ES2133798T3 - Ligandos del receptor x del acido retinoico. - Google Patents

Ligandos del receptor x del acido retinoico.

Info

Publication number
ES2133798T3
ES2133798T3 ES95930430T ES95930430T ES2133798T3 ES 2133798 T3 ES2133798 T3 ES 2133798T3 ES 95930430 T ES95930430 T ES 95930430T ES 95930430 T ES95930430 T ES 95930430T ES 2133798 T3 ES2133798 T3 ES 2133798T3
Authority
ES
Spain
Prior art keywords
pct
ligands
retinoic acid
acid receptor
sec
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 - Lifetime
Application number
ES95930430T
Other languages
English (en)
Inventor
Michael Klaus
Allen John 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
Application granted granted Critical
Publication of ES2133798T3 publication Critical patent/ES2133798T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • 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
    • 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 Table
    • 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 ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Nutrition Science (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Paints Or Removers (AREA)

Abstract

COMPUESTOS DE FORMULA (I), EN DONDE R 1 -R 7 , R SUP,10} Y EL ENLACE PUNTEADO, TIENEN EL SIGNIFICADO INDICADO EN LA DESCRIPCION. DICHOS COMPUESTOS SE UNEN A SELECTIVAMENTE A LOS RECEPTORES RXR RETINOIDES, Y SON UTILES COMO AGENTES ANTIPROLIFERATIVOS PARA INDICACIONES DERMATOLOGICAS Y ONCOLOGICAS.
ES95930430T 1994-08-10 1995-07-29 Ligandos del receptor x del acido retinoico. Expired - Lifetime ES2133798T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP94112461 1994-08-10
EP95110460 1995-07-05

Publications (1)

Publication Number Publication Date
ES2133798T3 true ES2133798T3 (es) 1999-09-16

Family

ID=26135772

Family Applications (1)

Application Number Title Priority Date Filing Date
ES95930430T Expired - Lifetime ES2133798T3 (es) 1994-08-10 1995-07-29 Ligandos del receptor x del acido retinoico.

Country Status (24)

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

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US5968908A (en) * 1994-12-19 1999-10-19 American Cyanamid Company Restricted 9-cis retinoids
IL116259A (en) * 1994-12-19 2000-07-16 American Cyanamid Co Analogs of 9-cis retinoic acid and their use
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
WO1997010813A1 (en) 1995-09-18 1997-03-27 Ligand Pharmaceuticals Incorporated Ppar gamma antagonists for treating obesity
ATE236115T1 (de) 1995-10-06 2003-04-15 Ligand Pharm Inc Dimer-selektive rxr modulatoren und verfahren zu ihrer verwendung
FR2746101B1 (fr) * 1996-03-14 1998-04-30 Composes bicycliques-aromatiques
EP0915825B1 (en) * 1996-06-21 2004-05-06 Allergan, Inc. Substituted tetrahydronaphthalene and dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity
DE69739828D1 (de) 1996-12-11 2010-05-12 Dana Farber Cancer Inst 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
KR20010032000A (ko) * 1997-11-12 2001-04-16 프리돌린 클라우스너, 롤란드 비. 보레르 레티노이드 길항제를 이용한 티-보조 세포 제2형 중재면역 질환의 치료
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
AU6941200A (en) 1999-08-27 2001-03-26 Ligand Pharmaceuticals Incorporated 8-substituted-6-trifluoromethyl-9-pyrido(3,2-g)quinoline compounds as androgen receptor modulators
WO2001016139A1 (en) 1999-08-27 2001-03-08 Ligand Pharmaceuticals Incorporated Androgen receptor modulator compounds and methods
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
CO5200852A1 (es) 1999-09-14 2002-09-27 Lilly Co Eli Moduladores rxr con mejorado perfil farmacologico ceptores x de los retinoides
EP1741447B1 (en) 2000-01-21 2013-09-18 Novartis AG Combinations comprising dipeptidylpeptidase-IV inhibitors and antidiabetic agents
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
US6313107B1 (en) 2000-08-29 2001-11-06 Allergan Sales, Inc. Methods of providing and using compounds having activity as inhibitors of cytochrome P450RAI
EP1373240B1 (en) * 2001-03-14 2005-06-15 Eli Lilly And Company Retinoid x receptor modulators
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
EP1653939A2 (en) * 2003-08-07 2006-05-10 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
CA2622600A1 (en) * 2005-10-25 2007-05-03 Werner Bollag Rxr agonists and antagonists, alone or in combination with ppar ligands, in the treatment of metabolic and cardiovascular diseases
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
US20160263189A1 (en) 2013-10-23 2016-09-15 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
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WO1995004036A1 (en) * 1993-01-11 1995-02-09 Ligand Pharmaceuticals Inc. 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
CA2196197C (en) 2007-04-17
NZ292121A (en) 1998-10-28
NO970580L (no) 1997-02-07
ATE181052T1 (de) 1999-06-15
TR199500976A2 (tr) 1996-06-21
HUT76839A (en) 1997-11-28
DE69510203D1 (de) 1999-07-15
CZ38297A3 (en) 1997-06-11
RU2146241C1 (ru) 2000-03-10
DE69510203T2 (de) 1999-12-23
CZ288526B6 (cs) 2001-07-11
DK0775103T3 (da) 1999-11-15
CY2170B1 (en) 2002-08-23
KR970704663A (ko) 1997-09-06
BR9508985A (pt) 1998-01-06
FI970547A (fi) 1997-02-07
EP0775103A1 (en) 1997-05-28
JP2848964B2 (ja) 1999-01-20
CN1152302A (zh) 1997-06-18
CA2196197A1 (en) 1996-02-22
PL318557A1 (en) 1997-06-23
GR3031154T3 (en) 1999-12-31
AU3382195A (en) 1996-03-07
NO970580D0 (no) 1997-02-07
AU696501B2 (en) 1998-09-10
FI970547A0 (fi) 1997-02-07
EP0775103B1 (en) 1999-06-09
HU218268B (hu) 2000-06-28
KR100363545B1 (ko) 2003-02-19
FI112357B (fi) 2003-11-28
US5801253A (en) 1998-09-01
WO1996005165A1 (en) 1996-02-22
JPH09512830A (ja) 1997-12-22
PL180048B1 (en) 2000-12-29
MX9700778A (es) 1997-05-31
NO307702B1 (no) 2000-05-15
CN1091092C (zh) 2002-09-18

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