KR930007446A - 트리아졸 유도체를 함유한 직장 투여용 약학 조성물 - Google Patents
트리아졸 유도체를 함유한 직장 투여용 약학 조성물 Download PDFInfo
- Publication number
- KR930007446A KR930007446A KR1019920018911A KR920018911A KR930007446A KR 930007446 A KR930007446 A KR 930007446A KR 1019920018911 A KR1019920018911 A KR 1019920018911A KR 920018911 A KR920018911 A KR 920018911A KR 930007446 A KR930007446 A KR 930007446A
- Authority
- KR
- South Korea
- Prior art keywords
- pharmaceutical composition
- triazole derivative
- triazol
- bis
- pharmaceutical
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract 15
- 229940042055 systemic antimycotics triazole derivative Drugs 0.000 title 1
- 150000003852 triazoles Chemical class 0.000 claims abstract 8
- -1 5-chloropyrid-2-yl Phenyl Chemical group 0.000 claims abstract 4
- 229910052740 iodine Inorganic materials 0.000 claims abstract 4
- 125000005456 glyceride group Chemical group 0.000 claims abstract 3
- 125000001424 substituent group Chemical group 0.000 claims abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims abstract 2
- 238000005809 transesterification reaction Methods 0.000 claims abstract 2
- ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical group CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 229930195734 saturated hydrocarbon Natural products 0.000 claims 2
- 239000000829 suppository Substances 0.000 claims 2
- 125000003626 1,2,4-triazol-1-yl group Chemical group [*]N1N=C([H])N=C1[H] 0.000 claims 1
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims 1
- YQGKGWNEBMFGBG-UHFFFAOYSA-N 2-(4-iodophenyl)-1,3-bis(1,2,4-triazol-1-yl)propan-2-ol Chemical compound C1=NC=NN1CC(C=1C=CC(I)=CC=1)(O)CN1C=NC=N1 YQGKGWNEBMFGBG-UHFFFAOYSA-N 0.000 claims 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- RFHAOTPXVQNOHP-UHFFFAOYSA-N fluconazole Chemical compound C1=NC=NN1CC(C=1C(=CC(F)=CC=1)F)(O)CN1C=NC=N1 RFHAOTPXVQNOHP-UHFFFAOYSA-N 0.000 claims 1
- 230000008014 freezing Effects 0.000 claims 1
- 238000007710 freezing Methods 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 230000008018 melting Effects 0.000 claims 1
- 238000002844 melting Methods 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 239000001294 propane Substances 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (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)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
본 발명은 에스테르 교환에 의해 제조된 반-합성 글리세라이드, 및 활성 성분으로서 하기 일반식(Ⅰ)의 트리아졸 유도체를 함유하는 직장 투여용 약학 조성물에 관한 것이다 :
상기식에서, R1은 F, Cl, Br, I, CF3, (C1-C4)알킬, (C1-C4)알콕시 및 5-클로로피리드-2-일로 이루어진 그룹중에서 독립적으로 선택된 1내지 3개의 치환체로 임의로 치환된 페닐이고; X는 OH, F, Cl 또는 Br 이고; R2는 H, CH3또는 F 이고; R3는 H 또는 F이다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (9)
- (a)약학 조성물의 총 중량에 대해 0.1 내지 25중량%를 차지하는, 적어도 하나의 하기 일반식(Ⅰ)의 치료활성 트리아졸 화합물, (b)C8내지 C18의 쇄 길이를 가지며 32℃ 내지 44℃ 범위의 융점을 갖는 포화 지방산 글리세라이드로 이루어져 있으며, 약학 조성물의 총 중량에 대해 80 내지 99.9중량%를 차지하는, 에스테르 교환에 의해 생성된 반-합성 글리세라이드 및 (c)40° 내지 70℃의 응고점을 가지며, 약학 조성물의 총 중량에 대해 0내지 8중량%를 차지하는 정제된 고형 포화 탄화수소의 혼합물을 포함하는 직장 투여용 약학 조성물.상기식에서, R1은 F, Cl, Br, I, CF3, (C1-C4)알킬, (C1-C4)알콕시 및 5-클로로피리드-2-일로 이루어진 그룹중에서 독립적으로 선택된 1내지 3개의 치환체로 임의로 치환된 페닐 라디칼이고; X는 OH, F, Cl 또는 Br이고; R2는 H, CH3또는 F 이고; R3는 H 또는 F 이다.
- 제1항에 있어서, 상기 치료 활성 물질(a)가 하기 일반식(Ⅱ)의 트리아졸 유도체인 약학 조성물.상기식에서, R1은 F, Cl, Br, I, CF3로 이루어진 그룹중에서 독립적으로 선택된 1내지 3개의 치환체로 임의로 치환된 페닐이고, X는 OH, F, Cl 또는 Br이다.
- 제1항에 있어서, 트리아졸 유도체(a)가 1,3-비스(1H-1,2,4-트리아졸-1-일)-2-브로모-2-(2,4-디클로로페닐)프로판인 약학 조성물.
- 제1항에 있어서, 트리아졸 유도체(a)가 1,3-비스(1H-1,2,4-트리아졸-1-일)-2-클로로-2-(2,4-디클로로페닐)프로판인 약학 조성물.
- 제1항에 있어서, 트리아졸 유도체(a)가 1,3-비스(1H-1,2,4-트리아졸-1-일)-2-(4-요오도페닐)프로판-2-올인 약학 조성물.
- 제1항에 있어서, 트리아졸 유도체(a)가 2,4-디플로오로-α,α-비스(1H-1,2,4-트리아졸-1-일메틸)벤질 알콜인 약학 조성물.
- 직장 투여용 좌약의 형태로 존재하고, 좌약 1개당 10내지 400㎎의 트리아졸 유도체(a)를 함유하는, 제1항 내지 제6항중 어느 한 항에 따른 약학 조성물의 약학 제제.
- 제7항에 있어서, 반-합성 글리세라이드(b)가 3미만의 요오드가 및 20미만의 하이드록실가를 갖는 약학 제제.
- 제7항 또는 제8항에 있어서, 포화 탄화수소(c)가 약학 조성물의 총 중량에 대해 2내지 5.5중량%의 양으로 존재하는 약학 제제.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DEP4134125.2 | 1991-10-15 | ||
| DE4134125A DE4134125C2 (de) | 1991-10-15 | 1991-10-15 | Triazol-Derivate enthaltende pharmazeutische Zusammensetzungen zur rektalen Applikation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR930007446A true KR930007446A (ko) | 1993-05-20 |
Family
ID=6442729
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019920018911A Abandoned KR930007446A (ko) | 1991-10-15 | 1992-10-14 | 트리아졸 유도체를 함유한 직장 투여용 약학 조성물 |
Country Status (18)
| Country | Link |
|---|---|
| EP (1) | EP0537729B1 (ko) |
| JP (1) | JPH05294830A (ko) |
| KR (1) | KR930007446A (ko) |
| AT (1) | ATE150970T1 (ko) |
| CA (1) | CA2080566C (ko) |
| DE (2) | DE4134125C2 (ko) |
| DK (1) | DK0537729T3 (ko) |
| ES (1) | ES2100998T3 (ko) |
| FI (1) | FI107232B (ko) |
| GR (1) | GR3023552T3 (ko) |
| HU (1) | HU213202B (ko) |
| IL (1) | IL103398A (ko) |
| MX (1) | MX9205898A (ko) |
| MY (1) | MY108576A (ko) |
| NO (1) | NO923992L (ko) |
| NZ (1) | NZ244734A (ko) |
| TW (1) | TW258661B (ko) |
| ZA (1) | ZA927907B (ko) |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2078719B (en) * | 1980-06-02 | 1984-04-26 | Ici Ltd | Heterocyclic compounds |
| DE3262386D1 (en) * | 1981-06-06 | 1985-03-28 | Pfizer Ltd | Antifungal agents, processes for their preparation, and pharmaceutical compositions containing them |
| GR79307B (ko) * | 1982-06-09 | 1984-10-22 | Pfizer | |
| DE3307217A1 (de) * | 1983-03-02 | 1984-09-06 | Bayer Ag, 5090 Leverkusen | Substituierte 1,3-diazolyl-2-propanole, verfahren zu ihrer herstellung und ihre verwendung als antimykotische mittel |
-
1991
- 1991-10-15 DE DE4134125A patent/DE4134125C2/de not_active Expired - Fee Related
-
1992
- 1992-10-09 IL IL10339892A patent/IL103398A/xx not_active IP Right Cessation
- 1992-10-13 MY MYPI92001843A patent/MY108576A/en unknown
- 1992-10-13 TW TW081108139A patent/TW258661B/zh active
- 1992-10-14 CA CA002080566A patent/CA2080566C/en not_active Expired - Fee Related
- 1992-10-14 NO NO92923992A patent/NO923992L/no unknown
- 1992-10-14 MX MX9205898A patent/MX9205898A/es unknown
- 1992-10-14 HU HU9203236A patent/HU213202B/hu not_active IP Right Cessation
- 1992-10-14 KR KR1019920018911A patent/KR930007446A/ko not_active Abandoned
- 1992-10-14 FI FI924639A patent/FI107232B/fi not_active IP Right Cessation
- 1992-10-14 ZA ZA927907A patent/ZA927907B/xx unknown
- 1992-10-14 NZ NZ244734A patent/NZ244734A/en not_active IP Right Cessation
- 1992-10-15 AT AT92117609T patent/ATE150970T1/de not_active IP Right Cessation
- 1992-10-15 ES ES92117609T patent/ES2100998T3/es not_active Expired - Lifetime
- 1992-10-15 EP EP92117609A patent/EP0537729B1/en not_active Expired - Lifetime
- 1992-10-15 DK DK92117609.5T patent/DK0537729T3/da active
- 1992-10-15 DE DE69218718T patent/DE69218718T2/de not_active Expired - Fee Related
- 1992-10-15 JP JP4277001A patent/JPH05294830A/ja active Pending
-
1997
- 1997-05-23 GR GR970401203T patent/GR3023552T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| FI924639L (fi) | 1993-04-16 |
| HUT65417A (en) | 1994-06-28 |
| ZA927907B (en) | 1993-04-21 |
| TW258661B (ko) | 1995-10-01 |
| DE69218718D1 (de) | 1997-05-07 |
| DE69218718T2 (de) | 1997-08-07 |
| GR3023552T3 (en) | 1997-08-29 |
| EP0537729A1 (en) | 1993-04-21 |
| ES2100998T3 (es) | 1997-07-01 |
| MY108576A (en) | 1996-10-31 |
| CA2080566C (en) | 1998-02-17 |
| IL103398A (en) | 1997-08-14 |
| FI924639A0 (fi) | 1992-10-14 |
| CA2080566A1 (en) | 1993-04-16 |
| DE4134125C2 (de) | 1995-02-02 |
| NO923992L (no) | 1993-04-16 |
| HU213202B (en) | 1997-03-28 |
| DK0537729T3 (da) | 1997-09-22 |
| HU9203236D0 (en) | 1992-12-28 |
| ATE150970T1 (de) | 1997-04-15 |
| FI107232B (fi) | 2001-06-29 |
| NZ244734A (en) | 1994-12-22 |
| MX9205898A (es) | 1993-05-01 |
| NO923992D0 (no) | 1992-10-14 |
| IL103398A0 (en) | 1993-03-15 |
| DE4134125A1 (de) | 1993-04-22 |
| JPH05294830A (ja) | 1993-11-09 |
| EP0537729B1 (en) | 1997-04-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0109 | Patent application |
Patent event code: PA01091R01D Comment text: Patent Application Patent event date: 19921014 |
|
| PG1501 | Laying open of application | ||
| A201 | Request for examination | ||
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 19950531 Comment text: Request for Examination of Application Patent event code: PA02011R01I Patent event date: 19921014 Comment text: Patent Application |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
Comment text: Notification of reason for refusal Patent event date: 19980311 Patent event code: PE09021S01D |
|
| PC1902 | Submission of document of abandonment before decision of registration | ||
| SUBM | Surrender of laid-open application requested |