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Therapeutic combinations comprising selective estrofen receptor modulator and parathyroid hormone

A parathyroid hormone and composition technology, applied in the direction of medical preparations containing active ingredients, drug combinations, organic active ingredients, etc., to increase bone mass, inhibit osteoporosis and related bone diseases, and reduce fracture rates

Inactive Publication Date: 2001-07-25
PFIZER PRODS ETAT DE CONNECTICUT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, estrogen and estrogen agonists alone are only expected to reduce fracture risk by about 50%, resulting in about 50% of osteopenic women still at risk for osteoporotic fracture

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] 6.5-month-old S-D female rats were subjected to mock surgery (n=18) or ovariectomized (OVX) (n=42), and 6 days after surgery, 9-day mock-surgery rats and 7 OVX rats were killed As a control group before treatment, while the remaining OVX rats were treated with PTH (40 μg / kg / day, subcutaneously injected (s.c.) with 0.1% bovine serum (BAS) solution), (-)-cis-6-phenyl-5- [4-(2-Pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetralin-2-ol (0.1 mg / kg / day in 5% ethanol / Oral gavage (o.g.) in water) or a combination of both (40 μg / kg / day, s.c. injection of PTH and 0.1 mg / kg / day, oral gavage (o.g.) of (-)-cis-6-phenyl-5-[ 4-(2-Pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetralin-2-ol) for 60 days. All rats were injected subcutaneously with 10 mg / kg calcein (Sigma Chemical Co., St. Louis, MO) 12 and 2 days before necropsy. The small tibial metaphysis was determined by standard static and dynamic histomorphometry techniques (Parfitt A.M. et al., Bone histomorphometry: Standardization of no...

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PUM

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Abstract

This invention is directed to pharmaceutical combination compositions and methods comprising (-)-cis-6-phenyl-5-(4-(2-pyrrolidin-1-yl-ethoxy)-phenyl)-5,6,7,8-tetrahydronaphthalene-2-ol or a pharmaceutically acceptable salt thereof and parathyroid hormone or a biologically active fragment thereof, methods of using such compositions and kits containing such compositions. The compositions are useful for treating musculoskeletal frailty, including osteoporosis, osteoporotic fracture, low bone mass and frailty.

Description

Background of the invention [0001] The present invention relates to therapeutic compositions comprising a selective estrogen receptor modulator (SERM) and parathyroid hormone (PTH) or a biologically active fragment thereof, which stimulate bone formation, increase bone mass and enhance the bone healing effects of PTH. The present invention also relates to a kit containing the composition and the use of the composition in the treatment of muscular and skeletal frailty, including osteoporosis, osteoporotic fractures, low bone quality, frailty, etc., in mammals, including humans. More specifically, the present invention relates to (-)-cis-6-phenyl-5-(4-(2-pyrrolidin-1-yl-ethoxy)-phenyl)-5,6,7,8 - a composition of tetralin-2-ol or a pharmaceutically acceptable salt thereof and parathyroid hormone or a bioactive fragment thereof, a kit containing the composition, and the composition for treating muscular dystrophy in mammals, including humans Applications in fragile bones, includi...

Claims

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Application Information

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IPC IPC(8): A61K38/22A61KA61K31/40A61K31/402A61K31/435A61K38/29A61P5/32A61P19/00A61P19/08A61P19/10C07CC07D
CPCA61K38/29A61P19/00A61P19/08A61P19/10A61P5/32A61K2300/00A61K31/40
Inventor 柯华珠戴维·D·汤普森
Owner PFIZER PRODS ETAT DE CONNECTICUT
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