KR970021073A - 피페리딘 유도체 결정, 이의 제조용 중간 생성물 및 이의 제조방법 - Google Patents

피페리딘 유도체 결정, 이의 제조용 중간 생성물 및 이의 제조방법 Download PDF

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KR970021073A
KR970021073A KR1019960047055A KR19960047055A KR970021073A KR 970021073 A KR970021073 A KR 970021073A KR 1019960047055 A KR1019960047055 A KR 1019960047055A KR 19960047055 A KR19960047055 A KR 19960047055A KR 970021073 A KR970021073 A KR 970021073A
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South Korea
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same
crystals
ylidene
dibenzo
piperidino
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KR1019960047055A
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KR100372964B1 (ko
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아키코 후지이
미에 구보
도모야 야마모토
지로 시마다
류이치 미하라
히로카즈 나오라
고지 아사이
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이나모리 쥰스케
아지노모토 가부시키가이샤
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D211/68—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D211/70—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 one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

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

Abstract

본 발명은 N-(2-(4-(5H-디벤조[a, d]사이클로헵텐-5-일리덴)피페리디노)에 틸)-1-포르밀-4-피페리딘카복스아미드 하이드로클로라이드의 1수화물 및 3수화물 결정에 관한 것이다. 본 발명의 1수화물 및 3수화물 결정은 우수한 안정성을 나타낸다. 1수화물은 우수한 경구 흡수성을 나타내고 3수화물은 분해 속도가 빨라 다양한 필요조건을 만족시키는 약품을 제조할 수 있다.

Description

피레리딘 유도체 결정, 이의 제조용 중간 생성물 및 이의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 1수화물 결정의 분말 X선 회절 패턴이고,
제2도는 3수화물 결정의 분말 X선 회절 패턴이며,
제3도는 α형 무수물 결정의 분말 X선 회절 패턴이고,
제4도는 β형 무수물 결정의 분말 X선 회절 패턴이며,
제5도는 1수화물 결정의 IR 흡수 스펙트럼이다.

Claims (12)

  1. N-(2-(4-(5H-디벤조[a, d]사이클로헵텐-5-일리덴]피페리디노)에틸)-1-포르밀-4-피페리딘카복스아미드 하이드로클로라이드 1수화물 결정.
  2. 제1항에 있어서, 분말 X선 회절에서의 피크가 6.3°, 11.3°, 18.7°, 19.6°, 20.3°, 21.2°, 22.8°, 25.2°, 26.0°및 26.4°의 회절각(2θ±0.1)에서 존재하는 결정.
  3. 분말 X선 회절에서의 피크가 6.3°, 11.3°, 18.6°, 19.4°, 20.3°, 20.9°, 22.7°및 26.3°의 회절각(2θ±0.1)에서 존재하는 N-(2-(4-(5H-디벤조[a, d]사이클로헵텐-5-일리덴]피페리디노)에틸)-1-포르밀-4-피페리딘카복스아미드 하이드로클로라이드 무수물 결정.
  4. 제3항에 따르는 N-(2-(4-(5H-디벤조[a, d]사이클로헵텐-5-일리덴)피페리디 노)에틸)-1-포르밀-4-피페리딘카복스아미드 하이드로클로라이드 무수물 결정을 습도 조절함을 포함하여, 제1항의 결정을 제조하는 방법.
  5. 제4항에 있어서, 습도 조절이 25 내지 90℃의 온도에서 수행되는 방법.
  6. 제4항에 있어서, 습도 조절이 50 내지 90%의 상대 습도에서 수행되는 방법.
  7. N-(2-(4-(5H-디벤조[a, d]사이클로헵텐-5-일리덴]피페리디노)에틸)-1-포르밀 -4-피페리딘카복스아미드 하이드로클로라이드 3수화물 결정.
  8. 제7항에 있어서, 분말 X선 회절에서의 피크가 14.6°, 19.6°, 21.8°, 22.3°, 22.9°, 24.1°, 26.6°및 28.3°의 회절각(2θ±0.1)에서 존재하는 결정.
  9. 분말 X선 회절에서의 피크가 12.8°, 15.0°, 19.4°, 22.4°, 23.8°, 27.2°및 27.9°의 회절각(2θ±0.1)에서 존재하는 N-(2-(4-(5H-디벤조[a,d]사이클로헵텐-5-일리덴]피페리디노)에틸)-1-포르밀-4-피페리딘카복스아미드 하이드로클로라이드 무수물 결정.
  10. 제9항에 따르는 N-(2-(4-(5H-디벤조[a,d]사이클로헵텐-5-일리덴]피페리디노)에틸)-1-포르밀-4-피페리딘카복스아미드 하이드로클로라이드 무수물 결정을 습도 조절함을 포함하여, 제7항의 결정을 제조하는 방법.
  11. 제10항에 있어서, 습도 조절이 25 내지 90℃의 온도에서 수행되는 방법.
  12. 제10항에 있어서, 습도 조절이 50 내지 90%의 상대 습도에서 수행되는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960047055A 1995-10-23 1996-10-21 피페리딘유도체결정,이의제조용중간생성물및이의제조방법 KR100372964B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP95-274175 1995-10-23
JP27417595 1995-10-23
JP96-263010 1996-10-03
JP8263010A JP2914324B2 (ja) 1995-10-23 1996-10-03 ピペリジン誘導体の結晶並びにその製造中間体及び製造方法

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KR970021073A true KR970021073A (ko) 1997-05-28
KR100372964B1 KR100372964B1 (ko) 2003-04-21

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US (3) US6184233B1 (ko)
EP (1) EP0770602B1 (ko)
JP (1) JP2914324B2 (ko)
KR (1) KR100372964B1 (ko)
CN (2) CN1293055C (ko)
AT (1) ATE256111T1 (ko)
CA (1) CA2188507C (ko)
DE (1) DE69631011T2 (ko)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE253048T1 (de) * 1997-04-09 2003-11-15 Ajinomoto Kk Verfahren zur herstellung von piperidincarbonsäureamiden
SE9902550D0 (sv) * 1999-07-02 1999-07-02 Astra Ab New crystalline forms
US7432391B2 (en) * 2005-05-24 2008-10-07 Daito Chemix Corporation Process for the production of tert-butyl N-(2-bromoethyl)carbamate

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2618151B1 (fr) * 1987-07-16 1991-01-11 Synthelabo Derives de piperidine, leur preparation et leur application en therapeutique
FR2620121B1 (fr) * 1987-09-09 1990-01-05 Synthelabo ((pyrimidinyl-2)-aminoalkyl)-1 piperidines, leur preparation et leur application en therapeutique
GB8729471D0 (en) * 1987-12-17 1988-02-03 Wyeth John & Brother Ltd New crystal form
ZA889365B (en) * 1987-12-22 1990-08-29 Lilly Co Eli Hydrates of andinotropic agent
EP0370712A3 (en) * 1988-11-18 1991-10-02 Ajinomoto Co., Inc. Ethylamine derivatives and hypotensives containing the same
CA2004211A1 (en) * 1988-11-30 1990-05-31 Masataka Syoji Piperidine derivatives and hyportensives containing the same
JPH03128354A (ja) * 1989-07-04 1991-05-31 Hokuriku Seiyaku Co Ltd ピペリジン誘導体
US5095022A (en) * 1989-07-04 1992-03-10 Hokuriku Pharmaceutical Co., Ltd. Piperidine derivatives and pharmaceutical compositions comprising the same
ES2023560A6 (es) * 1989-07-10 1992-01-16 Gema Sa Procedimiento para la produccion de hidrato de cefradina y solvato de cefradina y dimetilformamida.
MTP1076B (en) * 1990-01-12 1991-09-30 Ciba Geigy Ag Hemihydrate
EP0479601B1 (en) * 1990-10-05 1999-12-15 Ajinomoto Co., Inc. Piperidine derivatives and their use as antiarrhythmic agents
CA2101571A1 (en) * 1992-09-08 1994-03-09 Elizabeth A. Garofalo Crystalline dihydrate of a cephalosporin dihydrate salt and injectable compositions thereof
TW366343B (en) * 1994-04-20 1999-08-11 Ajinomoto Kk Piperidine derivatives and anti-platelet agents containing the same
KR102147429B1 (ko) * 2018-11-27 2020-08-24 주식회사 케이티 네트워크 연결이 해제된 가입자 단말의 위치 정보를 제공하는 방법

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KR100372964B1 (ko) 2003-04-21
EP0770602A3 (en) 1997-05-14
CA2188507C (en) 2006-04-04
CN1121402C (zh) 2003-09-17
JPH09176119A (ja) 1997-07-08
US6444821B2 (en) 2002-09-03
CN1293055C (zh) 2007-01-03
DE69631011D1 (de) 2004-01-22
US6184233B1 (en) 2001-02-06
JP2914324B2 (ja) 1999-06-28
ATE256111T1 (de) 2003-12-15
EP0770602B1 (en) 2003-12-10
US6232323B1 (en) 2001-05-15
EP0770602A2 (en) 1997-05-02
CN1515553A (zh) 2004-07-28
DE69631011T2 (de) 2004-10-21
CN1151403A (zh) 1997-06-11
CA2188507A1 (en) 1997-04-24
US20010056102A1 (en) 2001-12-27

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