POLYMORPHOUS FORMS OF 1-[4-(5-CYANOINDOLE-3-YL)BUTYL]-4-(2-CARBAMOYLBENOFURAN-5-YL)-PIPERAZINE HYDROCHLORIDE Russian patent published in 2007 - IPC C07D405/12 A61K31/501 A61P25/00 

Abstract RU 2303598 C2

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel crystalline modifications of 1-[4-(5-cyanoindole-3-yl)butyl]-4-(2-carbamoylbenzofuran-5-yl)-piperazine hydrochloride, crystalline modification of 1-[4-(5-cyanoindole-3-yl)butyl]-4-(2-carbamoylbenzofuran-5-yl)-piperazine hydrochloride hydrate (forms V, VI, VIII) and 1-[4-(5-cyanoindole-3-yl)butyl]-4-(2-carbamoylbenzofuran-5-yl)-piperazine hydrochloride anhydrate (forms IV, III, VII, IX). Proposed forms can be used in preparing solid medicinal formulations for treatment of or prophylaxis of depressive states, anxiety disorders, maniacal-depressive disorders, maniacal syndrome, dementia, disorders associated with substrates deficiency, disorder in sexual function, alimentary disorders, obesity, fibromyalgia, insomnia, psychiatric disorders, brain infarction, hypertension, in treatment of adverse effects in treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesirable post-delivery lactation. Also, invention relates to methods for synthesis of forms V and IV and to pharmaceutical compositions and pharmaceutical preparation based on thereof. Invention provides the improved solubility, reduced hygroscopicity and increased storage time of synthesized compounds and the preparation based on thereof.

EFFECT: improved and valuable properties of forms.

13 cl, 46 dwg, 2 tbl, 16 ex

Similar patents RU2303598C2

Title Year Author Number
NEW APPLICATION OF 1-[4-(5-CYANOINDOL-3-YL)BUTYL]-4-(2-CARBAMOYLBENZOFURANE-5-YL)-PIPERAZINE AND ITS PHYSIOLOGICALLY ACCEPTABLE SALTS 2000
  • Bartoshik Gerd
  • Zejfrid Kristof
  • Van-Amsterdam Kristof
  • Bettkher Khenning
  • Zedman Ehven
RU2237477C2
NOVEL CRYSTALLINE FORM OF (3-CYANO-1N-INDOL-7-YL)-[4-(4-FLUOROPHENETHYL)PIPERAZIN-1-YL]METHANONE HYDROCHLORIDE 2005
  • Bate Andreas
  • Khel'Fert Bernd
  • Knirime Ral'F
  • Zal Kristof
  • Kajner Ronal'D
RU2383532C2
3-PHENYLSULFONYL-8-PIPERAZIN-1-YL-QUINOLINES HAVING AFFINITY TO 5-HT6RECEPTOR, METHODS FOR PRODUCTION THEREOF (VARIANTS) 2003
  • Akhmed Makhmud
  • Dzhonson Kristofer Norbert
  • Dzhouns Martin K.
  • Makdonald Gregor Dzhejms
  • Moss Stefen Frederik
  • Tompson Mervin
  • Vejd Charlz Edvard
  • Vitti Devid
RU2309154C9
SYNTHESIS OF TRANS-8-CHLOR-5-METHYL-1-[4-(PYRIDINE-2-ILOXY)-CYCLOHEXYL]-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZABENZO[E]AZULENE AND ITS CRYSTAL FORMS 2014
  • Rotenkhojsler, Benno
  • Trussardi, Rene
  • Khoffmann-Emeri, Fabenn
  • Shvitter, Urs
  • Adam, Zhan-Mishel
  • Grassmann, Olaf
  • Khartung, Tomas
  • Ran, Frederik
  • Diodone, Ralf
  • Fleger, Kristof
  • Bartels, Bern
RU2775690C2
METHOD FOR PREPARING (3-CYANO-1H-INDOLE-7-YL)-[4-(4-FLUOROPHENETHYL)-PIPERAZINE-1-YL]METHANONE AND ITS SALTS 2001
  • Krass'E Ehlen
  • Ehkkert Uve
  • Bettkher Khenning
  • Bateh Andreas
  • Ehmmert Shteffen
RU2295519C2
4-[2-[[5-METHYL-1-(2-NAPHTHALINYL)-1H-PYRAZOL-3-YL]OXY]ETHYL]MORPHOLINE HYDROCHLORIDE POLYMORPH AND SOLVATES 2011
  • Berenger Majmo Ramon
  • Medrano Ruperes Khorkhe
  • Benet Bukhkhol'Ts Khordi
  • Puig Fernandes Laura
  • Pellekha Pukseu Laja
RU2560150C2
USING COMPOUND COMBINING PROPERTY OF SEROTONIN REVERSE UPTAKE INHIBITOR AND AGONIST OF 5-HT-RECEPTOR 2001
  • Gerd Bartoshik
RU2288719C2
POLYMORPH FORM OF 4-{[4-({[4-(2,2,2-TRIFLUOROETHOXY)-1,2-BENZISOXAZOL-3-YL]OXY}METHYL)PIPERIDIN-1-YL]METHYL}-TETRAHYDRO-2H-PYRAN-4-CARBOXYLIC ACID 2012
  • Numata Tojokharu
  • Noguti Khirokhide
  • Vaizumi Nobuaki
  • Kodzima Takasi
RU2616978C2
TARTARE SALT [(S)-2-[METHYL-3-(2-OXO-PYRROLIDIN-1-YL)- BENZENESULFONYLAMINO]-3-(4-METHYL-PIPERAZINE-1-YL)-3-OXO-PROPYL]AMIDE 5-CHLORINE-THIOPHENE-2- CARBOXYLIC ACID 2014
  • Lyafferrer Loran
  • Vijon Sebasten
  • Gote Sandrin
  • Burbon Andre
RU2664538C2
POLYMORPHOUS FORM OF 3-PHENYLSULFONYL-8-PIPERASINE-1-YL-QUINOLINE 2004
  • Gladvin Asa Ehlizabet
RU2355681C2

RU 2 303 598 C2

Authors

Bate Andreas

Khel'Fert Bernd

Nojenfel'D Shteffen

Knil' Khajke

Bartel'S Mattias

Rudol'F Zuzanne

Bettkher Khenning

Dates

2007-07-27Published

2002-06-05Filed