AR050155A1 - 3-aminoindazoles, un procedimiento de preparcion, uso de los compuestos para preparar medicamentos, dichos medicamentos y un compuesto intermediario - Google Patents

3-aminoindazoles, un procedimiento de preparcion, uso de los compuestos para preparar medicamentos, dichos medicamentos y un compuesto intermediario

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Publication number
AR050155A1
AR050155A1 ARP050102033A ARP050102033A AR050155A1 AR 050155 A1 AR050155 A1 AR 050155A1 AR P050102033 A ARP050102033 A AR P050102033A AR P050102033 A ARP050102033 A AR P050102033A AR 050155 A1 AR050155 A1 AR 050155A1
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Argentina
Prior art keywords
mono
hal
het
trisubstituted
con
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ARP050102033A
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English (en)
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Lars Thore Burgdorf
Rolf Gericke
Norbert Beier
Werner Mederski
Florian Lang
Dieter Dorsch
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Merck Patent Gmbh
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Publication of AR050155A1 publication Critical patent/AR050155A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
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    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
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    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Hematology (AREA)
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  • Obesity (AREA)
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Abstract

Los 3-aminoindazoles de la formula (1), son inhibidores de la SGK y pueden ser utilizados para el tratamiento de enfermedades y dolencias causadas por las SGK y tales como diabetes, obesidad, síndrome metabolico (dislipidemia), hipertonía sistémica y pulmonar, enfermedades cardiocirculatorias y renales, en general para todo tipo de fibrosis y procesos inflamatorios. Se reivindica el compuesto, un método de preparacion, su uso para preparar medicamentos y un kid para el compuesto y un compuesto intermediario de síntesis. Reivindicacion 1: Compuestos de la formula (1), en donde: W es -[C(R2)2]n-, -[C(R2)2]nCONR2[C(R2)2]n-, -[C(R2)2]nCONR2NR2[C(R2)2]n-, -[C(R2)2]nNR2CO[C(R2)2]n-, -[C(R2)2]nNR2CO[C(R2)2]nNR2-, -[C(R2)2]nO[C(R2)2]n-, - [C(R2)2]nNR2[C(R2)2]n-, -[C(R2)2]nN[C(R2)2R1][C(R2)2]n-, -[C(R2)2]nO[C(R2)2]nCONR2[C(R2)2]n-, -[C(R2)2]nNR2[C(R2)2]nCONR2[C(R2)2]n-, -[C(R2)2]nNR2COO[C(R2)2]n-, -[C(R2)2]nCO[C(R2)2]n-, -[C(R2)2]nCOO[C(R2)2]n-, -C(R2)=C(R29CONR2[C(R2)2]n o -C(R2)=N- NR2CO[C(R2)2]n; X es H, Hal, A, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2SO2A, CO2 o SO2NR2; R1 es un carbociclo o heterociclo saturado o insaturado mono o bicíclico con 0 a 4 átomos de N, O y/o S, que puede estar mono, bi o trisustituido con R2, Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-Het, -O-[C(R3)2]n-Het, -[C(R3)2]n-cicloalquilo, OR2, N(R2)2, NO2, CN, -[C(R2)2]nCOOR2, O-[C(R2)2]nCOOR2, -[C(R2)2]nCON(R2)2, -[C(R2)2]nCONR2N(R2)2, O-[C(R2)2]oCON(R2)2, O-[C(R2)2]oCONR2N(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2NR2, S(O)mA, =S, =NR3 y/u =O (oxígeno del carbonilo); R2 es H, A, -[C(R3)2]n-Ar', -[C(R3)2]n-Het', -[C(R3)2]n-cicloalquilo, -[C(R3)2]n-OR3, -[C(R3)2]n-COOA o -[C(R3)2]nN(R3)2; R3 es H o A; A es alquilo no ramificado o ramificado con C1-10, en donde uno o dos grupos CH2 pueden estar reemplazados por átomos de O o S y/o por grupos -CH=CH- y/o también 1-7 átomos de H pueden estar reemplazados por F; Ar es fenilo, naftilo o bifenilo insustituido o mono, di o trisustituido con Hal, A, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2N(R2)2, S(O)mA, -[C(R3)2]n-COOR2 u -O[C(R3)2]o-COOR2; Ar' es fenilo, naftilo o bifenilo insustituido o mono, di o trisustituido con Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2N(R3)2, S(O)mA, -[C(R3)2]n-COOR3 u -O[C(R3)2]o-COOR3; Het es un heterociclo saturado o insaturado mono o bicíclico con 1 a 4 átomos de N, O y/o S, que puede estar mono, bi o trisustituido con R2, Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-Het, -[C(R3)2]n-cicloalquilo, OR2, N(R2)2, NO2, CN, -[C(R2)2]nCOOR2, O--[C(R2)2]nCOOR2, -[C(R2)2]nCON(R2)2, -[C(R2)2]nCONR2N(R2)2, O-[C(R2)2]oCON(R2)2, O-[C(R2)2]oCONR2N(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2NR2, S(O)MA y/u =O (oxígeno del carbonilo); Het' es un heterociclo saturado o insaturado mono o bicíclico con 1 a 4 átomos de N, O y/o S, que puede estar mono, bi o trisustituido con R3, Hal, A, OR2, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, COR3, SO2NR3, S(O)mA, =S, =NR3 y/u =O (oxígeno del carbonilo), Hal es F, Cl, Br o I; m es 0, 1 o 2; n es 0, 1, 2, 3 o 4; o es 1, 2 o 3; así como sus derivados, sales, solvatos y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones.
ARP050102033A 2004-06-15 2005-05-18 3-aminoindazoles, un procedimiento de preparcion, uso de los compuestos para preparar medicamentos, dichos medicamentos y un compuesto intermediario AR050155A1 (es)

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DE102004028862A DE102004028862A1 (de) 2004-06-15 2004-06-15 3-Aminoindazole

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AR050155A1 true AR050155A1 (es) 2006-10-04

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US (1) US7872039B2 (es)
EP (1) EP1765788B1 (es)
JP (1) JP5128939B2 (es)
AR (1) AR050155A1 (es)
AT (1) ATE432924T1 (es)
AU (1) AU2005254617B2 (es)
CA (1) CA2570264C (es)
DE (2) DE102004028862A1 (es)
ES (1) ES2326897T3 (es)
WO (1) WO2005123688A2 (es)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6180731A (ja) * 1984-09-28 1986-04-24 Toshiba Corp 管球の製造方法
DE102004051277A1 (de) * 2004-10-21 2006-04-27 Merck Patent Gmbh Heterocyclische Carbonylverbindungen
DE102006005179A1 (de) * 2006-02-06 2007-08-09 Merck Patent Gmbh Aminoindazolderivate
DE102006005180A1 (de) * 2006-02-06 2007-08-09 Merck Patent Gmbh Indazol-heteroaryl-derivate
JP5255559B2 (ja) * 2006-03-31 2013-08-07 アボット・ラボラトリーズ インダゾール化合物
EP2044018A1 (en) 2006-07-11 2009-04-08 Pfizer Japan, Inc. Substituted n-bicyclicalkyl bicyclic carboxyamide compounds
DE102006033140A1 (de) 2006-07-18 2008-01-24 Merck Patent Gmbh Aminoindazolharnstoffderivate
TW200829578A (en) 2006-11-23 2008-07-16 Astrazeneca Ab Chemical compounds 537
JO2754B1 (en) 2006-12-21 2014-03-15 استرازينكا ايه بي Amylendazoleil derivatives for the treatment of glucocorticoid-mediated disorders
WO2008079073A1 (en) * 2006-12-22 2008-07-03 Astrazeneca Ab Indazolyl sulphonamide derivatives for the treatment of glucocorticoid receptor mediated disorders
DE102007002717A1 (de) * 2007-01-18 2008-07-24 Merck Patent Gmbh Heterocyclische Indazolderivate
DE102007022565A1 (de) 2007-05-14 2008-11-20 Merck Patent Gmbh Heterocyclische Indazolderivate
RU2487873C2 (ru) * 2007-06-08 2013-07-20 Эбботт Лэборетриз 5-замещенные индазолы в качестве ингибиторов киназы
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
WO2009133831A1 (ja) 2008-04-28 2009-11-05 旭化成ファーマ株式会社 フェニルプロピオン酸誘導体及びその用途
US20100080786A1 (en) 2008-05-20 2010-04-01 Markus Berger Phenyl or Pyridinyl Substituted Indazoles Derivatives
ES2548141T3 (es) 2008-11-20 2015-10-14 Glaxosmithkline Llc Compuestos químicos
EP2382197B1 (en) * 2008-12-30 2016-10-05 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
JP2012521429A (ja) * 2009-03-23 2012-09-13 メルク・シャープ・エンド・ドーム・コーポレイション 疼痛治療用のｐ２ｘ３受容体アンタゴニスト
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
AT509045B1 (de) 2010-01-29 2011-06-15 Planta Naturstoffe Vertriebsges M B H Verbindungen zur behandlung von asthma bronchiale
CA2786314A1 (en) * 2010-02-25 2011-09-01 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
KR20130006664A (ko) * 2010-03-16 2013-01-17 다나-파버 캔서 인스티튜트 인크. 인다졸 화합물 및 그의 용도
JP2013525438A (ja) * 2010-04-29 2013-06-20 アメリカ合衆国 ヒトピルビン酸キナーゼ活性剤
PE20140011A1 (es) 2010-09-03 2014-01-31 Forma Tm Llc Compuestos y composiciones novedosos para la inhibicion de nampt
GB2483736B (en) 2010-09-16 2012-08-29 Aragon Pharmaceuticals Inc Estrogen receptor modulators and uses thereof
AU2012300317B2 (en) * 2011-08-26 2016-12-01 Neupharma, Inc. Certain chemical entities, compositions, and methods
CN104080455B (zh) 2011-09-14 2018-07-31 润新生物公司 某些化学实体、组合物及方法
JP5827849B2 (ja) * 2011-09-20 2015-12-02 サノフイ Ｎ−［４−（１Ｈ−ピラゾロ［３，４−ｂ］ピラジン−６−イル）−フェニル］−スルホンアミド及び薬剤としてのその使用
CA2856291C (en) 2011-11-17 2020-08-11 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
US9670180B2 (en) 2012-01-25 2017-06-06 Neupharma, Inc. Certain chemical entities, compositions, and methods
JP6154887B2 (ja) * 2012-03-20 2017-06-28 セラゴン ファーマシューティカルズ，インク． エストロゲン受容体モジュレーターおよびその使用
EP2897618B1 (en) 2012-09-24 2021-11-17 Neupharma, Inc. Certain chemical entities, compositions, and methods
WO2014063068A1 (en) 2012-10-18 2014-04-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
WO2014075077A1 (en) 2012-11-12 2014-05-15 Neupharma, Inc. Certain chemical entities, compositions, and methods
TW201427658A (zh) 2012-12-10 2014-07-16 Merck Sharp & Dohme 藉由投予升糖素受體拮抗劑及膽固醇吸收抑制劑治療糖尿病之方法
TWI644899B (zh) 2013-02-04 2018-12-21 健生藥品公司 Ｆｌａｐ調節劑
EP3070085B1 (en) 2013-02-04 2019-01-09 Janssen Pharmaceutica NV Flap modulators
EP3057956B1 (en) 2013-10-18 2021-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
EP3097091A1 (en) * 2014-01-24 2016-11-30 AbbVie Inc. 6-phenyl- or 6-(pyridin-3-yl)indazole derivatives and methods of use
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
KR101731624B1 (ko) 2014-07-01 2017-05-04 광주과학기술원 세포 리프로그래밍 유도용 조성물
WO2016105528A2 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
JP6861166B2 (ja) 2015-03-27 2021-04-21 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド サイクリン依存性キナーゼの阻害剤
WO2016161571A1 (en) 2015-04-08 2016-10-13 Merck Sharp & Dohme Corp. Indazole and azaindazole btk inhibitors
CN106279119B (zh) * 2015-05-27 2020-06-16 上海海和药物研究开发有限公司 一种新型激酶抑制剂的制备及其应用
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
AU2016319125B2 (en) 2015-09-09 2021-04-08 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
DE102015012050A1 (de) * 2015-09-15 2017-03-16 Merck Patent Gmbh Verbindungen als ASIC-Inhibitoren und deren Verwendungen
SG11201901355SA (en) 2016-08-30 2019-03-28 Regeneron Pharma Methods of treating severe insulin resistance by interfering with glucagon receptor signaling
JOP20190053A1 (ar) 2016-09-23 2019-03-21 Novartis Ag مركبات أزا إندازول للاستخدام في إصابات الأوتار و/ أو الرباط
CA3033249A1 (en) * 2016-09-23 2018-03-29 Novartis Ag Indazole compounds for use in tendon and/or ligament injuries
EP3529278A1 (en) 2016-10-20 2019-08-28 Regeneron Pharmaceuticals, Inc. Methods of lowering blood glucose levels
CA3072103A1 (en) 2017-08-21 2019-02-28 Microbiotix, Inc. Metabolically stable n-acylaminooxadiazoles useful as antibacterial agents
EP3672620A1 (en) 2017-08-22 2020-07-01 Regeneron Pharmaceuticals, Inc. Methods of treating urea cycle disorders by interfering with glucagon receptor signaling
EP3543231A1 (en) * 2018-03-19 2019-09-25 ETH Zurich Compounds for treating cns- and neurodegenerative diseases
WO2021007477A1 (en) 2019-07-11 2021-01-14 E-Scape Bio, Inc. Indazoles and azaindazoles as lrrk2 inhibitors

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2971842A (en) * 1956-03-21 1961-02-14 Gen Aniline & Film Corp Light sensitive layers for photomechanical reproduction
US2996467A (en) * 1957-03-04 1961-08-15 Dow Chemical Co Asphalt-oil-rubber composition
DE1280878B (de) * 1961-11-30 1968-10-24 Smith Kline French Lab 3-Aminoindazole
PE20020451A1 (es) * 2000-09-15 2002-06-06 Vertex Pharma Compuestos de pirazol utiles como inhibidores de cinasa proteina
US20030114448A1 (en) * 2001-05-31 2003-06-19 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
WO2003051847A1 (en) * 2001-12-19 2003-06-26 Smithkline Beecham P.L.C. (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors
TW200306819A (en) * 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
ES2411655T3 (es) * 2002-05-17 2013-07-08 Pfizer Italia S.R.L. Derivados de aminoindazol activos como inhibidores de quinasas, procedimiento para su preparación y composiciones farmacéuticas que los comprenden
CA2497351C (fr) * 2002-09-05 2012-08-21 Aventis Pharma S.A. Nouveaux derives d'aminoindazoles a titre de medicaments et compositions pharmaceutiques les renfermant
EP1562935B1 (de) * 2002-10-28 2006-09-06 Bayer HealthCare AG Heteroaryloxy-substituierte phenylaminopyrimidine als rho-kinaseinhibitoren
EP1638941B1 (en) * 2003-05-22 2010-06-02 Abbott Laboratories Indazole, benzisoxazole, and benzisothiazole kinase inhibitors
US7297709B2 (en) * 2003-05-22 2007-11-20 Abbott Laboratories Indazole, benzisoxazole, and benzisothiazole kinase inhibitors
US7560467B2 (en) * 2003-06-19 2009-07-14 Smithkline Beecham Corporation Indazolo-tetrahydropyrimidine-carboxamide derivative kinase inhibitors
SE0301906D0 (sv) * 2003-06-26 2003-06-26 Astrazeneca Ab New compounds
JP2007500700A (ja) * 2003-07-29 2007-01-18 スミスクライン ビーチャム コーポレーション 化合物

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DE502005007427D1 (de) 2009-07-16
US20070232620A1 (en) 2007-10-04
US7872039B2 (en) 2011-01-18
CA2570264C (en) 2013-06-25
ATE432924T1 (de) 2009-06-15
AU2005254617B2 (en) 2011-05-26
AU2005254617A1 (en) 2005-12-29
DE102004028862A1 (de) 2005-12-29
EP1765788A2 (de) 2007-03-28
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CA2570264A1 (en) 2005-12-29

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