JP7161481B2 - １－（４－アミノ－５－ブロモ－６－（１ｈ－ピラゾール－１－イル）ピリミジン－２－イル）－１ｈ－ピラゾール－４－オール及びがんの治療におけるその使用 - Google Patents

１－（４－アミノ－５－ブロモ－６－（１ｈ－ピラゾール－１－イル）ピリミジン－２－イル）－１ｈ－ピラゾール－４－オール及びがんの治療におけるその使用 Download PDF

Info

Publication number
JP7161481B2
JP7161481B2 JP2019542717A JP2019542717A JP7161481B2 JP 7161481 B2 JP7161481 B2 JP 7161481B2 JP 2019542717 A JP2019542717 A JP 2019542717A JP 2019542717 A JP2019542717 A JP 2019542717A JP 7161481 B2 JP7161481 B2 JP 7161481B2
Authority
JP
Japan
Prior art keywords
amino acid
acid sequence
seq
cancer
pyrazol
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.)
Expired - Fee Related
Application number
JP2019542717A
Other languages
English (en)
Japanese (ja)
Other versions
JP2020507569A5 (enExample
JP2020507569A (ja
Inventor
ビリク，サネラ
ゴメス，ジュアン アルバート カマーチョ
スコット キャメロン，ジョン
ラリア，ジュリオ セサー キャストロ－パロミノ
ローランド，ジュニア ハワード，ダニー
Original Assignee
ノバルティス アーゲー
パロビオファルマ，ソシエダッド リミターダ
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 ノバルティス アーゲー, パロビオファルマ，ソシエダッド リミターダ filed Critical ノバルティス アーゲー
Publication of JP2020507569A publication Critical patent/JP2020507569A/ja
Publication of JP2020507569A5 publication Critical patent/JP2020507569A5/ja
Application granted granted Critical
Publication of JP7161481B2 publication Critical patent/JP7161481B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39558—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2827—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against B7 molecules, e.g. CD80, CD86
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/56—Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
    • C07K2317/565—Complementarity determining region [CDR]

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
JP2019542717A 2017-02-10 2018-02-08 １－（４－アミノ－５－ブロモ－６－（１ｈ－ピラゾール－１－イル）ピリミジン－２－イル）－１ｈ－ピラゾール－４－オール及びがんの治療におけるその使用 Expired - Fee Related JP7161481B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762457219P 2017-02-10 2017-02-10
US62/457,219 2017-02-10
PCT/IB2018/050783 WO2018146612A1 (en) 2017-02-10 2018-02-08 1-(4-amino-5-bromo-6-(1 h-pyrazol-1-yl)pyrimidin-2-yl)-1 h-pyrazol-4-ol and use thereof in the treatment of cancer

Publications (3)

Publication Number Publication Date
JP2020507569A JP2020507569A (ja) 2020-03-12
JP2020507569A5 JP2020507569A5 (enExample) 2021-03-18
JP7161481B2 true JP7161481B2 (ja) 2022-10-26

Family

ID=61274309

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2019542717A Expired - Fee Related JP7161481B2 (ja) 2017-02-10 2018-02-08 １－（４－アミノ－５－ブロモ－６－（１ｈ－ピラゾール－１－イル）ピリミジン－２－イル）－１ｈ－ピラゾール－４－オール及びがんの治療におけるその使用

Country Status (15)

Country Link
US (1) US11078191B2 (enExample)
EP (1) EP3579874B1 (enExample)
JP (1) JP7161481B2 (enExample)
KR (1) KR20190115053A (enExample)
CN (1) CN110290808B (enExample)
AU (2) AU2018217963B2 (enExample)
CA (1) CA3051986A1 (enExample)
DK (1) DK3579874T3 (enExample)
ES (1) ES2893006T3 (enExample)
HU (1) HUE057337T2 (enExample)
IL (1) IL268549B (enExample)
PL (1) PL3579874T3 (enExample)
PT (1) PT3579874T (enExample)
SI (1) SI3579874T1 (enExample)
WO (1) WO2018146612A1 (enExample)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108495651A (zh) * 2015-12-17 2018-09-04 诺华股份有限公司 抗pd-1的抗体分子及其用途
US10933064B2 (en) * 2017-05-31 2021-03-02 Novartis Ag Crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine and new salts

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013523711A (ja) 2010-03-31 2013-06-17 パロビオファルマ，エス．エル． アデノシンａ２ａ受容体拮抗薬としての４−アミノピリミジン誘導体

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
IL129299A0 (en) 1999-03-31 2000-02-17 Mor Research Applic Ltd Monoclonal antibodies antigens and diagnosis of malignant diseases
IL149820A0 (en) 2002-05-23 2002-11-10 Curetech Ltd Humanized immunomodulatory monoclonal antibodies for the treatment of neoplastic disease or immunodeficiency
US7119200B2 (en) * 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
ES2367430T3 (es) 2002-12-23 2011-11-03 Wyeth Llc Anticuerpos contra pd-1 y sus usos.
EP3530736A3 (en) 2005-05-09 2019-11-06 ONO Pharmaceutical Co., Ltd. Human monoclonal antibodies to programmed death 1 (pd-1) and methods for treating cancer using anti-pd-1 antibodies alone or in combination with other immunotherapeutics
KR101704734B1 (ko) 2005-07-01 2017-02-09 이. 알. 스퀴부 앤드 선즈, 엘.엘.씨. 예정 사멸 리간드 1 (피디-엘1)에 대한 인간 모노클로날 항체
PT2170959E (pt) 2007-06-18 2014-01-07 Merck Sharp & Dohme Anticorpos para o receptor humano de morte programada pd-1
US8168757B2 (en) 2008-03-12 2012-05-01 Merck Sharp & Dohme Corp. PD-1 binding proteins
WO2010098788A2 (en) 2008-08-25 2010-09-02 Amplimmune, Inc. Pd-i antagonists and methods for treating infectious disease
AU2009290544B2 (en) 2008-09-12 2015-07-16 Oxford University Innovation Limited PD-1 specific antibodies and uses thereof
WO2010036959A2 (en) 2008-09-26 2010-04-01 Dana-Farber Cancer Institute Human anti-pd-1, pd-l1, and pd-l2 antibodies and uses therefor
MX356367B (es) 2008-12-09 2018-05-25 Genentech Inc Anticuerpos anti-pd-l1 y su uso para mejorar la funcion de celulas t.
WO2010089411A2 (en) 2009-02-09 2010-08-12 Universite De La Mediterranee Pd-1 antibodies and pd-l1 antibodies and uses thereof
EP2504028A4 (en) 2009-11-24 2014-04-09 Amplimmune Inc SIMULTANEOUS INHIBITION OF PD-L1 / PD-L2
CN102892786B (zh) 2010-03-11 2016-03-16 Ucb医药有限公司 Pd-1抗体
US8907053B2 (en) 2010-06-25 2014-12-09 Aurigene Discovery Technologies Limited Immunosuppression modulating compounds
CA2833636A1 (en) 2011-04-20 2012-10-26 Amplimmune, Inc. Antibodies and other molecules that bind b7-h1 and pd-1
US8686119B2 (en) 2011-07-24 2014-04-01 Curetech Ltd. Variants of humanized immunomodulatory monoclonal antibodies
BR112014012819B1 (pt) 2011-11-28 2022-08-16 Merck Patent Gmbh Anticorpo anti-pd-l1 ou fragmento de ligação ao antígeno do mesmo e composição
RS61400B1 (sr) 2013-05-02 2021-02-26 Anaptysbio Inc Antitela usmerena protiv programirane smrti-1 (pd-1)
CA3175360C (en) 2013-05-31 2024-05-28 Sorrento Therapeutics, Inc. Antigen binding proteins that bind pd-1
AU2014276440A1 (en) * 2013-06-03 2015-11-05 Novartis Ag Combinations of an anti-PD-L1 antibody and a MEK inhibitor and/or a BRaf inhibitor
WO2014209804A1 (en) 2013-06-24 2014-12-31 Biomed Valley Discoveries, Inc. Bispecific antibodies
SMT202300039T1 (it) 2013-09-13 2023-03-17 Beigene Switzerland Gmbh Anticorpi anti-pd1 e loro uso come terapia e per diagnostica
GB201320729D0 (en) * 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Therapeutic compounds and their use
CR20160319A (es) 2013-12-12 2016-11-08 Jiangsu Hengrui Medicine Co Anticuerpo pd-1, fragmento de union al antigeno de este y uso médico de este
TWI681969B (zh) 2014-01-23 2020-01-11 美商再生元醫藥公司 針對ｐｄ-１的人類抗體
UA122479C2 (uk) 2014-01-24 2020-11-25 Дана-Фарбер Кенсер Інстітьют, Інк. Виділена молекула антитіла, яка зв’язується з людським білком програмованої смерті-1 (pd-1)
TWI693232B (zh) 2014-06-26 2020-05-11 美商宏觀基因股份有限公司 與pd-1和lag-3具有免疫反應性的共價結合的雙抗體和其使用方法
SG11201702401RA (en) * 2014-10-14 2017-04-27 Novartis Ag Antibody molecules to pd-l1 and uses thereof
TWI595006B (zh) 2014-12-09 2017-08-11 禮納特神經系統科學公司 抗ｐｄ－１抗體類和使用彼等之方法
WO2017025918A1 (en) * 2015-08-11 2017-02-16 Novartis Ag 5-bromo-2,6-di-(lh-pyrazol-l-yl)pyrimidin-4-amine for use in the treatment of cancer

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013523711A (ja) 2010-03-31 2013-06-17 パロビオファルマ，エス．エル． アデノシンａ２ａ受容体拮抗薬としての４−アミノピリミジン誘導体

Also Published As

Publication number Publication date
CN110290808B (zh) 2023-07-11
AU2018217963A1 (en) 2019-08-08
IL268549B (en) 2021-10-31
EP3579874A1 (en) 2019-12-18
CN110290808A (zh) 2019-09-27
RU2019128199A3 (enExample) 2021-05-14
EP3579874B1 (en) 2021-07-21
RU2019128199A (ru) 2021-03-10
IL268549A (en) 2019-09-26
HUE057337T2 (hu) 2022-05-28
US20190359600A1 (en) 2019-11-28
DK3579874T3 (da) 2021-10-11
US11078191B2 (en) 2021-08-03
PT3579874T (pt) 2021-10-07
PL3579874T3 (pl) 2022-02-28
WO2018146612A1 (en) 2018-08-16
AU2020256467B2 (en) 2022-03-03
AU2020256467A1 (en) 2020-11-12
AU2018217963B2 (en) 2020-11-19
JP2020507569A (ja) 2020-03-12
CA3051986A1 (en) 2018-08-16
ES2893006T3 (es) 2022-02-07
KR20190115053A (ko) 2019-10-10
SI3579874T1 (sl) 2021-11-30

Similar Documents

Publication Publication Date Title
JP7840847B2 (ja) Ｒａｓ阻害剤
US12516044B2 (en) Heterocyclic compounds as immunomodulators
TWI747879B (zh) 作為抗病毒劑之四環吡啶酮化合物
JP6437441B2 (ja) 抗ｃｄ２０抗体およびｐｉ３キナーゼ選択的阻害剤の組み合わせ
US11234977B2 (en) Fused tricyclic pyrazolo-dihydropyrazinyl-pyridone compounds as antivirals
JP6980649B2 (ja) イソキノリノン誘導体の固体形態、それを製造する方法、それを含む組成物、及びそれを使用する方法
TW202340208A (zh) 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物
TW202448871A (zh) 作為sos1抑制劑之唑基吡啶嗒酮醯胺
US10160726B2 (en) Quinolone derivatives as antibacterials
JP2021514982A (ja) インドール−２−カルボニル化合物及びｂ型肝炎治療のためのそれらの使用
UA122126C2 (uk) 1-((3s,4r)-4-(3-фторфеніл)-1-(2-метоксіетил)піролідин-3-іл)-3-(4-метил-3-(2-метилпіримідин-5-іл)-1-феніл-1h-піразол-5-іл)сечовина як інгібітор trka-кінази
KR20190003750A (ko) 암을 치료하기 위한 1-테트라히드로피라닐카르보닐-2,3-디히드로-1h-인돌 화합물
US9469625B2 (en) Organic compounds
KR20230118593A (ko) Alk-5 억제제 및 이의 용도
JP2021512103A (ja) Ｎａｍｐｔ阻害剤を含む抗体薬物複合体（ａｄｃｓ）
TW202115077A (zh) Ｍａｌｔ１抑制劑及其用途
AU2020256467B2 (en) 1-(4-amino-5-bromo-6-(1H-pyrazol-1-yl)pyrimidin-2-yl)-1H-pyrazol-4-ol and use thereof in the treatment of cancer
JP7273732B2 (ja) ５－ブロモ－２，６－ジ（１ｈ－ピラゾール－１－イル）ピリミジン－４－アミン及び新たな塩の結晶形
HK40010513B (en) 1-(4-amino-5-bromo-6-(1 h-pyrazol-1-yl)pyrimidin-2-yl)-1 h-pyrazol-4-ol and use thereof in the treatment of cancer
RU2791531C2 (ru) 1-(4-амино-5-бром-6-(1h-пиразол-1-ил)пиримидин-2-ил)-1h-пиразол-4-ол и его применение в лечении рака
CN101479246A (zh) 氨基-乙基-氨基-芳基(aeaa)化合物和它们的用途
TW202535865A (zh) 泛素特異性加工蛋白酶1 (usp1) 化合物

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210129

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20210129

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20211118

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20211124

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220224

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220419

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220715

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: 20220920

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20221014

R150 Certificate of patent or registration of utility model

Ref document number: 7161481

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees