CN102762557B - 三唑并吡啶 - Google Patents

三唑并吡啶 Download PDF

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Publication number
CN102762557B
CN102762557B CN201080061524.1A CN201080061524A CN102762557B CN 102762557 B CN102762557 B CN 102762557B CN 201080061524 A CN201080061524 A CN 201080061524A CN 102762557 B CN102762557 B CN 102762557B
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Prior art keywords
phenyl
triazolo
amino
pyridin
general formula
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Expired - Fee Related
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CN201080061524.1A
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Chinese (zh)
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CN102762557A (zh
Inventor
V·舒尔策
M·科皮茨
D·科泽蒙德
H·斯基洛克
B·巴德尔
P·利瑙
A·M·温内尔
H·布里姆
S·霍尔顿
G·西迈斯特
S·佩克特
U·伯默
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Bayer Pharma AG
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Bayer Pharma AG
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    • 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
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201080061524.1A 2009-11-30 2010-11-17 三唑并吡啶 Expired - Fee Related CN102762557B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09075535.6 2009-11-30
EP09075535A EP2343297A1 (en) 2009-11-30 2009-11-30 Triazolopyridines
PCT/EP2010/006994 WO2011063908A1 (en) 2009-11-30 2010-11-17 Triazolopyridines

Publications (2)

Publication Number Publication Date
CN102762557A CN102762557A (zh) 2012-10-31
CN102762557B true CN102762557B (zh) 2015-10-07

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CN201080061524.1A Expired - Fee Related CN102762557B (zh) 2009-11-30 2010-11-17 三唑并吡啶

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US (1) US9676766B2 (enExample)
EP (2) EP2343297A1 (enExample)
JP (1) JP5805653B2 (enExample)
KR (1) KR20120115290A (enExample)
CN (1) CN102762557B (enExample)
AR (1) AR079166A1 (enExample)
AU (1) AU2010324155B2 (enExample)
BR (1) BR112012012906A2 (enExample)
CA (1) CA2781915A1 (enExample)
CL (1) CL2012001391A1 (enExample)
CR (1) CR20120295A (enExample)
CU (1) CU24100B1 (enExample)
CY (1) CY1115866T1 (enExample)
DK (1) DK2507235T3 (enExample)
DO (1) DOP2012000150A (enExample)
EA (1) EA022353B1 (enExample)
EC (1) ECSP12011935A (enExample)
ES (1) ES2525069T3 (enExample)
GT (1) GT201200165A (enExample)
HN (1) HN2012001162A (enExample)
HR (1) HRP20141093T1 (enExample)
IL (1) IL219750A (enExample)
MA (1) MA33768B1 (enExample)
MX (1) MX2012006252A (enExample)
MY (1) MY160325A (enExample)
NZ (1) NZ600229A (enExample)
PE (1) PE20121509A1 (enExample)
PH (1) PH12012501055A1 (enExample)
PL (1) PL2507235T3 (enExample)
PT (1) PT2507235E (enExample)
RS (1) RS53670B1 (enExample)
SI (1) SI2507235T1 (enExample)
TN (1) TN2012000265A1 (enExample)
UA (1) UA108486C2 (enExample)
WO (1) WO2011063908A1 (enExample)
ZA (1) ZA201203806B (enExample)

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EP2343294A1 (en) 2009-11-30 2011-07-13 Bayer Schering Pharma AG Substituted triazolopyridines
EP2343297A1 (en) 2009-11-30 2011-07-13 Bayer Schering Pharma AG Triazolopyridines
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TWI541243B (zh) 2010-09-10 2016-07-11 拜耳知識產權公司 經取代咪唑并嗒
EP2651947B1 (en) 2010-12-17 2014-12-10 Bayer Intellectual Property GmbH 6-thio-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
CN103429592A (zh) 2010-12-17 2013-12-04 拜耳知识产权有限责任公司 作为mps-1和tkk抑制剂用于治疗过度增殖性病症的6-取代的咪唑并吡嗪
EP2651948A1 (en) 2010-12-17 2013-10-23 Bayer Intellectual Property GmbH Imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment hyperproliferative disorders
CN103370322B (zh) 2010-12-17 2016-02-10 拜耳知识产权有限责任公司 在过度增殖性病症的治疗中用作mps-1和tkk抑制剂的2-取代的咪唑并吡嗪
EP2651950A1 (en) 2010-12-17 2013-10-23 Bayer Intellectual Property GmbH 6 substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
JP5824065B2 (ja) 2010-12-17 2015-11-25 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 過剰増殖性障害の治療におけるｍｐｓ−１およびｔｋｋ阻害剤として使用するための６置換イミダゾピラジン
CN103582632B (zh) 2011-03-31 2015-08-19 拜耳知识产权有限责任公司 取代的苯并咪唑
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PL2699575T3 (pl) * 2011-04-21 2015-08-31 Bayer Ip Gmbh Triazolopirydyny
WO2012160029A1 (en) 2011-05-23 2012-11-29 Bayer Intellectual Property Gmbh Substituted triazolopyridines
UA112096C2 (uk) * 2011-12-12 2016-07-25 Байєр Інтеллектуал Проперті Гмбх Заміщені триазолопіридини та їх застосування як інгібіторів ttk
JP6166289B2 (ja) 2012-03-14 2017-07-19 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 置換イミダゾピリダジン
NZ703020A (en) * 2012-07-10 2017-08-25 Bayer Pharma AG Method for preparing substituted triazolopyridines
WO2014020043A1 (en) 2012-08-02 2014-02-06 Bayer Pharma Aktiengesellschaft Combinations for the treatment of cancer
WO2014020041A1 (en) 2012-08-02 2014-02-06 Bayer Pharma Aktiengesellschaft Combinations for the treatment of cancer
HK1215250A1 (zh) 2013-01-30 2016-08-19 Bayer Pharma Aktiengesellschaft 氨基取代的异噻唑
AR096469A1 (es) * 2013-06-06 2015-12-30 Bayer Pharma AG Composiciones farmacéuticas que comprenden compuestos del tipo triazolpiridinas
WO2014195274A1 (en) * 2013-06-07 2014-12-11 Bayer Pharma Aktiengesellschaft Substituted triazolopyridines
PT3008062T (pt) 2013-06-11 2017-06-07 Bayer Pharma AG Derivados de profármaco de triazolopiridinas substituídas
MA38656A1 (fr) 2013-06-11 2018-05-31 Bayer Pharma AG Combinaisons pour le traitement du cancer comprenant un inhibiteur de la kinase mps-1 et un inhibiteur de la mitose
EP2980088A1 (en) 2014-07-28 2016-02-03 Bayer Pharma Aktiengesellschaft Amino-substituted isothiazoles
CN106132963B (zh) 2014-04-07 2019-08-06 荷兰转化研究中心有限责任公司 (5,6-二氢)嘧啶并[4,5-e]吲嗪
EP2977375A1 (en) 2014-07-25 2016-01-27 Bayer Pharma Aktiengesellschaft Amino-substituted isoxazoles
EP2977376A1 (en) 2014-07-25 2016-01-27 Bayer Pharma Aktiengesellschaft Amino-substituted isoxazoles
EP2977377A1 (en) 2014-07-25 2016-01-27 Bayer Pharma Aktiengesellschaft Amino-substituted isoxazoles
CN107567503B (zh) 2015-04-17 2022-03-22 荷兰转化研究中心有限责任公司 用于ttk抑制剂化疗的预后生物标记
KR101686411B1 (ko) * 2015-12-28 2016-12-14 한국원자력의학원 피리딘계 유도체를 포함하는 암 예방 또는 치료용 조성물
CN107641118B (zh) * 2016-07-22 2020-11-06 爱科诺生物医药股份有限公司 具有细胞坏死抑制活性的化合物及其组合物和应用
JP7023217B2 (ja) 2017-12-01 2022-02-21 ダイキン工業株式会社 アルカリ接触する表面を有する構成要素
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US12522583B2 (en) 2018-11-07 2026-01-13 Dana-Farber Cancer Institute, Inc. Benzimidazole derivatives and aza-benzimidazole derivatives as Janus kinase 2 inhibitors and uses thereof
US12415816B2 (en) 2018-11-07 2025-09-16 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
TW202204350A (zh) 2020-05-06 2022-02-01 美商雅捷可斯治療公司 作為ｊａｋ２抑制劑之６－雜芳基氧基苯并咪唑及氮雜苯并咪唑
US12043632B2 (en) 2020-12-23 2024-07-23 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors
US20240123043A1 (en) * 2021-02-22 2024-04-18 Orgenesis Inc. Pharmaceutical compositions comprising ranpirnase
WO2023086320A1 (en) 2021-11-09 2023-05-19 Ajax Therapeutics, Inc. Forms and compositions of inhibitors of jak2
CA3234638A1 (en) 2021-11-09 2023-05-19 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors

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