AR042617A1 - Disorazoles y sus derivados, utiles para el tratamiento de enfermedades tumorales benignas y malignas, y el uso de dichos compuestos para la preparacion de medicamentos. - Google Patents

Disorazoles y sus derivados, utiles para el tratamiento de enfermedades tumorales benignas y malignas, y el uso de dichos compuestos para la preparacion de medicamentos.

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Publication number
AR042617A1
AR042617A1 ARP030103050A ARP030103050A AR042617A1 AR 042617 A1 AR042617 A1 AR 042617A1 AR P030103050 A ARP030103050 A AR P030103050A AR P030103050 A ARP030103050 A AR P030103050A AR 042617 A1 AR042617 A1 AR 042617A1
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AR
Argentina
Prior art keywords
alkyl
same
oxygen
hydrogen
double bond
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ARP030103050A
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English (en)
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Zentaris Gmbh
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Publication date
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Publication of AR042617A1 publication Critical patent/AR042617A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P17/12—Keratolytics, e.g. wart or anti-corn preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
    • A—HUMAN NECESSITIES
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    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
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    • A61P33/00—Antiparasitic agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
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  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)

Abstract

Medicamento que contiene al menos un derivado de disorazol de la fórmula general (1), útil preferentemente para el tratamiento de enfermedades tumorales benignas y malignas, en especial en caso de resistencia medicamentos a otros ingredientes activos y en caso de carcinoma con metástasis. En dicha fórmula (1), independientemente entre sí R1 es hidrógeno, OR4, es parte de un enlace doble con C5'; R2, R3 y R4: son hidrógeno, alquilo (C1-6) insustituido o sustituido, son alquilo (C1-4) sustituido por uno o varios átomos de flúor, con preferencia, un grupo trifluorometilo, son alquil(C1-4)-arilo(C6-14) insustituido o sustituido, son carboxilo, alcoxicarbonilo C1-4, alquilaminocarbonilo(C1-4)-alquilaminotiocarbonilo(C1-4), carboxialquilo C1-6 o alcoxi(C1-6)-carbonilalquilo(C1-6),donde la sustitución del radical alquilo por F, Cl, Br, I, CN, NH2, NH-alquilo (C1-20), NH-cicloalquilo (C3-12), OH, O-alquilo C1-20 puede ser una monosustitución en átomos iguales o diferentes o puede ser una polisustitución con sustituyentes iguales o diferentes, y donde la sustitución de un radical arilo por F, Cl, Br, I, CN, NH2, NH-alquilo (C1-20), OH, O-alquilo (C1-20) y/o heterociclilo C3-8 por 1 a 5 heteroátomos, con preferencia, nitrógeno, oxígeno, azufre puede ser una monosustitución en átomos iguales o diferentes o puede ser polisustitución con sustituyente iguales o diferentes; y X, Y: son en cada caso, de modo independiente entre sí o ambos, oxígeno, azufre, dos grupos hidroxi vecinos, dos grupos metoxi vecinos, parte de un enlace doble, donde se excluye un compuesto, en el cual R1 es metoxi, R2, R3 son hidrógeno, X es oxígeno e Y es parte de un enlace doble, sus tautómeros, isómeros E/Z, estereoisómeros, incluyendo los diastereómeros y enantiómeros, así como las sales de tolerancia fisiológica de los mismos. También se describe el uso de dichos compuestos para la preparación de medicamentos. Reivindicación 1: Medicamento que contiene al menos un derivado de disorazol de la fórmula general (1), caracterizado, de modo independiente entre sí, R1 es hidrógeno, OR4, es parte de un enlace doble con C5'; R2, R3 y R4: son hidrógeno, alquilo (C1-6) insustituido o sustituido, son alquilo (C1-4) sustituido por uno o varios átomos de flúor, con preferencia, un grupo trifluorometilo, son alquil(C1-4)-arilo(C6-14) insustituido o sustituido, son carboxilo, alcoxicarbonilo C1-4, alquilaminocarbonilo(C1-4)-alquilaminotiocarbonilo(C1-4), carboxialquilo C1-6 o alcoxi(C1-6)-carbonilalquilo(C1-6),donde la sustitución del radical alquilo por F, Cl, Br, I, CN, NH2, NH-alquilo (C1-20), NH-cicloalquilo (C3-12), OH, O-alquilo C1-20 puede ser una monosustitución en átomos iguales o diferentes o puede ser una polisustitución con sustituyentes iguales o diferentes, y donde la sustitución de un radical arilo por F, Cl, Br, I, CN, NH2, NH-alquilo (C1-20), OH, O-alquilo (C1-20) y/o heterociclilo C3-8 por 1 a 5 heteroátomos, con preferencia, nitrógeno, oxígeno, azufre puede ser una monosustitución en átomos iguales o diferentes o puede ser polisustitución con sustituyente iguales o diferentes; y X, Y: son en cada caso, de modo independiente entre sí o ambos, oxígeno, azufre, dos grupos hidroxi vecinos, dos grupos metoxi vecinos, parte de un enlace doble, donde se excluye un compuesto, en el cual R1 es metoxi, R2, R3 son hidrógeno, X es oxígeno e Y es parte de un enlace doble, sus tautómeros, isómeros E/Z, estereoisómeros, incluyendo los diastereómeros y enantiómeros, así como las sales de tolerancia fisiológica de los mismos.
ARP030103050A 2002-08-24 2003-08-22 Disorazoles y sus derivados, utiles para el tratamiento de enfermedades tumorales benignas y malignas, y el uso de dichos compuestos para la preparacion de medicamentos. AR042617A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US40559402P 2002-08-24 2002-08-24

Publications (1)

Publication Number Publication Date
AR042617A1 true AR042617A1 (es) 2005-06-29

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ID=31993935

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ARP030103050A AR042617A1 (es) 2002-08-24 2003-08-22 Disorazoles y sus derivados, utiles para el tratamiento de enfermedades tumorales benignas y malignas, y el uso de dichos compuestos para la preparacion de medicamentos.

Country Status (20)

Country Link
US (2) US20040106662A1 (es)
EP (1) EP1536789A1 (es)
JP (1) JP2006500398A (es)
KR (1) KR20050038632A (es)
CN (1) CN1678310A (es)
AR (1) AR042617A1 (es)
AU (1) AU2003296872B2 (es)
BR (1) BR0313789A (es)
CA (1) CA2438001A1 (es)
HR (1) HRP20050277A2 (es)
IL (1) IL166588A0 (es)
MX (1) MXPA05002157A (es)
NO (1) NO20051444L (es)
NZ (1) NZ538926A (es)
PL (1) PL376407A1 (es)
RU (1) RU2322236C2 (es)
TW (1) TW200404537A (es)
UA (1) UA79480C2 (es)
WO (1) WO2004024149A1 (es)
ZA (1) ZA200501196B (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5340155B2 (ja) * 2006-09-06 2013-11-13 エテルナ ツェンタリス ゲゼルシャフト ミット ベシュレンクテル ハフツング 細胞結合分子を有するジソラゾールのコンジュゲート及びそれらの誘導体、新規ジソラゾール誘導体、それらの製法ならびに使用
EP1900742A1 (en) * 2006-09-07 2008-03-19 AEterna Zentaris GmbH Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof
CN101578287B (zh) * 2006-09-06 2012-09-05 阿特纳赞塔里斯有限公司 地索拉唑及其衍生物与细胞结合分子的轭合物，新的地索拉唑衍生物，其制备方法及其应用
US11465997B2 (en) 2017-06-22 2022-10-11 William Marsh Rice University Synthesis of disorazoles and analogs thereof as potent anticancer agents

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1412332T3 (da) * 2001-07-31 2005-05-30 Univ Wayne State Quinolinderivater og anvendelse deraf som antitumormidler
UA79293C2 (en) * 2002-07-03 2007-06-11 Univ Wayne State 4-(7'-halo-2-quino (xa-) linyloxy)phenoxy propionic acid derivatives as antineoplastic agents
US7364877B2 (en) * 2002-12-06 2008-04-29 Kosan Biosciences, Inc. Polynucleotides encoding disorazole polyketide synthase polypeptides

Also Published As

Publication number Publication date
ZA200501196B (en) 2005-10-26
NO20051444L (no) 2005-05-19
MXPA05002157A (es) 2005-05-23
PL376407A1 (en) 2005-12-27
CA2438001A1 (en) 2004-02-24
UA79480C2 (en) 2007-06-25
EP1536789A1 (de) 2005-06-08
TW200404537A (en) 2004-04-01
RU2322236C2 (ru) 2008-04-20
NZ538926A (en) 2006-03-31
IL166588A0 (en) 2006-01-15
CN1678310A (zh) 2005-10-05
KR20050038632A (ko) 2005-04-27
RU2005108570A (ru) 2005-08-27
US20040106662A1 (en) 2004-06-03
AU2003296872B2 (en) 2008-02-14
WO2004024149A1 (de) 2004-03-25
AU2003296872A1 (en) 2004-04-30
JP2006500398A (ja) 2006-01-05
HRP20050277A2 (en) 2005-04-30
US20090311264A1 (en) 2009-12-17
BR0313789A (pt) 2005-07-05

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