BR112017014970A2 - macrociclos de piridazinona como inibidores de irak e usos dos mesmos - Google Patents

macrociclos de piridazinona como inibidores de irak e usos dos mesmos

Info

Publication number
BR112017014970A2
BR112017014970A2 BR112017014970A BR112017014970A BR112017014970A2 BR 112017014970 A2 BR112017014970 A2 BR 112017014970A2 BR 112017014970 A BR112017014970 A BR 112017014970A BR 112017014970 A BR112017014970 A BR 112017014970A BR 112017014970 A2 BR112017014970 A2 BR 112017014970A2
Authority
BR
Brazil
Prior art keywords
macrocycles
pyridazinone
irak inhibitors
irak
inhibitors
Prior art date
Application number
BR112017014970A
Other languages
English (en)
Other versions
BR112017014970B1 (pt
Inventor
Goutopoulos Andreas
Jorand-Lebrun Catherine
Yu Henry
Lan Ruoxi
Chen Xiaoling
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 BR112017014970A2 publication Critical patent/BR112017014970A2/pt
Publication of BR112017014970B1 publication Critical patent/BR112017014970B1/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
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • 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
    • 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
    • C07D487/12—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
    • 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
    • C07D498/16—Peri-condensed systems
    • 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
    • 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
    • C07D498/22—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 four or more hetero rings

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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Nutrition Science (AREA)
  • Communicable Diseases (AREA)

Abstract

a presente invenção refere-se a compostos da fórmula i e composições farmaceuticamente aceitáveis dos mesmos, úteis como inibidores de irak.
BR112017014970-2A 2015-02-06 2016-02-05 Macrociclos de piridazinona como inibidores de irak, seus usos, e composição farmacêutica BR112017014970B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562112793P 2015-02-06 2015-02-06
US62/112,793 2015-02-06
PCT/US2016/016708 WO2016127024A1 (en) 2015-02-06 2016-02-05 Pyridazinone macrocycles as irak inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
BR112017014970A2 true BR112017014970A2 (pt) 2018-03-27
BR112017014970B1 BR112017014970B1 (pt) 2022-11-16

Family

ID=55436166

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017014970-2A BR112017014970B1 (pt) 2015-02-06 2016-02-05 Macrociclos de piridazinona como inibidores de irak, seus usos, e composição farmacêutica

Country Status (15)

Country Link
US (2) US9624246B2 (pt)
EP (1) EP3253763B1 (pt)
JP (1) JP6920202B2 (pt)
KR (1) KR102551597B1 (pt)
CN (1) CN107428765B (pt)
AU (1) AU2016215184B2 (pt)
BR (1) BR112017014970B1 (pt)
CA (1) CA2970550C (pt)
ES (1) ES2841452T3 (pt)
HK (1) HK1246287A1 (pt)
IL (1) IL253519B (pt)
MX (1) MX2017009624A (pt)
RU (1) RU2708066C2 (pt)
SG (1) SG11201704651UA (pt)
WO (1) WO2016127024A1 (pt)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016127024A1 (en) * 2015-02-06 2016-08-11 Merck Patent Gmbh Pyridazinone macrocycles as irak inhibitors and uses thereof
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
WO2019120267A1 (zh) * 2017-12-22 2019-06-27 成都先导药物开发股份有限公司 一种咪唑并[1,2-b]哒嗪大环类激酶抑制剂
JP7328987B6 (ja) * 2018-04-05 2023-10-25 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｉｉ型ｉｒａｋ阻害剤としてのヘテロアリール化合物及びその使用
TWI842978B (zh) 2018-07-13 2024-05-21 美商基利科學股份有限公司 衍生物
WO2020036979A1 (en) 2018-08-13 2020-02-20 Gilead Sciences, Inc. Pyrrolo[1,2-b]pyridazine derivatives as irak4 inhibitors
TWI727392B (zh) 2018-08-13 2021-05-11 美商基利科學股份有限公司 噻二唑irak4抑制劑
WO2020036830A1 (en) 2018-08-13 2020-02-20 Gilead Sciences, Inc. Pyrrolo[1,2-b]pyridazine derivatives as irak4 inhibitors
US11998534B2 (en) * 2020-02-12 2024-06-04 Eubulus Biotherapeutics Inc. GPX4 inhibitor in combination with anticancer agent for treating proliferative disease
CN111603471B (zh) * 2020-06-24 2021-07-09 山东省科学院生物研究所 一种邻二氮杂环化合物在制备抑制tlr4受体的药物中的用途
CA3194090A1 (en) * 2020-09-30 2022-04-07 Takahiko Ito Macrocyclic compound

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000247959A (ja) * 1999-02-26 2000-09-12 Kowa Co ピリダジン−３−オン誘導体及びこれを含有する医薬
JP2010138073A (ja) * 2007-03-30 2010-06-24 Taisho Pharmaceutical Co Ltd ピコリン酸アミド化合物
US8703768B2 (en) * 2010-06-09 2014-04-22 Hoffmann-La Roche Inc. Nitrogen containing heteroaryl compounds
US9586948B2 (en) * 2012-10-08 2017-03-07 Merck Sharp & Dohme Corp. Inhibitors of IRAK4 activity
LT2953944T (lt) * 2013-02-07 2017-07-10 Merck Patent Gmbh Piridazinono amidų dariniai
CN105008371B (zh) * 2013-02-07 2018-09-18 默克专利股份公司 大环哒嗪酮衍生物
WO2016127024A1 (en) * 2015-02-06 2016-08-11 Merck Patent Gmbh Pyridazinone macrocycles as irak inhibitors and uses thereof

Also Published As

Publication number Publication date
JP6920202B2 (ja) 2021-08-18
JP2018505166A (ja) 2018-02-22
EP3253763B1 (en) 2020-09-30
WO2016127024A1 (en) 2016-08-11
CN107428765A (zh) 2017-12-01
IL253519A0 (en) 2017-09-28
KR20170113551A (ko) 2017-10-12
EP3253763A1 (en) 2017-12-13
BR112017014970B1 (pt) 2022-11-16
ES2841452T3 (es) 2021-07-08
US20170173019A1 (en) 2017-06-22
AU2016215184B2 (en) 2020-11-12
AU2016215184A1 (en) 2017-06-29
CN107428765B (zh) 2020-12-29
US10517872B2 (en) 2019-12-31
US9624246B2 (en) 2017-04-18
RU2017130761A (ru) 2019-03-06
NZ732527A (en) 2022-03-25
RU2017130761A3 (pt) 2019-07-17
CA2970550A1 (en) 2016-08-11
KR102551597B1 (ko) 2023-07-05
RU2708066C2 (ru) 2019-12-04
CA2970550C (en) 2023-09-19
SG11201704651UA (en) 2017-07-28
HK1246287A1 (zh) 2018-09-07
IL253519B (en) 2021-01-31
MX2017009624A (es) 2017-11-20
US20160229871A1 (en) 2016-08-11

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