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

A technology of composition and drug, applied in the direction of drug combination, bone diseases, organic active ingredients, etc.

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

[0016] Many GH deficiencies arise through defects in GH release, not primary defects in pituitary synthesis of GH

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 12

[0081] Example 12-amino-N-{1-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-[3-oxo-3a-pyridin-2-ylmethyl-2 -(2,2,2-Trifluoro-ethyl)-2,3,3a,4,6,7-Hexahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethyl} -2-Methyl-propionamide L-(+) tartrate

[0082] A. 4-Oxo-3-pyridin-2-ylmethyl-piperidine-1.3-dicarboxylate 1-tert-butyl 3-ethyl ester

[0083]At a temperature of about 0°C, hydrochloride of picolyl chloride (5.7 g, 34.7 mmol), potassium carbonate (14.4 g, 104.1 mmol) and potassium iodide (5.76 g, 34.7 mmol) Add 1-tert-butyl 3-ethyl 4-oxo-piperidine-1,3-dicarboxylate (10.34 g, 38.2 mmol) in DMF (40 mL). After stirring at about 0°C for about two hours, the ice bath was removed and DABCO (973 mg, 8.68 mmol) was added. The reaction mixture was stirred for about 30 minutes, then poured into a mixture of water and IPE. The organic layer was separated and washed with saturated aqueous sodium bicarbonate and saturated aqueous sodium chloride, washed with Na 2 SO 4 Dry and concentrate under vacuum. ...

Embodiment 2

[0104] Female S-D rats (Harlan) were sham-operated or ovariectomized (OVX) at 3.5 months of age. Drug administration started when the rats were 9 months old and 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 5 mg / kg / day of 2-amino-N -(1(R)-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-(3-oxo-3a(R)-pyridin-2-ylmethyl)-2 -(2,2,2-Trifluoro-ethyl)-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethyl) -2-methyl-propionamide, or (-)cis-6-phenyl-5-(4-(2-pyrrolidin-1-yl-ethoxy)-benzene alone at 0.1 mg / kg / day base)-5,6,7,8-tetralin-2-ol, or 2-amino-N-(1(R)-(2,4-difluoro-benzyloxymethyl)-2- Oxo-2-(3-oxo-3a(R)-pyridin-2-ylmethyl)-2-(2,2,2-trifluoro-ethyl)-2,3,3a,4,6 ,7-Hexahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethyl)-2-methyl-propionamide and (-)cis-6-phenyl-5-(4- (2-Pyrrolidin-1-yl-ethoxy)-phenyl)-5,6,7,8-tetralin-2-ol co-treatment for 4 weeks. In the composition group, 2-amino-N-(...

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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 2-amino-N-(1(R) -(2,4-difluoro- benzyloxymethyl) -2-oxo-2-(3- oxo-3a(R) -pyridin-2- ylmethyl)-2-( 2,2,2-trifluoro-ethyl) -2,3,3a,4,6,7 -hexahydro -pyrazolo [4,3-c]pyridin -5-yl)-ethyl) -2-methyl-propionamide 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 pharmaceutical composition of a selective estrogen receptor modulator (SERM) and a growth hormone secretagogue (GHS) which stimulates bone formation, increases bone mass, reduces serum lipid levels and increases muscle mass . The present invention also relates to kits containing such compositions and the use of such compositions for the treatment of musculoskeletal conditions including osteoporosis, osteoporotic fractures, low bone mass, fragility, low muscle mass, etc. in mammals, including humans. of brittleness. More specifically, 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 salt and 2-amino-N-(1(R)-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-( 3-oxo-3a(R)-pyridin-2-ylmethyl)-2-(2,2,2-trifluoro-ethyl)-2,3,3a,4,6,7-hexahydro- Compositions of pyrazolo[4,3-c]pyridin-5-yl)-ethyl)-2-methyl-propionamide or phar...

Claims

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Application Information

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IPC IPC(8): C07D295/08A61KA61K31/40A61K31/402A61K31/435A61K31/437A61K31/44A61K31/444A61P1/02A61P19/00A61P19/08A61P19/10A61P43/00C07DC07D471/04
CPCA61K31/44A61P1/02A61P19/00A61P19/08A61P19/10A61P43/00A61K31/40A61K2300/00
Inventor 柯华珠李梅L·C·潘D·D·汤姆森
Owner PFIZER PRODS ETAT DE CONNECTICUT
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