JP6268183B2 - Ｐｉ３キナーゼモジュレータとしてのヘテロ芳香族化合物、及びその使用方法 - Google Patents

Ｐｉ３キナーゼモジュレータとしてのヘテロ芳香族化合物、及びその使用方法 Download PDF

Info

Publication number
JP6268183B2
JP6268183B2 JP2015541973A JP2015541973A JP6268183B2 JP 6268183 B2 JP6268183 B2 JP 6268183B2 JP 2015541973 A JP2015541973 A JP 2015541973A JP 2015541973 A JP2015541973 A JP 2015541973A JP 6268183 B2 JP6268183 B2 JP 6268183B2
Authority
JP
Japan
Prior art keywords
cycloalkyl
cancer
alkyl
alkylene
mmol
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
JP2015541973A
Other languages
English (en)
Japanese (ja)
Other versions
JP2015536994A5 (enExample
JP2015536994A (ja
Inventor
シ、ニン
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sunshine Lake Pharma Co Ltd
Original Assignee
Sunshine Lake Pharma Co Ltd
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 Sunshine Lake Pharma Co Ltd filed Critical Sunshine Lake Pharma Co Ltd
Publication of JP2015536994A publication Critical patent/JP2015536994A/ja
Publication of JP2015536994A5 publication Critical patent/JP2015536994A5/ja
Application granted granted Critical
Publication of JP6268183B2 publication Critical patent/JP6268183B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/435—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
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015541973A 2012-11-14 2013-11-10 Ｐｉ３キナーゼモジュレータとしてのヘテロ芳香族化合物、及びその使用方法 Active JP6268183B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261726139P 2012-11-14 2012-11-14
US61/726,139 2012-11-14
PCT/US2013/069366 WO2014078211A1 (en) 2012-11-14 2013-11-10 Heteroaromatic compounds as pi3 kinase modulators and methods of use

Publications (3)

Publication Number Publication Date
JP2015536994A JP2015536994A (ja) 2015-12-24
JP2015536994A5 JP2015536994A5 (enExample) 2016-12-22
JP6268183B2 true JP6268183B2 (ja) 2018-01-24

Family

ID=50681898

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2015541973A Active JP6268183B2 (ja) 2012-11-14 2013-11-10 Ｐｉ３キナーゼモジュレータとしてのヘテロ芳香族化合物、及びその使用方法

Country Status (15)

Country Link
US (1) US9926324B2 (enExample)
EP (2) EP2919784B1 (enExample)
JP (1) JP6268183B2 (enExample)
KR (1) KR102148679B1 (enExample)
CN (1) CN104755085B (enExample)
AU (1) AU2013345107B2 (enExample)
BR (1) BR112015006726B1 (enExample)
CA (1) CA2889346C (enExample)
ES (1) ES2661380T3 (enExample)
MY (1) MY180641A (enExample)
RU (1) RU2665036C9 (enExample)
SG (1) SG11201502725TA (enExample)
TW (1) TWI574962B (enExample)
WO (1) WO2014078211A1 (enExample)
ZA (1) ZA201502575B (enExample)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104496940B (zh) * 2014-01-06 2017-03-15 广东东阳光药业有限公司 一种制备bcr‑abl抑制剂中间体的方法
US9868737B2 (en) * 2014-06-17 2018-01-16 Cisen Pharmaceutical Co., Ltd. Pyridino[1,2-A]pyrimidone analogue used as MTOR/P13K inhibitor
CN105503877A (zh) 2014-09-24 2016-04-20 和记黄埔医药（上海）有限公司 咪唑并哒嗪类化合物及其用途
EP3233862B1 (en) 2014-12-19 2019-07-03 Janssen Pharmaceutica NV Imidazopyridazine derivatives as pi3kbeta inhibitors
MX2017008076A (es) * 2014-12-19 2018-01-09 Janssen Pharmaceutica Nv DERIVADOS DE IMIDAZOPIRIDAZINA ENLAZADOS A HETEROCICLILO COMO INHIBIDORES DE PI3Kß.
LT3472160T (lt) * 2016-06-16 2021-04-26 Janssen Pharmaceutica Nv Biciklinio piridino, pirazino ir pirimidino dariniai kaip pi3k beta inhibitoriai
WO2018017633A1 (en) 2016-07-21 2018-01-25 Bristol-Myers Squibb Company TGF Beta RECEPTOR ANTAGONISTS
EP3527570A4 (en) 2016-10-14 2020-04-15 Jiangsu Hengrui Medicine Co., Ltd. FIVE-LINKED HETERARYARYLE CYCLE BRIDGE DERIVATIVE, METHOD FOR PREPARING SAME, AND MEDICAL USE THEREOF
HUE068842T2 (hu) * 2016-11-28 2025-01-28 Praxis Prec Medicines Inc Vegyületek és alkalmazási eljárásaik
CN108164525B (zh) * 2016-12-08 2020-09-08 沈阳药科大学 一种抗肿瘤化合物的制备方法和用途
MX393780B (es) 2017-01-17 2025-03-24 Heparegenix Gmbh Inhibidores de proteina cinasa para promover la regeneracion hepatica o reducir o prevenir la muerte de hepatocitos
FR3064364A1 (fr) * 2017-03-27 2018-09-28 S.P.C.M. Sa Methode de dosage de polymeres cationiques
TW202208354A (zh) 2020-04-29 2022-03-01 美商傳達治療有限公司 ＰＩ３Ｋα抑制劑及其使用方法
EP4399196A4 (en) * 2021-09-10 2025-08-06 Relay Therapeutics Inc PI3K-ALPHA INHIBITORS AND METHODS OF USE THEREOF
EP4522583A2 (en) * 2022-05-10 2025-03-19 Relay Therapeutics, Inc. Pi3k alpha inhibitors and methods of use thereof
CN120737113B (zh) * 2025-09-03 2025-11-21 湖北师范大学 一种三唑并哒嗪类化合物区域选择性c3-h炔基化的方法

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2036924C1 (ru) * 1989-01-31 1995-06-09 Такеда Кемикал Индастриз ЛТД Способ получения производных имидазо (1,2-b)пиридазина или их солей и производные имидазо (1,2-b)пиридазина или их соли
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
US5994341A (en) 1993-07-19 1999-11-30 Angiogenesis Technologies, Inc. Anti-angiogenic Compositions and methods for the treatment of arthritis
DE69417918T2 (de) 1993-11-30 2000-01-05 Mcgill University, Montreal Dna methyltransferase inhibierung
US5578716A (en) 1993-12-01 1996-11-26 Mcgill University DNA methyltransferase antisense oligonucleotides
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
US6268137B1 (en) 1996-05-22 2001-07-31 Methylgene, Inc. Specific inhibitors of DNA methyl transferase
US6020318A (en) 1997-05-30 2000-02-01 Methylgene, Inc. DNA methyltransferase genomic sequences and antisense oligonucleotides
EP0985035A2 (en) 1997-05-30 2000-03-15 McGILL UNIVERSITY Dna methyltransferase genomic sequences and antisense oligonucleotides
US6066625A (en) 1998-02-03 2000-05-23 Methylgene, Inc. Optimized antisense oligonucleotides complementary to DNA methyltransferase sequences
US6953783B1 (en) 1998-10-19 2005-10-11 Methylgene, Inc. Modulation of gene expression by combination therapy
EP1173562A2 (en) 1999-05-03 2002-01-23 Methylgene, Inc. Inhibition of histone deacetylase
ATE514674T1 (de) 1999-11-23 2011-07-15 Methylgene Inc Inhibitoren für histone-deacetylase
ATE489360T1 (de) 2000-03-24 2010-12-15 Methylgene Inc Inhibitoren der histon-deacetylase
EP2093292A2 (en) 2000-03-24 2009-08-26 Methylgene, Inc. Inhibition of specific histone deacetylase isoforms
WO2001090077A1 (en) * 2000-05-19 2001-11-29 Guilford Pharmaceuticals, Inc. Sulfonamide and carbamide derivatives of 6(5h)phenanthridinones and their uses
US7868204B2 (en) 2001-09-14 2011-01-11 Methylgene Inc. Inhibitors of histone deacetylase
MXPA04002397A (es) 2001-09-14 2004-12-02 Methylgene Inc Inhibidores de histona deacetilasa.
US6897220B2 (en) 2001-09-14 2005-05-24 Methylgene, Inc. Inhibitors of histone deacetylase
WO2004035525A1 (en) 2002-10-17 2004-04-29 Methylgene Inc. Inhibitors of histone deacetylase
AU2004276337B2 (en) 2003-09-24 2009-11-12 Methylgene Inc. Inhibitors of histone deacetylase
EP1735319B1 (en) 2004-03-26 2017-05-03 MethylGene Inc. Inhibitors of histone deacetylase
AU2005266803B2 (en) 2004-07-30 2011-10-27 Methylgene Inc. Inhibitors of VEGF receptor and HGF receptor signaling
WO2007075869A2 (en) 2005-12-23 2007-07-05 Ariad Pharmaceuticals, Inc. Bicyclic heteroaryl compounds
RU2009107705A (ru) * 2006-08-04 2010-09-10 Такеда Фармасьютикал Компани Лимитед (Jp) Конденсированное гетероциклическое соединение и его применение
WO2009039140A1 (en) * 2007-09-17 2009-03-26 Smithkline Beecham Corporation Pyridopyrimidine derivatives as pi3 kinase inhibitors
EP2211615A4 (en) * 2007-10-22 2010-10-13 Glaxosmithkline Llc PYRIDOSULFONAMIDE DERIVATIVES AS PI3 KINASE INHIBITORS
CA2710194C (en) * 2007-12-19 2014-04-22 Amgen Inc. Inhibitors of p13 kinase
WO2009111277A1 (en) * 2008-02-29 2009-09-11 Array Biopharma Inc. Imdizo [4. 5-b] pyridine derivatives used as raf inhibitors
AR071523A1 (es) * 2008-04-30 2010-06-23 Merck Serono Sa Compuestos biciclicos fusionados, un proceso para su preparacion, el compuesto para ser utilizado como medicamento en el tratamiento y profilaxis de enfermedades, una composicion farmaceutica y un conjunto que comprende paquetes separados del compuesto y de un ingrediente activo del medicamento
ES2709108T3 (es) 2009-08-17 2019-04-15 Intellikine Llc Compuestos heterocíclicos y usos de los mismos
ES2593256T3 (es) * 2010-05-21 2016-12-07 Infinity Pharmaceuticals, Inc. Compuestos químicos, composiciones y métodos para las modulaciones de cinasas
UY33597A (es) 2010-09-09 2012-04-30 Irm Llc Compuestos y composiciones como inhibidores de la trk
HRP20220319T1 (hr) 2011-05-19 2022-05-13 Fundación Del Sector Público Estatal Centro Nacional De Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Makrociklički spojevi kao inhibitori protein kinaze
WO2012174312A2 (en) 2011-06-15 2012-12-20 Glaxosmithkline Llc Benzimidazole derivatives as antiviral agents
KR101274986B1 (ko) 2011-07-27 2013-06-17 한국과학기술원 이미다조피리딘 유도체, 이를 포함하는 ＰＩ3Ｋ 및/또는 ｍＴＯＲ 저해제용 약학 조성물 및 ＰＩ3Ｋ 및/또는 ｍＴＯＲ과 연관된 질환 치료용 약학 조성물
GB201205669D0 (en) 2012-03-30 2012-05-16 Agency Science Tech & Res Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof

Also Published As

Publication number Publication date
HK1210956A1 (en) 2016-05-13
EP3299019B1 (en) 2019-10-09
AU2013345107B2 (en) 2016-02-25
CN104755085A (zh) 2015-07-01
US20140134133A1 (en) 2014-05-15
CA2889346C (en) 2018-09-25
TWI574962B (zh) 2017-03-21
BR112015006726B1 (pt) 2021-11-23
ZA201502575B (en) 2016-11-30
EP2919784A4 (en) 2016-07-06
EP2919784B1 (en) 2017-12-20
CN104755085B (zh) 2018-05-01
EP2919784A1 (en) 2015-09-23
ES2661380T3 (es) 2018-03-28
KR102148679B1 (ko) 2020-08-27
WO2014078211A1 (en) 2014-05-22
KR20150083833A (ko) 2015-07-20
EP3299019A1 (en) 2018-03-28
RU2665036C2 (ru) 2018-08-27
TW201422615A (zh) 2014-06-16
AU2013345107A1 (en) 2015-04-30
MY180641A (en) 2020-12-04
US9926324B2 (en) 2018-03-27
JP2015536994A (ja) 2015-12-24
BR112015006726A2 (pt) 2017-08-22
RU2015116102A (ru) 2017-01-10
RU2665036C9 (ru) 2018-11-12
CA2889346A1 (en) 2014-05-22
SG11201502725TA (en) 2015-05-28

Similar Documents

Publication Publication Date Title
JP6268183B2 (ja) Ｐｉ３キナーゼモジュレータとしてのヘテロ芳香族化合物、及びその使用方法
JP6389829B2 (ja) Ｐｉ３キナーゼモジュレータとしてのヘテロ芳香族化合物、及びその使用方法
WO2014089324A1 (en) Substituted cyclic compounds and methods of use
WO2014193647A2 (en) Alkenyl compounds and methods of use
CN103965199B (zh) 一种芳杂环化合物、包含它的药物组合物及其用途
WO2014089280A1 (en) Alkynyl compounds and methods of use
HK1210956B (en) Heteroaromatic compounds as pi3 kinase modulators and methods of use
BR122021014786B1 (pt) Composto, composição farmacêutica, e, uso de um composto ou de uma composição farmacêutica
HK1218385B (en) Heteroaromatic compounds as pi3 kinase modulators

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20161104

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20161104

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20170810

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20170822

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20171019

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20171212

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20171225

R150 Certificate of patent or registration of utility model

Ref document number: 6268183

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313117

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313113

S531 Written request for registration of change of domicile

Free format text: JAPANESE INTERMEDIATE CODE: R313531

S533 Written request for registration of change of name

Free format text: JAPANESE INTERMEDIATE CODE: R313533

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250