JP2009544588A - 薬剤中におけるアミジン基を有する活性物質の生物学的利用率の向上 - Google Patents
薬剤中におけるアミジン基を有する活性物質の生物学的利用率の向上 Download PDFInfo
- Publication number
- JP2009544588A JP2009544588A JP2009519786A JP2009519786A JP2009544588A JP 2009544588 A JP2009544588 A JP 2009544588A JP 2009519786 A JP2009519786 A JP 2009519786A JP 2009519786 A JP2009519786 A JP 2009519786A JP 2009544588 A JP2009544588 A JP 2009544588A
- Authority
- JP
- Japan
- Prior art keywords
- drug
- inhibitor
- dihydroxyamidine
- producing
- amidine
- 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.)
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- 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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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]
-
- 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
-
- 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
- A61P31/10—Antimycotics
-
- 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
- A61P31/12—Antivirals
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/08—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis for Pneumocystis carinii
-
- 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
-
- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
- C07C259/12—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
- C07D271/07—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Abstract
Description
Claims (8)
- 前記薬物が、プロテアーゼ阻害剤、DNAインターカレーター化合物、RNAインターカレーター化合物、ウイルス酵素阻害剤、およびN−メチル−D−アスパラギン酸受容体アンタゴニストの群から選択されることを特徴とする、請求項1に記載の薬剤の製造方法。
- 前記プロテアーゼ阻害剤が、トロンビン阻害剤、Xa因子阻害剤、VII因子阻害剤、凝固カスケードの全プロテアーゼの阻害剤、またはマトリプターゼ阻害剤であることを特徴とする、請求項2に記載の薬剤の製造方法。
- 前記プロテアーゼ阻害剤がウロキナーゼ阻害剤であることを特徴とする、請求項2に記載の薬剤の製造方法。
- 前記DNAインターカレーター化合物およびRNAインターカレーター化合物が、ペンタミジン、ジミナゼンまたはイソメタミジウムであることを特徴とする、請求項2に記載の薬剤の製造方法。
- 前記ウイルス酵素阻害剤がノイラミニダーゼ阻害剤であることを特徴とする、請求項2に記載の薬剤の製造方法。
- 前記薬物がN−メチル−D−アスパラギン酸受容体アンタゴニストであることを特徴とする、請求項2に記載の薬剤の製造方法。
- 前記薬物が、内臓リーシュマニア症および/または皮膚リーシュマニア症、トリパノソーマ症、またはニューモシスチス−カリニ肺炎の予防および治療、悪性腫瘍の成長の阻害、血液の凝固の阻害、血圧降下、神経保護、またはインフルエンザ感染症やHIV感染症等のウイルス感染症の治療のために投与されることを特徴とする、先行する請求項のいずれか1項に記載の薬剤の製造方法。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102006034256A DE102006034256A1 (de) | 2006-07-21 | 2006-07-21 | Verbesserung der Bioverfügbarkeit von Wirkstoffen mit Amidinfunktion in Arzneimitteln |
PCT/DE2007/001216 WO2008009264A1 (de) | 2006-07-21 | 2007-07-10 | Verbesserung der bioverfügbarkeit von wirkstoffen mit amidinfunktion in arzneimitteln |
Publications (1)
Publication Number | Publication Date |
---|---|
JP2009544588A true JP2009544588A (ja) | 2009-12-17 |
Family
ID=38721771
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009519786A Pending JP2009544588A (ja) | 2006-07-21 | 2007-07-10 | 薬剤中におけるアミジン基を有する活性物質の生物学的利用率の向上 |
Country Status (19)
Country | Link |
---|---|
US (1) | US20090270440A1 (ja) |
EP (2) | EP2046732B1 (ja) |
JP (1) | JP2009544588A (ja) |
KR (1) | KR20090075792A (ja) |
CN (2) | CN101506151A (ja) |
AU (1) | AU2007276526B2 (ja) |
CA (2) | CA2777173A1 (ja) |
CY (1) | CY1116941T1 (ja) |
DE (1) | DE102006034256A1 (ja) |
DK (1) | DK2046732T5 (ja) |
ES (1) | ES2555778T3 (ja) |
HK (2) | HK1210694A1 (ja) |
HU (1) | HUE025801T2 (ja) |
PL (1) | PL2046732T3 (ja) |
PT (1) | PT2046732E (ja) |
SG (1) | SG173401A1 (ja) |
SI (1) | SI2046732T1 (ja) |
WO (1) | WO2008009264A1 (ja) |
ZA (1) | ZA200901212B (ja) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE102008007381A1 (de) * | 2008-02-01 | 2009-08-13 | Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co.Kg | Amidine und Guanidine und deren Derivate zur Behandlung von Krankheiten |
DE102008007440A1 (de) * | 2008-02-01 | 2009-08-13 | Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co.Kg | Aminosäurederivate als Arzneistoffe |
US9662308B2 (en) | 2008-02-01 | 2017-05-30 | Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co. Kg | Orally bioavailable pentamidine prodrugs for the treatment of diseases |
DE102008061247A1 (de) | 2008-12-10 | 2010-06-24 | Christian-Albrechts-Universität Zu Kiel | Inhibitoren der Dimethylarginin Dimethylaminohydrolase |
DE102009004204A1 (de) * | 2009-01-09 | 2010-07-15 | Christian-Albrechts-Universität Zu Kiel | Verfahren zur verbesserten Bioaktivierung von Arzneistoffen |
CN103420994B (zh) * | 2012-05-24 | 2016-04-06 | 天津药物研究院 | 作为前药的达比加群酯衍生物及其制备方法和用途 |
CN103864710B (zh) * | 2014-03-24 | 2016-05-25 | 西安近代化学研究所 | 一种3-(3-氨基呋咱-4-基)-5-甲基-5-取代-4-羟基-4h,5h-1,2,4-恶二唑化合物的合成方法 |
CN103951660B (zh) * | 2014-03-24 | 2016-07-06 | 西安近代化学研究所 | 一种恶二唑化合物的合成方法 |
GB201615693D0 (en) | 2016-09-15 | 2016-11-02 | Combinatorx Infection Ltd | Combinations |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE4321444A1 (de) * | 1993-06-28 | 1995-01-05 | Bernd Prof Dr Clement | Pharmazeutische Zubereitung |
US5723495A (en) * | 1995-11-16 | 1998-03-03 | The University Of North Carolina At Chapel Hill | Benzamidoxime prodrugs as antipneumocystic agents |
US6740682B2 (en) * | 1997-08-29 | 2004-05-25 | Tularik Limited | Meta-benzamidine derivatives as serine protease inhibitors |
US6291514B1 (en) * | 1998-02-09 | 2001-09-18 | 3-Dimensional Pharmaceuticals, Inc. | Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors |
US7157596B2 (en) * | 2000-09-08 | 2007-01-02 | Dendreon Corporation | Inhibitors of serine protease activity of matriptase or MTSP1 |
US20040082585A1 (en) * | 2001-10-03 | 2004-04-29 | Pharmacia Corporation | Prodrugs of substituted polycyclic compounds useful for selective inhibition of the coagulation cascade |
-
2006
- 2006-07-21 DE DE102006034256A patent/DE102006034256A1/de not_active Withdrawn
-
2007
- 2007-07-10 EP EP07785614.4A patent/EP2046732B1/de not_active Not-in-force
- 2007-07-10 WO PCT/DE2007/001216 patent/WO2008009264A1/de active Application Filing
- 2007-07-10 CA CA2777173A patent/CA2777173A1/en not_active Abandoned
- 2007-07-10 SG SG2011052545A patent/SG173401A1/en unknown
- 2007-07-10 HU HUE07785614A patent/HUE025801T2/en unknown
- 2007-07-10 CA CA2658434A patent/CA2658434C/en not_active Expired - Fee Related
- 2007-07-10 PL PL07785614T patent/PL2046732T3/pl unknown
- 2007-07-10 PT PT77856144T patent/PT2046732E/pt unknown
- 2007-07-10 US US12/374,300 patent/US20090270440A1/en not_active Abandoned
- 2007-07-10 AU AU2007276526A patent/AU2007276526B2/en not_active Ceased
- 2007-07-10 JP JP2009519786A patent/JP2009544588A/ja active Pending
- 2007-07-10 ES ES07785614.4T patent/ES2555778T3/es active Active
- 2007-07-10 SI SI200731707T patent/SI2046732T1/sl unknown
- 2007-07-10 KR KR1020097002587A patent/KR20090075792A/ko not_active Application Discontinuation
- 2007-07-10 CN CNA2007800275303A patent/CN101506151A/zh active Pending
- 2007-07-10 CN CN201510045378.8A patent/CN104644619A/zh active Pending
- 2007-07-10 DK DK07785614.4T patent/DK2046732T5/en active
- 2007-07-10 EP EP15184167.3A patent/EP2987784A1/de not_active Withdrawn
-
2009
- 2009-02-20 ZA ZA2009/01212A patent/ZA200901212B/en unknown
-
2015
- 2015-11-17 CY CY20151101033T patent/CY1116941T1/el unknown
- 2015-11-19 HK HK15111410.2A patent/HK1210694A1/xx unknown
-
2016
- 2016-08-10 HK HK16109558.7A patent/HK1221455A1/zh unknown
Also Published As
Publication number | Publication date |
---|---|
HK1221455A1 (zh) | 2017-06-02 |
SG173401A1 (en) | 2011-08-29 |
DK2046732T3 (en) | 2015-11-16 |
AU2007276526A1 (en) | 2008-01-24 |
DE102006034256A1 (de) | 2008-01-31 |
WO2008009264A1 (de) | 2008-01-24 |
HUE025801T2 (en) | 2016-04-28 |
CA2658434E (en) | 2008-01-24 |
EP2987784A1 (de) | 2016-02-24 |
DK2046732T5 (en) | 2016-01-04 |
PL2046732T3 (pl) | 2016-02-29 |
EP2046732A1 (de) | 2009-04-15 |
SI2046732T1 (sl) | 2016-02-29 |
CA2658434C (en) | 2012-08-14 |
CY1116941T1 (el) | 2017-04-05 |
HK1210694A1 (en) | 2016-05-06 |
EP2046732B1 (de) | 2015-09-09 |
CN101506151A (zh) | 2009-08-12 |
ZA200901212B (en) | 2010-02-24 |
PT2046732E (pt) | 2016-01-06 |
US20090270440A1 (en) | 2009-10-29 |
CA2658434A1 (en) | 2008-01-24 |
AU2007276526B2 (en) | 2011-08-11 |
ES2555778T3 (es) | 2016-01-08 |
CN104644619A (zh) | 2015-05-27 |
CA2777173A1 (en) | 2008-01-24 |
KR20090075792A (ko) | 2009-07-09 |
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