CN1805939B - 用于治疗5ht2c受体相关病症的苯并氮杂卓衍生物 - Google Patents

用于治疗5ht2c受体相关病症的苯并氮杂卓衍生物 Download PDF

Info

Publication number
CN1805939B
CN1805939B CN2004800167803A CN200480016780A CN1805939B CN 1805939 B CN1805939 B CN 1805939B CN 2004800167803 A CN2004800167803 A CN 2004800167803A CN 200480016780 A CN200480016780 A CN 200480016780A CN 1805939 B CN1805939 B CN 1805939B
Authority
CN
China
Prior art keywords
alkyl
compound
haloalkyl
formula
halogen
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.)
Expired - Lifetime
Application number
CN2004800167803A
Other languages
English (en)
Chinese (zh)
Other versions
CN1805939A (zh
Inventor
贝弗利·W·布尔鲍姆
查尔斯三世·A·吉尔森
谢利·奥伊特斯
斯科特·A·埃斯特拉达
迪帕简·森古普塔
布莱恩·史密斯
马克斯·雷伊
乌尔里希·魏格尔
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.)
Eisai Co Ltd
Original Assignee
Arena Pharmaceuticals Inc
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 Arena Pharmaceuticals Inc filed Critical Arena Pharmaceuticals Inc
Priority claimed from PCT/US2004/019279 external-priority patent/WO2005019179A2/en
Publication of CN1805939A publication Critical patent/CN1805939A/zh
Application granted granted Critical
Publication of CN1805939B publication Critical patent/CN1805939B/zh
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs 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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
CN2004800167803A 2003-06-17 2004-06-16 用于治疗5ht2c受体相关病症的苯并氮杂卓衍生物 Expired - Lifetime CN1805939B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US47928003P 2003-06-17 2003-06-17
US60/479,280 2003-06-17
US51296703P 2003-10-21 2003-10-21
US60/512,967 2003-10-21
PCT/US2004/019279 WO2005019179A2 (en) 2003-06-17 2004-06-16 Benzazepine derivatives useful for the treatment of 5ht2c receptor associated diseases

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN2008100073149A Division CN101274911B (zh) 2003-06-17 2004-06-16 用于治疗5ht2c受体相关病症的苯并氮杂卓衍生物

Publications (2)

Publication Number Publication Date
CN1805939A CN1805939A (zh) 2006-07-19
CN1805939B true CN1805939B (zh) 2010-10-13

Family

ID=33563791

Family Applications (4)

Application Number Title Priority Date Filing Date
CN2004800167803A Expired - Lifetime CN1805939B (zh) 2003-06-17 2004-06-16 用于治疗5ht2c受体相关病症的苯并氮杂卓衍生物
CN2004800167733A Expired - Fee Related CN1805938B (zh) 2003-06-17 2004-06-16 用于治疗5ht2c受体相关疾病的苯并氮杂卓衍生物
CN2008100073149A Expired - Fee Related CN101274911B (zh) 2003-06-17 2004-06-16 用于治疗5ht2c受体相关病症的苯并氮杂卓衍生物
CN201010003763A Pending CN101792417A (zh) 2003-06-17 2004-06-16 用于治疗5ht2c受体相关疾病的苯并氮杂卓衍生物

Family Applications After (3)

Application Number Title Priority Date Filing Date
CN2004800167733A Expired - Fee Related CN1805938B (zh) 2003-06-17 2004-06-16 用于治疗5ht2c受体相关疾病的苯并氮杂卓衍生物
CN2008100073149A Expired - Fee Related CN101274911B (zh) 2003-06-17 2004-06-16 用于治疗5ht2c受体相关病症的苯并氮杂卓衍生物
CN201010003763A Pending CN101792417A (zh) 2003-06-17 2004-06-16 用于治疗5ht2c受体相关疾病的苯并氮杂卓衍生物

Country Status (14)

Country Link
US (3) US7704993B2 (enExample)
EP (2) EP2332920A3 (enExample)
JP (2) JP4782003B2 (enExample)
KR (1) KR101152521B1 (enExample)
CN (4) CN1805939B (enExample)
AU (1) AU2004253888B2 (enExample)
BR (1) BRPI0411470A (enExample)
CA (2) CA2529320C (enExample)
EA (1) EA016558B1 (enExample)
IL (1) IL172334A (enExample)
MX (1) MXPA05013366A (enExample)
NZ (1) NZ578503A (enExample)
WO (1) WO2005003096A1 (enExample)
ZA (2) ZA200510194B (enExample)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6953787B2 (en) 2002-04-12 2005-10-11 Arena Pharmaceuticals, Inc. 5HT2C receptor modulators
AU2004253888B2 (en) 2003-06-17 2010-11-11 Arena Pharmaceuticals, Inc. Benzazepine derivatives useful for the treatment of 5HT2C receptor associated diseases
MXPA05013364A (es) * 2003-06-17 2006-03-17 Arena Pharm Inc Procedimiento para preparar 3-benzazepinas.
WO2005042490A1 (en) * 2003-10-22 2005-05-12 Arena Pharmaceuticals, Inc. Benzazepine derivatives and methods of prophylaxis or treatment of 5ht2c receptor associated diseases
EP2400300A1 (en) 2004-08-25 2011-12-28 Takeda Pharmaceutical Company Limited Method of screening preventives/remedies for stress urinary incontinence
PT1838677E (pt) 2004-12-21 2009-11-16 Arena Pharm Inc Formas cristalinas do cloridrato de (r)-8-cloro-1-metil- 2,3,4,5-tetra-hidro-1h-3-benzazepina
SI1833473T1 (sl) * 2004-12-23 2010-01-29 Arena Pharm Inc Sestavki modulatorjev 5HT2C receptorjev in postopki uporabe
ES2397400T3 (es) 2005-09-01 2013-03-06 Eli Lilly & Company 6-arilalquilamino-2,3,4,5-tetrahidro-1H-benzo[D]azepinas como agonistas del receptor 5-HT2C
CA2619287C (en) * 2005-09-01 2013-10-22 Eli Lilly And Company 6-substituted 2,3,4,5-tetrahydro-1h-benzo[d]azepines as 5-ht2c receptor agonists
PL1924560T3 (pl) * 2005-09-01 2009-12-31 Lilly Co Eli 6 podstawione - 2,3,4,5 - tetrahydro-1h-benzo[d]azepiny jako agoniści receptora 5-ht2c
WO2007028132A2 (en) * 2005-09-01 2007-03-08 Eli Lilly And Company 6-N-LINKED HETEROCYCLE-SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-BENZO[d]AZEPINES AS 5-HT2C RECEPTOR AGONISTS
BRPI0707183A2 (pt) 2006-01-19 2011-04-26 Athersys Inc composto, composição farmacêutica, e, método de tratar uma doença, distúrbio e/ou condição em um paciente
WO2007120517A2 (en) 2006-04-03 2007-10-25 Arena Pharmaceuticals, Inc. Processes for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine and intermediates related thereto
WO2007132841A1 (ja) 2006-05-16 2007-11-22 Takeda Pharmaceutical Company Limited 縮合複素環化合物およびその用途
WO2007140213A1 (en) 2006-05-26 2007-12-06 Forest Laboratories Holdings Limited Pyridoazepine derivatives
US8299241B2 (en) 2006-12-05 2012-10-30 Arena Pharmaceuticals, Inc. Processes for preparing (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and intermediates thereof
CL2008000596A1 (es) * 2007-03-01 2008-09-05 Glaxo Group Ltd Forma de dosificacion que comprende 1-(6-[(3-ciclobutil-2,3,4,5-tetrahidro-1h-3-benzazepin-7-il)oxi]-3-piridinil)-2-pirrolidinona, un estabilizador, un excipiente; procedimiento de preparacion; y su uso para tratar enfermedades neurologicas.
JP5520051B2 (ja) 2007-11-15 2014-06-11 武田薬品工業株式会社 縮合ピリジン誘導体およびその用途
JP5491421B2 (ja) * 2008-03-04 2014-05-14 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−ｈｔ２ｃアゴニストである（ｒ）−８−クロロ−１−メチル−２，３，４，５−テトラヒドロ−１ｈ−３−ベンゾアゼピンに関連する中間体の調製のためのプロセス
UA108357C2 (xx) 2009-06-15 2015-04-27 Похідні піразинооксазепіну
CN102648170A (zh) 2009-06-18 2012-08-22 艾尼纳制药公司 制备5-ht2c受体激动剂的方法
JPWO2011071136A1 (ja) 2009-12-11 2013-04-22 アステラス製薬株式会社 線維筋痛症治療剤
US20110269744A1 (en) * 2010-03-12 2011-11-03 Astellas Pharma Inc. Benzazepine Compound
KR20130112848A (ko) 2010-06-02 2013-10-14 아레나 파마슈티칼스, 인크. 5-ｈｔ2ｃ 수용체 아고니스트의 제조 방법
SG188361A1 (en) * 2010-09-01 2013-04-30 Arena Pharm Inc Non-hygroscopic salts of 5-ht2c agonists
CA2808890A1 (en) 2010-09-01 2012-03-08 Arena Pharmaceuticals, Inc. Administration of lorcaserin to individuals with renal impairment
US20130267500A1 (en) 2010-09-01 2013-10-10 Arena Pharmaceuticals, Inc. 5-ht2c receptor agonists in the treatment of disorders ameliorated by reduction of norepinephrine level
WO2012030938A1 (en) * 2010-09-01 2012-03-08 Arena Pharmaceuticals, Inc. Salts of lorcaserin with optically active acids
JP6272695B2 (ja) 2010-09-01 2018-01-31 エーザイ・アール・アンド・ディー・マネジメント株式会社 体重管理のために有用な５−ｈｔ２ｃアゴニストの改変放出剤形
JP2013536858A (ja) * 2010-09-01 2013-09-26 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−ｈｔ２ｃアゴニストの速く溶解する剤形
CN102895233B (zh) * 2012-09-04 2015-06-24 苏州大学 苯并氮杂卓类化合物在制备预防或治疗癫痫的药物中的应用
JP2015534563A (ja) 2012-10-09 2015-12-03 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 体重管理の方法
WO2014060575A2 (en) * 2012-10-19 2014-04-24 Medichem S.A. Process for the enantioselective synthesis of a tetrahydrobenzazepine compound
EP2938345B1 (en) 2012-12-21 2018-08-22 ABT Holding Company Benzazepines as serotonin 5-ht2c receptor ligands and uses thereof
US9309262B2 (en) 2013-03-13 2016-04-12 Abt Holding Company Thienylindole azepines as serotonin 5-HT2C receptor ligands and uses thereof
CN103333111A (zh) * 2013-06-14 2013-10-02 苏州汇和药业有限公司 氯卡色林盐酸盐的制备方法
WO2015066344A1 (en) 2013-11-01 2015-05-07 Arena Pharmaceuticals, Inc. 5-ht2c receptor agonists and compositions and methods of use
CN104936947B (zh) * 2013-12-27 2017-03-08 杭州普晒医药科技有限公司 氯卡色林盐及其晶体、其制备方法和用途
WO2015170346A1 (en) 2014-05-09 2015-11-12 Council Of Scientific & Industrial Research A process for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-benzo[d]azepine its enantiomers
EA022748B1 (ru) * 2014-06-02 2016-02-29 Делкростон Менеджмент Лимитед Способы получения двойных солей лоркасерина (варианты), продукты способов, двойные соли, фармацевтические композиции для лечения и/или профилактики нарушений, связанных с ожирением, их применение и способ лечения и/или профилактики нарушений, связанных с ожирением
CN104016919A (zh) * 2014-06-18 2014-09-03 安徽省逸欣铭医药科技有限公司 一种绿卡色林类似物及其制备方法和用途
CN104130188B (zh) * 2014-08-05 2016-08-31 南京工业大学 8-氯-1-甲基-2,3,4,5-四氢-1h-3-苯并氮杂卓的制备方法
CN105693610B (zh) * 2014-11-28 2019-01-11 国药集团宜宾制药有限责任公司 氯卡色林中间体的制备方法
EP3288946B1 (en) * 2015-04-27 2019-08-21 Arena Pharmaceuticals, Inc. 5-ht2c receptor agonists and compositions and methods of use
CA3002525A1 (en) * 2015-07-31 2017-02-09 Arena Pharmaceuticals, Inc. 5-ht2c receptor agonists and compositions and methods of use
CN105777638B (zh) * 2016-01-06 2019-07-30 北京修正创新药物研究院有限公司 氯卡色林杂质的制备方法
CN106631823B (zh) * 2016-12-20 2022-04-26 天津泰普制药有限公司 一种氯卡色林中间体的制备方法
CN107353250B (zh) * 2016-12-27 2019-11-12 开封制药(集团)有限公司 一种氯卡色林的合成方法
US20210052600A1 (en) 2017-12-27 2021-02-25 Takeda Pharmaceutical Company Limited Therapeutic agents for stress urinary incontinence and incotinence of feces
CN108358796B (zh) * 2018-02-23 2021-03-23 广州同隽医药科技有限公司 一种绿卡色林关键中间体ⅰ的制备方法
CN110590695B (zh) * 2019-10-22 2023-03-21 南华大学 苯并氮杂环类化合物及其应用
CN115784911A (zh) * 2022-10-19 2023-03-14 山东省药学科学院 一种1-[2-(4-氯苯基)-乙基氨基]-2-丙醇的合成方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0285919A1 (en) * 1987-03-27 1988-10-12 Schering Corporation Substituted benzazepines, their preparation and pharmaceutical compositions containing them

Family Cites Families (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH481110A (de) 1967-02-17 1969-11-15 Geigy Ag J R Verfahren zur Herstellung von 1,2,4,5-Tetrahydro-3-azepinen
CH498122A (de) 1968-02-09 1970-10-31 Geigy Ag J R Verfahren zur Herstellung eines neuen Tetrahydroazepinderivates
CH500194A (de) * 1968-02-15 1970-12-15 Ciba Geigy Ag Verfahren zur Herstellung von Tetrahydroazepinderivaten
GB1268243A (en) 1968-03-11 1972-03-22 Wallace & Tiernan Inc 0,2,4,5,-tetrahydro-3h,3-benzazepines
US4233217A (en) 1968-03-11 1980-11-11 Pennwalt Corporation Substituted 1,2,4,5-tetrahydro-3H, 3 benzazepines
FR314F (enExample) 1968-03-22 1970-05-25
FR7736M (enExample) 1968-09-02 1970-03-09
US3716639A (en) 1970-03-11 1973-02-13 Ciba Geigy Corp Anorexigenic tetrahydrobenzazepines
US3795683A (en) 1970-08-19 1974-03-05 Hoffmann La Roche 2,3,4,5-tetrahydro-1h-3-benzazepines
LU65954A1 (enExample) 1972-08-25 1974-03-07
US4210749A (en) 1974-11-12 1980-07-01 Pennwalt Corporation Substituted 1,2,4,5-tetrahydro-3H,3 benzazepines
US4111957A (en) 1977-02-02 1978-09-05 Smithkline Corporation Substituted 1-thienyl and furyl-2,3,4,5-tetrahydro-1H-3-benzazepine compounds
US4108989A (en) 1977-04-01 1978-08-22 Smithkline Corporation 2,3,4,5-tetrahydro-1h-3-benzazepine-7,8-diones
CA1090797A (en) 1978-06-20 1980-12-02 Kenneth G. Holden Substituted 1-thienyl and furyl-2,3,4,5-tetrahydro-1h- 3-benzazepine compounds
AU515236B2 (en) 1978-06-26 1981-03-26 Smithkline Corporation Substituted-1-thienyl and furyl-2,3,4,5-tetrahydro-14-3 benzazepine derivatives
ZA792785B (en) 1978-07-07 1980-08-27 Smithkline Corp Mercapto substituted-2,3,4,5-tetrahydro-1h-3-benzazepines
US4477378A (en) 1980-02-05 1984-10-16 Schering Corp. Esters of substituted 8-hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines
EP0161350A1 (en) 1981-11-27 1985-11-21 Smithkline Beckman Corporation Process for preparing benzazepines
ZA827887B (en) 1981-11-27 1983-11-30 Smithkline Beckman Corp Pharmaceutical compositions and method of producing alpha2 antagonism
FR2525603A1 (fr) 1982-04-27 1983-10-28 Adir Benzoazacycloalkyl-spiro-imidazolinines, leur preparation et leur application en therapeutique
US4988690A (en) 1982-06-14 1991-01-29 Hoechst-Roussel Pharmaceuticals Inc. 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines and anti-depressant use thereof
DE3418270A1 (de) 1984-05-17 1985-11-21 Dr. Karl Thomae Gmbh, 7950 Biberach Neue aminotetralinderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
US4541954A (en) 1984-09-05 1985-09-17 Smithkline Beckman Corporation Method for preparing 6-chloro-N-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine
EP0204349A3 (de) 1985-06-01 1990-01-03 Dr. Karl Thomae GmbH Neue heteroaromatische Aminderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
EG18188A (en) * 1986-05-01 1992-09-30 Pfizer Ltd Process for preparation anti-arhythmia agents
US4762845A (en) 1986-05-21 1988-08-09 Abbott Laboratories 7-(3-Substituted imino-1-pyrrolidinyl)-quinolone-3-carboxylic acids
EP0285287A3 (en) 1987-03-23 1990-08-16 Smithkline Beecham Corporation 3-benzazepine compounds for use in treating gastrointestinal motility disorders
US5015639A (en) 1987-03-27 1991-05-14 Schering Corporation Substituted benzazepines, their preparation and pharmaceutical compositions containing them
US5247080A (en) 1987-03-27 1993-09-21 Schering Corporation Substituted benzazepines useful as intermediates for producing pharmaceutically active compounds
WO1988007858A1 (en) 1987-04-09 1988-10-20 Smithkline Beckman Corporation Sulfinyl and sulfonyl substituted 3-benzazepines
US4957914A (en) 1987-05-15 1990-09-18 Syntex (U.S.A.) Inc. 1,9-alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines
DK107688D0 (da) 1988-03-01 1988-03-01 Novo Industri As Carbaminsyreestere af substituerede 7-hydroxy-2,3,4,5-tetrahydro-1h-3-benzazepiner
US5422355A (en) 1989-06-02 1995-06-06 John Wyeth & Brother, Limited Composition for treating depression with (N-heteroaryl)alkylamines
US5178786A (en) 1989-08-04 1993-01-12 The Lubrizol Corporation Corrosion-inhibiting compositions and functional fluids containing same
CA2037162A1 (en) * 1990-03-12 1991-09-13 Steven Howard Shaber Heterocyclicacetonitriles and fungicidal use
WO1991019698A1 (en) 1990-06-15 1991-12-26 Schering Corporation 8-lower alkyl-5-cycloalkyl or 5-cycloalkenyl substitued benzazepines and pharmaceutical compositions containing them
US5275915A (en) 1991-06-05 1994-01-04 Dainippon Ink And Chemicals, Inc. Developer for light-sensitive material
PT100602A (pt) 1991-06-21 1993-09-30 Smithkline Beecham Plc Uso de derivados de tetra-hidrobenzazepinas, derivados de tetra-hidrobenzazepinas,sua preparacao e composicoes farmaceuticas que os contem
GB9116824D0 (en) 1991-08-05 1991-09-18 Smithkline Beecham Corp Chemical compounds
EP0558824A1 (en) 1992-02-04 1993-09-08 Duphar International Research B.V Method for the preparation of vicinal aminoalcohols and optically active O-protected derivatives thereof
JPH05339263A (ja) 1992-06-08 1993-12-21 Wakunaga Pharmaceut Co Ltd ジヒドロピリジン誘導体
JPH06298746A (ja) 1993-04-19 1994-10-25 Showa Denko Kk 環状イミド酸エステルの製造法
CA2166100A1 (en) 1993-06-23 1995-01-05 Richard A. Glennon Sigma receptor ligands and the use thereof
US5387685A (en) 1993-07-16 1995-02-07 American Cyanamid Co MDR reversal agents
GB9322976D0 (en) 1993-11-08 1994-01-05 Pfizer Ltd Therapeutic agents
DE4419246A1 (de) 1994-06-01 1995-12-07 Merckle Gmbh Heteroarylsubstituierte Pyrrolizinverbindungen und deren Anwendung in der Pharmazie
DE4419315A1 (de) 1994-06-01 1995-12-07 Merckle Gmbh Heteropyrrolizinverbindungen und deren Anwendung in der Pharmazie
DE4419247A1 (de) 1994-06-01 1995-12-07 Merckle Gmbh Sulfonylierte Pyrrolizincarbonsäureamide und deren Anwendung in der Pharmazie
DE4427838A1 (de) 1994-08-05 1996-02-08 Thomae Gmbh Dr K Kondensierte Azepinderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE4429079A1 (de) 1994-08-17 1996-02-22 Thomae Gmbh Dr K Cyclische Harnstoffderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
JPH08134048A (ja) 1994-11-08 1996-05-28 Sumitomo Chem Co Ltd オキサゾリン類の製造法
GB9508622D0 (en) 1995-04-28 1995-06-14 Pfizer Ltd Therapeutic agants
JPH0930960A (ja) 1995-07-18 1997-02-04 Takasago Internatl Corp 真菌感染症治療剤
JPH0987258A (ja) 1995-09-28 1997-03-31 Sumitomo Chem Co Ltd オキサゾリン類、その製造方法およびそれを用いる不斉シクロプロパンカルボン酸類の製造方法
CA2190708A1 (en) 1995-12-08 1997-06-09 Johannes Aebi Aminoalkyl substituted benzo-heterocyclic compounds
US5892116A (en) 1996-01-03 1999-04-06 Georgetown University Gelators
US5925651A (en) 1996-04-03 1999-07-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5691362A (en) 1996-06-05 1997-11-25 Schering-Plough Corporation Substituted benzene-fused hetero- and carbocyclics as nuerokinin antagonists
EP0920417A4 (en) 1996-08-15 1999-12-29 Smithkline Beecham Corp IL-8 RECEPTOR ANTAGONISTS
AU6290998A (en) 1997-03-07 1998-09-29 Novo Nordisk A/S 4,5,6,7-tetrahydro-thieno{3,2-c}pyridine derivatives, their preparation and use
AUPP020297A0 (en) 1997-11-05 1997-11-27 University Of Melbourne, The A novel receptor, and compounds which bind thereto
KR100620337B1 (ko) 1998-03-10 2006-09-13 오노 야꾸힝 고교 가부시키가이샤 카르복실산 유도체와 그 유도체를 유효 성분으로서함유하는 약제
EP0987235B1 (en) 1998-08-25 2003-03-12 MERCK PATENT GmbH Method for the conversion of arenes or alkenes with iodoalkenes, aryl iodides or arenediazonium salts
EP1074549B1 (en) 1999-08-06 2003-11-19 F. Hoffmann-La Roche Ag Tetrahydro-benzo(d)azepines and their use as antagonists at metabotropic glutamate receptors
DE60006618T2 (de) 1999-08-06 2004-09-23 F. Hoffmann-La Roche Ag Tetrahydro-benzo(d)azepine und deren Verwendung als metabotrope Glutamatrezeptor-Antagonisten
DE10003708A1 (de) 2000-01-28 2001-08-02 Solvent Innovation Gmbh Neuartige chirale ionische Flüssigkeiten und Verfahren zu ihrer Darstellung in enantiomerenreiner oder enantiomerenangereicherter Form
KR100815681B1 (ko) 2000-06-30 2008-03-20 글락소 그룹 리미티드 퀴나졸린 디토실레이트 염 화합물
JP4272423B2 (ja) 2000-11-14 2009-06-03 スミスクライン ビーチャム ピー エル シー ドーパミンｄ３受容体のモジュレーターとして有用なテトラヒドロベンズアゼピン誘導体（抗精神病剤）
DE10057751A1 (de) 2000-11-22 2002-05-23 Bayer Ag Neue Carbamat-substituierte Pyrazolopyridinderivate
GB0030710D0 (en) 2000-12-15 2001-01-31 Hoffmann La Roche Piperazine derivatives
JPWO2002074746A1 (ja) * 2001-03-16 2004-07-08 山之内製薬株式会社 ベンゾアゼピン誘導体
US6825198B2 (en) 2001-06-21 2004-11-30 Pfizer Inc 5-HT receptor ligands and uses thereof
MXPA04002785A (es) 2001-09-24 2004-07-29 Elan Pharm Inc Aminas sustituidas para tratamiento de enfermedad de alzheimer.
AU2003214873A1 (en) 2002-01-18 2003-09-02 Ceretek Llc Methods of treating conditions associated with an edg receptor
JP3813152B2 (ja) 2002-03-12 2006-08-23 メルク エンド カムパニー インコーポレーテッド 置換アミド類
US6953787B2 (en) 2002-04-12 2005-10-11 Arena Pharmaceuticals, Inc. 5HT2C receptor modulators
DE10220570A1 (de) 2002-05-08 2003-11-20 Bayer Ag Carbamat-substituierte Pyrazolopyridine
DE10261131A1 (de) 2002-12-20 2004-07-01 Grünenthal GmbH Substituierte 5-Aminomethyl-1H-pyrrol-2-carbonsäureamide
US7145012B2 (en) 2003-04-23 2006-12-05 Pfizer Inc. Cannabinoid receptor ligands and uses thereof
US7232823B2 (en) 2003-06-09 2007-06-19 Pfizer, Inc. Cannabinoid receptor ligands and uses thereof
MXPA05013364A (es) 2003-06-17 2006-03-17 Arena Pharm Inc Procedimiento para preparar 3-benzazepinas.
AU2004253888B2 (en) 2003-06-17 2010-11-11 Arena Pharmaceuticals, Inc. Benzazepine derivatives useful for the treatment of 5HT2C receptor associated diseases
WO2005042490A1 (en) 2003-10-22 2005-05-12 Arena Pharmaceuticals, Inc. Benzazepine derivatives and methods of prophylaxis or treatment of 5ht2c receptor associated diseases
WO2005042491A1 (en) 2003-10-22 2005-05-12 Arena Pharmaceuticals, Inc. Benzazepine derivatives and methods of prophylaxis or treatment of 5ht2c receptor associated diseases
PT1838677E (pt) 2004-12-21 2009-11-16 Arena Pharm Inc Formas cristalinas do cloridrato de (r)-8-cloro-1-metil- 2,3,4,5-tetra-hidro-1h-3-benzazepina
SI1833473T1 (sl) 2004-12-23 2010-01-29 Arena Pharm Inc Sestavki modulatorjev 5HT2C receptorjev in postopki uporabe

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0285919A1 (en) * 1987-03-27 1988-10-12 Schering Corporation Substituted benzazepines, their preparation and pharmaceutical compositions containing them

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Wei K.Chang,et al..Dopamine receptor binding properties of some2,3,4,5-tetrahydro-1H-3-benzaepine-7-ols with non-aromaticsubstituents in the 5-position.Bioorganic & Medicinal Chemical Letters2 5.1992,2(5),399-402. *

Also Published As

Publication number Publication date
JP4782003B2 (ja) 2011-09-28
ZA200510194B (en) 2007-02-28
US20130172322A1 (en) 2013-07-04
CN1805938A (zh) 2006-07-19
US20100173894A1 (en) 2010-07-08
ZA200510255B (en) 2006-12-27
NZ578503A (en) 2011-02-25
BRPI0411470A (pt) 2006-07-11
IL172334A (en) 2013-08-29
KR20060023156A (ko) 2006-03-13
CA2529320C (en) 2013-03-05
KR101152521B1 (ko) 2012-06-01
AU2004253888A1 (en) 2005-01-13
JP2007516941A (ja) 2007-06-28
AU2004253888B2 (en) 2010-11-11
US7704993B2 (en) 2010-04-27
CA2529320A1 (en) 2005-01-13
CN101274911A (zh) 2008-10-01
CA2888392A1 (en) 2005-03-03
JP2011162564A (ja) 2011-08-25
CN1805939A (zh) 2006-07-19
CN101792417A (zh) 2010-08-04
CN101274911B (zh) 2011-01-26
WO2005003096A1 (en) 2005-01-13
EA200600048A1 (ru) 2006-06-30
EP1633720A1 (en) 2006-03-15
IL172334A0 (en) 2011-08-01
CN1805938B (zh) 2010-06-16
MXPA05013366A (es) 2006-04-05
EP2332920A3 (en) 2011-12-21
EP2332920A2 (en) 2011-06-15
US8404675B2 (en) 2013-03-26
US20070142357A1 (en) 2007-06-21
EA016558B1 (ru) 2012-05-30

Similar Documents

Publication Publication Date Title
CN1805939B (zh) 用于治疗5ht2c受体相关病症的苯并氮杂卓衍生物
JP5421311B2 (ja) ３−ベンズアゼピンを調製する方法
CN101547892A (zh) 制备(r)-8-氯-1-甲基-2，3，4，5-四氢-1h-3-苯并氮杂卓的方法和其中间体
LU85978A1 (fr) Benzamides substitues pharmacologiquement actifs
NO310193B1 (no) 2,3,4,5-tetrahydro-1H-3-benzazepiner og farmasöytisk akseptable syreaddisjonssalter derav, farmasöytiske preparater somomfatter disse, samt anvendelse av dem til fremstilling avpreparatene
JPH04987B2 (enExample)
IL132353A (en) Procedure for preparation of 3N, N-disiclobutylamino - 8fluoro- -4,3 dihydro-H2-1 benzopyran-5-carboxamide and drug-acceptable salts
HK1160838B (en) 8-chloro-1 -methyl-2,3,4,5-tetrahydro-1 h-3benzazapine hydrochloride
HK1158308A (en) Processes for preparing 3-benzazepines
HK1157764A (en) Processes for preparing 3-benzazepines
HK1144428B (en) Processes for the separation of 3-benzazepine racemates
AU2012200805B2 (en) Benzazepine derivatives useful for the treatment of 5HT2C receptor associated diseases
JPS62283978A (ja) トランス−ベンゾピラン−〔４，３−ｂ〕−１，４−オキサジン誘導体

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
TR01 Transfer of patent right

Effective date of registration: 20180115

Address after: Tokyo City

Patentee after: Eisai Co.,Ltd.

Address before: Tokyo City

Patentee before: Eisai Co.,Ltd.

Effective date of registration: 20180115

Address after: Tokyo City

Patentee after: Eisai Co.,Ltd.

Address before: California, USA

Patentee before: ARENA PHARMACEUTICALS, Inc.

TR01 Transfer of patent right
CX01 Expiry of patent term

Granted publication date: 20101013

CX01 Expiry of patent term