KR970027079A - (r)-(-)-2-{n-[4-(1,1-디옥시도-3-옥소-2,3-디히드로-벤즈이소티아졸-2-일)-부틸]-아미노메틸}-크로만의 결정성 염산염 - Google Patents

(r)-(-)-2-{n-[4-(1,1-디옥시도-3-옥소-2,3-디히드로-벤즈이소티아졸-2-일)-부틸]-아미노메틸}-크로만의 결정성 염산염 Download PDF

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Publication number
KR970027079A
KR970027079A KR1019960056088A KR19960056088A KR970027079A KR 970027079 A KR970027079 A KR 970027079A KR 1019960056088 A KR1019960056088 A KR 1019960056088A KR 19960056088 A KR19960056088 A KR 19960056088A KR 970027079 A KR970027079 A KR 970027079A
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crystalline hydrochloride
hydrochloride according
crystalline
variant
spectral data
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KR1019960056088A
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English (en)
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알폰스 그루넨베르크
올리버 브렘
미카엘 콘라트
디트리히 자이델
Original Assignee
권터 슈마허, 클라우스 로이터
바이엘 악티엔게젤샤프트
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Publication of KR970027079A publication Critical patent/KR970027079A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

본 발명은 상온에서 안정한 형태로 존재하는 결정 형태의 (R)-(-)-2-{N-[4-(1,1-디옥시도-3-옥소-2,3-디히드로-벤즈이소티아졸-2-일)-부틸]-아미노메틸}-크로만 화합물의 염산염에 관한 것이다. DBCH의 결정성 변형체 II 는 준안정성이고 높은 습도에서 부분 전환을 하기 때문에, 제약학상 제제의 용도에서 제한적으로만 적용되었다. 본 발명에 따른 염산염의 결정성 변형체 V는 열역학적으로 안정하고 높은 대기습도에서도 전환되지 않아서 고형 약물, 특히 신경 퇴화치료를 위한 약물의 제조에 적합하다.

Description

(R)-(-)-2-{N-[4-(1,1-디옥시도-3-옥소-2,3-디히드로-벤즈이소티아졸-2-일)-부틸]-아미노메틸}-크로만의 결정성 염산염
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. (R)-(-)-2-{N-[4-(1,1-디옥시도-3-옥소-2,3-디히드로-벤즈이소티아졸-2-일)-부틸]-아미노메틸}-크로만의 화합물의 염산염
  2. 제1항에 있어서, 약 60℃에서 24J/g의 전이열로 전이하는 결정성 염산염.
  3. 제1 또는 제2항에 있어서, 표(1)의 X선 회절 데이타에 의해 특징되는 결정성 염산염.
    <표1>
  4. 제1 내지 제3항 중 어느 한 항에 있어서, 표(2)의 IR스펙트럼 데이타에 의해 특징되는 결정성 염산염.
  5. 제1내지 제4항 중 어느 한 항에 있어서, 표(3)의 고체상13C-NMR 스펙트럼 데이타에 의해 특징되는 결정성 염산염.
    (표3)
  6. 제1내지 제5항 중 어느 한 항에 있어서, 표(4)의 FIR 스펙트럼 데이타에 의해 특징되는 결정성 염산염.
    표(4)
  7. 제1내지 제6항 중 어느 한 항에 있어서, 표(5)의 라만 스펙트럼 데이타에 의해 특징되는 결정성 염산염.
    표(5)
  8. 변형체 II의 DBCH를 물 또는 불활성 유기 물질에 현탁시켜 청구항 제1 내지 제7항 중 어느 한 항에 따른 변형체 V로 양적으로 전환시키는 것을 특징으로 하는 청구항 제7에 따른 결정성 염산염의 제조 방법.
  9. 제1 내지 제7항 중 어느 한 항에 따른 결정성 염산염을 함유하는 약물.
  10. 약물 제조에 있어서의 제1 내지 제6항 중 어느 한 항에 따른 결정성 염산염의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960056088A 1995-11-22 1996-11-21 (r)-(-)-2-{n-[4-(1,1-디옥시도-3-옥소-2,3-디히드로-벤즈이소티아졸-2-일)-부틸]-아미노메틸}-크로만의 결정성 염산염 KR970027079A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19543478.1 1995-11-22
DE19543478A DE19543478A1 (de) 1995-11-22 1995-11-22 Kristallines Hydrochlorid von {(R)-(-)-2- N-[4-(1,1-Dioxido-3-oxo-2,3-dihydrobenzisothiazol-2-yl)-buytl]-aminomethyl}-chroman

Publications (1)

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KR970027079A true KR970027079A (ko) 1997-06-24

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US (1) US5830908A (ko)
EP (1) EP0775704B1 (ko)
JP (1) JPH09143180A (ko)
KR (1) KR970027079A (ko)
CN (1) CN1086703C (ko)
AR (1) AR004961A1 (ko)
AT (1) ATE201872T1 (ko)
AU (1) AU712922B2 (ko)
BR (1) BR9605646A (ko)
CA (1) CA2190700A1 (ko)
CZ (1) CZ289730B6 (ko)
DE (2) DE19543478A1 (ko)
DK (1) DK0775704T3 (ko)
EE (1) EE9600183A (ko)
ES (1) ES2159342T3 (ko)
GR (1) GR3036505T3 (ko)
HU (1) HUP9603237A3 (ko)
IL (1) IL119647A (ko)
MX (1) MX9605741A (ko)
MY (1) MY132473A (ko)
NO (1) NO307340B1 (ko)
NZ (1) NZ299780A (ko)
PL (1) PL317090A1 (ko)
PT (1) PT775704E (ko)
RU (1) RU2181723C2 (ko)
SG (1) SG44989A1 (ko)
SI (1) SI0775704T1 (ko)
SK (1) SK150096A3 (ko)
TR (1) TR199600930A2 (ko)
TW (1) TW449595B (ko)
UA (1) UA45338C2 (ko)
ZA (1) ZA969753B (ko)

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BRPI0916997A2 (pt) 2008-08-06 2020-12-15 Boehringer Ingelheim International Gmbh Inibidor de dpp-4 e seu uso
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
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CN1086703C (zh) 2002-06-26
NO964950L (no) 1997-05-23
CN1152574A (zh) 1997-06-25
ZA969753B (en) 1997-03-25
IL119647A0 (en) 1997-02-18
NO964950D0 (no) 1996-11-21
HU9603237D0 (en) 1997-01-28
PT775704E (pt) 2001-09-28
PL317090A1 (en) 1997-05-26
DE59607040D1 (de) 2001-07-12
ES2159342T3 (es) 2001-10-01
SK150096A3 (en) 1997-08-06
BR9605646A (pt) 1998-08-18
NO307340B1 (no) 2000-03-20
HUP9603237A3 (en) 1998-12-28
MX9605741A (es) 1997-05-31
NZ299780A (en) 1998-09-24
CA2190700A1 (en) 1997-05-23
SI0775704T1 (en) 2001-08-31
GR3036505T3 (en) 2001-11-30
EP0775704A1 (de) 1997-05-28
DE19543478A1 (de) 1997-05-28
AU7177296A (en) 1997-05-29
SG44989A1 (en) 1997-12-19
JPH09143180A (ja) 1997-06-03
EE9600183A (et) 1997-06-16
RU2181723C2 (ru) 2002-04-27
CZ289730B6 (cs) 2002-03-13
ATE201872T1 (de) 2001-06-15
US5830908A (en) 1998-11-03
IL119647A (en) 1999-12-22
EP0775704B1 (de) 2001-06-06
AR004961A1 (es) 1999-04-07
TW449595B (en) 2001-08-11
HUP9603237A2 (hu) 1998-01-28
DK0775704T3 (da) 2001-07-23
MY132473A (en) 2007-10-31
CZ342896A3 (en) 1997-06-11
UA45338C2 (uk) 2002-04-15
AU712922B2 (en) 1999-11-18
TR199600930A2 (tr) 1997-06-21

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