JP4737686B2 - 新しい医薬 - Google Patents
新しい医薬 Download PDFInfo
- Publication number
- JP4737686B2 JP4737686B2 JP2006505443A JP2006505443A JP4737686B2 JP 4737686 B2 JP4737686 B2 JP 4737686B2 JP 2006505443 A JP2006505443 A JP 2006505443A JP 2006505443 A JP2006505443 A JP 2006505443A JP 4737686 B2 JP4737686 B2 JP 4737686B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- formula
- methoxy
- proteinuria
- treatment
- 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.)
- Expired - Fee Related
Links
Classifications
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
-
- 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
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- 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)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Saccharide Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Description
R1は、ピリジル又はチアゾリルであり、そしてこれらはいずれも、場合によりC1-8アルキル又はC2-8アルケニルで置換されていてもよく;そして
a)R2は、メトキシであり、かつnは、0又は1であるか;あるいは
b)R2は、塩素であり、かつnは、0である]で示される化合物及び薬学的に許容しうるその塩に関するものであり、そして驚くべきことにこれらは、特にII型糖尿病の患者に投与されると、顕著なタンパク尿低下作用を示す。
以下の成分を含む錠剤は、従来法で製造することができる:
式(I)の化合物 10.1−100.0
乳糖 125.0
トウモロコシデンプン 75.0
タルク 4.0
ステアリン酸マグネシウム 1.0
式(I)の化合物 25.0
乳糖 150.0
トウモロコシデンプン 20.0
タルク 5.0
塩化ナトリウム 8.5mg
トリス(ヒドロキシメチル)アミノメタン 0.5mg
0.1N HCl PH8まで
注射用水 1.0mlまで
a)第1の単位投与剤形中のある量の式(I)の化合物;
b)第2等の単位投与剤形中の、ARB、ACEI、レニン阻害薬、アルドースレダクターゼ阻害薬、プロテインキナーゼCベータ−阻害薬、AGE架橋ブレーカー/阻害薬、ヘパリン型分子及びアルドステロン受容体アンタゴニストよりなる群から選択される、ある量の少なくとも1つの治療剤;並びに
c)該第1、第2等の単位投与剤形を含む容器
を含むことを特徴とするキットである。
本試験には、糖尿病性腎症の患者23名を含めた。本試験は、二重盲検の無作為化されたプラセボ対照試験である。全ての患者は、5−メチル−ピリジン−2−スルホン酸[6−メトキシ−5−(2−メトキシ−フェノキシ)−2−ピリジン−4−イル−ピリミジン−4−イル]−アミド(化合物A)での処置を開始する前の4週間、高用量アンギオテンシン受容体ブロッカー(ARB)で処置した。患者は、高用量ARBでの4週間の処置期間の終わりに、その24時間タンパク尿が>300mg/24時間であったならば試験に含めた。患者は無作為化して3群とした:高用量ARBに加えて、1日1回化合物A 20mg、化合物A 50mg、又はプラセボ。処置期間は4週間とした。主要な変数は、24時間タンパク尿とした。
24時間タンパク尿データにより、個々の群についてタンパク尿の低下が、化合物A 20mgでは−1.0±1.96g/24時間、そして化合物A 50mgでは−1.3±1.3g/24時間であることが判った。プラセボ群は、0.5±1.78g/24時間のタンパク尿の上昇を示した。この3群には化合物Aでの処置の開始時点の24時間タンパク尿には差があったが、プラセボ群と違って、化合物Aで処置した2群は、およそ1g/24時間の24時間タンパク尿の平均低下を示し、そしてこれは臨床的に意義がある。
Claims (4)
- 式(I)の化合物が、5−メチル−ピリジン−2−スルホン酸[6−メトキシ−5−(2−メトキシ−フェノキシ)−2−ピリジン−4−イル−ピリミジン−4−イル]−アミドである、請求項1記載の使用。
- 式(I)の化合物が、5−メチル−ピリジン−2−スルホン酸[6−メトキシ−5−(2−メトキシ−フェノキシ)−2−ピリジン−4−イル−ピリミジン−4−イル]−アミドである、請求項3記載の組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP03100549.9 | 2003-03-06 | ||
EP03100549A EP1454625A1 (en) | 2003-03-06 | 2003-03-06 | Pyridylsulfonamidyl-pyrimidines for the treatment of diabetic nephropathies |
PCT/EP2004/050242 WO2004078104A2 (en) | 2003-03-06 | 2004-03-03 | Pyridylsulfonamido pyrimidines for treating diabetic nephropathy |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2006519817A JP2006519817A (ja) | 2006-08-31 |
JP4737686B2 true JP4737686B2 (ja) | 2011-08-03 |
Family
ID=32799012
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2006505443A Expired - Fee Related JP4737686B2 (ja) | 2003-03-06 | 2004-03-03 | 新しい医薬 |
Country Status (27)
Country | Link |
---|---|
US (2) | US20060094731A1 (ja) |
EP (2) | EP1454625A1 (ja) |
JP (1) | JP4737686B2 (ja) |
KR (1) | KR101099189B1 (ja) |
CN (1) | CN100453081C (ja) |
AT (1) | ATE395063T1 (ja) |
AU (2) | AU2004216858B2 (ja) |
BR (1) | BRPI0408082A (ja) |
CA (1) | CA2517930C (ja) |
CY (1) | CY1108241T1 (ja) |
DE (1) | DE602004013734D1 (ja) |
DK (1) | DK1601361T3 (ja) |
EC (1) | ECSP056060A (ja) |
ES (1) | ES2305737T3 (ja) |
HK (1) | HK1083761A1 (ja) |
HR (1) | HRP20050860A2 (ja) |
IL (1) | IL170626A (ja) |
MX (1) | MXPA05009478A (ja) |
NO (1) | NO20054148L (ja) |
NZ (1) | NZ542155A (ja) |
PL (1) | PL1601361T3 (ja) |
PT (1) | PT1601361E (ja) |
RS (1) | RS20050683A (ja) |
SI (1) | SI1601361T1 (ja) |
UA (1) | UA82087C2 (ja) |
WO (1) | WO2004078104A2 (ja) |
ZA (1) | ZA200507122B (ja) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1595880A1 (en) * | 2004-05-13 | 2005-11-16 | Speedel Pharma AG | Crystalline forms of a pyridinyl-sulfonamide and their use as endothelin receptor antagonists |
WO2011158933A1 (ja) | 2010-06-17 | 2011-12-22 | 日東電工株式会社 | 腎線維症処置剤 |
WO2007031501A2 (en) * | 2005-09-12 | 2007-03-22 | Speedel Pharma Ag | Pyridylsulfonamidyl-pyrimidines for the prevention of blood vessel graft failure |
CN109260164A (zh) * | 2018-10-07 | 2019-01-25 | 威海贯标信息科技有限公司 | 一种阿伏生坦片剂组合物 |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH08208625A (ja) * | 1994-11-25 | 1996-08-13 | F Hoffmann La Roche Ag | 新規スルホンアミド類 |
JP2002538156A (ja) * | 1999-03-03 | 2002-11-12 | エフ.ホフマン−ラ ロシュ アーゲー | 4−ヘテロシクリルスルホンアミジル−6−メトキシ−5−(2−メトキシ−フェノキシ)−2−ピリジル−ピリミジン誘導体、その製造方法及びエンドセリン受容体アンタゴニストとしての使用 |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
HUT76542A (en) * | 1994-03-17 | 1997-09-29 | Ciba Geigy Ag | Use of valsartan for the preparation of pharmaceutical composition serving for the treatment of diabetic nephropathy |
JPH11513022A (ja) * | 1995-08-02 | 1999-11-09 | スミスクライン・ビーチャム・コーポレイション | エンドセリンレセプターアンタゴニスト |
AU2001263850A1 (en) * | 2000-04-20 | 2001-11-07 | Actelion Pharmaceuticals Ltd | Pyrimidine-sulfonamides having endothelin-antagonist activity |
-
2003
- 2003-03-06 EP EP03100549A patent/EP1454625A1/en not_active Withdrawn
-
2004
- 2004-03-03 DE DE602004013734T patent/DE602004013734D1/de not_active Expired - Lifetime
- 2004-03-03 CA CA2517930A patent/CA2517930C/en not_active Expired - Fee Related
- 2004-03-03 RS YUP-2005/0683A patent/RS20050683A/sr unknown
- 2004-03-03 AU AU2004216858A patent/AU2004216858B2/en not_active Ceased
- 2004-03-03 DK DK04716605T patent/DK1601361T3/da active
- 2004-03-03 EP EP04716605A patent/EP1601361B1/en not_active Expired - Lifetime
- 2004-03-03 SI SI200430798T patent/SI1601361T1/sl unknown
- 2004-03-03 UA UAA200509348A patent/UA82087C2/uk unknown
- 2004-03-03 WO PCT/EP2004/050242 patent/WO2004078104A2/en active IP Right Grant
- 2004-03-03 BR BRPI0408082-3A patent/BRPI0408082A/pt not_active IP Right Cessation
- 2004-03-03 US US10/548,080 patent/US20060094731A1/en not_active Abandoned
- 2004-03-03 AT AT04716605T patent/ATE395063T1/de active
- 2004-03-03 CN CNB2004800058469A patent/CN100453081C/zh not_active Expired - Fee Related
- 2004-03-03 PT PT04716605T patent/PT1601361E/pt unknown
- 2004-03-03 PL PL04716605T patent/PL1601361T3/pl unknown
- 2004-03-03 ES ES04716605T patent/ES2305737T3/es not_active Expired - Lifetime
- 2004-03-03 JP JP2006505443A patent/JP4737686B2/ja not_active Expired - Fee Related
- 2004-03-03 MX MXPA05009478A patent/MXPA05009478A/es active IP Right Grant
- 2004-03-03 KR KR1020057016511A patent/KR101099189B1/ko not_active IP Right Cessation
- 2004-03-03 NZ NZ542155A patent/NZ542155A/en not_active IP Right Cessation
-
2005
- 2005-09-01 IL IL170626A patent/IL170626A/en not_active IP Right Cessation
- 2005-09-05 ZA ZA200507122A patent/ZA200507122B/en unknown
- 2005-09-06 NO NO20054148A patent/NO20054148L/no not_active Application Discontinuation
- 2005-09-28 HR HR20050860A patent/HRP20050860A2/hr not_active Application Discontinuation
- 2005-09-29 EC EC2005006060A patent/ECSP056060A/es unknown
-
2006
- 2006-03-30 HK HK06103985A patent/HK1083761A1/xx not_active IP Right Cessation
-
2008
- 2008-07-28 US US12/219,751 patent/US20090005404A1/en not_active Abandoned
- 2008-08-06 CY CY20081100825T patent/CY1108241T1/el unknown
-
2009
- 2009-10-14 AU AU2009225323A patent/AU2009225323B2/en not_active Expired - Fee Related
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH08208625A (ja) * | 1994-11-25 | 1996-08-13 | F Hoffmann La Roche Ag | 新規スルホンアミド類 |
JP2002538156A (ja) * | 1999-03-03 | 2002-11-12 | エフ.ホフマン−ラ ロシュ アーゲー | 4−ヘテロシクリルスルホンアミジル−6−メトキシ−5−(2−メトキシ−フェノキシ)−2−ピリジル−ピリミジン誘導体、その製造方法及びエンドセリン受容体アンタゴニストとしての使用 |
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