Therapeutic combinations of (selective) estrogen receptor modulators (SERM) and growth hormone secretagogues (GHS) for treating musculoskeletal frailty

A use, carrier technology, applied in the drug combination form of selective estrogen receptor modulator and growth hormone secretagogue, and must be injected or field, can solve the problem of reducing carbohydrate utilization rate, infecting GH users, price Expensive and other problems, to achieve the effect of regressing osteoporosis and related bone diseases, reducing fracture rate, and increasing bone quality

Inactive Publication Date: 2001-06-27
PFIZER PRODS ETAT DE CONNECTICUT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] 2. Decreases the rate of utilization of carbohydrates in the cells of the body;
Therefore, the product is expensive and there is a risk that diseases related to pituitary origin may be transmitted to GH users (eg Jacob-Creutzfeld disease)
Recombinant GH has recently appeared and although it no longer poses any risk of infectious disease, it is still a very expensive product and must be given by injection or nasal spray

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Female S-D rats (Harlan) were sham-operated or ovariectomized (OVX) at 3.5 months of age. Dosing was started when the rats were 9 months old (5.5 months after surgery). Sham-operated rats received daily gavage of vehicle (10% ethanol in water), while OVX rats received daily gavage of vehicle, or 2-amino-N-(2-(3a(R)-benzyl -2-Methyl-3-oxo-2,3,3a,4,6,7-hexahydropyrazolo[4,3-c]pyridin-5-yl)-1(R)-benzyloxy Methyl-2-oxo-ethyl)-isobutyramide (5 mg / kg / day, used alone), or (-)-cis-6-phenyl-5-(4-(2-pyrrolidine-1 -yl-ethoxy)-phenyl)-5,6,7,8-tetralin-2-ol (0.1 mg / kg / day, used alone), or with 2-amino-N-(2- (3a(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydropyrazolo[4,3-c]pyridin-5-yl)- 1(R)-Benzyloxymethyl-2-oxo-ethyl)-isobutyramide and (-)-cis-6-phenyl-5-(4-(2-pyrrolidin-1-yl- Ethoxy)-phenyl)-5,6,7,8-tetralin-2-ol combination therapy for 4 weeks. In the combination therapy group, 2-amino-N-(2-(3a(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydropyrazolo [4,3-c]pyridin-5-yl)-1(...

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Abstract

This invention is directed to pharmaceutical combination compositions and methods containing (-)-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 2-amino-N-(2-(3a(R)-benzyl-2-methyl-3-oxo-2,3, 3a, 4,6,7-hexahydro-pyrazolo-[4,3-c]pyridin-5-yl)-1(R)-benzyloxymethyl-2-oxo-ethyl)-isobutyramide or a pharmaceutically acceptable salt 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, frailty and low muscle mass.

Description

Background of the invention [0001] The present invention relates to a drug combination of a selective estrogen receptor modulator (SERM) and a growth hormone secretagogue (GHS) that stimulates bone formation, increases bone mass, decreases serum lipid levels and increases muscle mass. The invention also relates to kits containing said combination and said combination for the treatment of musculoskeletal frailty, including osteoporosis, osteoporotic fractures, low bone mass, frailty, low muscle mass, in mammals, including humans. quality, etc. In particular, the present invention relates to (-)-cis-6-phenyl-5-(4-(2-pyrrolidin-1-yl-ethoxy)-phenyl)-5,6,7,8- Tetralin-2-ol or its pharmaceutically acceptable salts and 2-amino-N-(2-(3a(R)-benzyl-2-methyl-3-oxo-2,3,3a,4, 6,7-Hexahydropyrazolo[4,3-c]pyridin-5-yl)-1(R)-benzyloxymethyl-2-oxo-ethyl)-isobutyramide or its pharmaceutical Combinations with salts, kits containing said combinations and said combinations in mammals, including...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61KA61K31/437A61K31/16A61K31/40A61K31/402A61K31/4162A61K31/435A61P1/02A61P19/00A61P19/08A61P19/10A61P43/00C07C
CPCA61K31/435A61P1/02A61P19/00A61P19/08A61P19/10A61P43/00A61K31/40A61K2300/00
Inventor 柯华珠李梅L·C·潘D·D·汤普森
Owner PFIZER PRODS ETAT DE CONNECTICUT
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