CN110944995B - 5-溴-2,6-二(1h-吡唑-1-基)嘧啶-4-胺和新盐的晶型 - Google Patents

5-溴-2,6-二(1h-吡唑-1-基)嘧啶-4-胺和新盐的晶型 Download PDF

Info

Publication number
CN110944995B
CN110944995B CN201880035190.7A CN201880035190A CN110944995B CN 110944995 B CN110944995 B CN 110944995B CN 201880035190 A CN201880035190 A CN 201880035190A CN 110944995 B CN110944995 B CN 110944995B
Authority
CN
China
Prior art keywords
seq
amino acid
acid sequence
cancer
crystalline form
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
CN201880035190.7A
Other languages
English (en)
Chinese (zh)
Other versions
CN110944995A (zh
Inventor
崔凯
孔维勇
J·C·卡斯特罗-帕罗米诺拉里亚
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.)
Novartis AG
Palobiofarma SL
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 CN110944995A publication Critical patent/CN110944995A/zh
Application granted granted Critical
Publication of CN110944995B publication Critical patent/CN110944995B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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)
CN201880035190.7A 2017-05-31 2018-05-30 5-溴-2,6-二(1h-吡唑-1-基)嘧啶-4-胺和新盐的晶型 Active CN110944995B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2017086624 2017-05-31
CNPCT/CN2017/086624 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 (2)

Publication Number Publication Date
CN110944995A CN110944995A (zh) 2020-03-31
CN110944995B true CN110944995B (zh) 2024-03-12

Family

ID=62778954

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880035190.7A Active CN110944995B (zh) 2017-05-31 2018-05-30 5-溴-2,6-二(1h-吡唑-1-基)嘧啶-4-胺和新盐的晶型

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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1438890A (zh) * 2000-02-25 2003-08-27 弗·哈夫曼-拉罗切有限公司 腺苷受体调制剂
CN102892761A (zh) * 2010-03-31 2013-01-23 帕罗生物制药有限公司 4-氨基嘧啶衍生物和它们作为腺苷a2a 受体拮抗剂
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 (35)

* 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
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1438890A (zh) * 2000-02-25 2003-08-27 弗·哈夫曼-拉罗切有限公司 腺苷受体调制剂
CN102892761A (zh) * 2010-03-31 2013-01-23 帕罗生物制药有限公司 4-氨基嘧啶衍生物和它们作为腺苷a2a 受体拮抗剂
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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
罗杰英等.现代物理药剂学理论与实践.《现代物理药剂学理论与实践》.上海科学技术文献出版社,2005,第294-295页. *

Also Published As

Publication number Publication date
AU2018277241B2 (en) 2021-03-04
RU2019138329A (ru) 2021-07-01
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
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
CN111148745A (zh) Fgfr抑制剂的结晶形式及其制备方法
US11654144B2 (en) Crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1- yl)pyrimidin-4-amine and new salts
JP2022500406A (ja) 抗ウイルス性ピリドピラジンジオン化合物
JP7690284B2 (ja) Ido阻害剤の非晶質形態および結晶形態
TWI558399B (zh) 癌症之組合療法
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
JP2024119868A (ja) 病態および状態の処置に使用するための、エナンチオマー的に精製されたgperアゴニスト
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
JP7448541B2 (ja) 選択的エストロゲン受容体分解剤の新規な塩
CN115667241B (zh) TrkA抑制剂
CN110290808B (zh) 1-(4-氨基-5-溴-6-(1h-吡唑-1-基)嘧啶-2-基)-1h-吡唑-4-醇及其在治疗癌症中的用途
WO2021050580A1 (en) Crystalline form of a multi-tyrosine kinase inhibitor, method of preparation, and use thereof
JPWO2019006283A5 (enExample)
CN102046637B (zh) N-[[4-氟-2-(5-甲基-1H-1,2,4-三唑-1-基)苯基]甲基]-4,6,7,9-四氢-3-羟基-9,9-二甲基-4-氧代-嘧啶并[2,1-c][1,4]噁嗪-2-甲酰胺钠盐一水合物的晶体形式
HK40064763A (en) Crystalline form of a multi-tyrosine kinase inhibitor, method of preparation, and use thereof
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
HK40048894A (en) Antiviral pyridopyrazinedione compounds
EA049146B1 (ru) Аморфные и кристаллические формы ido-ингибиторов

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant