TWI814725B - 5-溴-2,6-二(1h-吡唑-1-基)嘧啶-4-胺及新穎鹽類之結晶型 - Google Patents

5-溴-2,6-二(1h-吡唑-1-基)嘧啶-4-胺及新穎鹽類之結晶型 Download PDF

Info

Publication number
TWI814725B
TWI814725B TW107118638A TW107118638A TWI814725B TW I814725 B TWI814725 B TW I814725B TW 107118638 A TW107118638 A TW 107118638A TW 107118638 A TW107118638 A TW 107118638A TW I814725 B TWI814725 B TW I814725B
Authority
TW
Taiwan
Prior art keywords
amino acid
seq
acid sequence
cancer
crystalline form
Prior art date
Application number
TW107118638A
Other languages
English (en)
Chinese (zh)
Other versions
TW201920152A (zh
Inventor
拉里亞 朱里歐 希薩 卡斯裘-帕羅米諾
崔凱
孔維勇
Original Assignee
瑞士商諾華公司
西班牙商派洛拜爾佛瑪公司
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 瑞士商諾華公司, 西班牙商派洛拜爾佛瑪公司 filed Critical 瑞士商諾華公司
Publication of TW201920152A publication Critical patent/TW201920152A/zh
Application granted granted Critical
Publication of TWI814725B publication Critical patent/TWI814725B/zh

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803Immunoglobulins [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
    • C07K16/2818Immunoglobulins [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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803Immunoglobulins [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
    • C07K16/2827Immunoglobulins [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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/505Medicinal preparations containing antigens or antibodies comprising antibodies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/545Medicinal preparations containing antigens or antibodies characterised by the dose, timing or administration schedule
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/50Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/56Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
    • C07K2317/565Complementarity 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)
TW107118638A 2017-05-31 2018-05-31 5-溴-2,6-二(1h-吡唑-1-基)嘧啶-4-胺及新穎鹽類之結晶型 TWI814725B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
WOPCT/CN2017/086624 2017-05-31
CN2017086624 2017-05-31
??PCT/CN2017/086624 2017-05-31

Publications (2)

Publication Number Publication Date
TW201920152A TW201920152A (zh) 2019-06-01
TWI814725B true TWI814725B (zh) 2023-09-11

Family

ID=62778954

Family Applications (1)

Application Number Title Priority Date Filing Date
TW107118638A TWI814725B (zh) 2017-05-31 2018-05-31 5-溴-2,6-二(1h-吡唑-1-基)嘧啶-4-胺及新穎鹽類之結晶型

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
IL291721B2 (en) 2024-07-01
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
TW202136274A (zh) Kras g12c抑制劑
TW202233625A (zh) Fgfr抑制劑及其製造及使用方法
CN110573504A (zh) 作为激酶抑制剂的杂环酰胺
JP2022500406A (ja) 抗ウイルス性ピリドピラジンジオン化合物
KR102630575B1 (ko) Ido 억제제의 무정형 및 결정질 형태
WO2020114388A1 (zh) 取代的吡唑并[1,5-a]吡啶化合物及包含该化合物的组合物及其用途
US11654144B2 (en) Crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1- yl)pyrimidin-4-amine and new salts
CN105829285A (zh) 喹唑啉酮和异喹啉酮衍生物
JP2024509268A (ja) 結晶形、それらを含有する組成物、及びそれらの使用方法
AU2017298035B2 (en) Succinate forms and compositions of Bruton's tyrosine kinase inhibitors
WO2025059366A1 (en) Ras inhibitors
TWI771280B (zh) 經取代之5,6-二氫-6-苯基苯并[f]異喹啉-2-胺化合物之固體形式
TW202216682A (zh) Alk5 抑製劑、共軛物及其用途
WO2025101776A1 (en) Heterocycles and uses thereof
JP2020507569A (ja) 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
JPWO2019006283A5 (enExample)
TW202440565A (zh) 結晶鹽形式
WO2025261505A1 (zh) 一种抗cdh17的抗体药物偶联物及其应用
TW202413348A (zh) Cdk抑制劑及其製備及使用方法
CN115151306A (zh) (r)-n-(4-氯苯基)-2-((1s,4s)-4-(6-氟喹啉-4-基)环己基)丙酰胺的盐/共晶
RU2023129737A (ru) Кристаллические формы 5"бром"2,6"ди(1h"пиразол"1"ил)пиримидин"4" амина и новых солей

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees