NO324248B1 - Substituerte beta-karboliner med IKB-kinaseinhiberende aktivitet, fremgangsmate for fremstilling derav, anvendelse derav samt farmasoytikum inneholdende minst en slik forbindelse - Google Patents

Substituerte beta-karboliner med IKB-kinaseinhiberende aktivitet, fremgangsmate for fremstilling derav, anvendelse derav samt farmasoytikum inneholdende minst en slik forbindelse Download PDF

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Publication number
NO324248B1
NO324248B1 NO20024338A NO20024338A NO324248B1 NO 324248 B1 NO324248 B1 NO 324248B1 NO 20024338 A NO20024338 A NO 20024338A NO 20024338 A NO20024338 A NO 20024338A NO 324248 B1 NO324248 B1 NO 324248B1
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Prior art keywords
alkyl
formula
hydrogen atom
compound
independently
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NO20024338A
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English (en)
Norwegian (no)
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NO20024338L (no
NO20024338D0 (no
Inventor
Hormoz Mazdiyasni
Olaf Ritzeler
Alfredo Castro
Louis Grenier
Francois Soucy
Wayne W Hancock
Vito Palombella
Julian Adams
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Sanofi Aventis Deutschland
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Priority claimed from EP00105514A external-priority patent/EP1134221A1/fr
Priority claimed from EP00125169A external-priority patent/EP1209158A1/fr
Priority claimed from PCT/EP2001/002237 external-priority patent/WO2001068648A1/fr
Application filed by Sanofi Aventis Deutschland filed Critical Sanofi Aventis Deutschland
Publication of NO20024338D0 publication Critical patent/NO20024338D0/no
Publication of NO20024338L publication Critical patent/NO20024338L/no
Publication of NO324248B1 publication Critical patent/NO324248B1/no

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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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NO20024338A 2000-03-15 2002-09-11 Substituerte beta-karboliner med IKB-kinaseinhiberende aktivitet, fremgangsmate for fremstilling derav, anvendelse derav samt farmasoytikum inneholdende minst en slik forbindelse NO324248B1 (no)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP00105514A EP1134221A1 (fr) 2000-03-15 2000-03-15 Bêta-carbolines substituées comme inhibiteurs de lkB kinase
EP00125169A EP1209158A1 (fr) 2000-11-18 2000-11-18 Bêta-carbolines subtituées
PCT/EP2001/002237 WO2001068648A1 (fr) 2000-03-15 2001-02-28 Beta-carbolines substituees ayant une activite inhibitrice de l'ikb-kinase

Publications (3)

Publication Number Publication Date
NO20024338D0 NO20024338D0 (no) 2002-09-11
NO20024338L NO20024338L (no) 2002-11-05
NO324248B1 true NO324248B1 (no) 2007-09-17

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NO20024338A NO324248B1 (no) 2000-03-15 2002-09-11 Substituerte beta-karboliner med IKB-kinaseinhiberende aktivitet, fremgangsmate for fremstilling derav, anvendelse derav samt farmasoytikum inneholdende minst en slik forbindelse

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US (3) US6627637B2 (fr)
JP (1) JP5000828B2 (fr)
KR (1) KR100826817B1 (fr)
CN (1) CN100509810C (fr)
AT (1) ATE465161T1 (fr)
AU (2) AU3741801A (fr)
BR (1) BR0109161A (fr)
CA (1) CA2402549A1 (fr)
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DE (1) DE60141895D1 (fr)
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IL (2) IL151695A0 (fr)
ME (1) MEP28108A (fr)
MX (1) MXPA02007981A (fr)
NO (1) NO324248B1 (fr)
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PL (1) PL357284A1 (fr)
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Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU3741801A (en) * 2000-03-15 2001-09-24 Aventis Pharma Gmbh Substituted beta-carbolines with ikb-kinase inhibiting activity
CA2436770A1 (fr) * 2001-02-01 2002-08-08 James R. Burke Methodes de traitement de maladies inflammatoires et immunitaires a l'aide d'inhibiteurs ikb kinase (ikk)
US9248124B2 (en) * 2001-11-07 2016-02-02 Millennium Pharmaceuticals, Inc. Use of inhibitors of IκB kinase for the treatment of cancer
US7462638B2 (en) * 2002-08-17 2008-12-09 Sanofi-Aventis Deutschland Gmbh Use of IκB-kinase inhibitors in pain therapy
US20040166095A1 (en) * 2003-02-25 2004-08-26 Blazar Bruce R. Methods for preventing GVHD
EA009121B1 (ru) * 2003-04-09 2007-10-26 Миллениум Фармасьютикалз, Инк. Бета-карболины, применяемые для лечения воспалительных заболеваний
EP2206713A1 (fr) * 2004-04-09 2010-07-14 Millennium Pharmaceuticals, Inc. Béta-carbolines utiles pour traiter une maladie inflammatoire
JP5094394B2 (ja) * 2005-04-20 2012-12-12 武田薬品工業株式会社 縮合複素環化合物
US8119655B2 (en) * 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
AU2006316322B2 (en) * 2005-11-22 2011-08-25 Merck Canada Inc. Tricyclic compounds useful as inhibitors of kinases
WO2009054965A1 (fr) * 2007-10-23 2009-04-30 Millennium Pharmaceuticals, Inc. Sel de n-(6-chloro-9h-pyrido[3,4-b]indol-8-yl)-4-[2-(2,6-diméthyl-4-morpholinyl)-2-oxoéthyl]-6,6-diméthylmorpholinecarboxamide
US20090137579A1 (en) * 2007-10-23 2009-05-28 Millennium Pharmaceuticals, Inc. Mesylate salt of an IKK inhibitor
MX2010006457A (es) * 2007-12-19 2010-07-05 Amgen Inc Compuestos fusionados de piridina, pirimidina y triazina como inhibidores de ciclo celular.
ES2523580T3 (es) 2008-01-11 2014-11-27 Albany Molecular Research, Inc. Piridoindoles substituidos con (1-Azinona)
CN101245066B (zh) * 2008-01-23 2010-11-10 复旦大学 一种制备7-烷氧基-2,9-二氮芴衍生物的方法
AU2009233951B2 (en) * 2008-04-07 2014-02-27 Amgen Inc. Gem-disubstituted and spirocyclic amino pyridines/pyrimidines as cell cycle inhibitors
EP2297347B1 (fr) 2008-05-14 2017-03-08 Millennium Pharmaceuticals, Inc. Méthodes et trousses pour surveiller les effets d'immunomodulateurs sur l'immunité adaptative
KR101764556B1 (ko) * 2008-06-11 2017-08-02 제넨테크, 인크. 디아자카르바졸 및 사용 방법
CA2725754C (fr) 2008-06-11 2017-05-23 Hazel Joan Dyke Diazacarbazoles et procedes d'utilisation
US20100074939A1 (en) * 2008-09-25 2010-03-25 Osteogenex Inc. Harmine compounds for promoting bone growth
CN101717397B (zh) * 2008-10-09 2012-11-28 中国科学院上海药物研究所 一类取代吡啶并[2',1':2,3]咪唑并[4,5-c]异喹啉酮类化合物及其合成方法和用途,以及包含该类化合物的药物组合物
JP2012532144A (ja) 2009-07-01 2012-12-13 アルバニー モレキュラー リサーチ， インコーポレイテッド アジノン置換アゼピノ［ｂ］インドールおよびピリド−ピロロ−アゼピンｍｃｈ−１拮抗薬、ならびにその作製方法および使用
WO2011003021A1 (fr) 2009-07-01 2011-01-06 Albany Molecular Research, Inc. Antagonistes de mch-1 azabicycloalcane-indoles et azabicycloalcane-pyrrolo-pyridines substitués par azinone, leurs procédés de fabrication et leur utilisation
WO2011003012A1 (fr) 2009-07-01 2011-01-06 Albany Molecular Research, Inc. Antagonistes de mch-1 azapolycycles substitués par azinone, leurs procédés de fabrication et leur utilisation
WO2011003007A1 (fr) 2009-07-01 2011-01-06 Albany Molecular Research, Inc. Antagonistes de mch-1 d’azabicycloalcane-indole et d’azabicycloalcane-pyrrolo-pyridine, procédés de préparation, et utilisation de ceux-ci
US20110183938A1 (en) * 2009-12-16 2011-07-28 Genentech, Inc. 1,7-diazacarbazoles and methods of use
RU2419431C1 (ru) * 2010-02-10 2011-05-27 Андрей Александрович Винник ПРОИЗВОДНЫЕ β-КАРБОЛИНА, ОБЛАДАЮЩИЕ ПРОТИВОТУБЕРКУЛЕЗНОЙ АКТИВНОСТЬЮ, ИХ ПРИМЕНЕНИЯ ДЛЯ ПРОИЗВОДСТВА ЛЕКАРСТВЕННОГО СРЕДСТВА, СПОСОБ ИХ СИНТЕЗА, А ТАКЖЕ НОВЫЕ МЕТОДЫ ЛЕЧЕНИЯ С ИХ ИСПОЛЬЗОВАНИЕМ
WO2011159857A1 (fr) * 2010-06-16 2011-12-22 Bristol-Myers Squibb Company Composés de carboline-carboxamide utiles en tant qu'inhibiteurs de kinases
US9168247B2 (en) 2010-06-25 2015-10-27 Facultes Universitaires Notre Dame De La Paix Beta carboline derivatives useful in the treatment of proliferative disorders
EP2455378A1 (fr) * 2010-11-03 2012-05-23 Philip Morris Products S.A. Dérivés de carbazole et de carboline, et préparation et applications thérapeutiques associées
US8993765B2 (en) 2010-12-21 2015-03-31 Albany Molecular Research, Inc. Tetrahydro-azacarboline MCH-1 antagonists, methods of making, and uses thereof
US8697700B2 (en) 2010-12-21 2014-04-15 Albany Molecular Research, Inc. Piperazinone-substituted tetrahydro-carboline MCH-1 antagonists, methods of making, and uses thereof
JP5854492B2 (ja) * 2011-02-24 2016-02-09 国立大学法人 岡山大学 軟骨細胞分化誘導促進剤
CA2830516C (fr) 2011-03-23 2017-01-24 Amgen Inc. Doubles inhibiteurs tricycliques fusionnes de cdk 4/6 et de flt3
CN102250089B (zh) * 2011-05-20 2012-11-14 中国科学院南海海洋研究所 β-咔啉生物碱及其在制备抗疟疾药物中的应用
CN113416187B (zh) 2013-03-14 2024-07-19 奥斯菲治疗有限公司 促进骨生长的烷基胺骆驼蓬碱衍生物
WO2014191726A1 (fr) * 2013-05-28 2014-12-04 Astrazeneca Ab Composés chimiques
ES2633987T3 (es) * 2013-07-02 2017-09-26 Bristol-Myers Squibb Company Derivados de pirido-carboxamidas tricíclicas como inhibidores de ROCK
US9663529B2 (en) * 2013-07-02 2017-05-30 Bristol-Myers Squibb Company Tricyclic pyrido-carboxamide derivatives as rock inhibitors
WO2018119208A1 (fr) 2016-12-22 2018-06-28 Global Blood Therapeutics, Inc. Inhibiteurs de l'histone méthyltransférase
WO2018226998A1 (fr) * 2017-06-09 2018-12-13 Global Blood Therapeutics, Inc. Composés d'azaindole utilisés en tant qu'inhibiteurs d'histone méthyltransférase
CN110636847B (zh) * 2018-04-25 2023-06-09 昂科克罗斯株式会社 用于预防及治疗肌肉疾病的组合物
JP2022504011A (ja) 2018-08-14 2022-01-13 オステオーク インコーポレイティド ピロロ－ジピリジン化合物
JP2021535091A (ja) 2018-08-14 2021-12-16 オステオーク インコーポレイティド フルオロβ−カルボリン化合物
US11485734B2 (en) 2018-10-02 2022-11-01 Northwestern University Beta-carbolines as positive allosteric modulators of the human serotonin receptor 2C (5-HT2C)
CN111374975A (zh) * 2018-12-27 2020-07-07 北京大学 去氢骆驼蓬碱的药物用途
CN112047940B (zh) * 2020-08-28 2021-06-29 南通大学 含1-(3,4-二甲氧基苯基)-β-咔啉单元的吡唑化合物的制备与用途
WO2024012554A1 (fr) * 2022-07-14 2024-01-18 上海日馨医药科技股份有限公司 Agoniste de tpk et procédé de traitement de maladies neurodégénératives l'utilisant
US11939330B1 (en) * 2023-08-25 2024-03-26 King Faisal University Pyrido[3,4-b]indole-6-carboxylic acid compounds as CK2 inhibitors

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE568675C (de) * 1930-10-04 1933-01-27 Boots Pure Drug Co Ltd Verfahren zur Herstellung von O-Alkyl-, Oxyalkyl- oder Alkylaminoalkylaethern des Harmols oder Harmalols
DK72180A (da) * 1979-04-10 1980-10-11 Ciba Geigy Ag Fremgangsmaade til fremstilling af diazatricycler samt salte deraf
DE3240514A1 (de) * 1982-10-29 1984-05-03 Schering AG, 1000 Berlin und 4709 Bergkamen Ss-carboline, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische praeparate
US4631149A (en) * 1983-07-25 1986-12-23 University Of Illinois Antiviral eudistomins from a marine tunicate
JPS63250378A (ja) * 1987-04-07 1988-10-18 Mitsubishi Kasei Corp インド−ル誘導体
CA2140722A1 (fr) 1994-01-24 1995-07-25 Joseph A. Jakubowski Beta-carboline-thromboxane-synthetase
DE4435477A1 (de) * 1994-10-04 1996-04-11 Bayer Ag Cycloalkano-indol- und -azaindol-derivate
US5532261A (en) * 1994-12-12 1996-07-02 Merck & Co., Inc. Carbapenem antibiotics, compositions containing such compounds and methods of use
US6093723A (en) * 1996-08-09 2000-07-25 Boehringer Ingelheim Pharmaceuticals, Inc. 4-substituted beta-carbolines and analogs thereof
EP0827746B1 (fr) * 1996-09-05 2002-04-03 Eli Lilly And Company Analogues de carbazole étant agonistes beta3-adrénergiques sélectifs
US5843721A (en) 1997-07-03 1998-12-01 Tularik Inc. Nucleic acids encoding human NIK protein
ZA9810766B (en) * 1997-11-28 1999-05-25 Mochida Pharm Co Ltd Novel compounds having cgmp-pde inhibitory activity
DE19807993A1 (de) * 1998-02-26 1999-09-02 Bayer Ag Verwendung von ß-Carbolinderivaten zur Bekämpfung von TNF-alpha-abhängigen Krankheiten
AU3741801A (en) * 2000-03-15 2001-09-24 Aventis Pharma Gmbh Substituted beta-carbolines with ikb-kinase inhibiting activity

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