LV11472B - Crystalline 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid monosodium trihydrate, process therefor and compositions and use thereof - Google Patents

Crystalline 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid monosodium trihydrate, process therefor and compositions and use thereof Download PDF

Info

Publication number: LV11472B
Authority: LV; Latvia
Prior art keywords: amino; acid; hydroxybutylidene; crystalline; bisphosphonic acid
Prior art date: 1989-06-09

Application number

LVP-96-28A

Other languages

English (en)

Latvian (lv)

Other versions

LV11472A (lv

Inventor

Gerald R Kieczykowski

David G Melillo

Ronald B Jobson

Gerald S Brenner

Original Assignee

Merck & Co Inc

Priority date (The priority date 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 date listed.)

1989-06-09

Filing date

1996-02-02

Publication date

1996-12-20

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=23431886&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=LV11472(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

1996-02-02 Application filed by Merck & Co Inc filed Critical Merck & Co Inc

1996-08-20 Publication of LV11472A publication Critical patent/LV11472A/xx

1996-12-20 Publication of LV11472B publication Critical patent/LV11472B/en

Links

238000000034 method Methods 0.000 title claims abstract description 21
239000000203 mixture Substances 0.000 title claims abstract description 6
239000002253 acid Substances 0.000 title abstract description 11
PAYGMRRPBHYIMA-UHFFFAOYSA-N sodium;trihydrate Chemical compound O.O.O.[Na] PAYGMRRPBHYIMA-UHFFFAOYSA-N 0.000 title description 4
BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims abstract description 18
AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims abstract description 13
229960003692 gamma aminobutyric acid Drugs 0.000 claims abstract description 8
238000002360 preparation method Methods 0.000 claims abstract description 7
229940098779 methanesulfonic acid Drugs 0.000 claims abstract description 6
HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 24
150000001875 compounds Chemical class 0.000 claims description 9
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 8
239000008194 pharmaceutical composition Substances 0.000 claims description 5
229910001868 water Inorganic materials 0.000 claims description 5
238000007605 air drying Methods 0.000 claims description 3
238000001914 filtration Methods 0.000 claims description 3
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 3
KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 claims description 2
238000001816 cooling Methods 0.000 claims description 2
NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 3
235000011007 phosphoric acid Nutrition 0.000 claims 2
229910000147 aluminium phosphate Inorganic materials 0.000 claims 1
239000001177 diphosphate Substances 0.000 claims 1
239000000843 powder Substances 0.000 claims 1
239000002904 solvent Substances 0.000 claims 1
238000005406 washing Methods 0.000 claims 1
FAIAAWCVCHQXDN-UHFFFAOYSA-N phosphorus trichloride Chemical compound ClP(Cl)Cl FAIAAWCVCHQXDN-UHFFFAOYSA-N 0.000 abstract description 6
150000003839 salts Chemical class 0.000 abstract description 4
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 abstract description 4
238000006243 chemical reaction Methods 0.000 description 15
239000000243 solution Substances 0.000 description 10
CAKRAHQRJGUPIG-UHFFFAOYSA-M sodium;[4-azaniumyl-1-hydroxy-1-[hydroxy(oxido)phosphoryl]butyl]-hydroxyphosphinate Chemical compound [Na+].NCCCC(O)(P(O)(O)=O)P(O)([O-])=O CAKRAHQRJGUPIG-UHFFFAOYSA-M 0.000 description 7
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
239000011541 reaction mixture Substances 0.000 description 4
238000004458 analytical method Methods 0.000 description 3
230000007062 hydrolysis Effects 0.000 description 3
238000006460 hydrolysis reaction Methods 0.000 description 3
238000004519 manufacturing process Methods 0.000 description 3
239000000725 suspension Substances 0.000 description 3
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
150000007513 acids Chemical class 0.000 description 2
229940124277 aminobutyric acid Drugs 0.000 description 2
238000003556 assay Methods 0.000 description 2
239000007795 chemical reaction product Substances 0.000 description 2
239000003085 diluting agent Substances 0.000 description 2
238000010438 heat treatment Methods 0.000 description 2
229910052757 nitrogen Inorganic materials 0.000 description 2
239000000376 reactant Substances 0.000 description 2
238000010992 reflux Methods 0.000 description 2
239000011734 sodium Substances 0.000 description 2
238000007711 solidification Methods 0.000 description 2
230000008023 solidification Effects 0.000 description 2
208000006386 Bone Resorption Diseases 0.000 description 1
229910014033 C-OH Inorganic materials 0.000 description 1
KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical compound NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 description 1
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
229910014570 C—OH Inorganic materials 0.000 description 1
206010020584 Hypercalcaemia of malignancy Diseases 0.000 description 1
DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
208000010191 Osteitis Deformans Diseases 0.000 description 1
208000001132 Osteoporosis Diseases 0.000 description 1
208000027868 Paget disease Diseases 0.000 description 1
OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 description 1
238000009835 boiling Methods 0.000 description 1
230000024279 bone resorption Effects 0.000 description 1
239000012267 brine Substances 0.000 description 1
229910052799 carbon Inorganic materials 0.000 description 1
239000003518 caustics Substances 0.000 description 1
201000010099 disease Diseases 0.000 description 1
230000006806 disease prevention Effects 0.000 description 1
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
238000001035 drying Methods 0.000 description 1
239000012530 fluid Substances 0.000 description 1
238000004128 high performance liquid chromatography Methods 0.000 description 1
208000008750 humoral hypercalcemia of malignancy Diseases 0.000 description 1
BHEPBYXIRTUNPN-UHFFFAOYSA-N hydridophosphorus(.) (triplet) Chemical compound [PH] BHEPBYXIRTUNPN-UHFFFAOYSA-N 0.000 description 1
229910052739 hydrogen Inorganic materials 0.000 description 1
239000001257 hydrogen Substances 0.000 description 1
125000004435 hydrogen atom Chemical class [H]* 0.000 description 1
230000003301 hydrolyzing effect Effects 0.000 description 1
208000027202 mammary Paget disease Diseases 0.000 description 1
238000002844 melting Methods 0.000 description 1
230000008018 melting Effects 0.000 description 1
238000002156 mixing Methods 0.000 description 1
238000006386 neutralization reaction Methods 0.000 description 1
238000005580 one pot reaction Methods 0.000 description 1
238000010979 pH adjustment Methods 0.000 description 1
239000002245 particle Substances 0.000 description 1
238000005954 phosphonylation reaction Methods 0.000 description 1
229910052698 phosphorus Inorganic materials 0.000 description 1
239000011574 phosphorus Substances 0.000 description 1
238000003918 potentiometric titration Methods 0.000 description 1
239000000047 product Substances 0.000 description 1
238000000746 purification Methods 0.000 description 1
238000010791 quenching Methods 0.000 description 1
230000000171 quenching effect Effects 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
238000004448 titration Methods 0.000 description 1

Classifications

- 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
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- 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
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or 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)
- 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

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
General Health & Medical Sciences (AREA)
Biochemistry (AREA)
Molecular Biology (AREA)
Chemical Kinetics & Catalysis (AREA)
Pharmacology & Pharmacy (AREA)
Diabetes (AREA)
Hematology (AREA)
Obesity (AREA)
Engineering & Computer Science (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Bioinformatics & Cheminformatics (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Seasonings (AREA)
Preparation Of Compounds By Using Micro-Organisms (AREA)

LVP-96-28A 1989-06-09 1996-02-02 Crystalline 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid monosodium trihydrate, process therefor and compositions and use thereof LV11472B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US07/363,820 US4922007A (en)	1989-06-09	1989-06-09	Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or salts thereof

Publications (2)

Publication Number	Publication Date
LV11472A LV11472A (lv)	1996-08-20
LV11472B true LV11472B (en)	1996-12-20

Family

ID=23431886

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
LVP-96-28A LV11472B (en)	1989-06-09	1996-02-02	Crystalline 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid monosodium trihydrate, process therefor and compositions and use thereof

Country Status (23)

Country	Link
US (1)	US4922007A (fr)
EP (1)	EP0402152B1 (fr)
JP (2)	JPH0662651B2 (fr)
KR (1)	KR0137455B1 (fr)
AT (1)	ATE129713T1 (fr)
AU (1)	AU625704C (fr)
CA (1)	CA2018477C (fr)
CH (1)	CH0402152H1 (fr)
CY (1)	CY1894A (fr)
DE (1)	DE69023280T2 (fr)
DK (1)	DK0402152T3 (fr)
ES (1)	ES2080116T3 (fr)
FI (1)	FI93219C (fr)
GR (1)	GR3018379T3 (fr)
HK (1)	HK69596A (fr)
HU (1)	HU211908A9 (fr)
IE (1)	IE69564B1 (fr)
IL (1)	IL94612A (fr)
LV (1)	LV11472B (fr)
NO (2)	NO177997C (fr)
NZ (1)	NZ233972A (fr)
PT (1)	PT94306B (fr)
ZA (1)	ZA904446B (fr)

Families Citing this family (118)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5356887A (en) *	1990-01-31	1994-10-18	Merck & Co., Inc.	Pharmaceutical compositions containing insoluble calcium salts of amino-hydroxybutylidene bisphoshonic acids
US5019651A (en) *	1990-06-20	1991-05-28	Merck & Co., Inc.	Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid (ABP) or salts thereof
US5039819A (en) *	1990-09-18	1991-08-13	Merck & Co., Inc.	Diphosphonate intermediate for preparing an antihypercalcemic agent
US5159108A (en) *	1990-09-18	1992-10-27	Merck & Co., Inc.	Process for preparing an antihypercalcemic agent
NZ253541A (en) *	1992-05-29	1997-01-29	Procter & Gamble Pharma	Cyclic quaternary-n-containing phosphonate derivatives and medicaments
US5753634A (en) *	1992-05-29	1998-05-19	The Procter & Gamble Company	Quaternary nitrogen containing phosphonate compounds, pharmaceutical compostions, and methods for treating abnormal calcium and phosphate metabolism
NZ253526A (en) *	1992-05-29	1997-01-29	Procter & Gamble Pharma	Thio-substituted heterocyclic phosphonate derivatives and medicaments
US5391743A (en) *	1992-05-29	1995-02-21	Procter & Gamble Pharmaceuticals, Inc.	Quaternary nitrogen-containing phosphonate compounds, pharmaceutical compositions, and methods of treating abnormal calcium and phosphate metabolism and methods of treating and preventing dental calculus and plaque
CA2188066C (fr) *	1992-05-29	2000-12-05	Susan Mary Kaas	Derives de substitution thio de phosphonates
US5763611A (en) *	1992-05-29	1998-06-09	The Procter & Gamble Company	Thio-substituted cyclic phosphonate compounds, pharmaceutical compositions, and methods for treating abnormal calcium and phosphate metabolism
FR2694558B1 (fr) *	1992-08-05	1994-10-28	Sanofi Elf	Monohydrate du sel disodique de l'acide 4-chlorophénylthiométhylène bisphosphonique, sa préparation, les compositions pharmaceutiques en contenant.
US6406714B1 (en)	1992-12-02	2002-06-18	Merck & Co., Inc.	Dry mix formulation for bisphosphonic acids
US6399592B1 (en)	1992-12-23	2002-06-04	Merck & Co., Inc.	Bishphosphonate/estrogen synergistic therapy for treating and preventing bone loss
FR2703590B1 (fr) *	1993-04-05	1995-06-30	Sanofi Elf	Utilisation de derives d'acide bisphosphonique pour la preparation de medicaments destines a favoriser la reparation osseuse .
TW257765B (fr) *	1993-08-25	1995-09-21	Merck & Co Inc
US5510517A (en) *	1993-08-25	1996-04-23	Merck & Co., Inc.	Process for producing N-amino-1-hydroxy-alkylidene-1,1-bisphosphonic acids
US5854227A (en) *	1994-03-04	1998-12-29	Hartmann; John F.	Therapeutic derivatives of diphosphonates
US20010007863A1 (en) *	1998-06-18	2001-07-12	Merck & Co., Inc.	Wet granulation formulation for bisphosphonic acids
US5462932A (en) *	1994-05-17	1995-10-31	Merck & Co., Inc.	Oral liquid alendronate formulations
US5449819A (en) *	1994-06-06	1995-09-12	Merck & Co., Inc.	Process for removing waste pox, alendronate and its by products
US5589691A (en) *	1994-06-06	1996-12-31	Merck & Co., Inc.	Process for recovery and recycle of methanesulfonic acid and phosphorous acid
US5780455A (en) *	1994-08-24	1998-07-14	Merck & Co., Inc.	Intravenous alendronate formulations
KR19980702210A (ko) *	1995-02-17	1998-07-15	폴락 돈나 엘	비척추골 골절의 위험률을 감소시키는 방법
CA2219354A1 (fr) *	1995-05-12	1996-11-14	Merck & Co., Inc.	Prevention des pertes de dnets par l'administration d'alendronate ou de ses sels
JPH11511041A (ja)	1995-06-06	1999-09-28	メルクエンドカンパニーインコーポレーテッド	整形外科的埋め込み装置の無菌性動揺を防止するビスホスホネートセメント組成物
WO1996039149A1 (fr) *	1995-06-06	1996-12-12	Merck & Co., Inc.	Formulations de sel de monosodium d'alendronate anhydre
CA2221844A1 (fr) *	1995-06-06	1996-12-12	Merck & Co., Inc.	Preparations d'alendronate disodique
IL129127A0 (en) *	1996-10-04	2000-02-17	Merck & Co Inc	Liquid alendronate formulations
JP2824453B2 (ja) *	1996-10-15	1998-11-11	株式会社ワカ製作所	コネクター
CA2197267C (fr) *	1997-02-11	2000-02-08	Yong Tao	Procede pour la preparation de l'acide 4-amino-1-hydroxybutylidene-1,1-bisphosphonique ou de ses sels
IL122009A0 (en) *	1997-10-21	1998-03-10	Unipharm Ltd	Salt of a bisphosphonic acid derivative
WO1999067809A1 (fr)	1998-06-24	1999-12-29	Merck & Co., Inc.	Compositions et procedes inhibant la resorption osseuse
US20030078211A1 (en) *	1998-06-24	2003-04-24	Merck & Co., Inc.	Compositions and methods for inhibiting bone resorption
US6008207A (en) *	1998-08-13	1999-12-28	Merck & Co., Inc.	Anhydrous alendronate monosodium salt formulations
EP1702924A3 (fr) *	1998-08-27	2007-07-18	Teva Pharmaceutical Industries Ltd	Formes de type hydrate du sel de sodium de l'alendronate, procédés de préparation et compositions pharmaceutiques
IL141423A (en)	1998-08-27	2005-09-25	Teva Pharma	Hydrate forms of alendronate sodium, processes for manufacture thereof, and pharmaceutical compositions thereof
US6331533B1 (en)	1998-11-16	2001-12-18	Merck & Co., Inc.	Method for inhibiting dental resorptive lesions
US6794536B1 (en)	1998-12-10	2004-09-21	Aesqen, Inc.	Method for preparation of disodium pamidronate
US6160165A (en)	1998-12-10	2000-12-12	Aesgen, Inc.	Method for preparation of disodium pamidronate
US6963008B2 (en) *	1999-07-19	2005-11-08	Teva Pharmaceutical Industries Ltd.	Hydrate forms of alendronate sodium, processes for manufacture thereof, and pharmaceutical compositions thereof
ES2153794B1 (es) *	1999-08-06	2001-10-16	Medichem Sa	Procedimiento para la obtencion del acido 4-amino-1-hidroxibutiliden-1,1-bisfosfonico y de su sal monosodica trihidratada.
AR021347A1 (es)	1999-10-20	2002-07-17	Cipla Ltd	Una composicion farmaceutica que contiene acido(s) bisfosfoncio o sal(es) del mismo y un proceso de preparacion de la misma
WO2001030788A1 (fr) *	1999-10-26	2001-05-03	A/S Gea Farmaceutisk Fabrik	Nouveaux sels d'acide 4- amino-1-hydroxy-butylidene-1,1-bisphosphonique, leur preparation et utilisation
US6476006B2 (en)	2000-06-23	2002-11-05	Teva Pharmaceutical Industries, Ltd.	Composition and dosage form for delayed gastric release of alendronate and/or other bis-phosphonates
US6558702B2 (en)	2001-04-13	2003-05-06	Alkermes Controlled Therapeutics, Inc.	Method of modifying the release profile of sustained release compositions
US20060269602A1 (en) *	2001-04-13	2006-11-30	Dasch James R	Method of modifying the release profile of sustained release compositions
CA2372450A1 (fr) *	2001-05-10	2001-09-19	Pharmaceutical Partners Of Canada Inc.	Preparation injectable liquide de pamidronate disodique
TR200101250A2 (tr) *	2001-05-10	2003-04-21	E�S Eczaciba�I �Zg�N K�Myasal �R�Nler Sanay� A.�.	4-amino-1-hidroksibutiliden-1,1-bifosfonik asit veya tuzlarının hazırlanmasına ilişkin proses
GB2383042A (en) *	2001-10-18	2003-06-18	Cipla Ltd	Amorphous alendronate sodium
SK2532004A3 (en) *	2001-12-21	2004-11-03	Procter & Gamble	Method for the treatment of bone disorders
US20050070504A1 (en) *	2001-12-21	2005-03-31	The Procter & Gamble Co.	Risedronate compositions and their methods of use
JP4502641B2 (ja) *	2002-01-24	2010-07-14	ティルタンファーマリミテッド	抗癌組み合わせおよびその使用方法
ITMI20020146A1 (it) *	2002-01-29	2003-07-29	Lyogen Ltd	Alendronato monosodico amorfo e processo per la sua preparazione
ITMI20020908A1 (it) *	2002-04-29	2003-10-29	Chemi Spa	Processo di preparazione di sodio alendronato
KR20060058151A (ko) *	2002-05-10	2006-05-29	에프. 호프만-라 로슈 아게	골다공증 치료 및 예방용 비스포스폰산
AU2003233569A1 (en) *	2002-05-17	2003-12-02	Teva Pharmaceutical Industries Ltd.	Use of certain diluents for making bisphosphonic acids
WO2003103664A1 (fr) *	2002-06-06	2003-12-18	Merck Frosst Canada & Co.	Derives d'imidazolidine-2-one disubstitues en 1,5 utiles en tant qu'agonistes du recepteur ep4 dans le traitement de troubles oculaires et de maladies osseuses
JP4485117B2 (ja) *	2002-06-27	2010-06-16	日東電工株式会社	保護剥離用フィルム
AU2003258433A1 (en) *	2002-08-28	2004-03-19	Merck Frosst Canada Ltd	Oxazolidin-2-one and thiazolidin-2-one derivatives for use as ep4 receptor agonists in the treatment of glaucoma
US20040138180A1 (en) *	2002-10-03	2004-07-15	Barr Laboratories, Inc.	Bisphosphonate composition and process for the preparation thereof
ES2291749T5 (es) *	2002-12-20	2011-07-21	F. Hoffmann-La Roche Ag	Formulación de altas dosis de ibandronato.
US20040206932A1 (en) *	2002-12-30	2004-10-21	Abuelyaman Ahmed S.	Compositions including polymerizable bisphosphonic acids and methods
HUP0300227A2 (hu) *	2003-01-28	2004-09-28	Richter Gedeon Vegyészeti Gyár Rt.	Eljárás nagy tisztaságú 2-szubsztituált -1-(hidroxi-etilidén)-1,1-biszfoszfonsavak és sóik előállítására
AU2004266623B8 (en) *	2003-08-12	2011-10-27	3M Deutschland Gmbh	Self-etching dental compositions and methods
JP4642762B2 (ja)	2003-08-21	2011-03-02	サン・ファーマシューティカル・インダストリーズ・リミテッド	ビスホスホン酸化合物の製造方法
AU2004266740B2 (en)	2003-08-21	2010-08-26	Merck Frosst Canada Ltd	Cathepsin cysteine protease inhibitors
CA2539359A1 (fr) *	2003-09-19	2005-03-31	Pfizer Products Inc.	Compositions pharmaceutiques et methodes de traitement consistant en des associations d'un derive de la 2-alkylidene-19-nor-vitamine d et d'un bisphosphonate
US20050113343A1 (en) *	2003-10-14	2005-05-26	Pliva - Research And Development Ltd.	Solid-state form of alendronate sodium and preparation thereof
US20050261250A1 (en) *	2004-05-19	2005-11-24	Merck & Co., Inc.,	Compositions and methods for inhibiting bone resorption
DK2283825T3 (da)	2004-05-24	2022-06-27	Theramex Hq Uk Ltd	Enterisk fast oral doseringsform af en bisfosfonat indeholdende et chelateringsmiddel
UA87854C2 (en)	2004-06-07	2009-08-25	Мерк Энд Ко., Инк.	N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
AU2005269869B2 (en) *	2004-07-08	2011-12-01	3M Innovative Properties Company	Dental methods, compositions, and kits including acid-sensitive dyes
CA2575976A1 (fr) *	2004-08-11	2006-02-23	3M Innovative Properties Company	Compositions auto-adhesives comprenant une pluralite de composes acides
US7361761B2 (en) *	2004-09-28	2008-04-22	Orchid Chemicals & Pharmaceuticals Ltd.	Process for the preparation of bisphosphonic acid
US7214818B2 (en)	2004-10-29	2007-05-08	Hoffmann-La Roche Inc.	Method for synthesizing bisphosphonate
CN1304401C (zh) *	2004-12-28	2007-03-14	浙江工业大学	一种阿伦膦酸的制备方法
AU2006302797B2 (en)	2005-03-02	2012-02-02	Merck Canada Inc.	Composition for inhibition of cathepsin K
CN101198316A (zh) *	2005-03-17	2008-06-11	伊兰制药国际有限公司	纳米微粒双膦酸盐组合物
EP1891081B1 (fr) *	2005-06-13	2014-08-20	Jubilant Organosys Limited	Procédé de production d acides bisphosphoniques et de formes de ceux-ci
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
US8003820B2 (en) *	2005-10-20	2011-08-23	Dr. Reddy's Laboratories Limited	Process for preparing bisphosphonic acids
EP2431427B1 (fr)	2005-10-31	2014-12-31	Cabot Corporation	Colorants modifiés et compositions d'encre à jet d'encre comportant les colorants modifiés
PT1803727E (pt)	2005-12-27	2009-06-15	Ipca Lab Ltd	Processo melhorado para o fabrico de ácido 4-amino-hidroxibutilideno-1,1 bisfosfónico e seus sais
WO2007083240A2 (fr)	2006-01-20	2007-07-26	Aurobindo Pharma Limited	Procede ameliore de preparation d’acides bisphosphoniques
CA2570949A1 (fr) *	2006-12-12	2008-06-12	Apotex Pharmachem Inc.	Solvate d'ibandronate sodique et de propyleneglycol et methodes de preparation connexes
JP5507256B2 (ja)	2006-12-13	2014-05-28	スリーエムイノベイティブプロパティズカンパニー	酸性成分及び光退色性染料を有する歯科用組成物の使用方法
SI2144919T1 (sl)	2007-04-11	2016-02-29	F. Hoffmann-La Roche Ag	Večstopenjska sinteza ibandronata
WO2008157050A1 (fr) *	2007-06-19	2008-12-24	Albemarle Corporation	Procédés de fabrication d'acides bisphosphoniques
WO2009050731A2 (fr) *	2007-06-20	2009-04-23	Alkem Laboratories Ltd	Procédé inédit de préparation de l'acide risédronique
US20090170815A1 (en) *	2007-12-28	2009-07-02	Roxane Laboratories Incorporated.	Alendronate oral liquid formulations
US20090197837A1 (en) *	2008-02-05	2009-08-06	Desai Vivek S	Alendronate formulations, method of making and method of use thereof
CN102124016A (zh) *	2008-07-11	2011-07-13	斯索恩有限公司	制备1-羟基亚烷基-1，1-双膦酸的方法
US20100130746A1 (en) *	2008-11-26	2010-05-27	Martin Kas	Process for Making Zoledronic Acid
US20120100206A1 (en)	2009-06-11	2012-04-26	Yissum Research Development Company Of The Hebrew University Of Jerusalem, Ltd.	Targeted liposomes comprising n-containing bisphosphonates and uses thereof
EP2470549B1 (fr)	2009-08-28	2014-07-16	Synthon B.V.	Procédé de fabrication d'acides 1-hydroxyalkylidène-1,1-biphosphoniques
KR20120095354A (ko)	2009-09-30	2012-08-28	가부시키가이샤 디엔피 파인 케미칼	잉크 조성물
CA2738045C (fr)	2010-05-28	2019-02-19	Simon Fraser University	Composes conjugues, leurs procedes de fabrication et leurs utilisations
EP2609101B1 (fr)	2010-07-14	2015-01-28	Pharmathen S.A.	Procédé de synthèse du sel d'acide 3-(n-méthyl-n-pentyl)amino-1-hydroxypropane-1,1-diphosphonique ou de ses dérivés
EP3378906A1 (fr)	2010-07-30	2018-09-26	Cabot Corporation	Composition à jet d'encre
CA2820019A1 (fr)	2010-12-06	2012-06-14	Effrx Pharmaceuticals Sa	Formulations effervescentes stables a base de bisphosphonate presentant des caracteristiques de solubilisation rapide
KR20140009266A (ko)	2010-12-27	2014-01-22	다이니폰 인사츠 가부시키가이샤	잉크젯 기록 방법
WO2012112363A1 (fr)	2011-02-14	2012-08-23	Merck Sharp & Dohme Corp.	Inhibiteurs de cystéine protéases, les cathepsines
CA2831368C (fr)	2011-03-29	2014-12-16	Dai Nippon Printing Co., Ltd.	Procede d'impression a jet d'encre et ensemble d'encre pour impression a jet d'encre
PT2731591T (pt)	2011-07-13	2020-09-18	Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd	Lipossomas que coencapsulam um bisfosfonato e um agente anfipático
GB201200868D0 (en)	2012-01-19	2012-02-29	Depuy Int Ltd	Bone filler composition
JP5722860B2 (ja)	2012-10-11	2015-05-27	株式会社Ｄｎｐファインケミカル	水性インクジェット受理溶液、この受理溶液を含むインクセット及びこのインクセットを用いたインクジェット記録方法
WO2015054089A1 (fr)	2013-10-08	2015-04-16	Merck Sharp & Dohme Corp.	Inhibiteurs de protéases à cystéine de type cathepsines
WO2015051479A1 (fr)	2013-10-08	2015-04-16	Merck Sharp & Dohme Corp.	Inhibiteurs de cystéine-protéases de type cathepsines
JP5779630B2 (ja)	2013-11-27	2015-09-16	株式会社Ｄｎｐファインケミカル	インクジェット記録用インク組成物、及びその製造方法、並びに、インクジェット記録方法
JP5676734B1 (ja)	2013-12-27	2015-02-25	株式会社Ｄｎｐファインケミカル	インクジェット記録用インク組成物、インクジェット記録方法、及び印刷物の製造方法
WO2015120580A1 (fr)	2014-02-11	2015-08-20	Merck Sharp & Dohme Corp.	Inhibiteurs de protéases à cystéine de type cathépsines
PL407922A1 (pl)	2014-04-16	2015-10-26	Wrocławskie Centrum Badań Eit + Spółka Z Ograniczoną Odpowiedzialnością	Nowe bisfosfoniany i ich zastosowanie
US9650414B1 (en)	2014-05-30	2017-05-16	Simon Fraser University	Dual-action EP4 agonist—bisphosphonate conjugates and uses thereof
SG11201609050UA (en)	2014-05-30	2016-12-29	Pfizer	Carbonitrile derivatives as selective androgen receptor modulators
CN104072538A (zh) *	2014-07-10	2014-10-01	陕西汉江药业集团股份有限公司	一种双膦酸盐类药物的合成方法
CN107849072B (zh)	2015-06-12	2020-12-15	西蒙弗雷泽大学	酰胺连接的ep4激动剂-二膦酸盐化合物及其用途
US12049475B2 (en)	2018-07-23	2024-07-30	Brise Pharmaceuticals Co., Ltd.	Bisphosphonate drug conjugates
WO2023275715A1 (fr)	2021-06-30	2023-01-05	Pfizer Inc.	Métabolites de modulateurs sélectifs du récepteur des androgènes

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE2534391C2 (de) *	1975-08-01	1983-01-13	Henkel KGaA, 4000 Düsseldorf	1-Hydroxy-3-aminoalkan-1,1-diphosphonsäuren
DE2745083C2 (de) *	1977-10-07	1985-05-02	Henkel KGaA, 4000 Düsseldorf	Hydroxydiphosphonsäuren und Verfahren zu deren Herstellung
DE2943498C2 (de) *	1979-10-27	1983-01-27	Henkel KGaA, 4000 Düsseldorf	Verfahren zur Herstellung von 3-Amino-1-hydroxypropan-1,1-diphosphonsäure
DE3016289A1 (de) *	1980-04-28	1981-10-29	Henkel KGaA, 4000 Düsseldorf	Verfahren zur herstellung von omega -amino-1-hydroxyalkyliden-1,1-bis-phosphonsaeuren
US4304734A (en) *	1980-10-16	1981-12-08	Vysoka Skola Chemicko-Technologicka	6-Amino-1-hydroxyhexylidene diphosphonic acid, salts and a process for production thereof
IT1201087B (it) *	1982-04-15	1989-01-27	Gentili Ist Spa	Bifosfonati farmacologicamente attivi,procedimento per la loro preparazione e relative composizioni farmaceutiche
US4639338A (en) *	1984-08-06	1987-01-27	Ciba-Geigy Corporation	Preparation of crystalline disodium 3-amino-1-hydroxypropane-1,1-diphosphonate pentahydrate
IT1196315B (it) *	1984-10-29	1988-11-16	Gentili Ist Spa	Procedimento per la preparazione di acidi difosfonici

1989
- 1989-06-09 US US07/363,820 patent/US4922007A/en not_active Expired - Lifetime
1990
- 1990-06-04 IL IL9461290A patent/IL94612A/en active IP Right Review Request
- 1990-06-07 CA CA002018477A patent/CA2018477C/fr not_active Expired - Lifetime
- 1990-06-07 FI FI902845A patent/FI93219C/fi active IP Right Grant
- 1990-06-07 PT PT94306A patent/PT94306B/pt not_active IP Right Cessation
- 1990-06-07 NZ NZ233972A patent/NZ233972A/en unknown
- 1990-06-08 KR KR1019900008394A patent/KR0137455B1/ko not_active Expired - Lifetime
- 1990-06-08 IE IE207390A patent/IE69564B1/en not_active IP Right Cessation
- 1990-06-08 AU AU57019/90A patent/AU625704C/en not_active Expired
- 1990-06-08 CH CH90306238T patent/CH0402152H1/fr unknown
- 1990-06-08 AT AT90306238T patent/ATE129713T1/de not_active IP Right Cessation
- 1990-06-08 NO NO902559A patent/NO177997C/no not_active IP Right Cessation
- 1990-06-08 ES ES90306238T patent/ES2080116T3/es not_active Expired - Lifetime
- 1990-06-08 DK DK90306238.8T patent/DK0402152T3/da active
- 1990-06-08 ZA ZA904446A patent/ZA904446B/xx unknown
- 1990-06-08 CY CY189490A patent/CY1894A/xx unknown
- 1990-06-08 DE DE69023280T patent/DE69023280T2/de not_active Expired - Lifetime
- 1990-06-08 EP EP90306238A patent/EP0402152B1/fr not_active Expired - Lifetime
- 1990-06-11 JP JP2152494A patent/JPH0662651B2/ja not_active Expired - Lifetime
1994
- 1994-03-04 JP JP6034560A patent/JPH0748391A/ja active Pending
- 1994-05-09 NO NO941726A patent/NO178228C/no not_active IP Right Cessation
1995
- 1995-06-14 HU HU95P/P00204P patent/HU211908A9/hu unknown
- 1995-12-13 GR GR950403512T patent/GR3018379T3/el unknown
1996
- 1996-02-02 LV LVP-96-28A patent/LV11472B/en unknown
- 1996-04-18 HK HK69596A patent/HK69596A/en not_active IP Right Cessation

Also Published As

Publication number	Publication date
HK69596A (en)	1996-04-26
PT94306A (pt)	1991-02-08
EP0402152A3 (fr)	1991-07-03
IL94612A0 (en)	1991-04-15
AU5701990A (en)	1990-12-13
NO177997B (no)	1995-09-25
FI93219B (fi)	1994-11-30
EP0402152A2 (fr)	1990-12-12
FI902845A0 (fi)	1990-06-07
AU625704B2 (en)	1992-07-16
CY1894A (en)	1990-06-08
PT94306B (pt)	1997-05-28
NO178228B (no)	1995-11-06
GR3018379T3 (en)	1996-03-31
DK0402152T3 (da)	1995-12-04
LV11472A (lv)	1996-08-20
NO178228C (no)	1996-02-14
JPH0662651B2 (ja)	1994-08-17
DE69023280T2 (de)	1996-06-20
KR910000768A (ko)	1991-01-30
IE902073L (en)	1990-12-09
NO902559D0 (no)	1990-06-08
NO902559L (no)	1990-12-10
IE69564B1 (en)	1996-10-02
KR0137455B1 (ko)	1998-05-01
CA2018477A1 (fr)	1990-12-09
NO177997C (no)	1996-01-03
CH0402152H1 (fr)	2006-02-28
IL94612A (en)	1995-03-30
JPH0748391A (ja)	1995-02-21
NO941726L (no)	1990-12-10
JPH03101684A (ja)	1991-04-26
NO941726D0 (no)	1994-05-09
CA2018477C (fr)	1995-08-01
HU211908A9 (en)	1996-01-29
AU625704C (en)	2001-07-26
ZA904446B (en)	1992-06-24
NZ233972A (en)	1992-05-26
FI93219C (fi)	1995-03-10
US4922007A (en)	1990-05-01
DE69023280D1 (de)	1995-12-07
ES2080116T3 (es)	1996-02-01
EP0402152B1 (fr)	1995-11-02
ATE129713T1 (de)	1995-11-15

Publication	Publication Date	Title
EP0402152B1 (fr)	1995-11-02	Sel cristallin trihydraté de l'acide amino-4 hydroxy-1 butylidène-bisphosphonique-1,1, procédé pour sa preparation et ses compositions et utilisation
EP0462663B1 (fr)	1995-09-27	Procédé amélioré pour la préparation des sels de l'acide 4-amino-1-hydroxybutylidène-1, 1-bisphosphonique (ABP)
EP0971938B1 (fr)	2002-07-10	Procede de production d'acide 4-amino-1-hydroxybutylidene-1,1-bisphosphonique ou de sels de ce dernier
Kieczykowski et al.	1995	Preparation of (4-amino-1-hydroxybutylidene) bisphosphonic acid sodium salt, MK-217 (alendronate sodium). An improved procedure for the preparation of 1-hydroxy-1, 1-bisphosphonic acids
AU7674394A (en)	1995-03-21	Process for producing n-amino-1-hydroxy-alkyl-idene-1,1-bisphosphonic acids
EP1390373B9 (fr)	2006-08-16	Procede de preparation d'acide 4-amino-1-hydroxybutylidene-1, 1-biphosphonique
AU770312B2 (en)	2004-02-19	Novel process for preparing alendronic acid
WO2007010556A1 (fr)	2007-01-25	Procede de production d'acide 4-amino-1-hydroxybutylidene-1,1-bisphosphonique ou sels de celui-ci
MXPA98001171A (en)	1999-02-01	Process for the production of 4-amino-1-hydroxybutyliden-1,1-bisphosphonic acid or salts from my
WO1992014679A1 (fr)	1992-09-03	Preparation de 32p-thiophosphates