AR059767A1 - Profarmacos de analogos de cc-1065 y sus conjugados, un procedimiento para su preparacion, una composicion farmaceutica que lo comprende y el uso de estos para la fabricacion de un medicamento para el tratamiento del cancer. - Google Patents

Profarmacos de analogos de cc-1065 y sus conjugados, un procedimiento para su preparacion, una composicion farmaceutica que lo comprende y el uso de estos para la fabricacion de un medicamento para el tratamiento del cancer.

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Publication number
AR059767A1
AR059767A1 ARP070100932A ARP070100932A AR059767A1 AR 059767 A1 AR059767 A1 AR 059767A1 AR P070100932 A ARP070100932 A AR P070100932A AR P070100932 A ARP070100932 A AR P070100932A AR 059767 A1 AR059767 A1 AR 059767A1
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AR
Argentina
Prior art keywords
prodrug
subunit
group
prodrugs
conjugates
Prior art date
Application number
ARP070100932A
Other languages
English (en)
Inventor
Robert Zhao
Ravi Chari
Original Assignee
Sanofi Aventis
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 Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR059767A1 publication Critical patent/AR059767A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/04Amoebicides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/10Anthelmintics
    • A61P33/12Schistosomicides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring systems containing three or more rings
    • C07D209/58[b]- or [c]-condensed
    • C07D209/60Naphtho [b] pyrroles; Hydrogenated naphtho [b] pyrroles
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Profármacos de análogos del antibiotico CC-1065 antitumoral que tiene un grupo protector escindible que contiene un ácido sulfonico que contiene carbamato de fenilo, en los que el grupo protector confiere mayor solubilidad en agua respecto al profármaco, y en los que el profármaco también tiene un resto tal como un sulfuro o un disulfuro, que pueden conjugarse a un reactivo de union a células tal como un anticuerpo. El uso terapéutico de tales conjugados profármacos se describe también; tales profármacos de agentes citotoxicos tienen uso terapéutico porque pueden liberar profármacos citotoxicos a una poblacion celular específica para conversion enzimática a fármacos citotoxicos de una manera dirigida. Reivindicacion 2: Un profármaco de acuerdo con la reivindicacion 1, en donde el análogo de CC-1065 se selecciona del grupo consistente en análogos formados a partir de una primera subunidad de formula (1) covalentemente enlazada a una segunda subunidad de la formula (2), (3), (4), (5), (6), (7), (8), (9), (10) o (11) a través de un enlace amida desde el grupo amino secundario del resto pirrolico de la primera subunidad al carboxilo C-2 de la segunda subunidad, en las que Y representa un grupo eliminable seleccionado de un haluro (fluoruro, cloruro, bromuro o yoduro), metanosulfonato, para-toluenosulfonato, trifluorometanosulfonato, mononitro- o dinitrofenolato; en donde R, R', R1-R6 son cada uno independientemente hidrogeno, alquilo C1-3 lineal, metoxi, hidroxilo, amino primario, amino secundario, amino terciario, o amido o un enlazador que proporciona enlace del profármaco a un agente de union a células, con tal de que al menos uno de R, R', R1-R6 sea un enlazador y en donde R7 es dicho grupo protector de ácido sulfonico que contiene carbamato, o sus sales farmacéuticamente aceptables, hidratos, o sales hidratadas, o las estructuras cristalinas polimorficas de estos compuestos o sus isomeros opticos, racematos, diastereoisomeros o enantiomeros.
ARP070100932A 2006-03-07 2007-03-06 Profarmacos de analogos de cc-1065 y sus conjugados, un procedimiento para su preparacion, una composicion farmaceutica que lo comprende y el uso de estos para la fabricacion de un medicamento para el tratamiento del cancer. AR059767A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP06290379A EP1832577A1 (en) 2006-03-07 2006-03-07 Improved prodrugs of CC-1065 analogs

Publications (1)

Publication Number Publication Date
AR059767A1 true AR059767A1 (es) 2008-04-30

Family

ID=36679356

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070100932A AR059767A1 (es) 2006-03-07 2007-03-06 Profarmacos de analogos de cc-1065 y sus conjugados, un procedimiento para su preparacion, una composicion farmaceutica que lo comprende y el uso de estos para la fabricacion de un medicamento para el tratamiento del cancer.

Country Status (18)

Country Link
US (2) US8012978B2 (es)
EP (2) EP1832577A1 (es)
JP (1) JP2009529030A (es)
KR (1) KR20080106919A (es)
AR (1) AR059767A1 (es)
AU (1) AU2007222123A1 (es)
BR (1) BRPI0708654A2 (es)
CA (1) CA2642870A1 (es)
DO (1) DOP2007000041A (es)
EA (1) EA200870327A1 (es)
IL (1) IL193673A0 (es)
MA (1) MA30322B1 (es)
MX (1) MX2008011431A (es)
NO (1) NO20083910L (es)
PE (1) PE20080691A1 (es)
TW (1) TW200813028A (es)
UY (1) UY30190A1 (es)
WO (1) WO2007102069A1 (es)

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US9901567B2 (en) 2007-08-01 2018-02-27 Syntarga B.V. Substituted CC-1065 analogs and their conjugates
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US20090155289A1 (en) * 2007-11-01 2009-06-18 Steve Roberts Furin-cleavable peptide linkers for drug-ligand conjugates
EP2344478B1 (en) 2008-11-03 2017-09-27 Syntarga B.V. Cc-1065 analogs and their conjugates
FR2947269B1 (fr) 2009-06-29 2013-01-18 Sanofi Aventis Nouveaux composes anticancereux
FR2949469A1 (fr) 2009-08-25 2011-03-04 Sanofi Aventis Derives anticancereux, leur preparation et leur application en therapeutique
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CA2991973C (en) 2015-07-12 2021-12-07 Suzhou M-Conj Biotech Co., Ltd. Bridge linkers for conjugation of a cell-binding molecule
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TW201808336A (zh) 2016-05-11 2018-03-16 賽諾菲公司 用抗muc1類美登素免疫綴合物抗體治療腫瘤的治療方案
WO2017197045A1 (en) 2016-05-11 2017-11-16 Movassaghi Mohammad Convergent and enantioselective total synthesis of communesin analogs
KR20220150408A (ko) 2016-11-14 2022-11-10 항저우 디에이씨 바이오테크 씨오, 엘티디 결합 링커, 그러한 결합 링커를 함유하는 세포 결합 분자-약물 결합체, 링커를 갖는 그러한 결합체의 제조 및 사용
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Also Published As

Publication number Publication date
WO2007102069A1 (en) 2007-09-13
BRPI0708654A2 (pt) 2011-06-07
JP2009529030A (ja) 2009-08-13
EP1993999A1 (en) 2008-11-26
MX2008011431A (es) 2008-09-22
MA30322B1 (fr) 2009-04-01
DOP2007000041A (es) 2007-10-31
AU2007222123A1 (en) 2007-09-13
EA200870327A1 (ru) 2009-02-27
UY30190A1 (es) 2008-10-31
IL193673A0 (en) 2009-05-04
PE20080691A1 (es) 2008-06-04
NO20083910L (no) 2008-12-01
CA2642870A1 (en) 2007-09-13
US8012978B2 (en) 2011-09-06
US20110280890A1 (en) 2011-11-17
KR20080106919A (ko) 2008-12-09
EP1832577A1 (en) 2007-09-12
US20090028821A1 (en) 2009-01-29
TW200813028A (en) 2008-03-16

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