Slow release microsphere preparation of derivative of 3,3 ¿C diphenyl propylamine as receptor antagon of toadstool alkali in use for injection

A technology of diphenylpropylamine derivative and sustained-release microsphere preparation, applied in 3 as a muscarinic receptor antagonist, can solve problems such as increased treatment cost, inability to long-act sustained release, and low bioavailability
CN1795845AInactive Publication Date: 2006-07-05长春健欣生物医药科技开发有限公司

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
长春健欣生物医药科技开发有限公司
Publication Date
2006-07-05
Estimated Expiration
Not applicable · inactive patent

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Abstract

A slowly-releasing microspherical medicine used for the injection to treat the diseases associated with the antagon of muscarinic receptor, the impulsive inoontinence and urination urgency or frequency is prepared from 3,3-diphenyl propylamine derivative, its optical enantiomer or cacemer, and the biodegradable medical high-molecular auxiliary. Its preparing process is also disclosed.
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Description

technical field

[0001] The present invention relates to a sustained-release microsphere preparation for injection of 3,3-diphenylpropylamine derivatives and a preparation method thereof. The present invention also relates to the preparation of said preparation for the treatment or auxiliary treatment of diseases related to muscarinic receptors and Use of medications for unstable or overactive bladder including urge incontinence, urinary urgency, or frequency. Background technique

[0002]

[0003] It is reported that (R)-N,N-diisopropyl-3-(2-hydroxy-5-hydroxymethylphenyl)-3-phenylpropylamine (Ia) and (R)-N,N-di Isopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropylamine (tolterodine) (II) is a muscarinic receptor antagonist (EP0325571; WO94 / 11337), which It can be used to treat unstable or overactive bladder including impulse incontinence, urgency or frequency. By modifying their structures, it is found that some of their derivatives or prodrugs have similar effects (EP0...

Claims

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