KR920000778A - 비스포스폰산 유도체, 그의 제조와 용도 - Google Patents
비스포스폰산 유도체, 그의 제조와 용도 Download PDFInfo
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- KR920000778A KR920000778A KR1019910010616A KR910010616A KR920000778A KR 920000778 A KR920000778 A KR 920000778A KR 1019910010616 A KR1019910010616 A KR 1019910010616A KR 910010616 A KR910010616 A KR 910010616A KR 920000778 A KR920000778 A KR 920000778A
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids, i.e. RP(=X)(XH)2 (X = S, Se)
- C07F9/40—Esters thereof
- C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
- C07F9/4025—Esters of poly(thio)phosphonic acids
- C07F9/405—Esters of poly(thio)phosphonic acids containing nitrogen substituent, e.g. N.....H or N-hydrocarbon group which can be substituted by halogen or nitro(so), N.....O, N.....S, N.....C(=X)- (X =O, S), N.....N, N...C(=X)...N (X =O, S)
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- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A—HUMAN NECESSITIES
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- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids, i.e. RP(=X)(XH)2 (X = S, Se)
- C07F9/3804—Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids, i.e. RP(=X)(XH)2 (X = S, Se) not used, see subgroups
- C07F9/3839—Polyphosphonic acids
- C07F9/3873—Polyphosphonic acids containing nitrogen substituent, e.g. N.....H or N-hydrocarbon group which can be substituted by halogen or nitro(so), N.....O, N.....S, N.....C(=X)- (X =O, S), N.....N, N...C(=X)...N (X =O, S)
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/58—Pyridine rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
- C07F9/6503—Five-membered rings
- C07F9/6506—Five-membered rings having the nitrogen atoms in positions 1 and 3
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
- C07F9/6509—Six-membered rings
- C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6524—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having four or more nitrogen atoms as the only ring hetero atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6536—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
- C07F9/6539—Five-membered rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (15)
- 하기 일반식(I)의 비스포스폰산 유도체 또는 그것의 염:(식중, A는 임의로 치환된 고리기이고, R1은 수소원자 또는 저급 알카노일기이며, R2, R3, R4및 R5는 같거나 다르고, 수소원자 또는 저급알킬기이며, m은 0,1 또는 2이며, n은 2-10의 정수이다.)
- 제1항에 있어서, 임의로 치환된 고리기의 고리기는 C6-14방향족 탄화수소기, 1-4개의 헤테로원자를 함유하는 5 또는 6원 방향족 헤테로고리기, C6-14방향족 탄화수소고리 또는 1-4개의 질소, 산소 및/또는 황원자를 함유하는 5 또는 6원 방향족 헤테로고리와 공역된 1-4개의 질소, 산소 및/또는 황원자를 함유하는 5 또는 6원 방향족 헤테로고리기, C3-7시클로알킬기, 또는 1-4개의 헤테로원자들을 함유하는 5 또는 6원 비-방향족 헤테로 고리기이며, 이들 고리기는 (1)할로겐원자, (2)니트로, (3)할로겐원자, 히드록시기 및 C1-6알콕시기로 구성되는 군에서 선택된 1-3개의 치환체로 치환될수 있는 C1-7알킬기, (4)할로겐 원자, 히드록시기 및 C1-6알콕시기로 구성되는 군에서 선택된 1-3개의 치환체로 치환될 수 있는 C3-7시클로알킬기, (5)히드록실, (6)할로겐, 히드록실 및 C1-6알콕시기로 구성되는 군에서 선택된 1-3개의 치환체로 치환될 수 있는 C1-6알콕시기, C4-6시클로알콕시기, C2-6알켄일옥시, C6-19아랄킬옥시, C2-7알카노일옥시 및 C6-14아릴옥시로 구성되는 군에서 선택된 보호된 히드록시기, (7)티올 및 (8)할로겐, 히드록시기 및 C1-6알콕시기로 구성되는 군에서 선택되는 1-3개의 치환체로 치환될 수 있는 C1-6알킬티오, C4-7시클로알킬티오, C7-19아랄킬티오 및 C2-7알카노일 티오기로 구성되는 군에서 선택되는 보호된 티올기의 군에서 선택되는 1-4개의 치환체로 임의로 치환된 것임을 특징으로 하는 화합물.
- 제1항에 있어서, R1으로 표시되는 저급알카노일이 C1-6알킬-카르보닐기인 화합물.
- 제1항에 있어서, R2, R3, R4및 R5로 표시되는 저급 알킬기가 C1-4알킬기인 화합물.
- 제1항에 있어서, A가 페닐기인 화합물.
- 제1항에 있어서, A는 피리딜기인 화합물.
- 제1항에 있어서, 4-(페닐티오)부틸아미노메틸렌비스포스폰산 또는 그것의 염 또는 C1-4알킬에스테르인 화합물.
- 제1항에 있어서, 4-(페닐티오)부틸아미노메틸렌비스폰스폰산인 화합물.
- 제1항에 있어서, 4-(2-피리딜티오)부틸아미노메틸렌비스포스폰산 또는 그것의 염 또는 C1-4알킬에스테르기인 화합물.
- 제1항에 있어서, 4-(2-피리딜티오)부틸아미노메틸렌비스포스폰산인 화합물.
- 제1항에 있어서, 4-[(4-메톡시페닐)티오)부틸아미노메틸렌비스포스폰산 또는 그것의 염 또는 C1-4알킬 에스테르기인 화합물.
- 제1항에 있어서, 4-[(1-메틸-1,2,3,4-테트라졸-5-일)티오]부틸아미노메틸렌비스포스폰산 또는 그것의 염 또는 C1-4알킬에스테르기인 화합물.
- 제1항에 있어서, 4-[(2-티아졸일)티오]부틸아미노메틸렌비스포스폰산 또는 그것의 염 또는 C1-4알킬에스테르기인 화합물.
- 일반식(Ⅱ)의 아민유도체를 일반식(Ⅲ)의 오르토포름산 유도체 및 일반식(Ⅳ)의 포스파이트 유도체와 반응시킨 다음, 임의로 아실화, 산화 및/또는 가수분해 시키는 것을 특징으로 하는 하기 일반식(I)의 화합물의 제조방법.(식중, A는 임의로 치환된 고리기이고, R1은 수소원자 또는 저급 알카노일기이며, R2, R3, R4및 R5는 같거나 다르고, 수소원자 또는 저급알킬기이며, m은 0,1 또는 2이며, n은 2-10의 정수이며, R6는 저급 알킬기이고, R7, R8, R9및 R10은 같거나 다르며 저급 알킬기이다.)
- 하기 일반식(I)의 화합물 또는 그것의 염, 그리고 약학적 허용가능한 담체, 희석제 또는 부형제를 함유하는 골-재흡수억제 조성물.(식중, A는 임의로 치환된 고리기이고, R1은 수소원자 또는 저급 알카노일기이며, R2, R3, R4및 R5는 같거나 다르고, 수소원자 또는 저급알킬기이며, m은 0,1 또는 2이며, n은 2-10의 정수이다.)※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
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JP16760090 | 1990-06-25 | ||
JP167600/1990 | 1990-06-25 | ||
JP410501/1990 | 1990-12-12 | ||
JP41050190 | 1990-12-12 | ||
JP9208091 | 1991-04-23 | ||
JP092080/1991 | 1991-04-23 |
Publications (1)
Publication Number | Publication Date |
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KR920000778A true KR920000778A (ko) | 1992-01-29 |
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Application Number | Title | Priority Date | Filing Date |
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KR1019910010616A KR920000778A (ko) | 1990-06-25 | 1991-06-25 | 비스포스폰산 유도체, 그의 제조와 용도 |
Country Status (13)
Country | Link |
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US (2) | US5376647A (ko) |
EP (1) | EP0464509B1 (ko) |
JP (1) | JP3072390B2 (ko) |
KR (1) | KR920000778A (ko) |
CN (1) | CN1057654A (ko) |
AT (1) | ATE127123T1 (ko) |
AU (1) | AU637508B2 (ko) |
CA (1) | CA2045293A1 (ko) |
DE (1) | DE69112511T2 (ko) |
FI (1) | FI913067A (ko) |
HU (1) | HUT57787A (ko) |
IE (1) | IE912115A1 (ko) |
NO (1) | NO912462L (ko) |
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EP0531253B1 (en) * | 1991-08-27 | 1997-01-08 | Ciba-Geigy Ag | N-substituted aminomethanediphosphonic acids |
EP0541037A3 (en) * | 1991-11-06 | 1997-02-26 | Takeda Chemical Industries Ltd | Squalene synthetase inhibitory composition and use thereof |
ATE290871T1 (de) * | 1995-09-29 | 2005-04-15 | Novartis Pharma Gmbh | Verfahren zur behandlung navikularer krankheiten bei pferden |
PL205637B1 (pl) * | 2004-10-22 | 2010-05-31 | Inst Farmaceutyczny | Sposób wytwarzania kwasu (R,E)-(1-{1-{3-[2-(7-chlorochinolin-2-ylo)etenylo]fenylo}-3-[2-(1-hydroksy-1-metyloetylo)fenylo] propylosulfanylometylo}cyklopropylo)octowego i/lub jego farmaceutycznie dopuszczalnych soli |
PL205444B1 (pl) * | 2007-05-02 | 2010-04-30 | Zak & Lstrok Ady Farmaceutyczn | Sposób wytwarzania soli sodowej kwasu 1-(((1(R)-(3-(2-(7--chloro-2- chinolinylo)-etenylo)fenylo)-3-(2-(1-hydroksy-1- metyloetylo)fenylo)propylo)sulfanylo)metylo)-cyklopropanooctowego |
US20160016982A1 (en) | 2009-07-31 | 2016-01-21 | Thar Pharmaceuticals, Inc. | Crystallization method and bioavailability |
ES2650665T3 (es) | 2009-07-31 | 2018-01-19 | Grünenthal GmbH | Método de cristalización y biodisponibilidad |
US9169279B2 (en) | 2009-07-31 | 2015-10-27 | Thar Pharmaceuticals, Inc. | Crystallization method and bioavailability |
US8748582B2 (en) | 2009-10-15 | 2014-06-10 | Monash University | Affinity ligands and methods for protein purification |
WO2012071517A2 (en) | 2010-11-24 | 2012-05-31 | Thar Pharmaceuticals, Inc. | Novel crystalline forms |
WO2017208070A1 (en) | 2016-05-31 | 2017-12-07 | Grünenthal GmbH | Bisphosphonic acid and coformers with lysin, glycin, nicotinamide for treating psoriatic arthritis |
JP2019518792A (ja) * | 2016-06-03 | 2019-07-04 | バイオビンク エルエルシー | ビスホスホネート・キノロン複合体及びそれらの用途 |
US10865220B2 (en) | 2016-06-03 | 2020-12-15 | Biovinc, Llc | Bisphosphonate quinolone conjugates and uses thereof |
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SU445675A1 (ru) * | 1972-12-28 | 1974-10-05 | Казанский государственный университет им. В.И.Ульянова-Ленина | Способ получени =фениламинотетралкилдифосфонметана |
NL7613779A (nl) * | 1975-12-16 | 1977-06-20 | Hoechst Ag | Werkwijze voor het bereiden van fosfor bevat- tende polyadducten. |
JPS5437829A (en) * | 1977-08-29 | 1979-03-20 | Nissan Chem Ind Ltd | Disulfonic acid type herbicidal and insecticidal agents |
FR2531088B1 (fr) * | 1982-07-29 | 1987-08-28 | Sanofi Sa | Produits anti-inflammatoires derives de l'acide methylenediphosphonique et leur procede de preparation |
FR2558837B1 (fr) * | 1984-01-26 | 1986-06-27 | Sanofi Sa | Derives de l'acide methylenediphosphonique, procede d'obtention et medicaments antirhumatismaux les contenant |
DE3540150A1 (de) * | 1985-11-13 | 1987-05-14 | Boehringer Mannheim Gmbh | Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel |
US4902679A (en) * | 1985-12-13 | 1990-02-20 | Norwich Eaton Pharmaceuticals, Inc. | Methods of treating diseases with certain geminal diphosphonates |
ES2039237T3 (es) * | 1986-04-24 | 1993-09-16 | Fujisawa Pharmaceutical Co., Ltd. | Procedimiento para preparar nuevos compuestos de acido difosfonico. |
US4973576A (en) * | 1987-03-10 | 1990-11-27 | Yamanouchi Pharmaceutical Co., Ltd. | Bisphophonic acid derivatives and pharmaceutical compositions containing the same |
KR880011136A (ko) * | 1987-03-11 | 1988-10-26 | 모리오까 시게오 | 아졸- 아미노메틸렌 비스포스폰산 유도체 |
IL86951A (en) * | 1987-07-06 | 1996-07-23 | Procter & Gamble Pharma | Methylene phosphonoalkylphosphinates and pharmaceutical preparations containing them |
CA1339805C (en) * | 1988-01-20 | 1998-04-07 | Yasuo Isomura | (cycloalkylamino)methylenebis(phosphonic acid) and medicines containing the same as an active |
JPH01258695A (ja) * | 1988-04-07 | 1989-10-16 | Yamanouchi Pharmaceut Co Ltd | (ピラゾリルアミノ)メチレンビス(ホスホン酸)誘導体及びその医薬 |
US4933472A (en) * | 1988-04-08 | 1990-06-12 | Yamanouchi Pharmaceutical Co., Ltd. | Substituted aminomethylenebis(phosphonic acid) derivatives |
PH26923A (en) * | 1989-03-08 | 1992-12-03 | Ciba Geigy | N-substituted amino alkanediphosphonic acids |
-
1991
- 1991-06-19 IE IE211591A patent/IE912115A1/en unknown
- 1991-06-21 AT AT91110239T patent/ATE127123T1/de not_active IP Right Cessation
- 1991-06-21 DE DE69112511T patent/DE69112511T2/de not_active Expired - Fee Related
- 1991-06-21 EP EP91110239A patent/EP0464509B1/en not_active Expired - Lifetime
- 1991-06-24 HU HU912105A patent/HUT57787A/hu unknown
- 1991-06-24 JP JP03151484A patent/JP3072390B2/ja not_active Expired - Fee Related
- 1991-06-24 FI FI913067A patent/FI913067A/fi not_active Application Discontinuation
- 1991-06-24 AU AU79287/91A patent/AU637508B2/en not_active Ceased
- 1991-06-24 NO NO91912462A patent/NO912462L/no unknown
- 1991-06-24 CA CA002045293A patent/CA2045293A1/en not_active Abandoned
- 1991-06-25 CN CN91104316A patent/CN1057654A/zh active Pending
- 1991-06-25 KR KR1019910010616A patent/KR920000778A/ko not_active Application Discontinuation
-
1993
- 1993-01-19 US US08/003,955 patent/US5376647A/en not_active Expired - Fee Related
-
1994
- 1994-09-09 US US08/303,665 patent/US5512552A/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
NO912462L (no) | 1991-12-27 |
US5512552A (en) | 1996-04-30 |
AU7928791A (en) | 1992-01-02 |
CA2045293A1 (en) | 1991-12-26 |
ATE127123T1 (de) | 1995-09-15 |
FI913067A0 (fi) | 1991-06-24 |
EP0464509A1 (en) | 1992-01-08 |
DE69112511D1 (de) | 1995-10-05 |
DE69112511T2 (de) | 1996-02-08 |
US5376647A (en) | 1994-12-27 |
EP0464509B1 (en) | 1995-08-30 |
HUT57787A (en) | 1991-12-30 |
NO912462D0 (no) | 1991-06-24 |
FI913067A (fi) | 1991-12-26 |
IE912115A1 (en) | 1992-01-01 |
AU637508B2 (en) | 1993-05-27 |
CN1057654A (zh) | 1992-01-08 |
JP3072390B2 (ja) | 2000-07-31 |
JPH05294979A (ja) | 1993-11-09 |
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Legal Events
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WITN | Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid |