CN101155804B - 用于治疗精神疾病的哌嗪取代的苯并噻吩 - Google Patents

用于治疗精神疾病的哌嗪取代的苯并噻吩 Download PDF

Info

Publication number
CN101155804B
CN101155804B CN2006800119230A CN200680011923A CN101155804B CN 101155804 B CN101155804 B CN 101155804B CN 2006800119230 A CN2006800119230 A CN 2006800119230A CN 200680011923 A CN200680011923 A CN 200680011923A CN 101155804 B CN101155804 B CN 101155804B
Authority
CN
China
Prior art keywords
alkyl
group
benzo
thiophen
piperazin
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN2006800119230A
Other languages
English (en)
Chinese (zh)
Other versions
CN101155804A (zh
Inventor
山下博司
松原淳
大岛邦生
黑田英明
伊藤展明
宫村伸
清水聪
田中达义
高桥永
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Otsuka Pharmaceutical Co Ltd
Original Assignee
Otsuka Pharmaceutical Co Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36645750&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN101155804(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Otsuka Pharmaceutical Co Ltd filed Critical Otsuka Pharmaceutical Co Ltd
Publication of CN101155804A publication Critical patent/CN101155804A/zh
Application granted granted Critical
Publication of CN101155804B publication Critical patent/CN101155804B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN2006800119230A 2005-04-14 2006-04-12 用于治疗精神疾病的哌嗪取代的苯并噻吩 Active CN101155804B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2005116698 2005-04-14
JP116698/2005 2005-04-14
PCT/JP2006/308162 WO2006112464A1 (en) 2005-04-14 2006-04-12 Piperazine-substituted benzothiophenes for treatment of mental disorders

Publications (2)

Publication Number Publication Date
CN101155804A CN101155804A (zh) 2008-04-02
CN101155804B true CN101155804B (zh) 2013-03-27

Family

ID=36645750

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2006800119230A Active CN101155804B (zh) 2005-04-14 2006-04-12 用于治疗精神疾病的哌嗪取代的苯并噻吩

Country Status (26)

Country Link
US (14) USRE48059E1 (enExample)
EP (1) EP1869025B3 (enExample)
KR (1) KR100937623B1 (enExample)
CN (1) CN101155804B (enExample)
AR (1) AR053577A1 (enExample)
AT (1) ATE496911T3 (enExample)
AU (1) AU2006237905C1 (enExample)
BR (1) BRPI0609785B8 (enExample)
CA (1) CA2602247C (enExample)
CY (2) CY1111206T1 (enExample)
DE (1) DE602006019838D1 (enExample)
DK (1) DK1869025T6 (enExample)
ES (1) ES2358631T7 (enExample)
HU (2) HUE011611T6 (enExample)
IL (1) IL185909A (enExample)
IN (1) IN2012DN00855A (enExample)
LT (1) LTC1869025I2 (enExample)
LU (1) LUC00086I2 (enExample)
MY (1) MY142746A (enExample)
NL (1) NL300946I2 (enExample)
PL (1) PL1869025T6 (enExample)
PT (1) PT1869025E (enExample)
SI (1) SI1869025T1 (enExample)
TW (1) TWI320783B (enExample)
WO (1) WO2006112464A1 (enExample)
ZA (1) ZA200708686B (enExample)

Families Citing this family (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0412263B1 (pt) 2003-07-22 2019-10-15 Arena Pharmaceuticals, Inc. Derivados de diaril e aril heteroaril uréia, uso e composição farmacêutica contendo os mesmos, bem como processo para preparação da dita composição
PE20061130A1 (es) 2004-11-19 2007-01-05 Arena Pharm Inc Derivados de 3-fenil-pirazol como moduladores del receptor de serotonina 5-ht2a
TWI320783B (en) 2005-04-14 2010-02-21 Otsuka Pharma Co Ltd Heterocyclic compound
EP2527329A1 (en) 2006-05-18 2012-11-28 Arena Pharmaceuticals, Inc. Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-ht2a serotonin receptor
USRE45337E1 (en) 2006-05-18 2015-01-13 Arena Pharmaceuticals, Inc. Ethers, secondary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
EP2018371B1 (en) 2006-05-18 2015-03-04 Arena Pharmaceuticals, Inc. Primary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
TWI415845B (zh) 2006-10-03 2013-11-21 Arena Pharm Inc 用於治療與5-ht2a血清素受體相關聯病症之作為5-ht2a血清素受體之調節劑的吡唑衍生物
WO2008047883A1 (en) * 2006-10-13 2008-04-24 Otsuka Pharmaceutical Co., Ltd. Piperazine-substituted benzothiophenes for treatment of mental disorders
US20080186971A1 (en) * 2007-02-02 2008-08-07 Tarari, Inc. Systems and methods for processing access control lists (acls) in network switches using regular expression matching logic
JP5393677B2 (ja) 2007-08-15 2014-01-22 アリーナ ファーマシューティカルズ, インコーポレイテッド 5−HT2Aセロトニン受容体に関連した障害の治療のための5−HT2Aセロトニン受容体のモジュレーターとしてのイミダゾ[1,2−a]ピリジン誘導体
BRPI0908807A2 (pt) * 2008-02-15 2015-07-28 Hoffmann La Roche Derivados de 3-alquil-piperazina e usos dos mesmos
PL2254887T3 (pl) 2008-02-22 2013-05-31 Actelion Pharmaceuticals Ltd Pochodne oksazolidynonu
US20110021538A1 (en) 2008-04-02 2011-01-27 Arena Pharmaceuticals, Inc. Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor
US9126946B2 (en) 2008-10-28 2015-09-08 Arena Pharmaceuticals, Inc. Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto
US9034911B2 (en) 2008-10-28 2015-05-19 Arena Pharmaceuticals, Inc. Composition of a 5-HT2A serotonin receptor modulator useful for the treatment of disorders related thereto
SMT201700430T1 (it) 2009-06-25 2018-01-11 Alkermes Pharma Ireland Ltd Composti eterociclici per il trattamento di disturbi neurologici e psicologici
US8980891B2 (en) 2009-12-18 2015-03-17 Arena Pharmaceuticals, Inc. Crystalline forms of certain 3-phenyl-pyrazole derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
US8536328B2 (en) 2010-05-04 2013-09-17 Alkermes Pharma Ireland Limited Process for synthesizing oxidized lactam compounds
CA2802733C (en) 2010-06-24 2017-11-21 Alkermes Pharma Ireland Limited Prodrugs of nh-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives
JOP20120083B1 (ar) 2011-04-05 2021-08-17 Otsuka Pharma Co Ltd توليفات تشتمل على بريكس ببرازول أو ملح منه وعقار ثاني للاستخدام في علاج اضطراب cns
JP5832558B2 (ja) 2011-07-28 2015-12-16 大塚製薬株式会社 ベンゾ[b]チオフェン化合物の製造方法
JO3227B1 (ar) * 2011-09-08 2018-03-08 Otsuka Pharma Co Ltd مشتقات بنزو ثيوفين بها استبدال ببرازين كعوامل مضادة للذهان
JO3753B1 (ar) 2011-10-14 2021-01-31 Otsuka Pharma Co Ltd قرص يتألف من 7-[4-(4-بينزو[بي]ثيوفين-4-ايل-ببرازين-1-1ايل)بوتكسيل]-1اتش-كوينولين-2-وان أو ملح منه
TWI679977B (zh) 2011-10-19 2019-12-21 大塚製藥股份有限公司 口服溶液
TW201332572A (zh) * 2011-12-28 2013-08-16 Otsuka Pharma Co Ltd 具有經取代的β-環糊精之藥物製劑
TWI562991B (en) * 2012-04-23 2016-12-21 Otsuka Pharma Co Ltd Dihydrate of benzothiophene compound or of a salt thereof, and process for producing the same
JOP20200109A1 (ar) 2012-04-23 2017-06-16 Otsuka Pharma Co Ltd مستحضر قابل للحقن
AR090775A1 (es) * 2012-04-23 2014-12-03 Otsuka Pharma Co Ltd Preparado inyectable
AU2013259551B2 (en) * 2012-05-09 2017-11-02 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
JOP20210047A1 (ar) 2012-10-25 2017-06-16 Otsuka Pharma Co Ltd عامل وقائي و/أو علاجي للأعراض السلوكية والنفسية المصحوبة بمرض تنكسي عصبي أو الأعراض الإندفاعية المصحوبة بمرض ذهني، يحتوي على بريكسبيرازول أو ملحه
EP2792359A1 (en) * 2013-04-19 2014-10-22 Merz Pharma GmbH & Co. KGaA Treatment of L-DOPA-induced dyskinesia with OPC-14523 or OPC-34712
KR101472916B1 (ko) * 2013-06-27 2014-12-16 한국과학기술연구원 모르폴린 또는 피페라진 화합물, 및 도네페질을 포함하는 인지 장애 관련 질병의 예방 또는 치료용 약학적 조성물
CN104557896A (zh) * 2013-10-18 2015-04-29 沈敬山 布瑞哌唑、其关键中间体及其盐的制备方法
CN104892589A (zh) * 2014-03-07 2015-09-09 中国科学院上海药物研究所 一类杂环化合物、其制备方法和用途
JP6797691B2 (ja) 2014-04-22 2020-12-09 大塚製薬株式会社 ブレクスピプラゾールとナルメフェンの組み合わせ剤及び物質関連障害を治療するためのその用途
CN104447723A (zh) * 2014-11-28 2015-03-25 瑞阳制药有限公司 7-(4-(4-(苯并[b]噻吩基)-1-哌嗪基)丁氧基)-2(1H)-喹啉酮的制备方法
CN105461703B (zh) * 2014-12-29 2019-05-17 深圳市泛谷药业股份有限公司 一种brexpiprazole的制备方法
CN105985314A (zh) * 2015-02-05 2016-10-05 苏州旺山旺水生物医药有限公司 布瑞哌唑类似物的制备方法
CN104844586A (zh) * 2015-04-16 2015-08-19 重庆医药工业研究院有限责任公司 一种依匹哌唑无定型物及其制备方法
CN104829588B (zh) * 2015-04-30 2017-03-29 苏州苏旺森生物医药科技有限公司 一种苯并[b]噻吩的制备方法及其中间体
CN104829603A (zh) * 2015-05-19 2015-08-12 杭州新博思生物医药有限公司 A晶型依匹唑派盐酸盐及其制备方法
WO2016201373A1 (en) 2015-06-12 2016-12-15 Axovant Sciences Ltd. Diaryl and arylheteroaryl urea derivatives useful for the prophylaxis and treatment of rem sleep behavior disorder
CA2992518A1 (en) 2015-07-15 2017-01-19 Axovant Sciences Gmbh Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of hallucinations associated with a neurodegenerative disease
CN105061414B (zh) * 2015-07-21 2019-01-01 杭州新博思生物医药有限公司 一锅法制备Brexpiprazole
WO2017025987A1 (en) 2015-08-11 2017-02-16 Mylan Laboratories Limited Process for the preparation of brexpiprazole
EP3150591A1 (en) 2015-10-02 2017-04-05 Crystal Pharma S.A.U Process and intermediates for the preparation of benzo[b]thiophene compounds
CN106749219A (zh) * 2015-11-20 2017-05-31 江苏恩华药业股份有限公司 一种内酰胺类衍生物及其应用
CN105440026A (zh) * 2015-12-04 2016-03-30 上海勋和医药科技有限公司 依匹哌唑的制备方法
CN105461704A (zh) * 2015-12-15 2016-04-06 南京艾德凯腾生物医药有限责任公司 一种依匹哌唑的制备方法
WO2017106641A1 (en) 2015-12-17 2017-06-22 Assia Chemical Industries Ltd. Solid state forms of brexpiprazole
CN106916148B (zh) * 2015-12-25 2021-07-06 上海科胜药物研发有限公司 一种合成依匹哌唑的方法
WO2017115287A1 (en) * 2015-12-28 2017-07-06 Honour (R&D) Process for the preparation of quinoline-2(1h)-one derivatives
CN106938982A (zh) * 2016-01-05 2017-07-11 连云港皓海医药科技有限公司 布瑞哌唑的制备方法及用于制备布瑞哌唑的化合物
CN105399736B (zh) * 2016-01-07 2018-10-19 安徽省逸欣铭医药科技有限公司 一种依匹哌唑新的制备方法
US10501450B2 (en) 2016-02-01 2019-12-10 Hexal Ag Anhydrate-free polymorphically pure micronized crystalline brexpiprazole di-hydrate for use in intramuscular injectable sustained release formulations
CN105541819B (zh) * 2016-02-04 2018-09-14 浙江永宁药业股份有限公司 一种依匹唑派的制备方法及其中间体和中间体的制备方法
US20170320862A1 (en) 2016-05-03 2017-11-09 Cadila Healthcare Limited Process for the preparation of brexpiprazole and intermediates thereof
CN107365305A (zh) 2016-05-12 2017-11-21 上海奥博生物医药技术有限公司 一种依匹哌唑新晶型及其制备方法
WO2017208251A1 (en) * 2016-05-31 2017-12-07 Cipla Limited A new stable polymorph of brexpiprazole and process for preparation thereof
WO2017216661A1 (en) 2016-06-17 2017-12-21 Jubilant Generics Limited Process for the preparation of brexpiprazole from 7-(4-chlorobutoxy)quinolin-2(1h)-one and 1-(benzo[b]thiophen-4-yl)piperazine
US10034861B2 (en) 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
PL233778B1 (pl) 2016-07-19 2019-11-29 Adamed Spolka Z Ograniczona Odpowiedzialnoscia Sposob wytwarzania brekspiprazolu oraz zastosowanie zwiazkow posrednich w sposobie wytwarzania brekspiprazolu
WO2018033484A1 (en) 2016-08-16 2018-02-22 Hexal Aktiengesellschaft Pharmaceutical compositions of a benzothiophene compound
US11123300B2 (en) 2016-08-16 2021-09-21 Hexal Ag Immediate release tablet of a benzothiophene compound
WO2018060916A1 (en) * 2016-09-28 2018-04-05 Alembic Pharmaceuticals Limited Process for the preparation of brexpiprazole and intermediates thereof
CN107936005A (zh) * 2016-10-13 2018-04-20 上海科胜药物研发有限公司 一种依匹哌唑新晶型ii及其制备方法
WO2018087775A1 (en) * 2016-11-09 2018-05-17 Msn Laboratories Private Limited, R&D Center Processes for the preparation of 7-{4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy}quinolin-2(1h)-one
CN111233848A (zh) * 2016-12-14 2020-06-05 上海博志研新药物技术有限公司 一种依匹哌唑甲醇合物、晶型a、及其制备方法和应用
WO2018141886A1 (en) 2017-02-02 2018-08-09 Hexal Aktiengesellschaft Crystalline brexpiprazole
WO2018172463A1 (en) 2017-03-22 2018-09-27 Amneal Pharmaceuticals Company Gmbh Process for the preparation of brexpiprazole
WO2019073481A1 (en) * 2017-10-12 2019-04-18 Indoco Remedies Limited PROCESS FOR THE PREPARATION OF BREXPIPRAZOLE AND ITS INTERMEDIATES
HRP20211784T1 (hr) 2017-12-14 2022-02-18 H. Lundbeck A/S Kombinacijski tretmani koji se sastoje od primjene 1h-pirazolo[4,3-b]piridina
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
EP3501506B1 (en) 2017-12-19 2019-10-09 Alfred E. Tiefenbacher (GmbH & Co. KG) Pharmaceutical tablet composition comprising brexpiprazole
CN117447475A (zh) 2017-12-20 2024-01-26 H.隆德贝克有限公司 作为PDE1抑制剂的吡唑并[4,3-b]吡啶和咪唑并[1,5-a]嘧啶
CN109988162A (zh) * 2017-12-29 2019-07-09 武汉兴华智慧医药科技有限公司 一种依匹哌唑衍生物及其制备方法
EP3545950A1 (en) 2018-03-26 2019-10-02 Adamed sp. z o.o. Pharmaceutical composition comprising brexpiprazole
WO2019242717A1 (zh) * 2018-06-21 2019-12-26 中国科学院上海药物研究所 一种苯并噻吩化合物的马来酸盐、其结晶形式及其用途
CN108947990A (zh) * 2018-07-20 2018-12-07 成都苑东生物制药股份有限公司 一种苯并噻吩类化合物的制备方法
WO2020087031A1 (en) 2018-10-26 2020-04-30 The Research Foundation For The State University Of New York Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia
CN111320582A (zh) * 2018-12-17 2020-06-23 江苏恩华药业股份有限公司 一种类酰胺类衍生物及其中间体的制备方法
CN111320619A (zh) * 2018-12-17 2020-06-23 江苏恩华药业股份有限公司 一种类酰胺类衍生物的杂质及用途
CN109970705B (zh) * 2019-05-14 2021-02-09 浙江工业大学 一种应用廉价金属铜制备依匹哌唑中间体及依匹哌唑的方法
WO2021029020A1 (ja) * 2019-08-13 2021-02-18 大塚製薬株式会社 経口医薬組成物
EP4132646A1 (en) * 2020-04-08 2023-02-15 Remix Therapeutics Inc. Compounds and methods for modulating splicing
CN116096715A (zh) * 2020-07-06 2023-05-09 泰科根公司 用于精神障碍或精神增强的有益苯并噻吩组合物
US11229644B1 (en) * 2020-12-31 2022-01-25 Lake O'hara Llc Methods of treating psychiatric disorders in obese patients with brexpiprazole
CN117769545A (zh) * 2021-08-05 2024-03-26 上海枢境生物科技有限公司 含三并环类衍生物调节剂、其制备方法和应用
CN115772175A (zh) * 2021-09-07 2023-03-10 中国科学院分子细胞科学卓越创新中心 噻吩并环化合物及其制备方法和应用
CN114181202A (zh) * 2021-12-17 2022-03-15 湖南省湘中制药有限公司 一种依匹哌唑的制备方法
CN118580229B (zh) * 2024-08-07 2024-12-27 湖南一格制药有限公司 布瑞哌唑的制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1139108A (zh) * 1995-03-17 1997-01-01 赫彻斯特马里恩鲁斯公司 取代苯并噻吩基哌嗪、作为药物的用途及其制备方法
CN1154105A (zh) * 1994-06-08 1997-07-09 H·隆德贝克有限公司 4-芳基-1-(二氢化茚甲基、二氢苯并呋喃甲基或二氢苯并噻吩甲基)哌啶、-四氢吡啶或哌嗪类化合物

Family Cites Families (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3910955A (en) 1970-12-21 1975-10-07 Aspro Nicholas Ltd Benzothiophene-ethylamines
DK574274A (enExample) 1973-12-06 1975-07-28 Ciba Geigy Ag
JPS54130587A (en) 1978-03-30 1979-10-09 Otsuka Pharmaceut Co Ltd Carbostyryl derivative
EP0005828B1 (de) 1978-06-06 1981-03-11 Hoechst Aktiengesellschaft Neue substituierte Phenylpiperazinderivate, diese enthaltende Arzneimittel und Verfahren zu deren Herstellung
DE2827566A1 (de) 1978-06-23 1980-01-10 Boehringer Mannheim Gmbh 1,2-dihydro-chinolin-2-on-derivate und verfahren zu ihrer herstellung
JPS5646812A (en) 1979-09-27 1981-04-28 Otsuka Pharmaceut Co Ltd Central nervous system depressant
JPS5649361A (en) 1979-09-28 1981-05-02 Otsuka Pharmaceut Co Ltd Carbostyril derivative
PH17194A (en) 1980-03-06 1984-06-19 Otsuka Pharma Co Ltd Novel carbostyril derivatives,and pharmaceutical composition containing the same
JPS56164186A (en) 1980-05-21 1981-12-17 Otsuka Pharmaceut Co Ltd Carbostyril derivative
IT1201087B (it) 1982-04-15 1989-01-27 Gentili Ist Spa Bifosfonati farmacologicamente attivi,procedimento per la loro preparazione e relative composizioni farmaceutiche
ATE81975T1 (de) 1984-12-21 1992-11-15 Duphar Int Res Arzneimittel mit psychotroper wirkung.
US4704390A (en) 1986-02-13 1987-11-03 Warner-Lambert Company Phenyl and heterocyclic tetrahydropyridyl alkoxy-benzheterocyclic compounds as antipsychotic agents
GB8704572D0 (en) 1987-02-26 1987-04-01 Lundbeck & Co As H Organic compounds
US4883795A (en) 1988-01-22 1989-11-28 Pfizer Inc. Piperazinyl-heterocyclic compounds
US4831031A (en) 1988-01-22 1989-05-16 Pfizer Inc. Aryl piperazinyl-(C2 or C4) alkylene heterocyclic compounds having neuroleptic activity
US5006528A (en) 1988-10-31 1991-04-09 Otsuka Pharmaceutical Co., Ltd. Carbostyril derivatives
WO1991000863A1 (en) 1989-07-07 1991-01-24 Pfizer Inc. Heteroaryl piperazine antipsychotic agents
CA2067475C (en) 1991-05-08 2000-10-10 Yasuo Oshiro Carbostyril derivatives and their use
US5436246A (en) * 1992-09-17 1995-07-25 Merrell Dow Pharmaceuticals Inc. Serotonin receptor agents
DK148392D0 (da) 1992-12-09 1992-12-09 Lundbeck & Co As H Heterocykliske forbindelser
US5506248A (en) 1993-08-02 1996-04-09 Bristol-Myers Squibb Company Pharmaceutical compositions having good dissolution properties
CA2157348A1 (en) 1994-09-01 1996-03-02 Aventis Pharmaceuticals Inc. 3-¬4-(1-substituted-4-piperazinyl)butyl|-4-thiazolidinone and related compounds
US5576321A (en) 1995-01-17 1996-11-19 Eli Lilly And Company Compounds having effects on serotonin-related systems
CR5278A (es) 1995-03-24 1996-07-04 Lilly Co Eli Formulacion oral de 2-metil-tieno-benzodiacepina
FR2735127B1 (fr) 1995-06-09 1997-08-22 Pf Medicament Nouvelles piperazines heteroaromatiques utiles comme medicaments.
EE04116B1 (et) 1995-09-15 2003-08-15 Synthlabo Kinolin-2(1H)-ooni derivaadid kui serotoniini antagonistid
AU6859096A (en) 1995-09-22 1997-04-09 Warner-Lambert Company Substituted cyclohexylamines as central nervous system agents
AU708053B2 (en) 1996-03-29 1999-07-29 Duphar International Research B.V. Piperazine and piperidine compounds
US5846982A (en) 1996-06-14 1998-12-08 Eli Lilly And Company Inhibition of serotonin reuptake
EP0934932A4 (en) 1996-08-22 2002-06-26 Meiji Seika Kaisha CHINOLINE DERIVATIVES AND PSYCHOTROPES MEDIUM
FR2761068B1 (fr) 1997-03-20 1999-04-23 Synthelabo Derives de piperazin-4-ylthieno[3,2-c]pyridin-4-yl-2- carboxamide, leur preparation et leur application en therapeutique
ES2128266B1 (es) 1997-07-08 2000-01-16 Vita Invest Sa Compuestos derivados de tiofeno y benzotiofeno y utilizacion y composicion correspondientes.
DE69819266T2 (de) 1997-09-02 2004-07-29 Duphar International Research B.V. Piperidin- und Piperazin Derivate als 5-HT1-Rezeptor-Agonisten
EP0901787B1 (en) 1997-09-10 2003-05-28 Takeda Chemical Industries, Ltd. Stabilized pharmaceutical composition
ATE225345T1 (de) 1998-06-30 2002-10-15 Lilly Co Eli Auf serotonin-verwandte systeme wirkende piperidin-derivate
AR022303A1 (es) 1999-01-22 2002-09-04 Lundbeck & Co As H Derivados de piperidina, tetrahidropiridina y piperazina, su preparacion y utilizacion
CN1164574C (zh) 1999-05-24 2004-09-01 三菱制药株式会社 苯氧基丙胺类化合物
WO2001009126A1 (en) 1999-07-29 2001-02-08 Eli Lilly And Company Serotonergic benzothiophenes
US6562375B1 (en) 1999-08-04 2003-05-13 Yamanouchi Pharmaceuticals, Co., Ltd. Stable pharmaceutical composition for oral use
AU2251801A (en) 1999-12-20 2001-07-03 Eli Lilly And Company Piperidine derivatives and their use as serotonin receptor antagonists
AR027133A1 (es) 1999-12-30 2003-03-12 Lundbeck & Co As H Derivados de heteroarilo, su preparacion y uso.
WO2003030868A1 (en) 2001-10-09 2003-04-17 Bristol-Myers Squibb Company Flashmelt oral dosage formulation
DE10043659A1 (de) 2000-09-05 2002-03-14 Merck Patent Gmbh Arylpiperazinderivate
ES2188344B1 (es) 2000-11-29 2004-09-16 Laboratorios Vita, S.A. Compuestos derivados de benzotiofeno, su procedimiento de obtencion y utilizacion de los mismos.
US7053092B2 (en) 2001-01-29 2006-05-30 Otsuka Pharmaceutical Co., Ltd. 5-HT1a receptor subtype agonist
IL157412A0 (en) 2001-02-16 2004-03-28 Aventis Pharmaceuticals Inc Av Novel heterocyclic amide derivatives and their use as dopamine d3 receptor ligands
JP4310605B2 (ja) 2001-05-25 2009-08-12 大塚製薬株式会社 医薬用組成物
AR033485A1 (es) 2001-09-25 2003-12-26 Otsuka Pharma Co Ltd Sustancia medicinal de aripiprazol de baja higroscopicidad y proceso para la preparacion de la misma
DE10151569A1 (de) 2001-10-23 2003-04-30 Basf Ag Thermisch härtbare Bindemittel
WO2003055467A1 (en) 2001-12-18 2003-07-10 Synthon B.V. Simvastatin dosage forms
MXPA05002007A (es) 2002-09-17 2005-04-28 Warner Lambert Co Piperazinas heterociclicas sustituidas para el tratamiento de la esquizofrenia.
WO2004029948A1 (de) 2002-09-20 2004-04-08 Osram Opto Semiconductors Gmbh Optischer abtastkopf und verfahren zur herstellung desselben
BR0314796A (pt) 2002-09-26 2005-07-26 Warner Lambert Co Piperazinas substituìdas heterocìclicas para o tratamento de esquizofrenia
WO2004060374A1 (en) 2002-12-27 2004-07-22 Otsuka Pharmaceutical Co., Ltd. Carbostyril derivatives and serotonin reuptake inhibitors for treatment of mood disorders
BRPI0305500B1 (pt) 2003-01-09 2018-01-23 Otsuka Pharmaceutical Co., Ltd. Processo para preparar aripiprazol
CA2523831C (en) 2003-04-29 2008-11-18 Pfizer Inc. 5,7-diaminopyrazolo[4,3-d]pyrimidines useful in the treatment of hypertension
CN102000336A (zh) 2003-05-23 2011-04-06 大塚制药株式会社 用于治疗情感障碍的喹诺酮衍生物和情绪稳定剂
US7160888B2 (en) * 2003-08-22 2007-01-09 Warner Lambert Company Llc [1,8]naphthyridin-2-ones and related compounds for the treatment of schizophrenia
GB0504203D0 (en) 2005-03-01 2005-04-06 Novartis Ag Organic compounds
EP1858514B1 (en) 2005-03-17 2014-11-26 Synthon B.V. Pharmaceutical tablets of crystalline type ii aripiprazole
TWI320783B (en) * 2005-04-14 2010-02-21 Otsuka Pharma Co Ltd Heterocyclic compound
UA97349C2 (uk) 2005-09-08 2012-02-10 Х. Луннбэк А/С Стійкі тверді склади сертиндолу
ATE419837T1 (de) 2006-01-05 2009-01-15 Teva Pharma Feuchtgranulierungsmethode zur herstellung pharmazeutischer aripiprazolzusammensetzungen
EP2156833B1 (en) 2007-05-11 2011-11-30 Santen Pharmaceutical Co., Ltd Prophylactic or therapeutic agent for posterior ocular disease comprising non-ergot selective d2 receptor agonist as active ingredient
US7968431B2 (en) 2008-07-15 2011-06-28 Taiwan Semiconductor Manufacturing Company, Ltd. Diffusion region routing for narrow scribe-line devices
WO2010052727A1 (en) 2008-11-04 2010-05-14 Ideal Cures Private Limited High performance film coating compositions
JP5832558B2 (ja) * 2011-07-28 2015-12-16 大塚製薬株式会社 ベンゾ[b]チオフェン化合物の製造方法
JO3227B1 (ar) * 2011-09-08 2018-03-08 Otsuka Pharma Co Ltd مشتقات بنزو ثيوفين بها استبدال ببرازين كعوامل مضادة للذهان
JO3753B1 (ar) 2011-10-14 2021-01-31 Otsuka Pharma Co Ltd قرص يتألف من 7-[4-(4-بينزو[بي]ثيوفين-4-ايل-ببرازين-1-1ايل)بوتكسيل]-1اتش-كوينولين-2-وان أو ملح منه
TWI562991B (en) * 2012-04-23 2016-12-21 Otsuka Pharma Co Ltd Dihydrate of benzothiophene compound or of a salt thereof, and process for producing the same

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1154105A (zh) * 1994-06-08 1997-07-09 H·隆德贝克有限公司 4-芳基-1-(二氢化茚甲基、二氢苯并呋喃甲基或二氢苯并噻吩甲基)哌啶、-四氢吡啶或哌嗪类化合物
CN1139108A (zh) * 1995-03-17 1997-01-01 赫彻斯特马里恩鲁斯公司 取代苯并噻吩基哌嗪、作为药物的用途及其制备方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CN 1139108 A,说明书1-30页.

Also Published As

Publication number Publication date
US20110152286A1 (en) 2011-06-23
US20140163039A1 (en) 2014-06-12
MY142746A (en) 2010-12-31
US20180214444A1 (en) 2018-08-02
CA2602247C (en) 2013-04-02
TWI320783B (en) 2010-02-21
DE602006019838D1 (de) 2011-03-10
US20160051548A1 (en) 2016-02-25
US9206167B2 (en) 2015-12-08
US8618109B2 (en) 2013-12-31
AU2006237905B2 (en) 2009-09-03
US9480686B2 (en) 2016-11-01
IN2012DN00855A (enExample) 2015-07-10
AU2006237905C1 (en) 2015-11-19
ZA200708686B (en) 2009-01-28
HK1112236A1 (en) 2008-08-29
US20190117648A1 (en) 2019-04-25
US7888362B2 (en) 2011-02-15
ATE496911T3 (de) 2011-02-15
LUC00086I2 (enExample) 2018-11-26
US20190321359A1 (en) 2019-10-24
LTPA2018509I1 (lt) 2018-09-10
BRPI0609785A2 (pt) 2010-04-27
USRE48059E1 (en) 2020-06-23
AR053577A1 (es) 2007-05-09
SI1869025T1 (sl) 2011-04-29
US20170368060A1 (en) 2017-12-28
KR100937623B1 (ko) 2010-01-20
NL300946I2 (nl) 2018-09-26
PT1869025E (pt) 2011-02-04
US20170231983A1 (en) 2017-08-17
EP1869025B3 (en) 2016-08-31
EP1869025A1 (en) 2007-12-26
HUE011611T6 (en) 2017-04-28
PL1869025T6 (pl) 2017-10-31
CY1111206T1 (el) 2015-06-11
CY2018028I1 (el) 2019-07-10
CN101155804A (zh) 2008-04-02
EP1869025B1 (en) 2011-01-26
DK1869025T3 (da) 2011-04-04
IL185909A (en) 2014-08-31
BRPI0609785B8 (pt) 2021-05-25
US20200237755A1 (en) 2020-07-30
KR20080002817A (ko) 2008-01-04
US8349840B2 (en) 2013-01-08
CY2018028I2 (el) 2019-07-10
US20100179322A1 (en) 2010-07-15
WO2006112464A1 (en) 2006-10-26
LTC1869025I2 (lt) 2019-05-10
ES2358631T3 (es) 2011-05-12
US9839637B1 (en) 2017-12-12
IL185909A0 (en) 2008-01-06
TW200716619A (en) 2007-05-01
HUS1800041I1 (hu) 2018-11-28
PL1869025T3 (pl) 2011-06-30
US20170000786A1 (en) 2017-01-05
US20130158044A1 (en) 2013-06-20
US20210113556A1 (en) 2021-04-22
BRPI0609785B1 (pt) 2020-10-20
DK1869025T6 (da) 2017-01-02
ES2358631T7 (es) 2016-11-17
CA2602247A1 (en) 2006-10-26
AU2006237905A1 (en) 2006-10-26

Similar Documents

Publication Publication Date Title
CN101155804B (zh) 用于治疗精神疾病的哌嗪取代的苯并噻吩
JP4540700B2 (ja) 医薬
JP4315393B2 (ja) 複素環化合物
CN101258147B (zh) 用于治疗cns疾病的4-哌嗪-1-基-4-苯并[b]噻吩衍生物
RU2402549C2 (ru) Пиперазин-замещенные бензотиофены для лечения психических расстройств
HK1112236B (en) Piperazine-substituted benzothiophenes for treatment of mental disorders
MX2007012626A (es) Benzotiofenos sustituidos con piperazina para el tratamiento de trastornos mentales.

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1112236

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1112236

Country of ref document: HK