EP2307015A2 - Composition pharmaceutique pour prévenir ou traiter l'ostéoporose à base de dérivés de benzamidine ou de sels de ceux-ci, et d'acide alendronique ou de sels de celui-ci - Google Patents

Composition pharmaceutique pour prévenir ou traiter l'ostéoporose à base de dérivés de benzamidine ou de sels de ceux-ci, et d'acide alendronique ou de sels de celui-ci

Info

Publication number
EP2307015A2
EP2307015A2 EP09803174A EP09803174A EP2307015A2 EP 2307015 A2 EP2307015 A2 EP 2307015A2 EP 09803174 A EP09803174 A EP 09803174A EP 09803174 A EP09803174 A EP 09803174A EP 2307015 A2 EP2307015 A2 EP 2307015A2
Authority
EP
European Patent Office
Prior art keywords
benzamidine
pentoxy
thiazol
phenoxy
isopropyl
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.)
Withdrawn
Application number
EP09803174A
Other languages
German (de)
English (en)
Other versions
EP2307015A4 (fr
Inventor
Jin Soo Lee
Yun Ha Hwang
Jei Man Ryu
Jae Hoon Park
Duk Kyun Chung
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Dong Wha Pharm Co Ltd
Original Assignee
Dong Wha Pharm Co Ltd
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.)
Filing date
Publication date
Application filed by Dong Wha Pharm Co Ltd filed Critical Dong Wha Pharm Co Ltd
Publication of EP2307015A2 publication Critical patent/EP2307015A2/fr
Publication of EP2307015A4 publication Critical patent/EP2307015A4/fr
Withdrawn legal-status Critical Current

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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A61K31/663—Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

  • osteoporosis means the state that minerals and substrates forming the bone are reduced abnormally in large amounts, even without any defect in the structure of the remaining bone, so that many pores are generated in the bone, making it like sponge and more likely to fracture. This may be referred to as "osteopenia”.
  • alendronic acid used in the present invention may be also prepared according to known processes, and a salt thereof or pharmaceutically acceptable salt thereof may be used without limitation, preferably its sodium salt.
  • the dosage of alendronic acid or a salt thereof is an effective amount for the prevention or treatment of osteoporosis, and determined depending on patient’s age and body weight, type of combination therapy, treatment frequency, type of desired efficacy, or administration method.
  • the compound may be administered in a typical amount.
  • alendronic acid or a salt thereof may be administered in a daily dose of 5 to 40 mg.
  • FIG. 2 is a graph showing the effect of individual or combination treatment of 0.3 ⁇ M N-hydroxy-4- ⁇ 5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl) phenoxy]pentoxy ⁇ benzamidine dimethanesulfonate and 0.2 ⁇ M alendronic acid on osteoclast differentiation, in which osteoclast differentiation was induced via co-culture of bone marrow cell and osteoblast, the cells were treated with each sample substance singly or simultaneously, and cultured for 7 days, and then TRAP staining was performed to count mature osteoclasts with 6 or more nuclei, expressed as a percentage to a control group.

Landscapes

  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

La présente invention concerne une composition pharmaceutique pour prévenir et traiter l'ostéoporose, qui comprend du N-hydroxy-4-{5-[4-(5-isopropyl-2-méthyl-1,3-thiazol-4-yl)phénoxy]pentoxy}benzamidine, du 4-{5-[4-(5-isopropyl-2-méthyl-1,3-thiazol-4-yl)phénoxy]pentoxy}benzamidine, ou des sels de ceux-ci, et de l'acide alendronique ou un sel de celui-ci. En tant que composition prophylactique ou thérapeutique pour l'ostéoporose, un traitement combiné à base de N-hydroxy-4-{5-[4-(5-isopropyl-2-méthyl-1,3-thiazol-4-yl)phénoxy]pentoxy}benzamidine, de 4-{5-[4-(5-isopropyl-2-méthyl-1,3-thiazol-4-yl)phénoxy]pentoxy}-benzamidine, ou de sels de ceux-ci et d'acide alendronique ou d'un sel de celui-ci permet d'assurer un excellent effet inhibiteur sur la différenciation des ostéoclastes, par comparaison avec chaque traitement individuel, ce qui s'avère être utile pour la prévention ou le traitement de l'ostéoporose.
EP09803174A 2008-08-01 2009-07-31 Composition pharmaceutique pour prévenir ou traiter l'ostéoporose à base de dérivés de benzamidine ou de sels de ceux-ci, et d'acide alendronique ou de sels de celui-ci Withdrawn EP2307015A4 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR20080075792 2008-08-01
PCT/KR2009/004277 WO2010013969A2 (fr) 2008-08-01 2009-07-31 Composition pharmaceutique pour prévenir ou traiter l'ostéoporose à base de dérivés de benzamidine ou de sels de ceux-ci, et d'acide alendronique ou de sels de celui-ci

Publications (2)

Publication Number Publication Date
EP2307015A2 true EP2307015A2 (fr) 2011-04-13
EP2307015A4 EP2307015A4 (fr) 2012-05-16

Family

ID=41610865

Family Applications (1)

Application Number Title Priority Date Filing Date
EP09803174A Withdrawn EP2307015A4 (fr) 2008-08-01 2009-07-31 Composition pharmaceutique pour prévenir ou traiter l'ostéoporose à base de dérivés de benzamidine ou de sels de ceux-ci, et d'acide alendronique ou de sels de celui-ci

Country Status (6)

Country Link
EP (1) EP2307015A4 (fr)
JP (1) JP2011529875A (fr)
KR (1) KR20100014173A (fr)
CN (1) CN102149380B (fr)
CA (1) CA2732863A1 (fr)
WO (1) WO2010013969A2 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20100014090A (ko) * 2008-08-01 2010-02-10 동화약품주식회사 벤즈아미딘 유도체 또는 이의 염, 및 비스포스포네이트를 포함하는 골다공증의 예방 또는 치료용 약학 조성물

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003007947A1 (fr) * 2001-07-19 2003-01-30 Dong Wha Pharm. Ind. Co., Ltd. Utilisation de derives de 4-[(4-thiazolyl)phenoxy]alcoxy-benzamidine dans le traitement de l'osteoporose
WO2006004369A1 (fr) * 2004-07-05 2006-01-12 Dong Wha Pharmaceutical. Ind. Co., Ltd. Composition pharmaceutique servant a traiter des fractures osseuses
WO2010013975A2 (fr) * 2008-08-01 2010-02-04 Dong Wha Pharmaceutical Co., Ltd. Composition pharmaceutique pour prévenir ou traiter l'ostéoporose comprenant un dérivé de benzamidine ou un sel de celui-ci, et du bisphosphonate

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5451700A (en) * 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
CN1144806A (zh) * 1996-07-25 1997-03-12 南京药物研究所 氨基二膦酸类骨吸收抑制剂及其钠盐的制备方法
CA2278190A1 (fr) * 1997-02-04 1998-08-06 Hong-Suk Suh Derive 3-amino-1,2-benzoisoxazole, procede de preparation et utilisation
US5998390A (en) * 1998-09-28 1999-12-07 The Research Foundation Of State University Of New York Combination of bisphosphonate and tetracycline
KR100317935B1 (ko) * 1999-10-20 2001-12-22 유승필 대사성 골질환 치료용 약제조성물 및 이의 제조방법
JP2003292453A (ja) * 2002-04-02 2003-10-15 Asahi Kasei Corp 骨疾患治療用医薬複合剤
JPWO2005002590A1 (ja) * 2003-07-01 2006-08-10 アステラス製薬株式会社 骨量増加誘導剤
JP2007502300A (ja) * 2003-08-13 2007-02-08 カイロン　コーポレイション Ｇｓｋ−３インヒビターおよびその使用
US7410977B2 (en) * 2004-04-28 2008-08-12 Merck & Co., Inc. Fluorinated 4-azasteroids as androgen receptor modulators
JP2009017222A (ja) * 2007-07-04 2009-01-22 Panasonic Corp 色調整装置、色調整方法および色調整装置の集積回路

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003007947A1 (fr) * 2001-07-19 2003-01-30 Dong Wha Pharm. Ind. Co., Ltd. Utilisation de derives de 4-[(4-thiazolyl)phenoxy]alcoxy-benzamidine dans le traitement de l'osteoporose
WO2006004369A1 (fr) * 2004-07-05 2006-01-12 Dong Wha Pharmaceutical. Ind. Co., Ltd. Composition pharmaceutique servant a traiter des fractures osseuses
WO2010013975A2 (fr) * 2008-08-01 2010-02-04 Dong Wha Pharmaceutical Co., Ltd. Composition pharmaceutique pour prévenir ou traiter l'ostéoporose comprenant un dérivé de benzamidine ou un sel de celui-ci, et du bisphosphonate

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
BLACK D M ET AL: "THE EFFECTS OF PARATHYROID HORMONE AND ALENDRONATE ALONE OR IN COMBINATION IN POSTMENOPAUSAL OSTEOPOROSIS", NEW ENGLAND JOURNAL OF MEDICINE, vol. 349, no. 13, 25 September 2003 (2003-09-25), pages 1207-1215, XP009045315, MASSACHUSETTS MEDICAL SOCIETY, BOSTON, MA, US ISSN: 1533-4406, DOI: 10.1056/NEJMOA031975 *
GREENSPAN SUSAN L ET AL: "Combination therapy with hormone replacement and alendronate for prevention of bone loss in elderly women: A randomized controlled trial.", JAMA (JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION), vol. 289, no. 19, 21 May 2003 (2003-05-21) , pages 2525-2533+CORR, XP002672632, ISSN: 0098-7484 *
See also references of WO2010013969A2 *

Also Published As

Publication number Publication date
CN102149380B (zh) 2012-12-05
CN102149380A (zh) 2011-08-10
WO2010013969A3 (fr) 2010-05-27
WO2010013969A2 (fr) 2010-02-04
KR20100014173A (ko) 2010-02-10
CA2732863A1 (fr) 2010-02-04
JP2011529875A (ja) 2011-12-15
EP2307015A4 (fr) 2012-05-16

Similar Documents

Publication Publication Date Title
US8227496B2 (en) Use of 4-[(4-thiazolyl)phenoxy]alkoxy-benzamidine derivatives for treatment of osteoporosis
US6693125B2 (en) Combinations of drugs (e.g., a benzimidazole and pentamidine) for the treatment of neoplastic disorders
US5476865A (en) Methods of inhibiting bone loss
US20130172304A1 (en) Pharmaceutical Compositions Comprising Flibanserin and a Further Agent in the Treatment of Sexual Disorders
US6043026A (en) Combination therapy for the prevention and treatment of osteoporosis
EP0652000A1 (fr) Inhibition d'angiogenese et de maladies angiogéniques
KR20170137201A (ko) 근육 위축 치료에 사용되는 유도체
WO2010013969A2 (fr) Composition pharmaceutique pour prévenir ou traiter l'ostéoporose à base de dérivés de benzamidine ou de sels de ceux-ci, et d'acide alendronique ou de sels de celui-ci
US7964584B2 (en) Method of treating or preventing osteoporosis comprising administering to a patient in need thereof an effective amount of pharmaceutical composition comprising benzamidine derivatives or their salts, and alendronic acid or its salt
JP5781077B2 (ja) ダウン症を治療するための方法および薬学的組成物
CN102149381A (zh) 包含苄脒衍生物或其盐和二膦酸盐、用于预防或治疗骨质疏松症的药物组合物
CA2199252A1 (fr) Procedes de traitement de l'osteoporose utilisant des phosphonates osteoactifs et une hormone parathiro?dienne
WO2019208968A1 (fr) Composition destinée à prévenir et à traiter une maladie musculaire
AU4054799A (en) Therapeutic combinations of (selective) estrogen receptor modulators (serm) and growth hormone secretagogues (ghs) for treating musculoskeletal frailty
AU3342099A (en) Therapeutic combinations of (selective) estrogen receptor modulators (serm) and growth hormone secretagogues (ghs) for treating musculoskeletal frailty
WO2012074184A1 (fr) Composition pharmaceutique pour empêcher ou traiter l'obésité, comprenant du sphingosine-1-phosphate ou un sel pharmaceutiquement acceptable de celui-ci en tant que principe actif
WO2018012683A1 (fr) Adjuvant anticancéreux
US20230310342A1 (en) Osteogenic agents and uses thereof
EP1513840B1 (fr) Composes et compositions de traitement du diabete et des troubles associes au diabete
WO2022065940A1 (fr) Utilisation d'agoniste de récepteur de sphingosine-1-phosphate
WO2024136627A1 (fr) Composition pharmaceutique contenant un inhibiteur du transporteur de sodium-glucose-2 et un bloqueur du récepteur de l'angiotensine ii pour la prévention ou le traitement d'une stéatose hépatique non alcoolique
US20190380999A1 (en) Combinations of genistein and bisphosphonates
US8507506B2 (en) Theophylline derivative inhibits osteoporosis
EP2177219A1 (fr) Agent préventif ou agent thérapeutique pour une maladie provoquée par un métabolisme osseux anormal
KR20120139581A (ko) 신규한 화합물, 이의 제조방법 및 이를 포함하는 골다공증 완화, 예방 또는 치료용 약학조성물

Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

17P Request for examination filed

Effective date: 20110201

AK Designated contracting states

Kind code of ref document: A2

Designated state(s): AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO SE SI SK SM TR

AX Request for extension of the european patent

Extension state: AL BA RS

DAX Request for extension of the european patent (deleted)
RIC1 Information provided on ipc code assigned before grant

Ipc: A61P 19/10 20060101ALI20120405BHEP

Ipc: A61K 31/663 20060101ALI20120405BHEP

Ipc: A61K 31/426 20060101AFI20120405BHEP

A4 Supplementary search report drawn up and despatched

Effective date: 20120416

17Q First examination report despatched

Effective date: 20130123

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN

18D Application deemed to be withdrawn

Effective date: 20130403