BR9307528A - Process for inspecting substance for ability to affect the formation of homodimer at retinoid x receptor, process for inspecting substance for ability to selectively induce heterodimer formation at retinoid receptor X, process for inspecting substance for the ability to affect the ability of a homodimer, in a retinoid receptor x, to bind to dna, process to inspect a response element for the ability to bind to a homodimer in retinoid receptor x, homodimer in retinoid receptor x , bicyclic aromatic compound, process to inhibit heterodimer activity at retinoid receptor x, process to promote transcription of a homodimer-activated gene at retinoid receptor in a cell, process to inhibit homodimer activity at retinoid receptor x, process to determine increased likelihood of pathology, process for treating pathology, process for active selectively formation of homodimer at retinoid receptor x in a cell, process to promote formation of homodimer at retinoid receptor x in a cell, pharmaceutical composition, process for modulating gene expression, and process for treating patient - Google Patents

Process for inspecting substance for ability to affect the formation of homodimer at retinoid x receptor, process for inspecting substance for ability to selectively induce heterodimer formation at retinoid receptor X, process for inspecting substance for the ability to affect the ability of a homodimer, in a retinoid receptor x, to bind to dna, process to inspect a response element for the ability to bind to a homodimer in retinoid receptor x, homodimer in retinoid receptor x , bicyclic aromatic compound, process to inhibit heterodimer activity at retinoid receptor x, process to promote transcription of a homodimer-activated gene at retinoid receptor in a cell, process to inhibit homodimer activity at retinoid receptor x, process to determine increased likelihood of pathology, process for treating pathology, process for active selectively formation of homodimer at retinoid receptor x in a cell, process to promote formation of homodimer at retinoid receptor x in a cell, pharmaceutical composition, process for modulating gene expression, and process for treating patient

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Publication number
BR9307528A
BR9307528A BR9307528-6A BR9307528A BR9307528A BR 9307528 A BR9307528 A BR 9307528A BR 9307528 A BR9307528 A BR 9307528A BR 9307528 A BR9307528 A BR 9307528A
Authority
BR
Brazil
Prior art keywords
homodimer
retinoid receptor
ability
retinoid
receptor
Prior art date
Application number
BR9307528-6A
Other languages
Portuguese (pt)
Inventor
Magnus Pfahl
Xiao-Kun Zhang
Jurgen M Lehman
Marcia I Dawson
James F Cameron
Peter D Hobbs
Ling Jong
Original Assignee
Jolla Cancer Research Foudatio
Stanford Res Inst Int
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 US07/982,305 external-priority patent/US5466861A/en
Priority claimed from US07/982,174 external-priority patent/US5552271A/en
Application filed by Jolla Cancer Research Foudatio, Stanford Res Inst Int filed Critical Jolla Cancer Research Foudatio
Publication of BR9307528A publication Critical patent/BR9307528A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • 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
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00—Drugs for skeletal disorders
    • 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
    • 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
    • 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
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    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A61P5/12—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH for decreasing, blocking or antagonising the activity of the posterior pituitary hormones
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    • C07—ORGANIC CHEMISTRY
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    • C07C63/00—Compounds having carboxyl groups bound to a carbon atoms of six-membered aromatic rings
    • C07C63/33—Polycyclic acids
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    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
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    • C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/30—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
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    • C07D319/06—1,3-Dioxanes; Hydrogenated 1,3-dioxanes not condensed with other rings
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    • 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
    • C07D333/26—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 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
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    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/70567—Nuclear receptors, e.g. retinoic acid receptor [RAR], RXR, nuclear orphan receptors
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Abstract

Patente de Invenção de <B>"COMPOSTOS AROMáTICOS BICìCLICOS LIGADOS E SEU USO NA MODULAçãO DE EXPRESSãO DE GENE DE RECEPTORES DE RETINóIDE"<D>. Compostos aromáticos bicíclicos ligados são providos tendo a estrutura em que R^ 1^, R^ 2^, R^ 3^, R^ 4^, R^ 5^ e n são como definido aqui. Os compostos novos são úteis para modular expressão de gene de receptores de ácido retinóico, receptores de vitamina D e receptore de tiróide. São também providos composições processos farmacêuticos para a modulação de expressão de gene.Patent of Invention of <B> "BICYCLIC AROMATIC COMPOUNDS CONNECTED AND THEIR USE IN MODULATION OF EXPRESSION OF THE GENE OF RETINOID RECEPTORS" <D>. Bicyclic aromatic compounds are provided having the structure in which R ^ 1 ^, R ^ 2 ^, R ^ 3 ^, R ^ 4 ^, R ^ 5 ^ and n are as defined herein. The novel compounds are useful for modulating gene expression of retinoic acid receptors, vitamin D receptors and thyroid receptors. Pharmaceutical process compositions for modulating gene expression are also provided.

BR9307528-6A 1992-11-25 1993-11-24 Process for inspecting substance for ability to affect the formation of homodimer at retinoid x receptor, process for inspecting substance for ability to selectively induce heterodimer formation at retinoid receptor X, process for inspecting substance for the ability to affect the ability of a homodimer, in a retinoid receptor x, to bind to dna, process to inspect a response element for the ability to bind to a homodimer in retinoid receptor x, homodimer in retinoid receptor x , bicyclic aromatic compound, process to inhibit heterodimer activity at retinoid receptor x, process to promote transcription of a homodimer-activated gene at retinoid receptor in a cell, process to inhibit homodimer activity at retinoid receptor x, process to determine increased likelihood of pathology, process for treating pathology, process for active selectively formation of homodimer at retinoid receptor x in a cell, process to promote formation of homodimer at retinoid receptor x in a cell, pharmaceutical composition, process for modulating gene expression, and process for treating patient BR9307528A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US07/982,305 US5466861A (en) 1992-11-25 1992-11-25 Bridged bicyclic aromatic compounds and their use in modulating gene expression of retinoid receptors
US07/982,174 US5552271A (en) 1992-06-16 1992-11-25 RXR homodimer formation
PCT/US1993/011492 WO1994012880A2 (en) 1992-11-25 1993-11-24 Rxr homodimer formation and bridged bicyclic aromatic compounds and their use in modulating gene expression

Publications (1)

Publication Number Publication Date
BR9307528A true BR9307528A (en) 1999-08-31

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BR9307528-6A BR9307528A (en) 1992-11-25 1993-11-24 Process for inspecting substance for ability to affect the formation of homodimer at retinoid x receptor, process for inspecting substance for ability to selectively induce heterodimer formation at retinoid receptor X, process for inspecting substance for the ability to affect the ability of a homodimer, in a retinoid receptor x, to bind to dna, process to inspect a response element for the ability to bind to a homodimer in retinoid receptor x, homodimer in retinoid receptor x , bicyclic aromatic compound, process to inhibit heterodimer activity at retinoid receptor x, process to promote transcription of a homodimer-activated gene at retinoid receptor in a cell, process to inhibit homodimer activity at retinoid receptor x, process to determine increased likelihood of pathology, process for treating pathology, process for active selectively formation of homodimer at retinoid receptor x in a cell, process to promote formation of homodimer at retinoid receptor x in a cell, pharmaceutical composition, process for modulating gene expression, and process for treating patient

Country Status (6)

Country Link
EP (1) EP0671005A1 (en)
JP (3) JPH08506323A (en)
AU (1) AU700706B2 (en)
BR (1) BR9307528A (en)
CA (1) CA2149882A1 (en)
WO (1) WO1994012880A2 (en)

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CA2149882A1 (en) 1994-06-09
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AU700706B2 (en) 1999-01-14
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