KR880002885A - 디포스폰산유도체, 이들의 제조방법 및 이들을 함유하는 제약조성물 - Google Patents
디포스폰산유도체, 이들의 제조방법 및 이들을 함유하는 제약조성물 Download PDFInfo
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- KR880002885A KR880002885A KR1019870008480A KR870008480A KR880002885A KR 880002885 A KR880002885 A KR 880002885A KR 1019870008480 A KR1019870008480 A KR 1019870008480A KR 870008480 A KR870008480 A KR 870008480A KR 880002885 A KR880002885 A KR 880002885A
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- het
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- 239000008194 pharmaceutical composition Substances 0.000 title claims 3
- XQRLCLUYWUNEEH-UHFFFAOYSA-N diphosphonic acid Chemical class OP(=O)OP(O)=O XQRLCLUYWUNEEH-UHFFFAOYSA-N 0.000 title claims 2
- 238000002360 preparation method Methods 0.000 title claims 2
- 150000001875 compounds Chemical class 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 7
- -1 Alkyl diphosphonic acid derivatives Chemical class 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 3
- 125000003277 amino group Chemical group 0.000 claims 3
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- UGUHFDPGDQDVGX-UHFFFAOYSA-N 1,2,3-thiadiazole Chemical group C1=CSN=N1 UGUHFDPGDQDVGX-UHFFFAOYSA-N 0.000 claims 2
- IMSODMZESSGVBE-UHFFFAOYSA-N 2-Oxazoline Chemical compound C1CN=CO1 IMSODMZESSGVBE-UHFFFAOYSA-N 0.000 claims 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 2
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 2
- ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical compound OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 2
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 239000011575 calcium Substances 0.000 claims 2
- 229910052791 calcium Inorganic materials 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 150000005690 diesters Chemical class 0.000 claims 2
- XQRLCLUYWUNEEH-UHFFFAOYSA-L diphosphonate(2-) Chemical compound [O-]P(=O)OP([O-])=O XQRLCLUYWUNEEH-UHFFFAOYSA-L 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- MTNDZQHUAFNZQY-UHFFFAOYSA-N imidazoline Chemical compound C1CN=CN1 MTNDZQHUAFNZQY-UHFFFAOYSA-N 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 229910052698 phosphorus Inorganic materials 0.000 claims 2
- 239000011574 phosphorus Substances 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 150000003852 triazoles Chemical class 0.000 claims 2
- 239000003513 alkali Substances 0.000 claims 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 1
- 239000012050 conventional carrier Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000002560 nitrile group Chemical group 0.000 claims 1
- SBOJXQVPLKSXOG-UHFFFAOYSA-N o-amino-hydroxylamine Chemical group NON SBOJXQVPLKSXOG-UHFFFAOYSA-N 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- ISIJQEHRDSCQIU-UHFFFAOYSA-N tert-butyl 2,7-diazaspiro[4.5]decane-7-carboxylate Chemical compound C1N(C(=O)OC(C)(C)C)CCCC11CNCC1 ISIJQEHRDSCQIU-UHFFFAOYSA-N 0.000 claims 1
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- 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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- 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
- A61P3/00—Drugs for disorders of the metabolism
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- 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
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
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- 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
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- 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 Table
- 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
- 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 Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having three nitrogen atoms as the only ring hetero atoms
- C07F9/6518—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 Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
- C07F9/653—Five-membered rings
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- 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 Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
- C07F9/653—Five-membered rings
- C07F9/65324—Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
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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 Table
- 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
- C07F9/6541—Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
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Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (10)
- 다음 일반식 (Ⅰ)의 알킬 디포스폰산 유도체 및 제약에 수용할 수 있는 이들의 염상기 식에서, Het는 부분적으로 할로겐화 될 수 있고, 알킬, 알콕시, 페닐, 시클로헥실, 시클로헥실메틸, 할로겐 또는 아미노에 의해 임의로 한번 또는 그 이상 치환될 수 있는 2 또는 3개의 헤테로원자를 함유하는 헤테로방향족 5-원고리이고, 여기서 2개의 인접한 알킬치환체들은 함께 고리를 형성할 수 있고, Y는 수소원자 또는 저급알킬이고, X는 수소원자, 히드록실기 또는 저급알킬기에 의해 임의로 치환된 아미노기이고, R는, 수소원자 또는 저급알킬기이고, 단 Het는 피라졸고리가 아니다.
- 제1항에 있어서, Het는 2 또는 3개의 헤테로원자를 함유하고, 이들 중의 적어도 하나는 질소원자인 5원고리임을 특징으로 하는 화합물.
- 제1항 또는 2항에 있어서, Het는 이미다졸, 이미다졸린, 이소옥사졸, 옥사졸, 옥사졸린, 티아졸, 티아졸린, 트리아졸, 옥사디아졸 또는 티아디아졸기임을 특징으로 하는 화합물.
- a) 다음 일반식 (Ⅱ)의 카르복실산과 아인산 또는 인산과 할로겐화인의 혼합물을 반응시키고, 계속하여 바누화시켜 유리 디포스폰산을 얻거나 ; 또는 b) 다음 일반식 (Ⅲ)의 염화 카르복실산을 다음 일반식 (Ⅳ)의 아인산 트리알킬과 반응시켜 다음 일반식 (Ⅴ)의 아실 포스포네이트를 얻고, 계속하여 다음 일반식 (Ⅵ)의 아인산디알킬과 반응시켜 다음 일반식 (Ⅶ)의 디포스포네이트를 얻고, 이 때 얻어진 테트라에스테로를 임의로 비누화시켜 다음 일반식 (Ⅰ)의 유리산 또는 해당하는 디에스테로를 얻거나 ; 또는 일반식 (Ⅰ)에서 X가 알칼기에 의해 임의로 치환된 아미노기일 때, c) 다음 일반식 (Ⅷ)의 카르복실산유도체를 다음 일반식 (Ⅸ)의 인화합물과 반응시키고 계속하여 임의로 비누화시키거나 ; 또는 일반식(Ⅰ)에서 X가 수소원자일 때, d) 일반식 (Ⅹ)의 화합물을 다음 일반식 (XI)의 화합물과 반응시켜 다음 일반식(XⅡ)의 디포스포네이트를 얻고, 이 때 얻어진 테트라에스테를 임의로 비누화시켜 다음 일반식 (Ⅰ)의 산 또는 해당하는 디에스테르를 얻음을 특징으로 하는 다음 일반식 (Ⅰ)의 알킬디포스폰산유도체 및 제약에 수용할 수 있는 이들의 염의 제조방법:상기 식에서, Het는 부분적으로 할로겐화될 수 있고, 알킬, 알콕시, 페닐, 시클로헥실, 시클로헥실메틸, 할로겐 또는 아미노에 의해 임의로 한번 또는 그 이상 치환될 수 있는 2 또는 3개의 헤테로원자를 함유하는 해테로방향족 5-원고리이고, 여기서 2개의 인접한 알킬 치환체들은 함께 고리를 형성할 수 있고, Y는 수소원자 또는 저급알킬이고, X는 수소원자, 히드록실기 또는 저급알킬기에 의해 임의로 치환된 아미노기이고, R은 수소원자 또는 저급알킬기이고, 단 Het는 피라졸고리가 아니다.상기 식에서, Het 및 Y는 상기에 정의한 바와 같다.상기 식에서, Het 및 Y는 상기에 정의한 바와 같다.상기 식에서, R'은 저급알킬기이다.상기 식에서, Het, Y 및 R'은 상기에 정의한 바와 같다.상기 식에서 R'은 상기에 정의한 바와 같다.상기 식에거 Het, Y 및 R'은 상기에 정의한 바와 같다.상기 식에서, Het 및 Y는 상기에 정의한 바와 같고, X는 니트릴, 아미노에테르 또는 N,N-디알킬카르복시아미도기이다.상기 식에서, T는 할로겐원자, 히드록실기 또는 OR'기이고, 여기서 R'은 상기에 정의한 바와 같다.상기 식에서, Het 및 Y는 상기에 정의한 바와 같고, A는 반응성 그룹이다.상기 식에서, R'은 상기에 정의한 바와 같다.상기 식에서, Het, Y 및 R'은 상기에 정의한 바와 같다.
- 제4항에 있어서, Het가 2 또는 3개의 헤테로 원자를 함유하고, 이들 중의 적어도 하나가 질소원자인 5원고리의 화합물인 일반식 (Ⅰ)의 화합물의 제조방법.
- 제4항 또는 5항에 있어서, Het가 이미다졸, 이미다졸린, 이소옥사졸, 옥사졸, 옥사졸린, 티아졸, 티아졸린, 트리아졸, 옥사디아졸 또는 티아디아졸기인 일반식 (Ⅰ)의 화합물의 제조방법.
- 청구범위 4항 내지 6항중의 어느 한항에 따른 방법에 의해 제조된 제1항에 따른 화합물.
- 청구범위 제1항 내지 3항 및 7항중의 어느 한 항에 따른 적어도 하나의 화합물 및 제약에 수용할 수 있는 통상적인 담체 및/또는 보조물질들을 함유하는 제약조성물.
- 칼슘대사 장해의 치료용 제약조성물의 제조를 위한 청구범위 제1항 내지 3항 및 7항 중의 어느 한 항에 따른 화합물의 용도.
- 칼슘대사 장해의 치료를 위한 청구범위 제1항 내지 3항 및 7항 중의 어느 한 항에 따른 화합물의 용도.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE3626058,4 | 1986-08-01 | ||
| DE19863626058 DE3626058A1 (de) | 1986-08-01 | 1986-08-01 | Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel |
| DE3626058.4 | 1986-08-01 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR880002885A true KR880002885A (ko) | 1988-05-12 |
| KR900004043B1 KR900004043B1 (ko) | 1990-06-09 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019870008480A KR900004043B1 (ko) | 1986-08-01 | 1987-08-01 | 디포스폰산유도체, 이들의 제조방법 및 이들을 함유하는 제약조성물 |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US4777163A (ko) |
| EP (1) | EP0258618B1 (ko) |
| JP (1) | JPH0725780B2 (ko) |
| KR (1) | KR900004043B1 (ko) |
| AT (1) | ATE75748T1 (ko) |
| AU (1) | AU605778B2 (ko) |
| CA (1) | CA1338895C (ko) |
| CS (1) | CS266345B2 (ko) |
| DD (1) | DD264442A5 (ko) |
| DE (3) | DE3626058A1 (ko) |
| DK (1) | DK168820B1 (ko) |
| ES (1) | ES2032782T3 (ko) |
| FI (1) | FI87223C (ko) |
| GR (1) | GR3004499T3 (ko) |
| HK (1) | HK47096A (ko) |
| HU (1) | HU198078B (ko) |
| IE (1) | IE60233B1 (ko) |
| IL (1) | IL83332A (ko) |
| LU (1) | LU90836I2 (ko) |
| MX (1) | MX7510A (ko) |
| NL (1) | NL300059I2 (ko) |
| PT (1) | PT85457B (ko) |
| ZA (1) | ZA875489B (ko) |
Families Citing this family (58)
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|---|---|---|---|---|
| IL77243A (en) * | 1984-12-21 | 1996-11-14 | Procter & Gamble | Pharmaceutical compositions containing geminal diphosphonic acid compounds and certain such novel compounds |
| ES2038692T4 (es) * | 1986-11-21 | 2012-02-10 | Novartis Ag | Procedimiento para la obtencion de acidos alcanodifosfonicos substituidos. |
| DE3640938A1 (de) * | 1986-11-29 | 1988-06-01 | Boehringer Mannheim Gmbh | Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindung enthaltende arzneimittel |
| HU199151B (en) * | 1987-03-10 | 1990-01-29 | Yamanouchi Pharma Co Ltd | Process for producing bis-phosphonic acid derivatives |
| EP0317505A1 (de) * | 1987-11-13 | 1989-05-24 | Ciba-Geigy Ag | Neue Azacycloalkylalkandiphosphonsäuren |
| US5190930A (en) * | 1987-12-11 | 1993-03-02 | Ciba-Geigy Corporation | Araliphatylaminoalkanediphosphonic acids |
| US5110807A (en) * | 1988-12-01 | 1992-05-05 | Ciba-Geigy Corporation | Araliphatylaminoalkanediphosphonic acids |
| DE3822650A1 (de) * | 1988-07-05 | 1990-02-01 | Boehringer Mannheim Gmbh | Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel |
| US4990503A (en) * | 1988-08-12 | 1991-02-05 | Yamanouchi Pharmaceutical Co., Ltd. | Heterocyclic bisphosphonic acid derivatives |
| US4932996A (en) * | 1988-10-18 | 1990-06-12 | Fmc Corporation | Phosphorylaminophenyltetrazolinone herbicides |
| US4954159A (en) * | 1988-10-18 | 1990-09-04 | Fmc Corporation | Phosphorylaminophenyltetrahydrophthalimide herbicides |
| US4902338A (en) * | 1988-11-04 | 1990-02-20 | Fmc Corporation | Phosphorylaminophenylhydantoin herbicides |
| US4898606A (en) * | 1988-10-14 | 1990-02-06 | Fmc Corporation | Phosphorylaminophenyltriazolinone herbicides |
| US5231091A (en) * | 1988-12-19 | 1993-07-27 | American Cyanamid Company | Bis-arylphosphate ester antagonists of platelet activating factor |
| US4983592A (en) * | 1988-12-19 | 1991-01-08 | American Cyanamid Co. | Bis-arylphosphate ester antagonists of platelet activating factor |
| US5147864A (en) * | 1988-12-19 | 1992-09-15 | American Cyanamid Company | Bis-arylphosphate ester antagonists of platelet activating factor |
| DE3917153A1 (de) * | 1989-05-26 | 1990-11-29 | Boehringer Mannheim Gmbh | Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel |
| US5139786A (en) * | 1989-07-07 | 1992-08-18 | Ciba-Geigy Corporation | Topical formulations |
| MX21452A (es) * | 1989-07-07 | 1994-01-31 | Ciba Geigy Ag | Preparaciones farmaceuticas que se administran en forma topica. |
| US5204334A (en) * | 1990-10-18 | 1993-04-20 | Ciba-Geigy Corporation | Benzoheterocyclylalkylaminoalkanediphosphonic acids, compositions thereof, and use thereof in the treatment of calcium metabolism disorders |
| US5202111A (en) * | 1991-05-09 | 1993-04-13 | Chesebrough-Pond's Usa Co., Division Of Conopco, Inc. | Phosphorylated polyhydroxy compounds for tartar control |
| EP0521622B1 (en) * | 1991-07-03 | 1997-08-13 | PHARMACIA & UPJOHN COMPANY | Pyrazolopyrimidine and pyrimidinyl bisphosphonic esters as anti-inflammatories |
| JPH08502287A (ja) * | 1992-10-09 | 1996-03-12 | ジ・アップジョン・カンパニー | 抗炎症剤としてのピリミジンビスホスホン酸エステルおよび（アルコキシメチルホスフィニル）アルキルホスホン酸 |
| US5591730A (en) * | 1993-10-12 | 1997-01-07 | The Regents Of The University Of California | Inhibition of urinary calculi growth |
| US5854227A (en) * | 1994-03-04 | 1998-12-29 | Hartmann; John F. | Therapeutic derivatives of diphosphonates |
| US7205404B1 (en) | 1999-03-05 | 2007-04-17 | Metabasis Therapeutics, Inc. | Phosphorus-containing prodrugs |
| US6677320B2 (en) | 2000-01-20 | 2004-01-13 | Hoffmann-La Roches Inc. | Parenteral bisphosphonate composition with improved local tolerance |
| US6410520B2 (en) | 2000-02-01 | 2002-06-25 | The Procter & Gamble Company | Selective crystallization of 3-pyridyl-1-hydroxyethylidene-1, 1-bisphosphonic acid sodium as the hemipentahydrate or monohydrate |
| US6562974B2 (en) | 2000-02-01 | 2003-05-13 | The Procter & Gamble Company | Process for making geminal bisphosphonates |
| EP1284754B1 (en) | 2000-05-05 | 2006-01-04 | F. Hoffmann-La Roche Ag | Gel-like pharmaceutical composition for subcutaneous administration comprising bisphosphonic acids or their salts |
| MXPA04006027A (es) * | 2001-12-21 | 2004-09-27 | Procter & Gamble | Metodo para el tratamiento de trastornos de los huesos. |
| KR20140021045A (ko) * | 2002-05-10 | 2014-02-19 | 에프. 호프만-라 로슈 아게 | 골다공증 치료 및 예방용 비스포스폰산 |
| US20060069067A1 (en) * | 2002-07-30 | 2006-03-30 | Bhatnagar Ajay S | Combination of an aromatase inhibitor with a bisphosphonate |
| JP4427453B2 (ja) * | 2002-12-20 | 2010-03-10 | エフ．ホフマン−ラ ロシュ アーゲー | 高用量イバンドロネート製剤 |
| WO2004075860A2 (en) * | 2003-02-27 | 2004-09-10 | Teva Pharmaceutical Industries Ltd. | Process for purification of zoledronic acid |
| WO2005005447A2 (en) * | 2003-07-03 | 2005-01-20 | Teva Pharmaceutical Industries Ltd. | Zoledronic acid crystal forms, zoledronate sodium salt crystal forms, amorphous zoledronate sodium salt, and processes for their preparation |
| US20050049693A1 (en) * | 2003-08-25 | 2005-03-03 | Medtronic Vascular Inc. | Medical devices and compositions for delivering biophosphonates to anatomical sites at risk for vascular disease |
| US20050119230A1 (en) * | 2003-09-18 | 2005-06-02 | Alexandra Glausch | Pharmaceutical products comprising bisphosphonated |
| US7214671B2 (en) * | 2004-02-19 | 2007-05-08 | Wisconsin Alumni Research Foundation | Use of 2-methylene-19-nor-20(S)-1α,25-dihydroxyvitamin D3 for the prophylaxis of bone diseases |
| US8012949B2 (en) * | 2004-10-08 | 2011-09-06 | The Board Of Trustees Of The University Of Illinois | Bisphosphonate compounds and methods with enhanced potency for multiple targets including FPPS, GGPPS, and DPPS |
| WO2006039721A2 (en) * | 2004-10-08 | 2006-04-13 | The Board Of Trustees Of The University Of Illinois | Bisphosphonate compounds and methods for bone resorption diseases, cancer, bone pain, immune disorders, and infectious diseases |
| US7687482B2 (en) * | 2006-03-17 | 2010-03-30 | The Board Of Trustees Of The University Of Illinois | Bisphosphonate compounds and methods |
| AR054673A1 (es) | 2005-07-28 | 2007-07-11 | Gador Sa | Una forma cristalina del acido zoledronico, un proceso para su obtencion y la composicion farmaceutica que la comprende |
| EP2561877A1 (en) | 2006-12-20 | 2013-02-27 | Mylan Pharmaceuticals ULC | A Composition containing a Bisphosphonic Acid in combination with Vitamin D |
| CA2671728C (en) * | 2006-12-20 | 2015-05-26 | Genpharm Ulc | Pharmaceutical composition comprising a hot-melt granulated lubricant |
| US20090023683A1 (en) * | 2007-07-16 | 2009-01-22 | Chandrasekhar Kocherlakota | Complexes comprising zoledronic acid and cyclodextrins |
| US20110015158A1 (en) | 2007-12-11 | 2011-01-20 | Viamet Pharmaceuticals, Inc. | Metalloenzyme inhibitors using metal binding moieties in combination with targeting moieties |
| MX2010010943A (es) * | 2008-04-04 | 2012-09-28 | Novartis Ag | Composicion farmaceutica con bisfosfonato. |
| AU2009334889A1 (en) * | 2008-12-23 | 2011-06-30 | Novartis Ag | Phenylalkyl-imidazole-bisphosphonate compounds |
| FR2954320B1 (fr) | 2009-12-17 | 2012-06-15 | Cll Pharma | Composition pharmaceutique orale suprabiodisponible contenant un acide biphosphonique ou un de ses sels |
| US8882740B2 (en) * | 2009-12-23 | 2014-11-11 | Stryker Trauma Gmbh | Method of delivering a biphosphonate and/or strontium ranelate below the surface of a bone |
| US8748097B1 (en) | 2011-12-02 | 2014-06-10 | President And Fellows Of Harvard College | Identification of agents for treating calcium disorders and uses thereof |
| CN106061984A (zh) | 2014-02-13 | 2016-10-26 | 配体药物公司 | 前药化合物及其用途 |
| PL407922A1 (pl) | 2014-04-16 | 2015-10-26 | Wrocławskie Centrum Badań Eit + Spółka Z Ograniczoną Odpowiedzialnością | Nowe bisfosfoniany i ich zastosowanie |
| EP3164136A4 (en) | 2014-07-02 | 2018-04-04 | Ligand Pharmaceuticals, Inc. | Prodrug compounds and uses therof |
| KR20200066690A (ko) | 2017-10-16 | 2020-06-10 | 칭화대학교 | 메발로네이트 경로 억제제 및 이의 약제학적 조성물 |
| US11613644B2 (en) * | 2017-11-20 | 2023-03-28 | Basf Se | Aqueous acrylic polymer latexes and their use as binders |
| CA3087932A1 (en) | 2018-01-09 | 2019-07-18 | Ligand Pharmaceuticals, Inc. | Acetal compounds and therapeutic uses thereof |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3203307A1 (de) * | 1982-01-27 | 1983-07-28 | Schering Ag, 1000 Berlin Und 4619 Bergkamen | Phosphonate, und diese enthaltende pharmazeutische verbindungen |
| EP0084822B1 (de) * | 1982-01-27 | 1986-01-08 | Schering Aktiengesellschaft | Diphosphonsäure-Derivate und diese enthaltende pharmazeutische Präparate |
| DE3203308A1 (de) * | 1982-01-27 | 1983-07-28 | Schering Ag, 1000 Berlin Und 4619 Bergkamen | Diphosphonsaeure-derivate und diese enthaltende pharmazeutische praeparate |
| DE3428524A1 (de) * | 1984-08-02 | 1986-02-13 | Boehringer Mannheim Gmbh, 6800 Mannheim | Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel |
| ES2038692T4 (es) * | 1986-11-21 | 2012-02-10 | Novartis Ag | Procedimiento para la obtencion de acidos alcanodifosfonicos substituidos. |
-
1986
- 1986-08-01 DE DE19863626058 patent/DE3626058A1/de not_active Withdrawn
-
1987
- 1987-07-24 US US07/077,228 patent/US4777163A/en not_active Expired - Lifetime
- 1987-07-25 AT AT87110830T patent/ATE75748T1/de active
- 1987-07-25 DE DE2001199050 patent/DE10199050I1/de active Pending
- 1987-07-25 EP EP87110830A patent/EP0258618B1/de not_active Expired - Lifetime
- 1987-07-25 ES ES198787110830T patent/ES2032782T3/es not_active Expired - Lifetime
- 1987-07-25 DE DE8787110830T patent/DE3778800D1/de not_active Expired - Lifetime
- 1987-07-26 IL IL83332A patent/IL83332A/xx not_active IP Right Cessation
- 1987-07-27 ZA ZA875489A patent/ZA875489B/xx unknown
- 1987-07-27 MX MX751087A patent/MX7510A/es unknown
- 1987-07-29 AU AU76256/87A patent/AU605778B2/en not_active Expired
- 1987-07-29 CA CA000543290A patent/CA1338895C/en not_active Expired - Lifetime
- 1987-07-30 JP JP62189069A patent/JPH0725780B2/ja not_active Expired - Lifetime
- 1987-07-30 PT PT85457A patent/PT85457B/pt unknown
- 1987-07-30 DD DD87305527A patent/DD264442A5/de not_active IP Right Cessation
- 1987-07-30 CS CS875702A patent/CS266345B2/cs not_active IP Right Cessation
- 1987-07-30 DK DK398187A patent/DK168820B1/da not_active IP Right Cessation
- 1987-07-31 FI FI873339A patent/FI87223C/fi not_active IP Right Cessation
- 1987-07-31 HU HU873542A patent/HU198078B/hu active Protection Beyond IP Right Term
- 1987-07-31 IE IE208387A patent/IE60233B1/en not_active IP Right Cessation
- 1987-08-01 KR KR1019870008480A patent/KR900004043B1/ko not_active IP Right Cessation
-
1992
- 1992-05-07 GR GR900400209T patent/GR3004499T3/el unknown
-
1996
- 1996-03-14 HK HK47096A patent/HK47096A/xx not_active IP Right Cessation
-
2001
- 2001-09-18 NL NL300059C patent/NL300059I2/nl unknown
- 2001-09-19 LU LU90836C patent/LU90836I2/fr unknown
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