BR112015018751A2 - derivados de piridazinona macrocíclicos - Google Patents

derivados de piridazinona macrocíclicos

Info

Publication number
BR112015018751A2
BR112015018751A2 BR112015018751A BR112015018751A BR112015018751A2 BR 112015018751 A2 BR112015018751 A2 BR 112015018751A2 BR 112015018751 A BR112015018751 A BR 112015018751A BR 112015018751 A BR112015018751 A BR 112015018751A BR 112015018751 A2 BR112015018751 A2 BR 112015018751A2
Authority
BR
Brazil
Prior art keywords
formula
pyridazinone derivatives
macrocyclic
compounds
present
Prior art date
Application number
BR112015018751A
Other languages
English (en)
Inventor
Jorand-Lebrun Catherine
Kulkarni Santosh
Christmann-Franck Serge
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of BR112015018751A2 publication Critical patent/BR112015018751A2/pt

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    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/504—Pyridazines; Hydrogenated pyridazines forming part of bridged ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • 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
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • 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]
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
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    • A61P37/02—Immunomodulators
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
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    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/18—Bridged systems
    • 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
    • C07D471/22—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 systems contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Immunology (AREA)
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  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
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  • Rheumatology (AREA)
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  • Cardiology (AREA)
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  • Hospice & Palliative Care (AREA)
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Abstract

resumo patente de invenção: "derivados de piridazinona macrocíclicos". a presente invenção refere-se a compostos de fórmula (i) em que r1, r2, r3, r4, l e z têm o significado dado na reivindicação 1 e seu uso na profilaxia e no tratamento de doenças. a presente invenção refere-se ainda a um kit e a uma composição farmacêutica compreendendo os compostos de fórmula (i) e/ou tautômeros, solvatos, sais e estereoisômeros dos mesmos farmaceuticamente úteis, bem como a um processo de síntese do composto de fórmula (i). 1/1
BR112015018751A 2013-02-07 2014-02-07 derivados de piridazinona macrocíclicos BR112015018751A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13154391 2013-02-07
PCT/EP2014/000337 WO2014121942A1 (en) 2013-02-07 2014-02-07 Macrocyclic pyridazinone derivatives

Publications (1)

Publication Number Publication Date
BR112015018751A2 true BR112015018751A2 (pt) 2017-07-18

Family

ID=47681773

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015018751A BR112015018751A2 (pt) 2013-02-07 2014-02-07 derivados de piridazinona macrocíclicos

Country Status (23)

Country Link
US (2) US9550794B2 (pt)
EP (1) EP2953952B1 (pt)
JP (1) JP6267729B2 (pt)
KR (1) KR102216812B1 (pt)
CN (1) CN105008371B (pt)
AU (1) AU2014214254B2 (pt)
BR (1) BR112015018751A2 (pt)
CA (1) CA2900442C (pt)
DK (1) DK2953952T3 (pt)
ES (1) ES2639717T3 (pt)
HK (1) HK1216645A1 (pt)
HR (1) HRP20171302T1 (pt)
HU (1) HUE035919T2 (pt)
IL (1) IL240291B (pt)
LT (1) LT2953952T (pt)
MX (1) MX367897B (pt)
PL (1) PL2953952T3 (pt)
PT (1) PT2953952T (pt)
RS (1) RS56269B1 (pt)
RU (1) RU2660435C2 (pt)
SG (1) SG11201506099XA (pt)
SI (1) SI2953952T1 (pt)
WO (1) WO2014121942A1 (pt)

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PT2953944T (pt) * 2013-02-07 2017-08-01 Merck Patent Gmbh Derivados de piridazinona-amidas
EP3253764B1 (en) * 2015-02-05 2021-06-09 Merck Patent GmbH Macrocyclic compounds as irak1/4 inhibitors and uses thereof
EP3253763B1 (en) * 2015-02-06 2020-09-30 Merck Patent GmbH Pyridazinone macrocycles as irak inhibitors and uses thereof
LT3286181T (lt) 2015-04-22 2021-04-26 Rigel Pharmaceuticals, Inc. Pirazolo junginiai ir junginių gamybos bei naudojimo būdas
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
EP3684366A4 (en) 2017-09-22 2021-09-08 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES OF THE LATEST
IL273432B (en) 2017-09-22 2022-09-01 Kymera Therapeutics Inc Protein compounds and their uses
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
SG11202005912PA (en) 2017-12-26 2020-07-29 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2019140387A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
US11485743B2 (en) 2018-01-12 2022-11-01 Kymera Therapeutics, Inc. Protein degraders and uses thereof
CA3102762A1 (en) * 2018-06-04 2019-12-12 Ohio State Innovation Foundation Eaat2 activators and methods of using thereof
WO2020010177A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Tricyclic crbn ligands and uses thereof
TWI721483B (zh) 2018-07-13 2021-03-11 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
US11352350B2 (en) 2018-11-30 2022-06-07 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
WO2020260252A1 (en) 2019-06-24 2020-12-30 Boehringer Ingelheim International Gmbh New macrocyclic compounds and derivatives as egfr inhibitors
CA3152264A1 (en) 2019-08-30 2021-03-04 Rigel Pharmaceuticals, Inc. Pyrazole compounds, formulations thereof, and a method for using the compounds and/or formulations
BR112022011651A2 (pt) 2019-12-17 2022-08-23 Kymera Therapeutics Inc Degradadores de irak e usos dos mesmos
EP4076524A4 (en) 2019-12-17 2023-11-29 Kymera Therapeutics, Inc. IRAQ DEGRADERS AND USES THEREOF
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
CN114057771B (zh) * 2020-12-03 2023-10-03 北京鞍石生物科技有限责任公司 大环化合物及其制备方法和应用
WO2024099395A1 (en) * 2022-11-10 2024-05-16 Beigene, Ltd. Compounds for the degradation of egfr kinase

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CA2458533C (en) * 2001-10-09 2011-01-04 Tularik Inc. Imidazole derivates as anti-inflammatory agents
MXPA05009972A (es) * 2003-03-18 2005-11-04 Kowa Co Derivado de fenilpiridazina soluble en agua y medicina que contiene el mismo.
JP2010502717A (ja) * 2006-09-07 2010-01-28 バイオジェン・アイデック・エムエイ・インコーポレイテッド インターロイキン１受容体関連キナーゼの調節物質
MX2011002470A (es) * 2008-09-08 2011-04-05 Merck Patent Gmbh Pirimidinas macrociclicas como inhibidores de aurora cinasa.
SI2655357T1 (sl) * 2010-12-20 2016-10-28 Merck Serono S.A. Derivati indazolil triazola kot zaviralci IRAK

Also Published As

Publication number Publication date
CN105008371A (zh) 2015-10-28
RU2015137756A (ru) 2017-03-13
US20150376206A1 (en) 2015-12-31
EP2953952A1 (en) 2015-12-16
CA2900442A1 (en) 2014-08-14
KR102216812B1 (ko) 2021-02-18
JP6267729B2 (ja) 2018-01-24
LT2953952T (lt) 2017-08-25
SI2953952T1 (sl) 2017-10-30
US20170143713A1 (en) 2017-05-25
US10064861B2 (en) 2018-09-04
MX2015010128A (es) 2017-07-26
AU2014214254A1 (en) 2015-09-17
MX367897B (es) 2019-09-11
AU2014214254B2 (en) 2018-03-29
ES2639717T3 (es) 2017-10-30
WO2014121942A1 (en) 2014-08-14
EP2953952B1 (en) 2017-06-07
KR20150118980A (ko) 2015-10-23
PT2953952T (pt) 2017-09-11
IL240291A0 (en) 2015-09-24
DK2953952T3 (en) 2017-08-28
RU2660435C2 (ru) 2018-07-06
RS56269B1 (sr) 2017-11-30
IL240291B (en) 2019-06-30
HUE035919T2 (en) 2018-05-28
US9550794B2 (en) 2017-01-24
HRP20171302T1 (hr) 2017-10-20
JP2016507539A (ja) 2016-03-10
PL2953952T3 (pl) 2017-10-31
CA2900442C (en) 2021-09-21
CN105008371B (zh) 2018-09-18
HK1216645A1 (zh) 2016-11-25
SG11201506099XA (en) 2015-09-29

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