BRPI0901157A2 - complexo molecular antineoplásico-testosterona - Google Patents

complexo molecular antineoplásico-testosterona Download PDF

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BRPI0901157A2
BRPI0901157A2 BRPI0901157-9A BRPI0901157A BRPI0901157A2 BR PI0901157 A2 BRPI0901157 A2 BR PI0901157A2 BR PI0901157 A BRPI0901157 A BR PI0901157A BR PI0901157 A2 BRPI0901157 A2 BR PI0901157A2
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testosterone
molecular
drug
molecular complex
antineoplastic
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BRPI0901157-9A
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English (en)
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Paiva Gerson Silva
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Univ Fed Pernambuco
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Priority to BRPI0901157-9A priority Critical patent/BRPI0901157A2/pt
Priority to PCT/BR2010/000161 priority patent/WO2010108251A2/pt
Publication of BRPI0901157A2 publication Critical patent/BRPI0901157A2/pt

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/243—Platinum; Compounds thereof
    • 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
    • A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/554—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis

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  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract

COMPLEXO MOLECULAR ANTINEOPLáSICO-TESTOSTERONA. A presente invenção trata de um COMPLEXO MOLECULAR ANTINEOPLASICO-TESTOSTERONA composto de uma cadeia molecular de testosterona (1), um fármaco antineoplásico e uma ponte molecular ou uma molécula. O presente composto está caracterizado por ser baseado em uma molécula de testosterona (1) unida quimicamente a um fármaco antineoplásico comercial, como a daunorrubicina ou doxorrubicina (2), cispiatina (3), carboplatina (4) ou cispíatina-berenil (5) por meio de uma ponte molecular do tipo carbamato (6) ou por uma molécula de N',N-disuccnimidil-carbonato (7). O complexo molecular é uma forma de "guiar" o fármaco anticâncer diretamente ao tumor, permitindo assim que o mesmo atue de forma seletiva na próstata, evitando assim efeitos em tecidos sadios uma vez que este tipo de câncer necessita de muita testosterona para se desenvolver.

Description

COMPLEXO MOLECULAR ANTINEOPLÁSICO-TESTOSTERONA
A presente Patente de Invenção refere-se a "COMPLEXO MOLECULARANTINEOPLÁSICO-TESTOSTERONA", ou mais particularmente a um compostomolecular capaz de atuar seletivamente no câncer de próstata sem danificar as célulassadias.
O câncer de próstata é o mais freqüentemente diagnosticado e a segunda causa deóbito por câncer em homens no mundo. Atualmente são usados três métodos de privaçãoandrogênica no tratamento paliativo de câncer de próstata metastático: 1) castraçãocirúrgica por orquiectomia para remover os órgãos produtores primários de andrógenos; 2)castração clínica por terapia com estrogênio ou LHRH (hormônio de liberação de LH) parareduzir a produção de LH (hormônio luteinizante); 3) terapia antiandrogênica direcionadaprimariamente aos órgãos-alvos (ou seja, próstata e pontos metastáticos).
Por outro lado, os andrógenos (classe de moléculas, que incluem a testosterona e aprogesterona, produzidas pelos testículos, ovários e glândulas supra-renais) entram emsuas células-alvos por difusão passiva, existindo evidências de que certos tumores, comoos de próstasta, possuem mecanismos que facilitam ou ativam o transporte deandrógenos. Por isso são chamados tumores dependentes de andrógenos.
Portanto, o objetivo da presente Patente de Invenção é propor uma forma dedestruir o câncer de próstata metástico (aquele que se espalha, a partir da próstata, paraoutros órgãos dependentes de andrógenos, como os testículos e túbulos seminíferos)usando o próprio andrógeno como carreador do antineoplásico (no presente caso, aadriamicina, um fármaco anti-câncer comprovadamente eficaz no tratamento de váriostipos de cânceres). É uma forma de "enganar" o tumor, permitindo assim que o fármaco"drible" o processo MDR (de resistência multidroga) e atue de forma seletiva nos órgãos-alvos, uma vez que o câncer de próstata se necessita de muita testosterona para sedesenvolver.
Para uma melhor compreensão do presente fármaco é feita a seguir uma descriçãodetalhada do mesmo, fazendo-se referência aos desenhos anexos, onde a:Figura 1 representa a estrutura dos complexos moleculares que compõem ocomplexo molecular antineoplásico-testosterona;
Figura 2 representa as estruturas das subunidades moleculares que compõem ocomplexo molecular antineoplásico-testosterona;
De acordo com estas ilustrações e em seus pormenores, mais particularmente asfiguras 1 e 2 a presente Patente de Invenção, "COMPLEXO MOLECULARANTINEOPLÁSICO-TESTOSTERONA" consta de uma cadeia molecular de testosterona(1) ligada quimicamente a um fármaco antineoplásico comercial, como a daunorrubicinaou doxorrubicina (2), cisplatina (3), carboplatina (4) ou cisplatina-berenil (5) por meio deuma ponte molecular do tipo carbamato (6) . O presente composto está caracterizado porser baseado em uma molécula de testosterona (1) unida quimicamente a um fármacoantineoplásico comercial (2, 3, 4, 5) por meio de uma ponte carbamato (6).
Como se percebe após o que foi exposto e ilustrado, trata-se de um complexomolecular capaz de combater preferencialmente o câncer de próstata devido ao fato de ofármaco antineoplásico (de uso comercial) estar ligado a um hormônio, a testosterona,este último sendo o alimento do câncer e o carreador do fármaco.

Claims (7)

1. COMPLEXO MOLECULAR ANTINEOPLÁSICO-TESTOSTERONA composto por umacadeia molecular de testosterona, um fármaco antineoplásico e uma ponte molecularcaracterizado por ser baseado na dita cadeia molecular de testosterona unidaquimicamente ao fármaco por meio de uma ponte molecular.
2. COMPLEXO MOLECULAR ANTINEOPLÁSICO-TESTOSTERONA conformereivindicação 1, caracterizado pelo fato de que o fármaco antineoplásico ser um fármacocomercial, como a daunorrubicina ou doxorrubicina (2), cisplatina (3), carboplatina (4) oucisplatina-berenil (5).
3. COMPLEXO MOLECULAR ANTINEOPLÁSICO-TESTOSTERONA conformereivindicação 1, caracterizado pelo fato de que a ponte molecular é o carbamato (6).
4. COMPLEXO MOLECULAR ANTINEOPLÁSICO-TESTOSTERONA composto por umacadeia molecular de testosterona, um fármaco antineoplásico e uma ponte molecularcaracterizado por ser baseado na dita cadeia molecular de testosterona unidaquimicamente ao fármaco por meio de uma molécula.
5. COMPLEXO MOLECULAR ANTINEOPLÁSICO-TESTOSTERONA conformereivindicação 4, caracterizado pelo fato de que o fármaco antineoplásico ser um fármacocomercial, como a daunorrubicina ou doxorrubicina (2), cisplatina (3), carboplatina (4) oucisplatina-berenil (5).
6.
COMPLEXO MOLECULAR ANTINEOPLÁSICO-TESTOSTERONA conformereivindicação 4, caracterizado pelo fato de que a molécula é uma molécula de N',N-disuccnimidil-carbonato (7).
BRPI0901157-9A 2009-03-27 2009-03-27 complexo molecular antineoplásico-testosterona BRPI0901157A2 (pt)

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BRPI0901157-9A BRPI0901157A2 (pt) 2009-03-27 2009-03-27 complexo molecular antineoplásico-testosterona
PCT/BR2010/000161 WO2010108251A2 (pt) 2009-03-27 2010-03-26 Complexo molecular antineoplásico-testosterona

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011123911A1 (pt) * 2010-04-09 2011-10-13 Universidade Federal De Pernambuco - Ufpe Compostos antitumorais testosterona-quimioterápico

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI1101556A2 (pt) * 2011-04-19 2015-07-14 Univ Fed De Pernambuco Ufpe Composto antitumoral testosterona - ( iodo radioativo)
JP2022532342A (ja) 2019-05-14 2022-07-14 ニューベイション・バイオ・インコーポレイテッド 抗がん核内ホルモン受容体標的化化合物
EP4058464A1 (en) 2019-11-13 2022-09-21 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
MX2023011241A (es) 2021-03-23 2023-10-03 Nuvation Bio Inc Compuestos dirigidos a receptores de hormonas nucleares contra el cancer.
EP4334314A1 (en) 2021-05-03 2024-03-13 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds

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* Cited by examiner, † Cited by third party
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BRMU8701986U2 (pt) * 2007-09-28 2010-02-23 Gerson Silva Paiva complexo molecular antineoplásico-testosterona

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011123911A1 (pt) * 2010-04-09 2011-10-13 Universidade Federal De Pernambuco - Ufpe Compostos antitumorais testosterona-quimioterápico

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Free format text: HOMOLOGADA A DESISTENCIA DO PEDIDO, SOLICITADA ATRAVES DA PETICAO NO 019110000198/PE DE 27.07.2011.