
WO2001007028A2 (en) * 1999-07-23 2001-02-01 Allergan Sales, Inc. The use of retinoid receptor antagonists in the treatment of prostate carcinoma
US6127382A (en) * 1999-08-16 2000-10-03 Allergan Sales, Inc. Amines substituted with a tetrahydroquinolinyl group an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
US20030114482A1 (en) * 1999-12-15 2003-06-19 Maurizio Pacifici Use of retinoid receptor antagonists or agonists in the treatment of cartilage and bone pathologies
US6313168B1 (en) * 1999-12-15 2001-11-06 Allergan Sales, Inc. Use of retinoid receptor antagonists in the treatment of cartilage and bone pathologies
WO2002018361A2 (en) * 2000-08-29 2002-03-07 Allergan, Inc. Compounds having activity as inhibitors of cytochrome p450rai
US6313107B1 (en) * 2000-08-29 2001-11-06 Allergan Sales, Inc. Methods of providing and using compounds having activity as inhibitors of cytochrome P450RAI
US6291677B1 (en) 2000-08-29 2001-09-18 Allergan Sales, Inc. Compounds having activity as inhibitors of cytochrome P450RAI
MXPA04003938A (es) * 2001-10-31 2004-06-18 Hoffmann La Roche Compuestos retinoides heterociclicos.
US6620963B1 (en) 2002-09-19 2003-09-16 Allergan, Inc. TRICYCLO[6.2.202,7]DODECA-2(7),3,5-TRIEN-4-CARBONYLAMINO-PHENYL AND TRICYCLO[6.2.202,7]DODECA-2(7),3,5-TRIEN-4-CARBONYLAMINO-HETEROARYL AND RELATED COMPOUNDS HAVING RARα RECEPTOR SELECTIVE BIOLOGICAL ACTIVITY
US6683092B1 (en) 2003-04-09 2004-01-27 Allergan, Inc. [3-(c5-14alkyl-2-oxo-1,2,3,4-tetrahydro-quinolin-6-yl)-3-oxo-propenyl]-phenyl and [3-(c5-14alkyl-2-oxo-1,2,3,4- tetrahydro-quinolin-6-yl)-3-oxo-propenyl]-heteroaryl derivatives having anti-tumor activity
US6734193B1 (en) 2003-06-03 2004-05-11 Allergan, Inc. (1,2,3,4-tetrahydroquinolin-8-yl)-heptatrienoic acid derivatives having serum glucose reducing activity
CA2551294A1 (en) * 2003-12-26 2005-07-21 Allergan, Inc. Disubstituted chalcone oximes having rary retinoid receptor antagonist activity
US7476673B2 (en) * 2003-12-30 2009-01-13 Allergan, Inc. Disubstituted chalcone oximes as selective agonists of RARγ retinoid receptors
AU2006299645B2 (en) 2005-09-30 2011-02-03 Io Therapeutics, Llc Treatment of cancer with specific RXR agonists
CN101316821A (zh) * 2005-09-30 2008-12-03 詹森药业有限公司 作为rxr激动剂用于治疗异常脂肪血症、高胆固醇血症和糖尿病的二氢-[1h]-喹啉-2-酮衍生物
US7723326B2 (en) * 2005-09-30 2010-05-25 Janssen Pharmaceutica N.V. Heterocyclic amide derivatives as RXR agonists for the treatment of dyslipidemia, hypercholesterolemia and diabetes
EP2026778B1 (de) * 2006-05-16 2018-11-14 Io Therapeutics, LLC Rar-antagonist oder rar-inverse agonist zur verwendung zur behandlung von nebenwirkungen einer chemotherapie und/oder strahlentherapie
US20090197878A1 (en) * 2008-02-01 2009-08-06 Wyeth SUBSTITUTED BENZO[d][1,3]OXAZIN-2(4H)-ONES AND RELATED DERIVATIVES AND THEIR USES FOR MODULATING THE PROGESTERONE RECEPTOR
CN104114171A (zh) 2011-12-13 2014-10-22 Io治疗公司 使用rxr激动剂的自身免疫紊乱的治疗
US9321750B2 (en) 2012-04-20 2016-04-26 Innov17 Llc ROR modulators and their uses
WO2013166015A1 (en) * 2012-04-30 2013-11-07 Anderson Gaweco Ror modulators and their uses
EP2844259A4 (de) 2012-04-30 2015-11-11 Anderson Gaweco Ror-modulatoren und deren verwendungen
CN106795138B (zh) * 2014-10-31 2020-04-14 豪夫迈·罗氏有限公司 新型二氢喹啉吡唑基化合物
WO2016066663A1 (en) * 2014-10-31 2016-05-06 F. Hoffmann-La Roche Ag Pyrazolyl-3,4-dihydroquinolin-2-one aldosterone synthase inhibitors
ES2941769T3 (es) 2015-10-31 2023-05-25 Io Therapeutics Inc Tratamiento de trastornos del sistema nervioso utilizando combinaciones de agonistas de RXR y hormonas tiroideas
EP3380086B1 (de) 2015-11-25 2021-10-13 IO Therapeutics, Inc. Cyp26-resistenten rar-alpha-selektiven agonisten bei der behandlung von krebs
US10946001B2 (en) 2016-03-10 2021-03-16 Io Therapeutics, Inc. Treatment of autoimmune diseases with combinations of RXR agonists and thyroid hormones
ES2926961T3 (es) 2016-03-10 2022-10-31 Io Therapeutics Inc Tratamiento de trastornos musculares con combinaciones de agonistas de RXR y hormonas tiroideas
EP3468600A4 (de) 2016-06-10 2019-11-13 IO Therapeutics, Inc. Rezeptorselektive retinoid- und rexinoidverbindungen und immunmodulatoren zur krebsimmuntherapie
NZ760459A (en) 2017-07-13 2023-05-26 Io Therapeutics Inc Receptor subtype and function selective retinoid and rexinoid compounds in combination with immune modulators for cancer immunotherapy
WO2019046591A1 (en) 2017-08-31 2019-03-07 Io Therapeutics, Inc. SELECTIVE RAR AGONISTS IN ASSOCIATION WITH IMMUNE MODULATORS IN ANTICANCER IMMUNOTHERAPY
AU2018335393A1 (en) 2017-09-20 2020-04-02 Io Therapeutics, Inc. Treatment of disease with esters of selective RXR agonists
US10966950B2 (en) 2019-06-11 2021-04-06 Io Therapeutics, Inc. Use of an RXR agonist in treating HER2+ cancers
EP4444288A1 (de) 2021-12-07 2024-10-16 Io Therapeutics, Inc. Verwendung eines rxr-agonisten zur behandlung von arzneimittelresistentem her2+-krebs
MX2024006978A (es) 2021-12-07 2024-07-19 Io Therapeutics Inc Uso de un agonista de rxr y taxanos en el tratamiento de cáncer her2+.

Family Cites Families (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4085091A (en) * 1976-12-16 1978-04-18 E. I. Dupont De Nemours And Company Thermally stable, rigid polyesters from thermally stable, rigid dibasic acids and aromatic dihydroxy compounds
US4326055A (en) * 1977-12-22 1982-04-20 Hoffmann-La Roche Inc. Stilbene derivatives
EP0047817A3 (de) * 1980-08-14 1982-05-26 F. HOFFMANN-LA ROCHE & CO. Aktiengesellschaft Hydrierte Naphthaline, deren Herstellung und Verwendung sowie derartige Naphthaline enthaltende Gemische
CH651034A5 (de) * 1982-05-12 1985-08-30 Hoffmann La Roche Chroman-, thiochroman- oder 1,2,3,4-tetrahydrochinolinderivate und ihre verwendung als arzneimittel-wirkstoffe.
DK158947C (da) * 1982-07-06 1991-01-21 Hoffmann La Roche Tetrahydronaphthalin-,benzofuran- og benzothiophenderivater, fremstilling og anvendelse deraf samt rodenticid indeholdende saadanne derivater
DE3475305D1 (en) * 1983-07-05 1988-12-29 Pfizer Carboxylic acid derivatives useful for inhibiting the degradation of cartilage
EP0155940A1 (de) * 1983-08-08 1985-10-02 Sri International Benzonorbornenyl, benzopyranyl und benzothiopyranyl retinsäure analogen
FR2562539B1 (fr) * 1984-04-06 1987-04-17 Chauvin Blache Lab Nouveaux derives de l'acide vinyl-4 benzoique, leur procede de preparation et leurs applications en therapeutique et comme ligands
US4826984A (en) * 1984-04-09 1989-05-02 The Board Of Regents For The Oklahoma Agricultural And Mechanical College Acting For And On Behalf Of Oklahoma State University Heteroarotinoid compounds as anticancer agents
JPS60222445A (ja) * 1984-04-19 1985-11-07 Yoshitomi Pharmaceut Ind Ltd フタル酸化合物
DE3580134D1 (de) * 1984-07-07 1990-11-22 Shudo Koichi Prof Dr Chem Benzoesaeurederivate.
JPS6122046A (ja) * 1984-07-07 1986-01-30 Koichi Shiyudo スチルベン誘導体
LU85544A1 (fr) * 1984-09-19 1986-04-03 Cird Derives heterocycliques aromatiques,leur procede de preparation et leur application dans les domaines therapeutique et cosmetique
DE3434942A1 (de) * 1984-09-22 1986-04-03 Basf Ag, 6700 Ludwigshafen Tetralin-derivate, ihre herstellung und verwendung
DE3434947A1 (de) * 1984-09-22 1986-04-03 Basf Ag, 6700 Ludwigshafen Isoxazolcarbonsaeure-derivate, ihre herstellung und verwendung
DE3434946A1 (de) * 1984-09-22 1986-04-03 Basf Ag, 6700 Ludwigshafen Diarylacetylene, ihre herstellung und verwendung
IL80270A0 (en) * 1985-10-11 1987-01-30 Cird Naphthalene derivatives,their preparation and pharmaceutical compositions containing them
DE3602473A1 (de) * 1986-01-28 1987-07-30 Basf Ag Vinylphenolderivate, ihre herstellung und verwendung
LU86351A1 (fr) * 1986-03-12 1987-11-11 Oreal Composes benzopyrannyl et benzothiopyrannyl benzoiques,leur procede de preparation et leur utilisation en cosmetique et en medecine humaine et veterinaire
DE3615157A1 (de) * 1986-05-05 1987-11-12 Schwabe Willmar Gmbh & Co 5-arylalkyl-4-alkoxy-2(5h)-furanone, zwischenprodukte und verfahren zu ihrer herstellung sowie ihre anwendung als therapeutische wirkstoffe
ZW6587A1 (en) * 1986-05-13 1987-12-02 Hoffmann La Roche Tetrahydro naphthanline derivatives
ZW7487A1 (en) * 1986-05-23 1987-12-16 Hoffmann La Roche Tetrahydronaphthaline and indane derivatives
ZW10287A1 (en) * 1986-07-15 1988-01-13 Hoffmann La Roche Tetrahydronaphthaline and indane derivatives
US4739098A (en) * 1986-09-22 1988-04-19 Allergan, Inc. Ethynylphenyl-containing retinoic acid derivatives
US4927947A (en) * 1986-12-24 1990-05-22 Allergan, Inc. Ethynylheteroaromatic-acids having retinoic acid-like activity
NZ222968A (en) * 1986-12-24 1990-05-28 Allergan Inc Ethynylheteroaromatic derivatives and medicaments
US5149705A (en) * 1987-03-13 1992-09-22 Allergan, Inc. Acetylenes disubstituted with a heteroaromatic group and a tetralin group and having retinoid like activity
CA1305480C (en) * 1987-03-20 1992-07-21 Roshantha A.S. Chandraratna Disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups having retinoid like activity
US5234926A (en) * 1987-03-20 1993-08-10 Allergan, Inc. Disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups having retinoid like activity
US5089509A (en) * 1988-09-15 1992-02-18 Allergan, Inc. Disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups having retinoid like activity
US5264578A (en) * 1987-03-20 1993-11-23 Allergan, Inc. Disubstituted acetylenes bearing heterobicyclic groups and heteroaromatic or phenyl groups having retinoid like activity
US4810804A (en) * 1987-03-26 1989-03-07 Allergan, Inc. Acetylenes disubstituted with a phenyl group and a heterobicyclic group having retinoid-like activity
ZA885192B (en) * 1987-08-19 1989-04-26 Hoffmann La Roche Pharmaceutical preparations
CA1298309C (en) * 1987-11-06 1992-03-31 Michael Klaus Benzocycloheptene derivatives
KR0139216B1 (ko) * 1988-04-11 1998-05-01 제임스 엠. 캐내지 레티노이드 유사활성을 갖는 페놀 또는 벤조산의 테트랄린 에스테르
US5231113A (en) * 1988-04-11 1993-07-27 Allergan, Inc. Tetralin esters of phenols or benzoic acids having retinoid like activity
US4895868A (en) * 1988-06-29 1990-01-23 Allergan, Inc. Thiochroman esters of phenols and terephthallates having retinoid-like activity
US5015658A (en) * 1988-06-29 1991-05-14 Allergan, Inc. Thiochroman esters of phenols and terephthallates having retinoid-like activity
AU626881B2 (en) * 1988-07-14 1992-08-13 F. Hoffmann-La Roche Ag Benzofused heterocyclics used as pharmaceuticals
CA2002864C (en) * 1988-11-29 1999-11-16 Eddy J. E. Freyne (1h-azol-1-ylmethyl) substituted quinoline, quinazoline or quinoxaline derivatives
US5068252A (en) * 1989-07-26 1991-11-26 Allergan, Inc. Methods of using phenylethenyl compounds having retinoid-like activity
US4992468A (en) * 1989-07-26 1991-02-12 Allergan, Inc. Phenylethenyl compounds having retinoid-like activity
US5053523A (en) * 1989-09-19 1991-10-01 Allergan, Inc. Ethynyl-chroman compounds
US5023341A (en) * 1989-09-19 1991-06-11 Allergan, Inc. Compounds having a disubstituted acetylene moiety and retinoic acid-like biological activity
US5248777A (en) * 1989-09-19 1993-09-28 Allergan, Inc. Process and intermediates for preparing compounds having a disubstituted acetylene moiety and retinoic acid-like biological activity
US5162546A (en) * 1989-09-19 1992-11-10 Allergan, Inc. Acetylenes disubstituted with a phenyl group and a 2-substituted chromanyl, thiochromanyl or 1,2,3,4-tetrahydroquinolinyl group having retinoid-like activity
US5399561A (en) * 1989-09-19 1995-03-21 Allergan, Inc. Acetylenes disubstituted with a phenyl or heteroaryl group and a 2-oxochromanyl, 2-oxothiochromanyl or 2-oxo-1,2,3,4-tetrahydro-quinolinyl group having retinoid-like biological activity
US4980369A (en) * 1989-09-19 1990-12-25 Allergan, Inc. Acetylenes disubstituted with a phenyl group and a 2-substituted chromanyl or thiochromanyl group having retinoid-like activity
US5045551A (en) * 1989-09-19 1991-09-03 Allergan, Inc. Acetylenes disubstituted with a heteroaromatic group and a 2-substituted chromanyl, thiochromanyl or 1,2,3,4-tetrahydroquinolinyl group having retinoid-like activity
US5183827A (en) * 1989-09-19 1993-02-02 Allergan, Inc. Acetylenes disubstituted with a heteroaromatic group and a 2-substituted chromanyl, thiochromanyl or 1,2,3,4-tetrahydroquinolinyl group having retinoid-like activity
US5272156A (en) * 1989-09-19 1993-12-21 Allergan, Inc. Acetylenes disubstituted with a heteroaromatic group and a 2-substituted 1,2,3,4-tetrahydroquinolinyl group having retinoid-like activity
US5175185A (en) * 1989-12-29 1992-12-29 Allergan, Inc. Acetylenes disubstituted with a heteroaromatic group and a substituted phenyl group having retinoid like activity
US5013744B1 (en) * 1989-12-29 1994-09-20 Allegran Inc Acetylenes disubstituted with a pyridinyl group and a substituted phenyl group having retinoid like activity
US5264456A (en) * 1989-12-29 1993-11-23 Allergan, Inc. Acetylenes disubstituted with a furyl group and a substituted phenyl group having retinoid like activity
US5006550A (en) * 1989-12-29 1991-04-09 Allergan, Inc. Chroman esters of phenols and benzoic acids having retinoid-like activity
US5202471A (en) * 1990-02-06 1993-04-13 Allergan, Inc. Alkyl, alkoxy and thioalkoxy substituted diphenyl acetylenes having retinoid like activity
WO1991016051A1 (en) * 1990-04-16 1991-10-31 Rhône-Poulenc Rorer International (Holdings) Inc. Styryl-substituted monocyclic and bicyclic heteroaryl compounds which inhibit egf receptor tyrosine kinase
LU87821A1 (fr) * 1990-10-12 1992-05-25 Cird Galderma Composes bi-aromatiques,et leur utilisation en medecine humaine et veterinaire et en cosmetique
DE69214632T2 (de) * 1991-02-13 1997-05-28 Allergan Inc 7-phenylethynyl-substituierte chromane und thiochromane mit retinoid-ähnlicher biologischer aktivität
US5134159A (en) * 1991-03-26 1992-07-28 Allergan, Inc. 7-chromanyl esters of phenols and benzoic acids having retinoid-like activity
CA2105379A1 (en) * 1991-03-26 1992-09-27 Roshantha A. S. Chandraratna Chromans and thiochromans with heteroarylethynyl substituents at the 7-position having retinoid-like biological activity
JP2980398B2 (ja) * 1991-04-17 1999-11-22 シャープ株式会社 電子写真感光体用塗布液の保存方法
US5326898A (en) * 1992-02-11 1994-07-05 Allergan, Inc. Substituted phenylethenyl compounds having retinoid-like biological activity
JP3499553B2 (ja) * 1992-02-11 2004-02-23 アラーガン、インコーポレイテッド レチノイド様生物学的活性を有するヘテロアリール置換フェニルエテニル化合物
DE69329278T2 (de) * 1992-04-22 2001-08-09 Ligand Pharmaceuticals, Inc. Retinoid-x rezeptor selektive verbindungen
US5324840A (en) * 1992-06-11 1994-06-28 Allergan, Inc. Method of treatment with compounds having retinoid-like activity and reduced skin toxicity and lacking teratogenic effects
US5455265A (en) * 1993-02-11 1995-10-03 Allergan, Inc. Method of treatment with compounds having selective agonist-like activity on RXR retinoid receptors
US5399586A (en) * 1993-03-11 1995-03-21 Allergan, Inc. Treatment of mammals afflicted with tumors with compounds having RXR retinoid receptor agonist activity
US5344959A (en) * 1993-05-18 1994-09-06 Allergan, Inc. Tetrahydronaphthyl and cyclopropyl substituted 1,3-butadienes having retinoid-like activity
US5475022A (en) * 1993-10-18 1995-12-12 Allergan, Inc. Phenyl or heteroaryl and tetrahydronaphthyl substituted diene compounds having retinoid like biological activity
US5470999A (en) * 1993-12-30 1995-11-28 Allergan, Inc. Cyclohexene and bicyclic aromatic substituted ethyne compounds having retinoid-like biological activity
US5451605A (en) * 1993-12-30 1995-09-19 Allergan, Inc. 1,2-epoxycyclohexanyl and bicyclic aromatic substituted ethyne compounds having retinoid-like biological activity
US5426118A (en) * 1993-12-30 1995-06-20 Allergan, Inc. [4-(1,2-epoxycyclohexanyl)but-3-en-1-ynyl]aromatic and heteroaromatic acids and derivatives having retinoid-like biological activity
CA2138000A1 (en) * 1994-01-03 1995-07-04 John E. Starrett, Jr. Retinoid-like compounds
US5498755A (en) * 1994-08-23 1996-03-12 Chandraratna; Roshantha A. Disubstituted aryl and heteroaryl imines having retinoid-like biological activity
US5514825A (en) * 1994-12-29 1996-05-07 Allergan, Inc. Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity
US5534641A (en) * 1994-12-29 1996-07-09 Allergan Acetylenes disubstituted with 2-tetrahydropyranoxyaryl and aryl or heteroaryl groups having retinoid-like biological activity
US5498795A (en) * 1994-12-29 1996-03-12 Allergan, Inc. Acetylenes disubstituted with hydroxyaryl and aryl or heteroaryl groups having retinoid-like biological activity
US5556996A (en) * 1994-12-29 1996-09-17 Allergan Oxiranyls disubstituted with a phenyl group and a substituted chromanyl or tetrahydroquinolinyl group having retinoid like activity
US5489584A (en) * 1994-12-29 1996-02-06 Allergan, Inc. Acetylenes disubstituted with a 5-amino or substituted 5-amino substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity
US5543534A (en) * 1994-12-29 1996-08-06 Allergan Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl or heteroaryl groups having retinoid-like biological activity
US5675024A (en) * 1995-11-22 1997-10-07 Allergan Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thiochroman and 1,2,3,4,-tetrahydroquinoline carboxylic acids, having an electron withdrawing substituent in the aromatic or heteroaromatic moiety, having retinoid-like biological activity

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AU5101198A (en) 1998-05-29
ES2219760T3 (es) 2004-12-01
CA2270893C (en) 2008-10-21
WO1998019999A1 (en) 1998-05-14
JP2001504458A (ja) 2001-04-03
AU729997B2 (en) 2001-02-22
US5739338A (en) 1998-04-14
DE69728893T2 (de) 2005-04-21
CA2270893A1 (en) 1998-05-14
EP0937045A1 (de) 1999-08-25
ATE265436T1 (de) 2004-05-15

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