(3,4-dichloro-phenyl)-((S)-3-propyl-pyrrolidin-3-yl)-methanone hydrochloride and manufacturing processes

US9527810B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9527810-B2
Application numberUS-201414522775-A
CountryUS
Kind codeB2
Filing dateOct 24, 2014
Priority dateApr 25, 2012
Publication dateDec 27, 2016
Grant dateDec 27, 2016

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  1. Title

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  2. Abstract

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  5. First independent claim

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Abstract

Official abstract text for this publication.

The present invention is concerned with a novel process for the preparation of a compound of formula I and its hydrates The compounds of formula I and the corresponding hydrates are pharmaceutically active substances.

First claim

Opening claim text (preview).

The invention claimed is: 1. A crystalline polymorph of (3,4-Dichloro-phenyl)-((S)-3-propyl-pyrrolidin-3-yl)-methanone hydrochloride of formula I or a hydrate thereof. 2. The crystalline polymorph of claim 1 which is (3,4-Dichloro-phenyl)-((S)-3-propyl-pyrrolidin-3-yl)-methanone hydrochloride quarterhydrate. 3. The crystalline polymorph of the compound of claim 1 , wherein the crystalline polymorph has an X-ray powder diffraction pattern having at least one characteristic peak expressed in values of degrees 2-theta at approximately degree 2-theta 5.5 9.4 10.6 12.5 14.6 16.2 16.6 17.3 18.6 19.6 22.2 22.7 23.1 23.7 25.3. 4. The crystalline polymorph of the compound of claim 1 , wherein the crystalline polymorph has an X-ray powder diffraction pattern having characteristic peaks expressed in values of degrees 2-theta at approximately degree 2-theta 5.5 9.4 10.6 12.5 14.6 16.2 16.6 17.3 18.6 19.6 22.2 22.7 23.1 23.7 25.3. 5. The crystalline polymorph of the compound of claim 1 , wherein the crystalline polymorph has an X-ray powder diffraction pattern as shown in FIG. 1 . 6. Substantially pure crystalline polymorph of 3,4-Dichloro-phenyl)-((S)-3-propyl-pyrrolidin-3-yl)-methanone hydrochloride quarterhydrate according to claim 1 . 7. The crystalline polymorph of the compound of claim 1 , wherein the crystalline polymorph has the following unit cell parameters a  6.14 Å b 16.70 Å c 17.43 Å alpha 66.73° beta 81.47° gamma  86.51°. 8. The crystalline polymorph of the compound of claim 1 , wherein the crystalline polymorph has an X-ray powder diffraction pattern having at least one characteristic peak expressed in values of degrees 2-theta at approximately degree 2-theta 5.2 10.5 12.3 15.3 15.6 16.0 17.1 18.8 23.0 23.9 27.2 28.2 30.5. 9. The crystalline polymorph of the compound of claim 1 , wherein the crystalline polymorph has an X-ray powder diffraction pattern as shown in FIG. 2 . 10. A pharmaceutical composition comprising a crystalline polymorph of a compound of claim 1 and a pharmaceutically acceptable carrier. 11. A method for treating depression, anxiety, or both, said method comprising administering to a subject in need thereof an effective amount of a crystalline polymorph of a compound of claim 1 .

Assignees

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Classifications

  • Antidepressants · CPC title

  • C07D207/08Primary

    with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms · CPC title

  • Anxiolytics · CPC title

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Frequently asked questions

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What does patent US9527810B2 cover?
The present invention is concerned with a novel process for the preparation of a compound of formula I and its hydrates The compounds of formula I and the corresponding hydrates are pharmaceutically active substances.
Who is the assignee on this patent?
Hoffmann La Roche
What technology area does this patent fall under?
Primary CPC classification C07D207/08. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Tue Dec 27 2016 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).