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Salt of abexinostat, associated crystalline form, a process for their preparation and pharmaceutical compositions containing them (Thu, 04 Sep 2014)
Abexinostat tosylate of formula (II): embedded image and its crystalline form I characterized by its X-Ray powder diffraction diagram, its Raman spectrum and its solid-state 13C CP/MAS NMR spectrum. Medicinal products containing the same which are useful in the treatment of cancer.
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NEW CRYSTALLINE FORM OF A BCL-2 INHIBITOR, A PROCESS FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING IT (Thu, 10 Jan 2019)
Crystalline form II of Compound A. HC1: (Formula) characterised by its X-ray powder diffraction diagram and solid-state 13C NMR spectrum, and pharmaceutical compositions containing it.
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DELTA CRYSTALLINE FORM OF THE ARGININE SALT OF PERINDOPRIL, A PROCESS FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSIITONS CONTAINING IT (Wed, 31 Jul 2013)

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Delta crystalline form of the arginine salt of perindopril, a process for its preparation, and pharmaceutical compositions containing it (Thu, 11 Jul 2013)
Delta crystalline form of the compound of formula (I): embedded image characterised by its X-ray powder diffraction diagram. Medicinal products containing the same which are useful in the treatment of cardiovascular diseases.
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Delta Crystalline Form of the Arginine Salt of Perindopril, a Process For Its Preparation, and Pharmaceutical Compositions Thereof (Thu, 17 Jan 2013)
DELTA CRYSTALLINE FORM OF THE ARGININE SALT OF PERINDOPRIL, A PROCESS FOR ITS PREPARATION, AND PHARMACEUTICAL COMPOSITIONS THEREOF Abstract Delta crystalline form of the compound of formula (I): characterised by its X-ray powder diffraction diagram. Medicaments and methods of medical treatment are also disclosed.
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Synthesis Process, and Crystalline Form of 4-{3-[cis-Hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}Benzamide Hydrochloride and Pharmaceutical Compositions Containing It (Thu, 07 Jun 2012)
SYNTHESIS PROCESS, AND CRYSTALLINE FORM OF 4-{3-[CIS-HEXAHYDROCYCLOPENTA[C]PYRROL-2(1 H) YL]PROPOXY}BENZAMIDE HYDROCHLORIDE AND PHARMACEUTICAL COMPOSITIONS CONTAINING IT Abstract The invention relates to an industrial synthesis process for, and crystalline form I of, the compound of formula (I): as well as crystalline form I of the associated free base. The invention also relates to medicaments and methods of medical treatment.
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SYNTHESIS PROCESS OF 4-{3-[CIS-HEXAHYDROCYCLOPENTA[C]PYRROL-2(1H)-YL]PROPOXY}BENZAMIDE HYDROCHLORIDE, CRYSTALLINE FORM OF SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME (Thu, 26 Jun 2014)
The present invention relates to an industrial synthesis process of a compound represented by chemical formula (I), a crystalline form I of the compound, a crystalline form I of a free base associated with the compound, and the use of the compound as a medicinal product. COPYRIGHT KIPO 2014
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DELTA CRYSTALLINE FORM OF ARGININE SALT OF PERINDOPRIL, A MANUFACTURING METHOD THEREOF, AND A PHARMACEUTICAL COMPOSITION INCLUDING THE SAME (Mon, 15 Jul 2013)
PURPOSE: A delta crystalline form of arginine salt of perindopril is provided to have a characteristic to be able to prevent conversion into octapeptide angiotensin II (vasopressor) and degradation of bradykinin (vasodilator) into inactivation peptide, and, therefore, contributes to a beneficial effect in cardiovascular diseases, in particular, arterial hypertension, heart failure, and stable coronary artery disease. CONSTITUTION: A delta crystalline form of perindopril L-arginine salt of Chemical formula (I), which is characterized in X-ray diffraction peak, is measured by using a diffractometer having a copper anticathode, and has Bragg's angle 2 theta (degree) of 4.3, 11.0, 13.2, 14.6, 16.0 and 21.9. The compound of Chemical formula (I), which is characterized in X-ray diffraction peak, is measured by using a diffractometer having a copper anticathode, and is expressed as the distance between planes d, Bragg's angle 2 theta, and a percentage to the strongest line. COPYRIGHT KIPO 2013 null [Reference numerals] (AA) Count; (BB) Position [*2 theta] (Copper (Cu)); (CC) X-ray diffraction view of a delta type perindopril L-arginine
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NOVEL SALTS OF A BCL-2 INHIBITOR,RELATED CRYSTALLINE FORMS,METHOD FOR PREPARING THE SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME (Thu, 11 Jul 2019)
Novel salts and related crystalline forms of Compound A : wherein the salt is selected in the following list: fumarate, hemifumarate, maleate, malonate, tosylate, hydrogensulfate, characterised by their X-ray powder diffraction diagram, method for preparing the same and pharmaceutical compositions containing them.
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Synthesis process, and crystalline form of 4-{3-[<i>cis</i>-hexahydrocyclopenta[<i>c</i>]pyrrol-2(1<i>H</i>)-yl]proxy}benzamide hydrochloride and pharmaceutical compositions containing it (Thu, 13 Dec 2012)
Industrial synthesis process for, and crystalline form I of, the compound of formula (I): embedded image and also crystalline form I of the associated free base. Medicinal products containing the same which are useful in the treatment of disorders of the histaminergic system.
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Process for the synthesis of 7-methoxy-naphthalene-1-carbaldehyde and application in the synthesis of agomelatine (Thu, 20 Oct 2016)
Process for the industrial synthesis of the compound of formula (I): embedded image
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Process for the enzymatic synthesis of (7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-triene-7-carboxylic acid or esters thereof, and application in the synthesis of ivabradine and salts thereof (Thu, 15 Aug 2013)
Process for the enzymatic synthesis of the compound of formula (I): embedded image wherein R1 represents a hydrogen atom or an alkyl group. Application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.
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Synthesis process, and crystalline form of 4-{3-[<i>cis</i>-hexahydrocyclopenta[<i>c</i>]pyrrol-2(1<i>H</i>)-yl]propoxy} benzamide hydrochloride and pharmaceutical compositions containing it (Thu, 10 Apr 2014)
Industrial synthesis process for the compound of formula (I): embedded image
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Process for the preparation of high purity perindopril and intermediates useful in the synthesis (Wed, 06 Aug 2003)
The invention relates to 1-ä2(S)-Ä1(S)-(ethoxycarbonyl)butylaminoÜpropionylü-(3aS,7aS)octahydro indol-2(S)-carboxylic acid of the Formula I and the t-butylamine salt of the Formula I' thereof free of contaminations derivable from dicyclohexyl carbodiimide, and a process for the preparation thereof. The invention also relates to new intermediates of the general Formula III (wherein R stands for lower alkyl or aryl lower alkyl). The compound of the Formula I - perindopril - is a known ACE inhibitor.
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Compounds of phosphinanes and azaphosphinanes, a process for their preparation and pharmaceutical compositions containing them (Thu, 18 Jan 2018)
Compounds of formula (I) embedded image wherein: Ak1 represents an alkyl chain, X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)—, —N(R)—CH2— or —CH2—N(R)—CH2—, m and R are as defined in the description, R1 and R2 each represent H when X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)— or —N(R)—CH2—, or together form a bond when X represents —CH2—N(R)—CH2—, R3 represents NH2, Cy-NH2, Cy-Ak3-NH2 or piperidin-4-yl, Cy and Ak3 are as defined in the description, R4 and R5, which may be identical or different, each represent H or F, their optical isomers, and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating conditions requiring a TAFIa inhibitor.
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NOVEL METHOD FOR PREPARATION OF CRYSTALLINE PERINDOPRIL ERBUMINE (Wed, 05 Jul 2006)
A process for preparation of crystalline perindopril erbumine of formula (II) which exhibits the X-ray (powder) diffraction pattern like that shown in the figure. The process comprises reacting a solution of perindopril of formula (I), in a solvent selected from N, N-dimethylformamide or dimethyl acetals of lower aliphatic aldehydes and ketones with tertiary butylamine and crystallization of the erbumine salt thus obtained by heating the reaction mixture to reflux, filtering hot, cooling gradually to 20 ºC to 30 ºC, and further cooling to 0º C to 15 ºC for 30 minutes to 1 hour and finally filtering off and drying the crystals.
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Process for the synthesis of agomelatine (Thu, 22 Dec 2016)
Process for the industrial synthesis of the compound of formula (I): embedded image
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COMPOUNDS OF PHOSPHINANES AND AZAPHOSPHINANES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (Thu, 31 Jan 2019)
Compounds of formula (I) embedded image wherein: Ak1 represents an alkyl chain, X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)—, N(R)—CH2— or —CH2—N(R)—CH2—, m and R are as defined in the description, R1 and R2 each represent H when X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)— or —N(R)—CH2—, or together form a bond when X represents —CH2—N(R)—CH2—, R3 represents NH2, Cy-NH2, Cy-Ak3-NH2 or piperidin-4-yl, Cy and Ak3 are as defined in the description, R4 and R5, which may be identical or different, each represent H or F, their optical isomers, and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating conditions requiring a TAFIa inhibitor.
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Novel phosphinane and azaphosphinane derivatives, method for preparing same and pharmaceutical compositions containing same (Thu, 20 Jul 2017)
Compounds of formula (I) in which: Ak1 represents an alkyl chain, X represents -(CH2)m-, -CH(R)-, -N(R)-,-CH2-N(R)-, –N(R)-CH2- or -CH2-N(R)-CH2-, m and R are as defined in the description, R1 and R2 each represent H when X represents -(CH2)m-, -CH(R)-, -N(R)-, -CH2-N(R)- or –N(R)-CH2-, or indeed together form a bond when X represents -CH2-N(R)-CH2-, R3 represents NH2, Cy-NH2, Cy-Ak3-NH2 or piperidin-4-yle, Cy and Ak3 are as defined in the description, R4 and R5, identical or different, each represent H or F, the optical isomers of same, and the pharmaceutically acceptable acid addition salts thereof. The invention also relates to drugs containing same.
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Isoquinoline compounds, a process for their preparation, and pharmaceutical compositions containing them (Thu, 18 May 2017)
A compound of formula (I): embedded image wherein the substituents are as defined in the description. Medicinal products containing the same which are useful in treating or preventing pathologies which are the result of activation of the RhoA/ROCK pathway and phosphorylation of the myosin light chain.
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