KR860004038A - 결정상 벤조티아진 디옥사이드 염의 제조방법 - Google Patents

결정상 벤조티아진 디옥사이드 염의 제조방법 Download PDF

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Publication number
KR860004038A
KR860004038A KR1019850008577A KR850008577A KR860004038A KR 860004038 A KR860004038 A KR 860004038A KR 1019850008577 A KR1019850008577 A KR 1019850008577A KR 850008577 A KR850008577 A KR 850008577A KR 860004038 A KR860004038 A KR 860004038A
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South Korea
Prior art keywords
solvent
polymorph
benzothiazine
dioxide
carboxamide
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KR1019850008577A
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English (en)
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KR870000291B1 (ko
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리 로버트슨 로버트
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터렌스 제이. 갈래거
화이자 인코포레이티드
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Publication of KR860004038A publication Critical patent/KR860004038A/ko
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/16—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • F—MECHANICAL ENGINEERING; LIGHTING; HEATING; WEAPONS; BLASTING
    • F16—ENGINEERING ELEMENTS AND UNITS; GENERAL MEASURES FOR PRODUCING AND MAINTAINING EFFECTIVE FUNCTIONING OF MACHINES OR INSTALLATIONS; THERMAL INSULATION IN GENERAL
    • F16L—PIPES; JOINTS OR FITTINGS FOR PIPES; SUPPORTS FOR PIPES, CABLES OR PROTECTIVE TUBING; MEANS FOR THERMAL INSULATION IN GENERAL
    • F16L57/00—Protection of pipes or objects of similar shape against external or internal damage or wear
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Engineering & Computer Science (AREA)
  • Engineering & Computer Science (AREA)
  • Health & Medical Sciences (AREA)
  • Mechanical Engineering (AREA)
  • Veterinary Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Cosmetics (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)
  • Saccharide Compounds (AREA)
  • Steroid Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

내용 없음

Description

결정상 벤조티아진 디옥사이드 염의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 브롬화 칼륨내에서의 N-(2-피리딜)-2-메틸-4-하이드록시-2H-1,2-벤조티아진-3-카복사미드 1, 1-디옥사이드 모노에탄올아민 염의 폴리모프 I 형태의 적외선 흡스 스팩트럼의 결과를 도시한 그래프.
제2도는 브롬화 칼륨내에서의 N-(2-피리딜)-2-메틸-4-하이드록시-2H-1,2-벤조티아진-3-카복사미드 1,1-디옥사이드 모노에탄올아민 염의 폴리모프 II 형태의 적외선 흡수 스펙트럼의 결과를 도시한 그래프.
제3도는 N-(2-피리딜) -2-메틸-4-하이드록시-2H-1,2-벤조티아진-3-카복사미드 1,1-디옥사이드, 모노에탄올아민 염의 폴리모프 I 형태의 특징적인 X-선 분말 회절의 결과를 도시한 그래프.
제4도는 N-(2-피리딜)-2-메틸-4-하이드록시-2H-1,2-벤조티아진-3-카복사미드 1,1-디옥사이드, 모노에탄올아민 염의 폴리모프 I 형태의 특징적인 X-선 분말 회절의 결과를 도시한 그래프.

Claims (10)

  1. N-(2-피리딜)-2-메틸-4-하이드록시-2H-1,2-벤조티아진-3-카복사미드 1,1-디옥사이드와 모노에탄올 아민을 반응시킨 후, 초기 폴리모프II 반응생성물을 극성 양성자성 용매 또는 극성이나 비극성 비양성자성 용매내에 가하여 수득한 용액을 약 20℃ 내지 용매의 환류온도까지의 온도에서 하기 폴리모프I의 형성이 거의 완결될때까지 교반시킨 다음, 상기 용액으로부터 하기 폴리모프I 형태를 침전시킴을 특징으로 하여, 178 내지 181℃에서 분해되면서 용융되고, 20회전시 10.6°, 12.1°, 13.0°, 17.4°, 17.6°, 18.1°, 19.3°, 20.4°, 21.1°, 21.9°, 26.4°, 28.7°, 29.0°, 30.4, 31.9° 및 32.5°에서 특정 피크들이 나타나는 특징적인 X-선 분말회절 도형을 나타내며 또한 브롬화 칼륨내에서의 적외선 흡수 스펙트럼 분석결과 아크(reciprocal)센티미터(cm-1) 단위로 1620, 1595, 1570, 1530, 1510, 1435, 1400, 1315, 1300, 1287, 1250, 1235, 1180, 1165, 1150, 1112, 1090, 1060, 1010, 990, 795, 930, 870, 800, 770, 755, 735, 660, 650, 620, 565, 540, 510, 455, 400 및 365의 특징적인 흡수 밴드들을 나타내는 N-(2-피리딜)-2-메틸-4-하이드록시-2H-1,2-벤조티아진-3-카복사미드-1,1-디옥사이드 모노에탄올아민염의 폴리모프 I 형태를 제조하는 방법.
  2. 제1항에 있어서, 사용한 용매가 극성 양성자성 용매임을 특징으로 하는 방법.
  3. 제2항에 있어서, 상기 용매가 저급알칸올임을 특징으로 하는 방법.
  4. 제3항에 있어서, 상기 용매가 메탄올임을 특징으로 하는 방법.
  5. 제3항에 있어서, 상기 용매가 에탄올임을 특징으로 하는 방법.
  6. 제1항에 있어서, 사용한 용매가 비양성자성 용매임을 특징으로 하는 방법.
  7. 제6항에 있어서, 상기 용매가 아세토니트릴임을 특징으로 하는 방법.
  8. 제6항에 있어서, 상기 용매가 아세톤임을 특징으로 하는 방법.
  9. 제6항에 있어서, 상기 용매가 메틸렌클로라이드임을 특징으로 하는 방법.
  10. 제1항에 있어서, 폴리모프 II를 함유하고 있는 용액을 약 3시간 이상동안 교반하여 폴리모프I을 수득함을 특징으로 하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019850008577A 1984-11-16 1985-11-16 결정상 벤조티아진 디옥사이드 염의 제조방법 KR870000291B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US672,028 1984-11-16
US06/672,028 US4582831A (en) 1984-11-16 1984-11-16 Anti-inflammatory polymorphic monoethanolamine salt of N-(2-pyridyl)-2-methyl-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide compound, composition, and method of use therefor

Publications (2)

Publication Number Publication Date
KR860004038A true KR860004038A (ko) 1986-06-16
KR870000291B1 KR870000291B1 (ko) 1987-02-25

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Country Status (28)

Country Link
US (1) US4582831A (ko)
EP (1) EP0182572B1 (ko)
JP (1) JPS61122284A (ko)
KR (1) KR870000291B1 (ko)
CN (1) CN1004001B (ko)
AT (1) ATE50257T1 (ko)
AU (1) AU556378B2 (ko)
CA (1) CA1209572A (ko)
DD (1) DD242405A5 (ko)
DE (1) DE3575925D1 (ko)
DK (1) DK171726B1 (ko)
EG (1) EG17621A (ko)
ES (1) ES8701712A1 (ko)
FI (1) FI82045C (ko)
GR (1) GR852772B (ko)
HU (1) HU197899B (ko)
IE (1) IE58288B1 (ko)
IL (1) IL77051A (ko)
IN (1) IN164207B (ko)
MY (1) MY101984A (ko)
NO (1) NO854574L (ko)
NZ (1) NZ214201A (ko)
PH (1) PH21322A (ko)
PL (1) PL149466B1 (ko)
PT (1) PT81490B (ko)
SU (1) SU1491339A3 (ko)
YU (1) YU44019B (ko)
ZA (1) ZA858773B (ko)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5436241A (en) * 1994-01-14 1995-07-25 Bristol-Myers Squibb Company Topical anti-inflammatory compositions containing piroxicam
US20030068829A1 (en) * 2001-06-25 2003-04-10 Symyx Technologies, Inc. High throughput crystallographic screening of materials
TWI280128B (en) * 2002-05-22 2007-05-01 Smithkline Beecham Corp 3'-[(2Z)-[1-(3,4- dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid bis-(monoethanolamine)
ECSP077628A (es) * 2007-05-03 2008-12-30 Smithkline Beechman Corp Nueva composición farmacéutica
BRPI1014548A2 (pt) 2009-05-29 2015-08-25 Glaxosmithkline Llc Métodos de administração de compostos agonistas de trombopoetina
ES2553114T3 (es) * 2009-07-29 2015-12-04 Nerviano Medical Sciences S.R.L. Sales de inhibidor de plk
GB0914287D0 (en) * 2009-08-14 2009-09-30 Pci Biotech As Compositions

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3591584A (en) * 1968-08-27 1971-07-06 Pfizer Benzothiazine dioxides
IN160683B (ko) * 1981-06-01 1987-07-25 Pfizer
US4434164A (en) * 1981-06-01 1984-02-28 Pfizer Inc. Crystalline benzothiazine dioxide salts
RO88420A (ro) * 1983-04-25 1986-01-30 Pfizer Inc,Us Procedeu pentru prepararea unor saruri bazice de piroxican depuse pe suporturi farmaceutice

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Publication number Publication date
IL77051A0 (en) 1986-04-29
FI854512A0 (fi) 1985-11-15
ES548878A0 (es) 1986-12-01
EP0182572B1 (en) 1990-02-07
HU197899B (en) 1989-06-28
DK171726B1 (da) 1997-04-14
KR870000291B1 (ko) 1987-02-25
YU44019B (en) 1990-02-28
CA1209572A (en) 1986-08-12
JPH0425957B2 (ko) 1992-05-06
US4582831A (en) 1986-04-15
EG17621A (en) 1991-08-30
IL77051A (en) 1989-03-31
MY101984A (en) 1992-02-29
FI82045B (fi) 1990-09-28
DK527585D0 (da) 1985-11-15
IE852852L (en) 1986-05-16
CN1004001B (zh) 1989-04-26
AU4995085A (en) 1986-05-22
YU178585A (en) 1987-12-31
DD242405A5 (de) 1987-01-28
PL149466B1 (en) 1990-02-28
JPS61122284A (ja) 1986-06-10
IN164207B (ko) 1989-01-28
ZA858773B (en) 1987-06-24
FI82045C (fi) 1991-01-10
PH21322A (en) 1987-09-28
HUT40116A (en) 1986-11-28
DK527585A (da) 1986-05-17
CN85108245A (zh) 1986-09-03
NZ214201A (en) 1988-07-28
AU556378B2 (en) 1986-10-30
DE3575925D1 (de) 1990-03-15
PL256259A1 (en) 1986-10-07
NO854574L (no) 1986-05-20
IE58288B1 (en) 1993-08-25
PT81490A (en) 1985-12-01
ATE50257T1 (de) 1990-02-15
ES8701712A1 (es) 1986-12-01
FI854512A (fi) 1986-05-17
SU1491339A3 (ru) 1989-06-30
PT81490B (pt) 1988-03-03
GR852772B (ko) 1986-03-14
EP0182572A1 (en) 1986-05-28

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