KR950016727A - 트롬보모듈린 발현을 증가시키는 방법 - Google Patents

트롬보모듈린 발현을 증가시키는 방법 Download PDF

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Publication number
KR950016727A
KR950016727A KR1019940034918A KR19940034918A KR950016727A KR 950016727 A KR950016727 A KR 950016727A KR 1019940034918 A KR1019940034918 A KR 1019940034918A KR 19940034918 A KR19940034918 A KR 19940034918A KR 950016727 A KR950016727 A KR 950016727A
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South Korea
Prior art keywords
compound
formula
hydrochloride salt
pyrrolidino
piperidino
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KR1019940034918A
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English (en)
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스코트 칼네크 데이비드
윌리암 그리넬 브라이언
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피터 지. 스트링거
일라이 릴리 앤드 캄파니
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Publication of KR950016727A publication Critical patent/KR950016727A/ko

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    • 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
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • 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
    • A61K31/40—Heterocyclic 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
    • 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
    • A61K31/40—Heterocyclic 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
    • A61K31/4025—Heterocyclic 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic 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

Abstract

본 발명은 치료를 필요로 하는 인간에게 효과량의 하기 일반식(I)의 화합물, 또는 그의 약학적으로 허용가능한 염 및 용매화물을 투여함을 포함하는, 트롬보모듈린 발현을 증가시키는 방법을 제공한다:
상기식에서,
R1및 R3는 독립적으로 수소, -CH3,(여기에서, Ar은 임의적으로 치환된 페닐이며; R2는 피롤리디노, 헥사메틸렌이미노 및 피페리디노로 이루어진 군으로부터 선택된다.
또한 본 발명에 포함되는 것은 일반식(I)의 화합물 효과량을 필요로 하는 인간에게 투여함을 포함하는, 혈전 질환 또는 장애를 억제하는 방법이다. 또한 본 발명에 포함되는 것은 일반식(I)의 화합물을 투여함을 포함하는, 단백질 C 활성화 속도를 증가시키는 방법이다.

Description

트롬보모듈린 발현을 증가시키는 방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 트롬보모듈린 발현을 증가시키는데 사용하기 위한 하기 일반식(I)의 화합물; 또는 그의 약학적으로 허용가능한 염 또는 용매화물:
    상기식에서,
    R1및 R3는 독립적으로 수소, -CH3,(여기에서, Ar은 임의적으로 치환된 페닐이며; R2는 피롤리디노 및 피페리디노로 이루어진 군으로부터 선택된다.
  2. 제1항에 있어서, 상기 화합물이 그의 하이드로클로라이드 염인 화합물.
  3. 제1항에 있어서, 예방 목적으로 투여하는 화합물.
  4. 제1항에 있어서, 상기 화합물이 하기 화합물 또는 그의 하이드로클로라이드 염인 화합물:
  5. 혈전 질환 또는 장애를 저해하는데 사용하기 위한 하기 일반식(I)의 화합물; 또는 그의 약학적으로 허용가능한 염 또는 용매화물:
    상기식에서,
    R1및 R3는 독립적으로 수소, -CH3,(여기에서, Ar은 임의적으로 치환된 페닐이며; R2는 피롤리디노 및 피페리디노로 이루어진 군으로부터 선택된다.
  6. 제5항에 있어서, 상기 화합물이 그의 하이드로클로라이드 염인 화합물.
  7. 제5항에 있어서, 예방 목적으로 투여하는 화합물,
  8. 제5항에 있어서, 상기 화합물이 하기 화합물 또는 그의 하이드로클로라이드 염인 화합물:
  9. 단백질 C 활성화를 중가시키는데 사용하기 위한 하기 일반식(I)의 화합물, 또는 그의 약학적으로 허용가능한 염 또는 용매화물:
    상기식에서,
    R1및 R3는 독립적으로 수소, -CH3,(여기에서, Ar은 임의적으로 치환된 페닐이며; R2는 피롤리디노 및 피페리디노로 이루어진 군으로부터 선택된다.
  10. 제9항에 있어서, 상기 화합물이 그의 하이드로클로라이드 염인 화합물.
  11. 제9항에 있어서, 예방 목적으로 투여하는 화합물.
  12. 제9항에 있어서, 상기 화합물이 하기 화합물 또는 그외 하이드로클로라이드 염인 화합물:
    ※ 참고사항 :최초출원 내용에 의하여 공개하는 것임.
KR1019940034918A 1993-12-21 1994-12-19 트롬보모듈린 발현을 증가시키는 방법 KR950016727A (ko)

Applications Claiming Priority (2)

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US08/170,944 US5476862A (en) 1993-12-21 1993-12-21 Methods of increasing thrombomodulin expression
US08/170,944 1993-12-21

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US (2) US5476862A (ko)
EP (1) EP0659427B1 (ko)
JP (1) JPH07196496A (ko)
KR (1) KR950016727A (ko)
CN (1) CN1044679C (ko)
AT (1) ATE220904T1 (ko)
AU (1) AU692194B2 (ko)
CA (1) CA2138490A1 (ko)
CZ (1) CZ288983B6 (ko)
DE (1) DE69431035T2 (ko)
DK (1) DK0659427T3 (ko)
ES (1) ES2180564T3 (ko)
HU (1) HUT71470A (ko)
IL (1) IL112036A (ko)
NO (1) NO310596B1 (ko)
NZ (1) NZ270169A (ko)
PH (1) PH31325A (ko)
PT (1) PT659427E (ko)
RU (2) RU2125450C1 (ko)
TW (1) TW273509B (ko)
UA (1) UA27910C2 (ko)
ZA (1) ZA9410079B (ko)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5492927A (en) * 1993-12-21 1996-02-20 Eli Lilly And Company Non-peptide tachykinin receptor antagonists to treat allergy
US6562862B1 (en) 1994-10-20 2003-05-13 Eli Lilly And Company Methods of inhibiting physiological conditions associated with an excess of neuropeptide Y
US5484808A (en) * 1995-02-09 1996-01-16 Eli Lilly And Company Methods of inhibiting cell-cell adhesion
US5843974A (en) * 1995-06-06 1998-12-01 Eli Lilly And Company Methods of inhibiting melanoma using Benzothiophenes as cytotoxic agents per se
US6545027B1 (en) 1995-06-07 2003-04-08 Eli Lilly And Company Methods of modulating NF-kB transcription factor
DE69622472T2 (de) * 1995-06-07 2003-02-06 Lilly Co Eli Behandlung von Krankheiten durch Induktion von BEF-1 Transkriptionsfaktor
IL120266A (en) 1996-02-28 2005-05-17 Pfizer Use of estrogen antagonists and estrogen agonists in the preparation of medicaments for inhibiting pathological conditions
TW442286B (en) * 1996-02-28 2001-06-23 Pfizer New therapeutic uses of estrogen agonists
US6025373A (en) * 1997-04-22 2000-02-15 Eli Lilly And Company Methods for reducing fibrinogen
US6103740A (en) * 1997-08-21 2000-08-15 Eli Lilly And Company Methods for lowering platelet counts
US7189703B2 (en) * 1998-01-09 2007-03-13 Intracell, Llc Treatment and diagnosis of alzheimer's disease
FR2777784B1 (fr) * 1998-04-27 2004-03-19 Arepa Composition pharmaceutique a base d'estrogene et de progesterone
US6353003B1 (en) * 1998-06-17 2002-03-05 Eli Lilly And Company Method for reducing levels of homocysteine and C-reactive protein
AU777770C (en) 1999-05-04 2005-11-10 Strakan International Limited Androgen glycosides and androgenic activity thereof
AU2001292308A1 (en) * 2000-09-30 2002-04-15 Mochida Pharmaceutical Co., Ltd. Preventives/remedies for hemolytic anemia
US20060148695A1 (en) * 2005-01-03 2006-07-06 National Cheng Kung University Novel angiogenic composition and use thereof
CA2680737C (en) * 2007-03-21 2015-12-15 Emisphere Technologies, Inc. Allyloxy and alkyloxy benzoic acid delivery agents

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* Cited by examiner, † Cited by third party
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US4133814A (en) * 1975-10-28 1979-01-09 Eli Lilly And Company 2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents
US4418068A (en) * 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
US4380635A (en) * 1981-04-03 1983-04-19 Eli Lilly And Company Synthesis of acylated benzothiophenes
US5075321A (en) * 1987-03-24 1991-12-24 University Of Pennsylvania Methods of treating diseases characterized by interactions of IgG-containing immune complexes with macrophage Fc receptors using antiestrogenic benzothiophenes
JP3157882B2 (ja) * 1991-11-15 2001-04-16 帝国臓器製薬株式会社 新規なベンゾチオフエン誘導体
AU672182B2 (en) * 1991-11-27 1996-09-26 Novo Nordisk A/S Piperidine derivatives and their use in treating psychosis

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DE69431035D1 (de) 2002-08-29
TW273509B (en) 1996-04-01
AU8155494A (en) 1995-06-29
CN1108932A (zh) 1995-09-27
HU9403664D0 (en) 1995-02-28
CN1044679C (zh) 1999-08-18
HUT71470A (en) 1995-11-28
CA2138490A1 (en) 1995-06-22
DK0659427T3 (da) 2002-09-02
NZ270169A (en) 1997-07-27
IL112036A (en) 1999-01-26
RU2190405C2 (ru) 2002-10-10
NO944915D0 (no) 1994-12-19
NO310596B1 (no) 2001-07-30
AU692194B2 (en) 1998-06-04
US5700815A (en) 1997-12-23
PH31325A (en) 1998-07-06
PT659427E (pt) 2002-11-29
ZA9410079B (en) 1996-06-19
EP0659427B1 (en) 2002-07-24
ES2180564T3 (es) 2003-02-16
US5476862A (en) 1995-12-19
RU2125450C1 (ru) 1999-01-27
RU94044356A (ru) 1996-10-10
CZ321194A3 (en) 1995-08-16
CZ288983B6 (cs) 2001-10-17
NO944915L (no) 1995-06-22
ATE220904T1 (de) 2002-08-15
JPH07196496A (ja) 1995-08-01
DE69431035T2 (de) 2003-01-30
IL112036A0 (en) 1995-03-15
EP0659427A1 (en) 1995-06-28
UA27910C2 (uk) 2000-10-16

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