JPH10500977A - ピリジルビスホスホン酸エステルよりなる治療用活性薬剤 - Google Patents
ピリジルビスホスホン酸エステルよりなる治療用活性薬剤Info
- Publication number
- JPH10500977A JPH10500977A JP8500400A JP50040096A JPH10500977A JP H10500977 A JPH10500977 A JP H10500977A JP 8500400 A JP8500400 A JP 8500400A JP 50040096 A JP50040096 A JP 50040096A JP H10500977 A JPH10500977 A JP H10500977A
- Authority
- JP
- Japan
- Prior art keywords
- pyridyl
- methylidene
- amino
- bisphosphonic acid
- group
- 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.)
- Granted
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
- A61K31/66—Phosphorus compounds
- A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- A61P3/02—Nutrients, e.g. vitamins, minerals
-
- 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)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Detergent Compositions (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.式Iで表わされるピリジルアミノメチリデンビスホスホン酸四エステル化合 物よりなる治療用活性薬剤。 [式中、R1〜R4は、各々、C1〜C5の直鎖状又は分岐状アルキル基であり、X 及びYは、各々独立に、水素、C1〜C5の直鎖状又は分岐状アルキル基、ハロゲ ン、水酸基、C1〜C5アルコキシ基、ベンジルオキシ基、アシルオキシ基、ニト ロ基、トリフルオロメチル基、又はNR5R6(R5及びR6は、同じでも異なって いてもよく、水素、C1〜C5アルキル基又はC1〜C5アシル基である)である。 ] 2.式Iにおいて、アルコキシ基及びアシル基中のアルキル基も含めて、C1〜 C5のアルキル基がメチル基又はエチル基であり、ハロゲンが塩素である請求項 1に記載の治療用活性薬剤。 3.式Iにおいて、R1〜R4は同一の基であって、好ましく はエチル基である請求項1又は2に記載の治療用活性薬剤。 4.式Iにおいて、ピリジル基が2−ピリジル基である請求項3に記載の治療用 活性薬剤。 5.[(2−ピリジルアミノ)メチリデン]ビスホスホン酸四エチルエステル、 [{(3−ヒドロキシ−2−ピリジル)アミノ}メチリデン]ビスホスホン 酸四エチルエステル、 [{(6−メトキシ−3−ピリジル)アミノ}メチリデン]ビスホスホン酸 四エチルエステル、 [(4−ピリジルアミノ)メチリデン]ビスホスホン酸四エチルエステル、 [{(5−クロロ−2−ピリジル)アミノ}メチリデン]ビスホスホン酸四 エチルエステル、 [{(5−メトキシ−2−ピリジル)アミノ}メチリデン]ビスホスホン酸 四エチルエステル、 [{(6−アミノ−2−ピリジル)アミノ}メチリデン]ビスホスホン酸四 エチルエステル、 [{(3−ニトロ−2−ピリジル)アミノ}メチリデン]ビスホスホン酸四 エチルエステル、 [{(3,5−ジクロロ−2−ピリジル)アミノ}メチリデン]ビスホスホ ン酸四エチルエステル、 [{(6−ヒドロキシ−3−ピリジル)アミノ}メチリ デン]ビスホスホン酸四エチルエステル、 [{(5−ヒドロキシ−2−ピリジル)アミノ}メチリデン]ビスホスホン 酸四エチルエステル、 [{(3−クロロ−5−トリフルオロメチルーピリジル)アミノ}メチリデ ン]ビスホスホン酸四エチルエステル、 [{(2−クロロ−3−ピリジル)アミノ}メチリデン]ビスホスホン酸四 エチルエステル、 [{(6−クロロ−3−ピリジル)アミノ}メチリデン]ビスホスホン酸四 エチルエステル、 [{(3−ベンジルオキシ−2−ピリジル)アミノ}メチリデン]ビスホス ホン酸四エチルエステル、 [{(5−ニトロ−2−ピリジル)アミノ}メチリデン]ビスホスホン酸四 エチルエステル、又は [{(5−ベンジルオキシ−2−ピリジル)アミノ}メチリデン]ビスホス ホン酸四エチルエステル、 である請求項1に記載の治療用活性薬剤。 6.悪性腫瘍による溶解性骨病、パジェット病、一次及び二次骨粗鬆症などの骨 病治療に使用するための請求項1〜5のいずれかに記載の治療用活性薬剤。 7.製薬的に許容される担体及び有効量の請求項1〜5のいずれかに記載の化合 物を含有することを特徴とする、悪性腫瘍による溶解性骨病、パジェット病、一 次および二次骨粗鬆 症などの骨病治療用医薬組成物。 8.悪性腫瘍による溶解性骨病、パジェット病、一次及び二次骨粗鬆症などの骨 病治療用医薬組成物製造に用いる請求項1〜5のいずれかに記載の治療用活性薬 剤。 9.悪性腫瘍による溶解性骨病、パジェット病、一次及び二次骨粗鬆症などの骨 病に感染した哺乳動物に対し、有効量の請求項1〜5のいずれかに記載の治療用 活性薬剤又は請求項7に記載の組成物を投与することを包含する該骨病の治療方 法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SE9402001-3 | 1994-06-09 | ||
SE9402001A SE9402001D0 (sv) | 1994-06-09 | 1994-06-09 | Pyridylbisphosphonates for use as a therapeutical agent |
PCT/FI1995/000315 WO1995033466A1 (en) | 1994-06-09 | 1995-06-02 | Pyridylbisphosphonates for use as a therapeutical agent |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH10500977A true JPH10500977A (ja) | 1998-01-27 |
JP3883137B2 JP3883137B2 (ja) | 2007-02-21 |
Family
ID=20394303
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP50040096A Expired - Lifetime JP3883137B2 (ja) | 1994-06-09 | 1995-06-02 | ピリジルビスホスホン酸エステルよりなる治療用活性薬剤 |
Country Status (27)
Country | Link |
---|---|
US (2) | US5866556A (ja) |
EP (1) | EP0762883B1 (ja) |
JP (1) | JP3883137B2 (ja) |
KR (1) | KR100363692B1 (ja) |
CN (1) | CN1077792C (ja) |
AT (1) | ATE208622T1 (ja) |
AU (1) | AU691616B2 (ja) |
BG (1) | BG63104B1 (ja) |
BR (1) | BR9508185A (ja) |
CZ (1) | CZ291477B6 (ja) |
DE (1) | DE69523914T2 (ja) |
DK (1) | DK0762883T3 (ja) |
EE (1) | EE03475B1 (ja) |
ES (1) | ES2162919T3 (ja) |
HK (1) | HK1012572A1 (ja) |
HU (1) | HU228618B1 (ja) |
IS (1) | IS1801B (ja) |
NO (1) | NO311069B1 (ja) |
NZ (1) | NZ287094A (ja) |
PL (1) | PL180705B1 (ja) |
PT (1) | PT762883E (ja) |
RO (1) | RO119433B1 (ja) |
RU (1) | RU2154482C2 (ja) |
SE (1) | SE9402001D0 (ja) |
SK (1) | SK282650B6 (ja) |
UA (1) | UA43918C2 (ja) |
WO (1) | WO1995033466A1 (ja) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ATE293450T1 (de) * | 1999-05-21 | 2005-05-15 | Novartis Pharma Gmbh | Verwendung von biphosphonsäuren zur behandlung von angiogenese |
IL150062A0 (en) | 1999-12-17 | 2002-12-01 | Ariad Pharma Inc | Proton pump inhibitors |
US20020132819A1 (en) * | 1999-12-17 | 2002-09-19 | Metcalf Chester A. | Novel purinse |
IL150059A0 (en) * | 1999-12-17 | 2002-12-01 | Ariad Pharma Inc | Novel heterocycles |
WO2002034269A1 (en) * | 2000-10-27 | 2002-05-02 | Schering Oy | Method for the preparation of a pharmaceutical composition, and its use |
WO2003070169A2 (en) * | 2002-02-19 | 2003-08-28 | Ilex Products, Inc. | Aminodiphosphonate apolipoprotein e modulators |
TW200413381A (en) * | 2002-11-04 | 2004-08-01 | Hoffmann La Roche | Novel amino-substituted dihydropyrimido [4,5-d]pyrimidinone derivatives, their manufacture and use as pharmaceutical agents |
US20050010305A1 (en) * | 2003-01-28 | 2005-01-13 | Lee Francis Y. | Novel bone graft composite |
US20050065171A1 (en) * | 2003-06-25 | 2005-03-24 | Shakespeare William C. | Substituted purine derivatives |
JP2005060303A (ja) * | 2003-08-12 | 2005-03-10 | Sutaagen:Kk | 不動性骨粗鬆の治療または予防剤 |
US7862552B2 (en) * | 2005-05-09 | 2011-01-04 | Boston Scientific Scimed, Inc. | Medical devices for treating urological and uterine conditions |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US447256A (en) * | 1891-02-24 | Apparatus for flashing and exhausting incandescent electric lamps | ||
US4447256A (en) * | 1977-07-20 | 1984-05-08 | Nissan Chemical Industries, Ltd. | N-(Unsubstituted or substituted pyridyl)aminomethylene-diphosphonic acids, herbicidal compositions containing same, their use for herbicides, and process for preparing same |
IL77243A (en) * | 1984-12-21 | 1996-11-14 | Procter & Gamble | Pharmaceutical compositions containing geminal diphosphonic acid compounds and certain such novel compounds |
US4973576A (en) * | 1987-03-10 | 1990-11-27 | Yamanouchi Pharmaceutical Co., Ltd. | Bisphophonic acid derivatives and pharmaceutical compositions containing the same |
EP0282309A3 (en) * | 1987-03-11 | 1990-03-14 | Yamanouchi Pharmaceutical Co. Ltd. | Azole-aminomethylene bisphosphonic acid derivatives |
-
1994
- 1994-06-09 SE SE9402001A patent/SE9402001D0/xx unknown
-
1995
- 1995-02-06 UA UA97010075A patent/UA43918C2/uk unknown
- 1995-06-02 CN CN95193416A patent/CN1077792C/zh not_active Expired - Lifetime
- 1995-06-02 PL PL95317612A patent/PL180705B1/pl unknown
- 1995-06-02 HU HU9603375A patent/HU228618B1/hu unknown
- 1995-06-02 PT PT95920122T patent/PT762883E/pt unknown
- 1995-06-02 ES ES95920122T patent/ES2162919T3/es not_active Expired - Lifetime
- 1995-06-02 BR BR9508185A patent/BR9508185A/pt not_active IP Right Cessation
- 1995-06-02 RO RO96-02286A patent/RO119433B1/ro unknown
- 1995-06-02 KR KR1019960706991A patent/KR100363692B1/ko not_active IP Right Cessation
- 1995-06-02 SK SK1572-96A patent/SK282650B6/sk not_active IP Right Cessation
- 1995-06-02 RU RU97100161/14A patent/RU2154482C2/ru active
- 1995-06-02 EE EE9600191A patent/EE03475B1/xx unknown
- 1995-06-02 AT AT95920122T patent/ATE208622T1/de active
- 1995-06-02 JP JP50040096A patent/JP3883137B2/ja not_active Expired - Lifetime
- 1995-06-02 CZ CZ19963561A patent/CZ291477B6/cs not_active IP Right Cessation
- 1995-06-02 NZ NZ287094A patent/NZ287094A/en not_active IP Right Cessation
- 1995-06-02 WO PCT/FI1995/000315 patent/WO1995033466A1/en active IP Right Grant
- 1995-06-02 DK DK95920122T patent/DK0762883T3/da active
- 1995-06-02 EP EP95920122A patent/EP0762883B1/en not_active Expired - Lifetime
- 1995-06-02 AU AU25698/95A patent/AU691616B2/en not_active Expired
- 1995-06-02 US US08/750,355 patent/US5866556A/en not_active Expired - Lifetime
- 1995-06-02 DE DE69523914T patent/DE69523914T2/de not_active Expired - Lifetime
-
1996
- 1996-12-02 IS IS4392A patent/IS1801B/is unknown
- 1996-12-06 NO NO19965228A patent/NO311069B1/no not_active IP Right Cessation
-
1997
- 1997-01-06 BG BG101116A patent/BG63104B1/bg unknown
-
1998
- 1998-12-17 HK HK98113970A patent/HK1012572A1/xx not_active IP Right Cessation
- 1998-12-23 US US09/219,692 patent/US6083938A/en not_active Expired - Lifetime
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