160359-68-2

Upstream product

• 85-44-9 phthalic anhydride 
• 67025-97-2 6β-naltrexamine 

Downstream Products

• 936833-87-3 2-((4R,4aS,7R,7aR,12bS,13S)-9-(benzyloxy)-3-(cyclopropylmethyl)-4a,13-dihydroxy-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl)isoindoline-1,3-dione 

Relevant academic research and scientific papers

CRYSTALLINE MICROPOWDER PARTICLES

Crystalline particles of N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-phthalimide or a pharmaceutically acceptable salt thereof are disclosed. The crystalline particles have a particle diameter distribution in which a particle diameter (D50) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 50% is within a range of 1 to 30 μm, and a particle diameter (D90) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 90% is not more than 90 μm, which crystalline particles have a degree of crystallinity of not less than 80%. By the crystalline particles, bioavailability of the active substance may be increased while ensuring storage stability of the compound.

THERAPEUTIC OR PROPHYLACTIC AGENT FOR FUNCTIONAL BOWEL DISORDER

A therapeutic or prophylactic agent for functional bowel disorders comprising as an effective ingredient a morphinan derivative having a nitrogen-containing cyclic group or a pharmaceutically acceptable acid addition salt thereof is disclosed. The therapeutic or prophylactic agent for functional bowel disorders comprises as an effective ingredient a morphinan derivative or a pharmaceutically acceptable acid addition salt thereof, having a specific structure, such as N-(17-cyclopeopylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-3,4,5,6-tetrahydrophthalimide tartaric acid salt (Compound 10).

MORPHINAN DERIVATIVES AS ANTI-ITCHING AGENT

A novel antipruritic useful for the treatment of pruritus accompanying various diseases is disclosed. The antipruritic comprises a specific morphinan derivative having a nitrogen-containing cyclic group or the pharmaceutically acceptable acid addition salt thereof such as N-(17-cyclopropylmethyl-4,5±-epoxy-3,14-dihydroxy-morphinan-62-yl)-phthalimide hydrochloric acid salt or N-( 17-cyclopropylmethyl-4,5±-epoxy-3,14-dihydroxy-morphinan-62-yl)-3,4,5,6-tetrahydrophthalimide tartaric acid salt.

REMEDIES OR PREVENTIVES FOR URINARY FREQUENCY OR URINARY INCONTINENCE AND MORPHINAN DERIVATIVES HAVING NITROGEN-CONTAINING HETEROCYCLIC GROUP

The invention provides a morphinan derivative of the Formula (I): [wherein R1 is methyl, cyclopropylmethyl or the like; R2 and R3 are hydroxy, methoxy, acetoxy or the like; both Y and Z are valence bonds, -C(=O)- or the like; X is C2-C5 carbon chain (one of the carbon atoms may be substituted by oxygen, sulfur or nitrogen) constituting a part of the ring structure, or the like; (R4)k is substituted or non-substituted benzene fused ring, carbonyl group or the like; R9 is hydrogen or the like; R10 and R11 are bound to represent -O-, or the like, and R6 is hydrogen or the like] or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a therapeutic or prophylactic agent for urinary frequency or urinary incontinence, comprising as an effective ingredient the morphinan derivative or the pharmaceutically acceptable acid addition salt thereof; a method for therapy or prophylaxis of the diseases, and use for the diseases. The compounds of the invention are useful as a new therapeutic or prophylactic agent for urinary frequency or urinary incontinence, free from side effects, and useful for the method for therapy or prophylaxis of the diseases and for use for the diseases.