IL291721B2 - 5-bromo-2'6-D1(1H-pyrazol-1-yl)pyrimidine-4-amine and new salts - Google Patents

5-bromo-2'6-D1(1H-pyrazol-1-yl)pyrimidine-4-amine and new salts

Info

Publication number
IL291721B2
IL291721B2 IL291721A IL29172122A IL291721B2 IL 291721 B2 IL291721 B2 IL 291721B2 IL 291721 A IL291721 A IL 291721A IL 29172122 A IL29172122 A IL 29172122A IL 291721 B2 IL291721 B2 IL 291721B2
Authority
IL
Israel
Prior art keywords
seq
acid sequence
amino acid
crystalline form
cancer
Prior art date
Application number
IL291721A
Other languages
English (en)
Hebrew (he)
Other versions
IL291721B1 (en
IL291721A (en
Original Assignee
Novartis Ag
Palobiofarma Sl
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 Novartis Ag, Palobiofarma Sl filed Critical Novartis Ag
Publication of IL291721A publication Critical patent/IL291721A/en
Publication of IL291721B1 publication Critical patent/IL291721B1/en
Publication of IL291721B2 publication Critical patent/IL291721B2/en

Links

Classifications

    • 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
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IGs], 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 [IGs], 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 [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IGs], 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 [IGs], 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
    • 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
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • 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
    • A61K2039/545—Medicinal preparations containing antigens or antibodies characterised by the dose, timing or administration schedule
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • 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)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Endocrinology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
IL291721A 2017-05-31 2018-05-30 5-bromo-2'6-D1(1H-pyrazol-1-yl)pyrimidine-4-amine and new salts IL291721B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2017086624 2017-05-31
PCT/IB2018/053839 WO2018220546A1 (en) 2017-05-31 2018-05-30 Crystalline forms of 5-bromo-2,6-di(1 h-pyrazol-1-yl)pyrimidin-4-amine and new salts

Publications (3)

Publication Number Publication Date
IL291721A IL291721A (en) 2022-05-01
IL291721B1 IL291721B1 (en) 2024-03-01
IL291721B2 true IL291721B2 (en) 2024-07-01

Family

ID=62778954

Family Applications (2)

Application Number Title Priority Date Filing Date
IL291721A IL291721B2 (en) 2017-05-31 2018-05-30 5-bromo-2'6-D1(1H-pyrazol-1-yl)pyrimidine-4-amine and new salts
IL270795A IL270795B2 (en) 2017-05-31 2018-05-30 -bromo-2'6-D1(1H-pyrsol-1-yl)pyrimidin-4-amine and new salts

Family Applications After (1)

Application Number Title Priority Date Filing Date
IL270795A IL270795B2 (en) 2017-05-31 2018-05-30 -bromo-2'6-D1(1H-pyrsol-1-yl)pyrimidin-4-amine and new salts

Country Status (18)

Country Link
US (2) US10933064B2 (enExample)
EP (1) EP3630751B1 (enExample)
JP (1) JP7273732B2 (enExample)
KR (1) KR20200018503A (enExample)
CN (1) CN110944995B (enExample)
AR (1) AR111906A1 (enExample)
AU (1) AU2018277241B2 (enExample)
BR (1) BR112019025149A2 (enExample)
CA (1) CA3065475A1 (enExample)
CL (2) CL2019003468A1 (enExample)
IL (2) IL291721B2 (enExample)
JO (1) JOP20190279A1 (enExample)
MX (1) MX2021014104A (enExample)
PH (1) PH12019502703A1 (enExample)
RU (2) RU2019138329A (enExample)
TW (1) TWI814725B (enExample)
WO (1) WO2018220546A1 (enExample)
ZA (1) ZA201907610B (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2986067T3 (es) * 2015-12-17 2024-11-08 Novartis Ag Moléculas de anticuerpos frente a PD-1 y usos de las mismas
JOP20190279A1 (ar) * 2017-05-31 2019-11-28 Novartis Ag الصور البلورية من 5-برومو -2، 6-داي (1h-بيرازول -1-يل) بيريميدين -4- أمين وأملاح جديدة
CA3100035A1 (en) 2018-08-27 2020-03-05 Regeneron Pharmaceuticals, Inc. Use of raman spectroscopy in downstream purification

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011121418A1 (en) * 2010-03-31 2011-10-06 Palobiofarma, S.L. 4 - aminopyrimidine derivatives and their as as adenosine a2a receptor antagonists
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

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL129299A0 (en) 1999-03-31 2000-02-17 Mor Research Applic Ltd Monoclonal antibodies antigens and diagnosis of malignant diseases
BR0108611A (pt) * 2000-02-25 2003-05-06 Hoffmann La Roche Moduladores de receptor de adenosina
IL149820A0 (en) 2002-05-23 2002-11-10 Curetech Ltd Humanized immunomodulatory monoclonal antibodies for the treatment of neoplastic disease or immunodeficiency
US7595048B2 (en) 2002-07-03 2009-09-29 Ono Pharmaceutical Co., Ltd. Method for treatment of cancer by inhibiting the immunosuppressive signal induced by PD-1
WO2004056875A1 (en) 2002-12-23 2004-07-08 Wyeth Antibodies against pd-1 and uses therefor
BRPI0417478A (pt) 2003-12-15 2007-05-08 Almirall Prodesfarma Ag 2,6-bis-heteroaril-4-aminopirimidinas como antagonistas de receptor de adenosina
DK2161336T4 (en) 2005-05-09 2017-04-24 Ono Pharmaceutical Co Human monoclonal antibodies for programmed death 1 (PD-1) and methods for treating cancer using anti-PD-1 antibodies alone or in combination with other immunotherapies
RS54271B1 (sr) 2005-07-01 2016-02-29 E. R. Squibb & Sons, L.L.C. Humana monoklonska antitela za ligand programirane smrti 1 (pd-l1)
US20070208040A1 (en) * 2006-03-02 2007-09-06 Elfatih Elzein A2a adenosine receptor antagonists
WO2008110891A2 (en) 2007-03-09 2008-09-18 Orchid Research Laboratories Limited, New heterocyclic compounds
US8153064B2 (en) 2007-03-22 2012-04-10 Doebler Ii Robert W Systems and devices for isothermal biochemical reactions and/or analysis
NZ582150A (en) 2007-06-18 2012-08-31 Msd Oss Bv Antibodies to human programmed death receptor pd-1
WO2009114335A2 (en) 2008-03-12 2009-09-17 Merck & Co., Inc. Pd-1 binding proteins
CN102203125A (zh) 2008-08-25 2011-09-28 安普利穆尼股份有限公司 Pd-1拮抗剂及其使用方法
EP2342229A1 (en) 2008-09-12 2011-07-13 ISIS Innovation Limited Pd-1 specific antibodies and uses thereof
MX2011003195A (es) 2008-09-26 2011-08-12 Dana Farber Cancer Inst Inc Anticuerpos anti-pd-1, pd-l1 y pd-l2 humanos y usos de los mismos.
HRP20170908T1 (hr) 2008-12-09 2017-09-22 F. Hoffmann - La Roche Ag Protutijela anti-pd-l1 i njihova uporaba za poboljšanje funkcije t-stanice
WO2010089411A2 (en) 2009-02-09 2010-08-12 Universite De La Mediterranee Pd-1 antibodies and pd-l1 antibodies and uses thereof
JP2013512251A (ja) 2009-11-24 2013-04-11 アンプリミューン、インコーポレーテッド Ｐｄ−ｌ１／ｐｄ−ｌ２の同時阻害
EP2545078A1 (en) 2010-03-11 2013-01-16 UCB Pharma, S.A. Pd-1 antibody
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
EP2734551B1 (en) 2011-07-24 2018-01-10 Cure Tech Ltd. Variants of humanized immunomodulatory monoclonal antibodies
RS61033B1 (sr) 2011-11-28 2020-12-31 Merck Patent Gmbh Antitela na pd-l1 i njihova upotreba
HRP20210122T1 (hr) 2013-05-02 2021-04-16 Anaptysbio, Inc. Protutijela usmjerena protiv programirane smrti-1 (pd-1)
US9676853B2 (en) 2013-05-31 2017-06-13 Sorrento Therapeutics, Inc. Antigen binding proteins that bind PD-1
WO2014209804A1 (en) 2013-06-24 2014-12-31 Biomed Valley Discoveries, Inc. Bispecific antibodies
SG11201601844TA (en) 2013-09-13 2016-04-28 Beigene Ltd Anti-pd1 antibodies and their use as therapeutics and diagnostics
SG11201604738TA (en) 2013-12-12 2016-07-28 Shanghai Hengrui Pharm Co Ltd Pd-1 antibody, antigen-binding fragment thereof, and medical application thereof
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
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
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
EP3206711B1 (en) 2014-10-14 2023-05-31 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
JP7161481B2 (ja) * 2017-02-10 2022-10-26 ノバルティス アーゲー 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
JOP20190279A1 (ar) * 2017-05-31 2019-11-28 Novartis Ag الصور البلورية من 5-برومو -2، 6-داي (1h-بيرازول -1-يل) بيريميدين -4- أمين وأملاح جديدة

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011121418A1 (en) * 2010-03-31 2011-10-06 Palobiofarma, S.L. 4 - aminopyrimidine derivatives and their as as adenosine a2a receptor antagonists
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

Also Published As

Publication number Publication date
AU2018277241B2 (en) 2021-03-04
RU2019138329A (ru) 2021-07-01
CN110944995B (zh) 2024-03-12
US20200163963A1 (en) 2020-05-28
WO2018220546A1 (en) 2018-12-06
JP2020521774A (ja) 2020-07-27
ZA201907610B (en) 2021-10-27
JP7273732B2 (ja) 2023-05-15
US11654144B2 (en) 2023-05-23
BR112019025149A2 (pt) 2020-06-23
CL2019003468A1 (es) 2020-08-14
IL291721B1 (en) 2024-03-01
CL2021002667A1 (es) 2022-07-01
IL270795B1 (en) 2023-08-01
CA3065475A1 (en) 2018-12-06
PH12019502703A1 (en) 2020-10-26
JOP20190279A1 (ar) 2019-11-28
TWI814725B (zh) 2023-09-11
EP3630751B1 (en) 2024-03-27
CN110944995A (zh) 2020-03-31
RU2019138329A3 (enExample) 2022-02-17
EP3630751A1 (en) 2020-04-08
US10933064B2 (en) 2021-03-02
AR111906A1 (es) 2019-08-28
IL291721A (en) 2022-05-01
TW201920152A (zh) 2019-06-01
US20210145831A1 (en) 2021-05-20
MX2021014104A (es) 2021-12-10
KR20200018503A (ko) 2020-02-19
RU2022102355A (ru) 2022-03-30
IL270795B2 (en) 2023-12-01
AU2018277241A1 (en) 2019-12-12
IL270795A (en) 2020-01-30

Similar Documents

Publication Publication Date Title
CA3069254C (en) Checkpoint inhibitor bispecific antibodies
TWI859319B (zh) 抗ｃｄ７３抗體及組合物
JP7027401B2 (ja) Ｔｉｍ３に対する抗体およびその使用
IL267625A (en) Anti-icos agonist antibodies and uses thereof
EP3615068A1 (en) Bcma-targeting agent, and combination therapy with a gamma secretase inhibitor
JP2022116269A5 (enExample)
RS59688B1 (sr) 5-bromo-2,6-di-(1h-pirazol-1-il)pirimidin-4-amin za upotrebu pri lečenju raka
IL269270B (en) Method and preparations for cellular immunotherapy
CN117222663A (zh) 使用结合nkg2d、cd16和肿瘤相关抗原的多特异性结合蛋白治疗癌症的方法
TWI755406B (zh) 包含pd-1拮抗劑和raf抑制劑的藥物組合的用途
IL291721B2 (en) 5-bromo-2'6-D1(1H-pyrazol-1-yl)pyrimidine-4-amine and new salts
JP2019526595A (ja) 血液癌を治療するための抗ｃｄ２０抗体、ｐｉ３キナーゼ−デルタ阻害剤および抗ｐｄ−１抗体または抗ｐｄ−ｌ１抗体の組み合わせ
JPWO2020132024A5 (enExample)
JP2020521774A5 (enExample)
WO2025036476A1 (en) Anti-b7-h3 antibodies and uses thereof
TW202527997A (zh) 靶向ｅｇｆｒ／ｃ—ｍｅｔ之抗體—藥物結合物以及其製備方法及用途
RU2023129737A (ru) Кристаллические формы 5"бром"2,6"ди(1h"пиразол"1"ил)пиримидин"4" амина и новых солей
JP2020507569A5 (enExample)
EP4118118A1 (en) Antibodies to cd40 with enhanced agonist activity
RU2019128199A (ru) 1-(4-амино-5-бром-6-(1h-пиразол-1-ил)пиримидин-2-ил)-1h-пиразол-4-ол и его применение в лечении рака
CA3232304A1 (en) Use of anti-cd40 antibody
WO2025046898A1 (ja) ３，５－二置換ベンゼンアルキニル化合物と免疫チェックポイント阻害薬を含む癌治療法
HRP20192192T1 (hr) 5-bromo-2,6-di-(1h-pirazol-1-il)pirimidin-4-amin za uporabu u liječenju raka
RU2021106602A (ru) 5-бром-2,6-ди-(1н-пиразол-1-ил)пиримидин-4-амин для применения в лечении рака