KR960700230A - 다중-약물 내성종양 제제로서 유용한 디아릴알킬 피페리딘(Diarylalkyl piperidines useful as multi-drug resistant tumor agents) - Google Patents

다중-약물 내성종양 제제로서 유용한 디아릴알킬 피페리딘(Diarylalkyl piperidines useful as multi-drug resistant tumor agents)

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Publication number
KR960700230A
KR960700230A KR1019950702950A KR19950702950A KR960700230A KR 960700230 A KR960700230 A KR 960700230A KR 1019950702950 A KR1019950702950 A KR 1019950702950A KR 19950702950 A KR19950702950 A KR 19950702950A KR 960700230 A KR960700230 A KR 960700230A
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KR
South Korea
Prior art keywords
compound
hydrogen
group
drug resistant
trimethoxyphenyl
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KR1019950702950A
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English (en)
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KR100377280B1 (ko
Inventor
피.순카라 사이
프리드만 쥴스
Original Assignee
게리 디. 스트리트
메렐 다우 파마슈티칼즈 인코포레이티드
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Publication of KR960700230A publication Critical patent/KR960700230A/ko
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Publication of KR100377280B1 publication Critical patent/KR100377280B1/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/16—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

본 발명은, 다중 약물 내성 종양에서 약물 내성을 역전시키는 일반식(Ⅰ)의 디아릴알킬 피페리딘에 관한 것이다. 이들 화합물은, 말기 단계의 종양 발생중에 활성화되고 특정 기원의 종양중에 본질적으로 존재하는 p-당단백질 펌프를 억제함으로써 작용하게 된다.

Description

다중-약물 내성 종양 제제로서 유용한 디아릴아킬 피페리딘(Diarylalkyl piperidines useful as multi-drug resistant tumor agents)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (17)

  1. 하기 일반식(1)의 화합물.
  3. 상기식에서, m은 0,1 또는 2로 이루어진 그룹중에서 선택되는 정수이고, n은 0,1,2 또는 3으로 이루어진 그룹중에서 선택되는 정수이며, R1및 R2는 각각 독립적으로 수소, 할로겐, C1-C4알킬 또는 C1-C4알콕시로 이루어진 그룹중에서 선택되고, Ar은 C1-C4알킬, C1-C4알콕시, C1-C4알킬티오, 할로겐, OCH2O, CF3, OCF3, OH, CN, NO2및 NH2로 이루어진 그룹중에서 선택되는 1 내지 3개 치환체로 임의 치환된 페닐; 또는 인돌릴이다.
  4. 제1항에 있어서, m 및 n이 1이고, Ar이 3,4,5-트리메톡시페닐이며, R1및 R2가 수소인 화합물.
  5. 제1항에 있어서, m 및 n이 1이고, Ar이 3,4-메틸렌디옥시페닐이며, R1및 R2가 수소인 화합물.
  6. 제1항에 있어서, m이 1이고, n이 2이고, Ar이 3,4-디메톡시페닐이고, R1및 R2가 수소인 화합물.
  7. 제1항에 있어서, m이 0이고, n이 1이고, Ar이 3,4,5-트리메톡시페닐이고, R1및 R2가 수소인 화합물.
  8. 제1항에 있어서, m 및 n이 1이고, Ar이 2-메톡시페닐이며, R1및 R2가 수소인 화합물.
  9. 하기 일반식(1)의 화합물 유효량을 치료를 요하는 환자에게 투여함으로써 화학요법제에 대한 약물 내성종양의 감도(sensitivity)를 증가시키는 방법.
  11. 상기식에서, m은 0,1 또는 2로 이루어진 그룹중에서 선택되는 정수이고, n은 0,1,2 또는 3으로 이루어진 그룹중에서 선택되는 정수이며, R1및 R2는 각각 독립적으로 수소, 할로겐, C1-C4알킬 또는 C1-C4알콕시로 이루어진 그룹중에서 선택되고, Ar은 C1-C4알킬, C1-C4알콕시, C1-C4알킬티오, 할로겐, OCH2O, CF3, OCF3, OH, CN, NO2및 NH2로 이루어진 그룹중에서 선택되는 1 내지 3개 치환체로 임의 치환된 페닐; 또는 인돌릴이다.
  12. 제7항에 있어서, m 및 n이 1이고, Ar이 3,4,5-트리메톡시페닐이고, R1및 R2가 수소인 화합물.
  13. 제7항에 있어서, m 및 n이 1이고, Ar이 3,4-메틸렌디옥시페닐이며, R1및 R2가 수소인 화합물.
  14. 제7항에 있어서, m이 1이고, n이 2이고, Ar이 3,4-디메틸톡시페닐이고, R1및 R2가 수소인 화합물.
  15. 제7항에 있어서, m이 0이고, n이 1이고, Ar이 3,4,5-트리메톡시페닐이고, R1및 R2가 수소인 화합물.
  16. 제7항에 있어서, m 및 n이 1이고, Ar이 2-메톡시페닐이며, R1및 R2가 수소인 화합물.
  17. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950702950A 1993-01-21 1993-12-17 디아릴알킬피페리딘을함유하는다중-약물내성종양치료효력증강용약제학적조성물 KR100377280B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US656993A 1993-01-21 1993-01-21
US08/006569 1993-01-21

Publications (2)

Publication Number Publication Date
KR960700230A true KR960700230A (ko) 1996-01-19
KR100377280B1 KR100377280B1 (ko) 2003-07-18

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KR1019950702950A KR100377280B1 (ko) 1993-01-21 1993-12-17 디아릴알킬피페리딘을함유하는다중-약물내성종양치료효력증강용약제학적조성물

Country Status (20)

Country Link
US (1) US5648365A (ko)
EP (1) EP0680470B1 (ko)
JP (1) JP3398748B2 (ko)
KR (1) KR100377280B1 (ko)
AT (1) ATE150748T1 (ko)
AU (1) AU679723B2 (ko)
CA (1) CA2152794C (ko)
DE (1) DE69309310T2 (ko)
DK (1) DK0680470T3 (ko)
ES (1) ES2102830T3 (ko)
FI (1) FI112474B (ko)
GR (1) GR3023188T3 (ko)
HU (1) HUT72078A (ko)
IL (1) IL108369A (ko)
MX (1) MX9400563A (ko)
NO (1) NO305166B1 (ko)
NZ (1) NZ261414A (ko)
TW (1) TW243445B (ko)
WO (1) WO1994017040A1 (ko)
ZA (1) ZA94317B (ko)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2135463T3 (es) * 1992-02-06 1999-11-01 Merrell Pharma Inc Inversion de la resistencia multi-medicamento por medio de derivados de trifenil-piperidina.
AU6366000A (en) * 1999-07-23 2001-02-13 Colorado State University Research Foundation Multidrug resistance pump inhibitors and uses thereof
US6693099B2 (en) 2000-10-17 2004-02-17 The Procter & Gamble Company Substituted piperazine compounds optionally containing a quinolyl moiety for treating multidrug resistance
US20030109448A1 (en) * 2001-11-07 2003-06-12 Crowley Kathleen S. Methods of promoting uptake and nuclear accumulation of polyamides in eukaryotic cells
KR100656490B1 (ko) 2001-11-26 2006-12-12 삼성에스디아이 주식회사 풀칼라 유기전계 발광표시소자 및 그의 제조방법
US8153184B2 (en) * 2001-11-26 2012-04-10 Samsung Mobile Display Co., Ltd. Organic EL display device and method of manufacturing the same
DK3466930T3 (da) 2013-02-08 2022-09-05 Gen Mills Inc Fødevareprodukt med reduceret natriumindhold
CN110372571B (zh) * 2018-04-12 2022-11-15 中国科学院大连化学物理研究所 一种2-(2,2-二芳基乙基)-环胺衍生物或盐及合成和应用与组合物

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ES2135463T3 (es) * 1992-02-06 1999-11-01 Merrell Pharma Inc Inversion de la resistencia multi-medicamento por medio de derivados de trifenil-piperidina.

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Publication number Publication date
EP0680470B1 (en) 1997-03-26
NZ261414A (en) 1997-06-24
CA2152794A1 (en) 1994-08-04
ES2102830T3 (es) 1997-08-01
CA2152794C (en) 1999-04-06
WO1994017040A1 (en) 1994-08-04
IL108369A (en) 1999-08-17
GR3023188T3 (en) 1997-07-30
TW243445B (ko) 1995-03-21
IL108369A0 (en) 1994-04-12
JPH08505870A (ja) 1996-06-25
AU6014894A (en) 1994-08-15
NO952885D0 (no) 1995-07-20
US5648365A (en) 1997-07-15
MX9400563A (es) 1994-07-29
FI112474B (fi) 2003-12-15
DK0680470T3 (ko) 1997-04-28
ATE150748T1 (de) 1997-04-15
FI953506A (fi) 1995-07-20
DE69309310T2 (de) 1997-11-06
ZA94317B (en) 1994-08-18
EP0680470A1 (en) 1995-11-08
NO305166B1 (no) 1999-04-12
AU679723B2 (en) 1997-07-10
FI953506A0 (fi) 1995-07-20
HUT72078A (en) 1996-03-28
KR100377280B1 (ko) 2003-07-18
DE69309310D1 (de) 1997-04-30
HU9502195D0 (en) 1995-09-28
NO952885L (no) 1995-09-20
JP3398748B2 (ja) 2003-04-21

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