Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are noscapine analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers. While the antitussive plant alkaloid, noscapine, binds tubulin, displays anticancer activity, and has a safe pharmacological profile in humans, structure-function analyzes pointed to a proton at position 9 of the isoquinoline ring that can be modified without compromising tubulin binding activity. Noscapine analogs with various functional moieties at position 9 on the isoquinoline ring kill human cancer cells resistant to other anti-microtubule agents, such as vincas and taxanes.

Joshi; Harish C.

Aneja; Ritu

Vangapandu; Surya N.

Emory University

Noscapine analogs and their use in treating cancers

An antitussive agent containing an octahydroisoquinoline derivative represented by the following compound or pharmacologically acceptable acid addition salt thereof: ##STR1##The compounds of the present invention have the significant antitussive action, and can thus be expected as medicines which can be used for all diseases accompanied with coughs, for example, various respiratory diseases such as cold, acute bronchitis, chronic bronchitis, bronchiectasis, pneumonia, pulmonary tuberculosis, silicosis and silicotuberculosis, lung cancer, upper respiratory inflammation (pharyngitis, laryngitis, nasal catarrhalis), asthmatic bronchitis, bronchial asthma, infantile asthma, (chronic) pulmonary emphysema, pneumoconiosis, pulmonary fibrosis, silicosis, pulmonary suppuration, pleurisy, tonsillitis, tussive urticaria, pertussis, etc. and coughs caused in bronchography or bronchoscopy, etc.

Toray Industries, Inc.

Antitussives

An agent for preventing/treating respiratory diseases contains, as an active ingredient, a compound represented by following Formula (I): ##STR00001## wherein A is a group represented by L-W [wherein L is a bond or CH.sub.2; and W is O, SOn (wherein n is 0 to 2), or --NR.sup.7-- (wherein R.sup.7 is hydrogen or lower alkyl)]; each of G.sup.1 and G.sup.2 is (CH.sub.2)r (wherein r is 0 to 2), provided that when n is 1, G.sup.1 and G.sup.2 may be bridged by lower alkylene; Y is a lower alkylene or (substituted) benzylidene; Z is a bond or O, provided that when Z is a bond, Y may form a 5- or 6-membered ring with carbon on the benzene ring; R.sup.1 is, for example, NO.sub.2, a lower alkoxycarbonyl, (substituted) carbamoyl, (protected) hydroxyl group, (protected) carboxyl, or (protected) N-hydroxycarbamoyl; each of R.sup.2 and R.sup.3 is hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy or NO.sub.2; each of R.sup.4 and R.sup.5 is, for example, hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy, CN, or lower alkylsulfonyl; and R.sup.6 is hydrogen or lower alkyl, a salt thereof or a solvate of them. It has excellent antitussive activity when used as an agent for preventing/treating respiratory diseases such as lung cancer, common cold syndrome, pulmonary tuberculosis, pneumonia, acute bronchitis or chronic bronchitis.

Mochida Pharmaceutical Co., Ltd.

Agent for treating respiratory diseases containing 4-hydroxypiperidine derivative as active ingredient

antitussives

cancro

neoplasms

antitussives/cancro

Noscapine analogs and their use in treating cancers

Antitussives

Agent for treating respiratory diseases containing 4-hydroxypiperidine derivative as active ingredient

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