KR910014376A - 반수화물 - Google Patents
반수화물 Download PDFInfo
- Publication number
- KR910014376A KR910014376A KR1019910000244A KR910000244A KR910014376A KR 910014376 A KR910014376 A KR 910014376A KR 1019910000244 A KR1019910000244 A KR 1019910000244A KR 910000244 A KR910000244 A KR 910000244A KR 910014376 A KR910014376 A KR 910014376A
- Authority
- KR
- South Korea
- Prior art keywords
- tetrahydroimidazo
- pyridin
- crystalline form
- hemihydrate
- water
- Prior art date
Links
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 5
- UKCVAQGKEOJTSR-UHFFFAOYSA-N Fadrozole hydrochloride Chemical compound Cl.C1=CC(C#N)=CC=C1C1N2C=NC=C2CCC1 UKCVAQGKEOJTSR-UHFFFAOYSA-N 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- -1 5,6,7,8-tetrahydroimidazo [1,5-a] pyridin-5-yl Chemical group 0.000 claims 2
- 102000014654 Aromatase Human genes 0.000 claims 2
- 108010078554 Aromatase Proteins 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- CLPFFLWZZBQMAO-UHFFFAOYSA-N 4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile Chemical compound C1=CC(C#N)=CC=C1C1N2C=NC=C2CCC1 CLPFFLWZZBQMAO-UHFFFAOYSA-N 0.000 claims 1
- 125000004938 5-pyridyl group Chemical group N1=CC=CC(=C1)* 0.000 claims 1
- 238000004279 X-ray Guinier Methods 0.000 claims 1
- QMEZUZOCLYUADC-UHFFFAOYSA-N hydrate;dihydrochloride Chemical compound O.Cl.Cl QMEZUZOCLYUADC-UHFFFAOYSA-N 0.000 claims 1
- 229910000041 hydrogen chloride Inorganic materials 0.000 claims 1
- IXCSERBJSXMMFS-UHFFFAOYSA-N hydrogen chloride Substances Cl.Cl IXCSERBJSXMMFS-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Saccharide Compounds (AREA)
- Compounds Of Alkaline-Earth Elements, Aluminum Or Rare-Earth Metals (AREA)
- Lubricants (AREA)
- Pyridine Compounds (AREA)
- Photoreceptors In Electrophotography (AREA)
- Liquid Crystal Substances (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (10)
- 결정성 반수화물 형태의 4-(5,6,7,8-테트라하이드로이미다조[1,5-a]피리딘-5-일)-벤조니트릴하이드로클로라이드.
- 제1항에 있어서, X-선 분말 패턴(Guinier camera, 구리-Ku1방사)이 하기 격자간격(d치) 및 상대 선 세기(세기)를 나타내는, 결정성 반수화물 형태의 4-(5,6,7,8-테트라하이드로이미다조[1,5-a]피리딘-5-일]-벤조니트릴하이드로클로라이드.
- 제1항에 있어서, 실질적으로 순수한 형태의 결정형.
- 제2항에 있어서, 실질적으로 순수한 형태의 결정형.
- 제1항 또는 2항에 따른 결정형의 4-(5,6,7,8-테트라하이드로이미다조[1,5-a]피리딘-5-일)-벤조니트릴하이드로클로라이드 및 하나이상의 약제학적으로 허용되는 담체를 함유하는 약제학적 제제.
- 제1항 내지 4항중 어느 한 항에 있어서, 동물 또는 인체를 치료하는 방법에서 사용하기 위한 결정형.
- 제1항 내지 4항중 어느 한 항에 있어서, 효소 아로마타제의 억제로 인한 질환의 치료시 사용하기 위한 결정형.
- 약제학적 제제를 제조하기 위한 제 1항 내지 4항중 어느 한 항에 따른 결정형의 용도.
- 효소 아로마타제의 억제로 인한 질환을 치료하기 위한 약제학적 제제의 제조를 위한 제 1항 내지 4항중 어느 한 항에 따른 결정형의 용도.
- (a)-4(5,6,7,8-테트라하이드로이미다조[1,5-a]피리딘-5-일)-벤조니트릴을 물의 존재하에 염화수소와 반응시키거나, (b) 제조될 구조식(Ⅰ)의 반수화물 보다 물을 덜 함유하는 4-(5,6,7,8-테트라하이드로이미다조[1,5-a]피리딘-5-일)-벤조니트릴하이드로클로라이드 형태를 물로 처리하거나, (c) 제조될 구조식(Ⅰ)의 반수화물보다 물을 더 함유하는 4-(5,6,7,8-테트라하이드로이미다조[1,5-a]피리딘-5-일)-벤조니트릴 하이드로클로라이드 형태로부터 물을 제거하거나, (d)물의 존재하에 상기 하이드로클로라이드와 다른4-(5,6,7,8-테트라하이드로이미다조[1,5-a]피리딘-5-일)-벤조니트릴 염의 구조식(Ⅰ)의 하이드로클로라이드 반수화물로 전환시킴을 특징으로 하여, 제1항 내지 4항중 어느 한 항에 따른 결정형을 제조하는 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CH100/90-0 | 1990-01-12 | ||
CH10090 | 1990-01-12 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR910014376A true KR910014376A (ko) | 1991-08-31 |
KR100191360B1 KR100191360B1 (ko) | 1999-06-15 |
Family
ID=4179261
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019910000244A KR100191360B1 (ko) | 1990-01-12 | 1991-01-10 | Ix-선다이아그램에 의해 특징화되는 결정성 반수화물 형태의 4-(5,6,7,8-테트라하이드로이미다조(1,5-a)피리딘-5-일)-벤조니트릴 하이드로클로라이드, 이의 제조방법 및 이를 함유하는 약제학적 제제 |
Country Status (33)
Country | Link |
---|---|
US (1) | US5098911A (ko) |
EP (1) | EP0437415B1 (ko) |
JP (1) | JP2694186B2 (ko) |
KR (1) | KR100191360B1 (ko) |
CN (1) | CN1037966C (ko) |
AT (1) | ATE125809T1 (ko) |
AU (1) | AU638085B2 (ko) |
BG (2) | BG60033A3 (ko) |
CA (1) | CA2033937C (ko) |
CZ (1) | CZ279823B6 (ko) |
DE (1) | DE59106101D1 (ko) |
DK (1) | DK0437415T3 (ko) |
DZ (1) | DZ1482A1 (ko) |
ES (1) | ES2075399T3 (ko) |
FI (1) | FI94528C (ko) |
GR (1) | GR3017027T3 (ko) |
HK (1) | HK1000663A1 (ko) |
HU (1) | HU216192B (ko) |
ID (1) | ID964B (ko) |
IE (1) | IE67512B1 (ko) |
IL (1) | IL96879A (ko) |
MA (1) | MA22040A1 (ko) |
MT (1) | MTP1076B (ko) |
NO (1) | NO175747C (ko) |
NZ (1) | NZ236735A (ko) |
PH (1) | PH27601A (ko) |
PL (3) | PL166500B1 (ko) |
PT (1) | PT96447B (ko) |
RO (1) | RO107408B1 (ko) |
RU (2) | RU2021271C1 (ko) |
SA (1) | SA93140021B1 (ko) |
TN (1) | TNSN91001A1 (ko) |
ZA (1) | ZA91229B (ko) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW208013B (ko) * | 1990-03-01 | 1993-06-21 | Daiichi Co Ltd | |
EP0457716A1 (de) * | 1990-04-20 | 1991-11-21 | Ciba-Geigy Ag | Naphthalinderivate |
TW224461B (ko) * | 1990-09-18 | 1994-06-01 | Ciba Geigy Ag | |
CH683151A5 (de) * | 1991-04-24 | 1994-01-31 | Ciba Geigy Ag | Antikonzeption bei weiblichen Primaten ohne Beeinflussung des menstruellen Zyklus. |
JP2914324B2 (ja) | 1995-10-23 | 1999-06-28 | 味の素株式会社 | 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 |
SG10201506874UA (en) | 2010-09-01 | 2015-10-29 | Arena Pharm Inc | Modified-release dosage forms of 5-ht2c agonists useful for weight management |
KR20180094131A (ko) | 2010-09-01 | 2018-08-22 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 신장 손상을 갖는 개체에 대한 로카세린의 투여 |
JP5749410B2 (ja) | 2012-01-17 | 2015-07-15 | ノバルティス アーゲー | ジヒドロピロロ[1,2−c]イミダゾリルアルドステロンシンターゼまたはアロマターゼ阻害薬の新たな形態および塩 |
BR112019007954A2 (pt) * | 2016-10-27 | 2019-07-02 | Damian Pharma Ag | inibidor da aldosterona sintase |
WO2018078049A1 (en) | 2016-10-27 | 2018-05-03 | Damian Pharma Ag | Aldosterone synthase inhibitor |
MX2020011471A (es) | 2018-05-03 | 2020-12-07 | Damian Pharma Ag | R-fadrozol para usar en el tratamiento de aldosteronismo. |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4588732A (en) * | 1982-12-21 | 1986-05-13 | Ciba-Geigy Corporation | Certain imidazo(1,5-a)pyridine derivatives and their use as thromboxane synthetase inhibitors |
US4617307A (en) * | 1984-06-20 | 1986-10-14 | Ciba-Geigy Corporation | Substituted imidazo[1,5-A]pyridine derivatives as aromatase inhibitors |
-
1990
- 1990-12-14 MT MT1076A patent/MTP1076B/xx unknown
-
1991
- 1991-01-02 PH PH41805A patent/PH27601A/en unknown
- 1991-01-02 US US07/636,816 patent/US5098911A/en not_active Expired - Lifetime
- 1991-01-03 ES ES91810003T patent/ES2075399T3/es not_active Expired - Lifetime
- 1991-01-03 AT AT91810003T patent/ATE125809T1/de not_active IP Right Cessation
- 1991-01-03 DK DK91810003.3T patent/DK0437415T3/da active
- 1991-01-03 EP EP91810003A patent/EP0437415B1/de not_active Expired - Lifetime
- 1991-01-03 DE DE59106101T patent/DE59106101D1/de not_active Expired - Lifetime
- 1991-01-04 IL IL9687991A patent/IL96879A/en not_active IP Right Cessation
- 1991-01-07 MA MA22312A patent/MA22040A1/fr unknown
- 1991-01-09 FI FI910126A patent/FI94528C/fi active
- 1991-01-09 DZ DZ910008A patent/DZ1482A1/fr active
- 1991-01-10 KR KR1019910000244A patent/KR100191360B1/ko not_active IP Right Cessation
- 1991-01-10 PL PL91304087A patent/PL166500B1/pl unknown
- 1991-01-10 PT PT96447A patent/PT96447B/pt not_active IP Right Cessation
- 1991-01-10 PL PL91304084A patent/PL167164B1/pl unknown
- 1991-01-10 RO RO146713A patent/RO107408B1/ro unknown
- 1991-01-10 AU AU69280/91A patent/AU638085B2/en not_active Expired
- 1991-01-10 NZ NZ236735A patent/NZ236735A/xx unknown
- 1991-01-10 CA CA002033937A patent/CA2033937C/en not_active Expired - Lifetime
- 1991-01-10 PL PL91288653A patent/PL166157B1/pl unknown
- 1991-01-11 IE IE10391A patent/IE67512B1/en not_active IP Right Cessation
- 1991-01-11 RU SU914894233A patent/RU2021271C1/ru active
- 1991-01-11 CZ CS9155A patent/CZ279823B6/cs not_active IP Right Cessation
- 1991-01-11 HU HU4/91A patent/HU216192B/hu unknown
- 1991-01-11 NO NO910137A patent/NO175747C/no not_active IP Right Cessation
- 1991-01-11 JP JP3065711A patent/JP2694186B2/ja not_active Expired - Lifetime
- 1991-01-11 ZA ZA91229A patent/ZA91229B/xx unknown
- 1991-01-11 TN TNTNSN91001A patent/TNSN91001A1/fr unknown
- 1991-01-11 CN CN91101118A patent/CN1037966C/zh not_active Expired - Lifetime
- 1991-01-14 BG BG93623A patent/BG60033A3/xx unknown
-
1992
- 1992-01-30 ID IDP190792A patent/ID964B/id unknown
- 1992-04-07 RU SU925011257A patent/RU2088584C1/ru active
- 1992-08-18 BG BG96793A patent/BG61489B2/bg unknown
-
1993
- 1993-06-29 SA SA93140021A patent/SA93140021B1/ar unknown
-
1995
- 1995-08-03 GR GR950401945T patent/GR3017027T3/el unknown
-
1997
- 1997-11-24 HK HK97102235A patent/HK1000663A1/xx not_active IP Right Cessation
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