KR950016744A - 트롬빈을 저해하는 방법 - Google Patents

트롬빈을 저해하는 방법 Download PDF

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Publication number
KR950016744A
KR950016744A KR1019940034935A KR19940034935A KR950016744A KR 950016744 A KR950016744 A KR 950016744A KR 1019940034935 A KR1019940034935 A KR 1019940034935A KR 19940034935 A KR19940034935 A KR 19940034935A KR 950016744 A KR950016744 A KR 950016744A
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South Korea
Prior art keywords
compound
formula
hydrochloride salt
pyrrolidino
piperidino
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KR1019940034935A
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English (en)
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존 살 다니엘
플로이드 스미쓰 제랄드
Original Assignee
피터 지. 스트링거
일라이 릴리 앤드 캄파니
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Publication of KR950016744A publication Critical patent/KR950016744A/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
    • A61K31/395—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

본 발명은 치료를 필요로 하는 인간에게 효과량의 하기 일반식( I )의 화합물, 또는 그의 약학적으로 허용가능한 염 또는 용매화물을 투여함을 포함하는, 트롬빈 및 그에 수반되는 질병 및 증상을 억제하는 방법을 제공한다 :
상기식에서,
R1및 R3는 독립적으로 수소,이고, 여기에서, Ar은 임의로 치환된 페닐이며; R2는 피롤리디노, 헥사메틸렌이미노 및 피페리디노로 이루어진 군으로부터 선택된다.

Description

트롬빈을 저해하는 방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (8)

  1. 트롬빈을 저해하는데 사용하기 위한 하기 일반식( I )의 화합물; 또는 그의 약학적으로 허용가능한 염 또는 용매화물:
    상기식에서,
    R1및 R3는 독립적으로 수소,이고, 여기에서, Ar은 임의로 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. 트롬빈을 저해해야 하는 질병 또는 중상을 억제하는데 사용하기 위한 하기 일반식( I )의 화합물; 또는 그의 약학적으로 허용가능한 염 또는 용매화물:
    상기식에서,
    R1및 R3는 독립적으로 수소,이고, 여기에서, Ar은 임의로 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:
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940034935A 1993-12-21 1994-12-19 트롬빈을 저해하는 방법 KR950016744A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/171,394 US5441965A (en) 1993-12-21 1993-12-21 Methods of inhibiting thrombin
US08/171,394 1993-12-21

Publications (1)

Publication Number Publication Date
KR950016744A true KR950016744A (ko) 1995-07-20

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US (3) US5441965A (ko)
EP (1) EP0664126B1 (ko)
JP (1) JPH07223947A (ko)
KR (1) KR950016744A (ko)
CN (1) CN1078070C (ko)
AT (1) ATE150308T1 (ko)
AU (1) AU693822B2 (ko)
CA (1) CA2138493A1 (ko)
CZ (1) CZ287725B6 (ko)
DE (1) DE69402173T2 (ko)
DK (1) DK0664126T3 (ko)
ES (1) ES2102154T3 (ko)
GR (1) GR3023537T3 (ko)
HU (1) HU224915B1 (ko)
IL (1) IL112048A (ko)
NO (1) NO313081B1 (ko)
NZ (1) NZ270185A (ko)
RU (1) RU94045846A (ko)
TW (1) TW321601B (ko)
UA (1) UA29446C2 (ko)
ZA (1) ZA9410084B (ko)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6515009B1 (en) 1991-09-27 2003-02-04 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US5811447A (en) 1993-01-28 1998-09-22 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US5770609A (en) 1993-01-28 1998-06-23 Neorx Corporation Prevention and treatment of cardiovascular pathologies
US6395494B1 (en) 1993-05-13 2002-05-28 Neorx Corporation Method to determine TGF-β
US6251920B1 (en) 1993-05-13 2001-06-26 Neorx Corporation Prevention and treatment of cardiovascular pathologies
US6491938B2 (en) 1993-05-13 2002-12-10 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US5595722A (en) 1993-01-28 1997-01-21 Neorx Corporation Method for identifying an agent which increases TGF-beta levels
US6197789B1 (en) 1995-06-07 2001-03-06 Neorx Corporation Prevention and treatment of cardiovascular pathologies with tamoxifen analogues
ATE406909T1 (de) 1993-05-13 2008-09-15 Poniard Pharmaceuticals Inc Prävention und behandlung von pathologien, die mit einer abnormalen proliferationglatter muskelzellen verbunden sind
US6562862B1 (en) 1994-10-20 2003-05-13 Eli Lilly And Company Methods of inhibiting physiological conditions associated with an excess of neuropeptide Y
US5545641A (en) * 1994-10-20 1996-08-13 Eli Lilly And Company Methods of inhibiting physiological conditions associated with an excess of bradykinin
US5484808A (en) * 1995-02-09 1996-01-16 Eli Lilly And Company Methods of inhibiting cell-cell adhesion
ES2180702T3 (es) * 1995-06-07 2003-02-16 Lilly Co Eli Tratamiento de patologias por la induccion del factor de transcripcion bef-1.
US6545027B1 (en) * 1995-06-07 2003-04-08 Eli Lilly And Company Methods of modulating NF-kB transcription factor
US5840747A (en) * 1995-06-07 1998-11-24 Eli Lilly And Company Calcium channel antagonists
JP2002500618A (ja) 1995-10-31 2002-01-08 イーライ・リリー・アンド・カンパニー 抗血栓性ジアミン
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
US5811437A (en) * 1996-05-21 1998-09-22 Eli Lilly And Company Methods of increasing nitric oxide synthesis
US5747509A (en) * 1996-06-03 1998-05-05 Schering Aktiengesellschaft Method for lowering plasma levels of lipoprotein(a)
ZA982877B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Treatment of central nervous system disorders with selective estrogen receptor modulators.
US6025373A (en) * 1997-04-22 2000-02-15 Eli Lilly And Company Methods for reducing fibrinogen
WO1998049161A1 (en) 1997-04-30 1998-11-05 Eli Lilly And Company Antithrombotic agents
WO1998049160A1 (en) 1997-04-30 1998-11-05 Eli Lilly And Company Antithrombotic agents
AU7170898A (en) 1997-04-30 1998-11-24 Eli Lilly And Company Antithrombotic agents
CA2288224A1 (en) 1997-04-30 1998-11-05 Mary George Johnson Antithrombotic agents
US6103740A (en) * 1997-08-21 2000-08-15 Eli Lilly And Company Methods for lowering platelet counts
US6187777B1 (en) 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases
TR200002855T2 (tr) * 1998-04-08 2000-12-21 Eli Lilly And Company Raloksifenin solunum yolu ile veya burundan uygulanması.
FR2777784B1 (fr) * 1998-04-27 2004-03-19 Arepa Composition pharmaceutique a base d'estrogene et de progesterone
US6284756B1 (en) 1998-04-30 2001-09-04 Eli Lilly And Company Antithrombotic agents
TR200003704T2 (tr) 1998-06-16 2001-06-21 Eli Lilly And Company Asetilkolin düzeylerini arttırma
US6288108B1 (en) 1998-06-16 2001-09-11 Eli Lilly And Company Methods for increasing levels of acetylcholine
US6353003B1 (en) 1998-06-17 2002-03-05 Eli Lilly And Company Method for reducing levels of homocysteine and C-reactive protein
EP0997460B1 (en) * 1998-10-28 2002-12-11 Eli Lilly And Company Benzothiophene compounds as antithrombotic agents and intermediates
PT1175433E (pt) 1999-05-04 2005-11-30 Strakan Int Ltd Glicosidos androgenos e sua actividade androgenica
JP3887588B2 (ja) * 2002-08-30 2007-02-28 株式会社リガク Ｘ線回折による応力測定法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US5395842A (en) * 1988-10-31 1995-03-07 Endorecherche Inc. Anti-estrogenic compounds and compositions
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

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US5688813A (en) 1997-11-18
JPH07223947A (ja) 1995-08-22
NO944932D0 (no) 1994-12-19
TW321601B (ko) 1997-12-01
AU8155894A (en) 1995-06-29
DK0664126T3 (da) 1997-09-01
HU9403675D0 (en) 1995-02-28
UA29446C2 (uk) 2000-11-15
IL112048A (en) 1999-03-12
US5508292A (en) 1996-04-16
DE69402173T2 (de) 1997-07-17
HUT71344A (en) 1995-11-28
GR3023537T3 (en) 1997-08-29
ES2102154T3 (es) 1997-07-16
NO944932L (no) 1995-06-22
RU94045846A (ru) 1996-10-20
ATE150308T1 (de) 1997-04-15
CN1107704A (zh) 1995-09-06
HU224915B1 (en) 2006-04-28
CN1078070C (zh) 2002-01-23
CZ287725B6 (en) 2001-01-17
ZA9410084B (en) 1996-06-19
US5441965A (en) 1995-08-15
NZ270185A (en) 1997-07-27
NO313081B1 (no) 2002-08-12
DE69402173D1 (de) 1997-04-24
IL112048A0 (en) 1995-03-15
EP0664126A1 (en) 1995-07-26
AU693822B2 (en) 1998-07-09
CA2138493A1 (en) 1995-06-22
CZ322694A3 (en) 1995-09-13
EP0664126B1 (en) 1997-03-19

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