Quinuclidine Derivative for COPD Bronchodilation
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Solution Overview
Problem
Current treatments for chronic obstructive pulmonary disease (COPD) with quinuclidine derivatives and N-phenylbenzamide compounds provide only limited long-term bronchodilation and do not adequately address chronic lung inflammation, necessitating a more effective therapeutic agent.
Innovation Solution
A novel quinuclidine derivative with a specific chemical structure, represented by general formula (1), offering prolonged bronchodilation and anti-inflammatory effects, is developed to treat COPD, comprising a quinuclidine ring with specific substituents and anions, and is formulated into various pharmaceutical forms for administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If existing quinuclidine derivatives and N-phenylbenzamide compounds are used for COPD treatment, then bronchodilation effect is achieved, but the duration of action is insufficient and anti-inflammatory effect is inadequate
Solution Approach 1:
The patent modifies the chemical structure parameters of quinuclidine derivatives by introducing specific substituents at defined positions (R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, R29, R30, R31, R32, R33, R34, R35, R36, R37, R38, R39, R40, R41, R42, R43, R44, R45, R46, R47, R48, R49, R50, R51, R52, R53, R54, R55, R56, R57, R58, R59, R60, R61, R62, R63, R64, R65, R66, R67, R68, R69, R70, R71, R72, R73, R74, R75, R76, R77, R78, R79, R80, R81, R82, R83, R84, R85, R86, R87, R88, R89, R90, R91, R92, R93, R94, R95, R96, R97, R98, R99, R100) to extend the duration of bronchodilation effect and enhance anti-inflammatory activity, directly resolving the contradiction between duration and therapeutic reliability
Solution Approach 2:
The patent creates composite chemical structures combining quinuclidine core with various functional groups and substituents, producing a compound with dual functionality (bronchodilation and anti-inflammatory effects) that simultaneously addresses both aspects of therapeutic effectiveness and duration
2Reliability
If existing quinuclidine derivatives are used, then some bronchodilation effect is achieved, but anti-inflammatory action is insufficient for adequate COPD treatment
Solution Approach 1:
The patent designs quinuclidine derivatives with multiple functional capabilities including bronchodilation and anti-inflammatory effects, making the compound universally effective against multiple pathogenic mechanisms of COPD simultaneously, thereby resolving the contradiction between reliability and adaptability
Data Source
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AI summary
Provided is a novel therapeutic agent for chronic obstructive pulmonary disease. Provided are a quinuclidine derivative and a medicament comprising the quinuclidine derivative. wherein R1 represents a hydrogen atom, a halogen atom, a lower alkyl group, a haloalkyl group, a lower alkoxy group, or a haloalkoxy group; Y represents -C(C=O)-O-, -CH2-, or -CH2O-; m represents an integer of 1 to 5; Z represents an oxygen atom or a sulfur atom; l represents a number of 0 or l; n represents an integer of 0 to 4 ; X- represents an anion; and a substituent of a quinuclidine ring represents a 1,3-bond, or 1,4-bond, provided that when m is 3, l is 1, and n is 0, R1 represents a halogen atom, a lower alkyl group, a haloalkyl group, a lower alkoxy group, or a haloalkoxy group.