BR112017013031A2 - derivados de imidazopiridazina ligados à heterociclila como inibidores de pi3kbeta - Google Patents

derivados de imidazopiridazina ligados à heterociclila como inibidores de pi3kbeta

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Publication number
BR112017013031A2
BR112017013031A2 BR112017013031A BR112017013031A BR112017013031A2 BR 112017013031 A2 BR112017013031 A2 BR 112017013031A2 BR 112017013031 A BR112017013031 A BR 112017013031A BR 112017013031 A BR112017013031 A BR 112017013031A BR 112017013031 A2 BR112017013031 A2 BR 112017013031A2
Authority
BR
Brazil
Prior art keywords
heterocyclyl
inhibitors
pi3kbeta
compounds
imidazopyridazine derivatives
Prior art date
Application number
BR112017013031A
Other languages
English (en)
Inventor
Gabriel Marcel DEMESTRE Christophe
Meyer Christophe
Jean-Claude Berthelot Didier
Thérèse Jeanne Pasquier Elisabeth
Jean Maurice MERCEY Guillaume
Noëlle Constance Pilatte Isabelle
Anne Mevellec Laurence
Meerpoel Lieven
Alexis Georges Querolle Olivier
René Angibaud Patrick
Coupa Sophie
Sophie Poncelet Virginie
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of BR112017013031A2 publication Critical patent/BR112017013031A2/pt

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    • 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
    • C07D405/10—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 linked by a carbon chain containing aromatic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • A61P13/00—Drugs for disorders of the urinary system
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    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

a presente invenção refere-se a derivados de imidazopiridazina ligados à heterociclila da fórmula (i) em que as variáveis têm o significado definido nas reivindicações. os compostos de acordo com a presente invenção são úteis como inibido-res de pi3kß. a invenção também se refere a processos para a prepa-ração de tais compostos novos, a composições farmacêuticas com-preendendo os referidos compostos como ingrediente ativo, bem como ao uso dos referidos compostos como medicamento.
BR112017013031A 2014-12-19 2015-12-18 derivados de imidazopiridazina ligados à heterociclila como inibidores de pi3kbeta BR112017013031A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14199344 2014-12-19
PCT/EP2015/080623 WO2016097359A1 (en) 2014-12-19 2015-12-18 Heterocyclyl linked imidazopyridazine derivatives as pi3kbeta inhibitors

Publications (1)

Publication Number Publication Date
BR112017013031A2 true BR112017013031A2 (pt) 2018-01-02

Family

ID=52134004

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017013031A BR112017013031A2 (pt) 2014-12-19 2015-12-18 derivados de imidazopiridazina ligados à heterociclila como inibidores de pi3kbeta

Country Status (18)

Country Link
US (1) US10202387B2 (pt)
EP (1) EP3233839B1 (pt)
JP (1) JP6586463B2 (pt)
KR (1) KR20170095243A (pt)
CN (1) CN107108633B (pt)
AU (1) AU2015366202B2 (pt)
BR (1) BR112017013031A2 (pt)
CA (1) CA2967546A1 (pt)
DK (1) DK3233839T3 (pt)
EA (1) EA029519B1 (pt)
ES (1) ES2760507T3 (pt)
HR (1) HRP20192162T1 (pt)
HU (1) HUE047382T2 (pt)
IL (1) IL252868B (pt)
LT (1) LT3233839T (pt)
MX (1) MX2017008076A (pt)
SI (1) SI3233839T1 (pt)
WO (1) WO2016097359A1 (pt)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA037401B1 (ru) 2015-10-09 2021-03-24 Янссен Фармацевтика Нв Производные хиноксалина и пиридопиразина в качестве ингибиторов pi3k
MX2018015707A (es) 2016-06-16 2019-03-21 Janssen Pharmaceutica Nv Derivados biciclicos de piridina, pirazina y pirimidina como inhibidores de pi3k beta.
US11130751B2 (en) 2017-03-29 2021-09-28 Janssen Pharmaceutica Nv Quinoxaline and pyridopyrazine derivatives as PI3K-beta inhibitors

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US20070078136A1 (en) 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
PE20070978A1 (es) * 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
JP2009544723A (ja) 2006-07-24 2009-12-17 スミスクライン・ビーチャム・コーポレイション Ｐｉ３キナーゼ阻害剤としてのチオゾリジンジオン誘導体
US20110021513A1 (en) 2006-09-07 2011-01-27 Biogen Idec Ma Inc. Modulators of interleukin-1 receptor-associated kinase
AU2008250328A1 (en) * 2007-05-09 2008-11-20 Novartis Ag Substituted imidazopyridazines as PI3K lipid kinase inhibitors
US20110046127A1 (en) * 2007-11-08 2011-02-24 Paolo Pevarello Imidazopyridazines for Use as Protein Kinase Inhibitors
CA2706946A1 (en) * 2007-11-28 2009-06-04 Schering Corporation 2-fluoropyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
KR20100128305A (ko) * 2008-02-28 2010-12-07 노파르티스 아게 Ｃ-ｍｅｔ 티로신 키나제 매개 질환의 치료를 위한 이미다조[1,2-ｂ]피리다진 유도체
WO2010007099A1 (en) * 2008-07-15 2010-01-21 Cellzome Limited 2-aminoimidazo[1,2-b]pyridazine derivatives as pi3k inhibitors
MX2012002066A (es) 2009-08-17 2012-03-29 Intellikine Inc Compuestos heterociclicos y usos de los mismos.
DE102009049679A1 (de) * 2009-10-19 2011-04-21 Merck Patent Gmbh Pyrazolopyrimidinderivate
WO2011058109A1 (en) 2009-11-12 2011-05-19 Ucb Pharma S.A. Fused bicyclic pyrrole and imidazole derivatives as kinase inhibitors
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TWI574962B (zh) * 2012-11-14 2017-03-21 加拓科學公司 作爲ｐｉ３激酶調節劑的芳雜環化合物及其使用方法和用途

Also Published As

Publication number Publication date
CN107108633B (zh) 2020-05-12
IL252868B (en) 2020-01-30
MX2017008076A (es) 2018-01-09
HRP20192162T1 (hr) 2020-02-21
WO2016097359A1 (en) 2016-06-23
EP3233839A1 (en) 2017-10-25
SI3233839T1 (sl) 2019-12-31
JP6586463B2 (ja) 2019-10-02
EA201791397A1 (ru) 2017-10-31
KR20170095243A (ko) 2017-08-22
AU2015366202A1 (en) 2017-05-25
IL252868A0 (en) 2017-08-31
EP3233839B1 (en) 2019-09-25
CN107108633A (zh) 2017-08-29
AU2015366202B2 (en) 2020-01-02
CA2967546A1 (en) 2016-06-23
ES2760507T3 (es) 2020-05-14
HUE047382T2 (hu) 2020-04-28
US10202387B2 (en) 2019-02-12
US20180057496A1 (en) 2018-03-01
DK3233839T3 (da) 2019-12-09
JP2017538765A (ja) 2017-12-28
LT3233839T (lt) 2019-12-10
EA029519B1 (ru) 2018-04-30

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