DE69510203T2 - Retinoesäure x-rezeptor liganden - Google Patents

Retinoesäure x-rezeptor liganden

Info

Publication number
DE69510203T2
DE69510203T2 DE69510203T DE69510203T DE69510203T2 DE 69510203 T2 DE69510203 T2 DE 69510203T2 DE 69510203 T DE69510203 T DE 69510203T DE 69510203 T DE69510203 T DE 69510203T DE 69510203 T2 DE69510203 T2 DE 69510203T2
Authority
DE
Germany
Prior art keywords
pct
retinoic acid
receptor ligands
sec
date
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
DE69510203T
Other languages
English (en)
Other versions
DE69510203D1 (de
Inventor
Michael Klaus
Allen Lovey
Peter Mohr
Michael Rosenberger
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.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of DE69510203D1 publication Critical patent/DE69510203D1/de
Application granted granted Critical
Publication of DE69510203T2 publication Critical patent/DE69510203T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids, i.e. RP(=X)(XH)2 (X = S, Se)
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4056—Esters of arylalkanephosphonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/52—Esters of acyclic unsaturated carboxylic acids having the esterified carboxyl group bound to an acyclic carbon atom
    • C07C69/533—Monocarboxylic acid esters having only one carbon-to-carbon double bond
    • C07C69/56—Crotonic acid esters; Vinyl acetic acid esters
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/10—Anti-acne 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
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/27—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation
    • C07C45/29—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation of hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/27—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation
    • C07C45/29—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation of hydroxy groups
    • C07C45/298—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation of hydroxy groups with manganese derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/63—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by introduction of halogen; by substitution of halogen atoms by other halogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00—Compounds having —CHO groups
    • C07C47/20—Unsaturated compounds having —CHO groups bound to acyclic carbon atoms
    • C07C47/24—Unsaturated compounds having —CHO groups bound to acyclic carbon atoms containing halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00—Compounds having —CHO groups
    • C07C47/20—Unsaturated compounds having —CHO groups bound to acyclic carbon atoms
    • C07C47/277—Unsaturated compounds having —CHO groups bound to acyclic carbon atoms containing ether groups, groups, groups, or groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/46—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing six-membered aromatic rings and other rings, e.g. cyclohexylphenylacetic acid
    • C07C57/50—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing six-membered aromatic rings and other rings, e.g. cyclohexylphenylacetic acid containing condensed ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/16—Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated
DE69510203T 1994-08-10 1995-07-29 Retinoesäure x-rezeptor liganden Expired - Fee Related DE69510203T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP94112461 1994-08-10
EP95110460 1995-07-05
PCT/EP1995/003021 WO1996005165A1 (en) 1994-08-10 1995-07-29 Retinoic acid x-receptor ligands

Publications (2)

Publication Number Publication Date
DE69510203D1 DE69510203D1 (de) 1999-07-15
DE69510203T2 true DE69510203T2 (de) 1999-12-23

Family

ID=26135772

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69510203T Expired - Fee Related DE69510203T2 (de) 1994-08-10 1995-07-29 Retinoesäure x-rezeptor liganden

Country Status (24)

Country Link
US (1) US5801253A (de)
EP (1) EP0775103B1 (de)
JP (1) JP2848964B2 (de)
KR (1) KR100363545B1 (de)
CN (1) CN1091092C (de)
AT (1) ATE181052T1 (de)
AU (1) AU696501B2 (de)
BR (1) BR9508985A (de)
CA (1) CA2196197C (de)
CY (1) CY2170B1 (de)
CZ (1) CZ288526B6 (de)
DE (1) DE69510203T2 (de)
DK (1) DK0775103T3 (de)
ES (1) ES2133798T3 (de)
FI (1) FI112357B (de)
GR (1) GR3031154T3 (de)
HU (1) HU218268B (de)
MX (1) MX9700778A (de)
NO (1) NO307702B1 (de)
NZ (1) NZ292121A (de)
PL (1) PL180048B1 (de)
RU (1) RU2146241C1 (de)
TR (1) TR199500976A2 (de)
WO (1) WO1996005165A1 (de)

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US5466861A (en) * 1992-11-25 1995-11-14 Sri International Bridged bicyclic aromatic compounds and their use in modulating gene expression of retinoid receptors
IL116259A (en) * 1994-12-19 2000-07-16 American Cyanamid Co Analogs of 9-cis retinoic acid and their use
US5968908A (en) * 1994-12-19 1999-10-19 American Cyanamid Company Restricted 9-cis retinoids
US7115728B1 (en) 1995-01-30 2006-10-03 Ligand Pharmaceutical Incorporated Human peroxisome proliferator activated receptor γ
US5675033A (en) * 1995-06-06 1997-10-07 Allergan 2,4-pentadienoic acid derivatives having retinoid-like biological activity
EP0788353A1 (de) 1995-09-18 1997-08-13 Ligand Pharmaceuticals, Inc. Ppar gamma antagonisten zur behandlung der fettleibigkeit
CA2233888A1 (en) 1995-10-06 1997-04-10 Ligand Pharmaceuticals Incorporated Dimer-selective rxr modulators and methods for their use
FR2746101B1 (fr) * 1996-03-14 1998-04-30 Composes bicycliques-aromatiques
CA2258313A1 (en) * 1996-06-21 1997-12-24 Allergan Sales, Inc. Substituted tetrahydronaphthalene and dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity
EP1410799B1 (de) 1996-12-11 2010-03-31 Dana-Farber Cancer Institute, Inc. Methoden und pharmazeutische Zusammensetzungen zur Inhibition des Tumorwachstums
US5919970A (en) * 1997-04-24 1999-07-06 Allergan Sales, Inc. Substituted diaryl or diheteroaryl methanes, ethers and amines having retinoid agonist, antagonist or inverse agonist type biological activity
EP1030662B1 (de) 1997-11-12 2006-08-02 F. Hoffmann-La Roche Ag Behandlung von t-helfer zel typ 2 vermittelten immunkrankheiten mit retinoid antagonisten
US6242196B1 (en) 1997-12-11 2001-06-05 Dana-Farber Cancer Institute Methods and pharmaceutical compositions for inhibiting tumor cell growth
CA2334545A1 (en) 1998-06-12 1999-12-16 Ligand Pharmaceuticals Incorporated Treatment of anti-estrogen resistant breast cancer using rxr modulators
US6147224A (en) * 1998-10-01 2000-11-14 Allergan Sales, Inc. 2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors
US6403638B1 (en) 1998-10-01 2002-06-11 Allergan Sales, Inc. 2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors
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
US6326397B1 (en) 1998-11-10 2001-12-04 Hoffman-La Roche Inc. Retinoid antagonists and use thereof
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
WO2001016133A2 (en) 1999-08-27 2001-03-08 Ligand Pharmaceuticals Incorporated 8-substituted-6-trifluoromethyl-9-pyrido[3,2-g]quinoline compounds as androgen receptor modulators
HUP0202814A3 (en) 1999-08-27 2003-11-28 Ligand Pharmaceuticals Inc San Androgen receptor modulator compounds and methods for their preparation and pharmaceutical compositions containing them and their use
CO5200852A1 (es) 1999-09-14 2002-09-27 Lilly Co Eli Moduladores rxr con mejorado perfil farmacologico ceptores x de los retinoides
DE60132723T2 (de) 2000-01-21 2009-01-29 Novartis Pharma Ag Zusammensetzungen bestehend aus Dipeptidylpeptidase-IV Inhibitoren und Antidiabetica
US6313107B1 (en) 2000-08-29 2001-11-06 Allergan Sales, Inc. Methods of providing and using compounds having activity as inhibitors of cytochrome P450RAI
US6369225B1 (en) 2000-08-29 2002-04-09 Allergan Sales, Inc. Compounds having activity as inhibitors of cytochrome P450RAI
US6380256B1 (en) 2000-08-29 2002-04-30 Allergan Sales, Inc. Compounds having activity as inhibitors of cytochrome P450RAI
ATE297910T1 (de) * 2001-03-14 2005-07-15 Lilly Co Eli Retinoid x rezeptormodulatoren
US6720423B2 (en) * 2002-04-30 2004-04-13 Allergan, Inc. Dihydrobenzofuran and dihydrobenzothiophene 2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors
AU2003286243A1 (en) * 2002-11-25 2004-06-18 Amedis Pharmaceuticals Ltd. Silicon compounds
US6759547B1 (en) * 2003-01-14 2004-07-06 Allergan, Inc. 5,6,7,8-tetrahydronaphthalen-2-yl 2,6-difluoroheptatrienoic acid derivatives having serum glucose reducing activity
US7019034B2 (en) * 2003-01-28 2006-03-28 Allergan, Inc. Compositions and methods for reducing serum glucose and triglyceride levels in diabetic mammals
US6759546B1 (en) 2003-02-04 2004-07-06 Allergan, Inc. 3,5-di-iso-propyl-heptatrienoic acid derivatives having serum glucose reducing activity
US6884820B2 (en) * 2003-04-03 2005-04-26 Allergan, Inc. 5,6,7,8-tetrahydronaphthalen-2-yl-7-fluoroalkyl-heptatrienoic acid derivatives having serum glucose reducing 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
WO2005013949A2 (en) * 2003-08-07 2005-02-17 Allergan, Inc. Method for treating cachexia with retinoid ligands
US6887896B1 (en) 2003-10-29 2005-05-03 Allergan, Inc. 7-[(7-Alkoxy)-chrom-3-en-6-yl]-heptatrienoic acid and 7-[(3-alkoxy)-5,6-dihydronaphthalen-2-yl]-heptatrienoic acid derivatives having serum glucose reducing activity
US9050310B2 (en) 2004-06-25 2015-06-09 Minas Theodore Coroneo Treatment of ocular lesions
EP1940378A1 (de) * 2005-10-25 2008-07-09 Werner Bollag Rxr-agonisten und antagonisten, allein oder in kombination mit ppar-liganden, bei der behandlung von metabolischen und kardiovaskulären erkrankungen
US20070185055A1 (en) * 2006-02-06 2007-08-09 Guang Liang Jiang Method for treating cachexia with retinoid ligands
US20090209601A1 (en) * 2008-02-15 2009-08-20 Wyeth Use of rxr agonists for the treatment of osteoarthritis
JP5877466B2 (ja) * 2012-02-29 2016-03-08 国立大学法人 岡山大学 テルペノイド由来レチノイド化合物
WO2015059632A1 (en) 2013-10-23 2015-04-30 Acadia Pharmaceuticals Inc. Treatment of a neurodegenerative disease or disorder
US11045441B2 (en) 2015-10-13 2021-06-29 Wisconsin Alumni Research Foundation Use of retinoic acid and analogs thereof to treat central neural apneas
AU2018341099B2 (en) * 2017-09-28 2023-11-02 Johnson & Johnson Consumer Inc. Cosmetic compositions and method of treating the skin
JP2022513114A (ja) 2018-11-26 2022-02-07 デナリ セラピューティクス インコーポレイテッド 脂質代謝調節不全の治療方法

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DE3580134D1 (de) * 1984-07-07 1990-11-22 Shudo Koichi Prof Dr Chem Benzoesaeurederivate.
CA2133587C (en) * 1992-04-22 2008-11-18 Marcus F. Boehm Compounds having selectivity for retinoid x receptors
US5466861A (en) * 1992-11-25 1995-11-14 Sri International Bridged bicyclic aromatic compounds and their use in modulating gene expression of retinoid receptors
CA2153236A1 (en) * 1993-01-11 1995-02-09 Marcus F. Boehm Compounds having selective activity for retinoid x receptors, and means for modulation of processes mediated by retinoid x receptors
US5344959A (en) * 1993-05-18 1994-09-06 Allergan, Inc. Tetrahydronaphthyl and cyclopropyl substituted 1,3-butadienes having retinoid-like activity

Also Published As

Publication number Publication date
CN1091092C (zh) 2002-09-18
CN1152302A (zh) 1997-06-18
DK0775103T3 (da) 1999-11-15
ATE181052T1 (de) 1999-06-15
CZ38297A3 (en) 1997-06-11
BR9508985A (pt) 1998-01-06
HU218268B (hu) 2000-06-28
AU3382195A (en) 1996-03-07
FI970547A (fi) 1997-02-07
RU2146241C1 (ru) 2000-03-10
NZ292121A (en) 1998-10-28
KR100363545B1 (ko) 2003-02-19
AU696501B2 (en) 1998-09-10
NO307702B1 (no) 2000-05-15
CA2196197C (en) 2007-04-17
HUT76839A (en) 1997-11-28
MX9700778A (es) 1997-05-31
PL180048B1 (en) 2000-12-29
US5801253A (en) 1998-09-01
CA2196197A1 (en) 1996-02-22
KR970704663A (ko) 1997-09-06
JP2848964B2 (ja) 1999-01-20
EP0775103A1 (de) 1997-05-28
NO970580D0 (no) 1997-02-07
PL318557A1 (en) 1997-06-23
CY2170B1 (en) 2002-08-23
DE69510203D1 (de) 1999-07-15
TR199500976A2 (tr) 1996-06-21
NO970580L (no) 1997-02-07
JPH09512830A (ja) 1997-12-22
CZ288526B6 (cs) 2001-07-11
FI970547A0 (fi) 1997-02-07
GR3031154T3 (en) 1999-12-31
WO1996005165A1 (en) 1996-02-22
FI112357B (fi) 2003-11-28
ES2133798T3 (es) 1999-09-16
EP0775103B1 (de) 1999-06-09

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