KR930023338A - Depo formulation - Google Patents

Depo formulation Download PDF

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Publication number
KR930023338A
KR930023338A KR1019930007736A KR930007736A KR930023338A KR 930023338 A KR930023338 A KR 930023338A KR 1019930007736 A KR1019930007736 A KR 1019930007736A KR 930007736 A KR930007736 A KR 930007736A KR 930023338 A KR930023338 A KR 930023338A
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KR
South Korea
Prior art keywords
dibenz
pyrrole
tetrahydro
chloro
trans
Prior art date
Application number
KR1019930007736A
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Korean (ko)
Inventor
요하네스 마리아 반 덴 외텔라아르 페트러스
Original Assignee
에프. 지. 엠. 헤르만스, 에이. 지. 제이. 베르미렌
악조 엔. 브이
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Application filed by 에프. 지. 엠. 헤르만스, 에이. 지. 제이. 베르미렌, 악조 엔. 브이 filed Critical 에프. 지. 엠. 헤르만스, 에이. 지. 제이. 베르미렌
Publication of KR930023338A publication Critical patent/KR930023338A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

본 발명은 데포우제제로서 유용한 우수한 특성을 지닌 고-불용성 화합물인, 트랜스--클로로-2-메틸-2,3,3a,12b-테트라히드로-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤의 헤미파모에이트 및 파모에이트염에 관한 것이다. 또한, 결정형태의트랜스-5-클로로-2-메틸-2,3,3a,12b-테트라히드로-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤의 파모에이트염을 함유한 약학제제도 개시되어있다. 그러한 제제는 투여후 2 내지 6주동안 치료에 유용한 양의 트랜스-5-클로로-2-메틸-2,3,3a,12b-테트라히드로-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤이 방출된다.The present invention relates to trans-chloro-2-methyl-2,3,3a, 12b-tetrahydro-1H-dibenz [2,3; 6,7, which is a high-insoluble compound having excellent properties useful as a depot agent. ] Hemopamoate and pamoate salt of oxepino- [4,5-c] pyrrole. In addition, crystalline form of trans-5-chloro-2-methyl-2,3,3a, 12b-tetrahydro-1H-dibenz [2,3; 6,7] oxepino- [4,5-c] pyrrole Pharmaceuticals containing pamoate salts are also disclosed. Such agents are useful in therapeutic amounts of trans-5-chloro-2-methyl-2,3,3a, 12b-tetrahydro-1H-dibenz [2,3; 6,7] oxe for 2-6 weeks after administration. Pino- [4,5-c] pyrrole is released.

본발명은 또한 통상적으로 트랜스-5-클로로-2-메틸-2,3,3a,12b-테트라히드로The present invention is also commonly referred to as trans-5-chloro-2-methyl-2,3,3a, 12b-tetrahydro

-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤을 파모인산과 반응시킴으로써 파모에이트 또는 헤미파모에이트 염을 형성시키는, 약학제제를 제조하는 방법에 관한 것이기도 하다.To a pharmaceutical preparation, wherein a pamoate or hemipamoate salt is formed by reacting -1H-dibenz [2,3; 6,7] oxepine- [4,5-c] pyrrole with pamophosphoric acid It is also.

Description

데포우제제Depot agent

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (9)

트랜스-5-클로로-2-메틸-2,3,3a,12b-테트라히드로-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤의 파모에이트 또는 헤미파모에이트염.Pamoate or hemi of trans-5-chloro-2-methyl-2,3,3a, 12b-tetrahydro-1H-dibenz [2,3; 6,7] oxepino- [4,5-c] pyrrole Pamoate salt. 치료에 사용하기 위한 트랜스-5-클로로-2-메틸-2,3,3a,12b-테트라히드로-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤 파모에이트 또는 헤미파모에이트.Trans-5-chloro-2-methyl-2,3,3a, 12b-tetrahydro-1H-dibenz [2,3; 6,7] oxepino- [4,5-c] pyrrole for use in therapy Pamoate or hemipamoate. 데포우 약학 제제의 제제시 사용하기 위한 트랜스-5-클로로-2-메틸2,3,3a,12b-테트라히드로-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤 파모에이트.Trans-5-chloro-2-methyl2,3,3a, 12b-tetrahydro-1H-dibenz [2,3; 6,7] oxepino- [4,5 for use in the preparation of depot pharmaceutical formulations -c] pyrrole pamoate. 트랜스-5-클로로-2-메틸-2,3,3a,12b-테트라히드로-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤 파모에이트를 함유하는 테포우 약학제제.Containing trans-5-chloro-2-methyl-2,3,3a, 12b-tetrahydro-1H-dibenz [2,3; 6,7] oxepino- [4,5-c] pyrrole pamoate Tepo Pharmaceuticals. 제 4항에 있어서,트랜스-5-클로로-2-메틸-2,3,3a,12b-테트라히드로-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤 파모에이트가 결정형으로 존재하는 데포우 제제The method of claim 4, wherein trans-5-chloro-2-methyl-2,3,3a, 12b-tetrahydro-1H-dibenz [2,3; 6,7] oxepino- [4,5-c] Depot preparations in which pyrrole pamoate is present in crystalline form 항 정신질환 활성을 지닌 의약의 제조를 위해 트랜스-5-클로로-2-메틸-2,Trans-5-chloro-2-methyl-2, for the manufacture of a medicament with antipsychotic activity, 3,3a,12b-테트라히드로-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤 파모에이트 또는 헤미파모에이트를 사용하는 방법.3,3a, 12b-tetrahydro-1H-dibenz [2,3; 6,7] oxepino- [4,5-c] pyrrole pamoate or hemipamoate. 트랜스-5-클로로-2-메틸-2,3,3a,12b-테트라히드로-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤의 유리염기를 파모인산과 반응시키는 것을 특징으로 하는 트랜스-5-클로로-2-메틸-2,3,3a,12b-테트라히드로-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤의 파모에이트염 또는 헤미파모에이트염을 포함하는 약학제품을 제조하는 방법.Free base of trans-5-chloro-2-methyl-2,3,3a, 12b-tetrahydro-1H-dibenz [2,3; 6,7] oxepino- [4,5-c] pyrrole Trans-5-chloro-2-methyl-2,3,3a, 12b-tetrahydro-1H-dibenz [2,3; 6,7] oxepino- [4,5- characterized by reacting with the phosphoric acid c] A method for producing a pharmaceutical product comprising the pamoate salt or hemipamoate salt of pyrrole. 데포우 약학 제제의 제조시 사용하기 위한 트랜스-5-클로로-2-메틸-2,3,3a,Trans-5-chloro-2-methyl-2,3,3a, for use in the preparation of depot pharmaceutical formulations, 12b-테트라히드로-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤 헤미파모에이트.12b-tetrahydro-1H-dibenz [2,3; 6,7] oxepino- [4,5-c] pyrrole hemimomoate. 트랜스-5-클로로-2-메틸-2,3,3a,12b-테트라히드로-1H-디벤즈[2,3;6,7]옥세피노-[4,5-c] 피롤 헤미파모에이트를 함유하는 데포우 약학제제.Trans-5-chloro-2-methyl-2,3,3a, 12b-tetrahydro-1H-dibenz [2,3; 6,7] oxepino- [4,5-c] pyrrole hemimomoate Depo Pharmaceuticals. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019930007736A 1992-05-08 1993-05-06 Depo formulation KR930023338A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP92201319.8 1992-05-08
EP92201319 1992-05-08

Publications (1)

Publication Number Publication Date
KR930023338A true KR930023338A (en) 1993-12-18

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JP (1) JPH0656840A (en)
KR (1) KR930023338A (en)
AU (1) AU3846293A (en)
CA (1) CA2095499A1 (en)
FI (1) FI932088A (en)
MX (1) MX9302711A (en)
NO (1) NO931671L (en)
ZA (1) ZA933134B (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2139051C1 (en) * 1994-03-02 1999-10-10 Акцо Нобель Н.В. Sublingual or transbuccal pharmaceutical composition
EA002580B1 (en) * 1998-09-30 2002-06-27 Эли Лилли Энд Компани 2-methyl-thieno-benzodiazepine formulation
DE10041479A1 (en) * 2000-08-24 2002-03-14 Sanol Arznei Schwarz Gmbh New pharmaceutical composition for the administration of N-0923
GB0216416D0 (en) * 2002-07-15 2002-08-21 Novartis Ag Organic compounds
US6987111B2 (en) * 2003-08-06 2006-01-17 Alkermes Controlled Therapeutics, Ii Aripiprazole, olanzapine and haloperidol pamoate salts
US8658687B2 (en) * 2009-06-24 2014-02-25 Merck Sharp & Dohme Corp. Injectable formulations containing asenapine and method of treatment using same
JP2021014404A (en) * 2017-10-13 2021-02-12 アステラス製薬株式会社 Triazolopyrazine derivative salt and crystal

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ZA933134B (en) 1993-11-30
AU3846293A (en) 1993-11-11
JPH0656840A (en) 1994-03-01
NO931671D0 (en) 1993-05-07
FI932088A (en) 1993-11-09
FI932088A0 (en) 1993-05-07
CA2095499A1 (en) 1993-11-09
NO931671L (en) 1993-11-09
MX9302711A (en) 1994-05-31

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