CA2379676A1 - Conception de stabilisateurs de polymerisation de la tubuline - Google Patents

Conception de stabilisateurs de polymerisation de la tubuline Download PDF

Info

Publication number
CA2379676A1
CA2379676A1 CA002379676A CA2379676A CA2379676A1 CA 2379676 A1 CA2379676 A1 CA 2379676A1 CA 002379676 A CA002379676 A CA 002379676A CA 2379676 A CA2379676 A CA 2379676A CA 2379676 A1 CA2379676 A1 CA 2379676A1
Authority
CA
Canada
Prior art keywords
group
substituted
acid
chain
derivatives
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.)
Abandoned
Application number
CA002379676A
Other languages
English (en)
Inventor
David C. Young
Dorit Arad
Arthur P. Bollon
Bradley W. Poland
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.)
Individual
Original Assignee
Cytoclonal Pharmaceutics Inc
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 Cytoclonal Pharmaceutics Inc filed Critical Cytoclonal Pharmaceutics Inc
Publication of CA2379676A1 publication Critical patent/CA2379676A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/58—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/81—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/82—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/87—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/14—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/36—Systems containing two condensed rings the rings having more than two atoms in common
    • C07C2602/44—Systems containing two condensed rings the rings having more than two atoms in common the bicyclo ring system containing eight carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

L'invention concerne un procédé permettant la conception de composés de remplacement du paclitaxel, qui stabilisent le processus de polymérisation de la tubuline. Ces composés en solution présentent les caractéristiques de conformation stérique du paclitaxel naturel et sont capables de se fixer à la protéine de tubuline au même site de liaison que le paclitaxel. Ces composés stabilisent la polymérisation de la tubuline par un mécanisme correspondant au mécanisme d'activité du paclitaxel. Comparés au paclitaxel naturel, ces composés présentent une solubilité accrue, sont plus faciles à synthétiser et offrent des possibilités de réactions combinatoires permettant une spécificité et d'une optimisation.
CA002379676A 1999-07-15 2000-07-17 Conception de stabilisateurs de polymerisation de la tubuline Abandoned CA2379676A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US14397399P 1999-07-15 1999-07-15
US60/143,973 1999-07-15
US17189299P 1999-12-23 1999-12-23
US60/171,892 1999-12-23
PCT/US2000/019524 WO2001005779A2 (fr) 1999-07-15 2000-07-17 Conception de stabilisateurs de polymerisation de la tubuline

Publications (1)

Publication Number Publication Date
CA2379676A1 true CA2379676A1 (fr) 2001-01-25

Family

ID=26841562

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002379676A Abandoned CA2379676A1 (fr) 1999-07-15 2000-07-17 Conception de stabilisateurs de polymerisation de la tubuline

Country Status (4)

Country Link
EP (1) EP1198461A2 (fr)
AU (1) AU6108300A (fr)
CA (1) CA2379676A1 (fr)
WO (1) WO2001005779A2 (fr)

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4349552A (en) * 1978-10-30 1982-09-14 Fujisawa Pharmaceutical Company, Ltd. 5-Fluorouracil derivatives, and their pharmaceutical compositions
EP0655053B1 (fr) * 1992-06-19 1997-09-03 James Black Foundation Limited Derives de bicyclooctane et bicycloheptane
US5302589A (en) * 1992-08-07 1994-04-12 Glaxo, Inc. Heterocyclic inhibitors of 5-α-testosterone reductase
US5658940A (en) * 1995-10-06 1997-08-19 Celgene Corporation Succinimide and maleimide cytokine inhibitors

Also Published As

Publication number Publication date
WO2001005779A2 (fr) 2001-01-25
EP1198461A2 (fr) 2002-04-24
WO2001005779A3 (fr) 2001-08-16
AU6108300A (en) 2001-02-05

Similar Documents

Publication Publication Date Title
Slee et al. Selectivity in the inhibition of HIV and FIV Protease: inhibitory and mechanistic studies of pyrrolidine-containing. alpha.-Keto amide and hydroxyethylamine core structures
RU2043346C1 (ru) Производные таксола и водорастворимые производные таксола
JPH1192468A (ja) 新規なタキサン誘導体
Fang et al. Recent progress in structure activity relationship and mechanistic studies of taxol analogues
CA2359561A1 (fr) Inhibiteurs de proteasome
Zhao et al. The conventional turns rather than irregular γ-/β-turn secondary structures accounting for the antitumor activities of cyclic peptide Phakellistatin 6 analogs
JP3759602B2 (ja) セファロマニンの酸化生成物
Wang et al. Design and discovery of novel dipeptide boronic acid ester proteasome inhibitors, an oral slowly-released prodrug for the treatment of multiple myeloma
Haberhauer et al. Synthesis of a second-generation pseudopeptide platform
Xu et al. Discovery and development of novel rhodanine derivatives targeting enoyl-acyl carrier protein reductase
Egbewande et al. The design, synthesis, and anti-inflammatory evaluation of a drug-like library based on the natural product valerenic acid
CA2379676A1 (fr) Conception de stabilisateurs de polymerisation de la tubuline
CN115010658B (zh) 一种化合物及其制备方法与应用
Bryans et al. An in vitro investigation into conformational aspects of gabapentin
JPH08176124A (ja) 新規な抗腫瘍性化合物
US9206201B2 (en) Boronic acid bearing liphagane compounds as inhibitors of P13K-α and/or β
FR2569696A1 (fr) Nouveaux analogues de la mitomycine, leur procede de preparation et leur application pharmaceutique
Faissat et al. New nitrogen mustards structurally related to (L)-carnitine
Debnath et al. QSAR Study on 5–N–Substituted–2–(Substituted Benzenesulphonyl) Glutamines as Antitumor Agents through Synthesis and Biological Evaluation: Part III, Internet Electron
CN116102534B (zh) 共价PARP PROTACs衍生物及其应用
CN113292627B (zh) Nqo1靶向的吲哚醌类23-羟基白桦酸衍生物、制备方法及用途
CN114605418B (zh) 一类具有抗肿瘤活性的依鲁替尼丙烯酰胺类衍生物及其合成方法与应用
JP7389809B2 (ja) 合成新規ピロロイミノキノンアルカロイド及び使用の方法
Altmann et al. On the Chemistry and Biology of the Marine Macrolides Zampanolide and Dactylolide
Fang et al. Structure modifications and their influences on antitumor and other related activities of taxol and its analogs

Legal Events

Date Code Title Description
FZDE Dead