RO115955B1 - Derivat de risperidonă, procedeu de obţinere şi compoziţie farmaceutică - Google Patents

Derivat de risperidonă, procedeu de obţinere şi compoziţie farmaceutică

Info

Publication number
RO115955B1
RO115955B1 RO95-01879A RO9501879A RO115955B1 RO 115955 B1 RO115955 B1 RO 115955B1 RO 9501879 A RO9501879 A RO 9501879A RO 115955 B1 RO115955 B1 RO 115955B1
Authority
RO
Romania
Prior art keywords
derivative
preparing
risperidone
pharmaceutical composition
chemical formula
Prior art date
Application number
RO95-01879A
Other languages
English (en)
Inventor
Jean Louis Mesens
Jozef Peeters
Original Assignee
Janssen Pharmaceutica N.V.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica N.V. filed Critical Janssen Pharmaceutica N.V.
Publication of RO115955B1 publication Critical patent/RO115955B1/ro

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
    • C07C65/105—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic
    • C07C65/11—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic with carboxyl groups on a condensed ring system containing two rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurosurgery (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)

Abstract

Grupul de invenţii se referă la un derivat de risperidonă, un procedeu de obţinere a acesteia, precum şi la o compoziţie farmaceutică care are în componenţă acest derivat de risperidonă. Derivatul de risperidonă, utilizat ca medicament, prezintă o structură corespunzătoare formulei chimice (I): are proprietăţi neuroleptice şi prezintă un punct de topire de 269,2°C. Procedeul de obţinere a derivatului de risperidonă cu formula chimică (I) constă în aceea că se tratează o soluţie de 3 - [2-[4-(6-fluor-1,2-benzisoxazol-3-il)-1-piperidinil]-6,7,8,9 -tetrahidro -2-metil -4H -pyrido [1,2 -a] pyrimidin -4 onă aflată într-un solvent inert constând din etanol, cu o soluţie de acid pamoic în solvent de N,N-dimetilformamidă, precipitatul rezultat se filtrează, se spală cu etanol şi se usucă în mod în sine cunoscut. Compoziţia farmaceutică, conform invenţiei, cuprinde un compus cu formula chimică (I), într-o cantitate eficientă din punct de vedere terapeutic, asociat cu un purtător acceptabil din punct de vedere farmaceutic şi se administrează într-o formă de dozare injectabilă, sub formă de suspensie apoasă. Compoziţia conform invenţiei include suplimentar alcool benzilic, esteri de sorbitan şi/sau un derivat de celuloză.
RO95-01879A 1993-04-28 1994-04-22 Derivat de risperidonă, procedeu de obţinere şi compoziţie farmaceutică RO115955B1 (ro)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP93201216 1993-04-28
PCT/EP1994/001296 WO1994025460A1 (en) 1993-04-28 1994-04-22 Risperidone pamoate

Publications (1)

Publication Number Publication Date
RO115955B1 true RO115955B1 (ro) 2000-08-30

Family

ID=8213799

Family Applications (1)

Application Number Title Priority Date Filing Date
RO95-01879A RO115955B1 (ro) 1993-04-28 1994-04-22 Derivat de risperidonă, procedeu de obţinere şi compoziţie farmaceutică

Country Status (32)

Country Link
US (2) US5612346A (ro)
EP (1) EP0697019B1 (ro)
JP (1) JP3478397B2 (ro)
KR (1) KR100307101B1 (ro)
CN (1) CN1041727C (ro)
AT (1) ATE163418T1 (ro)
AU (1) AU675136B2 (ro)
BG (1) BG62004B1 (ro)
CA (1) CA2160366C (ro)
CY (1) CY2107B1 (ro)
CZ (1) CZ286688B6 (ro)
DE (1) DE69408666T2 (ro)
DK (1) DK0697019T3 (ro)
ES (1) ES2113652T3 (ro)
FI (1) FI109125B (ro)
GR (1) GR3026028T3 (ro)
HK (1) HK1006059A1 (ro)
HU (1) HU218212B (ro)
IL (1) IL109448A (ro)
LV (1) LV12315B (ro)
NO (1) NO305083B1 (ro)
NZ (1) NZ266143A (ro)
PH (1) PH30476A (ro)
PL (1) PL182466B1 (ro)
RO (1) RO115955B1 (ro)
RU (1) RU2131428C1 (ro)
SG (1) SG47046A1 (ro)
SI (1) SI9420031B (ro)
SK (1) SK280589B6 (ro)
TW (1) TW376319B (ro)
WO (1) WO1994025460A1 (ro)
ZA (1) ZA942909B (ro)

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ATE288270T1 (de) * 1993-11-19 2005-02-15 Janssen Pharmaceutica Nv Mikroverkapselte 1,2-benzazole
US5453425A (en) * 1994-07-11 1995-09-26 Janssen Pharmaceutica N.V. Risperidone oral formulation
TW487572B (en) * 1996-05-20 2002-05-21 Janssen Pharmaceutica Nv Aqueous suspensions of 9-hydroxyrisperidone fatty acid esters
UA73715C2 (en) * 1997-09-30 2005-09-15 Lilly Co Eli Pharmaceutically acceptable formulation of olanzapine pamoate and its use for treatment
US6617321B2 (en) * 1997-09-30 2003-09-09 Eli Lilly And Company 2-methyl-thieno-benzodiazepine formulation
UA72189C2 (uk) 1997-11-17 2005-02-15 Янссен Фармацевтика Н.В. Фармацевтична композиція, що містить водну суспензію субмікронних ефірів 9-гідроксирисперидон жирних кислот
EA002580B1 (ru) * 1998-09-30 2002-06-27 Эли Лилли Энд Компани Готовая препаративная форма 2-метил-тиено-бензодиазепина
CA2349700A1 (en) * 1998-11-12 2000-05-18 Merck & Co., Inc. Therapeutic polymorphs of a gaba-a alpha-5 inverse agonist and pamoate formulations of the same
FR2802101B1 (fr) 1999-12-10 2003-02-28 Aventis Pharma Sa Association de cymemazine et d'un neuroleptique atypique
US6770478B2 (en) * 2000-02-10 2004-08-03 The Regents Of The University Of California Erythrocytic cells and method for preserving cells
US6495164B1 (en) 2000-05-25 2002-12-17 Alkermes Controlled Therapeutics, Inc. I Preparation of injectable suspensions having improved injectability
WO2002043766A1 (fr) * 2000-11-29 2002-06-06 Takeda Chemical Industries, Ltd. Compositions medicinales et leur procede de preparation
US20050232995A1 (en) 2002-07-29 2005-10-20 Yam Nyomi V Methods and dosage forms for controlled delivery of paliperidone and risperidone
US20060148826A1 (en) * 2002-08-23 2006-07-06 Ashish Gogia Stable aqueous solutions of risperidone and methods for their preparation
KR20040034996A (ko) * 2002-10-18 2004-04-29 한미약품 주식회사 리스페리돈의 개선된 제조방법
EP1615923A1 (en) * 2003-04-22 2006-01-18 Synthon B.V. Risperidone monohydrochloride
US6987111B2 (en) * 2003-08-06 2006-01-17 Alkermes Controlled Therapeutics, Ii Aripiprazole, olanzapine and haloperidol pamoate salts
ES2315721T5 (es) 2003-10-23 2012-08-24 Otsuka Pharmaceutical Co., Ltd. Formulación de aripiprazol inyectable estéril de liberación controlada y procedimiento
PL1708790T3 (pl) * 2003-12-02 2010-10-29 Pharmaneuroboost N V Zastosowanie pipamperonu oraz antagonisty receptora D2 lub antagonisty receptora serotoniny/dopaminy do leczenia zaburzeń psychotycznych
US7884096B2 (en) * 2003-12-02 2011-02-08 Pharmaneuroboost N.V. Method of treating mental disorders using of D4 and 5-HT2A antagonists, inverse agonists or partial agonists
WO2005072705A1 (en) * 2004-01-29 2005-08-11 Neuromolecular, Inc. Combination of a nmda receptor antagonist and a mao-inhibitor or a gadpf-inhibitor for the treatment of central nervous system-related conditions
ATE511512T1 (de) * 2005-01-05 2011-06-15 Lilly Co Eli Olanzapinpamoat-dihydrat
EP1695973A1 (en) * 2005-02-24 2006-08-30 Neuro3D Ocaperidone salt and pharmaceutical compositions containing the same
AR055099A1 (es) * 2005-07-28 2007-08-08 Alza Corp Formulaciones liquidas para la administracion controlada de derivados de bencisoxazol
JP2009508859A (ja) * 2005-09-15 2009-03-05 エラン ファーマ インターナショナル リミテッド ナノ粒子アリピプラゾール製剤
US8852638B2 (en) 2005-09-30 2014-10-07 Durect Corporation Sustained release small molecule drug formulation
BRPI0811319A2 (pt) 2007-05-25 2015-02-10 Tolmar Therapeutics Inc Composição fluida, método de formação de uma composição fluida, implante biodegrádavel formado in situ, método de formação de um implante biodegradável in situ, kit, implante e método de trataento
PT2170279T (pt) * 2007-07-31 2018-04-06 Otsuka Pharma Co Ltd Métodos para produção de suspensão de aripiprazole e formulação liofilizada
EP3909585A1 (en) * 2007-12-19 2021-11-17 Janssen Pharmaceutica NV Dosing regimen associated with long acting injectable paliperidone esters
US9034867B2 (en) 2011-03-18 2015-05-19 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising sorbitan esters
EP2702060B1 (en) * 2011-04-26 2015-12-30 Torrent Pharmaceuticals Limited Acid addition salts of risperidone and pharmaceutical compositions thereof
JP6471089B2 (ja) 2012-03-19 2019-02-13 アルカームス ファーマ アイルランド リミテッド 脂肪酸エステルを含む医薬組成物
JP6219918B2 (ja) 2012-03-19 2017-10-25 アルカームス ファーマ アイルランド リミテッド グリセロールエステルを含む医薬組成物
CA2867137C (en) 2012-03-19 2020-12-08 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising aripiprazole prodrugs and benzyl alcohol
AU2013245008B2 (en) 2012-04-04 2017-03-30 Intervet International B.V. Soft chewable pharmaceutical products
CN102659577B (zh) * 2012-04-07 2014-07-02 安徽绩溪县徽煌化工有限公司 一种亚甲基双羟基萘酸的制备方法
ES2792149T3 (es) 2012-09-19 2020-11-10 Alkermes Pharma Ireland Ltd Composiciones farmacéuticas que tienen estabilidad de almacenamiento mejorada
US9375433B2 (en) 2012-09-26 2016-06-28 Tangent Reprofiling Limited Modulators of androgen synthesis
BR112015006727B1 (pt) 2012-09-26 2022-08-16 Tangent Reprofiling Limited Uso de uma composição farmacêutica
MX2016012041A (es) 2014-03-20 2017-01-19 Alkermes Pharma Ireland Ltd Formulaciones de aripiprazol que tienen mayores velocidades de inyeccion.
CN106831594B (zh) * 2017-01-18 2018-02-02 力赛生物医药科技（厦门）有限公司 可乐定双羟萘酸盐及其制备方法
JP7384812B2 (ja) 2018-03-05 2023-11-21 アルカームス ファーマ アイルランド リミテッド アリピプラゾール投与戦略

Family Cites Families (1)

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US4804663A (en) * 1985-03-27 1989-02-14 Janssen Pharmaceutica N.V. 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles

Also Published As

Publication number Publication date
AU6721694A (en) 1994-11-21
US5612346A (en) 1997-03-18
DE69408666D1 (de) 1998-04-02
SI9420031B (sl) 2002-08-31
PL182466B1 (pl) 2002-01-31
PH30476A (en) 1997-05-28
ZA942909B (en) 1995-10-26
HU218212B (hu) 2000-06-28
CZ286688B6 (en) 2000-06-14
BG100094A (bg) 1996-05-31
CA2160366C (en) 2006-06-06
US5723467A (en) 1998-03-03
NZ266143A (en) 1996-07-26
DK0697019T3 (da) 1998-09-28
NO305083B1 (no) 1999-03-29
HU9501934D0 (en) 1995-09-28
ATE163418T1 (de) 1998-03-15
DE69408666T2 (de) 1998-06-18
HK1006059A1 (en) 1999-02-05
FI955166A0 (fi) 1995-10-27
CN1121719A (zh) 1996-05-01
NO954275L (no) 1995-10-26
BG62004B1 (bg) 1998-12-30
LV12315A (lv) 1999-07-20
CY2107B1 (en) 2002-04-26
SI9420031A (en) 1996-08-31
WO1994025460A1 (en) 1994-11-10
FI955166A (fi) 1995-10-27
JP3478397B2 (ja) 2003-12-15
JPH08509482A (ja) 1996-10-08
CA2160366A1 (en) 1994-11-10
HUT72970A (en) 1996-06-28
SK131395A3 (en) 1996-06-05
KR100307101B1 (ko) 2001-11-30
CZ270695A3 (en) 1996-01-17
PL311282A1 (en) 1996-02-05
FI109125B (fi) 2002-05-31
GR3026028T3 (en) 1998-04-30
CN1041727C (zh) 1999-01-20
IL109448A0 (en) 1994-07-31
ES2113652T3 (es) 1998-05-01
SK280589B6 (sk) 2000-04-10
IL109448A (en) 1997-03-18
RU2131428C1 (ru) 1999-06-10
EP0697019B1 (en) 1998-02-25
SG47046A1 (en) 1998-03-20
TW376319B (en) 1999-12-11
NO954275D0 (no) 1995-10-26
AU675136B2 (en) 1997-01-23
EP0697019A1 (en) 1996-02-21
LV12315B (en) 2000-03-20

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