EA200501584A1 - Бета-карболины, применяемые для лечения воспалительных заболеваний - Google Patents

Бета-карболины, применяемые для лечения воспалительных заболеваний

Info

Publication number
EA200501584A1
EA200501584A1 EA200501584A EA200501584A EA200501584A1 EA 200501584 A1 EA200501584 A1 EA 200501584A1 EA 200501584 A EA200501584 A EA 200501584A EA 200501584 A EA200501584 A EA 200501584A EA 200501584 A1 EA200501584 A1 EA 200501584A1
Authority
EA
Eurasian Patent Office
Prior art keywords
treatment
inflammatory diseases
beta
carbolins
ikk
Prior art date
Application number
EA200501584A
Other languages
English (en)
Other versions
EA009121B1 (ru
Inventor
Майкл Е. Хепперле
Джули Филдз Лю
Франсуа Суси
Йингчун Йе
Роберт С. Мюррей
Раман Пракаш
Джереми Д. Литтл
Альфредо Кастро
Хормоз Маздиясни
Пол Е. Флеминг
Доминик Рейнольдс
Original Assignee
Миллениум Фармасьютикалз, Инк.
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 Миллениум Фармасьютикалз, Инк. filed Critical Миллениум Фармасьютикалз, Инк.
Publication of EA200501584A1 publication Critical patent/EA200501584A1/ru
Publication of EA009121B1 publication Critical patent/EA009121B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/08—Bronchodilators
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Изобретением являются бета-карболиновые соединения формулы Iгде кольцо А представляет собой замещенное пиридинильное, пиримидинильное, морфолинильное, пиперидинильное, пиперазинильное, пирролидинильное, пиранильное, тетрагидрофуранильное, циклогексильное, циклопентильное или тиоморфолинильное кольцо и R, Rи R- такие, как приведено в описании изобретения. Эти соединения представляют собой ингибиторы IKK-2, которые являются эффективными для лечения IKK-2-опосредованных заболеваний, таких как воспалительные заболевания и рак.
EA200501584A 2003-04-09 2004-04-09 Бета-карболины, применяемые для лечения воспалительных заболеваний EA009121B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US46146803P 2003-04-09 2003-04-09
PCT/US2004/011080 WO2004092167A1 (en) 2003-04-09 2004-04-09 Beta-carbolines useful for treating inflammatory disease

Publications (2)

Publication Number Publication Date
EA200501584A1 true EA200501584A1 (ru) 2006-06-30
EA009121B1 EA009121B1 (ru) 2007-10-26

Family

ID=33299818

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200501584A EA009121B1 (ru) 2003-04-09 2004-04-09 Бета-карболины, применяемые для лечения воспалительных заболеваний

Country Status (22)

Country Link
US (2) US7727985B2 (ru)
EP (1) EP1611134A1 (ru)
JP (1) JP2006522824A (ru)
KR (1) KR20060006031A (ru)
CN (1) CN1802375A (ru)
AU (1) AU2004230952A1 (ru)
BR (1) BRPI0409263A (ru)
CA (1) CA2521300A1 (ru)
CO (1) CO5700746A2 (ru)
CR (1) CR8042A (ru)
EA (1) EA009121B1 (ru)
EC (1) ECSP056145A (ru)
HR (1) HRP20050926A2 (ru)
MA (1) MA27837A1 (ru)
MX (1) MXPA05010793A (ru)
NI (1) NI200500174A (ru)
NO (1) NO20054598L (ru)
OA (1) OA13115A (ru)
RS (1) RS20050832A (ru)
TN (1) TNSN05257A1 (ru)
WO (1) WO2004092167A1 (ru)
ZA (1) ZA200508198B (ru)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA009121B1 (ru) 2003-04-09 2007-10-26 Миллениум Фармасьютикалз, Инк. Бета-карболины, применяемые для лечения воспалительных заболеваний
DE602005020263D1 (de) * 2004-04-09 2010-05-12 Millennium Pharm Inc Für die behandlung von entzündlichen krankheiten nützliche beta-carboline
US8119655B2 (en) * 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
EP1954290B1 (en) * 2005-11-22 2012-07-25 Merck Sharp & Dohme Corp. Tricyclic compounds useful as inhibitors of kinases
CA2646316C (en) * 2006-03-15 2016-05-24 Theralogics, Inc. Methods of treating muscular wasting diseases using nf-kb activation inhibitors
WO2008002246A1 (en) * 2006-06-28 2008-01-03 Astrazeneca Ab A pharmaceutical composition comprising an ikk2 inhibitor and a second active ingrdient.
EP2125841A1 (en) * 2006-12-13 2009-12-02 Gilead Sciences, Inc. Monophosphates as mutual prodrugs of anti-inflammatory signal transduction modulators (aistm's) and beta-agonists for the treatment of pulmonary inflammation and bronchoconstriction
US20090131422A1 (en) * 2007-10-23 2009-05-21 Millennium Pharmaceuticals, Inc. Salts of an IKK inhibitor
WO2009054970A1 (en) * 2007-10-23 2009-04-30 Millennium Pharmaceuticals, Inc. Mesylate salt of an ikk inhibitor
JP5892791B2 (ja) 2008-05-14 2016-03-23 ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． 適応免疫における免疫調節物質の効果をモニターするための方法およびキット
CN102171204B (zh) 2008-10-02 2014-08-20 旭化成制药株式会社 8位取代异喹啉衍生物及其用途
EP2552428A1 (en) 2010-03-30 2013-02-06 Novartis AG Pkc inhibitors for the treatment of b-cell lymphoma having chronic active b-cell-receptor signalling
CN103596949A (zh) * 2011-03-28 2014-02-19 Sjt分子研究有限公司 用于代谢综合征的治疗的化合物
CN102416014B (zh) * 2011-09-13 2012-11-21 河南中医学院 一种生物碱类成分组合物在制备抗甲型h1n1流感病毒药物中的应用
CN102391323B (zh) * 2011-10-18 2013-09-25 首都医科大学 四氢-β-咔啉衍生物、其制备方法及其用途
KR101646916B1 (ko) 2015-07-13 2016-08-09 강원대학교산학협력단 베타-카르볼린 알칼로이드 화합물을 함유하는 염증성 질환의 예방 또는 치료용 조성물
CN108271369A (zh) 2015-10-23 2018-07-10 法尔玛赞公司 用于制备色胺及其衍生物的新工艺
CN109593089B (zh) * 2019-01-24 2022-01-28 西南大学 二氮杂螺癸烷哌啶甲酰胺类化合物制备和应用
CN112824387B (zh) * 2019-11-21 2023-03-21 济南尚博生物科技有限公司 一种2-甲基烟酸酯及其制备方法和应用
CN117510494B (zh) * 2023-11-07 2024-04-19 桂林医学院附属医院 β-咔啉-沙利度胺偶联物及其在制备逆转ABT-199耐药的药物中的应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69925840T2 (de) 1998-08-12 2006-05-04 Pfizer Products Inc., Groton Tace inhibitoren
DE19951360A1 (de) * 1999-10-26 2001-05-03 Aventis Pharma Gmbh Substituierte Indole
RU2277095C2 (ru) * 2000-03-15 2006-05-27 Санофи-Авентис Дойчланд Гмбх Замещенные бета-карболины
EP1268477B1 (en) * 2000-03-15 2010-04-21 Sanofi-Aventis Deutschland GmbH Substituted beta-carbolines with ikb-kinase inhibiting activity
BR0212617A (pt) * 2001-09-19 2005-02-09 Pharmacia Corp Compostos de pirazolila substituìdo para o tratamento de inflamação
WO2003039545A2 (en) * 2001-11-07 2003-05-15 Millennium Pharmaceuticals, Inc. Carboline derivatives as inhibitors of ikb in the treatment of multiple myeloma and others cancers
US7396943B2 (en) * 2003-03-07 2008-07-08 Eli Lilly And Company Opioid receptor antagonists
EA009121B1 (ru) 2003-04-09 2007-10-26 Миллениум Фармасьютикалз, Инк. Бета-карболины, применяемые для лечения воспалительных заболеваний

Also Published As

Publication number Publication date
TNSN05257A1 (en) 2007-07-10
OA13115A (en) 2006-11-10
US20100093713A1 (en) 2010-04-15
EP1611134A1 (en) 2006-01-04
JP2006522824A (ja) 2006-10-05
NO20054598D0 (no) 2005-10-06
ZA200508198B (en) 2007-01-31
HRP20050926A2 (en) 2006-06-30
EA009121B1 (ru) 2007-10-26
CO5700746A2 (es) 2006-11-30
AU2004230952A1 (en) 2004-10-28
WO2004092167A8 (en) 2006-01-05
US20040235839A1 (en) 2004-11-25
MA27837A1 (fr) 2006-04-03
CA2521300A1 (en) 2004-10-28
KR20060006031A (ko) 2006-01-18
BRPI0409263A (pt) 2006-03-28
RS20050832A (en) 2007-12-31
NO20054598L (no) 2005-10-27
CR8042A (es) 2006-05-30
US7727985B2 (en) 2010-06-01
NI200500174A (es) 2006-04-17
MXPA05010793A (es) 2005-12-05
ECSP056145A (es) 2006-04-19
WO2004092167A1 (en) 2004-10-28
CN1802375A (zh) 2006-07-12

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Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU