KR940005636A - 트리아졸릴티오메틸티오 세팔로스포린 염산염, 그의 수화물 결정 및 이들의 제조방법 - Google Patents
트리아졸릴티오메틸티오 세팔로스포린 염산염, 그의 수화물 결정 및 이들의 제조방법Info
- Publication number
- KR940005636A KR940005636A KR1019930014742A KR930014742A KR940005636A KR 940005636 A KR940005636 A KR 940005636A KR 1019930014742 A KR1019930014742 A KR 1019930014742A KR 930014742 A KR930014742 A KR 930014742A KR 940005636 A KR940005636 A KR 940005636A
- Authority
- KR
- South Korea
- Prior art keywords
- thiomethylthio
- iminoacetamido
- hydroxy
- hydrate
- carboxylic acid
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title claims abstract description 8
- 238000002360 preparation method Methods 0.000 title abstract 3
- 229930186147 Cephalosporin Natural products 0.000 title 1
- 229940124587 cephalosporin Drugs 0.000 title 1
- -1 cephalosporin hydrochloride Chemical class 0.000 title 1
- 238000000034 method Methods 0.000 claims abstract 5
- 125000001359 1,2,3-triazol-4-yl group Chemical group [H]N1N=NC([*])=C1[H] 0.000 claims abstract 2
- 239000004480 active ingredient Substances 0.000 claims abstract 2
- DKAGJZJALZXOOV-UHFFFAOYSA-N hydrate;hydrochloride Chemical compound O.Cl DKAGJZJALZXOOV-UHFFFAOYSA-N 0.000 claims description 3
- 238000002441 X-ray diffraction Methods 0.000 claims description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 6
- JHXOAXMCYMGJLQ-UHFFFAOYSA-N 2,3-dihydro-1,3-thiazol-2-amine Chemical compound NC1NC=CS1 JHXOAXMCYMGJLQ-UHFFFAOYSA-N 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 241000894006 Bacteria Species 0.000 claims 3
- 238000002425 crystallisation Methods 0.000 claims 2
- 230000008025 crystallization Effects 0.000 claims 2
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 150000004683 dihydrates Chemical class 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 abstract 2
- 231100000053 low toxicity Toxicity 0.000 abstract 1
- 238000001938 differential scanning calorimetry curve Methods 0.000 description 1
- 230000004907 flux Effects 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D501/00—Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
-
- 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
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Cephalosporin Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
본 발명은 강력한 항생물질 활성을 가지며 낮은 독성과 약학적으로 안정함으로써, 임상학적으로 유용한 항생물질 제제의 유효성분으로 유용한 7β-[(Z)-2-(2-아미노-4-티아졸린)-2-하이드록시 이미노아세트아미도]-3-(1,2,3-트리아졸-4-일)티오메틸티오-3-세펨-4-카복실산 염산염 및 그의 수화물 결정 및 이들의 제조방법에 관한 것이다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 S-1090 염산염 수화물 결정의 X-선 회절상으로, 강도(카운트 수)를 종축으로 20값을 횡축으로 나타낸다.
제2도는 S-1090 염산염 수화물 결정의 시차주사 열량 곡선으로, 열 유량(mW)을 종축으로 온도를 횡축으로 나타낸다.
Claims (9)
- 7β-[(Z)-2-(2-아미노-4-티아졸린)-2-하이드록시 이미노아세트아미도]-3-(1,2,3-트리아졸-4-일)티오메틸티오-3-세펨-4-카복실산 염산염.
- 하기 X-선 회절상을 나타내는 7β-[(Z)-2-(2-아미노-4-티아졸린)-2-하이드록시 이미노아세트아미도]-3-(1,2,3-트리아졸-4-일)티오메틸티오-3-세펨-4-카복실산 염산염 수화물 결정.
- 제2항에 있어서, 1 내지 2수화물에 상응하는 수분을 함유하는 염산염 수화물 결정.
- 7β-[(Z)-2-(2-아미노-4-티아졸린)-2-하이드록시 이미노아세트아미도]-3-(1,2,3-트리아졸-4-일)티오메틸티오-3-세펨-4-카복실산 염산과 반응시킴을 포함하는, 제1항에 청구한 화합물의 제조방법.
- 염산 수용액으로 부터 7β-[(Z)-2-(2-아미노-4-티아졸린)-2-하이드록시 이미노아세트아미도]-3-(1,2,3-트리아졸-4-일)티오메틸티오-3-세펨-4-카복실산을 결정화시킴을 포함하는, 제2항에 청구한 수화물 결정의 제조방법.
- 제5항에 있인서, 상기 염산 수용액의 PH가 -1 내지 5인 방법.
- 유효 성분으로서의, 제1항에 청구한 화합물 또는 제2항에 청구한 수화물 결정 효과랑을 이에 대한 약락적으로 허용되는 담체와 함께 함유하는 약학 제제.
- 제1항에 청구한 화합물 또는 제2항에 청구한 수화물 결정 교과량을 세균과 접촉시켜 세균을 억제하는 방법.
- 제1항에 청구된 화합물 또는 제2항에 청구된 수화물 결정 효과량을 감수성 세균에 감염된 환자에게 투여함으로써 상기 환자의 세균 감염을 치료하는 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP20496592 | 1992-07-31 | ||
| JP92-204965 | 1992-07-31 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR940005636A true KR940005636A (ko) | 1994-03-22 |
| KR100245938B1 KR100245938B1 (ko) | 2000-04-01 |
Family
ID=16499234
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019930014742A KR100245938B1 (ko) | 1992-07-31 | 1993-07-30 | 트리아졸릴티오메틸티오 세팔로스포린 염산염, 그의 결정성 수화물 및 이들의 제조방법 |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US5407929A (ko) |
| EP (1) | EP0581552B1 (ko) |
| KR (1) | KR100245938B1 (ko) |
| CN (1) | CN1037683C (ko) |
| AT (1) | ATE165360T1 (ko) |
| AU (1) | AU657866B2 (ko) |
| BR (1) | BR9303235A (ko) |
| CA (1) | CA2101502A1 (ko) |
| DE (1) | DE69318077T2 (ko) |
| ES (1) | ES2115725T3 (ko) |
| FI (1) | FI933391A (ko) |
| GR (1) | GR3026699T3 (ko) |
| HU (1) | HU219637B (ko) |
| IL (1) | IL106516A (ko) |
| MX (1) | MX9304611A (ko) |
| NO (1) | NO303734B1 (ko) |
| NZ (1) | NZ248285A (ko) |
| PH (1) | PH30109A (ko) |
| PL (2) | PL172835B1 (ko) |
| RU (1) | RU2118959C1 (ko) |
| TW (1) | TW307769B (ko) |
| UA (1) | UA37181C2 (ko) |
| ZA (1) | ZA935529B (ko) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2444772T3 (es) * | 2001-02-24 | 2014-02-26 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Derivados de xantina, su preparación y uso como medicamentos |
| AT413282B (de) * | 2002-02-01 | 2006-01-15 | Sandoz Ag | Kristalline salze der 7-(((5-amino-1,2,4-thiadiazol-3-yl) (fluoromethoxy-imino)acetyl)amino)-3- ((imino-1-piperazinylmethyl) |
| KR20030076759A (ko) * | 2002-03-21 | 2003-09-29 | 주식회사 엘지생명과학 | 신규 세팔로스포린 화합물 및 그의 제조 방법 |
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| US6727277B1 (en) | 2002-11-12 | 2004-04-27 | Kansas State University Research Foundation | Compounds affecting cholesterol absorption |
| DE202004021379U1 (de) | 2003-02-12 | 2008-02-21 | Ciba Specialty Chemicals Holding Inc. | Kristalline Formen von Pitivastatin Calcium |
| US7531650B2 (en) | 2003-03-27 | 2009-05-12 | Basilea Pharmaceutica Ag | Cephalosporin salts in crystalline form |
| US7501426B2 (en) * | 2004-02-18 | 2009-03-10 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions |
| DE102004054054A1 (de) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| DE102005035891A1 (de) | 2005-07-30 | 2007-02-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| CA2810522A1 (en) * | 2006-05-04 | 2007-11-15 | Boehringer Ingelheim International Gmbh | Polymorphs |
| PE20080251A1 (es) * | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| NZ600126A (en) * | 2007-08-17 | 2013-12-20 | Boehringer Ingelheim Int | Purine derivatives for use in the treatment of fap-related diseases |
| PE20140960A1 (es) * | 2008-04-03 | 2014-08-15 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| PE20100156A1 (es) * | 2008-06-03 | 2010-02-23 | Boehringer Ingelheim Int | Tratamiento de nafld |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| KR20190016601A (ko) | 2008-08-06 | 2019-02-18 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| MX2011001525A (es) * | 2008-08-15 | 2011-03-29 | Boehringer Ingelheim Int | Derivados de purina para su uso en el tratamiento de enfermedades relacionadas con fab. |
| CN102149407A (zh) | 2008-09-10 | 2011-08-10 | 贝林格尔.英格海姆国际有限公司 | 治疗糖尿病和相关病症的组合疗法 |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| BRPI0923121A2 (pt) | 2008-12-23 | 2015-08-11 | Boehringer Ingelheim Int | Formas salinas de compostos orgânico |
| TW201036975A (en) | 2009-01-07 | 2010-10-16 | Boehringer Ingelheim Int | Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy |
| ES2760917T3 (es) | 2009-11-27 | 2020-05-18 | Boehringer Ingelheim Int | Tratamiento de pacientes diabéticos genotipificados con inhibidores DPP-IV como la linagliptina |
| JP6034781B2 (ja) | 2010-05-05 | 2016-11-30 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 併用療法 |
| CA3164653A1 (en) | 2010-06-24 | 2011-12-29 | Boehringer Ingelheim International Gmbh | A combination comprising linagliptin and a long-acting insulin |
| US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
| US8883800B2 (en) | 2011-07-15 | 2014-11-11 | Boehringer Ingelheim International Gmbh | Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| EP2849755A1 (en) | 2012-05-14 | 2015-03-25 | Boehringer Ingelheim International GmbH | A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome |
| WO2013174767A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference |
| EP3110449B1 (en) | 2014-02-28 | 2023-06-28 | Boehringer Ingelheim International GmbH | Medical use of a dpp-4 inhibitor |
| JP2019517542A (ja) | 2016-06-10 | 2019-06-24 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | リナグリプチンおよびメトホルミンの組合せ |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IE65926B1 (en) * | 1990-07-19 | 1995-11-29 | Shionogi & Co | Thioalkylthio cephalosporin derivatives |
-
1993
- 1993-07-26 AT AT93305864T patent/ATE165360T1/de not_active IP Right Cessation
- 1993-07-26 DE DE69318077T patent/DE69318077T2/de not_active Expired - Fee Related
- 1993-07-26 EP EP93305864A patent/EP0581552B1/en not_active Expired - Lifetime
- 1993-07-26 TW TW082105942A patent/TW307769B/zh active
- 1993-07-26 ES ES93305864T patent/ES2115725T3/es not_active Expired - Lifetime
- 1993-07-27 UA UA93003172A patent/UA37181C2/uk unknown
- 1993-07-27 US US08/097,205 patent/US5407929A/en not_active Expired - Fee Related
- 1993-07-28 CA CA002101502A patent/CA2101502A1/en not_active Abandoned
- 1993-07-28 AU AU44227/93A patent/AU657866B2/en not_active Ceased
- 1993-07-28 HU HU9302194A patent/HU219637B/hu not_active IP Right Cessation
- 1993-07-28 IL IL106516A patent/IL106516A/en not_active IP Right Cessation
- 1993-07-29 PH PH46601A patent/PH30109A/en unknown
- 1993-07-29 NZ NZ24828593A patent/NZ248285A/en unknown
- 1993-07-29 PL PL93299870A patent/PL172835B1/pl unknown
- 1993-07-29 FI FI933391A patent/FI933391A/fi unknown
- 1993-07-29 PL PL93317972A patent/PL172830B1/pl unknown
- 1993-07-30 BR BR9303235A patent/BR9303235A/pt not_active Application Discontinuation
- 1993-07-30 RU RU93047027/04A patent/RU2118959C1/ru not_active IP Right Cessation
- 1993-07-30 KR KR1019930014742A patent/KR100245938B1/ko not_active IP Right Cessation
- 1993-07-30 NO NO932745A patent/NO303734B1/no unknown
- 1993-07-30 ZA ZA935529A patent/ZA935529B/xx unknown
- 1993-07-30 MX MX9304611A patent/MX9304611A/es unknown
- 1993-07-31 CN CN93117437A patent/CN1037683C/zh not_active Expired - Fee Related
-
1998
- 1998-04-23 GR GR980400753T patent/GR3026699T3/el unknown
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