JP7138641B2 - Malt1阻害剤としてのピラゾール誘導体 - Google Patents

Malt1阻害剤としてのピラゾール誘導体 Download PDF

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JP7138641B2
JP7138641B2 JP2019533465A JP2019533465A JP7138641B2 JP 7138641 B2 JP7138641 B2 JP 7138641B2 JP 2019533465 A JP2019533465 A JP 2019533465A JP 2019533465 A JP2019533465 A JP 2019533465A JP 7138641 B2 JP7138641 B2 JP 7138641B2
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Prior art keywords
pyridin
trifluoromethyl
pyrazole
carboxamide
triazol
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JP2020514267A (ja
JP2020514267A5 (enExample
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ル,ティアンバオ
ダグラス アリソン,ブレット
ケント バーベイ,ジョセフ
ジェイ. コンノリー,ピーター
デイビット カミングス,マックスウェル
ディールス,ガストン
パトリック エドワーズ,ジェームズ
ディー. クロイター,ケビン
フィリッパー,ウルライク
シェン,ファン
ウィルヘルムス ジョン フィッツゲラルド スリング,ヨハネス
ウ,トンフェイ
ジャン-クロード ベルテロット,ディディエ
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ヤンセン ファーマシューティカ エヌ.ベー.
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    • 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
    • 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
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic 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
    • A61K31/535—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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
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    • 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
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    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
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    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2019533465A 2016-12-21 2017-12-20 Malt1阻害剤としてのピラゾール誘導体 Active JP7138641B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662437384P 2016-12-21 2016-12-21
US62/437,384 2016-12-21
PCT/US2017/067516 WO2018119036A1 (en) 2016-12-21 2017-12-20 Pyrazole derivatives as malt1 inhibitors

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JP2020514267A JP2020514267A (ja) 2020-05-21
JP2020514267A5 JP2020514267A5 (enExample) 2021-02-04
JP7138641B2 true JP7138641B2 (ja) 2022-09-16

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US (2) US10954214B2 (enExample)
EP (1) EP3558969B1 (enExample)
JP (1) JP7138641B2 (enExample)
KR (1) KR102583317B1 (enExample)
CN (1) CN110214136A (enExample)
AR (1) AR110421A1 (enExample)
AU (2) AU2017382185C1 (enExample)
BR (1) BR112019012355A2 (enExample)
CA (1) CA3048027A1 (enExample)
CL (1) CL2019001709A1 (enExample)
CO (1) CO2019006622A2 (enExample)
EA (1) EA201991503A1 (enExample)
ES (1) ES2992411T3 (enExample)
IL (1) IL267343B2 (enExample)
MA (1) MA47125A (enExample)
MX (2) MX392673B (enExample)
PE (1) PE20191755A1 (enExample)
PH (1) PH12019501212A1 (enExample)
TN (1) TN2019000192A1 (enExample)
TW (1) TWI795381B (enExample)
UA (1) UA127920C2 (enExample)
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Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170107216A1 (en) 2015-10-19 2017-04-20 Incyte Corporation Heterocyclic compounds as immunomodulators
MD3377488T2 (ro) 2015-11-19 2023-02-28 Incyte Corp Compuși heterociclici ca imunomodulatori
ES2916874T3 (es) 2015-12-17 2022-07-06 Incyte Corp Derivados de N-fenil-piridina-2-carboxamida y su uso como moduladores de la interacción proteína/proteína PD-1/PD-L1
CA3009474A1 (en) 2015-12-22 2017-06-29 Incyte Corporation Heterocyclic compounds as immunomodulators
ES2906460T3 (es) 2016-05-06 2022-04-18 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
EP3464279B1 (en) 2016-05-26 2021-11-24 Incyte Corporation Heterocyclic compounds as immunomodulators
SG11201811414TA (en) 2016-06-20 2019-01-30 Incyte Corp Heterocyclic compounds as immunomodulators
MA45669A (fr) 2016-07-14 2019-05-22 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
US20180057486A1 (en) 2016-08-29 2018-03-01 Incyte Corporation Heterocyclic compounds as immunomodulators
TWI795381B (zh) 2016-12-21 2023-03-11 比利時商健生藥品公司 作為malt1抑制劑之吡唑衍生物
WO2018119286A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
US10308644B2 (en) 2016-12-22 2019-06-04 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018119221A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Pyridine derivatives as immunomodulators
WO2018119236A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
RU2764243C2 (ru) 2017-09-22 2022-01-14 ДЖУБИЛАНТ ЭПИПЭД ЭлЭлСи Гетероциклические соединения в качестве ингибиторов PAD
CN111225915B (zh) 2017-10-18 2023-03-07 朱比兰特埃皮帕德有限公司 作为pad抑制剂的咪唑并吡啶化合物
US11629135B2 (en) 2017-11-06 2023-04-18 Jubilant Prodell Llc Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation
RS65576B1 (sr) 2017-11-24 2024-06-28 Jubilant Episcribe Llc Heterociklična jedinjenja kao inhibitori prmt5
KR20200105678A (ko) 2017-12-28 2020-09-08 더 제너럴 하스피탈 코포레이션 Cbm 시그날로좀 복합체 표적화는 조절 t 세포의 종양 미세환경에 대한 염증유발을 유도함
CN112105610B (zh) 2018-03-13 2024-01-26 朱比连特普罗德尔有限责任公司 作为pd1/pd-l1相互作用/活化的抑制剂的双环化合物
SMT202300065T1 (it) 2018-03-30 2023-05-12 Incyte Corp Composti eterociclici come immunomodulatori
CN112752756B (zh) 2018-05-11 2024-06-25 因赛特公司 作为PD-L1免疫调节剂的四氢-咪唑并[4,5-c]吡啶衍生物
AU2019289223B2 (en) * 2018-06-18 2023-09-21 Janssen Pharmaceutica Nv Pyrazole derivatives as MALT1 inhibitors
EA202190055A1 (ru) * 2018-06-18 2021-04-23 Янссен Фармацевтика Нв Производные пиразола в качестве ингибиторов malt1
TW202045008A (zh) * 2019-02-01 2020-12-16 印度商皮埃企業有限公司 4-取代的異噁唑/異噁唑啉(雜)芳基脒化合物、及其製備與用途
EP3927324A1 (en) 2019-02-22 2021-12-29 Janssen Pharmaceutica NV Pharmaceutical formulations
BR112021016400A2 (pt) * 2019-02-22 2021-10-13 Janssen Pharmaceutica N.V. Forma cristalina de mono-hidrato de 1-(1-oxo-1,2-di-hidroisoquinolin-5-il)-5-(trifluorometil.)-n-(2-(trifluorometil)piridin-4-il)-1h-pirazol-4-carboxamida
US12404260B2 (en) 2019-04-11 2025-09-02 Janssen Pharmaceutica Nv Pyridine rings containing derivatives as MALT1 inhibitors
TW202115059A (zh) 2019-08-09 2021-04-16 美商英塞特公司 Pd—1/pd—l1抑制劑之鹽
JP7559059B2 (ja) 2019-09-30 2024-10-01 インサイト・コーポレイション 免疫調節剤としてのピリド[3,2-d]ピリミジン化合物
WO2021080015A1 (en) * 2019-10-24 2021-04-29 Ono Pharmaceutical Co., Ltd. Modulators of trek (twik related k+ channels) channel function
ES3055177T3 (en) * 2019-10-30 2026-02-10 Biogen Ma Inc Condensed pyridazine or pyrimidine as btk inhibitors
EP4058461A1 (en) 2019-11-11 2022-09-21 Incyte Corporation Salts and crystalline forms of a pd-1/pd-l1 inhibitor
CA3162140A1 (en) 2019-11-22 2021-05-27 Janssen Pharmaceutica Nv Methods for assessing efficacy of malt1 inhibitors using an nf-kb translocation assay
KR20220119037A (ko) 2019-11-22 2022-08-26 얀센 파마슈티카 엔.브이. MALT1 억제제의 효능 평가를 위한 NF-kB 조절 유전자 발현 분석
WO2021138298A1 (en) * 2019-12-30 2021-07-08 Rheos Medicines, Inc. Malt1 modulators and uses thereof
US20230235077A1 (en) 2020-06-24 2023-07-27 The General Hospital Corporation Materials and methods of treating cancer
JP2023539729A (ja) * 2020-08-21 2023-09-19 ヤンセン ファーマシューティカ エヌ.ベー. Malt1阻害剤の非晶質形態及びその製剤
EP4199911A1 (en) * 2020-08-21 2023-06-28 JANSSEN Pharmaceutica NV Pharmaceutical formulations comprising a malt1 inhibitor and a mixture of polyethylene glycol with a fatty acid
WO2022081967A1 (en) * 2020-10-16 2022-04-21 Rheos Medicines, Inc. Malt1 modulators and uses thereof
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
IL302590A (en) 2020-11-06 2023-07-01 Incyte Corp Process for preparing PD-1/PD-L1 inhibitor and salts and crystalline forms thereof
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
JP2023549835A (ja) * 2020-11-12 2023-11-29 モノプテロス セラピューティクス,インコーポレーテッド がんを治療する材料及び方法
GB202018412D0 (en) * 2020-11-23 2021-01-06 Exscientia Ltd Malt-1 modulators ii
WO2022167962A1 (en) * 2021-02-04 2022-08-11 Aurigene Discovery Technologies Limited Substituted pyrazolyl compounds as malt-1 inhibitors
EP4301365A1 (en) * 2021-03-03 2024-01-10 Janssen Pharmaceutica NV Combination therapy using a malt1 inhibitor and a btk inhibitor
KR20230154227A (ko) 2021-03-03 2023-11-07 얀센 파마슈티카 엔브이 치료적 유효 용량의 malt1 억제제 jnj-67856633(1-(1-옥소-1,2-다이하이드로아이소퀴놀린-5-일)-5-(트라이플루오로메틸)-n-(2-(트라이플루오로메틸)피리딘-4-일)-1h-피라졸-4-카르복스아미드)을 사용하는 병태의 치료 방법
CN117120427B (zh) * 2021-06-18 2026-07-21 上海拓界生物医药科技有限公司 一种malt1抑制剂及其制备方法和用途
EP4368618A1 (en) * 2021-07-05 2024-05-15 Betta Pharmaceuticals Co., Ltd Six-membered aryl or heteroaryl amides, and composition and use thereof
CN117715898A (zh) * 2021-07-05 2024-03-15 贝达药业股份有限公司 六元芳基或杂芳基酰胺类化合物及其组合物和用途
WO2023016995A1 (en) 2021-08-09 2023-02-16 Janssen Pharmaceutica Nv Compositions for use in treating b-cell malignancies
CN113912511B (zh) * 2021-11-29 2024-02-13 广东广康生化科技股份有限公司 一种联苯肼酯中间体的合成方法
JP2025501056A (ja) * 2021-12-30 2025-01-17 シャンハイ ハンソー バイオメディカル カンパニー リミテッド 三環系誘導体阻害剤、その製造方法と応用
KR20240144146A (ko) 2022-02-02 2024-10-02 오노 야꾸힝 고교 가부시키가이샤 Malt1 저해약을 유효 성분으로서 포함하는 암 치료제
CN119095837A (zh) * 2022-02-03 2024-12-06 希四克斯探索有限公司 作为malt1抑制剂的杂环衍生物
TW202425968A (zh) * 2022-08-26 2024-07-01 美商熱點醫療公司 吡唑基磺醯胺化合物及其在療法中之用途
TW202430031A (zh) 2022-09-30 2024-08-01 瑞士商先正達農作物保護股份公司 殺微生物之吡唑衍生物
TW202430514A (zh) 2022-09-30 2024-08-01 瑞士商先正達農作物保護股份公司 殺微生物之吡唑衍生物
JP2025539452A (ja) 2022-11-30 2025-12-05 シンジェンタ クロップ プロテクション アクチェンゲゼルシャフト 殺微生物テトラヒドロイソキノリン誘導体
CN118206543A (zh) * 2022-12-15 2024-06-18 江苏恒瑞医药股份有限公司 一种苯并[c][1,2,5]噁二唑化合物的结晶形式及其制备方法
CN118206538A (zh) * 2022-12-15 2024-06-18 江苏恒瑞医药股份有限公司 一种苯并[c][1,2,5]噁二唑化合物与酒石酸复合物及其晶型
CN120418243A (zh) * 2022-12-16 2025-08-01 江苏恒瑞医药股份有限公司 一种Malt1抑制剂的磷酸酯前药
TW202515550A (zh) * 2023-06-29 2025-04-16 大陸商上海翰森生物醫藥科技有限公司 三并環類抑制劑與抗癌劑在製備抗腫瘤藥物中的聯合應用
TW202515873A (zh) * 2023-06-29 2025-04-16 大陸商上海翰森生物醫藥科技有限公司 一種三并環類衍生物抑制劑的晶型及其製備方法
WO2025069270A1 (ja) * 2023-09-27 2025-04-03 日本新薬株式会社 アザインドール化合物及び医薬
AU2024357109A1 (en) 2023-10-06 2026-03-12 Ionctura Sa Combination of roginolisib with a malt1-gls inhibitor
WO2025114167A1 (en) 2023-11-28 2025-06-05 Syngenta Crop Protection Ag Microbiocidal pyrazole derivatives
WO2025174889A1 (en) * 2024-02-13 2025-08-21 Board Of Regents, The University Of Texas System Malt1 and btk dual inhibitors
WO2025191053A1 (en) 2024-03-14 2025-09-18 Syngenta Crop Protection Ag Microbiocidal pyrazole derivatives
WO2025210095A1 (en) 2024-04-03 2025-10-09 Syngenta Crop Protection Ag Microbiocidal tetrahydroisoquinoline compounds
WO2025210096A1 (en) 2024-04-03 2025-10-09 Syngenta Crop Protection Ag Fungicidal compositions

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004098518A2 (en) 2003-05-01 2004-11-18 Bristol-Myers Squibb Company Pyrazole-amide compounds useful as kinase inhibitors
JP2015096499A (ja) 2013-10-11 2015-05-21 田辺三菱製薬株式会社 医薬組成物
WO2015181747A1 (en) 2014-05-28 2015-12-03 Novartis Ag Novel pyrazolo pyrimidine derivatives and their use as malt1 inhibitors

Family Cites Families (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6339099B1 (en) 1997-06-20 2002-01-15 Dupont Pharmaceuticals Company Guanidine mimics as factor Xa inhibitors
GB9721964D0 (en) * 1997-10-16 1997-12-17 Pfizer Ltd Isoquinolines
DK173431B1 (da) 1998-03-20 2000-10-23 Gea Farmaceutisk Fabrik As Farmaceutisk formulering omfattende en 2-[[(2-pyridinyl)methyl]sulfinyl]benzimidazol med anti-ulcusaktivitet samt fremgangs
FR2795726A1 (fr) 1999-06-30 2001-01-05 Aventis Cropscience Sa Nouveaux pyrazoles fongicides
GB9925127D0 (en) 1999-10-22 1999-12-22 Pharmacia & Upjohn Spa Oral formulations for anti-tumor compounds
AU2002363250A1 (en) 2001-11-01 2003-05-12 Icagen, Inc. Pyrazole-amides and-sulfonamides
EP1622571A4 (en) * 2003-04-30 2012-05-02 Agensys Inc NUCLEIC ACIDS AND CORRESPONDING PROTEINS NAMED 109P1D4 FOR THE TREATMENT AND DETECTION OF CANCER
EP1847531A4 (en) 2005-02-09 2009-04-22 Takeda Pharmaceutical PYRAZOLE DERIVATIVE
CN100526430C (zh) 2005-10-19 2009-08-12 中国石油化工股份有限公司 一种生产清洁汽油的方法
TW200738682A (en) * 2005-12-08 2007-10-16 Organon Nv Isoquinoline derivatives
KR20090007347A (ko) 2006-03-22 2009-01-16 버텍스 파마슈티칼스 인코포레이티드 증식성 장애의 치료를 위한 c-MET 단백질 키나제 억제제
US20090253673A1 (en) 2006-07-12 2009-10-08 Min Ge Substituted Pyrazoles as Ghrelin Receptor Antagonists
CN101583601B (zh) 2007-01-17 2013-06-05 香港科技大学 作为褪黑素受体mt1和mt2的亚型选择性激动剂的异喹诺酮化合物
US8153798B2 (en) 2007-03-09 2012-04-10 High Point Pharmaceuticals, Llc Indole- and benzimidazole amides as hydroxysteroid dehydrogenase inhibitors
CN101366715A (zh) 2007-08-15 2009-02-18 上海医药工业研究院 一种雷帕霉素组合物及其制备方法
EP2222326B2 (en) 2007-11-21 2015-02-25 Vib Vzw Inhibitors of malt1 proteolytic activity and uses thereof
TWI607996B (zh) 2008-09-24 2017-12-11 巴地斯顏料化工廠 控制無脊椎害蟲之吡唑化合物
WO2010039039A1 (en) 2008-10-03 2010-04-08 Clavis Pharma Asa Oral formulations of gemcitabine derivatives
KR101061599B1 (ko) 2008-12-05 2011-09-02 한국과학기술연구원 비정상 세포 성장 질환의 치료를 위한 단백질 키나아제 저해제인 신규 인다졸 유도체, 이의 약학적으로 허용가능한염 및 이를 유효성분으로 함유하는 약학적 조성물
DE102009003954A1 (de) 2009-01-07 2010-07-08 Merck Patent Gmbh Pyridazinonderivate
US8252821B2 (en) 2009-04-14 2012-08-28 Bristol-Myers Squibb Company Bioavailable capsule compositions of amorphous alpha-(N-sulfonamido)acetamide compound
WO2011036885A1 (ja) 2009-09-25 2011-03-31 武田薬品工業株式会社 複素環化合物
MX380504B (es) 2010-06-03 2025-03-12 Pharmacyclics Llc El uso de inhibidores de la tirosina quinasa de bruton (btk).
US20120071497A1 (en) 2010-06-03 2012-03-22 Pharmacyclics, Inc. Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase
WO2011161612A1 (en) 2010-06-22 2011-12-29 Basf Se Process for preparing 4-hydroxypyridines
WO2012004217A1 (en) 2010-07-06 2012-01-12 Novartis Ag Cyclic ether compounds useful as kinase inhibitors
TW201236685A (en) 2010-11-11 2012-09-16 Daiichi Sankyo Co Ltd New pyrazole amide derivatives
JP6231085B2 (ja) 2012-05-31 2017-11-15 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト アミノキナゾリン誘導体及びピリドピリミジン誘導体
WO2014033447A2 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
EA201590916A1 (ru) 2012-11-09 2016-02-29 Корнэлл Юниверсити Низкомолекулярные ингибиторы malt1
WO2014086478A1 (en) 2012-12-03 2014-06-12 Helmholtz Zentrum München - Deutsches Forschungszentrum für Gesundheit und Umwelt (GmbH) Inhibitors of malt1 protease
MX2015008919A (es) 2013-01-10 2015-10-22 Gruenenthal Gmbh Carboxamidas basadas en pirazolilo i como inhibidores del canal de calcio activado por liberacion de calcio (crac).
WO2015192081A1 (en) 2014-06-13 2015-12-17 Byrd, John C. Biomarker for predicting response of cll to treatment with a btk inhibitor
WO2016005994A2 (en) 2014-07-06 2016-01-14 Gattefosse India Pvt. Ltd. Pharmaceutical composition comprising solid dispersion of bcs class ii drugs with gelucires
MX2017001656A (es) 2014-08-08 2017-07-24 Pharmacyclics Llc Combinaciones de inhibidor de tirosina cinasa de bruton y usos de estas.
BR112017004897A2 (pt) 2014-09-10 2017-12-12 Glaxosmithkline Ip Dev Ltd compostos inovadores como inibidores rearranjados durante a transfecção (ret)
WO2016090382A1 (en) 2014-12-06 2016-06-09 Intra-Cellular Therapies, Inc. Organic compounds
US10835524B2 (en) 2015-06-24 2020-11-17 University Of Florida Research Foundation, Incorporated Compositions for the treatment of pancreatic cancer and uses thereof
RS63359B1 (sr) 2015-11-06 2022-07-29 Incyte Corp Heterociklična jedinjenja kao inhibitori pi3k-gama
EP3374361A1 (en) * 2015-11-13 2018-09-19 Novartis AG Novel pyrazolo pyrimidine derivatives
JO3794B1 (ar) 2015-12-10 2021-01-31 Janssen Pharmaceutica Nv المركبات متعددة الحلقات كمثبطات لتيروزين كيناز بروتون
CN107021963A (zh) 2016-01-29 2017-08-08 北京诺诚健华医药科技有限公司 吡唑稠环类衍生物、其制备方法及其在治疗癌症、炎症和免疫性疾病上的应用
WO2017151786A1 (en) 2016-03-01 2017-09-08 University Of Maryland, Baltimore Wnt signaling pathway inhibitors for treatments of disease
WO2018020474A1 (en) 2016-07-29 2018-02-01 Lupin Limited Substituted thiazolo-pyridine compounds as malt1 inhibitors
WO2018103060A1 (en) 2016-12-09 2018-06-14 Janssen Pharmaceutica Nv Inhibitors of bruton's tyrosine kinase and methods of their use
ES2856248T3 (es) 2016-12-21 2021-09-27 Acerta Pharma Bv Inhibidores de imidazopirazina de la tirosina quinasa de Bruton
JOP20190141A1 (ar) 2016-12-21 2019-06-12 Bayer Pharma AG أشكال جرعات صيدلية تحتوي على مثبطات لقناة task-1 و task-3 واستخدامها في معالجة اضطراب تنفسي
TWI795381B (zh) 2016-12-21 2023-03-11 比利時商健生藥品公司 作為malt1抑制劑之吡唑衍生物
AU2017381433B2 (en) 2016-12-21 2024-11-14 Mereo Biopharma 3 Limited Use of anti-sclerostin antibodies in the treatment of osteogenesis imperfecta
JOP20190152A1 (ar) 2016-12-21 2019-06-20 Novartis Ag مضادات الميوستاتين، الآكتيفين أو مستقبلات الآكتيفين للاستخدام في علاج السمنة والحالات ذات الصلة
JOP20190148A1 (ar) 2016-12-21 2019-06-18 Bayer Pharma AG أشكال جرعات صيدلية تحتوي على مثبطات قنوات task-1 و task-3 واستخدامها لمعالجة الاضطرابات التنفسية
EP3576744A1 (en) 2017-02-01 2019-12-11 Medivir Aktiebolag Therapeutic applications of malt1 inhibitors
EP3592731A4 (en) 2017-03-08 2020-10-07 Cornell University MALT1 INHIBITORS AND THEIR USES
WO2018226150A1 (en) 2017-06-05 2018-12-13 Medivir Aktiebolag Pyrazolopyrimidine as malt-1 inhibitors
KR20200105678A (ko) 2017-12-28 2020-09-08 더 제너럴 하스피탈 코포레이션 Cbm 시그날로좀 복합체 표적화는 조절 t 세포의 종양 미세환경에 대한 염증유발을 유도함
EP3756268A1 (de) 2018-02-23 2020-12-30 Industrieanlagen-Betriebsgesellschaft mbH Vorrichtung zum erzeugen eines magnetfelds, insbesondere für ein induktives ladesystem, und primäreinrichtung eines induktiven ladesystems zum dynamischen aufladen von fahrzeugen
EA202190055A1 (ru) 2018-06-18 2021-04-23 Янссен Фармацевтика Нв Производные пиразола в качестве ингибиторов malt1
AU2019289223B2 (en) 2018-06-18 2023-09-21 Janssen Pharmaceutica Nv Pyrazole derivatives as MALT1 inhibitors
BR112021016400A2 (pt) 2019-02-22 2021-10-13 Janssen Pharmaceutica N.V. Forma cristalina de mono-hidrato de 1-(1-oxo-1,2-di-hidroisoquinolin-5-il)-5-(trifluorometil.)-n-(2-(trifluorometil)piridin-4-il)-1h-pirazol-4-carboxamida
EP3927324A1 (en) 2019-02-22 2021-12-29 Janssen Pharmaceutica NV Pharmaceutical formulations
US12404260B2 (en) 2019-04-11 2025-09-02 Janssen Pharmaceutica Nv Pyridine rings containing derivatives as MALT1 inhibitors
CA3162140A1 (en) 2019-11-22 2021-05-27 Janssen Pharmaceutica Nv Methods for assessing efficacy of malt1 inhibitors using an nf-kb translocation assay
KR20220119037A (ko) 2019-11-22 2022-08-26 얀센 파마슈티카 엔.브이. MALT1 억제제의 효능 평가를 위한 NF-kB 조절 유전자 발현 분석
WO2021138298A1 (en) 2019-12-30 2021-07-08 Rheos Medicines, Inc. Malt1 modulators and uses thereof
JP2023539729A (ja) 2020-08-21 2023-09-19 ヤンセン ファーマシューティカ エヌ.ベー. Malt1阻害剤の非晶質形態及びその製剤
EP4199911A1 (en) 2020-08-21 2023-06-28 JANSSEN Pharmaceutica NV Pharmaceutical formulations comprising a malt1 inhibitor and a mixture of polyethylene glycol with a fatty acid
KR20230154227A (ko) 2021-03-03 2023-11-07 얀센 파마슈티카 엔브이 치료적 유효 용량의 malt1 억제제 jnj-67856633(1-(1-옥소-1,2-다이하이드로아이소퀴놀린-5-일)-5-(트라이플루오로메틸)-n-(2-(트라이플루오로메틸)피리딘-4-일)-1h-피라졸-4-카르복스아미드)을 사용하는 병태의 치료 방법
EP4301365A1 (en) 2021-03-03 2024-01-10 Janssen Pharmaceutica NV Combination therapy using a malt1 inhibitor and a btk inhibitor

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004098518A2 (en) 2003-05-01 2004-11-18 Bristol-Myers Squibb Company Pyrazole-amide compounds useful as kinase inhibitors
JP2015096499A (ja) 2013-10-11 2015-05-21 田辺三菱製薬株式会社 医薬組成物
WO2015181747A1 (en) 2014-05-28 2015-12-03 Novartis Ag Novel pyrazolo pyrimidine derivatives and their use as malt1 inhibitors

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
MAUGER, Christelle,Adv.Synth.Catal.,2005年,347,773-782
STN International,CAS Registry No. 1907028-26-5,DATABASE REGISTRY [online], Retrieved from STN,Entered STN:,2016年05月10日
STN International,CAS Registry No. 1907875-04-0,DATABASE REGISTRY [online], Retrieved from STN,Entered STN,2016年05月11日
STN International,CAS Registry No.1898933-19-1,DATABASE REGISTRY [online], Retrieved from STN,Entered STN:,2016年04月27日

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