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Treating method and medicine kit containing somatotrophic hormone secretory agent

A somatotropin, hyperphagia technology, applied in the field of treatment and kits containing somatotropin secretors, which can solve the problem of expensive products

Inactive Publication Date: 2003-04-16
PFIZER PRODS ETAT DE CONNECTICUT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This results in a very expensive product and carries the risk that diseases related to the source of the pituitary gland may be transmitted to somatropin recipients
Recombinant somatropin is now available, which no longer carries any risk of spreading disease, but is still an expensive drug that must be given by injection
In addition, administration of exogenous growth hormone can result in side effects, including edema, independent of the pulsatile release observed with endogenous release of growth hormone

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0325] Raw material preparation

[0326] a) Pyridine-2-amino-5-sulfonic acid

[0327] 2-Aminopyridine (80 g, 0.85 mol) was added to oleum (320 g) in portions over 30 minutes, and the resulting solution was heated at 140° C. for 4 hours. After cooling, the reaction was poured into ice (200 g) and the mixture was stirred for a further 2 hours in the ice / salt bath. The resulting suspension was filtered, the solid was washed with ice water (200ml) and cold IMS (200ml) and dried by suction to give the title compound as a solid, 111.3g; LRMS: m / z 175 (M+1) + .

[0328] b) Pyridine-2-amino-3-bromo-5-sulfonic acid

[0329] Bromine (99g, 0.62mol) was added dropwise to a hot solution of the product from step a) (108g, 0.62mol) in water (600ml) over 1 hour so as to maintain a steady reflux. Once the addition was complete, the reaction was cooled and the resulting mixture was filtered. The solid was washed with water and dried by suction to give the title compound, 53.4 g; δ(...

Embodiment 2

[0344] 5-[2-isobutoxy-5-(4-ethylpiperazin-1-ylsulfonyl)pyridin-3-yl]-3-ethyl-2-(1-methyl Piperidin-4-yl)-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one

[0345] In a sealed container, the product from step b) below (90 mg, 0.156 mmol), potassium bis(trimethylsilyl)amide (156 mg, 0.78 mmol) and ethyl acetate (14 mg, 0.156 mmol) were dissolved in isopropanol (12ml) was stirred at 130°C for 6 hours. The cooled reaction mixture was poured into saturated aqueous sodium bicarbonate (60ml), extracted with ethyl acetate (60ml). The combined organic extracts were dried (MgSO 4 ), and evaporated under reduced pressure to give a gum. The crude product was purified by silica gel column chromatography using dichloromethane:methanol:0.88 ammonia (92.6:6.6:0.6) as eluent to obtain the title compound as a brown beige foam, 36 mg; δ(CDCl 3 )1.01(3H, t), 1.12(6H, d), 1.39(3H, t), 1.94(2H, m), 2.15(2H, m), 2.22-2.44(6H, m), 2.55(6H, m ), 3.02(4H,m), 3.14(4H,m), 4.22(1H,m), 4.43(2H,d), 8...

Embodiment 3

[0352] 5-[2-Ethoxy-5-(4-ethylpiperazin-1-ylsulfonyl)pyridin-3-yl]-3-ethyl-2-phenyl-2,6-di Hydrogen-7H-pyrazolo[4,3-d]pyrimidin-7-one Pyridine (0.1 ml, 1.08 mmol) was added to the product of step a) below (250 mg, 0.54 mmol), copper(II) acetate monohydrate (145 mg, 0.72 mmol), benzeneboronic acid (132 mg, 1.08 mmol) ) and 4 Å molecular sieves (392 mg) in dichloromethane (5 ml), the reaction was stirred at room temperature for 4 days. The reaction mixture was filtered and the filtrate was evaporated under reduced pressure. The crude product was purified by column chromatography on silica gel using dichloromethane:methanol:0.88 ammonia (97:3:0.5) as eluent and triturated with diethyl ether:hexane. The resulting solid was filtered and recrystallized from isopropanol:dichloromethane to afford the title compound as a solid, 200 mg, δ(CDCl 3 )1.02(3H, t), 1.47(3H, t), 1.60(3H, t), 2.42(2H, q), 2.58(4H, m), 3.10(2H, q), 3.17(4H, m), 4.76(2H,q), 7.40(1H,m), 7.51(2H,m), 7.80(2H,d)...

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Abstract

The present invention relates to methods of treating bulimia nervosa, male erectile dysfunction, female sexual dysfunction, thyroid cancer, breast cancer, or ameliorating ischemic nerve or muscle damage. The present invention also relates to kits that can be used in the treatment of bulimia nervosa, male erectile dysfunction, female sexual dysfunction, thyroid cancer, breast cancer, or ameliorating ischemic nerve or muscle damage. The present invention further relates to increasing gastrointestinal motility after surgery and increasing gastrointestinal motility in patients who have been administered an agent that decreases gastrointestinal motility.

Description

field of invention [0001] The present invention relates to methods of treating bulimia nervosa, male erectile dysfunction, female sexual dysfunction, thyroid cancer, breast cancer, or alleviating ischemic nerve or muscle damage. The present invention also relates to kits useful for treating bulimia nervosa, male erectile dysfunction, female sexual dysfunction, thyroid cancer, breast cancer, or alleviating ischemic nerve or muscle damage. The present invention also relates to methods of enhancing gastrointestinal motility postoperatively and in patients administered drugs that reduce gastrointestinal motility. Background of the invention [0002] The present invention relates to novel methods of treatment and kits comprising somatotropin secreting agents. [0003] Growth hormone, secreted by the pituitary gland, stimulates the growth of all viable tissues in the body. In addition, growth hormone is known to have the following fundamental effects on the metabolic processes o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61KA61K31/437A61K31/4375A61K31/444A61K31/495A61K31/4985A61K31/519A61K38/17A61K38/27A61K45/00A61P1/00A61P1/10A61P3/04A61P5/10A61P15/00A61P15/08A61P15/10A61P21/00A61P25/00A61P35/00A61P43/00C07DC07D471/04
CPCA61K31/495A61K31/437A61P1/00A61P1/10A61P15/00A61P15/08A61P15/10A61P21/00A61P25/00A61P35/00A61P3/04A61P43/00A61P5/10A61K31/4985
Inventor 菲利普·A·卡皮诺戴维·A·格里菲思约翰·R·N·哈德科克威廉·H·兰德舒尔茨莉迪亚·C·潘
Owner PFIZER PRODS ETAT DE CONNECTICUT
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